HRP20151187T1 - sGC STIMULATORI ILI sGC AKTIVATORI SAMOSTALNO I U KOMBINACIJI S INHBITORIMA PDE5 ZA LIJEÄŚENJE CISTIÄŚNE FIBROZE - Google Patents
sGC STIMULATORI ILI sGC AKTIVATORI SAMOSTALNO I U KOMBINACIJI S INHBITORIMA PDE5 ZA LIJEÄŚENJE CISTIÄŚNE FIBROZE Download PDFInfo
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- HRP20151187T1 HRP20151187T1 HRP20151187TT HRP20151187T HRP20151187T1 HR P20151187 T1 HRP20151187 T1 HR P20151187T1 HR P20151187T T HRP20151187T T HR P20151187TT HR P20151187 T HRP20151187 T HR P20151187T HR P20151187 T1 HRP20151187 T1 HR P20151187T1
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- Prior art keywords
- methyl
- fluorobenzyl
- pyrazolo
- pyridin
- phenyl
- Prior art date
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- 201000003883 Cystic fibrosis Diseases 0.000 title claims 14
- 229940127296 soluble guanylate cyclase stimulator Drugs 0.000 title claims 6
- 239000012190 activator Substances 0.000 title claims 4
- 101100189582 Dictyostelium discoideum pdeD gene Proteins 0.000 title 1
- 101150098694 PDE5A gene Proteins 0.000 title 1
- 102100029175 cGMP-specific 3',5'-cyclic phosphodiesterase Human genes 0.000 title 1
- WXXSNCNJFUAIDG-UHFFFAOYSA-N riociguat Chemical compound N1=C(N)C(N(C)C(=O)OC)=C(N)N=C1C(C1=CC=CN=C11)=NN1CC1=CC=CC=C1F WXXSNCNJFUAIDG-UHFFFAOYSA-N 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 6
- ATOAHNRJAXSBOR-UHFFFAOYSA-N BAY 41-2272 Chemical compound NC1=NC(C=2C3=CC=CN=C3N(CC=3C(=CC=CC=3)F)N=2)=NC=C1C1CC1 ATOAHNRJAXSBOR-UHFFFAOYSA-N 0.000 claims 5
- 229940079593 drug Drugs 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 5
- HFXJDFUTCVGWAQ-UHFFFAOYSA-N 1-[[2-[2-fluoro-3-(trifluoromethyl)phenyl]-5-methyl-1,3-thiazol-4-yl]methyl]pyrazole-4-carboxylic acid Chemical compound CC=1SC(C=2C(=C(C=CC=2)C(F)(F)F)F)=NC=1CN1C=C(C(O)=O)C=N1 HFXJDFUTCVGWAQ-UHFFFAOYSA-N 0.000 claims 4
- FTQHGWIXJSSWOY-UHFFFAOYSA-N nelociguat Chemical compound N1=C(N)C(NC(=O)OC)=C(N)N=C1C(C1=CC=CN=C11)=NN1CC1=CC=CC=C1F FTQHGWIXJSSWOY-UHFFFAOYSA-N 0.000 claims 4
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims 4
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 3
- YFJKHTZXXMBJEW-UHFFFAOYSA-N 2-[(4-chlorophenyl)sulfonylamino]-4,5-dimethoxy-n-(4-thiomorpholin-4-ylsulfonylphenyl)benzamide Chemical compound C=1C=C(S(=O)(=O)N2CCSCC2)C=CC=1NC(=O)C=1C=C(OC)C(OC)=CC=1NS(=O)(=O)C1=CC=C(Cl)C=C1 YFJKHTZXXMBJEW-UHFFFAOYSA-N 0.000 claims 2
- VAIBMQLMFYXTLJ-UHFFFAOYSA-N 2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]-5-pyridin-4-ylpyrimidin-4-amine Chemical compound NC1=NC(C=2C3=CC=CN=C3N(CC=3C(=CC=CC=3)F)N=2)=NC=C1C1=CC=NC=C1 VAIBMQLMFYXTLJ-UHFFFAOYSA-N 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- CLBKNBQBZVMYKT-UHFFFAOYSA-N 4-[[2-[3-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl]methyl]benzoic acid Chemical compound C1=CC(C(=O)O)=CC=C1CC1=CSC(C=2C=C(C=CC=2)C(F)(F)F)=N1 CLBKNBQBZVMYKT-UHFFFAOYSA-N 0.000 claims 2
- AQYFUZRYBJBAGZ-UHFFFAOYSA-N BAY-41-8543 Chemical compound NC1=NC(C=2C3=CC=CN=C3N(CC=3C(=CC=CC=3)F)N=2)=NC(N)=C1N1CCOCC1 AQYFUZRYBJBAGZ-UHFFFAOYSA-N 0.000 claims 2
- YNDMDCJWXXDPFE-UHFFFAOYSA-N GSK2181236A Chemical compound CC1=CC(C=2C=CC(OC(F)(F)F)=CC=2)=CC=C1COC1=CC=CC=C1C(N=1)=CC=CC=1N1N=CC(C(O)=O)=C1C(F)(F)F YNDMDCJWXXDPFE-UHFFFAOYSA-N 0.000 claims 2
- SECKRCOLJRRGGV-UHFFFAOYSA-N Vardenafil Chemical compound CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 SECKRCOLJRRGGV-UHFFFAOYSA-N 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- WPYWMXNXEZFMAK-UHFFFAOYSA-N cinaciguat Chemical compound C=1C=C(C(O)=O)C=CC=1CN(CCCCC(=O)O)CCC1=CC=CC=C1OCC(C=C1)=CC=C1CCC1=CC=CC=C1 WPYWMXNXEZFMAK-UHFFFAOYSA-N 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229960003310 sildenafil Drugs 0.000 claims 2
- 159000000000 sodium salts Chemical class 0.000 claims 2
- 229960002381 vardenafil Drugs 0.000 claims 2
- LGGWBDASODTKNP-UHFFFAOYSA-N 1-[[2-[3-chloro-5-(trifluoromethyl)phenyl]-5-methyl-1,3-thiazol-4-yl]methyl]pyrazole-4-carboxylic acid Chemical compound CC=1SC(C=2C=C(C=C(Cl)C=2)C(F)(F)F)=NC=1CN1C=C(C(O)=O)C=N1 LGGWBDASODTKNP-UHFFFAOYSA-N 0.000 claims 1
- RCJYGWGQCPDYSL-HZPDHXFCSA-N 7-[(3-bromo-4-methoxyphenyl)methyl]-1-ethyl-8-[[(1r,2r)-2-hydroxycyclopentyl]amino]-3-(2-hydroxyethyl)purine-2,6-dione Chemical compound C=1C=C(OC)C(Br)=CC=1CN1C=2C(=O)N(CC)C(=O)N(CCO)C=2N=C1N[C@@H]1CCC[C@H]1O RCJYGWGQCPDYSL-HZPDHXFCSA-N 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 229960000307 avanafil Drugs 0.000 claims 1
- WEAJZXNPAWBCOA-INIZCTEOSA-N avanafil Chemical compound C1=C(Cl)C(OC)=CC=C1CNC1=NC(N2[C@@H](CCC2)CO)=NC=C1C(=O)NCC1=NC=CC=N1 WEAJZXNPAWBCOA-INIZCTEOSA-N 0.000 claims 1
- 150000001875 compounds Chemical group 0.000 claims 1
- 229950003418 dasantafil Drugs 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- MVYUCRDXZXLFSB-UHFFFAOYSA-N lodenafil Chemical compound CCCC1=NN(C)C(C(N=2)=O)=C1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N(CC1)CCN1CCOC(=O)OCCN(CC1)CCN1S(=O)(=O)C(C=1)=CC=C(OCC)C=1C(N1)=NC(=O)C2=C1C(CCC)=NN2C MVYUCRDXZXLFSB-UHFFFAOYSA-N 0.000 claims 1
- 229950002245 mirodenafil Drugs 0.000 claims 1
- MIJFNYMSCFYZNY-UHFFFAOYSA-N mirodenafil Chemical compound C1=C(C=2NC=3C(CCC)=CN(CC)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)N1CCN(CCO)CC1 MIJFNYMSCFYZNY-UHFFFAOYSA-N 0.000 claims 1
- 229960000835 tadalafil Drugs 0.000 claims 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 claims 1
- 229960000438 udenafil Drugs 0.000 claims 1
- IYFNEFQTYQPVOC-UHFFFAOYSA-N udenafil Chemical compound C1=C(C=2NC=3C(CCC)=NN(C)C=3C(=O)N=2)C(OCCC)=CC=C1S(=O)(=O)NCCC1CCCN1C IYFNEFQTYQPVOC-UHFFFAOYSA-N 0.000 claims 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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Claims (12)
1. Uporaba sGC stimulatora ili aktivatora odabranog iz skupine koja sadrži 2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-(4-morfolinil)-4,6-pirimidindiamin (1), 2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-(4-piridinil)-4-pirimidinamin (2), metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinil(metil)karbamat (3), metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinilkarbamat (4), 3-(4-amino-5-ciklopropilpirimidin-2-il)-1-(2-fluorobenzil)1H-pirazolo[3,4-b]piridin (4a), natrijevu sol 5-kloro-2-(5-klorotiofen-2-sulfonilamino-N-(4-(morfolin-4-sulfonil)-fenil)-benzamida (6), 2-(4-kloro-fenilsulfonilamino)-4,5-dimetoksi-N-(4-(tiomorfolin-4-sulfonil)-fenil)-benzamid (7), i/ili 4-({(4-karboksibutil)[2-(2-{[4-(2-feniletil) benzil]oksi}fenil)etil]amino}metil) benzojevu kiselinu (5), 1-{6-[5-kloro-2-({4-trans-4-}trifluorometil)cikloheksil]benzil}oksi)fenil] piridin-2-il}-5-(trifluorometil)-1H-pirazol-4-karboksilnu kiselinu (8), 1-[6-(2-(2-metil-4-(4-trifluorometoksifenil)benziloksi)-fenil)piridin-2-il]-5-trifluorometil-pirazol-4-karboksilnu kiselinu (9), 1[6-(3,4-diklorofenil)-2-piridinil-5-(trifluorometil)-1H-pirazol-4-karboksilnu kiselinu (10), 1-({2-[3-kloro-5-(trifluorometil)fenil]-5-metil-1,3-tiazol-4-il}metil)-1H-pirazol-4-karboksilnu kiselinu (11), 4-({2-[3-(trifluorometil)fenil]-1,3-tiazol-4-il}metil)benzojevu kiselinu (12), 1-({2-[2-fluoro-3-(trifluorometil)fenil]-5-metil-1,3-tiazol-4-il}metil)-1H-pirazol-4-karboksilnu kiselinu (13) naznačena time da je za proizvodnju lijeka za liječenje cistične fibroze (CF).
2. Uporaba prema zahtjevu 1 sGC stimulatora odabranog iz skupine koja sadrži metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinil(metil)karbamat (3), metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinilkarbamat (4), 3-(4-amino-5-ciklopropilpirimidin-2-il)-1-(2-fluorobenzil)1H-pirazolo[3,4-b]piridin (4a) naznačena time da je za proizvodnju lijeka za liječenje cistične fibroze (CF).
3. Uporaba prema zahtjevima 1 i 2 metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinil(metil)karbamata (3) naznačena time da je za proizvodnju lijeka za liječenje cistične fibroze (CF).
4. Uporaba prema zahtjevima 1 do 2, 3-(4-amino-5-ciklopropilpirimidin-2-il)-1-(2-fluorobenzil)1H-pirazolo[3,4-b]piridina (4a) naznačena time da je za proizvodnju lijeka za liječenje cistične fibroze (CF).
5. Farmaceutska formulacija koja sadrži barem jedan spoj prema zahtjevima 1 do 4 naznačena time da je za uporabu kod pacijenata koji imaju cističnu fibrozu (CF).
6. Kombinacija barem jednog sGC stimulatora ili aktivatora odabranog iz skupine koja sadrži 2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-(4-morfolinil)-4,6-pirimidindiamin (1), 2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-(4-piridinil)-4-pirimidinamin (2), metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinil(metil)karbamat (3), metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinilkarbamat (4), 3-(4-amino-5-ciklopropilpirimidin-2-il)-1-(2-fluorobenzil)1H-pirazolo[3,4-b]piridin (4a), natrijevu sol 5-kloro-2-(5-klorotiofen-2-sulfonilamino-N-(4-(morfolin-4-sulfonil)-fenil)-benzamida (6), 2-(4-kloro-fenilsulfonilamino)-4,5-dimetoksi-N-(4-(tiomorfolin-4-sulfonil)-fenil)-benzamid (7), i/ili 4-({(4-karboksibutil)[2-(2-{[4-(2-feniletil) benzil] oksi}fenil)etil]amino}metil) benzojevu kiselinu (5), 1-{6-[5-kloro-2-({4-trans-4}trifluorometil)cikloheksil]benzil}oksi)fenil] piridin-2-il}-5-(trifluorometil)-1H-pirazol-4-karboksilnu kiselinu (8), 1-[6-(2-(2-metil-4-(4-trifluorometoksifenil)benziloksi)-fenil)piridin-2-il]-5-trifluorometil-pirazol-4-karboksilnu kiselinu (9), 1[6-(3,4-diklorofenil)-2-piridinil-5-(trifluorometil)-1H-pirazol-4-karboksilnu kiselinu (10), 1-({2-[3-kloro-5-(trifluorometil)fenil]-5-metil-1,3-tiazol-4-il}metil)-1H-pirazol-4-karboksilnu kiselinu (11), 4-({2-[3-(trifluorometil)fenil]-1,3-tiazol-4-il}metil)benzojevu kiselinu (12), 1-({2-[2-fluoro-3-(trifluorometil)fenil]-5-metil-1,3-tiazol-4-il}metil)-1H-pirazol-4-karboksilnu kiselinu (13) s inhibitorom PDE5 odabranim iz skupine koja sadrži Vardenafil, Sildenafil, Tadalafil, Udenafil, Dasantafil, Avanafil, Mirodenafil, Lodenafil, UK 369.003, UK 371.800, SLx2101 i LAS34179 naznačena time da kombinacija sadrži 0.01 do 10 mg sGC stimulatora ili aktivatora i 2.5 do 20 mg inhibitora PDE5.
7. Kombinacija prema zahtjevu 6 naznačena time da sGC stimulator je metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinil-(metil)karbamat (3) ili metil-4,6-diamino-2-[1-(2-fluorobenzil)-1H-pirazolo[3,4-b]piridin-3-il]-5-pirimidinilkarbamat (4).
8. Kombinacija prema zahtjevima 6 i 7 naznačena time da inhibitor PDE5 je Vardenafil ili Sildenafil.
9. Kombinacija prema zahtjevima 6 do 8 naznačena time da je za uporabu kao lijek.
10. Uporaba kombinacije prema zahtjevima 6 do 9 naznačena time da je za proizvodnju lijeka za liječenje cistične fibroze (CF).
11. Kombinacija prema zahtjevima 6 do 9 naznačena time da je za uporabu kod pacijenata koji imaju cističnu fibrozu (CF).
12. Farmaceutska formulacija naznačena time da sadrži barem jednu kombinaciju prema zahtjevima 6 do 8.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10152727 | 2010-02-05 | ||
| EP11701683.2A EP2531187B1 (en) | 2010-02-05 | 2011-02-03 | sGC STIMULATORS OR sGC ACTIVATORS ALONE AND IN COMBINATION WITH PDE5 INHBITORS FOR THE TREATMENT OF CYSTIC FIBROSIS |
| PCT/EP2011/051532 WO2011095534A1 (en) | 2010-02-05 | 2011-02-03 | sGC STIMULATORS OR sGC ACTIVATORS ALONE AND IN COMBINATION WITH PDE5 INHBITORS FOR THE TREATMENT OF CYSTIC FIBROSIS |
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| Publication Number | Publication Date |
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| HRP20151187T1 true HRP20151187T1 (hr) | 2015-12-04 |
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| HRP20151187TT HRP20151187T1 (hr) | 2010-02-05 | 2015-11-05 | sGC STIMULATORI ILI sGC AKTIVATORI SAMOSTALNO I U KOMBINACIJI S INHBITORIMA PDE5 ZA LIJEÄŚENJE CISTIÄŚNE FIBROZE |
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| EP (1) | EP2531187B1 (hr) |
| JP (2) | JP6143461B2 (hr) |
| KR (1) | KR101793304B1 (hr) |
| CN (3) | CN107929271A (hr) |
| AU (1) | AU2011212521B2 (hr) |
| BR (1) | BR112012019666A2 (hr) |
| CA (1) | CA2788969C (hr) |
| CL (1) | CL2012002173A1 (hr) |
| CR (1) | CR20120408A (hr) |
| CY (1) | CY1116878T1 (hr) |
| DK (1) | DK2531187T3 (hr) |
| EA (1) | EA025177B1 (hr) |
| ES (1) | ES2548394T3 (hr) |
| HK (1) | HK1212892A1 (hr) |
| HR (1) | HRP20151187T1 (hr) |
| HU (1) | HUE028008T2 (hr) |
| IL (1) | IL221012B (hr) |
| MA (1) | MA33984B1 (hr) |
| MX (1) | MX342944B (hr) |
| MY (2) | MY159697A (hr) |
| NZ (1) | NZ601612A (hr) |
| PL (1) | PL2531187T3 (hr) |
| PT (1) | PT2531187E (hr) |
| RS (1) | RS54336B1 (hr) |
| SG (1) | SG182819A1 (hr) |
| SI (1) | SI2531187T1 (hr) |
| SM (1) | SMT201500286B (hr) |
| TN (1) | TN2012000397A1 (hr) |
| UA (1) | UA112962C2 (hr) |
| WO (1) | WO2011095534A1 (hr) |
| ZA (1) | ZA201205532B (hr) |
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| NZ601612A (en) * | 2010-02-05 | 2014-08-29 | Bayer Ip Gmbh | Sgc stimulators or sgc activators alone and in combination with pde5 inhibitors for the treatment of cystic fibrosis |
| CN103038232B (zh) | 2010-05-26 | 2016-01-20 | 阿德弗里奥药品有限责任公司 | 单独的和与PDE5抑制剂相组合的sGC刺激剂、sGC活化剂用于治疗系统性硬化症(SSc)的用途 |
| CA2803688A1 (en) * | 2010-06-25 | 2011-12-29 | Bayer Intellectual Property Gmbh | Use of stimulators and activators of soluble guanylate cyclase for treating sickle-cell anemia and conserving blood substitutes |
| EP2594270A3 (en) * | 2011-11-18 | 2013-07-31 | BIP Patents | The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc) |
| PL2892891T3 (pl) | 2012-09-07 | 2020-01-31 | Boehringer Ingelheim International Gmbh | Alkoksypirazole jako aktywatory rozpuszczalnej cyklazy guanylanowej |
| EP3024455A1 (en) | 2013-07-25 | 2016-06-01 | Bayer Pharma Aktiengesellschaft | Sgc stimulators or sgc activators and pde5 inhibitors in combination with additional treatment for the therapy of cystic fibrosis |
| US20160317542A1 (en) | 2013-12-09 | 2016-11-03 | Respira Therapeutics, Inc. | Pde5 inhibitor powder formulations and methods relating thereto |
| CA2933250A1 (en) | 2013-12-11 | 2015-06-18 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| TW201625584A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
| ES2784477T3 (es) | 2014-07-22 | 2020-09-28 | Boehringer Ingelheim Int | Acidos carboxílicos heterocíclicos como activadores de guanilato ciclasa soluble |
| MX2017003516A (es) | 2014-09-17 | 2017-07-28 | Ironwood Pharmaceuticals Inc | Derivados de pirazol como estimuladores de guanilato ciclasa soluble (sgc). |
| JP2017527604A (ja) | 2014-09-17 | 2017-09-21 | アイアンウッド ファーマシューティカルズ インコーポレイテッド | ｓＧＣ刺激剤 |
| US20170298055A1 (en) | 2014-09-17 | 2017-10-19 | Ironwood Pharmaceuticals, Inc. | sGC STIMULATORS |
| JP2018537488A (ja) | 2015-12-18 | 2018-12-20 | ノバルティス アーゲー | インダン誘導体、ならびに可溶性グアニル酸シクラーゼ活性化剤としてのその使用 |
| US10131670B2 (en) | 2016-12-16 | 2018-11-20 | Cystic Fibrosis Foundation Therapeutics, Inc. | Bicyclic heteroaryl derivatives as CFTR potentiators |
| CN110305125B (zh) * | 2019-06-06 | 2021-09-03 | 山东新华制药股份有限公司 | 5-嘧啶-6-氧-吡唑并吡啶类衍生物及其制备方法和应用 |
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| US6331543B1 (en) * | 1996-11-01 | 2001-12-18 | Nitromed, Inc. | Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use |
| US5958926A (en) * | 1996-11-01 | 1999-09-28 | Nitromed, Inc. | Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses |
| BR9911914B1 (pt) * | 1998-07-08 | 2010-10-19 | n-arilamidas do ácido sulfonilaminocarboxìlico substituìdas por enxofre, processo para sua preparação, bem como preparações farmacêuticas que compreendem as mesmas. | |
| DE19834044A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Neue substituierte Pyrazolderivate |
| DE19834047A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Substituierte Pyrazolderivate |
| DE19943635A1 (de) | 1999-09-13 | 2001-03-15 | Bayer Ag | Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| AR031176A1 (es) * | 2000-11-22 | 2003-09-10 | Bayer Ag | Nuevos derivados de pirazolpiridina sustituidos con piridina |
| DE10220570A1 (de) | 2002-05-08 | 2003-11-20 | Bayer Ag | Carbamat-substituierte Pyrazolopyridine |
| DE102005016345A1 (de) * | 2005-04-09 | 2006-10-12 | Bayer Healthcare Ag | Neue Verwendung von 2-Phenyl-substituierten Imidazotriazinon-Derivaten |
| DE102005047946A1 (de) * | 2005-10-06 | 2007-05-03 | Bayer Healthcare Ag | Verwendung von Aktivatoren der löslichen Guanylatzyklase zur Behandlung von akuten und chronischen Lungenkrankheiten |
| US20080081816A1 (en) * | 2006-10-03 | 2008-04-03 | Kaohsiung Medical University | Anti-inflammation activity of newly synthesized xanthine derivatives kmup-1 and kmup-3 |
| US20100210643A1 (en) * | 2007-05-12 | 2010-08-19 | Bayer Schering Pharma Aktiengesellschaft | sGC STIMULATORS, sGC ACTIVATORS AND COMBINATIONS FOR THE TREATMENT OF UROLOGICAL DISORDERS |
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| PE20091258A1 (es) * | 2007-12-03 | 2009-09-12 | Smithkline Beecham Corp | Derivados de piridina como activadores de la guanilato ciclasa soluble |
| WO2009123316A1 (ja) * | 2008-04-04 | 2009-10-08 | 武田薬品工業株式会社 | 複素環誘導体及びその用途 |
| ES2559840T3 (es) * | 2008-06-04 | 2016-02-16 | Synergy Pharmaceuticals Inc. | Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos |
| NZ601612A (en) * | 2010-02-05 | 2014-08-29 | Bayer Ip Gmbh | Sgc stimulators or sgc activators alone and in combination with pde5 inhibitors for the treatment of cystic fibrosis |
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