发明名称 SALTS OF POTASSIUM ATP CHANNEL OPENERS AND USES THEREOF
摘要 Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
申请公布号 US2014364425(A1) 申请公布日期 2014.12.11
申请号 US201414466852 申请日期 2014.08.22
申请人 Essentialis, Inc. 发明人 Cowen Neil M.;Pasternak Richard C.
分类号 C07D285/24;A61K31/44;A61K31/549 主分类号 C07D285/24
代理机构 代理人
主权项 1. A method for treating dyslipidemia in a subject, the method comprising administering to the subject: a. a formulation comprising one or more omega-3 fatty acids, and b. a formulation comprising a therapeutically effective amount of a KATP channel opener, said KATP channel opener comprising: (i) an anion of a KATP channel opener selected from the group consisting of Formula I, Formula II, Formula III and Formula IV,wherein in Formulas I and II: R1 is selected from the group consisting of hydrogen, C1-C6 alkyl, substituted C1-C6 alkyl, cycloalkyl, and substituted cycloalkyl provided however that when R1 is a substituted C1-C6 alkyl or a substituted cycloalkyl, then the substituent does not include an amino group; R2a is hydrogen; R2b is hydrogen; X is a 1, 2 or 3 atom chain, wherein each atom is independently selected from carbon, sulfur and nitrogen, and each atom is optionally substituted with halogen, hydroxyl, C1-C6 alkyl, substituted C1-C6 alkyl, C1-C6 alkoxy, cycloalkyl, substituted cycloalkyl, or substituted C1-C6 alkoxy, provided however that when an atom of the chain is substituted with substituted C1-C6 alkyl, substituted C1-C6 alkoxy or substituted cycloalkyl, then the substituent does not include an amino group; and ring B is saturated, monounsaturated, polyunsaturated or aromatic, andwherein in Formulas III and IV: R1 is selected from the group consisting of hydrogen, C1-C6 alkyl, substituted C1-C6 alkyl, and cycloalkyl provided however that when R1 is a substituted C1-C6 alkyl, then the substituent does not include an amino group; R2a is hydrogen; R2b is hydrogen; R3 is selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, substituted C1-C6 alkyl, cycloalkyl and substituted cycloalkyl provided however that when R3 is a substituted C1-C6 alkyl, then the substituent does not include an amino group; R4 is selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, substituted C1-C6 alkyl, cycloalkyl and substituted cycloalkyl provided however that when R4 is a substituted C1-C6 alkyl, then the substituent does not include an amino group, and (ii) a cation selected from the group consisting of an alkali metal and a compound comprising an ammonium group comprising at least one tertiary amine group.
地址 Carlsbad CA US