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1. 发明申请

WO2007045496A1 NOVEL UROKINASE INHIBITORS 审中-公开
标题翻译：新型尿素酶抑制剂
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
申请人： UNIVERSITEIT ANTWERPEN , AUGUSTYNS, Koen , JOOSSENS, Jurgen , VAN DER VEKEN, Pieter , LAMBEIR, Anne-Marie Virginie Renée , SCHARPÉ, Simon , HAEMERS, Achiel
发明人： AUGUSTYNS, Koen , JOOSSENS, Jurgen , VAN DER VEKEN, Pieter , LAMBEIR, Anne-Marie Virginie Renée , SCHARPÉ, Simon , HAEMERS, Achiel
IPC分类号： C07F9/40
CPC分类号： C07F9/4006 , C07F9/4084
摘要： 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.
摘要翻译：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。

2. 发明申请

WO2012152807A1 ACTIVITY-BASED PROBES FOR THE UROKINASE PLASMINOGEN ACTIVATOR 审中-公开
标题翻译：基于活性的尿激酶激酶活化剂探针
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
申请人： UNIVERSITEIT ANTWERPEN , AUGUSTYNS, Koen , VAN DER VEKEN, Pieter , MESSAGIE, Jonas , JOOSSENS, Jurgen , LAMBEIR, Anne-Marie
发明人： AUGUSTYNS, Koen , VAN DER VEKEN, Pieter , MESSAGIE, Jonas , JOOSSENS, Jurgen , LAMBEIR, Anne-Marie
IPC分类号： A61K49/00 , C07F9/40
CPC分类号： A61K49/0052 , A61K49/0021 , A61K49/0032 , A61K49/0041 , C07F5/04 , C07F9/40 , C07F9/4006 , C07F9/65187 , C07F9/65522 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要： 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.
摘要翻译：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。

3. 发明申请

WO2004076434A1 DIPEPTIDYL PEPTIDASE INHIBITORS 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE抑制剂
公开(公告)号：WO2004076434A1
公开(公告)日：2004-09-10
申请号：PCT/IB2004/000525
申请日：2004-03-01
申请人： AIC , SCHARPE, Simon , AUGUSTYNS, Koen , HAEMERS, Achiel , LAMBEIR, Anne-Marie , DE MEESTER, Ingrid , SENTEN, Kristel , VAN DER VEKEN, Pieter
发明人： SCHARPE, Simon , AUGUSTYNS, Koen , HAEMERS, Achiel , LAMBEIR, Anne-Marie , DE MEESTER, Ingrid , SENTEN, Kristel , VAN DER VEKEN, Pieter
IPC分类号： C07D295/18
CPC分类号： C07D295/194 , C07D211/38 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/70 , C07D213/38 , C07D213/61 , C07D213/74 , C07D213/85 , C07D233/64 , C07D295/185 , C07D317/58 , C07D333/20 , C07D401/06
摘要： The present invention relates to novel inhibitors of serine type peptidases in general and of serine type dipeptidyl peptidases in particular. The present invention further relates to the use of the dipeptidyl peptidase inhibitors for selective inhibition of dipeptidyl peptidases. The present invention also relates to pharmaceutical compositions comprising these novel dipeptidyl peptidase inhibitors. The present invention further relates to the use of the novel inhibitors in therapy, diagnosis and research.
摘要翻译：本发明涉及丝氨酸型肽酶的新型抑制剂，特别涉及丝氨酸型二肽基肽酶。本发明还涉及二肽基肽酶抑制剂用于选择性抑制二肽基肽酶的用途。本发明还涉及包含这些新型二肽基肽酶抑制剂的药物组合物。本发明还涉及新型抑制剂在治疗，诊断和研究中的用途。

4. 发明申请

WO2004076433A1 DIPEPTIDYL PEPTIDASE INHIBITORS 审中-公开
标题翻译：二磷酸二肽酶抑制剂
公开(公告)号：WO2004076433A1
公开(公告)日：2004-09-10
申请号：PCT/IB2003/000792
申请日：2003-02-28
申请人： AIC , SCHARPE, Simon , AUGUSTYNS, Koen , HAEMERS, Achiel , LAMBEIR, Anne-Marie , DE MEESTER, Ingrid , SENTEN, Kristel , VAN DER VEKEN, Pieter
发明人： SCHARPE, Simon , AUGUSTYNS, Koen , HAEMERS, Achiel , LAMBEIR, Anne-Marie , DE MEESTER, Ingrid , SENTEN, Kristel , VAN DER VEKEN, Pieter
IPC分类号： C07D295/18
CPC分类号： C07D333/20 , C07D211/38 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/70 , C07D213/38 , C07D213/61 , C07D213/74 , C07D213/85 , C07D233/64 , C07D295/185 , C07D295/194 , C07D307/52 , C07D317/58 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/14
摘要： The present invention relates to novel inhibitors of serine type peptidases in general and of serine type dipeptidyl peptidases in particular. The present invention further relates to the use of the dipeptidyl peptidase inhibitors for selective inhibition of dipeptidyl peptidases. The present invention also relates to pharmaceutical compositions comprising these novel dipeptidyl peptidase inhibitors. The present invention further relates to the use of the novel inhibitors in therapy, diagnosis and research.
摘要翻译：本发明一般涉及新的丝氨酸型肽酶抑制剂，特别涉及丝氨酸型二肽基肽酶的新型抑制剂。本发明进一步涉及二肽基肽酶抑制剂用于选择性抑制二肽基肽酶的用途。本发明还涉及包含这些新型二肽基肽酶抑制剂的药物组合物。本发明进一步涉及新型抑制剂在治疗，诊断和研究中的用途。

5. 发明申请

WO2007016753A1 IMPROVED DENTAL PROSTHESIS STABILIZER 审中-公开
标题翻译：改进牙齿保护稳定器
公开(公告)号：WO2007016753A1
公开(公告)日：2007-02-15
申请号：PCT/BE2006/000075
申请日：2006-06-30
申请人： VAN DER KERKEN, André Jozef Ernest , VAN DER VEKEN, Pieter
发明人： VAN DER KERKEN, André Jozef Ernest , VAN DER VEKEN, Pieter
IPC分类号： A61C13/28
CPC分类号： A61C13/28
摘要： Improved dental prosthesis stabilizer ( 1 ) which is provided with two arms (2, 3) which are connected to each other by means of a hinge joint ( 4 ) and with which an upper dental prosthesis ( 3 7 ) and a lower dental prosthesis (38) are coupled to one another , whereby a spring ( 5 ) is provided at the hinge joint ( 4 ) with which the upper prosthesis ( 37 ) and the lower prosthes is ( 38 ) are pushed away from each other , characterised in that at least one of the arms (2, 3 ) is made telescopic and is formed of a bent far end ( 6 , 7 ) of the above-mentionned spring ( 5 ) , which can be axially moved in a bent guide (8, 9), which guide ( 8 , 9 ) is designed to be fixed on an upper dental prosthesis ( 37 ) or a lower dental prosthesis ( 38 ) or to be embedded therein .
摘要翻译：改进的牙科假体稳定器（1），其设置有通过铰链接头（4）彼此连接并且具有上部假牙（3 7）和下部牙科假体（2）的两个臂（2,3） 38）彼此联接，由此在所述铰链接头（4）处设置有弹簧（5），所述上假体（37）和所述下部假体（38）被彼此推开，其特征在于，在臂（2,3）中的至少一个被制造成可伸缩的并且由上述提到的弹簧（5）的弯曲的远端（6,7）形成，其可以在弯曲的引导件（8,9）中轴向移动，，该引导件（8,9）设计成固定在上部假牙（37）或下部牙科假体（38）上或嵌入其中。

6. 发明申请

WO2017198753A1 BIS(ACETAMIDOPHENYL) GUANIDINOPHENYLETHYLPHOSPHONATES FOR USE IN THE PREVENTION AND/OR TREATMENT OF PAR-RELATED DISEASES 审中-公开
标题翻译：用于预防和/或治疗疱疹相关疾病的BIS（乙酰氨基苯基）胍基苯基乙基膦酸酯
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
申请人： UNIVERSITEIT ANTWERPEN
发明人： AUGUSTYNS, Koen , JOOSSENS, Jurgen , VAN DER VEKEN, Pieter , COS, Paul , JOOSSEN, Cedric , DE WINTER, Benedicte Yvonne , CEULEERS, Hannah , VAN SPAENDONK, Hanne
IPC分类号： A61K31/688 , A61P27/02 , A61P29/00 , A61P17/00 , A61P11/00 , A61P1/00
摘要： 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.
摘要翻译：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。

7. 发明申请

WO2019154795A1 3-(BENZYLAMINO)-4-(CYCLOHEXYLAMINO)-N-(2-(PIPERAZIN-1-YL)ETHYL)BENZENESULFONAMIDE DERIVATIVES AND RELATED FERROSTATIN-1 ANALOGUES AS CELL DEATH INHIBITORS FOR TREATING E.G. STROKE 审中-公开
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
申请人： VIB VZW , UNIVERSITEIT ANTWERPEN , UNIVERSITEIT GENT
发明人： VANDENABEELE, Peter , VANDEN BERGHE, Tom , AUGUSTYNS, Koen , HOFMANS, Sam , VAN DER VEKEN, Pieter , DEVISSCHER, Lars
IPC分类号： C07C311/38 , C07D295/14 , C07D295/12 , C07D213/38 , A61K31/18 , A61K31/495 , A61K31/5375 , A61P9/10 , A61P3/10 , A61P37/06 , A61P25/28 , A61P25/16
摘要： 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.

8. 发明申请

WO2016075330A1 3,4-DIAMINOBENZENESULFONAMIDE DERIVATIVES FOR INHIBITING CELL DEATH 审中-公开
标题翻译：用于抑制细胞死亡的3,4-二氨基苯甲酰胺衍生物
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
申请人： VIB VZW , UNIVERSITEIT GENT , UNIVERSITEIT ANTWERPEN
发明人： VANDENABEELE, Peter , VANDEN BERGHE, Tom , AUGUSTYNS, Koen , JOOSSENS, Jurgen , VAN DER VEKEN, Pieter , HOFMANS, Sam
IPC分类号： C07D239/26 , C07C311/39 , C07C311/40 , C07D295/26 , C07D213/38 , A61K31/18 , A61K31/4409 , A61K31/495 , A61K31/535 , A61P25/28
CPC分类号： C07C311/39 , C07C311/40 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D213/38 , C07D239/26 , C07D295/26
摘要： 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.
摘要翻译：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。

9. 发明申请

WO2013068551A1 DISUBSTITUTED TRIAZINE DIMERS FOR TREATMENT AND/OR PREVENTION OF INFECTIOUS DISEASES 审中-公开
标题翻译：用于治疗和/或预防感染性疾病的分离的TRIAZINE二聚体
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
申请人： UNIVERSITEIT ANTWERPEN , HEERES, JAN , SHAKTURANA CV
发明人： HEERES, JAN , AUGUSTYNS, Koen , VAN DER VEKEN, Pieter , JOOSSENS, Jurgen , MUTHUSAMY, Venkatraj , MAES, Louis
IPC分类号： C07D251/52 , C07D251/70 , A61K31/53 , A61P31/00 , A61P31/12 , A61P31/18 , A61P33/00 , A61P33/02 , A61P33/06
CPC分类号： C07D403/12 , C07D251/52 , C07D251/70
摘要： 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.
摘要翻译：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。

10. 发明申请

WO2018096088A1 HALOGENATED BENZOTROPOLONES AS ATG4B INHIBITORS 审中-公开
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
申请人： UNIVERSITEIT ANTWERPEN , UNIVERSITAIR ZIEKENHUIS ANTWERPEN
发明人： AUGUSTYNS, Koen , CLEENEWERCK, Matthias , DE MEYER, Guido R.Y. , JOOSSENS, Jurgen , KURDI, Ammar , VAN DER VEKEN, Pieter , VANGESTEL, Christel , STROOBANTS, Sigrid , MARTINET, Wim
IPC分类号： C07C69/757 , C07C62/38 , C07C235/82 , A61K31/167 , A61K31/215 , A61P35/00
摘要： 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.

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