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1. 发明授权

US06864260B2 Indole-type derivatives as inhibitors of p38 kinase 有权
标题翻译：吲哚型衍生物作为p38激酶的抑制剂
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。

2. 发明授权

US07238712B2 Indole-type derivatives as inhibitors of p38 kinase 有权
标题翻译：吲哚型衍生物作为p38激酶的抑制剂
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。

3. 发明授权

US07304048B2 Indole-type derivatives as inhibitors of p38 kinase 有权
标题翻译：吲哚型衍生物作为p38激酶的抑制剂
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。

4. 发明授权

US07189726B2 Benzofuran derivatives as inhibitors of p38-α kinase 有权
标题翻译：苯并呋喃衍生物作为p38-α激酶的抑制剂
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。

5. 发明授权

US06867209B1 Indole-type derivatives as inhibitors of p38 kinase 有权
标题翻译：吲哚型衍生物作为p38激酶的抑制剂
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。

6. 发明授权

US07220763B2 Indole-type derivatives as inhibitors of p38 kinase 有权
标题翻译：吲哚型衍生物作为p38激酶的抑制剂
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。

7. 发明授权

US07488744B2 Indole-type derivatives as inhibitors of p38 kinase 有权
标题翻译：吲哚型衍生物作为p38激酶的抑制剂
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。

8. 发明授权

US07345045B2 Pyrido-pyrimidine compounds as medicaments 有权
标题翻译：吡啶 - 嘧啶化合物作为药物
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。

9. 发明授权

US07232824B2 Quinazoline derivatives as medicaments 有权
标题翻译：喹唑啉衍生物作为药物
公开(公告)号：US07232824B2
公开(公告)日：2007-06-19
申请号：US10957183
申请日：2004-09-30
申请人： Sundeep Dugar , Sarvajit Chakravarty , Alison Murphy , Glenn McEnroe , Aurelia Conte , John J. Perumattam
发明人： Sundeep Dugar , Sarvajit Chakravarty , Alison Murphy , Glenn McEnroe , Aurelia Conte , John J. Perumattam
IPC分类号： C07D239/94 , C07D471/04
CPC分类号： C07D471/04 , C07D475/10 , C07D487/04
摘要： Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0–3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5–6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1–C12 alkyl, C1–C12 alkenyl, C1–C12 alkynyl, or aryl C1–C12 alkyl, containing 0–4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are ═O, ═N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.
摘要翻译：喹唑啉衍生物具有下式：或其药学上可接受的盐; 其中Z 5，Z 6，Z 7和Z 8各自为N或CH，并且其中一个或多个两个Z 5，Z 6，Z 7和Z 8是N，并且其中两个相邻的Z位置不能是 N; 其中m和n各自独立地为0-3; 其中R 1独立地是OH，SH，NH 2，OR，SR，NHR，卤素或R卤化物; 其中两个相邻的R 1个基团可以连接形成5-6个成员的脂肪族杂环; 其中R 2独立地是R 1，R 2，R 2卤素，OR-卤素，NH 2，CONH 2或CONHR; 其中R是任选取代的C 1 -C 12烷基，C 1 -C 12 - 烯基，C

10. 发明授权

US06476031B1 Quinazoline derivatives as medicaments 有权
标题翻译：喹唑啉衍生物作为药物
公开(公告)号：US06476031B1
公开(公告)日：2002-11-05
申请号：US09383825
申请日：1999-08-27
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： C07D23994
CPC分类号： C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要： The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; 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R3是不干扰取代基;每个Z是CR2或N，其中环中不超过两个Z位置 A是N，并且其中环A中的两个相邻Z位不能是N;每个R2独立地是非干扰取代基; L是连接基; n是0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环状脂族，环状杂脂族，芳族或杂芳族部分的残基。

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