PROCESS FOR PREPARING CYCLIC ESTERS AND CYCLIC AMIDES
    4.
    发明授权
    PROCESS FOR PREPARING CYCLIC ESTERS AND CYCLIC AMIDES 有权
    用于生产环酯和环酰胺

    公开(公告)号:EP2941422B1

    公开(公告)日:2017-04-05

    申请号:EP14703824.4

    申请日:2014-02-07

    摘要: A process for preparing a cyclic ester or a cyclic amide includes contacting hydroxycarboxylic acid and/or amino-carboxylic acid, an ester thereof, or a salt thereof, with acidic zeolite. The hydroxycarboxylic acid is a 2- or 6-hydroxycarboxylic acid, and the amino carboxylic acid is a 2- or 6-amino-carboxylic acid. The zeolite may include two or three interconnected and non-parallel channel systems, in which a channel system includes 10- or more-membered ring channels, and in which a framework Si/X2 ratio is at least 24 as measured by NMR. X is Al or B. The zeolite may include three interconnected and non-parallel channel systems, in which at least two channel systems include 10- or more-membered ring channels, and in which a framework Si/X2 ratio is at least 6 as measured by NMR. The process may be performed at a pressure between 0.5 and 20 bar.

    METHOD FOR INHIBITION OF DEUBIQUITINATING ACTIVITY
    6.
    发明公开
    METHOD FOR INHIBITION OF DEUBIQUITINATING ACTIVITY 有权
    VERFAHREN ZUR HEMMUNG VON DEUBIQUITINIERENDERAKTIVITÄT

    公开(公告)号:EP2780326A4

    公开(公告)日:2015-04-22

    申请号:EP12841677

    申请日:2012-10-15

    申请人: VIVOLUX AB

    摘要: Compounds of the general structure S-1, wherein X and R1-R5 are defined in the specification, are capable of abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs and are useful in methods and compositions for treating cancer, in particular, cancer tumors refractory to treatment by state-of-the-art chemotherapy.

    摘要翻译: 通常结构S-1的化合物,其中X和R 1 -R 5在说明书中定义,能够消除19S RP DUB的去泛素化(DUB)活性,并且可用于治疗癌症的方法和组合物, 通过最先进的化学疗法治疗难治的癌症肿瘤。

    Neue 3-Amino/Hydroxy-4-[4-Benzoyl-Phenyl Carbonylamino/oxy]-Azepane und Homologe als Protein Kinase Hemmer
    8.
    发明公开
    Neue 3-Amino/Hydroxy-4-[4-Benzoyl-Phenyl Carbonylamino/oxy]-Azepane und Homologe als Protein Kinase Hemmer 失效
    Neue 3-氨基/羟基-4- [4-苯甲酰基 - 苯基羰基氨基/氧基] -Azepane和Homologe als蛋白激酶血液。

    公开(公告)号:EP0663393A1

    公开(公告)日:1995-07-19

    申请号:EP94120924.9

    申请日:1994-12-30

    摘要: Die Verbindungen der Formel I,

       worin R¹-R⁹, R¹⁵, A, X, Y, Z und an die in der Beschreibung angegebene Bedeutung haben, sind wirksam als Protein kinase-Hemme und können als Heilmittel, insbesondere zur Behandlung entzündlicher Hauterkrankungen, und von Alopezie verwendet werden.

    摘要翻译: 式(I)的苄氧基 - ,苯甲酰氧基 - 和苯甲酰基氨基 - 氮杂环庚烷及其盐是新的:A = substd。 2-,3-或4-吡啶基或2-或3-哌嗪基; X,Y = O或NH,但不是NH; Z = O,或当X = O,O或(H,H)时; n = 1-3; R 1 = H或F; R 2 = H; 低级烷氧基 或F; R 3 = H; 哦; 低级烷氧基 F; CF 3,低级烷氧基羰基; 或选择。 substd。 四唑基; R 4 = H; OH,低级烷氧基; 低级烷基 氯; F; CF3; COCH3; 二(低级烷基)氨基; 低级烷氧基 - 低级烷基; 等等。; R 5 = H,低级烷氧基,F或CF 3; 或R 3 + R 4 = -CH = CH-CH = CH-或亚乙二氧基; 或R 4 + R 5 = -CH = CH-CH = CH-; - (CH2)4-; 亚甲二氧基; 亚; -N = CH-CH = CH-; 等等。; R6 = H,OH; 低级烷氧基 F; 2,4-二氟 - Ph值; 低级烷氧基 - 低级烷基; 等等。; R 7 = H; OH,低级烷氧基; COOH; NH2或F; 或R 6 + R 7 = -N = CH-CH = N-或-N(Me)CH 2 CH 2 N(Me) - ; R 8 = H; 低级烷氧基 低级烷基或F; R 9 = H或F; R 10 = H; 哦; 低级烷氧基 或低级烷基; R 11 = H; 低级烷氧基 低级烷基 F; 或Br; R 12 = H; 哦; 低级烷氧基 COOH; 低级烷氧基羰基; 或NH2; R 13 = H; 哦; 低级烷氧基 低级烷基 COCH3; 或F; 或R 12 + R 13 = -CH = CH-CH = CH-; 或-C(OH)= CH-CH = CH-。 与R 12结合; R 14 = H; 低级烷基 或F; R 15 = H或脒基。 还要求保护的是中间体(II)。