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1. 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。

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。

4. 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。

5. 发明申请

US20080214597A1 Tricyclic Lactam Derivatives as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors 有权
公开(公告)号：US20080214597A1
公开(公告)日：2008-09-04
申请号：US11661468
申请日：2005-08-26
申请人： Libuse Jaraskova , Joannes Theodorus Maria Linders , Louis Jozef Elisabeth Van Der Veken , Gustaaf Henri Maria Willemsens
发明人： Libuse Jaraskova , Joannes Theodorus Maria Linders , Louis Jozef Elisabeth Van Der Veken , Gustaaf Henri Maria Willemsens
IPC分类号： A61K31/4745 , C07D209/56 , A61K31/403 , A61P29/00 , A61P9/00 , A61P35/04 , A61P3/00 , C07D487/04
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.

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