PA8528101A1 - PIRAZOL DERIVATIVES - Google Patents
PIRAZOL DERIVATIVESInfo
- Publication number
- PA8528101A1 PA8528101A1 PA20018528101A PA8528101A PA8528101A1 PA 8528101 A1 PA8528101 A1 PA 8528101A1 PA 20018528101 A PA20018528101 A PA 20018528101A PA 8528101 A PA8528101 A PA 8528101A PA 8528101 A1 PA8528101 A1 PA 8528101A1
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- Prior art keywords
- compounds
- formula
- syndrome
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- pharmaceutical compositions
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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
-
- 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
-
- 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)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Reproductive Health (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Gynecology & Obstetrics (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pregnancy & Childbirth (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Emergency 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
LA INVENCION PROPORCIONA COMPUESTOS DE LA FORMULA 1 DONDE R1, R2, R3, Y R4 SON COMO SE DEFINEN, Y SUS SALES FARMACEUTICAMENTE ACEPTABLES. SE INDICA QUE LOS COMPUESTOS DE FORMULA 1 TIENEN ACTIVIDAD PARA INHIBIR LAS cdk5, cdk2 GSK-3. PROPORCIONA COMPOSICIONES FARMACEUTICAS Y METODOS QUE COMPRENDEN COMPUESTOS DE FORMULA 1 PARA TRATAR Y PREVENIR ENFERMEDADES Y CONDICIONES QUE IMPLICAN CRECIMIENTO CELULAR ANORMAL, TALES COMO EL CANCER, Y ENFERMEDADES Y CONDICIONES NEURODEGENERATIVAS Y LAS AFECTADAS POR NEUROTRASMISION DE LA DOPAMINA. TAMBIEN SE DESCRIBEN COMPOSICIONES FARMACEUTICAS Y METODOS QUE COMPRENDEN COMPUESTOS DE FORMULA 1 PARA TRATAR FERTILIDAD MASCULINA Y LA MOTILIDAD ESPERMATICA; DIABETES MELLITUS; DETERIORO DE LA TOLERANCIA A LA GLUCOSA; SINDROME METABOLICO O SINDROME X; SINDROME DE POLIQUISTOSIS OVARICA, ADIPOGENESIS Y OBESIDAD; MIOGENESIS Y FRAGILIDAD, POR EJEMPLO EL DETERIORO DE LAS CARACTERISTICAS FISICAS RELACIONADO CON LA EDAD; SARCOPENIA AGUDA, POR EJEMPLO ATROFIA MUSCULAR Y/O CAQUEXIA ASOCIADA CON LAS QUEMADURAS, REPOSO EN CAMA, INMOVILIZACION DE MIEMBROS, O IMPORTANTE CIRUGIA TORACICA, ABDOMINAL, Y/O ORTOPEDICA; SEPSIS; CAIDA DEL CABELLO, CABELLO RALO Y CALVICIE; E INMUNODEFICIENCIA.THE INVENTION PROVIDES COMPOUNDS OF FORMULA 1 WHERE R1, R2, R3, AND R4 ARE AS DEFINED, AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS. IT IS INDICATED THAT THE COMPOUNDS OF FORMULA 1 HAVE ACTIVITY TO INHIBIT THE CDK5, CDK2 GSK-3. PROVIDES PHARMACEUTICAL COMPOSITIONS AND METHODS THAT INCLUDE FORMULA 1 COMPOUNDS TO TREAT AND PREVENT DISEASES AND CONDITIONS THAT IMPLICATE ABNORMAL CELLULAR GROWTH, SUCH AS CANCER, AND NEURODEGENERATIVE DISEASES AND CONDITIONS OF NEOPODRASTRUCTURE AND AFFECTANCE. PHARMACEUTICAL COMPOSITIONS AND METHODS THAT INCLUDE FORMULA 1 COMPOUNDS TO TREAT MALE FERTILITY AND SPERMAL MOTILITY ARE ALSO DESCRIBED; MELLITUS DIABETES; DETERIORATION OF GLUCOSE TOLERANCE; METABOLIC SYNDROME OR X SYNDROME; OVARICA POLYCHYSTOSIS, ADIPOGENESIS AND OBESITY SYNDROME; MIOGENESIS AND FRAGILITY, FOR EXAMPLE THE DETERIORATION OF PHYSICAL CHARACTERISTICS RELATED TO AGE; ACUTE SARCOPENIA, FOR EXAMPLE MUSCULAR ATROPHY AND / OR CAQUEXY ASSOCIATED WITH BURNS, BED REST, IMMOBILIZATION OF MEMBERS, OR IMPORTANT TORACICA SURGERY, ABDOMINAL, AND / OR ORTHOPEDIC; SEPSIS; HAIR FALL, RALO AND CALVICIE HAIR; 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 |
---|---|
PA8528101A1 true PA8528101A1 (en) | 2002-07-30 |
Family
ID=22861151
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PA20018528101A PA8528101A1 (en) | 2000-08-31 | 2001-08-31 | PIRAZOL DERIVATIVES |
Country Status (38)
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) |
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) |
Families Citing this family (73)
Publication number | Priority date | Publication date | Assignee | Title |
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AU2001292670A1 (en) | 2000-09-15 | 2002-03-26 | 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 |
US6610677B2 (en) | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
BR0116411A (en) | 2000-12-21 | 2003-11-11 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors |
WO2003026649A1 (en) * | 2001-09-27 | 2003-04-03 | Applied Research Systems Ars Holding N.V. | 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 |
MXPA04007832A (en) | 2002-02-11 | 2005-09-08 | Bayer Pharmaceuticals Corp | Aryl ureas with angiogenesis inhibiting activity. |
JP2006501191A (en) * | 2002-07-17 | 2006-01-12 | ファルマシア・イタリア・エス・ピー・エー | Heterobicyclic pyrazole derivatives as kinase inhibitors |
BR0315158A (en) | 2002-10-09 | 2005-08-16 | Pfizer Prod Inc | Pyrazole Compounds for the Treatment of Neurodegenative Disorders |
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