4,5-fused 1,2,4-triazolone

Abstract

To provide compounds which inhibit Dihydroorotate Dehydrogenase.SOLUTION: The present invention provides 4,5-annulated 1,2,4-triazolone compounds represented by formula (I), methods of preparing the compounds, intermediate compounds useful for preparing the compounds, pharmaceutical compositions and combinations comprising the compounds, and the use of the compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to 4,5-fused 1,2,4-triazolone compounds of general formula (I) as described and defined herein, processes for preparing said compounds, intermediate compounds useful in preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for the manufacture of pharmaceutical compositions for the treatment or prevention of diseases, particularly hyperproliferative and / or inflammatory disorders, as the sole agent or in combination with other active ingredients. [Background technology]

[0002] The present invention provides 4,5-fused 1,2,4-triazolone compounds of general formula (I) that inhibit dihydroorotate dehydrogenase (DHODH).

[0003] Acute myeloid leukemia (AML) is the most common acute leukemia in humans, with a 5-year survival rate of only approximately 30%. AML is a malignant tumor of the myeloid lineage of blood cells. The incidence and chances of cure are highly age-dependent. Standard chemotherapy for AML has not changed significantly in recent decades, highlighting the need for novel therapeutic approaches. A key feature of AML is the arrest of leukemic cells during the early stages of cell differentiation. The potential for leukemic differentiation therapy has been demonstrated with the success of ATRA or arsenic trioxide in inducing differentiation in acute promyelocytic leukemia (APL). Approximately 10% of AML cases belong to the APL subtype, in which leukemic cells harbor chromosomal translocations resulting in the fusion of an oncoprotein involving the retinoic acid receptor. Treatment with ATRA or arsenic trioxide dramatically increases patient survival, with overall survival rates exceeding 70%, but unfortunately, comparable differentiation therapies for non-APL AML are lacking (Management of acute promyelocytic leukemia: recommendations from an expert panel on behalf of the European LeukemiaNet, Sanz MA et al, Blood 2009, 113(9), 1875-1891). Therefore, new therapies that induce differentiation of AML cells are of great interest and medical need.

[0004] Dihydroorotate dehydrogenase (DHODH) DHODH is located in mitochondria and is the fourth and rate-limiting enzyme in de novo pyrimidine synthesis, converting dihydroorotate to orotic acid (Dihydroorotate-ubiquinone oxidoreductase links mitochondria in the biosynthesis of pyrimidine nucleotides, Loffler M. et al, Molecular and Cellular Biochemistry 1997, 174, 125-129).

[0005] DHODH is crucial for cell proliferation because pyrimidine production is essential for DNA and RNA synthesis. This enzyme is considered an attractive drug target for cancer, immunological, parasitic, and viral diseases, and DHODH small molecule inhibitors such as leflunomide / teriflunomide and brequinar have been approved for clinical use in rheumatoid arthritis and multiple sclerosis. Furthermore, preclinical studies have shown that DHODH inhibitors may be useful in the treatment of hematological cancers, solid tumors (e.g., neuroblastoma, melanoma, colon, breast, and lung tumors), parasitic diseases (e.g., malaria), and viral disease therapy.

[0006] US Patent No. 6,444,613 relates to the field of defoliants, in particular thidiazuron-containing mixtures, and their use in cotton crops. These mixtures contain, inter alia, 2,4,5-trisubstituted 1,2,4-triazolone compounds as herbicides, which inhibit the enzyme protoporphyrinogen-(IX) oxidase (PPO inhibitors).

[0007] WO 199802422 describes substituted aromatic carbonyl compounds, especially 2,4,5-trisubstituted 1,2,4-triazolone compounds, as herbicides.

[0008] From Chinese Patent No. 106543139, some triazolone compounds are known as pesticides.

[0009] US Patent Application Publication No. 2016 / 0251341 describes triazole compounds as serine protease inhibitors useful for inhibiting thrombin and / or kallikrein.

[0010] WO 2013 / 186692 describes triazolone compounds as mPGES-1 inhibitors, useful for the treatment of pain and / or inflammation from various diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases.

[0011] WO 2010 / 077686 describes sirtuin-modulating compounds, such as isoindolinones and related compounds, and methods of using them. Sirtuin-modulating compounds extend cellular lifespan and can be used to treat and / or prevent a wide variety of diseases and disorders, including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular diseases, blood clotting disorders, inflammation, cancer and / or flushing, and diseases or disorders that would benefit from increased mitochondrial activity. [Prior art documents] [Patent documents]

[0012] [Patent Document 1] U.S. Patent No. 6,444,613 [Patent Document 2] International Publication No. 199802422 Pamphlet [Patent Document 3] Chinese Patent No. 106543139 [Patent Document 4] US Patent Application Publication No. 2016 / 0251341 [Patent Document 5] International Publication No. 2013 / 186692 Brochure [Patent Document 6] International Publication No. 2010 / 077686 Brochure [Non-patent literature]

[0013] [Non-Patent Document 1] Management of acute promyelocytic leukemia:recommendations from an expert panel on behalf of the European LeukemiaNet, Sanz MA et al, Blood 2009, 113(9), 1875-1891 [Non-patent document 2] Dihydroorotat-ubiquinone oxidoreductase links mitochondria in the biosynthesis of pyrimidine nucleotides, Loffler M. et al, Molecular and Cellular Biochemistry 1997, 174, 125-129 Summary of the Invention

[0014] It has now been found that the compounds of the present invention (eg, 4,5-fused 1,2,4-triazolone compounds of general formula (I)) have surprising and advantageous properties, which in part form the basis of the present invention.

[0015] In particular, the compounds of the present invention have surprisingly been found to effectively inhibit DHODH and can therefore be used to treat or prevent diseases including hyperproliferative and / or inflammatory disorders, such as cancer. [Means for solving the problem]

[0016] According to one aspect, the present invention provides compounds of general formula (I): [ka] (In the formula, R 1 teeth C1-C8-alkyl groups (which may optionally be C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from the phenyl substituents are optionally substituted one, two or three times with one or more substituents independently selected from halogen atoms, C1-C3-alkyl groups, C1-C4-haloalkyl groups, C1-C3-alkoxy groups and hydroxy groups, C2-C8-haloalkyl group, C3-C8-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, hydroxy groups, phenyl groups and -N(R 7 )(R 8 ) groups, the phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from halogen atoms, C1-C3-alkyl groups, C1-C4-haloalkyl groups, C1-C3-alkoxy groups and hydroxy groups; C2-C6-cyanoalkyl groups, C2-C6-hydroxyalkyl groups, (C2-C6-hydroxyalkyl)-O-(C2-C6-alkyl)- group -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4-7 membered optionally unsaturated heterocyclic group which is attached to the rest of the molecule via a carbon atom and is optionally substituted once or twice, each substituent being independently selected from C1-C3 alkyl groups, 5-6 membered heteroaryl groups, -C(=O)O(C1-C4 alkyl) groups, -C(=O)(C1-C6 alkyl) groups, -C(=O)(C3-C6 cycloalkyl) groups, -S(=O)2(C1-C6 alkyl) groups and oxo(=O) groups; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, aryl, -O-aryl, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C6-alkyl), -S(=O)2-O-(C2-C6-alkenyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -N(O)2, -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two adjacent substituents of the phenyl group may be taken together to optionally form -N=, -NH-, -N(R 7 )-, -O-, -S-, and optionally forming a 5- or 6-membered heterocyclic, aromatic or non-aromatic ring containing a C(=O) group, the ring thus formed being optionally substituted once or twice, and each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(═O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) (independently selected from groups selected from and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of which is a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 2 represents a hydrogen atom or a halogen atom, R 3 teeth C1-C6 alkyl groups C3-C8-cycloalkyl groups, C1-C6-haloalkyl group, C1-C6-hydroxyalkyl group, C2-C6-alkenyl group, C2-C6 alkynyl group, a C4-C8-cycloalkenyl group, (C1-C6-alkyl)-N(R 7 )R 8 base, -(C1-C6-alkyl)-N(H)C(=O)R 6 base, -(C1-C6-alkyl)-N(H)C(=O)OR 15 base, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group wherein the 4- to 7-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group, the 4-7 membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3 alkyl group; and phenyl group which is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 4 and R 5 together form the 5- to 6-membered, optionally unsaturated heterocyclic ring A of sub-formula (i) [ka] (wherein ring A is a ring containing two essential atoms, a nitrogen atom bridging the two rings, and a carbon atom, and in addition, -O-, -S-, -S(=O)-, -S(=O)2-, -S(=O)(=NR 14 )-, -N=, -N(R 7 )-, -C(=O)-, -CH=, -CR 11 =, -C(R 12 )2-, -C(H)(R 13 )-) Forming R 6 is a hydrogen atom or C1-C6 alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C6 alkyl groups, C2-C6 alkenyl groups, C2-C6 hydroxyalkyl groups, haloalkyl groups, aryl groups, (C1-C6 alkyl)-aryl groups, and -(C2-C6 alkyl)-N(R 9 )(R 10 ) group represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group may optionally be C1-C6-alkyl, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C3-alkyl), -S(=O)2-(C2-C6-alkenyl) and -C(=O)OR 6 - and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 9 and R10 together with the nitrogen to which they are attached, Nitrogen-containing 4- to 7-membered heterocycloalkyl groups represents R 11 is independently for each occurrence a hydrogen atom, a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 12 represents, independently for each occurrence, a hydrogen atom, a halogen atom or a C1-C3-alkyl group; R 13 teeth C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1- to C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 14is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from R 15 teeth C1-C6 alkyl groups and benzyl groups represents a group selected from or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0017] definition 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, 4, or 5, particularly 1, 2, or 3.

[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] When a composite substituent is composed of two or more moieties, such as (C1-C3-alkoxy)-(C1-C6-alkyl)-, the position of a given moiety can be at any suitable position on the composite substituent, i.e., the C1-C3-alkoxy moiety can be attached to any carbon atom of the C1-C6-alkyl moiety of the (C1-C3-alkoxy)-(C1-C6-alkyl)- group. The first or last hyphen of such a composite substituent indicates the point of attachment of the composite substituent to the rest of the molecule. 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 can be attached at any suitable position on the ring, and is attached to any suitable carbon atom and / or heteroatom.

[0023] The term "comprising" as used herein includes "consisting of."

[0024] 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.

[0025] 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.

[0026] The term "C1-C8-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, 1,3-dimethylbutyl, heptyl or octyl radical, or an isomer thereof. In particular, the radicals have 1, 2, 3, 4, 5 or 6 carbon atoms ("C1-C6-alkyl"), such as 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 radicals. 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.

[0027] The term "C1-C6-hydroxyalkyl" means a linear or branched saturated monovalent hydrocarbon radical in which one or two hydrogen atoms have been replaced by a hydroxy group, as defined above for example, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxypropan-2-yl, 2-hydroxypropan-2-yl, 2,3-dihydroxypropyl, 1,3-dihydroxypropan-2-yl, 3-hydroxy-2-methylpropyl, 2-hydroxy-2-methyl-propyl, 1-hydroxy-2-methyl-propyl radicals. In particular, the group has 1, 2 or 3 carbon atoms ("C1-C3-hydroxyalkyl"), such as a hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 1,2-dihydroxyethyl, 3-hydroxypropyl, 2-hydroxypropyl, 1-hydroxypropyl, 1-hydroxypropan-2-yl, 2-hydroxypropan-2-yl, 2,3-dihydroxypropyl or 1,3-dihydroxypropan-2-yl group.

[0028] The term "C1-C6-alkylsulfanyl" means a linear or branched saturated monovalent radical of the formula (C1-C6-alkyl)-S-, wherein the term "C1-C6-alkyl" is as defined above, such as, for example, methylsulfanyl, ethylsulfanyl, propylsulfanyl, isopropylsulfanyl, butylsulfanyl, sec-butylsulfanyl, isobutylsulfanyl, tert-butylsulfanyl, pentylsulfanyl, isopentylsulfanyl, hexylsulfanyl radicals.

[0029] The term "C2-C8-haloalkyl" means a linear or branched saturated monovalent hydrocarbon radical, in which the term "C2-C8-alkyl" is as defined 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. The C2-C8-haloalkyl radical is, for example, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl or 1,3-difluoropropan-2-yl. In particular, the radical has 2, 3, 4, 5 or 6 carbon atoms ("C2-C6-haloalkyl").

[0030] 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 by identical or different halogen atoms. In particular, the halogen atoms are fluorine atoms. The C1-C6-haloalkyl radical is, for example, fluoromethyl, difluoromethyl, trifluoromethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl or 1,3-difluoropropan-2-yl. In particular, the group has 1, 2, 3 or 4 carbon atoms ("C1-C4-haloalkyl"), more in particular 1, 2 or 3 carbon atoms ("C1-C3-haloalkyl"), such as fluoromethyl, difluoromethyl, trifluoromethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl or 1,3-difluoropropan-2-yl.

[0031] 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, isopropoxy, n-butoxy, sec-butoxy, isobutoxy, tert-butoxy, pentyloxy, isopentyloxy or n-hexyloxy group, or an isomer thereof. In particular, said radical has 1, 2 or 3 carbon atoms ("C1-C3-alkoxy"), such as a methoxy, ethoxy, n-propoxy or isopropoxy group.

[0032] 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 atom is a fluorine atom. The C1-C6-haloalkoxy group is, for example, fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy or pentafluoroethoxy. In particular, the group has 1, 2 or 3 carbon atoms ("C1-C3-haloalkoxy"), for example, fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy or pentafluoroethoxy.

[0033] The term "C2-C6-alkenyl" denotes a straight-chain or branched monovalent hydrocarbon radical containing one double bond and having 2, 3, 4, 5 or 6 carbon atoms, in particular 2 or 3 carbon atoms ("C2-C3-alkenyl"), and if the alkenyl radical contains more than one double bond, the double bonds can be isolated from one another or conjugated to one another.The alkenyl group can be, 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-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-methylpent-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, 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 or 1-(1,1-dimethylethyl)ethenyl group.In particular, the group is allyl.

[0034] 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"). The C2-C6 alkynyl group is, 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, nyl, 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 or 3,3-dimethylbut-1-ynyl group.

[0035] The term "C3-C8-cycloalkyl" denotes a saturated monovalent monocyclic or bicyclic hydrocarbon ring ("C3-C8-cycloalkyl") containing 3, 4, 5, 6, 7 or 8 carbon atoms. The C3-C8-cycloalkyl group is, for example, a monocyclic hydrocarbon ring, such as a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl group, or a bicyclic hydrocarbon ring, such as a bicyclo[4.2.0]octyl or octahydropentalenyl. In particular, the group contains 3, 4, 5 or 6 carbon atoms ("C3-C6-cycloalkyl"), such as a cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl group. In particular, the group contains 4, 5, 6, 7 or 8 carbon atoms ("C4-C8-cycloalkyl"), such as a cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl group.

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

[0037] The term "C3-C8-cycloalkoxy" means a saturated monovalent monocyclic or bicyclic radical of the formula (C3-C8-cycloalkyl)-O-, containing 3, 4, 5, 6, 7 or 8 carbon atoms, in which the term "C3-C8-cycloalkyl" is defined above, such as a cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cycloheptyloxy or cyclooctyloxy radical. In particular, said radical has 3, 4, 5 or 6 carbon atoms ("C3-C6-cycloalkoxy"), such as a cyclopropyloxy, cyclobutyloxy, cyclopentyloxy or cyclohexyloxy radical.

[0038] The terms "4- to 7-membered heterocycloalkyl" and "4- to 6-membered heterocycloalkyl" refer to monocyclic saturated heterocycles containing one or two identical or different series N, O, and S ring heteroatoms, having a total of 4, 5, 6, or 7, or 4, 5, or 6 ring atoms, respectively.

[0039] The heterocycloalkyl group can be, but is not limited to, a four-membered ring such as, for example, azetidinyl, oxetanyl, or thietanyl; a five-membered ring such as, for example, tetrahydrofuranyl, 1,3-dioxolanyl, thiolanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, 1,1-dioxidethiolanyl, dioxidetetrahydrothiopyranyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl, or 1,3-thiazolidinyl; or a six-membered ring such as, for example, tetrahydropyranyl, tetrahydrothiopyranyl, piperidinyl, morpholinyl, dithianyl, thiomorpholinyl, piperazinyl, 1,3-dioxanyl, 1,4-dioxanyl, or 1,2-oxazinanyl, or a seven-membered ring such as, for example, azepanyl, 1,4-diazepanyl, or 1,4-oxazepanyl.

[0040] The terms "4- to 7-membered nitrogen-containing heterocycloalkyl" and "4- to 6-membered nitrogen-containing heterocycloalkyl" refer to monocyclic saturated heterocycles having a total of 4, 5, 6, or 7, or 4, 5, or 6 ring atoms, respectively, including one ring nitrogen atom and optionally one further ring heteroatom of the series: N, O, S atom.

[0041] The nitrogen-containing heterocycloalkyl group can be, but is not limited to, a four-membered ring such as, for example, azetidinyl; or a five-membered ring such as, for example, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, 1,2-oxazolidinyl, 1,3-oxazolidinyl, or 1,3-thiazolidinyl; or a six-membered ring such as, for example, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, or 1,2-oxazinanyl, or a seven-membered ring such as, for example, azepanyl, 1,4-diazepanyl, or 1,4-oxazepanyl.

[0042] The term "5- to 7-membered heterocycloalkenyl" means a monocyclic unsaturated non-aromatic heterocycle having a total of 5, 6, or 7 ring atoms, including one or two double bonds and one or two ring heteroatoms independently selected from the series: N, O, and S.

[0043] The heterocycloalkenyl group is, for example, 4H-pyranyl, 2H-pyranyl, 2,5-dihydro-1H-pyrrolyl, [1,3]dioxolyl, 4H-[1,3,4]thiadiazinyl, 2,5-dihydrofuranyl, 2,3-dihydrofuranyl, 2,5-dihydrothiophenyl, 2,3-dihydrothiophenyl, 4,5-dihydrooxazolyl or 4H-[1,4]thiazinyl.

[0044] The term "4- to 7-membered optionally unsaturated heterocyclic group" encompasses the terms "4- to 7-membered heterocycloalkyl" and "5- to 7-membered heterocycloalkenyl."

[0045] The term "aryl" includes aromatic ring systems, whether monocyclic or bicyclic, especially phenyl and naphthyl.

[0046] The term "a phenyl group in which two adjacent substituents together form a 5- or 6-membered, optionally aromatic or non-aromatic, ring, optionally containing a C(=O) group" includes naphthalinyl, indanyl and tetralinyl.

[0047] The term "heteroaryl" means a monovalent monocyclic or bicyclic aromatic ring having 5, 6, 8, 9 or 10 ring atoms (a "5-10 membered heteroaryl" group), especially 5, 6, 9 or 10 ring atoms, containing at least one ring heteroatom and optionally 1, 2 or 3 further ring heteroatoms of the series: N, O and / or S, and bonded via a ring carbon atom or optionally a ring nitrogen atom (where permitted by valence).

[0048] The heteroaryl group can be a 5-membered heteroaryl group (e.g., thienyl, furanyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, or tetrazolyl); or a 6-membered heteroaryl group (e.g., pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, or triazinyl); or a 9-membered heteroaryl group (e.g., benzofuranyl, benzothienyl, benzoxazolyl, benzisoxazolyl, benzimidazolyl, benzothiazolyl, benzotriazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, or purinyl); or a 10-membered heteroaryl group (e.g., 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] The term "C1-C6" as used herein, for example in the context of the definitions of "C1-C6-alkyl", "C1-C6-haloalkyl", "C1-C6-hydroxyalkyl", "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.

[0051] 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.

[0052] When a range of values ​​is given, the range includes each value and subrange within the range.

[0053] for example: "C1~C8" means C1, C2, C3, C4, C5, C6, C7, C8, C1~C8, C1~C7, C1~C6, C1~C5, C1~C4, C1~C3, C1~C2, C2~C8, C2~C7, C2~C6, C2~C5, C2~C4 , including C2~C3, 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; "C1~C6" means C1, C2, C3, C4, C5, C6, C1~C6, C1~C5, C1~C4, C1~C3, C1~C2, C2~C6 , including C2~C5, C2~C4, C2~C3, C3~C6, C3~C5, C3~C4, C4~C6, C4~C5 and C5~C6; "C1-C4" includes C1, C2, C3, C4, C1-C4, C1-C3, C1-C2, C2-C4, C2-C3, and C3-C4; "C1-C3" includes C1, C2, C3, C1-C3, C1-C2, and C2-C3; "C2-C6" includes C2, C3, C4, C5, C6, C2-C6, C2-C5, C2-C4, C2-C3, C3-C6, C3-C5, C3-C4, C4-C6, C4-C5 and C5-C6; "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~C 7、 C7~C 10、 C7~C9, C7~C8, C8~C10 , 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~C 7、 C7~C 10、 C7~C9, C7~C8, C8~C 10 , C8-C9 and C9-C 10 encompasses;

[0054] As used herein, the term "leaving group" refers to an atom or group of atoms that can 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.

[0055] The term "substituents" refers to groups "substituted" on an alkyl, haloalkyl, cycloalkyl, heterocyclyl, heterocycloalkenyl, cycloalkenyl, aryl, or heteroaryl group at any atom of that group, for example, replacing one or more hydrogen atoms therein. In one aspect, one or more substituents on a group are independently any single atom or any combination of two or more of the permissible atoms or groups of atoms depicted for that substituent. In another aspect, the substituents themselves may be substituted with any one of the above substituents. Furthermore, as used herein, the phrase "optionally substituted" means unsubstituted (e.g., substituted with H) or substituted.

[0056] It will be understood that the description of compounds herein is limited by the principles of chemical bonding known to those skilled in the art.Therefore, when a group can be substituted with one or more of several substituents, such substitution is selected to give a compound that is compatible with the principles of chemical bonding in terms of valence, etc., and is not inherently unstable.For example, any carbon atom will be bonded to two, three or four other atoms, in accordance with the four valence electrons of carbon. "Subject" means a mammal, including, but not limited to, a human or non-human mammal, such as a bovine, equine, canine, ovine, rodent, or feline.

[0057] It is possible for compounds of general formula (I) to exist in isotopic variations, and therefore the present invention includes one or more isotopic variations of compounds of general formula (I), particularly deuterium-containing compounds of general formula (I).

[0058] The term "isotopic variant" of a compound or reagent is defined as a compound that exhibits an unnatural ratio of one or more isotopes that constitute such compound.

[0059] The expression "unnatural proportion" with respect to an isotope means a proportion of such isotope that is greater 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.

[0060] 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.

[0061] For the treatment and / or prevention of the disorders specified herein, one or more isotopic variants of the compounds of general formula (I) preferably contain deuterium ("deuterium-containing compounds of general formula (I)"). One or more radioisotopes, 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 11Positron-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.

[0062] 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 rapid 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.

[0063] 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 said 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.

[0064] The selective incorporation of one or more deuterium atoms into a compound of general formula (I) may 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 changes in the ratio of parent compound to metabolites or the amounts of metabolites produced. Such changes may result in certain therapeutic advantages and may therefore be desirable in some circumstances. Decreased rates of metabolism and metabolic switching, altering the ratio of metabolites, have been reported (AE Mutlib et al., Toxicol. Appl. Pharmacol., 2000, 169, 102). These changes in exposure to parent drugs and metabolites can have important consequences for the pharmacokinetics, tolerability, and efficacy of deuterium-containing compounds of general formula (I). In some cases, 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: AE Mutlib et al., Toxicol. Appl. Pharmacol., 2000, 169, 102). In other cases, the primary effect of deuteration is to reduce 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, which could result in reduced side effects and enhanced efficacy, depending on the pharmacokinetic / pharmacodynamic relationship of the 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. Additional 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 reduce dosing requirements (e.g., fewer doses or lower dosages to achieve the desired effect) and / or may result in reduced metabolite levels.

[0065] A compound of general formula (I) may have multiple potential sites of metabolic attack. To optimize the above effects on physicochemical properties and metabolic profiles, deuterium-containing compounds of general formula (I) can be selected that have a specific pattern of one or more deuterium-hydrogen exchanges. 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 to, for example, cytochrome P. 450 It is located at the position of the compound of general formula (I), which is the site of attack for metabolizing enzymes such as

[0066] In another embodiment, the present invention relates to deuterium-containing compounds of general formula (I) having 1, 2, 3 or 4 deuterium atoms, in particular containing 1, 2 or 3 deuterium atoms.

[0067] When the plural of a word such as compounds, salts, polymorphs, hydrates, solvates, etc. is used herein, this is also considered to mean a single compound, salt, polymorph, isomer, hydrate, solvate, etc. As used herein, the terms "a" or "an" mean one or more.

[0068] 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.

[0069] The compounds of the present invention may contain one or more asymmetric centers, depending on the position and nature of various desired substituents.One or more asymmetric carbon atoms may be present in (R) or (S) configuration, which may result in a racemic mixture in the case of a single asymmetric center, or a diastereomeric mixture in the case of multiple asymmetric centers.In certain cases, asymmetry may exist due to restricted rotation around a given bond, for example, the central bond connecting two substituted aromatic rings of a specified compound.

[0070] Preferred isomers are those that result in the more desirable biological activity. These separated, pure or partially purified isomers or racemic mixtures of the compounds of the present invention are also within the scope of the present invention. Purification and separation of such materials can be accomplished by standard techniques known in the art.

[0071] 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.

[0072] To distinguish different types of isomers from one another, reference is made to IUPAC Rules Section E (Pure Appl Chem 45, 11-30, 1976).

[0073] 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.

[0074] Furthermore, it is possible for compounds of the invention to exist as tautomers, for example, any compound of the invention that includes an imidazopyridine moiety as a heteroaryl group may exist as, for example, a 1H tautomer or a 3H tautomer, or two tautomers, namely: [ka] can be present in any amount of mixture.

[0075] The present invention includes all possible tautomers of the compounds of the present invention as single tautomers or any mixture of said tautomers in any ratio.

[0076] Additionally, compounds of the present invention can exist as N-oxides, which are defined in that at least one nitrogen in a compound of the present invention is oxidized, and the present invention includes all such possible N-oxides.

[0077] The present invention also provides useful forms of the compounds of the present invention, such as metabolites, hydrates, solvates, prodrugs, salts, particularly pharmaceutically acceptable salts, and / or coprecipitates.

[0078] 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.

[0079] Furthermore, the compounds of the invention can exist in free form, e.g., 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.

[0080] The term "pharmaceutically acceptable salt" refers to an inorganic or organic acid addition salt of a compound of the present invention. See, for example, SM Berge, et al. "Pharmaceutical Salts," J. Pharm. Sci. 1977, 66, 1-19.

[0081] 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.

[0082] Further suitable pharmaceutically acceptable salts of the compounds of the present invention that are sufficiently acidic include 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.

[0083] 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.

[0084] The present invention includes all possible salts of the compounds of the present invention, either as a single salt or as any mixture of said salts in any ratio.

[0085] The present invention includes diastereomers, racemates, tautomers, N-oxides, hydrates, solvates and salts of the compounds of the present invention, and mixtures thereof.

[0086] 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 said salt forms obtained by each preparation and / or purification step is in most cases unknown.

[0087] 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.

[0088] 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).

[0089] 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.

[0090] 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.

[0091] According to certain embodiments, the present invention provides a compound of general formula (I) [ka] (In the formula, R 1 teeth C1-C8-alkyl groups (which may optionally be C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy (independently selected from groups selected from C2-C8-haloalkyl group, C3-C8-cycloalkyl groups, which are optionally substituted once or twice, each substituent being a halogen atom or hydroxy, phenyl and -N(R 7 )(R 8 ) independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy (independently selected from groups selected from C2-C6-cyanoalkyl groups, C2-C6-hydroxyalkyl groups, (C2-C6-hydroxyalkyl)-O-(C2-C6-alkyl)- group -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, 4-7 membered optionally unsaturated heterocyclic groups, which are attached to the rest of the molecule via a carbon atom and are optionally substituted once or twice, each substituent being C1-C3-alkyl, 5-6 membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C6-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C6-alkyl) and oxo(=O). are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, aryl, -O-aryl, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C6-alkyl), -S(=O)2-O-(C2-C6-alkenyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -N(O)2, -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two adjacent substituents of the phenyl group may be taken together to optionally form -N=, -NH-, -N(R 7)-, -O-, -S-, and optionally forming a 5- or 6-membered heterocyclic, aromatic or non-aromatic ring containing a C(=O) group, the ring thus formed being optionally substituted once or twice, and each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(═O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) (independently selected from groups selected from and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of which is a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 2 represents a hydrogen atom or a halogen atom, R 3 teeth C1-C6 alkyl groups C3-C8-cycloalkyl groups, C1-C6-haloalkyl group, C1-C6-hydroxyalkyl group, C2-C6-alkenyl group, C2-C6 alkynyl group, a C4-C8-cycloalkenyl group, (C1-C6-alkyl)-N(R 7 )R 8 base, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group wherein the 4- to 7-membered nitrogen-containing heterocycloalkyl group is attached to the alkyl group via a carbon atom of the heterocycloalkyl group, and the 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3-alkyl group, and phenyl group which is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 4 and R 5 together form the 5- to 6-membered, optionally unsaturated heterocyclic ring A of sub-formula (i) [ka] (wherein ring A is a ring that contains two essential atoms, a nitrogen atom and a carbon atom bridging the two rings, as well as -O-, -S-, -S(=O)-, -S(=O)2-, -N=, -N(R 7 )-, -C(=O)-, -CH=, -CR 11 =, -C(R 12 )2-, -CHR 13 -having an additional 3 to 6 members selected from Forming R 6 is a hydrogen atom or C1-C6 alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C6 alkyl groups, C2-C6 alkenyl groups, C2-C6 hydroxyalkyl groups, haloalkyl groups, aryl groups, (C1-C6 alkyl)-aryl groups, and -(C2-C6 alkyl)-N(R 9 )(R 10 ) group represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group may optionally be C1-C6-alkyl, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C3-alkyl), -S(=O)2-(C2-C6-alkenyl) and -C(=O)OR 6 - and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 9 and R 10together with the nitrogen to which they are attached, Nitrogen-containing 4- to 7-membered heterocycloalkyl groups represents R 11 is independently for each occurrence a hydrogen atom, a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 12 represents, independently for each occurrence, a hydrogen atom, a halogen atom or a C1-C3-alkyl group; R 13 teeth C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1- to C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from and tautomers, N-oxides and salts thereof, or salts of the tautomers or N-oxides of said compounds.

[0092] According to certain embodiments, the present invention provides a compound of general formula (I) [ka] (In the formula, R 1 teeth C1-C8 alkyl group, C2-C8 haloalkyl group, C3-C8 cycloalkyl group, C2-C6 cyanoalkyl group, C2-C6 hydroxyalkyl group, (C2-C6 hydroxyalkyl)-O-(C2-C6 alkyl)- group, -(C2-C6 alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4- to 7-membered optionally unsaturated heterocyclic group, a phenyl group, and a monocyclic or bicyclic heteroaryl group, The C1-C8 alkyl group may optionally be C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The C3-C8-cycloalkyl group is optionally substituted once or twice, each substituent being a halogen atom or hydroxy, phenyl and -N(R 7 )(R 8 ) independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The 4- to 7-membered, optionally unsaturated, heterocyclic group is attached to the remainder of the molecule through a carbon atom and is optionally substituted one or two times, and each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C6-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C6-alkyl) and oxo(=O) are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, aryl, -O-aryl, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R7 )(R 8 ), -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C6-alkyl), -S(=O)2-O-(C2-C6-alkenyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -N(O)2, -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two adjacent substituents of the phenyl group may be taken together to optionally form -N=, -NH-, -N(R 7 )-, -O-, -S-, and optionally forming a 5- or 6-membered heterocyclic, aromatic or non-aromatic ring containing a C(=O) group, the ring thus formed being optionally substituted once or twice, and each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(O)2, -N(O)2 and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(O)2, -N(O)2 and -N(R 7 )(R 8 ) are independently selected from groups selected from R 2 represents a hydrogen atom or a halogen atom, R 3 teeth C1-C6 alkyl group, C3-C8 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, C2-C6 alkynyl group, C4-C8 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group, and phenyl group represents a group selected from the 4-7 membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3 alkyl group, the 4- to 7-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OR 6, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2, -N(O)2 and -N(R 7 )(R 8 ) are independently selected from groups selected from R 4 and R 5 together form the 5- to 6-membered, optionally unsaturated heterocyclic ring A of sub-formula (i) [ka] (wherein ring A is a ring that contains two essential atoms, a nitrogen atom and a carbon atom bridging the two rings, as well as -O-, -S-, -S(=O)-, -S(=O)2-, -N=, -N(R 7 )-, -C(=O)-, -CH=, -CR 11 =, -C(R 12 )2-, -CHR 13 -having an additional 3 to 6 members selected from Forming R 6 is a hydrogen atom or C1-C6 alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C6 alkyl groups, C2-C6 alkenyl groups, C2-C6 hydroxyalkyl groups, haloalkyl groups, aryl groups, (C1-C6 alkyl)-aryl groups, and -(C2-C6 alkyl)-N(R 9 )(R 10 ) group represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group may optionally be C1-C6-alkyl, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C3-alkyl), -S(=O)2-(C2-C6-alkenyl) and -C(=O)OR 6 - and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 9 and R 10 together with the nitrogen to which they are attached, Nitrogen-containing 4- to 7-membered heterocycloalkyl groups represents R 11 is independently for each occurrence a hydrogen atom, a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 12 represents, independently for each occurrence, a hydrogen atom, a halogen atom or a C1-C3-alkyl group; R 13 teeth C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1- to C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from and tautomers, N-oxides or salts thereof, and tautomers or N-oxide salts of said compounds.

[0093] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C1-C8-alkyl groups (which may optionally be C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from C2-C8-haloalkyl group, C3-C8-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, hydroxy groups, phenyl groups and -N(R 7 )(R8 ) groups, the phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from halogen atoms, C1-C3-alkyl groups, C1-C4-haloalkyl groups, C1-C3-alkoxy groups and hydroxy groups; C2-C6-cyanoalkyl groups, C2-C6-hydroxyalkyl groups, (C2-C6-hydroxyalkyl)-O-(C2-C6-alkyl)- group -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4- to 7-membered heterocycloalkyl group, which is attached to the remainder of the molecule via a carbon atom of said 4- to 7-membered heterocycloalkyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C6-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C6-alkyl) group and an oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a 5- to 7-membered heterocycloalkenyl group which is attached to the rest of the molecule via a carbon atom of said 5- to 7-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C6-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C6-alkyl) group and an oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two substituents on said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are bonded to each other to form a group selected from indanyl group, tetralinyl group (the indanyl or tetralinyl group is optionally substituted once or twice, each substituent being a halogen atom, a C1-C6-alkyl group, a C1-C6-haloalkyl group, a C3-C8-cycloalkyl group, a C1-C6-alkoxy group, a C1-C6-haloalkoxy group, a C3-C8-cycloalkoxy group, a cyano group, a hydroxy group and -N(R 7 )(R 8 ) groups) and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C6-alkyl group, a C1-C6-haloalkyl group, a C3-C8-cycloalkyl group, a C1-C6-alkoxy group, a C1-C6-haloalkoxy group, a C3-C8-cycloalkoxy group, a cyano group, a hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but C1-C6 alkyl groups C3-C8-cycloalkyl groups, C1-C6-haloalkyl group, C1-C6-hydroxyalkyl group, C2-C6-alkenyl group, C2-C6 alkynyl group, a C4-C8-cycloalkenyl group, (C1-C6-alkyl)-N(R 7 )R 8 base, -(C1-C6-alkyl)-N(H)C(=O)R 6 base, -(C1-C6-alkyl)-N(H)C(=O)OR 15 base, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group wherein the 4-7 membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3 alkyl group; the 4- to 7-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; and a phenyl group, which is optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy; represents a group selected from R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11)-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5The remainder of each represents a CH2 group, R 6 is a hydrogen atom or C1-C6 alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C6-alkyl groups, C2-C6-hydroxyalkyl groups and -(C2-C6-alkyl)-N(R 9 )(R 10 ) group represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally C1-C3-alkyl, -S(=O)2(C1-C3-alkyl) and -C(=O)O(C1-C4-alkyl) and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 9 and R 10 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 7-membered heterocycloalkyl groups represents R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from R 15 but C1-C6 alkyl groups and benzyl groups represents a group selected from Provided is a compound of the above general formula (I), or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0094] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C1-C8 alkyl group, C2-C8 haloalkyl group, C3-C8 cycloalkyl group, C2-C6 cyanoalkyl group, C2-C6 hydroxyalkyl group, (C2-C6 hydroxyalkyl)-O-(C2-C6 alkyl)- group, -(C2-C6 alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4- to 7-membered heterocycloalkyl group, a 5- to 7-membered heterocycloalkenyl group, a phenyl group, an indanyl group, a tetralinyl group, and a monocyclic or bicyclic heteroaryl group; The C1-C8-alkyl group may optionally C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The C3-C8-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the rest of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group, and are optionally substituted one or two times; C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C6-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C6-alkyl) and oxo(=O) are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2, or 3 times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from or when two adjacent substituents of said phenyl group are attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are linked together to form a group selected from The indanyl or tetralinyl group is optionally substituted once or twice, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C3-C8-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C3-C8-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from R 2 represents a hydrogen atom or a fluorine atom, R 3 but C1-C6 alkyl group, C3-C8 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, C2-C6 alkynyl group, C4-C8 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group, and phenyl group represents a group selected from the 4-7 membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3 alkyl group, the 4- to 7-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X1 -X 2 -X 3 -X 4 -X 5 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 6 is a hydrogen atom or C1-C6 alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C6-alkyl groups, C2-C6-hydroxyalkyl groups and -(C2-C6-alkyl)-N(R 9 )(R 10 ) group represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally C1-C3-alkyl, -S(=O)2(C1-C3-alkyl) and -C(=O)O(C1-C4-alkyl) and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 9 and R 10 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 7-membered heterocycloalkyl groups represents R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from Provided are compounds of the above general formula (I), or tautomers, N-oxides or salts thereof, and salts of the tautomers or N-oxides.

[0095] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C1-C6-alkyl groups (which may optionally be C3-C6-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-alkoxy group and a hydroxy group. C2-C6-haloalkyl group, C3-C6-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, hydroxy groups, phenyl groups and -N(R 7 )(R 8 ) groups, the phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from halogen atoms, C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups and hydroxy groups; C2-C6-cyanoalkyl groups, C2-C6-hydroxyalkyl groups, (C2-C3-hydroxyalkyl)-O-(C2-C6-alkyl)- group -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4-6 membered heterocycloalkyl group which is attached to the remainder of the molecule via a carbon atom of said 4-6 membered heterocycloalkyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3 alkyl group, a 5-6 membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C3-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C3-alkyl) group and an oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy Independently selected from groups selected from a 5-6 membered heterocycloalkenyl group which is attached to the rest of the molecule via a carbon atom of said 5-6 membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3 alkyl group, a 5-6 membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C3-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C3-alkyl) group and an oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C3-alkyl, C3-C6-cycloalkyl, C1-C3-haloalkyl, C1-C3-hydroxyalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -(C1-C3-alkyl)-C(=O)OR 6 , -(C1-C3-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two substituents on said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are bonded to each other to form a group selected from indanyl groups, tetralinyl groups (which are optionally substituted once or twice, each substituent being a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C3-C6-cycloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, a C3-C6-cycloalkoxy group, a cyano group, a hydroxy group and -N(R 7 )(R 8 ) groups) and Monocyclic or bicyclic heteroaryl groups (which is optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C3-C6-cycloalkyl group, a C1-C3-alkoxy group, a C1-C3-haloalkoxy group, a C3-C6-cycloalkoxy group, a cyano group, a hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl, C2-C6 alkynyl group, C4-C6 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-N(H)C(=O)R 6 group, -(C1-C6-alkyl)-N(H)C(=O)OR 15 group, -(C1-C6-alkyl)-(4- to 6-membered nitrogen-containing heterocycloalkyl) group, and phenyl group represents a group selected from the 4-6-membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3-alkyl group, the 4- to 6-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11)-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 6 is a hydrogen atom or C1~C 4- Alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C3-alkyl groups, C2-C3-hydroxyalkyl groups and -(C2-C3-alkyl)-N(R 9 )(R 10 ) represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; The 4- to 6-membered nitrogen-containing heterocycloalkyl group may optionally C1-C3-alkyl, -S(=O)2(C1-C3-alkyl) and -C(=O)O(C1-C4-alkyl) and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 9 and R 10 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from R 15 but C1-C4 alkyl groups and benzyl groups represents a group selected from Provided is a compound of the above general formula (I), or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0096] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C1-C6 alkyl group, C2-C6 haloalkyl group, C3-C6 cycloalkyl group, C2-C6 cyanoalkyl group, C2-C6 hydroxyalkyl group, (C2-C3 hydroxyalkyl)-O-(C2-C6 alkyl)- group, -(C2-C6 alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, 4- to 6-membered heterocycloalkyl group, 5- to 6-membered heterocycloalkenyl group, phenyl group, indanyl group, tetralinyl group, and monocyclic or bicyclic heteroaryl group represents a group selected from The C1-C6-alkyl group may optionally C3-C6-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from The C3-C6-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from the 4- to 6-membered heterocycloalkyl group and the 5- to 6-membered heterocycloalkenyl group are attached to the rest of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group and the heterocycloalkenyl group, and are optionally substituted once or twice, and each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2, or 3 times, and each substituent is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C3-alkyl, C3-C6-cycloalkyl, C1-C3-haloalkyl, C1-C3-hydroxyalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -(C1-C3-alkyl)-C(=O)OR 6 , -(C1-C3-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from or when two adjacent substituents of said phenyl group are attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are linked together to form a group selected from The indanyl or tetralinyl group is optionally substituted once or twice, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-haloalkyl, C3-C6-cycloalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-haloalkyl, C3-C6-cycloalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from R 2 represents a hydrogen atom or a fluorine atom, R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl, C2-C6 alkynyl group, C4-C6 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-(4- to 6-membered nitrogen-containing heterocycloalkyl) group, and phenyl group represents a group selected from the 4-6-membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3-alkyl group, the 4- to 6-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X1 -X 2 -X 3 -X 4 -X 5 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 6 is a hydrogen atom or C1~C 4- Alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C3-alkyl groups, C2-C3-hydroxyalkyl groups and -(C2-C3-alkyl)-N(R 9 )(R 10 ) represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; The 4- to 6-membered nitrogen-containing heterocycloalkyl group may optionally C1-C3-alkyl, -S(=O)2(C1-C3-alkyl) and -C(=O)O(C1-C4-alkyl) and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 9 and R 10But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from Provided are compounds of the above general formula (I), as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0097] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C3-C6-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being a halogen atom, a phenyl group and -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom; C2-C6-hydroxyalkyl groups, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group which is attached to the remainder of the molecule via a carbon atom of said 4- to 6-membered heterocycloalkyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3 alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C3-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C3-alkyl) group and an oxo(=O) group; a phenyl group, which is optionally substituted one, two, three or four times, where each substituent is a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-hydroxyalkyl group, a C1-C3-alkoxy group, a cyano group, a hydroxy group, a -C(=O)OR 6 group, -C(=O)N(R 7 )(R 8 ) group, -N(R 7 )(R 8 ) group, -(C1-C3-alkyl)-N(R 7 )(R 8 ) group, -S(=O)2N(R 7 )(R 8 ) groups and SF5, Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together form -CH2-N(R 7 ) bonded to each other to form a group selected from —CH— and —O—CH—C(═O)—NH— an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups (which is optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C3-alkyl group, a C1-C3-alkoxy group, a hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-N(H)C(=O)OR 15 and phenyl groups represents a group selected from R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O-, -S- and -S(=O)(=NR 14 )- represents a group selected from X 1 , X 2 , X 3 and X 4 is C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 6 is a hydrogen atom or C1~C 4- Alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 7 and R 8 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 represents a hydrogen atom, R 12are the same or different and represent a hydrogen atom, a halogen atom, or a C1-C3 alkyl group, R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from R 14 is a hydrogen atom or Cyano and -C(=O)CF3 groups represents a group selected from R 15 represents a C1-C4 alkyl group; Provided is a compound of the above general formula (I), or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0098] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C3-C6-cycloalkyl group, C2-C6-hydroxyalkyl group, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, 4- to 6-membered heterocycloalkyl group, phenyl group, indanyl group, and monocyclic or bicyclic heteroaryl group represents a group selected from The C3-C6-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from the phenyl substituents are optionally substituted one, two or three times, each substituent independently selected from a halogen atom; the 4- to 6-membered heterocycloalkyl group is attached to the remainder of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group and is optionally substituted one or two times, and each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3 or 4 times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Hydroxyalkyl, C1-C3-Alkoxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ) and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R 7 )-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from the indanyl group is optionally substituted with a hydroxy group; The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from R 2 represents a hydrogen atom or a fluorine atom, R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 and phenyl groups represents a group selected from R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O- and -S- represents a group selected from X 1 , X 2 , X 3 and X 4 is C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 6 is a hydrogen atom or C1~C 4- Alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 7 and R 8 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 represents a hydrogen atom, R 12 are the same or different and represent a hydrogen atom, a halogen atom, or a C1-C3 alkyl group, R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from Provided are compounds of the above general formula (I), as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0099] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C3-C6-cycloalkyl groups, which are selected from cyclopropyl and cyclohexyl, and are optionally substituted once or twice, each substituent being a halogen atom, a phenyl group and -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom; C2-C6-hydroxyalkyl groups, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group which is attached to the rest of the molecule via a carbon atom of said 4- to 6-membered heterocycloalkyl group and is selected from azetidinyl, oxetanyl, tetrahydro-2H-pyranyl, tetrahydro-2H-thiopyranyl and piperidinyl, optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C3-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C3-alkyl) group and an oxo(=O) group; a phenyl group, which is optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-hydroxyalkyl group, a C1-C3-alkoxy group, a hydroxy group, a cyano group, a -C(=O)OR 6 group, -C(=O)N(R 7 )(R 8 ) group, -N(R 7 )(R 8 ) group, -(C1-C3-alkyl)-N(R 7 )(R 8 ) group, -S(=O)2N(R 7 )(R 8 ) groups and SF5, Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together form -CH2-N(R 7 ) bonded to each other to form a group selected from —CH— and —O—CH—C(═O)—NH— an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups selected from imidazolyl, 1,2-oxazolyl, pyrazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, 1,3-benzothiazolyl, pyrrolo[2,3-d]pyrimidinyl and quinolinyl; optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy group and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-N(H)C(=O)OR 15 and phenyl groups represents a group selected from R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1-X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O-, -S- and -S(=O)(=NH)- represents a group selected from X 1, X 2 , X 3 and X 4 One of them is C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 6 is a hydrogen atom or C1~C 4- Alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 7 and R 8 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 represents a hydrogen atom, R 12 are the same or different and represent a hydrogen atom, a halogen atom, or a C1-C3 alkyl group, R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from R 15 represents a C1-C4 alkyl group; Provided is a compound of the above general formula (I), or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0100] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C3-C6-cycloalkyl group, C2-C6-hydroxyalkyl group, -(C2-C6-alkyl)-N(R 7 )(R8 ) group, 4- to 6-membered heterocycloalkyl group, phenyl group, indanyl group, and monocyclic or bicyclic heteroaryl group represents a group selected from the C3-C6-cycloalkyl group is selected from cyclopropyl and cyclohexyl; The C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from the phenyl substituents are optionally substituted one, two or three times, each substituent independently selected from a halogen atom; the 4- to 6-membered heterocycloalkyl group is attached to the remainder of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group; Azetidinyl, oxetanyl, tetrahydro-2H-pyranyl, tetrahydro-2H-thiopyranyl, and piperidinyl is selected from The 4- to 6-membered heterocycloalkyl group is optionally substituted once or twice, and each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Hydroxyalkyl, C1-C3-Alkoxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8), -S(=O)2N(R 7 )(R 8 ) and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R 7 )-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from the indanyl group is optionally substituted with a hydroxy group; The monocyclic or bicyclic heteroaryl group is Imidazolyl, 1,2-oxazolyl, pyrazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, 1,3-benzothiazolyl, pyrrolo[2,3-d]pyrimidinyl, and quinolinyl is selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from R 2 represents a hydrogen atom or a fluorine atom, R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 and phenyl groups represents a group selected from R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2-X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O- and -S- represents a group selected from X 1 , X 2 , X 3 and X 4 One of them is C(R 12 ) represents two groups, X1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 6 is a hydrogen atom or C1~C 4- Alkyl group, benzyl group represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C3 alkyl groups Represents, or R 7 and R 8 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 represents a hydrogen atom, R 12 are the same or different and represent a hydrogen atom, a halogen atom, or a C1-C3 alkyl group, R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from Provided are compounds of the above general formula (I), as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0101] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C3-C6-cycloalkyl groups, which are selected from cyclopropyl and cyclohexyl groups, the C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a phenyl group, and a dimethylamino group; the phenyl substituents are optionally substituted with fluorine atoms; 2-hydroxy-2-methylpropyl group, 2-(dimethylamino)ethyl group, a 4- to 6-membered heterocycloalkyl group selected from azetidin-3-yl, oxetan-3-yl, tetrahydro-2H-pyran-4-yl, tetrahydro-2H-thiopyran-4-yl and piperidin-4-yl; optionally substituted once or twice, each substituent independently selected from the group consisting of methyl, ethyl, pyrazinyl, tert-butoxycarbonyl, acetyl, 1-cyclopropanecarbonyl, methylsulfonyl, and oxo (=O); a phenyl group, which is optionally substituted one, two or three times, and each substituent is a fluorine atom, a chlorine atom, a methyl group, an ethyl group, a difluoromethyl group, a trifluoromethyl group, a hydroxymethyl group, a methoxy group, a hydroxy group, a cyano group, a -C(=O)OH group, a -C(=O)OCH3 group, a -C(=O)OC(CH3) group, a -C(=O)NH 2、 independently selected from a -C(=O)N(CH3)2 group, an amino group, a methylamino group, an aminomethyl group, a -S(=O)2NH2 group, and an SF5 group; or two substituents of said phenyl group, when attached to adjacent ring atoms, are optionally linked to each other so as to form, together, a group selected from -CH-CH-NH-CH- and -O-CH-C(=O)-NH-. 2-hydroxyindan-1-yl group and Monocyclic or bicyclic heteroaryl groups (this is Imidazol-4-yl, 1,2-oxazol-4-yl, 1,2-oxazol-5-yl, pyrazol-3-yl, pyrazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, pyrazinyl, pyrimidin-4-yl, pyrimidin-5-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, 1,3-benzothiazol-6-yl, pyrrolo[2,3-d]pyrimidin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl and quinolin-8-yl is selected from optionally substituted one, two or three times, each substituent being independently selected from fluorine, chlorine, methyl, methoxy, hydroxy and morpholin-4-yl groups; represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but Propyl, cyclohexyl, trifluoromethyl, 1-hydroxyethyl, allyl, aminomethyl, (dimethylamino)methyl, (tert-butoxycarbonylamino)methyl, 2-(dimethylamino)ethyl, pyrrolidin-1-yl-methyl, and phenyl represents a group selected from R 4 and R 5 But together, *-(CH2)2-S-#, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-CH(OH)-(CH2)3-#, *-CH2-CH(OH)-(CH2)2-#, *-(CH2)2-CH(OH)-CH2-#, *-(CH2)3-C(H)(OH)-#, *-CH=CH-CH(OH)-CH2-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)3-S(=O)(=NH)-#, *-(CH2)5-#, *-(CH2)3-O-CH2-#, *-(CH2)2-N(H)-(CH2)2-#, *-CH=CH-CH=CH-#, *-N=CH-CH=CH-#, and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided is a compound of the above general formula (I), or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0102] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C3-C6-cycloalkyl group, 2-hydroxy-2-methylpropyl group, 2-(dimethylamino)ethyl group, 4- to 6-membered heterocycloalkyl group, phenyl group, 2-hydroxyindan-1-yl group, and monocyclic or bicyclic heteroaryl group represents a group selected from the C3-C6-cycloalkyl group is selected from cyclopropyl and cyclohexyl; The C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being a fluorine atom or Phenyl and dimethylamino are independently selected from groups selected from the phenyl substituents are optionally substituted with fluorine atoms; The 4- to 6-membered heterocycloalkyl group Azetidin-3-yl, oxetan-3-yl, tetrahydro-2H-pyran-4-yl, tetrahydro-2H-thiopyran-4-yl and piperidin-4-yl is selected from The 4- to 6-membered heterocycloalkyl group is optionally substituted once or twice, and each substituent is Methyl, ethyl, pyrazinyl, tert-butoxycarbonyl, acetyl, 1-cyclopropanecarbonyl, methylsulfonyl, and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted one, two or three times, each substituent being a fluorine atom or a chlorine atom or Methyl, ethyl, difluoromethyl, trifluoromethyl, hydroxymethyl, methoxy, cyano, -C(=O)OH, -C(=O)OCH3, -C(=O)OC(CH3)3, -C(=O)NH 2、 -C(=O)N(CH3)2, amino, methylamino, aminomethyl, -S(=O)2NH2 and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH-CH2-NH-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from The monocyclic or bicyclic heteroaryl group is Imidazol-4-yl, 1,2-oxazol-4-yl, 1,2-oxazol-5-yl, pyrazol-3-yl, pyrazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, pyrazinyl, pyrimidin-4-yl, pyrimidin-5-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, 1,3-benzothiazol-6-yl, pyrrolo[2,3-d]pyrimidin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl and quinolin-8-yl is selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a fluorine or chlorine atom or Methyl, methoxy, hydroxy and morpholin-4-yl are independently selected from groups selected from R 2represents a hydrogen atom or a fluorine atom, R 3 but Propyl, cyclohexyl, trifluoromethyl, 1-hydroxyethyl, allyl, (dimethylamino)methyl, 2-(dimethylamino)ethyl, pyrrolidin-1-yl-methyl and phenyl represents a group selected from R 4 and R 5 But together, *-(CH2)2-S-#, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-(CH2)3-C(H)(OH)-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)5-#, *-(CH2)3-O-CH2-#, *-(CH2)2-N(H)-(CH2)2-#, *-CH=CH-CH=CH-#, *-N=CH-CH=CH-#, and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of the above general formula (I), as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0103] According to further embodiments, the present invention provides compounds of general formula (I) above as exemplified in the experimental section.

[0104] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C1-C8-alkyl groups (which may optionally be C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from the phenyl substituents are optionally substituted one, two or three times with one or more substituents independently selected from halogen atoms, C1-C3-alkyl groups, C1-C4-haloalkyl groups, C1-C3-alkoxy groups and hydroxy groups, C2-C8-haloalkyl group, C3-C8-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, hydroxy groups, phenyl groups and -N(R 7 )(R 8 ) groups, the phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from halogen atoms, C1-C3-alkyl groups, C1-C4-haloalkyl groups, C1-C3-alkoxy groups and hydroxy groups; C2-C6-cyanoalkyl groups, C2-C6-hydroxyalkyl groups, (C2-C6-hydroxyalkyl)-O-(C2-C6-alkyl)- group -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4-7 membered optionally unsaturated heterocyclic group which is attached to the rest of the molecule via a carbon atom and is optionally substituted once or twice, each substituent being independently selected from C1-C3 alkyl groups, 5-6 membered heteroaryl groups, -C(=O)O(C1-C4 alkyl) groups, -C(=O)(C1-C6 alkyl) groups, -C(=O)(C3-C6 cycloalkyl) groups, -S(=O)2(C1-C6 alkyl) groups and oxo(=O) groups; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, aryl, -O-aryl, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C6-alkyl), -S(=O)2-O-(C2-C6-alkenyl), -S(=O)(=NR14 )(C1-C3-alkyl), -N(O)2, -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two adjacent substituents of the phenyl group may be taken together to optionally form -N=, -NH-, -N(R 7 )-, -O-, -S-, and optionally forming a 5- or 6-membered heterocyclic, aromatic or non-aromatic ring containing a C(=O) group, the ring thus formed being optionally substituted once or twice, and each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(═O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) (independently selected from groups selected from and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of which is a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R8 ) Independently selected from groups selected from represents a group selected from A compound of formula (I) above is provided. In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C1-C8-alkyl groups (which may optionally be C3-C8 cycloalkyl groups, phenyl groups and monocyclic or bicyclic heteroaryl groups and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy and C2-C8-haloalkyl group, C3-C8-cycloalkyl groups, which are optionally substituted one or two times, each of which is a halogen atom or a hydroxy group, a phenyl group and -N(R 7 )(R 8 ) groups, the phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy, C2-C6-cyanoalkyl groups, C2-C6-hydroxyalkyl groups, (C2-C6-hydroxyalkyl)-O-(C2-C6-alkyl)- group -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4-7 membered optionally unsaturated heterocyclic group which is attached to the rest of the molecule via a carbon atom and is optionally substituted once or twice, each substituent being independently selected from the group selected from C1-C3-alkyl, 5-6 membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C6-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C6-alkyl) and oxo(=O); The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or a C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, aryl, -O-aryl, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C6-alkyl), -S(=O)2-O-(C2-C6-alkenyl), -S(=O)(=NR 14)(C1-C3-alkyl), -N(O)2, -P(=O)(C1-C3-alkyl)2 and SF5, Alternatively, two adjacent substituents of the phenyl group may be taken together to optionally form -N=, -NH-, -N(R 7 )-, -O-, -S-, and optionally forming a 5- or 6-membered heterocyclic, aromatic or non-aromatic ring containing a C(=O) group, the ring thus formed being optionally substituted once or twice, and each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(═O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) (independently selected from groups selected from and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of which is a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, or salts of the tautomers or N-oxides of said compounds.

[0105] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C1-C8 alkyl group, C2-C8 haloalkyl group, C3-C8 cycloalkyl group, C2-C6 cyanoalkyl group, C2-C6 hydroxyalkyl group, (C2-C6 hydroxyalkyl)-O-(C2-C6 alkyl)- group, -(C2-C6 alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4- to 7-membered optionally unsaturated heterocyclic group, a phenyl group, and a monocyclic or bicyclic heteroaryl group, The C1-C8 alkyl group may optionally be C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The C3-C8-cycloalkyl group is optionally substituted once or twice, each substituent being a halogen atom or hydroxy, phenyl and -N(R 7 )(R 8 ) independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from said 4- to 7-membered, optionally unsaturated, heterocyclic group being attached to the remainder of the molecule through a carbon atom and optionally substituted once or twice, each substituent being C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C6-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C6-alkyl) and oxo(=O) are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2, or 3 times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, aryl, -O-aryl, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2N(R 7 )(R 8), -S(=O)2(C1-C6-alkyl), -S(=O)2-O-(C2-C6-alkenyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -N(O)2, -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two adjacent substituents of the phenyl group may be taken together to optionally form -N=, -NH-, -N(R 7 )-, -O-, -S-, and optionally forming a 5- or 6-membered heterocyclic, aromatic or non-aromatic ring containing a C(=O) group, the ring thus formed being optionally substituted once or twice, and each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(O)2, -N(O)2 and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(O)2, -N(O)2 and -N(R7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0106] According to a further embodiment, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or a C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 11 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5, or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are bonded to each other to form a group selected from Compounds of general formula (I) are provided: According to a further embodiment, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 represents a phenyl group, which is optionally substituted one or two times, each substituent being independently selected from a fluorine atom, a chlorine atom, and a methyl group; Compounds of general formula (I) are provided:

[0107] According to a further embodiment, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 is a C4-C8-cycloalkyl group or -(C3-C8-cycloalkyl)-N(R 7 )(R 8 ) groups, which are optionally substituted one or two times, each substituent being a halogen atom or hydroxy, phenyl and -N(R 7 )(R 8 ) independently selected from groups selected from wherein the phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom or a group selected from C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy; Provided are compounds of general formula (I), as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0108] According to a further embodiment, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 represents a 4- to 7-membered heterocycloalkyl group or a 5- to 7-membered heterocycloalkenyl group, wherein the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are optionally substituted once or twice, and each substituent is independently selected from the group consisting of C1-C3-alkyl, 5- to 6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C6-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C6-alkyl) and oxo(=O); the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups are attached to the rest of the molecule through a carbon atom of the heterocycloalkyl or heterocycloalkenyl group; Provided are compounds of general formula (I), as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0109] According to a further embodiment, the present invention provides a compound comprising R 1 represents an indanyl group, a tetralinyl group, or a monocyclic or bicyclic heteroaryl group; The indanyl or tetralinyl group is optionally substituted one or two times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C3-C8-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C3-C8-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of general formula (I), as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0110] According to a further embodiment, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C1-C8-alkyl groups (which may optionally be C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from C2-C8-haloalkyl group, C3-C8-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, hydroxy groups, phenyl groups and -N(R 7 )(R 8 ) groups, the phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from halogen atoms, C1-C3-alkyl groups, C1-C4-haloalkyl groups, C1-C3-alkoxy groups and hydroxy groups; C2-C6-cyanoalkyl groups, C2-C6-hydroxyalkyl groups, (C2-C6-hydroxyalkyl)-O-(C2-C6-alkyl)- group -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4- to 7-membered heterocycloalkyl group, which is attached to the remainder of the molecule via a carbon atom of said 4- to 7-membered heterocycloalkyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C6-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C6-alkyl) group and an oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a 5- to 7-membered heterocycloalkenyl group which is attached to the rest of the molecule via a carbon atom of said 5- to 7-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C6-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C6-alkyl) group and an oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two substituents on said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are bonded to each other to form a group selected from indanyl group, tetralinyl group (the indanyl or tetralinyl group is optionally substituted once or twice, each substituent being a halogen atom, a C1-C6-alkyl group, a C1-C6-haloalkyl group, a C3-C8-cycloalkyl group, a C1-C6-alkoxy group, a C1-C6-haloalkoxy group, a C3-C8-cycloalkoxy group, a cyano group, a hydroxy group and -N(R 7 )(R 8 ) groups) and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C6-alkyl group, a C1-C6-haloalkyl group, a C3-C8-cycloalkyl group, a C1-C6-alkoxy group, a C1-C6-haloalkoxy group, a C3-C8-cycloalkoxy group, a cyano group, a hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0111] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C1-C8 alkyl group, C2-C8 haloalkyl group, C3-C8 cycloalkyl group, C2-C6 cyanoalkyl group, C2-C6 hydroxyalkyl group, (C2-C6 hydroxyalkyl)-O-(C2-C6 alkyl)- group, -(C2-C6 alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8) group, a 4- to 7-membered heterocycloalkyl group, a 5- to 7-membered heterocycloalkenyl group, a phenyl group, an indanyl group, a tetralinyl group, and a monocyclic or bicyclic heteroaryl group; The C1-C8-alkyl group may optionally C3-C8-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The C3-C8-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the rest of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group, and are optionally substituted one or two times; C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C6-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C6-alkyl) and oxo(=O) are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2, or 3 times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from or when two adjacent substituents of said phenyl group are attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are linked together to form a group selected from The indanyl or tetralinyl group is optionally substituted one or two times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C3-C8-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C3-C8-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0112] According to a further embodiment, the present invention provides a method for producing a medicament for the treatment of a pulmonary arthritis, comprising: R 1 but C3-C8-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, hydroxy groups, phenyl groups and -N(R 7 )(R 8 ) groups, the phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from halogen atoms, C1-C3-alkyl groups, C1-C4-haloalkyl groups, C1-C3-alkoxy groups and hydroxy groups; a 4- to 7-membered heterocycloalkyl group, which is attached to the remainder of the molecule via a carbon atom of said 4- to 7-membered heterocycloalkyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C6-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C6-alkyl) group and an oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a 5- to 7-membered heterocycloalkenyl group which is attached to the rest of the molecule via a carbon atom of said 5- to 7-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C6-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C6-alkyl) group and an oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted one, two, or three times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from Alternatively, two substituents on said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are bonded to each other to form a group selected from indanyl group, tetralinyl group (the indanyl or tetralinyl group is optionally substituted once or twice, each substituent being a halogen atom, a C1-C6-alkyl group, a C1-C6-haloalkyl group, a C3-C8-cycloalkyl group, a C1-C6-alkoxy group, a C1-C6-haloalkoxy group, a C3-C8-cycloalkoxy group, a cyano group, a hydroxy group and -N(R 7 )(R 8 ) groups) and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C6-alkyl group, a C1-C6-haloalkyl group, a C3-C8-cycloalkyl group, a C1-C6-alkoxy group, a C1-C6-haloalkoxy group, a C3-C8-cycloalkoxy group, a cyano group, a hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0113] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but represents a group selected from a C3-C8 cycloalkyl group, a 4- to 7-membered heterocycloalkyl group, a 5- to 7-membered heterocycloalkenyl group, a phenyl group, an indanyl group, a tetralinyl group, and a monocyclic or bicyclic heteroaryl group, The C3-C8-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the rest of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group, and are optionally substituted one or two times; C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C6-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C6-alkyl) and oxo(=O) are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2, or 3 times, and each substituent is a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C6-alkyl)-N(R 7 )(R 8 ), -(C1-C6-alkyl)-C(=O)OR 6 , -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from or when two adjacent substituents of said phenyl group are attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are linked together to form a group selected from The indanyl or tetralinyl group is optionally substituted one or two times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C3-C8-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C3-C8-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0114] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C1-C6 alkyl group, C2-C6 haloalkyl group, C3-C6 cycloalkyl group, C2-C6 cyanoalkyl group, C2-C6 hydroxyalkyl group, (C2-C3 hydroxyalkyl)-O-(C2-C6 alkyl)- group, -(C2-C6 alkyl)-N(R 7 )(R 8 ) group, -(C1-C6-alkyl)-C(=O)N(R 7 )(R 8 ) group, 4- to 6-membered heterocycloalkyl group, 5- to 6-membered heterocycloalkenyl group, phenyl group, indanyl group, tetralinyl group, and monocyclic or bicyclic heteroaryl group represents a group selected from The C1-C6-alkyl group may optionally C3-C6-cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from The C3-C6-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from the 4- to 6-membered heterocycloalkyl group and the heterocycloalkenyl group are attached to the rest of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group and the heterocycloalkenyl group, and are optionally substituted one or two times; C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2, or 3 times, and each substituent is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C3-alkyl, C3-C6-cycloalkyl, C1-C3-haloalkyl, C1-C3-hydroxyalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -(C1-C3-alkyl)-C(=O)OR 6 , -(C1-C3-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from or when two adjacent substituents of said phenyl group are attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are linked together to form a group selected from The indanyl or tetralinyl group is optionally substituted one or two times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-haloalkyl, C3-C6-cycloalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-haloalkyl, C3-C6-cycloalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0115] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but represents a group selected from a C3-C6-cycloalkyl group, a 4- to 6-membered heterocycloalkyl group, a heterocycloalkenyl group, a phenyl group, an indanyl group, a tetralinyl group, and a monocyclic or bicyclic heteroaryl group, The C3-C6-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from the 4- to 6-membered heterocycloalkyl group and the heterocycloalkenyl group are attached to the rest of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group and the heterocycloalkenyl group, and are optionally substituted one or two times; C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2, or 3 times, and each substituent is a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C1-C3-alkyl, C3-C6-cycloalkyl, C1-C3-haloalkyl, C1-C3-hydroxyalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -(C1-C3-alkyl)-C(=O)OR 6 , -(C1-C3-alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ), -S(=O)2(C1-C3-alkyl), -S(=O)(=NR 14 )(C1-C3-alkyl), -P(=O)(C1-C3-alkyl)2 and SF5 Independently selected from groups selected from or when two adjacent substituents of said phenyl group are attached to adjacent ring atoms, optionally together represent: -CH2-N(R 7 )-CH2-, -CH2-O-CH2-, -O-CH2-C(=O)-NH- and -NH-C(=O)-NH- are linked together to form a group selected from The indanyl or tetralinyl group is optionally substituted one or two times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-haloalkyl, C3-C6-cycloalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-haloalkyl, C3-C6-cycloalkyl, C1-C3-alkoxy, C1-C3-haloalkoxy, C3-C6-cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0116] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being a halogen atom, a phenyl group and an -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom; C2-C6-hydroxyalkyl groups, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group which is attached to the remainder of the molecule via a carbon atom of said 4- to 6-membered heterocycloalkyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3 alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C3-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C3-alkyl) group and an oxo(=O) group; a phenyl group, which is optionally substituted one, two, three or four times, where each substituent is a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-hydroxyalkyl group, a C1-C3-alkoxy group, a cyano group, a hydroxy group, a -C(=O)OR 6 group, -C(=O)N(R 7 )(R 8 ) group, -N(R 7 )(R 8 ) group, -(C1-C3-alkyl)-N(R 7 )(R 8 ) group, -S(=O)2N(R 7 )(R 8 ) groups and SF5, Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together form -CH2-N(R 7 ) bonded to each other to form a group selected from —CH— and —O—CH—C(═O)—NH— an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups (which is optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C3-alkyl group, a C1-C3-alkoxy group, a hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0117] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl group, C2-C6-hydroxyalkyl group, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, 4- to 6-membered heterocycloalkyl group, phenyl group, indanyl group, and monocyclic or bicyclic heteroaryl group represents a group selected from The C3-C6-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from the phenyl substituents are optionally substituted one, two or three times, each substituent independently selected from a halogen atom; the 4- to 6-membered heterocycloalkyl group is attached to the remainder of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group and is optionally substituted one or two times, and each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3 or 4 times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Hydroxyalkyl, C1-C3-Alkoxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ) and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R 7 )-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from the indanyl group is optionally substituted with a hydroxy group; The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0118] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being a halogen atom, a phenyl group and an -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom; a 4- to 6-membered heterocycloalkyl group which is attached to the remainder of the molecule via a carbon atom of said 4- to 6-membered heterocycloalkyl group and is optionally substituted once or twice, each substituent being independently selected from a C1-C3 alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C3-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C3-alkyl) group and an oxo(=O) group; a phenyl group, which is optionally substituted one, two, three or four times, where each substituent is a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-hydroxyalkyl group, a C1-C3-alkoxy group, a cyano group, a hydroxy group, a -C(=O)OR 6 group, -C(=O)N(R 7 )(R 8 ) group, -N(R 7 )(R8 ) group, -(C1-C3-alkyl)-N(R 7 )(R 8 ) group, -S(=O)2N(R 7 )(R 8 ) groups and SF5, Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together form -CH2-N(R 7 ) bonded to each other to form a group selected from —CH— and —O—CH—C(═O)—NH— an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups (which is optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C3-alkyl group, a C1-C3-alkoxy group, a hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0119] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, 4- to 6-membered heterocycloalkyl groups, phenyl groups, indanyl groups, and monocyclic or bicyclic heteroaryl groups represents a group selected from The C3-C6-cycloalkyl group is optionally substituted once or twice, and each substituent is a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from the phenyl substituents are optionally substituted one, two or three times, each substituent independently selected from a halogen atom; the 4- to 6-membered heterocycloalkyl group is attached to the remainder of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group and is optionally substituted one or two times, and each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted 1, 2, 3 or 4 times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Hydroxyalkyl, C1-C3-Alkoxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ) and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R 7 )-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from the indanyl group is optionally substituted with a hydroxy group; The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0120] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are selected from cyclopropyl and cyclohexyl, and are optionally substituted once or twice, each substituent being a halogen atom, a phenyl group and -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom; C2-C6-hydroxyalkyl groups, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group which is attached to the rest of the molecule via a carbon atom of said 4- to 6-membered heterocycloalkyl group and is selected from azetidinyl, oxetanyl, tetrahydro-2H-pyranyl, tetrahydro-2H-thiopyranyl and piperidinyl, optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C3-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C3-alkyl) group and an oxo(=O) group; a phenyl group, which is optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-hydroxyalkyl group, a C1-C3-alkoxy group, a hydroxy group, a cyano group, a -C(=O)OR 6 group, -C(=O)N(R 7 )(R 8 ) group, -N(R 7 )(R 8 ) group, -(C1-C3-alkyl)-N(R 7 )(R 8) group, -S(=O)2N(R 7 )(R 8 ) groups and SF5, Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together form -CH2-N(R 7 ) bonded to each other to form a group selected from —CH— and —O—CH—C(═O)—NH— an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups selected from imidazolyl, 1,2-oxazolyl, pyrazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, 1,3-benzothiazolyl, pyrrolo[2,3-d]pyrimidinyl and quinolinyl; optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy group and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0121] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl group, C2-C6-hydroxyalkyl group, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, 4- to 6-membered heterocycloalkyl group, phenyl group, indanyl group, and monocyclic or bicyclic heteroaryl group represents a group selected from the C3-C6-cycloalkyl group is selected from cyclopropyl and cyclohexyl; The C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from the phenyl substituents are optionally substituted one, two or three times, each substituent independently selected from a halogen atom; the 4- to 6-membered heterocycloalkyl group is attached to the remainder of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group; Azetidinyl, oxetanyl, tetrahydro-2H-pyranyl, tetrahydro-2H-thiopyranyl, and piperidinyl is selected from The 4- to 6-membered heterocycloalkyl group is optionally substituted once or twice, and each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Hydroxyalkyl, C1-C3-Alkoxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ) and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R7 )-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from the indanyl group is optionally substituted with a hydroxy group; The monocyclic or bicyclic heteroaryl group is Imidazolyl, 1,2-oxazolyl, pyrazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, 1,3-benzothiazolyl, pyrrolo[2,3-d]pyrimidinyl, and quinolinyl is selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0122] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are selected from cyclopropyl and cyclohexyl, and are optionally substituted once or twice, each substituent being a halogen atom, a phenyl group and -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom; a 4- to 6-membered heterocycloalkyl group which is attached to the rest of the molecule via a carbon atom of said 4- to 6-membered heterocycloalkyl group and is selected from azetidinyl, oxetanyl, tetrahydro-2H-pyranyl, tetrahydro-2H-thiopyranyl and piperidinyl, optionally substituted once or twice, each substituent being independently selected from a C1-C3-alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C1-C4-alkyl) group, a -C(=O)(C1-C3-alkyl) group, a -C(=O)(C3-C6-cycloalkyl) group, a -S(=O)2(C1-C3-alkyl) group and an oxo(=O) group; a phenyl group, which is optionally substituted one, two or three times, each substituent being a halogen atom, a C1-C3-alkyl group, a C1-C3-haloalkyl group, a C1-C3-hydroxyalkyl group, a C1-C3-alkoxy group, a hydroxy group, a cyano group, a -C(=O)OR 6 group, -C(=O)N(R 7 )(R 8 ) group, -N(R 7 )(R 8 ) group, -(C1-C3-alkyl)-N(R 7 )(R 8 ) group, -S(=O)2N(R 7 )(R 8 ) groups and SF5, Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together form -CH2-N(R 7 ) bonded to each other to form a group selected from —CH— and —O—CH—C(═O)—NH— an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups selected from imidazolyl, 1,2-oxazolyl, pyrazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, 1,3-benzothiazolyl, pyrrolo[2,3-d]pyrimidinyl and quinolinyl; optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy group and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0123] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, 4- to 6-membered heterocycloalkyl groups, phenyl groups, indanyl groups, and monocyclic or bicyclic heteroaryl groups represents a group selected from the C3-C6-cycloalkyl group is selected from cyclopropyl and cyclohexyl; The C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from groups selected from the phenyl substituents are optionally substituted one, two or three times, each substituent independently selected from a halogen atom; the 4- to 6-membered heterocycloalkyl group is attached to the remainder of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group; Azetidinyl, oxetanyl, tetrahydro-2H-pyranyl, tetrahydro-2H-thiopyranyl, and piperidinyl is selected from The 4- to 6-membered heterocycloalkyl group is optionally substituted once or twice, and each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Hydroxyalkyl, C1-C3-Alkoxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ) and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R 7 )-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from the indanyl group is optionally substituted with a hydroxy group; The monocyclic or bicyclic heteroaryl group is Imidazolyl, 1,2-oxazolyl, pyrazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, 1,3-benzothiazolyl, pyrrolo[2,3-d]pyrimidinyl, and quinolinyl is selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0124] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are selected from cyclopropyl and cyclohexyl groups, the C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a phenyl group, and a dimethylamino group; the phenyl substituents are optionally substituted with fluorine atoms; 2-hydroxy-2-methylpropyl group, 2-(dimethylamino)ethyl group, a 4- to 6-membered heterocycloalkyl group selected from azetidin-3-yl, oxetan-3-yl, tetrahydro-2H-pyran-4-yl, tetrahydro-2H-thiopyran-4-yl and piperidin-4-yl; optionally substituted once or twice, each substituent independently selected from the group consisting of methyl, ethyl, pyrazinyl, tert-butoxycarbonyl, acetyl, 1-cyclopropanecarbonyl, methylsulfonyl, and oxo (=O); a phenyl group, which is optionally substituted one, two or three times, and each substituent is a fluorine atom, a chlorine atom, a methyl group, an ethyl group, a difluoromethyl group, a trifluoromethyl group, a hydroxymethyl group, a methoxy group, a hydroxy group, a cyano group, a -C(=O)OH group, a -C(=O)OCH3 group, a -C(=O)OC(CH3) group, a -C(=O)NH 2、 independently selected from a -C(=O)N(CH3)2 group, an amino group, a methylamino group, an aminomethyl group, a -S(=O)2NH2 group, and an SF5 group; or two substituents of said phenyl group, when attached to adjacent ring atoms, are optionally linked to each other so as to form, together, a group selected from -CH-CH-NH-CH- and -O-CH-C(=O)-NH-. 2-hydroxyindan-1-yl group and Monocyclic or bicyclic heteroaryl groups (this is Imidazol-4-yl, 1,2-oxazol-4-yl, 1,2-oxazol-5-yl, pyrazol-3-yl, pyrazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, pyrazinyl, pyrimidin-4-yl, pyrimidin-5-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, 1,3-benzothiazol-6-yl, pyrrolo[2,3-d]pyrimidin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl and quinolin-8-yl is selected from optionally substituted one, two or three times, each substituent being independently selected from fluorine, chlorine, methyl, methoxy, hydroxy and morpholin-4-yl groups; represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0125] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl group, 2-hydroxy-2-methylpropyl group, 2-(dimethylamino)ethyl group, 4- to 6-membered heterocycloalkyl group, phenyl group, 2-hydroxyindan-1-yl group, and monocyclic or bicyclic heteroaryl group represents a group selected from the C3-C6-cycloalkyl group is selected from cyclopropyl and cyclohexyl; The C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being a fluorine atom or Phenyl and dimethylamino are independently selected from groups selected from the phenyl substituents are optionally substituted with fluorine atoms; The 4- to 6-membered heterocycloalkyl group Azetidin-3-yl, oxetan-3-yl, tetrahydro-2H-pyran-4-yl, tetrahydro-2H-thiopyran-4-yl and piperidin-4-yl is selected from The 4- to 6-membered heterocycloalkyl group is optionally substituted once or twice, and each substituent is Methyl, ethyl, pyrazinyl, tert-butoxycarbonyl, acetyl, 1-cyclopropanecarbonyl, methylsulfonyl, and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted one, two or three times, each substituent being a fluorine atom or a chlorine atom or Methyl, ethyl, difluoromethyl, trifluoromethyl, hydroxymethyl, methoxy, cyano, -C(=O)OH, -C(=O)OCH3, -C(=O)OC(CH3)3, -C(=O)NH 2、 -C(=O)N(CH3)2, amino, methylamino, aminomethyl, -S(=O)2NH2 and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH-CH2-NH-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from The monocyclic or bicyclic heteroaryl group is Imidazol-4-yl, 1,2-oxazol-4-yl, 1,2-oxazol-5-yl, pyrazol-3-yl, pyrazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, pyrazinyl, pyrimidin-4-yl, pyrimidin-5-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, 1,3-benzothiazol-6-yl, pyrrolo[2,3-d]pyrimidin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl and quinolin-8-yl is selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a fluorine or chlorine atom or Methyl, methoxy, hydroxy and morpholin-4-yl Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0126] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are selected from cyclopropyl and cyclohexyl groups, the C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a phenyl group, and a dimethylamino group; the phenyl substituents are optionally substituted with fluorine atoms; a 4- to 6-membered heterocycloalkyl group selected from azetidin-3-yl, oxetan-3-yl, tetrahydro-2H-pyran-4-yl, tetrahydro-2H-thiopyran-4-yl and piperidin-4-yl; optionally substituted once or twice, each substituent independently selected from the group consisting of methyl, ethyl, pyrazinyl, tert-butoxycarbonyl, acetyl, 1-cyclopropanecarbonyl, methylsulfonyl, and oxo (=O); a phenyl group, which is optionally substituted one, two or three times, and each substituent is a fluorine atom, a chlorine atom, a methyl group, an ethyl group, a difluoromethyl group, a trifluoromethyl group, a hydroxymethyl group, a methoxy group, a hydroxy group, a cyano group, a -C(=O)OH group, a -C(=O)OCH3 group, a -C(=O)OC(CH3) group, a -C(=O)NH 2、 independently selected from a -C(=O)N(CH3)2 group, an amino group, a methylamino group, an aminomethyl group, a -S(=O)2NH2 group, and an SF5 group; or two substituents of said phenyl group, when attached to adjacent ring atoms, are optionally linked to each other so as to form, together, a group selected from -CH-CH-NH-CH- and -O-CH-C(=O)-NH-. 2-hydroxyindan-1-yl group and Monocyclic or bicyclic heteroaryl groups (this is Imidazol-4-yl, 1,2-oxazol-4-yl, 1,2-oxazol-5-yl, pyrazol-3-yl, pyrazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, pyrazinyl, pyrimidin-4-yl, pyrimidin-5-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, 1,3-benzothiazol-6-yl, pyrrolo[2,3-d]pyrimidin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl and quinolin-8-yl is selected from optionally substituted one, two or three times, each substituent being independently selected from fluorine, chlorine, methyl, methoxy, hydroxy and morpholin-4-yl groups; represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0127] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, 4- to 6-membered heterocycloalkyl groups, phenyl groups, 2-hydroxyindan-1-yl groups, and monocyclic or bicyclic heteroaryl groups represents a group selected from the C3-C6-cycloalkyl group is selected from cyclopropyl and cyclohexyl; The C3-C6-cycloalkyl group is optionally substituted once or twice, each substituent being a fluorine atom or Phenyl and dimethylamino are independently selected from groups selected from the phenyl substituents are optionally substituted with fluorine atoms; The 4- to 6-membered heterocycloalkyl group Azetidin-3-yl, oxetan-3-yl, tetrahydro-2H-pyran-4-yl, tetrahydro-2H-thiopyran-4-yl and piperidin-4-yl is selected from The 4- to 6-membered heterocycloalkyl group is optionally substituted once or twice, and each substituent is Methyl, ethyl, pyrazinyl, tert-butoxycarbonyl, acetyl, 1-cyclopropanecarbonyl, methylsulfonyl, and oxo(=O) are independently selected from groups selected from The phenyl group is optionally substituted one, two or three times, each substituent being a fluorine atom or a chlorine atom or Methyl, ethyl, difluoromethyl, trifluoromethyl, hydroxymethyl, methoxy, cyano, -C(=O)OH, -C(=O)OCH3, -C(=O)OC(CH3)3, -C(=O)NH 2、-C(=O)N(CH3)2, amino, methylamino, aminomethyl, -S(=O)2NH2 and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH-CH2-NH-CH2- and -O-CH2-C(=O)-NH- are linked together to form a group selected from The monocyclic or bicyclic heteroaryl group is Imidazol-4-yl, 1,2-oxazol-4-yl, 1,2-oxazol-5-yl, pyrazol-3-yl, pyrazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, pyrazinyl, pyrimidin-4-yl, pyrimidin-5-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, 1,3-benzothiazol-6-yl, pyrrolo[2,3-d]pyrimidin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl and quinolin-8-yl is selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each substituent being a fluorine or chlorine atom or Methyl, methoxy, hydroxy and morpholin-4-yl Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0128] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 2 represents a hydrogen atom or a halogen atom, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0129] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0130] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 2 represents a hydrogen atom or a fluorine atom, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0131] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 2 represents a fluorine atom, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0132] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 2 represents a chlorine atom or a fluorine atom, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0133] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 2 represents a chlorine atom, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0134] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 2 represents a hydrogen atom, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0135] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl groups C3-C8-cycloalkyl groups, C1-C6-haloalkyl group, C1-C6-hydroxyalkyl group, C2-C6-alkenyl group, C2-C6 alkynyl group, a C4-C8-cycloalkenyl group, (C1-C6-alkyl)-N(R 7 )R 8 base, -(C1-C6-alkyl)-N(H)C(=O)R 6 base, -(C1-C6-alkyl)-N(H)C(=O)OR 15 base, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) groups, which are linked to the alkyl group via a carbon atom of the heterocycloalkyl group and are optionally substituted with a C1-C3-alkyl group; and phenyl group which is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0136] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl groups C3-C8-cycloalkyl groups, C1-C6-haloalkyl group, C1-C6-hydroxyalkyl group, C2-C6-alkenyl group, C2-C6 alkynyl group, a C4-C8-cycloalkenyl group, (C1-C6-alkyl)-N(R 7 )R 8 base, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group wherein the 4- to 7-membered nitrogen-containing heterocycloalkyl group is attached to the alkyl group via a carbon atom of the heterocycloalkyl group, and optionally the 4- to 7-membered nitrogen-containing heterocycloalkyl group is substituted with a C1-C3-alkyl group, and phenyl group which is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2(C1-C6-alkyl), -N(O)2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0137] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl group, C3-C8 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, C2-C6 alkynyl group, C4-C8 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group, and phenyl group represents a group selected from the 4-7 membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3 alkyl group, the 4- to 7-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(O)OR 6 , hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), -S(=O)2, -N(O)2 and -N(R 7 )(R 8 ) Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0138] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl group, C3-C8 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, C2-C6 alkynyl group, C4-C8 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-N(H)C(=O)R 6 group, -(C1-C6-alkyl)-N(H)C(=O)OR 15 group, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group, and phenyl group represents a group selected from the 4-7 membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3 alkyl group, the 4- to 7-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0139] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl group, C3-C8 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, C2-C6 alkynyl group, C4-C8 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group, and phenyl group represents a group selected from the 4-7 membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3 alkyl group, the 4- to 7-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C4-haloalkyl, C1-C3-alkoxy and hydroxy Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0140] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl, C2-C6 alkynyl group, C4-C6 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-N(H)C(=O)R 6 group, -(C1-C6-alkyl)-N(H)C(=O)OR 15 group, -(C1-C6-alkyl)-(4- to 6-membered nitrogen-containing heterocycloalkyl) group wherein the 4-6 membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3 alkyl group; The 4-6-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group. and a phenyl group, which is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy Independently selected from groups selected from represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0141] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl, C2-C6 alkynyl group, C4-C6 cycloalkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-(4- to 6-membered nitrogen-containing heterocycloalkyl) group, and phenyl group represents a group selected from the 4-6-membered nitrogen-containing heterocycloalkyl group is optionally substituted with a C1-C3-alkyl group, the 4- to 6-membered nitrogen-containing heterocycloalkyl group is bonded to the alkyl group via a carbon atom of the heterocycloalkyl group; The phenyl group is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Alkoxy and Hydroxy Independently selected from groups selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0142] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 group, -(C1-C6-alkyl)-N(H)C(=O)OR 15 and phenyl groups represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0143] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but C1-C6 alkyl group, C3-C6 cycloalkyl group, C1-C6 haloalkyl group, C1-C6 hydroxyalkyl group, C2-C6 alkenyl group, (C1-C6 alkyl)-N(R 7 )R 8 and phenyl groups represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0144] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but Propyl, cyclohexyl, trifluoromethyl, 1-hydroxyethyl, allyl, (dimethylamino)methyl, 2-(dimethylamino)ethyl, pyrrolidin-1-yl-methyl and phenyl represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0145] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 3 but Propyl, cyclohexyl, trifluoromethyl, 1-hydroxyethyl, allyl, aminomethyl, (dimethylamino)methyl, (tert-butoxycarbonylamino)methyl, 2-(dimethylamino)ethyl, pyrrolidin-1-yl-methyl, and phenyl represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0146] In a further embodiment, the present invention provides a compound comprising R 4 and R 5 together form a 5- to 6-membered optionally unsaturated heterocyclic ring A of sub-formula (i) [ka]

[0147] (Subformula (i) may include, but is not limited to, [ka] (In the formula, X 1 , X 2 , X 3 , X 4 and X 5 -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2-; R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) a group selected from More specifically: A hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, a C1-C3 haloalkoxy group, or a cyano group. A group selected from represents More specifically, in the groups (ii) to (x), X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 represents, independently for each occurrence, a hydrogen atom, a halogen atom or a group selected from C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups, C1-C3-haloalkoxy groups and cyano groups (includes Even more particularly, there are provided compounds of formula (I) above, or tautomers, N-oxides or salts thereof, or tautomers or N-oxide salts of said compounds, which form the ring systems disclosed in the Examples.

[0148] In a further embodiment, the present invention provides a compound comprising R 4 and R 5 together form a 5- to 6-membered optionally unsaturated heterocyclic ring A of sub-formula (i) [ka]

[0149] (Subformula (i) may include, but is not limited to, [ka] (In the formula, X 1 , X 2 , X 3 , X 4 and X 5 -N(R 7)-, -O-, -S-, -S(=O)-, and -S(=O)2-; R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C6-Alkyl, C1-C6-Haloalkyl, C2-C6-Alkenyl, C2-C6-Alkynyl, Aryl, -(C1-C6-Alkyl)-Aryl, -Aryl-(C1-C6-Alkyl), C3-C8-Cycloalkyl, C1-C6-Alkoxy, -O(C2-C6-Alkenyl), C1-C6-Haloalkoxy, C3-C8-Cycloalkoxy, Aryl, -O-Aryl, Cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) a group selected from More specifically: A hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, a C1-C3 haloalkoxy group, or a cyano group. A group selected from represents More specifically, in the groups (ii) to (x), X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 represents, independently for each occurrence, a hydrogen atom, a halogen atom or a group selected from C1-C3-alkyl groups, C1-C3-haloalkyl groups, C1-C3-alkoxy groups, C1-C3-haloalkoxy groups and cyano groups (includes Even more particularly, there are provided compounds of formula (I) above which form the ring systems disclosed in the Examples, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0150] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2-X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2, X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0151] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12)2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0152] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0153] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0154] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0155] R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2 represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, and the tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0156] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7)-, -O-, -S- and -S(=O)(=NR 14 )- represents a group selected from X 1 , X 2 , X 3 and X 4 is C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0157] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -+, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0158] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O-, -S- and -S(=O)(=NR 14 )- represents a group selected from X 1 , X 2 , X 3 and X 4 is C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0159] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X3 -X 4 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O- and -S- represents a group selected from X 1 , X 2 , X 3 and X 4 One of the C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0160] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0161] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O- and -S- represents a group selected from X 1 , X 2 , X 3 and X 4 One of the C(R 12 ) represents two groups, X1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0162] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)2-S-#, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-CH(OH)-(CH2)3-#, *-CH2-CH(OH)-(CH2)2-#, *-(CH2)2-CH(OH)-CH2-#, *-(CH2)3-C(H)(OH)-#, *-CH=CH-CH(OH)-CH2-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)3-S(=O)(=NH)-#, *-(CH2)5-#, *-(CH2)3-O-CH2-#, *-(CH2)2-N(H)-(CH2)2-#, *-CH=CH-CH=CH-#, *-N=CH-CH=CH-#, and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0163] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)2-S-#, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-(CH2)3-C(H)(OH)-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)5-#, *-(CH2)3-O-CH2-#, *-(CH2)2-N(H)-(CH2)2-#, *-CH=CH-CH=CH-#, *-N=CH-CH=CH-#, and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0164] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 - and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X4 and X 5 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0165] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -# and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4and X 5 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0166] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 - and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X4 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0167] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0168] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-CH(OH)-(CH2)3-#, *-CH2-CH(OH)-(CH2)2-#, *-(CH2)2-CH(OH)-CH2-#, *-(CH2)3-C(H)(OH)-#, *-CH=CH-CH(OH)-CH2-#, *-(CH2)5-# and *-CH=CH-CH=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0169] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X2 -X 3 -X 4 -X 5 -#, and *-CH(R 13 )-X 1 -X 2 -X 3 -#, are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0170] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, and *-CH2-X1 -X 2 -X 3 -X 4 -X 5 -# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0171] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH=CH-CH(R 13 )-X 3 - and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 3 but C(R 12 )2 and CH(R 13 ) represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0172] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# group are bonded to each other to form In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0173] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0174] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7)-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0175] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, and *-CH(R 13 )-X 1 -X 2 -X 3 -# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0176] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, and *-CH2-X 1 -X 2 -X 3 -X4 -X 5 -# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0177] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH=CH-CH(R 13 )-X 3 -, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-#, and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 3 but -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0178] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-#, and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0179] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 - and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0180] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-(CH2)3-C(H)(OH)-#, *-(CH2)5-# and *-CH=CH-CH=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0181] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0182] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-(CH2)3-C(H)(OH)-#, and *-(CH2)5-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0183] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)2-S-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)3-S(=O)(=NH)-#, *-(CH2)3-O-CH2-#, *-(CH2)2-N(H)-(CH2)2-#, *-N=CH-CH=CH-# and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0184] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)2-S-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)3-O-CH2-#, *-(CH2)2-N(H)-(CH2)2-#, *-N=CH-CH=CH-# and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0185] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)2-S-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)3-S(=O)(=NH)-#, *-(CH2)3-O-CH2-#, and *-(CH2)2-N(H)-(CH2)2-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0186] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)2-S-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)3-O-CH2-#, and *-(CH2)2-N(H)-(CH2)2-#, are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0187] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-N=CH-CH=CH-# and *-CH=CH-N=CH-# are bonded to each other to form In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0188] R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 12represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0189] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5-#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0190] R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0191] R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2 represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, -(C1-C6-alkyl)-aryl, -aryl-(C1-C6-alkyl), C3-C8-cycloalkyl, C1-C6-alkoxy, -O(C2-C6-alkenyl), C1-C6-haloalkoxy, C3-C8-cycloalkoxy, aryl, -O-aryl, cyano, -C(=O)OR 6 -, hydroxy, -SH, -S-(C1-C6-alkyl), -S-(C2-C6-alkenyl), S(=O)2(C1-C6-alkyl), -S(=O)2-(C2-C6-alkenyl), -N(O)2 and -N(R 7 )(R 8 ) represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0192] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R8 ) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0193] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0194] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, or X 1 , X 2 , X3 and X 4 One of the -N(R 7 )-, -O-, -S- and -S(=O)(=NR 14 )- represents a group selected from X 1 , X 2 , X 3 and X 4 is C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 11 represents a hydrogen atom, R 12 are the same or different and represent a hydrogen atom, a halogen atom, or a C1-C3 alkyl group, R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from R 14 is a hydrogen atom or Cyano and -C(=O)CF3 groups represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0195] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 11 represents a hydrogen atom, R 12 are the same or different and represent a hydrogen atom, a halogen atom, or a C1-C3 alkyl group,

[0196] R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0197] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the -N(R 7)-, -O-, -S- and -S(=O)(=NR 14 )- represents a group selected from X 1 , X 2 , X 3 and X 4 is C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 11 represents a hydrogen atom, R 12 are the same or different and represent a hydrogen atom, a halogen atom, or a C1-C3 alkyl group, R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from R 14 is a hydrogen atom or Cyano and -C(=O)CF3 groups represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0198] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11)-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O- and -S- represents a group selected from X 1 , X 2 , X 3 and X 4 One of the C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 11 represents a hydrogen atom, R 12represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0199] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 11 represents a hydrogen atom, R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0200] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O- and -S- represents a group selected from X 1 , X 2 , X 3 and X 4 One of the C(R 12 ) represents two groups, X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 11 represents a hydrogen atom, R 12 represents independently for each occurrence a hydrogen atom, a halogen atom or a C1-C3-alkyl group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0201] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)2-S-#, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-(CH2)3-C(H)(OH)-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)5-#, *-(CH2)3-O-CH2-#, *-(CH2)2-N(H)-(CH2)2-#, *-CH=CH-CH=CH-#, *-N=CH-CH=CH-#, and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0202] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -, and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0203] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0204] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -, and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0205] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of each represents a CH2 group, R 11 represents a hydrogen atom, R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0206] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, and *-CH(R 13 )-X 1 -X 2 -X 3 -# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0207] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, and *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0208] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH=CH-CH(R 13 )-X 3 - and *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#, are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 3 but C(R 12 )2 and CH(R 13 ) represents a group selected from R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0209] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH=C(R 11 )-C(R 11 )=C(R 11 )-# group are bonded to each other to form In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0210] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X1 -X 2 -X 3 -X 4 -X 5 -#, *-CH(R 13 )-X 1 -X 2 -X 3 -#, *-CH=CH-CH(R 13 )-X 3 -#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-#, and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0211] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X3 -X 4 -X 5 -#, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0212] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X 1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -#, and *-CH(R 13 )-X 1 -X 2 -X 3 -# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0213] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH2-X1 -X 2 -#, *-CH2-X 1 -X 2 -X 3 -#, *-CH2-X 1 -X 2 -X 3 -X 4 -#, and *-CH2-X 1 -X 2 -X 3 -X 4 -X 5 -# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)- and -S(=O)2- represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 )2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of each represents a CH2 group, R 12 represents independently for each occurrence a hydrogen atom, a halogen atom, or a C1-C3-alkyl group; R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0214] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together *-CH=CH-CH(R 13 )-X 3 -, *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-#, and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 3 but -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O)2- represents a group selected from R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0215] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)2-S-#, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, *-(CH2)3-N(CH3)-#, *-(CH2)3-S-#, *-(CH2)3-S(=O)(=NH)-#, *-(CH2)5-#, *-(CH2)3-O-CH2-#, *-(CH2)2-N(H)-(CH2)2-#, *-N=CH-CH=CH-# and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0216] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)4-#, *-CH2-C(H)(C(=O)OH)-(CH2)2-#, *-CH2-CF2-(CH2)2-#, *-(CH2)3-C(H)(C(=O)OH)-#, *-CH(OH)-(CH2)3-#, *-CH2-CH(OH)-(CH2)2-#, *-(CH2)2-CH(OH)-CH2-#, *-(CH2)3-C(H)(OH)-#, *-CH=CH-CH(OH)-CH2-#, *-(CH2)5-#, and *-CH=CH-CH=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0217] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-CH2-C(CH3)2-CH2-O-#, *-(CH2)2-O-CH2-#, *-(CH2)3-O-#, and *-(CH2)3-O-CH2-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0218] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH2)3-N(CH3)-#, *-(CH2)3-S(=O)(=NH)-#, *-(CH2)2-N(H)-(CH2)2-#, *-N=CH-CH=CH-#, and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In a further embodiment, the present invention provides a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound. R 4 and R 5 But together *-N=C(R 11 )-C(R 11 )=C(R 11 )-#, *-CH=NC(R 11 )=C(R 11 )-#, *-CH=C(R 11 )-N=C(R 11 )-#, and *-CH=C(R 11 )-C(R 11)=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0219] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 6 is a hydrogen atom or C1-C6 alkyl groups and benzyl groups represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0220] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 6 is a hydrogen atom or C1-C4 alkyl groups and benzyl groups represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0221] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C6-alkyl groups, C2-C6-hydroxyalkyl groups and -(C2-C6-alkyl)-N(R9 )(R 10 ) group represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally C1-C3-alkyl, -S(=O)2(C1-C3-alkyl) and -C(=O)O(C1-C4-alkyl) substituted with a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0222] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C6-alkyl groups, C2-C6-hydroxyalkyl groups and -(C2-C6-alkyl)-N(R 9 )(R 10 ) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0223] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally C1-C3-alkyl, -S(=O)2(C1-C3-alkyl) and -C(=O)O(C1-C4-alkyl) substituted with a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0224] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C3-alkyl groups, C2-C3-hydroxyalkyl groups and -(C2-C3-alkyl)-N(R 9 )(R 10 ) represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; The 4- to 6-membered nitrogen-containing heterocycloalkyl group may optionally C1-C3-alkyl, -S(=O)2(C1-C3-alkyl) and -C(=O)O(C1-C4-alkyl) substituted with a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0225] R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C1-C3-alkyl groups, C2-C3-hydroxyalkyl groups and -(C2-C3-alkyl)-N(R 9 )(R 10 ) represents a group selected from and the tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0226] R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; The 4- to 6-membered nitrogen-containing heterocycloalkyl group may optionally C1-C3-alkyl, -S(=O)2(C1-C3-alkyl) and -C(=O)O(C1-C4-alkyl) substituted with a group selected from and the tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0227] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 7 and R 8 represents, independently for each occurrence, a hydrogen atom or a C1-C3-alkyl group; or R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0228] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 7 and R 8 represents, independently for each occurrence, a hydrogen atom or a C1-C3-alkyl group; Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0229] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 7 and R 8 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0230] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 9and R 10 represents, independently for each occurrence, a hydrogen atom or a C1-C3-alkyl group; or R 9 and R 10 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0231] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 9 and R 10 represents, independently for each occurrence, a hydrogen atom or a C1-C3-alkyl group; Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0232] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 9 and R 10 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0233] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 9 and R 10 represents, independently for each occurrence, a hydrogen atom or a C1-C3-alkyl group; or R 9 and R 10 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0234] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 9 and R 10 together with the nitrogen to which they are attached, represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0235] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C1-C3 alkyl groups, C1-C3 haloalkyl groups, C1-C3 alkoxy groups, C1-C3 haloalkoxy groups, and cyano groups represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0236] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 11 represents a hydrogen atom, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0237] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 12 represents independently for each occurrence a hydrogen atom, a halogen atom or a C1-C3-alkyl group, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0238] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0239] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0240] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 14 is a hydrogen atom or Cyano group and -C(=O)(C1-C3-haloalkyl) group represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0241] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 14 is a hydrogen atom or Cyano and -C(=O)CF3 groups represents a group selected from Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0242] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 14 represents a hydrogen atom, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0243] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 14 represents a group selected from the group consisting of a cyano group and a -C(=O)CF3 group, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0244] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 15 represents a group selected from C1-C6 alkyl groups and benzyl groups, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0245] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 15 represents a group selected from C1-C4 alkyl groups and benzyl groups, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0246] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 15 represents a C1-C4 alkyl group; Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0247] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being a halogen atom, a phenyl group and an -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom. C2-C6-hydroxyalkyl groups, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group, said 4- to 6-membered heterocycloalkyl group being attached to the remainder of the molecule through a carbon atom of said 4- to 6-membered heterocycloalkyl group, said 4- to 6-membered heterocycloalkyl group being optionally substituted once or twice, and each substituent being C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) Independently selected from groups selected from a phenyl group, which is optionally substituted one, two, three or four times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Hydroxyalkyl, C1-C3-Alkoxy, Hydroxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ) and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R 7 )-CH2- and -O-CH2-C(=O)-NH- are bonded to each other to form a group selected from an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups which is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0248] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being a halogen atom, a phenyl group and an -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom. C2-C6-hydroxyalkyl groups, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group, which is attached to the remainder of the molecule through a carbon atom of the 4- to 6-membered heterocycloalkyl group and is optionally substituted once or twice, and each substituent is independently selected from the group consisting of C1-C3-alkyl, 5- to 6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O); a phenyl group, which is optionally substituted one, two, three or four times, each substituent being a halogen atom or C1-C3-Alkyl, C1-C3-Haloalkyl, C1-C3-Hydroxyalkyl, C1-C3-Alkoxy, Hydroxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ) and SF5 Independently selected from groups selected from or when two substituents on said phenyl group are attached to adjacent ring atoms, they may optionally be taken together as: -CH2-N(R 7 )-CH2- and -O-CH2-C(=O)-NH- are bonded to each other to form a group selected from an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups which is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 2 represents a hydrogen atom or a fluorine atom, Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, and salts of the tautomers or N-oxides.

[0249] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl groups, which are optionally substituted once or twice, each of which is a halogen atom or a phenyl group and -N(R7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom. C2-C6-hydroxyalkyl groups, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group, said 4- to 6-membered heterocycloalkyl group being attached to the remainder of the molecule through a carbon atom of said 4- to 6-membered heterocycloalkyl group, and optionally substituted once or twice, wherein each substituent is C1-C3-alkyl, 5-6-membered heteroaryl, -C(=O)O(C1-C4-alkyl), -C(=O)(C1-C3-alkyl), -C(=O)(C3-C6-cycloalkyl), -S(=O)2(C1-C3-alkyl) and oxo(=O) Independently selected from groups selected from a phenyl group, which is optionally substituted one, two, three or four times, each substituent being a halogen atom or a C1-C3-alkyl, C1-C3-haloalkyl, C1-C3-hydroxyalkyl, C1-C3-alkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C1-C3-alkyl)-N(R 7 )(R 8 ), -S(=O)2N(R 7 )(R 8 ) and SF5, Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together form -CH2-N(R 7 )—CH— and —O—CH—C(═O)—NH—), an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups which is optionally substituted one, two or three times, each substituent being a halogen atom or C1-C3-alkyl, C1-C3-alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from

[0250] R 2 represents a chlorine atom or a fluorine atom, Provided is a compound of formula (I) above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound.

[0251] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C3-C6-cycloalkyl group, C2-C6-hydroxyalkyl group, -(C2-C6-alkyl)-N(R 7 )(R 8 ) group, 4- to 6-membered heterocycloalkyl group, phenyl group, indanyl group, and monocyclic or bicyclic heteroa...

Claims

1. A pharmaceutical composition for use in combination with a chemotherapeutic agent and / or anticancer agent and / or radiation therapy, comprising a compound of general formula (I), 【Chemical 1】 (In the formula, R 1 teeth C 1 ~C 8 -alkyl group (which may optionally be C 3 ~C ８ -cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents may optionally be substituted one, two or three times with a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -haloalkyl group, C 1 ~C 3 -substituted with one or more substituents independently selected from alkoxy and hydroxy groups; C 2 ~C 8 -haloalkyl group, C 3 ~C 8 -cycloalkyl groups, which are optionally substituted one or two times, each substituent being a halogen atom, a hydroxy group, a phenyl group, and -N(R 7 )(R 8 ) groups, The phenyl substituents are optionally substituted one, two or three times, each of which may be a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -haloalkyl group, C 1 ~C 3 -independently selected from alkoxy and hydroxy groups), C 2 ~C 6 -cyanoalkyl groups, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- group -(C 2 ~C 6 -alkyl)-N(R 7 )(R 8 ) group, -(C 1 ~C 6 -alkyl)-C(=O)N(R 7 )(R 8 ) group, A 4- to 7-membered, optionally unsaturated heterocyclic group which is attached to the rest of the molecule through a carbon atom and is optionally substituted once or twice, and each substituent is C 1 ~C 3 -Alkyl group, 5- to 6-membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C 1 ~C 6 -alkyl) group, -C(=O)(C 3 ~C 6 -cycloalkyl) group, -S(=O) 2 (C 1 ~C 6 -alkyl) group and oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2 or 3 times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 4 -haloalkyl, C 1 ~C 3 -alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C 1 ~C 6 -Alkyl, C 3 ~C 8 -cycloalkyl, C 1 ~C 6 -haloalkyl, C 1 ~C 6 -hydroxyalkyl, C 2 ~C 6 -Alkenyl, C 2 ~C 6 -alkynyl, aryl, -(C 1 ~C 6 -alkyl)-aryl, -aryl-(C 1 ~C 6 -alkyl), C 1 ~C 6 -alkoxy, -O(C 2 ~C 6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, hydroxy, -O-aryl, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C 1 ~C 6 -alkyl)-N(R 7 )(R 8 ), -(C 1 ~C 6 -alkyl)-C(=O)OR 6 , -(C 1 ~C 6 -alkyl)-C(=O)N(R 7 )(R 8 ), -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), -S(=O) 2 N(R 7 )(R 8 ), -S(=O) 2 (C 1 ~C 6 -alkyl), -S(=O) 2 -O-(C 2 ~C 6 -alkenyl), -S(=O)(=NR 14 )(C 1 ~C 3 -alkyl), -N(O) 2 , -P(=O)(C 1 ~C 3 -alkyl) 2 and S.F. 5 Independently selected from groups selected from Alternatively, two adjacent substituents of the phenyl group may be taken together to optionally form -N=, -NH-, -N(R 7 )-, -O-, -S-, and optionally forming a 5- or 6-membered, optionally heterocyclic, aromatic or non-aromatic ring containing a C(=O) group, the ring thus formed being optionally substituted once or twice, and each substituent being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -haloalkyl, C 2 ~C 6 -Alkenyl, C 2 ~C 6 -alkynyl, aryl, -(C 1 ~C 6 -alkyl)-aryl, -aryl-(C 1 ~C 6 -alkyl), C 3 ~C 8 -cycloalkyl, C 1 ~C 6 -alkoxy, -O(C 2 ~C 6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -cycloalkoxy, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), -S(=O) 2 (C 1 ~C 6 -alkyl), -N(O) 2 and -N(R 7 )(R 8 ) (independently selected from groups selected from) and monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of which is a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -haloalkyl, C 2 ~C 6 -Alkenyl, C 2 ~C 6 -alkynyl, -(C 1 ~C 6 -alkyl)-aryl, -aryl-(C 1 ~C 6 -alkyl), C 3 ~C 8 -cycloalkyl, C 1 ~C 6 -alkoxy, -O(C 2 ~C 6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), -S(=O) 2 (C 1 ~C 6 -alkyl), -N(O) 2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 2 represents a hydrogen atom or a halogen atom, R 3 teeth C 1 ~C 6 -alkyl group C 3 ~C 8 -cycloalkyl group, C 1 ~C 6 -haloalkyl group, C 1 ~C 6 -hydroxyalkyl group, C 2 ~C 6 -alkenyl group, C 2 ~C 6 -alkynyl group, C 4 ~C 8 -cycloalkenyl group, (C 1 ~C 6 -alkyl)-N(R 7 )R 8 base, -(C 1 ~C 6 -alkyl)-N(H)C(=O)R 6 base, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 base, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group wherein the 4- to 7-membered nitrogen-containing heterocycloalkyl group is attached to the alkyl group via a carbon atom of the heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally C 1 ~C 3 -substituted with alkyl groups), and phenyl group which is optionally substituted one, two or three times, each substituent being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -haloalkyl, C 2 ~C 6 -Alkenyl, C 2 ~C 6 -alkynyl, aryl, -(C 1 ~C 6 -alkyl)-aryl, -aryl-(C 1 ~C 6 -alkyl), C 3 ~C 8 -cycloalkyl, C 1 ~C 6 -alkoxy, -O(C 2 ~C 6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, -O-aryl, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), -S(=O) 2 (C 1 ~C 6 -alkyl), -N(O) 2 and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 4 and R 5 together form the 5- to 8-membered optionally unsaturated heterocyclic ring A of sub-formula (i) 【Chemistry 2】 (wherein ring A is a ring that can be any of -O-, -S-, -S(=O) ... 2 -, -S(=O)(=NR 14 )-, -N=, -N(R 7 )-, -C(=O)-, -CH=, -CR 11 =, -C(R 12 ) 2 -, -C(H)(R 13 )-) Forming R 6 is a hydrogen atom or C 1 ~C 6 Alkyl and benzyl groups represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C 1 ~C 6 -Alkyl group, C 2 ~C 6 -alkenyl group, C 2 ~C 6 -hydroxyalkyl groups, haloalkyl groups, aryl groups, (C 1 ~C 6 -alkyl)-aryl groups and -(C 2 ~C 6 -alkyl)-N(R 9 )(R 10 ) group represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally C 1 ~C 6 -Alkyl, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), -S(=O) 2 (C 1 ~C 3 -alkyl), -S(=O) 2 -(C 2 ~C 6 -alkenyl) and -C(=O)OR 6 and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C 1 ~C 3 -alkyl group Represents, or R 9 and R 10 together with the nitrogen to which they are attached, Nitrogen-containing 4- to 7-membered heterocycloalkyl groups represents R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C 1 ~C 6 -Alkyl, C 1 ~C 6 -haloalkyl, C 2 ~C 6 -Alkenyl, C 2 ~C 6 -alkynyl, aryl, -(C 1 ~C 6 -alkyl)-aryl, -aryl-(C 1 ~C 6 -alkyl), C 3 ~C 8 -cycloalkyl, C 1 ~C 6 -alkoxy, -O(C 2 ~C 6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, -O-aryl, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), S(=O) 2 (C 1 ~C 6 -alkyl), -S(=O) 2 -(C 2 ~C 6 -alkenyl), -N(O) 2 and -N(R 7 )(R 8 ) represents a group selected from R 12 is independently for each occurrence a hydrogen atom, a halogen atom or C 1 ~C 3 represents an alkyl group, R 13 teeth C 1 ~C 6 -Alkyl, C 1 ~C 6 -haloalkyl, C 2 ~C 6 -Alkenyl, C 2 ~C 6 -alkynyl, aryl, -(C 1 ~C 6 -alkyl)-aryl, -aryl-(C 1 ~C 6 -alkyl), C 3 ~C 8 -cycloalkyl, C 1 ~C 6 -alkoxy, -O(C 2 ~C 6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, -O-aryl, cyano, -C(=O)OR 6 , hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), S(=O) 2 (C 1 ~C 6 -alkyl), -S(=O) 2 -(C 2 ~C 6 -alkenyl), -N(O) 2 and -N(R 7 )(R 8 ) represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C 1 ~C 3 -haloalkyl) group represents a group selected from R 15 teeth C 1 ~C 6 -Alkyl and benzyl groups represents a group selected from or a tautomer, or salt thereof, or a salt of a tautomer of said compound.

2. R 1 but C 1 ~C 8 -alkyl group (which may optionally be C 3 ~C 8 -cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 4 -haloalkyl, C 1 ~C 3 -alkoxy and hydroxy Independently selected from groups selected from C 2 ~C 8 -haloalkyl group, C 3 ~C 8 -cycloalkyl groups, which are optionally substituted one or two times, each substituent being a halogen atom, a hydroxy group, a phenyl group, and -N(R 7 )(R 8 ) groups, The phenyl substituents are optionally substituted one, two or three times, each of which may be a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -haloalkyl group, C 1 ~C 3 -independently selected from alkoxy and hydroxy groups), C 2 ~C 6 -cyanoalkyl groups, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- group -(C 2 ~C 6 -alkyl)-N(R 7 )(R 8 ) group, -(C 1 ~C 6 -alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4- to 7-membered heterocycloalkyl group which is attached to the remainder of the molecule through a carbon atom of said 4- to 7-membered heterocycloalkyl group and is optionally substituted one or two times, and each substituent is C 1 ~C 3 -Alkyl group, 5- to 6-membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C 1 ~C 6 -alkyl) group, -C(=O)(C 3 ~C 6 -cycloalkyl) group, -S(=O) 2 (C 1 ~C 6 -alkyl) group and oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2 or 3 times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 4 -haloalkyl, C 1 ~C 3 -alkoxy and hydroxy Independently selected from groups selected from a 5- to 7-membered heterocycloalkenyl group which is attached to the rest of the molecule through a carbon atom of said 5- to 7-membered heterocycloalkenyl group and is optionally substituted one or two times, and each substituent is C 1 ~C 3 -Alkyl group, 5- to 6-membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C 1 ~C 6 -alkyl) group, -C(=O)(C 3 ~C 6 -cycloalkyl) group, -S(=O) 2 (C 1 ~C 6 -alkyl) group and oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2 or 3 times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 4 -haloalkyl, C 1 ~C 3 -alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C 1 ~C 6 -Alkyl, C 3 ~C 8 -cycloalkyl, C 1 ~C 6 -haloalkyl, C 1 ~C 6 -hydroxyalkyl, C 1 ~C 6 -alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C 1 ~C 6 -alkyl)-N(R 7 )(R 8 ), -(C 1 ~C 6 -alkyl)-C(=O)OR 6 , -(C 1 ~C 6 -alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O) 2 N(R 7 )(R 8 ), -S(=O) 2 (C 1 ~C 3 -alkyl), -S(=O)(=NR 14 )(C 1 ~C 3 -alkyl), -P(=O)(C 1 ~C 3 -alkyl) 2 and S.F. 5 Independently selected from groups selected from Alternatively, two substituents on said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH 2 -N(R 7 )-CH 2 -、-CH 2 -O-CH 2 -、-O-CH 2 -C(=O)-NH-および-NH-C(=O)-NH- are bonded to each other to form a group selected from an indanyl group, a tetralinyl group (said indanyl or tetralinyl group being optionally substituted once or twice, each substituent being a halogen atom, C 1 ~C 6 -Alkyl group, C 1 ~C 6 -haloalkyl group, C 3 ~C 8 -cycloalkyl group, C 1 ~C 6 -alkoxy group, C 1 ~C 6 -haloalkoxy group, C 3 ~C 8 -cycloalkoxy group, cyano group, hydroxy group and -N(R 7 )(R 8 ) groups) and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of which may be a halogen atom, C 1 ~C 6 -Alkyl group, C 1 ~C 6 -haloalkyl group, C 3 ~C 8 -cycloalkyl group, C 1 ~C 6 -alkoxy group, C 1 ~C 6 -haloalkoxy group, C 3 ~C 8 -cycloalkoxy group, cyano group, hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but C 1 ~C 6 -Alkyl group, C 3 ~C 8 -cycloalkyl group, C 1 ~C 6 -haloalkyl group, C 1 ~C 6 -hydroxyalkyl group, C 2 ~C 6 -alkenyl group, C 2 ~C 6 -alkynyl group, C 4 ~C 8 -cycloalkenyl group, (C 1 ~C 6 -alkyl)-N(R 7 )R 8 Group, -(C 1 ~C 6 -alkyl)-N(H)C(=O)R 6 Group, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 Group, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group wherein the 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally C 1 ~C 3 -substituted with an alkyl group, the 4- to 7-membered nitrogen-containing heterocycloalkyl group is attached to the alkyl group through a carbon atom of the heterocycloalkyl group; and a phenyl group, said phenyl group being optionally substituted one, two or three times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 4 -haloalkyl, C 1 ~C 3 -alkoxy and hydroxy Independently selected from groups selected from represents a group selected from R 4 and R 5 But together *-CH 2 -X 1 -X 2 -#、 *-CH 2 -X 1 -X 2 -X 3 -#、 *-CH 2 -X 1 -X 2 -X 3 -X 4 -#、 *-CH 2 -X 1 -X 2 -X 3 -X 4 -X 5 -#、 *-CH(R 13 )-X 1 -X 2 -X 3 -#、 *-CH=CH-CH(R 13 )-X 3 -#、 *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#、 *-N=C(R 11 )-C(R 11 )=C(R 11 )-#、 *-CH=N-C(R 11 )=C(R 11 )-#、 *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 ) 2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of the 2 Representing a group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O) 2 - represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 ) 2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of the 2 represents a group, R 6 is a hydrogen atom or C 1 ~C 6 Alkyl and benzyl groups represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C 1 ~C 6 -Alkyl group, C 2 ~C 6 -hydroxyalkyl groups and -(C 2 ~C 6 -alkyl)-N(R 9 )(R 10 ) group represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached represent a nitrogen-containing 4- to 7-membered heterocycloalkyl group; said 4- to 7-membered nitrogen-containing heterocycloalkyl group optionally C 1 ~C 3 -Alkyl, -S(=O) 2 (C 1 ~C 3 -alkyl) and -C(=O)O(C 1 ~C 4 -alkyl) and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C 1 ~C 3 -alkyl group Represents, or R 9 and R 10 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 7-membered heterocycloalkyl groups represents R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C 1 ~C 3 -Alkyl group, C 1 ~C 3 -haloalkyl group, C 1 ~C 3 -alkoxy group, C 1 ~C 3 -Haloalkoxy and cyano groups represents a group selected from R 12 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C 1 ~C 3 -haloalkyl) group represents a group selected from R 15 but C 1 ~C 6 -Alkyl and benzyl groups represents a group selected from or a tautomer, or salt thereof, or a salt of a tautomer of said compound.

3. R 1 but C 1 ~C 6 -alkyl group (which may optionally be C 3 ~C 6 -cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from The phenyl substituents are optionally substituted one, two or three times, each of which may be a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -haloalkyl group, C 1 ~C 3 -independently selected from alkoxy and hydroxy groups C 2 ~C 6 -haloalkyl group, C 3 ~C 6 -cycloalkyl groups, which are optionally substituted one or two times, each substituent being a halogen atom, a hydroxy group, a phenyl group, and -N(R 7 )(R 8 ) groups, The phenyl substituents are optionally substituted one, two or three times, each of which may be a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -haloalkyl group, C 1 ~C 3 -independently selected from alkoxy and hydroxy groups), C 2 ~C 6 -cyanoalkyl groups, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 3 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- group -(C 2 ~C 6 -alkyl)-N(R 7 )(R 8 ) group, -(C 1 ~C 6 -alkyl)-C(=O)N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group which is attached to the rest of the molecule through a carbon atom of said 4- to 6-membered heterocycloalkyl group and is optionally substituted one or two times, and each substituent is C 1 ~C 3 -Alkyl group, 5- to 6-membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C 1 ~C 3 -alkyl) group, -C(=O)(C 3 ~C 6 -cycloalkyl) group, -S(=O) 2 (C 1 ~C 3 -alkyl) group and oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2 or 3 times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -haloalkyl, C 1 ~C 3 -alkoxy and hydroxy Independently selected from groups selected from a 5- to 6-membered heterocycloalkenyl group which is attached to the rest of the molecule through a carbon atom of said 5- to 6-membered heterocycloalkenyl group and is optionally substituted one or two times, and each substituent is C 1 ~C 3 -Alkyl group, 5- to 6-membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C 1 ~C 3 -alkyl) group, -C(=O)(C 3 ~C 6 -cycloalkyl) group, -S(=O) 2 (C 1 ~C 3 -alkyl) group and oxo (=O) group; The 5- to 6-membered heteroaryl substituent is optionally substituted 1, 2 or 3 times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -haloalkyl, C 1 ~C 3 -alkoxy and hydroxy Independently selected from groups selected from a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 3 ~C 6 -cycloalkyl, C 1 ~C 3 -haloalkyl, C 1 ~C 3 -hydroxyalkyl, C 1 ~C 3 -alkoxy, C 1 ~C 3 -Haloalkoxy, C 3 ~C 6 -Cycloalkoxy, hydroxy, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C 1 ~C 3 -alkyl)-N(R 7 )(R 8 ), -(C 1 ~C 3 -alkyl)-C(=O)OR 6 , -(C 1 ~C 3 -alkyl)-C(=O)N(R 7 )(R 8 ), -S(=O) 2 N(R 7 )(R 8 ), -S(=O) 2 (C 1 ~C 3 -alkyl), -S(=O)(=NR 14 )(C 1 ~C 3 -alkyl), -P(=O)(C 1 ~C 3 -alkyl) 2 and S.F. 5 Independently selected from groups selected from Alternatively, two substituents on said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH 2 -N(R 7 )-CH 2 -、-CH 2 -O-CH 2 -、-O-CH 2 -C(=O)-NH-および-NH-C(=O)-NH- are bonded to each other to form a group selected from indanyl group, tetralinyl group (which is optionally substituted one or two times, each substituent being a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -haloalkyl group, C 3 ~C 6 -cycloalkyl group, C 1 ~C 3 -alkoxy group, C 1 ~C 3 -haloalkoxy group, C 3 ~C 6 -cycloalkoxy group, cyano group, hydroxy group and -N(R 7 )(R 8 ) groups) and Monocyclic or bicyclic heteroaryl groups (which is optionally substituted one, two or three times, each substituent being a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -haloalkyl group, C 3 ~C 6 -cycloalkyl group, C 1 ~C 3 -alkoxy group, C 1 ~C 3 -haloalkoxy group, C 3 ~C 6 -cycloalkoxy group, cyano group, hydroxy group and -N(R 7 )(R 8 ) groups) represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but C 1 ~C 6 -Alkyl group, C 3 ~C 6 -cycloalkyl, C 1 ~C 6 -haloalkyl group, C 1 ~C 6 -hydroxyalkyl group, C 2 ~C 6 -Alkenyl, C 2 ~C 6 -alkynyl group, C 4 ~C 6 -cycloalkenyl group, (C 1 ~C 6 -alkyl)-N(R 7 )R 8 Group, -(C 1 ~C 6 -alkyl)-N(H)C(=O)R 6 Group, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 Group, -(C 1 ~C 6 -alkyl)-(4- to 6-membered nitrogen-containing heterocycloalkyl) group wherein the 4- to 6-membered nitrogen-containing heterocycloalkyl group is optionally C 1 ~C 3 -substituted with an alkyl group, the 4-6 membered nitrogen-containing heterocycloalkyl group is attached to the alkyl group via a carbon atom of the heterocycloalkyl group; and a phenyl group, said phenyl group being optionally substituted one, two or three times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -haloalkyl, C 1 ~C 3 -alkoxy and hydroxy Independently selected from groups selected from represents a group selected from R 4 and R 5 But together *-CH 2 -X 1 -X 2 -#、 *-CH 2 -X 1 -X 2 -X 3 -#、 *-CH 2 -X 1 -X 2 -X 3 -X 4 -#、 *-CH 2 -X 1 -X 2 -X 3 -X 4 -X 5 -#、 *-CH(R 13 )-X 1 -X 2 -X 3 -#、 *-CH=CH-CH(R 13 )-X 3 -#、 *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#、 *-N=C(R 11 )-C(R 11 )=C(R 11 )-#、 *-CH=N-C(R 11 )=C(R 11 )-#、 *-CH=C(R 11 )-N=C(R 11 )-# and *-CH=C(R 11 )-C(R 11 )=N-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 ) 2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of the 2 Representing a group, or X 1 , X 2 , X 3 , X 4 and X 5 One of the -N(R 7 )-, -O-, -S-, -S(=O)-, -S(=O)(=NR 14 )- and -S(=O) 2 - represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R 12 ) 2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remainder of the 2 represents a group, R 6 is a hydrogen atom or C 1 ~C 4 -Alkyl and benzyl groups represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C 1 ~C 3 -Alkyl group, C 2 ~C 3 -hydroxyalkyl groups and -(C 2 ~C 3 -alkyl)-N(R 9 )(R 10 ) represents a group selected from or R 7 and R 8 together with the nitrogen to which they are attached represent a nitrogen-containing 4- to 6-membered heterocycloalkyl group; said 4- to 6-membered nitrogen-containing heterocycloalkyl group optionally C 1 ~C 3 -Alkyl, -S(=O) 2 (C 1 ~C 3 -alkyl) and -C(=O)O(C 1 ~C 4 -alkyl) and is substituted with a group selected from R 9 and R 10 is, independently for each occurrence, a hydrogen atom or C 1 ~C 3 -alkyl group Represents, or R 9 and R 10 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C 1 ~C 3 -Alkyl group, C 1 ~C 3 -haloalkyl group, C 1 ~C 3 -alkoxy group, C 1 ~C 3 -Haloalkoxy and cyano groups represents a group selected from R 12 is, independently for each occurrence, a hydrogen atom, a halogen atom, or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy group, -C(=O)OR 6 group and -C(=O)N(R 7 )(R 8 ) group represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)(C 1 ~C 3 -haloalkyl) group represents a group selected from R 15 but C 1 ~C 4 -Alkyl and benzyl groups represents a group selected from or a tautomer, or salt thereof, or a salt of a tautomer of said compound.

4. R 1 but C 3 ~C 6 -cycloalkyl groups, which are optionally substituted one or two times, each of which is selected from the group consisting of halogen atoms, phenyl groups, and -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom; C 2 ~C 6 -hydroxyalkyl group, -(C 2 ~C 6 -alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group which is attached to the rest of the molecule through a carbon atom of said 4- to 6-membered heterocycloalkyl group and is optionally substituted one or two times, and each substituent is C 1 ~C 3 -Alkyl group, 5- to 6-membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C 1 ~C 3 -alkyl) group, -C(=O)(C 3 ~C 6 -cycloalkyl) group, -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) groups; a phenyl group, which is optionally substituted one, two, three or four times, each of the substituents being a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -haloalkyl group, C 1 ~C 3 -hydroxyalkyl group, C 1 ~C 3 -Alkoxy group, cyano group, hydroxy group, -C(=O)OR 6 group, -C(=O)N(R 7 )(R 8 ) group, -N(R 7 )(R 8 ) group, -(C 1 ~C 3 -alkyl)-N(R 7 )(R 8 ) group, -S(=O) 2 N(R 7 )(R 8 ) group and SF 5 are independently selected from Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, may optionally be taken together to form -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -C(=O)-NH- an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups (which is optionally substituted one, two or three times, each substituent being a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -alkoxy groups, hydroxy groups and -N(R 7 )(R 8 ) groups) represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but C 1 ~C 6 -Alkyl group, C 3 ~C 6 -cycloalkyl group, C 1 ~C 6 -haloalkyl group, C 1 ~C 6 -hydroxyalkyl group, C 2 ~C 6 -alkenyl group, (C 1 ~C 6 -alkyl)-N(R 7 )R 8 Group, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 and phenyl groups represents a group selected from R 4 and R 5 But together *-CH 2 -X 1 -X 2 -#、 *-CH 2 -X 1 -X 2 -X 3 -#、 *-CH 2 -X 1 -X 2 -X 3 -X 4 -#、 *-CH(R 13 )-X 1 -X 2 -X 3 -#、 *-CH=CH-CH(R 13 )-X 3 -#、 *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#、 *-N=C(R 11 )-C(R 11 )=C(R 11 )-#、 and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 ) 2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of the 2 Representing a group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O-, -S- and -S(=O)(=NR 14 )- represents a group selected from X 1 , X 2 , X 3 and X 4 One of the C(R 12 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remainder of the 2 represents a group, R 6 is a hydrogen atom or C 1 ~C 4- Alkyl and benzyl groups represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C 1 ~C 3 -alkyl group Represents, or R 7 and R 8 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 represents a hydrogen atom, R 12 may be the same or different, and may be a hydrogen atom, a halogen atom, or a C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from R 14 is a hydrogen atom or Cyano group and -C(=O)CF 3 base represents a group selected from R 15 C 1 ~C 4 represents an alkyl group, or a tautomer, or salt thereof, or a salt of a tautomer of said compound.

5. R 1 but C 3 ~C 6 - a cycloalkyl group selected from cyclopropyl and cyclohexyl, optionally substituted once or twice, each substituent being a halogen atom, a phenyl group, and -N(R 7 )(R 8 ) groups, wherein said phenyl substituents are optionally substituted one, two or three times, each substituent being independently selected from a halogen atom; C 2 ~C 6 -hydroxyalkyl group, -(C 2 ~C 6 -alkyl)-N(R 7 )(R 8 ) group, a 4- to 6-membered heterocycloalkyl group which is attached to the remainder of the molecule through a carbon atom of said 4- to 6-membered heterocycloalkyl group and is selected from azetidinyl, oxetanyl, tetrahydro-2H-pyranyl, tetrahydro-2H-thiopyranyl, and piperidinyl, and which is optionally substituted once or twice, and each substituent is C 1 ~C 3 -Alkyl group, 5- to 6-membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C 1 ~C 3 -alkyl) group, -C(=O)(C 3 ~C 6 -cycloalkyl) group, -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) groups; a phenyl group, which is optionally substituted one, two or three times, each of the substituents being a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -haloalkyl group, C 1 ~C 3 -hydroxyalkyl group, C 1 ~C 3 -Alkoxy group, hydroxy group, cyano group, -C(=O)OR 6 group, -C(=O)N(R 7 )(R 8 ) group, -N(R 7 )(R 8 ) group, -(C 1 ~C 3 -alkyl)-N(R 7 )(R 8 ) group, -S(=O) 2 N(R 7 )(R 8 ) group and SF 5 are independently selected from Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, may optionally be taken together to form -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -C(=O)-NH- an indanyl group, which is optionally substituted with a hydroxy group; and Monocyclic or bicyclic heteroaryl groups selected from imidazolyl, 1,2-oxazolyl, pyrazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, 1,3-benzothiazolyl, pyrrolo[2,3-d]pyrimidinyl and quinolinyl; optionally substituted one, two or three times, each substituent being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -alkoxy, hydroxyl groups and -N(R 7 )(R 8 ) Independently selected from groups selected from represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but C 1 ~C 6 -Alkyl group, C 3 ~C 6 -cycloalkyl group, C 1 ~C 6 -haloalkyl group, C 1 ~C 6 -hydroxyalkyl group, C 2 ~C 6 -alkenyl group, (C 1 ~C 6 -alkyl)-N(R 7 )R 8 Group, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 and phenyl groups represents a group selected from R 4 and R 5 But together *-CH 2 -X 1 -X 2 -#、 *-CH 2 -X 1 -X 2 -X 3 -#、 *-CH 2 -X 1 -X 2 -X 3 -X 4 -#、 *-CH(R 13 )-X 1 -X 2 -X 3 -#、 *-CH=CH-CH(R 13 )-X 3 -#、 *-CH=C(R 11 )-C(R 11 )=C(R 11 )-#、 *-N=C(R 11 )-C(R 11 )=C(R 11 )-#、 and *-CH=C(R 11 )-N=C(R 11 )-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, In the group, X 1 , X 2 , X 3 and X 4 One of the C(R 12 ) 2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remainder of the 2 Representing a group, or X 1 , X 2 , X 3 and X 4 One of the -N(R 7 )-, -O-, -S- and -S(=O)(=NH)- represents a group selected from X 1 , X 2 , X 3 and X 4 One of the C(R 12 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remainder of the 2 represents a group, R 6 is a hydrogen atom or C 1 ~C 4- Alkyl and benzyl groups represents a group selected from R 7 and R 8 is, independently for each occurrence, a hydrogen atom or C 1 ~C 3 -alkyl group Represents, or R 7 and R 8 But together with the nitrogen to which they are bound, Nitrogen-containing 4- to 6-membered heterocycloalkyl groups represents R 11 represents a hydrogen atom, R 12 may be the same or different, and may be a hydrogen atom, a halogen atom, or a C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy group and -C(=O)OR 6 base represents a group selected from R 15 C 1 ~C 4 represents an alkyl group, or a tautomer, or salt thereof, or a salt of a tautomer of said compound.

6. R 1 but C 3 ~C 6 a cycloalkyl group selected from the group consisting of cyclopropyl and cyclohexyl groups, The C 3 ~C 6 -cycloalkyl group is optionally substituted once or twice, each substituent being independently selected from a fluorine atom, a phenyl group, and a dimethylamino group; wherein the phenyl substituent is optionally substituted with a fluorine atom; 2-hydroxy-2-methylpropyl group, 2-(dimethylamino)ethyl group, a 4- to 6-membered heterocycloalkyl group selected from azetidin-3-yl, oxetan-3-yl, tetrahydro-2H-pyran-4-yl, tetrahydro-2H-thiopyran-4-yl and piperidin-4-yl; optionally substituted once or twice, each substituent independently selected from the group consisting of methyl, ethyl, pyrazinyl, tert-butoxycarbonyl, acetyl, 1-cyclopropanecarbonyl, methylsulfonyl, and oxo (=O); a phenyl group, which is optionally substituted one, two or three times, and each substituent is a fluorine atom, a chlorine atom, a methyl group, an ethyl group, a difluoromethyl group, a trifluoromethyl group, a hydroxymethyl group, a methoxy group, a hydroxy group, a cyano group, a -C(=O)OH group, a -C(=O)OCH group, 3 group, -C(=O)OC(CH 3 ) group, -C(=O)NH 2、 -C(=O)N(CH 3 ) 2 group, amino group, methylamino group, aminomethyl group, -S(=O) 2 NH 2 Group and SF 5 independently selected from the group Alternatively, two substituents of said phenyl group, when attached to adjacent ring atoms, may optionally be taken together to form -CH-CH 2 -NH-CH 2 - and -O-CH 2 -C(=O)-NH- 2-hydroxyindan-1-yl group and Monocyclic or bicyclic heteroaryl groups (this is Imidazol-4-yl, 1,2-oxazol-4-yl, 1,2-oxazol-5-yl, pyrazol-3-yl, pyrazol-4-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazin-3-yl, pyrazinyl, pyrimidin-4-yl, pyrimidin-5-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, 1,3-benzothiazol-6-yl, pyrrolo[2,3-d]pyrimidin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl and quinolin-8-yl is selected from optionally substituted one, two or three times, each substituent being independently selected from fluorine, chlorine, methyl, methoxy, hydroxy and morpholin-4-yl; represents a group selected from R 2 represents a hydrogen atom, a chlorine atom, or a fluorine atom; R 3 but Propyl, cyclohexyl, trifluoromethyl, 1-hydroxyethyl, allyl, aminomethyl, (dimethylamino)methyl, (tert-butoxycarbonylamino)methyl, 2-(dimethylamino)ethyl, pyrrolidin-1-yl-methyl, and phenyl represents a group selected from R 4 and R 5 But together, *-(CH 2 ) 2 -S-#、 *-(CH 2 ) 4 -#、 *-CH 2 -C(H)(C(=O)OH)-(CH 2 ) 2 -#、 *-CH 2 -CF 2 -(CH 2 ) 2 -#、 *-(CH 2 ) 3 -C(H)(C(=O)OH)-#、 *-CH(OH)-(CH 2 ) 3 -#、 *-CH 2 -CH(OH)-(CH 2 ) 2 -#、 *-(CH 2 ) 2 -CH(OH)-CH 2 -#、 *-(CH 2 ) 3 -C(H)(OH)-#、 *-CH=CH-CH(OH)-CH 2 -#、 *-CH 2 -C(CH 3 ) 2 -CH 2 -O-#、 *-(CH 2 ) 2 -O-CH 2 -#、 *-(CH 2 ) 3 -O-#、 *-(CH 2 ) 3 -N(CH 3 )-#、 *-(CH 2 ) 3 -S-#、 *-(CH 2 ) 3 -S(=O)(=NH)-#、 *-(CH 2 ) 5 -#、 *-(CH 2 ) 3 -O-CH 2 -#、 *-(CH 2 ) 2 -N(H)-(CH 2 ) 2 -#、 *-CH=CH-CH=CH-#, *-N=CH-CH=CH-#, and *-CH=CH-N=CH-# are linked together to form a group selected from In the group, "*" is R 4 represents the point of attachment to the rest of the molecule, and "#" represents R 5 represents the point of attachment to the rest of the molecule, or a tautomer, or salt thereof, or a salt of a tautomer of said compound.

7. 1. A composition for use in combination with a chemotherapeutic agent and / or anti-cancer agent and / or radiation therapy, comprising a compound selected from the group consisting of: N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(2-fluorophenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yl-oxy]-N-[3-(trifluoromethyl)phenyl]benzamide, N-(1-acetylpiperidin-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(3-chloropyridin-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(2-chloro-6-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(4-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(5-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(2-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(3,5-dimethylpyrazin-2-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine)-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(5-methylpyrimidin-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(6-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-[2-methyl-6-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-[2-(difluoromethyl)phenyl]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(5-chloropyrimidin-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(3-chloropyridin-2-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]-N-[1-(pyrazin-2-yl)piperidin-4-yl]benzamide, N-[1-(cyclopropylcarbonyl)piperidin-4-yl]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo-[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-[1-(methylsulfonyl)piperidin-4-yl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(1-methyl-2-oxopiperidin-(4R,S)-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide (diastereomeric mixture), 5-fluoro-N-(1-methylpiperidin-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(2-aminophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-[2-(methylamino)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(2-amino-6-methylphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(4-amino-2-methylphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-[3-(trifluoromethyl)-phenyl]-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-[2-chloro-4-(pentafluoro-λ6-sulfanyl)phenyl]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(oxetan-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-[2-(difluoromethyl)phenyl]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzamide, N-(2-chloro-3-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[2-methyl-3-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[2-methyl-4-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-3,5-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(3,5-dimethyl-1,2-oxazol-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(4-methyl-1,2-oxazol-5-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(4-methyl-1H-imidazol-5-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(3-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-[2-(dimethylamino)ethyl]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(1-methylpiperidin-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-[4-(trifluoromethyl)-phenyl]-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-cyclopropyl-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-cyano-4-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2-cyano-5-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2-chloro-6-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, tert-butyl 3-{[5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzoyl]amino}azetidine-1-carboxylate, N-(azetidin-3-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(6-methoxy-2-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[1-(methylsulfonyl)piperidin-4-yl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(6-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(4,4-difluorocyclohexyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(1-ethylazetidin-3-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-[4-(dimethylamino)cyclohexyl]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-ethylphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-6-methylphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4-fluoro-6-methylphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2-chloro-4,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(4-fluoro-2,6-dimethylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4-methylpyridin-3-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,4-dimethylpyridin-3-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine)-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}-N-(2,4,6-trimethylpyridin-3-yl)benzamide, N-(6-chloro-2,3-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(2-methoxy-6-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-fluorophenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-phenyl-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(4-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(2,4,6-trifluorophenyl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-[2-(trifluoromethyl)-phenyl]-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(3-methylpyridin-2-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chlorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-dichlorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(5-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-cyano-3-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(1-methyl-1H-pyrazol-5-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(tetrahydro-2H-pyran-4-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-5-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[2-methyl-5-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(3-methylpyridin-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[2-methyl-6-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(1,3-dimethyl-1H-pyrazol-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(1,4-dimethyl-1H-pyrazol-3-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-hydroxy-2-methylpropyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[2-(hydroxymethyl)-3-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]-triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[3-(hydroxymethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(quinolin-8-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(quinolin-6-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 3-{[5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzoyl]amino}-4-methylbenzoic acid, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(quinolin-5-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-methylquinolin-5-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(quinolin-7-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(3-sulfamoyl-phenyl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-methylquinolin-6-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-methyl-1,3-benzothiazol-6-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(6-methyl-1H-indazol-5-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]-triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,3-dimethoxyphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(1H-indazol-7-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[1-(4-fluorophenyl)cyclopropyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridine)-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(4-fluoro-3-hydroxy-1H-indazol-6-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]-triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(3-carbamoyl-2-methylphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(1,1-dioxidetetrahydro-2H-thiopyran-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(4,4-difluorocyclohexyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-[2-methoxy-5-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(6-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(6-methoxy-2-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(2-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-[3-(dimethylcarbamoyl)phenyl]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-[1-(methylsulfonyl)piperidin-4-yl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(5-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-[6-(morpholin-4-yl)pyridazin-3-yl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(5-methoxypyrimidin-4-yl)-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(2-methoxypyrimidin-5-yl)-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(4,6-dimethoxypyrimidin-5-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(3,5-dimethylpyrazin-2-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(6-methoxypyrazin-2-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(3-methoxypyrazin-2-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(6-methoxypyridazin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(5,6-dimethylpyrimidin-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(4-methylpyrimidin-5-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(2,4-dimethylpyrimidin-5-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(3-methylpyrazin-2-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(5-methylpyrimidin-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(4-methylpyridazin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(5-fluoropyrimidin-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-[3-(morpholin-4-yl)pyrazin-2-yl]-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(4,6-dimethylpyrimidin-5-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, N-(3-amino-2-methylphenyl)-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, N-[4-amino-2-(trifluoromethyl)phenyl]-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(2-methyl-4-sulfamoylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, N-[2-(aminomethyl)-6-methylphenyl]-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, methyl 2-({2-[(1R)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzoyl}amino)-3-methylbenzoate, 2-[(1R)-1-cyclohexylethoxy]-N-(2,3-dihydro-1H-isoindol-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, N-(5-amino-3-methylpyridin-2-yl)-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-({2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)benzoyl}amino)-3-methylbenzoic acid, tert-butyl 4-({2-[(1S)-1-cyclohexylethoxy]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)benzoyl}amino)-3-methylbenzoate, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(2-fluorophenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]-triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(2-fluoro-6-methyl-phenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]-triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-[3-(trifluoromethyl)phenyl]benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]-triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(4-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(2,4,6-trifluorophenyl)benzamide, 2-[(1S)-1-Cyclohexylethoxy]-5-fluoro-N-(3-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-[2-(trifluoromethyl)phenyl]benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(3-methylpyridin-2-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(2,6-dichlorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4])triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(5-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(2,4-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]-triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-[2-(dimethylamino)ethyl]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-[2-fluoro-6-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(1-methyl-1H-pyrazol-5-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide, N-(2-cyano-4-fluorophenyl)-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, N-(2-chloro-5-fluorophenyl)-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-Cyclohexylethoxy]-5-fluoro-N-[2-methyl-5-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide 2-[(1S)-1-Cyclohexylethoxy]-5-fluoro-N-(3-methylpyridin-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide N-(2-chloro-6-fluorophenyl)-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-[2-methyl-3-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-[2-methyl-4-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, N-(2-chloro-3-fluorophenyl)-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(1,3-dimethyl-1H-pyrazol-4-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(1-methylpiperidin-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-N-(1,4-dimethyl-1H-pyrazol-3-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(2-hydroxy-2-methylpropyl)-4-(3-oxo-5,6,7,8-tetra-hydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-[2-(hydroxymethyl)-3-(trifluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-[(1S)-1-cyclohexylethoxy]-5-fluoro-N-(5-methyl-1,2-oxazol-4-yl)-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, N-(2-chloro-4-fluorophenyl)-2-[(1S)-1-cyclohexylethoxy]-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, N-(2-chloro-6-fluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(6-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(4-methylpyridin-3-yl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-Fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(2-methylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-dichlorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2-chloro-6-methylphenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2-chloro-4-fluoro-6-methylphenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2-chloro-4,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(4-fluoro-2-methylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(5-fluoro-2-methylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-[2-methyl-6-(trifluoromethyl)phenyl]-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-[2-(difluoromethyl)phenyl]-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2-chloro-3,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(3-fluoro-2-methylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-N-(2,4,6-trifluoro-phenyl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-dichloro-4-fluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(4,5-difluoro-2-methylphenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-[2-methyl-4-(trifluoromethyl)phenyl]-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-5-fluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(4-fluoro-2,6-dimethylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4-fluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2-cyano-4-fluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-Fluoro-N-(2-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(4-chloro-2-methylpyridin-3-yl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4-methylpyridin-3-yl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4,6-dimethylpyridin-3-yl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,4-dimethylpyridin-3-yl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(2-methoxy-6-methylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(6-chloro-2,3-difluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(6-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(2-chloro-6-fluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-fluorophenyl)-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]-N-[3-(trifluoromethyl)phenyl]benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(2-fluorophenyl)-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(2-methylphenyl)-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(2S)-pentan-2-yloxy]benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(1S)-1-phenylethoxy]benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(1S)-1-phenyl-ethoxy]benzamide, 5-fluoro-N-(2-fluorophenyl)-4-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(1S)-1-phenyl-ethoxy]benzamide, 5-fluoro-N-(2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(1S)-1-phenylethoxy]benzamide, 5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(1S)-1-phenyl-ethoxy]-N-[3-(trifluoromethyl)phenyl]benzamide, 5-fluoro-N-(2-methylphenyl)-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-6-fluorophenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]-oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-[2-(difluoromethyl)phenyl]-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]-oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-dichlorophenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]-oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4-fluoro-6-methylphenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-6-methylphenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4,6-difluorophenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-[2-methyl-6-(trifluoromethyl)phenyl]-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-dichloro-4-fluorophenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]-oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(4-fluoro-2,6-dimethylphenyl)-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]-oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(4-chloro-2-methylpyridin-3-yl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4-methylpyridin-3-yl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2-chloro-4,6-dimethylpyridin-3-yl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,4-dimethylpyridin-3-yl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-methoxy-6-methylphenyl)-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]-oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(6-chloro-2,3-difluorophenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]-oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3]oxazin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(8-methyl-3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrimidin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6-dihydro[1,3]thiazolo[2,3-c][1,2,4]triazol-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-3H,5H-[1,2,4]triazolo[3,4-c][1,4]oxazepin-2(9H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-6,7,8,9-tetrahydro-3H-[1,2,4]triazolo[4,3-a]azepin-2(5H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo[1,2,4]triazolo[4,3-a]pyrazin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3]thiazin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-4-(6,6-dimethyl-3-oxo-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3]oxazin-2(3H)-yl)-5-fluoro-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 4-(6,6-difluoro-3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-N-(2,6-difluoro-phenyl)-5-fluoro-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo[1,2,4]triazolo[4,3-b]pyridazin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 2-(4-[(2,6-difluorophenyl)carbamoyl]-2-fluoro-5-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}phenyl)-3-oxo-2,3,5,6,7,8-hexahydro[1,2,4]triazolo[4,3-a]pyridine-8-(R,S)-carboxylic acid (mixture of diastereomers), 2-(4-[(2-chloro-6-fluorophenyl)carbamoyl]-2-fluoro-5-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}phenyl)-3-oxo-2,3,5,6,7,8-hexahydro[1,2,4]triazolo[4,3-a]pyridine-8-(R,S)-carboxylic acid (mixture of diastereomers), 2-(4-[(2-chloro-6-fluorophenyl)carbamoyl]-2-fluoro-5-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}phenyl)-3-oxo-2,3,5,6,7,8-hexahydro[1,2,4]triazolo[4,3-a]pyridine-6-(R,S)-carboxylic acid (mixture of diastereomers), N-(2,6-difluorophenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2R)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2R)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-fluorophenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2R)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-fluoro-N-(2-fluorophenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(1S)-1-phenylethoxy]benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(1S)-1-phenylethoxy]benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-[(1S)-1-phenylethoxy]benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-2-{[(2R,3R)-3-hydroxybutan-2-yl]oxy}-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2R)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1-(pyrrolidin-1-yl)propan-2-yl]oxy}benzamide, N-[2-(difluoromethyl)phenyl]-2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(4-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(5-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-N-(3,5-dimethylpyrazin-2-yl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(6-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(4-methylpyridazin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(2-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, 2-{[(2S)-1-(dimethylamino)propan-2-yl]oxy}-5-fluoro-N-(2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide, rac-2-{[4-(dimethylamino)butan-2-yl]oxy}-5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]oxazin-2(8H)-yl)benzamide, rac-5-fluoro-N-(2-fluoro-6-methylphenyl)-4-(3-oxo-5,6-dihydro-3H-[1,2,4]triazolo[3,4-c][1,4]-oxazin-2(8H)-yl)-2-{[1-(pyrrolidin-1-yl)propan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(3-oxo-6,7,8,9-tetrahydro-3H-[1,2,4]triazolo[4,3-d][1,4]-diazepin-2(5H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-[(8R,S)-8-hydroxy-3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo-[4,3-a]pyridin-2(3H)-yl]-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide (diastereomeric mixture), 5-chloro-N-(2,6-difluorophenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-chloro-N-(2-chloro-6-fluorophenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-chloro-N-[1-(4-fluorophenyl)cyclopropyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin)-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-chloro-N-[2-(difluoromethyl)phenyl]-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-chloro-N-(4-methylpyridazin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3- a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-chloro-N-(6-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-chloro-N-(2-methoxy-4-methylpyridin-3-yl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, 5-chloro-N-(4-fluoro-2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide 5-chloro-N-(2-methylphenyl)-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluoro-4-hydroxyphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin)-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluoro-3-hydroxyphenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin)-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(8-imino-3,8-dioxo-5,6,7,8-tetrahydro-8λ) 6 -[1,2,4]triazolo-[3,4-b][1,3]thiazin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, N-(2,6-difluorophenyl)-5-fluoro-4-(7-hydroxy-3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(6-hydroxy-3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(6-hydroxy-3-oxo-5,6-dihydro[1,2,4]triazolo[4,3-a]-pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide N-(2,6-difluorophenyl)-5-fluoro-4-(8-hydroxy-3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide rac-tert-butyl [2-{2-[(2-chloro-6-fluorophenyl)carbamoyl]-4-fluoro-5-(3-oxo-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)phenoxy}propyl]carbamate, and rac-2-{[1-aminopropan-2-yl]oxy}-N-(2-chloro-6-fluorophenyl)-5-fluoro-4-(3-oxo-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)benzamide hydrochloride, or a tautomer or salt thereof, or a salt of a tautomer of said compound A composition comprising:

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