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1. 发明申请

WO2007034173A1 PURINE DERIVATIVES FOR THE TREATMENT OF VIRAL OR ALLERGIC DISEASES AND CANCERS 审中-公开
标题翻译：用于治疗病毒或过敏性疾病和癌症的嘌呤衍生物
公开(公告)号：WO2007034173A1
公开(公告)日：2007-03-29
申请号：PCT/GB2006/003490
申请日：2006-09-20
申请人： ASTRAZENECA AB , DAINIPPON SUMITOMO PHARMA CO. LTD. , ASTRAZENECA UK LIMITED , ABBOTT, Philip , BONNERT, Roger, Victor , BROUGH, Stephen , CHOHAN, Kamaldeep , MCINALLY, Thomas , THOM, Stephen , ISOBE, Yoshiaki , NAKAMURA, Kei , TOJO, Shingo
发明人： ABBOTT, Philip , BONNERT, Roger, Victor , BROUGH, Stephen , CHOHAN, Kamaldeep , MCINALLY, Thomas , THOM, Stephen , ISOBE, Yoshiaki , NAKAMURA, Kei , TOJO, Shingo
IPC分类号： C07D473/34 , A61K31/495 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号： C07D473/34
摘要： The present invention provides compounds of (I) wherein R 1 , Y 1 , X 1 , Z 1 , X 2 , Y 2 , A, Y 3 , n, R and R 2 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）的化合物，其中R 1，Y 1，X 1，Z 1， X 2，Y 2，A，Y 3，n，R和R 2如在规格，其制备方法，含有它们的药物组合物及其在治疗中的用途。

2. 发明申请

WO2012066336A1 BENZYLAMINE COMPOUNDS AS TOLL -LIKE RECEPTOR 7 AGONISTS 审中-公开
标题翻译：苯并咪唑化合物作为TOLL-LIGER受体7激动剂
公开(公告)号：WO2012066336A1
公开(公告)日：2012-05-24
申请号：PCT/GB2011/052246
申请日：2011-11-17
申请人： ASTRAZENECA AB , DAINIPPON SUMITOMO PHARMA CO., LTD. , ASTRAZENECA UK LIMITED , MCINALLY, Thomas , MOCHEL, Tobias , HASEGAWA, Futoshi , HORI, Seiji
发明人： MCINALLY, Thomas , MOCHEL, Tobias , HASEGAWA, Futoshi , HORI, Seiji
IPC分类号： C07D239/49 , C07D403/10 , C07D403/12 , A61K31/505 , A61K31/506 , A61P31/12 , A61P35/00 , A61P37/00
CPC分类号： C07D239/49 , C07D403/10 , C07D403/12
摘要： The invention concerns compounds of Formula (I), and pharmaceutically acceptable salts thereof: where such compounds act as TLR7 agonists and at the same time show advantageous selectivity over TLR8 and hERG, wherein the variable groups R 1 , R 2 and n are as defined herein. The invention also relates to methods for the preparation of such compounds and intermediates useful in the preparation thereof, to pharmaceutical compositions containing such compounds, to the use of such compounds in the preparation of medicaments, and to the use of such compounds in the treatment of conditions mediated by TLR7, such as allergic diseases, autoimmune diseases, viral diseases and, in particular, cancer.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐：其中这些化合物作为TLR7激动剂，同时对TLR8和hERG显示有利的选择性，其中可变基团R1，R2和n如本文所定义。本发明还涉及用于制备这些化合物和中间体的方法，其可用于制备它们，含有这些化合物的药物组合物，以及这些化合物在制备药物中的用途，以及这些化合物在治疗中的用途 TLR7介导的病症，如过敏性疾病，自身免疫性疾病，病毒性疾病，特别是癌症。

3. 发明申请

WO2008114008A1 9-SUBSTITUTED-8-OXO-ADENINE COMPOUNDS AS TOLL-LIKE RECEPTOR (TLR7 ) MODULATORS 审中-公开
标题翻译：作为类似感受器（TLR7）调节剂的9-替代的8-氧 - 腺嘌呤化合物
公开(公告)号：WO2008114008A1
公开(公告)日：2008-09-25
申请号：PCT/GB2008/000958
申请日：2008-03-19
申请人： ASTRAZENECA AB , DAINIPPON SUMITOMO PHARMA CO., LTD. , ASTRAZENECA UK LIMITED , BONNERT, Roger, Victor , MCINALLY, Thomas , THOM, Stephen
发明人： BONNERT, Roger, Victor , MCINALLY, Thomas , THOM, Stephen
IPC分类号： C07D473/18 , A61K31/522 , A61P37/00
CPC分类号： C07D473/18
摘要： The present invention provides compounds of formula (I): wherein R 1 , Y 1 , X 1 , L and R 2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use as modulation of toll-like receptor (especially TLR7).
摘要翻译：本发明提供式（I）化合物：其中R 1，Y 1，X 1，L 2和R 2， / SUP>如本说明书中所定义，及其药学上可接受的盐，以及其制备方法，含有它们的药物组合物及其作为toll样受体（特别是TLR7）调节剂的用途。

4. 发明申请

WO2008114006A1 9-SUBSTITUTED-8-OXO-ADENINE COMPOUNDS AS TOLL-LIKE RECEPTOR (TLR7) MODULATORS 审中-公开
标题翻译：作为类似感受器（TLR7）调节剂的9-替代的8-氧 - 腺嘌呤化合物
公开(公告)号：WO2008114006A1
公开(公告)日：2008-09-25
申请号：PCT/GB2008/000952
申请日：2008-03-19
申请人： ASTRAZENECA AB , DAINIPPON SUMITOMO PHARMA CO., LTD. , ASTRAZENECA UK LIMITED , BONNERT, Roger, Victor , MCINALLY, Thomas , THOM, Stephen
发明人： BONNERT, Roger, Victor , MCINALLY, Thomas , THOM, Stephen
IPC分类号： C07D473/18 , A61K31/522 , A61P37/00
CPC分类号： C07D473/18
摘要： The present invention provides compounds of formula (I), where n, R 1 , R 2 , A, X 1 , Y 1 , Z 1 , X 2 and Y 2 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，其中n，R 1，R 2，A，X 1，Y 2， 1，Z 1，X 2和Y 2如说明书中所定义，其制备方法，含有他们和他们在治疗中的用途。

5. 发明申请

WO2010133885A1 NOVEL PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND FURTHER DISEASES 审中-公开
标题翻译：新型吡嗪衍生物及其在治疗癌症和进一步疾病中的应用
公开(公告)号：WO2010133885A1
公开(公告)日：2010-11-25
申请号：PCT/GB2010/050825
申请日：2010-05-20
申请人： ASTRAZENECA AB , DAINIPPON SUMITOMO PHARMA CO., LTD , ASTRAZENECA UK LIMITED , BENNETT, Nicholas, James , MCINALLY, Thomas , THOM, Stephen
发明人： BENNETT, Nicholas, James , MCINALLY, Thomas , THOM, Stephen
IPC分类号： C07D239/49 , C07D401/12 , C07D403/12 , C07D413/12 , A61K31/505 , A61K31/5377 , A61P35/00
CPC分类号： C07D413/12 , C07D239/48 , C07D239/49
摘要： The invention concerns compounds of Formula (I): wherein L 1 , R 1 , R 2 , R 3 , R 4 and X are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.
摘要翻译：本发明涉及式（I）的化合物：其中L1，R1，R2，R3，R4和X如说明书中所定义。本发明还涉及制备这些化合物的方法，含有它们的药物组合物及其在治疗疾病中的用途，例如癌症。

6. 发明申请

WO2010133882A1 DISACCHARIN, DIFUMARIC ACID, DI-L-HYDROXY-2-NAPHTHOIC ACID AND MONO-BENZOIC ACID SALTS OF 4- (DIMETHYLAMIN0)BUTYL 2- (4- ( (2-AMINO-4-METHYL-6- (PENTYLAMINO) PYRIMIDIN- 5 -YL) METHYL) PHENYL)ACETATE 审中-公开
标题翻译： 4-（二甲基氨基）丁基2-（4 - （（2-氨基-4-甲基-6-（戊基氨基）吡啶） - 酮的异丙酸，二油酸，DI-L-羟基-2-萘甲酸和单羟基酸， 5 -YL）甲基）苯基）乙酸酯
公开(公告)号：WO2010133882A1
公开(公告)日：2010-11-25
申请号：PCT/GB2010/050822
申请日：2010-05-20
申请人： ASTRAZENECA AB , DAINIPPON SUMITOMO PHARMA CO., LTD. , ASTRAZENECA UK LIMITED , BENNETT, Nicholas, James , MCINALLY, Thomas , PIMM, Austen , THOM, Stephen , ISOBE, Yoshiaki
发明人： BENNETT, Nicholas, James , MCINALLY, Thomas , PIMM, Austen , THOM, Stephen , ISOBE, Yoshiaki
IPC分类号： C07D239/49 , A61K31/505 , A61P11/00 , A61P17/00 , A61P27/14 , A61P31/00 , A61P35/00
CPC分类号： C07D239/49 , C07D275/06
摘要： The invention provides salts of 4- (dimethylamino) butyl 2- (4- ( (2-amino-4-methyl-6- (pentylamino) pyrimidin-5-yl ) methyl ) phenyl ) acetate (compound (I)), pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供2-（4-（（2-氨基-4-甲基-6-（戊基氨基）嘧啶-5-基）甲基）苯基）乙酸4-（二甲基氨基）丁酯（化合物（I）），药物含有它们的组合物及其在治疗中的用途。

7. 发明申请

WO2008135791A1 IMIDAZOQUINOLINES WITH IMMUNO-MODULATING PROPERTIES 审中-公开
标题翻译：具有免疫调节特性的咪唑啉
公开(公告)号：WO2008135791A1
公开(公告)日：2008-11-13
申请号：PCT/GB2008/050328
申请日：2008-05-06
申请人： ASTRAZENECA AB , DAINIPPON SUMITOMO PHARMA CO. LTD. , ASTRAZENECA UK LIMITED , BONNERT, Roger, Victor , MCINALLY, Thomas , THOM, Stephen
发明人： BONNERT, Roger, Victor , MCINALLY, Thomas , THOM, Stephen
IPC分类号： C07D471/04 , A61K31/437 , A61P37/02
CPC分类号： C07D471/04
摘要： The present invention provides compounds of formula (I) wherein R a , R 1 , R 2 , R 3 , X 1 , Y 1 , Z 1 , A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as 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，其中R 1，R 2，R 2，R 3，，X 1，Y 1，Z 1，A，n和m如说明书中所定义，及其药学上可接受的盐，如以及其制备方法，含有它们的药物组合物及其在治疗中的用途。

8. 发明申请

WO1997014686A1 PHARMACEUTICALLY ACTIVE QUINAZOLINE COMPOUNDS 审中-公开
标题翻译：药物活性喹唑啉化合物
公开(公告)号：WO1997014686A1
公开(公告)日：1997-04-24
申请号：PCT/GB1996002496
申请日：1996-10-14
申请人： ASTRA PHARMACEUTICALS LIMITED , HAMLEY, Peter, Richard, John , PIMM, Austen, David , TINKER, Alan, Charles , BEATON, Haydn, Graham , McINALLY, Thomas
发明人： ASTRA PHARMACEUTICALS LIMITED
IPC分类号： C07D239/94
CPC分类号： C07D401/04 , C07D239/70 , C07D239/94 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04 , C07D471/10 , C07D487/10 , C07F7/0812
摘要： Compounds of formula (I) wherein R and R independently represent hydrogen, alkyl C1 to 6, alkoxy C1 to 6, alkylthio C1 to 6, halogen, hydroxyl or amino; R represent H or alkyl; R represents phenyl, a 6-membered heterocyclic aromatic ring containing one or two nitrogen atoms, or a 5-membered heterocylic aromatic ring containing 1 to 3 heteroatoms selected from O, N and S, which phenyl or heterocyclic aromatic ring may be optionally substituted by alkyl C1 to 6, alkoxy C1 to 6, halogen, hydroxyl, alkylthio C1 to 6, cyano, trifluoromethyl, nitro, hydroxymethyl, amino, a group -(CH2)c.NHCO2R , a group -(CH2)c.NR R , or a group -CO2R , or R represents hydrogen or alkyl C1 to 8, which alkyl group may be optionally susbtituted by amino or a group -NHCO2R ; and R represents hydrogen or alkyl C1 to 6; or R and R taken together represent a group (CH2)a.Z.(CH2)b; c represents an integer 0 to 2; and pharmaceutically acceptable salts thereof, have been found to be useful as a pharmaceuticals. The compounds may especially be used in the treatment of inflammatory disorders.
摘要翻译：式（I）的化合物，其中R 1和R 19独立地表示氢，C 1-6烷基，烷氧基C 1-6，烷硫基C 1-6，卤素，羟基或氨基; R 2表示H或烷基; R 3表示苯基，含有一个或两个氮原子的6元杂环芳环，或含有1至3个选自O，N和S的杂原子的5元杂芳环，该苯基或杂环芳环可以是任选被C1至6的烷基，烷氧基C1至6，卤素，羟基，烷硫基C1至6，氰基，三氟甲基，硝基，羟甲基，氨基， - （CH2）c.NHCO2R10， - （CH2 ）c.NR 5 R 6或基团-CO 2 R 11或R 3表示氢或C1至8的烷基，该烷基可以任选地被氨基或基团-NHCO 2 R 10取代 >; 且R 4表示氢或C1至6的烷基; 或R 3和R 4一起表示基团（CH 2）a.Z.（CH 2）b; c表示0〜2的整数，已经发现其药学上可接受的盐可用作药物。该化合物可特别用于治疗炎症性疾病。

9. 发明申请

WO1992014714A1 SUBSTITUTED PYRIDINONES AND PYRIMIDINONES AS ANGIOTENSIN II ANTAGONISTS 审中-公开
标题翻译：取代的吡啶酮和吡啶酮作为血管紧张素Ⅱ拮抗剂
公开(公告)号：WO1992014714A1
公开(公告)日：1992-09-03
申请号：PCT/GB1992000280
申请日：1992-02-17
申请人： FISONS PLC , BANTICK, John, Raymond , McINALLY, Thomas , TINKER, Alan, Charles , HIRST, Simon, Christopher
发明人： FISONS PLC
IPC分类号： C07D239/36
CPC分类号： C07D213/64 , C07D213/69 , C07D213/80 , C07D213/82 , C07D215/22 , C07D239/36 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/06 , C07D405/14
摘要： There are described substituted heterocycles of general formula (I), which are useful as angiotensin II antagonists. There are also described methods for making the compounds and pharmaceutical formulations, e.g. for the treatment of hypertension, comprising them.

10. 发明申请

WO2012080728A1 IMIDAZO [4, 5 -C] QUINOLIN- 1 -YL DERIVATIVE USEFUL IN THERAPY 审中-公开
标题翻译：咪唑并[4,5-C]喹啉-1-基衍生物用于治疗
公开(公告)号：WO2012080728A1
公开(公告)日：2012-06-21
申请号：PCT/GB2011/052474
申请日：2011-12-14
申请人： ASTRAZENECA AB , DAINIPPON SUMITOMO PHARMA CO., LTD , ASTRAZENECA UK LIMITED , MCINALLY, Thomas , PIMM, Austen
发明人： MCINALLY, Thomas , PIMM, Austen
IPC分类号： C07D471/04 , A61K31/4188 , A61K31/4745 , A61P11/06 , A61P17/06 , A61P37/08 , A61P17/04 , A61P17/12 , A61P31/12 , A61P31/18 , A61P31/04 , A61P1/16
CPC分类号： C07D471/04
摘要： The invention provides the compound of formula (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound 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，其含有该化合物的药物组合物和该化合物在治疗中的用途。

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