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公开(公告)号：US12077559B2
公开(公告)日：2024-09-03
申请号：US17282772
申请日：2019-10-21
Applicant: INDUSTRIALE CHIMICA S.R.L
Inventor： Claudio Delfrate , Davide Rigamonti , Tea Borelli , Roberto Lenna
CPC classification number: C07J7/002 , C07J17/00 , C07J33/002
Abstract: The present invention relates to a new process for the synthesis of 3α-hydroxy-5α-pregnan-20-one, commonly known as brexanolone, wherein the corresponding cyclic 20-ketal or cyclic 20-thioketal compound of formula (IV) is deprotected with the use or iodine in an organic solvent: (I).
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公开(公告)号：US11945836B2
公开(公告)日：2024-04-02
申请号：US17959592
申请日：2022-10-04
Applicant: Sage Therapeutics, Inc.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
IPC: A61K31/56 , A61K45/06 , C07J3/00 , C07J9/00 , C07J17/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00
CPC classification number: C07J41/0055 , A61K31/56 , A61K45/06 , C07J3/00 , C07J9/00 , C07J17/00 , C07J31/006 , C07J33/002 , C07J43/00 , C07J43/003 , C07J31/00
Abstract: Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6 and 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.
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公开(公告)号：US20230279043A1
公开(公告)日：2023-09-07
申请号：US17959592
申请日：2022-10-04
Applicant: Sage Therapeutics, Inc.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
IPC: C07J41/00 , C07J9/00 , C07J33/00 , C07J43/00 , C07J3/00 , C07J17/00 , C07J31/00 , A61K45/06 , A61K31/56
CPC classification number: C07J41/0055 , C07J9/00 , C07J33/002 , C07J43/003 , C07J3/00 , C07J17/00 , C07J43/00 , C07J31/006 , A61K45/06 , A61K31/56 , C07J31/00
Abstract: Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6 and 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.
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公开(公告)号：US20220289902A1
公开(公告)日：2022-09-15
申请号：US17637108
申请日：2020-08-28
Applicant: David C. Martin , Samadhan Suresh Nagane , Peter Sitarik
Inventor： David C. Martin , Samadhan Suresh Nagane , Peter Sitarik
IPC: C08G61/12 , C07D495/04 , C07D519/00 , C07J33/00 , H01B1/12
Abstract: Disclosed herein are functionalized 3,4-alkylenedioxythiophene (ADOT+) monomers represented by a chemical formula (CR1R2)(CR3R4)(CR4R6)xO2H2S, wherein x=0 or 1; wherein each of R1, R2, R3, R4, R5, and R6 is independently selected from hydrogen, a hydrocarbyl moiety, and a heteroatom-containing functional group; and wherein at least one of R1, R2, R3, R4, R5, and R6 comprises the heteroatom-containing functional group selected from an aldehyde, a maleimide, and their derivatives thereof. Also, disclosed herein are aldehyde derivatives represented by (ADOT-CH2—NH)pY and a maleimide derivative represented by (ADOT-(CH2)q—N)pZ where p=1-2 and each of Y and Z is a hydrocarbyl moiety or a biofunctional hydrocarbyl moiety. In an embodiment of the ADOT+ monomers, one of R1, R2, R3, R4, R5, and R6 is replaced by a direct bond to an amide group, an azide group, or an ester group of a biofunctional hydrocarbyl moiety. Also, disclosed herein are polymers and copolymers made therefrom.
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公开(公告)号：US11044931B2
公开(公告)日：2021-06-29
申请号：US16524437
申请日：2019-07-29
Applicant: BASF SE
Inventor： Thomas Subkowski , Claus Bollschweiler , Jens Wittenberg , Wolfgang Siegel , Ralf Pelzer
IPC: A23L27/20 , A61Q19/00 , A61K8/49 , C07J63/00 , C07C49/675 , A61K8/35 , A61K8/55 , C07D339/08 , C07D339/06 , C07D495/10 , C07D493/10 , C07D311/94 , C07D311/78 , C07D405/06 , C07D209/48 , C07D471/04 , C07D495/20 , C07D491/20 , C07F9/572 , A23L27/00 , C07J73/00 , C07J33/00 , C07C49/665 , C07J11/00
Abstract: The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.
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Patent Agency Ranking
公开(公告)号：US20210040140A1
公开(公告)日：2021-02-11
申请号：US17069691
申请日：2020-10-13
Inventor： Haiying HE , Hualing XIAO , Peng LI , Chunyan DU , Zhi LUO , Shuhui CHEN
Abstract: The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases.
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公开(公告)号：US10774108B2
公开(公告)日：2020-09-15
申请号：US15531313
申请日：2015-11-27
Applicant: Sage Therapeutics, Inc.
Inventor： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
IPC: C07J41/00 , C07J9/00 , C07J33/00 , C07J43/00 , C07J3/00 , C07J17/00 , C07J31/00 , A61K45/06 , A61K31/56
Abstract: Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6 and 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.
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公开(公告)号：US10093694B2
公开(公告)日：2018-10-09
申请号：US15423359
申请日：2017-02-02
Applicant: Guangzhou KangRui Biological Pharmaceutical Technology Co, Ltd. , The Regents of the University of California
Inventor： Rui Hou , Kang Zhang , Gen Li
Abstract: Described herein are compounds that inhibit or prevent protein aggregation, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with protein aggregation.
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公开(公告)号：US6117994A
公开(公告)日：2000-09-12
申请号：US64576
申请日：1998-04-22
Applicant: Catherine Geurts , Michel Vivat
Inventor： Catherine Geurts , Michel Vivat
CPC classification number: C07J13/005 , C07J21/006 , C07J41/0094 , C07J7/0055 , C07J71/001 , Y02P20/55
Abstract: A new process for the preparation of 16.beta.-methyl-steroids of the formula ##STR1## and novel intermediates.
Abstract translation: 一种制备16型β-甲基类固醇的新方法和新型中间体。
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公开(公告)号：US6015806A
公开(公告)日：2000-01-18
申请号：US478973
申请日：1995-06-07
Applicant: Fernand Labrie , Yves Merand , Shankar M. Singh
Inventor： Fernand Labrie , Yves Merand , Shankar M. Singh
IPC: A61K31/56 , A61K31/565 , A61K31/575 , A61K31/58 , C07J20060101 , C07J1/00 , C07J9/00 , C07J17/00 , C07J21/00 , C07J33/00 , C07J43/00 , C07J73/00
CPC classification number: A61K31/569 , A61K31/575
Abstract: Androgen nucleus derivatives having specified substituents at the 17.alpha. position are disclosed for use as antiandrogens for the treatment of androgen-dependent diseases. In some preferred embodiments, the compound ##STR1## is formulated together with pharmaceutically acceptable diluent or carrier for topical use in the treatment of androgen-dependent diseases associated with the skin.
Abstract translation: 公开了在17α位具有特定取代基的雄激素核衍生物用作治疗雄激素依赖性疾病的抗雄激素。 在一些优选的实施方案中，将化合物与药学上可接受的稀释剂或载体一起配制以用于局部用于治疗与皮肤相关的雄激素依赖性疾病。
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