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1. 发明授权

US06906205B2 Spiro and dispiro 1,2,4-trioxolane antimalarials 有权
标题翻译：螺和脱甲基-1,2,4-三恶烷抗疟药
公开(公告)号：US06906205B2
公开(公告)日：2005-06-14
申请号：US10742010
申请日：2003-12-19
申请人： Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile , Maniyan Padmanilayam , Yuangqing Tang , William N. Charman
发明人： Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile , Maniyan Padmanilayam , Yuangqing Tang , William N. Charman
IPC分类号： A61K31/335 , C07D323/02 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D417/06 , C07D417/12 , C07D491/10 , C07D491/20 , C07D493/10 , C07D495/10 , A61K31/357
CPC分类号： C07D405/06 , A61K31/335 , C07D323/02 , C07D405/12 , C07D405/14 , C07D413/10 , C07D417/06 , C07D417/12 , C07D491/10 , C07D493/10 , C07D495/10 , Y02A50/411 , Y02A50/423
摘要： A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.
摘要翻译：描述了使用螺或二脱氧-1,2,4-三恶烷来治疗疟疾，血吸虫病和癌症的方法和方法。优选的1,2,4-三氧杂环戊烷在三氧杂环戊烷基的一侧包括一个双金刚烷基，在三氧杂环戊烷基的另一侧包括一个螺环己基，因此螺环己基环优选在4位被取代。与青蒿素半合成衍生物相比，本发明的化合物在结构上简单，易于合成，无毒，对抗疟疾寄生虫有效。

2. 发明授权

US06825230B2 Spiro and dispiro 1,2,4-trixolane antimalarials 有权
标题翻译：螺和脱雄1,2,4-三环素抗疟药
公开(公告)号：US06825230B2
公开(公告)日：2004-11-30
申请号：US10642721
申请日：2003-08-18
申请人： Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile , Maniyan Padmanilayam , Yuanqing Tang , William N. Charman
发明人： Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile , Maniyan Padmanilayam , Yuanqing Tang , William N. Charman
IPC分类号： A61K31357
CPC分类号： C07D405/06 , A61K31/335 , A61K31/4747 , C07D323/02 , C07D405/12 , C07D417/06 , Y02A50/411 , Y02A50/423
摘要： A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.
摘要翻译：描述了使用螺或二脱氧-1,2,4-三恶烷来治疗疟疾，血吸虫病和癌症的方法和方法。优选的1,2,4-三氧杂环戊烷在三氧杂环戊烷基的一侧包括一个双金刚烷基，在三氧杂环戊烷基的另一侧包括一个螺环己基，因此螺环己基环优选在4位被取代。与青蒿素半合成衍生物相比，本发明的化合物在结构上简单，易于合成，无毒，对抗疟疾寄生虫有效。

3. 发明授权

US08067620B2 Dispiro 1,2,4-trioxolane antimalarials 有权
标题翻译： Dispiro 1,2,4-三恶烷抗疟药
公开(公告)号：US08067620B2
公开(公告)日：2011-11-29
申请号：US11930606
申请日：2007-10-31
申请人： Jonathan L. Vennerstrom , Yuxiang Dong , Susan A. Charman , Sergio Wittlin , Jacques Chollet , Darren J. Creek , Xiaofang Wang , Kamaraj Spiraghavan , Lin Zhou , Hugues Matile , William N. Charman
发明人： Jonathan L. Vennerstrom , Yuxiang Dong , Susan A. Charman , Sergio Wittlin , Jacques Chollet , Darren J. Creek , Xiaofang Wang , Kamaraj Spiraghavan , Lin Zhou , Hugues Matile , William N. Charman
IPC分类号： A61K31/357 , C07D323/02
CPC分类号： C07D493/10 , C07D323/02 , C07D405/12 , C07D413/12
摘要： A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.
摘要翻译：描述了使用螺或二脱氧-1,2,4-三恶烷来治疗疟疾，血吸虫病和癌症的方法和方法。优选的1,2,4-三氧杂环戊烷在三氧杂环戊烷基的一侧包括一个双金刚烷基，在三氧杂环戊烷基的另一侧包括一个螺环己基。与青蒿素半合成衍生物相比，本发明的化合物在结构上简单，易于合成，无毒，对抗疟疾寄生虫有效。本发明的化合物意外地提供了用于疟疾的单剂量治疗，以及针对其的预防活性。这些化合物对抗血吸虫病和癌症也是有效的。

4. 发明授权

US06486199B1 Spiro and dispiro 1,2,4-trioxolane antimalarials 有权
标题翻译：螺和脱甲基-1,2,4-三恶烷抗疟药
公开(公告)号：US06486199B1
公开(公告)日：2002-11-26
申请号：US09886666
申请日：2001-06-21
申请人： Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile
发明人： Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile
IPC分类号： A61K31335
CPC分类号： C07D405/12 , A61K31/335 , A61K31/357 , C07D323/02 , C07D405/14 , C07D491/10 , C07D493/10 , C07D495/10 , Y02A50/411 , Y02A50/423 , A61K2300/00
摘要： A means and method for treating malaria using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl or spiropiperidyl ring on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably functionalized or substituted at the 4-position or a spiropiperidyl ring that is functionalized or substituted at the nitrogen atom. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.
摘要翻译：描述了使用螺或二脱氧-1,2,4-三恶烷处理疟疾的方法和方法。优选的1,2,4-三氧杂环戊烷包括在三氧杂环戊烷基一侧的双金刚烷基，三氧杂环戊烷基的另一侧上的螺环己基或螺哌啶环，其中螺环己基环优选在4位官能化或取代或在氮原子上被官能化或取代的螺哌啶基环。与青蒿素半合成衍生物相比，本发明的化合物在结构上简单，易于合成，无毒，对抗疟疾寄生虫有效。

5. 发明授权

US07371778B2 Spiro and dispiro 1,2,4-trioxolane antimalarials 有权
标题翻译：螺和脱甲基-1,2,4-三恶烷抗疟药
公开(公告)号：US07371778B2
公开(公告)日：2008-05-13
申请号：US11121451
申请日：2005-05-04
申请人： Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile , Xiaofang Wang , Kamaraj Spiraghavan , William N. Chapman
发明人： Jonathan L. Vennerstrom , Yuxiang Dong , Jacques Chollet , Hugues Matile , Xiaofang Wang , Kamaraj Spiraghavan , William N. Chapman
IPC分类号： A61K31/357 , C07D323/02
CPC分类号： A61K31/335 , C07D323/02 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D417/06 , C07D417/12 , C07D491/10 , C07D493/10 , C07D495/10 , Y02A50/411 , Y02A50/423
摘要： A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.
摘要翻译：描述了使用螺或二脱氧-1,2,4-三恶烷来治疗疟疾，血吸虫病和癌症的方法和方法。优选的1,2,4-三氧杂环戊烷在三氧杂环戊烷基的一侧包括一个双金刚烷基，在三氧杂环戊烷基的另一侧包括一个螺环己基，因此螺环己基环优选在4位被取代。与青蒿素半合成衍生物相比，本发明的化合物在结构上简单，易于合成，无毒，对抗疟疾寄生虫有效。

6. 发明申请

US20090253797A1 CREATINE ORAL SUPPLEMENTATION USING CREATINE HYDROCHLORIDE SALT 有权
标题翻译：使用CREATINE盐酸盐进行口服口服补充
公开(公告)号：US20090253797A1
公开(公告)日：2009-10-08
申请号：US12477413
申请日：2009-06-03
申请人： Donald W. Miller , Jonathan L. Vennerstrom , Mark C. Faulkner
发明人： Donald W. Miller , Jonathan L. Vennerstrom , Mark C. Faulkner
IPC分类号： A61K31/198 , A61P21/06
CPC分类号： A61K31/198 , A23K20/105 , A23K20/142 , A23L33/10 , A23V2002/00 , A23V2250/306
摘要： Creatine oral supplementation using creatine hydrochloride salt, that may be added to a liquid or other beverage, or may be also used as an additive to solid oral dosages, or as a supplement, and which may be consumed by the athlete, or other party looking for immediate supplementation of strength, and may be added as a supplement within feed to livestock, in the veterinary area.
摘要翻译：使用肌酸盐酸盐的肌酸口服补充剂，其可以加入到液体或其它饮料中，或者也可以用作固体口服剂量或作为补充剂的添加剂，并且可以由运动员或其他方观察立即补充力量，并可在兽医领域作为畜牧饲料添加补充。

7. 发明申请

US20110172306A1 CREATINE ESTER PRONUTRIENT COMPOUNDS AND FORMULATIONS 审中-公开
标题翻译： CRETINE ESTER PRONUTRIENT COMPOUNDS AND FORMULATIONS
公开(公告)号：US20110172306A1
公开(公告)日：2011-07-14
申请号：US13069697
申请日：2011-03-23
申请人： Jonathan L. Vennerstrom , Donald W. Miller
发明人： Jonathan L. Vennerstrom , Donald W. Miller
IPC分类号： A61K31/221 , C07C257/14 , A61P3/02 , A61P25/16 , A61P25/00 , A61P21/00 , A61P9/00
CPC分类号： A23K20/142 , A23L33/10 , A23V2002/00 , A61K31/198 , A61K31/22 , A61K31/221 , A61K31/66 , A61K31/7004 , A23V2250/306
摘要： The present invention describes a method for providing creatine to an animal, which includes receiving a creatine ester by the animal. The creatine ester is suitable for being modified by the animal to form creatine.
摘要翻译：本发明描述了向动物提供肌酸的方法，其包括由动物接受肌酸酯。肌酸酯适合被动物修饰以形成肌酸。

8. 发明申请

US20110034421A1 CREATINE ORAL SUPPLEMENTATION USING CREATINE HYDROCHLORIDE SALT 有权
标题翻译：使用CREATINE盐酸盐进行口服口服补充
公开(公告)号：US20110034421A1
公开(公告)日：2011-02-10
申请号：US12909377
申请日：2010-10-21
申请人： Donald W. Miller , Jonathan L. Vennerstrom , Mark C. Faulkner
发明人： Donald W. Miller , Jonathan L. Vennerstrom , Mark C. Faulkner
IPC分类号： A61K31/195 , C07C279/14 , A61K31/661 , A61P21/06
CPC分类号： A61K31/198 , A23K20/10 , A23K20/105 , A23K20/142 , A23K50/10 , A23L2/52 , A23L33/10 , A23L33/175 , A23P10/40 , A23V2002/00 , A61K9/0053 , A61K31/185 , A61K31/195 , A61K31/661 , A23V2250/306 , A23V2200/33 , A23V2200/316
摘要： The present invention is directed to a third generation form of creatine, specifically a creatine hydrochloride salt, that drives significant improvements in muscle development and recovery due to its enhanced bio-availability, while causing fewer negative side effects compared to previous forms of creatine.
摘要翻译：本发明涉及第三代肌酸，特别是肌酸盐酸盐，其由于其增强的生物可利用性而促进肌肉发育和恢复的显着改善，同时与以前的肌酸形式相比，引起较少的负面副作用。

9. 发明授权

US5510356A Bisquinolines and processes for their production and use to treat malaria 失效
标题翻译：双喹啉及其生产和使用过程来治疗疟疾
公开(公告)号：US5510356A
公开(公告)日：1996-04-23
申请号：US770638
申请日：1991-10-03
申请人： Jonathan L. Vennerstrom
发明人： Jonathan L. Vennerstrom
IPC分类号： C07D215/46 , A61K31/47 , C07D215/38
CPC分类号： C07D215/46 , Y10S514/895
摘要： The present invention relates to new bisquinolines useful in the treatment of malaria and to processes for the production thereof. The invention also relates to methods for the treatment of malaria and, in particular, to the treatment of chloroquine-resistant strains of malaria. The compounds of the invention have the following formula: ##STR1## wherein R is a bivalent radical derived from an acyclic or cyclic hydrocarbon by removal of one hydrogen atom from each of two different carbon atoms. R' is hydrogen or lower alkyl (generally containing between about 1 and about 4 carbon atoms). X is hydrogen (--H), fluoro (--F), chloro (--Cl), bromo (--Br), trifluoromethyl (--CF.sub.3), cyano (--CN), or methylsulfoxide (--SOCH.sub.3). In its acyclic form, R generally contains at least two, and no more than about 12, carbon atoms and, preferably, is an unsubstituted straight or branched alkane. In its cyclic form, R contains at least three and, generally, no more than about eight carbon atoms and, preferably, is an unsubstituted cycloalkane. In a preferred embodiment, this invention relates to N,N-bis(7-chloroquinolin-4-yl)alkane diamines which are active against chloroquine-resistant malaria.The bisquinolines of this invention are useful agents against chloroquine-resistant malaria. .+-.-Trans-N.sup.1,N.sup.2 -Bis(7-chloro-quinolin-4-yl)cyclohexane-1,2-diamine is highly preferred for treatment of chloroquine-resistant malaria. This compound is one of the most potent antimalarials discovered to date and is clearly unique in its in vivo activity -80% and 100% cure rates being achieved at doses of 160 and 320 mg/kg, respectively.
摘要翻译：本发明涉及可用于治疗疟疾的新型双喹啉及其生产方法。本发明还涉及治疗疟疾的方法，特别是治疗氯喹抗性疟疾菌株。本发明的化合物具有下式：其中R是通过从两个不同的碳原子中的每一个除去一个氢原子而衍生自无环或环状烃的二价基团。 R'是氢或低级烷基（通常含有约1至约4个碳原子）。 X是氢（-H），氟（-F），氯（-Cl），溴（-Br），三氟甲基（-CF 3），氰基（-CN）或甲基亚砜（-SOCH 3）。在其无环形式中，R通常含有至少两个且不超过约12个碳原子，并且优选为未取代的直链或支链烷烃。在其环状中，R含有至少三个，通常不超过约八个碳原子，优选为未取代的环烷烃。在优选的实施方案中，本发明涉及对氯喹抗性疟疾具有活性的N，N-双（7-氯喹啉-4-基）烷烃二胺。本发明的双喹啉是抗氯喹抗性疟疾的有用药剂。 + / - 反式-N1，N2-双（7-氯 - 喹啉-4-基）环己烷-1,2-二胺是治疗氯喹抗性疟疾的方法。该化合物是迄今发现的最有效的抗疟药之一，其体内活性明显独特，分别在160和320mg / kg剂量下达到80％和100％的治愈率。

10. 发明授权

US08354450B2 Creatine oral supplementation using creatine hydrochloride salt 有权
公开(公告)号：US08354450B2
公开(公告)日：2013-01-15
申请号：US12909377
申请日：2010-10-21
申请人： Donald W. Miller , Jonathan L. Vennerstrom , Mark C. Faulkner
发明人： Donald W. Miller , Jonathan L. Vennerstrom , Mark C. Faulkner
IPC分类号： A61K31/195
CPC分类号： A61K31/198 , A23K20/10 , A23K20/105 , A23K20/142 , A23K50/10 , A23L2/52 , A23L33/10 , A23L33/175 , A23P10/40 , A23V2002/00 , A61K9/0053 , A61K31/185 , A61K31/195 , A61K31/661 , A23V2250/306 , A23V2200/33 , A23V2200/316
摘要： The present invention is directed to a third generation form of creatine, specifically a creatine hydrochloride salt, that drives significant improvements in muscle development and recovery due to its enhanced bio-availability, while causing fewer negative side effects compared to previous forms of creatine.

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