Patent classifications
C07C2603/62
CONTINUOUS FLOW PROCESSES FOR MAKING BICYCLIC COMPOUNDS
Processes for making bicyclic compounds and precursors thereof, and particularly for making [1.1.1]propellane and bicyclo[1.1.1]pentane and derivatives thereof, utilize continuous flow reaction methods and conditions. A continuous process for making [1.1.1]propellane can be conducted under reaction conditions that advantageously minimize clogging of a continuous flow reactor. A continuous flow process can be used to make precursors of [1.1.1]propellane.
NOVEL SUBSTITUTED CYCLOBUTYLBENZENE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
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ESTROGEN RECEPTOR MODULATORS
Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.
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ESTROGEN RECEPTOR MODULATORS
Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.
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ESTROGEN RECEPTOR MODULATORS
Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.
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DISULFIDE BIOCONJUGATION
Compounds and methods are provided for one-step functionalization of disulfide bonds in proteins.
Cyclopropanation of substituted alkenes
Disclosed is a cyclopropanation process comprising the step of reacting an alkene compound having at least one carbon-carbon double bond with at least one dihaloalkane. The reaction is carried out in the presence of (i) particulate metal Zn, (ii) catalytically effective amount of particulate metal Cu or a salt thereof, (iii) at least one haloalkylsilane, and (iv) at least one solvent.
Method of preparing substituted bicyclo[1.1.1] pentanes
A process for the preparation of a class of molecules, namely bicyclo[1.1.1]pentanes and derivatives thereof by reaction of [1.1.1]propellane with a variety of reagents under irradiation and/or in the presence of radical initiators to obtain bicyclo[1.1.1]pentanes asymmetrically substituted at position 1 and 3, which are useful as intermediates for the preparation of asymmetrically 1,3-disubstituted bicyclo[1.1.1]pentane derivatives and various physiologically active substances or materials containing these structures.
MODULATORS OF G PROTEIN-COUPLED RECEPTOR 88
Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: (I) wherein Ring A, Ring B, Ring C, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, L, m, n, and p are as defined herein. The compounds are modulators of G-protein coupled receptor 88 (GPR88). Also disclosed are pharmaceutical compositions comprising the compounds; and the compounds for use in the treatment of diseases mediated by GPR88, including Tourette's Syndrome, Huntington's Disease (HD), Addiction, Parkinson's Disease (PD), Schizophrenia, Alzheimer's disease, and Attention Deficit Hyperactivity Disorder (ADHD).
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Compositions And Methods of Synthesizing Shape Shifting Cyclic Peptides (Sscp) And Their Use in The Identification of Novel Therapeutic Compounds
The invention described herein includes a novel platform for the development of novel shapeshifting drug-like compounds that overcome physical mass limitations as they possess the ability to interconvert internally and spontaneously, i.e., shapeshift, between multiple chemical structures with varying pharmacophore properties. In one preferred embodiment, the invention include systems, methods, and compositions for the synthesis of novel bullvalene amino acid (Bvas) compounds that may further be incorporated into Shape Shifting Cyclic Peptides (SSCP) with varying pharmacophore properties and their use as novel therapeutic compounds.