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    Oligopeptidylargininol derivatives and their homologs, a process for their preparation, their use and agents containing them
    1.
    发明授权
    Oligopeptidylargininol derivatives and their homologs, a process for their preparation, their use and agents containing them 失效
    寡肽酰胆固醇衍生物及其同系物，其制备方法，其用途和含有它们的试剂

    公开(公告)号：US4713369A

    公开(公告)日：1987-12-15

    申请号：US829482

    申请日：1986-02-14

    申请人： Werner Stuber

    发明人： Werner Stuber

    IPC分类号： C07D207/16 ,  C07K1/113 ,  C07K5/06 ,  C07K5/065 ,  C07K14/81 ,  A61K37/43 ,  C07C103/20 ,  C07K5/08

    CPC分类号： C07K5/06078 ,  Y02P20/55

    摘要： The invention relates to new peptidylargininol derivatives and their homologs of the general formulaX-D-Phe-Pro-A-Y.(HB).sub.n,X being a hydrogen atom or a known protective group customary in peptide chemistry,D-Phe being D-phenylalanine,Pro being L-proline,A being a .omega.-guanidiano-.beta.-aminoalkanol residue of the formula --NHCH (CH.sub.2).sub.m NHC(NH)NH.sub.2 CH.sub.2 O, with m being 2 to 5, preferably an argininol residue or a homoargininol residue,Y being a hydrogen atom or an ester-forming group,B being an acid residue, andn being 0, 1 or 2,and to a process for the preparation of these compounds, to pharmaceutical agents containing these compounds, and to the use of these agents as thrombin inhibitors.

    摘要翻译： 本发明涉及通式XD-Phe-Pro-AY（HB）n，X为氢原子或肽化学中常用的已知保护基的新型肽基缩水甘油衍生物及其同系物，D-Phe为D-苯丙氨酸， Pro是L-脯氨酸，A是式-NHCH（CH 2）m NHC（NH）NH 2 CH 2 O的ω-胍基-β-氨基链烷醇残基，m为2至5，优选精氨醇残基或高精氨醇残基，Y为 氢原子或成酯基，B为酸残基，n为0,1或2，以及这些化合物的制备方法，含有这些化合物的药剂，以及这些试剂用作 凝血酶抑制剂。

    Novel sypathomimetic amine prodrugs
    3.
    发明授权
    Novel sypathomimetic amine prodrugs 失效

    公开(公告)号：US4313956A

    公开(公告)日：1982-02-02

    申请号：US108055

    申请日：1979-12-28

    申请人： Nicholas S. Bodor ,  Kenneth B. Sloan ,  Stefano A. Pogany

    发明人： Nicholas S. Bodor ,  Kenneth B. Sloan ,  Stefano A. Pogany

    IPC分类号： C07C233/16 ,  C07C149/40 ,  A61K31/165 ,  A61K31/22 ,  A61K31/235 ,  A61K31/245 ,  A61K31/25 ,  A61K31/265 ,  C07C67/02 ,  C07C69/00 ,  C07C69/74 ,  C07C69/76 ,  C07C79/46 ,  C07C97/16 ,  C07C101/20 ,  C07C101/44 ,  C07C101/72 ,  C07C102/00 ,  C07C103/20 ,  C07C153/00 ,  C09F5/08

    CPC分类号： C07C233/16 ,  Y02P20/55

    摘要： Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.2 is selected from the group consisting of straight or branched chain alkyl having from 1 to 20 carbon atoms; aryl having from 6 to 10 carbon atoms; cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 2 to 20 carbon atoms; cycloalkenyl having from 4 to 8 carbon atoms; alkynyl having from 2 to 20 carbon atoms; aralkyl, alkaryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, loweracyloxyalkyl, and carboxyalkyl, wherein alkyl, aryl, alkenyl and alkynyl are as defined above; saturated or unsaturated monoheterocyclic or polyheterocyclic, or fused heterocyclic, containing from 1 to 3 of any one or more of the hetero atoms N, S or O in each heterocyclic ring thereof and each such ring being from 3- to 8-membered; and mono-or poly-substituted derivatives of the above, each of said substituents being selected from the group consisting of lower alkyl, lower alkoxy, lower acyl, lower acyloxy, halo, haloloweralkyl, cyano, carbethoxy, loweralkylthio, amino, nitro, loweralkylamino, diloweralkylamino, carboxyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl and ##STR2## wherein R.sup.4 is hydrogen or alkyl having from 1 to 10 carbons; R.sup.3 is hydrogen, R.sup.2, lower acyl, cyano, haloloweralkyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl, --CH.sub.2 ONO.sub.2 and --CH.sub.2 OCOR.sup.2 ; R.sup.5 is hydrogen or lower alkyl; (ii) the structural formula (II): ##STR3## wherein X, R.sup.2 and R.sup.3 are as defined above and R.sup.1 is the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine; (iii) either of the structural formulae (I) or (II) wherein ##STR4## is the residue of any naturally occurring protein amino acid, the residue of any N-substituted naturally occurring amino acid, which N-substituent is lower alkyl or any amino acid protective group cleavable via hydrogenolysis or hydrolysis, or the residue of an N, N-lower dialkyl or C.sub.4 -C.sub.7 cycloalkylamino acid; and (iv) the non-toxic, pharmaceutically acceptable salts thereof.

    Ephedrine and pseudoephedrine precursors
    4.
    发明授权
    Ephedrine and pseudoephedrine precursors 失效
    麻黄碱和伪麻黄素前体

    公开(公告)号：US4277420A

    公开(公告)日：1981-07-07

    申请号：US78111

    申请日：1979-09-24

    申请人： Karl E. Koenig

    发明人： Karl E. Koenig

    IPC分类号： C07C233/00 ,  C07C233/12 ,  C07C103/20 ,  C07C103/75

    CPC分类号： C07C233/00 ,  C07C233/12

    摘要： Preparation of novel prochiral olefinic compounds which can be asymmetrically hydrogenated to enantiomers, which are converted to ephedrine and pseudoephedrine by described procedures.

    摘要翻译： 可以不对称氢化成对映体的新型前手性烯烃化合物的制备，其通过所述方法转化为麻黄碱和伪麻黄碱。

    N-(2-Aminocyclopentyl)-N-alkanoylanilides as CNS anti-depressants
    5.
    发明授权
    N-(2-Aminocyclopentyl)-N-alkanoylanilides as CNS anti-depressants 失效
    N-（2-氨基环戊基）-N-烷酰苯胺作为CNS抗抑郁剂

    公开(公告)号：US4204003A

    公开(公告)日：1980-05-20

    申请号：US876349

    申请日：1978-02-09

    申请人： Jacob Szmuszkovicz

    发明人： Jacob Szmuszkovicz

    IPC分类号： A61K31/16 ,  A61K31/27 ,  A61K31/40 ,  A61K31/445 ,  C07C233/02 ,  C07D295/096 ,  C07D295/12 ,  C07D295/135 ,  A61K31/165 ,  C07C103/20 ,  C07C103/22

    CPC分类号： C07D295/096 ,  A61K31/16 ,  A61K31/27 ,  A61K31/40 ,  A61K31/445 ,  C07C247/00 ,  C07D295/12 ,  C07D295/135

    摘要： N-(2-Aminocyclopentyl)N-alkanoylanilides and their 2-N-oxides of the formula ##STR1## e.g., trans-3,4-dichloro-N-[2-(dimethylamino)cyclopentyl]propionanilide, and their pharmacologically acceptable salts, have been found to possess potent Central Nervous System anti-depressant properties. Many of them are new.These compounds are promising anti-depressant drugs which are characterized by a better therapeutic ratio than imipramine, and long acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are disclosed.

    摘要翻译： N-（2-氨基环戊基）N-烷酰基苯胺及其2-N-氧化物，例如反式-3,4-二氯-N- [2-（二甲氨基）环戊基]丙酰苯胺及其药理学上可接受的盐 已被发现具有强大的中枢神经系统抗抑郁特性。 其中许多是新的。 这些化合物是有希望的抗抑郁药物，其特征在于比丙咪嗪具有更好的治疗比例，以及可能允许施用之间更长持续时间的长效活性，例如每天一次。 公开了含有这些化合物的药物组合物和用这些组合物治疗抑郁症的方法。

    Plasminogen activating enzyme-specific competitive inhibitor
    6.
    发明授权
    Plasminogen activating enzyme-specific competitive inhibitor 失效
    纤溶酶原激活酶特异性竞争性抑制剂

    公开(公告)号：US4165258A

    公开(公告)日：1979-08-21

    申请号：US620792

    申请日：1975-10-08

    申请人： E. Kendall Pye ,  Thomas Maciag ,  Michael K. Weibel ,  Melicote R. Iyengar

    发明人： E. Kendall Pye ,  Thomas Maciag ,  Michael K. Weibel ,  Melicote R. Iyengar

    IPC分类号： C12N9/72 ,  C12N9/99 ,  C07G7/02 ,  C07C103/20 ,  C07C103/28

    CPC分类号： C12N9/6462 ,  C12N9/99 ,  C12Y304/21073 ,  Y10S435/815

    摘要： A novel plasminogen activating enzyme-specific competitive inhibitor is disclosed consisting of an amino-terminated .alpha.-N-substituted aminocarboxylic acid, such as .alpha.-N-benzylsulfonyl-p-aminophenylalanine, or the acid derivatives thereof. The competitive inhibitor ligand, when covalently coupled to the surface of a water-insoluble solid support material through a spacer chain of at least 4 carbon atoms, is useful as a biospecific extracting agent for use in affinity chromatography of plasminogen activating enzymes, such as urokinase, cytokinase, and the like, from crude aqueous preparations thereof, such as mammalian urine, mammalian body tissue preparations, mammalian plasma and spent tissue culture growth medium.

    摘要翻译： 公开了一种新型的纤溶酶原激活酶特异性竞争性抑制剂，其由氨基封端的α-N-取代的氨基羧酸如α-N-苄基磺酰基 - 对氨基苯丙氨酸或其酸衍生物组成。 当竞争性抑制剂配体通过至少4个碳原子的间隔链与水不溶性固体支持材料的表面共价偶联时，可用作生物特异性提取剂，用于纤溶酶原激活酶如尿激酶的亲和层析 ，细胞激酶等，其粗制水性制剂如哺乳动物尿，哺乳动物身体组织制剂，哺乳动物血浆和废组织培养生长培养基。