US2023250128A1PendingUtilityA1
Neuroactive steroids and compositions thereof
Est. expiryMay 31, 2039(~12.8 yrs left)· nominal 20-yr term from priority
C07J 43/003C07J 1/0011C07J 9/00C07J 41/0055C07J 51/00C07J 11/00C07J 7/007C07J 1/0022C07J 21/008C07J 41/0094C07J 7/002C07J 9/005C07J 7/0085C07J 31/006C07J 5/0015C07J 71/001C07J 13/007C07J 17/00C07J 31/003C07J 21/00C07J 41/0088C07J 7/0095A61P 25/00A61P 25/18A61P 25/20A61P 25/28A61P 25/14A61P 25/24A61P 25/30A61P 25/08A61P 27/16A61P 9/00A61P 7/00A61P 29/00A61P 25/04A61K 31/58
78
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Cited by
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Claims
Abstract
Provided herein is a compound of Formula (I):or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7a, R7a, R11a, R11b, R12a, R12b, R16a, R16b, R19, R11a, R22, RX, RY and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.
Claims
exact text as granted — not AI-modified1 - 104 . (canceled)
105 . A method of treating a CNS-related disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I-e6):
a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising a compound of Formula (I-e6) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient;
wherein:
each of R 2a , R 2b , R 15a , and R 15b is hydrogen;
R 3 is unsubstituted C 1-3 alkyl, —CH 2 OCH 3 , or —CH 2 OCH 2 CH 3 ;
R 19 is hydrogen, methyl, or ethyl;
R X is —OH;
R Y is methyl; and
R 22 is —CN.
106 . The method of claim 105 , wherein R 3 is methyl, ethyl, or propyl.
107 . The method of claim 106 , wherein R 3 is methyl.
108 . The method of claim 106 , wherein R 3 is ethyl.
109 . The method of claim 106 , wherein R 3 is propyl.
110 . The method of claim 105 , wherein R 3 is —CH 2 OCH 3 .
111 . The method of claim 105 , wherein R 3 is —CH 2 OCH 2 CH 3 .
112 . The method of claim 105 , wherein R 19 is hydrogen.
113 . The method of claim 105 , wherein R 19 is methyl.
114 . The method of claim 105 , wherein R 19 is ethyl.
115 . The method of claim 105 , wherein the CNS-related disorder is a sleep disorder, a mood disorder, a schizophrenia spectrum disorder, a convulsive disorder, a disorder of memory and/or cognition, a movement disorder, a personality disorder, autism spectrum disorder, pain, traumatic brain injury, a vascular disease, a substance abuse disorder and/or withdrawal syndrome, tinnitus, or status epilepticus.
116 . The method of claim 105 , wherein the CNS-related disorder is depression.
117 . The method of claim 116 , wherein the depression is postpartum depression.
118 . The method of claim 116 , wherein the depression is major depressive disorder.
119 . The method of claim 118 , wherein the major depressive disorder is moderate major depressive disorder.
120 . The method of claim 118 , wherein the major depressive disorder is severe major depressive disorder.
121 . The method of claim 105 , wherein the CNS-related disorder is tremor.
122 . The method of claim 121 , wherein the tremor is essential tremor.
123 . The method of claim 105 , wherein the CNS-related disorder is seizure.
124 . The method of claim 105 , wherein the CNS-related disorder is epilepsy or status epilepticus.
125 . The method of claim 124 , wherein the CNS-related disorder is status epilepticus, and wherein the status epilepticus is convulsive status epilepticus or non-convulsive status epilepticus.
126 . The method of claim 105 , wherein the CNS-related disorder is Tourette's syndrome.
127 . The method of claim 105 , wherein the CNS-related disorder is obsessive compulsive disorder (OCD).
128 . A method of treating a CNS-related disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound selected from
Com-
pound
No.
Structure
2
3
7
11
15
24
26
a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
129 . The method of claim 128 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
130 . The method of claim 128 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
131 . The method of claim 128 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
132 . The method of claim 128 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
133 . The method of claim 128 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
134 . The method of claim 128 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
135 . The method of claim 128 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
136 . The method of claim 128 , wherein the CNS-related disorder is a sleep disorder, a mood disorder, a schizophrenia spectrum disorder, a convulsive disorder, a disorder of memory and/or cognition, a movement disorder, a personality disorder, autism spectrum disorder, pain, traumatic brain injury, a vascular disease, a substance abuse disorder and/or withdrawal syndrome, tinnitus, or status epilepticus.
137 . The method of claim 128 , wherein the CNS-related disorder is depression.
138 . The method of claim 137 , wherein the depression is postpartum depression.
139 . The method of claim 137 , wherein the depression is major depressive disorder.
140 . The method of claim 139 , wherein the major depressive disorder is moderate major depressive disorder.
141 . The method of claim 139 , wherein the major depressive disorder is severe major depressive disorder.
142 . The method of claim 128 , wherein the CNS-related disorder is tremor.
143 . The method of claim 142 , wherein the tremor is essential tremor.
144 . The method of claim 128 , wherein the CNS-related disorder is seizure.
145 . The method of claim 128 , wherein the CNS-related disorder is epilepsy or status epilepticus.
146 . The method of claim 145 , wherein the CNS-related disorder is status epilepticus, and wherein the status epilepticus is convulsive status epilepticus or non-convulsive status epilepticus.
147 . The method of claim 128 , wherein the CNS-related disorder is Tourette's syndrome.
148 . The method of claim 128 , wherein the CNS-related disorder is obsessive compulsive disorder (OCD).
149 . A method of treating a CNS-related disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound selected from
Com-
pound No.
Structure
29
42
44
a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
150 . The method of claim 149 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
151 . The method of claim 149 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
152 . The method of claim 149 , wherein the compound is a compound of the formula
or a pharmaceutically acceptable salt thereof.
153 . The method of claim 149 , wherein the CNS-related disorder is a sleep disorder, a mood disorder, a schizophrenia spectrum disorder, a convulsive disorder, a disorder of memory and/or cognition, a movement disorder, a personality disorder, autism spectrum disorder, pain, traumatic brain injury, a vascular disease, a substance abuse disorder and/or withdrawal syndrome, tinnitus, or status epilepticus.
154 . The method of claim 149 , wherein the CNS-related disorder is depression.
155 . The method of claim 154 , wherein the depression is postpartum depression.
156 . The method of claim 154 , wherein the depression is major depressive disorder.
157 . The method of claim 156 , wherein the major depressive disorder is moderate major depressive disorder.
158 . The method of claim 156 , wherein the major depressive disorder is severe major depressive disorder.
159 . The method of claim 149 , wherein the CNS-related disorder is tremor.
160 . The method of claim 159 , wherein the tremor is essential tremor.
161 . The method of claim 149 , wherein the CNS-related disorder is seizure.
162 . The method of claim 149 , wherein the CNS-related disorder is epilepsy or status epilepticus.
163 . The method of claim 162 , wherein the CNS-related disorder is status epilepticus, and wherein the status epilepticus is convulsive status epilepticus or non-convulsive status epilepticus.
164 . The method of claim 149 , wherein the CNS-related disorder is Tourette's syndrome.
165 . The method of claim 149 , wherein the CNS-related disorder is obsessive compulsive disorder (OCD).Join the waitlist — get patent alerts
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