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US 8,008,263 B2Granted
Organic compounds and their uses
AssigneeNovartis AG
InventorsShawn D. Britt, Lech Andrzej Ciszewski, Jiping Fu, Subramanian Karur, Yugang Liu, Peichao Lu, David Thomas Parker, Mahavir Prashad, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, 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.
Claims17
A compound of the Formula I:
- and pharmaceutically acceptable salts and stereoisomers thereof;
- wherein
- X is absent or selected from NR5a or oxygen;
- i and k are independently selected integers selected from the group consisting of 0, 1, 2, 3 and 4;
- j is an integer selected from the group consisting of 1, 2, 3 and 4, wherein the sum of i+j+k is less than or equal to 5 and greater than or equal to 2 when X is absent and the sum of i+j+k is less than or equal to 4 and greater than or equal to 1 when X is oxygen;
- p is 0, 1, 2 or 3;
- E is OH, NH2, N(H)C1-4alkyl, N(H)C3-6cycloalkyl, —C(O)NH— or —N(H)S(O)2—;
- R1 is absent, hydrogen, C1-4alkyl or C3-6cycloalkyl;
- R2 is C1-4alkyl, haloC1-4alkyl, or C3-6cycloalkylC0-2alkyl;
- R2a is hydrogen, C1-4alkyl, haloC1-4alkyl, or C3-6cycloalkylC0-2alkyl;
- or
- R2 and R2a, taken in combination form a three membered saturated ring, which ring is substituted with zero, one or two substituents independently selected from C1-4alkyl and C2-4alkenyl;
- R3 and R4 are independently selected from the group consisting of C1-6alkyl, C4-7cycloalkyl and C4-7cycloalkyl substituted with a C1-4alkyl residue;
- R5 represents zero to three residues on
- each independently selected at each occurrence from the group consisting of halogen, hydroxy, amino, C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, mono- and di-C1-4alkylamino, hydroxyC1-4alkyl, and C1-4alkoxyC1-4alkyl;
- R5a is independently selected at each occurrence from the group consisting of hydrogen, C1-4alkyl, haloC1-4alkyl, C3-6cycloalkyl, hydroxyC1-4alkyl, and C1-4alkoxyC1-4alkyl;
- and
- R6 and R7 are independently selected from hydrogen and C1-4alkyl.
15 more elements
A compound of the Formula Ia:
- and pharmaceutically acceptable salts and stereoisomers thereof;
- wherein
- i is an integer selected from the group consisting of 0, 1, 2, 3 and 4;
- j is an integer selected from the group consisting of 1, 2, 3 and 4, wherein the sum of i+j is less than or equal to 5 and greater than or equal to 2;
- p is 0, 1, 2 or 3;
- E is OH, NH2, N(H)C1-4alkyl, N(H)C3-6cycloalkyl, —C(O)NH— or —N(H)S(O)2—;
- R1 is absent, hydrogen, C1-4alkyl or C3-6cycloalkyl;
- R2 is C1-4alkyl, haloC1-4alkyl, or C3-6cycloalkylC0-2alkyl;
- R2a is hydrogen, C1-4alkyl, haloC1-4alkyl, or C3-6cycloalkylC0-2alkyl;
- or
- R2 and R2a, taken in combination form a three membered saturated ring, which ring is substituted with zero, one or two substituents independently selected from C1-4alkyl and C2-4alkenyl;
- R3 and R4 are independently selected from the group consisting of C1-6alkyl, C4-7cycloalkyl and C4-7cycloalkyl substituted with a C1-4alkyl residue;
- R5 represents zero to three residues on
- each independently selected at each occurrence from the group consisting of halogen, hydroxy, amino, C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, mono- and di-C1-4alkylamino, hydroxylC1-4alkyl, and C1-4alkoxyC1-4alkyl;
- R5a is independently selected at each occurrence from the group consisting of hydrogen, C1-4alkyl, haloC1-4alkyl, C3-6cycloalkyl, hydroxyC1-4alkyl, and C1-4alkoxyC1-4alkyl;
- and
- R6 and R7 are independently selected from hydrogen and C1-4alkyl.
14 more elements
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.