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1. 发明授权

US3664998A Process for converting peracylated cis-glycosy halides to peracylated trans-glycosyl halides and novel compounds 失效
标题翻译：将熟化的独联体糖蛋白转化为过氧化物转化糖蛋白和新化合物的方法
公开(公告)号：US3664998A
公开(公告)日：1972-05-23
申请号：US3664998D
申请日：1969-11-03
申请人： UPJOHN CO
发明人： BANNISTER BRIAN
IPC分类号： A61K31/70 , A61P31/04 , C07H9/04 , C07H13/04 , C07H15/16 , C07C47/18
CPC分类号： C07H9/04 , C07H13/04 , C07H15/16
摘要： A peracylated cis-glycosyl halide is converted to the corresponding isothiouronium halide. The latter is decomposed to the corresponding mercaptan ( Beta -anomer) which is concomitantly alkylated to the corresponding 1-thioglycoside. The latter is then converted to the trans-glycosyl halide by the reaction of halogen in an inert solvent. 6-Acylamino-6-deoxy2,3,4-tri-0-acyl- Alpha -D-galactopyranosyl bromide is in this way converted to the Beta -anomer. The Beta -anomer is then converted to the 1-thio- Alpha glycoside by the thiourea process using a tertiary base dipolar aprotic solvent, the resulting 1-thio- Alpha -glycoside deacylated, and the amino group reacylated to form antibacterially active 7,8-bisnorlincomycin or analog thereof.

2. 发明授权

US3574187A Process for making alkyl 7-o-alkyl-1-thio-alpha-lincosaminides and products thereof 失效
标题翻译：制备亚基7-O-烷基-1-硫代 - 氨基亚磺酰胺及其制品的方法
公开(公告)号：US3574187A
公开(公告)日：1971-04-06
申请号：US3574187D
申请日：1969-11-03
申请人： UPJOHN CO
发明人： BANNISTER BRIAN
IPC分类号： C07H9/04 , C07H15/16 , C07C47/18
CPC分类号： C07H9/04 , C07H15/16
摘要： ALKYL 7-O-ALKYL-1-THIO-A-LINCOSAMINIDES USEFUL AS INTERMEDIATES FOR PREPARING ANTIBACTERIALLY ACTIVE 7-O-ALKYLLINCOMYCINS ARE PREPARED BY CONVERTING 2''-HYDROXYETHYL 7-O-METHYL-1-THIO-A-LINCOSAMINIDE TO THE CORRESPONDING 1-BROMO SUGAR THEN REPLACING THE BROMO GROUP BY AN ALKYL MERCAPTO GROUP WHILE TH 2-,3-, AND 4-HYDROXYL GROUPS AND THE 6-AMINO GROUP ARE COVERED BY PROTECTIVE GROUPS, AND THEN REMOVING THE PROTECTIVE GROUPS; OR BY ACYLATIG AN ALKYL 6-N,7-O-ETHYLIDYNE-3,4-O-ISOPROPYLIDENE-1-THIO-A-LINCOSAMINIDE TO FORM THE 2-ACYLATE THEREOF, HYDROLYZING THE 6-N,7-O-ETHYLIDYNE GROUPING TO FORM ALKYL 2-O-ACYL-6-N-ACETYL-3,4-O-ISOPROPYLIDENE-1-THIO-ATHIOLINCOSAMINIDE, ALKYLATING THE 7-HYDROXY GROUP TO FORM ALKYL N-ACETYL-7-O-ALKYL-1-THIO-A-LINCOSAMINIDE, AND REMOVING THE N-ACETYL GROUP BY HYDRAZINOLYSIS AND THE 3,4ISOPROPYLIDENE GROUP BY HYDROLYSIS TO FORM THE DESIRED ALKYL 7-O-ALKYL-1-THIO-A-LINCOSAMINIDE.

3. 发明授权

US3907643A Process for producing the antibiotic U-44,590 失效
标题翻译：生产抗生素U-44,590的方法
公开(公告)号：US3907643A
公开(公告)日：1975-09-23
申请号：US54134675
申请日：1975-01-15
申请人： UPJOHN CO
发明人： DEBOER CLARENCE , BANNISTER BRIAN
IPC分类号： C07H19/12 , C12D9/00
CPC分类号： C07H19/12 , Y10S435/852 , Y10S435/903
摘要： New antibiotic U-44,590 and derivatives thereof, produced by the controlled fermentation of the new microorganism Streptomyces platensis var. clarensis var nova, NRRL 8035. This antibiotic and its derivatives are active against Gram-negative bacteria. Accordingly, they can be used in various environments to eradicate or control such bacteria.
摘要翻译：新型抗生素U-44,590及其衍生物，通过新型微生物链霉菌Streptomyces platensis var。这种抗生素及其衍生物对革兰氏阴性菌具有活性。因此，它们可以用于各种环境中以消除或控制这些细菌。

4. 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：

5. 发明授权

US3705889A Lincomycin analogs and process 失效
标题翻译： LINCOMYCIN模拟和过程
公开(公告)号：US3705889A
公开(公告)日：1972-12-12
申请号：US3705889D
申请日：1970-04-28
申请人： UPJOHN CO
发明人： BANNISTER BRIAN , MAGERLEIN BARNEY J
IPC分类号： C07H15/16 , C07C47/18
CPC分类号： C07H15/16
摘要： THE ANTIBIOTIC 7-O-(LOWER-ALKYL)-8-NORLINCOMYCIN AND ITS S-ANALOGS ARE PREPARED BY ALKYLATING 8-NORLINCOMYCIN AND ITS S-ANALOGS OR BY ACYLATING LOWER-ALKYL 7-O-(LOWERALKYL)-8-NOR-A-THIOLINCOSAMINIDE. NOVEL INTERMEDIATES INCLUDE LOWER-ALKYL N-ACETYL-8-NOR-A-THIOLINCOSAMINIDE; 6-DEAMINO-6-NITRO-8-NOR-A-THIOLINCOSAMINIDE, ITS PERACYLATE AND ITS 7-O-(LOWER-ALKYL) DERIVATIVES; AND LOWER-ALKYL 6-DEOXY-6-METHYLENE-6-NITRO-1-THIO-A-DGALACTOPYRANOSIDE PERACYLATE.

6. 发明授权

US3702322A Derivatives of lincomycin and its analogs and process 失效
标题翻译： LINCOMYCIN的衍生物及其类似物和方法
公开(公告)号：US3702322A
公开(公告)日：1972-11-07
申请号：US3702322D
申请日：1970-04-06
申请人： UPJOHN CO
发明人： BANNISTER BRIAN
IPC分类号： C07H15/16 , C08G18/38 , C07C47/18
CPC分类号： C08G18/3868 , C07H15/16
摘要： ALKYL 7-DEOXY-7(S)-OR-A-THIOLINCOSAMINIDES USEFUL AS INTERMEDIATES FOR PREPARING ANTIBACTERIALLY ACTIVE 7-DEOXY7(S)-OR-LINCOMYCINS ARE PREPARED BY OPENING THE AZIRIDINE RING OF ALKYL N-ACYL-6,7-ARIZIDINO-6-DEAMINO-7-DEOXYA-THIOLINCOSAMINIDES BY HYDROLYSIS OR ALCOHOLYSIS.

7. 发明授权

US3915954A Derivatives of lincomycin and its analogs and process 失效
标题翻译：林可霉素的衍生物及其类似物和方法
公开(公告)号：US3915954A
公开(公告)日：1975-10-28
申请号：US37060373
申请日：1973-06-18
申请人： UPJOHN CO
发明人： BANNISTER BRIAN
IPC分类号： C07H15/16
CPC分类号： C07H15/16
摘要： Alkyl 7-deoxy-7-RSn- Alpha -thiolincosaminides useful as intermediates for preparing antibacterially active 7-deoxy-7-RSnlincomycins are prepared by heating alkyl N-acyl-6,7-aziridino-6deamino-7-deoxy- Alpha -thiolincosaminides with an aliphatic, cycloaliphatic, or aromatic acyclic sulfide (mono, di, tri or tetrasulfide) in the presence of glacial acetic acid or other anhydrous lower alkanoic acid, or anhydrous benzoic acid or other arenoic acid of not more than 12 carbon atoms.
摘要翻译：通过加热N-酰基-6,7-氮丙啶-6-脱氨基-7-脱氧-N-烷基-7-氨基-7-氨基-3-硫代氨基甲酸N-烷基酯，可用作制备抗菌活性7-脱氧-7-RSn-线霉素的中间体7-烷氧基-7-脱氧-7-RSn- - 在冰醋酸或其他无水低级链烷酸或无水苯甲酸或其他不大于12的异烟酸存在下，使用脂族，脂环族或芳族无环硫醚（单，二，三或四硫化物）的α-硫代氨基甲酸碳原子。

8. 发明授权

US3907779A 5,6 Dihydro-5-azathymidine and derivatives 失效
标题翻译： 5,6二氢-5-氮杂胞苷及其衍生物
公开(公告)号：US3907779A
公开(公告)日：1975-09-23
申请号：US47132274
申请日：1974-05-20
申请人： UPJOHN CO
发明人： DEBOER CLARENCE , BANNISTER BRIAN
IPC分类号： C12P19/38 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61P31/04 , C07H19/12 , C12N1/20 , C12P1/06 , C12R1/585
CPC分类号： C07H19/12 , Y10S435/903
摘要： New antibiotic U-44,590 and derivatives thereof, produced by the controlled fermentation of the new microorganism Streptomyces platensis var. clarensis var nova, NRRL 8035. This antibiotic and its derivatives are active against Gram-negative bacteria. Accordingly, they can be used in various environments to eradicate or control such bacteria.
摘要翻译：新型抗生素U-44,590及其衍生物，通过新型微生物链霉菌Streptomyces platensis var。这种抗生素及其衍生物对革兰氏阴性菌具有活性。因此，它们可以用于各种环境中以消除或控制这些细菌。

9. 发明授权

US3697503A Lincomycin isothiouronium salts and process for preparing same 失效
标题翻译： LINCOMYCIN ISOTHIOURONIUM SALTS及其制备方法
公开(公告)号：US3697503A
公开(公告)日：1972-10-10
申请号：US3697503D
申请日：1969-11-03
申请人： UPJOHN CO
发明人： BANNISTER BRIAN
IPC分类号： C07H9/04 , C07H15/16 , C07C47/18
CPC分类号： C07H9/04 , C07H15/16
摘要： A peracylated trans-1-bromoglycoside is treated with thiourea in a tertiary amide, dipolar, aprotic solvent to form the corresponding peracylated cis- and trans-glycosyl isothiouronium salt, which is then converted to the corresponding peracylated 1-thioglycoses and alkyl peracylated 1-thioglycosides, and if desired, the cis anomers are isolated. 1-thioglycoses
摘要翻译：过酰基化反式1-溴代糖苷用硫脲在叔酰胺，偶极，非质子溶剂中处理以形成相应的过酰基化顺式和反式糖基异硫脲盐，然后将其转化为相应的过酰基化的1-硫代糖苷和过氧化1- 硫代糖苷类，如果需要，分离出顺式端基异构体。 1-巯基糖

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