Described herein are compounds that are semicarbazide-sensitive amine oxidase (SSAO) inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in treating or preventing a liver disease or condition.

The present disclosure provides a taxane compound and a preparation method and application thereof. The preparation method includes: protecting two hydroxyl groups in gemcitabine, conducting a condensation reaction between the protected gemcitabine and alkyl chloroformate, and removing of hydroxyl protecting groups to obtain an intermediate G1; protecting a first hydroxyl group of the intermediate G1, and then protecting the other one of the hydroxyl groups, and removing a protecting group of the first hydroxyl group to obtain an intermediate G2; reacting 7,10-di-troc-docetaxel with dianhydride to obtain an intermediate D1; conducting a condensation reaction between the intermediate D1 and the intermediate G2 to obtain an intermediate D2; and subjecting the intermediate D2 to hydroxyl deprotection to obtain a target product comprising the disclosed taxane compound.

The present disclosure provides a taxane compound and a preparation method and application thereof. The preparation method includes: protecting two hydroxyl groups in gemcitabine, conducting a condensation reaction between the protected gemcitabine and alkyl chloroformate, and removing of hydroxyl protecting groups to obtain an intermediate G1; protecting a first hydroxyl group of the intermediate G1, and then protecting the other one of the hydroxyl groups, and removing a protecting group of the first hydroxyl group to obtain an intermediate G2; reacting 7,10-di-troc-docetaxel with dianhydride to obtain an intermediate D1; conducting a condensation reaction between the intermediate D1 and the intermediate G2 to obtain an intermediate D2; and subjecting the intermediate D2 to hydroxyl deprotection to obtain a target product comprising the disclosed taxane compound.

The present invention provides a curable composition containing a compound represented by General Formula A and a compound represented by General Formula B.
ArL-Sp-Pol).sub.n(General Formula A) In General Formula A, Ar represents an n-valent group containing a nitrogen-containing fused aromatic ring as a partial structure; L represents a linking group such as O and C(O)O; Sp represents a single bond or a divalent linking group; Pol represents a hydrogen atom or a polymerizable group; n represents 1 or 2; and the compound represented by General Formula A has at least one polymerizable group. ##STR00001## In General Formula B, R, R, and R are each independently a hydrogen atom or a substituent; R and R or R and R may be bonded to each other to form a ring that may have a substituent; and W is a hydrogen atom or a substituent. Using the curable composition of the present invention, it is possible to form a cured product having a small Abbe number, a large partial dispersion ratio, and high light stability.

The present invention provides a curable composition containing a compound represented by General Formula A and a compound represented by General Formula B.
ArL-Sp-Pol).sub.n(General Formula A) In General Formula A, Ar represents an n-valent group containing a nitrogen-containing fused aromatic ring as a partial structure; L represents a linking group such as O and C(O)O; Sp represents a single bond or a divalent linking group; Pol represents a hydrogen atom or a polymerizable group; n represents 1 or 2; and the compound represented by General Formula A has at least one polymerizable group. ##STR00001## In General Formula B, R, R, and R are each independently a hydrogen atom or a substituent; R and R or R and R may be bonded to each other to form a ring that may have a substituent; and W is a hydrogen atom or a substituent. Using the curable composition of the present invention, it is possible to form a cured product having a small Abbe number, a large partial dispersion ratio, and high light stability.

The present invention relates to a method for the treatment of cancer in a cancer patient. In particular, the invention provides a method for the treatment comprising administering a taxane compound to a cancer patient, wherein the taxane compound is made by a process comprising treating a first compound represented by either Formula G or Formula M: ##STR00001##
with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

The present invention relates to a method for the treatment of cancer in a cancer patient. In particular, the invention provides a method for the treatment comprising administering a taxane compound to a cancer patient, wherein the taxane compound is made by a process comprising treating a first compound represented by either Formula G or Formula M: ##STR00001##
with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

The present invention is directed to processes from producing beta-lactone and beta-lactone derivatives using heterogenous catalysts. In preferred embodiments of the present invention, the processes comprise the steps: passing a feed stream comprising an epoxide reagent and a carbon monoxide reagent to a reaction zone; contacting the epoxide reagent and the carbon monoxide reagent with a heterogenous catalyst to produce a beta-lactone product in the reaction zone; and removing the beta-lactone product from the reaction zone. In preferred embodiments, the heterogenous catalyst comprises a solid support containing a cationic Lewis acid functional group and a metal carbonyl compound comprising at least one of anionic metal carbonyl compound or a neutral metal carbonyl compound. In certain preferred embodiments, the epoxide reagent and carbon monoxide reagent have a biobased content.

The present invention is directed to processes from producing beta-lactone and beta-lactone derivatives using heterogenous catalysts. In preferred embodiments of the present invention, the processes comprise the steps: passing a feed stream comprising an epoxide reagent and a carbon monoxide reagent to a reaction zone; contacting the epoxide reagent and the carbon monoxide reagent with a heterogenous catalyst to produce a beta-lactone product in the reaction zone; and removing the beta-lactone product from the reaction zone. In preferred embodiments, the heterogenous catalyst comprises a solid support containing a cationic Lewis acid functional group and a metal carbonyl compound comprising at least one of anionic metal carbonyl compound or a neutral metal carbonyl compound. In certain preferred embodiments, the epoxide reagent and carbon monoxide reagent have a biobased content.

The invention includes taxoid compounds represented by the formula: ##STR00001##
wherein: R.sup.1 represents a methyl group or a fluorine; R.sup.2 represents an alkyl or alkenyl group having one to six carbon atoms; or a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; R.sup.3 represents an alkyl, alkenyl, dialkylamino, alkylamino, or alkoxy group having one to six carbon atoms; a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; an aryl group having six to eighteen ring carbon atoms; or a heteroaryl group having three to seventeen ring carbon atoms; R.sup.4 represents hydrogen or a methyl group; and X represents hydrogen or fluorine.