A01N43/04

Cytotoxic-drug delivering molecules targeting HIV (CDM-Hs), cytotoxic activity against the human immunodeficiency virus and methods of use
09745334 · 2017-08-29 · ·

The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as CDM-Hs, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by introducing cytotoxic moieties to gp120-expressing cells, thereby causing cell death and preventing cell infection and spread of HIV. It is shown that CDM-Hs bind to gp120 and gp-120 expressing cells competitively with CD4, and these compounds cause cell death of HIV-infected cells, thereby decreasing viral infectivity. Compounds and methods are described herein.

Colloid bonded medicinal compounds
09737613 · 2017-08-22 · ·

The invention relates to colloids bound medicinal compounds or fluorescent markers, to a process for the preparation thereof, and to a pharmaceutical formulation containing such compounds.

Cyclic dinucleotides as anticancer agents

The present invention is directed to compounds of the formula ##STR00001##
wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Embolizing sclerosing hydrogel

A sclerosing embolizing hydrogel comprising from about 0.1% by weight to about 4.0% by weight of chitosan; from about 0.01M to about 1M of hydrochloric acid; from 0% by volume to about 40% by volume of iopamidol; from 0.5% by weight to about 25% by weight of β-glycerophosphate disodium salt; and from about 0.05% by weight to about 4% by weight of sodium tetradecyl sulphate. Also a kit for synthesizing the hydrogel and a method using the hydrogel to treat a vascular defect in a subject.

2′-alkynyl substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2′-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2′-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. ##STR00001##

Nucleoside and nucleotide derivatives

The present invention discloses compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR00001##
which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral/anti-proliferative compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral infection in a subject in need of such therapy with said compounds.

5-fluorouracil compounds
11427550 · 2022-08-30 · ·

The compounds are of the class of 5-fluorouracil derived acetal and hemiaminal ether compounds, useful in treating liver diseases and various types of cancer. The following formulas are representative of the class of compounds provided herein: ##STR00001##

Compositions and methods for activating stimulator of interferon gene-dependent signalling

The present invention provides highly active cyclic-di-nucleotide (CDN) immune stimulators that activate DCs via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides induce STING-dependent type I interferon production, wherein the cyclic purine dinucleotides present in the composition are substantially pure 2′,5′,2′,5′ and 2′,5′,3′,5′ CDNs, and preferably Rp,Rp stereoisomers thereof.

Antibacterial agents including histidine kinase inhibitors

An example composition includes a therapeutically effective amount of a histidine kinase inhibitor. The histidine kinase inhibitor includes at least one of a 6-benzo[d]thiazol-2-amine derivative, a purine derivative, an adenine derivative, an adenine-sulfonyl fluoride derivative, a riluzole analog, a riluzole-sulfonyl fluoride derivative, a 6-benzo[d]thiazol-2-amine-sulfonyl fluoride derivative, a 6,6′-oxybis(benzo[d]thiazol-2-amine) derivative, or a 6,6′-oxybis(benzo[d]thiazol-2-amine)-sulfonyl fluoride derivative. An example technique for treating a bacterial infection includes administering a composition comprising a histidine kinase inhibitor to a patient.

Anhydrous polymorphs of [(2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-YL)-3,4-dihydroxytetrahydrofuran-2-YL)] methyl nitrate and processes of preparation thereof

The present invention provides novel anhydrous polymorph forms of [(2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)]methyl nitrate (compound A), a selective adenosine A.sub.1 receptor agonist with a number of therapeutic uses including the treatment of elevated intra-ocular pressure. Also provided are methods for the preparation of the anhydrous polymorphic forms of compound A, pharmaceutical compositions and methods of treatment. ##STR00001##