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1. 发明申请

WO2003076417A2 OXO-AZABICYCLIC COMPOUNDS 审中-公开
标题翻译： OXO-AZABICYCLIC化合物
公开(公告)号：WO2003076417A2
公开(公告)日：2003-09-18
申请号：PCT/EP2003/002277
申请日：2003-03-06
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
IPC分类号： C07D239/91
CPC分类号： C07D471/04 , C07D239/91
摘要： A compound selected from those of formula (1): ~',Xi Gi X 2 (7l) I ,N - R 1 (I) 11 - G 2 X3 wherein: 5 • X,, X2, and X3, represent N or -CR3 in which R3 is as described in the description, • G, represents a group selected from those of formulae (i/a) and (i/b): R4 R6 \ R4 N (i/a) (i/b) in which R4, R5, and R6 are as defined in the description, • G2 represents a group selected from carbon-carbon triple bond, -CH=C=CH-, C=O, 10 C=S, S(O) n , in which nl represents an integer from 0 to 2 inclusive, or a group of formula (i/c): 11-1y -r ( i/c ) Y 1 in which Y1 represents O, S, -NH or -Nalkyl, and Y2 represents O, S, -NH or -Nalkyl, • n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, 15 • Z, represents -CRgR,o, wherein R9 and R I O areas defined in the description, • A represents a ring system, • R, represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d) (G3)q~(Z2 )~ (i/d) 20 in which p, Z2, B, q and G3 are as defined in the description 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 mettaloprotease.
摘要翻译：选自式（I）的化合物的化合物，其中：X 1，X 2和X 3表示N或-CR 3，其中R 3如描述中所述，G 1表示选自式（i / a）和（其中R 4，R 5和R 6如说明书中所定义，R 2表示选自碳 - 碳三键，-CH = C = CH-，C = O，C = S，S（O ）n1，其中n1表示0〜2的整数，或其中Y1表示O，S，-NH或-N烷基的式（i / c）基团，Y2表示O，S，-NH或-N烷基 n为0以上6以下的整数，m为0以上7以下的整数，Z1为-CR9R10，其中，R9和R10如说明书中所定义，A表示环系，R1表示选自 H，烷基，烯基，炔基，任选被取代的基团和其中p，Z2，B，q和G3如说明书中所定义的任选的其光学异构体，N-氧化物和加成其盐与药学上可接受的 le酸或碱，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

WO2003076416A1 OXO AZABICYCLIC COMPOUNDS 审中-公开
标题翻译： OXO AZABICYCLIC化合物
公开(公告)号：WO2003076416A1
公开(公告)日：2003-09-18
申请号：PCT/EP2002/003240
申请日：2002-03-08
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
IPC分类号： C07D239/91
CPC分类号： C07D471/04 , C07D239/91
摘要： A compound selected from those of formula (I): formula (I) wherein: - X 1 , X 2 , and X 3 , represent N or CR 3 in which R 3 is as described in the description, - G 1 represents a group selected from those of formulae (i/a) and (i/b): formula (II) in which R 4 , R 5 , and R 6 are as defined in the description, - G 2 represents a group selected from carbon-carbon triple bond, -CH=C=CH-, C=O, C=S, S(O) nt in which n1 represents an integer from 0 to 2 inclusive, or a group of formula (i/c): formula (III) in which Y 1 represents O, S, -NH or Nalkyl, and Y 2 represents O, S, -NH or Nalkyl, - n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Z 1 represents CR 9 R 10 , wherein R 9 and R 10 are as defined in the description, - A represents a ring system, - R 1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d): formula (IV) in which p, Z 2 , B, q and G 3 are as defined in the description 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 mettaloprotease.
摘要翻译：选自式（I）的化合物：式（I）其中：-X 1，X 2和X 3表示其中R 3如描述中所述的N或CR 3，-G1表示选自式 I / a）和（i / b）：其中R 4，R 5和R 6如说明书中所定义的式（II），-G2表示选自碳 - 碳三键，-CH = C = CH- ，C = O，C = S，S（O）nt，其中n1表示0〜2的整数，或式（i / c）：式（III）的基团，其中Y1表示O，S， NH或N烷基，Y2表示O，S，-NH或N烷基，-n为0〜6的整数，m为0〜7的整数，Z1表示CR9R10，其中R9和R10如描述，-A表示环系，-R 1表示选自H，烷基，烯基，炔基，任选取代的基团和式（I / d）的基团：式（IV）其中p，Z2，B， q和G3如说明书中所定义，并且任选地，其光学异构体，和其药学上可接受的酸或碱的加成盐和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

WO2003076417A3 OXO-AZABICYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2003076417A3
公开(公告)日：2003-09-18
申请号：PCT/EP2003/002277
申请日：2003-03-06
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
IPC分类号： C07D239/91
摘要： A compound selected from those of formula (I) wherein: X 1 , X 2 , and X 3 , represent N or -CR 3 in which R 3 is as described in the description, G 1 represents a group selected from those of formulae (i/a) and (i/b) in which R 4 , R 5 , and R 6 are as defined in the description, G 2 represents a group selected from carbon-carbon triple bond, -CH=C=CH-, C=O, C=S, S(O) n1 in which nl represents an integer from 0 to 2 inclusive, or a group of formula (i/c) in which Y 1 represents O, S, -NH or -Nalkyl, and Y 2 represents O, S, -NH or -Nalkyl, n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Z 1 represents -CR 9 R 10 ,wherein R 9 and R 10 are as defined in the description, A represents a ring system, R 1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d) in which p, Z 2 , B, q and G 3 are as defined in the description 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 mettaloprotease.

4. 发明申请

WO2005049574A1 ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雄激素受体调节剂
公开(公告)号：WO2005049574A1
公开(公告)日：2005-06-02
申请号：PCT/IB2004/003668
申请日：2004-11-08
申请人： WARNER-LAMBERT COMPANY LLC , HU, Lain-Yen , DU, Daniel, Yunlong , LEI, Huangshu , YUE, Wen-Song
发明人： HU, Lain-Yen , DU, Daniel, Yunlong , LEI, Huangshu , YUE, Wen-Song
IPC分类号： C07D213/74
CPC分类号： C07D213/85
摘要： The present invention is directed to a new class of 5-cyano-2-amino pyridines and to their use as androgen receptor modulators. A further aspect of the invention is directed to a new animal model for finding compounds capable of alleviating androgenic alopecia.
摘要翻译：本发明涉及一类新的5-氰基-2-氨基吡啶并且其用作雄激素受体调节剂。本发明的另一方面涉及一种用于发现能够减轻雄激素性脱发的化合物的新动物模型。

5. 发明申请

WO2002064598A1 THIENO'2,3-D PYRIMIDINDIONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： THIENO'2,3-D吡啶衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2002064598A1
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000204
申请日：2002-01-18
申请人： WARNER-LAMBERT COMPANY , HARTER, William, Glen , LI, Jie, Jack , ORTWINE, Daniel, Fred , SHULER, Kevon, Ray , YUE, Wen-Song
发明人： HARTER, William, Glen , LI, Jie, Jack , ORTWINE, Daniel, Fred , SHULER, Kevon, Ray , YUE, Wen-Song
IPC分类号： C07D495/04
CPC分类号： C07D487/04 , A61K31/519 , C07D491/04 , C07D495/04
摘要： Selective MMP-13 inhibitors are fused pyrimidinones of the formula or a pharmaceutically acceptable salt thereof, wherein: W, together with the carbon atoms to which it is attached, form a 5-membered ring diradical Y is O, S, SO, SO 2 , NR 5 , or CH¿2, ?A is-C-or S-; B is O or NR 5 ; or A and B are taken together to form -C≡C-; R 1 , R 4 , and R 5 are hydrogen, alkyl, alkenyl, alkynyl, (CH 2 ) n aryl, (CH 2 ) n cycloalkyl, C 1 C 6 alkanoyl, or (CH 2 ) n heteroaryl; R 2 and R 3 are hydrogen, alkyl, alkenyl, alkynyl CN, NO 2 , NR 4 R 5 , (CH 2 ) n cycloalkyl, (CH 2 ) n aryl, or (CH 2 ) n heteroaryl; R 2 may further be halo; n is an integer of from 0 to 5; and 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 O, S, or N, and substituted or unsubstituted; with the proviso that R?1 ¿and R 3 are not both selected from hydrogen and C 1- C 6 alkyl.
摘要翻译：选择性MMP-13抑制剂是下式的稠合嘧啶酮或其药学上可接受的盐，其中：W与其连接的碳原子一起形成5元环双基Y是O，S，SO，SO 2， NR 5，或CH 2，A是-C-或S-; B是O或NR 5; 或A和B一起形成-CC-; R 1，R 4和R 5是氢，烷基，烯基，炔基，（CH 2）n芳基，（CH 2）n环烷基，C 1 -C 6烷酰基或（CH 2）n杂芳基; R 2和R 3是氢，烷基，烯基，炔基CN，NO 2，NR 4 R 5，（CH 2）n环烷基，（CH 2）n芳基或（CH 2）n杂芳基; R 2还可以是卤素; n为0〜5的整数。和R 4和R 5与它们所连接的氮原子一起形成含有碳原子的3-8元环，任选地含有O，S或N以及取代或未取代的; 条件是R 1和R 3不都选自氢和C 1 -C 6烷基。

6. 发明公开

EP1687274A1 ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雄激素受体调节剂
公开(公告)号：EP1687274A1
公开(公告)日：2006-08-09
申请号：EP04798809.2
申请日：2004-11-08
申请人： Warner-Lambert Company LLC
发明人： HU, Lain-Yen , DU, Daniel Yunlong , LEI, Huangshu , YUE, Wen-Song
IPC分类号： C07D213/74 , A61K31/4965
CPC分类号： C07D213/85
摘要： The present invention is directed to a new class of 5-cyano-2-amino pyridines and to their use as androgen receptor modulators. A further aspect of the invention is directed to a new animal model for finding compounds capable of alleviating androgenic alopecia.

7. 发明公开

EP1492775A2 OXO-AZABICYCLIC COMPOUNDS 审中-公开
标题翻译： OXO-氮杂双环CONNECTIONS
公开(公告)号：EP1492775A2
公开(公告)日：2005-01-05
申请号：EP03708181.7
申请日：2003-03-06
申请人： Warner-Lambert Company LLC
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
IPC分类号： C07D239/91
CPC分类号： C07D471/04 , C07D239/91
摘要： A compound selected from those of formula (I) wherein: X1, X2, and X3, represent N or -CR3 in which R3 is as described in the description, G1 represents a group selected from those of formulae (i/a) and (i/b) in which R4, R5, and R6 are as defined in the description, G2 represents a group selected from carbon-carbon triple bond, -CH=C=CH-, C=O, C=S, S(O)n1 in which nl represents an integer from 0 to 2 inclusive, or a group of formula (i/c) in which Y1 represents O, S, -NH or -Nalkyl, and Y2 represents O, S, -NH or -Nalkyl, n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Z1 represents -CR9R10,wherein R9 and R10 are as defined in the description, A represents a ring system, R1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d) in which p, Z2, B, q and G3 are as defined in the description 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 mettaloprotease.

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