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1. 发明授权

US09365553B2 Heterocyclic compound and H1 receptor antagonist 有权
标题翻译：杂环化合物和H1受体拮抗剂
公开(公告)号：US09365553B2
公开(公告)日：2016-06-14
申请号：US13699892
申请日：2011-05-23
申请人： Makoto Okada , Koichi Hasumi , Takahiro Nishimoto , Miwa Yoshida , Kouki Ishitani , Tomoji Aotsuka , Hashime Kanazawa
发明人： Makoto Okada , Koichi Hasumi , Takahiro Nishimoto , Miwa Yoshida , Kouki Ishitani , Tomoji Aotsuka , Hashime Kanazawa
IPC分类号： C07D401/06 , C07D211/46 , C07D405/06 , C07D213/79 , C07D333/40 , C07D407/08 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号： C07D405/06 , C07D211/46 , C07D213/79 , C07D333/40 , C07D401/06 , C07D407/08 , C07D409/06 , C07D413/06 , C07D417/06
摘要： A heterocyclic compound useful as an antiallergic agent is provided.A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.
摘要翻译：提供了可用作抗过敏剂的杂环化合物。由下式（1）表示的化合物或其盐：其中环A是稠环或杂环; 环B是含有G和氮原子N作为其构成原子的杂环，其中G是CH或N; R1是羰基或亚烷基; R2a和R2b是烷基，环烷基，芳基或杂环基; X是氧原子或硫原子; Z是羟基，烷氧基，环烷氧基，芳氧基，芳烷氧基，氨基或N-取代氨基; 并且n为0或1; 条件是当环A为苯环时，或当环B为哌嗪环时，R 1为可具有取代基的亚烷基。

2. 发明申请

US20130085127A1 HETEROCYCLIC COMPOUND AND H1 RECEPTOR ANTAGONIST 有权
标题翻译：杂环化合物和H1受体拮抗剂
公开(公告)号：US20130085127A1
公开(公告)日：2013-04-04
申请号：US13699892
申请日：2011-05-23
申请人： Makoto Okada , Koichi Hasumi , Takahiro Nishimoto , Miwa Yoshida , Kouki Ishitani , Tomoji Aotsuka , Hashime Kanazawa
发明人： Makoto Okada , Koichi Hasumi , Takahiro Nishimoto , Miwa Yoshida , Kouki Ishitani , Tomoji Aotsuka , Hashime Kanazawa
IPC分类号： C07D405/06 , C07D401/06 , C07D211/46
CPC分类号： C07D405/06 , C07D211/46 , C07D213/79 , C07D333/40 , C07D401/06 , C07D407/08 , C07D409/06 , C07D413/06 , C07D417/06
摘要： A heterocyclic compound useful as an antiallergic agent is provided.A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.
摘要翻译：提供了可用作抗过敏剂的杂环化合物。由下式（1）表示的化合物或其盐：其中环A是稠环或杂环; 环B是含有G和氮原子N作为其构成原子的杂环，其中G是CH或N; R1是羰基或亚烷基; R2a和R2b是烷基，环烷基，芳基或杂环基; X是氧原子或硫原子; Z是羟基，烷氧基，环烷氧基，芳氧基，芳烷氧基，氨基或N-取代氨基; 并且n为0或1; 条件是当环A为苯环时，或当环B为哌嗪环时，R 1为可具有取代基的亚烷基。

3. 发明授权

US08193356B2 Heterocycle compound, and production process and application thereof 失效
标题翻译：杂环化合物及其制备方法和应用
公开(公告)号：US08193356B2
公开(公告)日：2012-06-05
申请号：US11991858
申请日：2006-09-15
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00 , A61P11/06
CPC分类号： C07D471/14 , C07D471/04
摘要： The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.
摘要翻译：本发明的化合物是具有特定杂环骨架的新型化合物，特别是具有通过3-位亚烷基键合的有机基团（例如，碳环和杂环）的吡唑并萘并吡啶骨架，具有磷酸二酯酶IV抑制活性。在吡唑并萘啶骨架的3位键合的环（碳环或杂环）中的至少一个和在5位键合的碳环可以具有卤代烷基和/或卤代烷氧基作为取代基。这种化合物或其盐可用作磷酸二酯酶IV抑制剂等。根据本发明，可以提供具有高磷酸二酯酶IV抑制作用的新型化合物。

4. 发明申请

US20100093782A1 Pyrazolonaphthyridine derivatives 审中-公开
标题翻译：吡唑并萘啶衍生物
公开(公告)号：US20100093782A1
公开(公告)日：2010-04-15
申请号：US12585430
申请日：2009-09-15
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： A61K31/4375 , C07D471/14 , A61P11/06
CPC分类号： A61K31/4375 , A61K31/444 , C07D471/14
摘要： The target is to provide PDE IV inhibitors which have a highly potent anti-asthmatic and/or COPD-prophylactic/therapeutic profile with unexpectedly excellent safety. A compound of the formula (1): wherein A is phenyl, pyridyl, 1-oxypyridyl, or thienyl, which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of hydroxyl, halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxyl, lower alkoxy-carbonyl, carboxy-lower alkylene, lower alkoxycarbonyl-lower alkylene, lower alkylsulfonyl, lower alkylsulfonyl-amino, and ureido; R1 is a group selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, nitro, lower alkoxy, amino, carboxyl, and lower alkoxycarbonyl; R2 is hydrogen or lower alkyl; and m is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof, possesses highly excellent PDE IV-specific inhibitory actions and is useful as an anti-asthmatic drug and/or a prophylactic/therapeutic drug for COPD with high safety.
摘要翻译：目标是提供具有非常有效的抗哮喘和/或COPD预防/治疗特征的PDE IV抑制剂，具有出人意料的极好的安全性。式（1）的化合物：其中A是苯基，吡啶基，1-氧代吡啶基或噻吩基，其可以是未取代的或任选地被一个或多个选自羟基，卤素，氰基，硝基，低级烷基，低级烷氧基，低级烷基羰基氧基，氨基，羧基，低级烷氧基 - 羰基，羧基 - 低级亚烷基，低级烷氧基羰基 - 低级亚烷基，低级烷基磺酰基，低级烷基磺酰基 - 氨基和脲基。 R 1是选自氢，羟基，卤素，氰基，硝基，低级烷氧基，氨基，羧基和低级烷氧基羰基的基团。 R2是氢或低级烷基; m为1〜3的整数。或其药学上可接受的盐具有非常优异的PDE IV特异性抑制作用，并且可用作具有高度安全性的抗哮喘药和/或用于COPD的预防/治疗药物。

5. 发明授权

US07608716B2 Pyrazolonaphthyridine derivative 有权
标题翻译：吡唑并萘啶衍生物
公开(公告)号：US07608716B2
公开(公告)日：2009-10-27
申请号：US10533806
申请日：2003-11-05
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： A61K31/4375 , C07D471/14 , C07D471/16
CPC分类号： A61K31/4375 , A61K31/444 , C07D471/14
摘要： The target is to provide PDE IV inhibitors which have a highly potent anti-asthmatic and/or COPD-prophylactic/therapeutic profile with unexpectedly excellent safety. A compound of the formula (1): wherein A is phenyl, pyridyl, 1-oxypyridyl, or thienyl, which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of hydroxyl, halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxyl, lower alkoxycarbonyl, carboxy-lower alkylene, lower alkoxycarbonyl-lower alkylene, lower alkylsulfonyl, lower alkylsulfonylamino, and ureido; R1 is a group selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, nitro, lower alkoxy, amino, carboxyl, and lower alkoxycarbonyl; R2 is hydrogen or lower alkyl; and m is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof, possesses highly excellent PDE IV-specific inhibitory actions and is useful as an anti-asthmatic drug and/or a prophylactic/therapeutic drug for COPD with high safety.
摘要翻译：目标是提供具有非常有效的抗哮喘和/或COPD预防/治疗特征的PDE IV抑制剂，具有出人意料的极好的安全性。式（1）的化合物：其中A是苯基，吡啶基，1-氧代吡啶基或噻吩基，其可以是未取代的或任选地被一个或多个选自羟基，卤素，氰基，硝基，低级烷基，低级烷氧基，低级烷基羰基氧基，氨基，羧基，低级烷氧基羰基，羧基 - 低级亚烷基，低级烷氧基羰基 - 低级亚烷基，低级烷基磺酰基，低级烷基磺酰基氨基和脲基。 R 1是选自氢，羟基，卤素，氰基，硝基，低级烷氧基，氨基，羧基和低级烷氧基羰基的基团。 R2是氢或低级烷基; m为1〜3的整数。或其药学上可接受的盐具有非常优异的PDE IV特异性抑制作用，并且可用作具有高度安全性的抗哮喘药和/或用于COPD的预防/治疗药物。

6. 发明申请

US20090131467A1 Heterocycle Compound, and Production Process and Application Thereof 失效
标题翻译：杂环化合物及其制备方法及应用
公开(公告)号：US20090131467A1
公开(公告)日：2009-05-21
申请号：US11991858
申请日：2006-09-15
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： A61K31/437 , C07D471/04 , A61P11/06 , A61P11/00
CPC分类号： C07D471/14 , C07D471/04
摘要： The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.
摘要翻译：本发明的化合物是具有特定杂环骨架的新型化合物，特别是具有通过3-位亚烷基键合的有机基团（例如，碳环和杂环）的吡唑并萘并吡啶骨架，具有磷酸二酯酶IV抑制活性。在吡唑并萘啶骨架的3位键合的环（碳环或杂环）中的至少一个和在5位键合的碳环可以具有卤代烷基和/或卤代烷氧基作为取代基。这种化合物或其盐可用作磷酸二酯酶IV抑制剂等。根据本发明，可以提供具有高磷酸二酯酶IV抑制作用的新型化合物。

7. 发明申请

US20060040972A1 Pyrazolonaphthyridine derivative 有权
标题翻译：吡唑并萘啶衍生物
公开(公告)号：US20060040972A1
公开(公告)日：2006-02-23
申请号：US10533806
申请日：2003-11-05
申请人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
发明人： Hashime Kanazawa , Tomoji Aotsuka , Kentarou Kumazawa , Kouki Ishitani , Takashi Nose
IPC分类号： A61K31/4745 , C07D471/14
CPC分类号： A61K31/4375 , A61K31/444 , C07D471/14
摘要： The target is to provide PDE IV inhibitors which have a highly potent anti-asthmatic and/or COPD-prophylactic/therapeutic profile with unexpectedly excellent safety. A compound of the formula (1): wherein A is phenyl, pyridyl, 1-oxypyridyl, or thienyl, which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of hydroxyl, halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxyl, lower alkoxycarbonyl, carboxy-lower alkylene, lower alkoxycarbonyl-lower alkylene, lower alkylsulfonyl, lower alkylsulfonylamino, and ureido; R1 is a group selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, nitro, lower alkoxy, amino, carboxyl, and lower alkoxycarbonyl; R2 is hydrogen or lower alkyl; and m is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof, possesses highly excellent PDE IV-specific inhibitory actions and is useful as an anti-asthmatic drug and/or a prophylactic/therapeutic drug for COPD with high safety.
摘要翻译：目标是提供具有非常有效的抗哮喘和/或COPD预防/治疗特征的PDE IV抑制剂，具有出人意料的极好的安全性。式（1）的化合物：其中A是苯基，吡啶基，1-氧代吡啶基或噻吩基，其可以是未取代的或任选地被一个或多个选自羟基，卤素，氰基，硝基，低级烷基，低级烷氧基，低级烷基羰基氧基，氨基，羧基，低级烷氧基羰基，羧基 - 低级亚烷基，低级烷氧基羰基 - 低级亚烷基，低级烷基磺酰基，低级烷基磺酰基氨基和脲基。 R 1是选自氢，羟基，卤素，氰基，硝基，低级烷氧基，氨基，羧基和低级烷氧基羰基的基团。 R 2是氢或低级烷基; m为1〜3的整数。或其药学上可接受的盐具有非常优异的PDE IV特异性抑制作用，并且可用作具有高度安全性的抗哮喘药和/或用于COPD的预防/治疗药物。

8. 发明授权

US07115623B2 PDE IV inhibitors 失效
标题翻译： PDE IV抑制剂
公开(公告)号：US07115623B2
公开(公告)日：2006-10-03
申请号：US10480378
申请日：2002-06-11
申请人： Tomoji Aotsuka , Kentarou Kumazawa , Nagatoshi Wagatsuma , Kouki Ishitani , Takashi Nose
发明人： Tomoji Aotsuka , Kentarou Kumazawa , Nagatoshi Wagatsuma , Kouki Ishitani , Takashi Nose
IPC分类号： C07D471/02 , A61K31/44
CPC分类号： C07D471/04
摘要： The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety. A compound of the formula (1): wherein A is methylene, lower alkylmethylene, carbonyl, etc., Y is a 5- or 6-membered heteroaryl group containing one or two heteroatoms selected from nitrogen, sulfur and oxygen, Z is i) a fused ring in which any of 5- or 6-membered heteroaryl groups is fused to a benzene ring, or ii) a phenyl group which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of nitro, amino, an amino nitrogen-containing group, etc., provided that when A is methylene, Y is a 5- or 6-membered heteroaryl group selected from the group consisting of pyrrolyl, pyridyl, etc., and Z is a phenyl group which may be unsubstituted or substituted, the substituent on said phenyl group is amino, or an amino nitrogen-containing group; or a pharmaceutically acceptable salt thereof, possesses excellent PDE IV inhibition and is useful as a pharmaceutical drug, preferably an anti-asthmatic, etc.
摘要翻译：目的是提供选择性PDE IV抑制剂，其具有优异的抗哮喘特征，具有优异的安全性。式（1）的化合物：其中A是亚甲基，低级烷基亚甲基，羰基等，Y是含有一个或两个选自氮，硫和氧的杂原子的5或6元杂芳基，Z是i）其中5-或6-元杂芳基中的任一个与苯环稠合的稠合环，或ii）可以是未取代的或任选被一个或多个选自以下的成员取代的苯基：硝基，氨基，氨基含氮基团等，条件是当A是亚甲基时，Y是选自吡咯基，吡啶基等的5或6元杂芳基，Z是可以是未取代或取代的，所述苯基上的取代基是氨基或氨基含氮基团; 或其药学上可接受的盐具有优异的PDE IV抑制作用，并且可用作药物，优选抗哮喘等。

9. 发明授权

US06642250B2 1,8-naphthyridin-2(1H)-one derivatives 失效
标题翻译： 1,8-二氮杂萘-2（1H） - 酮衍生物
公开(公告)号：US06642250B2
公开(公告)日：2003-11-04
申请号：US09889107
申请日：2001-07-11
申请人： Tomoji Aotsuka , Kentarou Kumazawa , Nagatoshi Wagatsuma , Kouki Ishitani
发明人： Tomoji Aotsuka , Kentarou Kumazawa , Nagatoshi Wagatsuma , Kouki Ishitani
IPC分类号： A61K3144
CPC分类号： C07D471/04
摘要： The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety. A compound of the formula (1): wherein: A is an unsubstituted or optionally substituted 5 or 6 membered heteroaryl group or a fused benzene ring in which any of the above-defined heteroaryl groups is fused to a benzene ring, B is carbon or nitrogen, R1 is hydrogen, lower alkyl, trifluoromethyl, hydroxyl, lower alkoxy, a residue derived from a carboxylic acid or a derivative thereof, amino, or an amino nitrogen-containing group, R2 is hydrogen, halogen, cyano, nitro, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, trifluoromethyl, hydroxyl, lower alkoxy, a residue derived from a carboxylic acid or a derivative thereof, amino, or an amino nitrogen-containing group, and m is an integer of from 1 to 8, both inclusive; or a pharmaceutically acceptable salt thereof possesses selective PDE IV inhibition and is useful as a pharmaceutical drug, preferably an anti-asthmatic, etc.
摘要翻译：目的是提供选择性PDE IV抑制剂，其具有优异的抗哮喘特征，具有优异的安全性。式（1）的化合物：其中：A是未取代或任选取代的5或6元杂芳基或稠合苯环，其中任何上述定义的杂芳基与苯环稠合，B是碳或氮，R 1是氢，低级烷基，三氟甲基，羟基，低级烷氧基，衍生自羧酸或其衍生物的氨基，氨基或氨基含氮基团，R 2是氢，卤素，氰基，硝基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，三氟甲基，羟基，低级烷氧基，衍生自羧酸或其衍生物的氨基，氨基或氨基含氮基团，m为1〜 8，均包括在内;或其药学上可接受的盐具有选择性的PDE IV抑制作用，并且可用作药物，优选抗哮喘等。

10. 发明申请

US20070197602A1 Combined pharmaceutical composition 审中-公开
标题翻译：组合药物组合物
公开(公告)号：US20070197602A1
公开(公告)日：2007-08-23
申请号：US10588725
申请日：2005-02-08
申请人： Hashime Kanazawa , Kouki Ishitani , Katsuichi Sudo , Naoto Tanimori
发明人： Hashime Kanazawa , Kouki Ishitani , Katsuichi Sudo , Naoto Tanimori
IPC分类号： A61K31/44 , A61K31/19 , A61K31/21 , A61K31/35
CPC分类号： A61K45/06 , A61K31/192 , A61K31/194 , A61K31/216 , A61K31/22 , A61K31/366 , A61K31/40 , A61K31/405 , A61K31/4418 , A61K31/445 , A61K31/47 , A61K31/7008 , A61K31/7028 , A61K2300/00
摘要： At least one hyperlipidemic agent selected from the group consisting of a fibrate compound (e.g., fenofibrate, bezafibrate, or a salt thereof) and an HMG-CoA reductase inhibitor (e.g., a statin compound, for example, pravastatin, atorvastatin, or salts thereof) is, as active ingredients, combined with an α-glucosidase inhibitor (e.g., voglibose, and acarbose) in the pharmaceutical composition of the present invention. The proportion of the α-glucosidase inhibitor may be about 0.001 to 50 parts by weight relative to 100 parts by weight of the hyperlipidemic agent. The present invention provides a pharmaceutical composition which is excellent in prophylactic and/or therapeutic effect on metabolic syndrome, hyperlipemia, diabetes, diabetes complications, etc, and has few side effects.
摘要翻译：至少一种选自贝特类化合物（例如非诺贝特，苯扎贝特或其盐）和HMG-CoA还原酶抑制剂（例如他汀类化合物，例如普伐他汀，阿托伐他汀或其盐的高脂血症药物）作为活性成分与本发明的药物组合物中的α-葡糖苷酶抑制剂（例如伏格列酮和阿卡波糖）组合。相对于100重量份的高脂血症药，α-葡糖苷酶抑制剂的比例可以为约0.001至50重量份。本发明提供了对代谢综合征，高脂血症，糖尿病，糖尿病并发症等的预防和/或治疗效果优异的副作用少的药物组合物。

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