Organic compounds
AssigneeNovartis AG
InventorsYen Liang CHEN, Jeyaraj DURAISWAMY, Sarah HALLER, Matthias KEIM, Ravinder Reddy KONDREDDI, Zheng YIN
Life of this patent
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Abstract
This invention relates to novel compounds that have various medicinal applications, e.g. for the treatment and/or prevention of viral infections.
Claims12
A compound of formula (I), or a pharmaceutically acceptable salt thereof:
- wherein:
- X is CH or CR6;
- R1 is halogen, NR7R8 or OR9;
- R2 is H, halogen, or NR7R8;
- R3 is H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, each of which is optionally substituted with one or more substituents;
- R4 is H, acyl or an amino acid ester;
- R5 is H, acyl or an amino acid ester;
- R6 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, heteroaryl, halogen, cyano, nitro, hydroxy, alkoxy, alkylthio, amino, alkylamino, carboxy, carboxamide or alkyloxycarbonyl, each of which is optionally substituted with one or more substituents;
- R7 and R8 are independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, heteroaryl, amino, alkylamino, arylamino, hydroxy, alkoxy, arylcarbonyl and alkylcarbonyl, each of which is optionally substituted with one or more substituents;
- and
- R9 is H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, heteroaryl, alkylcarbonyl or arylcarbonyl, each of which is optionally substituted with one or more substituents;
- wherein R4 and R5 are not both H.
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
A compound of formula:
- or a pharmaceutically acceptable salt thereof.
A compound selected from the group consisting of:
- (2R,3R,4R,5R)-2-(4-amino-pyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-hydroxymethyl-tetrahydrofuran-3,4-diol, a compound of formula (I),
- which shows an X-ray powder diffraction pattern having peaks, expressed in degrees 2θ±0.2 degrees 2θ, at about 2.3, 4.4, 21.4 and 23.8, or which exhibits an X-ray powder diffraction pattern substantially as shown in FIG. 4;
- and
- (2R,3R,4R,5R)-2-(4-amino-pyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-hydroxymethyl-tetrahydrofuran-3,4-diol, a compound of formula (I),
- which shows an X-ray powder diffraction pattern having peaks, expressed in degrees 2θ±0.2 degrees 2θ, at about 13.3, 14.4, 16.4, 18.3, 20.7, 26.1, 26.9 and 29.3, or which exhibits an X-ray powder diffraction pattern substantially as shown in FIG. 5.
A compound selected from the group consisting of (2R,3R,4R,5R)-2-(4-amino-pyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-hydroxymethyl-tetrahydrofuran-3,4-diol salicylate salt and (2R,3R,4R,5R)-2-(4-amino-pyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-hydroxymethyl-tetrahydrofuran-3,4-diol 2:1 napadisylate salt.
(2R,3R,4R,5R)-2-(4-amino-pyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-hydroxymethyl-tetrahydrofuran-3,4-diol salicylate salt which shows an X-ray powder diffraction pattern having peaks, expressed in degrees 2θ±0.2 degrees 2θ, at about 7.5, 10.7, 11.9, 13.1, 14.2, 15.1, 16.0, 17.0, 19.4, 20.9, 22.0, 22.9, 24.0, 25.9 and 27.0, or which exhibits an X-ray powder diffraction pattern substantially as shown in FIG. 2.
(2R,3R,4R,5R)-2-(4-amino-pyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-hydroxymethyl-tetrahydrofuran-3,4-diol 2:1 napadisylate salt which shows an X-ray powder diffraction pattern having peaks, expressed in degrees 2θ±0.2 degrees 2θ, at about 7.3, 10.4, 14.6, 15.4, 17.3, 18.5, 21.0, 22.0, 22.9, 23.8, 25.1, 26.6, 27.0, 29.2 and 30.2, or which exhibits an X-ray powder diffraction pattern substantially as shown in FIG. 3.
Dependencies are inferred from the claim text.