Novel compounds for treating inflammatory diseases

• Main Authors: RAINER WALTER, PETER NICKOLAUS, ROLF GOEGGEL, HORST DOLLINGER, JUERGEN MACK, JORG KLEY, RALF ANDERSKEWITZ, BIRGIT JUNG
• Format: Patent
• Language: English
• Published: 02.11.2006
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Heteroaryl derivatives (1) and their racemates, enantiomers, diastereomers, acid addition salts, solvates, hydrates and deuterated forms are new. Heteroaryl derivatives of formula (1) and their racemates, enantiomers, diastereomers, acid addition salts, solvates, hydrates and deuterated forms are new. A : CO, C=NH, 1-6C alkylene or 3-8C cycloalkylene; B1>phenyl or an aromatic or non-aromatic ring optionally containing two or three heteroatoms of O, S or N and optionally substituted with OH, O-1-6C alkyl, O-1-6C-haloalkyl, halo, 1-6C alkyl or 1-6C haloalkyl; B2>phenyl or hetero aryl containing 2 or 3 heteroatoms of O, S or N; X : e.g. O or S; n : 0-3; either R1>e.g. H, 1-6C alkyl, 1-6C haloalkyl; and R2>H, 1-6C alkyl or 1-6C haloalkyl; or NR1>R2>non-aromatic heterocycle containing 2 or 3 heteroatoms of O or N; or R2>+N+A+B1>bicyclic group of formula (g); A : CO, C=NH or 1-3C alkyl; m : 1-3; B1>sulfonyl compound of formula (h); Z1>H, OH, halo, 1-6C alkyl, 1-6C alkanol, O(1-6C alkyl), 6-10C aryl, O-6-10C aryl, NH2, NH(1-6C alkyl), N(1-6C) alkyl or 3-7C cycloalkyl; and R4>e.g. 1-6C alkyl, 3-8C cycloalkyl, 1-6C haloalkyl, CN or halo. Full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) a medicament combination comprising (1) and further active substance, such as beta-mimetic, anticholinergic, corticosteroid, further phosphodiesterase-4-inhibitors, leukotriene D4 antagonists, epidermal growth factor receptor inhibitor, dopamine agonists, H1-antihistaminic, platelet-activating factor antagonist and/or phosphatidylinositol-3 kinase inhibitor; and (2) intermediate compounds of formula (i-iii) or (I-V). PG : H or a suitable protection group; and G : NO2 or NH2. [Image] [Image] [Image] [Image] [Image] - ACTIVITY : Gastrointestinal-Gen.; Antidepressant; Neuroleptic; Antimanic; Neuroprotective; Nootropic; Antiparkinsonian; Analgesic; Cerebroprotective; CNS-Gen.; Respiratory-Gen.; Antiasthmatic; Antiinflammatory; Antiulcer. - MECHANISM OF ACTION : Phosphodiesterase-4 enzyme inhibitor.