HRP20192341T1 - 3.alfa.-etinil, 3.beta.-hidroksi-5.alfa.-pregnan-20-oksim za upotrebu u liječenju poremećaja cns - Google Patents

3.alfa.-etinil, 3.beta.-hidroksi-5.alfa.-pregnan-20-oksim za upotrebu u liječenju poremećaja cns Download PDF

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Publication number
HRP20192341T1
HRP20192341T1 HRP20192341TT HRP20192341T HRP20192341T1 HR P20192341 T1 HRP20192341 T1 HR P20192341T1 HR P20192341T T HRP20192341T T HR P20192341TT HR P20192341 T HRP20192341 T HR P20192341T HR P20192341 T1 HRP20192341 T1 HR P20192341T1
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Croatia
Prior art keywords
compound
pharmaceutically acceptable
alpha
diluent
steroid
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HRP20192341TT
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English (en)
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Torbjörn BÄCKSTRÖM
Gianna Ragagnin
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Umecrine Cognition Ab
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Publication of HRP20192341T1 publication Critical patent/HRP20192341T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/32Oximes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005Normal 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 only two carbon atoms, e.g. pregnane derivatives
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Anesthesiology (AREA)
  • Diabetes (AREA)
  • Toxicology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (14)

1. 3α-etinil, 3β-hidroksi, 5α-pregnan-20-oksim ili njegova farmaceutski prihvatljiva sol.
2. Farmaceutska formulacija koja obuhvaća spojeve kao što je definirano u patentnom zahtjevu 1, u mješavini s farmaceutski prihvatljivim pomoćnim sredstvom, razrjeđivačem ili nosačem.
3. Spoj kako je definiran u patentnom zahtjevu 1, za upotrebu u terapiji.
4. Spoj kako je definiran u patentnom zahtjevu 1, za upotrebu u postupku liječenja: (a) poremećaja CNS povezanog sa steroidom; (b) stanja ili simptoma uzrokovanih razvijanjem tolerancije nakon izlaganja 3-alfa-hidroksi-5-alfa/beta-steroidima; (c) stanja koje je pod utjecajem odvikavanja/apstinencije izlaganja 3-alfa-hidroksi-5-alfa/beta-steroidima; (d) jedne ili više nuspojave anti-inflamatornog steroida; (e) jedne ili više nuspojave postmenopauzalne terapije; i/ili (f) jedne ili više nuspojave oralnog kontraceptiva.
5. Spoj za upotrebu prema patentnom zahtjevu 4, gdje poremećaj CNS povezan sa steroidom je izabran iz grupe koju čine epilepsija, epilepsija ovisna o menstrualnom ciklusu, depresija, depresija povezana sa stresom, migrena, umor i posebno umor koji je povezan sa stresom, predmenstrualni sindrom, predmenstrualni disforični poremećaj, promjene raspoloženja povezane sa menstrualnim ciklusom, minimalno kognitivno oštećenje, kognitivno oštećenje, promjene u memoriji povezane s menstrualnim ciklusom, promjene u memoriji povezane sa stresom, poteškoće u učenju povezane sa stresom, hepatička encefalopatija, Downov sindrom, Alzheimerova bolest, poteškoće u koncentraciji povezane s menstrualnim ciklusom, poremećaji spavanja povezani s menstrualnim ciklusom i umorom, povećan apetit, prejedanje i pretilost, relaps zloupotrebe alkohola i opojnih sredstava, poremećaji ravnoteže, ’moment’ poremećaji i poteškoće u koordinaciji.
6. Spoj za upotrebu prema patentnom zahtjevu 5, gdje poremećaj je hepatička encefalopatija.
7. Spoj za upotrebu prema patentnom zahtjevu 6, gdje hepatička encefalopatija je Tip A hepatičke encefalopatije, Tip B hepatičke encefalopatije, Tip C hepatičke encefalopatije, minimalna hepatička encefalopatija, ili otvorena hepatička encefalopatija.
8. Spoj za upotrebu kao što je navedeno u patentnom zahtjevu 5, gdje je poremećaj Downov sindrom ili Alzheimerova bolest.
9. Kombinirani proizvod koji obuhvaća: (A) spoj kao što je definirano u patentnom zahtjevu 1; i (B) bar jedno drugo terapeutsko sredstvo koje je korisno u liječenju poremećaja CNS povezanog sa steroidom, pri čemu svaka od komponenti (A) i (B) je formulirana u mješavini s farmaceutski prihvatljivim pomoćnim sredstvom, razrjeđivačem ili nosačem.
10. Kombinirani proizvod kao što je navedeno u patentnom zahtjevu 9 koji obuhvaća farmaceutsku formulaciju uključujući spoj kao što je definirano u patentnom zahtjevu 1, bar jedno drugo farmaceutsko sredstvo koje je korisno u liječenju poremećaja CNS povezanog sa steroidom, i farmaceutski prihvatljivo pomoćno sredstvo, razrjeđivač ili nosač.
11. Kombinirani proizvod kao što je definirano u patentnom zahtjevu 9, koji obuhvaća komplet dijelova koji sadrže komponente: (a) farmaceutska formulacija koja obuhvaća spoj formule I kao što je definirano u patentnom zahtjevu 1, u mješavini s farmaceutski prihvatljivim pomoćnim sredstvom, razrjeđivačem ili nosačem; i (b) farmaceutska formulacija koja obuhvaća bar jedno drugo terapeutsko sredstvo koje je korisno u liječenju poremećaja CNS povezanog sa steroidom u mješavini s farmaceutski prihvatljivim pomoćnim sredstvom, nosačem ili razrjeđivačem, gdje komponente (a) i (b) su svaka dana u obliku koji je pogodan za davanje zajedno sa drugim.
12. Postupak za dobivanje spoja formule I kao što je definirano u patentnom zahtjevu 1, gdje proces obuhvaća reakciju 3α-etinil, 3β-hidroksi, 5α-pregnan-20-ona sa hidroksilaminom.
13. Postupak za dobivanje farmaceutske formulacije kao što je definirano u patentnom zahtjevu 2, gdje postupak obuhvaća dovođenje u vezu spoja kao što je definirano u patentnom zahtjevu 1 s farmaceutski prihvatljivim pomoćnim sredstvom, razrjeđivačem ili nosačem.
14. Postupak za dobivanje kombiniranog proizvoda kako je definirano u bilo kojem od patentnih zahtjeva 9 do 11, gdje postupak obuhvaća dovođenje u vezu spoja kao što je definirano u patentnom zahtjevu 1 s drugim terapeutskim sredstvom koje je korisno u liječenju poremećaja CNS povezanog sa steroidom, i bar jednim farmaceutski prihvatljivim pomoćnim sredstvom, razrjeđivačem ili nosačem.
HRP20192341TT 2015-01-12 2019-12-30 3.alfa.-etinil, 3.beta.-hidroksi-5.alfa.-pregnan-20-oksim za upotrebu u liječenju poremećaja cns HRP20192341T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE1500018 2015-01-12
PCT/GB2016/050059 WO2016113549A1 (en) 2015-01-12 2016-01-11 3.alpha.-ethynyl, 3.beta.-hydroxy-5.alpha.-pregnan-20-oxime for use in the treatment of cns disorders
EP16704468.4A EP3245217B1 (en) 2015-01-12 2016-01-11 3.alpha.-ethynyl, 3.beta.-hydroxy-5.alpha.-pregnan-20-oxime for use in the treatment of cns disorders

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HRP20192341T1 true HRP20192341T1 (hr) 2020-04-03

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HRP20192341TT HRP20192341T1 (hr) 2015-01-12 2019-12-30 3.alfa.-etinil, 3.beta.-hidroksi-5.alfa.-pregnan-20-oksim za upotrebu u liječenju poremećaja cns

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US (1) US10351589B2 (hr)
EP (1) EP3245217B1 (hr)
JP (1) JP6712599B2 (hr)
KR (1) KR102534043B1 (hr)
CN (1) CN107207560B (hr)
AR (1) AR103384A1 (hr)
AU (1) AU2016207865B2 (hr)
BR (1) BR112017014733B1 (hr)
CA (1) CA2971302C (hr)
CY (1) CY1122588T1 (hr)
DK (1) DK3245217T3 (hr)
ES (1) ES2764454T3 (hr)
HK (1) HK1244288A1 (hr)
HR (1) HRP20192341T1 (hr)
HU (1) HUE046759T2 (hr)
IL (1) IL253037B (hr)
MX (1) MX2017008953A (hr)
NZ (1) NZ733245A (hr)
PL (1) PL3245217T3 (hr)
PT (1) PT3245217T (hr)
RS (1) RS59736B1 (hr)
RU (1) RU2712786C2 (hr)
SI (1) SI3245217T1 (hr)
TW (1) TWI748936B (hr)
WO (1) WO2016113549A1 (hr)
ZA (1) ZA201704287B (hr)

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Publication number Publication date
KR20170097673A (ko) 2017-08-28
CN107207560B (zh) 2020-06-16
BR112017014733B1 (pt) 2023-04-25
PT3245217T (pt) 2020-01-14
HUE046759T2 (hu) 2020-03-30
NZ733245A (en) 2024-01-26
JP2018501290A (ja) 2018-01-18
BR112017014733A2 (pt) 2018-01-09
ES2764454T3 (es) 2020-06-03
US20170369522A1 (en) 2017-12-28
HK1244288A1 (zh) 2018-08-03
CA2971302C (en) 2023-06-27
RU2017126160A (ru) 2019-02-14
AU2016207865B2 (en) 2020-07-02
AU2016207865A1 (en) 2017-07-13
KR102534043B1 (ko) 2023-05-17
PL3245217T3 (pl) 2021-07-19
EP3245217B1 (en) 2019-10-02
CY1122588T1 (el) 2021-01-27
TWI748936B (zh) 2021-12-11
TW201639579A (zh) 2016-11-16
CA2971302A1 (en) 2016-07-21
IL253037B (en) 2020-09-30
AR103384A1 (es) 2017-05-03
DK3245217T3 (da) 2019-12-09
IL253037A0 (en) 2017-08-31
RU2712786C2 (ru) 2020-01-31
WO2016113549A1 (en) 2016-07-21
RU2017126160A3 (hr) 2019-04-11
US10351589B2 (en) 2019-07-16
JP6712599B2 (ja) 2020-06-24
RS59736B1 (sr) 2020-02-28
CN107207560A (zh) 2017-09-26
ZA201704287B (en) 2018-08-29
MX2017008953A (es) 2018-05-04
SI3245217T1 (sl) 2020-02-28
EP3245217A1 (en) 2017-11-22

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