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    2-IMIDAZOLINES
    11.
    发明申请
    2-IMIDAZOLINES 审中-公开
    2-咪唑啉

    公开(公告)号：WO2009003868A2

    公开(公告)日：2009-01-08

    申请号：PCT/EP2008057989

    申请日：2008-06-24

    Applicant: HOFFMANN LA ROCHE ,  GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN ,  NORCROSS ROGER ,  STALDER HENRI

    Inventor： GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN ,  NORCROSS ROGER ,  STALDER HENRI

    IPC: C07D233/10 ,  A61K31/415 ,  A61K31/4155 ,  A61P25/00 ,  C07D233/20 ,  C07D233/22 ,  C07D233/24 ,  C07D233/42 ,  C07D233/50 ,  C07D233/52 ,  C07D405/12

    CPC classification number: C07D233/24 ,  C07D233/20 ,  C07D233/22 ,  C07D233/42 ,  C07D233/52 ,  C07D405/12

    Abstract: The present invention relates to compounds of formula (I) wherein X-Y is -N(R2) -CH(R3)-, CH(R3)-N(R2)-, -NH-NH-, -O-CHR3-, -CHR3-O-, -S-CHR3, -CHR3-S- or -CHR3-CHR3 -; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, -(CH2)o-phenyl optionally substituted by lower alkoxy, -(CH2)o-C(O)-phenyl optionally substituted by lower alkoxy, -(CH2)o-O-phenyl optionally substituted by lower alkoxy, -(CH2)o-O-phenyl, CF3, cycloalkyl, NO2, amino or hydroxy; R2 is hydrogen, lower alkyl, phenyl optionally substituted by hydroxy or benzyl; R3/R3' are independently from each other hydrogen, lower alkyl or benzyl; Ar is phenyl, naphthyl, benzofuranyl or benzo [1,3] dioxolyl; n is 1, 2, 3 or 4; o is 0, 1, 2, 3 and to their pharmaceutically active salts, It has been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

    Abstract translation: 本发明涉及式（I）化合物，其中XY是-N（R2）-CH（R3） - ，CH（R3）-N（R2） - ， - NH-NH-，-O-CHR3-， - CHR 3 -O-，-S-CHR 3，-CHR 3 -S-或-CHR 3 -CHR 3 - ; 任选被低级烷氧基取代的 - （CH 2）o C（O） - 苯基，任选被低级烷氧基取代的 - （CH 2）o O-苯基， - （CH 2） （CH 2）o O-苯基，CF 3，环烷基，NO 2，氨基或羟基; R2是氢，低级烷基，任意被羟基或苄基取代的苯基; R3 / R3'彼此独立地为氢，低级烷基或苄基; Ar是苯基，萘基，苯并呋喃基或苯并[1,3]二氧杂环戊烯基; n为1,2,3或4; o是0,1,2,3及其药学活性盐。已经发现式（I）化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。 这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病， 癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病 。

    USE OF SUBSTITUTED 2-IMIDAZOLE OF IMIDAZOLINE DERIVATIVES
    12.
    发明申请
    USE OF SUBSTITUTED 2-IMIDAZOLE OF IMIDAZOLINE DERIVATIVES 审中-公开
    使用取代的咪唑啉衍生物的2-咪唑

    公开(公告)号：WO2007085557A3

    公开(公告)日：2007-09-20

    申请号：PCT/EP2007050443

    申请日：2007-01-17

    Applicant: HOFFMANN LA ROCHE ,  GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN ,  HOENER MARIUS ,  KOLCZEWSKI SABINE ,  NORCROSS ROGER ,  STALDER HENRI

    Inventor： GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN ,  HOENER MARIUS ,  KOLCZEWSKI SABINE ,  NORCROSS ROGER ,  STALDER HENRI

    IPC: A61K31/4164 ,  A61K31/4174 ,  A61P25/00 ,  C07D233/06 ,  C07D233/54 ,  C07D401/04 ,  C07D405/06 ,  C07D409/06

    CPC classification number: C07D233/06 ,  A61K31/4164 ,  A61K31/4178 ,  C07D233/20 ,  C07D233/22 ,  C07D233/56 ,  C07D233/64 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06

    Abstract: The present invention relates to the use of compounds of Formula (I), wherein R is hydrogen, tritium, hydroxy, amino, lower alkyl, cycloalkyl, lower alkoxy, halogen, cyano, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, phenyl, O-phenyl, -S-phenyl, optionally substituted by halogen, or is benzyl, benzyloxy, NHC(O)-lower alkyl or pyridin-2,3 or 4-yl; R 1 is hydrogen, hydroxy or lower alkyl; R 2 is hydrogen or lower alkyl; aryl is an aromatic group, selected from phenyl, naphthalen-1-yl or naphthalen-2-yl; hetaryl is an aromatic group, containing at least one O, N or S ring atom, selected from the group consisting of pyridine-3-yl, pyrazolyl, benzofuran-3-yl, benzofuran-4-yl, benzofuran-5-yl, benzofuran-6-yl, benzofuran-7-yl, thiophen-2-yl, thiophen-3-yl, benzo[b]thiophen-3-yl or indol-3-yl; n is 1, 2, 3, 4 or 5; when n is 2, 3, 4 or 5, R may be the same or not; the dotted line may be a bond or not; and to their pharmaceutically active salts for the preparation of medicaments for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

    Abstract translation: 本发明涉及式（I）化合物的用途，其中R是氢，氚，羟基，氨基，低级烷基，环烷基，低级烷氧基，卤素，氰基，被卤素取代的低级烷基， 苯基，O-苯基，-S-苯基，任选被卤素取代，或者是苄基，苄氧基，NHC（O） - 低级烷基或吡啶-2,3或4-基; R 1是氢，羟基或低级烷基; R 2是氢或低级烷基; 芳基是选自苯基，萘-1-基或萘-2-基的芳族基团; 杂芳基是含有至少一个O，N或S环原子的芳族基团，其选自吡啶-3-基，吡唑基，苯并呋喃-3-基，苯并呋喃-4-基，苯并呋喃-5-基， 苯并呋喃-6-基，苯并呋喃-7-基，噻吩-2-基，噻吩-3-基，苯并[b]噻吩-3-基或吲哚-3-基; n是1,2,3,4或5; 当n为2,3,4或5时，R可以相同或不同; 虚线可能是债券或不是; 及其药物活性盐在制备用于治疗抑郁症，焦虑症，双相性精神障碍，注意力缺陷多动障碍，压力相关障碍，精神障碍如精神分裂症，神经疾病如帕金森病，神经变性病症例如 阿尔茨海默病，癫痫，偏头痛，高血压，物质滥用和代谢障碍，例如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和功能障碍，睡眠和昼夜节律紊乱， 和心血管疾病。

    PHENYL- AND PYRIDINYL DERIVATIVES AS NEUROKININ 1 ANTAGONISTS
    13.
    发明申请
    PHENYL- AND PYRIDINYL DERIVATIVES AS NEUROKININ 1 ANTAGONISTS 审中-公开
    苯并吡啶衍生物作为神经营养因子1拮抗剂

    公开(公告)号：WO0050398A3

    公开(公告)日：2001-04-05

    申请号：PCT/EP0001224

    申请日：2000-02-15

    Applicant: HOFFMANN LA ROCHE

    Inventor： BOES MICHAEL ,  GALLEY GUIDO ,  GODEL THIERRY ,  HOFFMANN TORSTEN ,  HUNKELER WALTER ,  SCHNIDER PATRICK ,  STADLER HEINZ

    IPC: C07C211/44 ,  A61K31/167 ,  A61K31/44 ,  A61P25/00 ,  A61P29/00 ,  C07C211/54 ,  C07C233/29 ,  C07C233/33 ,  C07C233/44 ,  C07C317/14 ,  C07C317/40 ,  C07C323/41 ,  C07D213/75 ,  C07D213/79 ,  C07D213/81 ,  C07D295/12 ,  C07D295/135 ,  C07D401/04

    CPC classification number: C07D213/75 ,  C07C233/29 ,  C07C233/33 ,  C07C233/44 ,  C07C317/40 ,  C07C323/41 ,  C07D295/135

    Abstract: The invention relates to compounds of general formula (I), wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R is hydrogen or halogen; or R and R may be together -CH=CH-CH=CH-; R is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R is independently from each other hydrogen, lower alkyl or form a cycloalkyl group; R is hydrogen, halogen, lower alkyl, lower alkoxy, -N(R )2, -N(R )S(O)2-lower alkyl, -N(R )C(O)R or a cyclic tertiary amine of the group (a); R is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R is hydrogen, hydroxy, lower alkyl, -N(R )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(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R ) C(O)-, C(O)O- or -N(R )(CH2)m-; Y is -(CH2)n-, -O-, -S-, SO2-, -C(O)- or -N(R )-; Z is =N-, -CH= or -C(C1)=; n is 0 - 4; and, is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formula (I) have a high affinity to the NK-1 receptor.

    Abstract translation: 本发明涉及通式（I）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和R 1可以一起是-CH = CH-CH = CH-; R 2是氢，卤素，三氟甲基，低级烷氧基或氰基; R 3彼此独立地为氢，低级烷基或形成环烷基; R 4是氢，卤素，低级烷基，低级烷氧基，-N（R 5）2，-N（R 5）S（O）2-低级烷基，-N（R 5） C（O）R 5或（a）组的环状叔胺; R 5彼此独立地为氢，C 3-6 - 环烷基，苄基或低级烷基; R 6是氢，羟基，低级烷基，-N（R 5）CO-低级烷基，羟基 - 低级烷基，氰基，-CHO或5-或6-元杂环基，任选经由亚烷基键合 ，X是-C（O）N（R 5） - ， - （CH 2）m O - ， - （CH 2）m N（R 5） - ， - N（R 5）C（O） ，C（O）O-或-N（R 5）（CH 2）m - ; Y是 - （CH 2）n - ， - O - ， - S - ，SO 2 - ， - C（O） - 或-N（R 5） Z是= N-，-CH =或-C（C1）=; n为0-4; 是1或2; 及其药学上可接受的酸加成盐。 已经表明式（I）化合物对NK-1受体具有高亲和力。

    Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson
    15.
    发明专利
    Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson 未知

    公开(公告)号：MA37944B2

    公开(公告)日：2017-10-31

    申请号：MA37944

    申请日：2013-09-11

    Applicant: HOFFMANN LA ROCHE ,  HOFFMANN-LA ROCHE INC

    Inventor： GALLEY GUIDO ,  NORCROSS ROGER ,  PFLIEGER PHILIPPE

    IPC: A61K31/4155 ,  A61K31/454 ,  A61K31/5377 ,  A61P25/00 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

    Abstract: La présente invention concerne des composés de formule (i) dans laquelle r1 est phényle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alcoxy inférieur, cyano, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy, alcoxy inférieur substitué par halogène ou alcoxy inférieur substitué par hydroxy ; ou est pyridine-2, 3 ou 4-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, cyano, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy, alcoxy inférieur, alcoxy inférieur substitué par halogène ou alcoxy inférieur substitué par hydroxyle ; ou est pyrimidin-2, 4 ou 5-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alkyle inférieur substitué par hydroxy ou alkyle inférieur substitué par halogène ; ou est pyrazin-2-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy ou cyano ; ou est 2,2-difluorobenzo[d][1,3]dioxol-5-yle, ou est thiazolyle, facultativement substitué par alkyle inférieur substitué par halogène ; r2 est hydrogène ou alkyle inférieur ; r3 est hydrogène, amino ou alkyle inférieur ; z est une liaison, -ch2- ou -o- ; ou un sel d'addition d’acide pharmaceutiquement adapté. Il a maintenant été découvert que les composés de formule i ont une bonne affinité pour les récepteurs associés aux amines traces (taar), notamment taar1. Les composés peuvent être utilisés pour le traitement de la dépression, des troubles anxieux, du trouble bipolaire, de l'hyperactivité avec déficit de l'attention (adhd), des troubles relatifs au stress, des troubles psychotiques tels que la schizophrénie, des maladies neurologiques telles que la maladie de parkinson, des maladies neurodégénératives telles que la maladie d'alzheimer, de l'épilepsie, de la migraine, de l'hypertension, de l'abus d'alcool ou d'autres drogues et de troubles métaboliques tels que les troubles de l'alimentation, le diabète, les complications diabétiques, l'obésité, la dyslipidémie, les troubles de la consommation d'énergie et de l'assimilation, les troubles et le mauvais fonctionnement de l'homéostasie de la température corporelle, les troubles du sommeil et du rythme circadien, et les troubles cardiovasculaires.

    Derivados de benzamida substituídas e composição farmacêutica que os compreende
    17.
    发明专利
    Derivados de benzamida substituídas e composição farmacêutica que os compreende 未知

    公开(公告)号：BR112013030698B1

    公开(公告)日：2022-05-31

    申请号：BR112013030698

    申请日：2012-06-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： GALLEY GUIDO ,  PFLIEGER PHILIPPE ,  TRUSSARDI RENÉ ,  NORCROSS ROGER

    IPC: C07D265/30 ,  A61K31/4245 ,  A61P25/00 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

    Abstract: derivados de benzamida substituídas. a presente invenção refere-se aos compostos de fórmula em que r1 é hidrogênio, halogênio, ciano, alquila inferior, alquila inferior substituída por halogênio, alcóxi inferior, alcóxi inferior substituído por halogênio ou c(o)nh2, ou é fenila opcionalmente substituída por halogênio, ciano ou alcóxi inferior substituído por halogênio, ou é 2,2-difluorobenzo[d][1,3]dioxol-5-ila, ou é 6-(trifluorometil)pirazin-2-ila ou 5-(trifluorometil)pirazin-2-ila ou é 6-(trifluorometil)pirimidin-4-ila, ou é 6-(trifluorometil)piridin-3-ila, ou é 5-cianopirazin-2-ila ou é 2-(trifluorometil)pirimidin-4-ila; n é 1 ou 2 r2 é halogênio, alquila inferior ou ciano e r3 é hidrogênio, ou r2 é hidrogênio e r3 é halogênio, alquila inferior ou ciano; x é uma ligação, -nr'-, -ch2nh- ou -chr'-; r' é hidrogênio ou alquila inferior; z é uma ligação, -ch2- ou -o-; ar é fenila ou é heteroarila, selecionada a partir do grupo consistindo em 1h-indazol-3ila, piridina-2-ila, piridina-3-ila, piridina-4-ila, pirimidina-5-ila, 1h-pirazol-3-ila, 1h-pirazol-4-ila ou 1h-pirazol-5-ila; ou a um sal de adição de ácido farmaceuticamente adequado dos mesmos, que podem ser usados no tratamento da depressão, distúrbios de ansiedade, desordem bipolar, desordem da hiperatividade por déficit de atenção (adhd), desordens relacionadas com o estresse, desordens de psicoses, esquizofrenia, doenças neurológicas, doença de parkinson, distúrbios neurodegenerativas, doença de alzheimer, epilepsia, enxaqueca, hipertensão, abuso de drogas, desordens metabólicas, distúrbios alimentares, diabetes, complicações diabéticas, obesidade, dislipidemia, desordens do consumo de energia e assimilação, doenças e mau funcionamento da homeostase da temperatura corporal, perturbações do sono e do ritmo circadiano, e distúrbios cardiovasculares.

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