公开(公告)号：US08586625B2

公开(公告)日：2013-11-19

申请号：US12863271

申请日：2009-01-16

申请人： Anwar Rayan ,  Taher Nassar

发明人： Anwar Rayan ,  Taher Nassar

IPC分类号： A01N43/26 ,  A61K31/385 ,  C07D339/02 ,  C07D341/00 ,  C07D409/00 ,  A01N37/10 ,  A61K31/235

CPC分类号： A61K31/197 ,  A61K31/337 ,  A61K31/385 ,  A61K2300/00

摘要： A cytotoxic composition in which two moieties are conjugated covalently. A first moiety is a tax moiety, selected from the group consisting of taxanes, taxane derivatives, and or other closely relative compounds. A second moiety is an acid moiety selected from the group consisting of lipoic acid, acetylcysteine, compounds having an acidic group.

摘要翻译： 其中两个部分共价共轭的细胞毒性组合物。 第一部分是选自紫杉烷类，紫杉烷衍生物和/或其他密切相关的化合物的纳税部分。 第二部分是选自硫辛酸，乙酰半胱氨酸，具有酸性基团的化合物的酸部分。

公开(公告)号：US20130158070A1

公开(公告)日：2013-06-20

申请号：US13820678

申请日：2011-09-06

申请人： Taher Nassar

发明人： Taher Nassar

IPC分类号： C07D207/16 ,  C07C233/55 ,  C07D498/04 ,  C07D213/80 ,  C07D209/26 ,  C07C309/13 ,  C07C69/533

CPC分类号： A61K9/0014 ,  A61K31/401 ,  A61K31/616 ,  A61K47/542 ,  C07C69/58 ,  C07C69/587 ,  C07C233/55 ,  C07C309/15 ,  C07D207/16 ,  C07D209/26 ,  C07D213/80 ,  C07D498/04

摘要： Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and/or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis.

摘要翻译： 公开了衍生自不饱和脂肪酸和治疗活性剂的新型化学共轭物。 化学偶联物被设计和表征为COX-2和/或5-LOX抑制剂，并且可用于治疗炎性疾病和病症如阿尔茨海默病，帕金森病，哮喘，骨关节炎，类风湿性关节炎，疼痛，原发性痛经，克罗恩氏病 疾病和溃疡性结肠炎。

公开(公告)号：US20100144827A1

公开(公告)日：2010-06-10

申请号：US12519553

申请日：2007-12-20

申请人： Taher Nassar ,  Raiyn Nureldin ,  Anwar Rayan

发明人： Taher Nassar ,  Raiyn Nureldin ,  Anwar Rayan

IPC分类号： A61K31/401 ,  C07D207/16 ,  A61P35/00 ,  A61P1/00 ,  A61P37/06 ,  A61P29/00 ,  A61P3/10 ,  A61P9/00

CPC分类号： A61K47/55 ,  A61K47/542

摘要： The present application discloses conjugates comprising an aminic moiety covalently linked to a hydrophobic moiety, through an amidic bond, which are selective inhibitors of COX-2 enzyme and can be beneficially used in the treatment of various inflammatory disease or disorder and cancer.

摘要翻译： 本申请公开了包含通过酰胺键共价连接到疏水部分的氨基部分的缀合物，其是COX-2酶的选择性抑制剂，并且可以有利地用于治疗各种炎性疾病或病症和癌症。

公开(公告)号：US20100298421A1

公开(公告)日：2010-11-25

申请号：US12863271

申请日：2009-01-16

申请人： Anwar Rayan ,  Taher Nassar

发明人： Anwar Rayan ,  Taher Nassar

IPC分类号： A61K31/385 ,  C07D409/12 ,  A61P35/00

CPC分类号： A61K31/197 ,  A61K31/337 ,  A61K31/385 ,  A61K2300/00

摘要： A cytotoxic composition in which two moieties are conjugated covalently. A first moiety is a tax moiety, selected from the group consisting of taxanes, taxane derivatives, and or other closely relative compounds. A second moiety is an acid moiety selected from the group consisting of lipoic acid, acetylcysteine, compounds having an acidic group.

摘要翻译： 其中两个部分共价共轭的细胞毒性组合物。 第一部分是选自紫杉烷类，紫杉烷衍生物和/或其他密切相关的化合物的纳税部分。 第二部分是选自硫辛酸，乙酰半胱氨酸，具有酸性基团的化合物的酸部分。

公开(公告)号：US20050180997A1

公开(公告)日：2005-08-18

申请号：US10787122

申请日：2004-02-27

申请人： Simon Benita ,  Danny Goldstein ,  Taher Nassar ,  Ola Sader ,  Alain Razafindratsita ,  Gregory Lambert ,  Jean Kadouche

发明人： Simon Benita ,  Danny Goldstein ,  Taher Nassar ,  Ola Sader ,  Alain Razafindratsita ,  Gregory Lambert ,  Jean Kadouche

IPC分类号： A61K47/48 ,  A61K39/395

CPC分类号： A61K47/6905

摘要： A combination product comprising a positive oil in water emulsion wherein said emulsion comprises a compound presenting free NH2 groups, at its natural state, at the oil-water interface, and an antibody, wherein said compound is linked to said antibody by a heterobifunctional linker, linking said NH2 groups to SH groups on the antibody hinge region.

摘要翻译： 一种包含正水包油乳液的组合产品，其中所述乳液包含在其天然状态下在油 - 水界面处呈现游离NH 2基团的化合物和抗体，其中所述化合物连接 通过异双功能连接子与所述抗体连接，将所述NH 2基团与抗体铰链区上的SH基团连接。

公开(公告)号：US06692766B1

公开(公告)日：2004-02-17

申请号：US08750674

申请日：1997-02-28

申请人： Abraham Rubinstein ,  Raphael Radai ,  Michael Friedman ,  Boaz Tirosh ,  Muhammad Baluom ,  Taher Nassar

发明人： Abraham Rubinstein ,  Raphael Radai ,  Michael Friedman ,  Boaz Tirosh ,  Muhammad Baluom ,  Taher Nassar

IPC分类号： A61K910

CPC分类号： A61K9/2027 ,  A61K9/2013 ,  Y10S514/944 ,  Y10S514/946

摘要： The present invention relates to a controlled release drug delivery system comprising a drug which is susceptible to enzymatic degradation by enzymes present in the intestinal tract; and a polymeric matrix which undergoes erosion in the gastrointestinal tract comprising a hydrogel-forming polymer selected from the group consisting of (a) polymers which are themselves capable of enhancing absorption of said drug across the intestinal mucosal tissues and of inbihiting degradation of said drug by intestinal enzymes; and (b) polymers which are not themselves capable of enhancing absorption of said drug across the intestinal mucosal tissues and of inhibiting degradation of said drug by intestinal enzymes; wherein when the matrix comprises a polymer belonging to group (b) the delivery system further comprises an agent which enhances absorption of said drug across the intestinal mucosal tissues and/or an agent which inhibits degradation of said drug by intestinal enzymes and when the matrix comprises a polymer belonging to group (a) the delivery system optionally further comprises an agent which enhances absorption of said drug across the intestinal mucosal tissues and/or an agent which inhibits degradation of said drug by intestinal enzymes.

摘要翻译： 本发明涉及一种控释药物递送系统，其包含易于通过存在于肠道中的酶进行酶降解的药物; 以及在胃肠道中遭受侵蚀的聚合物基质，其包含选自以下的水凝胶形成性聚合物：（a）本身能够增强所述药物穿过肠粘膜组织的吸收的聚合物和所述药物的不利因素降解 肠酶; 和（b）本身不能增强所述药物穿过肠粘膜组织的吸收并且通过肠酶抑制所述药物降解的聚合物; 其中当所述基质包含属于组（b）的聚合物时，所述递送系统还包含增强所述药物穿过肠粘膜组织的吸收的试剂和/或通过肠酶抑制所述药物降解的药剂，并且当所述基质包含 属于（a）组的聚合物任选地还包含增强所述药物穿过肠粘膜组织的吸收的试剂和/或通过肠酶抑制所述药物降解的试剂。