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US 2012/0231998 A1Published application
Organic compounds and their uses
AssigneeNovartis AG
InventorsTrixi Brandl, Jiping Fu, Francois Lenoir, David Thomas Parker, Michael Patane, Branko Radetich, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic, Aregahegn Yifru, Rui Zheng
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Abstract
The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
Claims11
1-69. (canceled)
A method of treating HCV infection in subject in need thereof, comprising:
- administering to the subject a pharmaceutically acceptable amount of a compound of the Formula I:
- and pharmaceutically acceptable salts and stereoisomers thereof;
- wherein
- y is 0 or 1;
- n and p are each independently 0, 1 or 2;
- R14 is C(O) or SO2;
- R1, R2, W, R13 and V are each, independently, selected from hydrogen or from the group consisting of alkyl, alkyl-aryl, heteroalkyl, heterocyclyl, heteroaryl, aryl-heteroaryl, alkyl-heteroaryl, cycloalkyl, alkyloxy, alkyl-aryloxy, aryloxy, heteroaryloxy, heterocyclyloxy, cycloalkyloxy, amino, alkylamino, arylamino, alkyl-acylamino, arylamino, heteroarylamino, cycloalkylamino, carboxyalkylamino, mono- and di-alkylcarboxamide, aralkyloxy and heterocyclylamino;
- each of which may be further independently substituted one or more times with X1 and X2;
- wherein X1 is alkyl, alkenyl, alkenyl, cycloalkyl, cycloalkyl-alkyl, heterocyclyl, heterocyclylalkyl, aryl, alkylaryl, aralkyl, aryloxy, arylthio, arylheteroaryl, heteroaryl, heterocyclylamino, alkylheteroaryl, or heteroaralkyl;
- wherein X1 can be independently substituted with one or more X2 moieties which can be the same or different and are independently selected;
- wherein X2 is hydroxy, oxo, alkyl, cycloalkyl, spirocycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkoxy, aryloxy, thio, alkylthio, amino, mono- and di-alkylamino, arylamino, alkylsulfonyl, arylsulfonyl, alkylsulfonamido, arylsulfonamido, carboxy, carbalkoxy, carboxamido, alkoxycarbonylamino, alkoxycarbonyl, alkoxycarbonyloxy, alkylureido, arylureido, halogen, cyano, or nitro;
- wherein each X2 residue selected to be alkyl, alkoxy, and aryl can be unsubstituted or optionally independently substituted with one or more moieties which can be the same or different and are independently selected from alkyl, alkenyl, alkenyl, cycloalkyl, cycloalkyl-alkyl, heterocyclyl, heterocyclylalkyl, aryl, alkylaryl, aralkyl, arylheteroaryl, heteroaryl, heterocyclylamino, alkylheteroaryl and heteroaralkyl;
- W is also selected from the group consisting of C(O)—C(O)H, C═N—O—R24—C(O)-amine, C(O)—C(O)-amine, C(O)NR24S(O)pR24, C(O)NR24S(O)pN(R24)2 and C(O)—[C(O)]a-heterocycle, wherein the heterocycle may be independently substituted one or more times with aryl, C1-4-alkyl, C1-4-alkyl substituted by one or more halogen atoms, and C3-6-cycloalkyl, wherein a is 0 or 1, wherein each R24 is independently selected from hydrogen or the group consisting of C1-4-alkyl, C3-6-cycloalkylC0-4alkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocycle, each of which may be independently substituted one or more times with a halogen atom or C1-4-alkyl;
- V is also selected from the group consisting of -Q1-Q2, wherein Q1 is absent, C(O), N(H), N(C1-4-alkyl), C═N(CN), C═N(SO2CH3), C═N—COH—C1-4-alkyl, or C═N—COH, and Q2 is hydrogen or is selected from the group consisting of C1-4-alkyl, O—C1-4-alkyl, NH2, N(H)—C1-4-alkyl, N(C1-4-alkyl)2, SO2-aryl, SO2—C1-4-alkyl, C3-6-cycloalkyl-C0-4-alkyl, aryl, heteroaryl and heterocycle, each of which may be independently substituted one or more times with a halogen atom C1-4-alkyl, C1-4-alkyl substituted by one or more halogen atoms, or C3-6-cycloalkyl;
- or R1 and R2 may together form a 3, 4, 5, 6 or 7-membered ring that is aromatic or non-aromatic and may contain one or more heteroatoms, wherein the ring may be further substituted one or more times;
- R3 is selected from the group consisting of hydrogen, C1-4-alkyl and C3-6cycloalkylC0-4alkyl;
- the divalent residue:
- is selected from the group consisting of:
- R8, R9, R10, R11 and R12 are each, independently, selected from the group consisting of hydrogen, C1-4-alkyl and C3-6cycloalkylC0-4alkyl;
- or R3 and W may together form a 3, 4, 5, 6 or 7-membered ring that is aromatic or non-aromatic and may contain one or more heteroatoms, wherein the ring may be further substituted one or more times;
- and
- or when y is 0, R10 and V may together form a 3, 4, 5, 6 or 7-membered ring that is aromatic or non-aromatic and may contain one or more heteroatoms, wherein the ring may be further substituted one or more times.
19 more elements
71-73. (canceled)
Dependencies are inferred from the claim text.