Patent classifications
C07C275/26
FATTY ACID ANALOGUES AND METHODS OF USE
Provided herein are compounds, pharmaceutical compositions, and methods of treatment for various diseases or conditions, such as cancer. In one aspect, the method comprises the treatment of metastatic cancers. Compounds and methods provided herein are also used for the treatment of diseases such as inflammatory disease, cardiovascular disease, autoimmune disease, and dry eye syndrome. Further provided herein are dietary supplement formulations and methods for supporting a healthy lifestyle.
MITOFUSIN ACTIVATORS AND METHODS OF USE THEREOF
Compositions including small molecule mitofusin activators are described. The mitofusin activators are useful for treating diseases or disorders associated with a mitochondria-associated disease, disorder, or condition such as diseases or disorders associated with mitofusin 1 (MFN1) and/or mitofusin 2 (MFN2), or mitochondrial dysfunction. Methods of treatment, pharmaceutical formulations, and screening methods for identifying compounds that activate mitochondrial fusion are also described.
Reactive antibacterial compound and preparation method thereof
A reactive antibacterial compound and a preparation method thereof are provided herein. The reactive antibacterial compound is represented by the general formula (I) or (II): ##STR00001##
wherein R.sub.1 represents OCN-L-NHCOOR′, OCN-L-NHCONHR′, OCN-L-NHCOSR′, OCN-L-COOR′, or OCN-L-COONHR′. G1 represents OCN-M-NHCOOG′, OCN-M-NHCONHG′, OCN-M-NHCOSG′, OCN-M-COOG′, or OCN-M-COONHG′. L, M, R′ and G′ independently for each occurrence represent divalent alkyl and cycloalkyl having from 1 to 18 carbon atoms, optionally substituted by up to 18 heteroatoms. R.sub.4 and G.sub.4 independently for each occurrence represent a divalent alkyl and cycloalkyl having from 1 to 18 carbon atoms, optionally substituted by at most 18 heteroatoms. G.sub.2 and G.sub.3 independently for each occurrence represent —H, —F, —Cl, —Br, —I, —OCH3, —OCH2CH3, —OPr, —CN, —SCN, —NO, —NO2, a monovalent unsubstituted or substituted alkyl, cycloalkyl, or aryl having from 1 to 7 carbon atoms. Z and X independently for each occurrence represent —COO, —SO3, or —OPO2OR.sub.5. R.sub.5 represents a monovalent unsubstituted or substituted alkyl, cycloalkyl, or aryl having from 1 to 6 carbon atoms.
Reactive antibacterial compound and preparation method thereof
A reactive antibacterial compound and a preparation method thereof are provided herein. The reactive antibacterial compound is represented by the general formula (I) or (II): ##STR00001##
wherein R.sub.1 represents OCN-L-NHCOOR′, OCN-L-NHCONHR′, OCN-L-NHCOSR′, OCN-L-COOR′, or OCN-L-COONHR′. G1 represents OCN-M-NHCOOG′, OCN-M-NHCONHG′, OCN-M-NHCOSG′, OCN-M-COOG′, or OCN-M-COONHG′. L, M, R′ and G′ independently for each occurrence represent divalent alkyl and cycloalkyl having from 1 to 18 carbon atoms, optionally substituted by up to 18 heteroatoms. R.sub.4 and G.sub.4 independently for each occurrence represent a divalent alkyl and cycloalkyl having from 1 to 18 carbon atoms, optionally substituted by at most 18 heteroatoms. G.sub.2 and G.sub.3 independently for each occurrence represent —H, —F, —Cl, —Br, —I, —OCH3, —OCH2CH3, —OPr, —CN, —SCN, —NO, —NO2, a monovalent unsubstituted or substituted alkyl, cycloalkyl, or aryl having from 1 to 7 carbon atoms. Z and X independently for each occurrence represent —COO, —SO3, or —OPO2OR.sub.5. R.sub.5 represents a monovalent unsubstituted or substituted alkyl, cycloalkyl, or aryl having from 1 to 6 carbon atoms.
METHOD FOR PRODUCING CARBAMATE AND METHOD FOR PRODUCING ISOCYANATE
The present invention provides a method for producing a carbamate that includes a step (1) and a step (2) described below: (1) a step of producing a compound (A) having a urea linkage, using an organic primary amine having at least one primary amino group per molecule and at least one compound selected from among carbon dioxide and carbonic acid derivatives, at a temperature lower than the thermal dissociation temperature of the urea linkage; and (2) a step of reacting the compound (A) with a carbonate ester to produce a carbamate.
METHOD FOR PRODUCING CARBAMATE AND METHOD FOR PRODUCING ISOCYANATE
The present invention provides a method for producing a carbamate that includes a step (1) and a step (2) described below: (1) a step of producing a compound (A) having a urea linkage, using an organic primary amine having at least one primary amino group per molecule and at least one compound selected from among carbon dioxide and carbonic acid derivatives, at a temperature lower than the thermal dissociation temperature of the urea linkage; and (2) a step of reacting the compound (A) with a carbonate ester to produce a carbamate.
CO-CRYSTAL OF SORAFENIB DERIVATIVES AND PROCESS FOR PREPARATION THEREOF
The present disclosure provides compounds for the inhibition of soluble epoxide hydrolase and associate disease conditions, as well as a method of treating or preventing disorders in a subject by inhibition of soluble epoxide hydrolase.
CO-CRYSTAL OF SORAFENIB DERIVATIVES AND PROCESS FOR PREPARATION THEREOF
The present disclosure provides compounds for the inhibition of soluble epoxide hydrolase and associate disease conditions, as well as a method of treating or preventing disorders in a subject by inhibition of soluble epoxide hydrolase.
INDUSTRIAL PROCESS FOR THE PREPARATION OF CARIPRAZINE
In the process of the present invention, cariprazine is prepared by converting (trans-4-amino-cyclohexyl)-acetic acid ethyl ester hydrochloride to trans-4-aminocyclohexyl) acetic acid or its hydrochloride by hydrolysis, from the obtained product with addition of dimethylcarbamoyl derivative as a suitable reagent (trans-4-{[(dimethylamino)carbonyl]amino}cyclohexyl) acetic acid is formed, then the obtained compound is linked to 1-{2,3-dichlorophenyl)˜piperazine in the presence of carboxylic acid activating coupling reagent, and so 1,1-dimethyl-3-[trans-4-(2-oxo-2-(4-(2,3-dichlorophenyl)piperazin-1-yl-ethyl)cyclohexyl] urea is formed, which is converted to cariprazine borane adduct of formula (2) in the presence of reducing agent, and finally the product itself is eliminated directly or is obtained from its salt by a known method. The invention also relates to a group of intermediate compounds that are formed and/or used in the process according to the present invention.
COATING COMPOSITION COMPRISING A THERMOSET RESIN AND A THERMOPLASTIC RESIN
A powder coating composition comprising: a) a thermoset resin comprising an acid functional polyester material, b) a thermoplastic resin and c) a crosslinker material,
wherein the coating composition is substantially free of bisphenol A (BPA), bisphenol F (BPF), bisphenol A diglycidyl ether (BADGE) and bisphenol F diglycidyl ether (BFDGE).