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21. 发明授权

US4761425A Leukotriene antagonists 失效
标题翻译：白三烯拮抗剂
公开(公告)号：US4761425A
公开(公告)日：1988-08-02
申请号：US685807
申请日：1984-12-24
申请人： Yves Girard , Joshua Rokach
发明人： Yves Girard , Joshua Rokach
IPC分类号： A61K31/335 , C07C33/02 , C07C45/30 , C07C47/21 , C07D215/54 , C07D303/42 , C07D311/16 , C07D311/22 , C07D311/24 , C07F9/40 , C07K5/06 , A61K31/35
CPC分类号： C07K5/0606 , A61K31/335 , C07C323/00 , C07C33/02 , C07C45/305 , C07C47/21 , C07D215/54 , C07D303/42 , C07D311/16 , C07D311/22 , C07D311/24 , C07F9/4015
摘要： Compounds having 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, anti-inflammatory agents, and cytoprotective agents.
摘要翻译：具有下式的化合物：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，抗炎药和细胞保护剂。

22. 发明授权

US4717736A Antagonists of slow reacting substances of anaphylaxis 失效
标题翻译：慢性反应物质的过敏反应的拮抗剂
公开(公告)号：US4717736A
公开(公告)日：1988-01-05
申请号：US673649
申请日：1984-11-21
申请人： Joshua Rokach , Robert N. Young
发明人： Joshua Rokach , Robert N. Young
IPC分类号： A61K31/18 , A61K31/215 , A61K31/195 , A61K31/325 , A61K31/40 , C07C103/84 , C07D207/08
CPC分类号： A61K31/18
摘要： Compounds having 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, anti-inflammatory agents and cytoprotective agents.
摘要翻译：具有下式的化合物： + TR 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，抗炎药和细胞保护剂。

23. 发明授权

US4424355A Resolution of substituted dibenzo�b,f!thiepin-3-carboxylic acid-5-oxides with brucine or ephedrine 失效
标题翻译：取代二苯并[b，f]硫杂-3-羧酸-5-氧化物与布鲁丁或麻黄碱的拆分
公开(公告)号：US4424355A
公开(公告)日：1984-01-03
申请号：US351708
申请日：1982-02-24
申请人： Patrice C. Belanger , Haydn W. R. Williams , Joshua Rokach
发明人： Patrice C. Belanger , Haydn W. R. Williams , Joshua Rokach
IPC分类号： C07D337/14 , C07D405/14
CPC分类号： C07D337/14 , Y02P20/582
摘要： The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo�b,f!thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo�b,f!thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo�b,f!thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo�b,f!thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with brucine or ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer. The compounds obtained in high yield by this process are highly active prostaglandin antagonists which are useful in treating a variety of conditions such as allergic asthma.
摘要翻译：本发明涉及一种制备具有结构式“IMAGE”II的（ - ）7或8-氟二苯并[b，f]硫杂-3-羧酸-5-氧化物的高活性光学异构体的改进方法，其中氟取代基取代7或8位的氢。由式II表示的两种活性异构体是S（ - ）7-氟二苯并[b，f]硫杂-3-羧酸-5-氧化物和R（ - ）8-氟二苯并[b，f]硫杂-3-羧酸 -5-氧化物。特别关注外消旋的7或8氟二苯并[b，f]硫杂环庚烷-3-羧酸-5-氧化物的拆分，首先通过与酪氨酸或麻黄碱的盐形成形成和分离所述外消旋羧酸的非对映异构体，随后结晶并再生所需的（ - ）异构体并通过再生异构体的外消旋再循环（+）异构体。通过该方法以高产率获得的化合物是可用于治疗多种病症如过敏性哮喘的高活性前列腺素拮抗剂。

24. 发明授权

US4334077A Stereospecific sulfoxidation of dibenzo thiepins 失效
标题翻译：二苯并噻吩的立体特异性亚砜化反应
公开(公告)号：US4334077A
公开(公告)日：1982-06-08
申请号：US229223
申请日：1981-01-28
申请人： Patrice C. Belanger , Joshua Rokach , Robert N. Young , John Scheigetz
发明人： Patrice C. Belanger , Joshua Rokach , Robert N. Young , John Scheigetz
IPC分类号： C07D337/14
CPC分类号： C07D337/14
摘要： The present invention relates to a process for the preparation of an enantiomer of 7 or 8-fluoro-dibenzo[b,f]thiepin-3-carboxylic acid having a negative rotation and prostaglandin antagonist activity. The process involves preparation and separation of novel diastereoisomeric esters of 10-hydroxy-7 or 8 fluro-dibenzothiepin-3 carboxylic acid ester followed by stereospecific sulfoxidation of the selected diastereoisomer to produce the corresponding novel sulfoxide having a preponderance of the desired configuration of the sulfoxide entity followed by treatment of the product with a strong base to produce directly the desired (-)7 or 8 fluoro-dibenzo[b,f]thiepin-3 carboxylic acid 5-oxide having the structural formula shown below: ##STR1##
摘要翻译：本发明涉及制备具有负旋转和前列腺素拮抗剂活性的7或8-氟 - 二苯并[b，f]硫杂-3-羧酸的对映异构体的方法。该方法包括制备和分离新的非对映异构体的10-羟基-7或8-氟二苯并硫代-3-羧酸酯的酯，然后立即特异性磺化氧化所选的非对映异构体以产生相应的具有优选的亚砜所需构型的亚砜实体，然后用强碱处理产物，直接生产具有以下结构式的所需的（ - ）7或8氟二苯并[b，f]硫杂_β-羧酸5-氧化物：

25. 发明授权

US4094986A 2-R-Substituted-1,2,5-thiadiazole-3-one antimicrobials 失效
标题翻译： 2-R-取代的1,2,5-噻二唑-3-酮抗微生物
公开(公告)号：US4094986A
公开(公告)日：1978-06-13
申请号：US813015
申请日：1977-07-05
申请人： Joshua Rokach , Grant W. Reader
发明人： Joshua Rokach , Grant W. Reader
IPC分类号： A01N43/82 , C07D285/10 , A61K31/425
CPC分类号： C07D285/10 , A01N43/82
摘要： 2-R-substituted-1,2,5-thiadiazole-3-ones have broad spectrum antibacterial and antifungal activity. They are especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.

26. 发明授权

US08809382B2 5-oxo-ETE receptor antagonist compounds 有权
标题翻译： 5-氧代-ETE受体拮抗剂化合物
公开(公告)号：US08809382B2
公开(公告)日：2014-08-19
申请号：US13318697
申请日：2010-05-04
申请人： William S. Powell , Joshua Rokach
发明人： William S. Powell , Joshua Rokach
IPC分类号： A61K31/405 , C07D209/12 , C07D403/06
CPC分类号： C07D209/18 , C07C59/84 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/24 , C07D215/12 , C07D235/08 , C07D307/79 , C07D403/06
摘要： The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.
摘要翻译：本发明涉及作为5-氧代-ETE受体（如OXE受体）的拮抗剂的新颖的药学上有用的化合物。这些化合物可用作用于组织嗜酸性粒细胞增多症，特别是包括呼吸系统疾病在内的炎性疾病的疾病的治疗和/或预防剂。本发明还涉及药物组合物，使用这些化合物和组合物作为药物，以及治疗方法。

27. 发明授权

US5087638A Benzofuran derivatives 失效
标题翻译：苯并呋喃衍生物
公开(公告)号：US5087638A
公开(公告)日：1992-02-11
申请号：US372501
申请日：1989-06-28
申请人： Patrice C. Belanger , John Scheigetz , Joshua Rokach
发明人： Patrice C. Belanger , John Scheigetz , Joshua Rokach
IPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D307/86 , C07D333/54 , C07D333/56 , C07D405/06 , C07D409/06 , C07D417/06 , C07D493/04 , C07F9/655 , C08G18/61
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D307/86 , C07D333/54 , C07D333/56 , C07D405/06 , C07D409/06 , C07D417/06 , C07D493/04 , C07F9/65517 , C08G18/615 , Y10S514/826 , Y10S514/886
摘要： Benzofuran derivatives, 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, inflammation. The compounds are also useful as analgesics and as cytoprotective agents.
摘要翻译：公开了苯并呋喃衍生物，药物组合物和治疗方法。这些化合物可用作哺乳动物白细胞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，炎症的有用的治疗剂。该化合物也可用作止痛剂和细胞保护剂。

28. 发明授权

US4954638A Leukotriene by amides and hydrazides 失效
标题翻译：白三烯通过酰胺和酰肼
公开(公告)号：US4954638A
公开(公告)日：1990-09-04
申请号：US227038
申请日：1988-08-01
申请人： Robert N. Young , Joshua Rokach , Edward C. Hayes
发明人： Robert N. Young , Joshua Rokach , Edward C. Hayes
IPC分类号： A61K38/00 , A61K47/48 , C07D207/40 , C07D207/416 , C07D207/44 , C07D207/456 , C07D309/30 , C07K1/107 , C07K5/06 , C07K14/00 , C07K16/18 , C07K17/06 , G01N33/531 , G01N33/60 , G01N33/88
CPC分类号： A61K47/48238 , A61K47/48284 , C07C243/00 , C07D207/416 , C07D207/456 , C07D309/30 , C07K1/1077 , C07K14/00 , C07K16/18 , C07K17/06 , C07K5/0606 , G01N33/531 , G01N33/60 , G01N33/88 , A61K38/00
摘要： Leukotrienes may be conjugated with various proteins such as Bovine Serum Albumin (BSA) and Hemocyanin from Giant Keyhole Limpets (KLH) using 1,5-difluoro-2,4-dinitrobenzene or 6-N-maleimidohexanoic acid chloride as coupling agents.These conjugates are useful as reagents in a newly developed immunoassay for leukotrienes, as well as having potential utility as chemical immunotherapeutic agents in the treatment of various allergic and chronic inflammatory diseases of the skin, lung, and airways, including asthma, allergic rhinitis, rheumatoid arthritis, and skin diseases such as psoriasis and eczema.
摘要翻译：白细胞三烯可以使用1,5-二氟-2,4-二硝基苯或6-N-马来酰亚胺己酸氯化物作为偶联剂，与各种蛋白质例如牛血清白蛋白（BSA）和来自Giant Keyhole Limpets（KLH）的血蓝蛋白缀合。这些缀合物可用作新开发的白三烯免疫测定中的试剂，以及作为化学免疫治疗剂用于治疗皮肤，肺和气道各种过敏性和慢性炎性疾病（包括哮喘，过敏性鼻炎，类风湿病）的潜在用途关节炎和皮肤疾病如牛皮癣和湿疹。

29. 发明授权

US4871756A Leukotriene antagonists 失效
标题翻译：白三烯拮抗剂
公开(公告)号：US4871756A
公开(公告)日：1989-10-03
申请号：US15823
申请日：1987-02-17
申请人： John Gillard , Joshua Rokach , Patrice C. Belanger
发明人： John Gillard , Joshua Rokach , Patrice C. Belanger
IPC分类号： A61K31/215
CPC分类号： C07C323/00
摘要： Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4, E.sub.4 and the slow reacting substance of anaphylaxis.As such, these compounds will be useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
摘要翻译：具有下式的化合物：I是C4，D4，E4的白三烯和过敏反应缓慢反应物质的拮抗剂。因此，这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。

30. 发明授权

US4617407A Leukotriene antagonists 失效
公开(公告)号：US4617407A
公开(公告)日：1986-10-14
申请号：US645595
申请日：1984-08-30
申请人： Robert N. Young , Joshua Rokach
发明人： Robert N. Young , Joshua Rokach
IPC分类号： C07D307/79 , C07D307/80 , C07D311/58 , C07D307/88 , C07D311/04
CPC分类号： C07D307/79 , C07D307/80 , C07D311/58
摘要： Compounds having 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, anti-inflammatory and cytoprotective agents.

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