RU2419626C2 - Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы - Google Patents
Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы Download PDFInfo
- Publication number
- RU2419626C2 RU2419626C2 RU2008150615/04A RU2008150615A RU2419626C2 RU 2419626 C2 RU2419626 C2 RU 2419626C2 RU 2008150615/04 A RU2008150615/04 A RU 2008150615/04A RU 2008150615 A RU2008150615 A RU 2008150615A RU 2419626 C2 RU2419626 C2 RU 2419626C2
- Authority
- RU
- Russia
- Prior art keywords
- halogen
- optionally substituted
- compound according
- alkyl
- piperidinyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract 24
- 230000003213 activating effect Effects 0.000 title abstract 2
- 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
- 150000003839 salts Chemical class 0.000 claims abstract 6
- 108090000631 Trypsin Proteins 0.000 claims abstract 5
- 102000004142 Trypsin Human genes 0.000 claims abstract 5
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 5
- 239000012588 trypsin Substances 0.000 claims abstract 5
- 239000003814 drug Substances 0.000 claims abstract 2
- 229910052736 halogen Inorganic materials 0.000 claims 21
- 125000005843 halogen group Chemical group 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000003386 piperidinyl group Chemical group 0.000 claims 9
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- -1 substituted —O Chemical class 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000002541 furyl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 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 1
- 125000005959 diazepanyl group Chemical group 0.000 claims 1
- 125000004639 dihydroindenyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 102100029500 Prostasin Human genes 0.000 abstract 2
- 108010031970 prostasin Proteins 0.000 abstract 2
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 239000002753 trypsin inhibitor Substances 0.000 abstract 1
- DDPOIFYOZBCVPM-KZJMBQCBSA-N C=CCC(C(N(C[C@@H](C1)OC(N2CCCCC2)=O)C1C(NC(CCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)NC(OC1CCCCC1)=O Chemical compound C=CCC(C(N(C[C@@H](C1)OC(N2CCCCC2)=O)C1C(NC(CCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)NC(OC1CCCCC1)=O DDPOIFYOZBCVPM-KZJMBQCBSA-N 0.000 description 1
- XHCRBJKBMAINCU-CNDJQURISA-N C=CCCC(C(N(C[C@@H](C1)S(c2ccccc2)(=O)=O)[C@@H]1C(NC(CCCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)NC(OCc1ccccc1)=O Chemical compound C=CCCC(C(N(C[C@@H](C1)S(c2ccccc2)(=O)=O)[C@@H]1C(NC(CCCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)NC(OCc1ccccc1)=O XHCRBJKBMAINCU-CNDJQURISA-N 0.000 description 1
- USXIOSJJPVTWNZ-RCSIZABNSA-N CC(C(c1nc(cccc2)c2[o]1)=O)N/C(/C(C[C@H](C1)OCc(cc2)ccc2Cl)N1C(C(CCC1CCNCC1)NS(C)(=O)=O)=O)=[O]\C1CC(CN)CCC1 Chemical compound CC(C(c1nc(cccc2)c2[o]1)=O)N/C(/C(C[C@H](C1)OCc(cc2)ccc2Cl)N1C(C(CCC1CCNCC1)NS(C)(=O)=O)=O)=[O]\C1CC(CN)CCC1 USXIOSJJPVTWNZ-RCSIZABNSA-N 0.000 description 1
- CGCYJOLDPRJMEK-XJEQWAIASA-N CC(C(c1nc(cccc2)c2[o]1)=O)N/C(/[C@H](C[C@H](C1)OCc(cc2)ccc2Cl)N1C(C(CCCC1CCNCC1)NS(C)(=O)=O)=O)=[O]\c1cccc(CC(N)=N)c1 Chemical compound CC(C(c1nc(cccc2)c2[o]1)=O)N/C(/[C@H](C[C@H](C1)OCc(cc2)ccc2Cl)N1C(C(CCCC1CCNCC1)NS(C)(=O)=O)=O)=[O]\c1cccc(CC(N)=N)c1 CGCYJOLDPRJMEK-XJEQWAIASA-N 0.000 description 1
- DKEUBNDABDGERQ-XKTLMJIBSA-N CC([O]=S(C)(NCC(N(C[C@@H](C1)OC(N2CCCCC2)=O)C1C(NC(CCCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)=O)=C Chemical compound CC([O]=S(C)(NCC(N(C[C@@H](C1)OC(N2CCCCC2)=O)C1C(NC(CCCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)=O)=C DKEUBNDABDGERQ-XKTLMJIBSA-N 0.000 description 1
- GASCCANNURVZOH-UHFFFAOYSA-N CCCC(c1nc(cccc2)c2[o]1)=O Chemical compound CCCC(c1nc(cccc2)c2[o]1)=O GASCCANNURVZOH-UHFFFAOYSA-N 0.000 description 1
- RQGBFVLTFYRYKB-UHFFFAOYSA-N CCCC1CCNCC1 Chemical compound CCCC1CCNCC1 RQGBFVLTFYRYKB-UHFFFAOYSA-N 0.000 description 1
- ZVQJTTSXQNDKSM-DNMOBYMISA-N CCc1c(C)cccc1/[O]=C(\NCC(N(C[C@@H](C1)OC(N2CCCCC2)=O)C1C(NC(CCCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)/OCc1ccccc1 Chemical compound CCc1c(C)cccc1/[O]=C(\NCC(N(C[C@@H](C1)OC(N2CCCCC2)=O)C1C(NC(CCCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)/OCc1ccccc1 ZVQJTTSXQNDKSM-DNMOBYMISA-N 0.000 description 1
- YYBRVWPFCYHBBX-FANMGANHSA-N CN(Cc1ccc[o]1)C(O[C@H](CC1C(NC(CCCCCN)C(c2nc(cccc3)c3[o]2)=O)=O)CN1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O Chemical compound CN(Cc1ccc[o]1)C(O[C@H](CC1C(NC(CCCCCN)C(c2nc(cccc3)c3[o]2)=O)=O)CN1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O YYBRVWPFCYHBBX-FANMGANHSA-N 0.000 description 1
- YGQVCHVMZWARBD-OAIBZVRLSA-N CN(Cc1ccccc1)C(O[C@H](C[C@H]1C(NC(CCCCCN)C(c2nc(cccc3)c3[o]2)=O)=O)CN1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O Chemical compound CN(Cc1ccccc1)C(O[C@H](C[C@H]1C(NC(CCCCCN)C(c2nc(cccc3)c3[o]2)=O)=O)CN1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O YGQVCHVMZWARBD-OAIBZVRLSA-N 0.000 description 1
- ZKHCRRMIJZFPMK-MNALTYRASA-N CNCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC([C@H](C[C@H](C1)OCc(cc2)ccc2Cl)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O Chemical compound CNCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC([C@H](C[C@H](C1)OCc(cc2)ccc2Cl)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O ZKHCRRMIJZFPMK-MNALTYRASA-N 0.000 description 1
- BXKYJYBEBUKGED-GQOAJTFNSA-N CS(NC(CC=C1CCNCC1)C(N(C[C@@H](C1)OCc(cc2)ccc2Cl)C1C(NC(CCCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)(=O)=O Chemical compound CS(NC(CC=C1CCNCC1)C(N(C[C@@H](C1)OCc(cc2)ccc2Cl)C1C(NC(CCCCCN)C(c1nc(cccc2)c2[o]1)=O)=O)=O)(=O)=O BXKYJYBEBUKGED-GQOAJTFNSA-N 0.000 description 1
- KXFSOKNQYXBONA-LENVRHPRSA-N CS(NC(CCCC1CCNCC1)C(N(C[C@@H](C1)OCc(cc2)ccc2Cl)[C@@H]1C(NC(CCCCNC(N)=N)C(c1nc(cccc2)c2[s]1)=O)=O)=O)(=O)=O Chemical compound CS(NC(CCCC1CCNCC1)C(N(C[C@@H](C1)OCc(cc2)ccc2Cl)[C@@H]1C(NC(CCCCNC(N)=N)C(c1nc(cccc2)c2[s]1)=O)=O)=O)(=O)=O KXFSOKNQYXBONA-LENVRHPRSA-N 0.000 description 1
- HCEWSIPFNJYYPZ-NEPJUHHUSA-N CS(NCC(N(C[C@@H](C1)OC(N2CCCCC2)=O)[C@@H]1C(N=C)=O)=O)(=O)=O Chemical compound CS(NCC(N(C[C@@H](C1)OC(N2CCCCC2)=O)[C@@H]1C(N=C)=O)=O)(=O)=O HCEWSIPFNJYYPZ-NEPJUHHUSA-N 0.000 description 1
- BXYSRSGRKSJAHT-DUSLRRAJSA-N CSNCC(N(C[C@@H](C1)OCc(cc2)ccc2Cl)C1C(NCC(c1nc(cccc2)c2[o]1)=O)=O)=O Chemical compound CSNCC(N(C[C@@H](C1)OCc(cc2)ccc2Cl)C1C(NCC(c1nc(cccc2)c2[o]1)=O)=O)=O BXYSRSGRKSJAHT-DUSLRRAJSA-N 0.000 description 1
- WTJDXTOPDBNOIX-OKCGTBKXSA-N NC(N1CCC(CCC(C(c2nc(cccc3)c3[o]2)=O)NC(C(C[C@H](C2)OCc(cc3)ccc3Cl)N2C(C(CCc2ccccc2)NC(OCc2ccccc2)=O)=O)=O)CC1)=N Chemical compound NC(N1CCC(CCC(C(c2nc(cccc3)c3[o]2)=O)NC(C(C[C@H](C2)OCc(cc3)ccc3Cl)N2C(C(CCc2ccccc2)NC(OCc2ccccc2)=O)=O)=O)CC1)=N WTJDXTOPDBNOIX-OKCGTBKXSA-N 0.000 description 1
- WLHGVVOFXOKICF-MZIRRMNXSA-N NC(NCCC[C@@H](C(c1nc(cccc2)c2[s]1)=O)NC(C(C(CC1)c2ccccc2)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O)=N Chemical compound NC(NCCC[C@@H](C(c1nc(cccc2)c2[s]1)=O)NC(C(C(CC1)c2ccccc2)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O)=N WLHGVVOFXOKICF-MZIRRMNXSA-N 0.000 description 1
- PAFZNILMFXTMIY-UHFFFAOYSA-N NC1CCCCC1 Chemical compound NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 description 1
- PLZSKNQFCUWQNS-UAFRDEPYSA-N NCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OC/C=C/c(cc2)ccc2Cl)N1C(C(CCc1ccccc1)NC(OCC1CC1)=O)=O)=O Chemical compound NCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OC/C=C/c(cc2)ccc2Cl)N1C(C(CCc1ccccc1)NC(OCC1CC1)=O)=O)=O PLZSKNQFCUWQNS-UAFRDEPYSA-N 0.000 description 1
- SYXRGJLSNPCDTB-OCIIISRYSA-N NCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC([C@H](C[C@H](C1)OCc2ccccc2)N1C(C(CCc1ccccc1)NC(OC1CCCC1)=O)=O)=O Chemical compound NCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC([C@H](C[C@H](C1)OCc2ccccc2)N1C(C(CCc1ccccc1)NC(OC1CCCC1)=O)=O)=O SYXRGJLSNPCDTB-OCIIISRYSA-N 0.000 description 1
- JVHMSFUPMPJJDJ-PMIDXUABSA-N NCCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OC(N(CC2)CCC2=O)=O)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O Chemical compound NCCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OC(N(CC2)CCC2=O)=O)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O JVHMSFUPMPJJDJ-PMIDXUABSA-N 0.000 description 1
- QVXRUEDECIPEPT-FRCSALDRSA-N NCCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OC(N2CCCC2)=O)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O Chemical compound NCCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OC(N2CCCC2)=O)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O QVXRUEDECIPEPT-FRCSALDRSA-N 0.000 description 1
- SLHKZEKYFLLIBQ-VFNLOOTOSA-N NCCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OCC2CCCCC2)N1C([C@@H](Cc1cccc(Cl)c1)NC(OCC1CCCC1)=O)=O)=O Chemical compound NCCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OCC2CCCCC2)N1C([C@@H](Cc1cccc(Cl)c1)NC(OCC1CCCC1)=O)=O)=O SLHKZEKYFLLIBQ-VFNLOOTOSA-N 0.000 description 1
- KSLYZZXFVOGINR-PLPAUJIISA-N NCCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OCc(cc2)ccc2Cl)N1C(C(C/C=C/c1ccccc1)NC(OC1CCCCC1)=O)=O)=O Chemical compound NCCCCCC(C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OCc(cc2)ccc2Cl)N1C(C(C/C=C/c1ccccc1)NC(OC1CCCCC1)=O)=O)=O KSLYZZXFVOGINR-PLPAUJIISA-N 0.000 description 1
- IZQRODCCJRDVHF-OAIBZVRLSA-N NCCCCCC(C(c1nc(cccc2)c2[s]1)=O)NC([C@H](C[C@H](C1)OCc2ccccc2)N1C(C(CCCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O Chemical compound NCCCCCC(C(c1nc(cccc2)c2[s]1)=O)NC([C@H](C[C@H](C1)OCc2ccccc2)N1C(C(CCCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O IZQRODCCJRDVHF-OAIBZVRLSA-N 0.000 description 1
- LYRALOYTFFZGKR-KVEONSQOSA-N NCCCC[C@@H](C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OC(N(CC2)CCC2c2ccccc2)=O)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O Chemical compound NCCCC[C@@H](C(c1nc(cccc2)c2[o]1)=O)NC(C(C[C@H](C1)OC(N(CC2)CCC2c2ccccc2)=O)N1C(C(CCc1ccccc1)NC(OCc1ccccc1)=O)=O)=O LYRALOYTFFZGKR-KVEONSQOSA-N 0.000 description 1
- OEAJFPUFTFTUPA-UHFFFAOYSA-N O=C(CNC(C(CCC1)N1C(CNS=O)=O)=O)c1nc(cccc2)c2[o]1 Chemical compound O=C(CNC(C(CCC1)N1C(CNS=O)=O)=O)c1nc(cccc2)c2[o]1 OEAJFPUFTFTUPA-UHFFFAOYSA-N 0.000 description 1
- UHOVQNZJYSORNB-UHFFFAOYSA-N c1ccccc1 Chemical compound c1ccccc1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- 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
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80298306P | 2006-05-23 | 2006-05-23 | |
| US60/802,983 | 2006-05-23 | ||
| US86060406P | 2006-11-22 | 2006-11-22 | |
| US60/860,604 | 2006-11-22 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2008150615A RU2008150615A (ru) | 2010-06-27 |
| RU2419626C2 true RU2419626C2 (ru) | 2011-05-27 |
Family
ID=38565503
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008150615/04A RU2419626C2 (ru) | 2006-05-23 | 2007-05-16 | Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US7951823B2 (enExample) |
| EP (1) | EP2027143A2 (enExample) |
| JP (1) | JP2009538327A (enExample) |
| KR (1) | KR101069051B1 (enExample) |
| AR (1) | AR061109A1 (enExample) |
| AU (1) | AU2007253819B2 (enExample) |
| BR (1) | BRPI0712021A2 (enExample) |
| CA (1) | CA2651762A1 (enExample) |
| CL (1) | CL2007001481A1 (enExample) |
| MX (1) | MX2008014839A (enExample) |
| PE (1) | PE20080708A1 (enExample) |
| RU (1) | RU2419626C2 (enExample) |
| TW (1) | TW200813094A (enExample) |
| WO (1) | WO2007137080A2 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10676470B2 (en) | 2014-10-06 | 2020-06-09 | Cortexyme, Inc. | Inhibitors of lysine gingipain |
| US10730826B2 (en) | 2016-09-16 | 2020-08-04 | Cortexyme, Inc. | Ketone inhibitors of lysine gingipain |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0507577D0 (en) * | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| EP2019837B1 (en) * | 2006-05-23 | 2011-03-23 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| EP2027143A2 (en) * | 2006-05-23 | 2009-02-25 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| CA2677485A1 (en) * | 2007-02-09 | 2008-08-14 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| CA2677487A1 (en) | 2007-02-09 | 2008-08-14 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| IE20070935A1 (en) * | 2007-12-21 | 2009-06-24 | Trinity College Dublin | Guanidine based compounds and their use in the treatment of mental and neurological disorders. |
| MX2011011094A (es) * | 2009-04-20 | 2011-11-04 | Hoffmann La Roche | Derivados de prolina como inhibidores de catepsina. |
| JP2013518897A (ja) * | 2010-02-03 | 2013-05-23 | エムイーエイチ アソシエイツ，インコーポレイテッド | 選択的および生体活性的等配電子体としての多重置換フルオロメタン |
| MX2014006211A (es) * | 2011-11-25 | 2014-08-08 | Hoffmann La Roche | Nuevos derivados de pirrolidina como inhibidores de catepsina. |
| CN105001131A (zh) * | 2015-07-31 | 2015-10-28 | 吉尔生化（上海）有限公司 | 一种医药中间体nα-z-s-苄基-l-半胱氨酸-4-硝基苯酯的合成方法 |
| EP3374352A4 (en) | 2015-11-09 | 2019-10-02 | Cortexyme, Inc. | GINGIPAINE ARGININE INHIBITORS |
| CN110483437B (zh) * | 2018-05-14 | 2022-12-06 | 嘉兴维眸生物科技有限公司 | 一种含五元环的化合物及其制备和应用 |
| AU2020349353A1 (en) | 2019-09-17 | 2022-04-14 | Duke University | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| HUE064089T2 (hu) | 2020-04-16 | 2024-02-28 | Mereo Biopharma 4 Ltd | Alvelesztat neutrofil elasztáz inhibitort alkalmazó módszerek alfa-1-antitripszin hiány által közvetített légzõszervi megbetegedés kezelésére |
| AU2022373971A1 (en) | 2021-10-20 | 2024-04-04 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0291234A2 (en) * | 1987-05-11 | 1988-11-17 | Zeneca Inc. | Peptidic human leukocyte elastase (HLE) inhibitors |
| WO2000044733A1 (en) * | 1999-01-27 | 2000-08-03 | Ortho-Mcneil Pharmaceutical, Inc. | Peptidyl heterocyclic ketones useful as tryptase inhibitors |
| RU2181125C2 (ru) * | 1995-06-07 | 2002-04-10 | Орто Фармасьютикал Корпорейшн | Пептидильные гетероциклы, используемые при лечении тромбинассоциированных заболеваний |
| WO2005023804A1 (en) * | 2003-08-05 | 2005-03-17 | Janssen Pharmaceutica, N.V. | Peptidyl heterocyclic ketone derivatives and preparation processes |
Family Cites Families (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5672582A (en) | 1993-04-30 | 1997-09-30 | Merck & Co., Inc. | Thrombin inhibitors |
| US5726159A (en) | 1994-03-04 | 1998-03-10 | Eli Lilly And Company | Antithrombotic agents |
| ZA951617B (en) | 1994-03-04 | 1997-02-27 | Lilly Co Eli | Antithrombotic agents. |
| US5707966A (en) | 1994-03-04 | 1998-01-13 | Eli Lilly And Company | Antithrombotic agents |
| ZA951618B (en) | 1994-03-04 | 1996-08-27 | Lilly Co Eli | Antithrombotic agents |
| US5705487A (en) | 1994-03-04 | 1998-01-06 | Eli Lilly And Company | Antithrombotic agents |
| KR100347285B1 (ko) | 1994-06-02 | 2003-01-15 | 아벤티스 파마슈티칼스 인크. | 신규의엘라스타제저해제 |
| JPH0820597A (ja) | 1994-07-07 | 1996-01-23 | Meiji Seika Kaisha Ltd | トロンビン阻害作用を有する複素環カルボニル化合物 |
| US5618792A (en) | 1994-11-21 | 1997-04-08 | Cortech, Inc. | Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase |
| US5710130A (en) | 1995-02-27 | 1998-01-20 | Eli Lilly And Company | Antithrombotic agents |
| US5914319A (en) | 1995-02-27 | 1999-06-22 | Eli Lilly And Company | Antithrombotic agents |
| CA2176414A1 (en) | 1995-05-18 | 1996-11-19 | S. David Kimball | Acyl guanidine and amidine prodrugs |
| US6211154B1 (en) | 1995-06-07 | 2001-04-03 | Cor Therapeutics, Inc. | Ketoheterocyclic inhibitors of factor Xa |
| US6069130A (en) | 1995-06-07 | 2000-05-30 | Cor Therapeutics, Inc. | Ketoheterocyclic inhibitors of factor Xa |
| US5827866A (en) | 1995-06-07 | 1998-10-27 | Ortho Pharmaceutical Corporation | Peptidyl heterocycles useful in the treatment of thrombin related disorders |
| US5827860A (en) | 1995-06-07 | 1998-10-27 | Ortho Pharmaceutical Corporation | Peptidyl heterocycles useful in the treatment of thrombin related disorders |
| US6022861A (en) | 1995-06-07 | 2000-02-08 | Cor Therapeutics, Inc. | Ketoheterocyclic inhibitors of factor Xa |
| IL119466A (en) | 1995-11-03 | 2001-08-26 | Akzo Nobel Nv | Thrombin inhibitors, their preparation and pharmaceutical compositions containing them |
| TW523513B (en) | 1996-03-01 | 2003-03-11 | Akzo Nobel Nv | Serine protease inhibitors |
| CA2253835A1 (en) | 1996-06-18 | 1997-12-24 | Kent Alan Berryman | Process for the preparation of chiral keto-heterocycles of basic amino acids |
| IL121474A0 (en) | 1996-08-23 | 1998-02-08 | Akzo Nobel Nv | Thrombin inhibitors |
| NZ335276A (en) | 1996-10-18 | 2000-09-29 | Vertex Pharma | Inhibitors of serine proteases, particularly hepatitis C virus (HCV) NS3 (Non Structural Protein 3) protease |
| TR199901681T2 (xx) | 1996-12-06 | 2000-03-21 | Cortech, Inc. | Serin proteas inhibit�rleri. |
| US6004933A (en) | 1997-04-25 | 1999-12-21 | Cortech Inc. | Cysteine protease inhibitors |
| TR199902692T2 (xx) | 1997-05-02 | 2000-07-21 | Akzo Nobel N.V. | Serin proteaz inhibit�rleri. |
| PT1012180E (pt) | 1997-08-11 | 2005-04-29 | Boehringer Ingelheim Ca Ltd | Analogos de peptidos inibidores da hepatite c |
| US6323219B1 (en) | 1998-04-02 | 2001-11-27 | Ortho-Mcneil Pharmaceutical, Inc. | Methods for treating immunomediated inflammatory disorders |
| EP1114822A3 (en) | 1998-06-03 | 2002-11-13 | Cortech Inc. | Indoles and tetrahydroisoquinolines containing alpha-keto oxadiazoles as serine protease inhibitors |
| AR022061A1 (es) | 1998-08-10 | 2002-09-04 | Boehringer Ingelheim Ca Ltd | Peptidos inhibidores de la hepatitis c, una composicion farmaceutica que los contiene, el uso de los mismos para preparar una composicion farmaceutica, el uso de un producto intermedio para la preparacion de estos peptidos y un procedimiento para la preparacion de un peptido analogo de los mismos. |
| US6323180B1 (en) | 1998-08-10 | 2001-11-27 | Boehringer Ingelheim (Canada) Ltd | Hepatitis C inhibitor tri-peptides |
| US6242422B1 (en) | 1998-10-22 | 2001-06-05 | Idun Pharmacueticals, Inc. | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
| KR20000047461A (ko) | 1998-12-29 | 2000-07-25 | 성재갑 | 트롬빈 억제제 |
| JP2000256396A (ja) * | 1999-03-03 | 2000-09-19 | Dainippon Pharmaceut Co Ltd | 複素環式化合物およびその中間体ならびにエラスターゼ阻害剤 |
| GB9929552D0 (en) | 1999-12-14 | 2000-02-09 | Proteus Molecular Design | Compounds |
| WO2001002424A2 (en) | 1999-07-07 | 2001-01-11 | Du Pont Pharmaceuticals Company | Peptide boronic acid inhibitors of hepatitis c virus protease |
| GB9923710D0 (en) | 1999-10-08 | 1999-12-08 | Proteus Molecular Design | Chemical compounds |
| AU2055301A (en) | 1999-12-03 | 2001-06-12 | Bristol-Myers Squibb Pharma Company | Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease |
| US7012066B2 (en) | 2000-07-21 | 2006-03-14 | Schering Corporation | Peptides as NS3-serine protease inhibitors of hepatitis C virus |
| US7244721B2 (en) | 2000-07-21 | 2007-07-17 | Schering Corporation | Peptides as NS3-serine protease inhibitors of hepatitis C virus |
| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| EP1363898A4 (en) | 2001-03-02 | 2004-12-08 | Bristol Myers Squibb Co | COMPOUNDS SUITABLE AS MODULATORS OF MELANOCORTIN RECEPTORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
| KR100926244B1 (ko) | 2001-07-11 | 2009-11-12 | 버텍스 파마슈티칼스 인코포레이티드 | 브릿지된 바이사이클릭 세린 프로테아제 억제제 |
| WO2003013571A1 (en) | 2001-08-10 | 2003-02-20 | Palatin Technologies, Inc. | Peptidomimetics of biologically active metallopeptides |
| EP1480999A2 (en) | 2002-02-08 | 2004-12-01 | Idun Pharmaceuticals | (substituted)acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
| US7019019B2 (en) | 2002-12-23 | 2006-03-28 | Dendreon Corporation | Matriptase inhibitors and methods of use |
| MY148123A (en) | 2003-09-05 | 2013-02-28 | Vertex Pharma | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
| NZ546663A (en) | 2003-10-10 | 2010-01-29 | Vertex Pharma | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| KR20060118532A (ko) | 2003-12-11 | 2006-11-23 | 쉐링 코포레이션 | Ｃ형 간염 바이러스 ｎｓ３／ｎｓ４ａ 세린 프로테아제의억제제 |
| US20050222383A1 (en) | 2004-02-05 | 2005-10-06 | Irm Llc | Prostasin substrates and inhibitors |
| RU2006134005A (ru) | 2004-02-27 | 2008-04-10 | Шеринг Корпорейшн (US) | Новые соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с |
| EP1727811B1 (en) | 2004-03-24 | 2014-11-12 | Shire Orphan Therapies GmbH | New compounds for the inhibition of angiogenesis and use of thereof |
| CN1984922A (zh) | 2004-05-20 | 2007-06-20 | 先灵公司 | 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的取代脯氨酸 |
| WO2006006644A1 (ja) | 2004-07-14 | 2006-01-19 | Kyowa Hakko Kogyo Co., Ltd. | 複素環式化合物 |
| GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| US20060275366A1 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Controlled-release formulation |
| EP2019837B1 (en) | 2006-05-23 | 2011-03-23 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| EP2027143A2 (en) * | 2006-05-23 | 2009-02-25 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| AU2007342223B2 (en) | 2007-01-10 | 2011-02-24 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| CA2677487A1 (en) | 2007-02-09 | 2008-08-14 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| CA2677485A1 (en) | 2007-02-09 | 2008-08-14 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
-
2007
- 2007-05-16 EP EP07783835A patent/EP2027143A2/en not_active Withdrawn
- 2007-05-16 AU AU2007253819A patent/AU2007253819B2/en not_active Ceased
- 2007-05-16 KR KR1020087031129A patent/KR101069051B1/ko not_active Expired - Fee Related
- 2007-05-16 MX MX2008014839A patent/MX2008014839A/es active IP Right Grant
- 2007-05-16 RU RU2008150615/04A patent/RU2419626C2/ru not_active IP Right Cessation
- 2007-05-16 BR BRPI0712021-4A patent/BRPI0712021A2/pt not_active IP Right Cessation
- 2007-05-16 JP JP2009512222A patent/JP2009538327A/ja active Pending
- 2007-05-16 WO PCT/US2007/069059 patent/WO2007137080A2/en not_active Ceased
- 2007-05-16 US US11/749,430 patent/US7951823B2/en not_active Expired - Fee Related
- 2007-05-16 CA CA002651762A patent/CA2651762A1/en not_active Abandoned
- 2007-05-23 PE PE2007000642A patent/PE20080708A1/es not_active Application Discontinuation
- 2007-05-23 CL CL200701481A patent/CL2007001481A1/es unknown
- 2007-05-23 AR ARP070102231A patent/AR061109A1/es not_active Application Discontinuation
- 2007-05-23 TW TW096118422A patent/TW200813094A/zh unknown
-
2011
- 2011-04-19 US US13/089,973 patent/US8338469B2/en not_active Expired - Fee Related
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0291234A2 (en) * | 1987-05-11 | 1988-11-17 | Zeneca Inc. | Peptidic human leukocyte elastase (HLE) inhibitors |
| RU2181125C2 (ru) * | 1995-06-07 | 2002-04-10 | Орто Фармасьютикал Корпорейшн | Пептидильные гетероциклы, используемые при лечении тромбинассоциированных заболеваний |
| WO2000044733A1 (en) * | 1999-01-27 | 2000-08-03 | Ortho-Mcneil Pharmaceutical, Inc. | Peptidyl heterocyclic ketones useful as tryptase inhibitors |
| WO2005023804A1 (en) * | 2003-08-05 | 2005-03-17 | Janssen Pharmaceutica, N.V. | Peptidyl heterocyclic ketone derivatives and preparation processes |
Non-Patent Citations (1)
| Title |
|---|
| COSTANZO M J ET AL: "Potent, Small-Molecule Inhibitors of Human Mast Cell Tryptase. Antiasthmatic Action of a Dipeptide-Based Transition-State Analogue Containing a Benzothiazole Ketone" JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY 2003, vol.46, pages 3865-3876. COSTANZO M J ET AL: "In-Depth Study of Tripeptide-Based alpha-Ketoheterocycles as Inhibitors of Thrombin. Effective Utilization of the S1' Subsite and Its Implications to Structure-Based Drug Design" JOURNAL OF MEDICINAL CHEMISTRY, 2005, vol.48 pages 1984-2008. * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10676470B2 (en) | 2014-10-06 | 2020-06-09 | Cortexyme, Inc. | Inhibitors of lysine gingipain |
| RU2728785C2 (ru) * | 2014-10-06 | 2020-07-31 | Кортексим, Инк. | Ингибиторы лизинспецифичного гингипаина |
| US11332464B2 (en) | 2014-10-06 | 2022-05-17 | Cortexyme, Inc. | Inhibitors of lysine gingipain |
| US10730826B2 (en) | 2016-09-16 | 2020-08-04 | Cortexyme, Inc. | Ketone inhibitors of lysine gingipain |
| US11325884B2 (en) | 2016-09-16 | 2022-05-10 | Cortexyme, Inc. | Ketone inhibitors of lysine gingipain |
| US12110263B2 (en) | 2016-09-16 | 2024-10-08 | Lighthouse Pharmaceuticals, Inc. | Ketone inhibitors of lysine gingipain |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20090014217A (ko) | 2009-02-06 |
| US20070275906A1 (en) | 2007-11-29 |
| US7951823B2 (en) | 2011-05-31 |
| WO2007137080A3 (en) | 2008-01-24 |
| AR061109A1 (es) | 2008-08-06 |
| US20110257077A1 (en) | 2011-10-20 |
| CL2007001481A1 (es) | 2008-05-09 |
| AU2007253819B2 (en) | 2011-02-17 |
| KR101069051B1 (ko) | 2011-09-29 |
| WO2007137080A2 (en) | 2007-11-29 |
| MX2008014839A (es) | 2008-12-05 |
| RU2008150615A (ru) | 2010-06-27 |
| US8338469B2 (en) | 2012-12-25 |
| PE20080708A1 (es) | 2008-07-30 |
| EP2027143A2 (en) | 2009-02-25 |
| TW200813094A (en) | 2008-03-16 |
| AU2007253819A1 (en) | 2007-11-29 |
| BRPI0712021A2 (pt) | 2012-01-03 |
| CA2651762A1 (en) | 2007-11-29 |
| JP2009538327A (ja) | 2009-11-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2413727C2 (ru) | Производные пиразола и их применение в качестве ингибиторов рецепторных тирозинкиназ | |
| RU2483072C2 (ru) | Производные фосфоновой кислоты и их применение в качестве антагонистов рецептора p2y12 | |
| RU2401260C2 (ru) | Пиримидиновые производные | |
| RU2447060C2 (ru) | Ингибиторы сфингозинкиназы | |
| RU2468029C2 (ru) | Ингибиторы hcv ns3 протеазы | |
| JP2016509591A5 (enExample) | ||
| RU2454411C2 (ru) | Производные хинолина | |
| AR128079A1 (es) | Composición farmacéutica que comprende un compuesto de quinazolina | |
| SI2961736T1 (en) | Histone demethylase inhibitors | |
| RU2436776C2 (ru) | ДИАРИЛАМИН-СОДЕРЖАЩИЕ СОЕДИНЕНИЯ, КОМПОЗИЦИИ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРОВ с-КIT | |
| JP2016505536A5 (enExample) | ||
| RU2018137389A (ru) | Гетероциклические амиды, полезные в качестве модуляторов | |
| EA201991684A1 (ru) | Аналоги атазанавира (atv) для лечения вич-инфекций | |
| RU2003110577A (ru) | Гетероциклические соединения, связывающиеся с хемокиновыми рецепторами | |
| EA200900358A1 (ru) | Энантиомерно чистые фосфоиндолы в качестве ингибиторов hiv | |
| JP2020500182A5 (enExample) | ||
| JP2010531345A5 (enExample) | ||
| RU2007139453A (ru) | Гетеробициклические ингибиторы вируса гепатита с (hcv) | |
| JP2017518959A5 (enExample) | ||
| CS244670B2 (en) | Production method of aryloxypropanolamines | |
| RU2011100786A (ru) | Производные имидазопиридина в качестве ингибиторов рецепторных тирозинкиназ | |
| EA202191250A1 (ru) | Смеси и композиции, включающие 5-фтор-4-имино-3-метил-1-тозил-3,4-дигидропиримидин-2-он, и способы их применения | |
| RU2015109706A (ru) | Новые производные азабензимидазол гексагидрофуро[3, 2-в]фурана | |
| NZ590355A (en) | Stat3 inhibitor containing quinolinecarboxamide derivative as active ingredient | |
| RU2008150613A (ru) | Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20130517 |