公开(公告)号：US11439652B2

公开(公告)日：2022-09-13

申请号：US16937792

申请日：2020-07-24

申请人： SANTEN PHARMACEUTICAL CO., LTD. ,  DAIICHI SANKYO COMPANY, LIMITED

发明人： Yoko Endo ,  Kyohei Takahashi ,  Shinya Umezaki

IPC分类号： A61K31/661 ,  A61K9/08 ,  A61K31/573 ,  A61K31/5383 ,  A61P27/02 ,  A61P31/04 ,  A61K9/00 ,  A61K47/10 ,  A61K47/02 ,  A61P29/00 ,  A61K31/496 ,  A61K31/538 ,  C07J5/00 ,  C07C31/18 ,  C08G65/00

摘要： An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.

公开(公告)号：US11376228B2

公开(公告)日：2022-07-05

申请号：US16986303

申请日：2020-08-06

申请人： Genifarm Laboratories Inc ,  South China University of Technology

发明人： Shifa Zhu ,  Tongxiang Cao ,  Yongdong Wang ,  Zhipeng Huang

IPC分类号： A61K31/05 ,  C07C47/57 ,  C07C45/60 ,  C07D307/42 ,  C07D309/26 ,  C07D333/78 ,  C07J1/00 ,  C07J5/00 ,  A61P35/00 ,  A61K31/34 ,  A61K31/381

摘要： A polysubstituted benzene compound, preparation method thereof, and method of using the same. The compound has a formula I or I′, where X represents carbon, sulfur, or oxygen; R1 represents a C1-16 alkyl, C2-16 alkenyl, or C2-10 alkynyl; R2 represents hydrogen, halogen, C1-16 alkyl, C2-16 alkenyl, or C2-10 alkynyl; or an aryl group or a substituted aryl group by 1-5 groups selected from halogen, C1-26 alkyl, C1-3 halogenated alkyl, O—C1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; or a heteroaryl group or a substituted heteroaryl group by 1-5 groups selected from halogen, C1-26 alkyl, C1-3 halogenated alkyl, O—C1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; the heteroaryl group is a 3-10-membered heteroaryl group including N, S, O, or a combination thereof.

公开(公告)号：US11241446B2

公开(公告)日：2022-02-08

申请号：US16428386

申请日：2019-05-31

申请人： Sage Therapeutics, Inc.

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

IPC分类号： 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

摘要： 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：US20210299145A1

公开(公告)日：2021-09-30

申请号：US17223776

申请日：2021-04-06

申请人： COSMO TECHNOLOGIES LTD.

发明人： Mara GERLONI

IPC分类号： A61K31/573 ,  C07J5/00 ,  A61K9/00 ,  A61K45/06

摘要： The present invention relates to certain cortexolone derivatives of formula (I) and the use of the same as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. The present invention also relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of the pharmaceutical compositions as antitumor medicinal products.

公开(公告)号：US10995112B2

公开(公告)日：2021-05-04

申请号：US16598694

申请日：2019-10-10

申请人： NeurMedix, Inc.

发明人： Steven K. White ,  Igor Ivanisevic ,  Kyle Stephens ,  Mark Andres ,  Brenton Skylar Wolfe

IPC分类号： C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  A61K31/57

摘要： Described herein are solid state 17α-ethynylandrost-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17α-ethynylandrost-5-ene-3β,7β,17β-triol in treating numerous diseases and disorders, including hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions, and neurodegenerative conditions in subjects or human patients.

公开(公告)号：US20210094981A1

公开(公告)日：2021-04-01

申请号：US16924814

申请日：2020-07-09

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

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：US10857161B2

公开(公告)日：2020-12-08

申请号：US16226061

申请日：2018-12-19

申请人： ReveraGen BioPharma, Inc.

发明人： John M. McCall ,  Eric Hoffman ,  Kanneboyina Nagaraju

IPC分类号： A61K31/573 ,  A61K31/57 ,  C07J5/00 ,  A61K31/575

摘要： Provided herein is a pharmaceutical composition comprising a compound having the structural formula wherein the compound is present in an amount effective to treat or reduce the symptoms of muscular dystrophy. The therapeutically effective amount may be between 10 mg to 200 mg, or may be between 0.01 mg/kg to 10.0 mg/kg. Also provided are methods of treating or reducing the symptoms of muscular dystrophy, comprising the administration, to a patient in need thereof, of a therapeutically effective of the above compound.

公开(公告)号：US10780174B2

公开(公告)日：2020-09-22

申请号：US16063666

申请日：2016-12-22

申请人： The University of British Columbia

发明人： Marco A. Ciufolini ,  Pieter R. Cullis ,  Yuen Yi Tam ,  Joshua Zaifman

IPC分类号： A61K31/573 ,  A61K31/337 ,  A61K31/58 ,  A61K31/495 ,  A61K31/519 ,  A61K31/436 ,  A61K47/54 ,  C07J5/00 ,  C07J41/00 ,  C07D475/08 ,  C07J31/00 ,  C07D305/14 ,  C07J43/00 ,  C07D487/04 ,  C07D295/185 ,  A61P29/00 ,  A61P35/00

摘要： This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.

公开(公告)号：US10577390B2

公开(公告)日：2020-03-03

申请号：US15519480

申请日：2015-10-16

申请人： Sage Therapeutics, Inc.

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

IPC分类号： C07J43/00 ,  A61K45/06 ,  C07J9/00 ,  A61K31/575 ,  A61K31/58 ,  C07J1/00 ,  C07J3/00 ,  C07J5/00 ,  C07J7/00 ,  C07J11/00 ,  C07J13/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

摘要： Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein (II), A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b 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. (II)

公开(公告)号：US10391106B2

公开(公告)日：2019-08-27

申请号：US15639702

申请日：2017-06-30

申请人： Sage Therapeutics, Inc.

发明人： Gabriel Martinez Botella ,  Boyd L. Harrison ,  Albert J. Robichaud ,  Francesco G. Salituro ,  Richard T. Beresis

IPC分类号： 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

摘要： 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.