HRP20211282T1 - Oksisteroli i postupci njihovog korištenja - Google Patents
Oksisteroli i postupci njihovog korištenja Download PDFInfo
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- HRP20211282T1 HRP20211282T1 HRP20211282TT HRP20211282T HRP20211282T1 HR P20211282 T1 HRP20211282 T1 HR P20211282T1 HR P20211282T T HRP20211282T T HR P20211282TT HR P20211282 T HRP20211282 T HR P20211282T HR P20211282 T1 HRP20211282 T1 HR P20211282T1
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- 238000000034 method Methods 0.000 title claims 6
- 150000001875 compounds Chemical class 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 230000002496 gastric effect Effects 0.000 claims 3
- 208000014617 hemorrhoid Diseases 0.000 claims 3
- 208000016583 Anus disease Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease 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
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 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
- 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
- 206010028980 Neoplasm 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
- 208000006289 Rett Syndrome 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
- 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
- 206010042458 Suicidal ideation Diseases 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 208000026911 Tuberous sclerosis complex 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
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 208000029560 autism spectrum disease Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 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
- 239000001257 hydrogen Substances 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 206010022437 insomnia Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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
- 239000001301 oxygen Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 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
- 230000002265 prevention Effects 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
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 208000005809 status epilepticus Diseases 0.000 claims 1
- 201000009032 substance abuse Diseases 0.000 claims 1
- 231100000736 substance abuse Toxicity 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 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
-
- 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
-
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- 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
-
- A—HUMAN NECESSITIES
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- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- 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
- C07J41/0061—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 one of the carbon atoms being part of an amide group
-
- 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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Anesthesiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (13)
1. Spoj formule (I):
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time:
R1 je supstituirani ili nesupstituirani C1-6 alkil;
R2 je karbociklil ili heterociklil;
R5 je odsutan ili je vodik; i
[image]
predstavlja jednostruku ili dvostruku vezu, naznačen time da kada je jedno
[image]
dvostruka veza, drugo
[image]
je jednostruka veza
i R5 je odsutan;
naznačen time da je svaka instanca alkil grupe neovisno nesupstituirana ili supstituirana jednim ili više supstituenata.
2. Spoj prema patentnom zahtjevu 1, naznačen time da je R1 supstituirani C1-6 alkil; R1 je nesupstituirani C1-6 alkil; R1 je -CH3, -CF3 -CH2OCH3, ili -CH(CH3)(CF3), etil ili izopropil; ili R1 je metil ili etil.
3. Spoj prema patentnom zahtjevu 1, naznačen time da je R2 ciklopropil, ciklobutil, ciklopentil, cikloheksil; ili R2 je heterociklična grupa sa kisikom (na primjer, tetrahidropiran).
4. Spoj prema patentom zahtjevu 1, naznačen time da
[image]
4. predstavlja jednostruku vezu.
5. Spoj prema patentnom zahtjevu 1, naznačen time da je spoj Formule (I), spoj Formule (I-A) ili Formule (I-B):
[image]
6. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj Formule (I), spoj Formule (V):
[image]
ili njegova farmaceutski prihvatljiva sol; ili spoj Formule (V-A) ili Formule (V-B):
[image]
ili njihova farmaceutski prihvatljiva sol.
7. Spoj prema patentnom zahtjevu 1, naznačen time da je spoj Formule (I) izabrano između:
[image]
[image]
[image]
[image]
ili njihovih farmaceutski prihvatljivih soli.
8. Farmaceutska kompozicija koja sadrži spoj prema zahtjevu 1 ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv nosač.
9. Spoj prema patentnom zahtjevu 1, za primjenu u terapiji ili kao lijek.
10. Spoj prema zahtjevu 1, za primjenu u postupku izazivanja sedacije ili anestezije, naznačen time da postupak obuhvaća davanje subjektu efikasne količine spoja prema zahtjevu 1, ili njegove farmaceutski prihvatljive soli, ili njegove farmaceutske kompozicije.
11. Spoj prema patentnom zahtjevu 1, za primjenu u postupku liječenja ili sprečavanja poremećaja, naznačen time da je poremećaj gastrointestinalni (GI) poremećaj, na primjer, konstipacija, sindrom iritabilnog crijeva (IBS), upalna bolest crijeva (IBD) (na primjer, ulcerozni kolitis, Kronova bolest), strukturni poremećaji koji utječu na GI, analni poremećaji (na primjer, hemoroidi, unutrašnji hemoroidi, vanjski hemoroidi, analne pukotine, perianalni apscesi, analna fistula), polipi debelog crijeva, rak, kolitis, dijabetes ili poremećaj sinteze sterola, pri čemu se postupak sastoji od davanja subjektu kojem je potrebno liječenje, efikasne količine spoja prema patentnom zahtjevu 1, ili njegove farmaceutski prihvatljive soli, ili farmaceutske kompozicije.
12. Spoj prema patentnom zahtjevu 1, za primjenu u postupku liječenja ili sprečavanja stanja povezanih sa CNS-om, pri čemu postupak koji obuhvaća davanje subjektu kojem je potrebno liječenje, efikasne količine spoja prema patentnom zahtjevu 1, ili njegove farmaceutski prihvatljive soli ili njegove farmaceutske kompozicije.
13. Spoj za primjenu prema patentnom zahtjevu 12, naznačen time što je stanje povezano sa CNS, poremećaj prilagođavanja, anksiozni poremećaj (uključujući opsesivno-kompulzivni poremećaj, post-traumatski stresni poremećaj i socijalnu fobiju), kognitivni poremećaj (uključujući Alzheimerovu bolest i druge oblike demencije), disocijativni poremećaj, poremećaj prehrane, poremećaji raspoloženja (uključujući depresiju (na primjer, postporođajnu depresiju), bipolarni poremećaj, distimični poremećaj, suicidne težnje), šizofrenija ili drugi psihotični poremećaji (uključujući shizoafektivni poremećaj), poremećaj spavanja (uključujući nesanicu), poremećaje zloupotrebe supstanci, poremećaj ličnosti (uključujući opsesivno-kompulzivni poremećaj ličnosti), autistični spektar poremećaja (uključujući povezane sa mutacijama u Shank grupi proteina (na primjer, Shank3)), neurorazvojni poremećaji (uključujući Rettov sindrom, kompleks tuberozne skleroze), multipla skleroza, poremećaji sinteze sterola, bol (uključujući akutnu i kroničnu bol), encefalopatija kao posljedica medicinskog stanja (uključujući jetrenu encefalopatiju i encefalitis anti-NMDA receptora), epilepsija (uključujući status epilepticus i monogenske oblike epilepsije, poput Dravetove bolesti), moždani udar, traumatska povrede mozga, poremećaji kretanja (uključujući Huntingtonovu bolest i Parkinsonovu bolest), oštećenje vida, gubitak sluha, i tinitus.
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