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1. 发明授权

US07655676B2 Use of amide derivative of GE 2270 factor A3 for the treatment of acne 有权
标题翻译：使用GE 2270因子A3的酰胺衍生物治疗痤疮
公开(公告)号：US07655676B2
公开(公告)日：2010-02-02
申请号：US10518802
申请日：2003-06-06
申请人： Adriano Malabarba , Marco Cavaleri , Giorgio Mosconi , Daniela Jabes , Gabriela Romano
发明人： Adriano Malabarba , Marco Cavaleri , Giorgio Mosconi , Daniela Jabes , Gabriela Romano
IPC分类号： A61K31/44 , A01N43/78 , C07D277/60 , C07D417/00 , C07D513/00
CPC分类号： A61K38/12
摘要： Use of the compound of formula (I) and the pharmaceutically acceptable addition salts thereof for the manufacture of a medicament for topical treatment or 5 prevention of acne formula (I) wherein: R represents methoxymethyl, R1 represents methyl, Rz represents methyl, Y represents the group formula (II) The compound of formula (I) and the pharmaceutically acid addition salts thereof show selective activity against propionibacterium acne and are suitable for use in a method of treatment or prevention of acne.
摘要翻译：式（I）化合物及其药学上可接受的加成盐在制备用于局部治疗的药物或5防止痤疮配方（I）中的用途，其中：R表示甲氧基甲基，R1表示甲基，Rz表示甲基，Y表示基团式（II）式（I）化合物及其药学上可接受的酸加成盐显示对丙酸杆菌的选择性活性，适用于治疗或预防痤疮的方法。

2. 发明申请

US20080113902A1 Use of ramoplanin to treat diseases associated with the use of antibiotics 审中-公开
公开(公告)号：US20080113902A1
公开(公告)日：2008-05-15
申请号：US11906750
申请日：2007-10-03
申请人： Daniela Jabes , Timothy S. Leach , Richard F. Labaudiniere , Steven M. Rauscher , Giorgio Mosconi
发明人： Daniela Jabes , Timothy S. Leach , Richard F. Labaudiniere , Steven M. Rauscher , Giorgio Mosconi
IPC分类号： A61K38/14 , A61K38/12 , A61K31/573 , A61K31/405
CPC分类号： A61K45/06 , A61K31/573 , A61K31/58 , A61K38/16 , A61K2300/00
摘要： The invention features a method of treating or preventing a disease associated with the use of antibiotics in a patient in need thereof by administering to the patient ramoplanin in an amount and for a duration effective to treat said disease. The disease may be caused, for example, by the presence of a bacterium such as enterotoxin producing strains of C. difficile, C. perfringens, or S. aureus.

3. 发明授权

US07317001B2 Use of ramoplanin to treat diseases associated with the use of antibiotics 有权
标题翻译：使用拉莫拉宁治疗与使用抗生素相关的疾病
公开(公告)号：US07317001B2
公开(公告)日：2008-01-08
申请号：US10454998
申请日：2003-06-05
申请人： Daniela Jabes , Timothy S. Leach , Richard F. Labaudiniere , Steven M. Rauscher , Giorgio Mosconi
发明人： Daniela Jabes , Timothy S. Leach , Richard F. Labaudiniere , Steven M. Rauscher , Giorgio Mosconi
IPC分类号： A61K38/00
CPC分类号： A61K45/06 , A61K31/573 , A61K31/58 , A61K38/16 , A61K2300/00
摘要： The invention features a method of treating or preventing a disease associated with the use of antibiotics in a patient in need thereof by administering to the patient ramoplanin in an amount and for a duration effective to treat said disease. The disease may be caused, for example, by the presence of a bacterium such as enterotoxin producing strains of C. difficile, C. perfringens, or S. aureus.
摘要翻译：本发明的特征在于在有需要的患者中治疗或预防与使用抗生素相关的疾病的方法，其通过以有效治疗所述疾病的量和持续时间给予患者拉莫拉宁。该疾病可能是由于例如存在细菌如产生生产艰难梭菌，产气荚膜梭菌或金黄色葡萄球菌的肠毒素产生菌株引起的。

4. 发明申请

US20050032721A1 Methods of administering dalbavancin for treatment of skin and soft tissue infections 审中-公开
标题翻译：给予达巴万星治疗皮肤和软组织感染的方法
公开(公告)号：US20050032721A1
公开(公告)日：2005-02-10
申请号：US10942197
申请日：2004-09-15
申请人： Marco Cavaleri , Daniela Jabes , Timothy Henkel , Adriano Malabarba , Giorgio Mosconi , Martin Stogniew , Richard White
发明人： Marco Cavaleri , Daniela Jabes , Timothy Henkel , Adriano Malabarba , Giorgio Mosconi , Martin Stogniew , Richard White
IPC分类号： A61K31/70 , A61K31/704 , A61K38/12 , A61K38/14 , 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 dalbavancin for treatment of a bacterial infection, in particular an uncomplicated Gram-positive bacterial infection of skin and soft tissue. Dosing regimes include once weekly administration of dalbavancin, which often remains at therapeutic levels in the bloodstream for at least one week, providing prolonged therapeutic action against a bacterial infection.
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。本发明的方法包括给予达巴万星治疗细菌感染，特别是皮肤和软组织的不复杂革兰氏阳性细菌感染。给药方案包括每周一次给予达巴万星，达巴万星通常在血液中保持治疗水平至少一周，为细菌感染提供长时间的治疗作用。

5. 发明申请

US20100112091A1 USE OF RAMOPLANIN TO TREAT DISEASES ASSOCIATED WITH THE USE OF ANTIBIOTICS 审中-公开
标题翻译：使用RAMOPLANIN治疗与抗生素相关的疾病
公开(公告)号：US20100112091A1
公开(公告)日：2010-05-06
申请号：US12557099
申请日：2009-09-10
申请人： Daniela Jabes , Timothy S. Leach , Richard F. Labaudiniere , Steven M. Rauscher , Giorgio Mosconi
发明人： Daniela Jabes , Timothy S. Leach , Richard F. Labaudiniere , Steven M. Rauscher , Giorgio Mosconi
IPC分类号： A61K33/24 , A61K38/14 , A61P31/04
CPC分类号： A61K45/06 , A61K31/573 , A61K31/58 , A61K38/16 , A61K2300/00
摘要： The invention features a method of treating or preventing a disease associated with the use of antibiotics in a patient in need thereof by administering to the patient ramoplanin in an amount and for a duration effective to treat said disease. The disease may be caused, for example, by the presence of a bacterium such as enterotoxin producing strains of C. difficile, C. perfringens, or S. aureus.
摘要翻译：本发明的特征在于在有需要的患者中治疗或预防与使用抗生素相关的疾病的方法，其通过以有效治疗所述疾病的量和持续时间给予患者拉莫拉宁。该疾病可能是由于例如存在细菌如产生生产艰难梭菌，产气荚膜梭菌或金黄色葡萄球菌的肠毒素产生菌株引起的。

6. 发明授权

US06765003B1 3-Arylsulfonyl-2 (substituted methyl) propanoic acid derivatives as matrix metalloproteinase inhibitors 失效
标题翻译： 3-芳基磺酰基-2（取代甲基）丙酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US06765003B1
公开(公告)日：2004-07-20
申请号：US10030681
申请日：2002-04-09
申请人： Sergio Mantegani , Francesca Abrate , Pierluigi Bissolino , Paolo Cremonesi , Ettore Perrone , Daniela Jabes
发明人： Sergio Mantegani , Francesca Abrate , Pierluigi Bissolino , Paolo Cremonesi , Ettore Perrone , Daniela Jabes
IPC分类号： A61K3133
CPC分类号： C07D213/70 , C07C317/46 , C07C323/65 , C07D233/72 , C07D233/84 , C07D235/28 , C07D239/38 , C07D239/56 , C07D249/12 , C07D257/04 , C07D277/36 , C07D285/125 , C07D285/135 , C07D333/34
摘要： Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO—NH— or HO—, R1 is selected from phenyl, 4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (i.e., —NH—CO-Ph) and benzamido substituted on the terminal phenyl ring by C1-C4 alkyl, fluoro, chloro, cyano or C1-4 alkoxy; R2 is selected from (a) —S—Ar or —S—CH2—Ar wherein Ar is an aromatic moiety; (b) —O—Ar wherein Ar is as defined above; (c) —S-Het or —S—CH2-Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.
摘要翻译：作为式（I）的3-芳基磺酰基-2-甲基丙酸衍生物的化合物：其中X是HO-NH-或HO-，R1选自苯基，4-氯苯基，4-氟苯基，4-氰基苯基，苯甲酰氨基（即-NH-CO-Ph）和在末端苯环上被C1-C4烷基，氟，氯，氰基或C1-4烷氧基取代的苯甲酰氨基; R2选自（a）-S-Ar或-S-CH2-Ar，其中Ar是芳族部分; （b）-O-Ar，其中Ar定义如上; （c）-S-Het或-S-CH2-Het，其中Het是杂环; 和（d）2,5-二氧代-1-咪唑烷基或2,4-二氧代-1-咪唑啉基; 及其药学上可接受的盐; 对基质金属蛋白酶（MMPs）具有有效和选择性的抑制活性，因此可用于治疗和预防由MMP介导的疾病。

7. 发明授权

US06482827B1 Matrix metalloproteinase inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US06482827B1
公开(公告)日：2002-11-19
申请号：US09147798
申请日：1999-03-10
申请人： Marco Alpegiani , Pierluigi Bissolino , Francesca Abrate , Ettore Perrone , Riccardo Corigli , Daniela Jabes
发明人： Marco Alpegiani , Pierluigi Bissolino , Francesca Abrate , Ettore Perrone , Riccardo Corigli , Daniela Jabes
IPC分类号： A61K3116
CPC分类号： C07D213/74 , C07B2200/07 , C07C259/06 , C07C2601/08 , C07C2601/14 , C07D233/32 , C07D295/185 , C07D317/68 , C07D405/12
摘要： A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：作为式（I）的胺衍生物的化合物，其中W为-CNHOH或-COOH：R 1和R 2各自为氢或有机残基，R 3为有机基团，Q为仲或叔无环或环状酰氨基及其药学上可接受的盐，溶剂化物和水合物，是基质金属蛋白酶（MMPs）的抑制剂和从细胞释放肿瘤坏死因子-α（TNF）的抑制剂。因此，它们可用于预防，控制和治疗涉及MMP或TNF的疾病，特别是肿瘤和炎性疾病。还描述了其制备方法和含有它们的药物组合物。

8. 发明申请

US20050130914A1 Methods of administering dalbavancin for treatment of skin and soft tissue infections 审中-公开
标题翻译：给予达巴万星治疗皮肤和软组织感染的方法
公开(公告)号：US20050130914A1
公开(公告)日：2005-06-16
申请号：US10942604
申请日：2004-09-15
申请人： Marco Cavaleri , Daniela Jabes , Timothy Henkel , Adriano Malabarba , Giorgio Mosconi , Martin Stogniew , Richard White
发明人： Marco Cavaleri , Daniela Jabes , Timothy Henkel , Adriano Malabarba , Giorgio Mosconi , Martin Stogniew , Richard White
IPC分类号： A61K31/70 , A61K31/704 , A61K38/12 , A61K38/14 , 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 dalbavancin for treatment of a bacterial infection, in particular a Gram-positive bacterial complicated infection of skin and soft tissue. Dosing regimes include once weekly administration of dalbavancin, which often remains at therapeutic levels in the bloodstream for at least one week, providing prolonged therapeutic action against a bacterial infection.
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用于治疗细菌感染，特别是革兰氏阳性细菌复合皮肤和软组织感染。给药方案包括每周一次给予达巴万星，达巴万星通常在血液中保持治疗水平至少一周，为细菌感染提供长时间的治疗作用。

9. 发明授权

US06900175B2 Methods of administering dalbavancin for treatment of bacterial infections 有权
标题翻译：给予达巴万星治疗细菌感染的方法
公开(公告)号：US06900175B2
公开(公告)日：2005-05-31
申请号：US10714261
申请日：2003-11-14
申请人： Marco Cavaleri , Daniela Jabes , Timothy Henkel , Adriano Malabarba , Giorgio Mosconi , Martin Stogniew , Richard J. White
发明人： Marco Cavaleri , Daniela Jabes , Timothy Henkel , Adriano Malabarba , Giorgio Mosconi , Martin Stogniew , Richard J. White
IPC分类号： A61K31/70 , A61K31/704 , A61K38/12 , A61K38/14 , A61P31/04 , A61K38/16
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 dalbavancin for treatment of a bacterial infection, in particular a Gram-positive bacterial infection of skin and soft tissue. Dosing regimes include once weekly administration of dalbavancin, which often remains at therapeutic levels in the bloodstream for at least one week, providing prolonged therapeutic action against a bacterial infection.
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。本发明的方法包括给予达巴万星治疗细菌感染，特别是皮肤和软组织的革兰氏阳性细菌感染。给药方案包括每周一次给予达巴万星，达巴万星通常在血液中保持治疗水平至少一周，为细菌感染提供长时间的治疗作用。

10. 发明授权

US5480880A Penem derivatives 失效
标题翻译： Penem衍生物
公开(公告)号：US5480880A
公开(公告)日：1996-01-02
申请号：US972444
申请日：1993-04-09
申请人： Giuseppina Visentin , Franco Zarini , Daniela Jabes , Ettore Perrone , Costantino della Bruna , Marco Alpegiani
发明人： Giuseppina Visentin , Franco Zarini , Daniela Jabes , Ettore Perrone , Costantino della Bruna , Marco Alpegiani
IPC分类号： A61K31/43 , A61K31/431 , A61K31/44 , A61K31/675 , A61P31/04 , C07D499/88 , C07D499/883 , C07D499/893 , C07D499/897 , C07D499/00
CPC分类号： C07D499/88
摘要： The invention provides compounds of the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a negative charge or an ester residue; R is:a) --(CH.sub.2).sub.n --A--CO.sub.2 H, --(CH.sub.2)n--A--SO.sub.3 H or --(CH.sub.2).sub.n --A--PO.sub.3 H.sub.2, wherein n is either zero, one or two and A is a group --CH.dbd.CH-- (either E or Z), --OCH.sub.2 --, --SCH.sub.2 -- or --CHOH--;b) --(CH.sub.2).sub.n --PO.sub.3 H.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHCN, --(CH.sub.2).sub.n NHSO.sub.3 H, --(CH.sub.2).sub.n CONHSO.sub.2 CH.sub.3 or --(CH.sub.2).sub.n CONHSO.sub.2 CF.sub.3, wherein n is as defined above;c) --(CH.sub.2 S).sub.m --W--(CH.sub.2).sub.n Z, wherein W is an arylene group or a heterocyclediyl group, m is 0 or 1, n is as above defined, and Z represents CO.sub.2 H, PO.sub.3 H.sub.2, SO.sub.2 NHCN, NHSO.sub.3 H, CONHSO.sub.2 CH.sub.3 or CONHSO.sub.2 CF.sub.3 ;d) ##STR2## wherein Y is O or NH and X is NH, N--OH or N--O--(CH.sub.2).sub.n+1 COOH wherein n is as defined above; ore) --(CH.sub.2 S).sub.m --W', wherein W' is a heterocyclyl group convertible into an anion at physiological pH and m is as defined above.Compounds I, their salts and ester prodrugs have antibacterial activity.
摘要翻译： PCT No.PCT / EP92 / 01396 Sec。 371日期：1993年4月9日 102（e）日期1993年4月9日PCT提交1992年6月22日PCT公布。出版物WO93 / 00345 日本1993年1月7日。本发明提供通式Ⅰ（I）的化合物，其中R1是氢原子，负电荷或酯残基; R是：a） - （CH 2）n A-CO 2 H， - （CH 2）n A-SO 3 H或 - （CH 2）n A-PO 3 H 2，其中n是零，一个或两个，A是基团-CH = CH- E或Z），-OCH 2 - ， - CH 2 - 或-CHOH-; b） - （CH 2）n -PO 3 H 2， - （CH 2）n SO 2 NHCN， - （CH 2）n NHSO 3 H， - （CH 2）n CONHSO 2 CH 3或 - （CH 2）n CONHSO 2 CF 3，其中n如上所定义; c） - （CH 2 S）m W-（CH 2）n Z，其中W是亚芳基或杂环基，m是0或1，n如上所定义，Z代表CO 2 H，PO 3 H 2，SO 2 NHCN，NHSO 3 H，CONHSO 2 CH 3或CONHSO 2 CF 3 ; d）其中Y是O或NH，X是NH，N-OH或N-O-（CH 2）n + 1COOH，其中n如上定义; 或e） - （CH 2 S）m -W'，其中W'是在生理pH下可转化成阴离子的杂环基，m如上所定义。化合物I，其盐和酯前药具有抗菌活性。

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