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1. 发明授权

US11840528B2 Isoxazolyl ether derivatives as GABA 有权
公开(公告)号：US11840528B2
公开(公告)日：2023-12-12
申请号：US17119977
申请日：2020-12-11
申请人： Hoffmann-La Roche Inc.
发明人： Giuseppe Cecere , Katrin Groebke Zbinden , Maria-Clemencia Hernandez , Henner Knust , Andreas Koblet , Andres Miguel Olivares Morales , Angélique Patiny-Adam , Emmanuel Pinard , Valerie Runtz-Schmitt , Sandra Steiner
IPC分类号： C07D413/14 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D498/04
CPC分类号： C07D413/14 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D498/04
摘要： The invention provides novel compounds having the general formula (I) or (II)

wherein R2, R3, R5, R99, W, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.

2. 发明申请

US20160207885A1 INDOL AND INDAZOL DERIVATIVES 有权
标题翻译： INDOL和INDAZOL衍生物
公开(公告)号：US20160207885A1
公开(公告)日：2016-07-21
申请号：US15082754
申请日：2016-03-28
申请人： Hoffmann-La Roche Inc.
发明人： Theresa M. Ballard , Katrin Groebke Zbinden , Emmanuel Pinard , Thomas Ryckmans , Herve Schaffhauser
IPC分类号： C07D209/42 , C07D405/14 , C07D401/14 , C07D417/14 , C07D401/06 , C07D493/08 , C07D409/12 , C07D405/10 , C07D471/04 , C07D403/10 , C07D413/14
CPC分类号： C07D209/42 , C07D401/06 , C07D401/14 , C07D403/10 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/08
摘要： The present invention relates to compounds of formula wherein A is R is lower alkyl, —(CH2)z-C3-7-cycloalkyl or —(CH2)z—C4-6-heterocycloalkyl, which are optionally substituted by one to three hydroxy, lower alkyl, lower alkoxy or halogen, or is (endo)-7-oxabicyclo[2.2.1]heptan-2-yl; X is CH or N; Y1 is CR3 or N; Y2 is CR4; or or Y1 and Y2 may form together with the carbon atoms to which they are attach Y3 is N; Y4 is N; Y5 is NR7; R1 is hydrogen or halogen; R2 is hydrogen, halogen, cycloalkyl, lower alkyl or lower alkoxy; R3 is hydrogen, halogen, CN, —C(O)NH2, —C(O)NHCH3 or —C(O)N(CH3)2; R4 is hydrogen, a 5 or 6 membered heteroaryl or heterocyclyl group, selected from the group consisting of or is phenyl, —C(O)NH2, —CH2C(O)NH2, —C(O)NHCH3, —C(O)NH-cycloalkyl, —C(O)N(CH3)2, —NHC(O)O-lower alkyl, CN, lower alkoxy, lower alkoxy substituted by halogen, halogen or S(O)2CH3; R5 is phenyl; R6 is phenyl or thiazol-2-yl; R7 is pyridin-2-yl or pyrimidin-4-yl; p is 0 or 1; m is 1, 2 or 3; z is 0 or 1; or a pharmaceutically acceptable acid addition salt, a racemic mixture or 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：本发明涉及下式的化合物其中A是R是低级烷基， - （CH 2）z -C 3 -7-环烷基或 - （CH 2）z -C C 6 - 杂环烷基，其任选被一至三个羟基，低级烷基，低级烷氧基或卤素，或是（内）-7-氧杂二环[2.2.1]庚-2-基; X是CH或N; Y1是CR3或N; Y2是CR4; 或者Y 1和Y 2可以与它们所连接的碳原子一起形成，Y 3是N; Y4是N; Y5为NR7; R1是氢或卤素; R2是氢，卤素，环烷基，低级烷基或低级烷氧基; R3是氢，卤素，CN，-C（O）NH2，-C（O）NHCH3或-C（O）N（CH3）2; R 4是氢，5或6元杂芳基或杂环基，其选自或是苯基，-C（O）NH 2，-CH 2 C（O）NH 2，-C（O）NHCH 3，-C（O） NH - ， - C（O）N（CH 3）2，-NHC（O）O-低级烷基，CN，低级烷氧基，被卤素，卤素或S（O）2 CH 3取代的低级烷氧基; R5是苯基; R6是苯基或噻唑-2-基; R 7是吡啶-2-基或嘧啶-4-基; p为0或1; m为1,2或3; z为0或1; 或药学上可接受的酸加成盐，外消旋混合物或其相应的对映体和/或光学异构体。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

US20160145270A1 COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY 审中-公开
标题翻译：用于治疗脊柱肌瘤的化合物
公开(公告)号：US20160145270A1
公开(公告)日：2016-05-26
申请号：US14899397
申请日：2014-06-23
申请人： HOFFMANN-LA ROCHE INC. , PTC THERAPEUTICS INC.
发明人： Amal Dakka , Luke Green , Gary Karp , Jana Narasimhan , Nikolai Naryshkin , Emmanuel Pinard , Hongyan Qi , Hasane Ratni , Nicole Risher , Marla Weetall , Matthew Woll
IPC分类号： C07D519/00 , C07D263/56 , C07D413/12 , C07D487/04 , C07D471/04
CPC分类号： C07D519/00 , C07D263/56 , C07D413/12 , C07D471/04 , C07D487/04 , C07D487/10
摘要： The present invention provides compounds of formula (I) wherein A, B, X, Y, R1 and R2 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.
摘要翻译：本发明提供其中A，B，X，Y，R 1和R 2如本文所述的式（I）化合物及其药学上可接受的盐。此外，本发明涉及制备式（I）化合物，包含它们的药物组合物及其作为药物的用途。

4. 发明授权

US09067911B2 Piperidine derivatives 有权
标题翻译：哌啶衍生物
公开(公告)号：US09067911B2
公开(公告)日：2015-06-30
申请号：US13766840
申请日：2013-02-14
申请人： Hoffmann-La Roche Inc.
发明人： Sabine Kolczewski , Emmanuel Pinard , Henri Stalder
IPC分类号： C07D211/56 , A61K31/451 , C07D407/04 , C07D401/04 , C07D401/12 , C07D405/04 , C07D417/10 , C07D213/56 , C07D221/20
CPC分类号： C07D407/04 , A61K31/451 , C07D211/56 , C07D213/56 , C07D221/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D417/10
摘要： The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及其中R 1，R 2和Ar如本文所定义或其药学上可接受的酸加成盐的式I化合物与外消旋混合物或其相应的对映异构体和/或其光学异构体。这些化合物及其药物组合物可用于治疗神经和神经精神障碍。

5. 发明授权

US11091471B2 Isoxazolyl ether derivatives as GABAA α5 PAM 有权
公开(公告)号：US11091471B2
公开(公告)日：2021-08-17
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 , A61P25/28 , C07D471/04 , C07D487/10
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. 发明授权

US10640472B2 Phenoxymethyl derivatives 有权
公开(公告)号：US10640472B2
公开(公告)日：2020-05-05
申请号：US15910307
申请日：2018-03-02
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： A61K31/4196 , A61K31/4192 , A61K31/415 , A61K31/416 , A61K31/4162 , A61K31/50 , C07D249/04 , C07D249/08 , C07D231/12 , C07D231/20 , C07D231/00 , C07D231/14 , C07D487/04 , A61P27/02 , C07D249/12 , C07D409/12 , C07D413/12 , C07F7/08 , C07D401/12 , C07D407/12 , C07D407/04 , C07D471/04 , C07D237/14 , C07D403/12 , C07D417/12 , C07D231/56 , C07B41/04 , C07C205/04 , C07C255/50 , C07C317/14
CPC分类号： C07D249/08 , A61P27/02 , C07B41/04 , C07D231/12 , C07D231/20 , C07D231/56 , C07D237/14 , C07D249/04 , C07D249/12 , C07D401/12 , C07D403/12 , C07D407/04 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07F7/0812 , C07C205/04 , C07C255/50 , C07C317/14
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.

7. 发明授权

US10501482B2 Compounds for treating spinal muscular atrophy 有权
公开(公告)号：US10501482B2
公开(公告)日：2019-12-10
申请号：US15948444
申请日：2018-04-09
申请人： Hoffmann-La Roche Inc. , PTC Therapeutics Inc.
发明人： Amal Dakka , Luke Green , Gary Karp , Jana Narasimhan , Nikolai Naryshkin , Emmanuel Pinard , Hongyan Qi , Hasane Ratni , Nicole Risher , Marla Weetall , Matthew Woll
IPC分类号： C07D519/00 , C07D487/10 , C07D263/56 , C07D471/04 , C07D413/12 , C07D487/04
CPC分类号： C07D519/00 , C07D263/56 , C07D413/12 , C07D471/04 , C07D487/04 , C07D487/10
摘要： The present invention provides compounds of formula (I) wherein A, B, X, Y, R1 and R2 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

US20220411415A1 ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM 有权
公开(公告)号：US20220411415A1
公开(公告)日：2022-12-29
申请号：US17378410
申请日：2021-07-16
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 , A61P25/28 , C07D471/04 , C07D487/10
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.

9. 发明申请

US20180222925A1 COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY 审中-公开
公开(公告)号：US20180222925A1
公开(公告)日：2018-08-09
申请号：US15948444
申请日：2018-04-09
申请人： Hoffmann-La Roche Inc. , PTC Therapeutics Inc.
发明人： Amal Dakka , Luke Green , Gary Karp , Jana Narasimhan , Nikolai Naryshkin , Emmanuel Pinard , Hongyan Qi , Hasane Ratni , Nicole Risher , Marla Weetall , Matthew Woll
IPC分类号： C07D519/00 , C07D487/10 , C07D263/56 , C07D471/04 , C07D413/12 , C07D487/04
CPC分类号： C07D519/00 , C07D263/56 , C07D413/12 , C07D471/04 , C07D487/04 , C07D487/10
摘要： The present invention provides compounds of formula (I) wherein A, B, X, Y, R1 and R2 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.

10. 发明授权

US09932335B2 Pyrrolopyridine or pyrazolopyridine derivatives 有权
公开(公告)号：US09932335B2
公开(公告)日：2018-04-03
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, Y1, Y2, X, R and n are as defined herein.

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