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1. 发明申请

US20200339522A1 PHENOXYMETHYL DERIVATIVES 审中-公开
公开(公告)号：US20200339522A1
公开(公告)日：2020-10-29
申请号：US16811656
申请日：2020-03-06
申请人： Hoffmann-La Roche Inc.
发明人： Jerome HERT , Daniel HUNZIKER , Holger KUEHNE , Thomas LUEBBERS , Rainer E. MARTIN , Patrizio MATTEI , Werner NEIDHART , Hans RICHTER , Markus RUDOLPH , Emmanuel PINARD
IPC分类号： C07D249/08 , C07D487/04 , C07D249/12 , C07D409/12 , C07D413/12 , C07D231/12 , C07F7/08 , C07D401/12 , C07D407/12 , C07D407/04 , C07D471/04 , C07D237/14 , C07D403/12 , C07D417/12 , C07D231/56 , A61P27/02 , C07B41/04 , C07D231/20 , C07D249/04
摘要： The invention provides novel compounds having the general formula (I) wherein RA, RB, RC, RC1 and W are as defined herein, compositions including the compounds and methods of using the compounds.

2. 发明申请

US20160326144A1 FLOURO-NAPHTHYL DERIVATIVES 有权
标题翻译：甲基衍生物
公开(公告)号：US20160326144A1
公开(公告)日：2016-11-10
申请号：US15216435
申请日：2016-07-21
申请人： Hoffmann-La Roche Inc.
发明人： Katrin GROEBKE ZBINDEN , Emmanuel PINARD , Thomas RYCKMANS
IPC分类号： C07D405/14 , C07D213/56 , C07D309/14 , C07D401/04 , C07D213/61 , C07D405/12
CPC分类号： C07D405/14 , C07D213/56 , C07D213/61 , C07D309/14 , C07D401/04 , C07D405/12
摘要： The present invention relates to compounds of formula wherein R1 is C4-6-cycloalkyl or C4-6-heterocycloalkyl, which are optionally substituted by one or two substituents, selected from hydroxy or lower alkyl; A is phenyl, pyridinyl or piperidinyl; R2 is hydrogen, halogen, lower alkyl, cyano, C4-6-cycloalkyl, lower alkoxy, lower alkoxy substituted by halogen, or is a five- or six-membered heteroaryl, optionally substituted by lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.
摘要翻译：该化合物可用于治疗或预防阿尔茨海默氏病，认知障碍，精神分裂症，疼痛或睡眠障碍。

3. 发明申请

US20230135093A1 TRIAZOLYL DERIVATIVES AS GABA A ALPHA5 PAM 有权
公开(公告)号：US20230135093A1
公开(公告)日：2023-05-04
申请号：US18054651
申请日：2022-11-11
申请人： Hoffmann-La Roche Inc.
发明人： Giuseppe CECERE , Guillaume DÉCORET , Katrin GROEBKE ZBINDEN , Maria-Clemencia HERNANDEZ , Henner KNUST , Andreas KOBLET , Andres Miguel OLIVARES MORALES , Emmanuel PINARD , Valerie RUNTZ-SCHMITT
IPC分类号： C07D413/14 , C07D403/06 , C07D401/14 , C07D403/14 , C07D491/107
摘要： The invention provides compounds having the general formula (I) or (II) wherein R1, R2, R3, X, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.

4. 发明申请

US20230123268A1 AMINO-PYRIMIDINE CYCLO-AMIDES 有权
公开(公告)号：US20230123268A1
公开(公告)日：2023-04-20
申请号：US18062892
申请日：2022-12-07
申请人： Hoffmann-La Roche Inc.
发明人： Angélica BEURIER , Luke GREEN , Christian KRAMER , Dmitry MAZUNIN , Emmanuel PINARD , Hasane RATNI
IPC分类号： C07D487/04 , C07D471/04
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and n are as defined herein, compositions including methods of making the compounds and using the compounds as ATX inhibitors.

5. 发明申请

US20190300516A1 ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM 审中-公开
公开(公告)号：US20190300516A1
公开(公告)日：2019-10-03
申请号：US16432584
申请日：2019-06-05
申请人： Hoffmann-La Roche Inc.
发明人： Bernd BUETTELMANN , Giuseppe CECERE , Bernhard FASCHING , Katrin GROEBKE ZBINDEN , Maria-Clemencia HERNANDEZ , Henner KNUST , Andreas KOBLET , Emmanuel PINARD , Andrew THOMAS
IPC分类号： C07D413/14 , C07D471/04 , C07D487/10 , A61P25/28
摘要： Compounds having the formula (I) wherein R1, R2, R3, R4, R5, R6, X, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.

6. 发明申请

US20230112172A1 SUBSTITUED AMINO-PYRIMIDINES 有权
公开(公告)号：US20230112172A1
公开(公告)日：2023-04-13
申请号：US18062896
申请日：2022-12-07
申请人： Hoffmann-La Roche Inc.
发明人： Virginie BROM , Luke GREEN , Christian KRAMER , Dmitry MAZUNIN , Emmanuel PINARD , Hasane RATNI
IPC分类号： C07D413/04 , C07D403/04
摘要： The invention provides novel compounds having the general formula I wherein R1, R2, and R3 are as defined herein, compositions including the compounds and methods of using the compounds.

7. 发明申请

US20170197969A1 COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY 有权
公开(公告)号：US20170197969A1
公开(公告)日：2017-07-13
申请号：US15379057
申请日：2016-12-14
申请人： Hoffmann-La Roche Inc.
发明人： Emmanuel PINARD , Hasane RATNI , Luke GREEN , Patrick WILLIAMSON
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides compounds of formula (I) wherein A, X1, X2, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.

8. 发明申请

US20160194321A1 PYRROLOPYRIDINE OR PYRAZOLOPYRIDINE DERIVATIVES 有权
标题翻译：吡咯并吡啶或吡唑并吡啶衍生物
公开(公告)号：US20160194321A1
公开(公告)日：2016-07-07
申请号：US15068096
申请日：2016-03-11
申请人： Hoffmann-La Roche Inc.
发明人： Theresa Maria BALLARD , Emmanuel PINARD , Herve SCHAFFHAUSER , Katrin GROEBKE ZBINDEN , Thomas RYCKMANS , Alexander FLOHR
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula wherein R1 halogen, lower alkyl, lower alkoxy, cyano, phenyl, C(O)NHCH3, C(O)NH2, lower alkyl substituted by halogen or is a five-membered heteroaryl group, optionally substituted by lower alkyl; Y1 is N or CH; Y2 is CH; and if Y1 is CH, Y1 and Y2 may form together with the C-atoms to which they are attached a ring, containing —CH═N—N(CH3)—, —CH═N—N(H)—; X is CH or N; R is (CH2)m-cycloalkyl, optionally substituted by hydroxy, lower alkoxy or lower alkyl, or is tetrahydropyran, optionally substituted by hydroxy, or is lower alkoxy, substituted by hydroxy, or is lower alkyl substituted by one or two hydroxy, or is (CH2)m-pyridinyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, or is L-phenyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, and L is a bond, —CH(CH2OH)— or —CH2CH(OH)—; n is 0, 1 or 2; m is 0 or 1; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds of the present invention are muscarinic M1 receptor positive allosteric modulators (PAM) and hence are useful in the treatment of diseases, mediated by the muscarinic M1 receptor, such as Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.
摘要翻译：本发明涉及下式的化合物其中R1卤素，低级烷基，低级烷氧基，氰基，苯基，C（O）NHCH3，C（O）NH2，被卤素取代的低级烷基或是五元杂芳基，通过低级烷基; Y1是N或CH; Y2是CH; 并且如果Y 1是CH，则Y 1和Y 2可以与它们所连接的含有-CH = N-N（CH 3） - ， - CH = N-N（H） - 的环的C原子一起形成。 X是CH或N; R是任选被羟基，低级烷氧基或低级烷基取代的（CH 2）m - 环烷基，或任选被羟基取代的四氢吡喃，或被羟基取代的低级烷氧基，或被一个或两个羟基取代的低级烷基，或是任选被羟基取代的（CH 2）m - 吡啶基，或被羟基取代的低级烷基或低级烷基，或者是被羟基，被羟基取代的低级烷基或低级烷基取代的L-苯基，L是一个键，-CH （CH 2 OH） - 或-CH 2 CH（OH） - ; n为0,1或2; m为0或1; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应。本发明的化合物是毒蕈碱M1受体阳性变构调节剂（PAM），因此可用于治疗由毒蕈碱M1受体介导的疾病，如阿尔茨海默病，认知障碍，精神分裂症，疼痛或睡眠障碍。

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