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    • 64. 发明申请
    • Dosing regimen for gemcitabine HCV therapy
    • 吉西他滨HCV治疗的给药方案
    • US20030225029A1
    • 2003-12-04
    • US10367388
    • 2003-02-14
    • Lieven J. Stuyver
    • A61K031/7072A61K031/513
    • C07H19/06C07H19/16
    • A dosage regiment for the treatment of a Flaviviridae infection, including a hepatitis C viral infection, that includes administering gemcitabine (or its salt, prodrug or derivative, as described herein) in a dosage range of approximately 50 mg/m2 to about 1300 mg/m2 per day for between one and seven days (e.g. 1, 2, 3, 4, 5, 6, or 7 days) followed by cessation of therapy. Viral load is optionally monitored over time, and after cessation, viral rebound is monitored. Therapy is not resumed unless a significant viral load is again observed, and then therapy for 1-7 days and more preferred, 1, 2 or 3 days, is repeated. This therapy can be continued indefinitely to monitor and maintain the health of the patient.
    • 用于治疗黄病毒科感染(包括丙型肝炎病毒感染)的剂量组,其包括以约50mg / m 2至约约50mg / m 2的剂量范围施用吉西他滨(或其盐,前药或衍生物,如本文所述) 1300mg / m 2,每天1至7天(例如1,2,3,4,5,6或7天),然后停止治疗。 可随时随地监测病毒载量,停止后监测病毒反弹。 除非再次观察到显着的病毒载量,否则不会恢复治疗,然后重复1-7天,更优选1,2或3天的治疗。 这种治疗可以无限期地持续以监测和维持患者的健康。
    • 67. 发明申请
    • Substituted diamino-1,3,5-triazine derivatives
    • 取代的二氨基-1,3,5-三嗪衍生物
    • US20030199473A1
    • 2003-10-23
    • US10397760
    • 2003-03-26
    • Janssen Pharmaceutica N.V.
    • Paul A.J. JanssenJan HeeresHenri E.L. MoereelsMichael Joseph KuklaDonald W. Ludovici
    • A61K031/721A61K031/7072A61K031/551A61K031/66A61K031/513A61K031/16
    • C07D403/06C07D251/18C07D251/48C07D405/06C07D405/12C07D409/12
    • This invention concerns the compounds of formula 1 the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)aminocarbonyl; dihydro-2(3H)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)aminoC1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.
    • 本发明涉及式的化合物,其药学上可接受的酸加成盐及其立体化学异构形式,其中R 1和R 2各自独立地选自氢; 羟基; 氨基; 任选取代的C 1-6烷基; C 1-6烷氧基; C 1-6烷基羰基; C 1-6烷氧基羰基; Ar <1>; 单或二(C 1-6烷基)氨基; 单或二(C 1-6烷基)氨基羰基; 二氢-2(3H) - 呋喃酮; 或R 1和R 2一起可以形成吡咯烷基,哌啶基,吗啉基,叠氮基或单或二(C 1-6烷基)氨基C 1-4亚烷基; R 3是氢,Ar 1,C 1-6烷基羰基,C 1-6烷基,C 1-6烷氧基羰基,被C 1-6烷氧基羰基取代的C 1-6烷基; R 4,R 5,R 6,R 7和R 8各自独立地选自氢,卤素,C 1-6烷基,C 1-6烷氧基,氰基,氨基羰基,硝基,氨基, 三卤甲基或三卤代甲氧基; L是任选取代的C 1-10烷基; C3-10烯基; C3-10炔基; C 3-7环烷基; Ar 1是任选取代的苯基; 用于制造用于治疗患有HIV(人类免疫缺陷病毒)感染的受试者的药物。 它还涉及作为式(I)化合物的亚组的新化合物,其制备方法和包含它们的组合物。