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公开(公告)号：US5098996A
公开(公告)日：1992-03-24
申请号：US168494
申请日：1988-03-15
IPC分类号： A61K38/00 , C07D473/06 , C07D473/08 , C07D519/00 , C07K5/06 , C07K5/065
CPC分类号： C07D473/06 , C07D473/08 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： Radioactive fluorine can be easily introduced into biologically active molecules containing amino groups. A p-bromomethyl benzoyl group is coupled to the amino group of the biologically active molecule, and bromine is displaced by fluorine. Alternatively, the bromine on the bromomethylbenzoyl group is first displaced by fluorine, and the fluoromethyl benzoyl group is then coupled to the amino group of the biologically active molecule. The compounds so produced are useful in diagnostic nuclear medicine.
摘要翻译： 放射性氟可以容易地引入到含有氨基的生物活性分子中。 对溴甲基苯甲酰基与生物活性分子的氨基偶联，溴被氟取代。 或者，溴甲基苯甲酰基上的溴首先被氟取代，然后将氟甲基苯甲酰基与生物活性分子的氨基偶联。 如此制备的化合物可用于诊断性核医学。
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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.
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3.发明申请PEPTIDES BASED ON THE TRANSMEMBRANE DOMAIN OF A TOLL-LIKE RECEPTOR (TLR) FOR TREATMENT OF TLR-MEDIATED DISEASES 有权用于治疗TLR介导性疾病的TOLL-LIKE受体（TLR）的跨膜结构域的肽公开(公告)号：US20130225478A1
公开(公告)日：2013-08-29
申请号：US13811226
申请日：2011-07-19
IPC分类号： C07K14/705
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.
摘要翻译： 提供了能够抑制由选自TLR 1,2,4或6的Toll样受体（TLR）介导的细胞活化的肽，所述肽包含由跨膜结构域的跨膜结构域的序列组成或发现的序列 选自TLR 1,2,4或6的TLR，以及跨膜结构域侧翼的任选的细胞质和胞外区。 这些肽以及包含它们的药物组合物可用于治疗TLR介导的疾病。
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公开(公告)号：US20070072808A1
公开(公告)日：2007-03-29
申请号：US10560727
申请日：2004-06-18
申请人： Yechiel Shai , Dorit Avrahami
发明人： Yechiel Shai , Dorit Avrahami
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 add, 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。
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公开(公告)号：US08445636B2
公开(公告)日：2013-05-21
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： C07K1/00
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。
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公开(公告)号：US20120321668A1
公开(公告)日：2012-12-20
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： A61K38/08 , C07K7/08 , C07K14/155 , C07K4/02 , A61K38/03 , A61K38/10 , A61K38/16 , A61P29/00 , A61P37/00 , A61P25/00 , A61P17/06 , A61P3/10 , A61P21/04 , A61P5/00 , A61P1/16 , A61P1/04 , A61P17/00 , A61P19/02 , A61P17/14 , A61P11/06 , A61P11/00 , A61P11/02 , A61P37/08 , A61P13/12 , A61P31/00 , A61P19/08 , C07K7/06
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。
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7.发明申请DIASTEREOMERIC PEPTIDES USEFUL AS INHIBITORS OF MEMBRANE PROTEIN ASSEMBLY 审中-公开作为膜蛋白质组装的抑制剂有用的二酯类抗生素公开(公告)号：US20100240589A1
公开(公告)日：2010-09-23
申请号：US12774621
申请日：2010-05-05
申请人： Yechiel Shai
发明人： Yechiel Shai
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。
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8.发明授权Peptides derived from HIV-1 gp41 transmembrane domain for t-immunomodulation 有权衍生自HIV-1 gp41跨膜结构域的肽用于t-免疫调节公开(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。
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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。
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公开(公告)号：US20090270312A1
公开(公告)日：2009-10-29
申请号：US11722064
申请日：2006-01-24
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。
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