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US 8,476,224 B2Granted
Macrocycles and their uses
AssigneeNovartis AG
InventorsRoger Aki Fujimoto, Philipp Krastel, Matthew J. Lamarche
Life of this patent
Estimating the term…
Abstract
The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
Claims12
A compound of Formula III:
- and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, atropisomers or racemates thereof, including pyridine N-oxides thereof;
- wherein
- q is 1, or 2 and the fragment
- is selected from the group consisting of:
- q is 0 and E-R1 is selected from the group consisting of:
- R1 is selected from the group consisting of hydrogen, hydroxymethyl, and aminomethyl and R12:
- R2a is hydrogen, hydroxy or amino, or is selected from the group consisting of C1-8alkoxy, amino, mono- and di-C1-8alkylamino, C3-7cycloalkylC0-6alkoxy, each of which is substituted with hydroxy, oxo, halo, C1-8alkyl, haloC1-8alkyl, C1-8alkoxy, haloC1-8alkoxy, C3-7cycloalkylC0-6alkyl, COOH, NH2, mono- and di-C1-8alkylamino, tri-C1-8alkylammonium, heterocycleC0-6alkyl, heteroarylC0-6alkyl, or —(CH2—CH2—O—)n—R8;
- R3 is selected from R12, OR12, N(R12)2 or R13;
- R4 is selected from hydrogen, CO2R4a, C(O)N(R4a)2, OR3a, N(R3a)2, or C(R10)(R11)phenyl;
- R4a is independently selected at each occurrence from hydrogen, hydroxymethyl, aminomethyl or R12;
- R6 is hydrogen or C1-4alkyl;
- R7 is selected from the group consisting of H, OH, NH2, C1-8alkyl, C1-8alkoxy, and mono- and di-C1-8alkylamino;
- R7b is independently selected at each occurrence from the group consisting of H, C1-8alkyl and —(CH2—CH2—O—)n—R8;
- R8 is independently selected at each occurrence from the group consisting of H, C1-8alkyl and CH2CO2H;
- R10 is absent or hydrogen;
- R11 is oxo, OR4a, N(R4a)2, or ═NR4a;
- R12 is independently selected at each occurrence from the group consisting of
- R13 is independently selected from the group consisting of
- n is an integer of between 1-60,000 or is a mean of a plurality of integers having a value of between 1-60,000;
- and
- p is 0, 1, 2, 3, or 4.
18 more elements
A compound of Formula IV
- and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, atropisomers or racemates thereof, including pyridine N-oxides thereof;
- wherein
- E is selected from the group consisting of C(O), C(O)C(O), C(O)O, N(R9), C(O)N(R9), N(R9)C(O), N(R9)C(O)C(O), N(R9)C(O)O, N(R9)C(O)N(R9), S(O)2, S(O)2N(R9), N(R9)S(O)2, and N(R9)S(O)2N(R9);
- R1 is hydrogen or is selected from the group consisting of C1-8alkyl, C2-8alkenyl, C2-8alkynyl, C1-8alkoxy, cycloalkylC0-6alkyl, heterocycloalkylC0-6alkyl, arylC0-6alkyl, heteroarylC0-6alkyl each of which is substituted with 0 to 6 residues independently selected at each occurrence from the group consisting of hydroxy, oxo, C1-8alkyl, C1-8alkoxy, C3-7cycloalkylC0-6alkyl, COOH, NH2, mono- and di-C1-8alkylamino, tri-C1-8alkylammonium, heterocycleC0-6alkyl, heteroarylC0-6alkyl and —(CH2—CH2—O—)n—R8;
- R8 is independently selected at each occurrence from the group consisting of H, C1-8alkyl and CH2CO2H;
- and
- R9 is hydrogen or is selected from the group consisting of C1-8alkyl, C2-8alkenyl, C2-8alkynyl, C1-8alkoxy, cycloalkylC0-6alkyl, heterocycloalkylC0-6alkyl, arylC0-6alkyl, heteroarylC0-6alkyl each of which is substituted with 0 to 6 residues independently selected at each occurrence from the group consisting of hydroxy, oxo, C1-8alkyl, C1-8alkoxy, C3-7cycloalkylC0-6alkyl, COOH, NH2, mono- and di-C1-8alkylamino, tri-C1-8alkylammonium, heterocycleC0-6alkyl, heteroarylC0-6alkyl and —(CH2—CH2—O—)n—R8.
4 more elements
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.