公开(公告)号：US07449445B2

公开(公告)日：2008-11-11

申请号：US11252719

申请日：2005-10-19

Applicant: Kentaro Onizuka ,  Shuhei Tanaka ,  Hirokazu Sugihara ,  Atsuo Tamura

Inventor： Kentaro Onizuka ,  Shuhei Tanaka ,  Hirokazu Sugihara ,  Atsuo Tamura

IPC: A61K38/00 ,  A61K51/00 ,  A61K38/04 ,  C07K2/00 ,  C07K4/00 ,  C07K5/00 ,  C07K7/00 ,  C07K14/00 ,  C07K16/00 ,  C07K17/00 ,  A61M36/14 ,  A01N37/18

CPC classification number: C07K7/06 ,  C07K14/001 ,  Y10S930/28 ,  Y10S977/705 ,  Y10S977/729

Abstract: A peptide nanofiber having conductivity is provided. A conductive peptide nanofiber which includes a nanofiber formed through a manner of self-assembly of a peptide that has a nanofiber-forming ability and consists of an amino acid sequence of Xaa-Phe-Ile-Val-Ile-Phe-Xaa (SEQ ID NO: 1, wherein N-terminal Xaa is an arbitrary amino acid residue Xaa1; C-terminal Xaa is an arbitrary amino acid residue Xaa2; and Xaa1 and Xaa2 are an amino acid having an acidic side chain, an amino acid having a basic side chain, or an amino acid having a side chain with polarity according as acidity and basicity) or a derivative of the peptide and a conductive substance added thereto, the aforementioned conductive substance being added to an amino group of the peptide or the derivative.

Abstract translation: 提供了具有导电性的肽纳米纤维。 一种导电肽纳米纤维，其包括通过具有纳米纤维形成能力并由Xaa-Phe-Ile-Val-Ile-Phe-Xaa的氨基酸序列组成的肽的自组装形式的纳米纤维（SEQ ID NO： NO：1，其中N-末端Xaa是任意的氨基酸残基Xaa 1 C末端Xaa是任意的氨基酸残基Xaa 2和Xaa < 1和Xaa 2是具有酸性侧链，具有碱性侧链的氨基酸或具有根据酸度和碱度的极性侧链的氨基酸的氨基酸） 或肽的衍生物和加入其中的导电物质，将上述导电物质加入肽或其衍生物的氨基。

公开(公告)号：US07432243B2

公开(公告)日：2008-10-07

申请号：US10408415

申请日：2003-04-07

Applicant: Eugene G. Levin

Inventor： Eugene G. Levin

IPC: A61K38/18 ,  C07K17/00 ,  C07K14/50 ,  C07K19/00

CPC classification number: C07K14/503 ,  A61K38/00 ,  C07K2319/00 ,  Y10S930/28

Abstract: The invention relates to fragments of an amino acid sequence of mature, full length 24 kDa fibroblast growth factor-2 or an analog thereof. The fragments have an activity that inhibits the migration of cultured cells as well as inhibiting angiogenesis, tumor growth, or any other processes that involve the migration of cells in vivo. This fragment does not stimulate the proliferation of cells which is in contrast to activity shown by the mature, full-length 24 kDa fibroblast growth factor-2. The present invention also relates to a DNA molecule encoding the fragment, an expression vector and a transformed host containing the DNA molecule, and a method of producing the protein by culturing the transformed host. Moreover, the present invention relates to a therapeutic composition the 24 kDa fibroblast growth factor fragment and a pharmaceutically acceptable carrier.

公开(公告)号：US20080234248A1

公开(公告)日：2008-09-25

申请号：US12108885

申请日：2008-04-24

Applicant: Duane A. Burnett ,  John W. Clader

Inventor： Duane A. Burnett ,  John W. Clader

IPC: A61K31/397 ,  C07D205/02 ,  A61P9/00

CPC classification number: C07D405/12 ,  Y10S930/28

Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating atherosclerosis, hypercholesterolemia, or sitosterolemia, and for lowering plasma levels of sterols and/or stanols.

Abstract translation: 本发明提供由结构式（I）表示的化合物或式（I）化合物的药学上可接受的异构体，盐，溶剂合物或酯，其中每个取代基如本文所述，包括上述化合物的制剂，方法 用于制备它们以及用于治疗动脉粥样硬化，高胆固醇血症或静脉麻醉的方法，以及用于降低甾醇和/或甾醇的血浆水平。

公开(公告)号：US20080113906A1

公开(公告)日：2008-05-15

申请号：US10563551

申请日：2004-07-02

Applicant: Jeak Ling Ding ,  Bow Ho

Inventor： Jeak Ling Ding ,  Bow Ho

IPC: A61K38/17 ,  C07K14/47 ,  C07H21/04 ,  C12N15/63 ,  C12N5/06 ,  C12N1/20 ,  C12P21/00 ,  A61P31/04 ,  G01N33/554

CPC classification number: C12Y304/21084 ,  A61K38/00 ,  C12N9/6408 ,  Y10S435/975 ,  Y10S530/81 ,  Y10S930/28

Abstract: Endotoxin, also known as lipopolysaccharides (LPS), is the major mediator of septic shock due to Gram-negative bacterial infection. Chemically synthesized S3 peptide, derived from Sushi3 domain of Factor C, which is the endotoxin-sensitive serine protease of the limulus coagulation cascade, binds and neutralizes LPS activity. Fluorescent tagged-S3 is shown to detect LPS-containing bacteria. For large-scale production of S3 and to mimic other pathogen-recognizing molecules, tandem multimers of the S3 gene were constructed and expressed in E. coli. Tetramer of S3 for example is shown to display an enhanced inhibitory effect on LPS-induced activities. An affinity matrix based on tetramer of S3 is also shown to be particularly efficient at removing LPS.

Abstract translation: 内毒素也被称为脂多糖（LPS），是革兰氏阴性细菌感染引起的败血性休克的主要介质。 衍生自因子C的Sushi3结构域的化学合成的S3肽，其是鲎凝血级联的内毒素敏感的丝氨酸蛋白酶，其结合并中和LPS活性。 荧光标记的S3显示检测含LPS细菌。 为了大规模生产S3并模拟其他病原体识别分子，构建了S3基因的串联多聚体并在大肠杆菌中表达。 S3的四聚体显示出增强的对LPS诱导的活性的抑制作用。 基于S3的四聚体的亲和基质也显示出在去除LPS时特别有效。

公开(公告)号：US07368563B2

公开(公告)日：2008-05-06

申请号：US11705978

申请日：2007-02-13

Applicant: Duane A. Burnett ,  John W. Clader ,  Wayne Vaccaro

Inventor： Duane A. Burnett ,  John W. Clader ,  Wayne Vaccaro

IPC: C07H7/02 ,  A61K31/7052 ,  A61P9/10 ,  A61P3/06 ,  A61P25/28 ,  C07D205/08 ,  A61K31/397 ,  C07K2/00

CPC classification number: C07D403/12 ,  C07D205/08 ,  Y10S930/28

Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations iucluding the above compounds, processes for preparing the same and methods for treating vascular conditions, such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols.

Abstract translation: 本发明提供由结构式（I）表示的化合物：或式（I）化合物的药学上可接受的异构体，盐，溶剂合物或酯，其中每个取代基如本文所述，包括上述化合物，方法 用于制备相同的药物和治疗血管病症的方法，例如动脉粥样硬化或高胆固醇血症，糖尿病，肥胖症，中风，脱髓鞘和降低甾醇和/或甾醇的血浆水平。

公开(公告)号：US07208486B2

公开(公告)日：2007-04-24

申请号：US10792346

申请日：2004-03-03

Applicant: Duane A. Burnett ,  John W. Clader

Inventor： Duane A. Burnett ,  John W. Clader

IPC: C07D205/08 ,  A61K31/397 ,  A61K31/7052 ,  A61P3/06 ,  C07H7/02

CPC classification number: C07D405/12 ,  C07D405/14 ,  Y10S930/28

Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating vascular conditions, such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols.

公开(公告)号：US20070043017A1

公开(公告)日：2007-02-22

申请号：US11544718

申请日：2006-10-10

Applicant: Gerhard Jaehne ,  Wendelin Frick ,  Stefanie Flohr ,  Andreas Lindenschmidt ,  Heiner Glombik ,  Werner Kramer ,  Hubert Heuer ,  Hans-Ludwig Schaefer

Inventor： Gerhard Jaehne ,  Wendelin Frick ,  Stefanie Flohr ,  Andreas Lindenschmidt ,  Heiner Glombik ,  Werner Kramer ,  Hubert Heuer ,  Hans-Ludwig Schaefer

IPC: A61K31/397 ,  C07D205/02 ,  C07D403/02

CPC classification number: C07D403/12 ,  C07D205/08 ,  C07D453/02 ,  C07D487/08 ,  Y10S930/28

Abstract: One embodiment of the invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification. Other embodiments of the invention relate to physiologically acceptable salts of compounds of formula I, to processes for their preparation and to medicaments comprising these compounds. The compounds of the invention are suitable for use, for example, as hypolipidemics.

公开(公告)号：US06809180B2

公开(公告)日：2004-10-26

申请号：US09832464

申请日：2001-04-11

Applicant: Piet A. J. de Boer ,  Cynthia A. Hale

Inventor： Piet A. J. de Boer ,  Cynthia A. Hale

IPC: C07K14245

CPC classification number: C07K14/245 ,  G01N33/9446 ,  Y10S530/81 ,  Y10S530/811 ,  Y10S530/814 ,  Y10S530/817 ,  Y10S530/825 ,  Y10S930/28

Abstract: A method for screening compounds for antimicrobial activity is described that utilizes bacterial protein—protein binding in vitro. The method may be performed using immobilized elements and the immobilization may be carried out using a variety of immobilization means (e.g., columns, beads, adsorbents, nitrocellulose paper, etc.) in order to screen large libraries of compounds.

Abstract translation: 描述了筛选化合物用于抗微生物活性的方法，其在体外利用细菌蛋白质 - 蛋白质结合。 该方法可以使用固定化元件进行，并且可以使用各种固定装置（例如，柱，珠，吸附剂，硝化纤维素纸等）进行固定以筛选大量化合物文库。

公开(公告)号：US5443815A

公开(公告)日：1995-08-22

申请号：US807062

申请日：1991-11-27

Applicant: Richard T. Dean ,  William McBride ,  Scott Buttram

Inventor： Richard T. Dean ,  William McBride ,  Scott Buttram

IPC: A61K51/00 ,  A61K38/00 ,  A61K51/08 ,  C07B59/00 ,  C07F13/00 ,  C07K5/10 ,  C07K7/06 ,  C07K7/08 ,  C07K14/00 ,  C07K14/775

CPC classification number: C07K7/06 ,  A61K51/08 ,  A61K51/082 ,  A61K51/088 ,  C07B59/008 ,  C07K14/775 ,  A61K2121/00 ,  A61K2123/00 ,  A61K38/00 ,  Y10S930/28

Abstract: The invention relates to radiolabeled imaging of a mammalian body. The invention in particular provides for reagents labeled with technetium-99m for such imaging. The invention provides peptides which bind Tc-99m and which can be targeted to specific sites within a mammalian body.

Abstract translation: 本发明涉及哺乳动物体的放射性标记成像。 本发明特别提供了用于这种成像的用锝-99m标记的试剂。 本发明提供结合Tc-99m并可靶向哺乳动物体内特定位点的肽。

公开(公告)号：US5132111A

公开(公告)日：1992-07-21

申请号：US508258

申请日：1990-04-11

Applicant: Wylie W. Vale, Jr. ,  Jean E. F. Rivier ,  Jeffrey Schwartz

Inventor： Wylie W. Vale, Jr. ,  Jean E. F. Rivier ,  Jeffrey Schwartz

IPC: C07K14/575

CPC classification number: C07K14/57509 ,  Y10S514/805 ,  Y10S530/807 ,  Y10S930/28

Abstract: Agonists and antagonists of rCRF are disclosed that exhibit good binding affinity to CRF receptors. One exemplary agonist is: H-Ser-Gln-Glu-Pro-Pro-Ile-Ser- Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Met-Leu-Glu-Met- Ala-Arg-Ala-Glu-Gln-Glu-Ala-Glu-Gln-Ala-Ala-Leu-Asn-Arg- Leu-Leu-Leu-Glu-Glu-Ala-NH.sub.2. In the agonists, one or more of the first five N-terminal residues may be deleted or may be substituted by a peptide up to 10 amino acids long. A number of other substitutions may also be made throughout the chain. Similar peptides which function as CRF antagonists are created by deleting the first 7, 8 or 9 N-terminal residues. These analogs are coupled to a cytotoxin, such as gelonin, by a dialdehyde or the like, e.g., glutaraldehyde. The conjugates may be used to eliminate CRF Target Cells, and thus to regulate secretion of ACTH, .beta.-lipotropin and the like. Such conjugates can also be administered to alleviate conditions associated with hyperactivity of the hypothalamus-pituitary adrenal axis as well as neoplastic diseases associated with tumors that express CRF receptor.

Abstract translation: 公开了rCRF的激动剂和拮抗剂，其表现出对CRF受体的良好结合亲和力。 一个示例性的激动剂是：H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Met-Leu-Glu-Met- -Arg-Ala-Glu-Gln-Glu-Ala-Glu-Gln-Ala-Ala-Leu-Asn-Arg-Leu-Leu-Leu-Glu-Glu-Ala-NH2。 在激动剂中，前5个N-末端残基中的一个或多个可以被缺失，或者可被长达10个氨基酸的肽取代。 还可以在整个链中进行许多其它取代。 作为CRF拮抗剂起作用的相似肽通过缺失第7,8或9个N-末端残基而产生。 这些类似物通过二醛或类似物例如戊二醛与细胞毒素（例如gelonin）偶联。 缀合物可用于消除CRF靶细胞，并因此调节ACTH，β-Lipotropin等的分泌。 也可以施用这样的缀合物以减轻与下丘脑 - 垂体肾上腺轴的多动症相关的病症以及与表达CRF受体的肿瘤相关的肿瘤疾病。