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    Spirocyclic aminoacid derivatives, processes for their preparation, agents containing them and their use and new spirocyclic aminoacids as intermediates and processes for their preparation
    71.
    发明授权
    Spirocyclic aminoacid derivatives, processes for their preparation, agents containing them and their use and new spirocyclic aminoacids as intermediates and processes for their preparation 失效
    螺环氨基酸衍生物，其制备方法，含有它们的药剂及其用途和新的螺环氨基酸作为中间体及其制备方法

    公开(公告)号：US4620012A

    公开(公告)日：1986-10-28

    申请号：US569758

    申请日：1984-01-10

    申请人： Rainer Henning ,  Hansjorg Urbach ,  Volker Teetz ,  Reinhard Becker

    发明人： Rainer Henning ,  Hansjorg Urbach ,  Volker Teetz ,  Reinhard Becker

    IPC分类号： A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07D209/96 ,  C07D317/28 ,  C07D317/30 ,  C07D317/32 ,  C07D317/72 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K14/81 ,  C07C103/52 ,  A61K37/02

    CPC分类号： C07K5/0222 ,  C07D209/96 ,  C07D317/28 ,  C07D317/30 ,  A61K38/00

    摘要： The invention relates to new spirocyclic aminoacid derivatives of the formula I ##STR1## in which m denotes 1 or 2, n denotes 0 or 1, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen or alkyl which can be optionally substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted as defined above in the aryl radical, an S- or O- and/or N-heterocyclic radical or a side chain of an .alpha.-aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, processes for their preparation, agents containing them and their use and new spirocyclic aminoacids as intermediates and a process for their preparation.

    摘要翻译： 本发明涉及式I（I）的新的螺环氨基酸衍生物，其中m表示1或2，n表示0或1，R表示氢，烷基或芳烷基，R1表示氢或可任意取代的烷基 芳基或部分氢化的芳基，其中每一个可以被烷基，烷氧基或卤素取代，芳基烷基或芳酰基烷基，它们都可以如上所述被取代，在芳基 基团，S-或O-和/或N-杂环基团或α-氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z在一起 表示氧，X表示烷基，烯基，环烷基，芳基，其可以被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基和/或亚甲二氧基或3-吲哚基单取代或三取代， 准备工作 包含它们及其用途和新的螺环氨基酸作为中间体及其制备方法。

    PEPTIDES AND PEPTIDE DERIVATIVES AS WELL AS PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    72.
    发明申请
    PEPTIDES AND PEPTIDE DERIVATIVES AS WELL AS PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 审中-公开
    肽和肽衍生物作为含有其的药物组合物

    公开(公告)号：US20110098442A1

    公开(公告)日：2011-04-28

    申请号：US12280543

    申请日：2007-02-23

    申请人： Peter Petzelbauer ,  Rainer Henning ,  Sonja Reingruber

    发明人： Peter Petzelbauer ,  Rainer Henning ,  Sonja Reingruber

    IPC分类号： C07K14/00

    CPC分类号： C07K14/75 ,  A61K38/00 ,  Y02A50/385

    摘要： Peptides and peptide derivatives of the following general Formula (I): H2N-GHRPX1X2X3X4X5X6X7X8X9X10X11PX12PPPX13X14X15X16GYR—X17 (I), wherein: X1-X16 denote one of the 20 genetically encoded amino acids, X17 denotes OR1, with R1=hydrogen or (C1-C10-alkyl), or NR2R3, R2 and R3 being identical or different and denoting hydrogen, (C1-C10)-alkyl, or a residue -PEG5-60K, wherein the PEG-residue is linked to the N atom via a spacer, or a residue NH—Y-Z-PEG5-60K, wherein Y denotes a chemical bond or a genetically coded amino acid from among the group of S, C, K or R, and Z denotes a spacer by way of which a polyethylene glycol (PEG)-residue may be linked, as well as the physiologically acceptable salts thereof, or wherein: X15 or X16 denotes an amino acid from the group of C or K, which is linked to a residue Z-PEG5-60K via the heteroatom in the side chain, and wherein X17 denotes OR1, with R1=hydrogen or (C1-C10-alkyl), or NR2R3, R2 and R3 being identical or different and denoting hydrogen or (C1-C10)-alkyl, as well as the physiologically acceptable salts thereof.

    摘要翻译： 下列通式（I）的肽和肽衍生物：H2N-GHRPX1X2X3X4X5X6X7X8X9X10X11PX12PPPX13X14X15X16GYR-X17（I），其中：X1-X16表示20个遗传编码氨基酸之一，X17表示OR1，其中R1 =氢或（C1-C10 - 烷基）或NR 2 R 3，R 2和R 3相同或不同，表示氢，（C 1 -C 10） - 烷基或残基-PEG 5-60K，其中PEG残基通过间隔基与N原子相连，或 残基NH-YZ-PEG5-60K，其中Y表示S，C，K或R组中的化学键或遗传编码的氨基酸，Z表示间隔基，通过其可以使用聚乙二醇（PEG） 可以连接残基，以及其生理上可接受的盐，或其中：X15或X16表示C或K基团的氨基酸，其通过侧面的杂原子与残基Z-PEG5-60K连接 链，其中X17表示OR1，其中R1 =氢或（C1-C10-烷基）或NR2R3，R2和R3相同或不同，表示氢 基或（C 1 -C 10） - 烷基，以及其生理上可接受的盐。

    Peptides and peptide derivatives as well as pharmaceutical compositions containing the same
    73.
    发明授权
    Peptides and peptide derivatives as well as pharmaceutical compositions containing the same 失效
    肽和肽衍生物以及含有它们的药物组合物

    公开(公告)号：US07799758B2

    公开(公告)日：2010-09-21

    申请号：US11678535

    申请日：2007-02-23

    申请人： Peter Petzelbauer ,  Rainer Henning ,  Sonja Reingruber

    发明人： Peter Petzelbauer ,  Rainer Henning ,  Sonja Reingruber

    IPC分类号： A61K38/16 ,  C07K14/00

    CPC分类号： C07K14/75 ,  A61K38/00 ,  Y02A50/385

    摘要： Therapeutic compositions can include modified peptides which are derived from the chain of the Bbeta(15-42)-fibrin fragment and wherein one or several of the amino acids of the sequence have been substituted by genetically encoded or not genetically encoded amino acids or peptidomimetics. They may exist as free peptides or as C-terminal derivative and/or being linked to a polyethylene glycol (PEG)-polymer, and have anti-inflammatory and/or endothelium stabilizing effects. Esters or amides may for instance be taken into consideration as C-terminal derivatives. Processes for production of the peptides and derivatives thereof are also described.

    摘要翻译： 治疗组合物可以包括衍生自Bβ（15-42） - 纤维蛋白片段的链的修饰肽，并且其中序列的一个或几个氨基酸已被遗传编码的或未经遗传编码的氨基酸或肽模拟物取代。 它们可以作为游离肽或C末端衍生物存在和/或与聚乙二醇（PEG） - 聚合物连接，并具有抗炎和/或内皮稳定作用。 酯或酰胺可以例如被考虑为C末端衍生物。 还描述了肽及其衍生物的制备方法。

    Cis, endo-2-azabicycloalkane-3-carboxylic acid derivatives
    77.
    发明授权
    Cis, endo-2-azabicycloalkane-3-carboxylic acid derivatives 失效
    Cis，内-2-氮杂双环链烷-3-羧酸衍生物

    公开(公告)号：US5550255A

    公开(公告)日：1996-08-27

    申请号：US202478

    申请日：1994-02-28

    申请人： Hansj org Urbach ,  Rainer Henning ,  Winfried Hertzsch

    发明人： Hansj org Urbach ,  Rainer Henning ,  Winfried Hertzsch

    IPC分类号： C07D209/42 ,  A61K31/40 ,  C07D207/42 ,  C07D209/02 ,  C07D209/52 ,  A61K31/405

    CPC分类号： C07D207/42 ,  C07D209/52

    摘要： The invention relates to compounds of the formula I ##STR1## in which n is 1, 2 or 3,Z.sup.1 and Z.sup.2, and Z.sup.3 and Z.sup.4, in each case together represent a chemical bond orZ.sup.1, Z.sup.2, Z.sup.3 and Z.sup.4 in each case represent hydrogen,Z.sup.1 and Z.sup.2 being in the cis configuration relative to one another and the COR.sup.1 group on C atom 3 being in the endo configuration relative to the bicyclic ring system,R.sup.1 denotes hydroxyl, alkoxy, aralkoxy, amino, alkylamino or dialkylamino andR.sup.2 denotes hydrogen, alkyl, aryl, aralkyl, cycloalkyl or alkylcycloalkyl,processes for their preparation and their use.

    摘要翻译： 本发明涉及式Ⅰ（I）化合物，其中n为1,2或3，Z 1和Z 2，Z 3和Z 4各自在一起代表化学键或Z 1，Z 2，Z 3和Z 4 在每种情况下代表氢，Z1和Z2相对于彼此处于顺式构型，并且C原子3上的COR1基团相对于双环系统处于内部构型，R1表示羟基，烷氧基，芳烷氧基，氨基，烷基氨基或 二烷基氨基，R 2表示氢，烷基，芳基，芳烷基，环烷基或烷基环烷基，其制备及其用途。