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    • 2. 发明授权
    • Pyrrolobenzodiazepines
    • 吡咯并苯并二氮杂卓
    • US06562806B1
    • 2003-05-13
    • US09763814
    • 2001-02-26
    • David Edwin ThurstonPhilip Wilson Howard
    • David Edwin ThurstonPhilip Wilson Howard
    • A61K31555
    • C07D487/04Y02P20/55
    • A compound with formula (I) where R10 is a therapeutically removable nitrogen protecting group; R2 and R3 are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R, CH2—CO2H, CH2—SO2R, O—SO2—R, CO2R, COR and CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, nitro, Me3Sn; X is S, O or NH; R11 is either H or R; and where there is optionally a double bond between C1 and C2 or C2 and C3; and R8 is selected from H, R, OH, OR, halo, amino, nitro, Me3Sn, or R7 and R8 together form a group —O—(CH2)p—O—, where p is 1 or 2. Such compounds may be used in methods of ADEPT, GDEPT, NPEPT or PDT.
    • 具有式(I)的化合物,其中R 10是治疗性除去的氮保护基; R2和R3独立地选自:H,R,OH,OR,= O,= CH-R,= CH2,CH2-CO2R,CH2-CO2H,CH2-SO2R,O-SO2-R,CO2R,COR和CN ; R 6,R 7和R 9独立地选自H,R,OH,OR,卤素,氨基,硝基,Me 3 Sn; X是S,O或NH; R11是H或R; 并且其中C1和C2或C2和C3之间任选具有双键; 并且R 8选自H,R,OH,OR,卤素,氨基,硝基,Me 3 Sn或R 7和R 8一起形成基团-O-(CH 2)p O-,其中p为1或2。 在ADEPT,GDEPT,NPEPT或PDT的方法中。
    • 4. 发明授权
    • Detection and treatment of duplex polynucleotide damage
    • 检测和处理双链多核苷酸损伤
    • US06444661B1
    • 2002-09-03
    • US09448325
    • 1999-11-23
    • Jacqueline K. BartonBrian A. JacksonBrian P. Hudson
    • Jacqueline K. BartonBrian A. JacksonBrian P. Hudson
    • A61K31555
    • C07F15/008
    • Duplex polynucleotides containing damage or errors are detected with hindered intercalating compounds which are capable of intercalating only in the presence of such damage or error. Conditions characterized by the presence of polynucleotide errors or damage are treated with such compounds that are capable of catalyzing polynucleotide cleavage with light. Suitable compound include compounds of the formula: Rh(R1)(R2)(R3)3+ where R1 and R2 are each independently aryl, heteroaryl, substituted aryl or substituted heteroaryl of 1 to 5 rings, and R3 is a group of the formula where x and z are each independently an integer from 1 to 4 and y is an integer from 1 to 2, and R4, R5, and R6 are each independently H—, halo, HO—, H2N—, CN—, O2N—, HS—, O3S—, O3SO—, —COOH, —CONH2, R, RO—, RNH—, RaRbN—, RO3S—, RO3SO—, —COOR, —CONHR, or —CONRaRb, where R, Ra and Rb are each independently lower alkyl, cycloalkyl, lower alkenyl, lower alkynyl, or phenyl, or two R4, R5, or R6 together form a fused aryl ring.
    • 含有损伤或错误的双链多核苷酸用受阻的插入化合物检测,只能在存在这种损伤或错误的情况下插入。 以多核苷酸错误或损伤存在为特征的条件用能够用光催化多核苷酸切割的化合物处理。 合适的化合物包括下式的化合物:其中R 1和R 2各自独立地为1至5个环的芳基,杂芳基,取代的芳基或取代的杂芳基,并且R 3是式的基团,x和z各自独立地为1至4的整数 并且y是1-2的整数,R4,R5和R6分别独立地为H,卤素,HO-,H2N-,CN-,O2N-,HS-,O3S-,O3SO-,-COOH, - CONH2,R,RO-,RNH-,RaRbN-,RO3S-,RO3SO-,-COOR,-CONHR或-CONRaRb,其中R,Ra和Rb各自独立地为低级烷基,环烷基,低级烯基,低级炔基或 苯基或两个R 4,R 5或R 6一起形成稠合的芳基环。