公开(公告)号：US20050267119A1

公开(公告)日：2005-12-01

申请号：US11126915

申请日：2005-05-11

申请人： Hannguang Chao ,  Huji Tuerdi ,  Timothy Herpin ,  Jacques Roberge ,  Yalei Liu ,  R. Lawrence ,  Robert Rehfuss ,  Charles Clark ,  Jennifer Qiao ,  Timur Gungor ,  Patrick Lam ,  Tammy Wang ,  Rejean Ruel ,  Alexandre L'Heureux ,  Carl Thibeault ,  Gilles Bouthillier ,  Dora Schnur

发明人： Hannguang Chao ,  Huji Tuerdi ,  Timothy Herpin ,  Jacques Roberge ,  Yalei Liu ,  R. Lawrence ,  Robert Rehfuss ,  Charles Clark ,  Jennifer Qiao ,  Timur Gungor ,  Patrick Lam ,  Tammy Wang ,  Rejean Ruel ,  Alexandre L'Heureux ,  Carl Thibeault ,  Gilles Bouthillier ,  Dora Schnur

IPC分类号： A61K31/4439 ,  A61K31/444 ,  A61K31/501 ,  C07C275/30 ,  C07C275/32 ,  C07D213/40 ,  C07D213/75 ,  C07D213/89 ,  C07D231/40 ,  C07D231/50 ,  C07D237/22 ,  C07D333/36 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07F7/18 ,  C07D43/02 ,  C07D41/02

CPC分类号： C07D409/14 ,  C07C275/30 ,  C07C275/32 ,  C07D213/40 ,  C07D213/75 ,  C07D213/89 ,  C07D231/40 ,  C07D231/50 ,  C07D237/22 ,  C07D333/36 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07F7/1804

摘要： The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.

摘要翻译： 本发明提供了新的吡啶基或苯基脲及其类似物，它们是人P2Y 1受体的选择性抑制剂。 本发明还提供了相同的各种药物组合物以及治疗对P2Y受体活性的调节作用的疾病的方法。

公开(公告)号：US20050203146A1

公开(公告)日：2005-09-15

申请号：US11038862

申请日：2005-01-19

申请人： Timothy Herpin ,  George Morton ,  Robert Rehfuss ,  R. Lawrence ,  Michael Poss ,  Jacques Roberge ,  Timur Gungor

发明人： Timothy Herpin ,  George Morton ,  Robert Rehfuss ,  R. Lawrence ,  Michael Poss ,  Jacques Roberge ,  Timur Gungor

IPC分类号： A61K31/4178 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4439 ,  C07D235/30 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/02 ,  C07D413/12 ,  C07D413/14 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D513/04 ,  C07D43/02

CPC分类号： C07D401/12 ,  C07D235/30 ,  C07D401/14 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D513/04

摘要： The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.

摘要翻译： 本发明提供了新的氨基 - 苯并唑类似物，它们是人P2Y 1受体的选择性抑制剂。 本发明还提供了相同的各种药物组合物以及治疗对P2Y受体活性的调节作用的疾病的方法。

公开(公告)号：US20060025403A1

公开(公告)日：2006-02-02

申请号：US11199464

申请日：2005-08-08

申请人： Guixue Yu ,  John Macor ,  Timothy Herpin ,  R. Lawrence ,  George Morton ,  Rejean Ruel ,  Graham Poindexter ,  Edward Ruediger ,  Carl Thibault

发明人： Guixue Yu ,  John Macor ,  Timothy Herpin ,  R. Lawrence ,  George Morton ,  Rejean Ruel ,  Graham Poindexter ,  Edward Ruediger ,  Carl Thibault

IPC分类号： A61K31/4709 ,  A61K31/454 ,  A61K31/4025 ,  C07D43/02

CPC分类号： C07D401/12 ,  A61K38/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D495/04 ,  C07K5/06139 ,  C07K5/06191 ,  Y02A50/411 ,  Y02A50/463

摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is X is N or CH, W is —NR16R17, —NR16C(═O)R22, —NR16CO2R22, —OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.

摘要翻译： 具有式（I）的化合物及其药学上可接受的盐，水合物和前药，其中E是X是N或CH，W是-NR 16 R 17， ，-NR 16 C（-O）R 22，-NR 16 CO 2 R 22 或者如说明书中定义的杂芳基或杂环基，R 1至R 12，R 12， R 17，R 17，R 22，R 23，x，y和z定义如上 说明书可用作黑皮质素受体的调节剂，特别是MC-1R和MC-4R。

公开(公告)号：US07067525B2

公开(公告)日：2006-06-27

申请号：US10696761

申请日：2003-10-29

申请人： Guixue Yu ,  John Macor ,  Timothy Herpin ,  R. Michael Lawrence ,  George C. Morton ,  Rejean Ruel ,  Graham S. Poindexter ,  Edward H. Ruediger ,  Carl Thibault

发明人： Guixue Yu ,  John Macor ,  Timothy Herpin ,  R. Michael Lawrence ,  George C. Morton ,  Rejean Ruel ,  Graham S. Poindexter ,  Edward H. Ruediger ,  Carl Thibault

IPC分类号： A61K31/44 ,  A61K31/445 ,  C07D401/04 ,  C07D413/04 ,  C07D211/70

CPC分类号： C07D401/12 ,  A61K38/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D495/04 ,  C07K5/06139 ,  C07K5/06191 ,  Y02A50/411 ,  Y02A50/463

摘要： Compounds having the formula (I), G is a novel side chain selected from C2-6alkenyl, A3-aryl, —OR18, heteroaryl, A1-cyano, A2—OR17, A1—C(═O)R18, A1—CO2R18, A1—C(═O)NR18R19, A1—OC(═O)R18, A1—NR18C(═O)R19, A1—OC(═O)NR18R19, A1—NR18CO2R19, A1—NR18SO2R17, A1—SO2R17, A1—NR20C(═O)NR18R19, and A1—SR18; or when y is 0 or when W is not NHR22, G may be A1-heterocyclo, wherein A1 is a bond, C1-6alkylene or C2-alkenylene, A2 is C1-6alkylene or C2-6alkenylene, and A3 is C2-6alkenylene; W is selected from —NR21R22, —OR23, —NR21C(═O)R24, —NR21CO2R24, amidino, guanidino, or a heteroaryl, heterocyclo or C3-7cycloalkyl as defined in the specification, and X and R1 through R24 are as defined in the specification, are effective as modulators of melanocortin-receptors, particularly MC-1R and MC-4R.

公开(公告)号：US06979691B2

公开(公告)日：2005-12-27

申请号：US10090582

申请日：2002-03-04

申请人： Guixue Yu ,  John Macor ,  Timothy Herpin ,  R. Michael Lawrence ,  George C. Morton ,  Rejean Ruel ,  Graham S. Poindexter ,  Edward H. Ruediger ,  Carl Thibault

发明人： Guixue Yu ,  John Macor ,  Timothy Herpin ,  R. Michael Lawrence ,  George C. Morton ,  Rejean Ruel ,  Graham S. Poindexter ,  Edward H. Ruediger ,  Carl Thibault

IPC分类号： C07D233/64 ,  A61K31/4178 ,  A61K31/438 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4747 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/527 ,  A61K31/537 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/55 ,  A61K38/00 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/02 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/14 ,  A61P5/16 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P11/08 ,  A61P13/12 ,  A61P15/00 ,  A61P15/08 ,  A61P15/10 ,  A61P17/00 ,  A61P17/04 ,  A61P17/06 ,  A61P17/14 ,  A61P17/16 ,  A61P19/02 ,  A61P19/10 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P27/16 ,  A61P29/00 ,  A61P31/04 ,  A61P31/06 ,  A61P31/18 ,  A61P31/20 ,  A61P33/06 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D211/32 ,  C07D211/34 ,  C07D211/58 ,  C07D211/60 ,  C07D211/62 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D495/04 ,  C07D498/10 ,  C07K5/06 ,  C07K5/078 ,  A61K31/445

CPC分类号： C07D401/12 ,  A61K38/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D495/04 ,  C07K5/06139 ,  C07K5/06191 ,  Y02A50/411 ,  Y02A50/463

摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is X is N or CH, W is —NR16R17, —NR16C(═O)R22, —NR16CO2R22, —OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.

摘要翻译： 具有式（I）的化合物及其药学上可接受的盐，水合物和前药，其中E是X是N或CH，W是-NR 16 R 17， ，-NR 16 C（-O）R 22，-NR 16 CO 2 R 22 或者如说明书中定义的杂芳基或杂环基，R 1至R 12，R 12， R 17，R 17，R 22，R 23，x，y和z定义如上 说明书可用作黑皮质素受体的调节剂，特别是MC-1R和MC-4R。

公开(公告)号：US06713487B2

公开(公告)日：2004-03-30

申请号：US10090288

申请日：2002-03-04

申请人： Guixue Yu ,  John Macor ,  Timothy Herpin ,  R. Michael Lawrence ,  George C. Morton ,  Rejean Ruel ,  Graham S. Poindexter ,  Edward H. Ruediger ,  Carl Thibault

发明人： Guixue Yu ,  John Macor ,  Timothy Herpin ,  R. Michael Lawrence ,  George C. Morton ,  Rejean Ruel ,  Graham S. Poindexter ,  Edward H. Ruediger ,  Carl Thibault

IPC分类号： A61K31445

CPC分类号： C07D401/12 ,  A61K38/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D495/04 ,  C07K5/06139 ,  C07K5/06191 ,  Y02A50/411 ,  Y02A50/463

摘要： Compounds having the formula (I), —NR11R12; G is a novel side chain selected from C2-6alkenyl, A3-aryl, —OR18, heteroaryl, A1-cyano, A2—OR17, A1—C(═O)R18, A1—CO2R18, A1—C(═O)NR18R19, A1—OC(═O)R18, A1—NR18C(═O)R19, A1—OC(═O)NR18R19, A1—NR18CO2R19, A1—NR18SO2R17, A1—SO2R17, A1—NR20C(═O)NR18R19, and A1—SR18; or when y is 0 or when W is not NHR22, G may be A1-heterocyclo, wherein A1 is a bond, C1-6alkylene or C2-alkenylene, A2 is C1-6alkylene or C2-6alkenylene, and A3 is C2-6alkenylene; W is selected from —NR21R22, —OR23, —NR21C(═O)R24, —NR21CO2R24, amidino, guanidino, or a heteroaryl, heterocyclo or C3-7cycloalkyl as defined in the specification, and X and R1 through R24 are as defined in the specification, are effective as modulators of melanocortin-receptors, particularly MC-1R and MC-4R.

摘要翻译： 具有式（I），-NR 11 R 12的化合物; G是选自C2-6烯基，A3-芳基，-OR18，杂芳基，A1-氰基，A2-OR17，A1-C（= O）R18，A1-CO2R18，A1-C（= O）NR18R19 ，A1-OC（= O）R18，A1-NR18C（= O）R19，A1-OC（= O）NR18R19，A1-NR18CO2R19，A1-NR18SO2R17，A1-SO2R17，A1-NR20C（= O）NR18R19和 A1-SR18; 或当y为0或W不为NHR22时，G可为A1-杂环，其中A1为C1-6亚烷基或C2-亚烯基，A2为C1-6亚烷基或C2-6亚烯基，A3为C2-6亚烯基; W选自-NR 21 R 22，-OR 23，-NR 21 C（= O）R 24，-NR 21 CO 2 R 24，脒基，胍基或如说明书中定义的杂芳基，杂环或C 3-7环烷基，X和R 1至R 24如 该说明书作为黑皮质素受体，特别是MC-1R和MC-4R的调节剂是有效的。

公开(公告)号：US07041692B2

公开(公告)日：2006-05-09

申请号：US10464366

申请日：2003-06-17

申请人： Timothy Herpin ,  Gregory S. Bisacchi ,  Zulan Pi ,  E. Scott Priestley ,  T. G. Murali Dhar

发明人： Timothy Herpin ,  Gregory S. Bisacchi ,  Zulan Pi ,  E. Scott Priestley ,  T. G. Murali Dhar

IPC分类号： A61K31/42 ,  A61K31/41 ,  A61K31/415

CPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/4172 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  C07D233/56 ,  C07D249/08 ,  C07D263/48 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： Methods of treating Factor VIIa-associated conditions in a mammal are described, comprising administering to the mammal in need of treatment thereof an effective amount of at least one compound having the formula (I), or a pharmaceutically-acceptable salt, hydrate or prodrug thereof.

摘要翻译： 描述了治疗哺乳动物中因子VIIa相关病症的方法，包括向需要治疗的哺乳动物施用有效量的至少一种具有式（I）的化合物或其药学上可接受的盐，水合物或前体药物 。

公开(公告)号：US20060173057A1

公开(公告)日：2006-08-03

申请号：US11377104

申请日：2006-03-16

申请人： Timothy Herpin ,  Gregory Bisacchi ,  Zulan Pi ,  E. Priestley

发明人： Timothy Herpin ,  Gregory Bisacchi ,  Zulan Pi ,  E. Priestley

IPC分类号： A61K31/421 ,  C07D263/48 ,  A61K31/422

CPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/4172 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  C07D233/56 ,  C07D249/08 ,  C07D263/48 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： Methods of treating Factor VIIa-associated conditions in a mammal are described, comprising administering to the mammal in need of treatment thereof an effective amount of at least one compound having the formula (I), or a pharmaceutically-acceptable salt, hydrate or prodrug thereof.

公开(公告)号：US20070287713A1

公开(公告)日：2007-12-13

申请号：US11779319

申请日：2007-07-18

申请人： Peter Cheng ,  Sean Chen ,  Pratik Devasthale ,  Charles Ding ,  Timothy Herpin ,  Shung Wu ,  Hao Zhang ,  Wei Wang ,  Xiang-Yang Ye

发明人： Peter Cheng ,  Sean Chen ,  Pratik Devasthale ,  Charles Ding ,  Timothy Herpin ,  Shung Wu ,  Hao Zhang ,  Wei Wang ,  Xiang-Yang Ye

IPC分类号： A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/445 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/505 ,  A61P3/10 ,  C07D239/02 ,  C07D257/00 ,  C07D263/30 ,  C07D271/06 ,  C07D401/02 ,  C07D403/02 ,  C07D413/02

CPC分类号： C07D413/12 ,  C07D413/14

摘要： wherein Z1 is (CH2)q or C═O; Z2 is (CH2)p or C═O; D is —CH═ or C═O or (CH2)m where m is 0, 1, 2 or 3; n=0, 1 or 2; p=1 or 2; q=0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1, where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is —(CH2)x2—O—(CH2)x3— where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4 X5 and X6 is C. R1 is H or alkyl; R2 is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R2a, R2b and R2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R3, E, Z and Y are as defined herein.

公开(公告)号：US06846838B2

公开(公告)日：2005-01-25

申请号：US10464035

申请日：2003-06-17

申请人： William A. Slusarchyk ,  Scott A. Bolton ,  Timothy Herpin ,  Gregory S. Bisacchi ,  Zulan Pi ,  E. Scott Priestley

发明人： William A. Slusarchyk ,  Scott A. Bolton ,  Timothy Herpin ,  Gregory S. Bisacchi ,  Zulan Pi ,  E. Scott Priestley

IPC分类号： A61K31/136 ,  A61K31/4155 ,  A61K31/422 ,  A61K45/06 ,  A61P9/08 ,  C07D263/48 ,  A61K31/44 ,  A61K31/41 ,  A61K31/415 ,  A61K31/42

CPC分类号： C07D263/48 ,  A61K31/136 ,  A61K31/4155 ,  A61K31/422 ,  A61K45/06 ,  A61K2300/00

摘要： Compounds having the formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa.

摘要翻译： 具有式（I）化合物或其药学上可接受的盐，水合物或前体药物作为因子VIIa的抑制剂是有效的。