公开(公告)号：US20070232617A1

公开(公告)日：2007-10-04

申请号：US11752255

申请日：2007-05-22

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Qing Lu ,  Gregory Luedtke ,  Babu Mavunkel ,  John Perumattam ,  Richard Tester

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Qing Lu ,  Gregory Luedtke ,  Babu Mavunkel ,  John Perumattam ,  Richard Tester

IPC: A61K31/497 ,  A61K31/445 ,  C07D401/02 ,  C07D403/02

CPC classification number: C07D401/06 ,  C07D209/18 ,  C07D209/42 ,  C07D401/14 ,  C07D403/06 ,  C07D409/12 ,  C07D409/14

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.

Abstract translation: 本发明涉及使用包含通过哌啶或哌嗪核连接的苯基或噻吩基的化合物与吲哚残基一起抑制p38-α激酶的方法，其中吲哚残基在作为氨基或取代的氨基的环氮上强制取代基 。

公开(公告)号：US07238712B2

公开(公告)日：2007-07-03

申请号：US10156997

申请日：2002-05-28

Applicant: Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

Inventor： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

IPC: A61K31/445 ,  C07D401/06

CPC classification number: C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2–6 Å, and each of i and j is independently 0 or 1; Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0–3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0–4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0–2 wherein the sum of l and k is 0–3; Ar is an aryl group substituted with 0–5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5–24 Å.

Abstract translation: 本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物来抑制p38-α激酶的方法，其中表示单键或双键; 一个Z 2是CA或CR 8 A，另一个是CR 1，CR 1，2， 其中每个R 1，R 6和R 8独立为氢，NR 6，N 6， 或非干扰取代基; A是其中Y是COR 2或其等同体和R 2的-Wi-i-X 氢或非干扰取代基，W和X各自为2-6的间隔基，i和j各自独立地为0或1; Z 3是NR 7或O; 每个R 3独立地是非干扰取代基; n为0-3; L 1和L 2各自为连接体; 每个R 4独立地是非干扰取代基; m为0-4; Z 1是CR 5或N，其中R 5是氢或非干扰取代基; l和k中的每一个是0-2的整数，其中l和k的和为0-3; Ar是被0-5个非直链取代基取代的芳基，其中两个非干扰取代基可以形成稠环; 并且与L 2连接的Ar原子和α环的中心之间的距离为4.5-24埃。

公开(公告)号：US07223766B2

公开(公告)日：2007-05-29

申请号：US10811428

申请日：2004-03-26

Applicant: Sundeep Dugar ,  Sarvajit Chakravarty ,  Aurelia Conte ,  Jonathan Axon ,  Glenn McEnroe ,  Alison Murphy

Inventor： Sundeep Dugar ,  Sarvajit Chakravarty ,  Aurelia Conte ,  Jonathan Axon ,  Glenn McEnroe ,  Alison Murphy

IPC: A61K31/517 ,  C07D239/70

CPC classification number: C07D487/04 ,  A61K31/517 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04

Abstract: Compounds in which a pyrimidine nucleus is bridged at the 5 and 6 position and are further substituted at positions 2 and 4 with substituents comprising aromatic moieties are useful in treating subjects with rheumatoid arthritis ameliorated by inhibition of TGFβ activity.

Abstract translation: 其中嘧啶核在5和6位桥连并且在2和4位被含有芳族部分的取代基进一步取代的化合物可用于治疗通过抑制TGFbeta活性而改善的类风湿关节炎的受试者。

公开(公告)号：US20060281763A1

公开(公告)日：2006-12-14

申请号：US11390980

申请日：2006-03-27

Applicant: Jonathan Axon ,  Sarvajit Chakravarty ,  Barry Hart ,  Glenn McEnroe ,  Alison Murphy ,  Karen Pontius ,  Peijue Sheng ,  Xiaojing Wang ,  Shanthi Yellapregada

Inventor： Jonathan Axon ,  Sarvajit Chakravarty ,  Barry Hart ,  Glenn McEnroe ,  Alison Murphy ,  Karen Pontius ,  Peijue Sheng ,  Xiaojing Wang ,  Shanthi Yellapregada

IPC: C07D403/14 ,  C07D403/02 ,  A61K31/506

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D495/04

Abstract: Certain appropriately substituted forms of pyrimidine having a pyridylamine group at C-4 of the pyrimidine and an amide group on the pyridine ring are useful in the treatment of conditions associated with excessive TGFβ activity.

Abstract translation: 在嘧啶的C-4处具有吡啶基胺基的嘧啶的某些适当取代的形式和吡啶环上的酰胺基可用于治疗与过量TGFbeta活性相关的病症。

公开(公告)号：US20050220784A1

公开(公告)日：2005-10-06

申请号：US11136242

申请日：2005-05-23

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  John Perumattam ,  George Schreiner ,  David Liu ,  John Lewicki

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  John Perumattam ,  George Schreiner ,  David Liu ,  John Lewicki

IPC: A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K39/395 ,  A61P1/16 ,  A61P1/18 ,  A61P7/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D487/02

CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

Abstract: The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

Abstract translation: 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R 3是非干扰性取代基; 每个Z是CR 2或N，其中环A中不超过两个Z位是N，并且其中环A中的两个相邻Z位不能是N; 每个R 2独立地是非干扰取代基; L是连接体; n为0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环脂族，环状杂脂族，芳族或杂芳族部分的残基。