公开(公告)号：WO2013004995A8

公开(公告)日：2013-01-10

申请号：PCT/GB2012/000573

申请日：2012-07-05

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  COCKCROFT, Xiao-Ling ,  FARNABY, William ,  KINSELLA, Natasha ,  MERCHANT, Kevin ,  MILLER, David

Inventor： COCKCROFT, Xiao-Ling ,  FARNABY, William ,  KINSELLA, Natasha ,  MERCHANT, Kevin ,  MILLER, David

IPC: C07D239/54 ,  C07D239/60 ,  A61P25/18 ,  A61K31/513

Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

公开(公告)号：WO2009081105A2

公开(公告)日：2009-07-02

申请号：PCT/GB2008004171

申请日：2008-12-17

Applicant: UCB PHARMA SA ,  ALLEN DANIEL REES ,  BUCKLEY GEORGE MARTIN ,  BUERLI ROLAND ,  DAVENPORT RICHARD JOHN ,  KINSELLA NATASHA ,  LOCK CHRISTOPHER JAMES ,  LOWE CHRISTOPHER ,  MACK STEPHEN ROBERT ,  PITT WILLIAM ROSS ,  RATCLIFFE ANDREW JAMES ,  RICHARD MARIANNA DILANI ,  SABIN VERITY MARGARET ,  SHARPE ANDREW ,  TAIT LAURA JANE ,  WARRELOW GRAHAM JOHN ,  WILLIAMS SOPHIE CAROLINE

Inventor： ALLEN DANIEL REES ,  BUCKLEY GEORGE MARTIN ,  BUERLI ROLAND ,  DAVENPORT RICHARD JOHN ,  KINSELLA NATASHA ,  LOCK CHRISTOPHER JAMES ,  LOWE CHRISTOPHER ,  MACK STEPHEN ROBERT ,  PITT WILLIAM ROSS ,  RATCLIFFE ANDREW JAMES ,  RICHARD MARIANNA DILANI ,  SABIN VERITY MARGARET ,  SHARPE ANDREW ,  TAIT LAURA JANE ,  WARRELOW GRAHAM JOHN ,  WILLIAMS SOPHIE CAROLINE

IPC: C07D401/14 ,  A61K31/395 ,  A61P35/00 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D473/34 ,  C07D473/36

CPC classification number: C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D473/34 ,  C07D473/36

Abstract: A series of heteroaryl-substituted quinoxaline and quinoline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract translation: 因此，作为PI3激酶的选择性抑制剂的一系列杂芳基取代的喹喔啉和喹啉衍生物在医学中是有益的，例如在治疗炎症，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害感受性或眼科疾病中。

公开(公告)号：WO2013004995A1

公开(公告)日：2013-01-10

申请号：PCT/GB2012000573

申请日：2012-07-05

Applicant: TAKEDA PHARMACEUTICAL ,  COCKCROFT XIAO-LING FAN ,  FARNABY WILLIAM ,  KINSELLA NATASHA ,  MERCHANT KEVIN ,  MILLER DAVID

Inventor： COCKCROFT XIAO-LING FAN ,  FARNABY WILLIAM ,  KINSELLA NATASHA ,  MERCHANT KEVIN ,  MILLER DAVID

IPC: C07D239/54 ,  A61K31/513 ,  A61P25/18 ,  C07D239/60

CPC classification number: A61K31/513 ,  A61K45/06 ,  C07D239/22 ,  C07D239/54 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract translation: 本发明提供式（1）化合物及其药学上可接受的盐，其中R1，R2，Y和Z如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途。

公开(公告)号：WO2009081105A3

公开(公告)日：2009-07-02

申请号：PCT/GB2008/004171

申请日：2008-12-17

Applicant: UCB PHARMA S.A. ,  ALLEN, Daniel, Rees ,  BUCKLEY, George, Martin ,  BÜRLI, Roland ,  DAVENPORT, Richard, John ,  KINSELLA, Natasha ,  LOCK, Christopher, James ,  LOWE, Christopher ,  MACK, Stephen, Robert ,  PITT, William, Ross ,  RATCLIFFE, Andrew, James ,  RICHARD, Marianna, Dilani ,  SABIN, Verity, Margaret ,  SHARPE, Andrew ,  TAIT, Laura, Jane ,  WARRELOW, Graham, John ,  WILLIAMS, Sophie, Caroline

Inventor： ALLEN, Daniel, Rees ,  BUCKLEY, George, Martin ,  BÜRLI, Roland ,  DAVENPORT, Richard, John ,  KINSELLA, Natasha ,  LOCK, Christopher, James ,  LOWE, Christopher ,  MACK, Stephen, Robert ,  PITT, William, Ross ,  RATCLIFFE, Andrew, James ,  RICHARD, Marianna, Dilani ,  SABIN, Verity, Margaret ,  SHARPE, Andrew ,  TAIT, Laura, Jane ,  WARRELOW, Graham, John ,  WILLIAMS, Sophie, Caroline

IPC: C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D473/34 ,  C07D473/36 ,  A61K31/395 ,  A61P35/00

Abstract: A series of heteroaryl-substituted quinoxaline and quinoline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

公开(公告)号：WO2013027000A1

公开(公告)日：2013-02-28

申请号：PCT/GB2012/000672

申请日：2012-08-21

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  FARNABY, William ,  FIELDHOUSE, Charlotte ,  HAZEL, Katherine ,  KERR, Catrina ,  KINSELLA, Natasha ,  LIVERMORE, David ,  MERCHANT, Kevin ,  MILLER, David

Inventor： FARNABY, William ,  FIELDHOUSE, Charlotte ,  HAZEL, Katherine ,  KERR, Catrina ,  KINSELLA, Natasha ,  LIVERMORE, David ,  MERCHANT, Kevin ,  MILLER, David

IPC: C07D237/16 ,  C07D401/10 ,  C07D407/10 ,  A61K31/50 ,  A61K31/501 ,  A61P25/18 ,  A61P29/00 ,  A61P25/28

CPC classification number: A61K31/50 ,  A61K31/501 ,  A61K45/06 ,  C07D237/16 ,  C07D237/18 ,  C07D237/22 ,  C07D401/06 ,  C07D401/10 ,  C07D405/06 ,  C07D407/10 ,  C07F7/0812

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R 1 and R 2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其中R1和R2如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途。

公开(公告)号：WO2013004996A1

公开(公告)日：2013-01-10

申请号：PCT/GB2012/000574

申请日：2012-07-05

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  FARNABY, William ,  FIELDHOUSE, Charlotte ,  KERR, Catrina ,  KINSELLA, Natasha ,  LIVERMORE, David ,  MERCHANT, Kevin ,  MILLER, David ,  HAZEL, Katherine

Inventor： FARNABY, William ,  FIELDHOUSE, Charlotte ,  KERR, Catrina ,  KINSELLA, Natasha ,  LIVERMORE, David ,  MERCHANT, Kevin ,  MILLER, David ,  HAZEL, Katherine

IPC: C07D213/69 ,  C07D213/70 ,  C07D213/71 ,  C07D401/12 ,  C07D413/12 ,  A61K31/4412 ,  A61K31/4415 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00

CPC classification number: A61K31/4412 ,  A61K31/444 ,  A61K31/497 ,  A61K45/06 ,  C07D213/69 ,  C07D213/70 ,  C07D213/71 ,  C07D401/12 ,  C07D413/12

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R 1 is hydrogen or fluorine, one of A and B is R2, the other is a group -X-Y-R3. R3 represents a carbocyclic or heterocyclic ring. Further variables are as defined in the specification. Also claimed are- processes for their preparation, pharmaceutical compositions containing them and their use in therapy of diseases such as schizophrenia, cognitive disorders and pain by modulating the D-amino acid oxidase enzyme (DAAO).

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其中R 1是氢或氟，A和B之一是R 2，另一个是-X-Y-R 3基团。 R3表示碳环或杂环。 其他变量如本说明书中所定义。 还要求保护其制备方法，含有它们的药物组合物及其在治疗疾病如精神分裂症，认知障碍和通过调节D-氨基酸氧化酶（DAAO）的疼痛中的用途）。

公开(公告)号：WO2009071895A1

公开(公告)日：2009-06-11

申请号：PCT/GB2008/004011

申请日：2008-12-03

Applicant: UCB PHARMA S.A. ,  KINSELLA, Natasha ,  LOWE, Christopher ,  MORGAN, Trevor ,  PERRY, Benjamin Garfield ,  SABIN, Verity Margaret ,  SHARPE, Andrew

Inventor： KINSELLA, Natasha ,  LOWE, Christopher ,  MORGAN, Trevor ,  PERRY, Benjamin Garfield ,  SABIN, Verity Margaret ,  SHARPE, Andrew

IPC: C07D495/04 ,  A61K31/4365 ,  A61P29/00 ,  C07D417/14 ,  C07D513/04

CPC classification number: C07D513/04 ,  C07D417/14 ,  C07D495/04

Abstract: A series of fused bicyclic thiazole and thiophene derivatives which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, and in the 4-position by hydroxy, oxo or an amine moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. (I)

Abstract translation: 通过任选取代的吗啉-4-基部分在2-位被羟基，氧代或胺部分取代的一系列稠合双环噻唑和噻吩衍生物是PI3激酶的选择性抑制剂 因此在医学上有益，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病中。 （一世）

公开(公告)号：WO2007141504A1

公开(公告)日：2007-12-13

申请号：PCT/GB2007/002051

申请日：2007-06-04

Applicant: UCB PHARMA S.A. ,  ALEXANDER, Rikki Peter ,  BAILEY, Stuart ,  BRAND, Stephen ,  BROOKINGS, Daniel Christopher ,  BROWN, Julien Alistair ,  HAUGHAN, Alan Findlay ,  KINSELLA, Natasha ,  LOWE, Christopher ,  MACK, Stephen Robert ,  PITT, William Ross ,  RICHARD, Marianna Dilani ,  SHARPE, Andrew ,  TAIT, Laura Jane

Inventor： ALEXANDER, Rikki Peter ,  BAILEY, Stuart ,  BRAND, Stephen ,  BROOKINGS, Daniel Christopher ,  BROWN, Julien Alistair ,  HAUGHAN, Alan Findlay ,  KINSELLA, Natasha ,  LOWE, Christopher ,  MACK, Stephen Robert ,  PITT, William Ross ,  RICHARD, Marianna Dilani ,  SHARPE, Andrew ,  TAIT, Laura Jane

IPC: C07D333/66 ,  C07D333/68 ,  C07D409/12 ,  C07D409/14 ,  C07D451/04 ,  C07D453/02 ,  C07D471/04 ,  C07D495/04 ,  A61K31/55 ,  A61K31/5377 ,  A61P3/00

CPC classification number: C07D333/66 ,  C07D333/68 ,  C07D333/76 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D451/04 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract translation: 一系列5位二氢-1-苯并噻吩-7（4H） - 酮衍生物及其类似物，其在2-位被任选取代的吗啉-4-基部分取代，为PI3激酶的选择性抑制剂 酶在医学上有益，例如在治疗炎症，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害性感受性或眼科疾病中。