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1. 发明申请

WO2006108693A8 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
标题翻译：制备双相化合物的方法
公开(公告)号：WO2006108693A8
公开(公告)日：2007-10-04
申请号：PCT/EP2006003531
申请日：2006-04-06
申请人： SB PHARMCO INC , NEUROCRINE BIOSCIENCES INC , BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , STABILE PAOLO , TAMPIERI MARSIA
发明人： BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , STABILE PAOLO , TAMPIERI MARSIA
IPC分类号： C07D471/04 , C07D207/22
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper wherein the substituents are as defined in the claims .
摘要翻译：本发明涉及一种制备式（IA）化合物的方法，该化合物是由式（I）的中间体化合物通过铜催化的偶联反应而成为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂，其中取代基如权利要求中所定义。

2. 发明申请

WO2006108693A2 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
标题翻译：制备双相化合物的方法
公开(公告)号：WO2006108693A2
公开(公告)日：2006-10-19
申请号：PCT/EP2006003531
申请日：2006-04-06
申请人： SB PHARMCO INC , NEUROCRINE BIOSCIENCES INC , BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , STABILE PAOLO , TAMPIERI MARSIA
发明人： BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , STABILE PAOLO , TAMPIERI MARSIA
IPC分类号： C07D471/04 , C07D207/22
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper wherein the substituents are as defined in the claims.
摘要翻译：本发明涉及一种制备式（IA）化合物的方法，该化合物是由式（I）的中间体化合物通过铜催化的偶联反应而成为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂，其中取代基如权利要求中所定义。

3. 发明申请

WO2006108689A3 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
标题翻译：制备双相化合物的方法
公开(公告)号：WO2006108689A3
公开(公告)日：2007-02-01
申请号：PCT/EP2006003480
申请日：2006-04-06
申请人： SB PHARMCO INC , NEUROCRINE BIOSCIENCES INC , ANDREOTTI DANIELE , BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , SPADA SIMONE , STABILE PAOLO , TAMPIERI MARSIA
发明人： ANDREOTTI DANIELE , BACCHI SERGIO , DELPOGETTO MONICA , GUELFI SIMONE , PERBONI ALCIDE , RIBECAI ARIANNA , SPADA SIMONE , STABILE PAOLO , TAMPIERI MARSIA
IPC分类号： C07D471/04 , A61K31/437 , A61P1/00 , A61P25/00 , C07D207/22
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper, formulae (I) (Ia) wherein X is halogen; and the other substituents are as defined in the description.
摘要翻译：本发明涉及由式（I）的中间体化合物，通过铜催化的偶联反应制备作为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂的式（IA）化合物的新方法，式（I）（Ia）其中X是卤素; 并且其它取代基如说明书中所定义。

4. 发明申请

WO2006108693A3 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2006108693A3
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003531
申请日：2006-04-06
申请人： SB Pharmco Puerto Rico Inc , Neurocrine Biosciences Inc , BACCHI, Sergio , DELPOGETTO, Monica , GUELFI, Simone , PERBONI, Alcide , RIBECAI, Arianna , STABILE, Paolo , TAMPIERI, Marsia
发明人： BACCHI, Sergio , DELPOGETTO, Monica , GUELFI, Simone , PERBONI, Alcide , RIBECAI, Arianna , STABILE, Paolo , TAMPIERI, Marsia
IPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper wherein the substituents are as defined in the claims .

5. 发明申请

WO2006108689A2 PROCESS FOR PREPARING BICYCLIC COMPOUNDS 审中-公开
标题翻译：制备双相化合物的方法
公开(公告)号：WO2006108689A2
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003480
申请日：2006-04-06
申请人： SB PHARMCO PUERTO RICO INC , NEUROCRINE BIOSCIENCES INC , ANDREOTTI, Daniele , BACCHI, Sergio , DELPOGETTO, Monica , GUELFI, Simone , PERBONI, Alcide , RIBECAI, Arianna , SPADA, Simone , STABILE, Paolo , TAMPIERI, Marsia
发明人： ANDREOTTI, Daniele , BACCHI, Sergio , DELPOGETTO, Monica , GUELFI, Simone , PERBONI, Alcide , RIBECAI, Arianna , SPADA, Simone , STABILE, Paolo , TAMPIERI, Marsia
IPC分类号： C07D471/04 , A61K31/437 , A61P1/00 , A61P25/00
CPC分类号： C07D471/04 , C07D207/22
摘要： The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper (I) (Ia)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 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, haloC1-C6 alkoxy, hydroxy, haloC1-C6 alkyl; 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)NR 6 R 7 ; X is halogen; and R'' corresponds to R; R'' 1 corresponds to R 1 ; 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 by 1 to 3 R 10 groups; R'' 4 is hydrogen; R'' 5 corresponds to R 5 ; R'' 6 corresponds to R 6 ; R'' 7 corresponds to R 7 ; R'' 8 corresponds to R 8 ; R'' 9 corresponds to R 9 ; 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 corresponds to R 11 .
摘要翻译：本发明涉及由式（I）的中间体化合物通过铜催化的偶联反应制备式（IA）化合物的新方法，其为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂 I）（Ia）其中R是芳基或杂芳基，其各自可以被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，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; R 5是C 1 -C 4烷基，-OR 6或-NR 6 R 7; R 6是氢或C 1 -C 6烷基; R 7是氢或C 1 -C 6烷基; R 8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个或更多个R 11个基团取代; R 9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 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）NR _{6 - [R _{7 ; X是卤素; 并且R“对应于R; R“1 对应于R 1; R 2是氢，C 3 -C 7环烷基或基团R 9; R 3是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1至3个R 10个基团取代; R“4是氢; R“5”对应于R 5; R“6”对应于R 6; R“7对应于R 7; R“8对应于R 8; R“9对应于R 9; 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链烯基， 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个组; R“”11“对应于R 11。}}

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