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公开(公告)号:US11439652B2
公开(公告)日:2022-09-13
申请号:US16937792
申请日:2020-07-24
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.
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公开(公告)号:US11376228B2
公开(公告)日:2022-07-05
申请号:US16986303
申请日:2020-08-06
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.
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公开(公告)号:US11241446B2
公开(公告)日:2022-02-08
申请号:US16428386
申请日:2019-05-31
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.
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公开(公告)号:US20210299145A1
公开(公告)日:2021-09-30
申请号:US17223776
申请日:2021-04-06
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.
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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.
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.
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公开(公告)号:US20210094981A1
公开(公告)日:2021-04-01
申请号:US16924814
申请日:2020-07-09
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.
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公开(公告)号:US10857161B2
公开(公告)日:2020-12-08
申请号:US16226061
申请日:2018-12-19
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.
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公开(公告)号:US10780174B2
公开(公告)日:2020-09-22
申请号:US16063666
申请日:2016-12-22
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.
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公开(公告)号:US10577390B2
公开(公告)日:2020-03-03
申请号:US15519480
申请日:2015-10-16
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)
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公开(公告)号:US10391106B2
公开(公告)日:2019-08-27
申请号:US15639702
申请日:2017-06-30
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.
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