HRP20192044T1 - Agonisti i pripravci 5-ht2c receptora i metode uporabe - Google Patents

Agonisti i pripravci 5-ht2c receptora i metode uporabe Download PDF

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Publication number
HRP20192044T1
HRP20192044T1 HRP20192044TT HRP20192044T HRP20192044T1 HR P20192044 T1 HRP20192044 T1 HR P20192044T1 HR P20192044T T HRP20192044T T HR P20192044TT HR P20192044 T HRP20192044 T HR P20192044T HR P20192044 T1 HRP20192044 T1 HR P20192044T1
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Croatia
Prior art keywords
compound
individual
preparation
diazepino
difluoroethyl
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HRP20192044TT
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English (en)
Inventor
Albert S. Ren
Graeme Semple
Xiuwen Zhu
Carleton R. Sage
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Arena Pharmaceuticals, Inc.
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Application filed by Arena Pharmaceuticals, Inc. filed Critical Arena Pharmaceuticals, Inc.
Publication of HRP20192044T1 publication Critical patent/HRP20192044T1/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
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06Peri-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (24)

1. Spoj odabran između sljedećih spojeva, i njihovih farmaceutski prihvatljivih soli, hidrata i solvata: N-(2,2-difluoroetil)-7-metil-1,2,3,4,6,7-heksahidro-[1,4]diazepino [6,7,1-hi]indol-8-karboksamid (Spoj Br. 1); (S)-N-(2,2-difluoroetil)-7-metil-1,2,3,4,6,7-heksahidro-[1,4]diazepino [6,7,1-hi]indol-8-karboksamid (Spoj Br. 2); (R)-N-(2,2-difluoroetil)-7-metil-1,2,3,4,6,7-heksahidro-[1,4]diazepino [6,7,1-hi]indol-8-karboksamid (Spoj Br. 3); (S)-N-(2,2-difluoroetil)-7-etil-1,2,3,4,6,7-heksahidro-[1,4]diazepino [6,7,1-hi]indol-8-karboksamid (Spoj Br. 4); (R)-N-(2,2-difluoroetil)-7-etil-1,2,3,4,6,7-heksahidro-[1,4]diazepino [6,7,1-hi]indol-8-karboksamid (Spoj Br. 5); N-(2,2-difluoroetil)-7,7-dimetil-1,2,3,4,6,7-heksahidro-[1,4]diazepino [6,7,1-hi]indol-8-karboksamid (Spoj Br. 6); N-(2,2-difluoroetil)-2,3,4,6-tetrahidro-1H-spiro[[1,4]diazepino [6,7,1-hi]indol-7,1’-ciklobutan]-8-karboksamid (Spoj Br. 7); (S)-N-(2,2-difluoroetil)-7-(2,2,2-trifluoroetil)-1,2,3,4,6,7-heksahidro-[1,4]diazepino[6,7,1-hi]indol-8-karboksamid (Spoj Br. 8); i (R)-N-(2,2-difluoroetil)-7-(2,2,2-trifluoroetil)-1,2,3,4,6,7-heksahidro-[1,4]diazepino[6,7,1-hi]indol-8-karboksamid (Spoj Br. 9).
2. Spoj sukladno zahtjevu 1 pri čemu je spoj (R)-N-(2,2-difluoroetil)-7-metil-1,2,3,4,6,7-heksahidro-[1,4]diazepino[6,7,1-hi]indol-8-karboksamid (Spoj Br. 3) ili farmaceutski prihvatljiva sol, hidrat ili solvat istih.
3. Farmaceutski pripravak koji obuhvaća spoj sukladno zahtjevu 1 ili zahtjevu 2 i i farmaceutski prihvatljiv nosač.
4. Postupak za pripremu farmaceutskog pripravka, naznačen time da sadrži miješanje spoja iz zahtjeva 1 ili zahtjeva 2 i farmaceutski prihvatljivog nosača.
5. Spoj sukladno zahtjevu 1 ili zahtjevu 2 ili pripravak sukladno zahtjevu 3 za uporabu u postupku liječenja ljudskog ili životinjskog tijela terapijom.
6. Spoj sukladno zahtjevu 1 ili zahtjevu 2 ili pripravak sukladno zahtjevu 3 za uporabu u postupku vezanom za: smanjenje učestalosti pušenja duhana kod pojedinca koji pokušava smanjiti učestalost pušenja duhana; pomaganje u prestanku ili smanjenju uporabe duhanskih proizvoda kod pojedinca koji pokušava prestati ili smanjiti uporabu duhanskog proizvoda; pomoć pri prestanku pušenja i sprečavanju povezanog debljanja; kontroliranje debljanja povezano s prestankom pušenja od strane pojedinca koji pokušava prestati pušiti duhan; smanjenje debljanja povezano s prestankom pušenja od strane pojedinca koji pokušava prestati pušiti duhan; liječenje nikotinske ovisnosti, ovisnosti i/ili prestanka uporabe kod pojedinca koji pokušava liječiti ovisnost o nikotinu, ovisnost i/ili prestanak uporabe; ili smanjenje vjerojatnosti ponovne uporabe nikotina kod pojedinca koji pokušava prekinuti uzimanje nikotina.
7. Spoj ili pripravak za upotrebu u skladu s patentnim zahtjevom 6, pri čemu metoda uključuje: odabir pojedinca s početnim BMI ≥ 27 kg/m2; i propisivanje i/ili davanje pojedincu učinkovite količine spoja ili pripravka u trajanju od barem jedne godine.
8. Spoj ili pripravak za uporabu sukladno zahtjevu 6, pri čemu postupak obuhvaća: davanje spoja ili pripravka pojedincu; nadziranje pojedinčeva BMI tijekom primjene; i prekidanje primjene ako BMI pojedinca postane < 18.5 kg/m2 tijekom primjene.
9. Spoj ili pripravak za uporabu sukladno zahtjevu 6, pri čemu postupak obuhvaća: davanje spoja ili pripravka pojedincu s inicijalnim BMI ≤ 25 kg/m2; nadziranje tjelesne težine pojedinca tijekom primjene; i prekid navedenog davanja ako se tjelesna težina pojedinca smanji za više od oko 1% tijekom primjene.
10. Spoj ili pripravak za uporabu sukladno zahtjevu 6, pri čemu postupak obuhvaća: nadziranje tjelesne težine pojedinca tijekom primjene; i prekid navedenog davanja ako se tjelesna težina pojedinca smanji za više od 1 kg tijekom primjene.
11. Spoj ili pripravak za uporabu sukladno zahtjevima 6 do 10, pri čemu se pojedincu također propisuje i/ili daje dodatno sredstvo.
12. Spoj sukladno zahtjevu 1 ili zahtjevu 2 ili pripravak sukladno zahtjevu 3, naznačen time, da se upotrebljava u postupku za smanjenje unosa hrane kod pojedinca.
13. Spoj iz zahtjeva 1 ili zahtjeva 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku indukcije sitosti kod pojedinca.
14. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku liječenja pretilosti kod pojedinca.
15. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku prevencije pretilosti kod pojedinca.
16. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku nadzora tjelesne težine kod pojedinca.
17. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku liječenja dijabetesa tipa 2 kod pojedinca.
18. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku prevencije dijabetesa tipa 2 kod pojedinca.
19. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku liječenja ovisnosti kod pojedinca.
20. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku liječenja ovisnosti o alkoholu kod pojedinca.
21. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku liječenja poremećaja vezanog uz napadaje kod pojedinca.
22. Spoj ili pripravak za uporabu u skladu s patentnim zahtjevom 21, naznačen time što navedeni poremećaj vezan uz napadaje je epilepsija.
23. Spoj ili pripravak za uporabu u skladu s patentnim zahtjevom 21, naznačen time što navedeni poremećaj vezan uz napadaje je Dravet sindrom.
24. Spoj prema zahtjevu 1 ili zahtjevu 2 ili pripravak iz zahtjeva 3, naznačen time, da se upotrebljava u postupku liječenja poremećaja urinarne inkontinencije.
HRP20192044TT 2015-04-27 2019-11-12 Agonisti i pripravci 5-ht2c receptora i metode uporabe HRP20192044T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562153082P 2015-04-27 2015-04-27
EP16721320.6A EP3288946B1 (en) 2015-04-27 2016-04-26 5-ht2c receptor agonists and compositions and methods of use
PCT/US2016/029308 WO2016176177A1 (en) 2015-04-27 2016-04-26 5-ht2c receptor agonists and compositions and methods of use

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HRP20192044T1 true HRP20192044T1 (hr) 2020-02-07

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US (1) US10392390B2 (hr)
EP (1) EP3288946B1 (hr)
JP (1) JP6675688B2 (hr)
KR (1) KR102275505B1 (hr)
CN (1) CN107873030B (hr)
AU (1) AU2016255009B2 (hr)
BR (1) BR112017023088B1 (hr)
CA (1) CA3002544C (hr)
DK (1) DK3288946T3 (hr)
EA (1) EA034446B1 (hr)
ES (1) ES2757922T3 (hr)
HK (1) HK1244005B (hr)
HR (1) HRP20192044T1 (hr)
HU (1) HUE047169T2 (hr)
IL (1) IL255171A0 (hr)
MX (2) MX2017013902A (hr)
PT (1) PT3288946T (hr)
WO (1) WO2016176177A1 (hr)

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US20210052600A1 (en) 2017-12-27 2021-02-25 Takeda Pharmaceutical Company Limited Therapeutic agents for stress urinary incontinence and incotinence of feces
WO2019152475A1 (en) 2018-01-30 2019-08-08 Apnimed, Inc. (Delaware) Methods and compositions for treating sleep apnea
CN113692277A (zh) * 2019-02-08 2021-11-23 布里格姆妇女医院 用于治疗睡眠呼吸暂停的方法和组合物
JP2022529781A (ja) 2019-04-17 2022-06-24 コンパス パスファインダー リミテッド サイロシビンによるうつ病及び他の様々な障害の治療
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US20230293546A1 (en) * 2022-03-10 2023-09-21 Arena Pharmaceuticals, Inc. Methods of treatment
WO2023225773A1 (en) * 2022-05-23 2023-11-30 Sensorium Therapeutics, Inc. Solid forms of mesembrine and therapeutic uses thereof

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BR112017023088A2 (pt) 2018-07-10
KR20170140317A (ko) 2017-12-20
BR112017023088B1 (pt) 2023-10-03
WO2016176177A1 (en) 2016-11-03
DK3288946T3 (da) 2019-11-25
CA3002544C (en) 2024-03-05
EA034446B1 (ru) 2020-02-10
JP6675688B2 (ja) 2020-04-01
US20180186797A1 (en) 2018-07-05
HK1244005B (zh) 2020-04-17
ES2757922T3 (es) 2020-04-30
EA201792356A1 (ru) 2018-05-31
MX2020005898A (es) 2020-08-13
IL255171A0 (en) 2017-12-31
PT3288946T (pt) 2019-11-27
NZ737412A (en) 2021-06-25
JP2018519251A (ja) 2018-07-19
CN107873030A (zh) 2018-04-03
HUE047169T2 (hu) 2020-04-28
AU2016255009B2 (en) 2020-10-08
KR102275505B1 (ko) 2021-07-08
CN107873030B (zh) 2021-03-19
EP3288946B1 (en) 2019-08-21
AU2016255009A1 (en) 2017-12-14
MX2017013902A (es) 2018-03-16
EP3288946A1 (en) 2018-03-07
CA3002544A1 (en) 2016-11-03
US10392390B2 (en) 2019-08-27

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