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    CYANOANTHRANYLAMID-DERIVATE UND DEREN VERWENDUNG ALS ARZNEIMITTEL
    21.
    发明公开
    CYANOANTHRANYLAMID-DERIVATE UND DEREN VERWENDUNG ALS ARZNEIMITTEL 有权
    CYANOANTHRANYLAMID衍生物及其药物AS

    公开(公告)号：EP1387838A1

    公开(公告)日：2004-02-11

    申请号：EP02748691.9

    申请日：2002-05-03

    申请人： SCHERING AKTIENGESELLSCHAFT

    发明人： ERNST, Alexander ,  HUTH, Andreas ,  KRÜGER, Martin ,  THIERAUCH, Karl-Heinz ,  MENRAD, Andreas ,  HABEREY, Martin

    IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  A61K31/44 ,  A61P19/02 ,  A61P33/00

    CPC分类号： C04B35/632 ,  C07D401/12

    摘要： The invention relates to substituted cyanoanthranilamide derivatives, to the production and use thereof as medicaments for the treatment of diseases triggered by persistent angiogenesis. The inventive compounds can be used, for instance in psoriasis, Kaposis sarcoma, restenosis, e.g. stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia, arthritis, e.g. rheumatoid arthritis, hemangioma, angiofribroma, eye diseases, e.g. diabetic retinopathy, neovascular glaucoma, kidney diseases, e.g. glomerulonephritis, diabetic nephropathy, malign nephrosclerosis, thrombotic microangiopatic syndrome, transplantation rejections and glomerulopathy, fibrotic diseases such as liver cirrhosis, mesangial cell proliferative diseases, arteriosclerosis, injuries of nerve tissue and inhibition of reocclusion of blood vessels after balloon catheter treatment, in vascular prosthetics or after implantation of mechanical devices for keeping blood vessels open, e.g. stents, as immunosuppressants, as aid in scarless wound healing, age spots and contact dermatitis. The inventive compounds can also be used as VEGFR-3 inhibitors in lymphangiogenesis. The invention further relates to compounds of general formula (I), wherein A represents group -N(R7)-; Y1 to Y5 represent a nitrogen atom or group -CY6; Y6 represents cyano, halogen, C¿1?-C6-alkyl, C1-C6-alkoxy, amino or hydroxy, wherein at least one nitrogen atom is contained in the ring and at least one cyano radical is contained in the ring.

    20-ALKYL-7-OXOPROSTACYCLINDERIVATE UND VERFAHREN ZU IHRER HERSTELLUNG
    23.
    发明授权
    20-ALKYL-7-OXOPROSTACYCLINDERIVATE UND VERFAHREN ZU IHRER HERSTELLUNG 失效
    20-烷基-7-氧代环糊精衍生物及其生产方法

    公开(公告)号：EP0163672B1

    公开(公告)日：1991-05-15

    申请号：EP84904100.9

    申请日：1984-11-08

    申请人： SCHERING AKTIENGESELLSCHAFT

    发明人： NICKOLSON, Robert ,  VORBRÜGGEN, Helmut ,  STÜRZEBECHER, Claus - Steffen ,  HABEREY, Martin

    IPC分类号： C07D307/935 ,  A61K31/557

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07D307/937

    摘要： 20-alkyl-7-oxoprostacycline derivatives having the general formula (I) wherein R1 is either the rest OR3, R3 representing hydrogen or alkyl comprising from 1 to 10 atoms of carbon optionally substituted by halogen, phenyl, alkoxy having from 1 to 4 atoms of carbon or dialkylamino having from 1 to 4 atoms of carbon, cycloalkyl, aryl or a heterocyclic rest, or the rest NHR4, R4 representing hydrogen or an alkanoyl or alkansulphonyl rest having from 1 to 10 atoms of carbon; n is 1 or 2; A is a group-CH2-CH2-, cis -CH=CH- or trans -CH=CH-; W is a groupe (II) or (III) wherein the group OH may be esterified with benzoyl or alkane acid rest having from 1 to 4 atoms of carbon or etherified with a tetrahydropyranol-, tetrahydrofuranyl-, alkoxyalkyl-, or trialkylsilyle rest, the free or esterified OH group being in the alpha or beta position; R2 is a straight or branched chain alkyl comprising from 1 to 6 atoms of carbon; R5 is a hydroxy group esterified with an alkane acid rest having from 1 to 4 atoms of carbon or etherified with tetrahydropyranyl-, tetrahydrofuranyl-, alkoxy alkyl- or trialkylsilyle rest; R6 and R7 are hydrogen or a straight or branched chain alkyl having from 1 to 4 atoms of carbon or R6 and R7 form together a trimethylene radical, R8 and R9 form together a bound, hydrogen or a straight or branched chain alkyl having from 1 to 4 atoms of carbon and if R3 is hydrogen, the salts thereof with physiologically compatible bases; production thereof and utilization thereof as medicine.

    NEUE PROSTACYCLINE UND VERFAHREN ZU IHRER HERSTELLUNG
    24.
    发明授权
    NEUE PROSTACYCLINE UND VERFAHREN ZU IHRER HERSTELLUNG 失效
    新的预聚物及其制备方法

    公开(公告)号：EP0094951B1

    公开(公告)日：1985-10-30

    申请号：EP82903452.9

    申请日：1982-11-25

    申请人： SCHERING AKTIENGESELLSCHAFT

    发明人： NICKOLSON, Robert ,  VORBRUGGEN, Helmut ,  CASALS-STENZEL, Jorge ,  HABEREY, Martin

    IPC分类号： C07D307/935 ,  C07D407/12 ,  C07F7/18 ,  A61K31/34 ,  A61K31/557

    CPC分类号： C07D307/935 ,  C07C51/09 ,  C07C51/38 ,  C07C55/32 ,  C07C57/52 ,  C07C405/00 ,  C07C405/0033 ,  C07D307/937 ,  C07D407/12 ,  C07F7/1856 ,  C07F9/4015

    摘要： Prostacyclin derivatives having the general formula I wherein R1 is either the OR3 rest, wherein R3 may be hydrogen or an alkyl group with 1 to 10 atoms of carbon and optionally substituted by halogen, aryl, C1-C4-alkoxy or C1-C4-dialkyl-amino, a cyclo-alkyl group, an aryl group or an heterocyclic group, or the rest NHR4, wherein R4 may be hydrogen, an alkanoyl or alkane-sulfonyl group with 1 to 10 atoms of carbon, A represents either -CH2-CH2- , or -CH=CH- (trans), W represents either wherein the group OH is either esterified with a benzoyl rest or an alkanoyl rest having 1 to 4 atoms of carbon, or is etherified with a tetra-hydro-pyranyl, tetra-hydro-furanyl, alkoxy-alkyl (1 to 4 atoms of carbon) or tri-(C1 to C4-alkyl)-silyl rest, the free or esterified OH group being in the position alpha or beta ; the symbols D and E representing in common a direct bond or the symbol D representing itself an alkyl group in a straight or branched chain with 1 to 5 atoms of carbon and the symbol E representing an oxygen atom or a direct bond, the symbol R2 represents an alkyl group with a straight or branched chain having 1 to 6 atoms of carbon, an alkenyl group with a straight or branched chain having 2 to 6 atoms of carbon, group which may be substituted by phenyl, halogen or alkyl with 1 to 4 atoms of carbon or then, when the symbols D and E designate a direct bond, an alkinyl group with 2 to 6 atoms of carbon, optionally substituted in position 1 by halogen or alkyl with 1 to 4 atoms of carbon, the symbol R5 represents a hydroxy group which may be either esterified by an alkanoyl rest having 1 to 4 atoms of carbon, or etherified by a tetra-hydro-pyranyl, tetra-hydro-furanyl, alkoxy-alkyl or tri-alkyl-silyl rest and, providing that R3 is hydrogen, the salts of such derivatives with physiologically acceptable bases. Said compounds are characterized by a hypotensive activity and an inhibiting activity of thrombocyte aggregation. The invention also relates to preparation processes of such compounds.