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1. 发明公开

EP4015505A1 IMPROVED PROCESS FOR PRODUCING NITROXOLINE 审中-公开
公开(公告)号：EP4015505A1
公开(公告)日：2022-06-22
申请号：EP21180903.3
申请日：2021-06-22
申请人： Kopran Research Laboratories Limited
发明人： PANDEY, Anand Kumar , DONGARGE, Mahesh Yogiraj , CHAUGULE, Suryabhan Baban
IPC分类号： C07D215/28
摘要： Disclosed herein is an improved and cost effective process for preparation of Nitroxoline (5-nitro-8-oxyquinoline) free from process related genotoxic impurities. The process of the present invention significantly controls the formation of the undesired side-product i.e. 7-Nitro nitroxoline during oxidation of 5-nitroso-8-oxyquinoline and results in improved yield and purity of the product.

2. 发明公开

EP2852439A1 INHIBITORS OF THE ACTIVITY OF COMPLEX (III) OF THE MITOCHONDRIAL ELECTRON TRANSPORT CHAIN AND USE THEREOF 审中-公开
标题翻译： HEMMER DERAKTIVITÄTDES KOMPLEXES（III）DER MITOCHONDRIALEN ELEKTRONENTRANSPORTKETTE UND VERWENDUNG DAVON
公开(公告)号：EP2852439A1
公开(公告)日：2015-04-01
申请号：EP13727824.8
申请日：2013-05-23
申请人： Stemergie Biotechnology SA
发明人： CLEMENT-SCHATLO, Virginie , FESSARD, Thomas , BARBARAS, Damien , MATOS, Joana , CARREIRA, Erick
IPC分类号： A61P35/00 , A61P31/00 , A61K31/166 , A61K31/167 , A61K31/337 , A61K31/4164 , A61K31/4192 , A61K31/421 , A61K31/426 , C07C275/42 , C07D213/81 , C07D215/28 , C07C39/30 , C07C305/08 , C07D231/56
CPC分类号： C07D495/10 , A01N31/08 , A01N33/10 , A01N35/04 , A01N37/24 , A01N37/40 , A01N37/44 , A01N37/46 , A01N37/50 , A01N43/20 , A01N43/38 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/52 , A01N43/56 , A01N43/60 , A01N43/647 , A01N43/76 , A01N43/78 , A01N43/80 , A01N43/90 , A01N47/30 , A61K31/137 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/397 , A61K31/421 , A61K31/44 , A61K31/47 , A61K31/55 , A61K45/06 , C07C39/245 , C07C39/30 , C07C43/1787 , C07C49/245 , C07C49/825 , C07C215/50 , C07C233/25 , C07C233/33 , C07C235/60 , C07C235/62 , C07C237/38 , C07C237/40 , C07C237/42 , C07C237/44 , C07C251/48 , C07C275/42 , C07C311/08 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/42 , C07C2603/74 , C07D209/42 , C07D213/81 , C07D215/28 , C07D223/24 , C07D223/28 , C07D231/56 , C07D235/18 , C07D235/26 , C07D249/06 , C07D261/08 , C07D263/32 , C07D263/34 , C07D263/57 , C07D277/56 , C07D305/06 , C07D305/08 , C07D403/12 , C07D405/12 , C07D487/10 , C07D491/107 , C07D513/10
摘要： The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
摘要翻译：本发明涉及线粒体电子传递链复合体（III）的活性抑制剂及其在治疗和/或预防呈递肿瘤起始细胞的癌症中的用途。本发明还涉及单独或与其它药物活性剂组合含有所述抑制剂的药物组合物，以及它们作为药物或作为其作为线粒体呼吸抑制剂的性质有益的农药的用途。

3. 发明公开

EP2350012A4 QUINOLINE COMPOUNDS AS INHIBITORS OF ANGIOGENESIS, HUMAN METHIONINE AMINOPEPTIDASE, AND SIRT1, AND METHODS OF TREATING DISORDERS 有权
标题翻译：喹啉ALS血管生成，人道和METHIONINAMINOPEPTIDASE- SIRT1抑制剂AND METHOD FOR疾病治疗
公开(公告)号：EP2350012A4
公开(公告)日：2012-10-24
申请号：EP09819542
申请日：2009-10-06
申请人： UNIV JOHNS HOPKINS
发明人： LIU JUN O , SHIM JOONG SUP , CHONG CURTIS R , BHAT SHRIDHAR
IPC分类号： C07D215/28 , A61K31/47 , A61P35/00 , C07D215/04 , C07D417/14
CPC分类号： C07D215/04 , A61K31/47 , C07D417/14
摘要： Described herein are methods of inhibiting methionine aminopeptidase or SirT1, inhibiting angiogenesis, and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, SirT1 and/or angiogenesis, wherein a compound of the invention is administered to a subject.
摘要翻译：描述的是抑制甲硫氨酸氨肽酶或SIRT1，血管生成抑制，和治疗与甲硫氨酸氨基肽酶，SIRT1和/或血管生成，worin发明的化合物施用于受试者相关的疾病（或其症状）的方法。

4. 发明授权

EP1539700B1 8-HYDROXY QUINOLINE DERIVATIVES 有权转让
标题翻译： 8-羟基喹啉
公开(公告)号：EP1539700B1
公开(公告)日：2009-08-26
申请号：EP03763516.6
申请日：2003-07-16
申请人： Prana Biotechnology Limited
发明人： BARNHAM, Kevin, Jeffrey , GAUTIER, Elisabeth, Colette Louise , KOK, Gaik, Beng , KRIPPNER, Guy
IPC分类号： A61K31/47 , A61K31/4709 , A61P25/28 , C07D215/24 , C07D215/26 , C07D215/28 , C07D215/48
CPC分类号： C07D215/48 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/00 , C07D215/24 , C07D215/26 , C07D215/28 , C07D215/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14 , Y02A50/411 , A61K2300/00
摘要： The present invention relates to a method for the treatment, amelioration and/or prophylaxis of a neurological condition, in particular neurodegenerative disorders which comprises the administration of an effective amount of a compound of formula (I): to a subject in need thereof. The present invention also relates to a compound of formula (II) and processes for its preparation.

5. 发明公开

EP1998761A1 N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS 审中-公开
标题翻译： N-羟基磺酰胺衍生物与生理学NÜTZLICHENITROXYL-SPENDER
公开(公告)号：EP1998761A1
公开(公告)日：2008-12-10
申请号：EP07753345.3
申请日：2007-03-16
申请人： Johns Hopkins University School of Medicine , Cardioxyl Pharmaceuticals, Inc.
发明人： TOSCANO, John, P. , BROOKFIELD, Frederick, Arthur , COHEN, Andrew, D. , COURTNEY, Stephen, Martin , FROST, Lisa, Marie , KALISH, Vincent, Jacob
IPC分类号： A61K31/18 , A61P9/04 , C07C311/48 , C07C317/14 , C07C323/67 , C07D207/36 , C07D213/71 , C07D213/74 , C07D215/28 , C07D215/36 , C07D231/18 , C07D233/84 , C07D239/38 , C07D241/18 , C07D249/12
CPC分类号： C07C311/48 , C07C317/14 , C07C323/67 , C07D213/74 , C07D231/18 , C07D261/10 , C07D263/58 , C07D285/125 , C07D295/096 , C07D307/82 , C07D309/12 , C07D317/14 , C07D333/34 , C07D333/62
摘要： The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
摘要翻译：本发明涉及在生理条件下给予硝酰基（HNO）的N-羟基磺酰胺衍生物，并且可用于治疗和/或预防对硝酰病治疗有反应的疾病或病症的发作和/或发展，包括心力衰竭和缺血/再灌注伤害。新型N-羟基磺酰胺衍生物在生理条件下以控制速率释放NHO，并且通过改变N-羟基磺酰胺衍生物上官能团的性质和位置来调节HNO释放速率。

6. 发明公开

EP0317188A3 Heteroaromatic enamide derivatives and their use as pesticides 失效
标题翻译：异烟肼衍生物及其作为杀虫剂的用途
公开(公告)号：EP0317188A3
公开(公告)日：1990-11-22
申请号：EP88310633.8
申请日：1988-11-11
申请人： ROUSSEL UCLAF
发明人： Blade, Robert John , Peek, Robert John , Cockerill, George
IPC分类号： C07D215/22 , C07D405/12 , C07D215/54 , C07D215/14 , C07D215/36 , C07D215/26 , C07D215/28 , C07D215/20 , A01N43/42 , C07D217/24 , C07D237/30
CPC分类号： C07D215/227 , A01N43/42 , A01N49/00 , C07D215/14 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/28 , C07D215/36 , C07D215/54 , C07D217/24 , C07D237/28 , C07D237/30 , C07D239/95 , C07D241/44 , C07D277/68
摘要： Compound Of the formula (I) are disclosed
or a salt thereof, wherein Ar is an optionally substituted polycyclic ring system containing n rings, where n is the integer 2 or 3, at least n-1 rings being aromatic and containing one to three ring nitrogen atoms and optionally containing one or more additional heteroatoms; Q is an alkyl chain containing 1 to 12 carbon atoms and optionally containing a sulphur or one or two oxygen atoms; Q 1 is a group (C(R 2 )=C(R 3 )) a -(C(R 4 )=(C(R 5 )) wherein a is 0 or 1, R 2 , R 3 , R 4- and R 5 are the same or different, at least two being hydrogen and the other two being independently selected from hydrogen, halo, C 1-4 haloalkyl; X is oxygen or sulphur; and R 1 is selected from hydrogen and C 1-8 hydrocarbyl optionally substituted by dixalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C 1-6 alkoxy are described which have activity particularly against arthropod pests. Pesticidal formulations containing the compounds of the formula (1), their use in the control of pests and method for their preparation are also disclosed.

7. 发明公开

EP0254222A3 Quinolinoxy compounds, procedure for their synthesis and their application as antidotes 失效
标题翻译：喹啉氧化合物，其合成方法及其作为抗体的应用
公开(公告)号：EP0254222A3
公开(公告)日：1988-09-21
申请号：EP87110363
申请日：1987-07-17
申请人： HOECHST AKTIENGESELLSCHAFT
发明人： Sohn, Erich, Dr. , Handte, Reinhard, Dr. , Mildenberger, Hilmar, Dr. , Bauer, Klaus, Dr. , Bieringer, Hermann, Dr.
IPC分类号： C07D215/28 , C07D215/26 , C07D215/60 , C07D405/12 , C07D409/12 , C07D411/12 , A01N25/32 , A01N43/42
CPC分类号： C07D405/12 , A01N25/32 , C07D215/26 , C07D215/28 , C07D215/60 , C07D409/12 , C07D411/12

8. 发明公开

EP0086750A3 Use of quinoline derivatives in the protection of crop plants 失效
标题翻译：喹诺酮衍生物在保护作物植物中的应用
公开(公告)号：EP0086750A3
公开(公告)日：1984-03-28
申请号：EP83810059
申请日：1983-02-11
申请人： CIBA-GEIGY AG
发明人： Hubele, Adolf, Dr.
IPC分类号： A01N43/42 , A01N43/54 , C07D215/26 , C07D215/28 , C07D215/48 , C07D407/12 , C07D409/12 , C07D301/12
CPC分类号： C07D401/12 , A01N25/32 , C07D215/26 , C07D215/28 , C07D407/12 , C07D409/12

9. 发明公开

EP0094349A2 Verwendung von Chinolinderivaten zum Schützen von Kulturpflanzen 失效
标题翻译：为保护栽培植物使用的喹啉衍生物。
公开(公告)号：EP0094349A2
公开(公告)日：1983-11-16
申请号：EP83810186.3
申请日：1983-05-02
申请人： CIBA-GEIGY AG
发明人： Hubele, Adolf, Dr.
IPC分类号： C07D215/26 , C07D215/28 , C07D401/12 , C07D405/12 , C07D413/12 , A01N43/42
CPC分类号： C07D401/12 , A01N25/32 , A01N43/42 , C07D215/26 , C07D215/28 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Beim Verfahren zum Schützen von Kulturpflanzen gegen schädigende Wirkungen von Agrarchemikalien werden Chinolinderivate der Formel
worin

R 1 , R 2 und R 3 unabhängig voneinander Wasserstoff, Halogen, Nitro, Cyan, Alkyl oder Alkoxy,
R 4 , R 5 und Re unabhängig voneinander Wasserstoff, Halogen oder Alkyl,
X einen aliphatischen, acyclischen, gesättigten Kohlenwasserstoffrest mit 1 bis 3 Kohlenstoffatomen und
Y eine Carboxylgruppe oder ein Salz davon, eine Mercaptocarbonylgruppe oder ein Salz davon, eine Carbonsäureestergruppe, eine Carbonsäurethiolestergruppe, eine unsubstituierte oder substituierte Carbonsäureamidgruppe, ein cyclisiertes, unsubstituiertes oder substituiertes Derivat einer Carbonsäureamidgruppe oder eine Carbonsäurehydrazidgruppe oder X und Y zusammen einen unsubstituierten oder substituierten Tetrahydrofuran-2-on-Ring
bedeuten, unter Einschluss ihrer Säureadditionssalze und Metallkomplexe, oder Mittel, welche solche Derivate enthalten, eingesetzt. Es werden auch neue Chinolinderivate und ihre Herstellung beschrieben.
摘要翻译：在用来保护栽培植物免受的农业化学品的有害影响的方法是下式的喹啉衍生物其中R1，R2和R3独立地是氢，卤素，硝基，氰基，烷基或烷氧基，R4，R5和R6独立地是氢，卤素或烷基中，X为脂肪族，无环的，饱和的烃基为1至3个碳原子和Y是羧基或其盐，mercaptocarbonyl基或其盐，羧酸酯基，Carbonsäurethiolestergruppe，未取代或取代的羧酸酰胺基团，a的环化的，未取代或取代的衍生物甲酰胺或Carbonsäurehydrazidgruppe或X和Y一起表示未取代的或取代的四氢呋喃-2-环上，插入，包括它们的酸加成盐和金属配合物，或含有此类衍生物的组合物。新喹啉衍生物和它们的制备描述。

10. 发明公开

EP4194441A1 NITROXOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF 审中-实审
公开(公告)号：EP4194441A1
公开(公告)日：2023-06-14
申请号：EP21853559.9
申请日：2021-07-30
申请人： Jiangsu Yahong Meditech Co., Ltd. , Asieris Pharmaceuticals (Shanghai) Co., Ltd.
发明人： WU, Liang , DENG, Yijun , XIAO, Lu , PAN, Ke
IPC分类号： C07D215/28 , C07D401/04 , A61K31/47 , A61K31/4709 , A61K31/55 , A61K31/496 , A61K31/5377 , A61P35/00 , A61P31/00 , A61P13/00
摘要： The present invention discloses a nitroxoline derivative, a preparation method therefor, and use thereof. Specifically, the present discloses a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing same, and use thereof in treating infectious diseases or cancers. The compound of the present invention has excellent anti-tumor activity and antibacterial activity, and can be developed into a drug for treating tumors and infectious diseases. The definition of each group in general formula (I) is the same as that in the description.

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