[1,2,4]triazolo[1,5-c]quinazolin-5-amines
[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds inhibit AHR, addressing dysregulated immune responses and tumour growth in cancers, providing a therapeutic approach for treating various tumours and metastases.
Patent Information
- Authority / Receiving Office
- AU · AU
- Patent Type
- Applications
- Current Assignee / Owner
- DEUTES KREBSFORSCHUNGSZENT STIFTUNG DES OFFENTLICHEN RECHTS
- Filing Date
- 2020-08-10
- Publication Date
- 2026-07-09
AI Technical Summary
Current technologies do not effectively inhibit the Aryl Hydrocarbon Receptor (AHR) to treat or prevent conditions characterized by dysregulated immune responses, uncontrolled cell growth, and tumour growth, particularly in various types of cancers and metastases, which are mediated by AHR activation.
Development of [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds that specifically inhibit AHR activity, potentially in combination with other anti-cancer medications.
The compounds effectively inhibit AHR, offering therapeutic potential for treating or preventing cancers and conditions with dysregulated immune responses, including solid and liquid tumours, and their metastases, by modulating immune responses and inhibiting tumour growth.
Abstract
Description
The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses, as a sole agent or in combination with other active ingredients. BACKGROUND The AHR (Aryl Hydrocarbon Receptor) is a ligand-activated transcription factor, belonging to the basic helix-loop-helix / Per-Arnt-Sim (bHLH / PAS) family, and is located in the cytosol. Upon ligand binding, the AHR translocates to the nucleus where it heterodimerises with ARNT (AHR Nuclear Translocator) upon which it interacts with DREs (Dioxin Response Elements) of AHR-responsive genes to regulate their transcription. The AHR is best known for binding to environmental toxins and inducing the metabolic machinery, such as cytochrome P 450 enzymes (eg. CYP1A1, CYP1A2 and CYP1B1), required for their elimination (Reyes et al., Science, 1992, 256(5060):1193-5). Activation of AHR by xenobiotics has demonstrated its role in numerous cellular processes such as embryogenesis, tumourigenesis and inflammation. AHR is expressed in many cells of the immune system, including dendritic cells (DCs), macrophages, T cells and NK cells, and plays an important role in immunoregulation (Nguyen et al., Front Immunol, 2014, 5:551). The classic exogenous AHR ligands TCDD and 3-methylcholanthrene, for example, are known to induce profound immunosuppression, promote carcinogenesis and induce tumour growth (Gramatzki et al., Oncogene, 2009, 28(28):2593-605; Bui et al., Oncogene, 2009, 28(41):3642-51; Esser et al., Trends Immunol, 2009, 30:447-454). In the context of immunosuppression, AHR activation promotes regulatory T cell generation, inhibits Th1 and Th 17 differentiation, directly and indirectly, and decreases the activation and maturation of DCs (Wang et al., Clin Exp Immunol, 2014, 177(2):521-30; Mezrich et al., J Immunol, 2010, 185(6): 3190-8; Wei etal., Lab Invest, 2014, 94(5):528-35; Nguyen etal., PNAS, 2010,107(46):19961-6). AHR activation modulates the innate immune response and constitutive AHR expression has been shown to negatively regulate the type-l interferon response to viral infection (Yamada et al., Nat Immunol, 2016). Additionally, mice with a constitutively active AHR spontaneously develop tumours (Andersson et al., PNAS, 2002, 99(15):9990-5). In addition to xenobiotics, the AHR can also bind metabolic products of tryptophan degradation. Tryptophan metabolites, such as kynurenine and kynurenic acid, are endogenous AHR ligands that activate the AHR under physiological conditions (DiNatale et al., Toxicol Sci, 2010, 115(1):89-97; Mezrich et al., J Immunol, 2010, 185(6):3190-8; Opitz et al., Nature, 2011, 478(7368):197-203). Other endogenous ligands are known to bind the AHR although their physiological roles are currently unknown (Nguyen & Bradfield, Chern Res Toxicol, 2008, 21(1):102-116). The immunosuppressive properties of kynurenine and tryptophan degradation are well described and are implicated in cancer-associated immunosuppression. The enzymes indoleamine-2,3-dioxygenases 1 and 2 (IDO1 / IDO2) as well as tryptophan-2,3-dioxygenase 2 (TDO2) are responsible for catalysing the first and rate-limiting step of tryptophan metabolism. IDO1 / 2-mediated degradation of tryptophan in tumours and tumour-draining lymph nodes reduces anti-tumour immune responses and inhibition of IDO can suppress tumour formation in animal models (Uyttenhove et al., Nat Med, 2003, 9(10):1269-74 ; Liu et al., Blood, 2005, 115(17): 3520-30; Muller et al., Nat Med, 11(3):312-9; Metz, Cancer Res, 2007, 67(15):7082-7). TDO2 is also strongly expressed in cancer and can lead to the production of immunosuppressive kynurenine. In glioma, activation of the AHR by kynurenine, downstream of TDO-mediated tryptophan degradation, enhances tumour growth as a consequence of inhibiting anti-tumour immune responses as well as directly promoting tumour cell survival and motility (Opitz et al., Nature, 2011,478(7368):197-203). AHR ligands generated by tumour cells therefore act in both an autocrine and paracrine fashion on tumour cells and lymphocytes, respectively, to promote tumour growth. The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) which inhibit the AHR. State of the Art WO 2010 / 059401 relates to compounds and compositions for expanding the number of CD34+ cells for transplantation. In particular, WO 2010 / 059401 relates inter alia to heterocyclic compounds capable of down-regulating the activity and / or expression of AHR. WO 2012 / 015914 relates to compositions and methods for modulating AHR activity. In particular, WO 2012 / 015914 relates inter alia to heterocyclic compounds that modulate AHR activity for use in therapeutic compositions. WO 2007040565 relates to the use of [1,2,4]triazolo[1,5-c]pyrimidin-5-amine derivatives as adenosine receptor antagonists. US 6358964 relates to [1,2,4]triazolo[1,5-c]quinazolin-5-amine derivatives useful as potent modulators of the adenosine A3 receptor. However, the state of the art does not describe the [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) of the present invention as described and defined herein. It has now been found, and this constitutes the basis of the present invention, that the compounds of the present invention have surprising and advantageous properties. In particular, the compounds of the present invention have surprisingly been found to effectively inhibit AHR for which data are given in biological experimental section and may therefore be used for the treatment or prophylaxis of cancer or other conditions where exogenous and endogenous AHR ligands induce dysregulated immune responses, uncontrolled cell growth, proliferation and / or survival of tumour cells, immunosuppression in the context of cancer, inappropriate cellular immune responses, or inappropriate cellular inflammatory responses or diseases which are accompanied with uncontrolled cell growth, proliferation and / or survival of tumour cells, immunosuppression in the context of cancer inappropriate cellular immune responses, or inappropriate cellular inflammatory responses, particularly in which the uncontrolled cell growth, proliferation and / or survival of tumour cells, immunosuppression in the context of cancer, inappropriate cellular immune responses, or inappropriate cellular inflammatory responses is mediated by AHR, such as, for example, liquid and solid tumours, and / or metastases thereof, e.g. head and neck tumours including brain tumours and brain metastases, tumours of the thorax including non-small cell and small cell lung tumours, gastrointestinal tumours including colon, colorectal and pancreatic tumours, liver tumours, endocrine tumours, mammary and other gynecological tumours, urological tumours including renal, bladder and prostate tumours, skin tumours, and sarcomas, and / or metastases thereof. DESCRIPTION of the INVENTION In accordance with a first aspect, the present invention covers compounds of general formula (I): in which R1 represents phenyl or heteroaryl, optionally substituted one to three times, independently from each other, with halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, C1-C4-hydroxyalkyl, Ci-C4-alkoxy-Ci-C4-alkyl-, Cs-Ce-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, Cs-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl, -NR9R10, R9R10N-Ci-C4-alkyl-, Ci-C3-alkyl-S(O)m- or Ci-C3-alkyl-SO(NH)-; R2 represents hydrogen, Ci-C4-alkyl, Ci-C4-haloalkyl or Cs-Ce-cycloalkyl; R3 represents hydrogen, Ci-Ce-alkyl, phenyl or phenyl-Ci-C3-alkyl, wherein said Ci-Ce-alkyl group is optionally substituted, one or more times, independently from each other, with hydroxy, halogen, Ci-C4-alkoxy, -S(O)n-Ci-C4-alkyl, phenyl-Ci-C3-alkoxy or -NR9R10 and said phenyl groups are optionally substituted, one or more times, independently from each other, with hydroxy, halogen, cyano, Ci-C3-alkyl, Ci-C3-haloalkyl, Ci-C3-alkoxy or Ci-C3-haloalkoxy, or R2 and R3 together with the carbon atom to which they are attached form a 3- to 6-membered ring, said ring optionally containing one heteroatom selected from O, S, NH, NRa in which Ra represents a Ci-C4-alkyl group; R4 represents hydroxy, Ci-C4-alkoxy or -NR11R12, or R2 and R4 together represent *-C2-Cs-alkanediyl-X1-**, *-Ci-C2-alkanediyl-X2-Ci-C3-alkanediyl-** or *-Ci-C2-alkanediyl-X2-C2-C3-alkanediyl-X1-** to form a 5- to 9-membered ring, wherein * indicates the point of attachment of said group for R2 and ** indicates the point of attachment of said group for R4; R5 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, 4- to 6-membered heterocycloalkyl, -CO2-Ci-C4-alkyl, -CO-NR9R10 or-NR9R10; R6 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R7 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R8 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, 1-R15-Cs-Ce-cycloalkyl, -CO2-Ci-C4-alkyl, -CO-NR9R10, -NR9R10, Ci-C4-hydroxyalkyl, Ci-C4-alkoxy-Ci-C4-alkyl-, Ci-C4-alkyl-S-, Ci-C4-alkyl-S-Ci-C4-alkyl-, -S(=O)R’, -S(=O)2R’, -S(=O)2NH2, -S(=O)2NHR’, -S(=O)2N(R’)R”, -S(=O)(=NH)R’, 4- to 6-membered heterocycloalkyl, or-OR16; R9 and R10 are the same or different and represent, independently from each other, hydrogen, Ci-Cs-alkyl or tert-butoxycarbonyl, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRa in which Ra represents Ci-C4-alkyl or C1-C4-alkoxycarbonyl; R11 and R12 are the same or different and represent, independently from each other, hydrogen, Ci-C4-alkyl, C2-C4-hydroxyalkyl, Ci-C4-alkoxy-C2-C4-alkyl-, R9R10N-C2-C4-alkyl-, Cs-Ce-cycloalkyl, 4- to 7-membered heterocycloalkyl, said 4- to 7-membered heterocycloalkyl group is optionally substituted, one or two times, independently from each other, with hydroxy, oxo, halogen, Ci-C4-alkyl, Ci-C4-alkoxy, or-NR9R10, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRa in which Ra represents Ci-C4-alkyl or C1-C4-alkoxycarbonyl and is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, Ci-C4-alkyl, Ci-C4-alkoxy, or-NR9R10, or together with the nitrogen atom to which they are attached form a heterospirocycloalkyl group, which is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, Ci-C4-alkyl, Ci-C4-alkoxy, or-NR9R10, or together with the nitrogen atom to which they are attached form a bridged heterocycloalkyl group, which is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, Ci-C4-alkyl, Ci-C4-alkoxy, or-NR9R10; R13 represents hydrogen, Ci-C4-alkyl, benzyl, 4-methoxybenzyl or tert-butoxycarbonyl; WO 2021 / 028382 PCT / EP2020 / 072377 R14 represents hydrogen, Ci-C4-alkyl, benzyl or 4-methoxybenzyl; R15 represents Ci-Cs-alkyl or Ci-Cs-haloalkyl; R16 represents C2-Ce-hydroxyalkyl, Ci-C4-alkoxy-C2-Ce-alkyl-, or Cs-Ce-cycloalkyl; R’ and R” represent, independently from each other, Ci-Ce-alkyl, Ci-Ce-haloalkyl, or Cs-Ce-cycloalkyl; X1 represents O, S(O)m, or NR13; X2 represents O, S(O)m, or NR14; m represents 0, 1 or 2; n represents 0, 1 or 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. Further, it covers their use in combination with other anti cancer medications such as immunotherapeutics, targeted anti cancer agents or chemotherapy. DEFINITIONS The term “substituted” means that one or more hydrogen atoms on the designated atom or group are replaced with a selection from the indicated group, provided that the designated atom's normal valency under the existing circumstances is not exceeded. Combinations of substituents and / or variables are permissible. The term “optionally substituted” means that the number of substituents can be equal to or different from zero. Unless otherwise indicated, it is possible that optionally substituted groups are substituted with as many optional substituents as can be accommodated by replacing a hydrogen atom with a non-hydrogen substituent on any available carbon atom. Commonly, it is possible for the number of optional substituents, when present, to be 1, 2 or 3. The term “comprising” when used in the specification includes “consisting of’. If within the present text any item is referred to as “as mentioned herein”, it means that it may be mentioned anywhere in the present text. The terms as mentioned in the present text have the following meanings: The term “halogen” means a fluorine, chlorine, bromine or iodine, particularly a fluorine, chlorine or bromine atom. The term “Ci-Ce-alkyl” means a linear or branched, saturated, monovalent hydrocarbon group having 1, 2, 3, 4, 5 or 6 carbon atoms, e.g. a methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl, tert-butyl, pentyl, isopentyl, 2-methylbutyl, 1-methylbutyl, 1-ethylpropyl, 1,2-dimethylpropyl, neo-pentyl, 1,1-dimethylpropyl, hexyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1-ethylbutyl, 2-ethylbutyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 3,3-dimethylbutyl, 2,3-dimethylbutyl, 1,2-dimethylbutyl or 1,3-dimethylbutyl group, or an isomer thereof. Particularly, said group has 1,2, 3 or 4 carbon atoms (“Ci-C4-alkyl”), e.g. a methyl, ethyl, propyl, isopropyl, butyl, sec-butyl isobutyl, or tert-butyl group, more particularly 1, 2 or 3 carbon atoms (“Ci-Cs-alkyl”), e.g. a methyl, ethyl, n-propyl or isopropyl group. The term “Ci-Ce-haloalkyl” means a linear or branched, saturated, monovalent hydrocarbon group in which the term “Ci-Ce-alkyl” is as defined supra, and in which one or more of the hydrogen atoms are replaced, identically or differently, with a halogen atom. Particularly, said halogen atom is a fluorine atom. Said Ci-Ce-haloalkyl group is, for example, fluoromethyl, difluoromethyl, trifluoromethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl or 1,3-difluoropropan-2-yl. The term “Ci-C4-hydroxyalkyl” means a linear or branched, saturated, monovalent hydrocarbon group in which the term “Ci-C4-alkyl” is defined supra, and in which 1 or 2 hydrogen atoms are replaced with a hydroxy group, e.g. a hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-di-hydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxypropan-2-yl, 2-hydroxypropan-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxypropan-2-yl, 3-hydroxy-2-methyl-propyl, 2-hydroxy-2-methyl-propyl or 1-hydroxy-2-methyl-propyl group. The term “Ci-C4-alkoxy” means a linear or branched, saturated, monovalent group of formula (Ci-C4-alkyl)-O-, which means methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, sec-butoxy, isobutoxy or tert-butoxy. The term “Ci-C4-haloalkoxy” means a linear or branched, saturated, monovalent Ci-C4-alkoxy group, as defined supra, in which one or more of the hydrogen atoms is replaced, identically or differently, with a halogen atom. Particularly, said halogen atom is a fluorine atom. Said Ci-C4-haloalkoxy group is, for example, fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy or pentafluoroethoxy. The term “Ci-Cs-alkanediyl” means a bivalent saturated aliphatic radical regarded as derived from an Ci-Cs-alkane by removal of a hydrogen atom from each of the two terminal carbon atoms of the chain, e.g. a methylene, ethylene, propylene, trimethylene, tetramethylene or pentamethylene. The term “Cs-Ce-cycloalkyl” means a saturated, monovalent, monocyclic hydrocarbon ring which contains 3, 4, 5 or 6 carbon atoms (“Cs-Ce-cycloalkyl”). Said Cs-Ce-cycloalkyl group is a monocyclic hydrocarbon ring, e.g. a cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl. The term “4- to 7-membered heterocycloalkyl” means a monocyclic, saturated heterocycle with 4, 5, 6 or 7 ring atoms in total, which contains one or two identical or different heteroatomcontaining groups selected from the group consisting of-NRb-, -O-, -S-, -SO-, -SO2-, -SO2-NRb- , -SO(=NRb)-, wherein Rb means a hydrogen atom or a Ci-Cs-alkyl group. It being possible for said heterocycloalkyl group to be attached to the rest of the molecule via any one of the carbon atoms or, if present, a nitrogen atom. Said heterocycloalkyl group, without being limited thereto, can be a 4-membered ring, such as azetidinyl, oxetanyl or thietanyl, for example; or a 5-membered ring, such as tetrahydrofuranyl, 1,3-dioxolanyl, thiolanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, 1,1 -dioxidothiolanyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl or 1,3-thiazolidinyl, tetrahydrothiophene 1-oxide, 1,2-thiazolidine 1-oxide, 1,3-thiazolidine 1-oxide, tetrahydrothiophene 1,1-dioxide, 1,2-thiazolidine 1,1-dioxide, 1,3-thiazolidine 1,1-dioxide, 1,2,5-thiadiazolidine 1,1-dioxide, 1,2,4-thiadiazolidine 1,1-dioxide, 1,2,3-thiadiazolidine 1,1-dioxide, tetrahydro-1H-1A4-thiophen-1-imine 1-oxide, 1 A4,2-thiazolidin-1-imine 1-oxide or 1 A4,3-thiazolidin-1-imine 1-oxide, for example; or a 6-membered ring, such as tetrahydropyranyl, tetrahydrothiopyranyl, piperidinyl, morpholinyl, dithianyl, thiomorpholinyl, piperazinyl, 1,3-dioxanyl, 1,4-dioxanyl or 1,2-oxazinanyl, tetrahydro-2H-thiopyran 1-oxide, 1,2-thiazinane 1-oxide, 1,3-thiazinane 1-oxide, thiomorpholine 1-oxide, tetrahydro-2H-thiopyran 1,1-dioxide, 1,2-thiazinane 1,1-dioxide, 1,3-thiazinane 1,1-dioxide, thiomorpholine 1,1-dioxide, 1,2,6-thiadiazinane 1,1-dioxide, 1,2,5-thiadiazinane 1,1-dioxide, 1,2,4-thiadiazinane 1,1-dioxide, 1,2,3-thiadiazinane 1,1-dioxide, hexahydro- 1A4-thiopyran-1 -imine 1-oxide, 1A4,2-thiazinan-1-imine 1-oxide, 1A4,3-thiazinan-1-imine 1-oxide or 1A4-thiomorpholin-1-imine 1-oxide, or a 7-membered ring, such as azepanyl, 1,4-diazepanyl, 1,4-oxazepanyl, 1,4-thiazepanyl, or 1-imino-1A6,4-thiazepane-1-oxid, for example. The term “heterospirocycloalkyl” means a bicyclic, saturated heterocycle with 6, 7, 8, 9, 10 or 11 ring atoms in total, in which the two rings share one common ring carbon atom, which “heterospirocycloalkyl” contains one or two identical or different ring heteroatoms from the series: N, O, S; it being possible for said heterospirocycloalkyl group to be attached to the rest of the molecule via any one of the carbon atoms, except the spiro carbon atom, or, if present, a nitrogen atom. Said heterospirocycloalkyl group is, for example, azaspiro[2.3]hexyl, azaspiro[3.3]heptyl, oxaazaspiro[3.3]heptyl, thiaazaspiro[3.3]heptyl, oxaspiro[3.3]heptyl, oxazaspiro[5.3]nonyl, oxazaspiro[4.3]octyl, azaspiro[4,5]decyl, oxazaspiro [5.5]undecyl, diazaspiro[3.3]heptyl, thiazaspiro[3.3]heptyl, thiazaspiro[4.3]octyl, azaspiro[5.5]undecyl, or one of the further homologous scaffolds such as spiro[3.4]-, spiro[4.4]-, spiro[2.4]-, spiro[2.5]-, spiro[2.6]-, spiro[3.5]-, spiro[3.6]-, spiro[4.5]- and spiro[4.6]-. The term “bridged heterocycloalkyl” means a bicyclic, saturated heterocycle with 7, 8, 9 or 10 ring atoms in total, in which the two rings share two common ring atoms which are not adjacent, which “bridged heterocycloalkyl” contains one or two identical or different ring heteroatoms from the series: N, O, S; it being possible for said bridged heterocycloalkyl group to be attached to the rest of the molecule via any one of the carbon atoms or, if present, a nitrogen atom. Said bridged heterocycloalkyl group is, for example, azabicyclo[2.2.1]heptyl, oxazabicyclo[2.2.1]heptyl, thiazabicyclo[2.2.1]heptyl, diazabicyclo[2.2.1]heptyl, azabicyclo-[2.2.2]octyl, diazabicyclo[2.2.2]octyl, oxazabicyclo[2.2.2]octyl, thiazabicyclo[2.2.2]octyl, azabi-cyclo[3.2.1]octyl, diazabicyclo[3.2.1]octyl, oxazabicyclo[3.2.1]octyl, thiazabicyclo[3.2.1]octyl, azabicyclo[3.3.1]nonyl, diazabicyclo[3.3.1]nonyl, oxazabicyclo[3.3.1]nonyl, thiazabicyclo[3.3.1]-nonyl, azabicyclo[4.2.1]nonyl, diazabicyclo[4.2.1]nonyl, oxazabicyclo[4.2.1]nonyl, thiaza-bicyclo[4.2.1]nonyl, azabicyclo[3.3.2]decyl, diazabicyclo[3.3.2]decyl, oxazabicyclo[3.3.2]decyl, thiazabicyclo[3.3.2]decyl or azabicyclo[4.2.2]decyl. The term “heteroaryl” means a monovalent, monocyclic, bicyclic or tricyclic aromatic ring having 5, 6, 8, 9, 10, 11, 12, 13 or 14 ring atoms (a “5- to 14-membered heteroaryl” group), particularly 5, 6, 9 or 10 ring atoms, which contains at least one ring heteroatom and optionally one, two or three further ring heteroatoms from the series: N, O and / or S, and which is bound via a ring carbon atom or optionally via a ring nitrogen atom (if allowed by valency). Said heteroaryl group can be a 5-membered heteroaryl group, such as, for example, thienyl, furanyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl or tetrazolyl; or a 6-membered heteroaryl group, such as, for example, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl or triazinyl; or a tricyclic heteroaryl group, such as, for example, carbazolyl, acridinyl or phenazinyl; or a 9-membered heteroaryl group, such as, for example, benzofuranyl, benzothienyl, benzoxazolyl, benzisoxazolyl, benzimidazolyl, benzothiazolyl, benzotriazolyl, indazolyl, indolyl, isoindolyl, indolizinyl or purinyl; or a 10membered heteroaryl group, such as, for example, quinolinyl, quinazolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinoxalinyl or pteridinyl. The term “monocyclic heteroaryl” means a monovalent, aromatic ring having 5 or 6 ring atoms (a “5- or 6-membered heteroaryl” group), which contains at least one ring heteroatom and optionally one or two further ring heteroatoms from the series: N, O and / or S, and which is bound via a ring carbon atom or optionally via a ring nitrogen atom (if allowed by valency). Said heteroaryl group can be a 5-membered heteroaryl group, such as, for example, thienyl, furanyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl or tetrazolyl; or a 6-membered heteroaryl group, such as, for example, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl or triazinyl. In general, and unless otherwise mentioned, the heteroaryl or heteroarylene groups include all possible isomeric forms thereof, e.g:. tautomers and positional isomers with respect to the point of linkage to the rest of the molecule. Thus, for some illustrative non-restricting examples, the term pyridinyl includes pyridin-2-yl, pyridin-3-yl and pyridin-4-yl; or the term thienyl includes thien-2-yl and thien-3-yl. Where the plural form of the word compounds, salts, polymorphs, hydrates, solvates and the like, is used herein, this is taken to mean also a single compound, salt, polymorph, isomer, hydrate, solvate or the like. By "stable compound' or "stable structure" is meant a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent. The compounds of the present invention optionally contain one or more asymmetric centres, depending upon the location and nature of the various substituents desired. It is possible that one or more asymmetric carbon atoms are present in the (R) or (S) configuration, which can result in racemic mixtures in the case of a single asymmetric centre, and in diastereomeric mixtures in the case of multiple asymmetric centres. In certain instances, it is possible that asymmetry also be present due to restricted rotation about a given bond, for example, the central bond adjoining two substituted aromatic rings of the specified compounds. Further, it is possible for compounds of the present invention to exist as tautomers. For example, any compound which contains a [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one moiety for example can exist as a keto tautomer, or an enol tautomer, or even a mixture in any amount of the two tautomers, namely: enol tautomer keto tautomer [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one [1,2,4]triazolo[1,5-c]quinazolin-5-ol The present invention includes all possible tautomers of the compounds of the present invention as single tautomers, or as any mixture of said tautomers, in any ratio. Preferred compounds are those which produce the more desirable biological activity. Separated, pure or partially purified isomers and stereoisomers or racemic or diastereomeric mixtures of the compounds of the present invention are also included within the scope of the present invention. The purification and the separation of such materials can be accomplished by standard techniques known in the art. Preferred isomers are those which produce the more desirable biological activity. These separated, pure or partially purified isomers or racemic mixtures of the compounds of this invention are also included within the scope of the present invention. The purification and the separation of such materials can be accomplished by standard techniques known in the art. The optical isomers can be obtained by resolution of the racemic mixtures according to conventional processes, for example, by the formation of diastereoisomeric salts using an optically active acid or base or formation of covalent diastereomers. Examples of appropriate acids are tartaric, diacetyltartaric, ditoluoyltartaric and camphorsulfonic acid. Mixtures of diastereoisomers can be separated into their individual diastereomers on the basis of their physical and / or chemical differences by methods known in the art, for example, by chromatography or fractional crystallisation. The optically active bases or acids are then liberated from the separated diastereomeric salts. A different process for separation of optical isomers involves the use of chiral chromatography (e.g., HPLC columns using a chiral phase), with or without conventional derivatisation, optimally chosen to maximise the separation of the enantiomers. Suitable HPLC columns using a chiral phase are commercially available, such as those manufactured by Daicel, e.g., Chiracel OD and Chiracel OJ, for example, among many others, which are all routinely selectable. Enzymatic separations, with or without derivatisation, are also useful. The optically active compounds of the present invention can likewise be obtained by chiral syntheses utilizing optically active starting materials. In order to distinguish different types of isomers from each other reference is made to III PAC Rules Section E (Pure Appl Chern 45, 11-30, 1976). The present invention includes all possible stereoisomers of the compounds of the present invention as single stereoisomers, or as any mixture of said stereoisomers, e.g. (R)- or (S)-isomers, in any ratio. Isolation of a single stereoisomer, e.g. a single enantiomer or a single diastereomer, of a compound of the present invention is achieved by any suitable state of the art method, such as chromatography, especially chiral chromatography, for example. Further, the compounds of the present invention can exist as N-oxides, which are defined in that at least one nitrogen of the compounds of the present invention is oxidised. The present invention includes all such possible N-oxides. The present invention also covers useful forms of the compounds of the present invention, such as metabolites, hydrates, solvates, prodrugs, salts, in particular pharmaceutically acceptable salts, and / or co-precipitates. The compounds of the present invention can exist as a hydrate, or as a solvate, wherein the compounds of the present invention contain polar solvents, in particular water, methanol or ethanol for example, as structural element of the crystal lattice of the compounds. It is possible for the amount of polar solvents, in particular water, to exist in a stoichiometric or non-stoichiometric ratio. In the case of stoichiometric solvates, e.g. a hydrate, hemi-, (semi-), mono, sesqui-, di-, tri-, tetra-, penta- etc. solvates or hydrates, respectively, are possible. The present invention includes all such hydrates or solvates. Further, it is possible for the compounds of the present invention to exist in free form, e.g. as a free base, or as a free acid, or as a zwitterion, or to exist in the form of a salt. Said salt may be any salt, either an organic or inorganic addition salt, particularly any pharmaceutically acceptable organic or inorganic addition salt, which is customarily used in pharmacy, or which is used, for example, for isolating or purifying the compounds of the present invention. The term “pharmaceutically acceptable salt" refers to an inorganic or organic acid addition salt of a compound of the present invention. For example, see S. M. Berge, et al. “Pharmaceutical Salts,” J. Pharm. Sci. 1977, 66, 1-19. A suitable pharmaceutically acceptable salt of the compounds of the present invention may be, for example, an acid-addition salt of a compound of the present invention bearing a nitrogen atom, in a chain or in a ring, for example, which is sufficiently basic, such as an acid-addition salt with an inorganic acid, or “mineral acid”, such as hydrochloric, hydrobromic, hydroiodic, sulfuric, sulfamic, bisulfuric, phosphoric, or nitric acid, for example, or with an organic acid, such as formic, acetic, acetoacetic, pyruvic, trifluoroacetic, propionic, butyric, hexanoic, heptanoic, undecanoic, lauric, benzoic, salicylic, 2-(4-hydroxybenzoyl)-benzoic, camphoric, cinnamic, cyclopentanepropionic, digluconic, 3-hydroxy-2-naphthoic, nicotinic, pamoic, pectinic, 3-phenylpropionic, pivalic, 2-hydroxyethanesulfonic, itaconic, trifluoromethanesulfonic, dodecylsulfuric, ethanesulfonic, benzenesulfonic, para-toluenesulfonic, methanesulfonic, 2-naphthalenesulfonic, naphthalinedisulfonic, camphorsulfonic acid, citric, tartaric, stearic, lactic, oxalic, malonic, succinic, malic, adipic, alginic, maleic, fumaric, D-gluconic, mandelic, ascorbic, glucoheptanoic, glycerophosphoric, aspartic, sulfosalicylic, or thiocyanic acid, for example. Further, another suitably pharmaceutically acceptable salt of a compound of the present invention which is sufficiently acidic, is an alkali metal salt, for example a sodium or potassium salt, an alkaline earth metal salt, for example a calcium, magnesium or strontium salt, or an aluminium or a zinc salt, or an ammonium salt derived from ammonia or from an organic primary, secondary or tertiary amine having 1 to 20 carbon atoms, such as ethylamine, diethylamine, triethylamine, ethyldiisopropylamine, monoethanolamine, diethanolamine, triethanolamine, dicyclohexylamine, dimethylaminoethanol, diethylaminoethanol, tris(hydroxymethyl)aminomethane, procaine, dibenzylamine, / V-methylmorpholine, arginine, lysine, 1,2-ethylenediamine, / V-methylpiperidine, / V-methyl-glucamine, / V, / V-dimethyl-glucamine, / V-ethyl-glucamine, 1,6-hexanediamine, glucosamine, sarcosine, serinol, 2-amino-1,3-propanediol, 3-amino-1,2-propanediol, 4-amino-1,2,3-butanetriol, or a salt with a quarternary ammonium ion having 1 to 20 carbon atoms, such as tetramethylammonium, tetraethylammonium, tetra(n-propyl)ammonium, tetra(n-butyl)ammonium, N-ber\zy\-N,N,N-trimethylammonium, choline or benzalkonium. Those skilled in the art will further recognise that it is possible for acid addition salts of the claimed compounds to be prepared by reaction of the compounds with the appropriate inorganic or organic acid via any of a number of known methods. Alternatively, alkali and alkaline earth metal salts of acidic compounds of the present invention are prepared by reacting the compounds of the present invention with the appropriate base via a variety of known methods. The present invention includes all possible salts of the compounds of the present invention as single salts, or as any mixture of said salts, in any ratio. In the present text, in particular in the Experimental Section, for the synthesis of intermediates and of examples of the present invention, when a compound is mentioned as a salt form with the corresponding base or acid, the exact stoichiometric composition of said salt form, as obtained by the respective preparation and / or purification process, is, in most cases, unknown. Unless specified otherwise, suffixes to chemical names or structural formulae relating to salts, such as "hydrochloride", "trifluoroacetate", "sodium salt", or "x HCI", "x CF3COOH", "x Na+", for example, mean a salt form, the stoichiometry of which salt form not being specified. This applies analogously to cases in which synthesis intermediates or example compounds or salts thereof have been obtained, by the preparation and / or purification processes described, as solvates, such as hydrates, with (if defined) unknown stoichiometric composition. Furthermore, the present invention includes all possible crystalline forms, or polymorphs, of the compounds of the present invention, either as single polymorph, or as a mixture of more than one polymorph, in any ratio. Moreover, the present invention also includes prodrugs of the compounds according to the invention. The term “prodrugs” here designates compounds which themselves can be biologically active or inactive, but are converted (for example metabolically or hydrolytically) into compounds according to the invention during their residence time in the body. The invention further includes all possible crystallized and polymorphic forms of the inventive compounds, whereby the polymorphs are existing either as a single polymorph form or are existing as a mixture of several polymorphs in all concentrations. The compounds are either commercially available or can be prepared according to procedures available from the public domain, as understandable to the person skilled in the art. Specific examples are described in the Experimental Section. In accordance with a second embodiment of the first aspect, the present invention covers compounds of general formula (I), supra, in which: R1 represents phenyl or heteroaryl, optionally substituted one to three times, independently from each other, with halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, C3-C6-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, Cs-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl, -NR9R10 or R9R10N-Ci-C4-alkyl; R2 represents hydrogen, Ci-C4-alkyl, Ci-C4-haloalkyl or Cs-Ce-cycloalkyl; R3 represents hydrogen, Ci-Ce-alkyl, phenyl or phenyl-Ci-Cs-alkyl, wherein said Ci-Ce-alkyl group is optionally substituted, one or more times, independently from each other, with hydroxy, halogen, Ci-C4-alkoxy, -S(O)n-Ci-C4-alkyl, phenyl-Ci-Cs-alkoxy or -NR9R10 and said phenyl groups are optionally substituted, one or more times, independently from each other, with hydroxy, halogen, cyano, Ci-Cs-alkyl, Ci-Cs-haloalkyl, Ci-Cs-alkoxy or Ci-Cs-haloalkoxy, or R2 and R3 together with the carbon atom to which they are attached form a 3- to 6-membered ring, said ring optionally containing one heteroatom selected from O, S, NH, NRa in which Ra represents a Ci-C4-alkyl group; R4 represents hydroxy, Ci-C4-alkoxy or -NR11R12, or R2 and R4 together represent *-C2-Cs-alkanediyl-X1-**, *-Ci-C2-alkanediyl-X2-Ci-Cs-alkanediyl-** or *-Ci-C2-alkanediyl-X2-C2-C3-alkanediyl-X1-** to form a 5- to 9-membered ring, wherein * indicates the point of attachment of said group for R2 and ** indicates the point of attachment of said group for R4; R5 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R6 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R7 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R8 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R9 and R10 are the same or different and represent, independently from each other, hydrogen, Ci-Cs-alkyl or tert-butoxycarbonyl, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRa in which Ra represents a Ci-C4-alkyl group; R11 and R12 are the same or different and represent, independently from each other, hydrogen, Ci-C4-alkyl or Cs-Ce-cycloalkyl, wherein said Ci-C4-alkyl group is optionally substituted with hydroxy; R13 represents hydrogen, Ci-C4-alkyl, benzyl, 4-methoxybenzyl or tert-butoxycarbonyl; R14 represents hydrogen, Ci-C4-alkyl, benzyl or 4-methoxybenzyl; X1 represents O or NR13; WO 2021 / 028382 PCT / EP2020 / 072377 X2 represents O or NR14; n represents 0, 1 or 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In accordance with a third embodiment of the first aspect, the present invention covers compounds of general formula (I), supra, in which: R1 represents phenyl or monocyclic heteroaryl, optionally substituted one to two times, independently from each other, with halogen, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, Cs-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl or -NR9R10; R2 represents hydrogen or Ci-C4-alkyl; R3 represents hydrogen, Ci-C4-alkyl, phenyl or phenyl-methyl, wherein said Ci-C4-alkyl group is optionally substituted once with hydroxy, methoxy, -S(O)n-methyl, phenyl-methoxy or-NR9R10and said phenyl groups are optionally substituted once with hydroxy, or R2 and R3 together with the carbon atom to which they are attached form a 3- to 6-membered ring, said ring optionally containing one oxygen atom; R4 represents hydroxy, methoxy or -NR11R12, or R2 and R4 together represent a group selected from: wherein * indicates the point of attachment of said group with the NH group in formula (I); R5 represents hydrogen, halogen, Ci-C4-alkyl, methoxy, trifluoromethyl or cyclopropyl; R6 represents hydrogen, halogen or methyl; R7 represents hydrogen, halogen, methyl or methoxy; R8 represents hydrogen, halogen or methyl; R9 and R10 are the same or different and represent, independently from each other, hydrogen, methyl or tert-butoxycarbonyl; R11 and R12 are the same or different and represent, independently from each other, hydrogen, Ci-Cs-alkyl or C3-C4-cycloalkyl, wherein said Ci-Cs-alkyl group is optionally substituted with hydroxy; R13 represents hydrogen or methyl; X3 represents CH2 or NH; n represents 0 or 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In accordance with a forth embodiment of the first aspect, the present invention covers compounds of general formula (la): in which: R1 represents phenyl or heteroaryl, optionally substituted one to three times, independently from each other, with halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, Cs-Ce-cycloalkyl-Ci-C4-alkyl-, Cs-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl, -NR9R10 or R9R10N-Ci-C4-alkyl; R5 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R6 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R7 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R8 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R9 and R10 are the same or different and represent, independently from each other, hydrogen, Ci-Cs-alkyl or tert-butoxycarbonyl, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRa in which Ra represents a Ci-C4-alkyl group; R14 represents hydrogen, Ci-C4-alkyl, benzyl or 4-methoxybenzyl; X3 represents CH2 or NR14; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In accordance with a fifth embodiment of the first aspect, the present invention covers compounds of general formula (lb): in which: R1 represents phenyl, pyridinyl, pyridazinyl, furanyl, oxazolyl, pyrazolyl or oxadiazolyl, optionally substituted once or twice, independently from each other, with fluoro, chloro, Ci-C4-alkyl, methoxy, trifluoromethyl, trifluoromethoxy, cyclopropyl, oxanyl or-N(CH3)2; R5, R6, R7, R8 represent, independently from each other, hydrogen, fluoro, chloro, bromo, methyl, methoxy, trifluoromethyl or cyclopropyl; their polymorphs, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In accordance with a sixth embodiment of the first aspect, the present invention covers compounds of general formula (I): (I) in which R1 represents phenyl or heteroaryl, optionally substituted one to three times, independently from each other, with halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, C1-C4-hydroxyalkyl, Ci-C4-alkoxy-Ci-C4-alkyl-, Cs-Ce-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, Cs-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl, -NR9R10, R9R10N-Ci-C4-alkyl-, Ci-C3-alkyl-S(O)m- or Ci-C3-alkyl-SO(NH)-; R2 represents hydrogen, Ci-C4-alkyl, Ci-C4-haloalkyl or Cs-Ce-cycloalkyl; R3 represents hydrogen, Ci-Ce-alkyl, phenyl or phenyl-Ci-C3-alkyl, wherein said Ci-Ce-alkyl group is optionally substituted, one or more times, independently from each other, with hydroxy, halogen, Ci-C4-alkoxy, -S(O)n-Ci-C4-alkyl, phenyl-Ci-C3-alkoxy or -NR9R10 and said phenyl groups are optionally substituted, one or more times, independently from each other, with hydroxy, halogen, cyano, Ci-C3-alkyl, Ci-C3-haloalkyl, Ci-C3-alkoxy or Ci-C3-haloalkoxy, or R2 and R3 together with the carbon atom to which they are attached form a 3- to 6-membered ring, said ring optionally containing one heteroatom selected from O, S, NH, NRa in which Ra represents a Ci-C4-alkyl group; R4 represents hydroxy, Ci-C4-alkoxy or -NR11R12, or R2 and R4 together represent *-C2-Cs-alkanediyl-X1-**, *-Ci-C2-alkanediyl-X2-Ci-C3-alkanediyl-** or *-Ci-C2-alkanediyl-X2-C2-C3-alkanediyl-X1-** to form a 5- to 9-membered ring, wherein * indicates the point of attachment of said group for R2 and ** indicates the point of attachment of said group for R4; R5 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, 4- to 6-membered heterocycloalkyl, -CO2-Ci-C4-alkyl, -CO-NR9R10 or-NR9R10; R6 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R7 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; R8 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, 1-R15-Cs-Ce-cycloalkyl, -CO2-Ci-C4-alkyl, -CO-NR9R10 or-NR9R10; R9 and R10 are the same or different and represent, independently from each other, hydrogen, Ci-Cs-alkyl or tert-butoxycarbonyl, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRa in which Ra represents a Ci-C4-alkyl group; R11 and R12 are the same or different and represent, independently from each other, hydrogen, Ci-C4-alkyl or Cs-Ce-cycloalkyl, wherein said Ci-C4-alkyl group is optionally substituted with hydroxy; R13 represents hydrogen, Ci-C4-alkyl, benzyl, 4-methoxybenzyl or tert-butoxycarbonyl; R14 represents hydrogen, Ci-C4-alkyl, benzyl or 4-methoxybenzyl; R15 represents Ci-Cs-alkyl or Ci-Cs-haloalkyl; X1 represents O or NR13; X2 represents O or NR14; m represents 0, 1 or 2; n represents 0, 1 or 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In accordance with a second aspect, the present invention covers methods of preparing compounds of general formula (I) as defined supra, said methods comprising the step of allowing an intermediate compound of general formula (V): R1 (V), in which R1, R5, R6, R7 and R8 are as defined supra to react with a compound of general formula (VII): (VII), in which R2, R3 and R4 are as defined supra thereby giving a compound of general formula (I): (I), in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined supra. The present invention covers methods of preparing compounds of the present invention of general formula (I), said methods comprising the steps as described in the Experimental Section herein. In accordance with a third aspect, the present invention covers intermediate compounds which are useful for the preparation of the compounds of general formula (I), supra. Particularly, the inventions covers the intermediate compounds of general formula (V): R1 (V), in which R1, R5, R6, R7 and R8 are as defined supra. In accordance with a forth aspect, the present invention covers the use of said intermediate compounds for the preparation of a compound of general formula (I) as defined supra. Particularly, the inventions covers the use of intermediate compounds of general formula (V): R1 (V), in which R1, R5, R6, R7 and R8 are as defined supra for the preparation of a compound of general formula (I) as defined supra. The present invention covers the intermediate compounds which are disclosed in the Example Section of this text, infra. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R1 represents phenyl or heteroaryl, optionally substituted one to three times, independently from each other, with halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, C1-C4-haloalkoxy, Ci-C4-hydroxyalkyl, Ci-C4-alkoxy-Ci-C4-alkyl-, Cs-Ce-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, C3-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl, -NR9R10, R9R10N-Ci-C4-alkyl-, Ci-C3-alkyl-S(O)m- or Ci-C3-alkyl-SO(NH)-; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R1 represents phenyl or heteroaryl, optionally substituted one to three times, independently from each other, with halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, C3-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl, -NR9R10 or R9R10N-Ci-C4-alkyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R1 represents phenyl or monocyclic heteroaryl, optionally substituted one to three times, independently from each other, with halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, Cs-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl, -NR9R10 or R9R10N-Ci-C4-alkyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R1 represents phenyl or monocyclic heteroaryl, optionally substituted one to two times, independently from each other, with halogen, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, Cs-Ce-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl or -NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R1 represents phenyl or monocyclic heteroaryl, optionally substituted one to two times, independently from each other, with halogen, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, C3-Ce-cycloalkyl-Ci-C4-alkyl-, Cs-Ce-cycloalkyl-O-, 5- to 6-membered heterocycloalkyl or -NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R1 represents phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, furanyl, thiophenyl, pyrolyl, 1,2-thiazolyl, oxazolyl, triazolyl, imidazolyl, oxazolyl, pyrazolyl, oxadiazolyl, or imidazpyridinyl, optionally substituted once or twice, independently from each other, with fluoro, chloro, bromo, cyano, Ci-C4-alkyl, methoxy, trifluoromethyl, difluoromethoxy, trifluoromethoxy, cyclopropyl, cyclobutyl, cyclopropylmethyl, oxanyl or -N(CH3)2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R1 represents phenyl, pyridinyl, pyridazinyl, furanyl, oxazolyl, pyrazolyl or oxadiazolyl, optionally substituted once or twice, independently from each other, with fluoro, chloro, Ci-C4-alkyl, methoxy, trifluoromethyl, trifluoromethoxy, cyclopropyl, oxanyl or-N(CH3)2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R2 represents hydrogen, Ci-C4-alkyl, Ci-C4-haloalkyl or C3-Ce-cycloalkyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R2 represents hydrogen or Ci-C4-alkyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R3 represents hydrogen, Ci-Ce-alkyl, phenyl or phenyl-Ci-C3-alkyl, wherein said Ci-Ce-alkyl group is optionally substituted, one or more times, independently from each other, with hydroxy, halogen, Ci-C4-alkoxy, -S(O)n-Ci-C4-alkyl, phenyl-Ci-C3-alkoxy or -NR9R10 and said phenyl groups are optionally substituted, one or more times, independently from each other, with hydroxy, halogen, cyano, Ci-C3-alkyl, Ci-C3-haloalkyl, Ci-C3-alkoxy or Ci-C3-haloalkoxy; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R3 represents hydrogen, Ci-C4-alkyl, phenyl or phenyl-methyl, wherein said Ci-C4-alkyl group is optionally substituted once with hydroxy, methoxy, -S(O)n-methyl, phenyl-methoxy or-NR9R10and said phenyl groups are optionally substituted once with hydroxy; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R2 and R3 together with the carbon atom to which they are attached form a 3- to 6-membered ring, said ring optionally containing one heteroatom selected from O, S, NH, NRa in which Ra represents a Ci-C4-alkyl group; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R2 and R3 together with the carbon atom to which they are attached form a 3- to 6-membered ring, said ring optionally containing one oxygen atom; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R4 represents hydroxy, Ci-C4-alkoxy or -NR11R12; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R4 represents hydroxy, methoxy or -NR11R12; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R2 and R4 together represent *-C2-Cs-alkanediyl-X1-**, *-Ci-C2-alkanediyl-X2-Ci-Cs-alkanediyl-** or *-Ci-C2-alkanediyl-X2-C2-C3-alkanediyl-X1-** to form a 5- to 9-membered ring, wherein * indicates the point of attachment of said group for R2 and ** indicates the point of attachment of said group for R4; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R2 and R4 together represent a group selected from: wherein * indicates the point of attachment of said group with the NH group in formula (I); their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R5 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, 4- to 6-membered heterocycloalkyl, -CO2-Ci-C4-alkyl, -CO-NR9R10 or-NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R5 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R5 represents hydrogen, halogen, Ci-C4-alkyl, methoxy, trifluoromethyl or cyclopropyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R6 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R6 represents hydrogen, halogen or methyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R7 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R7 represents hydrogen, halogen, methyl or methoxy; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R8 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, 1-R15-Cs-Ce-cycloalkyl, -CO2-Ci-C4-alkyl, -CO-NR9R10, -NR9R10, Ci-C4-hydroxyalkyl, Ci-C4-alkoxy-Ci-C4-alkyl-, Ci-C4-alkyl-S-, Ci-C4-alkyl-S-Ci-C4-alkyl-, -S(=O)R’, -S(=O)2R’, -S(=O)2NH2, -S(=O)2NHR’, -S(=O)2N(R’)R”, -S(=O)(=NH)R’, 4- to 6-membered heterocycloalkyl, or-OR16; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R8 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, C1-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl, 1-R15-Cs-Ce-cycloalkyl, -CO2-Ci-C4-alkyl, -CO-NR9R10 or-NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R8 represents hydrogen, halogen, cyano, hydroxy, Ci-C4-alkyl, Ci-C4-alkoxy, Ci-C4-haloalkyl, Ci-C4-haloalkoxy, Cs-Ce-cycloalkyl or-NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R8 represents hydrogen, halogen or methyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R5, R6, R7, R8 represent, independently from each other, hydrogen, fluoro, chloro, bromo, methyl, methoxy, trifluoromethyl or cyclopropyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R9 and R10 are the same or different and represent, independently from each other, hydrogen, Ci-Cs-alkyl or tert-butoxycarbonyl, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRa in which Ra represents Ci-C4-alkyl or C1-C4-alkoxycarbonyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R9 and R10 are the same or different and represent, independently from each other, hydrogen, Ci-Cs-alkyl or tert-butoxycarbonyl, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRa in which Ra represents a Ci-C4-alkyl group; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R9 and R10 are the same or different and represent, independently from each other, hydrogen, methyl or tert-butoxycarbonyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R11 and R12 are the same or different and represent, independently from each other, hydrogen, Ci-C4-alkyl, C2-C4-hydroxyalkyl, Ci-C4-alkoxy-C2-C4-alkyl-, R9R10N-C2-C4-alkyl-, Cs-Ce-cycloalkyl, 4- to 7-membered heterocycloalkyl, said 4- to 7-membered heterocycloalkyl group is optionally substituted, one or two times, independently from each other, with hydroxy, oxo, halogen, Ci-C4-alkyl, Ci-C4-alkoxy, or-NR9R10, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRa in which Ra represents Ci-C4-alkyl or C1-C4-alkoxycarbonyl and is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, Ci-C4-alkyl, Ci-C4-alkoxy, or-NR9R10, or together with the nitrogen atom to which they are attached form a heterospirocycloalkyl group, which is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, Ci-C4-alkyl, Ci-C4-alkoxy, or-NR9R10, or together with the nitrogen atom to which they are attached form a bridged heterocycloalkyl group, which is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, Ci-C4-alkyl, Ci-C4-alkoxy, or-NR9R10; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R11 and R12 are the same or different and represent, independently from each other, hydrogen, Ci-C4-alkyl or Cs-Ce-cycloalkyl, wherein said Ci-C4-alkyl group is optionally substituted with hydroxy; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R11 and R12 are the same or different and represent, independently from each other, hydrogen, Ci-Cs-alkyl or C3-C4-cycloalkyl, wherein said Ci-Cs-alkyl group is optionally substituted with hydroxy; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R13 represents hydrogen, Ci-C4-alkyl, benzyl, 4-methoxybenzyl or tert-butoxycarbonyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R13 represents hydrogen or methyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R14 represents hydrogen, Ci-C4-alkyl, benzyl or 4-methoxybenzyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R15 represents Ci-Cs-alkyl or Ci-Cs-haloalkyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R15 represents methyl or trifluoromethyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R16 represents C2-Ce-hydroxyalkyl, Ci-C4-alkoxy-C2-Ce-alkyl-, or Cs-Ce-cycloalkyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: R’ and R” represent, independently from each other, Ci-Ce-alkyl, Ci-Ce-haloalkyl, or Cs-Ce-cycloalkyl; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: X1 represents O, S(O)m, or NR13; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: X1 represents O or NR13; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: X2 represents O, S(O)m, or NR14; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: X2 represents O or NR14; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: X3 represents CH2 or NR14; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: X3 represents CH2 or NH; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: m represents 0, 1 or 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: m represents 0 or 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: m represents 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: n represents 0, 1 or 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: n represents 0 or 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a further embodiment of the first aspect, the present invention covers compounds of formula (I), supra, in which: n represents 2; their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates and solvates, as well as their physiological acceptable salts and solvates of these salts, as well as mixtures of the same. In a particular further embodiment of the first aspect, the present invention covers combinations of two or more of the above mentioned embodiments under the heading “further embodiments of the first aspect of the present invention”. The present invention covers any sub-combination within any embodiment or aspect of the present invention of intermediate compounds of general formula (V), supra. The compounds of general formula (I) of the present invention can be converted to any salt, preferably pharmaceutically acceptable salts, as described herein, by any method which is known to the person skilled in the art. Similarly, any salt of a compound of general formula (I) of the present invention can be converted into the free compound, by any method which is known to the person skilled in the art. The compounds according to the invention of general formula (I) can be prepared according to 5 the following scheme 1. The scheme and procedures described below illustrate synthetic routes to the compounds of general formula (I) of the invention and are not intended to be limiting. It is clear to the person skilled in the art that the order of transformations as exemplified in scheme 1 can be modified in various ways. The order of transformations exemplified in this scheme is therefore not intended to be limiting. In addition, interconversion of any of the substituents R1, 10 R2, R3, R4, R5, R6, R7 or R8 can be achieved before and / or after the exemplified transformations. These modifications can be such as the introduction of protecting groups, cleavage of protecting groups, reduction or oxidation of functional groups, halogenation, metallation, metal-catalysed coupling reactions, substitution or other reactions known to the person skilled in the art. These transformations include those which introduce a functionality which allows for further 15 interconversion of substituents. Appropriate protecting groups and their introduction and cleavage are well-known to the person skilled in the art. Specific examples are described in the subsequent paragraphs. Scheme 1 shows a route for the preparation of compounds of general formula (I). (I) (V) Scheme 1: Route for the preparation of compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as given for general formula (I), supra and Ra represents 5 Ci-Ce-alkyl or Cs-Ce-alkenyl and Rb represents hydrogen or -C(O)O-Ra. Scheme 2 describes another route for the preparation of compounds of formula (I). (I) (X) Scheme 2: Route for the preparation of compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7, R8 and n have the meaning as given for general formula (I), supra. Scheme 3 describes an alternative route to prepare intermediates (IV). (II) (XI) (IV) Scheme 3: Route for the preparation of compounds of general formula (IV) in which R1, R5, R6, R7 and R8 have the meaning as given for general formula (I), supra. Scheme 4 describes another route for the preparation of compounds of formula (I). R1 (V) (XII) (I) Scheme 4: Route for the preparation of compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as given for general formula (I), supra. Scheme 5 describes another route for the preparation of compounds of formula (I). R1 (V) (XIII) (I) Scheme 5: Route for the preparation of compounds of general formula (I) in which R1, R2, R3, R5, R6, R7 and R8 have the meaning as given for general formula (I), supra, R4 10 represents -NR11R12 as given for general formula (I), supra, and R represents hydrogen, Ci-Ce- alkyl or Cs-Ce-alkenyl. Scheme 6 describes an alternative route to prepare intermediates (IV) and (IX) respectively. X = O, S 15 Scheme 6: Route for the preparation of compounds of general formula (IV) in which R1, R5, R6, R7 and R8 have the meaning as given for general formula (I), supra and X represents oxygen or sulfur. Scheme 7 describes an alternative route to prepare intermediates (IV) and (IX) respectively. (XVI) Y=CI, Br Suzuki reaction R1 (IV, IX) (XIV) X = O, S Scheme 7: Route for the preparation of compounds of general formula (IV) in which R1, R5, R6, R7 and R8 have the meaning as given for general formula (I), supra and X represents oxygen or 5 sulfur and Y represents chloro or bromo. Scheme 8 describes an alternative route to prepare intermediates (IV). (XVIII) Scheme 8: Route for the preparation of compounds of general formula (IV) in which R1, R5, R6, 5 R7 and R8 have the meaning as given for general formula (I), supra. Scheme 9 describes another route for the preparation of compounds of formula (I). (XX) 10 Scheme 9: Route for the preparation of compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as given for general formula (I), supra and R represents Ci-Ce-alkyl. Compounds of general formula (I) of the present invention demonstrate a valuable 15 pharmacological spectrum of action, which could not have been predicted. Compounds of the present invention have surprisingly been found to effectively inhibit AHR and it is possible therefore that said compounds be used for the treatment or prophylaxis of diseases, preferably cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, in humans and animals. Disorders and conditions particularly suitable for treatment with an AHR inhibitor of the present invention are liquid and solid tumours, such as cancers of the breast, respiratory tract, brain, reproductive organs, digestive tract, urinary tract, eye, liver, skin, head and neck, thyroid, parathyroid and their distant metastases. Those disorders also include lymphomas, sarcomas, and leukaemias. Examples of breast cancers include, but are not limited to, triple negative breast cancer, invasive ductal carcinoma, invasive lobular carcinoma, ductal carcinoma in situ, and lobular carcinoma in situ. Examples of cancers of the respiratory tract include, but are not limited to, small-cell and nonsmall-cell lung carcinoma, as well as bronchial adenoma and pleuropulmonary blastoma. Examples of brain cancers include, but are not limited to, brain stem and hypophtalmic glioma, cerebellar and cerebral astrocytoma, glioblastoma, medulloblastoma, ependymoma, as well as neuroectodermal and pineal tumour. Tumours of the male reproductive organs include, but are not limited to, prostate and testicular cancer. Tumours of the female reproductive organs include, but are not limited to, endometrial, cervical, ovarian, vaginal, and vulvar cancer, as well as sarcoma of the uterus. Examples of ovarian cancer include, but are not limited to serous tumour, endometrioid tumour, mucinous cystadenocarcinoma, granulosa cell tumour, Sertoli-Leydig cell tumour and arrhenoblastoma. Examples of cervical cancer include, but are not limited to squamous cell carcinoma, adenocarcinoma, adenosquamous carcinoma, small cell carcinoma, neuroendocrine tumour, glassy cell carcinoma and villoglandular adenocarcinoma. Tumours of the digestive tract include, but are not limited to, anal, colon, colorectal, esophageal, gallbladder, gastric, pancreatic, rectal, small-intestine, and salivary gland cancers. Examples of esophageal cancer include, but are not limited to esophageal cell carcinomas and adenocarcinomas, as well as squamous cell carcinomas, leiomyosarcoma, malignant melanoma, rhabdomyosarcoma and lymphoma,. Examples of gastric cancer include, but are not limited to intestinal type and diffuse type gastric adenocarcinoma. Examples of pancreatic cancer include, but are not limited to ductal adenocarcinoma, adenosquamous carcinomas and pancreatic endocrine tumours. Tumours of the urinary tract include, but are not limited to, bladder, penile, kidney, renal pelvis, ureter, urethral and human papillary renal cancers. Examples of kidney cancer include, but are not limited to renal cell carcinoma, urothelial cell carcinoma, juxtaglomerular cell tumour (reninoma), angiomyolipoma, renal oncocytoma, Bellini duct carcinoma, clear-cell sarcoma of the kidney, mesoblastic nephroma and Wilms' tumour. Examples of bladder cancer include, but are not limited to transitional cell carcinoma, squamous cell carcinoma, adenocarcinoma, sarcoma and small cell carcinoma. Eye cancers include, but are not limited to, intraocular melanoma and retinoblastoma. Examples of liver cancers include, but are not limited to, hepatocellular carcinoma (liver cell carcinomas with or without fibrolamellar variant), cholangiocarcinoma (intrahepatic bile duct carcinoma), and mixed hepatocellular cholangiocarcinoma. Skin cancers include, but are not limited to, squamous cell carcinoma, Kaposi’s sarcoma, malignant melanoma, Merkel cell skin cancer, and non-melanoma skin cancer. Head-and-neck cancers include, but are not limited to, squamous cell cancer of the head and neck, laryngeal, hypopharyngeal, nasopharyngeal, oropharyngeal cancer, salivary gland cancer, lip and oral cavity cancer and squamous cell. Lymphomas include, but are not limited to, AIDS-related lymphoma, non-Hodgkin’s lymphoma, cutaneous T-cell lymphoma, Burkitt lymphoma, Hodgkin’s disease, and lymphoma of the central nervous system. Sarcomas include, but are not limited to, sarcoma of the soft tissue, osteosarcoma, malignant fibrous histiocytoma, lymphosarcoma, and rhabdomyosarcoma. Leukemias include, but are not limited to, acute myeloid leukemia, acute lymphoblastic leukemia, chronic lymphocytic leukemia, chronic myelogenous leukemia, and hairy cell leukemia. The term “treating” or “treatment” as stated throughout this document is used conventionally, for example the management or care of a subject for the purpose of combating, alleviating, reducing, relieving, improving the condition of a disease or disorder, such as a carcinoma. The compounds of the present invention can be used in particular in therapy and prevention, i.e. prophylaxis, of tumour growth and metastases, especially in solid tumours of all indications and stages with or without pre-treatment of the tumour growth. Generally, the use of chemotherapeutic agents and / or anti-cancer agents in combination with a compound or pharmaceutical composition of the present invention will serve to: yield better efficacy in reducing the growth of a tumour or even eliminate the tumour as compared to administration of either agent alone, provide for the administration of lesser amounts of the administered chemotherapeutic agents, provide for a chemotherapeutic treatment that is well tolerated in the patient with fewer deleterious pharmacological complications than observed with single agent chemotherapies and certain other combined therapies, provide for treating a broader spectrum of different cancer types in mammals, especially humans, provide for a higher response rate among treated patients, provide for a longer survival time among treated patients compared to standard chemotherapy treatments, provide a longer time for tumour progression, and / or yield efficacy and tolerability results at least as good as those of the agents used alone, compared to known instances where other cancer agent combinations produce antagonistic effects. In addition, the compounds of general formula (I) of the present invention can also be used in combination with radiotherapy and / or surgical intervention. In a further embodiment of the present invention, the compounds of general formula (I) of the present invention may be used to sensitize a cell to radiation, i.e. treatment of a cell with a compound of the present invention prior to radiation treatment of the cell renders the cell more susceptible to DNA damage and cell death than the cell would be in the absence of any treatment with a compound of the present invention. In one aspect, the cell is treated with at least one compound of general formula (I) of the present invention. Thus, the present invention also provides a method of killing a cell, wherein a cell is administered one or more compounds of the present invention in combination with conventional radiation therapy. The present invention also provides a method of rendering a cell more susceptible to cell death, wherein the cell is treated with one or more compounds of general formula (I) of the present invention prior to the treatment of the cell to cause or induce cell death. In one aspect, after the cell is treated with one or more compounds of general formula (I) of the present invention, the cell is treated with at least one compound, or at least one method, or a combination thereof, in order to cause DNA damage for the purpose of inhibiting the function of the normal cell or killing the cell. In other embodiments of the present invention, a cell is killed by treating the cell with at least one DNA damaging agent, i.e. after treating a cell with one or more compounds of general formula (I) of the present invention to sensitize the cell to cell death, the cell is treated with at least one DNA damaging agent to kill the cell. DNA damaging agents useful in the present invention include, but are not limited to, chemotherapeutic agents (e.g. cis platin), ionizing radiation (X-rays, ultraviolet radiation), carcinogenic agents, and mutagenic agents. In other embodiments, a cell is killed by treating the cell with at least one method to cause or induce DNA damage. Such methods include, but are not limited to, activation of a cell signalling pathway that results in DNA damage when the pathway is activated, inhibiting of a cell signalling pathway that results in DNA damage when the pathway is inhibited, and inducing a biochemical change in a cell, wherein the change results in DNA damage. By way of a non-limiting example, a DNA repair pathway in a cell can be inhibited, thereby preventing the repair of DNA damage and resulting in an abnormal accumulation of DNA damage in a cell. In one aspect of the invention, a compound of general formula (I) of the present invention is administered to a cell prior to the radiation or other induction of DNA damage in the cell. In another aspect of the invention, a compound of general formula (I) of the present invention is administered to a cell concomitantly with the radiation or other induction of DNA damage in the cell. In yet another aspect of the invention, a compound of general formula (I) of the present invention is administered to a cell immediately after radiation or other induction of DNA damage in the cell has begun. In another aspect, the cell is in vitro. In another embodiment, the cell is in vivo. The compounds of the present invention can be administered as the sole pharmaceutical agent or in combination with one or more other pharmaceutically active ingredients where the combination causes no unacceptable adverse effects. The present invention also covers such pharmaceutical combinations. For example, the compounds of the present invention can be combined with: 1311-chTNT, abarelix, abemaciclib, abiraterone, acalabrutinib, aclarubicin, adalimumab, ado-trastuzumab emtansine, afatinib, aflibercept, aldesleukin, alectinib, alemtuzumab, alendronic acid, alitretinoin, altretamine, amifostine, aminoglutethimide, hexyl aminolevulinate, amrubicin, amsacrine, anastrozole, ancestim, anethole dithiolethione, anetumab ravtansine, angiotensin II, antithrombin III, apalutamide, aprepitant, arcitumomab, arglabin, arsenic trioxide, asparaginase, atezolizumab, avelumab, axicabtagene ciloleucel, axitinib, azacitidine, basiliximab, belotecan, bendamustine, besilesomab, belinostat, bevacizumab, bexarotene, bicalutamide, bisantrene, bleomycin, blinatumomab, bortezomib, bosutinib, buserelin, brentuximab vedotin, brigatinib, busulfan, cabazitaxel, cabozantinib, calcitonine, calcium folinate, calcium levofolinate, capecitabine, capromab, carbamazepine carboplatin, carboquone, carfilzomib, carmofur, carmustine, catumaxomab, celecoxib, celmoleukin, ceritinib, cetuximab, chlorambucil, chlormadinone, chlormethine, cidofovir, cinacalcet, cisplatin, cladribine, clodronic acid, clofarabine, cobimetinib, copanlisib, crisantaspase, crizotinib, cyclophosphamide, cyproterone, cytarabine, dacarbazine, dactinomycin, daratumumab, darbepoetin alfa, dabrafenib, dasatinib, daunorubicin, decitabine, degarelix, denileukin diftitox, denosumab, depreotide, deslorelin, dianhydrogalactitol, dexrazoxane, dibrospidium chloride, dianhydrogalactitol, diclofenac, dinutuximab, docetaxel, dolasetron, doxifluridine, doxorubicin, doxorubicin + estrone, dronabinol, durvalumab, eculizumab, edrecolomab, elliptinium acetate, elotuzumab, eltrombopag, Enasidenib, endostatin, enocitabine, enzalutamide, epirubicin, epitiostanol, epoetin alfa, epoetin beta, epoetin zeta, eptaplatin, eribulin, erlotinib, esomeprazole, estradiol, estramustine, ethinylestradiol, etoposide, everolimus, exemestane, fadrozole, fentanyl, filgrastim, fluoxymesterone, floxuridine, fludarabine, fluorouracil, flutamide, folinic acid, formestane, fosaprepitant, fotemustine, fulvestrant, gadobutrol, gadoteridol, gadoteric acid meglumine, gadoversetamide, gadoxetic acid, gallium nitrate, ganirelix, gefitinib, gemcitabine, gemtuzumab, Glucarpidase, glutoxim, GM-CSF, goserelin, granisetron, granulocyte colony stimulating factor, histamine dihydrochloride, histrelin, hydroxycarbamide, 1-125 seeds, lansoprazole, ibandronic acid, ibritumomab tiuxetan, ibrutinib, idarubicin, ifosfamide, imatinib, imiquimod, improsulfan, indisetron, incadronic acid, ingenol mebutate, inotuzumab ozogamicin, interferon alfa, interferon beta, interferon gamma, iobitridol, iobenguane (1231), iomeprol, ipilimumab, irinotecan, Itraconazole, ixabepilone, ixazomib, lanreotide, lansoprazole, lapatinib, lasocholine, lenalidomide, lenvatinib, lenograstim, lentinan, letrozole, leuprorelin, levamisole, levonorgestrel, levothyroxine sodium, lisuride, lobaplatin, lomustine, lonidamine, lutetium Lu 177 dotatate, masoprocol, medroxyprogesterone, megestrol, melarsoprol, melphalan, mepitiostane, mercaptopurine, mesna, methadone, methotrexate, methoxsalen, methylaminolevulinate, methylprednisolone, methyltestosterone, metirosine, midostaurin, mifamurtide, miltefosine, miriplatin, mitobronitol, mitoguazone, mitolactol, mitomycin, mitotane, mitoxantrone, mogamulizumab, molgramostim, mopidamol, morphine hydrochloride, morphine sulfate, mvasi, nabilone, nabiximols, nafarelin, naloxone + pentazocine, naltrexone, nartograstim, necitumumab, nedaplatin, nelarabine, neratinib, neridronic acid, netupitant / palonosetron, nivolumab, pentetreotide, nilotinib, nilutamide, nimorazole, nimotuzumab, nimustine, nintedanib, niraparib, nitracrine, nivolumab, obinutuzumab, octreotide, ofatumumab, olaparib, olaratumab, omacetaxine mepesuccinate, omeprazole, ondansetron, oprelvekin, orgotein, orilotimod, osimertinib, oxaliplatin, oxycodone, oxymethoIone, ozogamicine, p53 gene therapy, paclitaxel, palbociclib, palifermin, palladium-103 seed, palonosetron, pamidronic acid, panitumumab, panobinostat, pantoprazole, pazopanib, pegaspargase, PEG-epoetin beta (methoxy PEGepoetin beta), pembrolizumab, pegfilgrastim, peginterferon alfa-2b, pembrolizumab, pemetrexed, pentazocine, pentostatin, peplomycin, Perflubutane, perfosfamide, Pertuzumab, picibanil, pilocarpine, pirarubicin, pixantrone, plerixafor, plicamycin, poliglusam, polyestradiol phosphate, polyvinylpyrrolidone + sodium hyaluronate, polysaccharide-K, pomalidomide, ponatinib, porfimer sodium, pralatrexate, prednimustine, prednisone, procarbazine, procodazole, propranolol, quinagolide, rabeprazole, racotumomab, radium-223 chloride, radotinib, raloxifene, raltitrexed, ramosetron, ramucirumab, ranimustine, rasburicase, razoxane, refametinib , regorafenib, ribociclib, risedronic acid, rhenium-186 etidronate, rituximab, rolapitant, romidepsin, romiplostim, romurtide, rucaparib, samarium (153Sm) lexidronam, sargramostim, sarilumab, satumomab, secretin, siltuximab, sipuleucel-T, sizofiran, sobuzoxane, sodium glycididazole, sonidegib, sorafenib, stanozolol, streptozocin, sunitinib, talaporfin, talimogene laherparepvec, tamibarotene, tamoxifen, tapentadol, tasonermin, teceleukin, technetium (99mTc) nofetumomab merpentan, 99mTc-HYNIC-[Tyr3]-octreotide, tegafur, tegafur + gimeracil + oteracil, temoporfin, temozolomide, temsirolimus, teniposide, testosterone, tetrofosmin, thalidomide, thiotepa, thymalfasin, thyrotropin alfa, tioguanine, tisagenlecleucel, tocilizumab, topotecan, toremifene, tositumomab, trabectedin, trametinib, tramadol, trastuzumab, trastuzumab emtansine, treosulfan, tretinoin, trifluridine + tipiracil, trilostane, triptorelin, trametinib, trofosfamide, thrombopoietin, tryptophan, ubenimex, valatinib , valrubicin, vandetanib, vapreotide, vemurafenib, vinblastine, vincristine, vindesine, vinflunine, vinorelbine, vismodegib, vorinostat, vorozole, yttrium-90 glass microspheres, zinostatin, zinostatin stimalamer, zoledronic acid, zorubicin. The compounds of the invention can further be combined with other reagents targeting the immune system, such as immune checkpoint inhibitors. Compositions comprising a PD-1 / -L1 axis antagonist and an AHR antagonist and methods of using the same are provided herein. Data presented herein demonstrate that a combination of AHR inhibition and blockade of the PD-1 / -L1 axis reduces the growth of tumor cells in more than an additive manner. PD-1, along with its ligands PD-L1 and PD-L2, function as negative regulators of T cell activation. AHR suppresses immune cell function while increasing cancer cell proliferation and motility. PD-L1 is overexpressed in many cancers and overexpression of PD-1 often occurs concomitantly in tumor infiltrating T cells. Thus results in attenuation of T cell activation and evasion of immune surveillance, which contributes to impaired antitumor immune responses. (Keir M E et al. (2008) Annu. Rev. Immunol. 26:677). Simultaneously targeting both the PD-1 / -L1 axis and AHR enhances antitumor immune responses in more than an additive manner, leading to reduction of tumor growth that is unexpected. In some experiments, the resulting effect is greater than the expected or calculated additive effect of the individual components given separately. Thus, compositions comprising a PD-1 / -L1 axis antagonist and an AHR antagonist are surprisingly effective in enhancing an immune response and in the treatment of cancer. In addition, the inventive compounds can also be used as a therapeutic in a variety of other disorders wherein AHR is involved such as, cardiovascular and lung diseases. Accordingly, the compounds according to the invention are suitable for the treatment and / or prophylaxis in particular of cardiovascular, inflammatory and fibrotic disorders and of renal disorders, in particular of acute and chronic renal insufficiency, and also of acute and chronic renal failure. Accordingly, the compounds according to the invention can be used in medicaments for the treatment and / or prophylaxis of cardiovascular, inflammatory and fibrotic disorders, renal disorders, in particular of acute and chronic renal insufficiency, and also of acute and chronic renal failure. For the purpose of the present invention the term renal insufficiency comprises both acute and chronic manifestations of renal insufficiency, and also underlying or related renal disorders such as diabetic and non-diabetic nephropathies, hypertensive nephropathies, ischaemic renal disorders, renal hypoperfusion, intradialytic hypotension, obstructive uropathy, renal stenoses, glomerulopathies, glomerulonephritis (such as, for example, primary glomerulonephritides; minimal change glomerulonephritis (lipoidnephrosis); membranous glomerulonephritis; focal segmental glomerulosclerosis (FSGS); membrane-proliferative glomerulonephritis; crescentic glomerulonephritis; mesangioproliferative glomerulonephritis (IgA nephritis, Berger's disease); post-infectious glomerulonephritis; secondary glomerulonephritides: diabetes mellitus, lupus erythematosus, amyloidosis, Goodpasture syndrome, Wegener granulomatosis, Henoch-Schdnlein purpura, microscopic polyangiitis, acute glomerulonephritis, pyelonephritis (for example as a result of: urolithiasis, benign prostate hyperplasia, diabetes, malformations, abuse of analgesics, Crohn's disease), glomerulosclerosis, arteriolonecrose of the kidney, tubulointerstitial diseases, nephropathic disorders such as primary and congenital or aquired renal disorder, Alport syndrome, nephritis, immunological kidney disorders such as kidney transplant rejection and immunocomplex-induced renal disorders, nephropathy induced by toxic substances, nephropathy induced by contrast agents, diabetic and non-diabetic nephropathy, renal cysts, nephrosclerosis, hypertensive nephrosclerosis and nephrotic syndrome which can be characterized diagnostically, for example by abnormally reduced creatinine and / or water excretion, abnormally elevated blood concentrations of urea, nitrogen, potassium and / or creatinine, altered activity of renal enzymes, for example glutamyl synthetase, altered urine osmolarity or urine volume, elevated microalbuminuria, macroalbuminuria, lesions on glomerulae and arterioles, tubular dilatation, hyperphosphataemia and / or the need for dialysis. The present invention also comprises the use of the compounds according to the invention for the treatment and / or prophylaxis of sequelae of renal insufficiency, for example pulmonary oedema, heart failure, uremia, anemia, electrolyte disturbances (for example hypercalemia, hyponatremia) and disturbances in bone and carbohydrate metabolism. The present invention also comprises the use of the compounds according to the invention for the treatment and / or prevention of sequelae of renal insufficiency, for example pulmonary oedema, heart failure, uraemia, anaemia, electrolyte disturbances (for example hyperkalaemia, hyponatraemia) and disturbances in bone and carbohydrate metabolism. The compounds according to the invention are further suitable for the treatment and / or prevention of polycystic kidney disease (PCKD) and of the syndrome of inappropriate ADH secretion (SIADH). Furthermore, the compounds according to the invention are also suitable for the treatment and / or prophylaxis of metabolic syndrome, hypertension, resistant hypertension, acute and chronic heart failure, coronary heart disease, stable and unstable angina pectoris, peripheral and cardiac vascular disorders, arrhythmias, atrial and ventricular arrhythmias and impaired conduction, for example atrioventricular blocks degrees l-lll (AB block l-lll), supraventricular tachyarrhythmia, atrial fibrillation, atrial flutter, ventricular fibrillation, ventricular flutter, ventricular tachyarrhythmia, Torsade de pointes tachycardia, atrial and ventricular extrasystoles, AV-junctional extrasystoles, sick sinus syndrome, syncopes, AV-nodal re-entry tachycardia, Wolff-Parkinson-White syndrome, of acute coronary syndrome (ACS), autoimmune cardiac disorders (pericarditis, endocarditis, valvolitis, aortitis, cardiomyopathies), shock such as cardiogenic shock, septic shock and anaphylactic shock, aneurysms, boxer cardiomyopathy (premature ventricular contraction (PVC)), for treatment and / or prophylaxis of thromboembolic disorders and ischaemias such as myocardial ischaemia, myocardial infarction, stroke, cardiac hypertrophy, transient and ischaemic attacks, preeclampsia, inflammatory cardiovascular disorders, spasms of the coronary arteries and peripheral arteries, oedema formation, for example pulmonary oedema, cerebral oedema, renal oedema or oedema caused by heart failure, peripheral circulatory disturbances, reperfusion damage, arterial and venous thromboses, myocardial insufficiency, endothelial dysfunction, to prevent restenoses, for example after thrombolysis therapies, percutaneous transluminal angioplasties (PTA), transluminal coronary angioplasties (PTCA), heart transplants and bypass operations, and also micro- and macrovascular damage (vasculitis), increased levels of fibrinogen and of low-density lipoprotein (LDL) and increased concentrations of plasminogen activator inhibitor 1 (PAI-1), and also for treatment and / or prophylaxis of erectile dysfunction and female sexual dysfunction. In addition, the compounds according to the invention are also suitable for treatment and / or prophylaxis of asthmatic disorders, pulmonary arterial hypertension (PAH) and other forms of pulmonary hypertension (PH) including left-heart disease, HIV, sickle cell anaemia, thromboembolisms (CTEPH), sarcoidosis, COPD or pulmonary fibrosis-associated pulmonary hypertension, chronic-obstructive pulmonary disease (COPD), acute respiratory distress syndrome (ARDS), acute lung injury (ALI), alpha-1-antitrypsin deficiency (AATD), pulmonary fibrosis, pulmonary emphysema (for example pulmonary emphysema induced by cigarette smoke) and cystic fibrosis (CF). The compounds described in the present invention are also active compounds for control of central nervous system disorders characterized by disturbances of the NO / cGMP system. They are suitable in particular for improving perception, concentration, learning or memory after cognitive impairments like those occurring in particular in association with situations / diseases / syndromes such as mild cognitive impairment, age-associated learning and memory impairments, age-associated memory losses, vascular dementia, craniocerebral trauma, stroke, dementia occurring after strokes (post stroke dementia), post-traumatic craniocerebral trauma, general concentration impairments, concentration impairments in children with learning and memory problems, Alzheimer’s disease, Lewy body dementia, dementia with degeneration of the frontal lobes including Pick's syndrome, Parkinson’s disease, progressive dementia with corticobasal degeneration, amyolateral sclerosis (ALS), Huntington's disease, demyelinization, multiple sclerosis, thalamic degeneration, Creutzfeld-Jacob dementia, HIV dementia, schizophrenia with dementia or Korsakoff’s psychosis. They are also suitable for treatment and / or prophylaxis of central nervous system disorders such as states of anxiety, tension and depression, CNS-related sexual dysfunctions and sleep disturbances, and for controlling pathological disturbances of the intake of food, stimulants and addictive substances. The compounds according to the invention are furthermore also suitable for controlling cerebral blood flow and thus represent effective agents for controlling migraines. They are also suitable for the prophylaxis and control of sequelae of cerebral infarction (cerebral apoplexy) such as stroke, cerebral ischaemia and craniocerebral trauma. The compounds according to the invention can likewise be used for controlling states of pain and tinnitus. The compounds according to the invention are also suitable for treatment and / or prophylaxis of fibrotic disorders of the internal organs, for example the lung, the heart, the kidney, the bone marrow and in particular the liver, and also dermatological fibroses and fibrotic eye disorders. In the context of the present invention, the term fibrotic disorders includes in particular the following terms: hepatic fibrosis, cirrhosis of the liver, pulmonary fibrosis, endomyocardial fibrosis, nephropathy, glomerulonephritis, interstitial renal fibrosis, fibrotic damage resulting from diabetes, bone marrow fibrosis and similar fibrotic disorders, scleroderma, morphea, keloids, hypertrophic scarring (also following surgical procedures), naevi, diabetic retinopathy, proliferative vitroretinopathy and disorders of the connective tissue (for example sarcoidosis). The compounds according to the invention are also suitable for controlling postoperative scarring, for example as a result of glaucoma operations. The compounds according to the invention can also be used cosmetically for ageing and keratinized skin. Moreover, the compounds according to the invention are suitable for treatment and / or prophylaxis of hepatitis, neoplasms, osteoporosis, glaucoma and gastroparesis. The present invention further provides for the use of the compounds according to the invention for treatment and / or prophylaxis of disorders, especially the disorders mentioned above. The present invention further provides for the use of the compounds according to the invention for the treatment and / or prophylaxis of chronic renal disorders, acute and chronic renal insufficiency, diabetic, inflammatory or hypertensive nephropaties, fibrotic disorders, cardiac insufficiency, angina pectoris, hypertension, pulmonary hypertension, ischemias, vascular disorders, thromboembolic disorders, arteriosclerosis, sickle cell anemia, erectile dysfunction, benign prostate hyperplasia, dysuria associated with benign prostate hyperplasia, Huntington, dementia, Alzheimer and Creutzfeld-Jakob. The present invention further provides a method for treatment and / or prophylaxis of disorders, in particular the disorders mentioned above, using an effective amount of at least one of the compounds according to the invention. The present invention further provides a method for the treatment and / or prophylaxis of chronic renal disorders, acute and chronic renal insufficiency, diabetic, inflammatory or hypertensive nephropathies, fibrotic disorders, cardiac insufficiency, angina pectoris, hypertension, pulmonary hypertension, ischemias, vascular disorders, thromboembolic disorders, arteriosclerosis, sickle cell anemia, erectile dysfunction, benign prostate hyperplasia, dysuria associated with benign prostate hyperplasia, Huntington, dementia, Alzheimer and Creutzfeld-Jakob. In another embodiment, the inventive compounds can also be used to treat or to prevent uterine fibroids (uterine leiomyoma or uterine myoma) in women. Uterine fibroids are benign tumors of the myometrium, the smooth muscle layer of the uterus. Uterine fibroids grow slowly during a women's life, and their growth is dependent on the female sexual hormones estradiol and progesterone [Kawaguchi Ketal. Immunohistochemical analysis of oestrogen receptors, progesterone receptors and Ki-67 in leiomyoma and myometrium during the menstrual cycle and pregnancy Virchows Arch A Pathol Anat Histopathol. 1991 ;419(4):309-15.], therefore the highest prevalence of uterine fibroids with approx. 70% and >80% in white and afro-american women, respectively, is found from 35 years of age onwards to menopause, when they shrink due to reduced hormone levels [Baird DD et al. High cumulative incidence of uterine leiomyoma in black and white women: Ultrasound evidence Am J Obstet Gynecol. 2003 Jan;188(1):100-7.]. Approx 30% and 45% of white and afro-american women, respectively, do show clinically relevant symptoms due to their fibroids, which are heavy menstrual bleeding and pain, which is related to the menstrual cycle [David M et al. Myoma-associated pain frequency and intensity: a retrospective evaluation of 1548 myoma patients. Eur J Obstet Gynecol Reprod Biol. 2016 Apr; 199:137-40], Heavy menstrual bleeding in this respect is defined by a blood loss of more than 80 mL in a menstrual bleeding period [Fraser IS et al. The FIGO Recommendations on Terminologies and Definitions for Normal and Abnormal Uterine Bleeding, Semin Reprod Med 2011; 29(5): 383-390], Submucosal position of the uterine fibroids, e.g. those located directly below the endometrium, seems to have an even more severe effect on uterine bleeding, which may result in anemia in affected women [Yang JH et al. Impact of submucous myoma on the severity of anemia. Fertil Steril. 2011 Apr;95(5): 1769-72], Furthermore, uterine fibroids, due to their symptoms, do severly affect the quality of life of affected women [Downes E et al. The burden of uterine fibroids in five European countries. Eur J Obstet Gynecol Reprod Biol. 2010 Sep;152(1):96-102], So far, it is not understood how uterine fibroids do cause heavy menstrual bleeding. Disregulated genes in uterine fibroids, in comparison to normal myometrium, can give a hint to understand the underlying mechanisms. In published and internal studies, we found TDO2, Tryptophan 2,3-dioxygenase, being highly upregulated [Tsibris JC et al. Insights from gene arrays on the development and growth regulation of uterine leiomyomata. Fertil Steril. 2002 Jul;78(1): 114-21.]. TDO2 metabolizes the substrate L-Tryptophan to L-Kynurenine, which can be further metabolized to kynurenic acid. Both, L-Kynurenine and Kynurenic acid are physiological ligands and activators for the aryl hydrocarbon receptor AHR [Opitz CA et al. An endogenous tumourpromoting ligand of the human aryl hydrocarbon receptor Nature. 2011 Oct 5;478(7368):197-203], L-Kynurenine controls at least two physiological processes which are dysregulated in uterine fibroids. L-Kynurenine, synthesized by an upregulation of IDO (lndoleamine-2,3-dyoxygenase) or TDO2, and acting via the AHR receptor, suppresses the immune system and thus prevents immune cells from recognizing and clearing the tumor cells [Munn DH Blocking IDO activity to enhance anti-tumor immunity. Front Biosci (Elite Ed). 2012 Jan 1;4:734-45], Furthermore, an upregulation of L-Kynurenine leads to a vasodilation of vessels, and thus can directly increase blood loss and bleeding [Wang Y et al. Kynurenine is an endothelium-derived relaxing factor produced during inflammation Nature Medicine 16, 279-285 (2010)]. In summary, the upregulation of L-Kynurenine through activation of its physiological receptor AHR seems to support uterine fibroid growth by local suppression of the immune system, and might cause heavy menstrual bleeding by vasodilation of endometrial vessels in proximity to the tumor. Therefore, a systemic or local application of compounds from the present invention inhibiting activation of the AHR and thus blocking the effect of uterine fibroid derived L-Kynurenine presents a new and valid treatment option for uterine fibroids. Compounds of the present invention can be utilized to inhibit, block, reduce or decrease AHR activation by exogenous and / or endogenous ligands for the reduction of tumour growth and the modulation of dysregulated immune responses e.g. to block immunosuppression and increase immune cell activation and infiltration in the context of cancer and cancer immunotherapy; This method comprises administering to a mammal in need thereof, including a human, an amount of a compound of this invention, or a pharmaceutically acceptable salt, isomer, polymorph, metabolite, hydrate, solvate or ester thereof; which is effective to treat the disorder. The present invention also provides methods of treating a variety of other disorders wherein AHR is involved such as, but not limited to, inflammation, vaccination for infection & cancer, viral infections, obesity and diet-induced obesity, adiposity, metabolic disorders, hepatic steatosis and uterine fibroids. These disorders have been well characterized in humans, but also exist with a similar etiology in other mammals, and can be treated by administering pharmaceutical compositions of the present invention. The term “treating” or “treatment” as used in the present text is used conventionally, e.g., the management or care of a subject for the purpose of combating, alleviating, reducing, relieving, improving the condition of a disease or disorder, such as liquid and solid tumours. In accordance with a further aspect, the present invention covers compounds of general formula (I), as described supra, or stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, particularly pharmaceutically acceptable salts thereof, or mixtures of same, for use in the treatment or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling. The pharmaceutical activity of the compounds according to the invention can be explained by their activity as AHR inhibitors. In accordance with a further aspect, the present invention covers the use of compounds of general formula (I), as described supra, or stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, particularly pharmaceutically acceptable salts thereof, or mixtures of same, for the treatment or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, particularly liquid and solid tumours. In accordance with a further aspect, the present invention covers the use of a compound of formula (I), described supra, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, particularly a pharmaceutically acceptable salt thereof, or a mixture of same, for the prophylaxis or treatment of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, particularly liquid and solid tumours. In accordance with a further aspect, the present invention covers the use of compounds of general formula (I), as described supra, or stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, particularly pharmaceutically acceptable salts thereof, or mixtures of same, in a method of treatment or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, particularly liquid and solid tumours. In accordance with a further aspect, the present invention covers use of a compound of general formula (I), as described supra, or stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, particularly pharmaceutically acceptable salts thereof, or mixtures of same, for the preparation of a pharmaceutical composition, preferably a medicament, for the prophylaxis or treatment of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, particularly liquid and solid tumours. In accordance with a further aspect, the present invention covers a method of treatment or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, particularly liquid and solid tumours, using an effective amount of a compound of general formula (I), as described supra, or stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, particularly pharmaceutically acceptable salts thereof, or mixtures of same. In accordance with a further aspect, the present invention covers pharmaceutical compositions, in particular a medicament, comprising a compound of general formula (I), as described supra, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a salt thereof, particularly a pharmaceutically acceptable salt, or a mixture of same, and one or more excipients), in particular one or more pharmaceutically acceptable excipient(s). Conventional procedures for preparing such pharmaceutical compositions in appropriate dosage forms can be utilized. The present invention furthermore covers pharmaceutical compositions, in particular medicaments, which comprise at least one compound according to the invention, conventionally together with one or more pharmaceutically suitable excipients, and to their use for the above mentioned purposes. It is possible for the compounds according to the invention to have systemic and / or local activity. For this purpose, they can be administered in a suitable manner, such as, for example, via the oral, parenteral, pulmonary, nasal, sublingual, lingual, buccal, rectal, vaginal, dermal, transdermal, conjunctival, otic route or as an implant or stent. For these administration routes, it is possible for the compounds according to the invention to be administered in suitable administration forms. For oral administration, it is possible to formulate the compounds according to the invention to dosage forms known in the art that deliver the compounds of the invention rapidly and / or in a modified manner, such as, for example, tablets (uncoated or coated tablets, for example with enteric or controlled release coatings that dissolve with a delay or are insoluble), orally-disintegrating tablets, films / wafers, films / lyophylisates, capsules (for example hard or soft gelatine capsules), sugar-coated tablets, granules, pellets, powders, emulsions, suspensions, aerosols or solutions. It is possible to incorporate the compounds according to the invention in crystalline and / or amorphised and / or dissolved form into said dosage forms. Parenteral administration can be effected with avoidance of an absorption step (for example intravenous, intraarterial, intracardial, intraspinal or intralumbal) or with inclusion of absorption (for example intramuscular, subcutaneous, intracutaneous, percutaneous or intraperitoneal). Administration forms which are suitable for parenteral administration are, inter alia, preparations for injection and infusion in the form of solutions, suspensions, emulsions, lyophylisates or sterile powders. Examples which are suitable for other administration routes are pharmaceutical forms for inhalation [inter alia powder inhalers, nebulizers], nasal drops, nasal solutions, nasal sprays; tablets / films / wafers / capsules for lingual, sublingual or buccal administration; suppositories; eye drops, eye ointments, eye baths, ocular inserts, ear drops, ear sprays, ear powders, ear-rinses, ear tampons; vaginal capsules, aqueous suspensions (lotions, mixturae agitandae), lipophilic suspensions, emulsions, ointments, creams, transdermal therapeutic systems (such as, for example, patches), milk, pastes, foams, dusting powders, implants or stents. The compounds according to the invention can be incorporated into the stated administration forms. This can be effected in a manner known per se by mixing with pharmaceutically suitable excipients. Pharmaceutically suitable excipients include, inter alia, fillers and carriers (for example cellulose, microcrystalline cellulose (such as, for example, Avicel®), lactose, mannitol, starch, calcium phosphate (such as, for example, Di-Cafos®)), ointment bases (for example petroleum jelly, paraffins, triglycerides, waxes, wool wax, wool wax alcohols, lanolin, hydrophilic ointment, polyethylene glycols), bases for suppositories (for example polyethylene glycols, cacao butter, hard fat), solvents (for example water, ethanol, isopropanol, glycerol, propylene glycol, medium chainlength triglycerides fatty oils, liquid polyethylene glycols, paraffins), surfactants, emulsifiers, dispersants or wetters (for example sodium dodecyl sulfate), lecithin, phospholipids, fatty alcohols (such as, for example, Lanette®), sorbitan fatty acid esters (such as, for example, Span®), polyoxyethylene sorbitan fatty acid esters (such as, for example, Tween®), polyoxyethylene fatty acid glycerides (such as, for example, Cremophor®), polyoxethylene fatty acid esters, polyoxyethylene fatty alcohol ethers, glycerol fatty acid esters, poloxamers (such as, for example, Pluronic®), buffers, acids and bases (for example phosphates, carbonates, citric acid, acetic acid, hydrochloric acid, sodium hydroxide solution, ammonium carbonate, trometamol, triethanolamine), isotonicity agents (for example glucose, sodium chloride), adsorbents (for example highly-disperse silicas), viscosity-increasing agents, gel formers, thickeners and / or binders (for example polyvinylpyrrolidone, methylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, carboxymethylcellulose-sodium, starch, carbomers, polyacrylic acids (such as, for example, Carbopol®); alginates, gelatine), disintegrants (for example modified starch, carboxymethylcellulose-sodium, sodium starch glycolate (such as, for example, Explotab®), cross- linked polyvinylpyrrolidone, croscarmellose-sodium (such as, for example, AcDiSol®)), flow regulators, lubricants, glidants and mould release agents (for example magnesium stearate, stearic acid, talc, highly-disperse silicas (such as, for example, Aerosil®)), coating materials (for example sugar, shellac) and film formers for films or diffusion membranes which dissolve rapidly or in a modified manner (for example polyvinylpyrrolidones (such as, for example, Kollidon®), polyvinyl alcohol, hydroxypropylmethylcellulose, hydroxypropylcellulose, ethylcellulose, hydroxypropylmethylcellulose phthalate, cellulose acetate, cellulose acetate phthalate, polyacrylates, polymethacrylates such as, for example, Eudragit®)), capsule materials (for example gelatine, hydroxypropylmethylcellulose), synthetic polymers (for example polylactides, polyglycolides, polyacrylates, polymethacrylates (such as, for example, Eudragit®), polyvinylpyrrolidones (such as, for example, Kollidon®), polyvinyl alcohols, polyvinyl acetates, polyethylene oxides, polyethylene glycols and their copolymers and blockcopolymers), plasticizers (for example polyethylene glycols, propylene glycol, glycerol, triacetine, triacetyl citrate, dibutyl phthalate), penetration enhancers, stabilisers (for example antioxidants such as, for example, ascorbic acid, ascorbyl palmitate, sodium ascorbate, butylhydroxyanisole, butylhydroxytoluene, propyl gallate), preservatives (for example parabens, sorbic acid, thiomersal, benzalkonium chloride, chlorhexidine acetate, sodium benzoate), colourants (for example inorganic pigments such as, for example, iron oxides, titanium dioxide), flavourings, sweeteners, flavour- and / or odour-masking agents. The present invention furthermore relates to a pharmaceutical composition which comprise at least one compound according to the invention, conventionally together with one or more pharmaceutically suitable excipient(s), and to their use according to the present invention. In accordance with another aspect, the present invention covers pharmaceutical combinations, in particular medicaments, comprising at least one compound of general formula (I) of the present invention and at least one or more further active ingredients, in particular for the treatment and / or prophylaxis of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signalinggeneric name disorders, particularly liquid and solid tumours. The term “combination” in the present invention is used as known to persons skilled in the art, it being possible for said combination to be a fixed combination, a non-fixed combination or a kit-of-parts. A “fixed combination” in the present invention is used as known to persons skilled in the art and is defined as a combination wherein, for example, a first active ingredient, such as one or more compounds of general formula (I) of the present invention, and a further active ingredient are present together in one unit dosage or in one single entity. One example of a “fixed combination” is a pharmaceutical composition wherein a first active ingredient and a further active ingredient are present in admixture for simultaneous administration, such as in a formulation. Another example of a “fixed combination” is a pharmaceutical combination wherein a first active ingredient and a further active ingredient are present in one unit without being in admixture. A non-fixed combination or “kit-of-parts” in the present invention is used as known to persons skilled in the art and is defined as a combination wherein a first active ingredient and a further active ingredient are present in more than one unit. One example of a non-fixed combination or kit-of-parts is a combination wherein the first active ingredient and the further active ingredient are present separately. It is possible for the components of the non-fixed combination or kit-of-parts to be administered separately, sequentially, simultaneously, concurrently or chronologically staggered. Based upon standard laboratory techniques known to evaluate compounds useful for the treatment of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, by standard toxicity tests and by standard pharmacological assays for the determination of treatment of the conditions identified above in mammals, and by comparison of these results with the results of known active ingredients or medicaments that are used to treat these conditions, the effective dosage of the compounds of the present invention can readily be determined for treatment of each desired indication. The amount of the active ingredient to be administered in the treatment of one of these conditions can vary widely according to such considerations as the particular compound and dosage unit employed, the mode of administration, the period of treatment, the age and sex of the patient treated, and the nature and extent of the condition treated. The total amount of the active ingredient to be administered will generally range from about 0.001 mg / kg to about 200 mg / kg body weight per day, and preferably from about 0.01 mg / kg to about 20 mg / kg body weight per day. Clinically useful dosing schedules will range from one to three times a day dosing to once every four weeks dosing. In addition, it is possible for "drug holidays", in which a patient is not dosed with a drug for a certain period of time, to be beneficial to the overall balance between pharmacological effect and tolerability. It is possible for a unit dosage to contain from about 0.5 mg to about 1500 mg of active ingredient, and can be administered one or more times per day or less than once a day. The average daily dosage for administration by injection, including intravenous, intramuscular, subcutaneous and parenteral injections, and use of infusion techniques will preferably be from 0.01 to 200 mg / kg of total body weight. The average daily rectal dosage regimen will preferably be from 0.01 to 200 mg / kg of total body weight. The average daily vaginal dosage regimen will preferably be from 0.01 to 200 mg / kg of total body weight. The average daily topical dosage regimen will preferably be from 0.1 to 200 mg administered between one to four times daily. The transdermal concentration will preferably be that required to maintain a daily dose of from 0.01 to 200 mg / kg. The average daily inhalation dosage regimen will preferably be from 0.01 to 100 mg / kg of total body weight. Of course the specific initial and continuing dosage regimen for each patient will vary according to the nature and severity of the condition as determined by the attending diagnostician, the activity of the specific compound employed, the age and general condition of the patient, time of administration, route of administration, rate of excretion of the drug, drug combinations, and the like. The desired mode of treatment and number of doses of a compound of the present invention or a pharmaceutically acceptable salt or ester or composition thereof can be ascertained by those skilled in the art using conventional treatment tests. EXPERIMENTAL SECTION NMR peak forms are stated as they appear in the spectra, possible higher order effects have not been considered. The multiplicities are stated according to the signal form which appears in the spectrum, NMR-spectroscopic effects of a higher order were not taken into consideration. Multiplicity of the NMR signals: s = singlet, d = doublet, t = triplet, q = quartet, qi, quin = quintet, b, br = broad signal, m = multiplet. NMR signals: shift in ppm. Combinations of multiplicity could be e.g. dd = doublet from doublet. Chemical names were generated using the ACD / Name software from ACD / Labs. In some cases generally accepted names of commercially available reagents were used in place of ACD / Name generated names. Table 1 lists the abbreviations used in this paragraph and in the Examples section as far as they are not explained within the text body. Other abbreviations have their meanings customary per se to the skilled person. Table 1: Abbreviations ACN acetonitrile AcOH acetic acid BPR Back Pressure Regulator CDCI3 deuterochloroform DAD diode array detector DCM dichloromethane DEA diethylamine DIPEA N,N-diisopropylethylamine DMA N,N-dimethylacetamide DME 1,2-dimethoxyethane DMF N,N-dimethylformamide DMSO-d6 deuterated dimethyl sulfoxide DMSO dimethyl sulfoxide EtOAc ethyl acetate EtOH ethanol Eq ESI equivalent electrospray ionisation Expl. HATU example (7-aza-1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate HBTU O-benzotriazole- N, N, N’, N’-tetramethyl uroni um hexafluorophosphate HPLC high-pressure liquid chromatography KA kynurenic acid LCMS liquid chromatography coupled with mass spectrometry LPS lipopolysaccharide mL milliliter min. minute(s) M molar WO 2021 / 028382 PCT / EP2020 / 072377 mCPBA meta chloro perbenzoic acid MeLi methyl lithium MS mass spectrometry MTBE methyl tert-butyl ether MTP microtiter plate n-BuLi n-butyl lithium NMP N-methyl-2-pyrrolidone P PBMC pressure peripheral blood mononuclear cells Pd2(dba)3 Pd / C tris(dibenzylideneacetone)dipalladium(0) Palladium on activated charcoal (10% with 50% water) PLC pressure liquid chromatography PyBOB (benzotriazol-1 -yl)oxytripyrrolidinophosphonium hexafluorophosphate RP-HPLC reverse-phase high-pressure liquid chromatography Rt retention time rt, r.t. room temperature sat. saturated T3P 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphorinane 2,4,6-trioxide tBuBrettPhos Pd G3 [(2-Di-tert-butylphosphino-3,6-dimethoxy-2',4',6'-triisopropyl-1,1 biphenyl)-2-(2'-amino-1,T-biphenyl)]palladium(ll) methanesulfonate tBuBrettPhos 2-(Di-tert-butylphosphino)-2',4',6'-triisopropyl-3,6-dimethoxy- 1,1 '-biphenyl TEA triethylamine THF tetrahydrofuran TFA trifluoroacetic acid TLC thin layer chromatography TNFa tumour necrosis factor alpha pM UPLC micromolar Ultra high performance chromatography Xantphos 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene Xphos XPhos Pd G1 2-dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl [2-(2-aminoethyl)phenyl](chloro)palladium-dicyclohexyl(2',4',6'-triisopropyl[biphenyl]-2-yl)phosphine (1:1) XPhos Pd G4 methanesulfonato(2-dicyclohexylphosphino-2',4',6'-tri-iso-propy- 1,1'-biphenyl)(2'-methylamino-1,T-biphenyl-2-yl)palladium(ll) The various aspects of the invention described in this application are illustrated by the following examples which are not meant to limit the invention in any way. The example testing experiments described herein serve to illustrate the present invention and the invention is not limited to the examples given. EXPERIMENTAL SECTION - GENERAL PART All reagents, for which the synthesis is not described in the experimental part, are either commercially available, or are known compounds or may be formed from known compounds by known methods by a person skilled in the art. The compounds and intermediates produced according to the methods of the invention may require purification. Purification of organic compounds is well known to the person skilled in the art and there may be several ways of purifying the same compound. In some cases, no purification may be necessary. In some cases, the compounds may be purified by crystallization. In some cases, impurities may be stirred out using a suitable solvent. In some cases, the compounds may be purified by chromatography, particularly flash column chromatography, using for example prepacked silica gel cartridges, e.g. Biotage SNAP cartidges KP-Sil® or KP-NH® in combination with a Biotage autopurifier system (SP4® or Isolera Four®) and eluents such as gradients of hexane / ethyl acetate or DCM / methanol. In some cases, the compounds may be purified by preparative HPLC using for example a Waters autopurifier equipped with a diode array detector and / or on-line electrospray ionization mass spectrometer in combination with a suitable prepacked reverse phase column and eluents such as gradients of water and acetonitrile which may contain additives such as trifluoroacetic acid, formic acid or aqueous ammonia. In some cases, purification methods as described above can provide those compounds of the present invention which possess a sufficiently basic or acidic functionality in the form of a salt, such as, in the case of a compound of the present invention which is sufficiently basic, a trifluoroacetate or formate salt for example, or, in the case of a compound of the present invention which is sufficiently acidic, an ammonium salt for example. A salt of this type can either be transformed into its free base or free acid form, respectively, by various methods known to the person skilled in the art, or be used as salts in subsequent biological assays. It is to be understood that the specific form (e.g. salt, free base etc.) of a compound of the present invention as isolated and as described herein is not necessarily the only form in which said compound can be applied to a biological assay in order to quantify the specific biological activity. UPLC / MS-Methods Method 1: WO 2021 / 028382 PCT / EP2020 / 072377 Instrument: Waters Acquity LIPLCMS SingleQuad; Column: Acquity LIPLC BEH C18 1.7 pm, 50x2.1mm; eluent A: water+ 0.1 vol % formic acid (99%), eluent B: acetonitrile; gradient: 0-1.6 min 1-99% B, 1.6-2.0 min 99% B; flow 0.8 mL / min; temperature: 60 °C; DAD scan: 210-400 nm. Method 2 : Instrument: Waters Acquity LIPLCMS SingleQuad; Column: Acquity LIPLC BEH C18 1.7 pm, 50x2.1mm; eluent A: water + 0.2 vol % aqueous ammonia (32%), eluent B: acetonitrile; gradient: 0-1.6 min 1-99% B, 1.6-2.0 min 99% B; flow 0.8 mL / min; temperature: 60 °C; DAD scan: 210400 nm. Method 3: Column: XBridge BEH C18 2.5 pm 2.1 x 50 mm; Run Time: 4.70 min; Solvents: A) 10 mM ammonium bicarbonate pH 10, B) MeCN; Gradient: 2-98% B in 4.00 min, hold at 98% B to 4.70 min Method 4: Instrument: Waters Acquity LIPLCMS SingleQuad; Column: Acquity LIPLC BEH C18 1.7 pm, 50x2.1mm; eluent A: water+ 0.1 vol % formic acid (99%), eluent B: acetonitrile; gradient: 0-1.7 min 1-45% B, 1.7-1.72 min 45-99% B, 1.72-2.0 min 99% B; flow 0.8 ml / min; temperature: 60 °C; DAD scan: 210-400 nm. Method 5: Instrument: Waters Acquity LIPLCMS SingleQuad; Column: Acquity LIPLC CSH C18 1.7pm 50x2.1mm; eluent A: water + 0.2 vol % aqueous ammonia (32%), eluent B: acetonitrile; gradient: 0-1.6 min 1-99% B, 1.6-2.0 min 99% B; flow 0.8 ml / min; temperature: 60 °C; DAD scan: 210400 nm. EXPERIMENTAL SECTION - INTERMEDIATES Intermediate 1 methyl (2-cyanophenyl)carbamate NH 0^0 CH3 2-Aminobenzonitrile (CAS 1885-29-6, 3.84 g, 32.5 mmol) and potassium carbonate (13.5 g, 97.5 mmol) were solubilised in tetrahydrofuran (190 mL) and methyl carbonochloridate (CAS 79-221, 5.0 mL, 65 mmol) was added. The mixture was stirred at 80 °C overnight. The mixture was filtered, washed wih tetrahydrofuran and concentrated under reduced pressure to give 6.01 g (80 % purity, 84 % yield) of the title compound. LC-MS (Method 2): Rt = 0.77 min; MS (ESIneg): m / z = 175 [M-H]- 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.69 (s, 3H), 7.33 (td, 1H), 7.52 (d, 1H), 7.63-7.71 (m, 1H), 7.79 (dd, 1H), 9.77 (s, 1H). Intermediate 2 ethyl (2-cyano-6-fluorophenyl)carbamate 2-Amino-3-fluorobenzonitrile (500 mg, 3.67 mmol) was stirred in ethyl carbonochloridate (7.0 mL, 73 mmol) overnight at 100°C. The mixture was cooled to rt and concentrated under reduced pressure LC-MS (method 2): Rt = 0.81 min; MS (ESIneg): m / z = 207 [M-H]- 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.23 (t, 3H), 4.13 (q, 2H), 7.45 - 7.52 (m, 1H), 7.65 -7.74 (m, 2H), 9.70 (brs, 1H). Intermediate 3 methyl (2-cyano-6-methylphenyl)carbamate 2-Amino-3-methylbenzonitrile (1.00 g, 7.57 mmol) and potassium carbonate (3.14 g, 22.7 mmol) were solubilised in toluene and methyl carbonochloridate (1.2 ml, 15 mmol) was added. The mixture was stirred at 80°C overnight and 24 h at 120°C. The mixture was cooled to rt and filtered. The solid was washed with DCM and the filtrate was concentrated under reduced pressure to give 1.55 g (90 % purity, 97 % yield) of the tilte compound. The compound was used without further purification. LC-MS (method 2): Rt = 0.78 min; MS (ESIpos): m / z = 191 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.23 (s, 3H), 3.62 - 3.69 (m, 3H), 7.35 (t, 1H), 7.57 -7.62 (m, 1H), 7.67 (d, 1H), 9.42 - (s 1H). Intermediate 4 methyl (2-cyano-5-methylphenyl)carbamate i CH3 2-Amino-4-methylbenzonitrile (1.00 g, 7.57 mmol) and potassium carbonate (3.14 g, 22.7 mmol) were solubilised in THF (19 mL) and methyl carbonochloridate (1.2 mL, 15 mmol) was added. The mixture was stirred at 80°C overnight. The reactiom mixture was cooled to rt and filtered. The solid was washed wih THF and the filtrate concentrated under reduced pressure to give 1.50 g (95 % purity, 99 % yield) of the title compound without further purification. LC-MS (method 2): Rt = 0.92 min; MS (ESIneg): m / z = 189 [M-H]’ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.36 (s, 3H), 3.68 (s, 3H), 7.13 - 7.17 (m, 1H), 7.33 (s, 1H), 7.67 (d, 1H), 9.69 (s, 1H). Intermediate 5 methyl (2-cyano-5-fluorophenyl)carbamate 0^0 CH3 2-Amino-4-fluorobenzonitrile (1.00 g, 7.35 mmol) and potassium carbonate (3.05 g, 22.0 mmol) were solubilised in toluene (20 mL) and methyl carbonochloridate (1.1 mL, 15 mmol) was added. The mixture was stirred at 120°C overnight. The mixture was cooled to rt and filtered. The solid was washed with toluene and the filtrate was concentrated under reduced pressure to give 1g (72% yield) of the title compound. The compound was used without further purification. LC-MS (Method 2): Rt = 0.87 min; MS (ESIneg): m / z = 193 [M-H]- 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.71 (s, 3H), 7.21 (td, 1H), 7.47 (dd, 1H), 7.90 (dd, 1H), 9.98 (s, 1H). Intermediate 6 methyl (2-cyano-4-methylphenyl)carbamate 2-Amino-5-methylbenzonitrile (1.00 g, 7.57 mmol) and potassium carbonate (3.14 g, 22.7 mmol) were solubilised in THF (19 mL) and methyl carbonochloridate (1.2 mL, 15 mmol) was added. The mixture was stirred at 80°C overnight. The reaction mixture was cooled to rt and filtered. The solid was washed washed with THF and the filtrate was concentrated under reduced pressure to give 1.55 g (95 % purity, 102 % yield) of the tilte compound. LC-MS (method 2): Rt = 0.93 min; MS (ESIpos): m / z = 191 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.31 (s, 3H), 3.67 (s, 3H), 7.37 (d, 1H), 7.46 - 7.50 (m, 1H), 7.61 (dd, 1H), 9.64 (s, 1H). Intermediate 7 methyl (2-cyano-4-fluorophenyl)carbamate I ch3 2-Amino-5-fluorobenzonitrile (1.00 g, 7.35 mmol) and potassium carbonate (3.05 g, 22.0 mmol) were solubilised in THF (20 mL) and methyl carbonochloridate (1.1 mL, 15 mmol) was added. The mixture was stirred at 80°C overnight. The mixture was cooled to rt and filtered. The solid 5 was washed with THF and the filtrate was concentrated under reduced pressure to give 1.6 g of the title compound. The compound was used without further purification. LC-MS (Method 2): Rt = 0.81 min; MS (ESIneg): m / z = 193 [M-Hp 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.68 (s, 3H), 7.49 - 7.62 (m, 2H), 7.82 (dd, 1H), 9.77 (s, 1H). 10 Intermediate 8 ethyl (3-bromo-2-cyanophenyl)carbamate CH3 2-Amino-6-bromobenzonitrile (1.50 g, 7.61 mmol) was stirred in ethyl carbonochloridate (11 mL, 110 mmol) for 6h at reflux. The reaction mixture was cooled to rt and and concentrated under 15 reduced pressure to give 2.21 g of the tilte compound. The compound was used without further purification. LC-MS (method 2): Rt = 1.05 min; MS (ESIneg): m / z = 267 [M-Hp Intermediate 9 ethyl (3-chloro-2-cyanophenyl)carbamate 2-Amino-6-chlorobenzonitrile (1.75 g, 11.5 mmol) was stirred in ethyl carbonochloridate (20 mL, 210 mmol) for 6h at reflux. The mixture was cooled to rt and concentrated under reduced pressure to give 3.00 g of the crude title compound. The compound was used without further 5 purification. LC-MS (method 2): Rt = 1.06 min; MS (ESIneg): m / z = 223 [M-H]’ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.25 (t, 3H), 4.16 (q, 2H), 7.51 (d, 2H), 7.68 (dd, 1H), 9.95 (s, 1H). Intermediate 10 10 ethyl [2-cyano-3-(trifluoromethyl)phenyl]carbamate 2-Amino-6-(trifluoromethyl)benzonitrile (500 mg, 2.69 mmol) was stirred in ethyl carbonochloridate (5.0 mL, 52 mmol) for 4h at reflux. The reaction mixture was cooled to rt and concentrated under reduced pressure to give 740 mg of the crude title compound. The 15 compound was used without further purification. LC-MS (method 2): Rt = 1.10 min; MS (ESIneg): m / z = 257 [M-H]’ Intermediate 11 2-amino-6-cyclopropylbenzonitrile 2-Amino-6-bromobenzonitrile (500 mg, 2.54 mmol) was solubilised in 1,4-dioxane (25 mL). Cyclopropylboronic acid (262 mg, 3.05 mmol), cesium carbonate (71 pL, 10 mmol) and bis(diphenylphosphino)ferrocene-dichlorpalladium(ll)-dichlormethane complex (414 mg, 508 pmol) were added and the reaction was stirred for 10min at 130°C under microwave irradiation. The reaction mixture was filtered and the solid was washed with dioxane. The filtrate was concentrated under reduced pressure to give 748 mg of the title compounds. The copmpound was used without further purification. LC-MS (method 2): Rt = 0.99 min; MS (ESIneg): m / z = 157 [M-H]’ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 0.65 - 0.71 (m, 2H), 0.96 - 1.03 (m, 2H), 1.94 - 2.05 (m, 1H), 5.90 (s, 2H), 6.15 (d, 1H), 6.56 (dd, 1H), 7.15 (t, 1H). Intermediate 12 ethyl (2-cyano-3-cyclopropylphenyl)carbamate CH3 2-Amino-6-cyclopropylbenzonitrile (700 mg, 4.42 mmol) was stirred in ethyl carbonochloridate (6.3 mL, 66 mmol) for 4h at reflux. The reaction mixture was cooled to rt and concentrated under reduced pressure to give 901 mg (88 % yield) of the title compound.The compound was used without further purification LC-MS (method 2): Rt = 1.11 min; MS (ESIpos): m / z = 231 [M+H]+ Intermediate 13 methyl (2-cyano-3-methylphenyl)carbamate ch3 2-Amino-6-methylbenzonitrile (500 mg, 3.78 mmol) and potassium carbonate (1.57 g, 11.3 mmol) were solubilised in THF (9.6 mL) and methyl carbonochloridate (580 pL, 7.6 mmol) was carefully added. The mixture was stirred at 80°C overnight. The reaction mixture was cooled to rt and filtered. The solid was washed with THF and the filtrate was concentrated under reduced pressure to give 788 mg of the title compound. The compound was used without further purification. LC-MS (method 2): Rt = 0.89 min; MS (ESIneg): m / z = 189 [M-H]’ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.46 (s, 3H), 3.68 (s, 3H)., 7.24 (d, 1H), 7.33 (d, 1H), 7.50-7.58 (m, 1H), 9.69 (s, 1H). Intermediate 14 methyl (2-cyano-3-fluorophenyl)carbamate F 1 NH o^o ch3 2-Amino-6-fluorobenzonitrile (150 mg, 1.10 mmol) and potassium carbonate (457 mg, 3.31 mmol) were stirred in toluene (2.8 mL) and methyl carbonochloridate (170 pl, 2.2 mmol) was added. The mixture was stirred at 120°C overnight. The reaction mixture was cooled to rt and filtered. The filtrate was concentrated under reduced pressure to give 52 mg (100% purifty, 24% yield) of the tilte compound. The compound was used without further purification. LC-MS (Method 2): Rt = 0.83 min; MS (ESIpos): m / z = 193 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.70 (s, 3H), 7.22 - 7.31 (m, 1H), 7.39 (d, 1H), 7.72 (td, 1H), 10.04 (s, 1H). Intermediate 15 2-phenyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (2.00 g, 11.4 mmol) and benzohydrazide (CAS 613-94-5, 1.85 g, 13.6 mmol) were stirred in N-methylpyrrolidone (50 mL) at 120°C for 4 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60°C to give 2.09 g (90 % purity, 63 % yield) of the title compound. LC-MS (Method 2): Rt = 0.66 min; MS (ESIpos): m / z = 263 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.39 - 7.49 (m, 2H), 7.54 - 7.61 (m, 3H), 7.69 - 7.76 (m, 1H), 8.21 - 8.27 (m, 3H), 12.34 (s, 1H) Intermediate 16 5-chloro-2-phenyl[1,2,4]triazolo[1,5-c]quinazoline 2-Phenyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (2.10 g, 8.02 mmol) was solubilised in phosphorus(V) oxychloride (40 mL, 430 mmol), N,N-diisopropylethylamine (2.8 mL, 16 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was concentrated and the residue was diluted with dichloromethane. Precipitated product was filtered off and washed with dichloromethane to give 1.83 g (100 % purity, 81 % yield) of the title compound. C-MS (Method 2): Rt = 1.39 min; MS (ESIpos): m / z = 281 [M+H]+ 1H-NMR (500MHz, DMSO-d6): 5 [ppm]= 7.59 - 7.64 (m, 3H), 7.87 (td, 1H), 7.96 - 8.01 (m, 1H), 8.03 - 8.07 (m, 1H), 8.29 - 8.33 (m, 2H), 8.53 (dd, 1H) Intermediate 17 2-(4-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (129 mg, 733 pmol) and 4-chlorobenzohydrazide (CAS 53640-3, 150 mg, 879 pmol) were stirred in N-methylpyrrolidone (3.2 mL) at 120 °C for 4 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 265 mg (90 % purity, 110 % yield) of the title compound. LC-MS (Method 2): Rt = 0.80 min; MS (ESIpos): m / z = 297 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.39 - 7.49 (m, 2H), 7.63 - 7.68 (m, 2H), 7.72 (ddd, 1H), 8.20 - 8.26 (m, 3H), 12.38 (br s, 1H) Intermediate 18 5-chloro-2-(4-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazoline Cl ^^^N^CI 2-(4-Chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (430 mg, 1.45 mmol) was solubilised in phosphorus(V) oxychloride (22 mL, 230 mmol), N,N-diisopropylethylamine (2.5 mL, 14 mmol) was added carefully and the mixture was stirred overnight at 110°C. The mixture was concentrated and the residue was diluted with dichloromethane. Precipitated product was filtered off and washed with dichloromethane to give 518 mg (113 % yield) of the title compound. LC-MS (Method 2): Rt = 1.53 min; MS (ESIpos): m / z = 315 [M+H]+ 1H-NMR (400 MHz, DMSO-d6) 6 [ppm]: 1.207 (0.47), 1.218 (1.66), 1.234 (1.88), 1.252 (15.57), 1.269 (16.00), 1.273 (11.31), 1.288 (15.50), 1.305 (14.52), 3.072 (0.63), 3.083 (0.82), 3.091 (1.92), 3.101 (2.04), 3.109 (2.03), 3.119 (1.91), 3.138 (0.63), 3.492 (0.74), 3.519 (0.76), 3.549 (2.19), 3.563 (1.30), 3.577 (3.13), 3.589 (1.76), 3.596 (1.43), 3.606 (1.26), 3.622 (0.50), 5.944 (1.56), 7.416 (0.48), 7.481 (0.44), 7.501 (0.52), 7.631 (0.99), 7.652 (1.10), 7.665 (1.19), 7.686 (1.24), 7.718 (0.41), 7.870 (0.50), 7.983 (0.46), 8.034 (0.69), 8.209 (0.61), 8.215 (1.14), 8.236 (1.03), 8.287 (1.20), 8.308 (1.14), 8.504 (0.49), 8.523 (0.47), 9.428 (0.44), 12.433 (0.60). Intermediate 19 2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one F H Methyl (2-cyanophenyl)carbamate (150 mg, 851 pmol) and 3-fluorobenzohydrazide (CAS 49955-8, 197 mg, 1.28 mmol) were stirred in N,N-dimethylformamide (3.0 mL) at 120 °C overnight. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 221 mg (98 % purity, 91 % yield) of the title compound. LC-MS (Method 2): Rt = 0.67 min; MS (ESIpos): m / z = 281 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.37 - 7.49 (m, 3H), 7.64 (td, 1H), 7.73 (ddd, 1H), 7.90 - 7.98 (m, 1H), 8.08 (dt, 1H), 8.24 (dd, 1H), 12.39 (brs, 1H) Intermediate 20 5-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline F 2-(3-Fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (1.35 g, 4.82 mmol) was solubilised in phosphorus(V) oxychloride (10 mL, 110 mmol), N,N-diisopropylethylamine (8.4 mL, 48 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was concentrated and the residue was diluted with dichloromethane. Precipitated product was filtered off and washed with dichloromethane to give 1.27 g (99 % purity, 87 % yield) of the title compound. LC-MS (Method 2): Rt = 1.42 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.43-7.49 (m, 1H), 7.67 (td, 1H), 7.88 (ddd, 1H), 7.96 - 8.02 (m, 2H), 8.03-8.07 (m, 1H), 8.15 (dt, 1H), 8.50-8.56 (m, 1H) Intermediate 21 2-(1-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one H Methyl (2-cyanophenyl)carbamate (1.04 g, 5.93 mmol) and 1 -methyl-1 H-pyrazole-4-carbohydrazide (CAS 170020-91-4, 831 mg, 5.93 mmol) were stirred in N,N-dimethylformamide (21 mL) at 120 °C for 20 hours. Waterwas added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 943 mg (95 % purity, 57 % yield) of the title compound. LC-MS (Method 2): Rt = 0.47 min; MS (ESIpos): m / z = 267 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.94 (s, 3H), 7.36 - 7.42 (m, 1H), 7.44 (d, 1H), 7.70 (ddd, 1H), 8.01 (d, 1H), 8.16 (dd, 1H), 8.42 (s, 1H), 12.26 (s 1H) Intermediate 22 5-chloro-2-(1-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(1-Methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (943 mg, 3.54 mmol) was solubilised in phosphorus(V) oxychloride (10 mL, 107 mmol), N,N-diisopropylethylamine (6.2 mL, 35 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was concentrated and the residue was diluted with dichloromethane. Precipitated product was filtered off and washed with dichloromethane to give 963 mg (96 % purity, 92 % yield) of the title compound. LC-MS (Method 2): Rt = 0.97 min; MS (ESIpos): m / z = 285 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.96 (s, 3H), 7.84 (ddd, 1H), 7.96 (td, 1H), 7.99 - 8.04 (m, 1H), 8.09 (s, 1H), 8.45 (dd, 1H), 8.53 (s, 1H) Intermediate 23 2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one h3c O H Methyl (2-cyanophenyl)carbamate (2.00 g, 11.4 mmol) and 4-methoxybenzohydrazide (CAS 3290-99-1, 1.89 g, 11.4 mmol) were stirred in N,N-dimethylformamide (40 mL) at 120 °C for 20 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 3.23 g (95 % purity, 93 % yield) of the title compound. LC-MS (Method 2): Rt = 0.69 min; MS (ESIpos): m / z = 293 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.85 (s, 3H), 7.10 - 7.15 (m, 2H), 7.37 - 7.47 (m, 2H), 7.71 (ddd, 1H), 8.14-8.19 (m, 2H), 8.22 (dd, 1H), (NH proton is not visible) Intermediate 24 5-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline h3c 0 2-(4-Methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (305 mg, 1.00 mmol) was solubilised in phosphorus(V) oxychloride (5 mL, 54 mmol), N,N-diisopropylethylamine (1.8 mL, 10 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was concentrated and the residue was diluted with dichloromethane. Precipitated product was filtered off and washed with dichloromethane to give 173 mg (100 % purity, 53 % yield) of the title compound. LC-MS (Method 2): Rt = 1.38 min; MS (ESIpos): m / z = 311 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.87 (s, 3H), 7.12 - 7.18 (m, 2H), 7.86 (td, 1H), 7.97 (td, 1H), 8.01 - 8.06 (m, 1H), 8.20 - 8.27 (m, 2H), 8.51 (dd, 1H) Intermediate 25 2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline-5(6H)-thione h3c 0 2-lsothiocyanatobenzonitrile (CAS 81431-98-3, 100.0 mg, 624 pmol) and 4- methoxybenzohydrazide (CAS 3290-99-1, 103.4 mg, 624 pmol) were solubilised in isopropanol (20 mL, 261 mmol) and the mixture was stirred at reflux for 8 hours. The reaction was filtered and washed with isopropanol to give 177 mg (75 % purity, 69 % yield) of the title compound. LC-MS (method 2): Rt = 0.63 min; MS (ESIpos): m / z = 309 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.86 (s, 3H), 7.14 (d, 2H), 7.51 - 7.58 (m, 1H), 7.67 (d, 1H), 7.75-7.84 (m, 1H), 8.16-8.22 (m, 2H), 8.28 (dd, 1H), 13.96 (brs, 1H) Intermediate 26 2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (500 mg, 2.84 mmol) and 2-methylbenzohydrazide (CAS 7658-80-2, 426 mg, 2.84 mmol) were stirred in N,N-dimethylformamide (130 mL) at 120 °C for 20 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 666 mg (79 % purity, 67 % yield) of the title compound. LC-MS (Method 2): Rt = 0.72 min; MS (ESIpos): m / z = 277 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.70 (s, 3H), 7.35 - 7.48 (m, 5H), 7.72 (ddd, 1H), 8.09 - 8.14 (m, 1H), 8.23 (dd, 1H), 12.3 (s, 1H) Intermediate 27 5-chloro-2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(2-Methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (666 mg, 2.41 mmol) was solubilised in phosphorus(V) oxychloride (11 mL, 120 mmol), N,N-diisopropylethylamine (4.2 mL, 24 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was concentrated and the residue was diluted with dichloromethane. Precipitated product was filtered off and washed with dichloromethane to give 648 mg (100 % purity, 91 % yield) of the title compound. LC-MS (Method 2): Rt = 1.47 min; MS (ESIpos): m / z = 295 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.75 (s, 3H), 7.36 - 7.51 (m, 3H), 7.87 (ddd, 1H), 7.94 -8.00 (m, 1H), 8.03 - 8.07 (m, 1H), 8.13 - 8.21 (m, 1H), 8.52 (dd, 1H). Intermediate 28 2-[2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (250 mg, 1.42 mmol) and 2-(trifluoromethyl)benzohydrazide (CAS 344-95-6, 348 mg, 1.70 mmol) were stirred in N,N-dimethylformamide (3 mL) at 120 °C for 15 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 401 mg (86 % yield) of the title compound. LC-MS (Method 2): Rt = 0.70 min; MS (ESIpos): m / z = 331 [M+H]+ 1H-NMR (400 MHz, DMSO-d6) 5 [ppm]: 1.229 (0.63), 2.331 (2.77), 2.518 (11.72), 2.523 (7.45), 2.727 (3.41), 2.888 (4.04), 2.934 (0.55), 3.072 (2.77), 3.365 (1.35), 3.383 (0.55), 3.868 (1.50), 6.834 (1.66), 6.852 (3.09), 6.870 (1.90), 6.872 (1.90), 6.925 (3.01), 6.944 (3.41), 7.022 (7.60), 7.042 (8.55), 7.049 (3.80), 7.070 (2.53), 7.097 (5.15), 7.099 (5.07), 7.117 (10.06), 7.135 (6.42), 7.138 (5.78), 7.181 (0.71), 7.261 (0.71), 7.284 (2.14), 7.287 (2.38), 7.305 (2.85), 7.322 (1.58), 7.325 (1.43), 7.400 (2.38), 7.402 (2.53), 7.421 (4.99), 7.429 (4.36), 7.438 (3.80), 7.440 (3.96), 7.450 (6.89), 7.465 (6.18), 7.485 (5.78), 7.511 (3.09), 7.566 (0.71), 7.648 (1.19), 7.667 (2.61), 7.685 (2.30), 7.699 (3.01), 7.716 (10.77), 7.733 (12.28), 7.736 (12.75), 7.748 (10.22), 7.774 (8.79), 7.792 (8.00), 7.800 (6.89), 7.820 (5.15), 7.840 (10.69), 7.859 (8.71), 7.885 (2.61), 7.904 (1.19), 7.953 (5.39), 7.965 (9.82), 7.985 (8.63), 8.006 (0.79), 8.101 (0.48), 8.175 (3.96), 8.178 (4.20), 8.195 (3.96), 8.198 (3.64), 10.172 (1.74), 10.571 (3.09), 10.662 (16.00), 10.909 (1.82), 11.254 (0.55). Intermediate 29 5-chloro-2-[2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazoline 2-[2-(Trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (401 mg, 1.21 mmol) was solubilised in phosphorus(V) oxychloride (4.0 mL, 43 mmol), N,N-diisopropylethylamine (2.1 mL, 12 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was poured into ice and stirred for one hour. Precipitated product was filtered off, washed with water and dried at 60 °C under reduced pressure to give 232 mg (55 % yield) of the title compound. LC-MS (Method 2): Rt = 1.38 min; MS (ESIpos): m / z = 349 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.81 - 7.86 (m, 1H), 7.88 - 7.93 (m, 2H), 7.99 - 8.04 (m, 3H), 8.04-8.10 (m, 1H), 8.50 (dd, 1H). Intermediate 30 2-(3-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (1.50 g, 8.51 mmol) and 3-methylbenzohydrazide (CAS 13050-47-0, 1.28 g, 8.51 mmol) were stirred in N,N-dimethylformamide (30 mL) at 120 °C for 18 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 50 °C to give 1.87 g (79 % yield, 100% purity) of the title compound. LC-MS (method 3): Rt = 0.73 min., MS (ESIpos): m / z = 277 (M+H)+ 1H-NMR (400 MHz, methanol-d4): 5 [ppm] = 2.44 (s, 3H), 7.30-7.47 (m, 4H), 7.67-7.73 (m, 1H), 8.07 (d, 1H), 8.12 (s, 1H), 8.35 (d, 1H), NH not observed Intermediate 31 5-chloro-2-(3-methylphenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(3-Methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (1.87 g, 6.77 mmol) was solubilised in phosphorus(V) oxychloride (21 mL, 230 mmol), N,N-diisopropylethylamine (12 mL, 68 mmol) was added carefully and the mixture was stirred 3 hours at 100 °C and left to stand at room temperature for additional 72 hours. The mixture was concentrated and the residue was diluted with water. Precipitated product was filtered off, washed with water and dried under vacuum at 50 °C to give a mixture of product and starting material. It was reused. Again it was dissolved in phosphorus(V) oxychloride (21 mL, 230 mmol) and N,N-diisopropylethylamine (12 mL, 68 mmol) was added carefully. The mixture was stirred 4 hours at 100°C. Solvent was evaporated and the residue was slowly added to ice. A solid precipitate was filtered off, washed with water and dried under reduced pressure at 50 °C to afford crude material as a brown solid. It was suspended in dichloromethane and the solid was filtered off affording starting material (120 mg). The filtrate was concentrated under reduced pressure to give 929.3 mg of the title compound (80 % purity, 47 % yield). LC-MS (method 3): Rt = 1.17 min., MS (ESIpos): m / z = 295 (M+H)+ 1H-NMR (400 MHz, DMSO-d6): 5 [ppm] = 2.43 (s, 3H), 7.31-7.49 (m, 2H), 7.81-7.86 (m, 1H), 7.92-8.12 (m, 4H), 8.48-8.52 (m,1H) Intermediate 32 2-[3-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (1.50 g, 8.51 mmol) and 3-(trifluoromethyl)benzohydrazide (CAS 22227-25-4, 1.74 g, 8.51 mmol) were stirred in N,N-dimethylformamide (30 mL) at 120 °C for 18 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 1.72 g (61 % yield, 94 % purity) of the title compound. LC-MS (method 3): Rt = 0.79 min., MS (ESIpos): m / z = 331 (M+H)+ 1H-NMR (400 MHz, DMSO-d6): 5 [ppm] = 7.39 (t, 1H), 7.43 (d, 1H), 7.66-7.72 (m, 1H), 7.81 (t, 1H), 7.89 (s, 1H), 8.23 (dd, 1H), 8.43 (s, 1H), 8.48 (d, 1H). Intermediate 33 5-chloro-2-[3-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazoline 2-[3-(Trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (1.70 g, 67 % purity, 3.45 mmol) was added to phosphorus(V) oxychloride (20 mL, 210 mmol) at room temperature and N,N-diisopropylethylamine (6.0 mL, 34 mmol) was added slowly. The reaction mixture was warmed to 100 °C and stirred for 18 hours. Solvent was evaporated and the residue was poured into ice water and dichloromethane was added. The aqueous layer was extracted with dichloromethane thrice. The organic layers were combined, dried with magnesium sulfate and solvent was evaporated affording 1.88 g (119 % yield, 76 % purity) of the title compound. LC-MS (method 3): Rt = 1.19 min, (ESIpos): m / z = 349 (M+H)+ 1H-NMR (400 MHz, DMSO-d6) 5 [ppm] = 7.82-7.87 (m, 2H), 7.93-8.04 (m, 3H), 8.47-8.57 (m, 3H). Intermediate 34 2-(2-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one H Methyl (2-cyanophenyl)carbamate (1.50 g, 8.51 mmol) and 2-fluorobenzohydrazide (CAS 44624-2, 1.31 g, 8.51 mmol) were stirred in N,N-dimethylformamide (30 mL) at 120 °C for 18 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 50 °C to give 1.66 g (69 % yield, 99% purity) of the title compound. LC-MS (method 3): Rt = 0.59 min., MS (ESIpos): m / z = 281 (M+H)+ 1H-NMR (400 MHz, DMSO-d6): 5 [ppm] = 7.36-7.46 (m, 4H), 7.55-7.61 (m, 1H), 7.67-7.72 (m, 1H), 8.16-8.22 (m, 2H), 12.32 (s, 1H) Intermediate 35 5-chloro-2-(2-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(2-Fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (1.66 g, 5.92 mmol) was solubilised in phosphorus(V) oxychloride (20 mL, 210 mmol), N,N-diisopropylethylamine (10 mL, 59 mmol) was added carefully and the mixture was stirred 3 hours at 100 °C and left to stand at room temperature for additional 72 hours. The mixture was concentrated and the residue was diluted with warm water. A precipitated solid was filtered off, washed with water and dried under vacuo at 50 °C to give a mixture of product and starting material as a brown solid. It was suspended in dichloromethane and the solid was filtered off. The filtrate was concentrated under reduced pressure to give 1.01 g of the title compound (90 % purity, 51 % yield). LC-MS (method 3): Rt = 1.04 min., MS (ESIpos): m / z = 299 (M+H)+ 1H-NMR (400 MHz, DMSO-d6): 5 [ppm] = 7.36-7.47 (m, 2H), 7.59-7.66 (m, 1H), 7.82-7.87 (m, 1H), 7.93-7.99 (m, 1H), 8.03 (d, 1H), 8.27 (td, 1H), 8.49 (d, 1H), NH not observed Intermediate 36 2-(4-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (1.50 g, 8.51 mmol) and 4-methylbenzohydrazide (CAS 3619-22-5, 1.28 g, 8.51 mmol) were stirred in N,N-dimethylformamide (30 mL) at 120 °C for 18 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 50 °C to give 1.43 g (61 % yield, 91 % purity) of the title compound. WO 2021 / 028382 PCT / EP2020 / 072377 LC-MS (method 3): Rt = 0.71 min., MS (ESIpos): m / z = 277 (M+H)+ 1H-NMR (400 MHz, DMSO-d6): 5 [ppm] = 2.37 (s, 3H), 7.32-7.45 (m, 4H), 7.68 (t, 1H), 8.09 (d, 2H), 8.19 (d, 1H), 12.26 (br s, 1H) Intermediate 37 5 5-chloro-2-(4-methylphenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(4-Methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (340 mg, 1.23 mmol) was added to phosphorus(V) oxychloride (10 mL, 110 mmol) at room temperature and N,N-diisopropylethylamine (2.1 mL, 12 mmol) was added slowly. The reaction mixture was warmed 10 to 100 °C and stirred for 72 hours. Solvent was evaporated and the residue was poured into ice water. The aqueous layer was extracted with dichloromethane thrice. The organic layers were combined, dried with magnesium sulfate and solvent was evaporated affording 471 mg (114 % yield, 87 % purity) of the title compound. LC-MS (method 3): Rt = 1.14 min., MS (ESIpos): m / z = 295 (M+H)+ 15 1H-NMR (400 MHz, CDCI3): 5 [ppm] = 2.44 (s, 3H), 7.34 (d, 2H), 7.75 (t, 1H), 7.86 (t, 1H), 8.01 (d, 1H), 8.28 (d, 2H), 8.60 (d, 1H). Intermediate 38 2-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one F F Methyl (2-cyanophenyl)carbamate (250 mg, 1.42 mmol) and 4-(trifluoromethyl)benzohydrazide (CAS 339-59-3, 348 mg, 1.70 mmol) were stirred in N,N-dimethylformamide (3 mL) at 120 °C for 15 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 491 mg (100 % yield) of the title compound. LC-MS (Method 2): Rt = 0.83 min; MS (ESIpos): m / z = 331 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.40 - 7.49 (m, 2H), 7.73 (ddd, 1H), 7.96 (d, 2H), 8.25 (dd, 1H), 8.44 (d, 2H), 12.41 (s, 1H). Intermediate 39 5-chloro-2-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazoline F F V-F cot 2-[4-(Trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (491 mg, 1.49 mmol) was solubilised in phosphorus(V) oxychloride (5.0 mL, 54 mmol), N,N-diisopropylethylamine (2.6 mL, 15 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was poured into ice and stirred for one hour. Precipitated product was filtered off, washed with water and dried at 60 °C under reduced pressure to give 475 mg (92 % yield) of the title compound. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.89 (ddd, 1H), 7.97-8.03 (m, 3H), 8.05-8.09 (m, 1H), 8.51 (d, 2H), 8.55 (dd, 1H). Intermediate 40 2-(2-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (1.75 g, 9.93 mmol) and 2-chlorobenzohydrazide (CAS 581405-1, 1.69 g, 9.93 mmol) were stirred in N,N-dimethylformamide (30 mL) at 120 °C for 96 hours and at 140 °C for further 18 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 50 °C to give 1.93 g (65 % yield, 75 % purity) of the title compound. UPLC2-MS (short basic, 2-98%): Rt = 0.61 min., MS (ESIpos): m / z = 297 (M+H)+ 1H-NMR (400 MHz, MeOD-d3): 5 [ppm] = 7.40-7.55 (m, 4H), 7.58-7.62 (m, 1H), 7.69-7.75 (m, 1H), 7.91-7.95 (m, 1H), 8.30-8.34 (m, 1H). Intermediate 41 5-chloro-2-(2-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(2-Chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (170 mg, 573 pmol) was added to phosphorus(V) oxychloride (10 mL, 110 mmol) at room temperature and N,N-diisopropylethylamine (1000 pL, 5.7 mmol) was added slowly. The reaction mixture was warmed to 100 °C and stirred for 72 hours. The solvent was evaporated and azeotroped with toluene thrice to afford 2.69 g of the title compound as a dark brown oil. The material was taken onto next step without further purification. UPLC2-MS (short basic, 2-98%): Rt = 1.07 min., MS (ESIpos): m / z = 317 (M+H)+. Intermediate 42 2-(3-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (1.60 g, 9.08 mmol) and 3-chlorobenzohydrazide (CAS 167347-8, 1.55 g, 9.08 mmol) were stirred in N,N-dimethylformamide (30 mL) at 120 °C for 72 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 50 °C to give 2.38 g (88 % yield, 96 % purity) of the title compound. UPLC2-MS (short basic, 2-98%): Rt = 0.74 min., MS (ESIpos): m / z = 297 (M+H)+ 1H-NMR (400 MHz, DMSO-d6): 5 [ppm] = 7.39 (t, 1H), 7.43 (d, 1H), 7.56-7.62 (m, 2H), 7.677.72 (m, 1H), 8.13-8.18 (m, 2H), 8.21 (d, 1H), 12.34 (brs, 1H) Intermediate 43 5-chloro-2-(3-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(3-Chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (700 mg, 2.36 mmol) was added to phosphorus(V) oxychloride (15 mL, 160 mmol) at room temperature and N,N-diisopropylethylamine (6.2 mL, 35 mmol) was added slowly. The reaction mixture was warmed to 100 °C and stirred for 24 hours. Solvent was evaporated and the residue was poured into ice water. The aqueous layer was extracted with dichloromethane thrice. The organic layers were combined, dried with magnesium sulfate and solvent was evaporated affording 1.31 g (79 % yield, 45% purity) of the title compound. UPLC2-MS (short basic, 2-98%): Rt = 1.20 min., MS (ESIpos): m / z = 315 / 317 (M+H)+ (product) and 0.73 min., 40.04%. MS (ESIpos): m / z = 297 / 299 (M+H)+ (starting material) Intermediate 44 2-(2-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one H Methyl (2-cyanophenyl)carbamate (1.00 g, 5.68 mmol) and 2-methoxybenzohydrazide (CAS 7466-54-8,1.13 g, 6.81 mmol) were stirred in N-methylpyrrolidone (25 mL) at 120 °C for 8 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 846 mg (95 % purity, 48 % yield) of the title compound. LC-MS (Method 2): Rt = 0.65 min; MS (ESIpos): m / z = 293 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.12 (td, 1H), 7.22 (d, 1H), 7.38-7.43 (m, 1H), 7.45 (d, 1H), 7.49 - 7.56 (m, 1H), 7.71 (ddd, 1H), 7.92 (dd, 1H), 8.20 (dd, 1H), 12.31 (br s, 1H). Intermediate 45 5-chloro-2-(2-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(2-Methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (846 mg, 2.89 mmol) was solubilised in phosphorus(V) oxychloride (14 mL, 150 mmol), N,N-diisopropylethylamine (5.0 mL, 29 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was poured into ice and stirred for one hour. Organic solvent was evaporated and precipitated product was filtered off, washed with water and dried at 60 °C under reduced pressure to give 455 mg (100 % purity, 51 % yield) of the title compound. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.90 (s, 3H), 7.15 (td, 1H), 7.26 (d, 1H), 7.53-7.60 (m, 1H), 7.86 (ddd, 1H), 7.95 - 8.02 (m, 2H), 8.03 - 8.07 (m, 1H), 8.50 (dd, 1H). LC-MS (Method 2): Rt = 1.22 min; MS (ESIpos): m / z = 311 [M+H]+ Intermediate 46 2-(1 H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (250 mg, 1.42 mmol) and 1H-pyrazole-3-carbohydrazide (CAS 26275-64-9, 215 mg, 1.70 mmol) were stirred in N,N-dimethylformamide (3 mL) at 120 °C for 15 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 290 mg (81 % yield) of the title compound. LC-MS (Method 2): Rt = 0.46 min; MS (ESIpos): m / z = 253 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 6.86-6.97 (m, 1H), 7.38 - 7.50 (m, 2H), 7.71 (brt, 1H), 7.92 (s, 1H), 8.21 (d, 1H), 12.32 (br s, 1H), 13.31 (brs, 1H). Intermediate 47 5-chloro-2-(1 H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(1H-Pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (290 mg, 1.15 mmol) was solubilised in phosphorus(V) oxychloride (3.6 mL, 38 mmol), N,N-diisopropylethylamine (2.0 mL, 11 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was poured into ice and stirred for one hour. The organic solvent was evaporated and precipitated product was filtered off, washed with water and dried at 60 °C under reduced pressure to give 320 mg (38 % purity, 39 % yield) of the title compound. LC-MS (Method 2): Rt = 0.89 min; MS (ESIpos): m / z = 271 [M+H]+1H-NMR (400 MHz, DMSO-d6) 5 [ppm]: 1.211 (0.61), 1.227 (0.90), 1.249 (6.94), 1.265 (8.14), 1.277 (6.62), 1.282 (2.63), 1.294 (6.39), 2.518 (4.33), 2.523 (2.80), 3.105 (0.86), 3.116 (0.84), 3.124 (0.84), 3.134 (0.84), 3.577 (0.48), 3.587 (0.50), 3.593 (0.67), 3.603 (0.65), 3.609 (0.46), 3.620 (0.48), 5.655 (0.82), 5.923 (1.07), 6.897 (13.77), 6.903 (16.00), 6.977 (5.84), 6.982 (6.16), 7.398 (2.80), 7.400 (3.03), 7.418 (5.49), 7.436 (3.15), 7.438 (3.41), 7.464 (5.11), 7.483 (6.14), 7.528 (0.50), 7.694 (3.55), 7.698 (3.68), 7.712 (3.53), 7.716 (4.58), 7.719 (3.28), 7.733 (2.52), 7.736 (2.48), 7.845 (2.02), 7.849 (12.36), 7.854 (11.58), 7.863 (2.14), 7.866 (2.35), 7.868 (1.58), 7.882 (1.58), 7.886 (1.58), 7.911 (5.28), 7.916 (5.28), 7.955 (1.26), 7.959 (1.32), 7.973 (0.97), 7.976 (2.31), 7.980 (2.12), 7.994 (1.70), 7.998 (1.62), 8.033 (2.69), 8.035 (2.88), 8.054 (1.58), 8.196 (4.39), 8.199 (4.60), 8.215 (4.44), 8.218 (4.08), 8.490 (1.96), 8.493 (2.02), 8.508 (1.79), 8.512 (1.83), 12.344 (6.43). Intermediate 48 2-(1-methyl-1 H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one H Methyl (2-cyanophenyl)carbamate (503 mg, 2.86 mmol) and 1-methyl-1H-pyrazole-3-carbohydrazide (400 mg, 2.86 mmol) were stirred in DMF (10 mL) at 120°C for 20 h. Water was added to the mixture and the solid was filtered, washed with water and dried under reduced pressure at 60°C to give 630 mg of the tiltle compound that was used without further purification. LC-MS (method 2): Rt = 0.48 min; MS (ESIpos): m / z = 267 [M+H]+ Intermediate 49 5-chloro-2-(1-methyl-1 H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(1-Methyl-1H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (630 mg, 2.37 mmol) was stirred in phosphorus(V) oxychloride (6.0 mL) , N,N-diisopropylethylamine (4.1 mL, 24 mmol) was added carefully and the mixture was stirred for 3 h at 110°C. The mixture was poured into ice stirred for 1 h. The solid was filtered, washed with water and dried at 60°C under reduced pressure to give 485 mg of the title compound that was used without further purification. LC-MS (method 2): Rt = 1.00 min; MS (ESIpos): m / z = 285 [M+H]+ 1H-NMR (400MHz, DMS0-d6): 6 [ppm]= 3.99 (s, 3H), 6.94 (d, 1H), 7.86 (ddd, 1H), 7.91 (d, 1H), 7.94 - 8.00 (m, 1H), 8.01 - 8.06 (m, 1H), 8.50 (dd, 1H). Intermediate 50 2-(5-methyl-1 H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (250 mg, 1.42 mmol) and 5-methyl-1H-pyrazole-3-carbohydrazide (CAS 40535-14-6, 199 mg, 1.42 mmol) were stirred in N,N-dimethylformamide (5 mL) at 120 °C for 40 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 202 mg (70 % purity, 37 % yield) of the title compound. It was used without further purification. LC-MS (Method 2): Rt = 0.50 min; MS (ESIpos): m / z = 267 [M+H]+ 1H-NMR (400 MHz, DMSO-d6) 5 [ppm]: 2.287 (5.95), 2.321 (16.00), 2.522 (2.27), 2.669 (0.49), 2.726 (9.97), 2.885 (12.16), 6.469 (1.02), 6.624 (4.56), 6.698 (0.50), 7.000 (0.65), 7.019 (0.81), 7.064 (0.40), 7.081 (0.78), 7.101 (0.56), 7.390 (4.84), 7.408 (9.71), 7.428 (6.36), 7.437 (8.19), 7.457 (9.00), 7.684 (3.63), 7.703 (5.86), 7.722 (2.90), 7.948 (2.32), 7.966 (0.81), 8.177 (7.58), 8.180 (7.78), 8.197 (7.49), 10.547 (0.83), 10.616 (0.92), 12.290 (3.21), 12.970 (4.45), 13.552 (0.53). Intermediate 51 5-chloro-2-(5-methyl-1 H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(5-Methyl-1H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (200 mg, 751 pmol) was solubilised in phosphorus(V) oxychloride (3.5 mL, 38 mmol), N,N-diisopropylethylamine (1.3 mL, 7.5 mmol) was added carefully and the mixture was stirred for two days at 110 °C. The mixture was poured into ice and stirred for two hours. It was extracted with dichloromethane. The organic phase was dried over sodium sulfate and concentrated under reduced pressure to give 130 mg (92 % purity, 61 % yield) of the title compound. It was used without further purification. LC-MS (Method 2): Rt = 0.96 min; MS (ESIpos): m / z = 285 [M+H]+ 1H-NMR (400 MHz, DMSO-d6) 6 [ppm]: 1.196 (0.46), 1.205 (0.89), 1.213 (0.54), 1.220 (1.05), 1.237 (2.31), 1.246 (7.31), 1.255 (4.73), 1.262 (7.78), 1.269 (7.33), 1.286 (6.85), 2.310 (0.57), 2.331 (16.00), 2.518 (1.93), 2.523 (1.23), 2.664 (0.41), 2.669 (0.56), 3.114 (0.95), 3.124 (0.98), 3.133 (0.96), 3.143 (0.93), 3.568 (0.50), 3.585 (0.82), 3.594 (0.86), 3.601 (1.00), 3.611 (1.00), 3.618 (0.82), 3.627 (0.79), 3.643 (0.46), 5.759 (1.14), 6.723 (4.86), 6.725 (4.93), 7.838 (1.15), 7.841 (1.23), 7.856 (1.84), 7.858 (2.29), 7.861 (1.65), 7.875 (1.64), 7.878 (1.63), 7.948 (1.21), 7.952 (1.27), 7.969 (2.33), 7.973 (2.04), 7.987 (1.62), 7.990 (1.52), 8.025 (3.12), 8.044 (1.71), 8.085 (0.44), 8.472 (2.07), 8.474 (2.24), 8.492 (2.09), 8.494 (1.94). Intermediate 52 2-(1-methyl-1 H-pyrazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one H Methyl (2-cyanophenyl)carbamate (71.2 mg, 404 pmol) and 1-methyl-1H-pyrazole-5-carbohydrazide (85.0 mg, 607 pmol) were stirred in DMF (850 pL) overnight at 120°C. The reaction mixture was cooled to rt and diluted with water.The solid was filtered, washed with water WO 2021 / 028382 PCT / EP2020 / 072377 and dried under reduced pressure at 60°C to give 78.0 mg (72 % yield) of the title compound without further purification. LC-MS (Method 2): Rt = 0.53 min; MS (ESIpos): m / z = 267 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 4.29 (s, 3H), 6.99 (d, 1H), 7.40 - 7.44 (m, 1H), 7.46 (d, 1H), 7.60 (d, 1H), 7.73 (ddd, 1H), 8.22 (dd, 1H), 12.43 (s, 1H). Intermediate 53 5-chloro-2-(1-methyl-1 H-pyrazol-5-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(1-Methyl-1H-pyrazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (78.0 mg, 293 pmol) was solubilised in phosphorus(V) oxychloride (1.1 mL, 11 mmol), N,N-diisopropylethylamine (510 pL, 2.9 mmol) was added carefully and the mixture was stirred overnight at 110°C. The mixture was cooled to rt, was poured into ice and stirred for 1 h. The solid was filtered, washed with water and dried at 60°C under reduced pressure to provide 50.0 mg (60 % yield) the title compound without further purification. LC-MS (Method 2): Rt = 1.13 min; MS (ESIpos): m / z = 286 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 4.35 (s, 3H), 7.07 (d, 1H), 7.64 (d, 1H), 7.88 (ddd, 1H), 7.97 - 8.03 (m, 1H), 8.04 - 8.09 (m, 1H), 8.52 (dd, 1H). Intermediate 54 2-(1-ethyl-3-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (209 mg, 1.19 mmol) and 1-ethyl-3-methyl-1H-pyrazole-4- carbohydrazide (CAS 1177272-66-0, 200 mg, 1.19 mmol) were stirred in N,N- dimethylformamide (4.2 mL) at 120 °C for 20 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 200 mg (98 % purity, 56 % yield) of the title compound. LC-MS (Method 2): Rt = 0.56 min; MS (ESIpos): m / z = 295 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 1.41 (t, 3H), 2.54 (s, 3H), 4.15 (q, 2H), 7.34 - 7.56 (m, 2H), 7.70 (ddd, 1H), 8.15 (dd, 1H), 8.35 (s, 1H), 12.26 (brs, 1H). Intermediate 55 5-chloro-2-(1-ethyl-3-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(1-Ethyl-3-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (200 mg, 678 pmol) was solubilised in phosphorus(V) oxychloride (1.9 mL, 20 mmol), N,N-diisopropylethylamine (1.2 mL, 6.8 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was poured into ice and stirred for two hours. Precipitated product was filtered off, washed with water and dried at 60 °C under reduced pressure to give 128 mg (66 % purity, 40 % yield) of the title compound. It was used without purification. LC-MS (Method 2): Rt = 1.18 min; MS (ESIpos): m / z = 313 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1,42 (t, 3H), 2,53 (s, 3H), 4,16 (q, 2H), 7,84 (td, 1H), 7,95 (td, 1H), 8,02 (d, 1H), 8,44 (dd, 1H), 8,45 (s, 1H). Intermediate 56 2-(1 -ethyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (229 mg, 1.30 mmol) and 1 -ethyl-1 H-pyrazole-4-carbohydrazide (CAS 512809-51-7, 200 mg, 1.30 mmol) were stirred in N,N-dimethylformamide (4.6 mL) at 120 °C for 20 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 244 mg (100 % purity, 67 % yield) of the title compound. LC-MS (Method 2): Rt = 0.52 min; MS (ESIpos): m / z = 281 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.44 (t, 3H), 4.24 (q, 2H), 7.34 - 7.51 (m, 2H), 7.70 (ddd, 1H), 8.03 (d, 1H), 8.17 (dd, 1H), 8.46 (s, 1H), 12.26 (brs, 1H). Intermediate 57 5-chloro-2-(1-ethyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(1-Ethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (244 mg, 872 pmol) was solubilised in phosphorus(V) oxychloride (2.4 mL, 26 mmol), N,N-diisopropylethylamine (1.5 mL, 8.7 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was poured into ice and stirred for two hours. Precipitated product was filtered off, washed with water and dried at 60 °C under reduced pressure to give 133 mg (85 % purity, 43 % yield) of the title compound. It was used without purification. LC-MS (Method 2): Rt = 1.06 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1,45 (t, 3H), 4,25 (q, 2H), 7,84 (td, 1H), 7,96 (td, 1H), 8,02 (dd, 1H), 8,10 (s, 1H), 8,45 (dd, 1H), 8,57 (s, 1H). Intermediate 58 2-(1,5-dimethyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one H Methyl (2-cyanophenyl)carbamate (229 mg, 1.30 mmol) and 1,5-dimethyl-1H-pyrazole-4-carbohydrazide (CAS 864948-68-5, 200 mg, 1.30 mmol) were stirred in N,N-dimethylformamide (4.6 mL) at 120 °C for 20 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 287 mg (80 % purity, 63 % yield) of the title compound. LC-MS (Method 2): Rt = 0.52 min; MS (ESIpos): m / z = 281 [M+H]+ 1H-NMR (400 MHz, DMSO-d6) 5 [ppm]: 2.518 (2.95), 2.523 (1.96), 2.707 (15.66), 2.727 (0.94), 2.888 (1.08), 3.757 (4.57), 3.829 (16.00), 7.090 (0.60), 7.371 (0.92), 7.373 (1.03), 7.391 (1.90), 7.409 (1.20), 7.411 (1.33), 7.423 (1.90), 7.444 (2.14), 7.674 (1.11), 7.678 (1.14), 7.693 (1.11), 7.696 (1.54), 7.698 (1.13), 7.713 (0.85), 7.717 (0.85), 7.934 (5.92), 7.969 (0.42), 8.177 (1.54), 8.181 (1.61), 8.198 (1.58), 8.200 (1.47). Intermediate 59 5-chloro-2-(1,5-dimethyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(1,5-Dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (287 mg, 1.02 mmol) was solubilised in phosphorus(V) oxychloride (2.9 mL, 31 mmol), N,N-diisopropylethylamine (1.8 mL, 10 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was poured into ice and stirred for two hours. Precipitated product was filtered off, washed with water and dried at 60 °C under reduced pressure to give 237 mg (50 % purity, 39 % yield) of the title compound. The compound was used without purification. LC-MS (Method 2): Rt = 1.10 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2,70 (s, 3H), 3,83 (s, 3H), 7,84 (td, 1H), 7,96 (dd, 1H), 8,01 (s, 1H), 8,02 (d, 1H), 8,47 (dd, 1H). Intermediate 60 2-(1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (500 mg, 2.84 mmol) and 1H-pyrazole-4-carbohydrazide (358 mg, 2.84 mmol) were stirred in DMF (10 mL) overnight at 120°C. 1 H-pyrazole-4-carbohydrazide (358 mg, 2.84 mmol) was added and the reaction was stirred again overnight at 120°C. The reaction mixture was cooled to rt and diluted with water. The solid was filtered, washed with water and dried under reduced pressure at 60°C to give 430 mg (60 % yield) of the title compound. LC-MS (method 2): Rt = 0.46 min; MS (ESIpos): m / z = 253 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.35 - 7.48 (m, 2H), 7.70 (ddd, 1H), 8.09 (br s, 1H), 8.18 (dd, 1H), 8.44 (brs, 1H), 12.25 (brs, 1H), 13.31 (brs, 1H). Intermediate 61 5-chloro-2-(1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (215 mg, 852 pmol) was solubilised in phosphorus(V) oxychloride (2.8 mL, 30 mmol), N,N-diisopropylethylamine (1.5 mL, 8.5 mmol) was added carefully and the mixture was stirred overnight at 110°C. The mixture was carefully poured into ice and stirred for 1 h. The solid was filtered off, washed with water and dried at 60°C under reduced pressure to give 208 mg (90 % yield) of the title compound. The compound was used without further purification LC-MS (method 2): Rt = 0.87 min; MS (ESIpos): m / z = 271 [M+H]+ WO 2021 / 028382 PCT / EP2020 / 072377 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.84 (ddd, 1H), 7.93-7.99 (m, 1H), 8.00-8.04 (m, 1H), 8.35 (s, 2H), 8.47 (dd, 1H). Intermediate 62 2-chloro-4-hydrazinoquinazoline 2,4-Dichloroquinazoline (1 g, 5.02 mmol) was dissolved in THF (20 mL). Hydrazine hydrate (293 pL, 6.03 mmol) and triethylamine (2.52 mL, 18.09 mmol) were added. As the reaction mixture became viscous more THF (10 mL) was added. The reaction mixture was stirred overnight at rt. To the reaction mixture were added water (50 mL) and ethyl acetate (50 mL). The layers were separated and the aqueous phase was extracted two time with ethyl acetate (15 mL). The combined organic phases were washed with aqueous saturated ammonium chloride solution, dried over magnesium sulfate and concentrated under vacuum to afford 925 mg of the title compound which was used without further purification LC-MS (method 2): Rt = 0.60 min; MS (ESIpos): m / z = 195 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 4.84 (brs, 2H), 7.46 - 7.51 (m, 1H), 7.60 (d, 1H), 7.737.80 (m, 1H), 8.18 (brd, 1H), 10.12 (brs, 1H). Intermediate 63 N'-(2-chloroquinazolin-4-yl)-2-methyl-1,3-oxazole-4-carbohydrazide ch3 NH HN To a stirred solution of 2-methyl-1,3-oxazole-4-carboxylic acid (5 g, 39.3 mmol) in DMF (75 mL), N,N-diisopropylethylamine (10.15 g, 78.6 mmol) was added and the reaction mixture was cooled to 0°C. HATU (22.4 g, 58.9 mmol) was added followed by addition of 2-chloro-4-hydrazinoquinazoline (7.63 g, 0.125 mol). The reaction mixture was stirred for one hour and quenched with ice. The precipitate was filtered and washed with water and petroleum ether to afford the title compound. The crude material was used without further purification. Intermediate 64 2-(2-Methyl-1,3-oxazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one N'-(2-chloroquinazolin-4-yl)-2-methyl-1,3-oxazole-4-carbohydrazide (8.2 g, 28.7 mmol) was stirred in acetic acid (82 mL) at reflux for 6h. The reaction mixture was then cooled to rt and diluted with ice cold water. The precipitate was filtered and washed with water and petroleum ether to afford the title compound. The crude material was used without further purification. Intermediate 65 5-Chloro-2-(2-methyl-1,3-oxazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(2-Methyl-1,3-oxazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (3.3 g, 12.3 mmol) and N, N-diisopropylethylamine ((9.53 g, 74.0 mmol) were stirred four hours in POCI3 (114 mL) at reflux. The reaction was cooled to rt and diluted with DCM and ice cold water. The aqueous phase was extracted with DCM. The organic phase was dried (Na2SO4) filtered and concentrated under reduced pressure to give the title compound without further purification. Intermediate 66 2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (500 mg, 2.84 mmol) and 4-fluorobenzohydrazide (CAS 45606-4, 437 mg, 2.84 mmol) were stirred in N,N-dimethylformamide (10 mL) at 120 °C for 20 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 725 mg (96 % purity, 88 % yield) of the title compound. LC-MS (Method 2): Rt = 0.70 min; MS (ESIpos): m / z = 281 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.38 - 7.48 (m, 4H), 7.72 (ddd, 1H), 8.20 - 8.30 (m, 3H), 12.35 (brs, 1H). Intermediate 67 5-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(4-Fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (725 mg, 2.59 mmol) was solubilised in phosphorus(V) oxychloride (8.0 mL, 86 mmol), N,N-diisopropylethylamine (4.5 mL, 26 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was poured into ice and stirred for one hour. The organic solvent was evaporated and the solid was filtered off, washed with water and dried at 60 °C under reduced pressure to give 725 mg (99 % purity, 93 % yield) of the title compound. LC-MS (Method 2): Rt = 1.41 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.41 - 7.48 (m, 2H), 7.87 (ddd, 1H), 7.96-8.02 (m, 1H), 8.03 - 8.07 (m, 1H), 8.31 - 8.38 (m, 2H), 8.49 - 8.55 (m, 1H). Intermediate 68 2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (2.00 g, 11.4 mmol) and 3-methoxybenzohydrazide (CAS 5785-06-8, 2.26 g, 13.6 mmol) were stirred in N-methylpyrrolidone (50 mL) at 120 °C for 4 hours. Water was added to the mixture, precipitated product was filtered off, washed with water and dried under reduced pressure at 60 °C to give 2.63 g (93 % purity, 74 % yield) of the title compound. LC-MS (Method 2): Rt = 0.64 min; MS (ESIpos): m / z = 293 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.88 (s, 3H), 7.12 (ddd, 1H), 7.38 - 7.53 (m, 3H), 7.69 - 7.75 (m, 2H), 7.83 (dt, 1H), 8.24 (dd, 1H), 12.35 (s, 1H) Intermediate 69 5-chloro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline 2-(3-Methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (2.63 g, 8.99 mmol) was solubilised in phosphorus(V) oxychloride (26 mL, 282 mmol), N,N-diisopropylethylamine (16 mL, 90 mmol) was added carefully and the mixture was stirred overnight at 110 °C. The mixture was evaporated and the residue was diluted with ethyl acetate. Precipitated product was filtered off to give 2.86 g (100 % purity, 100 % yield) of the title compound. LC-MS (Method 2): Rt = 1.36 min; MS (ESIpos): m / z = 311 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.89 (s, 3H), 7.17 (ddd, 1H), 7.53 (t, 1H), 7.79 (dd, 1H), 7.84 - 7.92 (m, 2H), 7.98 (td, 1H), 8.03 - 8.08 (m, 1H), 8.53 (dd, 1H) Intermediate 70 N2-(tert-butoxycarbonyl)-N-propan-2-yl-D-alaninamide N-(tert-Butoxycarbonyl)-D-alanine (100 mg, 529 pmol), propan-2-amine (90 pL, 1.1 mmol), sodium hydrogen carbonate (133 mg, 1.59 mmol) and HATLI (402 mg, 1.06 mmol) were stirred in dichloromethane (1.5 mL) overnight at rt. The solid was filtered and washed with DCM. The filtrate was diluted with water and extracted with DCM / MeOH (9 / 1). The organic layer was dried (silicone filter) and concentrated under reduced pressure to give 97 mg (100 % purity, 80 % yield) of the title compound without further purification. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.03 (dd, 6H), 1.13 (d, 3H), 1.37 (s, 9H), 3.69 - 3.98 (m, 2H), 6.75 (brd, 1H), 7.56 (brd, 1H). Intermediate 71 N2-(tert-butoxycarbonyl)-N-cyclopropyl-D-alaninamide H3C h3c N-(tert-Butoxycarbonyl)-D-alanine (100 mg, 529 pmol), cyclopropanamine (60.4 mg, 1.06 mmol), sodium hydrogen carbonate (133 mg, 1.59 mmol) and HATLI (402 mg, 1.06 mmol) were stirred in dichloromethane (1.5 mL) overnight at rt. The solid was filtered and washed with DCM. The mixture was diluted with water and extracted with DCM / MeOH (9 / 1). The organic layer was dried (silicone filter) and concentrated under reduced pressure to give 155 mg (100 % purity, 96 % yield) of the title compound without further purification. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 0.34 - 0.40 (m, 2H), 0.58 - 0.61 (m, 2H), 0.75 - 0.82 (m, 1H), 1.11 (d, 3H), 1.36 (s, 9H), 3.79-3.90 (m, 1H), 6.77 (brd, 1H), 7.83 (brd, 1H). Intermediate 72 N2-(tert-butoxycarbonyl)-N-ethyl-D-alaninamide N-(tert-Butoxycarbonyl)-D-alanine (100 mg, 529 pmol), ethanamine (530 pL, 2.0 M in THF, 1.1 mmol), sodium hydrogen carbonate (133 mg, 1.59 mmol) and HATLI (402 mg, 1.06 mmol) were stirred in DCM (1.5 mL) overnight at rt. The mixture was diluted with water and extracted with DCM / MeOH (9 / 1). The organic layer was dried (silicone filter) and concentrated under reduced pressure, to give 155 mg (100 % purity, 94 % yield) of the title compound without further purification. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 0.99 (t, 3H), 1.14 (d, 3H), 1.37 (s, 9H), 3.01 - 3.09 (m, 2H), 3.88 (brt, 1H), 6.81 (brd, 1H), 7.73 (brs, 1H). Intermediate 73 N2-(tert-butoxycarbonyl)-N-methyl-D-alaninamide O h3c JL ch3 3 n 3 “ H H3C O NH h3c^t n 3 ch3 o N-(tert-Butoxycarbonyl)-D-alanine (100 mg, 529 pmol), methanamine (530 pL, 2.0 M in THF, 1.1 mmol), sodium hydrogen carbonate (133 mg, 1.59 mmol) and HATLI (402 mg, 1.06 mmol) were stirred in DCM (1.5 mL) overnight at rt. The mixture was diluted with water and extracted with DCM / MeOH (9 / 1). The organic layer was dried (silicone filter) and concentrated under reduced pressure, to give 110 mg (100 % purity, 92 % yield) of the title compound without further purification. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.14 (d, 3H), 1.37 (s, 9H), 2.56 (d, 3H), 3.82 - 3.95 (m, 1H), 6.85 (brd, 1H), 7.70 (brd, 1H). Intermediate 74 tert-butyl [(2R)-1-(cyclobutylamino)-1-oxopropan-2-yl]carbamate N-(tert-Butoxycarbonyl)-D-alanine (100 mg, 529 pmol), cyclobutanamine (75.2 mg, 1.06 mmol), sodium hydrogen carbonate (133 mg, 1.59 mmol) and HATLI (402 mg, 1.06 mmol) were stirred in DCM (1.5 mL) overnight at rt. The mixture was diluted with water and extracted with DCM / MeOH (9 / 1). The organic layer was dried (silicone filter) and concentrated under reduced pressure, to give 168 mg (75 % purity, 98 % yield) of the title compound without further purification. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.12 (d, 3H), 1.37 (s, 9H), 1.54 - 1.69 (m, 2H), 1.77 -1.96 (m, 2H), 2.06-2.19 (m, 2H), 3.87 (quin, 1H), 4.15 (sxt, 1H), 6.73 - 6.81 (m, 1H), 7.98 (brd, 1H). Intermediate 75 N2-(tert-butoxycarbonyl)-N,N-dimethyl-D-alaninamide O h3c JL ch3 3 n 3 - i H3C O NH CH3 h3c^t n 3 ch3 o N-(tert-Butoxycarbonyl)-D-alanine (100 mg, 529 pmol), N-methylmethanamine (530 pL, 2.0 M in THF, 1.1 mmol), sodium hydrogen carbonate (133 mg, 1.59 mmol) and HATLI (402 mg, 1.06 mmol) were stirred in DCM (1.5 mL) overnight at rt. The mixture was diluted with water and extracted with DCM / MeOH (9 / 1). The organic layer was dried (silicone filter) and concentrated under reduced pressure, to give 155 mg of the title compound without further purification. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.11 (d, 3H), 1.36 (s, 9H), 2.81 (s, 3H), 2.99 (s, 3H), 4.40 (quin, 1H), 6.89 (brd, 1H). Intermediate 76 N2-(tert-butoxycarbonyl)-N-(2-hydroxyethyl)-D-alaninamide 0 h3c o nh H h3c^T n 3 ch3 o N-(tert-Butoxycarbonyl)-D-alanine (100 mg, 529 pmol), 2-aminoethan-1-ol (64.6 mg, 1.06 mmol), sodium hydrogen carbonate (133 mg, 1.59 mmol) and HATLI (402 mg, 1.06 mmol) were stirred in DCM (1.5 mL) overnight at rt. The mixture was diluted with water and extracted with DCM / MeOH (9 / 1). The aqueous phase was lyophilized to give 600 mg of the crude title compound that was used without further purification. Intermediate 77 N2-(tert-butoxycarbonyl)-N-(3-hydroxypropyl)-D-alaninamide O H3C O NH HoC^I n 3 ch3 o N-(tert-Butoxycarbonyl)-D-alanine (100 mg, 529 pmol), 3-aminopropan-1-ol (79.4 mg, 1.06 mmol), sodium hydrogen carbonate (133 mg, 1.59 mmol) and HATLI (402 mg, 1.06 mmol) were stirred in DCM (1.5 mL) overnight at rt. The mixture was diluted with water and extracted with DCM / MeOH (9 / 1). The aqueous layer was lyophilized to give 58 mg of the crude title compound that was used without further purification. Intermediate 78 N-propan-2-yl-D-alaninamide hydrochloride xHCI N2-(tert-Butoxycarbonyl)-N-propan-2-yl-D-alaninamide (97.0 mg, 421 pmol) was solubilised in dichloromethane (5.6 mL) and methanol (1.4 mL). HCI (1.6 mL, 4.0 M in dioxane, 6.3 mmol) was added and the mixture was stirred overnight at rt. The reaction mixture was concentrated under reduced pressure to give 97 mg of the title compound. The compound was used without further purification. Intermediate 79 N-cyclopropyl-D-alaninamide hydrochloride xHCI N2-(tert-Butoxycarbonyl)-N-cyclopropyl-D-alaninamide (155 mg, 766 pmol) was dissoved in dichloromethane (5.0 mL) and methanol (2.0 mL), HCI (2.9 mL, 4.0 M in dioxane, 11 mmol) was added and the mixture was stirred overnight at rt. The reaction mixture was concentrated under reduced pressure to give 116 mg of the title product that was used without further purification. Intermediate 80 N-ethyl-D-alaninamide hydrochloride O H3C JL 3 v rr CH, nh2 h xHCI N2-(tert-Butoxycarbonyl)-N-ethyl-D-alaninamide (155 mg, 766 pmol) was dissoved in dichloromethane (5.0 mL) and methanol (2.0 mL), HCI (2.9 mL, 4.0 M in dioxane, 11 mmol) was added and the mixture was stirred overnight at rt. The reaction mixture was concentrated under reduced pressure to give 101 mg of the title compound that was used without further purification. Intermediate 81 N-methyl-D-alaninamide hydrochloride O H3C 11 CH, nh2 h xHCI N2-(tert-Butoxycarbonyl)-N-methyl-D-alaninamide (110 mg, 544 pmol) was dissoved in dichloromethane (5.0 mL) and methanol (2.0 mL), HCI (2.0 mL, 4.0 M in dioxane, 8.2 mmol) was added and the mixture was stirred overnight at rt. The reaction mixture was concentrated under reduced pressure to give 70 mg of the title compound that was used without further purification. Intermediate 82 N-cyclobutyl-D-alaninamide hydrochloride nh2 xHCI tert-butyl [(2R)-1-(cyclobutylamino)-1-oxopropan-2-yl]carbamate (168 mg, 75 % purity, 520 pmol) was dissoved in dichloromethane (4.8 mL) and methanol (1.9 mL), HCI (1.9 mL, 4.0 M in dioxane, 7.8 mmol) was added and the mixture was stirred overnight at rt. The reaction mixture was concentrated under reduced pressure to give 158 mg of the title compound that was used without further purification. Intermediate 83 N,N-dimethyl-D-alaninamide hydrochloride O i nh2 ch3 xHCI N2-(tert-Butoxycarbonyl)-N,N-dimethyl-D-alaninamide (153 mg, 70 % purity, 495 pmol) was dissoved in dichloromethane (5.0 mL) and methanol (1.5 mL), HCI (1.9 mL, 4.0 M in dioxane, 7.4 mmol) was added and the mixture was stirred overnight at rt. The reaction mixture was concentrated under reduced pressure to give 133 mg of the title compound that was used without further purification. Intermediate 84 N-(2-hydroxyethyl)-D-alaninamide hydrochloride O H3C JL OH NH2 h xHCI N2-(tert-butoxycarbonyl)-N-(2-hydroxyethyl)-D-alaninamide (600 mg, 20 % purity, 517 pmol) was dissoved in dichloromethane (4.7 mL) and methanol (1.9 mL), HCI (1.9 mL, 4.0 M in dioxane, 7.7 mmol) was added and the mixture was stirred overnight at rt. The reaction mixture was concentrated under reduced pressure to give 90 mg of the title compound that was used without further purification. Intermediate 85 N-(3-hydroxypropyl)-D-alaninamide hydrochloride 0 nh2 H XHCI N2-(tert-Butoxycarbonyl)-N-(3-hydroxypropyl)-D-alaninamide (58.0 mg, 235 pmol) was dissoved in dichloromethane (2.2 mL) and methanol (870 pl), HCI (880 pL, 4.0 M in dioxane, 3.5 mmol) was added and the mixture was stirred overnight at rt. The reaction mixture was concentrated 5 under reduced pressure to give 45 mg of the title compound that was used without further purification. Intermediate 86 2-(pyridin-2-yl)[1,2,4]triazolo[1,5-c]quinazoline-5(6H)-thione 10 2-lsothiocyanatobenzonitrile (CAS 81431-98-3, 500 mg, 3.12 mmol) and pyridine-2-carbohydrazide (CAS 1452-63-7, 428 mg, 3.12 mmol) were solubilised in 100 mL ethanol and the reaction mixture was stirred at reflux overnight. Precipitated product was filtered off, washed with ethanol and dried at 40 °C to give 769 mg (90 % purity, 79 % yield) of the title compound. LC-MS (Method 2): Rt = 0.50 min; MS (ESIpos): m / z = 280 [M+H]+ 15 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.54 - 7.61 (m, 2H), 7.69 (d, 1H), 7.78 - 7.85 (m, 1H), 8.04 (td, 1H), 8.29-8.35 (m, 2H), 8.77-8.82 (m, 1H), 14.08 (br s, 1H). Intermediate 87 2-(pyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazoline-5(6H)-thione 2-lsothiocyanatobenzonitrile (CAS 81431-98-3, 500 mg, 3.12 mmol) and pyridine-3-carbohydrazide (CAS 553-53-7, 428 mg, 3.12 mmol) were solubilised in ethanol (100 mL) and the mixture was stirred at reflux overnight. The reaction was filtered and washed with ethanol to give 754 mg (95 % purity, 82 % yield) of the title compound. LC-MS (Method 2): Rt = 0.49 min; MS (ESIpos): m / z = 280 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.53 - 7.59 (m, 1H), 7.64 (ddd, 1H), 7.69 (d, 1H), 7.78 - 7.86 (m, 1H), 8.32 (dd, 1H), 8.57 (dt, 1H), 8.77 (dd, 1H), 9.40 (dd, 1H), 14.09 (brs, 1H). Intermediate 88 2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazoline-5(6H)-thione 2-lsothiocyanatobenzonitrile (250 mg, 1.56 mmol) and pyridine-4-carbohydrazide (214 mg, 1.56 mmol) were solubilised in ethanol (50 mL) and the mixture was stirred at reflux overnight. The reaction was filtered, the solid was washed with ethanol and dried under reduced pressure to give 367 mg (100 % purity, 84 % yield) of the title compound. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.53 - 7.60 (m, 1H), 7.69 (d, 1H), 7.80 - 7.86 (m, 1H), 8.13-8.18 (m, 2H), 8.31 (dd, 1H), 8.80-8.84 (m, 2H), 14.12 (brs, 1H). Intermediate 89 2-(pyridazin-4-yl)[1,2,4]triazolo[1,5-c]quinazoline-5(6H)-thione N=N 2-lsothiocyanatobenzonitrile (CAS 81431-98-3, 100 mg, 624 pmol) and pyridazine-4-carbohydrazide (CAS 56932-26-4, 86.2 mg, 624 pmol) were solubilised in ethanol (2 mL) and the reaction mixture was stirred at reflux overnight. Precipitated product was filtered off, washed with ethanol and dried to give 138 mg (67 % purity, 53 % yield) of the title compound. LC-MS (Method 1): Rt = 0.71 min; MS (ESIpos): m / z = 281 [M+H]+ Intermediate 90 2-[4-(dimethylamino)phenyl][1,2,4]triazolo[1,5-c]quinazoline-5(6H)-thione HoC 2-lsothiocyanatobenzonitrile (CAS 81431-98-3, 186 mg, 1.16 mmol) and 4- (dimethylamino)benzohydrazide (CAS 19353-92-5, 208 mg, 1.16 mmol) were solubilised in ethanol (37 mL) and the reaction mixture was stirred at reflux overnight. Precipitated product was filtered off, washed with ethanol and dried to give 288 mg (86 % purity, 66 % yield) of the title compound. LC-MS (Method 2): Rt = 0.62 min; MS (ESIpos): m / z = 322 [M+H]+ 1H-NMR (400 MHz, DMSO-d6) 5 [ppm]: 1.035 (0.39), 1.052 (0.67), 1.070 (0.41), 2.518 (0.77), 2.523 (0.50), 2.948 (0.51), 2.997 (0.77), 3.014 (9.62), 3.020 (16.00), 6.767 (0.97), 6.789 (0.96), 6.843 (0.20), 6.850 (1.84), 6.855 (0.57), 6.867 (0.60), 6.872 (1.91), 6.879 (0.21), 7.251 (0.23), 7.270 (0.42), 7.287 (0.60), 7.306 (0.49), 7.506 (0.41), 7.508 (0.43), 7.526 (0.83), 7.544 (0.48), 7.546 (0.49), 7.635 (0.19), 7.651 (0.80), 7.671 (1.01), 7.761 (0.57), 7.765 (0.57), 7.779 (0.55), 7.782 (0.75), 7.785 (0.50), 7.800 (0.39), 7.804 (0.37), 7.872 (0.45), 7.893 (0.43), 8.052 (0.23), 8.059 (2.30), 8.064 (0.62), 8.077 (0.62), 8.082 (2.11), 8.089 (0.26), 8.098 (0.23), 8.118 (0.21), 8.261 (0.75), 8.264 (0.78), 8.281 (0.73), 8.284 (0.68), 10.864 (0.29). Intermediate 94 2-(furan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (200 mg, 1.14 mmol) and furan-2-carbohydrazide (143 mg, 1.14 mmol) were stirred in DMF (4.0 mL) at 120°C for 20 h. The reaction was diluted with water and the mixture was filtered. The solid was washed with water and dried under reduced pressure at 60°C to give 247 mg (80 % purity, 69 % yield) of the title compound. LC-MS (Method 2): Rt = 0.55 min; MS (ESIpos): m / z = 253 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 6.74 (dd, 1H), 7.25 (dd, 1H), 7.38 - 7.43 (m, 1H), 7.45 (d, 1H), 7.72 (ddd, 1H), 7.96 (dd, 1H), 8.19 (dd, 1H). (one proton is not visible.) Intermediate 95 5-chloro-2-(furan-2-yl)[1,2,4]triazolo[1,5-c]quinazoline 2-(Furan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (247 mg, 981 pmol) was solubilised in phosphorus(V) oxychloride (4.4 mL, 48 mmol), N,N-diisopropylethylamine (1.7 mL, 9.8 mmol) was added carefully and the mixture was stirred for 5 h at 110°C. The mixture was cooled to rt and concentrated under reduced pressure. The crude material was solubilized in DCM, poured into ice and stirred for 10 min. The solid was filtered, washed with water and dried under reduced pressure at 60°C to give 196 mg (80 % purity, 59 % yield) of the title compound without further purification. LC-MS (method 2): Rt = 1.15 min; MS (ESIpos): m / z = 271 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 6.78 (dd, 1H), 7.38 (dd, 1H), 7.86 (ddd, 1H), 7.96 - 8.07 (m, 3H), 8.46-8.52 (m, 1H). Intermediate 96 ethyl [2-(2-chloroquinazolin-4-yl)hydrazino](oxo)acetate To a stirredsuspension of 2-chloro-4-hydrazinylquinazoline (200 mg, 1.03 mmol) in dichloromethane (2 mL) was added triethylamine (0.43 mL, 3.08 mmol). At -5 °C ethyl chloro(oxo)acetate (132 pL, 1.18 mmol) was added dropwise. The reaction mixture was stirred at -5 °C to 0 °C for 1 hour. The precipitate was filtered off and washed with a small volume of water. The the precipitate in filtrate was filtered again but the second filtrate and the secont precipitate were combined and the pH was adjusted to 6 with hydrochloric acid (0.5M HCI, 0.6 mL). Dichloromethane (40 mL) was added, the layers were separated and the aqueous phase was extracted with dichloromethane. The combined organic phases were washed twice with water, dried over magnesium sulfate and concentrated giving 138 mg of the title compound which contained ca. 0.35 mole of trimethylamine and was used without purification in the next step. LC-MS (method 1): Rt = 0.81 min; MS (ESIpos): m / z = 295 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.32 (t, 3H), 4.33 (q, 2H), 7.49 - 7.65 (m, 2H), 7.79 (br s, 1H), 8.20 (brd, 1H), 10.16 (brs, 2H). Intermediate 97 ethyl 5-oxo-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazoline-2-carboxylate Ethyl [2-(2-chloroquinazolin-4-yl)hydrazino](oxo)acetate (13.6 g, 46.0 mmol) was stirred in acetic acid (136 mL) for 6h at reflux. The reaction mixture was then cooled to rt and diluted with ice cold water. The precipitate was filtered and the solid was washed with water and petroleum ether to give the title compound without further purification. Intermediate 98 ethyl 5-chloro[1,2,4]triazolo[1,5-c]quinazoline-2-carboxylate Ethyl 5-oxo-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazoline-2-carboxylate (11.4 g, 46.4 mmol) and N, N-diisopropylethylamine (36.0 g, 278 mmol) were stirred in POCI3 (114 mL). The reaction mixture was heated to reflux for 4h. The reaction mixture was cooled to rt and concentrated under reduced pressure. The crude mixture was diluted with DCM (200 mL) and ice cold water. The aqueous phase extracted with dichloromethane and the combined organic phase was dried (sodium sulphate), filtered and concentrated under reduced pressure to give the title compound without further purification. Intermediate 99 ethyl 5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-2-carboxylate Ethyl 5-chloro[1,2,4]triazolo[1,5-c]quinazoline-2-carboxylate (500 mg, 1.81 mmol), (3R)-3-aminoazepan-2-one (255 mg, 1.99 mmol) and N,N-diisopropylethylamine (630 pL, 3.6 mmol) were stirred in DMF (8.1 mL) for 2 h at 60°C. The reaction was cooled to rt and diluted with water. The solid was filtered, washed with water and dried under reduced pressure at 60°C to give 486 mg (73 % yield) of the title compound. LC-MS (method 2): Rt = 1.08 min; MS (ESIpos): m / z = 369 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.26 - 1.35 (m, 1H), 1.39 (t, 3H), 1.48 - 1.61 (m, 1H), 1.79- 1.94 (m, 2H), 1.97-2.06 (m, 1H), 2.26 - 2.35 (m, 1H), 3.10 - 3.21 (m, 1H), 3.30 - 3.41 (m, 1H), 4.47 (q, 2H), 4.82 (dd, 1H), 7.48 (ddd, 1H), 7.66 - 7.71 (m, 1H), 7.74 - 7.80 (m, 2H), 8.24 (dd, 1H), 8.29 (dd, 1H). Intermediate 100 7-fluoro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Ethyl (2-cyano-6-fluorophenyl)carbamate (200 mg, 961 pmol) and 3-fluorobenzohydrazide (178 mg, 1.15 mmol) were stirred in DMF (2.1 mL) overnight at 120°C. The reaction was cooled to rt 5 and diluted with water. The solid was filtered, washed with water and dried under reduced pressure at 60°C to give 240 mg (84 % yield) of the title compound without further purification. LC-MS (Method 2): Rt = 0.64 min; MS (ESIpos): m / z = 299 [M+H]+ The following intermediates were prepared similarly: Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 101 h3c 0 OCX F H 7-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.62 min; MS (ESIpos): m / z = 311 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 102 7-fluoro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin- 5(6H)-one LC-MS (Method 2): Rt = 0.47 min; MS (ESIpos): m / z = 285 [M+H]+ Intermediate 103 7-fluoro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.63 min; MS (ESIpos): m / z = 299 [M+H]+ Intermediate 104 2-(3-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.70 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.88 (s, 3H), 7.12 (ddd, 1H), 7.33 (t, 1H), 7.50 (t, 1H), 7.56 (d, 1H), 7.74 (dd, 1H), 7.83 (dt, 1H), 8.09-8.14 (m, 1H), 11.53 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 105 / VCH3 Ol 1 ch3 h 7-methyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.53 min; MS (ESIpos): m / z = 281 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.94 (s, 3H), 7.31 (t, 1H), 7.51 -7.57 (m, 1H), 8.01 (d, 1H), 8.04 (dd, 1H), 8.41 (s, 1H), 11.43 (s, 1H). Intermediate 106 h3c o ch3 h 2-(4-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.71 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.10-7.15 (m, 2H), 7.32 (t, 1H), 7.55 (d, 1H), 8.09 (d, 1H), 8.14-8.19 (m, 2H), 11.47 (br s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 107 2-(3-methoxyphenyl)-8-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.73 min; MS (ESIneg): m / z = 305 [M-H]“ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.44 (s, 3H), 3.87 (s, 3H), 7.11 (ddd, 1H), 7.20-7.27 (m, 2H), 7.48 (t, 1H), 7.71 (dd, 1H), 7.81 (dt, 1H), 8.11 (d, 1H), 12.28 (brs, 1H). Intermediate 108 8-methyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin- 5(6H)-one LC-MS (Method 2): Rt = 0.57 min; MS (ESIpos): m / z = 281 [M+H]+ Intermediate 109 8-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.65 min; MS (ESIpos): m / z = 311 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.12 (ddd, 1H), 7.19 (dd, 1H), 7.29 (td, 1H), 7.49 (t, 1H), 7.72 (dd, 1H), 7.81 (dt, 1H), 8.29 (dd, 1H), 12.45 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 110 O-CH3 H 8-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.65 min; MS (ESIpos): m / z = 311 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.09 - 7.14 (m, 2H), 7.19 (dd, 1H), 7.28 (td, 1H), 8.13-8.18 (m, 2H), 8.28 (dd, 1H), 12.40 (s, 1H). Intermediate 111 / =\ H 3 W / 7 ° 'N Yjl jL N^O H 2-(3-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.78 min; MS (ESIneg): m / z = 305 [M-H]-1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.45 (s, 3H), 3.88 (s, 3H), 7.12 (ddd, 1H), 7.35 (d, 1H), 7.49 (t, 1H), 7.54 (dd, 1H), 7.72 (dd, 1H), 7.81 (dt, 1H), 8.04 (d, 1H), 12.27 (br s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate ^N'N-CH3 112 'N Xjl JL H 9-methyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.59 min; MS (ESIpos): m / z = 281 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.43 (s, 3H), 3.94 (s, 3H), 7.34 (d, 1H), 7.52 (dd, 1H), 7.97 (s, 1H), 8.00 (s, 1H), 8.40 (s, 1H), 12.18 (s 1H). Intermediate / =\ H 3 ^-0 113 F Xi 1 H 9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.68 min; MS (ESIpos): m / z = 311 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.88 (s, 3H), 7.13 (ddd, 1H), 7.467.53 (m, 2H), 7.63 (td, 1H), 7.73 (dd, 1H), 7.82 (dt, 1H), 7.99 (dd, 1H), 12.41 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 114 / / 7 F Br N— / I JI N nn H 10-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.88 min; MS (ESIpos): m / z = 359 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.37 - 7.44 (m, 1H), 7.46 (dd, 1H), 7.58 (t, 1H), 7.65 (td, 1H), 7.70 (dd, 1H), 7.92 - 7.97 (m, 1H), 8.10 (dt, 1H), 12.54- 12.62 (s 1H). Intermediate 115 h3c 0 Br N—Z 1 JL n Ci X H 10-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.74 min; MS (ESIpos): m / z = 371 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.11 - 7.16 (m, 2H), 7.45 (dd, 1H), 7.56 (t, 1H), 7.68 (dd, 1H), 8.15-8.21 (m, 2H), 12.45 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 116 nSkkch3 Br N— / I Jl N UL X H 10-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.55 min; MS (ESIneg): m / z = 343 [M-H]-1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.95 (s, 3H), 7.44 (dd, 1H), 7.55 (t, 1H), 7.67 (dd, 1H), 8.00 (d, 1H), 8.39 (s, 1H), 12.42 (br s, 1H). Intermediate 117 F Br N— / T JI N Ci X H 10-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.75 min; MS (ESIneg): m / z = 357 [M-H]-1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.39 - 7.48 (m, 3H), 7.57 (t, 1H), 7.69 (dd, 1H), 8.25-8.32 (m, 2H), 12.51 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 118 / / 7 F Cl N— / I JI N nn H 10-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.74 min; MS (ESIpos): m / z = 315 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.38 - 7.45 (m, 2H), 7.51 (dd, 1H), 7.61 - 7.69 (m, 2H), 7.93 (ddd, 1H), 8.09 (dt, 1H), 12.55 (brs, 1H). Intermediate 119 h3c O Cl N— / T A n Ci 1 H 10-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.73 min; MS (ESIpos): m / z = 327 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.10-7.17 (m, 2H), 7.41 (dd, 1H), 7.49 (dd, 1H), 7.62 - 7.68 (m, 1H), 8.15 - 8.20 (m, 2H), 12.47 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 120 nSkkch3 Cl N— / T JI N UL X H 10-chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.54 min; MS (ESIpos): m / z = 301 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.94 (s, 3H), 7.40 (dd, 1H), 7.47 (dd, 1H), 7.61 - 7.67 (m, 1H), 8.01 (d, 1H), 8.41 (s, 1H), 12.43 (s, 1H). Intermediate 121 F Cl N— / I ji n Ci X H 10-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.74 min; MS (ESIpos): m / z = 315 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.38 - 7.46 (m, 3H), 7.50 (dd, 1H), 7.62 - 7.69 (m, 1H), 8.24 - 8.32 (m, 2H), 12.52 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 122 Z F f y—v F. ^F / t rt OTX H 2-(3-fluorophenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.79 min; MS (ESIpos): m / z = 349 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.38-7.46 (m, 1H), 7.66 (td, 1H), 7.76 (dd, 1H), 7.81 - 7.93 (m, 3H), 8.07 (dt, 1H), 12.71 (br s, 1H). Intermediate 123 h3c O f y—V R ^F / th Ci I H 2-(4-methoxyphenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5- c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.77 min; MS (ESIpos): m / z = 361 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.85 (s, 3H), 7.12 - 7.17 (m, 2H), 7.75 (dd, 1H), 7.80-7.89 (m, 2H), 8.13-8.18 (m, 2H), 12.62 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 124 CH3 / / N 13 F F—I— F N— / JI A N Ci X H 2-(1 -methyl-1 H-pyrazol-4-yl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5- c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.62 min; MS (ESIpos): m / z = 335 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.95 (s, 3H), 7.74 (dd, 1H), 7.79 - 7.88 (m, 2H), 7.98 (d, 1H), 8.36 (s, 1H), 12.58 (br s, 1H). Intermediate 125 F Fx 2-(4-fluorophenyl)-10-(trifluor 5(6H)-one LC-MS (Method 2): Rt = 0.79 n 1H-NMR (400MHz, DMSO-d6): 7.81 - 7.90 (m, 2H), 8.22 - 8.29 F t rt lx H omethyl)[1,2,4]triazolo[1,5-c]quinazolin- nin; MS (ESIpos): m / z = 349 [M+H]+ 6 [ppm]= 7.40 - 7.48 (m, 2H), 7.75 (dd, 1H), (m, 2H), 12.68 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate / / 7 F 126 Y UL 1 H 10-cyclopropyl-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.93 min; MS (ESIpos): m / z = 321 [M+H]+ H3C Intermediate 0 127 Y rC Ci 1 H 10-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin- 5(6H)-one LC-MS (Method 2): Rt = 0.95 min; MS (ESIpos): m / z = 333 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate JVCH3 128 Y rT UL JL H 10-cyclopropyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.69 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 0.85 (brd, 2H), 1.19 (brd, 2H), 3.73 - 3.84 (m, 1H), 3.94 (s, 3H), 6.90 (br d, 1H), 7.23 (br d, 1H), 7.54 (br t, 1H), 8.01 (s, 1H), 8.41 (s, 1H), 12.19 (br s, 1H). Intermediate / =\ H 3 129 ch3 n— / I 0 II V 1 II N OL £ H 2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.92 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.97 (s, 3H), 3.87 (s, 3H), 7.12 (ddd, 1H), 7.22 - 7.27 (m, 1H), 7.30 (d, 1H), 7.50 (t, 1H), 7.54 - 7.60 (m, 1H), 7.73 (dd, 1H), 7.83 (dt, 1H), 12.29 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 130 h3c 0 ch3 n— / I 0 II " 1 / / N Ci X H 2-(4-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.89 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.96 (s, 3H), 3.85 (s, 3H), 7.10 -7.15 (m, 2H), 7.24 (d, 1H), 7.29 (d, 1H), 7.53 - 7.60 (m, 1H), 8.14 - 8.19 (m, 2H), 12.24 (s, 1H). Intermediate 131 CH3 N CH3 N— / 1 JI N Ci I H 10-methyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.68 min; MS (ESIpos): m / z = 281 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.93 (s, 3H), 3.94 (s, 3H), 7.22 (d, 1H), 7.29 (d, 1H), 7.51 -7.58 (m, 1H), 8.01 (s, 1H), 8.41 (s, 1H), 12.20 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 132 H3C-0 up Ci 1 H 10-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.61 min; MS (ESIpos): m / z = 311 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.87 (s, 3H), 7.13 (dd, 1H), 7.23 -7.32 (m, 2H), 7.50 (t, 1H), 7.66-7.77 (m, 2H), 7.82 (brd, 1H), 12.53 (s, 1H). Intermediate 133 5-chloro-7-fluoro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline 5 7-Fluoro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (100 mg, 335 pmol) was solubilised in phosphorus(V) oxychloride (1.1 mL, 12 mmol), N,N-diisopropylethylamine (580 pL, 3.4 mmol) was added carefully and the mixture was stirred overnight at 110°C. The reaction mixture was cooled to rt, poured into ice and stirred for 1 h. The solid was filtered, washed with water and dried at 60°C under reduced pressure to give 91.0 mg (97 % purity, 83 % yield) of the 10 title compound. The compound was used without further purification. LC-MS (method 2): Rt = 1.40 min; MS (ESIpos): m / z = 317 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.43 - 7.50 (m, 1H), 7.68 (td, 1H), 7.84 - 7.92 (m, 2H), 8.00 (ddd, 1H), 8.15 (dt, 1H), 8.31 - 8.37 (m, 1H). The following intermediates were prepared similarly: Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 134 h3c 0 oxx F 5-chloro-7-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.35 min; MS (ESIpos): m / z = 329 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.87 (s, 3H), 7.11 - 7.18 (m, 2H), 7.81 - 7.89 (m, 2H), 8.21 - 8.27 (m, 2H), 8.29 - 8.34 (m, 1H). Intermediate 135 A / ": OCX ^V^N^CI F 5-chloro-7-fluoro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 0.98 min; MS (ESIpos): m / z = 303 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.96 (s, 3H), 7.80 - 7.87 (m, 2H), 8.10 (s, 1H), 8.23 - 8.28 (m, 1H), 8.55 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 136 F F 5-chloro-7-fluoro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.38 min; MS (ESIpos): m / z = 317 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.41 - 7.48 (m, 2H), 7.83 - 7.90 (m,2H), 8.30-8.38 (m, 3H). Intermediate 137 / =\ H 3 COL ch3 5-chloro-2-(3-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.53 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.70 (s, 3H), 3.89 (s, 3H), 7.16 (ddd, 1H), 7.52 (t, 1H), 7.71 - 7.79 (m, 2H), 7.85 (d, 1H), 7.89 (d, 1H), 8.36 (d, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 138 ^N'N'CH3 Out ch3 5-chloro-7-methyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.13 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.68 (s, 3H), 3.96 (s, 3H), 7.69 -7.75 (m, 1H), 7.80 - 7.86 (m, 1H), 8.08 (s, 1H), 8.28 (dd, 1H), 8.53 (s, 1H). Intermediate 139 h3c 0 Out ch3 5-chloro-2-(4-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.52 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.69 (s, 3H), 3.86 (s, 3H), 7.11 -7.17 (m, 2H), 7.70 - 7.76 (m, 1H), 7.83 (d, 1H), 8.19 - 8.25 (m, 2H), 8.30 -8.36 (m, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate / =\ H 3 140 XjOL Hgc^^^N^CI 5-chloro-2-(3-methoxyphenyl)-8-methyl[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.44 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.58 (s, 3H), 3.89 (s, 3H), 7.16 (ddd, 1H), 7.52 (t, 1H), 7.70 (dd, 1H), 7.77 (dd, 1H), 7.85 (s, 1H), 7.88 (dt, 1H), 8.41 (d, 1H). Intermediate ^•N"N-CH3 141 jOuL H gC^^^N^CI 5-chloro-8-methyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.07 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.56 (s, 3H), 3.95 (s, 4H), 7.67 (dd, 1H), 7.82 (s, 1H), 8.08 (d, 1H), 8.33 (d, 1H), 8.52 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 142 / =\ H 3 / 7 ° Xjfx F^^^N^CI 5-chloro-8-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.40 min; MS (ESIpos): m / z = 329 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.89 (s, 3H), 7.17 (ddd, 1H), 7.53 (t, 1H), 7.73 - 7.80 (m, 2H), 7.88 (dt, 1H), 7.93 (dd, 1H), 8.59 (dd, 1H). Intermediate 143 h3c 0 5-chloro-8-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.39 min; MS (ESIpos): m / z = 329 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.86 (s, 3H), 7.14 - 7.17 (m, 2H), 7.75 (td, 1H), 7.91 (dd, 1H), 8.20 - 8.24 (m, 2H), 8.57 (dd, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 144 / =\ H 3 W / 7 ° h3c^^J( > ^^^N^CI 5-chloro-2-(3-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.48 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.60 (s, 3H), 3.89 (s, 3H), 7.16 (ddd, 1H), 7.52 (t, 1H), 7.76 - 7.83 (m, 2H), 7.88 (dt, 1H), 7.93 (d, 1H), 8.33 (dd, 1H). Intermediate 145 A-CH'= XYa 5-chloro-9-methyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.09 min; MS (ESIpos): m / z = 299 [M+H]+ Intermediate 146 / =\ H 3 w / 7 ° F „ 5-chloro-9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.41 min; MS (ESIpos): m / z = 329 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.89 (s, 3H), 7.17 (ddd, 1H), 7.53 (t, 1H), 7.78 (dd, 1H), 7.84 - 7.91 (m, 2H), 8.13 (dd, 1H), 8.26 (dd, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 147 Z F Br N— / T JI N OCX 10-bromo-5-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.54 min; MS (ESIpos): m / z = 377 [M+H]+ Intermediate 148 h3c 0 Br N— / T JL N ^^^N^CI 10-bromo-5-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.49 min; MS (ESIpos): m / z = 389 [M+H]+ Intermediate 149 CH3 Br N— / I JI N 10-bromo-5-chloro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.12 min; MS (ESIpos): m / z = 363 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 150 F Br N— / I JI N ^^^N^CI 10-bromo-5-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.53 min; MS (ESIpos): m / z = 377 [M+H]+ Intermediate 151 / / / F Cl N— / T JI N ^^^N^CI 5,10-dichloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.51 min; MS (ESIpos): m / z = 333 [M+H]+ Intermediate 152 h3c 0 Cl N— / T JL n uCX ^^^N^CI 5,10-dichloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.46 min; MS (ESIpos): m / z = 345 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.14 - 7.19 (m, 2H), 7.89 - 8.02 (m, 3H), 8.22 - 8.28 (m, 2H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 153 N CH3 N Cl N— / cYx" ^^N^CI 5,10-dichloro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.08 min; MS (ESIpos): m / z = 319 [M+H]+ Intermediate 154 F Cl N— / I JL n oSX ^^^N^CI 5,10-dichloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.50 min; MS (ESIpos): m / z = 333 [M+H]+ Intermediate 155 Z F f y—" F. ^F / tn ^^^N^CI 5-chloro-2-(3-fluorophenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.52 min; MS (ESIpos): m / z = 367 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 156 F Fx 5-chloro-2-(4-methoxyphen> c]quinazoline LC-MS (Method 2): Rt = 1.49 r h3c 0 t rt ^^N^CI 1)-10-(trifluoromethyl)[1,2,4]triazolo[1,5- nin; MS (ESIpos): m / z = 379 [M+H]+ Intermediate 157 CH3 Zz N f y=x t rt COL 5-chloro-2-(1 -methyl-1 H-pyrazol-4-yl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.17 min; MS (ESIpos): m / z = 353 [M+H]+ Intermediate 158 F F^ 5-chloro-2-(4-fluorophenyl)-c]quinazoline LC-MS (Method 2): Rt = 1.52 r F _F / t rt xX 10-(trifluoromethyl)[1,2,4]triazolo[1,5- nin; MS (ESIpos): m / z = 367 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 159 Z F OCX 5-chloro-10-cyclopropyl-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.63 min; MS (ESIpos): m / z = 339 [M+H]+ Intermediate 160 h3c 0 ^^^N^CI 5-chloro-10-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.58 min; MS (ESIpos): m / z = 351 [M+H]+ Intermediate 161 ArCHs Oli 5-chloro-10-cyclopropyl-2-(1 -methyl-1 H-pyrazol-4- yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.25 min; MS (ESIpos): m / z = 325 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 162 / =\ H 3 ch3 n— / I II '' 1 JI N 5-chloro-2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.55 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.09 (s, 3H), 3.88 (s, 3H), 7.15 (ddd, 1H), 7.52 (t, 1H), 7.65 - 7.70 (m, 1H), 7.76 (dd, 1H), 7.80 - 7.86 (m, 2H), 7.86-7.90 (m, 1H). Intermediate 163 h3c 0 ch3 n— / I II V 1 JI N 5-chloro-2-(4-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5- c]quinazoline LC-MS (Method 2): Rt = 1.54 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (500MHz, DMSO-d6): 6 [ppm]= 3.10 (s, 3H), 3.86 (s, 3H), 7.16 (d, 2H), 7.66 - 7.70 (m, 1H), 7.81 - 7.87 (m, 2H), 8.22 - 8.27 (m, 2H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate CH N"UM3 164 ch3 n— / 1 JI N oTX 5-chloro-10-methyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.18 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.06 (s, 3H), 3.96 (s, 3H), 7.64 -7.68 (m, 1H), 7.80-7.85 (m, 2H), 8.08 (s, 1H), 8.52 (s, 1H). Intermediate / =\ H 3 165 W / 7 ° F N- / 65" 5-chloro-10-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 0.92 min; MS (ESIpos): m / z = 329 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.89 (s, 3H), 7.17 (ddd, 1H), 7.53 (t, 1H), 7.70-7.79 (m, 2H), 7.86-7.91 (m, 2H), 7.94-8.02 (m, 1H). Intermediate 166 benzyl 6-{[2-(1-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-5-oxo-1,4-diazepane-1 -carboxylate 5-Chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline, (211 mg, 739 pmol)-, benzyl 6-amino-5-oxo-1,4-diazepane-1-carboxylate (292 mg, 1.11 mmol) and N,N-diisopropylethylamine (260 pL, 1.5 mmol) were stirred in DMSO (3.0 mL) for 2 h at 60°C. The mixture was cooled to rt and diluted with water. The solid was filtered, washed with water and dried under reduced pressure at 60°C to give 182 mg (55 % purity, 26 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 1.08 min; MS (ESIpos): m / z = 512 [M+H]+ Intermediate 167 benzyl 6-{[2-(1-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-5-oxo-1,4-diazepane-1-carboxylate, enantiomer 1 Chiral HPLC separation of benzyl 6-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-5-oxo-1,4-diazepane-1-carboxylate was performed (Instrument: Labomatic HD5000, Labocord-5000; Gilson GX-241, Labcol Vario 4000; Column: Chiralpak IA 5p 250x30mm; Eluent: methanol + 0.1 vol-% diethylamine (99%) / ethanol 50:50%; flow rate 40.0 mL / min; UV 254 nm). Retention time of enantiomer 1: 5.73 min; [a]20 D :-96° (c=1) in DMSO. Instrument: Agilent HPLC 1260; Column: Chiralpak IA 3p 100x4,6mm; Eluent: methanol + 0.1 vol-% diethylamine (99%) / ethanol 50:50; flow rate 1.4 mL / min; temperature: 25 °C; DAD 254 nm Intermediate 168 benzyl 6-{[2-(1-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-5-oxo-1,4- diazepane-1-carboxylate, enantiomer 2 5 The title compound was prepared as described for intermediate 162. Retention time of enantiomer 2: 9.64 min [a]20 D :+95° (c=1) in DMSO The following intermediates were prepared in analogy to intermediate 161: Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 169 h3c 0 o o JI N OCa / O N H H H 0 benzyl 6-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-5-oxo-1,4-diazepane-1-carboxylate LC-MS (Method 2): Rt = 1.35 min; MS (ESIneg): m / z = 536 [M-H]-1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.90 - 3.15 (m, 1H), 3.42 - 3.56 (m, 1H), 3.86 (s, 3H), 4.10-4.27 (m, 1H), 4.55 - 4.70 (m, 1H), 4.88 - 5.01 (m, 1H), 5.20 (s, 2H), 7.11 - 7.24 (m, 4H), 7.31 - 7.49 (m, 5H), 7.60 - 7.80 (m, 1H), 7.85 (d, 1H), 8.19-8.26 (m, 2H), 8.30 (brd, 1H), 8.37-8.54 (m, 1H) Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 170 "TA A / N CXX XX H H H 0 benzyl 6-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5- yl]amino}-5-oxo-1,4-diazepane-1-carboxylate LC-MS (Method 2): Rt = 1.45 min; MS (ESIneg): m / z = 520 [M-H]- 1H-NMR (400MHz, DMSO-d6): 6 [ppm]=), 2.73 (s, 3H), 2.92 - 3.13 (m, 1H), 3.44-3.55 (m, 1H), 4.13 - 4.29 (m, 1H), 4.58 - 4.72 (m, 1H), 4.87 - 5.00 (m, 1H), 5.20 (br s, 2H), 7.19 (br s, 2H), 7.29 - 7.52 (m, 8H), 7.60 - 7.81 (m, 1H), 7.89 (d, 1H), 8.14 (br d, 1H), 8.31 (brd, 1H), 8.36-8.53 (m, 1H). Intermediate 171 h3c 0 o o ch3 n— / 1 JI N CXX xx H / / H O benzyl 6-{[2-(4-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5- c]quinazolin-5-yl]amino}-5-oxo-1,4-diazepane-1-carboxylate LC-MS (Method 2): Rt = 1.52 min; MS (ESIpos): m / z = 552 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 172 H3C-0 O O ___ JI N OOL jO H n H O benzyl 6-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-5-oxo-1,4-diazepane-1-carboxylate LC-MS (Method 2): Rt = 1.38 min; MS (ESIneg): m / z = 536 [M-Hf Intermediate 173 Ethyl (2-chloro-6-cyanophenyl)carbamate Y^NH ci 0^0 Ch3 5 2-Amino-3-chlorobenzonitrile (928 mg, 6.08 mmol) was stirred in ethyl carbonochloridate (9.3 mL, 97 mmol) for 48 h at reflux. The reaction mixture was cooled to rt and concentrated under reduced pressure to give 1.36 g (99 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 0.89 min; MS (ESIpos): m / z = 225 [M+H]+ 10 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.23 (t, 3H), 4.13 (q, 2H), 7.49 (t, 1H), 7.89 (ddd, 2H), 9.71 (brs, 1H). Intermediate 174 Ethyl [2-cyano-6-(trifluoromethyl)phenyl]carbamate 2-Amino-3-(trifluoromethyl)benzonitrile (500 mg, 2.69 mmol) was stirred in ethyl carbonochloridate (3.0 mL, 31 mmol) for 7 days at reflux. The mixture cooled to rt and concentrated under reduced pressure to give 621 mg (90 % yield) of the title compound that was 5 used without further purification. LC-MS (method 2): Rt = 1.01 min; MS (ESIpos): m / z = 259 [M+H]+ Intermediate 175 Ethyl (2-cyano-6-methoxyphenyl)carbamate o X h3cx o^o^ch3 10 2-Amino-3-methoxybenzonitrile (500 mg, 3.37 mmol) was stirred in ethyl carbonochloridate (4.8 mL, 51 mmol) for 18 h at reflux. The reaction mixture was cooled to rt and concentrated under reduced pressure to give 450 mg (61 % yield) of the title compound that was used without further purification. LC-MS (Method 2): Rt = 0.85 min; MS (ESIpos): m / z = 221 [M+H]+ 15 1H NMR (400MHz, DMSO-d6) 6 ppm= 9.13 (br s, 1 H), 7.31 - 7.52 (m, 3 H), 4.08 (q, 2 H), 3.83 (s, 3 H), 1.20 (t, 3 H). Intermediate 176 2-Amino-3-cyclopropylbenzonitrile 2-Amino-3-bromobenzonitrile (500 mg, 2.54 mmol) was solubilised in 1,4-dioxane (27 mL). cyclopropylboronic acid (262 mg, 3.05 mmol), cesium carbonate (3.31 g, 10.2 mmol) and bis(diphenylphosphino)ferrocene)dichlorpalladium(ll)*dichlormethane complex (414 mg, 508 pmol) were added and the reaction was stirred for 10 min at 130 °C under microwave irradiation. The reaction mixture was filtered and the filtrate was concentrated under reduced pressure. The crude material was purified by flash column chromatography to give 275 mg (91 % purity, 62 % yield) of the title compound. LC-MS (method 2): Rt = 1.04 min; MS (ESIpos): m / z = 159 [M+H]+ Intermediate 177 Ethyl (2-cyano-6-cyclopropylphenyl)carbamate A o^o ^ch3 2-Amino-3-cyclopropylbenzonitrile (275 mg, 1.74 mmol) was stirred in ethyl carbonochloridate (2.5 mL, 26 mmol) for 4 h at reflux. The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure to give 380 mg (85 % purity, 81 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 1.00 min; MS (ESIneg): m / z = 229 [M-H]- Intermediate 178 Ethyl (2-bromo-6-cyanophenyl)carbamate Y^NH Br O^O ^CH3 2-Amino-3-bromobenzonitrile (5.00 g, 25.4 mmol) was stirred in ethyl carbonochloridate (29 mL, 300 mmol) for 18 h at reflux. The mixture was cooled to rt and concentrated under reduced pressure to give 6.20 g (84 % purity, 76 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 0.90 min; MS (ESIpos): m / z = 269 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 1.23 (brt, 3H), 4.13 (q, 2H), 7.41 (t, 1H), 7.91 (dd, 1H), 8.00-8.12 (m, 1H), 9.66 (br s, 1H). Intermediate 179 Ethyl (2,4-dibromo-6-cyanophenyl)carbamate 2-Amino-3,5-dibromobenzonitrile (750 mg, 2.72 mmol) was stirred in ethyl carbonochloridate (5.0 mL, 52 mmol) for 18 h at reflux. The mixture was concentrated under reduced pressure to give 851 mg (66 % purity, 59 % yield) of the title compound that was used without further purification. LC-MS (Method 2): Rt = 1.07 min; MS (ESIpos): m / z = 347 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.29 (t, 3H), 4.19 (q, 2H), 8.32 (d, 1H), 8.42 (d, 1H), 9.78 (brs, 1H). Intermediate 180 Ethyl (2-cyano-5-methoxyphenyl)carbamate 2-Amino-4-methoxybenzonitrile (100 mg, 675 pmol) was stirred in ethyl carbonochloridate (1.4 mL, 15 mmol) for 18 h at 100 °C. The reaction mixture was cooled to rt and concentrated under reduced pressure to give 406 mg (74% yield) of the title compound that was used without further purification LC-MS (Method 2): Rt = 0.96 min; MS (ESIpos): m / z = 221 [M+H]+ WO 2021 / 028382 PCT / EP2020 / 072377 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 1.24 (t, 3H), 3.81 (s, 3H), 4.14 (q, 2H), 6.88 (dd, 1H), 7.09 (d, 1H), 7.70 (d, 1H), 9.66 (s, 1H). Intermediate 181 Ethyl (2-cyano-4,5-dimethoxyphenyl)carbamate CH3 2-Amino-4,5-dimethoxybenzonitrile (300 mg, 1.68 mmol) was stirred in ethyl carbonochloridate (2.9 mL, 31 mmol) for 6 h at reflux. The reaction mixture was cooled to rt and concentrated under reduced pressure to give 402 mg (100 % purity, 95 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 0.88 min; MS (ESIpos): m / z = 251 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.23 (t, 3H), 3.80 (s, 3 H), 3.78 (s, 3 H)4.12 (q, 2H), 7.05 (s, 1H), 7.30 (s, 1H), 9.48 (br s, 1H). Intermediate 182 Ethyl [2-cyano-5-(trifluoromethyl)phenyl]carbamate 2-Amino-4-(trifluoromethyl)benzonitrile (100 mg, 537 pmol) was stirred with ethyl carbonochloridate (1.0 mL) at 110 °C for 18 h. The reaction mixture was cooled to rt and concentrated under reduced pressure to give 136 mg (98 % yield) of the title compound that was used without further purification. LC-MS (Method 2): Rt = 1.14 min; MS (ESIneg): m / z = 257 [M-H]’ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.26 (t, 3H), 4.17 (q, 2H), 7.67 (d, 1H), 7.93 (s, 1H), 8.06 (d, 1H), 10.09 (s, 1H). Intermediate 183 Ethyl (5-bromo-2-cyanophenyl)carbamate ch3 2-Amino-4-bromobenzonitrile (400 mg, 2.03 mmol) was stirred in ethyl carbonochloridate (4.0 mL, 6.1 mmol) for 18 h at 110 °C. The reaction mixture was cooled to rt and concentrated under reduced pressure to give 406 mg (74 % yield) of the title compound that was used without further purification. LC-MS (Method 2): Rt = 1.10 min; MS (ESIpos): m / z = 269 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.25 (t, 3H), 4.16 (q, 2H), 7.54 (dd, 1H), 7.76 (d, 1H), 7.79 (d, 1H), 9.93 (s, 1H). Intermediate 184 Ethyl (2-cyano-4-fluorophenyl)carbamate 2-Amino-5-fluorobenzonitrile (300 mg, 2.20 mmol) was stirred in ethyl carbonochloridate (8.7 mL) for 6 h at reflux. The mixture was cooled to rt and concentrated under reduced pressure to give 463 mg (99 % purity, 100 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 0.93 min; MS (ESIpos): m / z = 207 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.25 (t, 3H), 4.15 (q, 2H), 7.49 - 7.55 (m, 1H), 7.55 -7.62 (m, 1H), 7.83 (dd, 1H), 9.74 (s, 1H). Intermediate 185 Ethyl (4-chloro-2-cyanophenyl)carbamate 2-Amino-5-chlorobenzonitrile (150 mg, 983 pmol) was stirred in ethyl carbonochloridate (3.9 mL) for 6 h at reflux. The mixture was cooled to rt and concentrated under reduced pressure to give 205 mg (100 % purity, 93 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 1.06 min; MS (ESIneg): m / z = 212 [M-H]’ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.25 (t, 3H), 4.15 (q, 2H), 7.54 (d, 1H), 7.74 (dd, 1H), 7.99 (d, 1H), 9.85 (s, 1H). Intermediate 186 Ethyl (2-cyano-4-methoxyphenyl)carbamate 2-Amino-5-methoxybenzonitrile (300 mg, 2.02 mmol) was stirred in ethyl carbonochloridate (8.0 mL) for 6 h at reflux. The mixture was cooled to rt and concentrated under reduced pressure to give 439 mg (96 % purity, 94 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 0.92 min; MS (ESIpos): m / z = 221 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.23 (t, 3H), 3.79 (s, 3H), 4.11 (q, 2H), 7.24 (dd, 1H), 7.35 (d, 1H), 7.38 (d, 1H), 9.47 (br s, 1H). Intermediate 187 Ethyl (4-bromo-2-cyanophenyl)carbamate H 2-Amino-5-bromobenzonitrile (600 mg, 3.05 mmol) was stirred in ethyl carbonochloridate (12 mL) for 6 h at reflux. The mixture was cooled to rt and concentrated under reduced pressure to give 835 mg of the title compound that was used without further purification. LC-MS (method 2): Rt = 1.09 min; MS (ESIneg): m / z = 267 [M-H]- 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.25 (t, 3H), 4.15 (q, 2H), 7.47 (d, 1H), 7.86 (dd, 1H), 8.09 (d, 1H), 9.84 (s, 1H). Intermediate 188 Ethyl (2-cyano-3-fluorophenyl)carbamate 2-Amino-6-fluorobenzonitrile (500 mg, 3.67 mmol) was stirred in ethyl carbonochloridate (7.0 mL, 73 mmol) for 18 h at 100 °C. The mixture was cooled to rt and concentrated under reduced 5 pressure to give 755 mg (99 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 0.96 min; MS (ESIneg): m / z = 207 [M-H]- 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.25 (t, 3H), 4.16 (q, 2H), 7.23 - 7.32 (m, 1H), 7.38 (d, 1H), 7.72 (td, 1H), 10.00 (s, 1H). 10 Intermediate 189 Ethyl (2-cyano-3-methoxyphenyl)carbamate 2-Amino-6-methoxybenzonitrile (200 mg, 1.35 mmol) was stirred in ethyl carbonochloridate (2.4 mL, 25 mmol) for 18 h at reflux The mixture was cooled to rt and concentrated under reduced 15 pressure to give 276 mg (75 % purity, 70 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 0.94 min; MS (ESIneg): m / z = 219 [M-H]- Intermediate 190 Ethyl 1-(propan-2-yl)-1 H-pyrazole-4-carboxylate Ethyl 1 H-pyrazole-4-carboxylate (100 mg, 714 pmol) was solubilised in anhydrous DMF (1.0 mL) and the mixture was cooled to 0 °C. Sodium hydride (37.1 mg, 60 % purity in mineral oil, 928 pmol) was added and the reaction mixture was stirred for 15 min at 0 °C. 2-lodopropane (85 pL, 860 pmol) was then added and the mixture was stirred for 18 h at rt. Saturated aqueous sodium hydrogencarbonate was added and the mixture was extracted with ethyl acetate. The organic layer was dried over a silicone filter and concentrated under reduced pressure to give 120 mg (92 % yield) of the title compound that was used without further purification. LC-MS (method 2): Rt = 0.93 min; MS (ESIpos): m / z = 183 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.26 (t, 3H), 1.41 (d, 6H), 4.20 (q, 2H), 4.55 (spt, 1H), 7.84 (s, 1H), 8.34 (s, 1H). Intermediate 191 1-(Propan-2-yl)-1H-pyrazole-4-carbohydrazide Ethyl 1-(propan-2-yl)-1H-pyrazole-4-carboxylate (60.0 mg, 329 pmol) was solubilised in ethanol (1.2 mL), hydrazine monohydrate (32 pl, 660 pmol) was added and the mixture was stirred for 18 h at rt. The reaction mixture was concentrated under reduced pressure to give 57 mg of the title compound that was used without further purification. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.40 (d, 6H), 4.00-4.42 (brs, 2H), 4.49 (spt, 1H), 7.82 (s, 1H), 8.17 (s, 1H), 9.28 (s, 1H). Intermediate 192 5-Methyl-1,3,4-oxadiazole-2-carbohydrazide 0 h3c Ethyl 5-methyl-1,3,4-oxadiazole-2-carboxylate (50.0 mg, 320 pmol) and hydrazine hydrate (78 pL, 1.6 mmol) were stirred in ethanol (2.0 mL) for 18 h at rt. The reaction mixture was then poured into water and lyophilised to give 30.0 mg (66 % yield) of the title compound that was used without further purification. Intermediate 193 Ethyl 4-chloro-2-(trifluoromethoxy)benzoate 4-Chloro-2-(trifluoromethoxy)benzoic acid (1.00 g, 4.16 mmol) in thionyl chloride (1.7 mL, 24 mmol) was stirred for 15 min at rt. At 0 °C ethanol (8.3 mL) was carefully added under strong gas evelution. After 30 min the reaction was stirred at 80 °C for 2.5 h. The reaction was allowed to cool down to rt and concentrated under vacuum. Aqueous saturated sodium hydrogencarbonate solution (25 mL) was added and the aqueous phase was extracted three times with ethyl acetate. The combined organic layers were dried over sodium sulfate and concentrated to give 1.12 g of the title compound which was used without further purification in the next step. LC-MS (Method 1): Rt = 1.40 min; MS (ESIpos): m / z = 269 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.30 (t, 3H), 4.33 (q, 2H), 7.68 (dd, 1H), 7.72 - 7.74 (m, 1H), 7.97 (d, 1H). Intermediate 194 Ethyl 5-chloro-2-(trifluoromethoxy)benzoate 5-Chloro-2-(trifluoromethoxy)benzoic acid (370 mg, 1.54 mmol) was dissolved in ethanol (3.5 mL). On an ice bath thionyl chloride (640 pL, 8.8 mmol) was carefully added under gas evolution and stirring was continued for 145 min on the ice bath. It was stirred for two hours under reflux and overnight at rt. The reaction mixture was concentrated under vacuum. The residue was treated twice with dichloriomethane and concentrated under reduced pressure obtaing 401 mg (97%) of the title compound which was used without further purification in the next step. LC-MS (Method 1): Rt = 1.42 min; MS (ESIpos): m / z = 269 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 1.30 (t, 3H), 4.33 (q, 2H), 7.58 (qd, 1H), 7.83 (dd, 1H), 7.95 (d, 1H). Intermediate 195 4-Chloro-2-(trifluoromethoxy)benzohydrazide F F\DF Ethyl 4-chloro-2-(trifluoromethoxy)benzoate (1.12 g, 4.15 mmol) and hydrazine hydrate (2.0 mL, 42 mmol) in ethanol (18 mL) were stirred at 80 °C for 22 h. The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure. Saturated aqueous ammonium chloride solution (50 mL) was added and it was extracted three time with ethyl acetate. The combined organic layers were dried over sodium sulfate and concentrated to afford 579 mg of the title compound which was used without further purification in the next step. LC-MS (Method 1): Rt = 0.84 min; MS (ESIpos): m / z = 255 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 4.54 (br s, 2H), 7.55 - 7.57 (m, 2H), 7.60 - 7.62 (m, 1H), 9.65 (brs, 1H). Intermediate 196 5-(Trifluoromethyl)pyridine-3-carbohydrazide Ammonium 5-(trifluoromethyl)nicotinate (500 mg, 2.40 mmol) was suspended in ethanol (3.0 mL). Sulfuric acid (96%, 147 pL, 2.8 mmol) was added and stirred under reflux for 23 h. Thionyl chloride (350 pL, 4.8 mmol) was added and the reaction mixture was stirred under reflux overnight. The reaction mixture was allowed to cool down to rt and hydrazine hydrate (930 pL, 19 mmol) was added and stirred overnight at rt. Then it was stirred under reflux overnight. The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure. Water was added and the aqueous phase was extracted four time with 1-butanol. The combined organic phases were dried over magnesium sulfate and concentrated. The residue was purified by HPLC. The collected aqueous fractions were concentrated under reduced pressure. Dichloromethane was added and evaporated under reduced pressure. This was repeated once more to give 149 mg (30%) of the title compound which was used without further purification in the next step. LC-MS (Method 2): Rt = 0.56 min; MS (ESIpos): m / z = 206 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 4.67 (brs, 2H), 8.52 (s, 1H), 9.11 - 9.16 (m, 1H), 9.23 - 9.26 (m, 1H), 10.20 (brs, 1H). Intermediate 197 3-(Methanesulfonyl)benzohydrazide NH2 H 3 O o Methyl 3-(methanesulfonyl)benzoate (100 mg, 467 pmol) was dissolved in methanol (2.3 mL). Hydrazine hydrate (114 pL, 2.33 mmol) was added and it was heated at 140 °C for 1 h in a microwave reactor (high absorption). The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure. The residue was partioned between saturated aqueous ammonium chloride solution and ethyl acetate. The layers were separated and the aqueous phase was extracted with ethyl acetate. The combined organic layers were washed with brine, dried over sodium sulfate, concentrated under reduce pressure and dried at 50 °C under vaccum yielding 54 mg (49%) of the title compound which was used without further purification in the next step. LC-MS (Method 1): Rt = 0.47 min; MS (ESIpos): m / z = 215 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.26 (s, 3H), 4.60 (brs, 2H), 7.75 (t, 1H), 8.06 (ddd, 1H), 8.13 (ddd, 1H), 8.33 (t, 1H), 10.05 (s, 1H). Intermediate 198 6-(Trifluoromethyl)pyridine-2-carbohydrazide O Methyl 6-(trifluoromethyl)pyridine-2-carboxylate (648 mg, 3.16 mmol) was dissolved in methanol (15 mL). Hydrazine hydrate (730 pL, 15 mmol) was added and it was heated at 140 °C for 1 h in a microwave reactor (high absorption). The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure. The residue was partioned between saturated aqueous ammonium chloride solution (15 mL) and ethyl acetate (15 mL). The layers were separated and the aqueous phase was extracted with ethyl acetate (twice 15 mL). The combined organic layers were washed with brine (10 mL), dried over magnesium sulfate, and concentrated under reduce pressure yielding 624 of the title compound which was used without further purification in the next step. LC-MS (Method 2): Rt = 0.67 min; MS (ESIpos): m / z = 206 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 4.66 (br s, 2H), 8.08 (dd, 1H), 8.21 - 8.30 (m, 2H), 9.92 (brs, 1H). Intermediate 199 5-Chloro-2-(trifluoromethoxy)benzohydrazide Ethyl 5-chloro-2-(trifluoromethoxy)benzoate (397 mg, 1.48 mmol) was dissolved in ethanol (3.2 mL) and hydrazine hydrate (360 pL, 7.4 mmol) was added. It was stirred at 90 °C bath temperature for 70 h. The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure. The residue and the residue of a second batch (ethyl 5-chloro-2-(trifluoromethoxy)benzoate, 58 mg, 216 pmol) which was synthesized under similar conditions was added. The combined residue was treated twice with dichloromethane and concentrated under reduce pressure to give 374 mg of the title compound which was used without further purification in the next step. LC-MS (Method 2): Rt = 0.84 min; MS (ESIpos): m / z = 255 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 4.54 (brs, 2H), 7.48 (qd, 1H), 7.58 (d, 1H), 7.66 (dd, 1H), 9.69 (brs, 1H). Intermediate 200 4-Methoxythiophene-3-carbohydrazide Methyl 4-methoxythiophene-3-carboxylate (938 mg, 4.45 mmol) was dissolved in ethanol (32.3 mL) and hydrazine hydrate (1.33 mL, 27.2 mmol) was added. It was stirred at 85 °C bath temperature for 44 h. The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure to obtain 935 mg (99.7%) of the title compound which was used without further purification in the next step. LC-MS (Method 2): Rt = 0.56 min; MS (ESIpos): m / z = 173 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.84 (s, 3H), 4.49 (brs, 2H), 6.73 (d, 1H), 7.96 (d, 1H), 8.76 (s, 1H). Intermediate 201 Thiophene-3-carbohydrazide Methyl thiophene-3-carboxylate (800 mg, 5.63 mmol) was dissolved in ethanol (16 mL) and hydrazine hydrate (1.37 mL, 28.1 mmol) was added. It was stirred under reflux for 90 h. The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure. The residue was dissolved in ethanol and concentrated to dryness. This process was repeated to yield 795 mg (94%) of the title compound which was used without further purification in the next step. 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 4.46 (brs, 2H), 7.49 (dd, 1H), 7.58 (dd, 1H), 8.09 (dd, 1H), 9.59 (s, 1H). Intermediate 202 2-Methylthiophene-3-carbohydrazide Methyl 2-methylthiophene-3-carboxylate (350 mg, 2.24 mmol) was dissolved in 1-butanol (3.5 mL) and hydrazine hydrate (545 pL, 11.2 mmol) was added. It was stirred at 120 °C bath temperature for 20 h. The reaction mixture was allowed to cool down to rt and concentrated under reduced pressure. The residue was treated with dichloromethane and concentrated under reduced pressure to dryness affording 340 mg (97%) of the title compound which was used without further purification in the next step. LC-MS (Method 2): Rt = 0.57 min; MS (ESIpos): m / z = 157 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.62 (s, 3H), 4.80 (br s, 2H), 7.24 - 7.29 (m, 2H), 9.36 (s, 1H). Intermediate 203 5-Methylthiophene-3-carbohydrazide Methyl 5-methylthiophene-3-carboxylate (950 mg, 6.08 mmol) was dissolved in ethanol (9.5 mL) and hydrazine hydrate (1.48 mL, 30.4 mmol) was added. It was stirred under reflux for 6 h and over the weekend at rt. The reaction mixture was concentrated under reduced pressure. The residue was treated with dichloromethane and concentrated to dryness obtaining 830 mg (87%) of the title compound which was used without further purification in the next step. LC-MS (Method 2): Rt = 0.61 min; MS (ESIpos): m / z = 157 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.43 (d, 3H), 4.42 (brs, 2H), 7.17 (t, 1H), 7.82 (d, 1H), 9.49 (s, 1H). Intermediate 204 7-Chloro-2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Ui Ethyl (2-chloro-6-cyanophenyl)carbamate (500 mg, 2.23 mmol) and pyridine-4-carbohydrazide (366 mg, 2.67 mmol) were stirred in DMF (24 mL) at 120 °C for 18 h. The reaction was cooled to rt and water was added to the mixture. The suspension was filtered, washed with water and dried under reduced pressure at 60 °C. to give 582 mg (88 % yield) of the title compound. 10 LC-MS (method 2): Rt = 0.55 min; MS (ESIpos): m / z = 298 [M+H]+ The following intermediates were prepared in analogy to intermediate 204: Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 205 ch3 N JL ^n^^ch3 OCX H 2-[1-(-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.59 min; MS (ESIpos): m / z = 295 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 1.48 (d, 6H), 4.62 (sept, 1H), 7.39 (td, 1H), 7.44 (d, 1H), 7.69 (ddd, 1H), 8.03 (s, 1H), 8.16 (dd, 1H), 8.47 (s, 1H), 12.22 (brs 1H). Intermediate 206 4 / 7 ci N- / 'Cl JI N OCX H 2-(2,3-dichlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.71 min; MS (ESIpos): m / z = 331 [M+H]+ Intermediate 207 F _ JI N OCX H 2-(2,5-difluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.65 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.39 - 7.56 (m, 4H), 7.73 (ddd, 1H), 7.94 - 7.96 (m, 1H), 8.23 (dd, 1H), 12.42 (br s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 208 / / N CH3 Oil H 2-(2-ethoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.66 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 1.35 (t, 3H), 4.17 (q, 2H), 7.10 (td, 1H), 7.21 (dd, 1H), 7.37 - 7.53 (m, 3H), 7.71 (ddd, 1H), 7.91 (dd, 1H), 8.20 (dd, 1H), 12.30 (brs, 1H). Intermediate 209 ch3 0¼ \=N BA Oli H 2-(5-methyl-1,3,4-oxadiazol-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.46 min; MS (ESIpos): m / z = 269 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.68 (s, 3H), 7.41 - 7.52 (m, 2H), 7.76 (ddd, 1H), 8.25 (dd, 1H), 12.54 (br s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 210 Br N- / 'Cl JL N OCX H 2-(4-bromo-2-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.75 min; MS (ESIpos): m / z = 375 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.39-7.44 (m, 1H), 7.46 (d, 1H), 7.73 (ddd, 1H), 7.77 (dd, 1H), 7.98 (d, 1H), 8.02 (d, 1H), 8.21 (dd, 1H), 12.43 (brs, 1H). Intermediate 211 F tv fl i. H 2-(2,4-difluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.65 min; MS (ESIpos): m / z = 299 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.28 - 7.35 (m, 1H), 7.38 - 7.44 (m, 1H), 7.45 (d, 1H), 7.50 (ddd, 1H), 7.72 (ddd, 1H), 8.21 (dd, 1H), 8.27 (td, 1H), 12.38(brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 212 h3c s Ot 1 H 2-[4-(methylsulfanyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.71 min; MS (ESIpos): m / z = 309 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.56 (s, 3H), 7.38 - 7.47 (m, 4H), 7.71 (ddd, 1H), 8.13 - 8.18 (m,2H), 8.23 (dd, 1H), 12.33 (brs, 1H). Intermediate 213 F Ol 1 F—|— F H F 2-(4-fluorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin- 5(6H)-one LC-MS (Method 2): Rt = 0.74 min; MS (ESIpos): m / z = 349 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 214 2-(3-fluorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin- 5(6H)-one LC-MS (Method 2): Rt = 0.75 min; MS (ESIpos): m / z = 349 [M+H]+ Intermediate 215 2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.59 min; MS (ESIpos): m / z = 335 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 216 h3c o orx o. H ch3 7-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)- one LC-MS (Method 2): Rt = 0.71 min; MS (ESIpos): m / z = 323 [M+H]+ Intermediate 217 h3c 0 Ori 1 H 7-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin- 5(6H)-one LC-MS (Method 2): Rt = 0.84 min; MS (ESIpos): m / z = 333 [M+H]+ Intermediate Structure Intermediate 218 Intermediate 219 Intermediate 220 lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR 3 N H 7-cyclopropyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5- c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.63 min; MS (ESIpos): m / z = 307 [M+H]+ 7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.69 min; MS (ESIpos): m / z = 371 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.11 - 7.16 (m, 2H), 7.35 (t, 1H), 8.01 (dd, 1H), 8.14-8.20 (m, 2H), 8.26 (dd, 1H), 11.39 (s, 1H). 7-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.72 min; MS (ESIneg): m / z = 357 [M-Hf Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 221 F OCX Br H 7-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.71 min; MS (ESIpos): m / z = 359 [M+H]+ Intermediate 222 N. CHo / / N 3 _ FC ocx Br H 7-bromo-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin- 5(6H)-one LC-MS (Method 2): Rt = 0.47 min; MS (ESIpos): m / z = 345 [M+H]+ Intermediate 223 7-\ F N- / 0-k F N F OCX Br H 7-bromo-2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.72 min; MS (ESIneg): m / z = 423 [M-Hp Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 224 / =N Ol 1 1 H Br 7-bromo-2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.56 min; MS (ESIpos): m / z = 342 [M+H]+ Intermediate 225 h3c 0 Br "Oil Br H 7,9-dibromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.78 min; MS (ESIneg): m / z = 449 [M-H]-1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.84 - 3.87 (m, 3H), 7.10 - 7.19 (m, 2H), 8.14-8.21 (m, 2H), 8.24 (d, 1H), 8.33 (d, 1H), 11.58 (br s, 1H). Intermediate 226 Z f 1 Br H 7,9-dibromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.80 min; MS (ESIneg): m / z = 437 [M-Hf Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 227 F 'OlI Br H 7,9-dibromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.81 min; MS (ESIpos): m / z = 436 [M+H]+ Intermediate 228 l\L CH, & Nx 3 XjOL Br H 7,9-dibromo-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.58 min; MS (ESIpos): m / z = 422 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 - 3.93 (m, 3H), 7.94 - 8.00 (m, 2H), 9.84 (s, 1H), 10.15 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 229 8-methoxy-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.52 min; MS (ESIpos): m / z = 297 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 3.93 (s, 3H), 6.90 (d, 1H), 7.00 (dd, 1H), 7.99 (d, 1H), 8.07 (d, 1H), 8.39 (s, 1H). Intermediate 230 8-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.71 min; MS (ESIpos): m / z = 323 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]=3.87 (s, 3 H), 3.84 (s, 3 H), 6.91 (d, 1H), 7.01 (dd, 1H), 7.08 - 7.14 (m,2H), 8.10 - 8.17 (m, 3H), 12.18 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 231 h3c 0 o JL ,N h3cx FT N JLJL JL ch3 h 8,9-dimethoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.63 min; MS (ESIpos): m / z = 353 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 3.89 (s, 3H), 3.92 (s, 3H), 6.96 (s, 1H), 7.08 - 7.15 (m, 2H), 7.55 (s, 1H), 8.13 - 8.19 (m, 2H), 12.11 (brs, 1H). Intermediate 232 / An'CH = O zN h3cx n JL JL JL ch3 h 8,9-dimethoxy-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.48 min; MS (ESIpos): m / z = 327 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.93 (s, 3 H), 3.90 (s, 3 H), 3.87 (s, 3 H)6.95 (s, 1H), 7.48 (s, 1H), 8.00 (d, 1H), 8.40 (s, 1H), 12.07 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 233 h3c 0 f jOC1 F F H 2-(4-methoxyphenyl)-8-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.74 min; MS (ESIpos): m / z = 361 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.10-7.17 (m, 2H), 7.69-7.77 (m, 2H), 8.16 - 8.19 (m, 2H), 8.43 (d, 1H), 12.54 (s, 1H). Intermediate 234 N 3 F XjL F F H 2-(1-methyl-1H-pyrazol-4-yl)-8-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.58 min; MS (ESIpos): m / z = 335 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 235 h3c 0 jOl JL HoC^^^N^O H 2-(4-methoxyphenyl)-8-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.74 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.45 (s, 3H), 3.85 (s, 3H), 7.09 -7.14 (m, 2H), 7.21 - 7.26 (m, 2H), 8.10 (d, 1H), 8.13 - 8.17 (m, 2H), 12.23 (s, 1H). Intermediate 236 h3c 0 H 8-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.69 min; MS (ESIpos): m / z = 371 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.10 - 7.14 (m, 2H), 7.55 - 7.60 (m, 2H), 8.12 - 8.17 (m, 3H), 12.37 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 237 Nx CH, N 3 XjCjL H 8-bromo-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.54 min; MS (ESIpos): m / z = 345 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.93 (s, 3H), 7.56 (dd, 1H), 7.58 (d, 1H), 8.01 (s, 1H), 8.08 (d, 1H), 8.41 (s, 1H), 12.33 (br s, 1H). Intermediate 238 h3c o F Xi 1 H 9-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.66 min; MS (ESIneg): m / z = 309 [M-H]-1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.07 - 7.17 (m, 2H), 7.47 (dd, 1H), 7.61 (td, 1H), 7.95 (dd, 1H), 8.12 - 8.21 (m, 2H), 12.35 (brs, 1H). Intermediate 239 I\L .CH3 / / Nx 3 - .-.J / Xi 1 H 9-fluoro-2-(1-methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin- 5(6H)-one Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR LC-MS (Method 5): Rt = 1.19 min; MS (ESIneg): m / z = 283 [M-Hf Intermediate 240 F - rC XiJL H 9-fluoro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.67 min; MS (ESIneg): m / z = 297 [M-Hf 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.38 - 7.45 (m, 2H), 7.48 (dd, 1H), 7.62 (td, 1H), 7.96 (dd, 1H), 8.21 - 8.31 (m, 2H), 12.41 (brs, 1H). Intermediate 241 N— / F F JI N XXX H 9-fluoro-2-(2-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.64 min; MS (ESIneg): m / z = 297 [M-Hf Intermediate 242 h3c o XXX H 9-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.72 min; MS (ESIpos): m / z = 327 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 7.10-7.15 (m, 2H), 7.45 (d, 1H), 7.75 (dd, 1H), 8.13-8.17 (m, 3H), 12.42 (brs, 1H). Intermediate 243 I\L CH, / / N 3 'n Xl 1 H 9-chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.54 min; MS (ESIpos): m / z = 301 [M+H]+ Intermediate 244 h3c 0 o ,N H3C" N L JL I H 9-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.66 min; MS (ESIneg): m / z = 321 [M-H]-1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.85 (s, 3H), 3.90 (s, 3H), 7.12 (d, 2H), 7.30-7.36 (m, 1H), 7.37-7.41 (m, 1H), 7.62 (d, 1H), 8.12-8.21 (m, 2H), 12.19 (s, 1H). Intermediate 245 hL ,CH, / / N 3 O zN h3cx FT N L JL jL H Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR 9-methoxy-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.51 min; MS (ESIneg): m / z = 295 [M-H]-1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.88 (s, 3H), 3.94 (s, 3H), 7.30 -7.36 (m, 1H), 7.36 - 7.40 (m, 1H), 7.55 (d, 1H), 8.02 (s, 1H), 8.43 (s, 1H), 12.15 (brs, 1H). Intermediate 246 F o JL ZN h3cx n L £ £ H 2-(4-fluorophenyl)-9-methoxy[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.68 min; MS (ESIneg): m / z = 309 [M-Hf 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.90 (s, 3H), 7.31 - 7.47 (m, 4H), 7.61 (d, 1H), 8.22 - 8.31 (m, 2H), 12.24 (s, 1H). Intermediate 247 u-P: o JL ZN H3CX N L £ £ H 2-(2-fluorophenyl)-9-methoxy[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.63 min; MS (ESIpos): m / z = 311 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.90 (s, 3H), 7.32 - 7.48 (m, 4H), 7.57-7.67 (m, 2H), 8.23 (td, 1H), 12.27 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 248 h3c 0 XjU1 H 2-(4-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.74 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.44 (s, 3H), 3.85 (s, 3H), 7.10 -7.15 (m, 2H), 7.34 (d, 1H), 7.53 (dd, 1H), 8.02 (d, 1H), 8.13-8.18 (m, 2H), 12.22 (brs, 1H). Intermediate 249 h3c 0 1 H 9-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.73 min; MS (ESIneg): m / z = 369 [M-H]-1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.85 (s, 3H), 7.09 - 7.17 (m, 2H), 7.39 (d, 1H), 7.87 (dd, 1H), 8.12 - 8.19 (m, 2H), 8.29 (d, 1H), 12.42 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 250 h3c 0 ch3 n— / 1 11 N Lil H 2-(4-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.89 min; MS (ESIpos): m / z = 307 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.96 (s, 3H), 3.85 (s, 3H), 7.10 -7.15 (m, 2H), 7.24 (d, 1H), 7.29 (d, 1H), 7.53 - 7.60 (m, 1H), 8.14 - 8.19 (m, 2H), 12.24 (brs, 1H). Intermediate 251 N. CH3 N 3 F N— / 1 JI N LI 1 H 10-fluoro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.46 min; MS (ESIpos): m / z = 285 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.94 (s, 3H), 7.19 - 7.28 (m, 2H), 7.69 (td, 1H), 8.00 (d, 1H), 8.43 (s, 1H), 12.43 (br s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 252 h3c 0 h3c / 3 O N— / 1 JI N Ci X H 10-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.60 min; MS (ESIpos): m / z = 323 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 3.85 (s, 3H), 4.02 (s, 3H), 6.97 -7.03 (m, 2H), 7.10 - 7.15 (m, 2H), 7.62 (t, 1H), 8.13 - 8.18 (m, 2H), 12.24 (br s, 1H). Intermediate 253 2-(4-Methoxyphenyl)-5-oxo-5,6-dihydro[1,2,4]tri azol o[ 1,5-c]quinazoline-10-carbonitrile h3c 0 10 10-Bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (50 mg, 0.14 mmol), bis[cinnamyl palladium(ll) chloride] (3.5 mg, 0.007 mmol), 1,1'-ferrocenediyl-bis(diphenylphosphine) (3.7 mg, 0.007 mmol) and zinc cyanide (15.8 mg, 0.14 mmol) were added to a 5 ml reaction vessel and the vessel sealed and flushed with argon. Degassed N,N-dimethylacetamid (1 ml) and N,N-diisopropylethylamin (47 pl 0.27 mmol), were added and the mixture heated overnight at 80°C. The mixture was cooled to RT, the precipitate filtered and washed with water. The solid material was dissolved in DCM and flushed though a 2 g silica column, and the column washed with a DCM:MeOH mixture (9:1), the eluent was collected and the solvent removed under reduced pressure yielding the title compound (43.9 mg, 0.12 mmol, 87%). LC-MS (method 1): Rt = 1.00 min; MS (ESIpos): m / z = 318.3 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 3.85 (s, 3 H) 7.13 - 7.20 (m, 2 H) 7.70 (d, 1 H) 7.76 - 8.02 (m, 2 H) 8.15-8.21 (m, 2 H) Intermediate 254 2-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile 10-Bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (177 mg, 0.51 mmol), bis[cinnamyl palladium(ll) chloride] (13.2 mg, 0.026 mmol), 1,1'-ferrocenediyl-bis(diphenylphosphine) (14.2 mg, 0.026 mmol) and zinc cyanide (60.2 mg, 0.51 mmol) were added to a 5 ml reaction vessel and the vessel sealed and flushed with argon. Degassed N,N-dimethylacetamid (2 ml) and N,N-diisopropylethylamin (179 pl, 1.03 mmol), were added and the mixture heated overnight at 80°C. The mixture was cooled to RT, the mixture was diluted with DCM, washed with NaHCOs (saturated aqueous solution), and the aquous phase extracted twice with DCM. The combined organic phases were dried passed through a water repellent filter, and purified by RP-HPLC (column: X-Brigde C18 5p 100x30mm; acetonitrile / water + 0.1% formic acid) yielding the title compound (32 mg, 0.10 mmol, 19%). LC-MS (method 1): Rt = 1.00 min; MS (ESIpos): m / z = 292.2 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 3.96 (s, 3 H) 7.70 (dd, 1 H) 7.81 (t, 1 H) 7.88 (d, 1 H) 7.99 (d, 1 H) 8.38 (s, 1 H) 12.47 - 12.70 (m, 1 H) Intermediate 255 2-(4-Fluorophenyl)-5-oxo-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile 10-Bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (157 mg, 0.43 mmol), bis[cinnamyl palladium(ll) chloride] (11.3 mg, 0.022 mmol), 1,1'-ferrocenediyl-bis(diphenylphosphine) (12.1 mg, 0.022 mmol) and zinc cyanide (51.3 mg, 0.44 mmol) were added to a 5 ml reaction vessel and the vessel sealed and flushed with argon. Degassed N,N-dimethylacetamid (2 ml) and N,N-diisopropylethylamin (152 pl, 0.87 mmol), were added and the mixture heated overnight at 80°C. The mixture was cooled to RT, the mixture was diluted with DCM, washed with NaHCOs (saturated aqueous solution), and the aquous phase extracted twice with DCM. The combined organic phases were dried passed through a water repellent filter, and purified by RP-HPLC (column: X-Brigde C18 5p 100x30mm; acetonitrile / water + 0.1% formic acid), yielding the title compound (53 mg, 0.16 mmol, 36%). LC-MS (method 1): Rt = 1.02 min; MS (ESIpos): m / z = 306.1 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 7.39 - 7.50 (m, 2 H) 7.73 (d, 1 H) 7.81 - 7.94 (m, 2 H) 8.28 (dd, 2 H) 12.54- 12.79 (m, 1 H) Intermediate 256 2-(3-Fluorophenyl)-5-oxo-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile 10-Bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (152 mg, 0.43 mmol), bis[cinnamyl palladium(ll) chloride] (11.0 mg, 0.021 mmol), 1,1'-ferrocenediyl-bis(diphenylphosphine) (11.7 mg, 0.021 mmol) and zinc cyanide (50.0 mg, 0.43 mmol) were added to a 5 ml reaction vessel and the vessel sealed and flushed with argon. Degassed N,N-dimethylacetamid (2 ml) and N,N-diisopropylethylamin (147 pl, 0.74 mmol), were added and the mixture heated overnight at 80°C. The mixture was cooled to RT, the mixture was diluted with DCM, washed with NaHCOs (saturated aqueous solution), and the aquous phase extracted twice with DCM. The combined organic phases were dried passed through a water repellent filter, and purified by RP-HPLC (column: X-Brigde C18 5p 100x30mm; acetonitrile / water + 0.1% formic acid), yielding the title compound (77 mg, 0.21 mmol, 50%). LC-MS (method 1): Rt = 1.02 min; MS (ESIpos): m / z = 306.1 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 5 ppm 7.40 - 7.48 (m, 1 H) 7.65 - 7.76 (m, 2 H) 7.83 - 7.95 (m, 3 H) 8.09 (dt, J=7.98, 1.08 Hz, 1 H) 12.72 (br s, 1 H) Intermediate 257 2-[2-(T rifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one Methyl (2-cyanophenyl)carbamate (800 mg, 4.54 mmol) and 2-(trifluoromethoxy)benzohydrazide (1.00 g, 4.54 mmol) were dissolved in DMF (16 mL). It was stirred at 120 °C for 72 h and at 130 °C for 96 h. The reaction mixture was allowed to cool down to rt, water was added (20 mL) and it was stirred for 15 minutes. The precipitate was filtered off, washed twice with water and dried under vacuum at 50 °C to afford 1.05 g (67%) of the title compound which was used without further purification in the next step. LC-MS (Method 1): Rt = 1.15 min; MS (ESIpos): m / z = 347 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.40 - 7.48 (m, 2H), 7.58 - 7.65 (m, 2H), 7.68 - 7.75 (m, 2H), 8.20 (dd, 1H), 8.28 (dd, 1H), 12.41 (br s, 1H). The following intermediates were prepared analogously to intermediate 256: Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 258 F F / =\ # 0 OCX H 2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.83 min; MS (ESIpos): m / z = 347 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.40 - 7.50 (m, 2H), 7.56 - 7.60 (m, 1H), 7.71 - 7.77 (m, 2H), 8.08-8.11 (m, 1H), 8.23-8.28 (m, 2H), 12.40 (s, 1H). Intermediate 259 F F-X F O OCX H 2-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 1): Rt = 1.23 min; MS (ESIpos): m / z = 347 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.40 - 7.45 (m, 1H), 7.46 (d, 1H), 7.55 - 7.61 (m, 2H), 7.73 (ddd, 1H), 8.24 (dd, 1H), 8.33 - 8.37 (m, 2H), 12.38 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 260 F F F-V Ch-f v—7 F fix H 2-[3,5-bis(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 1): Rt = 0.92 min; MS (ESIneg): m / z = 397 [m-H]- 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.40 - 7.45 (m, 1H), 7.47 (d, 1H), 7.74 (ddd, 1H), 8.29 (dd, 1H), 8.37 (s, 1H), 8.72 (s, 2H), 12.45 (br s, 1H). Intermediate 261 N=x F V—J F H 2-[5-(trifluoromethyl)pyridin-3-yl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.69 min; MS (ESIpos): m / z = 332 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.42 - 7.46 (m, 1H), 7.48 (d, 1H), 7.75 (ddd, 1H), 8.28 (dd, 1H), 8.76-8.79 (m, 1H), 9.19 (d, 1H), 9.64 (d, 1H), 12.48 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 262 0. PH3 __ / 'O Oi 1 H 2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.58 min; MS (ESIpos): m / z = 341 [m+H]+ 'H-NMR (400MHz, DMSO-de): 6 [ppm]= 3.31 (s, 3H), 7.41 - 7.50 (m, 2H), 7.71 - 7.77 (m, 1H), 8.14 (d, 2H), 8.26 (d, 1H), 8.48 (d, 2H), 12.42 (s, 1H). Intermediate 263 ,____, O / —\ ii <\ / )— S-CH, W / / II d / -- ° H 2-[3-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.85 min; MS (ESIpos): m / z = 341 [m+H]+ 'H-NMR (400MHz, DMSO-de): 6 [ppm]= 3.33 (s, 3H), 7.41 - 7.45 (m, 1H), 7.47 (d, 1H), 7.74 (ddd, 1H), 7.89 (t, 1H), 8.12 (ddd, 1H), 8.28 (dd, 1H), 8.56 (dt, 1H), 8.71 (t, 1H), 12.42 (br s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 264 Z \—=N OCX H 3-(5-oxo-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile LC-MS (Method 1): Rt = 0.97 min; MS (ESIpos): m / z = 288 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.40 - 7.49 (m, 2H), 7.73 (ddd, 1H), 7.81 (td, 1H), 8.03 (dt, 1H), 8.24 (dd, 1H), 8.50 - 8.55 (m, 2H), 12.40 (br s, 1H). Intermediate 265 Ol 1 H 4-(5-oxo-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile LC-MS (Method 1): Rt = 0.97 min; MS (ESIpos): m / z = 288 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.40 - 7.48 (m, 2H), 7.71 - 7.76 (m, 1H), 8.01 - 8.09 (m, 2H), 8.24 (dd, 1H), 8.35-8.42 (m, 2H), 12.42 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 266 Cl . JI N F (XX H 2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 1): Rt = 1.31 min; MS (ESIpos): m / z = 381 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.40 - 7.48 (m, 2H), 7.70 - 7.78 (m, 3H), 8.19 (dd, 1H), 8.33 (d, 1H), 12.43 (br s, 1H). Intermediate 267 Cl / \ F N— / 0- / . JI N F F Oxi H 2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.84 min; MS (ESIpos): m / z = 381 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.41 - 7.48 (m, 2H), 7.66 (dd, 1H), 7.73 (ddd, 1H), 7.78 (dd, 1H), 8.22 (dd, 1H), 8.28 (d, 1H), 12.46 (br s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate / =N 268 !A ’ fl 1 H 2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.53 min; MS (ESIneg): m / z = 280 [m-H]-1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.41 - 7.45 (m, 1H), 7.47 (d, 1H), 7.74 (ddd, 1H), 8.20 (dd, 1H), 8.23 (dd, 1H), 8.65 (d, 1H), 8.83 (d, 1H), 12.47 (brs, 1H). Intermediate <O—(-f 269 N F fr? H 2-[6-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.66 min; MS (ESIpos): m / z = 332 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.42 - 7.46 (m, 1H), 7.48 (d, 1H), 7.75 (ddd, 1H), 8.09 (dd, 1H), 8.29 (dd, 1H), 8.34 (t, 1H), 8.58 (d, 1H), 12.45 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate h3c yj 270 OCX H 2-(4-methoxythiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.62 min; MS (ESIpos): m / z = 299 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.88 (s, 3H), 6.81 (d, 1H), 7.40 (t, 1H), 7.44 (d, 1H), 7.68-7.73 (m, 1H), 8.16-8.21 (m, 2H), 12.29 (br s, 1H). Intermediate z^s 271 OCX H 2-(thiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.60 min; MS (ESIpos): m / z = 269 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 7.39 - 7.43 (m, 1H), 7.45 (d, 1H), 7.69-7.77 (m, 3H), 8.21 (dd, 1H), 8.32 (dd, 1H), 12.31 (brs, 1H). Intermediate Z^S 272 K. / ch3 N—K 5 ___ N OiX H 2-(2-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.71 min; MS (ESIpos): m / z = 283 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.89 (s, 3H), 7.38 - 7.47 (m, 3H), 7.63 (d, 1H), 7.71 (ddd, 1H), 8.21 (dd, 1H), 12.33 (brs, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 273 ch3 Z^S Oi 1 H 2-(5-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one LC-MS (Method 2): Rt = 0.69 min; MS (ESIpos): m / z = 283 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 5 [ppm]= 2.54 (d, 3H), 7.38 - 7.47 (m, 3H), 7.71 (ddd, 1H), 8.05 (d, 1H), 8.19 (dd, 1H), 12.30 (brs, 1H). Intermediate 274 2-(lmidazo[1,2-a]pyridin-7-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one 5 Methyl (2-cyanophenyl)carbamate (700 mg, 3.97 mmol) and imidazo[1,2-a]pyridine-7-carbohydrazide (700 mg, 3.97 mmol) were susspended in DMF (20 mL). It was stirred at 120 °C for 24 h. lmidazo[1,2-a]pyridine-7-carbohydrazide (100 mg, 0.57 mmol) was added and it was stirred at 120 °C for 24 h. The reaction mixture was allowed to cool down to rt and poured into water (100 mL). The precipitate was filtered off, washed four times with water and dried under 10 vacuum at 50 °C to yield 1.02 g of a crude product. 100 mg of the crude product in DMF (2.5 mL) was stirred at 120 °C over the weekend. The reaction mixture was allowed to cool down to rt and poured into water. The precipitate was filtered off, washed three times with water and dried at 50 °C under vacuum affording 88 mg of a crude product. All two crude products were combined and stirred in DMF (20 mL) at 130 °C for 120 h. The reaction mixture was allowed to reach rt and poured into water. The precipitate was filtered off, washed three times with water, dried at 50 °C under vacuum affording 919 mg ot the title compound which was used without further purification in the next step. LC-MS (Method 2): Rt = .56 min; MS (ESIpos): m / z = 303 [m+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.42 - 7.49 (m, 2H), 7.66 (dd, 1H), 7.70 - 7.77 (m, 2H), 8.11 (s, 1H), 8.27 (dd, 1H), 8.34 (s, 1H), 8.72 (d, 1H), 12.39 (br s, 1H). Intermediate 275 Methyl 2-(4-methoxyphenyl)-5-oxo-5,6-dihydro[1,2,4]triazolo[1,5-c]quinazoline-10-carboxylate H 10-Bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (396 mg, 1.07 mmol) was suspended in methanol / THF (13.2 mL, 10:1) in an autoclave (50 mL). Triethylamine (300 pL, 2.1 mmol) and 1,T-bis(diphenylphosphino)ferrocene-palladium(ll)dichloride dichloromethane complex (90 mg, 110 pmol) were added. The reaction mixture was purged three times with carbon monoxide at rt. Then, the autoclave was filled with carbon monoxide up to 12.7 bar and it was stirred for 30 min at rt. As the pressure was constant at 12.6 bar the carbon monoxide was released and the autocalve was evacuated under vacuum. The autoclave was filled with carbon monoxide up to 14.2 bar at 20 °C internal temperature. The reaction mixture was stirred for 24 h at 100 °C internal temperature. The reaction mixture was allowed to cool down to rt and the carbon monoxide was removed. The reaction mixture was concentrated and digested in ethyl acetate / dichloromethane. The insoluble residue was filtered off, washed with ethyl acetate and a few drops of dichloromethane, and the filtrate was concentrated under reduce pressure to yield 326 mg (87%) of the title product. LC-MS (Method 2): Rt = 0.67 min; MS (ESIpos): m / z = 351 [M+H]+ 1H-NMR (400 MHz, DMSO-d6) 5 [ppm]= 3.85 (s, 3H), 4.01 (s, 3H), 7.11 - 7.17 (m, 2H), 7.43 (dd, 1H), 7.54 (dd, 1H), 7.76 (dd, 1H), 8.08 - 8.14 (m, 2H). Intermediate 276 5,7-Dichloro-2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazoline Cl 7-Chloro-2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (482 mg, 1.62 mmol) was 5 stirred in POCI3 (5.0 mL, 54 mmol) and N,N-diisopropylethylamine (2.8 mL, 16 mmol) overnight at 110 °C. The mixture was poured into ice, and the solid was filtered, washed with water and dried under reduced pressure at 60 °C to give the title compound 530 mg (39 % purity, 40 % yield) that was used without further purification. LC-MS (method 2): Rt = 1.19 min; MS (ESIpos): m / z = 316 [M+H]+ 10 The following intermediates were prepared analogously to intermediate 275: Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 277 ch3 N JL / / xhr^CH3 Ori 5-chloro-2-[1 -(propan-2-yl)-1 H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.15 min; MS (ESIpos): m / z = 313 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 1.50 (d, 6H), 4.64 (spt, 1H), 7.84 (ddd, 1H), 7.93-7.99 (m, 1H), 8.00-8.04 (m, 1H), 8.11 (s, 1H), 8.45 (dd, 1H), 8.57 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 278 Z ci N- / 'Cl JL N OCX 5-chloro-2-(2,3-dichlorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.48 min; MS (ESIpos): m / z = 349 [M+H]+ Intermediate 279 F ^^^N^CI 5-chloro-2-(2,5-difluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.36 min; MS (ESIpos): m / z = 317 [M+H]+ Intermediate 280 / / N CH3 ^^^N^CI 5-chloro-2-(2-ethoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.35 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 1.41 (t, 3H), 4.20 (q, 2H), 7.14 (td, 1H), 7.25 (d, 1H), 7.53 (ddd, 1H), 7.86 (ddd, 1H), 7.97 (td, 1H), 8.02 - 8.09 (m, 2H), 8.50 (dd, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 281 5-chloro-2-(5-methyl-1,3,4-oxadiazol-2-yl)[1,2,4]triazolo[1,5- c]quinazoline LC-MS (Method 2): Rt = 0.94 min; MS (ESIpos): m / z = 287 [M+H]+ Intermediate 282 Br 2-(4-bromo-2-chlorophenyl)-5-chloro[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.56 min; MS (ESIpos): m / z = 331 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.81 (dd, 1H), 7.88 (ddd, 1H), 7.998.03 (m, 2H), 8.05 - 8.08 (m, 1H), 8.10 (d, 1H), 8.51 (dd, 1H). Intermediate 283 5-chloro-2-(2,4-difluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.35 min; MS (ESIpos): m / z = 317 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.32 - 7.39 (m, 1H), 7.54 (ddd, 1H), 7.87 (ddd, 1H), 7.96 - 8.02 (m, 1H), 8.03 - 8.08 (m, 1H), 8.35 (td, 1H), 8.51 (dd, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 284 h3c s occ 5-chloro-2-[4-(methylsulfanyl)phenyl][1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.45 min; MS (ESIpos): m / z = 327 [M+H]+ Intermediate 285 F OCX O^^N^CI F--F F 5-chloro-2-(4-fluorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.49 min; MS (ESIpos): m / z = 367 [M+H]+ Intermediate 286 Z V- F OCX ^Y^n^ci F--F F 5-chloro-2-(3-fluorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.50 min; MS (ESIpos): m / z = 367 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 287 l\L CH, / / N 3 OCX ^Y^n^ci F--F F 5-chloro-2-(1-methyl-1H-pyrazol-4-yl)-7- (trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.15 min; MS (ESIpos): m / z = 353 [M+H]+ Intermediate 288 h3c 0 OCX ch3 5-chloro-7-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.27 min; MS (ESIpos): m / z = 341 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.86 (s, 3H), 4.02 (s, 3H), 7.09 -7.21 (m, 2H), 7.51 (dd, 1H), 7.78 (t, 1H), 8.02 (dd, 1H), 8.15-8.25 (m, 2H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 289 h3c 0 OTX ^V^N^CI 5-chloro-7-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.56 min; MS (ESIpos): m / z = 351 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 0.87-0.93 (m, 2H), 1.15- 1.21 (m, 2H), 2.98 (tt, 1H), 3.86 (s, 3H), 7.12 - 7.17 (m, 2H), 7.40 (dd, 1H), 7.72 (t, 1H), 8.20 - 8.25 (m, 2H), 8.27 (dd, 1H). Intermediate 290 I\L .CH, & N 3 OCX 5-chloro-7-cyclopropyl-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.22 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 0.87-0.92 (m, 2H), 1.15- 1.21 (m, 2H), 2.98 (tt, 1H), 3.96 (s, 3H), 7.39 (dd, 1H), 7.71 (t, 1H), 8.09 (d, 1H), 8.21 (dd, 1H), 8.53 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 291 h3c 0 CO. Br 7-bromo-5-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.46 min; MS (ESIpos): m / z = 391 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.13-7.19 (m, 2H), 7.74 (t, 1H), 8.21 - 8.27 (m, 2H), 8.30 (dd, 1H), 8.52 (dd, 1H). Intermediate 292 Z F 03 col Br 7-bromo-5-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.50 min; MS (ESIpos): m / z = 377 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.41 - 7.49 (m, 2H), 7.76 (t, 1H), 8.29 - 8.39 (m, 3H), 8.53 (dd, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 293 F Ooi Br 7-bromo-5-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.49 min; MS (ESIpos): m / z = 377 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.43-7.50 (m, 1H), 7.68 (td, 1H), 7.77 (t, 1H), 8.00 (ddd, 1H), 8.15 (dt, 1H), 8.32 (dd, 1H), 8.54 (dd, 1H). Intermediate 294 N. CHo / / N 3 OOL ^Y^n^ci Br 7-bromo-5-chloro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.11 min; MS (ESIpos): m / z = 363 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 295 / “A F N—Z O-Lf JI N F OCT Br 7-bromo-5-chloro-2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.54 min; MS (ESIpos): m / z = 443 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.62 - 7.71 (m, 2H), 7.72 - 7.81 (m, 2H), 8.33 (dd, 1H), 8.41 (dd, 1H), 8.51 (dd, 1H). Intermediate / =N 296 Oil Br 7-bromo-5-chloro-2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.22 min; MS (ESIpos): m / z = 360 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 297 h3c 0 YjO' Br 7,9-dibromo-5-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2.): Rt = 1.63 min; MS (ESIpos): m / z = 467 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.13 - 7.21 (m, 2H), 8.21 - 8.27 (m, 2H), 8.54 (d, 1H), 8.60 - 8.66 (m, 1H). Intermediate 298 YjmL Br 7,9-dibromo-5-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline Intermediate 299 F Br 7,9-dibromo-5-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.42 - 7.52 (m, 2H), 8.32 - 8.40 (m, 2H), 8.56 (d, 1H), 8.65 (d, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 300 l\L CH, / / Nx 3 XaX Br 7,9-dibromo-5-chloro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline Intermediate 301 N. CH, / / N 3 jOCX O^^^N^CI ch3 5-chloro-8-methoxy-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5- c]quinazoline LC-MS (Method 2): Rt = 1.00 min; MS (ESIpos): m / z = 315 [M+H]+ 1H NMR (400 MHz, DMSO-d6) 6 ppm 3.96 (s, 3 H), 3.95 (s, 3 H)7.43 (dd, 1H), 7.49 (d, 1H), 8.04-8.09 (m, 1H), 8.33 (d, 1H), 8.51 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 302 h3c 0 O^^^N^CI ch3 5-chloro-8-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.37 min; MS (ESIpos): m / z = 341 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.86 (s, 3H), 3.97 (s, 3H), 7.12 -7.17 (m, 2H), 7.45 (dd, 1H), 7.51 (d, 1H), 8.19 - 8.24 (m, 2H), 8.39 (d, 1H). Intermediate 303 h3c 0 rK o JL ZN H3CX L JI J ch3 5-chloro-8,9-dimethoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.30 min; MS (ESIpos): m / z = 371 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.86 (s, 3H), 3.98 (s, 3H), 4.04 (s, 3H), 7.11 - 7.18 (m, 2H), 7.53 (s, 1H), 7.76 (s, 1H), 8.20 - 8.26 (m, 2H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 304 0 zN H3Cx N JL 1 J O^^^N^CI ch3 5-chloro-8,9-dimethoxy-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 0.95 min; MS (ESIpos): m / z = 345 [M+H]+ 1H NMR (400 MHz, DMSO-d6) 6 ppm 4.02 (s, 3 H), 3.97 (s, 3 H), 3.95 (s, 3 H)7.51 (s, 1H), 7.69 (s, 1H), 8.07 (d, 1H), 8.51 (s, 1H). Intermediate 305 h3c O F £|M F F 5-chloro-2-(4-methoxyphenyl)-8-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.51 min; MS (ESIpos): m / z = 379 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.15 (d, 2H), 8.14 (dd, 1H), 8.21 - 8.26 (m, 2H), 8.41 (s, 1H), 8.70 (d, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 306 Nx CH, N 3 \ jOCX F F 5-chloro-2-(1-methyl-1H-pyrazol-4-yl)-8-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.20 min; MS (ESIpos): m / z = 353 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.96 (s, 3H), 7.72 (s, 1H), 8.12 -8.15 (m, 1H), 8.41 (s, 1H), 8.57 (s, 1H), 8.65 (d, 1H). Intermediate 307 h3c 0 jXCX 5-chloro-2-(4-methoxyphenyl)-8-methyl[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.44 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.57 (s, 3H), 3.86 (s, 3H), 7.08 -7.23 (m, 2H), 7.69 (dd, 1H), 7.84 (s, 1H), 8.18-8.28 (m, 2H), 8.39 (d, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 308 h3c 0 jOTa Br^^^N^CI 8-bromo-5-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.54 min; MS (ESIpos): m / z = 389 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.14 - 7.17 (m, 2H), 8.01 (dd, 1H), 8.21 - 8.26 (m, 2H), 8.30 (d, 1H), 8.43 (d, 1H). Intermediate 309 / zVH3 XXX Br^^^N^CI 8-bromo-5-chloro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.19 min; MS (ESIpos): m / z = 363 [M+H]+ Intermediate 310 h3c 0 - XYjl 5-chloro-9-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.40 min; MS (ESIpos): m / z = 329 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.86 (s, 3H), 7.13-7.19 (m, 2H), 7.86 (td, 1H), 8.12 (dd, 1H), 8.20-8.26 (m, 3H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 311 N .CH3 / / N 3 XiX ^^^N^CI 5-chloro-9-fluoro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.02 min; MS (ESIpos): m / z = 303 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.96 (s, 3H), 7.85 (td, 1H), 8.06 -8.12 (m, 2H), 8.15 (dd, 1H), 8.52 (s, 1H). Intermediate 312 F - 5-chloro-9-fluoro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.43 min; MS (ESIpos): m / z = 317 [M+H]+ Intermediate 313 -..TV XXJl 5-chloro-9-fluoro-2-(2-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.35 min; MS (ESIpos): m / z = 317 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.42 - 7.49 (m, 2H), 7.88 (td, 1H), 8.14 (dd, 1H), 8.26 (dd, 1H), 8.30-8.37 (m, 2H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 314 h3c 0 C. XYa 5,9-dichloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.50 min; MS (ESIpos): m / z = 345 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.10 - 7.22 (m, 2H), 7.97-8.01 (m, 1H), 8.04-8.08 (m, 1H), 8.16-8.27 (m, 2H), 8.47 (d, 1H). Intermediate 315 I\L CH, N 3 YjlX 5,9-dichloro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.12 min; MS (ESIpos): m / z = 319 [M+H]+ Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 316 h3c 0 o ZN H3CX 'v Y N L £ J 5-chloro-9-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.38 min; MS (ESIpos): m / z = 341 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.86 (s, 3H), 4.01 (s, 3H), 7.12 -7.18 (m, 2H), 7.55 (dd, 1H), 7.80 (d, 1H), 7.95 (d, 1H), 8.20-8.28 (m, 2H). Intermediate 317 N CH3 N 3 O ZN h3cx n L Jl JL ^^^N^CI 5-chloro-9-methoxy-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.02 min; MS (ESIpos): m / z = 315 [M+H]+ Intermediate 318 F o JL ZN h3cx N L1 J 5-chloro-2-(4-fluorophenyl)-9-methoxy[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.42 min; MS (ESIpos): m / z = 329 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 4.02 (s, 3H), 7.41 - 7.48 (m, 2H), 7.57 (dd, 1H), 7.83 (d, 1H), 7.98 (d, 1H), 8.32 - 8.38 (m, 2H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 319 o JL N h3c' y n L £ £ 5-chloro-2-(2-fluorophenyl)-9-methoxy[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.34 min; MS (ESIpos): m / z = 329 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 4.02 (s, 3H), 7.42 - 7.51 (m, 2H), 7.57 (dd, 1H), 7.65 (dddd, 1H), 7.82 (d, 1H), 7.98 (d, 1H), 8.30 (td, 1H). Intermediate 320 h3c O XjlX 5-chloro-2-(4-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.44 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 2.59 (s, 3H), 3.86 (s, 3H), 7.13 -7.19 (m, 2H), 7.79 (dd, 1H), 7.92 (d, 1H), 8.19 - 8.25 (m, 2H), 8.29 - 8.32 (m, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 321 h3c 0 9-bromo-5-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.52 min; MS (ESIpos): m / z = 389 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.86 (s, 3H), 7.14 - 7.19 (m, 2H), 7.97 (d, 1H), 8.11 (dd, 1H), 8.21 - 8.26 (m, 2H), 8.61 (d, 1H). Intermediate 322 h3c o ch3 n— / 1 JI N 5-chloro-2-(4-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.54 min; MS (ESIpos): m / z = 325 [M+H]+ 1H-NMR (500MHz, DMSO-d6): 6 [ppm]= 3.10 (s, 3H), 3.86 (s, 3H), 7.16 (d, 2H), 7.66 - 7.70 (m, 1H), 7.81 - 7.87 (m, 2H), 8.22 - 8.27 (m, 2H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 323 utt 5-chloro-10-fluoro-2-(1 -methyl-1 H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 0.95 min; MS (ESIpos): m / z = 303 [M+H]+ Intermediate 324 h3c 0 h3c / 3 O N— / t jl n 5-chloro-10-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline LC-MS (Method 2): Rt = 1.26 min; MS (ESIpos): m / z = 341 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.86 (s, 3H), 4.11 (s, 3H), 7.14 -7.18 (m, 2H), 7.41 (d, 1H), 7.57 (dd, 1H), 7.88 (t, 1H), 8.19-8.26 (m, 2H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 325 h3c 0 n y—V I I N— / I ) / \ 5-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile LC-MS (Method 2): Rt = 1.30 min; MS (ESIpos): m / z = 336 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.87 (s, 3H), 7.17 - 7.22 (m, 2H), 8.09 (dd, 1H), 8.22 - 8.28 (m, 2H), 8.35 (dd, 1H), 8.39 (dd, 1H). Intermediate 326 N. CH, N 3 N )=^ I I N— / I j[ \ 5-chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile LC-MS (Method 2): Rt = 0.95 min; MS (ESIpos): m / z = 310 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 3.98 (s, 3H), 8.04 - 8.10 (m, 2H), 8.33 (dd, 1H), 8.37 (dd, 1H), 8.51 (s, 1H). Intermediate Structure lUPAC-Name LC-MS (method): Retention time; Mass found 1H-NMR Intermediate 327 F N V । । N— / I JI \ 5-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile LC-MS (Method 2): Rt = 1.32 min; MS (ESIpos): m / z = 324 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.46-7.53 (m, 2H), 8.11 (dd, 1H), 8.33 - 8.39 (m, 3H), 8.41 (dd, 1H). Intermediate 328 Z F n y—" I I N— / I ji \ 5-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile LC-MS (Method 2): Rt = 1.32 min; MS (ESIpos): m / z = 324 [M+H]+ 1H-NMR (400MHz, DMSO-d6): 6 [ppm]= 7.46-7.53 (m, 1H), 7.72 (td, 1H), 7.99 (ddd, 1H), 8.12 (dd, 1H), 8.16 (dt, 1H), 8.37 (dd, 1H), 8.42 (dd, 1H). Intermediate 329 5-Chloro-2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazoline 2-[2-(Trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5(6H)-one (600 mg, 1.73 mmol) was suspended in phosphoric trichloride (4.8 mL, 51.13 mmol). N,N-Diisopropylethylamine (3.0 mL, 17 mmol) was added and it was stirred at 110 °C for 4.5 h. The reaction mixture was allowed 5 to cool down to rt, poured into ice / water and stirred for 30 minutes. The precipitate was filtered, washed three times with water and dried under vacuum at 50 °C overnight yielding 585 mg (93%) of the title compound which was used without further ...
Claims
1. A compound of general formula (I):(I),in whichR1 represents phenyl or heteroaryl,optionally substituted one to three times, independently from each other, with halogen, cyano, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl-, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl-, C3-C6-cycloalkyl-O-, 4- to 6-membered heterocycloalkyl,-NR9R10, R9R10N-C1-C4-alkyl-, C1-C3-alkyl-S(O)m- or C1-C3-alkyl-SO(NH)-;R2 represents hydrogen, C1-C4-alkyl, C1-C4-haloalkyl or C3-C6-cycloalkyl;R3 represents hydrogen, C1-C6-alkyl, phenyl or phenyl-C1-C3-alkyl, whereinsaid C1-C6-alkyl group is optionally substituted, one or more times, independently from each other, with hydroxy, halogen, C1-C4-alkoxy, -S(O)n-C1-C4-alkyl, phenyl-C1-C3-alkoxy or -NR9R10 andsaid phenyl groups are optionally substituted, one or more times, independently from each other, with hydroxy, halogen, cyano, C1-C3-alkyl, C1-C3-haloalkyl, C1-C3-alkoxy or C1-C3-haloalkoxy, orR2 and R3 together with the carbon atom to which they are attached form a 3- to 6-membered ring, said ring optionally containing one heteroatom selected from O, S, NH, NRa in which Ra represents a C1-C4-alkyl group;R4 represents hydroxy, C1-C4-alkoxy or -NR11R12, orR2 and R4 together represent *-C2-C5-alkanediyl-X1-**, *-C1-C2-alkanediyl-X2-C1-C3-alkanediyl-** or *-C1-C2-alkanediyl-X2-C2-C3-alkanediyl-X1-** to form a 5- to 9-membered ring,2020328154 12 Jun 2026wherein * indicates the point of attachment of said group for R2 and ** indicates the point of attachment of said group for R4;R5 represents hydrogen, halogen, cyano, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C3-C6-cycloalkyl, 4- to 6-membered heterocycloalkyl,-CO2-C1-C4-alkyl, -CO-NR9R10 or -NR9R10;R6 represents hydrogen, halogen, cyano, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C3-C6-cycloalkyl or -NR9R10;R7 represents hydrogen, halogen, cyano, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C3-C6-cycloalkyl or -NR9R10;R8 represents hydrogen, halogen, cyano, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C3-C6-cycloalkyl, 1-R15-C3-C6-cycloalkyl, -CO2-C1-C4-alkyl, -CO-NR9R10, -NR9R10, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl-, C1-C4-alkyl-S-, C1-C4-alkyl-S-C1-C4-alkyl-, -S(=O)R’, -S(=O)2R’, -S(=O)2NH2, -S(=O)2NHR’,-S(=O)2N(R’)R’’, -S(=O)(=NH)R’, 4- to 6-membered heterocycloalkyl, or -OR16;R9 and R10 are the same or different and represent, independently from each other, hydrogen, C1-C3-alkyl or tert-butoxycarbonyl, or together with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRb in which Rb represents C1-C4-alkyl orC1-C4-alkoxycarbonyl;R11 and R12 are the same or different and represent, independently from each other, hydrogen, C1-C4-alkyl, C2-C4-hydroxyalkyl, C1-C4-alkoxy-C2-C4-alkyl-, R9R10N-C2-C4-alkyl-, C3-C6-cycloalkyl, 4- to 7-membered heterocycloalkyl, said 4- to 7membered heterocycloalkyl group is optionally substituted, one or two times, independently from each other, with hydroxy, oxo, halogen, C1-C4-alkyl, C1-C4-alkoxy, or -NR9R10, ortogether with the nitrogen atom to which they are attached form a 4- to 6-membered nitrogen containing heterocyclic ring, said ring optionally containing one additional heteroatom selected from O, S, NH, NRc in which Rc represents C1-C4-alkyl or2020328154 12 Jun 2026C1-C4-alkoxycarbonyl and is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, C1-C4-alkyl, C1-C4-alkoxy, or -NR9R10, ortogether with the nitrogen atom to which they are attached form a heterospirocycloalkyl group, which is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, C1-C4-alkyl, C1-C4-alkoxy, or-NR9R10, ortogether with the nitrogen atom to which they are attached form a bridged heterocycloalkyl group, which is optionally substituted, one or two times, independently from each other, with hydroxy, halogen, C1-C4-alkyl, C1-C4-alkoxy, or-NR9R10;R13 represents hydrogen, C1-C4-alkyl, benzyl, 4-methoxybenzyl or tertbutoxycarbonyl;R14 represents hydrogen, C1-C4-alkyl, benzyl or 4-methoxybenzyl;R15 represents C1-C3-alkyl or C1-C3-haloalkyl;R16 represents C2-C6-hydroxyalkyl, C1-C4-alkoxy-C2-C6-alkyl-, or C3-C6-cycloalkyl;R’ and R’’ represent, independently from each other, C1-C6-alkyl, C1-C6-haloalkyl, or C3-C6-cycloalkyl;X1 represents O, S(O)m, or NR13;X2 represents O, S(O)m, or NR14;m represents 0, 1 or 2;n represents 0, 1 or 2;or a polymorph, enantiomer, diastereomer, racemate, tautomer, N-oxide, hydrate or solvate thereof, or a physiological acceptable salt or solvate of the salt, or a mixture of the same.
2. The compound according to claim 1, wherein:R1 represents phenyl or monocyclic heteroaryl,optionally substituted one to two times, independently from each other, with halogen, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy,2020328154 12 Jun 2026C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl-, C3-C6-cycloalkyl-O-, 4- to 6membered heterocycloalkyl or -NR9R10;R2 represents hydrogen or C1-C4-alkyl;R3 represents hydrogen, C1-C4-alkyl, phenyl or phenyl-methyl, whereinsaid C1-C4-alkyl group is optionally substituted once with hydroxy, methoxy, -S(O)n-methyl, phenyl-methoxy or -NR9R10 andsaid phenyl groups are optionally substituted once with hydroxy, orR2 and R3 together with the carbon atom to which they are attached form a 3- to 6-membered ring, said ring optionally containing one oxygen atom;R4 represents hydroxy, methoxy or -NR11R12, orR2 and R4 together represent a group selected from:wherein * indicates the point of attachment of said group with the NH group informula (I);R5 represents hydrogen, halogen, C1-C4-alkyl, methoxy, trifluoromethyl orcyclopropyl;R6 represents hydrogen, halogen or methyl;R7 represents hydrogen, halogen, methyl or methoxy;R8 represents hydrogen, halogen or methyl;R9 and R10 are the same or different and represent, independently from each other, hydrogen, methyl or tert-butoxycarbonyl;R11 and R12 are the same or different and represent, independently from each other, hydrogen, C1-C3-alkyl or C3-C4-cycloalkyl, wherein said C1-C3-alkyl group is optionally substituted with hydroxy;R13 represents hydrogen or methyl;X3 represents CH2 or NH;2020328154 12 Jun 2026n represents 0 or 2;or a polymorph, enantiomer, diastereomer, racemate, tautomer, N-oxide, hydrate or solvate thereof, or a physiological acceptable salt or solvate of the salt, or a mixture of the same.
3. The compound according to claim 1 or 2 which is selected from the group consisting of: (3S)-3-[(2-phenyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]azepan-2-oneN2-(2-phenyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl)-D-serinamideN2-(2-phenyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl)-D-valinamide(2R)-2-[(2-phenyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]butanamide(3R)-3-[(2-phenyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]azepan-2-one(3R)-3-{[2-(4-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(4-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3S)-3-{[2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one3-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one3-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-oneN2-[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-serinamide(2R)-2-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one2020328154 12 Jun 2026(3S)-3-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one6-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-onetert-butyl [(5S)-6-amino-5-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-6-oxohexyl]carbamateN2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-serinamideN2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-leucinamide3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-oneN2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-L-lysinamide6-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(3R)-3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one2020328154 12 Jun 2026(3S)-3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3S)-3-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one3-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one3-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(6R)-6-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(3R)-3-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3S)-3-{[2-(2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-({2-[2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(3-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[3-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(2-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(2-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(2-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[2-(5-methyl-1H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-ethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1,5-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one (3R)-3-{[2-(2-methyl-1,3-oxazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one (3S)-3-{[2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one (3S)-3-{[2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one (3R)-3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one (3S)-3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one 3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one 3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-oneN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-serinamide3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-methylpyrrolidin-2-oneN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-L-alaninamide N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-leucinamideN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-L-valinamideN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-L-tyrosinamideN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-L-serinamide2020328154 12 Jun 2026N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]alaninamide3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}oxetane-3-carboxamide(2R)-2-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(2R)-2-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-2-phenylacetamideN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-phenylalaninamideN-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-serineN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamideN-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-leucineN-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valine(2R)-2-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanoic acidN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-methioninamideO-benzyl-N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-threoninamideN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-methylalaninamide1-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}cyclopentane-1-carboxamide1-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}cyclohexane-1-carboxamidetert-butyl [(5S)-6-amino-5-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-6-oxohexyl]carbamateN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-methyl-L-alaninamideN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valinamidemethyl N-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valinateN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-propan-2-yl-D-alaninamideN-cyclopropyl-N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamideN-ethyl-N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide2020328154 12 Jun 2026N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-methyl-D-alaninamideN-cyclobutyl-N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamideN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N,N-dimethyl-D-alaninamideN-(2-hydroxyethyl)-N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamideN-(3-hydroxypropyl)-N2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide(2R)-4-(methanesulfonyl)-2-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamid(2R)-2-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-4-(methylsulfonyl)butanamideN2-[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-L-lysinamide6-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(3R)-3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3S)-3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-methylpyrrolidin-2-one(3R)-3-{[2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-methylpyrrolidin-2-one(3R)-3-{[2-(pyridin-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(pyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(pyridazin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-({2-[4-(dimethylamino)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(3-hydroxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(furan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-methyl-1,2,4-oxadiazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-ethyl-1,2,4-oxadiazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[3-(propan-2-yl)-1,2,4-oxadiazol-5-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(3-tert-butyl-1,2,4-oxadiazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[3-(trifluoromethyl)-1,2,4-oxadiazol-5-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[7-fluoro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-fluoro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(3-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-methyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3S)-3-{[2-(4-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-methoxyphenyl)-8-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(3-methoxyphenyl)-8-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[8-methyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[8-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[8-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3S)-3-{[8-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[8-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[8-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[8-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(3-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3S)-3-{[2-(3-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(3-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[9-methyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one3-{[9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one3-{[9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[10-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-fluorophenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[2-(4-fluorophenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-cyclopropyl-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-cyclopropyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one3-{[2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one3-{[2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[10-methyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-oneN2-[10-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide(3R)-3-{[10-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3S)-3-{[9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[9-fluoro-2-(3-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one2020328154 12 Jun 2026(3R)-3-{[2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3S)-3-{[2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one6-{[2-(4-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(3R)-3-{[7-chloro-2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(2,3-dichlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2,5-difluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-ethoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(5-methyl-1,3,4-oxadiazol-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-bromo-2-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2,4-difluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[4-(methylsulfanyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(4-fluorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-cyclopropyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-({7-bromo-2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-{[7-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[7-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-({7-bromo-2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one(3R)-3-({7-bromo-2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3R)-3-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one2020328154 12 Jun 2026(3R)-3-{[7-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[7-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[7-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-8-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-8-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[8-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[8-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-fluoro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-fluoro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-fluoro-2-(2-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-methoxy-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[2-(4-fluorophenyl)-9-methoxy[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-fluorophenyl)-9-methoxy[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-fluoro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2-(4-methoxyphenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile2-(1-methyl-1H-pyrazol-4-yl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile2-(4-fluorophenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrile2-(3-fluorophenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-10-carbonitrilemethyl 2-(4-methoxyphenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carboxylate(3R)-3-{[8-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-onemethyl 2-(4-methoxyphenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-10-carboxylate(6R)-6-{[7-chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-{[2-(2-ethoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-bromo-2-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({2-[4-(methylsulfanyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[2-(1-methyl-1H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(furan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({2-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({2-[2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[2-(2,3-dichlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({7-bromo-2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-methyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[8-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)-8-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)-8-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[8-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[8-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[9-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[9-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[9-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)-9-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[10-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[10-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[10-bromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[10-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-{[2-(4-methoxyphenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1-methyl-1H-pyrazol-4-yl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-fluorophenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(3-fluorophenyl)-10-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(3-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)-10-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[10-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one6-{[10-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one6-{[10-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one6-{[10-cyclopropyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one6-{[10-cyclopropyl-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[10-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[10-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[10-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[10-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-{[10-cyclopropyl-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[10-cyclopropyl-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(3R)-3-({2-[3-(hydroxymethyl)-1,2,4-oxadiazol-5-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[3-(methoxymethyl)-1,2,4-oxadiazol-5-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-[(2-{3-[(dimethylamino)methyl]-1,2,4-oxadiazol-5-yl}[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]azepan-2-one(3R)-3-({2-[3-(2-hydroxyethyl)-1,2,4-oxadiazol-5-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R, R)-3-({2-[4-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R, S)-3-({2-[4-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one(3R)-3-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3R)-1-methyl-3-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-oneN2-{2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-serinamide(2R)-2-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3S)-3-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one2020328154 12 Jun 2026N-methyl-N2-{2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-norvalinamideN-butyl-N2-{2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}glycinamideN-ethyl-2-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2R)-N-ethyl-2-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2S)-N-ethyl-2-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamideN-propyl-N2-{2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-alaninamideN2-{2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}norleucinamideN2-{2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-norleucinamideN2-{2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-L-norleucinamideN-[2-(dimethylamino)ethyl]-N2-{2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-alaninamide(3R)-3-({2-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one(3R)-1-methyl-3-({2-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-oneN2-{2-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-serinamide(2R)-2-({2-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3S)-3-({2-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one2020328154 12 Jun 2026(3R)-3-{[2-(4-methoxythiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxythiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(4-methoxythiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3S)-3-{[2-(4-methoxythiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxythiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-methylpyrrolidin-2-one(2R)-2-{[2-(4-methoxythiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamideN2-[2-(4-methoxythiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-methyl-D-norvalinamide(3R)-3-{[2-(thiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(thiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(thiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(thiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(2R)-2-{[2-(thiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3R)-1-methyl-3-{[2-(thiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(2-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(2-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[2-(2-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-1-methyl-3-{[2-(2-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one2020328154 12 Jun 2026(2R)-2-{[2-(2-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3R)-3-{[2-(5-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(5-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(5-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-1-methyl-3-{[2-(5-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(5-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-oneN-methyl-N2-[2-(5-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-norvalinamide(2R)-2-{[2-(5-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3R)-3-({2-[3,5-bis(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[3,5-bis(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one(2R)-2-({2-[3,5-bis(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[5-(trifluoromethyl)pyridin-3-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[4-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3R)-3-({2-[4-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one2020328154 12 Jun 2026(2R)-2-({2-[4-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamideN-methyl-N2-{2-[4-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-norvalinamide(3R)-3-{[2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one (3R)-3-({2-[6-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-({2-[6-(trifluoromethyl)pyridin-2-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one(3R)-3-({2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3S)-3-({2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-({2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamideN2-{2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-methyl-D-norvalinamide(2R)-2-({2-[3-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2R)-2-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide 3-(5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile (2R)-2-{[2-(3-cyanophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide 3-(5-{[(3R)-2-oxopyrrolidin-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile 3-(5-{[(3R)-2-oxopiperidin-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile 3-(5-{[(3S)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile (2R)-2-{[2-(4-cyanophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide2020328154 12 Jun 20264-(5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile4-(5-{[(3R)-2-oxopyrrolidin-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile4-(5-{[(3R)-2-oxopiperidin-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile(3R)-3-{[2-(imidazo[1,2-a]pyridin-7-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-oneN2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-propan-2-yl-D-alaninamide(3R)-3-{[2-(4-methoxyphenyl)-9-(propan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-fluorophenyl)-7-(propan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-fluorophenyl)-7-(propan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-8-(propan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-10-(oxetan-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-10-(oxan-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-(4-methoxyphenyl)-7-[1-(trifluoromethyl)cyclopropyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-7-(1-methylcyclopropyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2-(4-methoxyphenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-8-carbonitrile2-(4-methoxyphenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-9-carbonitrile2-(4-fluorophenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2-(1-methyl-1H-pyrazol-4-yl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2020328154 12 Jun 2026(3R)-3-{[10-(difluoromethyl)-9-methyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[8-(difluoromethyl)-9-methyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(difluoromethyl)-9-methyl-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({9-methyl-2-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(6R)-6-({2-[3-(dimethylamino)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[2-(3,4-dimethoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxy-2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({2-[4-(cyclopropyloxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[2-(5-bromofuran-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(3-aminophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({2-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-[(2-{4-[(propan-2-yl)oxy]phenyl}[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]-1,4-diazepan-5-one(6R)-6-({2-[1-(cyclopropylmethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[10-chloro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)-9-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-{[7-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-fluorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(3-fluorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-fluoro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-fluoro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-fluoro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)-7-(propan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({2-(1-methyl-1H-pyrazol-4-yl)-7-[1-(trifluoromethyl)cyclopropyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-({2-(4-methoxyphenyl)-7-[1-(trifluoromethyl)cyclopropyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(3R)-3-({2-[1-(2-methoxyethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one3-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azocan-2-one(2S)-2-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide2020328154 12 Jun 2026(3R)-3-{[2-(1-methyl-1H-1,2,3-triazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one1-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}cyclopropane-1-carboxamide4-(5-{[(3S)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrileN-butyl-N2-{2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}glycinamideN2-{2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-propyl-D-alaninamide(3R)-3-({2-[4-bromo-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-oneN-butyl-N2-[2-(3-cyanophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]alaninamide(2S)-2-{[2-(3-cyanophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide3-(5-{[2-oxoazocan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile(3R)-3-({2-[3-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-{[2-(3-bromophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3R)-3-({2-[3-(dimethylamino)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one3-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azocan-2-one(2S)-2-({2-[3-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[3-(methylsulfanyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2S)-2-({2-[2-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2R)-2-({2-[2-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-{[2-(2-bromophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3S)-3-{[2-(2-bromophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-bromophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-({2-[2-(dimethylamino)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3R)-3-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one(3R)-1-methyl-3-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one3-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azocan-2-one(2S)-2-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamideN-ethyl-2-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamideN-methyl-N2-{2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-norvalinamideN-propyl-N2-{2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-alaninamideN-butyl-N2-{2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}glycinamideN2-{2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}norleucinamideN2-{2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-serinamide(2R)-2-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide2020328154 12 Jun 2026(3R)-3-({2-[2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3R)-3-({2-[2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one3-({2-[2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azocan-2-one(2S)-2-({2-[2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2R)-2-({2-[2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamideN2-{2-[2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-methyl-D-norvalinamide(3R)-3-({2-[2-(methylsulfanyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(5-fluoropyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one (3R)-3-{[2-(5-chloropyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one (3S)-3-{[2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one (3R)-3-{[2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one (3R)-3-{[2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one (2R)-2-{[2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide N-butyl-N2-[2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]glycinamideN2-[2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-methyl-D-norvalinamide N2-[2-(3-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-propyl-D-alaninamide (3R)-3-({2-[2-(trifluoromethyl)pyridin-3-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one2020328154 12 Jun 2026(2R)-2-({2-[2-(trifluoromethyl)pyridin-3-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[4-(trifluoromethyl)pyridin-3-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-({2-[4-(trifluoromethyl)pyridin-3-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[5-fluoro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[5-fluoro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-oneN2-{2-[5-fluoro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-methyl-D-norvalinamideN2-{2-[5-fluoro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-propyl-D-alaninamide(2R)-2-({2-[5-fluoro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3R)-3-({2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-oneN2-{2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-methyl-D-norvalinamideN2-{2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-propyl-D-alaninamideN-butyl-N2-{2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}glycinamide2020328154 12 Jun 2026(2R)-2-({2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[5-bromo-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[5-bromo-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-({2-[5-bromo-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[4-methoxy-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[4-methoxy-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-oneN2-{2-[4-methoxy-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-methyl-D-norvalinamide(2R)-2-({2-[4-methoxy-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[4-methoxy-2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[4-methoxy-2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2S)-2-({2-[4-methoxy-2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2R)-2-({2-[4-methoxy-2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[4-fluoro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one2020328154 12 Jun 2026(3R)-3-({2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3R)-3-({2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-oneN-butyl-N2-{2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}alaninamide(2S)-2-({2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2R)-2-({2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2S)-2-({2-[4-bromo-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)piperidin-2-one(3R)-3-({2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)pyrrolidin-2-one3-({2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azocan-2-one(3S)-3-({2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1-methylazepan-2-one(2R)-2-({2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2S)-2-({2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamideN-butyl-N2-{2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}alaninamide2020328154 12 Jun 2026(3R)-3-({2-[1-(difluoromethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1-cyclopropyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3,5-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(5-bromofuran-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(4-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[2-(4-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(2R)-2-{[2-(4-methylthiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3R)-3-{[2-(4-fluorophenyl)-9-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-fluorophenyl)-9-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-9-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-9-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[9-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-8-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[8-methoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[8-methoxy-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-fluoro-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-fluoro-2-(pyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-chloro-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-chloro-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-oneN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valinamide(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide4-(7-bromo-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile4-(7-bromo-5-{[(3S)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile4-(7-bromo-5-{[(3R)-2-oxopiperidin-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile4-(7-bromo-5-{[(3R)-2-oxopyrrolidin-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrileN2-[7-bromo-2-(4-cyanophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-methyl-D-norvalinamide(2R)-2-{[7-bromo-2-(4-cyanophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(2S)-2-{[7-bromo-2-(4-cyanophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3R)-3-({7-bromo-2-[4-methoxy-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one2020328154 12 Jun 2026(3S)-3-({7-bromo-2-[4-methoxy-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-({7-bromo-2-[4-methoxy-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2S)-2-({7-bromo-2-[4-methoxy-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({7-bromo-2-[4-methoxy-2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({7-bromo-2-[4-methoxy-2-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-({7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2S)-2-({7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3S)-3-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valinamide(3R)-3-{[7-bromo-2-(1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[2-(3-fluorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(4-methoxyphenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3S)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}piperidin-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(4-methoxyphenyl)-7-(propan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(propan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[8,9-dimethoxy-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[8,9-dimethoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7,9-dibromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7,9-dibromo-2-(3-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7,9-dibromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7,9-dibromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[1-(oxetan-3-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one2020328154 12 Jun 2026(3R)-3-({2-[1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-[(2-{1-[2-(dimethylamino)ethyl]-1H-pyrazol-4-yl}[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]azepan-2-one(3R)-3-({2-[1-(oxan-4-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[1-(cyclopropylmethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1-cyclobutyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[3-(trifluoromethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1,3-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1,2,5-trimethyl-1H-pyrrol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one1,5-dimethyl-3-(5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)-1H-pyrrole-2-carbonitrile(3R)-3-{[2-(1-tert-butyl-1H-pyrazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one3R)-3-{[2-(5-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-imidazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[2-(2-chlorothiophen-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[4-(cyclopropyloxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-[(2-{4-[(propan-2-yl)oxy]phenyl}[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]azepan-2-one(3R)-3-{[2-(4-hydroxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[4-(difluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(4-ethoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[4-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(2-hydroxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2-(5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile(3R)-3-{[2-(4-aminophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-aminophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-aminophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2,6-dimethylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3,4-dimethoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-chloro-4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-fluoro-3-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxy-3-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxy-2-methylphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-fluoro-4-hydroxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-({2-[2-fluoro-4-(methylsulfanyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(2-fluoro-4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-[(2-{3-fluoro-4-[(propan-2-yl)oxy]phenyl}[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]azepan-2-one(3R)-3-{[2-(3,4-difluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-fluoro-4-hydroxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-fluoro-4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(5-methylpyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(6-aminopyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-fluoropyridin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(6-fluoropyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(2-fluoropyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(5-fluoro-6-methylpyridin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(pyrimidin-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[2-(trifluoromethyl)pyrimidin-5-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(pyridazin-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1,2-thiazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[1-(piperidin-4-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[10-(azetidin-3-yl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-[(2-{2-[methanesulfinyl]phenyl}[1,2,4]triazolo[1,5-c]quinazolin-5-yl)amino]azepan-2-one2020328154 12 Jun 2026(3R)-3-({2-[2-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[2-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[3-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-onemethyl 2-(1-methyl-1H-pyrazol-4-yl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carboxylatepropan-2-yl 2-(4-methoxyphenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carboxylate(3R)-3-{[2-(4-methoxyphenyl)-7-(morpholin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-10-(morpholin-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(6R)-6-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-methyl-1,4-diazepan-5-oneethyl N-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninateN-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanine(3R, R)-3-({2-[3-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R, S)-3-({2-[3-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R, R)-3-({2-[2-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R, S)-3-({2-[2-(S-methylsulfonimidoyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-N-ethyl-2-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2S)-N-ethyl-2-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide2020328154 12 Jun 2026N-cyclohexyl-N2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamideN-cyclopentyl-N2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide(3R)-3-{[7-ethoxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(2,2-difluoropropoxy)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-hydroxy-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-7-(3,3,3-trifluoropropoxy)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one4-[5-{[(3R)-2-oxoazepan-3-yl]amino}-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-2-yl]benzonitrile(3R)-3-({2-[4-chloro-2-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[4-chloro-2-(difluoromethoxy)phenyl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-ethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-cyclopropyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[1-(propan-2-yl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1,3-dimethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3S)-3-({7-bromo-2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(6S)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-oxazepan-5-one(3S)-3-({2-[4-bromo-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2S)-2-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-propylbutanamideN2-{7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-butyl-D-alaninamide(2S)-2-({7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-propylbutanamideN2-{7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-butyl-L-alaninamideN2-{7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-butyl-L-alaninamide(2S)-2-{[2-(pyrazin-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3R)-3-{[2-(pyrazin-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(2S)-2-{[2-(1-methyl-1H-1,2,3-triazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(2R)-2-{[2-(pyrazin-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamideN2-{7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-propyl-D-alaninamideN2-{7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-propyl-D-alaninamide(2S)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3S)-3-{[2-(pyrazin-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide2020328154 12 Jun 2026(2R)-2-({2-[4-bromo-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2S)-2-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(6R)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-oxazepan-5-one(2R)-2-({2-[4-bromo-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3S)-3-({2-[4-bromo-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2S)-2-({2-[4-bromo-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3R)-3-({2-[4-bromo-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(2R)-2-({2-[2-(1,1,2,2-tetrafluoroethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(2S)-2-({2-[2-(1,1,2,2-tetrafluoroethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)butanamide(3S)-3-({2-[2-(1,1,2,2-tetrafluoroethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[2-(1,1,2,2-tetrafluoroethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-oneN-butyl-N2-{2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-L-alaninamide4-[5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-2-yl]benzonitrile(6R)-6-({2-[4-chloro-2-(trifluoromethoxy)phenyl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-({2-[4-chloro-2-(difluoromethoxy)phenyl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-{[2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1-ethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-({7-bromo-2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-({2-[1-(propan-2-yl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one4-(7-bromo-5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile4-(5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}[1,2,4]triazolo[1,5-c]quinazolin-2-yl)benzonitrile(6R)-6-({2-[5-fluoro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-({2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one2-(4-methoxyphenyl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile(3R)-3-({2-[4-methoxy-3-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-oneN2-{7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-butyl-D-alaninamideN-butyl-N2-{2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-alaninamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-butyl-L-alaninamide(3R)-3-{[2-(4-methoxyphenyl)-10-(propan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(6R)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one hydrochloride4,4-dimethyl-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(-)-4,4-dimethyl-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(+)-4,4-dimethyl-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one3-(dimethylamino)-N-methyl-N2-[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide(6R)-6-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-oxazepan-5-one(3R)-1-methyl-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}pyrrolidin-2-one(3R)-3-{[2-(1,5-dimethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-3-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[1-(difluoromethyl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1H-pyrazol-3-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-ethyl-3,5-dimethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-1-methyl-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1,3-dimethyl-1H-pyrazol-5-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-cyclobutyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-({2-[1-(cyclopropylmethyl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1-cyclopropyl-3,5-dimethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(3-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-cyclopropyl-1,3-thiazol-2-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[3-methyl-1-(propan-2-yl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1-cyclopropyl-3-ethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(trifluoromethyl)-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-oneN-butyl- N2-[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide(3R)-3-{[7-methoxy-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-7-methoxy[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-ethyl-1H-pyrazol-4-yl)-7-methoxy[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-methoxy-2-(1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-methoxy-2-(1-methyl-1H-1,2,3-triazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-cyclopropyl-1H-pyrazol-4-yl)-7-methoxy[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[2-(1-cyclobutyl-1H-pyrazol-4-yl)-7-methoxy[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-[1-(propan-2-yl)-1H-pyrazol-4-yl]-7-(trifluoromethoxy)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one5-{[(3R)-2-oxoazepan-3-yl]amino}-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2-(1-cyclopropyl-1H-pyrazol-4-yl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2-(1-cyclobutyl-1H-pyrazol-4-yl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2-[1-(difluoromethyl)-1H-pyrazol-4-yl]-5-{[(3R)-2-oxoazepan-3-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile5-{[(3R)-2-oxoazepan-3-yl]amino}-2-(1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile(3R)-3-{[2-(4-methoxyphenyl)-7-(methylsulfanyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-(4-methoxyphenyl)-7-[(propan-2-yl)sulfanyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({2-(1-methyl-1H-pyrazol-4-yl)-7-[(propan-2-yl)sulfanyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[7-(ethylsulfanyl)-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(ethylsulfanyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({7-(methylsulfanyl)-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-7-(methylsulfanyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(morpholin-4-yl)propan-1-oneN-[2-(dimethylamino)ethyl]- N2-{2-[4-(methanesulfonyl)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-alaninamideN2-{2-[5-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-[2-(dimethylamino)ethyl]-D-alaninamideN-[2-(dimethylamino)ethyl]- N2-[2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide(2R)-2-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(4-methylpiperazin-1-yl)propan-1-one(2R)-2-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(morpholin-4-yl)propan-1-oneN2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(morpholin-4-yl)ethyl]-D-alaninamideN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(4-methylpiperazin-1-yl)ethyl]-D-alaninamideN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(morpholin-4-yl)ethyl]-D-alaninamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(morpholin-4-yl)ethyl]-D-alaninamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(4-methylpiperazin-1-yl)ethyl]-D-alaninamideN-(2-amino-2-methylpropyl)- N2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(morpholin-4-yl)propan-1-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(4-methylpiperazin-1-yl)propan-1-oneN-[2-(dimethylamino)ethyl]- N2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide2020328154 12 Jun 2026(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(4-methylpiperazin-1-yl)propan-1-oneN-(2-amino-2-methylpropyl)- N2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamideN-(2-amino-2-methylpropyl)- N2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamideformic acid N-[2-(dimethylamino)ethyl]- N2-{2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-alaninamide (1 / 1)N-[2-(dimethylamino)ethyl]- N2-{2-[2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-D-alaninamide(2R)-2-{[2-(1-methyl-1H-1,2,3-triazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-butyl-D-alaninamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-propyl-D-alaninamide(2R)-2-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-propylbutanamide(2R)-2-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-ethylbutanamide(2S)-2-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-ethylbutanamide(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(2S)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-5-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamideN2-{7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-propyl-L-alaninamide(2S)-2-({7-bromo-2-[4-chloro-2-(difluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-butylbutanamide2020328154 12 Jun 2026(2S)-2-{[2-(1-methyl-1H-pyrazol-5-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(2R)-2-{[2-(1-methyl-1H-pyrazol-5-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}butanamide(3S)-3-{[2-(1-methyl-1H-pyrazol-5-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-5-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-oneN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[3-(dimethylamino)propyl]-D-alaninamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[3-(dimethylamino)propyl]-D-alaninamideN2-{7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-N-propyl-L-alaninamide(2R)-2-({7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-propylbutanamide(2S)-2-({7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-butylbutanamide(2R)-2-({7-bromo-2-[4-chloro-2-(trifluoromethoxy)phenyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-N-butylbutanamide(3R)-3-{[7-bromo-2-(1,3-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-chloro-2-(1-cyclopropyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({7-chloro-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[7-chloro-2-(1-ethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-chloro-2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-({7-cyclopropyl-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[7-chloro-2-(1,3-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({7-bromo-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[7-bromo-2-(1,5-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(1-cyclobutyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({7-bromo-2-[1-(cyclopropylmethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-({7-bromo-2-[1-(difluoromethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[7-bromo-2-(4-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-bromo-2-(1-ethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({7-bromo-2-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(4-chlorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-onebenzyl (6R)-6-({7-fluoro-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-5-oxo-1,4-diazepane-1-carboxylate(6S)-6-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-thiazepan-5-one(6S)-6-({2-[1-(propan-2-yl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-thiazepan-5-one2020328154 12 Jun 2026(6S)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-thiazepan-5-one(6R)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-thiazepan-5-one(6R)-6-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-thiazepan-5-one(3R)-3-{[7-(methanesulfonyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-7-(propane-2-sulfonyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(ethanesulfonyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(propane-2-sulfonyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({7-(methanesulfonyl)-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-one(3R)-3-{[2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-7-(methanesulfonyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(6R)-6-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1A6,4-thiazepane-1,1,5-trione(1R*,6R)-6-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1A4,4-thiazepane-1,5-dione(6S)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1A6,4-thiazepane-1,1,5-trione(6S)-6-({2-[1-(propan-2-yl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1A6,4-thiazepane-1,1,5-trione(3R)-3-{[7-(S-methanesulfonimidoyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(6R)-6-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-imino-1A6,4-thiazepane-1,5-dione2020328154 12 Jun 2026(3R)-3-{[7-(methanesulfonyl)-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(2-hydroxypropan-2-yl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(hydroxymethyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(2-hydroxypropan-2-yl)-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[10-(hydroxymethyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-({2-(4-methoxyphenyl)-7-[(methylsulfanyl)methyl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)azepan-2-oneethyl N-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninatemethyl N-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valinatemethyl N-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valinateN-[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanineN-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanineN-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanineN-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valineN-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-valine(2R)-2-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(morpholin-4-yl)propan-1-one(2R)-1-(4-methylpiperazin-1-yl)-2-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}propan-1-one(2R)-1-[3-(dimethylamino)pyrrolidin-1-yl]-2-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}propan-1-oneN-[2-(dimethylamino)ethyl]-N-methyl- N2-[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide2020328154 12 Jun 2026N-(2-methoxyethyl)-N-methyl- N2-[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamideN-[2-(4-methylpiperazin-1-yl)ethyl]- N2-[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninamide(2R)-2-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(2-oxa-6-azaspiro[3.3]heptan-6-yl)propan-1-oneN2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(4-methylpiperazin-1-yl)ethyl]-D-alaninamidetert-butyl 4-{N-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}piperazine-1-carboxylatetert-butyl 4-{N-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}piperazine-1-carboxylatetert-butyl 4-[2-({N-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}amino)ethyl]piperazine-1-carboxylateN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-(2-methoxyethyl)-D-alaninamidetert-butyl 4-{N-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}piperazine-1-carboxylatetert-butyl [2-({N-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}amino)ethyl]methylcarbamatetert-butyl [2-({N-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}amino)ethyl]methylcarbamatetert-butyl [2-({N-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}amino)ethyl]methylcarbamatetert-butyl 4-[2-({N-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}amino)ethyl]piperazine-1-carboxylatetert-butyl 4-[2-({N-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}amino)ethyl]piperazine-1-carboxylatemethyl 4-{N-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}piperazine-1-carboxylate2020328154 12 Jun 2026N2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(piperidin-1-yl)ethyl]-D-alaninamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(piperidin-1-yl)ethyl]-D-alaninamideN2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(piperidin-1-yl)ethyl]-D-alaninamide(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]propan-1-oneN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-(2-hydroxy-2-methylpropyl)-D-alaninamideN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-(2-hydroxy-2-methylpropyl)-D-alaninamide(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(2S)-2-methylmorpholin-4-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(2S)-2-methylmorpholin-4-yl]propan-1-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(3R)-3,4-dimethylpiperazin-1-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(3R)-3-methylmorpholin-4-yl]propan-1-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(3R)-3-methylmorpholin-4-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(3R)-3,4-dimethylpiperazin-1-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]propan-1-one2020328154 12 Jun 2026(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(2-oxa-6-azaspiro[3.3]heptan-6-yl)propan-1-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(2-oxa-6-azaspiro[3.3]heptan-6-yl)propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(6-methyl-2,6-diazaspiro[3.3]heptan-2-yl)propan-1-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(6-methyl-2,6-diazaspiro[3.3]heptan-2-yl)propan-1-onetert-butyl 6-{N-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}-2,6-diazaspiro[3.3]heptane-2-carboxylatetert-butyl 6-{N-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}-2,6-diazaspiro[3.3]heptane-2-carboxylate(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-3-methyl-1-(4-methylpiperazin-1-yl)butan-1-oneN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-(2-methoxyethyl)-D-valinamideN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(4-methylpiperazin-1-yl)ethyl]-D-valinamide(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-3-methyl-1-(morpholin-4-yl)butan-1-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-3-methyl-1-(morpholin-4-yl)butan-1-oneN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(4-methylpiperazin-1-yl)ethyl]-D-valinamide(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-3-methyl-1-(4-methylpiperazin-1-yl)butan-1-oneN2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-(2-methoxyethyl)-D-valinamide2020328154 12 Jun 20262-(1-methyl-1H-pyrazol-4-yl)-5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2-(1-cyclopropyl-1H-pyrazol-4-yl)-5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2-(1-cyclobutyl-1H-pyrazol-4-yl)-5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile2-[1-(difluoromethyl)-1H-pyrazol-4-yl]-5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile5-{[(6R)-5-oxo-1,4-diazepan-6-yl]amino}-2-(1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazoline-7-carbonitrile(6R)-6-{[7-(methanesulfonyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-(methanesulfonyl)-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-(ethylsulfanyl)-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-(ethylsulfanyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-(ethanesulfonyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-methoxyphenyl)-7-(propane-2-sulfonyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-(ethanesulfonyl)-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1-methyl-1H-pyrazol-4-yl)-7-(propane-2-sulfonyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({7-(methanesulfonyl)-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-{[2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-7-(methanesulfonyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1-methyl-1H-pyrazol-5-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(4-chlorophenyl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(1,3-dimethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(1-cyclopropyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-chloro-2-(1,3-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({7-cyclopropyl-2-[1-(cyclopropylmethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-({7-cyclopropyl-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-({7-chloro-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[7-chloro-2-(1-ethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-chloro-2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[7-cyclopropyl-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-({2-[1-(propan-2-yl)-1H-pyrazol-4-yl]-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(1,3-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-{[2-(1-cyclopropyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[7-chloro-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-chloro-2-(1-cyclopropyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(1-methyl-1H-pyrazol-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({7-bromo-2-[1-(cyclopropylmethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[2-(1,5-dimethyl-1H-pyrazol-4-yl)-7-fluoro[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[2-(4-methoxyphenyl)-7-methyl[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({7-fluoro-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6S)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[7-bromo-2-(4-fluorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1,3-dimethyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(4-chlorophenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one2020328154 12 Jun 2026(6R)-6-({7-bromo-2-[1-(difluoromethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(1,5-dimethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(1-ethyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-({7-bromo-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6R)-6-({7-bromo-2-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(6S)-6-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-({7-bromo-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}amino)-1,4-diazepan-5-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(piperazin-1-yl)propan-1-one hydrogen chloride (1 / 1)(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(piperazin-1-yl)propan-1-oneN2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(methylamino)ethyl]-D-alaninamide hydrogen chloride (1 / 1)(2R)-2-{[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-(piperazin-1-yl)propan-1-one hydrogen chloride (1 / 1)N2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(methylamino)ethyl]-D-alaninamideN2-[2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(methylamino)ethyl]-D-alaninamide hydrogen chloride (1 / 1)N2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(methylamino)ethyl]-D-alaninamide hydrogen chloride (1 / 1)N2-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(piperazin-1-yl)ethyl]-D-alaninamide hydrogen chloride (1 / 2)2020328154 12 Jun 2026N2-[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-N-[2-(piperazin-1-yl)ethyl]-D-alaninamide hydrogen chloride (1 / 2)(6R)-6-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-methyl-1,4-diazepan-5-one(6R)-6-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-methyl-1,4-diazepan-5-one(3R)-3-{[7-(3-methoxy-3-methylbutoxy)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(2-hydroxy-2-methylpropoxy)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(cyclobutyloxy)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(cyclopropyloxy)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(3-hydroxy-3-methylbutoxy)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-7-(2-oxopyrrolidin-1-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[2-(4-methoxyphenyl)-7-(oxetan-3-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(methoxymethyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(methoxymethyl)-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one(3R)-3-{[7-(dimethylamino)-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-amino}azepan-2-one(3R)-3-{[7-(dimethylamino)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-amino}-azepan-2-one(3R)-3-{[2-(1-ethyl-1H-pyrazol-4-yl)-7-fluoro[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}azepan-2-one2020328154 12 Jun 2026(3R)-3-{[2-(1,5-dimethyl-1H-pyrazol-4-yl)-7-fluoro[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-amino}azepan-2-one(3R)-3-({7-fluoro-2-[1-(propan-2-yl)-1H-pyrazol-4-yl][1,2,4]triazolo[1,5-c]quinazolin-5-yl}-amino)azepan-2-one(3R)-3-{[7-(methanesulfonimidoyl)-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-amino}azepan-2-oneethyl N-[2-(1-methyl-1H-pyrazol-4-yl)-7-(trifluoromethyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninateethyl N-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alaninatemethyl 4-{N-[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-D-alanyl}piperazine-1-carboxylate(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]propan-1-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]propan-1-one(2R)-2-{[7-bromo-2-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(2R)-2-methylmorpholin-4-yl]propan-1-one(2R)-2-{[7-bromo-2-(4-methoxyphenyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1-[(2R)-2-methylmorpholin-4-yl]propan-1-one(6R)-6-{[7-bromo-2-(1-cyclopropyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6S)-6-{[7-bromo-2-(1-cyclopropyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[7-chloro-2-(1-ethyl-3-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one(6R)-6-{[2-(1-ethyl-1H-pyrazol-4-yl)-7-fluoro[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino}-1,4-diazepan-5-one2020328154 12 Jun 2026their polymorphs, enantiomeres, diastereomeres, racemates, tautomeres, N-oxides, hydrates, solvates, or their physiological acceptable salts or solvates of these salts, or mixtures of the same.
4. A method of preparing a compound of general formula (I) according to any one of claims 1 to 3, said method comprising the step of allowing an intermediate compound of general formula (V):N Cl(V),in which R1, R5, R6, R7 and R8 are as defined for the compound of general formula (I) according to claim 1 or 2,to react with a compound of general formula (VII):(VII),in which R2, R3 and R4 are as defined for the compound of general formula (I) according to claim 1 or 2,thereby giving a compound of general formula (I):(I),in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined for the compound of general formula (I) according to claim 1 or 2.2020328154 12 Jun 20265. A compound according to any one of claims 1 to 3 for use in the treatment or prophylaxis of a disease.
6. A pharmaceutical composition comprising a compound according to any one of claims 1 to 3 and one or more pharmaceutically acceptable excipients.
7. A pharmaceutical combination comprising:• one or more first active ingredients, being one or more compounds according to any one of claims 1 to 3, and• one or more pharmaceutical active anti cancer compounds or• one or more pharmaceutical active immune checkpoint inhibitors.
8. A method for the treatment or prophylaxis of a disease associated with aberrant AHR signaling, comprising administering to a subject in need thereof a compound according to any one of claims 1 to 3 or a pharmaceutical composition according to claim 6 or 7.
9. Use of a compound of general formula (I) according to any one of claims 1 to 3 for the preparation of a medicament for the treatment or prophylaxis of a disease associated with aberrant AHR signaling.
10. The method of claim 8 or the use of claim 9, wherein the disease is cancer or a condition associated with a dysregulated immune response.
11. The method or use of claim 10, wherein the disease or condition is a solid tumour or a liquid tumour.
12. A compound of general formula (V):2020328154 12 Jun 2026N XI(V),in which R1, R5, R6, R7 and R8 are as defined for the compound of general formula (I) according to claim 1 or 2,with the proviso that R5, R6, R7 and R8 do not represent hydrogen at the same time, whenR1 is phenyl or 4-chlorophenyl, and with the further proviso that the compound is not 5,9-dichloro-2-(2-furyl) [1,2,4]triazolo[1,5-c]quinazoline.
13. Use of a compound of general formula (V)N XI(V)in which R1, R5, R6, R7 and R8 are as defined for the compound of general formula (I) according to claim 1 or 2, for the preparation of a compound of general formula (I) according to any one of claims 1 to 3.