公开(公告)号：US11780875B2

公开(公告)日：2023-10-10

申请号：US17472744

申请日：2021-09-13

申请人： Sage Therapeutics, Inc.

发明人： Boyd L. Harrison ,  Gabriel Martinez Botella ,  Albert Jean Robichaud ,  Francesco G. Salituro

IPC分类号： C07J41/00 ,  C07J5/00 ,  C07J7/00 ,  C07J17/00 ,  C07J1/00 ,  C07J13/00 ,  C07J21/00

CPC分类号： C07J41/005 ,  C07J5/0015 ,  C07J7/002 ,  C07J7/009 ,  C07J17/00 ,  C07J1/0011 ,  C07J7/007 ,  C07J7/0085 ,  C07J13/007 ,  C07J21/00 ,  C07J21/006 ,  C07J21/008

摘要： 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：US20180111960A1

公开(公告)日：2018-04-26

申请号：US15566097

申请日：2016-02-26

申请人： NORATECH PHARMACEUTICALS, INC.

发明人： Cheng-Gang LIN ,  Li GUI ,  Pan CHEN ,  Zhi-Xuan WANG ,  Tong-Wei GUAN ,  Yuan-Yuan YIN ,  Yu-Ling LU

IPC分类号： C07J9/00 ,  C07J21/00 ,  C07J1/00 ,  C07J13/00

CPC分类号： C07J9/005 ,  C07J1/0011 ,  C07J13/007 ,  C07J21/008

摘要： The present invention discloses method for preparing deoxycholic acid (DCA) or an ester thereof or a pharmaceutically acceptable salt thereof. Said compounds may be applied to remove a fat deposition.

公开(公告)号：US20170190732A1

公开(公告)日：2017-07-06

申请号：US15459492

申请日：2017-03-15

申请人： Washington University ,  Sage Therapeutics, Inc.

发明人： Douglas Covey ,  Albert Jean Robichaud

IPC分类号： C07J41/00 ,  C07J13/00 ,  C07J9/00 ,  C07J1/00 ,  C07J21/00

CPC分类号： A61K31/58 ,  A61K31/56 ,  A61K31/565 ,  A61K31/566 ,  A61K31/573 ,  C07J1/0011 ,  C07J1/0018 ,  C07J1/0029 ,  C07J5/0015 ,  C07J7/002 ,  C07J9/005 ,  C07J13/007 ,  C07J21/00 ,  C07J21/006 ,  C07J21/008 ,  C07J41/0005 ,  C07J41/0016 ,  C07J41/0094 ,  C07J51/00

摘要： The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

公开(公告)号：US09611270B2

公开(公告)日：2017-04-04

申请号：US14815686

申请日：2015-07-31

申请人： University of Kansas

发明人： Jeffrey Aube ,  Emily E. Scott ,  Charlie Fehl

IPC分类号： C07D487/04 ,  C07J73/00 ,  C07J71/00 ,  C07J43/00 ,  C07D401/04 ,  C07J31/00 ,  C07J21/00

CPC分类号： C07D487/04 ,  C07D401/04 ,  C07J21/008 ,  C07J31/006 ,  C07J43/003 ,  C07J71/001 ,  C07J73/005

摘要： Compounds according to formula I or II are provided. Such compounds are useful in treating cancers, such as leukemia, colon cancer, breast cancer, or prostate cancer by beneficially inhibiting CYP17A1. Pharmaceutical compositions and methods including the compounds are also provided.

公开(公告)号：US20160251391A9

公开(公告)日：2016-09-01

申请号：US14767235

申请日：2014-02-14

申请人： WASHINGTON UNIVERSITY

发明人： Douglas Covey

IPC分类号： C07J1/00

CPC分类号： C07J1/00 ,  C07C35/42 ,  C07C43/307 ,  C07C2603/26 ,  C07C2603/40 ,  C07J13/002 ,  C07J15/005 ,  C07J21/00 ,  C07J21/008 ,  C07J31/006 ,  C07J41/0094 ,  C07J51/00 ,  C07J61/00 ,  C07J63/008 ,  C07J71/001 ,  C07J75/005

摘要： The present disclosure is generally directed to neuroactive enantiomeric 15-, 16- and 17-substituted steroids with additional optional substituents at carbons 3, 4, 6, 7, 10 and 13, and pharmaceutically acceptable salts thereof, for use as, for example, modulators for GABA type-A receptors. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

公开(公告)号：US20150259376A1

公开(公告)日：2015-09-17

申请号：US14434057

申请日：2013-10-04

申请人： Washington University

发明人： Douglas F. Covey

IPC分类号： C07J41/00

CPC分类号： C07J41/0094 ,  C07J1/0011 ,  C07J21/008

摘要： The present disclosure is generally directed to neuroactive 19-alkoxy-17(20)-Z-vinylcyano-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

摘要翻译： 本公开一般涉及本文所述的神经活性的19-烷氧基-17（20）-Z-乙烯基氰取代的类固醇及其药学上可接受的盐，用作例如麻醉剂和/或用于治疗 与GABA功能和活动有关的疾病。 本公开进一步涉及包含这些化合物的药物组合物。

公开(公告)号：US20140088053A1

公开(公告)日：2014-03-27

申请号：US14007577

申请日：2012-03-26

申请人： Donald Poirier ,  René Maltais ,  Jenny Roy

发明人： Donald Poirier ,  René Maltais ,  Jenny Roy

IPC分类号： C07J41/00 ,  C07J43/00 ,  C07J1/00 ,  A61K31/5685 ,  A61K31/58 ,  A61K45/06 ,  A61K31/567

CPC分类号： C07J41/0005 ,  A61K31/566 ,  A61K31/567 ,  A61K31/5685 ,  A61K31/58 ,  A61K31/675 ,  A61K31/69 ,  A61K45/06 ,  A61K51/04 ,  C07J1/0007 ,  C07J1/0062 ,  C07J21/00 ,  C07J21/008 ,  C07J31/006 ,  C07J41/0011 ,  C07J41/0038 ,  C07J41/0072 ,  C07J43/003 ,  C07J43/006 ,  C07J51/00 ,  C12Y101/01051

摘要： The present application discloses 17β hydroxy steroid dehydrogenase (17β HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17β HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17β HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17β HSD1 and 17β HSD3 that have a spiro-morpholine substituent at C20.

摘要翻译： 本申请公开了17＆bgr; 羟基类固醇脱氢酶（17＆bgr; HSD）1型，3,10型抑制剂及其用途（单独和组合）用于治疗癌症和其他疾病。 17＆bgr HSD1抑制剂包括在C 16上具有非 - 氨基甲酰基苄基取代基的雌二醇衍生物。 HSD3 / HSD10抑制剂包括在C3位被磺酰胺哌嗪取代的雄酮衍生物。 还公开了作为17＆amp; Bgr的抑制剂的化合物。 HSD1和17＆bgr; HSD3在C20具有螺吗啉取代基。

公开(公告)号：US20130303500A1

公开(公告)日：2013-11-14

申请号：US13813398

申请日：2011-07-29

申请人： Konstantinos Alevizopoulos ,  Theodora Calogeropoulou

发明人： Konstantinos Alevizopoulos ,  Theodora Calogeropoulou

IPC分类号： C07J43/00

CPC分类号： C07J43/003 ,  C07J1/0011 ,  C07J21/006 ,  C07J21/008 ,  C07J41/0016 ,  C07J51/00 ,  C07J71/0005

摘要： The invention features compounds, pharmaceutical compositions and methods useful for the treatment of neoplasia. In particular embodiments, the compounds of the invention are useful for the treatment of multidrug resistant neoplasia.

摘要翻译： 本发明的特征在于可用于治疗瘤形成的化合物，药物组合物和方法。 在具体实施方案中，本发明的化合物可用于治疗多药耐药性肿瘤。

公开(公告)号：US08088758B2

公开(公告)日：2012-01-03

申请号：US10983887

申请日：2004-11-09

申请人： Josef Messinger ,  Heinrich-Hubert Thole ,  Bettina Husen ,  Bartholomeus Johannes Van Steen ,  Gyula Schneider ,  Johannes Bernardus Everardus Hulshof ,  Pasi Koskimies ,  Nina Johansson ,  Jerzy Adamski

发明人： Josef Messinger ,  Heinrich-Hubert Thole ,  Bettina Husen ,  Bartholomeus Johannes Van Steen ,  Gyula Schneider ,  Johannes Bernardus Everardus Hulshof ,  Pasi Koskimies ,  Nina Johansson ,  Jerzy Adamski

IPC分类号： A61K31/58 ,  C07J1/00 ,  C07J43/00

CPC分类号： C07J1/0059 ,  C07J21/008 ,  C07J41/0044 ,  C07J43/003

摘要： 3,15-substituted estrone compounds which act as inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration, as well as the general use of selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.

摘要翻译： 3,15-取代的雌酮化合物，其作为17β-羟基类固醇脱氢酶I（17＆amp; -HSD1）的抑制剂，其盐，含有这些化合物的药物制剂，制备这些化合物的方法，以及这些化合物的治疗用途，特别是 类固醇激素依赖性疾病或病症的治疗或抑制，例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶I型酶和/或需要降低内源性17β-雌二醇浓度的病症，以及 一般使用选择性17＆bgr-羟基类固醇脱氢酶1型抑制剂，其除了具有雌激素受体以外还没有纯化的拮抗性结合亲和力，用于治疗或抑制良性妇科疾病，特别是子宫内膜异位症。

公开(公告)号：US07842680B2

公开(公告)日：2010-11-30

申请号：US12406033

申请日：2009-03-17

申请人： Henry A. Lardy ,  Padma Marwah ,  Ashok Marwah

发明人： Henry A. Lardy ,  Padma Marwah ,  Ashok Marwah

IPC分类号： A61K31/56 ,  A61K31/58 ,  C07J5/00 ,  C07J7/00 ,  C07J21/00

CPC分类号： C07J1/00 ,  C07J1/0011 ,  C07J21/00 ,  C07J21/008

摘要： The instant invention provides potent antiandrogen compounds, such as 3β-acetoxyandrost-1,5-diene-17-ethylene ketal and 3β-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

摘要翻译： 本发明提供了有效的抗雄激素化合物，例如3'-乙酰氧基雄甾-1,5-二烯-17-亚乙基缩酮和3'-羟基雄-1,5-二烯-17-亚乙基缩酮，以及它们用于预防的方法 和治疗由雄激素受体介导的生物学条件。 因此，例如，本发明的化合物可用于预防和治疗前列腺癌。 此外，已经发现本发明的化合物可用于预防和治疗雄激素依赖性癌症如雄激素依赖性前列腺癌。 最后，本发明化合物可用于治疗抗雄激素诱导的戒断综合征。