Patent classifications
C07D313/00
MACROLIDE BREFELDIN A ESTER DERIVATIVES AND USE THEREOF
The present disclosure relates to the field of medicinal chemistry, and specifically to the use in the inhibition of tumor proliferation activity of ester derivatives of brefeldin A represented by Formula (I). The new compounds provided herein are prominent in the prevention or treatment of hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, gastric cancer, lung cancer, Bart's esophageal cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymphoma, kidney cancer, brain cancer, nerve cancer, nasopharyngeal cancer, oral cancer and colorectal cancer, and have the potential to be developed as novel antitumor agents.
MACROLIDE BREFELDIN A ESTER DERIVATIVES AND USE THEREOF
The present disclosure relates to the field of medicinal chemistry, and specifically to the use in the inhibition of tumor proliferation activity of ester derivatives of brefeldin A represented by Formula (I). The new compounds provided herein are prominent in the prevention or treatment of hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, gastric cancer, lung cancer, Bart's esophageal cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymphoma, kidney cancer, brain cancer, nerve cancer, nasopharyngeal cancer, oral cancer and colorectal cancer, and have the potential to be developed as novel antitumor agents.
NOVEL MOLECULE WITH ANTI-CANCER ACTIVITY
The present invention provides a new compound of formula (II), extracted from Chaetomorpha Cannabina seaweed. (II) The methods for extraction from the seaweed, the fractionation and isolation of the compound, the determination of the stereochemistry and its use for inhibiting the growth of cancer cells are provided.
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NOVEL MOLECULE WITH ANTI-CANCER ACTIVITY
The present invention provides a new compound of formula (II), extracted from Chaetomorpha Cannabina seaweed. (II) The methods for extraction from the seaweed, the fractionation and isolation of the compound, the determination of the stereochemistry and its use for inhibiting the growth of cancer cells are provided.
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POLYCYCLIC COMPOUNDS AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
The present invention relates to soluble epoxide hydrolase (sEH) inhibitors of formula (I) to processes for their obtention and to their therapeutic indications.
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POLYCYCLIC COMPOUNDS AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
The present invention relates to soluble epoxide hydrolase (sEH) inhibitors of formula (I) to processes for their obtention and to their therapeutic indications.
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SPLICING MODULATOR ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.
SPLICING MODULATOR ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.
Sulfuric acid ester or salt thereof, and surfactant
A sulfuric acid ester containing a plurality of carbonyl groups or a salt thereof, and a surfactant. The sulfuric acid ester is a compound represented by the following formula:
R.sup.1—C(═O)—R.sup.2—C(═O)—R.sup.3—OSO.sub.3X wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein; X is H, a metal atom, NR.sup.4.sub.4, imidazolium optionally containing a substituent, pyridinium optionally containing a substituent, or phosphonium optionally containing a substituent, where R.sup.4s are each H or an organic group and are the same as or different from each other; and any two of R.sup.1, R.sup.2, and R.sup.3 optionally bind to each other to form a ring.
CERTAIN ARYL PLADIENOLIDE COMPOUNDS AND METHODS OF USE
The present disclosure provides pladienolide compounds, pharmaceutical compositions containing such compounds, and pladienolide compounds for use in methods of medical treatment. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are pladienolide compounds for use in methods of treating cancers by administering at least one pladienolide compound disclosed herein and at least one additional therapy.