http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-071236-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_985e586742507c77adffd57be9bc530e http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12a9e9ce63eb0bbf3658453fb50a6d9b |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-08 |
| filingDate | 2009-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2010-06-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-071236-A1 |
| titleOfInvention | CYCLE INHIBITORS OF 11BETA-HYDROXIESTEROID DEHYDROGENASE 1 |
| abstract | xi C1-6, C3-6 halocycloalkoxy, halocycloalkylalkyl The present application refers to C4-7 pharmaceutic salts, C1-6 alkylthio, C3-6 cycloalkylthio, C4-7 cycloalkylalkylthio, C1-6 haloalkylthio, and halogenic acceptable compositions thereof and pharmaceutical compositions thereof, which are useful for C3-6 paraloalkylthio, C4-7 halocycloalkylalkylthio, C1-6 alkanesulfinyl, C3-6 cycloalkanesulfinyl, ci therapeutic treatment of C4-7 associacloalkylalkanesulfinyl diseases, haloalkanesulphonylated with modulation or inhibition of 11betads in mammals , also refers to compositions C C1-6, halocycloalkanesulfinyl C3-6, halocycloalkharmaceuticals of the compounds and methods for suuilalcanosulfinyl C4-7, alkanesulfonyl C1-6, cic use in the reduction or control of the production of deloalkanesulfonyl C3-6, cycloalkylalkanesulfonyl in a cell or the inhibition of conv C4-7, haloalkanesulfonyl C1-6, halocycloalkanesulfonyl C3-6, halocycloalkylalkanesulfoni C4-7, cortisone ersion in cortisol in a cell. Claim 1: A compound of formula (1) in which C1-6 alkylamino, C1-6 dialkylamino, C1-6 alkoxy-C1-6 alkoxy, C1-6 haloalkoxy-C1-6 alkoxy, alkoxy: R1 is (a) absent or (b) is selected from C1-6 arbonyl, H2NCO, H2NSO2, C1-6 alkylaminocarbonyl, C2-6 alkenyl, C2-6 alkynyl, C1-3 alkoxy-C1-3 alkoxy or C1-3 alkoxy-C1- alkyl 3 and C1-6, C1-6 dialkylaminocarbonyl, C1-3-alkoxy is optionally substituted with up to four C1-3 grupkylaminocarbonyl, heterocyclylcarbonyl, C1-6 alkylaminosulfonyl, C1-dialkylaminosulfonyl independently selected from fluorine, c-6, heterocyclylsulfonyl, C1- alkylcarbonylamino iano, oxo, R4, R4O-, (R4) 2N-, R4O2C-, R4S, R4S (= O) 6, C1-6 alkylcarbonylamino-C1-6 alkyl, alkyl-, R4S (= O) 2-, R4C ( = O) NR4-, (R4) 2NC (= O) -, (R4) 2NC (= O) O-, (R4) 2NC (= O) NR4-, R4OC (= O) NR4-, (R4) 2NC (= NCN) lfonylamino C1-6, alkylsulfonylamino C1-6-alkyl C1-6, alkoxycarbonyl C1-6-alkoxy C1-6, alkoxy C1-NR4-, (R4O) 2P (= O) O-, (R4O) 2P (= O) NR4-, R4OS (= O ) 2NR4-, (R4) 2NS (= O) 2O-, (R4) 2NS (= O) 2NR4-, R4S (= O) 2NR4-, 6-C1-6 alkyl, C1-6 haloalkoxy-C1-6 alkyl , C1-6 hydroxyalkoxy, heteroaryl, oxo, C1-R4S aminoalkyl (= O) 2NHC (= O) -, R4S (= O) 2NHC (= O) O-, R4S (= O) 2NHC (= O) NR4- , R4OS (= O) 2NHC (= O) -, R4OS (= O) 2NHC (= O) O-, R46, C1-6 alkylamino-C1-6 alkyl, C1OS dialkylamino (= O) 2NHC (= O) NR4 -, (R4) 2NS (= O) 2NHC (= O) -, (R4) 2NS (-6-C1-6 alkylamino-C2-6 alkoxy, C1-6 alkylamino-C2-6 alkoxy, C1-6 dialkylamino- C2-6 alkoxy, alkyl = O) 2NHC (= O) O-, (R4) 2NS (= O) 2NHC (= O) NR4-, R4C (= O) NHS (= O) 2-, R4C (= O ) NHS (= O) 2O-, R4C (= O) NHS (= O) 2NR4-, R4lC1-6carbonyl, C3-6 cycloalkylcarbonyl, cycloaOC (= O) NHS (= O) 2-, R4OC (= O) NHS (= O) 2O-, R4OC (= O) NHS (= C3-6 alkylaminocarbonyl, C3-6 cycloalkyl O) 2NR4-, (R4) 2NC (= O) NHS (= O) 2-, (R4 ) 2NC (= O) NHS (= O) 2C1-6 aminocarbonyl, C3O- dicycloalkylaminocarbonyl, (R4) 2NC (= O) NHS (= O) 2NR4, heterocyclyl, heteroa-6, C3-6 cycloalkylaminosulfonyl, C3-6 cycloalkyl C 1-6 alkyl amino sulfonyl, dicycloalkylaminosuryl, arylamino and heteroarylamino; A1 is (a) a bond or (b) C1-3 alkylene, CH2CH2O, where the C3-6 oxylfonyl, C1-6 cyanoalkyl, C1-6 aminocarbonylalkyl, C1-6 alkylaminocarbonyl-dno bond is attached to Cy1 or CH2C (= O), where the C1-6 dialkylaminocarbonyl-C1-6 alkyl, cycloalkyl carbonyl carbon is attached to Cy1; Cy1 is aryl, heteroaryl, monocyclic cycloalkyl or heterocyclyl mlaminocarbonyl C3-6-C1-6 alkyl, cycloalkyl C3-6-alkyl C1-6-aminocarbonylalkyl C1-6 and dicycloalonocyclic and is optionally substituted with 1 aquylaminocarbonyl C3-6-alkyl C1- 6; R3 4 groups independently selected from fona were selected from C1-6 alkyl, C2-6 alkenyl, lower alkynyl, chlorine, bromine, iodine, cyano, nitro, amino, hydroxy, carboxy, C1-6 alkyl, C1-6 hydroxyalkyl -6, C3-5 cycloalkyl-C1-4 alkyl, C1-3 alkoxy-C3-6 acycloalkyl, C3-6 hydroxycycloalkyl, C1-3 cycloolkoxy or C1-3 alkoxy-C1-3 alkyl and is optionally substituted with up to four groups selecalkylalkyl C4-7 alkyl, C2-6 alkenyl, haloalkenyl independently ionized between fluorine, cyano, C2-6 oxoC2-6, C2-6 alkynyl, C3-6 alkynyl C2-4, haloC1-6 alkyl, halo, R4 , R4O-, (R4) 2N-, R4O2C-, R4C (= O) O-, R4S, R4S (= C3-6 cycloalkyl, C4-7 halocycloalkylalkyl, alO) -, R4S (= O) 2-, R4C ( = O) NR4-, (R4) 2NC (= O) -, (R4) 2NCkoxy C1-6, cycloalkoxy C3-6, cycloalkylalkoxyC4 - (= O) O-, (R4) 2NC (= O) NR4-, R4OC (= O) NR4-, (R4) 2NC (= NC7, C1-6 haloalkoxy, C3-6 halocycloalkoxy) NR4-, (R4O) 2P (= O) O-, (R4O) 2P (= O) NR4-, R4OS (= O) 2 Noalkylalkoxy C4-7, C1-6 alkylthio, cycloalkylthioR4-, (R4) 2NS (= O) 2O-, (R4) 2NS (= O) 2NR4-, R4S (= O) 2NR4 C3-6, cycloalkylalkylthio C4-7, haloalkylthio C1-, R4S (= O) 2NHC (= O) -, R4S (= O) 2NHC (= O) O-, R4S (= O) 2NH-6, halocycloalkylthio C3-6, halocycloalkylalkylC (= O) NR4-, R4OS (= O) 2NHC (= O ) -, R4OS (= O) 2NHC (= O) O-, uncle C4-7, C1-6 alkanesulfinyl, cycloalkanesulfiniR4OS (= O) 2NHC (= O) NR4-, (R4) 2NS (= O) 2NHC (= O) -, (R4) 2Nlo C3-6, cycloalkylalkanesulfinyl C4-7, haloalcaS (= O) 2NHC (= O) O-, (R4) 2NS (= O) 2NHC (= O) NR4-, R4C (= O ) NHS (= O) 2-, R4C (= O) NHS (= O) 2O-, R4C (= O) NHS (= O) 2NR4-, C1-6 nosulfinyl, C3-6 halocycloalkanesulfinyl, C4-7 halocycloalkylalkyl alkanesulfinyl, alkanesulfonyl R4OC (= O) NHS (= O) 2-, R4OC (= O) NHS (= O) 2O-, R4OC (= O) NHS (= O) 2NR4-, (R4) 2NC (= O) NHS (= O) 2-, (R4) 2NC (= O) NHS (= Oo C1-6, C3-6 cycloalkanesulfonyl) 2O-, (R4) 2NC (= O) NHS (= O) 2NR4, spirocycloalkyl; C4-7 nosulfonyl, C1-6 haloalkanesulfonyl, halocycloalkanesulfonyl (3-6, halocycloalkylalkanesulfheterocyclyl (optionally substituted with alkyl, haloalkyl, halogen or oxo), heteroaryl (C4-7, C1-6 alkylamino, C1-6 alkyloxy, C1-6 alkyloxy 6-C1-6 alkoxy, C1-6 haloalkoxy-C1-alkoxy substituted with alkyl, haloalkyl, alc-6, C1-6 alkoxycarbonyl, H2NCO, H2NSO2, C1-6 alkylamioxy, alkylthio, alkylsulfonyl, halogen, C1-6 trifluonocarbonyl, dialkylaminocarbonyl , alchrometyl, dialkylamino, nitro, cyano, CO2H, CONH2, substituted N-monoalkyl amido, N amido, C1-3-dialkyloxy C1-3-alkylaminocarbonyl C1-3, heterocyclyl-substituted or oxo), aryl-amino (optionally susrbonyl, alkylaminosulfonyl C1 -6, dialkylaminostubstituted with alkyl, alkoxy, alkylthio, C1-6 alkylsulfulfonyl, heterocyclylsulfonyl, alkylcarbononyl, halogen, trifluoromethyl, dialkylamino, C1-6 alkylamino, C1-6 alkylcarbonylaminoC1-6 alkyl, C1-6 alkyl sulfonylamino, C1-6 alkyl -sulfonyl itro, cyano, CO2H, CONH2, N-monoalkyl-C1-6-alkylaminoalkyl, C1-6 alkoxycarbonyl-C1-6 alkoxy and N, N-dialkyl-substituted amido) and heteroaryl, C1-6-alkoxy-C1-6 alkyl, C1-6 haloalkoxy-alquillamino (optionally substituted with alkyl, C1-6 haloo, C1-6 hydroxyalkoxy, heteroaryl, oxo, aminalkyl, alkoxy, alkylthio, alkylsulfonyl, halogen, trifluoromethyl, dialkylamino, nitro, cyano, C1-6 alkyl, alkylamino C1-6-C1-6 alkyl, CO2H dial, CONH2, N-monoalkyl substituted amido, C1-6 amidokylamino C1-6-alkylamino C2-6, alkylamino C1-6-alkoxy C2-6, dialkylamino C1-6 -alkoxy N, N-dialkyl-substituted or oxo); and R4 was selected from C2-6, C1-6 alkylcarbonyl, cycloalkylcarbonyl a independently from H, C1-6 alkyl, C1-6 haloalkyl, C1-6 aminoalkyl, C1-6-alC3-6 alkylamino, C3-6 cycloalkylaminocarbonyl, cycloalkyl C1-6, C1-6 dialkylamino-C1-6 alkyl, hydroC3-6-C1-6 alkylcarbonyl, dicycloalkylaminoxyalkyl C1-6 and C1-6 alkoxy-C1-6 alkyl; or a C3-6 scarbonyl, C3-6 cycloalkylaminosulfonyl, pharmaceutically acceptable cial, enantiomer or C3-6-alkyl C1-6-amino-sulfonyl, C3-6-dicycloalkylaminosulfonyl, the same as the C1 -6 aminotereomer, with the condition that the C1-cocarbonyl -6, C1-6 alkylaminocarbonyl is not a compound represented by the C1-6 founyl, C1-6 dialkylaminocarbonyl C1-6 alkyl structural formulas PR-258 or PR-291, or a pharmaceutically acceptable salt, enantiomer or diastereo, cycloalkylaminocarbonyl C3-6- C1-6 alkyl, C3-6 cycloalkyl C1-6 alkylcarbonylalkylC 1-6 alkyl thereof. and dicycloalkylaminocarbonyl C3-6-C1-6 alkyl; the pyridine ring in the formula (1) is optionally substituted with 1 to 4 groups independently selected from fluorine, chlorine, bromine, iodine, cyano, nitro, amino, hydroxy, carboxy, C1-6 alkyl, C1-6 hydroxyalkyl, cycloalkyl C3-6, hydroxycycloalkyl C3-6, cycloalkylalkylC4-7, alkenyl C2-6, haloalkenyl C2-6, hydroxyalkenyl C2-6, alkynyl C2-6, cycloalkyl C3-6-alkynyl C2-4, haloalkyl C1-6, halocycloalkyl C3-6, C4-7 halocycloalkylalkyl, C1-6 alkoxy, C3-6 cycloalkoxy, C4-7 cycloalkyloxy, C1-6 haloalkoxy, C3-6 halocycloalkoxy, C4-7 halocycloalkylalkoxy, C3-6 cycloalkylthio, cycloalkylalkyl C4-7, C1-6 haloalkylthio, halocicloalquiltio C3-6, C4-7 halocicloalquilalquiltio, alkanesulfinyl C1-6, C3-6 cicloalcanosulfinilo, cicloalquilalcanosulfinilo C4-7, C1-6 haloalcanosulfinilo, halocicloalcanosulfinilo C3-6, C4-7 halocicloalquilalcanosulfinilo, alkanesulfonyl C1-6, C3-6 cycloalkanesulfonyl, C4-7 cycloalkylalkanesulfonyl, halo C1-6 alkanesulfonyl, C3-6 halocycloalkanesulfonyl, C4-7 halocycloalkylalkanesulfonyl, C1-6 alkylamino, C1-6 dialkylamino, C1-6 alkoxy-C1-6 alkoxy, C1-6 haloalkoxy C1-6 alkoxy, C1-6 alkoxycarbonyl, H2NCO, H2NSO2, C1-6 alkylaminocarbonyl, C1-6 dialkylaminocarbonyl, C1-3 alkoxy-C1-3 alkylaminocarbonyl, heterocyclylcarbonyl, C1-6 alkylaminosulfonyl, C1-6 dialkylaminosulfonyl, heterocyclylsulfonyl, C1-6 alkylcarbonylaminoC1-6 alkylcarbonylamino -6, C 1-6 alkylsulfonylamino, C 1-6 alkylsulfonylamino-C 1-6 alkyl, C 1-6 alkoxycarbonyl, C 1-6 alkoxy, C 1-6 alkoxy, C 1-6 haloalkoxy-C 1-6 alkyl, C 1-6 hydroxyalkoxy -6, heteroaryl, oxo, C1-6 aminoalkyl, C1-6 alkylamino-C1-6 alkyl, C1-6 dialkylamino-C1-6 alkylamino-C2-6 alkylamino, C1-6 alkylamino-C2-6 alkoxy, C1- dialkylamino 6-C2-6 alkoxy, C1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, cycloalkylaminocar |
| priorityDate | 2008-05-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 54.