BR112019005869A8 - Derivados de cromano, isocromano e dihidroisobenzofurano como moduladores alostéricos negativos de mglur2, composições e seu uso - Google Patents

Derivados de cromano, isocromano e dihidroisobenzofurano como moduladores alostéricos negativos de mglur2, composições e seu uso

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Publication number
BR112019005869A8
BR112019005869A8 BR112019005869A BR112019005869A BR112019005869A8 BR 112019005869 A8 BR112019005869 A8 BR 112019005869A8 BR 112019005869 A BR112019005869 A BR 112019005869A BR 112019005869 A BR112019005869 A BR 112019005869A BR 112019005869 A8 BR112019005869 A8 BR 112019005869A8
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BR
Brazil
Prior art keywords
mglur2
pharmaceutically acceptable
disorders
compounds
acceptable salt
Prior art date
Application number
BR112019005869A
Other languages
English (en)
Other versions
BR112019005869A2 (pt
BR112019005869B1 (pt
Inventor
K Sebhat Iyassu
Arasappan Ashok
B Hoyt Scott
R Wilkening Robert
Demong Duane
Original Assignee
Merck Sharp & Dohme
Merck Sharp & Dohme Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme, Merck Sharp & Dohme Llc filed Critical Merck Sharp & Dohme
Publication of BR112019005869A2 publication Critical patent/BR112019005869A2/pt
Publication of BR112019005869A8 publication Critical patent/BR112019005869A8/pt
Publication of BR112019005869B1 publication Critical patent/BR112019005869B1/pt

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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
    • A61K31/01Hydrocarbons
    • A61K31/015Hydrocarbons carbocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61P25/14Drugs 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
    • A61P25/20Hypnotics; 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
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22Bridged ring systems
    • C07D221/24Camphidines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/02Halogenated hydrocarbons
    • A61K31/025Halogenated hydrocarbons carbocyclic
    • A61K31/03Halogenated hydrocarbons carbocyclic aromatic

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

A presente invenção fornece certos compostos de cromano, isocromano e dihidroisobenzofurano substituídos de fórmula (I) ou um sal farmaceuticamente aceitável dos mesmos, em que o anel A é uma porção selecionada de: (II), (III), (IV) e (V), e o anel B, n, R1, R2, R2A, R3 e R3A são como definidos aqui. Os compostos da invenção são úteis como inibidores de mGluR2 ou moduladores alostéricos negativos (NAMs) de mGluR2, e podem ser úteis em métodos de tratar um paciente para doenças ou transtornos em que o receptor do NAM de mGluR2 está envolvido, tais como doença de Alzheimer, deficiência cognitiva, deficiência cognitiva leve, esquizofrenia e outras doenças de humor, transtornos da dor e transtornos do sono, administrando-se ao paciente uma quantidade terapeuticamente eficaz de um composto da invenção ou um sal farmaceuticamente aceitável do mesmo. A invenção também é direcionada à composições farmacêuticas compreendendo um composto da invenção ou um sal farmaceuticamente aceitável do mesmo, (opcionalmente em combinação com um ou mais ingredientes ativos adicionais), e um carreador farmaceuticamente aceitável, e ao uso dos compostos e composições farmacêuticas da invenção no tratamento de tais doenças.
BR112019005869-9A 2016-09-27 2017-09-25 Compostos derivados de cromano , isocromano e dihidroisobenzofurano como moduladores alostéricos negativos de mglur2, composição farmacêutica, combinação e seu uso BR112019005869B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662400150P 2016-09-27 2016-09-27
US62/400,150 2016-09-27
PCT/US2017/053155 WO2018063955A1 (en) 2016-09-27 2017-09-25 CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

Publications (3)

Publication Number Publication Date
BR112019005869A2 BR112019005869A2 (pt) 2019-06-11
BR112019005869A8 true BR112019005869A8 (pt) 2023-05-02
BR112019005869B1 BR112019005869B1 (pt) 2023-08-01

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CN109983022B (zh) 2022-06-07
JOP20190058B1 (ar) 2023-09-17
EP3519416A1 (en) 2019-08-07
KR20190056418A (ko) 2019-05-24
AU2017334870A1 (en) 2019-03-28
PL3519416T3 (pl) 2021-09-06
DK3519416T3 (da) 2021-05-25
GEP20217266B (en) 2021-06-25
TWI764934B (zh) 2022-05-21
IL265366B (en) 2021-12-01
JP6992109B2 (ja) 2022-02-15
LT3519416T (lt) 2021-06-10
MX2019003492A (es) 2019-09-19
CO2019002673A2 (es) 2019-03-29
US20190247374A1 (en) 2019-08-15
UA123687C2 (uk) 2021-05-12
IL265366A (en) 2019-05-30
HUE054898T2 (hu) 2021-10-28
SI3519416T1 (sl) 2021-08-31
HRP20210793T1 (hr) 2021-09-03
TN2020000161A1 (en) 2022-04-04
US10335399B2 (en) 2019-07-02
ECSP19020742A (es) 2019-04-30
PE20190609A1 (es) 2019-04-23
JP6681517B2 (ja) 2020-04-15
US20210015800A1 (en) 2021-01-21
ES2868973T3 (es) 2021-10-22
MD3519416T2 (ro) 2021-09-30
JOP20190058A1 (ar) 2019-03-24
NI201900025A (es) 2019-05-27
JP6945605B2 (ja) 2021-10-06
AR109714A1 (es) 2019-01-16
PT3519416T (pt) 2021-05-13
US20220218676A1 (en) 2022-07-14
US20180085358A1 (en) 2018-03-29
CR20190147A (es) 2019-05-17
ZA201901701B (en) 2023-03-29
MA46342A (fr) 2019-08-07
TW201815794A (zh) 2018-05-01
JP2020011989A (ja) 2020-01-23
US10806724B2 (en) 2020-10-20
AU2020270468B2 (en) 2022-02-17
CN109983022A (zh) 2019-07-05
TN2020000160A1 (en) 2022-04-04
CA3037537A1 (en) 2018-04-05
WO2018063955A1 (en) 2018-04-05
CL2019000778A1 (es) 2019-05-31
AU2017334870C1 (en) 2020-12-17
AU2020270468A1 (en) 2020-12-10
PH12019500597A1 (en) 2019-07-24
BR112019005869A2 (pt) 2019-06-11
CA3037537C (en) 2021-06-15
KR102296043B1 (ko) 2021-08-30
EA038627B1 (ru) 2021-09-24
JP2019529468A (ja) 2019-10-17
MY196807A (en) 2023-05-03
RS61890B1 (sr) 2021-06-30
JP2020111596A (ja) 2020-07-27
MA46342B1 (fr) 2021-05-31
DOP2019000076A (es) 2019-07-15
AU2017334870B2 (en) 2020-08-20
CY1124346T1 (el) 2022-07-22
EP3519416B1 (en) 2021-03-31
GEP20217279B (en) 2021-08-10
EA201990818A1 (ru) 2019-08-30

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Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07G Grant request does not fulfill article 229-c lpi (prior consent of anvisa) [chapter 7.7 patent gazette]

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B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B25A Requested transfer of rights approved

Owner name: MERCK SHARP AND DOHME LLC (US)

B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 25/09/2017, OBSERVADAS AS CONDICOES LEGAIS