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    PYRAZOLOPYRIMIDINE AND PYRAZOLOTRIAZINE
    1.
    发明专利
    PYRAZOLOPYRIMIDINE AND PYRAZOLOTRIAZINE 失效

    公开(公告)号：JP2000186090A

    公开(公告)日：2000-07-04

    申请号：JP6114999

    申请日：1999-03-09

    Applicant: HOFFMANN LA ROCHE

    Inventor： BOES MICHAEL ,  RIEMER CLAUS ,  STADLER HEINZ

    IPC: A61K31/00 ,  A61K31/4162 ,  A61K31/505 ,  A61K31/519 ,  A61K31/529 ,  A61K31/53 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D231/54 ,  C07D251/72 ,  C07D487/04 ,  C07D495/14

    Abstract: PROBLEM TO BE SOLVED: To obtain a new pyrazolopyrimidine compound and a new pyrazolotriazine compound which have selective affinity with 5HT-6 receptors and are useful for preventing and treating central nerve disorders such as psychoses, manic depressive psychosis, dysmnesia, and Alzheimer's disease. SOLUTION: Compounds of formula I and II (R1 is phenyl; R2 is H, a lower alkyl or the like; R3 is amino, imidazolyl or the like; R4 is H, a hydroxy-lower alkyl or the like; R5 is H, a halogen or the like), and their salts, for example, 3-benzenesulfonyl-5-methyl-2-methylsulfanyl-pyrazolo[1,5-a]pyrimidin-7 -ylamine. The compound of formula I is obtained by reacting a compound of formula III with a compound of the formula: HR3 and then converting the reaction product into its salt. The compound of formula III is preferably dissolved in DMF, and the compound of the formula: HR3 is also dissolved in DMF or an alcohol, followed by reacting the compounds in the solution. The compound of the formula: HR3 is preferably piperazine, NH3, imidazole, or the like. The compound of formula III is preferably obtained from a compound of formula IV as a starting compound.

    PHENYL- AND PYRIDINYL DERIVATIVES AS NEUROKININ 1 ANTAGONISTS
    4.
    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
    5.
    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。

    PYRIMIDINE DERIVATIVES
    7.
    发明申请
    PYRIMIDINE DERIVATIVES 审中-公开
    吡嗪衍生物

    公开(公告)号：WO0242280A3

    公开(公告)日：2002-08-22

    申请号：PCT/EP0113084

    申请日：2001-11-13

    Applicant: HOFFMANN LA ROCHE

    Inventor： STADLER HEINZ

    IPC: C07D239/36 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/04 ,  A61P1/12 ,  A61P9/00 ,  A61P11/06 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/24 ,  A61P25/30 ,  A61P25/34 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/52 ,  C07D239/56 ,  C07D401/04

    CPC classification number: C07D239/47 ,  C07D239/52 ,  C07D239/56 ,  C07D401/04

    Abstract: The invention relates to compounds of the general formula (I) wherein R is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, -S-lower alkyl, -S(O)2-lower alkyl, -N(R)-(CH2)n-N(R)2, -O-(CH2)n-N(R)2, -N(R)2, or a cyclic tertiary amine which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker -O(CH2)n-; R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R /R is, independently from each other, hydrogen or lower alkyl; R is independently from each other halogen, trifluoromethyl or lower alkoxy; X is-C(O)N(R) or -N(R)C(O)-; Y is -O-,-S-,-SO2-, or -N(R)-; n is 1,2,3 or 4; and m is 0,1 or 2; and to pharmaceutically acceptable acid addition salts thereof. They have a good affitity to the NK1 receptor and they are therefore suitable in the treatment of diseases, related to this receptor.

    Abstract translation: 本发明涉及通式（I）的化合物，其中R 1是低级烷基，低级烷氧基，吡啶基，嘧啶基，苯基，-S-低级烷基，-S（O）2 - 低级烷基，-N（R ） - （CH 2）n N（R）2，-O-（CH 2）n N（R）2，-N（R）2）或可以含有一个另外的选自N，O或S的杂原子的环状叔胺， 并且其中该基团可以通过接头-O（CH 2）n - 与嘧啶环连接; R 2是氢，低级烷基，低级烷氧基，卤素或三氟甲基; R 3 / R 3'彼此独立地为氢或低级烷基; R 4彼此独立地为卤素，三氟甲基或低级烷氧基; X是-C（O）N（R）或-N（R）C（O） - ; Y是-O - ， - S - ， - SO2-或-N（R） - ; n为1,2,3或4; m为0,1或2; 及其药学上可接受的酸加成盐。 它们对NK1受体具有良好的依赖性，因此适用于与该受体有关的疾病的治疗。

    ARYLETHYNYL DERIVATIVES
    9.
    发明专利
    ARYLETHYNYL DERIVATIVES 未知

    公开(公告)号：MY171743A

    公开(公告)日：2019-10-27

    申请号：MYPI2015000777

    申请日：2013-09-23

    Applicant: HOFFMANN LA ROCHE

    Inventor： JAESCHKE GEORG ,  LINDEMANN LOTHAR ,  VIEIRA ERIC ,  STADLER HEINZ

    IPC: C07D413/04 ,  A61K31/444 ,  A61P25/18

    Abstract: The present invention relates to ethynyl derivatives of formula (I) wherein ? R is phenyl, 3-fluorophenyl, 4-fluorophenyl or 2,5-di-fluorophenyl; ? or to a pharmaceutically acceptable acid addition salt, in enantiomerically pure form with the absolute configuration as shown in formula (I). It has now surprisingly been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) which are useful for the treatment of schizophrenia, cognitive disorders, fragile X sydrome or autism and which show advantageous biochemical-, physicochemical- and pharmacodynamic-properties compared to compounds of prior art.

    ETHYNYL DERIVATIVES AS MGLUR5 ALLOSTERIC MODULATORS
    10.
    发明专利
    ETHYNYL DERIVATIVES AS MGLUR5 ALLOSTERIC MODULATORS 未知

    公开(公告)号：MY170822A

    公开(公告)日：2019-09-01

    申请号：MYPI2014001004

    申请日：2012-10-04

    Applicant: HOFFMANN LA ROCHE

    Inventor： JAESCHKE GEORG ,  LINDEMANN LOTHAR ,  VIEIRA ERIC ,  STADLER HEINZ ,  RICCI ANTONIO ,  RUEHER DANIEL

    Abstract: The present invention relates to ethynyl derivatives of formula I. wherein U is Nor CH, R is hydrogen, halogen, lower alkyl or lower alkoxy; Y 1s -N(R r, -0- or -C(R R? )-; wherein R' is hydrogen or lower alkyl and R'IR'' are independently hydrogen, hydroxy, lower alkyl or lower alkoxy; V is -N(R').'or -C(R7R7 ), wherein R' is hydrogen or lower alkyl and R7/R,. are independently from each other hydrogen, lower alkyl, CH -lower alkoxy or may form together with the carl:,on atom to which they are attached a C,-C,-cycloalkyl; R1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; m is O or l; in case m is 1, R'IR3' are independently from each other hydrogen, lower alkyl, CH2-lower alkoxy or may form together with the carbon atom to which they are attached a C3-C6-cycloallcyl; n is O or 1; in case n is 1, R2/R2 are independently from each other hydrogen, lower alkyl, CH2-lower alkoxy or may form together with the carbon atom to which they are attached a C,-C,-cycloalkyl; if m is 1 and n is 0, R' and R7 may form together with the carbon atoms to which they are attached a C..-cycloalkyl; or if mis 1 and n is 1, R2 and R3 or R3 and R7 may form together with the carbon atoms to which they are attached a c.,6-cycloalkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula I are allostetic modulators of the metabotropic glutamate receptor subtype 5 (mGluR5). (No suitable figure)

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