Patent classifications
C07D513/08
SALTS AND POLYMORPHS OF CERTAIN MCL-1 INHIBITORS
The present disclosure relates salts and the crystalline forms of certain 3′,4,4′,5-tetrahydro-2H,2′H-spiro[benzo[b][1,4]oxazepine-3,1′-naphthalene] derivatives as well as pharmaceutical formulations and therapeutic uses thereof. The present disclosure also relates to preparing such salts, crystalline forms and pharmaceutical formulations.
Mono- or di-substituted indole derivatives as dengue viral replication inhibitors
The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using the compounds and also relates to use of the compounds as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
Mono- or di-substituted indole derivatives as dengue viral replication inhibitors
The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using the compounds and also relates to use of the compounds as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
NITROGEN-CONTAINING CONDENSED RING COMPOUNDS HAVING DOPAMINE D3 ANTAGONISTIC EFFECT
Novel compounds having D3 receptor antagonistic activity are provided.
A compound represented by formula (I):
##STR00001##
wherein ring A is a heterocycle, X.sup.1 is each independently CR.sup.4aR.sup.4b, X.sup.2 is each independently CR.sup.4cR.sup.4d, Y.sup.1 and Y.sup.2 are each independently a carbon atom or a nitrogen atom, L is —N(R.sup.6)—C(═O)— or the like, W is cyclyl or the like, R.sup.2 and R.sup.3 are each independently substituted or unsubstituted alkyl or the like, R.sup.1a, R.sup.1b, R.sup.4a to R.sup.4d, and R.sup.6 are each independently hydrogen atoms or the like, p is 1 or 2, q is an integer of 1 to 3, n is an integer of 1 to 4, s is an integer of 0 to 4, or a pharmaceutically acceptable salt thereof.
NITROGEN-CONTAINING CONDENSED RING COMPOUNDS HAVING DOPAMINE D3 ANTAGONISTIC EFFECT
Novel compounds having D3 receptor antagonistic activity are provided.
A compound represented by formula (I):
##STR00001##
wherein ring A is a heterocycle, X.sup.1 is each independently CR.sup.4aR.sup.4b, X.sup.2 is each independently CR.sup.4cR.sup.4d, Y.sup.1 and Y.sup.2 are each independently a carbon atom or a nitrogen atom, L is —N(R.sup.6)—C(═O)— or the like, W is cyclyl or the like, R.sup.2 and R.sup.3 are each independently substituted or unsubstituted alkyl or the like, R.sup.1a, R.sup.1b, R.sup.4a to R.sup.4d, and R.sup.6 are each independently hydrogen atoms or the like, p is 1 or 2, q is an integer of 1 to 3, n is an integer of 1 to 4, s is an integer of 0 to 4, or a pharmaceutically acceptable salt thereof.
Macrocyclic compounds that inhibit MCL-1 protein
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stenoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer. ##STR00001##
Macrocyclic compounds that inhibit MCL-1 protein
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stenoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer. ##STR00001##
QUINOLINYL-PYRAZINE-CARBOXAMIDE COMPOUNDS AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a quinolinyl-pyrazine-carboxamide (or similar) structure which function as activators of the cholesterol biosynthesis pathway within cancer cells and/or immune cells, which function as activators of the cell cycle regulation pathway within cancer cells and/or immune cells, and which function as up-regulators of HMGCS1 protein expression within cancer cells and/or immune cells, and which function as effective therapeutic agents for treating, ameliorating, and preventing various forms of cancer and other inflammatory disease.
Macrocycles as factor XIA inhibitors
The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
MACROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.