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11 条记录 (耗时 0.012 秒)

    Diaza-spiro[3,5] nonane derivatives
    3.
    发明公开
    Diaza-spiro[3,5] nonane derivatives 有权
    氮杂 - 螺[3,5]壬烷衍生物在

    公开(公告)号：EP0970957A1

    公开(公告)日：2000-01-12

    申请号：EP99110943.0

    申请日：1999-06-07

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Adam, Geo ,  Cesura, Andrea ,  Jenck, Francois ,  Kolczewski, Sabine ,  Roever, Stephan ,  Wichmann, Jürgen

    IPC分类号： C07D471/10 ,  A61K31/445

    CPC分类号： C07D471/10

    摘要： The invention relates to compounds of the general formula
    wherein

    R 1 is C 6-12 -cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl;
    R 2 is =O or hydrogen,
    R 3 is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, -CH 2 OR 5 or -CH 2 N(R 5 ) 2;
    R 4 is hydrogen or -CH 2 OR 5 ;
    R 5 is hydrogen or lower alkyl;
    Ⓐ is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy;
    to racemic mixtures and their corresponding enantiomers and or pharmaceutically acceptable acid addition salts thereof.

    The compounds of the present invention are agonists and/or antagonists of the orphamin FQ (OFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

    摘要翻译： 本发明涉及通式为CHEM的化合物，其中R 1为C 6-12 - 环烷基，任选被低级烷基或C（O）O低级烷基，茚满-1-基或茚满-2-基取代， 任选被低级烷基取代; 苊-1-基; 双环-3-氨基-9-基，八氢 - 茚-2-基; 2,3-二氢-1H-phenalen -1-基; 2,3,3a，4,5,6-六氢-1H-吩酚-1-基，十氢 - 薁-2-基; bicycloÄ6.2.0Üdec-9-基; 十氢萘-1-基，十氢萘-2-基; 四氢 - 萘-1-基，四氢 - 萘-2-基或2-氧代-1,2-二苯基 - 乙基; R 2是= O或氢，R 3是氢，异吲哚基-1,3-二酮，低级烷氧基，低级烷基，氨基，苄氧基，-CH 2 OR 5或-CH 2 N（R 5）2 ; R 4是氢或-CH 2 OR 5; R 5是氢或低级烷基; 芳基和环烷基是任选被低级烷基，卤素或烷氧基取代的环己基或苯基; 外消旋混合物及其相应的对映体及其药学上可接受的酸加成盐。 本发明的化合物是神经元FQ（OFQ）受体的激动剂和/或拮抗剂，因此可用于治疗与该受体有关的疾病。

    Di-or triaza-spiro(4,5)decane derivatives
    4.
    发明公开
    Di-or triaza-spiro(4,5)decane derivatives 有权
    Diazder Triazaspiro [4,5]破坏

    公开(公告)号：EP0963985A2

    公开(公告)日：1999-12-15

    申请号：EP99110954.7

    申请日：1999-06-07

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Adam, Geo ,  Cesura, Andrea ,  Jenck, Francois ,  Kolczewski, Sabine ,  Roever, Stephan ,  Wichmann, Jürgen

    IPC分类号： C07D471/10 ,  A61K31/44 ,  C07D513/10 ,  C07D498/10

    CPC分类号： C07D471/10 ,  C07D513/10

    摘要： The present invention relates to compounds of the general formula
    wherein

    R 1 is C 6 - 10 -cycloalkyl, optionally substituted by lower alkyl or -C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl;
    R 2 is hydrogen; lower alkyl; =O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy;
    Ⓐ is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy;
    X is -CH(OH)-; -C(O)-; -CHR 3 -; -CR 3 =; -O-; -S-; -CH(COOR 4 )- or - C(COOR 4 )=;
    Y is -CH 2 -; -CH=; -CH(COOR 4 )-, -C(COOR 4 )=; or -C(CN)-;
    R 3 is hydrogen or lower alkoxy;
    R 4 is lower alkyl, cycloalkyl, phenyl, or benzyl
    and
    either a or b is optionally an additional bond,
    and to pharmaceutically acceptable acid addition salts thereof.

    The compounds are agonists and/or antagonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

    摘要翻译： 本发明涉及通式的化合物，其中R 1为任选被低级烷基或-C（O）O-低级烷基取代的C 6-10 - 环烷基; 十氢 - 萘-1-基; 十氢萘-2-基; 茚满-1-基或茚满-2-基，任选被低级烷基取代; 十氢薁-2-基; bicycloÄ6.2.0Üdec-9-基; 苊-1-基; 2,3-二氢-1H-phenalen -1-基; 2,3,3a，4,5,6-六氢-1H-苯并芬-1-基或八氢茚-2-基; R 2是氢; 低级烷基 = O或苯基，任选被低级烷基，卤素或烷氧基取代; 芳基和环烷基是任选被低级烷基，卤素或烷氧基取代的环己基或苯基; X是-CH（OH） - ; -C（O） - ; -CHR <3> - ; -CR <3> =; -O-; -S-; -CH（COOR 4） - 或-C（COOR 4）=; Y是-CH 2 - ; -CH =; -CH（COOR 4） - ， - C（COOR 4）=; 或-C（CN） - ; R 3是氢或低级烷氧基; R 4是低级烷基，环烷基，苯基或苄基，并且a或b任选是另外的键，以及其药学上可接受的酸加成盐。 这些化合物是孤儿素FQ（QFQ）受体的激动剂和/或拮抗剂，因此可用于治疗与该受体有关的疾病。

    Di-or triaza-spiro(4,5)decane derivatives
    6.
    发明公开
    Di-or triaza-spiro(4,5)decane derivatives 有权
    二 - 奥得三氮杂螺[4.5] decanderivate

    公开(公告)号：EP0963985A3

    公开(公告)日：2001-01-24

    申请号：EP99110954.7

    申请日：1999-06-07

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Adam, Geo ,  Cesura, Andrea ,  Jenck, Francois ,  Kolczewski, Sabine ,  Roever, Stephan ,  Wichmann, Jürgen

    IPC分类号： C07D471/10 ,  A61K31/44 ,  C07D513/10 ,  C07D498/10

    CPC分类号： C07D471/10 ,  C07D513/10

    摘要： The present invention relates to compounds of the general formula wherein R 1 is C 6 - 10 -cycloalkyl, optionally substituted by lower alkyl or -C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; R 2 is hydrogen; lower alkyl; =O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; A○ is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; X is -CH(OH)-; -C(O)-; -CHR 3 -; -CR 3 =; -O-; -S-; -CH(COOR 4 )- or - C(COOR 4 )=; Y is -CH 2 -; -CH=; -CH(COOR 4 )-, -C(COOR 4 )=; or -C(CN)-; R 3 is hydrogen or lower alkoxy; R 4 is lower alkyl, cycloalkyl, phenyl, or benzyl and either a or b is optionally an additional bond, and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists and/or antagonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

    Spiro(piperidine-4,1'-pyrrolo(3,4-c)pyrrole)
    7.
    发明公开
    Spiro(piperidine-4,1'-pyrrolo(3,4-c)pyrrole) 有权
    螺（哌啶4,1'吡咯并（3,4-c）的吡咯）

    公开(公告)号：EP0963987A3

    公开(公告)日：2001-01-17

    申请号：EP99110944.8

    申请日：1999-06-07

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Adam, Geo ,  Dautzenberg, Frank ,  Kolczewski, Sabine ,  Roever, Stephan ,  Wichmann, Jürgen

    IPC分类号： C07D471/20 ,  A61K31/44

    CPC分类号： C07D471/20

    摘要： The present invention relates to compounds of the general formula    wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na + excretion, arterial blood pressure disorders and metabolic disorders such as obesity.

    Spiro(piperidine-4,1'-pyrrolo(3,4-c)pyrrole)
    9.
    发明公开
    Spiro(piperidine-4,1'-pyrrolo(3,4-c)pyrrole) 有权
    螺（哌啶4,1'吡咯并（3,4-c）的吡咯）

    公开(公告)号：EP0963987A2

    公开(公告)日：1999-12-15

    申请号：EP99110944.8

    申请日：1999-06-07

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Adam, Geo ,  Dautzenberg, Frank ,  Kolczewski, Sabine ,  Roever, Stephan ,  Wichmann, Jürgen

    IPC分类号： C07D471/20 ,  A61K31/44

    CPC分类号： C07D471/20

    摘要： The present invention relates to compounds of the general formula
       wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof.
    The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na + excretion, arterial blood pressure disorders and metabolic disorders such as obesity.

    摘要翻译： 本发明涉及通式的化合物，其中取代基在本申请中描述及其药学上可接受的酸加成盐。 本发明的化合物可用于治疗与孤儿素FQ（OFQ）受体相关的疾病，其包括精神病学，神经学和生理学疾病，例如焦虑和压力障碍，抑郁症，创伤，由于阿尔茨海默病或其他因素引起的记忆丧失 痴呆症，认知障碍和癫痫发作缺陷，癫痫和惊厥，急性和/或慢性疼痛状况，上瘾药物戒断症状，​​控制水分平衡，Na +排泄，动脉血压障碍和代谢性疾病如肥胖症。

    5H-Thiazolo (3,2-a) pyrimidine derivatives
    10.
    发明公开
    5H-Thiazolo (3,2-a) pyrimidine derivatives 失效
    5H-噻唑并（3,2-a）嘧啶衍生物

    公开(公告)号：EP0891978A3

    公开(公告)日：1999-02-03

    申请号：EP98112915.8

    申请日：1998-07-11

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Adam, Geo ,  Kolczewski, Sabine ,  Mutel, Vincent ,  Wichmann, Jürgen ,  Woltering, Thomas Johannes

    IPC分类号： C07D513/04 ,  A61K31/505 ,  C07D239/40

    CPC分类号： C07D513/04 ,  C07D239/40

    摘要： The invention is concerned with compounds of the general formula
    wherein
    R 1 signifies hydrogen, lower alkyl, phenyl or benzyl, R 2 signifies lower alkyl, lower alkoxy, -O(CH 2 ) n N(R 13 )(R 14 ), -(CH 2 ) n N(R 13 )(R 14 ) or -N(R 15 )(CH 2 ) n N(R 13 )(R 14 ), R 3 -R 12 signify hydrogen, halogen, trifluoromethyl, lower alkyl, cycloalkyl, lower alkoxy, hydroxy, nitro, cyano, -N(R 13 ) 2 , phenyl, phenyloxy, benzyl or benzyloxy, or R 6 and R 7 together signify a benzene ring, R 13 -R 15 signify hydrogen, lower alkyl or cycloalkyl and n signifies 1-5, as well as their pharmaceutically acceptable salts. These compounds are suitable for the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease,Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate-deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, chronic pain, dyskinesia and depressions.

    摘要翻译： 本发明涉及下列通式的化合物其中R1表示氢，低级烷基，苯基或苄基，R2表示低级烷基，低级烷氧基，-O（CH2）nN（R13）（R14）， - （CH2）nN（R13 （R14）或-N（R15）（CH2）nN（R13）（R14），R3-R12表示氢，卤素，三氟甲基，低级烷基，环烷基，低级烷氧基，羟基，硝基，氰基， 2，苯基，苯氧基，苄基或苄氧基，或者R6和R7一起表示苯环，R13-R15表示氢，低级烷基或环烷基，n表示1-5，以及它们的药学上可接受的盐。 这些化合物适用于控制或预防急性和/或慢性神经疾病，例如由旁路手术或移植引起的脑功能受限，大脑供血不足，脊髓损伤，头部损伤，妊娠引起的缺氧，心脏骤停 ，低血糖，阿尔茨海默病，亨廷顿舞蹈病，ALS，由AIDS引起的痴呆，眼损伤，视网膜病，认知障碍，由药物引起的特发性帕金森综合征或帕金森综合征以及导致谷氨酸缺陷功能的病症，例如 肌肉痉挛，惊厥，偏头痛，尿失禁，尼古丁成瘾，精神病，鸦片成瘾，焦虑，呕吐，慢性疼痛，运动障碍和沮丧。