CO2018009889A2 - Moduladores alostéricos de receptores de acetilcolina nicotínicos - Google Patents

Moduladores alostéricos de receptores de acetilcolina nicotínicos

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Publication number
CO2018009889A2
CO2018009889A2 CONC2018/0009889A CO2018009889A CO2018009889A2 CO 2018009889 A2 CO2018009889 A2 CO 2018009889A2 CO 2018009889 A CO2018009889 A CO 2018009889A CO 2018009889 A2 CO2018009889 A2 CO 2018009889A2
Authority
CO
Colombia
Prior art keywords
nicotinic acetylcholine
allosteric modulators
compounds
acetylcholine receptors
disease
Prior art date
Application number
CONC2018/0009889A
Other languages
English (en)
Inventor
M Brendan Crowley
T Brian Campbell
L Joseph Duffy
J Thomas Greshock
G Deodial Guiadeen
Andrew John Harvey
C Belinda Huff
J Kenneth Leavitt
L Vanessa Rada
M John Sanders
D William Shipe
M Linda Suen
M Ian Bell
Original Assignee
Merck Sharp & Dohme
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 filed Critical Merck Sharp & Dohme
Publication of CO2018009889A2 publication Critical patent/CO2018009889A2/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Biomedical Technology (AREA)
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  • Neurosurgery (AREA)
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  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Control Of El Displays (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente divulgación se refiere a compuestos de fórmula I que son útiles como moduladores de nAChR a7, a composiciones que comprenden dichos compuestos y al uso de dichos compuestos para prevenir, tratar o mejorar enfermedades, en particular trastornos del sistema nervioso central tales como alteraciones cognitivas en enfermedad de Alzheimer, la enfermedad de Parkinson y esquizofrenia, así como para disquinesia inducida por L-DOPA e inflamación
CONC2018/0009889A 2016-03-22 2018-09-19 Moduladores alostéricos de receptores de acetilcolina nicotínicos CO2018009889A2 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662311888P 2016-03-22 2016-03-22
US201662369778P 2016-08-02 2016-08-02
PCT/US2017/023127 WO2017165256A1 (en) 2016-03-22 2017-03-20 Allosteric modulators of nicotinic acetylcholine receptors

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CO2018009889A2 true CO2018009889A2 (es) 2018-10-22

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CONC2018/0009889A CO2018009889A2 (es) 2016-03-22 2018-09-19 Moduladores alostéricos de receptores de acetilcolina nicotínicos

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EP (2) EP3433234B1 (es)
JP (1) JP6526352B2 (es)
KR (1) KR102203552B1 (es)
CN (1) CN109153649B (es)
AR (1) AR107928A1 (es)
AU (1) AU2017237930B2 (es)
CA (1) CA3018185C (es)
CL (1) CL2018002697A1 (es)
CO (1) CO2018009889A2 (es)
CR (1) CR20180452A (es)
CY (1) CY1124828T1 (es)
DK (1) DK3433234T3 (es)
DO (1) DOP2018000204A (es)
EC (1) ECSP18078877A (es)
ES (1) ES2901197T3 (es)
GE (1) GEP20207149B (es)
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TW (1) TWI616438B (es)
UA (1) UA120571C2 (es)
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US10258045B2 (en) 2016-10-12 2019-04-16 Dow Agrosciences Llc Molecules having pesticidal utility and intermediates, compositions and processes related thereto
JP7041141B2 (ja) * 2016-11-01 2022-03-23 メルク・シャープ・アンド・ドーム・コーポレーション 置換された二環式ヘテロアリール系ニコチン性アセチルコリン受容体アロステリック調節剤
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
WO2019000238A1 (en) * 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
JP7221944B2 (ja) * 2017-09-19 2023-02-14 メルク・シャープ・アンド・ドーム・エルエルシー ニコチン性アセチルコリン受容体のヘテロアリールアロステリックモジュレーター
WO2019212927A1 (en) * 2018-05-01 2019-11-07 Merck Sharp & Dohme Corp. Spiropiperidine allosteric modulators of nicotinic acetylcholine receptors
HU231414B1 (hu) * 2018-07-13 2023-08-28 Richter Gedeon Nyrt. Tiadiazin származékok
HU231478B1 (hu) 2018-07-13 2024-02-28 Richter Gedeon Nyrt. Szubsztituált (aza)indol származékok
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