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11. 再颁专利

USRE29558E Lincomycin analogs 失效
标题翻译：林可霉素类似物
公开(公告)号：USRE29558E
公开(公告)日：1978-02-28
申请号：US730835
申请日：1976-10-08
申请人： Brian Bannister
发明人： Brian Bannister
IPC分类号： C07H5/02 , C07D327/04 , C07D327/06 , C07H3/02 , C07H5/08 , C07H15/16
CPC分类号： C07H15/16 , C07D327/04 , C07D327/06 , Y02P20/55
摘要： Compounds of the formula: ##STR1## are disclosed, wherein R.sub.1 taken independently is hydrogen; R.sub.2 taken independently is the moiety ##STR2## wherein Ac is carboxacyl or an acyl group of formula: ##STR3## wherein Z is hydrogen, lower alkyl or a protective group removable by hydrogenolysis; R.sub.5 is lower alkyl; R.sub.1 and R.sub.2 when together are the divalent group; ##STR4## wherein Z and R.sub.5 are as defined above; R.sub.3 is hydrogen when R.sub.1 and R.sub.2 are taken together and is a monovalent thio group of formula: ##STR5## located in the 7(S)-position when R.sub.1 and R.sub.2 are taken independently, A represents hydrogen or hydroxyl, B represents hydrogen or hydroxyalkyl, n is the integer 0 when B is hydroxyalkyl and n is an integer of 0 to 1, inclusive, when B is hydrogen, X is oxygen .[.or sulfur.]., D is the acyl radical of a lower hydrocarbon carboxylic acid; R.sub.4 is lower alkyl and Y is carboxacyl or hydrogen.Disclosed also are methods of making and using the novel compounds of the invention, which are useful intermediates in the chemical synthesis of useful antibacterial lincomycin analogs. Certain of the compounds of the invention are also active as antibacterial agents.

12. 发明授权

US3870699A Lincomycin analogs 失效
标题翻译：林可霉素类似物
公开(公告)号：US3870699A
公开(公告)日：1975-03-11
申请号：US33845973
申请日：1973-03-06
申请人： UPJOHN CO
发明人： BANNISTER BRIAN
IPC分类号： C07H5/02 , C07D327/04 , C07D327/06 , C07H3/02 , C07H5/08 , C07H15/16 , C07C47/18
CPC分类号： C07H15/16 , C07D327/04 , C07D327/06 , Y02P20/55
摘要： LOCATED IN THE 7(S)-position when R1 and R2 are taken independently, A represents hydrogen or hydroxyl, B represents hydrogen or hydroxyalkyl, n is the integer 0 when B is hydroxyalkyl and n is an integer of 0 to 1, inclusive, when B is hydrogen, X is oxygen or sulfur, D is the acyl radical of a lower hydrocarbon carboxylic acid; R4 is lower alkyl and Y is carboxacyl or hydrogen. Disclosed also are methods of making and using the novel compounds of the invention, which are useful intermediates in the chemical synthesis of useful antibacterial lincomycin analogs. Certain of the compounds of the invention are also active as antibacterial agents.

WHEREIN Z and R5 are as defined above; R3 is hydrogen when R1 and R2 are taken together and is a monovalent thio group of formula:

WHEREIN Z is hydrogen, lower alkyl or a protective group removable by hydrogenolysis; R5 is lower alkyl; R1 and R2 when together are the divalent group;

WHEREIN Ac is carboxacyl or an acyl group of formula:

ARE DISCLOSED, WHEREIN R1 taken independently is hydrogen; R2 taken independently is the moiety

Compounds of the formula:
摘要翻译：下式的化合物：

13. 发明授权

US09255119B2 Process for perparing fondaparinux sodium and intermediates useful in the synthesis thereof 有权
标题翻译：磺草肝素钠和中间体的合成方法
公开(公告)号：US09255119B2
公开(公告)日：2016-02-09
申请号：US14256235
申请日：2014-04-18
申请人： Reliable Biopharmaceutical Corporation
发明人： Sourena Nadji , James T. Smoot , Joseph A. Vanartsdalen
IPC分类号： C07H15/00 , C07G3/00 , C07H17/00 , C07H1/00 , C07H5/08 , C07H5/10 , C07H5/04 , A61K31/737 , C07H13/04 , C08B37/00 , C07H5/06 , C07H19/01
CPC分类号： C07H1/00 , A61K31/737 , C07H5/04 , C07H5/06 , C07H5/08 , C07H5/10 , C07H13/04 , C07H19/01 , C08B37/0063 , A61K2300/00
摘要： Processes for the synthesis of the Factor Xa anticoagulent Fondaparinux, and related compounds are described. Also described are protected pentasaccharide intermediates as well as efficient and scalable processes for the industrial scale production of Fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions.
摘要翻译：描述了因子Xa抗凝血药磺达肝素合成的方法及相关化合物。还描述了受保护的五糖中间体以及通过经过脱保护和磺化反应的顺序转化受保护的五糖中间体的，用于工业规模生产磺达肝素钠的有效和可扩展的方法。

14. 发明授权

US6040433A Sulfinyl hexose derivatives useful for glycosylation 失效
标题翻译：用于糖基化的亚磺酰基己糖衍生物
公开(公告)号：US6040433A
公开(公告)日：2000-03-21
申请号：US822131
申请日：1997-03-21
申请人： Daniel E. Kahne , Lin Yan
发明人： Daniel E. Kahne , Lin Yan
IPC分类号： C07H1/00 , C07H5/08 , C07H15/14 , C07H15/203 , C07G3/00
CPC分类号： C07H15/14 , C07H5/08
摘要： Hexose derivatives are described which facilitate control over the stereochemistry of the glycosyl bond formed in the course of a solid phase glycosylation reaction. Methods for their use are also described.
摘要翻译：描述了己糖衍生物，其有助于控制在固相糖基化反应过程中形成的糖基键的立体化学。还描述了它们的使用方法。

15. 发明授权

US5473063A Synthesis of furanosyl compounds useful as intermediates in preparation of nucleoside analogues 失效
标题翻译：用作核苷类似物制备中间体的呋喃糖基化合物的合成
公开(公告)号：US5473063A
公开(公告)日：1995-12-05
申请号：US030168
申请日：1993-05-20
申请人： Bjorn O. Classon , Bengt B. Samuelsson , Imgemar S. Kvarnstrom , Lars G. Svansson , Stefan C. T. Svensson
发明人： Bjorn O. Classon , Bengt B. Samuelsson , Imgemar S. Kvarnstrom , Lars G. Svansson , Stefan C. T. Svensson
IPC分类号： A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P33/10 , C07D239/46 , C07D405/04 , C07D473/00 , C07D473/02 , C07F9/6512 , C07F9/6558 , C07F9/6561 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H3/02 , C07H5/08
CPC分类号： A61K31/70 , A61K31/505 , A61K31/52 , C07D405/04 , C07D473/00 , C07F9/65121 , C07F9/65586 , C07F9/65616 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要： Compounds of formulae ##STR1## wherein X is O;R.sup.1 is OH, phosphate, diphosphate, triphosphate or (CH.sub.2).sub.n --O--CH.sub.2 --O--P(.dbd.O)(OH).sub.2 wherein n is 0-2;R.sup.2 is H and R.sup.3 is CH.sub.3, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 SH, CH.sub.2 F or CH.sub.2 N.sub.3 ; orR3 is H and R.sup.2 is CH.sub.3, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 SH, CH.sub.2 F or CH.sub.2 N.sub.3 ;and Z is Cl, Br, I, acyloxy or alkoxy;are synthesized from acyclic intermediates and are subsequently useful in the preparation of nucleoside analogues with antiviral activity against retroviruses such as HIV and hepatitis B.
摘要翻译： PCT No.PCT / SE91 / 00653 Sec。 371日期：1993年5月20日 102（e）日期1993年5月30日PCT 1991年9月27日PCT PCT。公开号WO92 / 06102 日期：1992年4月16日。公式或的化合物，其中X为O; R1是OH，磷酸酯，二磷酸酯，三磷酸酯或（CH2）n-O-CH2-O-P（= O）（OH）2，其中n是0-2; R2是H，R3是CH3，CH2OH，CH2-O-CH3，CH2SH，CH2F或CH2N3; 或R 3为H且R 2为CH 3，CH 2 OH，CH 2 -O-CH 3，CH 2 SH，CH 2 F或CH 2 N 3; Z为Cl，Br，I，酰氧基或烷氧基; 由无环中间体合成，随后可用于制备具有针对逆转录病毒如HIV和乙型肝炎的抗病毒活性的核苷类似物。

16. 发明授权

US4359461A Mono-, di- and tri-adamantylcarbonyl- digalactopyranosyl- glucopyranosyl- fructofuranose sulfate salts 失效
标题翻译：单 - ，二 - 和三 - 金刚烷基 - 半乳糖吡喃糖基 - 吡喃葡萄糖基 - 呋喃果糖硫酸盐
公开(公告)号：US4359461A
公开(公告)日：1982-11-16
申请号：US315789
申请日：1981-10-28
申请人： Vijay G. Nair , Seymour Bernstein
发明人： Vijay G. Nair , Seymour Bernstein
IPC分类号： A61K31/70 , A61K31/715 , A61K31/73 , C07H5/08
CPC分类号： A61K31/70
摘要： Mono-, di- and tri-adamantylcarbonyl- digalactopyranosyl- glucopyranosyl- fructofuranose sulfate salts, useful as complement inhibitors and the process of making such compounds.
摘要翻译：可用作补体抑制剂的单 - ，二 - 和三 - 金刚烷基 - 半乳糖吡喃葡萄糖 - 吡喃葡萄糖 - 呋喃果糖硫酸盐，以及制备此类化合物的方法。

17. 发明授权

US4278789A Lincomycin compounds 失效
标题翻译：林可霉素化合物
公开(公告)号：US4278789A
公开(公告)日：1981-07-14
申请号：US148056
申请日：1980-05-19
申请人： Robert D. Birkenmeyer
发明人： Robert D. Birkenmeyer
IPC分类号： C07H5/08 , A61K31/395 , A61K31/44 , A61K31/445 , A61K31/452 , A61K31/55 , A61K31/7064 , A61P31/04 , C07H15/06 , C07H15/16 , C07H15/26 , C08J3/24 , C08J9/06 , C08J9/10 , C08L25/06 , C08L25/08
CPC分类号： C07H15/16
摘要： Novel useful analogs of the well known antibiotics lincomycin and clindamycin. These analogs are prepared by condensing a cyclic acid with a sugar amine.
摘要翻译：公知的抗生素林可霉素和克林霉素的新型有用类似物。这些类似物通过将环状酸与糖胺缩合来制备。

18. 发明授权

US4228274A 1-Substituted glycopyranosides 失效
标题翻译： 1-取代的吡喃糖苷
公开(公告)号：US4228274A
公开(公告)日：1980-10-14
申请号：US922897
申请日：1978-07-10
申请人： Mitree M. Ponpipom , Robert L. Bugianesi , Philippe L. Durette , Howard M. Katzen , Tsung-Ying Shen
发明人： Mitree M. Ponpipom , Robert L. Bugianesi , Philippe L. Durette , Howard M. Katzen , Tsung-Ying Shen
IPC分类号： C07H13/04 , C07H15/04 , C07H15/14 , C07H5/06 , C07H5/08
CPC分类号： C07H13/04 , C07H15/04 , C07H15/14
摘要： The invention disclosed herein relates to novel 1-deoxy-glycopyranosides, preferably 1-deoxy-D-mannopyranosides, having in the 1-position of the pyranoside ring an .omega.-aminoalkylthio, .omega.-aminoalkyloxy or .omega.-aminoalkanoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxy-glycopyranosides starting with the corresponding tetra-O-acetyl-glycopyranosyl bromide or amine. These .omega.-amino(alkylthio, alkyloxy or alkanoylamino)-1-deoxy-glycopyranosides, and in particular 1-[(6'-aminohexyl)thio or oxy]-1-deoxy-D-mannopyranosides, possess insulin-like activity.
摘要翻译：本文公开的本发明涉及在吡喃糖苷环的1位具有ω-氨基烷硫基，ω-氨基烷氧基或ω-氨基烷酰基氨基取代基的1-脱氧-D-甘露吡喃糖苷类的新型1-脱氧-D-吡喃甘露糖苷，以及由相应的四-O-乙酰基 - 吡喃葡糖基溴或胺开始制备这些1-取代-1-脱氧 - 糖吡喃糖苷的新方法。这些ω-氨基（烷硫基，烷氧基或烷酰氨基）-1-脱氧 - 糖吡喃糖苷，特别是1 - [（6'-氨基己基）硫代或氧基] -1-脱氧-D-甘露吡喃糖苷类，具有胰岛素样活性。

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