Cyclic &agr;-amino-&ggr;-hydroxyamide compounds
    1.
    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。

    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。

    Aminotriazole compounds
    5.
    发明授权
    Aminotriazole compounds 失效
    氨基三唑化合物

    公开(公告)号:US06596749B2

    公开(公告)日:2003-07-22

    申请号:US09799199

    申请日:2001-03-05

    IPC分类号: A61K314196

    摘要: Method of treating with compounds of formula (I): wherein: n is 0 or 1, W represents —CO— or S(O)q and q is 0, 1 or 2, G represents a G1, G2, G3 or G4 group as defined in the description, Z represents alkyl, aryl, heteroaryl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylakenyl, heteroarylalkynyl or heteroarylalkyl each optionally substituted, A represents a grouping selected from —A2—, —A1—A2—, —A2—A1—, and —A1—A2—A1— wherein A1 is alkylene and A2 represents phenylene, cycloalkylene, naphthylene or heteroarylene each optionally substituted, R represents hydrogen, alkyl, aryl, heteroaryl, arylalkyl arylalkenyl, arylalkynyl, heteroarylakenyl, heteroarylalkynyl or heteroarylalkyl each optionally substituted, R1 represents alkyl, aryl, heteroaryl, arylalkyl arylalkenyl, arylalkynyl, heteroarylakenyl, heteroarylalkynyl or heteroarylalkyl each optionally substituted, and medicinal products containing the same are useful as Neuropeptide Y receptor ligands.

    摘要翻译: 用式(I)化合物处理的方法:其中:n为0或1,W为-CO-或S(O)q,q为0,1或2,G为G1,G2,G3或G4基团 Z表示烷基,芳基,杂芳基,芳基烷基,芳基烯基,芳基炔基,杂芳基酰基,杂芳基炔基或杂芳基烷基,各自任选取代,A表示选自-A2-,-A1-A2-,-A2-A1- 和-A1-A2-A1-,其中A1是亚烷基,A2代表亚苯基,亚环烷基,亚萘基或亚杂芳基,各自任选取代,R表示氢,烷基,芳基,杂芳基,芳基烷基芳基烯基,芳基炔基,杂芳基酰基,杂芳基炔基或杂芳基烷基, R 1表示烷基,芳基,杂芳基,芳基烷基芳基烯基,芳基炔基,杂芳基酰基,杂芳基炔基或杂芳基烷基,各自任选被取代,并且含有它们的医药产品可用作神经肽Y受体配体。

    Methods of identifying or screening for agents that binds the Ob-Re
    10.
    发明授权
    Methods of identifying or screening for agents that binds the Ob-Re 失效
    鉴定或筛选结合Ob-Re的药剂的方法

    公开(公告)号:US06770444B2

    公开(公告)日:2004-08-03

    申请号:US09116676

    申请日:1998-07-16

    IPC分类号: G01N3353

    摘要: This invention provides an isolated nucleic acid encoding a polypeptide, a purified polypeptide, vectors comprising isolated nucleic acid encoding a polypeptide, cells comprising such vectors, antibodies directed to a polypeptide, nucleic acid probes useful for detecting nucleic acid encoding a polypeptide, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a polypeptide, nonhuman transgenic animals which express DNA encoding a normal or a mutant polypeptide, methods of isolating a polypeptide, methods of treatment eating disorders as well as methods of determining binding of compounds to polypeptides.

    摘要翻译: 本发明提供了编码多肽的分离的核酸,纯化的多肽,包含分离的编码多肽的核酸,包含此类载体的细胞,针对多肽的抗体,可用于检测编码多肽的核酸的核酸探针,反义寡核苷酸互补 编码多肽的独特的核酸序列,表达编码正常或突变多肽的DNA的非人类转基因动物,分离多肽的方法,进食障碍的治疗方法以及确定化合物与多肽结合的方法。