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NZ738582B2 - Oxysterols and methods of use thereof - Google Patents
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NZ738582B2 - Oxysterols and methods of use thereof - Google Patents

Oxysterols and methods of use thereof Download PDF

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Publication number
NZ738582B2
NZ738582B2 NZ738582A NZ73858216A NZ738582B2 NZ 738582 B2 NZ738582 B2 NZ 738582B2 NZ 738582 A NZ738582 A NZ 738582A NZ 73858216 A NZ73858216 A NZ 73858216A NZ 738582 B2 NZ738582 B2 NZ 738582B2
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NZ
New Zealand
Prior art keywords
independently
compound
alkyl
acceptable salt
xrb
Prior art date
Application number
NZ738582A
Other versions
NZ738582A (en
Inventor
Botella Gabriel Martinez
Albert Jean Robichaud
Francesco G Salituro
Original Assignee
Sage Therapeutics Inc
Filing date
Publication date
Application filed by Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Priority claimed from PCT/US2016/041160 external-priority patent/WO2017007832A1/en
Publication of NZ738582A publication Critical patent/NZ738582A/en
Publication of NZ738582B2 publication Critical patent/NZ738582B2/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Abstract

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R5, and R8are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Claims (67)

What is claimed is:
1. A compound of Formula (I-AA): (I-AA) or a pharmaceutically acceptable salt thereof, wherein: R1 is C1-6 alkyl; each of R2 and R3 is independently hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, or R2 and R3, together with the carbon atom to which they are attached, form a 3-8 membered carbocyclyl or heterocyclyl; each of R4 and R5 is independently hydrogen, -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, (Rd)2, -(CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, - (CH2)pC(O)ORc, or any amino acid e; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; each of n, m, and p is independently 1, 2, 3, or 4; provided that R4 and R5 are not both hydrogen; R8 is absent or en; and represents a single or double bond, wherein when one is a double bond, the other is a single bond and R8 is absent, wherein: each instance of C1-6 alkyl is independently optionally substituted with 1-5 tuents independently selected from the group consisting of halogen, -CN, -OH, C1- 6 alkoxy, -NH2, -CO2H, and -C(O)(C1-6 alkyl); and each instance of carbocyclyl and heterocyclyl is independently ally substituted with 1-5 substituents ndently selected from the group consisting of halogen, -CN, -OH, C1-6 alkyl, C1-6 alkoxy, -NH2, -CO2H, and -C(O)(C1-6 alkyl).
2. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R4 is not hydrogen.
3. The nd of claim 1, or a pharmaceutically acceptable salt f, wherein R5 is not hydrogen.
4. The compound of claim 1, or a ceutically acceptable salt thereof, wherein each of R4 and R5 is independently hydrogen, -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, - C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or - (CH2)pC(O)ORc; each of Ra and Rb is independently selected from -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is ndently 1 or 2; and each of n, m, p is independently 1, 2, 3, or 4, provided that R4 and R5 are not both hydrogen.
5. The compound of claim 1, or a pharmaceutically acceptable salt thereof, n R4 is hydrogen, -S(O)xRb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, - (CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or pC(O)ORc; each of Ra and Rb is independently selected from -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; and each of n, m, p is ndently 1, 2, 3, or 4.
6. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R1 is methyl, -CF3, -CH2OCH3, ethyl, or isopropyl.
7. The compound of claim 6, or a pharmaceutically acceptable salt thereof, wherein R1 is methyl or ethyl.
8. The compound of claim 1, or a ceutically acceptable salt thereof, wherein each of R2 and R3 is independently hydrogen, methyl, -CF3, ethyl, isopropyl, cyclopropyl, or butyl.
9. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R4 is - P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, - (CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or -(CH2)pC(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; each of n, m, p is independently 1, 2, 3, or 4; and R5 is hydrogen.
10. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R4 is en and R5 is -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, - (CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or - (CH2)pC(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is ndently hydrogen or C1-6 alkyl; each x is independently 1 or 2; and each of n, m, p is independently 1, 2, 3, or 4.
11. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein each of R4 and R5 is ndently -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, (Rd)2, - (CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or - C(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; and each of n, m, p is ndently 1, 2, 3, or 4.
12. The compound of claim 1, or a pharmaceutically acceptable salt f, wherein when R4 is hydrogen, R5 is -S(O)xRb and x is 2, Rb is not -OH.
13. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen; R5 is -P(O)(Ra)2, -S(O)xRb, c, -C(O)ORc, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, - (CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, pOC(O)Rc, or -(CH2)pC(O)ORc; each of Ra and Rb is ndently selected from -ORd or C1-6 alkyl; each Rc is ndently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; and each of n, m, p is independently 1, 2, 3, or 4; wherein when R5 is -S(O)xRb and x is 2, Rb is not -OH.
14. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R4 is - P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, - (CH2)mOS(O)xRb, or -(CH2)pOC(O)Rc.
15. The compound of claim 14, or a pharmaceutically acceptable salt thereof, wherein each of Ra and Rb is independently -ORd, Rd is hydrogen or C1-6 alkyl, and x is 2.
16. The compound of claim 14, or a pharmaceutically able salt thereof, wherein Rc is -CH2NH2, -CH2CH2CO2H, -CH(CH(CH3)2)NH2, or -CH(CH3)NH2.
17. The compound of claim 14, or a pharmaceutically acceptable salt thereof, wherein each of n, m, and p is independently 1 or 2.
18. The compound of claim 14, or a pharmaceutically acceptable salt thereof, wherein R4 is -P(O)OH2, -S(O)2OH, (O)(OH)2, -C(O)CH3, -C(O)CH2NH2, -C(O)CH2CH2C(O)OH, - C(O)CH(CH(CH3)2)NH2, or -C(O)CH(CH3)NH2,.
19. The compound of claim 1, or a ceutically acceptable salt thereof, wherein R5 is - P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, - (CH2)mOS(O)xRb, or -(CH2)pOC(O)Rc.
20. The compound of claim 19, or a ceutically acceptable salt thereof, wherein each of Ra and Rb is independently -ORd, Rd is hydrogen or substituted or unsubstituted alkyl, and x is 2.
21. The compound of claim 19, or a pharmaceutically acceptable salt thereof, wherein each of n, m, and p is independently 1 or 2.
22. The nd of claim 19, or a pharmaceutically acceptable salt f, wherein R5 is -P(O)OH2, -S(O)2OH, -CH2OP(O)(OH)2, -C(O)CH3, -C(O)CH2NH2, -C(O)CH2CH2C(O)OH, - C(O)CH(CH(CH3)2)NH2, or -C(O)CH(CH3)NH2.
23. The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein each of is a single bond.
24. The compound of claim 1, wherein the compound of Formula (I-AA) is a compound of Formula (I-A) or a (I-B): (I-A) or (I-B), or a pharmaceutically acceptable salt thereof.
25. The compound of claim 24, wherein the compound of Formula (I-AA) is a nd of Formula (I-B): (I-B), or a pharmaceutically acceptable salt thereof.
26. The compound of claim 25, or a pharmaceutically acceptable salt thereof, wherein R1 is methyl, -CF3, H3, ethyl, or isopropyl.
27. The compound of claim 25, or a pharmaceutically acceptable salt thereof, wherein each of R2 and R3 is independently en, methyl, -CF3, ethyl, isopropyl, cyclopropyl, or butyl.
28. The compound of claim 27, or a pharmaceutically acceptable salt f, wherein each of R2 and R3 is independently hydrogen, methyl, -CF3, ethyl, or isopropyl.
29. The nd of claim 25, or a pharmaceutically acceptable salt thereof, wherein R4 is -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, - (CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or -(CH2)pC(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is ndently hydrogen or C1-6 alkyl; each x is independently 1 or 2; each of n, m, p is independently 1, 2, 3, or 4; and R5 is hydrogen.
30. The compound of claim 25, or a ceutically acceptable salt thereof, wherein R4 is en and R5 is -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, - (CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or - (CH2)pC(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is ndently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; and each of n, m, p is independently 1, 2, 3, or 4.
31. The compound of claim 25, or a pharmaceutically acceptable salt thereof, wherein each of R4 and R5 is independently Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, - (CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or - (CH2)pC(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; and each of n, m, p is independently 1, 2, 3, or 4.
32. The compound of claim 25, or a pharmaceutically acceptable salt f, wherein: each of R4 and R5 is independently hydrogen, -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, -(CH2)pOC(O)Rc, or -(CH2)pC(O)ORc; each of Ra and Rb is independently selected from -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is ndently hydrogen or C1-6 alkyl; each x is independently 1 or 2; and each of n, m, p is independently 1, 2, 3, or 4, provided that R4 and R5 are not both hydrogen and wherein when R4 is hydrogen and R5 is -S(O)xRb and x is 2, Rb is not -OH.
33. The compound of claim 25, or a ceutically acceptable salt thereof, wherein R4 is hydrogen; R5 is -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, -(CH2)pOC(O)Rc, or -(CH2)pC(O)ORc; each of Ra and Rb is independently selected from -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; each of n, m, p is independently 1, 2, 3, or 4; and wherein when R5 is -S(O)xRb and x is 2, Rb is not -OH.
34. The compound of claim 25, or a pharmaceutically acceptable salt f, wherein R4 is -P(O)(Ra)2, Rb, -C(O)Rc, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, or -(CH2)pOC(O)Rc.
35. The compound of claim 34, or a pharmaceutically acceptable salt thereof, wherein R4 is -P(O)OH2, -S(O)2OH, -CH2OP(O)(OH)2, -C(O)CH3, -C(O)CH2NH2, -C(O)CH2CH2C(O)OH, - C(O)CH(CH(CH3)2)NH2, or -C(O)CH(CH3)NH2.
36. The compound of claim 33, or a pharmaceutically acceptable salt thereof, wherein R5 is -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, nOP(O)(Ra)2, -(CH2)mOS(O)xRb, or -(CH2)pOC(O)Rc.
37. The compound of claim 25, or a ceutically acceptable salt thereof, wherein R5 is -P(O)(OH)2, -S(O)2OH, -CH2OP(O)(OH)2, -C(O)CH3, -C(O)CH2NH2, H2CH2C(O)OH, -C(O)CH(CH(CH3)2)NH2, or -C(O)CH(CH3)NH2.
38. The nd of claim 25, or a pharmaceutically acceptable salt thereof, wherein when R4 is hydrogen, R5 is not -S(O)2OH.
39. The compound of claim 25, wherein the compound of Formula (I-B) is a nd of a (I-C): (I-C), or a pharmaceutically acceptable salt thereof.
40. The compound of claim 39, or a pharmaceutically acceptable salt thereof, wherein R1 is methyl, -CF3, -CH2OCH3, ethyl, or isopropyl.
41. The compound of claim 40, or a pharmaceutically acceptable salt thereof, wherein R1 is methyl or ethyl.
42. The compound of claim 39, or a pharmaceutically acceptable salt thereof, wherein R4 is -P(O)(Ra)2, Rb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, - (CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or -(CH2)pC(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; each of n, m, p is independently 1, 2, 3, or 4; and R5 is hydrogen.
43. The compound of claim 42, or a pharmaceutically acceptable salt thereof, wherein R4 is -P(O)(Ra)2, -S(O)xRb, c, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, or -(CH2)pOC(O)Rc.
44. The compound of claim 43, or a pharmaceutically acceptable salt thereof, wherein R4 is OH)2, -S(O)2OH, (O)(OH)2, H3, -C(O)CH2NH2, -C(O)CH2CH2C(O)OH, -C(O)CH(CH(CH3)2)NH2, or -C(O)CH(CH3)NH2.
45. The compound of claim 39, or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen and R5 is -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, - (CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, -(CH2)mOS(O)xRb, -(CH2)pOC(O)Rc, or - (CH2)pC(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is ndently 1 or 2; and each of n, m, p is independently 1, 2, 3, or 4.
46. The compound of claim 45, or a ceutically acceptable salt thereof, wherein R5 is -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -(CH2)nOP(O)(Ra)2, -C(O)N(Rd)2, -(CH2)xC(O)N(Rd)2, - (CH2)mOS(O)xRb, or -(CH2)pOC(O)Rc.
47. The compound of claim 46, or a pharmaceutically able salt thereof, wherein R5 is -P(O)(OH)2, -S(O)2OH, (O)(OH)2, -C(O)CH3, -C(O)CH2NH2, -C(O)CH2CH2C(O)OH, -C(O)CH(CH(CH3)2)NH2, or -C(O)CH(CH3)NH2.
48. The compound of claim 39, or a pharmaceutically acceptable salt thereof, wherein each of R4 and R5 is independently -P(O)(Ra)2, -S(O)xRb, -C(O)Rc, -C(O)ORc, -C(O)N(Rd)2, - (CH2)xC(O)N(Rd)2, -(CH2)nOP(O)(Ra)2, mOS(O)xRb, -(CH2)pOC(O)Rc, or - (CH2)pC(O)ORc; each of Ra and Rb is independently -ORd or C1-6 alkyl; each Rc is independently C1-6 alkyl; each Rd is independently hydrogen or C1-6 alkyl; each x is independently 1 or 2; and each of n, m, p is independently 1, 2, 3, or 4.
49. The compound of claim 39, wherein the compound of Formula (I-C) is a compound of Formula (I-D): (I-D), or a pharmaceutically acceptable salt thereof.
50. A nd selected from: , , H2N (S) , , , , , , S ONa H H HO , , , , , , , , , , , , , , or P ONa NaO H H NaO .
51. A compound selected from: , , or .
52. A ceutically acceptable salt of: , , H2N (S) , , , , , , , , , , , , , or .
53. A pharmaceutical composition comprising a compound of any one of claims 1-51, and a pharmaceutically acceptable carrier.
54. A pharmaceutical composition comprising a pharmaceutically acceptable salt of any one of claims 1-49 and 52, and a pharmaceutically acceptable carrier.
55. Use of a compound or pharmaceutically acceptable salt of any one of claims 1-52, or a pharmaceutical composition of claim 53 or 54, in the manufacture of a medicament for inducing sedation or anesthesia.
56. Use of a compound or ceutically acceptable salt of any one of claims 1-52, or a pharmaceutical composition of claim 53 or 54, in the manufacture of a medicament for ng or preventing a disorder.
57. The use of claim 56, wherein the disorder is a gastrointestinal (GI) disorder, a structural er affecting the GI tract, an anal disorder, colon polyps, cancer, colitis, diabetes, or a sterol synthesis disorder.
58. The use of claim 57, wherein the disorder is a GI disorder, n the GI disorder is inflammatory bowel disease.
59. The use of claim 57, wherein the disorder is cancer, diabetes, or a sterol sis disorder.
60. Use of a compound or pharmaceutically acceptable salt of any one of claims 1-52, or a pharmaceutical composition of claim 53 or 54, in the cture of a medicament for treating or preventing a CNS-related condition.
61. The use of claim 60, wherein the CNS-related condition is an adjustment disorder, an anxiety er, a ive er, a dissociative disorder, an eating disorder, a mood disorder, a psychotic disorder, a sleep disorder, a substance-related disorder, a personality disorder, an autism spectrum disorder, a neurodevelopmental disorder, multiple sclerosis, a sterol synthesis disorder, pain, an encephalopathy secondary to a medical condition, a seizure disorder, stroke, traumatic brain injury, a movement disorder, vision ment, hearing loss, or tinnitus.
62. The use of claim 61, wherein the CNS-related condition is a sterol synthesis disorder.
63. The use of claim 60, wherein the CNS-related condition is schizophrenia.
64. The use of claim 61, wherein the CNS-related condition is an autism spectrum disorder.
65. The use of claim 60, n the CNS-related condition is Huntington’s disease or Parkinson’s disease.
66. The use of claim 60, wherein the CNS-related condition is mer’s disease.
67. The use of claim 60, n the CNS-related condition is anti-NMDA receptor encephalitis.
NZ738582A 2016-07-06 Oxysterols and methods of use thereof NZ738582B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562189065P 2015-07-06 2015-07-06
PCT/US2016/041160 WO2017007832A1 (en) 2015-07-06 2016-07-06 Oxysterols and methods of use thereof

Publications (2)

Publication Number Publication Date
NZ738582A NZ738582A (en) 2024-10-25
NZ738582B2 true NZ738582B2 (en) 2025-01-28

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