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85 条记录 (耗时 0.031 秒)

    Benzothiazole derivatives
    21.
    发明申请
    Benzothiazole derivatives 有权
    苯并噻唑衍生物

    公开(公告)号：US20060019949A1

    公开(公告)日：2006-01-26

    申请号：US11183503

    申请日：2005-07-18

    申请人： Alexander Flohr ,  Claus Riemer

    发明人： Alexander Flohr ,  Claus Riemer

    IPC分类号： A61K31/5377 ,  C07D413/14

    CPC分类号： C07D417/12

    摘要： The present invention relates to compounds of formulae IA and IB wherein R1 and R2 are each independently lower alkyl or —(CH2)m—O-lower alkyl, or together with the N atom to which they are attached form a heterocyclic ring; R3 is hydrogen or lower alkyl; R4 is lower alkyl; hetaryl is 3H-imidazole-2,4-diyl or 1H-pyrazole-1,4-diyl; n is 1 or 2; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used for the treatment of Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, ADHD, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or for the treatment of asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse, or for use as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for coronary artery disease and heart failure.

    摘要翻译： 本发明涉及式IA和IB的化合物，其中R 1和R 2各自独立地为低级烷基或 - （CH 2 CH 2） 或者与它们所连接的N原子一起形成杂环; R 3是氢或低级烷基; R 4是低级烷基; 杂芳基是3H-咪唑-2,4-二基或1H-吡唑-1,4-二基; n为1或2; m为1或2; 及其药学上可接受的酸加成盐。 这些化合物可用于治疗阿尔茨海默氏病，帕金森病，亨廷顿病，神经保护，精神分裂症，焦虑症，疼痛，呼吸缺陷，抑郁症，ADHD，药物成瘾如苯丙胺，可卡因，阿片样物质，乙醇，尼古丁，大麻素， 或用于治疗哮喘，过敏反应，缺氧，局部缺血，癫痫发作和药物滥用，或用作镇静剂，肌肉松弛剂，抗精神病药，抗癫痫剂，抗惊厥药和心脏保护剂用于冠状动脉疾病和心力衰竭。

    Amino-triazolopyridine derivatives
    25.
    发明授权
    Amino-triazolopyridine derivatives 失效

    公开(公告)号：US06355653B1

    公开(公告)日：2002-03-12

    申请号：US09645127

    申请日：2000-08-24

    申请人： Gerda Huber Trottmann ,  Walter Hunkeler ,  Roland Jakob-Roetne ,  Gavin John Kilpatrick ,  Matthias Heinrich Nettekoven ,  Claus Riemer

    发明人： Gerda Huber Trottmann ,  Walter Hunkeler ,  Roland Jakob-Roetne ,  Gavin John Kilpatrick ,  Matthias Heinrich Nettekoven ,  Claus Riemer

    IPC分类号： A61K314439

    CPC分类号： C07D471/04

    摘要： The invention relates to compounds of formula wherein R1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, —(CH2)nOH, halogen or lower alkoxy, and wherein the heteroaryl groups may be optionally linked to the pyrazole ring via an alkylene or alkenyl group, or is phenyl, optionally substituted by one or two substituents being lower alkyl, hydroxy-lower alkyl, halogen, hydroxy or lower alkoxy or is —O(CH2)n,phenyl, benzofuryl, indolyl or benzothiophenyl, or is —S-lower alkyl; R2 and R4 are independently from each other hydrogen, cyano or —S(O)2-phenyl; R3 is hydrogen, halogen or is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, —(CH2)n-aryl, hydroxy, halogen, lower alkoxy, morpholinyl, amino, lower alkylamino or —C(O)NR′2, and wherein R′ is lower alkyl or hydrogen, or is phenyl, optionally substituted by one or two substituents being halogen, lower alkyl, lower alkoxy, amino, di-lower alkyl amino, CF3, —OCF3, —NHC(O)lower alkyl, cyano, —C(O)-lower alkyl, —C(O)O-lower alkyl, —S-lower alkyl, —S(O)2NH-phenyl, —S(O)2-methylpiperazinyl; or is —NR′R″, wherein R′ and R″ are independently from each other hydrogen, —(CH2)nphenyl, which phenyl ring is optionally substituted by halogen or lower alkoxy, —CH(lower alkyl)-phenyl, indan-1-yl, 1,2,3,4-tetrahydro-naphthalen, or cycloalkyl; or is —O-phenyl, which phenyl ring is optionally substituted by halogen, lower alkyl or lower alkoxy, —O-tetrahydronaphthalenyl or —O—CH2-6-methyl-pyridin-2-yl; or is -benzo[1,3]dioxolyl, -1H-indol-5-yl, naphthyl, benzofuran-2-yl, 1,3,4,9-tetrahydro-b-carbolin-2-yl, piperidin-1-yl, pyrrolidin-1-yl, piperazin-4-yl-methyl or morpholinyl; R5 is —NR2, wherein R may be the same or different and is hydrogen, lower alkyl, phenyl, benzyl, —CO-lower alkyl, —CO-lower alkoxy, -lower alkenyl, —CO(CH2)n-phenyl or —COO(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by CF3, lower alkoxy, halogen or lower alkyl, —CO(CH2)3-NHCO-lower alkoxy, —(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by lower alkoxy, CF3 or halogen, or is 4,5-dihydro-1H-imidazol-2-yl-benzoic acid, 1,4,5,6-tetrahydro-pyrimidin-2-yl-benzoic acid or 4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-yl-benzoic acid; n is 0-4 and their pharmaceutically acceptable salts

    Pyrimidine compounds
    27.
    发明授权
    Pyrimidine compounds 失效
    嘧啶化合物

    公开(公告)号：US5688798A

    公开(公告)日：1997-11-18

    申请号：US714030

    申请日：1996-09-11

    申请人： Thierry Godel ,  Claus Riemer

    发明人： Thierry Godel ,  Claus Riemer

    IPC分类号： A61K31/505 ,  A61P25/18 ,  C07D239/26 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D401/06 ,  C07D239/28

    CPC分类号： C07D239/26 ,  C07D239/42 ,  C07D239/48 ,  C07D401/06

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each individually are lower-alkyl or amino, A is ##STR2## B is hydrogen in A.sup.4, A.sup.5 and A.sup.6 ; ##STR3## in A.sup.1 -A.sup.6 ; lower-alkoxy in A.sup.4 -A.sup.6 ; and lower-alkyl, styryl, phenylethynyl or benzoyloxy-lower-alkyl in A.sup.1 and A.sup.2 ; n is 0, 1 or 2; m, p are, independently 0, 1 and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halogen, lower-alkyl, trifluoromethyl, lower-alkoxy or nitro, and pharmaceutically acceptable acid addition salts thereof. These compounds are useful in the control or prevention of illnesses which are caused by disorders of the dopamine system, in particular psychotic illnesses such as schizophrenia.

    摘要翻译： 其中R 1和R 2各自独立地是低级烷基或氨基，其中A是A，B和A中的氢; A1-A6中的 A4-A6中的低级烷氧基; 和A1和A2中的低级烷基，苯乙烯基，苯基乙炔基或苯甲酰氧基 - 低级烷基; n为0,1或2; m，p独立地为0,1和R3，R4，R5和R6各自独立地为氢，卤素，低级烷基，三氟甲基，低级烷氧基或硝基，及其药学上可接受的酸加成盐。 这些化合物可用于控制或预防由多巴胺系统疾病引起的疾病，特别是精神病如精神分裂症。

    2-aminoquinolines
    29.
    发明授权
    2-aminoquinolines 失效
    2-氨基喹啉

    公开(公告)号：US08350028B2

    公开(公告)日：2013-01-08

    申请号：US12398415

    申请日：2009-03-05

    申请人： Sabine Kolczewski ,  Claus Riemer ,  Olivier Roche ,  Lucinda Steward ,  Juergen Wichmann ,  Thomas Woltering

    发明人： Sabine Kolczewski ,  Claus Riemer ,  Olivier Roche ,  Lucinda Steward ,  Juergen Wichmann ,  Thomas Woltering

    IPC分类号： C07D215/38 ,  C07D413/02

    CPC分类号： C07D405/12 ,  C07D215/38 ,  C07D491/08

    摘要： The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein R1 and R2 are as described herein and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists, useful for 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.

    摘要翻译： 本发明涉及式I的2-氨基喹啉衍生物，其中R 1和R 2如本文所述及其药学上可接受的盐，含有它们的药物组合物及其制备方法。 这些化合物是可用于预防和/或治疗抑郁症，焦虑障碍，精神分裂症，恐慌症，广场恐惧症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆症， 饮食行为障碍，性功能障碍，睡眠障碍，药物滥用，运动障碍如帕金森病，精神病或胃肠道疾病。