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)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Control Of El Displays (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Pyridine 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) EP3978479A1 (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) GEAP202014908A (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 (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3578541B1 (en) 2015-04-17 2025-05-28 Corteva Agriscience LLC Compositions comprising molecules having pesticidal utility, and processes related thereto
CA3038847A1 (en) 2016-10-12 2018-04-19 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
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
WO2019060210A1 (en) 2017-09-19 2019-03-28 Merck Sharp & Dohme Corp. HETEROARYLIC ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
JOP20200272A1 (ar) * 2018-05-01 2020-11-01 Merck Sharp & Dohme مُعدّلات تفارغية سبيروبيريدين لمستقبلات أستيل كولين نيكوتينية
HU231414B1 (hu) * 2018-07-13 2023-08-28 Richter Gedeon Nyrt. Tiadiazin származékok
HU231333B1 (hu) * 2018-07-13 2023-01-28 Richter Gedeon Nyrt Spirokromán származékok
HU231478B1 (hu) 2018-07-13 2024-02-28 Richter Gedeon Nyrt. Szubsztituált (aza)indol származékok
US20210393621A1 (en) 2018-10-26 2021-12-23 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
US12331022B2 (en) 2019-05-02 2025-06-17 Merck Sharp & Dohme Llc Spiropiperidine allosteric modulators of nicotinic acetylcholine receptors
CN114727974A (zh) 2019-07-30 2022-07-08 艾科尼佐治疗股份有限公司 Hdac6抑制剂及其用途
US12534458B2 (en) 2019-11-05 2026-01-27 Merck Sharp & Dohme Llc 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
WO2022169985A1 (en) 2021-02-03 2022-08-11 Eikonizo Therapeutics, Inc. Hdac6 inhibitors and uses thereof
EP4404934A4 (en) * 2021-09-21 2025-07-16 Merck Sharp & Dohme Llc ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
JP2024539008A (ja) * 2021-10-12 2024-10-28 ブラウン ユニバーシティ 多形膠芽腫処置
AU2023250964A1 (en) 2022-04-08 2024-11-07 Eikonizo Therapeutics, Inc. Oxadiazole hdac6 inhibitors and uses thereof

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
AR017014A1 (es) 1997-07-22 2001-08-22 Astrazeneca Ab Compuestos de triazolo [4,5-d]pirimidina, composiciones farmaceuticas, uso de los mismos para preparar medicamentos y procesos para la preparacionde dichos compuestos
MXPA00007634A (es) 1998-02-17 2003-09-10 Astrazeneca Uk Ltd Nuevos compuestos de triazol (4,5-d) pirimidina.
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
WO2001055146A1 (en) 2000-01-29 2001-08-02 Lg Chem Investment Ltd. FACTOR Xa INHIBITORS WITH ARYL-AMIDINES AND DERIVATIVES, AND PRODRUGS THEREOF
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
CZ20032644A3 (en) 2001-03-29 2004-06-16 Bristol-Myers Squibb Company 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
WO2004063179A1 (en) 2003-01-06 2004-07-29 Eli Lilly And Company Substituted arylcyclopropylacetamides as glucokinase activators
EP1833804A1 (en) * 2004-12-28 2007-09-19 AstraZeneca AB Aryl sulphonamide modulators
EP1934237A2 (en) * 2005-08-24 2008-06-25 Rib-X Pharmaceuticals, 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
KR101178674B1 (ko) * 2007-10-04 2012-08-30 에프. 호프만-라 로슈 아게 사이클로프로필 아릴 아마이드 유도체 및 이의 용도
ES2471919T3 (es) 2007-12-19 2014-06-27 Amgen, Inc Derivados de ácido fenilac�tico como moduladores de inflamación
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2010018095A1 (en) 2008-08-12 2010-02-18 F. Hoffmann-La Roche Ag Salicylamide derivatives as nicotinic alpha 7 modulators
ES2551557T3 (es) 2008-12-19 2015-11-19 Boehringer Ingelheim International Gmbh Pirimidin-4-carboxamidas cíclicas como antagonistas del receptor CCR2 para el tratamiento de inflamaciones, asma y EPOC
US8993808B2 (en) 2009-01-21 2015-03-31 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
EP2853531A3 (en) 2009-06-11 2015-08-12 AbbVie Bahamas Ltd. Antiviral compounds
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
WO2011019538A1 (en) * 2009-08-13 2011-02-17 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
WO2012012410A2 (en) 2010-07-19 2012-01-26 Dr. Reddy's Laboratories Ltd. Kappa opioid receptor agonists
US20120108500A1 (en) 2010-10-07 2012-05-03 Naoki Sakane Compositions and Methods for Modulating Immunodeficiency Virus Transcription
WO2012083170A1 (en) 2010-12-16 2012-06-21 Abbott Laboratories Anti-viral compounds
KR101925971B1 (ko) 2011-01-28 2018-12-06 에스케이바이오팜 주식회사 피리돈 유도체 및 이를 포함하는 약학적 조성물
AU2012212393B2 (en) 2011-02-02 2015-06-11 Bionomics Limited Positive allosteric modulators of the alpha 7 nicotinic acetylcholine receptor and uses thereof.
AU2012221800B2 (en) 2011-02-23 2016-10-27 Lupin Limited Heteroaryl derivatives as alpha7 nAChR modulators
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
HRP20180913T1 (hr) 2011-07-08 2018-07-27 H. Lundbeck A/S Pozitivni alosterni modulatori receptora nikotinskog acetilkolina
UA111746C2 (uk) 2011-07-08 2016-06-10 Х. Луннбек А/С Позитивні алостеричні модулятори нікотинового рецептора ацетилхоліну
WO2013020622A1 (en) 2011-08-08 2013-02-14 Merck Patent Gmbh N-(benzimimdazol-2-yl)-cyclopropane carboxamides as lysophosphatidic acid antagonists
WO2014006120A1 (en) 2012-07-06 2014-01-09 H. Lundbeck A/S New positive allosteric modulators of nicotinic acetylcholine receptor
EP2888229B1 (en) * 2012-08-01 2019-02-06 Merck Sharp & Dohme Corp. alpha7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF
EP2928860A1 (en) * 2012-12-10 2015-10-14 H. Lundbeck A/S New positive allosteric modulators of nicotinic acetylcholine receptor
HK1220626A1 (zh) 2013-03-15 2017-05-12 The Centre For Drug Research And Development 具细胞毒性和抗有丝分裂的化合物以及其使用方法
US9593096B2 (en) 2013-04-24 2017-03-14 Merck Sharp & Dohme Corp. 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
MX2016008448A (es) 2013-12-27 2017-01-09 Zymeworks Inc Conjugados de var2csa-farmaco.
KR102384740B1 (ko) 2013-12-27 2022-04-07 자임워크스 인코포레이티드 약물 접합체를 위한 설폰아마이드-함유 연결 시스템
CN106794181A (zh) 2014-06-04 2017-05-31 托马斯·黑勒戴药物研究基金会 用于治疗炎性和自身免疫性病况的mth1抑制剂
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
EP3433234A1 (en) 2019-01-30
US9926285B2 (en) 2018-03-27
KR102203552B1 (ko) 2021-01-18
MA43756A (fr) 2021-05-19
GEAP202014908A (en) 2020-03-10
US20190337910A1 (en) 2019-11-07
CY1124828T1 (el) 2022-11-25
AR107928A1 (es) 2018-06-28
PE20181851A1 (es) 2018-12-03
JP2019512508A (ja) 2019-05-16
DK3433234T3 (da) 2022-01-03
RS62704B1 (sr) 2022-01-31
WO2017165256A1 (en) 2017-09-28
PH12018502028B1 (en) 2024-01-24
BR112018069456A2 (pt) 2019-02-05
LT3433234T (lt) 2021-12-10
GEP20207149B (en) 2020-09-10
MD3433234T2 (ro) 2022-02-28
PT3433234T (pt) 2021-12-22
MX376257B (es) 2025-03-07
EP3978479A1 (en) 2022-04-06
PH12018502028A1 (en) 2019-07-15
CO2018009889A2 (es) 2018-10-22
JP6526352B2 (ja) 2019-06-05
EP3433234B1 (en) 2021-10-27
ZA201806141B (en) 2019-08-28
HRP20211960T1 (hr) 2022-03-18
PL3433234T3 (pl) 2022-01-24
MY195948A (en) 2023-02-27
UA120571C2 (uk) 2019-12-26
NZ747408A (en) 2024-07-05
CA3018185A1 (en) 2017-09-28
US9840481B2 (en) 2017-12-12
DOP2018000204A (es) 2019-07-15
CL2018002697A1 (es) 2018-12-28
KR20180127644A (ko) 2018-11-29
SI3433234T1 (sl) 2022-01-31
US20180030007A1 (en) 2018-02-01
CR20180452A (es) 2019-02-06
US20170275260A1 (en) 2017-09-28
MA43756B1 (fr) 2021-11-30
AU2017237930B2 (en) 2019-02-07
CN109153649A (zh) 2019-01-04
MX2018011453A (es) 2019-01-10
JOP20170067B1 (ar) 2021-08-17
CA3018185C (en) 2020-09-15
TWI616438B (zh) 2018-03-01
CN109153649B (zh) 2022-04-19
HUE057460T2 (hu) 2022-05-28
ES2901197T3 (es) 2022-03-21
IL261807A (en) 2018-10-31
SG11201808220VA (en) 2018-10-30
TN2018000322A1 (en) 2020-01-16
AU2017237930A1 (en) 2018-10-11
TW201733989A (zh) 2017-10-01
SV2018005743A (es) 2019-01-18

Similar Documents

Publication Publication Date Title
CO2018009889A2 (es) Moduladores alostéricos de receptores de acetilcolina nicotínicos
NI202000074A (es) Moduladores alostéricos de espiropiperidina de receptores nicotínicos de acetilcolina
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
CL2018001089A1 (es) Sales de valbenazina y polimorfos de las mismas.
MX2019000980A (es) Compuestos y composiciones y usos de los mismos.
DOP2014000230A (es) Agentes para tratar trastornos que implican la modulación de receptores de rianodina
CR20160394A (es) Heteroaril amidas como inhibidores de agregación de proteína
UY35628A (es) ?compuestos heteroaromáticos y su uso como ligandos d1 de dopamina?.
ECSP15004780A (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.
CL2015002545A1 (es) Nuevos compuestos inhibidores de la fosfodiesterasa del tipo 10a.
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.
MX2014014751A (es) Compuestos de heteroarilo y metodos de uso 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.
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.