HRP20110201T1 - Spojevi i sastavi kao inhibitori proteaze kanalizirane aktivacije - Google Patents
Spojevi i sastavi kao inhibitori proteaze kanalizirane aktivacije Download PDFInfo
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- HRP20110201T1 HRP20110201T1 HR20110201T HRP20110201T HRP20110201T1 HR P20110201 T1 HRP20110201 T1 HR P20110201T1 HR 20110201 T HR20110201 T HR 20110201T HR P20110201 T HRP20110201 T HR P20110201T HR P20110201 T1 HRP20110201 T1 HR P20110201T1
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- 150000001875 compounds Chemical class 0.000 title claims abstract 35
- 230000003213 activating effect Effects 0.000 title 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims abstract 11
- 150000003839 salts Chemical class 0.000 claims abstract 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 9
- 125000003118 aryl group Chemical group 0.000 claims abstract 7
- 125000003386 piperidinyl group Chemical group 0.000 claims abstract 7
- 125000000217 alkyl group Chemical group 0.000 claims abstract 6
- 125000002837 carbocyclic group Chemical group 0.000 claims abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 6
- 125000001475 halogen functional group Chemical group 0.000 claims abstract 4
- 125000002950 monocyclic group Chemical group 0.000 claims abstract 4
- 125000001424 substituent group Chemical group 0.000 claims abstract 2
- 125000001425 triazolyl group Chemical group 0.000 claims abstract 2
- 101000798702 Homo sapiens Transmembrane protease serine 4 Proteins 0.000 claims 6
- 102100032471 Transmembrane protease serine 4 Human genes 0.000 claims 6
- 102000035195 Peptidases Human genes 0.000 claims 5
- 108091005804 Peptidases Proteins 0.000 claims 5
- 239000004365 Protease Substances 0.000 claims 5
- 230000004913 activation Effects 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 102100037942 Suppressor of tumorigenicity 14 protein Human genes 0.000 claims 4
- 210000001519 tissue Anatomy 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 102100022046 Brain-specific serine protease 4 Human genes 0.000 claims 2
- 108010059081 Cathepsin A Proteins 0.000 claims 2
- 102000005572 Cathepsin A Human genes 0.000 claims 2
- 108091006146 Channels Proteins 0.000 claims 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 claims 2
- 101000897856 Homo sapiens Adenylyl cyclase-associated protein 2 Proteins 0.000 claims 2
- 101000896891 Homo sapiens Brain-specific serine protease 4 Proteins 0.000 claims 2
- 101000836079 Homo sapiens Serpin B8 Proteins 0.000 claims 2
- 101000836075 Homo sapiens Serpin B9 Proteins 0.000 claims 2
- 101000661807 Homo sapiens Suppressor of tumorigenicity 14 protein Proteins 0.000 claims 2
- 101000637855 Homo sapiens Transmembrane protease serine 11E Proteins 0.000 claims 2
- 101000798707 Homo sapiens Transmembrane protease serine 13 Proteins 0.000 claims 2
- 101000638154 Homo sapiens Transmembrane protease serine 2 Proteins 0.000 claims 2
- 101000798700 Homo sapiens Transmembrane protease serine 3 Proteins 0.000 claims 2
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 claims 2
- 108010028275 Leukocyte Elastase Proteins 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 108010091175 Matriptase Proteins 0.000 claims 2
- 101100069392 Mus musculus Gzma gene Proteins 0.000 claims 2
- 102100033174 Neutrophil elastase Human genes 0.000 claims 2
- 102100032001 Transmembrane protease serine 11E Human genes 0.000 claims 2
- 102100032467 Transmembrane protease serine 13 Human genes 0.000 claims 2
- 102100031989 Transmembrane protease serine 2 Human genes 0.000 claims 2
- 108090000631 Trypsin Proteins 0.000 claims 2
- 102000004142 Trypsin Human genes 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
- 229960003910 promethazine Drugs 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 239000012588 trypsin Substances 0.000 claims 2
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000025678 Ciliary Motility disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 102000016911 Deoxyribonucleases Human genes 0.000 claims 1
- 108010053770 Deoxyribonucleases Proteins 0.000 claims 1
- 101000598054 Homo sapiens Transmembrane protease serine 11B Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- MYEJFUXQJGHEQK-ALRJYLEOSA-N Proscillaridin Chemical compound O[C@@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@H]1O[C@@H]1C=C2CC[C@H]3[C@@]4(O)CC[C@H](C5=COC(=O)C=C5)[C@@]4(C)CC[C@@H]3[C@@]2(C)CC1 MYEJFUXQJGHEQK-ALRJYLEOSA-N 0.000 claims 1
- 102100037023 Transmembrane protease serine 11B Human genes 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000000954 anitussive effect Effects 0.000 claims 1
- 230000003110 anti-inflammatory effect Effects 0.000 claims 1
- 229940124584 antitussives Drugs 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 210000000424 bronchial epithelial cell Anatomy 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 229940124630 bronchodilator Drugs 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 229960001340 histamine Drugs 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000037427 ion transport Effects 0.000 claims 1
- 239000007788 liquid Substances 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 210000003097 mucus Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000009266 primary ciliary dyskinesia Diseases 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 230000000241 respiratory effect Effects 0.000 claims 1
- 210000002345 respiratory system Anatomy 0.000 claims 1
- 210000003296 saliva Anatomy 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- -1 C1- 6alkyl Chemical group 0.000 abstract 1
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
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- 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
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Abstract
Spoj formule (1): ili njegove farmaceutski prihvatljive soli, naznačen time, da O-(CR2)p-R2 je supstituent na bilo kojoj poziciji na prstenu A; J je 5-12 člani monociklički ili sjedinjen karbociklički prsten, heterociklički prsten koji obuhvaća N, O i/ili S; arilni ili heteroarilni prsten, pod uvjetom da J nije triazolil; B je ili (CR2)k-R5;Y je veza, -SO2-, -NHCO- ili -O-(CO)-; R1 je halo, -(CR2)l-NR6R7, -(CR2)l-NRC(=NR)-NR6R7, -(CR2)l-C(=NR)-NR6R7, -C(O)-(CR2)l-NR6R7, -(CR2)l-NRSO2R6, -(CR2)l-NR-C(O)-R6, -(CR2)l-SO2NR6R7, ili -(CR2)l-OR6, ili opcijski supstituiran C1-6alkoksi, C1-6alkil, C2-6alkenil ili C2-6alkinil; ili opcijski supstituiran karbociklički prsten, heterociklički prsten, aril ili heteroaril; R3 je C1-6alkil, C2-6alkenil, C2-6alkinil ili -(CR2)l-R5; alternativno, NH-Y-R3 zajedno tvore NH2;R2, R4 i R5 su neovisno opcijski supstituiran 5-12 člani karbociklički prsten, heterociklički prsten, aril ili heteroaril; ili R4 je H, C1-6alkil, C2-6alkenil, C2-6alkinil, ili gdje P je C ili N, a prsten E zajedno s P tvore opcijski supstituiran 5-12 člani monociklički ili sjedinjen prsten; R6 i R7 su neovisno H, C1-6alkil, C2-6alkenil, C2-6alkinil ili -(CR2)l-R5; svaki R je H, ili C1-6alkil, C2-6alkenil, ili C2-6alkinil; l je 0-6; k, m, n i p su neovisno 1-6; x je 0-4; pod uvjetom da R4 je piperidinil kada NH-Y-R3 zajedno tvore NH2; i nadalje pod uvjetom da R5 je piperidinil kada B je (CR2)k-R5.Patent sadrži još 26 patentnih zahtjeva.
Claims (27)
1. Spoj formule (1):
[image]
ili njegove farmaceutski prihvatljive soli, naznačen time, da
O-(CR2)p-R2 je supstituent na bilo kojoj poziciji na prstenu A;
J je 5-12 člani monociklički ili sjedinjen karbociklički prsten, heterociklički prsten koji obuhvaća N, O i/ili S; arilni ili heteroarilni prsten, pod uvjetom da J nije triazolil;
B je
[image]
ili (CR2)k-R5;
Y je veza, -SO2-, -NHCO- ili -O-(CO)-;
R1 je halo, -(CR2)l-NR6R7, -(CR2)l-NRC(=NR)-NR6R7, -(CR2)l-C(=NR)-NR6R7, -C(O)-(CR2)l-NR6R7, -(CR2)l-NRSO2R6, -(CR2)l-NR-C(O)-R6, -(CR2)l-SO2NR6R7, ili -(CR2)l-OR6, ili opcijski supstituiran C1-6alkoksi, C1-6alkil, C2-6alkenil ili C2-6alkinil; ili opcijski supstituiran karbociklički prsten, heterociklički prsten, aril ili heteroaril;
R3 je C1-6alkil, C2-6alkenil, C2-6alkinil ili -(CR2)l-R5; alternativno, NH-Y-R3 zajedno tvore NH2;
R2, R4 i R5 su neovisno opcijski supstituiran 5-12 člani karbociklički prsten, heterociklički prsten, aril ili heteroaril; ili R4 je H, C1-6alkil, C2-6alkenil, C2-6alkinil, ili
[image]
gdje P je C ili N, a prsten E zajedno s P tvore opcijski supstituiran 5-12 člani monociklički ili sjedinjen prsten;
R6 i R7 su neovisno H, C1-6alkil, C2-6alkenil, C2-6alkinil ili -(CR2)l-R5;
svaki R je H, ili C1-6alkil, C2-6alkenil, ili C2-6alkinil;
l je 0-6;
k, m, n i p su neovisno 1-6;
x je 0-4;
pod uvjetom da R4 je piperidinil kada NH-Y-R3 zajedno tvore NH2; i nadalje pod uvjetom da R5 je piperidinil kada B je (CR2)k-R5.
2. Spoj prema zahtjevu 1, naznačen time, da J je tiofenil, tiazolil, fenil, piridil, indazolil, piperidinil ili pirolidinil.
3. Spoj prema zahtjevu 1, naznačen time, da R1je halo, C1-6alkil, CF3, OCF3, fenil, -(CR2)l-NR6R7, -(CR2)l-C(=NR)-NR6R7, -C(O)-(CR2)l-NR6R7, -(CR2)l-NR-SO2R6, -(CR2)l-NR-C(O)-R6, -(CR2)l-SO2NR6R7, ili-(CR2)l-OR6; pri čemu svaki l je 0-1; i
R, R6 i R7 su neovisno H ili C1-6alkil.
4. Spoj prema zahtjevu 1, naznačen time, da R2je fenil ili cikloheksil, od kojih je svaki opcijski supstituiran s halo, SO2(C1-6alkil), ili opcijski halogenirani C1-6alkil ili C1-6alkoksi.
5. Spoj prema zahtjevu 1, naznačen time, da R4je opcijski supstituirani piperidinil, cikloheksil, fenil,
[image]
6. Spoj prema zahtjevu 1, naznačen time, da Y je veza, SO2 ili -O-(CO)-.
7. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj ima formulu (2):
[image]
gdje R2 i J su neovisno opcijski supstituirani 6-člani aril; R3 je C1-6alkil, C2-6alkenil, C2-6alkinil ili -(CR2)l-R5; ili NH-Y-R3 zajedno tvore NH2; svaki R u (CR2) je H ili C1-6alkil; i
m, n i p su neovisno 1-2,
ili njegove farmaceutski prihvatljive soli.
8. Spoj prema zahtjevu 7, naznačen time, da R2 i J su neovisno opcijski supstituirani fenil.
9. Spoj prema zahtjevu 7, naznačen time, da x je 1-3.
10. Spoj prema zahtjevu 7, naznačen time, da Y je SO2.
11. Spoj prema zahtjevu 7, naznačen time, da R3 je C1-6alkil ili opcijski supstituirani benzil.
12. Spoj prema zahtjevu 7, naznačen time, da R4 je opcijski supstituirani piperidinil.
13. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj je odabran iz skupine koja se sastoji od:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
i
[image]
ili njegove farmaceutski prihvatljive soli.
14. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj je odabran iz skupine koja se sastoji od:
[image]
ili njegove farmaceutski prihvatljive soli.
15. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj je odabran iz skupine koja se sastoji od:
[image]
ili njegove farmaceutski prihvatljive soli.
16. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj je odabran iz skupine koja se sastoji od:
[image]
ili njegove farmaceutski prihvatljive soli.
17. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj je
[image]
ili njegove farmaceutski prihvatljive soli.
18. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj je
[image]
ili njegove farmaceutski prihvatljive soli.
19. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj je
[image]
ili njegove farmaceutski prihvatljive soli.
20. Farmaceutski sastav, naznačen time, da sadrži terapeutski učinkovitu količinu spoja prema bilo kojem od zahtjeva 1-19.
21. Spoj prema bilo kojem od zahtjeva 1 do 19, naznačen time, da služi za inhibiciju proteaze kanalizirane aktivacije u stanici ili sustavu tkiva ili kod sisavaca, pri čemu spomenuta proteaza kanalizirane aktivacije je protazin, PRSS22, TMPRSS11 (npr. TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptaza (MTSP-1), CAP2, CAP3, tripzin, katepzin A, ili neutrofil elastaza.
22. Uporaba spoja prema bilo kojem od zahtjeva 1 do 19, naznačena time, da služi za proizvodnju lijeka za liječenje stanja prouzrokovanog proteazom kanalizirane aktivacije u stanici ili sustavu tkiva ili kod sisavaca, i opcijski u kombinaciji s drugim terapeutskim sredstvom, pri čemu spomenuta proteaza kanalizirane aktivacije je protazin, PRSS22, TMPRSS11 (npr. TMPRSS 11B, TMPRSS11E), TMPRSS2. TMPRSS3, TMPRSS4 (MTSP-2), matriptaza (MTSP-1), CAP2, CAP3, tripzin, katepzin A, ili neutrofil elastaza.
23. Uporaba prema zahtjevu 22, naznačena time, da spomenuto stanje je povezano s premještanjem tekućine preko epitela za transport iona ili s nakupljanjem sluzi i pljuvačke u respiratornom tkivu, ili s njihovom kombinacijom.
24. Uporaba prema zahtjevu 22, naznačena time, da spomenuto stanje je cistična fibroza, primarna cilijarna diskinezija, rak pluća, kronični bronhitis, kronična opstrukcijska plućna bolest, astma ili upala respiratornog trakta.
25. Uporaba prema zahtjevu 22, naznačena time, da spomenuto drugo terapeutsko sredstvo je protuupalno, bronhodilatorno, histaminsko, antitusivno, antibiotičko ili DNase, i primjenjuje se prije, istovremeno sa, ili nakon davanja spoja prema bilo kojem od zahtjeva 1 do 19.
26. Spoj prema zahtjevu 21 ili uporaba prema zahtjevu 22, naznačen(a) time, da spomenuta proteaza kanalizirane aktivacije je protazin.
27. Spoj prema zahtjevu 21 ili uporaba prema zahtjevu 22, naznačen(a) time, da spomenuta stanica ili sustav tkiva obuhvaća bronhijalne epitelne stanice.
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| US89147407P | 2007-02-23 | 2007-02-23 | |
| PCT/US2007/085366 WO2008085608A1 (en) | 2007-01-10 | 2007-11-21 | Compounds and compositions as channel activating protease inhibitors |
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| GB0507577D0 (en) * | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
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2007
- 2007-11-21 DE DE602007011670T patent/DE602007011670D1/de active Active
- 2007-11-21 DK DK07854747.8T patent/DK2104535T3/da active
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- 2007-11-21 EP EP10013675A patent/EP2279777A2/en not_active Withdrawn
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- 2007-11-21 EA EA200900920A patent/EA016199B1/ru not_active IP Right Cessation
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2008
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2009
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