C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 65/26 (2006.01) A61K 31/00 (2006.01) C07C 43/235 (2006.01) C07C 43/247 (2006.01) C07C 45/68 (2006.01) C07C 47/575 (2006.01) C07C 49/755 (2006.01) C07C 49/84 (2006.01) C07C 69/94 (2006.01) C07C 217/80 (2006.01) C07C 233/25 (2006.01) C07C 235/42 (2006.01) C07C 243/38 (2006.01) C07C 251/34 (2006.01) C07C 251/44 (2006.01) C07C 251/48 (2006.01) C07C 251/66 (2006.01) C07C 255/54 (2006.01) C07C 259/10 (2006.01) C07C 275/32 (2006.01) C07C 275/34 (2006.01) C07D 237/32 (2006.01) C07F 9/38 (2006.01)
Patent
CA 2182792
A compound of structure (I), wherein, when R8 = H: R1 = alkyl, cycloalkyl, arylalkyl, aryl; R2 = cycloalkyl, aryl, C3-C10 alkyl; X, Y = O, S(O)n, NH; Z = CH2OH, NHSO2R3, CHO, CO2R3, CONHR4R5, CN, COR6, H, halo, NHCN, NHCONR4R5, CONR4OR5, CONR4NR5R6, 1-tetrazole, S(O)nOH, S(O)nNR3R4, C=NOH, C(=N(OH)NH2, OCONR7R6, P(O)(OR4)2, NH2, SH, OH, OS(O)2R3, C(O)CO2R3, C(O)CONR3R4, CH(OH)CO2R3, CHFCO2R3, CF2CO2R3, CH(OH)CONR3R4, CF2CONR3R4, C=NNH2, C(=NOC(=O)R3)R4, C(=NNHC(=O)R3)R4, C(=NOH)R3, C(=NNR3)R4, NHC(=O)R6 or C(O)CONH2; R3, R4, R5, R6, R7 = hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl; or a compound of Structure I, wherein: R1 = alkyl, cycloalkyl, aryalkyl, or aryl; R2 = cycloalkyl, aryl, or alkyl; X, Y = CH2, O, S(O)n), or NH; R3, R4, R5, R6, R7 are each, independently, hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl; R8 = CO2R3, CONR3, or R8 and Z are concatenated such that R8Z = C(O)NHNHC(O), (CH2)mC(=W), V(CH2)mC(=W), or VnCH=CH(CH2)nC(=W); where V = O, S(O)n, NH; W = O, NOH, NHNH2, NOC(O)CH3, or NNHC(O)CH3; halo = Cl, Br, or I; fluoroalkyl = CF3CHF2, CH2F, CH2CF3, C2F5; cycloalkyl = C3-C6 cycloalkyl; aryalkyl = C1-C4 aryl; aryl = phenyl, furanyl, thienyl, or pyridyl; n = 0-2; and m = 2-4 or pharmaceutically acceptable salts thereof, useful in the treatment of asthma, or allergic or inflammatory diseases, as well as methods of treatment and pharmaceutical compositions utilizing the same.
L'invention concerne un composé ayant la formule (I). Dans cette fomule, lorsque R¿8? = H, R¿1? = alkyle, cycloalkyle, arylalkyle, aryle; R¿2? = cycloalkyle, aryle, C¿3?-C¿10? alkyle; X, Y = O, S(O)¿n?, NH; Z = CH¿2?OH, NHSO¿2?R¿3?, CHO, CO¿2?R¿3?, CONHR¿4?R¿5?, CN, COR¿6?, H, halo, NHCN, NHCONR¿4?R¿5?, CONR¿4?OR¿5?, CONR¿4?NR¿5?R¿6?, 1-tétrazole, S(O)¿n?OH, S(O)¿n?NR¿3?R¿4?, C=NOH, C(=N(OH)NH¿2?, OCONR¿7?R¿6?, P(O)(OR¿4?)¿2?, NH¿2?, SH, OH, OS(O)¿2?R¿3?, C(O)CO¿2?R¿3?, C(O)CONR¿3?R¿4?, CH(OH)CO¿2?R¿3?, CHFCO¿2?R¿3?, CF¿2?CO¿2?R¿3?, CH(OH)CONR¿3?R¿4?, CF¿2?CONR¿3?R¿4?, C=NNH¿2?, C(=NOC(=O)R¿3?)R¿4?, C(=NNHC(=O)R¿3?)R¿4?, C(=NOH)R¿3?, C(=NNR¿3?)R¿4?, NHC(=O)R¿6? or C(O)CONH¿2?; R¿3?, R¿4?, R¿5?, R¿6?, R¿7? = hydrogène, alkyle, aryle, aryalkyle, cycloalkyle, ou fluoroalkyle; ou un composé de la formule (I), où R¿1? = alkyle, cycloalkyle, aryalkyle, or aryle; R¿2? = cycloalkyle, aryle, ou alkyle; X, Y = CH¿2?, O, S(O)¿n?), ou NH; R¿3?, R¿4?, R¿5?, R¿6?, R¿7? sont chacun d'une manière indépendante un hydrogène, alkyle, aryle, aryalkyle, cycloalkyle, ou fluoroalkyle; R¿8? = CO¿2?R¿3?, CONR¿3?, ou R¿8? et Z sont reliés pour que R¿8?Z = C(O)NHNHC(O), (CH¿2?)¿m?C(=W), V(CH¿2?)¿m?C(=W); ou V¿n?CH=CH(CH¿2?)¿n?C(=W); où V = O, S(O)¿n?, NH; W = O, NOH, NHNH¿2?, NOC(O)CH¿3?, ou NNHC(O)CH¿3?; halo = Cl, Br, or I; fluoroalkyle = CF¿3?CHF¿2?, CH¿2?F, CH¿2?CF¿3?, C¿2?F¿5?; cycloalkyle = C¿3?-C¿6? cycloalkyle; aryalkyle = C¿1?-C¿4? aryle; aryle = phényle, furanyle, thiényle, or pyridyle; n = 0-2; et m = 2-4. L'invention concerne également les sels de ces composés, acceptables sur le plan pharmaceutique. Ces produits sont utiles pour le traitement de l'asthme, d'allergies ou de maladies inflammatoires. L'invention concerne également des compositions pharmaceutiques contenant ces produits et leur utilisation.
Caggiano Thomas J.
Prol Joseph Jr.
American Home Products Corporation
Ridout & Maybee Llp
LandOfFree
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