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公开(公告)号：EP0753065B1
公开(公告)日：2003-05-14
申请号：EP95913225.9
申请日：1995-03-28
CPC分类号： C07K16/465 , A61K38/00 , C07K16/2854 , C07K2317/24 , C07K2319/00
摘要： This invention relates to whole antibodies of neutral isotype having specificity for E-selectin, process for their preparation (using vectors), pharmaceutical compositions containing them, and their use in therapy (e.g. for inflammatory disorders) and diagnosis. Said antibodies are variants of natural antibodies altered in the Fc region, especially in the CH2 domain, so that the interactions with antibodies Fc receptors and complement are absent or very low.
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2.发明授权
公开(公告)号：EP0862560B1
公开(公告)日：2003-04-02
申请号：EP96939171.3
申请日：1996-11-20
发明人： DAVIS, Peter David , MOFFAT, David Festus Charles , DAVIS, Jeremy Martin , HUTCHINGS, Martin Clive
IPC分类号： C07D239/42 , C07D239/48 , C07D401/04 , C07D417/04 , C07D409/04 , A61K31/505
CPC分类号： C07D401/04 , C07D239/42 , C07D239/48 , C07D417/04
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公开(公告)号：EP1173569A1
公开(公告)日：2002-01-23
申请号：EP00927406.9
申请日：2000-04-17
IPC分类号： C12N15/12 , C07K14/705 , C12N15/62 , A61K38/17
CPC分类号： C07K14/705 , A61K38/00 , C07K2319/00
摘要： The invention relates to synthetic signalling molecules, which are based on sequences derived from primary signalling motifs such as immunoglobulin tyrosine receptor-based activation motifs (ITAMs). The use of such signalling molecules within chimeric receptor proteins allows one to tailor the level of intracellular signalling mediated by the chimeric receptor. Proteins containing, and nucleic acids encoding, such synthetic signalling molecules suitable for use in medicine, are described.
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公开(公告)号：EP1160255A1
公开(公告)日：2001-12-05
申请号：EP01203352.8
申请日：1997-12-10
IPC分类号： C07K16/00
CPC分类号： C07K16/00 , A61K47/68 , A61K2039/505 , C07K16/22 , C07K16/241 , C07K16/3007 , C07K2317/55
摘要： Monovalent antibody fragments are described, each of which has one or more polymer molecules site - specifically attached through a sulphur atom of a cysteine residue located outside of the variable region domain of the antibody. The polymers include synthetic or naturally occurring polymers such as polyalkylene, polyalkenylenes, polyoxyalkylenes or polysaccharides. Each fragment may be attached to one or more effector or reporter molecules, and is of use in therapy or diagnostics where it has markedly improved binding and/or pharmacokinetic properties when compared to other antibody fragments which have the same number and type of polymer molecules, but in which the polymer molecules are randomly attached.
摘要翻译： 描述了单价抗体片段，其各自具有一个或多个聚合物分子，其位点特异性地通过位于抗体的可变区结构域外的半胱氨酸残基的硫原子连接。 聚合物包括合成或天然存在的聚合物，例如聚亚烷基，聚烯烃，聚氧化烯或多糖。 每个片段可以连接到一个或多个效应物或报告分子上，并且在治疗或诊断中有用，其中与具有相同数量和类型的聚合物分子的其它抗体片段相比，其显着改善了结合和/或药代动力学性质， 但其中聚合物分子是随机连接的。
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5.发明授权TRISUBSTITUTED PHENYL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS AND PROCESSES FOR THEIR PREPARATION 失效DREISUBSTITUIRTE PHENYLDERIVATE ALS PHOSPHODIESTERASEHEMMER UND VERFAHREN ZUR IHRE HERSTELLUNG
公开(公告)号：EP0640065B1
公开(公告)日：2001-10-17
申请号：EP94908454.5
申请日：1994-03-09
IPC分类号： C07C43/235 , A01N43/40 , C07D213/30 , C07D237/08 , C07D241/12 , A01N43/48
CPC分类号： C07D213/30 , C07C255/37 , C07C2601/08 , C07D213/73 , C07D237/08 , C07D241/12
摘要： Compounds of general formula (1) are described wherein Y is a halogen atom or a group -OR1, where R1 is an optionally substituted alkyl group; X is -O-, -S- or -N(R7)-, where R7 is a hydrogen atom or an alkyl group; R2 is an optionally substituted cycloalkyl or cycloalkenyl group; R?3 and R4¿, which may be the same or different, is each a hydrogen atom or an alkyl, -CO¿2R?8 (where R8 is a hydrogen atom or an alkyl, aryl, or aralkyl group), -CONR9R10 (where R?9 and R10¿ which may be the same or different is each a hydrogen atom or an alkyl, aryl or aralkyl group), -CSNR9R10, -CN, -CH¿2?CN group; Z is -(CH2)n- (where n is zero or an integer 1, 2 or 3; R?5¿ is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R6 is a hydrogen atom or a hydroxyl group; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
摘要翻译： 描述通式（1）的化合物，其中Y是卤素原子或-OR 1基团，其中R 1是任选取代的烷基; X是-O - ， - S-或-N（R 7） - ，其中R 7是氢原子或烷基; R2是任选取代的环烷基或环烯基; R 3和R 4可以相同或不同，分别为氢原子或烷基-CO 2 R 8（其中R 8为氢原子或烷基，芳基或芳烷基），-CONR 9 R 10（其中R 9和R 10可以 各自为氢原子或烷基，芳基或芳烷基），-CSNR 9 R 10，-CN，-CH 2 CN基团; Z是 - （CH 2）n - （其中n是0或整数1,2或3; R 5是任选地含有一个或多个选自氧，硫或氮原子的杂原子的任选取代的单环或双环芳基; R 6是 氢原子或羟基;以及其盐，溶剂合物，水合物，前药和N-氧化物。根据本发明的化合物是有效和选择性的磷酸二酯酶IV型抑制剂，并且可用于预防和治疗诸如哮喘的疾病，其中 存在不需要的炎性反应或肌肉痉挛。
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6.发明公开THIOCARBOXAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF ALPHA-4 INTEGRINS 审中-公开THIOCARBOXAMIDDERIVATIVE及其作为ALPHA-4整联蛋白抑制剂
公开(公告)号：EP1066271A1
公开(公告)日：2001-01-10
申请号：EP99942586.1
申请日：1999-03-24
发明人： Archibald, Sarah Catherine , HEAD, John Clifford , WARRELLOW, Graham John , PORTER, John Robert
IPC分类号： C07D277/06 , A61K31/425
CPC分类号： C07D277/06 , Y10S977/904
摘要： Compounds of formula (1), wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R?2 and R3¿, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group -(CH¿2)tR?7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (-CO¿2?H) or a derivative thereof; and the salts, solvates and hydrates thereof are described. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
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7.发明公开PEPTIDE SEQUENCES AS HINGE REGIONS IN PROTEINS LIKE IMMUNOGLOBULIN FRAGMENTS AND THEIR USE IN MEDICINE 有权肽序列，如蛋白铰链区的免疫球蛋白片段和它们在医学
公开(公告)号：EP1015495A2
公开(公告)日：2000-07-05
申请号：EP98944070.6
申请日：1998-09-21
IPC分类号： C07K16/00
CPC分类号： C07K7/08 , C07K16/3007 , C07K2317/14 , C07K2317/24 , C07K2317/53 , C07K2317/54 , C07K2317/55 , C07K2317/94 , C07K2319/70 , Y10S530/866 , Y10S530/867
摘要： Peptides of the formula (1) NTCPPCPXYCPPCPAC are described wherein X and Y, which may be the same or different, is each a neutral aliphatic L-amino acid residue, and protected and reactive derivatives thereof. The peptides may be used as hinge regions in proteins, where they are capable of being covalently coupled to achieve dimeric structure, for example as found in antibodies.
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公开(公告)号：EP0560947B1
公开(公告)日：2000-05-03
申请号：EP92912329.7
申请日：1992-06-11
发明人： KING, David, John 59 Yaverland Drive , TURNER, Alison 43 Braemar Gardens , BEELEY, Nigel, Robert, Arnold , MILLICAN, Thomas, Andrew 3 Harcourt Close
IPC分类号： C07K5/08 , G01N33/577 , C07D207/44 , A61K39/395 , C07D255/02
CPC分类号： C07D207/452 , A61K38/00 , A61K51/10 , A61K51/1045 , A61K2123/00 , C07D403/12 , C07K5/0215 , C07K16/00 , C07K16/30 , C07K16/3007
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9.发明公开
公开(公告)号：EP0970056A1
公开(公告)日：2000-01-12
申请号：EP98909633.4
申请日：1998-03-13
IPC分类号： C07D239/46 , C07D401/12 , A61K31/505
CPC分类号： C07D239/47 , C07D401/12
摘要： Compounds of formula (1) are described and the salts, solvates, hydrates and N-oxides thereof, in which R?1, R2, R3, R4, R5, R6 and R7¿ have the meanings given in Claim 1. The compounds are selective inhibitors of protein kinases, especially src-family protein kinases and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.
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公开(公告)号：EP0948544A1
公开(公告)日：1999-10-13
申请号：EP97947810.0
申请日：1997-12-10
IPC分类号： A61K39 , A61K47 , A61P1 , A61P11 , A61P17 , A61P19 , A61P25 , A61P29 , A61P31 , A61P35 , A61P37 , C07K16 , C12N15
CPC分类号： C07K16/00 , A61K47/68 , A61K2039/505 , C07K16/22 , C07K16/241 , C07K16/3007 , C07K2317/55
摘要： Monovalent antibody fragments are described, each of which has one or more polymer molecules site-specifically attached through a sulphur atom of a cysteine residue located outside of the variable region domain of the antibody. The polymers include synthetic or naturally occurring polymers such as polyalkylenes, polyalkenylenes, polyoxyalkylenes or polysaccharides. Each fragment may be attached to one or more effector or reporter molecules, and is of use in therapy or diagnostics where it has markedly improved binding and/or pharmacokinetic properties when compared to other antibody fragments which have the same number and type of polymer molecules, but in which the polymer molecules are randomly attached.
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