[EN] N-(4-(OXAZOL-5-YL)PHENYL)CHROMANE-3-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS STIMULATORS OF THE PRODUCTION OF RETINAL PRECURSOR CELLS FOR THE TREATMENT OF NEURORETINAL DISEASES<br/>[FR] DÉRIVÉS DE N-(4-(OXAZOL-5-YL) PHÉNYL)CHROMANE-3-CARBOXAMIDE ET COMPOSÉS APPARENTÉS EN TANT QUE STIMULATEURS DE LA PRODUCTION DE CELLULES PRÉCURSEURS RÉTINIENNES POUR LE TRAITEMENT DE MALADIES NEURORÉTINIENNES
申请人：ENDOGENA THERAPEUTICS INC
公开号：WO2020140050A1
公开（公告）日：2020-07-02
New compounds and to a method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, comprising administering compound of the formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or, if applicable, a corresponding diastereomer thereof, wherein: A is a is selected from the group consisting of a 5-oxazolyl, a pyridine-4-yl, a triazolyl, a oxadiazolyl, a imidazolyl and a 2-methyloxazol-5-yl residue, R1, and R12 are independently selected from the group consisting of hydrogen, fluoro, chloro, methoxy, trifluoromethyl, methyl and difluoromethoxy, B is selected from the group consisting of a residue of formula (II), (III), (IV), (V), (VI), (VII), (VIII) and (IX) wherein, II*II denotes the point of attachment to the remainder of the molecule, and R2, R3, R4, R5, R2 I, R3 I, R4 I, R5 I, R2 II, R3 II R4 II, R5 II, R2 III, R3 III, R4 III, R5 III, R2 IV, R3 IV, R4 IV, R5 IV, R2 V, R3 V, R4 V, R5 V , R2 VI, R3 VI, R4 VI, R5 VI,R2 VII, R3 VII, R4 VII, R5 VII, are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, 2,2,2-trifluoromethyl and difluoromethoxy.
新化合物及治疗导致光感受器丧失或外视网膜退化的视网膜疾病的方法，包括给予式(I)的化合物或其药学上可接受的盐、消旋混合物、相应对映体或如适用的话，相应的二对映体，其中：A选自由5-噁唑基、吡啶-4-基、三唑基、噁二唑基、咪唑基和2-甲氧基噁唑-5-基残基的群组，R1和R12独立选自氢、氟、氯、甲氧基、三氟甲基、甲基和二氟甲氧基的群组，B选自式(II)、(III)、(IV)、(V)、(VI)、(VII)、(VIII)和(IX)的残基的群组，其中，II*II表示与分子其余部分的连接点，R2、R3、R4、R5、R2 I、R3 I、R4 I、R5 I、R2 II、R3 II、R4 II、R5 II、R2 III、R3 III、R4 III、R5 III、R2 IV、R3 IV、R4 IV、R5 IV、R2 V、R3 V、R4 V、R5 V、R2 VI、R3 VI、R4 VI、R5 VI、R2 VII、R3 VII、R4 VII、R5 VII独立选自氢、具有1至3个碳原子的直链或支链烷基、氟、氯、溴、甲氧基、乙氧基、丙氧基、2,2,2-三氟甲基和二氟甲氧基的群组。
