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1. 发明申请

WO2002064568A1 PYRIDINE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：吡啶基金属蛋白酶抑制剂
公开(公告)号：WO2002064568A1
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000345
申请日：2002-02-04
申请人： WARNER-LAMBERT COMPANY , BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , O'BRIEN, Patrick, Michael , ORTWINE, Daniel, Fred , PATT, William, Chester , SHULER, Kevon, Ray , WILSON, Michael, William
发明人： BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , O'BRIEN, Patrick, Michael , ORTWINE, Daniel, Fred , PATT, William, Chester , SHULER, Kevon, Ray , WILSON, Michael, William
IPC分类号： C07D213/80
CPC分类号： C07D213/80 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Selective MMP-13 inhibitors are pyridine derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: R 1 and R 2 independently are hydrogen, halo, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, NO 2 , NR 4 R 5 , CN, or CF 3 ; E is independently O or S; A and B independently are OR 4 or NR 4 R 5 ; R 4 and R 5 independently are H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, (CH 2 ) n aryl, (CH 2 ) n cycloalkyl, (CH 2 ) n heteroaryl, or R 4 and R 5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6.
摘要翻译：选择性MMP-13抑制剂是式（I）的吡啶衍生物或其药学上可接受的盐，其中：R 1和R 2独立地是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基， C 2 -C 6烯基，C 2 -C 6炔基，NO 2，NR 4 R 5，CN或CF 3; E独立地为O或S; A和B分别是OR 4或NR 4 R 5; R 4和R 5独立地是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，（CH 2）n芳基，（CH 2）n环烷基，（CH 2）n杂芳基或R 4 和R 5与它们所连接的氮原子一起形成含有3至8元环的碳原子并且任选地含有选自O，S或NH的杂原子，并且任选地被取代或未取代; n为0〜6。

2. 发明申请

WO2002064572A1 QUINAZOLINES AS MMP-13 INHIBITORS 审中-公开
标题翻译：喹唑啉作为MMP-13抑制剂
公开(公告)号：WO2002064572A1
公开(公告)日：2002-08-22
申请号：PCT/EP2002/001979
申请日：2002-02-11
申请人： WARNER-LAMBERT COMPANY , ANDRIANJARA, Charles , CHANTEL-BARVIAN, Nicole , GAUDILLIERE, Bernard , JACOBELLI, Henri , ORTWINE, Daniel, Fred , PATT, William, Chester , PHAM, Ly , KOSTLAN, Catherine, Rose , WILSON, Michael, William
发明人： ANDRIANJARA, Charles , CHANTEL-BARVIAN, Nicole , GAUDILLIERE, Bernard , JACOBELLI, Henri , ORTWINE, Daniel, Fred , PATT, William, Chester , PHAM, Ly , KOSTLAN, Catherine, Rose , WILSON, Michael, William
IPC分类号： C07D239/96
CPC分类号： C07D401/06 , A61K31/517 , A61K31/519 , A61K31/525 , C07D239/95 , C07D239/96 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D471/04
摘要： A compound selected from those of formula (I): in which: R 1 represents a group selected from hydrogen, amino, alkyl, alkenyl, aminoalkyl, aryl, arylalkyl, heterocycle, and cycloalkylalkyl, optionally substituted, W represents oxygen, sulphur, or =N-R', in which R' is as defined in the description, X 1 , X 2 and X 3 represent nitrogen or -C-R 6 in which R 6 is as defined in the description, Y represents oxygen, sulphur, -NH, or -N(C 1 -C 6 )alkyl, Z represents oxygen, sulphur, -NR 7 in which R 7 is as defined in the description, and optionally carbon atom, n is an integer from 1 to 8 inclusive, Z 1 represents -CR 8 R 9 wherein R 8 and R 9 are as defined in the description, A represents aromatic or non-aromatic, heterocyclic or non-heterocyclic ring system, m is an integer from 0 to 7 inclusive, the group(s) R 2 is (are) is as defined in the description, R 3 represents hydrogen, alkyl, alkenyl, alkynyl, or a group of formula: in which Z 2 , B, R 5 , P and q are as defined in the description, optionally, the racemic forms thereof, isomers thereof, N-oxydes thereof, and the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.
摘要翻译：选自式（I）的化合物：其中：R1表示选自氢，氨基，烷基，烯基，氨基烷基，芳基，芳基烷基，杂环和环烷基烷基的基团，任选取代的W表示氧，硫或= N-R'，其中R'如说明书中所定义，X 1，X 2和X 3表示氮或-C-R 6，其中R 6如说明书中所定义，Y表示氧，硫，-NH或-N （C 1 -C 6）烷基，Z表示氧，硫，-NR 7，其中R 7如说明书中所定义，并且任选地为碳原子，n为1-8以下的整数，Z1表示-CR8R9，其中R8和R9为 A描述芳族或非芳族，杂环或非杂环环系，m是0至7的整数，包括端值在内，R2是（是）如说明书中所定义，R 3表示氢，烷基，烯基，炔基或下式的基团：其中Z2，B，R5，P和q如说明书中所定义，任选地，外消旋其形式，其异构体，N-氧化物及其药学上可接受的盐，以及含有它们的药物可用作13型基质金属蛋白酶的特异性抑制剂。

3. 发明申请

WO2004014366A1 HETERO BIARYL DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： HETERO BIARYL衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2004014366A1
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003616
申请日：2003-08-03
申请人： WARNER-LAMBERT COMPANY LLC , BUNKER, Amy, Mae , MORRIS, Mark, Anthony , O'BRIEN, Patrick, Michael , WILSON, Michael, William
发明人： BUNKER, Amy, Mae , MORRIS, Mark, Anthony , O'BRIEN, Patrick, Michael , WILSON, Michael, William
IPC分类号： A61K31/41
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/10 , C07D271/107 , C07D285/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/12 , C07D409/06 , C07D413/10 , C07D417/10 , C07D417/12
摘要： This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R l , Q, S, T, U, V, and R 2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a' pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a' compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency,,inflammatory bowel, disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically, acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active, component as described in the specification.
摘要翻译：本发明提供由式I定义的化合物或其药学上可接受的盐，其中R 1，Q，S，T，U，V和R 2如说明书中所定义。本发明还提供包含本说明书中定义的式I化合物或其药学上可接受的盐以及“药学上可接受的载体，稀释剂或赋形剂”的药物组合物。本发明还提供了在动物中抑制MMP-13酶的方法，包括向动物施用式I化合物或其药学上可接受的盐。本发明还提供了治疗由患者中的MMP-13酶介导的疾病的方法，包括单独或在药物组合物中向患者施用“式I化合物或其药学上可接受的盐。本发明还提供治疗诸如心脏病，多发性硬化，骨关节炎和类风湿性关节炎，除了骨关节炎或类风湿性关节炎之外的关节炎，心功能不全，炎性肠病，疾病，心力衰竭，年龄相关性黄斑变性，慢性阻塞性肺疾病，哮喘，牙周疾病，牛皮癣，动脉粥样硬化和骨质疏松症，其包括向患者施用单独或药物组合物中的式I化合物或其药学上可接受的盐。本发明还提供了包含式I化合物或其药学上可接受的盐以及说明书中描述的另一种药学活性成分的组合。

4. 发明申请

WO2004007469A1 NEW ALKYNYLATED QUINAZOLIN COMPOUNDS AS MMP-13 INHIBITORS 审中-公开
标题翻译：新的烷基喹唑啉化合物作为MMP-13抑制剂
公开(公告)号：WO2004007469A1
公开(公告)日：2004-01-22
申请号：PCT/EP2002/008475
申请日：2002-07-12
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , WILSON, Michael, William , PICARD, Joseph, Armand
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , WILSON, Michael, William , PICARD, Joseph, Armand
IPC分类号： C07D239/96
CPC分类号： C07D231/12 , C07D233/56 , C07D239/96 , C07D249/08 , C07D403/06 , C07D471/04 , C07D487/04 , C07F7/1856
摘要： A compound selected from those of formula (I) wherein W¿1? represents O, S, or -NR¿3? in which R¿3? represents hydrogen, alkyl, OH or CN; W¿2? represents a group selected from hydrogen, CF¿3?, NH¿2?, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W¿1? and W¿2? form together a group of formula -N=X¿4?-W¿3?- as defined in the description, X¿1?, X¿2? and X¿3? represent N or C optionally substituted, n is 0 to 8, Z represents -CR¿12?R¿13?, wherein R¿12? and R¿13? are as defined in the description, A represents a ring system, the groups R¿2? represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R¿1? represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.
摘要翻译：选自式（I）的化合物，其中W 1表示O，S或-NR 3，其中R？3？表示氢，烷基，OH或CN; W¿2？表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳烷基，环烷基烷基，杂环，这些基团任选取代的基团，或W 1 和W？2？形成一组式-N = X-4'-W 3' - 如说明书中所定义的X 1，X 2，和X？3？表示N或C任选取代，n为0至8，Z表示-CR 12 R 13，其中R 12，和R ?? 13？如在描述中所定义的，A代表一个环系，R = 表示如描述中定义的氢或各种化学基团，q为0至7; R¿1？代表氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用作特异性抑制剂 13型基质金属蛋白酶。

5. 发明申请

WO2003033478A1 ALKYNYLATED FUSED RING PYRIMIDINE COMPOUNDS AS MATRIX METALLOPROTEASE-13 INHIBITORS 审中-公开
标题翻译：作为基质METALLOPROTEASE-13抑制剂的烷基化的环烯丙基化合物
公开(公告)号：WO2003033478A1
公开(公告)日：2003-04-24
申请号：PCT/EP2002/012194
申请日：2002-10-11
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , WILSON, Michael, William , PICARD, Joseph, Armand
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , WILSON, Michael, William , PICARD, Joseph, Armand
IPC分类号： C07D239/96
CPC分类号： C07D231/12 , A61K31/517 , C07D233/56 , C07D239/96 , C07D249/08 , C07D403/06 , C07D471/04 , C07D487/04 , C07F7/1856
摘要： A compound selected from those of formula (I), wherein W 1 represents O, S, or -NR 3 in which R 3 represents hydrogen, alkyl, OH or CN; W 2 represents a group selected from hydrohen, CF 3 , NH 2 , monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W 1 and W 2 form together a group of formula -N=X 4 -W 3 - as defined in the description, X 1 , X 2 and X 3 represent N or C optionally substituted, n is 0 to 8, Z represents -CR 12 R 13 , wherein R 12 and R 13 are as defined in the description, A represents a ring system, the groups R 2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R 1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.
摘要翻译：选自式（I）的化合物，其中W 1表示O，S或-NR 3，其中R 3表示氢，烷基，OH或CN; W2代表选自氢化物，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基，环烷基烷基，杂环，这些基团任选取代的基团，或者W1和W2一起形成式-N = X4 -W3-如说明书中所定义，X 1，X 2和X 3表示N或C任选取代，n为0至8，Z表示-CR 12 R 13，其中R 12和R 13如说明书中所定义，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用作特异性抑制剂的13型基质金属蛋白酶。

6. 发明申请

WO2004108715A1 3-ARYLOXY AND 3-HETEROARYLOXY SUBSTITUTED BENZO(B) THIOPHENES AS THERAPEUTIC AGENTS WITH PI3K ACTIVITY 审中-公开
标题翻译： 3-ARYLOXY和3-HETEROARYLOXY取代的苯甲（B）THIOPHENES作为具有PI3K活性的治疗药物
公开(公告)号：WO2004108715A1
公开(公告)日：2004-12-16
申请号：PCT/IB2004/001823
申请日：2004-06-04
申请人： WARNER-LAMBERT COMPANY LLC , BRUENDL, Michelle, Marie , CONNOLLY, Michael, Kevin , GOODMAN, Annise Paige , GOGLIOTTI, Rocco, Dean , LEE, Helen, Tsenwhei , PLUMMER, Mark, Stephen , SEXTON, Karen, Elaine , SHAHRIPOUR, Aurash, Bavarsad , REICHARD, Gregory, Adam , VISNICK, Melean , WILSON, Michael, William
发明人： BRUENDL, Michelle, Marie , CONNOLLY, Michael, Kevin , GOODMAN, Annise Paige , GOGLIOTTI, Rocco, Dean , LEE, Helen, Tsenwhei , PLUMMER, Mark, Stephen , SEXTON, Karen, Elaine , SHAHRIPOUR, Aurash, Bavarsad , REICHARD, Gregory, Adam , VISNICK, Melean , WILSON, Michael, William
IPC分类号： C07D409/12
CPC分类号： C07D409/12 , C07D409/14
摘要： The present invention provides benzo[b]thiophenes of Formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , and L have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (I).
摘要翻译：本发明提供式（I）的苯并[b]噻吩，其中R 1，R 2，R 3，R 4，R 5和L具有为此定义的任何值在本说明书及其药学上可接受的盐中，其可用作治疗疾病和病症（包括炎性疾病，心血管疾病和癌症）的药剂。还提供了包含一种或多种式（I）化合物的药物组合物。

7. 发明申请

WO2004014916A1 PYRIMIDINE FUSED BICYCLIC METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：双嘧达莫熔融双相金属蛋白酶抑制剂
公开(公告)号：WO2004014916A1
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003570
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , WILSON, Michael, William
发明人： WILSON, Michael, William
IPC分类号： C07D487/04
CPC分类号： C07D401/12 , C07D239/70 , C07D473/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula (I), wherein A, B, X, Y, and R?1¿ are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.
摘要翻译：本发明涉及式（I）的稠合双环金属蛋白酶抑制剂，其中A，B，X，Y和R 1如说明书中所定义，以及治疗关节炎，炎症，癌症的药物组合物和方法和其他疾病。

8. 发明申请

WO2004014923A1 PYRIMIDINONE FUSED BICYCLIC METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： PYRIMIDINONE熔融双金属金属蛋白酶抑制剂
公开(公告)号：WO2004014923A1
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003522
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , PICARD, Joseph, Armand , WILSON, Michael, William
发明人： PICARD, Joseph, Armand , WILSON, Michael, William
IPC分类号： C07D513/04
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention relates to fused bicyclic metal loproteinase inhibitors of the formula (I), wherein A, B, X, Y, and R' are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.
摘要翻译：本发明涉及式（I）的稠合双环金属蛋白酶抑制剂，其中A，B，X，Y和R'如说明书中所定义，以及治疗关节炎，炎症，癌症和其他疾病。

9. 发明申请

WO2004014908A1 HETEROBICYLCIC METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：异种金属蛋白酶抑制剂
公开(公告)号：WO2004014908A1
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003478
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , WILSON, Michael, William
发明人： WILSON, Michael, William
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D513/04
摘要： The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula (I) wherein ring B is selected from the group consisting of: and A, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.
摘要翻译：本发明涉及式（I）的稠合双环金属蛋白酶抑制剂，其中环B选自：（II），（III），（IV），（V）和A，X，Y和R1 如本说明书中所定义，以及治疗关节炎，炎症，癌症和其它疾病的药物组合物和方法。

10. 发明申请

WO2004014375A2 FUSED BICYCLIC METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：融合双环金属蛋白酶抑制剂
公开(公告)号：WO2004014375A2
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003523
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , WILSON, Michael, William
发明人： WILSON, Michael, William
IPC分类号： A61K31/437
CPC分类号： C07D495/04 , C07D513/04
摘要： The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula, Formula (I), wherein A, B, X, Y, and R 1 are as defined in the specification, and to pharmaceutical compositions and methods of threating arthritis, inflammation, cancer and other disorders.
摘要翻译：本发明涉及式（I）的稠合双环金属蛋白酶抑制剂，其中A，B，X，Y和R 1如上定义的式说明书以及涉及关节炎，炎症，癌症和其他疾病的药物组合物和方法。

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