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1. 发明授权

US4024333A Synthesis of daunosamine hydrochloride from a D-mannose starting material 失效
标题翻译：从D-甘露糖起始原料合成盐酸丹麦诺胺
公开(公告)号：US4024333A
公开(公告)日：1977-05-17
申请号：US698689
申请日：1976-06-22
申请人： Derek Horton , Wolfgang F. Weckerle
发明人： Derek Horton , Wolfgang F. Weckerle
IPC分类号： C07H5/06 , C07H15/04 , C07G11/00
CPC分类号： C07H5/06 , C07H15/04
摘要： A method for synthesizing daunosamine hydrochloride from methyl .alpha.-D-mannopyranoside. The major features of the preparative route involve the formation of a 2-deoxy-3-keto intermediate, whose oxime is reduced with high stereoselectivity to the D-ribo-3-amino compound, followed by a stereospecific step late in the sequence to introduce the terminal C-methyl group with inversion at C-5, to generate the required L-lyxo stereochemistry. The synthesis procedure affords daunosamine hydrochloride in 40% overall yield, with no chromatographic procedures for isolation being required in any of the steps.
摘要翻译：从α-D-吡喃半乳糖苷甲基合成盐酸丹麦诺胺的方法。制备途径的主要特征包括形成2-脱氧-3-酮中间体，其肟以高立体选择性降低至D-核糖-3-氨基化合物，随后在序列后期立体选择性步骤末端C-甲基在C-5反转，产生所需的L-lyxo立体化学。该合成方法提供了总体产率为40％的盐酸丹麦诺胺，在任何步骤中都不需要用于分离的色谱法。

2. 发明授权

US4427664A 2'Halo derivatives of daunomycin, desmethoxy daunomycin, adriamycin and carminomycin 失效
标题翻译：道诺霉素，去甲氧基柔红霉素，阿霉素和卡明霉素的2'Halo衍生物
公开(公告)号：US4427664A
公开(公告)日：1984-01-24
申请号：US408942
申请日：1982-08-17
申请人： Derek Horton , Waldemar Priebe
发明人： Derek Horton , Waldemar Priebe
IPC分类号： C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： The compounds are derived from aglycons which may be daunomycin, desmethoxy daunomycin, adriamycin and carminomycin. A preferred compound is ##STR1## (1) R'=H; R.sup.2 =OMe; X; Y (2) R'=OH; R.sup.2 =OMe; X; Y(3) R'=H; R.sup.2 =H; X; Y(4) R'=H; R.sup.2 =OH; X; YwhereX=I, Cl, Br, or F andY=OH or AcO (acetoxy)where Y is AcO or OH and R'=H and R.sup.2 =OMe.These compounds are effective showing high anti-leukemic activity against P388 murine leukemia.
摘要翻译：这些化合物衍生自可以是道诺霉素，去甲氧基柔红霉素，阿霉素和卡明霉素的糖苷。优选的化合物是（1）R'= H; R2 = OMe; X; Y（2）R'= OH; R2 = OMe; X; Y（3）R'= H; R2 = H; X; Y（4）R'= H; R2 = OH; X; Y，其中X = I，Cl，Br或F，Y = OH或AcO（乙酰氧基）（1）R'= H; R2 = OMe; X; Y（2）R'= OH; R2 = OMe; X; Y（3）R'= H; R2 = H; X; Y（4）R'= H; R2 = OH; X; 其中X = I，Cl，Br或F，Y = OH或AcO（乙酰氧基），其中Y是AcO或OH，R'= H，R2 = OMe。这些化合物对P388鼠白血病具有高抗白血病活性。

3. 发明授权

US4772688A 14-acyloxy-2'-halo-anthracycline anti-cancer antibiotics 失效
标题翻译： 14-酰氧基-2'-卤 - 蒽环类抗癌抗生素
公开(公告)号：US4772688A
公开(公告)日：1988-09-20
申请号：US42624
申请日：1987-04-23
申请人： Derek Horton , Waldemar Priebe , Richard L. Wolgemuth
发明人： Derek Horton , Waldemar Priebe , Richard L. Wolgemuth
IPC分类号： C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Compounds of the formula (I) and pharmaceutical preparations containing the same are disclosed ##STR1## wherein R.sup.1 is --OOCR.sup.3 or --OOC(CH.sub.2).sub.n COOR.sup.4 ; R.sup.2 is hydrogen, hydroxy or methoxy; one of X and X' is a halogen atom selected from the group consisting of fluorine, chlorine, bromine and iodine and the other is hydrogen; one of Y and Y' is hydrogen and the other is selected from the group consisting of hydrogen, hydroxy and acyloxy; one of Z and Z' is hydrogen and the other is selected from the group consisting of hydrogen, hydroxy and acyloxy; R.sup.3 is an alkyl group containing 1 to 8 carbon atoms; R.sup.4 is a hydrogen atom, a metal atom, or an alkyl group containing 1 to 4 carbon atoms; and n is an integer of 0 to 6. These compounds are active in the inhibition of malignant diseases.
摘要翻译：公开了式（I）化合物和含有该化合物的药物制剂，其中R 1是-OOCR 3或-OOC（CH 2）n COOR 4; R2是氢，羟基或甲氧基; X和X'之一是选自氟，氯，溴和碘的卤素原子，另一个是氢; Y和Y'之一是氢，另一个选自氢，羟基和酰氧基; Z和Z'之一是氢，另一个选自氢，羟基和酰氧基; R3是含有1至8个碳原子的烷基; R4是氢原子，金属原子或含有1至4个碳原子的烷基; n为0〜6的整数。这些化合物在恶性疾病的抑制中具有活性。

4. 发明授权

US4870058A 14-Acyloxy-2'-halo-anthracycline anti-cancer antibiotics 失效
标题翻译： 14-Acyloxy-2-halo-anthracycline抗癌抗生素
公开(公告)号：US4870058A
公开(公告)日：1989-09-26
申请号：US151755
申请日：1988-02-03
申请人： Derek Horton , Waldemar Priebe
发明人： Derek Horton , Waldemar Priebe
IPC分类号： C07H15/252
CPC分类号： C07H15/252
摘要： Compounds of the formula (I) and pharmaceutical preparations containing the same are disclosed ##STR1## wherein R.sup.1 is --OOCR.sup.3 or --OOC(CH.sub.2).sub.n COOR.sup.4 ; R.sup.2 is hydrogen, hydroxy or methoxy; one of X and X' is a halogen atom selected from the group consisting of fluorine, chlorine, bromine and iodine and the other is hydrogen; one of Y and Y' is hydrogen and the other is selected from the group consisting of hydrogen, hydroxy and acyloxy; one of Z and Z' is hydrogen and the other is selected from the group consisting of hydrogen, hydroxy and acyloxy; R.sup.3 is an alkyl group containing 1 to 8 carbon atoms; R.sup.4 is a hydrogen atom, a metal atom, or an alkyl group containing 1 to 4 carbon atoms; and n is an integer of 0 to 6. These compounds are active in the inhibition of malignant diseases.
摘要翻译：公开了式（I）化合物和含有该化合物的药物制剂，其中R 1是-OOCR 3或-OOC（CH 2）n COOR 4; R2是氢，羟基或甲氧基; X和X'之一是选自氟，氯，溴和碘的卤素原子，另一个是氢; Y和Y'之一是氢，另一个选自氢，羟基和酰氧基; Z和Z'之一是氢，另一个选自氢，羟基和酰氧基; R3是含有1至8个碳原子的烷基; R4是氢原子，金属原子或含有1至4个碳原子的烷基; n为0〜6的整数。这些化合物在恶性疾病的抑制中具有活性。

5. 发明授权

US4663445A 1-fluoro, 4-fluoro, and 1,4-difluoro-2'-halo anthracycline antibiotics 失效
标题翻译： 1-氟，4-氟和1,4-二氟-2'-卤代蒽环类抗生素
公开(公告)号：US4663445A
公开(公告)日：1987-05-05
申请号：US714148
申请日：1985-03-20
申请人： John S. Swenton , Derek Horton , Waldemar Priebe , Gary W. Morrow
发明人： John S. Swenton , Derek Horton , Waldemar Priebe , Gary W. Morrow
IPC分类号： C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline antibiotics represented by the formula (I) ##STR1## wherein R is hydrogen or hydroxyl, one of X and Y is fluorine and the other is hydrogen or both X and Y are fluorine, and S is a 2-halo sugar moiety; pharmaceutical preparations containing the same; and a method for inhibiting the growth of mammalian tumors are disclosed.
摘要翻译：由式（I）表示的蒽环类抗生素其中R是氢或羟基，X和Y之一是氟，另一个是氢或X和Y都是氟，S是2-卤代糖部分; 含有该药物的药物制剂; 并且公开了抑制哺乳动物肿瘤生长的方法。

6. 发明授权

US4537882A 4-Demethoxy-3'-desamino-2'-halo-anthracycline and pharmaceutical composition containing same 失效
标题翻译： 4-脱甲氧基-3'-脱氨基-2'-卤代蒽环和含有它们的药物组合物
公开(公告)号：US4537882A
公开(公告)日：1985-08-27
申请号：US609072
申请日：1984-05-10
申请人： Derek Horton , Waldemar Priebe
发明人： Derek Horton , Waldemar Priebe
IPC分类号： C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252
摘要： Compounds of the formula (I), acid addition salts thereof, and pharmaceutical preparations containing the same are disclosed ##STR1## wherein R.sup.1 is hydroxy; one of X and X' is hydrogen and the other is a halogen atom selected from the group consisting of fluorine, chlorine, bromine, and iodine; one of Y and Y' is hydrogen and the other is selected from the group consisting of hydrogen, hydroxy and --OCOR; one of Z and Z' is hydrogen and the other is hydrogen, hydroxy or --OCOR; and R is a lower alkyl group.
摘要翻译：公开了式（I）化合物，其酸加成盐和含有其的药物制剂，其中R1是羟基; X和X'之一是氢，另一个是选自氟，氯，溴和碘的卤素原子; Y和Y'之一是氢，另一个选自氢，羟基和-OCOR; Z和Z'之一是氢，另一个是氢，羟基或-OCOR; 且R为低级烷基。

7. 发明授权

US4201773A 7-O-(2,6-Dideoxy-.alpha.-L-lyxo-hexopyranosyl)-daunomycinone, desmethoxy daunomycinone, adriamycinone, and carminomycinone 失效
标题翻译： 7-O-（2,6-二脱氧-α-L-赖索 - 六吡喃糖基） - 日光霉素酮，去甲氧基道诺霉素，阿霉素酮和卡明霉素酮
公开(公告)号：US4201773A
公开(公告)日：1980-05-06
申请号：US928252
申请日：1978-07-26
申请人： Derek Horton , Wolfgang Weckerle , Ernst F. Fuchs , Tak M. Cheung , Beat Winter , Roderick J. Sorenson
发明人： Derek Horton , Wolfgang Weckerle , Ernst F. Fuchs , Tak M. Cheung , Beat Winter , Roderick J. Sorenson
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , A61P35/02 , C07H3/02 , C07H13/04 , C07H15/04 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/04 , C07H13/04 , C07H15/252 , C07H3/02 , Y10S514/908
摘要： A series of compounds showing high antileukemic activity against P388 murine leukemia and increased aqueous solubility due to substitution of --OH for the known --NH.sub.2 at the 3' position of the hexopyranose sugar, i.e., daunosamine.These compounds are coupled products of aglycon selected from daunomycinone, desmethoxy daunomycinone, adriamycinone and carminomycinone. These compounds are coupled at the 0-7 position of the aglycon with an .alpha.-L-lyxo hexopyranose sugar, which sugar isomer particularly sustains or potentiates the biological activity of the coupled compound as well as ameliorates the dose related cardiotoxicity of the parent and known compounds set out below: ##STR1##
摘要翻译：一系列化合物对P388鼠白血病显示出高抗白血病活性，并且由于在六吡喃糖糖的3'位置即daunosamine上取代-OH已知的-NH 2而增加水溶性。这些化合物是选自道诺霉素酮，去甲氧基道诺霉素酮，阿霉素酮和卡明霉素酮的糖苷配基的偶联产物。这些化合物在糖苷配基的0-7位与α-L-赖索倍半吡糖糖偶联，所述糖异构体特别维持或增强偶联化合物的生物活性，并且改善了母体的剂量相关的心脏毒性和已知的化合物如下：

8. 发明授权

US4562177A 3'-Amino-2' halo-anthracycline antibiotics 失效
标题翻译： 3'-氨基-2'卤代蒽环类抗生素
公开(公告)号：US4562177A
公开(公告)日：1985-12-31
申请号：US487841
申请日：1983-04-22
申请人： Derek Horton , Waldemar A. Priebe
发明人： Derek Horton , Waldemar A. Priebe
IPC分类号： C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a hydroxyl group; R.sup.2 is a hydrogen atom or a hydroxyl or methoxyl group; X is a fluorine, chlorine, bromine or iodine atom; one of Y and Y' is a hydrogen atom and the other is a hydrogen atom or a hydroxyl or acyloxy group; R.sup.3 and R.sup.4 are each independently a hydrogen atom, an alkyl group, a halo- or phenyl-substituted alkyl group, an acyl group or a halo- or phenyl-substituted acyl group or R.sup.3 and R.sup.4 together form a polymethylene chain having 4 to 6 carbon atoms, are useful as anti-tumor agents, especially for treating leukemia; in particular these compounds exhibit high antileukemic activity against P388 murine leukemia.
摘要翻译：其中R1是氢原子或羟基的式“IMAGE”的化合物; R2是氢原子或羟基或甲氧基; X是氟，氯，溴或碘原子; Y和Y'之一是氢原子，另一个是氢原子或羟基或酰氧基; R 3和R 4各自独立地为氢原子，烷基，卤代或苯基取代的烷基，酰基或卤代或苯基取代的酰基，或者R 3和R 4一起形成具有4至6个碳原子可用作抗肿瘤剂，特别是用于治疗白血病; 特别是这些化合物对P388鼠白血病具有高抗白血病活性。

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