Peptide compounds containing a cyclic amide structure
    4.
    发明授权
    Peptide compounds containing a cyclic amide structure 失效
    含有环状结构的肽类化合物

    公开(公告)号:US5190923A

    公开(公告)日:1993-03-02

    申请号:US710283

    申请日:1991-06-04

    摘要: The invention relates to compounds of formula (I): ##STR1## in which: A represents, with the carbon and nitrogen atoms to which it is linked, cyclic amide as defined in the description,B represents, with the nitrogen and carbon atoms to which it is linked, saturated polycyclic structure as defined in the description,R represents hydrogen, optionally substituted lower alkyl, optionally substituted (4-imidazolyl)methyl, (3-pyrazolyl)methyl or optionally substituted (2-pyridyl)methyl,their enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid.Medicinal products.

    摘要翻译: 本发明涉及式(I)化合物:其中:A表示与其连接的碳原子和氮原子,描述中定义的环酰胺,B表示与氮和 与其连接的碳原子,如描述中所定义的饱和多环结构,R表示氢,任选取代的低级烷基,任选取代的(4-咪唑基)甲基,(3-吡唑基)甲基或任选取代的(2-吡啶基)甲基 ,它们的对映异构体,非对映异构体和差向异构体以及它们与药学上可接受的酸的加成盐。 药用产品。

    Substituted amino acid compounds
    6.
    发明授权
    Substituted amino acid compounds 失效
    取代的氨基酸化合物

    公开(公告)号:US5151432A

    公开(公告)日:1992-09-29

    申请号:US629823

    申请日:1990-12-19

    CPC分类号: C07K5/0222 A61K38/00

    摘要: The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 represents a linear or branched, lower or higher alkoxy group or a substituted or unsubstituted amino group,R.sub.2 represents a lower alkyl group unsubstituted or substituted with an amino group,R.sub.3 represents an amino, lower or higher alkoxy or a hydroxyl group, with the proviso, however, that at least one amino group is present in R.sub.1 or R.sub.3,R.sub.4 represents a hydrogen atom or an aryl group,m is equal to 1 or 2,n is between 1 and 6, andRa and Rb, which may be identical or different, represent a hydrogen atom when m=1, or a hydrogen atom or an alkyl group when m=2 andmedicinal products.

    摘要翻译: 本发明涉及式(I)的化合物:其中:R1表示直链或支链,低级或高级烷氧基或取代或未取代的氨基,R2表示未取代或取代的低级烷基 氨基,R3表示氨基,低级或高级烷氧基或羟基,但条件是R1或R3中至少有一个氨基,R4表示氢原子或芳基,m为 等于1或2,n为1至6,当m = 1时,Ra和Rb可相同或不同,表示氢原子,当m = 2时为氢原子或烷基,药物。

    Piperidine compounds
    7.
    发明授权
    Piperidine compounds 失效
    哌啶化合物

    公开(公告)号:US5652246A

    公开(公告)日:1997-07-29

    申请号:US546263

    申请日:1995-10-20

    CPC分类号: C07D401/06 C07D471/04

    摘要: The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 represents alkyl, phenyl, naphthyl, pyridyl or thienyl group, each phenyl, naphthyl, pyridyl or thienyl optionally being substituted,R.sub.2 represents a hydrogen atom or a substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, cycloalkyl, piperidino or substituted or unsubstituted amino group,X represents CO or SO.sub.2,R.sub.3 represents hydrogen or alkyl,R.sub.4 represents alkyl, substituted or unsubstituted phenyl or trihalomethyl, or else R.sub.3 and R.sub.4 form, together with the carbon atoms which carry them, cyclo(C.sub.3 -C.sub.7)alkenyl,A represents phenyl, naphthyl or pyridyl ring, each phenyl, naphthyl or pyridyl ring optionally being substituted,their isomers, the corresponding quaternary ammonium salts of the piperidine and their addition salts with a pharmaceutically acceptable acid, an medicinal products containing the same are useful as antagonists of NK.sub.1 receptors.

    摘要翻译: 本发明涉及式(I)化合物:其中:R 1表示烷基,苯基,萘基,吡啶基或噻吩基,每个苯基,萘基,吡啶基或噻吩基任选被取代,R 2表示氢 原子或取代或未取代的烷基,取代或未取代的苯基,环烷基,哌啶子基或取代或未取代的氨基,X表示CO或SO 2,R 3表示氢或烷基,R 4表示烷基,取代或未取代的苯基或三卤甲基, R 4与携带它们的碳原子一起形成环(C 3 -C 7)链烯基,A代表苯基,萘基或吡啶环,每个苯基,萘基或吡啶基任选被取代,它们的异构体是相应的季铵盐 哌啶及其与药学上可接受的酸的加成盐,含有它们的药物可用作NK1受体的拮抗剂。

    Tripeptide compounds having a nitrogenous polycyclic structure
    9.
    发明授权
    Tripeptide compounds having a nitrogenous polycyclic structure 失效
    具有含氮多环结构的三肽化合物

    公开(公告)号:US5047400A

    公开(公告)日:1991-09-10

    申请号:US207710

    申请日:1988-06-16

    CPC分类号: C07K5/0815

    摘要: The invention relates to the compounds of general formula: ##STR1## in which: X denotes either an oxygen atom, or two hydrogen atoms;Y denotes either a hydrogen atom, or a hydroxyl group;or Y denotes an amino group on condition that X denotes two hydrogen atoms;R denotes a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms, optionally substituted with one or more hydroxy, amino, mercapto, methylthio or carboxy groups, or aryl groups such as phenyl, pyridyl or thienyl; ##STR2## denotes a polycyclic nitrogenous structure; their enantiomers, epimers and diastereoisomers, as well as their addition salts with a pharmaceutically acceptable acid or base.

    摘要翻译: 本发明涉及以下通式的化合物:其中:X表示氧原子或两个氢原子; Y表示氢原子或羟基; 或者Y表示氨基,条件是X表示两个氢原子; R表示氢原子或具有1至6个碳原子的直链或支链烷基,任选被一个或多个羟基,氨基,巯基,甲硫基或羧基取代,或芳基如苯基,吡啶基或噻吩基 ; “IMAGE”表示多环含氮结构; 它们的对映体,差向异构体和非对映异构体,以及它们与药学上可接受的酸或碱的加成盐。

    Alpha-amino-acid compounds
    10.
    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。