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PE20120031A1 - Compuestos aril metil benzoquinazolinona como moduladores alostericos positivos del receptor m1 - Google Patents

Compuestos aril metil benzoquinazolinona como moduladores alostericos positivos del receptor m1

Info

Publication number
PE20120031A1
PE20120031A1 PE2011001058A PE2011001058A PE20120031A1 PE 20120031 A1 PE20120031 A1 PE 20120031A1 PE 2011001058 A PE2011001058 A PE 2011001058A PE 2011001058 A PE2011001058 A PE 2011001058A PE 20120031 A1 PE20120031 A1 PE 20120031A1
Authority
PE
Peru
Prior art keywords
receptor
positive allosteric
allosteric modulators
compounds
methyl
Prior art date
Application number
PE2011001058A
Other languages
English (en)
Inventor
Scott D Kuduk
Douglas C Beshore
Marco Christina Di
Thomas J Greshock
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 PE20120031A1 publication Critical patent/PE20120031A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/08—Acetic acid
    • C07C53/10—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/19—Acids containing three or more carbon atoms
    • C07C53/21—Acids containing three or more carbon atoms containing fluorine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biomedical Technology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

REFERIDA A UN COMPUESTO DE FORMULA I, DONDE X, E, Z Y Q SON CADA UNO C, CH O UNO DE X, E, Z Y Q ES N Y LOS OTROS CH, C O JUNTOS INCLUYENDO R1 ESTAN ENLAZADOS PARA FORMAR NAFTILO; R1 ES H, ARILO, HETEROARILO, HALOGENO, CN, ENTRE OTROS; R2 ES H, ARILO, O-(ALQUILO C1-C6), CICLOALQUILO C3-C8, ENTRE OTROS; R3 ES H, ALQUILO C1-C6, HALOGENO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-(4-METOXIBENCIL)-3-(5-METIL)-1H-PIRAZOL-3-ILBENZO[H]QUINAZOLIN-4(3H)-ONA; RAC-3-[TRANS-2-HIDROXICICLOHEXIL]-6-{[6-(1-METIL-1H-PIRAZOL-4-IL)PIRIDINA-3-IL]METIL}BENZO[H] QUINAZOLIN-4(3H)-ONA; ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES ALOSTERICOS POSITIVOS DEL RECEPTOR M1 MUSCARINICO, UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER Y OTRAS ENFERMEDADES MEDIADAS POR EL RECEPTOR M1
PE2011001058A 2008-11-20 2009-11-19 Compuestos aril metil benzoquinazolinona como moduladores alostericos positivos del receptor m1 PE20120031A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19974008P 2008-11-20 2008-11-20

Publications (1)

Publication Number Publication Date
PE20120031A1 true PE20120031A1 (es) 2012-02-05

Family

ID=41565956

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011001058A PE20120031A1 (es) 2008-11-20 2009-11-19 Compuestos aril metil benzoquinazolinona como moduladores alostericos positivos del receptor m1

Country Status (36)

Country Link
US (4) US8557832B2 (es)
EP (1) EP2358686B1 (es)
JP (1) JP5102397B2 (es)
KR (1) KR101305590B1 (es)
CN (1) CN102292323B (es)
BR (1) BRPI0921924A2 (es)
CA (1) CA2743562C (es)
CO (1) CO6361928A2 (es)
CR (1) CR20110268A (es)
CY (1) CY1113665T1 (es)
DK (1) DK2358686T3 (es)
DO (1) DOP2011000135A (es)
EA (1) EA019098B1 (es)
EC (1) ECSP11011066A (es)
ES (1) ES2393694T3 (es)
GE (1) GEP20156348B (es)
GT (1) GT201100127A (es)
HN (1) HN2011001358A (es)
HR (1) HRP20120992T1 (es)
IL (1) IL212573A (es)
MA (1) MA32898B1 (es)
MX (1) MX2011005284A (es)
MY (1) MY162502A (es)
NI (1) NI201100100A (es)
NZ (1) NZ592961A (es)
PE (1) PE20120031A1 (es)
PL (1) PL2358686T3 (es)
PT (1) PT2358686E (es)
RS (1) RS52528B (es)
SG (1) SG171769A1 (es)
SI (1) SI2358686T1 (es)
SV (1) SV2011003912A (es)
TN (1) TN2011000209A1 (es)
UA (1) UA100459C2 (es)
WO (1) WO2010059773A1 (es)
ZA (1) ZA201103612B (es)

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HRP20120992T1 (hr) 2012-12-31
CY1113665T1 (el) 2016-06-22
HN2011001358A (es) 2014-03-03
SV2011003912A (es) 2011-10-13
EP2358686A1 (en) 2011-08-24
EA019098B1 (ru) 2014-01-30
US20110224198A1 (en) 2011-09-15
UA100459C2 (en) 2012-12-25
DK2358686T3 (da) 2013-01-07
MX2011005284A (es) 2011-06-17
EP2358686B1 (en) 2012-09-26
NZ592961A (en) 2012-09-28
CA2743562C (en) 2014-03-18
IL212573A (en) 2015-01-29
US20140005182A1 (en) 2014-01-02
TN2011000209A1 (en) 2012-12-17
US9708273B2 (en) 2017-07-18
IL212573A0 (en) 2011-06-30
CN102292323B (zh) 2014-12-24
GEP20156348B (en) 2015-08-25
US8883810B2 (en) 2014-11-11
US20160229813A1 (en) 2016-08-11
CA2743562A1 (en) 2010-05-27
SG171769A1 (en) 2011-07-28
US20150031713A1 (en) 2015-01-29
PL2358686T3 (pl) 2013-02-28
JP2012509343A (ja) 2012-04-19
CN102292323A (zh) 2011-12-21
WO2010059773A1 (en) 2010-05-27
RS52528B (sr) 2013-04-30
KR101305590B1 (ko) 2013-09-09
AU2009316578A1 (en) 2011-06-23
MY162502A (en) 2017-06-15
PT2358686E (pt) 2012-12-06
CR20110268A (es) 2011-07-01
US8557832B2 (en) 2013-10-15
JP5102397B2 (ja) 2012-12-19
HK1154587A1 (en) 2012-04-27
CO6361928A2 (es) 2012-01-20
MA32898B1 (fr) 2011-12-01
EA201170705A1 (ru) 2011-12-30
BRPI0921924A2 (pt) 2015-12-29
ECSP11011066A (es) 2011-06-30
DOP2011000135A (es) 2011-07-31
SI2358686T1 (sl) 2013-05-31
ES2393694T3 (es) 2012-12-27
NI201100100A (es) 2011-09-12
ZA201103612B (en) 2012-01-25
KR20110073596A (ko) 2011-06-29
GT201100127A (es) 2014-02-10

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