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131 条记录 (耗时 0.028 秒)

    2,5',N6-trisubstituted adenosine derivatives
    1.
    发明授权
    2,5',N6-trisubstituted adenosine derivatives 失效
    2,5'，N6-三取代腺苷衍生物

    公开(公告)号：US5589467A

    公开(公告)日：1996-12-31

    申请号：US306232

    申请日：1994-09-14

    申请人： Jesper Lau ,  Lars J. S. Knutsen

    发明人： Jesper Lau ,  Lars J. S. Knutsen

    IPC分类号： C07H19/167 ,  A61K31/00 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7076 ,  A61K31/708 ,  A61P25/00 ,  C07H19/16 ,  C07H19/67

    CPC分类号： C07H19/16

    摘要： A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein X is halogen, amino, perhalomethyl, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio or C.sub.1-6 -alkylamino;A is methyl, halomethyl, cyanomethyl, aminomethyl, vinyl, methylthiomethyl or methoxymethyl;R.sup.1 is selected from optionally substituted N-bonded heterocyclics.The compounds have been found useful for treating central nervous system ailments.

    摘要翻译： 式（I）化合物或其药学上可接受的盐：其中X为卤素，氨基，全卤甲基，氰基，C 1-6 - 烷氧基，C 1-6 - 烷硫基或C 1-6 - 烷基氨基; A是甲基，卤代甲基，氰基甲基，氨基甲基，乙烯基，甲硫基甲基或甲氧基甲基; R 1选自任选取代的N-键合杂环。 已经发现这些化合物可用于治疗中枢神经系统疾病。

    2-chloro-N.sup.6 -substituted adenosines, their pharmaceutical compositions, and activity in treating ischemias
    2.
    发明授权
    2-chloro-N.sup.6 -substituted adenosines, their pharmaceutical compositions, and activity in treating ischemias 失效
    2-氯-N6取代的腺苷，其药物组合物和治疗缺血的活性

    公开(公告)号：US5430027A

    公开(公告)日：1995-07-04

    申请号：US61892

    申请日：1993-05-14

    申请人： Lars J. S. Knutsen ,  Jesper Lau

    发明人： Lars J. S. Knutsen ,  Jesper Lau

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P9/00 ,  A61P25/00 ,  C07H19/16 ,  C07H19/167

    CPC分类号： C07H19/16

    摘要： Adenosine compounds having the following structure ##STR1## wherein X is halogen, perhalomethyl, acetamido, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio or C.sub.1-6 -alkylamino; andR.sup.1 is --NR.sup.2 R.sup.3 or YR.sup.4, wherein Y is oxygen or sulfur;R.sup.2 is phenyl, C.sub.1-6 -alkyl or substituted C.sub.1-6 -alkyl; andR.sup.4 is naphthyl, partly saturated naphthyl; optionally phenyl or phenoxy substituted C.sub.1-6 -alkyl wherein the phenyl and phenoxy substituents are also optionally substituted, or optionally phenyl or phenoxy substituted C.sub.3-8 -cycloalkyl and their pharmaceutically acceptable salts are useful in the treatment of myocardial and cerebral ischemias.

    摘要翻译： 具有以下结构的腺苷化合物，其中X为卤素，全卤代甲基，乙酰氨基，氰基，C 1-6 - 烷氧基，C 1-6 - 烷硫基或C 1-6 - 烷基氨基; 且R 1为-NR 2 R 3或YR 4，其中Y为氧或硫; R 2是苯基，C 1-6 - 烷基或取代的C 1-6 - 烷基; 并且R 4是萘基，部分饱和的萘基; 任选的苯基或苯氧基取代的C 1-6 - 烷基，其中苯基和苯氧基取代基也任选被取代，或任选地苯基或苯氧基取代的C 3-8 - 环烷基及其药学上可接受的盐可用于治疗心肌和脑缺血。

    C2,N.sup.6 -disubstituted adenosine derivatives
    3.
    发明授权
    C2,N.sup.6 -disubstituted adenosine derivatives 失效
    C2，N6-二取代腺苷衍生物

    公开(公告)号：US5432164A

    公开(公告)日：1995-07-11

    申请号：US963878

    申请日：1992-10-20

    申请人： Lars J. S. Knutsen ,  Jesper Lau

    发明人： Lars J. S. Knutsen ,  Jesper Lau

    IPC分类号： C07H19/167 ,  A61K20060101 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P25/00 ,  C07D20060101 ,  C07H20060101 ,  C07H19/16

    CPC分类号： C07H19/16

    摘要： A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein X is halogen, perhalomethyl, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, or C.sub.1-6 -alkylamino; andR.sup.1 is selected from N-bonded heterocycles.The compound with the greatest ability to discriminate between the A1 and A2 adenosine receptors is 2-chloro-N-[4-phenoxy-1-piperidinyl]adenosine. These adenosine derivatives are useful as anti-convulsants.

    摘要翻译： 式（I）化合物或其药学上可接受的盐：其中X为卤素，全卤甲基，氰基，C 1-6 - 烷氧基，C 1-6 - 烷硫基或C 1-6 - 烷基氨基; 并且R 1选自N-键合杂环。 具有区分A1和A2腺苷受体的最大能力的化合物是2-氯-N- [4-苯氧基-1-哌啶基]腺苷。 这些腺苷衍生物可用作抗惊厥药。

    DOUBLE-ACYLATED GLP-1 DERIVATIVES WITH A LINKER
    9.
    发明申请
    DOUBLE-ACYLATED GLP-1 DERIVATIVES WITH A LINKER 有权
    具有连接子的双取代的GLP-1衍生物

    公开(公告)号：US20130338068A1

    公开(公告)日：2013-12-19

    申请号：US13883946

    申请日：2011-11-09

    申请人： Jacob Kofoed ,  Jesper Lau ,  Lars Linderoth ,  Patrick William Garibay ,  Thomas Kruse

    发明人： Jacob Kofoed ,  Jesper Lau ,  Lars Linderoth ,  Patrick William Garibay ,  Thomas Kruse

    IPC分类号： C07K14/605

    CPC分类号： C07K14/605 ,  A61K47/542

    摘要： The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from HOOC—(CH2)x—CO-*, and  Chem. 1: HOOC—C6H4-0-(CH2)y—CO-*,  Chem. 2: in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises *-NH—(CH2)q—CH[(CH2)w—NH2]—CO-*,  Chem. 3: wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are potent, protracted, and suitable for oral administration.

    摘要翻译： 本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第18位的位置处的第一个K残基，另一个的第二个K残基 位置和与GLP-1（7-37）相比最多12个氨基酸变化; 该衍生物分别包含通过接头分别连接到所述第一和第二K残基的两个伸长部分，其中伸长部分选自HOOC-（CH 2）x -CO- *和Chem。 1：HOOC-C6H4-0-（CH2）y-CO- *，Chem。 2：其中x是6-18的整数，y是3-17的整数; 并且连接体包含* -NH-（CH 2）q-CH [（CH 2）w -NH 2] -CO - *， 3：其中q是0-5的整数，w是0-5的整数; 或其药学上可接受的盐，酰胺或酯。 本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型肽和侧链中间体。 衍生物有效，延长，适合口服。