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12 条记录 (耗时 0.028 秒)

    Imino compounds
    5.
    发明授权
    Imino compounds 失效

    公开(公告)号：US4251542A

    公开(公告)日：1981-02-17

    申请号：US944220

    申请日：1978-09-20

    申请人： Atso Ilvespaa ,  Walter Fuhrer

    发明人： Atso Ilvespaa ,  Walter Fuhrer

    IPC分类号： C07D207/18 ,  A61K31/40 ,  A61K31/415 ,  A61K31/445 ,  A61K31/451 ,  A61P3/08 ,  C07D207/20 ,  C07D207/24 ,  C07D211/70 ,  C07D223/04 ,  C07D223/06 ,  C07D233/22 ,  C07D233/24 ,  C07D207/08 ,  C07D207/12

    CPC分类号： C07D233/22 ,  C07D207/20 ,  C07D207/24 ,  C07D211/70 ,  C07D223/04 ,  C07D223/06 ,  C07D233/24 ,  Y10S514/884

    摘要： The present invention provides new imino compounds having the formula I ##STR1## wherein R.sub.1 represents an aliphatic or cycloaliphatic hydrocarbon radical, unsubstituted or substituted phenyl, or phenyl-lower alkyl or diphenyl-lower alkyl, which radicals are unsubstituted or substituted in the phenyl ring(s),R.sub.2 represents unsubstituted or substituted phenyl, unsubstituted or substituted monocyclic heteroaryl or lower alkyl,R.sub.3 represents hydrogen, lower alkyl, a carbonyl group linked with R.sub.2 to form a five-membered ring, or the group R.sub.6 --CO wherein R.sub.6 represents lower alkyl or unsubstituted or substituted phenyl,R.sub.4 represents, if present, hydrogen or lower alkyl which is independent or is linked with R.sub.1 to form a five- to seven-membered ring which can contain as ring members two aromatic ring carbon atoms of an unsubstituted or substituted phenyl or phenyl-lower-alkyl radical R.sub.1, and as a six- or seven-membered ring also epoxy or lower alkylimino which is separated by two, or at least two, carbon atoms from the nitrogen atom given in the formula I,R.sub.5 represents, if present, hydrogen or lower alkyl,A represents a straight- or branched-chain lower alkylene having 2 to (5-n.sub.1 -n.sub.2) chain members,Z represents epoxy, epithio, imino or lower alkylimino, andm.sub.1 and m.sub.2 represent 0 or 1 and together always represent 1,n.sub.1 represents 1 or, if Z represents imino or lower alkylimino and n.sub.2 represents 1, can also represent 0,n.sub.2 represents 0 or 1,and wherein two additional bonds, either corresponding to the dashed lines or corresponding to the dotted lines, are present, with m.sub.1 representing 0 in the former case and m.sub.2 representing 0 in the latter case, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, particularly hypoglycaemic activity, and can be used as oral antidiabetics. Specific embodiments are 2-[2-(cyclohexylimino)-2-phenyl-ethylidene]-pyrrolidine and 2-[2-(cis-2-cyclohexyl-cyclopentylimino)-2-phenylethylidene]-pyrrolidine, and their pharmaceutically acceptable acid addition salts.

    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups
    7.
    发明授权
    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
    由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物

    公开(公告)号：US4758584A

    公开(公告)日：1988-07-19

    申请号：US011183

    申请日：1987-02-05

    申请人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

    发明人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

    IPC分类号： C07D233/54 ,  C07D401/12 ,  C07D417/12 ,  C07K5/02 ,  A61K37/64 ,  C07K5/08

    CPC分类号： C07D233/64 ,  C07D401/12 ,  C07D417/12 ,  C07K5/0227 ,  Y10S530/86

    摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

    摘要翻译： 式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合 基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，亚磺酰基或磺酰基，R 6代表取代的氨基， 具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

    Substituted tetrapeptides
    8.
    发明授权
    Substituted tetrapeptides 失效
    取代四肽

    公开(公告)号：US4595677A

    公开(公告)日：1986-06-17

    申请号：US554735

    申请日：1983-11-23

    申请人： Bernhard Riniker ,  Peter Buhlmayer ,  Walter Fuhrer

    发明人： Bernhard Riniker ,  Peter Buhlmayer ,  Walter Fuhrer

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K7/02 ,  C07K7/14 ,  A61K37/02

    CPC分类号： C07K5/0227 ,  C07K7/02 ,  C07K7/14 ,  A61K38/00 ,  Y10S530/86

    摘要： Tetrapeptides of the formula I, ##STR1## in which R.sup.1 represents hydrogen or acyl, R.sup.2 represents alkyl or aralkyl, R.sup.3 represents free or functionally modified hydroxy, R.sup.4 represents free or substituted amino or free or etherified hydroxy, and -Pro-, -Phe- and -His- respectively represent the bivalent radicals of the amino acids proline, phenylalanine and histidine or the (D)-isomers thereof, salts of such compounds having salt-forming groups, and processes for their manufacture.The compounds inhibit the action of the enzyme renin and can be used as antihypertensives and for the treatment of cardiac insufficiency.

    摘要翻译： 式I的四肽，其中R 1表示氢或酰基，R 2表示烷基或芳烷基，R 3表示游离或官能改性的羟基，R 4表示游离或取代的氨基或游离的或醚化的羟基，和-Pro- ，-Phe-和-His-分别表示氨基酸脯氨酸，苯丙氨酸和组氨酸或其（D）异构体的二价基团，这些具有成盐基团的化合物的盐及其制备方法。 该化合物抑制酶肾素的作用，可用作抗高血压药物和治疗心功能不全。

    2-(Iminoethylidene)-pyrrolidines and tautomeric 2-(aminoethenyl)-1-pyrrolines
    9.
    发明授权
    2-(Iminoethylidene)-pyrrolidines and tautomeric 2-(aminoethenyl)-1-pyrrolines 失效
    2-（亚氨基亚乙基） - 吡咯烷和互变异构的2-（氨基乙烯基）-1-吡咯啉

    公开(公告)号：US4130652A

    公开(公告)日：1978-12-19

    申请号：US771294

    申请日：1977-02-23

    申请人： Atso Ilvespaa ,  Walter Fuhrer

    发明人： Atso Ilvespaa ,  Walter Fuhrer

    IPC分类号： C07D207/18 ,  A61K31/40 ,  A61K31/415 ,  A61K31/445 ,  A61K31/451 ,  A61P3/08 ,  C07D207/20 ,  C07D207/24 ,  C07D211/70 ,  C07D223/04 ,  C07D223/06 ,  C07D233/22 ,  C07D233/24 ,  C09B23/00

    CPC分类号： C07D233/22 ,  C07D207/20 ,  C07D207/24 ,  C07D211/70 ,  C07D223/04 ,  C07D223/06 ,  C07D233/24 ,  Y10S514/884

    摘要： The present invention provides new imino compounds having the formula I ##STR1## wherein R.sub.1 represents an aliphatic or cycloaliphatic hydrocarbon radical, unsubstituted or substituted phenyl, or phenyl-lower alkyl or diphenyl-lower alkyl, which radicals are unsubstituted or substituted in the phenyl ring(s),R.sub.2 represents unsubstituted or substituted phenyl, unsubstituted or substituted monocyclic heteroaryl or lower alkyl,R.sub.3 represents hydrogen, lower alkyl, a carbonyl group linked with R.sub.2 to form a five-membered ring, or the group R.sub.6 --CO wherein R.sub.6 represents lower alkyl or unsubstituted or substituted phenyl,R.sub.4 represents, if present, hydrogen or lower alkyl which is independent or is linked with R.sub.1 to form a five- to seven-membered ring which can contain as ring members two aromatic ring carbon atoms of an unsubstituted or substituted phenyl or phenyl-lower-alkyl radical R.sub.1, and as a six- or seven-membered ring also epoxy or lower alkylimino which is separated by two, or at least two, carbon atoms from the nitrogen atom given in the formula I,R.sub.5 represents, if present, hydrogen or lower alkyl,A represents a straight- or branched-chain lower alkylene having 2 to (5-n.sub.1 -n.sub.2) chain members,Z represents epoxy, epithio, imino or lower alkylimino, andM.sub.1 and m.sub.2 represent 0 or 1 and together always represent 1,N.sub.1 represents 1 or, if Z represents imino or lower alkylimino and n.sub.2 represents 1, can also represent 0,N.sub.2 represents 0 or 1,And wherein two additional bonds, either corresponding to the dashed lines or corresponding to the dotted lines, are present, with m.sub.1 representing 0 in the former case and m.sub.2 representing 0 in the latter case, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, particularly hypoglycaemic activity.

    摘要翻译： 本发明提供具有式I 的新的亚氨基化合物