HRP20080608T3 - Triazolopiridinilsulfanilni derivati kao inhibitori p38 map kinaze - Google Patents
Triazolopiridinilsulfanilni derivati kao inhibitori p38 map kinazeInfo
- Publication number
- HRP20080608T3 HRP20080608T3 HR20080608T HRP20080608T HRP20080608T3 HR P20080608 T3 HRP20080608 T3 HR P20080608T3 HR 20080608 T HR20080608 T HR 20080608T HR P20080608 T HRP20080608 T HR P20080608T HR P20080608 T3 HRP20080608 T3 HR P20080608T3
- Authority
- HR
- Croatia
- Prior art keywords
- independently selected
- optionally substituted
- halogen
- alkyl
- co2h
- Prior art date
Links
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title 1
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 title 1
- 108010068338 p38 Mitogen-Activated Protein Kinases Proteins 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 150000002367 halogens Chemical class 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000001624 naphthyl group Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000002619 bicyclic group Chemical group 0.000 abstract 3
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- -1 CONR5R6 Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 125000004193 piperazinyl group Chemical group 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 101100054666 Streptomyces halstedii sch3 gene Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 abstract 1
- 125000004092 methylthiomethyl group Chemical group [H]C([H])([H])SC([H])([H])* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- Dermatology (AREA)
Abstract
Spoj formule (I), ili njegova farmaceutski prihvatljiva sol i/ili solvat (uključujući hidrat); ,gdjeR1 je CH3, SCH3, SCH2CH3, CH2CH3, H ili CH2SCH3; R1a je CH3 ili CH2CH3;R2 je heteroaril, heterociklil, aril ili karbociklil; R3 je heteroaril, heterociklil, aril, karbociklil ili R7;R7 je (C1-C6)alkil izborno supstituirani s jednim ili više supstituenata, koje se neovisno bira između OH, halogena, NR5R6, (C1-C8)alkoksi, -S(O)p(C1-C8)alkila, CO2H, CONR5R6, heteroarila, heterociklila, arila, karbociklila, ariloksi, karbocikliloksi, heteroariloksi,te heterocikliloksi; p je 0, 1 ili 2; svakog od R5 i R6 se neovisno bira između H i (C1-C4)alkila, gdje je navedeni (C1-C4)alkil izborno supstitiran s jednim ili više supstituenata, koje se neovisno bira između OH i halogena, ili R5 i R6, zajedno s dušikom, na kojeg su vezani, tvore piperazinilnu, piperidinilnu, morfolinilnu ili pirolidinilna skupinu, gdje je svaki od navedenih piperazinila, piperidinila, morfolinila i pirolidinila izborno supstituiran s jednim ili više OH; "aril" znači fenil ili naftil, gdje su navedeni fenil ili naftil izborno supstituirani s jednim ili više supstituenata, koje se neovisno bira između halogena, -CN, -CO2H,ON, CONR5R6, R7, te R8;R8 se bira između (C1-C6)alkila, (C1-C6)alkoksi, -CO2(C1-C6)alkila, -S(O)p(C1-C6)alkila, -CO(C1-C6) alkila, te (C3-C7)cikloalkila; svaki R5 je izborno supstituiran s jednim iliviše supstituenata, koje se neovisno bira između:(C1-C6)alkoksi, izborno supstituiranog s jednim ili više supstituenata, koje se neovisno bira između OH, halogena, CO2H, CONR5R6, te NR5R6,-S(O)p(C1-C6)alkila, izborno supstituiranog s jednim ili više supstituenata, koje se neovisno bira između OH, halogena, CO2H, CONR5R6, te NR5R6,OH, halogena, NR5R6,CO2H, CONR5R6, teR9;R9 je heteroaril2, heterociklil2, aril2, karbociklil2, aril2oksi, karbociklil2oksi, heteroaril2oksi ili heterociklil2oksi; "aril2" znači fenil ili naftil, gdje su navedeni fenil ili naftil izborno supstituirani s jednim ili više supstituenata, koje se neovisno bira između halogena, -CN, CO2H, OH, te CONR5R6;"karbociklil" znači mono- ili biciklički, zasićeni ili djelomično nezasićeni prstenasti sustav, koji sadrži 3 do 10 atoma ugljika u prstenu, izborno supstituiran s jednim ili više supstituenata, koje se neovisno bira između halogena, -CN, -CO2H, OH, CONR5R6, R8, te R9;"karbociklil2" znači mono- ili biciklički, zasićeni ili djelomično nezasićeni prstenasti sustav, koji sadrži 3 do 10 atoma ugljika u prstenu, izborno supstituiran s jednim ili više supstituenata, koje se neovisno bira između halogena, -CN, -CO2H, OH, te CONR5R6;svaki "heterociklil", i "heterociklil2" neovisno znači 3- do 10- člana, zasićena ili djelomično nezasićena, mono- ili biciklička skupina, koja sadrži 1 do 4 heteroatoma u prstenu, koje se neovisno bira između N, O, te S; svaki "heteroaril", te svaki "heteroaril2", neovisno znači 5- do 10- člana, mono- ili biciklička, aromatska skupina, koja sadrži 1 do 4 heteroatoma u prstenu, koje se neo
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GB0418015A GB0418015D0 (en) | 2004-08-12 | 2004-08-12 | New compounds |
US69155905P | 2005-06-17 | 2005-06-17 | |
PCT/IB2005/002574 WO2006018718A2 (en) | 2004-08-12 | 2005-08-09 | Triazolopyridinylsulfanyl derivatives as p38 map kinase inhibitors |
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