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11. 发明申请

WO03008412A3 HETERO-BICYCLIC CRF ANTAGONISTS 审中-公开
标题翻译：异源双相CRF拮抗剂
公开(公告)号：WO03008412A3
公开(公告)日：2003-05-01
申请号：PCT/EP0207865
申请日：2002-07-15
申请人： GLAXO GROUP LTD , DI FABIO ROMANO , MICHELI FABRIZIO , ST-DENIS YVES
发明人： DI FABIO ROMANO , MICHELI FABRIZIO , ST-DENIS YVES
IPC分类号： C07D471/00 , A61K31/437 , A61K31/4375 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/14 , A61P3/04 , A61P5/38 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/02 , A61P17/00 , A61P17/06 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, wherein R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R5, nitro, -NR6R7, cyano, and a group R8; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR6R7 or cyano; R2 is hydrogen, C3-C7 cycloalkyl, or a group R9; R3 is C3-C7 cycloalkyl, or a group R9; or R2 and R3 together with N form a 5-14 membered heterocycle, which may be substituted 1 to 3 R10 groups; R4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R5 is a C1-C4 alkyl, -OR6 or NR6R7; R6 is hydrogen or C1-C6 alkyl; R7 is hydrogen or C1-C6 alkyl; R8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R11 groups; R9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, halo C1-C6 alkoxy, hydroxy, halo C1-C6 alkyl; R10 is a group R8, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, C(O)NR6R7, phenyl which may be substituted by 1 to 4 R11 groups; R11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR6R7; X is carbon or nitrogen; n is 1 or 2; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供式（I）化合物，其包括其立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，其各自可以被1-4个选自以下的基团取代：卤素，C 1 -C 6烷基， C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-C（O）R 5，硝基，-NR 6 R 7，氰基和基团R 8; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 6 R 7或氰基; R2是氢，C3-C7环烷基或基团R9; R 3为C 3 -C 7环烷基或基团R 9; 或R 2和R 3与N一起形成5-14元杂环，其可以被取代1至3个R 10基团; R4是氢，C1-C6烷基，卤素或卤素C1-C6烷基; R5是C1-C4烷基，-OR6或NR6R7; R6是氢或C1-C6烷基; R7是氢或C1-C6烷基; R8是5-6元杂环，其可以是饱和的或可以含有一至三个双键，并且其可以被1个或多个R 11基团取代; R9是可以被一个或多个选自以下的基团取代的C 1 -C 6烷基：C 3 -C 7环烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基，羟基，卤代C 1 -C 6烷基; R 10是基团R 8，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，羟基，卤素，硝基，氰基，C（O）NR 6 R 7，可被1至4个R 11基团取代的苯基; R 11是C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，羟基，卤素，硝基，氰基或C（ O）NR6R7; X是碳或氮; n为1或2; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

12. 发明申请

WO2002088095A1 FUSED PYRIMIDINES AS ANTAGONISTS OF THE CORTICOTROPIN RELEASING FACTOR (CRF) 审中-公开
标题翻译：作为抗氧化剂释放因子（CRF）的拮抗剂的FUSED PYRIMININES
公开(公告)号：WO2002088095A1
公开(公告)日：2002-11-07
申请号：PCT/GB2002/002029
申请日：2002-04-30
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , CAPELLI, Anna, Maria , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
发明人： CAPELLI, Anna, Maria , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
IPC分类号： C07D239/70
CPC分类号： C07D487/04 , A61K51/0459 , A61K51/0463 , A61K51/0465 , C07D239/70 , C07D239/94 , C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein the variables are as defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供了式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中变量如本说明书所定义，其制备方法，含有它们的药物组合物及其在治疗由促肾上腺皮质激素释放因子（CRF）。

13. 发明申请

WO1995035297A1 NOVEL SUBSTITUTED PURINYL DERIVATIVES WITH IMMUNOMODULATING ACTIVITY 审中-公开
标题翻译：具有免疫调节活性的新型取代的嘌呤衍生物
公开(公告)号：WO1995035297A1
公开(公告)日：1995-12-28
申请号：PCT/CA1995000356
申请日：1995-06-21
申请人： BIOCHEM PHARMA INC. , PENNEY, Christopher , ZACHARIE, Boulos , GAGNON, Lyne , ATTARDO, Giorgio , CONNOLLY, Timothy , ST-DENIS, Yves , KADHIM, Salam , ELY, Guy
发明人： BIOCHEM PHARMA INC.
IPC分类号： C07D473/00
CPC分类号： A61K31/7052 , A61K31/52 , A61K38/00 , C07D473/00 , C07D473/34 , C07K5/0808 , A61K31/505 , A61K31/675 , A61K31/513 , A61K2300/00
摘要： The present invention covers substituted purinyl compounds. In particular, the present invention concerns 6-substituted purinyl alkoxycarbonyl amino acids, more particularly arginine derivatives. The present invention further includes substituted purinyl compounds which stimulate the immune system and thereby help protect the body against pathogens and cancer.
摘要翻译：本发明涉及取代的嘌呤基化合物。特别地，本发明涉及6-取代的嘌呤基烷氧基羰基氨基酸，更特别是精氨酸衍生物。本发明还包括刺激免疫系统并由此有助于保护身体免受病原体和癌症的取代的嘌呤基化合物。

14. 发明申请

WO2008148853A1 N-PHENYL HYDRAZIDES AS MODULATORS OF THE GHRELIN RECEPTOR 审中-公开
标题翻译：作为GHRELIN受体的调节剂的N-苯基水杨酸
公开(公告)号：WO2008148853A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057018
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
发明人： BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
IPC分类号： C07D213/54 , C07D239/26 , C07D307/79 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/72 , C07D333/76 , C07D405/06 , C07D471/04 , C07D487/04 , C07D295/15 , A61K31/498
CPC分类号： C07D333/76 , C07D211/34 , C07D213/56 , C07D213/61 , C07D239/26 , C07D295/15 , C07D307/81 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/60 , C07D405/06 , C07D471/04 , C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: each R 1 is independently selected from the group consisting of Cl, Br, CH 3 and CF 3 ; X is carbon or nitrogen; R 1a is H or a straight C 1-3 alkyl group; R 2a is H or a methyl group R 2 is selected from the group consisting of C 1-3 alkyl, H and -(CH 2 ) n -, wherein n is 3 or 4 and the terminal carbon of the chain is bonded to the carbon atom adjacent to the nitrogen bearing the R 2 group, such that a fused 6,5 or 6,6-bicyclic ring is formed. Y is selected from the group consisting of: phenyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C 1-3 alkyl, C 1-3 alkoxy, halogen, C 1-3 alkyl substituted by 1 to 7 fluoro atoms and C 1-3 alkoxy substituted by 1 to 7 fluoro atoms; pyridyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C 1-3 alkyl, OCH 3 , CF 3 , CN, and halogen; naphthyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of F and OCH 3 ; pyrimidinyl; imidazo[1,2-a]pyridine-6-yl; benzothiophen-2-yl; benzothiophen-5-yl; benzofuran-2-yl; dibenzo[b,d]furan-3-yl; dibenzo[b,d]thiophen-2-yl; dibenzo[b,d]thiophen-4-yl; 1,3- benzodioxol-5-yl; 2,3-dihydro-1,4-benzodioxin-5-yl; 2,3-dihydro-1,4-benzodioxin-6-yl; 2,3- dihydro-1-benzofuran-4-yl; 2,2-difluoro-1,3-benzodiox-4-yl; pyridazinyl; imidazolyl; oxazolyl; pyrazolyl; thiazolyl; and triazolyl; with the proviso that when Y is 2,3-dihydro-1,4-benzodioxin-6-yl, R 1 is not Cl; processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂化物，其中：每个R 1独立地选自Cl，Br，CH 3和CF 3; X是碳或氮; R 1a是H或直链C 1-3烷基; R2a是H或甲基R2选自C1-3烷基，H和 - （CH2）n-，其中n是3或4，并且该链的末端碳键合到邻近的碳原子上含有R2基团的氮，使得形成稠合的6,5或6,6-双环。 Y选自：可以是未取代的或被一个或多个独立地选自C 1-3烷基，C 1-3烷氧基，卤素，被1至7个氟原子取代的C 1-3烷基和C 1 由1-7个氟原子取代的3-烷氧基; 吡啶基，其可以是未取代的或被一个或多个独立地选自C 1-3烷基，OCH 3，CF 3，CN和卤素的取代基取代; 萘基，其可以是未取代的或被一个或多个独立地选自F和OCH 3的取代基取代; 嘧啶; 咪唑并[1,2-a]吡啶-6-基; 苯并噻吩-2-基; 苯并噻吩-5-基; 苯并呋喃-2-基; 二苯并[b，d]呋喃-3-基; 二苯并[b，D]噻吩-2-基; 二苯并[b，D]噻吩-4-基; 1,3-苯并间二氧杂环戊烯-5-基; 2,3-二氢-1,4-苯并二恶英-5-基; 2,3-二氢-1,4-苯并二恶英-6-基; 2,3-二氢-1-苯并呋喃-4-基; 2,2-二氟-1,3- benzodiox -4-基; 哒嗪; 咪唑; 恶唑; 吡唑; 噻唑基; 和三唑基; 条件是当Y是2,3-二氢-1,4-苯并二恶英-6-基时，R 1不是Cl; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，例如作为生长激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）的调节剂和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

15. 发明申请

WO2004094419A1 CONDENSED N-HETEROCYCLIC COMPOUNDS AND THEIR USE AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：简明的N-杂环化合物及其作为CRF受体拮抗剂的用途
公开(公告)号：WO2004094419A1
公开(公告)日：2004-11-04
申请号：PCT/IB2004/001283
申请日：2004-04-08
申请人： SB PHARMCO PUERTO RICO INC , NEUROCRINE BIOSCIENCES INC , ST-DENIS, Yves
发明人： ST-DENIS, Yves
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 .alkenyl, ,C2-C6 - alkynyl, - halo - C1=C6 - aIkoxy, - =C(O)RZ, - nitro, - hydroxy, =NR3R4i cyano, and or a group Z; R, is hydrogen, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 3 R 4 or cyano; D, G is -C- optionally substituted; A is -C- optionally substituted; X is carbon or-nitrogen; Y is nitrogen or -C- optionally substituted; W is a 4-8 carbocyclic membered ring, which may be saturated or may contain one to three double bonds,, and in which: - one carbon atom is replaced by a carbonyl or S(O) m ; and - one to four carbon atoms may optionally be replaced by oxygen, nitrogen or NR 14 , S(O) m , carbonyl, and such ring may be further substituted by I to 8 substituents; Z is a 5-6 membered heterocycle or a phenyl, which may be substituted by I to 8 substituents; m is an integer from 0 to 2, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供了包含立体异构体，前体药物和药学上可接受的盐或溶剂合物（式（I））的式（I）化合物，其中虚线可以表示双键; R是芳基或杂芳基，其各自可以被1-4个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基， - 炔基， - - 卤代C 1 -C 6烷基氧基， - = C（O）R Z， - 硝基， - 羟基，= NR 3 R 4氰基和/或基团Z; R 3是氢，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; D，G是-C-任选取代的; A是-C-任选取代的; X是碳或氮; Y是氮或-C-任选取代的; W是4-8碳环元环，其可以是饱和的或可以含有一至三个双键，其中： - 一个碳原子被羰基或S（O）m取代; 和 - 1-4个碳原子可以任选地被氧，氮或NR 14，S（O）m，羰基取代，并且这样的环可进一步被1至8个取代基取代; Z是5-6元杂环或苯基，其可以被1至8个取代基取代; m为0〜2的整数，其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

16. 发明申请

WO2003008414A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2003008414A1
公开(公告)日：2003-01-30
申请号：PCT/US2002/022394
申请日：2002-07-15
申请人： SB PHARMCO PUERTO RICO INC. , NEUROCRINE BIOSCIENCES INC. , DI FABIO, Romano , MICHELI, Fabrizio , REGAN, Collin, F. , SCHWAEBE, Michael, K. , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , REGAN, Collin, F. , SCHWAEBE, Michael, K. , ST-DENIS, Yves
IPC分类号： C07D471/16
CPC分类号： C07D471/16
摘要： The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof Please insert formula (I) here: to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明涉及包括立体异构体，前体药物和药学上可接受的盐或溶剂化物的式（I）的三环吡啶化合物。请在此处插入式（I）：其制备方法，含有它们的药物组合物及其在治疗中的用途的促肾上腺皮质激素释放因子（CRF）介导的病症。

17. 发明申请

WO2003008412A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2003008412A2
公开(公告)日：2003-01-30
申请号：PCT/EP2002/007865
申请日：2002-07-15
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , ST-DENIS, Yves
IPC分类号： C07D471/00
CPC分类号： C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, wherein R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R 5 , nitro, -NR 6 R 7 , cyano, and a group R 8 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 6 R 7 or cyano; R 2 is hydrogen, C3-C7 cycloalkyl, or a group R 9 ; R 3 is C3-C7 cycloalkyl, or a group R 9 ; or R 2 and R 3 together with N form a 5-14 membered heterocycle, which may be substituted 1 to 3 R 10 groups; R 4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R 5 is a C1-C4 alkyl, -OR 6 or NR 6 R 7 ; R 6 is hydrogen or C1-C6 alkyl; R 7 is hydrogen or C1-C6 alkyl; R 8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R 11 groups; R 9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, halo C1-C6 alkoxy, hydroxy, halo C1-C6 alkyl; R 10 is a group R 8 , C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, C(O)NR 6 R 7 , phenyl which may be substituted by 1 to 4 R 11 groups; R 11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR 6 R 7 ; X is carbon or nitrogen; n is 1 or 2; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供式（I）化合物，其包括其立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，其各自可以被1-4个选自以下的基团取代：卤素，C 1 -C 6烷基， C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-C（O）R 5，硝基，-NR 6 R 7，氰基和基团R 8; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 6 R 7或氰基; R2是氢，C3-C7环烷基或基团R9; R 3为C 3 -C 7环烷基或基团R 9; 或R 2和R 3与N一起形成5-14元杂环，其可以被取代1至3个R 10基团; R4是氢，C1-C6烷基，卤素或卤素C1-C6烷基; R5是C1-C4烷基，-OR6或NR6R7; R6是氢或C1-C6烷基; R7是氢或C1-C6烷基; R8是5-6元杂环，其可以是饱和的或可以含有一至三个双键，并且其可以被1个或多个R 11基团取代; R9是可以被一个或多个选自以下的基团取代的C 1 -C 6烷基：C 3 -C 7环烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基，羟基，卤代C 1 -C 6烷基; R 10是基团R 8，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，羟基，卤素，硝基，氰基，C（O）NR 6 R 7，可被1至4个R 11基团取代的苯基; R 11是C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，羟基，卤素，硝基，氰基或C（ O）NR6R7; X是碳或氮; n为1或2; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

18. 发明申请

WO1998009987A1 LACTAM INHIBITORS OF THROMBIN 审中-公开
标题翻译：酪氨酸激酶抑制剂
公开(公告)号：WO1998009987A1
公开(公告)日：1998-03-12
申请号：PCT/US1997015312
申请日：1997-09-05
申请人： BIOCHEM PHARMA, INC. , ST-DENIS, Yves , SIDDIQUI, M., Arshad , CODY, Wayne, Livingston , EDMUNDS, Jeremy, John , PLUMMER, Janet, Samartino
发明人： BIOCHEM PHARMA, INC.
IPC分类号： C07K05/078
CPC分类号： C07K5/0821 , C07K5/0202 , C07K5/06139
摘要： This invention relates to heterocyclic inhibitors of the enzyme thrombin, their preparation, and pharmaceutical compositions thereof having general formula (I), wherein W, X, Y R1 to R3 are as defined herein. Also, the invention relates to the use of such compounds and compositions as anticoagulants and as agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction.
摘要翻译：本发明涉及酶凝血酶的杂环抑制剂及其制备方法及其具有通式（I）的药物组合物，其中W，X，Y R1至R3如本文所定义。此外，本发明涉及这样的化合物和组合物作为抗凝剂和作为药剂的用途，用于治疗和预防血栓形成疾病如静脉血栓形成，肺栓塞和动脉血栓形成，导致急性缺血事件如心肌梗塞或脑梗死。

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