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1. 发明申请

WO1998028265A1 NITROMETHYLTHIOBENZENE DERIVATIVES AS INHIBITORS OF ALDOSE REDUCTASE 审中-公开
标题翻译：作为降糖酶抑制剂的硝基苯甲酮衍生物
公开(公告)号：WO1998028265A1
公开(公告)日：1998-07-02
申请号：PCT/EP1997006981
申请日：1997-12-12
申请人： MERCK PATENT GMBH , COLLONGES, François , DUMAS, Hervé , LARDY, Claude , DURBIN, Philippe
发明人： MERCK PATENT GMBH
IPC分类号： C07C317/34
CPC分类号： C07D307/91 , C07C317/34 , C07C317/40 , C07C317/42 , C07C323/49 , C07C2601/14 , C07D333/34
摘要： The invention concerns novel compounds of general formula (1) in which: P, T1, T2, X and n are as defined in claim 1, their tautomeric forms, and their additive salts with pharmaceutically acceptable bases. The invention also concerns methods for preparing these compounds and their applications as medicines. These compounds inhibit the aldose reductase enzyme and can be used in the treatment or prevention of peripheral and autonomous neurological diabetic complications, renal and ocular disorders such as cataract and retinopathy.
摘要翻译：本发明涉及通式（1）的新化合物，其中：P，T1，T2，X和n如权利要求1所定义，其互变异构形式及其与药学上可接受的碱的添加盐。本发明还涉及制备这些化合物及其作为药物的应用的方法。这些化合物抑制醛糖还原酶，可用于治疗或预防外周和自主神经性糖尿病并发症，肾和眼部疾病如白内障和视网膜病变。

2. 发明申请

WO9413658A3 BENZOCYCLOHEPTENES, BENZOXEPINES AND BENZOTHIEPINES 审中-公开
标题翻译：苯并环庚烯，苯并吖庚因和苯并吖庚因
公开(公告)号：WO9413658A3
公开(公告)日：1994-08-04
申请号：PCT/EP9303445
申请日：1993-12-07
申请人： MERCK PATENT GMBH , BERTHELON JEAN JACQUES , BRUNET MICHEL , NOBLET MARC , DURBIN PHILIPPE , GUERRIER DANIEL , LUONG TRONG NGHIA
发明人： BERTHELON JEAN-JACQUES , BRUNET MICHEL , NOBLET MARC , DURBIN PHILIPPE , GUERRIER DANIEL , LUONG TRONG NGHIA
IPC分类号： C07D215/14 , A61K31/355 , A61K31/55 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/08 , A61P17/00 , A61P21/02 , A61P25/02 , C07C57/30 , C07C59/68 , C07D213/24 , C07D213/30 , C07D213/57 , C07D213/60 , C07D213/89 , C07D313/08 , C07D405/04 , C07D409/04 , C07D493/04 , A61K31/335 , A61K31/38 , C07D213/26 , C07D337/08
CPC分类号： C07D213/30 , C07D213/57 , C07D213/89 , C07D405/04 , C07D409/04 , C07D493/04 , Y02P20/55
摘要： PCT No. PCT/EP93/03445 Sec. 371 Date Aug. 5, 1994 Sec. 102(e) Date Aug. 5, 1994 PCT Filed Dec. 7, 1993 PCT Pub. No. WO94/13658 PCT Pub. Date Jun. 23, 1994The subject of the invention is compounds of general formula: I in which: X represents O or CHR, R1, R2, R3 and R4, which are identical or different, represent a hydrogen atom or a C1-C7 alkyl group, it being possible for R1 to additionally form a bond with R; R5 represents a hydrogen atom, a hydroxyl group or R5, taken together with R7, forms a bond or a >O; group; R6 represents a group of formula: in which R10 and R11, taken together with the carbon atom to which they are attached, form a nitrogenous heterocyclic group, and their N-oxides and pharmaceutically acceptable salts. These compounds are powerful activators of potassium channels.
摘要翻译： PCT No.PCT / EP93 / 03445 371日期：1994年8月5日 102（e）日期1994年8月5日PCT 1993年12月7日PCT公布。公开号WO94 / 13658 日期1994年6月23日本发明的主题是下列通式的化合物：其中：X表示O或CHR，R1，R2，R3和R4相同或不同，表示氢原子或C1 -C 7烷基，R1可以另外与R形成键; R5代表氢原子，羟基或R5与R7一起形成键或a O; 组; R 6表示下式的基团：其中R 10和R 11与它们所连接的碳原子一起形成含氮杂环基，以及它们的N-氧化物和药学上可接受的盐。这些化合物是钾通道的强大激活剂。

3. 发明申请

WO2004028537A1 USE OF THIAZOLIDINEDIONE DERIVATIVES AS ALDOSE REDUCTASE INHIBITORS 审中-公开
标题翻译：噻唑烷二酮衍生物作为还原抑制剂的使用
公开(公告)号：WO2004028537A1
公开(公告)日：2004-04-08
申请号：PCT/EP2003/008888
申请日：2003-08-11
申请人： MERCK PATENT GMBH , MOINET, Gérard , BOTTON, Gérard , DURBIN, Philippe , MESANGEAU, Didier
发明人： MOINET, Gérard , BOTTON, Gérard , DURBIN, Philippe , MESANGEAU, Didier
IPC分类号： A61K31/425
CPC分类号： A61K31/427 , A61K31/425 , A61K31/426 , A61K38/28 , A61K2300/00
摘要： The present invention relates to the use of thiazolidinedione derivatives as aldose reductase inhibitors.
摘要翻译：本发明涉及噻唑烷二酮衍生物作为醛糖还原酶抑制剂的用途。

4. 发明申请

WO1994013658A2 BENZOCYCLOHEPTENES, BENZOXEPINES AND BENZOTHIEPINES 审中-公开
标题翻译：苯并噻唑啉，苯并吖庚因和苯并HI嗪
公开(公告)号：WO1994013658A2
公开(公告)日：1994-06-23
申请号：PCT/EP1993003445
申请日：1993-12-07
申请人： MERCK PATENT GMBH , BERTHELON, Jean-Jacques , BRUNET, Michel , NOBLET, Marc , DURBIN, Philippe , GUERRIER, Daniel , LUONG, Trong, Nghia
发明人： MERCK PATENT GMBH
IPC分类号： C07D313/08
CPC分类号： C07D213/30 , C07D213/57 , C07D213/89 , C07D405/04 , C07D409/04 , C07D493/04 , Y02P20/55
摘要： The subject of the invention is compounds of general formula (I), in which: X represents O or CHR; R1, R2, R3 and R4, which are identical or different, represent a hydrogen atom or a C1-C7 alkyl group, it being possible for R1 to additionally form a bond with R; R5 represents a hydrogen atom, a hydroxyl group or R5, taken together with R7, forms a bond or a O group; R6 represents a group of formula (a) in which R10 and R11, taken together with the carbon atom to which they are attached, form a nitrogenous heterocyclic group, and their N-oxides and pharmaceutically acceptable salts. These compounds are powerful activators of potassium channels.
摘要翻译：本发明的主题是通式（I）的化合物，其中：X表示O或CHR; R1，R2，R3和R4相同或不同，表示氢原子或C1-C7烷基，R1可以另外与R形成键; R5表示氢原子，羟基或R5，与R7一起形成键或 O基团; R 6表示其中R 10和R 11与它们所连接的碳原子一起形成含氮杂环基的式（a）基团及其N-氧化物和药学上可接受的盐。这些化合物是钾通道的强大激活剂。

5. 发明申请

WO2005021590A1 PROMOTER OF THE HUMAN FATP5 GENE AND USES 审中-公开
标题翻译：人类FATP5基因和用途的促销者
公开(公告)号：WO2005021590A1
公开(公告)日：2005-03-10
申请号：PCT/EP2004/008747
申请日：2004-08-04
申请人： MERCK PATENT GMBH , MARTIN, Geneviève , AUGERT, Guy , ASFARI, Maryam , DUPONT, Hervé , RUGGIERO, Daniel , DURBIN, Philippe
发明人： MARTIN, Geneviève , AUGERT, Guy , ASFARI, Maryam , DUPONT, Hervé , RUGGIERO, Daniel , DURBIN, Philippe
IPC分类号： C07K14/47
CPC分类号： C07K14/705
摘要： The invention relates to an isolated human nucleic acid, characterized in that it corresponds to the promoter of the human FATP5 protein, and to an isolated human nucleic acid coding for a protein, particularly for the human FATP5 protein, placed under the dependence of said promoter. The invention further relates to a vector comprising said nucleic acid, or to a host cell into which said nucleic acid or said vector has been introduced. Finally, the invention relates to the use of said nucleic acid, said vector or said host cell in a method of identifying a product capable of modulating the expression of a nucieotide sequence placed under the dependence of said promoter of the human FATP5 protein, and to said method of identification. The invention finally relates to the product capable of modulating the expression of a nucleotide sequence placed under the dependence of said promoter of the human FATP5 protein, and to the use of said product in the preparation of a drug for preventing and/or treating diabetes or for inducing the β oxidation of fatty acids in the liver.
摘要翻译：本发明涉及一种分离的人核酸，其特征在于它对应于人FATP5蛋白的启动子，以及编码一种分离的人核酸，其编码一种蛋白，特别是对于人FATP5蛋白，其置于所述启动子。本发明进一步涉及包含所述核酸的载体，或涉及引入了所述核酸或载体的宿主细胞。最后，本发明涉及所述核酸，所述载体或所述宿主细胞在鉴定能够调节在人FATP5蛋白的所述启动子的依赖下置换的核苷酸序列的表达的产物的方法中的用途，以及所述识别方法。本发明最终涉及能够调节在人FATP5蛋白的所述启动子的依赖下置换的核苷酸序列的表达的产物，以及所述产物在制备用于预防和/或治疗糖尿病的药物中的用途用于诱导肝脏中脂肪酸的β氧化。

6. 发明申请

WO1993007109A1 3,4-DIHYDRO-4-OXO-3-(PROP-2-ENYL)-1-PHTALAZINEACETIC ACIDS AND DERIVATIVES, PREPARATIONS THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译： 3,4-二氢-4-氧代-3-（丙-2-烯）-1-苯甲酸和衍生物，其制备物和含有其的药物
公开(公告)号：WO1993007109A1
公开(公告)日：1993-04-15
申请号：PCT/FR1992000920
申请日：1992-10-02
申请人： LIPHA, LYONNAISE INDUSTRIELLE PHARMACEUTIQUE , COLLONGES, François , DUMAS, Hervé , DURBIN, Philippe , GUERRIER, Daniel
发明人： LIPHA, LYONNAISE INDUSTRIELLE PHARMACEUTIQUE
IPC分类号： C07C22/04
CPC分类号： C07D409/06 , C07C17/00 , C07C17/14 , C07C17/16 , C07C17/2635 , C07C17/38 , C07C22/04 , C07C22/08 , C07C25/02 , C07C25/24 , C07C45/44 , C07C45/565 , C07D237/32 , C07D333/12 , C07C47/55
摘要： Novel 3,4-dihydro-4-oxo-3-(prop-2-enyl)-1-phtalazineacetic acids and derivatives of formula (I) in which R1, R2 and R3 are the same or different and stand for H, a halogen or a linear or branched aliphatic, saturated or unsaturated radical, substituted or not by at least one halogen or R4 residue such as defined below, except when R4 is H; R4 and R5 are the same or different and stand for H, a linear or branched aliphatic radical, saturated or unsaturated, an aryl or heteroaryl radical, said radicals being substituted or not by at least one grouping such as fluorine, chlorine, bromine, methyl or trifluoromethyl, where R4 and R5 do not simultaneously denote H; R6 stands for a hydroxy or alkoxy radical; R7 stands for H, a halogen, a linear or branched aliphatic saturated or unsaturated radical, an alkoxy radical, said radicals being substituted or not by an aliphatic or halogenated radical, a nitro group, a substituted or unsubstituted amino group, S(O)n R8 or a cyano group; n is equal to 0, 1 or 2; R8 is an aliphatic, linear or branched radical, an aryl or heteroaryl radical, an amino radical, said radicals being substituted or not by an aliphatic or halogenated radical. The invention also relates to the optional tautomeric forms of said acids and their pharmaceutically acceptable base addition salts. Also described is a process for preparing said compounds and the drugs containing same.

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