Patent classifications
C07J71/00
Therapeutically active estratrienthiazole derivatives as inhibitors of 17 B-hydroxysteroid dehydrogenase, type 1
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R6 are as defined in the claims. The invention further relates to their use as inhibitors of 17-HSD and in treatment or prevention of steroid hormone de-pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof. ##STR00001##
SUSTAINED-RELEASE PHARMACEUTICAL COMPOSITION FOR TREATMENT AND PREVENTION OF EYE DISEASE
The present invention relates to a terpenoid derivative that has the ability to activate the Keap1/Nrf2/ARE signaling pathway and is excellent in anti-inflammatory action and cytoprotective action, and a sustained-release pharmaceutical composition effective for the treatment and prevention of a posterior eye disease caused by oxidative stress, comprising the terpenoid derivative as an active ingredient. The present invention provides a local administration-type sustained-release pharmaceutical composition for the treatment or prevention of a posterior eye disease, comprising the terpenoid derivative of the present invention as an active ingredient, wherein the sustained-release pharmaceutical composition maintains a pharmacological action thereof for 1 week or longer by the sustained release of the terpenoid derivative under physiological conditions and has a base material administrable to the vitreous body and a form administrable to the vitreous body.
Method of making and using 7α, 11β-dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate
Methods of using 7,11-dimethyl-17-hydroxy-4-estren-3-one bucyclate (I) and 7,11-dimethyl-17-hydroxyestr-4-en-3-one 17-undecanoate (II) ##STR00001##
for various hormonal therapies, dosage forms comprising 7,11-dimethyl-17-hydroxy-4-estren-3-one bucyclate and 7,11-dimethyl-17-hydroxyestr-4-en-3-one 17-undecanoate, and processes for their preparation.
Withanolides useful for the treatment of neurodegenerative diseases
Provided herein are synthetic analogs of withanolide natural products of formula (I), wherein R1-R4 are as defined herein, and their pharmaceutical uses in treating neurodegenerative diseases.
Certain chemical entities, compositions, and methods
Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.
Substituted steroids for the treatment of cancer
A compound and pharmaceutically acceptable salts thereof for treating cancer, having a structure represented by the following formula (I) or formula (II): ##STR00001##
in which X and Y each individually represent: ##STR00002## R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 individually represents hydrogen atom, acyl having 20 or less carbon atoms, alkyl having 20 or less carbon atoms, alkanoyl having 20 or less carbon atoms, aroyl having 20 or less carbon atoms, aryl having 20 or less carbon atoms, aralkyl having 20 or less carbon atoms, sulfonyl having 20 or less carbon atoms, phosphonyl having 20 or less carbon atoms, or haloacyl having 20 or less carbon atoms.
Processes and Compositions Obtained from the Solanum Genus of Plants
Pure saponins and processes for making such saponins are described herein. In addition, cosmetic compositions, such as skin care compositions, comprising such saponins and methods for improving skin health and appearance with such skincare compositions are also described herein.
NOVEL PROCESS FOR PREPARATION OF CORTICOSTEROIDS
The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R.sub.1 and R.sub.2 is hydrogen or C.sub.1-C.sub.8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R.sub.3 is hydrogen or wherein R.sub.5 represents C.sub.1-C.sub.8 straight, branched alkyl chain or cycloalkyl; R.sub.4 is hydrogen or halogen; R.sub.6 is hydrogen or halogen;
##STR00001##
PREPARATIONS OF HYDROPHOBIC THERAPEUTIC AGENTS, METHODS OF MANUFACTURE AND USE THEREOF
The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).
17-beta-hydroxywithanolides and use thereof in treating cancer
Disclosed are compounds suitable for enhancing cancer treatment, for example, a compound of formula (I): (I) wherein R.sup.1 is as defined herein. Also disclosed is a method of enhancing the response of cancer cells in a mammal to treatment with an apoptosis inducing ligand, a method of inducing apoptosis in cancer cells in a mammal, and a method of treating prostate cancer in mammal in need thereof comprising administration of a compound described herein. ##STR00001##