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1. 发明授权

US07622589B2 Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效
标题翻译：取代磺酰基氨基芳基甲基环丙烷甲酰胺作为VR1受体拮抗剂
公开(公告)号：US07622589B2
公开(公告)日：2009-11-24
申请号：US11384127
申请日：2006-03-17
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： C07D213/02 , A61K31/44 , A61K31/445
CPC分类号： C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
摘要： This invention provides a compound of the formula (I): wherein, variables A, B, D, E, and R1 to R11 are as defined in the specification.
摘要翻译：本发明提供式（I）的化合物：其中变量A，B，D，E和R 1至R 11如说明书中所定义。

2. 发明申请

US20060205980A1 Substituted N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists 失效
公开(公告)号：US20060205980A1
公开(公告)日：2006-09-14
申请号：US11372706
申请日：2006-03-10
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： C07C311/46
CPC分类号： C07C311/08
摘要： This invention provides a compound of the formula (I): wherein R1 represents (C1-C6)alkyl; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkyl or halo(C1-C6)alkyl; R3 represents a halogen atom, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, [(C1-C6)alkyl]NH—, or [(C1-C6)alkyl]2N—; R4 represents a halogen atom, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, [(C1-C6)alkyl]NH—, or [(C1-C6)alkyl]2N—; R5 represents a halogen atom, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy, H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, or [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl; and * indicates a chiral centre; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

3. 发明授权

US07915448B2 Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效
公开(公告)号：US07915448B2
公开(公告)日：2011-03-29
申请号：US12578061
申请日：2009-10-13
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： C07C311/03 , A61K31/18
CPC分类号： C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
摘要： This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6) alkyl, halo(C1-C6) alkyl, hydroxy(C1-C6) alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy; H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl or 5- or 6- membered heterocyclic ring containing at least one nitrogen atom; R8 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkoxy, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; or R7 and R8, when E is CR9, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy and hydroxy(C1-C6)alkyl; and R12 represents hydrogen, halogen, (C1-C6)alkyl or hydroxy(C1-C6)alkyl; or a pharmaceutically acceptable salt or solvate thereof.

4. 发明授权

US07566739B2 Substituted N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists 失效
标题翻译：取代的N-磺酰基氨基苯乙基-2-苯氧基乙酰胺化合物作为VR1受体拮抗剂
公开(公告)号：US07566739B2
公开(公告)日：2009-07-28
申请号：US11372706
申请日：2006-03-10
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： A61K31/18 , C07C311/09 , C07C311/08
CPC分类号： C07C311/08
摘要： This invention provides compounds of the formula (I) useful for the treatment of disease conditions caused by over activation of Vr1 receptors such as pain or the like in mammals as well as compositions comprising them.
摘要翻译：本发明提供了可用于治疗由过度活化Vr1受体（例如哺乳动物的疼痛等）引起的疾病状况的式（I）化合物以及包含它们的组合物。

5. 发明申请

US20060211741A1 Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效
公开(公告)号：US20060211741A1
公开(公告)日：2006-09-21
申请号：US11384127
申请日：2006-03-17
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： A61K31/4412 , A61K31/18 , C07D213/75
CPC分类号： C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
摘要： This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy; H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl or 5- or 6-membered heterocyclic ring containing at least one nitrogen atom; R8 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkoxy, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; or R7 and R8, when E is CR9, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy and hydroxy(C1-C6)alkyl; and R12 represents hydrogen, halogen, (C1-C6)alkyl or hydroxy(C1-C6)alkyl; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

6. 发明授权

US07001917B2 Pyrazole compounds as anti-inflammatory and analgesic agents 失效
标题翻译：吡唑化合物作为抗炎和止痛剂
公开(公告)号：US07001917B2
公开(公告)日：2006-02-21
申请号：US10409881
申请日：2003-04-09
申请人： Misato Hirano , Kazunari Nakao , Seiji Nukui , Tatsuya Yamagishi
发明人： Misato Hirano , Kazunari Nakao , Seiji Nukui , Tatsuya Yamagishi
IPC分类号： A61K31/415 , C07D231/10 , A61P29/00
CPC分类号： C07D231/12 , C07D231/16 , C07D231/38 , C07D401/04 , C07D401/12 , C07D403/12 , C07D417/04 , C07D417/12 , C07D521/00
摘要： This invention provides a compound of the formula (I): wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 represents an alkyl group, etc.; R4 represents an aryl group, etc.; A represents an aryl1, etc; B represents an alkylene etc.; X represents NH, etc.; or a pharmaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglandin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供了式（

7. 发明授权

US06956050B2 Imidazole compounds as anti-inflammatory and analgesic agents 失效
标题翻译：咪唑化合物作为抗炎镇痛剂
公开(公告)号：US06956050B2
公开(公告)日：2005-10-18
申请号：US10409836
申请日：2003-04-09
申请人： Misato Hirano , Satoru Iguchi , Kazunari Nakao , Tatsuya Yamagishi
发明人： Misato Hirano , Satoru Iguchi , Kazunari Nakao , Tatsuya Yamagishi
IPC分类号： C07D233/60 , A61K31/4164 , A61K31/4439 , A61P1/04 , A61P3/10 , A61P5/00 , A61P7/02 , A61P7/04 , A61P9/00 , A61P11/06 , A61P13/12 , A61P15/08 , A61P19/02 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/06 , A61P25/20 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/12 , A61P31/16 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/08 , A61P43/00 , C07D233/54 , C07D233/61 , C07D233/88 , C07D235/08 , C07D401/04 , C07D401/12 , C07D417/04 , C07D521/00 , A61K31/4178 , C07D233/64
CPC分类号： C07D233/64 , C07D233/88 , C07D235/08 , C07D401/12 , C07D521/00
摘要： This invention provides a compound of the formula (I): wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 represents a hydrogen atom, an alkyl group, etc.; R4 represents an aryl group, etc.; A represents an aryl1, etc; B represents an alkylene etc.; X represents NH, etc.; or a pharmaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物：其中：R 1表示氢原子，烷基等; R 2表示氢原子，卤素原子等; R 3表示氢原子，烷基等; R 4表示芳基等; A表示芳基等; B表示亚烷基等。 X表示NH等。或这种化合物的药学上可接受的酯及其药学上可接受的盐。这些化合物可用于治疗由前列腺素介导的医学病症如疼痛，发热或炎症等。本发明还提供包含上述化合物的药物组合物。

8. 发明授权

US07964732B2 Substituted bicyclocarboxyamide compounds 失效
标题翻译：取代的双环羧基酰胺化合物
公开(公告)号：US07964732B2
公开(公告)日：2011-06-21
申请号：US12063159
申请日：2007-11-09
申请人： Koji Ando , Andrew Anthony Calabrese , Matthew Alexander James Duncton , Kentaro Futatsugi , Misato Hirano , Satochi Nagayama
发明人： Koji Ando , Andrew Anthony Calabrese , Matthew Alexander James Duncton , Kentaro Futatsugi , Misato Hirano , Satochi Nagayama
IPC分类号： A61P25/00 , A61P29/00 , A61P11/00 , A61P1/00
CPC分类号： C07D401/12 , C07D231/12
摘要： This invention provides a compound of the formula These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供下式的化合物这些化合物可用于治疗哺乳动物VR1受体过度活化（如疼痛等）引起的疾病状况。本发明还提供了包含上述化合物的药物组合物。

9. 发明申请

US20100267769A1 Substituted Bicyclocarboxyamide Compounds 失效
标题翻译：取代的双环羧基酰胺化合物
公开(公告)号：US20100267769A1
公开(公告)日：2010-10-21
申请号：US12063159
申请日：2007-11-09
申请人： Koji Ando , Andrew Anthony Calabrese , Matthew Alexander James Duncton , Kentaro Futatsugi , Misato Hirano , Satochi Nagayama
发明人： Koji Ando , Andrew Anthony Calabrese , Matthew Alexander James Duncton , Kentaro Futatsugi , Misato Hirano , Satochi Nagayama
IPC分类号： A61K31/415 , C07D401/12 , C07D231/12 , A61K31/4709 , A61P25/00 , A61P29/00 , A61P11/00 , A61P1/00
CPC分类号： C07D401/12 , C07D231/12
摘要： This invention provides a compound of the formula These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供下式的化合物这些化合物可用于治疗哺乳动物VR1受体过度活化（如疼痛等）引起的疾病状况。本发明还提供了包含上述化合物的药物组合物。

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