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1. 发明申请

US20080312140A1 Compositions and Methods for Preventing or Treating Hiv Infection 审中-公开
标题翻译：预防或治疗感染的组合物和方法
公开(公告)号：US20080312140A1
公开(公告)日：2008-12-18
申请号：US11916519
申请日：2006-06-22
申请人： Chaim Gilon , Shira Cohen , Christian Devaux , Laurence Briant-Longuet , Martine Bardy
发明人： Chaim Gilon , Shira Cohen , Christian Devaux , Laurence Briant-Longuet , Martine Bardy
IPC分类号： A61K38/02 , C07K2/00 , A61P31/18
CPC分类号： C07K5/1008 , C07K5/06078 , C07K14/70514
摘要： The present invention is directed to compositions and methods of preventing for treating a retroviral infection, more particularly an HIV (human immunodeficiency virus) infection, and even more particularly an HIV-1 infection. The compositions and methods involve molecules that mimic the active site of the human CD4 protein.
摘要翻译：本发明涉及预防治疗逆转录病毒感染，特别是HIV（人类免疫缺陷病毒）感染，甚至更特别是HIV-1感染的组合物和方法。组合物和方法涉及模拟人CD4蛋白的活性位点的分子。

2. 发明授权

US08658603B2 Compositions and methods for inducing an immune response 有权
标题翻译：用于诱导免疫应答的组合物和方法
公开(公告)号：US08658603B2
公开(公告)日：2014-02-25
申请号：US13331354
申请日：2011-12-20
申请人： Joseph Holoshitz , Song Ling , Xiujun Pi , Denise de Almeida , Chaim Gilon , Amnon Hoffman
发明人： Joseph Holoshitz , Song Ling , Xiujun Pi , Denise de Almeida , Chaim Gilon , Amnon Hoffman
IPC分类号： A61K38/12
CPC分类号： A61K39/00 , A61K39/0011 , A61K39/02 , A61K39/04 , A61K39/39 , A61K2039/55566 , A61K2039/57 , C07K7/06 , C07K14/70539
摘要： The present invention provides compositions and methods for inducing an immune response in a subject. In particular, the present invention provides compositions comprising immunostimulatory ligands (ISL) and methods of inducing an immune response in a subject therewith. Compositions and methods of the present invention find use in, among other things, clinical (e.g. therapeutic and preventative medicine (e.g., vaccination)) and research applications.
摘要翻译：本发明提供了用于在受试者中诱导免疫应答的组合物和方法。特别地，本发明提供包含免疫刺激配体（ISL）的组合物以及在其受试者中诱导免疫应答的方法。本发明的组合物和方法尤其可用于临床（例如治疗和预防性药物（例如疫苗接种））和研究应用。

3. 发明授权

US6117974A Libraries of backbone-cyclized peptidomimetics 失效
标题翻译：骨架环化肽模拟物库
公开(公告)号：US6117974A
公开(公告)日：2000-09-12
申请号：US569042
申请日：1995-12-07
申请人： Chaim Gilon , Vered Hornik
发明人： Chaim Gilon , Vered Hornik
IPC分类号： G01N33/566 , A61K38/00 , C07K1/04 , C07K5/00 , C07K7/22 , C07K7/56 , C07K14/00 , C07K14/655 , C07K17/02 , G01R31/3185 , A61K38/12 , C07K1/046
CPC分类号： C07K7/22 , C07K1/047 , C07K14/001 , C07K14/6555 , C07K7/56 , G01R31/318541 , A61K38/00 , Y02P20/55
摘要： Libraries of novel backbone-cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units used in the synthesis of these backbone-cyclized peptide analogs are N(((-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N(((-functionalized) amino acids are incorporated into a library of peptide sequences, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by libraries of backbone-cyclized bradykinin analogs, somatostatin analogs, BPI analogs and Substance P analogs having biological activity. Further embodiments of the invention are Interleukin-6 receptor derived peptides having ring structures involving backbone cyclization.
摘要翻译：通过经由氨基酸衍生物的α氮连接的桥连基团形成新的骨架环化肽类似物的文库，以提供新的非肽链。用于合成这些骨架环化肽类似物的新型构建单元是构建成包括间隔基和末端官能团的N（（（ - 官能化））氨基酸，这些N（（（ - （ - 引入肽序列文库，优选在固相肽合成期间，反应性末端官能团被特异保护基团保护，所述保护基团可被选择性地除去以实现骨架至骨架或骨架至侧链环化。本发明例如骨架环化的缓激肽类似物，生长抑素类似物，BPI类似物和具有生物活性的物质P类似物的文库。本发明的其它实施方案是具有涉及骨架环化的环结构的白细胞介素-6受体衍生的肽。

4. 发明授权

US5770687A Comformationally constrained backbone cyclized somatostatin analogs 失效
标题翻译：组合受限的骨架环化生长抑素类似物
公开(公告)号：US5770687A
公开(公告)日：1998-06-23
申请号：US690090
申请日：1996-07-31
申请人： Vered Hornik , Alon Seri-Levy , Gary Gellerman , Chaim Gilon
发明人： Vered Hornik , Alon Seri-Levy , Gary Gellerman , Chaim Gilon
IPC分类号： A61K38/04 , A61K38/00 , A61P3/00 , A61P5/00 , A61P35/00 , C07K1/04 , C07K7/06 , C07K7/50 , C07K7/64 , C07K14/00 , C07K14/655 , G01R31/3185 , A61K38/12
CPC分类号： C07K1/047 , C07K14/001 , C07K14/655 , C07K14/6555 , G01R31/318541 , A61K38/00 , Y02P20/55
摘要： Novel peptide analogs are disclosed. The novel peptides are conformationally constrained backbone cyclized somatostatin analogs. Methods for synthesizing the somatostatin analogs and for producing libraries of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions in the treatment of endocrine disorders, neoplasms and metabolic disorders are also disclosed.
摘要翻译：公开了新的肽类似物。新型肽是构象约束的骨架环化生长抑素类似物。还公开了用于合成生长抑素类似物和生产生长抑素类似物文库的方法。此外，还公开了包含生长抑素类似物的药物组合物，以及使用这些组合物治疗内分泌紊乱，赘生物和代谢紊乱的方法。

5. 发明授权

US5656655A Styryl-substituted heteroaryl compounds which inhibit EGF receptor tyrosine kinase 失效
标题翻译：抑制EGF受体酪氨酸激酶的苯乙烯基取代的杂芳基化合物
公开(公告)号：US5656655A
公开(公告)日：1997-08-12
申请号：US444696
申请日：1995-05-19
申请人： Alfred P. Spada , Paul E. Persons , Alexander Levitzki , Chaim Gilon , Aviv Gazit
发明人： Alfred P. Spada , Paul E. Persons , Alexander Levitzki , Chaim Gilon , Aviv Gazit
IPC分类号： A61K31/404 , A61K31/4406 , C07D209/18 , C07D213/57 , C07D209/04 , A61K31/40
CPC分类号： C07D213/57 , A61K31/404 , A61K31/4406 , C07D209/18
摘要： A method of inhibiting cell proliferation in a patient suffering from such disorder comprising the administration to the patient of a pharmaceutically effective amount of a pharmaceutical composition containing, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, of the formula ##STR1## wherein the radicals are defined in the specification.
摘要翻译：一种抑制患有这种病症的患者的细胞增殖的方法，包括向患者施用药学有效量的药物组合物，其包含与药学上可接受的载体，化合物或其药学上可接受的盐的混合物式其中基团在说明书中定义。

6. 发明申请

US20050266496A1 Heterocyclic compounds, combinatorial libraries thereof and methods of selecting drug leads 审中-公开
标题翻译：杂环化合物，其组合文库和选择药物引线的方法
公开(公告)号：US20050266496A1
公开(公告)日：2005-12-01
申请号：US11086722
申请日：2005-03-22
申请人： Chaim Gilon
发明人： Chaim Gilon
IPC分类号： C07B61/00 , C07D285/00 , C07D285/38 , C07K1/04 , C12Q1/68 , C07D245/02 , G01N33/53
CPC分类号： C07D285/00 , C07D285/38 , C07K1/047 , C40B40/00
摘要： Heterocyclic compounds having a relatively flexible backbone are used to create combinatorial libraries that permit screening for lead compounds and selection of drug candidates for a variety of uses in human and veterinary medicine as well as in agriculture. The compounds of the library generally differ in ring size and chirality of substituents on the ring. Also disclosed are methods for providing and screening these libraries, preferably in an automated or computerizable manner, such as by using a computer program to virtually screen the compounds in order to identify those that are predicted to have bioactive conformations that should give rise to desirable biological effects.
摘要翻译：具有相对柔性骨架的杂环化合物用于产生组合文库，其允许筛选铅化合物和选择候选药物用于人类和兽医学以及农业中的各种用途。文库的化合物通常在环上取代基的环尺寸和手性不同。还公开了用于提供和筛选这些文库的方法，优选以自动化或可计算的方式，例如通过使用计算机程序来虚拟筛选化合物，以便鉴定那些预期具有生物活性构象的那些文库，其应当产生理想的生物效果。

7. 发明授权

US06664368B1 Inhibition of nuclear import by backbone cyclic peptide analogs 失效
标题翻译：通过骨架环肽类似物抑制核进口
公开(公告)号：US06664368B1
公开(公告)日：2003-12-16
申请号：US09564677
申请日：2000-05-04
申请人： Assaf Friedler , Abraham Loyter , Chaim Gilon , Amnon Wolf
发明人： Assaf Friedler , Abraham Loyter , Chaim Gilon , Amnon Wolf
IPC分类号： C07K750
CPC分类号： C07K14/005 , C12N2740/16322
摘要： The design and the synthesis of backbone cyclic peptide analogs which functionally mimic the nuclear localization signal (NLS) region of macromolecules is disclosed. The principles of the invention are exemplified for the NLS sequences of the human immunodeficiency virus type 1 proteins MA, Vpr, Tat and NLS-like sequences of HIV-1 protein Vif. We disclose the discovery of a novel, highly potent backbone cyclic peptide, designated BCvir, which inhibits nuclear import with an IC50 value of 35 nM. This inhibitory potency is to be compared to 12 &mgr;M exhibited by the linear parent HIV-1 MA NLS peptide. BCvir also reduced HIV-1 production by 75% in infected non-dividing cultured human T-cells and was relatively resistant to tryptic digestion. These properties render backbone cyclic peptide analogs of NLS or NLS-like sequences as candidates for novel drugs based on blocking nuclear import of viral genomes.
摘要翻译：公开了功能上模拟大分子的核定位信号（NLS）区域的骨架环肽类似物的设计和合成。对于HIV-1蛋白Vif的人免疫缺陷病毒1型蛋白MA，Vpr，Tat和NLS样序列的NLS序列，举例说明了本发明的原理。我们公开了一种称为BCvir的新型高效骨架环肽的发现，其抑制核导入，IC50值为35nM。将该抑制效力与线性亲本HIV-1 MA NLS肽显示的12μM进行比较。在感染的非分裂培养的人类T细胞中，BCvir还将艾滋病毒1的产量降低了75％，并且相对抗胰蛋白酶消化。这些性质使NLS或NLS样序列的骨架环肽类似物作为基于阻断核进入病毒基因组的新型药物的候选物。

8. 发明授权

US06265375B1 Conformationally constrained backbone cyclized peptide analogs 失效
标题翻译：构象受限的骨架环化肽类似物
公开(公告)号：US06265375B1
公开(公告)日：2001-07-24
申请号：US09120237
申请日：1998-07-22
申请人： Chaim Gilon , Doron Eren , Irina Zeltser , Alon Seri-Levy , Gal Gitan , Dan Muller
发明人： Chaim Gilon , Doron Eren , Irina Zeltser , Alon Seri-Levy , Gal Gitan , Dan Muller
IPC分类号： A61K3808
CPC分类号： C07K14/001 , A61K38/00 , C07C271/22 , C07K7/02 , C07K7/18 , C07K7/56 , C07K14/6555 , G01R31/318541 , Y02P20/55
摘要： Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N&agr;(&ohgr;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N&agr;(&ohgr;-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.
摘要翻译：通过经由氨基酸衍生物的α氮连接的桥连基团形成新的主链环化肽类似物以提供新的非肽键。公开的新型建筑单元是构建成包括间隔基和末端官能团的Nalpha（ω-官能化）氨基酸。将这些Nalpha（ω-官能化）氨基酸中的一种或多种掺入肽序列中，优选在固相肽合成期间。反应性末端官能团被特定的保护基团保护，该保护基团可被选择性地去除以实现骨架 - 骨架或主链 - 侧链环化。具有生物活性的骨架环化缓激肽拮抗剂具体举例说明本发明。本发明的其它实施方案是具有一个或两个环结构的生长抑素类似物，其涉及骨架环化。

9. 发明授权

US5990277A Semipeptoid farnesyl protein transferase inhibitors and analogs thereof 失效
标题翻译：半皮型法呢基蛋白转移酶抑制剂及其类似物
公开(公告)号：US5990277A
公开(公告)日：1999-11-23
申请号：US707082
申请日：1996-09-03
申请人： Alexander Levitzki , Chaim Gilon , Hadas Reuveni
发明人： Alexander Levitzki , Chaim Gilon , Hadas Reuveni
IPC分类号： A61K38/00 , C07K5/103 , A61K38/07
CPC分类号： C07K5/1013 , A61K38/00
摘要： A farnesyl protein transferase (i.e., farnesyltransferase) inhibitors formed as peptoid and semipeptoid peptidomimetic compounds derived from a farnesyltransferase universal recognition tetrapeptide sequence CAAX (i.e., CAAX motif) and analogs thereof, and to the use of these compounds and analogs and ester derivatives thereof as chemotherapeutic agents in oncogenic or non-oncogenic Ras associated cancers and proliferative diseases.
摘要翻译：由法呢基转移酶通用识别四肽序列CAAX（即CAAX基序）及其类似物衍生的拟胆碱和半皮下模拟肽化合物形成的法呢基蛋白转移酶（即法呢基转移酶）抑制剂以及这些化合物及其类似物和酯衍生物作为致癌或非致癌性Ras相关癌症和增殖性疾病中的化学治疗剂。

10. 发明授权

US08198218B2 Heterocyclic compounds, combinatorial libraries thereof and methods of selecting drug leads 有权
标题翻译：杂环化合物，其组合文库和选择药物引线的方法
公开(公告)号：US08198218B2
公开(公告)日：2012-06-12
申请号：US12474318
申请日：2009-05-29
申请人： Chaim Gilon
发明人： Chaim Gilon
IPC分类号： C40B40/02
CPC分类号： C07D285/00 , C07D285/38 , C07K1/047 , C40B40/00
摘要： Heterocyclic compounds having a relatively flexible backbone are used to create combinatorial libraries that permit screening for lead compounds and selection of drug candidates for a variety of uses in human and veterinary medicine as well as in agriculture. The compounds of the library generally differ in ring size and chirality of substituents on the ring. Also disclosed are methods for providing and screening these libraries, preferably in an automated or computerizable manner, such as by using a computer program to virtually screen the compounds in order to identify those that are predicted to have bioactive conformations that should give rise to desirable biological effects.
摘要翻译：具有相对柔性骨架的杂环化合物用于产生组合文库，其允许筛选铅化合物和选择药物候选物以用于人类和兽医学以及农业中的各种用途。文库的化合物通常在环上取代基的环尺寸和手性不同。还公开了用于提供和筛选这些文库的方法，优选以自动化或可计算的方式，例如通过使用计算机程序来虚拟筛选化合物，以便鉴定那些预期具有生物活性构象的那些文库，其应当产生理想的生物效果。

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