BRPI0606464A2 - pharmaceutical compounds, their use and preparation process and pharmaceutical composition - Google Patents
pharmaceutical compounds, their use and preparation process and pharmaceutical compositionInfo
- Publication number
- BRPI0606464A2 BRPI0606464A2 BRPI0606464-7A BRPI0606464A BRPI0606464A2 BR PI0606464 A2 BRPI0606464 A2 BR PI0606464A2 BR PI0606464 A BRPI0606464 A BR PI0606464A BR PI0606464 A2 BRPI0606464 A2 BR PI0606464A2
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- pharmaceutical
- kinases
- pharmaceutical composition
- preparation process
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title 1
- -1 2,6-dichlorophenyl Chemical group 0.000 abstract 3
- 108091007914 CDKs Proteins 0.000 abstract 2
- 102000003903 Cyclin-dependent kinases Human genes 0.000 abstract 2
- 108090000266 Cyclin-dependent kinases Proteins 0.000 abstract 2
- 108091007911 GSKs Proteins 0.000 abstract 2
- 102000004103 Glycogen Synthase Kinases Human genes 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 238000011321 prophylaxis Methods 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
- 238000011282 treatment Methods 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
COMPOSTOS FARMACêUTICOS, USO E PROCESSO DE PREPARAçãO DOS MESMOS E COMPOSIçãO FARMACêUTICA. A presente invenção refere-se a compostos da fórmula (1): ou um sal, tautómero, solvato ou N-óxidos do mesmo; onde: R¹ é selecionado de 2,6-diclorofenila; 2,6-difluorfenila; um grupo fenil 2,3,6-trissubstituído onde os substituintes são flúor, cloro, metila ou metóxi; e um grupo R^ 0^ onde R^ 0^ é um grupo carbocíclico ou heterocíclico de 3-12 membros, ou C~ 1-8~ hidrocarbila opcionalmente substituído; R^ 2a^ e R^ 2b^ são cada um hidrogênio ou metila; e R³ é como definido nas reivindicações. Os compostos têm atividade como inibidores de cinases ciclina- dependentes (CDK) e cinases glicogênio sintase cinases (GSK) e são úteis no tratamento ou na profilaxia de doenças ou condições mediadas pelas cinases.PHARMACEUTICAL COMPOUNDS, USE AND PROCESS FOR PREPARING THEMSELVES AND PHARMACEUTICAL COMPOSITION. The present invention relates to compounds of formula (1): or a salt, tautomer, solvate or N-oxides thereof; where: R¹ is selected from 2,6-dichlorophenyl; 2,6-difluorphenyl; a 2,3,6-trisubstituted phenyl group wherein the substituents are fluorine, chlorine, methyl or methoxy; and a group R4 O4 where R4 O4 is a 3-12 membered carbocyclic or heterocyclic group, or optionally substituted C1-8 hydrocarbyl; R 2a 4 and R 2 2b 4 are each hydrogen or methyl; and R³ is as defined in the claims. The compounds have activity as inhibitors of cyclin-dependent kinases (CDK) and glycogen synthase kinases (GSK) and are useful in the treatment or prophylaxis of kinases-mediated diseases or conditions.
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 |
| US65193905P | 2005-02-09 | 2005-02-09 | |
| PCT/GB2006/000196 WO2006077419A1 (en) | 2005-01-21 | 2006-01-20 | Pyrazole derivatives for the inhibition of cdk' s and gsk' s |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0606464A2 true BRPI0606464A2 (en) | 2009-06-30 |
Family
ID=40794093
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0606464-7A BRPI0606464A2 (en) | 2005-01-21 | 2006-01-20 | pharmaceutical compounds, their use and preparation process and pharmaceutical composition |
Country Status (1)
| Country | Link |
|---|---|
| BR (1) | BRPI0606464A2 (en) |
-
2006
- 2006-01-20 BR BRPI0606464-7A patent/BRPI0606464A2/en not_active IP Right Cessation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 5A E 6A ANUIDADES. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2161 DE 05/06/2012. |