C07C2602/24

TRICYCLODECANE DIMETHANOL COMPOSITION AND PREPARATION METHOD OF THE SAME
20230192577 · 2023-06-22 ·

Provided are a tricyclodecane dimethanol composition which may be suitably used in preparing a polyester resin exhibiting excellent solvent resistance and chemical resistance when forming a coating film and having excellent solubility in organic solvents or water, and a preparation method thereof.

(22E)-2-methylene-26,27-cyclo-22-dehydro-1α-hydroxy-19-norvitamin D3 derivatives

Cyclopropane-containing vitamin D analogs of formulas I and IV are provided. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions. ##STR00001##

1-deoxy analogs of 1,25-dihydroxyvitamin D3 compounds

This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.

SHIP1 MODULATORS AND METHODS RELATED THERETO

Compounds of formula (II):

##STR00001##

wherein

##STR00002##

R.sup.1, R.sup.2, R.sup.5 and R.sup.13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

Fungicidal N-bicycloalkyl and N-tricycloalkyl pyrazole-4-(thio)carboxamide derivatives

The present invention relates to fungicidal N-bicycloalkyl and N-tricycloalkyl pyrazole-4-(thio)carboxamide derivatives of formula (I), wherein T represents O or S; n represents 0 or 1; and B represents where the bond marked by * is attached to the (CZ2Z3)n-N amide moiety, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. ##STR00001##

Anthracene derivatives, luminescent materials and organic electroluminescent devices

Anthracene derivatives each having a structure including an anthracene skeleton, a phenanthrene skeleton selected from among various phenanthrene skeletons different in bonding site which is bonded to the 9-position of the anthracene skeleton and a group selected from among various aryl groups and so on which is bonded to the 10-position of the anthracene skeleton. Organic EL devices made by using the derivatives exhibit high light emission efficiency and a long life.

IMPROVED, COST EFFECTIVE PROCESS FOR SYNTHESIS OF VITAMIN D3 AND ITS ANALOGUE CALCIFEDIOL FROM ERGOSTEROL

Disclosed herein is an improved and efficient process for synthesis of vitamin D3 and its analogue Calcifediol from Ergosterol. Particularly, the present invention discloses the synthesis of key intermediate 3β-tert-Butyldimethylsilyloxy-22-hydroxy-23,24-bisnorchola-5,7-diene (5), and novel intermediate β-tert-Butyldimethylsilyloxy-22-iodo-23,24-bisnorchola-5,7-diene (9) by a simple and cost effective process. The industrially viable processes for preparation of said intermediate(s) results in providing provitamins with various side chains and the desired products in high yield.

METHODS OF MANUFACTURING TREPROSTINIL AND TREPROSTINIL DERIVATIVE PRODRUGS

Methods for making prodrugs of trepreostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing prostacyclin compounds comprising treprostinil covalently linked to a linear C.sub.5-C.sub.18 alkyl, branched C.sub.5-C.sub.18 alkyl, linear C.sub.2-C.sub.18 alkenyl, branched C.sub.3-C.sub.18 alkenyl, aryl, aryl-C.sub.1-C.sub.18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.

SHIP1 MODULATORS AND METHODS RELATED THERETO

Compounds of formula (I):

##STR00001##

where R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and R.sup.7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

25-OH vitamin D derivatives for determining vitamin D metabolites
11199553 · 2021-12-14 · ·

The present invention relates to new vitamin D compounds which are bonded to a labelling group at the C3 stereocentre by means of a linker. The present invention further relates to a method for producing these vitamin D compounds and to the use of an intermediate for producing these compounds. The present invention also relates to a method for quantitatively determining vitamin D using a vitamin D compound according to the invention as a tracer. Furthermore, the present invention relates to a reagent for determining vitamin D, containing a compound according to the invention, and to the use thereof for determining vitamin D.