公开(公告)号：EP2021314A1

公开(公告)日：2009-02-11

申请号：EP07760976.6

申请日：2007-04-20

申请人： Ortho-McNeil Pharmaceutical, Inc. ,  Cellzome Limited

发明人： WILSON, Francis ,  REID, Alison ,  READER, Valerie ,  HARRISON, Richard John ,  SUNOSE, Mihiro ,  HERNADEZ-PERNI, Remedios ,  MAJOR, Jeremy ,  BOUSSARD, Cyrille ,  SMELT, Kathryn ,  TAYLOR, Jess ,  LEFORMAL, Adeline ,  CANSFIELD, Andrew ,  BURCKHARDT, Svenja ,  HO, Chih Yung ,  ZHANG, Yan

IPC分类号： C07C59/68 ,  C07C229/42 ,  A61K31/192 ,  A61K31/196 ,  A61P25/28

CPC分类号： C07C229/42 ,  C07C59/68

摘要： The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4 R9, and R10, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity, wherein A is O, NH, S; X is a bond or a group -CR5R6 Υ is a carboxy group -C(O)OH or a substituted or unsubstituted tetrazole group..

公开(公告)号：EP2016039A1

公开(公告)日：2009-01-21

申请号：EP07760900.6

申请日：2007-04-19

申请人： Ortho-McNeil Pharmaceutical, Inc. ,  Cellzome Limited

发明人： WILSON, Francis ,  REID, Alison ,  READER, Valerie ,  HARRISON, Richard, John ,  SUNOSE, Mihiro ,  HERNADEZ-PERNI, Remedios ,  MAJOR, Jeremy ,  BOUSSARD, Cyrille ,  SMELT, Kathryn ,  TAYLOR, Jess ,  LEFORMAL, Adeline ,  CANSFIELD, Andrew ,  BURCKHARDT, Svenja ,  ZHANG, Yan ,  HO, Chih Yung

IPC分类号： C07C51/09 ,  C07C57/38 ,  C07C57/58 ,  C07C59/64 ,  C07D257/04 ,  A61K31/192 ,  A61P25/28

CPC分类号： C07D257/04 ,  C07C51/09 ,  C07C57/38 ,  C07C57/58 ,  C07C59/56 ,  C07C59/64 ,  C07C63/331 ,  C07C69/65

摘要： The present invention relates to compounds having the general formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, R10 given below, and solvates, hydrates, esters, and pharmaceutically acceptable salts thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.

公开(公告)号：EP2057158B1

公开(公告)日：2015-08-12

申请号：EP07803060.8

申请日：2007-08-30

申请人： Cellzome Limited

发明人： WILSON, Francis ,  RAMSDEN, Nigel ,  BELL, Kathryn ,  CANSFIELD, Andrew ,  BURCKHARDT, Svenja ,  TAYLOR, Jess ,  SUNOSE, Mihiro ,  MIDDLEMISS, David

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P37/00 ,  A61P35/00

CPC分类号： C07D471/04

公开(公告)号：EP2855451A1

公开(公告)日：2015-04-08

申请号：EP13724816.7

申请日：2013-05-23

申请人： Cellzome Limited

发明人： HARRISON, Richard John ,  RAMSDEN, Nigel ,  MAJOR, Jeremy ,  MOREL, Adeline ,  CONVERY, Laura ,  SUNOSE, Mihiro ,  LYNCH, Rosemary ,  ADREGO, Rita ,  JONES, Alison

IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  A61K31/505 ,  A61P37/00

CPC分类号： A61K31/506 ,  A61K31/505 ,  A61K31/5377 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107

摘要： The present invention relates to compounds of formula (I), wherein R, R
1 , X
1 to X
5 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，R 1，X 1至X 5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，炎性，自身免疫性，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。

公开(公告)号：EP2758379A1

公开(公告)日：2014-07-30

申请号：EP12761738.9

申请日：2012-09-21

申请人： Cellzome Limited

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.

公开(公告)号：EP2222674A1

公开(公告)日：2010-09-01

申请号：EP08854698.1

申请日：2008-11-21

申请人： Cellzome Limited

发明人： RAMSDEN, Nigel ,  BELL, Kathryn ,  CANSFIELD, Andrew ,  TAYLOR, Jess ,  SUNOSE, Mihiro ,  MIDDLEMISS, David ,  NEUBAUER, Gitte

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P37/00

CPC分类号： C07D471/04

摘要： The invention relates to compounds of formula (I) Said compounds are useful as protein kinase inhibitors, especially inhibitors of P13K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.

公开(公告)号：EP1805129B1

公开(公告)日：2009-03-18

申请号：EP05799330.5

申请日：2005-10-21

申请人： Cellzome Limited

发明人： WILSON, Francis ,  REID, Alison ,  READER, Valerie ,  HARRISON, Richard, John ,  SUNOSE, Mihiro ,  HERNANDEZ-Perni, Remedios ,  MAJOR, Jeremy ,  BOUSSARD, Cyrille ,  SMELT, Kathryn ,  TAYLOR, Jess ,  LEFORMAL, Adeline ,  CANSFIELD, Andrew ,  BURCKHARDT, Svenja

IPC分类号： C07C59/68 ,  C07C59/72 ,  C07D295/22 ,  C07D261/08 ,  C07D309/06 ,  C07D295/18 ,  C07C235/34 ,  C07C311/17 ,  C07C317/22 ,  A61P25/28 ,  A61K31/192

CPC分类号： C07C59/68 ,  C07C59/72 ,  C07C233/54 ,  C07C235/42 ,  C07C311/29 ,  C07C317/22 ,  C07C317/46 ,  C07C2601/02 ,  C07C2601/14 ,  C07D261/08 ,  C07D295/192 ,  C07D295/26 ,  C07D309/06

摘要： The present invention relates to compounds having the general formula (I) with the definitions of A, X, R1-R6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of Ϝ-secretase activity.

公开(公告)号：EP2222674B1

公开(公告)日：2015-11-11

申请号：EP08854698.1

申请日：2008-11-21

申请人： Cellzome Limited

发明人： RAMSDEN, Nigel ,  BELL, Kathryn ,  CANSFIELD, Andrew ,  TAYLOR, Jess ,  SUNOSE, Mihiro ,  MIDDLEMISS, David ,  NEUBAUER, Gitte

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P37/00

CPC分类号： C07D471/04

公开(公告)号：EP2057158B8

公开(公告)日：2015-09-30

申请号：EP07803060.8

申请日：2007-08-30

申请人： Cellzome Limited

发明人： WILSON, Francis ,  RAMSDEN, Nigel ,  BELL, Kathryn ,  CANSFIELD, Andrew ,  BURCKHARDT, Svenja ,  TAYLOR, Jess ,  SUNOSE, Mihiro ,  MIDDLEMISS, David

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P37/00 ,  A61P35/00

CPC分类号： C07D471/04

公开(公告)号：EP2443106A1

公开(公告)日：2012-04-25

申请号：EP10725721.4

申请日：2010-06-17

申请人： Cellzome Limited

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.