公开(公告)号：US20140011827A1

公开(公告)日：2014-01-09

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

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.

公开(公告)号：US20140005214A1

公开(公告)日：2014-01-02

申请号：US14005595

申请日：2012-03-14

申请人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Helen J. Mitchell ,  Cheng Wang

发明人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Helen J. Mitchell ,  Cheng Wang

IPC分类号： C07D401/12

CPC分类号： C07D401/12 ,  A61K31/445

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。

公开(公告)号：US20100298269A1

公开(公告)日：2010-11-25

申请号：US12864120

申请日：2009-02-04

申请人： Ian M. Bell ,  Steven N. Gallicchio ,  Valentino J. Stella

发明人： Ian M. Bell ,  Steven N. Gallicchio ,  Valentino J. Stella

IPC分类号： A61K31/675 ,  C07F9/6561 ,  A61P29/00 ,  A61P3/10 ,  A61P9/00 ,  A61P11/06 ,  A61P19/02 ,  A61P17/00

CPC分类号： C07D471/04 ,  C07F9/6561

摘要： Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are useful in the treatment or prevention of diseases in which 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： 公开了式（I）的前药化合物（其中变量R 1和R 2如本文所述），其是CGRP受体的拮抗剂的类似物，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。

公开(公告)号：US5760054A

公开(公告)日：1998-06-02

申请号：US722001

申请日：1996-10-01

申请人： Joel R. Huff ,  Hee-Yoon Lee ,  Jennie B. Nerenberg ,  Wayne J. Thompson ,  Ian M. Bell

发明人： Joel R. Huff ,  Hee-Yoon Lee ,  Jennie B. Nerenberg ,  Wayne J. Thompson ,  Ian M. Bell

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。