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1. 发明授权

US5597848A Benzenesulfonamide derivatives and use thereof 失效
标题翻译：苯磺酰胺衍生物及其用途
公开(公告)号：US5597848A
公开(公告)日：1997-01-28
申请号：US397068
申请日：1995-03-16
申请人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Nobuo Ogawa , Shunichiro Sakurai , Tomio Suzuki
发明人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Nobuo Ogawa , Shunichiro Sakurai , Tomio Suzuki
IPC分类号： C07C311/19 , C07C311/29 , A61K31/24
CPC分类号： C07C311/29 , C07C311/19
摘要： A benzenesulfonamide derivative represented by the following general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom; R.sup.2 represents a C.sub.1 -C.sub.10 straight- or branched-chain alkyl group, a C.sub.3 -C.sub.8 cycloalkyl group which may be substituted with one or more C.sub.1 -C.sub.6 alkyl groups on its ring, a C.sub.1 -C.sub.6 alkyl group substituted with one or more C.sub.3 -C.sub.8 cycloalkyl groups, 1-adamantylmethyl group, 2-norbornylmethyl group, or a C.sub.1 -C.sub.6 alkyl group substituted with one or more phenyl groups whose benzene ring may have one or more substituents; R.sup.3 represents a hydrogen atom or a lower alkyl group; and n is an integer of from 2 to 4, and a pharmacologically acceptable salt thereof. The present compounds have thromboxane A.sub.2 antagonistic activity, leucotriene antagonistic activity and the like and useful as a platelet aggregation inhibitor, antithrombotic agent, antiasthmatic agent and antiallergic agent.
摘要翻译： PCT No.PCT / JP93 / 01382 Sec。 371日期1995年3月16日 102（e）1995年3月16日PCT PCT 1993年9月29日PCT公布。公开号WO94 / 07848 日本1994年4月14日由以下通式表示的苯磺酰胺衍生物：其中R 1表示氢原子，低级烷基，低级烷氧基或卤素原子; R2表示C1-C10直链或支链烷基，可以在其环上被一个或多个C 1 -C 6烷基取代的C 3 -C 8环烷基，被一个或多个C 3取代的C 1 -C 6烷基 -C8环烷基，1-金刚烷基甲基，2-降冰片基甲基或被苯环可以具有一个或多个取代基的一个或多个苯基取代的C 1 -C 6烷基; R3表示氢原子或低级烷基; n为2〜4的整数，及其药理学上可接受的盐。本发明化合物具有血栓素A2拮抗活性，白三烯拮抗活性等，可用作血小板聚集抑制剂，抗血栓形成剂，止喘剂和抗过敏剂。

2. 发明授权

US5126337A Thiazetoquinoline-3-carboxylic acid derivative and a pharmaceutical composition comprising the same 失效
标题翻译：噻唑烷-3-羧酸衍生物和包含其的药物组合物
公开(公告)号：US5126337A
公开(公告)日：1992-06-30
申请号：US505138
申请日：1990-04-05
申请人： Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Noriyuki Yagi , Toshihiko Yoshida , Tomio Suzuki
发明人： Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Noriyuki Yagi , Toshihiko Yoshida , Tomio Suzuki
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： A thiazetoquinoline-3-carboxylic acid derivative represented by the general formula (I) ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl group; R.sub.2 is a fluorine atom or a chlorine atom; R.sub.3 is a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a halogenated lower alkanoyl, or alkoxycarbonyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, and a pharmacologically acceptable salt thereof, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for the treatment of an infectious disease by administering the same, are disclosed.

3. 发明授权

US4971990A Phenoxyethylamine derivatives, for preparing the same and composition for exhibiting excellent .alpha..sub.1 -blocking activity containing the same 失效
标题翻译：苯氧基乙胺衍生物，其制备方法和用于表现出优异的α1-阻断活性的组合物
公开(公告)号：US4971990A
公开(公告)日：1990-11-20
申请号：US301354
申请日：1989-01-24
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kazuya Mitani , Shunichiro Sakurai
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kazuya Mitani , Shunichiro Sakurai
IPC分类号： C07C311/27 , C07D295/26
CPC分类号： C07D295/26 , C07C311/27
摘要： Phenoxyethylamine derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.5 represent lower-alkyl, R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen or lower-alkyl, or ##STR2## represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R.sub.4 represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent .alpha..sub.1 -blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.

4. 发明授权

US6075035A Crystal of hydrate and process for preparation thereof 失效
标题翻译：水合物晶体及其制备方法
公开(公告)号：US6075035A
公开(公告)日：2000-06-13
申请号：US11752
申请日：1998-02-23
申请人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Noriyuki Kado , Nobuhiko Iwasaki , Hiroyuki Nishino , Makoto Takeshita
发明人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Noriyuki Kado , Nobuhiko Iwasaki , Hiroyuki Nishino , Makoto Takeshita
IPC分类号： C07D491/04 , C07D491/044 , A01N43/42
CPC分类号： C07D491/04
摘要： Dihydrate crystal of 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid providing high-intensity diffraction peaks at diffraction angles (2.theta.) of about 4.2.degree., 17.0.degree., and 21.3.degree. in a powder X-ray diffraction profile; a medicament comprising the dihydrate crystal; and a process for preparing the dihydrate crystal which comprises the steps of treating a crystalline substance containing an anhydride crystal of the above compound with hydrous acetone, and subjecting the product to drying treatment and moistening treatment.
摘要翻译： PCT No.PCT / JP96 / 02352 Sec。 371日期1998年2月23日 102（e）1998年2月23日PCT PCT 1996年8月23日PCT公布。出版物WO97 / 09330 日期1997年3月13日提供高强度衍射峰的3- [4-（8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基）哌啶子基]丙酸的二水合晶体在衍射角（2θ）为约4.2°，17.0°和21.3°的粉末X射线衍射图中; 包含二水合物晶体的药物; 以及制备二水合物晶体的方法，包括以下步骤：用含水丙酮处理含有上述化合物的无水物结晶的结晶物质，并对产物进行干燥处理和润湿处理。

5. 发明授权

US5500422A Benzamide derivative 失效
标题翻译：苯甲酰胺衍生物
公开(公告)号：US5500422A
公开(公告)日：1996-03-19
申请号：US348808
申请日：1994-11-28
申请人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Nobuhiko Iwasaki , Hiroyuki Nishino , Makoto Takeshita
发明人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Nobuhiko Iwasaki , Hiroyuki Nishino , Makoto Takeshita
IPC分类号： C07D211/58 , C07D451/04 , C07D451/14 , C07D211/36 , A61K31/445
CPC分类号： C07D451/04 , C07D211/58 , C07D451/14
摘要： A benzamide derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkanoyl group; R.sup.2 represents a hydrogen atom or a halogen atom; R.sup.3 represents a lower alkoxy group; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a lower alkyl group, or a lower alkoxy group; A represents C.sub.1 -C.sub.7 alkylene group which may optionally be substituted with a lower alkyl group; X represents a methylene group, an oxygen atom, or a sulfur atom; m represents an integer of from 0 to 3; n represents an integer of from 0 to 3; and p represents an integer of from 0 to 2 and a pharmacologically acceptable salt thereof is provided. These compounds are useful since they have gastrointestinal stimulating activity, and a pharmaceutical composition comprising said compound is useful for the treatment of gastrointestinal diseases.
摘要翻译：由下式表示的苯甲酰胺衍生物：其中R 1表示氢原子或低级烷酰基; R2表示氢原子或卤素原子; R3表示低级烷氧基; R4代表氢原子或低级烷基; R5表示氢原子，低级烷基或低级烷氧基; A表示可以被低级烷基取代的C1-C7亚烷基; X表示亚甲基，氧原子或硫原子; m表示0〜3的整数， n表示0〜3的整数， p表示0〜2的整数，并且其药理学上可接受的盐。这些化合物是有用的，因为它们具有胃肠道刺激活性，并且包含所述化合物的药物组合物可用于治疗胃肠道疾病。

6. 发明授权

US5859026A Quinoline carboxylic acid 失效
标题翻译：喹啉羧酸
公开(公告)号：US5859026A
公开(公告)日：1999-01-12
申请号：US860469
申请日：1997-07-09
申请人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Noriyuki Kada , Toshihiko Yoshida , Yoichi Yamamoto
发明人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Noriyuki Kada , Toshihiko Yoshida , Yoichi Yamamoto
IPC分类号： C07D401/04 , A61K31/47 , C07D215/233
CPC分类号： C07D401/04
摘要： 5-Amino-7-((3S,4S)-3-amino-4-methyl (or ethyl)-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid or a pharmacologically acceptable salt thereof represented by the following formula wherein asymmetric carbon atoms marked with asterisks are in the S-configurations and R.sup.1 represents methyl group or ethyl group; and an antibacterial agent comprising said compound as an active ingredient. ##STR1##
摘要翻译： PCT No.PCT / JP95 / 02614 Sec。 371日期1997年7月9日第 102（e）日期1997年7月9日PCT 1995年12月20日PCT PCT。公开号WO96 / 22988 日期：19965年9月1日 - 氨基-7 - （（3S，4S）-3-氨基-4-甲基（或乙基）-1-吡咯烷基）-1-环丙基-6-氟-1,4-二氢-8 - 甲基-4-氧代喹啉-3-羧酸或其药理学上可接受的盐，其中标有星号的不对称碳原子为S-构型，R1表示甲基或乙基; 以及包含所述化合物作为活性成分的抗菌剂。

7. 发明授权

US4528287A 6-Fluoro-1, 4-dihydro-4-oxo-7-substituted piperazinylquinoline-3-carboxylic acids and the method for preparing the same 失效
标题翻译： 6-氟-1,4-二氢-4-氧代-7-取代的哌嗪基喹啉-3-羧酸及其制备方法
公开(公告)号：US4528287A
公开(公告)日：1985-07-09
申请号：US651423
申请日：1984-09-17
申请人： Yasuo Itoh , Hideo Kato , Nobuo Ogawa , Eiichi Koshinaka , Tomio Suzuki , Noriyuki Yagi
发明人： Yasuo Itoh , Hideo Kato , Nobuo Ogawa , Eiichi Koshinaka , Tomio Suzuki , Noriyuki Yagi
IPC分类号： C07D401/02 , C07D215/56 , A61K31/47 , C07D401/04
CPC分类号： C07D215/56
摘要： The invention is concerned with the novel piperazinylquinoline-3-carboxylic acids represented by formula (I) ##STR1## or a pharmacologically-acceptable salt thereof, a process for the preparation of them, and a pharmaceutical composition which contains these new compounds as active ingredient and can be used as the therapeutic agent against bacteria.
摘要翻译：本发明涉及由式（I）表示的新型哌嗪基喹啉-3-羧酸或其药学上可接受的盐，其制备方法和含有这些新化合物的药物组合物作为活性成分，可以用作抗细菌的治疗剂。

8. 发明授权

US5334594A Amphoteric tricyclic compound 失效
标题翻译：两性三环化合物
公开(公告)号：US5334594A
公开(公告)日：1994-08-02
申请号：US15812
申请日：1993-02-10
申请人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Noriyuki Kado , Nobuhiko Iwasaki , Hiroyuki Nishino , Makoto Takeshita
发明人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Noriyuki Kado , Nobuhiko Iwasaki , Hiroyuki Nishino , Makoto Takeshita
IPC分类号： A61K31/445 , A61K31/00 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/55 , A61P11/00 , A61P17/00 , A61P27/16 , A61P37/00 , A61P37/08 , A61P43/00 , C07D491/04 , C07D491/044 , C07D491/052
CPC分类号： C07D491/04
摘要： Novel amphoteric tricyclic compound represented by the following formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a halogen atom; X represents --O--, --CH.sub.2 O--, or --OCH.sub.2 --; and Y represents a C.sub.2 -C.sub.5 alkylene group which may optionally be substituted with a lower alkyl group, and a pharmacologically acceptable salt thereof are disclosed. Also disclosed are a pharmaceutical composition comprising the same and a method for treatment of an allergic disease or bronchial asthma.
摘要翻译：由下式表示的新型两性三环化合物：其中R 1表示氢原子或卤素原子; X表示-O-，-CH 2 O-或-OCH 2 - ; 并且Y表示可以任选被低级烷基取代的C 2 -C 5亚烷基，并且其公开的药理学上可接受的盐。还公开了包含其的药物组合物和治疗过敏性疾病或支气管哮喘的方法。

9. 发明授权

US5395832A Benzamide derivatives 失效
标题翻译：苯甲酰胺衍生物
公开(公告)号：US5395832A
公开(公告)日：1995-03-07
申请号：US104095
申请日：1993-08-11
申请人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Nobuhiko Iwasaki , Hiroyuki Nishino , Makoto Takeshita
发明人： Yasuo Ito , Hideo Kato , Shingo Yasuda , Nobuhiko Iwasaki , Hiroyuki Nishino , Makoto Takeshita
IPC分类号： C07D211/58 , C07D451/04 , C07D451/14 , A61K31/46 , A61K31/44
CPC分类号： C07D451/04 , C07D211/58 , C07D451/14
摘要： A benzamide derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkanoyl group; R.sup.2 represents a hydrogen atom or a halogen atom; R.sup.3 represents a lower alkoxy group; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a lower alkyl group, or a lower alkoxy group; A represents C.sub.1 -C.sub.7 alkylene group which may optionally be substituted with a lower alkyl group; X represents a methylene group, an oxygen atom, or a sulfur atom; m represents an integer of from 0 to 3; n represents an integer of from 0 to 3; and p represents an integer of from 0 to 2 and a pharmacologically acceptable salt thereof is provided. These compounds are useful since they have gastrointestinal stimulating activity, and a pharmaceutical composition comprising said compound is useful for the treatment of gastrointestinal diseases.
摘要翻译： PCT No.PCT / JP92 / 00134 Sec。 371日期：1993年8月11日 102（e）日期1993年8月11日PCT提交1992年2月12日PCT公布。公开号WO92 / 14705 日本9月3日，1992。一种苯甲酰胺衍生物，由下式表示：其中R1表示氢原子或低级烷酰基; R2表示氢原子或卤素原子; R3表示低级烷氧基; R4代表氢原子或低级烷基; R5表示氢原子，低级烷基或低级烷氧基; A表示可以被低级烷基取代的C1-C7亚烷基; X表示亚甲基，氧原子或硫原子; m表示0〜3的整数， n表示0〜3的整数， p表示0〜2的整数，并且其药理学上可接受的盐。这些化合物是有用的，因为它们具有胃肠道刺激活性，并且包含所述化合物的药物组合物可用于治疗胃肠道疾病。

10. 发明授权

US5344828A Piperazinealkanoic acid and a pharmaceutical composition comprising the same 失效
标题翻译：哌嗪烷酸和包含其的药物组合物
公开(公告)号：US5344828A
公开(公告)日：1994-09-06
申请号：US663154
申请日：1991-03-01
申请人： Hiroyuki Sawanishi , Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kouji Morikawa
发明人： Hiroyuki Sawanishi , Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kouji Morikawa
IPC分类号： A61K31/55 , A61K31/00 , A61K31/554 , A61P1/00 , A61P1/08 , A61P9/06 , A61P9/12 , A61P25/00 , A61P25/04 , A61P37/08 , A61P43/00 , C07D223/20 , C07D267/20 , C07D281/16 , C07D487/04 , C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D487/04 , C07D223/20 , C07D267/20 , C07D281/16
摘要： Novel polycyclic compounds represented by the following formula: A--(CH.sub.2).sub.n --COOR.sup.1, wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n represents an integer of from 0 to 5; and A is a group represented by the following formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; and Y represents a methylene group, an oxygen atom, or a sulfur atom, or A is a group represented by the following formula: ##STR2## and pharmacologically acceptable salts thereof are disclosed. Also disclosed are a method for preparing the same, a pharmaceutical composition comprising the same, an antiallergic agent and an agent for bronchial asthma comprising the same, and a method for treatment of an allergic disease or bronchial asthma comprising the step of administering the same.
摘要翻译：由下式表示的新型多环化合物：A-（CH 2）n -COOR 1，其中R 1表示氢原子或低级烷基; n表示0〜5的整数， A是由下式表示的基团：其中X表示氢原子或卤素原子; Y表示亚甲基，氧原子或硫原子，或A为下式表示的基团：其中，可以列举出其药理学上可接受的盐。还公开了其制备方法，包含其的药物组合物，抗过敏剂和包含其的支气管哮喘剂，以及治疗过敏性疾病或支气管哮喘的方法，包括施用该过敏性疾病或支气管哮喘的步骤。

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