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    VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
    62.
    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：US07517894B2

    公开(公告)日：2009-04-14

    申请号：US10870491

    申请日：2004-06-18

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

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

    IPC分类号： A61K31/4439 ,  C07D401/04

    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。

    Cyanoanthranilamide derivatives and the use thereof as medicaments
    63.
    发明授权
    Cyanoanthranilamide derivatives and the use thereof as medicaments 失效
    氰基脒酰胺衍生物及其作为药物的用途

    公开(公告)号：US07429592B2

    公开(公告)日：2008-09-30

    申请号：US10476761

    申请日：2002-05-03

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

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

    IPC分类号： C07D401/12 ,  A61K31/44 ,  A61K31/47

    CPC分类号： C04B35/632 ,  C07D401/12

    摘要： Substituted cyanoanthranilamide 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, 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： 取代的氰基邻氨基苯甲酰胺衍生物，其制备和用作治疗由持续血管发生引发的疾病的药物。 根据本发明的化合物可以用作牛皮癣，卡波西肉瘤，再狭窄，例如支架诱导的再狭窄，子宫内膜异位症，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。

    N-oxide anthranylamide derivatives and their use as medicaments
    65.
    发明申请
    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：US20050032816A1

    公开(公告)日：2005-02-10

    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： A61K31/4425 ,  A61K31/47 ,  A61P1/04 ,  A61P1/16 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P27/02 ,  A61P27/06 ,  A61P35/00 ,  A61P35/02 ,  A61P37/06 ,  A61P43/00 ,  C07D213/89 ,  C07D401/12 ,  C07D405/12 ,  A61K31/4965 ,  A61K31/44 ,  A61K31/505

    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。

    .beta.-carbolin-3-carboxylic acid derivatives useful for treating anxiety and related disorders
    66.
    发明授权
    .beta.-carbolin-3-carboxylic acid derivatives useful for treating anxiety and related disorders 失效
    可用于治疗焦虑和相关疾病的β-咔啉-3-羧酸衍生物

    公开(公告)号：US5010077A

    公开(公告)日：1991-04-23

    申请号：US188145

    申请日：1988-04-25

    申请人： Claus T. Braestrup ,  Mogens C. Nielsen ,  Joergen A. Christensen ,  Mogens Engelstoft ,  Henning Schou ,  Ulrich Eder ,  Gunter Neef ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen

    发明人： Claus T. Braestrup ,  Mogens C. Nielsen ,  Joergen A. Christensen ,  Mogens Engelstoft ,  Henning Schou ,  Ulrich Eder ,  Gunter Neef ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen

    IPC分类号： C07D471/04 ,  C07H13/10

    CPC分类号： C07D471/04 ,  C07H13/10

    摘要： A .beta.-carbolin-3-carboxylic acid derivative of the formula ##STR1## wherein: X is oxygen, sulphur or NR.sup.10, wherein R.sup.10 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkenyl, C.sub.3-7 -cycloalkyl or C.sub.3-7 -cycloalkenyl;R.sup.3 is (a) C.sub.1-10 -alkoxy, C.sub.1-10 -alkenyloxy, C.sub.6-10 -aryloxy, C.sub.7-11 -aralkoxy or C.sub.8-12 -aralkenyloxy, each optionally substituted with one or more hydroxy groups, halogen atoms, CF.sub.3 groups, C.sub.1-10 -alkoxy groups or C.sub.2-4 -alkenyloxy groups or each optionally substituted with an amino, di-C.sub.1-6 -alkylamino, C.sub.1-10 -alkoxycarbonyl or C.sub.1-10 -alkenyloxycarbonyl group; or (b) NR.sup.11 R.sup.12, wherein R.sup.11 and R.sup.12 are the same or different and each is (i) hydrogen, (ii) hydroxy, (iii) C.sub.1-10 -alkyl, (iv) C.sub.2-10 -alkenyl, (v) C.sub.6-10 -aryl, (vi) C.sub.7-11 -aralkyl, (vii) C.sub.8-12 -aralkenyl, (viii) C.sub.3-7 -cycloalkyl, or (ix) C.sub.3-7 -cycloalkenyl, each of groups (iii)-(ix) optionally substituted with hydroxy, carboxamido, carboxy, C.sub.1-10 -alkoxycarbonyl or C.sub.1-10 -alkenyloxycarbonyl; or (x) amino optionally substituted with C.sub.1-10 -alkyl, C.sub.2-10 -alkenyl, C.sub.6-10 -aryl, C.sub.7-11 -aralkyl, C.sub.8-12 -aralkenyl, C.sub.3-7 -cycloalkyl or C.sub.3-7 -cycloalkenyl; or wherein R.sup.11 and R.sup.12 together with the connecting nitrogen atom form a 5-, 6- or 7-membered heterocyclic ring, which may also contain one additional N or one O atom, and which may be optionally substituted with the same groups of substituents listed for groups (iii)-(ix) above, with the proviso that R.sup.11 and R.sup.12 cannot both be hydroxy; or wherein X and R.sup.3 together represent a single nitrogen atom;R.sup.4 is hydrogen, C.sub.1-10 -alkyl, C.sub.2-10 -alkenyl, C.sub.3-7 -cycloalkyl, C.sub.3-7 -cycloalkenyl, C.sub.7-10 -aralkyl, C.sub.8-10 -aralkenyl, phenyl, C.sub.7-10 -alkoxyphenyl or C.sub.8-10 -alkenyloxyphenyl;R.sup.A is F, Cl, Br, I, NO.sub.2, NR.sup.13 R.sup.14, NHCOR.sup.13, CN, COOR.sup.13, OR.sup.13, SCH.sub.3 or SO.sub.2 NR.sup.11 R.sup.12, wherein R.sup.13 and R.sup.14 each is hydrogen or C.sub.1-6 -alkyl optionally substituted with hydroxy or halogen; and wherein R.sup.11 and R.sup.12 are as defined above, and wherein there may be 1-4 identical or different R.sup.A 's; andR.sup.9 is hydrogen, C.sub.1-8 -alkyl, C.sub.1-8 -alkenyl, C.sub.1-8 -alkoxycarbonyl, C.sub.1-8 -alkenyloxycarbonyl, or C.sub.1-8 -alkenyloxy;with the proviso that R.sup.11 and R.sup.12 are not both hydrogen, when X is oxygen and when R.sup.4, R.sup.A and R.sup.9 each is hydrogen; that one of R.sup.11 and R.sup.12 is not hydrogen when the other is amino and when X is oxygen and R.sup.4, R.sup.A and R.sup.9 each are hydrogen; and that R.sup.4, R.sup.A and R.sup.9 each is not hydrogen when X is oxygen and R.sup.3 is OCH.sub.3.have valuable pharmacological properties.

    1,2-disubstituted ergolines useful for producing central antidopanminergic or .alpha.2-receptor-blocking activity
    67.
    发明授权
    1,2-disubstituted ergolines useful for producing central antidopanminergic or .alpha.2-receptor-blocking activity 失效
    可用于产生中枢抗过敏能或α2受体阻断活性的1,2-二取代的麦角醇

    公开(公告)号：US4874768A

    公开(公告)日：1989-10-17

    申请号：US915358

    申请日：1986-10-06

    申请人： Andreas Huth ,  Gerhard Sauer ,  Helmut Wachtel

    发明人： Andreas Huth ,  Gerhard Sauer ,  Helmut Wachtel

    IPC分类号： A61K31/48 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D457/12

    CPC分类号： C07D457/12

    摘要： The disclosure relates to 1,2-substituted ergoline derivatives of general Formula I ##STR1## wherein X is an oxygen or sulfur atom,R.sup.1 is a lower alkyl group,R.sup.2 is halogen, acyl, a saturated or unsaturated lower alkyl group which can optionally be substituted by OR.sup.4 wherein R.sup.4 is hydrogen, lower alkyl, tetrahydropyranyl or cycloalkyl, or by an optionally substituted aryl residue, an S-R.sup.5 -group wherein R.sup.5 means a lower alkyl group which can optionally be substituted by aryl or an optionally substituted aryl residue, a ##STR2## wherein n=2 o4 3, or a --CHO-group, R.sup.3 is lower alkyl or acyl, andC.sub.9 -C.sub.10 is a CC-single or a CC-double bond, and the hydrogen atom in the 10-position is in the .alpha.-location if C.sub.9 -C.sub.10 is a CC-single bond, as well as the acid addition salts thereof. The compounds exhibit valuable pharmacological properties.

    摘要翻译： 本公开涉及通式I的I取代麦角灵衍生物（I）其中X是氧或硫原子，R 1是低级烷基，R 2是卤素，酰基，饱和或不饱和的低级烷基 其可以任选地被OR 4取代，其中R 4是氢，低级烷基，四氢吡喃基或环烷基，或被任选取代的芳基残基取代，其中R 5表示可任选地被芳基或任选地取代的芳基残基取代的低级烷基 取代的芳基残基，其中n = 2 o4 3，或-CHO-基团，R 3为低级烷基或酰基，C 9 -C 10为CC-单或CC-双键， 如果C9-C10是CC-单键，则10位是α位置，以及其酸加成盐。 该化合物显示出有价值的药理学性质。

    2-substituted ergoline urea and thio-urea derivatives having neurolyptic/dopaminergic activity
    68.
    发明授权
    2-substituted ergoline urea and thio-urea derivatives having neurolyptic/dopaminergic activity 失效
    2-取代麦角蛋白尿素和具有神经选择性/多巴胺能活性的硫脲衍生物

    公开(公告)号：US4826851A

    公开(公告)日：1989-05-02

    申请号：US915356

    申请日：1986-10-06

    申请人： Andreas Huth ,  Gerhard Sauer ,  Helmut Wachtel

    发明人： Andreas Huth ,  Gerhard Sauer ,  Helmut Wachtel

    IPC分类号： A61K31/48 ,  A61P25/18 ,  C07D457/12

    CPC分类号： C07D457/12

    摘要： Novel 2-substituted ergolinyl urea and thioruea derivatives are disclosed, as well as their use as pharmaceuticals, specifically as neuroleptics. The compounds, which possess central dopaminergic activity, have the formula ##STR1## wherein X is an oxygen or sulfur atom,R.sup.1 is a lower alkyl group,Y is a sulfur atom, S--CH.sub.2 --, C.sub.2 H.sub.4 --, --CH.dbd.CH--, or --C.tbd.C--,R.sup.2 is an aromatic ring of 5-6 atoms, 0-3 of which are O, S or N; or an aromatic ring of 5-6 atoms, 0-3 of which are O, S or N, and which is substituted by C.sub.1-2 -alkyl, C.sub.1-2 -alkoxy, nitrile, nitro, amino, C.sub.1-2 -alkylamino, carbonylamino or halo group, and C.sub.9 C.sub.10 is a CC-single or a CC-double bond and, if C.sub.9 C.sub.10 means a CC-single bond, the hydrogen atom in the 10-position is in the .alpha.-location,or a pharmaceutically acceptable acid addition salt thereof, wherein, if X is an oxygen atom, R.sup.1 is methyl and C.sub.9 C.sub.10 is a single bond, Y--R.sup.2 does not mean --C.sub.2 H.sub.4 -phenyl or --C.tbd.C--phenyl.

    摘要翻译： 公开了新型2-取代的麦角酰羟基尿素和硫醇衍生物，以及它们作为药物的用途，特别是作为精神安定药。 具有中枢多巴胺能活性的化合物具有式（I）其中X为氧或硫原子，R 1为低级烷基，Y为硫原子，S-CH 2 - ，C 2 H 4 - ， - CH = CH-或-C 3位C-，R 2为5-6个原子的芳环，其中0-3为O，S或N; 或5-6个原子的芳环，其中0-3是O，S或N，并被C1-2烷基，C1-2 - 烷氧基，腈，硝基，氨基，C1-2 - 烷基氨基 ，羰基氨基或卤代基，C9C10为CC-单或CC-双键，如果C9C10表示CC-单键，则10-位的氢原子位于α位，或其药学上可接受的酸 其中，如果X是氧原子，则R1是甲基，C9C10是单键，Y-R2不是指-C2H4-苯基或-C3ONC-苯基。

    Process for the production of .beta.-carbolines by dehydrogenation
    69.
    发明授权
    Process for the production of .beta.-carbolines by dehydrogenation 失效
    通过脱氢生产β-咔啉的方法

    公开(公告)号：US4644062A

    公开(公告)日：1987-02-17

    申请号：US825718

    申请日：1986-02-03

    申请人： Gregor Haffer ,  Helmut Borner ,  Andreas Huth

    发明人： Gregor Haffer ,  Helmut Borner ,  Andreas Huth

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： .beta.-carbolines of formula I ##STR1## wherein R=C.sub.1-5 alkylR.sup.4 =H, C.sub.1-5 alkyl or --(CH.sub.2).sub.n --OR with n=1 or 2 andR.sup.A =H, R, (CHR).sub.n --OR, OCH.sub.2 Ph, OPh, OPh(Cl,Br),OR,OCH.sub.2 Ph(Cl,Br) NRR, Cl or Br,wherein n and R have the above meanings and there are one or two R.sup.A 's are prepared, by dehydrogenation at reaction temperatures below ambient temperature in an inert solvent with tert-butyl hypochlorite and a tertiary amine.

    摘要翻译： 式I的β-咔啉其中R = C 1 -C 5烷基R 4 = H，C 1-5烷基或 - （CH 2）n -OR，其中n = 1或2，RA = H，R ）n-OR，OCH 2 Ph，OPh，OPh（Cl，Br），OR，OCH 2 Ph（Cl，Br）NRR，Cl或Br，其中n和R具有上述含义，并且通过脱氢制备一个或两个RA 在低于环境温度的反应温度下在惰性溶剂中与次氯酸叔丁酯和叔胺反应。