HRP20200872T1 - Kombinacija čistih antagonista 5-ht6 receptora sa inhibitorima acetilholinesteraze - Google Patents

Kombinacija čistih antagonista 5-ht6 receptora sa inhibitorima acetilholinesteraze Download PDF

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HRP20200872T1
HRP20200872T1 HRP20200872TT HRP20200872T HRP20200872T1 HR P20200872 T1 HRP20200872 T1 HR P20200872T1 HR P20200872T T HRP20200872T T HR P20200872TT HR P20200872 T HRP20200872 T HR P20200872T HR P20200872 T1 HRP20200872 T1 HR P20200872T1
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methyl
piperazinyl
sulfonyl
methoxy
indole
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HRP20200872TT
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Ramakrishna Nirogi
Anil Karbhari Shinde
Pradeep Jayarajan
Gopinadh Bhyrapuneni
Ramasastri Kambhampati
Venkateswarlu Jasti
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Suven Life Sciences Limited
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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
    • 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
    • A61K31/28Compounds containing heavy metals
    • A61K31/305Mercury compounds
    • A61K31/31Mercury compounds containing nitrogen
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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)
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  • Chemical & Material Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
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  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)

Claims (17)

1. Kombinacija, naznačena time, što sadrži čisti antagonist 5-HT6 receptora i inhibitor acetilkolinesteraze; pri čemu: čisti antagonist 5-HT6 receptora se bira između 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola; 1-[(4-fluorofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola; i 1-[(4-izopropilfenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola; ili farmaceutski prihvatljive soli istog.
2. Kombinacija kako je navedeno u patentnom zahtjevu 1, naznačena time, što je čisti antagonist 5-HT6 receptora 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indol ili njegova farmaceutski prihvatljiva sol.
3. Kombinacija kako je navedeno u patentnom zahtjevu 1 ili patentnom zahtjevu 2, naznačena time, što se farmaceutski prihvatljiva sol čistog antagonista 5-HT6 receptora bira između 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indol dimezilat monohidrata; 1-[(4-fluorofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indol dihidroklorida; i 1-[(4-izopropilfenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indol dihidroklorida.
4. Kombinacija kako je navedeno u patentnom zahtjevu 1, naznačena time, što se inhibitor acetilkolinesteraze bira između donepezila, galantamina i rivastigmina ili farmaceutski prihvatljive soli istog.
5. Kombinacija kako je navedeno u patentnom zahtjevu 1 ili patentnom zahtjevu 4, naznačena time, što se inhibitor acetilkolinesteraze bira između donepezila i rivastigmina ili farmaceutski prihvatljive soli istog ili je inhibitor acetilkolinesteraze ili njegova farmaceutski prihvatljiva sol donepezil hidroklorid.
6. Kombinacija kako je navedeno u bilo kojem od patentnih zahtjeva 1 do 5, za upotrebu u liječenju kognitivnih poremećaja kod pacijenta, poželjno pri čemu se kognitivni poremećaj bira između Alzheimerove bolesti, šizofrenije, Parkinsonove bolesti, demencije sa Lewyjevim tijelima, vaskularne demencije i frontotemporalne demencije.
7. Spoj 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indol ili njegova farmaceutski prihvatljiva sol za upotrebu u kombinaciji sa inhibitorom acetilkolinesteraze za liječenje Alzheimerove bolesti kod pacijenta.
8. Spoj za upotrebu prema patentnom zahtjevu 7, kao dodatno liječenje kod pacijenta koji je na stabilnom liječenju inhibitorom acetilkolinesteraze.
9. Spoj za upotrebu kako je navedeno u patentnom zahtjevu 7 ili patentnom zahtjevu 8, naznačen time, što se inhibitor acetilkolinesteraze bira između donepezila, galantamina i rivastigmina ili farmaceutski prihvatljive soli istog, ili je inhibitor acetilkolinesteraze donepezil i rivastigmin ili farmaceutski prihvatljiva sol istog.
10. Spoj za upotrebu kako je navedeno u patentnom zahtjevu 7 ili patentnom zahtjevu 8, naznačen time, što je 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indol ili njegova farmaceutski prihvatljiva sol 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indol dimezilat monohidrat.
11. Spoj za upotrebu kako je navedeno u patentnom zahtjevu 9, naznačen time, što liječenje uključuje primjenu kod pacijenta: (a) 1 mg do 200 mg 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola ili njegove farmaceutski prihvatljive soli na dan; ili (b) gdje liječenje uključuje primjenu kod pacijenta 1 mg do 10 mg 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola ili njegove farmaceutski prihvatljive soli na dan; ili (c) gdje liječenje uključuje primjenu kod pacijenta 25 mg do 125 mg 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola ili njegove farmaceutski prihvatljive soli na dan; ili (d) gdje liječenje uključuje primjenu kod pacijenta 150 mg do 200 mg 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola ili njegove farmaceutski prihvatljive soli na dan; ili (e) gdje liječenje uključuje primjenu kod pacijenta 25 mg do 75 mg 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola ili njegove farmaceutski prihvatljive soli na dan; ili (f) gdje liječenje uključuje primjenu kod pacijenta 75 mg do 150 mg 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola ili njegove farmaceutski prihvatljive soli na dan; ili (g) gdje liječenje uključuje primjenu kod pacijenta 1 mg do 30 mg donepezila ili njegove farmaceutski prihvatljive soli na dan, ili (h) gdje liječenje uključuje primjenu kod pacijenta 5 mg do 25 mg donepezila ili njegove farmaceutski prihvatljive soli na dan, ili (i) gdje liječenje uključuje primjenu kod pacijenta 10 mg do 25 mg donepezila ili njegove farmaceutski prihvatljive soli na dan.
12. Farmaceutski pripravak, naznačen time, što uključuje kombinaciju kako je navedeno u bilo kojem od patentnih zahtjeva 1 do 5, i farmaceutski prihvatljive ekscipijente ili kombinaciju istog.
13. Farmaceutski pripravak kako je navedeno u patentnom zahtjevu 12, za upotrebu u liječenju kognitivnih poremećaja koji se biraju između Alzheimerove bolesti, šizofrenije, Parkinsonove bolesti, demencije sa Lewyjevim tijelima, vaskularne demencije i frontotemporalne demencije.
14. Farmaceutski pripravak kako je navedeno u patentnom zahtjevu 12 ili patentnom zahtjevu 13, naznačen time, što su 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indol ili njegova farmaceutski prihvatljiva sol prisutni: (a) u količini od 1 mg do 300 mg, ili (b) u količini od 35 mg do 200 mg, ili (c) u količini od 200 mg do 300 mg, ili (d) u količini od 75 mg ili 150 mg.
15. Farmaceutski pripravak kako je navedeno u patentnom zahtjevu 12 ili patentnom zahtjevu 13, naznačen time, što su donepezil ili njegova farmaceutski prihvatljiva sol prisutni u količini od: (a) 2 mg do 30 mg, ili (b) količini od 5 mg do 25 mg, ili (c) u količini od 5 mg, ili (d) u količini od 10 mg, ili (e) u količini od 23 mg.
16. Spoj za upotrebu kako je navedeno u patentnom zahtjevu 7, naznačen time, što liječenje uključuje primjenu 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola ili njegove farmaceutski prihvatljive soli kod pacijenta oralnim, nazalnim, lokalnim, dermalnim ili parenteralnim putem.
17. Spoj za upotrebu kako je navedeno u patentnom zahtjevu 7, naznačen time, što liječenje uključuje primjenu 1-[(2-bromofenil)sulfonil]-5-metoksi-3-[(4-metil-1-piperazinil)metil]-1H-indola ili njegove farmaceutski prihvatljive soli kod pacijenta jednom do tri puta dnevno, jednom do tri puta tjedno ili jednom do tri puta mjesečno.
HRP20200872TT 2016-05-18 2020-06-02 Kombinacija čistih antagonista 5-ht6 receptora sa inhibitorima acetilholinesteraze HRP20200872T1 (hr)

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IN201641017205 2016-05-18
EP16766622.1A EP3484467B1 (en) 2016-05-18 2016-08-03 Combination of pure 5-ht6 receptor antagonists with acetylcholinesterase inhibitors
PCT/IB2016/054673 WO2017199071A1 (en) 2016-05-18 2016-08-03 Combination of pure 5-ht6 receptor antagonists with acetylcholinesterase inhibitors

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US (1) US11458135B2 (hr)
EP (1) EP3484467B1 (hr)
JP (1) JP6606299B2 (hr)
KR (1) KR102015484B1 (hr)
CN (2) CN114642667A (hr)
AU (1) AU2016407427B2 (hr)
BR (1) BR112018073419A2 (hr)
CA (1) CA3023819C (hr)
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EA (1) EA036347B1 (hr)
ES (1) ES2796181T3 (hr)
HR (1) HRP20200872T1 (hr)
HU (1) HUE050819T2 (hr)
IL (1) IL262921B (hr)
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MA (1) MA45639B1 (hr)
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ME (1) ME03731B (hr)
MX (1) MX2018014185A (hr)
NZ (1) NZ748280A (hr)
PL (1) PL3484467T3 (hr)
PT (1) PT3484467T (hr)
RS (1) RS60422B1 (hr)
SG (1) SG11201809856SA (hr)
SI (1) SI3484467T1 (hr)
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CN111084768A (zh) * 2018-10-24 2020-05-01 中国科学院昆明动物研究所 吉非罗齐及其衍生物用于治疗和/或预防神经退行性疾病的用途
CN111084776A (zh) * 2018-10-24 2020-05-01 中国科学院昆明动物研究所 匹立尼酸及其衍生物用于治疗和/或预防神经退行性疾病的用途
JP2023506724A (ja) * 2019-12-02 2023-02-20 スヴェン・ライフ・サイエンシーズ・リミテッド 認知症患者の行動心理学的症状の治療
CA3162938A1 (en) * 2019-12-02 2021-06-10 Suven Life Sciences Limited Methods for treating behavioral and psychological symptoms in patients with dementia

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JP4559230B2 (ja) * 2002-11-28 2010-10-06 スベン ライフ サイエンシズ リミティド セロトニン受容体に対する親和性を有する新規n−アリールスルホニル−3−置換されたインドール、その調製方法、それを含有する医薬組成物
PE20071143A1 (es) 2006-01-13 2008-01-20 Wyeth Corp Composicion farmaceutica que comprende un inhibidor de acetilcolinesterasa y un antagonista 5-hidroxitriptamina-6
ES2366958T3 (es) * 2006-06-23 2011-10-27 Laboratorios Del Dr. Esteve, S.A. Combinación de un inhibidor de la colinesterasa y un compuesto con afinidad por el receptor 5-ht6.
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CA2929309C (en) * 2013-12-02 2018-07-03 Suven Life Sciences Limited Process for large scale production of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1h-indole dimesylate monohydrate

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RS60422B1 (sr) 2020-07-31
ME03731B (me) 2021-01-20
MX2018014185A (es) 2019-02-25
PL3484467T3 (pl) 2020-08-24
SI3484467T1 (sl) 2020-10-30
DK3484467T3 (da) 2020-06-08
US11458135B2 (en) 2022-10-04
US20190125743A1 (en) 2019-05-02
ES2796181T3 (es) 2020-11-26
EA201892529A1 (ru) 2019-03-29
SG11201809856SA (en) 2018-12-28
CY1123013T1 (el) 2021-10-29
EP3484467A1 (en) 2019-05-22
BR112018073419A2 (pt) 2019-03-19
MD3484467T2 (ro) 2020-06-30
CN109069468A (zh) 2018-12-21
CA3023819A1 (en) 2017-11-23
WO2017199071A1 (en) 2017-11-23
PT3484467T (pt) 2020-06-16
CA3023819C (en) 2019-10-22
AU2016407427A1 (en) 2018-11-22
IL262921A (en) 2018-12-31
AU2016407427B2 (en) 2019-11-21
KR20190002700A (ko) 2019-01-08
JP2019516699A (ja) 2019-06-20
NZ748280A (en) 2020-07-31
KR102015484B1 (ko) 2019-08-28
EP3484467B1 (en) 2020-04-29
HUE050819T2 (hu) 2021-01-28
CN114642667A (zh) 2022-06-21
EA036347B1 (ru) 2020-10-29
JP6606299B2 (ja) 2019-11-13
MA45639B1 (fr) 2020-06-30
LT3484467T (lt) 2020-07-10
ZA201807468B (en) 2020-02-26

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