14 results about "CETP inhibitor" patented technology

The invention belongs to the technical field of chemical synthesis of medicines, and particularly relates to a preparation method of a CETP inhibitor Obicterapib. The invention provides three preparation schemes. According to the scheme I, 2-phenyl pentenoate and (R)-N-(1-phenethyl)-4-(trifluoromethyl) aniline are subjected to a reaction, and a target compound Obicterapib is prepared through hydrolysis, cyclization, acylation, asymmetric chiral amine and other multi-step reactions; according to the second scheme, 4-halogenated benzotrifluoride reacts with (R)-3-amino valeronitrile, then nitrile hydrolysis is carried out, the product reacts with ethyl chloroformate, bis (trifluoromethyl) benzyl bromide, bis (pinacolato) diboron and ethyl 4-bromobutyrate, and finally hydrolysis is carried out to prepare the target compound Obictapib. According to the third scheme, (R)-3-(4-trifluoromethyl-phenyl amino)-valeric acid is substituted by amino to obtain a compound (R)-3-[4-(trifluoromethyl) phenyl amino]-valeric acid amide, then the compound (R)-3-[4-(trifluoromethyl) phenyl amino]-valeric acid amide reacts with ethyl chloroformate, bis (trifluoromethyl) benzyl bromide, bis (pinacolato) diboron, ethyl 4-bromobutyrate and 5-bromine-2-chloropyrimidine, and finally hydrolysis is conducted to prepare the target compound Obictapib.

The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor for use in the treatment of a subject suffering from or at an increased risk of cardiovascular disease, in particular hyperlipidemia or mixed dyslipidemia. Another aspect of the invention relates to a pharmaceutical composition for treating a subject suffering from or having an increased risk of cardiovascular disease, wherein the composition comprises a therapeutically effective amount of the CETP inhibitor.

This invention relates to methods and compositions useful in subjects suffering from or at risk of suffering from sepsis or other dysregulated inflammatory responses. It has been demonstrated that the CETP inhibitor obicetrapib not only preserved or increased HDL-C and Apo A1 levels, but also reduced an important pro-inflammatory marker, IL-1β, and significantly increased survival, relative to placebo, in a suitable sepsis mouse model. Thus, broadly stated, the present invention concerns the use of CETP inhibitors in the prevention, treatment, management or amelioration of sepsis, or other dysregulated inflammatory responses in a subject.

Genotyping methods and compositions for selecting patients with cardiovascular disease who will benefit from treatment with HDL-raising or HDL mimicking agent, in particular with a CETP inhibitor / modulator.

The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor for use in the treatment of an individual suffering from or at increased risk of cardiovascular disease, in particular hyperlipidemia or mixed dyslipidemia. Another aspect of the invention relates to a pharmaceutical composition for use in the treatment of an individual suffering from or at increased risk of cardiovascular disease, wherein the composition comprises a therapeutically effective amount of the CETP inhibitor.

The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor:(Compound A) for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia. A further aspect of the present invention relates to a pharmaceutical composition for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, wherein the composition comprises a therapeutically effective amount of said Compound A CETP inhibitor.

Cholesteryl ester transfer protein inhibitors for use in the treatment or prevention of cardiovascular disease and pharmaceutical compositions containing the same. The present invention relates to cholesteryl ester transfer protein (CETP) inhibitors for use in the treatment of an individual suffering from or at increased risk of cardiovascular disease, in particular hyperlipidemia or mixed dyslipidemia. Another aspect of the invention relates to a pharmaceutical composition for use in the treatment of an individual suffering from or at increased risk of cardiovascular disease, wherein the composition comprises a therapeutically effective amount of the CETP inhibitor.

This invention relates to methods and compositions useful in subjects with age- related macular degeneration, in particular dry age-related macular degeneration. It has been demonstrated that the CETP inhibitor obicetrapib increases the plasma level of pre-beta-1 HDL, as well as total plasma lutein, zeaxanthin and tocopherol. More in particular, it has been found that the levels of these lipophilic anti-oxidants are also particularly elevated in pre-beta-1 HDL, which can pass the BrM and reach the retina with relative ease. These constitute particularly strong support for the treatment of AMD using a CETP inhibitor. Thus, broadly stated, the present invention concerns the use of CETP inhibitors in the treatment of age related macular degeneration.

Cholesteryl ester transfer protein inhibitors and pharmaceutical compositions containing the same for use in the treatment or prevention of cardiovascular diseases. The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor for use in the treatment of a subject suffering from or at an increased risk of cardiovascular disease, in particular hyperlipidemia or mixed dyslipidemia. Another aspect of the invention relates to a pharmaceutical composition for treating a subject suffering from or having an increased risk of cardiovascular disease, wherein the composition comprises a therapeutically effective amount of the CETP inhibitor.

This invention relates to methods and compositions useful in subjects with age-related macular degeneration, in particular dry age-related macular degeneration. It has been demonstrated that the CETP inhibitor obicetrapib increases the plasma level of pre-beta-1 HDL, as well as total plasma lutein, zeaxanthin and tocopherol. More in particular, it has been found that the levels of these lipophilic anti-oxidants are also particularly elevated in pre-beta-1 HDL, which can pass the BrM and reach the retina with relative ease. These constitute particularly strong support for the treatment of AMD using a CETP inhibitor. Thus, broadly stated, the present invention concerns the use of CETP inhibitors in the treatment of age related macular degeneration.

The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor for use in the treatment of an individual suffering from or at increased risk of cardiovascular disease, in particular hyperlipidemia or mixed dyslipidemia. Another aspect of the invention relates to a pharmaceutical composition for use in the treatment of an individual suffering from or at increased risk of cardiovascular disease, wherein the composition comprises a therapeutically effective amount of the CETP inhibitor.

The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor:(Compound A) for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia. A further aspect of the present invention relates to a pharmaceutical composition for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, wherein the composition comprises a therapeutically effective amount of said Compound A CETP inhibitor.

The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor for use in the treatment of a subject suffering from or at an increased risk of cardiovascular disease, in particular hyperlipidemia or mixed dyslipidemia. Another aspect of the invention relates to a pharmaceutical composition for treating a subject suffering from or having an increased risk of cardiovascular disease, wherein the composition comprises a therapeutically effective amount of the CETP inhibitor.

The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor:(Compound A) for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia. A further aspect of the present invention relates to a pharmaceutical composition for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, wherein the composition comprises a therapeutically effective amount of said Compound A CETP inhibitor.