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    Method of treating bone or prostate cancer with selective bradykinin B1 receptor antagonists
    1.
    发明授权
    Method of treating bone or prostate cancer with selective bradykinin B1 receptor antagonists 有权
    用选择性缓激肽B1受体拮抗剂治疗骨或前列腺癌的方法

    公开(公告)号：US07932228B2

    公开(公告)日：2011-04-26

    申请号：US11451142

    申请日：2006-06-12

    申请人： François Nantel ,  Roger Chammas ,  Pierre Sirois ,  Bruno Joseph Battistini

    发明人： François Nantel ,  Roger Chammas ,  Pierre Sirois ,  Bruno Joseph Battistini

    IPC分类号： A61K38/10 ,  C07K7/18

    CPC分类号： A61K38/08 ,  A61K31/282 ,  A61K31/337

    摘要： Provided is a method for the use of a bradykinin B1 receptor antagonist of formula I: X-CO-Aaa0-Aaa1-Aaa2-Aaa3-Gly-α(Me)Phe-Ser-D-βNal-Aaa8-OH (I) or a pharmaceutically acceptable salt or hydrate thereof wherein: X is CnH2n+1 or CiH2i—C6H5, where n is an integer from 1 to 3, and i is an integer from 0 to 3; Aaa0 is Lys, Orn or Cit; Aaa1 is Arg or Cit, and preferably Arg; Aaa2 is Oic, Hyp or Pro, and preferably Oic; Aaa3 is Pro or Oic, and preferably Pro; and Aaa8 is Ile, Leu or Nle, and preferably Ile, for the treatment of metastases, cancers and/or chemotherapy-induced neuropathies, comprising the administration of the compound to a patient in need of such treatment. Also provided are compositions containing such antagonists and their thereof.

    摘要翻译： 提供了使用式I的缓激肽B1受体拮抗剂的方法：X-CO-Aaa0-Aaa1-Aaa2-Aaa3-Gly-α（Me）Phe-Ser-D-bgr; Nal-Aaa8-OH（I ）或其药学上可接受的盐或水合物，其中：X为C n H 2n + 1或C 1 H 21 -C 6 H 5，其中n为1至3的整数，i为0至3的整数; Aaa0是Lys，Orn或Cit; Aaa1是Arg或Cit，优选Arg; Aaa2是Oic，Hyp或Pro，优选Oic; Aaa3是Pro或Oic，优选Pro; Aaa8是Ile，Leu或Nle，优选Ile，用于治疗转移，癌症和/或化学疗法诱发的神经病，包括向需要这种治疗的患者施用该化合物。 还提供了含有这些拮抗剂及其制备方法的组合物。

    DUAL ANTAGONISM OF ENDOTHELIN TYPE A AND BRADYKININ B1 RECEPTORS FOR TREATING PAIN AND PREVENTING CARTILAGE DEGRADATION
    2.
    发明申请
    DUAL ANTAGONISM OF ENDOTHELIN TYPE A AND BRADYKININ B1 RECEPTORS FOR TREATING PAIN AND PREVENTING CARTILAGE DEGRADATION 审中-公开
    内皮素A型和BRADYKININ B1受体的双重拮抗剂治疗疼痛和预防卡他汀降解

    公开(公告)号：US20120202744A1

    公开(公告)日：2012-08-09

    申请号：US13366036

    申请日：2012-02-03

    申请人： Florina MOLDOVAN ,  Gabriel Nathan Kaufman ,  Pierre Sirois

    发明人： Florina MOLDOVAN ,  Gabriel Nathan Kaufman ,  Pierre Sirois

    IPC分类号： A61K38/12 ,  A61P29/00 ,  A61P19/02 ,  A61P25/04

    CPC分类号： A61K38/08 ,  A61K38/12 ,  A61K2300/00

    摘要： The present invention relates to the field of anatomy, and more particularly to the control of pain and to the prevention and treatment of osteoarthritic cartilage degradation. Described herein are methods for treating pain which comprise administering to a subject in need a combination of (i) an antagonist of the endothelin type A receptor (ETA) and (ii) an antagonist of the bradykinin B1 receptor (BKB1). Also described are methods for preventing osteoarthritic cartilage degradation and pharmaceutical compositions for treating pain, for preventing osteoarthritic cartilage degradation, and/or for preventing osteoarthritic joint inflammation, in subjects.

    摘要翻译： 本发明涉及解剖学领域，更具体地涉及控制疼痛和预防和治疗骨关节炎软骨退化。 本文描述了治疗疼痛的方法，其包括向需要的受试者施用（i）A型内皮素受体拮抗剂（ETA）和（ii）缓激肽B1受体拮抗剂（BKB1）的组合。 还描述了用于预防骨关节炎软骨降解的方法和用于治疗受试者的疼痛，用于预防骨关节炎软骨退化和/或预防骨关节炎关节炎症的药物组合物。

    Selective bradykinin (BK) B1 peptidic receptor antagonists and uses thereof
    5.
    发明授权
    Selective bradykinin (BK) B1 peptidic receptor antagonists and uses thereof 有权
    选择性缓激肽（BK）B1肽受体拮抗剂及其应用

    公开(公告)号：US07211566B2

    公开(公告)日：2007-05-01

    申请号：US10405088

    申请日：2003-04-01

    申请人： Domenico Regoli ,  Witold Neugebauer ,  Fernand Gobeil ,  Bichov Gabra ,  Pierre Sirois

    发明人： Domenico Regoli ,  Witold Neugebauer ,  Fernand Gobeil ,  Bichov Gabra ,  Pierre Sirois

    IPC分类号： A61K38/00 ,  A61K38/04 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00

    CPC分类号： C07K7/18 ,  A61K38/00

    摘要： The present invention provides for a novel peptidic antagonist for the bradykinin B1 (BKB1) receptor having very good to excellent affinities and selectivity for the BKB1 receptor, in vitro and in vivo increase resistance to enzymatic degradation, superior pharmacokinetic properties, capability to significantly reduce microvascular leakage observed alongside diabetic-induced increase in vascular permeability, capability to significantly reduced the state of hyperalgesia alongside diabetes, capability to significantly reduce the infiltration of pro-inflammatory cells and general state of inflammation alongside allergic asthma.

    摘要翻译： 本发明提供了一种用于缓冲激素B1（BKB 1 H 2）受体的新型肽拮抗剂，其在体外和体外对BKB 1 H 2受体具有非常好的至优异的亲和力和选择性 体内增加对酶降解的抗性，优异的药代动力学性质，显着降低血管渗透的可能性，同时伴随着糖尿病引起的血管通透性增加，显着降低与糖尿病同时降低痛觉过敏状态的能力，显着减少促炎细胞浸润的能力，以及 一般情况与过敏性哮喘一起发生。

    Method of treating cancer and neuropathic complications induced by chemotherapeutic agents using selective Bradykinin B1 receptor antagonists
    7.
    发明申请
    Method of treating cancer and neuropathic complications induced by chemotherapeutic agents using selective Bradykinin B1 receptor antagonists 有权
    使用选择性缓激肽B1受体拮抗剂治疗由化学治疗剂诱导的癌症和神经性并发症的方法

    公开(公告)号：US20070015715A1

    公开(公告)日：2007-01-18

    申请号：US11451142

    申请日：2006-06-12

    申请人： Francois Nantel ,  Roger Chammas ,  Pierre Sirois ,  Bruno Battistini

    发明人： Francois Nantel ,  Roger Chammas ,  Pierre Sirois ,  Bruno Battistini

    IPC分类号： A61K38/08 ,  A61K31/337 ,  A61K31/282

    CPC分类号： A61K38/08 ,  A61K31/282 ,  A61K31/337

    摘要： The present invention relates to a method for the use of a bradykinin B1 receptor antagonist of formula I: X—CO-Aaa0-Aaa1-Aaa2-Aaa3-Gly-α(Me)Phe-Ser-D-βNal-Aaa8-OH  (I)or a pharmaceutically acceptable salt or hydrate thereof wherein: X is CnH2n+1 or CiH2i—C6H5, where n is an integer from 1 to 3, and i is an integer from 0 to 3; Aaa0 is Lys, Orn or Cit; Aaa1 is Arg or Cit, and preferably Arg; Aaa2 is Oic, Hyp or Pro, and preferably Oic; Aaa3 is Pro or Oic, and preferably Pro; and Aaa8 is Ile, Leu, Nle, and preferably Ile, for the treatment of metastases, cancers and/or chemotherapy-induced neuropathies, comprising the administration of said compound to a patient in need of such treatment. The present invention also relates to compositions containing such antagonists and the uses thereof.

    摘要翻译： 本发明涉及使用式I的缓激肽B1受体拮抗剂的方法：<？in-line-formula description =“In-line Formulas”end =“lead”→> X-CO-Aaa 0A-Aaa 1 -Aaa 2 -Aaa 3 -Gly-α（Me）Phe-Ser-D-βNal- Aaa 8 -OH（I）<？in-line-formula description =“In-line Formulas”end =“tail”？>或其药学上可接受的盐或水合物，其中：X为C < H 2 H 2n + 1或C 1 H 2 C 1 -C 6 H 3 其中n为1〜3的整数，i为0〜3的整数， Aaa 是Lys，Orn或Cit; Aaa 1是Arg或Cit，优选Arg; Aaa 2是Oic，Hyp或Pro，优选Oic; Aaa 3是Pro或Oic，优选Pro; Aaa 8是Ile，Leu，Nle，优选Ile，用于治疗转移，癌症和/或化学疗法诱发的神经病，包括向需要这种治疗的患者施用所述化合物 。 本发明还涉及含有这种拮抗剂的组合物及其用途。