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    • 5. 发明申请
    • SYNTHETIC MACROCYCLIC COMPOUNDS FOR TREATING CANCER
    • 用于治疗癌症的合成大环化合物
    • WO2008098138A1
    • 2008-08-14
    • PCT/US2008/053334
    • 2008-02-07
    • THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICESBEWLEY, Carole, A.METAFERIA, Belhu, B.
    • BEWLEY, Carole, A.METAFERIA, Belhu, B.
    • C07D267/00A61K31/395A61P35/00
    • C07D267/00
    • Disclosed herein are macrocyclic compounds that are effective to inhibit cell migration. In one embodiment, the compounds have the structure: or any pharmaceutically acceptable salt or solvate thereof, wherein: m is O or 1; R 1 , R 2 and R 3 independently are H, aralkyl, acyl, lower alkyl or silyl; X is -C(O)N(R 4 )- or -C(S)N(R 4 )-; -C(O)-; -C(S)-; Y is -OC(O)-; -OC(O)N(R 5 )-; -N(R 5 )C(0)-; or -OC(O)O-; G comprises a saturated or unsaturated aliphatic chain having from 2 to about 10 atoms in the chain, the chain optionally including 1, 2, or 3 heteroatoms; the chain optionally being substituted with 1, 2 or 3 substituents independently selected from lower alkyl, -OR 6 , epoxy, aziridinyl, cyclopropyl, -NR 7 R 8 and halo; R 4 , R 5 , R 6 , R 7 and R 8 independently are selected from H, lower alkyl and acyl. Also disclosed are methods for making and using compounds as well as pharmaceutical compositions including one or more of the disclosed macrocycles.
    • 本文公开了有效抑制细胞迁移的大环化合物。 在一个实施方案中,所述化合物具有以下结构:或其任何药学上可接受的盐或溶剂合物,其中:m为O或1; R 1,R 2和R 3独立地是H,芳烷基,酰基,低级烷基或甲硅烷基; X是-C(O)N(R 4) - 或-C(S)N(R 4) - ; -C(O) - ; -C(S) - ; Y为-OC(O) - ; -OC(O)N(R 5 ) - ; -N(R 5 )C(O) - ; 或-OC(O)O-; G包含在链中具有2至约10个原子的饱和或不饱和脂族链,该链任选地包括1,2或3个杂原子; 该链任选被1,2或3个独立地选自低级烷基,-OR 6,环氧基,氮丙啶基,环丙基,-NR 7 R 8的取代基取代 和光环; R 4,R 5,R 6,R 7和R 8独立地是 选自H,低级烷基和酰基。 还公开了制备和使用化合物的方法以及包含一种或多种所公开的大环化合物的药物组合物。
    • 6. 发明申请
    • HYDRAZONE AGENTS TO TREAT CUTANEOUS LESIONS
    • HYDRAZONE代理治疗CUTANEOUS LESIONS
    • WO2007025186A2
    • 2007-03-01
    • PCT/US2006/033318
    • 2006-08-25
    • DEKK-TEC, INC.MORGAN, Lee, Roy
    • MORGAN, Lee, Roy
    • A61K31/15A61P17/12A61P35/00A61P17/06
    • A61K31/15
    • A method is disclosed for treating hyperproliferative body surface lesions, including cancerous or precancerous lesion, such as warts or anogenital cancers, by applying a polyaryl mononitro- or dinitrophenylhydrazone such as wherein R 1 is hydrogen, hydroxy, 2- or 4-hydroxyphenyl, acetate, nitroso, phosphate, azido, nitrile, amino, dimethylamino, sulfate, methylsulfonate, phosphate, succinate or another water soluble electrophilic group capable of hydrogen bonding; R2 is C 6 H 4 OH, C 6 H 4 N 3 , C 6 H 4 CN, 4-HO-C 6 H 4 -C 6 H 4 , C 6 H 4 OPO 2 OH, C 6 H 4 OSO 2 H, C 6 H 4 NH 2 , C 6 H 4 NHM e2 , C 6 H 4 OSO 2 Me, C 6 H 4 OCO(CH 2 ) x CO 2 H, or C 6 H 5 Cl; and X is C 6 H 3 -2,4(NO 2 ) 2 , C 6 H 4 -4(NO 2 ), C 6 H 4 -3 (NO 2 ), or C 6 H 3 -2,4(NO 2 ) 2 . In a particular example, R 1 is OH, R 2 is C 6 H 4 OH and X is C 6 H 3 -2,4(NO 2 ) 2 .
    • 公开了一种用于治疗过度增生的身体表面损伤的方法,包括癌或癌前病变,例如疣或肛门癌,通过应用多芳基单硝基或二硝基苯腙,其中R 1是氢,羟基,2 - 或4-羟基苯基,乙酸酯,亚硝基,磷酸酯,叠氮基,腈,氨基,二甲基氨基,硫酸酯,甲基磺酸酯,磷酸酯,琥珀酸酯或其他能够氢键合的水溶性亲电基团; R 2是C 6 H 4 OH,C 6 H 4 N 3 N, C 6 H 4 CN,4-HO-C 6 H 4 -C 6, C 4 H 4,C 6 H 4,OH 2,OH,C 6, H 4,OH 2,C 6 H 4,NH 2,C 6, C 6 H 4 NH 3 C 2 H 5,C 6 H 4,OH 2, C,C 6 H 2 O 2(CH 2)2 CO 2 CH 2, H或C 6 H 5 Cl; 和X为C 6 H 3 -2 4(NO 2)2,C 6 H 4 - 4(NO 2 2),C 6 H 4 - 3(NO 3) 或者C 6 H 3 -2 4(NO 2 2)2 。 在具体实例中,R 1是OH,R 2是C 6 H 4 OH,X是C 6 ħ 3 -2,4(NO 2 2
    • 7. 发明申请
    • CONJUGATED AROMATIC COMPOUNDS FOR DIAGNOSIS AND THERAPY
    • 联合用于诊断和治疗的芳香化合物
    • WO2006119284A2
    • 2006-11-09
    • PCT/US2006/016824
    • 2006-05-03
    • DEKK-TEC, INC.MORGAN, Lee Roy
    • MORGAN, Lee Roy
    • A61K31/15A61K41/00C07C251/80C07C251/82
    • C07C251/80C07C251/82
    • Disclosed herein are compounds, compositions and methods for using such compounds and compositions in the treatment of hyperproliferative conditions, including precancerous and cancerous conditions. In one embodiment, the compounds include resonance modulating compounds that can be used in the method as a coupling agent that is capable of interacting with the immune system to monitor or stimulate immune function. Such resonance modulators have inherent electromagnetic properties that attract immune cells to a target area to which the resonance modulating agent has been applied. Electromagnetic properties (such as a voltage amplitude) of the target region are altered in the presence of the resonance modulator, and serve as an indicator of immune function. An external stimulus (such as an applied electromagnetic field) can also be applied to the resonance modulator to enhance its immune stimulating and attractant properties. Particular examples of resonance modulators are disclosed, and these substances generally possess resonating intramolecular dipole moments that are capable of electrostatic interaction with biological environments. In certain examples the compounds aggregate at sites of therapeutic action to enhance their therapeutic activity. In other examples the compounds stimulate platelet production.
    • 本文公开了使用这些化合物和组合物来治疗过度增殖病症(包括癌前病变和癌症病症)的化合物,组合物和方法。 在一个实施方案中,所述化合物包括共振调节化合物,其可以在该方法中用作偶联剂,其能够与免疫系统相互作用以监测或刺激免疫功能。 这种共振调制剂具有将免疫细胞吸引到已经施加共振调节剂的目标区域的固有电磁特性。 在谐振调制器的存在下改变目标区域的电磁特性(如电压振幅),并且作为免疫功能的指标。 外部刺激(例如施加的电磁场)也可以应用于共振调制器以增强其免疫刺激和引诱特性。 公开了共振调制剂的具体实例,并且这些物质通常具有能够与生物环境静电相互作用的共振的分子内偶极矩。 在某些实例中,化合物在治疗作用的部位聚集以增强其治疗活性。 在其他实例中,化合物刺激血小板产生。