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    2-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-N-[6-(1,1-DIOXO-1lambd6-THIOMORPHOLIN-4-YL)-4-(2-METHYL OR 4-FLUORO-2-METHYL SUBSTITUTED)PHENYL-PYRIDIN-3-YL]-N-METHYL-ISOBUTYRAMIDE
    4.
    发明申请
    2-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-N-[6-(1,1-DIOXO-1lambd6-THIOMORPHOLIN-4-YL)-4-(2-METHYL OR 4-FLUORO-2-METHYL SUBSTITUTED)PHENYL-PYRIDIN-3-YL]-N-METHYL-ISOBUTYRAMIDE 审中-公开
    2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1-氨基-6-吗啉-4-基）-4-（2-甲基或4-氟-2-甲基取代的 ）苯基 - 吡啶-3-基] -N-甲基 - 异丁酰胺

    公开(公告)号：WO03011860A3

    公开(公告)日：2003-09-04

    申请号：PCT/EP0208311

    申请日：2002-07-26

    Applicant: HOFFMANN LA ROCHE

    Inventor： BALLARD THERESA MARIA ,  HOFFMANN TORSTEN ,  POLI SONIA MARIA ,  SCHNIDER PATRICK ,  SLEIGHT ANDREW

    IPC: A61K31/541 ,  A61P1/00 ,  A61P1/08 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/02 ,  A61P13/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D213/75

    CPC classification number: C07D213/75

    Abstract: The invention relates to the compounds 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambd6-thiomorpholin-4-yl)-4-o-tolyl-pyridin-3-yl]-N-methyl-isobutyramide and 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambd6 -thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide, which may be used for the treatment of migraine, rheumatoid arthritis, asthma, bronchial hyperreactivity, inflammatory bowel disease or for the treatment of disorders including Parkinson's disease, anxiety, depression, pain, headache, Alzheimer's disease, multiple sclerosis,oedema, allergic rhinitis, Crohn's disease, ocular injury, ocular inflammatory diseases, psychosis, motion sickness, induced vomiting, emesis, urinary incontinence, psychoimmunologic or psychosomatic disorders, cancer, withdrawel symptoms of addictive drugs from opiates or nicotine, traumatic brain injury or benign prostatic hyperplasia.

    Abstract translation: 本发明涉及化合物2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1,11-硫代吗啉-4-基）-4-邻甲苯基 - 吡啶-3-基 - 基] -N-甲基 - 异丁酰胺和2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1-氨基-6-硫代吗啉-4-基）-4-（4- 氟-2-甲基 - 苯基） - 吡啶-3-基] -N-甲基 - 异丁酰胺，其可用于治疗偏头痛，类风湿性关节炎，哮喘，支气管高反应性，炎性肠病或用于治疗疾病，包括 帕金森病，焦虑症，抑郁症，疼痛，头痛，阿尔茨海默氏病，多发性硬化症，水肿，过敏性鼻炎，克罗恩病，眼部损伤，眼部炎症性疾病，精神病，运动病，诱发性呕吐，呕吐，尿失禁，心理免疫或心身疾病， 癌症，从阿片剂或尼古丁，外伤性脑损伤或良性前列腺增生症中消除上瘾药物的症状。

    NK1 ANTAGONISTS
    5.
    发明申请
    NK1 ANTAGONISTS 审中-公开
    NK1拮抗剂

    公开(公告)号：WO2006089658A3

    公开(公告)日：2006-12-21

    申请号：PCT/EP2006001310

    申请日：2006-02-14

    Applicant: HOFFMANN LA ROCHE ,  HOFFMANN TORSTEN ,  SCHNIDER PATRICK

    Inventor： HOFFMANN TORSTEN ,  SCHNIDER PATRICK

    IPC: C07D213/75 ,  A61K31/44 ,  A61P25/18 ,  C07D213/82

    CPC classification number: C07D213/75 ,  C07D213/82

    Abstract: The present invention relates to compounds of the formula (I), wherein R 1 /R 1' are hydrogen or methyl; X is -C(O)N(CH 3 )- or -N(CH 3 )C(O)-; and to pharmaceutically acceptable acid addition salts thereof for the treatment of numerous inflammatory conditions, migraine, rheumatoid arthritis, asthma, inflammatory bowel disease, mediation of the emetic reflex, Parkinson's disease, anxiety, depression, psychosis, motion sickness, induced vomiting, pain, headache, migraine, Alzheimer's disease, multiple sclerosis, attenuation of morphine withdrawal, cardiovascular changes, oedema, such as oedema caused by thermal injury, chronic inflammatory diseases such as rheumatoid arthritis, asthma/bronchial hyperreactivity and other respiratory diseases including allergic rhinitis, inflammatory diseases of the gut including ulcerative colitis and Crohn's disease, ocular injury and ocular inflammatory diseases, traumatic brain injury, motion sickness, emesis and psychoimmunologic or psychosomatic disorders.

    Abstract translation: 本发明涉及式（I）的化合物，其中R 1，R 1，R 1'是氢或甲基; X是-C（O）N（CH 3） - 或-N（CH 3）C（O） - ; 及其药学上可接受的酸加成盐用于治疗许多炎性疾病，偏头痛，类风湿性关节炎，哮喘，炎性肠病，催吐反射介导，帕金森病，焦虑症，抑郁症，精神病，晕动病，诱发的呕吐，疼痛， 头痛，偏头痛，阿尔茨海默病，多发性硬化症，吗啡戒断减弱，心血管改变，水肿如热损伤引起的水肿，慢性炎性疾病如类风湿性关节炎，哮喘/支气管高反应性和其他呼吸系统疾病，包括过敏性鼻炎，炎性疾病 包括溃疡性结肠炎和克罗恩病，眼部损伤和眼部炎性疾病，创伤性脑损伤，晕动病，呕吐和精神免疫或心身疾病。

    PHENYL- AND PYRIDINYL DERIVATIVES AS NEUROKININ 1 ANTAGONISTS
    7.
    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。

    5-PHENYL-PYRIMIDINE DERIVATIVES
    8.
    发明申请
    5-PHENYL-PYRIMIDINE DERIVATIVES 审中-公开
    5-苯基 - 吡啶衍生物

    公开(公告)号：WO0073278A2

    公开(公告)日：2000-12-07

    申请号：PCT/EP0004702

    申请日：2000-05-24

    Applicant: HOFFMANN LA ROCHE

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

    IPC: A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/08 ,  A61P9/00 ,  A61P11/02 ,  A61P11/06 ,  A61P17/02 ,  A61P25/00 ,  A61P25/06 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D213/00 ,  C07D239/00 ,  C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D295/00 ,  C07D401/04

    CPC classification number: C07D239/28 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48

    Abstract: The invention relates to compounds of general formula (I) wherein R is hydrogen or halogen; R is hydrogen, halogen, lower alkyl or lower alkoxy; R is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R /R are independently from each other hydrogen or lower alkyl; R 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(R )2, -(CH2)n-NH-(CH2)n+1N(R )2, -(CH2)n+1N(R )2, or -O-(CH2)n+1N(R )2, wherein R is hydrogen or lower alkyl; R is hydrogen; R and R or R and R may be together with the two carbon ring atoms -CH=CH-CH=CH-, with the proviso that n for R is 1; n is independently 0 - 2; and X is -C(O)N(R )- or -N(R )C(O)-; and pharmaceutically acceptable acid addition salts thereof. Compounds of formula (I) have a high affinity to the NK-1 receptor. They are therefore useful for the treatment or diseases which relate to this receptor.

    Abstract translation: 本发明涉及通式（I）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 4彼此独立地为氢或低级烷基; - （CH 2）n - 吗啉基， - （CH 2）n + 1-烷基， - （CH 2）n - 咪唑基，-O-（CH 2）n + 1-吗啉基，-O-（CH 2）n + 1-哌啶基，低级烷基 - 硫烷基，低级烷基 - 磺酰基，苄基氨基，-NH-（CH 2）n + 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是氢; R 2和R 6或R 1和R” 6>可以与两个碳环原子-CH = CH-CH = CH-一起，条件是R 1的n为1; n独立地为0-2;且X为-C（O）N （R 4） - 或-N（R 4）C（O） - 及其药学上可接受的酸加成盐。式（I）化合物对NK-1受体具有高亲和力 因此可用于与该受体相关的治疗或疾病。

    PYRROLIDINE DERIVATIVES AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS
    10.
    发明专利
    PYRROLIDINE DERIVATIVES AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS 未知

    公开(公告)号：CA2682506C

    公开(公告)日：2016-05-24

    申请号：CA2682506

    申请日：2008-04-09

    Applicant: HOFFMANN LA ROCHE

    Inventor： BISSANTZ CATERINA ,  HOFFMANN TORSTEN ,  JABLONSKI PHILIPPE ,  KNUST HENNER ,  NETTEKOVEN MATTHIAS ,  RATNI HASANE ,  WU XIHAN

    IPC: C07D207/14 ,  A61K31/5377 ,  A61P25/28 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D471/10

    Abstract: The invention relates to pyrrolidine derivatives of formula (I) wherein R1 is hydrogen, halogen or lower alkyl; R2 is hydrogen, halogen, lower alkoxy or lower alkyl substituted by halogen; R3 is -(CH2)p-heterocyclyl optionally substituted by lower alkyl, halogen, -S(O)2-lower alkyl, -C(O)-lower alkyl, -C(O)O-lower alkyl, hydroxy, lower alkyl substituted by hydroxy, -(CH2)p-O-lower alkyl, -NHCO-lower alkyl, or is C3-6-cycloalkyl optionally substituted by =O, -(CH2)p-O-lower alkyl or lower alkinyl, or is unsubstituted or substituted aryl or heteroaryl, wherein the substituents are selected from the group consisting of lower alkyl, CN, -S(O)2-lower alkyl, halogen, -C(O) -lower alkyl, hydroxy, lower alkoxy or lower alkoxy substituted by halogen; or is -(CH2)P-NR4R5; R4/R5 are independently from each other hydrogen, lower alkyl, -(CRR')p-lower alkyl substituted by hydroxy, -(CRR')p-O-lower alkyl, -(CRR')p-S-lower alkyl, -(CRR')p-O-lower alkyl substituted by hydroxy or C3-6-cycloalkyl; R/R' are independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; o is 1 or 2; P is 0, 1, 2, 3 or 4; or to pharmaceutically active acid-addition salts thereof.

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