HRP20110073T1 - Imidazo- i triazolopiridini kao inhibitori 11-beta hidroksisteroid dehidrogenaze tip i - Google Patents
Imidazo- i triazolopiridini kao inhibitori 11-beta hidroksisteroid dehidrogenaze tip i Download PDFInfo
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- HRP20110073T1 HRP20110073T1 HR20110073T HRP20110073T HRP20110073T1 HR P20110073 T1 HRP20110073 T1 HR P20110073T1 HR 20110073 T HR20110073 T HR 20110073T HR P20110073 T HRP20110073 T HR P20110073T HR P20110073 T1 HRP20110073 T1 HR P20110073T1
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- 102000004277 11-beta-hydroxysteroid dehydrogenases Human genes 0.000 title claims 3
- 108090000874 11-beta-hydroxysteroid dehydrogenases Proteins 0.000 title claims 3
- 239000003112 inhibitor Substances 0.000 title claims 2
- 150000005232 imidazopyridines Chemical class 0.000 title 1
- 150000008523 triazolopyridines Chemical class 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 claims abstract 93
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 91
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 79
- 229910052736 halogen Inorganic materials 0.000 claims abstract 60
- 150000002367 halogens Chemical class 0.000 claims abstract 60
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 53
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 29
- 239000001257 hydrogen Substances 0.000 claims abstract 29
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 25
- 150000001875 compounds Chemical class 0.000 claims abstract 17
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 239000012453 solvate Substances 0.000 claims abstract 2
- 125000000217 alkyl group Chemical group 0.000 claims 81
- 125000003545 alkoxy group Chemical group 0.000 claims 59
- -1 bicyclo[2,2,2]octyl Chemical group 0.000 claims 47
- 125000004093 cyano group Chemical group *C#N 0.000 claims 40
- 125000001188 haloalkyl group Chemical group 0.000 claims 37
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 28
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 25
- 125000001424 substituent group Chemical group 0.000 claims 25
- 125000004414 alkyl thio group Chemical group 0.000 claims 24
- 125000004104 aryloxy group Chemical group 0.000 claims 24
- 125000003282 alkyl amino group Chemical group 0.000 claims 16
- 125000004103 aminoalkyl group Chemical group 0.000 claims 16
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 16
- 125000005110 aryl thio group Chemical group 0.000 claims 16
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 16
- 125000004438 haloalkoxy group Chemical group 0.000 claims 16
- 125000003342 alkenyl group Chemical group 0.000 claims 12
- 125000001769 aryl amino group Chemical group 0.000 claims 12
- 125000005241 heteroarylamino group Chemical group 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 125000004659 aryl alkyl thio group Chemical group 0.000 claims 8
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 8
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 8
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 8
- 125000002252 acyl group Chemical group 0.000 claims 7
- 125000005236 alkanoylamino group Chemical group 0.000 claims 7
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 7
- 125000005418 aryl aryl group Chemical group 0.000 claims 7
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims 7
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 7
- 125000005325 aryloxy aryl group Chemical group 0.000 claims 7
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 7
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 7
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 7
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 7
- 238000000034 method Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 2
- BGCPLWWYPZAURQ-UHFFFAOYSA-N 5-[[5-chloro-2-(2,2,6,6-tetramethylmorpholin-4-yl)pyrimidin-4-yl]amino]-3-(3-hydroxy-3-methylbutyl)-1-methylbenzimidazol-2-one Chemical compound ClC=1C(=NC(=NC=1)N1CC(OC(C1)(C)C)(C)C)NC1=CC2=C(N(C(N2CCC(C)(C)O)=O)C)C=C1 BGCPLWWYPZAURQ-UHFFFAOYSA-N 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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Abstract
Spoj formule (1) enantiomeri, dijastereomeri, solvati ili njihove soli, naznačeni time što: W je aril, cikloalkil, heteroaril ili heterociklil, od čega sve po izboru može biti supstituirano s R1, R1a, R1b, R1c i R1d;R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a,
Claims (17)
1. Spoj formule (1)
[image]
enantiomeri, dijastereomeri, solvati ili njihove soli, naznačeni time što:
W je aril, cikloalkil, heteroaril ili heterociklil, od čega sve po izboru može biti supstituirano s R1, R1a, R1b, R1c i R1d;
R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, -SOR2a, -SO2R2a, -NR2SO2R6, -NR2CO2R6, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, alkenil, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
ili alternativno bilo koji od dva R1, R1a, R1b, R1c i R1d se mogu uzeti zajedno kako bi tvorili fuzionirani aril, heteroaril, heterociklil prsten ili spiro heterociklil prsten;
L je veza, O, S, SO, SO2, alkenil, cikloalkil, NR5, CR2R2a, CR2R2aCR2bR2c, SO2NR2, OCR2R2a, OCR2R2aCR2bR2c, CR2R2aO, CR2bR2cCR2R2aO, N(R5)CR2R2a, CR2R2aN(R5), SCR2R2a, CR2R2aS, CR2R2aSO, CR2R2aSO2, SOCR2R2a, SO2CR2R2a, CR2R2aOCR2bR2c, CR2R2aSCR2bR2c, CR2R2aSO2CR2bR2c, SO2NR2CR2aR2b, COCR2R2a CR2R2aCO, CONR5CR2aR2b, CR2R2aCR2bR2cS, CR2R2aCR2bR2cSO, CR2R2aCR2bR2cSO2, uz uvjet da L nije veza kada je W fenil;
R2, R2a, R2b i R2c su nezavisno jedan od drugog vodik, halogen, alkil ili haloalkil;
ili alternativno bilo koji od dva R2, R2a, R2b, i R2c se mogu uzeti zajedno na koji su atom spojeni kako bi tvorili cikloalkil, halogenom supstituirani cikloalkil ili heterociklički prsten;
R3, R3a i R3b su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, -SOR2a, -SO2R2a, -NR2SO2R6, -NR2CO2R6, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, alkenil, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NRsSO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je heterociklil koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R5, uvijek kada se pojavljuje, je nezavisno vodik, alkil, cikloalkil, aril, haloalkil, COR2a, CO2R2a, SO2NR2R2a, ili SO2R2a;
R6, uvijek kada se pojavljuje, je nezavisno alkil, cikloalkil, aril ili heteroaril, od čega sve po izboru može biti supstituirano s R7, R7a, R7b, i R7c; i
R7, R7a, R7b, i R7c, uvijek kada se pojavljuju, su nezavisno jedan od drugog halogen, alkil, haloalkil, alkoksi, aril, ariloksi, arilaril, arilalkil, arilalkiloksi, alkenil, cikloalkil, cikloalkilalkil, cikloalkilalkiloksi, amino, -OH, hidroksialkil, acil, heteroaril, heteroariloksi, heteroarilalkil, heteroarilalkoksi, ariloksialkil, alkiltio, arilalkiltio, ariloksiaril, alkilamido, alkanoilamino, arilkarbonilamino, -NO2, -CN ili tiol.
2. Spoj prema zahtjevu 1, naznačen time što:
W je aril, cikloalkil ili heteroaril, od čega sve po izboru može biti supstituirano s R1, R1a, R1b, R1c i R1d;
R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, -SOR2a, -SO2R2a, -NR2SO2R6, -NR2CO2R6, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, alkenil, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
L je veza, O, S, SO, SO2, NR2, CR2R2a, CR2R2aCR2bR2c, SO2NR2, OCR2R2a, CR2R2aO, SCR2R2a, CR2R2aS, SOCR2R2a, SO2CR2R2a, CR2R2aOCR2bR2c, CR2R2aSCR2bR2c, CR2R2aSO2CR2bR2c, SO2NR2CR2aR2b ili CONR5CR2aR2b;
R2, R2a, R2b i R2c su nezavisno jedan od drugog vodik, halogen, alkil ili haloalkil;
R3, R3a i R3b su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, -SOR2a, -SO2R2a, -NR2SO2R6, -NR2CO2R6, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, alkenil, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5CORb, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je heterociklil koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R5, uvijek kada se pojavljuje, je nezavisno vodik, alkil, cikloalkil, aril, haloalkil, COR2a ili CO2R2a;
R6, uvijek kada se pojavljuje, je nezavisno alkil, cikloalkil, aril ili heteroaril, od čega sve po izboru može biti supstituirano s R7, R7a, R7b, i R7c; i
R7, R7a, R7b, i R7c, uvijek kada se pojavljuju, su nezavisno jedan od drugog halogen, alkil, haloalkil, alkoksi, aril, ariloksi, arilaril, arilalkil, arilalkiloksi, alkenil, cikloalkil, cikloalkilalkil, cikloalkilalkiloksi, amino, -OH, hidroksialkil, acil, heteroaril, heteroariloksi, heteroarilalkil, heteroarilalkoksi, ariloksialkil, alkiltio, arilalkiltio, ariloksiaril, alkilamido, alkanoilamino, arilkarbonilamino, -NO2, -CN ili tiol.
3. Spoj prema zahtjevu 1, naznačen time što:
W je aril, cikloalkil ili heteroaril, od čega sve po izboru može biti supstituirano s R1, R1a, R1b, R1c i R1d;
R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, -SOR2a, -SO2R2a, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
L je veza, O, S, SO, SO2, NR2, CR2R2a, CR2R2aCR2bR2c, OCR2R2a, CR2R2aO, SCR2R2a, CR2R2aS, CR2R2aOCR2bR2c, CR2R2aSCR2bR2c, CR2R2aSO2CR2bR2c ili SO2NR2CR2aR2b;
R2, R2a, R2b i R2c su nezavisno jedan od drugog vodik, halogen, alkil ili haloalkil;
R3, R3a i R3b su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, -SOR2a, -SO2R2a, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je heterociklil koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R6, uvijek kada se pojavljuje, je nezavisno alkil, cikloalkil, aril ili heteroaril, od čega sve po izboru može biti supstituirano s R7, R7a, R7b, i R7c; i
R7, R7a, R7b, i R7c, uvijek kada se pojavljuju, su nezavisno jedan od drugog halogen, alkil, haloalkil, alkoksi, aril, ariloksi, arilaril, arilalkil, arilalkiloksi, alkenil, cikloalkil, cikloalkilalkil, cikloalkilalkiloksi, amino, -OH, hidroksialkil, acil, heteroaril, heteroariloksi, heteroarilalkil, heteroarilalkoksi, ariloksialkil, alkiltio, arilalkiltio, ariloksiaril, alkilamido, alkanoilamino, arilkarbonilamino, -NO2, -CN ili tiol.
4. Spoj prema zahtjevu 1, naznačen time što:
W je aril ili heteroaril, od čega oba po izboru mogu biti supstituirani s R1, R1a, R1b, R1c i R1d;
R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
L je veza, O, S, SO, SO2, CR2R2a, OCR2R2a, CR2R2aO, SO2NR2CR2aR2b ili CR2R2aOCR2bR2c;
R2, R2a, R2b i R2c su nezavisno jedan od drugog vodik, halogen, alkil ili haloalkil;
R3, R3a i R3b su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, -CONR2R2a, -SO2NR2R2a, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je heterociklil koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R6, uvijek kada se pojavljuje, je nezavisno alkil, cikloalkil, aril ili heteroaril, od čega sve po izboru može biti supstituirano s R7, R7a, R7b, i R7c; i
R7, R7a, R7b, i R7c, uvijek kada se pojavljuju, su nezavisno jedan od drugog halogen, alkil, haloalkil, alkoksi, aril, ariloksi, arilaril, arilalkil, arilalkiloksi, alkenil, cikloalkil, cikloalkilalkil, cikloalkilalkiloksi, amino, -OH, hidroksialkil, acil, heteroaril, heteroariloksi, heteroarilalkil, heteroarilalkoksi, ariloksialkil, alkiltio, arilalkiltio, ariloksiaril, alkilamido, alkanoilamino, arilkarbonilamino, -NO2, -CN ili tiol.
5. Spoj prema zahtjevu 1, naznačen time što:
W je aril ili heteroaril, od čega oba po izboru mogu biti supstituirani s R1, R1a, R1b, R1c i R1d;
R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
L je veza, O, S, SO, SO2, CR2R2a, OCR2R2a, CR2R2aO, SO2NR2CR2aR2b ili CR2R2aOCR2bR2c;
R2, R2a, R2b i R2c su nezavisno jedan od drugog vodik, halogen, alkil ili haloalkil;
R3, R3a i R3b su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, -CO2R2a, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, -COR6, -CO2R6, -CO2H, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, -COR6, -CO2R6, -CO2H, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je heterociklil koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, -COR6, -CO2R6, -CO2H, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R6, uvijek kada se pojavljuje, je nezavisno alkil, cikloalkil, aril ili heteroaril, od čega sve po izboru može biti supstituirano s R7, R7a, R7b, i R7c; i
R7, R7a, R7b, i R7c, uvijek kada se pojavljuju, su nezavisno jedan od drugog halogen, alkil, haloalkil, alkoksi, aril, ariloksi, arilaril, arilalkil, arilalkiloksi, alkenil, cikloalkil, cikloalkilalkil, cikloalkilalkiloksi, amino, -OH, hidroksialkil, acil, heteroaril, heteroariloksi, heteroarilalkil, heteroarilalkoksi, ariloksialkil, alkiltio, arilalkiltio, ariloksiaril, alkilamido, alkanoilamino, arilkarbonilamino, -NO2, -CN ili tiol.
6. Spoj prema zahtjevu 1, naznačen time što:
W je aril koji po izboru može biti supstituiran s R1, R1a, R1b, R1c i R1d;
R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
L je veza, O, S, SO, SO2, CR2R2a, OCR2R2a, CR2R2aO, SO2NR2CR2aR2b ili CR2R2aOCR2bR2c;
R2, R2a, R2b i R2c su nezavisno jedan od drugog vodik, halogen, alkil ili haloalkil;
R3, R3a i R3b su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, arilamino, heteroarilamino, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, -COR6, -CO2R6, -CO2H, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, -COR6, -CO2R6, -CO2H, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je heterociklil koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, -COR6, -CO2R6, -CO2H, -CONR2R2a, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R6, uvijek kada se pojavljuje, je nezavisno alkil, cikloalkil, aril ili heteroaril, od čega sve po izboru može biti supstituirano s R7, R7a, R7b, i R7c; i
R7, R7a, R7b, i R7c, uvijek kada se pojavljuju, su nezavisno jedan od drugog halogen, alkil, haloalkil, alkoksi, aril, ariloksi, arilaril, arilalkil, arilalkiloksi, alkenil, cikloalkil, cikloalkilalkil, cikloalkilalkiloksi, amino, -OH, hidroksialkil, acil, heteroaril, heteroariloksi, heteroarilalkil, heteroarilalkoksi, ariloksialkil, alkiltio, arilalkiltio, ariloksiaril, alkilamido, alkanoilamino, arilkarbonilamino, -NO2, -CN ili tiol.
7. Spoj prema zahtjevu 1, naznačen time što:
W je aril koji po izboru može biti supstituiran s R1, R1a, R1b, R1c i R1d;
R1, R1a, R1b, R1c i R1d su vodik, halogen, -OH, -CN, -NO2, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
L je veza, O, S, CR2R2a, OCR2R2a, CR2R2aO ili CR2R2aOCR2bR2c;
R2, R2a, R2b i R2c su nezavisno jedan od drugog vodik, halogen, alkil ili haloalkil;
R3, R3a i R3b su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, aril, heteroaril ili heterociklil, gdje aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, -COR6, -CO2R6, -CO2H, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, -COR6, -CO2R6, -CO2H, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R6, uvijek kada se pojavljuje, je nezavisno alkil, cikloalkil, aril ili heteroaril; i
R7, R7a, R7b, i R7c, uvijek kada se pojavljuju, su nezavisno jedan od drugog halogen, alkil, haloalkil, alkoksi, aril, ariloksi, arilaril, arilalkil, arilalkiloksi, alkenil, cikloalkil, cikloalkilalkil, cikloalkilalkiloksi, amino, -OH, hidroksialkil, acil, heteroaril, heteroariloksi, heteroarilalkil, heteroarilalkoksi, ariloksialkil, alkiltio, arilalkiltio, ariloksiaril, alkilamido, alkanoilamino, arilkarbonilamino, -NO2, -CN ili tiol.
8. Spoj prema zahtjevu 1, naznačen time što:
W je fenil koji po izboru može biti supstituiran s R1, R1a, R1b, R1c i R1d;
R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, aril, heteroaril ili heterociklil;
L je O, S, SCH2, OCH2, CH2O ili CH2OCH2;
R3, R3a i R3b su nezavisno jedan od drugog vodik, halogen, -OH, -CN, -NO2, alkil, haloalkil, cikloalkil, alkoksi, ariloksi, haloalkoksi, alkiltio, ariltio, arilsulfonil, alkilamino, aminoalkil, aril, heteroaril ili heterociklil;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -CN, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c;
R6, uvijek kada se pojavljuje, je nezavisno alkil, cikloalkil, aril ili heteroaril; i
R7, R7a, R7b, i R7c, uvijek kada se pojavljuju, su nezavisno jedan od drugog halogen, alkil, haloalkil, alkoksi, aril, ariloksi, arilalkil, cikloalkil, amino, -OH, hidroksialkil, heteroaril, heteroariloksi, heteroarilalkil, alkiltio, arilalkiltio, -NO2 ili -CN.
9. Spoj prema zahtjevu 1, naznačen time što ima formulu IA:
[image]
gdje:
L se izabire između O, S, OCH2, CH2OCH2 i SO2NHCH2; i
R3, R3a i R3b su nezavisno jedan od drugog izabrani između vodika, halogena, -CF3, OCF3, alkil ili alkoksil; ili
gdje:
R1, R1a, R1b, R1c i R1d su nezavisno jedan od drugog vodik, halogen, alkil, haloalkil, cikloalkil, alkoksi, haloalkoksi, aril, heteroaril ili heterociklil;
L je O;
R3, R3a i R3b su nezavisno jedan od drugog izabrani između vodika ili halogena;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -OCOR6, haloalkil, haloalkoksi, aril ili heterociklil; i
R6, uvijek kada se pojavljuje, je nezavisno alkil ili cikloalkil; ili
gdje:
L se izabire između O, OCH2 i CH2OCH2;
R4 je biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, od kojih oba mogu po izboru biti supstituirani s jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NRsSO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; ili
R4 je cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; i
R6, uvijek kada se pojavljuje, je nezavisno alkil ili cikloalkil; ili
gdje:
L se izabire između O, OCH2 i CH2OCH2;
R4 je fuzionirani ili premošteni cikloalkil, drugačiji od biciklo[2,2,2]oktil ili biciklo[2,2,1]heptil, koji može po izboru biti supstituiran jednim ili više supstituenata izabranih između halogena, -OH, -OR6, -SR6, -OCOR6, -CN, -NR5COR6, -NR5SO2R6, -COR6, -CO2R6, -CO2H, -OCONR2R2a, -CONR2R2a, -NR5CO2R6, -SO2R6, alkil, alkoksi, aril, amino, heterociklil ili heteroaril, gdje alkil, alkoksi, aril, heteroaril ili heterociklil mogu po izboru biti supstituirani s R7, R7a, R7b, i R7c; i
R6, uvijek kada se pojavljuje, je nezavisno alkil ili cikloalkil.
10. Spoj prema zahtjevu 1, naznačen time što ima sljedeću formulu
[image]
[image]
[image]
11. Spoj prema zahtjevu 10, naznačen time što ima sljedeću formulu:
[image]
12. Spoj prema zahtjevu 10, naznačen time što ima sljedeću formulu:
[image]
13. Farmaceutska smjesa, naznačena time što sadrži spoj prema bilo kojem od zahtjeva 1 do 12.
14. Farmaceutska smjesa prema zahtjevu 13, naznačena time što dalje sadrži barem jednu drugu vrstu terapijskog sredstva.
15. Spoj prema bilo kojem od zahtjeva 1 do 12, naznačen time što se koristi u postupku liječenja, prevencije ili usporavanja razvoja bolesti za koju je potrebno liječenje inhibitorom 11-beta-hidroksisteroid dehidrogenaze tip I.
16. Spoj prema bilo kojem od zahtjeva 1 do 12, naznačen time što se koristi u postupku liječenja, prevencije ili usporavanja razvoja dijabetesa, hiperglikemije, pretilosti, dislipidemije, hipertenzije, kognitivnih poremećaja, reumatoidnog artritisa, osteoartritisa, glaukoma i metaboličkog sindroma.
17. Spoj prema bilo kojem od zahtjeva 1 do 12, naznačen time što se koristi u postupku inhibicije enzima 11-beta-hidroksisteroid dehidrogenaze tip I.
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| US68899305P | 2005-06-09 | 2005-06-09 | |
| US11/448,947 US7579360B2 (en) | 2005-06-09 | 2006-06-07 | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| PCT/US2006/022576 WO2006135795A1 (en) | 2005-06-09 | 2006-06-08 | Imidazo- and triazolopyridines as inhibitors of 11-beta hydroxysteroid dehydrogenase type i |
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| US20070299103A1 (en) | 2004-12-01 | 2007-12-27 | Ulrich Abel | [1,2,4]Triazolo[4,3-A]Pyridine Derivatives for the Treatment of Hyperproliferative Diseases |
| WO2006080533A1 (ja) | 2005-01-31 | 2006-08-03 | Mochida Pharmaceutical Co., Ltd. | ３－アミノ－１,２,４－トリアゾール誘導体 |
| WO2007007688A1 (ja) | 2005-07-08 | 2007-01-18 | Mochida Pharmaceutical Co., Ltd. | ３,５－ジアミノ－１,２,４－トリアゾール誘導体 |
| BRPI0710110A2 (pt) | 2006-03-31 | 2011-08-02 | Novartis Ag | compostos orgánicos |
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2006
- 2006-06-07 US US11/448,947 patent/US7579360B2/en active Active
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- 2006-06-08 SI SI200630920T patent/SI1888582T1/sl unknown
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- 2006-06-08 DE DE602006018135T patent/DE602006018135D1/de active Active
- 2006-06-08 JP JP2008515986A patent/JP4994368B2/ja not_active Expired - Fee Related
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- 2006-06-08 AU AU2006257924A patent/AU2006257924B2/en not_active Ceased
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- 2006-06-08 EP EP06784721A patent/EP1888582B1/en active Active
- 2006-06-08 PL PL06784721T patent/PL1888582T3/pl unknown
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- 2006-06-08 AR ARP060102406A patent/AR054385A1/es unknown
- 2006-06-08 DK DK06784721.0T patent/DK1888582T3/da active
- 2006-06-08 PE PE2006000636A patent/PE20070164A1/es not_active Application Discontinuation
- 2006-06-08 KR KR1020087000469A patent/KR20080019276A/ko not_active Application Discontinuation
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2007
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