公开(公告)号：US09217027B2

公开(公告)日：2015-12-22

申请号：US12665256

申请日：2008-06-18

Applicant: Maria Kazimtrova ,  R. Manjunatha Kini ,  Cho Yeow Koh

Inventor： Maria Kazimtrova ,  R. Manjunatha Kini ,  Cho Yeow Koh

IPC: A61K51/00 ,  A61M36/14 ,  G01N33/53 ,  C12N15/09 ,  C12N1/20 ,  C12N15/00 ,  C12N9/96 ,  C12N9/99 ,  A61K38/57 ,  C07K14/81 ,  C07K14/745 ,  A61K38/00 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  A61K38/04 ,  A61K38/36 ,  A61K51/08 ,  C07K7/06 ,  C07K7/08 ,  C12Q1/56

CPC classification number: C07K14/811 ,  A61K38/36 ,  A61K38/57 ,  A61K51/08 ,  C07K7/06 ,  C07K7/08 ,  C12Q1/56

Abstract: The invention relates to thrombin inhibitors derived from the salivary glands of haematophagous arthropods and in particular to bivalent and trivalent thrombin inhibitors that act by interacting with thrombin at two or three different sites.

Abstract translation: 本发明涉及来自血液节肢动物唾液腺的凝血酶抑制剂，特别涉及通过在两个或三个不同位点与凝血酶相互作用的二价和三价凝血酶抑制剂。

公开(公告)号：US20130183237A1

公开(公告)日：2013-07-18

申请号：US12665256

申请日：2008-06-18

Applicant: Maria Kazimirova ,  R. Manjunatha Kini ,  Cho Yeow Koh

Inventor： Maria Kazimirova ,  R. Manjunatha Kini ,  Cho Yeow Koh

IPC: C07K14/81 ,  A61K51/08 ,  C12Q1/56 ,  C07K7/08 ,  C07K7/06

CPC classification number: C07K14/811 ,  A61K38/36 ,  A61K38/57 ,  A61K51/08 ,  C07K7/06 ,  C07K7/08 ,  C12Q1/56

Abstract: The invention relates to thrombin inhibitors derived from the salivary glands of haematophagous arthropods and in particular to bivalent and trivalent thrombin inhibitors that act by interacting with thrombin at two or three different sites.

Abstract translation: 本发明涉及来自血液节肢动物唾液腺的凝血酶抑制剂，特别涉及通过在两个或三个不同位点与凝血酶相互作用的二价和三价凝血酶抑制剂。

公开(公告)号：US20120135931A1

公开(公告)日：2012-05-31

申请号：US13319051

申请日：2010-05-05

Applicant: R. Manjunatha Kini ,  Cho Yeow Koh ,  Kunchithapadam Swaminathan ,  Kumar Sundramurthy

Inventor： R. Manjunatha Kini ,  Cho Yeow Koh ,  Kunchithapadam Swaminathan ,  Kumar Sundramurthy

IPC: A61K38/58 ,  C07K14/815 ,  C07K7/06 ,  C07K14/81 ,  C12N1/21 ,  C12N1/19 ,  C12N5/10 ,  C12N15/15 ,  C12N15/113 ,  C12N15/63 ,  A61K38/57 ,  A61P7/00 ,  A61K38/08 ,  A61K38/10 ,  C07K1/107 ,  C07K7/08

CPC classification number: C07K14/811

Abstract: The present invention relates to a method of modifying serine protease inhibitors in order to acquire or enhance any one of a variety of desired properties, including extent of inhibition, maintenance of inhibition following cleavage of the serine protease inhibitor by the target serine protease, speed of binding to the serine protease, neutralisation, and binding affinity. The present invention also relates to the products of such modifications and the uses of such products, in particular, their use in therapy.

Abstract translation: 本发明涉及一种修饰丝氨酸蛋白酶抑制剂的方法，以获得或增强各种所需性质中的任何一种，包括抑制程度，维持丝氨酸蛋白酶抑制剂被靶丝氨酸蛋白酶切割后的抑制作用 与丝氨酸蛋白酶结合，中和和结合亲和力。 本发明还涉及这些修饰的产品和这些产品的用途，特别是它们在治疗中的用途。

公开(公告)号：US5965698A

公开(公告)日：1999-10-12

申请号：US532818

申请日：1996-05-03

Applicant: Herbert J. Evans ,  R. Manjunatha Kini

Inventor： Herbert J. Evans ,  R. Manjunatha Kini

IPC: A61K38/00 ,  C07K1/00 ,  C07K1/107 ,  C07K14/75 ,  A61K38/04 ,  A61K38/10 ,  A61K38/16 ,  A61K38/36

CPC classification number: C07K1/00 ,  C07K1/1075 ,  C07K14/75 ,  A61K38/00

Abstract: Homologs and analogs of naturally-occurring polypeptides contain one or more interaction sites of the natural counterpart. The interaction sites are flanked by conformation-constraining moieties, such as proline or cysteine.

公开(公告)号：US5948887A

公开(公告)日：1999-09-07

申请号：US933402

申请日：1997-09-19

Applicant: Herbert J. Evans ,  R. Manjunatha Kini

Inventor： Herbert J. Evans ,  R. Manjunatha Kini

IPC: A61K38/00 ,  C07K1/00 ,  C07K1/107 ,  C07K14/70 ,  C07K14/75 ,  C07K7/06 ,  A61K38/04 ,  C07K3/08

CPC classification number: C07K14/70 ,  C07K1/00 ,  C07K1/1075 ,  C07K14/75 ,  A61K38/00

Abstract: Homologs and analogs of naturally-occurring polypeptides contain one or more interaction sites of the natural counterpart. The interaction sites are flanked by conformation-constraining moieties, such as proline or cysteine.

公开(公告)号：US07317003B2

公开(公告)日：2008-01-08

申请号：US09766412

申请日：2001-01-22

Applicant: Ruowen Ge ,  R. Manjunatha Kini

Inventor： Ruowen Ge ,  R. Manjunatha Kini

IPC: A61K38/00 ,  C07K16/00 ,  C12P21/06 ,  C12N1/20

CPC classification number: C07K14/52 ,  A61K38/00 ,  C12N9/6435 ,  C12Y304/21007

Abstract: The present invention provides peptides having potent anti-angiogenic activity and endothelial cell proliferation inhibition activity. The peptides can be administered as pharmaceutical compositions for prevention or treatment of undesired angiogenesis, for instance for prevention of tumor metastasis or inhibition of primary tumor growth.

Abstract translation: 本发明提供具有有效的抗血管生成活性和内皮细胞增殖抑制活性的肽。 肽可以作为用于预防或治疗不需要的血管发生的药物组合物施用，例如用于预防肿瘤转移或抑制原发性肿瘤生长。

公开(公告)号：US6111069A

公开(公告)日：2000-08-29

申请号：US933843

申请日：1997-09-19

Applicant: Herbert J. Evans ,  R. Manjunatha Kini

Inventor： Herbert J. Evans ,  R. Manjunatha Kini

IPC: A61K38/00 ,  C07K1/00 ,  C07K1/107 ,  C07K14/70 ,  C07K14/75 ,  C07K7/06 ,  A61K38/04 ,  A61K37/02 ,  C07K3/08

CPC classification number: C07K14/70 ,  C07K1/00 ,  C07K1/1075 ,  C07K14/75 ,  A61K38/00

Abstract: Homologs and analogs of naturally-occurring polypeptides contain one or more interaction sites of the natural counterpart. The interaction sites are flanked by conformation-constraining moieties, such as proline or cysteine.

公开(公告)号：US5928896A

公开(公告)日：1999-07-27

申请号：US934222

申请日：1997-09-19

Applicant: Herbert J. Evans ,  R. Manjunatha Kini

Inventor： Herbert J. Evans ,  R. Manjunatha Kini

IPC: A61K38/00 ,  C07K1/00 ,  C07K1/107 ,  C07K14/75 ,  C12P21/06 ,  A61K38/04 ,  C12P19/34

CPC classification number: C07K1/00 ,  C07K1/1075 ,  C07K14/75 ,  A61K38/00

Abstract: Homologs and analogs of naturally-occurring polypeptides contain one or more interaction sites of the natural counterpart. The interaction sites are flanked by conformation-constraining moieties, such as proline or cysteine.

公开(公告)号：US06258550B1

公开(公告)日：2001-07-10

申请号：US09413492

申请日：1999-10-06

Applicant: Herbert J. Evans ,  R. Manjunatha Kini

Inventor： Herbert J. Evans ,  R. Manjunatha Kini

IPC: G01N3353

CPC classification number: C07K1/1075 ,  A61K38/00 ,  C07K1/00 ,  C07K14/75

Abstract: Among other things, methods of obtaining putative protein-protein interaction sites of biologically-active polypeptides are provided. The methods include searching the polypeptides for a regions that are flanked on each termini by at least one proline residue; and isolating or producing the flanked regions.

Abstract translation: 提供了获得生物活性多肽的推定蛋白质 - 蛋白质相互作用位点的方法。 所述方法包括：通过至少一个脯氨酸残基搜索在每个末端侧翼的区域的多肽; 并分离或产生侧翼区。

公开(公告)号：US06200954B1

公开(公告)日：2001-03-13

申请号：US09385442

申请日：1999-08-30

Applicant: Ruowen Ge ,  R. Manjunatha Kini

Inventor： Ruowen Ge ,  R. Manjunatha Kini

IPC: A61K3800

CPC classification number: C12N9/6435 ,  A61K38/00 ,  C07K14/52 ,  C12Y304/21007

Abstract: The present invention provides peptides having potent anti-angiogenic activity. The peptides can be administered as pharmaceutical compositions for prevention or treatment of undesired angiogenesis, for instance for prevention of tumor metastasis or inhibition of primary tumor growth.

Abstract translation: 本发明提供具有有效的抗血管生成活性的肽。 肽可以作为用于预防或治疗不需要的血管发生的药物组合物施用，例如用于预防肿瘤转移或抑制原发性肿瘤生长。