BRPI0411122A - pirazol[3,4-b]piridin-6-onas como inibidores gsk-3 - Google Patents
pirazol[3,4-b]piridin-6-onas como inibidores gsk-3Info
- Publication number
- BRPI0411122A BRPI0411122A BRPI0411122-2A BRPI0411122A BRPI0411122A BR PI0411122 A BRPI0411122 A BR PI0411122A BR PI0411122 A BRPI0411122 A BR PI0411122A BR PI0411122 A BRPI0411122 A BR PI0411122A
- Authority
- BR
- Brazil
- Prior art keywords
- gsk
- pyridin
- inhibitors
- pyrazol
- ones
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
- 101150090422 gsk-3 gene Proteins 0.000 title 1
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical class OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 201000004384 Alopecia Diseases 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 abstract 1
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000024963 hair loss Diseases 0.000 abstract 1
- 230000003676 hair loss Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
Classifications
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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
- A61K31/435—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
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61P25/18—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
- A61P25/22—Anxiolytics
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- 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
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- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
"PIRAZOL¢3,4-b!PIRIDIN-6-ONAS COMO INIBIDORES GSK-3". A presente invenção proporciona compostos de fórmula (I) , os seus estereoisómeros e pró-fármacos, e os sais farmaceuticamente aceitáveis dos compostos, estereoisómeros e pró-fármacos, em que R¬ 1¬, R¬ 2¬ e R¬ 3¬ são como aqui definidos; as suas formulações farmacêuticas; e a sua utilização no tratamento de, entre outras coisas, patologias, doenças e sintomas, tais como distúrbio bipolar, diabetes, demência, Doença de Alzheimer, acidente vascular cerebral, esquizofrenia, depressão, perda de cabelo e câncer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US48320103P | 2003-06-27 | 2003-06-27 | |
PCT/IB2004/002026 WO2005000304A1 (en) | 2003-06-27 | 2004-06-14 | Pyrazolo[3,4-b]pyridin-6-ones as gsk-3 inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BRPI0411122A true BRPI0411122A (pt) | 2006-07-18 |
Family
ID=33552042
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0411122-2A BRPI0411122A (pt) | 2003-06-27 | 2004-06-14 | pirazol[3,4-b]piridin-6-onas como inibidores gsk-3 |
Country Status (10)
Country | Link |
---|---|
US (1) | US7300944B2 (pt) |
EP (1) | EP1641455B1 (pt) |
JP (1) | JP4637834B2 (pt) |
AT (1) | ATE403428T1 (pt) |
BR (1) | BRPI0411122A (pt) |
CA (1) | CA2525245C (pt) |
DE (1) | DE602004015603D1 (pt) |
ES (1) | ES2308186T3 (pt) |
MX (1) | MXPA05013628A (pt) |
WO (1) | WO2005000304A1 (pt) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2258359A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation with sabcomelin |
EP1928437A2 (en) | 2005-08-26 | 2008-06-11 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
JP2009512711A (ja) | 2005-10-21 | 2009-03-26 | ブレインセルス,インコーポレイティド | Pde阻害による神経新生の調節 |
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 |
EP2021000A2 (en) | 2006-05-09 | 2009-02-11 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
US20080103105A1 (en) * | 2006-09-22 | 2008-05-01 | Braincells, Inc. | HMG CoA REDUCTASE MEDIATED MODULATION OF NEUROGENESIS |
WO2009017453A1 (en) * | 2007-07-30 | 2009-02-05 | Astrazeneca Ab | New therapeutic combination of an antipsychotic and a gsk3 inhibitor 958 |
GB0719299D0 (en) | 2007-10-03 | 2007-11-14 | Optinose As | Nasal delivery devices |
WO2010099217A1 (en) | 2009-02-25 | 2010-09-02 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
ES2530345T3 (es) * | 2010-09-02 | 2015-03-02 | Merck Patent Gmbh | Derivados de pirazolopiridinona como antagonistas del receptor del LPA |
WO2014078568A1 (en) | 2012-11-14 | 2014-05-22 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
WO2015111545A1 (ja) * | 2014-01-21 | 2015-07-30 | 第一三共株式会社 | 縮合ピラゾール誘導体 |
CA2945263A1 (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 |
MX373865B (es) * | 2015-09-01 | 2025-03-04 | Taiho Pharmaceutical Co Ltd | Compuesto novedoso de pirazolo[3,4-d] pirimidina o sal del mismo |
CN106946879B (zh) * | 2017-03-14 | 2018-11-23 | 牡丹江医学院 | 一种用于降血脂的药物及其制备方法 |
GB201811169D0 (en) | 2018-07-06 | 2018-08-29 | Kancera Ab | New compounds |
CA3228862A1 (en) * | 2021-08-03 | 2023-02-09 | Beigene, Ltd. | Pyrazolopyridinone compounds |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4020072A (en) * | 1976-05-04 | 1977-04-26 | E. R. Squibb & Sons, Inc. | 5-Aminomethyl-1H-pyrazolo[3,4-b]pyridines |
US20020103185A1 (en) * | 2000-08-31 | 2002-08-01 | Sanner Mark A. | Pyrazole derivatives |
JP2004509891A (ja) * | 2000-09-22 | 2004-04-02 | スミスクライン ビーチャム パブリック リミテッド カンパニー | 抗糖尿病薬としてのピラゾロピリジンおよびピラゾロピリダジン |
US7105532B2 (en) * | 2000-12-19 | 2006-09-12 | Smithkline Beecham Corporation | Pyrazolo[3,4-c]pyridines as gsk-3 inhibitors |
GB0128287D0 (en) * | 2001-11-26 | 2002-01-16 | Smithkline Beecham Plc | Novel method and compounds |
-
2004
- 2004-06-14 CA CA2525245A patent/CA2525245C/en not_active Expired - Fee Related
- 2004-06-14 DE DE602004015603T patent/DE602004015603D1/de not_active Expired - Lifetime
- 2004-06-14 ES ES04736783T patent/ES2308186T3/es not_active Expired - Lifetime
- 2004-06-14 MX MXPA05013628A patent/MXPA05013628A/es not_active Application Discontinuation
- 2004-06-14 AT AT04736783T patent/ATE403428T1/de not_active IP Right Cessation
- 2004-06-14 EP EP04736783A patent/EP1641455B1/en not_active Expired - Lifetime
- 2004-06-14 BR BRPI0411122-2A patent/BRPI0411122A/pt not_active IP Right Cessation
- 2004-06-14 WO PCT/IB2004/002026 patent/WO2005000304A1/en active IP Right Grant
- 2004-06-14 JP JP2006516566A patent/JP4637834B2/ja not_active Expired - Fee Related
- 2004-06-23 US US10/875,009 patent/US7300944B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
DE602004015603D1 (de) | 2008-09-18 |
WO2005000304A1 (en) | 2005-01-06 |
MXPA05013628A (es) | 2006-02-24 |
EP1641455A1 (en) | 2006-04-05 |
EP1641455B1 (en) | 2008-08-06 |
US7300944B2 (en) | 2007-11-27 |
CA2525245A1 (en) | 2005-01-06 |
ES2308186T3 (es) | 2008-12-01 |
US20040266815A1 (en) | 2004-12-30 |
JP2007516170A (ja) | 2007-06-21 |
ATE403428T1 (de) | 2008-08-15 |
JP4637834B2 (ja) | 2011-02-23 |
CA2525245C (en) | 2010-10-19 |
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Legal Events
Date | Code | Title | Description |
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B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 5A, 6A, 7A E 8A ANUIDADES. |
|
B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012. |