Provided is a urination disorder-improving agent useful for treating or improving (or alleviating) a urination disorder regardless of the degree or presence of prostatomegaly. The urination disorder-improving agent contains a 2-oxapregnane compound represented by the following formula (1) as an active ingredient. (In the formula, R.sub.1 to R.sub.3 represent an alkyl group such as methyl group, R.sub.4 represents an alkylcarbonyl group such as acetyl group, X represents a halogen atom such as a chlorine atom, Y represents a hydroxyl group or oxo group bonded to the 11-position, 15-position, or 16-position of the steroid skeleton.)

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N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.

The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-alkyl- or 2-aromatic-substituted tanshinone I derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments. When Z=R, said derivative is 2-alkyl-substituted tanshinone I; when Z=Ar, said derivative is 2-aryl-substituted tanshinone I; when Z=Het, said derivative is 2-heteroaryl- or 2-heterocyclyl-substituted tanshinone I. ##STR00001##

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

Tripyolide-nucleic acid aptamer derivatives, a preparation method and use thereof are shown. The structure of the triptolide-nucleic acid aptamer derivatives is as shown by formula I, wherein the definitions of R.sub.1-R.sub.7, G, A, B, M, Z and X are described. The present invention uses a nucleic acid aptamer and triptolide or modified compounds thereof as the starting materials, and introduces a linking group A at the C-14 hydroxyl group, epoxy groups and five-membered ring lactones in triptolide, then connects it to a nucleic acid aptamer B, and obtains the triptolide-nucleic acid aptamer derivatives. The triptolide-nucleic acid aptamer derivatives of the present invention have the characteristics of good targeting, a high anti-cancer activity, low toxicity and side effects, good water solubility and high bioavailability, and the preparation method of the present invention is scientific and reasonable and has a controllable quality and good repeatability, and is thereby suitable for production.

A method for producing telomerase activators which provide to obtain new/novel molecules (metabolites) from saponin group compounds by using biotransformation with endophytic fungi and telomerase activators obtained by this method. Included is the elucidation of chemical structures and investigation of the effects of telomerase enzyme activation in cells. These molecules have the potential to be used in diseases and/or conditions that can be treated/ameliorated by telomerase activation and associated with telomere shortening (For example; HIV, degenerative diseases, acute and chronic wound healing, ex vivo cell therapies and stem cell proliferation due to increment in vitro and ex-vivo replicative capacity of cells).

The invention relates to the field of medicine and to the chemical and pharmacological industry, and concerns medicaments for the treatment of breast cancer. In particular the invention relates to a use of 3-O-sulfamoyloxy-7β-methyl-D-homo-6-oxaestra-1,3,5 (10),8(9)-tetraen-17a-one as an anti-cancer agent in monotherapy and adjuvant therapy of breast cancer, including the triple negative breast cancer.

Provided herein is a compound of Formula (I-I), or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I), and methods of using the compounds, e.g. in the treatment of CNS-related disorders. ##STR00001##

This disclosure provides triptolide-conjugates, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, as well methods of using such compounds in the treatment of conditions/diseases, such as those relating to cancer, immunomodulation and/or inflammation.

The present disclosure provides for a synthetic strategy to incorporate a C12α-hydroxy group from the methylene (—CH2-) in a steroid backbone, combining synthetic chemistry and enzymology techniques to develop a selective inhibitor for cytochrome P450 8B1, and developing a selective P450 8B1 inhibitor, which can be used as a tool to study P450 8B1 and treat health issues.