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31. 发明授权

US06274583B1 Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US06274583B1
公开(公告)日：2001-08-14
申请号：US09345652
申请日：1999-06-30
申请人： Michael A. Patane , Mark G. Bock , Randall C. Newton
发明人： Michael A. Patane , Mark G. Bock , Randall C. Newton
IPC分类号： A61K31495
CPC分类号： C07D295/155 , C07D211/64
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α-1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

32. 发明授权

US06255315B1 Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US06255315B1
公开(公告)日：2001-07-03
申请号：US09458169
申请日：1999-12-09
申请人： Michael A. Patane , Harold G. Selnick , Mark G. Bock
发明人： Michael A. Patane , Harold G. Selnick , Mark G. Bock
IPC分类号： A61K31513
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha relductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为α1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物具有选择性地放松富集α1a受体亚型的平滑肌组织的能力，而不会同时引起低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人类5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，从而实现了由良性前列腺增生的作用引起的急性和慢性缓解。

33. 发明授权

US6080760A Alpha 1A adrenergic receptor antagonists 失效
公开(公告)号：US6080760A
公开(公告)日：2000-06-27
申请号：US98806
申请日：1998-06-17
申请人： Michael A. Patane , Mark G. Bock
发明人： Michael A. Patane , Mark G. Bock
IPC分类号： C07D205/04 , C07D239/22 , C07D413/06 , A61K31/421 , C07D211/32 , C07D263/26
CPC分类号： C07D239/22 , C07D205/04 , C07D413/06
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

34. 发明授权

US6075038A Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US6075038A
公开(公告)日：2000-06-13
申请号：US973622
申请日：1997-12-04
申请人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger
发明人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger
IPC分类号： A61K31/445 , A61K31/58 , A61P11/00 , C07D211/60 , C07D417/06 , A61K31/4453 , C07D211/06 , C07D401/04
CPC分类号： C07D417/06 , A61K31/58 , C07D211/60
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral fining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译： PCT No.PCT / US96 / 09363 Sec。 371 1997年12月4日第 102（e）日期1997年12月4日PCT提交1996年6月4日PCT公布。公开号WO96 / 40135 日期：1996年12月19日本发明涉及某些新型化合物及其衍生物，其合成及其作为选择性α-1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道澄清。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

35. 发明授权

US5185331A Triazolobenzodiazepines 失效
标题翻译：三苯并二恶英
公开(公告)号：US5185331A
公开(公告)日：1993-02-09
申请号：US699850
申请日：1991-05-14
申请人： Roger M. Freidinger , Mark G. Bock , Ben E. Evans
发明人： Roger M. Freidinger , Mark G. Bock , Ben E. Evans
IPC分类号： A61K31/55 , A61P25/04 , A61P25/20 , A61P25/30 , A61P27/02 , A61P35/00 , C07D487/04
CPC分类号： A61K31/55
摘要： Pharmaceutical compositions containing Triazolobenzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.

36. 发明授权

US4820834A Benzodiazepine analogs 失效
标题翻译：苯二氮卓类似物
公开(公告)号：US4820834A
公开(公告)日：1989-04-11
申请号：US26420
申请日：1987-03-16
申请人： Ben E. Evans , Roger M. Freidinger , Mark G. Bock
发明人： Ben E. Evans , Roger M. Freidinger , Mark G. Bock
IPC分类号： C07D243/14 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K38/00 , A61P1/00 , A61P1/04 , A61P25/00 , A61P43/00 , C07C271/22 , C07D209/20 , C07D209/48 , C07D243/16 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07F9/22 , C07F9/38 , C07F9/645 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/097
CPC分类号： C07D403/04 , C07C271/22 , C07D209/20 , C07D209/48 , C07D243/16 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0821 , A61K38/00
摘要： Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).
摘要翻译：公开了作为胃泌素和缩胆囊素（CCK）的拮抗剂的下列公式的苯并二氮杂类似物： I。

37. 发明授权

US4636491A Renin inhibitory peptides having improved solubility 失效
标题翻译：具有改善溶解度的肾素抑制肽
公开(公告)号：US4636491A
公开(公告)日：1987-01-13
申请号：US593754
申请日：1984-03-27
申请人： Mark G. Bock , Robert M. DiPardo , Joshua S. Boger , Ben E. Evans , Roger Freidinger
发明人： Mark G. Bock , Robert M. DiPardo , Joshua S. Boger , Ben E. Evans , Roger Freidinger
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07K5/02 , C07K7/02 , A61K37/64
CPC分类号： C07K5/0227 , Y10S530/86
摘要： Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
摘要翻译：式（Ⅰ）及其类似物的肾素抑制肽抑制肾素，可用于治疗各种形式的肾素相关性高血压和醛固酮增多症。

38. 发明授权

US4594191A Process for preparing a benzodiazepinedione derivative 失效
标题翻译：制备苯并二氮二酮衍生物的方法
公开(公告)号：US4594191A
公开(公告)日：1986-06-10
申请号：US725885
申请日：1985-04-22
申请人： Mark G. Bock , Ben E. Evans , Roger M. Freidinger , Steven M. Pitzenberger
发明人： Mark G. Bock , Ben E. Evans , Roger M. Freidinger , Steven M. Pitzenberger
IPC分类号： C07D487/04 , C07D403/14 , C07D403/06
CPC分类号： C07D487/04
摘要： A non-fermentation process for preparing a benzodiazepinedione of the formula: ##STR1## and intermediates is disclosed.
摘要翻译：公开了用于制备下式的苯并二氮杂二酮的非发酵方法：＆lt; IMAGE＆gt;和中间体。

39. 发明授权

US4559339A Indol-3-yl-quinazolino-1,4-benzodiazepin-5,13-diones 失效
标题翻译：吲哚-3-基 - 喹唑啉-1,4-苯并二氮杂-5,13-二酮
公开(公告)号：US4559339A
公开(公告)日：1985-12-17
申请号：US695118
申请日：1985-01-25
申请人： Mark G. Bock , Roger M. Freidinger , Ben E. Evans
发明人： Mark G. Bock , Roger M. Freidinger , Ben E. Evans
IPC分类号： A61K31/55 , A61P1/00 , C07D487/04 , C07D403/14
CPC分类号： C07D487/04
摘要： Novel indol-3-yl-quinazolino-1,4-benzodiazepin-5,13-diones, which are antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.
摘要翻译：作为缩胆囊素（CCK）功能的拮抗剂的新颖的吲哚-3-基 - 喹唑啉-1,4-苯并二氮杂-5,13-二酮从通过某些曲霉菌菌株好氧发酵制备的化合物制备这些化合物，以及使用这些化合物拮抗CCK的功能，该拮抗作用是有用的，例如用于治疗和预防哺乳动物，特别是人的胃肠道，中枢神经和食欲调节系统的紊乱。

40. 发明授权

US4554272A Substituted quinazolino-1,4-benzodiazepin-6,9-diones and their preparation 失效
标题翻译：取代的喹唑啉-1,4-苯并二氮杂-6,9-二酮及其制备
公开(公告)号：US4554272A
公开(公告)日：1985-11-19
申请号：US695119
申请日：1985-01-25
申请人： Mark G. Bock , Roger M. Freidinger
发明人： Mark G. Bock , Roger M. Freidinger
IPC分类号： A61K31/55 , A61P9/00 , C07D487/04 , C07K5/078 , C07D403/14
CPC分类号： C07D487/04 , C07K5/06156 , Y02P20/582
摘要： Tetracyclic compounds of the formula: ##STR1## and a process for their preparation are disclosed. The compounds have cholecystokinin inhibiting activity.
摘要翻译：公开了下式的四环化合物：其制备方法。该化合物具有胆囊收缩素抑制活性。

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