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1. 发明申请

WO2004006922A1 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA 审中-公开
标题翻译：作为低密度脂蛋白受体表达诱导剂治疗高脂血症的ARYL哌啶衍生物
公开(公告)号：WO2004006922A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007612
申请日：2003-07-11
申请人： GLAXO GROUP LIMITED , BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
发明人： BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
IPC分类号： A61K31/445
CPC分类号： C07D401/04 , C07D211/14 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines of formula (I) and their use in therapy.
摘要翻译：本发明涉及上调LDL受体（LDL-r）表达的新化合物及其制备方法，含有它们的药物组合物及其医疗用途。更具体地，本发明涉及式（I）的新型芳族哌啶及其在治疗中的用途。

2. 发明申请

WO2004006924A1 ARYL PIPERIDINE DERIVATIVES AND USE THEREOF TO REDUCE ELEVATED LEVELS OF LDL-CHOLESTEROL 审中-公开
标题翻译： ARYL PIPERIDINE衍生物及其用途，以降低LDL-胆固醇的高度水平
公开(公告)号：WO2004006924A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007615
申请日：2003-07-11
申请人： GLAXO GROUP LIMITED , BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
发明人： BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
IPC分类号： A61K31/445
CPC分类号： C07D413/12 , C07D211/22 , C07D417/12
摘要： This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines and their use in therapy.
摘要翻译：本发明涉及上调LDL受体（LDL-r）表达的新化合物及其制备方法，含有它们的药物组合物及其医疗用途。更具体地说，本发明涉及新型芳香族哌啶及其在治疗中的应用。

3. 发明申请

WO2004006923A1 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA 审中-公开
标题翻译：作为低密度脂蛋白受体表达诱导剂治疗高脂血症的ARYL哌啶衍生物
公开(公告)号：WO2004006923A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007613
申请日：2003-07-11
申请人： GLAXO GROUP LIMITED , BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
发明人： BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
IPC分类号： A61K31/445
CPC分类号： C07D401/04 , C07D207/16 , C07D211/22 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression. and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines of formula (I) and their use in therapy. wherein Ar 1 is substituted, by at least one R 1 group selected from: -O(CR a R b ) n C(O)NR X R y , -O(CH 2 ) n CN, -O(CH 2 )nO(CH 2 ) m OR 2 , -O(CH 2 )nCO 2 R 2 , -OS0 2 NR x R y , -OSO 2 (CH 2 ) p CH 3 , -(CR a R b ) n C(O)NR X R y , -(CH 2 ) n CN, -(CH 2 ) n O(CH 2 )mOR 2 , -(CH 2 ) n CO 2 R 2 , -(CH 2 ) n C(O)R 2 , - SO 2 NR x R y , -SO 2 (CH 2 ) p CH 3 , -CH=CHC(O)NR x R y , -CH=CHCN, -CH=CHCO 2 R 2 , -CO 2 R 2 , - C(O)R 2 , -C(O)NR x R y and C 2-5 alkenyl.
摘要翻译：本发明涉及上调LDL受体（LDL-r）表达的新化合物。及其制备方法，含有它们的药物组合物及其医疗用途。更具体地，本发明涉及式（I）的新型芳族哌啶及其在治疗中的用途。其中Ar 1被至少一个选自以下的R 1取代：-O（CR a R b）n C（O）NR X R y，-O（CH 2）n CN，-O（CH 2）n O ）mOR 2，-O（CH 2）n CO 2 R 2，-OSO 2 NR x R y，-OSO 2（CH 2）p CH 3， - （CR a R b）n C（O）NR X R y， - （CH 2）nCN， - （CH 2）（CH2）mOR2， - （CH2）nCO2R2， - （CH2）nC（O）R 2，-SO2NRxRy，-SO2（CH2）pCH3，-CH = CHC（O）NRxRy， -CH = CHCN，-CH = CHCO 2 R 2，-CO 2 R 2，-C（O）R 2，-C（O）NR x R y和C 2-5烯基。

4. 发明申请

WO2004007493A1 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA 审中-公开
标题翻译：作为低密度脂蛋白受体表达诱导剂治疗高脂血症的ARYL哌啶衍生物
公开(公告)号：WO2004007493A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007617
申请日：2003-07-11
申请人： GLAXO GROUP LIMITED , BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
发明人： BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
IPC分类号： C07D417/12
CPC分类号： C07D417/12 , C07D211/22 , C07D417/14
摘要： This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines of formula (I) and their use in therapy. wherein Ar 1 is substituted by at least one R' group selected from: -O(CR a R b ) n C(O)NR x R y ,. -O(CH 2 ) n CN, -O(CH 2 )nO(CH2) m OR 2 , -O(CH 2 )nCO 2 R 2 , -OSO 2 NR X R y , -OSO 2 (CH 2 ) p CH 3 , -(CR a R b ) n C(O)NR X R y , -(CH 2 ) n CN, -(CH 2 )nO(CH 2 ) m OR 2 , -(CH 2 ) n CO 2 R 2 , -(CH 2 )nC(O)R 2 , - SO 2 NR X R y , -SO 2 (CH 2 ) p CH 3 , -CH=CHC(O)NR x R y , -CH=CHCN, -CH=CHCO 2 R 2 , -CO 2 R 2 , - C(O)R 2 , -C(O)NR X R y and C 2-5 alkenyl; and Ar 2 is substituted by 1-4 groups independently selected from the group consisting of: (CH 2 ) n OH and -C0 2 (CH 2 ) p CH 3 .
摘要翻译：本发明涉及上调LDL受体（LDL-r）表达的新化合物及其制备方法，含有它们的药物组合物及其医疗用途。更具体地说，本发明涉及式（I）的新型芳族哌啶及其在治疗中的用途。其中Ar 1被至少一个选自以下的R 1基团取代：-O（CR a R b）n C（O）NR x R y。 -O（CH2）nCN，-O（CH2）nO（CH2）mOR2，-O（CH2）nCO2R2，-OSO2NRXRy，-OSO2（CH2）pCH3， - （CRαR）nC（O）NRXRy， - （CH2）nCN， - （CH2）nO（CH2）mOR2， - （CH2）nCO2R2， - （CH2）nC（O） SO 2 NR X R y，-SO 2（CH 2）p CH 3，-CH = CHC（O）NR x R y，-CH = CHCN，-CH = CHCO 2 R 2，-CO 2 R 2，-C（O）R 2，-C O）NR X R y和C 2-5烯基; 并且Ar 2被独立地选自：（CH 2）n OH和-CO 2（CH 2）p CH 3的1-4个基团取代。

5. 发明申请

WO2002096894A1 THIAZOLE OR OXAZOLE DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT OF CARDIOVASCULAR AND RELATED DISEASES 审中-公开
标题翻译：可用于治疗心血管和相关疾病的噻唑或氧唑衍生物
公开(公告)号：WO2002096894A1
公开(公告)日：2002-12-05
申请号：PCT/EP2002/005885
申请日：2002-05-29
申请人： GLAXO GROUP LIMITED , DUMAITRE, Bernard, Andre , GOSMINI, Romain, Luc, Marie
发明人： DUMAITRE, Bernard, Andre , GOSMINI, Romain, Luc, Marie
IPC分类号： C07D277/56
CPC分类号： C07D417/06 , C07D277/56
摘要： A compound of formula (1) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof: wherein R 1 and R 2 are independently H or C 1-3 alkyl or R 1 and R 2 which are bonded to the same carbon atom may together with the carbon atom to which they are bonded form a 3-5 membered cycloalkyl ring; X 1 represents O or S; Each R 3 , R 4 , R 8 and R 9 independently represents H, halogen, -CH 3 and OCH 3 ; R 5 represents H or C 1-6 alkyl or R 4 and R 5 together form a 3-6 membered cycloalkyl ring. X 2 represents NH, NCH 3 or O; One of Y and Z is N, and the other is O or S; R 6 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one more halogen, CF 3 , C 1-6 straight or branched alkyl (optionally substituted by halogen), with the provision that when R 6 is pyridyl, the N is unsubstituted. R 7 represents C 1-6 alkyl, (optionally substituted by one or halogens), -C 0-6 alkyl-5 membered heteroaryl C 0-6 alkyl (O) n - phenyl, wherein n is 0 or 1, with the proviso that when R 1 and R 2 are methyl, R 8 and R 9 are H, R 5 is H, then R 7 cannot be CH 3 or CF 3 .
摘要翻译：式（1）的化合物及其药学上可接受的盐，溶剂合物和可水解的酯：其中R 1和R 2独立地是H或C 1-3烷基或R 1和R 2，它们与相同的碳原子可以与它们所键合的碳原子一起形成3-5元环烷基环; X1表示O或S; 每个R 3，R 4，R 8和R 9独立地表示H，卤素，-CH 3和OCH 3; R 5表示H或C 1-6烷基或R 4和R 5一起形成3-6元环烷基环。 X2表示NH，NCH 3或O; Y和Z之一是N，另一个是O或S; R 6表示苯基或吡啶基（其中N在2或3位），并且任选地被另外一个卤素，CF 3，C 1-6直链或支链烷基（任选被卤素取代）取代，其条件是当R 6是吡啶基，N是未取代的。 R 7表示C 1-6烷基（任选被一个或多个卤素取代），-C 0-6烷基-5-元杂芳基C 0-6烷基（O）n - 苯基，其中n为0或1，条件是当R 1和R 2为甲基时，R 8和R 9为H，R 5为H，则R 7不能为CH 3或CF 3。

6. 发明申请

WO2004000785A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2004000785A2
公开(公告)日：2003-12-31
申请号：PCT/EP2003/006417
申请日：2003-06-18
申请人： SMITHKLINE BEECHAM CORPORATION , DODIC, Nerina , DUMAITRE, Bernard, Andre , GELLIBERT, Francoise, Jeanne , SIERRA, Michael, Lawrence
发明人： DODIC, Nerina , DUMAITRE, Bernard, Andre , GELLIBERT, Francoise, Jeanne , SIERRA, Michael, Lawrence
IPC分类号： C07C229/00
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：

7. 发明公开

EP1351937A1 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION 审中-公开
标题翻译： ARYL哌啶衍生物作为LDL-受体表达的诱导剂
公开(公告)号：EP1351937A1
公开(公告)日：2003-10-15
申请号：EP01900548.7
申请日：2001-01-15
申请人： GLAXO GROUP LIMITED
发明人： BOUILLOT, Anne M. J. , BOMBRUN, Agnes , DUMAITRE, Bernard, Andre , GOSMINI, Romain, Luc, Marie , CONGREVE, Miles Stuart
IPC分类号： C07D211/14 , A61K31/445 , C07D211/26 , C07D417/12 , A61P3/06
CPC分类号： C07D417/12 , A61K31/445 , C07D211/22
摘要： The invention relates to a compound of formula (I), wherein Ar1 represents phenyl, naphthyl or phenyl fused by a C3-8cycloalkyl, where each group is optionally substituted by methylenedioxy or one or two groups independently represented by R1; Ar2 represents phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from halogen, C1-4 alkyl and C1-4 alkoxy; Ar3 represents a phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from hydroxy, alkyl, C1-4 alkoxy, C2-4 alkenyl, C2-4 alkenyloxy, C1-4 perfluoroalkoxy, C1-4 acylamino or an electron withdrawing group; A represents -C(H)-; E represents -C1-6 alkylene-; X represents -CON(H or C1-4alkyl)- or -N(H or C1-4alkyl)CO-; Y represents a direct link; R1 represents halogen, -S(C¿1-4? alkyl)-, -O-(C0-4 alkylene)-R?2¿ or -(C¿0-4?alkylene)-R?2¿, where each alkylene group may additionally incorporate an oxygen in the chain, with the proviso that there are at least two carbon atoms between any chain heteroatoms; R2 represents: i) hydrogen, C¿1-4? perfluoroalkyl, C2-3 alkenyl, ii) phenyl, naphthyl, a 5- or 6-membered heteroaromatic group or 1,2,3,4-tetrahydronaphthyl, optionally substituted by one or two halogen, hydroxy, C1-4 alkyl, C1-4 alkoxy groups, iii) C3-8cycloalkyl, a 3-7 membered heterocycloalkyl, iv) amino, C1-4 alkylamino or di-C1-4alkylamino, with the proviso that there are at least two carbon atoms between any chain heteroatoms; to salts, solvates and compositions thereof and their use in treating disorders associated with elevated levels of circulating LDL-cholesterol.
摘要翻译：本发明涉及式（I）的化合物，其中Ar1代表被C3-8环烷基稠合的苯基，萘基或苯基，其中每个基团任选被亚甲二氧基或一个或两个独立代表R1的基团取代; Ar 2表示苯基或5-6元杂芳族基团，其中每个基团任选被1-4个独立地选自卤素，C 1-4烷基和C 1-4烷氧基的基团取代; Ar 3代表苯基或5-6元杂芳族基团，其中每个基团任选被1-4个独立地选自羟基，烷基，C 1-4烷氧基，C 2-4烯基，C 2-4烯氧基，C 1-4全氟烷氧基，C 1-4酰基氨基或吸电子基团; A代表-C（H） - ; E表示-C 1-6亚烷基 - ; X代表-CON（H或C 1-4烷基） - 或-N（H或C 1-4烷基）CO-; Y代表直接联系; R 1代表卤素，-S（C 1-4 - 烷基） - ， - O-（C 0-4亚烷基）-R 2'或 - （C 0-4亚烷基）-R 2'，其中每个亚烷基可另外在链中引入氧，条件是在任何链杂原子之间存在至少两个碳原子; R2代表：i）氢，C 1-4 - 全氟烷基，C 2-3烯基，ii）苯基，萘基，任选被一个或两个卤素取代的5-或6-元杂芳族基团或1,2,3,4-四氢萘基，羟基，C 1-4烷基， 4烷氧基，iii）C 3-8环烷基，3-7元杂环烷基，iv）氨基，C 1-4烷基氨基或二-C 1-4烷基氨基，条件是在任何链杂原子之间存在至少两个碳原子; 涉及它们的盐，溶剂化物和组合物以及它们在治疗与循环LDL-胆固醇水平升高相关的病症中的用途。

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