HRP20100489T1 - Kombinacije koje sadrže antimuskarinska sredstva i pde4 inhibitore - Google Patents
Kombinacije koje sadrže antimuskarinska sredstva i pde4 inhibitore Download PDFInfo
- Publication number
- HRP20100489T1 HRP20100489T1 HR20100489T HRP20100489T HRP20100489T1 HR P20100489 T1 HRP20100489 T1 HR P20100489T1 HR 20100489 T HR20100489 T HR 20100489T HR P20100489 T HRP20100489 T HR P20100489T HR P20100489 T1 HRP20100489 T1 HR P20100489T1
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- Croatia
- Prior art keywords
- pde4 inhibitor
- combination
- combination according
- simultaneous
- separate
- Prior art date
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- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title claims abstract 13
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 title claims abstract 13
- 239000003149 muscarinic antagonist Substances 0.000 title claims 7
- 239000002253 acid Substances 0.000 claims abstract 4
- 150000001450 anions Chemical class 0.000 claims abstract 4
- 239000005557 antagonist Substances 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 229940126214 compound 3 Drugs 0.000 claims abstract 3
- NZEQHVXFILCVRD-CLBCXVIASA-N [(2r)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-2-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate Chemical compound C([C@H]1OC(=O)C(O)(C=2SC=CC=2)C=2SC=CC=2)C(CC2)CC[N+]12CCCOC1=CC=CC=C1 NZEQHVXFILCVRD-CLBCXVIASA-N 0.000 claims abstract 2
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 208000023504 respiratory system disease Diseases 0.000 claims 5
- 229940079593 drug Drugs 0.000 claims 4
- 101150015280 Cel gene Proteins 0.000 claims 3
- CFBUZOUXXHZCFB-OYOVHJISSA-N chembl511115 Chemical compound COC1=CC=C([C@@]2(CC[C@H](CC2)C(O)=O)C#N)C=C1OC1CCCC1 CFBUZOUXXHZCFB-OYOVHJISSA-N 0.000 claims 3
- 229950001653 cilomilast Drugs 0.000 claims 3
- MNDBXUUTURYVHR-UHFFFAOYSA-N roflumilast Chemical compound FC(F)OC1=CC=C(C(=O)NC=2C(=CN=CC=2Cl)Cl)C=C1OCC1CC1 MNDBXUUTURYVHR-UHFFFAOYSA-N 0.000 claims 3
- 229960002586 roflumilast Drugs 0.000 claims 3
- DDYUBCCTNHWSQM-UHFFFAOYSA-N 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-(1,3-dioxoisoindol-2-yl)propanamide Chemical compound COC1=CC=C(C(CC(N)=O)N2C(C3=CC=CC=C3C2=O)=O)C=C1OC1CCCC1 DDYUBCCTNHWSQM-UHFFFAOYSA-N 0.000 claims 2
- XDBHURGONHZNJF-UHFFFAOYSA-N 6-[2-(3,4-diethoxyphenyl)-1,3-thiazol-4-yl]pyridine-2-carboxylic acid Chemical compound C1=C(OCC)C(OCC)=CC=C1C1=NC(C=2N=C(C=CC=2)C(O)=O)=CS1 XDBHURGONHZNJF-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- 102000007202 Muscarinic M3 Receptor Human genes 0.000 claims 2
- 108010008405 Muscarinic M3 Receptor Proteins 0.000 claims 2
- 208000018569 Respiratory Tract disease Diseases 0.000 claims 2
- 230000008485 antagonism Effects 0.000 claims 2
- 229940124748 beta 2 agonist Drugs 0.000 claims 2
- 239000003246 corticosteroid Substances 0.000 claims 2
- 229960001334 corticosteroids Drugs 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229950002896 tetomilast Drugs 0.000 claims 2
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 claims 2
- VXYDHPDQMSVQCU-UHFFFAOYSA-N 2-[4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)piperidin-1-yl]-n-hydroxyacetamide Chemical compound COC1=CC=C(C2(CCN(CC(=O)NO)CC2)C#N)C=C1OC1CCCC1 VXYDHPDQMSVQCU-UHFFFAOYSA-N 0.000 claims 1
- UTUUPXBCDMQYRR-HSZRJFAPSA-N 4-[(2r)-2-(3-cyclopentyloxy-4-methoxyphenyl)-2-phenylethyl]pyridine Chemical compound COC1=CC=C([C@H](CC=2C=CN=CC=2)C=2C=CC=CC=2)C=C1OC1CCCC1 UTUUPXBCDMQYRR-HSZRJFAPSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 102000010918 Cysteinyl leukotriene receptors Human genes 0.000 claims 1
- 108050001116 Cysteinyl leukotriene receptors Proteins 0.000 claims 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 claims 1
- 102100037346 Substance-P receptor Human genes 0.000 claims 1
- DHCOPPHTVOXDKU-UHFFFAOYSA-N Tofimilast Chemical compound C1CN2C(C=3SC=CC=3)=NN=C2C2=C1C(CC)=NN2C1CCCC1 DHCOPPHTVOXDKU-UHFFFAOYSA-N 0.000 claims 1
- YPFLFUJKZDAXRA-UHFFFAOYSA-N [3-(carbamoylamino)-2-(2,4-dichlorobenzoyl)-1-benzofuran-6-yl] methanesulfonate Chemical compound O1C2=CC(OS(=O)(=O)C)=CC=C2C(NC(N)=O)=C1C(=O)C1=CC=C(Cl)C=C1Cl YPFLFUJKZDAXRA-UHFFFAOYSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- PCCPERGCFKIYIS-AWEZNQCLSA-N daxalipram Chemical compound C1=C(OC)C(OCCC)=CC([C@@]2(C)OC(=O)NC2)=C1 PCCPERGCFKIYIS-AWEZNQCLSA-N 0.000 claims 1
- -1 denbufilin Chemical compound 0.000 claims 1
- OMFNSKIUKYOYRG-MOSHPQCFSA-N drotaverine Chemical compound C1=C(OCC)C(OCC)=CC=C1\C=C/1C2=CC(OCC)=C(OCC)C=C2CCN\1 OMFNSKIUKYOYRG-MOSHPQCFSA-N 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- STTRYQAGHGJXJJ-LICLKQGHSA-N filaminast Chemical compound COC1=CC=C(C(\C)=N\OC(N)=O)C=C1OC1CCCC1 STTRYQAGHGJXJJ-LICLKQGHSA-N 0.000 claims 1
- 229950006884 filaminast Drugs 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 229950008462 lirimilast Drugs 0.000 claims 1
- DPHDSIQHVGSITN-UHFFFAOYSA-N n-(3,5-dichloropyridin-4-yl)-2-[1-[(4-fluorophenyl)methyl]-5-hydroxyindol-3-yl]-2-oxoacetamide Chemical compound C1=C(C(=O)C(=O)NC=2C(=CN=CC=2Cl)Cl)C2=CC(O)=CC=C2N1CC1=CC=C(F)C=C1 DPHDSIQHVGSITN-UHFFFAOYSA-N 0.000 claims 1
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims 1
- 238000004806 packaging method and process Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000000144 pharmacologic effect Effects 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- RRRUXBQSQLKHEL-UHFFFAOYSA-N piclamilast Chemical compound COC1=CC=C(C(=O)NC=2C(=CN=CC=2Cl)Cl)C=C1OC1CCCC1 RRRUXBQSQLKHEL-UHFFFAOYSA-N 0.000 claims 1
- 229950005184 piclamilast Drugs 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044551 receptor antagonist Drugs 0.000 claims 1
- 239000002464 receptor antagonist Substances 0.000 claims 1
- HJORMJIFDVBMOB-UHFFFAOYSA-N rolipram Chemical compound COC1=CC=C(C2CC(=O)NC2)C=C1OC1CCCC1 HJORMJIFDVBMOB-UHFFFAOYSA-N 0.000 claims 1
- 229950005741 rolipram Drugs 0.000 claims 1
- 229960000278 theophylline Drugs 0.000 claims 1
- 229950003899 tofimilast Drugs 0.000 claims 1
- 229940122694 Muscarinic M3 receptor antagonist Drugs 0.000 abstract 1
- 239000003681 muscarinic M3 receptor antagonist Substances 0.000 abstract 1
Classifications
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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- Wrappers (AREA)
Abstract
Kombinacija, naznačena time, da sadrži (a) inhibitor PDE4 i (b) antagonist muskarinskih receptora M3, koji antagonist je spoj 3 (R)-(2-hidroksi-2,2-ditien-2-ilacetoksi)-1-(3-fenoksipropil)-1-azoniabiciklo[2.2.2]oktan, u obliku soli koja sadrži anion X, koji je farmaceutski prihvatljiv anion mono ili polivalentne kiseline. Patent sadrži još 18 patentnih zahtjeva.
Claims (19)
1. Kombinacija, naznačena time, da sadrži (a) inhibitor PDE4 i (b) antagonist muskarinskih receptora M3, koji antagonist je spoj 3 (R)-(2-hidroksi-2,2-ditien-2-ilacetoksi)-1-(3-fenoksipropil)-1-azoniabiciklo[2.2.2]oktan, u obliku soli koja sadrži anion X, koji je farmaceutski prihvatljiv anion mono ili polivalentne kiseline.
2. Kombinacija u skladu s patentnim zahtjevom 1, naznačena time, da je antagonist M3 muskarinskih receptora (b) spoj 3(R)-(2-hidroksi-2,2-ditien-2-ilacetoksi)-1-(3-fenoksipropil)-1-azoniabiciklo[2.2.2]oktan bromid.
3. Kombinacija u skladu s patentnim zahtjevom 1 ili 2, naznačena time, da je inhibitor PDE4 odabran iz skupine koju čine: teofilin, drotaverin hidroklorid, cilomilast, roflumilast, denbufilin, rolipram, tetomilast, enprofilin, arofilin, cipamfilin, tofimilast, filaminast, piklamilast, (R)-(+)-4-[2-(3-ciklopentiloksi-4-metoksifenil)-2-feniletil]piridin, mesopram, N-(3,5-dikloro-4-piridinil)-2-[l-(4-fluorobenzil)-5-hidroksi-1H-indol-3-il]-2-oksoacetamid, CDC-801 (ex. Celgene), CC-1088 (ex. Celgene), Lirimilast, ONO-6126 (ex. Ono), CC-10004 (ex. Celgene) i MN-001 (ex. Kvorin), po izboru u obliku njihovih racemata, enantiomera, dijastereomera i mješavina navedenog te, po izboru, njihovih farmakološki kompatibilnih adicijskih soli kiselina.
4. Kombinacija u skladu s patentnim zahtjevom 3, naznačena time, da je inhibitor PDE4 odabran iz skupine koju čine cilomilast, roflumilast, denbufilin i tetomilast, po izboru u obliku njihovih racemata, enantiomera, dijastereomera i mješavina navedenog te, po izboru, njihovih farmakološki kompatibilnih adicijskih soli kiselina.
5. Kombinacija u skladu s patentnim zahtjevom 4, naznačena time, da je inhibitor PDE4 roflumilast.
6. Kombinacija u skladu s patentnim zahtjevom 4, naznačena time, da je inhibitor PDE4 cilomilast.
7. Kombinacija u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačena time, da su djelatne tvari (a) i (b) sadržane u jednom farmaceutskom pripravku.
8. Kombinacija u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačena time, da dodatno sadržava (c) dodatni djelatni spoj koji je odabran između: (a) β2-agonista, (b) kortikosteroida, (c) antagonista leukotrien-D4 receptora, (d) inhibitora egfr-kinaze, (e) inhibitora p38 kinaze i (f) agonista NK1 receptora.
9. Kombinacija u skladu s patentnim zahtjevom 8, naznačena time, da je djelatni spoj (c) odabran iz skupine koju čine (a) β2-agonisti i (b) kortikosteroidi.
10. Uporaba (a) inhibitora PDE4 kako se definira u bilo kojem od patentnih zahtjeva 1 i 3 do 6 i (b) antagonista muskarinskih receptora M3 kako se definiraju u patentnom zahtjevu 1 ili 2, naznačena time, da se koristi za pripravu lijeka za istovremenu, paralelnu, odvojenu ili sekvencijsku primjenu u liječenju bolesti dišnih putova koja reagira na M3 antagonizam kod bolesnika.
11. Uporaba u skladu s patentnim zahtjevom 10, naznačena time, da je bolest dišnih putova astma ili kronična opstruktivna bolest pluća (COPD).
12. Proizvedeni lijek, naznačen time, da sadrži (a) inhibitor PDE4 kako se definira u bilo kojem od patentnih zahtjeva 1 i 3 do 6 i (b) antagonist muskarinskih receptora M3 kako se definira u patentnom zahtjevu 1 ili 2, u obliku kombiniranog pripravka za istovremenu, paralelnu, odvojenu ili sekvencijsku primjenu u liječenju bolesnika koji boluje od ili je osjetljiv na bolest dišnih putova koja reagira na M3 antagonizam.
13. Proizvedeni lijek u skladu s patentnim zahtjevom 12, naznačen time, da dodatno sadržava djelatni spoj (c) kako se definira u patentnom zahtjevu 8 ili 9.
14. Komplet dijelova, naznačen time, da sadrži (b) antagonist muskarinskih receptora M3 kako se definira u patentnom zahtjevu 1 ili 2 zajedno s uputama za istovremenu, paralelnu, odvojenu ili sekvencijsku primjenu u kombinaciji s (a) inhibitorom PDE4 kako se definira u bilo kojem od patentnih zahtjeva 1 i 3 do 6 za liječenje bolesnika koji boluje od ili je osjetljiv na bolest dišnih putova kako se definira u patentnom zahtjevu 10 ili 11.
15. Komplet u skladu s patentnim zahtjevom 14, naznačen time, da dodatno sadrži djelatni spoj (c) kako se definira u patentnom zahtjevu 8 ili 9.
16. Pakiranje, naznačeno time, da sadrži (b) antagonist muskarinskih receptora M3 kako se definira u patentnom zahtjevu 1 ili 2 i (a) inhibitor PDE4 kako se definira u bilo kojem od patentnih zahtjeva 1 i 3 do 6 za istovremenu, paralelnu, odvojenu ili sekvencijsku primjenu u liječenju bolesti dišnih putova kako se definira u patentnom zahtjevu 10 ili 11.
17. Pakiranje u skladu s patentnim zahtjevom 16, naznačeno time, da dodatno sadrži djelatni spoj (c) kako se definira u patentnom zahtjevu 8 ili 9.
18. Uporaba (b) antagonista muskarinskih receptora M3 kako se definira u patentnom zahtjevu 1 ili 2, naznačena time, da se koristi za pripravu lijeka za istovremenu, paralelnu, odvojenu ili sekvencijsku primjenu u kombinaciji s (a) inhibitorom PDE4 kako se definira u bilo kojem od patentnih zahtjeva 1 i 3 do 6 za liječenje bolesti dišnih putova kako se definira u patentnom zahtjevu 10 ili 11.
19. Uporaba (a) inhibitora PDE4 kako se definira u bilo kojem od patentnih zahtjeva 1 i 3 do 6, naznačena time, da se koristi za pripravu lijeka za istovremenu, paralelnu, odvojenu ili sekvencijsku primjenu u kombinaciji s (b) antagonistom muskarinskih receptora M3 kako se definira u patentnom zahtjevu 1 ili 2 za liječenje bolesti dišnih putova kako se definira u patentnom zahtjevu 10 ili 11.
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HRP20090215TT HRP20090215T4 (hr) | 2004-05-31 | 2009-04-09 | Kombinacije koje sadrže antimuskarinska sredstva i beta-adrenergiäśke agoniste |
HR20100489T HRP20100489T1 (hr) | 2004-05-31 | 2010-09-03 | Kombinacije koje sadrže antimuskarinska sredstva i pde4 inhibitore |
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