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1. WO2010131030 - PYRIDYLUREA DERIVATIVES AND THEIR THERAPEUTIC USE

Publication Number WO/2010/131030
Publication Date 18.11.2010
International Application No. PCT/GB2010/050767
International Filing Date 11.05.2010
IPC
C07D 213/75 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with 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
72Nitrogen atoms
75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 401/10 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
CPC
C07D 213/75
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 401/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
Applicants
  • PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED [GB]/[GB] (AllExceptUS)
  • BESWICK, Amanda [GB]/[GB] (UsOnly)
  • WASZKOWYCZ, Bohdan [GB]/[GB] (UsOnly)
  • VAN NIEL, Monique Bodil [NL]/[GB] (UsOnly)
Inventors
  • BESWICK, Amanda
  • WASZKOWYCZ, Bohdan
  • VAN NIEL, Monique Bodil
Agents
  • PERRY, Robert, Edward
Priority Data
0908317.114.05.2009GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PYRIDYLUREA DERIVATIVES AND THEIR THERAPEUTIC USE
(FR) DÉRIVÉS DE PYRIDYLURÉE ET LEUR UTILISATION THÉRAPEUTIQUE
Abstract
(EN) Compounds of formula (IA) are inhibitors of p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract formula (IA). wherein R 1 is a radical of formula (IIA), (IIB), or (IIC); wherein m is 0 or 1; T is N or CH; R 2a, R 2b, R 2c are independently selected from H, halogen and C1 -C6 alkyl; R3 is H or F; R4 is -CH3; -C2 H5; -CH2OH, CH2SCH3; - SCH3 or -SC2H5; R5 is -CH3 or -C2H5; R6 is H, or represents one or more 10 substituents, each independently selected from C1 -C6 alkyl, hydroxy, halogen, and radicals of formulae (IIIA), (IIIB) and (IIIC):IA)(IIIB)(IIIC); wherein R61a and R61b are independently H or C1-C6 alkyl, or R61a and R61b taken together with the nitrogen to which they are attached to form a 6-membered 15 heterocyclic ring optionally containing a further heteroatom selected from N and O; n is 0, 1 or 2; p is 1 or 2; R7 is H or F; and R8 is H or CONH2.
(FR) La présente invention a pour objet des composés de formule (IA) qui sont des inhibiteurs des inhibiteurs de p38 MAPK, utiles en tant qu'agents anti-inflammatoires dans le traitement, entre autres, des maladies des voies respiratoires. Formule (IA), R 1 étant un radical de formules (IIA), (IIB), ou (IIC) ; m étant 0 ou 1 ; T étant N ou CH ; R 2a, R 2b, R 2c étant indépendamment choisis parmi H, un halogène et un alkyle en C1 à C6 ; R3 étant H ou F ; R4 étant -CH3 ; -C2H5 ; -CH2OH, CH2SCH3 ; -SCH3 ou -SC2H5 ; R5 étant -CH3 ou -C2H5 ; R6 étant H, ou représentant un ou plusieurs substituants 10, chacun étant indépendamment choisi parmi un alkyle en C1 à C6, un hydroxy, un halogène, et des radicaux de formules (IIIA), (IIIB) et (IIIC) : (IIIA)(IIIB)(IIIC) ; R61a et R61b étant indépendamment H ou un alkyle en C1 à C6, ou R61a et R61b pris conjointement avec l'azote auquel ils sont reliés formant un cycle hétérocyclique 15 à 6 chaînons contenant facultativement un autre hétéroatome choisi parmi N et O ; n étant 0, 1 ou 2 ; p étant 1 ou 2 ; R7 étant H ou F ; et R8 étant H ou CONH2.
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