BRPI0408189A - 8'-piridinil-dihidroespiro-[cicloalquil]-pirimido[1,2-a]p irimidin-6-ona substituìda e derivados de 8'-pirimidinil-dihidroespiro-[cicloalquil]-pirimido[1,2- a]pirimidin-6-ona e seus usos contra doenças neurodegenerativas - Google Patents

8'-piridinil-dihidroespiro-[cicloalquil]-pirimido[1,2-a]p irimidin-6-ona substituìda e derivados de 8'-pirimidinil-dihidroespiro-[cicloalquil]-pirimido[1,2- a]pirimidin-6-ona e seus usos contra doenças neurodegenerativas

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Publication number
BRPI0408189A
BRPI0408189A BRPI0408189-7A BRPI0408189A BRPI0408189A BR PI0408189 A BRPI0408189 A BR PI0408189A BR PI0408189 A BRPI0408189 A BR PI0408189A BR PI0408189 A BRPI0408189 A BR PI0408189A
Authority
BR
Brazil
Prior art keywords
dihydrospiro
pyrimidin
cycloalkyl
ring
substituted
Prior art date
Application number
BRPI0408189-7A
Other languages
English (en)
Inventor
Pascal George
Alistair Lochead
Mourad Saady
Franck Slowinski
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
Application filed by Sanofi Aventis, Mitsubishi Pharma Corp filed Critical Sanofi Aventis
Publication of BRPI0408189A publication Critical patent/BRPI0408189A/pt

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    • 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • 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
    • 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
    • A61P25/14—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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
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    • 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
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    • A61P35/00—Antineoplastic agents
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    • A—HUMAN NECESSITIES
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    • 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

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  • Engineering & Computer Science (AREA)
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  • Psychiatry (AREA)
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  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"8<39>-PIRIDINIL-DIHIDROESPIRO-¢CICLOALQUIL!-PIRIMIDO¢1 ,2-A!PIRIMIDIN-6-ONA SUBSTITUìDA E DERIVADOS DE 8<39>-PIRIMIDINIL-DIHIDROESPIRO-¢CICLOALQUIL!-PIRIMIDO¢ 1,2A!PIRIMIDIN-6-ONA E SEUS USOS CONTRA DOENçAS NEURODEGENERATIVAS". A invenção refere-se a um derivado de dihidroespiro-¢cicloalquil!pirimidona representado pela fórmula (I) ou um seu sal onde: X representa dois átomos de hidrogênio, um átomo de enxofre, um átomo de oxigênio ou um grupo C~ 1-2~ alquila e um átomo de hidrogênio; Y representa uma ligação, um grupo carbonila, um grupo metileno opcionalmente substituído; Rl representa um anel 2, 3 ou 4-piridina ou um anel 2, 4 ou 5-pirimidina, o anel sendo opcionalmente substituído; R2 representa um anel benzeno ou um anel naftaleno; os anéis sendo opcionalmente substituídos; R3 representa um átomo de hidrogênio, um grupo C~ 1-6~ alquila ou um átomo de halogênio; m representa 1 a 4; n representa O a 3; p representa O a 2; q representa O a 2, p+q sendo inferior a 4. A invenção refere-se também a um medicamento compreendendo o dito derivado ou um seu sal como um ingrediente ativo que é usado para tratamento preventivo e/ou terapêutico de uma doença neurodegenerativa causada por atividade anormal de GSK3<225>, tal como doença de Alzheimer.
BRPI0408189-7A 2003-03-07 2004-03-05 8'-piridinil-dihidroespiro-[cicloalquil]-pirimido[1,2-a]p irimidin-6-ona substituìda e derivados de 8'-pirimidinil-dihidroespiro-[cicloalquil]-pirimido[1,2- a]pirimidin-6-ona e seus usos contra doenças neurodegenerativas BRPI0408189A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03290569A EP1454909B1 (en) 2003-03-07 2003-03-07 8'-pyridinyl-dihydrospiro- (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one and 8'-pyrimidinyl-dihydrospiro (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one derivatives and their use against neurodegenerative diseases
PCT/EP2004/003051 WO2004078760A1 (en) 2003-03-07 2004-03-05 SUBSTITUTED 8'-PYRIDINYL-DIHYDROSPIRO-[CYCLOALKYL]-PYRIMIDO [1,2-a] PYRIMIDIN-6-ONE AND 8'-PYRIMIDINYL-DIHYDROSPIRO-[CYCLOALKYL]-PYRIMIDO [1,2-a] PYRIMIDIN-6-ONE DERIVATIVES AND THEIR USE AGAINST NEUROGENERATIVE DISEASES

Publications (1)

Publication Number Publication Date
BRPI0408189A true BRPI0408189A (pt) 2006-03-21

Family

ID=32799103

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0408189-7A BRPI0408189A (pt) 2003-03-07 2004-03-05 8'-piridinil-dihidroespiro-[cicloalquil]-pirimido[1,2-a]p irimidin-6-ona substituìda e derivados de 8'-pirimidinil-dihidroespiro-[cicloalquil]-pirimido[1,2- a]pirimidin-6-ona e seus usos contra doenças neurodegenerativas

Country Status (25)

Country Link
US (2) US7294632B2 (pt)
EP (2) EP1454909B1 (pt)
JP (1) JP4639182B2 (pt)
KR (1) KR101069984B1 (pt)
CN (1) CN100463908C (pt)
AR (1) AR043485A1 (pt)
AT (1) ATE469153T1 (pt)
AU (1) AU2004218250B2 (pt)
BR (1) BRPI0408189A (pt)
CA (1) CA2516937C (pt)
CY (1) CY1111057T1 (pt)
DE (1) DE602004027354D1 (pt)
DK (1) DK1603915T3 (pt)
EA (1) EA008172B1 (pt)
ES (1) ES2346311T3 (pt)
IL (1) IL170461A (pt)
MX (1) MXPA05009574A (pt)
NO (1) NO20054140L (pt)
NZ (1) NZ542135A (pt)
PL (1) PL1603915T3 (pt)
PT (1) PT1603915E (pt)
SI (1) SI1603915T1 (pt)
TW (1) TWI320785B (pt)
WO (1) WO2004078760A1 (pt)
ZA (1) ZA200507107B (pt)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008543844A (ja) * 2005-06-14 2008-12-04 シェーリング コーポレイション アスパルチルプロテアーゼ阻害剤
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス,インコーポレイティド ムスカリン性受容体調節による神経発生
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
US7985756B2 (en) 2005-10-21 2011-07-26 Braincells Inc. Modulation of neurogenesis by PDE inhibition
WO2007053596A1 (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
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
EP1992620A1 (en) * 2007-05-16 2008-11-19 Sanofi-Aventis Arylamide pyrimidone derivatives for the treatment of neurodegenerative diseases
EP1992625A1 (en) * 2007-05-16 2008-11-19 Sanofi-Aventis Arylamide pyrimidone compounds
EP1992621A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Heteroarylamide-substituted pyrimidone derivatives for the treatment of neurodegenerative diseases
EP1992624A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Heteroarylamide pyrimidone compounds
EP2138493A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidone derivatives
EP2138495A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted pyrimido[2,1-a]isoquinolin-4-one derivatives
EP2138494A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted alkyl pyrimidin-4-one derivatives
EP2138485A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted N-Oxide pyrazine derivatives
EP2138492A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidin-4-one derivatives
EP2138498A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted tricyclic derivatives against neurodegenerative diseases
EP2138488A1 (en) 2008-06-26 2009-12-30 sanofi-aventis 4-(pyridin-4-yl)-1H-[1,3,5]triazin-2-one derivatives as GSK3-beta inhibitors for the treatment of neurodegenerative diseases
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
MX2012000103A (es) 2009-07-02 2012-05-22 Sanofi Sa Nuevos derivados de 1,2,3,4-tetrahidro-pirimido (1,2-a) pirimidin-6-ona, su preparacion y su uso farmaceutica.
US8815853B2 (en) 2010-12-23 2014-08-26 Sanofi Pyrimidinone derivatives, preparation thereof and pharmaceutical use thereof
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
FR2992316A1 (fr) 2012-06-22 2013-12-27 Sanofi Sa Derives de pyrimidinones, leur preparation et leur application en therapeutique
US20170165230A1 (en) 2014-04-09 2017-06-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity

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FR2812636A1 (fr) * 2000-08-02 2002-02-08 Novapharme Nouveaux derives 2-phenyl imidazo[1.2-a]pyrimidin-5-ones et 2-phenyl 2,3-dihydro imidazo[1,2-a]pyrimidin-5-ones
AU1224902A (en) * 2000-09-01 2002-03-13 Sanofi Synthelabo 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
EP1184385A1 (en) * 2000-09-01 2002-03-06 Sanofi-Synthelabo 1-[Alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-pyridin-4-yl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one derivatives
EP1184383A1 (en) * 2000-09-01 2002-03-06 Sanofi-Synthelabo 9-[Alkyl], 9-[(heteroaryl)alkyl] and 9-[(aryl)alkyl]-2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
NZ547205A (en) * 2001-09-21 2007-11-30 Sanofi Aventis Intermediates of 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
DE60206946T2 (de) * 2001-09-21 2006-07-27 Sanofi-Aventis Substituierte 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-on- und 7-pyrimidinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1h)onderivate gegen neurodegenerative erkrankungen
EP1295885A1 (en) * 2001-09-21 2003-03-26 Sanofi-Synthelabo 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
EP1295884A1 (en) * 2001-09-21 2003-03-26 Sanofi-Synthelabo 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

Also Published As

Publication number Publication date
MXPA05009574A (es) 2006-05-19
WO2004078760A1 (en) 2004-09-16
EA008172B1 (ru) 2007-04-27
EP1603915A1 (en) 2005-12-14
US7507743B2 (en) 2009-03-24
CN1777607A (zh) 2006-05-24
DE602004027354D1 (de) 2010-07-08
PT1603915E (pt) 2010-07-22
ATE469153T1 (de) 2010-06-15
AU2004218250A1 (en) 2004-09-16
KR101069984B1 (ko) 2011-10-04
NO20054140L (no) 2005-12-02
US7294632B2 (en) 2007-11-13
TWI320785B (en) 2010-02-21
KR20050106500A (ko) 2005-11-09
EP1454909B1 (en) 2008-08-20
PL1603915T3 (pl) 2010-10-29
DK1603915T3 (da) 2010-08-30
JP4639182B2 (ja) 2011-02-23
NO20054140D0 (no) 2005-09-06
AU2004218250B2 (en) 2010-02-25
CA2516937A1 (en) 2004-09-16
AR043485A1 (es) 2005-08-03
SI1603915T1 (sl) 2010-08-31
CA2516937C (en) 2011-10-25
HK1085740A1 (en) 2006-09-01
EP1454909A1 (en) 2004-09-08
CY1111057T1 (el) 2015-06-11
CN100463908C (zh) 2009-02-25
JP2006519814A (ja) 2006-08-31
TW200510418A (en) 2005-03-16
EA200501241A1 (ru) 2006-04-28
IL170461A (en) 2011-11-30
ZA200507107B (en) 2006-11-29
US20060025431A1 (en) 2006-02-02
US20080081819A1 (en) 2008-04-03
ES2346311T3 (es) 2010-10-14
NZ542135A (en) 2008-06-30
EP1603915B1 (en) 2010-05-26

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