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1. 发明申请

WO2014204872A9 COMPOSITION AND METHOD FOR INHIBITION OF PKNG FROM MYCOBACTERIUM TUBERCULOSIS 审中-公开
标题翻译：用于抑制来自MYCOBACTERIUM TUBCCOSOS的PKNG的组合物和方法
公开(公告)号：WO2014204872A9
公开(公告)日：2015-02-12
申请号：PCT/US2014042592
申请日：2014-06-16
申请人： COMPLEXA INC
发明人： BATTHYANY DIGHIERO CARLOS IGNACIO , DURAN ROSARIO
IPC分类号： A61K31/20 , A61K35/74 , A61P29/00 , A61P35/00
CPC分类号： A61K31/201

2. 发明申请

WO2014204872A2 COMPOSITION AND METHOD FOR INHIBITION OF PKNG FROM MYCOBACTERIUM TUBERCULOSIS 审中-公开
标题翻译：用于抑制来自MYCOBACTERIUM TUBCCOSOS的PKNG的组合物和方法
公开(公告)号：WO2014204872A2
公开(公告)日：2014-12-24
申请号：PCT/US2014/042592
申请日：2014-06-16
申请人： COMPLEXA, INC.
发明人： BATTHYANY DIGHIERO, Carlos, Ignacio , DURAN, Rosario
CPC分类号： A61K31/201
摘要： PknG from Mycobacterium tuberculosis is a Ser/Thr protein kinase that regulates key metabolic processes within the bacterial cell as well as signaling pathways from the infected host cell. This multi-domain protein has a conserved canonical kinase domain with N- and C-terminal flanking regions of unclear functional roles. The N-terminus harbors a rubredoxin-like domain (Rbx), a bacterial protein module characterized by an iron ion coordinated by four cysteine residues. Disruption of Rbx-metal binding site by simultaneous mutations of all the key cysteine residues significantly impairs PknG activity. This encouraged us to evaluate the effect of a nitro- fatty acid (9- and 10-nitro-octadeca-9-cis-enoic acid; OA-NO 2 ) on PknG activity. Fatty acid nitroalkenes are electrophilic species produced during inflammation and metabolism that react with nucleophilic residues of target proteins (i.e. Cys and His), modulating protein functions and subcellular distribution in a reversible-manner. In accordance with the present invention, administration of OA-NO 2 inhibits kinase activity by covalently adducting PknG outside its catalytic domain. Mass spectrometry-based analysis established that cysteines located at Rbx are the specific targets of the nitroalkene. Cys-nitroalkylation is a Michael addition reaction typically reverted by thiols. However, the reversible OA-NO 2 mediated nitroalkylation of the kinase results in an irreversible inhibition of PknG. Cys adduction by OA-NO 2 induced iron release from the Rbx domain, revealing a new strategy for the specific inhibition of PknG. Altogether our results highlight the relevance of Rbx domain as an interesting new target for PknG inhibition. In addition, the reactivity of electrophilic fatty acids towards Rbx-Cys points to its potential as modulators of critical cell signaling activities and as model molecules for specific PknG inhibitors development.
摘要翻译：来自结核分枝杆菌的PknG是一种Ser / Thr蛋白激酶，其调节细菌细胞内的关键代谢过程以及来自受感染宿主细胞的信号传导途径。该多结构域蛋白具有保守的规范激酶结构域，具有不明确功能作用的N-和C-末端侧翼区。 N末端含有一个rubredoxin样结构域（Rbx），一个细胞蛋白模块，其特征是由四个半胱氨酸残基配位的铁离子。通过所有关键半胱氨酸残基的同时突变破坏Rbx-金属结合位点显着损害PknG活性。这促使我们评估硝基脂肪酸（9-和10-硝基 - 十八碳-9-顺式 - 烯酸; OA-NO2）对PknG活性的影响。脂肪酸硝基烯烃是在炎症和代谢期间产生的亲核物质，其与靶蛋白（即Cys和His）的亲核残基反应，以可逆方式调节蛋白质功能和亚细胞分布。根据本发明，OA-NO2的施用通过在其催化结构域外共价加成PknG来抑制激酶活性。基于质谱法的分析表明，位于Rbx的半胱氨酸是硝基烯烃的具体目标。 Cys-硝基烷基化是通常由硫醇还原的迈克尔加成反应。然而，可逆的OA-NO2介导的激酶的硝基烷基化导致PknG的不可逆抑制。通过OA-NO2诱导的Cys诱导诱导铁从Rbx结构域的释放，揭示了PknG特异性抑制的新策略。总之，我们的研究结果突出了Rbx结构域作为PknG抑制的一个有趣的新目标的相关性。此外，亲电脂肪酸对Rbx-Cys的反应性指示其作为关键细胞信号传导活性的调节剂的潜力，并且作为特异性PknG抑制剂发育的模型分子。

3. 发明申请

WO2017059451A1 PREVENTION, TREATMENT AND REVERSAL OF DISEASE USING THERAPEUTICALLY EFFECTIVE AMOUNTS OF ACTIVATED FATTY ACIDS 审中-公开
标题翻译：使用激活的脂肪酸的治疗有效量的预防，治疗和逆转疾病
公开(公告)号：WO2017059451A1
公开(公告)日：2017-04-06
申请号：PCT/US2016/055206
申请日：2016-10-03
申请人： COMPLEXA, INC.
发明人： JORKASKY, Diane
IPC分类号： A61K31/20 , C07F9/02 , C11D1/28
CPC分类号： A61K31/201
摘要： Various embodiments of this invention are directed to pharmaceutical compositions and methods for treating diseases, including focal segmental glomerulosclerosis or pulmonary arterial hypertension. The compositions of such embodiments include activated fatty acids such as alkyl substituted fatty acids, keto fatty acids and nitro fatty acids. The methods of various embodiments include administering an effective amount of 10-nitro-9(E)-octadec-9-enoic acid to treat such diseases.
摘要翻译：本发明的各种实施方案涉及用于治疗疾病的药物组合物和方法，包括局灶性节段性肾小球硬化或肺动脉高压。这些实施方案的组合物包括活性脂肪酸，例如烷基取代的脂肪酸，酮脂肪酸和硝基脂肪酸。各种实施方案的方法包括施用有效量的10-硝基-9（E） - 十八碳-9-烯酸以治疗这些疾病。

4. 发明申请

WO2012006014A3 MULTI-COMPONENT PHARMACEUTICALS FOR TREATING DIABETES 审中-公开
标题翻译：用于治疗糖尿病的多组分药物
公开(公告)号：WO2012006014A3
公开(公告)日：2012-05-10
申请号：PCT/US2011042011
申请日：2011-06-27
申请人： MILLER RAYMOND A , COMPLEXA INC
发明人： MILLER RAYMOND A
IPC分类号： A61K31/201 , A61K31/20 , A61K31/202 , A61P3/00 , A61P3/10
CPC分类号： A61K31/201 , A61K31/4439 , A61K38/28 , A61K45/06 , A61K2300/00
摘要： Activated fatty acids, pharmaceutical composition compositions including activated fatty acids, methods for using activated fatty acids to treat diabetes, and methods for preparing activated fatty acids are provided herein.
摘要翻译：活性脂肪酸，包括活性脂肪酸的药物组合物组合物，使用活性脂肪酸治疗糖尿病的方法，以及制备活性脂肪酸的方法。

5. 发明申请

WO2015073527A1 NITROALKENE TOCOPHEROLS AND ANALOGS THEREOF FOR USE IN THE TREATMENT AND PREVENTION OF INFLAMMATION RELATED CONDITIONS 审中-公开
标题翻译： NITROALKENE TOCOPHEROLS及其类似物用于治疗和预防相关病症
公开(公告)号：WO2015073527A1
公开(公告)日：2015-05-21
申请号：PCT/US2014/065203
申请日：2014-11-12
申请人： COMPLEXA, INC.
发明人： BATTHYANY DIGHIERO, Carlos, Ignacio , LOPEZ GONZALEZ, Gloria, Virginia
IPC分类号： C07D311/74 , A61K31/35 , A61P29/00
CPC分类号： C07D311/72 , C07D311/66 , G01N2800/52 , G01N2800/7095
摘要： Within the scope of the present invention is a new pharmacological strategy for the treatment of atherosclerosis based on the main pathogenic role that low density lipoproteins and chronic inflammation play in atherogenesis. This pharmacological approach implies that the hybrid compound would be selectively incorporated into the lipoproteins particles during the normal metabolism and due to the presence of the chromanol structure of tocopherol. Once the nitroalkene-vitamin E-analog is incorporated into the LDL, this lipoprotein will carry it all over the body, including the atherosclerotic lesions, where the hybrid compound will be able to exert the potent anti-inflammatory and anti-atherogenic properties similar to nitrated fatty acids but without the disadvantages of β-oxidation and lack of control over the targeting and localization of the compound.
摘要翻译：在本发明的范围内，基于低密度脂蛋白和慢性炎症在动脉粥样硬化形成中发挥的主要致病作用，是治疗动脉粥样硬化的新的药理学策略。这种药理学方法意味着杂合化合物将在正常代谢期间选择性地并入脂蛋白颗粒中，并且由于存在生育酚的色原烷醇结构。一旦硝基烯 - 维生素E类似物掺入低密度脂蛋白，该脂蛋白将其全身携带，包括动脉粥样硬化病变，其中杂交化合物将能够发挥有效的抗炎和抗动脉粥样硬化性质，类似于硝酸脂肪酸，但没有β-氧化的缺点，并且对化合物的靶向和定位缺乏控制。

6. 发明申请

WO2012099557A3 FATTY ACID INHIBITORS 审中-公开
标题翻译：脂肪酸抑制剂
公开(公告)号：WO2012099557A3
公开(公告)日：2012-10-26
申请号：PCT/US2010055100
申请日：2010-11-02
申请人： COMPLEXA INC , BRANCHAUD BRUCE
发明人： BRANCHAUD BRUCE
IPC分类号： A61K31/185 , A61K31/336 , A61K31/337 , A61K31/70
CPC分类号： C07D303/48 , C07C57/03 , C07C205/55 , C07C2601/02 , C07D203/08 , C07D205/04 , C07D303/38 , C07D305/04 , C07D305/06 , C07D305/08 , C07D331/02 , C07D331/04
摘要： Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.
摘要翻译：本文提供了脂肪酸抑制剂，包括脂肪酸抑制剂的药物组合物，使用脂肪酸抑制剂治疗各种疾病的方法以及制备脂肪酸抑制剂的方法。

7. 发明申请

WO2009134383A3 VINYL SUBSTITUTED FATTY ACIDS 审中-公开
标题翻译： VINYL替代脂肪酸
公开(公告)号：WO2009134383A3
公开(公告)日：2010-01-21
申请号：PCT/US2009002628
申请日：2009-04-30
申请人： COMPLEXA INC , FREEMAN BRUCE A , BRANCHAUD BRUCE
发明人： FREEMAN BRUCE A , BRANCHAUD BRUCE
IPC分类号： C07C205/50 , A61K31/201 , A61P7/00 , A61P9/00 , A61P13/00 , A61P15/00 , A61P17/00 , A61P19/00 , A61P25/00
CPC分类号： C07C205/50
摘要： Activated fatty acids, pharmaceutical compositions including activated fatty acids, methods for using activated fatty acids to treat a variety of diseases, and methods for preparing activated fatty acids are provided herein.
摘要翻译：本文提供活性脂肪酸，包括活性脂肪酸的药物组合物，使用活性脂肪酸治疗各种疾病的方法和制备活性脂肪酸的方法。

8. 发明申请

WO2013055899A3 COMPOSITIONS USEFUL IN TREATING NEPHROPATHY AND METHODS FOR PREPARATION OF SAME 审中-公开
标题翻译：用于治疗恶性肿瘤的组合物及其制备方法
公开(公告)号：WO2013055899A3
公开(公告)日：2013-10-31
申请号：PCT/US2012059722
申请日：2012-10-11
申请人： COMPLEXA INC , CUSHING DANIEL JOSEPH
发明人： CUSHING DANIEL JOSEPH
IPC分类号： A61K31/201 , A61K31/4178 , A61K49/04 , A61P35/00
CPC分类号： A61K31/201 , A61K31/202 , A61K31/401 , A61K31/4184 , A61K33/24 , A61K45/06 , A61K49/0438 , A61K49/103 , A61K49/106 , A61N5/10 , C07H13/06 , A61K2300/00
摘要： Activated fatty acids, pharmaceutical composition compositions including activated fatty acids, methods for using activated fatty acids to treat nephropathy, and methods for preparing activated fatty acids are provided herein.
摘要翻译：本文提供活性脂肪酸，包括活性脂肪酸的药物组合物组合物，使用活性脂肪酸治疗肾病的方法和制备活性脂肪酸的方法。

9. 发明申请

WO2013055899A2 COMPOSITIONS USEFUL IN TREATING NEPHROPATHY AND METHODS FOR PREPARATION OF SAME 审中-公开
标题翻译：用于治疗肾病的组合物及其制备方法
公开(公告)号：WO2013055899A2
公开(公告)日：2013-04-18
申请号：PCT/US2012/059722
申请日：2012-10-11
申请人： COMPLEXA, INC. , CUSHING, Daniel, Joseph
发明人： CUSHING, Daniel, Joseph
CPC分类号： A61K31/201 , A61K31/202 , A61K31/401 , A61K31/4184 , A61K33/24 , A61K45/06 , A61K49/0438 , A61K49/103 , A61K49/106 , A61N5/10 , C07H13/06 , A61K2300/00
摘要： Activated fatty acids, pharmaceutical composition compositions including activated fatty acids, methods for using activated fatty acids to treat nephropathy, and methods for preparing activated fatty acids are provided herein.
摘要翻译：本文提供了活化的脂肪酸，包括活化的脂肪酸的药物组合物组合物，使用活化的脂肪酸治疗肾病的方法以及制备活化的脂肪酸的方法。

10. 发明申请

WO2012099557A2 FATTY ACID INHIBITORS 审中-公开
标题翻译：脂肪酸抑制剂
公开(公告)号：WO2012099557A2
公开(公告)日：2012-07-26
申请号：PCT/US2010/055100
申请日：2010-11-02
申请人： COMPLEXA, INC . , BRANCHAUD, Bruce
发明人： BRANCHAUD, Bruce
IPC分类号： A61K31/185 , A61K31/336 , A61K31/337 , A61K31/70
CPC分类号： C07D303/48 , C07C57/03 , C07C205/55 , C07C2601/02 , C07D203/08 , C07D205/04 , C07D303/38 , C07D305/04 , C07D305/06 , C07D305/08 , C07D331/02 , C07D331/04
摘要： Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.
摘要翻译：本文提供了脂肪酸抑制剂，包括脂肪酸抑制剂的药物组合物，使用脂肪酸抑制剂治疗各种疾病的方法以及制备脂肪酸抑制剂的方法。

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