C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 213/74 (2006.01) A61K 31/4409 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61K 31/4725 (2006.01) A61K 31/496 (2006.01) A61K 31/5355 (2006.01) A61K 31/5377 (2006.01) A61K 31/55 (2006.01) A61K 31/675 (2006.01) A61P 35/00 (2006.01) C07D 401/12 (2006.01) C07D 413/12 (2006.01) C07F 9/44 (2006.01)
Patent
CA 2728806
The present application discloses novel squaric acid derivatives of the formula A: from -C(=O)-, -S(=O)2-, -C(=S)- and -P(=O)(R5)-; B: -, -O-, -NR6- and -C(=O)-NR6-; D : -, -O-, -CR7R8- and -NR9; m=0-12; n = 0-12; m+n = 1-20; p=0-2; R1 : heteroaryl, aryl; R2 : H, C1-12-alkyl, C3-12-cy- cloalkyl, -[CH2CH20]1-10-(C1-6-alkyl),C1-12-alkenyl, aryl, heterocyclyl, het- eroaryl; R3 : C1-12-alkyl, C3-12-cycloalkyl, -[CH2CH20]1-10-(C1-6-alkyl), C1- 12- alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3 : N-containing hetero- cyclic/heteroaromatic ring; R4 and R4* : H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and viral infections, adult respiratory distress syndrome, ataxia telengiectasia).
Cette invention concerne de nouveaux dérivés de lacide squarique de formule A : à partir de -C(=O)-, -S(=O)2-, -C(=S)- et de -P(=O)(R5)-; B : -, -O-, -NR6- et -C(=O)-NR6-; D : -, -O-, -CR7R8- et -NR9; m = 0 à 12; n = 0 à 12; m+n = 1 à 20; p = 0 à 2; R1 : hétéroaryle, aryle; R2 : H, C1-12-alkyle, C3-12-cycloalkyle, -[CH2CH2O]1-10-(C1-6-alkyle),C1-12-alcényle, aryle, hétérocyclyle, hétéroaryle; R3 : C1-12-alkyle, C3-12-cycloalkyle, -[CH2CH2O]1-10-(C1-6-alkyle), C1-12-alcényle, aryle, hétérocyclyle, hétéroaryle; ou R2 et R3 : cycle hétérocyclique/hétéroaromatique azoté; R4 et R4* : H, C1-12-alkyle, C1-12-alcényle; et leurs sels et promédicaments pharmaceutiquement acceptables, et leur utilisation dans le traitement des maladies/affections causées par une augmentation du taux de NamPRT (inflammations et troubles des réparations tissulaires, en particulier la polyarthrite rhumatoïde, les maladies inflammatoires chroniques intestinales, lasthme et la BPCO, lostéoarthrite, lostéoporose et les affections fibrogènes; la dermatose; les maladies auto-immunes dont le lupus érythémateux systémique, la sclérose en plaques, larthrite psoriasique, la spondylarthrite ankylosante, le rejet de greffe (tissus et organes), la maladie dAlzheimer, laccident vasculaire cérébral, lathérosclérose, la resténose, le diabète, la glomérulonéphrite, le cancer, la cachexie, linflammation associée avec linfection et les infections virales, le syndrome de détresse respiratoire de ladulte, la télangiectasie).
Bjoerkling Fredrik
Christensen Mette Knak
Sim & Mcburney
Topotarget A/s
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