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公开(公告)号:EP1735330A1
公开(公告)日:2006-12-27
申请号:EP05733590.3
申请日:2005-03-18
申请人: N.V. Organon
CPC分类号: C07J43/003 , C07J5/00 , C07J43/00 , C07J53/001
摘要: The subject invention provides a compound according to Formula I, wherein Formula (1) is O, NOH, NO(1-4C)alkyl, NO(1-4C)acyl; Al-A5 are C, substituted with RI, or N, provided that at least one and not more than three of Al-A5 are N; or one or two of Al, A2 and A5 are N, and the others are C, substituted with Rl, and A3 and A4 together represent a fused benzo ring or a fused five- or six-membered nitrogen-containing aromatic ring, both optionally substituted with one or more halogen and/or (1-4C)alkyl; RI is H, halogen, (1 -4C)alkyl, (1 -4C)alkoxy; R2 is H, (1-4C)alkyl or (1-6C)alkenyl, both optionally substituted with an (6-10)aryl group, which is optionally substituted with one or more halogen and/or (1-4C)alkyl; and R3 is H or (1-4C)alkyl, optionally substituted with one or more halogen atoms; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl; or R2 together with R3 forms a 3-, 4-, 5- or 6-membered carbocyclic ring; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl); or R2 is H or (1-4C)alkyl; and R3 together with R4 forms a 5-, 6- or 7-membered saturated or unsaturated carbocyclic ring; R5 is H or (1-4C)alkyl; or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.
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公开(公告)号:EP2066677A1
公开(公告)日:2009-06-10
申请号:EP07820620.8
申请日:2007-09-26
申请人: N.V. Organon
发明人: REWINKEL, Johannes Bernardus Maria , FOLMER, Brigitte Johanna Bernita , OLLERO-OLLERO, Maria Lourdes , IBRAHIM, Hemen
IPC分类号: C07D498/04 , A61P5/24 , A61P15/18 , A61K31/553
CPC分类号: C07D498/04
摘要: The present invention provides new progesterone receptor modulators (I) and (II) which are (cis)-8-fluorodibenzo[b,f]pyrido[1,2-d] oxazepine-1 -amine compounds and uses thereof.
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公开(公告)号:EP1495030B1
公开(公告)日:2008-08-13
申请号:EP03720570.5
申请日:2003-04-01
申请人: N.V. Organon
发明人: HERMKENS, Pedro Harold Han , LUCAS, Hans , DOLS, Paul Peter Marie Antonius , REWINKEL, Johannes Bernardus Maria , FOLMER, Brigitte Johanna Bernita
IPC分类号: C07D498/04 , C07D513/04 , C07D471/04 , A61K31/55 , A61P5/24 , A61P35/00
CPC分类号: C07D471/04 , C07D513/04
摘要: The present invention provides compounds according to general Formula (I), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a prodrug thereof. More particularly, the present invention provides high affinity non-steroidal compounds which are agonists, partial agonists or antagonists of the progesterone receptor.
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公开(公告)号:EP2066677B1
公开(公告)日:2010-08-18
申请号:EP07820620.8
申请日:2007-09-26
申请人: N.V. Organon
发明人: REWINKEL, Johannes Bernardus Maria , FOLMER, Brigitte Johanna Bernita , OLLERO-OLLERO, Maria Lourdes , IBRAHIM, Hemen
IPC分类号: C07D498/04 , A61P5/24 , A61P15/18 , A61K31/553
CPC分类号: C07D498/04
摘要: The present invention provides new progesterone receptor modulators (I) and (II) which are (cis)-8-fluorodibenzo[b,f]pyrido[1,2-d] oxazepine-1 -amine compounds and uses thereof.
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公开(公告)号:EP1735330B1
公开(公告)日:2007-11-28
申请号:EP05733590.3
申请日:2005-03-18
申请人: N.V. Organon
CPC分类号: C07J43/003 , C07J5/00 , C07J43/00 , C07J53/001
摘要: The subject invention provides a compound according to Formula I, wherein Formula (1) is O, NOH, NO(1-4C)alkyl, NO(1-4C)acyl; Al-A5 are C, substituted with RI, or N, provided that at least one and not more than three of Al-A5 are N; or one or two of Al, A2 and A5 are N, and the others are C, substituted with Rl, and A3 and A4 together represent a fused benzo ring or a fused five- or six-membered nitrogen-containing aromatic ring, both optionally substituted with one or more halogen and/or (1-4C)alkyl; RI is H, halogen, (1 -4C)alkyl, (1 -4C)alkoxy; R2 is H, (1-4C)alkyl or (1-6C)alkenyl, both optionally substituted with an (6-10)aryl group, which is optionally substituted with one or more halogen and/or (1-4C)alkyl; and R3 is H or (1-4C)alkyl, optionally substituted with one or more halogen atoms; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl; or R2 together with R3 forms a 3-, 4-, 5- or 6-membered carbocyclic ring; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl); or R2 is H or (1-4C)alkyl; and R3 together with R4 forms a 5-, 6- or 7-membered saturated or unsaturated carbocyclic ring; R5 is H or (1-4C)alkyl; or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.
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