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

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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
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PE
Peru
Prior art keywords
receptor
positive allosteric
allosteric modulators
compounds
methyl
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PE2011001058A
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English (en)
Inventor
Scott D Kuduk
Douglas C Beshore
Marco Christina Di
Thomas J Greshock
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Merck Sharp & Dohme
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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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/08Acetic acid
    • C07C53/10Salts thereof
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/19Acids containing three or more carbon atoms
    • C07C53/21Acids containing three or more carbon atoms containing fluorine
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/15Fumaric acid
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
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    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
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    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

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

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PE20120031A1 true PE20120031A1 (es) 2012-02-05

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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)
HK (1) HK1154587A1 (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)
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SG (1) SG171769A1 (es)
SI (1) SI2358686T1 (es)
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TN (1) TN2011000209A1 (es)
UA (1) UA100459C2 (es)
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MY162502A (en) 2017-06-15
CA2743562C (en) 2014-03-18
JP2012509343A (ja) 2012-04-19
NI201100100A (es) 2011-09-12
BRPI0921924A2 (pt) 2015-12-29
SG171769A1 (en) 2011-07-28
CY1113665T1 (el) 2016-06-22
EP2358686A1 (en) 2011-08-24
WO2010059773A1 (en) 2010-05-27
HK1154587A1 (en) 2012-04-27
NZ592961A (en) 2012-09-28
CN102292323A (zh) 2011-12-21
US20140005182A1 (en) 2014-01-02
US8883810B2 (en) 2014-11-11
UA100459C2 (en) 2012-12-25
MX2011005284A (es) 2011-06-17
SI2358686T1 (sl) 2013-05-31
ECSP11011066A (es) 2011-06-30
US20110224198A1 (en) 2011-09-15
CN102292323B (zh) 2014-12-24
IL212573A0 (en) 2011-06-30
TN2011000209A1 (en) 2012-12-17
DOP2011000135A (es) 2011-07-31
CA2743562A1 (en) 2010-05-27
GEP20156348B (en) 2015-08-25
KR101305590B1 (ko) 2013-09-09
US20160229813A1 (en) 2016-08-11
MA32898B1 (fr) 2011-12-01
IL212573A (en) 2015-01-29
EA019098B1 (ru) 2014-01-30
HRP20120992T1 (hr) 2012-12-31
CO6361928A2 (es) 2012-01-20
PT2358686E (pt) 2012-12-06
SV2011003912A (es) 2011-10-13
CR20110268A (es) 2011-07-01
EA201170705A1 (ru) 2011-12-30
US20150031713A1 (en) 2015-01-29
US9708273B2 (en) 2017-07-18
ZA201103612B (en) 2012-01-25
RS52528B (en) 2013-04-30
PL2358686T3 (pl) 2013-02-28
AU2009316578A1 (en) 2011-06-23
JP5102397B2 (ja) 2012-12-19
ES2393694T3 (es) 2012-12-27
DK2358686T3 (da) 2013-01-07
US8557832B2 (en) 2013-10-15
EP2358686B1 (en) 2012-09-26
HN2011001358A (es) 2014-03-03
GT201100127A (es) 2014-02-10
KR20110073596A (ko) 2011-06-29

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