中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

170 records (took 0.022 seconds)

    SUBSTITUTED 1, 4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVE COMBINED WITH AN OPIOID ANALGESIC AND THEIR USE FOR THE TREATMENT OF PAIN AND SIDE-EFFECTS ASSOCIATED WITH OPIOID-BASED TREATMENTS
    1.
    发明申请
    SUBSTITUTED 1, 4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVE COMBINED WITH AN OPIOID ANALGESIC AND THEIR USE FOR THE TREATMENT OF PAIN AND SIDE-EFFECTS ASSOCIATED WITH OPIOID-BASED TREATMENTS 审中-公开
    取代4-DI-PIPERIDIN-4-YL-哌啶衍生物与阿片样物质联用及其用于治疗与基于阿片类药物治疗相关的疼痛和副作用的用途

    公开(公告)号：WO2004110415A3

    公开(公告)日：2005-02-10

    申请号：PCT/EP2004051048

    申请日：2004-06-07

    Applicant: JANSSEN PHARMACEUTICA NV ,  JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  DE BOECK BENOIT CHRISTIAN ALBE ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROOSBROECK YVES EMIEL MARI ,  MEERT THEO FRANS

    Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  DE BOECK BENOIT CHRISTIAN ALBE ,  LEENAERTS JOSEPH ELISABETH ,  VAN ROOSBROECK YVES EMIEL MARI ,  MEERT THEO FRANS

    IPC: A61K31/496 ,  A61K31/551 ,  A61K45/06 ,  A61P1/08 ,  A61P11/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/36 ,  A61K31/33 ,  A61K31/433 ,  A61K31/4468 ,  A61K31/485

    CPC classification number: A61K45/06 ,  A61K31/496 ,  A61K31/551 ,  A61K2300/00

    Abstract: This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in opioidbased acute and chronic pain treatments, more in particular in inflammatory, postoperative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK1-receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise a pharmaceutically acceptable carrier and, as active ingredients, a therapeutically effective amount of an opioid analgesic and NKI -antagonists according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochernically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side­effects associated with opioid analgesics, in particular emesis, respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.

    Abstract translation: 本发明涉及基于阿片样物质治疗疼痛和/或伤害感受的新制剂，其包括具有神经激肽拮抗活性的阿片类镇痛药和1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK1拮抗活性，所述制剂的用途 用于制备用于预防和/或治疗呕吐，疼痛和/或伤害感受的药物，特别是在阿片样物质的急性和慢性疼痛治疗中，特别是在炎性，术后，急诊室（ER），突破性，神经性和 癌症疼痛治疗和NK1受体拮抗剂在制备用于预防和/或治疗基于阿片样物质的疼痛治疗中的呼吸抑制的药物中的用途。 根据本发明的药物制剂包含药学上可接受的载体和作为活性成分的治疗有效量的根据通式（I）的阿片类镇痛药和NKI拮抗剂其药学上可接受的酸或碱加成盐，立体选择性 其异构体形式，其N-氧化物形式和其前药，其中所有取代基如权利要求1中所定义。根据本发明的药物组合物在很大程度上降低了与阿片类镇痛药有关的多种不希望的副作用，特别是呕吐， 呼吸抑制和耐受性，从而增加所述阿片样物质在疼痛治疗中的总耐受性。

    USE OF MTKI 1 FOR TREATING OR PREVENTING BONE CANCER
    2.
    发明申请
    USE OF MTKI 1 FOR TREATING OR PREVENTING BONE CANCER 审中-公开
    使用MTKI 1治疗或预防骨癌

    公开(公告)号：WO2008049904A3

    公开(公告)日：2009-01-15

    申请号：PCT/EP2007061501

    申请日：2007-10-25

    Applicant: JANSSEN PHARMACEUTICA NV ,  PERERA TIMOTHY PIETRO SUREN ,  JANICOT MICHEL MARIE FRANCOIS ,  MEERT THEO FRANS ,  FREYNE EDDY JEAN EDGARD

    Inventor： PERERA TIMOTHY PIETRO SUREN ,  JANICOT MICHEL MARIE FRANCOIS ,  MEERT THEO FRANS ,  FREYNE EDDY JEAN EDGARD

    IPC: A61K31/529 ,  A61P35/00 ,  A61P35/04

    CPC classification number: A61K31/529

    Abstract: The present invention is concerned with the finding that the macrocyclic quinazoline derivative 4,6-ethanediylidenepyrimido[4,5-b][6,1,12]benzoxadiazacyclo-pentadecine, 17-bromo-8,9,10,11,12,13, 14,19-octahydro-20-methoxy-13-methyl-, described as compound 22 in PCT publication WO2004/105765, is useful in the manufacture of a medicament for the treatment or prevention of bone cancers and methods for killing bone cancer cells, including osteosarcomas, chondrosarcomas, myeloma bone disease and osteolytic bone metastases from other primary sites. It accordingly provides methods for treating, preventing, delaying or mitigating bone cancer, or for preventing and treating of bone loss associated with cancer metastases.

    Abstract translation: 本发明涉及大环喹唑啉衍生物4,6-乙二亚甲基嘧啶并[4,5-b] [6,1,12]苯并恶二氮杂环十五碳烯，17-溴-8,9,10,11,12， 在PCT公开WO2004 / 105765中描述为化合物22的13,14,19-八氢-20-甲氧基-13-甲基可用于制备用于治疗或预防骨癌的药物和用于杀死骨癌的方法 细胞，包括骨肉瘤，软骨肉瘤，骨髓瘤骨病和其他原发部位的骨溶解性骨转移。 因此，它提供了治疗，预防，延缓或减轻骨癌或预防和治疗与癌症转移相关的骨丢失的方法。

    5.
    发明专利
    未知

    公开(公告)号：BRPI0718021A2

    公开(公告)日：2013-11-12

    申请号：BRPI0718021

    申请日：2007-10-25

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： PERERA TIMOTHY PIETRO SUREN ,  JANICOT MICHEL MARIE FRANCOIS ,  MEERT THEO FRANS ,  FREYNE EDDY JEAN EDGARD

    IPC: A61K31/529 ,  A61P35/00 ,  A61P35/04

    Abstract: The present invention is concerned with the finding that the macrocyclic quinazoline derivative 4,6-ethanediylidenepyrimido[4,5-b][6,1,12]benzoxadiazacyclo-pentadecine, 17-bromo-8,9,10,11,12,13, 14,19-octahydro-20-methoxy-13-methyl-, described as compound 22 in PCT publication WO2004/105765, is useful in the manufacture of a medicament for the treatment or prevention of bone cancers and methods for killing bone cancer cells, including osteosarcomas, chondrosarcomas, myeloma bone disease and osteolytic bone metastases from other primary sites. It accordingly provides methods for treating, preventing, delaying or mitigating bone cancer, or for preventing and treating of bone loss associated with cancer metastases.

    8.
    发明专利
    未知

    公开(公告)号：AT395062T

    公开(公告)日：2008-05-15

    申请号：AT04741745

    申请日：2004-06-07

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  LEENAERTS JOSEPH E ,  VAN ROOSBROECK Y E M ,  MEERT THEO FRANS

    IPC: A61K31/496 ,  A61K31/4468 ,  A61K31/485 ,  A61P25/04

    Abstract: This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1-(1,2-disubstituted piperidinyl)-4-substituted piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK 1 -receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression and tolerance in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise NK 1 -antagonists according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid analgesics, in particular respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.

Patent Agency Ranking