C07F9/65586

Synthesis of Phosphoramidates

A process for the preparation of a compound of formula (I) including all isomers, stereoisomers, enantiomers and diastereomers thereof (I), and salts thereof; the process comprising providing a mixture comprising a compound of formula (II) and a compound of formula (III) subjecting the mixture provided in a) to reaction conditions in the presence of one or more Lewis acids to the mixture provided in a), obtaining a mixture comprising the compound of formula (I).

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A PROCESS FOR THE PREPARATION OF NUCLEOSIDE PHOSPHORAMIDATE

The present invention pertains to process for preparing nucleoside phosphoramidate and its intermediate. The present invention provides novel intermediate, its process for preparation and its use for the preparation of Sofosbuvir.

Polymeric tandem dyes with linker groups
11453783 · 2022-09-27 · ·

Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I): ##STR00001##
or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1, L.sup.2, L.sup.3, L.sup.4, M.sup.1, M.sup.2, m and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.

DIOXOLANE ANALOGUES OF URIDINE FOR THE TREATMENT OF CANCER
20170267705 · 2017-09-21 ·

The invention provides compounds of the formula:

##STR00001## R.sup.1 is OR.sup.11, or NR.sup.5R.sup.5′; R.sup.2 is H or F; R.sup.5 is H, OH, C.sub.1-C.sub.6 alkyl, OH, C(═O)R.sup.6, O(C═O)R.sup.6 or O(C═O)OR.sup.6; R.sup.5′ is H or C.sub.1-C.sub.6 alkyl; R.sup.6 is C.sub.1-C.sub.6 alkyl or C.sub.3-C.sub.7 cycloalkyl; R.sup.13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R.sup.22; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.

Heterocyclic compound and organic light-emitting device including the same

A heterocyclic compound and an organic light-emitting device including the same are provided. The organic light-emitting device includes: a first electrode; a second electrode facing the first electrode; and an organic layer disposed between the first electrode and the second electrode, where the organic layer may include an emission layer and at least one of the heterocyclic compound described above.

Cyclic phosphonate substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. ##STR00001##

Alvocidib prodrugs having increased bioavailability

Compounds having the following structure (I): ##STR00001##
or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R.sup.1, R.sup.2 or R.sup.3 is —P(═O)(OH).sub.2, and the other two of R.sup.1, R.sup.2 and R.sup.3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.

FUNCTIONALIZING NANOFIBRES
20170252460 · 2017-09-07 ·

Methods for functionalizing the surface of nanofiber substrates, including electrospun fibres and non-woven or woven mats of fibres are described. Functionalised nanofiber substrates presenting biologically active moieties such as biotin and saccharides are described.

CARBORANE COMPOUNDS, CARBORANE ANALOGS, AND METHODS OF USE THEREOF

Disclosed are method of treating fibrotic conditions using carboranes and carborane analogs. Also disclosed herein are compounds comprising dicarba-closo-dodecaborane or a dicarba-closo-dodecaborane analog. The compounds can be, for example, estrogen receptor beta (ERβ) agonists. In some examples, the compounds can be selective ERβ agonists. Also provided herein are methods of treating, preventing, or ameliorating cancer in a subject, suppressing tumor growth in a subject, treating an inflammatory disease in a subject, treating a neurodegenerative disease in a subject, treating a psychotropic disorder in a subject, or a combination thereof, by administering to a subject a therapeutically effective amount of one or more of the compounds or compositions described herein, or a pharmaceutically acceptable salt thereof.

METABOLICALLY STABLE PRODRUGS

Provided are prodrugs of various therapeutic agents that provide enhanced bioavailability of the therapeutic agent, and methods of treatment conditions in a subject by administration of the one or prodrugs. As provided herein a prodrug includes a therapeutic agent covalently attached to a cap, the cap having a structure according to formula (I) where: R.sup.1 is a branched or linear substituted or unsubstituted C2-C6 alkyl, alkenyl, or alkynl; X is —S(0).sub.2-; R.sup.2 is a branched or linear substituted or unsubstituted C4-C20 alkyl, alkenyl, or alkynyl; and R.sup.3 is —H, C3-C5 cycloalkyl, C3-C5 cycloheteroalkyl, —C(CH.sub.3).sub.3, —CF.sub.3, —C(CF.sub.3).sub.3, or a substituted or unsubstituted phenyl.

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