-
公开(公告)号：US20190169226A1
公开(公告)日：2019-06-06
申请号：US16269779
申请日：2019-02-07
Applicant: Sage Therapeutics, Inc.
Inventor： Boyd L. Harrison , Gabriel Martinez Botella , Albert Jean Robichaud , Francesco G. Salituro
CPC classification number: C07J41/005 , C07J1/0011 , C07J5/0015 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J7/009 , C07J13/007 , C07J17/00 , C07J21/00 , C07J21/006 , C07J21/008
Abstract: Described herein are steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
-
公开(公告)号：US20180141971A1
公开(公告)日：2018-05-24
申请号：US15639702
申请日：2017-06-30
Applicant: Sage Therapeutics, Inc.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert J. Robichaud , Francesco G. Salituro , Richard T. Beresis
IPC: C07J43/00 , C07J9/00 , C07J7/00 , C07J17/00 , C07J33/00 , C07J1/00 , C07J13/00 , C07J3/00 , C07J21/00 , C07J41/00
CPC classification number: A61K31/58 , A61K31/573 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J3/00 , C07J3/005 , C07J5/0015 , C07J7/00 , C07J7/002 , C07J7/007 , C07J7/008 , C07J7/0085 , C07J9/00 , C07J13/007 , C07J15/00 , C07J17/00 , C07J21/00 , C07J31/006 , C07J33/002 , C07J41/0066 , C07J43/003
Abstract: Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, and R4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
-
公开(公告)号：US20180051052A1
公开(公告)日：2018-02-22
申请号：US15143312
申请日：2016-04-29
Applicant: SAGE THERAPEUTICS, INC.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
CPC classification number: C07J43/003 , C07J3/00 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J21/00 , C07J31/006
Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (1): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.
-
公开(公告)号：US20170342103A1
公开(公告)日：2017-11-30
申请号：US15681983
申请日：2017-08-21
Applicant: Sage Therapeutics, Inc.
Inventor： Ravindra B. Upasani , Benny C. Askew , Boyd L. Harrison , Francesco G. Salituro , Albert J. Robichaud
CPC classification number: C07J43/003 , C07J5/0015 , C07J7/002 , C07J7/008 , C07J7/0085 , C07J9/005 , C07J31/006
Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III): where R1, R2, R3, R3′, R4, R6a, R6a, R11a, and R11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.
-
5.发明授权19-nor C3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof 有权19-不是C3-三取代C21-N-吡唑基类固醇及其使用方法公开(公告)号：US09512165B2
公开(公告)日：2016-12-06
申请号：US14785171
申请日：2014-04-17
Applicant: SAGE THERAPEUTICS, INC.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
IPC: C07J3/00 , C07J7/00 , C07J15/00 , C07J5/00 , C07J43/00 , A61K9/00 , C07J1/00 , C07J13/00 , C07J21/00 , C07J31/00
CPC classification number: A61K31/58 , A61K9/0019 , A61K31/573 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J3/00 , C07J5/0015 , C07J5/0053 , C07J7/00 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J15/00 , C07J21/00 , C07J31/006 , C07J43/003
Abstract: Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I), and pharmaceutically acceptable salts thereof; wherein, R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
-
Patent Agency Ranking
公开(公告)号：US20160229887A1
公开(公告)日：2016-08-11
申请号：US14913920
申请日：2014-08-22
Applicant: SAGE THERAPEUTICS, INC.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco Gerald Salituro , Robert Jason Herr , Robert Borbo Kargbo
IPC: C07J43/00
CPC classification number: C07J43/003 , A61K31/58 , A61K45/06 , C07J1/0059 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J21/00 , C07J21/008 , A61K2300/00
Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein -------, R1, R2, R5, A and L are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
Abstract translation: 本文描述了式（I）的神经活性类固醇或其药学上可接受的盐; 其中 - ， - ，R1，R2，R5，A和L如本文所定义。 在某些实施方案中，可以想到这样的化合物表现为GABA调节剂。 本发明还提供包含本发明化合物和使用和治疗方法的药物组合物，例如用于诱导镇静和/或麻醉。
-
7.发明申请19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF 有权19-NOR C3，3-取代的C21-N-吡唑啉甾体及其使用方法公开(公告)号：US20160108080A1
公开(公告)日：2016-04-21
申请号：US14785171
申请日：2014-04-17
Applicant: SAGE THERAPEUTICS, INC.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
CPC classification number: A61K31/58 , A61K9/0019 , A61K31/573 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J3/00 , C07J5/0015 , C07J5/0053 , C07J7/00 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J15/00 , C07J21/00 , C07J31/006 , C07J43/003
Abstract: Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I), and pharmaceutically acceptable salts thereof; wherein-, R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful NI for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
Abstract translation: 本文提供了式（I）的19-不是C3,3-二取代的C21-吡唑基类固醇及其药学上可接受的盐; 其中 - ，R1，R2，R3a，R3b，R4a，R4b，R5，R6和R7如本文所定义。 预期这样的化合物可用于预防和治疗各种CNS相关病症，例如睡眠障碍，情绪障碍，精神分裂症谱系障碍，惊厥性障碍，记忆障碍和/或认知障碍，运动障碍，个性 疾病，自闭症谱系障碍，疼痛，创伤性脑损伤，血管疾病，药物滥用障碍和/或戒断综合征以及耳鸣。
-
8.发明申请19-NOR C3, 3-DISUBSTITUTED C21-C-BOUND HETEROARYL STEROIDS AND METHODS OF USE THEREOF 有权19-NOR C3，3-取代的C21-C-结合的异源甾体及其使用方法公开(公告)号：US20160083417A1
公开(公告)日：2016-03-24
申请号：US14785175
申请日：2014-04-17
Applicant: SAGE THERAPEUTICS, INC.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
CPC classification number: A61K31/58 , A61K31/573 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J3/00 , C07J3/005 , C07J5/0015 , C07J7/00 , C07J7/002 , C07J7/007 , C07J7/008 , C07J7/0085 , C07J9/00 , C07J13/007 , C07J15/00 , C07J17/00 , C07J21/00 , C07J31/006 , C07J33/002 , C07J41/0066 , C07J43/003
Abstract: Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein, , R1, R2, R3a, R3b, R4a, and R4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
Abstract translation: 本文提供了式（I）的19-或不含C3,3-二取代的类固醇：及其药学上可接受的盐; 其中，R1，R2，R3a，R3b，R4a和R4b如本文所定义，A是如本文定义的碳键取代或未取代的5-至6-元杂芳基环。 预期这样的化合物可用于预防和治疗各种CNS相关病症，例如睡眠障碍，情绪障碍，精神分裂症谱系障碍，惊厥性疾病，记忆障碍和/或认知障碍，运动障碍，人格障碍 ，自闭症谱系障碍，疼痛，创伤性脑损伤，血管疾病，药物滥用障碍和/或戒断综合征以及耳鸣。
-
9.发明授权17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-acyloxyalkylene phenyl derivatives, methods for the production thereof and use thereof for treating diseases 有权17-羟基-17-五氟乙基 - 雌-4,4（10） - 二烯-11-酰氧基亚烷基苯基衍生物，其制备方法和用于治疗疾病的用途公开(公告)号：US09096639B2
公开(公告)日：2015-08-04
申请号：US13384332
申请日：2010-07-07
Applicant: Ulrich Klar , Wolfgang Schwede , Carsten Moller , Andrea Rotgeri , Ursula Krenz
Inventor： Ulrich Klar , Wolfgang Schwede , Carsten Moller , Andrea Rotgeri , Ursula Krenz
CPC classification number: C07J1/0081 , A61K31/573 , A61K31/58 , C07J7/0085 , C07J41/0044 , C07J41/0083 , C07J43/003
Abstract: The invention relates to 17-hydroxy-13-methyl-17-pentafluoroethyl-11-acyloxyalkylenephenyldodecahydrocyclopenta[a]phenanthren-3-one derivatives of the formula I with progesterone-antagonizing action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.
Abstract translation: 本发明涉及式I的17-羟基-13-甲基-17-五氟乙基-11-酰氧基亚烷基十一烷基十氢环戊并[a]菲-3-酮衍生物与孕酮拮抗作用及其制备方法，用于治疗和 （或肌瘤，子宫平滑肌瘤），子宫内膜异位症，重度月经出血，脑膜瘤，荷尔蒙依赖性乳腺癌等的病症的治疗和/或预防用药物，以及 与绝经相关的投诉，或生育控制和紧急避孕。
-
10.发明申请公开(公告)号：US20100113408A1
公开(公告)日：2010-05-06
申请号：US12641172
申请日：2009-12-17
Applicant: Hyun K. Kim , Richard P. Blye , Pemmaraju N. Rao , James W. Cessac , Carmie K. Acosta
Inventor： Hyun K. Kim , Richard P. Blye , Pemmaraju N. Rao , James W. Cessac , Carmie K. Acosta
CPC classification number: C07J5/00 , C07J5/0053 , C07J7/00 , C07J7/0085 , C07J9/00 , C07J21/006 , C07J41/00 , C07J41/0016 , C07J41/0083 , C07J41/0094 , C07J51/00 , C07J71/001 , Y10S514/841
Abstract: A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce labor; and for contraception.
Abstract translation: 具有以下通式的化合物：其中：R 1是选自-OCH 3，-SCH 3，-N（CH 3）2，-NHCH 3，-CHO，-COCH 3和-CHOHCH 3的成员; R2是选自卤素，烷基，酰基，羟基，烷氧基，酰氧基，碳酸烷基酯，环戊氧基，S-烷基和S-酰基的成员; R3是选自烷基，羟基，烷氧基和酰氧基的成员; R4是选自氢和烷基的成员; 并且X是选自由以下组成的组的成员：= O和= NO-OR 5，其中R 5是选自氢和烷基的成员。 除了提供式I化合物之外，本发明提供了其中式I化合物有利地用于拮抗内源性孕酮的方法; 诱发月经; 治疗子宫内膜异位症; 治疗痛经; 治疗内分泌激素依赖性肿瘤; 治疗子宫肌瘤; 抑制子宫内膜增生; 诱导劳动; 和避孕。
-
-
-
-
-
-
-
-
-
Search Results
146
records
(took 0.045 seconds)
