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11. 发明授权

US06583159B1 Substitute 1-(piperidin-4-yl)-3-(aryl)-isothioureas, their preparation and therapeutic use 失效
标题翻译：替代1-（哌啶-4-基）-3-（芳基） - 异硫脲，其制备和治疗用途
公开(公告)号：US06583159B1
公开(公告)日：2003-06-24
申请号：US09889811
申请日：2001-07-20
申请人： Jean-François Patoiseau , Jean-Pierre Rieu , Gareth John , Bruno Legrand , Yvan Verscheure
发明人： Jean-François Patoiseau , Jean-Pierre Rieu , Gareth John , Bruno Legrand , Yvan Verscheure
IPC分类号： A61K31445
CPC分类号： C07D211/58
摘要： The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.
摘要翻译：本发明涉及式（I）的化合物，其中：R 1和R 2相同或不同，表示饱和或不饱和的烷基，分支或不具有1至7个碳原子; R3至R8相同或不同，表示氢，支链或不支链，含有1至5个碳原子的烷基，酰氧基，支链或不支化，含有1至5个碳原子，卤代，硝基，羟基，酰基或烷氧基含有1至5个碳原子的二烷基氨基，含有1至5个碳原子的二烷基氨基，三氟甲基或三氟甲氧基; Z表示氧或硫原子或亚甲基; m表示0和4之间的整数; n表示2〜7的整数，和它们的纯对映异构体和混合物，式（I）化合物的治疗上可接受的矿物或有机盐及其可能的水合物。

12. 发明授权

US08546402B2 Chromone derivatives, a process for their preparation and their therapeutic applications 有权
标题翻译：色酮衍生物，其制备方法及其治疗应用
公开(公告)号：US08546402B2
公开(公告)日：2013-10-01
申请号：US13393542
申请日：2010-08-31
申请人： Pierre Sokoloff , Thierry Imbert , Ludovic Leriche , Jean-François Patoiseau , Jean-Pierre Rieu
发明人： Pierre Sokoloff , Thierry Imbert , Ludovic Leriche , Jean-François Patoiseau , Jean-Pierre Rieu
IPC分类号： A61K31/496 , C07D405/06
CPC分类号： C07D311/22 , C07D405/12 , C07D413/12 , C07D493/04
摘要： The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.
摘要翻译：本发明涉及色酮衍生物，其制备方法，其药物组合物及其作为D3多巴胺能配体作为中枢神经系统病症药物的应用。

13. 发明申请

US20120178678A1 DERIVATIVES OF 2H PYRIDAZIN- 3 -ONES, THEIR PREPARATION AND THEIR USE AS SCD-1 INHIBITORS 有权
标题翻译： 2H吡啶-3-酮的衍生物，其制备及其作为SCD-1抑制剂的用途
公开(公告)号：US20120178678A1
公开(公告)日：2012-07-12
申请号：US13388884
申请日：2010-08-05
申请人： Elisabeth Dupont-Passelaigue , Samuel Mialhe , Jean-Pierre Rieu , Didier Junquero , Karine Valeille
发明人： Elisabeth Dupont-Passelaigue , Samuel Mialhe , Jean-Pierre Rieu , Didier Junquero , Karine Valeille
IPC分类号： A61K31/501 , C07D403/12 , C07D401/06 , A61P3/04 , A61P3/10 , A61P3/06 , A61P3/00 , A61P9/10 , A61P1/16 , A61P9/00 , A61P35/00 , A61P17/00 , A61P17/10 , A61P17/06 , A61P17/08 , A61K38/28 , A61K38/26 , A61K31/513 , A61K38/22 , A61P31/04 , A61P5/28 , A61P35/02 , C12N9/99 , C07D401/12
CPC分类号： C07D237/22 , C07D401/12 , C07D403/12
摘要： The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: —R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, —when n=m=1, W represents CH then Y represents oxygen, —U represents: either —(C═O)CH2NH— and is branched at position 4 of pyridazinone, then R2 represents H, or —(C═O)NH— and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, —R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders.
摘要翻译：本发明涉及通式（I）的化合物，其特征在于（式1）其中特别地：-R 1表示一个或多个基团，例如三氟甲基，卤素如F，Cl， - 当n = m = 1时， W表示CH，Y表示氧，-U表示： - （C = O）CH 2 NH-，并且在哒嗪酮的4位具有支链，则R2表示H或 - （C = O）NH-，U在（4），（5）或（6），则R2表示H，-R3表示氢或甲基，加成盐与药学上可接受的碱和酸和不同的异构体，以及它们的混合物以任何比例用作用于治疗肥胖症，2型糖尿病和脂质疾病的SCD-1酶抑制剂。

14. 发明申请

US20120157463A1 CHROMONE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATIONS 有权
标题翻译：色酮衍生物，其制备方法及其治疗应用
公开(公告)号：US20120157463A1
公开(公告)日：2012-06-21
申请号：US13393542
申请日：2010-08-31
申请人： Pierre Sokoloff , Thierry Imbert , Jean-François Patoiseau , Jean-Pierre Rieu
发明人： Pierre Sokoloff , Thierry Imbert , Jean-François Patoiseau , Jean-Pierre Rieu
IPC分类号： A61K31/496 , C07D405/14 , C07D413/14 , A61K31/506 , A61P25/00 , A61P25/32 , A61P25/30 , A61P25/16 , A61P25/18 , A61P25/14 , A61P25/22 , A61P25/24 , C07D405/06 , A61P15/00
CPC分类号： C07D311/22 , C07D405/12 , C07D413/12 , C07D493/04
摘要： The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.
摘要翻译：本发明涉及色酮衍生物，其制备方法，其药物组合物及其作为D3多巴胺能配体作为中枢神经系统病症药物的应用。

15. 发明授权

US6011032A Heterocyclic compounds for treating myocardial ischemia 失效
标题翻译：用于治疗心肌缺血的杂环化合物
公开(公告)号：US6011032A
公开(公告)日：2000-01-04
申请号：US11207
申请日：1998-01-26
申请人： Jean-Pierre Rieu , Jean-Fran.cedilla.ois Patoiseau , Gareth W. John , Bruno Legrand , Jean-Pierre Valentin
发明人： Jean-Pierre Rieu , Jean-Fran.cedilla.ois Patoiseau , Gareth W. John , Bruno Legrand , Jean-Pierre Valentin
IPC分类号： A61K31/00 , A61K31/55 , A61K31/553 , A61K31/554 , A61P9/00 , A61P9/10 , C07D413/12 , C07D417/12 , A61K31/54 , A61K31/535 , C07D265/12 , C07D279/16
CPC分类号： C07D413/12 , C07D417/12
摘要： Substituted N-heterocyclyl-1-aryloxyalkyl-4-piperldineamines of formula (I) ##STR1## wherein each of R.sub.1 to R.sub.4, which are the same or different, is hydrogen, optionally branched C.sub.1-4 alkyl, optionally branched C.sub.1-4 alkyloxy, halo, nitro, hydroxy, or trifluoromethyl or trifluoromethoxyl; R.sub.5 is hydrogen, optionally branched C.sub.1-6 alkyl, optionally branched C.sub.7-12 phenylalkyl optionally substituted on the phenyl by one or more radicals having the same definition as R.sub.1 ; W and X are oxygen or sulphur; Y is C.sub.2-6 polymethylene or --CH.sub.2 --CH(OH)--CH.sub.2 --; and n is 0 or 1; and pure R or S isomers of said compounds, where applicable, as well as mixtures thereof, as well as therapeutically-acceptable organic or inorganic salts and hydrates of the compounds and a method for preparing the compounds and their use as drugs are all disclosed.
摘要翻译： PCT No.PCT / FR96 / 01176 Sec。 371日期1998年1月26日 102（e）1998年1月26日PCT PCT 1996年7月25日PCT公布。出版物WO97 / 05134 日期1997年2月13日，式（I）的取代的N-杂环基-1-芳氧基烷基-4-哌嗪胺其中R 1至R 4各自相同或不同，为氢，任选支链C 1-4烷基，任选支链C1- 4-烷氧基，卤素，硝基，羟基或三氟甲基或三氟甲氧基; R 5是氢，任选支链的C 1-6烷基，任意支化的C 7-12苯基烷基，其在苯基上被一个或多个与R 1相同定义的基团取代; W和X是氧或硫; Y为C2-6多亚甲基或-CH2-CH（OH）-CH2-; 并且n为0或1; 并且所有化合物的纯R或S异构体，如适用，以及其混合物，以及化合物的治疗上可接受的有机或无机盐和水合物，以及制备化合物的方法及其作为药物的用途。

16. 发明授权

US5071850A 2,3-dihydro-3-arylalkylaminoalkyl-4H-1,3-benzoxazin-4-one derivatives, their preparation and their application as medicinal products which are useful in therapy 失效
标题翻译： 2,3-二羟基-3-亚甲基氨基亚氨基-4H-1,3-苯并恶嗪-4-酮衍生物，其制备及其作为有用的治疗药物的应用
公开(公告)号：US5071850A
公开(公告)日：1991-12-10
申请号：US403757
申请日：1989-09-06
申请人： Jean-Pierre Rieu
发明人： Jean-Pierre Rieu
IPC分类号： A61K31/535 , A61K31/536 , A61K31/537 , A61P9/06 , A61P9/08 , A61P9/10 , A61P43/00 , C07D265/12 , C07D265/22 , C07D413/12 , C07D498/04
CPC分类号： C07D265/12 , C07D265/22
摘要： The invention relates to the new 3-arylalkylaminoalkyl-4H-1,3-benzoxazin-4-one derivatives of general formula ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen, a branched or unbranched lower alkyl group or an alkyloxy, halo, nitro, amino, acylamino or dialkylamino group, and R.sub.1 and R.sub.2 on one hand and R.sub.3, R.sub.4 on the other hand can fuse to give a divalent group and more especially --OCH.sub.2 O--, --OCH.sub.2 CH.sub.2 O-- and --CH.dbd.CH--CH.dbd.CH--; R.sub.5 and R.sub.6, which may be identical or different, denote a hydrogen, a saturated or unsaturated, branched or unbranched alkyl group containing from 1 to 15 carbon atoms or a cycloalkyl group, and R.sub.5 and R.sub.6 can fuse to give a --(CH.sub.2).sub.p -- group with p=2 to 7; R.sub.7 denotes a hydrogen, a saturated or unsaturated, branched or unbranched alkyl group containing from 1 to 15 carbon atoms, a cycloalkyl group, a substituted or unsubstituted aryl and a substituted or unsubstituted arylalkyl; the values of m and n, which may be identical or different, can vary from 1 to 4 inclusive; as well as the therapeutically acceptable organic or inorganic salts of I. The compounds are useful as medicinal products in the treatment of disorders of the cardiovascular system.
摘要翻译：本发明涉及通式为I的新的3-芳基烷基氨基烷基-4H-1,3-苯并恶嗪-4-酮衍生物，其中：R 1，R 2，R 3和R 4可以相同或不同，表示氢，支链或非支链的低级烷基或烷氧基，卤素，硝基，氨基，酰氨基或二烷基氨基，另一方面R 1和R 2与R 3，R 4可以融合，得到二价基团，更特别是-OCH 2 O - ，-OCH 2 CH 2 O-和-CH = CH-CH = CH-; R5和R6可以相同或不同，表示氢，饱和或不饱和的，支链或非支链的含有1至15个碳原子的烷基或环烷基，R5和R6可以融合，得到 - （CH 2） p = 2〜7; R7表示氢，含有1至15个碳原子的饱和或不饱和支链或非支链烷基，环烷基，取代或未取代的芳基和取代或未取代的芳基烷基; 可以相同或不同的m和n的值可以在1到4之间变化; 以及I的治疗上可接受的有机或无机盐。该化合物可用作治疗心血管系统疾病的药物。

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