BR0113574A - Derivados de pirazol e uso dos mesmos como inibidores de proteìna quinase - Google Patents
Derivados de pirazol e uso dos mesmos como inibidores de proteìna quinaseInfo
- Publication number
- BR0113574A BR0113574A BR0113574-0A BR0113574A BR0113574A BR 0113574 A BR0113574 A BR 0113574A BR 0113574 A BR0113574 A BR 0113574A BR 0113574 A BR0113574 A BR 0113574A
- Authority
- BR
- Brazil
- Prior art keywords
- formula
- compounds
- syndrome
- protein kinase
- kinase inhibitors
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
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- 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
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- 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
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P25/28—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
- A61P3/00—Drugs for disorders of the metabolism
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- 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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- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
- C07D231/40—Acylated on said nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Reproductive Health (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Psychiatry (AREA)
- Pregnancy & Childbirth (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
"DERIVADOS DE PIRAZOL E USO DOS MESMOS COMO INIBIDORES DE PROTEìNA QUINASE". A invenção proporciona compostos de fórmula 1 em que R^ 1^, R^ 2^, R^ 3^, e R^ 4^ sejam tal como se definem, e os seus sais farmaceuticamente aceitáveis. Anunciam-se os compostos de fórmula 1 como tendo atividade inibidora de cdk2 e GSK-3. Composições farmacêuticas e métodos que incluam compostos de fórmula (1) para o tratamento e a prevenção de doenças e estados incluindo o crescimento anormal das células, tais como o câncer, e doenças e estados neurodegenerativos e os que sejam afetados pela neurotransmissão de dopamina. Também se descrevem composições farmacêuticas e métodos que incluam compostos de fórmula 1 para o tratamento das fertilidade masculina e mobilidade do esperma; diabetes mellitus; déficet de tolerância à glicose; síndrome metabólico ou síndrome X; síndrome policístico dos ovários; adipogênese e obesidade; miogênese e fragilidade, por exemplo o declínio no desempenho físico relacionado com a idade; sarcopenia aguda, por exemplo a atrofia muscular e/ou a caquéxia associada a queimaduras, permanência em acamado, imobilização dos membros, ou grande cirurgia toráxica, abdominal, e/ou a cirurgia ortopédica; sépsia; perda capilar, enfraquecimento do cabelo, e calvície; e imunodeficiência.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22941500P | 2000-08-31 | 2000-08-31 | |
| PCT/IB2001/001540 WO2002018346A1 (en) | 2000-08-31 | 2001-08-24 | Pyrazole derivatives and their use as protein kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0113574A true BR0113574A (pt) | 2003-07-22 |
Family
ID=22861151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0113574-0A BR0113574A (pt) | 2000-08-31 | 2001-08-24 | Derivados de pirazol e uso dos mesmos como inibidores de proteìna quinase |
Country Status (39)
| Country | Link |
|---|---|
| EP (1) | EP1313710A1 (pt) |
| JP (1) | JP2004507526A (pt) |
| KR (1) | KR20030027093A (pt) |
| CN (1) | CN1518543A (pt) |
| AP (1) | AP2001002266A0 (pt) |
| AR (1) | AR035345A1 (pt) |
| AU (1) | AU2001280009A1 (pt) |
| BG (1) | BG107455A (pt) |
| BR (1) | BR0113574A (pt) |
| CA (1) | CA2420363A1 (pt) |
| CR (1) | CR6881A (pt) |
| CZ (1) | CZ2003468A3 (pt) |
| DO (1) | DOP2001000243A (pt) |
| DZ (1) | DZ3398A1 (pt) |
| EA (1) | EA200300205A1 (pt) |
| EC (1) | ECSP034480A (pt) |
| EE (1) | EE200300085A (pt) |
| GT (1) | GT200100179A (pt) |
| HN (1) | HN2001000192A (pt) |
| HR (1) | HRP20030140A2 (pt) |
| HU (1) | HUP0302669A3 (pt) |
| IL (1) | IL154016A0 (pt) |
| IS (1) | IS6687A (pt) |
| MA (1) | MA26946A1 (pt) |
| MX (1) | MXPA03001785A (pt) |
| NO (1) | NO20030958L (pt) |
| NZ (1) | NZ523656A (pt) |
| OA (1) | OA12368A (pt) |
| PA (1) | PA8528101A1 (pt) |
| PE (1) | PE20020470A1 (pt) |
| PL (1) | PL360742A1 (pt) |
| PY (1) | PY0121331A (pt) |
| SK (1) | SK2002003A3 (pt) |
| SV (1) | SV2002000618A (pt) |
| TN (1) | TNSN01132A1 (pt) |
| UY (1) | UY26909A1 (pt) |
| WO (1) | WO2002018346A1 (pt) |
| YU (1) | YU14703A (pt) |
| ZA (1) | ZA200301064B (pt) |
Families Citing this family (87)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE538794T1 (de) | 1999-01-13 | 2012-01-15 | Bayer Healthcare Llc | Gamma carboxyarylsubstituierte diphenylharnstoffverbindungen als p38 kinasehemmer |
| US7351834B1 (en) | 1999-01-13 | 2008-04-01 | Bayer Pharmaceuticals Corporation | ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| US7473691B2 (en) | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6613776B2 (en) | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| EP1317450B1 (en) | 2000-09-15 | 2006-11-22 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6610677B2 (en) | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| NZ526472A (en) | 2000-12-21 | 2004-04-30 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors |
| DK1441724T3 (da) * | 2001-09-27 | 2007-12-03 | Serono Lab | Fremgangsmåde til forögelse af endogene testosteronniveauer |
| WO2003068229A1 (en) | 2002-02-11 | 2003-08-21 | Bayer Pharmaceuticals Corporation | Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors |
| MXPA04007832A (es) | 2002-02-11 | 2005-09-08 | Bayer Pharmaceuticals Corp | Aril-ureas con actividad inhibitoria de angiogenesis. |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| ES2304531T3 (es) * | 2002-07-17 | 2008-10-16 | Pfizer Italia S.R.L. | Derivados heterobiciclicos de pirazol como inhibidores de quinasa. |
| DK1532145T3 (da) | 2002-08-02 | 2007-01-15 | Vertex Pharma | Pyrazolpræparater der er anvendelige som inhibitorer af GSK-3 |
| WO2004033434A1 (en) * | 2002-10-09 | 2004-04-22 | Pfizer Products Inc. | Pyrazole compounds for treatment of neurodegenerative disorders |
| EP1551842A1 (en) * | 2002-10-15 | 2005-07-13 | Smithkline Beecham Corporation | Pyradazine compounds as gsk-3 inhibitors |
| WO2004076414A2 (en) * | 2003-02-27 | 2004-09-10 | Smithkline Beecham Corporation | Novel compounds |
| WO2004113274A2 (en) | 2003-05-20 | 2004-12-29 | Bayer Pharmaceuticals Corporation | Diaryl ureas with kinase inhibiting activity |
| JP4220548B2 (ja) * | 2003-06-05 | 2009-02-04 | エラン ファーマシューティカルズ，インコーポレイテッド | アシル化されたアミノ酸・アミジルピラゾール、および関連化合物 |
| GB0317127D0 (en) * | 2003-07-22 | 2003-08-27 | Astex Technology Ltd | Pharmaceutical compounds |
| PL2256106T3 (pl) | 2003-07-22 | 2015-08-31 | Astex Therapeutics Ltd | Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3) |
| EA010485B1 (ru) | 2003-07-23 | 2008-10-30 | Байер Фамэсьютиклс Копэрейшн | Производное n,n'-дифенилмочевины, фармацевтическая композиция (варианты) и способ лечения и предупреждения заболеваний и состояний с его использованием (варианты) |
| MXPA06000933A (es) * | 2003-07-25 | 2006-03-30 | Pfizer | Compuestos de aminopirazol y uso como inhibidores de chk1. |
| ATE473967T1 (de) * | 2003-11-26 | 2010-07-15 | Pfizer Prod Inc | Aminopyrazolderivate als gsk-3-inhibitoren |
| CA2550361C (en) | 2003-12-19 | 2014-04-29 | Prabha Ibrahim | Compounds and methods for development of ret modulators |
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| EP1742921A2 (en) * | 2004-04-21 | 2007-01-17 | AstraZeneca AB | Pyrazole derivatives useful for the treatment of cancer |
| CN101010315A (zh) | 2004-04-30 | 2007-08-01 | 拜耳制药公司 | 用于治疗癌症的取代的吡唑基脲衍生物 |
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| GB9811427D0 (en) * | 1998-05-29 | 1998-07-22 | Zeneca Ltd | Chemical compounds |
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