公开(公告)号：US06358985B1

公开(公告)日：2002-03-19

申请号：US09342577

申请日：1999-06-29

申请人： Neville J. Anthony ,  Ian M. Bell ,  Douglas C. Beshore ,  Terrence M. Ciccarone ,  S. Jane de Solms ,  Christopher J. Dinsmore ,  Gerald E. Stokker

发明人： Neville J. Anthony ,  Ian M. Bell ,  Douglas C. Beshore ,  Terrence M. Ciccarone ,  S. Jane de Solms ,  Christopher J. Dinsmore ,  Gerald E. Stokker

IPC分类号： A61K314164

CPC分类号： A61K31/4174 ,  A61K31/00

摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

公开(公告)号：US06410534B1

公开(公告)日：2002-06-25

申请号：US09347673

申请日：1999-06-29

申请人： Christopher J. Dinsmore ,  Ian M. Bell ,  Douglas C. Beshore ,  Theresa M. Williams

发明人： Christopher J. Dinsmore ,  Ian M. Bell ,  Douglas C. Beshore ,  Theresa M. Williams

IPC分类号： A61K314188

CPC分类号： C07D498/04 ,  A61K31/415 ,  A61K31/335 ,  A61K2300/00

摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

公开(公告)号：US06441017B1

公开(公告)日：2002-08-27

申请号：US09656653

申请日：2000-09-07

申请人： Ian M. Bell ,  Douglas C. Beshore ,  Steven N. Gallicchio ,  C. Blair Zartman

发明人： Ian M. Bell ,  Douglas C. Beshore ,  Steven N. Gallicchio ,  C. Blair Zartman

IPC分类号： A61K314015

CPC分类号： C07D498/18 ,  A61K31/337 ,  A61K31/4178 ,  A61K45/06 ,  A61K47/665 ,  A61K47/6898 ,  B82Y5/00 ,  A61K2300/00

摘要： The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

摘要翻译： 本发明涉及抑制异戊烯基 - 蛋白转移酶（FTase）和癌基因蛋白Ras的异戊烯化的大环化合物。 本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。

公开(公告)号：US06248756B1

公开(公告)日：2001-06-19

申请号：US09248883

申请日：1999-02-11

申请人： Neville J. Anthony ,  Christopher Dinsmore ,  Robert P. Gomez ,  John H. Hutchinson ,  John S. Wai ,  Theresa M. Williams ,  Ian M. Bell ,  Mark W. Embrey ,  Thorsten E. Fisher

发明人： Neville J. Anthony ,  Christopher Dinsmore ,  Robert P. Gomez ,  John H. Hutchinson ,  John S. Wai ,  Theresa M. Williams ,  Ian M. Bell ,  Mark W. Embrey ,  Thorsten E. Fisher

IPC分类号： A61K314468

CPC分类号： C07D401/06 ,  C07D211/62 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferas (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

摘要翻译： 本发明涉及抑制法尼基蛋白转移（Fatease-protein transferas，FTase）和致癌基因蛋白Ras的法呢基化的化合物。 本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。

公开(公告)号：US5939439A

公开(公告)日：1999-08-17

申请号：US995744

申请日：1997-12-22

申请人： Neville J. Anthony ,  Samuel L. Graham ,  Lekhanh O. Tran ,  Ian M. Bell ,  S. Jane deSolms ,  Robert P. Gomez ,  Michelle Sparks Kuo ,  William C. Lumma, Jr. ,  Debra S. Perlow ,  Anthony W. Shaw ,  John S. Wai ,  Steven D. Young

发明人： Neville J. Anthony ,  Samuel L. Graham ,  Lekhanh O. Tran ,  Ian M. Bell ,  S. Jane deSolms ,  Robert P. Gomez ,  Michelle Sparks Kuo ,  William C. Lumma, Jr. ,  Debra S. Perlow ,  Anthony W. Shaw ,  John S. Wai ,  Steven D. Young

IPC分类号： C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D401/04 ,  A61K31/44

CPC分类号： C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

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。

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.

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。

公开(公告)号：US08071772B2

公开(公告)日：2011-12-06

申请号：US12085131

申请日：2006-11-14

申请人： Ian M. Bell ,  Harold G. Selnick ,  Craig A. Stump ,  Cory R. Theberge ,  C. Blair Zartman

发明人： Ian M. Bell ,  Harold G. Selnick ,  Craig A. Stump ,  Cory R. Theberge ,  C. Blair Zartman

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。