C07C311/04

Heterocyclic inhibitors of the sodium channel

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(III) or Compounds (1)-(65) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.

SHIP1 MODULATORS AND METHODS RELATED THERETO

Compounds of formula (I):

##STR00001##

where R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and R.sup.7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

SHIP1 MODULATORS AND METHODS RELATED THERETO

Compounds of formula (I):

##STR00001##

where R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and R.sup.7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Compounds having a structure of Formula I:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Compounds having a structure of Formula I:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Methods for Making Functionalized Fluorinated Monomers, Fluorinated Monomers, and Compositions for Making the Same
20220213016 · 2022-07-07 ·

A method of making a functionalized fluorinated monomer for use in making oligomers and polymers that can be used to improve surface properties of polymer-derived systems, such as coatings. The method of making a functionalized fluorinated monomer includes reacting at least one fluorinated nucleophilic reactant, such as a fluorinated alcohol, with at least one compound containing at least one epoxide group. Other methods include reaction of a fluorinated alcohol with a cyclic carboxylic anhydride. In another embodiment, a method includes reacting a fluorinated mesylate, tosylate or triflate with an amine, alkoxide or phenoxide. In other embodiments, the method includes reacting a fluorinated alcohol with an alkyl halide, or reacting a fluorinated alkyl halide with an amine. The functionalized fluorinated monomers may be used as intermediates and reacted to modify the functional groups thereon. Further, the functionalized fluorinated monomers may be reacted to form polymers or oligomers, or with polymers or oligomers having functional groups to modify the polymer or oligomer through the functional group thereon.

Methods for Making Functionalized Fluorinated Monomers, Fluorinated Monomers, and Compositions for Making the Same
20220213016 · 2022-07-07 ·

A method of making a functionalized fluorinated monomer for use in making oligomers and polymers that can be used to improve surface properties of polymer-derived systems, such as coatings. The method of making a functionalized fluorinated monomer includes reacting at least one fluorinated nucleophilic reactant, such as a fluorinated alcohol, with at least one compound containing at least one epoxide group. Other methods include reaction of a fluorinated alcohol with a cyclic carboxylic anhydride. In another embodiment, a method includes reacting a fluorinated mesylate, tosylate or triflate with an amine, alkoxide or phenoxide. In other embodiments, the method includes reacting a fluorinated alcohol with an alkyl halide, or reacting a fluorinated alkyl halide with an amine. The functionalized fluorinated monomers may be used as intermediates and reacted to modify the functional groups thereon. Further, the functionalized fluorinated monomers may be reacted to form polymers or oligomers, or with polymers or oligomers having functional groups to modify the polymer or oligomer through the functional group thereon.

Bisphenol derivatives and their use as androgen receptor activity modulators

Compounds having a structure of Formula I ##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Bisphenol derivatives and their use as androgen receptor activity modulators

Compounds having a structure of Formula I ##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR USE

Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.