HRP20141199T1 - Kombinacija od spoja glyt1 s antipsihoticima - Google Patents

Kombinacija od spoja glyt1 s antipsihoticima Download PDF

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Publication number
HRP20141199T1
HRP20141199T1 HRP20141199AT HRP20141199T HRP20141199T1 HR P20141199 T1 HRP20141199 T1 HR P20141199T1 HR P20141199A T HRP20141199A T HR P20141199AT HR P20141199 T HRP20141199 T HR P20141199T HR P20141199 T1 HRP20141199 T1 HR P20141199T1
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Croatia
Prior art keywords
methanone
piperazin
methanesulfonyl
trifluoro
pyridin
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HRP20141199AT
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English (en)
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Daniela Alberati
Jean-Luc Moreau
Joseph G. Wettstein
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F. Hoffmann - La Roche Ag
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Application filed by F. Hoffmann - La Roche Ag filed Critical F. Hoffmann - La Roche Ag
Publication of HRP20141199T1 publication Critical patent/HRP20141199T1/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
    • A61K31/495Heterocyclic 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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (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 (9)

1. Farmaceutska kombinacija, naznačena time, da obuhvaća netipičan antipsihotički lijek i antagonist receptora GlyT1 sljedeće formule I: [image] u kojoj Ar je supstituirana 6-člana heteroaril-skupina koja sadrži jedan, dva ili tri atoma dušika, i pri čemu heteroaril-skupine mogu biti supstituirane s jednim ili više supstituenata odabranih iz skupine koju čine halogen, (C1-C6)-alkil ili (C1-C6)-alkil supstituiran s halogenom; R1 je vodik ili (C1-C6)-alkil; R2 je (C1-C6)-alkil supstituiran s halogenom; R3, R4 i R6 su međusobno neovisno vodik, halogen (C1-C6)-alkil ili (C1-C6)-alkoksi; R5 je SO2R10; R10 je (C1-C6)-alkil opcijski supstituiran s halogenom; i njihove farmaceutski prikladne kiselinske adicijske soli, kao i njihove enantiomerne oblike.
2. Farmaceutska kombinacija prema zahtjevu 1, naznačena time, da obuhvaća netipičan antipsihotički lijek odabran iz skupine koju čine risperidon, paliperidon, olanzapin, aripiprazol, kvetiapin ili ciprazidon te antagonist receptora GlyT1 odabran od sljedećih: rac-[4-(3-kloro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon, rac-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-[4-(5-trifluorometil-piridin-2-il)-piperazin-1-il]-metanon, rac-[4-(5-bromo-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon, rac-[4-(3-fluoro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon, rac-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-[4-(6-trifluorometil-piridin-2-il)-piperazin-1-il]-metanon, [5-metansulfonil-2-((S ili R)-2,2,2-trifluoro-1-metil-etoksi)-fenil]-[4-(5-trifluorometil-piridin-2-il)-piperazin-1-il]-metanon, [5-metansulfonil-2-((R ili S)-2,2,2-trifluoro-1-metil-etoksi)-fenil]-[4-(5-trifluorometil-piridin-2-il)-piperazin-1-il]-metanon, [4-((3-fluoro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-((S)-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon ili [4-((3-fluoro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1,1-dimetil-etoksi)-fenil]-metanon.
3. Farmaceutska kombinacija prema zahtjevu 2, naznačena time, da obuhvaća netipičan antipsihotički lijek, odabran iz skupine koju čine risperidon, paliperidon, olanzapin, aripiprazol, kvetiapin ili ciprazidon te antagonist receptora GlyT1: [4-(3-fluoro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon.
4. Farmaceutska kombinacija, naznačena time, da obuhvaća netipičan antipsihotički lijek odabran iz skupine koju čine olanzapin ili risperidon i antagonist receptora GlyT1 koji je sljedeći: [image] i njihove farmaceutski prikladne kiselinske adicijske soli, kao i njihove enantiomerne oblike.
5. Farmaceutska kombinacija prema zahtjevu 1, koja obuhvaća netipičan antipsihotički lijek i antagonist receptora GlyT1, naznačena time, da se upotrebljava u liječenju pozitivnih i negativnih simptoma kod shizofrenije.
6. Uporaba farmaceutske kombinacije koja obuhvaća netipičan antipsihotički lijek i antagonist receptora GlyT1 sljedeće formule: [image] u kojoj Ar je supstituirana 6-člana heteroaril-skupina koja sadrži jedan, dva ili tri atoma dušika, i pri čemu heteroaril-skupine mogu biti supstituirane s jednim ili više supstituenata odabranih iz skupine koju čine halogen, (C1-C6)-alkil ili (C1-C6)-alkil supstituiran s halogenom; R1 je vodik ili (C1-C6)-alkil; R2 je (C1-C6)-alkil supstituiran s halogenom; R3, R4 i R6 su međusobno neovisno vodik, halogen (C1-C6)-alkil ili (C1-C6)-alkoksi; R5 je SO2R10; R10 je (C1-C6)-alkil opcijski supstituiran s halogenom; i njihove farmaceutski prikladne kiselinske adicijske soli, kao i njihove enantiomerne oblike, naznačena time, da je za proizvodnju lijeka za liječenje pozitivnih i negativnih simptoma kod shizofrenije.
7. Uporaba farmaceutske kombinacije prema zahtjevu 6, koja obuhvaća netipičan antipsihotički lijek odabran iz skupine koju čine risperidon, paliperidon, olanzapin, aripiprazol, kvetiapin ili ciprazidon te antagonist receptora GlyT1 odabran od sljedećih: rac-[4-(3-kloro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon, rac-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-[4-(5-trifluorometil-piridin-2-il)-piperazin-1-il]-metanon, rac-[4-(5-bromo-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon, rac-[4-(3-fluoro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon, rac-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-[4-(6-trifluorometil-piridin-2-il)-piperazin-1-il]-metanon, [5-metansulfonil-2-((S ili R)-2,2,2-trifluoro-1-metil-etoksi)-fenil]-[4-(5-trifluorometil-piridin-2-il)-piperazin-1-il]-metanon, [5-metansulfonil-2-((R ili S)-2,2,2-trifluoro-1-metil-etoksi)-fenil]-[4-(5-trifluorometil-piridin-2-il)-piperazin-1-il]-metanon, [4-((3-fluoro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-((S)-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon ili [4-((3-fluoro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1,1-dimetil-etoksi)-fenil]-metanon, naznačena time, da je za proizvodnju lijeka za liječenje pozitivnih i negativnih simptoma kod shizofrenije.
8. Uporaba farmaceutske kombinacije prema zahtjevu 7, koja obuhvaća netipičan antipsihotički lijek odabran iz skupine koju čine risperidon, paliperidon, olanzapin, aripiprazol, kvetiapin ili ciprazidon te sljedeći antagonist receptora GlyT1: [4-(3-fluoro-5-trifluorometil-piridin-2-il)-piperazin-1-il]-[5-metansulfonil-2-(2,2,2-trifluoro-1-metil-etoksi)-fenil]-metanon, naznačena time, da je za proizvodnju lijeka za liječenje pozitivnih i negativnih simptoma kod shizofrenije.
9. Uporaba farmaceutske kombinacije prema zahtjevu 8, naznačena time, da se koristi kombinacija koja obuhvaća netipičan antipsihotički lijek odabran iz skupine koju čine olanzapin ili risperidon te antagonist receptora GlyT1 koji je sljedeći: [image] i njihove farmaceutski prikladne kiselinske adicijske soli, kao i njihove enantiomerne oblike.
HRP20141199AT 2010-08-09 2014-12-11 Kombinacija od spoja glyt1 s antipsihoticima HRP20141199T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10172316 2010-08-09
PCT/EP2011/063533 WO2012019970A1 (en) 2010-08-09 2011-08-05 Combination of glyt1 compound with antipsychotics
EP11739097.1A EP2603219B1 (en) 2010-08-09 2011-08-05 Combination of glyt1 compound with antipsychotics

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HRP20141199T1 true HRP20141199T1 (hr) 2015-02-13

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US (1) US20120035156A1 (hr)
EP (1) EP2603219B1 (hr)
JP (1) JP2013533297A (hr)
KR (1) KR101455947B1 (hr)
CN (1) CN103068388A (hr)
AR (1) AR084401A1 (hr)
AU (1) AU2011288536B2 (hr)
BR (1) BR112013003068A2 (hr)
CA (1) CA2803656A1 (hr)
CL (1) CL2013000378A1 (hr)
CR (1) CR20130027A (hr)
CY (1) CY1115886T1 (hr)
DK (1) DK2603219T3 (hr)
EA (1) EA201291477A1 (hr)
EC (1) ECSP13012431A (hr)
ES (1) ES2521596T3 (hr)
HR (1) HRP20141199T1 (hr)
MA (1) MA34457B1 (hr)
MX (1) MX2013001166A (hr)
NZ (1) NZ604891A (hr)
PE (1) PE20131100A1 (hr)
PL (1) PL2603219T3 (hr)
PT (1) PT2603219E (hr)
SG (1) SG187108A1 (hr)
SI (1) SI2603219T1 (hr)
TW (1) TW201211019A (hr)
WO (1) WO2012019970A1 (hr)
ZA (1) ZA201300434B (hr)

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BR112015022174B1 (pt) 2013-03-13 2022-07-05 Sage Therapeutics, Inc Compostos esteróides neuroativos, sua composição farmacêutica e seu uso
KR20160068975A (ko) * 2013-12-03 2016-06-15 에프. 호프만-라 로슈 아게 약학 조성물
IL248567B (en) * 2014-04-30 2022-08-01 Univ Nat Taiwan Use of compounds known as d-amino acid oxidase inhibitors
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WO2016057713A1 (en) * 2014-10-07 2016-04-14 Sage Therapeutics, Inc. Neuroactive compounds and methods of use thereof
ES2884086T3 (es) 2015-07-06 2021-12-10 Sage Therapeutics Inc Oxisteroles y sus procedimientos de uso
PE20180483A1 (es) 2015-07-06 2018-03-07 Sage Therapeutics Inc Oxiesteroles y metodos de uso de los mismos
US10696712B2 (en) 2015-07-06 2020-06-30 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
ES2921010T3 (es) 2016-04-01 2022-08-16 Sage Therapeutics Inc Oxisteroles y procedimientos de uso de los mismos
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
RS62222B1 (sr) 2016-07-07 2021-09-30 Sage Therapeutics Inc 24-hidroksisteroli supstituisani na poziciji 11 za upotrebu u lečenju stanja povezanih sa nmda
AU2017337121B2 (en) 2016-09-30 2022-01-27 Sage Therapeutics, Inc. C7 substituted oxysterols and methods as NMDA modulators
CN115181153A (zh) 2016-10-18 2022-10-14 萨奇治疗股份有限公司 氧甾醇及其使用方法
CN110072874B (zh) 2016-10-18 2022-08-12 萨奇治疗股份有限公司 氧甾醇及其使用方法
CN107469087A (zh) * 2017-09-10 2017-12-15 孙永丽 用于治疗精神病的制剂
JP7355747B2 (ja) * 2017-11-14 2023-10-03 エスケー バイオファーマスティカルズ カンパニー リミテッド カルバメート化合物を含む統合失調症の予防、軽減又は治療用配合物
KR20220125326A (ko) 2020-01-09 2022-09-14 디스크 메디슨, 인크. 적혈구형성 프로토포르피린증, x-연계된 프로토포르피린증, 또는 선천성 적혈구 조혈포르피린증을 글리신 운반 억제제로 치료하는 방법

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KR20130045379A (ko) 2013-05-03
PT2603219E (pt) 2014-11-25
CY1115886T1 (el) 2017-01-25
AU2011288536B2 (en) 2014-10-09
DK2603219T3 (da) 2014-10-13
KR101455947B1 (ko) 2014-10-28
WO2012019970A1 (en) 2012-02-16
NZ604891A (en) 2015-01-30
BR112013003068A2 (pt) 2016-06-28
MA34457B1 (fr) 2013-08-01
SG187108A1 (en) 2013-02-28
US20120035156A1 (en) 2012-02-09
EP2603219A1 (en) 2013-06-19
CA2803656A1 (en) 2012-02-16
ES2521596T3 (es) 2014-11-13
ZA201300434B (en) 2013-09-25
AU2011288536A1 (en) 2013-01-31
ECSP13012431A (es) 2013-03-28
CL2013000378A1 (es) 2013-05-03
CR20130027A (es) 2013-03-04
CN103068388A (zh) 2013-04-24
EA201291477A1 (ru) 2013-06-28
PL2603219T3 (pl) 2015-03-31
JP2013533297A (ja) 2013-08-22
MX2013001166A (es) 2013-03-22
SI2603219T1 (sl) 2014-12-31
TW201211019A (en) 2012-03-16
PE20131100A1 (es) 2013-09-23
EP2603219B1 (en) 2014-09-17
AR084401A1 (es) 2013-05-15

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