TWI320785B - Dihydrospiro-[cycloalkyl]-pyrimidone derivatives and the use thereof - Google Patents

Dihydrospiro-[cycloalkyl]-pyrimidone derivatives and the use thereof Download PDF

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Publication number
TWI320785B
TWI320785B TW093105914A TW93105914A TWI320785B TW I320785 B TWI320785 B TW I320785B TW 093105914 A TW093105914 A TW 093105914A TW 93105914 A TW93105914 A TW 93105914A TW I320785 B TWI320785 B TW I320785B
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TW
Taiwan
Prior art keywords
group
dihydrospiro
pyrimidin
pyrimido
pyrimidine
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TW093105914A
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English (en)
Chinese (zh)
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TW200510418A (en
Inventor
Pascal George
Alistair Lochead
Mourad Saady
Franck Slowinski
Philippe Yaiche
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Sanofi Aventis
Mitsubishi Pharma Corp
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Publication of TW200510418A publication Critical patent/TW200510418A/zh
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    • 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
    • C07D487/10Spiro-condensed systems
    • 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P25/24Antidepressants
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW093105914A 2003-03-07 2004-03-05 Dihydrospiro-[cycloalkyl]-pyrimidone derivatives and the use thereof TWI320785B (en)

Applications Claiming Priority (1)

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 derivatives -one and their use against neurodegenerative diseases

Publications (2)

Publication Number Publication Date
TW200510418A TW200510418A (en) 2005-03-16
TWI320785B true TWI320785B (en) 2010-02-21

Family

ID=32799103

Family Applications (1)

Application Number Title Priority Date Filing Date
TW093105914A TWI320785B (en) 2003-03-07 2004-03-05 Dihydrospiro-[cycloalkyl]-pyrimidone derivatives and the use thereof

Country Status (25)

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

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20080025079A (ko) 2005-06-14 2008-03-19 쉐링 코포레이션 아스파르틸 프로테아제 억제제
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
US7678363B2 (en) 2005-08-26 2010-03-16 Braincells Inc Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs
WO2007047978A2 (en) 2005-10-21 2007-04-26 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
CA2651813A1 (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
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
EP2138495A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted pyrimido[2,1-a]isoquinolin-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
EP2138492A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidin-4-one derivatives
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
SI2448940T1 (sl) 2009-07-02 2014-10-30 Sanofi Derivati 6,7,8,9-tetrahidro-pirimido(1,2-a)pirimidin-4-ona, njihova priprava in njihova farmacevtska uporaba
WO2012085244A1 (fr) 2010-12-23 2012-06-28 Sanofi Derives de pyrimidinone, leur preparation et leur utilisation pharmaceutique
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
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
ATE269333T1 (de) * 2000-09-01 2004-07-15 Sanofi Synthelabo 2-pyridinyl-6,7,8,9-tetrahydropyrimido(1,2- a)pyrimidin-4-on- und 7-pyridinyl-2,3- dihydroimidazo(1,2-a)pyrimidin-5 1honderivate
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
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
KR100868840B1 (ko) * 2001-09-21 2008-11-14 사노피-아벤티스 신경퇴행성 장애를 위한 치환된2-피리미디닐-6,7,8,9-테트라히드로피리미도[1,2-a]피리미딘-4-온 및7-피리미디닐-2,3-디히드로이미다조[1,2-a]피리미딘-5(1h)온 유도체
DE60227718D1 (de) * 2001-09-21 2008-08-28 Sanofi Aventis Verwendung von 2-Fuoro-3-Ketoestern zur Herstellung von 3-Fuoro-6,7,8,9-tetrahydro-4H-pyrimidoÄ1,2-aÜpyrimidin-4-onen
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

Also Published As

Publication number Publication date
KR20050106500A (ko) 2005-11-09
AU2004218250A1 (en) 2004-09-16
HK1085740A1 (en) 2006-09-01
CY1111057T1 (el) 2015-06-11
CN1777607A (zh) 2006-05-24
DK1603915T3 (da) 2010-08-30
IL170461A (en) 2011-11-30
TW200510418A (en) 2005-03-16
CA2516937A1 (en) 2004-09-16
AR043485A1 (es) 2005-08-03
JP2006519814A (ja) 2006-08-31
EP1454909A1 (en) 2004-09-08
MXPA05009574A (es) 2006-05-19
EP1603915A1 (en) 2005-12-14
AU2004218250B2 (en) 2010-02-25
EP1454909B1 (en) 2008-08-20
ES2346311T3 (es) 2010-10-14
US7294632B2 (en) 2007-11-13
NO20054140L (no) 2005-12-02
SI1603915T1 (sl) 2010-08-31
NO20054140D0 (no) 2005-09-06
KR101069984B1 (ko) 2011-10-04
PL1603915T3 (pl) 2010-10-29
PT1603915E (pt) 2010-07-22
JP4639182B2 (ja) 2011-02-23
NZ542135A (en) 2008-06-30
CN100463908C (zh) 2009-02-25
DE602004027354D1 (de) 2010-07-08
EP1603915B1 (en) 2010-05-26
ATE469153T1 (de) 2010-06-15
BRPI0408189A (pt) 2006-03-21
US20060025431A1 (en) 2006-02-02
US20080081819A1 (en) 2008-04-03
US7507743B2 (en) 2009-03-24
EA008172B1 (ru) 2007-04-27
WO2004078760A1 (en) 2004-09-16
EA200501241A1 (ru) 2006-04-28
CA2516937C (en) 2011-10-25
ZA200507107B (en) 2006-11-29

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