Patent classifications
C07J41/0044
THERAPEUTICALLY ACTIVE STEROIDAL DERIVATIVES
The invention relates to compounds of formula (II),
##STR00001##
and pharmaceutically acceptable salts thereof,
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 pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Described herein are neuroactive steroids of the Formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof; wherein , A, R.sup.1, R.sup.2, and R.sup.3 are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use, e.g., for treating a subject suffering from a disease or disorder described herein.
PRODRUG AND PROFLUORESCENT COMPOUNDS FOR SELECTIVE MITOCHONDRIAL IMAGING AND THERAPEUTIC TARGETING
The present invention relates to the use of prodrugs susceptible to nitroreductase (NTR) activation. In particular, provided herein are mitochondria-targeting prodrug compounds and probes, including profluorescent near-infrared (NIR) probes and non-fluorescent prodrugs, as well as to methods of using said prodrug compounds and probes for imaging mitochondria and for mitochondria-specific delivery of therapeutic agents.
6-substituted estradiol derivatives and methods of use
Disclosed are compounds of the formula: ##STR00001##
and the respective enantiomers, stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of such compounds; which can be useful in the treatment of various types of cancer.
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.
Tripartite Androgen Receptor Eliminators, Methods and Uses Thereof
The present specification discloses tripartite androgen receptor eliminators (AREs), pharmaceutical compositions and medicaments comprising such AREs, methods and uses for such AREs and compositions and medicaments, and methods and uses for AREs and compositions and medicaments for treating an androgen receptor signaling-mediated condition, disease or disorder.
Longer-acting progestin prodrug contraceptives
Described herein are progestin compounds that have extended release rates and that can be used without an estrogen to produce a contraceptive state.
Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof
The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. ##STR00001##
Prodrug and profluorescent compounds for selective mitochondrial imaging and therapeutic targeting
The present invention relates to the use of prodrugs susceptible to nitroreductase (NTR) activation. In particular, provided herein are mitochondria-targeting prodrug compounds and probes, including profluore scent near-infrared (NIR) probes and non-fluorescent prodrugs, as well as to methods of using said prodrug compounds and probes for imaging mitochondria and for mitochondria-specific delivery of therapeutic agents.
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Provided herein is a compound of Formula (I)
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein ring D and the substituents are defined herein. Also provided are pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of using the compound of Formula (I) in the treatment of CNS-related disorders.