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1. 发明授权

US5432192A Tricyclic compounds and method for treating allergic diseases 失效
标题翻译：三环化合物和治疗过敏性疾病的方法
公开(公告)号：US5432192A
公开(公告)日：1995-07-11
申请号：US122603
申请日：1993-10-01
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： A61K31/195 , A61K31/335 , A61K31/35 , A61K31/352 , A61P37/08 , A61P43/00 , C07C229/14 , C07D311/80 , C07D311/82 , C07D313/12 , C07D313/14
CPC分类号： C07D313/14 , C07C229/14 , C07D311/82 , C07D313/12 , C07C2103/32
摘要： Tricyclic compounds represented by the following formula: ##STR1## wherein X represents --CH.dbd.CH--, --CH.sub.2 O--, or --O--;R.sup.1 represents a lower alkyl group,R.sup.2 represents a hydrogen atom or a lower alkyl group; andn represents an integer of from 1 to 5, pharmacologically acceptable salts thereof, and a method for preparing the same. The present compounds have anti-allergic and anti-histaminic activities and reduced side effects, and are useful as anti-allergic agents and anti-histaminic agents.
摘要翻译： PCT No.PCT / JP92 / 00365 Sec。 371日期：1993年10月1日 102（e）日期1993年10月1日PCT 1991年3月26日PCT公布。第WO92 / 17440号公报日期：10月15日，1992.由下式表示的三环化合物：其中X表示-CH = CH-，-CH 2 O-或-O-; R1表示低级烷基，R2表示氢原子或低级烷基; 和n表示1〜5的整数，其药理学上可接受的盐及其制备方法。本发明化合物具有抗过敏和抗组胺活性并减少副作用，并且可用作抗过敏剂和抗组胺剂。

2. 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。

3. 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.

4. 发明授权

US5095022A Piperidine derivatives and pharmaceutical compositions comprising the same 失效
标题翻译：哌啶衍生物和包含其的药物组合物
公开(公告)号：US5095022A
公开(公告)日：1992-03-10
申请号：US538085
申请日：1990-06-13
申请人： Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Hiroyuki Nishino , Jun Sakaguchi
发明人： Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Hiroyuki Nishino , Jun Sakaguchi
IPC分类号： C07D211/70 , C07D405/04
CPC分类号： C07D405/04 , C07D211/70
摘要： A piperidine derivative represented by the following general formula (I): ##STR1## wherein R represents a hydrogen atom or a lower alkyl group; X represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or --CH.sub.2 O--; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represented an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), a method for preparation of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).

5. 发明授权

US5153207A Piperidine derivative, method for preparation thereof, and a pharmaceutical composition comprising the same 失效
标题翻译：哌啶衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5153207A
公开(公告)日：1992-10-06
申请号：US520064
申请日：1990-05-03
申请人： Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Hiroyuki Nishino , Jun Sakaguchi
发明人： Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Hiroyuki Nishino , Jun Sakaguchi
IPC分类号： C07D211/46 , C07D211/54
CPC分类号： C07D211/54 , C07D211/46
摘要： A piperidine derivative represented by the following general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkoxy group; R.sub.3 represents a hydrogen atom or a lower alkyl group; X represents an oxygen atom or a sulfur atom; Y represents an alkylene group having 1 to 7 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represents an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).

6. 发明授权

US4912116A Propiophenone derivatives for treatment of pollakiuria (frequency urination) 失效
标题翻译：用于治疗尿频的苯丙酮衍生物（排尿）
公开(公告)号：US4912116A
公开(公告)日：1990-03-27
申请号：US136912
申请日：1987-12-22
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Kouji Morikawa , Toshie Yamauchi
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Kouji Morikawa , Toshie Yamauchi
IPC分类号： C07D295/10 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/445 , A61K31/535 , A61K31/54 , A61K31/55 , A61P13/02 , A61P15/00 , C07D307/79 , C07D317/58 , C07D405/06
CPC分类号： A61K31/535 , A61K31/40 , A61K31/445 , A61K31/55 , Y10S514/906
摘要： A method for the treatment of pollakiurea in a subject in need thereof, comprising the step of administering to said subject an effective antipollakiurea amount of a propiophenone of the formula (I) ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each independently represents hydrogen, halogen, lower alkyl- or halogeno-lower-alkyl, lower-alkoxy, or cycloalkyl having 3-8 carbon atoms, two of which R.sub.1, R.sub.2, and R.sub.3 groups may combine to form methylenedioxy or ethyleneoxy, R.sub.4 represents hydrogen or a lower-alkyl, and A represents pyrrolidinyl-, piperidinyl-, morpholinyl-, or azepinyl or a pharmaceutically-acceptable acid addition salt thereof, is disclosed.

7. 发明授权

US4525356A N-substituted flavone-8-carboxamides 失效
标题翻译： N-取代的黄酮-8-甲酰胺
公开(公告)号：US4525356A
公开(公告)日：1985-06-25
申请号：US546481
申请日：1983-10-28
申请人： Yasuo Itho , Hideo Kato , Nobuo Ogawa , Kagari Yamagishi , Eiichi Koshinaka , Kazuya Mitani
发明人： Yasuo Itho , Hideo Kato , Nobuo Ogawa , Kagari Yamagishi , Eiichi Koshinaka , Kazuya Mitani
IPC分类号： C07D311/30 , C07D405/12 , A61K31/35 , C07D405/10
CPC分类号： C07D405/12 , C07D311/30
摘要： Derivatives of N-substituted flavone-8-carboxamides represented by general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an ethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a halogen atom or a nitro group, R.sub.3 represents a hydrogen atom or a lower alkyl group, k represents 0, 1, 2, or 3, m represents 0 or 1; X and Y, which must be different, represent a hydrogen atom or methyl group. A represents an amino group having the formula ##STR2## wherein, R.sub.4 and R.sub.5, which may be the same or different, represent a lower alkyl group or a cyclic amino group together with the nitrogen atom and with or without an oxygen atom, R.sub.6 represents a lower alkyl group and n represents 2 or 3, are disclosed, as well as pharmaceutical compositions thereof and method of treating therewith.The N-substituted flavone-8-carboxamides derivatives are useful as agents for treatment of dysurea.
摘要翻译：由通式（I）表示的N-取代的黄酮-8-甲酰胺的衍生物其中R1表示氢原子，甲基或乙基，R2表示氢原子，低级烷基，低级烷氧基卤素原子或硝基，R3表示氢原子或低级烷基，k表示0,1,2或3，m表示0或1; X和Y必须不同，表示氢原子或甲基。 A表示具有式“IMAGE”的氨基，其中可以相同或不同的R 4和R 5与氮原子一起表示低级烷基或环状氨基，并且具有或不具有氧原子，R6表示低级烷基和n代表2或3，以及其药物组合物和其处理方法。 N-取代的黄酮-8-甲酰胺衍生物可用作治疗尿素的药剂。

8. 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.

9. 发明授权

US4638009A Derivatives of 3-pyrrolidinopropiophenone and a process for preparation thereof 失效
标题翻译： 3-吡咯烷基苯丙酮的衍生物及其制备方法
公开(公告)号：US4638009A
公开(公告)日：1987-01-20
申请号：US573862
申请日：1984-01-25
申请人： Yasuo Itho , Hideo Kato , Nobuo Ogawa , Kagari Yamagishi , Eiichi Koshinaka , Hiroyuki Nishino
发明人： Yasuo Itho , Hideo Kato , Nobuo Ogawa , Kagari Yamagishi , Eiichi Koshinaka , Hiroyuki Nishino
IPC分类号： C07D295/108 , A61K31/41 , C07D207/06
CPC分类号： C07D295/108
摘要： Certain 4'-alkyl-2-methyl-3-pyrrolidinopropiophenones, acid addition salts thereof, their method of preparation, pharmaceutical compositions embodying the same, and a method of muscle relaxation therewith, are disclosed.
摘要翻译：公开了某些4'-烷基-2-甲基-3-吡咯烷基苯丙酮，其酸加成盐，其制备方法，含有其的药物组合物及其与肌肉松弛的方法。

10. 发明授权

US4612329A Pharmaceutical alpha-aminoalkyl-alpha-alkylphenylacetonitriles 失效
标题翻译：药物α-氨基烷基-α-烷基苯基乙腈
公开(公告)号：US4612329A
公开(公告)日：1986-09-16
申请号：US786742
申请日：1985-10-11
申请人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Sakae Kurata , Hiroyuki Nishino , Toshihiko Yoshida
发明人： Yasuo Itoh , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Sakae Kurata , Hiroyuki Nishino , Toshihiko Yoshida
IPC分类号： A61K31/275 , A61K31/445 , C07C20060101 , C07C255/58 , C07D20060101 , C07D211/08 , C07D295/08 , C07C121/78
CPC分类号： C07C255/00
摘要： Novel alpha-aminoalkyl-alpha-alkylphenylacetonitrile derivatives useful for treatment of cartino vaso diseases, a peripheral circulatory insufficiency and cerebral circulation failure are disclosed.
摘要翻译：公开了用于治疗纸浆血管疾病，外周循环功能不全和脑循环衰竭的新型α-氨基烷基-α-烷基苯基乙腈衍生物。

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