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1. 发明授权

US5750509A Amide derivatives of antibiotic A 40926 失效
标题翻译：抗生素A 40926的酰胺衍生物
公开(公告)号：US5750509A
公开(公告)日：1998-05-12
申请号：US640681
申请日：1996-04-30
申请人： Adriano Malabarba , Romeo Ciabatti , Gianbattista Panzone , Alessandra Maria Marazzi
发明人： Adriano Malabarba , Romeo Ciabatti , Gianbattista Panzone , Alessandra Maria Marazzi
IPC分类号： A61K38/00 , C07K9/00 , A61K38/14 , C07K7/50
CPC分类号： C07K9/008 , A61K38/00 , Y10S930/19
摘要： The present invention is directed to novel antibiotic A 40926 derivatives characterized by having a carboxy, (C.sub.1 -C.sub.4) alkoxy-carbonyl, aminocarbonyl, (C.sub.1 -C.sub.4) alkylaminocarbonyl, di (C.sub.4 -C.sub.4)alkylaminocarbonyl or hydroxymethyl substituent on the N-acylaminoglucuronyl moiety and a hydroxy or a polyamine substituent in position 63 of the molecule. The compounds of the invention show high in vitro activity against glycopeptide resistant Enterococci and Staphylococci.
摘要翻译：本发明涉及新型抗菌素A40926衍生物，其特征在于在N-酰氨基葡萄糖醛酸基上具有羧基，（C 1 -C 4）烷氧羰基，氨基羰基，（C 1 -C 4）烷基氨基羰基，二（C 4 -C 4）烷基氨基羰基或羟甲基取代基部分和位于分子63位的羟基或多胺取代基。本发明的化合物显示出对耐糖耐肠球菌和葡萄球菌的高体外活性。

2. 发明授权

US06218505B1 Chemical process for preparing amide derivatives of antibiotic A 40926 失效
标题翻译：制备抗生素A 40926的酰胺衍生物的化学方法
公开(公告)号：US06218505B1
公开(公告)日：2001-04-17
申请号：US09155869
申请日：1998-10-07
申请人： Gianbattista Panzone , Alessandra Maria Marazzi , Ermenegildo Restelli , Anacleto Gianantonio
发明人： Gianbattista Panzone , Alessandra Maria Marazzi , Ermenegildo Restelli , Anacleto Gianantonio
IPC分类号： C07K1113
CPC分类号： C07K9/008
摘要： Improved chemical process for preparing the compounds of formula (I), wherein: R1 represents (C9-C12)alkyl; M represents hydrogen, &agr;-D-mannopyranosyl or 6-O-acetyl-&agr;-D-mannopyranosyl and Y represents an amino group of formula —NR2-alk1-(NR3-alk2)p-(NR4-alk3)q-W. One aspect of the invention refers to the preparation of the intermediate compound of formula (III) (which corresponds to the above compound of formula (I) wherein R1 and M are as above defined and Y is hydroxy), by reacting a compound of formula (II) (which corresponds to the above compound of formula (I) wherein R1 and M are as above defined and Y is hydroxymethyl), with a (C1-C4)alkanol in the presence of a concentrated mineral acid, using the same alkanol as the reaction solvent and submitting the obtained ester compound to a reductive process by adding an alkali metal borohndride into the same reaction mixture. A further aspect of the invention refers to the amidation reaction for obtaining the compound of formula (I), which is carried out by reacting a compound of formula (III) with a suitable amine of formula (IV): NHR3-alk1-(NR4-alk2)p-(NR5-alk3)q-W, wherein R3, R4, R5, alk1, alk2, alk3, p, q and W are as defined in formula (I), in an inert organic solvent, in the presence of a condensing agent and setting the initial pH of the mixture (measured after diluting a sample of the reaction mixture with 9 volumes of water) at a value of from 6.5 to 9.0. By combining the above improved steps into a single process, it is possible to set up a particularly convenient process for preparing the compounds of formula (I). In addition, a purification method involving the use of polyamide resins and aqueous eluents is provided.
摘要翻译：制备式（I）化合物的改进的化学方法，其中：R 1表示（C 9 -C 12）烷基; M代表氢，α-D-吡喃甘露糖基或6-O-乙酰基-α-D-吡喃甘露糖基，Y代表式-NR2-alk1-（NR3-alk2）p-（NR4-alk3）q-W的氨基。本发明的一个方面是指式（III）的中间体化合物（其对应于上述式（I）的化合物，其中R 1和M如上所定义且Y是羟基），通过使式（II）（其对应于上述式（I）化合物，其中R 1和M如上所定义，Y是羟甲基）与（C1-C4）烷醇在浓无机酸存在下，使用相同的链烷醇作为反应溶剂，并将所得的酯化合物通过向相同的反应混合物中加入碱金属硼氢化物而进行还原过程。本发明的另一方面涉及获得式（I）化合物的酰胺化反应，其通过使式（III）的化合物与式（IV）的合适的胺反应来进行：NHR 3 - 烷基（NR 4 -alk2）p-（NR5-alk3）qW，其中R3，R4，R5，alk1，alk2，alk3，p，q和W如式（I）中所定义，在惰性有机溶剂中，缩合剂并设定混合物的初始pH（在用9体积水稀释反应混合物的样品后测量）的值为6.5至9.0。通过将上述改进的步骤结合到单一方法中，可以建立用于制备式（I）化合物的特别方便的方法。此外，提供了涉及使用聚酰胺树脂和水性洗脱剂的纯化方法。

3. 发明申请

US20050106691A1 Process for the production of ramoplanin-like amide derivatives 有权
标题翻译：拉莫拉宁类酰胺衍生物的制备方法
公开(公告)号：US20050106691A1
公开(公告)日：2005-05-19
申请号：US10505881
申请日：2003-02-26
申请人： Romeo Ciabatti , Sonia Maffiolt , Anna Checchia , Gabriella Romano , Gianpaolo Candiani , Gianbattista Panzone
发明人： Romeo Ciabatti , Sonia Maffiolt , Anna Checchia , Gabriella Romano , Gianpaolo Candiani , Gianbattista Panzone
IPC分类号： A61K38/00 , A61P31/04 , C07K7/08 , C07K7/56 , C07K9/00 , C07K11/02 , C12P13/00
CPC分类号： C07K7/08 , C07K9/008
摘要： The invention regards a process for the production of ramoplanin-like derivatives of formula (I): RAMO-NC—CO—R (I), wherein the radical R represents a hydrocarbon radical and the portion RAMO-NH— represents deacylated ramoplanin, any of its factors or ramoplanose. The compound of Formula (I) are obtained by reacting a carboxylic acid R—COOH with deacylated ramoplanin, any of its factors or ramoplanose protected on the ornitine amino groups. New compounds wherein the hydrocarbon radical R is different form those characaterizing the ramoplanin and ramoplanose natural products and their tetrahydro-derivatives are calimed. The new compounds have the same or better antinfective activity, lower haemolytic effect and better tolerability profile than ramoplanin.
摘要翻译：本发明涉及制备式（I）的拉莫拉宁衍生物的方法：RAMO-NC-CO-R（I），其中基团R表示烃基，部分RAMO-NH-表示脱酰基拉莫拉宁，任何的因素或ramoplanose。式（I）化合物通过使羧酸R-COOH与脱酰基拉莫拉宁反应，其任何因子或在鸟氨酸上保护的拉米布糖反应得到。其中烃基R不同的新化合物形成了拉莫拉宁和拉莫拉诺天然产物及其四氢衍生物的特征加压。新化合物与拉莫拉宁相比具有相同或更好的抗感染活性，较低的溶血作用和更好的耐受性。

4. 发明授权

US07169890B2 Process for the production of ramoplanin-like amide derivatives 有权
标题翻译：拉莫拉宁类酰胺衍生物的制备方法
公开(公告)号：US07169890B2
公开(公告)日：2007-01-30
申请号：US10505881
申请日：2003-02-26
申请人： Romeo Ciabatti , Sonia Maffioli , Anna Checchia , Gabriella Romano , Gianpaolo Candiani , Gianbattista Panzone
发明人： Romeo Ciabatti , Sonia Maffioli , Anna Checchia , Gabriella Romano , Gianpaolo Candiani , Gianbattista Panzone
IPC分类号： C07K11/02
CPC分类号： C07K7/08 , C07K9/008
摘要： The invention regards a process for the production of ramoplanin-like derivatives of formula (I): RAMO-NC—CO—R (I), wherein the radical R represents a hydrocarbon radical and the portion RAMO-NH— represents deacylated ramoplanin, any of its factors or ramoplanose. The compound of Formula (I) are obtained by reacting a carboxylic acid R—COOH with deacylated ramoplanin, any of its factors or ramoplanose protected on the ornitine amino groups. New compounds wherein the hydrocarbon radical R is different form those characaterizing the ramoplanin and ramoplanose natural products and their tetrahydro-derivatives are calimed. The new compounds have the same or better antinfective activity, lower haemolytic effect and better tolerability profile than ramoplanin.
摘要翻译：本发明涉及制备式（I）的拉莫拉宁衍生物的方法：RAMO-NC-CO-R（I），其中基团R表示烃基，部分RAMO-NH-表示脱酰基拉莫拉宁，任何的因素或ramoplanose。式（I）化合物通过使羧酸R-COOH与脱酰基拉莫拉宁反应，其任何因子或在鸟氨酸上保护的拉米布糖反应得到。其中烃基R不同的新化合物形成了拉莫拉宁和拉莫拉诺天然产物及其四氢衍生物的特征加压。新化合物与拉莫拉宁相比具有相同或更好的抗感染活性，较低的溶血作用和更好的耐受性。

5. 发明授权

US06559312B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06559312B2
公开(公告)日：2003-05-06
申请号：US09731654
申请日：2000-12-08
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21122
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer of 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是0或1的整数; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，m是整数0。

6. 发明授权

US06552200B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06552200B2
公开(公告)日：2003-04-22
申请号：US09725259
申请日：2000-11-29
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21122
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1represented hydroxy, n is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基，n为整数0的第二个键。

7. 发明授权

US06479663B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06479663B2
公开(公告)日：2002-11-12
申请号：US09726625
申请日：2000-12-01
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21114
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy m is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的整数为0的第二个键。

8. 发明授权

US06348597B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06348597B2
公开(公告)日：2002-02-19
申请号：US09824788
申请日：2001-04-04
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21114
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 和其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，m是整数0。

9. 发明授权

US5378837A Process for preparing 2'-(diethylamino)rifamycin P (P/DEA) 失效
标题翻译：制备2' - （二乙基氨基）利福霉素P（P / DEA）
公开(公告)号：US5378837A
公开(公告)日：1995-01-03
申请号：US134515
申请日：1993-10-08
申请人： Gianbattista Panzone , Anacleto Gianantonio
发明人： Gianbattista Panzone , Anacleto Gianantonio
IPC分类号： A61K31/425 , A61K31/429 , A61P31/04 , A61P31/06 , A61P31/12 , C07D513/18 , A61K31/395
CPC分类号： C07D513/18
摘要： The present invention relates to a new one-pot process for preparing 2'-(diethylamino)rifamycin P and its 25-desacetyl derivative which consists in cyclizing 3-bromorifamycin S or its 25-desacetyl derivative, dissolved in dimethylformamide, with 1,1-diethylthiourea and reducing, without isolation, the obtained 1,2-quinonimine intermediate with a mild reducing agent.
摘要翻译：本发明涉及一种制备2' - （二乙基氨基）利福霉素P及其25-去乙酰基衍生物的新的一锅法，该方法包括将溶解在二甲基甲酰胺中的3-溴霉素S或其25-脱乙酰基衍生物环化，并将所得1,2-醌亚胺中间体用温和还原剂还原，不分离。

10. 发明授权

US06566526B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06566526B2
公开(公告)日：2003-05-20
申请号：US09725291
申请日：2000-11-29
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21122
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 to 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 ; R 1和R 2一起形成带有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是0至1的整数; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，为直链或支链; A为氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，m是整数0。

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