Patent classifications
C07C67/313
NOVEL SALTS AND POLYMORPHIC FORM OF BEMPEDOIC ACID
The present invention relates to novel pharmaceutically acceptable salts of Bempedoic acid, novel intermediates of Bempedoic acid, novel crystalline form of Bempedoic acid and novel processes for the preparation of Bempedoic acid or its intermediates thereof.
BIFUNCTIONAL LINKER FOR BISCONJUGATION, METHOD OF SYNTHESIS, AND METHOD OF USE
A bifunctional linker of Formula 1
##STR00001##
wherein in Formula I, at least one of R.sup.1 to R.sup.4 is —COOR.sup.5 and R.sup.5 is —C.sub.0-C.sub.10alkyl(C.sub.2-C.sub.10alkynyl) or —C.sub.0-C.sub.10alkyl-C.sub.2-C.sub.10alkenyl(C.sub.2-C.sub.10alkynyl), preferably a terminal alkynyl. The bifunctional linker is used in a cycloaddition to tether two entities, for example a protein or antibody, and an active agent, to form a bisconjugate. The bifunctional linker also be used to form a conjugate, followed by cycloaddition in the presence of a comonomer composition to form a bisconjugate including a protein or antibody linked to an adhesive polymer network. Catalysis can be provided by a copper-containing paint on a surface to adhere the bisconjugate to the surface. Methods of synthesis and use of the bisconjugates imaging, diagnostic, and therapeutic applications are also described.
BIFUNCTIONAL LINKER FOR BISCONJUGATION, METHOD OF SYNTHESIS, AND METHOD OF USE
A bifunctional linker of Formula 1
##STR00001##
wherein in Formula I, at least one of R.sup.1 to R.sup.4 is —COOR.sup.5 and R.sup.5 is —C.sub.0-C.sub.10alkyl(C.sub.2-C.sub.10alkynyl) or —C.sub.0-C.sub.10alkyl-C.sub.2-C.sub.10alkenyl(C.sub.2-C.sub.10alkynyl), preferably a terminal alkynyl. The bifunctional linker is used in a cycloaddition to tether two entities, for example a protein or antibody, and an active agent, to form a bisconjugate. The bifunctional linker also be used to form a conjugate, followed by cycloaddition in the presence of a comonomer composition to form a bisconjugate including a protein or antibody linked to an adhesive polymer network. Catalysis can be provided by a copper-containing paint on a surface to adhere the bisconjugate to the surface. Methods of synthesis and use of the bisconjugates imaging, diagnostic, and therapeutic applications are also described.
PROCESS FOR THE PREPARATION OF CIS-ALPHA,BETA SUBSTITUTED CYCLOPENTANONES
Described herein is a process for the preparation of a mixture of compounds of formula
##STR00001##
having a weight ratio of the cis-diastereomers to trans-diastereoisomers higher than 1:1, where R.sub.1 represents a C.sub.1-8 alkyl group, a C.sub.2-8 alkenyl group or a C.sub.2-8 alkynyl group, each optionally substituted with one or two of a C.sub.1-4 alkyl alkoxy ether group and/or a C.sub.1-4 alkyl carboxylester group and R.sub.2 represents a C.sub.1-6 alkyl, a C.sub.2-6 alkenyl or a C.sub.2-6 alkynyl group, each optionally substituted with a C.sub.1-4 alkyl alkoxy ether group, a carboxylic acid group or a C.sub.1-4 alkyl carboxylester group and compounds suitable in the process.
PROCESS FOR THE PREPARATION OF CIS-ALPHA,BETA SUBSTITUTED CYCLOPENTANONES
Described herein is a process for the preparation of a mixture of compounds of formula
##STR00001##
having a weight ratio of the cis-diastereomers to trans-diastereoisomers higher than 1:1, where R.sub.1 represents a C.sub.1-8 alkyl group, a C.sub.2-8 alkenyl group or a C.sub.2-8 alkynyl group, each optionally substituted with one or two of a C.sub.1-4 alkyl alkoxy ether group and/or a C.sub.1-4 alkyl carboxylester group and R.sub.2 represents a C.sub.1-6 alkyl, a C.sub.2-6 alkenyl or a C.sub.2-6 alkynyl group, each optionally substituted with a C.sub.1-4 alkyl alkoxy ether group, a carboxylic acid group or a C.sub.1-4 alkyl carboxylester group and compounds suitable in the process.
MIXED OXIDES FOR THE OXIDATIVE CLEAVAGE OF LIPIDS USING OXYGEN TO AFFORD MONO- AND DI-CARBOXYLIC ACIDS
This invention relates to the synthesis of new catalysts based on earth crust abundant mixed oxides that can produce cleavage of fatty acids (FA), FA methyl esters, or even lipids in a single step using oxygen as oxidant in solventless conditions.
METHOD FOR PRODUCING BIFUNCTIONAL COMPOUND HAVING NORBORNANE SKELETON
The present invention provides a method for producing a bifunctional compound having a norbornane skeleton, the method comprising a step of hydroformylating a compound having an olefin with carbon monoxide and hydrogen, wherein the molar ratio of the carbon monoxide to the hydrogen during the reaction is 55/45 or more and 95/5 or less in the hydroformylating step.
METHOD FOR PRODUCING BIFUNCTIONAL COMPOUND HAVING NORBORNANE SKELETON
The present invention provides a method for producing a bifunctional compound having a norbornane skeleton, the method comprising a step of hydroformylating a compound having an olefin with carbon monoxide and hydrogen, wherein the molar ratio of the carbon monoxide to the hydrogen during the reaction is 55/45 or more and 95/5 or less in the hydroformylating step.
Catalyst and a Process for the Production of Ethylenically Unsaturated Carboxylic Acids or Esters
A catalyst has a modified silica support and comprises a modifier metal, zirconium and/or hafnium, and a catalytic metal on the modified support. The catalyst has at least a proportion, typically, at least 25%, of modifier metal present in moieties having a total of up to 2 modifier metal atoms. The moieties may be derived from a monomeric and/or dimeric cation source.
A method of production: provides a silica support with isolated silanol groups with optional treatment to provide isolated silanol groups (—SiOH) at a level of <2.5 groups per nm.sup.2; contacting the optionally treated silica support with a monomeric zirconium or hafnium modifier metal compound to effect adsorption onto the support; and optionally calcining the modified support for a time and temperature sufficient to convert the monomeric zirconium or hafnium compound adsorbed on the surface to an oxide or hydroxide of zirconium or hafnium in preparation for catalyst impregnation.
AN IMPROVED PROCESS FOR THE PREPARATION OF (2S)-2-[(4R)-2-OXO-4-PROPYLTETRAHYDRO-1H-PYRROL-1-YL] BUTANAMIDE AND ITS INTERMEDIATES THEREOF
The present invention relates to an improved process for the preparation of (2S)-2-[(4R)-2-oxo-4-propyltetrahydro-1H-pyrrol-1-yl] butanamide compound of formula-1, its intermediates, novel salt compounds of intermediates of the compound of formula-1. Further the use of novel salts in the preparation of the compound of formula-1. The present invention also relates to the novel process for the preparation of the compound of formula-1.