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11. 发明授权

US4845083A Method of inhibiting mammalian leukotriene biosynthesis 失效
标题翻译：抑制哺乳动物白三烯生物合成的方法
公开(公告)号：US4845083A
公开(公告)日：1989-07-04
申请号：US1946
申请日：1987-01-09
申请人： Rejean Fortin , Cheuk K. Lau , Yvan Guindon , Joshua Rokach , Christiane Yoakim
发明人： Rejean Fortin , Cheuk K. Lau , Yvan Guindon , Joshua Rokach , Christiane Yoakim
IPC分类号： C07D265/38 , C07D279/20 , C07D279/22 , C07D279/30 , C07D279/34 , C07D293/10
CPC分类号： C07D279/34 , C07D265/38 , C07D279/20 , C07D279/22 , C07D279/30 , C07D293/10
摘要： Phenothiazine derivatives and analogs thereof having the Formula I are useful as inhibitors of the biosynthesis of mammalian leukotrienes. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation, and are useful as cytoprotective agents. ##STR1##
摘要翻译：具有式I的吩噻嗪衍生物及其类似物可用作哺乳动物白三烯生物合成的抑制剂。因此，这些化合物是用于治疗过敏性疾病，哮喘，心血管疾病和炎症的有用的治疗剂，并且可用作细胞保护剂。我

12. 发明授权

US4820867A Phenoxypropoxy halophenylacetic acids as leukotriene antagonists 失效
标题翻译：苯氧基丙氧基卤代苯乙酸作为白三烯拮抗剂
公开(公告)号：US4820867A
公开(公告)日：1989-04-11
申请号：US855051
申请日：1986-04-22
申请人： Patrice Belanger , Rejean Fortin , Yvan Guindon , Christiane Yoakim , Joshua Rokach
发明人： Patrice Belanger , Rejean Fortin , Yvan Guindon , Christiane Yoakim , Joshua Rokach
IPC分类号： C07C45/71 , C07C49/84 , C07C49/86 , C07C59/90 , C07C65/01 , C07D257/04 , C07D285/10
CPC分类号： C07D285/10 , C07C255/00 , C07C45/71 , C07C49/84 , C07C49/86 , C07C59/90 , C07D257/04
摘要： Compounds of the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.
摘要翻译：下式的化合物是C4，D4和E4的白细胞三烯的拮抗剂，其是过敏反应的缓慢反应物质。这些化合物可用作抗哮喘，抗过敏和抗炎剂。

13. 发明授权

US4666907A Phenothiazine and derivatives and analogs and use as leukotriene biosynthesis inhibitors 失效
标题翻译：吩噻嗪及其衍生物和类似物，并用作白三烯生物合成抑制剂
公开(公告)号：US4666907A
公开(公告)日：1987-05-19
申请号：US654991
申请日：1986-09-26
申请人： Rejean Fortin , Cheuk K. Lau , Yvan Guindon , Joshua Rokach , Christiane Yoakim
发明人： Rejean Fortin , Cheuk K. Lau , Yvan Guindon , Joshua Rokach , Christiane Yoakim
IPC分类号： C07D265/38 , C07D279/20 , C07D279/22 , C07D279/30 , C07D279/34 , C07D293/10 , A61K31/535 , A61K31/54
CPC分类号： C07D265/38 , C07D279/20 , C07D279/22 , C07D279/30 , C07D279/34 , C07D293/10
摘要： Phenothiazine derivatives and analogs thereof having the Formula I are useful as inhibitors of the biosynthesis of mammalian leukotrienes. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation, and are useful as cytoprotective agents. ##STR1##
摘要翻译：具有式I的吩噻嗪衍生物及其类似物可用作哺乳动物白三烯生物合成的抑制剂。因此，这些化合物是用于治疗过敏性疾病，哮喘，心血管疾病和炎症的有用的治疗剂，并且可用作细胞保护剂。我

14. 发明授权

US5126326A Enzyme inhibiting peptide derivatives 失效
标题翻译：酶抑制肽衍生物
公开(公告)号：US5126326A
公开(公告)日：1992-06-30
申请号：US361895
申请日：1989-06-06
申请人： Paul C. Anderson , Yvan Guindon , Christiane Yoakim
发明人： Paul C. Anderson , Yvan Guindon , Christiane Yoakim
IPC分类号： C12N9/99 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0227
摘要： Disclosed herein are peptide derivatives which inhibit the activities of human immunodeficiency virus (HIV) protease and renin. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is a derived amino acid based on an O.sup.4 -(carboxymethyl)-tyrosyl residue, R.sup.2 and are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CHR.sup.18 --C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or one and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives are useful as agents for combatting HIV infections and for treating renin-associated hypertension and congestive heart failure.
摘要翻译：本文公开了抑制人免疫缺陷病毒（HIV）蛋白酶和肾素的活性的肽衍生物。肽衍生物可以由通式R 1 -R 2 -Y-R 3 -R 4表示，其中R 1是基于O 4 - （羧甲基） - 酪氨酰残基R2的衍生氨基酸，并且是氨基酸或类似氨基酸残基（R3可以任选地不存在），Y是非肽连接单元，例如辛基，R4是[-NR17CHR18-C（O）] pZ，其中R17是氢或低级烷基，R18是氨基酸或类似的氨基酸侧链，p是0或1，Z是末端基团（例如羟基或氨基），或R 4是-NR 17 CR 18（R 21）CH 2 OH，其中R 17和R 18如上所述，R 21是氢，低级烷基或羟基（低级）烷基。该衍生物可用作抗艾滋病毒感染和治疗肾素相关性高血压和充血性心力衰竭的药剂。

15. 发明授权

US5081145A Indole-2-alkanoic acids compositions of and anti allergic use thereof 失效
标题翻译：吲哚-2-链烷酸组合物及其过敏用途
公开(公告)号：US5081145A
公开(公告)日：1992-01-14
申请号：US473551
申请日：1990-02-01
申请人： Yvan Guindon , John W. Gillard , Christiane Yoakim , Thomas R. Jones , Rejean Fortin
发明人： Yvan Guindon , John W. Gillard , Christiane Yoakim , Thomas R. Jones , Rejean Fortin
IPC分类号： C07D209/22
CPC分类号： C07D209/22
摘要： Indole-2-alkanoic acids are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, inflammation, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion and dismenorrhea and as cytoprotective agents.
摘要翻译：吲哚-2-链烷酸被公开。化合物作为前列腺素和血栓素拮抗剂，可用于治疗哮喘，炎症，腹泻，高血压，心绞痛，血小板聚集，脑痉挛，早产，自然流产和死亡以及细胞保护剂。

16. 发明授权

US4940719A Tetrahydrocarbazole esters, pharmaceutical compositions and use 失效
标题翻译：四氢咔唑酯，药物组合物和用途
公开(公告)号：US4940719A
公开(公告)日：1990-07-10
申请号：US101611
申请日：1987-09-28
申请人： John W. Gillard , Christiane Yoakim , Yvan Guindon , Yves Girard
发明人： John W. Gillard , Christiane Yoakim , Yvan Guindon , Yves Girard
IPC分类号： A61K31/40 , A61K31/403 , A61K45/06 , A61P3/00 , A61P43/00 , C07D209/86 , C07D209/88 , C07D403/12 , C07D405/12
CPC分类号： C07D403/12 , C07D209/86 , C07D209/88 , C07D405/12
摘要： Tetrahydrocarbazole esters are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion and dysmenorrhea and nephrotoxicity caused by cyclosporin A and as cytoprotective agents.
摘要翻译：公开了四氢咔唑酯。化合物作为前列腺素和血栓素拮抗剂，可用于治疗由环孢菌素A和细胞保护剂引起的哮喘，腹泻，高血压，心绞痛，血小板聚集，脑痉挛，早产，自然流产和痛经和肾毒性。

17. 发明授权

US5135940A Leukotriene antagonists 失效
标题翻译：白三烯拮抗剂
公开(公告)号：US5135940A
公开(公告)日：1992-08-04
申请号：US672520
申请日：1991-03-20
申请人： Patrice C. Belanger , Joshua Rokach , Rejean Fortin , Christiane Yoakim , Yvan Guindon
发明人： Patrice C. Belanger , Joshua Rokach , Rejean Fortin , Christiane Yoakim , Yvan Guindon
IPC分类号： A61K31/19 , C07C45/71 , C07C59/90 , C07D207/26 , C07D207/32 , C07D207/33 , C07D233/74 , C07D257/04 , C07D307/58 , C07D317/34
CPC分类号： C07D207/26 , C07C317/00 , C07C323/00 , C07C45/71 , C07C59/90 , C07D207/33 , C07D233/74 , C07D257/04 , C07D307/58 , C07D317/34
摘要： Compounds of the Formulae: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.
摘要翻译：式XI的化合物是XI，D4和E4的白三烯，过敏反应缓慢反应物质的拮抗剂。这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。

18. 发明授权

US5021447A Tetrahydrocarbazole 1-alkanoic acids and pharmaecutical compositions 失效
标题翻译：四氢咔唑1-链烷酸和药物组合物
公开(公告)号：US5021447A
公开(公告)日：1991-06-04
申请号：US268824
申请日：1988-11-07
申请人： Yvan Guindon , Christiane Yoakim , John W. Gillard , Yves Girard
发明人： Yvan Guindon , Christiane Yoakim , John W. Gillard , Yves Girard
IPC分类号： C07D209/86 , C07D209/88 , C07D403/06
CPC分类号： C07D403/06 , C07D209/86 , C07D209/88
摘要： Tetrahydrocarbazole 1-alkanoic acids are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion and dysmenorrhea and as cytoprotective agents.
摘要翻译：公开了四氢咔唑1-链烷酸。化合物作为前列腺素和血栓素拮抗剂起作用，可用于治疗哮喘，腹泻，高血压，心绞痛，血小板聚集，脑痉挛，早产，自然流产和痛经以及细胞保护剂。

19. 发明授权

US4808608A Tetrahydrocarbazole 1-alkanoic acids, pharmaceutical compositions and use 失效
标题翻译：四氢咔唑1-链烷酸，药物组合物和用途
公开(公告)号：US4808608A
公开(公告)日：1989-02-28
申请号：US76424
申请日：1987-07-21
申请人： Yvan Guindon , Christiane Yoakim , John W. Gillard , Yves Girard
发明人： Yvan Guindon , Christiane Yoakim , John W. Gillard , Yves Girard
IPC分类号： A61K31/40 , A61K31/403 , A61P3/00 , A61P7/02 , A61P11/00 , A61P25/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D209/86 , C07D209/88 , C07D403/06
CPC分类号： C07D403/06 , C07D209/86 , C07D209/88
摘要： Tetrahydrocarbazole 1-alkanoic acids are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, diarrhea, hypertension, angina, platlet aggregation, cerebral spasm, premature labor, spontaneous abortion and dysmenorrhea and as cytoprotective agents.
摘要翻译：公开了四氢咔唑1-链烷酸。这些化合物作为前列腺素和血栓素拮抗剂，可用于治疗哮喘，腹泻，高血压，心绞痛，血小板聚集，脑痉挛，早产，自然流产和痛经以及细胞保护剂。

20. 发明授权

US4667032A Phenothiazone derivatives and analogs 失效
公开(公告)号：US4667032A
公开(公告)日：1987-05-19
申请号：US786257
申请日：1985-10-10
申请人： Cheuk K. Lau , Christiane Yoakim , Joshua Rokach , Rejean Fortin , Yvan Guindon
发明人： Cheuk K. Lau , Christiane Yoakim , Joshua Rokach , Rejean Fortin , Yvan Guindon
IPC分类号： A61K31/495 , A61K31/535 , A61K31/54 , C07C46/06 , C07D241/46 , C07D265/34 , C07D265/38 , C07D279/18 , C07D279/34 , C07D279/36 , C07D293/10
CPC分类号： C07D293/10 , A61K31/495 , A61K31/535 , A61K31/54 , C07C46/06 , C07D241/46 , C07D265/34 , C07D265/38 , C07D279/18 , C07D279/34 , C07D279/36
摘要： Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.

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