Patent classifications
C07B2200/07
LSD DERIVATIVES, SYNTHESIS & METHOD FOR TREATMENT OF DISEASES AND DISORDERS
LSD derivative compounds and polymorphs thereof, methods for their synthesis, compositions and treatment of diseases and disorders are described herein, the compounds having the structure of Formula I:
##STR00001##
including pharmaceutically acceptable salts, hydrates, solvates, tautomers, enantiomers, diastereomers, racemates, polymorphs or combinations thereof; wherein: R.sup.1 to R.sup.14 are each independently selected from H, or a substituted or unsubstituted hydrocarbon group and X is selected from a halo group.
Synthesis of eribulin mesylate
A preparation method of an intermediate compound of formula II ((1R,2S,3S,4S,5S,6R,11S,14S,17S,19R,21R,23S,25R,26R,27S,31R,34S)-25-[(2S)-2,3-dihydroxy]-2,5-dihydroxy-26-methoxy-19-methyl-13,20-dimethylene-24,35,36,37,38,39-hexaoxane[29.3.1.1.sup.3,6.1.sup.4,34.11.sup.1,14.1.sup.17,21.0.sup.23,27]nonatriacontan-8,29-dione) for eribulin mesylate is provided, including subjecting a compound of formula I to a reaction with an additive in the presence of tetra-n-butylammonium fluoride (TBAF). The additive is piperidine hydrochloride or pyridine hydrochloride, and a reaction formula is as follows: ##STR00001## The present invention aims to avoid the problem that a traditional synthetic route has a low yield.
CRYSTALLINE FORM OF CAPSID PROTEIN ASSEMBLY INHIBITOR CONTAINING N HETERO FIVE-MEMBERED RING, AND APPLICATION THEREOF
Disclosed by the present application is a crystalline form of a capsid protein assembly inhibitor containing an N hetero five-membered ring; specifically disclosed is the crystalline form of the compound of formula I; also comprised is an the application of said crystalline form in the preparation of a drug for preventing or treating diseases benefiting from the inhibition of capsid protein assembly.
##STR00001##
AFFINITY ILLUDOFULVENE CONJUGATES
In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker.
SARS-COV-2 MAIN PROTEASE INHIBITORS
The present disclosure relates to certain molecules, pharmaceutical compositions containing them, and methods of using them to treat viral infections.
20-HETE receptor (GPR75) antagonists and methods of use
The present invention concerns compounds and their use to treat cardiovascular disease, renal disease, thrombic disease, stroke, metabolic syndrome, cell proliferation, and ischemic cardiovascular disorders. Compounds of the present invention display significant potency as antagonists of 20-hydroxyeicosatetraenoic acid (20-HETE), and function as anti-hypertensive, anti-inflammatory, or anti-growth agents.
Synthesis of tipifarnib
Provided herein are methods of preparing a desired enantiomer 6-[amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl) methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone, otherwise known as tipifarnib.
Substituted piperidines as BTK inhibitors
Substituted piperidines as BTK inhibitors, a preparation method thereof and a pharmaceutical application thereof. The substituted piperidines is a compound represented by a general formula (I) or a stereoisomer or a pharmaceutically acceptable salt thereof, and the substituted piperidines is used to treat BTK-related diseases such as tumors or autoimmune system diseases.
B-L-K formula (I)
PROSTAGLANDIN EP4 RECEPTOR ANTAGONIST COMPOUNDS
The disclosures herein relate to novel compounds of formula (1): (1) and salts thereof, wherein A, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.10 and R.sup.11 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with EP.sub.4 receptors.
##STR00001##
PROCESS FOR SYNTHESIS OF PICOLINAMIDES
The present technology relates to processes, mixtures and intermediates useful for making picolinamide fungicides. The picolinamide compounds are prepared by processes that include coupling together a 4-methoxy-3-acyloxypicolinic acid with key 2-amino-L-alaninate esters derived from substituted 2-phenylethanols.