知搜-全球专利检索

  1. Login
  2. Sign Up

Search Results

30 records (took 0.015 seconds)

    Synthesis and use of &agr;-ketoamide derivatives and arrays
    1.
    发明授权
    Synthesis and use of &agr;-ketoamide derivatives and arrays 失效
    α-酮酰胺衍生物和阵列的合成和应用

    公开(公告)号：US06452050B1

    公开(公告)日：2002-09-17

    申请号：US09531737

    申请日：2000-03-21

    Applicant: Carmen M. Baldino ,  David L. Coffen ,  Stewart D. Chipman ,  Hong Cheng

    Inventor： Carmen M. Baldino ,  David L. Coffen ,  Stewart D. Chipman ,  Hong Cheng

    IPC: C07C23307

    CPC classification number: C40B40/04 ,  C07C275/40 ,  C07C335/20 ,  C07D333/60

    Abstract: The invention is based on new methods for making and using compounds and arrays of novel &agr;-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 &agr;-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutical agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.

    Abstract translation: 本发明基于制备和使用新型α-酮酰胺的化合物和阵列的新方法，以及通过这些方法制备的阵列和化合物。 这些新型化合物是蛋白水解酶的潜在抑制剂，特别是半胱氨酸蛋白酶如克鲁津。 新方法的应用已经导致了一系列新的抑制剂的鉴定，其中有大约38,000个α-酮酰胺衍生物，具有针对三个半胱氨酸蛋白酶：克鲁津，木瓜蛋白酶和组织蛋白酶B的比活性。这些化合物和其它化合物 通过本文所述的方法鉴定可用于例如开发用于治疗与这些蛋白酶相关的疾病（例如恰加斯病）的药剂。 虽然所公开的化合物对克鲁津，木瓜蛋白酶，组织蛋白酶B具有比活性，但本文所述的方法也可用于鉴定其它蛋白酶的抑制剂。

    Spiro[pyrrolidine-2,3′-oxindole] compounds and method of use
    2.
    发明授权
    Spiro[pyrrolidine-2,3′-oxindole] compounds and method of use 失效
    螺[吡咯烷-2,3'-羟吲哚]化合物及其使用方法

    公开(公告)号：US06358750B1

    公开(公告)日：2002-03-19

    申请号：US09535719

    申请日：2000-03-27

    Applicant: Demosthenes Fokas ,  David L. Coffen ,  William J. Ryan

    Inventor： Demosthenes Fokas ,  David L. Coffen ,  William J. Ryan

    IPC: G01N33566

    CPC classification number: C07D487/10 ,  C40B40/00 ,  G01N33/573 ,  G01N33/68 ,  G01N33/86

    Abstract: The invention provides spiro[pyrrolidine-2,3′-oxindole] compounds and libraries of these compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, &agr;-amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles). The new libraries can be assayed using any of many known screening procedures for activity, e.g., biological activity. For example, the libraries can be screened for activity as drugs (e.g., anticancer drugs, antibiotics, antiviral drugs, antiinflammatory drugs, analgesics, immunomodulators, neuroleptics, sedatives, stimulants, or diagnostic aids), bioseparation agents, or pesticides (e.g., herbicides, insecticides, or rodenticides).

    Abstract translation: 本发明提供了螺[吡咯烷-2,3'-羟吲哚]化合物和这些化合物的文库，其通过各种取代的异头ins素，α-氨基酸和dipolarophicity的立体和区域选择性反应（例如反式查尔酮，丙烯酸酯 酯或乙烯基羟吲哚）。 可以使用许多已知的活性筛选方法（例如生物活性）来测定新的文库。 例如，图书馆可以作为药物（例如，抗癌药物，抗生素，抗病毒药物，抗炎药，止痛剂，免疫调节剂，精神安定药，镇静剂，兴奋剂或诊断辅助剂），生物分离剂或杀虫剂（例如除草剂 ，杀虫剂或杀鼠剂）。

    Glycidic acid ester and process of preparation
    3.
    发明授权
    Glycidic acid ester and process of preparation 失效
    糖苷酸酯及其制备方法

    公开(公告)号：US5008411A

    公开(公告)日：1991-04-16

    申请号：US416295

    申请日：1989-10-02

    Applicant: David L. Coffen ,  Pradeep B. Madan ,  Alan Schwartz

    Inventor： David L. Coffen ,  Pradeep B. Madan ,  Alan Schwartz

    IPC: C07C319/20 ,  C07C323/56 ,  C07D281/08 ,  C07D281/10

    CPC classification number: C07C319/20 ,  C07D281/08 ,  C07D281/10 ,  C07C2101/14

    Abstract: A process for the preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl or nitro; or R.sub.1 and R.sub.2 taken together with the benzene ring to which they are attached are naphthalene, and Ar is p-lower alkoxy phenyl.which comprises reacting ##STR2## wherein R.sub.1 and R.sub.2 are as described above with the compound of the formula ##STR3## wherein Ar is as described above, in an aromatic organic compound. The intermediates formed by the process of the invention are useful in the production of thiazepin-4(5H)-ones which have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure and agents for treating ischemia.

    Abstract translation: 制备式IV化合物的方法，其中R 1和R 2各自独立地为氢，1至4个碳原子的烷基，1至4个碳原子的烷氧基，卤素，三氟甲基或硝基; 或者R 1和R 2与它们所连接的苯环一起为萘，Ar为对低级烷氧基苯基。 其中包括使其中R 1和R 2如上所述的其中Ar如上所述的式IIIa化合物在芳族有机化合物中反应。 通过本发明的方法形成的中间体可用于制备具有钙通道阻断剂活性的硫氮平-4（5H）酮，因此可用作降低血压的药剂和用于治疗缺血的药剂。

    Novel 4-phenoxy-5-sulfamylbenzoic acid
    7.
    发明授权
    Novel 4-phenoxy-5-sulfamylbenzoic acid 失效
    新型4-苯氧基-5-亚磺酰基苯甲酸

    公开(公告)号：US4208535A

    公开(公告)日：1980-06-17

    申请号：US925004

    申请日：1978-07-14

    Applicant: David L. Coffen

    Inventor： David L. Coffen

    IPC: C07D207/26 ,  C07D207/27 ,  C07D295/155 ,  C07C143/78 ,  A61K31/195

    CPC classification number: C07D207/27 ,  C07D295/155 ,  Y10S514/869

    Abstract: Novel 3-(butylamino) or (1-pyrrolidinyl)-4-phenoxy-5-sulfamylbenzoic acid derivatives where the butyl group contains either a double bond or a hydroxy, ketone, acid or ester functional group or groups, said compounds being useful as diuretics.

    Abstract translation: 新的3-（丁基氨基）或（1-吡咯烷基）-4-苯氧基-5-亚磺酰基苯甲酸衍生物，其中丁基含有双键或羟基，酮，酸或酯官能团或基团，所述化合物可用作 利尿剂。

Patent Agency Ranking