HRP20201262T1 - Kombinacija inverzivnih agonista histamin-3 receptora sa inhibitorima acetilkolinesteraze - Google Patents

Kombinacija inverzivnih agonista histamin-3 receptora sa inhibitorima acetilkolinesteraze Download PDF

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Publication number
HRP20201262T1
HRP20201262T1 HRP20201262TT HRP20201262T HRP20201262T1 HR P20201262 T1 HRP20201262 T1 HR P20201262T1 HR P20201262T T HRP20201262T T HR P20201262TT HR P20201262 T HRP20201262 T HR P20201262T HR P20201262 T1 HRP20201262 T1 HR P20201262T1
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Croatia
Prior art keywords
morpholin
yloxy
phenyl
pharmaceutically acceptable
acetamide
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HRP20201262TT
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English (en)
Inventor
Ramakrishna Nirogi
Anil Karbhari Shinde
Abdul Rasheed Mohammed
Pradeep Jayarajan
Gopinadh Bhyrapuneni
Venkateswarlu Jasti
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Suven Life Sciences Limited
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Publication of HRP20201262T1 publication Critical patent/HRP20201262T1/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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • 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
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (18)

1. Kombinacija koja sadrži inverzni agonist histamin-3 receptora i inhibitor acetilholinesteraze; naznačena time da je inverzni agonist histamin-3 receptora izabran iz grupe koja se sastoji od: N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamida; N-[4-(1-Ciklopropilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamida; i N-[4-(1-Izopropilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamida; ili njihove farmaceutski prihvatljive soli.
2. Kombinacija prema patentnom zahtjevu 1, naznačena time da je inhibitor acetilholinesteraze izabran iz grupe koja se sastoji od donepezila, rivastigmina i galantamina ili njihove farmaceutski prihvatljive soli.
3. Kombinacija prema patentnom zahtjevu 1, naznačena time da inverzni agonist histamin-3 receptora je N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid ili njegova farmaceutski prihvatljiva sol.
4. Kombinacija prema patentnom zahtjevu 1 ili patentnom zahtjevu 3, naznačena time da je farmaceutski prihvatljiva sol inverznog agonista histamin-3 receptora izabrana od N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid dihidrohlorida; N-[4-(1-Ciklopropilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid tartarata; i N-[4-(1-Izopropilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid tartarata.
5. Kombinacija prema patentnom zahtjevu 1, 3 ili 4, naznačena time da inverzni agonist histamin-3 receptora je N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid dihidrohlorid.
6. Kombinacija prema patentnom zahtjevu 1 ili patentnom zahtjevu 2, naznačena time da inhibitor acetilholinesteraze je donepezil ili njegova farmaceutski prihvatljiva sol ili pri čemu, inhibitor acetilholinesteraze je donepezil hidrohlorid.
7. Kombinacija koja sadrži N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid dihidrohlorid i donepezil hidrohlorid.
8. Kombinacija prema bilo kojem od patentnih zahtjeva 1 do 7, za uporabu u liječenju kognitivnih poremećaja kod pacijenta.
9. Kombinacija za uporabu prema patentnom zahtjevu 8, naznačeno time da je kognitivni poremećaj izabran od Alzheimer-ove bolesti, šizofrenije, Parkinson-onove bolesti, demencije sa Lewy-telima, vaskularne demencije, frontotemporalne demencije, Down-ovog sindroma ili Tourette-ovog sindroma.
10. Spoj, N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il) acetamid ili njegova farmaceutski prihvatljiva sol za uporabu u kombinaciji sa inhibitorom acetilholinesteraze za liječenje Alzheimer-ove bolesti kod pacijenta.
11. Spoj za uporabu prema patentnom zahtjevu 10, kao dodatno liječenje kod pacijenta na stabilnom liječenju sa inhibitorom acetilholinesteraze.
12. Spoj za uporabu prema patentnom zahtjevu 10 ili patentnom zahtjevu 11, naznačen time da je inhibitor acetilholinesteraze izabran od donepezila, rivastigmina i galantamina ili njegove farmaceutski prihvatljive soli.
13. Spoj za uporabu prema patentnom zahtjevu 10 ili patentnom zahtjevu 11, (a) naznačeno time da liječenje sadrži primjenu na pacijenta 0.1 mg do 100 mg N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamida ili njegove farmaceutski prihvatljive soli na dan, ili (b) time da liječenje sadrži primjenu na pacijenta 0.1 mg do 60 mg N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid ili njegove farmaceutski prihvatljive soli na dan, ili (c) time da liječenje sadrži primjenu na pacijenta 0.1 mg do 30 mg N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid ili njegove farmaceutski prihvatljive soli na dan; ili (d) time da liječenje sadrži primjenu na pacijenta 1 mg do 30 mg donepezila, ili farmaceutski prihvatljive soli na dan.
14. Farmaceutski pripravak koji sadrži kombinaciju prema bilo kojem od patentnih zahtjeva 1 do 7, i farmaceutski prihvatljive ekscipijente ili njihovu kombinaciju.
15. Farmaceutski pripravak prema patentnom zahtjevu 14, za uporabu u liječenju kognitivnih poremećaja izabranih od Alzheimer-ove bolesti, šizofrenije, Parkinson-onove bolesti, demencije sa Lewy-telima, vaskularne demencije i frontotemporalne demencije.
16. Farmaceutski pripravak prema patentnom zahtjevu 14 ili patentnom zahtjevu 15, (a) naznačen time da N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid ili njegova farmaceutski prihvatljiva sol su prisutni u količini od 0.1 mg do 100 mg, ili (b) time da N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid ili njegova farmaceutski prihvatljiva sol su prisutni u količini od 0.1 mg do 60 mg, ili (c) time da N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamid ili njegova farmaceutski prihvatljiva sol su prisutni u količini od 0.1 mg to 30 mg; ili (d) time da donepezil ili njegova farmaceutski prihvatljiva sol su prisutni u količini od 2 mg do 30 mg.
17. Spoj za uporabu prema patentnom zahtjevu 10, naznačen time da liječenje sadrži primjenu N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamida ili njegove farmaceutski prihvatljive soli na pacijenta oralnim, nazalnim, lokalnim, dermalnim ili parenteralnim putevima.
18. Spoj za uporabu prema patentnom zahtjevu 10, naznačen time da liječenje sadrži primjenu N-[4-(1-Ciklobutilpiperidin-4-iloksi)fenil]-2-(morfolin-4-il)acetamida ili njegove farmaceutski prihvatljive soli na pacijenta jednom do tri puta na dan, jednom do tri puta tjedno ili jednom do tri puta mjesečno.
HRP20201262TT 2016-08-18 2020-08-11 Kombinacija inverzivnih agonista histamin-3 receptora sa inhibitorima acetilkolinesteraze HRP20201262T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN201641028166 2016-08-18
PCT/IB2017/054938 WO2018033847A1 (en) 2016-08-18 2017-08-14 Combination of histamine-3 receptor inverse agonists with acetylcholinesterase inhibitors
EP17768234.1A EP3500253B1 (en) 2016-08-18 2017-08-14 Combination of histamine-3 receptor inverse agonists with acetylcholinesterase inhibitors

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US (1) US10603323B2 (hr)
EP (1) EP3500253B1 (hr)
JP (1) JP6734470B2 (hr)
KR (1) KR102039585B1 (hr)
CN (1) CN109640975B (hr)
AU (1) AU2017313427B2 (hr)
BR (1) BR112019002645A2 (hr)
CA (1) CA3033039C (hr)
CY (1) CY1123238T1 (hr)
DK (1) DK3500253T3 (hr)
EA (1) EA032957B1 (hr)
ES (1) ES2810983T3 (hr)
HR (1) HRP20201262T1 (hr)
HU (1) HUE052003T2 (hr)
IL (1) IL264406B (hr)
LT (1) LT3500253T (hr)
MA (1) MA45990B1 (hr)
MD (1) MD3500253T2 (hr)
ME (1) ME03812B (hr)
MX (1) MX2019001696A (hr)
NZ (1) NZ750150A (hr)
PL (1) PL3500253T3 (hr)
PT (1) PT3500253T (hr)
RS (1) RS60669B1 (hr)
SG (1) SG11201900681SA (hr)
SI (1) SI3500253T1 (hr)
WO (1) WO2018033847A1 (hr)
ZA (1) ZA201900467B (hr)

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WO2019229509A1 (en) * 2018-05-31 2019-12-05 Suven Life Sciences Limited Method of treatment with histamine-3 receptor inverse agonist

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KR20120035183A (ko) * 2009-06-10 2012-04-13 선오비온 파마슈티컬스 인코포레이티드 히스타민 h3 역 작용제 및 길항제, 및 이의 사용 방법
CN103443093B (zh) * 2011-02-23 2015-02-25 苏文生命科学有限公司 作为组胺h3受体配体的化合物
FR2974729B1 (fr) 2011-05-02 2013-04-19 Servier Lab Nouvelle association entre le 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1h)-yl]propoxy}benzamide et un inhibiteur de l'acetylcholinesterase et les compositions pharmaceutiques qui la contiennent
HUP1300139A2 (en) * 2013-03-06 2014-09-29 Richter Gedeon Nyrt Phenoxypiperidine h3 antagonists
SG11201601306QA (en) 2013-09-09 2016-03-30 Sanofi Sa An h3 receptor antagonist combined with a cholinesterase inhibitor for use in the treatment of alzheimer's disease

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MD3500253T2 (ro) 2020-09-30
ZA201900467B (en) 2020-06-24
SI3500253T1 (sl) 2020-10-30
NZ750150A (en) 2020-08-28
CA3033039A1 (en) 2018-02-22
DK3500253T3 (da) 2020-08-17
EA201990480A1 (ru) 2019-05-31
MA45990B1 (fr) 2020-08-31
WO2018033847A1 (en) 2018-02-22
MX2019001696A (es) 2019-07-04
KR20190031330A (ko) 2019-03-25
AU2017313427A1 (en) 2019-02-28
RS60669B1 (sr) 2020-09-30
ES2810983T3 (es) 2021-03-10
LT3500253T (lt) 2020-08-25
JP2019524794A (ja) 2019-09-05
CN109640975A (zh) 2019-04-16
EP3500253B1 (en) 2020-06-24
PT3500253T (pt) 2020-08-05
MA45990A (fr) 2019-06-26
BR112019002645A2 (pt) 2019-05-28
ME03812B (me) 2021-04-20
IL264406A (en) 2019-02-28
SG11201900681SA (en) 2019-02-27
US20190160075A1 (en) 2019-05-30
EA032957B1 (ru) 2019-08-30
HUE052003T2 (hu) 2021-04-28
US10603323B2 (en) 2020-03-31
IL264406B (en) 2019-07-31
CN109640975B (zh) 2020-10-20
CY1123238T1 (el) 2021-10-29
JP6734470B2 (ja) 2020-08-05
EP3500253A1 (en) 2019-06-26
PL3500253T3 (pl) 2020-11-16
KR102039585B1 (ko) 2019-11-01
AU2017313427B2 (en) 2020-01-30
CA3033039C (en) 2020-06-23

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