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公开(公告)号：US4929639A
公开(公告)日：1990-05-29
申请号：US208665
申请日：1988-06-20
申请人： Hiroyuki Setoi , Akio Kuroda , Hirokazu Tanaka , Hideo Hirai , Hiroshi Marusawa , Masashi Hashimoto
发明人： Hiroyuki Setoi , Akio Kuroda , Hirokazu Tanaka , Hideo Hirai , Hiroshi Marusawa , Masashi Hashimoto
IPC分类号： A61K31/357 , A61P7/02 , C07D309/06 , C07D319/06 , C07D405/12 , C07D409/12
CPC分类号： C07D405/12 , C07D309/06 , C07D319/06 , C07D409/12
摘要： The invention relates to treatment of diseases caused by thromboxane A.sub.2 comprising administering a compound ##STR1## wherein R.sup.1 is hydrogen or lower alkyl,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl andR.sup.3 is --CH.dbd.N--R.sup.4 in which R.sup.4 is arylureido or arylthioureido andX is --O--,or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US4916152A
公开(公告)日：1990-04-10
申请号：US187240
申请日：1988-04-28
申请人： Hiroyuki Setoi , Hideo Hirai , Hiroshi Marusawa , Akio Kuroda , Hirokazu Tanaka , Masashi Hashimoto
发明人： Hiroyuki Setoi , Hideo Hirai , Hiroshi Marusawa , Akio Kuroda , Hirokazu Tanaka , Masashi Hashimoto
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/66 , A61P7/00 , A61P7/02 , A61P11/00 , A61P13/02 , A61P15/00 , C07D207/12 , C07D207/14 , C07D207/16 , C07D409/12 , C07F9/572
CPC分类号： C07D207/16 , C07D207/12 , C07D207/14
摘要： The invention relates to novel compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkoxycarbonyl, phenylsulfonyl, phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, nitro, lower alkoxy, mono (or di or tri)halo(lower)alkyl and lower alkyl, phenylcarbamoyl, lower alkylsulfonyl, benzoyl or thienylsulfonyl;R.sup.2 is phenylsulfonyl or phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, lower alkyl, lower alkoxy and mono(or di or tri)halo(lower)alkyl,R.sup.3 is carboxy(lower)alkyl, lower alkyl substituted with carboxy and 1 to 3 halogen atom(s), esterified carboxy(lower)alkyl, carbamoyl(lower)alkyl, lower alkylsulfonylcarbamoyl(lower)alkyl, phenylsulfonylcarbamoyl(lower)alkyl, carboxyphenyl, esterified carboxyphenyl, carboxy, esterified carboxy, hydroxy(lower)alkyl, sulfino(lower)alkyl, phosphono(lower)alkyl, di(lower)alkoxyphosphoryl(lower)alkyl or halo(lower)alkyl,R.sup.7 is hydrogen or lower alkyl, andA is ##STR2## in which R.sup.8 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof, useful as therapeutic agents for thrombosis, asthma and nephritis.
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公开(公告)号：US5210092A
公开(公告)日：1993-05-11
申请号：US748954
申请日：1991-08-23
申请人： Teruo Oku , Hiroyuki Setoi , Hiroshi Kayakiri , Shigeki Satoh , Takayuki Inoue , Yuki Saitoh , Akio Kuroda , Hirokazu Tanaka
发明人： Teruo Oku , Hiroyuki Setoi , Hiroshi Kayakiri , Shigeki Satoh , Takayuki Inoue , Yuki Saitoh , Akio Kuroda , Hirokazu Tanaka
IPC分类号： A61K31/415 , A61K31/435 , A61K31/52 , A61P9/00 , A61P9/12 , A61P43/00 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D495/04
CPC分类号： C07D403/14 , C07D471/04 , C07D495/04 , Y02P20/55
摘要： The invention concerns compounds of the formula ##STR1## represents a condensed or uncondensed imidazolyl ring and the rest of the variables are defined in the specification. They are angiotensin II antagonists useful for treating hypertension, etc.
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公开(公告)号：US5215994A
公开(公告)日：1993-06-01
申请号：US758688
申请日：1991-09-12
申请人： Teruo Oku , Hiroyuki Setoi , Hiroshi Kayakiri , Shigeki Satoh , Takayuji Inoue , Yuki Saitoh , Akio Kuroda , Hirokazu Tanaka
发明人： Teruo Oku , Hiroyuki Setoi , Hiroshi Kayakiri , Shigeki Satoh , Takayuji Inoue , Yuki Saitoh , Akio Kuroda , Hirokazu Tanaka
IPC分类号： C07D403/14 , C07D471/04 , C07D495/04
CPC分类号： C07D403/14 , C07D471/04 , C07D495/04
摘要： The invention relates to compounds of the formula ##STR1## wherein ##STR2## represents a condensed or uncondensed imidazolyl ring and the rest of the variables are as defined in the specification. They are angiotensin II antagonists useful for treating hypertension, etc..
摘要翻译： 本发明涉及式“IMAGE”的化合物，其中“IMAGE”表示缩合或未缩合的咪唑基环，其余变量如说明书中所定义。 它们是可用于治疗高血压等的血管紧张素II拮抗剂。
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公开(公告)号：US5354759A
公开(公告)日：1994-10-11
申请号：US8646
申请日：1993-01-25
申请人： Teruo Oku , Hiroyuki Setoi , Hiroshi Kayakiri , Shigeki Satoh , Takayuki Inoue , Yuki Sawada , Akio Kuroda , Hirokazu Tanaka
发明人： Teruo Oku , Hiroyuki Setoi , Hiroshi Kayakiri , Shigeki Satoh , Takayuki Inoue , Yuki Sawada , Akio Kuroda , Hirokazu Tanaka
IPC分类号： A61K31/435 , C07D471/04
CPC分类号： A61K31/435 , C07D471/04
摘要： This invention related to compounds of the formula ##STR1## wherein the radicals are as defined in the claims. The compounds are angiotensin II antagonists useful in treating hypertension, etc.
摘要翻译： 本发明涉及式IMA的化合物，其中基团如权利要求中所定义。 这些化合物是可用于治疗高血压等的血管紧张素II拮抗剂
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公开(公告)号：US5514701A
公开(公告)日：1996-05-07
申请号：US95350
申请日：1993-07-23
IPC分类号： C07D207/14 , C07D207/32 , C07D207/335 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D521/00 , A61K31/40
CPC分类号： C07D207/335 , C07D207/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , Y10S514/826
摘要： This invention relates to pyrrolidine derivatives and pharmaceutically acceptable salts, their pharmaceutical compositions, and methods of use as thromboxane A.sub.2 antagonists and/or thromboxane A.sub.2 synthetase inhibitors in the treatment of thrombotic diseases, asthma or nephritis, e.g. of the formula: ##STR1## wherein R.sup.1 is thienyl(lower)alkyl, furyl(lower)alkyl or pyrrolyl(lower)alkyl.
摘要翻译： 本发明涉及吡咯烷衍生物及其药学上可接受的盐，其药物组合物，以及作为血栓素A2拮抗剂和/或血栓素A2合成酶抑制剂用于治疗血栓性疾病，哮喘或肾炎的方法。 （低级）烷基或吡咯基（低级）烷基。
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公开(公告)号：US5130323A
公开(公告)日：1992-07-14
申请号：US421399
申请日：1989-10-13
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61P1/04 , A61P9/00 , A61P9/10 , A61P29/00 , A61P37/08 , A61P43/00 , C07D207/14 , C07D207/32 , C07D207/335 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D521/00
CPC分类号： C07D207/335 , C07D207/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The invention relates to pyrrolidine derivatives having thromboxane A.sub.2 antagonism and TXA.sub.2 synthetase-inhibitory activity, of the formula ##STR1## wherein R.sup.1 is pyridyl(lower)alkyl, R.sup.2 is an acyl group selected from the group consisting of lower alkanoyl, lower alkoxycarbonyl, lower alkylsulfonyl, phenylsulfonyl, benzoyl, phenyl(lower)alkanoyl, cyclo(lower)alkyl(lower)alkanoyl, phenyl(lower)alkoxycarbonyl and phenylcarbamoyl, each of which may have 1 to 3 substituent(s) selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro and mono(or di or tri)halo(lower)alkyl, andR.sup.3 is carboxy(lower)alkyl, protected carboxy(lower)alkyl, carboxyphenyl or protected carboxyphenyl,or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US5264453A
公开(公告)日：1993-11-23
申请号：US843196
申请日：1992-02-28
IPC分类号： C07D207/14 , C07D207/32 , C07D207/335 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D521/00 , C07D207/10 , A61K31/40
CPC分类号： C07D207/335 , C07D207/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , Y10S514/826
摘要： This invention relates to pyrrolidine derivatives and pharmaceutically acceptable salts thereof of the structure ##STR1## where R.sup.1, R.sup.2, and R.sup.3 are as defined herein. These compounds are for pharmaceutical use in treating thrombotic diseases, asthma or nephritis.
摘要翻译： 本发明涉及其中R1，R2和R3如本文所定义的结构“IMAGE”的吡咯烷衍生物及其药学上可接受的盐。 这些化合物用于治疗血栓性疾病，哮喘或肾炎的药物。
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公开(公告)号：US4743614A
公开(公告)日：1988-05-10
申请号：US859587
申请日：1986-03-04
IPC分类号： A61K38/00 , C07D207/20 , C07D233/54 , C07K5/072 , C12P13/00 , A61K31/165 , A61K31/195 , A61K31/405 , A61K31/415
CPC分类号： C07D233/64 , C07D207/20 , C07K5/06113 , C12P13/005 , C12P13/02 , C12P13/04 , C12R1/645 , A61K38/00
摘要： Novel compounds of the following formula have restorative pharmacological activities in immuno-deficient hosts, ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is hydrogen, carboxy or a protected carboxy group,R.sup.3 is hydrogen, carboxy or a protected carboxy group,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carbamoyl(lower)alkyl or protected carbamoyl(lower)alkyl,R.sup.5 is hydrogen or lower alkyl, andR.sup.6 is hydrogen, hydroxyphenyl(lower)alkyl, imidazolyl(lower)alkyl or indolyl(lower)alkyl.
摘要翻译： 下式的新化合物在免疫缺陷型宿主中具有恢复性药理学活性，其中R1是氨基或被保护的氨基，R2是氢，羧基或被保护的羧基，R3是氢，羧基或被保护的羧基 ，R4是低级烷基，氨基（低级）烷基，被保护的氨基（低级）烷基，氨基甲酰基（低级）烷基或被保护的氨基甲酰基（低级）烷基，R5是氢或低级烷基，R6是氢，羟基苯基（低级）烷基， 咪唑基（低级）烷基或吲哚基（低级）烷基。
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公开(公告)号：US5521170A
公开(公告)日：1996-05-28
申请号：US220695
申请日：1994-03-31
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61K31/495 , A61K31/55 , A61K31/551 , A61P1/16 , A61P3/08 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D209/08 , C07D209/34 , C07D215/08 , C07D223/16 , C07D223/20 , C07D241/40 , C07D241/44 , C07D243/04 , C07D243/12 , C07D243/14 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D471/04 , C07D241/36 , C07D245/06
CPC分类号： C07D223/16 , C07D209/08 , C07D215/08 , C07D223/20 , C07D241/44 , C07D243/04 , C07D243/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D471/04
摘要： Compounds having the structure below ##STR1## and pharmaceutically acceptable salts thereof exhibit vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in the liver, activity for inhibiting growth of mesagium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, and are useful in treating or preventing hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic or circulation disorder, oxytocin related diseases and the like.
摘要翻译： 具有以下结构的化合物及其药学上可接受的盐显示出加压素拮抗活性，血管舒张活性，降血压活性，抑制肝中糖释放的活性，抑制中期细胞生长的活性，水利尿活性，血小板凝集抑制活性， 催产素拮抗活性等，可用于治疗或预防高血压，心力衰竭，肾功能不全，水肿，腹水，血管加压素副作用综合征，肝硬化，低钠血症，低钾血症，糖尿病或循环障碍，催产素相关疾病等。
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