AP2001002266A0 - Pyrazole derivatives. - Google Patents
Pyrazole derivatives.Info
- Publication number
- AP2001002266A0 AP2001002266A0 APAP/P/2001/002266A AP2001002266A AP2001002266A0 AP 2001002266 A0 AP2001002266 A0 AP 2001002266A0 AP 2001002266 A AP2001002266 A AP 2001002266A AP 2001002266 A0 AP2001002266 A0 AP 2001002266A0
- Authority
- AP
- ARIPO
- Prior art keywords
- formula
- compounds
- sydrome
- pharmaceutical compositions
- conditions
- Prior art date
Links
- 150000003217 pyrazoles Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 201000004384 Alopecia Diseases 0.000 abstract 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 206010006895 Cachexia Diseases 0.000 abstract 1
- 101150053721 Cdk5 gene Proteins 0.000 abstract 1
- 208000036119 Frailty Diseases 0.000 abstract 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract 1
- 206010028289 Muscle atrophy Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 206010036049 Polycystic ovaries Diseases 0.000 abstract 1
- 206010040047 Sepsis Diseases 0.000 abstract 1
- 230000003187 abdominal effect Effects 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 230000011759 adipose tissue development Effects 0.000 abstract 1
- 206010003549 asthenia Diseases 0.000 abstract 1
- 230000036621 balding Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 101150073031 cdk2 gene Proteins 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- 230000007423 decrease Effects 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
- 229960003638 dopamine Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000035558 fertility Effects 0.000 abstract 1
- 239000008103 glucose Substances 0.000 abstract 1
- 101150090422 gsk-3 gene Proteins 0.000 abstract 1
- 208000024963 hair loss Diseases 0.000 abstract 1
- 230000003676 hair loss Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000002503 metabolic effect Effects 0.000 abstract 1
- 230000020763 muscle atrophy Effects 0.000 abstract 1
- 201000000585 muscular atrophy Diseases 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 230000000399 orthopedic effect Effects 0.000 abstract 1
- 230000036314 physical performance Effects 0.000 abstract 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000022379 skeletal muscle tissue development Effects 0.000 abstract 1
- 230000019100 sperm motility Effects 0.000 abstract 1
- 238000001356 surgical procedure Methods 0.000 abstract 1
- 230000005062 synaptic transmission Effects 0.000 abstract 1
- 210000000115 thoracic cavity Anatomy 0.000 abstract 1
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
- C07D231/40—Acylated on said nitrogen atom
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P3/08—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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- 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
-
- 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
-
- 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)
- 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)
- Endocrinology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Reproductive Health (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (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
The invention provides compounds of formula 1 wherein r1, r2,r3, and r4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and gsk-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating and preventing diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative disease and conditions and those affected by dopamine neurotransmission. Also described are pharmaceutical compositions and methods comprising compounds of formula 1 for treating male fertility and sperm motility; diabetes mellitus; impared glucose tolerance; metabolic sydrome or sydrome x; polycystic ovary sydrome; adipogenesis and obesity; myogenesis and frailty, for example age-related decline in physical performance; acute sacopenia, for example muscle atrophy and/or cachexia associated with burns, bed rest, limb immobilization, or major thoracic, abdominal, and/or orthopedic surgery; sepsis; hair loss, hair thinning, and balding; and immunodefiency.
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 |
|---|---|
| AP2001002266A0 true AP2001002266A0 (en) | 2001-09-30 |
Family
ID=22861151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| APAP/P/2001/002266A AP2001002266A0 (en) | 2000-08-31 | 2001-08-24 | Pyrazole 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) | NO20030958D0 (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) |
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| ME00275B (en) | 1999-01-13 | 2011-02-10 | Bayer Corp | ?-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
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| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
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| US6610677B2 (en) | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
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| WO2004035588A1 (en) * | 2002-10-15 | 2004-04-29 | Smithkline Beecham Corporation | Pyradazine compounds as gsk-3 inhibitors |
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| NZ505844A (en) * | 1997-12-22 | 2003-10-31 | Bayer Ag | Inhibition of raf kinase using substituted heterocyclic ureas |
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| DE60024631T2 (en) * | 1999-07-26 | 2006-06-14 | Banyu Pharma Co Ltd | Biaryl UREA DERIVATIVES |
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| EE200200065A (en) * | 1999-08-12 | 2003-04-15 | Pharmacia Italia S.P.A. | 3-Aminopyrazole Derivatives, Their Preparation and Use as Anticancer Agents, and Pharmaceutical Composition Containing Them |
| CA2392971C (en) * | 1999-11-30 | 2008-10-07 | Pfizer Products Inc. | 2,4-diaminopyrimidine compounds useful as immunosuppressants |
| CA2398446A1 (en) * | 2000-04-18 | 2001-10-25 | Agouron Pharmaceuticals, Inc. | Pyrazoles for inhibiting protein kinases |
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