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公开(公告)号:US5439906A
公开(公告)日:1995-08-08
申请号:US155672
申请日:1993-11-22
IPC分类号: C07D487/04 , A61K31/55 , A61P9/06
CPC分类号: A61K31/55 , Y10S514/821
摘要: Imidazobenzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##
摘要翻译: 具有3-位氨基或脲官能团的咪唑并 - (1,5) - 二氮杂衍生物可用于治疗心律失常。 化合物具有结构式:
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公开(公告)号:US5026703A
公开(公告)日:1991-06-25
申请号:US535816
申请日:1990-06-11
IPC分类号: A61K31/50 , A61K38/00 , A61K38/11 , A61P13/02 , A61P15/00 , C07D487/22 , C07K5/10 , C07K7/16 , C07K7/64
摘要: Peptide compounds of formula I are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for the stoppage of labor prepatory to Caesarian delivery. ##STR1##
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公开(公告)号:US08022215B2
公开(公告)日:2011-09-20
申请号:US12866387
申请日:2009-02-04
CPC分类号: C07D221/02 , C07D215/56 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/10 , C07D409/10 , C07D409/14 , C07D413/10
摘要: The present invention is directed to fused pyridone compounds of formula (I) (I) that are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译: 本发明涉及作为M1受体阳性变构调节剂的式(I)(I)的融合吡啶酮化合物,其可用于治疗涉及M1受体的疾病,例如阿尔茨海默病,精神分裂症,疼痛或 睡眠障碍 本发明还涉及包含该化合物的药物组合物,以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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公开(公告)号:US5834464A
公开(公告)日:1998-11-10
申请号:US640730
申请日:1996-05-06
IPC分类号: C07D487/04 , A61K31/395
CPC分类号: C07D487/04
摘要: Imidazolinobenzodiazepines are cholecystokinin B (CCK-B) antagonists useful as anxiolytic agents. The compounds have structures such as: ##STR1##
摘要翻译: PCT No.PCT / US94 / 13325 Sec。 371日期:1996年5月6日 102(e)日期1996年5月6日PCT 1994年11月18日PCT PCT。 WO95 / 14693 PCT出版物 日期1995年6月1日咪唑啉二氮卓类是可用作抗焦虑剂的胆囊收缩素B(CCK-B)拮抗剂。 化合物具有如下结构:
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公开(公告)号:US20100324088A1
公开(公告)日:2010-12-23
申请号:US12866387
申请日:2009-02-04
IPC分类号: A61K31/47 , C07D221/04 , A61K31/455 , C07D215/56 , A61K31/4709 , C07D401/10 , A61P25/28 , A61P25/00 , A61P29/00
CPC分类号: C07D221/02 , C07D215/56 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/10 , C07D409/10 , C07D409/14 , C07D413/10
摘要: The present invention is directed to fused pyridone compounds of formula (I) (I) that are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译: 本发明涉及作为M1受体阳性变构调节剂的式(I)(I)的融合吡啶酮化合物,其可用于治疗涉及M1受体的疾病,例如阿尔茨海默病,精神分裂症,疼痛或 睡眠障碍 本发明还涉及包含该化合物的药物组合物,以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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公开(公告)号:US5218114A
公开(公告)日:1993-06-08
申请号:US848794
申请日:1992-03-10
IPC分类号: A61K31/55 , A61K31/551 , A61P1/00 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/30 , A61P27/02 , A61P43/00 , C07D243/16 , C07D243/18 , C07D243/24 , C07D403/06
CPC分类号: C07D403/06 , C07D243/24
摘要: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).
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公开(公告)号:US4628084A
公开(公告)日:1986-12-09
申请号:US815620
申请日:1986-01-02
申请人: Mark G. Bock , Daniel F. Veber , Robert M. DiPardo
发明人: Mark G. Bock , Daniel F. Veber , Robert M. DiPardo
IPC分类号: C07D243/24
CPC分类号: C07D243/24
摘要: The present invention provides an improved process for producing 3-acylamino benzodiazepines of the formula: ##STR1## wherein: R is loweralkyl of from 1-6 carbon atoms, aryl such as phenyl and halophenyl, aralkyl, alkyloxy, aralkyloxy, indolyl or substituted indolyl;R' is hydrogen, loweralkyl of from 1-6 carbon atoms, carboxymethyl or carbalkoxymethyl wherein the alkoxy groups contain from 1-4 carbon atoms;X is hydrogen or halogen;Y is hydrogen or halogen.These compounds are useful because of their activity as cholecystokinin (CCK) inhibitors.
摘要翻译: 本发明提供了一种改进的下式的3-酰基氨基苯并二氮杂的方法:其中:R是1-6个碳原子的低级烷基,芳基如苯基和卤代苯基,芳烷基,烷氧基,芳烷氧基,吲哚基或取代的 吲哚基 R'是氢,1-6个碳原子的低级烷基,羧甲基或烷氧基甲基,其中烷氧基含有1-4个碳原子; X是氢或卤素; Y是氢或卤素。 由于它们作为胆囊收缩素(CCK)抑制剂的活性,这些化合物是有用的。
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公开(公告)号:US08895580B2
公开(公告)日:2014-11-25
申请号:US13499335
申请日:2010-10-01
IPC分类号: A61K31/4745 , A61K31/5377 , C07D519/00 , C07D471/04 , C07D473/00 , C07D487/02 , C07D495/04 , A61K31/535
CPC分类号: C07D405/04 , A61K31/535 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/02 , C07D491/056 , C07D495/04 , C07F7/0812
摘要: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译: 本发明涉及式(I)的喹啉酮 - 吡唑啉酮化合物,其为M1受体阳性变构调节剂,可用于治疗涉及M1受体的疾病,例如阿尔茨海默氏病,精神分裂症,疼痛或睡眠障碍 。 本发明还涉及包含该化合物的药物组合物,以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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9.
公开(公告)号:US20120196845A1
公开(公告)日:2012-08-02
申请号:US13499335
申请日:2010-10-01
IPC分类号: A61K31/4745 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/519 , C07D519/00 , A61K31/498 , A61K31/52 , A61P25/28 , A61P25/18 , A61P29/00 , A61P25/00 , C07D471/04 , A61K31/501
CPC分类号: C07D405/04 , A61K31/535 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/02 , C07D491/056 , C07D495/04 , C07F7/0812
摘要: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译: 本发明涉及式(I)的喹啉酮 - 吡唑啉酮化合物,其为M1受体阳性变构调节剂,可用于治疗涉及M1受体的疾病,例如阿尔茨海默氏病,精神分裂症,疼痛或睡眠障碍 。 本发明还涉及包含该化合物的药物组合物,以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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公开(公告)号:US06436962B1
公开(公告)日:2002-08-20
申请号:US09671518
申请日:2000-09-27
IPC分类号: A61K31445
CPC分类号: C07D401/06 , A61K45/06 , C07D233/76 , C07D401/14 , C07D471/10
摘要: Arylhydantoin derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically 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 can be achieved.
摘要翻译: 公开了乙内酰脲衍生物及其药学上可接受的盐。 还描述了这些化合物的合成及其作为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。 这些化合物通常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,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。
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