公开(公告)号：US08986712B2

公开(公告)日：2015-03-24

申请号：US13512556

申请日：2010-11-29

申请人： Yechiel Shai ,  Irun R. Cohen ,  Tomer Cohen

发明人： Yechiel Shai ,  Irun R. Cohen ,  Tomer Cohen

IPC分类号： A61K39/21 ,  A61K38/08 ,  A61K38/04 ,  A61K38/10 ,  A61K38/16 ,  C07K14/005 ,  A61P11/00 ,  A61P37/02 ,  A61P37/08

CPC分类号： C07K14/005 ,  C12N2740/16122

摘要： The present invention relates to peptides, derivatives and analogs comprising an amino acid sequence derived from the transmembrane domain of HIV gp41 protein, pharmaceutical compositions comprising same, and uses thereof for therapy of inflammatory diseases and disorders, such as T-cell and/or monocyte mediated diseases.

摘要翻译： 本发明涉及包含衍生自HIV gp41蛋白的跨膜结构域的氨基酸序列的肽，衍生物和类似物，包含其的药物组合物及其用于治疗炎性疾病和病症如T细胞和/或单核细胞的用途 介导的疾病。

公开(公告)号：US20090275503A1

公开(公告)日：2009-11-05

申请号：US12066626

申请日：2006-09-21

申请人： Yechiel Shai ,  Irun R. Cohen ,  Francisco Quintana ,  Doron Gerber

发明人： Yechiel Shai ,  Irun R. Cohen ,  Francisco Quintana ,  Doron Gerber

IPC分类号： A61K38/16 ,  C07K2/00 ,  C07K7/06 ,  C07K7/08 ,  C07K14/00 ,  A61P37/00 ,  A61K38/02 ,  A61K38/08 ,  A61K38/10

CPC分类号： A61K38/1774

摘要： The present invention provides diastereomeric peptides derived from the T Cell Receptor alpha Transmembrane Domain, and lipophilic conjugates thereof, which peptides and conjugates are effective in preventing or treating T cell mediated inflammatory diseases. The invention provides pharmaceutical compositions comprising these diastereomeric peptides and conjugates, and uses thereof for therapy of inflammatory diseases, autoimmunity and graft rejection.

摘要翻译： 本发明提供了衍生自T细胞受体α跨膜结构域的非对映异构体肽及其亲脂性缀合物，该肽和缀合物可有效预防或治疗T细胞介导的炎性疾病。 本发明提供包含这些非对映体肽和缀合物的药物组合物及其用于治疗炎性疾病，自身免疫和移植物排斥反应的用途。

公开(公告)号：US20090270312A1

公开(公告)日：2009-10-29

申请号：US11722064

申请日：2006-01-24

申请人： Yechiel Shai ,  Irun R. Cohen ,  Francisco J. Quintana ,  Doron Gerber

发明人： Yechiel Shai ,  Irun R. Cohen ,  Francisco J. Quintana ,  Doron Gerber

IPC分类号： A61K38/16 ,  A61K38/08 ,  C07K14/00 ,  C07K7/00

CPC分类号： C07K14/005 ,  A61K38/162 ,  C07K2319/00 ,  C12N2740/16122

摘要： The present invention provides pharmaceutical compositions and methods for prevention or treatment of autoimmune diseases and other T cell mediated inflammatory diseases and conditions, which comprise as an active ingredient an effective quantity of a peptide derived from HIV gp41 fusion peptide domain or fragments, analogs, homologs and derivatives thereof. The invention further provides novel peptides derived from HIV gp41 fusion peptide domain, useful in the treatment of T cell mediated pathologies.

摘要翻译： 本发明提供了用于预防或治疗自身免疫性疾病和其它T细胞介导的炎性疾病和病症的药物组合物和方法，其包含有效量的源自HIV gp41融合肽结构域或片段，类似物，同系物的有效成分 及其衍生物。 本发明还提供了衍生自HIV gp41融合肽结构域的新型肽，其可用于治疗T细胞介导的病理学。

公开(公告)号：US20080096809A1

公开(公告)日：2008-04-24

申请号：US10583996

申请日：2004-12-22

申请人： Yechiel Shai

发明人： Yechiel Shai

IPC分类号： A61K38/00 ,  A61P43/00 ,  C07K14/00 ,  C07K7/00

CPC分类号： C07K14/195 ,  A61K38/00 ,  C07K14/005 ,  C12N2740/16122

摘要： The present invention relates to membrane binding diastereomeric peptides comprising amino acid sequences corresponding to a fragment of a transmembrane proteins, wherein at least two amino acid residues of the diastereomeric peptides being in a D-isomer configuration. The diastereomeric peptides are useful in inhibiting fusion membrane protein events, including specifically viral replication and transmission.

摘要翻译： 本发明涉及包含对应于跨膜蛋白片段的氨基酸序列的膜结合非对映体肽，其中非对映异构肽的至少两个氨基酸残基为D-异构体构型。 非对映体肽可用于抑制融合膜蛋白事件，特别是病毒复制和传播。

公开(公告)号：US07001983B1

公开(公告)日：2006-02-21

申请号：US09367714

申请日：1998-02-19

申请人： Yechiel Shai ,  Ziv Oren

发明人： Yechiel Shai ,  Ziv Oren

IPC分类号： C07K7/00

CPC分类号： C07K14/001 ,  A61K38/00 ,  C07K14/43572 ,  C07K14/461

摘要： Non-hemolytic cytolytic agents selected from peptides, complexes of bundled peptides, mixtures of peptides or random peptide copolymers have a selected cytolytic activity manifested in that they have a cytolytic activity on pathogenic cells, being cells which are non-naturally occurring with the body consisting of microbial pathogenic organisms and malignant cells; and are non-hemolytic, having no cytolytic effect on red blood cells. The peptides may be cyclic derivatives of natural peptides such as pardaxin and mellitin and fragments thereof in which L-amino acid residues are replaced by corresponding D-amino acid residues, or are diastereomers of linear peptides composed of varying ratios of at least positively charged amino acid and at least one hydrophobic amino acid, and in which at one of the amino acid residues is a D-amino acid. Pharmaceutical compositions comprising the non-hemolytic cytolytic agents can be used for the treatment of several diseases caused by pathogens including antibacterial, fungal, viral mycoplamsa and protozoan infections and for the treatment of cancer.

摘要翻译： 选自肽，肽束复合物，肽混合物或随机肽共聚物的非溶血细胞溶解剂具有选择的细胞溶解活性，其表现为它们对致病细胞具有细胞溶解活性，是与人体非天然存在的细胞 的微生物病原菌和恶性细胞; 并且是非溶血性的，对红细胞没有细胞溶解作用。 肽可以是天然肽的环状衍生物，例如泛珠蛋白和麦角蛋白及其片段，其中L-氨基酸残基被相应的D-氨基酸残基替代，或者是由至少带正电氨基的不同比例组成的线性肽的非对映异构体 酸和至少一个疏水性氨基酸，并且其中一个氨基酸残基是D-氨基酸。 包含非溶血性溶解剂的药物组合物可用于治疗由包括抗菌，真菌，病毒支原体和原生动物感染在内的病原体引起的几种疾病和用于治疗癌症。

公开(公告)号：US4698208A

公开(公告)日：1987-10-06

申请号：US743074

申请日：1985-06-10

申请人： Abraham Patchornik ,  Yechiel Shai ,  Shimeon Pass

发明人： Abraham Patchornik ,  Yechiel Shai ,  Shimeon Pass

IPC分类号： C07C51/09 ,  B01J19/00 ,  C07B31/00 ,  C07B61/00 ,  C07C51/00 ,  C07C67/00 ,  C07C227/00 ,  C07C227/18 ,  C07C227/20 ,  C07C233/47 ,  C07C241/00 ,  C07C251/24 ,  C07C313/00 ,  C07C319/24 ,  C07C323/63 ,  C07D303/38 ,  C07F7/18 ,  C07F9/09 ,  C07F9/12 ,  C07F9/145 ,  C07H1/00 ,  C07H21/00 ,  C07K1/04 ,  C08L89/00 ,  C40B60/14 ,  G05D7/00

CPC分类号： C07H21/00 ,  B01J19/0046 ,  C07C249/16 ,  C07D303/38 ,  C07F7/1852 ,  C07F9/094 ,  B01J2219/00286 ,  B01J2219/00391 ,  B01J2219/005 ,  B01J2219/0059 ,  B01J2219/00596 ,  B01J2219/00686 ,  B01J2219/00698 ,  B01J2219/0072 ,  C40B60/14

摘要： An automated apparatus for conducting a broad range of organic synthesis reactions includes a first column carring a polymeric support, a second column carrying a second polymer support, and conduits connecting the two columns and permitting the circulation of fluids therebetween. In operation each polymeric support carries a different reactive species and a liquid medium containing a specifically selected intermediate reactant, in a solvent, is circulated between the columns in order to remove the reactive species from the first support by reaction with the intermediate, and to permit the reactive species thus removed to react with the reactive second support, at the same time regenerating the original intermediate reactant. Sensors are placed at the entrance and exit of the second column carrying the second polymeric support. The sensors are capable of sensing the relative presence of the intermediate reactant. When the same content of intermediate reactant is sensed at both the entrance and exit of the second column, the computer causes the circulation to be automatically stopped as this indicates complete loading of the second column.

公开(公告)号：US09890202B2

公开(公告)日：2018-02-13

申请号：US13811226

申请日：2011-07-19

申请人： Yechiel Shai ,  Avner Fink ,  Eliran-Moshe Reuven ,  Liraz Shmuel-Galia

发明人： Yechiel Shai ,  Avner Fink ,  Eliran-Moshe Reuven ,  Liraz Shmuel-Galia

IPC分类号： A61K38/16 ,  A61K38/10 ,  A61K38/00 ,  A61K38/04 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  C07K14/705 ,  C07K7/08 ,  C07K4/00 ,  C07K14/00 ,  A61K38/03

CPC分类号： C07K14/705 ,  A61K38/00 ,  A61K38/03 ,  A61K38/04 ,  A61K38/10 ,  A61K38/16 ,  C07K4/00 ,  C07K7/08 ,  C07K14/00 ,  Y02A50/411

摘要： Peptides are provided that are capable of inhibiting cell activation mediated by a Toll-like receptor (TLR) selected from TLR 1, 2, 4 or 6, said peptide comprising a sequence consisting of, or found within, the sequence of the transmembrane domain of a TLR selected from TLR 1, 2, 4 or 6 and optionally cytoplasmic and extracellular regions flanking the transmembrane domain. These peptides as well as pharmaceutical composition comprising them are useful for the treatment of TLR-mediated disease.

公开(公告)号：US20120028887A1

公开(公告)日：2012-02-02

申请号：US13260902

申请日：2010-03-28

申请人： Yechiel Shai ,  Yael Wexler-Cohen

发明人： Yechiel Shai ,  Yael Wexler-Cohen

IPC分类号： A61K38/16 ,  A61P31/18 ,  A61P31/14 ,  C07K14/00 ,  C12N7/06

CPC分类号： C07K14/005 ,  A61K47/542 ,  A61K47/551 ,  A61K47/554 ,  A61K49/0017 ,  C12N2740/16122

摘要： The invention provides lipophilic conjugates comprising a short isolated peptide coupled to a hydrophobic moiety, the peptide comprising a sequence derived from the HIV-1 gp41 N-terminal heptad repeat domain, said peptide after conjugation to the hydrophobic moiety possesses anti-fusogenic activity higher than prior to conjugation. The lipophilic conjugates are suitable for treatment of infections caused by human and non-human retroviruses, especially HIV.

摘要翻译： 本发明提供了包含与疏水部分偶联的短分离肽的亲脂性缀合物，所述肽包含衍生自HIV-1 gp41 N-末端七肽重复结构域的序列，所述肽在与疏水部分共轭后具有高于 在共轭之前。 亲脂性缀合物适用于治疗由人和非人类逆转录病毒，特别是艾滋病毒引起的感染。

公开(公告)号：US20100160213A1

公开(公告)日：2010-06-24

申请号：US12685202

申请日：2010-01-11

申请人： Yechiel Shai ,  Dorit Avrahami

发明人： Yechiel Shai ,  Dorit Avrahami

IPC分类号： A61K38/06 ,  A61K38/07 ,  A61K38/12 ,  A61K38/05 ,  C07K5/10 ,  C07K5/08 ,  C07K5/06

CPC分类号： C07K5/06086 ,  A61K38/00 ,  A61K47/542 ,  C07K5/0815 ,  C07K5/1019 ,  C07K7/06 ,  C07K7/08 ,  C07K14/46

摘要： The invention provides lipophilic conjugates comprising a peptide coupled to a fatty acid, the peptide comprising at least two positively charged amino acid residues, said peptide after conjugation to the fatty acid possessing antibacterial, antifungal, and/or anticancer activity higher than prior to conjugation. The lipophilic conjugates are suitable for treatment of infections caused by pathogenic organisms such as bacteria and fungi. The lipophilic conjugates are also suitable for sanitation, as disinfectants, or for food preservation.

摘要翻译： 本发明提供了亲脂性缀合物，其包含与脂肪酸偶联的肽，所述肽包含至少两个带正电荷的氨基酸残基，所述肽与缀合之后具有比缀合之前更高的抗细菌，抗真菌和/或抗癌活性的脂肪酸缀合。 亲脂性缀合物适用于治疗由病原体如细菌和真菌引起的感染。 亲脂性缀合物也适用于卫生，消毒剂或食品保鲜。

公开(公告)号：US07671011B2

公开(公告)日：2010-03-02

申请号：US10560727

申请日：2004-06-18

申请人： Yechiel Shai ,  Dorit Avrahami

发明人： Yechiel Shai ,  Dorit Avrahami

IPC分类号： C07K7/00

CPC分类号： C07K5/06086 ,  A61K38/00 ,  A61K47/542 ,  C07K5/0815 ,  C07K5/1019 ,  C07K7/06 ,  C07K7/08 ,  C07K14/46

摘要： Lipophilic conjugates comprise a peptide coupled to a fatty acid The peptide comprises at least two positively charged amino acid residues; the peptide after conjugation to the fatty acid possessing antibacterial, antifungal, and/or anticancer activity higher than prior to conjugation. The lipophilic conjugates are suitable for treatment of infections caused by pathogenic organisms such as bacteria and fungi. The lipophilic conjugates are also suitable for sanitation, as disinfectants, or for food preservation.

摘要翻译： 亲脂性缀合物包含与脂肪酸偶联的肽。 肽包含至少两个带正电荷的氨基酸残基; 在与缀合之后具有更高抗菌，抗真菌和/或抗癌活性的脂肪酸缀合后的肽。 亲脂性缀合物适用于治疗由病原体如细菌和真菌引起的感染。 亲脂性缀合物也适用于卫生，消毒剂或食品保鲜。