Patent classifications
C07D209/42
SUBSTITUTED INDOLE MCL-1 INHIBITORS
The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
BICYCLIC CARBOXAMIDES AND METHODS OF USE THEREOF
Compounds, compositions and methods are provided for modulating the activity of EP.sub.2 and EP.sub.4 receptors, and for the treatment, prevention and amelioration of one or more symptoms of diseases or disorders related to the activity of EP.sub.2 and EP.sub.4 receptors. In certain embodiments, the compounds are antagonists of both the EP.sub.2 and EP.sub.4 receptors.
BICYCLIC CARBOXAMIDES AND METHODS OF USE THEREOF
Compounds, compositions and methods are provided for modulating the activity of EP.sub.2 and EP.sub.4 receptors, and for the treatment, prevention and amelioration of one or more symptoms of diseases or disorders related to the activity of EP.sub.2 and EP.sub.4 receptors. In certain embodiments, the compounds are antagonists of both the EP.sub.2 and EP.sub.4 receptors.
FLOW CHEMISTRY SYNTHESIS OF ISOCYANATES
The disclosure provides, inter alia, safe and environmentally-friendly methods, such as flow chemistry, to synthesize isocyanates, such as methylene diphenyl diisocyanate, toluene diisocyanate, hexamethylene diisocyanate, isophorone diisocyanate, and tetramethylxylene diisocyanate.
CHEMICALS AND USE OF HYPOHALITES IN MECHANISM-BASED SELECTIVE DUAL RADICAL ORGANIC SYNTHESES
Embodiments of the present invention provide for syntheses of pattern-specific compounds using hypohalites, such as hypochlorous acid, sodium hypochlorite and potassium hypoiodite, as dual-radical generators, wherein the synthesis can be implemented by a cyclization reaction, a dehydrogenation reaction, a hydroxylation reaction, a decarboxylation reaction, or any combination of the above four.
METHYL 2-ALLYL-1 -METHYL-3-OXOINDOLINE-2-CARBOXYLATE AND 9A-ALLYL-1,2,3,9A-TETRAHYDRO- 9H-PYRROLO[1,2-A]INDOL-9-ONE DERIVATIVES AND RELATED COMPOUNDS FOR USE AS FLUORESCENT MARKERS FOR LABELLING OF DRUGS, AMINO ACIDS AN PROTEINS
Compounds of formulae (3) and (I) for use as fluorescent markers for labelling an amine containing target drug, an amino acid or a protein are disclosed. Exemplary compounds are e.g. (II) (III) (IV).
METHYL 2-ALLYL-1 -METHYL-3-OXOINDOLINE-2-CARBOXYLATE AND 9A-ALLYL-1,2,3,9A-TETRAHYDRO- 9H-PYRROLO[1,2-A]INDOL-9-ONE DERIVATIVES AND RELATED COMPOUNDS FOR USE AS FLUORESCENT MARKERS FOR LABELLING OF DRUGS, AMINO ACIDS AN PROTEINS
Compounds of formulae (3) and (I) for use as fluorescent markers for labelling an amine containing target drug, an amino acid or a protein are disclosed. Exemplary compounds are e.g. (II) (III) (IV).
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., (cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., (cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
MACROCYCLIC INDOLES AS MCL-1 INHIBITORS
Disclosed is compound of formula I and the pharmaceutically acceptable salts and solvates thereof, wherein R, R.sup.1a, R.sup.1b, R.sup.1h, L.sup.2, L.sup.3, #, #, # are as defined as set forth in the re) specification. Disclosed is compound of formula I for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.
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