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1. 发明授权

US5468750A Heterocycle-coupled substituted pyrrolo[3,2-c]pyridin-2-carboxylic acids 失效
标题翻译：杂环偶联取代的吡咯并[3,2-c]吡啶-2-羧酸
公开(公告)号：US5468750A
公开(公告)日：1995-11-21
申请号：US273943
申请日：1994-07-12
申请人： Andre Bachy , Laurent Fraisse , Peter Keane , Etienne Mendes , Jean-Claude Vernieres , Jacques Simiand
发明人： Andre Bachy , Laurent Fraisse , Peter Keane , Etienne Mendes , Jean-Claude Vernieres , Jacques Simiand
IPC分类号： A61K31/435 , A61P3/00 , A61P3/08 , C07D471/04 , C07D471/14 , C07D495/04 , C07D495/14 , A61K31/44 , A61K31/495
CPC分类号： C07D471/04 , C07D471/14 , C07D495/04 , C07D495/14
摘要： A compound of formula ##STR1## in which A represents S;R.sub.1 is selected from the group consisting of OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, phenyl, benzyl (C.sub.1 -C.sub.4)alkyl NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 ;R.sub.2 is selected from the group consisting of OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, and NZ.sub.1 Z.sub.2 ;R.sub.3 is selected from the group consisting of H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl, and benzyl;B is selected from the group consisting of phenyl; pyridyl; phenyl substituted by one or more groups selected from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 wherein Z.sub.1 and Z.sub.2 are selected, independently of each other, from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, formyl, and benzyl or --NZ.sub.1 Z.sub.2 is selected from the group consisting of pyrrolidinyl, piperidinyl, morpholino, hexahydroazepino, ##STR2## piperazino, piperazino substituted in position 4 by (C.sub.1 -C.sub.8)alkyl, benzyl or diphenylmethyl; and pyridyl substituted by one or more groups selected from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 wherein Z.sub.1 and Z.sub.2 are selected, independently of each other, from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, formyl, and benzyl, or NZ.sub.1 Z.sub.2 is selected from the group consisting of pyrrolidinyl, piperidinyl, morpholino, hyxahydroazepino, ##STR3## piperazino, and piperazino substituted in position 4 by (C.sub.1 -C.sub.8)alkyl, benzyl or diphenylmethyl; or its salt with an acid or a base.
摘要翻译：其中A表示S的式（Ⅰ）化合物; R1选自OH，（C1-C12）烷基，（C1-C12）烷氧基，苄氧基，苯基，苄基（C1-C4）烷基NZ1Z2和NZ1Z2; R2选自OH，SH，（C1-C4）烷氧基，（C1-C4）烷硫基和NZ1Z2; R 3选自H，（C 1 -C 4）烷基，（C 1 -C 4）烷硫基，（C 1 -C 4）烷氧基，苯基和苄基; B选自苯基; 吡啶基被选自卤素，（C1-C6）烷基，（C1-C6）烷氧基，CF3，CH2NZ1Z2和NZ1Z2中的一个或多个基团取代的苯基，其中Z1和Z2彼此独立地选自H，（C 1 -C 6）烷基，甲酰基和苄基或-NZ 1 Z 2选自吡咯烷基，哌啶基，吗啉代，六氢氮杂环庚烷，哌嗪子基，哌嗪基，其在第4位被（C 1 -C 8）烷基取代，苄基或二苯基甲基 ; 和被一个或多个选自卤素，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，CF 3，CH 2 NZ 1 Z 2和NZ 1 Z 2的基团取代的吡啶基，其中Z 1和Z 2彼此独立地选自H ，（C 1 -C 6）烷基，甲酰基和苄基，或NZ 1 Z 2选自吡咯烷基，哌啶基，吗啉代，杂环吖庚因，哌嗪子基和在位置4上被（C 1 -C 8）烷基取代的哌嗪基，苄基或二苯基甲基; 或其与酸或碱的盐。

2. 发明授权

US5360799A Substituted thienyl- or pyrrolylcarboxyclic acid derivatives, their preparation and medicines containing them 失效
标题翻译：取代的噻吩基或吡咯基羧基酸衍生物，其制备方法和含有它们的药物
公开(公告)号：US5360799A
公开(公告)日：1994-11-01
申请号：US109073
申请日：1993-08-19
申请人： Andre Bachy , Laurent Fraisse , Peter Keane , Etienne Mendes , Jean-Claude Vernieres , Jacques Simiand
发明人： Andre Bachy , Laurent Fraisse , Peter Keane , Etienne Mendes , Jean-Claude Vernieres , Jacques Simiand
IPC分类号： A61K31/435 , A61P3/00 , A61P3/08 , C07D471/04 , C07D471/14 , C07D495/04 , C07D495/14 , A61K31/44 , A61K31/55 , C07D413/14
CPC分类号： C07D471/04 , C07D471/14 , C07D495/04 , C07D495/14
摘要： Compounds of formula ##STR1## in which R.sub.1 represents OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, benzyl, phenyl, (C.sub.1 -C.sub.4)alkylNZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; R.sub.2 represents OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio or NZ.sub.1 Z.sub.2 ; R.sub.3 represents H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl or benzyl; A represents N and R represents H or (C.sub.1 -C.sub.4)alkyl which can be substituted by phenyl or NZ.sub.1 Z.sub.2 ; B represents phenyl which is coupled to the pyridyl ring and is optionally substituted by one or more groups chosen from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; and Z.sub.1 and Z.sub.2 represent, independently of each other, H, (C.sub.1 -C.sub.6) alkyl, formyl or benzyl, or they form with the nitrogen atom to which they are attached an optionally substituted saturated heterocycle and their salts.
摘要翻译：其中R 1表示OH，（C 1 -C 12）烷基，（C 1 -C 12）烷氧基，苄氧基，苄基，苯基，（C 1 -C 4）烷基NZ 1 Z 2或NZ 1 Z 2的式I化合物; R2代表OH，SH，（C1-C4）烷氧基，（C1-C4）烷硫基或NZ1Z2; R3表示H，（C1-C4）烷基，（C1-C4）烷硫基，（C1-C4）烷氧基，苯基或苄基; A表示N，R表示H或可被苯基或NZ1Z2取代的（C1-C4）烷基; B表示与吡啶基环偶联并且任选被一个或多个选自卤素，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，CF 3，CH 2 NZ 1 Z 2或NZ 1 Z 2的基团取代的苯基; 并且Z 1和Z 2彼此独立地表示H，（C 1 -C 6）烷基，甲酰基或苄基，或者与它们所连接的氮原子一起形成任选取代的饱和杂环及其盐。

3. 发明授权

US08304440B2 Combination of a bis-thiazolium salt or a precursor thereof and artemisinin or a derivative thereof for treating acute malaria 失效
标题翻译：双噻唑鎓盐或其前体与青蒿素或其衍生物的组合用于治疗急性疟疾
公开(公告)号：US08304440B2
公开(公告)日：2012-11-06
申请号：US12851747
申请日：2010-08-06
申请人： Laurent Fraisse , Henri Vial , Sharon Aurore Wein
发明人： Laurent Fraisse , Henri Vial , Sharon Aurore Wein
IPC分类号： A61K31/425 , A61K31/335 , A61K31/35
CPC分类号： A61K31/426 , A61K31/357 , A61K31/37 , A61K31/427 , Y02A50/411 , A61K2300/00
摘要： The present invention relates to a combination of antimalarial active ingredients, namely a bisthiazolium salt or a precursor thereof and artemisinin or derivatives thereof. The invention also relates to a pharmaceutical composition comprising such a combination and use thereof in the treatment and/or prevention of malaria.
摘要翻译：本发明涉及抗疟活性成分，即双噻唑盐或其前体与青蒿素或其衍生物的组合。本发明还涉及包含这种组合及其在治疗和/或预防疟疾中的用途的药物组合物。

4. 发明授权

US07842711B2 Indazolecarboxamide derivatives for the treatment and prevention of malaria 失效
标题翻译： Indazolecarboxamide衍生物用于治疗和预防疟疾
公开(公告)号：US07842711B2
公开(公告)日：2010-11-30
申请号：US11531332
申请日：2006-09-13
申请人： Hugues D'Orchymont , Laurent Fraisse , André Zimmermann
发明人： Hugues D'Orchymont , Laurent Fraisse , André Zimmermann
IPC分类号： A01N43/56 , A61K31/47 , A61K31/44 , A61K31/505 , A61K31/425 , A61K31/41
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4725 , A61K31/506 , Y02A50/411
摘要： The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.
摘要翻译：本发明涉及治疗或预防疟疾的方法，其包括向有需要的患者施用有效量的基础或加成形式的通式（I）的1H-吲唑-3-甲酰胺衍生物盐，或者以水合物或所述碱或酸加成盐的溶剂化物的形式存在。

5. 发明申请

US20110021467A1 INDAZOLECARBOXAMIDE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF MALARIA 审中-公开
标题翻译：用于治疗和预防疟疾的异吲哚酰胺衍生物
公开(公告)号：US20110021467A1
公开(公告)日：2011-01-27
申请号：US12896203
申请日：2010-10-01
申请人： Hugues D'ORCHYMONT , Laurent Fraisse , André Zimmermann
发明人： Hugues D'ORCHYMONT , Laurent Fraisse , André Zimmermann
IPC分类号： A61K31/635 , A61K31/444 , A61K31/4725 , A61K31/4439 , A61P33/06 , A61P33/02
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4725 , A61K31/506 , Y02A50/411
摘要： The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.
摘要翻译：本发明涉及治疗或预防疟疾的方法，其包括向有需要的患者施用有效量的基础或加成形式的通式（I）的1H-吲唑-3-甲酰胺衍生物盐，或者以水合物或所述碱或酸加成盐的溶剂化物的形式存在。

6. 发明授权

US06634442B1 Process for using biodegradable drilling muds 有权
标题翻译：使用生物降解钻井泥浆的方法
公开(公告)号：US06634442B1
公开(公告)日：2003-10-21
申请号：US09744284
申请日：2001-05-07
申请人： Josiane Durrieu , Christian Zurdo , Alain Rabion , Laurent Fraisse , Michel Guillerme
发明人： Josiane Durrieu , Christian Zurdo , Alain Rabion , Laurent Fraisse , Michel Guillerme
IPC分类号： E10K700
CPC分类号： C09K8/34 , C09K8/36
摘要： Process for using biodegradable drilling muds, characterized in that a able surface sludge which is stable up to about 100° C., with an adjustable filtrate-reducing power of from 2 to 13 cm3 depending on the amount of filtrate-reducing agent used, and with an electrical stability of greater than or equal to 1000 volts, is introduced into the well at the start of drilling, and in that, when the temperature of the terrain passed through reaches 100° C., the surface sludge is replaced with a bottom sludge which is stable at a temperature above 200° C., the volume of the surface sludge representing from 60 to 80% by volume relative to the total volume of sludge used.
摘要翻译：使用可生物降解的钻井泥浆的方法，其特征在于可生物降解的表面污泥，其稳定性高达约100℃，可调节的滤液减少功率为2至13cm 3，这取决于滤液还原剂的量使用，并具有大于或等于1000伏的电气稳定性，在钻井开始时被引入井中，并且当通过的地形温度达到100℃时，表面污泥被替换具有在200℃以上稳定的底部污泥，表面污泥的体积相对于所用污泥的总体积为60〜80体积％。

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