BRPI0606317A2 - compostos de pirazol, uso dos mesmos e composição farmacêutica - Google Patents
compostos de pirazol, uso dos mesmos e composição farmacêuticaInfo
- Publication number
- BRPI0606317A2 BRPI0606317A2 BRPI0606317-9A BRPI0606317A BRPI0606317A2 BR PI0606317 A2 BRPI0606317 A2 BR PI0606317A2 BR PI0606317 A BRPI0606317 A BR PI0606317A BR PI0606317 A2 BRPI0606317 A2 BR PI0606317A2
- Authority
- BR
- Brazil
- Prior art keywords
- group
- pharmaceutical composition
- compounds
- pyrazole compounds
- activity
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 150000003217 pyrazoles Chemical class 0.000 title 1
- -1 tautomers Chemical class 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 abstract 1
- 102100032857 Cyclin-dependent kinase 1 Human genes 0.000 abstract 1
- 101710106279 Cyclin-dependent kinase 1 Proteins 0.000 abstract 1
- 102100036239 Cyclin-dependent kinase 2 Human genes 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 102000001267 GSK3 Human genes 0.000 abstract 1
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 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
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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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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- 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
- C07D401/14—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 three or more hetero rings
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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
- C07D405/12—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 linked by a chain containing hetero atoms as chain links
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- 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
- C07D405/14—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 three or more hetero rings
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- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- C07D413/12—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 chain containing hetero atoms as chain links
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- 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
- C07D417/14—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 three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
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- Neurosurgery (AREA)
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- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
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- Pulmonology (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Psychology (AREA)
- Obesity (AREA)
Abstract
COMPOSTOS DE PIRAZOL, USO DOS MESMOS E COMPOSIçãO FARMACêUTICA. A presente invenção refere-se a compostos da Fórmula (I): ou sal, tautómeros, N-óxidos ou solvatos destes em que: R¹ é selecionado de: (a) 2,6-diclorofenila; (b) 2,6-difluorofenila; (o) um grupo fenila 2,3,6-trissubstituído em que os substituintes para o grupo fenila são selecionados de flúor, cloro, metila e metóxi; (d) um grupo R^ 0^; (e) um grupo R^ 1a^; (f) um grupo R^ 1b^; (g) um grupo R^ 1c^; (h) um grupo R^ 1d^; e (j) 2,6-difluorofenilamino; em que R^ 0^, R^ 1b^, R^ 1b^, R^ 1c^, R^ 1d^, R^ 2a^, R^ 2b^ e R³ são como definidos na reivindicação. Os compostos tém atividade como inibidores de cinase de CDK (tal como CDK1 ou CDK2) e atividade de glicogênio sintase cinase-3.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64621705P | 2005-01-21 | 2005-01-21 | |
| GB0501480A GB0501480D0 (en) | 2005-01-22 | 2005-01-22 | Pharmaceutical compounds |
| GB0501748A GB0501748D0 (en) | 2005-01-27 | 2005-01-27 | Pharmaceutical compounds |
| US65133905P | 2005-02-09 | 2005-02-09 | |
| PCT/GB2006/000191 WO2006077414A1 (en) | 2005-01-21 | 2006-01-20 | Pyrazole derivatives for the inhibition of cdk' s and gsk' s |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0606317A2 true BRPI0606317A2 (pt) | 2009-06-16 |
Family
ID=35967182
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0606107-9A BRPI0606107A2 (pt) | 2005-01-21 | 2006-01-20 | compostos farmacêuticos, seus proocessos de preparação, usos dos mesmos na fabricação de medicamento e composição farmacêutica compreendendo os referidos compostos |
| BRPI0606317-9A BRPI0606317A2 (pt) | 2005-01-21 | 2006-01-20 | compostos de pirazol, uso dos mesmos e composição farmacêutica |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0606107-9A BRPI0606107A2 (pt) | 2005-01-21 | 2006-01-20 | compostos farmacêuticos, seus proocessos de preparação, usos dos mesmos na fabricação de medicamento e composição farmacêutica compreendendo os referidos compostos |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US20080306069A1 (pt) |
| EP (3) | EP1846395A1 (pt) |
| JP (3) | JP2008528465A (pt) |
| KR (3) | KR20070107049A (pt) |
| AR (3) | AR052559A1 (pt) |
| AU (3) | AU2006207313A1 (pt) |
| BR (2) | BRPI0606107A2 (pt) |
| CA (3) | CA2593656A1 (pt) |
| IL (3) | IL184499A0 (pt) |
| MA (3) | MA29255B1 (pt) |
| MX (3) | MX2007008782A (pt) |
| NO (3) | NO20073955L (pt) |
| PE (3) | PE20061073A1 (pt) |
| TN (3) | TNSN07278A1 (pt) |
| WO (3) | WO2006077414A1 (pt) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ544756A (en) | 2003-07-22 | 2009-09-25 | Astex Therapeutics Ltd | 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators |
| TW200533657A (en) | 2004-02-17 | 2005-10-16 | Esteve Labor Dr | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1845975A1 (en) * | 2005-01-21 | 2007-10-24 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors and further antitumor agents |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| AU2006207321B2 (en) * | 2005-01-21 | 2012-09-06 | Astex Therapeutics Limited | Pharmaceutical compounds |
| US20080139620A1 (en) * | 2005-01-21 | 2008-06-12 | Astex Therapeutics Limited | Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's |
| AR054425A1 (es) * | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| EP1845973B1 (en) * | 2005-01-21 | 2015-08-12 | Astex Therapeutics Limited | Pharmaceutical compounds |
| AR052559A1 (es) * | 2005-01-21 | 2007-03-21 | Astex Therapeutics Ltd | Derivados de pirazol para inhibir cdk's y gsk's |
| US20090036607A1 (en) * | 2005-03-03 | 2009-02-05 | Mitsubishi Rayon Co., Ltd. | Polymer particle, resin composition containing same, and molded body |
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