Alpha-amino-acid compounds
    2.
    发明授权
    Alpha-amino-acid compounds 失效
    α-氨基酸化合物

    公开(公告)号:US06706742B2

    公开(公告)日:2004-03-16

    申请号:US10146272

    申请日:2002-05-15

    IPC分类号: C07D27704

    摘要: Compound selected from those of formula (I): wherein: represents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single bond or phenylene, R1 and R2, which may be identical or different, each represent hydrogen or alkyl, R3 represents alkyl, nitro or cyano, Y represents NR4 or CHNO2, R4 represents hydrogen or alkyl, its tautomers when they exist, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, with the exclusion of compounds wherein, simultaneously, represents an unsubstituted 5-membered nitrogen-containing heterocycle, Ak represents —(CH2)3—, X represents a single bond, Y represents NH and R3 represents nitro. Medicinal products containing the same which are useful as dipeptidyl peptidase IV inhibitors.

    摘要翻译: 选自式(I)的化合物的化合物:其中:表示任选取代的5元含氮杂环,Ak表示亚烷基链,X表示单键或亚苯基,R 1和R 2可以相同或不同,各自相同或不同 代表氢或烷基,R3代表烷基,硝基或氰基,Y代表NR4或CHNO2,R4代表氢或烷基,其互变异构体存在时,其光学异构体及其与药学上可接受的酸的加成盐,排除化合物 其中,同时代表未取代的5元含氮杂环,Ak表示 - (CH2)3-,X表示单键,Y表示NH,R3表示硝基。含有该二价基团的肽酶IV 抑制剂。

    Alpha-amino acid sulphonyl compounds
    3.
    发明授权
    Alpha-amino acid sulphonyl compounds 失效
    α-氨基酸磺酰基化合物

    公开(公告)号:US06716843B2

    公开(公告)日:2004-04-06

    申请号:US10109407

    申请日:2002-03-28

    IPC分类号: A61K3140

    摘要: Compound of formula (I): wherein:  represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or phenylalanylprolyl, Ak represents an alkylene or heteroalkylene chain, X represents a single bond or optionally substituted phenylene, R2 represents optionally substituted alkyl, (C3-C10)cycloalkyl, or —NR2aR2b wherein R2a and R2b, which may be the same or different, each represent hydrogen or alkyl or, together with the nitrogen atom carrying them, form a nitrogen-containing heterocycle, Y represents R3 represents hydrogen or a group selected from alkyl, (C3-C7) cycloalkyl and aryl, R4, R5 and R6, which may be the same or different, each represent hydrogen or alkyl, or R4 and R6, or R5 and R6, together with the atoms carrying them, form an imidazolidine or dihydrobenzimidazole ring, its optical isomers and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as inhibitors of dipeptidyl-peptidase IV.

    摘要翻译: 式(I)化合物:其中:表示任选取代的5元含氮杂环,R 1表示氢,烷基,酰基,脯氨酰基,丙氨酰,组氨酰脯氨酰基或苯丙氨酰脯氨酰基,Ak表示亚烷基或杂亚烷基链,X表示 单键或任选取代的亚苯基,R 2表示任选取代的烷基,(C 3 -C 10)环烷基或-NR 2 a R 2b,其中可以相同或不同的R 2a和R 2b各自代表氢或烷基,或与携带它们的氮原子一起 ,形成含氮杂环,Y表示R 3表示氢或选自烷基,(C 3 -C 7)环烷基和芳基的基团,R 4,R 5和R 6可以相同或不同,各自表示氢或烷基,或R 4 和R6或R5和R6与携带它们的原子一起形成咪唑烷或二氢苯并咪唑环,其光学异构体及其与药学上可接受的酸的加成盐。含有相同的喔 ch可用作二肽基肽酶IV的抑制剂。

    Use of liver X receptor agonists
    5.
    发明授权
    Use of liver X receptor agonists 失效
    使用肝脏X受体激动剂

    公开(公告)号:US08030335B2

    公开(公告)日:2011-10-04

    申请号:US11920141

    申请日:2006-05-10

    IPC分类号: A61K31/44 A61K31/18

    摘要: The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.

    摘要翻译: 本发明一般涉及肝X受体(LXR)治疗的新型治疗用途。 更具体地说,本发明涉及LXR激动剂在制备可用于治疗和/或预防与β细胞变性相关的疾病(例如糖尿病)的药物中的用途,以及增加体内存活力的方法 胰岛细胞,包括使所述胰岛细胞与LXR激动剂接触。

    Cyclic &agr;-amino-&ggr;-hydroxyamide compounds
    7.
    发明授权
    Cyclic &agr;-amino-&ggr;-hydroxyamide compounds 失效
    环状α-氨基-γ-羟基酰胺化合物

    公开(公告)号:US06593312B2

    公开(公告)日:2003-07-15

    申请号:US10173993

    申请日:2002-06-18

    IPC分类号: A61K31425

    摘要: A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.

    摘要翻译: 式(I)的化合物:其中:表示任选取代的具有4至8个环成员的饱和碳环,可以相同或不同的R 1和R 4各自表示氢或酰基,R 2和R 3可以相同 或不同的,各自表示氢或烷基,R 5和R 6可以相同或不同,各自表示氢或烷基,或者R 5和R 6一起与带有氮原子一起形成任选取代的含氮杂环,其立体异构体 ,以及其与药学上可接受的酸的加成盐。含有该药物的药物可用于治疗葡萄糖不耐症或与高血糖相关的病症。