Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.19, R.sup.5, R.sup.3a, R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.18, R.sup.D, and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of C(0)N(R.sup.55a)(R.sup.55b), N(R.sup.55a)(R.sup.55b), N(R.sup.55b)C(O)(R.sup.55a), and R.sup.55C wherein R.sup.55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders. ##STR00001##

Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.19, R.sup.5, R.sup.3a, R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.18, R.sup.D, and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of C(0)N(R.sup.55a)(R.sup.55b), N(R.sup.55a)(R.sup.55b), N(R.sup.55b)C(O)(R.sup.55a), and R.sup.55C wherein R.sup.55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders. ##STR00001##

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.

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.

Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.19, R.sup.5, R.sup.3a, R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.18, R.sup.D, and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of C(O)N(R.sup.55a)(R.sup.55b), N(R.sup.55a)(R.sup.55b), N(R.sup.55b)C(O)(R.sup.55a), and R.sup.55C wherein R.sup.55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders. ##STR00001##

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.

Described herein are progestin compounds that have extended release rates and that can be used without an estrogen to produce a contraceptive state.

Disclosed are compounds of the formula: ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, C.sub.1-C.sub.6 alkyl, halo, a sulfate, a glucuronide, OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, N(CH.sub.2).sub.n; a phosphate group, and a phosphinate group; R.sub.9 is hydrogen, halogen or alkyl; R.sub.11 is selected from the group consisting of H, C.sub.1-C.sub.6 alkyl, halogen, a sulfate, a glucoronide, SO.sub.2NH.sub.2, COOH, CN, CH.sub.2CN, NHCN, CHO, CHOCH.sub.3, COO salt, OSO.sub.2alkyl, NH.sub.2, and NHCO(CH.sub.2).sub.n; R.sub.12 is selected from the group consisting of H, a C.sub.1-C.sub.6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C.sub.1-C.sub.12 alkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, halogen, a glucoronide, NH.sub.2, SO.sub.2NH.sub.2, COOH, CN, CH.sub.2CN, NHCN, CHO, COOsalt, OSO.sub.2alkyl, SH, SCH.sub.3, CH[(CH.sub.2).sub.nCH.sub.3]COOCH.sub.3, (CH.sub.2).sub.mCOOCH.sub.3, (CH.sub.2).sub.mOCH.sub.3, (CH.sub.2).sub.mO(CH.sub.2).sub.nCH.sub.3, (CH.sub.2).sub.mSCH.sub.3, (CH.sub.2).sub.mS(CH.sub.2).sub.nCH.sub.3, (CH.sub.2).sub.mNH(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkenyl-O(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkenyl-S(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkenyl-N(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkynyl-O(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkynyl-S(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkynyl-N(CH.sub.2).sub.nCH.sub.3, (CH.sub.2).sub.mOH, (CH.sub.2).sub.mONH.sub.2, (CH.sub.2).sub.mSNH.sub.2, NH(CH.sub.2).sub.mCH.sub.3, NH(CH.sub.2).sub.mOCH.sub.3, NH(CH.sub.2).sub.mCHOHCOOH, N(CH.sub.3).sub.2, (CH.sub.2).sub.m(NH)CH.sub.2OH, NHCOOH, (CH.sub.2).sub.mNHCOOH, NO.sub.2, SCN, SO.sub.2alkyl, B(OH).sub.2, (CH.sub.2).sub.mN(CH.sub.3)SO.sub.2NH.sub.3, (CH.sub.2).sub.mNHSO.sub.2NH.sub.2, NHC(S) CH.sub.3, and NHNH.sub.2; and Y is selected from hydrogen, O, OCO(R.sub.6) and OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, othe

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.

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.