公开(公告)号：WO2014030052A3

公开(公告)日：2014-04-17

申请号：PCT/IB2013001818

申请日：2013-08-21

Applicant: GLAXO GROUP LTD

Inventor： CLEVELAND SEAN MATTHEW ,  SALOMON STEFAN

IPC: C07K16/00 ,  A61K39/00

CPC classification number: A61K31/245 ,  A61K39/0005 ,  A61K39/3955 ,  A61K2300/00

Abstract: The present disclosure provides a means of stabilising an antibody, in particular in protease-rich environments such as the stomach and intestine. A composition, in particular a pharmaceutical composition, comprising an antibody and camostat mesylate is provided, together with uses of said composition as a medicament and in methods of treatment. Compositions of the disclosure are particularly useful in the topical treatment of gastrointestinal conditions, such as Crohn's Disease or ulcerative colitis, or for direct activity in the gut mucosal immune system.

Abstract translation: 本公开提供了稳定抗体的手段，特别是在富含蛋白酶的环境例如胃和肠中。 提供包含抗体和甲磺酸卡莫司他的组合物，特别是药物组合物，以及所述组合物作为药物和治疗方法的用途。 本公开的组合物特别用于局部治疗胃肠病症如克罗恩氏病或溃疡性结肠炎，或用于肠道粘膜免疫系统中的直接活性。

公开(公告)号：WO2013024059A9

公开(公告)日：2014-04-03

申请号：PCT/EP2012065782

申请日：2012-08-13

Applicant: GLAXO GROUP LTD ,  ASHMAN CLAIRE ,  BIRCHLER MARY ,  DE WILDT RUDOLF M T ,  HOLLAND CLAIRE ,  LEWIS ALAN PETER ,  MORLEY PETER ,  SANDAL THOMAS ,  STEWARD MICHAEL

Inventor： ASHMAN CLAIRE ,  BIRCHLER MARY ,  DE WILDT RUDOLF M T ,  HOLLAND CLAIRE ,  LEWIS ALAN PETER ,  MORLEY PETER ,  SANDAL THOMAS ,  STEWARD MICHAEL

IPC: C07K16/00

CPC classification number: C07K16/42 ,  C07K16/00 ,  C07K16/22 ,  C07K16/2878 ,  C07K2317/40 ,  C07K2317/567 ,  C07K2317/569 ,  C07K2317/60 ,  C07K2317/64 ,  C07K2319/00

Abstract: The present invention relates to modified proteins and peptides that have reduced ability to bind to pre-existing antibodies. Such modified protein/peptide molecules can comprise C-terminal additions, extensions or tags and/or certain amino acid substitutions. Such modified molecules (e.g. fusions and conjugates) comprise proteins, peptides, antigen binding molecules, antibodies or antibody fragments such as single variable domains e.g. human immunoglobulin (antibody) single variable domains, and also single variable domains derived from non-human sources such as a llama or camel, e.g. a VHH including a nanobodyTM (described in e.g. WO 94/04678 and WO 95/04079 inter alia). The invention further relates to uses, formulations, compositions comprising such modified C terminally extended and/or amino acid substituted molecules and also to methods of production and expression of these molecules.

Abstract translation: 本发明涉及具有降低与先前存在的抗体结合的能力的修饰的蛋白质和肽。 这种修饰的蛋白质/肽分子可以包含C-末端添加，延伸或标签和/或某些氨基酸取代。 这样的修饰分子（例如融合物和缀合物）包括蛋白质，肽，抗原结合分子，抗体或抗体片段，例如单个可变结构域，例如， 人免疫球蛋白（抗体）单可变结构域，以及衍生自非人来源的单可变结构域，例如美洲驼或骆驼，例如。 包括纳米体系的VHH（例如WO 94/04678和WO 95/04079等）。 本发明还涉及包含这种修饰的C末端延伸和/或氨基酸取代分子的用途，制剂，组合物，以及这些分子的生产和表达方法。

公开(公告)号：WO2013014208A3

公开(公告)日：2013-05-10

申请号：PCT/EP2012064632

申请日：2012-07-25

Applicant: GLAXO GROUP LTD ,  ASHMAN CLAIRE ,  CATCHPOLE IAN RICHARD ,  HUGHES-THOMAS ZOE ,  LEWIS ALAN PETER ,  STEWARD MICHAEL

Inventor： ASHMAN CLAIRE ,  CATCHPOLE IAN RICHARD ,  HUGHES-THOMAS ZOE ,  LEWIS ALAN PETER ,  STEWARD MICHAEL

IPC: C07K16/22 ,  A61P27/02

CPC classification number: C07K16/22 ,  A61K2039/505 ,  A61K2039/54 ,  A61K2039/70 ,  C07K16/46 ,  C07K2317/31 ,  C07K2317/33 ,  C07K2317/35 ,  C07K2317/52 ,  C07K2317/565 ,  C07K2317/569 ,  C07K2317/60 ,  C07K2317/64 ,  C07K2317/76 ,  C07K2317/92 ,  C07K2319/00

Abstract: The present invention is directed to antigen binding constructs comprising one or two epitope binding domains separated by a single chain Fc region of an antibody, wherein each epitope binding domain in capable of binding to VEGF, to dimers comprising two antigen binding constructs of the invention, pharmaceutical compositions comprising said dimers and their use in the treatment of diseases associated with VEGF signalling, such as diabetic macular edema (DME), wet age-related macular degeneration (Wet AMD), diabetic retinopathy, retinal vein occlusion (RVO), and corneal neovascularisation, and polynucleotide sequences encoding said antigen binding constructs.

Abstract translation: 本发明涉及包含通过抗体的单链Fc区分离的一个或两个表位结合结构域的抗原结合构建体，其中能够结合VEGF的每个表位结合域与包含本发明的两个抗原结合构建体的二聚体， 包含所述二聚体的药物组合物及其用于治疗与VEGF信号传导相关的疾病，例如糖尿病性黄斑水肿（DME），湿性年龄相关性黄斑变性（湿性AMD），糖尿病性视网膜病变，视网膜静脉阻塞（RVO）和角膜 新血管形成和编码所述抗原结合构建体的多核苷酸序列。

公开(公告)号：WO2012080243A2

公开(公告)日：2012-06-21

申请号：PCT/EP2011072600

申请日：2011-12-13

Applicant: GLAXO GROUP LTD ,  DWYER ANDREW NEIL ,  GORDON ANDREW ,  URQUHART MICHAEL

Inventor： DWYER ANDREW NEIL ,  GORDON ANDREW ,  URQUHART MICHAEL

IPC: C07C46/00

CPC classification number: C07C46/00 ,  C07C45/41 ,  C07C51/60 ,  C07C69/76 ,  C07C69/78 ,  C07C2601/14 ,  C07D307/89 ,  C07D311/76 ,  C07C50/32 ,  C07C61/40 ,  C07C47/457

Abstract: Disclosed herein is novel process for preparation of atovaquone, which process includes reacting1H-2-benzopyran-1,4(3H)-dione with 4-(4-chlorophenyl)cyclohexanecarbaldehyde. The invention further discloses novel intermediates useful in the preparation of atovaquone.

Abstract translation: 本文公开的是制备阿托伐醌的新方法，该方法包括使H-2-苯并吡喃-1,4（3H） - 二酮与4-（4-氯苯基）环己烷甲醛反应。 本发明还公开了可用于制备阿托瓦醌的新型中间体。

公开(公告)号：WO2012069433A2

公开(公告)日：2012-05-31

申请号：PCT/EP2011070604

申请日：2011-11-21

Applicant: GLAXO GROUP LTD ,  BEMBRIDGE GARY PETER ,  CHUNG CHUN-WA ,  FEENEY MARIA ,  FORD SUSANNAH KAREN ,  KIRBY IAN ,  MCADAM RUTH

Inventor： BEMBRIDGE GARY PETER ,  CHUNG CHUN-WA ,  FEENEY MARIA ,  FORD SUSANNAH KAREN ,  KIRBY IAN ,  MCADAM RUTH

IPC: C07K16/24

CPC classification number: C07K16/248 ,  C07K16/24 ,  C07K16/244 ,  C07K2317/10 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/51 ,  C07K2317/515 ,  C07K2317/522 ,  C07K2317/524 ,  C07K2317/526 ,  C07K2317/54 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/569 ,  C07K2317/76 ,  C07K2317/92

Abstract: The present invention concerns antigen binding proteins and fragments thereof which specifically bind Oncostatin M (OSM), particularly human OSM (hOSM) and which inhibit the binding of OSM to the gp130 receptor but does not directly interact with site II residues. The invention also concerns a method of humanising antibodies. Further disclosed are pharmaceutical compositions, screening and medical treatment methods.

Abstract translation: 本发明涉及特异性结合制瘤素M（OSM），特别是人OSM（hOSM）并且抑制OSM与gp130受体的结合但不直接与位点II残基相互作用的抗原结合蛋白及其片段。 本发明还涉及一种人源化抗体的方法。 进一步公开的是药物组合物，筛选和治疗方法。

公开(公告)号：WO2012022703A3

公开(公告)日：2012-04-26

申请号：PCT/EP2011064000

申请日：2011-08-12

Applicant: GLAXO GROUP LTD ,  DE ANGELIS ELENA ,  ENEVER CAROLYN ,  LIU HAIQUN ,  PUPECKA-SWIDER MALGORZATA ,  SCHON OLIVER

Inventor： DE ANGELIS ELENA ,  ENEVER CAROLYN ,  LIU HAIQUN ,  PUPECKA-SWIDER MALGORZATA ,  SCHON OLIVER

IPC: C07K16/18 ,  C12N15/13

CPC classification number: C07K16/18 ,  A61K47/6843 ,  C07K2317/21 ,  C07K2317/33 ,  C07K2317/565 ,  C07K2317/569 ,  C07K2317/90 ,  C07K2317/92

Abstract: The invention relates to improved variants of the anti-serum albumin immunoglobulin single variable domain DOM7h-14-10, as well as ligands and drug conjugates comprising such variants, compositions, nucleic acids, vectors and hosts.

Abstract translation: 本发明涉及抗血清白蛋白免疫球蛋白单可变结构域DOM7h-14-10的改良变体，以及包含此类变体，组合物，核酸，载体和宿主的配体和药物缀合物。

公开(公告)号：WO2011051820A3

公开(公告)日：2011-12-15

申请号：PCT/IB2010003289

申请日：2010-10-28

Applicant: GLAXO GROUP LTD ,  UNIV BRISTOL ,  BAILEY ANDREW MARK ,  COLLINS CATHERINE ,  CRAWFORD AMANDA ,  FOSTER GARY ,  GRIFFIN ALISON MICHELLE ,  KILARU SREEDHAR ,  SCROGHAM ANGELA ,  SPENCE DAVID

Inventor： BAILEY ANDREW MARK ,  COLLINS CATHERINE ,  CRAWFORD AMANDA ,  FOSTER GARY ,  GRIFFIN ALISON MICHELLE ,  KILARU SREEDHAR ,  SCROGHAM ANGELA ,  SPENCE DAVID

IPC: C12N1/00 ,  C12N15/74

CPC classification number: C12P15/00 ,  C12N15/52 ,  C12Y205/01029

Abstract: This invention relates to a novel Pleuromutilin gene cluster and methods of increasing yields of Pleuromutilin produced by Clitopilus and related basidiomycete species.

Abstract translation: 本发明涉及一种新型的Pleuromutilin基因簇和增加由Clitopilus和相关担子菌种产生的Pleuromutilin产量的方法。

公开(公告)号：WO2011054783A3

公开(公告)日：2011-07-07

申请号：PCT/EP2010066577

申请日：2010-11-02

Applicant: GLAXO GROUP LTD ,  AMIRA PHARMACEUTICALS INC ,  CRAWFORD CLAIRE FRANCES ,  GARCIA SANDRINE ,  GRAHAM JONATHAN PAUL ,  HARLING SANDRA JANE ,  HENLEY NICHOLAS PAUL ,  HERMITAGE STEPHEN ANDREW ,  HUTCHINSON JOHN HOWARD ,  KEEL TREVOR RAYMOND ,  KENNEDY ANDREW ,  MASON ANDREW MCMURTRIE ,  SCOTT MARK SIMON ,  SMITH NEIL MICHAEL ,  STOCK NICHOLAS SIMON ,  TATENO YUICHI ,  TROUW LEONTINE SASKIA ,  TURNER PETER GRAHAM ,  WALLIS CHRISTOPHER JOHN ,  WILLACY ROBERT DAVID

Inventor： CRAWFORD CLAIRE FRANCES ,  GARCIA SANDRINE ,  GRAHAM JONATHAN PAUL ,  HARLING SANDRA JANE ,  HENLEY NICHOLAS PAUL ,  HERMITAGE STEPHEN ANDREW ,  HUTCHINSON JOHN HOWARD ,  KEEL TREVOR RAYMOND ,  KENNEDY ANDREW ,  MASON ANDREW MCMURTRIE ,  SCOTT MARK SIMON ,  SMITH NEIL MICHAEL ,  STOCK NICHOLAS SIMON ,  TATENO YUICHI ,  TROUW LEONTINE SASKIA ,  TURNER PETER GRAHAM ,  WALLIS CHRISTOPHER JOHN ,  WILLACY ROBERT DAVID

IPC: C07D403/14

CPC classification number: C07D403/14

Abstract: The present invention provides processes useful for preparing 5-lipoxygenase activating protein (FLAP) inhibitors and their intermediates. In particular, processes for preparing 3-[3-(tert-butylsulfanyl)-1-[4-(6-ethoxy-pyridin-3-yl)benzyl]-5-(5-methyl-pyridin-2-yl-methoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid, the anhydrous Form C polymorph of sodium 3-[3- (tert-butylsulfanyl)-1-[4-(6-ethoxy-pyridin-3-yl)benzyl]-5-(5-methyl-pyridin-2-yl-methoxy)-1H- indol-2-yl]-2,2-dimethyl-propionate, and intermediates useful in said processes are provided.

Abstract translation: 本发明提供了可用于制备5-脂氧合酶活化蛋白（FLAP）抑制剂及其中间体的方法。 特别地，制备3- [3-（叔丁基硫烷基）-1- [4-（6-乙氧基 - 吡啶-3-基）苄基] -5-（5-甲基 - 吡啶-2-基 - 甲氧基 ）-1H-吲哚-2-基] -2,2-二甲基 - 丙酸，3- [3-（叔丁基硫烷基）-1- [4-（6-乙氧基 - 吡啶-2-基） （5-甲基 - 吡啶-2-基 - 甲氧基）-1H-吲哚-2-基] -2,2-二甲基 - 丙酸酯，以及可用于所述方法的中间体。

公开(公告)号：WO2009135854A3

公开(公告)日：2010-11-04

申请号：PCT/EP2009055437

申请日：2009-05-05

Applicant: GLAXO GROUP LTD ,  FIDANBOYLU MEHMET ,  PAPANICOLAOU IRENE

Inventor： FIDANBOYLU MEHMET ,  PAPANICOLAOU IRENE

IPC: A61K9/51

CPC classification number: A61K9/5138 ,  A61K9/0051 ,  A61K9/1647 ,  A61K9/5153 ,  A61K9/5192 ,  A61K2039/505

Abstract: The present invention provides methods of encapsulating biologically active agents such as proteins in particulate carriers such as nanoparticles. Also provided are compositions comprising particulate carriers obtainable by such methods and uses of such compositions in treatment.

Abstract translation: 本发明提供了将生物活性剂如蛋白质包封在颗粒载体如纳米颗粒中的方法。 还提供了包含可通过这些方法和这些组合物在处理中的用途获得的颗粒载体的组合物。

公开(公告)号：WO2010119078A1

公开(公告)日：2010-10-21

申请号：PCT/EP2010054910

申请日：2010-04-14

Applicant: GLAXO GROUP LTD ,  DINNELL KEVIN

Inventor： DINNELL KEVIN

IPC: C07D401/14 ,  A61K31/4427 ,  A61P25/00

CPC classification number: C07D401/14

Abstract: This invention relates to modulation of the a7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof: wherein R1 is imidazolyl, pyridinyl or pyrimidinyl, any of which is optionally substituted by one group independently selected from C1-3alkyl and C1-3alkoxy.

Abstract translation: 本发明涉及通过式（I）化合物或其盐调节a7烟碱乙酰胆碱受体（nAChR）：其中R1是咪唑基，吡啶基或嘧啶基，其中任何一个任选被一个独立地选自C1- 3-烷基和C 1-3烷氧基。