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1. 发明申请

US20220363667A1 T-TYPE CALCIUM CHANNEL BLOCKER 有权
公开(公告)号：US20220363667A1
公开(公告)日：2022-11-17
申请号：US17259357
申请日：2019-07-17
申请人： Nippon Chemiphar Co., Ltd. , Kinki University
发明人： Hiroto Tanaka , Isao Ooi , Daisuke Saito , Kohei Hayashida , Kohei Yamamoto , Atsufumi Kawabata
IPC分类号： C07D401/14 , A61P25/04 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04 , C07F7/08 , C07D413/14 , C07D491/107 , C07D417/14 , C07D403/12 , C07D403/14 , C07D413/04 , C07D491/113 , C07D409/04
摘要： To provide a novel T-type calcium channel blocker.
A compound represented by the following General Formula (I), a tautomer or a stereoisomer of the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound, the tautomer, the stereoisomer, or the salt is used as a T-type calcium channel blocker. wherein A represents a phenyl which may have a substituent, a 4-membered to 6-membered heteroaryl ring composed of one to three identical or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom and carbon atoms as ring-constituting atoms, or a heterocondensed ring composed of the heteroaryl ring and either a benzene ring or a 6-membered heteroaryl ring composed of one to two nitrogen atoms and carbon atoms, while here, the heteroaryl ring or the heterocondensed ring may have a substituent and is bonded to a nitrogen atom of the adjacent cyclic amino by means of a carbon atom constituting these rings; B represents a phenyl which may have a substituent, a 5-membered or 6-membered heteroaryl ring composed of one to three identical or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom and carbon atoms as ring-constituting atoms, or a heterocondensed ring composed of the heteroaryl ring and either a benzene ring or a 6-membered heteroaryl ring composed of one to two nitrogen atoms and carbon atoms, while here, the heteroaryl ring or the heterocondensed ring may have a substituent and is bonded to the adjacent cyclopropyl ring by means of a carbon atom constituting these rings; R1 and R2, which may be identical or different, each represent a hydrogen atom, a halogen atom, or the like; R3 represents a hydrogen atom, a halogen atom, or the like; n and m, which may be identical or different, each represent 0 or 1; and p represents 1 or 2.

2. 发明授权

US09873683B2 P2X4 receptor antagonist 有权
公开(公告)号：US09873683B2
公开(公告)日：2018-01-23
申请号：US14903382
申请日：2014-07-11
申请人： NIPPON CHEMIPHAR CO., LTD. , KYUSHU UNIVERSITY
发明人： Shogo Sakuma , Kunio Kobayashi , Masatoshi Ushioda , Daisuke Saito , Toshiyasu Imai , Kazuhide Inoue
IPC分类号： C07D243/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D403/10 , C07D401/04 , C07D403/08 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14
CPC分类号： C07D403/10 , C07D401/04 , C07D401/14 , C07D403/08 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The present invention relates to a compound represented by the following general formula (II), wherein, in the formula, R1a to R6a represent hydrogen atom, an alkyl group having 1 to 8 carbon atoms, and the like, Xa represents C or N, Ya represents N or C(═O), provided that when Xa is C, Ya represents N, and when Xa is N, Ya represents C(═O), the double line consisting of the solid line and the broken line represents a single bond or double bond, Aa represents benzene ring, pyridine ring, and the like, Da represents tetrazole ring, imidazole ring, and the like, Ea represents —(CR9aR10a)p-Ta-, and Ga represents benzene ring, pyridine ring, and the like, which has a P2X4 receptor antagonistic activity.

3. 发明授权

US10633349B2 P2X4 receptor antagonist 有权
公开(公告)号：US10633349B2
公开(公告)日：2020-04-28
申请号：US15923685
申请日：2018-03-16
申请人： NIPPON CHEMIPHAR CO., LTD
发明人： Masatoshi Ushioda , Kunio Kobayashi , Daisuke Saito , Shogo Sakuma , Toshiyasu Imai , Kazuhide Inoue
IPC分类号： C07D243/24 , C07D243/38 , C07D401/02 , C07D471/04 , C07D243/10 , C07D403/12 , C07D401/12 , C07D405/12 , C07D243/12 , C07D409/12 , C07D401/04 , C07D413/12
CPC分类号： C07D243/10 , C07D243/12 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R1 and R2 represent hydrogen atom and the like, or R1 and R2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R3 and R4 represent hydrogen atom and the like, R5 represents hydrogen atom and the like, R6 and R7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(═O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(═O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(═O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.

4. 发明授权

US09969700B2 P2X4 receptor antagonist 有权
公开(公告)号：US09969700B2
公开(公告)日：2018-05-15
申请号：US15176857
申请日：2016-06-08
申请人： NIPPON CHEMIPHAR CO., LTD
发明人： Masatoshi Ushioda , Kunio Kobayashi , Daisuke Saito , Shogo Sakuma , Toshiyasu Imai , Kazuhide Inoue
IPC分类号： C07D243/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D243/10 , C07D401/04 , C07D413/12 , C07D471/04
CPC分类号： C07D243/10 , C07D243/12 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R1 and R2 represent hydrogen atom and the like, or R1 and R2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R3 and R4 represent hydrogen atom and the like, R5 represents hydrogen atom and the like, R6 and R7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(═O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(═O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(═O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.

5. 发明授权

US09624223B2 Morphinan derivative 有权
公开(公告)号：US09624223B2
公开(公告)日：2017-04-18
申请号：US14772188
申请日：2013-10-15
申请人： THE KITASATO INSTITUTE , NIPPON CHEMIPHAR CO., LTD.
发明人： Hiroshi Nagase , Hideaki Fujii , Eriko Nakata , Yoshikazu Watanabe , Daisuke Saito , Toshihiro Takahashi
IPC分类号： C07D471/08 , C07D491/20 , C07D471/10
CPC分类号： C07D471/08 , C07D471/10 , C07D491/20
摘要： The present invention relates to a morphinan derivative represented by the following general formula (I), wherein R1 represents hydrogen, C1-6 alkyl, C6-10 aryl, etc., R2 and R3, which are the same or different, represent hydrogen, hydroxy, etc., R4 and R5 represent hydrogen, C1-6 alkyl, etc., R6 represents hydrogen, hydroxy, C1-6 alkyl, etc., X represents O or CH2, Y represents C═O, C(═O)O, etc., and m and n, which are the same or different, represent an integer of 0 to 2 (m and n are not 0 at the same time), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as an analgesic, antianxiety drug, etc. containing the same as an active ingredient.

6. 发明授权

US10173990B2 URAT1 inhibitor 有权
公开(公告)号：US10173990B2
公开(公告)日：2019-01-08
申请号：US15507888
申请日：2015-12-28
申请人： Nippon Chemiphar Co., Ltd. , J-Pharma Co., Ltd. , DeThree Res. Lab. Inc.
发明人： Tsuyoshi Endo , Kunio Kobayashi , Hiroto Tanaka , Daisuke Saito , Masuharu Hirano , Hitoshi Endou , Naohiko Anzai
IPC分类号： C07D275/04 , C07D411/04 , C07C255/54 , C07D215/20 , C07D215/36 , C07C321/24 , C07D417/12 , C07D471/04 , C07D263/54 , C07D209/08 , C07D277/62 , C07D285/14 , C07D213/30 , A61K31/277 , A61K31/404 , A61K31/423 , A61K31/428 , A61K31/433 , A61K31/437 , A61K31/4406 , A61K31/47 , A61K31/33
摘要： Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R1a, R2a, R6a, and R7a represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, R3a and R8a form a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which R3a and R8a are bonded, R4a and R5a form a benzene ring together with two carbon atoms to which R4a and R5a are bonded or represent any of the groups represented by R1a described above, Wa represents CR10a or N, and where, R10a represents any of the groups represented by R1a, Xa represents an oxygen atom or a sulfur atom, Ya represents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Za represents CO2H).

7. 发明申请

US20170290795A1 URAT1 INHIBITOR 审中-公开
公开(公告)号：US20170290795A1
公开(公告)日：2017-10-12
申请号：US15507888
申请日：2015-12-28
申请人： Nippon Chemiphar Co., Ltd. , J-Pharma Co., Ltd. , DeThree Res. Lab. Inc.
发明人： Tsuyoshi Endo , Kunio Kobayashi , Hiroto Tanaka , Daisuke Saito , Masaharu Hirano , Hitoshi Endou , Naohiko Anzai
IPC分类号： A61K31/33 , A61K31/404 , C07D215/20 , A61K31/47 , C07D471/04 , A61K31/277 , A61K31/428
CPC分类号： A61K31/33 , A61K31/277 , A61K31/404 , A61K31/423 , A61K31/428 , A61K31/433 , A61K31/437 , A61K31/4406 , A61K31/47 , C07C255/54 , C07C321/24 , C07D209/08 , C07D213/30 , C07D215/20 , C07D215/36 , C07D263/54 , C07D275/04 , C07D277/62 , C07D285/14 , C07D411/04 , C07D417/12 , C07D471/04
摘要： Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R1a, R2a, R6a, and R7a represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, R3a and R8a form a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which R3a and R8a are bonded, R4a and R5a form a benzene ring together with two carbon atoms to which R4a and R5a are bonded or represent any of the groups represented by R1a described above, Wa represents CR10a or N, and where, R10a represents any of the groups represented by R1a, Xa represents an oxygen atom or a sulfur atom, Ya represents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Za represents CO2H.)

8. 发明申请

US20230087342A1 AZEPANE DERIVATIVE 有权
公开(公告)号：US20230087342A1
公开(公告)日：2023-03-23
申请号：US17762134
申请日：2020-09-29
申请人： Nippon Chemiphar Co., Ltd.
发明人： Yoshikazu Watanabe , Daisuke Saito , Kohei Hayashida , Kohei Yamamoto , Mayu Namiki , Yuzo Mogi , Masahiro Yata
IPC分类号： C07D471/08 , C07D519/00 , A61P29/00
摘要： Provided are: an azepan derivative represented by general formula (I) and a pharmaceutically acceptable salt thereof (in the formula: R1 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, etc.; R2 and R3 are the same as or different from each other, and represent a hydrogen atom, a C1-6 alkyl group which may have a substituent, etc.; R4 and R5 are the same as or different from each other, and represent a hydrogen atom, a C1-6 alkyl group which may have a substituent, etc.; R6 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, etc.; R7 and R8 are the same as or different from each other, and represent a hydrogen atom, a C1-6 alkyl group which may have a substituent, etc.; R9 and R10 are the same as or different from each other, and represent a hydrogen atom, a C1-6 alkyl group which may have a substituent, etc.; R11 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, etc.; A and B differently represent a methyl group, a carbonyl group, etc.; and X represents a nitrogen atom or an N-oxide.).

9. 发明授权

US11434207B2 P2X4 receptor antagonist 有权
公开(公告)号：US11434207B2
公开(公告)日：2022-09-06
申请号：US16826877
申请日：2020-03-23
申请人： NIPPON CHEMIPHAR CO., LTD
发明人： Masatoshi Ushioda , Kunio Kobayashi , Daisuke Saito , Shogo Sakuma , Toshiyasu Imai , Kazuhide Inoue
IPC分类号： A61P25/04 , A61P29/00 , A61P43/00 , C07D243/10 , C07D403/12 , C07D401/12 , C07D405/12 , C07D243/12 , C07D409/12 , C07D401/04 , C07D413/12 , C07D471/04
摘要： The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R1 and R2 represent hydrogen atom and the like, or R1 and R2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R3 and R4 represent hydrogen atom and the like, R5 represents hydrogen atom and the like, R6 and R7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(═O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(═O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(═O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.

10. 发明授权

US09840497B2 P2X4 receptor antagonist 有权
公开(公告)号：US09840497B2
公开(公告)日：2017-12-12
申请号：US14903382
申请日：2014-07-11
申请人： NIPPON CHEMIPHAR CO., LTD. , KYUSHU UNIVERSITY
发明人： Shogo Sakuma , Kunio Kobayashi , Masatoshi Ushioda , Daisuke Saito , Toshiyasu Imai , Kazuhide Inoue
IPC分类号： C07D243/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D403/10 , C07D401/04 , C07D403/08 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The present invention relates to a compound represented by the following general formula (II), wherein, in the formula, R1a to R6a represent hydrogen atom, an alkyl group having 1 to 8 carbon atoms, and the like, Xa represents C or N, Ya represents N or C(═O), provided that when Xa is C, Ya represents N, and when Xa is N, Ya represents C(═O), the double line consisting of the solid line and the broken line represents a single bond or double bond, Aa represents benzene ring, pyridine ring, and the like, Da represents tetrazole ring, imidazole ring, and the like, Ea represents —(CR9aR10a)p-Ta-, and Ga represents benzene ring, pyridine ring, and the like, which has a P2X4 receptor antagonistic activity.

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