-
31.发明授权
公开(公告)号：US5248797A
公开(公告)日：1993-09-28
申请号：US928587
申请日：1992-08-13
Applicant: Phaik-Eng Sum
Inventor： Phaik-Eng Sum
IPC: B01J23/10 , B01J23/40 , B01J23/74 , C07B61/00 , C07C231/12 , C07C237/26
CPC classification number: C07C231/12 , C07C237/26 , C07C2103/46
Abstract: The invention relates to a novel method for producing [4S-(4alpha, 12aalpha)]-9-amino-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide, hereinafter called 9-amino-6-demethyl-6-deoxytetracycline, which compound is a valuable intermediate for synthesis of tetracyclines.
-
![CRYSTALLINE SALTS OF (4S,4AS,5AR,12AS)-4-DIMETHYLAMINO-3,10,12,12A-TETRAHYDROXY-7-[(METHOXY(METHYL)AMINO)-METHYL]-1,11-DIOXO-1,4,4A,5,5A,6,11,12A-OCTAHYDRO-NAPHTHACENE-2-CARBOXYLIC ACID AMIDE AND METHODS OF USING THE SAME](/abs-image/US/2013/01/10/US20130012480A1/abs.jpg.150x150.jpg)
32.发明申请CRYSTALLINE SALTS OF (4S,4AS,5AR,12AS)-4-DIMETHYLAMINO-3,10,12,12A-TETRAHYDROXY-7-[(METHOXY(METHYL)AMINO)-METHYL]-1,11-DIOXO-1,4,4A,5,5A,6,11,12A-OCTAHYDRO-NAPHTHACENE-2-CARBOXYLIC ACID AMIDE AND METHODS OF USING THE SAME 有权（4S，4AS，5AR，12AS）-4-二甲基氨基-3,10,12,12-四氢化-7- [（甲基（甲基）氨基） - 甲基] -1,11-二氧代-1,4- ，4A，5,5A，6,11,12A-OCTAHYDRO-NAPHTHACENE-2-羧酸酰胺及其使用方法公开(公告)号：US20130012480A1
公开(公告)日：2013-01-10
申请号：US13471275
申请日：2012-05-14
Applicant: Catherine Coulter , Sean M. Johnston , Farzaneh Seyedi
Inventor： Catherine Coulter , Sean M. Johnston , Farzaneh Seyedi
IPC: C07C237/26 , A61P31/04 , A61P17/10 , A61P17/00 , A61K31/65 , C07C309/04
CPC classification number: C07C237/26 , C07B2200/07 , C07B2200/13 , C07C239/20 , C07C309/04 , C07C2103/46 , C07C2603/46
Abstract: A crystalline mono hydrochloride salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide is disclosed having improved stability. In addition, a crystalline mono mesylate salt and crystalline mono sulfate salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide are also disclosed having improved stability. A pharmaceutical composition containing the crystalline salts and methods of treating inflammatory skin disorders and bacterial infections comprising administering the crystalline salts are also disclosed.
Abstract translation: （4S，4aS，5aR，12aS）-4-二甲基氨基-3,10,12,12a-四羟基-7 - [（甲氧基（甲基）氨基） - 甲基] -1,11-二氧代 - 公开了具有改进的稳定性的1,4,4a，5,5a，6,11,12a-八氢 - 并四烯-2-羧酸酰胺。 另外，（4S，4aS，5aR，12aS）-4-二甲基氨基-3,10,12,12a-四羟基-7 - [（甲氧基（甲基）氨基） - 甲基的结晶单甲磺酸盐和结晶一硫酸盐 ] -1,11-二氧代-1,4,4a，5,5a，6,11,12a-八氢 - 并四苯-2-甲酸酰胺，其具有改进的稳定性。 还公开了含有结晶盐的药物组合物和治疗炎性皮肤病症和细菌感染的方法，包括给予结晶盐。
-
公开(公告)号：US6143161A
公开(公告)日：2000-11-07
申请号：US317396
申请日：1999-05-24
Applicant: William Heggie , Jose Galindro , Pedro Santos , Luis Carvalho
Inventor： William Heggie , Jose Galindro , Pedro Santos , Luis Carvalho
IPC: A61K31/65 , A61K31/00 , A61P43/00 , C07C20060101 , C07C231/00 , C07C231/12 , C07C235/82 , C07C237/26 , C25B20060101 , C25B3/00 , C25B3/04 , C25B7/00
CPC classification number: C07C231/12 , C07C2103/46
Abstract: The present invention refers to a process for the preparation of 4-(des-dimethylamino)-tetracyclines, which compounds have a therapeutical application. The starting tetracyclines are treated with a methylating agent and the resulting trimethylammonium salts are reduced by electrolysis in an aqueous solution at acidic pH, in the presence of an adequate electrolyte. A direct electrical current with a potential of 0.5-1.5 volts is applied between two convenient electrodes until the reaction is complete. The 4-(des-dimethylamino)-tetracyclines are isolated by extraction with an organic solvent.
Abstract translation: 本发明涉及制备4-（去二甲基氨基）四环素的方法，该化合物具有治疗应用。 起始的四环素用甲基化剂处理，所得的三甲基铵盐通过在酸性pH下，在足够的电解质存在下，在水溶液中电解而还原。 在两个方便的电极之间施加电位为0.5-1.5伏特的直流电，直到反应完成。 通过用有机溶剂萃取分离4-（去二甲基氨基）四环素。
-
34.发明授权7-(substituted)-8-(substituted)-9-(substitued amino)-6-demethyl-6-deoxytetracyclines 失效7-（取代的）-8-（取代的）-9-（取代的氨基）-6-去甲基-6-脱氧四环素
公开(公告)号：US5886175A
公开(公告)日：1999-03-23
申请号：US352310
申请日：1994-12-08
Applicant: Phaik-Eng Sum , Ving J. Lee , Joseph J. Hlavka , Raymond T. Testa
Inventor： Phaik-Eng Sum , Ving J. Lee , Joseph J. Hlavka , Raymond T. Testa
IPC: A61K31/65 , A61P31/00 , A61P31/04 , C07C20060101 , C07C237/26 , C07C239/18 , C07C243/20 , C07C245/20 , C07C247/18 , C07C255/41 , C07C271/24 , C07C271/60 , C07C309/39 , C07C309/65 , C07C317/28 , C07C323/59 , C07D205/04 , C07D207/16 , C07D209/52 , C07D221/22 , C07D231/14 , C07D233/61 , C07D233/96 , C07D241/12 , C07D249/04 , C07D249/08 , C07D249/10 , C07D249/16 , C07D257/04 , C07D261/08 , C07D265/30 , C07D265/36 , C07D279/12 , C07D295/08 , C07D295/14 , C07D295/20 , C07D295/22 , C07D307/18 , C07D333/06 , C07D333/36 , C07D453/06 , C07D471/08 , C07D487/08 , C07C231/12 , C07C233/64
CPC classification number: C07C237/26 , C07C243/20 , C07C245/20 , C07C247/18 , C07C271/24 , C07C271/60 , C07C309/65 , C07C2103/46
Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.
Abstract translation: 本发明提供了可用作制备6-去甲基-6-反四环素类抗生素的中间体的式（VI）VI和VI的化合物。
-
35.发明授权9- (substituted amino) -alpha-6-deoxy-5-oxy tetracycline derivatives, their preparation and their use as antibiotics 失效9-（取代氨基）-α-6-脱氧-5-氧四环素衍生物，其制备及其作为抗生素的用途
公开(公告)号：US5834450A
公开(公告)日：1998-11-10
申请号：US682640
申请日：1996-07-22
Applicant: Wei-guo Su
Inventor： Wei-guo Su
IPC: A61K31/65 , A61P31/04 , C07C237/26 , C07C311/08 , A01N37/18
CPC classification number: C07C237/26 , C07C2103/46
Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in the specification and the pharmaceutically acceptable salts of such compounds. Compounds of the formula I exhibit antibiotic activity against a wide range of gram-positive and gram-negative organisms, including organisms that are resistant to tetracycline antibiotics.
Abstract translation: PCT No.PCT / IB95 / 00026 Sec。 371日期：1996年7月22日 102（e）日期1996年7月22日PCT提交1995年1月12日PCT公布。 出版物WO95 / 22529 日期1995年8月24日本发明涉及式（I）的化合物，其中R 1，R 2和R 3如本说明书中所定义，并且该化合物的药学上可接受的盐。 式I的化合物对广泛的革兰氏阳性和革兰氏阴性生物体，包括对四环素抗生素具有抗性的生物具有抗生素活性。
-
Patent Agency Ranking
公开(公告)号：US5538954A
公开(公告)日：1996-07-23
申请号：US265193
申请日：1994-06-24
Applicant: Torben Koch , Hjarne Dyrsting
Inventor： Torben Koch , Hjarne Dyrsting
IPC: A61K38/14 , C07C237/26 , C07F9/117 , C07H5/10 , C07H11/00 , C07H11/04 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C07H17/08 , C08B37/02 , A61K31/70 , C07H5/00
CPC classification number: C07H17/08 , A61K38/14 , C07C237/26 , C07F9/117 , C07H11/00 , C07H11/04 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C07H5/10 , C08B37/0021 , C07C2103/46
Abstract: A salt of sucrose-octa-O-sulfonic acid and a tetracycline useful in inhibiting protein synthesis of bacteria.
Abstract translation: 蔗糖 - 八-O-邻磺酸和四环素的盐可用于抑制细菌的蛋白质合成。
-
37.发明授权
公开(公告)号：US5530117A
公开(公告)日：1996-06-25
申请号：US455923
申请日：1995-05-31
Applicant: Joseph J. Hlavka , Phaik-Eng Sum , Yakov Gluzman , Ving J. Lee , Adma A. Ross
Inventor： Joseph J. Hlavka , Phaik-Eng Sum , Yakov Gluzman , Ving J. Lee , Adma A. Ross
IPC: C07C237/26 , C07D205/04 , C07D277/22 , C07D277/46 , C07D307/68 , C07D333/24 , C07D333/34 , C07D333/38 , C07D205/08 , C07D211/06 , C07D265/30 , C07D293/10
CPC classification number: C07D333/38 , C07C237/26 , C07D205/04 , C07D277/46 , C07D307/68 , C07D333/24 , C07D333/34 , C07C2103/46
Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.
Abstract translation: 本发明涉及新的7-取代-9-（取代氨基）-6-脱甲基-6-脱氧四环素化合物。 这些化合物可用于治疗由广谱细菌生物引起的感染，包括耐四环素的细菌生物。
-
38.发明授权7-(substituted)-8-(substituted)-9-(substituted amino)-6-demethyl-6-deoxytetracyclines 失效7-（取代的）-8-（取代的）-9-（取代的氨基）-6-去甲基-6-脱氧四环素
公开(公告)号：US5512553A
公开(公告)日：1996-04-30
申请号：US454966
申请日：1995-05-31
Applicant: Phaik-Eng Sum , Ving J. Lee , Joseph J. Hlavka , Raymond T. Testa
Inventor： Phaik-Eng Sum , Ving J. Lee , Joseph J. Hlavka , Raymond T. Testa
IPC: A61K31/65 , A61P31/00 , A61P31/04 , C07C20060101 , C07C237/26 , C07C239/18 , C07C243/20 , C07C245/20 , C07C247/18 , C07C255/41 , C07C271/24 , C07C271/60 , C07C309/39 , C07C309/65 , C07C317/28 , C07C323/59 , C07D205/04 , C07D207/16 , C07D209/52 , C07D221/22 , C07D231/14 , C07D233/61 , C07D233/96 , C07D241/12 , C07D249/04 , C07D249/08 , C07D249/10 , C07D249/16 , C07D257/04 , C07D261/08 , C07D265/30 , C07D265/36 , C07D279/12 , C07D295/08 , C07D295/14 , C07D295/20 , C07D295/22 , C07D307/18 , C07D333/06 , C07D333/36 , C07D453/06 , C07D471/08 , C07D487/08
CPC classification number: C07C237/26 , C07C243/20 , C07C245/20 , C07C247/18 , C07C271/24 , C07C271/60 , C07C309/65 , C07C2103/46
Abstract: The invention provides compounds of formula ##STR1## wherein X, R and R.sup.1 are defined in the specification. These compounds are useful as antibiotic agents.
Abstract translation: 本发明提供式I的化合物，其中X，R和R 1在本说明书中定义。 这些化合物可用作抗生素。
-
39.发明授权Process for producing 7-(substituted)-8-(substituted-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines 失效制备7-（取代的）-8-（取代的-9 - [（取代的甘氨酰基）酰胺基] -6-脱甲基-6-脱氧四环素的方法
公开(公告)号：US5495032A
公开(公告)日：1996-02-27
申请号：US312593
申请日：1994-09-27
Applicant: Phaik-Eng Sum , Ving J. Lee , Joseph J. Hlavka , Raymond T. Testa
Inventor： Phaik-Eng Sum , Ving J. Lee , Joseph J. Hlavka , Raymond T. Testa
IPC: C07D295/12 , A61K31/397 , A61K31/445 , A61K31/65 , A61P31/00 , A61P31/04 , C07C20060101 , C07C231/12 , C07C237/26 , C07C239/20 , C07C255/41 , C07C309/39 , C07C309/65 , C07C323/59 , C07D205/04 , C07D205/12 , C07D207/06 , C07D207/16 , C07D207/32 , C07D207/327 , C07D211/34 , C07D213/56 , C07D231/12 , C07D233/60 , C07D233/61 , C07D239/26 , C07D265/02 , C07D265/30 , C07D295/14 , C07D295/15 , C07D295/22 , C07D295/24 , C07D307/54 , C07D401/06 , C07D487/04 , C07D487/08 , C07D521/00 , C07C233/64
CPC classification number: C07D207/327 , C07C237/26 , C07D205/04 , C07D207/16 , C07D213/56 , C07D231/12 , C07D233/56 , C07D249/08 , C07D265/02 , C07D295/15 , C07D295/24 , C07D307/54 , C07D487/04 , C07C2101/02 , C07C2101/04 , C07C2103/46
Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein, R, R.sup.3, R.sup.4, X and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar-protic or a polar-aprotic solvent. The resulting compounds are useful as antibiotics.
Abstract translation: 本发明提供了一种制备下式化合物的方法：其中R，R 3，R 4，X和W在本说明书中定义，其中下式的化合物：与亲核试剂反应 在极性 - 质子或极性 - 非质子溶剂的存在下在惰性气氛中制备式WH。 所得化合物可用作抗生素。
-
40.发明授权
公开(公告)号：US5495030A
公开(公告)日：1996-02-27
申请号：US299769
申请日：1994-09-01
Applicant: Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
Inventor： Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
IPC: A61K31/65 , A61P31/00 , A61P31/04 , C07C20060101 , C07C237/26 , C07C239/18 , C07C239/20 , C07C255/50 , C07C271/22 , C07C323/29 , C07D207/06 , C07D207/14 , C07D207/16 , C07D207/30 , C07D209/02 , C07D211/14 , C07D211/56 , C07D213/40 , C07D213/74 , C07D221/22 , C07D231/12 , C07D231/14 , C07D241/04 , C07D241/14 , C07D249/02 , C07D249/04 , C07D249/08 , C07D265/28 , C07D279/04 , C07D295/14 , C07D295/15 , C07D295/215 , C07D295/24 , C07D307/33 , C07D333/20 , C07D333/36 , C07F15/00 , C07C50/22
CPC classification number: C07D213/40 , C07C237/26 , C07C239/18 , C07C239/20 , C07C271/22 , C07D295/15 , C07D295/215 , C07D295/24 , C07D333/20 , C07C2103/46
Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1 and Y are defined in the specification. The compounds are useful for the production of 6-demethyl-6-deoxytracycline derivatives.
Abstract translation: 本发明提供下式的化合物：其中R，R 1和Y在本说明书中定义。 该化合物可用于生产6-脱甲基-6-脱氧四环素衍生物。
-
-
-
-
-
-
-
-
-
Search Results
43
records
(took 0.039 seconds)
