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1. 发明授权

US09029424B2 Orally bioavailable stilbenoids-compositions and therapeutic applications thereof 有权
标题翻译：口服生物可利用的扁桃体组合物及其治疗应用
公开(公告)号：US09029424B2
公开(公告)日：2015-05-12
申请号：US13847582
申请日：2013-03-20
申请人： Muhammed Majeed , Kalyanam Nagabhushanam , Jefferey Reinhardt , Samuel Manoharan Thomas , Krishnamani Jayaraman
发明人： Muhammed Majeed , Kalyanam Nagabhushanam , Jefferey Reinhardt , Samuel Manoharan Thomas , Krishnamani Jayaraman
IPC分类号： A61K31/09 , A01N31/14 , A61K31/075 , C07C39/21 , C07C43/23
CPC分类号： A61K31/09 , A01N31/14 , A61K31/05 , A61K31/075 , C07C39/20 , C07C39/21 , C07C43/23
摘要： Disclosed is a novel sirtuin modulating composition comprising an orally bioavailable SIRT-1 enhancing compound 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I. Also disclosed is an anti-acne composition comprising 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I. Further, a novel sirtuin modulating composition comprising an orally bioavailable SIRT-1 enhancing compound 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II is also disclosed.
摘要翻译：公开了一种新型的沉默调节蛋白调节组合物，其包含由STR＃I表示的口服生物可利用的SIRT-1增强化合物3,5-二甲氧基-3,4'-二羟基芪。还公开了包含由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋的抗痤疮组合物。此外，还公开了包含由STR＃II表示的口服生物可利用的SIRT-1增强化合物2,3'，5'，6-四羟基 - 反式 - 二苯乙烯的沉默调节蛋白调节组合物。

2. 发明申请

US20130217782A1 Orally bioavailable stilbenoids-Compositions and therapeutic applications thereof 审中-公开
标题翻译：口服生物可利用的扁桃体组合物及其治疗应用
公开(公告)号：US20130217782A1
公开(公告)日：2013-08-22
申请号：US13847582
申请日：2013-03-20
申请人： Muhammed Majeed , Kalyanam Nagabhushanam , Jefferey Reinhardt , Samuel Manoharan Thomas , Krishnamani Jayaraman
发明人： Muhammed Majeed , Kalyanam Nagabhushanam , Jefferey Reinhardt , Samuel Manoharan Thomas , Krishnamani Jayaraman
IPC分类号： A61K31/09
CPC分类号： A61K31/09 , A01N31/14 , A61K31/05 , A61K31/075 , C07C39/20 , C07C39/21 , C07C43/23
摘要： Disclosed is a novel sirtuin modulating composition comprising an orally bioavailable SIRT-1 enhancing compound 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I. Also disclosed is an anti-acne composition comprising 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I. Further, a novel sirtuin modulating composition comprising an orally bioavailable SIRT-1 enhancing compound 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II is also disclosed.
摘要翻译：公开了一种新型的沉默调节蛋白调节组合物，其包含由STR＃I表示的口服生物可利用的SIRT-1增强化合物3,5-二甲氧基-3,4'-二羟基芪。还公开了包含由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋的抗痤疮组合物。此外，还公开了包含由STR＃II表示的口服生物可利用的SIRT-1增强化合物2,3'，5'，6-四羟基 - 反式 - 二苯乙烯的沉默调节蛋白调节组合物。

3. 发明申请

US20100204340A1 ORALLY BIOAVAILABLE STILBENOIDS- COMPOSITIONS AND THERAPEUTIC APPLICATIONS THEREOF 审中-公开
标题翻译： ORALLY BIOAVAILABLE STILBENOIDS-COMPOSITIONS AND THERAPEUTIC APPLICATIONS WITHEROF
公开(公告)号：US20100204340A1
公开(公告)日：2010-08-12
申请号：US12499239
申请日：2009-07-08
申请人： Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Krishnamani Jayaraman
发明人： Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Krishnamani Jayaraman
IPC分类号： A61K31/09 , C07C43/243 , A61P3/04
CPC分类号： A61K31/09 , A61K31/05 , C07C39/21 , C07C43/23
摘要： A novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis, and nutraceutical and cosmeceutical compositions comprising 3,5-dimethoxy-3,4′-dihydroxystilbene useful for anti-obesity and anti-cellulite therapy, are disclosed. Further the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 and 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are disclosed. The enhancement of SIRT-1 polypeptide activity of the said compounds is unexpectedly much higher than resveratrol or its natural analog pterostilbene. Sirtuin modulating compositions comprising an orally bioavailable SIRT-1 enhancing compounds (i) 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I and (ii) 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are also disclosed. An additional embodiment, also discloses the enhanced anti-Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I and compositions thereof.
摘要翻译：由STR＃1代表的一种新颖，生物可利用和安全的扁桃体3,5-二甲氧基-3,4'-二羟基茋，具有意想不到的增强的防止伴随脂肪细胞末端分化的脂质积聚的能力，从而抑制脂肪形成，以及营养和药妆公开了包含可用于抗肥胖和抗脂肪团治疗的3,5-二甲氧基-3,4'-二羟基茋的组合物。另外，公开了由STR＃1代表的3,5-二甲氧基-3,4'-二羟基茋的增强的SIRT-1活化能力和由STR＃II表示的2,3'，5'，6-四羟基 - 反式 - 二苯乙烯。所述化合物的SIRT-1多肽活性的增强出乎意料地高于白藜芦醇或其天然类似物p芪烯。包含口服生物可利用的SIRT-1增强化合物（i）由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋和（ⅱ）2,3'，5'，6-四羟基 - 也公开了由STR＃II代表的二苯乙烯。另外的实施方案还公开了由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋的增强的抗丙酸杆菌痤疮活性及其组合物。

4. 发明授权

US09056074B2 Orally bioavailable stilbenoids—compositions and therapeutic applications thereof 有权
标题翻译：口服生物可利用的扁桃体组合物及其治疗应用
公开(公告)号：US09056074B2
公开(公告)日：2015-06-16
申请号：US13588409
申请日：2012-08-17
申请人： Krishnamani Jayaraman , Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas
发明人： Krishnamani Jayaraman , Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas
IPC分类号： A61K31/05 , A61K31/09 , C07C39/21 , C07C43/23
CPC分类号： A61K31/09 , A61K31/05 , C07C39/21 , C07C43/23
摘要： A novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis, and nutraceutical and cosmeceutical compositions comprising 3,5-dimethoxy-3,4′-dihydroxystilbene useful for anti-obesity and anti-cellulite therapy, are disclosed. Further the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 and 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are disclosed. The enhancement of SIRT-1 polypeptide activity of the said compounds is unexpectedly much higher than resveratrol or its natural analog pterostilbene. Sirtuin modulating compositions comprising an orally bioavailable SIRT-1 enhancing compounds (i) 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I and (ii) 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are also disclosed. An additional embodiment, also discloses the enhanced anti-Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I and compositions thereof.
摘要翻译：由STR＃1代表的一种新颖，生物可利用和安全的扁桃体3,5-二甲氧基-3,4'-二羟基茋，具有意想不到的增强的防止伴随脂肪细胞末端分化的脂质积聚的能力，从而抑制脂肪形成，以及营养和药妆公开了包含可用于抗肥胖和抗脂肪团治疗的3,5-二甲氧基-3,4'-二羟基茋的组合物。另外，公开了由STR＃1代表的3,5-二甲氧基-3,4'-二羟基茋的增强的SIRT-1活化能力和由STR＃II表示的2,3'，5'，6-四羟基 - 反式 - 二苯乙烯。所述化合物的SIRT-1多肽活性的增强出乎意料地高于白藜芦醇或其天然类似物p芪烯。包含口服生物可利用的SIRT-1增强化合物（i）由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋和（ⅱ）2,3'，5'，6-四羟基 - 也公开了由STR＃II代表的二苯乙烯。另外的实施方案还公开了由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋的增强的抗丙酸杆菌痤疮活性及其组合物。

5. 发明授权

US09050284B2 Orally bioavailable stilbenoids—compositions and therapeutic applications thereof 有权
标题翻译：口服生物可利用的扁桃体组合物及其治疗应用
公开(公告)号：US09050284B2
公开(公告)日：2015-06-09
申请号：US12367840
申请日：2009-02-09
申请人： Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Krishnamani Jayaraman
发明人： Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Krishnamani Jayaraman
IPC分类号： A61K31/05 , A61K31/075 , A61K31/09 , C07C39/20 , C07C39/21 , C07C43/23 , A01N31/14
CPC分类号： A61K31/09 , A01N31/14 , A61K31/05 , A61K31/075 , C07C39/20 , C07C39/21 , C07C43/23
摘要： Disclosed is a novel sirtuin modulating composition comprising an orally bioavailable SIRT-1 enhancing compound 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I. Also disclosed is an anti-acne composition comprising 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I. Further, a novel sirtuin modulating composition comprising an orally bioavailable SIRT-1 enhancing compound 2,3′,5′, 6-tetrahydroxy-trans-stilbene represented by STR#II is also disclosed.
摘要翻译：公开了一种新型的沉默调节蛋白调节组合物，其包含由STR＃I表示的口服生物可利用的SIRT-1增强化合物3,5-二甲氧基-3,4'-二羟基芪。还公开了包含由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋的抗痤疮组合物。此外，还公开了包含由STR＃II表示的口服生物可利用的SIRT-1增强化合物2,3'，5'，6-四羟基 - 反式 - 二苯乙烯的沉默调节蛋白调节组合物。

6. 发明申请

US20130017605A1 ORALLY BIOAVAILABLE STILBENOIDS- COMPOSITIONS AND THERAPEUTIC APPLICATIONS THEREOF 审中-公开
标题翻译： ORALLY BIOAVAILABLE STILBENOIDS-COMPOSITIONS AND THERAPEUTIC APPLICATIONS WITHEROF
公开(公告)号：US20130017605A1
公开(公告)日：2013-01-17
申请号：US13588409
申请日：2012-08-17
申请人： Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Krishnamani Jayaraman
发明人： Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Krishnamani Jayaraman
IPC分类号： C12N5/077
CPC分类号： A61K31/09 , A61K31/05 , C07C39/21 , C07C43/23
摘要： A novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by SIR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis, and nutraceutical and cosmeceutical compositions comprising, dimethoxy-3,4′-dihydroxystilbene useful for anti-obesity and anti-cellulite therapy, are disclosed. Further the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 and 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are disclosed. The enhancement of SIRT-1 polypeptide activity of the said compounds is unexpectedly much higher than resveratrol or its natural analog pterostilbene. Sirtuin modulating compositions comprising an orally bioavailable SIRT-1 enhancing compounds (i) 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I and (ii) 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by are also disclosed. An additional embodiment, also discloses the enhanced anti-Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I and compositions thereof.
摘要翻译：由SIR＃1代表的一种新颖的，生物可利用和安全的芪类化合物3,5-二甲氧基-3,4'-二羟基茋，具有意想不到的增强的防止脂肪细胞末端分化的脂质积累，从而抑制脂肪形成的能力，以及营养和药妆公开了包含用于抗肥胖和抗脂肪团治疗的二甲氧基-3,4'-二羟基茋的组合物。另外，公开了由STR＃1代表的3,5-二甲氧基-3,4'-二羟基茋的增强的SIRT-1活化能力和由STR＃II表示的2,3'，5'，6-四羟基 - 反式 - 二苯乙烯。所述化合物的SIRT-1多肽活性的增强出乎意料地高于白藜芦醇或其天然类似物p芪烯。包含口服生物可利用的SIRT-1增强化合物（i）由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋和（ⅱ）2,3'，5'，6-四羟基 - 所表示的二苯乙烯也被公开。另外的实施方案还公开了由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋的增强的抗丙酸杆菌痤疮活性及其组合物。

7. 发明申请

US20100204339A1 Orally Bioavailable Stilbenoids- Compositions and Therapeutic Applications Thereof 有权
标题翻译：口服生物可利用的扁桃体组合物及其治疗应用
公开(公告)号：US20100204339A1
公开(公告)日：2010-08-12
申请号：US12367840
申请日：2009-02-09
申请人： Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Krishnamani Jayaraman
发明人： Muhammed Majeed , Jeffrey Reinhardt , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Krishnamani Jayaraman
IPC分类号： A61K31/075 , C07C43/188 , C07C39/205 , A61P17/10
CPC分类号： A61K31/09 , A01N31/14 , A61K31/05 , A61K31/075 , C07C39/20 , C07C39/21 , C07C43/23
摘要： Disclosed is a novel sirtuin modulating composition comprising an orally bioavailable SIRT-1 enhancing compound 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I. Also disclosed is an anti-acne composition comprising 3,5-dimethoxy- 3,4′-dihydroxystilbenes represented by STR#I. Further, a novel sirtuin modulating composition comprising an orally bioavailable SIRT-1 enhancing compound 2,3′,5′, 6-tetrahydroxy-trans-stilbene represented by STR#II is also disclosed.
摘要翻译：公开了一种新型的沉默调节蛋白调节组合物，其包含由STR＃I表示的口服生物可利用的SIRT-1增强化合物3,5-二甲氧基-3,4'-二羟基芪。还公开了包含由STR＃I表示的3,5-二甲氧基-3,4'-二羟基茋的抗痤疮组合物。此外，还公开了包含由STR＃II表示的口服生物可利用的SIRT-1增强化合物2,3'，5'，6-四羟基 - 反式 - 二苯乙烯的沉默调节蛋白调节组合物。

8. 发明授权

US08394852B2 Inotilone derivatives as coherent biological response modifier (cBMR) 有权
标题翻译：联酮衍生物作为相关生物反应调节剂（cBMR）
公开(公告)号：US08394852B2
公开(公告)日：2013-03-12
申请号：US12872675
申请日：2010-08-31
申请人： Muhammed Majeed , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Subbalakshmi Prakash
发明人： Muhammed Majeed , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Subbalakshmi Prakash
IPC分类号： A61K31/34
CPC分类号： C07D307/58 , A23L31/00 , A23L33/10 , A61K31/341
摘要： Optimal compositions of derivatives of 5-methyl-3(2H)-furanone compounds and phenylpropanoid polyketides related to inotilone, that exert biological response modification in health and disease, and their method of preparation, are disclosed. Methods of treating degenerative conditions stemming from over-expression of inducible nitric oxide synthase (iNOS) using these compositions are also disclosed.
摘要翻译：本发明公开了5-甲基-3（2H） - 呋喃酮化合物和苯丙素类聚酮化合物与艾吐子酮有关的衍生物的最佳组合物，其在健康和疾病中发挥生物反应修饰及其制备方法。还公开了使用这些组合物治疗由诱导型一氧化氮合酶（iNOS）过表达引起的退行性病症的方法。

9. 发明授权

US07521580B1 Non-cytotoxic synthetic analogues of (1E, 6E)-1, 7-Bis (4-hydroxy-3-methoxyphenyl)-1, 6-heptadiene-3, 5-Dione and therapeutic applications thereof in cystic fibrosis 有权
标题翻译：（1E，6E）-1,7-双（4-羟基-3-甲氧基苯基）-1,6-庚二烯-3,5-二酮的非细胞毒性合成类似物及其在囊性纤维化中的治疗应用
公开(公告)号：US07521580B1
公开(公告)日：2009-04-21
申请号：US12032955
申请日：2008-02-18
申请人： Muhammed Majeed , Rajinder Kumar Bammi , Natarajan Sankaran , Subbalakshmi Prakash , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Susmitha Anand , Geetha Kanhangad-Gangadharan
发明人： Muhammed Majeed , Rajinder Kumar Bammi , Natarajan Sankaran , Subbalakshmi Prakash , Kalyanam Nagabhushanam , Samuel Manoharan Thomas , Susmitha Anand , Geetha Kanhangad-Gangadharan
IPC分类号： C07C49/203 , C07C49/215 , A61K31/12
CPC分类号： C07C49/248 , A61K31/12 , C07C45/74
摘要： Disclosed are novel, synthetic analogues of (1E,6E)-1,7-Bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione and the therapeutic applications for cystic fibrosis thereof in correcting altered CFTR trafficking and the associated impaired chloride (Cl−) ion transport. Introduction of branched-alkyl groups ortho to the phenolic groups gave rise to clinical compounds with vastly improved trafficking of delF508CFTR and with no cytotoxicity.
摘要翻译：公开了（1E，6E）-1,7-双（4-羟基-3-甲氧基苯基）-1,6-庚二烯-3,5-二酮的新型合成类似物，以及用于其改变的囊性纤维化的治疗应用 CFTR贩运和相关的氯化物（Cl - ）离子迁移。引入酚基团邻位的支链烷基产生临床化合物，其具有大大改善的delF508CFTR的运输并且没有细胞毒性。

10. 发明申请

US20160002141A1 SYNTHESIS OF CALEBIN-A AND ITS BIOLOGICALLY ACTIVE ANALOGS 有权
标题翻译： CALEBIN-A及其生物活性模拟物的合成
公开(公告)号：US20160002141A1
公开(公告)日：2016-01-07
申请号：US14320649
申请日：2014-07-01
申请人： Muhammed Majeed , Kalyanam Nagabhushanam , Anju Majeed , Samuel Manoharan Thomas
发明人： Muhammed Majeed , Kalyanam Nagabhushanam , Anju Majeed , Samuel Manoharan Thomas
IPC分类号： C07C67/10
CPC分类号： C07C67/10 , C07C67/11 , C07C69/732 , C07C69/734
摘要： Disclosed is a simple, economical, industrially scalable green synthetic process for Calebin-A and its biologically active analogs.
摘要翻译：公开了Calebin-A及其生物活性类似物的简单，经济，可工业可扩展的绿色合成方法。

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