CR20140085A - Inhibidores de pde10 de pirimidina - Google Patents

Inhibidores de pde10 de pirimidina

Info

Publication number
CR20140085A
CR20140085A CR20140085A CR20140085A CR20140085A CR 20140085 A CR20140085 A CR 20140085A CR 20140085 A CR20140085 A CR 20140085A CR 20140085 A CR20140085 A CR 20140085A CR 20140085 A CR20140085 A CR 20140085A
Authority
CR
Costa Rica
Prior art keywords
pde10 inhibitors
pyrimidine
relates
present
compounds
Prior art date
Application number
CR20140085A
Other languages
English (en)
Inventor
Christopher D Cox
Vadim Dudkin
Jeffrey Kern
Mark E Layton
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 CR20140085A publication Critical patent/CR20140085A/es

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Classifications

    • 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
    • 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
    • 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
    • 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

Landscapes

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

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, lapsicosis o la enfermedad de Huntington, y aquellos asociados con la hipofunción del cuerpo estriado o la disfunción de los ganglios basales.
CR20140085A 2011-08-25 2014-02-24 Inhibidores de pde10 de pirimidina CR20140085A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161527392P 2011-08-25 2011-08-25

Publications (1)

Publication Number Publication Date
CR20140085A true CR20140085A (es) 2014-05-02

Family

ID=47746797

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20140085A CR20140085A (es) 2011-08-25 2014-02-24 Inhibidores de pde10 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)
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)
PH (1) PH12014500424A1 (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)

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EP2763533B1 (en) 2011-10-06 2021-12-29 Merck Sharp & Dohme Corp. Triazolyl pde10 inhibitors
CA2851082A1 (en) 2011-10-06 2013-04-11 Merck Sharp & Dohme Corp. 1,3-substituted azetidine pde10 inhibitors
WO2014078216A1 (en) 2012-11-15 2014-05-22 Merck Sharp & Dohme Corp. Cyclobutyl benzimidazoles as pde10 inhibitors
US9359348B2 (en) 2012-11-15 2016-06-07 Merck Sharp & Dohme Corp. Cyclopropyl imidazopyridine PDE10 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
US9663513B2 (en) 2012-11-20 2017-05-30 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
WO2015148379A1 (en) 2014-03-24 2015-10-01 Novartis Ag Monobactam organic compounds for the treatment of bacterial infections
WO2018095877A1 (en) * 2016-11-28 2018-05-31 Boehringer Ingelheim International Gmbh Indanylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
WO2020002280A1 (en) 2018-06-27 2020-01-02 F. Hoffmann-La Roche Ag Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
CN116640118B (zh) 2018-06-27 2025-12-19 豪夫迈·罗氏有限公司 放射性标记的大麻素受体2配体
CN119161323A (zh) 2018-06-27 2024-12-20 豪夫迈·罗氏有限公司 作为大麻素受体2的抑制剂的新型吡啶和吡嗪化合物
MX2022015400A (es) * 2020-06-05 2023-03-16 Noema Pharma Ag Uso del inhibidor de la fosfodiesterasa a 10 para el tratamiento del sindrome de tourette.
US12544364B2 (en) 2020-06-05 2026-02-10 Noema Pharma Ag Use of a phosphodiesterase 10 inhibitor for the treatment of tourette syndrome
CN117295731A (zh) * 2021-03-17 2023-12-26 默沙东有限责任公司 Pde10化合物的前药
US20250188057A1 (en) * 2022-03-11 2025-06-12 Merck Sharp & Dohme Llc Non-aromatic cyclic-pyrimidine analogs as glucosylceramide synthase inhibitors
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
US20260060983A1 (en) * 2022-08-31 2026-03-05 Merck Sharp & Dohme Llc Sustained release delivery of a pde10 inhibitor
CN120187717A (zh) * 2022-11-11 2025-06-20 杭州中美华东制药有限公司 1,5-萘啶类cGAS抑制剂及其用途
AU2024247059A1 (en) * 2023-03-29 2025-10-30 Merck Sharp & Dohme (Uk) Limited Controlled release pde10a formulations

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EP1755611A1 (en) 2004-06-07 2007-02-28 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
ATE472543T1 (de) 2005-01-07 2010-07-15 Pfizer Prod Inc Heteroaromatische chinolinverbindungen und deren verwendung als pde10-inhibitoren
GB0506883D0 (en) * 2005-04-05 2005-05-11 Astrazeneca Ab Chemical compounds
SI1869032T1 (sl) * 2005-04-05 2008-12-31 Astrazeneca Ab Pirimidinski derivati za uporabo kot sredstva proti raku
NL2000397C2 (nl) * 2006-01-05 2007-10-30 Pfizer Prod Inc Bicyclische heteroarylverbindingen als PDE10 inhibitoren.
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JPWO2010024258A1 (ja) * 2008-08-29 2012-01-26 塩野義製薬株式会社 Pi3k阻害活性を有する縮環アゾール誘導体
JP5290406B2 (ja) 2008-09-04 2013-09-18 田辺三菱製薬株式会社 三置換ピリミジン化合物及びそのpde10阻害薬としての使用
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Also Published As

Publication number Publication date
MA35508B1 (fr) 2014-10-02
JP5648147B2 (ja) 2015-01-07
KR20140053356A (ko) 2014-05-07
IL230997A0 (en) 2014-03-31
PE20141535A1 (es) 2014-11-06
WO2013028590A1 (en) 2013-02-28
PL2748151T3 (pl) 2016-09-30
IL230997A (en) 2015-08-31
MY157301A (en) 2016-05-31
CL2014000450A1 (es) 2014-08-22
US20140228368A1 (en) 2014-08-14
TW201313699A (zh) 2013-04-01
DK2748151T3 (en) 2016-07-04
BR112014004310B8 (pt) 2023-04-18
BR112014004310B1 (pt) 2022-03-03
ME02419B (me) 2016-09-20
ES2572527T3 (es) 2016-06-01
AU2012299080B2 (en) 2016-03-17
EP2748151A1 (en) 2014-07-02
HK1193410A1 (zh) 2014-09-19
SG2014013536A (en) 2014-07-30
UA109735C2 (xx) 2015-09-25
CN103917528A (zh) 2014-07-09
RS54788B1 (sr) 2016-10-31
BR112014004310A2 (pt) 2017-03-28
EP2748151B1 (en) 2016-03-16
CA2845578C (en) 2016-02-16
EP2748151A4 (en) 2015-01-07
HUE028451T2 (en) 2016-12-28
CN103917528B (zh) 2016-04-20
JP2014524471A (ja) 2014-09-22
US9062059B2 (en) 2015-06-23
MX2014002178A (es) 2014-05-01
EA201490492A1 (ru) 2014-06-30
PH12014500424A1 (en) 2016-08-03
EA023685B1 (ru) 2016-06-30
AR087628A1 (es) 2014-04-09
NI201400014A (es) 2014-07-25
CY1117622T1 (el) 2017-04-26
CO6890101A2 (es) 2014-03-10
KR101655635B1 (ko) 2016-09-07
SI2748151T1 (sl) 2016-06-30
AU2012299080A1 (en) 2014-03-06
CA2845578A1 (en) 2013-02-28
HRP20160635T1 (hr) 2016-07-01
TN2014000070A1 (en) 2015-07-01
MX357241B (es) 2018-06-29
DOP2014000039A (es) 2014-06-01
TWI450895B (zh) 2014-09-01
NZ621245A (en) 2014-12-24
ZA201401272B (en) 2017-09-27

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