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1. 发明申请

WO2013050508A1 MORPHOLINO SUBSTITUTED BICYCLIC PYRIMIDINE UREA OR CARBAMATE DERIVATIVES AS MTOR INHIBITORS 审中-公开
标题翻译：作为MTOR抑制剂的吗啉取代的双环PYRIMIDINE UREA或碳酸酯衍生物
公开(公告)号：WO2013050508A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069676
申请日：2012-10-05
申请人： CELLZOME LIMITED , LYNCH, Rosemary , CANSFIELD, Andrew David , HARDY, Daniel Paul , FEUTRILL, John Thomas , ADREGO, Rita , ELLARD, Katie , LADDUWAHETTY, Tammy
发明人： LYNCH, Rosemary , CANSFIELD, Andrew David , HARDY, Daniel Paul , FEUTRILL, John Thomas , ADREGO, Rita , ELLARD, Katie , LADDUWAHETTY, Tammy
IPC分类号： C07D417/02 , A61K31/519
CPC分类号： C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/5386 , C07D417/02 , C07D498/08
摘要： The invention relates to compounds of formula (I) wherein m, o, R a , R b , R 1 and T 1 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）的化合物，其中m，o，Ra，Rb，R1和T1具有在说明书和权利要求书中引用的含义。所述化合物可用作mTOR的抑制剂，用于治疗或预防mTOR相关疾病和病症。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

2. 发明申请

WO2012136622A1 DIHYDROPYRROLO PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS 审中-公开
标题翻译：二氢吡咯烷酮衍生物作为MTOR抑制剂
公开(公告)号：WO2012136622A1
公开(公告)日：2012-10-11
申请号：PCT/EP2012/055953
申请日：2012-04-02
申请人： CELLZOME LIMITED , LYNCH, Rosemary , CANSFIELD, Andrew, David , HARDY, Daniel, Paul , SCANLON, Jane, Elizabeth , ADREGO, Rita
发明人： LYNCH, Rosemary , CANSFIELD, Andrew, David , HARDY, Daniel, Paul , SCANLON, Jane, Elizabeth , ADREGO, Rita
IPC分类号： C07D487/04 , A61K31/519 , A61P37/00 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to compounds of formula (I), wherein X, R 1 , R 2 , T 0 , o have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中X，R1，R2，T0，o具有在说明书和权利要求书中引用的含义。所述化合物可用作mTOR的抑制剂，用于治疗或预防mTOR相关疾病和病症。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

3. 发明申请

WO2012062704A1 PYRIDINE COMPOUNDS AND AZA ANALOGUES THEREOF AS TYK2 INHIBITORS 审中-公开
标题翻译：吡啶化合物和作为TYK2抑制剂的AZA类似物
公开(公告)号：WO2012062704A1
公开(公告)日：2012-05-18
申请号：PCT/EP2011/069553
申请日：2011-11-07
申请人： CELLZOME LIMITED , ELLARD, Katie , MAJOR, Jeremy , JONES, Alison , LYNCH, Rosemary , RAMSDEN, Nigel
发明人： ELLARD, Katie , MAJOR, Jeremy , JONES, Alison , LYNCH, Rosemary , RAMSDEN, Nigel
IPC分类号： C07D239/42 , C07D403/12 , A61K31/505 , A61K31/506 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D239/42 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of formula (I), wherein R 1 to R 3 , X 1 , X 2 have the meaning as cited in the description and the claims. Said compounds are useful as TYK2 inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as their use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R 1至R 3，X 1，X 2具有在说明书和权利要求书中引用的含义。所述化合物可用作治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫介导的疾病的TYK2抑制剂。本发明还涉及包含所述化合物的药物组合物以及它们作为药物的用途。

4. 发明申请

WO2010146133A1 HETEROCYCLYLAMINOPYRIMIDINES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的杂环亚氨基嘧啶
公开(公告)号：WO2010146133A1
公开(公告)日：2010-12-23
申请号：PCT/EP2010/058574
申请日：2010-06-17
申请人： CELLZOME LIMITED , SUNOSE, Mihiro , MAJOR, Jeremy , HARRISON, Richard, John , FREEMAN, Jay , MOREL, Adeline
发明人： SUNOSE, Mihiro , MAJOR, Jeremy , HARRISON, Richard, John , FREEMAN, Jay , MOREL, Adeline
IPC分类号： C07D403/12 , C07D413/12 , A61K31/506 , A61P37/00 , A61P29/00
CPC分类号： C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I), wherein R 1 to R 6 and T 0 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70, Syk or JAK3 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R1至R6和T0具有在说明书和权利要求书中引用的含义。所述化合物可用作ZAP-70，Syk或JAK3的抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病，免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

5. 发明申请

WO2013092854A1 PYRIMIDINE-2,4-DIAMINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：嘧啶-2,4-二胺衍生物作为激酶抑制剂
公开(公告)号：WO2013092854A1
公开(公告)日：2013-06-27
申请号：PCT/EP2012/076371
申请日：2012-12-20
申请人： CELLZOME LIMITED , HOBSON, Andrew , ADDISON, Glynn , RAMSDEN, Nigel , HARRISON, John
发明人： HOBSON, Andrew , ADDISON, Glynn , RAMSDEN, Nigel , HARRISON, John
IPC分类号： C07D403/14 , A61K31/506 , A61P35/00 , A61P37/00
CPC分类号： C07D413/14 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The present invention relates to compounds of formula (I) wherein X, R, Y 0 , T 0A , T 0B have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immuno logically-mediated diseases. The invention also relates to pharmaceutical compositions including said compoundsand their use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中X，R，Y0，T0A，T0B具有在说明书和权利要求书中引用的含义。所述化合物可用作JAK抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫逻辑介导的疾病。本发明还涉及包含所述化合物的药物组合物及其作为药物的用途。

6. 发明申请

WO2013041652A1 MORPHOLINO SUBSTITUTED UREA OR CARBAMATE DERIVATIVES AS MTOR INHIBITORS 审中-公开
标题翻译：作为MTOR抑制剂的吗啉取代的尿素或碳酸酯衍生物
公开(公告)号：WO2013041652A1
公开(公告)日：2013-03-28
申请号：PCT/EP2012/068590
申请日：2012-09-21
申请人： CELLZOME LIMITED , LYNCH, Rosemary , CANSFIELD, Andrew David , HARDY, Daniel Paul , SUNOSE, Mihiro , MOREL, Adeline , CONVERY, Laura , ADREGO, Rita
发明人： LYNCH, Rosemary , CANSFIELD, Andrew David , HARDY, Daniel Paul , SUNOSE, Mihiro , MOREL, Adeline , CONVERY, Laura , ADREGO, Rita
IPC分类号： C07D251/22 , C07D401/12 , C07D407/12 , C07D413/04 , A61K31/53 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P35/00
CPC分类号： C07D498/08 , C07D251/22 , C07D401/12 , C07D407/12 , C07D413/04 , C07D413/14
摘要： The invention relates to compounds of formula (I), wherein m, n, R 1 , T 0 and T 1 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中m，n，R 1，T 0和T 1具有在说明书和权利要求书中引用的含义。所述化合物可用作mTOR的抑制剂，用于治疗或预防mTOR相关疾病和病症。本发明还涉及包含所述化合物的药物组合物以及作为药物的用途。

7. 发明申请

WO2013041407A1 HYDROXAMIC ACIDS AS HDAC6 INHIBITORS 审中-公开
标题翻译：羟基酸作为HDAC6抑制剂
公开(公告)号：WO2013041407A1
公开(公告)日：2013-03-28
申请号：PCT/EP2012/067721
申请日：2012-09-11
申请人： CELLZOME AG , CELLZOME LIMITED , RAMSDEN, Nigel , BELL, Kathryn
发明人： RAMSDEN, Nigel , BELL, Kathryn
IPC分类号： A61K31/166 , C07D209/18 , C07D215/14 , A61P37/00
CPC分类号： A61K31/166 , C07C259/06 , C07C311/08 , C07C311/13 , C07C311/17 , C07D209/08 , C07D209/18 , C07D217/04
摘要： A hydroxamic acid of formula (I) or a pharmaceutically acceptable salt thereof for use in a method for treating or preventing an immunological, inflammatory, autoimmune or allergic disorder or disease, or a transplant rejection, or a graft-versus host disease, or a neurogenerative disease, or neuron injury, where the symbols in formula (I) have the following meanings: X is aryl, heteroaryl, cycloalkyl or heterocyclyl, any of which is unsubstituted or substituted, or H; L is C 1 -C 14 saturated alkylene or C 2 -C 8 -alkenylene, wherein the alkylene or alkenylene is unsubstituted or substituted, wherein one or two of the carbon atoms of the alkylene or alkenylene is replaced by NR', R' being hydrogen, alkyl, acyl, hydrogen, arylalkyl or, together with R, is (C 1 -C 3 )-alkylene, and wherein one or two of the carbon atoms of the alkylene or alkenylene is optionally replaced with O, S, S(O), S(O)2 or C(O); and R is H or, together with R', (C 1 -C 3 )-alkylene.
摘要翻译：用于治疗或预防免疫，炎症，自身免疫或过敏性疾病或疾病或移植排斥或移植物抗宿主病的方法中的式（I）的异羟肟酸或其药学上可接受的盐，或神经元损伤，其中式（I）中的符号具有以下含义：X是芳基，杂芳基，环烷基或杂环基，其中任何一个是未取代或取代的，或H; L是C1-C14饱和亚烷基或C2-C8-亚烯基，其中亚烷基或亚烯基是未取代或取代的，其中亚烷基或亚烯基的一个或两个碳原子被NR'取代，R'是氢，烷基，酰基，氢，芳基烷基或与R一起为（C 1 -C 3） - 亚烷基，并且其中亚烷基或亚烯基的一个或两个碳原子任选被O，S，S（O），S（O ）2或C（O）; 并且R是H或与R'，（C 1 -C 3） - 亚烷基一起。

8. 发明申请

WO2012143320A1 (7H-PYRROLO[2,3-D]PYRIMIDIN-2-YL)AMINE COMPOUNDS AS JAK3 INHIBITORS 审中-公开
标题翻译：（7H-吡咯并[2,3-D]嘧啶-2-基）胺化合物作为JAK3抑制剂
公开(公告)号：WO2012143320A1
公开(公告)日：2012-10-26
申请号：PCT/EP2012/056887
申请日：2012-04-16
申请人： CELLZOME LIMITED , OXENFORD, Sally , HOBSON, Andrew , OLIVER, Kathryn , RAMSDEN, Nigel
发明人： OXENFORD, Sally , HOBSON, Andrew , OLIVER, Kathryn , RAMSDEN, Nigel
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P37/06 , A61P35/00 , A61P37/08
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I) wherein X 1 to X 5 , Y, and Z 1 to Z 3 have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）的化合物，其中X 1至X 5，Y和Z 1至Z 3具有在说明书和权利要求书中引用的含义。所述化合物可用作JAK抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

9. 发明申请

WO2012000970A1 TRIAZOLOPYRIDINES AS TYK2 INHIBITORS 审中-公开
标题翻译：作为TYK2抑制剂的三唑并吡啶
公开(公告)号：WO2012000970A1
公开(公告)日：2012-01-05
申请号：PCT/EP2011/060777
申请日：2011-06-28
申请人： CELLZOME LIMITED , ELLARD, Katie , RAMSDEN, Nigel
发明人： ELLARD, Katie , RAMSDEN, Nigel
IPC分类号： A61K31/4196 , C07D249/20 , A61P37/02 , A61P37/08 , A61P37/06 , A61P35/00
CPC分类号： C07D471/04 , A61K31/4196 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of Formula (I), wherein R 1 to R 6 have the meaning as cited in the description and the claims. Said compounds are useful as TYK2 inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immuno logically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as their use as medicaments.
摘要翻译：本发明涉及式（I）的化合物，其中R 1至R 6具有在说明书和权利要求书中引用的含义。所述化合物可用作治疗或预防免疫，炎症，自身免疫，过敏性疾病和免疫逻辑介导的疾病的TYK2抑制剂。本发明还涉及包含所述化合物的药物组合物以及它们作为药物的用途。

10. 发明申请

WO2011134831A1 PYRAZOLE COMPOUNDS AS JAK INHIBITORS 审中-公开
标题翻译：吡咯化合物作为JAK抑制剂
公开(公告)号：WO2011134831A1
公开(公告)日：2011-11-03
申请号：PCT/EP2011/056158
申请日：2011-04-18
申请人： CELLZOME LIMITED , HARRISON, Richard, John , OXENFORD, Sally , HOBSON, Andrew , RAMSDEN, Nigel , MILLER, Warren
发明人： HARRISON, Richard, John , OXENFORD, Sally , HOBSON, Andrew , RAMSDEN, Nigel , MILLER, Warren
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P29/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I), wherein R 1 , R 2 , R 1a , R 1b have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R1，R2，R1a，R1b具有在说明书和权利要求书中引用的含义。所述化合物可用作JAK抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

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