发明名称 Cycloalkylamines as monoamine reuptake inhibitors
摘要 The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
申请公布号 US8877975(B2) 申请公布日期 2014.11.04
申请号 US201012688474 申请日期 2010.01.15
申请人 Sunovion Pharmaceuticals Inc. 发明人 Shao Liming;Wang Fengjiang;Malcolm Scott Christopher;Hewitt Michael Charles;Bush Larry R.;Ma Jianguo;Varney Mark A.;Campbell Una;Engel Sharon Rae;Hardy Larry Wendell;Koch Patrick;Campbell John E.
分类号 C07C211/17;A61K31/137;C07C211/29;C07C211/40;C07C215/42;C07C215/44;C07C217/52;C07C217/74;C07C323/32;C07D207/06;C07D207/08;C07D211/14;C07D265/14;C07D277/28;C07D295/06;C07D307/52;C07D317/58;C07D317/72;C07D319/06;C07D333/20;C07D491/056 主分类号 C07C211/17
代理机构 Choate, Hall & Stewart LLP 代理人 Choate, Hall & Stewart LLP ;Reid Andrea L. C.;Klein Daniel A.
主权项 1. A compound having a structure according to Formula (II): wherein m is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; Ar is wherein Y and Z are (i) both halogen; or (ii) one of Y and Z is CF3 or OCF3, and the other is hydrogen; each X is independently H, halogen, CF3, OR5, acyl, C(O)OR5, NR6R7, substituted or unsubstituted alkyl, or substituted or unsubstituted heteroalkyl; wherein each R5 is independently H, acyl, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, or substituted or unsubstituted aryl;each R6 and R7 is independently H, or substituted or unsubstituted alkyl; each R1 and R2 is independently H, or substituted or unsubstituted alkyl; and R3 and R4 are each independently H, substituted or unsubstituted alkyl, or substituted or unsubstituted heteroalkyl; or a pharmaceutically acceptable salt, enantiomer, diastereomer, racemic mixture, enantiomerically enriched mixture, or enantiomerically pure form thereof; wherein substituents for alkyl or heteroalkyl radicals are selected from unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted aryl, unsubstituted heteroaryl, unsubstituted heterocycloalkyl, —OR′, ═O, ═NR′, ═N—OR′, —NR′R″, —SR′, -halogen, —SiR′R″R′″, —OC(O)R′, —C(O)R′, —CO2R′, —CONR′R″, —OC(O)NR′R″, —NR″C(O)R′, —NR′—C(O)NR″R′″, —NR″CO2R′, —NR—C(NR′R″R′″)═NR″″, —NR—C(NR′R″)═NR′″, —S(O)R′, —S(O)2R′, —S(O)2NR′R″, —NRSO2R′, —CN and —NO2 in a number ranging from zero to (2m′+1), where m′ is the total number of carbon atoms in such a radical; R′, R″, R′″ and R′″ are each independently selected from hydrogen, unsubstituted heteroalkyl, unsubstituted aryl, unsubstituted alkyl, alkoxy or thioalkoxy groups, or arylalkyl groups; and substituents for aryl radicals are selected from unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted aryl, unsubstituted heteroaryl, unsubstituted heterocycloalkyl, —OR′, ═O, ═NR′, ═N—OR′, —NR′R″, —SR′, -halogen, —SiR′R″R′″, —OC(O)R′, —C(O)R′, —CO2R′, —CONR′R″, —OC(O)NR′R″, —NR″C(O)R′, —NR′—C(O)NR″R′″, —NR″CO2R′, —NR—C(NR′R″R′″)═NR″″, —NR—C(NR′R″)═NR′″, —S(O)R′, —S(O)2R′, —S(O)2NR′R″, —NRSO2R′, —CN, —NO2, —R′, —N3, —CH(Ph)2, fluoro(C1-C4)alkoxy, and fluoro(C1-C4)alkyl, in a number ranging from zero to the total number of open valences on the aromatic ring system; and where R′, R″, R′″ and R′″ are each independently selected from hydrogen, unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted aryl and unsubstituted heteroaryl.
地址 Marlborough MA US