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1. 发明授权

US09655975B2 Prodrug using nitroimidazole 有权
公开(公告)号：US09655975B2
公开(公告)日：2017-05-23
申请号：US14376459
申请日：2013-02-13
申请人： UNIVERSITY OF TSUKUBA
发明人： Yukio Nagasaki , Yutaka Ikeda , Hikaru Hisano
IPC分类号： A61K47/46 , A61K47/48 , C07D233/91 , C07D403/06 , C07H15/252 , C07D475/08 , C07H15/244 , C07H19/06 , A61K31/196 , A61K31/198 , A61K31/519 , A61K31/58 , A61K31/704 , A61K31/7068 , C07H15/24 , C07D487/04 , C07J43/00
CPC分类号： A61K47/48061 , A61K31/196 , A61K31/198 , A61K31/519 , A61K31/58 , A61K31/704 , A61K31/7068 , A61K47/545 , C07D233/91 , C07D403/06 , C07D475/08 , C07D487/04 , C07H15/24 , C07H15/244 , C07H15/252 , C07H19/06 , C07J43/003
摘要： Provided is a prodrug of 2-nitro-1-imidazolepropionic acid and a therapeutically active organic compound having on the molecule an amino group, a cyclic amino group or a hydroxyl group, particularly a prodrug in which the therapeutically active organic compound is selected from among antitumor agents. The prodrug cleaves specifically under hypoxic conditions in vivo to exhibit the inherent therapeutic activity.

2. 发明授权

US06875746B1 Anticancer anthraquinones and method of use thereof 失效
标题翻译：抗癌蒽醌类及其使用方法
公开(公告)号：US06875746B1
公开(公告)日：2005-04-05
申请号：US10355483
申请日：2003-01-31
申请人： Muraleedharan G. Nair , Robert H. Cichewicz , Navindra P. Seeram , Yanjun Zhang
发明人： Muraleedharan G. Nair , Robert H. Cichewicz , Navindra P. Seeram , Yanjun Zhang
IPC分类号： C07H15/244 , A61K31/122 , A61K31/21 , A61K31/70 , A61K31/704 , A61P33/10 , A61P33/12 , C07C50/34 , C07C50/38 , C07C66/02 , C07C69/157 , A01N43/04 , A01N37/00
CPC分类号： A61K31/70 , A61K31/21 , C07C50/38 , Y02A50/423
摘要： Anthraquinones are described which have anticancer or antitumor activity and which are useful for inhibiting cancer cells and cells comprising tumors in vitro or in vivo. Preferably, the anthraquinones have the chemical formula: wherein R1 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R2 is a group containing 1-12 carbons selected from the group consisting of alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate and combinations thereof; and R3 is a group containing 1 to 12 carbons selected from the group consisting of methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, and combinations thereof. The preferred anthraquinones are 1-hydroxy-2-acetyl-3,6-methyl anthraquinone, 2-acetyl-3,6-methyl anthraquinone monoacetate, 1-hydroxy-2-acetyl-3,7-methyl anthraquinone, 2-acetyl-3,7-methyl anthraquinone monoacetate, 1,2,8-trihydroxy-3-methyl anthraquinone, 1,8-dihydroxy-2-O-β-D-glucopyranoside anthraquinone, 1,2,8-trihydroxy-3-hydroxymethyl anthraquinone, and 1,8-dihydroxy-3-carboxy anthraquinone.
摘要翻译：描述了具有抗癌或抗肿瘤活性的蒽醌，其可用于在体外或体内抑制癌细胞和包含肿瘤的细胞。优选地，蒽醌具有以下化学式：其中R 1选自氢，烷基和取代的烷基; R2是含有选自烷基，取代的烷基，醛，羟基，羟甲基，酸基，碳水化合物及其组合的1-12个碳的基团; 并且R 3是选自甲基，烷基，取代的烷基，醛，羟基，羟甲基，酸基，碳水化合物及其组合中的1至12个碳的基团。优选的蒽醌是1-羟基-2-乙酰基-3,6-甲基蒽醌，2-乙酰基-3,6-甲基蒽醌单乙酸酯，1-羟基-2-乙酰基-3,7-甲基蒽醌，2-乙酰基 - 3,7-甲基蒽醌单乙酸酯，1,2,8-三羟基-3-甲基蒽醌，1,8-二羟基-2-O-β-D-吡喃葡萄糖苷蒽醌，1,2,8-三羟基-3-羟甲基蒽醌，和1,8-二羟基-3-羧基蒽醌。

3. 发明授权

US5710260A Method of extracting sennosides A, B and A1 失效
标题翻译：方法A，B和A1的提取
公开(公告)号：US5710260A
公开(公告)日：1998-01-20
申请号：US614772
申请日：1995-12-21
申请人： Alfons Carcasona , Wolf Grimminger , Pentti Hietala , Helga Zaeske , Klaus Witthohn
发明人： Alfons Carcasona , Wolf Grimminger , Pentti Hietala , Helga Zaeske , Klaus Witthohn
IPC分类号： C07H15/24 , C07H15/244 , A61K35/78 , C07H1/00
CPC分类号： C07H15/24
摘要： Sennosides A, B and Al of the formula: ##STR1## which are substantially free from sennosides C, D and Dl, and from aloe-emodin derivatives, are prepared by a process wherein a) a sennoside mixture is reduced to rhein-9-anthrone-8-glucoside and aloe-emodin-9-anthrone-8-glucoside, b) a liquid-liquid partitioning of the compounds obtained is carried out between a polar organic solvent which is only partly miscible with water and an aqueous phase and c) the rhein-9-anthrone-8-glycosides contained after the partitioning in the aqueous phase is again oxidized to the corresponding sennosides and these are recovered.
摘要翻译：通过以下方法制备基本上不含番茄苷C，D和D1以及来自芦荟大黄素衍生物的公式：IMAGE的Sennosides A，B和Al，其中a）将sennoside混合物还原成大黄酸-9- 蒽酮-8-葡萄糖苷和芦荟大黄素-9-蒽酮-8-葡萄糖苷，b）所得化合物的液 - 液分配在仅与水和水相部分混溶的极性有机溶剂和c ）在水相中分配后含有的大黄酸-9-蒽酮-8-糖苷被再次氧化成相应的天花苷，并且这些被回收。

4. 发明授权

US5621002A Prodrugs for enzyme mediated activation 失效
标题翻译：用于酶介导活化的前药
公开(公告)号：US5621002A
公开(公告)日：1997-04-15
申请号：US302459
申请日：1994-09-09
申请人： Klaus Bosslet , J org Czech , Dieter Hoffmann , Andrea Vasella , Roland Hoos , Fran.cedilla.ois Tillequin , Jean-Claude Florent , Michel Azoulay , Claude Monneret , Jean-Claude Jacquesy , Jean-Pierre Gesson , Michel Koch
发明人： Klaus Bosslet , J org Czech , Dieter Hoffmann , Andrea Vasella , Roland Hoos , Fran.cedilla.ois Tillequin , Jean-Claude Florent , Michel Azoulay , Claude Monneret , Jean-Claude Jacquesy , Jean-Pierre Gesson , Michel Koch
IPC分类号： C07H15/203 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K47/48 , A61P35/00 , A61P43/00 , C07H15/244 , A61K31/335 , A61K31/34
CPC分类号： B82Y5/00 , A61K47/48092 , A61K47/48761 , Y10S514/01
摘要： Enzymatically clearable prodrugs with reduced Michaelis-Menten constant (Km) are described.
摘要翻译：描述了具有降低的Michaelis-Menten常数（Km）的可酶促清除的前药。

5. 发明授权

US5118673A Uses of aloe products 失效
标题翻译：使用芦荟产品
公开(公告)号：US5118673A
公开(公告)日：1992-06-02
申请号：US558905
申请日：1990-07-27
申请人： Robert H. Carpenter , Harley R. McDaniel , Bill H. McAnalley
发明人： Robert H. Carpenter , Harley R. McDaniel , Bill H. McAnalley
IPC分类号： A61K31/715 , A61K36/886 , C07H15/24 , C07H15/244 , C08B37/00
CPC分类号： C08B37/0087 , A61K31/715 , A61K31/736 , A61K36/886 , C07H15/24 , C07H15/244 , C08B37/00 , A61K2039/55583 , Y10S514/935
摘要： Acemannan has been shown to be effective in treating a number of conditions where the principal mechanism of resolution or cure requires intervention by the patient's immune system. Acemannan has direct stimulatory effects on the immune system. Methods for treating cancer, viral diseases, respiratory and immune regulatory diseases, inflammations, infections and infestations by administering an acetylated mannan derivative, such as acemannan derived from aloe, are described. The method finds use in tissue cultures, animals and plants.
摘要翻译：艾司曼尼已被证明能有效地治疗许多解决或治愈的主要机制需要患者免疫系统干预的情况。 Acemannan对免疫系统具有直接的刺激作用。描述了通过施用乙酰化的甘露聚糖衍生物如来自芦荟的acemannan来治疗癌症，病毒性疾病，呼吸和免疫调节性疾病，炎症，感染和感染的方法。该方法可用于组织培养，动物和植物。

6. 发明授权

US5091371A Antifungal and antiviral antibiotic, benanomicin A 4"'-O-sulfate or its salt, and the production and uses thereof 失效
标题翻译：抗真菌和抗病毒抗生素，贝那霉素A 4“' - O-硫酸盐或其盐及其生产和用途
公开(公告)号：US5091371A
公开(公告)日：1992-02-25
申请号：US545696
申请日：1990-06-29
申请人： Tomio Takeuchi , Shinichi Kondo , Daishiro Ikeda
发明人： Tomio Takeuchi , Shinichi Kondo , Daishiro Ikeda
IPC分类号： C07H15/24 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , C07H15/244
CPC分类号： C07H15/244
摘要： As a new antifungal and antiviral antibiotic is provided benanomicin A 4"'-O-sulfate or a salt thereof having formula (I) ##STR1## wherein M.sup.1 denotes a mono-valent alkali metal atom or a di-valent alkaline earth metal atom or a hydrogen atom and A denotes an organic base; n is zero when M.sup.1 is an alkali metal atom or alkaline earth metal atom but n is 1 or zero when M.sup.1 is a hydrogen atom, and M.sup.2 denotes a hydrogen atom or an alkali metal atom or an alkaline earth metal atom. This new compound is useful as antifungal agent to treat fungal infections in mammals and as antiviral agent to inhibitingly treat HIV.
摘要翻译：作为新的抗真菌剂和抗病毒抗生素，提供了具有式（I）的苯那霉素A 4“' - O-硫酸盐或其盐，其中M1表示一价碱金属原子或二碱式金属原子或氢原子，A表示有机碱; 当M1为碱金属原子或碱土金属原子，当M1为氢原子时，n为1或为零，m为氢原子或碱金属原子或碱土金属原子时，n为0。这种新化合物可用作抗真菌剂，用于治疗哺乳动物的真菌感染，以及作为抗病毒剂来抑制HIV治疗。

7. 发明授权

US4939125A Acyl derivatives of urdamycin A, their preparation and their use 失效
标题翻译：尿素霉素A的酰基衍生物，其制备及其用途
公开(公告)号：US4939125A
公开(公告)日：1990-07-03
申请号：US89442
申请日：1987-10-05
申请人： Axel Zeeck , Thomas Ciesiolka , Hans Zahner , Hannelore Drautz
发明人： Axel Zeeck , Thomas Ciesiolka , Hans Zahner , Hannelore Drautz
IPC分类号： C07H15/252 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/244
CPC分类号： C07H15/244 , Y10S435/896 , Y10S514/908
摘要： The O-acyl derivatives of urdamycin A exhibit an antibiotic or antitumoral activity.
摘要翻译：尿绿霉素A的O-酰基衍生物显示抗生素或抗肿瘤活性。

8. 发明授权

US4459291A Compounds having antibiotic activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments 失效
标题翻译：具有抗生素活性的化合物，其制备方法，含有它们的药物组合物及其作为药物的用途
公开(公告)号：US4459291A
公开(公告)日：1984-07-10
申请号：US400537
申请日：1982-07-21
申请人： Kunikatsu Shirahata , Takao Iida
发明人： Kunikatsu Shirahata , Takao Iida
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , C07D493/18 , C07H15/244 , C07H17/04 , C12P19/60 , C12R1/465 , C07H15/24 , A61K31/35 , A61K31/71 , C07D311/02
CPC分类号： C07D493/18 , C07H17/04 , C12P19/60 , C12R1/465
摘要： New antibacterial compounds, DC--45--A.sub.1 and DC--45--A.sub.2 are produced by fermentation of a microorganism belonging to the genus Streptomyces. The antibiotics are accumulated in the culture liquor and are isolated therefrom. These compounds are also prepared by acid hydrolysis of known compounds, DC--45--A or DC--45--B.sub.2. DC--45--A.sub.2 is also prepared by acid hydrolysis of DC--45--A.sub.1.
摘要翻译：新型抗菌化合物DC-45-A1和DC-45-A2通过发酵属于链霉菌属的微生物产生。抗生素在培养液中积聚并从中分离。这些化合物也可以通过已知化合物DC-45-A或DC-45-B2的酸水解来制备。 DC-45-A2也通过DC-45-A1的酸水解制备。

9. 发明授权

US3925354A Process for the production of an 1-n-(s)-alpha- substituted-w-aminoacyl) derivative of neamine, 3', 4'-dideoxyneamine, ribostamycin or 3',4'-dideoxyribostamycin 失效
标题翻译：制备1-N-（S）-ALPHA-取代的W-氨基亚氨基的方法）衍生物，3'，4'-二脱氧山梨醇，RIBOSTAMYCIN或3'，4'-二氧代吡啶甲酰胺
公开(公告)号：US3925354A
公开(公告)日：1975-12-09
申请号：US40208673
申请日：1973-10-01
申请人： MICROBIAL CHEM RES FOUND
发明人： UMEZAWA HAMAO , UMEZAWA SUMIO , TSUCHIYA OSAMU
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61K31/704 , A61P31/04 , C07H15/224 , C07H15/23 , C07H15/236 , C07H15/244 , C07H1/00
CPC分类号： C07H15/224 , C07H15/23 , C07H15/234
摘要： A new process of synthetizing an 1-N-((S)- Alpha -substitutedomega -aminoacyl) derivatives of aminoglycosidic antibiotic, including known compounds such as butirosin B as well as new compounds such as the derivatives of neamines and deoxyribostamycins, is provided according to this invention, in which process the initial aminoglycosidic antibiotic is poly-Nalkloxy- or -aralkyloxy- or aryloxy-carbonylated, the resulting poly-N-alkyloxy- or aralkyloxy- or aryloxy-carbonylated product is treated with a strong base such as sodium hydroxide or an alkali metal hydride to form the cyclic carbamate derivative according to new reactions and in which the cyclic carbamate derivative is treated with a weak base such as barium hydroxide to convert the 1-amino group of the antibiotic selectively into the free state while the other amino groups still remain in the protected condition. The 1-amino group of the antibiotic having the other amino groups protected is then acylated by reacting with the (S)- Alpha -substituted-107 -amino acid, and the acylation product is treated so as to remove the amino-protecting groups, giving the desired compound.

10. 发明授权

US3893997A Pseudodisaccharide intermediates 失效
标题翻译：伪二糖中间体
公开(公告)号：US3893997A
公开(公告)日：1975-07-08
申请号：US48449574
申请日：1974-07-01
申请人： SMITHKLINE CORP
发明人： COOPER DAVID J , WEISBACH JERRY A
IPC分类号： C07H15/244 , C07H15/224 , C07H15/23 , C07H15/236 , C07C47/18
CPC分类号： C07H15/224 , C07H15/23 , C07H15/234 , Y02P20/55
摘要： Epoxides of pseudodisaccharides such as neamine, paromamine and the like are prepared. These compounds are useful intermediates to prepare other pseudodisaccharides which have antibacterial activity.
摘要翻译：制备假二糖的环氧化物，如neamine，paromamine等。这些化合物是制备具有抗菌活性的其它假二糖的有用中间体。

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