ECSP034480A - PIRAZOL DERIVATIVES - Google Patents
PIRAZOL DERIVATIVESInfo
- Publication number
- ECSP034480A ECSP034480A EC2003004480A ECSP034480A ECSP034480A EC SP034480 A ECSP034480 A EC SP034480A EC 2003004480 A EC2003004480 A EC 2003004480A EC SP034480 A ECSP034480 A EC SP034480A EC SP034480 A ECSP034480 A EC SP034480A
- Authority
- EC
- Ecuador
- Prior art keywords
- formula
- compounds
- syndrome
- pharmaceutical compositions
- conditions
- 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
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- 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
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- 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
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- 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
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- 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)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Obesity (AREA)
- Neurosurgery (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Pregnancy & Childbirth (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
La invención proporciona compuestos de la fórmula I donde R1, R2, R3, R4 son como se definen y sus sales farmacéuticamente aceptables. Se indica que los compuestos de la fórmula 1 tienen actividad para inhibir las cdk5, cdk2 y GSK-3. Proporciona composiciones farmacéuticos y métodos que comprenden compuestos de la fórmula 1 para tratar y prevenir enfermedades y condiciones que implican crecimiento celular anormal, tales como el cáncer, enfermedades y condiciones neurodegenerativas y las afectadas por la neurotrasmisión de la dopamina. También se describen composiciones farmacéuticas y métodos que comprenden compuestos de fórmula 1 para tratar la fertilidad masculina y la motilidad espermática, diabetes mellitus, deterioro de la tolerancia a la glucosa, síndrome metabólico o síndrome X ; síndrome de poliquistosis ovárica, adipogénesis y obesidad; miogénesis y fragilidad, por ejemplo el deterioro de las características físicas relacionado com. la edad ; sarcopenia aguda, por ejemplo atrofia muscular y/o caquexia asociada con las quemaduras, reposo en cama, inmovilización de miembros o importante cirugía toráxico, abdominal, y/o ortopédica; sepsis; caída del cabello, raro y calvicie; e inmunodeficiencia.The invention provides compounds of the formula I wherein R1, R2, R3, R4 are as defined and their pharmaceutically acceptable salts. The compounds of formula 1 are indicated to have activity to inhibit cdk5, cdk2 and GSK-3. It provides pharmaceutical compositions and methods comprising compounds of the formula 1 for treating and preventing diseases and conditions that involve abnormal cell growth, such as cancer, neurodegenerative diseases and conditions and those affected by the neurotransmission of dopamine. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating male fertility and sperm motility, diabetes mellitus, impaired glucose tolerance, metabolic syndrome or syndrome X are also described; polycystic ovarian syndrome, adipogenesis and obesity; myogenesis and fragility, for example the deterioration of physical characteristics related to com. age ; acute sarcopenia, for example muscular atrophy and / or cachexia associated with burns, bed rest, limb immobilization or major thoracic, abdominal, and / or orthopedic surgery; sepsis; hair loss, rare and baldness; and immunodeficiency.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22941500P | 2000-08-31 | 2000-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP034480A true ECSP034480A (en) | 2003-03-31 |
Family
ID=22861151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2003004480A ECSP034480A (en) | 2000-08-31 | 2003-02-17 | PIRAZOL DERIVATIVES |
Country Status (39)
| Country | Link |
|---|---|
| EP (1) | EP1313710A1 (en) |
| JP (1) | JP2004507526A (en) |
| KR (1) | KR20030027093A (en) |
| CN (1) | CN1518543A (en) |
| AP (1) | AP2001002266A0 (en) |
| AR (1) | AR035345A1 (en) |
| AU (1) | AU2001280009A1 (en) |
| BG (1) | BG107455A (en) |
| BR (1) | BR0113574A (en) |
| CA (1) | CA2420363A1 (en) |
| CR (1) | CR6881A (en) |
| CZ (1) | CZ2003468A3 (en) |
| DO (1) | DOP2001000243A (en) |
| DZ (1) | DZ3398A1 (en) |
| EA (1) | EA200300205A1 (en) |
| EC (1) | ECSP034480A (en) |
| EE (1) | EE200300085A (en) |
| GT (1) | GT200100179A (en) |
| HN (1) | HN2001000192A (en) |
| HR (1) | HRP20030140A2 (en) |
| HU (1) | HUP0302669A3 (en) |
| IL (1) | IL154016A0 (en) |
| IS (1) | IS6687A (en) |
| MA (1) | MA26946A1 (en) |
| MX (1) | MXPA03001785A (en) |
| NO (1) | NO20030958L (en) |
| NZ (1) | NZ523656A (en) |
| OA (1) | OA12368A (en) |
| PA (1) | PA8528101A1 (en) |
| PE (1) | PE20020470A1 (en) |
| PL (1) | PL360742A1 (en) |
| PY (1) | PY0121331A (en) |
| SK (1) | SK2002003A3 (en) |
| SV (1) | SV2002000618A (en) |
| TN (1) | TNSN01132A1 (en) |
| UY (1) | UY26909A1 (en) |
| WO (1) | WO2002018346A1 (en) |
| YU (1) | YU14703A (en) |
| ZA (1) | ZA200301064B (en) |
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| DK1318997T3 (en) | 2000-09-15 | 2006-09-25 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors |
| US7473691B2 (en) | 2000-09-15 | 2009-01-06 | 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 |
| HUP0400639A3 (en) | 2000-12-21 | 2010-03-29 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them |
| US20040198799A1 (en) * | 2001-09-27 | 2004-10-07 | Brondyk William H. | Methods of increasing endogenous testosterone levels |
| US20030216396A1 (en) | 2002-02-11 | 2003-11-20 | Bayer Corporation | Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors |
| US7838541B2 (en) | 2002-02-11 | 2010-11-23 | Bayer Healthcare, Llc | Aryl ureas with angiogenesis inhibiting activity |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
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| DE60308387T2 (en) | 2002-08-02 | 2007-09-20 | Vertex Pharmaceuticals Inc., Cambridge | Pyrazole-containing Compounds and Their Use as GSK-3 Inhibitors |
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| EP1047418B1 (en) * | 1997-12-22 | 2005-07-27 | Bayer Pharmaceuticals Corp. | Inhibition of raf kinase using substituted heterocyclic ureas |
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| US6387900B1 (en) * | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
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