C07C2602/24

New Pleuromutilin Antibiotic Compounds, Compositions and Methods of Use and Synthesis
20190352262 · 2019-11-21 ·

The present invention is directed to novel pleuroniutilin antibiotic compounds, intermediates which are useful for making these novel amibioiic compounds and related methods and pharmaceutical compositions for treating pathogens, especially bacterial infections, including gram negative bacteria and synthesizing these compounds.

2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs

This invention discloses 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-1-hydroxyvitamin D.sub.3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows low activity in vivo on bone calcium mobilization, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.

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.

COMPOSITIONS AND METHODS OF TREATING CONDITIONS
20240131036 · 2024-04-25 ·

The present disclosure provides for pharmaceutical composition and methods of treating a condition using the pharmaceutical composition. The condition to be treated in a subject in need of treatment can include an infection or non-viral hyper-inflammation/immune hyperactivation condition. The infection can be a coronavirus infection, HIV infection, influenza infection, or the like, where a direct or indirect result of the infection can be respiratory distress, oxidative stress, and the like that can lead to acute respiratory distress syndrome (ARDS) and/or organ dysfunction or failure.

INDENE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC APPLICATIONS
20240116845 · 2024-04-11 ·

Provided herein are an indene compound, e.g., a compound of Formula (I), and a pharmaceutical composition thereof. Also provided herein is a method of their use for treating, preventing, or ameliorating one or more symptoms of a fibrotic disease.

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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.

METHODS FOR IMPROVED PRODUCTION OF VITAMINS D2 AND D3
20190322621 · 2019-10-24 · ·

It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.

Circular economy methods of preparing unsaturated compounds

Methods of preparing unsaturated compounds or analogs through dehydrogenation of corresponding saturated compounds and/or hydrogenation of aromatic compounds are disclosed.

SITE-SPECIFIC CHEMOENZYMATIC PROTEIN MODIFICATIONS

The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.

Compositions relating to vitamin D

The present invention discloses compositions that comprise compounds relating to vitamin D. These compounds are useful for assays in the determination and distinguishing of certain 3-epimeric 25 hydroxyvitamin D and non-epimeric 25 hydroxyvitamin D. The compositions of the present invention may be used for example as immunogens used to develop antibodies to certain vitamin D compounds or conjugates used in assays for certain vitamin D compounds or used as a solid phase reagent in assays. The composition comprises a compound of one or more of the generic formula (R.sup.1).sub.p-(L).sub.q-Z.