公开(公告)号：WO2012013682A3

公开(公告)日：2012-05-18

申请号：PCT/EP2011062837

申请日：2011-07-26

Applicant: UCB PHARMA SA ,  SPITALI MARIANGELA ,  SYMMONS JONATHAN ,  WHITCOMBE RICHARD ,  PEARCE-HIGGINS MARK ROBERT

Inventor： SPITALI MARIANGELA ,  SYMMONS JONATHAN ,  WHITCOMBE RICHARD ,  PEARCE-HIGGINS MARK ROBERT

IPC: C07K1/18 ,  C07K1/36

CPC classification number: C07K16/241 ,  C07K1/18 ,  C07K1/36 ,  C07K2317/14 ,  C07K2317/55

Abstract: The present invention relates to a process for the purification of an antibody fragment from a periplasmic cell extract comprising a first cation exchange chromatography step and a second anion exchange chromatography step.

Abstract translation: 本发明涉及从周质细胞提取物纯化抗体片段的方法，其包括第一阳离子交换层析步骤和第二阴离子交换层析步骤。

公开(公告)号：WO2011061246A2

公开(公告)日：2011-05-26

申请号：PCT/EP2010067731

申请日：2010-11-18

Applicant: UCB PHARMA SA ,  HEYWOOD SAM PHILIP ,  HUMPHREYS DAVID PAUL ,  LAWSON ALASTAIR DAVID GRIFFITHS

Inventor： HEYWOOD SAM PHILIP ,  HUMPHREYS DAVID PAUL ,  LAWSON ALASTAIR DAVID GRIFFITHS

IPC: C07K16/00

CPC classification number: C07K16/00 ,  C07K2317/35 ,  C07K2319/30 ,  C07K2319/31

Abstract: A multivalent antibody fusion protein comprising: a heavy chain comprising, in sequence from the N-terminal, a variable domain nominally VH1, a CH1 region and a further variable domain nominally VH2, a light chain comprising, in sequence from the N-terminal, a variable domain nominally VL1, a CL domain and a variable domain nominally VL2, wherein said heavy and light chains are aligned to provide a first binding site formed by a first variable domain pair of VH1 and VL1 and a second binding site formed by a second variable domain pair of VH2 and VL2, and said fusion protein is conjugated to a PEG polymer.

Abstract translation: 一种多价抗体融合蛋白，其包含：重链，其从N-末端开始依次包含可变结构域名义上的VH1，CH1区和另外的可变结构域名义上的VH2，轻链依次包含N-末端， 可变结构域名义上为VL1，CL结构域和名义上可变域为VL2，其中所述重链和轻链对齐以提供由VH1和VL1的第一可变结构域对形成的第一结合位点和由第二可变结构域形成的第二结合位点 VH2和VL2的可变结构域对，并且所述融合蛋白与PEG聚合物缀合。

公开(公告)号：WO2010035012A9

公开(公告)日：2011-03-17

申请号：PCT/GB2009002310

申请日：2009-09-25

Applicant: UCB PHARMA SA ,  ADAMS RALPH ,  HANCOCK LAURA ,  HEYWOOD SAM PHILIP

Inventor： ADAMS RALPH ,  HANCOCK LAURA ,  HEYWOOD SAM PHILIP

IPC: C07K16/46 ,  C07K16/18 ,  C07K16/24 ,  C07K16/28

CPC classification number: C07K16/468 ,  C07K16/18 ,  C07K16/245 ,  C07K16/28 ,  C07K16/2878 ,  C07K2317/24 ,  C07K2317/31 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/569 ,  C07K2317/62 ,  C07K2317/624 ,  C07K2317/92

Abstract: A multivalent antibody fusion protein which comprises an immunoglobulin moiety, for example a Fab or Fab' fragment, with a first specificity for an antigen of interest, and further comprises two single domain antibodies (dAb) with specificity for a second antigen of interest, wherein the two single domain antibodies are linked by a disulfide bond. There is also provided particular dual specificity antibody fusion proteins comprising a Fab or Fab' fragment and one or more single domain antibodies which may be stabilised by a disulfide bond therebetween.

Abstract translation: 一种多价抗体融合蛋白，其包含对目的抗原具有第一特异性的免疫球蛋白部分，例如Fab或Fab'片段，并且还包含对目的第二抗原具有特异性的两个单结构域抗体（dAb），其中 两个单结构域抗体通过二硫键连接。 还提供了特异的双重特异性抗体融合蛋白，其包含Fab或Fab'片段和一个或多个单结构域抗体，其可以通过它们之间的二硫键来稳定。

公开(公告)号：WO2010079345A3

公开(公告)日：2010-11-25

申请号：PCT/GB2010000040

申请日：2010-01-12

Applicant: UCB PHARMA SA ,  LAWSON ALASTAIR DAVID GRIFFITHS

Inventor： LAWSON ALASTAIR DAVID GRIFFITHS

IPC: G01N33/68

CPC classification number: C07K16/24 ,  C07K2299/00 ,  C07K2317/55 ,  C07K2317/76 ,  G01N33/6803 ,  G01N2500/04 ,  G06F19/16 ,  G06F19/70

Abstract: The present invention relates to an improved method for drug discovery comprising using contact residue information derived from antibody-protein target interactions to help to direct the growth of small molecule fragments during the synthesis of a drug candidate. In particular, the present invention relates to the use of atomic structural information derived from antibody-protein interactions to guide the growth of small molecular fragments during lead optimisation, thus generating small molecule compounds which can alter the biological activity of a target protein.

Abstract translation: 本发明涉及用于药物发现的改进方法，其包括使用衍生自抗体 - 蛋白质靶相互作用的接触残基信息来帮助在合成候选药物期间引导小分子片段的生长。 特别地，本发明涉及从抗体 - 蛋白质相互作用衍生的原子结构信息在铅优化过程中引导小分子片段的生长，从而产生可改变靶蛋白的生物活性的小分子化合物。

公开(公告)号：WO2009090499A3

公开(公告)日：2009-07-23

申请号：PCT/IB2008/003984

申请日：2008-12-29

Applicant: UCB PHARMA SA ,  MORGAN, Darrell, P.

Inventor： MORGAN, Darrell, P.

IPC: A61M5/31 ,  A61M5/32

Abstract: The syringe systems disclosed herein provide in part devices for allowing patients with compromised joint strength to more easily administer medicine. Certain exemplary syringe embodiments include a handle forming a handgrip, a syringe barrel that magnifies the dosage marks located on an inner barrel, and a tip cap slidably engageable with the syringe barrel for shielding a needle.

公开(公告)号：WO2009090499A2

公开(公告)日：2009-07-23

申请号：PCT/IB2008003984

申请日：2008-12-29

Applicant: UCB PHARMA SA ,  MORGAN DARRELL P

Inventor： MORGAN DARRELL P

IPC: A61M5/31 ,  A61M5/32

CPC classification number: A61M5/3202 ,  A61M5/3134 ,  A61M5/3137 ,  A61M5/31511 ,  A61M5/3204 ,  A61M2005/3139 ,  A61M2205/585 ,  A61M2205/586

Abstract: The syringe systems disclosed herein provide in part devices for allowing patients with compromised joint strength to more easily administer medicine. Certain exemplary syringe embodiments include a handle forming a handgrip, a syringe barrel that magnifies the dosage marks located on an inner barrel, and a tip cap slidably engageable with the syringe barrel for shielding a needle.

Abstract translation: 本文公开的注射器系统部分地提供允许具有受损的关节强度的患者更容易地管理药物的装置。 某些示例性注射器实施例包括形成手柄的手柄，放大位于内筒上的剂量标记的注射器筒，以及与注射器筒可滑动地接合以用于屏蔽针的尖端帽。

公开(公告)号：WO2008138591A3

公开(公告)日：2009-03-05

申请号：PCT/EP2008003838

申请日：2008-05-13

Applicant: UCB PHARMA SA ,  DAVENPORT RICHARD JOHN ,  RATCLIFFE ANDREW JAMES ,  JONES MARK WILLIAM

Inventor： DAVENPORT RICHARD JOHN ,  RATCLIFFE ANDREW JAMES ,  JONES MARK WILLIAM

IPC: C07D263/56 ,  A61K31/41 ,  A61P35/00 ,  C07D277/66 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D263/56 ,  C07D277/66 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention concerns bicyclic and heterobicyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract translation: 本发明涉及双环和杂双环衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

公开(公告)号：WO2008132142A3

公开(公告)日：2009-01-15

申请号：PCT/EP2008055022

申请日：2008-04-24

Applicant: UCB PHARMA SA ,  KENDA BENOIT ,  TURET LAURENT ,  QUESNEL YANNICK ,  MICHEL PHILIPPE ,  ATES ALI

Inventor： KENDA BENOIT ,  TURET LAURENT ,  QUESNEL YANNICK ,  MICHEL PHILIPPE ,  ATES ALI

IPC: A61K31/4015 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/417 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/45 ,  A61K31/4704 ,  A61K31/472 ,  A61K31/55 ,  C07D207/38 ,  C07D215/22 ,  C07D233/32

CPC classification number: C07D233/32 ,  A61K31/4015 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/417 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/45 ,  A61K31/4704 ,  A61K31/472 ,  A61K31/55 ,  C07D215/227 ,  C07D217/24 ,  C07D263/20 ,  C07D263/22 ,  C07D263/38 ,  C07D277/14 ,  C07D277/34 ,  C07D277/68 ,  C07D401/06 ,  C07D403/06 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D519/00

Abstract: The present invention relates to compounds having the formula (I), its geometrical isomers, enantiomers, diastereomers and mixtures, or a pharmaceutically acceptable salt thereof, wherein Y is O, S or NR8; R1 is hydrogen or C1-6 alky!; R2 is hydrogen; R3 is -CONR5R6, -COR7, an imidazolyl, an imidazopyridinyl, an imidazopyridazinyl or a 1 H-indol-1-yl; R5, R6 are the same or different and are independently selected from hydrogen and C1-6 alkyl; R7 is a C1-6 alkyl; R8 is CN or C1-6 alkylsulfonyl; A is a monocyclic or bicyclic heterocyclic moiety selected from the group consisting of imidazolidin-1-yl, 1,3-oxazoIidin-3-yl, 2,5dihydro-1H-pyrrol-1-yl, 1,3-thiazol-3(2H)-yl, 1,3-thiazolidin-3-yl, pyrrolidin-1-yl, piperidin-1-yl, azepan-1-yl, 5,6-dihydro-4H-thieno[3,2-b]pyrrol-4-yl, hexahydro-4H,-thieno[3,2-b]pyrrol-4-yl, 2,3-dihydro-1H-thieno[3,4-b]pyrrol-1-yl, 1,3-benzothiazol-3(2H)-yl, 1,3-benzoxazol-3(2H)-yl, pyrazolo[1,5-al]pyridin-1 (2H)-yl, 3,4-dihydroisoquinolin-2(1H)-yl, 3,4-dihydroquinolin-1(2H)-yl, 1,3,4,5-tetrahydro-2H-2-benzazepin-2-yl, 1,2,4,5-tetrahydra-3H-3-benzazepin-3-yl; for the manufacture of a medicament for the treatment or prevention of CNS disorders including epilepsy.

Abstract translation: 本发明涉及具有式（I）的化合物，其几何异构体，对映体，非对映异构体及其混合物或其药学上可接受的盐，其中Y是O，S或NR8; R1是氢或C1-6烷基; R2是氢; R3是-CONR5R6，-COR7，咪唑基，咪唑并吡啶基，咪唑并哒嗪基或1H-吲哚-1-基; R5，R6相同或不同，独立地选自氢和C1-6烷基; R7是C1-6烷基; R8是CN或C1-6烷基磺酰基; A是选自咪唑烷-1-基，1,3-恶唑烷-3-基，2,5二氢-1H-吡咯-1-基，1,3-噻唑-3（ 2H） - 基，1,3-噻唑烷-3-基，吡咯烷-1-基，哌啶-1-基，氮杂环庚烷-1-基，5,6-二氢-4H-噻吩并[3,2-b]吡咯 -4-基，六氢-4H - 噻吩并[3,2-b]吡咯-4-基，2,3-二氢-1H-噻吩并[3,4-b]吡咯-1-基， 苯并噻唑-3（2H） - 基，1,3-苯并恶唑-3（2H） - 基，吡唑并[1,5-a]吡啶-1（2H） - 基，3,4-二氢异喹啉-2（1H） 3,4-二氢喹啉-1（2H） - 基，1,3,4,5-四氢-2H-苯并吖庚因-2-基，1,2,4,5-四氢-3H-3-苯并吖庚因 -3-基; 用于制备用于治疗或预防包括癫痫在内的CNS疾病的药物。

公开(公告)号：WO2007107345A3

公开(公告)日：2008-04-10

申请号：PCT/EP2007002485

申请日：2007-03-21

Applicant: UCB PHARMA SA ,  TYRRELL NICHOLAS DAVID ,  TREMAYNE NEIL ,  EVANS GRAHAM ROBERT

Inventor： TYRRELL NICHOLAS DAVID ,  TREMAYNE NEIL ,  EVANS GRAHAM ROBERT

IPC: C07D213/24 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D213/24

Abstract: A process for preparing l-halo-2,7-naphthyridinyl derivatives is described (I), wherein X is Cl or Br; which process comprises the following steps: (i) reaction of a 3-cyano-4-methylpyridine derivative of formula (A): with a compound of formula (II), in the presence of an N,N-dimethylformamide diC 1 - 6 alkylacetal; to give an enamine derivative of formula (III), (ii) cyclisation of the enamine of formula (III), to obtain the compound of formula (IV), (iii) reaction of the compound of formula (IV) with a halogenating agent, to obtain a compound of formula (I).

Abstract translation: 描述了制备1-卤代-2,7-萘啶衍生物的方法（I），其中X是Cl或Br; 该方法包括以下步骤：（i）式（A）的3-氰基-4-甲基吡啶衍生物与式（II）化合物在N，N-二甲基甲酰胺二盐酸盐存在下反应， 1 - _{6 alkylacetal; 得到式（III）的烯胺衍生物，（ii）式（III）的烯胺环化，得到式（Ⅳ）化合物，（ⅲ）式（Ⅳ）化合物与卤化剂的反应 ，得到式（I）的化合物。}

公开(公告)号：WO2008020206A2

公开(公告)日：2008-02-21

申请号：PCT/GB2007003114

申请日：2007-08-15

Applicant: UCB PHARMA SA ,  LAING VICTORIA ELIZABETH ,  BROOKINGS DANIEL CHRISTOPHER ,  CARBERY RACHEL JANE ,  GASCON SIMORTE JOSE MIGUEL ,  HUTCHINGS MARTIN CLIVE ,  LANGHAM BARRY JOHN ,  LOWE MARTIN ALEXANDER

Inventor： LAING VICTORIA ELIZABETH ,  BROOKINGS DANIEL CHRISTOPHER ,  CARBERY RACHEL JANE ,  GASCON SIMORTE JOSE MIGUEL ,  HUTCHINGS MARTIN CLIVE ,  LANGHAM BARRY JOHN ,  LOWE MARTIN ALEXANDER

IPC: C07D495/04 ,  A61K31/55 ,  A61P9/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D495/04

Abstract: A series of 4,5,6,7-tetrahydrothieno[2,3-c]azepin-8-one derivatives, and analogues thereof, which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.

Abstract translation: 一系列4,5,6,7-四氢噻吩并[2,3-c]吖庚因-8-酮衍生物及其类似物，其在2-位被取代的苯胺基部分取代，是人MEK的选择性抑制剂 （MAPKK）酶相应地在医学中有益，例如在治疗炎症，自身免疫，心血管，增殖（包括肿瘤）和伤害性疾病）中。