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公开(公告)号:US5691323A
公开(公告)日:1997-11-25
申请号:US440153
申请日:1995-05-12
申请人: Wayne J. Thompson , Michael F. Sugrue , Richard W. Ransom , Pierre J. Mallorga , Ian M. Bell , Anthony M. Smith
发明人: Wayne J. Thompson , Michael F. Sugrue , Richard W. Ransom , Pierre J. Mallorga , Ian M. Bell , Anthony M. Smith
IPC分类号: C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , A61K31/38 , A61K31/34 , C07D403/14
CPC分类号: C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12
摘要: Compounds, 1,3-dihydro-1-{1-�piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
摘要翻译: 化合物,1,3-二氢-1- {1- [哌啶-4-基]哌啶-4-基} -2H-苯并咪唑-2-酮和1,3-二氢-1- {4-氨基-1- 环己基} -2H-苯并咪唑-2-酮及其衍生物,其制备方法,使用方法和药物组合物。 这些化合物具有抗毒蕈碱活性,可用于治疗和/或预防近视(俗称近视)。
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公开(公告)号:US5574044A
公开(公告)日:1996-11-12
申请号:US329757
申请日:1994-10-27
申请人: Wayne J. Thompson , Michael F. Sugrue , Richard W. Ransom , Pierre J. Mallorga , Ian M. Bell , Anthony M. Smith
发明人: Wayne J. Thompson , Michael F. Sugrue , Richard W. Ransom , Pierre J. Mallorga , Ian M. Bell , Anthony M. Smith
IPC分类号: C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , A61K31/445
CPC分类号: C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12
摘要: Compounds, 1,3-dihydro-1-{1-[piperidin-4-yl]piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
摘要翻译: 化合物,1,3-二氢-1- {1- [哌啶-4-基]哌啶-4-基} -2H-苯并咪唑-2-酮和1,3-二氢-1- {4-氨基-1- 环己基} -2H-苯并咪唑-2-酮及其衍生物,其制备方法,使用方法和药物组合物。 这些化合物具有抗毒蕈碱活性,可用于治疗和/或预防近视(俗称近视)。
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公开(公告)号:US5718912A
公开(公告)日:1998-02-17
申请号:US736705
申请日:1996-10-28
申请人: Wayne J. Thomspon , Pierre Mallorga , Richard W. Ransom , Ian M. Bell , Michael F. Sugrue , Peter M. Munson
发明人: Wayne J. Thomspon , Pierre Mallorga , Richard W. Ransom , Ian M. Bell , Michael F. Sugrue , Peter M. Munson
IPC分类号: C07D401/04 , A61F2/00 , A01N43/40 , A61K31/445
CPC分类号: C07D401/04
摘要: This invention is concerned with novel 1-�cycloalkylpioeridin-4-yl!-2H benzimidazolones, their compositions and method of use. The novel compounds are selective muscarinic agonists of the m2 subtype with low activity at the m3 subtype. The compounds are effective for the treatment of glaucoma with fewer side effects than the pilocarpine therapy.
摘要翻译: 本发明涉及新的1- [环烷基吡啶-4-基] -2H-苯并咪唑酮,其组合物和使用方法。 新型化合物是m2亚型的选择性毒蕈碱激动剂,在m3亚型下具有低活性。 该化合物对于治疗与毛果芸香碱治疗相比副作用较小的青光眼有效。
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4.
公开(公告)号:US5939414A
公开(公告)日:1999-08-17
申请号:US959264
申请日:1997-10-28
申请人: Ian M. Bell , Daria Jean Hazuda , James P. Guare, Jr. , Peter M. Munson , Wayne J. Thompson , Joseph P. Vacca
发明人: Ian M. Bell , Daria Jean Hazuda , James P. Guare, Jr. , Peter M. Munson , Wayne J. Thompson , Joseph P. Vacca
IPC分类号: A61K31/5513 , C07D243/20 , C07D403/12 , A61K31/55 , C07D243/14
CPC分类号: C07D403/12 , A61K31/5513 , C07D243/20
摘要: Compounds having a benzodiazepine hydrazide core are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译: 描述了具有苯并二氮杂肼核心的化合物。 这些化合物可用作抑制HIV整合酶,预防或治疗HIV感染和治疗AIDS,作为化合物,药学上可接受的盐,药物组合物成分,无论是否与其他抗病毒药,免疫调节剂,抗生素或其他抗生素组合使用 疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号:US5760054A
公开(公告)日:1998-06-02
申请号:US722001
申请日:1996-10-01
IPC分类号: A61K31/435 , A61K31/445 , A61K31/475 , A61K31/505 , A61P13/02 , A61P15/00 , A61P17/00 , A61P43/00 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10 , C07D495/04 , C07D495/20 , C07D498/04 , C07D498/10 , C07D513/04 , C07D513/10 , C07D401/04 , C07D471/10
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10 , C07D513/04 , C07D513/10
摘要: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1C adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hypertrophy. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha1C 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: PCT No.PCT / US95 / 04590 Sec。 371日期:1996年10月1日 102(e)日期1996年10月1日PCT提交1995年4月13日PCT公布。 WO95 / 28397 PCT出版物 日期1995年10月26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-1C肾上腺素能受体拮抗剂的用途。 这些化合物的一种应用是治疗良性前列腺肥大。 这些化合物具有选择性地放松富集α1C受体亚型的平滑肌组织的能力,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。
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6.
公开(公告)号:US09409916B2
公开(公告)日:2016-08-09
申请号:US14005673
申请日:2012-03-14
申请人: Ian M. Bell , Justin Belardi
发明人: Ian M. Bell , Justin Belardi
IPC分类号: C07D487/10 , C07D471/10
CPC分类号: C07D487/10 , C07D471/10
摘要: The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译: 本发明涉及作为CGRP受体的拮抗剂的哌啶酮甲酰胺螺乙内酰脲衍生物,其可用于治疗或预防涉及CGRP的疾病,例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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公开(公告)号:US20120122900A1
公开(公告)日:2012-05-17
申请号:US13293177
申请日:2011-11-10
申请人: Ian M. Bell , Mark E. Fraley , Steven N. Gallicchio , Anthony Ginnetti , Helen J. Mitchell , Daniel V. Paone , Donnette D. Staas , Cheng Wang , C. Blair Zartman
发明人: Ian M. Bell , Mark E. Fraley , Steven N. Gallicchio , Anthony Ginnetti , Helen J. Mitchell , Daniel V. Paone , Donnette D. Staas , Cheng Wang , C. Blair Zartman
IPC分类号: A61K31/437 , A61K31/527 , A61P25/06 , C07D471/20
CPC分类号: A61K31/4545 , A61K31/435 , A61K31/438 , C07D471/10 , C07D471/20
摘要: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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公开(公告)号:US08143266B2
公开(公告)日:2012-03-27
申请号:US12595704
申请日:2008-04-11
申请人: Ian M. Bell , Harold G. Selnick , Craig A. Stump
发明人: Ian M. Bell , Harold G. Selnick , Craig A. Stump
IPC分类号: A61K31/437 , C07D221/20
CPC分类号: C07D471/20
摘要: Compounds of formula I: (wherein variables A1, A2, B, m, n, J, X, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译: 式I化合物(其中变量A1,A2,B,m,n,J,X,R4,G1,G2,G3和Y如本文所述),其是CGRP受体的拮抗剂,其可用于治疗或 预防CGRP涉及的疾病,如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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公开(公告)号:US20120065190A1
公开(公告)日:2012-03-15
申请号:US12520146
申请日:2007-12-14
申请人: Ian M. Bell , Harold G. Selnick
发明人: Ian M. Bell , Harold G. Selnick
IPC分类号: A61K31/55 , C07D487/04 , A61P25/08 , A61P25/06 , A61P9/12 , C07D519/00 , A61P29/00
CPC分类号: C07D487/04 , A61K31/55 , A61K45/06 , C07D471/10 , C07D471/20 , C07D498/20 , C07D519/00
摘要: Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译: 式I化合物(其中变量A1,m,R1,R2,R3,R4和Z如本文所述),其是CGRP受体的拮抗剂,其可用于治疗或预防涉及CGRP的疾病, 如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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公开(公告)号:US08071772B2
公开(公告)日:2011-12-06
申请号:US12085131
申请日:2006-11-14
IPC分类号: C07D471/04
CPC分类号: C07D471/20 , C07D519/00
摘要: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2, J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译: 式I化合物(其中变量A1,A2,A3,A4,A5,A6,A7,B,E1,E2,E3,E4,E5,G1,G2,J和K如本文所述) CGRP受体,其可用于治疗或预防涉及CGRP的疾病,例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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