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    Amidinophenol derivatives
    62.
    发明授权
    Amidinophenol derivatives 失效
    脒基苯酚衍生物

    公开(公告)号：US5432178A

    公开(公告)日：1995-07-11

    申请号：US121499

    申请日：1993-09-16

    Applicant: Hisao Nakai ,  Masanori Kawamura ,  Tsumoru Miyamoto

    Inventor： Hisao Nakai ,  Masanori Kawamura ,  Tsumoru Miyamoto

    IPC: C07D295/18 ,  A61K31/235 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/495 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C257/18 ,  C07C323/59 ,  C07C323/62 ,  C07C323/63 ,  C07D205/04 ,  C07D207/08 ,  C07D207/16 ,  C07D209/20 ,  C07D223/04 ,  C07D295/185 ,  C07D295/192 ,  A61K31/445 ,  C07D241/04 ,  C07D295/182

    CPC classification number: C07D295/185 ,  C07C257/18 ,  C07C323/59 ,  C07C323/62 ,  C07D207/16 ,  C07D209/20 ,  C07D295/192 ,  C07C2101/02 ,  C07C2101/04 ,  C07C2101/10 ,  C07C2101/14

    Abstract: Amidinophenol derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO.sub.2, (vii) benzoyl, (viii) COOR.sup.4 (in which R.sup.4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R.sup.5).dbd.C(R.sup.6)-- (in which R.sup.5 and R.sup.6 are H or C1-4 alkyl; R.sup.3 is (i) CON(R.sup.7)(R.sup.8), (ii) CON(R.sup.9)--CH(R.sup.7)(R.sup.8) or (iii) ##STR2## in which ##STR3## is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R.sup.10 is H, C7-10 phenylalkyl or COOR.sup.13 (in which R.sup.13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R.sup.7 and R.sup.8 do not represent hydrogen at the same time, and (ii) when at least one group in R.sup.7, R.sup.8 and R.sup.9 represents the group containing t-butyl ester, the other groups do not represent tile group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA.sub.2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.

    Abstract translation: 式（I）的脒基苯酚衍生物：其中R 1和R 2是（ⅰ）H，（ⅱ）C 1-4烷基，（ⅲ）C 1-4烷氧基，（ⅳ）C 2-5酰基，（ v）卤素，（vi）NO 2，（vii）苯甲酰基，（viii）COOR 4（其中R 4是C 1-3烷基）; A是键，C1-4亚烷基，-C（R5）= C（R6） - （其中R5和R6是H或C1-4烷基; R3是（i）CON（R7）（R8） CON（R9）-CH（R7）（R8）或（iii）其中IMAGE是含有1或2个N原子的4-7元单环杂环; R10是H，C7-10苯基烷基 或COOR13（其中R13为H，C1-4烷基或C7-10苯基烷基））; 条件是（i）R7和R8不同时代表氢，和（ii）当R7，R8和R9中的至少一个基团代表含有叔丁基的基团时，其它基团不表示 含羧基的瓷​​砖组; 或其酸加成盐对PLA2和各种蛋白酶如胰蛋白酶，纤溶酶，凝血酶，激肽释放酶，特别是胰蛋白酶具有抑制活性，可用于预防和/或治疗各种炎性疾病，过敏性疾病，传播性疾病 血管内凝血，胰腺炎，胰腺炎和多器官功能衰竭的严重程度。

    Fungicidal substituted amino acid amides
    65.
    发明授权
    Fungicidal substituted amino acid amides 失效
    杀真菌剂取代氨基酸酰胺

    公开(公告)号：US5411987A

    公开(公告)日：1995-05-02

    申请号：US23241

    申请日：1993-02-25

    Applicant: Detlef Wollweber ,  Thomas Seitz ,  Wilhelm Brandes

    Inventor： Detlef Wollweber ,  Thomas Seitz ,  Wilhelm Brandes

    IPC: C07D295/00 ,  A01N47/10 ,  A01N47/12 ,  A01N47/18 ,  C07C269/06 ,  C07C271/22 ,  C07C271/24 ,  C07C271/34 ,  C07C271/36 ,  C07C323/41 ,  C07D213/40 ,  C07D265/30 ,  C07D295/18 ,  C07D295/185 ,  C07D521/00 ,  A01N37/46 ,  C07C271/44

    CPC classification number: C07D295/185 ,  A01N47/12 ,  A01N47/18 ,  C07C271/22 ,  C07C323/41 ,  C07C2101/14

    Abstract: Combating fungi with substituted amine acid derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, cycloalkyl or cycloalkenyl,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and represent hydrogen, cycloalkyl or alkyl, orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring, andR.sup.6 represents hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, unsubstituted or substituted phenylalkyl, unsubstituted or substituted phenyl or unsubstituted or substituted cycloalkyl, or represents unsubstituted or substituted heterocyclyl or heterocyclylalkyl,orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a heterocyclyl radical, which can contain further hetero atoms.

    Abstract translation: 用式（I）的取代的胺酸衍生物与R1代表烷基，烯基，炔基，卤代烷基，卤代烯基，卤代链烯基，环烷基或环烯基，R2，R3，R4和R5相同或不同，代表氢 ，环烷基或烷基，或R 3和R 4与它们所键合的碳原子一起形成环烷基环，R 6表示氢，烷基，烯基，炔基，氰基烷基，未取代或取代的苯基烷基，未取代或取代的苯基或未取代的 或取代的环烷基，或表示未取代或取代的杂环基或杂环基烷基，或者R 5和R 6与它们所键合的氮原子一起表示可含有其它杂原子的杂环基。

    Process for making optically active .alpha.-amino ketones
    69.
    发明授权
    Process for making optically active .alpha.-amino ketones 失效
    制备光学活性α-氨基酮的方法

    公开(公告)号：US5364961A

    公开(公告)日：1994-11-15

    申请号：US898853

    申请日：1992-06-15

    Applicant: John J. Talley

    Inventor： John J. Talley

    IPC: B01J31/24 ,  C07C231/12 ,  C07C233/47 ,  C07C233/11 ,  C07D295/18

    CPC classification number: B01J31/2409 ,  C07C231/12 ,  C07C233/47 ,  B01J2231/645 ,  B01J2531/822 ,  B01J31/24

    Abstract: The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

    Abstract translation: 本发明包括选择性的新型光学活性α-氨基酮，其本身可用或用作制备用作抗生素，抗生素增强剂或酶抑制剂的已知酮亚甲基伪肽的中间体。 此外，本发明提供了一种脱氢/不对称氢化的方法，以获得具有两个手性中心的基本上纯的对映体。

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