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1. 发明申请

WO2004062665A1 HETEROARYL- SUBSTITUTED PYRROLO` 2, 3- B! PYRIDINE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译： HETEROARYL-替代PYRROLO` 2，3-B！吡啶衍生物作为CRF受体拮抗剂
公开(公告)号：WO2004062665A1
公开(公告)日：2004-07-29
申请号：PCT/EP2004/000409
申请日：2004-01-14
申请人： SB PHARMCO PUERTO RICO INC , NEUROCRINE BIOSCIENCES INC , GLAXO GROUP LIMITED , CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： A61K31/437
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, 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：本发明提供了包括其立体异构体，前体药物和药学上可接受的盐或溶剂合物的式（I）化合物，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）。

2. 发明申请

WO2002100863A1 CORTICOTROPIN RELEASING FACTOR ANTAGONISTS 审中-公开
标题翻译： CORTICOTROPIN释放因子拮抗剂
公开(公告)号：WO2002100863A1
公开(公告)日：2002-12-19
申请号：PCT/GB2002/002656
申请日：2002-06-11
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
发明人： DI FABIO, Romano , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K51/0459 , C07B2200/05 , 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 R is aryl or heteroaryl and each of the above groups R 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, -COR 4 , nitro, -NR 3 R 4 cyano, or a group R 5 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 3 R 4 or cyano; R 2 corresponds to a group CHR 6 R 7 ; R 3 is hydrogen, C1-C6 alkyl; R 4 independently from R 3 , has the same meanings; R 5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R 5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R 6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R 6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R 7 independently from R 6 , has the same meanings; X is carbon or nitrogen; 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，其包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至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，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; 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 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中上述基团R 5可以被一个或多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，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自：C 1 -C 6烷氧基和羟基的基团取代; R7独立于R6，具有相同的含义; X是碳或氮; 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。

3. 发明申请

WO2002087573A1 CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CRF受体拮抗剂
公开(公告)号：WO2002087573A1
公开(公告)日：2002-11-07
申请号：PCT/GB2002/001981
申请日：2002-04-30
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , ST-DENIS, Yves
IPC分类号： A61K31/4353
CPC分类号： C07D471/06 , C07D487/06
摘要： The present invention relates to tricyclic pyrimidines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereofwherein R is aryl or heteroaryl, wherein each of the above groups R may be substituted by 1 to 4 substituents indendently selected from the group consisting of:halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 mono or dialkylamino, nitro, cyano and a group R 4 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, NH 2 , halogen or cyano; R 2 is hydrogen or C(H) n (R 5 ) q (CH 2 ) p ZR 6 ; R 3 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl or [CH(R 5 )(CH 2 ) p ] m ZR 6 ; R 4 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R 4 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 mon a or dialkylamino, nitro, and cyano; R 5 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl or (CH 2 ) p ZR 6 ; R 6 is C1-C6 alkyl, which may be substituted by one or more groups selected from halogen, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 alkoxy, C1-C6 mono or dialkylamino, nitro, cyano and a group R 4 ; Y and X are independently carbon or nitrogen; m and n are independently 0 or 1; p is 0 or an integer from 1 to 4;q is 1 or 2;Z is a bond, O, NH or S;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：本发明涉及式（I）的三环嘧啶化合物，包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其中R是芳基或杂芳基，其中上述基团R中的每一个可以被1至4个取代基所取代，由以下组成：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 1 -C 6单或二烷基氨基，硝基，氰基和 R4; 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，NH 2，卤素或氰基; R2是氢或C（H）n（R5）q（CH2）pZR6; R3是氢，C2-C6烯基，C2-C6炔基或[CH（R5）（CH2）p] mZR6; R4是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 4可以被一个或多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 1 -C 6单烷基或二烷基氨基，硝基和氰基; R5是氢，C2-C6烯基，C2-C6炔基或（CH2）pZR6; R6是C1-C6烷基，其可以被一个或多个选自卤素，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 1 -C 6烷氧基，C 1 -C 6 单或二烷基氨基，硝基，氰基和基团R 4; Y和X独立地为碳或氮; m和n独立地为0或1; p为0或1至4的整数; q为1或2; Z为O，NH或S键;其制备方法为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）。

4. 发明申请

WO0125219A3 PIPERAZINE COMPOUNDS 审中-公开
标题翻译：哌嗪化合物
公开(公告)号：WO0125219A3
公开(公告)日：2001-12-13
申请号：PCT/EP0009722
申请日：2000-10-05
申请人： GLAXO GROUP LTD , ALVARO GIUSEPPE , FABIO ROMANO DI , GIOVANNINI RICCARDO , GUERCIO GIUSEPPE , ST DENIS YVES , URSINI ANTONELLA
发明人： ALVARO GIUSEPPE , DI FABIO ROMANO , GIOVANNINI RICCARDO , GUERCIO GIUSEPPE , ST-DENIS YVES , URSINI ANTONELLA
IPC分类号： A61K31/495 , A61K31/496 , A61P1/04 , A61P11/06 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , C07D241/04 , C07D401/06 , C07D403/06
CPC分类号： C07D401/06 , A61K31/135 , A61K31/196 , A61K31/495 , A61K31/496 , C07D241/04 , C07D403/06 , A61K2300/00
摘要： The present invention relates to piperazine derivatives of formula (I) wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents hydrogen or a C1-4 alkyl group; R2 represents hydrogen, a C1-4 alkyl, C2-6 alkenyl or a C3-7 cycloalkyl group; or R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5-6 membered heterocyclic group; R3 represents a trifluoromethyl, a C1-4 alkyl, a C1-4 alkoxy, a trifluoromethoxy or a halogen group; R4 represents hydrogen, a (CH2)qR7 or a (CH2)rCO(CH2)pR7 group; R5 represents hydrogen, a C1-4 alkyl or a COR6 group; R6 represents hydrogen, hydroxy, amino, methylamino, dimethylamino a 5 membered heteroaryl group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen or a 6 membered heteroaryl group containing 1 to 3 nitrogen atoms; R7 represents hydrogen, hydroxy or NR8R9 wherein R8 and R9 represent independently hydrogen or C1-4 alkyl optionally substituted by hydroxy, or by amino; R10 represents hydrogen, a C1-4 alkyl I group or R10 together with R2 represents a C3-7 cycloalkyl group; m is zero or an integer from 1 to 3; n is zero or an integer from 1 to 3; both p and r are independently zero or an integer from 1 to 4; q is an integer from 1 to 4; provided that, when R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5 to 6 membered heterocyclic group, i) m is 1 or 2; ii) when m is 1, R is not fluorine and iii) when m is 2, the two substituents R are not both fluorine,and pharmaceutically acceptable salts and solvates thereof.
摘要翻译：本发明涉及式（I）的哌嗪衍生物，其中R表示卤素原子或C1-4烷基; R1表示氢或C1-4烷基; R 2表示氢，C 1-4烷基，C 2-6烯基或C 3-7环烷基; 或R 1和R 2与它们所连接的氮原子和碳原子分别表示5-6元杂环基; R3表示三氟甲基，C1-4烷基，C1-4烷氧基，三氟甲氧基或卤素基团; R4表示氢，（CH2）qR7或（CH2）rCO（CH2）pR7基团; R5代表氢，C1-4烷基或COR6基团; R 6表示氢，羟基，氨基，甲基氨基，二甲基氨基，含有1至3个选自氧，硫和氮的杂原子或含有1至3个氮原子的6元杂芳基的5元杂芳基; R 7表示氢，羟基或NR 8 R 9，其中R 8和R 9独立地表示氢或任选被羟基取代的C 1-4烷基或氨基; R 10表示氢，C 1-4烷基I基或R 10与R 2一起代表C 3-7环烷基; m为0或1〜3的整数; n为0或1〜3的整数; p和r分别独立为零或1至4的整数; q是1至4的整数; 条件是当R1和R2与它们所连接的氮原子和碳原子分别表示5至6元杂环基时，i）m为1或2; ii）当m为1时，R不为氟，iii）当m为2时，两个取代基R不同时为氟，其药学上可接受的盐和溶剂化物。

5. 发明申请

WO1996019483A1 LOW MOLECULAR WEIGHT BICYCLIC THROMBIN INHIBITORS 审中-公开
标题翻译：低分子量双分子抑制剂
公开(公告)号：WO1996019483A1
公开(公告)日：1996-06-27
申请号：PCT/CA1995000708
申请日：1995-12-21
申请人： BIOCHEM PHARMA INC. , DIMAIO, John , SIDDIQUI, M., Arshad , GILLARD, John, W. , ST-DENIS, Yves , TARAZI, Micheline , PREVILLE, Patrice , LEVESQUE, Sophie , BACHAND, Benoit
发明人： BIOCHEM PHARMA INC.
IPC分类号： C07D513/04
CPC分类号： C07D487/04 , A61K38/00 , C07D513/04 , C07K5/0202 , C07K5/06078 , C07K5/06139 , C07K5/0812 , C07K5/0821
摘要： This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin having formula (I), their preparation, and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo 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. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.
摘要翻译：本发明涉及具有式（I）的酶凝血酶的杂环竞争性抑制剂的发现，其制备及其药物组合物。此外，本发明还涉及这些化合物和组合物在体外作为抗凝剂和体内作为治疗和预防血栓形成疾病例如静脉血栓形成，肺栓塞和动脉血栓形成作为导致急性缺血事件如心肌梗死的药物的用途或脑梗塞。此外，这些化合物和组合物具有治疗用途，用于预防和治疗与冠状动脉旁路手术相关的凝血病以及经腔血管成形术后的再狭窄事件。

6. 发明申请

WO1994011382A1 ANTINEOPLASTIC HETERONAPHTHOQUINONES 审中-公开
标题翻译： ANTINEOPLOSTIC HETERONAPHTHOQUINONES
公开(公告)号：WO1994011382A1
公开(公告)日：1994-05-26
申请号：PCT/CA1993000463
申请日：1993-11-05
申请人： BIOCHEM PHARMA INC. , ATTARDO, Giorgio , BREINING, Tibor , COURCHESNE, Marc , KRAUS, Jean-Louis , LAMOTHE, Serge , LAVALLEE, Jean-François , LEBEAU, Elaine , NGUYEN, Dieu , REJ, Rabindra , ST-DENIS, Yves , WANG, Wuyi , XU, Yao-Chang , BARBEAU, France
发明人： BIOCHEM PHARMA INC.
IPC分类号： C07H17/00
CPC分类号： C07H15/252 , C07D311/76 , C07D311/92 , C07D335/08 , C07H17/00 , C07H17/04
摘要： Tricyclic heteronaphthoquinone derivatives, that have antineoplastic activity, are disclosed, together with processes for their synthesis. Some of these anti-neoplastics compounds have a saccharide moiety. Some members of this structurally distinct group exhibit activity against multiple drug resistant cancer cells.
摘要翻译：公开了具有抗肿瘤活性的三环杂萘醌衍生物及其合成方法。这些抗肿瘤化合物中的一些具有糖部分。该结构不同组的一些成员表现出抗多种耐药性癌细胞的活性。

7. 发明申请

WO2008148854A1 GHRELIN MODULATORS 审中-公开
标题翻译： GHRELIN调制器
公开(公告)号：WO2008148854A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057019
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： C07D401/06
CPC分类号： C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, 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，例如作为生长调节剂激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

8. 发明申请

WO2004094420A1 CONDENSED N-HETEROCYCLIC COMPOUNDS AND THEIR USE AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：简便的N-杂环化合物及其作为CRF受体拮抗剂的用途
公开(公告)号：WO2004094420A1
公开(公告)日：2004-11-04
申请号：PCT/IB2004/001350
申请日：2004-04-07
申请人： SB PHARMCO PUERTO RICO INC , NEUROCRINE BIOSCIENCES INC , ANDREOTTI, Daniele , BERNASCONI, Giovanni , CASTIGLIONI, Emiliano , CONTINI, Stefania , DI FABIO, Romano , FAZZOLARI, Elettra , FERIANI, Aldo , GENTILE, Gabriella , MATTIOLI, Mario , MINGARDI, Anna , SABBATINI, Fabio , ST-DENIS, Yves
发明人： ANDREOTTI, Daniele , BERNASCONI, Giovanni , CASTIGLIONI, Emiliano , CONTINI, Stefania , DI FABIO, Romano , FAZZOLARI, Elettra , FERIANI, Aldo , GENTILE, Gabriella , MATTIOLI, Mario , MINGARDI, Anna , SABBATINI, Fabio , 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 lkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R 2 , nitro, hydroxy, -NR 3 R 4 , cyano and or a group Z; R 1 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 Cl-C6 alkoxy, halogen, NR 3 R 4 or cyano; D, G is . -C- optionally substituted; X is carbon or nitrogen; Y is nitrogen or -C- optionally substituted; W is a 4-8 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 12 , S(O) m , carbonyl, and such ring may be further substituted by 1 to 8 substituents; Z is a 5-6 membered heterocycle, which may be substituted by 1 to 8 R 5 groups or a phenyl ring, which may be substituted by 1 to 4 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：本发明提供了包括立体异构体，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，C 2 -C 6炔基，卤素 C 1 -C 6烷氧基，-C（O）R 2，硝基，羟基，-NR 3 R 4，氰基和/或Z; R 1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为-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个碳原子可以任选被氧，氮或NR 12，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，其可以被1至8个R5基团取代或可被1至4个取代基取代的苯基环; m为0至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。

9. 发明申请

WO2002094826A1 TRI-AND TETRAAZA-ACENAPHTHYLEN DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为CRF受体拮抗剂的三硝基苯并噻吩衍生物
公开(公告)号：WO2002094826A1
公开(公告)日：2002-11-28
申请号：PCT/GB2002/002377
申请日：2002-05-21
申请人： NEUROCRINE INC. , SB PHARMCO PUERTO RICO INC. , DI FABIO, Romano , GENTILE, Gabriella , HADDACH, Mustapha , ST-DENIS, Yves , WILLIAMS, John, Patrick
发明人： DI FABIO, Romano , GENTILE, Gabriella , HADDACH, Mustapha , ST-DENIS, Yves , WILLIAMS, John, Patrick
IPC分类号： C07D471/16
CPC分类号： C07D471/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure of formula (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, R1, R2, R4, R5, R6, A, X, and Y are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。本发明的CRF受体拮抗剂具有以下结构式（I）：其包括立体异构体，其前药和药学上可接受的盐，R 1，R 2，R 4，R 5，R 6，A，X和Y如本文所定义。还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

10. 发明申请

WO1995012588A1 ANTINEOPLASTIC HETERONAPHTHOQUINONES 审中-公开
标题翻译： ANTINEOPLOSTIC HETERONAPHTHOQUINONES
公开(公告)号：WO1995012588A1
公开(公告)日：1995-05-11
申请号：PCT/CA1994000210
申请日：1994-05-06
申请人： BIOCHEM PHARMA INC. , ATTARDO, Giorgio , WANG, Wuyi , BREINING, Tibor , LI, TieChao , ST.-DENIS, Yves , KRAUS, Jean-Louis
发明人： BIOCHEM PHARMA INC.
IPC分类号： C07D311/76
CPC分类号： C07D493/04 , C07D311/76 , C07D311/92 , C07D335/08 , C07H17/00 , C07H17/04 , C07H17/08
摘要： Tricyclic heteronaphthoquinone derivatives, that have antineoplastic activity, are disclosed, together with processes for their synthesis. Some of these antineoplastic compounds have a saccharide moiety. Some members of this structurally distinct group exhibit activity against multiple drug resistant cancer cells.
摘要翻译：公开了具有抗肿瘤活性的三环杂萘醌衍生物及其合成方法。这些抗肿瘤化合物中的一些具有糖部分。该结构不同组的一些成员表现出抗多种耐药性癌细胞的活性。

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