HRP20140893T1 - Derivati 3,4,4a,10b-tetrahidro-1h-tiopirano-[4,3-c]izokinolina - Google Patents
Derivati 3,4,4a,10b-tetrahidro-1h-tiopirano-[4,3-c]izokinolina Download PDFInfo
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- HRP20140893T1 HRP20140893T1 HRP20140893AT HRP20140893T HRP20140893T1 HR P20140893 T1 HRP20140893 T1 HR P20140893T1 HR P20140893A T HRP20140893A T HR P20140893AT HR P20140893 T HRP20140893 T HR P20140893T HR P20140893 T1 HRP20140893 T1 HR P20140893T1
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- Prior art keywords
- methyl
- ethyl
- oxadiazol
- tetrazol
- methoxy
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- ZQCSTHXMOLTGJA-UHFFFAOYSA-N 3,4,4a,10b-tetrahydro-1h-thiopyrano[4,3-c]isoquinoline Chemical class N1=CC2=CC=CC=C2C2C1CCSC2 ZQCSTHXMOLTGJA-UHFFFAOYSA-N 0.000 title 1
- -1 pyrazol-4-yl Chemical group 0.000 claims 262
- 150000001875 compounds Chemical class 0.000 claims 34
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 32
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 29
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 11
- 238000011321 prophylaxis Methods 0.000 claims 11
- 238000011282 treatment Methods 0.000 claims 11
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 10
- 125000001153 fluoro group Chemical group F* 0.000 claims 10
- 230000001154 acute effect Effects 0.000 claims 9
- 229910052731 fluorine Inorganic materials 0.000 claims 8
- 239000011737 fluorine Substances 0.000 claims 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 8
- 208000030090 Acute Disease Diseases 0.000 claims 7
- 208000017667 Chronic Disease Diseases 0.000 claims 6
- 208000006673 asthma Diseases 0.000 claims 6
- 208000030603 inherited susceptibility to asthma Diseases 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 210000002345 respiratory system Anatomy 0.000 claims 6
- 206010006458 Bronchitis chronic Diseases 0.000 claims 4
- 201000003883 Cystic fibrosis Diseases 0.000 claims 4
- 206010014561 Emphysema Diseases 0.000 claims 4
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 4
- 206010006451 bronchitis Diseases 0.000 claims 4
- 208000007451 chronic bronchitis Diseases 0.000 claims 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 4
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 4
- 208000002815 pulmonary hypertension Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001359 1,2,3-triazol-4-yl group Chemical group [H]N1N=NC([*])=C1[H] 0.000 claims 2
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 claims 2
- 125000004505 1,2,4-oxadiazol-5-yl group Chemical group O1N=CN=C1* 0.000 claims 2
- 125000004515 1,2,4-thiadiazol-3-yl group Chemical group S1N=C(N=C1)* 0.000 claims 2
- 125000004516 1,2,4-thiadiazol-5-yl group Chemical group S1N=CN=C1* 0.000 claims 2
- 125000001305 1,2,4-triazol-3-yl group Chemical group [H]N1N=C([*])N=C1[H] 0.000 claims 2
- 125000004509 1,3,4-oxadiazol-2-yl group Chemical group O1C(=NN=C1)* 0.000 claims 2
- 125000004521 1,3,4-thiadiazol-2-yl group Chemical group S1C(=NN=C1)* 0.000 claims 2
- 208000018569 Respiratory Tract disease Diseases 0.000 claims 2
- 239000012752 auxiliary agent Substances 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 claims 2
- 125000004498 isoxazol-4-yl group Chemical group O1N=CC(=C1)* 0.000 claims 2
- 125000004499 isoxazol-5-yl group Chemical group O1N=CC=C1* 0.000 claims 2
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 2
- 125000004289 pyrazol-3-yl group Chemical group [H]N1N=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 claims 2
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 208000014085 Chronic respiratory disease Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 1
- 125000002140 imidazol-4-yl group Chemical group [H]N1C([H])=NC([*])=C1[H] 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
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- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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Claims (28)
1. Spoj, naznačen time, da je to spoj formule 1
[image]
u kojoj
A je S, S(O) ili S(O)2,
ili
R1 je 1-4C-alkoksi, 3-7C-cikloalkoksi, 3-7C-cikloalkilmetoksi, ili 1-4C-alkoksi pretežno ili potpuno supstituiran s fluorom i
R2 je 1-4C-alkoksi, 3-7C-cikloalkoksi, 3-7C-cikloalkilmetoksi, ili 1-4C-alkoksi pretežno ili potpuno supstituiran s fluorom,
ili
R1 i R2 zajedno tvore 1-2C-alkilendioksi-skupinu,
R3 je peteročlani heterociklički prsten koji je supstituiran s R4 i odabran je od sljedećih: pirazol-3-il, pirazol-4-il, tiofen-2-il, tiofen-3-il, imidazol-2-il, imidazol-4-il, izoksazol-3-il, izoksazol-4-il, izoksazol-5-il, 1,3-oksazol-2-il, 1,3-oksazol-4-il, 1,3-oksazol-5-il, 1,3-tiazol-2-il, 1,3-tiazol-4-il, 1,3-tiazol-5-il, 1,2,3-triazol-4-il, 1,2,4-triazol-3-il, 1,2,4-oksadiazol-3-il, 1,2,4-oksadiazol-5-il, 1,3,4-oksadiazol-2-il, 1,2,4-tiadiazol-5-il, 1,2,4-tiadiazol-3-il, 1,3,4-tiadiazol-2-il, tetrazol-2-il ili tetrazol-5-il, gdje
R4 je 1-4C-alkil, metoksimetil, metoksietil, metoksipropil, etoksimetil, propiloksimetil, etoksietil, metilsulfanilmetil, metilsulfaniletil, metilsulfanilpropil, etilsulfanilmetil, propilsulfanilmetil ili etilsulfaniletil,
R5 je nesupstituirani fenil, fenil supstituiran s R6 ili fenil supstituiran s R6 i R7, gdje R6 je halogen, 1-4C-alkil ili 1-4C-alkoksi, i
R7 je halogen, 1-4C-alkil ili 1-4C-alkoksi, ili
R6 i R7 zajedno tvore 1-2C-alkilendioksi-skupinu,
ili stereoizomer od toga spoja.
2. Spoj formule 1 prema zahtjevu 1, naznačen time, da
A je S, S(O) ili S(O)2,
ili
R1 je 1-4C-alkoksi, 3-7C-cikloalkoksi, 3-7C-cikloalkilmetoksi ili 1-4C-alkoksi pretežno ili potpuno supstituiran s fluorom i
R2 je 1-4C-alkoksi, 3-7C-cikloalkoksi, 3-7C-cikloalkilmetoksi ili 1-4C-alkoksi pretežno ili potpuno supstituiran s fluorom,
ili
R1 i R2 zajedno tvore 1-2C-alkilendioksi-skupinu,
R3 je peteročlani heterociklički prsten koji je supstituiran s R4 i odabran je od sljedećih: pirazol-3-il, pirazol-4-il, izoksazol-3-il, izoksazol-4-il, izoksazol-5-il, 1,3-oksazol-2-il, 1,3-oksazol-4-il, 1,3-oksazol-5-il, 1,3-tiazol-2-il, 1,3-tiazol-4-il, 1,3-tiazol-5-il, 1,2,3-triazol-4-il, 1,2,4-triazol-3-il, 1,2,4-oksadiazol-3-il, 1,2,4-oksadiazol-5-il, 1,3,4-oksadiazol-2-il, 1,2,4-tiadiazol-5-il, 1,2,4-tiadiazol-3-il, 1,3,4-tiadiazol-2-il ili tetrazol-5-il, gdje
R4 je 1-4C-alkil, metilsulfanilmetil, etilsulfanilmetil, metilsulfaniletil, metoksimetil, etoksimetil ili metoksietil, i
R5 je nesupstituirani fenil,
ili stereoizomer toga spoja.
3. Spoj formule 1 prema zahtjevu 1, naznačen time, da
A je S, S(O) ili S(O)2,
ili
R1 je 1-2C-alkoksi, ili 1-2C-alkoksi pretežno ili potpuno supstituiran s fluorom i R2 je 1-2C-alkoksi ili 1-2C-alkoksi pretežno ili potpuno supstituiran s fluorom,
ili
R1 i R2 zajedno tvore 1-2C-alkilendioksi-skupinu,
R3 je 1-metil-1H-imidazol-2-il, 1-etil-1H-imidazol-2-il, 5-etil-tiofen-2-il, 5-metil-tiofen-2-il, 3-metil-tiofen-2-il, 3-etil-tiofen-2-il, 1-metil-pirazol-3-il, 1-etil-pirazol-3-il, 1-metil-pirazol-4-il, 2-etil-pirazol-4-il, 4-metil-1,3-oksazol-2-il, 4-etil-1,3-oksazol-2-il, 5-metil-1,3-oksazol-2-il, 5-etil-1,3-oksazol-2-il, 2-metil-1,3-oksazol-4-il, 2-metil-1,3-oksazol-4-il, 2-etil-1,3-oksazol-4-il, 2-metil-1,3-oksazol-5-il, 2-etil-1,3-oksazol-5-il, 4-metil-1,3-oksazol-5-il, 4-etil-1,3-oksazol-5-il, 3-metil-izoksazol-5-il, 3-etil-izoksazol-5-il, 5-metil-izoksazol-3-il, 5-etil-izoksazol-3-il, 4-metil-1,3-tiazol-2-il, 4-etil-1,3-tiazol-2-il, 5-metil-1,3-tiazol-2-il, 2-metil-1,3-tiazol-4-il, 2-etil-1,3-tiazol-4-il, 2-metil-1,3-tiazol-5-il, 2-etil-1,3-tiazol-5-il, 3-metoksimetil-1,2,4-oksadiazol-5-il, 3-etoksimetil-1,2,4-oksadiazol-5-il, 3-metoksipropil-1,2,4-oksadiazol-5-il, 3-propoksimetil-1,2,4-oksadiazol-5-il, 3-metilsulfanilmetil-1,2,4-oksadiazol-5-il, 3-etilsulfanilmetil-1,2,4-oksadiazol-5-il, 3-metilsulfanilpropil-1,2,4-oksadiazol-5-il, 3-propilsulfanilmetil-1,2,4-oksadiazol-5-il, 3-metil-1,2,4-oksadiazol-5-il, 3-etil-1,2,4-oksadiazol-5-il, 5-metil-1,3,4-oksadiazol-2-il, 5-etil-1,3,4-oksadiazol-2-il, 5-tert-butil-1,3,4-oksadiazol-2-il, 5-metoksimetil-1,3,4-oksadiazol-2-il, 5-etoksimetil-1,3,4-oksadiazol-2-il, 5-metilsulfanilmetil-1,3,4-oksadiazol-2-il, 5-etilsulfanilmetil-1,3,4-oksadiazol-2-il, 5-metil-1,2,4-oksadiazol-3-il, 5-etil-1,2,4-oksadiazol-3-il, 3-metil-1,2,4-tiadiazol-5-il, 3-metil-1,2,4-tiadiazol-5-il, 3-etil-1,2,4-tiadiazol-5-il, 2-metil-1,2,3-triazol-4-il, 2-etil-1,2,3-triazol-4-il, 1-metil-1,2,3-triazol-4-il, 1-etil-1,2,3-triazol-4-il, 1-metil-1H-1,2,4-triazol-3-il, 1-etil-1H-1,2,4-triazol-3-il, 1-metil-1H-tetrazol-5-il, 1-etil-1H-tetrazol-5-il, 2-metil-2H-tetrazol-5-il, 2-etil-2H-tetrazol-5-il, 5-etil-2H-tetrazol-2-il, 5-metil-2H-tetrazol-2-il, 1-metoksimetil-1H-tetrazol-5-il, 1-etoksimetil-1H-tetrazol-5-il, 2-metoksimetil-2H-tetrazol-5-il, 2-etoksimetil-2H-tetrazol-5-il, 1-metilsulfanilmetil-1H-tetrazol-5-il, 1-etil-sulfanilmetil-1H-tetrazol-5-il, 2-metilsulfanilmetil-2H-tetrazol-5-il ili 2-etilsulfanilmetil-2H-tetrazol-5-il,
R5 je nesupstituirani fenil, fenil supstituiran s R6 ili fenil supstituiran s R6 i R7 gdje R6 je fluor, metil ili metoksi, i
R7 je fluor, metil ili metoksi,
ili stereoizomer toga spoja.
4. Spoj prema zahtjevu 1, naznačen time, da
A je S, S(O) ili S(O)2,
ili
R1 je 1-2C-alkoksi ili 1-2C-alkoksi pretežno ili potpuno supstituiran s fluorom i R2 je 1-2C-alkoksi ili 1-2C-alkoksi pretežno ili potpuno supstituiran s fluorom,
ili
R1 i R2 zajedno tvore 1-2C-alkilendioksi-skupinu,
R3 je 1-metil-pirazol-3-il, 1-etil-pirazol-3-il, 1-metil-pirazol-4-il, 2-etil-pirazol-4-il, 4-metil-1,3-oksazol-2-il, 4-etil-1,3-oksazol-2-il, 5-metil-1,3-oksazol-2-il, 5-etil-1,3-oksazol-2-il, 2-metil-1,3-oksazol-4-il, 2-metil-1,3-oksazol-4-il, 2-etil-1,3-oksazol-4-il, 2-metil-1,3-oksazol-5-il, 2-etil-1,3-oksazol-5-il, 3-metil-izoksazol-5-il, 3-etil-izoksazol-5-il, 5-metil-izoksazol-3-il, 5-etil-izoksazol-3-il,4-metil-1,3-tiazol-2-il, 4-etil-1,3-tiazol-2-il, 5-metil-1,3-tiazol-2-il, 2-metil-1,3-tiazol-4-il, 2-etil-1,3-tiazol-4-il, 2-metil-1,3-tiazol-5-il, 2-etil-1,3-tiazol-5-il, 3-metoksimetil-1,2,4-oksadiazol-5-il, 3-etoksimetil-1,2,4-oksadiazol-5-il, 3-metilsulfanilmetil-1,2,4-oksadiazol-5-il, 3-etilsulfanilmetil-1,2,4-oksadiazol-5-il, 3-metil-1,2,4-oksadiazol-5-il, 3-etil-1,2,4-oksadiazol-5-il, 5-metil-1,3,4-oksadiazol-2-il, 5-etil-1,3,4-oksadiazol-2-il, 5-metoksimetil-1,3,4-oksadiazol-2-il, 5-etoksimetil-1,3,4-oksadiazol-2-il, 5-metilsulfanilmetil-1,3,4-oksadiazol-2-il, 5-etilsulfanilmetil-1,3,4-oksadiazol-2-il, 5-metil-1,2,4-oksadiazol-3-il, 5-etil-1,2,4-oksadiazol-3-il, 3-metil-1,2,4-tiadiazol-5-il, 3-metil-1,2,4-tiadiazol-5-il, 3-etil-1,2,4-tiadiazol-5-il, 2-metil-1,2,3-triazol-il, 2-etil-1,2,3-triazol-4-il, 1-metil-1,2,3-triazol-4-il, 1-etil-1,2,3-triazol-4-il, 1-metil-1H-tetrazol-5-il, 1-etil-1H-tetrazol-5-il, 2-metil-2H-tetrazol-5-il, 2-etil-2H-tetrazol-5-il, 1-metoksimetil-1H-tetrazol-5-il, 1-etoksimetil-1H-tetrazol-5-il, 2-metoksimetil-2H-tetrazol-5-il, 2-etoksimetil-2H-tetrazol-5-il, 1-metil-sulfanilmetil-1H-tetrazol-5-il, 1-etilsulfanilmetil-1H-tetrazol-5-il, 2-metilsulfanilmetil-2H-tetrazol-5-il ili 2-etilsulfanilmetil-2H-tetrazol-5-il, i
R5 je nesupstituirani fenil,
ili stereoizomer toga spoja.
5. Spoj formule 1 prema zahtjevu 1, naznačen time, da
A je S, S(O) ili S(O)2,
R1 je metoksi ili etoksi, R2 je metoksi,
R3 je 1-metil-1H-imidazol-2-il, 5-etil-tiofen-2-il, 3-metil-tiofen-2-il, 1-etil-pirazol-3-il, 2-etil-pirazol-4-il, 4-etil-1,3-oksazol-2-il, 5-etil-1,3-oksazol-2-il, 2-etil-1,3-oksazol-4-il, 2-etil-1,3-oksazol-5-il, 4-metil-1,3-oksazol-5-il, 3-etil-izoksazol-5-il, 5-metil-izoksazol-3-il, 4-metil-1,3-tiazol-2-il, 5-metil-1,3-tiazol-2-il, 2-metil-1,3-tiazol-4-il, 2-metil-1,3-tiazol-5-il, 3-metoksimetil-1,2,4-oksadiazol-5-il, 3-metoksipropil-1,2,4-oksadiazol-5-il, 3-propoksimetil-1,2,4-oksadiazol-5-il, 3-metilsulfanilmetil-1,2,4-oksadiazol-5-il, 3-etil-1,2,4-oksadiazol-5-il, 5-etil-1,3,4-oksadiazol-2-il, 5-tert-butil-1,3,4-oksadiazol-2-il, 5-metoksimetil-1,3,4-oksadiazol-2-il, 5-metil-1,2,4-oksadiazol-3-il, 3-etil-1,2,4-tiadiazol-5-il, 2-etil-1,2,3-triazol-4-il, 1-etil-1,2,3-triazol-4-il, 1-metil-1H-1,2,4-triazol-3-il, 1-etil-1H-tetrazol-5-il, 2-etil-2H-tetrazol-5-il, 5-etil-2H-tetrazol-2-il, 1-metoksimetil-1H-tetrazol-5-il ili 2-metoksimetil-2H-tetrazol-5-il, i
R5 je fenil, 1,3-benzodioksol-5-il, 2-fluorofenil, 4-fluorofenil, 2,3-difluorofenil,
3,4-difluorofenil, 2-metoksi-4-fluorofenil, 2-metoksi-5-fluorofenil ili 2,5-dimetoksifenil.
ili stereoizomer toga spoja.
6. Spoj formule 1 prema zahtjevu 1, naznačen time, da
A je S, S(O) ili S(O)2, R1 je metoksi ili etoksi, R2 je metoksi,
R3 je 1-etil-pirazol-3-il, 2-etil-pirazol-4-il, 4-etil-1,3-oksazol-2-il, 5-etil-1,3-oksazol-2-il, 2-etil-1,3-oksazol-4-il, 2-etil-1,3-oksazol-5-il, 3-etil-izoksazol-5-il, 5-metil-izoksazol-3-il, 4-metil-1,3-tiazol-2-il, 5-metil-1,3-tiazol-2-il, 2-metil-1,3-tiazol-4-il, 2-metil-1,3-tiazol-5-il, 3-metoksimetil-1,2,4-oksadiazol-5-il, 3-metilsulfanilmetil-1,2,4-oksadiazol-5-il, 3-etil-1,2,4-oksadiazol-5-il, 5-etil-1,3,4-oksadiazol-2-il, 5-metoksimetil-1,3,4-oksadiazol-2-il, 5-metil-1,2,4-oksadiazol-3-il, 3-etil-1,2,4-tiadiazol-5-il, 2-etil-1,2,3-triazol-4-il, 1-etil-1,2,3-triazol-4-il, 1-etil-1H-tetrazol-5-il, 2-etil-2H-tetrazol-5-il, 1-metoksimetil-1H-tetrazol-5-il ili 2-metoksimetil-2H-tetrazol-5-il, i
R5 je nesupstituirani fenil,
ili stereoizomer toga spoja.
7. Spoj formule 1 prema zahtjevu 1, naznačen time, da
A je S, S(O) ili S(O)2,
R1 je etoksi,
R2 je metoksi,
R3 je 5-etil-1,3-oksazol-2-il, 3-etil-izoksazol-5-il, 5-metil-izoksazol-3-il, 2-metil-1,3-tiazol-5-il, 3-metoksimetil-1,2,4-oksadiazol-5-il, 3-metilsulfanilmetil-1,2,4-oksadiazol-5-il, 3-etil-1,2,4-oksadiazol-5-il, 5-metil-1,2,4-oksadiazol-3-il, 1-etil-1H-tetrazol-5-il, 2-etil-2H-tetrazol-5-il, 1-metoksimetil-1H-tetrazol-5-il ili 2-metoksimetil-2H-tetrazol-5-il, i
R5 je nesupstituirani fenil,
ili stereoizomer toga spoja.
8. Spoj prema zahtjevu 1, naznačen time, da ima formulu 1p ili 1m
[image]
gdje
A je S, S(O) ili S(O)2,
R1 je etoksi,
R2 je metoksi,
R3 je 2-etil-2H-terazol-5-il, i
R5 je nesupstituirani fenil,
ili stereoizomer toga spoja.
9. Spoj prema zahtjevu 1, naznačen time, da je odabran iz skupine koju čine:
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(5-etil-1,3-oksazol-2-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(5-metil-1,2,4-oksadiazol-3-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(3-etilizoksazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(5-etil-1,3,4-oksadiazol-2-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(4-etil-1,3-oksazol-2-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(5-metilizoksazol-3-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-(1-{4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]benzoil}piperidin-4-il)-1-[(3-etil-1,2,4-oksadiazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-{[5-(metoksimetil)-1,3,4-oksadiazol-2-il]metil}-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-1,3-oksazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-metil-1,3-tiazol-4-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion,
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-({3-[(metilsulfanil)metil]-1,2,4-oksadiazol-5-il}metil)-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(5-metil-1,3-tiazol-2-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(4-metil-1,3-tiazol-2-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-2H-tetrazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-(1-{4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]benzoil}piperidin-4-il)-1-{[3-(metoksimetil)-1,2,4-oksadiazol-5-il]metil}-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-1,3-oksazol-4-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(1-etil-1H-pirazol-4-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(1-etil-1H-pirazol-3-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-2,2-dioksido-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-2H-tetrazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-metil-1,3-tiazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-2H-1,2,3-triazol-4-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(3-etil-1,2,4-tiadiazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(1-etil-1H-1,2,3-triazol-4-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion,
3-[1-({4-[(2R,4aR,10bR)-9-etoksi-8-metoksi-2-oksido-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-2H-tetrazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(2S,4aR,10bR)-9-etoksi-8-metoksi-2-oksido-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-2H-tetrazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({3-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-2H-tetrazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({3-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(3-etil-1,2,4-oksadiazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion;
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-{[2-(metoksimetil)-2H-tetrazol-5-il]metil}-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion i
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c] izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-{[1-(metoksimetil)-1H-tetrazol-5-il]metil}-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion.
10. Spoj formule 1 prema zahtjevu 1, naznačen time, da je to
3-[1-({4-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-2H-tetrazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion.
11. Spoj formule 1 prema zahtjevu 1, naznačen time, da je to
3-[1-({3-[(4aR,10bR)-9-etoksi-8-metoksi-3,4,4a,10b-tetrahidro-1H-tiopirano[4,3-c]izokinolin-6-il]fenil}karbonil)piperidin-4-il]-1-[(2-etil-2H-tetrazol-5-il)metil]-6-feniltieno[3,2-d]pirimidin-2,4(1H,3H)-dion.
12. Spoj formule 1 ili njegov stereoizomer prema bilo kojem od zahtjeva 1 do 9, naznačen time, da se upotrebljava u liječenju ili profilaksi bolesti.
13. Spoj formule 1 prema zahtjevu 10, naznačen time, da se upotrebljava u liječenju ili profilaksi bolesti.
14. Spoj formule 1 prema zahtjevu 11, naznačen time, da se upotrebljava u liječenju ili profilaksi bolesti.
15. Farmaceutski sastav, naznačen time, da obuhvaća barem jedan od spojeva formule 1 ili njegovih stereoizomera prema bilo kojem od zahtjeva 1 do 9 zajedno s barem jednim farmaceutski prihvatljivim pomoćnim sredstvom.
16. Farmaceutski sastav, naznačen time, da obuhvaća spoj formule 1 prema zahtjevu 10 zajedno s barem jednim farmaceutski prihvatljivim pomoćnim sredstvom.
17. Farmaceutski sastav, naznačen time, da obuhvaća spoj formule 1 prema zahtjevu 11 zajedno s barem jednim farmaceutski prihvatljivim pomoćnim sredstvom.
18. Uporaba spoja formule 1 ili njegovog stereoizomera prema bilo kojem od zahtjeva 1 do 9, naznačena time, da je za proizvodnju farmaceutskog sastava za liječenje ili profilaksu akutne ili kronične bolesti dišnih puteva.
19. Uporaba spoja formule 1 prema zahtjevu 10, naznačena time, da je za proizvodnju farmaceutskog sastava za liječenje ili profilaksu akutne ili kronične bolesti dišnih puteva.
20. Uporaba spoja formule 1 prema zahtjevu 11, naznačena time, da je za proizvodnju farmaceutskog sastava za liječenje ili profilaksu akutne ili kronične bolesti dišnih puteva.
21. Uporaba prema bilo kojem od zahtjeva 18 do 20, naznačena time, da je akutna ili kronična bolest dišnih puteva odabrana iz skupine koja se sastoji od intersticijalne bolesti pluća, pulmonarne fibroze, cistične fibroze, bronhijalne astme, kroničnog bronhitisa, emfizema, kronične opstrukcijske bolesti pluća (COPD) i pulmonarne hipertenzije povezane s COPD.
22. Uporaba prema bilo kojem od zahtjeva 19 i 20, naznačena time, da akutna ili kronična bolest dišnih puteva je bronhijalna astma.
23. Uporaba prema bilo kojem od zahtjeva 19 i 20, naznačena time, da akutna ili kronična bolest dišnih puteva je kronična opstrukcijska bolest pluća (COPD).
24. Spoj formule 1 ili njegov stereoizomer prema bilo kojem od zahtjeva 1 do 9, naznačen time, da se upotrebljava u liječenju ili profilaksi akutne ili kronične bolesti dišnih puteva, koja je odabrana iz skupine koja se sastoji od intersticijalne bolesti pluća, pulmonarne fibroze, cistične fibroze, bronhijalne astme, kroničnog bronhitisa, emfizema, kronične opstrukcijske bolesti pluća (COPD) i pulmonarne hipertenzije povezane s COPD.
25. Spoj formule 1 prema zahtjevu 10, naznačen time, da se upotrebljava u liječenju ili profilaksi akutne ili kronične bolesti dišnih puteva, koja je odabrana iz skupine koja se sastoji od intersticijalne bolesti pluća, pulmonarne fibroze, cistične fibroze, bronhijalne astme, kroničnog bronhitisa, emfizema, kronične opstrukcijske bolesti pluća (COPD) i pulmonarne hipertenzije povezane s COPD.
26. Spoj formule 1 prema zahtjevu 11, naznačen time, da se upotrebljava u liječenju ili profilaksi akutne ili kronične bolesti dišnih puteva, koja je odabrana iz skupine koja se sastoji od intersticijalne bolesti pluća, pulmonarne fibroze, cistične fibroze, bronhijalne astme, kroničnog bronhitisa, emfizema, kronične opstrukcijske bolesti pluća (COPD) i pulmonarne hipertenzije povezane s COPD.
27. Spoj formule 1 prema bilo kojem od zahtjeva 10 i 11, naznačen time, da se upotrebljava u liječenju ili profilaksi bronhijalne astme.
28. Spoj formule 1 prema bilo kojem od zahtjeva 10 i 11, naznačen time, da se upotrebljava u liječenju ili profilaksi kronične opstrukcijske bolesti pluća (COPD).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09179982 | 2009-12-18 | ||
| US31555210P | 2010-03-19 | 2010-03-19 | |
| PCT/EP2010/069704 WO2011073231A1 (en) | 2009-12-18 | 2010-12-15 | 3,4,4A,10B-TETRAHYDRO-1H-THIOPYRANO-[4, 3-c] ISOQUINOLINE DERIVATIVES |
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| HRP20140893T1 true HRP20140893T1 (hr) | 2014-11-07 |
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| HRP20140893AT HRP20140893T1 (hr) | 2009-12-18 | 2014-09-17 | Derivati 3,4,4a,10b-tetrahidro-1h-tiopirano-[4,3-c]izokinolina |
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| US (1) | US9018175B2 (hr) |
| EP (2) | EP2813509B1 (hr) |
| JP (1) | JP5645961B2 (hr) |
| KR (1) | KR20120123313A (hr) |
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| BR (1) | BR112012014058A8 (hr) |
| CA (1) | CA2784013A1 (hr) |
| CO (1) | CO6551705A2 (hr) |
| DK (1) | DK2513119T3 (hr) |
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| WO2014016548A2 (en) * | 2012-07-27 | 2014-01-30 | Cipla Limited | Pharmaceutical composition |
| WO2014090990A1 (en) * | 2012-12-13 | 2014-06-19 | Ludwig Aigner | Leukotriene pathway antagonists for the treatment of dementia, cognitive deficits in parkinson's disease and/or learning and memory deficiencies in parkinson's disease |
| AU2014211755B2 (en) | 2013-02-04 | 2017-07-06 | Grunenthal Gmbh | 4-amino substituted condensed pyrimidine compounds as PDE4 inhibitors |
| ES2638850T3 (es) | 2013-02-19 | 2017-10-24 | Pfizer Inc. | Compuestos de azabenzimidazol como inhibidores de las isoenzimas de la PDE4 para el tratamiento de trastornos del SNC y otros trastornos |
| JP6713982B2 (ja) | 2014-07-24 | 2020-06-24 | ファイザー・インク | ピラゾロピリミジン化合物 |
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