-
公开(公告)号:US06864260B2
公开(公告)日:2005-03-08
申请号:US10157048
申请日:2002-05-28
申请人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
发明人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
IPC分类号: A61P43/00 , C07D209/24 , C07D401/06 , C07D401/14 , A61K31/495 , C07D403/06
CPC分类号: C07D209/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要: The invention is directed to methods to inhibit p38-α kinase using compounds which contain a phenyl group linked through a piperazine ring to a substituted indole.
摘要翻译: 本发明涉及使用含有通过哌嗪环与取代的吲哚连接的苯基的化合物来抑制p38-α激酶的方法。
-
公开(公告)号:US07238712B2
公开(公告)日:2007-07-03
申请号:US10156997
申请日:2002-05-28
申请人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
发明人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
IPC分类号: A61K31/445 , C07D401/06
CPC分类号: C07D209/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要: 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.
摘要翻译: 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:US07304048B2
公开(公告)日:2007-12-04
申请号:US10156996
申请日:2002-05-28
申请人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
发明人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
IPC分类号: A61K31/55 , C07D223/02 , C07D243/08
CPC分类号: C07D209/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要: The invention is directed to methods to inhibit p38-α kinase using compounds containing an aromatic system coupled through a 7-membered heterocycle to an indole-type system.
摘要翻译: 本发明涉及使用含有通过7-元杂环偶联到吲哚型系统的芳族体系的化合物来抑制p38-α激酶的方法。
-
公开(公告)号:US07189726B2
公开(公告)日:2007-03-13
申请号:US10146703
申请日:2002-05-14
申请人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
发明人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
IPC分类号: A61K31/495 , A61K31/445
CPC分类号: C07D209/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要: The invention is directed to methods to inhibit p38-α kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine.
摘要翻译: 本发明涉及使用含有通过哌啶与苯并呋喃部分偶联的芳香残基的化合物来抑制p38-α激酶的方法。
-
公开(公告)号:US06867209B1
公开(公告)日:2005-03-15
申请号:US09575060
申请日:2000-05-19
申请人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
发明人: Babu J. Mavunkel , Sarvajit Chakravarty , John J. Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
IPC分类号: C07D209/08 , C07D209/24 , C07D235/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D471/04 , A61K31/495 , C07D241/04
CPC分类号: C07D235/06 , C07D209/08 , C07D209/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D471/04
摘要: 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; as 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 1 and k is an integer from 0-2 wherein the sum of 1 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.
摘要翻译: 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抑制p38-α激酶的方法,其中
表示单键或双键;一个Z 2为CA或CR <8> A,另一个为CR <1> ,CR 1,NR 6或N,其中每个R 1,R 6和R 8独立地是氢或非干扰取代基; A是-Wi-COX j Y,其中Y是COR 2或 其等同基团和R 2是氢或非干扰取代基,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为NR 7 >或O;每个R 3独立地为非干扰取代基; n为0-3; L 1和L 2各自为连接基;每个R 4独立地为非干扰取代基; m为0 -4; Z 1是CR 5或N,其中R 5是氢或非干扰取代基; 1和k各自是整数fr om 0-2其中1和k的和为0-3; Ar是被0-5个非干扰取代基取代的芳基,其中两个非干扰取代基可以形成稠环; 并且连接到L 2的Ar原子与α环的中心之间的距离为4.5-24。 -
公开(公告)号:US07220763B2
公开(公告)日:2007-05-22
申请号:US10654840
申请日:2003-09-03
申请人: Sarvajit Chakravarty , Sundeep Dugar , Qing Lu , Gregory R. Luedtke , Babu J. Mavunkel , John J. Perumattam , Richland W. Tester
发明人: Sarvajit Chakravarty , Sundeep Dugar , Qing Lu , Gregory R. Luedtke , Babu J. Mavunkel , John J. Perumattam , Richland W. Tester
IPC分类号: A01N43/64 , A61K31/41 , C07D209/04
CPC分类号: C07D401/06 , C07D209/18 , C07D209/42 , C07D401/14 , C07D403/06 , C07D409/12 , C07D409/14
摘要: 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.
摘要翻译: 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至吲哚残基来抑制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:US07488744B2
公开(公告)日:2009-02-10
申请号:US11752255
申请日:2007-05-22
申请人: Sarvajit Chakravarty , Sundeep Dugar , Qing Lu , Gregory R. Luedtke , Babu J. Mavunkel , John J. Perumattam , Richard Tester
发明人: Sarvajit Chakravarty , Sundeep Dugar , Qing Lu , Gregory R. Luedtke , Babu J. Mavunkel , John J. Perumattam , Richard Tester
IPC分类号: A01N43/64 , A61K31/41 , C07D209/04
CPC分类号: C07D401/06 , C07D209/18 , C07D209/42 , C07D401/14 , C07D403/06 , C07D409/12 , C07D409/14
摘要: 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.
摘要翻译: 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至吲哚残基来抑制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:US20070161649A1
公开(公告)日:2007-07-12
申请号:US11689418
申请日:2007-03-21
申请人: Babu Mavunkel , Sarvajit Chakravarty , John Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
发明人: Babu Mavunkel , Sarvajit Chakravarty , John Perumattam , Sundeep Dugar , Qing Lu , Xi Liang
IPC分类号: A61K31/496 , A61K31/454 , C07D403/02
CPC分类号: C07D209/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要: 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 1 and k is an integer from 0-2 wherein the sum of 1 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.
摘要翻译: 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; 1和k中的每一个是0-2的整数,其中1和k之和为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:US06410540B1
公开(公告)日:2002-06-25
申请号:US09385494
申请日:1999-08-27
申请人: R. Richard Goehring , Gregory R. Luedtke , Babu J. Mavunkel , Sarvajit Chakravarty , Sundeep Dugar , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人: R. Richard Goehring , Gregory R. Luedtke , Babu J. Mavunkel , Sarvajit Chakravarty , Sundeep Dugar , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号: A61K3150
CPC分类号: A61K45/06 , A61K31/00 , A61K31/426 , A61K31/4365 , A61K31/437 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/522 , Y02A50/411
摘要: The invention is directed to methods to treat conditions mediated by p38-&agr;kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein Z is N or CR1, R1 is a noninterfering substituent, each of X1 and X2 is a linker, Ar1 and Ar2 are identical or different, and represent optionally substituted C1-C20 hydrocarbyl residues wherein at least one of Ar1 and Ar2 is an optionally substituted aryl group, with the proviso that when X2 is CH2 or an isostere thereof, X1 is CO or an isostere thereof, and Ar2 is optionally substituted phenyl, Ar1 is other than an optionally substituted indolyl, benzimidazolyl or benzotriazolyl substituent, and wherein said optionally substituted phenyl is not an optionally substituted indolyl, benzimidazolyl, or benzotriazolyl, Y is a noninterfering substituent, wherein n is an integer from 0-4, and wherein m is an integer from 0-4 and 1 is an integer from 0-3.
摘要翻译: 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治疗由p38-阿拉蛋白酶介导的病症的方法,其中Z是N或CR1,R1是不干扰取代基,X1和X2分别是 连接基,Ar 1和Ar 2相同或不同,并且表示任选取代的C 1 -C 20烃基残基,其中Ar 1和Ar 2中的至少一个是任选取代的芳基,条件是当X 2是CH 2或其等同体时,X 1是CO 或其等同物,Ar 2是任选取代的苯基,Ar 1不同于任选取代的吲哚基,苯并咪唑基或苯并三唑基取代基,并且其中所述任选取代的苯基不是任选取代的吲哚基,苯并咪唑基或苯并三唑基,Y是非干扰取代基, 其中n是0-4的整数,其中m是0-4的整数,1是0-3的整数。
-
公开(公告)号:US07345045B2
公开(公告)日:2008-03-18
申请号:US11053121
申请日:2005-02-07
申请人: Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人: Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号: A61K31/4375 , C07D471/04
CPC分类号: C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要: 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.
摘要翻译: 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。
-
-
-
-
-
-
-
-
-