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1. 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。

2. 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：

3. 发明授权

US4863958A Benzofuran derivatives useful as inhibitors of mammalian leukotriene biosynthesis 失效
标题翻译：苯并呋喃衍生物可用作哺乳动物白细胞三烯生物合成的抑制剂
公开(公告)号：US4863958A
公开(公告)日：1989-09-05
申请号：US183877
申请日：1988-04-20
申请人： Patrice C. Belanger , John Scheigetz , Joshua Rokach
发明人： Patrice C. Belanger , John Scheigetz , Joshua Rokach
IPC分类号： C07D333/54 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/41 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P1/04 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/86 , C07D333/56 , C07D405/06 , C07D407/06 , C07D409/06 , C07D417/06 , C07D493/04 , C07F9/655
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
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 ar 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。化合物ar也可用作止痛剂和作为细胞保护剂。

4. 发明授权

US4728735A 10,11-dihydro-dibenzo-[b,f][1,4]-thiazepin derivatives 失效
标题翻译： 10,11-二氢 - 二苯并[b，f] [1,4] - 噻嗪衍生物
公开(公告)号：US4728735A
公开(公告)日：1988-03-01
申请号：US928747
申请日：1986-11-10
申请人： Patrice C. Belanger , Joshua Rokach , John Scheigetz
发明人： Patrice C. Belanger , Joshua Rokach , John Scheigetz
IPC分类号： C07D281/16 , A61K31/55
CPC分类号： C07D281/16
摘要： Compounds of the Formula I: ##STR1## are inhibitors of the mammalian 5-lipoxygenase enzyme system of the arachidonic acid cascade. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation and are useful as cytoprotective agents.
摘要翻译：式I化合物：I是哺乳动物5-脂肪氧合酶系统的花生四烯酸级联的抑制剂。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。

5. 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。

6. 发明授权

US4634766A 1,4-diaza-phenothiazines 失效
标题翻译： 1,4-二氮杂 - 吩噻嗪
公开(公告)号：US4634766A
公开(公告)日：1987-01-06
申请号：US660595
申请日：1984-10-15
申请人： Joseph G. Atkinson , Yvan Guindon , Patrice C. Belanger , Joshua Rokach
发明人： Joseph G. Atkinson , Yvan Guindon , Patrice C. Belanger , Joshua Rokach
IPC分类号： A61K31/495 , A61K31/535 , A61K31/54 , C07D241/18 , C07D498/04 , C07D513/04 , C07D513/16
CPC分类号： C07D513/04 , A61K31/495 , A61K31/535 , A61K31/54 , C07D241/18
摘要： Compounds of the Formula I: ##STR1## are inhibitors of the mammalian 5-lipoxygenase enzyme system of the arachidonic acid cascade. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.
摘要翻译：式I化合物：I是哺乳动物5-脂肪氧合酶系统的花生四烯酸级联的抑制剂。因此，这些化合物是治疗过敏性疾病，哮喘，心血管疾病和炎症的有用的治疗剂。

7. 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。

8. 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。

9. 发明授权

US4968821A 4,7-benzofurandione derivatives 失效
标题翻译： 4,7-苯并呋喃二酮衍生物
公开(公告)号：US4968821A
公开(公告)日：1990-11-06
申请号：US217264
申请日：1988-07-11
申请人： Julian Adams , Yvan Guindon , Patrice C. Belanger , Michel L. Belley , Joshua Rokach
发明人： Julian Adams , Yvan Guindon , Patrice C. Belanger , Michel L. Belley , Joshua Rokach
IPC分类号： C07D307/86 , C07D407/10 , C07D417/10
CPC分类号： C07D407/10 , C07D307/86 , C07D417/10
摘要： 4,7-Benzofurandione derivatives of Formula I, 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, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention. ##STR1##
摘要翻译：公开了式I的4,7-苯并呋喃二酮衍生物，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，牛皮癣和过敏性结膜炎的有用治疗剂。该化合物也可用作止痛剂和细胞保护剂。还公开了可用于制备本发明的4,7-苯并呋喃二酸的新型中间体。我

10. 发明授权

US4667055A Leukotriene antagonists 失效
标题翻译：白三烯拮抗剂
公开(公告)号：US4667055A
公开(公告)日：1987-05-19
申请号：US713927
申请日：1985-03-20
申请人： John Gillard , Joshua Rokach , Patrice C. Belanger
发明人： John Gillard , Joshua Rokach , Patrice C. Belanger
IPC分类号： A61K31/19 , A61K45/06 , C07C149/40
CPC分类号： C07C323/00 , Y10S514/826 , Y10S514/861 , Y10S514/863 , Y10S514/886
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，D4E4的白细胞三烯的拮抗剂和过敏反应的缓慢反应物质。因此，这些化合物可用作抗哮喘，抗过敏，抗炎和细胞保护剂。

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