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    Use of phenoxy-piperzine derivatives
    5.
    发明授权
    Use of phenoxy-piperzine derivatives 失效
    苯氧基 - 哌嗪衍生物的使用

    公开(公告)号：US5614526A

    公开(公告)日：1997-03-25

    申请号：US639384

    申请日：1996-04-29

    Applicant: Thierry Godel ,  Deborah Hartman ,  Claus Riemer

    Inventor： Thierry Godel ,  Deborah Hartman ,  Claus Riemer

    IPC: C07D295/08 ,  A61K31/34 ,  A61K31/341 ,  A61K31/495 ,  A61K31/496 ,  A61P25/00 ,  A61P25/18 ,  A61P43/00 ,  C07D307/68

    CPC classification number: A61K31/496 ,  A61K31/495

    Abstract: A method of treating or preventing illnesses caused by a disorder of the dopamine system. The method comprises administering to a host in need of such treatment or prevention an effective amount of a pharmaceutical composition comprising a compound of the formula ##STR1## wherein R.sup.1 and R.sup.3 each independently are hydrogen, aryl, carbamoyl, lower-alkyl-carbonyl, lower-alkyl, halogen, lower-alkyl-carbonyl-amino, lower-alkenyl-carbonyl-amino, amino, arylamino, aryloxy, nitro, aryl-acetyl, lower-alkanoyl-lower-alkyl, alkyl-sulphonyl-amino, ureido or furan-2-yl-carbonyl-amino andR.sup.2 is hydrogen, lower-alkyl, trifluoromethyl, halogen, lower-alkoxy, lower-alkyl-carbonyl or lower-alkyl-carbonyl-amino orR.sup.1 and R.sup.2 together are --OCH.sub.2 O--, --O(CH.sub.2).sub.2 O-- or --(CH.sub.2).sub.3 --,R.sup.4 is hydrogen, halogen, hydroxy, lower-alkyl, lower-alkoxy or nitro,R.sup.5 is hydrogen, halogen or lower-alkoxy,R.sup.6 is hydrogen, lower-alkyl, halogen, hydroxy, amino, lower-alkoxy, trifluoromethyl, nitro or lower-alkyl-carbonyl-amino andR.sup.7 is hydrogen or lower-alky-carbonyl,or a pharmaceutically acceptable salt of a compound of formula I, and a pharmaceutically inert carrier material.

    Abstract translation: 治疗或预防由多巴胺系统紊乱引起的疾病的方法。 该方法包括向需要这种治疗或预​​防的宿主施用有效量的包含下式化合物的药物组合物，其中R 1和R 3各自独立地为氢，芳基，氨基甲酰基，低级 - 烷基 - 羰基， 低级烷基，卤素，低级烷基 - 羰基 - 氨基，低级烯基 - 羰基 - 氨基，氨基，芳基氨基，芳氧基，硝基，芳基 - 乙酰基，低级 - 烷酰基 - 低级 - 烷基，烷基 - 磺酰基 - 氨基，脲基或 呋喃-2-基 - 羰基 - 氨基和R 2是氢，低级 - 烷基，三氟甲基，卤素，低级 - 烷氧基，低级 - 烷基 - 羰基或低级 - 烷基 - 羰基 - 氨基或R 1和R 2一起是-OCH 2 O-，-O（ CH 2）2 O-或 - （CH 2）3 - ，R 4是氢，卤素，羟基，低级烷基，低级烷氧基或硝基，R 5是氢，卤素或低级烷氧基，R 6是氢，低级 - 烷基， ，氨基，低级烷氧基，三氟甲基，硝基或低级 - 烷基 - 羰基 - 氨基和R 7为氢或低级 - 羰基 - 或其药学上可接受的盐 mula I和药学惰性载体材料。

    Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
    8.
    发明授权
    Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation 失效
    可用作神经激肽1受体拮抗剂的二氮杂衍生物及其形成方法

    公开(公告)号：US06452001B2

    公开(公告)日：2002-09-17

    申请号：US09854885

    申请日：2001-05-14

    Applicant: Guido Galley ,  Annick Goergler ,  Thierry Godel ,  Reinhard Heck

    Inventor： Guido Galley ,  Annick Goergler ,  Thierry Godel ,  Reinhard Heck

    IPC: C07D24300

    CPC classification number: C07D401/06 ,  C07D243/14 ,  C07D403/06 ,  C07D409/06 ,  C07D487/04

    Abstract: The invention relates to compounds of the formula wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl; R3 is hydrogen, lower alkyl, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is ═O, ═N(CH2)nCH3 or ═N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group —CR5═N—N═; R5 is hydrogen, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl; n is 0, 1, 2 or 3; and pharmaceutically acceptable acid addition salts and enantiomeric forms thereof. The compounds are useful in the treatment of diseases, related to the NK-1 receptor.

    Abstract translation: 本发明涉及式I的化合物，R 2彼此独立地为芳基或杂芳基，其中杂芳基含有一个或两个选自N，O或S的杂原子，其中芳基或杂芳基任选被1 3个取代基，它们彼此独立地为卤素，CF 3，低级烷氧基或低级烷基; R 3为氢，低级烷基， - （CH 2）n N（R）2， - （CH 2）n - 杂芳基或为 - （CH 2 ）杂环任选被卤素，CF 3，低级烷氧基或低级烷基取代; R 4是= O，= N（CH 2）n CH 3或= N（CH 2）n N（R）2; R 3和R 4可以 与它们所连接的N和C原子一起是-CR5 = NN =; R 5是氢， - （CH 2）n N（R）2， - （CH 2）n - 杂芳基或是 - （CH 2）n - 非芳族杂环，所述杂环任选被卤素，CF 3，低级烷氧基或低级烷基取代; R为氢或低级烷基; n为0,1,2或3;及其药学上可接受的酸加成盐及其对映体形式。 该化合物可用于治疗与NK-1受体有关的疾病。

    3-phenyl-pyridine-derivatives
    10.
    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

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

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

    IPC: A61K3150

    CPC classification number: C07D213/75 ,  C07D213/38 ,  C07D213/81

    Abstract: 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.

    Abstract translation: 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。

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