Patent classifications
C07J41/0016
THERAPEUTICALLY ACTIVE STEROIDAL DERIVATIVES
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof
##STR00001##
wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD1 and in treatment or prevention of steroid hormone dependent 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.
CHEMICAL COMPOUNDS AND USE THEREOF FOR IMPROVING MUSCULAR QUALITY
Chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, a method of improving muscular quality in sarcopenic mammals and treating and/or preventing sarcopenia using the chemical compounds and, in particular, sarcopenic obesity and the associated complications and/or pathologies thereof, such as loss of strength, muscle mass, performance and of physical and movement capacity. Also, a method of improving muscle quality in obese mammals and treating and/or preventing of obesity and associated complications and/or pathologies, advantageously type 2 diabetes and metabolic syndrome, using the chemical compounds.
Polyethylene Glycol-Conjugated Glucocorticoid Prodrugs and Compositions and Methods Thereof
Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for treating inflammatory and autoimmune diseases, including but not limited to lupus, are disclosed.
CATIONIC STEROID ANTIMICROBIAL DIAGNOSTIC, DETECTION, SCREENING AND IMAGING METHODS
The invention relates to diagnostic, detection, screening and imaging methods. In various embodiments, methods of diagnosis, detection, screening and imaging include administering a cationic steroid antimicrobial or CSA to a subject having or at risk of having an infection or a hyperproliferative disorder (e.g., a tumor, cancer or neoplasia) in an amount effective to diagnose or detect the infection or the hyperproliferative disorder (e.g., a tumor, cancer or neoplasia) in the subject. In a particular aspect, a detectable CSA, namely CSA-13 labeled with .sup.99mTc is used to detect the presence of an infection.
THERAPEUTICALLY ACTIVE STEROIDAL DERIVATIVES
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof
##STR00001##
wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD1 and in treatment or prevention of steroid hormone dependent 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.
Cationic steroid antimicrobial diagnostic, detection, screening and imaging methods
The invention relates to diagnostic, detection, screening and imaging methods. In various embodiments, methods of diagnosis, detection, screening and imaging include administering a cationic steroid antimicrobial or CSA to a subject having or at risk of having an infection or a hyperproliferative disorder (e.g., a tumor, cancer or neoplasia) in an amount effective to diagnose or detect the infection or the hyperproliferative disorder (e.g., a tumor, cancer or neoplasia) in the subject. In a particular aspect, a detectable CSA, namely CSA-13 labeled with .sup.99mTc is used to detect the presence of an infection.
Chemical compounds and use thereof for improving muscular quality
Chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, a method of improving muscular quality in sarcopenic mammals and treating and/or preventing sarcopenia using the chemical compounds and, in particular, sarcopenic obesity and the associated complications and/or pathologies thereof, such as loss of strength, muscle mass, performance and of physical and movement capacity. Also, a method of improving muscle quality in obese mammals and treating and/or preventing of obesity and associated complications and/or pathologies, advantageously type 2 diabetes and metabolic syndrome, using the chemical compounds.
3-ALPHA SUBSTITUTED 3-BETA-HYDROXY-17-OXIMATED ANDROSTANE COMPOUND FOR MODULATION OF THE ALPHA-3 SUBTYPE OF THE GABAA RECEPTOR
The present disclosure concerns the novel compound 3.alpha.-ethynyl-3.beta.-hydroxy-5.alpha.-androstan-17-methoxime, the medical use thereof and in particular use in the treatment of diseases and disorders associated with an a3 subtype of the GABAA receptor, for example treatment of obesity, hyperphagia disorder, Prader-Willi's syndrome, polycystic ovarian syndrome, and/or diabetes. Said disclosure is also concerned with reducing and/or preventing overweight. Additionally, related pharmaceutical and cosmetic compositions are disclosed.
Progesterone Phosphate Analogs and Uses Related Thereto
This disclosure relates to progesterone phophate derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation such as those resulting from traumatic brain injury or stroke.
GPX4 Inhibitors and Senolytic Compounds and Uses Thereof
The present invention relates to compounds that kill senescent cells i.e., senolytic compounds and compounds which inhibit GPX4. The present invention also provides compounds and methods for treating senescence-associated diseases or disorders, and compounds and methods for treating diseases or disorders impacted by GPX4.