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1. 发明授权

US07384950B2 Thienopyrimidinediones and their use in the modulation of autoimmune disease 失效
标题翻译：噻吩并嘧啶二酮及其在调节自身免疫性疾病中的应用
公开(公告)号：US07384950B2
公开(公告)日：2008-06-10
申请号：US10483162
申请日：2002-07-24
申请人： Rachel Heulwen Reynolds , Anthony Howard Ingall , Rukhsana Tasneem Rasul , Simon David Guile , Martin Edward Cooper
发明人： Rachel Heulwen Reynolds , Anthony Howard Ingall , Rukhsana Tasneem Rasul , Simon David Guile , Martin Edward Cooper
IPC分类号： A61K31/519 , C07D495/04 , A61P11/06
CPC分类号： C07D495/04
摘要： The invention relates to a compound of formula (1); wherein: R1 and R2 each independently represent a C1-6alkyl, C3-6 alkenyl, C3-6 cycloalkyl C1-3 alkyl or C3-6 cycloalkyl; each of which may be optionally substituted by 1 to 3 halogen atoms; R3 is isoxyzolidin-2-ylcarbonyl or tetrahydroisoxazin-2-ylcarbonyl wherein each ring is optionally substituted by one hydroxy group; Q is CO— or C(R4)(R5)-(wherein R4 is a hydrogen atom or C1-4alkyl and R5 is a hydrogen atom or hydroxy group); Ar is a 5- to 10-membered aromatic ring system wherein up to 4 ring atoms may be heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted by one or more substituents as defined in the specification. It also relates to methods of preparing, pharmaceutical compositions containing and methods of using the compound of the formula (1), particularly in the modulation of autoimmune disease
摘要翻译：本发明涉及式（1）的化合物; 其中：R 1和R 2各自独立地表示C 1-6烷基，C 3-6亚烷基，C 3-6环烷基C 1-3烷基或C 3-6环烷基; 其各自可以任选被1至3个卤素原子取代; R 3是异恶唑烷-2-基羰基或四氢异恶嗪-2-基羰基，其中每个环任选被一个羟基取代; Q是CO-或C（R 4）（R 5） - （其中R 4是氢原子或C 1 -4个烷基，R 5是氢原子或羟基）; Ar是5至10元芳族环系统，其中多达4个环原子可以是独立地选自氮，氧和硫的杂原子，该环系统任选地被一个或多个如说明书中定义的取代基取代。它还涉及制备方法，含药物组合物和使用式（1）化合物的方法，特别是调节自身免疫疾病

2. 发明申请

US20080207642A1 Thienopyrimidinediones and Their Use in the Modulation of Autoimmune Disease 审中-公开
标题翻译：噻吩并嘧啶二酮及其在自身免疫性疾病调控中的应用
公开(公告)号：US20080207642A1
公开(公告)日：2008-08-28
申请号：US12111792
申请日：2008-04-29
申请人： Rachel Heulwen Reynolds , Anthony Howard Ingall , Rukhsana Tasneem Rasul , Simon David Guile , Martin Edward Cooper
发明人： Rachel Heulwen Reynolds , Anthony Howard Ingall , Rukhsana Tasneem Rasul , Simon David Guile , Martin Edward Cooper
IPC分类号： A61K31/497 , A61K31/519 , A61P37/00 , A61P11/00 , A61P35/00
CPC分类号： C07D495/04
摘要： The invention relates to a compound of formula (1): in which R1 and R2 each independently represent a C1-6alkyl, C3-6alkenyl, C3-6cycloalkylC1-3alkyl or C3-6cycloalkyl; each of which is optionally substituted by 1 to 3 halogen atoms; R3 is isoxazolidin-2-ylcarbonyl or tetrahydroisoxazin-2-ylcarbonyl wherein each ring is optionally substituted by one hydroxy group; Q is —CO— or —C(R4)(R5)— in which R4 is a hydrogen atom or C1-4alkyl and R5 is a hydrogen atom or hydroxy group; and Ar is a 5- to 10-membered aromatic ring system in which up to 4 ring atoms may be heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulphur, the ring system being optionally substituted by one or more substituents as defined in the specification. It also relates to methods of preparing, pharmaceutical compositions containing and methods of using the compound of the formula (1), particularly in the modulation of autoimmune disease.
摘要翻译：本发明涉及式（1）的化合物：其中R 1和R 2各自独立地表示C 1-6烷基， C 3-6烯基，C 3-6环烷基C 1-3烷基或C 3-6环烷基; 它们各自任选被1至3个卤素原子取代; R 3是异恶唑烷-2-基羰基或四氢异恶嗪-2-基羰基，其中每个环任选被一个羟基取代; Q是-CO-或-C（R 4）（R 5） - ，其中R 4是氢原子或C _{1-4个烷基，R 5是氢原子或羟基; 并且Ar是5-至10-元芳族环系统，其中多达4个环原子可以是独立地选自氮，氧和硫的杂原子，所述环系统任选地被一个或多个如规格。它还涉及制备方法，含药物组合物和使用式（1）化合物的方法，特别是调节自身免疫性疾病。}

3. 发明授权

US07064126B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US07064126B2
公开(公告)日：2006-06-20
申请号：US10542194
申请日：2004-01-15
申请人： Martin Edward Cooper , Simon David Guile , Anthony Howard Ingall , Rukhsana Tasneem Rasul
发明人： Martin Edward Cooper , Simon David Guile , Anthony Howard Ingall , Rukhsana Tasneem Rasul
IPC分类号： C07D495/04 , A61K31/5025
CPC分类号： C07D495/04
摘要： The invention relates to thienopyridazinones of formula (I): wherein: R1 is C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl which is optionally substituted by C1-6 alkyl, each of the above being optionally substituted by one or more halogen atoms; R2 is C1-6 alkyl; R3 is a group CO—G or SO2—G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and C1-4 alkyl; Q is CR5R6 where R5 and R6 are as defined in the specification; and R4 is a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described.
摘要翻译：本发明涉及式（I）的噻吩并哒嗪酮：其中：R 1是C 1-6烷基，C 2-6链烯基或C 任选被C 1-6烷基取代的，任选被一个或多个卤素原子取代的C 3-6环烷基; R 2是C 1-6烷基; R 3是基团CO-G或SO 2 -G，其中G是含有氮原子的5-或6-元环，和选自氧和/ 硫邻近氮，并且任选地被多至3个选自羟基和C 1-4烷基的基团取代; Q是CR 5，其中R 5和R 6如说明书中所定义; 并且R 4是含有0至4个独立地选自氮，氧和硫的杂原子的5至10元单环或双环芳族环系统，所述环系统如上所述被任选地取代在本说明书及其药学上可接受的盐和溶剂化物中。还描述了其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是在调节自身免疫疾病中。

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