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1. 发明授权

US5482966A Oxime derivatives 失效
标题翻译：肟衍生物
公开(公告)号：US5482966A
公开(公告)日：1996-01-09
申请号：US240464
申请日：1994-06-13
申请人： Thomas G. C. Bird , Patrick Ple
发明人： Thomas G. C. Bird , Patrick Ple
IPC分类号： A61K31/425 , A61K31/505 , A61P29/00 , A61P37/08 , A61P43/00 , C07D239/42 , C07D307/20 , C07D309/08 , C07D309/10 , C07D317/22 , C07D405/04 , C07D409/02 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/12 , A61K31/35 , A61K31/34
CPC分类号： C07D405/04 , C07D307/20 , C07D309/10 , C07D317/22 , C07D409/04 , C07D417/04
摘要： The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I的肟衍生物，其中R 4包括氢，羧基，氨基甲酰基，氨基，氰基，三氟甲基，（1-4C）烷基氨基，二（1-4C）烷基氨基和（1-4C）烷基 ; R5包括氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，（2-5C）烷酰基，卤代 - （2-4C）烷基和羟基 - （2-4C）烷基; Ar1是亚苯基或杂芳基双基; A1是直接连接到X1，或A1是（1-4C）亚烷基; X1是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基或杂芳基双基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其与A2和A3所连接的碳原子一起形成具有5或6个环原子的环，其中A2和A3各自为（1 -3C）亚烷基，X 2为氧基，硫基，亚磺酰基，磺酰基或亚氨基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

2. 发明授权

US5512594A Ether derivatives having 5-lipoxygenase inhibitory activity 失效
标题翻译：具有5-脂氧合酶抑制活性的醚衍生物
公开(公告)号：US5512594A
公开(公告)日：1996-04-30
申请号：US440132
申请日：1995-05-12
申请人： Thomas G. C. Bird , Graham C. Crawley , Michael S. Large , Patrick Ple
发明人： Thomas G. C. Bird , Graham C. Crawley , Michael S. Large , Patrick Ple
IPC分类号： A61K31/40 , A61K31/47 , A61K31/55 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D405/12 , C07D409/14 , C07D417/14 , C07D493/08 , A61K31/405 , C07D409/12
CPC分类号： C07D405/12 , C07D409/14 , C07D417/14 , C07D493/08
摘要： The invention concerns ether derivatives of the formula IQ.sup.1 -X-Ar-Q.sup.2 Iwherein Q.sup.1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; X is oxy, thio, sulphinyl or sulphonyl; Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazolediyl, thiadiazolediyl or oxadiazolediyl; and Q.sup.2 is selected from the groups of the formulae II and III: ##STR1## wherein R.sup.1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl; R.sup.2 is (1-4C)alkyl; and R.sup.3 is hydrogen or (1-4C)alkyl; or R.sup.2 and R.sup.3 are linked to form a methylene, vinylene, ethylene or trimethylene group; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I Q1-X-Ar-Q2I的醚衍生物，其中Q1是含有一个或两个氮杂原子的任选取代的9,10或11元双环杂环部分，并任选地含有另外的选自氮，氧和硫; X是氧基，硫基，亚磺酰基或磺酰基; Ar是任选取代的亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基，噻唑二基，恶唑二基，噻二唑二基或恶二唑二基。和Q2选自式II和III的基团：其中R 1是氢，（2-5C）烷酰基或任选取代的苯甲酰基; R2是（1-4C）烷基; 并且R 3是氢或（1-4C）烷基; 或R 2和R 3连接形成亚甲基，亚乙烯基，亚乙基或三亚甲基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

3. 发明授权

US5478842A Ether derivatives having 5-lipoxygenase inhibitory activity 失效
标题翻译：具有5-脂氧合酶抑制活性的醚衍生物
公开(公告)号：US5478842A
公开(公告)日：1995-12-26
申请号：US234148
申请日：1994-04-28
申请人： Thomas G. C. Bird , Graham C. Crawley , Michael S. Large , Patrick Ple
发明人： Thomas G. C. Bird , Graham C. Crawley , Michael S. Large , Patrick Ple
IPC分类号： A61K31/40 , A61K31/47 , A61K31/55 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D405/12 , C07D409/14 , C07D417/14 , C07D493/08 , C07D405/14
CPC分类号： C07D405/12 , C07D409/14 , C07D417/14 , C07D493/08
摘要： The invention concerns ether derivatives of the formula IQ.sup.1 --X--Ar--Q.sup.2 IwhereinQ.sup.1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;X is oxy, thio, sulphinyl or sulphonyl;Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazoiediyl, thiadiazoiediyl or oxadiazolediyl; andQ.sup.2 is selected from the groups of the formulae II and III: ##STR1## wherein R.sup.1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl;R.sup.2 is (1-4C)alkyl; andR.sup.3 is hydrogen or (1-4C)alkyl;or R.sup.2 and R.sup.3 are linked to form a methylene, vinylene, ethylene or trimethylene group;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I Q1-X-Ar-Q2I的醚衍生物，其中Q1是含有一个或两个氮杂原子的任选取代的9,10或11元双环杂环部分，并任选地含有另外的选自氮，氧和硫; X是氧基，硫基，亚磺酰基或磺酰基; Ar是任选取代的亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基，噻唑二基，恶唑二基，噻二唑基或恶二唑二基。并且Q2选自式II和III的基团：其中R 1是氢，（2-5C）烷酰基或任选取代的苯甲酰基; R2是（1-4C）烷基; 并且R 3是氢或（1-4C）烷基; 或R 2和R 3连接形成亚甲基，亚乙烯基，亚乙基或三亚甲基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

4. 发明授权

US5332757A Oxime derivatives 失效
标题翻译：肟衍生物
公开(公告)号：US5332757A
公开(公告)日：1994-07-26
申请号：US14564
申请日：1993-02-08
申请人： Thomas G. C. Bird , Patrick Ple
发明人： Thomas G. C. Bird , Patrick Ple
IPC分类号： A61K31/425 , A61K31/505 , A61P29/00 , A61P37/08 , A61P43/00 , C07D239/42 , C07D307/20 , C07D309/08 , C07D309/10 , C07D317/22 , C07D405/04 , C07D409/02 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/12 , A61K31/35 , A61K31/34
CPC分类号： C07D405/04 , C07D307/20 , C07D309/10 , C07D317/22 , C07D409/04 , C07D417/04
摘要： The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 - which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I的肟衍生物，其中R 4包括氢，羧基，氨基甲酰基，氨基，氰基，三氟甲基，（1-4C）烷基氨基，二（1-4C）烷基氨基和（1-4C）烷基 ; R5包括氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，（2-5C）烷酰基，卤代 - （2-4C）烷基和羟基 - （2-4C）烷基; Ar1是亚苯基或杂芳基双基; A1是直接连接到X1，或A1是（1-4C）亚烷基; X1是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基或杂芳基双基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其与A2和A3所连接的碳原子一起形成具有5或6个环原子的环，其中A2和A3各自为（1 -3C）亚烷基，X 2为氧基，硫基，亚磺酰基，磺酰基或亚氨基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

5. 发明授权

US07696214B2 Quinazoline derivatives for the treatment of tumours 有权
标题翻译：喹唑啉衍生物用于治疗肿瘤
公开(公告)号：US07696214B2
公开(公告)日：2010-04-13
申请号：US11283415
申请日：2005-11-21
申请人： Laurent François André Hennequin , Patrick Ple
发明人： Laurent François André Hennequin , Patrick Ple
IPC分类号： C07D239/72 , A01N43/54 , A61K31/517
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/12 , C07D405/12 , C07D405/14
摘要： The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumor disease.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物，其中Q1，Z，m，R1，R2，R3和Q2各自具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用作在实体瘤疾病的遏制和/或治疗中作为抗侵入剂的药物的用途。

6. 发明授权

US07498335B2 Method of producing an antiangiogenic or vascular permeability reducing effect 失效
标题翻译：产生抗血管生成或血管通透性降低作用的方法
公开(公告)号：US07498335B2
公开(公告)日：2009-03-03
申请号：US10220140
申请日：2001-03-01
申请人： Laurent Francois Andre Hennequin , Graham Charles Crawley , Darren McKerrecher , Patrick Ple , Jeffrey Philip Poyser , Christine Marie Paul Lambert
发明人： Laurent Francois Andre Hennequin , Graham Charles Crawley , Darren McKerrecher , Patrick Ple , Jeffrey Philip Poyser , Christine Marie Paul Lambert
IPC分类号： A61K31/517
CPC分类号： A61K31/519 , A61K31/517 , A61K31/5377
摘要： The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human.
摘要翻译：本发明涉及使用式（I）的喹唑啉衍生物，其中Q1包括任选被诸如卤代，三氟甲基和氰基的基团取代的喹唑啉环，或下式的基团：Q 3 -X 1，其中X 1包括直接键和O和Q3包括芳基，芳基 - （1-6C）烷基，杂环基和杂环基 - （1-6C）烷基; R2和R3各自为氢或（1-6C）烷基; Z包括O，S和NH; 和Q2包括芳基和芳基 - （1-3C）烷基或其药学上可接受的盐在制备用于在温血动物中产生抗血管生成和/或血管通透性降低作用的药物中，例如一个人。

7. 发明授权

US07115615B2 Quinazoline derivatives 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US07115615B2
公开(公告)日：2006-10-03
申请号：US10344678
申请日：2001-08-15
申请人： Laurent Francois Andre Hennequin , Patrick Ple , Christine Marie Paul Lambert
发明人： Laurent Francois Andre Hennequin , Patrick Ple , Christine Marie Paul Lambert
IPC分类号： A01N43/54 , A61K31/517 , A61K31/535 , C07D239/70 , C07D413/00 , C07D419/00
CPC分类号： C07D405/12 , C07D405/14
摘要： The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物，其中m，R 1，n，R 2和R 3 3中的每一个具有描述中定义的含义; 其制备方法，含有它们的药物组合物及其在制备用作在实体瘤疾病的遏制和/或治疗中作为抗侵入剂的药物的用途。

8. 发明授权

US07049438B2 Quinazoline derivatives for treatment of tumours 有权
标题翻译：喹唑啉衍生物治疗肿瘤
公开(公告)号：US07049438B2
公开(公告)日：2006-05-23
申请号：US10275382
申请日：2001-06-01
申请人： Laurent François André Hennequin , Patrick Ple
发明人： Laurent François André Hennequin , Patrick Ple
IPC分类号： C07D239/72 , A01N43/54
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/12 , C07D405/12 , C07D405/14
摘要： The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease
摘要翻译：本发明涉及式（I）的喹唑啉衍生物，其中Q 1，Z，m，R 1，R 2，R 2， > 3＆gt;和＆lt; 2＆gt; 2具有在说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于在遏制和/或治疗实体瘤疾病中作为抗侵入剂的药物的用途

9. 发明授权

US08569298B2 Pyridine compounds 有权
标题翻译：吡啶化合物
公开(公告)号：US08569298B2
公开(公告)日：2013-10-29
申请号：US12999025
申请日：2009-06-15
申请人： Bernard Christophe Barlaam , Patrick Ple , Kevin Michael Foote , Clifford David Jones
发明人： Bernard Christophe Barlaam , Patrick Ple , Kevin Michael Foote , Clifford David Jones
IPC分类号： C07D217/24 , C07D401/12 , A61K31/4709
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.
摘要翻译：本发明涉及抑制粘着斑激酶功能的化合物，其制备方法，含有它们作为活性成分的药物组合物，作为药物的用途，以及它们在制备用于温热治疗的药物中的用途，血液动物如人类的疾病如癌症。

10. 发明授权

US08530470B2 Chromenone derivatives 有权
标题翻译：色酮酮衍生物
公开(公告)号：US08530470B2
公开(公告)日：2013-09-10
申请号：US13444221
申请日：2012-04-11
申请人： Bernard Christophe Barlaam , Sebastien Louis Degorce , Christine Marie Paul Lambert-Van Der Brempt , Jean-Jacques Marcel Lohmann , Patrick Ple
发明人： Bernard Christophe Barlaam , Sebastien Louis Degorce , Christine Marie Paul Lambert-Van Der Brempt , Jean-Jacques Marcel Lohmann , Patrick Ple
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： C07D413/14 , A61K31/5377 , A61K31/715 , C07D417/14
摘要： The invention concerns chromenone compounds of Formula I; or pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, n and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
摘要翻译：本发明涉及式I的色烯酮化合物; 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，n和R 6中的每一个在本说明书中具有上文定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。

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