MA35508B1 - Inhibiteurs pyrimidines de pde10 - Google Patents

Inhibiteurs pyrimidines de pde10

Info

Publication number
MA35508B1
MA35508B1 MA6829A MA36829A MA35508B1 MA 35508 B1 MA35508 B1 MA 35508B1 MA 6829 A MA6829 A MA 6829A MA 36829 A MA36829 A MA 36829A MA 35508 B1 MA35508 B1 MA 35508B1
Authority
MA
Morocco
Prior art keywords
pde10
treatment
relates
present
compounds
Prior art date
Application number
MA6829A
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 MA35508B1 publication Critical patent/MA35508B1/fr

Links

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
    • 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

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 présente invention concerne des composés pyrimidines qui sont utiles en tant qu'agents thérapeutiques pour le traitement de troubles du système nerveux central associés à la phosphodiestérase 10 (pde10). La présente invention concerne également l'utilisation de tels composés pour le traitement de troubles neurologiques et psychiatriques, tels que la schizophrénie, la psychose ou la maladie de huntington, et ceux associés à une hypofonction striatale ou d'un dysfonctionnement des noyaux gris centraux.
MA6829A 2011-08-25 2014-03-13 Inhibiteurs pyrimidines de pde10 MA35508B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161527392P 2011-08-25 2011-08-25
PCT/US2012/051522 WO2013028590A1 (fr) 2011-08-25 2012-08-20 Inhibiteurs pyrimidines de pde10

Publications (1)

Publication Number Publication Date
MA35508B1 true MA35508B1 (fr) 2014-10-02

Family

ID=47746797

Family Applications (1)

Application Number Title Priority Date Filing Date
MA6829A MA35508B1 (fr) 2011-08-25 2014-03-13 Inhibiteurs pyrimidines de pde10

Country Status (36)

Country Link
US (1) US9062059B2 (fr)
EP (1) EP2748151B1 (fr)
JP (1) JP5648147B2 (fr)
KR (1) KR101655635B1 (fr)
CN (1) CN103917528B (fr)
AR (1) AR087628A1 (fr)
AU (1) AU2012299080B2 (fr)
BR (1) BR112014004310B8 (fr)
CA (1) CA2845578C (fr)
CL (1) CL2014000450A1 (fr)
CO (1) CO6890101A2 (fr)
CR (1) CR20140085A (fr)
CY (1) CY1117622T1 (fr)
DK (1) DK2748151T3 (fr)
DO (1) DOP2014000039A (fr)
EA (1) EA023685B1 (fr)
ES (1) ES2572527T3 (fr)
HR (1) HRP20160635T1 (fr)
HU (1) HUE028451T2 (fr)
IL (1) IL230997A (fr)
MA (1) MA35508B1 (fr)
ME (1) ME02419B (fr)
MX (1) MX357241B (fr)
MY (1) MY157301A (fr)
NI (1) NI201400014A (fr)
PE (1) PE20141535A1 (fr)
PH (1) PH12014500424A1 (fr)
PL (1) PL2748151T3 (fr)
RS (1) RS54788B1 (fr)
SG (1) SG2014013536A (fr)
SI (1) SI2748151T1 (fr)
TN (1) TN2014000070A1 (fr)
TW (1) TWI450895B (fr)
UA (1) UA109735C2 (fr)
WO (1) WO2013028590A1 (fr)
ZA (1) ZA201401272B (fr)

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Publication number Priority date Publication date Assignee Title
WO2013052526A1 (fr) 2011-10-06 2013-04-11 Merck Sharp & Dohme Corp. Inhibiteurs triazolyles de pde10
AU2012318874A1 (en) 2011-10-06 2014-05-15 Merck Sharp & Dohme Corp. 1,3-substituted azetidine 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
EP2919783B1 (fr) * 2012-11-15 2018-01-31 Merck Sharp & Dohme Corp. Cyclopropylimidazopyridine utilisable en tant qu'inhibiteur de pde10
WO2014081617A1 (fr) 2012-11-20 2014-05-30 Merck Sharp & Dohme Corp. Dérivés de pyridone substitués utilisés en tant qu'inhibiteurs de pde10
EP2922823B1 (fr) * 2012-11-20 2018-10-31 Merck Sharp & Dohme Corp. Inhibiteurs pyrimidines de pde10
WO2014139150A1 (fr) * 2013-03-15 2014-09-18 Merck Sharp & Dohme Corp. Dérivés de pyridizinone substitués utilisés en tant qu'inhibiteurs de la pde10
MX373444B (es) 2014-03-24 2020-04-30 Novartis Ag Compuestos organicos de monobactam para el tratamiento de infecciones bacterianas.
JP7008704B2 (ja) * 2016-11-28 2022-01-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング インダニルアミノピリジルシクロプロパンカルボン酸、その医薬組成物及び使用
JP7478672B2 (ja) 2018-06-27 2024-05-07 エフ. ホフマン-ラ ロシュ アーゲー カンナビノイド受容体2の阻害剤としての新規なアゼチジン置換ピリジン及びピラジン化合物
CN112638430B (zh) 2018-06-27 2023-05-16 豪夫迈·罗氏有限公司 放射性标记的大麻素受体2配体
CA3096777A1 (fr) 2018-06-27 2020-02-02 F. Hoffmann-La Roche Ag Nouveaux composes de pyridine et de pyrazine en tant qu'inhibiteurs du recepteur cannabinoide 2
US12544364B2 (en) 2020-06-05 2026-02-10 Noema Pharma Ag Use of a phosphodiesterase 10 inhibitor for the treatment of tourette syndrome
CN116137811B (zh) * 2020-06-05 2026-01-09 诺埃玛制药公司 用于治疗杜尔雷斯综合征的磷酸二酯酶10抑制剂的用途
IL305923A (en) * 2021-03-17 2023-11-01 Merck Sharp & Dohme Llc Prodrugs for PDE10 compounds
EP4490148A4 (fr) * 2022-03-11 2026-03-18 Merck Sharp & Dohme Llc Analogues de pyrimidine cycliques non aromatiques utilisés en tant qu'inhibiteurs de glucosylcéramide synthase
WO2023192170A1 (fr) * 2022-04-01 2023-10-05 Merck Sharp & Dohme Llc Procédé de préparation de ((1s,2s)-2-(5-méthylpyridin-2-yl)cyclopropyl)méthanol
WO2023184486A1 (fr) * 2022-04-01 2023-10-05 Merck Sharp & Dohme Llc Procédé de préparation de ((1s, 2s)-2-(5-méthylpyridin-2-yl)cyclopropyl)-méthanol
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 (fr) * 2022-08-31 2024-03-07 Merck Sharp & Dohme Llc Administration à libération prolongée d'un inhibiteur de pde10
WO2024099135A1 (fr) * 2022-11-11 2024-05-16 杭州中美华东制药有限公司 Inhibiteur de 1,5-naphtyridine cgas et son utilisation
CN120936353A (zh) * 2023-03-29 2025-11-11 默沙东有限责任公司 控释pde10a制剂

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EP1755611A1 (fr) 2004-06-07 2007-02-28 Pfizer Products Inc. Inhibition de la phosphodiesterase 10 dans le traitement des etats pathologiques associes a l'obesite et au syndrome metabolique
CA2583654C (fr) 2004-10-12 2015-02-17 Maxlinear, Inc. Architecture de recepteur a frequence intermediaire generee numeriquement
KR100896380B1 (ko) 2005-01-07 2009-05-08 화이자 프로덕츠 인코포레이티드 헤테로방향족 퀴놀린 화합물 및 pde10 저해제로서의그의 용도
GB0506883D0 (en) * 2005-04-05 2005-05-11 Astrazeneca Ab Chemical compounds
JP2008534662A (ja) * 2005-04-05 2008-08-28 アストラゼネカ アクチボラグ 抗癌剤として使用されるピリミジン誘導体
NL2000397C2 (nl) * 2006-01-05 2007-10-30 Pfizer Prod Inc Bicyclische heteroarylverbindingen als PDE10 inhibitoren.
US20090176829A1 (en) 2006-05-02 2009-07-09 Pfizer Inc Bicyclic heteroaryl compounds as pde10 inhibitors
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MX2011002399A (es) 2008-09-04 2011-04-07 Mitsubishi Tanabe Pharma Corp Compuestos pirimidina tri-sustituida y su uso como inhibidores de fosfodiesterasa 10.
EP2342191B1 (fr) 2008-09-10 2013-03-20 Mitsubishi Tanabe Pharma Corporation Composés cycliques aromatiques azotés à 6 chaînons et leur utilisation
TW201030001A (en) * 2008-11-14 2010-08-16 Amgen Inc Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors
ES2397934T3 (es) * 2008-12-17 2013-03-12 Amgen Inc. Compuestos de aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10
WO2011008931A2 (fr) * 2009-07-15 2011-01-20 Cystic Fibrosis Foundation Therapeutics, Inc. Composés arylpyrimidines et thérapie de combinaison comprenant ceux-ci pour traiter une mucoviscidose et des troubles apparentés
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
WO2012044561A2 (fr) * 2010-09-30 2012-04-05 Merck Sharp & Dohme Corp. Inhibiteurs de 2-alcoxy pyrimidine pde10
WO2012044562A2 (fr) * 2010-09-30 2012-04-05 Merck Sharp & Dohme Corp. Inhibiteurs de pyrazolopyrimidine pde10

Also Published As

Publication number Publication date
BR112014004310B1 (pt) 2022-03-03
CO6890101A2 (es) 2014-03-10
US20140228368A1 (en) 2014-08-14
EP2748151A1 (fr) 2014-07-02
ZA201401272B (en) 2017-09-27
EA201490492A1 (ru) 2014-06-30
AU2012299080B2 (en) 2016-03-17
SI2748151T1 (sl) 2016-06-30
CN103917528A (zh) 2014-07-09
CR20140085A (es) 2014-05-02
BR112014004310A2 (pt) 2017-03-28
CA2845578A1 (fr) 2013-02-28
NI201400014A (es) 2014-07-25
EA023685B1 (ru) 2016-06-30
MY157301A (en) 2016-05-31
ES2572527T3 (es) 2016-06-01
US9062059B2 (en) 2015-06-23
ME02419B (fr) 2016-09-20
TWI450895B (zh) 2014-09-01
IL230997A0 (en) 2014-03-31
KR101655635B1 (ko) 2016-09-07
HRP20160635T1 (hr) 2016-07-01
UA109735C2 (xx) 2015-09-25
WO2013028590A1 (fr) 2013-02-28
JP5648147B2 (ja) 2015-01-07
DK2748151T3 (en) 2016-07-04
DOP2014000039A (es) 2014-06-01
CL2014000450A1 (es) 2014-08-22
KR20140053356A (ko) 2014-05-07
MX357241B (es) 2018-06-29
JP2014524471A (ja) 2014-09-22
CN103917528B (zh) 2016-04-20
EP2748151A4 (fr) 2015-01-07
PH12014500424A1 (en) 2016-08-03
PL2748151T3 (pl) 2016-09-30
RS54788B1 (sr) 2016-10-31
CA2845578C (fr) 2016-02-16
TN2014000070A1 (en) 2015-07-01
PE20141535A1 (es) 2014-11-06
IL230997A (en) 2015-08-31
MX2014002178A (es) 2014-05-01
NZ621245A (en) 2014-12-24
BR112014004310B8 (pt) 2023-04-18
HUE028451T2 (en) 2016-12-28
EP2748151B1 (fr) 2016-03-16
AR087628A1 (es) 2014-04-09
CY1117622T1 (el) 2017-04-26
TW201313699A (zh) 2013-04-01
AU2012299080A1 (en) 2014-03-06
SG2014013536A (en) 2014-07-30
HK1193410A1 (zh) 2014-09-19

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