专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2005108360A1 PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译：吡咯烷-2-酮和哌啶-2-酮衍生物作为11-羟基甾醇脱氢酶抑制剂
公开(公告)号：WO2005108360A1
公开(公告)日：2005-11-17
申请号：PCT/EP2005/051968
申请日：2005-04-29
申请人： JANSSEN PHARMACEUTICA N.V. , JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , BUYCK, Christophe, Francis, Robert, Nestor , VAN DER VEKEN, Louis Jozef Elisabeth , DIMITROV, Vladimir, Dimtchev , NIKIFOROV, Theo, Teofanov
发明人： JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , BUYCK, Christophe, Francis, Robert, Nestor , VAN DER VEKEN, Louis Jozef Elisabeth , DIMITROV, Vladimir, Dimtchev , NIKIFOROV, Theo, Teofanov
IPC分类号： C07D207/26
CPC分类号： C07D211/76 , C07D207/26 , C07D207/267 , C07D405/06
摘要： Formula (I), the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C 1-3 alkyl linker optionally substituted with one or two substituents selected from C 1-4 alkyl, C 1-3 alkyloxy-C 1-4 alkyl-, hydroxy-C 1-4 alkyl, hydroxy, C 1-3 alkyloxy- or phenyl-C 1-4 alkyl; M represents a direct bond or a C 1-3 alkyl linker optionally substituted with one or two substituents selected from hydroxy, C 1-4 alkyl or C 1-4 alkyloxy; R 1 and R 2 each independently represent hydrogen, halo, cyano, hydroxy, C 1-4 alkyl optionally substituted with halo, C 1-4 alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar 1 and halo; or R 1 and R 2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R 3 represents hydrogen, halo, C 1-4 alkyl, C 1-4 alkyloxy-, cyano or hydroxy; R 4 represents hydrogen, halo, C 1-4 alkyl, C 1-4 alkyloxy-, cyano or hydroxy; R 5 represents hydrogen, C 1-4 alkyl or Ar 2 -C 1-4 alky-; R 6 represents hydrogen, halo, C 1-4 alkyl Or C 1-4 alkyoxy-; Ar 1 and Ar 2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C 1-4 alkyl, C 1-4 alkyloxy-, or phenyl-C 1-4 alkyl; for use as a medicine.
摘要翻译：式（I），N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n为1或2; L表示任选被一个或两个选自C 1-4烷基，C 1-3烷氧基-C 1-4烷基 - ，羟基-C 1-4烷基，羟基，C 1-3烷氧基或苯基-C 1-4烷基的取代基取代的C 1-3烷基接头。 M表示直接键或任选被一个或两个选自羟基，C 1-4烷基或C 1-4烷氧基的取代基取代的C 1-3烷基接头; R 1和R 2各自独立地表示氢，卤素，氰基，羟基，任选被卤素取代的C 1-4烷基，C 1-4烷氧基 - 任选被一个或任选被两个或三个选自羟基，Ar 1 >和光环; 或R 1和R 2与它们所连接的苯环一起形成萘基或1,3-苯并二恶唑基，其中所述萘基或1,3-苯并二恶唑基任选被卤素取代; R 3表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R 4表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R 5表示氢，C 1-4烷基或Ar 2 -C 1-4烷基; R 6表示氢，卤素，C 1-4烷基或C 1-4烷氧基 - ; Ar 1和Ar 2各自独立地表示苯基或萘基，其中所述苯基和萘基任选被C 1-4烷基，C 1-4烷氧基 - 或苯基-C 1-4烷基取代; 用作药物。

2. 发明申请

WO2006024628A1 TRICYCLIC LACTAM DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译：作为11-羟基甾醇脱氢酶抑制剂的三聚赖氨酸衍生物
公开(公告)号：WO2006024628A1
公开(公告)日：2006-03-09
申请号：PCT/EP2005/054198
申请日：2005-08-26
申请人： JANSSEN PHARMACEUTICA N.V. , JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , VAN DER VEKEN, Louis, Jozef, Elisabeth , WILLEMSENS, Gustaaf, Henri, Maria
发明人： JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , VAN DER VEKEN, Louis, Jozef, Elisabeth , WILLEMSENS, Gustaaf, Henri, Maria
IPC分类号： C07D209/64 , C07D471/04 , C07D495/04 , A61K31/403 , A61K31/407 , A61K31/437 , A61P3/00 , C07D209/60
CPC分类号： C07D471/04 , A61K31/4745 , A61K45/06 , C07D209/58 , C07D209/60 , C07D209/64 , C07D495/04
摘要： Compounds of formulae (I) and (I bis) are useful as 11BETA-HSD1 inhibitors for treatment of obesity.
摘要翻译：式（I）和（I bis）的化合物可用作治疗肥胖症的11BETA-HSD1抑制剂。

3. 发明申请

WO2006024627A2 N-2 ADAMANTANYL-2-PHENOXY-ACETAMIDE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： N-2 ADAMANTANYL-2-苯甲酰胺衍生物作为11-氢化羟基脱氢酶抑制剂
公开(公告)号：WO2006024627A2
公开(公告)日：2006-03-09
申请号：PCT/EP2005054197
申请日：2005-08-26
申请人： JANSSEN PHARMACEUTICA NV , JAROSKOVA LIBUSE , LINDERS JOANNES THEODORUS MARI , VAN DER VEKEN LOUIS JOZEF ELIS , WILLEMSENS GUSTAAF HENRI MARIA , BISCHOFF FRANCOIS PAUL
发明人： JAROSKOVA LIBUSE , LINDERS JOANNES THEODORUS MARI , VAN DER VEKEN LOUIS JOZEF ELIS , WILLEMSENS GUSTAAF HENRI MARIA , BISCHOFF FRANCOIS PAUL
IPC分类号： A61K31/165 , A61P3/04 , A61P3/10 , A61P9/00 , A61P19/10 , A61P25/28 , A61P27/06 , C07C235/22 , C07D307/85 , C07D311/66 , C07D319/20
CPC分类号： A61K31/165 , C07C235/22 , C07C237/04 , C07C271/38 , C07C307/08 , C07C311/07 , C07C311/09 , C07C311/20 , C07C2603/74 , C07D207/27 , C07D263/20 , C07D265/36 , C07D295/32 , C07D307/85 , C07D311/66 , C07D319/20
摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1, 2, 3, or 4; Z represents O, S, NR 6 , SO or SO 2 ; R 1 represent hydrogen, cyano, hydroxy, or C 1-4 alkyl optionally substituted with halo, R 2 represents hydrogen, C 1-4 alkyl, or C 1-4 alkyloxy-; R 3 represents hydrogen, C 1-4 alkyl, C 1-4 alkyloxy- or R 3 combined with R 2 form together a divalent radical selected from the group consisting of -O-CH 2 - (a), -NR 7 -CH 2 - (b), -(CR 8 R 9 ) m - (c) and -CR 10 = (d) wherein m represents 1 or 2 and R 7 , R 8 , R 9 and R 10 are each independently selected from hydrogen or C 1-4 alkyl; R 4 represents hydrogen, halo, hydroxy, cyano, amino, NR 11 R 12 , C 1-4 alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R 4 represents C 1-4 alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R 5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C 1-4 alkyloxycarbonyl, hydroxycarbonyl, NR 13 R 14 or C 1-4 alkyl substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C 1-4 alkyloxy or NR 15 R 16 ; R 6 represents hydrogen; R 11 and R 12 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 13 and R 14 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 15 and R 16 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 17 and R 18 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-.
摘要翻译： N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n为1,2,3或4; Z表示O，S，NR 6，SO或SO 2; R 1表示任选被卤素取代的氢，氰基，羟基或C 1-4烷基，R 2表示氢，C 1 -C 4烷基， 1-4烷基或C 1-4烷氧基 - ; R 3表示氢，C 1-4烷基，C 1-4 - 烷氧基 - 或R 3 - ，其与 R 2一起形成选自-O-CH 2 - （a），-NR 7 -CH 2的二价基团，（c）和（c）和（c）和（c） >其中m表示1或2，R 7，R 8，R 9和R SUP > 10 各自独立地选自氢或C 1-4烷基; R 4表示氢，卤素，羟基，氰基，氨基，NR 11，R 12，C 1-4，任选被一个或任选被两个或三个选自羟基和卤素或R 4取代的取代基取代的烷氧基代表任选被一个或可能的两个或多个选自羟基和卤素的三个取代基; R 5表示氢，卤素，氰基，氨基，苯基，羟基，C 1-4烷氧基羰基，羟基羰基，NR 13 R 12，被一个或多个选自羟基羰基，苯基，C 1-4烷氧基或NR 15的取代基取代的C 1-4烷基或C 1-4烷基， SUP> - [R ^{16 ; R 6表示氢; R 11和R 12各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 13和R 14各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 15和R 16各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 17和R 18各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - 。}

4. 发明申请

WO2004056745A3 ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译：作为11-β羟基类固醇脱氢酶抑制剂的酰胺乙酰胺
公开(公告)号：WO2004056745A3
公开(公告)日：2004-11-11
申请号：PCT/EP0351021
申请日：2003-12-16
申请人： JANSSEN PHARMACEUTICA NV , LINDERS JOANNES THEODORUS MARI , WILLEMSENS GUSTAAF HENRI MARIA , GILISSEN RONALDUS ARNODUS HEND , BUYCK CHRISTOPHE FRANCIS ROBER , VANHOOF GRETA CONSTANTIA PETER , VAN DER VEKEN LOUIS JOZEF ELIS , JAROSKOVA LIBUSE
发明人： LINDERS JOANNES THEODORUS MARI , WILLEMSENS GUSTAAF HENRI MARIA , GILISSEN RONALDUS ARNODUS HEND , BUYCK CHRISTOPHE FRANCIS ROBER , VANHOOF GRETA CONSTANTIA PETER , VAN DER VEKEN LOUIS JOZEF ELIS , JAROSKOVA LIBUSE
IPC分类号： A61K31/165 , A61K31/335 , A61K31/40 , A61K31/44 , A61P3/04 , A61P3/10 , C07C233/11 , C07C233/14 , C07C233/22 , C07C233/23 , C07C233/32 , C07C233/41 , C07C233/58 , C07C235/36 , C07C235/40 , C07C237/20 , C07C237/22 , C07C255/41 , C07C255/57 , C07C271/22 , C07D207/12 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/08 , C07D215/48 , C07D217/06 , C07D217/26 , C07D243/08 , C07D257/04 , C07D277/40 , C07D277/48 , C07D295/088 , C07D295/092 , C07D295/155 , C07D295/185 , C07D309/12 , C07D311/58 , C07D311/64 , C07D317/60 , C07D317/72 , C07D333/24 , C07D333/68 , C07D335/06
CPC分类号： C07D207/27 , C07C233/11 , C07C233/14 , C07C233/22 , C07C233/23 , C07C233/32 , C07C233/41 , C07C233/58 , C07C235/36 , C07C235/40 , C07C237/20 , C07C237/22 , C07C255/41 , C07C255/57 , C07C271/22 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/06 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07C2602/18 , C07C2602/42 , C07C2602/46 , C07C2603/62 , C07C2603/66 , C07C2603/70 , C07C2603/74 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/08 , C07D215/48 , C07D217/06 , C07D217/26 , C07D243/08 , C07D257/04 , C07D277/40 , C07D277/48 , C07D295/088 , C07D295/155 , C07D295/185 , C07D309/12 , C07D311/58 , C07D311/64 , C07D317/60 , C07D317/72 , C07D333/24 , C07D333/68 , C07D335/06
摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R and R each independently represents hydrogen C1-4alkyl, NR R , C1-4alkyloxy; or R and R taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R or R may be absent to form an unsaturated bond; R represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R represents a monovalent radical having one of the following formulae, wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het or Ar wherein said C3-8cycloalkyl, Het or Ar are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR R , C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het and NR R , and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R and R each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R and R each independently represent hydrogen or C1-4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or Cl-4alkyloxycarbonyl; L represents C1-4alkyl; Het represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het represents piperidinyl, pyrrolidinyl or morpholinyl; Ar represents phenyl, naphtyl or indenyl.
摘要翻译： N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n代表1或2的整数; R 1和R 2各自独立地表示氢C 1-4烷基，NR 9 R 10，C 1-4烷氧基; 或者R 1和R 2与它们所连接的碳原子一起形成C 3-6环烷基; 并且其中n是2时，可以不存在R 1或R 2以形成不饱和键; R 3代表C 6-12环烷基，优选选自环辛基和环己基，或者R 3代表具有下式之一的一价基团，其中所述C 6-12环烷基或一价基团可以任选被一个，或者在可能的情况下两个，三个或更多个选自C 1-4烷基，C 1-4烷氧基，卤素或羟基的取代基; Q代表Het 1或Ar 2，其中所述C 3-8环烷基，Het 1或Ar 2任选被一个或在可能的情况下被两个或更多个选自卤素，C 1-4烷基，C 1-4烷氧基，羟基，硝基，NR 5 R 6，被一个或在可能的情况下被两个，三个或更多个取代基取代的C 1-4烷氧基，所述取代基各自独立地选自羟基羰基，Het 2和NR 7 R 8，以及C1 被一个或在可能的情况下被两个或三个卤素取代基取代的芳基， R 5和R 6各自独立地表示氢，C 1-4烷基或被苯基取代的C 1-4烷基; R 1和R 8各自独立地表示氢或C 1-4烷基; R9和R10各自独立地表示氢，C1-4烷基或C1-4烷氧基羰基; L代表C 1-4烷基; Het 1表示选自吡啶基，噻吩基或1,3-苯并二氧杂环戊烯基的杂环; Het 2代表哌啶基，吡咯烷基或吗啉基; Ar 2代表苯基，萘基或茚基。

5. 发明申请

WO2008049806A1 PIPERIDINE OR PIPERAZINE SUBSTITUTED TETRAHYDRO-NAPHTHALENE-1-CARBOXYLIC ACID MTP INHIBITING COMPOUNDS 审中-公开
标题翻译：哌啶或哌啶取代的四氢萘-1-羧酸的MTP抑制化合物
公开(公告)号：WO2008049806A1
公开(公告)日：2008-05-02
申请号：PCT/EP2007/061286
申请日：2007-10-22
申请人： JANSSEN PHARMACEUTICA NV , MEERPOEL, Lieven , LINDERS, Joannes Theodorus Maria , JAROSKOVA, Libuse , VIELLEVOYE, Marcel , BACKX, Leo Jacobus Jozef , BERTHELOT, Didier Jean-Claude , BUSSCHER, Guuske Frederike
发明人： MEERPOEL, Lieven , LINDERS, Joannes Theodorus Maria , JAROSKOVA, Libuse , VIELLEVOYE, Marcel , BACKX, Leo Jacobus Jozef , BERTHELOT, Didier Jean-Claude , BUSSCHER, Guuske Frederike
IPC分类号： C07D211/58 , C07D241/20 , C07D295/10 , C07D401/12 , C07D401/14 , A61K31/495 , A61K31/445 , A61P3/00
CPC分类号： C07D241/20 , C07D211/58 , C07D295/10 , C07D401/12 , C07D401/14
摘要： The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
摘要翻译：本发明涉及具有apoB分泌/ MTP抑制活性和伴随的降脂活性的新型哌啶或哌嗪取代的四氢 - 萘-1-羧酸衍生物。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途。

6. 发明申请

WO2006024627A3 N-2 ADAMANTANYL-2-PHENOXY-ACETAMIDE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
公开(公告)号：WO2006024627A3
公开(公告)日：2006-03-09
申请号：PCT/EP2005/054197
申请日：2005-08-26
申请人： JANSSEN PHARMACEUTICA N.V. , JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , VAN DER VEKEN, Louis, Jozef, Elisabeth , WILLEMSENS, Gustaaf, Henri, Maria , BISCHOFF, François Paul
发明人： JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , VAN DER VEKEN, Louis, Jozef, Elisabeth , WILLEMSENS, Gustaaf, Henri, Maria , BISCHOFF, François Paul
IPC分类号： A61K31/165 , C07C235/22 , C07D307/85 , C07D311/66 , C07D319/20 , A61P3/04 , A61P3/10 , A61P9/00 , A61P19/10 , A61P25/28 , A61P27/06
摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1, 2, 3, or 4; Z represents O, S, NR 6 , SO or SO 2 ; R 1 represent hydrogen, cyano, hydroxy, or C 1-4 alkyl optionally substituted with halo, R 2 represents hydrogen, C 1-4 alkyl, or C 1-4 alkyloxy-; R 3 represents hydrogen, C 1-4 alkyl, C 1-4 alkyloxy- or R 3 combined with R 2 form together a divalent radical selected from the group consisting of -O-CH 2 - (a), -NR 7 -CH 2 - (b), -(CR 8 R 9 ) m - (c) and -CR 10 = (d) wherein m represents 1 or 2 and R 7 , R 8 , R 9 and R 10 are each independently selected from hydrogen or C 1-4 alkyl; R 4 represents hydrogen, halo, hydroxy, cyano, amino, NR 11 R 12 , C 1-4 alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R 4 represents C 1-4 alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R 5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C 1-4 alkyloxycarbonyl, hydroxycarbonyl, NR 13 R 14 or C 1-4 alkyl substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C 1-4 alkyloxy or NR 15 R 16 ; R 6 represents hydrogen; R 11 and R 12 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 13 and R 14 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 15 and R 16 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 17 and R 18 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-.

7. 发明申请

WO2004056745A2 ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： ADAMANTYL ACETAMIDES as 11-BETA HYDROXYSTERIDID DEHYDROGENASE INHIBITORS
公开(公告)号：WO2004056745A2
公开(公告)日：2004-07-08
申请号：PCT/EP2003/051021
申请日：2003-12-16
申请人： JANSSEN PHARMACEUTICA N.V. , LINDERS, Joannes, Theodorus, Maria , WILLEMSENS, Gustaaf, Henri, Maria , GILISSEN, Ronaldus, Arnodus, Hendrika, Joseph , BUYCK, Christophe, Francis, Robert, Nestor , VANHOOF, Greta, Constantia, Peter , VAN DER VEKEN, Louis, Jozef, Elisabeth , JAROSKOVA, Libuse
发明人： LINDERS, Joannes, Theodorus, Maria , WILLEMSENS, Gustaaf, Henri, Maria , GILISSEN, Ronaldus, Arnodus, Hendrika, Joseph , BUYCK, Christophe, Francis, Robert, Nestor , VANHOOF, Greta, Constantia, Peter , VAN DER VEKEN, Louis, Jozef, Elisabeth , JAROSKOVA, Libuse
IPC分类号： C07C233/11
CPC分类号： C07D207/27 , C07C233/11 , C07C233/14 , C07C233/22 , C07C233/23 , C07C233/32 , C07C233/41 , C07C233/58 , C07C235/36 , C07C235/40 , C07C237/20 , C07C237/22 , C07C255/41 , C07C255/57 , C07C271/22 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/06 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07C2602/18 , C07C2602/42 , C07C2602/46 , C07C2603/62 , C07C2603/66 , C07C2603/70 , C07C2603/74 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/08 , C07D215/48 , C07D217/06 , C07D217/26 , C07D243/08 , C07D257/04 , C07D277/40 , C07D277/48 , C07D295/088 , C07D295/155 , C07D295/185 , C07D309/12 , C07D311/58 , C07D311/64 , C07D317/60 , C07D317/72 , C07D333/24 , C07D333/68 , C07D335/06
摘要： The N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R 1 and R 2 each independently represents hydrogen C 1-4 alkyl, NR 9 R 10 , C 1-4 alkyloxy; or R 1 and R 2 taken together with the carbon atom with which they are attached form a C 3-6 cycloalkyl; and where n is 2, either R 1 or R 2 may be absent to form an unsaturated bond; R 3 represents a C 6-12 cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R 3 represents a monovalent radical having one of the following formulae, wherein said C 6-12 cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C 1-4 alkyl, C 1-4 alkyloxy, halo or hydroxy; Q represents Het 1 or Ar 2 wherein said C 3-8 cycloalkyl, Het 1 or Ar 2 are optionally substituted with one or where possible two or more substituents selected from halo, C 1-4 alkyl, C 1-4 alkyloxy, hydroxy, nitro, NR 5 R 6 , C 1-4 alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het 2 and NR 7 R 8 , and C 1-4 alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R 5 and R 6 each independently represent hydrogen, C 1-4 alkyl, or C 1-4 alkyl substituted with phenyl; R 1 and R 8 each independently represent hydrogen or C 1-4 alkyl; R 9 and R 10 each independently represent hydrogen, C 1-4 alkyl or C l-4 alkyloxycarbonyl; L represents C 1-4 alkyl; Het 1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het 2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar 2 represents phenyl, naphtyl or indenyl.
摘要翻译： N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n表示1或2的整数; R 1和R 2各自独立地表示氢，C 1-4烷基，NR 9 R 10，C 1-4烷氧基，或R 1和R 2与它们所连接的碳原子一起形成C 3-6环烷基; 并且其中n为2时，R 1或R 2可以不存在以形成不饱和键; R 3表示C6-12环烷基，优选选自环辛基和环己基，或R 3表示具有下式之一的一价基团，其中所述C 6-12环烷基或一价基团可任选地被一个或在可能的情况下可能有两个，三个或更多个选自C 1-4烷基，C 1-4烷氧基，卤素或羟基的取代基; Q表示Het 1或Ar 2，其中所述C 3-8环烷基，Het 1或Ar 2任选被一个或可能的两个或多个选自卤素，C 1-4烷基，C 1-4烷氧基，羟基，硝基，NR 5 R 6，被一个或可能的两个，三个或更多个各自独立地选自羟基羰基，Het 2和NR 7 R 8的取代基取代的C 1-4烷氧基，和C 1 被一个或两个或三个卤素取代基取代的4-烷基，优选三氟甲基; R 5和R 6各自独立地表示氢，C 1-4烷基或被苯基取代的C 1-4烷基; R 1和R 8各自独立地表示氢或C 1-4烷基; R 9和R 10各自独立地表示氢，C 1-4烷基或C 1-4烷氧基羰基; L表示C 1-4烷基; Het 1表示选自吡啶基，噻吩基或1,3-苯并二恶唑基的杂环; Het 2表示哌啶基，吡咯烷基或吗啉基; Ar 2表示苯基，萘基或茚基。

8. 发明申请

WO2006024627A9 N-2 ADAMANTANYL-2-PHENOXY-ACETAMIDE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： N-2 ADAMANTANYL-2-苯甲酰胺衍生物作为11-氢化羟基脱氢酶抑制剂
公开(公告)号：WO2006024627A9
公开(公告)日：2008-02-14
申请号：PCT/EP2005054197
申请日：2005-08-26
申请人： JANSSEN PHARMACEUTICA NV , JAROSKOVA LIBUSE , LINDERS JOANNES THEODORUS MARI , VAN DER VEKEN LOUIS JOZEF ELIS , WILLEMSENS GUSTAAF HENRI MARIA , BISCHOFF FRANCOIS PAUL
发明人： JAROSKOVA LIBUSE , LINDERS JOANNES THEODORUS MARI , VAN DER VEKEN LOUIS JOZEF ELIS , WILLEMSENS GUSTAAF HENRI MARIA , BISCHOFF FRANCOIS PAUL
IPC分类号： A61K31/165 , A61P3/04 , A61P3/10 , A61P9/00 , A61P19/10 , A61P25/28 , A61P27/06 , C07C235/22 , C07D307/85 , C07D311/66 , C07D319/20
CPC分类号： A61K31/165 , C07C235/22 , C07C237/04 , C07C271/38 , C07C307/08 , C07C311/07 , C07C311/09 , C07C311/20 , C07C2603/74 , C07D207/27 , C07D263/20 , C07D265/36 , C07D295/32 , C07D307/85 , C07D311/66 , C07D319/20
摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1, 2, 3, or 4; Z represents O, S, NR 6 , SO or SO 2 ; R 1 represent hydrogen, cyano, hydroxy, or C 1-4 alkyl optionally substituted with halo, R 2 represents hydrogen, C 1-4 alkyl, or C 1-4 alkyloxy-; R 3 represents hydrogen, C 1-4 alkyl, C 1-4 alkyloxy- or R 3 combined with R 2 form together a divalent radical selected from the group consisting of -O-CH 2 - (a), -NR 7 -CH 2 - (b), -(CR 8 R 9 ) m - (c) and -CR 10 = (d) wherein m represents 1 or 2 and R 7 , R 8 , R 9 and R 10 are each independently selected from hydrogen or C 1-4 alkyl; R 4 represents hydrogen, halo, hydroxy, cyano, amino, NR 11 R 12 , C 1-4 alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R 4 represents C 1-4 alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R 5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C 1-4 alkyloxycarbonyl, hydroxycarbonyl, NR 13 R 14 or C 1-4 alkyl substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C 1-4 alkyloxy or NR 15 R 16 ; R 6 represents hydrogen; R 11 and R 12 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 13 and R 14 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 15 and R 16 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-; R 17 and R 18 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkylcarbonyl-.
摘要翻译： N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n为1,2,3或4; Z表示O，S，NR 6，SO或SO 2; R 1表示任选被卤素取代的氢，氰基，羟基或C 1-4烷基，R 2表示氢，C 1 -C 4烷基， 1-4烷基或C 1-4烷氧基 - ; R 3表示氢，C 1-4烷基，C 1-4 - 烷氧基 - 或R 3 - ，其与 R 2一起形成选自-O-CH 2 - （a），-NR 7 -CH 2的二价基团，（c）和（c）和（c）和（c） >其中m表示1或2，R 7，R 8，R 9和R SUP > 10 各自独立地选自氢或C 1-4烷基; R 4表示氢，卤素，羟基，氰基，氨基，NR 11，R 12，C 1-4，任选被一个或任选被两个或三个选自羟基和卤素或R 4取代的取代基取代的烷氧基代表任选被一个或可能的两个或多个选自羟基和卤素的三个取代基; R 5表示氢，卤素，氰基，氨基，苯基，羟基，C 1-4烷氧基羰基，羟基羰基，NR 13 R 12，被一个或多个选自羟基羰基，苯基，C 1-4烷氧基或NR 15的取代基取代的C 1-4烷基或C 1-4烷基， SUP> - [R ^{16 ; R 6表示氢; R 11和R 12各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 13和R 14各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 15和R 16各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 17和R 18各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - 。}

9. 发明申请

WO2005108361A1 ADAMANTYL PYRROLIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： ADAMANTYL PYRRIDIDI-2-ONE DERIVATIVES as 11-BETA HYDROXYSTERIDID DEHYDROGENASE INHIBITORS
公开(公告)号：WO2005108361A1
公开(公告)日：2005-11-17
申请号：PCT/EP2005/051970
申请日：2005-04-29
申请人： JANSSEN PHARMACEUTICA N.V. , JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , BUYCK, Christophe, Francis, Robert, Nestor , VAN DER VEKEN, Louis, Jozef, Elisabeth
发明人： JAROSKOVA, Libuse , LINDERS, Joannes, Theodorus, Maria , BUYCK, Christophe, Francis, Robert, Nestor , VAN DER VEKEN, Louis, Jozef, Elisabeth
IPC分类号： C07D207/26
CPC分类号： C07D207/26 , C07D207/267 , C07D211/76 , C07D453/06
摘要： The N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; M represents a direct bond or a C 1-3 alkyl linker optionally substituted with one or two substituents selected from C 1-4 alkyl, C 1-3 alkyloxy-C 1-4 alkyl-, hydroxy-C 1-4 alkyl-, hydroxy, C 1-3 alkyloxy- or phenyl-C 1-4 alkyl-; R 1 and R 2 each independently represent hydrogen, halo, cyano, hydroxy, C l-4 alkyl optionally substituted with halo, C 1-4 alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar 1 and halo ; R 3 represents hydrogen, halo, C 1-4 alkyl, C 1-4 alkyloxy-, cyano or hydroxy; R 4 represents hydrogen, halo, C l-4 alkyl, hydroxy, cyano or C 1-4 alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R 5 represents hydrogen, C 1-4 alkyl or Ar 2 -C 1-4 alkyl-; R 6 represents hydrogen, hydroxy, halo, C 1-4 alkyl or C 1-4 alkyoxy-; R 7 represents hydrogen or R 7 and R 5 taken together with the carbon atom to which they are attached from a -C 2 -alkyl- linker; Ar 1 and Ar 2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C 1-4 alkyl, C 1-4 alkyloxy-, or phenyl-C 1-4 alkyl.
摘要翻译： N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n为1或2; M表示直接键或任选被一个或两个选自C 1-4烷基，C 1-3烷氧基-C 1-4 - 烷基 - ，羟基-C 1-4 - 烷基 - ，羟基，C 1-3烷氧基 - 或苯基-C 1 -4alkyl-; R 1和R 2各自独立地表示氢，卤素，氰基，羟基，任选被卤素取代的C 1-4烷基，C 1-4烷氧基 - 任选被一个或任选被两个或三个选自羟基，Ar 1 >和光环; R 3表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R 4表示氢，卤素，C 1-4烷基，羟基，氰基或C 1-4烷氧基 - 任选地被一个或可能的两个或三个选自羟基和卤素的取代基取代; R 5表示氢，C 1-4烷基或Ar 2 -C 1-4烷基 - ; R 6表示氢，羟基，卤代，C 1-4烷基或C 1-4烷氧基 - ; R 7表示氢或R 7和R 5与它们所连接的碳原子一起从-C2-烷基 - 连接基取代; Ar 1和Ar 2各自独立地表示苯基或萘基，其中所述苯基和萘基任选被C 1-4烷基，C 1-4烷氧基 - 或苯基-C 1-4烷基取代。

10. 发明申请

WO2005085226A1 MTP INHIBITING ARYL PIPERIDINES OR PIPERAZINES SUBSTITUTED WITH 5-MEMBERED HETEROCYCLES 审中-公开
标题翻译： MTP抑制由5个成员的杂环取代的芳基哌嗪或哌嗪
公开(公告)号：WO2005085226A1
公开(公告)日：2005-09-15
申请号：PCT/EP2005/051010
申请日：2005-03-07
申请人： JANSSEN PHARMACEUTICA N.V. , MEERPOEL, Lieven , BACKX, Leo, Jacobus, Jozef , JAROSKOVA, Libuse , ROEVENS, Peter, Walter, Maria , VAN DER VEKEN, Louis, Jozef, Elisabeth , VIELLEVOYE, Marcel , LINDERS, Joannes, Theodorus, Maria
发明人： MEERPOEL, Lieven , BACKX, Leo, Jacobus, Jozef , JAROSKOVA, Libuse , ROEVENS, Peter, Walter, Maria , VAN DER VEKEN, Louis, Jozef, Elisabeth , VIELLEVOYE, Marcel , LINDERS, Joannes, Theodorus, Maria
IPC分类号： C07D401/04
CPC分类号： C07D233/54 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes (Formula (I)). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
摘要翻译：本发明涉及用具有apoB分泌/ MTP抑制活性和伴随的降脂活性的某些5-元杂环取代的新的芳基哌啶或哌嗪化合物。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗高脂血症，肥胖症和II型糖尿病的药物（式（I））的用途。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式