US2015158903A1PendingUtilityA1
Neuroactive steroids, compositions, and uses thereof
Individually held — no corporate assignee on recordPriority: Sep 8, 2011Filed: Sep 7, 2012Published: Jun 11, 2015
Est. expirySep 8, 2031(~5.1 yrs left)· nominal 20-yr term from priority
Inventors:Ravindra B. UpasaniBoyd L. HarrisonBenny C. Askew, Jr.Jean-Cosme DodartFrancesco G. SalituroAlbert Jean Robichaud
A61P 43/00A61P 9/10A61P 25/16A61P 25/30A61P 25/24A61P 25/14A61P 25/08A61P 25/20A61P 25/32A61P 27/16A61P 25/04A61P 25/18A61P 25/28A61P 25/22A61P 25/36A61P 25/00C07J 75/00C07J 9/005C07J 1/0029C07J 7/007C07J 31/006C07J 41/0011C07J 3/00C07J 31/003C07J 9/00C07J 1/00C07J 41/0055C07J 43/003C07J 41/00C07J 41/0005C07J 31/00A61K 31/575A61K 31/57
58
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Claims
Abstract
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L 1 , L 2 , L 3 , X 1 , X 2 , Y, R z4 , R z5 , R z6 , n, R 1 , R 2 , R 3a , R 3b , R 4a , R 4b , R 6a , R 6b , R 7a , R 7b , R 11a , R 11b , R 14 , R 17 , R 19 , R 20 , R 23a , R 23b , and R 24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
Claims
exact text as granted — not AI-modified1 . A compound of Formula:
or a pharmaceutically acceptable salt thereof;
wherein:
Z is a group of the formula (i), (ii), (iii), (iv), or (v):
L 1 and L 2 are selected from a group consisting of a bond, a substituted or unsubstituted C 1 -C 6 alkylene, a substituted or unsubstituted C 2 -C 6 alkenylene, substituted or unsubstituted C 2 -C 6 alkynylene, a substituted or unsubstituted hetero C 1 -C 6 alkylene, a substituted or unsubstituted hetero C 2 -C 6 alkenylene, and a substituted or unsubstituted hetero C 2 -C 6 alkynylene;
L 3 is a substituted or unsubstituted C 1 -C 6 alkylene, a substituted or unsubstituted C 2 -C 6 alkenylene, substituted or unsubstituted C 2 -C 6 alkynylene, a substituted or unsubstituted hetero C 1 -C 6 alkylene, a substituted or unsubstituted hetero C 2 -C 6 alkenylene, or a substituted or unsubstituted hetero C 2 -C 6 alkynylene;
each instance of X 1 and X 2 is independently —O—, —S—, or —NH—;
R 1 is hydrogen or substituted or unsubstituted alkyl;
R 3b is hydrogen;
R 3a is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
each instance of R 2 , R 11a , and R 11b is independently hydrogen or —OR B1 , wherein R B1 is hydrogen or substituted or unsubstituted alkyl, or R 11a and R 11b are joined to form an oxo (═O) group;
each of R 6a and R 6b is independently hydrogen, halo, or substituted or unsubstituted alkyl, and represents a single or double bond, provided if a double bond is present, then one of R 6a or R 6b is absent, and provided if a single bond is present, then the hydrogen at C5 is in the alpha or beta position;
each instance of R 19 and R 20 is independently hydrogen or —CH 3 ;
and each instance of R 23a and R 23b is independently hydrogen, halogen, or substituted or unsubstituted alkyl, or R 23a and R 23b are joined together to form substituted or unsubstituted C 3 -C 6 cycloalkyl;
R 24 is hydrogen or substituted or unsubstituted alkyl;
Y is —O—, —S—, or —NR Z5 —;
R Z4 is independently substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —OR Z5 , —SR Z5 , or —N(R Z5 ) 2 ;
each instance of R Z5 is independently hydrogen or substituted or unsubstituted alkyl; and
each instance of R Z6 is independently hydrogen or substituted or unsubstituted alkyl, or two R Z6 groups are joined to form a C 3-6 carbocyclic ring; and
the subscript n is 0 or 1;
provided the following compounds are specifically excluded:
2 . The compound of claim 1 wherein Z is a group of formula:
3 . The compound of claim 2 , wherein L 3 is a group of formula:
wherein p is 1, 2, or 3; and each instance of R Z7 and R Z8 is, independently, hydrogen, halo, substituted or unsubstituted C 1-6 alkyl, or —OR Z5 .
4 . The compound of claim 2 , wherein L 3 is a group of formula:
wherein w is 0 or 1 and p is 1, 2, or 3, or w is 1 and p is 0, 1, 2, or 3; and each instance of R Z7 and R Z8 is independently hydrogen, halo, substituted or unsubstituted C 1-6 alkyl, or —OR Z5 .
5 . The compound of claim 2 , wherein L 3 is a group of formula:
6 . The compound of claim 2 , wherein L 3 is a group of formula:
7 . The compound of claim 2 , wherein L 3 is a group of formula:
8 . The compound of claim 1 , wherein Z is of formula
9 . The compound of claim 8 , wherein the group
is of the formula:
10 . The compound of claim 1 , Z is of formula
11 . The compound of claim 10 , wherein Y is —O— and L 3 is an alkylene or heteroalkylene group.
12 . The compound of claim 11 , wherein the group
is of the formula:
13 . The compound of claim 1 , wherein Z is of formula
14 . The compound of claim 13 , wherein Y is —O— and L 3 is an alkylene or heteroalkylene.
15 . The compound of claim 14 , wherein the group
is of the formula:
16 . The compound of claim 1 , wherein the group —X 1 R 3b is in the beta position, and R 3a is in the alpha position.
17 . The compound of claim 1 , wherein —X 1 R 3b is —OH.
18 . The compound of claim 1 , wherein R 3a is hydrogen.
19 . The compound of claim 1 , wherein R 3a is substituted or unsubstituted alkyl.
20 . The compound of claim 1 , wherein represents a double bond and R 6a is halo or substituted or unsubstituted alkyl
21 . The compound of claim 1 , wherein R 6b is halo or substituted or unsubstituted alkyl.
22 . The compound of claim 1 , wherein R 2 is hydrogen.
23 . The compound of claim 1 , wherein R 2 is —OR B .
24 . The compound of claim 1 , wherein R 11b is hydrogen or —OR B , and R 11a is hydrogen.
25 . The compound of claim 1 , wherein R 11a and R 11b together form an oxo group.
26 . The compound of claim 1 , wherein represents a single bond, and the hydrogen at C5 is in the alpha position.
27 . The compound of claim 1 , wherein represents a double bond.
28 . The compound of claim 1 , wherein R 19 is —CH 3 .
29 . The compound of claim 1 , wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
30 . (canceled)
31 . The compound of claim 1 , wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
32 . The compound of claim 1 , wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
33 . The compound of claim 1 , wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
34 . The compound of claim 1 , wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
35 . The compound of claim 1 , wherein the compound is selected from the group consisting of:
36 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and an effective amount of a compound of any one of the preceding claims.
37 . A method for preventing, treating, ameliorating or managing a disease or condition which comprises administering to a patient in need of such prevention, treatment, amelioration or management, a prophylactically or therapeutically effective amount of a compound or pharmaceutical composition of any one of the preceding claims.
38 - 41 . (canceled)Join the waitlist — get patent alerts
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