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1. 发明申请

US20080096869A1 ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 有权
公开(公告)号：US20080096869A1
公开(公告)日：2008-04-24
申请号：US11958593
申请日：2007-12-18
申请人： Joannes Linders , Gustaaf Willemsens , Ronaldus Arnodus Gilissen , Christophe Francis Buyck , Greta Vanhoof , Louis Van Der Veken , Libuse Jaroskova
发明人： Joannes Linders , Gustaaf Willemsens , Ronaldus Arnodus Gilissen , Christophe Francis Buyck , Greta Vanhoof , Louis Van Der Veken , Libuse Jaroskova
IPC分类号： A61K31/551 , A61K31/165 , A61K31/357 , A61K31/47 , C07D217/04 , C07D243/08 , C07D317/28 , C07D265/30 , C07D241/04 , C07C233/03 , A61K31/495 , A61K31/535
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.

2. 发明申请

US20070197610A1 Benzisoxazoles 审中-公开
公开(公告)号：US20070197610A1
公开(公告)日：2007-08-23
申请号：US10598957
申请日：2005-03-11
申请人： Ludo Kennis , Greta Vanhoof , Jean-Pierre Bongartz , Marcel Luyckx , Wenda Minke
发明人： Ludo Kennis , Greta Vanhoof , Jean-Pierre Bongartz , Marcel Luyckx , Wenda Minke
IPC分类号： A61K31/426 , A61K31/428 , A61K31/425 , A61K31/42 , C07D413/02 , C07D417/02
CPC分类号： A61K31/423 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/428 , C07D261/20
摘要： The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer from 1 to 3; X represents amino, hydroxy, -oxo or -Z-R1; Y is absent when X represents -Z-R1 and —(C═O)—R6 when X represents oxo; Z represents carbonyl, -oxy-carbonyl- or —NR5-carbonyl-; R1 represents C1-4alkyl, Ar1, Ar1—C1-4alkyl-, —NR3R4 or -Het1; R2 represents hydrogen, halo, nitro, hydroxycarbonyl-, C1-4alkyloxy or C1-4alkyl; R3 and R4 are each independently selected from hydrogen, Ar3 or C1-4alkyl; R5 represents hydrogen, C1-4alkylcarbonyl- or Ar4-carbonyl-; R6 represents a substituent selected from the group consisting of C1-4alkyl, Ar5, Ar6—C1-4alkyl- or NR7R8; R7 and R8 are each independently selected from hydrogen, Het4 or C1-4alkyl; Het1 represents a heterocycle selected from oxazolyl, isoxazolyl, imidazolyl or pyrazolyl wherein said heterocycle is optionally substituted with one, two or three substitutents selected from the group consisting of amino, C1-4alkyl, hydroxy-C1-4alkyl, phenyl, phenyl-C1-4alkyl- and phenyl substituted with one or more halo substitutents; Het4 represents a heterocycle selected from oxazolyl or isoxazolyl, wherein said heterocycle is optionally substituted with one or more substitutents selected from the group consisting of amino, C1-4alkyl, hydroxy-C1-4alkyl-, phenyl, phenyl-C1-4alkyl and phenyl substituted with one or more halo substitutents; and Ar1, Ar2, Ar3, Ar4, Ar5 or Ar6 each independently represents phenyl optionally substituted one or where possible two or more substitutents selected from halo, nitro, C1-4alkyl, hydroxy or C1-4alkyloxy-.

3. 发明申请

US20060079506A1 Adamantyl acetamides as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
公开(公告)号：US20060079506A1
公开(公告)日：2006-04-13
申请号：US10540616
申请日：2003-12-16
申请人： Joannes Linders , Gustaaf Willemsens , Ronaldus Gilissen , Christophe Francis Buyck , Greta Vanhoof , Louis Van Der Veken , Libuse Jaroskova
发明人： Joannes Linders , Gustaaf Willemsens , Ronaldus Gilissen , Christophe Francis Buyck , Greta Vanhoof , Louis Van Der Veken , Libuse Jaroskova
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/502 , A61K31/501 , A61K31/497 , A61K31/4965 , A61K31/4172 , A61K31/4745
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.

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