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1. 发明申请

WO9817628A3 A SOLID-PHASE TECHNOLOGY FOR THE PREPARATION OF AMIDES 审中-公开
标题翻译：一种用于制备AMIDES的固相技术
公开(公告)号：WO9817628A3
公开(公告)日：1998-09-03
申请号：PCT/GB9702914
申请日：1997-10-22
申请人： PEPTIDE THERAPEUTICS LTD , JOHNSON TONY , QUIBELL MARTIN
发明人： JOHNSON TONY , QUIBELL MARTIN
IPC分类号： C07D241/08 , C07B61/00 , C07C47/565 , C07C51/367 , C07C59/74 , C07C59/92 , C07C69/712 , C07C231/02 , C07C231/10 , C07C233/00 , C07K1/04 , C07K1/06 , C08F8/30 , C07C59/125 , C07C69/708 , C07K1/00
CPC分类号： C07C59/74 , C07C69/712 , C07C231/10 , C07K1/045 , C07K1/047
摘要： A method for the solid phase synthesis of compounds of formula (1), in which either or both of R1 or R2 are combinatorially variable by a process represented by scheme (4) and wherein: X is (a), (b), (c) or (d); Y is H or a side chain functional group protective moiety such as Fmoc; R21 is an intermediate form of R2 which is subsequently chemically transformed to give the desired R2; and n is between 2 and 12, preferably 4. The invention also provides compounds and combinatorial libraries of compounds of formula (1), as well as intermediate compounds for use in the method.

2. 发明申请

WO9854209A3 HUMAN MAFA 审中-公开
标题翻译：人力资源
公开(公告)号：WO9854209A3
公开(公告)日：1999-03-11
申请号：PCT/GB9801572
申请日：1998-05-29
申请人： PEPTIDE THERAPEUTICS LTD , HEWITT ELLEN LOUISE , LAMERS MARIA BARDINA ANTONIA C , LAMONT ALAN , WILLIAMS DAVID HUGH
发明人： HEWITT ELLEN LOUISE , LAMERS MARIA BARDINA ANTONIA C , LAMONT ALAN , WILLIAMS DAVID HUGH
IPC分类号： A61K38/00 , C07K14/47 , C07K14/705 , C07K16/28 , C07K7/00
CPC分类号： C07K16/2851 , A61K38/00 , C07K14/4726 , C07K14/705 , C07K14/7056
摘要： This invention relates to polypeptides, nucleotide sequences, antibodies or fragments thereof, ligands and compositions and their use in the medical fields of inflammation and allergy, disease examples of which include rheumatoid arthritis and asthma. In addition the invention relates to a method for production of the polypeptides. Methods of disease treatment are suggested relying on agents developed in combination with the cloning of the human MAFA molecule. A use of the invention addresses the prevention of cell activation events in vivo which could lead to therapies for the prevention of tumour growth.

3. 发明申请

WO9923109A3 A METHOD FOR MAPPING THE ACTIVE SITES BOUND BY ENZYMES THAT COVALENTLY MODIFY SUBSTRATE MOLECULES 审中-公开
标题翻译：一种通过酶促共价修饰底物分子来定位有活性位点的方法
公开(公告)号：WO9923109A3
公开(公告)日：1999-07-08
申请号：PCT/GB9803259
申请日：1998-10-30
申请人： PEPTIDE THERAPEUTICS LTD , CLARK JONATHAN , LAMONT ALAN , WILLIAMS DAVID
发明人： CLARK JONATHAN , LAMONT ALAN , WILLIAMS DAVID
IPC分类号： C12Q1/48 , A61K38/00 , A61K38/55 , A61K45/00 , A61P43/00 , C07B61/00 , C07K1/04 , C12Q1/42 , A61K38/08 , G01N33/68
CPC分类号： C07K1/047 , A61K38/00
摘要： This invention provides for the active site mapping of enzymes which catalyse covalent modification including, but not limited to phosphorylation, acylation, dephosphorylation in which a fixed residue (known as the catalytic residue) such as a tyrosine, serine, threonine, histidine, aspartic acid residue or any other residue containing an appropriate side chain is modified. Mapping of protein kinases is exemplified. The method of the invention has an additional level of complexity over and above that of the self-deconvoluting libraries described in WO97/42216. This involves making a library of smaller libraries (referred to as subsets) where a fixed residue is moved stepwise through the sequence of amino acids or other groups (such as peptidomimetics). Using 5 subsets of libraries of peptides of 5 amino acids allows the mapping of a sequence of 9 amino acids. In general one could carry out the invention using n subsets of n-mer peptides so as to provide mapping data for the residues from -(n-1) to +(n-1) either side of the active site. Thus in general the length of the mapped sequence would be (2n)-1. In this invention there is no need to separate modified from unmodified sequences because of the self deconvoluting nature of the library. The assay screen produces a series of hits, the patterns of which reveal the unique sequences in each well. This enables a pattern of substrate preferences to be determined for any enzyme. The unique sequences obtained using this invention can be used to provide substrates for high throughput assays and provide detailed information about the active site to aid rational drug design. This invention can also be used as an inhibitor library to screen against known modifying enzymes where a known substrate exists and can be set up in an assay format.
摘要翻译：本发明提供催化共价修饰的酶的活性位点作图，包括但不限于磷酸化，酰化，去磷酸化，其中固定的残基（称为催化残基）如酪氨酸，丝氨酸，苏氨酸，组氨酸，天冬氨酸残基或含有适当侧链的任何其他残基被修饰。蛋白激酶的图谱是示例性的。本发明的方法比WO97 / 42216中描述的自去卷积文库具有更高的复杂程度。这涉及制作一个较小的文库（称为亚组）的库，其中固定的残基逐步移动通过氨基酸或其他基团（例如肽模拟物）的序列。使用5个氨基酸的肽库的5个亚组允许绘制9个氨基酸的序列。通常可以使用n个n聚体肽亚组来实施本发明，从而为从活性位点两侧的 - （n-1）至+（n-1）的残基提供映射数据。因此，通常映射序列的长度将是（2n）-1。在本发明中，由于文库的自去卷积性质，不需要将修饰与未修饰的序列分开。化验屏幕产生一系列命中，其中的模式显示每个孔中的独特序列。这使得可以为任何酶确定底物偏好的模式。使用本发明获得的独特序列可以用于提供用于高通量测定的底物并且提供关于活性位点的详细信息以帮助合理的药物设计。本发明也可以用作抑制剂文库筛选已知的修饰酶，其中已知的底物存在并且可以以测定形式建立。

4. 发明申请

WO9740065A3 SUBSTRATES AND INHIBITORS OF PROTEOLYTIC ENZYMES 审中-公开
标题翻译：蛋白酶基质和抑制剂
公开(公告)号：WO9740065A3
公开(公告)日：1997-12-04
申请号：PCT/GB9701157
申请日：1997-04-24
申请人： PEPTIDE THERAPEUTICS LTD , QUIBELL MARTIN , JOHNSON TONY , HART TERANCE
发明人： QUIBELL MARTIN , JOHNSON TONY , HART TERANCE
IPC分类号： C12N9/99 , B01J19/00 , C07K1/04 , C07K5/06 , C07K7/02 , C07K7/06 , C40B30/04 , C40B60/14 , G01N33/15 , G01N33/53 , G01N33/566 , G01N33/68
CPC分类号： C07K7/06 , B01J19/0046 , B01J2219/00315 , B01J2219/00504 , B01J2219/0072 , C07K1/047 , C07K5/06043 , C07K5/06191 , C07K7/02 , C40B60/14 , G01N33/68
摘要： The present invention relates to the field of compounds which are substrates or inhibitors of proteolytic enzymes and to apparatus and methods for identifying substrates or inhibitors for proteolytic enzymes. We have devised a combinatorial method for the rapid identification of binding motifs which will greatly expedite the synthesis of inhibitors of a variety of proteolytic enzymes such as aspartyl proteases, serine proteases, metallo proteases and cysteinyl proteases.

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