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US 2020/0239398 A1Published application
Methylene-cycloalkylacetate derivatives and their use in treatment of neurotropic conditions
AssigneeYissum Research Development Company of the Hebrew University of Jerusalem
InventorsDmitry TSVELIKHOVSKY, Philip LAZAROVICI, Dikla HAHAM, David LANKRI
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Abstract
Methylene-cycloalkylacetate compounds and derivatives thereof and their use in methods for treatment of neurotropic conditions.
Claims20
A compound having the general formula (I), including any stereoisomer or salt thereof:
- wherein
- R101 is selected from H, straight or branched C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl;
- m is an integer selected from 1-10;
- —C(m)— is selected from a straight or branched alkylene, straight or branched alkenylene, straight or branched alkynylene;
- optionally interrupted by at least one heteroatom;
- R102 is selected from —C(═O)R108, —C(═S)R109, —C(═P)R110, —C(═CR111R112)R113, straight or branched C2-C10 alkenyl, straight or branched C2-C10 alkynyl;
- each of R108, R109, R110, R111, R112 and R113 are independently is selected from a group consisting of OH, —OR114, —NH2, —NHR115, —NR116R117;
- each of R114, R115, R116 and R117 are independently selected from straight or branched C1-C10 alkyl;
- l is an integer selected from 1-10;
- —C(l)— is selected from a straight or branched alkylene, straight or branched alkenylene, straight or branched alkynylene;
- optionally interrupted by at least one heteroatom;
- R103, R104, R105 are each independently selected from H, straight or branched C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl;
- provided that when R101 is H
- (i) at least one of R103, R104 and R105 is different than H;
- OR
- (ii) m>1.
13 more elements
A method of treatment of a neurotropic condition in a subject in need thereof;
- said method comprising administering to said subject a compound of the general formula (II), including any stereoisomer or salt thereof:
- wherein
- Ring A is optionally a saturated or unsaturated ring having optionally at least one heteroatom;
- and is optionally substituted by at least one group selected from straight or branched C1-C10 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C10 alkynyl, CN, —OR4, —NR5R6, —C(═O)R7, halogen;
- R4, R5 and R6 are each independently selected from H, halogen, straight or branched C1-C10 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C10 alkynyl;
- R7 is selected from H, straight or branched C1-C10 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C10 alkynyl, halogen, OH, O(C1-C10)alkyl, NH2, amine;
- n is an integer selected from 1-10;
- —C(n)— is selected from a straight or branched alkylene, straight or branched alkenylene, straight or branched alkynylene;
- optionally interrupted by at least one heteroatom;
- m is an integer selected from 1-10;
- —C(m)— is selected from a straight or branched alkylene, straight or branched alkenylene, straight or branched alkynylene;
- optionally interrupted by at least one heteroatom;
- R1 is selected from —C(═O)R8, —C(═S)R9, —C(═P)R10, —C(═CR11R12)R13, straight or branched C2-C10 alkenyl, straight or branched C2-C10 alkynyl;
- each of R8, R9, R10, R11, R12 and R13 are independently is selected from a group consisting of OH, —OR14, —NH2, —NHR15, —NR16R17;
- each of R14, R15, R16 and R17 are independently selected from straight or branched C1-C10 alkyl;
- R2 is selected from O, S, CR18R19;
- each of R18 and R19 is independently selected from H, straight or branched C1-C10 alkyl, halogen, CF3SO3, OH, C1-C10 alkoxy.
- l is an integer selected from 1-10;
- —C(l)— is selected from a straight or branched alkylene, straight or branched alkenylene, straight or branched alkynylene;
- optionally interrupted by at least one heteroatom;
- R3 is selected from C(═O)R20, OR21, C(═O)OR22, CF3SO3, straight or branched C2-C10 alkenyl, straight or branched C2-C10 alkynyl;
- each of alkenyl or alkylenyl groups are optionally substituted by at least one group selected from C(═O)R23, OR24, halogen, CF3SO3;
- each of R20, R21, R22, R23 and R24 is independently selected from H, OH, halogen, straight or branched C1-C10 alkyl, straight or branched C1-C10 alkoxy, NH2, amine.
20 more elements
Dependencies are inferred from the claim text.