Patent classifications
C07J1/0074
19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof
Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
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.
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.
19-NOR NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF
Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I):
##STR00001##
and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.
6-substituted estradiol derivatives and methods of use
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
19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF
Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
USE OF ST-TYPE LIPID COMPOUNDS IN PREPARATION OF NUCLEIC ACID DELIVERY REAGENT AND RELATED PRODUCT
A use of one or more lipid compounds in the delivery of nucleic acids, and a lipid nucleic acid mixture, pharmaceutical composition or kit comprising the lipid compounds and nucleic acids. The lipid compounds can promote the absorption, particularly oral absorption, of nucleic acids, and promote entry of nucleic acids into target sites in a subject in need thereof.
19-nor neuroactive steroids and methods of use thereof
Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): ##STR00001##
and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.
19-NOR C3, 3-DISUBSTITUTED C21-C-BOUND HETEROARYL STEROIDS AND METHODS OF USE THEREOF
Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
19-nor C3,3-disubstituted C21-n-pyrazolyl steroids and methods of use thereof
Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.