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1. 发明授权

US09012494B2 Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
标题翻译：吡咯烷-2-酮和哌啶-2-酮衍生物作为11-β羟基类固醇脱氢酶抑制剂
公开(公告)号：US09012494B2
公开(公告)日：2015-04-21
申请号：US11632675
申请日：2005-04-29
申请人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Christophe Francis Robert Nestor Buyck , Louis Jozef Elisabeth Van Der Veken , Vladimir Dimtchev Dimitrov , Theo Teofanov Nikiforov
发明人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Christophe Francis Robert Nestor Buyck , Louis Jozef Elisabeth Van Der Veken , Vladimir Dimtchev Dimitrov , Theo Teofanov Nikiforov
IPC分类号： A61K31/4015 , C07D207/12 , C07D207/267 , C07D207/26 , C07D211/76 , C07D405/06
CPC分类号： C07D211/76 , C07D207/26 , C07D207/267 , C07D405/06
摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 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; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.
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; 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 - 任选被一个或可能的两个或三个选自羟基，Ar 1和卤素的取代基取代; 或者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; R4代表氢，卤素，C1-4烷基，C1-4烷氧基，氰基或羟基; R5表示氢，C1-4烷基或Ar2-C1-4烷基; R 6表示氢，卤素，C 1-4烷基或C 1-4烷氧基 - ; Ar1和Ar2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. 发明授权

US07332524B2 Adamantyl acetamides as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
公开(公告)号：US07332524B2
公开(公告)日：2008-02-19
申请号：US10540616
申请日：2003-12-16
申请人： Joannes Theodorus Maria Linders , Gustaaf Henri Maria Willemsens , Ronaldus Arnodus Hendrika Joseph Gilissen , Christophe Francis Robert Nestor Buyck , Greta Constantia Peter Vanhoof , Louis Jozef Elisabeth Van Der Veken , Libuse Jaroskova
发明人： Joannes Theodorus Maria Linders , Gustaaf Henri Maria Willemsens , Ronaldus Arnodus Hendrika Joseph Gilissen , Christophe Francis Robert Nestor Buyck , Greta Constantia Peter Vanhoof , Louis Jozef Elisabeth Van Der Veken , Libuse Jaroskova
IPC分类号： A61K31/165 , C07C233/57
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; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 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 Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R6, C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het2 and NR7R8, and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R5 and R6 each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R7 and R8 each independently represent hydrogen or C1-4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or C1-4alkyloxycarbonyl; L represents C1-4alkyl; Het1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar2 represents phenyl, naphtyl or indenyl.

3. 发明申请

US20080139625A1 Pyrrolidin-2-One and Piperidin-2-One Derivatives as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors 有权
公开(公告)号：US20080139625A1
公开(公告)日：2008-06-12
申请号：US11632675
申请日：2005-04-29
申请人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Christophe Francis Robert Nestor Buyck , Louis Jozef Elizabeth Van Der Veken , Vladimir Dimichev Dimitrov , Theo Teofanov Nikiforov
发明人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Christophe Francis Robert Nestor Buyck , Louis Jozef Elizabeth Van Der Veken , Vladimir Dimichev Dimitrov , Theo Teofanov Nikiforov
IPC分类号： A61K31/4015 , C07D207/12 , C07D405/10 , A61P3/00 , A61K31/4412 , C07D211/40
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 C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 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; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.

4. 发明授权

US07687644B2 Adamantyl pyrrolidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
标题翻译：金刚烷基吡咯烷-2-酮衍生物作为11-β羟基类固醇脱氢酶抑制剂
公开(公告)号：US07687644B2
公开(公告)日：2010-03-30
申请号：US11632195
申请日：2005-04-29
申请人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Christophe Francis Robert Buyck , Louis Jozef Elisabeth Van der Veken
发明人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Christophe Francis Robert Buyck , Louis Jozef Elisabeth Van der Veken
IPC分类号： C07D207/00 , A61K31/40
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 C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl-, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl-; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy-optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, hydroxy, cyano or C1-4alkyloxy-optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, C1-4alkyl or Ar2—C1-4alkyl-; R6 represents hydrogen, hydroxy, halo, C1-4alkyl or C1-4alkyoxy-; R7 represents hydrogen or R7 and R5 taken together with the carbon atom to which they are attached from a —C2-alkyl-linker; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl.
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 -4-烷基 - ; 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 - 任选被一个或可能的两个或三个选自羟基，Ar 1和卤素的取代基取代; 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，羟基，氰基或C 1-4烷氧基 - 任选地被一个或其中可能的两个或三个选自羟基和卤素的取代基取代; R5表示氢，C1-4烷基或Ar2-C1-4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代表氢或R 7和R 5与它们所连接的碳原子一起从-C2-烷基 - 连接基中取代; 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。

5. 发明授权

US08563591B2 Tricyclic lactam derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
标题翻译：三环内酰胺衍生物作为11-β羟基类固醇脱氢酶抑制剂
公开(公告)号：US08563591B2
公开(公告)日：2013-10-22
申请号：US11661468
申请日：2005-08-26
申请人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Louis Jozef Elisabeth Van Der Veken , Gustaaf Henri Maria Willemsens
发明人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Louis Jozef Elisabeth Van Der Veken , Gustaaf Henri Maria Willemsens
IPC分类号： C07D209/62 , A61K31/403 , A61K31/404
CPC分类号： C07D471/04 , A61K31/4745 , A61K45/06 , C07D209/58 , C07D209/60 , C07D209/64 , C07D495/04
摘要： the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents C or N; Y represents C or N; L represents a methyl or a direct bond; Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b); Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b); R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR3R4 or C1-4alkyl optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8; R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-; R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R7 and R8 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; A represents phenyl or a monocyclic heterocycle selected from the group consisting of thiophenyl, furanyl, oxazolyl, thiazolyl, imidazolyl, isoxazolyl, isothiazolyl, pyrridinyl, pyridazinyl, pyrimidinyl and piperazinyl.
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X表示C或N; Y表示C或N; L表示甲基或直接键; Z 1表示直接键，C 1-2烷基 - 或式-CH 2 -CH =（a）或-CH =（b））的二价基团。 Z2表示直接键，C1-2烷基 - 或式-CH2-CH =（a）或-CH =（b）的二价基团; R 1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 3 R 4或任选被一个或多个选自羟基羰基，苯基，C 1-4烷氧基或NR 5 R 6的取代基取代的C 1-4烷基或R 1表示C 1-4烷氧基 - 任选地被一个或多个选自羟基羰基，苯基，C 1-4烷氧基或NR 7 R 8的取代基取代; R 2表示氢，卤素，C 1-4烷基或C 1-4烷氧基 - ; R3和R4各自独立地表示氢，C1-4烷基或C1-4烷基羰基; R5和R6各自独立地表示氢，C1-4烷基或C1-4烷基羰基 - ; R 7和R 8各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; A表示苯基或选自噻吩基，呋喃基，恶唑基，噻唑基，咪唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和哌嗪基的单环杂环。

6. 发明申请

US20100004263A1 MTP INHIBITING ARYL PIPERIDINES OR PEPERAZINES SUBSTITUTED WITH5-MEMBERED HETEROCYCLES 有权
标题翻译： MTP抑制由5个成员的杂环取代的芳基哌嗪或哌啶
公开(公告)号：US20100004263A1
公开(公告)日：2010-01-07
申请号：US12341567
申请日：2008-12-22
申请人： Lieven Meerpoel , Leo Jacobus Jozef Backx , Libuse Jaroskova , Peter Walter Maria Roevens , Louis Jozef Elisabeth Van Der Veken , Marcel Viellevoye , Joannes Theodorus Maria Linders
发明人： Lieven Meerpoel , Leo Jacobus Jozef Backx , Libuse Jaroskova , Peter Walter Maria Roevens , Louis Jozef Elisabeth Van Der Veken , Marcel Viellevoye , Joannes Theodorus Maria Linders
IPC分类号： A61K31/497 , C07D409/02 , C07D409/14 , C07D411/14 , C07D413/04 , A61K31/454 , A61K31/445 , A61P3/10
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. 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。

7. 发明授权

US08344181B2 N-2 adamantanyl-2-phenoxy-acetamide derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
标题翻译： N-2金刚烷基-2-苯氧基乙酰胺衍生物作为11-β羟基类固醇脱氢酶抑制剂
公开(公告)号：US08344181B2
公开(公告)日：2013-01-01
申请号：US11661470
申请日：2005-08-26
申请人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Louis Jozef Elisabeth Van Der Veken , Gustaaf Henri Maria Willemsens , François Paul Bischoff
发明人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Louis Jozef Elisabeth Van Der Veken , Gustaaf Henri Maria Willemsens , François Paul Bischoff
IPC分类号： C07C233/05 , A61K31/16
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 Z represents O, S, NR6, SO or SO2; R1 represents hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of —O—CH2— (a), —NR7—CH2— (b), —(CR8R9)m- (c) and —CR10═ (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR13R14 or C1-4alkyl substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR15R16; R6 represents hydrogen; R11 and R12 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R13 and R14 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R15 and R16 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R17 and R18 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-.
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Z表示O，S，NR6，SO或SO2; R 1表示氢，氰基，羟基或任选被卤素取代的C 1-4烷基，R 2表示氢，C 1-4烷基或C 1-4烷氧基 - ; R 3表示氢，C 1-4烷基，C 1-4烷氧基或与R 2结合的R 3一起形成选自-O-CH 2 - （a），-NR 7 -CH 2 - （b）， - （CR 8 R 9） m-（c）和-CR 10 =（d）其中m表示1或2，并且R 7，R 8，R 9和R 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，或者R 4表示任选地被一个或两个或三个选自羟基和卤素的取代基; 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 14或被一个或多个选自羟基羰基，苯基，C 1-4烷氧基或NR 15 R 16的取代基取代的C 1-4烷基; R6代表氢; 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。

8. 发明授权

US07968601B2 Adamantyl acetamides as 11-β hydroxysteroid dehydrogenase inhibitors 有权
标题翻译：金刚烷基乙酰胺为11-＆bgr; 羟类固醇脱氢酶抑制剂
公开(公告)号：US07968601B2
公开(公告)日：2011-06-28
申请号：US11958593
申请日：2007-12-18
申请人： Joannes Theodorus Maria Linders , Gustaaf Henri Maria Willemsens , Ronaldus Arnodus Hendrika Joseph Gilissen , Christophe Francis Robert Nester Buyck , Greta Constantia Peter Vanhoof , Louis Jozef Elisabeth Van Der Veken , Libuse Jaroskova
发明人： Joannes Theodorus Maria Linders , Gustaaf Henri Maria Willemsens , Ronaldus Arnodus Hendrika Joseph Gilissen , Christophe Francis Robert Nester Buyck , Greta Constantia Peter Vanhoof , Louis Jozef Elisabeth Van Der Veken , Libuse Jaroskova
IPC分类号： A61K31/551 , A61K31/165 , A61K31/357 , A61K31/47 , A61K31/495 , A61K31/535 , C07D217/04 , C07D243/08 , C07D317/28 , C07D265/30 , C07D241/04 , C07C233/03
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; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 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 Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R6, C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het2 and NR7R8, and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R5 and R6 each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R7 and R8 each independently represent hydrogen or C1-4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or C1-4alkyloxycarbonyl; L represents C1-4alkyl; Het1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar2 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为2时，R 1或R 2可以不存在以形成不饱和键; R3表示C6-12环烷基，优选选自环辛基和环己基，或R3表示具有下列结构式之一的一价基团，其中所述C 6-12环烷基或一价基团可以任选地被一个取代，或在可能的情况下被两个，三个或更多个取代选自C 1-4烷基，C 1-4烷氧基，卤素或羟基的取代基; Q表示Het1或Ar2，其中所述C 3-8环烷基，Het1或Ar2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，三个或更多个取代基，各自独立地选自羟基羰基，Het2和NR7R8，以及被一个或其中可能的两个或三个卤素取代基，优选三氟甲基取代的C 1-4烷基; R5和R6各自独立地表示氢，C1-4烷基或被苯基取代的C1-4烷基; R 7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表示C 1-4烷基; Het1表示选自吡啶基，噻吩基或1,3-苯并二恶唑基的杂环; Het2表示哌啶基，吡咯烷基或吗啉基; Ar 2表示苯基，萘基或茚基。

9. 发明授权

US07816360B2 MTP inhibiting aryl piperidines or piperazines substituted with 5-membered heterocycles 有权
标题翻译： MTP抑制芳基哌啶或被5元杂环取代的哌嗪
公开(公告)号：US07816360B2
公开(公告)日：2010-10-19
申请号：US12341567
申请日：2008-12-22
申请人： Lieven Meerpoel , Leo Jacobus Jozef Backx , Libuse Jaroskova , Peter Walter Maria Roevens , Louis Jozef Elisabeth Van Der Veken , Marcel Viellevoye , Joannes Theodorus Maria Linders
发明人： Lieven Meerpoel , Leo Jacobus Jozef Backx , Libuse Jaroskova , Peter Walter Maria Roevens , Louis Jozef Elisabeth Van Der Veken , Marcel Viellevoye , Joannes Theodorus Maria Linders
IPC分类号： A61K31/496 , A61K31/454 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12 , C07D487/04 , C07D233/74 , C07D249/12
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. 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。

10. 发明授权

US07504400B2 MTP inhibiting aryl piperydines or piperazines substituted with 5-membered heterocycles 有权
标题翻译：用5元杂环取代的MTP抑制芳基哌啶或哌嗪
公开(公告)号：US07504400B2
公开(公告)日：2009-03-17
申请号：US10589515
申请日：2005-03-07
申请人： Lieven Meerpoel , Leo Jacobus Jozef Backx , Libuse Jaroskova , Peter Walter Maria Roevens , Louis Jozef Elisabeth Van Der Veken , Marcel Viellevoye , Joannes Theodorus Maria Linders
发明人： Lieven Meerpoel , Leo Jacobus Jozef Backx , Libuse Jaroskova , Peter Walter Maria Roevens , Louis Jozef Elisabeth Van Der Veken , Marcel Viellevoye , Joannes Theodorus Maria Linders
IPC分类号： A61K31/496 , A61K31/454 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D417/121
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. 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, hyper-triglyceridemia, 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。

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