公开(公告)号：WO2019154795A1

公开(公告)日：2019-08-15

申请号：PCT/EP2019/052751

申请日：2019-02-05

Applicant: VIB VZW ,  UNIVERSITEIT ANTWERPEN ,  UNIVERSITEIT GENT

Inventor： VANDENABEELE, Peter ,  VANDEN BERGHE, Tom ,  AUGUSTYNS, Koen ,  HOFMANS, Sam ,  VAN DER VEKEN, Pieter ,  DEVISSCHER, Lars

IPC: C07C311/38 ,  C07D295/14 ,  C07D295/12 ,  C07D213/38 ,  A61K31/18 ,  A61K31/495 ,  A61K31/5375 ,  A61P9/10 ,  A61P3/10 ,  A61P37/06 ,  A61P25/28 ,  A61P25/16

Abstract: The present invention relates to 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 (Fer-1) analogues as cell death inhibitors by inhibition of ferroptosis and/or oxytosis for the treatment of stroke, myocardial infarction, diabetes, sepsis, the prevention of transplant rejection, neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, dementia with Lewy bodies and Friedreich's ataxia. The present invention further relates to pharmaceutical compositions of these compounds and discloses methods for making the compounds and the corresponding intermediate.

公开(公告)号：WO2016075330A1

公开(公告)日：2016-05-19

申请号：PCT/EP2015/076680

申请日：2015-11-16

Applicant: VIB VZW ,  UNIVERSITEIT GENT ,  UNIVERSITEIT ANTWERPEN

Inventor： VANDENABEELE, Peter ,  VANDEN BERGHE, Tom ,  AUGUSTYNS, Koen ,  JOOSSENS, Jurgen ,  VAN DER VEKEN, Pieter ,  HOFMANS, Sam

IPC: C07D239/26 ,  C07C311/39 ,  C07C311/40 ,  C07D295/26 ,  C07D213/38 ,  A61K31/18 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/535 ,  A61P25/28

CPC classification number: C07C311/39 ,  C07C311/40 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07C2603/74 ,  C07D213/38 ,  C07D239/26 ,  C07D295/26

Abstract: The present invention relates to a novel class of compounds having the structure of formula (I) and pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof. These compounds inhibit or reduce the non-apoptotic cell death forms ferroptosis and/or oxytosis rendering them useful for the treatment of various conditions disclosed herein.

Abstract translation: 本发明涉及具有式（I）结构的新一类化合物和包含式（I）化合物或其药学上可接受的盐的药物组合物。 这些化合物抑制或减少非凋亡细胞死亡形式的铁锈和/或催产，使得它们可用于治疗本文公开的各种病症。

公开(公告)号：WO2017198753A1

公开(公告)日：2017-11-23

申请号：PCT/EP2017/061933

申请日：2017-05-18

Applicant: UNIVERSITEIT ANTWERPEN

Inventor： AUGUSTYNS, Koen ,  JOOSSENS, Jurgen ,  VAN DER VEKEN, Pieter ,  COS, Paul ,  JOOSSEN, Cedric ,  DE WINTER, Benedicte Yvonne ,  CEULEERS, Hannah ,  VAN SPAENDONK, Hanne

IPC: A61K31/688 ,  A61P27/02 ,  A61P29/00 ,  A61P17/00 ,  A61P11/00 ,  A61P1/00

Abstract: The present invention relates to compounds for use in the prevention and/or treatment of PAR-related diseases, such as for example: pain and ocular disorders. More in particular, the present invention provides bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of pancreatitis-related pain, IBS (irritable bowel syndrome), IBD (inflammatory bowel disease), dry eye disease and conjunctivitis sicca. These inhibitors were found to have a different inhibitory profile compared to diphenyl guanidinophenylethylphosphonates leading to a more pronounced effect on these conditions.

Abstract translation: 本发明涉及用于预防和/或治疗PAR相关疾病的化合物，例如疼痛和眼部疾病。 更特别地，本发明提供用于预防和/或治疗胰腺炎相关疼痛，IBS（肠易激综合征），IBD（炎性肠病），干眼病和干燥性结膜炎的双（乙酰​​氨基苯基）胍基苯基乙基膦酸酯。 发现这些抑制剂与二苯基胍基苯基乙基膦酸盐相比具有不同的抑制特性，导致对这些条件更显着的影响。

公开(公告)号：WO2013068551A1

公开(公告)日：2013-05-16

申请号：PCT/EP2012/072308

申请日：2012-11-09

Applicant: UNIVERSITEIT ANTWERPEN ,  HEERES, JAN ,  SHAKTURANA CV

Inventor： HEERES, JAN ,  AUGUSTYNS, Koen ,  VAN DER VEKEN, Pieter ,  JOOSSENS, Jurgen ,  MUTHUSAMY, Venkatraj ,  MAES, Louis

IPC: C07D251/52 ,  C07D251/70 ,  A61K31/53 ,  A61P31/00 ,  A61P31/12 ,  A61P31/18 ,  A61P33/00 ,  A61P33/02 ,  A61P33/06

CPC classification number: C07D403/12 ,  C07D251/52 ,  C07D251/70

Abstract: The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases such as African trypanosomiasis, Chagas disease, Leishmaniasis, Malaria and HIV. The invention further relates to the prevention and/or treatment of these diseases.

Abstract translation: 本发明涉及包含通过有机接头共价连接的两个二取代三嗪环的新化合物（I），从而产生二聚体。 这些化合物显示针对感染性疾病如非洲锥虫病，恰加斯病，利什曼病，疟疾和艾滋病毒的致病感染因子的活性。 本发明还涉及这些疾病的预防和/或治疗。

公开(公告)号：WO2018096088A1

公开(公告)日：2018-05-31

申请号：PCT/EP2017/080319

申请日：2017-11-24

Applicant: UNIVERSITEIT ANTWERPEN ,  UNIVERSITAIR ZIEKENHUIS ANTWERPEN

Inventor： AUGUSTYNS, Koen ,  CLEENEWERCK, Matthias ,  DE MEYER, Guido R.Y. ,  JOOSSENS, Jurgen ,  KURDI, Ammar ,  VAN DER VEKEN, Pieter ,  VANGESTEL, Christel ,  STROOBANTS, Sigrid ,  MARTINET, Wim

IPC: C07C69/757 ,  C07C62/38 ,  C07C235/82 ,  A61K31/167 ,  A61K31/215 ,  A61P35/00

Abstract: The present invention relates to compounds having a benzotropolone core, and compositions containing said compounds acting as ATG4B inhibitors, thereby inhibiting autophagy. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.

公开(公告)号：WO2015144933A1

公开(公告)日：2015-10-01

申请号：PCT/EP2015/056908

申请日：2015-03-30

Applicant: UNIVERSITEIT ANTWERPEN

Inventor： JOOSSENS, Jurgen ,  AUGUSTYNS, Koen ,  LAMBEIR, Anne-Marie ,  VAN DER VEKEN, Pieter ,  VAN SOOM, Jeroen ,  MAGDOLEN, Viktor

IPC: C07F9/6539 ,  C07F9/6561

CPC classification number: C07F9/6561 ,  A61K49/0052 ,  C07F9/4087 ,  C07F9/588 ,  C07F9/650964 ,  C07F9/650988 ,  C07F9/65182 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655345 ,  C07F9/65583 ,  C07F9/65586 ,  C12Q1/37 ,  G01N2333/96433

Abstract: The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.

Abstract translation: 本发明涉及具有获得对KLK4的有效抑制活性所必需的共同化学结构和/或可用于检测KLK4肽及其活性的新型化合物和探针。 它还涉及这些化合物和方法在体外和体内通过利用所述探针或抑制剂来抑制和/或检测KLK4活性的用途。 本发明的化合物与至少在苯基胍（代替例如苄基胍）和/或尾部基团中存在杂原子的现有技术化合物不同，它们的组合存在意外地导致有效和选择性的KLK4抑制活性 。

公开(公告)号：WO2013139727A1

公开(公告)日：2013-09-26

申请号：PCT/EP2013/055525

申请日：2013-03-18

Applicant: UNIVERSITEIT ANTWERPEN ,  HEERES, Jan ,  SHAKTURANA CV

Inventor： HEERES, Jan ,  VAN DER VEKEN, Pieter ,  JOOSSENS, Jurgen ,  MUTHUSAMY, Venkatraj ,  AUGUSTYNS, Koen ,  ARIËN, Kevin Karel Florentina ,  VANHAM, Guido Louis Emile

IPC: C07D251/70 ,  A61K31/53 ,  A61P31/18

CPC classification number: C07D251/70 ,  A61K31/18 ,  A61K31/53 ,  C07D251/52

Abstract: The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.

Abstract translation: 本发明涉及HIV-1感染领域，特别是提供含有三嗪环和合适间隔物的新化合物。 根据本发明的化合物非常适合于预防和/或治疗HIV-1感染，特别是显示针对HIV-1抗NNRTI抗性病毒的改善的活性。

公开(公告)号：WO2013107820A1

公开(公告)日：2013-07-25

申请号：PCT/EP2013/050845

申请日：2013-01-17

Applicant: UNIVERSITEIT ANTWERPEN ,  FOX CHASE CANCER CENTER

Inventor： JANSEN, Koen ,  DE MEESTER, Ingrid ,  HEIRBAUT, Leen ,  CHENG, Jonathan D ,  JOOSSENS, Jurgen ,  AUGUSTYNS, Koen ,  VAN DER VEKEN, Pieter

IPC: C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  A61K31/401 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.

Abstract translation: 本发明涉及对FAP（成纤维细胞活化蛋白）具有高选择性和特异性的新型抑制剂。 所述抑制剂可用作人和/或兽医药物，特别是用于治疗和/或预防FAP相关疾病，例如但不限于增殖性疾病。

公开(公告)号：WO2012152807A1

公开(公告)日：2012-11-15

申请号：PCT/EP2012/058490

申请日：2012-05-09

Applicant: UNIVERSITEIT ANTWERPEN ,  AUGUSTYNS, Koen ,  VAN DER VEKEN, Pieter ,  MESSAGIE, Jonas ,  JOOSSENS, Jurgen ,  LAMBEIR, Anne-Marie

Inventor： AUGUSTYNS, Koen ,  VAN DER VEKEN, Pieter ,  MESSAGIE, Jonas ,  JOOSSENS, Jurgen ,  LAMBEIR, Anne-Marie

IPC: A61K49/00 ,  C07F9/40

CPC classification number: A61K49/0052 ,  A61K49/0021 ,  A61K49/0032 ,  A61K49/0041 ,  C07F5/04 ,  C07F9/40 ,  C07F9/4006 ,  C07F9/65187 ,  C07F9/65522 ,  C07F9/65583 ,  C07F9/65586 ,  C07F9/6561

Abstract: The present invention relates to selective trypsine-like serine protease activity-based probes, in particular urokinase plasminogen activator-activity based probes, the use thereof and methods for detecting selective urokinase activity by making use of said probes.

Abstract translation: 本发明涉及基于选择性胰蛋白酶样丝氨酸蛋白酶活性的探针，特别是基于尿激酶纤溶酶原激活物活性的探针，其用途和通过利用所述探针检测选择性尿激酶活性的方法。

公开(公告)号：WO2007045496A1

公开(公告)日：2007-04-26

申请号：PCT/EP2006/010147

申请日：2006-10-20

Applicant: UNIVERSITEIT ANTWERPEN ,  AUGUSTYNS, Koen ,  JOOSSENS, Jurgen ,  VAN DER VEKEN, Pieter ,  LAMBEIR, Anne-Marie Virginie Renée ,  SCHARPÉ, Simon ,  HAEMERS, Achiel

Inventor： AUGUSTYNS, Koen ,  JOOSSENS, Jurgen ,  VAN DER VEKEN, Pieter ,  LAMBEIR, Anne-Marie Virginie Renée ,  SCHARPÉ, Simon ,  HAEMERS, Achiel

IPC: C07F9/40

CPC classification number: C07F9/4006 ,  C07F9/4084

Abstract: The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to the use of said uPA inhibitor compounds as a medicament and the use of said uPA inhibitor compounds for the preparation of a medicament for the treatment of conditions chosen from the group comprising cancer, tumour growth, tumour invasion, tumour metastasis, diabetic retinopathy, hemorrhagic atherosclerosis and inflammatory conditions, such as rheumatoid arthritis and psoriasis.

Abstract translation: 本发明涉及对尿激酶纤溶酶原激活物（uPA）具有抑制活性的新化合物; 制备所述uPA抑制剂化合物的方法; 涉及包含所述uPA抑制剂化合物的药物组合物; 涉及使用所述uPA抑制剂化合物作为药物，以及所述uPA抑制剂化合物用于制备用于治疗选自以下的病症的药物的用途：选自癌症，肿瘤生长，肿瘤侵袭，肿瘤转移，糖尿病性视网膜病变，出血性 动脉粥样硬化和炎性病症，如类风湿性关节炎和牛皮癣。