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

Abstract

The present invention relates to triazolone compounds, compounds of general formula (I): (In the formula, R 1 , R 2 , R 3 , R 4 and R 5 is as 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 disorders, as the sole agent or in combination with other active ingredients.

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 for 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, in particular 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) which 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 about 30%. AML is a malignant tumor of the myeloid lineage of blood cells. The incidence and chance of cure are highly age-dependent. The standard of chemotherapy for AML has not changed significantly in recent decades, highlighting the need for novel therapeutic approaches. The main characteristic of AML is the differentiation arrest of leukemic cells at the early stage of cell differentiation. The potential for leukemic differentiation therapy can be seen with the success of ATRA or arsenic trioxide to induce differentiation in acute promyelocytic leukemia (APL). Approximately 10% of AML belong to the APL subtype, in which the leukemic cells harbor a chromosomal translocation resulting in the fusion of an oncoprotein with a retinoic acid receptor. Although treatment with ATRA or arsenic trioxide has led to a dramatic increase in patient survival, with overall survival rates exceeding 70%, 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 dihydroorotic acid to orotic acid (Dihydroorotat-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, as 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 cancer indications, the treatment of solid tumors (e.g., neuroblastoma, melanoma, colon, breast and lung tumors), the treatment of 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 their use. Sirtuin-modulating compounds can be used to extend cell lifespan and treat and / or prevent a wide variety of diseases and disorders, including, for example, diseases or disorders associated with 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. Pat. No. 6,444,613 [Patent Document 2] International Publication No. 199802422 Brochure [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 invention (eg, the 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 a compound of general formula (I): [ka] (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 one, two or three times selected from the group consisting of halogen atoms, 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 - a haloalkyl group, C 3 ~C 8 - a cycloalkyl group, which is optionally substituted one or two times, each of the substituents 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 is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -Haloalkyl group, C 1 ~C 3 - independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, 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 remainder of the molecule through a carbon atom and is optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C1 ~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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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, aryl, -O-aryl, cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R8 ), -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 the groups selected from or two adjacent substituents of said phenyl group taken together may optionally be -N=, -NH-, -N(R 7 )-, -O-, -S-, 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, each substituent being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C 2 ~C6 -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, aryl, -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 the group consisting of 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 the group consisting of 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 - a 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 basis, -(C 1 ~C 6 -alkyl)-N(H)C(=O)R 6 basis, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 basis, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group (The 4-7-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 C 1 ~C 3 -substituted with an alkyl group, and Phenyl group which is 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, 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, aryl, -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 ~C6 -alkyl), -N(O) 2 and -N(R 7 )(R 8 ) (independently selected from the group consisting of represents a group selected from R 4 and R 5 together form a 5- to 6-membered, optionally unsaturated heterocyclic ring A of subformula (i) [ka] (In the formula, ring A is a ring that is composed of two essential atoms, a nitrogen atom bridging the two rings, and a carbon atom, and further includes -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 )-) having an additional 3 to 6 member selected from Forming R 6 is a hydrogen atom or C 1 ~C 6 Alkyl group, benzyl group 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 group, haloalkyl group, aryl group, (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), C3 ~C 8 -Cycloalkyl, C 1 ~C 6 -alkoxy, -O(C 2 ~C 6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, aryl, -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), C1 -~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, aryl, -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, 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, under 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 indicated, 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. In general, when 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, for example, the definition of a substituent of a compound of general formula (I) of the present invention means "1, 2, 3, 4 or 5, in particular 1, 2, 3 or 4, more in particular 1, 2 or 3, even more in particular 1 or 2".

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

[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] Complex substituents consist of two or more moieties, e.g. (C 1 ~C 3 -alkoxy)-(C 1 ~C 6 In the case of -alkyl-, the position of the given moiety can be at any suitable position of the composite substituent, i.e., C 1 ~C 3 - the alkoxy moiety is 1 ~C 3 -alkoxy)-(C 1 ~C 6 -alkyl)-group C 1 ~C 6- can be attached to any carbon atom of the alkyl moiety. The first or last hyphen of such a composite substituent indicates the point of attachment of said 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, said substituent can be attached at any suitable position of said ring and is attached to a suitable carbon atom and / or a suitable heteroatom.

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

[0024] In the text, when any item is referred to as "mentioned in the present specification", it means that it may be mentioned anywhere in the text.

[0025] The 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] "C 1 ~C 8 The term "C 2 -alkyl" means a linear or branched saturated monovalent hydrocarbon radical having 1, 2, 3, 4, 5 or 6 carbon atoms, such as, for example, 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, said radicals have 1, 2, 3, 4, 5 or 6 carbon atoms ("C 2 -alkyl" means a linear or branched saturated monovalent hydrocarbon radical having 1, 2, 3, 4, 5 or 6 carbon atoms, such as, for example, methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl, tert-butyl, pentyl, isopentyl, 2-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. 1 ~C 6-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 groups. In particular, said groups have 1, 2, 3 or 4 carbon atoms ("C 1 ~C 4 -alkyl"), for example, methyl, ethyl, propyl, isopropyl, butyl, sec-butyl isobutyl, or tert-butyl groups, more particularly having 1, 2 or 3 carbon atoms ("C 1 ~C 3 -alkyl"), for example, a methyl, ethyl, n-propyl or isopropyl group.

[0027] "C 1 ~C 6 The term "C-hydroxyalkyl" refers to 1 ~C 6 The term "C -alkyl" is defined above and means a linear or branched saturated monovalent hydrocarbon radical in which one or two hydrogen atoms are replaced by a hydroxy group, such as, for example, the 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 groups. In particular, said groups have 1, 2 or 3 carbon atoms ("C 1 ~C 3-hydroxyalkyl"), for example 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] "C 1 ~C 6 The term -alkylsulfanyl refers to 1 ~C 6 -alkyl" is as defined above. 1 ~C 6 The term "sulfanyl" refers to a linear or branched saturated monovalent radical of the formula (III)-alkyl)-S-, for example, methylsulfanyl, ethylsulfanyl, propylsulfanyl, isopropylsulfanyl, butylsulfanyl, sec-butylsulfanyl, isobutylsulfanyl, tert-butylsulfanyl, pentylsulfanyl, isopentylsulfanyl, hexylsulfanyl.

[0029] "C 2 ~C 8 The term "C-haloalkyl" refers to 2 ~C 8 The term "C-alkyl" refers to a linear or branched saturated monovalent hydrocarbon radical as defined above, and in which one or more of the hydrogen atoms are replaced, identically or differently, by a halogen atom. In particular, said halogen atom is a fluorine atom. 2 ~C 8 -Haloalkyl groups are, for example, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl or 1,3-difluoropropan-2-yl. In particular, said groups have 2, 3, 4, 5 or 6 carbon atoms ("C 2 ~C 6 -haloalkyl").

[0030] "C 1 ~C6 The term "C-haloalkyl" refers to 1 ~C 6 The term "C-alkyl" refers to a linear or branched saturated monovalent hydrocarbon radical as defined above, and in which one or more of the hydrogen atoms are replaced, identically or differently, by a halogen atom. In particular, said halogen atom is a fluorine atom. 1 ~C 6 -Haloalkyl groups are, for example, fluoromethyl, difluoromethyl, trifluoromethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 3,3,3-trifluoropropyl or 1,3-difluoropropan-2-yl. In particular, said groups have 1, 2, 3 or 4 carbon atoms ("C 1 ~C 4 -haloalkyl"), more particularly having 1, 2 or 3 carbon atoms ("C 1 ~C 3 -haloalkyl"), 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.

[0031] "C 1 ~C 6 The term "C-alkoxy" refers to 1 ~C 6 -alkyl" is defined as above. 1 ~C 6 In particular, said groups have 1, 2 or 3 carbon atoms ("C 1 ~C 3 -alkoxy"), for example, a methoxy, ethoxy, n-propoxy or isopropoxy group.

[0032] "C 1 ~C 6 The term "haloalkoxy" refers to a linear or branched saturated monovalent C alkyl group as defined above, in which one or more hydrogen atoms are replaced by halogen atoms, either identically or differently. 1 ~C 6 In particular, the halogen atom is a fluorine atom. 1 ~C 6 -Haloalkoxy groups are, for example, fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy or pentafluoroethoxy. In particular, said groups have 1, 2 or 3 carbon atoms ("C 1 ~C 3 -haloalkoxy"), for example, a fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoro-ethoxy or pentafluoroethoxy group.

[0033] "C 2 ~C 6 The term "alkenyl" includes one double bond and has 2, 3, 4, 5 or 6 carbon atoms, particularly 2 or 3 carbon atoms ("C 2 ~C 3"-alkenyl" means a linear or branched monovalent hydrocarbon radical, and if the alkenyl group contains more than one double bond, the double bonds can be isolated from one another or conjugated to one another.The alkenyl groups include, for example, ethenyl (or "vinyl"), prop-2-en-1-yl (or "allyl"), prop-1-en-1-yl, but-3-enyl, but-2-enyl, but-1-enyl, pent-4-enyl, pent-3-enyl, pent-2-enyl, pent-1-enyl, hex-5-enyl, hex-4-enyl, hex-3-enyl, hex-2-enyl, hex-1-enyl, prop-1-en-2-yl (or "isopropenyl"), 2-methylprop-2-enyl, 1-methylprop-2-enyl, 2-methylprop-1-enyl, 2 ... per-1-enyl, 1-methylprop-1-enyl, 3-methylbut-3-enyl, 2-methylbut-3-enyl, 1-methylbut-3-enyl, 3-methylbut-2-enyl, 2-methylbut-2-enyl, 1-methylbut-2-enyl, 3-methylbut-1-enyl, 2-methylbut-1-enyl, 1-methylbut-1-enyl, 1,1-dimethylprop-2-enyl, 1-ethylprop-1-enyl, 1-propylvinyl, 1-isopropylvinyl, 4-methylpent-4-enyl, 3-methylpent-4-enyl, 2-methylpent-4-enyl, 1 -Methylpent-4-enyl, 4-methylpent-3-enyl, 3-methylpent-3-enyl, 2-methylpent-3-enyl, 1-methylpent-3-enyl, 4-methylpent-2-enyl, 3-methylpent-2-enyl, 2-methylpent-2-enyl, 1-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, said group is allyl.

[0034] "C 2 ~C 6 The term "alkynyl" refers to an alkynyl group containing one triple bond and having 2, 3, 4, 5 or 6 carbon atoms, particularly 2 or 3 carbon atoms ("C 2 ~C 3 The C refers to a linear or branched monovalent hydrocarbon group containing the C 2 ~C 6 Alkynyl groups include, 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, 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] "C 3 ~C 8 The term "cycloalkyl" means a saturated monovalent monocyclic or bicyclic hydrocarbon ring containing 3, 4, 5, 6, 7, or 8 carbon atoms ("C 3 -C 8 The C 3 ~C 8-Cycloalkyl groups are, for example, monocyclic hydrocarbon rings, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl groups, or bicyclic hydrocarbon rings, such as bicyclo[4.2.0]octyl or octahydropentalenyl. In particular, said groups contain 3, 4, 5 or 6 carbon atoms ("C 3 ~C 6 -cycloalkyl"), for example, cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl groups. In particular, said groups contain 4, 5, 6, 7 or 8 carbon atoms ("C 4 ~C 8 -cycloalkyl"), for example, a cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl group.

[0036] "C 4 ~C 8 The term "cycloalkenyl" means 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 ("C 4 ~C 6 -cycloalkenyl). 4 ~C 8 -Cycloalkenyl groups are monocyclic hydrocarbon rings, such as cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl or cyclooctenyl groups, or bicyclic hydrocarbon rings, such as bicyclo[2.2.1]hept-2-enyl or bicyclo[2.2.2]oct-2-enyl.

[0037] "C 3 ~C 8 The term "cycloalkoxy" refers to an alkoxy group that contains 3, 4, 5, 6, 7 or 8 carbon atoms. 3 ~C 8 -cycloalkyl" is as defined above, 3 ~C 8-cycloalkyl)-O- means a saturated monovalent monocyclic or bicyclic radical, for example a cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cycloheptyloxy or cyclooctyloxy radical. In particular, said radicals have 3, 4, 5 or 6 carbon atoms ("C 3 ~C 6 -cycloalkoxy"), for example, a cyclopropyloxy, cyclobutyloxy, cyclopentyloxy or cyclohexyloxy group.

[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 4-membered ring such as, for example, azetidinyl, oxetanyl, or thietanyl; a 5-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 6-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 7-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 series of ring heteroatoms: N, O, S atoms.

[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 1 or 2 double bonds and 1 or 2 ring heteroatoms independently selected from the series: N, O, 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 which are mono- or bicyclic, especially phenyl and naphthyl.

[0046] The term "a phenyl group where two adjacent substituents taken 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 ("5-10 membered heteroaryl" groups), 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, bonded via a ring carbon atom or optionally a ring nitrogen atom (where permitted by valence).

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

[0049] In general, unless otherwise stated, a heteroaryl or heteroarylene group includes all possible isomeric forms thereof, such as tautomers and positional isomers, with respect to the point of attachment to the rest of the molecule. Thus, for some illustrative non-limiting examples, the term pyridinyl includes pyridin-2-yl, pyridin-3-yl, and pyridin-4-yl; or the term thienyl includes thien-2-yl and thien-3-yl.

[0050] In the text, for example, "C 1 ~C 6 -alkyl", "C 1 ~C 6 -haloalkyl", "C 1 ~C 6-hydroxyalkyl", "C 1 ~C 6 -alkoxy" or "C 1 ~C 6 "C-haloalkoxy" as used in the context of the definition 1 ~C 6 The term "alkyl" 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] Additionally, as used herein, the text may refer to, for example, “C 3 ~C 8 "C-cycloalkyl" as used in the context of the definition 3 ~C 8 The term "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: "C 1 ~C 8 " is C 1 , C 2 , C 3 , C 4 , C 5 , C 6 , C 7 , C 8 , C 1 ~C 8 , C 1 ~C 7 , C 1 ~C 6 , C 1 ~C 5 , C 1 ~C 4 , C 1 ~C 3 , C 1 ~C 2 , C 2 ~C 8 , C 2 ~C 7 , C 2 ~C 6 , C2 ~C 5 、C 2 ~C 4 、C 2 ~C 3 、C 3 ~C 8 、C 3 ~C 7 、C 3 ~C 6 、C 3 ~C 5 、C 3 ~C 4 、C 4 ~C 8 、C 4 ~C 7 、C 4 ~C 6 、C 4 ~C 5 、C 5 ~C 8 、C 5 ~C 7 、C 5 ~C 6 、C 6 ~C 8 、C 6 ~C 7 and C 7 ~C 8 comprising; 「C 1 ~C 6 」means C 1 、C 2 、C 3 、C 4 、C 5 、C 6 、C 1 ~C 6 、C 1 ~C 5 、C 1 ~C 4 、C 1 ~C 3 、C 1 ~C 2 、C 2 ~C 6 、C 2 ~C 5 、C 2 ~C 4 、C 2 ~C 3 、C 3 ~C 6 、C 3 ~C5 , C 3 ~C 4 , C 4 ~C 6 , C 4 ~C 5 and C 5 ~C 6 Includes; "C 1 ~C 4 " is C 1 , C 2 , C 3 , C 4 , C 1 ~C 4 , C 1 ~C 3 , C 1 ~C 2 , C 2 ~C 4 , C 2 ~C 3 and C 3 ~C 4 Includes; "C 1 ~C 3 " is C 1 , C 2 , C 3 , C 1 ~C 3 , C 1 ~C 2 and C 2 ~C 3 Includes; "C 2 ~C 6 " is C 2 , C 3 , C 4 , C 5 , C 6 , C 2 ~C 6 , C 2 ~C 5 , C 2 ~C 4 , C 2 ~C 3 , C 3 ~C 6 , C 3 ~C 5 , C 3 ~C 4 , C 4 ~C 6 , C 4 ~C5 and C 5 ~C 6 Includes; "C 3 ~C 8 " is C 3 , C 4 , C 5 , C 6 , C 7 , C 8 , C 3 ~C 8 , C 3 ~C 7 , C 3 ~C 6 , C 3 ~C 5 , C 3 ~C 4 , C 4 ~C 8 , C 4 ~C 7 , C 4 ~C 6 , C 4 ~C 5 , C 5 ~C 8 , C 5 ~C 7 , C 5 ~C 6 , C 6 ~C 8 , C 6 ~C 7 and C 7 ~C 8 Includes; "C 3 ~C 6 " is C 3 , C 4 , C 5 , C 6 , C 3 ~C 6 , C 3 ~C 5 , C 3 ~C 4 , C 4 ~C 6 , C 4 ~C 5 and C 5 ~C 6 Includes; "C 4 ~C 8 " is C 4 , C5 , C 6 , C 7 , C 8 , C 4 ~C 8 , C 4 ~C 7 , C 4 ~C 6 , C 4 ~C 5 , C 5 ~C 8 , C 5 ~C 7 , C 5 ~C 6 , C 6 ~C 8 , C 6 ~C 7 and C 7 ~C 8 Includes; "C 4 ~C 7 " is C 4 , C 5 , C 6 , C 7 , C 4 ~C 7 , C 4 ~C 6 , C 4 ~C 5 , C 5 ~C 7 , C 5 ~C 6 and C 6 ~C 7 Includes; "C 4 ~C 6 " is C 4 , C 5 , C 6 , C 4 ~C 6 , C 4 ~C 5 and C 5 ~C 6 Includes; "C 5 ~C 10 " is C 5 , C 6 , C 7 , C 8 , C 9 , C 10 , C 5 ~C10 , C 5 ~C 9 , C 5 ~C 8 , C 5 ~C 7 , C 5 ~C 6 , C 6 ~C 10 , C 6 ~C 9 , C 6 ~C 8 , C 6 ~C 7、 C 7 ~C 10、 C 7 ~C 9 , C 7 ~C 8 , C 8 ~C 10 , C 8 ~C 9 and C 9 ~C 10 Includes; "C 6 ~C 10 " is C 6 , C 7 , C 8 , C 9 , C 10 , C 6 ~C 10 , C 6 ~C 9 , C 6 ~C 8 , C 6 ~C 7、 C 7 ~C 10、 C 7 ~C 9 , C 7 ~C 8 , C 8 ~C 10 , C 8 ~C 9 and C 9 ~C 10 Includes;

[0054] As used herein, the term "leaving group" refers to an atom or group of atoms that is displaced in a chemical reaction as a stable species with the bonding electrons. In particular, such leaving groups are selected from the group comprising halides, in particular fluorides, chlorides, bromides or iodides, (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 a group "substituted" on an alkyl, haloalkyl, cycloalkyl, heterocyclyl, heterocycloalkenyl, cycloalkenyl, aryl or heteroaryl group at any atom of the group, for example replacing one or more hydrogen atoms therein. In one aspect, one or more substituents on a group are independently any combination of just one or more of any of the permissible atoms or groups of atoms depicted for that substituent. In another aspect, the substituent itself may be substituted with any one of the above substituents. Additionally, 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 may be substituted by one or more of several substituents, such substitutions are 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 agreement with the four valence electrons of carbon. By "subject" is meant a mammal, including, but not limited to, a human or a non-human mammal, such as a cow, horse, dog, sheep, rodent or cat.

[0057] It is possible for compounds of general formula (I) to exist as 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. Natural abundances of isotopes as applied in this context are 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 11 Positron-emitting isotopes, such as C, can be incorporated into the compounds of general formula (I). These isotopic variants of the compounds of general formula (I) are useful for in vivo imaging applications. 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 said reagent isotopic variant. Depending on the desired location of deuteration, in some cases D 2The deuterium of O can be directly incorporated into compounds or incorporated into reagents useful for synthesizing such compounds. 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 deuteration 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 are replaced by one or more deuterium atoms, and the abundance of deuterium at each deuterated position of the compound of general formula (I) is higher than the natural abundance of deuterium, which is about 0.015%. In particular, in the deuterium-containing compound of general formula (I), the abundance of deuterium at each deuterated position of the compound of general formula (I) is higher than 10%, 20%, 30%, 40%, 50%, 60%, 70% or 80% at said one or more positions, preferably higher than 90%, 95%, 96% or 97%, and even more preferably higher 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 the compounds 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, leading to changes in the ratio of parent compound to metabolites or the amount of metabolites produced. Such changes may result in certain therapeutic advantages and therefore may be desirable in some circumstances. A decrease in the rate of metabolism and metabolic switching, with altered ratios of metabolites, has been reported (AE Mutlib et al., Toxicol. Appl. Pharmacol., 2000, 169, 102). These changes in exposure to parent drug and metabolites can have important consequences with respect to 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 main effect of deuteration is to decrease the rate of systemic clearance. As a result, the biological half-life of the compound increases. Potential clinical benefits would include the ability to maintain similar systemic exposure with lower peak levels and higher trough levels, which could result in fewer side effects and increased 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 decrease in the rate of metabolism has resulted in increased exposure of the drug without altering the rate of total body 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. lower number of doses or lower dosage to achieve the desired effect) and / or may result in reduced amounts of metabolites.

[0065] A compound of general formula (I) may have multiple possible sites of attack on metabolism. In order to optimize the above effects on physicochemical properties and metabolic profiles, a deuterium-containing compound of general formula (I) can be selected that has a certain 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 a carbon atom and / or bonded to a cytochrome P, for example. 450 It is located at the position of the compound of general formula (I) which is the site of attack for metabolic 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 words such as compounds, salts, polymorphs, hydrates, solvates, etc. are used herein, this is taken to mean a single compound, salt, polymorph, isomer, hydrate, solvate, etc. The terms "a" or "an" as used herein 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.It is possible that one or more asymmetric carbon atoms are present in (R) or (S) configuration, which can result in racemic mixtures in the case of a single asymmetric center, and diastereomeric mixtures 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 that joins two substituted aromatic rings of a specified compound.

[0070] The preferred isomers are those which provide the more desirable biological activity. These separated, pure or partially purified isomers or racemic mixtures of the compounds of the invention are also within the scope of the 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, formation of diastereoisomeric salts or formation of covalent diastereomers with optically active acids or bases. Examples of suitable acids include tartaric acid, diacetyltartaric acid, ditoluoyltartaric acid and camphorsulfonic acid. Mixtures of diastereoisomers 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 includes the use of chiral chromatography (e.g., HPLC columns using chiral phases), 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 present invention is achieved by any suitable prior art method, for example chromatography, in particular chiral chromatography.

[0074] Additionally, it is possible for the 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] may 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 as any mixture of said tautomers in any ratio.

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

[0077] The present invention also provides useful forms of the compounds of the invention, such as metabolites, hydrates, solvates, prodrugs, salts, particularly pharma- ceutically 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 exist in stoichiometric or non-stoichiometric ratios. In the case of stoichiometric solvates, for example, hydrates, hemi-, (semi-), mono-, sesqui-, di-, tri-, tetra-, penta-isosolvates, or hydrates are respectively possible. The present invention includes all such hydrates or solvates.

[0079] It is further possible for the compounds of the invention to exist in free form, e.g., as a free base or free acid or zwitterion, or in salt form, which may be any salt, either an organic or inorganic addition salt, in particular any pharma- ceutically acceptable organic or inorganic addition salt customarily used in pharmacology or used, e.g., 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 pharma- ceutically acceptable salts of the compounds of the present invention include, for example, acid addition salts of compounds of the present invention having a nitrogen atom in the chain or ring that is sufficiently basic, 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, glycerophosphoric acid, aspartic acid, sulfosalicylic acid or thiocyanic acid.

[0082] Further suitable pharma- ceutically acceptable salts of the compounds of the invention which are sufficiently acidic are alkali metal salts, e.g. sodium or potassium salts, alkaline earth metal salts, e.g. 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, e.g. 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 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 a number of 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 stoichiometric composition of said salt forms obtained by the respective preparation and / or purification steps is in most cases unknown.

[0087] Unless otherwise specified, for example, "hydrochloride", "trifluoroacetate", "sodium salt" or "xHCl", "xCF 3 COOH, 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 the synthetic intermediates or example compounds or their salts are obtained by the preparation and / or purification steps 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 which may itself be biologically active or inactive, but which 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 ~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 the group consisting of C 2 ~C 8 - a haloalkyl group, C 3 ~C 8 - a cycloalkyl group, which is optionally substituted one or two times, each substituent being a halogen atom or hydroxy, phenyl and -N(R 7 )(R 8 ) independently selected from the group consisting of 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 the group consisting of C 2 ~C 6 -cyanoalkyl group, 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 remainder of the molecule through a carbon atom and is optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 6 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 6 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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, aryl, -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 the groups selected from or two adjacent substituents of said phenyl group taken together may optionally be -N=, -NH-, -N(R 7 )-, -O-, -S-, 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, 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, aryl, -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 the group consisting of and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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, -(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 the group consisting of 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 - a 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 basis, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) 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 the 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally 1 ~C 3 -substituted with an alkyl group, and Phenyl group which is 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, 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, aryl, -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 the group consisting of represents a group selected from R 4 and R 5 together form a 5- to 6-membered, optionally unsaturated heterocyclic ring A of subformula (i) [ka] (In the formula, ring A is -O-, -S-, -S(=O)-, -S(=O)-, in addition to the two essential atoms, the nitrogen atom and the carbon atom bridging the two rings. 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 C 1 ~C 6 Alkyl group, benzyl group 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 group, haloalkyl group, aryl group, (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, aryl, -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, aryl, -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 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 C 1 ~C 8 -Alkyl group, C 2 ~C8 -Haloalkyl group, C 3 ~C 8 -Cycloalkyl group, C 2 ~C 6 -Cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- groups, -(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, a phenyl group and a monocyclic or bicyclic heteroaryl group, Said C 1 ~C 8 The -alkyl group is optionally 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 are independently selected from the groups selected from Said C 3 ~C 8 -Cycloalkyl groups are optionally substituted one or two times, each substituent being a halogen atom or a hydroxyl, phenyl and -N(R 7 )(R 8 ) independently selected from the group consisting of 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 are independently selected from the 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, each substituent being C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 6 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 6 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups selected from The phenyl group 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 ~C6 -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, aryl, -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 the groups selected from or two adjacent substituents of said phenyl group taken together may optionally be -N=, -NH-, -N(R 7 )-, -O-, -S-, 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, 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, aryl, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), -S(O) 2 , -N(O) 2 and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl groups are optionally substituted one, two or three times, each of the substituents 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, -(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 , -N(O) 2 and -N(R 7 )(R 8 ) are independently selected from the groups 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 group, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) groups and phenyl groups represents a group selected from The 4-7 membered nitrogen-containing heterocycloalkyl group is optionally C 1 ~C 3 - substituted with an alkyl group, the 4-7 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 of the substituents 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, aryl, -O-aryl, cyano, -C(O)OR 6 , hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6-alkenyl), -S(=O) 2 , -N(O) 2 and -N(R 7 )(R 8 ) are independently selected from the groups selected from R 4 and R 5 together form a 5- to 6-membered, optionally unsaturated heterocyclic ring A of subformula (i) [ka] (In the formula, ring A is -O-, -S-, -S(=O)-, -S(=O)-, in addition to the two essential atoms, the nitrogen atom and the carbon atom bridging the two rings. 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 C 1 ~C 6 Alkyl group, benzyl group 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 group, haloalkyl group, aryl group, (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 R8 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, C1 ~C 6 -alkoxy, -O(C 2 ~C 6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, aryl, -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, C3 ~C 8 -Cycloalkoxy, aryl, -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 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 cancer, comprising: 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 the group consisting of C 2 ~C 8 - a haloalkyl group, C 3 ~C 8 - a cycloalkyl group, which is optionally substituted one or two times, each of the substituents 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 is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -Haloalkyl group, C 1 ~C 3 - independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, 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, each substituent being C 1 ~C 3 -Alkyl group, 5-6 membered heteroaryl group, -C(=O)O(C 1 ~C 4 -alkyl) group, -C(=O)(C 1 ~C6 -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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A 5- to 7-membered heterocycloalkenyl group which is attached to the remainder of the molecule through a carbon atom of said 5- to 7-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 the groups selected from or 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- and -NH-C(=O)-NH- are bonded together to form a group selected from indanyl group, 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 groups, cyano groups, hydroxy groups and -N(R 7 )(R 8 ) groups. and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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 groups, cyano 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 8 -cycloalkyl group, C 1 ~C 6 - a 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 basis, -(C 1 ~C 6 -alkyl)-N(H)C(=O)R 6 basis, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 basis, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) group wherein the 4-7 membered nitrogen-containing heterocycloalkyl group is optionally C 1 ~C 3 - substituted with an alkyl group, The 4-7 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 of the substituents being a halogen atom or a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3- independently selected from the group consisting of alkoxy and hydroxy 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=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 4represents 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 remaining ones are CH 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 remaining ones are CH 2 represents a group, R 6 is a hydrogen atom or C 1 ~C 6 Alkyl group, benzyl group 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; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is 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, C1 ~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 Groups 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 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 cancer, comprising: R 1 but C 1 ~C 8 -Alkyl group, C 2 ~C 8 -Haloalkyl group, C 3 ~C 8 -Cycloalkyl group, C 2 ~C 6 -Cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2~C 6 -alkyl)- groups, -(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, a 5- to 7-membered heterocycloalkenyl group, a phenyl group, an indanyl group, a tetralinyl group, and a monocyclic or bicyclic heteroaryl group; Said C 1 ~C 8 -alkyl group optionally 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 are independently selected from the groups selected from Said C 3 ~C 8 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from the groups 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 are independently selected from the groups selected from The 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups are attached to the remainder of the molecule through a carbon atom of the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups, and are optionally substituted one or two times, and each substituent is C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 6 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 6 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl 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 are independently selected from the groups selected from The phenyl group 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, C3 ~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 the groups selected from or two adjacent substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 -, -CH 2 -O-CH 2 -, -O-CH 2 -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 C 1 ~C 6 -Alkyl, C 1 ~C6 -Haloalkyl, C 3 ~C 8 -Cycloalkyl, C 1 ~C 6 -Alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C 3 ~C 8 -Cycloalkyl, C 1 ~C 6 -Alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from R 2 represents a hydrogen 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 ~C6 -alkyl)-N(R 7 )R 8 group, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) groups and phenyl groups represents a group selected from The 4- to 7-membered nitrogen-containing heterocycloalkyl group may optionally be C 1 ~C 3 - substituted with an 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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups 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=C(R 11 )-C(R 11 )=C(R 11 )-#, *-N=C(R11 )-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 remaining ones are CH 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)- and -S(=O) 2 - represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 One of the C(R12 ) 2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5 The remaining ones are CH 2 represents a group, R 6 is a hydrogen atom or C 1 ~C 6 Alkyl group, benzyl group 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; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is 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 Groups 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 Provided are compounds of the above general formula (I), or tautomers, N-oxides or salts thereof, and tautomers or salts of N-oxides thereof.

[0095] According to certain embodiments, the present invention provides a method for producing a medicament for the treatment of a cancer, comprising: R 1 but C 1 ~C 6 -alkyl group (which may optionally be C 3 ~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, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -independently selected from an alkoxy group and a hydroxy group C 2 ~C 6 - a haloalkyl group, C 3 ~C 6 - a cycloalkyl group, which is optionally substituted one or two times, each of the substituents 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 is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 - independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, 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 remainder of the molecule through a carbon atom of said 4- to 6-membered heterocycloalkyl group and is optionally substituted one or two times, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A 5- to 6-membered heterocycloalkenyl group which is attached to the remainder of the molecule through a carbon atom of said 5- to 6-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 )(C1 ~C 3 -alkyl), -P(=O)(C 1 ~C 3 -alkyl) 2 and S.F. 5 Independently selected from the groups selected from or 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- and -NH-C(=O)-NH- are bonded together to form a group selected from indanyl, tetralinyl, which are optionally substituted one or two times, each of the substituents being a halogen atom, 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 groups, cyano groups, hydroxy groups and -N(R 7 )(R 8 ) groups. and Monocyclic or Bicyclic Heteroaryl Groups which is 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 3 ~C 6 -Cycloalkyl group, C 1 ~C 3 -alkoxy group, C 1 ~C3 -haloalkoxy group, C 3 ~C 6 -Cycloalkoxy groups, cyano 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, 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) groups and phenyl groups represents a group selected from The 4- to 6-membered nitrogen-containing heterocycloalkyl group may optionally be C 1 ~C 3 - substituted with an alkyl group, the 4-6 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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups 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=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 remaining ones are CH 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 remaining ones are CH 2represents a group, R 6 is a hydrogen atom or C 1 ~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 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; The 4- to 6-membered nitrogen-containing heterocycloalkyl group is 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 11is, 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 Groups 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 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 cancer, comprising: R 1 but C 1 ~C 6 -Alkyl group, C 2 ~C 6 -Haloalkyl group, C 3 ~C 6 -Cycloalkyl group, C 2 ~C6 -Cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 3 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- groups, -(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, a 5- to 6-membered heterocycloalkenyl group, a phenyl group, an indanyl group, a tetralinyl group, and a monocyclic or bicyclic heteroaryl group. represents a group selected from Said C 1 ~C 6 -alkyl group optionally 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 is a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups selected from Said C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from the groups 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 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups selected from the 4- to 6-membered heterocycloalkyl group and the 5- to 6-membered heterocycloalkenyl group are attached to the remainder 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, and each substituent is C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl 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 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups selected from The phenyl group 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, C1 ~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 the groups selected from or two adjacent substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 -, -CH 2 -O-CH 2 -, -O-CH 2 -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 C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 3 ~C 6 -Cycloalkyl, C 1 ~C 3 -Alkoxy, C 1 ~C 3 -Haloalkoxy, C 3 ~C 6 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 3 ~C 6 -Cycloalkyl, C 1 ~C 3 -Alkoxy, C 1 ~C 3 -Haloalkoxy, C 3 ~C 6 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from R 2 represents a hydrogen 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 ~C6 -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)-(4- to 6-membered nitrogen-containing heterocycloalkyl) groups and phenyl groups represents a group selected from The 4- to 6-membered nitrogen-containing heterocycloalkyl group may optionally be C 1 ~C 3 - substituted with an alkyl group, the 4-6 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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups 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 -X2 -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 remaining ones are CH 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)- 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 remaining ones are CH 2 represents a group, R 6 is a hydrogen atom or C 1 ~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 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; The 4- to 6-membered nitrogen-containing heterocycloalkyl group is 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 Groups 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 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 cancer, comprising: R 1 but C 3 ~C 6 -cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, 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 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 optionally substituted one or two times, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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) groups 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)OR6 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 or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -C(=O)-NH- Indanyl groups, which are optionally substituted with hydroxy groups and Monocyclic or Bicyclic Heteroaryl Groups which is 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 -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 X4 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 remaining ones are CH 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 C(R 12 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 represents a group, R 6 is a hydrogen atom or C 1 ~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 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 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy groups 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, 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 cancer, comprising: R 1 but C 3 ~C 6 -Cycloalkyl group, C 2 ~C 6 -hydroxyalkyl group, -(C 2 ~C 6 -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 Said C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from the groups selected from said phenyl substituents are optionally substituted one, two or three times, each substituent being 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, each substituent being C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The phenyl group is optionally substituted one, two, three or four times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Hydroxyalkyl, C 1 ~C 3 -Alkoxy, 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 ), -S(=O) 2 N(R 7 )(R 8 ) and S.F. 5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Alkoxy, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from R 2 represents a hydrogen 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 and phenyl group 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 -X1 -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 remaining ones are CH 2 Representing a 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 C(R 12 ) 2 represents a group, X 1 , X2 , X 3 and X 4 The remaining ones are CH 2 represents a group, R 6 is a hydrogen atom or C 1 ~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 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 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy groups 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 cancer, comprising: 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, the 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, optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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) groups 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 or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -C(=O)-NH- Indanyl groups, which are optionally substituted with hydroxy groups 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 and -N(R 7 )(R 8 ) (independently selected from the group consisting of 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, (C1 ~C 6 -alkyl)-N(R 7 )R 8 group, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 and phenyl group 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 3and 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 remaining ones are CH 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 remaining ones are CH 2 represents a group, R 6 is a hydrogen atom or C 1 ~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 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 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy groups and -C(=O)OR 6 base represents a group selected from R 15 C 1 ~C 4 represents an 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 cancer, comprising: R 1 but C 3 ~C 6 -Cycloalkyl group, C 2 ~C 6 -hydroxyalkyl group, -(C 2 ~C 6 -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 Said C 3 ~C 6 - the cycloalkyl groups are selected from cyclopropyl and cyclohexyl, C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from the groups selected from said phenyl substituents are optionally substituted one, two or three times, each substituent being 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 C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The phenyl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Hydroxyalkyl, C 1 ~C 3 -Alkoxy, 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 ), -S(=O) 2 N(R 7 )(R 8 ) and S.F.5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Alkoxy, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from R 2 represents a hydrogen 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 )R8 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=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 remaining ones are CH 2 Representing a group, or X1 , 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 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 represents a group, R 6 is a hydrogen atom or C 1 ~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 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 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy groups 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 cancer, comprising: R 1 but C 3 ~C 6 - a cycloalkyl group selected from the group consisting of cyclopropyl and cyclohexyl groups, C 3 ~C 6 -cycloalkyl groups are optionally substituted one or two times, each substituent being independently selected from a fluorine atom, a phenyl group, and a dimethylamino group; the phenyl substituents being 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; and optionally substituted once or twice, each substituent being 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, where 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 5independently selected from the group or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent -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 and 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 -#、 *-(CH2 ) 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, 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 cancer, comprising: R 1 but C 3 ~C 6 -Cycloalkyl groups, 2-hydroxy-2-methylpropyl groups, 2-(dimethylamino)ethyl 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 Said C 3 ~C 6 - the cycloalkyl groups are selected from cyclopropyl and cyclohexyl, C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a fluorine atom or Phenyl and dimethylamino are independently selected from the 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 the 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)OCH 3 , -C(=O)OC(CH 3 ) 3 , -C(=O)NH 2、 -C(=O)N(CH 3 ) 2 , amino, methylamino, aminomethyl, -S(=O) 2 NH 2 and S.F. 5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent: -CH-CH 2 -NH-CH 2 - and -O-CH 2 -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 the groups selected from R 2 represents 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, *-(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)-#, *-(CH2 ) 3 -C(H)(OH)-#, *-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 ) 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, 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) as 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 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 one, two or three times selected from the group consisting of halogen atoms, 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 - a haloalkyl group, C 3 ~C 8 - a cycloalkyl group, which is optionally substituted one or two times, each of the substituents 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 is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -Haloalkyl group, C 1 ~C 3 - independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, 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 remainder of the molecule through a carbon atom and is optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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, aryl, -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 the groups selected from or two adjacent substituents of said phenyl group taken together may optionally be -N=, -NH-, -N(R 7 )-, -O-, -S-, 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, 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, aryl, -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 the group consisting of and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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, -(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 the group consisting of 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 C 1 ~C 8 -alkyl group (which may optionally be C 3 ~C 8 -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 C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group selected from C 2 ~C 8 - a haloalkyl group, C 3 ~C 8 -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 of which is a halogen atom or a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 - independently selected from the groups selected from alkoxy and hydroxy; C 2 ~C 6 -cyanoalkyl group, 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(R7 )(R 8 ) group, A 4- to 7-membered, optionally unsaturated heterocyclic group which is attached to the remainder of the molecule through a carbon atom and is optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 6 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 6 -alkyl) and oxo (=O); The 5- to 6-membered heteroaryl substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents being a halogen atom or a 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, aryl, -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 the groups selected from or two adjacent substituents of said phenyl group taken together may optionally be -N=, -NH-, -N(R 7)-, -O-, -S-, 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, 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, aryl, -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 the group consisting of and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C2 ~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 the group consisting of represents a group selected from Provided are compounds of formula (I) above, as well as tautomers, N-oxides and salts thereof, or tautomers or N-oxide salts of said compounds.

[0105] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 1 but C 1 ~C 8 -Alkyl group, C 2 ~C 8 -Haloalkyl group, C 3 ~C 8 -Cycloalkyl group, C 2 ~C 6 -Cyanoalkyl group, C 2 ~C 6-hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- groups, -(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, a phenyl group and a monocyclic or bicyclic heteroaryl group, Said C 1 ~C 8 -alkyl group is optionally 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 are independently selected from the groups selected from Said C 3 ~C 8 -cycloalkyl groups are optionally substituted one or two times, each substituent being a halogen atom or a hydroxyl, phenyl and -N(R 7 )(R 8 ) independently selected from the group consisting of 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 ~C3 -Alkoxy and hydroxy are independently selected from the 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 one or two times, each substituent being C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 6 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 6 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl 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 are independently selected from the groups selected from The phenyl group 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-(C1 ~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, aryl, -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 the groups selected from or two adjacent substituents of said phenyl group taken together may optionally be -N=, -NH-, -N(R 7 )-, -O-, -S-, 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, 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, aryl, -O-aryl, cyano, -C(O)OH, hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), -S(O) 2 , -N(O) 2 and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C2 ~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 , -N(O) 2 and -N(R 7 )(R 8 ) Independently selected from the 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 method for treating a pulmonary circulation comprising the steps of: R 1 is a phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents being a halogen atom or a 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 11 )(C 1 ~C 3 -alkyl), -P(=O)(C 1 ~C 3 -alkyl) 2 and S.F. 5 Independently selected from the groups selected from or two substituents of 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- and -NH-C(=O)-NH- are bonded together to form a group selected from A compound of general formula (I) is provided: According to a further embodiment, the present invention provides a method for producing a method for treating a pulmonary circulation comprising the steps of: R 1represents 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; A compound of general formula (I) is provided:

[0107] According to a further embodiment, the present invention provides a method for producing a method for treating a pulmonary circulation comprising the steps of: R 1 C 4 ~C 8 -cycloalkyl group or -(C 3 ~C 8 -cycloalkyl)-N(R 7 )(R 8 ) groups, which are optionally substituted one or two times, each substituent being a halogen atom or a hydroxy, phenyl and -N(R 7 )(R 8 ) independently selected from the group consisting of The phenyl substituents are optionally substituted one, two or three times, each of which is a halogen atom or a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -alkoxy and hydroxy; Provided are compounds of general formula (I), as well as their tautomers, N-oxides and salts, and salts of the tautomers or N-oxides.

[0108] According to a further embodiment, the present invention provides a method for producing a method for treating a pulmonary circulation comprising the steps of: R 1 represents a 4- to 7-membered heterocycloalkyl group or a 5- to 7-membered heterocycloalkenyl group, said 4- to 7-membered heterocycloalkyl group and said 5- to 7-membered heterocycloalkenyl group being optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 6 -alkyl), -C(=O)(C3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 6 -alkyl) and oxo (=O); the 4- to 7-membered heterocycloalkyl and 5- to 7-membered heterocycloalkenyl groups are attached to the remainder of the molecule via a carbon atom in the heterocycloalkyl or heterocycloalkenyl group; Provided are compounds of general formula (I), as well as their tautomers, N-oxides and salts, and salts of the tautomers or N-oxides.

[0109] According to a further embodiment, the present invention relates to 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 once or twice, each substituent being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C 3 ~C 8 -Cycloalkyl, C 1 ~C 6 -Alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C 3 ~C 8 -Cycloalkyl, C 1 ~C 6-Alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from the groups selected from Provided are compounds of general formula (I), as well as their tautomers, N-oxides and salts, and salts of the tautomers or N-oxides.

[0110] According to a further embodiment, the present invention provides a method for producing a method for treating a pulmonary circulation comprising the steps of: 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 the group consisting of C 2 ~C 8 - a haloalkyl group, C 3 ~C 8 - a cycloalkyl group, which is optionally substituted one or two times, each of the substituents 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 is a halogen atom, C 1 ~C 3 -Alkyl group, C 1~C 4 -Haloalkyl group, C 1 ~C 3 - independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, 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, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3-Alkoxy and hydroxy (independently selected from the group consisting of A 5- to 7-membered heterocycloalkenyl group which is attached to the remainder of the molecule through a carbon atom of said 5- to 7-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 the groups selected from or 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- and -NH-C(=O)-NH- are bonded together to form a group selected from indanyl group, 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, C1 ~C 6 -alkoxy group, C 1 ~C 6 -haloalkoxy group, C 3 ~C 8 -Cycloalkoxy groups, cyano groups, hydroxy groups and -N(R 7 )(R 8 ) groups. and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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 groups, cyano groups, hydroxy groups 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 C 1 ~C 8 -Alkyl group, C 2 ~C 8 -Haloalkyl group, C 3 ~C 8 -Cycloalkyl group, C 2 ~C 6 -Cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2 ~C6 -alkyl)- groups, -(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, a 5- to 7-membered heterocycloalkenyl group, a phenyl group, an indanyl group, a tetralinyl group, and a monocyclic or bicyclic heteroaryl group; Said C 1 ~C 8 -alkyl group optionally 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 are independently selected from the groups selected from Said C 3 ~C 8 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from the groups 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 are independently selected from the groups selected from the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder 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, and each substituent is C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 6 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 6 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl 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 are independently selected from the groups selected from The phenyl group 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 ~C8 -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 the groups selected from or two adjacent substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 -, -CH 2 -O-CH 2 -, -O-CH 2 -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 C 1 ~C 6 -Alkyl, C 1 ~C 6-Haloalkyl, C 3 ~C 8 -Cycloalkyl, C 1 ~C 6 -Alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C 3 ~C 8 -Cycloalkyl, C 1 ~C 6 -Alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from the 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 method for treating a pulmonary circulation comprising the steps of: R 1 but C 3 ~C 8 - a cycloalkyl group, which is optionally substituted one or two times, each of the substituents 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 is a halogen atom, C 1 ~C3 -Alkyl group, C 1 ~C 4 -Haloalkyl group, C 1 ~C 3 - independently selected from an alkoxy group and a hydroxy 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, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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 substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A 5- to 7-membered heterocycloalkenyl group which is attached to the remainder of the molecule through a carbon atom of said 5- to 7-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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 (C1 ~C 6 -alkyl) group and oxo (=O) group; The 5- to 6-membered heteroaryl substituents are optionally substituted one, two or three times, each of which is selected from the group consisting of a halogen atom and a C 1 ~C 3 -Alkyl, C 1 ~C 4 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy (independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 the groups selected from or 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- and -NH-C(=O)-NH- are bonded together to form a group selected from indanyl group, 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 groups, cyano groups, hydroxy groups and -N(R 7 )(R 8 ) groups. and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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 groups, cyano groups, hydroxy groups 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 C 3 ~C 8 - represents a group selected from a 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, Said C 3 ~C 8 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from the groups 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 are independently selected from the groups selected from the 4- to 7-membered heterocycloalkyl group and the 5- to 7-membered heterocycloalkenyl group are attached to the remainder 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, and each substituent is C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 6 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 6 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl 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 are independently selected from the groups selected from The phenyl group 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 the groups selected from or two adjacent substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 -, -CH 2 -O-CH 2 -, -O-CH 2 -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 C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C 3 ~C 8 -Cycloalkyl, C1 ~C 6 -Alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C 3 ~C 8 -Cycloalkyl, C 1 ~C 6 -Alkoxy, C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from the 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 C 1 ~C 6 -Alkyl group, C 2 ~C 6 -Haloalkyl group, C 3 ~C 6 -Cycloalkyl group, C 2 ~C 6 -Cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 3 -hydroxyalkyl)-O-(C 2 ~C6 -alkyl)- groups, -(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, a 5- to 6-membered heterocycloalkenyl group, a phenyl group, an indanyl group, a tetralinyl group, and a monocyclic or bicyclic heteroaryl group. represents a group selected from Said C 1 ~C 6 -alkyl group optionally 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 is a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups selected from Said C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from the groups 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 3 -Haloalkyl, C 1 ~C 3-Alkoxy and hydroxy are independently selected from the groups selected from the 4- to 6-membered heterocycloalkyl group and the heterocycloalkenyl group are attached to the remainder 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, and each substituent is C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl 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 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups selected from The phenyl group 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 ~C6 -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 the groups selected from or two adjacent substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 -, -CH 2 -O-CH 2 -, -O-CH 2 -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 C 1 ~C 3 -Alkyl, C 1 ~C 3-Haloalkyl, C 3 ~C 6 -Cycloalkyl, C 1 ~C 3 -Alkoxy, C 1 ~C 3 -Haloalkoxy, C 3 ~C 6 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 3 ~C 6 -Cycloalkyl, C 1 ~C 3 -Alkoxy, C 1 ~C 3 -Haloalkoxy, C 3 ~C 6 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from the 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 C 3 ~C 6 - represents a group selected from a 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, Said C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Hydroxy, phenyl and -N(R 7 )(R 8 ) are independently selected from the groups 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 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups selected from the 4- to 6-membered heterocycloalkyl group and the heterocycloalkenyl group are attached to the remainder 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, and each substituent is C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The 5- to 6-membered heteroaryl 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 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy are independently selected from the groups selected from The phenyl group 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 the groups selected from or two adjacent substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH2 -N(R 7 )-CH 2 -, -CH 2 -O-CH 2 -, -O-CH 2 -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 C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 3 ~C 6 -Cycloalkyl, C 1 ~C 3 -Alkoxy, C 1 ~C 3 -Haloalkoxy, C 3 ~C 6 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) are independently selected from the groups selected from The monocyclic or bicyclic heteroaryl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 3 ~C 6 -Cycloalkyl, C 1 ~C 3 -Alkoxy, C 1 ~C 3 -Haloalkoxy, C 3 ~C 6 -Cycloalkoxy, cyano, hydroxy and -N(R 7 )(R 8 ) Independently selected from the 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 C 3 ~C 6 -cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, 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 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 optionally substituted one or two times, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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) groups 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 or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -C(=O)-NH- Indanyl groups, which are optionally substituted with hydroxy groups and Monocyclic or Bicyclic Heteroaryl Groups which is 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 -Alkoxy groups, hydroxy groups 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 C 3 ~C 6 -Cycloalkyl group, C 2 ~C 6 -hydroxyalkyl group, -(C2 ~C 6 -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 Said C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from the groups selected from said phenyl substituents are optionally substituted one, two or three times, each substituent being 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, each substituent being C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The phenyl group is optionally substituted one, two, three or four times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Hydroxyalkyl, C 1 ~C 3 -Alkoxy, Cyano, -C(=O)OR6 , -C(=O)N(R 7 )(R 8 ), -N(R 7 )(R 8 ), -(C 1 ~C 3 -alkyl)-N(R 7 )(R 8 ), -S(=O) 2 N(R 7 )(R 8 ) and S.F. 5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from the 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 C 3 ~C 6 -cycloalkyl groups, which are optionally substituted one or two times, each of the substituents being halogen atoms, 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 a halogen atom; 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 optionally substituted one or two times, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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) groups 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 or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent -CH 2-N(R 7 )-CH 2 - and -O-CH 2 -C(=O)-NH- Indanyl groups, which are optionally substituted with hydroxy groups and Monocyclic or Bicyclic Heteroaryl Groups which is 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 -Alkoxy groups, hydroxy groups 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 C 3 ~C 6 -Cycloalkyl groups, 4- to 6-membered heterocycloalkyl groups, phenyl groups, indanyl groups, and monocyclic or bicyclic heteroaryl groups represents a group selected from Said C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from the groups selected from said phenyl substituents are optionally substituted one, two or three times, each substituent being 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, each substituent being C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The phenyl group is optionally substituted one, two, three or four times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Hydroxyalkyl, C 1 ~C 3 -Alkoxy, 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 ), -S(=O) 2 N(R 7 )(R 8 ) and S.F. 5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 - 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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from the 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 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, the 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, optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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) groups 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 or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent -CH 2 -N(R 7 )-CH 2 - and -O-CH2 -C(=O)-NH- Indanyl groups, which are optionally substituted with hydroxy groups 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 and -N(R 7 )(R 8 ) (independently selected from the group consisting of 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 C 3 ~C 6 -Cycloalkyl group, C 2 ~C 6 -hydroxyalkyl group, -(C 2 ~C 6 -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 Said C 3 ~C 6 - the cycloalkyl groups are selected from cyclopropyl and cyclohexyl, C 3 ~C6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from the groups selected from said phenyl substituents are optionally substituted one, two or three times, each substituent being 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 C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The phenyl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3 -Hydroxyalkyl, C 1 ~C 3 -Alkoxy, Cyano, -C(=O)OR 6 , -C(=O)N(R 7 )(R 8 ), -N(R7 )(R 8 ), -(C 1 ~C 3 -alkyl)-N(R 7 )(R 8 ), -S(=O) 2 N(R 7 )(R 8 ) and S.F. 5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from the 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 ~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, the 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 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, optionally substituted once or twice, each substituent being C 1 ~C 3 -Alkyl group, 5-6 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) groups 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(R7 )(R 8 ) group, -S(=O) 2 N(R 7 )(R 8 ) group and SF 5 are independently selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -C(=O)-NH- Indanyl groups, which are optionally substituted with hydroxy groups 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 and -N(R 7 )(R 8 ) (independently selected from the group consisting of 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 C 3 ~C 6 -Cycloalkyl groups, 4- to 6-membered heterocycloalkyl groups, phenyl groups, indanyl groups, and monocyclic or bicyclic heteroaryl groups represents a group selected from Said C 3 ~C 6 - the cycloalkyl groups are selected from cyclopropyl and cyclohexyl, C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a halogen atom or Phenyl and -N(R 7 )(R 8 ) are independently selected from the groups selected from said phenyl substituents are optionally substituted one, two or three times, each substituent being 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 C 1 ~C 3 -Alkyl, 5-6 membered heteroaryl, -C(=O)O(C 1 ~C 4 -alkyl), -C(=O)(C 1 ~C 3 -alkyl), -C(=O)(C 3 ~C 6 -cycloalkyl), -S(=O) 2 (C 1 ~C 3 -alkyl) and oxo (=O) are independently selected from the groups selected from The phenyl group is optionally substituted one, two or three times, each of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Haloalkyl, C 1 ~C 3-Hydroxyalkyl, C 1 ~C 3 -Alkoxy, 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 ), -S(=O) 2 N(R 7 )(R 8 ) and S.F. 5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH 2 -N(R 7 )-CH 2 - and -O-CH 2 -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 of the substituents being a halogen atom or C 1 ~C 3 -Alkyl, C 1 ~C 3 -Alkoxy, hydroxy and -N(R 7 )(R 8 ) Independently selected from the 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 C 3 ~C 6 - a cycloalkyl group selected from the group consisting of cyclopropyl and cyclohexyl groups, C 3 ~C 6 -cycloalkyl groups are optionally substituted one or two times, each substituent being independently selected from a fluorine atom, a phenyl group, and a dimethylamino group; the phenyl substituents being 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; and optionally substituted once or twice, each substituent being 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, where 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 5independently selected from the group or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent -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 and 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 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 C 3 ~C 6 -Cycloalkyl groups, 2-hydroxy-2-methylpropyl groups, 2-(dimethylamino)ethyl 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 Said C3 ~C 6 - the cycloalkyl groups are selected from cyclopropyl and cyclohexyl, C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a fluorine atom or Phenyl and dimethylamino are independently selected from the 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 the 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)OCH 3 , -C(=O)OC(CH 3 ) 3 , -C(=O)NH 2、 -C(=O)N(CH 3 ) 2 , amino, methylamino, aminomethyl, -S(=O) 2 NH 2 and S.F. 5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH-CH 2 -NH-CH2 - and -O-CH 2 -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 the 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 C 3 ~C 6 - a cycloalkyl group selected from the group consisting of cyclopropyl and cyclohexyl groups, C 3 ~C 6 -cycloalkyl groups are optionally substituted one or two times, each substituent being independently selected from a fluorine atom, a phenyl group, and a dimethylamino group; the phenyl substituents being 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; and optionally substituted once or twice, each substituent being 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, where 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 or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent -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 and 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 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 C 3 ~C 6 -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 Said C 3 ~C 6 - the cycloalkyl groups are selected from cyclopropyl and cyclohexyl, C 3 ~C 6 - the cycloalkyl group is optionally substituted one or two times, each substituent being a fluorine atom or Phenyl and dimethylamino are independently selected from the 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 the 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)OCH 3 , -C(=O)OC(CH 3 ) 3 , -C(=O)NH 2、 -C(=O)N(CH 3 ) 2 , amino, methylamino, aminomethyl, -S(=O) 2 NH 2 and S.F. 5 Independently selected from the groups selected from or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent: -CH-CH 2 -NH-CH 2 - and -O-CH 2 -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 the 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 C 1 ~C 6 -Alkyl group C 3 ~C 8 -cycloalkyl group, C 1 ~C 6 - a haloalkyl group, C 1 ~C6 -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 basis, -(C 1 ~C 6 -alkyl)-N(H)C(=O)R 6 basis, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 basis, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) groups, which are attached to the alkyl group via a carbon atom of the heterocycloalkyl group, and optionally 1 ~C 3 -substituted with an alkyl group, and Phenyl group which is optionally substituted one, two or three times, each of the substituents 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 ~C6 -alkenyl), C 1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, aryl, -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 the group consisting of 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 C 1 ~C 6 -Alkyl group C 3 ~C 8 -cycloalkyl group, C 1 ~C 6 - a 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 basis, -(C 1 ~C 6 -alkyl)-(4- to 7-membered nitrogen-containing heterocycloalkyl) 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 optionally the 4- to 7-membered nitrogen-containing heterocycloalkyl group is 1 ~C 3 -substituted with an alkyl group, and Phenyl group which is optionally substituted one, two or three times, each of the substituents 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, aryl, -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 the group consisting of 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 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)-(4- to 7-membered nitrogen-containing heterocycloalkyl) groups and phenyl groups represents a group selected from The 4- to 7-membered nitrogen-containing heterocycloalkyl group may optionally be C 1 ~C 3 - substituted with an 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 of the substituents being a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C 6 -Haloalkyl, C 2 ~C 6 -Alkenyl, C 2 ~C6 -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, aryl, -O-aryl, cyano, -C(O)OR 6 , hydroxy, -SH, -S-(C 1 ~C 6 -alkyl), -S-(C 2 ~C 6 -alkenyl), -S(=O) 2 , -N(O) 2 and -N(R 7 )(R 8 ) Independently selected from the 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 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 ~C6 -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) groups and phenyl groups represents a group selected from The 4- to 7-membered nitrogen-containing heterocycloalkyl group may optionally be C 1 ~C 3 - substituted with an 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 of the substituents 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 the 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 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, C2 ~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)-(4- to 7-membered nitrogen-containing heterocycloalkyl) groups and phenyl groups represents a group selected from The 4- to 7-membered nitrogen-containing heterocycloalkyl group may optionally be C 1 ~C 3 - substituted with an 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 of the substituents 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 the 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 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, 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 The 4-6 membered nitrogen-containing heterocycloalkyl group may optionally be C 1 ~C 3 - substituted with an 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 of the substituents 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 the group consisting of 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 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)-(4- to 6-membered nitrogen-containing heterocycloalkyl) groups and phenyl groups represents a group selected from The 4-6 membered nitrogen-containing heterocycloalkyl group may optionally be C 1 ~C 3 - substituted with an alkyl group, the 4-6 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 of the substituents 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 the 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 C 1 ~C 6 -Alkyl group, C 3 ~C 6 -Cycloalkyl group, C 1 ~C 6 -Haloalkyl group, C 1 ~C6 -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 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 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 and phenyl 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.

[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 subformula (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 -represents a group independently selected from R 11 is independently for each occurrence a hydrogen atom, a halogen atom or C 1 ~C 6 -Alkyl, C 1 ~C6 -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, aryl, -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 ) A group selected from More specifically: Hydrogen atom, 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 A group selected from represents More specifically, in the groups (ii) to (x), X 1 , X2 , 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 remaining are CH 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 remaining are CH 2 represents a group, 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 ~C3 -represents a group selected from a haloalkoxy group and a cyano group ), Even more specifically, there are provided compounds of formula (I) as above, or a tautomer, N-oxide or salt thereof, or a tautomer or N-oxide salt of said compound, 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 subformula (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 -represents a group independently selected from 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 -C6 -alkoxy, -O(C 2 -C 6 -alkenyl), C 1 -C 6 -Haloalkoxy, C 3 -C 8 -Cycloalkoxy, aryl, -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 ) A group selected from More specifically: Hydrogen atom, 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 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 X5 The remaining are CH 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)- 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 remaining are CH 2 represents a group, 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 -represents a group selected from a haloalkoxy group and a cyano group ), Even more specifically, there are provided compounds of formula (I) above which form the ring systems disclosed in the Examples, as well as the tautomers, N-oxides and salts thereof, and the 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 5But 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=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 , X2 , 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 remaining ones are CH 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 remaining ones are CH 2 Representing a 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 *-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=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 remaining ones are CH 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)- 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 remaining ones are CH 2 Representing a 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 *-CH 2 -X 1 -X 2 -#, *-CH 2 -X 1 -X 2 -X 3 -#, *-CH 2 -X 1 -X2 -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=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 , X3 , X 4 and X 5 The remaining ones are CH 2 Representing a 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 *-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=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 remaining ones are CH 2 Representing a 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 *-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=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 X5 The remaining ones are CH 2 Representing a 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 *-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=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)- 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 remaining ones are CH 2 Representing a group, and the tautomers, N-oxides and salts thereof, and the 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 *-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 remaining ones are CH 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 C(R 12 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 Representing a 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 *-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 remaining ones are CH 2 Representing a 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 *-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 -N(R 7 )-, -O-, -S- and -S(=O)(=NR 14 )- represents a group selected from X 1 , X 2 , X 3 and X 4 C(R 12 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 Representing a 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 *-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=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 remaining ones are CH 2 Representing a 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 ) 2 represents a group, X 1 , X 2 , X 3 and X4 The remaining ones are CH 2 Representing a 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 *-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=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 X1 , X 2 , X 3 and X 4 The remaining ones are CH 2 Representing a 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 *-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=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 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 Representing a 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, *-(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, 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 R5 are combined to form *-(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 2 ) 3 -C(H)(OH)-#, *-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 ) 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, 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 *-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 - 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 5represents 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 remaining ones are CH 2 Representing a 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 *-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 -# 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 remaining ones are CH 2 Representing a 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 *-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 - and *-CH=C(R11 )-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 remaining ones are CH 2 Representing a 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 *-CH 2 -X 1 -X 2 -#, *-CH 2 -X 1 -X 2 -X 3 -#, *-CH 2 -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 remaining ones are CH 2 Representing a 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, *-(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 -#, *-(CH2 ) 2 -CH(OH)-CH 2 -#, *-(CH 2 ) 3 -C(H)(OH)-#, *-CH=CH-CH(OH)-CH 2 -#, *-(CH 2 ) 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 *-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 -#, 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 remaining ones are CH 2 Representing a 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 *-CH 2 -X 1 -X 2 -#, *-CH 2 -X 1 -X 2 -X 3 -#, *-CH 2 -X 1 -X 2 -X 3 -X 4 -#, and *-CH 2 -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 remaining ones are CH 2 Representing a 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 *-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 -, *-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 remaining ones are CH 2 Representing a 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 *-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 -#, *-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 X5 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 remaining ones are CH 2 Representing a 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 *-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 -#, and *-CH(R 13 )-X1 -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 remaining ones are CH 2 Representing a 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 *-CH 2 -X 1 -X 2 -#, *-CH 2 -X 1-X 2 -X 3 -#, *-CH 2 -X 1 -X 2 -X 3 -X 4 -#, and *-CH 2 -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 remaining ones are CH 2 Representing a 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 *-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 - 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 5represents 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 remaining ones are CH 2 Representing a 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, *-(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 2 ) 3 -C(H)(OH)-#, *-(CH 2 ) 5 -# and *-CH=CH-CH=CH-# are linked together to form a group selected from In the group, "*" is R 4represents 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 *-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 -# 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 remaining ones are CH 2 Representing a 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, *-(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 2 ) 3 -C(H)(OH)-#, and *-(CH 2 ) 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, *-(CH 2 ) 2 -S-#, *-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 ) 3 -O-CH 2 -#, *-(CH 2 ) 2 -N(H)-(CH 2 ) 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, *-(CH 2 ) 2 -S-#, *-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 -O-CH 2 -#, *-(CH 2 ) 2 -N(H)-(CH 2 ) 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, *-(CH 2 ) 2 -S-#, *-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 ) 3 -O-CH 2 -#, and *-(CH 2 ) 2 -N(H)-(CH 2 ) 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, *-(CH 2 ) 2 -S-#, *-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-#, *-(CH2 ) 3 -O-CH 2 -#, and *-(CH 2 ) 2 -N(H)-(CH 2 ) 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 *-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=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 X5 The remaining ones are CH 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 remaining ones are CH 2 represents a group, 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), C1 ~C 6 -Haloalkoxy, C 3 ~C 8 -Cycloalkoxy, aryl, -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 but 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, aryl, -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 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 *-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=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 remaining ones are CH 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)- and -S(=O) 2 - represents a group selected from X 1 , X 2 , X 3 , X 4 and X 5One 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 remaining ones are CH 2 represents a group, 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 Groups 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 *-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=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 X1 , X 2 , X 3 , X 4 and X 5 The remaining ones are CH 2 represents a group, 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, aryl, -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 ~C3 represents an alkyl group, R 13 but 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, aryl, -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 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 *-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=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 5represents 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 remaining ones are CH 2 represents a group, 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, aryl, -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 but 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, aryl, -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 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 *-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=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 remaining ones are CH 2 represents a group, 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 3represents an alkyl group, R 13 but Hydroxy group, -C(=O)OR 6 Groups 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.

[0193] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: 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=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)- 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 remaining ones are CH 2 represents a group, 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, R13 but Hydroxy group, -C(=O)OR 6 Groups 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 *-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 5represents 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 remaining ones are CH 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 C(R 12 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 represents a group, R 11 represents a hydrogen atom, R 12 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy groups 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 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 *-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 , X2 , 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 remaining ones are CH 2 represents a group, R 11 represents a hydrogen atom, R 12 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group,

[0196] R 13 but Hydroxy groups 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 *-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 -N(R 7 )-, -O-, -S- and -S(=O)(=NR 14 )- represents a group selected from X 1 , X 2 , X 3 and X 4 C(R 12 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 represents a group, R 11 represents a hydrogen atom, R 12 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy groups and -C(=O)OR 6base 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 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 *-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=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 remaining ones are CH 2 Representing a 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 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 represents a group, R 11 represents a hydrogen atom, 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 groups 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 *-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=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 remaining ones are CH 2 represents a group, R 11 represents a hydrogen atom, 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 groups 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 *-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=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 ) 2 represents a group, X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 represents a group, R 11 represents a hydrogen atom, R 12 is, independently for each occurrence, a hydrogen atom, a halogen atom or C 1 ~C 3 represents an 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, *-(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 2 ) 3 -C(H)(OH)-#, *-CH 2 -C(CH 3 ) 2 -CH 2 -O-#, *-(CH2 ) 2 -O-CH 2 -#, *-(CH 2 ) 3 -O-#, *-(CH 2 ) 3 -N(CH 3 )-#, *-(CH 2 ) 3 -S-#, *-(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, 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 *-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 -, 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 remaining ones are CH 2 represents a group, 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 Groups 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: 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 -#, 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 4represents 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 remaining ones are CH 2 represents a group, 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 Groups 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: R4 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 -, 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 remaining ones are CH 2 represents a group, 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 Groups 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 *-CH 2 -X 1 -X 2 -#, *-CH 2 -X 1 -X 2 -X 3 -#, *-CH 2 -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 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 C(R 12 ) 2 and CH(R 13 ) represents a group selected from X 1 , X 2 , X 3 and X 4 The remaining ones are CH 2 represents a group, R 11 represents a hydrogen atom, 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 groups 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 *-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 -#, 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 remaining ones are CH 2 represents a group, 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, R13 but Hydroxy group, -C(=O)OR 6 Groups 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 *-CH 2 -X 1 -X 2 -#, *-CH 2 -X 1 -X 2 -X 3 -#, *-CH 2 -X 1 -X 2 -X 3 -X 4 -#, and *-CH 2 -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 remaining ones are CH 2 represents a group, 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 Groups 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 ~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 Groups 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 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 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 *-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 -#, *-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 remaining ones are CH 2 represents a group, 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 Groups 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 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 *-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 -#, *-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 remaining ones are CH 2 represents a group, 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 ~C3 represents an alkyl group, R 13 but Hydroxy group, -C(=O)OR 6 Groups 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 *-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 -#, 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 X5 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 remaining ones are CH 2 represents a group, 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 Groups 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 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 *-CH 2 -X 1 -X 2 -#, *-CH 2 -X 1 -X 2 -X 3 -#, *-CH 2 -X 1 -X 2 -X 3 -X 4 -#, and *-CH 2 -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 remaining ones are CH 2 represents a group, R12 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 Groups 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 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 13 but Hydroxy group, -C(=O)OR 6 Groups 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 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, *-(CH 2 ) 2 -S-#, *-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 -#, *-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, *-(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 ) 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, *-CH 2 -C(CH 3 ) 2 -CH 2 -O-#, *-(CH 2 ) 2 -O-CH 2 -#, *-(CH 2 ) 3 -O-#, and *-(CH 2 ) 3 -O-CH 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.

[0218] In a further embodiment, the present invention provides a method for producing a pharmaceutical composition comprising: R 4 and R 5 But together, *-(CH 2 ) 3 -N(CH 3 )-#, *-(CH 2 ) 3 -S(=O)(=NH)-#, *-(CH 2 ) 2 -N(H)-(CH 2 ) 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 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 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 C 1 ~C 6 -Alkyl 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 C 1 ~C 4 -Alkyl 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 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; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is optionally C 1 ~C 3 -Alkyl, -S(=O) 2 (C 1 ~C 3 -alkyl) and -C(=O)O(C 1 ~C 4 -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 C 1 ~C 6 -Alkyl group, C 2 ~C 6 -hydroxyalkyl groups and -(C...

Claims

1. Compounds of formula (I) 【Chemistry 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 one, two or three times selected from the group consisting of halogen atoms, 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 - a haloalkyl group, C 3 ~C 8 -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 of which is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -Haloalkyl group, C 1 ~C 3 -independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- groups, -(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 remainder of the molecule through a carbon atom and is optionally substituted once or twice, each substituent being 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 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 the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 the groups selected from or two adjacent substituents of said phenyl group taken together may optionally be -N=, -NH-, -N(R 7 )-, -O-, -S-, 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, 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 the group selected from and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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, -(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 the group consisting of 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 - a 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 basis, -(C 1 ~C 6 -alkyl)-N(H)C(=O)R 6 base, -(C 1 ~C 6 -alkyl)-N(H)C(=O)OR 15 basis, -(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 of the substituents 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 the group consisting of represents a group selected from R 4 and R 5 together form a 5- to 8-membered, optionally unsaturated heterocyclic ring A of subformula (i) 【Chemistry 2】 (wherein, ring A is a ring that is a nitrogen atom and a carbon atom that bridge the two rings, which are the two essential atoms, and is also -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 )-, with an additional 3 to 6 members selected from 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 group, haloalkyl group, aryl group, (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 the group consisting of C 2 ~C 8 - a haloalkyl group, C 3 ~C 8 -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 of which is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -Haloalkyl group, C 1 ~C 3 -independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- groups, -(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 which is optionally substituted one or two times, each substituent being 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 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 the group consisting of A 5- to 7-membered heterocycloalkenyl group which is attached to the remainder of the molecule through a carbon atom of said 5- to 7-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being 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 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 the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 the groups selected from or 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 together to form a group selected from indanyl group, 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 groups, cyano groups, hydroxy groups and -N(R 7 )(R 8 ) groups). and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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 groups, cyano 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 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 4-7 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 of the substituents 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 the group consisting of 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 remaining ones are CH 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 remaining ones are CH 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; The 4- to 7-membered nitrogen-containing heterocycloalkyl group is 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 Groups 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 2. A compound according to claim 1, 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 is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 - independently selected from an alkoxy group and a hydroxy group C 2 ~C 6 - a haloalkyl group, C 3 ~C 6 -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 of which is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 3 -Haloalkyl group, C 1 ~C 3 -independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 3 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- groups, -(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 remainder of the molecule through a carbon atom of said 4- to 6-membered heterocycloalkyl group and is optionally substituted one or two times, each substituent being 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 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 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy Independently selected from the group consisting of A 5- to 6-membered heterocycloalkenyl group which is attached to the remainder of the molecule through a carbon atom of said 5- to 6-membered heterocycloalkenyl group and is optionally substituted once or twice, each substituent being 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 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 3 -Haloalkyl, C 1 ~C 3 -Alkoxy and hydroxy Independently selected from the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 the groups selected from or 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 together to form a group selected from indanyl, tetralinyl, which are optionally substituted one or two times, each of the substituents being a halogen atom, 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 groups, cyano groups, hydroxy groups 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 groups, cyano 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, 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 4-6 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 of the substituents 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 the group consisting of 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 remaining ones are CH 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 remaining ones are CH 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; The 4- to 6-membered nitrogen-containing heterocycloalkyl group is 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 Groups 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 2. A compound according to claim 1, 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 the substituents being halogen atoms, phenyl groups and -N(R 7 )(R 8 ) groups, 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 optionally substituted one or two times, each substituent being 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) groups 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 independently selected from the group or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent -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 remaining ones are CH 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 remaining ones are CH 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 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy groups 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, 2. A compound according to claim 1, 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, 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, optionally substituted once or twice, each substituent being 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) groups 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 independently selected from the group or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally together represent -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 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 and -N(R 7 )(R 8 ) Independently selected from the group consisting of 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 group 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 remaining ones are CH 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 remaining ones are CH 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 are the same or different, hydrogen atoms, halogen atoms or C 1 ~C 3 represents an alkyl group, R 13 but Hydroxy groups and -C(=O)OR 6 base represents a group selected from R 15 C 1 ~C 4 represents an alkyl group, 2. A compound according to claim 1, 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, C 3 ~C 6 -cycloalkyl groups are optionally substituted one or two times, each substituent being independently selected from a fluorine atom, a phenyl group, and a dimethylamino group; wherein said 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 being 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, where 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 base 、 -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 or two substituents of said phenyl group, when attached to adjacent ring atoms, optionally taken together, represent -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 and 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, 2. A compound according to claim 1, or a tautomer or salt thereof, or a salt of a tautomer of said compound.

7. 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-oxopiperidine-(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 (mixture of diastereomers), 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 (mixture of diastereomers), 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.

8. A process for preparing a compound of general formula (I) according to any one of claims 1 to 6, comprising the step of: 【Chemistry 3】 (In the formula, R 2 , R 3 , R 4 and R 5 is as defined for the compounds of general formula (I) according to any one of claims 1 to 6. with a compound of general formula (X): 【Chemistry 4】 (In the formula, R 1 is as defined for the compounds of general formula (I) according to any one of claims 1 to 6. React with Thereby, compounds of the general formula (I): 【Chemistry 5】 (In the formula, R 1 , R 2 , R 3 , R 4 and R 5 is as defined for the compounds of general formula (I) according to any one of claims 1 to 6. obtaining and then optionally converting said compound into a solvate, salt and / or solvate of said salt using a corresponding (i) solvent and / or (ii) base or acid.

9. A pharmaceutical composition comprising a compound of general formula (I) as defined in any one of claims 1 to 6 or a compound as defined in claim 7, together with one or more pharma- ceutically acceptable excipients.

10. one or more first active ingredients selected from the compounds of general formula (I) according to any one of claims 1 to 6 and the compounds according to claim 7, and - one or more further active ingredients selected from anticancer drugs 23. A pharmaceutical combination comprising:

11. A pharmaceutical composition comprising a compound of general formula (I) according to any one of claims 1 to 6 or a compound according to claim 7 for treating or preventing a disease.

12. 12. The pharmaceutical composition of claim 11, wherein the disease is a hyperproliferative or inflammatory disorder.

13. The pharmaceutical composition of claim 12, wherein the disease is cancer.

14. 14. The pharmaceutical composition of claim 13, wherein the cancer disease is selected from solid tumors, leukemia and lymphoma.

15. 15. The pharmaceutical composition of claim 14, wherein the cancer disease is selected from lung cancer, glioblastoma, prostate cancer, acute myeloid leukemia and lymphoma.

16. For the preparation of a compound of general formula (I) according to any one of claims 1 to 6, Compounds of general formula (IX): 【Chemistry 6】 (In the formula, R 2 , R 3 , R 4 and R 5 is as defined for the compounds of general formula (I) according to any one of claims 1 to 6. Use of.

17. For the preparation of a compound of general formula (I) according to any one of claims 1 to 6, Compounds of formula (X): 【Chemistry 7】 (In the formula, R 1 is as defined for the compounds of general formula (I) according to any one of claims 1 to 6. Use of.

18. A composition comprising a compound according to any one of claims 1 to 6 or a compound according to claim 7 for use in a method of treating lymphoma in a subject, the method comprising administering to the subject an effective amount of a compound according to any one of claims 1 to 6 or a compound according to claim 7.

19. A composition comprising a compound according to any one of claims 1 to 6 or a compound according to claim 7 for use in a method of reducing proliferation of a cell, the method comprising contacting the cell with an effective amount of a compound according to any one of claims 1 to 6 or a compound according to claim 7.

20. Compounds of formula (I) 【Chemistry 8】 (In the formula, R 4 and R 5 are bonded to each other so that, together with the nitrogen atom and carbon atom to which they are attached, they form a 5- to 7-membered saturated or partially unsaturated ring substituted once with a hydroxy group. A method for producing Compounds of formula (Ia) 【Chemistry 9】 (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 one, two or three times selected from the group consisting of halogen atoms, 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 - a haloalkyl group, C 3 ~C 8 -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 of which is a halogen atom, C 1 ~C 3 -Alkyl group, C 1 ~C 4 -Haloalkyl group, C 1 ~C 3 -independently selected from an alkoxy group and a hydroxy group; C 2 ~C 6 -cyanoalkyl group, C 2 ~C 6 -hydroxyalkyl group, (C 2 ~C 6 -hydroxyalkyl)-O-(C 2 ~C 6 -alkyl)- groups, -(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 remainder of the molecule through a carbon atom and is optionally substituted once or twice, each substituent being 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 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 the group selected from A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 the groups selected from or two adjacent substituents of said phenyl group taken together may optionally be -N=, -NH-, -N(R 7 )-, -O-, -S-, 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, 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 the group selected from and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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, -(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 the group consisting of 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 - a 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 of the substituents 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 the group consisting of represents a group selected from R 4 and R 5 Let's get 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 -# are linked together to form a group selected from X 1 , X 2 , X 3 and X 4 Ha-CH 2 - and 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 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 group, haloalkyl group, aryl group, (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 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 with Escherichia coli transformed with a plasmid having the nucleic acid sequences of SEQ ID NO:1 and SEQ ID NO:2 in a culture medium to form a compound of general formula (I).

21. Compounds of formula (I) according to claim 20 【Chemistry 10】 (In the formula, R 4 and R 5 Let's get together *-CH(OH)-X 1 -X 2 -#、 *-CH 2 -CH(OH)-X 2 -#、 *-CH(OH)-X 1 -X 2 -X 3 -#、 *-CH 2 -CH(OH)-X 2 -X 3 -#、 *-CH 2 -X 1 -CH(OH)-X 3 -#、 *-CH=CH-CH(OH)-X 3 -#、 *-CH(OH)-X 1 -X 2 -X 3 -X 4 -#、 *-CH 2 -CH(OH)-X 2 -X 3 -X 4 -#、 *-CH 2 -X 1 -CH(OH)-X 3 -X 4 -#、 *-CH 2 -X 1 -X 2 -CH(OH)-X 4 -#、 are linked together to form a group selected from X 1 , X 2 , X 3 and X 4 Ha-CH 2 - and 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) A method for producing Compounds of formula (Ia) 【Chemistry 11】 (In the formula, R 4 and R 5 Let's get 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 -# are linked together to form a group selected from X 1 , X 2 , X 3 and X 4 Ha-CH 2 - and 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) with Escherichia coli transformed with a plasmid having the nucleic acid sequences of SEQ ID NO:1 and SEQ ID NO:2 in a culture medium to form a compound of general formula (I).

22. 22. The method of claim 20 or 21, wherein the reaction occurs under aerobic conditions in the temperature range of 20-30°C, and the medium is a buffer solution, a nutrient solution and optionally a complexing agent.

23. 23. A composition for use in the method according to any one of claims 20 to 22, comprising E. coli transformed with a plasmid having the nucleic acid sequence of SEQ ID NO:1 and SEQ ID NO:

2.

24. A compound of formula (Ia) 【Chemistry 12】 (In the formula, R 4 and R 5 Let's get 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 -# are linked together to form a group selected from X 1 , X 2 , X 3 and X 4 Ha-CH 2 - and 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) By reacting with the compound of the general formula (I) 【Chemistry 13】 (In the formula, R1 is C 1 -C 8 -alkyl groups (which may optionally be C 3 -C 8 -cycloalkyl, phenyl and monocyclic or bicyclic heteroaryl and is substituted with a group selected from said phenyl substituents are optionally substituted one, two or three times with one or more substituents independently selected from halogen atoms, C 1 -C 3 -alkyl groups, C 1 -C 4 -haloalkyl groups, C 1 -C 3 -alkoxy groups and hydroxy groups; C2-C8-haloalkyl groups, C 3 -C 8 -cycloalkyl groups, which are optionally substituted once or twice, each substituent being independently selected from 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, C 1 -C 3 -alkyl groups, C 1 -C 4 -haloalkyl groups, C 1 -C 3 -alkoxy groups and hydroxy groups; C2-C6-cyanoalkyl groups, C2-C6-hydroxyalkyl groups, the (C 2 -C 6 -hydroxyalkyl)-O—(C 2 -C 6 -alkyl)- group, the -(C2-C6-alkyl)-N(R7)(R8) group, the -(C1-C6-alkyl)-C(=O)N(R7)(R8) group, a 4- to 7-membered, optionally unsaturated heterocyclic group which is attached to the remainder of the molecule via a carbon atom and which is optionally substituted once or twice, each substituent being independently selected from a C 1 -C 3 -alkyl group, a 5- to 6-membered heteroaryl group, a -C(=O)O(C 1 -C 4 -alkyl) group, a -C(=O)(C 1 -C 6 -alkyl) group, a -C(=O)(C 3 -C 6 -cycloalkyl) group, a -S(=O) 2 (C 1 -C 6 -alkyl) group and an oxo(=O) group; The 5- to 6-membered heteroaryl 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 the group consisting of A phenyl group, which is optionally substituted 1, 2, 3, 4 or 5 times, each of the substituents 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 SF 5 Independently selected from the groups selected from Alternatively, two adjacent substituents of said phenyl group may together form a 5- or 6-membered, optionally heterocyclic, aromatic or non-aromatic ring, optionally having 1 to 3 heteroatoms independently selected from -N=, -NH-, -N(R 7 )-, -O-, -S- and optionally containing a C(=O) group, the ring thus formed being optionally substituted once or twice, 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 the group selected from and Monocyclic or bicyclic heteroaryl groups, which are optionally substituted one, two or three times, each of the substituents 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, -(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 the group consisting of represents a group selected from R 2 represents a hydrogen atom or a halogen atom; R3 is C1-C6-alkyl groups C3-C8-cycloalkyl groups, C 1 -C 6 -haloalkyl groups, C 1 -C 6 -hydroxyalkyl groups, C2-C6-alkenyl groups, C2-C6-alkynyl groups, C 4 -C 8 -cycloalkenyl groups, the (C 1 -C 6 -alkyl)-N(R 7 )R 8 group, the -(C1-C6-alkyl)-N(H)C(=O)R6 group, -(C1-C6-alkyl)-N(H)C(=O)OR15 groups, -(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; said 4-7 membered nitrogen-containing heterocycloalkyl group optionally substituted with a C 1 -C 3 -alkyl group; and Phenyl group which is optionally substituted one, two or three times, each of the substituents 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 the group consisting of represents a group selected from R 6 is a hydrogen atom or C 1 -C 6 alkyl groups and benzyl groups represents a group selected from R 7 and R 8 are, independently for each occurrence, a hydrogen atom or C 1 -C 6 -alkyl groups, C 2 -C 6 -alkenyl groups, 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 ) groups; 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 are, 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 represent Nitrogen-containing 4- to 7-membered heterocycloalkyl groups represents R 14 is a hydrogen atom or Cyano and -C(=O)(C1-C3-haloalkyl) groups represents a group selected from R15 is C 1 -C 6 -Alkyl and benzyl groups represents a group selected from Use of a plasmid having the nucleic acid sequence of SEQ ID NO: 1 and the nucleic acid sequence of SEQ ID NO: 2 for preparing a transformed Escherichia coli for producing R in general formula (I) 4 and R 5 Let's get together *-CH(OH)-X 1 -X 2 -#、 *-CH 2 -CH(OH)-X 2 -#、 *-CH(OH)-X 1 -X 2 -X 3 -#、 *-CH 2 -CH(OH)-X 2 -X 3 -#、 *-CH 2 -X 1 -CH(OH)-X 3 -#、 *-CH=CH-CH(OH)-X 3 -#、 *-CH(OH)-X 1 -X 2 -X 3 -X 4 -#、 *-CH 2 -CH(OH)-X 2 -X 3 -X 4 -#、 *-CH 2 -X 1 -CH(OH)-X 3 -X 4 -#、 *-CH 2 -X 1 -X 2 -CH(OH)-X 4 -#、 are linked together to form a group selected from X 1 , X 2 , X 3 and X 4 Ha-CH 2 - and In the group, "*" represents R 4 represents the point of attachment of R to the rest of the molecule, and "#" represents the R 5 and the rest of the molecule, to represent the point of attachment, use.

Images