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公开(公告)号：US08324204B2
公开(公告)日：2012-12-04
申请号：US12303713
申请日：2007-06-04
申请人： Rikki Peter Alexander , Stuart Bailey , Stephen Brand , Daniel Christopher Brookings , Julien Alistair Brown , Alan Findlay Haughan , Natasha Kinsella , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Marianna Dilani Richard , Andrew Sharpe , Laura Jane Tait
发明人： Rikki Peter Alexander , Stuart Bailey , Stephen Brand , Daniel Christopher Brookings , Julien Alistair Brown , Alan Findlay Haughan , Natasha Kinsella , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Marianna Dilani Richard , Andrew Sharpe , Laura Jane Tait
IPC分类号： A61K31/535
CPC分类号： 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
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20100305066A1
公开(公告)日：2010-12-02
申请号：US12303713
申请日：2007-06-04
申请人： Rikki Peter Alexander , Stuart Bailey , Stephen Brand , Daniel Christopher Brookings , Julien Alistair Brown , Alan Findlay Haughan , Natasha Kinsella , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Marianna Dilani Richard , Andrew Sharpe , Laura Jane Tait
发明人： Rikki Peter Alexander , Stuart Bailey , Stephen Brand , Daniel Christopher Brookings , Julien Alistair Brown , Alan Findlay Haughan , Natasha Kinsella , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Marianna Dilani Richard , Andrew Sharpe , Laura Jane Tait
IPC分类号： A61K31/695 , C07D413/04 , A61K31/5377 , C07D413/14 , C07F7/08 , C07D495/04 , A61K31/55 , A61P3/00 , A61P13/00 , A61P9/00 , A61P25/00 , A61P27/02 , A61P37/00
CPC分类号： 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
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US09290456B2
公开(公告)日：2016-03-22
申请号：US14240045
申请日：2012-08-21
申请人： William Farnaby , Charlotte Fieldhouse , Katherine Hazel , Catrina Kerr , Natasha Kinsella , David Livermore , Kevin Merchant , David Miller
发明人： William Farnaby , Charlotte Fieldhouse , Katherine Hazel , Catrina Kerr , Natasha Kinsella , David Livermore , Kevin Merchant , David Miller
IPC分类号： C07D237/16 , C07D401/06 , A61K31/50 , A61K31/501 , C07D401/10 , C07D407/10 , A61K45/06 , C07D237/18 , C07D237/22 , C07D405/06 , C07F7/08
CPC分类号： A61K31/50 , A61K31/501 , A61K45/06 , C07D237/16 , C07D237/18 , C07D237/22 , C07D401/06 , C07D401/10 , C07D405/06 , C07D407/10 , C07F7/0812
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译： 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。
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公开(公告)号：US20150030704A1
公开(公告)日：2015-01-29
申请号：US14240045
申请日：2012-08-21
申请人： William Farnaby , Charlotte Fieldhouse , Katherine Hazel , Catrina Kerr , Natasha Kinsella , David Livermore , Kevin Merchant , David Miller
发明人： William Farnaby , Charlotte Fieldhouse , Katherine Hazel , Catrina Kerr , Natasha Kinsella , David Livermore , Kevin Merchant , David Miller
IPC分类号： C07D237/16 , C07D401/06 , A61K45/06 , C07D237/18 , C07D237/22 , C07D405/06 , A61K31/50 , A61K31/501
CPC分类号： A61K31/50 , A61K31/501 , A61K45/06 , C07D237/16 , C07D237/18 , C07D237/22 , C07D401/06 , C07D401/10 , C07D405/06 , C07D407/10 , C07F7/0812
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译： 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。
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公开(公告)号：US20140248378A1
公开(公告)日：2014-09-04
申请号：US14131337
申请日：2012-07-05
IPC分类号： A61K31/513 , C07D239/22 , C07D403/12 , C07D401/12 , A61K45/06 , C07D471/04 , C07D413/12 , C07D405/12
CPC分类号： A61K31/513 , A61K45/06 , C07D239/22 , C07D239/54 , C07D239/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20130052281A1
公开(公告)日：2013-02-28
申请号：US13591859
申请日：2012-08-22
申请人： William FARNABY , Charlotte FIELDHOUSE , Catrina KERR , Natasha KINSELLA , David LIVERMORE , Kevin MERCHANT , David MILLER , Katherine HAZEL
发明人： William FARNABY , Charlotte FIELDHOUSE , Catrina KERR , Natasha KINSELLA , David LIVERMORE , Kevin MERCHANT , David MILLER , Katherine HAZEL
IPC分类号： C07D237/16 , C07D401/06 , C07D237/18 , A61K31/50 , A61K31/501 , C07D405/06 , C07D237/22 , A61K31/55 , A61K31/5513 , A61K31/554 , A61K31/53 , A61K31/519 , A61K33/00 , A61P25/18 , A61P25/00 , A61P29/00 , C07F7/10
CPC分类号： A61K31/50 , A61K31/501 , A61K45/06 , C07D237/16 , C07D237/18 , C07D237/22 , C07D401/06 , C07D401/10 , C07D405/06 , C07D407/10 , C07F7/0812
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译： 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。
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公开(公告)号：US10085986B2
公开(公告)日：2018-10-02
申请号：US14131337
申请日：2012-07-05
IPC分类号： C07F9/02 , A61K31/513 , C07D239/54 , C07D239/60 , A61K45/06 , C07D239/22 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： 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.
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8.发明授权5- or 6-substituted 3-hydroxy-2 (1 H)-pyridinones as D-amino acid oxidase (DAAO) inhibitors in therapy of diseases such as schizophrenia, cognitive disorder and pain 有权5-或6-取代的3-羟基-2（1H） - 吡啶酮作为D-氨基酸氧化酶（DAAO）抑制剂治疗精神分裂症，认知障碍和疼痛等疾病公开(公告)号：US09180122B2
公开(公告)日：2015-11-10
申请号：US14131343
申请日：2012-07-05
申请人： William Farnaby , Charlotte Fieldhouse , Catrina Kerr , Natasha Kinsella , David Livermore , Kevin Merchant , David Miller , Katherine Hazel
发明人： William Farnaby , Charlotte Fieldhouse , Catrina Kerr , Natasha Kinsella , David Livermore , Kevin Merchant , David Miller , Katherine Hazel
IPC分类号： A61K31/4412 , A61K31/444 , A61K31/497 , A61K45/06 , C07D213/69 , C07D213/70 , C07D213/71 , C07D401/12 , C07D413/12
CPC分类号： A61K31/4412 , A61K31/444 , A61K31/497 , A61K45/06 , C07D213/69 , C07D213/70 , C07D213/71 , C07D401/12 , C07D413/12
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 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).
摘要翻译： 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）。
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公开(公告)号：US20110105508A1
公开(公告)日：2011-05-05
申请号：US12809394
申请日：2008-12-17
申请人： Daniel Rees Allen , George Martin Buckley , Roland Bürli , John Richard Davenport , Natasha Kinsella , Christopher James Lock , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Andrew James Ratcliffe , Marianna Dilani Richard , Verity Margaret Sabin , Andrew Sharpe , Laura Jane Tait , Graham John Warrelow , Sophie Caroline Williams
发明人： Daniel Rees Allen , George Martin Buckley , Roland Bürli , John Richard Davenport , Natasha Kinsella , Christopher James Lock , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Andrew James Ratcliffe , Marianna Dilani Richard , Verity Margaret Sabin , Andrew Sharpe , Laura Jane Tait , Graham John Warrelow , Sophie Caroline Williams
IPC分类号： A61K31/53 , A61K31/498 , C07D473/00 , A61K31/52 , A61K31/506 , C07D401/02 , C07D403/02 , A61K31/4725 , A61P29/00 , A61P9/00 , A61P25/00 , A61P3/00 , A61P27/02
CPC分类号： C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36
摘要： 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.
摘要翻译： 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。
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10.发明申请5- OR 6-SUBSTITUTED 3-HYDROXY-2(1H)-PYRIDINONES AS D-AMINO ACID OXIDASE (DAAO) INHIBITORS IN THERAPY OF DISEASES SUCH AS SCHIZOPHRENIA, COGNITIVE DISORDER AND PAID 有权5-或6-取代的3-羟基-2（1H） - 吡啶酮作为D-氨基酸氧化酶（DAAO）抑制剂治疗疾病如SCHIZOPHRENIA，认知障碍和PAID公开(公告)号：US20140243353A1
公开(公告)日：2014-08-28
申请号：US14131343
申请日：2012-07-05
申请人： William Farnaby , Charlotte Fieldhouse , Catrina Kerr , Natasha Kinsella , David Livermore , Kevin Merchant , David Miller , Katherine Hazel
发明人： William Farnaby , Charlotte Fieldhouse , Catrina Kerr , Natasha Kinsella , David Livermore , Kevin Merchant , David Miller , Katherine Hazel
IPC分类号： C07D413/12 , A61K31/4412 , C07D401/12 , A61K45/06 , A61K31/497 , C07D213/69 , C07D213/71 , C07D213/70 , A61K31/444
CPC分类号： A61K31/4412 , A61K31/444 , A61K31/497 , A61K45/06 , C07D213/69 , C07D213/70 , C07D213/71 , C07D401/12 , C07D413/12
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 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).
摘要翻译： 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）。
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