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1. 发明申请

WO1996000238A1 T CELL EPITOPES OF RYE GRASS POLLEN ALLERGEN 审中-公开
标题翻译： RYE GRASS POLLEN ALLERGEN的T细胞抗原
公开(公告)号：WO1996000238A1
公开(公告)日：1996-01-04
申请号：PCT/GB1995001493
申请日：1995-06-26
申请人： PEPTIDE THERAPEUTICS LIMITED , LEWIN, Ian, Victor , BUNGY, Ali, Gholam
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K07/06
CPC分类号： C07K14/415 , A61K38/00 , C07K2319/00
摘要： The present invention relates to the immunodominant T cell epitope of rye grass, its minimal sequence, its role in hayfever and its use in the manufacture of a medicament for the treatment or prophylaxis of hayfever. According to the present invention there is provided a polypeptide of nine amino acid residues including the six amino acid residues VXRIDT, and analogues and mimetics thereof. The polypeptide can be administered to provide a method for treatment or prophylaxis of allergies particularly of rye grass allergy or hayfever.
摘要翻译：本发明涉及黑麦草的免疫显性T细胞表位，其最小序列，其在干草中的作用及其在制备用于治疗或预防干草的药物中的用途。根据本发明，提供了包含六个氨基酸残基VXRIDT的九个氨基酸残基的多肽及其类似物和模拟物。可以施用多肽以提供治疗或预防特别是黑麦草过敏或过敏的过敏的方法。

2. 发明申请

WO1996006357A1 SCREEN FOR POTENTIAL THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：潜在治疗化合物的筛选
公开(公告)号：WO1996006357A1
公开(公告)日：1996-02-29
申请号：PCT/GB1995001912
申请日：1995-08-14
申请人： PEPTIDE THERAPEUTICS LIMITED , STANWORTH, Denis, Raymond , LEWIN, Ian, Victor , MAMAN, Sarita , JONES, Valerie
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： G01N33/68
CPC分类号： C07K16/4291 , G01N33/6854 , G01N2500/00
摘要： The present invention provides a screen which utilises a direct biochemical interaction between moieties to determine whether or not a potential therapeutic compound (PTC) may be useful as a drug. It will be particularly useful in combinatorial approaches to drug design and testing. The screen of the invention allows determination of the binding ability of a PTC with the three amino acid motif of a decapeptide within the C epsilon 4 region of IgE, or a similar amino acid motif. Any such binding should be indicative of a potential therapeutic effect. The screen comprises: (i) a binding compound which includes a recognition site and a binding site having the sequence of amino acid residues Xaa1-Xaa2-Xaa3; and (ii) a mono or polyclonal wholly, semi- or non-synthetic antibody or fragment thereof (A1) which is able to bind selectively to the binding site; wherein Xaa1 and Xaa3 are the same or different positively charged amino acid residues such as Lys, Arg or His, preferably Lys or Arg, most preferably Lys; and Xaa2 is any other amino acid residue, preferably a neutrally charged amino acid residue, more preferably Thr, Pro, Gly or Ala, most preferably Thr.
摘要翻译：本发明提供一种利用部分之间的直接生物化学相互作用来确定潜在的治疗化合物（PTC）是否可用作药物的筛选。在药物设计和测试的组合方法中将特别有用。本发明的筛选允许确定PTC与IgE的Cε4区域内的十肽的三个氨基酸基序或相似的氨基酸基序的结合能力。任何此类结合应指示潜在的治疗效果。筛选包括：（i）包含识别位点和具有氨基酸残基Xaa1-Xaa2-Xaa3序列的结合位点的结合化合物; 和（ii）能够选择性结合结合位点的单克隆或多克隆全抗体或非合成抗体或其片段（A1）; 其中Xaa1和Xaa3是相同或不同的带正电荷的氨基酸残基，例如Lys，Arg或His，优选Lys或Arg，最优选Lys; 并且Xaa2是任何其它氨基酸残基，优选中性带电荷的氨基酸残基，更优选Thr，Pro，Gly或Ala，最优选Thr。

3. 发明申请

WO1995010532A1 COMPOUNDS USEFUL IN ANTI-ALLERGY TREATMENT 审中-公开
标题翻译：化合物用于抗过敏治疗
公开(公告)号：WO1995010532A1
公开(公告)日：1995-04-20
申请号：PCT/GB1994002230
申请日：1994-10-11
申请人： PEPTIDE THERAPEUTICS LIMITED , LEWIN, Ian, Victor , STANWORTH, Denis, Raymond
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K05/093
CPC分类号： C07K7/06 , A61K38/00 , C07K5/0819 , C07K5/1021
摘要： Pharmaceutically acceptable compounds of less than 1200 MW for use in the treatment of IgE-mediated allergies comprising a first negatively charged atom or group and a second negatively charged atom or group, separated by a spacing group effective conformationally to position said negatively charged atoms or groups so that they will neutralize the lysine residues of the amino acid sequence Lys Thr Lys at positions 497-499 of the C ELEMENT 4 constant domain of cell-bound human IgE, but excluding any compounds already known for this purpose such as DSCG and nedocromil sodium and toxic compounds. In a second aspect, the present invention provides peptides of formula (I) (in which the left-hand side represents the N-terminus and the right-hand side the C terminus): R m Xaa Sp Xaa R n wherein: R represents a residue of an amino acid or of a sequence of two or three amino acids, which may be the same or different; R represents a residue of an amino acid or of a sequence of two or three amino acids, which may be the same or different; (but preferably any amino acid residue of R or R adjacent to an Xaa residue is neither positively nor negatively charged); Xaa represents a residue of a negatively charged amino acid, preferably Glu; Sp represents a spacing residue, preferably of a non-charged amino acid, preferably Pro, or of a non-charged dipeptide, which provides the spacing required for the negatively charged groups of the Xaa residues to be sufficiently proximal to the lysine residues of the amino acid sequence Lys Thr Lys at positions 497-499 of the C ELEMENT 4 constant domain of cell-bound human IgE to neutralise them; Xaa represents a residue of a negatively charged amino acid, preferably Glu; and m and n denote the number of amino acids in R and R respectively and each of m and n independently is 0, 1, 2 or 3, and the sum of m plus n is from 0 to 3; and their terminal functional derivatives; both per se and for use in the treatment of IgE-mediated allergies.
摘要翻译：用于治疗IgE介导的过敏症的小于1200MW的药学上可接受的化合物，其包含第一带负电荷的原子或第二带负电荷的原子或基团，所述原子或基团由间隔基团分隔，所述间隔基团有效构造所述带负电荷的原子或基团使得它们将中和细胞结合人IgE的C ELEMENT 4恒定结构域的位置497-499处的氨基酸序列Lys Thr Lys的赖氨酸残基，但不包括已知为此目的的任何化合物，例如DSCG和奈多罗米钠和有毒化合物。在第二方面，本发明提供式（I）的肽（其中左侧表示C末端的N末端和右侧）：R 1 m Xaa 1 Sp Xaa R 2 n其中：R 1表示氨基酸的残基或两个或三个氨基酸的序列，其可以相同或不同; R 2表示氨基酸的残基或两个或三个氨基酸的序列，其可以相同或不同; （但优选与Xaa残基相邻的R 1或R 2的任何氨基酸残基既不是正的也不是带负电荷的）; Xaa 1表示带负电荷的氨基酸的残基，优选为Glu; Sp表示间隔残基，优选非带电荷的氨基酸，优选Pro或非带电二肽，其提供Xaa残基的带负电荷基团足够接近赖氨酸残基所需的间隔氨基酸序列Lys Thr Lys位于细胞结合人IgE的C ELEMENT 4恒定区的第497-499位，以中和它们; Xaa 2表示带负电荷的氨基酸的残基，优选为Glu; m和n分别表示R 1和R 2中的氨基酸数，m和n各自独立地为0,1,2或3，m + n的和为0〜3。及其末端功能衍生物; 本身也用于治疗IgE介导的过敏。

4. 发明申请

WO1996014333A1 PEPTIDES FOR ANTI-ALLERGY TREATMENT 审中-公开
标题翻译：用于抗过敏治疗的肽
公开(公告)号：WO1996014333A1
公开(公告)日：1996-05-17
申请号：PCT/GB1995002580
申请日：1995-11-03
申请人： PEPTIDE THERAPEUTICS LIMITED , STANWORTH, Denis, Raymond , LEWIN, Ian, Victor
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00 , A61K39/00 , C07K7/08
摘要： Peptides of the above-mentioned sequence wherein Xaa is any amino acid residue, but most preferably Val or Ile, and their simple derivatives, including those chain-extended at the N-terminus or C-terminus, are useful in anti-allergy treatment.
摘要翻译：上述序列的肽，其中Xaa是任何氨基酸残基，但最优选Val或Ile，及其简单衍生物，包括在N末端或C末端扩链的那些，可用于抗过敏治疗。

5. 发明申请

WO1998017628A2 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：WO1998017628A2
公开(公告)日：1998-04-30
申请号：PCT/GB1997002914
申请日：1997-10-22
申请人： PEPTIDE THERAPEUTICS LIMITED , JOHNSON, Tony , QUIBELL, Martin
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07C231/10
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 R or R 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; R2 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.
摘要翻译：用于固相合成式（1）化合物的方法，其中R 1或R 2中的任一个或两个可以由方案（4）表示的方法组合可变，其中：X为（a），（b），（c）或（d）; Y是H或侧链官能团保护部分如Fmoc; R2 1是R2的中间形式，随后化学转化得到所需的R2; 并且n为2至12，优选为4.本发明还提供式（1）化合物的化合物和组合文库，以及用于该方法的中间体化合物。

6. 发明申请

WO1996005852A1 TREATMENT OF INFLAMMATORY DISEASES OF THE GASTRO-INTESTINAL TRACT 审中-公开
标题翻译：治疗胃肠疾病的炎症性疾病
公开(公告)号：WO1996005852A1
公开(公告)日：1996-02-29
申请号：PCT/GB1995001913
申请日：1995-08-14
申请人： PEPTIDE THERAPEUTICS LIMITED , STANWORTH, Denis, Raymond
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： A61K38/04
CPC分类号： A61K38/04 , A61K38/57 , C07K16/42
摘要： The present invention provides use of a peptide or ligand in the manufacture of a medicament for the treatment of certain inflammatory diseases of the gastro-intestinal tract, such as coeliac disease, Crohn's disease, ulcerative colitis etc., and a method of treatment of the diseases comprising administering an effective dose of a medicament comprising the peptide or ligand. The peptide has not more than 20 amino acid residues, and comprises a thiol-active cysteine residue and at least two positively charged amino acid residues situated at, adjacent or near to the N terminus or at, adjacent or near to the C terminus or at, adjacent or near to both termini; or this peptide and a pharmaceutically acceptable diluent or carrier. Preferably the peptide or analog comprises amino acid residues having a sequence selected from the group which comprises: Cys-Lys-Lys, His-Cys-Lys-Lys (SEQ ID NO:1). Also, the invention can provide a method of treatment of IDGIT comprising administering an effective dose of a peptide or analogue thereof having general formula (I) wherein m is 0 or 1, n is 0 or 1 and m + n is 1 or 2; J and J represent sequences of positively charged amino acid residues; Z , Z , B and B represent sequences of residues of positively charged, negatively charged or neutral amino acid residues or sequences of any mixture of positively charged, negatively charged or neutral amino acid residues; x = 0 or 1, y = 0 or 1, and x + y = 1 or 2; c = 0 to 4, d = 0 to 4; and a = 0 to 18 and b = 0 to 18 with the proviso that when m = 0 at least one of B and Z is a positively charged amino acid residue and when n is 0 at least one of B and Z is a positively charged amino acid residue, and when m = n = 1 and y is 0 at least one of Z , B , B and Z is a positively charged amino acid residue and when m = n = 1 and x = 0 at least one of Z , B , B and Z is a positively charged amino acid residue: B and B may also represent a non-peptide spacer arm of a length equivalent to that determined by the length of b and c residues of amino acids.
摘要翻译：本发明提供肽或配体在制备用于治疗胃肠道某些炎性疾病如乳糜泻，克罗恩病，溃疡性结肠炎等的药物中的用途，以及治疗疾病包括施用有效剂量的包含肽或配体的药物。肽具有不超过20个氨基酸残基，并且包含硫醇活性半胱氨酸残基和至少两个带正电荷的氨基酸残基，位于，邻近或接近N末端或在C末端附近或附近，或位于，邻近或接近两个终点; 或该肽和药学上可接受的稀释剂或载体。优选地，肽或类似物包含具有选自以下的序列的氨基酸残基：Cys-Lys-Lys，His-Cys-Lys-Lys（SEQ ID NO：1）。此外，本发明可以提供治疗IDGIT的方法，包括给予有效剂量的通式（I）的肽或其类似物，其中m为0或1，n为0或1，m + n为1或2; J 1和J 2代表带正电荷的氨基酸残基的序列; Z 1，Z 2，B 1和B 2表示带正电荷，带负电荷或中性氨基酸残基或任何带正电荷，带负电荷或中性氨基酸残基混合物的序列的序列 ; x = 0或1，y = 0或1，x + y = 1或2; c = 0〜4，d = 0〜4; 和a = 0至18且b = 0至18，条件是当m = 0时，B 2和Z 2中的至少一个为带正电荷的氨基酸残基，当n为0时，B中的至少一个为 Z 1和Z 1是带正电荷的氨基酸残基，当m = n = 1且y为0时，Z 1，B 1，B 2和Z 2中的至少一个为1，是带正电荷的氨基酸残基，当m = n = 1且x = 0时，Z 1，B 1，B 2和Z 2中的至少一个是带正电荷的氨基酸残基：B ＆lt; 1＆gt;和B＆lt; 2＆gt;也可以表示长度等于由氨基酸的b和c残基的长度确定的长度的非肽间隔臂。

7. 发明申请

WO1996005231A1 PEPTIDES AND ANTIBODIES AND THEIR USE IN TREATMENT OF CARCINOMAS 审中-公开
标题翻译：肽和抗体及其在治疗癌症中的应用
公开(公告)号：WO1996005231A1
公开(公告)日：1996-02-22
申请号：PCT/GB1995001893
申请日：1995-08-10
申请人： PEPTIDE THERAPEUTICS LIMITED , STANWORTH, Denis, Raymond , JONES, Valerie
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K16/42
CPC分类号： C07K16/4291 , A61K38/00
摘要： The invention provides for the use of immunoactive peptides (antigens) for active immunisation to produce antibodies which prevent "triggering" of histamine release by mast cell degranulation and consequently inhibit carcinoma proliferation. The invention also provides for the use of antibodies for passive immunisation, which antibodies prevent "triggering" of histamine release by mast cell degranulation and consequently inhibit carcinoma proliferation. The invention provides use of an immunogen comprising a covalent conjugate of a residue of a histamine-releasing peptide having a cationic N terminus and a hydrophobic C terminus, together with a residue capable of eliciting antibodies against this peptide in the manufacture of a medicament for the treatment of carcinomas, especially mammary adenocarcinomas. Preferably, the residue of a histamine-releasing peptide has the sequence Lys-Thr-Lys-Gly-Ser-Gly-Phe-Phe-Val-Phe (SEQ ID NO:1).
摘要翻译：本发明提供了用于主动免疫的免疫活性肽（抗原）用于产生抗体的抗体，所述抗体通过肥大细胞脱颗粒“阻止”组胺释放并因此抑制癌细胞增殖。本发明还提供了用于被动免疫的抗体的用途，所述抗体通过肥大细胞脱颗粒阻止“触发”组胺释放，从而抑制癌细胞增殖。本发明提供了包含具有阳离子N末端和疏水性C末端的组胺释放肽的残基的共价缀合物的免疫原的用途，以及能够引发针对该肽的抗体的残基在制备用于治疗癌症，特别是乳腺癌。优选地，组胺释放肽的残基具有序列Lys-Thr-Lys-Gly-Ser-Gly-Phe-Phe-Val-Phe（SEQ ID NO：1）。

8. 发明申请

WO1997046582A1 MENINGOCOCCAL VACCINE 审中-公开
公开(公告)号：WO1997046582A1
公开(公告)日：1997-12-11
申请号：PCT/GB1997001518
申请日：1997-06-05
申请人： PEPTIDE THERAPEUTICS LIMITED , LAING, Peter , DARSLEY, Michael , TIGHE, Patrick, Jason
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K14/22
CPC分类号： C07K7/06 , A61K38/00 , C07K7/08 , C07K14/22
摘要： The present invention relates to an anti-meningococcal vaccine, particularly for group-B serotype meningococcus. The invention provides antigenic peptide ligands which can act as an immunogen capable of eliciting an immune response to produce antibodies against the capsular polysaccharide of group-B meningococci (CPS-B).
摘要翻译：本发明涉及抗脑膜炎球菌疫苗，特别是涉及B组血清型脑膜炎球菌的抗脑膜炎球菌疫苗。本发明提供可作为能够引发免疫应答以产生针对B组脑膜炎球菌（CPS-B）的荚膜多糖的抗体的免疫原的抗原肽配体。

9. 发明申请

WO1997042216A1 AUTO-DECONVOLUTING COMBINATORIAL LIBRARIES 审中-公开
标题翻译：自动解除组合图书馆
公开(公告)号：WO1997042216A1
公开(公告)日：1997-11-13
申请号：PCT/GB1997001158
申请日：1997-04-24
申请人： PEPTIDE THERAPEUTICS LIMITED , QUIBELL, Martin , JOHNSON, Tony , HART, Terance
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K01/04
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 apparatus and methods which provide the rapid generation of structure/activity relationships using auto-deconvoluting combinatorial libraries, which facilitate the invention of novel active compounds. The invention provides apparatus and methods which can be used for the rapid generation of structure/activity relationship (SAR) data, and, therefore, the characterisation of the active motif of any group of compounds. The invention provides libraries of compounds which interact with an active moiety, and apparatus and methods to identify such compounds. The active moieties may be (but are not limited to) enzymes, receptors, antibodies, etc. The interaction of the active moiety with the compounds of the library may be (but is not limited to) the interaction of a substrate or inhibitor with an enzyme, the interaction of a ligand with a receptor, the interaction of an antigen or antigenic epitope with an antibody, etc.
摘要翻译：本发明涉及使用自动去卷积组合库快速产生结构/活性关系的装置和方法领域，其促进了新型活性化合物的发明。本发明提供了可用于快速产生结构/活性关系（SAR）数据的装置和方法，并因此用于表征任何一组化合物的活性基序。本发明提供了与活性部分相互作用的化合物文库，以及鉴定这些化合物的装置和方法。活性部分可以是（但不限于）酶，受体，抗体等。活性部分与文库化合物的相互作用可以是（但不限于）底物或抑制剂与酶，配体与受体的相互作用，抗原或抗原表位与抗体的相互作用等

10. 发明申请

WO1998003543A1 IDENTIFICATION OF SHORT PEPTIDE SEQUENCES REPRESENTING EPITOPES OF GLYCOPROTEIN G OF HSV-2 USING A PHAGE PEPTIDE DISPLAY LIBRARY 审中-公开
标题翻译：鉴定使用噬菌体肽显示库的HSV-2糖蛋白G的表位序列
公开(公告)号：WO1998003543A1
公开(公告)日：1998-01-29
申请号：PCT/GB1997001990
申请日：1997-07-24
申请人： PEPTIDE THERAPEUTICS LIMITED , GRABOWSKA, Anna, Marie , IRVING, William, Lucien , LAING, Peter
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K14/035
CPC分类号： C40B40/02 , A61K38/00 , A61K39/00 , C07K14/005 , C07K2319/00 , C12N15/1037 , C12N2710/16622 , G01N33/56994 , G01N33/6878 , G01N2333/035
摘要： The invention provides a polypeptide consisting of 3 to 38 amino acid residues, having the sequence of SEG ID:1 or a portion thereof; and analogous polypeptide derivatives by virtue of point mutation, amino acid substitution, deletion or addition; SEQ ID:1 = A PPP PE H R GGPEEF EGAGDG EPP EDDDSATGLAFRTPN wherein the sequence includes histidine residue H ; and wherein E may be substituted in order of preference by D > T ; and wherein R may be substituted by A ; which sequence is recognised by anti-gG2 positive human sera from patients with HSV-2 infection and is not recognised by anti-gG2 negative sera from patients with HSV-1 infection; and antibodies raised thereto; and prophylactic and therapeutic and diagnostic uses thereof relating to HSV-2 infection.
摘要翻译：本发明提供了由3至38个氨基酸残基组成的具有SEG ID：1序列或其部分的多肽; 和通过点突变，氨基酸取代，缺失或添加的类似的多肽衍生物; SEQ ID：1 = A 1 PPP 4 PE 6 H 7 R GGPEEF 14 EGAGDG 20 EPD 23 EDDDSATGLAFRTPN 38其中该序列包括组氨酸残基H <7 >; 并且其中E 6可以以D 6的优先顺序被取代; 并且其中R 8可以被A 8取代; 该序列由具有HSV-2感染的患者的抗gG2阳性人血清识别，并且未被患有HSV-1感染的患者的抗gG2阴性血清识别; 和抗体; 以及与HSV-2感染相关的预防和治疗和诊断用途。

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