JP6254194B2 - ホスホジエステラーゼ１０阻害剤（ｐｄｅ−１０）としての新規ピリミジン誘導体 - Google Patents

ホスホジエステラーゼ１０阻害剤（ｐｄｅ−１０）としての新規ピリミジン誘導体 Download PDF

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JP6254194B2
JP6254194B2 JP2015554139A JP2015554139A JP6254194B2 JP 6254194 B2 JP6254194 B2 JP 6254194B2 JP 2015554139 A JP2015554139 A JP 2015554139A JP 2015554139 A JP2015554139 A JP 2015554139A JP 6254194 B2 JP6254194 B2 JP 6254194B2
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bromo
diamine
pyrimidine
pyrazol
group
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JP2016505059A5 (enExample
JP2016505059A (ja
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フアン、カマチョ、ゴメス
フリオ、カストロ、パロミノ、ラリア
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Palobiofarma SL
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Palobiofarma SL
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2015554139A 2013-01-24 2014-01-23 ホスホジエステラーゼ１０阻害剤（ｐｄｅ−１０）としての新規ピリミジン誘導体 Active JP6254194B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ESP201330082 2013-01-24
ES201330082A ES2480341B1 (es) 2013-01-24 2013-01-24 Nuevos derivados de pirimidina como inhibidores de la fosfodiesterasa 10 (PDE-10)
PCT/EP2014/051290 WO2014114695A1 (en) 2013-01-24 2014-01-23 New pyrimidine derivatives as phosphodiesterase 10 inhibitors (pde-10)

Publications (3)

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JP2016505059A JP2016505059A (ja) 2016-02-18
JP2016505059A5 JP2016505059A5 (enExample) 2017-12-21
JP6254194B2 true JP6254194B2 (ja) 2017-12-27

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JP2015554139A Active JP6254194B2 (ja) 2013-01-24 2014-01-23 ホスホジエステラーゼ１０阻害剤（ｐｄｅ−１０）としての新規ピリミジン誘導体

Country Status (23)

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US (1) US9447095B2 (enExample)
EP (1) EP2948443B1 (enExample)
JP (1) JP6254194B2 (enExample)
KR (1) KR101869144B1 (enExample)
CN (1) CN105008346B (enExample)
AU (1) AU2014209950B2 (enExample)
BR (1) BR112015017678B1 (enExample)
CA (1) CA2897260C (enExample)
CY (1) CY1118552T1 (enExample)
DK (1) DK2948443T3 (enExample)
EA (1) EA026330B1 (enExample)
ES (2) ES2480341B1 (enExample)
HR (1) HRP20161495T1 (enExample)
HU (1) HUE031831T2 (enExample)
LT (1) LT2948443T (enExample)
ME (1) ME02551B (enExample)
MX (1) MX361160B (enExample)
PL (1) PL2948443T3 (enExample)
PT (1) PT2948443T (enExample)
RS (1) RS55449B1 (enExample)
SI (1) SI2948443T1 (enExample)
SM (1) SMT201600428B (enExample)
WO (1) WO2014114695A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017133657A1 (en) * 2016-02-05 2017-08-10 Savira Pharmaceuticals Gmbh Pyridine and pyrimidine derivatives and their use in treatment, amelioration or prevention of influenza
CN107286146B (zh) * 2017-07-05 2020-07-31 上海肇钰医药科技有限公司 作为腺苷a2a受体拮抗剂的4-氨基嘧啶衍生物及其用途
CN116836162B (zh) * 2023-05-24 2025-09-05 南方医科大学 吡唑[4,3-c]吡啶类化合物或其药学上可接受的盐及其应用

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008110891A2 (en) * 2007-03-09 2008-09-18 Orchid Research Laboratories Limited, New heterocyclic compounds
RU2531274C2 (ru) 2009-05-07 2014-10-20 Энвиво Фармасьютикалз, Инк. Феноксиметильные гетероциклические соединения
WO2010138430A1 (en) 2009-05-27 2010-12-02 Merck Sharp & Dohme Corp. Alkoxy tetrahydro-pyridopyrimidine pde10 inhibitors
EP2446416B1 (en) 2009-06-24 2014-04-30 Koninklijke Philips N.V. Establishing a contour of a structure based on image information
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
PT2544679T (pt) 2010-03-12 2019-07-11 Omeros Corp Inibidores de pde-10 e composições e métodos relacionados
EP2549875B1 (en) 2010-03-25 2015-05-13 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
ES2365960B1 (es) * 2010-03-31 2012-06-04 Palobiofarma, S.L Nuevos antagonistas de los receptores de adenosina.
CN103038229B (zh) 2010-05-26 2016-05-11 桑诺维恩药品公司 杂芳基化合物及其使用方法
US8592423B2 (en) 2011-06-21 2013-11-26 Bristol-Myers Squibb Company Inhibitors of PDE10
JP2014528446A (ja) * 2011-10-06 2014-10-27 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． １，３−置換アゼチジンｐｄｅ１０阻害剤

Also Published As

Publication number Publication date
BR112015017678B1 (pt) 2023-02-14
US9447095B2 (en) 2016-09-20
MX361160B (es) 2018-11-28
CN105008346B (zh) 2018-11-13
ES2611170T3 (es) 2017-05-05
SI2948443T1 (sl) 2016-12-30
KR20150126601A (ko) 2015-11-12
WO2014114695A1 (en) 2014-07-31
DK2948443T3 (en) 2016-12-12
SMT201600428B (it) 2017-01-10
ES2480341A1 (es) 2014-07-25
CY1118552T1 (el) 2017-07-12
CA2897260C (en) 2018-11-20
AU2014209950B2 (en) 2017-04-20
PT2948443T (pt) 2016-11-15
JP2016505059A (ja) 2016-02-18
HUE031831T2 (en) 2017-08-28
PL2948443T3 (pl) 2017-02-28
LT2948443T (lt) 2016-12-12
CN105008346A (zh) 2015-10-28
AU2014209950A1 (en) 2015-08-27
HRP20161495T1 (hr) 2016-12-16
CA2897260A1 (en) 2014-07-31
BR112015017678A2 (pt) 2017-07-11
ES2480341B1 (es) 2015-01-22
EA201591369A1 (ru) 2016-01-29
EP2948443B1 (en) 2016-08-31
KR101869144B1 (ko) 2018-07-19
MX2015009627A (es) 2016-04-25
ME02551B (me) 2017-02-20
RS55449B1 (sr) 2017-04-28
US20150336953A1 (en) 2015-11-26
EA026330B1 (ru) 2017-03-31
EP2948443A1 (en) 2015-12-02

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