BR0308109A - Derivados 2-piridinil e 2-pirimidinil-6,7,8,9-tetraidro-pirimido[1,2-a] pirimidin-4-ona substituìdos com hetero arila - Google Patents

Derivados 2-piridinil e 2-pirimidinil-6,7,8,9-tetraidro-pirimido[1,2-a] pirimidin-4-ona substituìdos com hetero arila

Info

Publication number
BR0308109A
BR0308109A BR0308109-5A BR0308109A BR0308109A BR 0308109 A BR0308109 A BR 0308109A BR 0308109 A BR0308109 A BR 0308109A BR 0308109 A BR0308109 A BR 0308109A
Authority
BR
Brazil
Prior art keywords
atom
group
pyridinyl
pyrimidinyl
tetrahydro
Prior art date
Application number
BR0308109-5A
Other languages
English (en)
Inventor
Alistair Lochead
Alain Nedelec
Mourad Saady
Philippe Yaiche
Original Assignee
Sanofi Aventis
Mitsubishi Pharma Corp
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
Priority claimed from EP02290486A external-priority patent/EP1348708A1/en
Priority claimed from EP02290485A external-priority patent/EP1340758A1/en
Application filed by Sanofi Aventis, Mitsubishi Pharma Corp filed Critical Sanofi Aventis
Publication of BR0308109A publication Critical patent/BR0308109A/pt

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    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Addiction (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Agronomy & Crop Science (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Dentistry (AREA)

Abstract

"DERIVADOS 2-PIRIDINIL E 2-PIRIMIDINIL-6,7,8,9-TETRAIDRO-PIRIMIDO[1,2-AIPIRIMIDIN-4 -ONA SUBSTITUìDOS COM HETERO ARILA". A presente invenção refere-se a um derivado de pirimidona representado pela fórmula (1) ou um seu sal onde: (1) X representa dois átomos de hidrogênio, um átomo de enxofre, um átomo de oxigênio ou um grupo alquila C~ 1-2~ e um átomo de hidrogênio; Y representa uma ligação, um grupo etenileno, um grupo etinileno, ou um grupo metileno opcionalmente substituído; R1 representa um anel 2, 3 ou 4-piridina ou um anel 2, 4 ou 5-pirimidina opcionalmente substituído; R2 representa um anel bicíclico heterocíclico, tendo 1-4 heteroátomos selecionados de um átomo de oxigênio, um átomo de enxofre e um átomo de nitrogênio e tendo 5-9 átomos de carbono, de fórmula (II) R3 representa um átomo de hidrogênio, um grupo alquila C~ 1-6~, um grupo hidróxi, um grupo alcóxi C~ 1-4~ ou um átomo de halogênio; R4 representa um átomo de hidrogênio, um grupo alquila C~ 1-6~ um grupo alcóxi C~ 1-4~ ou um átomo de halogênio. A invenção refere-se também a um medicamento compreendendo o dito derivado ou um seu sal como um ingrediente ativo que é usado para o tratamento preventivo e/ou terapêutico de uma doença neurodegenerativa causada por anormal atividade de GSK3<225> ou GSK3<225> e cdk5/p25, tal como mal de Alzheimer.
BR0308109-5A 2002-02-28 2003-02-26 Derivados 2-piridinil e 2-pirimidinil-6,7,8,9-tetraidro-pirimido[1,2-a] pirimidin-4-ona substituìdos com hetero arila BR0308109A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP02290486A EP1348708A1 (en) 2002-02-28 2002-02-28 Heteroaryl substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives
EP02290485A EP1340758A1 (en) 2002-02-28 2002-02-28 Heteroaryl substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives
PCT/EP2003/002651 WO2003072579A1 (en) 2002-02-28 2003-02-26 HETEROARYL SUBSTITUTED 2-PYRIDINYL AND 2-PYRIMIDINYL -6,7,8,9- TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES

Publications (1)

Publication Number Publication Date
BR0308109A true BR0308109A (pt) 2005-01-04

Family

ID=27767034

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0308109-5A BR0308109A (pt) 2002-02-28 2003-02-26 Derivados 2-piridinil e 2-pirimidinil-6,7,8,9-tetraidro-pirimido[1,2-a] pirimidin-4-ona substituìdos com hetero arila

Country Status (22)

Country Link
US (2) US7232827B2 (pt)
EP (1) EP1480983B1 (pt)
JP (1) JP4458851B2 (pt)
KR (1) KR101030629B1 (pt)
CN (1) CN1315832C (pt)
AR (1) AR038619A1 (pt)
AT (1) ATE309247T1 (pt)
AU (1) AU2003221500B9 (pt)
BR (1) BR0308109A (pt)
CA (1) CA2474823C (pt)
DE (1) DE60302221T2 (pt)
DK (1) DK1480983T3 (pt)
EA (1) EA007737B1 (pt)
ES (1) ES2250883T3 (pt)
IL (1) IL163287A (pt)
MX (1) MXPA04008364A (pt)
NO (1) NO329805B1 (pt)
NZ (1) NZ534466A (pt)
PL (1) PL372465A1 (pt)
SI (1) SI1480983T1 (pt)
TW (1) TWI303637B (pt)
WO (1) WO2003072579A1 (pt)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1454910A1 (en) 2003-03-07 2004-09-08 Sanofi-Synthelabo Substituted pyrimidinyl-2-(diaza-bicyclo-alkyl)-pyrimidone derivatives
MXPA05009575A (es) 2003-03-07 2006-05-19 Sanofi Aventis Derivados de 2-(diaza-biciclo-alquil)-pirimidona substituidos.
EP1557417B1 (en) * 2003-12-19 2007-03-07 Sanofi-Aventis Substituted 8'-pyri(mi)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a] pyrimidin-6-one derivatives
WO2005083105A2 (en) * 2004-02-26 2005-09-09 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with glycogen synthase kinase 3 beta (gsk3b)
DE102004010194A1 (de) * 2004-03-02 2005-10-13 Aventis Pharma Deutschland Gmbh 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate, ihre Herstellung und Verwendung in Arzneimitteln
DE102004010207A1 (de) * 2004-03-02 2005-09-15 Aventis Pharma S.A. Neue 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate
EP2275095A3 (en) 2005-08-26 2011-08-17 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258357A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP2377530A3 (en) 2005-10-21 2012-06-20 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2382975A3 (en) 2006-05-09 2012-02-29 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
PT2448940E (pt) * 2009-07-02 2014-09-03 Sanofi Sa Derivados de 6,7,8,9-tetra-hidro-pirimido{1,2-α} pirimidin- 4-ona, sua preparação e sua utilização farmacêutica
JP5663571B2 (ja) * 2009-07-02 2015-02-04 サノフイ 新規２，３−ジヒドロ−１Ｈ−イミダゾ｛１，２−ａ｝ピリミジン−５−オン誘導体、これらの調製およびこれらの薬学的使用
FR2947551B1 (fr) * 2009-07-02 2012-05-18 Sanofi Aventis Nouveaux derives de 1,2,3,4-tetrahydro-pyrimido{1,2-a)pyrimidin-6-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb)
FR2947550B1 (fr) * 2009-07-02 2012-05-18 Sanofi Aventis Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb)
CN102715186A (zh) * 2012-06-15 2012-10-10 王学权 一种增效除草组合物
FR2992314B1 (fr) 2012-06-22 2015-10-16 Sanofi Sa Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique
BR112016022519A8 (pt) * 2014-04-01 2018-03-06 Pfizer cromeno e 1,1a,2,7b-tetra-hidrociclopropa[c]cromeno piridopirazinadionas como moduladores de gama-secretase
WO2015155738A2 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
US11130762B2 (en) * 2017-05-24 2021-09-28 Abbisko Therapeutics Co., Ltd. Azaaryl derivative, preparation method therefor, and application thereof for use in pharmacy

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW520362B (en) * 1996-12-05 2003-02-11 Amgen Inc Substituted pyrimidine compounds and pharmaceutical composition comprising same
AR023052A1 (es) 1998-09-25 2002-09-04 Mitsuharu Yoshimura Milton Derivados de pirimidona
ES2222396T3 (es) * 2000-09-01 2005-02-01 Sanofi-Aventis Compuestos utiles como ingrediente activo de un medicamento para el tratamiento preventivo y/o terapeutico de enfermedades neurodegenerativas.

Also Published As

Publication number Publication date
ES2250883T3 (es) 2006-04-16
EP1480983B1 (en) 2005-11-09
EP1480983A1 (en) 2004-12-01
JP4458851B2 (ja) 2010-04-28
CN1315832C (zh) 2007-05-16
EA007737B1 (ru) 2006-12-29
AU2003221500A1 (en) 2003-09-09
CA2474823C (en) 2011-02-22
NO329805B1 (no) 2010-12-20
TWI303637B (en) 2008-12-01
NO20043565L (no) 2004-11-25
AU2003221500B9 (en) 2008-11-20
AU2003221500C1 (en) 2008-10-02
CN1649871A (zh) 2005-08-03
KR20040087333A (ko) 2004-10-13
AU2003221500B2 (en) 2008-02-14
DE60302221D1 (de) 2005-12-15
DE60302221T2 (de) 2006-08-03
ATE309247T1 (de) 2005-11-15
DK1480983T3 (da) 2006-03-27
IL163287A (en) 2009-12-24
JP2005519086A (ja) 2005-06-30
TW200402421A (en) 2004-02-16
SI1480983T1 (sl) 2006-04-30
WO2003072579A1 (en) 2003-09-04
CA2474823A1 (en) 2003-09-04
MXPA04008364A (es) 2005-07-26
NZ534466A (en) 2006-04-28
US7232827B2 (en) 2007-06-19
US20070225300A1 (en) 2007-09-27
PL372465A1 (en) 2005-07-25
KR101030629B1 (ko) 2011-04-20
EA200400936A1 (ru) 2005-02-24
AR038619A1 (es) 2005-01-19
US20050222172A1 (en) 2005-10-06
US7465737B2 (en) 2008-12-16

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