专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 发明申请

WO2002064547A2 ISOPHTHALIC ACID DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：邻苯二甲酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2002064547A2
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000344
申请日：2002-02-04
申请人： WARNER-LAMBERT COMPANY , BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , DYER, Richard, Dennis , JOHNSON, Adam, Richard , PATT, William, Chester
发明人： BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , DYER, Richard, Dennis , JOHNSON, Adam, Richard , PATT, William, Chester
IPC分类号： C07C235/60
CPC分类号： C07D213/30 , C07C69/80 , C07C69/90 , C07C69/92 , C07C229/60 , C07C233/66 , C07C233/69 , C07C233/73 , C07C233/75 , C07C233/78 , C07C235/60 , C07D285/14 , C07D317/54 , C40B50/14
摘要： Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula (I) wherein: R 1 , R 2 , and R 3 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 ; each 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, optionally containing heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.
摘要翻译：选择性MMP-13抑制剂是式（I）的间苯二甲酸衍生物，其中：R 1，R 2和R 4独立地选自： 3独立地为氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6烷氧基，C 2 -C 6链烯基，C 2 -C 6炔基，NO

4. 发明申请

WO2002064571A1 PYRIMIDINE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：哌嗪基金属蛋白酶抑制剂
公开(公告)号：WO2002064571A1
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000190
申请日：2002-01-18
申请人： WARNER-LAMBERT COMPANY , BARVIAN, Nicole, Chantel , PATT, William, Chester
发明人： BARVIAN, Nicole, Chantel , PATT, William, Chester
IPC分类号： C07D239/28
CPC分类号： C07D239/28 , A61K31/505 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Selective MMP-13 inhibitors are pyrimidine derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R 2 is 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, (CH2)n aryl, (CH 2 )n cycloalkyl, (CH2)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）的嘧啶衍生物或其药学上可接受的盐，其中R 2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 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。

5. 发明申请

WO2004052373A1 BENZOXAZIN-3-ONES AND DERIVATIVES THEREOF AS INHIBITORS OF PI3K 审中-公开
标题翻译：作为PI3K的抑制剂的苯并恶嗪-3-酮及其衍生物
公开(公告)号：WO2004052373A1
公开(公告)日：2004-06-24
申请号：PCT/IB2003/005451
申请日：2003-11-25
申请人： WARNER-LAMBERT COMPANY LLC , BARVIAN, Nicole, Chantel , KOLZ, Christine, Nylund , PARA, Kimberly, Suzanne , PATT, William, Chester , VISNICK, Melean
发明人： BARVIAN, Nicole, Chantel , KOLZ, Christine, Nylund , PARA, Kimberly, Suzanne , PATT, William, Chester , VISNICK, Melean
IPC分类号： A61K31/538
CPC分类号： C07D413/06 , C07D405/06 , C07D413/14 , C07D417/06 , C07D417/14
摘要： The present invention provides compounds of Formula (I) wherein W, Q, E, D, R 6 , R 7 , R 8 , Y, K, R 9 , R 1O , R 12 , G, and the double bond denoted "*" have any of the values defined therefore 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). The compounds are inhibitors of phosphoinsitide-3-kinase (P13K).
摘要翻译：本发明提供式（I）化合物，其中W，Q，E，D，R 6，R 7，R 8，Y，K，R 9，R 10， 12＆gt;，G所示的双键，并且表示为“*”的双键具有在本说明书中定义的任何值及其药学上可接受的盐，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。还提供了包含一种或多种式（I）化合物的药物组合物。这些化合物是磷酸三磷酯-3-激酶（P13K）的抑制剂。

6. 发明申请

WO1995005376A1 SUBSTITUTED 2(5H)FURANONE, 2(5H)THIOPHENONE AND 2(5H)PYRROLONE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS ENDOTHELIN ANTAGONISTS 审中-公开
标题翻译：取代2（5H）呋喃酮，2（5H）噻吩酮和2（5H）吡咯烷酮衍生物，其制备及其用作内皮素拮抗剂
公开(公告)号：WO1995005376A1
公开(公告)日：1995-02-23
申请号：PCT/US1994009091
申请日：1994-08-09
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BERRYMAN, Kent, Alan , DOHERTY, Annette, Marian , EDMUNDS, Jeremy, John , PATT, William, Chester , PLUMMER, Mark, Stephen , REPINE, Joseph, Thomas
IPC分类号： C07D407/04
CPC分类号： C07D405/04 , C07C45/41 , C07C45/71 , C07C45/74 , C07C47/11 , C07C47/235 , C07C47/575 , C07C49/813 , C07C49/84 , C07C59/90 , C07D307/60 , C07D405/06 , C07D405/14 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D409/14
摘要： Compounds of formula (I), or a tautomeric open chain keto-acid form thereof or a pharmaceutically acceptable salt thereof wherein: R1 is alkyl substituted or unsubstituted, straight, or branched, of from 1 to 12 carbon atoms, cycloalkyl substituted or unsubstituted of from 3 to 12 carbon atoms, phenyl substituted with from 1 to 5 substituents, naphthyl unsubstituted or substituted with from 1 to 5 substituents, or heteroaryl unsubstituted or substituted with from 1 to 5 substituents; R2 is alkyl substituted or unsubstituted, straight, or branched of from 1 to 12 carbon atoms, cycloalkyl substituted or unsubstituted of from 3 to 12 carbon atoms, aryl which is unsubstituted or substituted with from 1 to 5 substituents, heteroaryl wich is unsubstituted or substituted with from 1 to 3 substituents; R3 is alkyl substituted or unsubstituted, straight, or branched, of from 1 to 12 carbon atoms, cycloalkyl substituted or unsubstituted of from 3 to 12 carbon atoms, aryl which is unsubstituted or substituted with from 1 to 5 substituents, heteroaryl which is unsubstituted or substituted with from 1 to 3 substituents; R4 is hydrogen, hydroxy, halogen, SR5, OR5 wherein R5 is alkyl or substituted alkyl of from 1 to 7 carbon atoms, NR6R7 wherein R6 and R7 are each independently hydrogen, alkyl, substituted alkyl, substituted or unsubstituted phenyl, and (CH2)nOR5 wherein n is an integer of from 1 to 3; X is oxygen, S or NR8 wherein R8 is hydrogen, alkyl or substituted alkyl with the proviso that when R1 is monosubstituted phenyl and the substituent is p-methoxy, R3 is not unsubstituted phenyl, monosubstituted phenyl, or mesityl and with the further proviso when R2 is alkyl substituted, the substituent is not oxygen at the alpha -position to the furanone ring and with the further proviso that R1 and R3 are not both alkyl or alkyl substituted in the same molecule, their use as nonpeptide antagonists of endothelin I, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, and diabetes.
摘要翻译：式（I）化合物或其互变异构开环酮酸形式或其药学上可接受的盐，其中：R 1为烷基取代或未取代的，直链或支链的1至12个碳原子，取代或未取代的 3至12个碳原子，被1至5个取代基取代的苯基，未取代或被1至5个取代基取代的萘基，或未取代或被1至5个取代基取代的杂芳基; R 2是具有1至12个碳原子的烷基取代或未取代的，直链或支链的，取代或未取代的3至12个碳原子的环烷基，未被取代或被1至5个取代基取代的芳基，未取代或取代的杂芳基具有1至3个取代基; R3是具有1至12个碳原子的烷基取代或未取代的，直链或支链的，取代或未取代的3-12个碳原子的环烷基，未被取代或被1至5个取代基取代的芳基，未取代的或未被取代的杂芳基被1至3个取代基取代; R4是氢，羟基，卤素，SR5，OR5，其中R5是1或7个碳原子的烷基或取代的烷基，NR6R7，其中R6和R7各自独立地是氢，烷基，取代的烷基，取代或未取代的苯基和（CH2） nOR5其中n是1至3的整数; X是氧，S或NR8，其中R8是氢，烷基或取代的烷基，条件是当R 1是单取代的苯基且取代基是对甲氧基时，R 3不是未取代的苯基，单取代的苯基或者均三甲基，进一步的条件是 R2是烷基取代的，取代基不是位于呋喃酮环的α-位上的氧，另外条件是R 1和R 3不在同一分子中被烷基或烷基取代，它们作为内皮素I的非肽拮抗剂用作以及其制备方法及其药物组合物，其可用于治疗升高的内皮素水平，急性和慢性肾衰竭，高血压，心肌梗死，心肌缺血，脑血管痉挛，脑缺血，脑梗塞，肝硬化，败血性休克，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病，胃粘膜损伤，出血性休克，缺血性肠病，中风和糖尿病。

7. 发明公开

EP1294687A2 1,2,4-TRISUBSTITUTED BENZENES AS INHIBITORS OF 15-LIPOXYGENASE 审中-公开
标题翻译： 1,2,4-三取代奔驰衍生物及其作为脂氧合酶抑制剂15
公开(公告)号：EP1294687A2
公开(公告)日：2003-03-26
申请号：EP01935151.9
申请日：2001-05-08
申请人： WARNER-LAMBERT COMPANY
发明人： BARVIAN, Nicole, Chantel , O'BRIAN, Patrick, Michael , PATT, William, Chester , PICARD, Joseph, Armand , SLISKOVIC, Drago, Robert
IPC分类号： C07D209/14 , C07D333/16 , C07D213/30 , C07D209/48 , C07D295/088 , C07D295/08 , A61K31/33 , A61P43/00
CPC分类号： C07D209/48 , C07D209/14 , C07D213/30 , C07D295/088 , C07D333/16
摘要： The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.

8. 发明授权

EP1368323B1 PYRIMIDINE MATRIX METALLOPROTEINASE INHIBITORS 有权
标题翻译： PYRIMIDINMATRIXMETALLOPROTEINASEINHIBITOREN
公开(公告)号：EP1368323B1
公开(公告)日：2010-06-30
申请号：EP02740096.9
申请日：2002-01-18
申请人： Warner-Lambert Company LLC
发明人： BARVIAN, Nicole, Chantel , PATT, William, Chester
IPC分类号： C07D239/28 , A61K31/505 , C07D405/12 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61P19/02
CPC分类号： C07D239/28 , A61K31/505 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Selective MMP-13 inhibitors are pyrimidine derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen, halo, hydroxy, C¿1?-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR?4 R5¿, CN, or CF¿3?; E is independently O or S; A and B independently are OR?4 or NR4R5; R4 and R5¿ independently are H, C¿1?-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R?4 and R5¿ 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.

9. 发明公开

EP1368323A1 PYRIMIDINE MATRIX METALLOPROTEINASE INHIBITORS 有权
标题翻译：嘧啶基质金属蛋白酶抑制剂
公开(公告)号：EP1368323A1
公开(公告)日：2003-12-10
申请号：EP02740096.9
申请日：2002-01-18
申请人： Warner-Lambert Company LLC
发明人： BARVIAN, Nicole, Chantel , PATT, William, Chester
IPC分类号： C07D239/28 , A61K31/505 , C07D405/12 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61P19/02
CPC分类号： C07D239/28 , A61K31/505 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Selective MMP-13 inhibitors are pyrimidine derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen, halo, hydroxy, C¿1?-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR?4 R5¿, CN, or CF¿3?; E is independently O or S; A and B independently are OR?4 or NR4R5; R4 and R5¿ independently are H, C¿1?-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R?4 and R5¿ 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）的嘧啶衍生物或其药学上可接受的盐，其中R 2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， C6炔基，NO2，NR4R5，CN或CF3; E独立地是O或S; A和B独立地是OR 4或NR 4 R 5; R4和R5独立地为H，C1-C6烷基，C2-C6烯基，C2-C6炔基，（CH2）n芳基，（CH2）n环烷基，（CH2）n杂芳基或R4和R5 当与它们所连接的氮一起形成含有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被取代的3-至8-元环时; n是0到6。

10. 发明公开

EP1368324A1 QUINAZOLINES AS MMP-13 INHIBITORS 审中-公开
标题翻译：喹唑啉AS MMP-13抑制剂
公开(公告)号：EP1368324A1
公开(公告)日：2003-12-10
申请号：EP02722137.3
申请日：2002-02-11
申请人： Warner-Lambert Company LLC
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 , C07D401/12 , C07D405/12 , C07D409/12 , C07D405/14 , C07D409/14 , C07D471/04 , C07D403/12 , C07D403/10 , A61K31/5025 , A61K31/505
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: R1 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, X1, X2 and X3 represent nitrogen or -C-R6 in which R6 is as defined in the description, Y represents oxygen, sulphur, -NH, or -N(C1-C6)alkyl, Z represents oxygen, sulphur, -NR7 in which R7 is as defined in the description, and optionally carbon atom, n is an integer from 1 to 8 inclusive, Z1 represents -CR8R9 wherein R8 and R9 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) R2 is (are) is as defined in the description, R3 represents hydrogen, alkyl, alkenyl, alkynyl, or a group of formula: in which Z2, B, R5, 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.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式