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1. 发明申请

US20100210570A1 LINCOMYCIN DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT 失效
标题翻译： LINCOMYCIN衍生物和包含它们作为活性成分的抗微生物剂
公开(公告)号：US20100210570A1
公开(公告)日：2010-08-19
申请号：US12451744
申请日：2008-05-30
申请人： Yoshinari Wakiyama , Kou Kumura , Satomi Masaki , Kazutaka Ueda , Yasuo Sato , Chika Kikuchi , Eijirou Umemura , Yoko Hirai , Hiroshi Kondo
发明人： Yoshinari Wakiyama , Kou Kumura , Satomi Masaki , Kazutaka Ueda , Yasuo Sato , Chika Kikuchi , Eijirou Umemura , Yoko Hirai , Hiroshi Kondo
IPC分类号： A61K31/7056 , C07H15/16 , A61P31/04 , A61P11/00
CPC分类号： C07H15/16
摘要： An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R1 representsN-optionally substituted C1-6 alkyl-N-optionally substituted C1-6 alkylamino-C1-6 alkyl; R2 represents a hydrogen atom or optionally substituted C1-6 alkyl; R3 represents optionally substituted C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.
摘要翻译：本发明的目的是提供式（1）化合物或其药理学上可接受的盐或溶剂化物，其中A表示芳基; R1表示N-任选取代的C 1-6烷基-N-任选取代的C 1-6烷基氨基-C 1-6烷基; R2表示氢原子或任选取代的C 1-6烷基; R3表示任选取代的C 1-6烷基或C 3-6环烷基-C 1-4烷基; m为1〜3; n为0; 并且p为0至2.该化合物是对感染性疾病的治疗中最近引起问题的抗性肺炎链球菌具有有效活性的新型林可霉素衍生物。此外，该化合物可用作抗微生物剂，并且可用于预防或治疗细菌感染性疾病。

2. 发明申请

US20030073826A1 Crystaline clindamycin free base 审中-公开
标题翻译：克林霉素游离碱
公开(公告)号：US20030073826A1
公开(公告)日：2003-04-17
申请号：US10227902
申请日：2002-08-26
发明人： Robert S. Chao , Michael Hawley , Lisa M. Reeder , Donald P. Jones
IPC分类号： C07H015/16
CPC分类号： C07H13/10 , C07H15/16 , C07H15/26
摘要： A processes for preparing crystalline clindamycin free base is provided.
摘要翻译：提供了制备结晶克林霉素游离碱的方法

3. 发明申请

US20030073648A1 Crystaline clindamycin free base 审中-公开
标题翻译：克林霉素游离碱
公开(公告)号：US20030073648A1
公开(公告)日：2003-04-17
申请号：US10228356
申请日：2002-08-26
发明人： Robert S. Chao , Michael Hawley , Lisa M. Reeder , Donald P. Jones
IPC分类号： A61K031/7056 , C07H005/04
CPC分类号： C07H13/10 , C07H15/16 , C07H15/26
摘要： The antibiotic drug clindamycin is provided as a crystalline free base. Three polymorphic/pseudopolymorphic forms of crystalline clindamycin free base are disclosed. Also provided are pharmaceutical compositions comprising crystalline clindamycin free base. Processes for preparing crystalline clindamycin free base and compositions thereof are also provided along with methods for treating medical conditions with the pharmaceutical compositions.
摘要翻译：提供抗生素药物克林霉素作为结晶游离碱。公开了结晶克林霉素游离碱的三种多晶型/假多晶型形式。还提供了包含结晶克林霉素游离碱的药物组合物。还提供了制备结晶克林霉素游离碱及其组合物的方法以及用药物组合物治疗医学病症的方法。

4. 发明授权

US5004731A Unsaturated cycloaliphatic esters of macrolidic and lincosamidic antibiotics and pharmaceutical and cosmetic compositions containing them 失效
标题翻译：大环内酯和磺酰胺抗生素的不饱和脂环族酯和含有它们的药物和化妆品组合物
公开(公告)号：US5004731A
公开(公告)日：1991-04-02
申请号：US266598
申请日：1988-11-03
申请人： Michel Philippe , Henri Sebag
发明人： Michel Philippe , Henri Sebag
IPC分类号： A61K8/00 , A61K8/34 , A61K8/35 , A61K8/37 , A61K8/49 , A61K8/60 , A61K8/73 , A61K8/89 , A61K8/891 , A61K31/70 , A61K31/7028 , A61K31/7042 , A61K31/7048 , A61P17/00 , A61Q19/00 , C07H15/16 , C07H17/08
CPC分类号： A61K8/602 , A61Q19/00 , C07H15/16 , C07H17/08 , Y10S514/844 , Y10S514/859
摘要： Unsaturated cycloaliphatic esters of macrolidic and lincosamidic antibiotics are employed in the treatment of acne.
摘要翻译：大环内酯和磺胺类抗生素的不饱和脂环族酯用于治疗痤疮。

5. 发明授权

US5004729A Aromatic esters of macrolidic and lincosamidic antibiotics and pharmaceutical and cosmetic compositions containing them 失效
标题翻译：大环内酯和磺酰胺抗生素的芳族酯和含有它们的药物和化妆品组合物
公开(公告)号：US5004729A
公开(公告)日：1991-04-02
申请号：US266862
申请日：1988-11-03
申请人： Michel Philippe , Henri Sebag
发明人： Michel Philippe , Henri Sebag
IPC分类号： A61K8/00 , A61K8/34 , A61K8/35 , A61K8/37 , A61K8/60 , A61K8/73 , A61K8/89 , A61K8/891 , A61K31/70 , A61K31/7028 , A61K31/7042 , A61K31/7048 , A61P17/00 , A61Q19/00 , C07H15/16 , C07H17/08
CPC分类号： A61K8/602 , A61Q19/00 , C07H15/16 , C07H17/08 , Y10S514/844 , Y10S514/859
摘要： Aromatic esters of macrolidic and lincosamidic antibiotics are employed in the treatment of acne.
摘要翻译：大环内酯和磺胺类抗生素的芳族酯用于治疗痤疮。

6. 发明授权

US3923602A Composition of matter and process 失效
标题翻译：物质和过程的组成
公开(公告)号：US3923602A
公开(公告)日：1975-12-02
申请号：US54573475
申请日：1975-01-31
申请人： UPJOHN CO
发明人： ARGOUDELIS ALEXANDER D , COATS JOHN H , JOHNSON LEROY E
IPC分类号： C07H15/16 , C12D9/00
CPC分类号： C07H15/16 , Y10S435/803 , Y10S435/886
摘要： Microbiological processes for preparing new celestosaminide antibiotics by using the microorganism Streptomyces caelestis, NRRL 2418, and disclosed mutants Streptomyces caelestis mutant 22227a, NRRL 5320, and Streptomyces caelestis mutant 22218a, NRRL 5481.
摘要翻译：通过使用微生物链霉菌链霉菌NRRL 2418和公开的突变体链霉菌（Streptomyces caelestis）突变体22227a，NRRL 5320和链霉菌（Streptomyces caelestis）突变体22218a，NRRL 5481制备新的celestosaminide抗生素的微生物过程。

7. 发明授权

US3856943A Compositions and process 失效
标题翻译：组成和过程
公开(公告)号：US3856943A
公开(公告)日：1974-12-24
申请号：US42514873
申请日：1973-12-17
申请人： UPJOHN CO
发明人： BIRKENMEYER R
IPC分类号： C07H15/16 , A01N9/00
CPC分类号： C07H15/16
摘要： THE ZWITTERION THEREOF OR THE HEMI-SALT THEREOF; R is alkyl of not more than 4 carbon atoms; and R1 is alkyl of not more than 8 carbon atoms in association with a pharmaceutical carrier. The compounds have clindamycin-like antibacterial activity and provide particularly high concentrations of compound in the urinary tract thereby being particularly useful in treating bacterial infections of the upper and lower urinary tract as well as L-forms in the kidney.
OR THE ACID ADDITION SALTS THEREOF WHEREIN Halo is chlorine, bromine, or iodine, X is a member selected from the group consisting of hydrogen, an acyl radical of an aliphatic carboxylic acid having from 2 to 18 carbon atoms, inclusive,

1''-( Beta -Hydroxyethyl)-1''-demethylclindamycin compounds of the formula:
摘要翻译： 1' - （β-羟基乙基）-1'-去甲基克林霉素化合物，其结构如下：

8. 发明授权

US3812096A N-demethylcelesticetin derivatives 失效
标题翻译： N-DEMETHYLCELESTICETIN衍生物
公开(公告)号：US3812096A
公开(公告)日：1974-05-21
申请号：US26172472
申请日：1972-06-12
申请人： UPJOHN CO
发明人： ARGOUDELIS A , COATS J , SEBEK O
IPC分类号： C07H15/16 , C07C129/18
CPC分类号： C07H15/16 , Y10S435/886
摘要： NEW ANTIBIOTICS, N-DEMETHYL-7-O-DEMETHYLCELESTICETIN (IV) AND N-DEMETHYLCELESTICETIN (IVA), ARE PRODUCED CONCOMITANTLY BY THE CONTROLLED FERMENTATION OF THE NEW MICRO-ORGANISM STREPTOMYCES CALESTIS STRAIN 22218A IN AN AQUEOUS NUTRIENT MEDIUM. THESE ANTIBIOTICS ARE ANTIBACTERIALLY ACTIVE AND ALSO CAN BE CONVERTED TO VARIOUS ANTIBACTERIALLY ACTIVE ANALOGUES.

9. 发明授权

US3812014A Process for preparing lincomycin 失效
标题翻译：制备LINCOMYCIN的方法
公开(公告)号：US3812014A
公开(公告)日：1974-05-21
申请号：US27878472
申请日：1972-08-08
申请人： UPJOHN CO
发明人： ARGOUDELIS A , COATS J
IPC分类号： C12P19/64 , C12P1/06 , C12R1/465 , C12D9/00
CPC分类号： C07H15/16 , Y10S435/886
摘要： A MICROBIOLOGICAL PROCESS FOR PREPARING THE ANTIBIOTIC LINCOMYCIN WITHOUT THE CONCOMITANT PRODUCTION OF LINCOMYCIN B (4''-DEPROPYL-4''-ETHYLLINOCOMYCIN). THE ABSENCE OF LINCONMYCON B IN THE FERMENTATION BEER RESULTS IN INCREASED LINCOMYCIN RECOVERY EFFICIENCY FROM THE FERMENTATION BEER.

10. 发明授权

US3737425A Derivatives of lincomycin 失效
标题翻译： LINCOMYCIN的衍生物
公开(公告)号：US3737425A
公开(公告)日：1973-06-05
申请号：US3737425D
申请日：1970-04-06
申请人： UPJOHN CO
发明人： BANNISTER B
IPC分类号： C07H15/14 , C07H15/16 , C08B19/00
CPC分类号： C07H15/14 , C07H15/16
摘要： ALKYL A-THIOLINCOSAMINIDE IS REACTED WITH PERIODATE TO FORM ALKYL 1-THIO-A-D-GALACTOHEXODIALDO-1,5-PYRANOSIDE, WHICH IS REACTED WITH CYANIDE TO FORM ALKYL 6-CYANO-1-THIOA-D-GALACTOPYRANOSIDE. THE LATTER IS CONVERTED TO ANTIBACTERIALLY ACTIVE 8-NOR-LINECOMYCINS, FIRST THE 3,4-O-POSITIONS ARE COVERED BY AN YLIDENE GROUP. THIS CAN BE DONE INITIALLY BY DEACYLATING ALKYL N-ACETYL-3,4-O-YLIDENE-A-THIOLINOSOMINIDES. THE RESULTING ALKYL 3,4-O-YLIDENE-A-THIOLINCOSAMINIDE IS TREATED SUCCESSIVELY WITH PERIODATE AND CYANIDE. THE ALKYL 6-CYANO-3,4-O-YLIDENE-A-THIOLINCOSAMINIDE IS THEN TOSYLATED AND THE RESULTING 2,7-DI-O-TOSYL DERIVATIVES ARE REDUCED WITH LITHIUM ALUMINUM HYDRIDE TO FORM THE 6,7-AXIRIDINO DERIVATIVE WHICH ON N-ACYLATION AND SOLVOYLIS, DECAYLATION, AND REACYLATION WITH THE ACID MOIETY OF LINCOMYCIN OR AN ANALOG THEREOF, YIELDS THE DESIRED 7-NOR-LINCOMYCIN OR ANALOG THEREOF. WHEN THE SOLVOYLSIS IS AFFECTED WITH METHANOL OR OTHER ALKANOL, ANTIBACTERIALLY ACTIVE 7-O-ALKYL-8-NORLINCOMYCINS ARE OBTAINED.

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