ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS

WIPO Patent Application WO2004056745

A3

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 C1-4alkyl, NR<9>R<10>, C1-4alkyloxy; or R<1> and R<2> taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R<1> or R<2> may be absent to form an unsaturated bond; R<3> represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R<3> 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<1> or Ar<2> wherein said C3-8cycloalkyl, Het<1> or Ar<2> are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR<5>R<6>, C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het<2> and NR<7>R<8>, and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R<5> and R<6> each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R<1> and R<8> each independently represent hydrogen or C1-4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or Cl-4alkyloxycarbonyl; L represents C1-4alkyl; 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.

LINDERS JOANNES THEODORUS MARI (NL)
WILLEMSENS GUSTAAF HENRI MARIA (BE)
GILISSEN RONALDUS ARNODUS HEND (BE)
BUYCK CHRISTOPHE FRANCIS ROBER (BE)
VANHOOF GRETA CONSTANTIA PETER (BE)
VAN DER VEKEN LOUIS JOZEF ELIS (BE)
JAROSKOVA LIBUSE (BE)

PCT/EP2003/051021

November 11, 2004

December 16, 2003

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JANSSEN PHARMACEUTICA NV (BE)
LINDERS JOANNES THEODORUS MARI (NL)
WILLEMSENS GUSTAAF HENRI MARIA (BE)
GILISSEN RONALDUS ARNODUS HEND (BE)
BUYCK CHRISTOPHE FRANCIS ROBER (BE)
VANHOOF GRETA CONSTANTIA PETER (BE)
VAN DER VEKEN LOUIS JOZEF ELIS (BE)
JAROSKOVA LIBUSE (BE)

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; C07D207/27; 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; C07D207/26; (IPC1-7): C07C233/11; C07C235/36; C07C233/14; C07C233/23; C07C233/58; C07C271/22; C07C237/20; C07C233/41; C07C233/22; C07C237/22; C07C233/32; C07D317/72; C07D295/088; C07D207/12; C07D213/56; A61K31/165; A61K31/335; A61K31/40; A61K31/44; A61P3/04; A61P3/10

WO1999026927A2	1999-06-03
WO1998011073A1	1998-03-19
WO2001090090A1	2001-11-29

US3919313A	1975-11-11
DE1959898A1	1970-06-18
FR1399615A	1965-05-21
DE2624290A1	1977-04-14
US3622567A	1971-11-23
US3526656A	1970-09-01
US2510945A	1950-06-13

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DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248035, Database accession no. Reaction ID 1481005
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248036, Database accession no. Reaction ID 127579
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248037, Database accession no. BRN 8562669
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248038, Database accession no. Reaction ID 378559
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DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248042, Database accession no. BRN 397713
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248043, Database accession no. BRN 2697500
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248044, Database accession no. BRN 2443257
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248045, Database accession no. Reaction ID 4215309
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248046, Database accession no. Reaction ID 1136477
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248047, Database accession no. Reaction ID 79088
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248048, Database accession no. BRN 23725
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248049, Database accession no. Reaction ID 1040871
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DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002248051, Database accession no. Reaction ID 382918
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