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1. 发明申请

US20060247233A1 Thiazoles inhibitors of the alk-5 receptor 审中-公开
标题翻译：噻唑抑制剂的alk-5受体
公开(公告)号：US20060247233A1
公开(公告)日：2006-11-02
申请号：US10560691
申请日：2004-06-14
申请人： Nerina Dodic , Frederic Donche , Jeanne Gellibert
发明人： Nerina Dodic , Frederic Donche , Jeanne Gellibert
IPC分类号： A61K31/538 , A61K31/4709 , A61K31/4439 , A61K31/427 , C07D417/14
CPC分类号： C07D417/14
摘要： The invention relates to novel aminothiazole derivatives which are inhibitors of the transforming growth factor, (“TGF”)-β signaling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase (“ALK”)-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway
摘要翻译：本发明涉及作为转化生长因子（“TGF”）-β信号通路抑制剂的新型氨基噻唑衍生物，特别是TGF-βI型或激活素样激酶（“ALK”）的smad2或smad3的磷酸化 “）-5受体，其制备方法及其在医学中的用途，特别是治疗和预防由该途径介导的疾病状态

2. 发明申请

US20050234029A1 Compounds 审中-公开
标题翻译：化合物
公开(公告)号：US20050234029A1
公开(公告)日：2005-10-20
申请号：US10522967
申请日：2003-07-29
申请人： Nerina Dodic , Francoise Gellibert
发明人： Nerina Dodic , Francoise Gellibert
IPC分类号： A61K31/444 , A61K31/496 , A61K31/5377 , A61P1/04 , A61P1/16 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/02 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/28 , A61P25/32 , A61P27/02 , A61P31/12 , A61P41/00 , A61P43/00 , C07D471/04 , A61K31/33
CPC分类号： C07D471/04
摘要： The invention relates to novel imidazopyridine derivatives which are inhibitors of the transforming growth factor, (“TGF”)-β signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase (“ALK”)-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
摘要翻译：本发明涉及作为转化生长因子（“TGF”）-β信号通路的抑制剂的新的咪唑并吡啶衍生物，特别是TGF-βI型或激活素样激酶（“ALK”）的smad2或smad3的磷酸化 “）-5受体，其制备方法及其在医学中的用途，特别是治疗和预防由该途径介导的疾病状态。

3. 发明授权

US07241793B2 Phenyloxyalkanonic acid derivatives as hPPAR activators 失效
标题翻译：苯氧基亚油酸衍生物作为hPPAR活化剂
公开(公告)号：US07241793B2
公开(公告)日：2007-07-10
申请号：US10518347
申请日：2003-06-18
申请人： Nerina Dodic , Bernard André Dumaître , Francoise Jeanne Gellibert , Michael Lawrence Sierra
发明人： Nerina Dodic , Bernard André Dumaître , Francoise Jeanne Gellibert , Michael Lawrence Sierra
IPC分类号： A61K31/415 , A61K31/4155 , C07D231/38 , C07D231/12
CPC分类号： C07D231/12 , C07D231/38 , C07D271/06 , C07D277/28 , C07D277/42 , C07D409/12 , C07D417/12
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或可水解的酯，其中：

4. 发明申请

US20050222424A1 Phenyloxyalkanonic acid derivatives as hppar activators 失效
标题翻译：苯氧基碳酸衍生物作为hppar活化剂
公开(公告)号：US20050222424A1
公开(公告)日：2005-10-06
申请号：US10518347
申请日：2003-06-18
申请人： Nerina Dodic , Bernard Dumaitre , Francoise Gellibert , Michael Sierra
发明人： Nerina Dodic , Bernard Dumaitre , Francoise Gellibert , Michael Sierra
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/4245 , A61K31/426 , A61K31/427 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50 , A61P9/04 , A61P9/10 , A61P25/00 , A61P43/00 , C07D231/12 , C07D231/38 , C07D271/06 , C07D277/20 , C07D277/28 , C07D277/42 , C07D409/12 , C07D417/12 , C07D413/02 , C07D417/02 , C07D45/02 , C07D49/02
CPC分类号： C07D231/12 , C07D231/38 , C07D271/06 , C07D277/28 , C07D277/42 , C07D409/12 , C07D417/12
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或可水解的酯，其中：

5. 发明授权

US07022856B2 Carboline derivatives 失效
标题翻译：碳氢化合物衍生物
公开(公告)号：US07022856B2
公开(公告)日：2006-04-04
申请号：US10470407
申请日：2001-12-18
申请人： Mark W. Orme , Jason S. Sawyer , Agnes Bombrun , Romain L. Gosmini , Anne Bouillot , Nerina Dodic , Michael Sierra
发明人： Mark W. Orme , Jason S. Sawyer , Agnes Bombrun , Romain L. Gosmini , Anne Bouillot , Nerina Dodic , Michael Sierra
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.
摘要翻译：一般结构式的化合物及其化合物及其盐和溶剂化物的用途作为治疗剂。

6. 发明申请

US20060004051A1 Compounds 审中-公开
标题翻译：化合物
公开(公告)号：US20060004051A1
公开(公告)日：2006-01-05
申请号：US10522968
申请日：2003-07-29
申请人： Nerina Dodic , Francoise Gellibert
发明人： Nerina Dodic , Francoise Gellibert
IPC分类号： C07D417/14 , A61K31/5377 , A61K31/496 , A61K31/444
CPC分类号： C07D417/14
摘要： The invention relates to novel aminothiazole derivatives which are inhibitors of the transforming growth factor, (“TGF”)-β signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase (“ALK”)-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
摘要翻译：本发明涉及作为转化生长因子（“TGF”）-β信号通路抑制剂的新型氨基噻唑衍生物，特别是TGF-βI型或激活素样激酶（“ALK”）的smad2或smad3的磷酸化 “）-5受体，其制备方法及其在医学中的用途，特别是治疗和预防由该途径介导的疾病状态。

7. 发明授权

US5663179A Certain isoquinoline derivatives having anti-tumor properties 失效
标题翻译：某些具有抗肿瘤特性的异喹啉衍生物
公开(公告)号：US5663179A
公开(公告)日：1997-09-02
申请号：US356323
申请日：1994-12-29
申请人： Bernard Andre Dumaitre , Nerina Dodic , Alain Claude-Marie Daugan , Pascal Maurice Charles Pianetti
发明人： Bernard Andre Dumaitre , Nerina Dodic , Alain Claude-Marie Daugan , Pascal Maurice Charles Pianetti
IPC分类号： A61K31/165 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61K31/425 , A61K31/426 , A61K31/47 , A61K31/472 , A61K31/54 , A61K31/5415 , A61P35/00 , C07C233/70 , C07C233/75 , C07C233/80 , C07C235/84 , C07D209/42 , C07D215/48 , C07D215/52 , C07D215/54 , C07D217/02 , C07D217/04 , C07D217/18 , C07D217/26 , C07D241/44 , C07D241/46 , C07D277/20 , C07D277/56 , C07D279/20 , C07D311/86 , C07D335/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , A61K31/44 , C07D407/12
CPC分类号： C07D401/12 , C07C233/70 , C07C233/75 , C07D209/42 , C07D215/48 , C07D215/52 , C07D217/04 , C07D217/26 , C07D241/44 , C07D241/46 , C07D335/16 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07C2103/18
摘要： Compounds are described of general formula (I) ##STR1## and salts and solvates thereof, including physiologically acceptable salts and solvates thereof, in which:Z represents either Het, ##STR2## Het represents an optionally substituted bicyclic or tricyclic ring selected from acricine isoquinolin-1-yl, isoquinolin-3-yl,The novel compounds of formula (I) can sensitize multi-drug resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an anti-tumour drug.
摘要翻译： PCT No.PCT / EP93 / 01802 Sec。 371日期1994年12月29日第 102（e）1994年12月29日PCT PCT 1993年8月8日PCT公布。出版物WO94 / 01408 日本1994年1月20日化合物描述了通式（I）的化合物及其盐和溶剂合物，包括其生理学上可接受的盐和溶剂化物，其中：Z代表Het，或 Het 代表选自acricine异喹啉-1-基，异喹啉-3-基的任选取代的二环或三环。式（I）的新化合物可使多药耐药性癌细胞对化学治疗剂敏感，并可配制用于治疗，特别是改善或增加抗肿瘤药物的功效。

8. 发明申请

US20050245520A1 2-Phenylpyridin-4-yl derivatives as alk5 inhibitors 审中-公开
标题翻译： 2-苯基吡啶-4-基衍生物作为alk5抑制剂
公开(公告)号：US20050245520A1
公开(公告)日：2005-11-03
申请号：US10522969
申请日：2003-07-29
申请人： Nerina Dodic , Francoise Gellibert
发明人： Nerina Dodic , Francoise Gellibert
IPC分类号： A61K31/444 , A61K31/496 , A61K31/5377 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/02 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/28 , A61P27/02 , A61P29/00 , C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D521/00 , C07D413/14 , C07D43/14
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/14 , C07D417/14 , C07D471/04
摘要： This invention relates to novel 2-phenylpyridin-4-yl heterocyclyl derivatives which are inhibitors of the transforming growth factor, (“TGF”)-β signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase (“ALK”)-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
摘要翻译：本发明涉及作为转化生长因子（“TGF”）-β信号传导途径抑制剂的新型2-苯基吡啶-4-基杂环基衍生物，特别是TGF-βI型的smad2或smad3的磷酸化，激活素样激酶（“ALK”）-5受体，其制备方法及其在医学中的应用，特别是治疗和预防由该途径介导的疾病状态。

9. 发明授权

US5604237A Acridine derivatives 失效
标题翻译：吖啶衍生物
公开(公告)号：US5604237A
公开(公告)日：1997-02-18
申请号：US468620
申请日：1995-06-06
申请人： Bernard A. Dumaitre , Nerina Dodic
发明人： Bernard A. Dumaitre , Nerina Dodic
IPC分类号： A61K31/47 , A61K31/473 , A61P35/00 , A61P43/00 , C07C205/11 , C07C205/26 , C07C205/37 , C07C205/56 , C07D219/04 , C07D219/06 , C07D401/12 , A61K31/435
CPC分类号： C07D401/12 , C07C205/11 , C07C205/26 , C07C205/37 , C07C205/56 , C07D219/06
摘要： These are provided compounds of formula I ##STR1## wherein A represents an oxygen or a sulphur atom, a bond or a group (CH.sub.2).sub.1 NR.sup.9 (where 1 represents zero or 1 and R.sup.9 represents a hydrogen atom or a methyl group); B represents a C.sub.1-4 alkylene chain optionally substituted by a hydroxyl group, except that the hydroxyl group and moiety A can not be attached to the same carbon atom when A represents an oxygen or sulphur atom or a group (CH.sub.2).sub.1 NR.sup.9, or when A represents a bond B may also represent a C.sub.2-4 alkenylene chain; R.sup.3 represents a hydrogen atom or a C.sub.1-4 alkyl group; m represents 1 or 2; R.sup.7 represents a hydrogen atom or R.sup.3 and R.sup.7 together form a group --(CH.sub.2).sub.n -- where n represents 1 or 2. These compounds can sensitize multidrug-resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an antitumor drug.
摘要翻译：这些是式I化合物其中A表示氧或硫原子，键或基团（CH 2）1 NHR 9（其中1表示0或1，R 9表示氢原子或甲基）; B表示任选被羟基取代的C 1-4亚烷基链，除了当A表示氧或硫原子或基团（CH 2）1 NHR 9时，羟基和A部分不能连接到相同的碳原子上，或者当 A表示键B也可以表示C2-4亚链烯基; R3表示氢原子或C1-4烷基; m表示1或2; R7代表氢原子或R3和R7一起形成基团 - （CH 2）n - ，其中n表示1或2.这些化合物可使多重耐药性癌细胞对化学治疗剂敏感，并可配制用于治疗，特别是改善或增加抗肿瘤药物的功效。

10. 发明专利

AU8179901A Benzamide derivatives and their use as apob-100 and mtp inhibitors 未知
公开(公告)号：AU8179901A
公开(公告)日：2001-12-11
申请号：AU8179901
申请日：2001-06-01
申请人： GLAXO GROUP LTD , NERINA DODIC
发明人： DAUGAN ALAIN CLAUDE-MARIE
IPC分类号： C07D295/12 , A61K31/495 , A61K31/496 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P43/00 , C07D207/335 , C07D213/40 , C07D231/12 , C07D271/06 , C07D277/28 , C07D295/135 , C07D521/00
摘要： The present invention relates to a compound of formula (I); wherein R represents isopropyl or trifluoromethyl; R represents hydrogen, C1-4alkyl, chloro, fluoro or trifluoromethyl; R represents(i) phenyl, optionally substituted by cyano, halogen, trifluoromethyl or an optionally substituted 5-membered heteroaromatic group, where optional substitution is effected by C1-4alkyl, (ii) a 5-membered heteroaromatic group, optionally substituted by halogen, cyano or C1-4alkyl, (ii) aminocabonyl, or(iv) ethyl or eth-1-enyl; R represents cyano, methyl, acetyl, a 5-membered heteoaromatic group, optionally substituted by C1-4alkyl or phenyl or a group X-Y-Z; X represents a carboxy, oxo, C1-6alkylene, carboxamido or thiocarboxamido linking group; Y represents a direct link or C1-4alkylene, Z represents (i) hydrogen, (ii) trifluoromethyl, (iii) cyano, (iv) phenyl (v) a 5- or 6-membered heteroaromatic group, optionally substituted by C1-4alkyl, with the proviso that when X represents C1-4alkylene, Y and Z do not represent a direct link and hydrogen respectively, or when X represents oxo, Y and Z do not represent C1-6alkylene and hydrogen respectively; or a physiologically acceptable salt, solvate or derivative thereof, to compositions comprising the compound, processes for their preparation and their use in treating conditions ameliorated by an apoB-100 and/or MTP inhibitor.

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