C07D305/14

PROCESSES FOR PRODUCING BETA-LACTONE AND BETA-LACTONE DERIVATIVES WITH HETEROGENOUS CATALYSTS
20190047972 · 2019-02-14 · ·

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.

PROCESSES FOR PRODUCING BETA-LACTONE AND BETA-LACTONE DERIVATIVES WITH HETEROGENOUS CATALYSTS
20190047972 · 2019-02-14 · ·

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.

MULTI-ARM POLYMERIC PRODRUG CONJUGATES OF TAXANE-BASED COMPOUNDS
20190008822 · 2019-01-10 ·

Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of taxane-based compounds and/or fluorinated forms thereof. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the taxane-based compound is achieved.

MULTI-ARM POLYMERIC PRODRUG CONJUGATES OF TAXANE-BASED COMPOUNDS
20190008822 · 2019-01-10 ·

Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of taxane-based compounds and/or fluorinated forms thereof. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the taxane-based compound is achieved.

Acid-labile lipophilic prodrugs of cancer chemotherapeutic agents

The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.

Acid-labile lipophilic prodrugs of cancer chemotherapeutic agents

The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.

Crystalline forms of dimethoxy docetaxel and methods for preparing the same

The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2-benzoyloxy-5,20-epoxy-1-hydroxy-7, 10-dimethoxy-9-oxo-tax-11-ene-13-yle, and to the preparation thereof.

Crystalline forms of dimethoxy docetaxel and methods for preparing the same

The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2-benzoyloxy-5,20-epoxy-1-hydroxy-7, 10-dimethoxy-9-oxo-tax-11-ene-13-yle, and to the preparation thereof.

PEG derivative

Provided is a new therapeutic agent for a malignant tumor, which is highly safe, sustains an antitumor effect, and can improve the means for administration and the number of times of administration. Disclosed is a compound of Formula (1), or a salt thereof:
C[CH.sub.2O(CH.sub.2CH.sub.2O).sub.mCH.sub.2COR.sup.1R.sup.2].sub.4(1) wherein R.sup.1 represents a single bond, N(R.sup.3)(CH.sub.2).sub.n1CO, or N(R.sup.4)(CH.sub.2).sub.n2N (R.sup.5)CO(CH.sub.2).sub.n3CO; R.sup.2 represents a group of Formula (a), (b), (c), (d), (e), or (f): ##STR00001## ##STR00002## m represents a number of from 10 to 1,000; and an arrow represents a bonding site.

WATER-SOLUBLE DOCETAXEL ANTICANCER DRUG COMPOUND AND PREPARATION METHOD AND USE THEREOF
20180303949 · 2018-10-25 ·

The present invention discloses a water-soluble docetaxel anticancer drug compound having the structure of Formula I below:

##STR00001## in which R=CH.sub.3, CH.sub.2CH.sub.3, CH.sub.2CH.sub.2CH.sub.3, or CH.sub.2CH.sub.2CH.sub.2CH.sub.3; and n=5-500.

The active moiety docetaxel in the anticancer drug compound is covalently conjugated to a polyethylene glycol monoalkyl ether through a linker diglycoloyl (carbonyl methoxyacetyl) to form the water-soluble docetaxel anticancer drug compound.

The present invention also relates to a preparation method of the drug compound and use thereof.