[go: up one dir, main page]

ECSP18078877A - Moduladores alostéricos de receptores de acetilcolina nicotínicos - Google Patents

Moduladores alostéricos de receptores de acetilcolina nicotínicos

Info

Publication number
ECSP18078877A
ECSP18078877A ECSENADI201878877A ECDI201878877A ECSP18078877A EC SP18078877 A ECSP18078877 A EC SP18078877A EC SENADI201878877 A ECSENADI201878877 A EC SENADI201878877A EC DI201878877 A ECDI201878877 A EC DI201878877A EC SP18078877 A ECSP18078877 A EC SP18078877A
Authority
EC
Ecuador
Prior art keywords
compounds
nicotinic acetylcholine
allosteric modulators
acetylcholine receptors
disease
Prior art date
Application number
ECSENADI201878877A
Other languages
English (en)
Inventor
J Greshock Thomas
M Suen Linda
John Harvey Andrew
L Duffy Joseph
t campbell Brian
L Rada Vanessa
M Bell Ian
D Shipe William
G Guiadeen Deodial
M Crowley Brendan
C Huff Belinda
M Sanders John
J Leavitt Kenneth
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 ECSP18078877A publication Critical patent/ECSP18078877A/es

Links

Classifications

    • 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
    • A61K31/415—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
    • 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
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/107—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with two aryl or substituted aryl radicals attached in positions 2 and 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • C07D277/26—Radicals substituted by sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (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)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Control Of El Displays (AREA)
  • Steroid Compounds (AREA)

Abstract

La presente divulgación se refiere a compuestos de fórmula I (descrita por la imagen que se remite en anexo) 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
ECSENADI201878877A 2016-03-22 2018-10-19 Moduladores alostéricos de receptores de acetilcolina nicotínicos ECSP18078877A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662311888P 2016-03-22 2016-03-22
US201662369778P 2016-08-02 2016-08-02

Publications (1)

Publication Number Publication Date
ECSP18078877A true ECSP18078877A (es) 2019-02-28

Family

ID=58455680

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI201878877A ECSP18078877A (es) 2016-03-22 2018-10-19 Moduladores alostéricos de receptores de acetilcolina nicotínicos

Country Status (39)

Country Link
US (3) US9840481B2 (es)
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 (2) GEP20207149B (es)
HR (1) HRP20211960T1 (es)
HU (1) HUE057460T2 (es)
IL (1) IL261807A (es)
JO (1) JOP20170067B1 (es)
LT (1) LT3433234T (es)
MA (1) MA43756B1 (es)
MD (1) MD3433234T2 (es)
MX (1) MX376257B (es)
MY (1) MY195948A (es)
PE (1) PE20181851A1 (es)
PH (1) PH12018502028B1 (es)
PL (1) PL3433234T3 (es)
PT (1) PT3433234T (es)
RS (1) RS62704B1 (es)
SG (1) SG11201808220VA (es)
SI (1) SI3433234T1 (es)
SV (1) SV2018005743A (es)
TN (1) TN2018000322A1 (es)
TW (1) TWI616438B (es)
UA (1) UA120571C2 (es)
WO (1) WO2017165256A1 (es)
ZA (1) ZA201806141B (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107529748B (zh) 2015-04-17 2020-12-25 美国陶氏益农公司 具有杀虫效用的分子，以及与其相关的中间体、组合物和方法
EP3964495A1 (en) 2016-10-12 2022-03-09 Dow AgroSciences LLC Molecules having pesticidal utility, and compositions, and processes, related thereto
EP3534888B1 (en) * 2016-11-01 2022-04-06 Merck Sharp & Dohme Corp. Substituted bicyclic heteroaryl allosteric modulators of nicotinic acetylcholine receptors
US10357493B2 (en) 2017-03-10 2019-07-23 Selenity Therapeutics (Bermuda), Ltd. 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
CA3073212A1 (en) 2017-09-19 2019-03-28 Merck Sharp & Dohme Corp. Heteroaryl allosteric modulators of nicotinic acetylcholine receptors
DK3788043T3 (da) * 2018-05-01 2024-12-16 Merck Sharp & Dohme Llc Spiropiperidin som allosteriske modulatorer af nicotinacetylcholinreceptorer
HU231333B1 (hu) 2018-07-13 2023-01-28 Richter Gedeon Nyrt Spirokromán származékok
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
WO2020087031A1 (en) 2018-10-26 2020-04-30 The Research Foundation For The State University Of New York Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia
TW202039420A (zh) * 2018-11-26 2020-11-01 美商富曼西公司 用於防治無脊椎害蟲的間二醯胺化合物
EP3962483A4 (en) * 2019-05-02 2023-01-25 Merck Sharp & Dohme LLC ALLOSTERIC SPIROPIPERIDINE MODULATORS OF NICOTINE ACETYLCHOLINE RECEPTORS
JP2022543106A (ja) 2019-07-30 2022-10-07 エイコニゾ セラピューティクス，インコーポレーテッド Ｈｄａｃ６インヒビターおよびそれらの使用
WO2021091751A1 (en) * 2019-11-05 2021-05-14 Merck Sharp & Dohme Corp. Spiropiperidine allosteric modulators of nicotinic acetylcholine receptors
CN111233783B (zh) * 2020-03-13 2021-11-16 温州大学 异噻唑-4-基二硫化物衍生物的合成方法
US20250002448A1 (en) * 2021-09-21 2025-01-02 Merck Sharp & Dohme Llc Allosteric modulators of nicotinic acetylcholine receptors
WO2023064771A1 (en) * 2021-10-12 2023-04-20 Brown University Glioblastoma multiforme treatments

Family Cites Families (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3487154A (en) 1967-04-03 1969-12-30 Smithkline Corp Method of lowering blood pressure
US3522302A (en) 1967-05-16 1970-07-28 Smithkline Corp P-(2-aminocycloalkyl)benzenesulfonamides
FR2508033A1 (fr) 1981-06-23 1982-12-24 Fabre Sa Pierre Aryl-1 aminomethyl-2 cyclopropanes carboxylates (z), leur preparation et leur application en tant que medicaments utiles dans le traitement d'algies diverses
US5286736A (en) 1990-11-22 1994-02-15 Dr. Karl Thomae Gmbh Pyridyl compounds and pharmaceutical compositions containing these compounds
TW394761B (en) 1993-06-28 2000-06-21 Hoffmann La Roche Novel Sulfonylamino Pyrimidines
FR2751645B1 (fr) 1996-07-29 1998-12-24 Sanofi Sa Amines pour la fabrication de medicaments destines a empecher la proliferation de cellules tumorales
TW530058B (en) 1997-07-22 2003-05-01 Astra Pharma Prod Triazolo [4,5-d]pyrimidine compounos and their use and process for preparation
CA2316264A1 (en) 1998-02-17 1999-08-19 Brian Springthorpe Novel triazolo(4,5-d)pyrimidine compounds
SE9802574D0 (sv) 1998-07-17 1998-07-17 Astra Pharma Prod Novel compounds
US6887870B1 (en) 1999-10-12 2005-05-03 Bristol-Myers Squibb Company Heterocyclic sodium/proton exchange inhibitors and method
JP2003523356A (ja) 2000-01-29 2003-08-05 エルジー シーアイ リミテッド アリール−アミジンを持つＸａ因子阻害剤とその誘導体、及びそれらのプロドラッグ
US6630469B2 (en) 2000-05-09 2003-10-07 Bristol-Myers Squibb Company 5-HT7 receptor antagonists
FR2810664B1 (fr) * 2000-06-27 2004-12-24 Adir Nouveaux composes cyclopropaniques 1,1 et 1,2-dissubstitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA2442525A1 (en) 2001-03-29 2002-10-10 Mendi Higgins Cyclopropylindole derivatives as selective serotonin reuptake inhibitors
AU2003215024B2 (en) 2002-03-26 2008-02-21 Merck Sharp & Dohme Corp. Spirocyclic amides as cannabinoid receptor modulators
CA2509086C (en) 2003-01-06 2012-08-21 Eli Lilly And Company Substituted arylcyclopropylacetamides as glucokinase activators
WO2006071184A1 (en) * 2004-12-28 2006-07-06 Astrazeneca Ab Aryl sulphonamide modulators
WO2007025089A2 (en) * 2005-08-24 2007-03-01 Rib-X Pharmaceutical, Inc. Triazole compounds and methods of making and using the same
CN102058571B (zh) 2005-09-09 2012-09-19 有限会社肯菲思 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)氨基甲酰基]苯甲酸在制备用于预防及/或治疗肠疾病的药物中的应用
AU2008307195B2 (en) 2007-10-04 2012-11-22 F. Hoffmann-La Roche Ag Cyclopropyl aryl amide derivatives and uses thereof
EA201001029A1 (ru) 2007-12-19 2011-06-30 Амген Инк. Производные фенилуксусной кислоты в качестве модуляторов процесса воспаления
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
CN102119142B (zh) 2008-08-12 2013-12-04 弗·哈夫曼-拉罗切有限公司 作为烟碱α7调节剂的水杨酰胺衍生物
US20120053164A1 (en) 2008-12-19 2012-03-01 Boehringer Ingelheim International Gmbh Cyclic pyrimidin-4-carboxamides as ccr2 receptor antagonists for treatment of inflammation, asthma and copd
EP2389362B1 (en) 2009-01-21 2019-12-11 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
AR077060A1 (es) 2009-06-11 2011-07-27 Abbott Lab Compuestos antivirales
US8937150B2 (en) 2009-06-11 2015-01-20 Abbvie Inc. Anti-viral compounds
WO2010144959A1 (en) 2009-06-18 2010-12-23 Fibrotech Therapeutics Pty Ltd Analogues of anti-fibrotic agents
US8552022B2 (en) 2009-08-13 2013-10-08 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
US9303027B2 (en) 2010-07-19 2016-04-05 Dr. Reddy's Laboratories Ltd. Kappa opioid receptor agonists
JP2013540767A (ja) 2010-10-07 2013-11-07 ザ ジェイ． デヴィッド グラッドストーン インスティテューツ 免疫不全ウイルス転写を調節するための組成物および方法
CA2819894A1 (en) 2010-12-16 2012-06-21 Abbvie Inc. Anti-viral compounds
KR101925971B1 (ko) 2011-01-28 2018-12-06 에스케이바이오팜 주식회사 피리돈 유도체 및 이를 포함하는 약학적 조성물
EP2670731B1 (en) 2011-02-02 2016-05-25 Bionomics Limited Positive allosteric modulators of the alpha 7 nicotinic acetylcholine receptor and uses thereof.
BR112013021602A2 (pt) * 2011-02-23 2019-09-24 Lupin Ltd derivados de heteroarila como moduladores de nachr alfa7.
WO2012151361A1 (en) 2011-05-03 2012-11-08 Concert Pharmaceuticals Inc. Carbamoylpyridone derivatives
ES2606043T3 (es) 2011-07-05 2017-03-17 Lupin Limited Derivados de biarilo como moduladores de nAChR
UA111746C2 (uk) * 2011-07-08 2016-06-10 Х. Луннбек А/С Позитивні алостеричні модулятори нікотинового рецептора ацетилхоліну
HRP20180913T1 (hr) 2011-07-08 2018-07-27 H. Lundbeck A/S Pozitivni alosterni modulatori receptora nikotinskog acetilkolina
ES2609003T3 (es) 2011-08-08 2017-04-18 Merck Patent Gmbh Carboxamidas de n-(bencimimazol-2-il) -ciclopropano como antagonistas de ácido lisofosfatídico
WO2014006120A1 (en) 2012-07-06 2014-01-09 H. Lundbeck A/S New positive allosteric modulators of nicotinic acetylcholine receptor
CN104884432A (zh) * 2012-08-01 2015-09-02 默沙东公司 α7烟碱乙酰胆碱受体调节剂及其用途-I
WO2014090731A1 (en) 2012-12-10 2014-06-19 H. Lundbeck A/S New positive allosteric modulators of nicotinic acetylcholine receptor
US10201614B2 (en) 2013-03-15 2019-02-12 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
WO2014172759A1 (en) 2013-04-24 2014-10-30 Bionomics Limited α7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF - III
TW201446243A (zh) * 2013-06-03 2014-12-16 Lupin Ltd 4-(5-(4-氯苯基)-2-(2-環丙基乙醯基)-1,4-二甲基-1氫-吡咯-3-基)苯磺醯胺作為α7尼古丁乙醯膽鹼受體調節劑
EP3086815B1 (en) 2013-12-27 2022-02-09 Zymeworks Inc. Sulfonamide-containing linkage systems for drug conjugates
BR112016015105A8 (pt) 2013-12-27 2018-04-24 Var2 Pharmaceuticals Aps conjugados var2csa-droga
JP6635949B2 (ja) 2014-06-04 2020-01-29 トーマス・ヘレデイズ・スティフテルス・フォー・メディシンスク・フォルスクニング 炎症性および自己免疫性の病気の処置のためのｍｔｈ１阻害剤
WO2015187088A1 (en) 2014-06-04 2015-12-10 Thomas Helledays Stiftelse För Medicinsk Forskning Mth1 inhibitors for treatment of cancer
WO2015191799A1 (en) * 2014-06-13 2015-12-17 Merck Sharp & Dohme Corp. Alpha-7 nicotinic acetylcholine receptor modulators and uses thereof

Also Published As

Publication number Publication date
MX2018011453A (es) 2019-01-10
SV2018005743A (es) 2019-01-18
ES2901197T3 (es) 2022-03-21
JP6526352B2 (ja) 2019-06-05
PT3433234T (pt) 2021-12-22
PH12018502028A1 (en) 2019-07-15
AU2017237930A1 (en) 2018-10-11
CN109153649B (zh) 2022-04-19
IL261807A (en) 2018-10-31
MY195948A (en) 2023-02-27
UA120571C2 (uk) 2019-12-26
RS62704B1 (sr) 2022-01-31
US20180030007A1 (en) 2018-02-01
NZ747408A (en) 2024-07-05
HUE057460T2 (hu) 2022-05-28
GEAP202014908A (en) 2020-03-10
CA3018185C (en) 2020-09-15
MX376257B (es) 2025-03-07
US20170275260A1 (en) 2017-09-28
EP3433234A1 (en) 2019-01-30
SG11201808220VA (en) 2018-10-30
DK3433234T3 (da) 2022-01-03
CO2018009889A2 (es) 2018-10-22
US9840481B2 (en) 2017-12-12
GEP20207149B (en) 2020-09-10
CL2018002697A1 (es) 2018-12-28
TWI616438B (zh) 2018-03-01
TN2018000322A1 (en) 2020-01-16
JOP20170067B1 (ar) 2021-08-17
ZA201806141B (en) 2019-08-28
CN109153649A (zh) 2019-01-04
LT3433234T (lt) 2021-12-10
AU2017237930B2 (en) 2019-02-07
PE20181851A1 (es) 2018-12-03
PH12018502028B1 (en) 2024-01-24
BR112018069456A2 (pt) 2019-02-05
KR102203552B1 (ko) 2021-01-18
CY1124828T1 (el) 2022-11-25
CA3018185A1 (en) 2017-09-28
US20190337910A1 (en) 2019-11-07
TW201733989A (zh) 2017-10-01
WO2017165256A1 (en) 2017-09-28
CR20180452A (es) 2019-02-06
JP2019512508A (ja) 2019-05-16
DOP2018000204A (es) 2019-07-15
US9926285B2 (en) 2018-03-27
MD3433234T2 (ro) 2022-02-28
AR107928A1 (es) 2018-06-28
MA43756B1 (fr) 2021-11-30
KR20180127644A (ko) 2018-11-29
SI3433234T1 (sl) 2022-01-31
MA43756A (fr) 2021-05-19
PL3433234T3 (pl) 2022-01-24
EP3433234B1 (en) 2021-10-27
EP3978479A1 (en) 2022-04-06
HRP20211960T1 (hr) 2022-03-18

Similar Documents

Publication Publication Date Title
ECSP18078877A (es) Moduladores alostéricos de receptores de acetilcolina nicotínicos
SV2017005434A (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
MX2019000980A (es) Compuestos y composiciones y usos de los mismos.
NI202000074A (es) Moduladores alostéricos de espiropiperidina de receptores nicotínicos de acetilcolina
DOP2014000230A (es) Agentes para tratar trastornos que implican la modulación de receptores de rianodina
UY35628A (es) ?compuestos heteroaromáticos y su uso como ligandos d1 de dopamina?.
CO7280468A2 (es) Antagonistas del receptor de 5-ht3
CL2019001891A1 (es) Derivados de bis-heteroarilo bicíclicos como moduladores de agregación de proteínas.
DOP2017000117A (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
CO2017005588A2 (es) 2-amino-5,5-difluoro-6-(fluorometil)-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
UY36218A (es) “derivados de piridina como moduladores alostéricos positivos del receptor muscarínico m1”
UY37947A (es) Amidas de imidazopiridina sustituidas y su uso
MX377304B (es) Derivados de piperazina como moduladores de los receptores x del hígado.
CL2016000019A1 (es) Compuestos derivados de dihidroxifenilo deuterado o una sal de los mismos; composición farmacéutica que los comprende y su uso para el tratamiento de trastornos mediados por neurotransmisores tales como hipotensión, trastornos del sueño, enfermedad de alzheimer y depresión.
MX2016012645A (es) Composiciones y metodos para tratar enfermedades neurodegenerativas.
MX2019000982A (es) Compuestos y composiciones y usos de los mismos.
MX365438B (es) Compuestos de tipo 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostericos positivos de receptores mglur2.
MX2014014751A (es) Compuestos de heteroarilo y metodos de uso de los mismos.
PE20151424A1 (es) Compuesto farmaceutico para la prevencion y el tratamiento de un trastorno o una enfermedad cognitivos, neurodegenerativos o neuronales
IN2014MU00276A (es)
CL2012001128A1 (es) Compuestos derivados de quinuclidina, moduladores del receptor de acetilcolina nicotinico alfa-7; composicion farmaceutica que los comprende; y uso para el tratamiento de esquizofrenia, enfermedad de alzheimer, trastornos cognitivos, artritis reumatoide, osteoartritis, colitis ulcerativa, enfermedad de crohn y diabetes.