- NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
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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.
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Page/Page column 132; 133
(2015/12/17)
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- 19-NOR C3,3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF
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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.
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Page/Page column 107
(2014/11/11)
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- 19-NOR NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF
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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.
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Page/Page column 121; 122
(2014/11/11)
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- The Preparation of 7α- and 7β-Allyloestradiol, and an Unusual Titanium(IV) Chloride Mediated Dimerisation
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17β-Acetoxyoestra-4,6-dien-3-one reacts with allyltrimethylsilane in the presence of fluoride ion to give the 7α- and 7β-allyloestr-4-en-3-ones in low yield.With titanium(IV) chloride catalysis, the 7α-allyloestr-4-en-3-one is the only product at -78 deg C, but its novel 6β,6'β-'dimer' is also formed at higher temperatures.The isomeric 7-allyloestr-4-en-3-ones have been aromatised to give 7α- and 7β-allyloestradiols.
- Miller, Barry W.,Kirk, David M.
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p. 2127 - 2156
(2007/10/02)
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- Synthesis of gon-4-enes
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1. A therapeutic composition having progestational activity comprising as active ingredient a 17-aliphatic carboxylic acid ester of 17α-ethynyl-18-methyl-19-nortestosterone and a pharmaceutical carrier for said compound.
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- Synthesis of 13-alkyl-gon-4-ones
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The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.
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- Steroidal imidazole 1 carboxylic acid esters
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A variety of steroidal esters of imidazole 1 carboxylic acid and related acids was prepared by reaction of the steroidal alcohol with N,N' carbonyldiimidazole or by displacement of phenol from steroid phenylcarbonates. One compound, 21c (the imidazole 1 carboxylate of 19 norethisterone), was found to have an interesting separation of progestational from androgenic activity.
- Fahrenholtz,Boris,Kennedy Jr,Kierstead
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p. 337 - 342
(2007/10/10)
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