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1. WO2009053269 - NOVEL KINASE INHIBITORS

Publication Number WO/2009/053269
Publication Date 30.04.2009
International Application No. PCT/EP2008/063758
International Filing Date 14.10.2008
IPC
C07D 213/63 2006.01
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
62Oxygen or sulfur atoms
63One oxygen atom
C07D 401/12 2006.01
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
12linked by a chain containing hetero atoms as chain links
C07D 401/14 2006.01
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
14containing three or more hetero rings
C07D 403/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14containing three or more hetero rings
C07D 409/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 413/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
A61P 17/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH]/[CH] (AllExceptUS)
  • DEWDNEY, Nolan James [US]/[US] (UsOnly)
  • GABRIEL, Tobias [DE]/[CH] (UsOnly)
  • KONDRU, Rama K. [IN]/[US] (UsOnly)
  • LOU, Yan [CN]/[US] (UsOnly)
  • SOTH, Michael [US]/[US] (UsOnly)
Inventors
  • DEWDNEY, Nolan James
  • GABRIEL, Tobias
  • KONDRU, Rama K.
  • LOU, Yan
  • SOTH, Michael
Agents
  • HEIROTH, Ulrike
Priority Data
61/000,13923.10.2007US
61/086,41605.08.2008US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL KINASE INHIBITORS
(FR) NOUVEAUX INHIBITEURS DE KINASE
Abstract
(EN)
Pyridine and pyrimidine compounds according to formula (I) wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula (I) and at least one carrier, diluent or excipient.
(FR)
L'invention concerne des composés de pyridine et de pyrimidine selon la formule (I), dans laquelle R1, R2, R3, R4, R5, X1 et A sont tels que décrits dans le présent document, qui inhibent Btk. Les composés décrits dans le présent document sont utiles pour moduler l'activité de Btk et pour traiter les maladies associées avec une activité excessive de Btk. Les composés sont également utiles pour traiter des maladies inflammatoires et auto-immunes associées avec une prolifération aberrante des cellules B, telles que l'arthrite rhumatoïde. L'invention concerne également des compositions qui contiennent des composés de formule I et au moins un véhicule, diluant ou excipient.
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