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1. 发明授权

EP1326853B1 THIADIAZOLES AND OXADIAZOLES AND THEIR USE AS PHOSPHODIESTERASE-7 INHIBITORS 有权
标题翻译：噻二唑，恶二唑和及其作为抑制剂磷酸二酯酶7
公开(公告)号：EP1326853B1
公开(公告)日：2005-09-07
申请号：EP01969804.2
申请日：2001-10-01
申请人： Warner-Lambert Company LLC
发明人： VERGNE, Fabrice , DUCROT, Pierre , ANDRIANJARA, Charles , BERNARDELLI, Patrick , LORTHIOIS, Edwige
IPC分类号： C07D285/135 , C07D271/113 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D453/02 , A61K31/433 , A61K31/55 , A61K31/439 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61P29/00 , A61P37/00
CPC分类号： C07D285/135 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/02
摘要： The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following formula (I):in which, Y is S or O,R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted,R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted,R3 is X2-R'3, in which X2 is a binding group and R'3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted,or their pharmaceutically acceptable derivatives,the process for their preparation and their use for the manufacture of a medicament for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.

2. 发明公开

EP1361873A2 MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： MATRIX-金属蛋白酶缝边
公开(公告)号：EP1361873A2
公开(公告)日：2003-11-19
申请号：EP02710275.5
申请日：2002-02-13
申请人： Warner-Lambert Company LLC
发明人： ANDRIANJARA, Charles , ORTWINE, Daniel, Fred , PAVLOVSKY, Alexander, Gregory , ROARK, William, Howard
IPC分类号： A61K31/16 , A61K31/36 , A61K31/41 , A61K31/44 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/54 , A61P19/00 , C07C233/00 , C07D213/02 , C07D239/02 , C07D239/72 , C07D285/14 , C07D285/22 , C07D317/44 , C07D401/02 , C07D417/02 , C07D495/02
CPC分类号： C07D471/04 , A61K31/00 , C07C235/60 , C07D213/30 , C07D213/40 , C07D239/96 , C07D285/14 , C07D285/24 , C07D285/32 , C07D317/54 , C07D317/58 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/12 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Compounds are provided that bind allosterically to the catalytic domain of MMP-13 and comprise a hydrophobic group, first and second hydrogen bond acceptors and at least one, and preferably both, of a third hydrogen bond acceptor and a second hydrophobic group. Cartesian coordinates for centroids of the above features are defined in the specification. When the ligand binds to MMP-13, the first, second and third (when present) hydrogen bond acceptors bond respectively with Thr245, Thr247 and Met 253, the first hydrophobic group locates within the S1' channel of MMP-13 and the second hydrophobic group (when present) is relatively open to solvent. The compounds specifically inhibit the matrix metalloproteinase-13 enzyme and thus are useful for treating diseases resulting from tissue breakdown, such as heart disease, multiple sclerosis, arthritis, atherosclerosis, and osteoporosis.

3. 发明公开

EP1326853A1 NEW THIADIAZOLES AND OXADIAZOLES AND THEIR USE AS PHOSPHODIESTERASE-7 INHIBITORS 有权
标题翻译：噻二唑，恶二唑和及其作为抑制剂磷酸二酯酶7
公开(公告)号：EP1326853A1
公开(公告)日：2003-07-16
申请号：EP01969804.2
申请日：2001-10-01
申请人： Warner-Lambert Company LLC
发明人： VERGNE, Fabrice , DUCROT, Pierre , ANDRIANJARA, Charles , BERNARDELLI, Patrick , LORTHIOIS, Edwige
IPC分类号： C07D285/135 , C07D271/113 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D453/02 , A61K31/433 , A61K31/55 , A61K31/439 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61P29/00 , A61P37/00
CPC分类号： C07D285/135 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/02
摘要： The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following formula (I):in which, Y is S or O,R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted,R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted,R3 is X2-R'3, in which X2 is a binding group and R'3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted,or their pharmaceutically acceptable derivatives,the process for their preparation and their use for the manufacture of a medicament for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.

4. 发明授权

EP1362048B1 TRIAZOLO COMPOUNDS AS MMP INHIBITORS 有权
标题翻译： TRIAZOLOVERBINDUNGEN作为MMP抑制剂
公开(公告)号：EP1362048B1
公开(公告)日：2005-05-04
申请号：EP02702366.2
申请日：2002-02-11
申请人： Warner-Lambert Company LLC
发明人： ANDRIANJARA, Charles , JACOBELLI, Henry , GAUDILLIERE, Bernard , BREUZARD, Francine
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： A compound selected from those of formula (I): in which: W represents N or C-R1; in which R1 is as defined in the description, X represents N or C-R2 in which R2 is as defined in the description, Y represents a group selected from oxygen, sulfur, -NH, and -Nalkyl, Z represents a group selected from oxygen, sulphur, -NR8 in which R8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z1 represents a group -CR9R10 wherein R9 and R10, are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R4 is (are) as defined in the description, R3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula (II): in which p, Z2, B, q, and R13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of tpe-13 matrix mettaloprotease.

5. 发明公开

EP1362048A1 TRIAZOLO COMPOUNDS AS MMP INHIBITORS 有权
标题翻译： TRIAZOLO化合物作为MMP抑制剂
公开(公告)号：EP1362048A1
公开(公告)日：2003-11-19
申请号：EP02702366.2
申请日：2002-02-11
申请人： Warner-Lambert Company LLC
发明人： ANDRIANJARA, Charles , JACOBELLI, Henry , GAUDILLIERE, Bernard , BREUZARD, Francine
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： A compound selected from those of formula (I): in which: W represents N or C-R1; in which R1 is as defined in the description, X represents N or C-R2 in which R2 is as defined in the description, Y represents a group selected from oxygen, sulfur, -NH, and -Nalkyl, Z represents a group selected from oxygen, sulphur, -NR8 in which R8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z1 represents a group -CR9R10 wherein R9 and R10, are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R4 is (are) as defined in the description, R3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula (II): in which p, Z2, B, q, and R13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of tpe-13 matrix mettaloprotease.
摘要翻译：选自式（I）化合物的化合物：其中：W代表N或C-R1; 其中R 1如说明书中所定义，X表示N或C-R 2，其中R 2如说明书中所定义，Y表示选自氧，硫，-NH和-N烷基的基团，Z表示选自氧，硫，-NR8（其中R8如说明书中所定义）和任选地取决于Y的定义的碳，n是0-8的整数，包括端值，Z1表示基团-CR9R10，其中R9和R10如该描述中，该基团任选地包含多个键或杂原子，A表示环状基团，m是0至7的整数，包括端值，基团R 4是（如）在说明书中定义的，R 3表示选自氢，烷基，烯基，炔基和式（II）基团：其中p，Z2，B，q和R13如说明书中所定义，任选地，其外消旋形式，其异构体，其N-氧化物，及其药学上可接受的盐，以及含有它们的药物都可用作药物 tpe-13基质mettaloprotease的特异性抑制剂。

6. 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.

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