公开(公告)号：US06534510B2

公开(公告)日：2003-03-18

申请号：US09815404

申请日：2001-03-22

申请人： James C. Barrow ,  Bruce D. Dorsey ,  Harold G. Selnick ,  Phung L. Ngo

发明人： James C. Barrow ,  Bruce D. Dorsey ,  Harold G. Selnick ,  Phung L. Ngo

IPC分类号： C07D40100

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D471/04

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein A is

摘要翻译： 本发明的化合物可用于抑制凝血酶和相关的血栓闭塞，并且选自：或其药学上可接受的盐，其中A是

公开(公告)号：US06515011B2

公开(公告)日：2003-02-04

申请号：US10023776

申请日：2001-12-18

申请人： Harold G. Selnick ,  James C. Barrow ,  Philippe G. Nantermet ,  Peter D. Williams ,  Kenneth J. Stauffer ,  Philip E. Sanderson ,  Kenneth E. Rittle ,  Matthew M. Morrissette ,  Catherine M. Wiscount ,  Lekhanh O. Tran ,  Terry A. Lyle ,  Donnette D. Staas

发明人： Harold G. Selnick ,  James C. Barrow ,  Philippe G. Nantermet ,  Peter D. Williams ,  Kenneth J. Stauffer ,  Philip E. Sanderson ,  Kenneth E. Rittle ,  Matthew M. Morrissette ,  Catherine M. Wiscount ,  Lekhanh O. Tran ,  Terry A. Lyle ,  Donnette D. Staas

IPC分类号： A61K3140

CPC分类号： C07D401/06 ,  A61K38/00 ,  C07D205/04 ,  C07D207/16 ,  C07D403/12 ,  C07K5/06 ,  C07K5/06034 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06191

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.

摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓闭塞：或其药学上可接受的盐，例如， 其中R 3是-CH 2 NH 2，-CH 2 CH 2 NH 2或-CH 2 NHC（O）OC（CH 3）3。

公开(公告)号：US06235759B1

公开(公告)日：2001-05-22

申请号：US09428973

申请日：1999-10-28

申请人： James C. Barrow ,  Philippe G. Nanterment ,  Harold G. Selnick

发明人： James C. Barrow ,  Philippe G. Nanterment ,  Harold G. Selnick

IPC分类号： A61K3144

CPC分类号： C07D401/14 ,  A61K31/56 ,  C07D211/90 ,  A61K31/445 ,  A61K2300/00

摘要： Novel dihydropyridinone and pyrrolinone compounds and pharmaceutically acceptable salts thereof 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 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： 公开了新的二氢吡啶酮和吡咯啉酮化合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。

公开(公告)号：US6037354A

公开(公告)日：2000-03-14

申请号：US99031

申请日：1998-06-17

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： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D263/06 ,  A61K31/42 ,  C07D263/04 ,  C07D277/04

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 reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

公开(公告)号：US09120781B2

公开(公告)日：2015-09-01

申请号：US13697179

申请日：2011-05-10

申请人： Tong-Shuang Li ,  Ernest J. Mceachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Yongbao Zhu ,  Kun Liu ,  Harold G. Selnick

发明人： Tong-Shuang Li ,  Ernest J. Mceachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Yongbao Zhu ,  Kun Liu ,  Harold G. Selnick

IPC分类号： C07D263/56 ,  C07D263/58 ,  C07D277/82 ,  C07D413/04 ,  C07D417/04 ,  C07D277/64 ,  C07D263/52 ,  C07D277/60

CPC分类号： C07D417/04 ,  C07D263/52 ,  C07D263/56 ,  C07D263/58 ,  C07D277/60 ,  C07D277/64 ,  C07D277/82 ,  C07D413/04

摘要： The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

摘要翻译： 本发明提供了用于选择性抑制糖苷酶的化合物（I）的化合物，以及化合物的前药以及包含化合物的化合物或前药的药物组合物。 本发明还提供了治疗与O-GlcNAcase的缺乏或过度表达相关的疾病和障碍的方法，O-GlcNAc的积累或缺乏。

公开(公告)号：US08927507B2

公开(公告)日：2015-01-06

申请号：US14006888

申请日：2012-03-16

申请人： Ernest J. McEachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Craig A. Coburn ,  Kun Liu ,  Harold G. Selnick

发明人： Ernest J. McEachern ,  David J. Vocadlo ,  Yuanxi Zhou ,  Craig A. Coburn ,  Kun Liu ,  Harold G. Selnick

IPC分类号： C08B37/00 ,  C07D487/02 ,  A61K31/70 ,  A61K31/425 ,  C12Q1/34 ,  C07H13/04 ,  C07H9/06

CPC分类号： C07H9/06 ,  C07H13/04 ,  C12Q1/34 ,  G01N2333/924 ,  G01N2500/04

摘要： The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

公开(公告)号：US20140213584A9

公开(公告)日：2014-07-31

申请号：US13884061

申请日：2011-11-08

申请人： Craig A. Coburn ,  Kun Liu ,  Ernest J. McEachern ,  Changwei Mu ,  Harold G. Selnick ,  David J. Vocadlo ,  Yaode Wang ,  Zhongyong Wei ,  Yuanxi Zhou

发明人： Craig A. Coburn ,  Kun Liu ,  Ernest J. McEachern ,  Changwei Mu ,  Harold G. Selnick ,  David J. Vocadlo ,  Yaode Wang ,  Zhongyong Wei ,  Yuanxi Zhou

IPC分类号： C07D513/14

CPC分类号： C07D513/14 ,  C07D513/04 ,  C07H9/06 ,  C07H13/04 ,  C07H13/12 ,  C07H15/18 ,  C12Q1/48 ,  G01N2500/02

摘要： The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

公开(公告)号：US08372859B2

公开(公告)日：2013-02-12

申请号：US12594993

申请日：2008-04-07

申请人： Michael R. Wood ,  June Kim ,  Melody McWherter ,  Harold G. Selnick ,  Kathy Schirripa

发明人： Michael R. Wood ,  June Kim ,  Melody McWherter ,  Harold G. Selnick ,  Kathy Schirripa

IPC分类号： A61K31/44 ,  A01N43/50

CPC分类号： C07D235/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

摘要： Compounds of formula I: (wherein variables A, m, n, J, Re, Rf, R4, Ea, Eb, Ec, RPG 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; and 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A，m，n，J，Re，Rf，R4，Ea，Eb，Ec，RPG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; 和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。

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。

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。