C07D263/22

TETRADENTATE LIGAND, AND PRODUCTION METHOD THEREFOR, SYNTHETIC INTERMEDIATE THEREOF, AND TRANSITION METAL COMPLEX THEREOF

The present invention relates to: a compound as a ligand in a variety of catalytic organic synthetic reactions; a method for producing the compound; a synthetic intermediate of the compound; and a transition metal complex which has the compound as a ligand. The compound includes a compound represented by the following general formula (1.sup.A):

##STR00001##

Cyclopropylamine compounds as histone demethylase inhibitors

The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R.sup.1, and R.sup.2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy. ##STR00001##

Cyclopropylamine compounds as histone demethylase inhibitors

The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R.sup.1, and R.sup.2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy. ##STR00001##

HEPATITIS B ANTIVIRAL AGENTS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:


X-A-Y-L-R(I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Necrosis Inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Necrosis Inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

NAMPT MODULATORS

Provided are compounds of Formula (I):

##STR00001## or a pharmaceutically acceptable salt thereof, wherein Ring A, Ring B, L, R.sup.B, R.sup.C, n, and p are as defined herein.

Also provided are pharmaceutically acceptable compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

SYNTHESIS OF N-VINYL COMPOUNDS BY REACTING NH-COMPOUNDS WITH ACETYLENE IN PRESENCE OF HOMOGENEOUS PHOSPHINE CATALYST

A process to produce N-vinyl compounds by homogeneous catalysis can be performed. Acetylene is reacted with a compound having at least one nitrogen bearing a substitutable hydrogen residue in a liquid phase in the presence of at least one phosphine as a catalyst to produce the compounds.

Necrosis inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

METHOD FOR CATALYTICALLY ACTIVATING CARBON DIOXIDE AS CARBONYLATION REAGENT WITH INORGANIC SULFUR

Provided is a method for catalytically activating carbon dioxide as a carbonylation reagent with inorganic sulfur. In the method, carbon dioxide can be used to replace a toxic and harmful carbonylation reagent in the presence of H.sub.2S and an alkali for the synthesis of a carbonyl-containing fine chemical product. The method has a relatively high atomic economy and can reduce the generation of by-products.