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1. 发明公开

EP0932598A1 ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME 失效
标题翻译： ASPARAT ESTER ALS INHIBITOREN VON INTERLEUKIN-1 BETA-KONVERTIERENDEN ENZYMEN
公开(公告)号：EP0932598A1
公开(公告)日：1999-08-04
申请号：EP97911715.0
申请日：1997-10-09
申请人： WARNER-LAMBERT COMPANY , BASF AKTIENGESELLSCHAFT
发明人： ALBRECHT, Hans, P. , ALLEN, Hamish, John , BRADY, Kenneth, Dale , CAPRATHE, Bradley, William , GILMORE, John, Lodge , HARTER, William, Glen , HAYS, Sheryl, Jeanne , KOSTLAN, Catherine, Rose , LUNNEY, Elizabeth, Ann , PARA, Kimberly, Suzanne , THOMAS, Anthony, Jerome , WALKER, Nigel
IPC分类号： C07D233 , A61K31 , A61K38 , A61P1 , A61P25 , A61P29 , A61P31 , A61P43 , C07C233 , C07C271 , C07C275 , C07C311 , C07C317 , C07C323 , C07C327 , C07D207 , C07D209 , C07D211 , C07D213 , C07D217 , C07D239 , C07D277 , C07D307 , C07D333 , C07K5
CPC分类号： C07D207/08 , A61K38/00 , C07C233/47 , C07C233/51 , C07C271/22 , C07C275/16 , C07C311/03 , C07C311/06 , C07C311/19 , C07C317/04 , C07C317/44 , C07C323/52 , C07C327/32 , C07C2601/10 , C07C2602/10 , C07C2602/42 , C07D207/27 , C07D207/28 , C07D209/08 , C07D209/18 , C07D211/34 , C07D211/76 , C07D213/55 , C07D213/75 , C07D217/24 , C07D233/36 , C07D239/10 , C07D307/79 , C07D333/24 , C07D333/38 , C07D333/54 , C07K5/0202
摘要： The present invention relates to compounds that are inhibitors of interleukin-1β converting enzyme that have formula (I). This invention also relates to a method of treatment of stroke, inflammatory diseases, reperfusion injury, Alzheimer's disease, and shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1β converting enzyme.
摘要翻译：本发明涉及作为具有式（I）的白细胞介素-1β转换酶的抑制剂的化合物。本发明还涉及治疗中风，炎性疾病，再灌注损伤，阿尔茨海默病和志贺氏菌病的方法，以及含有作为白细胞介素-1β转化酶抑制剂的化合物的药学上可接受的组合物。

2. 发明公开

EP1082127A1 SUCCINAMIDE INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME 有权
标题翻译：白细胞介素-1β转化酶的琥珀酰胺抑制剂
公开(公告)号：EP1082127A1
公开(公告)日：2001-03-14
申请号：EP99918930.1
申请日：1999-04-30
申请人： WARNER-LAMBERT COMPANY , BASF Aktiengesellschaft
发明人： CAPRATHE, Bradley, William , GILMORE, John, Lodge , HARTER, William, Glen , HAYS, Sheryl, Jeanne , KNAPP, Kristen, Michele , KOSTLAN, Catherine, Rose , LUNNEY, Elizabeth, Ann , PARA, Kimberly, Suzanne , GALATSIS, Paul , THOMAS, Anthony, Jerome
IPC分类号： A61K38/05 , C07D211/14 , C07D265/28
CPC分类号： C07D257/04 , C07C233/47 , C07C255/29 , C07C311/10 , C07C311/13 , C07C2602/42 , C07D209/16 , C07D213/40 , C07D215/12 , C07D231/56 , C07D233/64 , C07D235/06 , C07D235/08 , C07D249/18 , C07D307/33 , C07D311/14 , C07D405/12
摘要： The present invention provides compounds of Formula (I), pharmaceutical compositions comprising a compound of Formula (I), and methods of treatment of stroke; inflammatory diseases such as rheumatoid arthritis or inflammatory bowel disease; septic shock; reperfusion injury; Alzheimer's disease; shigellosis; and multiple sclerosis.

3. 发明公开

EP0946502A1 SULFONAMIDE INTERLEUKIN-BETA CONVERTING ENZYME INHIBITORS 失效
标题翻译：磺酰胺抑制剂缬氨酸1-BETA-KONVERTIERENDEN-ENZYME
公开(公告)号：EP0946502A1
公开(公告)日：1999-10-06
申请号：EP97910074.0
申请日：1997-10-09
申请人： WARNER-LAMBERT COMPANY
发明人： ALBRECHT, Hans, P. , ALLEN, Hamish, John , BRADY, Kenneth, Dale , HARTER, William, Glen , KOSTLAN, Catherine, Rose , ROTH, Bruce, David , WALKER, Nigel
IPC分类号： A61K31 , A61P9 , A61P19 , A61P25 , A61P29 , A61P31 , A61P43 , C07C311 , C07D217 , C07K5 , A61K38
CPC分类号： C07K5/1024 , A61K38/00 , C07C311/06 , C07C311/19 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07C2603/18 , C07D217/24 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/0804 , C07K5/0812 , C07K5/0815 , C07K5/0819 , C07K5/0821 , C07K5/1005 , C07K5/1016 , C07K5/1019 , C07K5/1021
摘要： The present invention relates to compounds that are inhibitors of interleukin-1β converting enzyme that have the Formula (I). This invention also relates to a method of treatment of stroke, reperfusion injury, Alzheimer's disease, shigellosis, inflammatory diseases, and septic shock and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1β converting enzyme.
摘要翻译：本发明涉及作为具有式（I）的白细胞介素-1β转换酶的抑制剂的化合物。本发明还涉及治疗中风，再灌注损伤，阿尔茨海默病，志贺氏菌病，炎症性疾病和败血性休克的方法以及含有作为白细胞介素-1β转换酶抑制剂的化合物的药学上可接受的组合物。

4. 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.

5. 发明授权

EP0946502B1 SULFONAMIDE INTERLEUKIN-BETA CONVERTING ENZYME INHIBITORS 失效
标题翻译：苏氨酸抑制剂DESILELEKIN-1-BETA KONVERTIERENDEN ENZYMS
公开(公告)号：EP0946502B1
公开(公告)日：2002-12-18
申请号：EP97910074.0
申请日：1997-10-09
申请人： WARNER-LAMBERT COMPANY , Abbott GmbH & Co. KG
发明人： ALBRECHT, Hans, P. , ALLEN, Hamish, John , BRADY, Kenneth, Dale , HARTER, William, Glen , KOSTLAN, Catherine, Rose , ROTH, Bruce, David , WALKER, Nigel
IPC分类号： C07C311/13 , C07C311/24 , C07C311/06 , C07C311/10 , C07K5/062 , C07K5/072 , C07D217/24 , A61K31/18
CPC分类号： C07K5/1024 , A61K38/00 , C07C311/06 , C07C311/19 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07C2603/18 , C07D217/24 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/0804 , C07K5/0812 , C07K5/0815 , C07K5/0819 , C07K5/0821 , C07K5/1005 , C07K5/1016 , C07K5/1019 , C07K5/1021
摘要： The present invention relates to compounds that are inhibitors of interleukin-1β converting enzyme that have the Formula (I). This invention also relates to a method of treatment of stroke, reperfusion injury, Alzheimer's disease, shigellosis, inflammatory diseases, and septic shock and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1β converting enzyme.
摘要翻译：本发明涉及作为具有式（I）的白细胞介素-1β转换酶的抑制剂的化合物。本发明还涉及治疗中风，再灌注损伤，阿尔茨海默病，志贺氏菌病，炎症性疾病和败血性休克的方法以及含有作为白细胞介素-1β转换酶抑制剂的化合物的药学上可接受的组合物。

6. 发明公开

EP0569493A1 SUBSTITUTED 4,6-DI-TERTIARY-BUTYL-5-HYDROXY-PYRIMIDINES 失效
标题翻译：替代物4,6-DI-TERT.BUTYL-5-羟基吡啶。
公开(公告)号：EP0569493A1
公开(公告)日：1993-11-18
申请号：EP92905078.0
申请日：1992-01-17
申请人： WARNER-LAMBERT COMPANY
发明人： BELLIOTTI, Thomas, Richard , CONNOR, David, Thomas , KOSTLAN, Catherine, Rose
IPC分类号： A61K31 , A61P1 , A61P9 , A61P11 , A61P29 , A61P43 , C07D239 , C07D401 , C07D413 , C07D417
CPC分类号： C07D239/36 , C07D239/34 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , Y02P20/55
摘要： L'invention concerne les nouveaux composés 1,2,4- et 1,3,4-thiadiazoles et oxadiazoles ainsi que 1,2,4-triazoles à substitution 4,6-dibutyle tertiaire-5-hydroxy-pyrimidine, ainsi que les additions et leurs sels de base pharmaceutiquement acceptables, des compositions pharmaceutiques les renfermant, ainsi que leurs procédés d'utilisation. On a découvert que les composés de l'invention présentent une activité d'inhibiteur de 5-lipoxygénase et/ou cyclooxygénase offrant une possibilité de traitement par ladite inhibition des troubles tels que l'inflammation, l'arthrite, les douleurs, la fièvre et notamment la polyarthrite rhumatoïde, l'arthrose, d'autres troubles inflammatoires, le psoriasis, des maladies allergiques, l'asthme, les infections intestinales inflammatoires, des ulcères gastro-intestinaux, des troubles cardiovasculaires, y compris la cardiopathie ischémique et l'athérosclérose, ainsi qu'une détérioration des cellules induites par ischémie, notamment une détérioration du cerveau provoquée par une attaque. On peut également les utiliser localement afin de traiter l'acné, les coups de soleil, le psoriasis et l'eczéma. On peut également traiter les troubles pulmonaires, gastro-intestinaux, inflammatoires, dermatologiques et cardiovasculaires induits par leucotriènes. Les composés de l'invention présentent également une utilité potentielle comme anti-oxydants induits par leucotriènes. L'utilisation préférée réside dans le traitement de troubles inflammatoires. Ainsi, l'invention constitue également une composition pharmaceutique ou un procédé de production d'une composition pharmaceutique destinée à être utilisée dans le traitement des troubles pathologiques précités.

7. 发明授权

EP1082127B1 SUCCINAMIDE INHIBITORS OF INTERLEUKIN-1BETA CONVERTING ENZYME 有权
标题翻译： SUCCINAMID HEMMSTOFFE DES INTERLEUKIN-1 BETA KONVERTIERENDEN ENZYMS
公开(公告)号：EP1082127B1
公开(公告)日：2005-06-22
申请号：EP99918930.1
申请日：1999-04-30
申请人： WARNER-LAMBERT COMPANY LLC
发明人： CAPRATHE, Bradley, William , GILMORE, John, Lodge , HARTER, William, Glen , HAYS, Sheryl, Jeanne , KNAPP, Kristen, Michele , KOSTLAN, Catherine, Rose , LUNNEY, Elizabeth, Ann , PARA, Kimberly, Suzanne , GALATSIS, Paul , THOMAS, Anthony, Jerome
IPC分类号： A61K38/05 , C07D211/14 , C07D265/28 , A61P29/00
CPC分类号： C07D257/04 , C07C233/47 , C07C255/29 , C07C311/10 , C07C311/13 , C07C2602/42 , C07D209/16 , C07D213/40 , C07D215/12 , C07D231/56 , C07D233/64 , C07D235/06 , C07D235/08 , C07D249/18 , C07D307/33 , C07D311/14 , C07D405/12

8. 发明授权

EP0652874B1 2-HETEROCYCLIC-5-HYDROXY-1,3-PYRIMIDINES USEFUL AS ANTIINFLAMMATORY AGENTS 失效
标题翻译： 2杂环基-5-羟基-1,3-嘧啶作为抗炎剂的
公开(公告)号：EP0652874B1
公开(公告)日：2003-11-05
申请号：EP93918407.3
申请日：1993-07-27
申请人： WARNER-LAMBERT COMPANY LLC
发明人： CONNOR, David, Thomas , KOSTLAN, Catherine, Rose , UNANGST, Paul, Charles
IPC分类号： C07D403/04 , C07D417/04 , A61K31/505
CPC分类号： C07D403/04 , C07D413/04 , C07D417/04
摘要： The present invention is novel compounds which are 2-heterocyclic-4,6-ditertiarybutyl-5-hydroxy-1,3-pyrimidines, where heterocyclic is selected from imidazole, thiazole, and oxazole, and pharmaceutically acceptable additional salts, bases, and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of, for example, preferably inflammation.

9. 发明公开

EP0652874A1 2-HETEROCYCLIC-5-HYDROXY-1,3-PYRIMIDINES USEFUL AS ANTIINFLAMMATORY AGENTS 失效
标题翻译： 2杂环基-5-羟基-1,3-嘧啶作为抗炎剂是有用的。
公开(公告)号：EP0652874A1
公开(公告)日：1995-05-17
申请号：EP93918407.0
申请日：1993-07-27
申请人： WARNER-LAMBERT COMPANY
发明人： CONNOR, David, Thomas , KOSTLAN, Catherine, Rose , UNANGST, Paul, Charles
IPC分类号： A61K31 , A61P29 , A61P37 , A61P43 , C07D403 , C07D413 , C07D417
CPC分类号： C07D403/04 , C07D413/04 , C07D417/04
摘要： The present invention is novel compounds which are 2-heterocyclic-4,6-ditertiarybutyl-5-hydroxy-1,3-pyrimidines, where heterocyclic is selected from imidazole, thiazole, and oxazole, and pharmaceutically acceptable additional salts, bases, and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of, for example, preferably inflammation.

10. 发明公开

EP0569491A1 2-SUBSTITUTED-4,6-DI-TERTIARY-BUTYL-5-HYDROXY-1,3-PYRIMIDINES USEFUL AS ANTIINFLAMMATORY AGENTS 失效
标题翻译： 2-取代的4,6-二 - 叔丁基-5-羟基-1,3-嘧啶作为抗炎剂是有用的。
公开(公告)号：EP0569491A1
公开(公告)日：1993-11-18
申请号：EP92905024.0
申请日：1992-01-17
申请人： WARNER-LAMBERT COMPANY
发明人： CONNOR, David, Thomas , KOSTLAN, Catherine, Rose
IPC分类号： A61K31 , A61P29 , A61P37 , A61P43 , C07D239 , C07D263 , C07D401 , C07D403 , C07D413 , C07D417
CPC分类号： C07D417/06 , C07D239/34 , C07D263/32 , C07D401/04 , C07D401/06 , C07D403/06 , C07D413/06
摘要： L'invention concerne les nouveaux composés pyrimidines-1,3, hydroxy-5, dibutyle-4,6 tertiaire substituées en position 2 ainsi que leurs sels d'addition ou de base d'acides pharmaceutiquement acceptables, des compositions pharmaceutiques les contenant ainsi que leurs procédés d'utilisation. On a découvert que lesdits composés ont une activité d'inhibiteurs de 5-lipoxygénase et/ou cyclo-oxygénase permettant le traitement d'états que l'on peut améliorer par ladite inhibition, parmi lesquels l'inflammation, l'arthrite, les douleurs, la fièvre et analogues. Ainsi, l'invention constitue également une composition pharmaceutique ou un procédé de production d'une composition pharmaceutique destinée à être utilisée dans le traitement des états précités.

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