5696-51-5Relevant academic research and scientific papers
NEUROACTIVE STEROIDS AND COMPOSITIONS AND METHODS THEREOF
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Paragraph 00209, (2021/06/11)
The invention provides novel neuroactive steroids and pharmaceutical compositions thereof, as well as methods of their preparation and use, in therapy of various diseases and conditions, for example, various neurological or brain diseases.
TETRAZOLONE SUBSTITUTED STEROIDS AND USE THEREOF
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Paragraph 443; 445-446, (2020/07/31)
The present disclosure relates to compounds of formula (AI), (I), (AII), and (II), or a pharmaceutically acceptable salt, solvate, stereoisomer, or tautomer thereof, a pharmaceutical composition comprising a compound of formula (AI), (I), (AII), and (II), and use thereof, wherein R2, R3, R4, R5, R6, R7, R10, R11a, R11b, R12, R16, R19a, R19b, and R20 are described herein. Such compounds are envisioned useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, movement disorders, convulsive disorders, schizophrenin spectrum disorders, disorders of memory and/or cognition, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, or tinnitus etc.
Steroid compound, application and preparation method thereof
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Paragraph 0059-0061, (2020/07/24)
The invention relates to a steroid compound, an application and a preparation method thereof. The compounds are expected to be capable of effectively treating neuropsychiatric diseases, and have goodactive efficacy, pharmacokinetic (PK) performance, oral
C17, C20, AND C21 SUBSTITUTED NEUROACTIVE STEROIDS AND THEIR METHODS OF USE
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Page/Page column 193; 194; 207; 208, (2018/03/25)
Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.
Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1′-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor
Martinez Botella, Gabriel,Salituro, Francesco G.,Harrison, Boyd L.,Beresis, Richard T.,Bai, Zhu,Blanco, Maria-Jesus,Belfort, Gabriel M.,Dai, Jing,Loya, Carlos M.,Ackley, Michael A.,Althaus, Alison L.,Grossman, Scott J.,Hoffmann, Ethan,Doherty, James J.,Robichaud, Albert J.
, p. 7810 - 7819 (2017/10/06)
Certain classes of neuroactive steroids (NASs) are positive allosteric modulators (PAM) of synaptic and extrasynaptic GABAA receptors. Herein, we report new SAR insights in a series of 5β-nor-19-pregnan-20-one analogues bearing substituted pyrazoles and triazoles at C-21, culminating in the discovery of 3α-hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1′-yl)-19-nor-5β-pregnan-20-one (SAGE-217, 3), a potent GABAA receptor modulator at both synaptic and extrasynaptic receptor subtypes, with excellent oral DMPK properties. Compound 3 has completed a phase 1 single ascending dose (SAD) and multiple ascending dose (MAD) clinical trial and is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD), major depressive disorder (MDD), and essential tremor (ET).
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
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Page/Page column 78, (2016/06/14)
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.
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
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Page/Page column 67; 68, (2015/12/17)
Provided herein are 19-nor C3, 3-disubstituted steroids of Formula (I) : and pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4are as defined herein, and A is a heteroaryl ring system comprising 3 or 4 nitrogens 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.
19-NOR C3,3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF
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Page/Page column 85, (2014/11/11)
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 R7are 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.
19-NOR NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF
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Page/Page column 82; 83, (2014/11/11)
Provided herein are 3,3-disubstituted19-nor-steroidal compounds according to Formula(I): and pharmaceutical compositions thereof. 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, 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, tinnitus, status epilepticus.
19-NOR NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF
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Page/Page column 98, (2014/11/11)
Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. 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, 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, tinnitus, and status epilepticus.
