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1. 发明申请

WO2010089115A8 MULTISPECIFIC PEPTIDES 审中-公开
标题翻译：多功能肽
公开(公告)号：WO2010089115A8
公开(公告)日：2011-12-22
申请号：PCT/EP2010000689
申请日：2010-02-04
申请人： MEDICAL RES COUNCIL , WINTER GREGORY PAUL , HEINIS CHRISTIAN , BERNARD ELISE , LOAKES DAVID , TITE JOHN PAUL , VAYSBURD MARINA , TEUFEL DANIEL PAUL , RIECHMANN LUTZ
发明人： WINTER GREGORY PAUL , HEINIS CHRISTIAN , BERNARD ELISE , LOAKES DAVID , TITE JOHN PAUL , VAYSBURD MARINA , TEUFEL DANIEL PAUL , RIECHMANN LUTZ
IPC分类号： A61K47/48 , G01N33/68
CPC分类号： C12N15/1037 , A61K47/55 , A61K47/64 , A61K47/643 , C07K14/001 , C12N15/1044 , C12N15/1058 , C40B40/08 , C40B40/10 , C40B50/06 , G01N33/531
摘要： The invention relates to a method for providing a multispecific peptide ligand comprising a polypeptide covalently linked to a molecular scaffold at three or more amino acid residues and capable of binding to two or more separate targets, comprising the steps of: (a) providing a first repertoire of polypeptides, each polypeptide comprising two or more reactive groups capable of covalent linkage to a molecular scaffold, and at least one loop which comprises a sequence of two or more amino acids subtended between two of said reactive groups; (b) providing a second repertoire of polypeptides as described in (a); (c) joining at least one loop of one or more members of the first repertoire to at least one loop of one or more members of the second repertoire to form at least one polypeptide comprising two loops, and (d) conjugating the composite polypeptide(s) to a molecular scaffold at at least three amino acid positions.
摘要翻译：本发明涉及一种提供多特异性肽配体的方法，所述多特异性肽配体包含在三个或更多个氨基酸残基处共价连接到分子支架并能够结合两个或更多个单独靶标的多肽，包括以下步骤：（a）提供第一多肽的所有组成部分，每个多肽包含两个或更多个能够与分子支架共价连接的反应性基团，以及至少一个环，其包含两个或更多个氨基酸的序列，对应于两个所述反应性基团; （b）提供如（a）所述的第二组多肽; （c）将第一组合物中的一个或多个成员的至少一个环连接到第二组合物的一个或多个成员的至少一个环，以形成至少一个包含两个环的多肽，和（d）将复合多肽（ s）至少在三个氨基酸位置分子支架。

2. 发明申请

WO2011018227A3 PEPTIDE LIBRARIES 审中-公开
标题翻译：肽库
公开(公告)号：WO2011018227A3
公开(公告)日：2011-04-07
申请号：PCT/EP2010004948
申请日：2010-08-12
申请人： MEDICAL RES COUNCIL , WINTER PAUL GREGORY , HEINIS CHRISTIAN , BERNARD ELISE , LOAKES DAVID , TEUFEL DANIEL PAUL
发明人： WINTER PAUL GREGORY , HEINIS CHRISTIAN , BERNARD ELISE , LOAKES DAVID , TEUFEL DANIEL PAUL
IPC分类号： C12N15/10 , A61K47/00 , A61K47/48 , C12N15/00 , C40B40/02 , G01N33/00 , G01N33/68
CPC分类号： C12N15/1037 , C07K1/00 , C07K1/042 , C07K1/113 , C07K2318/00
摘要： The invention relates to a method for altering the conformational diversity of a first repertoire of polypeptide ligands, comprising a plurality of polypeptides comprising at least two reactive groups separated by a loop sequence covalently linked to a molecular scaffold which forms covalent bonds with said reactive groups, to produce a second repertoire of polypeptide ligands, comprising assembling said second repertoire from the polypeptides and structural scaffold of said first repertoire, incorporating one of the following alterations: (a) altering at least one reactive group; or (b) altering the nature of the molecular scaffold; or (c) altering the bond between at least one reactive group and the molecular scaffold; or (d) any combination of (a), (b) or (c).
摘要翻译：本发明涉及用于改变多肽配体的第一组库的构象多样性的方法，所述方法包括多个多肽，所述多肽包含至少两个反应基团，所述反应基团通过共价连接至与所述反应基团形成共价键的分子支架的环状序列分开，以产生第二多肽配体库，包括从所述第一库所的多肽和结构支架组装所述第二库，并入以下改变之一：（a）改变至少一个反应基团; 或（b）改变分子支架的性质; 或（c）改变至少一个反应性基团与分子支架之间的键; 或（d）（a），（b）或（c）的任何组合。

3. 发明申请

WO03039450A2 IMPROVEMENTS IN OR RELATING TO INHIBITION OF VIRUSES 审中-公开
标题翻译：改善或相关于病毒的抑制
公开(公告)号：WO03039450A2
公开(公告)日：2003-05-15
申请号：PCT/GB0205031
申请日：2002-11-07
申请人： MEDICAL RES COUNCIL , LOAKES DAVID , BROWN DANIEL , BALZARINI JAN , MORIYAMA KEI , NEGISHI KAZUO , CAMERON CRAIG , ARNOLD JAMIE , CASTRO CHRISTIAN , KORNEEVA VICTORIA , GRACI JASON
发明人： LOAKES DAVID , BROWN DANIEL , BALZARINI JAN , MORIYAMA KEI , NEGISHI KAZUO , CAMERON CRAIG , ARNOLD JAMIE , CASTRO CHRISTIAN , KORNEEVA VICTORIA , GRACI JASON
IPC分类号： C07H19/067 , A01N43/90 , A61K31/519 , A61K31/52 , A61K31/675 , A61K31/7068 , A61K31/7076 , A61P31/14 , C07H19/16 , C07H19/167 , A61K
CPC分类号： C07H19/16
摘要： Disclosed is a pharmaceutical composition comprising a ribonucleoside analogue in accordance with general formula (I) or (II) as herein defined , in admixture with a physiologically acceptable excipient diluent or carrier.
摘要翻译：公开了包含根据本文定义的通式（I）或（II）的核糖核苷类似物与生理上可接受的赋形剂稀释剂或载体的混合物的药物组合物。

4. 发明申请

WO2007135380A3 ANTIPARASITIC COMPOUNDS AND COMPOSITIONS 审中-公开
标题翻译：抗微生物化合物和组合物
公开(公告)号：WO2007135380A3
公开(公告)日：2008-07-31
申请号：PCT/GB2007001820
申请日：2007-05-17
申请人： MEDICAL RES COUNCIL , LOAKES DAVID , TOO KATHLEEN
发明人： LOAKES DAVID , TOO KATHLEEN
IPC分类号： C07D473/16 , A61K31/404 , A61K31/416 , A61K31/52 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P33/02 , A61P33/06 , C07D209/04 , C07D231/56 , C07D473/30 , C07H19/02 , C07H19/052 , C07H19/16
CPC分类号： A61K31/404 , A61K31/416 , A61K31/52 , A61K31/7052 , A61K31/7076 , A61K31/708 , C07D209/40 , C07D209/42 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/30 , C07D473/34 , C07D487/04
摘要： Disclosed is use of a compound having a structure according to general formula (I) defined below, in the manufacture of a medicament to treat and/or prevent a parasitic infection or infestation in a mammalian subject wherein X 1 = N or CH or C=O (X 2 = NH) or C=S (X 2 = NH) or C-OR 1 or C-halogen or C-azide; X 2 = N or CR 1 or C-halogen or CS(O) n R 1 where n = 0-2 or a (C) m linker where m = 1-3 between X 2 and X 6 or C-X 5 X 6 (in which case X 5 X 6 at C6 (purine numbering) is replaced by H or NHR 1 or O or OR 1 or S or SR 1 ); X 3 = N or CH or C-NO 2 ; X 4 = N or CH or C-NO 2 or C-NR 1 R 2 or an amidine derivative or a guanidinium derivative; X 5 = O or NR 1 or CR 1 R 2 ; X 6 = OR 1 or O-acyl or 0-S(O) n R 1 or NR 1 R 2 or NH-acyl or N(Acyl) 2 or NH-OS(O) 2 R 1 or NH-S(O) n R 1 where n = 0-2 or a hydrazone derivative or an oxime derivative, but if X 5 = O, X 6 cannot = O or X 5 X 6 is an amidine or an N-substituted pyridine or substituted guanidine; Y = H or NH 2 or NR 1 R 2 or -O (X 3 = NH) or OR 1 or F or Cl or Br or I or CR 1 R 2 R 3 or S(O) n R 1 where n = 0-2 or azide or X 5 X 6 (in which case X 5 X 6 at C6 (purine numbering) is replaced by H or NHR 1 or O or OR 1 or S or SR 1 ); R 1 , R 2 , R 3 are independently selected from the group consisting of H or (optionally substituted), alkyl, alkenyl or alkynyl or aryl or aralkyl where the substituents may be selected from H, OH, NH 2 , halogen, N 3 , CN, CHO, COOR', C0NR' 2 , OR, NE' 2 , SR', NR'NR' 2 , NR'OR', NO 2 and R' is alkyl, alkenyl, alkynyl, aralkyl, acyl, sulfonyl; Z = H or substituted (alkyl or alkenyl or alkynyl or aralkyl) or a sugar derivative of general formula (II) in the ß-configuration where: B is the nucleobase from Formula (I); X 7 = CH 2 or O or NR 1 or S; R 4 = H or OH or OR 1 or halogen or azide or a phosphate derivative; R 5 = H or F or CH 3 ; R 6 = H or OH or OR 1 or halogen or azide or a phosphate derivative; and R 7 = H or halogen or R 1 or a derivative of an amino acid or PO 3 H 2 or P 2 O 6 H 3 or P 3 O 9 H 4 or a methylene derivative of P 2 O 6 H 3 or P 3 O 9 H 4 or a masked phosphate or a phosphonate derivative (5'-O replaced with CH 2 ).
摘要翻译：本发明公开了具有下述通式（I）结构的化合物在制备用于治疗和/或预防哺乳动物受试者的寄生虫感染或侵染的药物中的用途，其中X < = N或CH或C = O（X 2 N = NH）或C = S（X 2 N = NH）或C-OR 1 或C-卤素或C-叠氮化物; X 2 = N或CR 1或C - 卤素或CS（O）n R 1 R 1其中n = 0-2或其中在X 2和X 6或CX 5之间的m = 1-3的（C）m < （在这种情况下）C6（嘌呤编号）的X 5 X 6取代为H或NHR 1 或O或OR 1或S或SR 1）; X 3 = N或CH或C-NO 2; X 4 = N或CH或C-NO 2或C-NR 1 R 2或脒衍生物或胍衍生物; X 5 = O或NR 1或CR 1 R 2 2; 或者O - 酰基或0-S（O）n R 1或NR 1，或者NH-酰基或N（酰基）2或NH-OS（O）2 R 2，其中n = 0-2或腙衍生物或肟衍生物，但如果X C6（嘌呤编号）的5个X 6位被H或NHR 1或O或OR 1取代，或S或 SR _{1 ）; R 1，R 2，R 3，R 3独立地选自H或（任选取代的），烷基，烯基或炔基或芳基或芳烷基，其中取代基可以选自H，OH，NH 2，卤素，N 3，CN，CHO，COOR'，C0NR' / SUB，OR，NE'2，SR'，NR'NR'2，NR'OR'，NO 2和R' 烷基，烯基，炔基，芳烷基，酰基，磺酰基; Z = H或通式（II）的取代的（烷基或烯基或炔基或芳烷基）或糖衍生物，其中：B是式（I）的核碱基; X 7或CH 2或O或NR 1或S; R 4 = H或OH或OR 1或卤素或叠氮化物或磷酸酯衍生物; R 5 = H或F或CH 3; R 6 = H或OH或OR 1或卤素或叠氮化物或磷酸酯衍生物; 和R 7 = H或卤素或R 1或氨基酸或PO 3 H 2的衍生物，或者P 2 3 3或3 3 > 4 或者P 2 O 3 H 3或S 3 O 3的亚甲基衍生物，或者掩蔽的磷酸盐或膦酸盐衍生物（5'-O被CH 2取代）。}

5. 发明申请

WO9906422A3 BASE ANALOGUES 审中-公开
标题翻译：基础模拟
公开(公告)号：WO9906422A3
公开(公告)日：1999-06-03
申请号：PCT/GB9802306
申请日：1998-07-31
申请人： NYCOMED AMERSHAM PLC , SIMMONDS ADRIAN , HAMILTON ALAN , SMITH CLIFFORD , LOAKES DAVID , BROWN DANIEL , HILL FERGAL , KUMAR SHIV , NAMPALLI SATYAM , MCDOUGALL MARK
发明人： SIMMONDS ADRIAN , HAMILTON ALAN , SMITH CLIFFORD , LOAKES DAVID , BROWN DANIEL , HILL FERGAL , KUMAR SHIV , NAMPALLI SATYAM , MCDOUGALL MARK
IPC分类号： G01N33/532 , A61K31/7042 , A61K31/7072 , A61P31/12 , C07H19/00 , C07H21/00 , C12Q1/68 , G01N33/53 , C07H19/06
CPC分类号： G01N33/5308 , C07H21/00
摘要： Nucleoside analogues or base analogues having structure (I), where X = O or NH or S, Y = N or CHR or CR , W = N or NR or CHR or CR or S, n = 1 or 2; each R is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR where R is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.
摘要翻译：具有结构（I）的核苷类似物或碱基类似物，其中X = O或NH或S，Y = N或CHR 6或CR 6，W = N或NR 6或CHR 6或CR < 6>或S，n = 1或2; 每个R 6独立地是H或O或烷基或链烯基或烷氧基或芳基或报道部分; 必要时（即当Y和/或W为N或CR 6而R 6不为O时），Y与W或W与W之间存在双键，Q为H或糖或糖类似物或核酸骨架或骨架类似物。

6. 发明专利

CA2750969C STRUCTURED PEPTIDE PROCESSING 未知
公开(公告)号：CA2750969C
公开(公告)日：2019-05-07
申请号：CA2750969
申请日：2010-02-04
申请人： MEDICAL RES COUNCIL
发明人： WINTER GREGORY PAUL , HEINIS CHRISTIAN , BERNARD ELISE , LOAKES DAVID , VAYSBURD MARINA
IPC分类号： C40B40/10 , C12N15/00 , C12P21/06 , C12Q1/37 , C40B30/04 , C40B40/02 , G01N33/68
摘要： The invention relates to a method for modifying one or more peptide ligands, comprising polypeptides covalently linked to a molecular scaffold at two or more amino acid residues, comprising the steps of providing one or more peptide ligands, wherein the polypeptide comprises two or more reactive groups which form a covalent linkage to the molecular scaffold, and at least one loop which comprises a sequence of two or more amino acids subtended between two of said reactive groups; exposing the peptide ligands to one or more proteases; and sorting the ligands according to the extent of proteolytic cleavage.

7. 发明专利

CA2770240C METHODS FOR INCREASING DIVERSITY IN A LIBRARY OF POLYPEPTIDE LIGANDS 未知
公开(公告)号：CA2770240C
公开(公告)日：2018-01-16
申请号：CA2770240
申请日：2010-08-12
申请人： MEDICAL RES COUNCIL
发明人： WINTER PAUL GREGORY , HEINIS CHRISTIAN , BERNARD ELISE , LOAKES DAVID , TEUFEL DANIEL PAUL
IPC分类号： C07K14/435 , A61K47/00 , C12N15/00 , C40B40/02 , G01N33/00 , G01N33/68
摘要： The invention relates to a method for altering the conformational diversity of a first repertoire of polypeptide ligands, comprising a plurality of polypeptides comprising at least two reactive groups separated by a loop sequence covalently linked to a molecular scaffold which forms covalent bonds with said reactive groups, to produce a second repertoire of polypeptide ligands, comprising assembling said second repertoire from the polypeptides and structural scaffold of said first repertoire, incorporating one of the following alterations: (a) altering at least one reactive group; or (b) altering the nature of the molecular scaffold; or (c) altering the bond between at least one reactive group and the molecular scaffold; or (d) any combination of (a), (b) or (c).

8. 发明专利

SG173460A1 MULTISPECIFIC PEPTIDES 未知
公开(公告)号：SG173460A1
公开(公告)日：2011-09-29
申请号：SG2011054400
申请日：2010-02-04
申请人： MEDICAL RES COUNCIL
发明人： WINTER GREGORY PAUL , HEINIS CHRISTIAN , BERNARD ELISE , LOAKES DAVID , TITE JOHN PAUL , VAYSBURD MARINA , TEUFEL DANIEL PAUL
摘要： The invention relates to a method for providing a multispecific peptide ligand comprising a polypeptide covalently linked to a molecular scaffold at three or more amino acid residues and capable of binding to two or more separate targets, comprising the steps of: (a) providing a first repertoire of polypeptides, each polypeptide comprising two or more reactive groups capable of covalent linkage to a molecular scaffold, and at least one loop which comprises a sequence of two or more amino acids subtended between two of said reactive groups; (b) providing a second repertoire of polypeptides as described in (a); (c) joining at least one loop of one or more members of the first repertoire to at least one loop of one or more members of the second repertoire to form at least one polypeptide comprising two loops, and (d) conjugating the composite polypeptide(s) to a molecular scaffold at at least three amino acid positions.

9. 发明专利

SG173169A1 STRUCTURED PEPTIDE PROCESSING 未知
公开(公告)号：SG173169A1
公开(公告)日：2011-09-29
申请号：SG2011054392
申请日：2010-02-04
申请人： MEDICAL RES COUNCIL
发明人： WINTER PAUL GREGORY , HEINIS CHRISTIAN , BERNARD ELISE , LOAKES DAVID , VAYSBURD MARINA
摘要： The invention relates to a method for modifying one or more peptide ligands, comprising polypeptides covalently linked to a molecular scaffold at two or more amino acid residues, comprising the steps of providing one or more peptide ligands, wherein the polypeptide comprises two or more reactive groups which form a covalent linkage to the molecular scaffold, and at least one loop which comprises a sequence of two or more amino acids subtended between two of said reactive groups; exposing the peptide ligands to one or more proteases; and sorting the ligands according to the extent of proteolytic cleavage.

10. 发明专利

AT339434T 未知
公开(公告)号：AT339434T
公开(公告)日：2006-10-15
申请号：AT01947617
申请日：2001-06-29
申请人： MEDICAL RES COUNCIL
发明人： KUMAR SHIV , MCDOUGALL MARK , NAMPALLI SATYAM , NEAGU CONSTANTIN , LOAKES DAVID , BROWN DAN
IPC分类号： C12N15/09 , A61K31/7064 , A61P31/12 , C07D487/04 , C07F9/09 , C07F9/6561 , C07H19/23 , C07H21/04 , C12P19/40 , C12Q1/68 , G01N33/58 , C07H21/00 , G01N33/53 , A61K31/706
摘要： The present invention describes novel compounds of the formulaWherein Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue, Y=O, S, NR , where R is H, alkyl alkenyl, alkynyl, X is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl or a combination thereof or, preferably, a reporter group. The novel compounds are suitable for incorporation in oligonucleotides and polynucleotides.

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