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    Tripeptide derivatives with central nervous system activity and preparation thereof
    1.
    发明授权
    Tripeptide derivatives with central nervous system activity and preparation thereof 失效
    具有中枢神经系统活性的三肽衍生物及其制备方法

    公开(公告)号：US4018912A

    公开(公告)日：1977-04-19

    申请号：US599450

    申请日：1975-07-28

    申请人： Amedeo Failli ,  Hans U. Immer ,  Manfred Gotz

    发明人： Amedeo Failli ,  Hans U. Immer ,  Manfred Gotz

    IPC分类号： C07K5/08 ,  A61K38/00 ,  A61K38/06 ,  A61P25/00 ,  C07K1/02 ,  C07K1/113 ,  C07K5/097 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K5/0823 ,  Y02P20/55

    摘要： The tripeptide derivatives of formula 1H--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R.sup.1 is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.

    摘要翻译： 式1的HL-Pro-N（R1）CH（R2）CO-Y-R3（1）的三肽衍生物，其中R 1是氢，低级烷基或NR 4 R 5，其中R 4和R 5各自是低级烷基，R 2是氢或更低 烷基，R3是氨基，低级烷基氨基，二（低级）烷基氨基或氨基（低级）烷基氨基，Y是氨基酸残基Gly或D-Ala之一，条件是当R 1是NR 4 R 5时，其中R 4和R 5如本文所定义 并且R 2和Y如本文所定义，R 3是低级烷基氨基，二（低级）烷基氨基或氨基（低级）烷基氨基，并且公开了其制备方法。 式1的三肽衍生物具有中枢神经系统活性，并给出了其使用方法。

    Derivatives of imidazolidin-2-ones and -2-thiones
    2.
    发明授权
    Derivatives of imidazolidin-2-ones and -2-thiones 失效
    咪唑烷-2-酮衍生物和2,3-噻二唑的衍生物

    公开(公告)号：US3979380A

    公开(公告)日：1976-09-07

    申请号：US585019

    申请日：1975-06-09

    申请人： Amedeo Failli ,  Manfred Gotz

    发明人： Amedeo Failli ,  Manfred Gotz

    IPC分类号： C07D233/88 ,  C07D235/02 ,  C07D401/04 ,  C07D403/04

    CPC分类号： C07D235/02

    摘要： There are disclosed herein derivatives of imidazolidin-2-ones and -2-thiones of the formula I ##SPC1##and their acid addition salts with pharmacologically acceptable acids, in which R.sup.1 is hydrogen or lower alkyl; R.sup.2 is lower alkyl, nitrothiazolyl, or nitrofuryl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached are a heterocyclic group containing 4-6 carbon atoms, or 4 carbon atoms and an additional nitrogen atom which may optionally be substituted with a lower alkyl group, or 4 carbon atoms and an oxygen atom, R.sup.3 is hydrogen or lower alkyl; R.sup.4 is lower alkyl or aralkyl, or R.sup.3 and R.sup.4 together with the carbon atom 5 of the imidazolidine ring to which they are attached are a carbocyclic ring containing 5-6 carbon atoms attached in spiro fashion to said imidazolidine ring; R.sup.5 is lower alkyl or cycloalkyl containing from 5-6 carbon atoms; and X is an oxygen or a sulfur atom. The compounds of this invention possess positive inotropic activity and are useful as cardiac stimulants.

    摘要翻译： 本文公开了式I的咪唑烷-2-酮和2-硫杂的衍生物及其与药理学上可接受的酸的酸加成盐，其中R 1是氢或低级烷基; R2是低级烷基，硝基噻唑基或硝基呋喃基; 或R 1和R 2与它们所连接的氮一起是含有4-6个碳原子或4个碳原子的杂环基，以及另外的氮原子，其可任选被低级烷基或4个碳原子和 氧原子，R3是氢或低级烷基; R 4是低级烷基或芳烷基，或者R 3和R 4与它们所连接的咪唑烷环的碳原子5一起是含5-6个碳原子的碳环，所述碳环与所述咪唑烷环螺旋连接; R5是含有5-6个碳原子的低级烷基或环烷基; X是氧或硫原子。 本发明的化合物具有正性肌力活性，可用作心脏兴奋剂。

    Biphenyl vasopressin agonists
    3.
    发明申请
    Biphenyl vasopressin agonists 失效

    公开(公告)号：US20060276456A1

    公开(公告)日：2006-12-07

    申请号：US11502982

    申请日：2006-08-11

    申请人： Kevin Memoli ,  Amedeo Failli ,  Thomas Caggiano ,  Jay Shumsky ,  Eugene Trybulski ,  John Dusza

    发明人： Kevin Memoli ,  Amedeo Failli ,  Thomas Caggiano ,  Jay Shumsky ,  Eugene Trybulski ,  John Dusza

    IPC分类号： A61K31/551 ,  C07D487/02

    CPC分类号： C07D243/10 ,  C07D243/38 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04

    摘要： A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.

    Biphenyl vasopressin agonists
    8.
    发明申请
    Biphenyl vasopressin agonists 失效
    联苯加压素激动剂

    公开(公告)号：US20050075328A1

    公开(公告)日：2005-04-07

    申请号：US10980939

    申请日：2004-11-04

    申请人： Amedeo Failli ,  John Dusza ,  Thomas Caggiano ,  Jay Shumsky ,  Kevin Memoli ,  Eugene Trybulski

    发明人： Amedeo Failli ,  John Dusza ,  Thomas Caggiano ,  Jay Shumsky ,  Kevin Memoli ,  Eugene Trybulski

    IPC分类号： A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/5517 ,  A61P5/02 ,  A61P13/00 ,  A61P13/02 ,  C07D243/10 ,  C07D243/38 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04 ,  C07D487/12

    CPC分类号： C07D243/10 ,  C07D243/38 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04

    摘要： A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.

    摘要翻译： 式（I）或（II）的化合物：其中：Y是选自NR或 - （CH 2）n的部分; 其中R是氢或（C1-C6）低级烷基，n是1; （C1-C6）低级烷基，卤素，氰基，CF3，羟基，（C1-C6）低级烷氧基，（C1-C6）低级烷氧基，（C1-C6）低级烷氧基，（C1-C6） C 1 -C 6低级烷氧基羰基，羧基-CONH 2，-CONH [（C 1 -C 6）低级烷基]，-CON [（C 1 -C 6）低级烷基] 或（2）任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的具有一个氮原子的6元芳族（不饱和）杂环; 表示：（1）任选被一个或两个取代基取代的苯环，所述取代基独立地选自氢，（C 1 -C 6）低级烷基，卤素，氰基，CF 3，羟基，（C 1 -C 6）低级烷氧基或 （C 1 -C 6）低级烷氧基羰基，羧基，-CONH 2，-CONH [（C 1 -C 6）低级烷基]，-CON [（C 1 -C 6）低级烷基] 或（2）任选被（C 1 -C 6）低级烷基，（C 1 -C 6）低级烷氧基或卤素取代的具有一个氮原子的5元芳族（不饱和）杂环; 或（3）具有一个氮原子，任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的6元芳族（不饱和）杂环; 表示任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的具有一个硫原子的5元芳族（不饱和）杂环; R 1是下式的部分，R 2，R 3，R 7，R 8和R 9独立地选自氢

    N-Substituted cyclopeptide derivatives
    9.
    发明授权
    N-Substituted cyclopeptide derivatives 失效
    N-取代的环肽衍生物

    公开(公告)号：US4351828A

    公开(公告)日：1982-09-28

    申请号：US164663

    申请日：1980-06-30

    申请人： Amedeo Failli ,  Hans U. Immer ,  Manfred K. Gotz

    发明人： Amedeo Failli ,  Hans U. Immer ,  Manfred K. Gotz

    IPC分类号： A61K38/00 ,  C07K7/64 ,  A61K37/00

    CPC分类号： C07K7/64 ,  A61K38/00 ,  Y10S930/19 ,  Y10S930/27 ,  Y10S930/29

    摘要： The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.

    摘要翻译： 式I的N-取代的环肽衍生物，其中R 1是低级烷基，R 2是低级烷基或环（低级）烷基，R 3是中性氨基酸侧链，Y是一个肽残基， 公开了9个氨基酸残基和制备式I化合物的方法。 式I的化合物是有用的抗菌和抗真菌剂。 也公开了药物组合物。