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1. 发明授权

US10000509B2 Broad spectrum beta-lactamase inhibitors 有权
公开(公告)号：US10000509B2
公开(公告)日：2018-06-19
申请号：US15808204
申请日：2017-11-09
申请人： Gladius Pharmaceuticals Corporation
发明人： Larry Sutton , Sophia Yu
IPC分类号： C07D501/22 , C07D501/24 , C07D501/60 , A01N43/90 , A61K31/43
CPC分类号： C07D501/24 , A01N43/90 , C07D501/22 , C07D501/60
摘要： Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

2. 发明申请

US20160362422A1 BROAD SPECTRUM BETA-LACTAMASE INHIBITORS 有权
公开(公告)号：US20160362422A1
公开(公告)日：2016-12-15
申请号：US15247536
申请日：2016-08-25
申请人： GLADIUS PHARMACEUTICALS CORPORATION
发明人： Larry SUTTON , Sophia YU
IPC分类号： C07D501/24 , A01N43/90 , C07D501/22
CPC分类号： C07D501/24 , A01N43/90 , C07D501/22 , C07D501/60
摘要： Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

3. 发明授权

US09006421B2 Cephalosporin compositions and methods of manufacture 有权
标题翻译：头孢菌素组合物和制造方法
公开(公告)号：US09006421B2
公开(公告)日：2015-04-14
申请号：US14211526
申请日：2014-03-14
申请人： Cubist Pharmaceuticals, Inc.
发明人： Jan-Ji Lai , Pradip M. Pathare , Laxma Kolla , Adrien F. Soret
IPC分类号： C07D501/06 , C07D501/04 , C07F9/6561 , A61K31/546 , A61K31/433 , A61K31/426 , A61K31/41 , A61K31/545
CPC分类号： C07D501/59 , A61K31/41 , A61K31/426 , A61K31/433 , A61K31/545 , A61K31/546 , A61K31/675 , C07D501/04 , C07D501/06 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/56 , C07D501/57 , C07F9/65613
摘要： Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
摘要翻译：本文提供了一种合成头孢菌素抗生素化合物的方法，包括在单一步骤中将受保护的7-氨基转化为7-甲酰胺部分。

4. 发明授权

US08883772B2 Broad spectrum beta-lactamase inhibitors 有权
标题翻译：广谱β-内酰胺酶抑制剂
公开(公告)号：US08883772B2
公开(公告)日：2014-11-11
申请号：US12248760
申请日：2008-10-09
申请人： Larry Sutton , Sophia Yu
发明人： Larry Sutton , Sophia Yu
IPC分类号： A61K31/545 , C07D501/16 , A61K31/546 , C07D501/22 , C07D501/24
CPC分类号： C07D501/24 , A01N43/90 , C07D501/22 , C07D501/60
摘要： Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Compounds of the invention include those of formula: and pharmacologically acceptable salts thereof where variables Z, Y, M, y, n, R, R4, R5, R1 and R2 are as defined in the specification. M most generally represents a chemical moiety which is in conjugation with the nitrogen of the core beta-lactam ring system of the compound, such that one or more reactive species, e.g., electrophilic or nucleophilic sites are generated on modification of M which is initiated by cleavage of the beta-lactam ring. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions containing compounds of the invention for treatment or prevention of bacterial infections and methods of treatment of such infections employing such compounds.
摘要翻译：广谱β-内酰胺酶抑制剂。除了β-内酰胺酶抑制之外，某些抑制剂还表现出有效的抗生素活性。本发明的化合物被设计成使得在β-内酰胺环切割时产生可以使β-内酰胺酶失活的活性部分。本发明的化合物包括其中变量Z，Y，M，y，n，R，R 4，R 5，R 1和R 2如说明书中所定义的式的化学式及其药学上可接受的盐。 M最通常代表与化合物核心β-内酰胺环系统的氮共轭的化学部分，使得在修饰M时产生一个或多个反应性物质，例如亲电或亲核位点，其由M β-内酰胺环的裂解。还提供了制备β-内酰胺酶抑制剂和表现出这种抑制作用的β-内酰胺抗生素的方法。另外提供了含有用于治疗或预防细菌感染的本发明化合物的药物组合物，以及使用这些化合物治疗这种感染的方法。

5. 发明授权

US08173840B2 Compounds with high therapeutic index 有权
标题翻译：化合物治疗指数高
公开(公告)号：US08173840B2
公开(公告)日：2012-05-08
申请号：US11343557
申请日：2006-01-30
申请人： V. Ravi Chandran
发明人： V. Ravi Chandran
IPC分类号： C07K229/00
CPC分类号： A61K38/12 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616 , Y02A50/411
摘要： The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
摘要翻译：本发明涉及由与其上具有羟基，氨基，羧基或酰化衍生物的药物或药物结合的氨基酸组成的新型治疗化合物。这些高治疗指数衍生物与其制备的药物具有相同的效用，并且它们具有增强的药理学和药物性质。事实上，本发明的新型药物衍生物增强至少一种如本文所定义的治疗质量。本发明还涉及含有其的药物组合物。

6. 发明申请

US20110269689A1 HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS 审中-公开
标题翻译：高渗透组合物及其应用
公开(公告)号：US20110269689A1
公开(公告)日：2011-11-03
申请号：US13133021
申请日：2009-12-04
申请人： Chongxi Yu
发明人： Chongxi Yu
IPC分类号： A61K38/08 , A61K31/165 , C07C311/59 , A61K31/64 , C07J7/00 , A61K31/567 , C07J1/00 , A61K31/565 , C07D499/44 , A61K31/43 , C07D501/60 , A61K31/546 , C07K7/06 , C07C229/42 , A61K31/196 , A61K31/621 , C07C69/86 , C07C405/00 , A61K31/5575 , A61P25/28 , A61P31/04 , A61P35/00 , A61P17/00 , A61P3/10 , A61P3/04 , C07C237/20
CPC分类号： A61K31/352 , A61K47/54 , C07D207/34 , C07D209/42 , C07D211/34 , C07D215/18 , C07D231/14 , C07D277/56 , C07D295/088 , C07D313/14 , C07D417/04 , C07D491/048 , C07D501/22 , Y02A50/483
摘要： High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
摘要翻译：母体化合物的高渗透组成（HPC），能够穿透具有高渗透效率的生物屏障。在经过一个或多个生物屏障之后，HPC能够转化为母体药物或母体药物相关化合物如代谢物，因此可以对母体药物或母体药物相关化合物的条件进行处理。此外，HPC能够达到其母体药物或母体药物相关化合物可能无法进入或在目标区域提供足够浓度的区域，例如，NSAIA的HPC已经证明了治疗脱发的迹象。可以通过各种施用途径将HPC施用于受试者，例如局部递送至具有高浓度或系统地施用于生物学受试者的病症的作用部位并以更快的速率进入总体循环。

7. 发明申请

US20100069446A1 L-THREONINE DERIVATIVES OF HIGH THERAPEUTIC INDEX 有权
公开(公告)号：US20100069446A1
公开(公告)日：2010-03-18
申请号：US12557030
申请日：2009-09-10
申请人： V. Ravi Chandran
发明人： V. Ravi Chandran
IPC分类号： A61K31/44 , C07C229/02 , A61K31/22 , C07D307/93 , A61K31/343 , C07D213/80 , C07D233/54 , A61K31/4164 , A61P43/00
CPC分类号： A61K38/12 , A61K38/10 , A61K45/06 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616
摘要： The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

8. 发明申请

US20090131394A1 BROAD SPECTRUM BETA-LACTAMASE INHIBITORS 有权
公开(公告)号：US20090131394A1
公开(公告)日：2009-05-21
申请号：US12248760
申请日：2008-10-09
申请人： Larry Sutton , Sophia Yu
发明人： Larry Sutton , Sophia Yu
IPC分类号： A61K31/545 , C07D501/16 , A61K31/546
CPC分类号： C07D501/24 , A01N43/90 , C07D501/22 , C07D501/60
摘要： Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.
摘要翻译：广谱β-内酰胺酶抑制剂。除了β-内酰胺酶抑制之外，某些抑制剂还表现出有效的抗生素活性。本发明的化合物被设计成使得在β-内酰胺环切割时产生可以使β-内酰胺酶失活的活性部分。还提供了制备β-内酰胺酶抑制剂和表现出这种抑制作用的β-内酰胺抗生素的方法。另外提供了用于治疗或预防细菌感染的药物组合物和治疗这种感染的方法。

9. 发明申请

US20070191331A1 Crystalline forms of cefdinir potassium salt 审中-公开
标题翻译：头孢地尼钾盐的结晶形式
公开(公告)号：US20070191331A1
公开(公告)日：2007-08-16
申请号：US11591217
申请日：2006-10-31
申请人： Vinod Kansal , Dhirenkumar Mistry , Saurabh Pandey , Rakesh Patel , Shlomit Wizel , Jean Hildesheim
发明人： Vinod Kansal , Dhirenkumar Mistry , Saurabh Pandey , Rakesh Patel , Shlomit Wizel , Jean Hildesheim
IPC分类号： A61K31/545 , C07D501/14
CPC分类号： C07D501/22 , C07D501/00
摘要： The present invention encompasses the solid state chemistry of cefdinir potassium salt.
摘要翻译：本发明包括头孢地尼钾盐的固态化学。

10. 发明申请

US20060025399A1 Crystalline anhydrous cefdinir and crystalline cefdinir hydrates 审中-公开
公开(公告)号：US20060025399A1
公开(公告)日：2006-02-02
申请号：US11177202
申请日：2005-07-08
申请人： Devalina Law , Rodger Henry , Xiaochun Lou
发明人： Devalina Law , Rodger Henry , Xiaochun Lou
IPC分类号： A61K31/545 , C07D501/14
CPC分类号： A61K31/546 , C07D501/22 , Y02A50/473
摘要： A novel crystalline cefdinir anhydrate and novel crystalline cefdinir hydrates, ways to make them and use them, compositions comprising them and made with them, and methods of treatment using them are disclosed.

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