公开(公告)号：US20080234319A1

公开(公告)日：2008-09-25

申请号：US12052908

申请日：2008-03-21

申请人： Simon David Guile ,  Mark Ebden

发明人： Simon David Guile ,  Mark Ebden

IPC分类号： A61K31/4709 ,  C07D401/04 ,  C07C211/17

CPC分类号： C07D401/04 ,  C07D403/04

摘要： The invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, wherein R1, R2, R3 and n are as defined in the specification

摘要翻译： 本发明提供式（I）化合物，其制备方法，含有它们的药物组合物，制备药物组合物的方法及其在治疗中的用途，其中R 1，R 2， ＆lt; / SUP＆gt;，R 3和n如说明书中所定义

公开(公告)号：US20080221131A1

公开(公告)日：2008-09-11

申请号：US12124319

申请日：2008-05-21

申请人： Simon David Guile

发明人： Simon David Guile

IPC分类号： A61K31/519 ,  A61P11/00 ,  A61P9/00 ,  A61P35/04

CPC分类号： C07D495/04

摘要： The invention relates to thienopyrimidinediones of formula (I): in which R1, R2, Q are as defined in the specification, and Ar and Ar2 are selected from certain aromatic ring systems which may be optionally substituted, as defined in the specification.Processes for the preparation of compounds of formula (I), pharmaceutical compositions containing them and their use in therapy are also described.

摘要翻译： 本发明涉及式（I）的噻吩并嘧啶二酮：其中R 1，R 2，Q如说明书中所定义，Ar和Ar < 选自某些芳族环系统，其可以任选地被取代，如说明书中所定义的。 还描述了制备式（I）化合物，含有它们的药物组合物及其在治疗中的用途的方法。

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

公开(公告)号：US20090143428A1

公开(公告)日：2009-06-04

申请号：US12324397

申请日：2008-11-26

申请人： Simon David Guile ,  Toby Thompson

发明人： Simon David Guile ,  Toby Thompson

IPC分类号： A61K31/4709 ,  C07D401/04 ,  A61P29/00

CPC分类号： C07D401/04

摘要： The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.

摘要翻译： 本发明提供了本说明书中定义的式（I）化合物，其制备方法，含有它的药物组合物，制备药物组合物的方法及其在治疗中的用途。

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。}

公开(公告)号：US20080214579A1

公开(公告)日：2008-09-04

申请号：US12115171

申请日：2008-05-05

申请人： Simon David Guile

发明人： Simon David Guile

IPC分类号： A61K31/519 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06

CPC分类号： C07D495/04

摘要： The invention relates to thienopyrimidinediones of formula (1): in which R1, R2, R3, Q, and Ar are defined in the specification. The invention also relates to processes for the preparation of the compounds of formula (1), pharmaceutical compositions containing these compounds, and use of these compounds in therapy, in particular in immunosuppression therapy.

摘要翻译： 本发明涉及式（1）的噻吩并嘧啶二酮：其中R 1，R 2，R 3，Q和Ar定义在 规格。 本发明还涉及制备式（1）化合物的方法，含有这些化合物的药物组合物，以及这些化合物在治疗中的用途，特别是在免疫抑制治疗中的用途。

公开(公告)号：US08106073B2

公开(公告)日：2012-01-31

申请号：US12324397

申请日：2008-11-26

申请人： Simon David Guile ,  Toby Thompson

发明人： Simon David Guile ,  Toby Thompson

IPC分类号： A01N43/42 ,  C07D215/44

CPC分类号： C07D401/04

摘要： The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.

摘要翻译： 本发明提供了本说明书中定义的式（I）化合物，其制备方法，含有它的药物组合物，制备药物组合物的方法及其在治疗中的用途。

公开(公告)号：US07964616B2

公开(公告)日：2011-06-21

申请号：US12052908

申请日：2008-03-21

申请人： Mark Ebden ,  Simon David Guile

发明人： Mark Ebden ,  Simon David Guile

IPC分类号： A61K31/04 ,  C07D215/38

CPC分类号： C07D401/04 ,  C07D403/04

摘要： The invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, wherein R1, R2, R3 and n are as defined in the specification

摘要翻译： 本发明提供式（I）化合物，其制备方法，含有它们的药物组合物，制备药物组合物的方法及其在治疗中的用途，其中R1，R2，R3和n如说明书中所定义

公开(公告)号：US07393854B2

公开(公告)日：2008-07-01

申请号：US10542457

申请日：2004-01-15

申请人： Simon David Guile ,  Anthony Howard Ingall

发明人： Simon David Guile ,  Anthony Howard Ingall

IPC分类号： A61K31/519 ,  C07D495/04 ,  A61P11/06

CPC分类号： C07D495/04

摘要： The invention relates to thienopyrimidinediones of formula (I): wherein: R1, R2, Q are as defined in the specification, and Ar and Ar2 are selected from certain aromatic ring systems which may be optionally substituted, as defined in the specification. Processes for the preparation of compounds of formula (I), pharmaceutical compositions containing them and their use in therapy are also described and claimed.

摘要翻译： 本发明涉及式（I）的噻吩并嘧啶二酮：其中：R 1，R 2，Q如说明书中所定义，Ar和Ar 2， 选自某些芳族环系统，其可以任选地被取代，如说明书中所定义的。 还描述和要求保护制备式（I）化合物的方法，含有它们的药物组合物及其在治疗中的用途。

公开(公告)号：US07384951B2

公开(公告)日：2008-06-10

申请号：US10542197

申请日：2004-01-15

申请人： Simon David Guile

发明人： Simon David Guile

IPC分类号： A61K31/519 ,  C07D496/04 ,  A61P11/06

CPC分类号： C07D495/04

摘要： The invention relates to thienopyrimidinediones of formula (1) wherein R1 and R2 each independently represent a C1-6alkyl, C3-6alkyl, C3-6alkenyl, C3-5cycloalkylC1-3alkyl or C3-6cycloalkyl; each of which may be optionally substituted by 1 to 3 halogen atoms 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; the ring being substituted by at least one group as defined in the specification, Q is CR4R5 where R4 is hydrogen, fluorine or C1-6 alkyl and R5 is hydrogen, fluorine or hydroxy; and Ar is a 5-10-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 groups defined in the specification; as well as pharmaccutically acceptable salts and solvates thereof. Processes for their preparation of the compounds, pharmaceutical compositions containing them and their use in therapy, in particular in immunosuppressive therapy are also described

摘要翻译： 本发明涉及式（1）的噻吩并嘧啶二酮，其中R 1和R 2各自独立地表示C 1-6烷基，C _{3-6个环烷基; 其中每个可以被1至3个卤素原子任选取代。R 3是基团CO-G或SO 2 -G，其中G是5-或6-元 环，其含有氮原子和与氮相邻的选自氧和硫的第二杂原子; 该环被说明书中定义的至少一个基团取代，Q是CR 4，其中R 4是氢，氟或 C 1-6烷基和R 5是氢，氟或羟基; 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，该环系统任选被说明书中定义的一个或多个基团取代; 以及其药学上可接受的盐和溶剂化物。 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，特别是在免疫抑制治疗中的用途}