EA201591369A1 - Новые производные пиримидина в качестве ингибиторов фосфодиэстеразы 10 (pde-10) - Google Patents

Новые производные пиримидина в качестве ингибиторов фосфодиэстеразы 10 (pde-10)

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Publication number
EA201591369A1
EA201591369A1 EA201591369A EA201591369A EA201591369A1 EA 201591369 A1 EA201591369 A1 EA 201591369A1 EA 201591369 A EA201591369 A EA 201591369A EA 201591369 A EA201591369 A EA 201591369A EA 201591369 A1 EA201591369 A1 EA 201591369A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pde
inhibitors
new
phosphodesterase
inhibitor
Prior art date
Application number
EA201591369A
Other languages
English (en)
Other versions
EA026330B1 (ru
Inventor
Хуан Камачо Гомес
Хулио Кастро Паломино Лария
Original Assignee
Палобиофарма С.Л
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.)
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Publication date
Application filed by Палобиофарма С.Л filed Critical Палобиофарма С.Л
Publication of EA201591369A1 publication Critical patent/EA201591369A1/ru
Publication of EA026330B1 publication Critical patent/EA026330B1/ru

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    • 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
    • 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
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    • 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

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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)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Настоящее изобретение относится к новым производным пиримидина формулы (I) в качестве ингибиторов фермента фосфодиэстеразы 10 (PDE-10), фармацевтическим композициям, содержащим эффективное количество таких соединений, и к использованию соединений для производства лекарственного средства для лечения патологических состояний или заболеваний, состояние которых можно улучшать ингибированием фермента фосфодиэстеразы 10, таких как неврологические, психиатрические, респираторные или метаболические заболевания.
EA201591369A 2013-01-24 2014-01-23 Новые производные пиримидина в качестве ингибиторов фосфодиэстеразы 10 (pde-10) EA026330B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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 (2)

Publication Number Publication Date
EA201591369A1 true EA201591369A1 (ru) 2016-01-29
EA026330B1 EA026330B1 (ru) 2017-03-31

Family

ID=50071592

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201591369A EA026330B1 (ru) 2013-01-24 2014-01-23 Новые производные пиримидина в качестве ингибиторов фосфодиэстеразы 10 (pde-10)

Country Status (23)

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

Families Citing this family (2)

* 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

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080221103A1 (en) 2007-03-09 2008-09-11 Orchid Research Laboratories Ltd. New heterocyclic compounds
AU2009345802B2 (en) 2009-05-07 2016-05-26 Forum Pharmaceuticals Inc. Phenoxymethyl heterocyclic compounds
US8492392B2 (en) 2009-05-27 2013-07-23 Merck Sharp & Dohme Corp. Alkoxy tetrahydro-pyridopyrimidine PDE10 inhibitors
JP6007102B2 (ja) 2009-06-24 2016-10-12 コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． 画像情報に基づいた構造の輪郭の決定
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
WO2011112828A1 (en) 2010-03-12 2011-09-15 Omeros Corporation Pde10 inhibitors and related compositions and methods
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
AU2012318874A1 (en) * 2011-10-06 2014-05-15 Merck Sharp & Dohme Corp. 1,3-substituted azetidine PDE10 inhibitors

Also Published As

Publication number Publication date
MX2015009627A (es) 2016-04-25
ES2611170T3 (es) 2017-05-05
MX361160B (es) 2018-11-28
ES2480341B1 (es) 2015-01-22
CY1118552T1 (el) 2017-07-12
US20150336953A1 (en) 2015-11-26
CA2897260A1 (en) 2014-07-31
JP2016505059A (ja) 2016-02-18
JP6254194B2 (ja) 2017-12-27
US9447095B2 (en) 2016-09-20
EP2948443B1 (en) 2016-08-31
SMT201600428B (it) 2017-01-10
DK2948443T3 (en) 2016-12-12
RS55449B1 (sr) 2017-04-28
CA2897260C (en) 2018-11-20
HUE031831T2 (en) 2017-08-28
KR20150126601A (ko) 2015-11-12
WO2014114695A1 (en) 2014-07-31
EP2948443A1 (en) 2015-12-02
ES2480341A1 (es) 2014-07-25
BR112015017678A2 (pt) 2017-07-11
KR101869144B1 (ko) 2018-07-19
ME02551B (me) 2017-02-20
HRP20161495T1 (hr) 2016-12-16
CN105008346A (zh) 2015-10-28
PL2948443T3 (pl) 2017-02-28
EA026330B1 (ru) 2017-03-31
BR112015017678B1 (pt) 2023-02-14
AU2014209950B2 (en) 2017-04-20
CN105008346B (zh) 2018-11-13
PT2948443T (pt) 2016-11-15
SI2948443T1 (sl) 2016-12-30
LT2948443T (lt) 2016-12-12
AU2014209950A1 (en) 2015-08-27

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