公开(公告)号：US11241446B2

公开(公告)日：2022-02-08

申请号：US16428386

申请日：2019-05-31

Applicant: Sage Therapeutics, Inc.

Inventor： Gabriel Martinez Botella ,  Boyd L. Harrison ,  Albert Jean Robichaud ,  Francesco G. Salituro ,  Richard Thomas Beresis

IPC: A61K31/58 ,  A61K31/473 ,  C07J3/00 ,  C07J7/00 ,  C07J15/00 ,  C07J43/00 ,  A61K9/00 ,  C07J5/00 ,  A61K31/573 ,  C07J1/00 ,  C07J13/00 ,  C07J21/00 ,  C07J31/00

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.

公开(公告)号：US10391106B2

公开(公告)日：2019-08-27

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: C07J3/00 ,  C07J7/00 ,  C07J9/00 ,  C07J15/00 ,  C07J17/00 ,  C07J33/00 ,  C07J43/00 ,  A61K31/573 ,  A61K31/58 ,  C07J1/00 ,  C07J5/00 ,  C07J13/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00

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：US10202413B2

公开(公告)日：2019-02-12

申请号：US14767235

申请日：2014-02-14

Applicant: Washington University

Inventor： Douglas Covey

IPC: A61K31/56 ,  A61K31/566 ,  A61K31/568 ,  A61K31/5685 ,  C07J1/00 ,  C07J21/00 ,  C07J15/00 ,  C07J41/00 ,  C07C35/42 ,  C07J13/00 ,  C07J31/00 ,  C07J51/00 ,  C07J61/00 ,  C07J63/00 ,  C07J71/00 ,  C07J75/00 ,  C07C43/307

Abstract: 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：US09855281B2

公开(公告)日：2018-01-02

申请号：US15037399

申请日：2014-11-20

Applicant: Scott Freeman Consultant, LLC

Inventor： Scott Freeman

IPC: A61K31/56 ,  A61K31/565 ,  A61K9/00 ,  C07J11/00 ,  A61K45/06 ,  C07J1/00 ,  C07J15/00

CPC classification number: A61K31/565 ,  A61K9/0019 ,  A61K9/0053 ,  A61K45/06 ,  C07J1/007 ,  C07J15/00 ,  A61K2300/00

Abstract: A composition for enhancing libido of a pharmaceutically effective amount of a libido-enhancing therapeutic of (5S,10R,13S,17S)-13-methyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17yl acetate (Formula I), (3S,5S,10R,13S,17S)-3-hydroxy-13-methylhexadecahydro-1H-cyclopenta[a]phenanthren-17yl acetate (Formula II), (5S,10S,13S,17S)-17-hydroxy-13-methyltetradecahydro-1H-cyclopenta[a]phenanthren-3(2H)-one (Formula III), isomers thereof, analogs thereof, or combinations thereof, and a pharmaceutically acceptable carrier. A method of enhancing libido, by administering the composition to an individual in need of an enhanced libido, and enhancing libido in the individual or animal which is male or female. A method of enhancing libido, by administering the composition of the present invention to an individual at an age when libido and sexual desire have naturally decreased, and enhancing libido in the individual. A composition for enhancing libido and arousal, including a pharmaceutically effective amount of a libido-enhancing therapeutic in combination with a sexual dysfunction therapeutic. A method of enhancing libido and arousal.

公开(公告)号：US20160340383A1

公开(公告)日：2016-11-24

申请号：US15227936

申请日：2016-08-03

Applicant: Zhengyuantang (Tianjin Binhai New Area) Biotech Co., Ltd.

Inventor： Yaozhou ZHANG ,  Jiachen SUN ,  Lei JIANG ,  Jian ZHANG ,  Yujiao CHEN ,  Xiaoqian ZHANG ,  Simiao DU ,  Pengai GU ,  Jinsong CUI

IPC: C07J15/00

CPC classification number: C07J15/005 ,  C07B2200/13

Abstract: (3α,9β,10α,13α,14β,17α,20S,22E)-Ergosta-5,7,22-trien-3-ol. A method for preparing the same by drying a fruiting body of Cordyceps militaris, grinding the fruiting body to yield ultrafine powders; boiling and extracting the ultrafine powders, centrifuging and collecting a precipitate. A method for treating a tumor by administering to a patient in need of treating a tumor (3α,9β,10α,13α,14β,17α,20S,22E)-ergosta-5,7,22-trien-3-ol.

Abstract translation: （3α，9β，10α，13α，14β，17α，20S，22E）-Ergosta-5,7,2-三烯-3-醇。 通过干燥冬虫夏草的子实体制备该方法，研磨子实体以产生超细粉末; 煮沸并提取超细粉末，离心收集沉淀物。 通过对需要治疗肿瘤的患者（3α，9β，10α，13α，14β，17α，20S，22E） - 麦角甾-5,7,2-三烯-3-醇进行治疗来治疗肿瘤的方法。

公开(公告)号：US5304291A

公开(公告)日：1994-04-19

申请号：US21902

申请日：1993-02-24

Applicant: Berthus Bout ,  Ronald Voorhaar

Inventor： Berthus Bout ,  Ronald Voorhaar

IPC: C07J1/00 ,  C07C401/00 ,  C07J15/00 ,  C07J75/00 ,  C07G13/00

CPC classification number: C07J15/005 ,  C07C401/00

Abstract: The invention relates to a method of preparing a 9beta,10alpha-5,7-diene steroid by irradiating the corresponding 9alpha,10beta-5,7-diene steroid with filtered ultraviolet light from an indium lamp.

Abstract translation: 本发明涉及通过用铟灯过滤的紫外光照射相应的9α，10beta-5,7-二烯类固醇来制备9beta，10α-5,7-二烯类固醇的方法。

公开(公告)号：US4044004A

公开(公告)日：1977-08-23

申请号：US695610

申请日：1976-06-14

Applicant: Gabriel Saucy ,  John William Scott

Inventor： Gabriel Saucy ,  John William Scott

IPC: A61K31/5685 ,  C07D261/08 ,  C07D261/18 ,  C07D295/145 ,  C07D317/72 ,  C07F9/653 ,  C07J1/00 ,  C07J15/00 ,  C07J43/00

CPC classification number: C07D317/72 ,  A61K31/5685 ,  C07D261/08 ,  C07D261/18 ,  C07D295/145 ,  C07F9/653 ,  C07J1/00 ,  C07J1/0059 ,  C07J15/00 ,  C07J15/005 ,  C07C2103/16

Abstract: The novel intermediates and processes of this invention provide a new synthetic route for the preparation of pharmaceutically valuable 19-norsteroids. Further, the intermediates and processes of the invention provide a novel route for the preparation of pharmaceutically valuable estrones. The present invention provides a facile total synthesis of 19.beta.-alkyl-C/D-trans-steroidal materials. This desirable result is obtained via a unique asymmetric induction followed by subsequent stereospecific reaction steps. As a precursor to the steroidal Ring A, a 3,5-disubstituted-4-isoxazolylmethylene group is employed in this synthesis.

Abstract translation: 本发明的新颖中间体和方法为制备药学上有价值的19-降胆甾醇提供了新的合成途径。 此外，本发明的中间体和方法提供了用于制备药学上有价值的酮的新途径。 本发明提供了19个β-烷基-C / D-反式甾体材料的简便总合成。 通过独特的不对称诱导，然后随后的立体特异性反应步骤获得该期望的结果。 作为甾体环A的前体，在该合成中使用3,5-二取代-4-异恶唑基亚甲基。

公开(公告)号：US3951958A

公开(公告)日：1976-04-20

申请号：US487988

申请日：1974-07-12

Applicant: Klaus Prezewowsky ,  Henry Laurent ,  Helmut Hofmeister ,  Rudolf Wiechert ,  Friedmund Neumann ,  Yukishige Nishino

Inventor： Klaus Prezewowsky ,  Henry Laurent ,  Helmut Hofmeister ,  Rudolf Wiechert ,  Friedmund Neumann ,  Yukishige Nishino

IPC: C07J1/00 ,  C07J15/00 ,  C07J17/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00 ,  C07J75/00

CPC classification number: C07J41/0072 ,  C07J1/0059 ,  C07J15/00 ,  C07J17/00 ,  C07J43/003 ,  C07J71/001 ,  C07J71/0031

Abstract: 1,3-Dihydroxy-8.alpha.-estratrienes of the formula ##SPC1##Wherein R is lower-alkyl and --A--B is ##SPC2##Wherein R' is a saturated or unsaturated hydrocarbon group and R" is lower-alkyl, aralkyl or phenyl, and the esters and ethers thereof, possess strong vaginotropic but only weak utertropic activity and are useful in the treatment of estrogenic deficiency conditions where uteral effects are not desired.

Abstract translation: 式WHEREIN R是低级烷基的1,3-二羟基-8α-三亚甲基，-AB是WHEREIN R'是饱和或不饱和烃基，R“是低级烷基，芳烷基或苯基，酯和 其醚类具有强烈的阴性，但仅具有弱的致命性活性，并且可用于治疗不期望产生效果的雌激素缺乏症状。

公开(公告)号：US3700703A

公开(公告)日：1972-10-24

申请号：US3700703D

申请日：1970-07-02

Applicant: PHILIPS CORP

Inventor： MOORSELAAR RUDOLF VAN

IPC: C07C20060101 ,  C07J1/00 ,  C07J15/00 ,  C07C169/20

CPC classification number: C07J53/00

Abstract: New 18-methyl-9 Beta ,10 Alpha -steroids of the androstane series, methods of producing the same, pharmaceutical preparations containing said compounds as active ingredients and methods of producing the said preparations.

Abstract translation: 雄甾烷系列的新的18-甲基-9β，10个α-类固醇，其制备方法，含有所述化合物作为活性成分的药物制剂和制备所述制剂的方法。

公开(公告)号：US3700661A

公开(公告)日：1972-10-24

申请号：US3700661D

申请日：1968-11-22

Applicant: HOFFMANN LA ROCHE

Inventor： SAUCY GABRIEL ,  SCOTT JOHN WILLIAM

IPC: C07J75/00 ,  C07D261/08 ,  C07D261/18 ,  C07D295/145 ,  C07D317/72 ,  C07F9/54 ,  C07F9/653 ,  C07J1/00 ,  C07J15/00 ,  C07D85/22

CPC classification number: C07D317/72 ,  C07C2603/16 ,  C07D261/08 ,  C07D261/18 ,  C07D295/145 ,  C07F9/54 ,  C07F9/653 ,  C07J1/0059 ,  C07J15/005 ,  Y02P20/55

Abstract: THE NOVEL INTERMEDIATES AND PROCESSES OF THIS INVENTION PROVIDE A NEW SYNTHETIC ROUTE FOR THE PREPARATION OF PHARMACEUTICALLY VALUABLE 19-NOR-STEROIDS. FURTHER, THE INTERMEDIATES AND PROCESSES OF THE INVENTION PROVIDE A NOVEL ROUTE FOR THE PREPARATION OF PHARMACEUTICALLY VALUABLE ESTRONES. THE PRESENT INVENTION PROVIDES A FACILE TOTAL SYNTHESIS OF 13B-ALKYL-C/D-TRANS-STEROIDAL MATERIALS. THIS DESIRABLE RESULT IS OBTAINED VIA A UNIQUE ASYMMETRIC INDUCTION FOLLOWED BY SUBSEQUENT STEREO-SPECIFIC REACTION STEPS. AS A PRECURSOR TO THE STEROIDAL RING A, A 3,5-DISUBSTITUTED4-ISOXAZOLYLMETHYLENE GROUP IS EMPLOYED IN THIS SYNTHESIS.