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    5-fluorocarbacyclins, their preparation and pharmaceutical use
    1.
    发明授权
    5-fluorocarbacyclins, their preparation and pharmaceutical use 失效
    5-氟卡巴环素，其制备和药物用途

    公开(公告)号：US5190964A

    公开(公告)日：1993-03-02

    申请号：US480448

    申请日：1990-02-15

    申请人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Martin Haberey ,  Claus-Steffen Sturzebecher ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Martin Haberey ,  Claus-Steffen Sturzebecher ,  Michael-Harold Town

    IPC分类号： C07C405/00 ,  C07D263/14

    CPC分类号： C07D263/14 ,  C07C405/0083

    摘要： 5-fluorocarbacyclin derivatives of the Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH orA is --CH.sub.2 --CH.sub.2 --, trans --CH.dbd.CH-- or --C.tbd.C--,W is a free or functionally modified hydroxymethylene group or free or functionally modified ##STR2## in which the OH group can be in the .alpha.-- or .beta.-position, D is ##STR3## a C.sub.1-10 -aliphatic group (e.g., alkyl or alkenyl) which optionally can be substituted by fluorine atoms,n is 1, 2 or 3,E is a direct bond, --C.tbd.C-- or --CR.sub.6 .tbd.CR.sub.7 -- in which R.sub.6 represents a hydrogen atom or an alkyl group with 1-5 atoms and R.sub.7 represents a hydrogen atom, a halogen atom or an alkyl group with 1-5 C atoms,R.sub.4 is alkyl, cycloalkyl or optionally substituted aryl or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy groupand, when R.sub.2 is a hydrogen atom, its salts with physiologically compatible bases,have valuable pharmacological properties.

    摘要翻译： 其中R 1是CH 2 OH或A是-CH 2 -CH 2 - ，反式-CH = CH-或-CB 3 C，其中W是游离的或官能改性的羟基亚甲基，或游离或官能改性的羟基亚甲基， 官能改性的“IMAGE”，其中OH基团可以是α或β-位，D是可任选被氟原子取代的C 1-10脂族基团（例如烷基或烯基），n 是1,2或3，E是直接键，-C 3 D或-CR 6 3BOND CR 7 - ，其中R 6表示氢原子或具有1-5个原子的烷基，R 7表示氢原子，卤素原子 或具有1-5个C原子的烷基，R4是烷基，环烷基或任选取代的芳基或杂环基，R5是游离或官能改性的羟基，当R2是氢原子时，其与生理上相容的碱的盐， 具有宝贵的药理性质。

    N-oxide anthranylamide derivatives and their use as medicaments
    4.
    发明授权
    N-oxide anthranylamide derivatives and their use as medicaments 失效
    N-氧化物苯甲酰胺衍生物及其作为药物的用途

    公开(公告)号：US07459470B2

    公开(公告)日：2008-12-02

    申请号：US10476755

    申请日：2002-05-03

    申请人： Alexander Ernst ,  Andreas Huth ,  Martin Krueger ,  Karl-Heniz Thierauch ,  Andreas Menrad ,  Martin Haberey

    发明人： Alexander Ernst ,  Andreas Huth ,  Martin Krueger ,  Karl-Heniz Thierauch ,  Andreas Menrad ,  Martin Haberey

    IPC分类号： A61K31/47 ,  C07D213/89

    CPC分类号： C07D213/89 ,  C07D401/12 ,  C07D405/12

    摘要： Substituted N-oxidanthranilamide derivatives, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds according to the invention can be used as or in the case of psoriasis, Kaposi's sarcoma, restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver, mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.

    摘要翻译： 描述了取代的N-氧化邻氨基苯甲酰胺衍生物，其作为用于治疗由持续性血管生成触发的疾病的药剂的生产和用途被描述。 根据本发明的化合物可以用作银屑病，卡波西肉瘤，再狭窄，子宫内膜异位症，克罗恩病，霍奇金病，白血病，牛皮癣， 关节炎，如类风湿关节炎，血管瘤，血管纤维瘤; 眼睛疾病如糖尿病性视网膜病变，新生血管性青光眼; 肾脏疾病如肾小球性肾炎，糖尿病肾病，恶性肾硬化，血栓性微血管病综合征，移植排斥反应和肾小球病; 纤维化疾病，如肝硬化，肾小球膜细胞增生性疾病，动脉硬化，神经组织损伤，以及球囊导管治疗后血管再狭窄的抑制，血管修复术或机械装置用于保持血管开放的诸如 例如作为免疫抑制剂的支架，作为无疤痕愈合的支持，老年角化病和接触性皮炎。 在淋巴管生成的情况下，根据本发明的化合物也可以用作VEGFR-3抑制剂。

    VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
    8.
    发明申请
    VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines 失效
    VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶

    公开(公告)号：US20050054654A1

    公开(公告)日：2005-03-10

    申请号：US10870491

    申请日：2004-06-18

    申请人： Andreas Huth ,  Ludwig Zorn ,  Martin Krueger ,  Stuart Ince ,  Karl Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

    发明人： Andreas Huth ,  Ludwig Zorn ,  Martin Krueger ,  Stuart Ince ,  Karl Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

    IPC分类号： C07D213/61 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D43/02 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07D41/02

    CPC分类号： C07D213/61 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

    摘要： VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver; mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.

    摘要翻译： 描述了VEGFR-2和VEGFR-3抑制性邻氨基苯酰胺吡啶酰胺，其作为用于治疗由持续血管发生引起的疾病的药物的制备和用途，以及用于制备化合物的中间产物。 根据本发明的化合物可用于或在肿瘤或转移生长的情况下，牛皮癣，卡波西肉瘤，再狭窄，例如支架诱导的再狭窄，子宫内膜异位，克罗恩病，霍奇金病，白血病; 关节炎，如类风湿关节炎，血管瘤，血管纤维瘤; 眼睛疾病如糖尿病性视网膜病变，新生血管性青光眼; 肾脏疾病如肾小球性肾炎，糖尿病肾病，恶性肾硬化，血栓性微血管病综合征，移植排斥反应和肾小球病; 纤维化疾病，如肝硬化; 肾小球膜细胞增生性疾病，动脉硬化，神经组织损伤，以及球囊导管治疗后血管假体中或使用机械装置用于保持血管开放（例如，支架）作为免疫抑制剂的抑制，作为免疫抑制剂 无疤痕愈合，老年角化病和接触性皮炎的支持。 在淋巴管生成的情况下，根据本发明的化合物也可以用作VEGFR-3抑制剂。