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

Applicant: CELLZOME LIMITED ,  ELLARD, Katie ,  MAJOR, Jeremy ,  JONES, Alison ,  LYNCH, Rosemary ,  RAMSDEN, Nigel

Inventor： ELLARD, Katie ,  MAJOR, Jeremy ,  JONES, Alison ,  LYNCH, Rosemary ,  RAMSDEN, Nigel

IPC: C07D239/42 ,  C07D403/12 ,  A61K31/505 ,  A61K31/506 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D239/42 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2010007100A1

公开(公告)日：2010-01-21

申请号：PCT/EP2009/059076

申请日：2009-07-15

Applicant: CELLZOME LTD ,  RAMSDEN, Nigel ,  BELL, Kathryn ,  CANSFIELD, Andrew ,  TAYLOR, Jess ,  SUNOSE, Mihiro ,  MIDDLEMISS, David ,  ELLARD, Katie

Inventor： RAMSDEN, Nigel ,  BELL, Kathryn ,  CANSFIELD, Andrew ,  TAYLOR, Jess ,  SUNOSE, Mihiro ,  MIDDLEMISS, David ,  ELLARD, Katie

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: The invention relates to compounds of formula (I) wherein T 1 and R 1 to R 3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, 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.

Abstract translation: 本发明涉及式（I）化合物，其中T1和R1至R3具有在说明书和权利要求书中引用的含义。 所述化合物可用作蛋白激酶抑制剂，特别是用于治疗或预防免疫学，炎症，自身免疫或过敏性疾病的PI3K抑制剂。 本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及制备和用作药物。

公开(公告)号：WO2008025822A1

公开(公告)日：2008-03-06

申请号：PCT/EP2007/059052

申请日：2007-08-30

Applicant: CELLZOME (UK) LTD. ,  WILSON, Francis ,  RAMSDEN, Nigel

Inventor： WILSON, Francis ,  RAMSDEN, Nigel

IPC: C07D487/04 ,  A61K31/5025 ,  A61K31/519 ,  A61P3/10 ,  A61P7/12 ,  A61P11/08 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P37/02 ,  A61P37/08

CPC classification number: C07D487/04

Abstract: The invention relates to compounds of formula (I) wherein A 1 , A 2 , X and R 1 to R 5 have the meaning as cited in the description and the claims. Said compounds are useful as Itk protein kinase inhibitors for the treatment or prophylaxis o f immunological, inflammatory 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.

Abstract translation: 本发明涉及式（I）的化合物，其中A 1，A 2，X和R 1至R 5， SUP>具有在说明书和权利要求中引用的含义。 所述化合物可用作Itk蛋白激酶抑制剂用于治疗或预防免疫学，炎症或过敏性疾病。 本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及制备和用作药物。

公开(公告)号：WO2013174895A1

公开(公告)日：2013-11-28

申请号：PCT/EP2013/060563

申请日：2013-05-23

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

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

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

CPC classification number: 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

Abstract: 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.

Abstract translation: 本发明涉及式（I）化合物，其中R，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。

公开(公告)号：WO2012022681A3

公开(公告)日：2013-01-31

申请号：PCT/EP2011063905

申请日：2011-08-12

Applicant: CELLZOME LTD ,  BELL KATHRYN ,  PITON NELLY ,  DAGOSTIN CLAUDIO ,  BOUSSARD CYRILLE ,  RATCLIFFE ANDREW ,  RAMSDEN NIGEL

Inventor： BELL KATHRYN ,  PITON NELLY ,  DAGOSTIN CLAUDIO ,  BOUSSARD CYRILLE ,  RATCLIFFE ANDREW ,  RAMSDEN NIGEL

IPC: C07D487/04 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D491/107 ,  C07D498/08 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R 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.

Abstract translation: 本发明涉及其中X1至X5，Y，Z1至Z3和R具有在说明书和权利要求书中引用的含义的式（I）化合物。 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。

公开(公告)号：WO2011029807A1

公开(公告)日：2011-03-17

申请号：PCT/EP2010/063077

申请日：2010-09-07

Applicant: CELLZOME LIMITED ,  HARRISON, Richard, John ,  HOBSON, Andrew ,  RAMSDEN, Nigel

Inventor： HARRISON, Richard, John ,  HOBSON, Andrew ,  RAMSDEN, Nigel

IPC: C07D239/48 ,  C07D403/12 ,  A61K31/505 ,  A61K31/506 ,  A61P37/00 ,  A61P35/00

CPC classification number: C07D403/12 ,  C07D239/48

Abstract: The present invention relates to compounds of formula (I), wherein X 1 to X 3 , R, R 2 to R 7 and AA 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.

Abstract translation: 本发明涉及式（I）化合物，其中X1至X3，R，R2至R7和AA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。

公开(公告)号：WO2010118986A1

公开(公告)日：2010-10-21

申请号：PCT/EP2010/054685

申请日：2010-04-09

Applicant: CELLZOME LIMITED ,  HARRISON, Richard John ,  HOBSON, Andrew ,  RAMSDEN, Nigel

Inventor： HARRISON, Richard John ,  HOBSON, Andrew ,  RAMSDEN, Nigel

IPC: C07D403/12 ,  C07D239/48 ,  C07D407/12 ,  A61K31/506 ,  A61K31/5377 ,  A61P35/00

CPC classification number: C07D407/12 ,  C07D239/48 ,  C07D403/12

Abstract: The present invention relates to compounds of formula (I) wherein AA, R 2 to R 7 and X 1 to X 3 have the meaning as cited in the description and the claims. Said compounds are useful as selective inhibitors of JAK3 over JAK2 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.

Abstract translation: 本发明涉及其中AA，R2至R7和X1至X3具有如在说明书和权利要求中引用的含义的式（I）化合物。 所述化合物可用作JAK3的选择性抑制剂，用于治疗或预防免疫学，炎性，自身免疫性，过敏性疾病和免疫介导的疾病。 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。

公开(公告)号：WO2009127642A2

公开(公告)日：2009-10-22

申请号：PCT/EP2009054436

申请日：2009-04-15

Applicant: CELLZOME LTD ,  RAMSDEN NIGEL

Inventor： RAMSDEN NIGEL

IPC: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61P25/28 ,  C07D403/12 ,  C07D413/12

CPC classification number: C07D403/12 ,  C07D239/48 ,  C07D413/12

Abstract: The invention relates to compounds of formula (I), wherein R1 to R9 and R4a have the meaning as cited in the description and the claims for use in a for use in a method of treating or preventing diseases and disorders associated with LRRK2. Said compounds are useful as inhibitors of LRRK2 for the treatment or prophylaxis of neurodegenerative diseases, like Parkinson's disease or Alzheimer's disease. The invention also relates to the preparation of such compounds.

Abstract translation: 本发明涉及式（I）化合物，其中R 1至R 9和R 4a具有在用于治疗或预防与LRRK2相关的疾病和病症的方法中的描述和权利要求中引用的含义。 所述化合物可用作LRRK2的抑制剂，用于治疗或预防神经变性疾病，如帕金森病或阿尔茨海默氏病。 本发明还涉及这些化合物的制备。

公开(公告)号：WO2009112490A1

公开(公告)日：2009-09-17

申请号：PCT/EP2009/052789

申请日：2009-03-10

Applicant: CELLZOME LIMITED ,  MAJOR, Jeremy ,  HARRISON, Richard, John ,  RAMSDEN, Nigel ,  MIDDLEMISS, David ,  KRUSE, Ulrich ,  DREWES, Gerard

Inventor： MAJOR, Jeremy ,  HARRISON, Richard, John ,  RAMSDEN, Nigel ,  MIDDLEMISS, David ,  KRUSE, Ulrich ,  DREWES, Gerard

IPC: C07D239/48 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D401/12 ,  C07D407/12 ,  A61K31/505 ,  A61K31/506 ,  A61K31/538 ,  A61K31/5377 ,  A61P37/06 ,  A61P37/08

CPC classification number: C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The invention relates to compounds of formula (I), wherein R 1 to R 9 and R 4a have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 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, the preparation of such compounds as well as the use as medicaments.

Abstract translation: 本发明涉及式（I）化合物，其中R1至R9和R4a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，这些化合物的制备以及作为药物的用途。

公开(公告)号：WO2009080638A3

公开(公告)日：2009-07-02

申请号：PCT/EP2008/067682

申请日：2008-12-17

Applicant: Cellzome Limited ,  HARRISON, Richard John ,  MAJOR, Jeremy ,  MIDDLEMISS, David ,  RAMSDEN, Nigel ,  KRUSE, Ulrich ,  DREWES, Gerard

Inventor： HARRISON, Richard John ,  MAJOR, Jeremy ,  MIDDLEMISS, David ,  RAMSDEN, Nigel ,  KRUSE, Ulrich ,  DREWES, Gerard

IPC: C07D239/48 ,  C07D403/14 ,  A61K31/505 ,  A61P37/00 ,  A61P29/00

Abstract: The invention relates to compounds of formula (I). Said compounds are useful as inhibitors of ZAP-70 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, the preparation of such compounds as well as the use as medicaments.