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    CYCLIC PEPTIDE DERIVATIVES AS INHIBITORS OF INTEGRIN alpha V beta 6
    11.
    发明申请
    CYCLIC PEPTIDE DERIVATIVES AS INHIBITORS OF INTEGRIN alpha V beta 6 审中-公开
    环状肽衍生物作为抑制剂的整合素v的β6

    公开(公告)号：WO0105810A3

    公开(公告)日：2001-05-17

    申请号：PCT/EP0006188

    申请日：2000-07-03

    Applicant: MERCK PATENT GMBH ,  JONCZYK ALFRED ,  DIEFENBACH BEATE ,  GOODMAN SIMON ,  GROTH ULRICH ,  ZISCHINSKY GUNTHER

    Inventor： JONCZYK ALFRED ,  DIEFENBACH BEATE ,  GOODMAN SIMON ,  GROTH ULRICH ,  ZISCHINSKY GUNTHER

    IPC: A61K38/00 ,  A61P7/02 ,  A61P9/10 ,  A61P17/02 ,  A61P17/06 ,  A61P19/10 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P43/00 ,  C07K7/50 ,  C07K7/64 ,  C07K7/56 ,  A61K38/04

    CPC classification number: C07K7/64 ,  A61K38/00

    Abstract: The invention relates to novel peptide derivatives of formula (I): Cyclo-(Arg-X -Asp-X -X -X -X -X -R ); which are biologically active as ligands of integrin alpha v beta 6, X representing Ser, Gly or Thr; X representing Leu, Ile, Nle, Val or Phe; X representing Asp, Glu, Lys or Phe; X representing Gly, Ala or Ser; X representing Leu, Ile, Nle, Val or Phe; X representing Arg, Har or Lys; and R being left out or representing one or more omega -aminocarboxylic acid radicals, said omega -aminocarboxylic acid radical(s) being 500 to 2500 pm in length. Said amino acids can also be derivatised and the D and L forms of the optically active amino acid radicals are enclosed. The invention also relates to the physiologically suitable salts and solvates of the inventive derivatives.

    Abstract translation: 本发明涉及适用作的整合素v的β6配体的生物活性式（I）的新型肽衍生物：环（精氨酸 - X <1> -Asp-X <2> -X <3> -X <4> -X <5> -X <6> -R <1>），其中X <1>丝氨酸，甘氨酸或Thr，X <2>亮氨酸，异亮氨酸，NLE，缬氨酸或Phe，X <3>天冬氨酸，谷氨酸， 赖氨酸或Phe，X <4>甘氨酸，丙氨酸，或Ser，X <5>亮氨酸，异亮氨酸，NLE，缬氨酸或Phe，X <6>精氨酸中，HAr或Lys，R <1>不存在或一种或多种ω-Aminocarbonsäurerest （e）其中，所述一种或多种ω-Aminocarbonsäurerest（E）具有500至2500分的长度已平均，其中所述氨基酸也可以被衍生化，其被并入D-和光学活性的氨基酸残基的L型， 和生理上可接受的盐和溶剂合物。

    CYCLIC PEPTIDE DERIVATIVES
    12.
    发明申请
    CYCLIC PEPTIDE DERIVATIVES 审中-公开
    CYCLO肽衍生物

    公开(公告)号：WO1998027112A1

    公开(公告)日：1998-06-25

    申请号：PCT/EP1997007048

    申请日：1997-12-15

    Applicant: MERCK PATENT GMBH ,  HÖLZEMANN, Günter ,  FITTSCHEN, Claus ,  GOODMAN, Simon

    Inventor： MERCK PATENT GMBH

    IPC: C07K07/56

    CPC classification number: C07K7/56 ,  A61K38/00

    Abstract: Compounds of the formula (I) Cyclo-(Arg-X-Asp-R ) in which X means Gly, Ala or NH-NH-CO, R means a radical of formula (II), and R , R , and R have the meanings given in claim 1, and their salts, can be used as integrin inhibitors, in particular for the prevention and treatment of circulatory diseases, in cases of thrombosis, cardiac infarction, coronary heart disease, arteriosclerosis, pathological symptoms that are sustained or propagated by angiogenesis, and in tumour therapy.

    Abstract translation: 式（I）化合物：环 - （Arg-X-天冬氨酸-R <1>），其中X为Gly，Ala或NH-NH-CO，R <1>是下式基团（II），且R <2 >，R <3>，和R <4>具有权利要求1中给出的含义和它们的盐可以用作整联蛋白抑制剂，特别是用于循环，血栓形成障碍，心肌梗死，冠状动脉心脏疾病，动脉硬化，其中的预防和治疗 其由血管发生维持或传播，并且在肿瘤治疗中使用的病理过程。

    SPECIFIC THERAPY AND MEDICAMENT USING INTEGRIN LIGANDS FOR TREATING CANCER
    14.
    发明申请
    SPECIFIC THERAPY AND MEDICAMENT USING INTEGRIN LIGANDS FOR TREATING CANCER 审中-公开
    使用整合配体治疗癌症的特殊治疗和药物

    公开(公告)号：WO2009010287A2

    公开(公告)日：2009-01-22

    申请号：PCT/EP2008005831

    申请日：2008-07-17

    Applicant: MERCK PATENT GMBH ,  KRUEGER STEFAN ,  GOODMAN SIMON

    Inventor： KRUEGER STEFAN ,  GOODMAN SIMON

    IPC: A61K38/00 ,  A61P35/00

    CPC classification number: A61K45/06

    Abstract: The invention relates to a combination therapy for the treatment of tumors and tumor metastases comprising administration of integrin ligands, preferably integrin antagonists, together with co-therapeutic agents or therapy forms that have synergistic efficacy when administered consecutively with said ligands, such as chemotherapeutic agents and or radiation therapy. The therapy results in a synergistic potential increase of the inhibition effect of each individual therapeutic on tumor cell proliferation, yielding more effective treatment than found by administering an individual component alone, concurrently or not in the dosage regime of the present invention.

    Abstract translation: 本发明涉及用于治疗肿瘤和肿瘤转移的组合疗法，其包括施用整联蛋白配体，优选整联蛋白拮抗剂，以及当与所述配体连续施用时具有协同效力的辅助治疗剂或疗法形式，例如化疗剂和 或放射疗法。 该疗法导致每种单独治疗剂对肿瘤细胞增殖的抑制作用的协同潜在增加，产生比通过同时或不在本发明的剂量方案中单独施用单独组分而发现的更有效的治疗。

    COMBINATION THERAPY USING ANTI-ANGIOGENIC AGENTS AND TNFa
    17.
    发明申请
    COMBINATION THERAPY USING ANTI-ANGIOGENIC AGENTS AND TNFa 审中-公开
    使用抗血管生成剂和TNFa的联合治疗

    公开(公告)号：WO2002085405A2

    公开(公告)日：2002-10-31

    申请号：PCT/EP2002/004298

    申请日：2002-04-18

    Applicant: MERCK PATENT GMBH ,  GRELL, Matthias ,  GOODMAN, Simon ,  RUEGG, Curzio

    Inventor： GRELL, Matthias ,  GOODMAN, Simon ,  RUEGG, Curzio

    IPC: A61K38/19

    CPC classification number: A61K38/08 ,  A61K38/191 ,  A61K38/217 ,  A61K39/39541 ,  A61K2300/00

    Abstract: The invention relates to a combination therapy for the treatment of tumors metastases comprising administration of anti-angiogenic agents and tumor necrosis factor alpha (TNFa) optionally together with other cytotoxic agents, such as interferon gamma (IFNy) orchemotherapeutic agents such as anti-EGFR antibodies. The method and the pharmaceuticalcompositions comprising said agents can result in a synergistic potentiation of the tumor cell proliferation inhibition effect of each individual therapeutic agent, yielding more effective treatment than found by administering an individual component alone.

    Abstract translation: 本发明涉及用于治疗肿瘤转移的组合疗法，包括任选地与其它细胞毒剂如干扰素γ（IFNγ）或化学治疗剂如抗EGFR抗体一起施用抗血管生成剂和肿瘤坏死因子α（TNFa） 。 包含所述试剂的方法和药物组合物可以导致每种单独治疗剂的肿瘤细胞增殖抑制作用的协同增强作用，产生比通过单独施用单独组分发现的更有效的治疗。

    INHIBITORS OF INTEGRIN αvβ6
    18.
    发明申请
    INHIBITORS OF INTEGRIN αvβ6 审中-公开
    INTEGRIN alpha v beta 6的抑制剂

    公开(公告)号：WO2002074730A1

    公开(公告)日：2002-09-26

    申请号：PCT/EP2002/001836

    申请日：2002-02-21

    Applicant: MERCK PATENT GMBH ,  SCHADT, Oliver ,  JONCZYK, Alfred ,  STÄHLE, Wolfgang ,  GOODMAN, Simon

    Inventor： SCHADT, Oliver ,  JONCZYK, Alfred ,  STÄHLE, Wolfgang ,  GOODMAN, Simon

    IPC: C07C237/04

    CPC classification number: C07D213/74 ,  C07D401/12 ,  C07D409/12

    Abstract: Novel biphenyl derivatives of the general formula (I) in which R 1 , R 1' , R 1" , R 2 , R 2' , R 3 and n are as defined in Claim 1, their stereoisomers and their physiologically acceptable salts or solvates are novel integrin inhibitors which preferentially inhibit the α v β 6 integrin receptor. The novel compounds can be used, in particular, as medicaments.

    Abstract translation: 通式（I）的新型联苯衍生物，其中R 1，R 1，R 1，R 2，R 2'，R 3和n如 权利要求1，其立体异构体及其生理学上可接受的盐或溶剂合物是优选抑制αvβ6整联蛋白受体的新型整联蛋白抑制剂，特别是作为药物使用。

    PHENYLALAMINE DERIVATIVES AS INTEGRIN INHIBITORS
    20.
    发明申请
    PHENYLALAMINE DERIVATIVES AS INTEGRIN INHIBITORS 审中-公开
    苯丙氨酸衍生物作为整联蛋白抑制剂

    公开(公告)号：WO1998000395A1

    公开(公告)日：1998-01-08

    申请号：PCT/EP1997003275

    申请日：1997-06-23

    Applicant: MERCK PATENT GMBH ,  DIEFENBACH, Beate ,  FITTSCHEN, Claus ,  GOODMAN, Simon ,  MÄRZ, Joachim ,  RADDATZ, Peter ,  WIESNER, Matthias ,  ANZALI, Soheila

    Inventor： MERCK PATENT GMBH

    IPC: C07C311/06

    CPC classification number: C07D277/46 ,  C07C311/06 ,  C07C311/14 ,  C07C311/19 ,  C07D231/40 ,  C07D233/88 ,  C07D235/30 ,  C07D257/04

    Abstract: Compounds of formula (I) wherein X, Y, Z, R , R , R and R have the meaning stated in claim 1, with the proviso that at least one element chosen from the group X, Y, Z must be CH2, as well as their physiologically harmless salts, can be used as integrin inhibitors, particularly for prophylaxis and treatment of circulatory diseases, in case of thrombosis, heart infarct, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological processes which are maintained or propagated by angiogenesis, and in tumor therapy.

    Abstract translation: 其中X，Y，Z，R <1>，R <2>，R <3>和R <4>已经根据权利要求1中所示的含义，其条件是至少一个元素选自式（I）的化合物 必须从基团X，Y中选择，Z为CH 2，和它们的生理学可接受的盐可以用作整联蛋白抑制剂，特别是对循环，血栓形成，心肌梗塞，冠状动脉心脏疾病，动脉硬化症，骨质疏松症的疾病的预防和治疗，在病理过程，由 招待血管生成或传播并在肿瘤治疗中使用。

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