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
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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
- A61K31/41—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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- 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
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- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- 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]
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- Chemical & Material Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
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- 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)
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- Ophthalmology & Optometry (AREA)
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- 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)
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| 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 |
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| RU2008150615A RU2008150615A (ru) | 2010-06-27 |
| RU2419626C2 true RU2419626C2 (ru) | 2011-05-27 |
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| 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) |
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| 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 |
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| GB0507577D0 (en) * | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| WO2007140117A1 (en) * | 2006-05-23 | 2007-12-06 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| US7951823B2 (en) * | 2006-05-23 | 2011-05-31 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| CN101600428A (zh) * | 2007-02-09 | 2009-12-09 | Irm责任有限公司 | 作为通道活化蛋白酶抑制剂的化合物和组合物 |
| CA2677485A1 (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. |
| PL2421826T3 (pl) * | 2009-04-20 | 2014-03-31 | Hoffmann La Roche | Pochodne proliny jako inhibitory katepsyn |
| CA2826623A1 (en) * | 2010-02-03 | 2011-08-11 | Meh Associates, Inc | Multiple substituted fluoromethanes as selective and bioactive isosteres |
| 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 |
| CA3004095A1 (en) | 2015-11-09 | 2017-05-18 | Cortexyme, Inc. | Inhibitors of arginine gingipain |
| 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 |
| CA3154761A1 (en) | 2019-09-17 | 2021-03-25 | Mereo Biopharma 4 Limited | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| SI4106757T1 (sl) | 2020-04-16 | 2023-11-30 | Mereo Biopharma 4 Limited | Postopki, ki vključujejo zaviralec nevtrofilne elastaze alvelestat, za zdravljenje bolezni dihal, ki jo sproži pomanjkanje antitripsina alfa-1 |
| WO2023067103A1 (en) | 2021-10-20 | 2023-04-27 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
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| DK2104535T3 (da) | 2007-01-10 | 2011-04-04 | Irm Llc | Forbindelser og sammensætninger som kanalaktiverende proteaseinhibitorer |
| CN101600428A (zh) | 2007-02-09 | 2009-12-09 | Irm责任有限公司 | 作为通道活化蛋白酶抑制剂的化合物和组合物 |
| CA2677485A1 (en) | 2007-02-09 | 2008-08-14 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
-
2007
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- 2007-05-16 CA CA002651762A patent/CA2651762A1/en not_active Abandoned
- 2007-05-16 EP EP07783835A patent/EP2027143A2/en not_active Withdrawn
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- 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 WO PCT/US2007/069059 patent/WO2007137080A2/en not_active Ceased
- 2007-05-16 MX MX2008014839A patent/MX2008014839A/es active IP Right Grant
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- 2007-05-23 AR ARP070102231A patent/AR061109A1/es not_active Application Discontinuation
- 2007-05-23 CL CL200701481A patent/CL2007001481A1/es unknown
- 2007-05-23 TW TW096118422A patent/TW200813094A/zh unknown
- 2007-05-23 PE PE2007000642A patent/PE20080708A1/es not_active Application Discontinuation
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2011
- 2011-04-19 US US13/089,973 patent/US8338469B2/en not_active Expired - Fee Related
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| 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 |
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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 |
|---|---|
| TW200813094A (en) | 2008-03-16 |
| KR20090014217A (ko) | 2009-02-06 |
| KR101069051B1 (ko) | 2011-09-29 |
| US8338469B2 (en) | 2012-12-25 |
| JP2009538327A (ja) | 2009-11-05 |
| EP2027143A2 (en) | 2009-02-25 |
| AU2007253819A1 (en) | 2007-11-29 |
| CL2007001481A1 (es) | 2008-05-09 |
| CA2651762A1 (en) | 2007-11-29 |
| US20070275906A1 (en) | 2007-11-29 |
| BRPI0712021A2 (pt) | 2012-01-03 |
| WO2007137080A3 (en) | 2008-01-24 |
| US20110257077A1 (en) | 2011-10-20 |
| US7951823B2 (en) | 2011-05-31 |
| AR061109A1 (es) | 2008-08-06 |
| MX2008014839A (es) | 2008-12-05 |
| PE20080708A1 (es) | 2008-07-30 |
| WO2007137080A2 (en) | 2007-11-29 |
| AU2007253819B2 (en) | 2011-02-17 |
| RU2008150615A (ru) | 2010-06-27 |
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