摘要:
This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.
摘要:
Compounds of the formula (I) in which: R1 is (CH2)nY; n is 1 or 2; Y is NHSO2R2 or X1—W—X2—R3; X1 is O or NH; W is C═O, C═S, C═NH, or SO2; X2 is O or NH, provided that X1 and X2 are not both O; R2 is C1-10 alkyl; C2-10 alkenyl; C2-10 alkynyl; aryl; aryl-C1-10 alkyl; aryl-C2-10 alkenyl; aryl-C2-10alkynyl; C3-8 cycloalkyl or C3-8-cycloalkyl-C1-10 alkyl; and R3 is hydrogen, C1-10alkyl; C2-10 alkenyl; C2-10 alkynyl; aryl; aryl-C1-10 alkyl; aryl-C2-10 alkenyl; aryl-C2-10 alkynyl; C3-8 cycloalkyl; or C3-8-cycloalkyl-C1-10 alkyl; or a salt or ester thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system.
摘要翻译:式(I)的化合物,其中:R 1是(CH 2)n Y; n为1或2; Y是NHSO 2 R 2或X 1 -WX 2 - 3 - 3 ; X 1是O或NH; W是C-O,C-S,C-NH或SO 2。 X 2是O或NH,条件是X 1和X 2都不是O; R 2是C 1-10烷基; C 2-10链烯基; C 2-10炔基; 芳基; 芳基-C 1-10烷基; 芳基-C 2-10链烯基; 芳基-C 2-10炔基; C 3-8环烷基或C 3-8 - 环烷基-C 1-10烷基; R 3是氢,C 1-10烷基; C 2-10链烯基; C 2-10炔基; 芳基; 芳基-C 1-10烷基; 芳基-C 2-10链烯基; 芳基-C 2-10炔基; C 3-8环烷基; 或C 3-8 - 环烷基-C 1-10烷基; 或其盐或酯调节代谢型谷氨酸受体功能,并且可用于治疗中枢神经系统疾病。
摘要:
Compounds of formula (I) in which R1 is halo-C1-10 alkyl; halo-C2-10 alkenyl; or (CH2)nY in which n is 1 or 2 and Y is OH, CN, N3, OR3, SH, S(O)pR4, S(O)3H, NH2, NHR5, NR6R7, NHCOR8, NO2, CO2H, CONHR9, 1H-tetrazol-5-yl, 5-phenyltetrazol-2-yl or PO3H2; R3, R5, R6, R7, R8 and R9 are each selected independently from C1-4 alkyl, aryl and aryl-C1-4 alkyl; R4 is selected from C1-4 alkyl, aryl, aryl-C1-4 alkyl, and 1H-tetrazol-5-yl, carboxy-(1-4C)alkyl and 1H-tetrazol-5-yl-C1-4 alkyl; and p is 0, 1, 2 or 3; or a salt or ester thereof, provided that R1 is not methoxymethyl, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system.
摘要翻译:其中R 1为卤代C 1-10烷基的式(I)化合物; 卤代-C2-10烯基; 或其中n为1或2且Y为OH,CN,N 3,OR 3,SH,S(O)p R 4,S(O)3 H,NH 2,NHR 5,NR 6 R 7,NHCOR 8,NO 2,CO 2 H,CONHR 9的(CH 2)n Y ,1H-四唑-5-基,5-苯基四唑-2-基或PO 3 H 2; R 3,R 5,R 6,R 7,R 8和R 9各自独立地选自C 1-4烷基,芳基和芳基-C 1-4烷基; R 4选自C 1-4烷基,芳基,芳基-C 1-4烷基和1H-四唑-5-基,羧基 - (1-4C)烷基和1H-四唑-5-基-C 1-4烷基; p为0,1,2或3; 或其盐或酯,条件是R1不是甲氧基甲基,调节代谢型谷氨酸受体功能,并且可用于治疗中枢神经系统的病症。
摘要:
This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.
摘要:
This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.
摘要:
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.
摘要:
This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.
摘要:
Compounds of the formula (I) in which R1 is C1-10 allyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system
摘要翻译:式(I)的化合物,其中R 1为C 1-10烯丙基; C 2-10烯基; C 2-10炔基; 苯基-C 2-10烷基或苯基-C 2-10烯基; 调节代谢型谷氨酸受体功能,可用于治疗中枢神经系统疾病
摘要:
Compounds of the formula (I) in which R1, R2 and X1 have the meanings given in the specification, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system
摘要:
A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.