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    Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors
    5.
    发明公开
    Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors 有权
    四氢苯并[d]吖庚因和它们作为代谢型谷氨酸受体拮抗剂的用途

    公开(公告)号：EP1074549A2

    公开(公告)日：2001-02-07

    申请号：EP00116091.0

    申请日：2000-07-27

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Adam, Geo ,  Binggeli, Alfred ,  Maerki, Hans-Peter ,  Mutel, Vincent ,  Wilhelm, Maurice ,  Wostl, Wolfgang

    IPC分类号： C07D403/04 ,  A61K31/55 ,  A61P43/00 ,  C07D403/14 ,  C07D401/04 ,  C07D223/04 ,  C07D405/14 ,  C07D487/04 ,  C07D401/14 ,  C07F7/18 ,  C07D471/04 ,  G01N33/50

    CPC分类号： C07D403/04

    摘要： The present invention is concerned with 1,2,4,5-tetrahydro-benzo[d]azepin derivatives of the general formula
    wherein

    R 1 signifies hydrogen, lower alkyl, oxygen, halogen, or

    -OR, -O(C 3 -C 6 )cycloalkyl, -O(CHR) n -(C 3 -C 6 )cycloalkyl, -O(CHR) n CN, -O(CHR) n CF 3 , -O(CHR)(CHR) n NR 2 , -O(CHR)(CHR) n OR, -O(CHR) n -lower alkenyl, -OCF 3 , -OCF 2 -R, -OCF 2 -lower alkenyl, -OCHRF, -OCHF-lower alkenyl, -OCF 2 CRF 2 , -OCF 2 Br, -O(CHR) n CF 2 Br, -O(CHR) n -phenyl, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -O(CHR)(CHR) n -morpholino, -O(CHR)(CHR) n -pyrrolidino, -O(CHR)(CHR) n -piperidino, -O(CHR)(CHR) n -imidazolo, -O(CHR)(CHR) n -triazolo, -O(CHR) n -pyridino, -O(CHR)(CHR) n -OSi-lower alkyl, -O(CHR)(CHR) n OS(O) 2 -lower alkyl, -O(CH 2 ) n CH=CF 2 , -O(CHR) n -2,2-dimethyl-[1.3]dioxolane, -O(CHR) n -CHOR-CH 2 OR, -O(CHR) n -CHOR-(CHR) n -CH 2 OR or
    -SR or -S(CHR) n COOR, or
    -NR 2 , -N(R)(CHR)(CHR) n OR, -N(R)(CHR) n CF 3 , -N(R)(CHR)(CHR) n -morpholino, -N(R)(CHR)(CHR) n -imidazolo, -N(R)(CHR)(CHR) n -pyrrolidino, -N(R)(CHR)(CHR) n -pyrrolidin-2-one, -N(R)(CHR)(CHR) n -piperidino, -N(R)(CHR)(CHR) n -triazolo, -N(R)(CHR) n -pyridino, or

    n is 1-6;
    R signifies hydrogen, lower alkyl or lower alkenyl, independently from each other, if more than one R is present;
    R 2 signifies nitro or cyano;
    R 3 signifies hydrogen, lower alkyl, =O, =S, -SR, -S(O) 2 -lower alkyl, -(C 3 -C 6 )cycloalky or piperazino, optionally substituted by lower alkyl, or

    -CONR 2 , -(CHR) n CONR 2 , -(CHR) n OR, -(CH 2 ) n -CF 3 , -CF 3 , -(CHR) n OC(O)CF 3 , -(CHR) n COOR, -(CHR) n SC 6 H 5 , wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -(CHR) n -1,3-dioxo-1,3-dihydro-isoindol, -(CHR) n -tetrahydro-pyran-2-yloxy or -(CHR) n -S-lower alkyl, or
    -NR 2 , -NRCO-lower alkyl, -NRCHO, -N(R)(CHR) n CN, -N(R)(CHR) n CF 3 , -N(R)(CHR)(CHR) n -OR, -N(R)C(O)(CHR) n O-lower alkyl, -NR(CHR) n -lower alkyl, -NR(CHR)(CHR) n -OR, -N(R)(CHR)(CHR) n -O-phenyl, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -N(R)(CHR) n -lower alkenyl, -N(R)(CHR)(CHR) n -O-(CHR) n OR, -N(R)(CHR) n C(O)O-lower alkyl, -N(R)(CHR) n C(O)NR-lower alkyl, -N(R)(CH 2 ) n -2,2-dimethyl-[1.3]dioxolane, -N(R)(CHR)(CHR) n morpholino, -N(R)(CHR) n -pyridino, -N(R)(CHR)(CHR) n -piperidino, -N(R)(CHR)(CHR) n -pyrrolidino, -N(R)(CHR)(CHR) n -O-pyridino, -N(R)(CHR)(CHR) n imidazolo, -N(R)(CHR) n -CR 2 -(CHR) n -OR, -N(R)(CHR) n -CR 2 -OR, -N(R)(CHR) n -CHOR-CH 2 OR, -N(R)(CHR) n -CHOR-(CHR) n -CH 2 OR, or
    -OR, -O(CHR) n CF 3 , -OCF 3 , -O(CHR)(CHR) n -O-phenyl, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -O(CHR)(CHR) n -O-lower alkyl, -O(CHR) n -pyridino or -O(CHR)(CHR) n -morpholino; and

    R 4 signifies hydrogen, lower alkyl, lower alkenyl or nitro, or

    -OR, -OCF 3 , -OCF 2 -R, -OCF 2 -lower alkenyl, -OCHRF, -OCHF-lower alkenyl, -O(CHR) n CF 3 , or
    -(CHR) n CHRF, -(CHR) n CF 2 R, -(CHR) n CF 3 , -(C 3 -C 6 )cycloalkyl, -(CHR) n (C 3 -C 6 )cycloalkyl, -(CHR) n CN, -(CHR) n -phenyl, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -(CHR)(CHR) n OR, -(CHR) n CHORCH 2 OR, -(CHR)(CHR) n NR 2 , -(CHR) n COOR, -(CHR)(CHR) n OSi-lower alkyl, -(CHR)(CHR) n -OS(O) 2 -lower alkyl, -(CH 2 ) n -CH=CF 2 , -CF 3 , -CF 2 -R, -CF 2 -lower alkenyl, -CHRF, -CHF-lower alkenyl, -(CHR) n -2,2-dimethyl-[1.3]dioxolane, -(CH 2 ) n -2-oxo-azepan-1-yl, -(CHR)(CHR) n -morpholino, -(CHR) n -pyridino, -(CHR)(CHR) n -imidazolo, -(CHR)(CHR) n -triazolo, -(CHR)(CHR) n -pyrrolidino, optionally substituted by -(CH 2 ) n OH, -(CHR)(CHR) n -3-hydroxy-pyrrolidino or -(CHR)(CHR) n -piperidino, or
    -NR 2 , -N(R)(CHR) n -pyridino, -N(R)C(O)O-lower alkyl, -N(CH 2 CF 3 )C(O)O-lower alkyl, -N[C(O)O-lower alkyl] 2 , -NR-NR-C(O)O-lower alkyl or -N(R)(CHR) n CF 3 , -NRCF 3 , -NRCF 2 -R, -NRCF 2 -lower alkenyl, -NRCHRF, -NRCHF-lower alkenyl;
    or is absent, if X is -N= or =N-;
    or R 4 and R 1 or R 3 and R 4 are interconnected to the groups -(CH 2 ) 3-5 -, -(CH 2 ) 2 -N=, -CH=N-N=-, -CH=CH-N=, -NH-CH=CH- or -NR-CH 2 -CH 2 - and form together with the N and C atoms to which they are attached an additional ring;

    R 5 , R 6 signify hydrogen, lower alkyl, lower alkoxy, amino, nitro, -SO 2 NH 2 or halogen; or
    R 5 and R 6 are interconnected to the group -O-CH 2 -O- and form together with the C atoms to which they are attached an additional 5-membered ring;
    R 7 , R 8 signify hydrogen, lower alkyl, lower alkoxy, amino, nitro or halogen;
    R 9 , R 10 signify hydrogen or lower alkyl;
    R 11 , R 12 signifies hydrogen, lower alkyl, hydroxy, lower alkoxy, lower alkoxycarbonyloxy or lower alkanoyloxy;
    R 13 , R 14 signify hydrogen, tritium or lower alkyl;
    R 15 , R 16 signifies hydrogen, tritium, lower alkyl, hydroxy, lower alkoxy, lower alkoxycarbonyloxy or lower alkanoyloxy or are together an oxo group; or
    X signifies -N=, =N-, -N C= or =C
    Y signifies -N=, =N-, -NH-, -CH= or =CH-; and
    the dotted line may be a bond,
    as well as with their pharmaceutically acceptable salts in their racemic and optically active form.
    It has surprisingly been found that the compounds of general formula I are antagonists at metabotropic glutamate receptors and therefore useful for the treatment of diseases related to these receptors.

    5H-Thiazolo (3,2-a) pyrimidine derivatives
    6.
    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。

    5H-Thiazolo (3,2-a) pyrimidine derivatives
    7.
    发明公开
    5H-Thiazolo (3,2-a) pyrimidine derivatives 失效
    -5H-噻唑并〔3,2-α〕pyrimidinderivate

    公开(公告)号：EP0891978A2

    公开(公告)日：1999-01-20

    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： 本发明涉及通式为CHEM的化合物，其中R 1表示氢，低级烷基，苯基或苄基，R 2表示低级烷基，低级烷氧基，-O（CH 2）n N（R 13） ）（R 14）， - （CH 2）n N（R 13）（R 14）或-N（R 15）（CH 2）n N（R 13）（R 14） R 3 -R 12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，-N（R 13）2，苯基，苯氧基，苄基或苄氧基，或 R 6和R 7一起表示苯环，R 13 -R 15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/或慢性神经障碍，例如由旁路手术或移植引起的限制性脑功能，对脑的供血不足，脊髓损伤，头部损伤，怀孕导致的缺氧，心跳骤停 ，低血糖症，阿尔茨海默病，亨廷顿氏舞蹈症，ALS，AIDS引起的痴呆，眼睛损伤，视网膜病变，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乏功能的病症，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。