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1. 发明授权

US5602229A Pentapeptide antibiotics 失效
标题翻译：五肽抗生素
公开(公告)号：US5602229A
公开(公告)日：1997-02-11
申请号：US440868
申请日：1995-05-15
申请人： Adriano Malabarba , Romeo Ciabatti , J urgen K. Kettenring
发明人： Adriano Malabarba , Romeo Ciabatti , J urgen K. Kettenring
IPC分类号： A61K38/00 , A61P31/04 , C07K1/02 , C07K1/107 , C07K7/06 , C07K7/64 , C07K9/00 , C07K14/195 , C07K14/41
CPC分类号： C07K9/008 , A61K38/00
摘要： Pentapeptide antibiotics of the formula ##STR1## wherein W, Z, X.sub.1, X.sub.2 and T represent the relative portions of an antibiotic of the dalbaheptide group (glycopeptide antibiotics), Y represents a carboxyacid group, a functional derivative of a carboxyacid group or a hydroxymethyl group. The invention includes the salts of the above represented pentapeptide antibiotics with acids or bases as well as their inner salts.
摘要翻译：其中W，Z，X 1，X 2和T代表达巴己定组（糖肽抗生素）的抗生素的相对部分，Y代表羧酸基团，羧酸基团的官能衍生物或羟甲基组。本发明包括上述五肽抗生素与酸或碱的盐以及它们的内盐。

2. 发明授权

US5438117A Hexapeptides deriving from aglucoteicoplanin and a process for preparing them 失效
标题翻译：衍生自葡萄糖赤藓宁平凝素的六肽及其制备方法
公开(公告)号：US5438117A
公开(公告)日：1995-08-01
申请号：US264228
申请日：1994-06-23
申请人： Adriano Malabarba , Romeo Ciabatti
发明人： Adriano Malabarba , Romeo Ciabatti
IPC分类号： A61K38/00 , C07K9/00
CPC分类号： C07K9/008 , A61K38/00
摘要： Hexapeptides of formula (I) deriving from aglucoteicoplanin and their salts with acids and bases as well as their inner salts wherein R is hydrogen or a protecting ##STR1## group of the amino function. The products of formula (I), wherein R is hydrogen, possess antimicrobial activity in particular against coagulase-negative strains and some S. aureus and S. epidermidis strains which have low sensitivity toward teicoplanin. The hexapeptides are produced by reductive cleavage of aglucoteicoplanin with alkali metal borohydrides in the presence of a hydroalcoholic mixture as solvent.
摘要翻译：衍生自葡萄糖赤汤凝胶的式（I）的六肽及其与酸和碱的盐以及其内盐，其中R是氢或氨基官能团的保护基（I）基团。其中R为氢的式（I）的产物具有抗微生物活性，特别是抗凝固酶阴性菌株和一些对替考拉宁具有低敏感性的金黄色葡萄球菌和表皮葡萄球菌菌株。通过在作为溶剂的水醇混合物存在下，用碱金属硼氢化物还原性切割阴茎葡聚糖蛋白来制备六肽。

3. 发明授权

US5684127A Tetrapeptides deriving from dalbaheptide antibiotics 失效
公开(公告)号：US5684127A
公开(公告)日：1997-11-04
申请号：US468732
申请日：1995-06-06
申请人： Adriano Malabarba , Romeo Ciabatti
发明人： Adriano Malabarba , Romeo Ciabatti
IPC分类号： A61K38/00 , C07K5/107 , C07K9/00 , C07K1/02 , A61K38/07 , C07K5/10 , C07K5/12
CPC分类号： C07K9/008 , C07K5/1016 , A61K38/00 , Y02P20/55
摘要： Tetrapeptides of general formula (I) deriving from dalbaheptide antibiotics ##STR1## wherein: W and Z represent the relative portions of the aglycon of an antibiotic of the dalbaheptide group (aglucodalbaheptides); Y represents a carboxylic group or a functional derivative of said carboxylic group; R and R.sub.0 each independently represent amino or a protected amino group; R.sub.1 represents hydrogen or a protecting group of the carboxylic function; and its salts with acids and bases as well as its inner salts. A process for producing the tetrapeptides of formula (I) from the corresponding dalbaheptides and aglucodalbaheptides.

4. 发明授权

US5648456A Pentapeptide antibiotics 失效
标题翻译：五肽抗生素
公开(公告)号：US5648456A
公开(公告)日：1997-07-15
申请号：US454807
申请日：1995-05-31
申请人： Adriano Malabarba , Romeo Ciabatti , Jurgen Kurt Kettenring
发明人： Adriano Malabarba , Romeo Ciabatti , Jurgen Kurt Kettenring
IPC分类号： A61K38/00 , A61P31/04 , C07K1/02 , C07K1/107 , C07K7/06 , C07K7/64 , C07K9/00 , C07K14/195 , C07K14/41 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K9/008 , A61K38/00
摘要： Pentapeptide antibiotics of the formula ##STR1## wherein W, Z, X.sub.1, X.sub.2 and T represent the relative portions of an antibiotic of the dalbaheptide group (glyccpeptide antibiotics), Y represents a carboxyacid group, a functional derivative of said carboxyacid group or a hydroxymethyl group. The invention includes the salts of the above represented pentapeptide antibiotics with acids or bases as well as their inner salts.The compounds are obtained by reductive cleavage of the peptidic bond between the second and the third aminoacid of the seven aminoacid chain of dalbaheptides (glycopeptide antibiotics). The inventions concerns also the reductive cleavage process which implies using an alkali metal borohydride as the reagent. The compounds show antibacterial activity against staphylococcal and streptococcal strains.
摘要翻译：其中W，Z，X 1，X 2和T代表达巴庚肽组（glyccpeptide抗生素）的抗生素的相对部分，Y代表羧酸基团，所述羧酸基团的官能衍生物或羟甲基组。本发明包括上述五肽抗生素与酸或碱的盐以及它们的内盐。化合物通过还原性切割达巴庚啶（glycopeptide antibiotics）的七个氨基酸链的第二和第三个氨基酸之间的肽键来获得。本发明还涉及使用碱金属硼氢化物作为试剂的还原性裂解方法。该化合物对葡萄球菌和链球菌菌株具有抗菌活性。

5. 发明授权

US5644025A Tetrapeptides deriving from dalbaheptide antibiotics 失效
标题翻译：来自达贝己定抗生素的四肽
公开(公告)号：US5644025A
公开(公告)日：1997-07-01
申请号：US391378
申请日：1995-02-17
申请人： Adriano Malabarba , Romeo Ciabatti
发明人： Adriano Malabarba , Romeo Ciabatti
IPC分类号： A61K38/00 , C07K5/107 , C07K9/00 , C07K5/12 , C07K7/64
CPC分类号： C07K9/008 , C07K5/1016 , A61K38/00 , Y02P20/55
摘要： Tetrapeptides of general formula (I) deriving from dalbaheptide antibiotics ##STR1## wherein: W and Z represent the relative portions of the aglycon of an antibiotic of the dalbaheptide group (aglucodalbaheptides);Y represents a carboxylic group or a functional derivative of said carboxylic group;R and R.sub.0 each independently represent amino or a protected amino group;R.sub.1 represents hydrogen or a protecting group of the carboxylic function;and its salts with acids and bases as well as its inner salts.A process for producing the tetrapeptides of formula (I) from the corresponding dalbaheptides and aglucodalbaheptides.
摘要翻译：（I）衍生自达拉庚啶抗生素的通式（I）的四肽其中：W和Z代表达贝己定组（aglucodalbaheptides）的抗生素的糖苷配基的相对部分; Y表示所述羧基的羧基或官能衍生物; R和R 0各自独立地表示氨基或被保护的氨基; R1表示氢或羧基官能团的保护基; 及其与酸和碱的盐以及其内盐。从相应的达巴庚啶和氨基甜菜苷生产式（I）的四肽的方法。

6. 发明授权

US5869449A 38-decarboxy-38-hydroxymethyl derivatives of teiocoplanin antibiotics and a process for preparing them 失效
标题翻译： 38-脱羧-338-羟甲基衍生物的布立康宁抗生素及其制备方法
公开(公告)号：US5869449A
公开(公告)日：1999-02-09
申请号：US872461
申请日：1997-06-10
申请人： Adriano Malabarba , Romeo Ciabatti
发明人： Adriano Malabarba , Romeo Ciabatti
IPC分类号： A61K38/00 , A61P31/04 , C07K1/113 , C07K7/06 , C07K9/00 , A61K38/12 , C07K11/02
CPC分类号： C07K9/008 , A61K38/00 , Y02P20/55 , Y10S930/19
摘要： The present invention is directed to novel 38-decarboxy-38-hydroxymethyl derivatives of teicoplanin antiobiotics and a process for preparing them which includes submitted the corresponding lower alkyl ester precursor to a reduction reaction in the presence of an alkali metal borohydride. The compounds of the invention show an improved antibacterial activity against some clinical isolates of Staphylococci somewhat resistant to teicoplanin.The teicoplanin derivatives of the present invention are represented by the following formula: ##STR1## wherein: X represents hydroxymethyl;R represents hydrogen or --N�(C.sub.9 -C.sub.12)aliphatic acyl!-.beta.-D-2-deoxy-2-aminoglucopyranosyl;R.sub.1 represents hydrogen or N-acetyl-.beta.-D-2-deoxy-2-aminoglucopyranosyl;R.sub.2 represents hydrogen of alpha-D-mannopyranosyl;R.sub.3 represents hydrogen or a protecting group of the amino function; and the acid addition salts thereof; with the proviso that R.sub.1 represents hydrogen only when R and R.sub.2 are simultaneously hydrogen.
摘要翻译：本发明涉及替考拉宁抗生素的新型38-脱羧基-3-羟甲基衍生物及其制备方法，其包括在碱金属硼氢化物存在下将相应的低级烷基酯前体进行还原反应。本发明的化合物显示出对某些对替考拉宁耐药的葡萄球菌的一些临床分离物具有改善的抗菌活性。本发明的替考拉宁衍生物由下式表示：其中：X代表羟甲基; R代表氢或-N [（C 9 -C 12）脂族酰基]-β-D-2-脱氧-2-氨基吡喃葡萄糖基; R1代表氢或N-乙酰基-β-D-2-脱氧-2-氨基吡喃葡萄糖基; R2表示α-D-吡喃甘露糖基的氢; R3表示氢或氨基官能团的保护基; 及其酸加成盐; 条件是仅当R和R 2同时为氢时，R 1表示氢。

7. 发明授权

US5674840A Synthetic aglucodalbaheptide antibiotics 失效
标题翻译：合成抗菌素类抗生素
公开(公告)号：US5674840A
公开(公告)日：1997-10-07
申请号：US532629
申请日：1995-12-26
申请人： Adriano Malabarba , Romeo Ciabatti
发明人： Adriano Malabarba , Romeo Ciabatti
IPC分类号： A61K38/00 , A61K38/08 , A61K38/14 , A61P31/04 , C07K1/06 , C07K7/06 , C07K9/00
CPC分类号： C07K7/06 , C07K9/008 , Y02P20/55
摘要： Synthetic aglucodalbaheptides of formula (I) wherein W and Z, each independently, represent the relative portions of the aglycon of an antibiotic of the dalbaheptide group. Y represents a carboxylic group or a functional derivative of said carboxylic group; R and R.sub.1, each independently, represent hydrogen or a protecting group of the amino function. R.sub.2 represents hydrogen; and their salts with acid and bases as well as their inner salts. A process for producing the aglucodabaheptides of formula (I) and their use as medicaments.
摘要翻译： PCT No.PCT / EP94 / 01154 Sec。 371日期1995年12月26日第 102（e）日期1995年12月26日PCT 1994年4月14日PCT PCT。公开号WO94 / 26780 PCT 日期1994年11月24日式（I）的合成氨基甜菜苷类化合物其中W和Z各自独立地代表达那贝肽组抗生素的糖苷配基的相对部分。 Y表示所述羧基的羧基或官能衍生物; R和R 1各自独立地表示氢或氨基官能团的保护基。 R2表示氢; 和它们与酸和碱的盐以及它们的内盐。制备式（I）的吡啶并庚啶的方法及其作为药物的用途。

8. 发明授权

US5500410A Substituted alkylamide derivatives of teicoplanin 失效
标题翻译：替考拉宁的取代烷基酰胺衍生物
公开(公告)号：US5500410A
公开(公告)日：1996-03-19
申请号：US461208
申请日：1995-06-05
申请人： Adriano Malabarba , Pierfausto Seneci , Jurgen K. Kettenring , Romeo Ciabatti
发明人： Adriano Malabarba , Pierfausto Seneci , Jurgen K. Kettenring , Romeo Ciabatti
IPC分类号： C07K9/00 , A61K38/08 , A61K38/12 , A61K38/14
CPC分类号： C07K9/008
摘要： The present invention is directed to new C.sup.63 amide derivatives of teicoplanin wherein the amide moiety is derived from a di- or poly-alkylamine, and to a process for preparing them. The derivatives are prepared by reacting a teicoplanin-like product with an active ester forming reagent such as chloroacetonitrile and then contacting said active ester with the appropriate di- or poly-alkylamine. The amide derivatives of the invention are active against gram positive and gram negative bacteria.
摘要翻译：本发明涉及替考拉宁的新C63酰胺衍生物，其中酰胺部分衍生自二 - 或多 - 烷基胺，以及制备它们的方法。通过使替考拉宁样产物与活性酯形成试剂如氯乙腈反应制备衍生物，然后使所述活性酯与合适的二 - 或多烷基胺接触。本发明的酰胺衍生物对革兰氏阳性菌和革兰氏阴性菌具有活性。

9. 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。

10. 发明申请

US20090305953A1 DALBAVANCIN COMPOSITIONS FOR TREATMENT OF BACTERIAL INFECTIONS 审中-公开
标题翻译：用于治疗细菌感染的DALBAVANCIN组合物
公开(公告)号：US20090305953A1
公开(公告)日：2009-12-10
申请号：US12474438
申请日：2009-05-29
申请人： Luigi Colombo , Adriano Malabarba , Martin Stogniew
发明人： Luigi Colombo , Adriano Malabarba , Martin Stogniew
IPC分类号： A61K38/16 , A61P31/04
CPC分类号： A61K38/14 , A61K31/70 , A61K31/704 , A61K38/00 , A61K2300/00
摘要： The invention provides methods and compositions for treatment of bacterial infections. Methods of the invention include administration of a mixture of dalbavancin multimers and monomers for treatment of a bacterial infection, in particular a Gram-positive bacterial infection of skin and soft tissue. Compositions comprise a mixture of dalbavancin multimer and monomer and a stabilizer, such as dextrose.
摘要翻译：本发明提供了用于治疗细菌感染的方法和组合物。本发明的方法包括施用达巴万星多聚体和用于治疗细菌感染的单体的混合物，特别是皮肤和软组织的革兰氏阳性细菌感染。组合物包括达巴万星多聚体和单体以及稳定剂如葡萄糖的混合物。

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