Dihydrooxadiazinones

Abstract

The present invention relates to dihydroxydiazinon compounds of the general formula (I): (In the formula, R 1 , R 2 , R 3 and R 4 is as defined herein), methods for preparing the compounds, intermediate compounds useful in preparing the compounds, pharmaceutical compositions and combinations comprising the compounds, and use of the compounds to manufacture pharmaceutical compositions for the treatment or prevention of diseases, particularly hyperproliferative diseases, either as the sole agent or in combination with other active ingredients.

Description

[Technical Field]

[0001] The present invention provides dihydrooxadiazinones of general formula (I) as described and defined herein, methods for preparing the compounds, pharmaceutical compositions and uses of the compounds for treating or preventing diseases, particularly hyperproliferative diseases. [Background technology]

[0002] Cancer kills more than 550,000 people in the United States and more than 8 million people worldwide each year. New drugs, including small molecules, molecules that affect tissue-specific growth requirements, and immunomodulatory agents, have been shown to benefit subsets of patients whose cancers harbor unique genomic mutations or other characteristics. Unfortunately, many cancer patients are left without effective treatment options.

[0003] One approach to identifying new anticancer drugs is phenotypic screening to discover novel small molecules that exhibit potent selectivity across cancer cell lines, followed by predictive chemogenomics to identify cellular features associated with drug response. In the 1990s, Weinstein and colleagues demonstrated that compound cytotoxicity profiles could be used to identify cellular characteristics, such as gene expression profiles and DNA copy number, that correlate with drug sensitivity. In recent years, automated high-throughput chemosensitivity testing of large panels of cell lines, combined with comprehensive genomic and phenotypic characterization of cell lines, has greatly increased our ability to identify cancer cell line features that mediate response to small molecules. Phenotypic observations of small molecule sensitivity can be correlated with expression patterns or somatic alterations, as in the case of trastuzumab-sensitive HER2-amplified breast cancer or erlotinib-sensitive EGFR-mutated lung cancer.

[0004] Phenotypic screening has identified some compounds known in the literature to be PDE3 inhibitors as useful in the treatment of certain cancers. Cell sensitivity typically requires coexpression of PDE3A and / or PDE3B with Schlafen 12 (SLFN12) polynucleotides or polypeptides. PDE3A / B inhibitors that induce drug sensitivity have been shown to stabilize the formation of complexes between PDE3A or PDE3B and SLFN12. PDE3A / B inhibitors that do not induce cell sensitivity typically do not stabilize the PDE3A- or PDE3B-SLFN12 complex.

[0005] Several PDE-3 inhibitors, such as milrinone, cilostazol, and levosimendan, are approved for the clinical treatment of cardiovascular indications or thrombocythemia (anagrelide), but not for cancer indications. A recent quality review of PDE inhibitors (Nature Reviews Drug Discovery 13, 290–314, (2014)) barely mentions cancer. Several PDE-3 inhibitors are known from International Publication Nos. 2014 / 164704, 2017 / 027854, and 2017 / 134231.

[0006] In particular, the undesirable effects of PDE-3 inhibitors mediated by their cardiac mode of action (Movsesian & Kukreja, SHFrancis et al. (eds.), Phosphodiesterases as Drug Targets, Handbook of Experimental Pharmacology 204, 2011; pp. 237ff) may limit their therapeutic use on a short-term or / and long-term basis, for example in cancer patients, where an adequate therapeutic window is required.

[0007] Although some dihydrooxadiazinones are known, the prior art does not describe the dihydrooxadiazinones of general formula (I) of the present invention as described and defined herein. [Prior art documents] [Patent documents]

[0008] [Patent Document 1] International Publication No. 2014 / 164704 Brochure [Patent Document 2] International Publication No. 2017 / 027854 Brochure [Patent Document 3] International Publication No. 2017 / 134231 Brochure [Non-patent literature]

[0009] [Non-Patent Document 1] Nature Reviews Drug Discovery 13, 290–314, (2014) [Non-patent document 2] Movsesian & Kukreja, SH Francis et al. (eds.), Phosphodiesterases as Drug Targets, Handbook of Experimental Pharmacology 204, 2011; p. 237ff. Summary of the Invention

[0010] It has now been found that the compounds of the present invention have surprising and advantageous properties, which form at least in part one basis for the present invention.

[0011] In particular, the compounds of the present invention surprisingly exhibit IC 50 It has been shown that compounds inhibit tumor cell proliferation at IC values ​​below 100 nM. Furthermore, compounds require higher concentrations for PDE3A and / or PDE3B inhibition, and IC values ​​for enzyme PDE3A and / or PDE3B inhibition are 50 IC values ​​for tumor cell proliferation 50The value of PDE3A-SLFN12 can be more than 2.5 times higher than the value.Without being bound by theory, this feature of inhibitory properties can be related to the induction of PDE3A-SLFN12 complex and / or the improvement of pharmacokinetic parameters in vivo or in vitro and / or the improvement of physicochemical properties and / or the improvement of safety pharmacological properties.Therefore, due to these advantageous properties, the compound described herein can be used for treating or preventing hyperproliferative diseases such as cancer disease.

[0012] The present invention provides compounds of general formula (I) that regulate the formation of PDE3A- and / or PDE3B-SLFN12 complexes, their preparation methods, pharmaceutical compositions, and uses thereof, as well as methods for treating or preventing diseases, particularly hyperproliferative diseases, more particularly cancer diseases. These and other features of the present teachings are presented herein. [Means for solving the problem]

[0013] According to a first aspect, the present invention provides compounds of general formula (I): [ka] (In the formula, R 1 is selected from a hydrogen atom, a halogen atom, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from a hydrogen atom and a halogen atom; R 3 teeth C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C9-cycloalkyl groups optionally substituted by hydroxy groups, C5-C9-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, -S-, -S(O)-, S(O)2 and -NR 9 - is a 3- to 9-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from In some cases, -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -CH2-O-, -NR 9 -CH2- and -CH2-NR 9 - further comprising a bridging group selected from: optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-haloalkyl group; C1-C3-alkoxy groups; C1-C3-haloalkoxy group; C(O)NR 5 R 6 Groups and NR 5 R 6 base a 3- to 9-membered heterocycloalkyl group independently selected from Partially unsaturated, 5- to 9-membered heterocycloalkyl groups optionally substituted with 1, 2, or 3 substituents, each of which may be an oxo group (=O), a C1-C3-alkyl group, or -C(O)R 5 R 6 groups and halogen atoms), aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6groups), monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group and NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and N.R. 7 R 8 basis Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom, a C1-C6-alkyl group, a -C1-C5-alkylene-O-C1-C5-alkyl group, a -C1-C5-alkylene-S-C1-C5-alkyl group, a C3-C6-cycloalkyl group and a C3-C5-heterocycloalkyl group; R 7 / R 8 teeth Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl group, which is optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, C(O)NR 5 R 6 group, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally substituted by 1 or 2 substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; 3- to 7-membered heterocycloalkyl groups, which themselves are optionally substituted with C1-C3-alkyl or oxo (=O) groups heteroaryl groups which themselves are optionally substituted by C1-C3-alkyl groups; (independently selected from -C1-C5-alkylene-O-C1-C5-alkyl group, -C1-C5-alkylene-S-C1-C5-alkyl group, -C1~C5-Alkylene-NR 5 -C1 to C5 alkyl group, C3-C6-cycloalkyl groups optionally substituted by hydroxy groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond. or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

[0014] The compounds are suitable for treating patients with cancers sensitive to treatment with phosphodiesterase 3A / B (PDE3A / B) modulators by detecting the co-expression of PDE3A and / or PDE3B with Schlafen 12 (SLFN12) and / or SLFN12L mRNA, polynucleotide or polypeptide, and / or the lack of decreased expression of CREB3L1 mRNA, polynucleotide or polypeptide in cancer cells derived from such patients.

[0015] definition Unless otherwise defined, all technical and scientific terms used herein have the meanings that are commonly understood by those skilled in the art to which this invention belongs.The following references provide those skilled in the art with many of the general definitions of the terms used in this invention: Singleton et al., Dictionary of Microbiology and Molecular Biology (2nd edition 1994); The Cambridge Dictionary of Science and Technology (Walker, ed., 1988); The Glossary of Genetics, 5th edition, R. Rieger et al. (ed.), Springer Verlag (1991); and Hale & Marham, The HarperCollins Dictionary of Biology (1991).As used herein, the following terms have the meanings that are ascribed to them below, unless otherwise specified.

[0016] The structure depicted includes all allowed rotations about the bonds.

[0017] The term "substituted" means that one or more hydrogen atoms on the specified atom or group are replaced with one selected from the indicated group, provided that the normal valence of the specified atom in the circumstances present is not exceeded. Combinations of substituents and / or variables are permissible.

[0018] The term "optionally substituted" means that the number of substituents can be equal to or different from 0. Unless otherwise specified, an optionally substituted group can be substituted with as many optional substituents as can be accommodated by replacing a hydrogen atom with a non-hydrogen substituent on any available carbon or nitrogen atom. Generally, if present, the number of optional substituents can be 1, 2, 3, particularly 1 or 2.

[0019] As used herein, the term "one or more" in the definition of substituents, for example, in compounds of general formula (I) of the present invention, means "1, 2, 3, 4 or 5, particularly 1, 2, 3 or 4, more particularly 1, 2 or 3, even more particularly 1 or 2".

[0020] As used herein, an oxo substituent represents an oxygen atom that is attached to a carbon or sulfur atom via a double bond.

[0021] The term "ring substituent" means a substituent attached to an aromatic or non-aromatic ring that replaces an available hydrogen atom on the ring.

[0022] A compound substituent is composed of multiple moieties, e.g., (C1-C4-alkyl)-O-(C1-C4-alkyl)-, and the first or last hyphen in such a compound substituent indicates the point of attachment of the compound substituent to the rest of the molecule. If a compound substituent is substituted, the substituent may be attached at any suitable carbon atom of the compound substituent.

[0023] When a ring containing carbon atoms and optionally one or more heteroatoms, such as nitrogen, oxygen, or sulfur atoms, is substituted with a substituent, the substituent may be attached at any suitable position on the ring and is attached to a suitable carbon atom and / or a suitable heteroatom.

[0024] The term "comprising" as used herein includes "consisting of."

[0025] In the text, when any item is referred to as "mentioned in this specification", it means that it can be mentioned anywhere in the text.

[0026] Terms referred to in this document have the following meanings: The term "halogen atom" means a fluorine, chlorine, bromine or iodine atom, in particular a fluorine, chlorine or bromine atom.

[0027] The term "C1-C6-alkyl" means a linear or branched saturated monovalent hydrocarbon radical having 1, 2, 3, 4, 5 or 6 carbon atoms, such as 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. In particular, the radicals have 1, 2, 3 or 4 carbon atoms ("C1-C4-alkyl"), such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl or tert-butyl radicals, and more in particular have 1, 2 or 3 carbon atoms ("C1-C3-alkyl"), such as methyl, ethyl, n-propyl or isopropyl radicals.

[0028] The term "alkylene" is derived from the term "alkyl" as a divalent component designated by adding "ene" to the term "alkyl," e.g., "methyl" becomes "methylene," meaning a "-CH-" component with open bonds of branched components at each end of the longest chain.

[0029] The term "C1-C6-haloalkyl" means a linear or branched saturated monovalent hydrocarbon radical in which the term "C1-C6-alkyl" is defined as above and in which one or more hydrogen atoms are replaced, identically or differently, by halogen atoms. In particular, the halogen atoms are fluorine atoms. C1-C6-haloalkyl groups are, 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, more particularly trifluoromethyl.

[0030] The term "C1-C6-alkoxy" means a linear or branched saturated monovalent radical of the formula (C1-C6-alkyl)-O-, where the term "C1-C6-alkyl" is defined above, such as a methoxy, ethoxy, n-propoxy, iso-propoxy, n-butoxy, sec-butoxy, iso-butoxy, tert-butoxy, pentyloxy, isopentyloxy or n-hexyloxy group, or an isomer thereof.

[0031] The term "C1-C6-haloalkoxy" means a linear or branched saturated monovalent C1-C6-alkoxy group as defined above, in which one or more hydrogen atoms are replaced by identical or different halogen atoms. In particular, the halogen atoms are fluorine atoms. C1-C6-haloalkoxy groups are, for example, fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy or pentafluoroethoxy.

[0032] The term "C2-C6-alkenyl" denotes a straight-chain or branched monovalent hydrocarbon radical containing one or two double bonds and having 2, 3, 4, 5 or 6 carbon atoms, in particular 2 or 4 carbon atoms ("C2-C4-alkenyl"); if an alkenyl group contains more than one double bond, the double bonds can be isolated from one another or conjugated to one another. Alkenyl groups include, for example, ethenyl (or "vinyl"), prop-2-en-1-yl (or "allyl"), prop-1-en-1-yl, but-3-enyl, but-2-enyl, but-1-enyl, pent-4-enyl, pent-3-enyl, pent-2-enyl, pent-1-enyl, hex-5-enyl, hex-4-enyl, hex-3-enyl, hex-2-enyl, hex-1-enyl, prop-1-en-2-yl (or "isopropenyl") ), 2-methylprop-2-enyl, 1-methylprop-2-enyl, 2-methylprop-1-enyl, 1-methylprop-1-enyl, 3-methylbut-3-enyl, 2-methylbut-3-enyl, 1-methylbut-3-enyl, 3-methylbut-2-enyl, 2-methylbut-2-enyl, 1-methylbut-2-enyl, 3-methylbut-1-enyl, 2-methylbut-1-enyl, 1-methylbut-1-enyl, 1,1-dimethylprop-2-enyl, 1- Ethylprop-1-enyl, 1-propylvinyl, 1-isopropylvinyl, 4-methylpent-4-enyl, 3-methylpent-4-enyl, 2-methylpent-4-enyl, 1-methylpent-4-enyl, 4-methylpent-3-enyl, 3-methylpent-3-enyl, 2-methylpent-3-enyl, 1-methylpent-3-enyl, 4-methylpent-2-enyl, 3-methylpent-2-enyl, 2-methylpent-2-enyl, 1-methylpenta -2-enyl, 4-methylpent-1-enyl, 3-methylpent-1-enyl, 2-methylpent-1-enyl, 1-methylpent-1-enyl, 3-ethylbut-3-enyl, 2-ethylbut-3-enyl, 1-ethylbut-3-enyl, 3-ethylbut-2-enyl, 2-ethylbut-2-enyl, 1-ethylbut-2-enyl, 3-ethylbut-1-enyl, 2-ethylbut-1-enyl, 1-ethylbut-1-enyl, 2-propylprop-2-enyl, The 1-propylprop-2-enyl, 2-isopropylprop-2-enyl, 1-isopropylprop-2-enyl, 2-propylprop-1-enyl, 1-propylprop-1-enyl, 2-isopropylprop-1-enyl, 1-isopropylprop-1-enyl, 3,3-dimethylprop-1-enyl, 1-(1,1-dimethylethyl)ethenyl, buta-1,3-dienyl, penta-1,4-dienyl or hexa-1,5-dienyl radicals. In particular, the radicals are vinyl or allyl, propenyl, isopropenyl, butenyl or isobutenyl radicals.

[0033] The term "C2-C6-alkynyl" denotes a linear or branched monovalent hydrocarbon radical containing one triple bond and containing 2, 3, 4, 5 or 6 carbon atoms, especially 2 or 3 carbon atoms ("C2-C3-alkynyl"). C2-C6-alkynyl groups are, for example, ethynyl, prop-1-ynyl, prop-2-ynyl (or "propargyl"), but-1-ynyl, but-2-ynyl, but-3-ynyl, pent-1-ynyl, pent-2-ynyl, pent-3-ynyl, pent-4-ynyl, hex-1-ynyl, hex-2-ynyl, hex-3-ynyl, hex-4-ynyl, hex-5-ynyl, 1-methylprop-2-ynyl, 2-methylbut-3-ynyl, 1-methylbut-3-ynyl, 1-methylbut-2-ynyl, 3-methylbut-1-ynyl, 1-ethylprop-2-ynyl, 3-methylpent-4-ynyl. Alkynyl groups include ethynyl, 2-methylpent-4-ynyl, 1-methylpent-4-ynyl, 2-methylpent-3-ynyl, 1-methylpent-3-ynyl, 4-methylpent-2-ynyl, 1-methylpent-2-ynyl, 4-methylpent-1-ynyl, 3-methylpent-1-ynyl, 2-ethylbut-3-ynyl, 1-ethylbut-3-ynyl, 1-ethylbut-2-ynyl, 1-propylprop-2-ynyl, 1-isopropylprop-2-ynyl, 2,2-dimethylbut-3-ynyl, 1,1-dimethylbut-3-ynyl, 1,1-dimethylbut-2-ynyl, and 3,3-dimethylbut-1-ynyl groups. In particular, the alkynyl group is ethynyl, prop-1-ynyl, or prop-2-ynyl.

[0034] The term "C3-C9-cycloalkyl" denotes a saturated monovalent monocyclic or bicyclic hydrocarbon ring containing 3, 4, 5, 6, 7 or 8 carbon atoms. C3-C8-cycloalkyl groups are, for example, monocyclic hydrocarbon rings such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl groups, and also include, for example, bicyclic hydrocarbon rings such as bicyclo[4.2.0]octyl, bicyclo[2.2.1]heptyl or octahydropentalenyl, as well as fused-, bridged- and spiro-cycloalkyl ring systems such as the spirocycloalkyl systems defined below.

[0035] The term "spirocycloalkyl" refers to a saturated monovalent bicyclic hydrocarbon group in which two rings share one common ring carbon atom, the bicyclic hydrocarbon group containing 5, 6, 7, 8, or 9 carbon atoms, and the spirocycloalkyl group can be attached to the remainder of the molecule through any one of the carbon atoms except the spiro carbon atom. Examples of spirocycloalkyl groups include spiro[2.2]pentyl, spiro[2.3]hexyl, spiro[2.4]heptyl, spiro[2.5]octyl, spiro[2.6]nonyl, spiro[3.3]heptyl, spiro[3.4]octyl, spiro[3.5]nonyl, spiro[3.6]decyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[4.6]undecyl, and spiro[5.5]undecyl. The term "C5-C6-cycloalkenyl" refers to the resulting cyclopentenyl, cyclohexenyl, cyclopentadienyl, cyclohexadienyl groups.

[0036] The term "C4-C9-cycloalkenyl" denotes a monovalent monocyclic or bicyclic hydrocarbon ring containing 4, 5, 6, 7, 8 or 9 carbon atoms and one double bond. In particular, the ring contains 4, 5 or 6 carbon atoms ("C4-C6-cycloalkenyl"). A C4-C8-cycloalkenyl group is a monocyclic hydrocarbon ring, such as a cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl or cyclooctenyl group, or a bridged ring system, as well as a bicyclic hydrocarbon ring, such as a bicyclo[2.2.1]hept-2-enyl or bicyclo[2.2.2]oct-2-enyl, bicyclo[3.1.0]hex-2-enyl.

[0037] The terms "3- to 9-membered heterocycloalkyl" and "3- to 6-membered heterocycloalkyl" refer to saturated heterocycles having a total of 3, 4, 5, 6, 7, 8, or 9 ring atoms, respectively, containing one or two ring heteroatoms selected from the same or different series N, O, and S, and 3, 4, 5, or 6 ring atoms, respectively, where the heterocycloalkyl group is attached to the remainder of the molecule through any one of the carbon atoms or heteroatoms. This also includes bicyclic ring systems, either fused, bridged, or spiro, as defined below. This also potentially includes NR 7 R 8 groups (wherein the N atoms are not R groups that form a non-aromatic ring with the N atom to which they are attached) 7 and R 8 The term "heterocycloalkane" as used herein refers to a compound consisting of a heterocycloalkyl group, as defined herein, and a hydrogen atom to which the heterocycloalkyl group is attached at one valence.

[0038] Heterocycloalkyl groups can be, but are not limited to, three- or four-membered rings such as, for example, azacyclopropyl, oxacyclopropyl, azetidinyl, oxetanyl, or thietanyl; five-membered rings such as, for example, tetrahydrofuranyl, 1,3-dioxolanyl, thiolanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, 1,1-dioxidethiolanyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl, or 1,3-thiazolidinyl; or six-membered rings such as tetrahydropyranyl, tetrahydrothiopyranyl, piperidinyl, morpholinyl, dithianyl, thiomorpholinyl, piperazinyl, 1,3-dioxanyl, 1,4-dioxanyl, or 1,2-oxazinanyl, or fused systems such as, for example, azabicyclo[3.1.0]hexan-3-yl.

[0039] In particular, "4- to 6-membered heterocycloalkyl" refers to a 4- to 6-membered heterocycloalkyl as defined above containing one ring nitrogen atom, oxygen atom, or sulfur atom, and if it contains a nitrogen atom, it may optionally contain one additional ring heteroatom of the series: N, O, S. More specifically, "5- or 6-membered heterocycloalkyl" refers to a monocyclic saturated heterocycle having a total of 5 or 6 ring atoms, including one ring nitrogen atom and optionally one additional ring heteroatom of the series: N, O. The heterocycloalkyl group is attached to the rest of the molecule through any carbon atom or, if applicable, any nitrogen atom. Both of these may include the bicyclic ring systems described above.

[0040] The term "partially unsaturated 3- to 9-membered heterocycloalkyl" refers to a monocyclic unsaturated non-aromatic heterocycle having a total of 5, 6, 7, 8, or 9 ring atoms, including one or two double bonds and one or two ring heteroatoms of the same or different series: N, O, S; the partially unsaturated heterocycloalkyl group can be attached to the remainder of the molecule through any one of the carbon atoms or, if present, the nitrogen atom. The term "partially unsaturated heterocycloalkane," as used herein, refers to a compound consisting of a partially unsaturated heterocycloalkyl group, as defined herein, and a hydrogen atom to which the partially unsaturated heterocycloalkyl group is attached at one of its valencies.

[0041] Partially unsaturated heterocycloalkyl groups are, for example, 4H-pyranyl, 2H-pyranyl, 3,6-dihydro-2H-pyran-4-yl, 5,6-dihydro-2H-pyran-3-yl, tetrahydropyridinyl, such as 1,2,3,6-tetrahydropyridin-4-yl, dihydropyridinyl, such as 1,6-dihydropyridinyl, 6-oxo-1,6-dihydropyridin-3-yl, 2,5-dihydro-1H-pyrrolyl, [1,3]dioxolyl, 4H-[1,3,4]thiadiazinyl, 2,5-dihydrofuranyl, 2,3-dihydrofuranyl, 2,5-dihydrothio-phenyl, 2,3-dihydrothiophenyl, 4,5-dihydrooxazolyl or 4H-[1,4]thiazinyl.

[0042] The term "fused heterocycloalkyl" means a bicyclic saturated heterocycle containing one or two ring heteroatoms of the same or different series: N, O, S, where the two rings share two adjacent ring atoms and have a total of 6, 7, 8, or 9 ring atoms, or a total of 5, 6, or 7 ring atoms, respectively; the fused heterocycloalkyl group can be attached to the rest of the molecule through any one of the carbon atoms or, if present, the nitrogen atom.

[0043] Fused heterocycloalkyl groups are, for example, 3-azabicyclo[3.1.0]hexan-3-yl, 3-azabicyclo[3.2.0]heptan-3-yl, azabicyclo[3.3.0]octyl, azabicyclo[4.3.0]nonyl, diazabicyclo[4.3.0]nonyl, oxazabicyclo[4.3.0]nonyl or thiazabicyclo[4.3.0]nonyl.

[0044] The term "bridged heterocycloalkyl" refers to a bicyclic saturated heterocycle having a total of 7, 8, or 9 ring atoms, or a total of 7 ring atoms, respectively, containing one or two ring heteroatoms of the same or different series: N, O, S, where the two rings share two common ring atoms that are not adjacent; the bridged heterocycloalkyl group can be attached to the rest of the molecule through any one of the carbon atoms or, if present, the nitrogen atom. Examples of bridged heterocycloalkyl groups include 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, azabicyclo[3.2.1]octyl, diazabicyclo[3.2.1]octyl, and the like. .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, thiazabicyclo[4.2.1]nonyl.

[0045] The term "heterospirocycloalkyl" refers to a bicyclic saturated heterocycle having a total of 6, 7, 8, or 9 ring atoms, containing one or two ring heteroatoms of the same or different series: N, O, S, where the two rings share one common ring carbon atom; the heterospirocycloalkyl group can be attached to the rest of the molecule through any one of the carbon atoms other than the spiro carbon atom or, if present, the nitrogen atom. Heterospirocycloalkyl groups include, for example, azaspiro[2.3]hexyl, azaspiro[3.3]heptyl, oxazaspiro[3.3]heptyl, thiazaspiro[3.3]heptyl, 2λ 6 -thia-6-azaspiro[3.3]heptane-2,2-dione, oxaspiro[3.3]heptyl, oxazaspiro[5.3]nonyl, oxazaspiro[4.3]octyl, diazaspiro[3.3]heptyl, thiazaspiro[3.3]heptyl, thiazaspiro[4.3]octyl, or one of 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]-.

[0046] The term "aryl" refers to an aromatic monocyclic, bicyclic (two fused rings), tricyclic (three fused rings), or polycyclic (two or more fused rings) hydrocarbon ring system having 6 to 20 (e.g., 6 to 10 ring carbon atoms). Non-limiting examples of aryl groups include phenyl or naphthyl (e.g., 1-naphthyl, 2-naphthyl, etc.).

[0047] The term "heteroaryl" refers to a monovalent monocyclic or bicyclic aromatic ring having 5, 6, 8, 9, or 10 ring atoms (a "5-10 membered heteroaryl" group), particularly 5, 6, 9, or 10 ring atoms, containing at least one ring heteroatom and optionally one, two, or three additional ring heteroatoms of the series: N, O, and / or S, and bonded to the remainder of the molecule via a ring carbon atom or heteroatom. The term "heteroarene," as used herein, refers to a compound consisting of a heteroaryl group, as defined herein, and a hydrogen atom to which the heteroaryl group is bonded at one of its valencies.

[0048] Heteroaryl groups include 5-membered heteroaryl groups (such as thienyl, furanyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, or tetrazolyl); or 6-membered heteroaryl groups (such as pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, or triazinyl); or tricyclic heteroaryl groups (such as carbazolyl, acridinyl, or furanyl). or a 9-membered heteroaryl group (such as benzofuranyl, benzothienyl, benzoxazolyl, benzisoxazolyl, benzimidazolyl, benzothiazolyl, benzotriazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, or purinyl); or a 10-membered heteroaryl group (such as quinolinyl, quinazolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, or pteridinyl).

[0049] In general, unless otherwise specified, a heteroaryl or heteroarylene group includes all its possible isomeric forms, such as tautomers and positional isomers, with respect to the point of attachment to the rest of the molecule. Thus, for some illustrative, non-limiting 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.

[0050] In particular, heteroaryl groups are 2H-pyrrol-1-yl, 1H-pyrazol-4-yl, 1H-pyrazol-5-yl groups, optionally substituted by one or two methyl groups; 1,2-thiazol-4-yl, 1,3-thiazol-5-yl, pyridin-3-yl, pyridin-4-yl, and pyridin-5-yl groups, each optionally substituted by one or two substituents, each independently selected from halogen atoms, methyl groups, trifluoromethyl groups, methoxy groups, and NH groups; 1H-indol-6-yl, 1H-indazol-6-yl, and 1H-benzimidazol-6-yl groups, each optionally substituted by one or two substituents, each independently selected from halogen atoms, methyl groups, trifluoromethyl groups, methoxy groups, and NH groups.

[0051] In particular, heteroaryl groups are: a 2H-pyrrol-1-yl group optionally substituted with one or two substituents, each substituent being independently selected from a hydrogen atom, a cyano group, and a methyl group; a 1H-pyrazol-4-yl group optionally substituted by one or two methyl groups; a 1H-pyrazol-5-yl group optionally substituted by one or two methyl groups; a 1,2-thiazol-4-yl group optionally substituted by one or two methyl groups; a 1,3-thiazol-5-yl group optionally substituted by one or two methyl groups; pyridin-3-yl and pyridin-5-yl groups, each of which is optionally substituted with one or two substituents, each of which is independently selected from halogen atoms, methyl groups, trifluoromethyl groups, methoxy groups, and NH groups; These are the 1H-indol-6-yl group, the 1H-indazol-6-yl group and the 1H-benzimidazol-6-yl group.

[0052] More specifically, the heteroaryl group is a pyridinyl group optionally substituted with an amino group, or a pyrazolyl group optionally substituted with a difluoromethyl or trifluoromethyl group.

[0053] Even more specifically, the heteroaryl group is a 4-pyridinyl group substituted with an amino group, or It is a 1H-pyrazol-4-yl or 1H-pyrazol-1-yl group optionally substituted with a difluoromethyl or trifluoromethyl group.

[0054] The term "C1-C6" as used herein, for example in the context of the definitions of "C1-C6-alkyl", "C1-C6-haloalkyl", "C1-C6-alkoxy" or "C1-C6-haloalkoxy", refers to an alkyl group having a finite number of carbon atoms, from 1 to 6, i.e., 1, 2, 3, 4, 5 or 6 carbon atoms.

[0055] Furthermore, as used herein, the term "C3-C8" as used herein, for example, in the context of the definition of "C3-C8-cycloalkyl", refers to a cycloalkyl group having a finite number of carbon atoms, from 3 to 8, i.e., 3, 4, 5, 6, 7 or 8 carbon atoms.

[0056] When a range of values ​​is given, the range includes each value and sub-range within the range.

[0057] for example: "C1~C6" means C1, C2, C3, C4, C5, C6, C1~C6, C1~C5, C1~C4, C1~C3, C1~C2, C2~C6 , C2~C5, C2~C4, C2~C3, C3~C6, C3~C5, C3~C4, C4~C6, C4~C5 and C5~C6; "C2~C6" is C2, C3, C4, C5, C6, C2~C6, C2~C5, C2~C4, C2~C3, C3~C6, C3~C 5、 including C3-C4, C4-C6, C4-C5 and C5-C6; "C3~C10 ” is C3, C4, C5, C6, C7, C8, C9, C 10 , C3~C 10 , C3~C9, C3~C8, C3~C7, C3~C6, C3~C5, C3~C4, C4~C 10 , C4~C9, C4~C8, C4~C7, C4~C6, C4~C5, C5~C 10 , C5~C9, C5~C8, C5~C7, C5~C6, C6~C 10 , C6~C9, C6~C8, C6~C7, C7~C 10 , C7~C9, C7~C8, C8~C 10 , C8-C9 and C9-C 10 encompasses; "C3-C8" includes C3, C4, C5, C6, C7, C8, C3-C8, C3-C7, C3-C6, C3-C5, C3-C4, C4-C8, C4-C7, C4-C6, C4-C5, C5-C8, C5-C7, C5-C6, C6-C8, C6-C7 and C7-C8; "C3-C6" includes C3, C4, C5, C6, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5, and C5-C6; "C4-C8" includes C4, C5, C6, C7, C8, C4-C8, C4-C7, C4-C6, C4-C5, C5-C8, C5-C7, C5-C6, C6-C8, C6-C7, and C7-C8; "C4-C7" includes C4, C5, C6, C7, C4-C7, C4-C6, C4-C5, C5-C7, C5-C6, and C6-C7; "C4-C6" includes C4, C5, C6, C4-C6, C4-C5, and C5-C6; "C5~C 10 ” is C5, C6, C7, C8, C9, C 10 , C5~C 10 , C5~C9, C5~C8, C5~C7, C5~C6, C6~C 10 , C6~C9, C6~C8, C6~C7, C7~C 10 , C7~C9, C7~C8, C8~C 10 , C8-C9 and C9-C 10 encompasses; "C6~C 10" is C6, C7, C8, C9, C 10 , C6~C 10 , C6~C9, C6~C8, C6~C7, C7~C 10 , C7~C9, C7~C8, C8~C 10 , C8-C9 and C9-C 10 Includes.

[0058] Unless otherwise specified or obvious from the context, the term "about" as used herein is understood to mean within the normal tolerance range in the art, for example, within 2 standard deviations of the mean. About can be understood to be within 10%, 9%, 8%, 7%, 6%, 5%, 4%, 3%, 2%, 1%, 0.5%, 0.1%, 0.05% or 0.01% of the specified value. Unless otherwise clear from the context, all numerical values ​​provided herein are modified by the term about.

[0059] By "agent" is meant any small molecule chemical compound, antibody, nucleic acid molecule or polypeptide, or fragment thereof.

[0060] By "ameliorate" is meant to lessen, inhibit, attenuate, reduce, arrest or stabilize the onset or progression of a disease.

[0061] "Analog" refers to a molecule that is not identical but has similar functional or structural characteristics. For example, a polypeptide analog retains the biological activity of the corresponding native polypeptide but has certain biochemical modifications that enhance the analog's function compared to the native polypeptide. Such biochemical modifications could, for example, increase the analog's protease resistance, membrane permeability, or half-life without altering ligand binding. Analogs can include unnatural amino acids.

[0062] In this disclosure, "comprises," "comprising," "containing," "having," and the like can have the meaning ascribed to them in U.S. patent law and can mean "includes," "including," and the like; "consisting essentially of" or "consists essentially" likewise have the meaning ascribed to them in U.S. patent law, and the terms are open-ended, permitting the presence of more than what is recited so long as the basic or novel characteristics of the recited items are not changed by the presence of more than what is recited, but excluding prior art embodiments.

[0063] "Detecting" refers to identifying the presence, absence, or amount of the analyte being detected. In certain embodiments, the analyte is a PDE3A or SLFN12 polypeptide.

[0064] "Disease" means any condition or disorder that impairs or interferes with the normal function of a cell, tissue, or organ. Examples of diseases include hyperproliferative disorders, such as cancer types, including adenocarcinoma, breast cancer, cervical cancer, liver cancer, lung cancer, and melanoma.

[0065] " Effective amount " refers to the amount of compound described herein that is required to improve the symptoms of disease compared with untreated patients.The effective amount of one or more active compounds used to carry out the present invention for the therapeutic treatment of disease varies depending on the mode of administration, age, weight and general health of the subject.Finally, the attending physician or veterinarian will determine the appropriate amount and administration schedule.This amount is called "effective" amount.In yet another embodiment, PDE3A modulator is a compound of formula (I).

[0066] As used herein, the term "leaving group" refers to an atom or group of atoms that will be displaced in a chemical reaction as a stable species with the bonding electrons. In particular, such leaving groups are selected from the group comprising halide, especially fluoride, chloride, bromide or iodide, (methylsulfonyl)oxy, [(trifluoromethyl)sulfonyl]oxy, [(nonafluorobutyl)sulfonyl]oxy, (phenylsulfonyl)oxy, [(4-methylphenyl)sulfonyl]oxy, [(4-bromophenyl)sulfonyl]oxy, [(4-nitrophenyl)sulfonyl]oxy, [(2-nitrophenyl)sulfonyl]oxy, [(4-isopropylphenyl)sulfonyl]oxy, [(2,4,6-triisopropylphenyl)sulfonyl]oxy, [(2,4,6-trimethylphenyl)sulfonyl]oxy, [(4-tert-butyl-phenyl)sulfonyl]oxy and [(4-methoxyphenyl)sulfonyl]oxy.

[0067] "Modulator" means any agent that binds to a polypeptide and alters the biological function or activity of that polypeptide. Modulators include, but are not limited to, agents that reduce or eliminate the biological function or activity of a polypeptide (e.g., "inhibitors"). For example, a modulator may inhibit the catalytic activity of a polypeptide. Modulators include, but are not limited to, agents that increase or decrease binding of a polypeptide to another agent. For example, a modulator can promote binding of a polypeptide to another polypeptide.

[0068] Unless otherwise stated or obvious from context, as used herein, the term "or" is understood to be inclusive. Unless otherwise stated or obvious from context, as used herein, the terms "a," "an," and "the" are understood to be singular or plural.

[0069] When the plural of a word such as compounds, salts, polymorphs, hydrates, solvates, etc. is used herein, this is also taken to mean a single compound, salt, polymorph, isomer, hydrate, solvate, etc.

[0070] 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.

[0071] The term "prodrugs" or "prodrug" refers to compounds that may themselves be biologically active or inactive, but are converted (e.g., metabolically or hydrolytically) into compounds according to the present invention during their residence in the body. Derivatives (biological precursors or prodrugs) of compound 6 and its salts that are converted into compound 6 and its salts in a biological system are encompassed by the present invention. The biological system may be, for example, a mammalian organism, particularly a human subject. The biological precursor is, for example, converted into the compound of formula (I) or its salt by a metabolic process.

[0072] The term "one or more pharmaceutically acceptable salts" of a compound of formula (I) includes those derived from pharmaceutically acceptable inorganic and organic acids and bases. See, for example, S. M. Berge et al., "Pharmaceutical Salts," J. Pharm. Sci. 1977, 66, 1-19.

[0073] As used herein, the term "pharmaceutically acceptable salt" refers to a salt formed by the addition of a pharmaceutically acceptable acid or base to a compound disclosed herein.

[0074] As used herein, the phrase "pharmaceutically acceptable" refers to a substance that is acceptable for use in pharmaceutical applications from a toxicological standpoint and does not adversely interact with active ingredients.

[0075] As used herein, unless otherwise specified or clear from the context, when a range is provided, the upper and lower limits are always included. Ranges provided herein are understood to be abbreviations of all values ​​within the range. For example, a range of 1 to 50 is understood to include any number, combination of numbers, or subrange from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, or 50.

[0076] "Baseline" means a standard or control condition.

[0077] The recitation of a list of chemical groups in any definition of a variable herein includes definition of that variable as any single group or combination of listed groups. The recitation of an embodiment of a variable or aspect herein includes that embodiment as any single embodiment or in combination with any other embodiment or portion thereof. DETAILED DESCRIPTION OF THE INVENTION

[0078] In a first aspect, the present invention provides a compound of formula (I) [ka] (In the formula, R 1 is selected from a hydrogen atom, a halogen atom, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from a hydrogen atom and a halogen atom; R 3 teeth C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C9-cycloalkyl groups optionally substituted by hydroxy groups, C5-C9-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, -S-, -S(O)-, S(O)2 and -NR 9 - is a 3- to 9-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from In some cases, -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -CH2-O-, -NR 9 -CH2- and -CH2-NR 9 - further comprising a bridging group selected from: optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-haloalkyl group; C1-C3-alkoxy groups; C1-C3-haloalkoxy group; C(O)NR 5 R 6 Groups and NR 5 R 6 basis a 3- to 9-membered heterocycloalkyl group independently selected from Partially unsaturated, 5- to 9-membered heterocycloalkyl groups optionally substituted with 1, 2, or 3 substituents, each of which may be an oxo group (=O), a C1-C3-alkyl group, or -C(O)R 5 R 6 groups and halogen atoms), aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group and NR5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group or an NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and N.R. 7 R 8 basis Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom, a C1-C6-alkyl group, a -C1-C5-alkylene-O-C1-C5-alkyl group, a -C1-C5-alkylene-S-C1-C5-alkyl group, a C3-C6-cycloalkyl group and a C3-C5-heterocycloalkyl group; R 7 / R 8 teeth Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl group, which is optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, C(O)NR 5 R 6 group, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally substituted by 1 or 2 substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; 3- to 7-membered heterocycloalkyl groups, which themselves are optionally substituted with C1-C3-alkyl or oxo (=O) groups heteroaryl groups which themselves are optionally substituted by C1-C3-alkyl groups; (independently selected from -C1-C5-alkylene-O-C1-C5-alkyl group, -C1-C5-alkylene-S-C1-C5-alkyl group, -C1~C5-Alkylene-NR 5 -C1 to C5 alkyl group, C3-C6-cycloalkyl groups optionally substituted by hydroxy groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond. or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

[0079] The present invention is further based, at least in part, on the discovery that compounds of formula (I) are PDE3A- or PDE3B-SLFN12 complex modulators.

[0080] Thus, in a further embodiment, the present invention further provides a method for selecting a subject having cancer that responds to a PDE3A- or PDE3B-SLFN12 complex modulator, particularly a compound of formula (I), comprising the step of detecting co-expression of PDE3A and / or PDE3B and Schlafen12 (SLFN12) polypeptides or polynucleotides in cancer cells derived from the subject.

[0081] In a further embodiment, the present invention provides a method for determining that expression of a CREB3L1 or SLFN12 polynucleotide or polypeptide is reduced or undetectable in cancer cells that have acquired resistance to PDE3A- and / or PDE3B-SLFN12 complex modulators, to prevent ineffective treatment with compounds of formula (I).

[0082] Therefore, the present invention provides - identifying a subject with a malignant tumor that may respond to PDE3A and / or PDE3B-SLF12 complex modulator treatment, in particular treatment with a compound of formula (I), based on the levels of PDE3A and / or PDE3B and SLFN12 expression in a biological sample from the subject containing cancer cells; - administering an effective amount of a compound of formula (I).

[0083] In certain embodiments, the present invention provides a method for producing a pharmaceutical composition comprising: - identifying a subject with a malignancy resistant to PDE3A and / or PDE3B-SLF12 complex modulator treatment, particularly treatment with a compound of formula (I), based on a loss or reduction in the level of CREB3L1 or SLFN12 expression relative to a reference; - thereafter excluding those subjects from the envisaged treatment schedule with the compound of formula (I).

[0084] Compound Forms and Salts The compounds of formula (I) can exist in free form, for example as a free base or free acid or zwitterion, or in salt form, which can be any salt, either organic or inorganic addition salt, particularly any pharmaceutically acceptable organic or inorganic addition salt customarily used in pharmacy or used, for example, to isolate or purify the compounds of the invention.

[0085] Salts can be formed, for example, between an anion and a positively charged substituent (e.g., amino) on the compounds described herein. Suitable anions include chloride, bromide, iodide, sulfate, nitrate, phosphate, citrate, methanesulfonate, trifluoroacetate, and acetate. Similarly, salts can be formed between a cation and a negatively charged substituent (e.g., carboxylate) on the compounds described herein. Suitable cations include sodium, potassium, magnesium, calcium, and ammonium cations (such as tetramethylammonium). Examples of prodrugs include C-substituted carboxylic acid groups that can provide active compounds upon administration to a subject. 1~6 Alkyl esters are included.

[0086] Suitable pharmaceutically acceptable salts of the compounds of the present invention include, for example, acid addition salts of compounds of the present invention that are sufficiently basic and have a nitrogen atom in the chain or in the ring, for example, acid addition salts with inorganic or "mineral acids" such as hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, sulfamic acid, bisulfuric acid, phosphoric acid or nitric acid, or organic acids such as formic acid, acetic acid, acetoacetic acid, pyruvic acid, trifluoroacetic acid, propionic acid, butyric acid, hexanoic acid, heptanoic acid, undecanoic acid, lauric acid, benzoic acid, salicylic acid, 2-(4-hydroxybenzoyl)-benzoic acid, camphoric acid, cinnamic acid, cyclopentanepropionic acid, digluconic acid, 3-hydroxy-2-naphthoic acid, nicotinic acid , pamoic acid, pectinic acid, 3-phenylpropionic acid, pivalic acid, 2-hydroxyethanesulfonic acid, itaconic acid, trifluoromethanesulfonic acid, dodecylsulfuric acid, ethanesulfonic acid, benzenesulfonic acid, para-toluenesulfonic acid, methanesulfonic acid, 2-naphthalenesulfonic acid, naphthalenedisulfonic acid, camphorsulfonic acid, citric acid, tartaric acid, stearic acid, lactic acid, oxalic acid, malonic acid, succinic acid, malic acid, adipic acid, alginic acid, maleic acid, fumaric acid, D-gluconic acid, mandelic acid, ascorbic acid, glucoheptanoic acid, glycerophosphate, aspartic acid, sulfosalicylic acid or thiocyanic acid.

[0087] Further examples of suitable acid salts include acetate, adipate, alginate, aspartate, benzoate, benzenesulfonate, bisulfate, butyrate, citrate, camphorate, camphorsulfonate, digluconate, dodecyl sulfate, ethanesulfonate, formate, fumarate, glucoheptanoate, glycolate, hemisulfate, heptanoate, hexanoate, hydrochloride, hydrobromide, hydroiodide, 2-hydroxyethanesulfonate, lactate, maleate, malonate, methanesulfonate, 2-naphthalenesulfonate, nicotinate, nitrate, palmoate, pectinate, persulfate, 3-phenylpropionate, phosphate, picrate, pivalate, propionate, salicylate, succinate, sulfate, tartrate, thiocyanate, tosylate, and undecanoate salts. Other acids, such as oxalic acid, which are not themselves pharmaceutically acceptable, can be used in the preparation of salts useful as intermediates in obtaining the compounds of the present invention and their pharmaceutically acceptable acid addition salts.

[0088] Further suitable pharmaceutically acceptable salts of compounds of formula (I) that are sufficiently acidic are alkali metal salts, such as sodium or potassium salts, alkaline earth metal salts, such as calcium, magnesium or strontium salts, or aluminum or zinc salts, or ammonia or organic primary, secondary or tertiary amines having 1 to 20 carbon atoms, such as ethylamine, diethylamine, triethylamine, ethyldiisopropylamine, monoethanolamine, diethanolamine, triethanolamine, dicyclohexylamine, dimethylaminoethanol, diethylaminoethanol, tris(hydroxymethyl)aminomethane, procaine, dibenzylamine, N-methylmorpholine, , arginine, lysine, 1,2-ethylenediamine, N-methylpiperidine, N-methyl-glucamine, N,N-dimethyl-glucamine, N-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 quaternary ammonium ion having 1 to 20 carbon atoms, such as tetramethylammonium, tetraethylammonium, tetra(n-propyl)ammonium, tetra(n-butyl)ammonium, N-benzyl-N,N,N-trimethylammonium, choline or benzalkonium.

[0089] In certain embodiments, salts derived from appropriate bases include alkali metal (e.g., sodium), alkaline earth metal (e.g., magnesium), ammonium, and N-(alkyl)4 + Salts are included. The present invention also contemplates the quaternization of any basic nitrogen-containing groups of the compounds disclosed herein. Such quaternization may result in water- or oil-soluble or dispersible products. Salt forms of any compounds of the formulas herein may be amino acid salts of carboxyl groups (e.g., L-arginine, -lysine, -histidine salts).

[0090] Lists of suitable salts are found in Remington's Pharmaceutical Sciences, 17th ed., Mack Publishing Company, Easton, Pa., 1985, p. 1418; Journal of Pharmaceutical Science, 66, 2 (1977); and Pharmaceutical Salts: Properties, Selection, and Use A Handbook; Wermuth, C.G. and Stahl, P.H. (eds.) Verlag Helvetica Chimica Acta, Zurich, 2002 [ISBN 3-906390-26-8], each of which is incorporated herein by reference in its entirety.

[0091] Those skilled in the art will further recognize that acid addition salts of the claimed compounds can be prepared by reacting the compounds with the appropriate inorganic or organic acid via any of several known methods. Alternatively, alkali and alkaline earth metal salts of acidic compounds of the invention are prepared by reacting the compounds of the invention with the appropriate base via a variety of known methods.

[0092] The present invention includes all possible salts of the compounds of the present invention, either as a single salt or as any mixture of salts in any ratio.

[0093] The neutral forms of the compounds can be regenerated by contacting the salt with a base or acid and isolating the parent compound in the conventional manner. The parent form of the compound differs from the various salt forms in certain physical properties, such as solubility in polar solvents, but otherwise the salts are equivalent to the parent form of the compound for purposes of the present invention.

[0094] When compounds are referred to herein, particularly in the experimental section, for the synthesis of intermediates and examples of the present invention as salt forms with the corresponding bases or acids, the exact stoichiometry of the salt forms obtained by each preparation and / or purification step is in most cases unknown.

[0095] Unless otherwise specified, for example, "hydrochloride", "trifluoroacetate", "sodium salt" or "xHCl", "xCF3COOH", "xNa + A suffix to a chemical name or structural formula for a salt, such as "," denotes the salt form, and does not specify the stoichiometry of the salt form.

[0096] This also applies if synthetic intermediates or example compounds or salts thereof are obtained by the preparation and / or purification process as solvates, such as hydrates of unknown stoichiometric composition (if defined).

[0097] In addition to salt forms, the present invention provides compounds in prodrug form. Prodrugs of the compounds described herein are compounds that undergo chemical changes under physiological conditions to provide the compounds of the present invention. Furthermore, prodrugs can be converted to the compounds of the present invention by chemical or biochemical methods in an ex vivo environment. For example, prodrugs can be slowly converted to the compounds of the present invention when placed in a transdermal patch reservoir with a suitable enzyme or chemical reagent. Prodrugs are often useful because, in some situations, they may be easier to administer than the parent drug. They may, for example, be more bioavailable by oral administration than the parent drug. Prodrugs may also have improved solubility in pharmacological compositions over the parent drug. A wide variety of prodrug derivatives are known in the art, such as those derived from hydrolytic cleavage or oxidative activation of the prodrug. A non-limiting example of a prodrug would be a compound of the present invention that is administered as an ester (the "prodrug"), but is then metabolically hydrolyzed to the carboxylic acid, the active agent. Further examples include peptidyl derivatives of the compounds of the present invention.

[0098] The compounds of the present invention can exist as hydrates or solvates, and for example, the compounds of the present invention contain polar solvents, particularly water, methanol, or ethanol, as structural elements of the crystal lattice of the compounds. The amount of polar solvent, particularly water, can be stoichiometric or non-stoichiometric. In the case of stoichiometric solvates, for example, hydrates, hemi-, (semi-), mono-, sesqui-, di-, tri-, tetra-, penta-isosolvates, or hydrates are possible. The present invention includes all such hydrates or solvates.

[0099] The present invention also includes various hydrate and solvate forms of the compounds.

[0100] The compounds of the present invention may also contain unnatural proportions of atomic isotopes at one or more of the atoms that constitute such compounds. For example, the compounds may contain unnatural proportions of atomic isotopes, such as tritium ( 3 H), iodine-125( 125 I) or carbon-14 ( 14 The compounds of formula (I) may be radiolabeled with a radioactive isotope, such as C. All isotopic variations of the compounds of the present invention, whether radioactive or not, are intended to be encompassed within the scope of the present invention. In particular, compounds of formula (I) containing deuterium. [ka]

[0101] Formula (Ia) may include a compound in position D in which any of the hydrogen atoms may be replaced by a deuterium atom. 1 , D 2 , D 3 and D 4 Furthermore, residue R 1 ~R 4 In R, such an exchange may be possible if these residues contain heteroatom-H or carbon-H bonds available for chemical reaction. To obtain heteroatom-D or carbon-D bonds, hydrogen atoms can be replaced with deuterium atoms using methods known to those skilled in the art. 1 , R 2 or R 4Any of the groups themselves can be deuterium instead of hydrogen.

[0102] Thus, one aspect of the present invention is to provide a compound comprising independently R 1 , R 2 Or R 4 is deuterium, and / or any of the hydrogen atoms shown in formula (I) is replaced by a deuterium atom, and / or R 1 , R 2 , R 3 Or R 4 are compounds having deuterium atoms at any combination of chemically accessible positions or simultaneously deuterated positions.

[0103] The term "isotopic variant" of a compound or reagent is defined as a compound exhibiting an unnatural ratio of one or more isotopes comprising such compound. The term "isotopic variant of a compound of general formula (I)" is defined as a compound of general formula (I) exhibiting an unnatural ratio of one or more isotopes comprising such compound. The term "unnatural ratio" means a ratio of such isotope that is higher than its natural abundance. The natural abundance of isotopes as applied in this context is described in "Isotopic Compositions of the Elements 1997", Pure Appl. Chem., 70(1), 217-235, 1998. Examples of such isotopes include stable radioactive isotopes of hydrogen, carbon, nitrogen, oxygen, phosphorus, sulfur, fluorine, chlorine, bromine, and iodine, e.g., 2 H (deuterium), 3 H (tritium), 11 C. 13 C. 14 C. 15 N, 17 O. 18 O. 32 P, 33 P, 33 S, 34 S, 35 S, 36 S, 18 F, 36 Cl, 82 Br,123 I, 124 I, 125 I, 129 I and 131 I can be mentioned.

[0104] For the treatment and / or prevention of the diseases specified herein, one or more isotopic variants of the compounds of general formula (I) may contain deuterium ("deuterium-containing compounds of general formula (I)"). One or more radioactive isotopes, e.g. 3 H or 14 Isotopic variations of compounds of general formula (I), such as those incorporating C, are useful, for example, in drug and / or substrate tissue distribution studies. These isotopes are particularly preferred for their ease of incorporation and detectability. 18 F or 11 Positron-emitting isotopes such as C can be incorporated into the compounds of general formula (I). These isotopic variants of the compounds of general formula (I) are useful for in vivo imaging applications. Deuterium-containing and 13 C-containing compounds can be used in mass spectrometry in preclinical or clinical research settings.

[0105] Isotopic variants of compounds of general formula (I) can generally be prepared by methods known to those skilled in the art, such as those described in the schemes and / or examples herein, by substituting a reagent, preferably a deuterium-containing reagent, for the isotopic variant. Depending on the desired location of deuteration, in some cases, the deuterium from DO can be incorporated directly into the compound or into a reagent useful for synthesizing such a compound. Deuterium gas is also a useful reagent for incorporating deuterium into molecules. Catalytic deuteration of olefinic and acetylenic bonds is a direct route for the incorporation of deuterium. Metal catalysts (i.e., Pd, Pt, and Rh) can be used to directly exchange deuterium for hydrogen in hydrocarbon-containing functional groups in the presence of deuterium gas. A variety of deuterated reagents and synthetic building blocks are commercially available from companies such as, for example, C / D / N Isotopes, Quebec, Canada; Cambridge Isotope Laboratories Inc., Andover, MA, USA; and CombiPhos Catalysts, Inc., Princeton, NJ, USA.

[0106] The term "deuterium-containing compound of general formula (I)" is defined as a compound of general formula (I) in which one or more hydrogen atoms have been replaced by one or more deuterium atoms, and the abundance of deuterium at each deuterated position of the compound of general formula (I) is greater than the natural abundance of deuterium, which is about 0.015%. In particular, in a deuterium-containing compound of general formula (I), the abundance of deuterium at each deuterated position of the compound of general formula (I) is greater than 10%, 20%, 30%, 40%, 50%, 60%, 70%, or 80% at one or more positions, preferably greater than 90%, 95%, 96%, or 97%, and even more preferably greater than 98% or 99%. It is understood that the abundance of deuterium at each deuterated position is independent of the abundance of deuterium at one or more other deuterated positions.

[0107] Selective incorporation of one or more deuterium atoms into compounds of general formula (I) can alter the physicochemical properties (e.g., acidity [CL Perrin et al., J. Am. Chem. Soc., 2007, 129, 4490], basicity [CL Perrin et al., J. Am. Chem. Soc., 2005, 127, 9641], lipophilicity [B. Testa et al., Int. J. Pharm., 1984, 19(3), 271]) and / or metabolic profile of the molecule, resulting in a change in the ratio of parent compound to metabolites or the amount of metabolites formed. Such changes may result in certain therapeutic advantages and may therefore be desirable in some situations. Decreased rates of metabolism and metabolic switching, with altered metabolite ratios, have been reported (AEMutlib et al., Toxicol. Appl. Pharmacol., 2000, 169, 102). These changes in exposure to the parent drug and metabolites can have important consequences for the pharmacokinetics, tolerability, and efficacy of deuterium-containing compounds of general formula (I). In some instances, deuterium substitution reduces or eliminates the formation of undesirable or toxic metabolites and enhances the formation of desirable metabolites (e.g., Nevirapine: AM Sharma et al., Chem. Res. Toxicol., 2013, 26, 410; Efavirenz: AEMutlib et al., Toxicol. Appl. Pharmacol., 2000, 169, 102). In other instances, the primary effect of deuteration is to decrease the rate of systemic clearance. As a result, the biological half-life of the compound increases. Potential clinical benefits would include the ability to maintain similar systemic exposure with reduced peak and increased trough levels. This may result in reduced side effects and enhanced efficacy, depending on the pharmacokinetic / pharmacodynamic relationship of a particular compound. ML-337 (CJ Wenthur et al., J. Med. Chem., 2013, 56, 5208) and odanacatib (K. Kassahun et al., WO 2012 / 112363) are examples of this deuterium effect.Still other cases have been reported in which a decreased rate of metabolism resulted in increased drug exposure without altering the rate of systemic clearance (e.g., rofecoxib: F. Schneider et al., Arzneim. Forsch. / Drug. Res., 2006, 56, 295; telaprevir: F. Maltais et al., J. Med. Chem., 2009, 52, 7993). Deuterated drugs that exhibit this effect may result in reduced dosing requirements (e.g., fewer doses or lower dosages to achieve the desired effect) and / or may result in reduced amounts of metabolites.

[0108] A compound of general formula (I) may have multiple potential metabolic attack sites. To optimize the above effects on physicochemical properties and metabolic profiles, a deuterium-containing compound of general formula (I) can be selected that has one or more specific patterns of deuterium-hydrogen exchange. In particular, one or more deuterium atoms of one or more deuterium-containing compounds of general formula (I) are bonded to carbon atoms and / or located at positions of the compound of general formula (I).

[0109] In some embodiments, the compound of formula (I) may be an isomer. "Isomers" are different compounds that have the same molecular formula. "Stereoisomers" are isomers that differ only in the way the atoms are arranged in space. As used herein, the term "isomer" includes any and all geometric and stereoisomers. For example, "isomers" include geometric double bond cis- and trans-isomers, also referred to as E-isomers and Z-isomers; R- and S-enantiomers; diastereomers, (d)-isomers and (l)-isomers, racemic mixtures thereof; and other mixtures thereof, as falling within the scope of the present invention.

[0110] symbol -----indicates a bond that may be a single bond or a double bond as described herein. Provided herein are various geometric isomers and mixtures thereof resulting from the arrangement of substituents around a carbon-carbon double bond or the arrangement of substituents around a carbon ring. Substituents around a carbon-carbon double bond are designated as being in the "Z" or "E" configuration, and the terms "Z" and "E" are used according to IUPAC standards. Unless otherwise specified, structures depicting double bonds encompass both the "E" and "Z" isomers.

[0111] Alternatively, substituents around a carbon-carbon double bond can be designated "cis" or "trans," with "cis" referring to substituents on the same side of the double bond and "trans" referring to substituents on opposite sides of the double bond. The arrangement of substituents around a carbocyclic ring can also be designated "cis" or "trans," with the term "cis" referring to substituents on the same side of the plane of the ring and the term "trans" referring to substituents on opposite sides of the plane of the ring. A mixture of compounds in which substituents are located on both the same and opposite sides of the plane of the ring is designated "cis / trans."

[0112] The compounds of the present invention optionally contain one or more asymmetric centers, e.g., carbon atoms bearing four different substituents, depending on the location and nature of the various desired substituents. It is possible for one or more asymmetric carbon atoms to be present in either the (R) or (S) configuration, resulting in a racemic mixture in the case of a single asymmetric center, or a diastereomeric mixture in the case of multiple asymmetric centers. The term "(±)" is used to indicate a racemic mixture where appropriate. In certain instances, asymmetry may exist due to restricted rotation about a given bond, e.g., the central bond joining two substituted aromatic rings in a specified compound. When a compound is an enantiomer, the stereochemistry at each chiral carbon can be designated as either (R) or (S). Resolved compounds of unknown absolute configuration can be designated (+) or (-) depending on the direction (dextrorotatory or levorotatory) they rotate plane-polarized light at the wavelength of the sodium D line. Some of the compounds described herein contain one or more asymmetric centers and can therefore give rise to enantiomers, diastereomers, and other stereoisomeric forms that can be defined as (R)- or (S)- in terms of the absolute stereochemistry at each asymmetric atom. The present chemical compounds, pharmaceutical compositions, and methods are meant to include all such possible isomers, including racemic mixtures, optically substantially pure forms, and intermediate mixtures.

[0113] Preferred compounds are those that provide the more desirable biological activity. Separate, pure or partially purified isomers and stereoisomers, or racemic or diastereomeric mixtures, of the compounds of the invention are also within the scope of the invention. The purification and separation of such materials can be achieved by standard techniques known in the art, including chiral high-pressure liquid chromatography (HPLC), formation and crystallization of chiral salts, or can be prepared by asymmetric synthesis.

[0114] Optical isomers can be obtained by conventional resolution of racemic mixtures, for example, by the formation of diastereomeric salts or covalent diastereomers with optically active acids or bases. Examples of suitable acids include tartaric acid, diacetyltartaric acid, ditoluoyltartaric acid, and camphorsulfonic acid. Diastereoisomeric mixtures can be separated into individual diastereomers based on their physical and / or chemical differences by methods known in the art, for example, chromatography or fractional crystallization. The optically active base or acid is then liberated from the separated diastereomeric salts. Another method for separating optical isomers involves the use of chiral chromatography (e.g., an HPLC column using a chiral phase), with or without conventional derivatization, which may be selected to maximize the separation of the enantiomers. Suitable HPLC columns using chiral phases are commercially available, for example, those manufactured by Daicel, among others, such as Chiracel OD and Chiracel OJ, all of which are routinely selectable. Enzymatic separations, with or without derivatization, are also useful. The optically active compounds of this invention can also be obtained by chiral syntheses utilizing optically active starting materials.

[0115] To distinguish different types of isomers from one another, reference is made to IUPAC Rules Section E (Pure Appl Chem 45, 11-30, 1976).

[0116] The present invention includes all possible stereoisomers of the compounds of the present invention, either as single stereoisomers or as any mixture of stereoisomers in any ratio, e.g., (R)- or (S)-isomers. The stereoisomer that exhibits the desired effect is preferred. 4 In the case of compounds of formula (I) where = methyl, it has been discovered that compounds with the methyl group in the S configuration have significantly superior pharmacological effects.

[0117] Therefore, R 4 In one aspect of the present invention relating to the arrangement of the alkyl group in R 4=C1-C3-alkyl, more specifically R 4 = Including compounds of formula (Ia) in which the methyl is in the S configuration. [ka]

[0118] Isolation of a single stereoisomer, for example a single enantiomer or a single diastereomer, of a compound of the invention is achieved by any suitable prior art method, such as chromatography, in particular chiral chromatography.

[0119] Furthermore, it is possible for compounds of the present invention to exist as tautomers. For example, any compound of the present invention that includes an imidazopyridine moiety as a heteroaryl group can exist, for example, as a 1H tautomer or a 3H tautomer, or a mixture of any amount of the two tautomers, i.e.: [ka]

[0120] The present invention includes all possible tautomers of the compounds of the present invention as single tautomers or any mixture of tautomers in any ratio.

[0121] Additionally, the compounds of the present invention can potentially exist as N-oxides, which are defined in that at least one nitrogen in the compounds of the present invention is oxidized, and the present invention includes all such chemically possible N-oxides.

[0122] Furthermore, the present invention includes all possible crystalline forms or polymorphs of the compounds of the present invention, either as a single polymorph or as a mixture of two or more polymorphs in any ratio.

[0123] Furthermore, the present invention also includes prodrugs of the compounds according to the present invention. The term "prodrug" as used herein refers to a compound that may itself be biologically active or inactive, but that is converted (e.g., metabolically or hydrolytically) into a compound according to the present invention during its residence in the body.

[0124] Thus, the present invention includes prodrugs of compounds of formula (I).

[0125] In yet another embodiment, the present invention includes stereoisomers, tautomers, N-oxides, hydrates, solvates or salts of compounds of formula (I), or mixtures thereof.

[0126] In another embodiment, the present invention includes a stereoisomer, tautomer, hydrate, solvate or salt of a compound of formula (I), or a mixture thereof.

[0127] In a further embodiment, the present invention includes stereoisomers, tautomers, solvates or salts of compounds of formula (I), or mixtures thereof.

[0128] In still further embodiments, the present invention includes stereoisomers, tautomers, solvates or salts of compounds of formula (I), or mixtures thereof.

[0129] In yet another embodiment, the present invention includes stereoisomers, tautomers or salts of compounds of formula (I), or mixtures thereof.

[0130] Further Aspects and Embodiments According to an embodiment of the first aspect, the present invention provides a method for manufacturing a semiconductor device comprising: R 1 is selected from a hydrogen atom, a halogen atom, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, S(O)2 and -NR 9 - is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; C(O)NR 5 R 6 Groups and NR 5 R 6 basis a 3- to 7-membered heterocycloalkyl group independently selected from Partially unsaturated, optionally C1-C3-alkyl groups, -C(O)R 5 R 6 -O-, -S- and -NR- substituted with a substituent selected from a group and a halogen atom 9 -, an aryl group optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, and a NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, cyano groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 base Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, C(O)NR 5 R 6 group, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 3- to 7-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C7-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0131] According to an embodiment of the first aspect, the present invention provides a method for manufacturing a semiconductor device comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl group, -O- and -NR 9 - is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; and C(O)NR 5 R 6 base a 3- to 7-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms;9 a 5- to 7-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group: and N.R. 7 R 8 groups (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9a 3- to 7-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C7-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0132] According to an embodiment of the first aspect, the present invention provides a method for manufacturing a semiconductor device comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C4-C6-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl group, -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; a 3- to 6-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 a 5- to 6-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with one or two substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group: and N.R. 7 R 8 groups (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, hydroxy groups, C1-C3-alkoxy group, C3-C6-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 4- to 6-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted with hydroxy groups or C1-C3-alkyl groups a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0133] According to an embodiment of the first aspect, the present invention provides compounds of general formula (I): [ka] (In the formula, R 1 is selected from a hydrogen atom, a halogen atom, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from a hydrogen atom and a halogen atom; R 3 is a halogen atom, C2-C6-alkenyl group, C3-C6-cycloalkyl group, C5-C6-cycloalkenyl group, C3-C7-heterocycloalkyl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom and a C1-C3-alkyl group, a hydroxy group, NR 5 R 6 group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group), partially unsaturated, optionally substituted C5-C7-heterocycloalkyl groups with 1, 2 or 3 substituents, each of which is independently selected from an oxo group (=O), a C1-C3-alkyl group and a halogen atom; aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group or an NR 5 R 6 independently selected from the group and N.R. 7 R 8 base is selected from R 4 is selected from a hydrogen atom and a C1-C3 alkyl group, R 5 / R 6 are independently selected from a hydrogen atom, a C1-C6-alkyl group, a -C1-C5-alkylene-O-C1-C5-alkyl group, a -C1-C5-alkylene-S-C1-C5-alkyl group, a C3-C6-cycloalkyl group and a C3-C5-heterocycloalkyl group, R 7 / R 8 represents a hydrogen atom and a C1-C6-alkyl group, -C1-C5-alkylene-O-C1-C5-alkyl group, -C1-C5-alkylene-S-C1-C5-alkyl group, -C1-C5-alkylene-NR5 independently selected from C1-C5-alkyl groups, C3-C6-cycloalkyl groups, and C3-C5-heterocycloalkyl groups; Or R 7 and R 8 together optionally represent -O-, -S- and -NR 9 -, containing 1 or 2 additional heteroatoms selected from the group consisting of optionally halogen atoms, C1-C3 alkyl groups, hydroxy groups, cyano groups, oxo groups (=O) and NR 5 R 6 forming a 3-, 4-, 5-, 6- or 7-membered ring substituted once, twice or three times with substituents selected from the group R 7 and R 8 taken together to form a 5-, 6-, or 7-membered ring, the ring may optionally be joined with -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -NR 9 -CH2-; R 9 is a hydrogen atom or a C1-C3 alkyl group. or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

[0134] According to an embodiment of the first aspect, the present invention provides a method for manufacturing a semiconductor device comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, and a C1-C3 haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but halogen atoms, C2-C4-alkenyl group, C5-C6-cycloalkenyl group, C3-C6-heterocycloalkyl groups optionally substituted by one or two substituents, each substituent being independently selected from halogen atoms and C1-C3-alkyl groups; partially unsaturated, optionally substituted C5-C6-heterocycloalkyl groups with one or two substituents, each of which is independently selected from an oxo group (=O), a C1-C3-alkyl group and a halogen atom; Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group or an NR 5 R 6 independently selected from the group and N.R. 7 R 8 base Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom, a C1-C6-alkyl group, a -C1-C3-alkylene-O-C1-C3-alkyl group, a -C1-C3-alkylene-S-C1-C3-alkyl group and a C3-C5-heterocycloalkyl group, R 7 / R 8 is a hydrogen atom and a C1-C6-alkyl group, -C1-C3-alkylene-O-C1-C3-alkyl group, -C1-C3-alkylene-S-C1-C3-alkyl group, -C1-C3-alkylene-NR 5 -independently selected from C1-C3-alkyl groups, C3-C6-cycloalkyl groups, and C3-C5-heterocycloalkyl groups, or R 7 and R 8 together, optionally -O-, -S- and -NR 9 -, containing 1 or 2 additional heteroatoms selected from the group consisting of optionally halogen atoms, C1-C3 alkyl groups, hydroxy groups, cyano groups, oxo groups (=O) and NR 5 R 6 forming a 3-, 4-, 5-, 6- or 7-membered ring substituted once, twice or three times with substituents selected from the group R 9 is a hydrogen atom or a C1-C3 alkyl group, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0135] According to a second embodiment of the first aspect, the present invention provides a method for manufacturing a semiconductor device comprising: R 1 is selected from halogen atoms, C1-C3-alkyl groups and C1-C3-haloalkyl groups; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but halogen atoms, C2-C4-alkenyl group, C5-C6-cycloalkenyl group, C3-C6-heterocycloalkyl groups optionally substituted by one or two substituents, each substituent being independently selected from halogen atoms and C1-C3-alkyl groups; partially unsaturated C5-C6-heterocycloalkyl groups optionally substituted with an oxo group (=O); Phenyl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group or an NR 5 R 6 independently selected from the group and N.R. 7R 8 basis Selected from; R 4 is selected from a hydrogen atom and a methyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C3 alkyl group; R 7 / R 8 are independently selected from a hydrogen atom, a C3-C5-cycloalkyl group and a C1-C6-alkyl group; Or R 7 and R 8 together optionally containing one additional oxygen atom, forming a 4-, 5- or 6-membered ring, optionally substituted once or twice with substituents selected from halogen atoms and C1-C3-alkyl groups, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0136] According to a third embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from CF3, -CH3, -OCF3 and a fluorine atom; R 2 is selected from hydrogen atoms; R 3 but halogen atoms, C2-C4-alkenyl group, C5-C6-cycloalkenyl group, C3-C6-heterocycloalkyl groups optionally substituted by one or two substituents, each substituent being independently selected from halogen atoms and C1-C3-alkyl groups; partially unsaturated C5-C6-heterocycloalkyl groups optionally substituted with an oxo group (=O); Phenyl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group or an NR 5 R 6 independently selected from the group and N.R. 7 R 8 basis Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C3 alkyl group; R 7 / R 8 are independently selected from a hydrogen atom and a C1-C6-alkyl group; Or R 7 and R 8 together optionally containing one additional oxygen atom, forming a 4-, 5- or 6-membered ring, optionally substituted once or twice with substituents selected from halogen atoms and C1-C3-alkyl groups, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0137] According to a fourth embodiment of the first aspect, the present invention provides a method for manufacturing a semiconductor device comprising: R 1 is selected from CF3, -CH3, -OCF3 and a fluorine atom; R 2 is selected from hydrogen atoms, R 3 but halogen atoms, a prop-1-en-1-yl group optionally substituted by a methyl group; a piperidin-1-yl group optionally substituted with one or two substituents, each substituent independently selected from a fluorine atom and a methyl group; a morpholin-4-yl group optionally substituted by one or two methyl groups; a pyrrolidin-1-yl group optionally substituted by one or two halogen atoms, a 1,2,3,6-tetrahydropyridin-4-yl group optionally substituted by a methyl group; adithidin-1-yl group, 3,6-dihydro-1H-pyran-4-yl group, a 6-oxo-1,6-dihydropyridin-3-yl group optionally substituted with one or two substituents, each substituent independently selected from a hydrogen atom and a methyl group; cyclopent-1-en-1-yl group, a phenyl group optionally substituted with 1, 2 or 3 substituents, each independently selected from halogen atoms, hydroxy groups, methyl groups, ethyl groups, CF3, CF2H groups, methoxy groups, CF3O groups, NH2 groups and NHCH3 groups; a 2H-pyrrol-1-yl group optionally substituted with one or two substituents, each independently selected from a hydrogen atom, a cyano group, and a methyl group; a 1H-pyrazol-4-yl group optionally substituted with one or two substituents, each independently selected from a methyl group, an ethyl group, or a CF group; a 1H-pyrazol-5-yl group optionally substituted by a methyl group; 1,2-oxazol-4-yl optionally substituted by one or two methyl groups; a 1,2-thiazol-4-yl group optionally substituted by a methyl group; a 1,3-thiazol-5-yl group optionally substituted by a methyl group; pyridin-3-yl, pyridin-4-yl and pyridin-5-yl groups, each of which is optionally substituted with one or two substituents, each of which is independently selected from halogen atoms, methyl groups, CF3 groups, methoxy groups and NH2 groups; a pyrimidin-5-yl group optionally substituted by a methyl group; 1H-indol-6-yl group, a 1H-indazol-6-yl group optionally substituted by a methyl group; a 1H-benzimidazol-6-yl group optionally substituted by a methyl group; NH(C2H5) group, NH(C3H7) group, NH(C4H9) group, NCH3(C4H9) group, NH(C5H 11 ) group, NH (cyclopentyl) group, NCH3 (cyclopentyl) group Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0138] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group and a C1-C3-haloalkyl group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C3-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, a C5-C6-cycloalkenyl group optionally substituted by a hydroxy group; -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally substituted with hydroxy groups a 3- to 6-membered heterocycloalkyl group independently selected from: a 5- to 7-membered partially unsaturated heterocycloalkyl group optionally substituted with one or two substituents, each substituent being independently selected from a C1-C3-alkyl group and a halogen atom; aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with one or two substituents, each of which is a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group, and NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and N.R. 7 R 8 basis Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6 alkyl groups which is optionally substituted with 1, 2, 3 or 4 substituents, halogen atoms, cyano and hydroxy groups, C1-C3 alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by 1 or 2 substituents, the substituents being independently selected from C1-C3-alkyl groups, hydroxy groups and C1-C3-hydroxyalkyl groups; 3- to 7-membered heterocycloalkyl groups, which themselves are optionally substituted by C1-C3-alkyl groups Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted by hydroxy groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups and hydroxy groups; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0139] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group and a C1-C3-haloalkyl group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but -O- and -NR 9 -, and A 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, each of which is halogen atoms; hydroxy group C1-C3-alkyl groups optionally further substituted with hydroxy groups are independently selected from an aryl group optionally substituted with one or two substituents, each substituent being independently selected from a halogen atom, a hydroxy group, and a C1-C3-haloalkyl group; optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 base Selected from; R 4 is selected from a hydrogen atom and a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C3 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1 or 2, 3 or 4 substituents, Halogen atoms, hydroxy groups, C1-C3-alkoxy group, C3-C5-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 -, a 5- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted with hydroxy groups or C1-C3-alkyl groups a 4- to 5-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0140] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from CF3 and fluorine atoms; R 2 is a hydrogen atom; R 3 but an aryl group optionally substituted with a substituent selected from a halogen atom and a C1-C3-haloalkyl group, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group and N.R. 7 R 8 basis Selected from; R 4 is selected from a hydrogen atom and a methyl group; R 5 / R 6 is a hydrogen atom or a methyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C3-alkyl groups, which are optionally substituted with 1, 2 or 4 substituents, Halogen atoms, hydroxyl groups, and methoxy groups (independently selected from are independently selected from The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0141] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from a hydrogen atom, a fluorine atom, a cyano group, a methyl group, an OCF3 group, a CHF2 group, and a CF3 group; R 2 is selected from a hydrogen atom or a fluorine atom; R 3 but C1-C6-alkyl groups, which are optionally substituted, the substituents being selected from 2-hydroxy, methoxy and morpholino groups; C2-C6-alkenyl groups optionally substituted by methoxy groups; a cyclohexyl group optionally substituted with a hydroxy group; C5-C7-cycloalkenyl group; a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a fluorine atom, a —C(O)NH2 group, a hydroxy group, a methyl group, an ethyl group, a hydroxymethyl group, a cyano group, and an amino group; partially unsaturated 5- to 6-membered heterocycloalkyl groups optionally substituted with methyl groups; a phenyl group optionally substituted with 1, 2, or 3 substituents, the substituents being independently selected from methyl, ethyl, fluorine, chlorine, amino, hydroxy, methoxy, cyano, difluoromethyl, trifluoromethyl, and methylamino; a 5-membered heteroaryl group optionally substituted with one or two substituents, the substituents being independently selected from methyl, ethyl, trifluoromethyl, difluoromethyl, and cyano; a 6-membered heteroaryl group optionally substituted with one or two substituents, the substituents being independently selected from methyl, fluorine, chlorine, trifluoromethyl, amino, and methoxy; a bicyclic heteroaryl group optionally substituted with a methyl group; NR 7 R 8 basis, (R 7 R 8 is a hydrogen atom, a C1-C6 alkyl group optionally substituted by one or two substituents (the substituents are independently selected from an amino group, a methoxy group, an ethoxy group, a cyano group, a hydroxy group, a trifluoromethyl group, a cyclopropyl group, a 2,2-dimethylcyclopropyl group, a 1-hydroxycyclobutyl group, a 3-hydroxycyclobutyl group, a methyloxetanyl group, an oxolanyl group, an oxanyl group, a methyloxanyl group, a tetrahydrofuranyl group, an oxopyrrolidinyl group, an oxopiperidinyl group, a methyl-1H-imidazolyl group, a 1H-pyrazolyl group, a 1H-imidazolyl group, a 1-methyl-1H-pyrazolyl group, a pyrazinyl group, a pyridinyl group, and a pyrimidinyl group); C5-C7-cycloalkyl groups optionally substituted with hydroxy groups, 4- to 6-membered heterocycloalkyl groups optionally substituted with methyl groups is selected from R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0142] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from a hydrogen atom, a fluorine atom, a cyano group, a CH3 group, an OCF3 group, a CHF2 group, and a CF3 group; R 2 is selected from a hydrogen atom (in many cases) or a fluorine atom; R 3 but Methyl group, propan-2-yl group, 2-methylpropyl group, 2-hydroxypropan-2-yl group, 3,3-dimethylbutyl group, 3-methoxypropyl group, a —CH2-(morpholin-4-yl) group, prop-1-en-2-yl group, 2-methylprop-1-en-1-yl group, 3,3-dimethylbut-1-en-1-yl group, 3-methoxyprop-1-en-1-yl group, 4-hydroxycyclohexyl group, Cyclopent-1-en-1-yl group, cyclohex-1-en-1-yl group, bicyclo[2.2.1]hept-2-en-2-yl group Oxan-3-yl group, 3,3-difluoroazetidin-1-yl group, azetidine-3-carboxamide, 2-hydroxyazetidin-1-yl group, 3-hydroxy-3-methylazetidin-1-yl group, 2-(hydroxymethyl)azetidin-1-yl group, 3-cyano-3-methylazetidin-1-yl group, 2,4-dimethylazetidin-1-yl group, -2λ6-thia-6-azaspiro[3.3]heptane-2,2-dione group, 3-hydroxypyrrolidin-1-yl group, 3,3-difluoropyrrolidin-1-yl group, 3-azabicyclo[3.1.0]hexan-3-yl group, 1 -amino-3-azabicyclo[3.1.0]hexan-3-yl group, 4-fluoropiperidin-1-yl group, 4,4-fluoropiperidin-1-yl group, 4-cyanopiperidin-1-yl group, 4-fluoro-4-methylpiperidin-1-yl group, 4-ethyl-4-hydroxypiperidin-1-yl group, 4-hydroxypiperidin-1-yl group, 3-hydroxypiperidin-1-yl group, 3-aminocarbonylpiperidin-1-yl group, morpholin-4-yl group, 2-methylmorpholin-4-yl group, 2,6-dimethylmorpholin-4-yl group, 4-methylpiperazin-1-yl group, 2,5-dihydrofuran-3-yl group, 5,6-dihydro-2H-pyran-3-yl group, 3,6-dihydro-2H-pyran-4-yl group, 1,2,3,6-tetrahydropyridin-4-yl group, 1-methyl-1,2,3,6-tetrahydropyridin-4-yl group, 6-oxo-1,6-dihydropyridin-3-yl group, phenyl group, 2-methylphenyl group, 2-ethylphenyl group, 2-fluorophenyl group, 2-aminophenyl group, 2-hydroxyphenyl group, 2-methoxyphenyl group nyl group, 2,4-dimethylphenyl group, 2-fluoro-4-methylphenyl group, 2-fluoro-4-aminophenyl group, 4-cyano-2-methylphenyl group, 2-chloro-4-fluorophenyl group, 2,3-difluorophenyl group, 2-fluoro-3-aminophenyl group, 2,5-difluorophenyl group, 2,6-difluorophenyl group, 4-fluoro-6-methylphenyl group, (2-difluoromethyl)phenyl group, 2-cyanophenyl group, 2,4-difluorophenyl group, 3 -methylphenyl group, 3-aminophenyl group, 3-fluorophenyl group, 3-hydroxyphenyl group, 3,4-difluorophenyl group, 3-amino-4-methylphenyl group, 3-amino-4-chlorophenyl group, 3-amino-4-fluorophenyl group, 3-fluoro-4-methylphenyl group, 4-amino-3-fluorophenyl group, 4-fluoro-3-methylphenyl group, 4-fluoro-3-hydroxyphenyl group, 3-hydroxy-4-methylphenyl group, 4-methylphenyl group, 4-fluorophenyl group, 4-chlorophenyl group, 4-(difluoromethyl)phenyl group, 4-(trifluoromethyl)phenyl group, 4-cyanophenyl group, 4-aminophenyl group, 4-(methylamino)phenyl group, 4-hydroxyphenyl group, 4-methoxyphenyl group, 3,5-difluorophenyl group, 2,4,5-trifluorophenyl group, 2,3,4-trifluorophenyl group, 3,4,5-trifluorophenyl group, 3-amino-4,6-difluorophenyl group, 1H-pyrazol-4-yl group, 1-methyl-1H-pyrazol-4-yl group, 1-ethyl-3-(trifluoromethyl)-1H-pyrazol-1-yl group, 1H-pyrazol-4-yl group, 1-(propan-2-yl)-1H-pyrazol-4-yl group, 1-(difluoromethyl)-1H-pyrazol-4-yl group, 1-methyl-1H-pyrazol-5-yl group, 3-methyl-1H-pyrazol-4-yl group, 1,3-dimethyl-1H-pyrazol-4-yl group, 3,5-dimethyl-1H-pyrazol-4-yl group, 1-methyl-3-(trifluoromethyl)-1H- pyrazol-4-yl group, 3-(trifluoromethyl)-1H-pyrazol-4-yl group, 1-methyl-5-cyano-1H-pyrrol-2-yl group, 1-ethyl-1H-imidazol-4-yl group, 4-(trifluoromethyl)-1H-imidazol-1-yl group, 3,5-dimethyl-1,2-oxazol-4-yl group, 1,2-thiazol-4-yl group, 2-methyl-1,3-thiazol-5-yl group, 5-(trifluoromethyl)thiophen-2-yl group, 5-cyano-4-methyl-thiophen-2-yl group, 5-(trifluoromethyl)thiophen-3-yl group, pyridin-2-yl group, 5-methyl-pyridin-2-yl group, 5-chloro-pyridin-2-yl group, 5-fluoro-pyridin-2-yl group, pyridin-3-yl group, 4-methylpyridin-3-yl group, 2-methylpyridin-3-yl group, 6-fluoropyridin-3-yl group, 6-methylpyridin-3-yl group, 6-(trifluoromethyl)pyridin-3-yl group, 6-aminopyridin-3-yl group, 6-methoxypyridin-3-yl group, 5-fluoro-6-methylpyridin-3-yl group, 2-methoxy-6-methylpyridin-3-yl group, pyridin-4-yl group, 2-methylpyridin-4-yl group, 2-methoxypyridin-4-yl group, 2-aminopyridin-4-yl group, 3-methylpyridin-4-yl group, pyrimidin-5-yl group, 2-methylpyridin-5-yl group, 1-benzothiophen-2-yl group, imidazo[1,2-a]pyridin-6-yl group, 1-methyl-1H-benzimidazol-6-yl group, 1-methyl-1H-indazol-6-yl group, 1H-indazol-6-yl group, 1H-indol-6-yl group, 1H-indol-5-yl group, Methylamino group, ethylamino group, (propan-2-yl)amino group, propylamino group, butylamino group, tert-butylamino group, pentylamino group, ethyl(methyl)amino group, (butyl)methylamino group, aminocarbonylmethyl group, (2-aminoethyl)amino group, (2-methylpropyl)amino group, (3-methylbutyl)amino group, (2-methoxyethyl)amino group, (2-ethoxyethyl)amino group, (3-methoxypropyl)amino group, (3-cyanopropyl)amino group, (2-hydroxypropyl)amino group, (2-hydroxy-2 -methylpropyl)amino group, (2-methoxypropyl)amino group, (2-ethoxypropyl)amino group, (3,3,3-trifluoro-2-hydroxypropyl)amino group, (2-methoxy-2-methylpropyl)amino group, (2-methoxybutyl)amino group, (3-hydroxybutyl)amino group, (1-hydroxybutan-2-yl)amino group, (4-hydroxybutan-2-yl)amino group, (1-hydroxypentan-2-yl)amino group, (3-hydroxy-3-methylbutyl)amino group, (2-hydroxy-3-methoxypropyl)amino group, (Cyclopropylmethyl)amino group, (1-cyclopropylethyl)amino group, ((1-hydroxycyclobutyl)methyl)amino group, (1-hydroxy-4-methylpentan-2-yl)amino group, (1,3-dihydroxybutan-2-yl)amino group, (2,2-dimethylcyclopropyl)methyl]amino group, (dicyclopropylmethyl)amino group, (3-hydroxycyclobutyl)amino group, [1-(hydroxymethyl)cyclobutyl]methyl group, cyclopentylamino group, (2-hydroxycyclopentyl)amino group, (cyclopentyl)(methyl) )amino group, (4-hydroxycyclohexyl)amino group, bicyclo[2.2.1]heptan-2-yl]amino group, [(3-methyloxetan-3-yl)methyl]amino group, (oxetan-3-yl)amino group, (oxolan-3-yl)methyl)amino group, (tetrahydrofuran-2-ylmethyl)amino group, (oxan-4-yl)amino group, ((oxan-4-yl)methyl)amino group, ((4-methyloxan-4-yl)methyl)amino group, (3-methyloxetan-3-yl)methyl]amino group, [(5-oxopyrrolidin-2-yl)methyl ethyl]amino group, [(6-oxopiperidin-3-yl)methyl]amino group, [(1-methyl-1H-imidazol-2-yl)methyl]amino group, [2-(1H-pyrazol-1-yl)ethyl]amino group, [2-(1H-imidazol-5-yl)ethyl]amino group, (3-(1H-imidazol-1-yl)propyl)amino group, [(1-methyl-1H-pyrazol-5-yl)methyl]amino group, [(1H-pyrazol-3-yl)methyl]amino group, [(1-methyl-1H-pyrazol-3-yl)methyl]amino group, [(1-methyl-1H-pyrazol-4-yl)methyl]amino group, [(pyrazin-2-yl)methyl]amino group, [(pyridin-3-yl)methyl]amino group, [(pyrimidin-5-yl)methyl]amino group, [(pyrimidin-2-yl)methyl]amino group is selected from R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0143] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from CF3 and a fluorine atom; R 2 is selected from hydrogen atoms, R 3 but halogen atoms, a prop-1-en-1-yl group optionally substituted by a methyl group; a piperidin-1-yl group optionally substituted with one or two substituents, each substituent independently selected from a fluorine atom and a methyl group; a morpholin-4-yl group optionally substituted by one or two methyl groups; a pyrrolidin-1-yl group optionally substituted by one or two halogen atoms, a 1,2,3,6-tetrahydropyridin-4-yl group optionally substituted by a methyl group; adithidin-1-yl group, 3,6-dihydro-1H-pyran-4-yl group, a 6-oxo-1,6-dihydropyridin-3-yl group optionally substituted with one or two substituents, each substituent independently selected from a hydrogen atom and a methyl group; cyclopent-1-en-1-yl group, a phenyl group optionally substituted with 1, 2 or 3 substituents, each independently selected from halogen atoms, hydroxy groups, methyl groups, ethyl groups, CF3, CF2H groups, methoxy groups, CF3O groups, NH2 groups and NHCH3 groups; a 2H-pyrrol-1-yl group optionally substituted with one or two substituents, each substituent independently selected from a hydrogen atom, a cyano group, and a methyl group; a 1H-pyrazol-4-yl group optionally substituted with one or two substituents, each substituent independently selected from a methyl group, an ethyl group, or a CF3 group; a 1H-pyrazol-5-yl group optionally substituted by a methyl group; 1,2-oxazol-4-yl optionally substituted by one or two methyl groups; a 1,2-thiazol-4-yl group optionally substituted by a methyl group, a 1,3-thiazol-5-yl group optionally substituted by a methyl group; pyridin-3-yl, pyridin-4-yl and pyridin-5-yl groups, each of which is optionally substituted with one or two substituents, each of which is independently selected from halogen atoms, methyl groups, CF3 groups, methoxy groups and NH2 groups; a pyrimidin-5-yl group optionally substituted by a methyl group; 1H-indol-6-yl group, a 1H-indazol-6-yl group optionally substituted by a methyl group; a 1H-benzimidazol-6-yl group optionally substituted by a methyl group; NH(C2H5) group, NH(C3H7) group, NH(C4H9) group, NCH3(C4H9) group, NH(C5H 11 ) group, NH (cyclopentyl) group, NCH3 (cyclopentyl) group Selected from; R 4 is selected from a hydrogen atom and a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0144] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4-(4,4-difluoropiperidin-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-chloro-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(4-fluoro-4-methylpiperidin-1-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(4-fluoropiperidin-1-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3',4'-difluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2,2'-dimethylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,6-dihydro-2H-pyran-4-yl)-3-methylphenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(1H-pyrazol-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(6-oxo-1,6-dihydropyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(pyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(pyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-6-methyl-5-(3,4,5-trifluorophenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-[3,5-difluoro-4-(morpholin-4-yl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-{3,5-difluoro-4-[(2S)-2-methylmorpholin-4-yl]phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-(4-bromophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (rac)-6-methyl-5-[4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3,5-difluoro-4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 2-(morpholin-4-yl)-5-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)benzonitrile, 3-chloro-2-(morpholin-4-yl)-5-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)benzonitrile, 5-{4-[2,6-dimethylmorpholin-4-yl]-3-fluorophenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-(3-fluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-(3,5-difluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,3-difluoropyrrolidin-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(2-methylpyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(1-methyl-1H-pyrazol-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,4'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(pyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-amino-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-hydroxy-4'-methyl-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{3-(trifluoromethyl)-4-[6-(trifluoromethyl)pyridin-3-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-fluoro-3'-hydroxy-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[5'-amino-2',4'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-amino-3'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(6-aminopyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-4'-methyl-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-2'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-amino-2'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3-methyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1H-indazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(5-fluoro-6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1,2-thiazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 1-methyl-5-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]-1H-pyrrole-2-carbonitrile, 5-[2,4'-bis(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1,3-dimethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-methoxy-6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-methyl-1,3-thiazol-5-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-(methylamino)-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-fluoro-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3',4',5'-trifluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[2',5'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-4'-fluoro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3',4'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1H-indol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-methylprop-1-en-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[2',3'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(morpholin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(butylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1H-pyrazol-4-yl)-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(propylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(6-methylpyridin-3-yl)-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(azetidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1H-benzimidazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(pentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1H-indazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-fluoro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(6-fluoropyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(3-methylpyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(2-methylpyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-2'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2'-chloro-2,4'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopent-1-en-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2'-ethyl-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(6-methoxypyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,4'-difluoro-3'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-3'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-aminopyridin-4-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-(difluoromethyl)-2-fluorobiphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(pyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(2-methylpyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(2-methoxypyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(2-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(6-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',4',5'-tetrafluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',3',4'-tetrafluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',5'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 2'-fluoro-4'-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)biphenyl-4-carbonitrile, 5-(2'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3'-amino-2-fluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-3'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-4'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-2'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,3',4'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(pyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',3'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,3',5'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',4'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-2',4'-dimethylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,3'-difluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',6'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-2'-methoxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,3'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(4-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-(3-fluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4-(morpholin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-(-[(3-chloro-4-(morpholin-4-yl)-5-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 6S)-5-(-[(4-chloro-3-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-(-[(4-fluoro-3-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-chloro-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4-chloro-3-methylphenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-6-methyl-5-(4-morpholino-3-(trifluoromethyl)phenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,5-dimethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-4-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-ethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[cyclopentyl(methyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[butyl(methyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and 5-[3'-Fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group consisting of:

[0145] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4-(4,4-difluoropiperidin-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-chloro-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(4-fluoro-4-methylpiperidin-1-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(4-fluoropiperidin-1-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3',4'-difluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2,2'-dimethylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,6-dihydro-2H-pyran-4-yl)-3-methylphenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(1H-pyrazol-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(6-oxo-1,6-dihydropyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(pyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(pyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-6-methyl-5-(3,4,5-trifluorophenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-[3,5-difluoro-4-(morpholin-4-yl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-{3,5-difluoro-4-[(2S)-2-methylmorpholin-4-yl]phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-6-methyl-5-[4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3,5-difluoro-4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 2-(morpholin-4-yl)-5-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)benzonitrile, 3-chloro-2-(morpholin-4-yl)-5-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)benzonitrile, 5-{4-[2,6-dimethylmorpholin-4-yl]-3-fluorophenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-(3-fluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-(3,5-difluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,3-difluoropyrrolidin-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(2-methylpyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-methyl-4-(1-methyl-1H-pyrazol-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,4'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(pyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-amino-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-hydroxy-4'-methyl-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{3-(trifluoromethyl)-4-[6-(trifluoromethyl)pyridin-3-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-fluoro-3'-hydroxy-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[5'-amino-2',4'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-amino-3'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(6-aminopyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-4'-methyl-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-2'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-amino-2'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3-methyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1H-indazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(5-fluoro-6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1,2-thiazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 1-methyl-5-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]-1H-pyrrole-2-carbonitrile, 5-[2,4'-bis(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1,3-dimethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-methoxy-6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-methyl-1,3-thiazol-5-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-(methylamino)-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-fluoro-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3',4',5'-trifluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[2',5'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3'-amino-4'-fluoro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3',4'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1H-indol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-methylprop-1-en-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[2',3'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(morpholin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(butylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1H-pyrazol-4-yl)-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(propylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(6-methylpyridin-3-yl)-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(azetidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1H-benzimidazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(pentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1H-indazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-fluoro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(6-fluoropyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(3-methylpyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(2-methylpyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-2'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2'-chloro-2,4'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopent-1-en-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2'-ethyl-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(6-methoxypyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,4'-difluoro-3'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-3'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-aminopyridin-4-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-(difluoromethyl)-2-fluorobiphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(pyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(2-methylpyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(2-methoxypyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(2-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(6-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',4',5'-tetrafluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',3',4'-tetrafluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',5'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 2'-fluoro-4'-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)biphenyl-4-carbonitrile, 5-(2'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3'-amino-2-fluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-3'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-4'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-2'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,3',4'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(pyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',3'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,3',5'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',4'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-2',4'-dimethylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,3'-difluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,2',6'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2-fluoro-2'-methoxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,3'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(4-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-(3-fluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4-(morpholin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-(-[(3-chloro-4-(morpholin-4-yl)-5-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 6S)-5-(-[(4-chloro-3-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-(-[(4-fluoro-3-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-chloro-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4-chloro-3-methylphenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-6-methyl-5-(4-morpholino-3-(trifluoromethyl)phenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,5-dimethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-4-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-ethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[cyclopentyl(methyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[butyl(methyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and 5-[3'-Fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group consisting of:

[0146] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4-methyl-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[3-methoxyprop-1-en-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-[4'-hydroxy-2-(trifluoromethyl)-2',3',4',5'-tetrahydro[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(5,6-dihydro-2H-pyran-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(imidazo[1,2-a]pyridin-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[3,3-dimethylbut-1-en-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{3-(trifluoromethyl)-4-[5-(trifluoromethyl)thiophen-3-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(prop-1-en-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-benzothiophen-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2,5-dihydrofuran-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopent-1-en-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1-ethyl-1H-imidazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 3-methyl-5-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]thiophene-2-carbonitrile, 5-{4-[1-(propan-2-yl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-[4-(bicyclo[2.2.1]hept-2-en-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[2'-fluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{3-(trifluoromethyl)-4-[5-(trifluoromethyl)thiophen-2-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(5-methylpyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(5-fluoropyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(5-chloropyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(pyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[2'-(difluoromethyl)-2-fluoro[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(2,4'-difluoro-2'-methyl[1,1'-biphenyl]-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 2'-fluoro-2-methyl-4'-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)[1,1'-biphenyl]-4-carbonitrile, 5-[4-(2-methylprop-1-en-1-yl)-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4-(2-aminopyridin-4-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4-(pyridin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4-(6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[2'-fluoro-4'-methyl-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[2',4',5'-trifluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[2',3',4'-trifluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[2',5'-difluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 4'-[(6S)-6-methyl-2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl]-2'-(trifluoromethyl)[1,1'-biphenyl]-2-carbonitrile, (6S)-5-[4-(1H-indol-5-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4'-hydroxy-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[3'-hydroxy-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[3'-amino-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[2',4'-difluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[3'-fluoro-4'-methyl-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[2'-fluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[2'-methoxy-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[3'-fluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4-(4-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4-(3-methylpyridin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4-(2-methylpyridin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4-(1H-indol-6-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[2'-ethyl-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4-(6-methoxypyridin-3-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4'-methoxy-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4'-methyl-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-fluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-fluoro-5-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{3-(difluoromethyl)-4-[1-(difluoromethyl)-1H-pyrazol-4-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-{4-[(morpholin-4-yl)methyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(morpholin-4-yl)methyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[2-(difluoromethyl)-4'-fluoro[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(difluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-(difluoromethyl)-4-(6-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopent-1-en-1-yl)-3-(difluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-(difluoromethyl)-4-(1H-pyrazol-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3-hydroxy-3-methylazetidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-[4-{[3,3,3-trifluoro-2-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(oxan-4-yl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(cis / trans)-3-hydroxycyclobutyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(rac)-2,4-dimethylazetidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(cis or trans)-2,4-dimethylazetidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[3,3,3-trifluoro-2(S)-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-hydroxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(trans)-4-hydroxycyclohexyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(cyclopropylmethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(3-methyloxetan-3-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, -{4-[(3-methoxypropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-({[(rac)-oxolan-2-yl]methyl}amino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[2(R)-2-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(3R)-3-hydroxybutyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(2S)-2-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(1-hydroxycyclobutyl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(3-methylbutyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-methoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[ethyl(methyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(tert-butylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-({[(2R)-oxolan-2-yl]methyl}amino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(pyrazin-2-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(4-hydroxypiperidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(2S)-1-hydroxybutan-2-yl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3-hydroxypiperidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (racemic mixture), (rac)-1-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]piperidine-3-carboxamide, 5-{4-[(3-hydroxy-2,2-dimethylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(4,4-difluoropiperidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(1R,2R,4R)-bicyclo[2.2.1]heptan-2-yl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(3S)-3-hydroxypyrrolidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-{4-[(2-hydroxy-3-methoxypropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(1-methyl-1H-pyrazol-5-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(1H-pyrazol-3-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[2-(1H-pyrazol-1-yl)ethyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 1-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]piperidine-4-carbonitrile, (rac)-5-{4-[(1-cyclopropylethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-{4-[(2-ethoxypropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (rac)-5-{4-[(2-methoxypropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(3-ethoxyazetidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(pyrimidin-2-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(oxolan-3-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (racemic mixture), 5-[4-{[(2S)-4-hydroxybutan-2-yl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-[4-{[(6-oxopiperidin-3-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-[4-{[(2,2-dimethylcyclopropyl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-({[1-(hydroxymethyl)cyclobutyl]methyl}amino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2S)-2-(hydroxymethyl)azetidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 3-methyl-1-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]azetidine-3-carbonitrile, 5-[4-(3-azabicyclo[3.1.0]hexan-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(4-ethyl-4-hydroxypiperidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 4-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)anilino]butanenitrile, 6-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]-2λ 6 -thia-6-azaspiro[3.3]heptane-2,2-dione, N 2 -[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]glycinamide, 5-{4-[(3R)-3-hydroxypyrrolidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-methoxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-({[(2S)-oxolan-2-yl]methyl}amino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-ethoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(1S,2R)-2-hydroxycyclopentyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(oxetan-3-yl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{3-(difluoromethyl)-4-[1-(propan-2-yl)-1H-pyrazol-4-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[3-fluoro-4-(morpholin-4-yl)-5-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[4-(trifluoromethyl)-1H-imidazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3-methoxypropyl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-methylpropyl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(3,3-dimethylbutyl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(propan-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (rac)-5-{4-[oxan-3-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (trans)-5-{4-[4-hydroxycyclohexyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (trans isomer), (cis)-5-{4-[4-hydroxycyclohexyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-aminoethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one-hydrochloride salt, 5-{4-[1-amino-3-azabicyclo[3.1.0]hexan-3-yl]-3-(trifluoromethyl)-phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one-hydrochloride, 5-[4-(methylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-[4-(4-methylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-hydroxypropan-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4-(3,3-difluoroazetidin-1-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and (6S)-5-[4-(3-hydroxy-3-methylazetidin-1-yl)-3-(trifluoromethyl)-phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0147] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4-(4,4-difluoropiperidin-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(3',4'-difluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(1,2-thiazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(2-methyl-1,3-thiazol-5-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(propylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4'-Fluoro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(cyclopentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2,5-dihydrofuran-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(5-chloropyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (6S)-5-[4-(2-aminopyridin-4-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and (6S)-5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(morpholin-4-yl)methyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (cis / trans)-5-[4-{[3-hydroxycyclobutyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-{[3,3,3-trifluoro-2(S)-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-hydroxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-methoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[(pyrazin-2-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-(2-methylpropyl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and (6S)-5-[4-(3-hydroxy-3-methylazetidin-1-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0148] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4-(4,4-difluoropiperidin-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-(3',4'-difluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(1,2-thiazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(2-methyl-1,3-thiazol-5-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(propylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4'-Fluoro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(cyclopentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(2,5-dihydrofuran-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(5-chloropyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-{4-[(morpholin-4-yl)methyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (cis / trans)-5-[4-{[3-hydroxycyclobutyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-{[(pyrazin-2-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 5-[4-(2-methylpropyl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (6S)-5-[4-(3-hydroxy-3-methylazetidin-1-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0149] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[3,3,3-trifluoro-2(S)-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-hydroxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-methoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4-(2-aminopyridin-4-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0150] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0151] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: (6S)-5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[3,3,3-trifluoro-2(S)-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-hydroxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-methoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4-(2-aminopyridin-4-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0152] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[3,3,3-trifluoro-2(S)-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-hydroxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and 5-{4-[(2-methoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0153] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4-(2-aminopyridin-4-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0154] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

[0155] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0156] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: (6S)-5-[4-(2-aminopyridin-4-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0157] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0158] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0159] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0160] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0161] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: (6S)-5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0162] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-[4-{[3,3,3-trifluoro-2(S)-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0163] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-{4-[(2-hydroxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one and or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof, of the general formula (I) selected from the group:

[0164] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: 5-{4-[(2-methoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

[0165] According to a further embodiment of the first aspect, the present invention provides compounds specifically exemplified in the experimental section, or stereoisomers, tautomers, N-oxides, hydrates, solvates or salts thereof, or mixtures thereof.

[0166] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from a hydrogen atom, a halogen atom, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C9-cycloalkyl groups optionally substituted by hydroxy groups, C5-C9-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, -S-, -S(O)-, S(O)2 and -NR 9 - is a 3- to 9-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from In some cases, -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -CH2-O-, -NR 9 -CH2- and -CH2-NR 9 - further comprising a bridging group selected from: optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally substituted with hydroxy groups; C1-C3-haloalkyl group; C1-C3-alkoxy groups; C1-C3-haloalkoxy group; C(O)NR 5 R 6 Groups and NR 5 R 6 basis a 3- to 9-membered heterocycloalkyl group independently selected from: Partially unsaturated, 5- to 9-membered heterocycloalkyl groups optionally substituted with 1, 2, or 3 substituents, each of which may be an oxo group (=O), a C1-C3-alkyl group, or -C(O)R 5 R 6groups and halogen atoms), aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group or an NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and N.R. 7 R 8 basis Selected from; R 4 is a hydrogen atom; R 5 / R 6 are independently selected from a hydrogen atom, a C1-C6-alkyl group, a -C1-C5-alkylene-O-C1-C5-alkyl group, a -C1-C5-alkylene-S-C1-C5-alkyl group, a C3-C6-cycloalkyl group and a C3-C5-heterocycloalkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6 alkyl groups which is optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, C(O)NR 5 R 6 group, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally substituted by 1 or 2 substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; a 3- to 7-membered heterocycloalkyl group, which itself is optionally substituted by a C1-C3-alkyl group or an oxo (=O) group; Heteroaryl groups which themselves are optionally substituted by C1-C3-alkyl groups (independently selected from -C1-C5-alkylene-O-C1-C5-alkyl group, -C1-C5-alkylene-S-C1-C5-alkyl group, -C1~C5-Alkylene-NR 5 -C1 to C5 alkyl group, C3-C6-cycloalkyl groups optionally substituted by hydroxy groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0167] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from a hydrogen atom, a halogen atom, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from a hydrogen atom and a halogen atom; R 3 but halogen atoms, C2-C6-alkenyl group, C3-C6-cycloalkyl group C5-C6-cycloalkenyl group, C3-C7-heterocycloalkyl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom and a C1-C3-alkyl group, a hydroxy group, NR 5 R 6 group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group), partially unsaturated, optionally substituted C5-C7-heterocycloalkyl groups with 1, 2 or 3 substituents, each of which is independently selected from an oxo group (=O), a C1-C3-alkyl group and a halogen atom; aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group or an NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and N.R. 7 R 8 basis is selected from R 4 is a hydrogen atom, R 5 / R 6 are independently selected from a hydrogen atom, a C1-C6-alkyl group, a -C1-C5-alkylene-O-C1-C5-alkyl group, a -C1-C5-alkylene-S-C1-C5-alkyl group, a C3-C6-cycloalkyl group and a C3-C5-heterocycloalkyl group; R 7 / R 8is a hydrogen atom and a C1-C6-alkyl group, -C1-C5-alkylene-O-C1-C5-alkyl group, -C1-C5-alkylene-S-C1-C5-alkyl group, -C1-C5-alkylene-NR 5 independently selected from C1-C5-alkyl groups, C3-C6-cycloalkyl groups, and C3-C5-heterocycloalkyl groups; Or R 7 and R 8 together, optionally -O-, -S- and -NR 9 -, containing 1 or 2 additional heteroatoms selected from the group consisting of optionally halogen atoms, C1-C3 alkyl groups, hydroxy groups, cyano groups, oxo groups (=O) and NR 5 R 6 forming a 3-, 4-, 5-, 6- or 7-membered ring substituted once, twice or three times with substituents selected from the group R 7 and R 8 taken together to form a 5-, 6- or 7-membered ring, the ring may optionally be -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -NR 9 -CH2-; R 9 is a hydrogen atom or a C1-C3 alkyl group, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0168] According to another embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, S(O)2 and -NR 9 - is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; C(O)NR 5 R 6 Groups and NR 5 R 6 basis a 3- to 7-membered heterocycloalkyl group independently selected from: -O-, -S- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3 alkyl groups and halogen atoms; 9 a 5- to 7-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, cyano groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from; R 4 is a hydrogen atom; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, C(O)NR 5 R 6 group, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 3- to 7-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C7-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0169] According to another embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, S(O)2 and -NR 9 - is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; C(O)NR 5 R 6 Groups and NR 5 R 6 basis a 3- to 7-membered heterocycloalkyl group independently selected from -O-, -S- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3 alkyl groups and halogen atoms; 9 a 5- to 7-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, or an NR 5 R 6 groups), optionally halogen atoms, C1-C3-alkyl groups, cyano groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from; R 4 is a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, C(O)NR 5 R 6 group, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 3- to 7-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C7-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0170] According to another embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, and a C1-C3 haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but halogen atoms, C2-C4-alkenyl group, C5-C6-cycloalkenyl group, C3-C6-heterocycloalkyl groups optionally substituted by one or two substituents, each substituent being independently selected from halogen atoms and C1-C3-alkyl groups; partially unsaturated, optionally substituted C5-C6-heterocycloalkyl groups with one or two substituents, each of which is independently selected from an oxo group (=O), a C1-C3-alkyl group and a halogen atom; Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group or an NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and N.R. 7 R 8 basis Selected from; R 4 is a hydrogen atom; R 5 / R 6 are independently selected from a hydrogen atom, a C1-C6-alkyl group, a -C1-C3-alkylene-O-C1-C3-alkyl group, a -C1-C3-alkylene-S-C1-C3-alkyl group and a C3-C5-heterocycloalkyl group, R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), and C1-C6-alkyl groups, -C1-C3-alkylene-O-C1-C3-alkyl groups, -C1-C3-alkylene-S-C1-C3-alkyl groups, and -C1-C3-alkylene-NR 5 -C1-C3 alkyl group, C3-C6 cycloalkyl group, C3-C5 heterocycloalkyl group are independently selected from Or R 7 and R 8 together, optionally -O-, -S- and -NR 9 -, containing 1 or 2 additional heteroatoms selected from the group consisting of optionally halogen atoms, C1-C3 alkyl groups, hydroxy groups, cyano groups, oxo groups (=O) and NR 5 R 6 forming a 3-, 4-, 5-, 6- or 7-membered ring substituted once, twice or three times with substituents selected from the group R 9 is a hydrogen atom or a C1-C3 alkyl group, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0171] According to yet another embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from CF3, -CH3, -OCF3 and a fluorine atom; R 2 is selected from hydrogen atoms; R 3 but halogen atoms, C2-C4-alkenyl group, C5-C6-cycloalkenyl group, C3-C6-heterocycloalkyl groups optionally substituted by one or two substituents, each substituent being independently selected from halogen atoms and C1-C3-alkyl groups; partially unsaturated C5-C6-heterocycloalkyl groups optionally substituted with an oxo group (=O); Phenyl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group or an NR 5 R 6 independently selected from the group and N.R. 7 R 8 base Selected from; R 4 is a hydrogen atom; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C3 alkyl group; R 7 / R 8 are independently selected from a hydrogen atom and a C1-C6-alkyl group; Or R 7 and R 8 together optionally containing one additional oxygen atom, forming a 4-, 5- or 6-membered ring, optionally substituted once or twice with substituents selected from halogen atoms and C1-C3-alkyl groups, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0172] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from CF3, -CH3, -OCF3 and a fluorine atom; R 2 is selected from hydrogen atoms, R 3 but halogen atoms, a prop-1-en-1-yl group optionally substituted by a methyl group; a piperidin-1-yl group optionally substituted with one or two substituents, each substituent independently selected from a fluorine atom and a methyl group; a morpholin-4-yl group optionally substituted by one or two methyl groups; a pyrrolidin-1-yl group optionally substituted by one or two halogen atoms, a 1,2,3,6-tetrahydropyridin-4-yl group optionally substituted by a methyl group; adithidin-1-yl group, a 3,6-dihydro-1H-pyran-4-yl group, a 6-oxo-1,6-dihydropyridin-3-yl group optionally substituted with one or two substituents, each substituent independently selected from a hydrogen atom and a methyl group; cyclopent-1-en-1-yl group, a phenyl group optionally substituted with 1, 2 or 3 substituents, each independently selected from halogen atoms, hydroxy groups, methyl groups, ethyl groups, CF3, CF2H groups, methoxy groups, CF3O groups, NH2 groups and NHCH3 groups; a 2H-pyrrol-1-yl group optionally substituted with one or two substituents, each independently selected from a hydrogen atom, a cyano group, and a methyl group; a 1H-pyrazol-4-yl group optionally substituted with one or two substituents, each independently selected from a methyl group, an ethyl group, or a CF group; a 1H-pyrazol-5-yl group optionally substituted by a methyl group; 1,2-oxazol-4-yl optionally substituted by one or two methyl groups; a 1,2-thiazol-4-yl group optionally substituted by a methyl group; a 1,3-thiazol-5-yl group optionally substituted by a methyl group; pyridin-3-yl, pyridin-4-yl and pyridin-5-yl groups, each of which is optionally substituted with one or two substituents, each of which is independently selected from halogen atoms, methyl groups, CF3 groups, methoxy groups and NH2 groups; a pyrimidin-5-yl group optionally substituted by a methyl group; 1H-indol-6-yl group, a 1H-indazol-6-yl group optionally substituted by a methyl group; a 1H-benzimidazol-6-yl group optionally substituted by a methyl group; NH(C2H5) group, NH(C3H7) group, NH(C4H9) group, NCH3(C4H9) group, NH(C5H 11 ) group, NH (cyclopentyl) group, NCH3 (cyclopentyl) group Selected from; R 4is a hydrogen atom, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0173] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from CF3, -CH3, -OCF3 and a fluorine atom; R 2 is selected from hydrogen atoms, R 3 but a prop-1-en-1-yl group optionally substituted by a methyl group; a piperidin-1-yl group optionally substituted with one or two substituents, each substituent independently selected from a fluorine atom and a methyl group; a morpholin-4-yl group optionally substituted by one or two methyl groups; a pyrrolidin-1-yl group optionally substituted by one or two halogen atoms, a 1,2,3,6-tetrahydropyridin-4-yl group optionally substituted by a methyl group; adithidin-1-yl group, 3,6-dihydro-1H-pyran-4-yl group, a 6-oxo-1,6-dihydropyridin-3-yl group optionally substituted with one or two substituents, each substituent independently selected from a hydrogen atom and a methyl group; cyclopent-1-en-1-yl group, a phenyl group optionally substituted with 1, 2 or 3 substituents, each independently selected from halogen atoms, hydroxy groups, methyl groups, ethyl groups, CF3, CF2H groups, methoxy groups, CF3O groups, NH2 groups and NHCH3 groups; a 2H-pyrrol-1-yl group optionally substituted with one or two substituents, each independently selected from a hydrogen atom, a cyano group, and a methyl group; a 1H-pyrazol-4-yl group optionally substituted with one or two substituents, each independently selected from a methyl group, an ethyl group, or a CF group; a 1H-pyrazol-5-yl group optionally substituted by a methyl group; 1,2-oxazol-4-yl optionally substituted by one or two methyl groups; a 1,2-thiazol-4-yl group optionally substituted by a methyl group; a 1,3-thiazol-5-yl group optionally substituted by a methyl group; pyridin-3-yl, pyridin-4-yl and pyridin-5-yl groups, each of which is optionally substituted with one or two substituents, each of which is independently selected from halogen atoms, methyl groups, CF3 groups, methoxy groups and NH2 groups; a pyrimidin-5-yl group optionally substituted by a methyl group; 1H-indol-6-yl group, a 1H-indazol-6-yl group optionally substituted by a methyl group; a 1H-benzimidazol-6-yl group optionally substituted by a methyl group; NH(C2H5) group, NH(C3H7) group, NH(C4H9) group, NCH3(C4H9) group, NH(C5H 11 ) group, NH (cyclopentyl) group, NCH3 (cyclopentyl) group Selected from; R 4 is a hydrogen atom, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0174] According to yet another embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl group, -O- and -NR 9 - is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; and C(O)NR 5 R 6 base a 3- to 7-membered heterocycloalkyl group independently selected from: -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 a 5- to 7-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 base Selected from; R 4 is a hydrogen atom; R5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 3- to 7-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C7-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups and hydroxy groups; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0175] According to yet another embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl group, -O- and -NR 9 - is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; and C(O)NR 5 R 6 basis a 3- to 7-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 a 5- to 7-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 groups), optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from; R 4 is a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 3- to 7-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C7-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0176] According to a further embodiment of the first aspect, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is selected from halogen atoms, C1-C3-alkyl groups and C1-C3-haloalkyl groups; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but halogen atoms, C2-C4-alkenyl group, C5-C6-cycloalkenyl group, C3-C6-heterocycloalkyl groups optionally substituted by one or two substituents, each substituent being independently selected from halogen atoms and C1-C3-alkyl groups; partially unsaturated C5-C6-heterocycloalkyl groups optionally substituted with an oxo group (=O); Phenyl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group or an NR 5 R 6 independently selected from the group and N.R. 7 R 8 basis Selected from; R 4 is a hydrogen atom; R 5 / R 6are independently selected from a hydrogen atom and a C1-C3 alkyl group; R 7 / R 8 are independently selected from a hydrogen atom, a C3-C5-cycloalkyl group and a C1-C6-alkyl group; Or R 7 and R 8 together optionally containing one additional oxygen atom, forming a 4-, 5- or 6-membered ring, optionally substituted once or twice with substituents selected from halogen atoms and C1-C3-alkyl groups, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0177] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C4-C6-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl group, -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups a 3- to 6-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 -, an aryl group optionally substituted with one or two substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or a 5- to 6-membered heterocycloalkyl group containing a heteroatom selected from the group consisting of -, 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from; R 4 is a hydrogen atom; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, hydroxy groups, C1-C3-alkoxy group, C3-C6-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 4- to 6-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups, a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0178] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C4-C6-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl group, -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; a 3- to 6-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 a 5- to 6-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with one or two substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from; R 4 is a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, hydroxy groups, C1-C3-alkoxy group, C3-C6-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 4- to 6-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted with hydroxy groups or C1-C3-alkyl groups a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0179] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from CF3 and a fluorine atom; R 2 is selected from hydrogen atoms, R 3 but halogen atoms, a prop-1-en-1-yl group optionally substituted by a methyl group; a piperidin-1-yl group optionally substituted with one or two substituents, each substituent independently selected from a fluorine atom and a methyl group; a morpholin-4-yl group optionally substituted by one or two methyl groups; a pyrrolidin-1-yl group optionally substituted by one or two halogen atoms, a 1,2,3,6-tetrahydropyridin-4-yl group optionally substituted by a methyl group; adithidin-1-yl group, 3,6-dihydro-1H-pyran-4-yl group, a 6-oxo-1,6-dihydropyridin-3-yl group optionally substituted with one or two substituents, each substituent independently selected from a hydrogen atom and a methyl group; cyclopent-1-en-1-yl group, a phenyl group optionally substituted with 1, 2 or 3 substituents, each independently selected from halogen atoms, hydroxy groups, methyl groups, ethyl groups, CF3, CF2H groups, methoxy groups, CF3O groups, NH2 groups and NHCH3 groups; a 2H-pyrrol-1-yl group optionally substituted with one or two substituents, each independently selected from a hydrogen atom, a cyano group, and a methyl group; a 1H-pyrazol-4-yl group optionally substituted with one or two substituents, each independently selected from a methyl group, an ethyl group, or a CF group; a 1H-pyrazol-5-yl group optionally substituted by a methyl group; 1,2-oxazol-4-yl optionally substituted by one or two methyl groups; a 1,2-thiazol-4-yl group optionally substituted by a methyl group; a 1,3-thiazol-5-yl group optionally substituted by a methyl group; pyridin-3-yl, pyridin-4-yl and pyridin-5-yl groups, each of which is optionally substituted with one or two substituents, each of which is independently selected from halogen atoms, methyl groups, CF3 groups, methoxy groups and NH2 groups; a pyrimidin-5-yl group optionally substituted by a methyl group; 1H-indol-6-yl group, a 1H-indazol-6-yl group optionally substituted by a methyl group; a 1H-benzimidazol-6-yl group optionally substituted by a methyl group; NH(C2H5) group, NH(C3H7) group, NH(C4H9) group, NCH3(C4H9) group, NH(C5H11 ) group, NH (cyclopentyl) group, NCH3 (cyclopentyl) group Selected from; R 4 is a hydrogen atom, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0180] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group and a C1-C3-haloalkyl group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C3-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, a C5-C6-cycloalkenyl group optionally substituted by a hydroxy group; -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally substituted with hydroxy groups a 3- to 6-membered heterocycloalkyl group independently selected from: a 5- to 7-membered partially unsaturated heterocycloalkyl group optionally substituted with one or two substituents, each substituent being independently selected from a C1-C3-alkyl group and a halogen atom; aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 groups), monocyclic or bicyclic heteroaryl groups optionally substituted with one or two substituents, each of which is selected from halogen atoms, C1-C3-alkyl groups, cyano groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups, hydroxy groups and NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and N.R. 7 R 8 basis Selected from; R 4 is a hydrogen atom; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6 alkyl groups which is optionally substituted with 1, 2, 3 or 4 substituents, halogen atoms, cyano groups and hydroxy groups, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally substituted by 1 or 2 substituents, the substituents being independently selected from C1-C3-alkyl groups, hydroxy groups and C1-C3-hydroxyalkyl groups; 3- to 7-membered heterocycloalkyl groups, which themselves are optionally substituted by C1-C3-alkyl groups, Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted by hydroxy groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0181] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group and a C1-C3-haloalkyl group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C3-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, a C5-C6-cycloalkenyl group optionally substituted by a hydroxy group; -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally substituted with hydroxy groups a 3- to 6-membered heterocycloalkyl group independently selected from: a 5- to 7-membered partially unsaturated heterocycloalkyl group optionally substituted with one or two substituents, each substituent being independently selected from a C1-C3-alkyl group and a halogen atom; aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 groups), monocyclic or bicyclic heteroaryl groups optionally substituted with one or two substituents, each of which is selected from halogen atoms, C1-C3-alkyl groups, cyano groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups, hydroxy groups and NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and N.R. 7 R 8 base Selected from; R 4 is a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C6 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6 alkyl groups which is optionally substituted with 1, 2, 3 or 4 substituents, halogen atoms, cyano groups and hydroxy groups, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally substituted by 1 or 2 substituents, the substituents being independently selected from C1-C3-alkyl groups, hydroxy groups and C1-C3-hydroxyalkyl groups; 3- to 7-membered heterocycloalkyl groups, which themselves are optionally substituted by C1-C3-alkyl groups, Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted by hydroxy groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0182] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group and a C1-C3-haloalkyl group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from A 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, each of which is halogen atoms; hydroxy group C1-C3-alkyl groups optionally further substituted with hydroxy groups are independently selected from an aryl group optionally substituted with one or two substituents, each substituent being independently selected from a halogen atom, a hydroxy group, and a C1-C3-haloalkyl group; optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from; R 4 is a hydrogen atom; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C3 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1 or 2, 3 or 4 substituents, Halogen atoms, hydroxy groups; C1-C3-alkoxy group, C3-C5-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 5-6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from -; Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups; a 4- to 5-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0183] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from a hydrogen atom, a halogen atom, a C1-C3-alkyl group and a C1-C3-haloalkyl group; R 2 is selected from hydrogen atoms and halogen atoms; R 3 but -O- and -NR 9 -, and A 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, each of which is halogen atoms; hydroxy group C1-C3-alkyl groups optionally further substituted with hydroxy groups are independently selected from an aryl group optionally substituted with one or two substituents, each substituent being independently selected from a halogen atom, a hydroxy group, and a C1-C3-haloalkyl group; optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from; R 4is a C1-C3 alkyl group; R 5 / R 6 are independently selected from a hydrogen atom and a C1-C3 alkyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1 or 2, 3 or 4 substituents, Halogen atoms, hydroxy groups, C1-C3-alkoxy group, C3-C5-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 -, a 5- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C6-cycloalkyl groups optionally substituted with hydroxy groups or C1-C3-alkyl groups a 4- to 5-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; are independently selected from R 9 is a hydrogen atom, a C1-C3 alkyl group, or a bond; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0184] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from CF3 and fluorine atoms; R 2 is a hydrogen atom; R 3 but an aryl group optionally substituted with a substituent selected from a halogen atom and a C1-C3-haloalkyl group, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group and N.R. 7 R 8 basis Selected from; R 4 is a hydrogen atom; R 5 / R 6 is a hydrogen atom or a methyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C3-alkyl groups, which are optionally substituted with 1, 2 or 4 substituents, Halogen atoms, hydroxyl groups, and methoxy groups (independently selected from are independently selected from The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0185] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from CF3 and fluorine atoms; R 2 is a hydrogen atom; R 3 but an aryl group optionally substituted with a substituent selected from a halogen atom and a C1-C3-haloalkyl group, C1-C3-haloalkyl groups and NR 5 R 6a monocyclic heteroaryl group substituted with a substituent selected from the group and N.R. 7 R 8 basis Selected from; R 4 is a C1-C3 alkyl group; R 5 / R 6 is a hydrogen atom or a methyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C3-alkyl groups, which are optionally substituted with 1, 2 or 4 substituents, Halogen atoms, hydroxyl groups, and methoxy groups (independently selected from are independently selected from The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0186] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from CF3 and fluorine atoms; R 2 is a hydrogen atom; R 3 but an aryl group optionally substituted with a substituent selected from a halogen atom and a C1-C3-haloalkyl group, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group and N.R. 7 R 8 basis Selected from; R 4 is a methyl group; R 5 / R 6 is a hydrogen atom or a methyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C3-alkyl groups, which are optionally substituted with 1, 2 or 4 substituents, Halogen atoms, hydroxyl groups, and methoxy groups (independently selected from are independently selected from The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0187] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is selected from CF3 and fluorine atoms; R 2 is a hydrogen atom; R 3 but an aryl group optionally substituted with a substituent selected from a halogen atom and a C1-C3-haloalkyl group, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group and N.R. 7 R 8 basis Selected from; R 4 is a methyl group having an S configuration; R 5 / R 6 is a hydrogen atom or a methyl group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C3-alkyl groups, which are optionally substituted with 1, 2 or 4 substituents, Halogen atoms, hydroxyl groups, and methoxy groups (independently selected from are independently selected from The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0188] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, a fluorine atom, an OCF3 group, or a CH3 group, R 2 is a hydrogen atom, R 3 but C1-C4 alkyl group, a phenyl group optionally substituted with one or two substituents, the substituents being selected from halogen atoms; a 4- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being selected from a halogen atom, a methyl group, or a hydroxy group; partially unsaturated 5-membered heterocycloalkyl groups; heteroaryl groups optionally substituted with C1-C3-haloalkyl groups, NH2 groups, methyl groups, chlorine atoms, C1-C3-haloalkyl groups, and NR 7 R 8 basis is selected from R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C4-C5-cycloalkyl group or C1-C4-alkyl group which is optionally substituted one or more times with substituents, a halogen atom, a hydroxy group, a heterocycloalkyl group, or a heteroaryl group (independently selected from are independently selected from R 4is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0189] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, a fluorine atom, an OCF3 group, or a CH3 group, R 2 is a hydrogen atom, R 3 but C1-C4 alkyl group, a phenyl group optionally substituted with one or two substituents, the substituents being selected from fluorine or chlorine atoms; a 4- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being selected from a fluorine atom, a methyl group, or a hydroxy group; partially unsaturated 5-membered heterocycloalkyl groups; Heteroaryl groups optionally substituted with NH, methyl, chlorine, trifluoromethyl and difluoromethyl groups; NR 7 R 8 basis is selected from R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C4-C5-cycloalkyl group or C1-C4-alkyl group which is optionally substituted one or more times with substituents, fluorine atom, hydroxy group, heterocycloalkyl group or heteroaryl group (independently selected from are independently selected from R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0190] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group or a CH3 group; R 2 is a hydrogen atom; R 3 is a phenyl group optionally substituted with a halogen atom, a heteroaryl group optionally substituted with a C1-C3-haloalkyl group, or NR 7 R 8 It is the basis, R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), or C1-C4 alkyl group which is optionally substituted one or more times with substituents, Halogen atom, hydroxy group, or C1-C3 alkoxy group (independently selected from are independently selected from R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0191] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group or a CH3 group; R 2 is a hydrogen atom; R 3 is a phenyl group optionally substituted with a fluorine atom or a chlorine atom, a pyridyl group or a pyrazolyl group optionally substituted with a CHF2 group or a CF3 group, or NR 7 R 8 It is the basis, R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), or C2-C4 alkyl group which is optionally substituted one or more times with substituents, fluorine atom, hydroxy group, or methoxy group (independently selected from are independently selected from R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0192] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group optionally substituted by a halogen atom or a heteroaryl group optionally substituted by a C1-C3-haloalkyl group, R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0193] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group optionally substituted with a halogen atom or a heteroaryl group optionally substituted with a CHF2 or CF3 group, R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0194] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group optionally substituted by a halogen atom or a heteroaryl group optionally substituted by a C1-C3-haloalkyl group, R 4 is a hydrogen atom, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0195] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group optionally substituted by a halogen atom or a heteroaryl group optionally substituted by a C1-C3-haloalkyl group, R 4 is a methyl group, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0196] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group optionally substituted by a halogen atom or a 5-membered heteroaryl group optionally substituted by a C1-C3-haloalkyl group, R4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0197] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group optionally substituted by a halogen atom or a 6-membered heteroaryl group optionally substituted by a C1-C3-haloalkyl group, R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0198] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 but a phenyl group substituted with a fluorine atom or a chlorine atom; pyrazolyl groups substituted with CHF2 or CF3 groups, and Pyridine group substituted with NH2 or NHCH3 groups is selected from

[0199] R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0200] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1is a CF3 group, R 2 is a hydrogen atom, R 3 but a phenyl group substituted with a fluorine atom; pyrazolyl groups substituted with CHF2 or CF3 groups, and Pyridine group substituted with NH2 or NHCH3 groups is selected from

[0201] R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0202] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 but a phenyl group substituted with a fluorine atom or a chlorine atom; pyrazolyl groups substituted with CHF2 or CF3 groups, and Pyridine group substituted with NH2 or NHCH3 groups is selected from

[0203] R 4 is a hydrogen atom, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0204] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 but fluorine-substituted phenyl groups; pyrazolyl groups substituted with CHF2 or CF3 groups, and Pyridine group substituted with NH2 or NHCH3 groups Selected from; R 4 is a hydrogen atom, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0205] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 but a phenyl group substituted with a fluorine atom or a chlorine atom; pyrazolyl groups substituted with CHF2 or CF3 groups, and Pyridine group substituted with NH2 or NHCH3 groups is selected from

[0206] R 4 is a methyl group, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0207] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 but a phenyl group substituted with a fluorine atom; pyrazolyl groups substituted with CHF2 or CF3 groups, and Pyridine group substituted with NH2 or NHCH3 groups is selected from

[0208] R 4 is a methyl group, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0209] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group substituted with a fluorine atom, or a 1H-pyrazol-4-yl group or a 1H-pyrazol-1-yl group substituted with a CHF2 group or a CF3 group, R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0210] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group substituted with a fluorine atom, or a 1H-pyrazol-4-yl group or a 1H-pyrazol-1-yl group substituted with a CHF2 group or a CF3 group, R 4 is a hydrogen atom, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0211] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3is selected from a phenyl group substituted with a fluorine atom, or a 1H-pyrazol-4-yl group or a 1H-pyrazol-1-yl group substituted with a CHF2 group or a CF3 group, R 4 is a methyl group, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0212] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group substituted with a fluorine atom, a 1H-pyrazol-4-yl group substituted with a CHF2 group, or a 1H-pyrazol-1-yl group substituted with a CF3 group; R 4 is a hydrogen atom or a methyl group; The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0213] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R 1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group substituted with a fluorine atom, a 1H-pyrazol-4-yl group substituted with a CHF2 group, or a 1H-pyrazol-1-yl group substituted with a CF3 group; R 4 is a hydrogen atom, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0214] According to yet a further embodiment of the first aspect, the present invention provides a method for producing a cellular membrane comprising: R1 is a CF3 group, R 2 is a hydrogen atom, R 3 is selected from a phenyl group substituted with a fluorine atom, a 1H-pyrazol-4-yl group substituted with a CHF2 group, or a 1H-pyrazol-1-yl group substituted with a CF3 group; R 4 is a methyl group, The present invention provides a compound of general formula (I) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof:

[0215] Further embodiments of the present invention: In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a hydrogen atom, a halogen atom, a cyano group, a C1-C3 alkyl group, a C1-C3 haloalkyl group or a C1-C3 haloalkoxy group, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0216] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group or a C1-C3 haloalkoxy group, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0217] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a hydrogen atom, a fluorine atom, a methyl group, a trifluoromethyl group or a trifluoromethoxy group; Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0218] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a hydrogen atom, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0219] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a halogen atom, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0220] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a C1-C3-haloalkyl group; Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0221] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a CHF2 group or a CF3 group, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0222] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a fluorine atom or a trifluoromethyl group; Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0223] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a fluorine atom, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0224] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a trifluoromethyl group; Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0225] In a further embodiment of the first aspect or any embodiment derived therefrom, R 1 and R 2 are each independently a halogen atom (e.g., F and / or Cl), and R 4 is methyl, R 3 is not morpholinyl.

[0226] In a further embodiment of the first aspect or any embodiment derived therefrom, R 1 and R 2 are each independently a halogen atom (e.g., F and / or Cl) or a C1-C3-haloalkyl group, and R 4 is methyl, R 3 is not morpholinyl.

[0227] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 2 is a hydrogen atom or a halogen atom, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0228] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a fluorine atom or a trifluoromethyl group, and R 2 is a hydrogen atom or a methyl group; Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0229] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a trifluoromethyl group, and R 2 is a hydrogen atom, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0230] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 1 is a fluorine atom, and R 2 is a hydrogen atom, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0231] In a further embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 2 is a hydrogen atom, Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0232] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C9-cycloalkyl groups optionally substituted by hydroxy groups, C5-C9-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, -S-, -S(O)-, S(O)2 and -NR 9 - is a 3- to 9-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from In some cases, -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -CH2-O-, -NR 9 -CH2- and -CH2-NR 9 - further comprising a bridging group selected from: optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-haloalkyl group; C1-C3-alkoxy groups; C1-C3-haloalkoxy group; C(O)NR 5 R 6 Groups and NR 5 R 6 basis a 3- to 9-membered heterocycloalkyl group independently selected from: Partially unsaturated, 5- to 9-membered heterocycloalkyl groups optionally substituted with 1, 2, or 3 substituents, each of which may be an oxo group (=O), a C1-C3-alkyl group, or -C(O)R 5 R 6 groups and halogen atoms), aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group or an NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and NR 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0233] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C9-cycloalkyl groups optionally substituted by hydroxy groups, C5-C9-cycloalkenyl group optionally substituted with a hydroxy group -O-, -S-, -S(O)-, S(O)2 and -NR 9 - is a 3- to 9-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from In some cases, -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -CH2-O-, -NR 9 -CH2- and -CH2-NR 9 -, further comprising a bridging group selected from optionally substituted with 1, 2, or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-haloalkyl group; C1-C3-alkoxy groups; C1-C3-haloalkoxy group; C(O)NR 5 R 6 Groups and NR 5 R 6 basis a 3- to 9-membered heterocycloalkyl group independently selected from Partially unsaturated, 5- to 9-membered heterocycloalkyl groups optionally substituted with 1, 2, or 3 substituents, each of which may be an oxo group (=O), a C1-C3-alkyl group, or -C(O)R 5 R 6 groups and halogen atoms), aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group or an NR 5 R 6 groups, with the proviso that a monocyclic heteroaryl group is not a pyridinyl group; and NR 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0234] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C9-cycloalkyl groups optionally substituted by hydroxy groups, C5-C9-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, -S-, -S(O)-, S(O)2 and -NR 9 - is a 3- to 9-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from In some cases, -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -CH2-O-, -NR 9 -CH2- and -CH2-NR 9 - further comprising a bridging group selected from: optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-haloalkyl group; C1-C3-alkoxy groups; C1-C3-haloalkoxy group; C(O)NR 5 R 6 Groups and NR 5 R 6 base a 3- to 9-membered heterocycloalkyl group independently selected from: Partially unsaturated, 5- to 9-membered heterocycloalkyl groups optionally substituted with 1, 2, or 3 substituents, each of which may be an oxo group (=O), a C1-C3-alkyl group, or -C(O)R 5 R 6 groups and halogen atoms), aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group or an NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-2-yl group, a pyridin-3-yl group, or a pyridin-4-yl group; and NR 7 R 8 base Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0235] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: Any R 3 When is a heterocycloalkyl component, the component is optionally substituted with 1, 2 or 3 substituents, each of which is fluorine atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-haloalkyl group; C1-C3-alkoxy groups; C1-C3-haloalkoxy group; C(O)NR 5 R 6 Groups and NR 5 R 6 base are independently selected from Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0236] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: Any R 3 When is a heterocycloalkyl component, the component is optionally substituted with one or two substituents, each of which is fluorine atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; C(O)NR 5 R 6 Groups and NR 5 R 6 base are independently selected from Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0237] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: Any R 3 When is a heterocycloalkyl component, the component is optionally substituted with one or two substituents, each of which is fluorine atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; and C(O)NR 5 R 6 base are independently selected from Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0238] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: Any R 3 When is a heterocycloalkyl component, the component is optionally substituted with one or two substituents, each of which is fluorine atoms; cyano group; hydroxy group C1-C3-alkyl groups optionally further substituted with hydroxy groups; are independently selected from Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0239] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: Any R 3When is a heterocycloalkyl component, the component is optionally substituted with 1, 2 or 3 substituents, each of which is fluorine atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; are independently selected from Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0240] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: Any R 3 When is a heterocycloalkyl component, the component is optionally substituted with one or two substituents, each of which is fluorine atoms; hydroxy group C1-C3-alkyl groups optionally further substituted with hydroxy groups; are independently selected from Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0241] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl groups optionally substituted by hydroxy groups, -O-, S(O)2 and -NR 9- is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; C(O)NR 5 R 6 Groups and NR 5 R 6 base a 3- to 7-membered heterocycloalkyl group independently selected from Partially unsaturated, optionally C1-C3-alkyl groups, -C(O)R 5 R 6 -O-, -S- and -NR- substituted with a substituent selected from a group and a halogen atom 9 a 5- to 7-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, cyano groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and NR 7 R 8 base Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0242] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl group, -O- and -NR 9 - is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; and C(O)NR 5 R 6 base a 3- to 7-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 a 5- to 7-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and NR 7 R 8 base Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0243] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted with substituents selected from hydroxy groups, C1-C4-alkoxy groups and 3- to 7-membered heterocycloalkyl groups, C2-C6-alkenyl groups optionally substituted by C1-C4-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, C5-C7-cycloalkenyl group, -O- and -NR 9 - is a 3- to 7-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; C1-C3-alkoxy groups; and C(O)NR 5 R 6 base a 3- to 7-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 a 5- to 7-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups substituted with one, two or three substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3 alkyl group, a C1-C3 haloalkyl group or a NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and NR 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0244] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; a 3- to 6-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 a 5- to 6-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups optionally substituted with one or two substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0245] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; a 3- to 6-membered heterocycloalkyl group independently selected from -O- and -NR, which are partially unsaturated and optionally substituted with substituents selected from C1-C3-alkyl groups and halogen atoms; 9 a 5- to 6-membered heterocycloalkyl group containing a heteroatom selected from Aryl groups substituted with one or two substituents (each substituent is a halogen atom, a hydroxy group, a cyano group, a C1-C3 alkyl group, a C1-C3 haloalkyl group, or an NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0246] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C3-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, a C5-C6-cycloalkenyl group optionally substituted by a hydroxy group; -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups a 3- to 6-membered heterocycloalkyl group independently selected from a 5- to 7-membered partially unsaturated heterocycloalkyl group optionally substituted with one or two substituents, each substituent being independently selected from a C1-C3-alkyl group and a halogen atom; aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with one or two substituents, each of which is a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group, and NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and NR 7 R 8 base Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0247] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C3-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, a C5-C6-cycloalkenyl group optionally substituted by a hydroxy group; -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups; a 3- to 6-membered heterocycloalkyl group independently selected from a 5- to 7-membered partially unsaturated heterocycloalkyl group optionally substituted with one or two substituents, each substituent being independently selected from a C1-C3-alkyl group and a halogen atom; An aryl group substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, a C1-C3 haloalkoxy group, or a NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with one or two substituents, each of which is a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group, and NR 5 R 6 groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and NR 7 R 8 base Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0248] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but C1-C6-alkyl groups optionally substituted by 1 or 2 substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group; C2-C6-alkenyl groups optionally substituted by C1-C3-alkoxy groups, C3-C7-cycloalkyl groups optionally substituted by hydroxy groups, a C5-C6-cycloalkenyl group optionally substituted by a hydroxy group; -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally further substituted with hydroxy groups a 3- to 6-membered heterocycloalkyl group independently selected from a 5- to 7-membered partially unsaturated heterocycloalkyl group optionally substituted with one or two substituents, each substituent being independently selected from a C1-C3-alkyl group and a halogen atom; An aryl group substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, a C1-C3 haloalkoxy group, or a NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with one or two substituents, each of which is a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group, and NR 5 R 6groups, with the proviso that the monocyclic heteroaryl group is not a pyridin-4-yl group; and NR 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0249] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; hydroxy group C1-C3-alkyl groups optionally further substituted with hydroxy groups; a 3- to 6-membered heterocycloalkyl group independently selected from an aryl group optionally substituted with one or two substituents, each substituent being independently selected from a halogen atom, a hydroxy group, and a C1-C3-haloalkyl group; optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0250] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; hydroxy group C1-C3-alkyl groups optionally further substituted with hydroxy groups; a 3- to 6-membered heterocycloalkyl group independently selected from a phenyl group optionally substituted by one or two substituents, each substituent being independently selected from a halogen atom, a hydroxy group, and a C1-C3-haloalkyl group; optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 base Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0251] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but -O- and -NR 9 - is a 3- to 6-membered heterocycloalkyl group containing 1 or 2 heteroatoms independently selected from optionally substituted with 1 or 2 substituents, each of which is halogen atoms; hydroxy group C1-C3-alkyl groups optionally further substituted with hydroxy groups; a 3- to 6-membered heterocycloalkyl group independently selected from a phenyl group substituted by one or two substituents, each substituent being independently selected from a halogen atom, a hydroxy group, and a C1-C3-haloalkyl group; optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0252] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but an aryl group optionally substituted with a substituent selected from a halogen atom and a C1-C3-haloalkyl group, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group; and N.R. 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0253] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but a phenyl group optionally substituted by a substituent selected from a halogen atom and a C1-C3-haloalkyl group, C1-C3-haloalkyl groups and NR5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group; and N.R. 7 R 8 basis Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0254] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but Methyl group, propan-2-yl group, 2-methylpropyl group, 2-hydroxypropan-2-yl group, 3,3-dimethylbutyl group, 3-methoxypropyl group, a —CH2-(morpholin-4-yl) group, prop-1-en-2-yl group, 2-methylprop-1-en-1-yl group, 3,3-dimethylbut-1-en-1-yl group, 3-methoxyprop-1-en-1-yl group, 4-hydroxycyclohexyl group, Cyclopent-1-en-1-yl group, cyclohex-1-en-1-yl group, bicyclo[2.2.1]hept-2-en-2-yl group Oxan-3-yl group, 3,3-difluoroazetidin-1-yl group, azetidine-3-carboxamide, 2-hydroxyazetidin-1-yl group, 3-hydroxy-3-methylazetidin-1-yl group, 2-(hydroxymethyl)azetidin-1-yl group, 3-cyano-3-methylazetidin-1-yl group, 2,4-dimethylazetidin-1-yl group, -2λ6-thia-6-azaspiro[3.3]heptane-2,2-dione group, 3-hydroxypyrrolidin-1-yl group, 3,3-difluoropyrrolidin-1-yl group, 3-azabicyclo[3.1.0]hexan-3-yl group, 1 -amino-3-azabicyclo[3.1.0]hexan-3-yl group, 4-fluoropiperidin-1-yl group, 4,4-fluoropiperidin-1-yl group, 4-cyanopiperidin-1-yl group, 4-fluoro-4-methylpiperidin-1-yl group, 4-ethyl-4-hydroxypiperidin-1-yl group, 4-hydroxypiperidin-1-yl group, 3-hydroxypiperidin-1-yl group, 3-aminocarbonylpiperidin-1-yl group, morpholin-4-yl group, 2-methylmorpholin-4-yl group, 2,6-dimethylmorpholin-4-yl group, 4-methylpiperazin-1-yl group, 2,5-dihydrofuran-3-yl group, 5,6-dihydro-2H-pyran-3-yl group, 3,6-dihydro-2H-pyran-4-yl group, 1,2,3,6-tetrahydropyridin-4-yl group, 1-methyl-1,2,3,6-tetrahydropyridin-4-yl group, 6-oxo-1,6-dihydropyridin-3-yl group, phenyl group, 2-methylphenyl group, 2-ethylphenyl group, 2-fluorophenyl group, 2-aminophenyl group, 2-hydroxyphenyl group, 2-methoxyphenyl group nyl group, 2,4-dimethylphenyl group, 2-fluoro-4-methylphenyl group, 2-fluoro-4-aminophenyl group, 4-cyano-2-methylphenyl group, 2-chloro-4-fluorophenyl group, 2,3-difluorophenyl group, 2-fluoro-3-aminophenyl group, 2,5-difluorophenyl group, 2,6-difluorophenyl group, 4-fluoro-6-methylphenyl group, (2-difluoromethyl)phenyl group, 2-cyanophenyl group, 2,4-difluorophenyl group, 3 -methylphenyl group, 3-aminophenyl group, 3-fluorophenyl group, 3-hydroxyphenyl group, 3,4-difluorophenyl group, 3-amino-4-methylphenyl group, 3-amino-4-chlorophenyl group, 3-amino-4-fluorophenyl group, 3-fluoro-4-methylphenyl group, 4-amino-3-fluorophenyl group, 4-fluoro-3-methylphenyl group, 4-fluoro-3-hydroxyphenyl group, 3-hydroxy-4-methylphenyl group, 4-methylphenyl group, 4-fluorophenyl group, 4-chlorophenyl group, 4-(difluoromethyl)phenyl group, 4-(trifluoromethyl)phenyl group, 4-cyanophenyl group, 4-aminophenyl group, 4-(methylamino)phenyl group, 4-hydroxyphenyl group, 4-methoxyphenyl group, 3,5-difluorophenyl group, 2,4,5-trifluorophenyl group, 2,3,4-trifluorophenyl group, 3,4,5-trifluorophenyl group, 3-amino-4,6-difluorophenyl group, 1H-pyrazol-4-yl group, 1-methyl-1H-pyrazol-4-yl group, 1-ethyl-3-(trifluoromethyl)-1H-pyrazol-1-yl group, 1H-pyrazol-4-yl group, 1-(propan-2-yl)-1H-pyrazol-4-yl group, 1-(difluoromethyl)-1H-pyrazol-4-yl group, 1-methyl-1H-pyrazol-5-yl group, 3-methyl-1H-pyrazol-4-yl group, 1,3-dimethyl-1H-pyrazol-4-yl group, 3,5-dimethyl-1H-pyrazol-4-yl group, 1-methyl-3-(trifluoromethyl)-1H- pyrazol-4-yl group, 3-(trifluoromethyl)-1H-pyrazol-4-yl group, 1-methyl-5-cyano-1H-pyrrol-2-yl group, 1-ethyl-1H-imidazol-4-yl group, 4-(trifluoromethyl)-1H-imidazol-1-yl group, 3,5-dimethyl-1,2-oxazol-4-yl group, 1,2-thiazol-4-yl group, 2-methyl-1,3-thiazol-5-yl group, 5-(trifluoromethyl)thiophen-2-yl group, 5-cyano-4-methyl-thiophen-2-yl group, 5-(trifluoromethyl)thiophen-3-yl group, pyridin-2-yl group, 5-methyl-pyridin-2-yl group, 5-chloro-pyridin-2-yl group, 5-fluoro-pyridin-2-yl group, pyridin-3-yl group, 4-methylpyridin-3-yl group, 2-methylpyridin-3-yl group, 6-fluoropyridin-3-yl group, 6-methylpyridin-3-yl group, 6-(trifluoromethyl)pyridin-3-yl group, 6-aminopyridin-3-yl group, 6-methoxypyridin-3-yl group, 5-fluoro-6-methylpyridin-3-yl group, 2-methoxy-6-methylpyridin-3-yl group, pyridin-4-yl group, 2-methylpyridin-4-yl group, 2-methoxypyridin-4-yl group, 2-aminopyridin-4-yl group, 3-methylpyridin-4-yl group, pyrimidin-5-yl group, 2-methylpyridin-5-yl group, 1-benzothiophen-2-yl group, imidazo[1,2-a]pyridin-6-yl group, 1-methyl-1H-benzimidazol-6-yl group, 1-methyl-1H-indazol-6-yl group, 1H-indazol-6-yl group, 1H-indol-6-yl group, 1H-indol-5-yl group, Methylamino group, ethylamino group, (propan-2-yl)amino group, propylamino group, butylamino group, tert-butylamino group, pentylamino group, ethyl(methyl)amino group, (butyl)methylamino group, aminocarbonylmethyl group, (2-aminoethyl)amino group, (2-methylpropyl)amino group, (3-methylbutyl)amino group, (2-methoxyethyl)amino group, (2-ethoxyethyl)amino group, (3-methoxypropyl)amino group, (3-cyanopropyl)amino group, (2-hydroxypropyl)amino group, (2-hydroxy-2 -methylpropyl)amino group, (2-methoxypropyl)amino group, (2-ethoxypropyl)amino group, (3,3,3-trifluoro-2-hydroxypropyl)amino group, (2-methoxy-2-methylpropyl)amino group, (2-methoxybutyl)amino group, (3-hydroxybutyl)amino group, (1-hydroxybutan-2-yl)amino group, (4-hydroxybutan-2-yl)amino group, (1-hydroxypentan-2-yl)amino group, (3-hydroxy-3-methylbutyl)amino group, (2-hydroxy-3-methoxypropyl)amino group, (Cyclopropylmethyl)amino group, (1-cyclopropylethyl)amino group, ((1-hydroxycyclobutyl)methyl)amino group, (1-hydroxy-4-methylpentan-2-yl)amino group, (1,3-dihydroxybutan-2-yl)amino group, (2,2-dimethylcyclopropyl)methyl]amino group, (dicyclopropylmethyl)amino group, (3-hydroxycyclobutyl)amino group, [1-(hydroxymethyl)cyclobutyl]methyl group, cyclopentylamino group, (2-hydroxycyclopentyl)amino group, (cyclopentyl)(methyl) )amino group, (4-hydroxycyclohexyl)amino group, bicyclo[2.2.1]heptan-2-yl]amino group, [(3-methyloxetan-3-yl)methyl]amino group, (oxetan-3-yl)amino group, (oxolan-3-yl)methyl)amino group, (tetrahydrofuran-2-ylmethyl)amino group, (oxan-4-yl)amino group, ((oxan-4-yl)methyl)amino group, ((4-methyloxan-4-yl)methyl)amino group, (3-methyloxetan-3-yl)methyl]amino group, [(5-oxopyrrolidin-2-yl)methyl ethyl]amino group, [(6-oxopiperidin-3-yl)methyl]amino group, [(1-methyl-1H-imidazol-2-yl)methyl]amino group, [2-(1H-pyrazol-1-yl)ethyl]amino group, [2-(1H-imidazol-5-yl)ethyl]amino group, (3-(1H-imidazol-1-yl)propyl)amino group, [(1-methyl-1H-pyrazol-5-yl)methyl]amino group, [(1H-pyrazol-3-yl)methyl]amino group, [(1-methyl-1H-pyrazol-3-yl)methyl]amino group, [(1-methyl-1H-pyrazol-4-yl)methyl]amino group, [(pyrazin-2-yl)methyl]amino group, [(pyridin-3-yl)methyl]amino group, [(pyrimidin-5-yl)methyl]amino group, [(pyrimidin-2-yl)methyl]amino group Selected from: Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0255] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides an aryl group R 3 is a phenyl group optionally substituted with one or two fluorine atoms, chlorine atoms or trifluoromethyl groups, as well as their stereoisomers, tautomers, N-oxides, hydrates, solvates and salts, and mixtures thereof.

[0256] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides an aryl group R 3 is a phenyl group substituted with a fluorine atom, as well as its stereoisomers, tautomers, N-oxides, hydrates, solvates and salts, and mixtures thereof.

[0257] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 but a phenyl group optionally substituted with 1, 2 or 3 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, or a NR 5 R 6 independently selected from the group optionally halogen atoms, C1-C3-alkyl groups, cyano groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group (provided that the monocyclic heteroaryl group is not a pyridin-4-yl group); and N.R. 7 R 8 base and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0258] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 but optionally halogen atoms, C1-C3-alkyl groups, cyano groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and NR 5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group; or NR 7 R 8 base and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0259] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 but optionally halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups and NR 5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0260] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 but substituted heterocycloalkyl groups such as 4,4-difluoropiperidin-1-yl groups; partially unsaturated heterocycloalkyl groups such as 2,5-dihydrofuran-3-yl groups; substituted phenyl groups such as a 4-fluorophenyl group, a 3,4-difluorophenyl group, and a 4-chlorophenyl group; substituted heteroaryl groups such as a 1,2-thiazol-4-yl group, a 2-methyl-1,3-thiazol-5-yl group, a 1-(difluoromethyl)-1H-pyrazol-4-yl group, a 3-(trifluoromethyl)-1H-pyrazol-1-yl group, a 5-chloropyridin-2-yl group, a 2-aminopyridin-4-yl group, a (morpholin-4-yl)methyl group, a 2-hydroxy-2-methylpropyl group, a 2-methylpropyl group, a pyrazin-2-yl)methyl group, or a 3-hydroxy-3-methylazetidin-1-yl group; and NR groups such as 4-(propylamino), 4-(cyclopentylamino; [3-hydroxycyclobutyl]amino, [3,3,3-trifluoro-2-hydroxypropyl]amino, and 2-methoxyethyl)amino groups 7 R 8 base and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0261] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3is a C1-C6-alkyl group optionally substituted with one or two substituents, each substituent being independently selected from a hydroxy group, a C1-C4-alkoxy group and a 3- to 7-membered heterocycloalkyl group, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0262] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 is a C2-C6-alkenyl group optionally substituted with a C1-C4-alkoxy group, as well as its stereoisomers, tautomers, N-oxides, hydrates, solvates and salts, and mixtures thereof.

[0263] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 is a C3-C9-cycloalkyl group optionally substituted with a hydroxy group, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof. In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides compounds of formula (I) above, wherein R 3 is a C5-C9-cycloalkenyl group optionally substituted with a hydroxy group, C5:150, 201, C7:154 (bridged), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof. In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides compounds of formula (I) above, wherein R 3 -O-, -S-, -S(O)-, S(O)2 and -NR 9 - a 3- to 9-membered heterocycloalkyl group containing 1, 72, 234, 239, 2, 207, or 3 heteroatoms independently selected from: In some cases, -O-, -NR 9 -, -CH2-, -CH2-CH2-, -O-CH2-, -CH2-O-, -NR 9 -CH2- and -CH2-NR 9-, and may further comprise a bridging group selected from optionally substituted with 1, 18, 239, 243, 275, 2 or 3 substituents, each of which is halogen atoms; oxo (=O) group; cyano group; hydroxy groups; C1-C3-alkyl groups optionally substituted with 1, 2 or 3 substituents, the substituents being independently selected from hydroxy groups; C1-C3-haloalkyl group; C1-C3-alkoxy groups; C1-C3-haloalkoxy group; C1-C3-hydroxyalkoxy group; C(O)NR 5 R 6 groups and NR 5 R 6 basis and the stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0264] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 is partially unsaturated and optionally substituted with 1, 2 or 3 substituents, -O-, -S- and -NR 9 In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides compounds of formula (I) above, wherein R is a 5-9 membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from the group consisting of: 3 but, an aryl group optionally substituted with 1, 3 or 4 substituents, each of which is halogen atoms, hydroxy groups, cyano group, C1-C3-alkyl groups, C1-C3-haloalkyl group, C1-C3-alkoxy group, C1-C3-haloalkoxy groups, and NR 5 R 6 basis (independently selected from In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound of formula (I) above, wherein R 3 is a monocyclic or bicyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms, C1-C3-alkyl groups, cyano group, C1-C3-haloalkyl group, C1-C3-alkoxy group, hydroxy groups, and NR 5 R 6 basis and the stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0265] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 is partially unsaturated and optionally substituted with 1, 2 or 3 substituents, -O-, -S- and -NR 9 In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides compounds of formula (I) above, wherein R is a 5-9 membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from the group consisting of: 3 but, an aryl group optionally substituted with 1, 3 or 4 substituents, each of which is halogen atoms, hydroxy groups, cyano group, C1-C3-alkyl groups, C1-C3-haloalkyl group, C1-C3-alkoxy group, C1-C3-haloalkoxy groups, and NR 5 R 6 basis (independently selected from In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound of formula (I) above, wherein R 3 is a monocyclic or bicyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms, C1-C3-alkyl groups, cyano group, C1-C3-haloalkyl group, C1-C3-alkoxy group, hydroxy groups, and NR 5 R 6 basis (independently selected from the heterocycloalkyl group is a 6-membered ring; Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0266] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 is partially unsaturated and optionally substituted with 1, 2 or 3 substituents, -O-, -S- and -NR 9In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides compounds of formula (I) above, wherein R is a 5-9 membered heterocycloalkyl group containing 1, 2, or 3 heteroatoms independently selected from the group consisting of: 3 but, an aryl group optionally substituted with 1, 3 or 4 substituents, each of which is halogen atoms, hydroxy groups, cyano group, C1-C3-alkyl groups, C1-C3-haloalkyl group, C1-C3-alkoxy group, C1-C3-haloalkoxy groups, and NR 5 R 6 basis (independently selected from In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound of formula (I) above, wherein R 3 is a monocyclic or bicyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents, each of which is halogen atoms, C1-C3-alkyl groups, cyano group, C1-C3-haloalkyl group, C1-C3-alkoxy group, hydroxy groups, and NR 5 R 6 basis (independently selected from the heterocycloalkyl group is a 5-membered ring; Provided are compounds of formula (I) above, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0267] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 NR 7 R 8 The present invention provides compounds of formula (I) above, which are a group, as well as stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof.

[0268] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 NR 7 R 8 is a group; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6 alkyl groups which is optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, C(O)NR 5 R 6 group, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally substituted by 1 or 2 substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; a 3- to 7-membered heterocycloalkyl group, which itself is optionally substituted by a C1-C3-alkyl group or an oxo (=O) group; Heteroaryl groups which themselves are optionally substituted by C1-C3-alkyl groups (independently selected from -C1-C5-alkylene-O-C1-C5-alkyl group, -C1-C5-alkylene-S-C1-C5-alkyl group, -C1~C5-Alkylene-NR 5 -C1 to C5 alkyl group, C3-C6-cycloalkyl groups optionally substituted by hydroxy groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein the compound is independently selected from the group consisting of:

[0269] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a compound comprising: R 3 NR 7 R 8 It is a base; R 7 / R 8 but Hydrogen atom (However, R 7 =R 8 = hydrogen is excluded), C1-C6-alkyl groups, which are optionally substituted with 1, 2, 3 or 4 substituents, Halogen atoms, cyano groups, hydroxy groups, C(O)NR 5 R 6 group, NR 5 R 6 basis, C1-C3-alkoxy group, C3-C7-cycloalkyl groups optionally further substituted with one or two substituents, the substituents being independently selected from C1-C3-alkyl groups, oxo (=O) groups, hydroxy groups and C1-C3-hydroxyalkyl groups; -O- and -NR, optionally further substituted with C1-C3-alkyl groups 9 a 3- to 7-membered heterocycloalkyl group containing 1, 2 or 3 heteroatoms independently selected from: Heteroaryl groups optionally further substituted with C1-C3-alkyl groups (independently selected from C3-C7-cycloalkyl groups optionally substituted by hydroxy groups or C1-C3-alkyl groups, and a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being independently selected from a C1-C3 alkyl group and a hydroxy group; and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof, wherein the compound is independently selected from the group consisting of:

[0270] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 but halogen atoms, C2-C6-alkenyl group, C3-C6-cycloalkyl group, C5-C6-cycloalkenyl group, C3-C7-heterocycloalkyl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom and a C1-C3-alkyl group, a hydroxy group, NR 5 R 6 group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group), partially unsaturated, optionally substituted C5-C7-heterocycloalkyl groups with 1, 2 or 3 substituents, each of which is independently selected from an oxo group (=O), a C1-C3-alkyl group and a halogen atom; aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, or an NR 5 R 6 independently selected from the group Monocyclic or bicyclic heteroaryl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, a C1-C3-alkyl group, a cyano group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group, a hydroxy group or an NR 5 R 6 independently selected from the group and N.R. 7 R8 basis That is, A compound of formula (I) above is provided.

[0271] In another embodiment of the first aspect or any embodiment derived therefrom, the present invention provides a method for treating a cancer cell comprising: R 3 is a C2-C6 alkenyl group, C3-C6-cycloalkyl group, C5-C6-cycloalkenyl group, C3-C7-heterocycloalkyl groups optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom and a C1-C3-alkyl group, a hydroxy group, NR 5 R 6 group, a C1-C3-haloalkyl group, and a C1-C3-haloalkoxy group), partially unsaturated, optionally substituted C5-C7-heterocycloalkyl groups with 1, 2 or 3 substituents, each of which is independently selected from an oxo group (=O), a C1-C3-alkyl group and a halogen atom; aryl groups optionally substituted with 1, 2, 3 or 4 substituents, each of which may be a halogen atom, a hydroxy group, a cyano group, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-...

Claims

1. Compounds of formula (I) 【Chemistry 1】 (In the formula, R 1 is a hydrogen atom, a halogen atom, a cyano group, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and C 1 ~C 3 - haloalkoxy groups; R 2 is selected from a hydrogen atom and a halogen atom; R 3 is (i) to (ix) below: (i) C optionally substituted with 1 or 2 substituents 1 ~C 6 -Alkyl group (each substituent is a hydroxyl group, C 1 ~C 4 - independently selected from alkoxy groups and 3- to 7-membered heterocycloalkyl groups; (ii) In some cases, C 1 ~C 4 - C substituted with an alkoxy group 2 ~C 6 -alkenyl group; (iii) C optionally substituted with a hydroxy group 3 ~C 9 -cycloalkyl group; (iv) C optionally substituted with a hydroxy group 5 ~C 9 -cycloalkenyl group; (v)-O-, -S-, -S(O)-, -S(O) 2 --and--NR 9 - 3-9 membered heterocycloalkyl groups containing 1, 2 or 3 atomic groups independently selected from In some cases, -O-, -NR 9 -, -CH 2 -, -CH 2 -CH 2 -, -O-CH 2 -, -CH 2 -O-, -NR 9 -CH 2 - and -CH 2 -NR 9 -, further comprising a bridging group selected from Optionally substituted with 1, 2 or 3 substituents, each of which is selected from the following (a) to (j): (a) a halogen atom; (b) an oxo (=O) group; (c) a cyano group; (d) a hydroxy group; (e) C optionally further substituted with a hydroxy group 1 ~C 3 - alkyl group; (f)C 1 ~C 3 - haloalkyl group; (g) C 1 ~C 3 -alkoxy group; (h)C 1 ~C 3 - a haloalkoxy group; (i) C(O)NR 5 R 6 Groups; and (j)NR 5 R 6 base a 3- to 9-membered heterocycloalkyl group independently selected from: (vi) A partially unsaturated 5- to 9-membered heterocycloalkyl group, optionally substituted with 1, 2 or 3 substituents, each of which is an oxo group (=O), C 1 ~C 3 -Alkyl group, -C(O)R 5 R 6 groups and halogen atoms; (vii) an aryl group optionally substituted with 1, 2, 3 or 4 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -alkoxy group, C 1 ~C 3 -haloalkoxy group and NR 5 R 6 (independently selected from the group consisting of aryl, aryloxy ... (viii) a monocyclic or bicyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, C 1 ~C 3 -Alkyl group, cyano group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -Hydroxyalkyl group, C 1 ~C 3 -Alkoxy group, hydroxy group and NR 5 R 6 with the proviso that said optionally substituted monocyclic heteroaryl group is not 4-pyridyl; and (ix)NR 7 R 8 base Selected from: R 4 is a hydrogen atom and C 1 ~C 3 - alkyl groups; R 5 / R 6 is a hydrogen atom, C 1 ~C 6 -Alkyl group, -C 1 ~C 5 -Alkylene-O-C 1 ~C 5 -Alkyl group, -C 1 ~C 5 -Alkylene-S-C 1 ~C 5 -Alkyl group, C 3 ~C 6 -Cycloalkyl groups and C 3 ~C 5 - independently selected from heterocycloalkyl groups; R 7 / R 8 means (i) to (vi) of the following: (i) a hydrogen atom (wherein R 7 = R 8 = hydrogen is excluded); (ii) C 1 ~C 6 -Alkyl group which is optionally substituted with 1, 2, 3 or 4 substituents, the substituents being selected from the following (a) to (i): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; (d)C(O)NR 5 R 6 base; (e)NR 5 R 6 base; (f)C 1 ~C 3 -alkoxy group; (g) C optionally substituted with 1 or 2 substituents 3 ~C 7 -Cycloalkyl group (said substituents are C 1 ~C 3 -Alkyl group, oxo (=O) group, hydroxy group and C 1 ~C 3 -hydroxyalkyl groups; (h) Itself may be C 1 ~C 3 - a 3- to 7-membered heterocycloalkyl group substituted with an alkyl or oxo (=O) group; and (i) It may itself be C 1 ~C 3 - Heteroaryl group substituted with alkyl group (independently selected from); (iii)-C 1 ~C 5 -Alkylene-O-C4~C 5 - alkyl group; (iv)-C 1 ~C 5 -Alkylene-S-C 1 ~C 5 - alkyl group; (v) C optionally substituted with a hydroxy group 3 ~C 6 -cycloalkyl group; and (vi) a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being C 1 ~C 3 independently selected from alkyl groups and hydroxy groups. are independently selected from R 9 is a hydrogen atom or C 1 ~C 3 -alkyl group or a bond) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

2. R 1 is a hydrogen atom, a halogen atom, a cyano group, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and C 1 ~C 3 - haloalkoxy groups; R 2 is selected from a hydrogen atom and a halogen atom; R 3 However, the following (i) to (ix): (i) optionally a hydroxy group, C 1 ~C 4 - C substituted with a substituent selected from an alkoxy group and a 3- to 7-membered heterocycloalkyl group 1 ~C 6 - alkyl group; (ii) C, if necessary 1 ~C 4 - C substituted with an alkoxy group 2 ~C 6 -alkenyl group; (iii) C optionally substituted with a hydroxy group 3 ~C 7 -cycloalkyl group; (iv) C optionally substituted with a hydroxy group 5 ~C 7 -cycloalkenyl group; (v) -O-, -S(O) 2 --and--NR 9 - 3- to 7-membered heterocycloalkyl groups containing 1 or 2 atomic groups independently selected from Optionally substituted with one or two substituents, each of which is selected from the following (a) to (g): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; (d) C optionally further substituted with a hydroxy group 1 ~C 3 - alkyl group; (e)C 1 ~C 3 -alkoxy group; (f)C(O)NR 5 R 6 Groups; and (g)NR 5 R 6 base a 3- to 7-membered heterocycloalkyl group independently selected from: (vi) partially unsaturated, optionally with C 1 ~C 3 -O-, -S- and -NR substituted with a substituent selected from an alkyl group and a halogen atom; 9 -; a 5- to 7-membered heterocycloalkyl group containing an atomic group selected from -; (vii) an aryl group optionally substituted with one, two or three substituents, each of which is a halogen atom, a hydroxyl group, a cyano group, 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -alkoxy group and NR 5 R 6 independently selected from the group (viii) optionally a halogen atom, C 1 ~C 3 -Alkyl group, cyano group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -alkoxy group and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group consisting of the following: (with the proviso that the monocyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents is not a pyridin-4-yl group); and (ix)NR 7 R 8 base Selected from: R 4 is hydrogen atom and C 1 ~C 3 - alkyl groups; R 5 / R 6 is hydrogen atom and C 1 ~C 6 - independently selected from alkyl groups; R 7 / R 8 However, the following (i) to (iv): (i) a hydrogen atom (wherein R 7 = R 8 = Hydrogen is excluded), (ii) C 1 ~C 6 an alkyl group, which is optionally substituted with 1, 2, 3 or 4 substituents, the substituents being selected from the following (a) to (i): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; (d)C(O)NR 5 R 6 base; (e)NR 5 R 6 base; (f)C 1 ~C 3 -alkoxy group; (g) C optionally further substituted with one or two substituents 3 ~C 7 -Cycloalkyl group (said substituents are C 1 ~C 3 -Alkyl group, oxo (=O) group, hydroxy group and C 1 ~C 3 -hydroxyalkyl groups; (h) In some cases, C 1 ~C 3 -O- and -NR further substituted with alkyl groups 9 - 3- to 7-membered heterocycloalkyl groups containing 1, 2 or 3 groups independently selected from: (i) In some cases, C 1 ~C 3 - a heteroaryl group further substituted with an alkyl group (independently selected from); (iii) optionally a hydroxy group or C 1 ~C 3 -C substituted with alkyl group 3 ~C 7 -cycloalkyl groups, and (iv) a 3- to 6-membered heterocycloalkyl group, optionally substituted with one or two substituents, the substituents being C 1 ~C 3 independently selected from alkyl groups and hydroxy groups. are independently selected from R 9 is a hydrogen atom or C 1 ~C 3 - an alkyl group or a bond, 2. The compound of claim 1, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

3. R 1 is a hydrogen atom, halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and C 1 ~C 3 - haloalkoxy groups; R 2 is selected from a hydrogen atom and a halogen atom; R 3 However, the following (i) to (ix): (i) optionally a hydroxy group, C 1 ~C 4 - C substituted with a substituent selected from an alkoxy group and a 3- to 7-membered heterocycloalkyl group 1 ~C 6 - alkyl group; (ii) C, if necessary 1 ~C 4 - C substituted with an alkoxy group 2 ~C 6 -alkenyl group; (iii) C optionally substituted with a hydroxy group 3 ~C 7 -cycloalkyl group; (iv) C 5 ~C 7 -cycloalkenyl group; (v) -O- and -NR 9 - 3- to 7-membered heterocycloalkyl groups containing 1 or 2 atomic groups independently selected from Optionally, further substituted with one or two substituents, each of which is selected from the following (a) to (f): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; (d) C optionally further substituted with a hydroxy group 1 ~C 3 - alkyl group; (e)C 1 ~C 3 -alkoxy groups; and (f)C(O)NR 5 R 6 base a 3- to 7-membered heterocycloalkyl group independently selected from: (vi) partially unsaturated, optionally with C 1 ~C 3 -O- and -NR substituted with a substituent selected from an alkyl group and a halogen atom; 9 -; a 5- to 7-membered heterocycloalkyl group containing an atomic group selected from -; (vii) an aryl group optionally substituted with one, two or three substituents, each of which is a halogen atom, a hydroxyl group, a cyano group, 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and NR 5 R 6 (independently selected from the group consisting of aryl, aryloxy ... (viii) optionally a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -alkoxy group and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group consisting of the following: (with the proviso that the monocyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents is not a pyridin-4-yl group); and (ix)NR 7 R 8 base Selected from: R 4 is hydrogen atom and C 1 ~C 3 - alkyl groups; R 5 / R 6 is hydrogen atom and C 1 ~C 6 - independently selected from alkyl groups; R 7 / R 8 However, the following (i) to (iv): (i) a hydrogen atom (wherein R 7 = R 8 = Hydrogen is excluded), (ii) C 1 ~C 6 an alkyl group, which is optionally substituted with 1, 2, 3 or 4 substituents, the substituents being selected from the following (a) to (h): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; (d)NR 5 R 6 base; (e)C 1 ~C 3 -alkoxy group; (f) C optionally further substituted with one or two substituents 3 ~C 7 -Cycloalkyl group (said substituents are C 1 ~C 3 -Alkyl group, oxo (=O) group, hydroxy group and C 1 ~C 3 -hydroxyalkyl groups; (g) In some cases, C 1 ~C 3 -O- and -NR further substituted with alkyl groups 9 - 3- to 7-membered heterocycloalkyl groups containing 1, 2 or 3 groups independently selected from: (h) C, if necessary 1 ~C 3 - a heteroaryl group further substituted with an alkyl group (independently selected from); (iii) optionally a hydroxy group or C 1 ~C 3 -C substituted with alkyl group 3 ~C 7 -cycloalkyl groups, and (iv) a 3- to 6-membered heterocycloalkyl group, optionally substituted with one or two substituents, the substituents being C 1 ~C 3 independently selected from alkyl groups and hydroxy groups. are independently selected from R 9 is a hydrogen atom or C 1 ~C 3 - an alkyl group or a bond, 2. The compound of claim 1, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

4. R 1 is a hydrogen atom, halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and C 1 ~C 3 - haloalkoxy groups; R 2 is selected from a hydrogen atom and a halogen atom; R 3 However, the following (i) to (ix): (i) optionally a hydroxy group, C 1 ~C 4 - C substituted with a substituent selected from an alkoxy group and a 3- to 7-membered heterocycloalkyl group 1 ~C 6 - alkyl group; (ii) C, if necessary 1 ~C 4 - C substituted with an alkoxy group 2 ~C 6 -alkenyl group; (iii) C optionally substituted with a hydroxy group 4 ~C 6 -cycloalkyl group; (iv) C 5 ~C 7 -cycloalkenyl group; (v) -O- and -NR 9 - 3-6 membered heterocycloalkyl groups containing 1 or 2 atomic groups independently selected from Optionally, further substituted with one or two substituents, each of which is selected from the following (a) to (d): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; and (d) C optionally further substituted with a hydroxy group 1 ~C 3 -Alkyl group a 3- to 6-membered heterocycloalkyl group independently selected from: (vi) partially unsaturated, optionally with C 1 ~C 3 -O- and -NR substituted with a substituent selected from an alkyl group and a halogen atom; 9 -; a 5- to 6-membered heterocycloalkyl group containing an atomic group selected from -; (vii) an aryl group optionally substituted with one or two substituents, each of which is a halogen atom, a hydroxyl group, a cyano group, 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and NR 5 R 6 independently selected from the group (viii) optionally a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -alkoxy group and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group consisting of the following: (with the proviso that the monocyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents is not a pyridin-4-yl group); and (ix)NR 7 R 8 base Selected from: R 4 is hydrogen atom and C 1 ~C 3 - alkyl groups; R 5 / R 6 is hydrogen atom and C 1 ~C 6 - independently selected from alkyl groups; R 7 / R 8 However, the following (i) to (iv): (i) a hydrogen atom (wherein R 7 = R 8 = hydrogen is excluded); (ii) C 1 ~C 6 an alkyl group, which is optionally substituted with 1, 2, 3 or 4 substituents, the substituents being selected from the following (a) to (f): (a) a halogen atom; (b) a hydroxy group; (c)C 1 ~C 3 -alkoxy group; (d) C optionally further substituted with one or two substituents 3 ~C 6 -Cycloalkyl group (said substituents are C 1 ~C 3 -Alkyl groups and C 1 ~C 3 -hydroxyalkyl groups; (e) In some cases, C 1 ~C 3 -O- and -NR further substituted with alkyl groups 9 - 4-6 membered heterocycloalkyl groups containing 1, 2 or 3 groups independently selected from: (f) In some cases, C 1 ~C 3 - a heteroaryl group further substituted with an alkyl group (independently selected from); (iii) optionally a hydroxy group or C 1 ~C 3 -C substituted with alkyl group 3 ~C 6 -cycloalkyl group; and (iv) a 3- to 6-membered heterocycloalkyl group, optionally substituted with one or two substituents, the substituents being C 1 ~C 3 independently selected from alkyl groups and hydroxy groups. are independently selected from R 9 is a hydrogen atom or C 1 ~C 3 - an alkyl group or a bond, 2. The compound of claim 1, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

5. R 1 is a hydrogen atom, halogen atom, C 1 ~C 3 -Alkyl groups and C 1 ~C 3 - haloalkyl groups; R 2 is selected from a hydrogen atom and a halogen atom; R 3 However, the following (i) to (ix): (i) C optionally substituted with 1 or 2 substituents 1 ~C 6 -Alkyl group (each substituent is a hydroxyl group, C 1 ~C 4 - independently selected from alkoxy groups and 3- to 7-membered heterocycloalkyl groups; (ii) In some cases, C 1 ~C 3 - C substituted with an alkoxy group 2 ~C 6 -alkenyl group; (iii) C optionally substituted with a hydroxy group 3 ~C 7 -cycloalkyl group; (iv) C optionally substituted with a hydroxy group 5 ~C 6 -cycloalkenyl group; (v) -O- and -NR 9 - 3-6 membered heterocycloalkyl groups containing 1, 2 or 3 atomic groups independently selected from Optionally substituted with 1, 2 or 3 substituents, each of which is selected from the following (a) to (e): (a) a halogen atom; (b) an oxo (=O) group; (c) a cyano group; (d) a hydroxy group; and (e) C optionally further substituted with a hydroxy group 1 ~C 3 -Alkyl group a 3- to 6-membered heterocycloalkyl group independently selected from: (vi) a partially unsaturated 5- to 7-membered heterocycloalkyl group, optionally substituted with one or two substituents, each of which is C 1 ~C 3 - independently selected from alkyl groups and halogen atoms; (vii) an aryl group optionally substituted with 1, 2, 3 or 4 substituents, each of which is a halogen atom, a hydroxy group, a cyano group, 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -alkoxy group, C 1 ~C 3 -haloalkoxy group and NR 5 R 6 independently selected from the group (viii) Monocyclic or bicyclic heteroaryl groups optionally substituted with one or two substituents, each of which may be a halogen atom, C 1 ~C 3 -Alkyl group, cyano group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -Alkoxy group, hydroxy group and NR 5 R 6 with the proviso that said optionally substituted monocyclic heteroaryl group is not a pyridin-4-yl group; and (ix)NR 7 R 8 base Selected from: R 4 is hydrogen atom and C 1 ~C 3 - alkyl groups; R 5 / R 6 is hydrogen atom and C 1 ~C 6 - independently selected from alkyl groups; R 7 / R 8 However, the following (i) to (iv): (i) a hydrogen atom (wherein R 7 = R 8 = hydrogen is excluded); (ii) C 1 ~C 6 an alkyl group, which is optionally substituted with 1, 2, 3 or 4 substituents, the substituents being selected from the following (a) to (g): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; (d) C 1 ~C 3 -alkoxy group; (e) C optionally substituted with 1 or 2 substituents 3 ~C 7 -Cycloalkyl group (said substituents are C 1 ~C 3 -Alkyl groups, hydroxyl groups and C 1 ~C 3 -hydroxyalkyl groups; (f) Itself may be C 1 ~C 3 -3 to 7 membered heterocycloalkyl groups substituted with alkyl groups; and (g) In some cases, C 1 ~C 3 - a heteroaryl group further substituted with an alkyl group (independently selected from); (iii) C optionally substituted with a hydroxy group 3 ~C 6 -cycloalkyl group; and (iv) a 3- to 6-membered heterocycloalkyl group, optionally substituted with one or two substituents, the substituents being C 1 ~C 3 independently selected from alkyl groups and hydroxy groups. are independently selected from R 9 is a hydrogen atom or C 1 ~C 3 - an alkyl group or a bond, 2. The compound of claim 1, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

6. R 1 is a hydrogen atom, halogen atom, C 1 ~C 3 -Alkyl groups and C 1 ~C 3 - haloalkyl groups; R 2 is selected from a hydrogen atom and a halogen atom; R 3 However, the following (i) to (iv): (i) -O- and -NR 9 -, A 3- to 6-membered heterocycloalkyl group optionally further substituted with one or two substituents, each of which is selected from the group Halogen atoms; Hydroxy groups; and C optionally further substituted with hydroxy groups 1 ~C 3 -Alkyl group (independently selected from); (ii) an aryl group optionally substituted with one or two substituents, each of which is a halogen atom, a hydroxyl group, or a C 1 ~C 3 -haloalkyl groups; (iii) optionally a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and NR 5 R 6 a monocyclic or bicyclic heteroaryl group substituted with a substituent selected from the group consisting of the following: (with the proviso that the monocyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents is not a pyridin-4-yl group); and (iv)NR 7 R 8 base Selected from: R 4 is hydrogen atom and C 1 ~C 3 - alkyl groups; R 5 / R 6 is hydrogen atom and C 1 ~C 3 - independently selected from alkyl groups; R 7 / R 8 However, the following (i) to (iv): (i) a hydrogen atom (wherein R 7 = R 8 = hydrogen is excluded); (ii) C 1 ~C 6 an alkyl group, which is optionally substituted with 1 or 2, 3 or 4 substituents, the substituents being selected from the following (a) to (f): (a) a halogen atom; (b) a hydroxy group; (c)C 1 ~C 3 -alkoxy group; (d) C optionally further substituted with one or two substituents 3 ~C 5 -Cycloalkyl group (said substituents are C 1 ~C 3 -Alkyl groups and C 1 ~C 3 -hydroxyalkyl groups; (e) In some cases, C 1 ~C 3 -O- and -NR further substituted with alkyl groups 9 -, ... (f) In some cases, C 1 ~C 3 - a heteroaryl group further substituted with an alkyl group (independently selected from); (iii) optionally a hydroxy group or C 1 ~C 3 -C substituted with alkyl group 3 ~C 6 -cycloalkyl group; and (iv) a 4- to 5-membered heterocycloalkyl group, optionally substituted with one or two substituents, the substituents being C 1 ~C 3 independently selected from alkyl groups and hydroxy groups. are independently selected from R 9 is a hydrogen atom or C 1 ~C 3 - an alkyl group or a bond, 2. The compound of claim 1, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

7. R 1 CF 3 and a fluorine atom; R 2 is a hydrogen atom; R 3 However, the following (i) to (iii): (i) optionally a halogen atom and C 1 ~C 3 - an aryl group substituted with a substituent selected from haloalkyl groups; (ii) C 1 ~C 3 -Haloalkyl groups and NR 5 R 6 a monocyclic heteroaryl group substituted with a substituent selected from the group (iii)NR 7 R 8 base Selected from: R 4 is selected from a hydrogen atom and a methyl group; R 5 / R 6 are independently selected from a hydrogen atom and a methyl group; R 7 / R 8 However, the following (i) to (ii): (i) a hydrogen atom (wherein R 7 = R 8 = hydrogen is excluded); and (ii) C 1 ~C 3 an alkyl group, which is optionally substituted with 1, 2 or 4 substituents, said substituents being independently selected from halogen atoms, hydroxy groups and methoxy groups; are independently selected from 2. The compound of claim 1, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

8. The following groups: 5-[4-(4,4-difluoropiperidin-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (1), 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (3), 5-[3-fluoro-4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (4), 5-[3-fluoro-4-(4-fluoro-4-methylpiperidin-1-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (5), 5-[3-fluoro-4-(4-fluoropiperidin-1-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (6), 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (7), 5-(3',4'-difluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (8), 5-(4'-fluoro-2,2'-dimethylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (9), 5-[4-(3,6-dihydro-2H-pyran-4-yl)-3-methylphenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (10), 5-[3-methyl-4-(1H-pyrazol-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (11), 5-[3-methyl-4-(6-oxo-1,6-dihydropyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (12), 5-[3-methyl-4-(pyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (13), 5-[3-methyl-4-(pyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (14), 5-(3'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (15), (rac)-6-methyl-5-(3,4,5-trifluorophenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (16), (rac)-5-[3,5-difluoro-4-(morpholin-4-yl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (17), (rac)-5-{3,5-difluoro-4-[(2S)-2-methylmorpholin-4-yl]phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (18), (rac)-6-methyl-5-[4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (20), 5-[3,5-difluoro-4-(morpholin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (21), 2-(morpholin-4-yl)-5-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)benzonitrile (22), 3-chloro-2-(morpholin-4-yl)-5-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)benzonitrile (23), 5-{4-[2,6-dimethylmorpholin-4-yl]-3-fluorophenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (24), (6S)-5-(3-fluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (25-1), (6S)-5-(3,5-difluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (25-2), 5-[4-(3,3-difluoropyrrolidin-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (26), 5-(2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (27), 5-[3-methyl-4-(2-methylpyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (28), 5-[3-methyl-4-(1-methyl-1H-pyrazol-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (29), 5-(2,4'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (30), 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (31), 5-[4-(6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (32), 5-[4-(pyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (33), 5-[4'-amino-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (34), 5-[3'-hydroxy-4'-methyl-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (35), 5-{3-(trifluoromethyl)-4-[6-(trifluoromethyl)pyridin-3-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (36), 5-[4'-fluoro-3'-hydroxy-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (37), 5-[5'-amino-2',4'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (38), 5-[4'-amino-3'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (39), 5-[4-(6-aminopyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (40), 5-[3'-amino-4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (41), 5-[3'-amino-4'-methyl-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (42), 5-[3'-amino-2'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (43), 5-[4'-amino-2'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (44), 5-[4-(1-methyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (45), 5-[4-(3-methyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (46), 5-[4-(1H-indazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (47), 5-[4-(5-fluoro-6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (48), 5-[4-(1,2-thiazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (49), 1-Methyl-5-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]-1H-pyrrole-2-carbonitrile (50), 5-[2,4'-bis(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (51), 5-[4-(1,3-dimethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (52), 5-[4-(2-methoxy-6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (53), 5-[4-(2-methyl-1,3-thiazol-5-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (54), 5-[4'-(methylamino)-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (55), 5-[3'-amino-4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (56), 5-[4-fluoro-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (57), 5-[3',4',5'-trifluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (58), 5-[2',5'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (59), 5-[3'-amino-4'-fluoro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (60), 5-[3',4'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (61), 5-[4-(1H-indol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (62), 5-[4-(2-methylprop-1-en-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (63), 5-[2',3'-difluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (64), 5-[4-(morpholin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (65), 5-[4-(butylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (66), 5-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (67), 5-[4-(1-methyl-1H-pyrazol-4-yl)-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (68), 5-[4-(propylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (69), 5-[4-(6-methylpyridin-3-yl)-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (70), 5-[4'-chloro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (71), 5-[4-(azetidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (72), 5-[4-(1-methyl-1H-benzimidazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (73), 5-[4-(pentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (74), 5-[4-(1-methyl-1H-indazol-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (75), 5-[4'-fluoro-2-(trifluoromethoxy)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (76), 5-[3-fluoro-4-(6-fluoropyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (77), 5-[3-fluoro-4-(3-methylpyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (78), 5-[3-fluoro-4-(2-methylpyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (79), 5-(4'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (80), 5-(2-fluoro-2'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (81), 5-(2'-chloro-2,4'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (82), 5-[4-(cyclopent-1-en-1-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (83), 5-(2'-ethyl-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (84), 5-[3-fluoro-4-(6-methoxypyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (85), 5-(2,4'-difluoro-3'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (86), 5-(2-fluoro-3'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (87), 5-(2-fluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (88), 5-(2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (89), 5-[4-(2-aminopyridin-4-yl)-3-fluorophenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (90), 5-(3'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (91), 5-[4'-(difluoromethyl)-2-fluorobiphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (92), 5-[3-fluoro-4-(2-methylpyrimidin-5-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (94), 5-[3-fluoro-4-(2-methoxypyridin-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (95), 5-[3-fluoro-4-(2-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (96), 5-[3-fluoro-4-(6-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (97), 5-(2,2',4',5'-tetrafluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (98), 5-(2,2',3',4'-tetrafluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (99), 5-(2,2',5'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (100), 2'-fluoro-4'-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)biphenyl-4-carbonitrile (101), 5-(2'-amino-2-fluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (102), 5-(3'-amino-2-fluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (103), 5-(2-fluoro-3'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (104), 5-(2-fluoro-4'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (105), 5-(2-fluoro-2'-hydroxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (106), 5-(2,3',4'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (107), 5-[3-fluoro-4-(pyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (108), 5-(2,2',3'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (109), 5-(2,3',5'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (110), 5-(2,2',4'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (111), 5-(2-fluoro-2',4'-dimethylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (112), 5-(2,3'-difluoro-4'-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (113), 5-(2,2'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (114), 5-(2,2',6'-trifluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (115), 5-(2-fluoro-2'-methoxybiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (116), 5-(2,3'-difluorobiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (117), 5-[3-fluoro-4-(4-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (118), (rac)-5-(3-fluoro-4-morpholinophenyl)-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (119), (6S)-6-methyl-5-[4-(morpholin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (120), (6S)-5-(-[(3-chloro-4-(morpholin-4-yl)-5-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (121), (6S)-5-(-[(4-chloro-3-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (122), (6S)-5-(-[(4-fluoro-3-(trifluoromethyl)phenyl)-)]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (123), 5-[4-chloro-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (124), 5-(4-chloro-3-methylphenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (125), (rac)-6-methyl-5-(4-morpholino-3-(trifluoromethyl)phenyl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (126), 5-{4-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (127), 5-[4-(3,5-dimethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (128), 5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (129), 5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-4-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (130), 5-[4-(1-ethyl-1H-pyrazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (131), 5-{4-[cyclopentyl(methyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (132), 5-[4-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (133), 5-{4-[butyl(methyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (134), (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (135), 5-[4-(cyclopentylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (136), 5-[3'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (138), 5-[4-methyl-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (139), 5-{4-[3-methoxyprop-1-en-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (140), (rac)-5-[4'-hydroxy-2-(trifluoromethyl)-2',3',4',5'-tetrahydro[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (141), 5-[4-(5,6-dihydro-2H-pyran-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (142), 5-[4-(imidazo[1,2-a]pyridin-6-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (143), 5-{4-[3,3-dimethylbut-1-en-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (144), 5-{3-(trifluoromethyl)-4-[5-(trifluoromethyl)thiophen-3-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (145), 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (146), 5-[4-(prop-1-en-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (147), 5-[4-(1-benzothiophen-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (148), 5-[4-(2,5-dihydrofuran-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (149), 5-[4-(cyclopent-1-en-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (150), 5-[4-(1-ethyl-1H-imidazol-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (151), 3-Methyl-5-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]thiophene-2-carbonitrile (152), 5-{4-[1-(propan-2-yl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (153), (rac)-5-[4-(bicyclo[2.2.1]hept-2-en-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (154), 5-[2'-fluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (155), 5-{3-(trifluoromethyl)-4-[5-(trifluoromethyl)thiophen-2-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (156), 5-[4-(5-methylpyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (157), 5-[4-(5-fluoropyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (158), 5-[4-(5-chloropyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (159), 5-[4-(pyridin-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (160), 5-[2'-(difluoromethyl)-2-fluoro[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (161), 5-(2,4'-difluoro-2'-methyl[1,1'-biphenyl]-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (162), 2'-Fluoro-2-methyl-4'-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)[1,1'-biphenyl]-4-carbonitrile (163), 5-[4-(2-methylprop-1-en-1-yl)-3-(trifluoromethoxy)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (164), (6S)-5-[4-(2-aminopyridin-4-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (165), (6S)-6-methyl-5-[4-(6-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (167), (6S)-5-[2'-fluoro-4'-methyl-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (168), (6S)-6-methyl-5-[2',4',5'-trifluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (169), (6S)-6-methyl-5-[2',3',4'-trifluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (170), (6S)-5-[2',5'-difluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (171), 4'-[(6S)-6-methyl-2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl]-2'-(trifluoromethyl)[1,1'-biphenyl]-2-carbonitrile (172), (6S)-5-[4-(1H-indol-5-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (173), (6S)-5-[4'-hydroxy-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (174), (6S)-5-[3'-hydroxy-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (175), (6S)-5-[3'-amino-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (176), (6S)-5-[2',4'-difluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (177), (6S)-5-[3'-fluoro-4'-methyl-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (178), (6S)-5-[2'-fluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (179), (6S)-5-[2'-methoxy-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (180), (6S)-5-[3'-fluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (181), (6S)-6-methyl-5-[4-(4-methylpyridin-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (182), (6S)-6-methyl-5-[4-(3-methylpyridin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (183), (6S)-6-methyl-5-[4-(2-methylpyridin-4-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (184), (6S)-5-[4-(1H-indol-6-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (185), (6S)-5-[4-(6-methoxypyridin-3-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (187), (6S)-5-[4'-methoxy-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (188), (6S)-6-methyl-5-[4'-methyl-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (189), (6S)-5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (190), 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (191), 5-[4'-fluoro-2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (192), 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-fluoro-5-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (193), 5-{3-(difluoromethyl)-4-[1-(difluoromethyl)-1H-pyrazol-4-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (195), (6S)-6-methyl-5-{4-[(morpholin-4-yl)methyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (196), 5-{4-[(morpholin-4-yl)methyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (197), 5-[2-(difluoromethyl)-4'-fluoro[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (198), 5-[4'-chloro-2-(difluoromethyl)[1,1'-biphenyl]-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (199), 5-[3-(difluoromethyl)-4-(6-methylpyridin-3-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (200), 5-[4-(cyclopent-1-en-1-yl)-3-(difluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (201), 5-[3-(difluoromethyl)-4-(1H-pyrazol-4-yl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (202), 5-[4-(3-hydroxy-3-methylazetidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (203), (rac)-5-[4-{[3,3,3-trifluoro-2-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (204), 5-{4-[(oxan-4-yl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (205), 5-[4-{[(cis / trans)-3-hydroxycyclobutyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (206), 5-{4-[(rac)-2,4-dimethylazetidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (207), 5-{4-[(cis or trans)-2,4-dimethylazetidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (208), 5-[4-{[3,3,3-trifluoro-2(S)-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (209), 5-{4-[(2-hydroxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (210), 5-[4-{[(trans)-4-hydroxycyclohexyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (211), 5-{4-[(cyclopropylmethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (212), 5-[4-{[(3-methyloxetan-3-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (213), 5-{4-[(3-methoxypropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (214), 5-[4-({[(rac)-oxolan-2-yl]methyl}amino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (215), 5-[4-{[2(R)-2-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (216), 5-[4-{[(3R)-3-hydroxybutyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (217), 5-[4-{[(2S)-2-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (218), 5-[4-{[(1-hydroxycyclobutyl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (219), 5-{4-[(3-methylbutyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (220), 5-{4-[(2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (221), 5-{4-[(2-methoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (222), 5-{4-[ethyl(methyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (223), 5-[4-(tert-butylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (224), 5-[4-({[(2R)-oxolan-2-yl]methyl}amino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (225), 5-[4-{[(pyrazin-2-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (226), 5-[4-(4-hydroxypiperidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (227), 5-[4-{[(2S)-1-hydroxybutan-2-yl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (228), 5-[4-(3-hydroxypiperidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (racemic mixture) (229), (rac)-1-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]piperidine-3-carboxamide (230), 5-{4-[(3-hydroxy-2,2-dimethylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (231), 5-[4-(4,4-difluoropiperidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (232), 5-[4-{[(1R,2R,4R)-bicyclo[2.2.1]heptan-2-yl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (233), 5-{4-[(3S)-3-hydroxypyrrolidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (234), (rac)-5-{4-[(2-hydroxy-3-methoxypropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (235), 5-[4-{[(1-methyl-1H-pyrazol-5-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (236), 5-[4-{[(1H-pyrazol-3-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (237), 5-[4-{[2-(1H-pyrazol-1-yl)ethyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (238), 1-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]piperidine-4-carbonitrile (239), (rac)-5-{4-[(1-cyclopropylethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (240), (rac)-5-{4-[(2-ethoxypropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (241), (rac)-5-{4-[(2-methoxypropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (242), 5-[4-(3-ethoxyazetidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (243), 5-[4-{[(pyrimidin-2-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (244), 5-[4-{[(oxolan-3-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (racemic mixture) (245), 5-[4-{[(2S)-4-hydroxybutan-2-yl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (246), (rac)-5-[4-{[(6-oxopiperidin-3-yl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (247), (rac)-5-[4-{[(2,2-dimethylcyclopropyl)methyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (248), 5-[4-({[1-(hydroxymethyl)cyclobutyl]methyl}amino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (249), 5-{4-[(2S)-2-(hydroxymethyl)azetidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (250), 3-Methyl-1-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]azetidine-3-carbonitrile (251), 5-[4-(3-azabicyclo[3.1.0]hexan-3-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (252), 5-[4-(4-ethyl-4-hydroxypiperidin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (253), 4-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)anilino]butanenitrile (254), 6-[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]-2λ 6 -Thia-6-azaspiro[3.3]heptane-2,2-dione (255), N 2 -[4-(2-oxo-3,6-dihydro-2H-1,3,4-oxadiazin-5-yl)-2-(trifluoromethyl)phenyl]glycinamide (256), 5-{4-[(3R)-3-hydroxypyrrolidin-1-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (257), 5-{4-[(2-methoxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (258) 5-[4-({[(2S)-oxolan-2-yl]methyl}amino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (259), 5-{4-[(2-ethoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (260), 5-[4-{[(1S,2R)-2-hydroxycyclopentyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (261), 5-{4-[(oxetan-3-yl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (262), 5-{3-(difluoromethyl)-4-[1-(propan-2-yl)-1H-pyrazol-4-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (263), 5-[3-fluoro-4-(morpholin-4-yl)-5-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (264), (6S)-6-Methyl-5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (265), (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[4-(trifluoromethyl)-1H-imidazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (266), 5-[4-(3-methoxypropyl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (267), 5-[4-(2-methylpropyl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (268), 5-[4-(3,3-dimethylbutyl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (269), 5-[4-(propan-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (270), (rac)-5-{4-[oxan-3-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (271), (trans)-5-{4-[4-hydroxycyclohexyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (trans isomer) (272), (cis)-5-{4-[4-hydroxycyclohexyl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (273), 5-{4-[(2-aminoethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one-hydrochloric acid salt (274), 5-{4-[1-amino-3-azabicyclo[3.1.0]hexan-3-yl]-3-(trifluoromethyl)-phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one-hydrochloric acid salt (275), 5-[4-(methylamino)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (276), (6S)-6-methyl-5-[4-(4-methylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (277), 5-[4-(2-hydroxypropan-2-yl)-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (278), (6S)-5-[4-(3,3-difluoroazetidin-1-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (279) and (6S)-5-[4-(3-hydroxy-3-methylazetidin-1-yl)-3-(trifluoromethyl)-phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one (280) or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof.

9. 5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-(4'-fluoro-2-methylbiphenyl-4-yl)-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4'-chloro-2-(trifluoromethyl)biphenyl-4-yl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)-phenyl}-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-[4-{[3,3,3-trifluoro-2(S)-hydroxypropyl]amino}-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-hydroxy-2-methylpropyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[(2-methoxyethyl)amino]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 5-{4-[1-(difluoromethyl)-1H-pyrazol-4-yl]-3-(trifluoromethyl)phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-5-[4-(2-aminopyridin-4-yl)-3-(trifluoromethyl)phenyl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, (6S)-6-methyl-5-{3-(trifluoromethyl)-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, or a stereoisomer, tautomer, N-oxide, hydrate, solvate or salt thereof, or a mixture thereof 9. The compound of claim 8, selected from the group consisting of:

10. (6S)-5-[4'-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one 9. The compound of claim 8, wherein

11. A method for preparing a compound according to any one of claims 1 to 10, comprising the steps of: Intermediate compound of general formula (II): 【Chemistry 2】 (In the formula, X is Cl, Br, I, or (C 1 ~C 4 -alkylsulfonyl)oxy, (C 1 ~C 4 is a leaving group selected from (phenylsulfonyl)oxy and (phenylsulfonyl)oxy, wherein the phenyl in the (phenylsulfonyl)oxy is optionally substituted with 1, 2, 3, 4 or 5 substituents, each of which is selected from halogen, nitro, cyano, C 1 ~C 4 -Alkyl and C 1 ~C 4 - independently selected from: - alkoxy; R 1 is a hydrogen atom, a fluorine atom, a cyano group, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and C 1 ~C 3 - haloalkoxy groups; R 2 is selected from a hydrogen atom and a fluorine atom; R 4 is a hydrogen atom and C 1 ~C 3 -alkyl groups), Under palladium catalyzed coupling conditions, Boronic acids of formula (IIIa): (R x )B(OH) 2 (IIIa), Boronic ester of formula (IIIb): (R x )B(OR Y ) 2 (IIIb), and Tetrafluoroborate salt of formula (IIIc): (R x )BF 4 (IIIc) An organoboron compound selected from (In the formula, R x means (i) to (vii) of the following: (i) C optionally substituted with 1 or 2 substituents 1 ~C 6 -Alkyl group (each substituent is a hydroxyl group, C 1 ~C 4 - independently selected from an alkoxy group and a 3- to 7-membered heterocycloalkyl group; (ii) In some cases, C 1 ~C 4 - C substituted with an alkoxy group 2 ~C 6 -alkenyl group; (iii) C optionally substituted with a hydroxy group 5 ~C 9 -cycloalkenyl group, (iv)-O-, -S-, -S(O)-, -S(O) 2 --and--NR 9 - 3-9 membered heterocycloalkyl groups containing 1, 2 or 3 atomic groups independently selected from In some cases, -O-, -NR 9 -, -CH 2 -, -CH 2 -CH 2 -, -O-CH 2 -, -CH 2 -O-, -NR 9 -CH 2 - and -CH 2 -NR 9 -, further comprising a bridging group selected from Optionally substituted with 1, 2 or 3 substituents, each of which is selected from the following (a) to (j): (a) a halogen atom; (b) an oxo (=O) group; (c) a cyano group; (d) a hydroxy group; (e) C optionally further substituted with a hydroxy group 1 ~C 3 - alkyl group; (f)C 1 ~C 3 - haloalkyl group; (g) C 1 ~C 3 -alkoxy group; (h)C 1 ~C 3 - a haloalkoxy group; (i) C(O)NR 5 R 6 Groups, and (j)NR 5 R 6 base a 3- to 9-membered heterocycloalkyl group independently selected from: (v) a partially unsaturated 5- to 9-membered heterocycloalkyl group, optionally substituted with 1, 2 or 3 substituents, each of which is an oxo group (=O), C 1 ~C 3 -Alkyl group, -C(O)NR 5 R 6 groups and halogen atoms), (vi) an aryl group optionally substituted with 1, 2, 3 or 4 substituents, each of which is a halogen atom, a hydroxyl group, a cyano group, 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -alkoxy group, C 1 ~C 3 -haloalkoxy group and NR 5 R 6 independently selected from the group (vii) a monocyclic or bicyclic heteroaryl group optionally substituted with 1, 2 or 3 substituents, each of which may be a halogen atom, 1 ~C 3 -Alkyl group, cyano group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -Alkoxy group, hydroxy group and NR 5 R 6 groups, with the proviso that said optionally substituted monocyclic heteroaryl group with 1, 2 or 3 substituents is not a pyridin-4-yl group. Selected from: R 5 / R 6 is a hydrogen atom, C 1 ~C 6 -Alkyl group, -C 1 ~C 5 -Alkylene-O-C 1 ~C 5 -Alkyl group, -C 1 ~C 5 -Alkylene-S-C 1 ~C 5 -Alkyl group, C 3 ~C 6 -Cycloalkyl groups and C 3 ~C 5 - independently selected from heterocycloalkyl groups; R 9 is a hydrogen atom or C 1 ~C 3 - an alkyl group or a bond, RY is C 1 ~C 6 - alkyl or two residues RY together form C 2 ~C 6 -alkylene group) Bases, and Dichlorobis(triphenylphosphine)palladium, Tetrakistriphenylphosphinepalladium(0), Palladium(II) acetate / triscyclohexylphosphine, Tris(dibenzylideneacetone)dipalladium, Bis(diphenylphosphineferrocenyl)palladium(II) chloride, 1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene(1,4-naphthoquinone)palladium dimer, Allyl(chloro)(1,3-dimesityl-1,3-dihydro-2H-imidazol-2-ylidene)palladium, Palladium(II) acetate / dicyclohexyl(2',4',6'-triisopropyl) -biphenyl-2-yl)phosphine, [1,1-bis(diphenylphosphino)ferrocene]palladium(II) chloride monodichloromethane adduct, [1,1'-bis(diphenylphosphino)ferrocene]dichloropalladium(II), chloro(2-dicyclohexylphosphino-2',4',6'-triisopropyl-1,1'-biphenyl)[2-(2'-amino-1,1'-biphenyl)]palladium(II), palladium(II) acetate and (2-dicyclohexylphosphino-2',4',6'-triisopropyl-1,1'-biphenyl)[2-(2'-amino-1,1'-biphenyl)]palladium(II). A palladium catalyst selected from and optionally comprising step A of reacting in the presence of 2-(dicyclohexylphosphino)-2',4',6'-triisopropylbiphenyl, or Intermediate compound of general formula (II): 【Chemistry 3】 (In the formula, X is F or Cl, provided that when X is Cl, R 1 or R 2 cannot be F; R 1 is a hydrogen atom, a halogen atom, a cyano group, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and C 1 ~C 3 - haloalkoxy groups; However, when X is Cl, R 1 cannot be a fluorine atom; R 2 is selected from a hydrogen atom and a halogen atom; However, when X is Cl, R 2 cannot be a fluorine atom; R 4 is a hydrogen atom and C 1 ~C 3 -alkyl groups), HNR 7 R 8 and the corresponding amines selected from cyclic amines having one N-H in the ring portion, said cyclic amines being selected from 3- to 9-membered heterocycloalkanes, partially unsaturated 5- to 9-membered heterocycloalkanes and heteroarenes, optionally as a free base or salt. (in HNR 7 R 8, R 7 / R 8 means (i) to (vi) of the following: (i) a hydrogen atom (wherein R 7 = R 8 = hydrogen is excluded); (ii) C 1 ~C 6 -Alkyl group which is optionally substituted with 1, 2, 3 or 4 substituents, the substituents being selected from the following (a) to (i): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; (d)C(O)NR 5 R 6 base; (e)NR 5 R 6 base; (f)C 1 ~C 3 -alkoxy group; (g) C optionally substituted with 1 or 2 substituents 3 ~C 7 -Cycloalkyl group (said substituents are C 1 ~C 3 -Alkyl group, oxo (=O) group, hydroxy group and C 1 ~C 3 -hydroxyalkyl groups; (h) Itself may be C 1 ~C 3 - a 3- to 7-membered heterocycloalkyl group substituted with an alkyl or oxo (=O) group; and (i) It may itself be C 1 ~C 3 - Heteroaryl group substituted with alkyl group are independently selected from (iii)-C 1 ~C 5 -Alkylene-O-C4~C 5 - alkyl group; (iv)-C 1 ~C 5 -Alkylene-S-C 1 ~C 5 - alkyl group; (v) C optionally substituted with a hydroxy group 3 ~C 6 -cycloalkyl group; and (iv) a 3- to 6-membered heterocycloalkyl group, optionally substituted with one or two substituents, the substituents being C 1 ~C 3 independently selected from alkyl groups and hydroxy groups. (independently selected from Step B comprises reacting optionally in the presence of a base and optionally in the presence of an inert solvent at a temperature between room temperature and 160° C., or Intermediate compound of general formula (II): 【Chemistry 4】 (In the formula, X is Cl, Br, I, or (C 1 ~C 4 -alkylsulfonyl)oxy, (C 1 ~C 4 is a leaving group selected from (phenylsulfonyl)oxy and (phenylsulfonyl)oxy, wherein the phenyl in the (phenylsulfonyl)oxy is optionally substituted with 1, 2, 3, 4 or 5 substituents, each of which is selected from halogen, nitro, cyano, C 1 ~C 4 -Alkyl and C 1 ~C 4 - independently selected from: - alkoxy; R 1 is a hydrogen atom, a fluorine atom, a cyano group, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl groups and C 1 ~C 3 - haloalkoxy groups; R 2 is selected from a hydrogen atom and a fluorine atom; R 4 is a hydrogen atom and C 1 ~C 3 -alkyl groups), HNR 7 R 8 and the corresponding amines selected from cyclic amines having one N-H in the ring portion, said cyclic amines being selected from 3- to 9-membered heterocycloalkanes, partially unsaturated 5- to 9-membered heterocycloalkanes and heteroarenes, optionally as a free base or salt. (in HNR 7 R 8, R 7 / R 8 means (i) to (vi) of the following: (i) a hydrogen atom (wherein R 7 = R 8 = Hydrogen is excluded), (ii) C 1 ~C 6 -Alkyl group which is optionally substituted with 1, 2, 3 or 4 substituents, the substituents being selected from the following (a) to (i): (a) a halogen atom; (b) a cyano group; (c) a hydroxy group; (d)C(O)NR 5 R 6 base; (e)NR 5 R 6 base; (f)C 1 ~C 3 -alkoxy group; (g) C optionally substituted with 1 or 2 substituents 3 ~C 7 -Cycloalkyl group (said substituents are C 1 ~C 3 -Alkyl group, oxo (=O) group, hydroxy group and C 1 ~C 3 -hydroxyalkyl groups; (h) Itself may be C 1 ~C 3 - a 3- to 7-membered heterocycloalkyl group substituted with an alkyl or oxo (=O) group; and (i) It may itself be C 1 ~C 3 - Heteroaryl group substituted with alkyl group are independently selected from (iii)-C 1 ~C 5 -Alkylene-O-C4~C 5 - alkyl group; (iv)-C 1 ~C 5 -Alkylene-S-C 1 ~C 5 - alkyl group; (v) C optionally substituted with a hydroxy group 3 ~C 6 -cycloalkyl group; and (vi) a 3- to 6-membered heterocycloalkyl group optionally substituted with one or two substituents, the substituents being C 1 ~C 3 independently selected from alkyl and hydroxy groups; (independently selected from In the presence of a base, the palladium catalyst used in step A, and 2-(dicyclohexylphosphino)-2',4',6'-triisopropyl-1,1'-biphenyl or 2,2'-bis(diphenylphosphino)-1,1'-binaphthalene, in an inert solvent at a temperature between 60°C and 160°C. C. comprising reacting A process for obtaining a compound according to any one of claims 1 to 10 using one of said steps.

12. Regarding compound (II): R 1 is a trifluoromethyl group, and R 2 is a hydrogen atom, Regarding step A: Suzuki coupling conditions are used and the palladium catalyst is chloro(2-dicyclohexylphosphino-2',4',6'-triisopropyl-1,1'-biphenyl)[2-(2'-amino-1,1'-biphenyl)]palladium(II); and / or Two residues RY together form -C(CH 3 ) 2 -C(CH 3 ) 2 - to form a pinacol ester, and the base is potassium carbonate or potassium acetate; and / or Regarding step C: The palladium catalyst is tris(dibenzylideneacetone)dipalladium(0); A method for preparing the compound of claim 11.

13. For step A, x A method for preparing a compound according to claim 11, wherein is a methyl group optionally substituted with a 3- to 7-membered heterocycloalkyl group.

14. 11. A pharmaceutical composition comprising a compound according to any one of claims 1 to 10 and one or more pharma- ceutically acceptable excipients.

15. - one or more first active ingredients which are compounds according to any one of claims 1 to 10, and one or more further active ingredients 23. A pharmaceutical composition comprising:

16. 13. A composition comprising a compound according to any one of claims 1 to 10 for treating or preventing a disease.

17. 17. The composition of claim 16, wherein the disease is a hyperproliferative disease.

18. The composition of claim 17, wherein the hyperproliferative disease is a cancer disease.

19. 19. The composition of claim 18, wherein the cancer disease is brain cancer, breast cancer, cervical cancer, AML, lung cancer, skin cancer, esophageal cancer, ovarian cancer, pancreatic cancer and prostate cancer.

20. A compound having the structure of general formula (II): 【Chemistry 5】 (In the formula, R 1 is a fluorine atom or a trifluoromethyl group, and R 2 is a hydrogen atom or a methyl group, and R 4 has the meaning defined for the compounds according to any one of claims 1 to 8, and X is a fluorine, chlorine, bromine or iodine atom.

21. 5-[4-chloro-3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-1,3,4-oxadiazin-2-one, 21. The compound according to claim 20, selected from:

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