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71. 发明授权

US4472573A Nitrosourea derivative and process for preparing same 失效
标题翻译：亚硝基脲衍生物及其制备方法
公开(公告)号：US4472573A
公开(公告)日：1984-09-18
申请号：US358818
申请日：1982-03-16
申请人： Tamio Morikawa , Kenji Tsujihara , Mikio Takeda , Yoshihisa Arai
发明人： Tamio Morikawa , Kenji Tsujihara , Mikio Takeda , Yoshihisa Arai
IPC分类号： C07H15/04 , A61K31/70 , A61K31/7028 , A61P35/00 , A61P35/02 , C07H13/12 , C07H15/12 , C07H11/02
CPC分类号： C07H13/12
摘要： A nitrosourea compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl and R.sup.2 is lower alkyl or lower alkoxy-lower alkyl, which may be prepared by nitrosation of a compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are the same as defined above. Said nitrosourea compound is useful as an anti-tumor or anti-leukemic agent.
摘要翻译：一种下式的亚硝基脲化合物：其中R1是低级烷基，R2是低级烷基或低级烷氧基 - 低级烷基，其可以通过亚化下式化合物制备：其中R1和R2相同如上所述。所述的亚硝基脲化合物可用作抗肿瘤或抗白血病药。

72. 发明授权

US4431636A Bis(4-O-polyhexaose-thio)-phenyl ureas and method of use 失效
标题翻译：双（4-O-聚己糖 - 硫代） - 苯基脲和使用方法
公开(公告)号：US4431636A
公开(公告)日：1984-02-14
申请号：US380986
申请日：1982-05-24
申请人： Robert E. Schaub , Janis Upeslacis , Seymour Bernstein
发明人： Robert E. Schaub , Janis Upeslacis , Seymour Bernstein
IPC分类号： C07H3/04 , C07H5/04 , A61K31/72 , C07H13/12
CPC分类号： C07H3/04 , C07H5/04 , Y10S514/825 , Y10S514/885
摘要： Poly-cation salts of bis (4-O-polyhexaose-thio)-phenyl urea sulfate derivatives, useful as modulators of the complement system, the intermediates thereof and the process of making such intermediates and end products.
摘要翻译：双（4-O-聚己糖 - 硫） - 苯基尿素硫酸盐衍生物的多阳离子盐，可用作补体系统的调节剂，其中间体以及制备此类中间体和终产物的方法。

73. 发明授权

US4362721A Penicillanic and cephalosporanic derivatives, preparation thereof, and pharmaceutical compositions containing same 失效
标题翻译：青霉烷和头孢菌素衍生物，其制备物和含有它们的药物组合物
公开(公告)号：US4362721A
公开(公告)日：1982-12-07
申请号：US327058
申请日：1981-12-03
申请人： Giorgio Ferrari , Vittorio Vecchietti
发明人： Giorgio Ferrari , Vittorio Vecchietti
IPC分类号： A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D499/00 , C07D499/68 , C07D501/22 , C07D519/06 , C07H13/12 , A61K31/70 , C07H15/26
CPC分类号： C07H13/12 , C07D499/00
摘要： There are disclosed penicillanic and cephalosporanic derivatives of the formula: ##STR1## wherein R is H or --OH; R.sub.1 is a carbohydrate hexose radical of 3-O-glucose, 6-O-galactose, 3-O-glucose acetals, 3-O-glucose ketals, 6-O-galactose acetals, and 6-O-galactose ketals, and R.sub.2 is: ##STR2## where R.sub.3 is H or an alkali or alkaline-earth metal. The preparation of the derivatives and pharmaceutical compositions containing same are also disclosed.A process according to the invention comprises reacting a compound of the formula ##STR3## with a hexose carbohydrate, in --OH protected form, in an aqueous medium, in the presence of a water-miscible organic solvent, in the presence of a base, the reaction product being optionally transformed into the derivative wherein R.sub.1 is a carbohydrate in the unprotected form by treatment with Lewis' acid or a hydrogen halide acid.The compounds according to the invention are used in pharmaceutical compositions useful for treatment of infections by gram-positive and gram-negative pathogenous bacteria.
摘要翻译：公开了下式的青霉素和头孢菌素衍生物：其中R是H或-OH;（I）其中R是H或-OH; R1是3-O-葡萄糖，6-O-半乳糖，3-O-葡萄糖缩醛，3-O-葡萄糖缩酮，6-O-半乳糖缩醛和6-O-半乳糖缩酮的碳水化合物己糖基，R2 是： + TR 其中R3是H或碱金属或碱土金属。还公开了含有它们的衍生物和药物组合物的制备。根据本发明的方法包括在水溶性有机溶剂的存在下，在碱的存在下，使式IMA的化合物与-OH保护形式的己糖碳水化合物在水性介质中反应，反应产物任选地转化为衍生物，其中R1是未保护形式的碳水化合物，用路易斯酸或卤化氢酸处理。根据本发明的化合物用于治疗革兰氏阳性和革兰氏阴性病原菌感染的药物组合物中。

74. 发明授权

US4349546A D-Allose derivative and preparation method therefor 失效
标题翻译： D-赖氨酸衍生物及其制备方法
公开(公告)号：US4349546A
公开(公告)日：1982-09-14
申请号：US245920
申请日：1981-03-20
申请人： Masahide Yamada , Kenichi Edanami , Toshio Kuroda
发明人： Masahide Yamada , Kenichi Edanami , Toshio Kuroda
IPC分类号： A61K31/70 , A61K31/7024 , A61P35/00 , C07H13/12 , C08B37/00
CPC分类号： C07H13/12 , Y02P20/55 , Y10S514/908
摘要： 3-[3-(2-Haloethyl)-3-nitrosoureido]-3-deoxy-D-alloses are new, antitumor compounds having a far lower myelotoxicity as compared with conventional antitumor agents. They are obtained by treating 3-[3-(2-haloethyl)ureido]-3-deoxy-1,2,5,6,-di-O-isopropylidene-.alpha.-D-allofuranoses with a nitrosating agent and then hydrolyzing the protective group in the presence of an acid.
摘要翻译： 3- [3-（2-卤代乙基）-3-亚硝基脲基] -3-脱氧-D-同位素是与常规抗肿瘤剂相比具有远低于骨髓毒性的新型抗肿瘤化合物。它们是通过用亚硝化剂处理3- [3-（2-卤代乙基）脲基] -3-脱氧-1,2,5,6， - 二-O-异亚丙基-α-异构呋喃虫糖，然后水解保护基团在存在酸的情况下。

75. 发明授权

US4334058A Rutin poly(H--)sulfate salts and related compounds 失效
标题翻译：芦丁聚（H-）硫酸盐和相关化合物
公开(公告)号：US4334058A
公开(公告)日：1982-06-08
申请号：US181251
申请日：1980-08-25
申请人： Vijay G. Nair , Seymour Bernstein
发明人： Vijay G. Nair , Seymour Bernstein
IPC分类号： C07H1/00 , C07H17/07 , A61K31/70 , C07H11/00 , C07H13/12
CPC分类号： C07H17/07 , Y10S514/834
摘要： Rutin poly(H--)sulfate and salts thereof useful as complement inhibitors.
摘要翻译： Rutin聚（H-）硫酸盐及其盐可用作补体抑制剂。

76. 发明授权

US4266025A Production of N-substituted derivatives of 1-desoxy-nojirimycin 失效
标题翻译： 1-脱氧 - nojirimycin的N-取代衍生物的制备
公开(公告)号：US4266025A
公开(公告)日：1981-05-05
申请号：US97099
申请日：1979-11-23
申请人： Gunther Kinast , Michael Schedel
发明人： Gunther Kinast , Michael Schedel
IPC分类号： C12P17/12 , C07C271/16 , C07D211/46 , C07H13/12 , C12P19/26 , C12P19/44 , C12R1/01 , C12R1/15 , C12R1/645
CPC分类号： C07H13/12 , C07C271/16 , C07D211/46 , C12P19/26
摘要： The invention relates to a process for the production of compounds of the formula ##STR1## in which R is hydrogen or optionally substituted alkyl, alkenyl, aralkyl or aryl, by microbiological transformation of ##STR2## follow by catalytic hydrogenation. The compounds obtained are useful for the treatment of diabetes, hyperlipoproteinaemia and adiposity which comprises aerobically cultivates, in the presence of an assimilable source of carbon nitrogen, at a temperature of 20.degree. to 45.degree. C. and pH between 2 and 10 and in the presence of an effective amount of a compound of the formula ##STR3## in which R has the above-given meaning and,R.sub.1 denotes an optionally substituted benzyl radical or an optionally substituted .beta.-alkenyl group,an aerobic microorganism or an extract of aerobic microorganism capable, in a nutrient medium containing a compound of the formula (X), or accumulating an amount of a compound of the formula ##STR4## in which R and R.sub.1 have the above-mentioned meanings andsubjecting the resulting compound of the general formula XI to catalytic hydrogenation.
摘要翻译：本发明涉及通过催化氢化随后的微生物转化制备式（I）化合物的方法，其中R是氢或任选取代的烷基，烯基，芳烷基或芳基。。所获得的化合物可用于治疗糖尿病，高脂蛋白血症和肥胖，其包括在可同化的碳氮源的存在下，在20°至45℃的温度和2至10之间的pH下进行有氧培养，并且在存在有效量的式（X）化合物，其中R具有上述含义，R 1表示任选取代的苄基或任选取代的β-链烯基，需氧微生物或提取物在含有式（X）化合物的营养培养基中，或者累积一定量的式（XI）化合物，其中R和R 1具有上述含义，并使所得的通式XI的化合物进行催化氢化。

77. 发明授权

US4241053A Novel nitrosourea compounds and process for preparing the same 失效
标题翻译：新型亚硝基脲类化合物及其制备方法
公开(公告)号：US4241053A
公开(公告)日：1980-12-23
申请号：US66421
申请日：1979-08-14
申请人： Kenji Tsujihara , Masakatsu Ozeki , Yoshihisa Arai
发明人： Kenji Tsujihara , Masakatsu Ozeki , Yoshihisa Arai
IPC分类号： C07H13/12 , A61K31/70 , A61K31/73
CPC分类号： C07H13/12
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is lower alkoxy, lower alkoxy-methoxy or 2-hydroxy-ethoxy, R.sup.2 is aldo-pentofuranosyl, aldo-pentopyranosyl, aldohexopyranosyl or O-aldo-hexopyranosyl-(1.fwdarw.4)-aldo-hexopyranosyl, and A is straight or branched alkylene of one to four carbon atoms, said alkylene being substituted with from 0 to at least one lower alkoxy group, is disclosed. A new intermediate used in the preparation of this compound is also disclosed. The end products are useful for inhibiting the growth of malignant tumor cells in warm-blooded animals; especially Leukemia and Ejrlich ascites carcinoma. Effectiveness on human beings has not yet been demonstrated.
摘要翻译：下式的化合物，其中R 1是低级烷氧基，低级烷氧基 - 甲氧基或2-羟基 - 乙氧基，R 2是氢 - 戊呋喃糖基，醛 - 吡喃葡萄糖基，羟基六吡喃糖基或O-羟基 - 六吡喃糖基 - （1-> 4） - 六氢吡喃糖基，A是1-4个碳原子的直链或支链亚烷基，所述亚烷基被0至至少一个低级烷氧基取代。还公开了用于制备该化合物的新中间体。最终产品可用于抑制温血动物中恶性肿瘤细胞的生长; 尤其是白血病和Ejrlich腹水癌。对人类的有效性尚未得到证实。

78. 发明授权

US4123607A Alkylated derivatives of antibiotic BM123.gamma. 失效
标题翻译：抗生素BM123的烷基化衍生物{65
公开(公告)号：US4123607A
公开(公告)日：1978-10-31
申请号：US801898
申请日：1977-05-31
申请人： Joseph J. Hlavka , Panayota Bitha
发明人： Joseph J. Hlavka , Panayota Bitha
IPC分类号： C07H15/203 , C07H13/12
CPC分类号： C07H15/203
摘要： This disclosure describes a novel series of potent antibacterial agents derived by reductive alkylation of antibiotic BM123.gamma. with certain classes of aldehydes and ketones.
摘要翻译：本公开描述了通过用某些类别的醛和酮将抗生素BM123γ还原烷基化衍生的一系列有效的抗菌剂。

79. 发明授权

US4120954A 2,2',2"-[S-Phenenyltris(carbonylimino) ]tris-2-deoxy-D-glucopyranose and salts thereof 失效
标题翻译： 2,2 {40,2 {41- {8-苯基苯基三（羰基亚氨基）{9三-2-脱氧-D-吡喃葡萄糖及其盐
公开(公告)号：US4120954A
公开(公告)日：1978-10-17
申请号：US784202
申请日：1977-04-04
申请人： Joseph Peter Joseph , Seymour Bernstein
发明人： Joseph Peter Joseph , Seymour Bernstein
IPC分类号： C07H13/00 , C07H13/08 , C07H13/12 , A61K31/70
CPC分类号： C07H13/08 , C07H13/00 , C07H13/12
摘要： 2,2',2"-[s-Phenenyltris(carbonylimino)]tris-2-deoxy-D-glucopyranose and salts thereof, useful as complement inhibitors.
摘要翻译： 2,2'，2“ - [s-苯基三（羰基亚氨基）]三-2-脱氧-D-吡喃葡萄糖及其盐，可用作补体抑制剂。

80. 发明授权

US4096250A Tri-substituted phosphinegold(I) 1-thio-.beta.-D-glucopyranosides 失效
标题翻译：三取代磷腈金（I）1-硫代 - {62 -D-吡喃葡萄糖苷
公开(公告)号：US4096250A
公开(公告)日：1978-06-20
申请号：US772035
申请日：1977-02-25
申请人： David T. Hill
发明人： David T. Hill
IPC分类号： A61K31/70 , A61K31/7135 , A61P29/00 , C07F1/00 , C07H15/04 , C07H15/14 , C07H15/18 , C07H23/00 , C07H11/04 , C07H13/12
CPC分类号： C07H15/04 , C07F1/00 , C07H15/14 , C07H15/18 , C07H23/00 , Y10S514/825
摘要： The compounds are tri-substituted phosphinegold(I) 1-thio-.beta.-D-glucopyranosides which have antiarthritic activity and, in particular, are of use in the treatment of rheumatoid arthritis. Of the three substituents on the phosphine one is optionally substituted phenyl and the others are lower alkyl or lower alkoxy.
摘要翻译：这些化合物是具有抗关节炎活性的三取代膦酸（I）1-硫代-β-D-吡喃葡萄糖苷，特别是用于治疗类风湿性关节炎。在膦上的三个取代基之一是任选取代的苯基，而其它取代基是低级烷基或低级烷氧基。

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