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公开(公告)号：WO2022043486A1
公开(公告)日：2022-03-03
申请号：PCT/EP2021/073722
申请日：2021-08-27
发明人： GRALL-ULSEMER, Sandra , GUBA, Wolfgang , LERNER, Christian , LI, Mingming , LIU, Yongqiang , RUDOLPH, Markus , SCHMITT, Sébastien , URNER, Lorenz , WANG, Yongguang , WANG, Min , WANG, Jianhua , YANG, Song , ZHOU, Chengang , MATTEI, Patrizio
IPC分类号： A61P31/04 , C07D401/14 , C07D403/14 , A61K31/4439 , A61K31/496 , A61K31/501 , A61K31/505
摘要： The invention provides novel imidazole pyrazole derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein A and R1-R7 are as described herein: Formula (I) Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
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公开(公告)号：WO2021259815A1
公开(公告)日：2021-12-30
申请号：PCT/EP2021/066725
申请日：2021-06-21
发明人： BELL, Andrew Simon , BESNARD, Jérémy , BRADLEY, Anthony Richard , GREEN, Luke , HAAP, Wolfgang , KOCER, Buelent , KUGLSTATTER, Andreas , LUCAS, Xavier , MATTEI, Patrizio , MAZUNIN, Dmitry , RATNI, Hasane , RIEMER, Claus , VAN HOORN, Willem Paul
IPC分类号： C07D239/95 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/04 , C07D471/04 , C07D473/04 , A61P35/00 , A61K31/00
摘要： The present invention provides compounds of formula I or II: wherein X1, X3, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula I, pharmaceutical compositions comprising them and their use as medicaments.
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公开(公告)号：WO2018167001A1
公开(公告)日：2018-09-20
申请号：PCT/EP2018/056140
申请日：2018-03-13
发明人： MATTEI, Patrizio , HERT, Jérôme , HUNZIKER, Daniel , RUDOLPH, Markus , SCHMITZ, Petra , DI GIORGIO, Patrick , GOMME, Justin
IPC分类号： C07D401/14 , C07D405/14 , A61K31/397 , A61K31/4025 , A61K31/496 , C07D401/10 , C07D401/12 , C07D403/10 , C07D409/14 , C07D417/14 , A61P27/02
摘要： The invention provides novel compounds having the general formula (I) wherein R 1 is selected from substituted phenyl, pyridinyl or thiophenyl, R 2 is selected from optionally substituted aminosulphonylphenyl, aminosulphonylpyridinyl, aminosulphonylthiophenyl or aminosulphonylthiazolyl, X is nitrogen or carbon, Y is a linking group, Z is a direct bond or a linking group, m = 0-5, n = 0-5 with the proviso that m+n is 2-5, compositions including the compounds and the use of the compounds in the treatment or prophylaxis of ocular conditions.
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公开(公告)号：WO2017050791A1
公开(公告)日：2017-03-30
申请号：PCT/EP2016/072347
申请日：2016-09-21
发明人： DI GIORGIO, Patrick , HERT, Jérôme , HUNZIKER, Daniel , MATTEI, Patrizio , RUDOLPH, Markus , SCHMITZ, Petra , ULLMER, Christoph
IPC分类号： C07D471/04 , C07D487/04 , A61K31/407 , A61K31/437 , A61K31/5517 , A61P29/00 , A61P1/00 , A61P25/00 , A61P37/00
CPC分类号： C07D487/04 , A61K31/407 , A61K31/437 , A61K31/5517 , C07D471/04
摘要： The invention provides novel compounds having the general formula (I) wherein R 1 , R 2 ,Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R 1，R 2，Y，W，m，n，p和q如本文所定义，包括该化合物的组合物和使用该化合物的方法。
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5.发明申请BICYCLIC COMPOUNDS AS AUTOTAXIN (ATX) AND LYSOPHOSPHATIDIC ACID (LPA) PRODUCTION INHIBITORS 审中-公开双酚化合物（ATX）和赖氨酸（LPA）生产抑制剂
公开(公告)号：WO2015144605A1
公开(公告)日：2015-10-01
申请号：PCT/EP2015/056032
申请日：2015-03-23
发明人： DI GIORGIO, Patrick , HERT, Jérôme , HUNZIKER, Daniel , KUEHNE, Holger , MATTEI, Patrizio , RUDOLPH, Markus
IPC分类号： C07D487/04 , A61K31/407 , A61K31/55 , A61P3/00 , A61P1/16
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention provides novel compounds having the general formula (I) wherein R 1 , R 2 , A, W, m, n, p and q are as described herein, compositions including the compounds. The compounds of formula (I) are useful as autotaxin (ATX) inhibitors which are inhibitors of lysophosphatidic acid (LPA) production and thus modulators of LPA levels and associated signaling; in particular they are useful for the treatment or prophylaxis of renal conditions, liver conditions, inflammatory conditions, conditions of the nervous system, conditions of the respiratory system, vascular and cardiovascular conditions, fibrotic diseases, cancer, ocular conditions, metabolic conditions, cholestatic and other forms of chronic pruritus and acute and chronic organ transplant rejection.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R1，R2，A，W，m，n，p和q如本文所述，包括该化合物的组合物。 式（I）化合物可用作自分泌素（ATX）抑制剂，其是溶血磷脂酸（LPA）产生的抑制剂，因此可用作LPA水平和相关信号传导的调节剂; 特别是它们可用于治疗或预防肾脏病症，肝脏病症，炎性病症，神经系统状况，呼吸系统状况，血管和心血管疾病，纤维化疾病，癌症，眼部病症，代谢病症，胆汁淤积和 其他形式的慢性瘙痒和急慢性器官移植排斥反应。
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公开(公告)号：WO2019206853A1
公开(公告)日：2019-10-31
申请号：PCT/EP2019/060272
申请日：2019-04-23
发明人： BLEICHER, Konrad , CHEANG, Daniella , DI GIORGIO, Patrick , HU, Taishan , JENNY, Christian , MATTEI, Patrizio , SCHMITZ, Petra , STOLL, Theodor
摘要： The present invention provides compounds of formula (I) wherein X 1 , X 2 , R 1 to R 6 and A are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by bacteria.
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公开(公告)号：WO2017050747A1
公开(公告)日：2017-03-30
申请号：PCT/EP2016/072277
申请日：2016-09-20
发明人： HERT, Jérôme , HUNZIKER, Daniel , MATTEI, Patrizio , RUDOLPH, Markus , SCHMITZ, Petra , ULLMER, Christoph
IPC分类号： C07D487/04 , A61K31/407 , A61P27/02
CPC分类号： C07D487/04
摘要： The invention provides novel compounds having the general formula (I) wherein R 1 , R 2 , R 9 , Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 9，Y，W，m，n，p和q如本文所定义，包括该化合物的组合物和使用该化合物的方法。
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公开(公告)号：WO2016162390A1
公开(公告)日：2016-10-13
申请号：PCT/EP2016/057549
申请日：2016-04-07
发明人： HERT, Jérôme , HUNZIKER, Daniel , KURATLI, Christoph , MARTIN, Rainer E. , MATTEI, Patrizio , SATZ, Alexander Lee
IPC分类号： C07D403/02 , A61K31/517
CPC分类号： C07D239/90 , A61K31/517 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The invention provides novel compounds having the general formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 12 , R 13 , R 14 , A 1 , A 2 , A 3 , n and m are as described herein.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R12，R13，R14，A1，A2，A3，n和m分别为 在此描述。
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公开(公告)号：WO2017050732A1
公开(公告)日：2017-03-30
申请号：PCT/EP2016/072243
申请日：2016-09-20
发明人： DI GIORGIO, Patrick , HERT, Jérôme , HUNZIKER, Daniel , MATTEI, Patrizio , RUDOLPH, Markus , SCHMITZ, Petra
IPC分类号： C07D487/04 , C07D519/00 , A61K31/407 , A61P27/02
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention provides novel compounds having the general formula (I), (I) wherein R 1 , R 2 , R 9 , Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
摘要翻译： 本发明提供具有通式（I），（I）的新化合物，其中R1，R2，R9，Y，W，m，n，p和q如本文所定义，包括该化合物的组合物和使用该化合物的方法。
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10.发明申请
公开(公告)号：WO2023280733A1
公开(公告)日：2023-01-12
申请号：PCT/EP2022/068362
申请日：2022-07-04
发明人： GRALL-ULSEMER, Sandra Marie Joseph , HAN, Xingchun , KNECHT, Joel Lukas , LERNER, Christian , LI, Mingming , LIU, Yongqiang , MATTEI, Patrizio , NETTEKOVEN, Matthias , PFLIEGER, Philippe , STOLL, Theodor , WANG, Jianhua , WANG, Min , WANG, Yongguang , YANG, Song , ZHOU, Chengang
IPC分类号： C07D233/70 , C07D403/12 , C07D403/14 , C07D417/14 , C07D487/04 , A61K31/496 , A61K31/4178 , A61P31/04
摘要： The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
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