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1. 发明申请

WO2002076949A1 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有CB1拮抗活性的4,5-二氢-1H-吡唑衍生物
公开(公告)号：WO2002076949A1
公开(公告)日：2002-10-03
申请号：PCT/EP2002/003079
申请日：2002-03-18
申请人： SOLVAY PHARMACEUTICALS B.V. , LANGE, Josephus, H.M. , KRUSE, Cornelis, G , TIPKER, Jacobus , HOOGENDOORN, Jan
发明人： LANGE, Josephus, H.M. , KRUSE, Cornelis, G , TIPKER, Jacobus , HOOGENDOORN, Jan
IPC分类号： C07D231/06
CPC分类号： C07D231/08
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives having S configuration at the 4-position of their 4,5-dihydro pyrazole ring which are potent antagonists of the cannabis CB 1 -receptor.The compounds have the general formula (I) wherein- R and R 1 are the same or different and represent 3-pyridyl or 4-pyridyl or phenyl which may be substituted with halogen or methoxy,- R 2 and R 3 are the same or different and represent hydrogen, alkyl (1-3 C) or dimethylamino- R 4 represents phenyl which may be substituted with 1 or 2 substituents selected from the group halogen atoms, trifluoromethyl, methoxy and alkyl (1-3 C)and tautomers, prodrugs and salts thereof.These enantiomers are much more potent and selective antagonists of the cannabis CB 1 -receptor, than the other enantiomer.
摘要翻译：本发明涉及一组在其4,5-二氢吡唑环4位上具有S构型的4,5-二氢-1H-吡唑衍生物，它们是大麻CB1-受体的有效拮抗剂。化合物具有通式（I）其中R和R 1相同或不同并且表示可被卤素或甲氧基取代的3-吡啶基或4-吡啶基或苯基，R 2和R 3相同或不同，表示氢，烷基（1-3C）或二甲基氨基-R4表示可以被1或2个选自卤素原子，三氟甲基，甲氧基和烷基（1-3C）的取代基取代的苯基及其互变异构体，前体药物和盐。这些对映体是比其他对映体更有效和选择性的大麻CB1受体拮抗剂。

2. 发明申请

WO2003026648A1 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING POTENT CB1-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有活性CB1-拮抗活性的4,5-DIHYDRO-1H-吡唑衍生物
公开(公告)号：WO2003026648A1
公开(公告)日：2003-04-03
申请号：PCT/EP2002/010435
申请日：2002-09-17
申请人： SOLVAY PHARMACEUTICALS B.V. , KRUSE, Cornelis, G. , LANGE, Josephus, H.M. , TIPKER, Jacobus , HERREMANS, Arnoldus, H.J. , VAN STUIVENBERG, Herman, H.
发明人： KRUSE, Cornelis, G. , LANGE, Josephus, H.M. , TIPKER, Jacobus , HERREMANS, Arnoldus, H.J. , VAN STUIVENBERG, Herman, H.
IPC分类号： A61K31/415
CPC分类号： C07D231/06 , C07D401/04 , C07D401/12 , C07D409/04
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB 1 ) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.
摘要翻译：本发明涉及一组新的4,5-二氢-1H-吡唑衍生物，它们是用于治疗与大麻素系统紊乱有关的疾病的有效大麻素（CB1）受体拮抗剂。化合物具有通式（Ia）或（Ib），其中符号具有说明书中给出的含义。本发明还涉及制备这些化合物的方法，以及含有一种或多种这些化合物作为活性组分的药物组合物。

3. 发明申请

WO2003026647A1 NOVEL 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有CB1拮抗活性的新的4,5-二氢-1H-吡唑衍生物
公开(公告)号：WO2003026647A1
公开(公告)日：2003-04-03
申请号：PCT/EP2002/010433
申请日：2002-09-17
申请人： SOLVAY PHARMACEUTICALS B.V. , KRUSE, Cornelis, G. , LANGE, Josephus, H.M. , TIPKER, Jacobus , HERREMANS, Arnoldus, H.J. , VAN STUIVENBERG, Herman, H.
发明人： KRUSE, Cornelis, G. , LANGE, Josephus, H.M. , TIPKER, Jacobus , HERREMANS, Arnoldus, H.J. , VAN STUIVENBERG, Herman, H.
IPC分类号： A61K31/415
CPC分类号： C07D231/06 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/04
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.
摘要翻译：本发明涉及一组新的4,5-二氢-1H-吡唑衍生物，它们是用于治疗与大麻素系统紊乱有关的疾病的有效大麻素（CB1）受体拮抗剂。化合物具有通式（I），其中符号具有说明书中给出的含义。本发明还涉及制备这些化合物的方法，以及含有一种或多种这些化合物作为活性组分的药物组合物。

4. 发明授权

EP1268435B1 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB 1-ANTAGONISTIC ACTIVITY 有权
标题翻译：具有CB1拮抗活性4,5-二氢-1H-吡唑衍生物
公开(公告)号：EP1268435B1
公开(公告)日：2006-11-22
申请号：EP01915398.0
申请日：2001-03-22
申请人： Solvay Pharmaceuticals B.V.
发明人： LANGE, Josephus, H., M. , KRUSE, Cornelis, G. , TIPKER, Jacobus , TULP, Martinus, T., M. , VAN VLIET, Bernardus, J.
IPC分类号： C07D231/06 , C07D409/04 , C07D401/04 , A61K31/415 , A61P25/04 , A61P9/00 , C07D231/08
CPC分类号： C07D231/06 , C07D231/08 , C07D401/04 , C07D409/04
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent antagonists of the cannabis CB1-receptor. The compounds have general formula (I) wherein R and R1 are the same or different and represent phenyl, thienyl or pyridyl which groups may be substituted with 1, 2 or 3 substituents Y or R and/or R1 represent naphtyl, R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy, Aa represents one of the groups (i), (ii), (iii), (iv) or (v), Bb represents sulfonyl or carbonyl, R3 represents benzyl, phenyl, thienyl or pyridyl which may be substituted with 1, 2 or 3 substituents Y or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents naphtyl.

5. 发明公开

EP1212320A2 PHENYLPIPERAZINES AS SEROTONIN REUPTAKE INHIBITORS 有权
标题翻译：苯基衍生物血清素回收抑制剂的
公开(公告)号：EP1212320A2
公开(公告)日：2002-06-12
申请号：EP00962355.4
申请日：2000-08-22
申请人： Solvay Pharmaceuticals B.V.
发明人： VAN HES, Roelof , VAN DER HEIJDEN, Johannes, A., M. , KRUSE, Cornelis, G. , TIPKER, Jacobus , TULP, Martinus, T., M. , VISSER, Gerben, M. , VAN VLIET, Bernard, J.
IPC分类号： C07D405/12 , C07D401/12 , C07D413/12 , C07D417/12 , C07D209/34 , C07D403/12 , C07D209/40 , A61K31/496
CPC分类号： C07D401/12 , C07D209/34 , C07D209/40 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to a group of phenylpiperazines having high affinity for the dopamine D2-receptor and are good serotonin reuptake inhibitors (SRI's). The invention relates to a group of phenylpiperazine derivatives of formula (I) wherein: a.o. x is 1) a group of formula (1) wherein: S1 is hydrogen or halogen; S2 and S3 are independently hydrogen, alkyl (1-6C), phenyl or benzyl; S4 represents two hydrogen atoms or an oxo group, S5 is H or alkyl (1-4C); and Y is C, O or S, and salts there of.

6. 发明授权

EP1373216B1 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 有权
标题翻译：具有CB1拮抗活性的4,5-二氢-1H-吡唑衍生物
公开(公告)号：EP1373216B1
公开(公告)日：2004-12-15
申请号：EP02726190.8
申请日：2002-03-18
申请人： Solvay Pharmaceuticals B.V.
发明人： LANGE, Josephus, H.M. , KRUSE, Cornelis, G , TIPKER, Jacobus , HOOGENDOORN, Jan
IPC分类号： C07D231/06 , C07D401/04 , A61K31/415 , A61P25/00
CPC分类号： C07D231/08
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives having S configuration at the 4-position of their 4,5-dihydro pyrazole ring which are potent antagonists of the cannabis CB1-receptor.The compounds have the general formula (I) wherein- R and R1 are the same or different and represent 3-pyridyl or 4-pyridyl or phenyl which may be substituted with halogen or methoxy,- R2 and R3 are the same or different and represent hydrogen, alkyl (1-3 C) or dimethylamino- R4 represents phenyl which may be substituted with 1 or 2 substituents selected from the group halogen atoms, trifluoromethyl, methoxy and alkyl (1-3 C)and tautomers, prodrugs and salts thereof.These enantiomers are much more potent and selective antagonists of the cannabis CB1-receptor, than the other enantiomer.
摘要翻译：本发明涉及一组新的4,5-二氢-1H-吡唑衍生物，它们的4,5-二氢吡唑环的4位具有S构型，它们是大麻CB 1受体的有效拮抗剂。化合物具有其中-R和R1相同或不同并表示3-吡啶基或4-吡啶基或可被卤素或甲氧基取代的苯基的通式（I）：-R 2和R 3相同或不同并且代表氢，烷基（1-3C）或二甲基氨基-R 4代表可以被1或2个选自卤素原子，三氟甲基，甲氧基和烷基（1-3C）的取代基取代的苯基及其互变异构体，前药和盐。这些对映异构体是比其他对映异构体更有效和选择性的大麻CB 1受体拮抗剂。

7. 发明授权

EP1212320B1 PHENYLPIPERAZINES AS SEROTONIN REUPTAKE INHIBITORS 有权
标题翻译：苯基衍生物血清素回收抑制剂的
公开(公告)号：EP1212320B1
公开(公告)日：2005-07-06
申请号：EP00962355.4
申请日：2000-08-22
申请人： Solvay Pharmaceuticals B.V.
发明人： VAN HES, Roelof , VAN DER HEIJDEN, Johannes, A., M. , KRUSE, Cornelis, G. , TIPKER, Jacobus , TULP, Martinus, T., M. , VISSER, Gerben, M. , VAN VLIET, Bernard, J.
IPC分类号： C07D405/12 , C07D401/12 , C07D413/12 , C07D417/12 , C07D209/34 , C07D403/12 , C07D209/40 , A61K31/496
CPC分类号： C07D401/12 , C07D209/34 , C07D209/40 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to a group of phenylpiperazines having high affinity for the dopamine D2-receptor and are good serotonin reuptake inhibitors (SRI's). The invention relates to a group of phenylpiperazine derivatives of formula (I) wherein: a.o. x is 1) a group of formula (1) wherein: S1 is hydrogen or halogen; S2 and S3 are independently hydrogen, alkyl (1-6C), phenyl or benzyl; S4 represents two hydrogen atoms or an oxo group, S5 is H or alkyl (1-4C); and Y is C, O or S, and salts there of.

8. 发明公开

EP1268435A1 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB 1-ANTAGONISTIC ACTIVITY 有权
标题翻译： 4,5-DIHYDRO-1H-PYRAZOLDERIVATE MIT CB1-ANTAGONISTISCHERAKTIVITÄT
公开(公告)号：EP1268435A1
公开(公告)日：2003-01-02
申请号：EP01915398.0
申请日：2001-03-22
申请人： Solvay Pharmaceuticals B.V.
发明人： LANGE, Josephus, H., M. , KRUSE, Cornelis, G. , TIPKER, Jacobus , TULP, Martinus, T., M. , VAN VLIET, Bernardus, J.
IPC分类号： C07D231/06 , C07D409/04 , C07D401/04 , A61K31/415 , A61P25/04 , A61P9/00 , C07D231/08
CPC分类号： C07D231/06 , C07D231/08 , C07D401/04 , C07D409/04
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent antagonists of the cannabis CB1-receptor. The compounds have general formula (I) wherein R and R1 are the same or different and represent phenyl, thienyl or pyridyl which groups may be substituted with 1, 2 or 3 substituents Y or R and/or R1 represent naphtyl, R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy, Aa represents one of the groups (i), (ii), (iii), (iv) or (v), Bb represents sulfonyl or carbonyl, R3 represents benzyl, phenyl, thienyl or pyridyl which may be substituted with 1, 2 or 3 substituents Y or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents naphtyl.
摘要翻译：本发明涉及可以是大麻CB1-受体的有效拮抗剂的新的4,5-二氢-1H-吡唑化合物。化合物具有式（I），其中R和R 1相同或不同，代表未取代或取代的苯基，噻吩基或吡啶基或萘基。萘基R 2表示氢，羟基，C 1-3 - 烷氧基，乙酰氧基或丙酰氧基，A a表示如本文所定义的基团（ⅰ），（ⅱ），（ⅲ），（ⅳ）或（Ⅴ）中的一种，Bb表示磺酰基或羰基，R 3表示苄基，苯基，噻吩基或吡啶基，其各自为未取代或取代的，或R3表示C1-8支链或非支链烷基或C3-8环烷基，或R3表示萘基。

9. 发明公开

EP1373216A1 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 有权
标题翻译：具有CB1拮抗活性4,5-二氢-1H-吡唑衍生物
公开(公告)号：EP1373216A1
公开(公告)日：2004-01-02
申请号：EP02726190.8
申请日：2002-03-18
申请人： Solvay Pharmaceuticals B.V.
发明人： LANGE, Josephus, H.M. , KRUSE, Cornelis, G , TIPKER, Jacobus , HOOGENDOORN, Jan
IPC分类号： C07D231/06 , C07D401/04 , A61K31/415 , A61P25/00
CPC分类号： C07D231/08
摘要： The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives having S configuration at the 4-position of their 4,5-dihydro pyrazole ring which are potent antagonists of the cannabis CB1-receptor.The compounds have the general formula (I) wherein- R and R1 are the same or different and represent 3-pyridyl or 4-pyridyl or phenyl which may be substituted with halogen or methoxy,- R2 and R3 are the same or different and represent hydrogen, alkyl (1-3 C) or dimethylamino- R4 represents phenyl which may be substituted with 1 or 2 substituents selected from the group halogen atoms, trifluoromethyl, methoxy and alkyl (1-3 C)and tautomers, prodrugs and salts thereof.These enantiomers are much more potent and selective antagonists of the cannabis CB1-receptor, than the other enantiomer.

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