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    PYRAZOLOPYRIMIDINE AND PYRAZOLOTRIAZINE
    2.
    发明专利
    PYRAZOLOPYRIMIDINE AND PYRAZOLOTRIAZINE 失效

    公开(公告)号：JP2000186090A

    公开(公告)日：2000-07-04

    申请号：JP6114999

    申请日：1999-03-09

    Applicant: HOFFMANN LA ROCHE

    Inventor： BOES MICHAEL ,  RIEMER CLAUS ,  STADLER HEINZ

    IPC: A61K31/00 ,  A61K31/4162 ,  A61K31/505 ,  A61K31/519 ,  A61K31/529 ,  A61K31/53 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D231/54 ,  C07D251/72 ,  C07D487/04 ,  C07D495/14

    Abstract: PROBLEM TO BE SOLVED: To obtain a new pyrazolopyrimidine compound and a new pyrazolotriazine compound which have selective affinity with 5HT-6 receptors and are useful for preventing and treating central nerve disorders such as psychoses, manic depressive psychosis, dysmnesia, and Alzheimer's disease. SOLUTION: Compounds of formula I and II (R1 is phenyl; R2 is H, a lower alkyl or the like; R3 is amino, imidazolyl or the like; R4 is H, a hydroxy-lower alkyl or the like; R5 is H, a halogen or the like), and their salts, for example, 3-benzenesulfonyl-5-methyl-2-methylsulfanyl-pyrazolo[1,5-a]pyrimidin-7 -ylamine. The compound of formula I is obtained by reacting a compound of formula III with a compound of the formula: HR3 and then converting the reaction product into its salt. The compound of formula III is preferably dissolved in DMF, and the compound of the formula: HR3 is also dissolved in DMF or an alcohol, followed by reacting the compounds in the solution. The compound of the formula: HR3 is preferably piperazine, NH3, imidazole, or the like. The compound of formula III is preferably obtained from a compound of formula IV as a starting compound.

    SULFONAMIDE AND ITS USE
    3.
    发明专利
    SULFONAMIDE AND ITS USE 失效

    公开(公告)号：JPH1067734A

    公开(公告)日：1998-03-10

    申请号：JP16706097

    申请日：1997-06-24

    Applicant: HOFFMANN LA ROCHE

    Inventor： BOES MICHAEL ,  GODEL THIERRY ,  RIEMER CLAUS ,  SLEIGHT ANDREW

    IPC: A61K31/63 ,  A61K31/18 ,  A61K31/325 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/505 ,  A61P25/00 ,  C07C311/21 ,  C07C311/38 ,  C07C311/44 ,  C07D209/08 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D403/04

    Abstract: PROBLEM TO BE SOLVED: To obtain a medicine containing one of specific sulfonamide compounds partially including new compounds as an active ingredient, having good affinity for 5HT-6 receptors and useful for treating central nerve diseases such as psychosis, schizophrenia, manic depressive psychosis and depression. SOLUTION: This medicine contains a compound of formula I [R is H, amino, an alkylamino, an alkyl, etc.; R is H, an alkyl; Z is a group of formula II (R is H, amino, CF3 , an alkyl, etc.; R is amino, an alkyl, an alkoxy, etc.), a group of formula III (R is H, a halogen, an alkoxy, etc.; R is an alkyl, an alkylamino, an alkoxy, CF3 , etc.), etc.] or its pharmaceutically permissible salt. E.g. a compound (salt) of formula IV (R is H, an alkoxy, etc.; R is amino, an alkylamino), a compound (salt) of formula V (R is H, an alkylamino, etc.; R is an alkyl, CF3 , etc.), etc., are new among the compound of formula I. The compound of formula I is suitable for the treatments of dysmnesia, Parkinson's disease, amyotrophic lateral aclerosis, Alzheimer's disease and Huntington's disease.

    2-AMINOQUINOLINE DERIVATIVES AS 5-HT ( 5A) RECEPTOR ANTAGONISTS
    7.
    发明申请
    2-AMINOQUINOLINE DERIVATIVES AS 5-HT ( 5A) RECEPTOR ANTAGONISTS 审中-公开
    作为5-HT（5A）受体拮抗剂的2-氨基喹啉衍生物

    公开(公告)号：WO2009109493A3

    公开(公告)日：2009-10-29

    申请号：PCT/EP2009052195

    申请日：2009-02-25

    Applicant: HOFFMANN LA ROCHE ,  KOLCZEWSKI SABINE ,  RIEMER CLAUS ,  ROCHE OLIVIER ,  STEWARD LUCINDA ,  WICHMANN JUERGEN ,  WOLTERING THOMAS

    Inventor： KOLCZEWSKI SABINE ,  RIEMER CLAUS ,  ROCHE OLIVIER ,  STEWARD LUCINDA ,  WICHMANN JUERGEN ,  WOLTERING THOMAS

    IPC: C07D215/38 ,  A61K31/47 ,  A61K31/4709 ,  A61P25/00 ,  C07D405/12

    CPC classification number: C07D215/38 ,  C07D405/12

    Abstract: The present invention is concerned with 2-Aminoquinoline derivatives as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders. In particular, the present invention is concerned with compounds of the general Formula (I) wherein R1 and -Z-Ar1 are as described herein.

    Abstract translation: 本发明涉及作为5-HT5A受体拮抗剂的2-氨基喹啉衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。 本发明的活性化合物可用于预防和/或治疗抑郁症，焦虑症，精神分裂症，恐慌症，广场恐怖症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆，病症 饮食行为，性功能障碍，睡眠障碍，滥用药物，运动障碍如帕金森病，精神病或胃肠道疾病。 特别地，本发明涉及通式（I）的化合物，其中R1和-Z-Ar1如本文所述。

    RADIOLABELED NK3 RECEPTOR ANTAGONIST
    8.
    发明申请
    RADIOLABELED NK3 RECEPTOR ANTAGONIST 审中-公开
    放射性NK3受体拮抗剂

    公开(公告)号：WO2009049791A2

    公开(公告)日：2009-04-23

    申请号：PCT/EP2008008439

    申请日：2008-10-07

    Applicant: HOFFMANN LA ROCHE ,  BISSANTZ CATERINA ,  MALHERBE PARICHEHR ,  RIEMER CLAUS ,  SPOOREN WILL

    Inventor： BISSANTZ CATERINA ,  MALHERBE PARICHEHR ,  RIEMER CLAUS ,  SPOOREN WILL

    IPC: C07D215/52 ,  A61K31/47

    CPC classification number: C07D215/52

    Abstract: The present invention relates to a radiolabeled Neurokinin 3 receptor antagonist of the general formula (I) wherein R1 is a radiolabeled lower alkyl and a method for identifying a compound that can bind to a NK3R comprising a) contacting a compound of interest with a sample comprising the NK3R in the presence of the radiolabeled NK3R antagonist of any one of claims 1 to 3; and b) monitoring whether the compound of interest influences the binding of said radiolabeled NK3R antagonist to said NK3R. Furthermore, the present invention relates also to a mutant NK3R and uses thereof.

    Abstract translation: 本发明涉及通式（I）的放射性标记的神经激肽3受体拮抗剂，其中R 1是放射性标记的低级烷基，和鉴定可以结合NK 3 R的化合物的方法，包括a）使目的化合物与样品接触，所述样品包含 在权利要求1至3中任一项的放射性标记的NK3R拮抗剂存在下的NK3R; 和b）监测感兴趣的化合物是否影响所述放射性标记的NK3R拮抗剂与所述NK3R的结合。 此外，本发明还涉及突变型NK3R及其用途。

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