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1.发明授权
公开(公告)号：US5849756A
公开(公告)日：1998-12-15
申请号：US450491
申请日：1995-05-26
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/47 , A61K31/4704 , A61P37/02 , A61P37/04 , A61P37/06 , C07D209/34 , C07D215/50
CPC分类号： C07D215/50 , A61K31/405 , A61K31/4704 , C07D209/34
摘要： Pharmaceutical compositions for the modulation of the immune reaction of warm blooded animals that are derivatives of the 2-oxindole-3-acetic acid or the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid are described, and whereby the derivatives can optionally be in an equilibrium with each other. The derivatives included in the pharmaceutical compositions comprise those compounds which are already described in the literature and also new compounds. Furthermore, new derivatives of the the 2-oxindole-3-acetic acid and the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid are described, particularly also the the pure antipodes of the mixture of enantiomeres of the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid.
摘要翻译： 描述了作为2-羟基吲哚-3-乙酸或2-氧代-1,2,3,4-四氢喹啉-4-羧酸的衍生物的温血动物的免疫反应调节用药物组合物，以及 由此衍生物可以任选地彼此平衡。 包含在药物组合物中的衍生物包括已经在文献中描述的那些化合物，也是新的化合物。 此外，还描述了2-羟基吲哚-3-乙酸和2-氧代-1,2,3,4-四氢喹啉-4-羧酸的新衍生物，特别是对映异构体的对映体混合物的纯对映体 2-氧代-1,2,3,4-四氢喹啉-4-羧酸。
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2.发明授权Glycosides isolated from pollen, their sugar-free decomposition products and derivatives thereof 失效从花粉中分离的糖苷，其无糖分解产物及其衍生物
公开(公告)号：US5712377A
公开(公告)日：1998-01-27
申请号：US672651
申请日：1996-06-28
IPC分类号： C07H15/18 , A61K31/70 , A61K31/7028 , A61K36/00 , A61P31/12 , A61P31/18 , A61P35/00 , C07C62/32 , C07C62/34 , C07C69/757 , C07H15/26 , C07H17/08 , C07C315/00
CPC分类号： C07H17/08 , C07C62/32 , C07C62/34 , C07C69/757
摘要： What are described are new glucosides and their sugar-free decomposition products, as well as synthetically produced derivatives, which can be used as active components of pharmaceutical compositions. The novel glucosides have been isolated from aqueous extracts of vegetable pollen. These novel glucosides, sugar-free decomposition products and their derivatives have the effectiveness to modulate the immune system of warm blooded animals and they can be used as active components in pharmaceutical compositions for the treatment of tumors and virus-related diseases.
摘要翻译： 所描述的是新的葡糖苷及其无糖分解产物，以及可用作药物组合物的活性组分的合成产生的衍生物。 新型葡萄糖苷已经从植物花粉的水提取物中分离出来。 这些新型糖苷，无糖分解产物及其衍生物具有调节温血动物免疫系统的有效性，可用作药物组合物中用于治疗肿瘤和病毒相关疾病的活性成分。
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3.发明授权公开(公告)号：US07622470B2
公开(公告)日：2009-11-24
申请号：US11141868
申请日：2005-05-31
IPC分类号： A61K31/495
CPC分类号： A61K31/519 , A61K31/525 , A61K31/7068 , A61K2300/00
摘要： T cell lymphoma is treated by administering to a patient suffering from T cell lymphoma a therapeutically effective amount of 10-propargyl-10-deazaaminopterin. Remission is observed in human patients, even with drug resistant T cell lymphoma at weekly dosages levels as low as 30 mg/m2. In general, the 10-propargyl-10-deazaaminopterin is administered in an amount of from 30 to 275 mg/m2 per dose.
摘要翻译： 通过向患有T细胞淋巴瘤的患者施用治疗有效量的10-炔丙基-10-脱氮氨基蝶呤来治疗T细胞淋巴瘤。 在人类患者中观察到缓解，即使是耐药性T细胞淋巴瘤，每周剂量水平低至30mg / m2。 通常，10-炔丙基-10-脱氮氨基蝶呤以每剂量30至275mg / m 2的量施用。
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公开(公告)号：US5167963A
公开(公告)日：1992-12-01
申请号：US558923
申请日：1990-07-27
IPC分类号： A61K31/505 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , Y10S424/15 , Y10S514/937 , Y10S514/944 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要： 8,10-Dideazatetrahydrofolic acid derivatives of the formula: ##STR1## where R.sub.1 and R.sub.2 are selected from hydrogen and alkyl having from one to about eight carbon atoms and the carboxylates and acid addition salts thereof, showing strong inhibition of L1210 murine leukemia cells in culture, modest inhibition of glycinamide ribotide transformylase and aminoimidazole carboxamide ribotide transferase, and insignificant inhibition of dihydrofolate reductase and thymidylate synthase enzymes.
摘要翻译： 8,10-二氮杂四氢叶酸衍生物，其分子式如下：其中R 1和R 2选自氢和具有1至约8个碳原子的烷基及其羧酸盐和酸加成盐，表现出强烈的抑制作用 L1210小鼠白血病细胞培养，适度抑制甘氨酰胺核糖核酸转化酶和氨基咪唑羧酰胺核糖转移酶，以及二氢叶酸还原酶和胸苷酸合酶的抑制作用。
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公开(公告)号：US4369319A
公开(公告)日：1983-01-18
申请号：US233280
申请日：1981-02-10
IPC分类号： A61K9/00 , A61K9/02 , A61K31/505 , A61K31/519 , A61P35/00 , A61P35/02 , C07D475/08
CPC分类号： A61K9/0019 , A61K31/505 , A61K9/02 , C07D475/08 , Y10S514/908
摘要： A process and composition are provided employing 10-deazaminopterin and 10-alkyl derivatives thereof for the treatment of leukemia, as well as other tumor systems including those of ascitic character, and also a process for preparing 10-deazaminopterin compounds.
摘要翻译： 提供了使用10-脱氨基蝶呤及其10-烷基衍生物治疗白血病的方法和组合物，以及包括腹水特征的其它肿瘤系统，以及制备10-脱氨甲蝶呤化合物的方法。
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6.发明授权公开(公告)号：US08299078B2
公开(公告)日：2012-10-30
申请号：US12603117
申请日：2009-10-21
IPC分类号： A61K31/495
CPC分类号： A61K31/519 , A61K31/525 , A61K31/7068 , A61K2300/00
摘要： T cell lymphoma is treated by administering to a patient suffering from T cell lymphoma a therapeutically effective amount of 10-propargyl-10-deazaaminopterin. Remission is observed in human patients, even with drug resistant T cell lymphoma at weekly dosages levels as low as 30 mg/m2. In general, the 10-propargyl-10-deazaaminopterin is administered in an amount of from 30 to 275 mg/m2 per dose.
摘要翻译： 通过向患有T细胞淋巴瘤的患者施用治疗有效量的10-炔丙基-10-脱氮氨基蝶呤来治疗T细胞淋巴瘤。 在人类患者中观察到缓解，即使是耐药性T细胞淋巴瘤，每周剂量水平低至30mg / m2。 通常，10-炔丙基-10-脱氮氨基蝶呤以每剂量30至275mg / m 2的量施用。
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7.发明申请公开(公告)号：US20100120777A1
公开(公告)日：2010-05-13
申请号：US12603117
申请日：2009-10-21
IPC分类号： A61K31/519 , A61P35/00
CPC分类号： A61K31/519 , A61K31/525 , A61K31/7068 , A61K2300/00
摘要： T cell lymphoma is treated by administering to a patient suffering from T cell lymphoma a therapeutically effective amount of 10-propargyl-10-deazaaminopterin. Remission is observed in human patients, even with drug resistant T cell lymphoma at weekly dosages levels as low as 30 mg/m2. In general, the 10-propargyl-10-deazaaminopterin is administered in an amount of from 30 to 275 mg/m2 per dose.
摘要翻译： 通过向患有T细胞淋巴瘤的患者施用治疗有效量的10-炔丙基-10-脱氮氨基蝶呤来治疗T细胞淋巴瘤。 在人类患者中观察到缓解，即使是耐药性T细胞淋巴瘤，每周剂量水平低至30mg / m2。 通常，10-炔丙基-10-脱氮氨基蝶呤以每剂量30至275mg / m 2的量施用。
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8.发明授权Combinations of 10-propargyl-10-deazaaminopterin and taxols and methods of using same in the treatment of tumors 有权10-炔丙基-10脱氨基蝶呤和紫杉醇的组合及其在肿瘤治疗中的应用方法公开(公告)号：US06323205B1
公开(公告)日：2001-11-27
申请号：US09505571
申请日：2000-02-17
IPC分类号： A61K31505
CPC分类号： C07D475/08 , A61K31/505 , A61K31/519 , A61K31/555 , A61K33/24 , A61K31/475 , A61K31/335 , A61K2300/00
摘要： Preliminary clinical studies in humans have now been done which show both the efficacy of 10-propargyl-10dAM and a preferred dosage schedule for such treatments. In addition, it has now been determined that combinations of 10-propargyl-10-deazaaminopterin (preferably highly purified forms, substantially free of 10-deazaaminopterin) with taxols exhibit synergistic effectiveness in the treatment of tumors. 10-propargyl-10-deazaaminopterin and a taxol in therapeutically effective amounts can be administered concurrently, one right after the other, or with a period of time in between.
摘要翻译： 现在已经进行了人类的初步临床研究，其显示了10-炔丙基-10dAM的功效和这种治疗的优选剂量方案。 此外，现在已经确定，10-炔丙基-10-脱氮氨基蝶呤（优选高度纯化的形式，基本上不含10-脱氮氨基蝶呤）与紫杉醇的组合在肿瘤治疗中表现出协同的有效性。 10-炔丙基-10-脱氮氨基蝶呤和治疗有效量的紫杉醇可以同时给药，一个接一个给药，或者一段时间。
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9.发明授权Heteroaroyl 10-deazaamino-pterine compounds and use for rheumatoid arthritis 失效十二烷酰基10-脱氮氨基 - 蝶呤化合物，用于类风湿性关节炎
公开(公告)号：US5354751A
公开(公告)日：1994-10-11
申请号：US90750
申请日：1993-07-12
IPC分类号： C07D471/04 , C07D475/08 , A61K31/505
CPC分类号： C07D471/04 , C07D475/08
摘要： There is disclosed certain heteroaroyl 10-deazaaminopterin and 5, 10 and 8, 10 di deazaminopterin compounds and their use for treatment of rheumatoid arthritis and related diseases and preparative process.Also disclosed are 10 alkenyl-(and alkynyl) 10-deazaminopterins also disclosed for treatment of rheumatoid arthritis and for leukemia and ascites tumors and preparative process.
摘要翻译： 公开了一些杂芳酰化的10-脱氮氨基蝶呤和5,10,10,8,10二脱氨基蝶呤化合物及其用于治疗类风湿性关节炎和相关疾病及其制备方法。 还公开了还公开用于治疗类风湿性关节炎和白血病和腹水肿瘤的10种烯基 - （和炔基）10-脱氨基蝶呤和制备方法。
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公开(公告)号：US4532241A
公开(公告)日：1985-07-30
申请号：US571505
申请日：1984-01-17
IPC分类号： C07D471/04 , A61K31/505 , C07D487/04
CPC分类号： C07D471/04
摘要： 10-Alkyl-8,10-dideazaminopterins of the formula ##STR1## where R is hydrogen or alkyl of 1 to about 8 carbon and their carboxylate and acid addition salts are described. These compounds exhibit antineoplastic activity that is similar to, but more effective than, methotrexate.
摘要翻译： 其中R为氢或1至约8个碳的烷基及其羧酸盐和酸加成盐的式“IMAGE”的10-烷基-8,10-二氮杂opter。素。 这些化合物表现出与甲氨蝶呤相似但更有效的抗肿瘤活性。
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