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EA200500322A1 - COMPOUNDS OF DIHYDROPYRAZOLOPIRIDINE - Google Patents

COMPOUNDS OF DIHYDROPYRAZOLOPIRIDINE

Info

Publication number
EA200500322A1
EA200500322A1 EA200500322A EA200500322A EA200500322A1 EA 200500322 A1 EA200500322 A1 EA 200500322A1 EA 200500322 A EA200500322 A EA 200500322A EA 200500322 A EA200500322 A EA 200500322A EA 200500322 A1 EA200500322 A1 EA 200500322A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
present
dihydropyrazolopiridine
immunostimulants
gsk
Prior art date
Application number
EA200500322A
Other languages
Russian (ru)
Inventor
Тосиюки Кохара
Кендзи Фукунага
Токуси Ханано
Original Assignee
Мицубиси Фарма Корпорейшн
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 Мицубиси Фарма Корпорейшн filed Critical Мицубиси Фарма Корпорейшн
Publication of EA200500322A1 publication Critical patent/EA200500322A1/en

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P25/14—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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Настоящее изобретение относится к соединению дигидропиразолопиридина, представленого формулой (I), где каждый символ является таким, как определено в описании, его оптически активным формам, фармацевтически приемлемым солям и гидратам. Соединения по настоящему изобретению проявляют селективную и сильную ингибирующую активность по отношению к киназе-3 бета-гликогенсинтазы (GSK-3β) и применимы в качестве лекарственных средств для профилактики и/или лечения диабета, диабетических осложнений и нейродегенеративных заболеваний или в качестве иммуностимуляторов.Международная заявка была опубликована вместе с отчетом о международном поиске.The present invention relates to a dihydropyrazolopyridine compound represented by formula (I), wherein each symbol is as defined in the description, its optically active forms, pharmaceutically acceptable salts, and hydrates. The compounds of the present invention exhibit selective and strong inhibitory activity against beta-glycogen synthase kinase-3 (GSK-3β) and are useful as medicines for the prevention and / or treatment of diabetes, diabetic complications and neurodegenerative diseases or as immunostimulants. International application was published with the international search report.

EA200500322A 2002-08-07 2003-08-01 COMPOUNDS OF DIHYDROPYRAZOLOPIRIDINE EA200500322A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002230581 2002-08-07
PCT/JP2003/009787 WO2004014910A1 (en) 2002-08-07 2003-08-01 Dihydropyrazolopyridine compounds

Publications (1)

Publication Number Publication Date
EA200500322A1 true EA200500322A1 (en) 2005-08-25

Family

ID=31711689

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200500322A EA200500322A1 (en) 2002-08-07 2003-08-01 COMPOUNDS OF DIHYDROPYRAZOLOPIRIDINE

Country Status (14)

Country Link
EP (1) EP1537106A1 (en)
JP (1) JP2005534713A (en)
KR (1) KR20050069977A (en)
CN (1) CN1675209A (en)
AR (1) AR040961A1 (en)
AU (1) AU2003250539A1 (en)
BR (1) BR0313262A (en)
CA (1) CA2494785A1 (en)
EA (1) EA200500322A1 (en)
IL (1) IL166482A0 (en)
MX (1) MXPA05001434A (en)
NO (1) NO20051153L (en)
WO (1) WO2004014910A1 (en)
ZA (1) ZA200501842B (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2655171C2 (en) * 2013-04-05 2018-05-24 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Salt of pyrazoloquinoline derivative and crystal thereof
US11147803B2 (en) 2017-06-01 2021-10-19 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine
US11311530B2 (en) 2017-06-01 2022-04-26 Eisai R&D Management Co., Ltd. Lewy body disease therapeutic agent containing pyrazoloquinoline derivative
US11484502B2 (en) 2017-06-01 2022-11-01 Eisai R&D Management Co., Ltd. Pharmaceutical composition comprising PDE9 inhibitor
US11833146B2 (en) 2017-06-01 2023-12-05 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil

Families Citing this family (31)

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DE602006005242D1 (en) * 2005-06-27 2009-04-02 Sanofi Aventis PYRAZOLOPYRIDINE DERIVATIVES AS INHIBITORS OF KINASE 1 OF THE BETA ADRENEER RECEPTOR
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
BRPI0715160A2 (en) 2006-08-08 2013-06-11 Sanofi Aventis arylamimoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, drugs comprising these compounds, and their use
EP2025674A1 (en) 2007-08-15 2009-02-18 sanofi-aventis Substituted tetra hydro naphthalines, method for their manufacture and their use as drugs
CL2009001152A1 (en) 2008-05-13 2009-10-16 Array Biopharma Inc Compounds derived from n- (4- (nitrogen cycloalkyl-1-yl) -1h-pyrrolo [2,3-b] pyridin-3-yl) amide, kinase inhibitors; Preparation process; pharmaceutical composition; and its use for the treatment of a proliferative disease.
WO2010003624A2 (en) 2008-07-09 2010-01-14 Sanofi-Aventis Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
WO2010068601A1 (en) 2008-12-08 2010-06-17 Sanofi-Aventis A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof
CA2749884C (en) 2009-01-28 2018-01-23 Cara Therapeutics, Inc. Bicyclic pyrazolo-heterocycles
US7741350B1 (en) 2009-01-28 2010-06-22 Cara Therapeutics, Inc. Bicyclic pyrazolo-heterocycles
ES2443016T3 (en) 2009-08-26 2014-02-17 Sanofi New crystalline hydrates of heteroaromatic fluoroglycosides, pharmaceutical products comprising these compounds, and their use
FR2951172B1 (en) 2009-10-13 2014-09-26 Pf Medicament PYRAZOLOPYRIDINE DERIVATIVES AS ANTI-CANCER AGENT
WO2011107494A1 (en) 2010-03-03 2011-09-09 Sanofi Novel aromatic glycoside derivatives, medicaments containing said compounds, and the use thereof
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
WO2012120053A1 (en) 2011-03-08 2012-09-13 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8895547B2 (en) 2011-03-08 2014-11-25 Sanofi Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof
EP2683701B1 (en) 2011-03-08 2014-12-24 Sanofi Oxathiazine derivatives substituted with benzyl or heteromethylene groups, method for their preparation, their usage as medicament, medicament containing same and its use
EP2683698B1 (en) 2011-03-08 2017-10-04 Sanofi Benzyl-oxathiazine derivates substituted with adamantane or noradamantane, medicaments containing said compounds and use thereof
WO2012120055A1 (en) 2011-03-08 2012-09-13 Sanofi Di- and tri-substituted oxathiazine derivates, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2766349B1 (en) 2011-03-08 2016-06-01 Sanofi Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2683702B1 (en) 2011-03-08 2014-12-24 Sanofi New substituted phenyl oxathiazine derivatives, method for their manufacture, medicines containing these compounds and their application
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
SMT201800270T1 (en) 2013-12-13 2018-07-17 Daiichi Sankyo Co Ltd 5-hydroxy-4-(trifluoromethyl)pyrazolopyridine derivative
CN104140427A (en) * 2014-07-05 2014-11-12 湖南华腾制药有限公司 Preparation method of tetrahydropyrazolo[1,5-a]pyridine
CN111217754B (en) * 2018-11-23 2023-04-07 兰州大学 Preparation method of 5-amino-4-cyanopyrazole

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US4916140A (en) * 1988-09-28 1990-04-10 Merrell Dow Pharmaceuticals Inc. Antiepileptic pyrazolopyridines
AU4878601A (en) * 2000-04-20 2001-11-07 Mitsubishi Corporation Aromatic amide compounds
CA2437215A1 (en) * 2001-02-02 2002-08-15 Mitsubishi Pharma Corporation Dihydropyrazolopyridine compounds and pharmaceutical use thereof

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2655171C2 (en) * 2013-04-05 2018-05-24 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Salt of pyrazoloquinoline derivative and crystal thereof
US11147803B2 (en) 2017-06-01 2021-10-19 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine
US11311530B2 (en) 2017-06-01 2022-04-26 Eisai R&D Management Co., Ltd. Lewy body disease therapeutic agent containing pyrazoloquinoline derivative
US11484502B2 (en) 2017-06-01 2022-11-01 Eisai R&D Management Co., Ltd. Pharmaceutical composition comprising PDE9 inhibitor
US11833146B2 (en) 2017-06-01 2023-12-05 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil

Also Published As

Publication number Publication date
AU2003250539A1 (en) 2004-02-25
CN1675209A (en) 2005-09-28
BR0313262A (en) 2005-07-12
KR20050069977A (en) 2005-07-05
NO20051153L (en) 2005-04-04
IL166482A0 (en) 2006-01-15
EP1537106A1 (en) 2005-06-08
ZA200501842B (en) 2006-05-31
WO2004014910A1 (en) 2004-02-19
JP2005534713A (en) 2005-11-17
CA2494785A1 (en) 2004-02-19
MXPA05001434A (en) 2005-06-06
AR040961A1 (en) 2005-04-27

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