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    • 4. 发明申请
    • REAGENTS AND PROCEDURES FOR HIGH-SPECIFICITY LABELING
    • 高特异性标签的试剂和程序
    • WO2003107010A1
    • 2003-12-24
    • PCT/US2003/018792
    • 2003-06-13
    • RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    • EBRIGHT, Richard, H.EBRIGHT, Yon, W.
    • G01N33/68
    • C07F9/78C07F9/706C07F9/806G01N33/533G01N33/582Y10S436/80
    • A molecule with two pendant phenylarsine moieties according to the general structural Formula (I) and tautomers, acids, and salts thereof, wherein: (i) Rl or R2, are each independently O-, S-, OR 3 or SR 3 with the provision that if either Rl or R2 is absent, the other remaining group is =0 or =S; or Rl and R2, together with the arsenic atom, form a ring according to one of the general structural Formulae (II), (III), (IV), or (V), wherein R3 is H, CH(OH)CH20H, or (CH2)y- Y, with q being 1-4 and Y being H, OH, NH2, SH, COOH, OAc, CONH2 or CN, and Z represents a hydrocarbon chain comprising 2-4 singly or doubly bonded carbon atoms each of which may be further substituted with one or more of hydrogen, methyl, ethyl, 1-propyl, 2-propyl, methoxy, hydroxy, amino, carboxy, sulfo, oxo, thio, halo (fluoro, chloro, bromo, or fluoro) and (CH2)„ "SO3, wherein n" is 1 or 2.
    • 具有根据一般结构式(I)的两个侧链胂基部分的分子和互变异构体,酸和其盐,其中:(i)R 1或R 2各自独立地为O,S-,OR 3或SR 3,其中 规定如果R1或R2不存在,另一个剩余的基团为= 0或= S; 或者R 1和R 2与砷原子一起形成根据通式(II),(III),(IV)或(V)之一的环,其中R 3是H,CH(OH)CH 2 OH, 或(CH2)y-Y,其中q为1-4,Y为H,OH,NH2,SH,COOH,OAc,CONH2或CN,Z表示包含2-4个单键或双键碳原子的烃链 可以进一步被氢,甲基,乙基,1-丙基,2-丙基,甲氧基,羟基,氨基,羧基,磺基,氧代,硫代,卤代(氟,氯,溴或氟)中的一个或多个取代, 和(CH 2)“”SO 3,其中n“为1或2。
    • 8. 发明申请
    • ARYL SUBSTITUTED AMINO ACIDS, CNS INFLUENCING AGENTS
    • ARYL替代氨基酸,CNS影响剂
    • WO1995015941A1
    • 1995-06-15
    • PCT/GB1994002689
    • 1994-12-09
    • UNIVERSITY OF BRISTOLTOCRIS COOKSON LIMITEDWATKINS, Jeffrey, CliftonJANE, David, EdwardBRISE, Ewan, Fraser
    • UNIVERSITY OF BRISTOLTOCRIS COOKSON LIMITED
    • C07C229/36
    • C07C229/38C07C229/36C07C229/50C07C2601/02C07C2601/08C07F9/304C07F9/306C07F9/3834C07F9/3882C07F9/74C07F9/76C07F9/78
    • Compounds of formula (I) are disclosed, wherein: Ar is an aromatic group having up to 10 carbon atoms substituted by at least one substituent selected from hydroxy, carboxy, phosphono, -PO2H(OR ), phosphinico, -PO2H(R ), -OPO3H2, -OPO2H(OR ), arsono, -AsO2H(OR ), arsinico, -AsO2H(R ), tetrazolyl, sulpho, sulphino, sulpheno, thio, -OSO3H and -(CR R )qY, where Y is carboxy, phosphono, -PO2H(OR ), phosphinico, -PO2H(R ), -OPO3H2, -OPO2H(OR ), arsono, -AsO2H(OR ), arsinico, -AsO2H(R ), tetrazolyl, sulpho, sulphino, sulpheno, -OSO3H and R and R are the same or different and are selected from hydrogen, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl or halo or R and R together constitute an oxo group, q is an integer from 0 to 3; Ar being optionally further substituted by one or more substituents selected from fluoro, chloro, bromo, iodo, nitro, cyano, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, haloalkyl (such as trifluoromethyl), aryl or azido; R is hydrogen, C1 to C6 alkyl, C2 to C6 alkenyl or C2 to C6 alkynyl, aryl, aralkyl, biaryl or C3 to C8 cycloalkyl, haloalkyl or hydroxyalkyl; R , R , R and R are the same or different and are selected from hydrogen, C1 to C6 alkyl, C2 to C6 alkenyl and C2 to C6 alkynyl; R is C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, aryl, aralkyl, biaryl or C3 to C8 cycloalkylene; Q is carboxy, C1 to C6 alkoxycarbonyl, aminocarbonyl, C1 to C6 alkylaminocarbonyl or hydroxamic acid; and p is an integer form 0 to 3; R and R , R and Ar, R and Ar, R and Ar and R and NR R optionally being linked to form a carbocyclic ring and pharmaceutically acceptable acid or base addition salts thereof. The compounds may be used as agents to influence the central nervous system.
    • 公开了式(I)的化合物,其中:Ar是具有至多10个碳原子的芳基,被至少一个选自羟基,羧基,膦酰基,-PO2H(OR 6),亚磷酰基,-PO2H( R 6),-OPO 3 H 2,-OPO 2 H(OR 6),arsono,-AsO 2 H(OR 6),亚硫酰基,-AsO 2 H(R 6),四唑基,磺基, -OSO 3 H和 - (CR 7 R 8)q Y,其中Y是羧基,膦酰基,-PO2H(OR 6),亚磷酰基,-PO2H(R6),-OPO3H2,-OPO2H (OR 6),亚砷基,-AsO 2 H(R 6),四唑基,磺基,亚磺酰基,磺基,-OSO 3 H和R 7和R 8相同 或不同,并且选自氢,C1至C6烷基,C2至C6烯基,C2至C6炔基或卤素或R 7和R 8一起构成氧代基,q为0至3的整数; Ar任选进一步被一个或多个选自氟,氯,溴,碘,硝基,氰基,C 1至C 6烷基,C 2至C 6烯基,C 2至C 6炔基,卤代烷基(例如三氟甲基),芳基或叠氮基的取代基取代。 R 3是氢,C 1至C 6烷基,C 2至C 6烯基或C 2至C 6炔基,芳基,芳烷基,联芳基或C 3至C 8环烷基,卤代烷基或羟烷基; R 1,R 2,R 4和R 5相同或不同,并且选自氢,C 1至C 6烷基,C 2至C 6烯基和C 2至C 6炔基; R 6是C 1 -C 6烷基,C 2至C 6烯基,C 2至C 6炔基,芳基,芳烷基,联芳基或C 3至C 8亚环烷基; Q为羧基,C1至C6烷氧基羰基,氨基羰基,C1至C6烷基氨基羰基或异羟肟酸; p为0〜3的整数; R 1和R 2,R 3和Ar,R 1和Ar,R 2和Ar和R 3和NR 4 R 5任选被连接形成 碳环和其药学上可接受的酸或碱加成盐。 该化合物可用作影响中枢神经系统的药剂。