MX357241B - Inhibidores de fosfodiesterasa 10 de pirimidina. - Google Patents

Inhibidores de fosfodiesterasa 10 de pirimidina.

Info

Publication number
MX357241B
MX357241B MX2014002178A MX2014002178A MX357241B MX 357241 B MX357241 B MX 357241B MX 2014002178 A MX2014002178 A MX 2014002178A MX 2014002178 A MX2014002178 A MX 2014002178A MX 357241 B MX357241 B MX 357241B
Authority
MX
Mexico
Prior art keywords
pde10 inhibitors
pyrimidine
present
compounds
pyrimidine pde10
Prior art date
Application number
MX2014002178A
Other languages
English (en)
Other versions
MX2014002178A (es
Inventor
Christopher D Cox
Mark E Layton
Vadim Dudkin
Jeffrey Kern
Izzat T Raheem
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 MX2014002178A publication Critical patent/MX2014002178A/es
Publication of MX357241B publication Critical patent/MX357241B/es

Links

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    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • 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
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

Abstract

La presente invención se refiere a compuestos de pirimidina que son útiles como agentes terapéuticos para el tratamiento de trastornos del sistema nervioso central asociados con la fosfodiesterasa 10 (PDE10); la presente invención también se refiere al uso de dichos compuestos para tratar trastornos neurológicos y psiquiátricos, tales como la esquizofrenia, la psicosis o la enfermedad de Huntington, y aquellos asociados con la hipofunción del cuerpo estriado o la disfunción de los ganglios basales.
MX2014002178A 2011-08-25 2012-08-20 Inhibidores de fosfodiesterasa 10 de pirimidina. MX357241B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161527392P 2011-08-25 2011-08-25
PCT/US2012/051522 WO2013028590A1 (en) 2011-08-25 2012-08-20 Pyrimidine pde10 inhibitors

Publications (2)

Publication Number Publication Date
MX2014002178A MX2014002178A (es) 2014-05-01
MX357241B true MX357241B (es) 2018-06-29

Family

ID=47746797

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014002178A MX357241B (es) 2011-08-25 2012-08-20 Inhibidores de fosfodiesterasa 10 de pirimidina.

Country Status (36)

Country Link
US (1) US9062059B2 (es)
EP (1) EP2748151B1 (es)
JP (1) JP5648147B2 (es)
KR (1) KR101655635B1 (es)
CN (1) CN103917528B (es)
AR (1) AR087628A1 (es)
AU (1) AU2012299080B2 (es)
BR (1) BR112014004310B8 (es)
CA (1) CA2845578C (es)
CL (1) CL2014000450A1 (es)
CO (1) CO6890101A2 (es)
CR (1) CR20140085A (es)
CY (1) CY1117622T1 (es)
DK (1) DK2748151T3 (es)
DO (1) DOP2014000039A (es)
EA (1) EA023685B1 (es)
ES (1) ES2572527T3 (es)
HK (1) HK1193410A1 (es)
HR (1) HRP20160635T1 (es)
HU (1) HUE028451T2 (es)
IL (1) IL230997A (es)
MA (1) MA35508B1 (es)
ME (1) ME02419B (es)
MX (1) MX357241B (es)
MY (1) MY157301A (es)
NI (1) NI201400014A (es)
PE (1) PE20141535A1 (es)
PL (1) PL2748151T3 (es)
RS (1) RS54788B1 (es)
SG (1) SG2014013536A (es)
SI (1) SI2748151T1 (es)
TN (1) TN2014000070A1 (es)
TW (1) TWI450895B (es)
UA (1) UA109735C2 (es)
WO (1) WO2013028590A1 (es)
ZA (1) ZA201401272B (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2012318874A1 (en) 2011-10-06 2014-05-15 Merck Sharp & Dohme Corp. 1,3-substituted azetidine PDE10 inhibitors
WO2013052526A1 (en) 2011-10-06 2013-04-11 Merck Sharp & Dohme Corp. Triazolyl pde10 inhibitors
US9284302B2 (en) 2012-11-15 2016-03-15 Merck Sharp & Dohme Corp. Cyclobutyl benzimidazoles as PDE 10 inhibitors
TW201422610A (zh) 2012-11-15 2014-06-16 Merck Sharp & Dohme 作爲pde10抑制劑之經二級醇取代之三唑
WO2014078217A1 (en) * 2012-11-15 2014-05-22 Merck Sharp & Dohme Corp. Cyclopropyl imidazopyridine pde10 inhibitors
EP2922823B1 (en) * 2012-11-20 2018-10-31 Merck Sharp & Dohme Corp. Pyrimidine pde10 inhibitors
EP2922543B1 (en) 2012-11-20 2017-05-24 Merck Sharp & Dohme Corp. Substituted pyridone derivatives as pde10 inhibitors
WO2014139150A1 (en) * 2013-03-15 2014-09-18 Merck Sharp & Dohme Corp. Substituted pyridizinone derivatives as pde10 inhibitors
AP2016009374A0 (en) 2014-03-24 2016-08-31 Novartis Ag Monobactam organic compounds for the treatment of bacterial infections
US10125101B2 (en) 2016-11-28 2018-11-13 Boehringer Ingelheim International Gmbh Indanylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
TWI813203B (zh) * 2021-03-17 2023-08-21 美商默沙東有限責任公司 Pde10化合物之前藥
WO2023184486A1 (en) * 2022-04-01 2023-10-05 Merck Sharp & Dohme Llc Process for preparing ( (1s, 2s) -2- (5-methylpyridin-2-yl) cyclopropyl) -methanol
CN115403527B (zh) * 2022-07-20 2024-03-29 西安近代化学研究所 一种还原胺化法合成杀菌剂乙嘧酚的方法
WO2024049721A1 (en) * 2022-08-31 2024-03-07 Merck Sharp & Dohme Llc Sustained release delivery of a pde10 inhibitor

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2568929A1 (en) 2004-06-07 2005-12-22 Pfizer Products Inc. Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions
EP1810411A2 (en) 2004-10-12 2007-07-25 Maxlinear, Inc. A receiver architecture with digitally generated intermediate frequency
WO2006072828A2 (en) 2005-01-07 2006-07-13 Pfizer Products Inc. Heteroaromatic quinoline compounds and their use as pde10 inhibitors
DE602006002271D1 (de) * 2005-04-05 2008-09-25 Astrazeneca Ab Pyrimidinderivate zur verwendung als antikrebsmittel
GB0506883D0 (en) * 2005-04-05 2005-05-11 Astrazeneca Ab Chemical compounds
NL2000397C2 (nl) * 2006-01-05 2007-10-30 Pfizer Prod Inc Bicyclische heteroarylverbindingen als PDE10 inhibitoren.
WO2007129183A2 (en) 2006-05-02 2007-11-15 Pfizer Products Inc. Bicyclic heteroaryl compounds as pde10 inhibitors
EP2327704A4 (en) * 2008-08-29 2012-05-09 Shionogi & Co RING-CONDENSED AZOL DERIVATIVE WITH PI3K-INHIBITING EFFECT
CN102143951A (zh) 2008-09-04 2011-08-03 田边三菱制药株式会社 三取代嘧啶化合物及其作为pde10抑制剂的用途
JP2012501962A (ja) 2008-09-10 2012-01-26 田辺三菱製薬株式会社 芳香族含窒素六員環化合物及びその使用
TW201030001A (en) * 2008-11-14 2010-08-16 Amgen Inc Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors
WO2010077992A1 (en) * 2008-12-17 2010-07-08 Amgen Inc. Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors
WO2011008931A2 (en) 2009-07-15 2011-01-20 Cystic Fibrosis Foundation Therapeutics, Inc. Arylpyrimidine compounds and combination therapy comprising same for treating cystic fibrosis & related disorders
TWI481607B (zh) * 2009-12-17 2015-04-21 Lundbeck & Co As H 作為pde10a酵素抑制劑的2-芳基咪唑衍生物
US8470820B2 (en) * 2010-01-22 2013-06-25 Hoffman-La Roche Inc. Nitrogen-containing heteroaryl derivatives
EP2621926B1 (en) * 2010-09-30 2017-08-30 Merck Sharp & Dohme Corp. Pyrazolopyrimidine pde10 inhibitors
US8785467B2 (en) * 2010-09-30 2014-07-22 Merck Sharp & Dohme Corp. Alkoxy pyrimidine PDE10 inhibitors

Also Published As

Publication number Publication date
ES2572527T3 (es) 2016-06-01
PL2748151T3 (pl) 2016-09-30
HUE028451T2 (en) 2016-12-28
BR112014004310A2 (pt) 2017-03-28
CN103917528B (zh) 2016-04-20
EP2748151A4 (en) 2015-01-07
MX2014002178A (es) 2014-05-01
RS54788B1 (sr) 2016-10-31
BR112014004310B8 (pt) 2023-04-18
DK2748151T3 (en) 2016-07-04
ZA201401272B (en) 2017-09-27
CN103917528A (zh) 2014-07-09
NZ621245A (en) 2014-12-24
CO6890101A2 (es) 2014-03-10
PE20141535A1 (es) 2014-11-06
EP2748151B1 (en) 2016-03-16
CA2845578A1 (en) 2013-02-28
CR20140085A (es) 2014-05-02
EA023685B1 (ru) 2016-06-30
AU2012299080B2 (en) 2016-03-17
ME02419B (me) 2016-09-20
JP2014524471A (ja) 2014-09-22
AU2012299080A1 (en) 2014-03-06
SG2014013536A (en) 2014-07-30
JP5648147B2 (ja) 2015-01-07
EP2748151A1 (en) 2014-07-02
TWI450895B (zh) 2014-09-01
MY157301A (en) 2016-05-31
CA2845578C (en) 2016-02-16
KR20140053356A (ko) 2014-05-07
NI201400014A (es) 2014-07-25
IL230997A0 (en) 2014-03-31
TW201313699A (zh) 2013-04-01
BR112014004310B1 (pt) 2022-03-03
AR087628A1 (es) 2014-04-09
WO2013028590A1 (en) 2013-02-28
HRP20160635T1 (hr) 2016-07-01
US9062059B2 (en) 2015-06-23
EA201490492A1 (ru) 2014-06-30
KR101655635B1 (ko) 2016-09-07
CY1117622T1 (el) 2017-04-26
CL2014000450A1 (es) 2014-08-22
DOP2014000039A (es) 2014-06-01
MA35508B1 (fr) 2014-10-02
IL230997A (en) 2015-08-31
SI2748151T1 (sl) 2016-06-30
US20140228368A1 (en) 2014-08-14
TN2014000070A1 (en) 2015-07-01
UA109735C2 (xx) 2015-09-25
HK1193410A1 (zh) 2014-09-19

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