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31. 发明申请

WO1998025949A1 SUBSTITUTED 5-AMINO-1,3,4-THIADIAZOLE-2-THIONES 审中-公开
标题翻译：取代的5-氨基-1,3,4-噻二唑-2-基
公开(公告)号：WO1998025949A1
公开(公告)日：1998-06-18
申请号：PCT/US1997022534
申请日：1997-12-09
申请人： PROSCRIPT, INC. , OLEKSYSZYN, Jozef , JACOBSON, Alan, R.
发明人： PROSCRIPT, INC.
IPC分类号： C07K05/08
CPC分类号： C07K5/06139 , A61K31/433 , A61K31/4725 , A61K31/58 , A61K38/00 , C07K5/06078 , C07K5/06165
摘要： The use of N5-substituted 5-amino-1,3,4-thiadiazole-2-thiols as metalloproteinases to inhibit matrix metalloproteinase enzymes and cartilage degradation is disclosed. Methods of treating diseases caused by over-activity of matrix metalloproteinases, such as osteoarthritis and rheumatoid arthritis, are also disclosed.
摘要翻译：公开了使用N5-取代的5-氨基-1,3,4-噻二唑-2-硫醇作为金属蛋白酶抑制基质金属蛋白酶和软骨降解。还公开了治疗由基质金属蛋白酶如骨关节炎和类风湿性关节炎过度活动引起的疾病的方法。

32. 发明申请

WO1998020024A1 LIGANDS FOR PHOSPHATASE BINDING ASSAY 审中-公开
标题翻译：用于磷酸酶结合测定的配体
公开(公告)号：WO1998020024A1
公开(公告)日：1998-05-14
申请号：PCT/CA1997000824
申请日：1997-11-03
申请人： MERCK FROSST CANADA INC. , DESMARAIS, Sylvie , FRIESEN, Richard , ZAMBONI, Robert
发明人： MERCK FROSST CANADA INC.
IPC分类号： C07K05/08
CPC分类号： C07K5/0827
摘要： Disclosed are new ligands for use in a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, -SH (or -S ), in the cysteine, which then adversely affects the binding ability of the enzyme. Specifically disclosed is an assay for tyrosine phosphatases and cysteine proteases, including capsases and cathepsins, e.g., Cathepsin K(O2), utilizing scintillation proximity assay (SPA) technology. The assay has important applications in the discovery of compounds for the treatment and study of, for example, diabetes, immunosuppression, cancer, Alzheimer's disease and osteoporosis. The novel feature of the use of a mutant enzyme can be extended to its use in a wide variety of conventional colorimetric, photometric, spectrophotometric, radioimmunoassay and ligand-binding competitive assays.
摘要翻译：公开了用于蛋白酶和磷酸酶的结合测定的新配体，其在其结合位点含有半胱氨酸或作为酶结合的必需结构组分。半胱氨酸的巯基是酶的机理蛋白水解和水解性质中的亲核基团。该测定法可用于测定新的未知配体和化合物的混合物与酶竞争性结合的能力，与酶的已知结合剂，例如已知的酶抑制剂。通过使用天然或天然野生型酶的突变形式，其中丝氨酸或另一种氨基酸例如丙氨酸取代半胱氨酸，克服了测定程序中来自外来氧化和烷化剂的干扰问题。干扰是由于半胱氨酸中巯基-SH（或-S - ）的氧化或烷基化而产生的，其然后不利地影响酶的结合能力。具体公开的是利用闪烁亲近测定（SPA）技术测定酪氨酸磷酸酶和半胱氨酸蛋白酶，包括热囊酶和组织蛋白酶，例如组织蛋白酶K（O 2）。该测定在发现用于治疗和研究例如糖尿病，免疫抑制，癌症，阿尔茨海默氏病和骨质疏松症的化合物中具有重要应用。使用突变酶的新颖特征可以扩展到其用于各种常规比色，光度，分光光度，放射免疫测定和配体结合竞争性测定中。

33. 发明申请

WO1995028420A1 METHIONINE SULFONE AND S-SUBSTITUTED CYSTEINE SULFONE DERIVATIVES AS ENZYME INHIBITORS 审中-公开
标题翻译：甲硫氨酸和S-取代的CYSTEINE SULFONE衍生物作为酶抑制剂
公开(公告)号：WO1995028420A1
公开(公告)日：1995-10-26
申请号：PCT/US1995004954
申请日：1995-04-18
申请人： CORVAS INTERNATIONAL, INC. , ABELMAN, Matthew, M. , ARDECKY, Robert, John , NUTT, Ruth, Foelsche
发明人： CORVAS INTERNATIONAL, INC.
IPC分类号： C07K05/08
CPC分类号： C07K5/0606 , A61K38/00
摘要： This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
摘要翻译：本发明涉及抑制凝血酶或因子Xa的化合物。该化合物含有醛官能团和甲硫氨酸砜或S-取代的半胱氨酸砜残基。化合物及其药物组合物可用于预防怀疑具有以异常血栓形成为特征的病症的哺乳动物的血栓形成。

34. 发明申请

WO1995027729A1 OPIATE RECEPTOR LIGANDS 审中-公开
标题翻译：优良的受体配体
公开(公告)号：WO1995027729A1
公开(公告)日：1995-10-19
申请号：PCT/US1995004679
申请日：1995-04-11
申请人： CHIRON CORPORATION
发明人： CHIRON CORPORATION , SPELLMEYER, David, C. , MOOS, Walter, H. , MARTIN, Eric, J. , ZUCKERMANN, Ronald, N. , STAUBER, Gregory , SHOEMAKER, Kevin, R. , GOFF, Dane
IPC分类号： C07K05/08
CPC分类号： C07K5/0806 , A61K38/00
摘要： Compounds of formula (1) bind opioid receptors wherein X and Y are each independently (2).
摘要翻译：式（1）的化合物结合阿片受体，其中X和Y各自独立地（2）。

35. 发明申请

WO1993011153A1 PEPTIDES AND ANTIBODIES FOR TREATMENT OF RHEUMATOID ARTHRITIS 审中-公开
标题翻译：用于治疗炎症性角膜炎的肽和抗体
公开(公告)号：WO1993011153A1
公开(公告)日：1993-06-10
申请号：PCT/GB1992002174
申请日：1992-11-25
申请人： BRITISH TECHNOLOGY GROUP LTD. , KIRBY, Julian , LEWIN, Ian, Victor , NAYYAR, Sarita , STANWORTH, Denis, Raymond
发明人： BRITISH TECHNOLOGY GROUP LTD.
IPC分类号： C07K05/08
CPC分类号： C07K14/8125 , C07K16/38 , C07K16/42
摘要： A synthetic peptide of not more than 20 amino acid residues or analogue thereof comprising a thiol-active cysteine residue and at least two positively charged amino acid residues situated on (but not necessarily adjacent to) the N-terminal side, on (but not necessarily adjacent to) the C-terminal side or on (but not necessarily adjacent to) both the N- and C-terminal sides of the thiol active cysteine for use in therapy.

36. 发明申请

WO1993005069A1 NEW ISOSTERIC PEPTIDES 审中-公开
标题翻译：新的异位肽
公开(公告)号：WO1993005069A1
公开(公告)日：1993-03-18
申请号：PCT/SE1992000584
申请日：1992-08-25
申请人： AKTIEBOLAGET ASTRA
发明人： AKTIEBOLAGET ASTRA , ATRASH, Butrus , JONES, David, Michael , SZELKE, Michael
IPC分类号： C07K05/08
CPC分类号： C07K5/06078 , A61K38/00 , Y10S514/822
摘要： The invention relates to new competitive inhibitors of thrombin, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as anticoagulants for prophylaxis and treatment of thromboembolic diseases, according to formula (1), wherein A represents -CH2-, -CH=CH-, -CH2-CH2- or -CH2-CH2-CH2-; Y represents O or S(O)p, where p is 0, 1 or 2; R?1, R2, R3, R3A, R4¿ and m are defined as in the claims, either as such or in the form of a physiologically acceptable salt and including stereoisomers.

37. 发明申请

WO1992022570A1 INHIBITORS OF PICORNAVIRUS PROTEASES 审中-公开
标题翻译： PICORNAVIRUS蛋白抑制剂
公开(公告)号：WO1992022570A1
公开(公告)日：1992-12-23
申请号：PCT/US1992005167
申请日：1992-06-12
申请人： CHIRON CORPORATION
发明人： CHIRON CORPORATION , MALCOLM, Bruce , YANG, Chi, Ching
IPC分类号： C07K05/08
CPC分类号： C07K7/06 , C07K5/0808 , C07K14/005 , C12N2770/32022
摘要： Compounds of formula (I) inhibit the proteolytic activity of picornaviral proteases, and are thus effective antiviral agents. In formula (I) R1 is -OR3 or -NR3R4, where R3 is lower alkyl, hydroxy, lower alkoxy, or aryl-lower alkyl, and R4 is H or lower alkyl; R2 is H or lower acyl; n is an integer from 2 to 40 inclusive; X is an anchor group selected from the group consisting of -CHO, -C=N, -COCH2F, -COCH2Cl, -COCH2N2, -CH=N-NHC(=S)NH2 or -COCOR5 where R5 is lower alkyl, lower alkoxy, lower aryl, aryl-lower alkyl or aryl-lower alkoxy; and aa indicates an amino acid; wherein (aa)n is an amino acid sequence recognized specifically by said selected protease.
摘要翻译：式（I）化合物抑制微小RNA病毒蛋白酶的蛋白水解活性，因此是有效的抗病毒剂。在式（I）中，R 1是-OR 3或-NR 3 R 4，其中R 3是低级烷基，羟基，低级烷氧基或芳基 - 低级烷基，R 4是H或低级烷基; R2是H或低级酰基; n为2〜40的整数， X是选自-CHO，-C = N，-COCH2F，-COCH2Cl，-COCH2N2，-CH = N-NHC（= S）NH2或-COCOR5的锚定基团，其中R5是低级烷基，低级烷氧基，低级芳基，芳基 - 低级烷基或芳基 - 低级烷氧基; 和aa表示氨基酸; 其中（aa）n是所述选择的蛋白酶特异性识别的氨基酸序列。

38. 发明申请

WO1992004371A1 KININOGENASE INHIBITORS 审中-公开
标题翻译：基因抑制剂
公开(公告)号：WO1992004371A1
公开(公告)日：1992-03-19
申请号：PCT/GB1991001479
申请日：1991-09-02
申请人： FERRING PEPTIDE RESEARCH PARTNERSHIP KB , SZELKE, Michael , EVANS, David, Michael , JONES, David, Michael
发明人： FERRING PEPTIDE RESEARCH PARTNERSHIP KB
IPC分类号： C07K05/08
CPC分类号： C07K5/02 , C07K5/0227
摘要： Kininogenase inhibitors, optimally not exceeding the size of a hexapeptide, represented by (II), wherein A and B = amino acyl (including amino acyl analogue) the same or different forming a dipeptide group the amino acid of A carrying a terminal group and being any amino or imino-acid residue (but preferably of D-configuration) and of B being a lipophilic amino-acid residue of D- or L-configuration but not proline or a proline analogue, or a conformational analogue of said dipeptide group wherein the peptide link is replaced by -CH2-NH- ('reduced'), -CH(OH)-CH2- ('hydroxy'), -CO-CH2 ('keto'), -CH2-CH2- ('hydrocarbon') or other conformational mimic of the peptide bond and in (III) the side chain R is that of a basic amino acid or amino acid analogue (preferably of L-configuration), and R is H or lower alkyl(C1-C4) or C or the peptide link comprising -N(R)- is replaced leading to a conformational mimic as above; Y = a binding enhancing or carbonyl activating group preferably selected from H (when A or B must be cyclohexylalanine, preferably D if at A or L if at B) or alkyl (C1-C20) or fluoroalkyl (C2-C12); substituted oxymethylene; thiomethylene; sulphoxymethylene; sulphonylmethylene; aminomethylene; hydrazino-methylene; -CH2-Het (where Het = a substituted or unsubstituted heterocycle); substituted amino (but when the resulting compound is a secondary alkylamide B must not be phenylalanine); an amino-acid group or its ester or amide; a carboxylic secondary amide or primary amide, when B must be cyclohexylalanine or adamantylalanine or other bulky lipophilic, non-aromatic amino-acid (not Ala Leu Ile Val Nva Met Nle Phe Tyr Trp Nal (1)); tertiary-carboxamide; carboxy-alkyl group or its ester or amide or amino acyl derivative.
摘要翻译：激肽原酶抑制剂最好不超过由（II）表示的六肽的大小，其中A和B =氨基酰基（包括氨基酰基类似物）相同或不同，形成携带末端基团的A的氨基酸的二肽基团任何氨基或亚氨基酸残基（但优选D构型）和B是D-或L-构型的亲脂性氨基酸残基，但不是脯氨酸或脯氨酸类似物或所述二肽基团的构象类似物，其中肽链连接被-CH 2 -NH-（“还原”），-CH（OH）-CH 2 - （'羟基'），-CO-CH 2（'酮基），-CH 2 -CH 2 - （“烃基” 或其它构型模拟物，并且在（III）中，侧链R 1是碱性氨基酸或氨基酸类似物（优选L-构型）的那些，并且R是H或低级烷基（C1-C4 ）或Cα或包含-N（R） - 的肽连接被取代，导致如上所述的构象模拟物; Y =优选选自H的结合增强或羰基活化基团（当A或B必须为环己基丙氨酸时，优选D，如果在A或L，如果在B）或烷基（C 1 -C 20）或氟代烷基（C 2 -C 12）; 取代的甲醛; 硫代亚甲基; sulphoxymethylene; sulphonylmethylene; 氨基亚甲基; 肼基的亚甲基; -CH 2 -Het（其中Het =取代或未取代的杂环）; 取代的氨基（但当所得化合物为仲烷基酰胺B时，不得为苯丙氨酸）; 氨基酸基或其酯或酰胺; 当B必须为环己基丙氨酸或金刚烷基丙氨酸或其它大体积的亲脂性非芳族氨基酸（不是Ala Leu Ile Val Nva Met Nle Phe Tyr Trp Nal（1））时，羧基仲酰胺或伯酰胺; 叔酰胺; 羧基 - 烷基或其酯或酰胺或氨基酰基衍生物。

39. 发明申请

WO1991018011A1 INHIBITION OF CELL ADHESION USING INTERCELLULAR ADHESION MOLECULE-1-LIKE PEPTIDES AND/OR ANALOGUES THEREOF 审中-公开
标题翻译：使用细胞粘附分子-1型肽和/或其模拟物抑制细胞粘附
公开(公告)号：WO1991018011A1
公开(公告)日：1991-11-28
申请号：PCT/AU1991000205
申请日：1991-05-14
申请人： SWINBURNE LIMITED , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL ... , THE CALIFORNIA INSTITUTE OF TECHNOLOGY , FECONDO, John, Vincent , BOYD, Andrew, Wallace , KENT, Stephen, Brian, Henry
发明人： SWINBURNE LIMITED , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL ... , THE CALIFORNIA INSTITUTE OF TECHNOLOGY
IPC分类号： C07K05/08
CPC分类号： C07K16/2803 , A61K38/00 , C07K14/70525 , Y02A50/473
摘要： The present invention is directed to Intercellular Adhesion Molecule-1-like peptides, analogues thereof and antibodies thereto, to pharmaceutical compositions comprising same and the use thereof to inhibit or reduce cell adhesion in mammals. The present invention also relates to a method for fingerprinting the functional domain of a polypeptide or protein.
摘要翻译：本发明涉及包含其的药物组合物的细胞间粘附分子-1样肽，其类似物和其抗体，以及其用于抑制或降低哺乳动物细胞粘附的用途。本发明还涉及用于指纹多肽或蛋白质的功能结构域的方法。

40. 发明申请

WO1991012268A1 NOVEL PEPTIDE SUBSTRATES, METHOD OF PREPARATION AND USE IN C PROTEIN DETERMINATION 审中-公开
标题翻译：新肽基质，制备和使用C蛋白质测定方法
公开(公告)号：WO1991012268A1
公开(公告)日：1991-08-22
申请号：PCT/FR1990000973
申请日：1990-12-31
申请人： SERBIO , QUENTIN, Gérard , MARTINOLI, Jean-Luc
发明人： SERBIO
IPC分类号： C07K05/08
CPC分类号： C07K5/0821 , C12Q1/56 , C12Q2337/12 , G01N2333/96461 , Y02P20/55
摘要： Peptide compounds, as novel industrial products, chosen from the series consisting of (i) tripeptides having the formula: Y-A1-A2-A3-R in which Y represents H or a suitable group blocking the N-terminated end, A1 represents an amino-acid group chosen from the series consisting of the groups (2-oxo-thiazolidin-4-yl)carbonyl (THC), (2-oxo-tetrahydro-1,3-thiazin-5-yl)carbonyl (TZC), thiazolidine-4-carbonyl (ATC) and tetrahydro-1,3-thiazin-5-yl)carbonyl (AZC), A2 represents an amino-acid group chosen from the series comprising the groups Pro, 3Hyp and 4Hyp where the 3Hyp and 4Hyp OH lateral group is capable of being protected by a protecting ether or ester group, A3 represents an amino-acid group chosen from the series comprising the groups Arg and Lys and R represents a labelling means; and (ii) their addition salts. These novel compounds are useful as substrates for C protein determination.

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