Patent classifications
C07D473/24
HIV INHIBITING BICYCLIC PYRIMIDINE DERIVATIVES
HIV replication inhibitors of formula
##STR00001##
N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a.sup.1=a.sup.2-a.sup.3=a.sup.4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b.sup.1=b.sup.2-b.sup.3=b.sup.4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; optionally substituted C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; R.sup.2 is OH; halo; optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O).sub.pR.sup.6; C(═NH)R.sup.6; R.sup.2a is CN; amino; substituted amino; optionally substituted C.sub.1-6alkyl; halo; optionally substituted C.sub.1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R.sup.16; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; —C(═N—O—R.sup.8)—C.sub.1-4alkyl; R.sup.7 or X—R.sup.7; R.sup.3 is CN; amino; C.sub.1-6alkyl; halo; optionally substituted C.sub.1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; —C(═N—O—R.sup.8)—C.sub.1-4alkyl; R.sup.7; —X—R.sup.7; R.sup.4 is halo; OH; optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; C.sub.3-7cycloalkyl; C.sub.1-6alkyloxy; CN; nitro; polyhaloC.sub.1-6alkyl; polyhaloC.sub.1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C.sub.1-4alkyl)amino or R.sup.7; -A-B— is —CR.sup.5═N—, —N═N—, —CH.sub.2—CH.sub.2—, —CS—NH—, —CO—NH—, —CH═CH—;
pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.
2-AMINO-S6-SUBSTITUTED THIOPURINE COMPOUNDS AS INHIBITORS OF THE ENPP1 PROTEIN
Compounds, pharmaceutical compositions, and methods are provided herein that may be used to treat cancer, infectious disease, and other conditions associated with ectonucleotide pyrophosphatase pyrophosphatase-phosphodiesterase (ENPP1) dysfunction.
2-AMINO-S6-SUBSTITUTED THIOPURINE COMPOUNDS AS INHIBITORS OF THE ENPP1 PROTEIN
Compounds, pharmaceutical compositions, and methods are provided herein that may be used to treat cancer, infectious disease, and other conditions associated with ectonucleotide pyrophosphatase pyrophosphatase-phosphodiesterase (ENPP1) dysfunction.
Heterocyclic compounds and uses as anticancer agents
The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
Heterocyclic compounds and uses as anticancer agents
The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
STABILIZATION OF MHC COMPLEXES
Provided, inter alia, are methods and compositions for treating cancer.
STABILIZATION OF MHC COMPLEXES
Provided, inter alia, are methods and compositions for treating cancer.
HIV inhibiting bicyclic pyrimidine derivatives
HIV replication inhibitors of formula ##STR00001##
N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a.sup.1=a.sup.2-a.sup.3=a.sup.4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b.sup.1=b.sup.2-b.sup.3=b.sup.4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; optionally substituted C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; R.sup.2 is OH; halo; optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O).sub.pR.sup.6; C(═NH)R.sup.6; R.sup.2a is CN; amino; substituted amino; optionally substituted C.sub.1-6alkyl; halo; optionally substituted C.sub.1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R.sup.16; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; —C(═N—O—R.sup.8)—C.sub.1-4alkyl; R.sup.7 or —X—R.sup.7; R.sup.3 is CN; amino; C.sub.1-6alkyl; halo; optionally substituted C.sub.1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; —C(═N—O—R.sup.8)—C.sub.1-4alkyl; R.sup.7; —X—R.sup.7; R.sup.4 is halo; OH; optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; C.sub.3-7cycloalkyl; C.sub.1-6alkyloxy; CN; nitro; polyhaloC.sub.1-6alkyl; polyhaloC.sub.1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C.sub.1-4alkyl)amino or R.sup.7; -A-B— is —CR.sup.5═N—, —N═N—, —CH.sub.2—CH.sub.2—, —CS—NH—, —CO—NH—, —CH═CH—;
pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.
METFORMIN DERIVATIVES
The present invention relates to novel biguanide derivatives including their pharmaceutically acceptable salts. The invention also relates processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing and the uses of such compounds in treating disorders such as diabetes.
Sulfonimidoylpurinone compounds and methods of treatment using the same
The present invention relates to compounds of formula (I), ##STR00001## wherein R.sup.1, R.sup.2 and R.sup.3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.