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公开(公告)号：US4853389A
公开(公告)日：1989-08-01
申请号：US186499
申请日：1988-04-26
IPC分类号： C07D239/48
CPC分类号： C07D239/48
摘要： This invention relates to substituted 5-pyrimidinesulfonamides, pharmaceutically acceptable salts thereof and to processes for synthesis thereof. Other aspects of the invention concern pharmaceutical compositions containing an instant compound as active ingredient and methods of treatment where there is an indicated need for an antihypertensive and/or diuretic agent.
摘要翻译： 本发明涉及取代的5-嘧啶磺酰胺及其药学上可接受的盐及其合成方法。 本发明的其它方面涉及含有本发明化合物作为活性成分的药物组合物以及需要抗高血压剂和/或利尿剂的治疗方法。
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2.发明授权5 step process for preparing certain 2,4-diamino-5-pyrimidine-sulfonyl ureas 失效制备某些2,4-二氨基-5-嘧啶磺酰脲的5步法
公开(公告)号：US4914203A
公开(公告)日：1990-04-03
申请号：US333476
申请日：1989-04-05
IPC分类号： C07D239/48
CPC分类号： C07D239/48
摘要： This invention relates to substituted 5-pyrimidinesulfonamides, pharmaceutically acceptable salts thereof and to processes for synthesis thereof. Other aspects of the invention concern pharmaceutical compositions containing an instant compound as active ingredient and methods of treatment where there is an indicated need for an antihypertensive and/or diuretic agent.
摘要翻译： 本发明涉及取代的5-嘧啶磺酰胺及其药学上可接受的盐及其合成方法。 本发明的其它方面涉及含有本发明化合物作为活性成分的药物组合物以及需要抗高血压剂和/或利尿剂的治疗方法。
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![Oxathiepino[6,5-b]dihydropyridines, and related compositions and methods](/abs-image/US/2002/11/05/US06476022B1/abs.jpg.150x150.jpg)
3.发明授权Oxathiepino[6,5-b]dihydropyridines, and related compositions and methods 有权Oxathiepino [6,5-b]二氢吡啶类，以及相关组合物和方法公开(公告)号：US06476022B1
公开(公告)日：2002-11-05
申请号：US09603262
申请日：2000-06-23
IPC分类号： C07D49704
CPC分类号： C07D497/04
摘要： This invention provides novel oxathiepino[6,5-b]dihydropyridines. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.
摘要翻译： 本发明提供了新的氧硫杂环庚烯[6,5-b]二氢吡啶。 这些化合物可用作具有心血管，抗哮喘和抗纤维支配作用的钙通道拮抗剂。 因此，本发明还提供了用于预防和治疗诸如超敏反应，过敏，哮喘，支气管痉挛，痛经，食管痉挛，青光眼，早产，尿路障碍，胃肠蠕动障碍和心血管疾病等疾病的药物组合物以及方法。
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4.发明授权Substituted 3-pyridyl-4-arylpyrroles, and related therapeutic and prophylactic methods 有权取代的3-吡啶基-4-芳基吡咯，以及相关的治疗和预防方法公开(公告)号：US06562843B1
公开(公告)日：2003-05-13
申请号：US09561534
申请日：2000-04-28
申请人： James L. Bullington
发明人： James L. Bullington
IPC分类号： A61K314439
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04
摘要： This invention provides novel substituted 3-pyridyl-4-arylpyrroles, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by reducing TNF-&agr; production and/or p38 activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
摘要翻译： 本发明提供了新的取代的3-吡啶基-4-芳基吡咯，以及包含其的药物组合物，其可用于治疗通过在适当细胞中降低TNF-α产生和/或p38活性而改善的病症。 本发明还提供了使用本发明的药物组合物的治疗和预防方法。
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公开(公告)号：US06410553B1
公开(公告)日：2002-06-25
申请号：US09751005
申请日：2000-12-28
IPC分类号： A61K3155
CPC分类号： C07D495/04
摘要： This invention provides novel benzosulfones of the following formulae: These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.
摘要翻译： 本发明提供新的下式的苯并砜：这些化合物可用作具有心血管，止喘和抗纤维支配作用的钙通道拮抗剂。 因此，本发明还提供了用于预防和治疗诸如超敏反应，过敏，哮喘，支气管痉挛，痛经，食管痉挛，青光眼，早产，尿路障碍，胃肠蠕动障碍和心血管疾病等疾病的药物组合物以及方法。
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![Dithiepino[6,5-b]pyridines, and related compositions and methods](/abs-image/US/2001/09/18/US06291454B1/abs.jpg.150x150.jpg)
6.发明授权公开(公告)号：US06291454B1
公开(公告)日：2001-09-18
申请号：US09580882
申请日：2000-05-30
IPC分类号： A61K3154
CPC分类号： C07D495/04
摘要： This invention provides novel dithiepino[6,5-b]pyridines of the following formulae. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthinatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.
摘要翻译： 本发明提供下列通式的新型二硫杂环庚烯[6,5-b]吡啶。这些化合物可用作具有心血管，抗衰老和抗纤维支配作用的钙通道拮抗剂。 因此，本发明还提供了用于预防和治疗诸如超敏反应，过敏，哮喘，支气管痉挛，痛经，食管痉挛，青光眼，早产，尿路障碍，胃肠蠕动障碍和心血管疾病等疾病的药物组合物以及方法。
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公开(公告)号：US06562824B2
公开(公告)日：2003-05-13
申请号：US09847228
申请日：2001-05-02
IPC分类号： A61K314965
CPC分类号： C07D495/04 , C07D211/90 , C07D497/04
摘要： This invention relates to novel dihydropyridine soft drugs of the formula &PHgr;OOR1, where &PHgr; is a dihydropyridine moiety. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibroncho-constriction activity. Use of such soft drug analogs permits the administration of greater doses of the claimed dihydropyridine compounds without intolerable systemic effects. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasim, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders, while avoiding unwanted systemic effects.
摘要翻译： 本发明涉及式PHIOOR1的新的二氢吡啶软的药物，其中PHI是二氢吡啶部分。 这些化合物可用作具有心血管，抗哮喘和抗纤维蛋白回缩活性的钙通道拮抗剂。 使用这种软性药物类似物允许施用更大剂量的要求保护的二氢吡啶化合物，而不会产生不能容忍的全身作用。 因此，本发明还提供了用于预防和治疗诸如超敏反应，过敏，哮喘，支气管扩张症，痛经，食管痉挛，青光眼，早产，尿道紊乱，胃肠蠕动障碍和心血管疾病等疾病的药物组合物以及方法， 同时避免不必要的全身效应。
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![Benzo-fused dithiepino[6,5-b]pyridines, and related compositions and methods](/abs-image/US/2002/10/29/US06472530B1/abs.jpg.150x150.jpg)
8.发明授权Benzo-fused dithiepino[6,5-b]pyridines, and related compositions and methods 有权苯并稠合的二硫杂环庚烯[6,5-b]吡啶，以及相关的组合物和方法公开(公告)号：US06472530B1
公开(公告)日：2002-10-29
申请号：US09653024
申请日：2000-09-01
IPC分类号： C07D22116
CPC分类号： C07D495/04
摘要： This invention provides novel dithiepino[6,5-b]pyridines of the following formulae: These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.
摘要翻译： 本发明提供下列结构式的新型二硫杂环庚烯[6,5-b]吡啶：这些化合物可用作具有心血管，止喘和抗纤维支配作用的钙通道拮抗剂。 因此，本发明还提供了用于预防和治疗诸如超敏反应，过敏，哮喘，支气管痉挛，痛经，食管痉挛，青光眼，早产，尿路障碍，胃肠蠕动障碍和心血管疾病等疾病的药物组合物以及方法。
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公开(公告)号：US06410552B1
公开(公告)日：2002-06-25
申请号：US09751002
申请日：2000-12-28
IPC分类号： A61K3155
CPC分类号： C07D497/04
摘要： This invention provides novel benzoethers of the following formulae: These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.
摘要翻译： 本发明提供下式的新型苯醚：这些化合物可用作具有心血管，抗哮喘和抗纤维支配作用的钙通道拮抗剂。 因此，本发明还提供了用于预防和治疗诸如超敏反应，过敏，哮喘，支气管痉挛，痛经，食管痉挛，青光眼，早产，尿路障碍，胃肠蠕动障碍和心血管疾病等疾病的药物组合物以及方法。
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公开(公告)号：US5834521A
公开(公告)日：1998-11-10
申请号：US693861
申请日：1996-08-05
IPC分类号： A61K31/015 , A61K31/03 , A61K31/04 , A61K31/085 , A61K31/12 , A61K31/135 , A61K31/165 , A61K31/215 , A61P13/02 , A61P15/00 , C07C13/66 , C07C23/46 , C07C25/22 , C07C39/17 , C07C43/21 , C07C43/215 , C07C43/225 , C07C43/23 , C07C49/755 , C07C49/84 , C07C65/26 , C07C69/00 , C07C69/157 , C07C69/65 , C07C69/734 , C07C205/20 , C07C205/37 , C07C205/42 , C07C211/61 , C07C217/16 , C07C217/24 , C07C233/07 , C07C233/11 , C07C233/15 , C07D257/04 , C07F9/12 , A61K31/09
CPC分类号： C07D257/04 , C07C13/66 , C07C205/20 , C07C205/37 , C07C205/42 , C07C211/61 , C07C217/24 , C07C233/07 , C07C233/15 , C07C25/22 , C07C39/17 , C07C43/21 , C07C43/215 , C07C43/225 , C07C43/23 , C07C49/755 , C07C49/84 , C07C65/26 , C07C69/017 , C07C69/157 , C07C69/16 , C07C69/63 , C07F9/12 , C07C2103/40
摘要： Tetracyclic compounds having the following structure are described: ##STR1## wherein R.sub.1 -R.sub.10 are as defined. The tetracyclic compounds are capable of potent effects on steroid sensitive tissues and have demonstrated increased uterine weight, antiovulatory effects and potent steroid receptor binding. The compounds have therapeutic utility in reproductive applications such as fertility control, labor induction, ovulation induction and spermatogenesis. Methods for preparing the tetracyclic compounds from substituted indanones are also described.
摘要翻译： 描述具有以下结构的四环化合物：其中R 1 -R 10如上所定义。 四环化合物能够对类固醇敏感组织产生有效的作用，并且已经证明子宫重量增加，抗疟药效应和有效的类固醇受体结合。 这些化合物在繁殖应用中具有治疗效用，例如生育控制，劳动诱导，排卵诱导和精子发生。 还描述了从取代的茚满酮制备四环化合物的方法。
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