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公开(公告)号：US08399483B2
公开(公告)日：2013-03-19
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 Warrellow , 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 Warrellow , Sophie Caroline Williams
IPC分类号： A61K31/47
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, said substituted derivatives having the general formula
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，例如在治疗炎性，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，所述 具有通式的取代衍生物
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公开(公告)号：US08242116B2
公开(公告)日：2012-08-14
申请号：US12306151
申请日：2007-06-26
申请人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crépy , Anne Marie Foley , Richard Jeremy Franklin , Alan Findlay Haughan , Helen Tracey Horsley , William Mark Jones , Bénédicte Irma Léonce Frédérique Lallemand , Stephen Robert Mack , Trevor Morgan , Patrick Marie Ghislain Pasau , David Jonathan Phillips , Verity Margaret Sabin , George Martin Buckley , Kerry Jenkins , Benjamin Garfield Perry
发明人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crépy , Anne Marie Foley , Richard Jeremy Franklin , Alan Findlay Haughan , Helen Tracey Horsley , William Mark Jones , Bénédicte Irma Léonce Frédérique Lallemand , Stephen Robert Mack , Trevor Morgan , Patrick Marie Ghislain Pasau , David Jonathan Phillips , Verity Margaret Sabin , George Martin Buckley , Kerry Jenkins , Benjamin Garfield Perry
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： C07D495/04 , C07D513/04 , C07D513/12 , C07D519/00
摘要： A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-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6,7-二氢[1,3]噻唑并[5,4-c]吡啶-4（5H） - 酮衍生物及其类似物，其在2-位被任选取代的吗啉-4- 作为PI3激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎性，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：US20100069361A1
公开(公告)日：2010-03-18
申请号：US12445056
申请日：2007-10-10
IPC分类号： A61K31/538 , C07D413/04 , C07D513/04 , A61K31/55 , A61P29/00 , A61P37/00 , A61P9/00 , A61P25/28 , A61P35/00 , A61P27/02 , A61P3/00
CPC分类号： C07D417/04 , C07D498/04 , C07D513/04
摘要： A series of 5,5-dimethyl-5,6-dihydro-1,3-benzothiazol-7(4H)-one and 7,7-dimethyl-5,6,7,8-tetrahydro-4H-[1,3]thiazolo[5,4-c]azepin-4-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted benzofused 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. Formula (I).
摘要翻译： 一系列5,5-二甲基-5,6-二氢-1,3-苯并噻唑-7（4H） - 酮和7,7-二甲基-5,6,7,8-四氢-4H- [1,3 ]噻唑并[5,4-c]氮杂-4-酮衍生物及其类似物，其在2-位被任选取代的苯并稠合的吗啉-4-基部分取代，作为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，伤害感受或眼科疾病中。 式（I）。
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公开(公告)号：US5753666A
公开(公告)日：1998-05-19
申请号：US691339
申请日：1996-08-02
申请人： Steven Colin Beasley , John Gary Montana , Hazel Joan Dyke , Alan Findlay Haughan , George Martin Buckley , Andrew Douglas Baxter
发明人： Steven Colin Beasley , John Gary Montana , Hazel Joan Dyke , Alan Findlay Haughan , George Martin Buckley , Andrew Douglas Baxter
IPC分类号： C07D471/04 , A61K31/00 , A61K31/4375 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/47 , A61K31/505 , A61K31/519 , A61K31/529 , A61P11/00 , A61P31/00 , A61P31/10 , A61P37/00 , A01N43/54 , C07D471/00
CPC分类号： A61K31/4375 , A61K31/444 , A61K31/47 , A61K31/519
摘要： 1-Alkyl-substituted-quinolone-3-carboxamides have therapeutic utility via inhibition of Phosphodiesterase IV esterase and/or Tumor Necrosis Factor activity.
摘要翻译： 1-烷基取代的喹诺酮-3-甲酰胺通过抑制磷酸二酯酶IV酯酶和/或肿瘤坏死因子活性具有治疗效用。
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公开(公告)号：US08093238B2
公开(公告)日：2012-01-10
申请号：US12445056
申请日：2007-10-10
IPC分类号： C07D498/04 , C07D513/04 , A61K31/428 , A61K31/429
CPC分类号： C07D417/04 , C07D498/04 , C07D513/04
摘要： A series of 5,5-dimethyl-5,6-dihydro-1,3-benzothiazol-7(4H)-one and 7,7-dimethyl-5,6,7,8-tetrahydro-4H-[1,3]thiazolo[5,4-c]azepin-4-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted benzofused 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. Formula (I).
摘要翻译： 一系列5,5-二甲基-5,6-二氢-1,3-苯并噻唑-7（4H） - 酮和7,7-二甲基-5,6,7,8-四氢-4H- [1,3 ]噻唑并[5,4-c]氮杂-4-酮衍生物及其类似物，其在2-位被任选取代的苯并稠合的吗啉-4-基部分取代，作为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，伤害感受或眼科疾病中。 式（I）。
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公开(公告)号：US07888344B2
公开(公告)日：2011-02-15
申请号：US11912801
申请日：2006-04-25
申请人： Rikki Peter Alexander , Pavandeep Aujla , Mark James Batchelor , Daniel Christopher Brookings , George Martin Buckley , Karen Viviane Lucile Crepy , Claire Louise Kulisa , James Petrie Turner
发明人： Rikki Peter Alexander , Pavandeep Aujla , Mark James Batchelor , Daniel Christopher Brookings , George Martin Buckley , Karen Viviane Lucile Crepy , Claire Louise Kulisa , James Petrie Turner
IPC分类号： A61K31/55 , A61K31/535 , C07D498/04 , C07D413/14
CPC分类号： C07D277/82 , A61K31/4184 , A61K31/4188 , A61K31/55 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/04
摘要： A series of 5,6-dihydro-1,3-benzothiazol-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 PD 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： 通过任选取代的吗啉-4-基部分在2位被取代的一系列5,6-二氢-1,3-苯并噻唑-7（4H） - 酮衍生物及其类似物是选择性抑制剂 因此PD激酶在医学上有益，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。
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公开(公告)号：US20080306060A1
公开(公告)日：2008-12-11
申请号：US11912801
申请日：2006-04-25
申请人： Rikki Peter Alexander , Pavandeep Aujla , Mark James Batchelor , Daniel Christopher Brookings , George Martin Buckley , Karen Viviane Lucile Crepy , Claire Louise Kulisa , James Petrie Turner
发明人： Rikki Peter Alexander , Pavandeep Aujla , Mark James Batchelor , Daniel Christopher Brookings , George Martin Buckley , Karen Viviane Lucile Crepy , Claire Louise Kulisa , James Petrie Turner
IPC分类号： A61K31/5377 , C07D413/14 , C07D413/04 , A61P25/00
CPC分类号： C07D277/82 , A61K31/4184 , A61K31/4188 , A61K31/55 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/04
摘要： A series of 5,6-dihydro-1,3-benzothiazol-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 PD 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： 通过任选取代的吗啉-4-基部分在2位被取代的一系列5,6-二氢-1,3-苯并噻唑-7（4H） - 酮衍生物及其类似物是选择性抑制剂 因此PD激酶在医学上有益，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。
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公开(公告)号：US06313116B1
公开(公告)日：2001-11-06
申请号：US09780911
申请日：2001-02-09
申请人： Hazel Joan Dyke , Andrew Sharpe , Hannah Jayne Kendall , Richard John Davenport , Verity Margaret Sabin , George Martin Buckley , Marianna Dilani Richard , Alan Findlay Haughan
发明人： Hazel Joan Dyke , Andrew Sharpe , Hannah Jayne Kendall , Richard John Davenport , Verity Margaret Sabin , George Martin Buckley , Marianna Dilani Richard , Alan Findlay Haughan
IPC分类号： A61K31428
CPC分类号： C07D417/12
摘要： Compounds that are inhibitors of phosphodiesterase and have therapeutic utility, are of formula (i) wherein R1 is C3-6 cycoalkyl, or C1-3 alkyl optionally substituted with one or more fluorine atoms; R2 is C1-6 alkyl, C3-6 cycloalkyl, CF3, CH2CF3, C2F5 or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, are each H, C1-3 alkyl, halogen, CF3 or CN, provided that both are not H; or a pharmaceutically-acceptable salt thereof
摘要翻译： 作为磷酸二酯酶抑制剂并具有治疗效用的化合物具有式（ⅰ），其中R 1为C 3-6季烷基或任选被一个或多个氟原子取代的C 1-3烷基; R 2为C 1-6烷基，C 3-6环烷基 ，CF 3，CH 2 CF 3，C 2 F 5或NR 4 R 5; R 3为部分式（A），（B）或（C）的吡唑，咪唑或异恶唑基; NR4R5为含氮杂环; R6为C1-3烷基; 和R 7和R 8相同或不同，各自为H，C 1-3烷基，卤素，CF 3或CN，条件是两者均不为H;或其药学上可接受的盐
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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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公开(公告)号：US20100137302A1
公开(公告)日：2010-06-03
申请号：US12306151
申请日：2007-06-26
申请人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crepy , Anne Marie Foley , Richard Jeremy Franklin , Alan Findlay Haughan , Helen Tracey Horsley , William Mark Jones , Benedicte Irma Leonce Frederique Lallemand , Stephen Robert Mack , Trevor Morgan , Patrick Marie Ghislain Pasau , David Jonathan Phillips , Verity Margaret Sabin , George Martin Buckley , Kerry Jenkins , Benjamin Garfield Perry
发明人： Rikki Peter Alexander , Pavandeep Singh Aujla , Karen Viviane Lucile Crepy , Anne Marie Foley , Richard Jeremy Franklin , Alan Findlay Haughan , Helen Tracey Horsley , William Mark Jones , Benedicte Irma Leonce Frederique Lallemand , Stephen Robert Mack , Trevor Morgan , Patrick Marie Ghislain Pasau , David Jonathan Phillips , Verity Margaret Sabin , George Martin Buckley , Kerry Jenkins , Benjamin Garfield Perry
IPC分类号： A61K31/5377 , C07D513/04 , A61P35/04
CPC分类号： C07D495/04 , C07D513/04 , C07D513/12 , C07D519/00
摘要： A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-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6,7-二氢[1,3]噻唑并[5,4-c]吡啶-4（5H） - 酮衍生物及其类似物，其在2-位被任选取代的吗啉-4- 作为PI3激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎性，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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