公开(公告)号：US20120122859A1

公开(公告)日：2012-05-17

申请号：US13186078

申请日：2011-07-19

Applicant: Chris Allen Broka ,  David Scott Carter ,  Michael Patrick Dillon ,  Anthony P.D.W. Ford ,  Ronald Charles Hawley ,  Alam Jahangir ,  Amy Geraldine Moore ,  Daniel Warren Parish

Inventor： Chris Allen Broka ,  David Scott Carter ,  Michael Patrick Dillon ,  Anthony P.D.W. Ford ,  Ronald Charles Hawley ,  Alam Jahangir ,  Amy Geraldine Moore ,  Daniel Warren Parish

IPC: A61K31/505 ,  A61P11/00 ,  A61K31/506 ,  A61K31/5383

CPC classification number: A61K31/506 ,  A61K31/505 ,  A61K31/513 ,  A61K31/538 ,  Y10S514/826

Abstract: Methods for treating respiratory and gastrointestinal diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

Abstract translation: 用于治疗由P2X3和/或P2X2 / 3受体拮抗剂介导的呼吸道和胃肠道疾病的方法，所述方法包括向有需要的受试者施用有效量的式（I）化合物或其药学上可接受的盐， 其中D，X，Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。

公开(公告)号：US08008298B2

公开(公告)日：2011-08-30

申请号：US12378977

申请日：2009-02-20

Applicant: Joe Timothy Bamberg ,  Daisy Joe DuBois ,  Todd Richard Elworthy ,  Robert Than Hendricks ,  Johannes Cornelius Hermann ,  Alam Jahangir ,  Rama K. Kondru ,  Remy Lemoine ,  Yan Lou ,  Timothy D. Owens ,  David Bernard Smith ,  Michael Soth ,  Hanbiao Yang

Inventor： Joe Timothy Bamberg ,  Daisy Joe DuBois ,  Todd Richard Elworthy ,  Robert Than Hendricks ,  Johannes Cornelius Hermann ,  Alam Jahangir ,  Rama K. Kondru ,  Remy Lemoine ,  Yan Lou ,  Timothy D. Owens ,  David Bernard Smith ,  Michael Soth ,  Hanbiao Yang

IPC: A61K31/495

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

Abstract translation: 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量Q1，R和X如本文所述定义，其抑制JAK和SYK并且可用于治疗自身免疫和炎性疾病。

公开(公告)号：US07589090B2

公开(公告)日：2009-09-15

申请号：US12072663

申请日：2008-02-27

Applicant: Michael Patrick Dillon ,  Alam Jahangir

Inventor： Michael Patrick Dillon ,  Alam Jahangir

IPC: C07D239/48 ,  A61K31/506

CPC classification number: C07D413/12 ,  C07D239/46 ,  C07D239/48 ,  C07D403/12

Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the compounds being of formula (I): wherein R1, R2, R3 and R4 are as defined herein.

Abstract translation: 用于治疗由P2X3和/或P2X2 / 3受体拮抗剂介导的疾病的化合物和方法，所述化合物具有式（I）：其中R 1，R 2，R 3和R 4如本文所定义。

公开(公告)号：US20070049758A1

公开(公告)日：2007-03-01

申请号：US11510216

申请日：2006-08-25

Applicant: Michael Dillon ,  Alam Jahangir ,  Amy Moore ,  Paul Wagner

Inventor： Michael Dillon ,  Alam Jahangir ,  Amy Moore ,  Paul Wagner

IPC: C07D239/46 ,  C07D403/02

CPC classification number: C07D239/48

Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

Abstract translation: 用于治疗由P2X 3和/或P2X 3/3受体拮抗剂介导的疾病的化合物和方法，所述方法包括向有需要的受试者施用有效量的 式（I）的化合物：其中D，X，R 1，R 2，R 3，R 4， R 5，R 5，R 6，R 7和R 8如本文所定义。

公开(公告)号：US20070049534A1

公开(公告)日：2007-03-01

申请号：US11509890

申请日：2006-08-25

Applicant: Michael Dillon ,  Alam Jahangir ,  Clara Lin

Inventor： Michael Dillon ,  Alam Jahangir ,  Clara Lin

IPC: A61K31/506 ,  A61K31/505 ,  C07K5/04 ,  A61K38/05 ,  A61K38/04 ,  C07D239/48

CPC classification number: C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the compounds being of formula (I): wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

Abstract translation: 用于治疗由P2X 3和/或P2X 3/3受体拮抗剂介导的疾病的化合物和方法，所述式（I）的化合物：其中D，X， R 1，R 2，R 3，R 4，R 5， R 6，R 7和R 8如本文所定义。

公开(公告)号：US07141584B2

公开(公告)日：2006-11-28

申请号：US10731607

申请日：2003-12-09

Applicant: Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

Inventor： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

IPC: A61K31/454 ,  C07D401/12

CPC classification number: C07D401/10 ,  C07D233/50 ,  C07D403/12 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D417/10

Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.

Abstract translation: 本发明涉及选自由式I表示的化合物组的IP受体拮抗剂：其中：R 1是由式（A），（B）或（C）表示的基团; 和说明书中定义的其它取代基及其药学上可接受的盐或晶体形式; 和含有它们的药物组合物; 以及用作治疗剂的方法。

公开(公告)号：US07078401B2

公开(公告)日：2006-07-18

申请号：US10887700

申请日：2004-07-09

Applicant: Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir

Inventor： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir

IPC: A61K31/5377 ,  A61K31/4168 ,  C07D413/12 ,  C07D233/06

CPC classification number: C07D295/096 ,  C07D211/72 ,  C07D233/50 ,  C07D239/14 ,  C07D243/08 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04

Abstract: Methods for treatment of IP antagonist mediated diseases or conditions by administration to a subject in need thereof a compound of formula (I) wherein R1, R2, A and X are as defined herein. Also disclosed are compounds and related compositions.

Abstract translation: 通过给予有需要的受试者治疗IP拮抗剂介导的疾病或病症的方法，其中R 1，R 2，A和X的式（I）化合物是 如本文所定义。 还公开了化合物和相关组合物。

公开(公告)号：US06472536B1

公开(公告)日：2002-10-29

申请号：US09666065

申请日：2000-09-19

Applicant: Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

Inventor： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

IPC: C07D23350

CPC classification number: C07D401/10 ,  C07D233/50 ,  C07D403/12 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D417/10

Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.

Abstract translation: 本发明涉及选自由式I表示的化合物组的IP受体拮抗剂：其中：R1是由式（A），（B）或（C）表示的基团;以及本说明书中定义的其它取代基，它们 药学上可接受的盐或其晶体形式; 和含有它们的药物组合物; 以及用作治疗剂的方法。

公开(公告)号：US06184242B2

公开(公告)日：2001-02-06

申请号：US09137507

申请日：1998-08-20

Applicant: Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

Inventor： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

IPC: A61K314168

CPC classification number: C07D401/10 ,  C07D233/50 ,  C07D403/12 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D417/10

Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.

Abstract translation: 本发明涉及选自由式I表示的化合物组的IP受体拮抗剂：其中：R1是由式（A），（B）或（C）表示的基团;以及本说明书中定义的其它取代基， 药学上可接受的盐或其晶体形式; 和含有它们的药物组合物; 以及用作治疗剂的方法。

公开(公告)号：US08318764B2

公开(公告)日：2012-11-27

申请号：US12884243

申请日：2010-09-17

Applicant: Alam Jahangir ,  Stephen M Lynch ,  Michael Soth ,  Hanbiao Yang

Inventor： Alam Jahangir ,  Stephen M Lynch ,  Michael Soth ,  Hanbiao Yang

IPC: C07D487/18 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61K31/33

CPC classification number: C07D487/18

Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.

Abstract translation: 本发明涉及式I的新型大环化合物的用途，其中变量Q，Q1，Q2，Q3和Q4如本文所述定义，其抑制JAK并且可用于治疗自身免疫和炎性疾病 。