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1. 发明申请

WO2017009651A1 2-AMINO-1,3,4-THIADIAZINE AND 2-AMINO-1,3,4-OXADIAZINE BASED ANTIFUNGAL AGENTS 审中-公开
标题翻译： 2-氨基-1,3,4-噻二嗪和2-氨基-1,3,4-氧杂吖啶基的抗真菌剂
公开(公告)号：WO2017009651A1
公开(公告)日：2017-01-19
申请号：PCT/GB2016/052132
申请日：2016-07-14
申请人： F2G LIMITED
发明人： SIBLEY, Graham Edward Morris , MALMSTRÖM, Lars Jonas , LARSSON, Johanna Maria
IPC分类号： C07D417/06 , C07D417/12 , C07D285/16 , A61K31/54 , A61P31/10
CPC分类号： C07D285/16 , A61K31/549 , A61K45/06 , A61P31/10 , C07D417/06 , C07D417/12
摘要： The invention provides a compound which is a diazine of formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt thereof, for use as an antifungal agent: (I) wherein X, N', C', A and E are as defined herein. The invention also provides a compound of Formula (I) as defined herein.
摘要翻译：本发明提供一种化合物，其为式（I）的二嗪或其互变异构体或其药学上可接受的盐，用作抗真菌剂：（I）其中X，N'，C'，A和E为本文定义。本发明还提供如本文定义的式（I）化合物。

2. 发明申请

WO2016079536A1 ANTIFUNGAL AGENTS 审中-公开
标题翻译：反真菌药
公开(公告)号：WO2016079536A1
公开(公告)日：2016-05-26
申请号：PCT/GB2015/053546
申请日：2015-11-20
申请人： F2G LIMITED
发明人： SIBLEY, Graham Edward Morris , LAW, Derek , OLIVER, Jason David , BIRCH, Michael
IPC分类号： C07D403/14 , A61K31/506 , A01N43/60 , A61P31/10
CPC分类号： A61K31/4025 , A61K31/496 , C07D403/14
摘要： The invention provides a pyrrole compound, which compound is (a)2-(1,5-dimethyl-3- phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2- oxoacetamideor a deuterated derivative thereof, or(b)2-(1,5-dimethyl-3-phenyl-1H-pyrrol- 2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)-3-hydroxyphenyl)-2-oxoacetamide or a deuterated derivative thereof, or (c) a prodrug of compound (a) or a prodrug of compound (b), or a pharmaceutically acceptable salt or agriculturally acceptable salt of (a), (b) or (c). Also provided are combinations and compositions comprising the compound and known antifungal agents. The invention also relates to the therapeutic use of a compound of the invention in prevention or treatment of fungal diseases. It also relates to the use of:2-(1,5-dimethyl-3-phenyl-1H- pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide or an agriculturally acceptable salt thereof, or 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4- (5-fluoropyrimidin-2-yl)piperazin-1-yl)-3-hydroxyphenyl)-2-oxoacetamide or an agriculturally acceptable salt thereof, as an agricultural fungicide.
摘要翻译：本发明提供一种吡咯化合物，该化合物是（a）2-（1,5-二甲基-3-苯基-1H-吡咯-2-基）-N-（4-（4-（5-氟嘧啶-2-基）哌啶-1-基）苯基）-2-氧代乙酰胺或其氘代衍生物，或（b）2-（1,5-二甲基-3-苯基-1H-吡咯-2-基）-N-（4- （4-（5-氟嘧啶-2-基）哌嗪-1-基）-3-羟基苯基）-2-氧代乙酰胺或其氘代衍生物，或（c）化合物（a）的前药或化合物 b）或（a），（b）或（c）的药学上可接受的盐或农业上可接受的盐。还提供了包含该化合物和已知抗真菌剂的组合和组合物。本发明还涉及本发明化合物在预防或治疗真菌疾病中的治疗用途。它还涉及2-（1,5-二甲基-3-苯基-1H-吡咯-2-基）-N-（4-（4-（5-氟嘧啶-2-基）哌嗪-1-基） - 基）苯基）-2-氧代乙酰胺或其农业上可接受的盐，或2-（1,5-二甲基-3-苯基-1H-吡咯-2-基）-N-（4-（4-（5- 氟代嘧啶-2-基）哌嗪-1-基）-3-羟基苯基）-2-氧代乙酰胺或其农业上可接受的盐作为农业杀真菌剂。

3. 发明申请

WO2017203270A1 PHARMACEUTICAL FORMULATION 审中-公开
标题翻译：药物制剂
公开(公告)号：WO2017203270A1
公开(公告)日：2017-11-30
申请号：PCT/GB2017/051494
申请日：2017-05-25
申请人： F2G LIMITED
发明人： LAW, Derek , SIBLEY, Graham Edward Morris
IPC分类号： A61K31/506 , A61K9/16 , A61P31/10
摘要： A pharmaceutical composition suitable for oral administration comprising particles of 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide is provided. Also provided is a pharmaceutical composition suitable for parenteral administration wherein the composition comprises 2-(1,5-dimethyl- 3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide. The compositions are useful in the treatment of fungal infection in a subject in need thereof.
摘要翻译：适用于口服的药物组合物包含2-（1,5-二甲基-3-苯基-1H-吡咯-2-基）-N-（4-（4-（5 - 氟嘧啶-2-基）哌嗪-1-基）苯基）-2-氧代乙酰胺。还提供了适用于肠胃外给药的药物组合物，其中组合物包含2-（1,5-二甲基-3-苯基-1H-吡咯-2-基）-N-（4-（4-（5-氟嘧啶-2 基）哌嗪-1-基）苯基）-2-氧代乙酰胺。该组合物可用于治疗有需要的受试者的真菌感染。

4. 发明申请

WO2009144473A1 ANTIFUNGAL COMBINATION THERAPY 审中-公开
标题翻译：反复组合治疗
公开(公告)号：WO2009144473A1
公开(公告)日：2009-12-03
申请号：PCT/GB2009/001357
申请日：2009-05-29
申请人： F2G LIMITED , BIRCH, Michael , SIBLEY, Graham, Edward, Morris , LAW, Derek , OLIVER, Jason, David
发明人： BIRCH, Michael , SIBLEY, Graham, Edward, Morris , LAW, Derek , OLIVER, Jason, David
IPC分类号： A61K45/06 , A61P31/10
CPC分类号： A61K45/06 , A61K31/437 , A61K2300/00
摘要： The invention provides pharmaceutical combinations comprising a combination of an antifungal indolizine compound of formula (I) or a pharmaceutically acceptable salt thereof and a second antifungal agent: wherein: Rl, R2, R3, R4, R5, R6, R7, X and X 1 are as defined herein. The invention also provides pharmaceutical compositions comprising an antifungal indolizine compound of formula (I) or a pharmaceuticall acceptable salt thereof, a second antifungal agent and a pharmaceutically acceptable diluent or carrier. The combinations and compositions are useful in the prevention or treatment of a fungal disease. A combination of an indolizine compound of formula (I) or agriculturally acceptable salts thereof and a second antifungal agent may also be used as an agricultural fungicide.
摘要翻译：本发明提供包含式（I）的抗真菌中氮茚化合物或其药学上可接受的盐与第二抗真菌剂的组合的药物组合：其中：R1，R2，R3，R4，R5，R6，R7，X和X1是如本文所定义。本发明还提供包含式（I）的抗真菌中氮茚化合物或其药学上可接受的盐，第二抗真菌剂和药学上可接受的稀释剂或载体的药物组合物。组合和组合物可用于预防或治疗真菌病。式（I）的中氮茚化合物或其农业上可接受的盐和第二抗真菌剂的组合也可以用作农业杀真菌剂。

5. 发明申请

WO2008145963A1 2-OXO-2- (2-PHENYL-5,6,7,8-TETRAHYDRO-INDOLIZIN-3-YL) -ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ANTIFUNGAL AGENTS 审中-公开
标题翻译： 2-氧代-2-（2-苯基-5,6,7,8-四氢 - 吲哚啉-3-基） - 乙酰胺衍生物及相关化合物作为抗真菌剂
公开(公告)号：WO2008145963A1
公开(公告)日：2008-12-04
申请号：PCT/GB2008/001738
申请日：2008-05-21
申请人： F2G LIMITED , PAYNE, Lloyd, James , DOWNHAM, Robert , SIBLEY, Graham, Edward, Morris , EDWARDS, Philip , DAVIES, Gareth, Morse
发明人： PAYNE, Lloyd, James , DOWNHAM, Robert , SIBLEY, Graham, Edward, Morris , EDWARDS, Philip , DAVIES, Gareth, Morse
IPC分类号： C07D471/04 , A61K31/437 , A01N43/40 , A61P31/10
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: Rl, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
摘要翻译：本发明提供式（I）化合物及其药用和农业上可接受的盐：其中：R1，R2，R3，R4，R5，R6，R7，R8，A1，L1和n如本文所定义。这些化合物及其药学上可接受的盐可用于制备用于预防或治疗真菌病的药物。式（I）化合物及其农业上可接受的盐也可以用作农业杀真菌剂。

6. 发明申请

WO2009133379A8 DIHYDROOROTATE DEHYDROGENASE AS ANTIFUNGAL DRUG TARGET AND QUINAZOLINONE-BASED INHIBITORS THEREOF 审中-公开
公开(公告)号：WO2009133379A8
公开(公告)日：2009-11-05
申请号：PCT/GB2009/001114
申请日：2009-05-01
申请人： F2G LIMITED , OLIVER, Jason, David , THAIN, John, Leslie , BROMLEY, Michael, John , SIBLEY, Graham, Edward, Morris , BIRCH, Michael
发明人： OLIVER, Jason, David , THAIN, John, Leslie , BROMLEY, Michael, John , SIBLEY, Graham, Edward, Morris , BIRCH, Michael
IPC分类号： C12Q1/32 , C12N9/02 , C07D239/72 , A61P31/10
摘要： A method of identifying an antifungal agent which targets a DHODH protein (alias PyrE, dihydroorotate dehydrogenase, EC: 1.3.99.11) of a fungus comprising contacting a candidate substance with a fungal DHODH protein and determining whether the candidate substance binds or modulates the DHODH protein, wherein binding or modulation indicates that the candidate substance is an antifungal agent. Specific examples concern Aspergillus fumigatus and Candida albicans DHODH proteins. DHODH inhibitors with a Quinazolinone core are also disclosed.

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