C07C233/88

COMPOUNDS FOR TARGETED PROTEIN DEGRADATION
20240174708 · 2024-05-30 ·

Provided are compounds, including compositions comprising the same, which function to recruit various target proteins (e.g., client proteins of 14-3-3 proteins) to an E3 ubiquitin ligase enzyme for ubiquitination and subsequent degradation, and methods of using the same.

COMPOUNDS FOR TARGETED PROTEIN DEGRADATION
20240174708 · 2024-05-30 ·

Provided are compounds, including compositions comprising the same, which function to recruit various target proteins (e.g., client proteins of 14-3-3 proteins) to an E3 ubiquitin ligase enzyme for ubiquitination and subsequent degradation, and methods of using the same.

Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.

Compound having BLT inhibitory activity and composition, for preventing or treating inflammatory diseases, comprising same as active ingredient

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.

Compound having BLT inhibitory activity and composition, for preventing or treating inflammatory diseases, comprising same as active ingredient

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.

Method for preparing creatine fatty esters, creatine fatty esters thus prepared and uses thereof

The present invention concerns a method for preparing a creatine fatty ester or derivative thereof comprising at least one step consisting in reacting a diprotected creatinine with a molecule bearing at least one alcohol functional group and of formula ROH in which R represents a hydrocarbon radical containing at least 4 carbon atoms. The present invention also concerns particular creatine fatty esters or derivative thereof and medical uses thereof.

SYNTHESIS OF SUBSTITUTED AMIDOBENZOATE COMPOUNDS, THE COMPOUNDS OBTAINED AND THE USE THEREOF AS PHTHALATE FREE INTERNAL ELECTRON DONOR FOR POLYMERIZATION OF OLEFINS

The present invention relates to a compound according to Formula (I) wherein R.sup.1 is a hydrocarbyl group selected from the group consisting of alkyl, alkenyl, aryl, aralkyl, and alkylaryl groups, and one or more combinations thereof; wherein R.sup.2 is a hydrogen atom, an aryl group or an alkyl group; and wherein R.sup.3, R.sup.4, R.sup.5 and R.sup.6, are the same or different and are each independently a hydrogen atom, a halogen atom, a cyano group, an amino group, a hydrocarbyl group selected from the group consisting of alkyl, alkenyl, aryl, aralkyl, and alkylaryl groups or an alkoxy group, and one or more combinations thereof as internal electron donor and to a process for the synthesis of a compound according to Formula (I), wherein R.sup.1 is a hydrocarbyl group selected from the group consisting of alkyl, alkenyl, aryl, aralkyl, alkoxycarbonyl and alkylaryl groups, and one or more combinations thereof; wherein R.sup.2 is a hydrogen atom or an alkyl group; wherein R.sup.3, R.sup.4, R.sup.5 and R.sup.6, are the same or different and are each independently selected from a group consisting of a hydrogen atom; a hydrocarbyl, preferably, said process comprising the step of reacting a compound according to Formula (II) [R.sup.1C(O)Cl] with a compound according to Formula (III) to obtain the compound according to Formula (I) and to the use of these compounds as internal donor in Ziegler-Natta catalysis of olefins.

##STR00001##