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    5-phenyl-pyrimidine derivatives
    3.
    发明授权
    5-phenyl-pyrimidine derivatives 失效
    5-苯基 - 嘧啶衍生物

    公开(公告)号：US06756380B1

    公开(公告)日：2004-06-29

    申请号：US09575789

    申请日：2000-05-22

    申请人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    发明人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    IPC分类号： C07D23932

    CPC分类号： C07D239/28 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48

    摘要： Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon ring atoms to which they are attached form a fused ring, with the proviso that n for R1 is 1; n is independently 0-2; and X is —C(O)N(R4″)— or —N(R4″)C(O)—; and pharmaceutically acceptable acid addition salts thereof.

    摘要翻译： 描述通式的化合物：其中R 1是氢或卤素; R 2是氢，卤素，低级烷基或低级烷氧基; R 3是卤素，三氟甲基，低级烷氧基或低级烷基; R 4 R 5是氢或低级烷基; R 5是低级烷基，低级烷氧基，氨基，羟基，羟基 - 低级烷基， - （CH 2）n - 哌嗪基，任选被低级烷基取代， （CH2）n-吗啉基， - （CH2）n + 1-咪唑基，-O-（CH2）n + 1-吗啉基，-O-（CH2）n + 1-哌啶基，低级烷基 - ，苄基氨基，-NH-（CH 2）n + 1N（R 4“）2， - （CH 2）n -NH-（CH 2）n + 1N（R 4”）2， - （CH 2） n + 1N（R 4“）2或-O-（CH 2）n + 1N（R 4”）2，其中R 4“是氢或低级烷基; R 6' R 2和R 6或R 1和R 6可以一起为-CH = CH-CH = CH-，其中R 2和R 6或R 1为氢; 和R 6分别与它们所连接的两个碳环原子一起形成稠合环，条件是R 1的n为1; n独立地为0-2; 和X是-C（O）N（R“”） - 或-N（R“”）C（O） - ;及其药学上可接受的酸加成盐。

    Biphenyl derivatives
    5.
    发明授权
    Biphenyl derivatives 失效
    联苯衍生物

    公开(公告)号：US06291465B1

    公开(公告)日：2001-09-18

    申请号：US09513147

    申请日：2000-02-25

    申请人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    发明人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    IPC分类号： C07C23300

    CPC分类号： C07D295/155 ,  C07C217/54 ,  C07C233/15 ,  C07C233/44 ,  C07C233/66 ,  C07C235/42

    摘要： The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy halogen, amino, —N(R6)2 or trifluoromethyl; R1 is hydrogen lower alkoxy or halogen, R and R1 may be together —CH═CH—CH═CH—; R2 is halogen, lower alkyl or trifluoromethyl; R3 is hydrogen or lower alkyl; R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl; R5 is hydrogen, nitro, amino or —N(R6)2; R6 is hydrogen or lower alkyl, X is —C(O)N(R6)—, —(CH2)nO—, (CH2)nN(R6)—, —N(R6)C(O)— or —N(R6)(CH2)n—; and n is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.

    摘要翻译： 本发明涉及式的化合物，其中R是氢，低级烷基，低级烷氧基卤素，氨基，-N（R6）2或三氟甲基; R1是氢低级烷氧基或卤素，R和R1可以一起是-CH = CH-CH = CH-; R 2为卤素，低级烷基或三氟甲基; R 3为氢或低级烷基; R 4为氢或环状叔胺，任选被低级烷基取代; R 5为氢，硝基，氨基或-N（R 6） X是-C（O）N（R6） - ， - （CH2）nO-，（CH2）nN（R6） - ， - （R6）C（O） - 或-N ）（CH 2）n - 和n为1或2;及其药学上可接受的酸加成盐。式I化合物可用于治疗与NK-1受体有关的疾病。

    4-phenyl-pyrimidine derivatives
    7.
    发明授权
    4-phenyl-pyrimidine derivatives 失效
    4-苯基 - 嘧啶衍生物

    公开(公告)号：US06274588B1

    公开(公告)日：2001-08-14

    申请号：US09575382

    申请日：2000-05-22

    申请人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    发明人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    IPC分类号： C07D23924

    CPC分类号： C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04

    摘要： The invention provides compounds of the formula wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R1 and R2 may together be —CH═CH—CH═CH—, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4′ are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, —(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, —(CH2)n-morpholinyl, —(CH2)n-piperidinyl, —(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; and n is 0-2; X is —C(O)N(R4″)— or —N(R4″)C(O)—; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds have a good affinity to the NK-1 receptor and may therefore used for the treatment of diseases related to this receptor.

    摘要翻译： 本发明提供的化合物，其中R 1是氢或卤素; R 2是氢，卤素，低级烷基或低级烷氧基; R 1和R 2一起可以是-CH = CH-CH = CH-，其中R 1和R 2与两个碳环 它们所连接的原子形成稠环; R3是卤素，三氟甲基，低级烷基或低级烷氧基; R4 / R4'各自独立地是氢或低级烷基; R5是低级烷基，低级烷氧基，氨基，苯基，羟基 - 低级 烷基，氰基 - 低级烷基，氨基甲酰基 - 低级烷基，吡啶基，嘧啶基， - （CH2）n-哌嗪基，其任选被一个或两个低级烷基或羟基 - 低级烷基取代， - （CH 2） - （CH 2）n - 哌啶基， - （CH 2）n + 1-咪唑基，低级烷基 - 硫烷基，低级烷基磺酰基，苄基氨基，-NH-（CH 2）n + n + 1N（R4“）2，-O-（CH2）n + 1-吗啉基，-O-（CH2）n + 1-哌啶基或-O-（CH2）n + 1N（R4” 其中R4“是氢或低级烷基; 和n为0-2; X为-C（O）N（R4“） - 或-N（R4”）C（O） - ;以及其药学上可接受的酸加成盐。 对NK-1受体具有良好的亲和性，因此可用于治疗与该受体有关的疾病。

    3-phenyl-pyridine-derivatives
    9.
    发明授权
    3-phenyl-pyridine-derivatives 失效
    3-苯基 - 吡啶衍生物

    公开(公告)号：US06225316B1

    公开(公告)日：2001-05-01

    申请号：US09505359

    申请日：2000-02-16

    申请人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    发明人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    IPC分类号： A61K3150

    CPC分类号： C07D213/75 ,  C07D213/38 ,  C07D213/81

    摘要： The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together —CH═CH—CH═CH—; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, —N(R5)2, —N(R5)S(O)2-lower alkyl, —N(R5)C(O)R5 or a cyclic tertiary amine of the group R5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, —N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, —CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is —C(O)N(R5)—, —(CH2)mO—, —(CH2)mN(R5)—, —N(R5)C(O)—, or —N(R5)(CH2)m—; n is 0-4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.

    摘要翻译： 本发明涉及式Ⅳ的化合物，其中R是氢，低级烷基，低级烷氧基，卤素或三氟甲基; R 1是氢或卤素; 或R 1可以是-CH = CH-CH = CH-; R 2是氢，卤素，三氟甲基，低级烷氧基或氰基; R 3是氢，低级烷基或形成环烷基; R 4是氢，-N（R 5） 2，-N（R 5）S（O）2-低级烷基，-N（R 5）C（O）R 5或基团R 5的环状叔胺彼此独立地为氢，C 3-6 - 环烷基，苄基 或低级烷基; R6是氢，羟基，低级烷基，-N（R5）CO-低级烷基，羟基 - 低级烷基，氰基，-CHO或5-或6-元杂环基，任选地通过亚烷基键合，X 是（C） - （CH 2）m O - ， - （CH 2）m N（R 5） - ， - N（R 5）C（O） - 或-N（R 5） - ; n为0-4; 和m为1或2;以及其药学上可接受的酸加成盐。已经显示上述化合物对NK-1受体具有良好的亲和力。

    Serotonin receptor binding benzo[e]isoindoles and benzo[h]isoquinolines
    10.
    发明授权
    Serotonin receptor binding benzo[e]isoindoles and benzo[h]isoquinolines 失效
    5-羟色胺受体结合苯并[e]异吲哚和苯并[h]异喹啉

    公开(公告)号：US06310208B1

    公开(公告)日：2001-10-30

    申请号：US09003446

    申请日：1998-01-06

    申请人： Michael Bös ,  Heinz Stadler ,  Jürgen Wichmann

    发明人： Michael Bös ,  Heinz Stadler ,  Jürgen Wichmann

    IPC分类号： C07D49156

    CPC分类号： C07D221/10

    摘要： Since the compounds in accordance with the invention can bind to serotonin receptors (5HT2), they are especially suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic attacks, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioral disorders, addiction, obesity, bulimia etc., nervous system damage caused by trauma, stroke, neurodegenerative diseases etc.; cardiovascular disorders such as hypertension, thrombosis, stroke etc.; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

    摘要翻译： 由于根据本发明的化合物可以结合5-羟色胺受体（5HT2），所以它们特别适用于治疗或预防中枢神经障碍如沮丧，双相情感障碍，焦虑状态，睡眠和性障碍，精神病，精神分裂症，偏头痛 以及与头痛或不同类型的疼痛，人格障碍或强迫症，社交恐惧症或惊恐发作，精神有机疾病，儿童精神障碍，侵略性，与年龄有关的记忆障碍和行为障碍，成瘾， 肥胖，贪食等，由创伤，中风，神经变性疾病等引起的神经系统损伤; 心血管疾病如高血压，血栓形成，中风等; 和胃肠道疾病如胃肠道运动功能障碍。