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41. 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。

42. 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

43. 发明授权

US3692767A Process for making lincomycin and analogs thereof and novel compounds obtained thereby 失效
标题翻译：制备LINCOMYCIN及其类似物及其获得的新化合物的方法
公开(公告)号：US3692767A
公开(公告)日：1972-09-19
申请号：US3692767D
申请日：1970-05-06
申请人： UPJOHN CO
发明人： MAGERLEIN BARNEY J
IPC分类号： B01F15/04 , C07H15/16 , C07C47/18
CPC分类号： C07H15/16 , B01F15/04
摘要： Lincomycin is formed by tosylating methyl 1-thio- Alpha -Dgalacto-octopyranoside to form methyl 6-O-(p-toluenesulfonyl)-1thio- Alpha -D-galactopyranoside, acylating the resulting compound to form the peracylate, replacing the tosyl group with iodine to form peracylated methyl 6-deoxy-6-iodo-1-thio- Alpha D-galactopyranoside, replacing the iodo group by a nitro group to form peracylated methyl 6-deoxy-6-nitro-1-thio- Alpha -Dgalactopyranoside, treating the latter with acetaldehyde and sodium methoxide to form methyl 6-deamino-6-nitro- Alpha thiolincosaminide, reducing the latter with lithium aluminum hydride to form methyl Alpha -thiolincosaminide, and acylating the latter with trans-1-methyl-4-propyl-L-2-pyrrolidinecarboxylic acid. By substituting other aldehydes and/or other 1-thio- Alpha -D-galactopyranosides, analogs of lincomycin are obtained.
摘要翻译：通过将1-硫代-α-D-半乳糖 - 辛吡喃甲酸甲苯磺酰化形成甲基纤维素形成6-O-（对甲苯磺酰基）-1-硫代-α-D-吡喃半乳糖苷甲基酯，酰化所得化合物以形成过苯甲酸酯，代替甲苯磺酰基与碘形成过酰基化甲基6-脱氧-6-碘-1-硫代-α-D-吡喃半乳糖苷，用碘基代替碘代，形成过酰基化甲基6-脱氧-6-硝基-1-硫代 - α-D-吡喃半乳糖苷，用乙醛和甲醇钠处理后者，形成6-脱氨基-6-硝基-α-硫代吗啉氨基甲酸酯，用氢化铝锂还原后者，形成α-硫代氨基甲酰甲酰甲酯，并用反式 -1-甲基-4-丙基-L-2-吡咯烷羧酸。通过用其他醛和/或其它1-硫代-α-D-吡喃半乳糖苷取代，可以得到林可霉素的类似物。

44. 发明授权

US3689474A 7-mercapto-7-deoxylincomycins and process for preparing the same 失效
标题翻译： 7-MERCAPTO-7-去氧肾上腺素及其制备方法
公开(公告)号：US3689474A
公开(公告)日：1972-09-05
申请号：US3689474D
申请日：1970-08-04
申请人： UPJOHN CO
发明人： KAGAN FRED , MAGERLEIN BARNEY J
IPC分类号： C07H15/16 , C07G11/00
CPC分类号： C07H15/16
摘要： WHICH ON ACYLATION YIELDS COMPOUNDS OF FORMULA I.

HYDROPYRAN

2-(R-S-),3,4,5-TRI(HO-),6-(CH3-CH(-SH)-CH(-NH2)-)TETRA-

AND HEATING IT WITH HYDROGEN SULFIDE IN AN INERT SOLVENT FOR FORM A COMPOUND OF THE FORMULA:

PYRAN

2-(R-S-),3,4,5-TRI(HO-),6-((-CH(-CH3)-NH-)>CH-)TETRAHYDRO-

AN INERT SOLVENT IN THE PRESENCE OF AN ACID ACCEPTOR, THE 2-, 3-, AND 4-HYDROXY GROUP MAY BE COVERSED WITH PROTECTIVE GROUPS, TO FORM A NOVEL COMPOUND OF THE FORMULA:

HYDROPYRAN

2-(R-S-),3,4,5-TRI(HO-),6-(CH3-CH(-HALO)-CH(-NH2)-)TETRA-

ARE PREPARED BY HEATING A COMPOUND OF THE FORMULA:

TETRAHYDROPYRAN

2-(R-S-),3,4,5-TRI(HO-),6-(CH3-CH(-SH)-CH(-NH-CO-R4)-)

ANTIBACTERIAL COMPOUNDS OF THE FORMULA:

45. 发明授权

US3671647A Lincomycin 3-nucleotides and the salts thereof 失效
标题翻译： LINCOMYCIN 3核和它的销售
公开(公告)号：US3671647A
公开(公告)日：1972-06-20
申请号：US3671647D
申请日：1971-03-24
申请人： UPJOHN CO
发明人： ARGOUDELIS ALEXANDER D , COATS JOHN H
IPC分类号： C07H15/16 , C07H19/04 , C07C47/18
CPC分类号： C07H19/04 , C07H15/16 , Y10S435/886
摘要： This invention relates to novel antibacterial compounds and to processes for preparing them. It is particularly directed to novel 3-nucleotides of lincomycin, and of analogs thereof, and of celesticetins. The compounds of the invention can be shown by the following formula:

WHEREIN Y is -SR wherein R is alkyl of one to six carbon atoms, inclusive, , OR -S-CH2-CH2-OH, R1 is H, or cis or trans lower-alkyl of from one to eight carbon atoms, inclusive; R2 is H, CH3, or C2H5; X is OH, chlorine, bromine, iodine or -OR3 wherein R3 is alkyl of one to six carbon atoms, inclusive, each in the (R) or (S) configuration; and Z is a nucleoside -5''- phosphate group wherein said nucleoside can be adenosine, guanosine, cytidine or uridine; and salts thereof. Examples of alkyl of from one to eight carbon atoms are methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, and octyl and isomers thereof.
摘要翻译：本发明涉及新的抗菌化合物及其制备方法。特别涉及林可霉素及其类似物和celesticetins的新型3-核苷酸。本发明的化合物可用下式表示：

46. 发明授权

US3598806A Process for preparing lincomycin-3-monoacylates 失效
标题翻译：制备LINCOMYCIN-3-MONOACYLATES的方法
公开(公告)号：US3598806A
公开(公告)日：1971-08-10
申请号：US3598806D
申请日：1969-04-15
申请人： UPJOHN CO
发明人： MOROZOWICH WALTER
IPC分类号： B01J31/00 , C07H15/16 , C07C47/18
CPC分类号： C07H15/16
摘要： THIS INVENTION RELATES TO A NOVEL PROCESS FOR THE MANUFACTURE OF LINCOMYCIN-3-MONOACYLATE COMPOUNDS, INCLUDING NOVEL 7-HALOGENATED LINCOMYCIN-3-MONOACYLATE COMPOUNDS, SELECTED FROM THE GROUP CONSISTING OF THE FREE BASES AND ACID ADDITION SALTS OF THE FORMULA:

2-RS-,3,5-DI-HO-,3-AC-O-,6-((4-R1,1-R2-PYRROLIDIN-3-YL)-

CO-NH-CH(-CH(-X)-CH3))-TETRAHYDROPYRAN

WHEREIN R IS ALKYL OF 1 TO 6 CARBON ATOMS, INCLUSIVE; R1 IS ALKYL OF 2 TO 8 CARBON ATOMS, INCLUSIVE; R2 IS ALKYL OF 1 TO 8 CARBON ATOMS, INCLUSIVE, OR HYDROGEN; X IS HYDROXY, CHLORINE, BROMINE OR IODINE; AND AC IS THE ACYL RADICAL OF A HYDROCARBON CARBOXYLIC ACID CONTAINING 1 TO 18 CARBON ATOMS, INCLUSIVE. IN THE ABOVE FORMULA I, THE VERTICAL WAVY LINE F IS USED TO INDICATE THAT THE GROUP R1 CAN BE IN THE CIS POSITION (BELOW THE PLANE OF THE RING) OF IN THE TRANS POSITION (ABOVE THE PLANE OF THE RING), WITH RESPECT TO THE CARBONYL GROUP. THE HORIZONTAL WAVY LINE $ IS USED TO INDICATE THAT BOTH EPIMERS ARE TO BE INCLUDED IN THE GROUP, THE 7(R) (OR D-ERYTHRO) CONFIGURATION AND THE 7(S) (OR L-THREO) CONFIGURATION. THESE LINCOMYCIN-3-MONOACYLATE COMPOUNDS CAN BE USED AS ANTIBACTERIAL AGENTS, FOR EXAMPLE TO INHIBIT THE GROWTH OF STAPHYLOCOCCUS AUREUS AND SARCINA LUTEA ON DENTAL AND MEDICAL EQUIPMENT CONTAMINATED WITH THESE ORGANISMS. THE NOVEL 7-HALOGENATED 3-MONOACYLATE ESTERS ARE PARTICULARLY ADVANTAGEOUS IN HAVING GREATER ANTIBACTERIAL ACTIVITY THAN THE 7-HYDROXY ESTERS. THE NOVEL PROCESS FOR SELECTIVE 3-MONOACYLATION OF LINCOMYCIN COMPOUNDS OF THIS INVENTION COMPRISES MIXING A SOLUTION OF THE LINCOMYCIN COMPOUND OR ITS ACID ADDITION SALT WITH THE ACID ANHYDRIDE OR ACYL HALIDE OF A HYDROCARBON CARBOXYLIC ACID AND A STERICALLY HINDERED STRONGLY BASIC TERTIARY AMINE AND REACTING UNDER MILD CONDITIONS.

47. 发明授权

US3580904A 7-halo-7-deoxy-lincomycin derivatives 失效
标题翻译： 7-HALO-7-去氧山梨醇衍生物
公开(公告)号：US3580904A
公开(公告)日：1971-05-25
申请号：US3580904D
申请日：1969-04-03
申请人： UPJOHN CO
发明人： MOROZOWICH WALTER , SINKULA ANTHONY A
IPC分类号： C07H15/16 , C07C47/18
CPC分类号： C07H15/16 , Y10S516/07
摘要： ANTIBACTERIAL COMPOUNDS OF THE FORMULA:

2-(R-S-),3-(R-COO-),4,5-DI(HO-),6-((1-R3,4-R1-PYRROLIDIN-

2-YL)-CO-NH-CH(-CH(-X)-CH3)-)TETRAHYDROPYRAN

AND THE SALTS THEREOF, AND THE 3,4-O-ARYLIDENE DERIVATIVES.

48. 发明授权

US3539689A 7-halo-lincomycin composition and process of treatment 失效
标题翻译： 7-HALO-LINCOMYCIN组合物和治疗过程
公开(公告)号：US3539689A
公开(公告)日：1970-11-10
申请号：US3539689D
申请日：1968-02-09
申请人： UPJOHN CO
发明人： BIRKENMEYER ROBERT D , KAGAN FRED
IPC分类号： C07D207/16 , C07D207/22 , C07H15/16 , C12P19/64 , A61K27/00
CPC分类号： C07D207/22 , C07D207/16 , C07H15/16 , C12P19/64

49. 发明授权

US3502648A 7-halo-7-deoxythiolincosaminides and process for preparing the same 失效
标题翻译： 7-羟基-7-脱氧山梨糖醇胺及其制备方法
公开(公告)号：US3502648A
公开(公告)日：1970-03-24
申请号：US3502648D
申请日：1967-12-22
申请人： UPJOHN CO
发明人： BIRKENMEYER ROBERT D , KAGAN FRED
IPC分类号： C07D207/22 , C07H15/16 , C12P19/64 , C07D7/04
CPC分类号： C07H15/16 , C07D207/22 , C12P19/64

50. 发明授权

US3487068A Lincomycin-2-phosphates,7-substituted compounds and salts thereof 失效
标题翻译： LINCOMYCIN-2-PHOSPHATES，7-取代的化合物及其盐
公开(公告)号：US3487068A
公开(公告)日：1969-12-30
申请号：US3487068D
申请日：1966-12-16
申请人： UPJOHN CO
发明人： MOROZOWICH WALTER , LAMB DONALD J
IPC分类号： C07F9/08 , C07H15/16 , C07D99/04 , A61K21/00 , C07D27/04
CPC分类号： A61K31/70 , C07H15/16

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