HRP20210526T1 - Oksisteroli i postupci za njihovu uporabu - Google Patents
Oksisteroli i postupci za njihovu uporabu Download PDFInfo
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- HRP20210526T1 HRP20210526T1 HRP20210526TT HRP20210526T HRP20210526T1 HR P20210526 T1 HRP20210526 T1 HR P20210526T1 HR P20210526T T HRP20210526T T HR P20210526TT HR P20210526 T HRP20210526 T HR P20210526T HR P20210526 T1 HRP20210526 T1 HR P20210526T1
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- compound
- formula
- pharmaceutically acceptable
- acceptable salt
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- 238000000034 method Methods 0.000 title claims 8
- 150000001875 compounds Chemical class 0.000 claims 46
- 150000003839 salts Chemical class 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 150000002431 hydrogen Chemical class 0.000 claims 16
- -1 -CHF2 Chemical group 0.000 claims 15
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 11
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 9
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 8
- 125000004452 carbocyclyl group Chemical group 0.000 claims 8
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 3
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims 3
- 230000002496 gastric effect Effects 0.000 claims 3
- 208000014617 hemorrhoid Diseases 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 208000016583 Anus disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000028017 Psychotic disease Diseases 0.000 claims 2
- 229930182558 Sterol Natural products 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 150000003432 sterols Chemical class 0.000 claims 2
- 235000003702 sterols Nutrition 0.000 claims 2
- 238000003786 synthesis reaction Methods 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002091 Anaesthesia Diseases 0.000 claims 1
- 206010048946 Anal abscess Diseases 0.000 claims 1
- 206010002153 Anal fissure Diseases 0.000 claims 1
- 208000008958 Anti-N-Methyl-D-Aspartate Receptor Encephalitis Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000014644 Brain disease Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010011878 Deafness Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 206010072378 Encephalitis autoimmune Diseases 0.000 claims 1
- 208000032274 Encephalopathy Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000009531 Fissure in Ano Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 208000032580 NMDA receptor encephalitis Diseases 0.000 claims 1
- 208000029726 Neurodevelopmental disease Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000009916 Postpartum depression Diseases 0.000 claims 1
- 208000004680 Rectal Fistula Diseases 0.000 claims 1
- 102100030681 SH3 and multiple ankyrin repeat domains protein 3 Human genes 0.000 claims 1
- 101710101741 SH3 and multiple ankyrin repeat domains protein 3 Proteins 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 206010039897 Sedation Diseases 0.000 claims 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 1
- 206010041250 Social phobia Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010047571 Visual impairment Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 208000012826 adjustment disease Diseases 0.000 claims 1
- 230000037005 anaesthesia Effects 0.000 claims 1
- 206010002156 anal fistula Diseases 0.000 claims 1
- 208000029188 anti-NMDA receptor encephalitis Diseases 0.000 claims 1
- 208000029560 autism spectrum disease Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 208000018459 dissociative disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000024732 dysthymic disease Diseases 0.000 claims 1
- 230000010370 hearing loss Effects 0.000 claims 1
- 231100000888 hearing loss Toxicity 0.000 claims 1
- 208000016354 hearing loss disease Diseases 0.000 claims 1
- 208000007386 hepatic encephalopathy Diseases 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 206010022437 insomnia Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 208000030459 obsessive-compulsive personality disease Diseases 0.000 claims 1
- 230000036407 pain Effects 0.000 claims 1
- 208000022821 personality disease Diseases 0.000 claims 1
- 208000014081 polyp of colon Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 208000022610 schizoaffective disease Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 230000036280 sedation Effects 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 208000005809 status epilepticus Diseases 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 208000029257 vision disease Diseases 0.000 claims 1
- 230000004393 visual impairment Effects 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
-
- 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
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
- C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
- C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
- C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
- C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Anesthesiology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (20)
1. Spoj formule (I):
[image]
ili njegova farmaceutski prihvatljiva sol, u kojem:
R1 je C1-6 alkil;
svaki od R2 i R3 je neovisno vodik, halogen, C1-6 alkil ili karbociklil; ili
R2 i R3, zajedno sa atomom ugljika za koji su vezani, formiraju 3-8 -člani prsten;
R6 je odsutan ili vodik;
svaki od R7 i R8 je neovisno vodik, halogen, C1-6 alkil ili karbociklil; ili
svaki od R7 i R8, zajedno sa atomom ugljika za koji su vezani, formiraju 3-8 -člani prsten; ili
R2 i R7, zajedno sa atomima ugljika za koje su vezani, formiraju 3-8 -člani prsten;
n je 1, 2 ili 3;
[image]
predstavlja jednostruku ili dvostruku vezu, pri čemu kada je jedan
[image]
jednostruka veza, drugi
[image]
je dvostruka veza;
i kada je jedan od
[image]
dvostruka veza, R6 je odsutan; i
pri čemu svaki slučaj alkil grupe može biti nesupstituiran ili supstituiran sa jednim ili više supstituenata.
2. Spoj prema patentnom zahtjevu 1, naznačen time što je svaki
[image]
2. jednostruka veza.
3. Spoj prema patentnom zahtjevu 1, naznačen time što R1 je metil, -CHF2, -CF3, -CH2OCH3, -CH2OCH2CH3, etil ili izopropil.
4. Spoj prema patentnom zahtjevu 1, naznačen time što svaki od R2 i R3 je neovisno vodik, C1-6 alkil ili karbociklil, ili gdje su R2 i R3 uzeti zajedno sa atomom ugljika za koji su vezani tako da formiraju 3-8 -člani prsten;
ili gdje su R2 i R3 uzeti zajedno sa atomom ugljika za koji su vezani tako da formiraju 3-8 -člani prsten koji je karbociklil prsten (npr., ciklopropil).
5. Spoj prema patentnom zahtjevu 4, naznačen time što svaki od R2 i R3 je neovisno vodik, metil, -CF3, etil, CH2CF3, propil, izopropil, ciklopropil ili butil; R2 je vodik, metil, -CF3 ili etil; R3 je metil, -CF3, etil, CH2CF3, propil, izopropil, ciklopropil ili butil; R2 je vodik i R3 je C1-6 alkil; ili R2 je C1-6 alkil i R3 je C1-6 alkil.
6. Spoj prema patentnom zahtjevu 1, naznačen time što R7 i R8 su vodik; ili gdje je n jednako 1 i R7 i R8 su vodik.
7. Spoj prema patentnom zahtjevu 1, naznačen time što spoj formule (I) je:
i) spoj formule (II):
[image]
ili njegova farmaceutski prihvatljiva sol;
ii) spoj formule (II-A) ili formule (II-B):
[image]
ili njegova farmaceutski prihvatljiva sol;
iii) spoj formule (II-B-i) ili formule (II-B-ii):
[image]
ili njegova farmaceutski prihvatljiva sol;
iv) spoj formule (II-B-iii):
[image]
ili njegova farmaceutski prihvatljiva sol;
v) spoj formule (III):
[image]
ili njegova farmaceutski prihvatljiva sol;
vi) spoj formule (III-A) ili formule (III-B):
[image]
ili
[image]
ili njegova farmaceutski prihvatljiva sol;
vii) spoj formule (III-C) ili formule (III-D):
[image]
ili
[image]
ili njegova farmaceutski prihvatljiva sol;
viii) spoj formule (III-E) ili formule (III-F):
[image]
ili
[image]
ili njegova farmaceutski prihvatljiva sol;
ix) spoj formule (III-A-i-a) ili formule (III-B-i-a):
[image]
ili
[image]
[image]
ili njegova farmaceutski prihvatljiva sol;
x) spoj formule (IV):
[image]
ili njegova farmaceutski prihvatljiva sol;
xi) spoj formule (V):
[image]
ili njegova farmaceutski prihvatljiva sol;
xii) je spoj formule (V-A):
[image]
ili njegova farmaceutski prihvatljiva sol;
xiii) spoj formule (V-B):
[image]
ili njegova farmaceutski prihvatljiva sol;
xiv) spoj formule (V-C) ili formule (V-D):
[image]
ili
[image]
ili njegova farmaceutski prihvatljiva sol;
xv) spoj formule (V-E-i):
[image]
ili njegova farmaceutski prihvatljiva sol; ili
xvi) spoj formule (V-E-ii) ili (V-E-iii):
[image]
ili
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentnom zahtjevu 7, koji je spoj formule (III-A-i-a) ili formule (III-B-i-a), i pri čemu R1 je metil, -CHF2, -CF3, -CH2OCH3 ili -CH2OCH2CH3, etil ili izopropil.
9. Spoj prema patentnom zahtjevu 7, koji je spoj formule (III), i pri čemu je svaki od R2 i R3 neovisno vodik, C1-6 alkil ili karbociklil, i pri čemu su R2 i R3 uzeti zajedno sa atomom ugljika za koji su vezani tako da formiraju 3-8 -člani prsten; svaki od R2 i R3 je neovisno vodik, C1-6 alkil ili karbociklil;
svaki od R2 i R3 je neovisno vodik, metil, -CF3, etil, CH2CF3, propil, izopropil, ciklopropil ili butil;
R2 je vodik, metil, -CF3 ili etil; i R3 je neovisno vodik, metil, -CF3, etil, CH2CF3, propil, izopropil, ciklopropil ili butil; ili R3 je metil, -CF3, etil, -CH2CF3, propil, izopropil, ciklopropil, ili butil.
10. Spoj prema patentnom zahtjevu 7, koji je spoj formule (IV), i pri čemu R1 je metil, -CHF2, -CF3, -CH2OCH3, ili -CH2OCH2CH3, etil ili izopropil.
11. Spoj prema patentnom zahtjevu 7, koji je spoj formule (IV), i pri čemu je svaki od R2 i R3 neovisno vodik, C1-6 alkil ili karbociklil, i pri čemu su R2 i R3 uzeti zajedno sa atomom ugljika za koji su vezani tako da formiraju 3-8 -člani prsten; svaki od R2 i R3 je neovisno vodik, C1-6 alkil ili karbociklil;
svaki od R2 i R3 je neovisno vodik, metil, -CF3, etil, CH2CF3, propil, izopropil, ciklopropil ili butil;
R2 je vodik, metil, -CF3 ili etil i R3 je neovisno vodik, metil, -CF3, etil, CH2CF3, propil, izopropil, ciklopropil ili butil; ili R3 je metil, -CF3, etil, -CH2CF3, propil, izopropil, ciklopropil, butil i R2 je neovisno vodik, C1-6 alkil ili karbociklus.
12. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj izabran iz grupe koja se sastoji od:
[image]
i
[image]
ili njihove farmaceutski prihvatljive soli.
13. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj izabran od:
[image]
[image]
[image]
[image]
ili njihove farmaceutski prihvatljive soli.
14. Farmaceutski pripravak koja sadrži spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol i farmaceutski prihvatljiv nosač.
15. Spoj prema patentnom zahtjevu 1, za uporabu u terapiji ili kao lijek.
16. Spoj prema patentnom zahtjevu 1 za uporabu u postupku izabranom od;
i) postupka za indukciju sedacije ili anestezije;
ii) postupka za liječenje ili prevenciju gastrointestinalnog (GI) poremećaja npr., konstipacije, sindroma iritabilnog crijeva (IBS), upalne bolesti crijeva (IBD) (npr., ulceroznog kolitisa, Kronove bolesti), strukturnih poremećaja koji pogađaju GI, analnih poremećaja (npr., hemoroida, unutrašnjih hemoroida, vanjskih hemoroida, analnih fisura, perianalnih apscesa, analnih fistula), polipa na debelom crijevu, raka, kolitisa; i
iii) postupka za liječenje ili prevenciju stanja povezanog sa CNS-om,
pri čemu postupak sadrži primjenu na subjekta kod koga postoji potreba za tim efikasne količine spoja prema patentnom zahtjevu 1, ili njegove farmaceutski prihvatljive soli ili njegovog farmaceutskog pripravka.
17. Spoj za uporabu prema patentnom zahtjevu 16, naznačen time što poremećaj je upalna bolest crijeva; rak, dijabetes, ili poremećaj sinteze sterola ili metabolički poremećaj.
18. Spoj za uporabu prema patentnom zahtjevu 16, naznačen time što postupak je postupak za liječenje ili prevenciju stanja povezanog sa CNS-om izabranog od poremećaja prilagođavanja, poremećaja anksioznosti (uključujući opsesivno-kompulzivni poremećaj, posttraumatski stresni poremećaj i socijalnu fobiju), kognitivnog poremećaja (uključujući Alzheimer-ovu bolest i druge oblike demencije), disocijativnog poremećaja, poremećaja ishrane, poremećaja raspoloženja (uključujući depresiju (npr., postpartalnu depresiju), bipolarni poremećaj, distimični poremećaj, suicidalnost), shizofrenije ili drugog psihotičnog poremećaja (uključujući shizoafektivni poremećaj), poremećaja spavanja (uključujući nesanicu), poremećaja povezanog sa supstancom, poremećaja ličnosti (uključujući opsesivno-kompulzivni poremećaj ličnosti), poremećaja spektra autizma (uključujući one koji uključuju mutacije Shank grupe proteina (npr., Shank3)), neurorazvojnih poremećaja (uključujući Rett-ov sindrom, kompleks tuberozne skleroze), multiple skleroze, poremećaja sinteze sterola, bola (uključujući akutnu i kroničnu bol), encefalopatije sekundarne medicinskom stanju (uključujući hepatičku encefalopatiju i anti-NMDA receptor encefalitis), poremećaja napada (uključujući status epileptikus i monogene oblike epilepsije kao što je Dravet-ova bolest), moždanog udara, traumatske povrede mozga, poremećaja kretanja (uključujući Huntington-ovu bolest i Parkinson-ovu bolest), oštećenja vida, gubitka sluha i tinitusa.
19. Spoj prema patentnom zahtjevu 1, naznačen time što spoj je:
[image]
20. Farmaceutski prihvatljiva sol spoja prema patentnom zahtjevu 1, naznačena time što spoj je
[image]
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562189048P | 2015-07-06 | 2015-07-06 | |
| US201662280394P | 2016-01-19 | 2016-01-19 | |
| PCT/US2016/041168 WO2017007836A1 (en) | 2015-07-06 | 2016-07-06 | Oxysterols and methods of use thereof |
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| CN103958540B (zh) | 2011-09-08 | 2017-12-05 | 萨奇治疗股份有限公司 | 神经活性类固醇、组合物、及其用途 |
| SI3461834T1 (sl) | 2013-03-13 | 2021-11-30 | Sage Therapeutics, Inc. | Nevroaktivni steroidi |
| ES2970222T3 (es) | 2014-06-18 | 2024-05-27 | Sage Therapeutics Inc | Oxiesteroles y procedimientos de uso de los mismos |
| WO2016007762A1 (en) | 2014-07-09 | 2016-01-14 | Duke University | Compositions and methods for the repair of myelin |
| CA2991214C (en) | 2015-07-06 | 2024-04-30 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| WO2017007840A1 (en) | 2015-07-06 | 2017-01-12 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| JP6882996B2 (ja) | 2015-07-06 | 2021-06-02 | セージ セラピューティクス， インコーポレイテッド | オキシステロールおよびそれらの使用の方法 |
| PL3436022T3 (pl) | 2016-04-01 | 2022-08-08 | Sage Therapeutics, Inc. | Oksysterole i sposoby ich stosowania |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| EP3919502A1 (en) | 2016-07-07 | 2021-12-08 | Sage Therapeutics, Inc. | 11-substituted 24-hydroxysterols for use in the treatment of nmda related conditions |
| MA46351A (fr) | 2016-09-30 | 2021-06-02 | Sage Therapeutics Inc | Oxystérols substitués en c7 et procédés en tant que modulateurs nmda |
| WO2018075698A1 (en) | 2016-10-18 | 2018-04-26 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| MA46566A (fr) | 2016-10-18 | 2019-08-28 | Sage Therapeutics Inc | Oxystérols et leurs procédés d'utilisation |
| US11458146B2 (en) | 2017-01-13 | 2022-10-04 | Duke University | Compositions and methods for the treatment of myelin related and inflammation related diseases or disorders |
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| CN113667734B (zh) * | 2021-07-16 | 2022-05-24 | 四川大学华西医院 | Shank3片段序列甲基化检测试剂在制备精神分裂症诊断试剂盒中的用途 |
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