公开(公告)号：WO2022128849A1

公开(公告)日：2022-06-23

申请号：PCT/EP2021/085376

申请日：2021-12-13

Applicant: GALAPAGOS NV

Inventor： LÉPINE, Renaud, Henri, Marcel ,  SCHILS, Didier, Philippe, Robert ,  CORVELEYN, Sam Bob ,  LYNCH, Michael, Anthony ,  LEBLANC, Nicolas, Valentin ,  DULOS, Gradus Johannes

IPC: C07D403/06 ,  A61K31/496 ,  A61P19/00

Abstract: The present invention relates to solid forms of (5S)-cyclopropyl-5-[3-[(3S)-4-(3,5-difluorophenyl)-3-methyl-piperazin-1-yl]-3-oxo-propyl]imidazolidine-2,4-dione and to pharmaceutical preparations comprising them and methods of their manufacture, as well as the use of said solid forms or preparations for the prophylaxis and/or treatment of inflammatory conditions, muscular disease, fibrotic diseases, viral infection, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis, especially osteoarthritis.

公开(公告)号：WO2019171267A1

公开(公告)日：2019-09-12

申请号：PCT/IB2019/051761

申请日：2019-03-05

Applicant: GALAPAGOS NV ,  MORPHOSYS AG

Inventor： VANDEGHINSTE, Nick Ernest René ,  EYERICH, Kilian Georg ,  LAUFFER, Felix Josef

IPC: C07K16/24

Abstract: The present invention relates to the use of an antibody or antibody fragment specific for IL-17C in the prophylaxis and/or treatment of autoimmune skin diseases. In one embodiment, the antibody or antibody fragment specific for IL-17C comprises a HCDR1 region of amino acid sequence SEQ ID NO: 7, a HCDR2 region of amino acid sequence SEQ ID NO: 8, a HCDR3 region of amino acid sequence of SEQ ID NO: 9, a LCDR1 region of amino acid sequence SEQ ID NO: 13, a LCDR2 region of amino acid sequence of SEQ ID NO: 14 and a LCDR3 region of amino acid sequence SEQ ID NO: 15. In another embodiment, the antibody or antibody fragment specific for IL-17C comprises a variable heavy chain of SEQ ID NO: 17 and a variable light chain of SEQ ID NO: 16. In some embodiments the autoimmune skin disease is selected from pemphigus vulgaris, bullous pemphigoid, vasculitis, pyoderma gangrenosum and Sweet's disease.

公开(公告)号：WO2019105886A1

公开(公告)日：2019-06-06

申请号：PCT/EP2018/082537

申请日：2018-11-26

Applicant: GALAPAGOS NV

Inventor： ALVEY, Luke, Jonathan ,  ANNOOT, Denis, Maurice ,  BONNATERRE, Florence, Marie-Emilie ,  BUCHER, Denis ,  DUTHION, Béranger ,  JARY, Hélène ,  PEIXOTO, Christophe ,  TEMAL-LAIB, Taoues ,  TIRERA, Amynata

IPC: C07D403/04 ,  C07D471/04 ,  A61K31/437 ,  A61P9/00 ,  A61P37/00

Abstract: The present invention discloses compounds according to Formula (I): wherein R 1 , R 2 , R 3a , R 3b , X, Y 1 , Y 2 , Y 3 , and Z are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of TNFα, interferons, IL-6, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

公开(公告)号：WO2019030275A1

公开(公告)日：2019-02-14

申请号：PCT/EP2018/071487

申请日：2018-08-08

Applicant: GALAPAGOS NV

Inventor： VAN DER AAR, Elisabeth, Martina ,  VAN DE STEEN, Olivier, Frans, Jozef, Maria

IPC: G16H20/10 ,  G16H30/40 ,  G16H50/50 ,  A61B6/03 ,  A61K31/5025 ,  C07D471/04

Abstract: GAL-289-PCT 37 ABSTRACT The present invention relates to the use of the compound according to Formula I in the prophylaxis and/or treatment of fibrotic diseases, more particularly idiopathic pulmonary fibrosis.

公开(公告)号：WO2019012284A1

公开(公告)日：2019-01-17

申请号：PCT/GB2018/051983

申请日：2018-07-12

Applicant: GALAPAGOS NV ,  CALCHAN LIMITED

Inventor： AMANTINI, David ,  MESIC, Milan ,  SAXTY, Gordon ,  POLJAK, Tanja ,  VUJASINOVIC, Ines ,  ZIHER, Dinko ,  WITTY, David ,  GIBSON, Karl Richard

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61P9/00 ,  A61P25/04 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00

Abstract: The present invention relates to pyrrolopyrimidine compounds according to Formula (I) and their use in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. In a particular aspect, the present compounds are ASK inhibitors, particularly ASK1 inhibitors. The present invention also provides methods for the production of a compound of the invention, pharmaceutical compositions comprising a compound of the invention, the use of the compounds in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. (Formula (I))

公开(公告)号：WO2018149925A1

公开(公告)日：2018-08-23

申请号：PCT/EP2018/053803

申请日：2018-02-15

Applicant: GALAPAGOS NV

Inventor： BRYS, Reginald, Christophe, Xavier ,  GALIEN, René, Alexandre ,  DE VOS, Steve, Irma, Joel ,  AMANTINI, David ,  CLÉMENT-LACROIX, Philippe

IPC: A61K31/444 ,  A61K31/541 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00

Abstract: The present invention discloses compositions comprising compounds according to Formula I wherein R 1 , R 2 , and Cy are as defined herein, and a second compound having a JAK inhibiting activity. The present invention relates to composition, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases, allergic diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound of the invention

公开(公告)号：WO2018116185A1

公开(公告)日：2018-06-28

申请号：PCT/IB2017/058179

申请日：2017-12-19

Applicant: ABBVIE S.À.R.L. ,  GALAPAGOS NV

Inventor： CHAN, Vincent S. ,  KYM, Philip R. ,  SHEKHAR, Shashank ,  WANG, Xueqing

IPC: C07D407/12 ,  A61P11/00 ,  A61P11/12 ,  A61K31/352

Abstract: The invention discloses compounds of Formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 , R 16 , A, R 19 , R 20 , and R 21 are as defined herein. The present invention relates to deuterated compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

公开(公告)号：WO2018087202A1

公开(公告)日：2018-05-17

申请号：PCT/EP2017/078701

申请日：2017-11-09

Applicant: GALAPAGOS NV

Inventor： TASSET, Chantal, Thérèse ,  HARRISON, Pille ,  GALIEN, René, Alexandre ,  SUNDY, John, Sargent ,  MCHUTCHISON, John, G. ,  O'RIORDAN, Thomas ,  MOZAFFARIAN, Neelufar ,  PATEL, Uptal, Dinesh ,  WATKINS, Timothy, R. ,  GOSSAGE, David, L.

IPC: A61K31/541 ,  A61K45/06 ,  A61P17/14 ,  A61P17/00 ,  A61P37/00 ,  A61P13/12 ,  A61P9/00 ,  A61P1/16 ,  A61P11/00 ,  A61P25/00

Abstract: The present invention relates to the use of compounds or pharmaceutical compositions comprising the same for use in the prophylaxis and/or treatment of alopecia areata, vitiligo, cutaneous lupus, lupus nephritis, giant cell arteritis, sarcoidosis and/or sarcoidosis-related conditions. In particular the compounds are JAK1 inhibitors.

Abstract translation: 本发明涉及包含其的化合物或药物组合物用于预防和/或治疗斑秃，白癜风，皮肤狼疮，狼疮肾炎，巨细胞动脉炎，结节病和 /或结节病相关病症。 特别是化合物是JAK1抑制剂。

公开(公告)号：WO2018065921A1

公开(公告)日：2018-04-12

申请号：PCT/IB2017/056126

申请日：2017-10-04

Applicant: ABBVIE S.Á.R.L. ,  GALAPAGOS NV

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  DESROY, Nicolas ,  GFESSER, Gregory A. ,  GRESZLER, Stephen N. ,  KOENIG, John R. ,  KYM, Philip R. ,  LIU, Bo ,  SCANIO, Marc J. ,  SEARLE, Xenia ,  WANG, Xueqing ,  YEUNG, Ming C. ,  ZHAO, Gang

IPC: C07D207/16 ,  C07D401/12 ,  A61K31/4025 ,  A61K31/4439 ,  A61P11/00

Abstract: The invention discloses compounds of Formula (I) wherein R 1 , R 2 , R 2A , R 3 , R 3A , R 4 , and R 5 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

Abstract translation: 本发明公开了式（I）的化合物，其中R 1，R 2，R 2，A，R 4，R 5， R 3，R 4，R 5和R 5如本文所定义。 本发明涉及化合物及其在治疗囊性纤维化中的用途，其制备方法，包含其的药物组合物，以及通过施用本发明化合物治疗囊性纤维化的方法。

公开(公告)号：WO2017187321A1

公开(公告)日：2017-11-02

申请号：PCT/IB2017/052349

申请日：2017-04-24

Applicant: ABBVIE S.À.R.L. ,  GALAPAGOS NV

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  CHAN, Vincent ,  GRIEME, Timothy A. ,  KOENIG, John R. ,  KYM, Philip R. ,  LIU, Bo ,  MALAGU, Karine Fabienne ,  PATEL, Sachin V. ,  SCANIO, Marc ,  SEARLE, Xenia B. ,  SHEKHAR, Shashank ,  WANG, Xueqing ,  YEUNG, Ming C.

IPC: C07D311/58 ,  A61K31/352 ,  C07D311/60 ,  C07D407/12 ,  C07D407/14 ,  A61P11/00

Abstract: The present invention provides for compounds of formula (I), wherein R 1 , m, Z, G 1 , R 2 , and R 3 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Abstract translation: 本发明提供了式（I）的化合物，其中R 1，m，Z，G 1，R 2， R 3和R 3具有本说明书中定义的任何值及其药学上可接受的盐，其可用作治疗由CFTR介导和调节的疾病和病症的试剂，包括 囊性纤维化，SJ氏综合征，胰腺功能不全，慢性阻塞性肺病和慢性阻塞性气道疾病。 还提供了由一种或多种式（I）化合物组成的药物组合物。