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93 条记录 (耗时 0.035 秒)

    Process for the preparation of 4-alkoxyalkyl .beta.-carbolines
    45.
    发明授权
    Process for the preparation of 4-alkoxyalkyl .beta.-carbolines 失效
    4-烷氧基烷基β-咔啉的制备方法

    公开(公告)号：US4945163A

    公开(公告)日：1990-07-31

    申请号：US238086

    申请日：1988-08-30

    申请人： Andreas Huth ,  Dieter Rahtz ,  Ralph Rohde ,  Ralph Schmiechen ,  Dieter Seidelmann

    发明人： Andreas Huth ,  Dieter Rahtz ,  Ralph Rohde ,  Ralph Schmiechen ,  Dieter Seidelmann

    IPC分类号： B01J27/12 ,  C07B61/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： A process is disclosed for the preparation of 4-alkoxyalkyl .beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is an optionally substituted aliphatic hydrocarbon residue,R.sup.3 is lower alkyl, andR.sup.A is hydrogen, halogen, COOR.sup.4 or OR.sup.5, R.sup.4 meaning lower alkyl and R.sup.5 meaning hydrogen, lower alkyl, cycloalkyl, or optionally substituted pheny,by reaction of a compound of Formula II in the presence of AgBF.sub.4 with an alcohol of the formula R.sup.2 OH wherein R.sup.2 has the meanings given above.

    摘要翻译： 公开了用于制备通式I的4-烷氧基烷基β-咔啉衍生物的方法，其中R1是氢或甲基，R2是任选取代的脂族烃残基，R3是低级烷基，RA是氢，卤素 COOR4或OR5，R4表示低级烷基，R5表示氢，低级烷基，环烷基或任选取代的苯基，通过式Ⅱ化合物在AgBF 4存在下与式R 2 OH的醇反应，其中R2具有给定的含义 以上。

    Substituted 5H-pyrimido[5,4-b]indoles
    46.
    发明授权
    Substituted 5H-pyrimido[5,4-b]indoles 失效
    取代的5H-嘧啶并[5,4-b]吲哚

    公开(公告)号：US4564610A

    公开(公告)日：1986-01-14

    申请号：US562248

    申请日：1983-12-16

    申请人： Dieter Rahtz ,  Andreas Huth ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Herbert H. Schneider ,  Claus T. Braestrup

    发明人： Dieter Rahtz ,  Andreas Huth ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Herbert H. Schneider ,  Claus T. Braestrup

    IPC分类号： A61K31/505 ,  A61P25/00 ,  C07D209/42 ,  C07D487/04 ,  C07F9/6561

    CPC分类号： C07D487/04 ,  C07D209/42 ,  C07F9/6561

    摘要： Substituted 5H-pyrimido[5,4-b]indoles of Formula I ##STR1## wherein R.sup.2 is halogen; the oxadiazolyl group ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms; C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, or ##STR3## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR4## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, C.sub.3-5 -alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; andR.sup.A is hydrogen; the oxadiazolyl group ##STR5## wherein R" is lower alkyl with up to 3 carbon atoms; halogen, nitro, OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, ##STR6## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR7## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, cycloalkyl, C.sub.3-5 -alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; orPO(OR).sub.2 wherein R is C.sub.1-5 -alkyl, exhibit strong affinity for binding to benzodiazepine receptors.The novel compounds are suitable for use in psychopharmaceutical preparations.

    摘要翻译： 取代的式I的5H-嘧啶并[5,4-b]吲哚其中R 2是卤素; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; C 1-5 - 烷基，环烷基，芳烷基或芳基; ORI，nn为0,1或2，或其中R 1为氢，C 1-5 - 烷基，环烷基，芳烷基或芳基的SO nRI; 其中RII和RIII是氢，C1-5-烷基，C3-5-烯基，环烷基，芳烷基，芳基，或具有连接的N-原子的5-或6-元杂环; RA为氢; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; 卤素，硝基，ORI，nn为0,1或2的SO nRI，其中R 1为氢，C 1-5 - 烷基，环烷基，芳烷基或芳基; 其中RII和RIII是氢，C1-5烷基，环烷基，C3-5-烯基，芳烷基，芳基，或具有连接的N-原子的5或6元杂环; 或其中R为C 1-5 - 烷基的PO（OR）2表现出对苯并二氮杂受体结合的强亲合力。 新型化合物适用于精神药物制剂。

    VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
    48.
    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：US20070015794A1

    公开(公告)日：2007-01-18

    申请号：US11525091

    申请日：2006-09-22

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

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

    IPC分类号： A61K31/444 ,  A61K31/44 ,  C07D401/02 ,  C07D213/72

    CPC分类号： C07D213/72 ,  C07D401/02

    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
    49.
    发明授权
    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：US07615565B2

    公开(公告)日：2009-11-10

    申请号：US11525091

    申请日：2006-09-22

    申请人： Andreas Huth ,  Ludwig Zorn ,  Martin Kruger ,  Stuat Ince ,  Karl-Heinz Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

    发明人： Andreas Huth ,  Ludwig Zorn ,  Martin Kruger ,  Stuat Ince ,  Karl-Heinz Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

    IPC分类号： A61K31/47 ,  C07D217/22

    CPC分类号： C07D213/72 ,  C07D401/02

    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。