On May 3, 2007, Hurt, Clarence Ray; Pennell, Andrewm. K.; Wright, John Jessen; Wang, Qiang; Leleti, Manmohan Reddy; Thomas, William D.; Li, Yandong; Dragoli, Dean R. published a patent.Formula: C10H10O3 The title of the patent was Substituted dihydropyridines as C5a receptor modulators and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:
Compounds of formula I are provided that are modulators of the C5a receptor. Compounds of formula I wherein A is N or C; B is halo, CN, NO2, CO2H and derivatives, CONH2 and derivatives, NH and derivatives, etc.; R1 is H, amino, (un)substituted C1-8 (di)alkylamino, (un)substituted C1-8 alkoxy, (un)substituted C1-8 (halo)alkyl, etc.; C1 and C2 are independently (un)substituted (hetero)aryl, (un)substituted (hetero)aryl-C1-4 alkyl, (un)substituted (hetero)cycloalkyl, and (un)substituted (hetero)cycloalkyl-C1-4 alkyl; L1 is bond, (un)substituted C1-8 (hetero)alkylene, (un)substituted C1-8 alkenylene, (un)substituted C2-8 alkynylene, S, SO, SO2, O, NH and derivatives; R2 is OH and derivatives, NH2 and derivatives, C1-8 (halo)alkyl, C3-6 cycloalkyl, C2-8 alkenyl, (hetero)aryl, etc.; R3 is H, C1-6 (halo)alkyl, C1-6 acyl, C3-8 cycloalkyl, (hetero)aryl, etc.; D is O, S, and NOH and derivatives; and their pharmaceutically acceptable salts thereof, are claimed. The compounds are substituted dihydropyridines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathol. activation of C5a receptors. Example compound II was prepared by condensation of 4-methylbenzaldehyde with acetone; the resulting (E)-4-(4-methylphenyl)-3-buten-2-one underwent cyclization with di-Et malonate followed by decarboxylation to give 4-(4-methylphenyl)cyclohexane-1,3-dione, which underwent cyclization with 3-hydroxybenzaldehyde, cyclopentyl acetoacetate and ammonium acetate to give compound II. All the invention compounds were evaluated for their C5a receptor modulatory activity. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Formula: C10H10O3
The Article related to dihydropyridine preparation c5a receptor modulator treatment disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Formula: C10H10O3
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