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US 2003/0158180 A1Published application
Naphthamide neurokinin antagonists for use as medicaments
OwnerPeter Bernsteininventor
Life of this patent
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Abstract
A compound having the general formula (Ia) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
Claims14
A compound having the formula
- 32
- wherein:
- R1 is —OR6, —NR6R7, —NOC1-6alkyl or —NR7NR6R7;
- R2 is —OR6 or C1-12alkyl;
- R3 is H, halogen, —OR7 or —CN;
- R4 is H, C1-6alkyl or —OR7;
- R5 is H or C1-6alkyl;
- R6 is independently, at each instance, H, C1-6alkyl, R7OC1-6alkyl-, R7C(=O)C1-6alkyl-, R7R7NC(═O)C1-6alkyl-, R7R7NC1-6alkylNR7C(═O)—, R8-, R8C1-6alkyl- or —(CH2)mphenyl, wherein the phenyl is substituted by 1, 2 or three substituents selected from C1-6allylthio, C1-6alkylsulfinyl, C1-6alkylsulfonyl, trifluoromethylthio, trifluoromethylsulfinyl, C1-6alkanesulfonamido, C1-6alkanoyl, C1-6alkoxy-carbonyl, succinamido, carbamoyl, C1-6alkylcarbamoyl, di-C1-6alkylcarbamoyl, C1-6alkoxy-C1-6alkylcarbamoyl, N-methylcarbamoyl, C1-6alkanoylamino, ureido, C1-6ureido, di-C1-6alkylureido, amino, C1-6alkylamino and di-C1-6alkylamino;
- R7 is independently, at each instance, H or C1-6alkyl;
- or
- R6 and R7 together are —(CH2)2O(CH2)2—, —(CH2)2S(═O)m(CH2)2—, —(CH2)2N(CO2R7)(CH2)2— or —(CH2)2NR7(CH2)2—;
- R8 is a 5- or 6-membered saturated or unsaturated heterocycle containing 1, 2 or 3 nitrogen atoms and additionally subsituted with 0 or 1 oxo groups;
- m is independently, at each instance 0, 1 or 2;
- and
- X1 and X2 are independently H, —CH3 or halogen;
- or any pharmaceutically-acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.