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    BIS-AMINO ACID HYDROXYETHYLAMINO SULFONAMIDE RETROVIRAL PROTEASE INHIBITORS
    5.
    发明申请
    BIS-AMINO ACID HYDROXYETHYLAMINO SULFONAMIDE RETROVIRAL PROTEASE INHIBITORS 审中-公开
    BIS-氨基酸羟基乙酰氨基磺酰胺逆转录酶抑制剂

    公开(公告)号：WO1996028464A1

    公开(公告)日：1996-09-19

    申请号：PCT/US1996002685

    申请日：1996-03-07

    Applicant: G.D. SEARLE & CO. ,  GETMAN, Daniel, P. ,  DESCRESCENZO, Gary, A. ,  FRESKOS, John, N. ,  VASQUEZ, Michael, L. ,  SIKORSKI, James, A. ,  DEVADAS, Balekudru ,  NAGARAJAN, Srinivasan ,  BROWN, David, L. ,  MCDONALD, Joseph, J.

    Inventor： G.D. SEARLE & CO.

    IPC: C07K05/062

    CPC classification number: C07K5/06026 ,  A61K38/00

    Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds of formula (I) are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and the treatment of a retroviral infection.

    Abstract translation: 选择的式（I）的双氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及这种逆转录病毒蛋白酶抑制剂，更具体地涉及所选择的新化合物，用于抑制逆转录病毒蛋白酶如人类免疫缺陷病毒（HIV）蛋白酶的组合物和方法，预防性地预防逆转录病毒感染或逆转录病毒的扩散，以及 治疗逆转录病毒感染。

    DIASTEREOMERIC PURE TRIFLUOROMETHYL KETONE PEPTIDE DERIVATIVES AS INHIBITORS OF HUMAN LEUKOCYTE ELASTASE
    6.
    发明申请
    DIASTEREOMERIC PURE TRIFLUOROMETHYL KETONE PEPTIDE DERIVATIVES AS INHIBITORS OF HUMAN LEUKOCYTE ELASTASE 审中-公开
    作为人类白细胞弹性蛋白酶抑制剂的二异氰酸酯三氟乙烯酮衍生物

    公开(公告)号：WO1995021855A1

    公开(公告)日：1995-08-17

    申请号：PCT/GB1995000242

    申请日：1995-02-07

    Applicant: ZENECA LIMITED ,  PEGG, Stephen, John ,  SEPENDA, George, Joseph ,  DAVIES, Elwyn, Peter ,  VEALE, Chris, Allan

    Inventor： ZENECA LIMITED

    IPC: C07K05/062

    CPC classification number: C07K5/06052 ,  A61K38/00 ,  C07K5/06191

    Abstract: The present invention relates to crystalline forms of the compound ( S )-1-[( S )-2-(4-methoxybenzamido)-3-methylbutyryl]- N -[( S )-2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide (I) and crystalline solvates thereof which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes phrmaceutical compositions containing the crystalline forms and solvates, processes for preparing the crystalline forms and solvates and intermediates useful in the synthesis of the crystalline forms and solvates.

    Abstract translation: 本发明涉及化合物（S）-1 - [（S）-2-（4-甲氧基苯甲酰氨基）-3-甲基丁酰基] - u的结晶形式 N - [（S）-2-甲基-1-（三氟乙酰基）丙基]吡咯烷-2-甲酰胺（I）及其结晶溶剂化物，它们是人白细胞弹性蛋白酶抑制剂 HLE），也称为人嗜中性粒细胞弹性蛋白酶（HNE），使其在需要这种抑制时有用，例如用于药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。 本发明还包括含有结晶形式和溶剂化物的制剂组合物，用于制备结晶形式的溶剂合物和溶剂合物的方法以及可用于合成结晶形式和溶剂合物的中间体。

    NOVEL PEPTIDE COMPOUNDS AND MEDICINAL COMPOSITIONS THEREOF
    7.
    发明申请
    NOVEL PEPTIDE COMPOUNDS AND MEDICINAL COMPOSITIONS THEREOF 审中-公开
    新型肽类化合物及其药物组合物

    公开(公告)号：WO1997011091A1

    公开(公告)日：1997-03-27

    申请号：PCT/JP1996002697

    申请日：1996-09-19

    Applicant: KIRIN BEER KABUSHIKI KAISHA ,  KATAOKA, Shiro ,  NISHITOBA, Tsuyoshi ,  TAKAHASHI, Motoo ,  SAWA, Eiji ,  KAMISHOHARA, Masaru

    Inventor： KIRIN BEER KABUSHIKI KAISHA

    IPC: C07K05/062

    CPC classification number: C07K14/715 ,  A61K38/00 ,  G01N33/5091 ,  G01N2333/715

    Abstract: Novel peptides having the activity of regulating the function of a cell membrane receptor which carries an intracellular carboxy-terminal amino acid sequence of -A1-A2-A3, carrying an amino acid sequence consisting of at least three amino acids in the lengthwise direction, and having a carboxy-terminal sequence of -X-Y-Z (wherein X is the same as A1 or represents an amino acid belonging to the same category as A1 does; Y represents an L-amino acid or glycine; and Z is the same as A3 or represents an amino acid belonging to the same category as A3 does); derivatives thereof improved in the biological stability, cell membrane permeability or the above-mentioned regulating activity of the same and pharmaceutically acceptable salts thereof; medicinal compositions containing these compounds; a method for analyzing the function of a receptor or the C-terminus thereof by using these compounds; a method for regulating the signal transmission by a cell membrane receptor; and a method for treating diseases in association with the signal transmission by cell membrane receptors.

    Abstract translation: 具有调节携带具有长度方向由至少三个氨基酸组成的氨基酸序列的-A1-A2-A3的细胞内羧基末端氨基酸序列的细胞膜受体功能活性的新型肽，以及 具有-XYZ的羧基末端序列（其中X与A1相同或表示与A1相同类别的氨基酸; Y表示L-氨基酸或甘氨酸; Z表示与A3相同或表示 属于与A3相同类别的氨基酸）; 其衍生物改善了其生物稳定性，细胞膜通透性或其上述调节活性及其药学上可接受的盐; 含有这些化合物的药物组合物; 通过使用这些化合物分析受体或其C-末端的功能的方法; 用于调节细胞膜受体的信号传导的方法; 以及通过细胞膜受体与信号传递相关的疾病的治疗方法。

    TRICYCLIC ANTIDEPRESSANT DERIVATIVES AND CONJUGATED USEFUL IN IMMUNOASSAYS
    8.
    发明申请
    TRICYCLIC ANTIDEPRESSANT DERIVATIVES AND CONJUGATED USEFUL IN IMMUNOASSAYS 审中-公开
    三抗抗生素衍生物并联合用于免疫功能

    公开(公告)号：WO1997008192A1

    公开(公告)日：1997-03-06

    申请号：PCT/US1996013378

    申请日：1996-08-19

    Applicant: BIOSITE DIAGNOSTICS INCORPORATED

    Inventor： BIOSITE DIAGNOSTICS INCORPORATED ,  BUECHLER, Kenneth, Francis ,  NOAR, Joseph, Barry

    IPC: C07K05/062

    CPC classification number: C07K5/06026 ,  C07D223/28 ,  G01N33/9466

    Abstract: The present invention is directed to novel tricyclic antidepressant derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to tricyclic antidepressant and tricyclic antidepressant metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels my be used in the immunoassay process.

    Abstract translation: 本发明涉及新型的三环抗抑郁药衍生物，其被合成用于与抗原（蛋白质或多肽）共价连接以制备三环抗抑郁药和三环抗抑郁药代谢物的抗体或受体。 所得的新抗原可以用于使用标准方法生产抗体或受体。 一旦产生，抗体或受体和共价连接到蛋白质，多肽或标记物的新型衍生物可用于免疫测定过程。

    ACYL AMINO ACETAMIDE DERIVATIVES WITH AGONIST ACTIVITY FOR CCK-A RECEPTORS
    9.
    发明申请
    ACYL AMINO ACETAMIDE DERIVATIVES WITH AGONIST ACTIVITY FOR CCK-A RECEPTORS 审中-公开
    ACYA氨基酰胺衍生物与CCK-A受体的激活活性

    公开(公告)号：WO1996011940A1

    公开(公告)日：1996-04-25

    申请号：PCT/EP1995004026

    申请日：1995-10-12

    Applicant: GLAXO WELLCOME INC. ,  DEZUBE, Milana ,  HIRST, Gavin, Charles ,  WILLSON, Timothy, Mark ,  SHERRILL, Ronald, George ,  SUGG, Elizabeth, Ellen ,  SZEWCZYK, Jerzy, Ryszard

    Inventor： GLAXO WELLCOME INC.

    IPC: C07K05/062

    CPC classification number: C07D223/16 ,  A61K38/00 ,  C07D243/14 ,  C07D403/06 ,  C07D403/12 ,  C07K5/0222 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/06104 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0821

    Abstract: A CCK-A agonist of the general formula (I) R R NCOCH2N(R )COR and physiologically acceptable salts thereof wherein, R is independently C3-6alkyl, C3-6cycloalkyl, C3-6alkenyl, phenyl, -(CH2)pCN or -(CH2)pCOO(C1-4alkyl) and R is independently C3-6alkyl, C3-6cycloalkyl, C3-6alkenyl, benzyl, phenyl or phenyl mono- or disubstituted independently with C1-3alkyl, cyano, hydroxy, dimethylamino, -O(C1-4alkyl), -O(CH2C6H5), -NH(C1-4alkyl), -COO(C1-4alkyl), -N(C1-4alkyl)2 pyrrolidino, morpholino, halogen or C1-3alkyl substituted by one or more fluorine atoms or R is C1-2alkyl and R is phenyl substituted at the 2- or 4-position with chloro, methyl, methoxy or methoxycarbonyl; or R and R together with the nitrogen atom to which they are attached represent the group of formula (II), wherein R is hydrogen or methyl, R represents hydrogen, hydroxy, fluoro dimethylamino, C1-4alkoxy or benzyloxy, and m is zero, 1 or 2; R represents a group selected from C1-6alkyl; phenyl or phenyl substituted by one or two groups independently selected from C1-3alkyl, C1-4alkoxy or halogen; or thiophenyl; R is a group of formula (III) or (IV).

    Abstract translation: 通式（I）R 1 R 2 NCOCH 2 N（R 3）COR 4的CCK-A激动剂及其生理学上可接受的盐，其中R 1独立地为C 3-6烷基， C 1-6烯基，苯基， - （CH 2）pCN或 - （CH 2）p COO（C 1-4烷基）和R 2独立地是C 3-6烷基，C 3-6环烷基，C 3-6烯基，苄基， 氰基，羟基，二甲基氨基，-O（C 1-4烷基）， - O（CH 2 C 6 H 5），-NH（C 1-4烷基），-COO（C 1-4烷基）， - N（C 1-4烷基） ）2吡咯烷子基，吗啉代，卤素或被一个或多个氟原子取代的C 1-3烷基或R 1是C 1-2烷基，R 2是在2-或4-位被氯，甲基，甲氧基或 甲氧羰基; 或R 1和R 2与它们所连接的氮原子一起代表式（II）的基团，其中R 7是氢或甲基，R 8表示氢，羟基，氟二甲基氨基 ，C 1-4烷氧基或苄氧基，m为0,1或2; R 3表示选自C 1-6烷基的基团; 苯基或被一个或两个独立地选自C 1-3烷基，C 1-4烷氧基或卤素的基团取代的苯基; 或噻吩基; R 4是式（III）或（IV）的基团。

    PEPTIDYL COMPOUNDS AND THEIR THERAPEUTIC USE AS INHIBITORS OF METALLOPROTEINASES
    10.
    发明申请
    PEPTIDYL COMPOUNDS AND THEIR THERAPEUTIC USE AS INHIBITORS OF METALLOPROTEINASES 审中-公开
    肽类化合物及其治疗用途作为金属蛋白酶抑制剂

    公开(公告)号：WO1995013289A1

    公开(公告)日：1995-05-18

    申请号：PCT/GB1994002471

    申请日：1994-11-10

    Applicant: CHIROSCIENCE LIMITED ,  MONTANA, John ,  DICKENS, Jonathon ,  OWEN, David, Alan ,  BAXTER, Andrew, Douglas

    Inventor： CHIROSCIENCE LIMITED

    IPC: C07K05/062

    CPC classification number: C07K5/0606 ,  A61K38/00 ,  C07K5/06043 ,  Y02A50/411 ,  Y10S530/868

    Abstract: A compound of formula (I), wherein R is C1-6 alkyl, C2-6 alkenyl, aryl, (C1-6 alkyl)aryl or C1-6 alkyl-AR where A is O, NR or S(O)m, where m = 0-2, and the or each R is H, C1-4 alkyl, aryl or (C1-4 alkyl)aryl; R is H or C1-6 alkyl; either R is H or C1-6 alkyl optionally substituted by amino (NH2), arylamino, protected amino, aryl, di(C1-6 alkyl)amino, mono(C1-6 alkyl)amino, CO2H, protected carboxyl, carbamoyl, mono(C1-6 alkyl)carbamoyl or di(C1-6 alkyl)carbamoyl, and R is H or C1-6 alkyl, or NR4R5 is pyrrolidino, piperidino or morpholino; R is optionally-substituted C3-6 cycloalkyl, C3-6 cycloalkenyl, C1-6 alkyl, benzyl, (C1-6 alkoxy)benzyl, benzyloxybenzyl or 3-indolylmethyl; Alk is C1-6 alkyl or C2-6 alkenyl and n = 0 or 1; R is H or R CO where R is C1-4 alkyl, (C1-4 alkyl)aryl, C3-6 cycloalkyl, (C3-6 cycloalkyl)C1-4 alkyl, C2-6 alkenyl or (C2-6 alkenyl)aryl; and R is H, C1-4 alkyl, (C1-4 alkyl)aryl or aryl; or a salt, solvate or hydrate thereof. Such compounds may be used to treat conditions associated with metalloproteinase, TNF and/or other activity.

    Abstract translation: 式（I）化合物，其中R 1为C 1-6烷基，C 2-6烯基，芳基，（C 1-6烷基）芳基或C 1-6烷基-Ar 9，其中A为O， 9或S（O）m，其中m = 0-2，并且每个R 9是H，C 1-4烷基，芳基或（C 1-4烷基）芳基; R 2是H或C 1-6烷基; R 4是H或任选被氨基（NH 2），芳基氨基，保护的氨基，芳基，二（C 1-6烷基）氨基，单（C 1-6烷基）氨基，CO 2 H，被保护的羧基取代的C 1-6烷基， 氨基甲酰基，单（C 1-6烷基）氨基甲酰基或二（C 1-6烷基）氨基甲酰基，R 5为H或C 1-6烷基，或NR 4 R 5为吡咯烷子基，哌啶子基或吗啉代; R 6是任选取代的C 3-6环烷基，C 3-6环烯基，C 1-6烷基，苄基，（C 1-6烷氧基）苄基，苄氧基苄基或3-吲哚甲基; Alk是C 1-6烷基或C 2-6烯基，n = 0或1; R 7是H或R 10 CO，其中R 10是C 1-4烷基，（C 1-4烷基）芳基，C 3-6环烷基，（C 3-6环烷基）C 1-4烷基，C 2-6 烯基或（C 2-6烯基）芳基; 和R 8是H，C 1-4烷基，（C 1-4烷基）芳基或芳基; 或其盐，溶剂合物或水合物。 这些化合物可用于治疗与金属蛋白酶，TNF和/或其他活性相关的病症。

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