AP1019A - Inhibitors of serinre proteases, particularly hepatitis C virus NS3 protease. - Google Patents
Inhibitors of serinre proteases, particularly hepatitis C virus NS3 protease. Download PDFInfo
- Publication number
- AP1019A AP1019A APAP/P/1999/001512A AP9901512A AP1019A AP 1019 A AP1019 A AP 1019A AP 9901512 A AP9901512 A AP 9901512A AP 1019 A AP1019 A AP 1019A
- Authority
- AP
- ARIPO
- Prior art keywords
- virus
- hepatitis
- protease
- hcv
- inhibitors
- Prior art date
Links
- 102000035195 Peptidases Human genes 0.000 title abstract description 9
- 108091005804 Peptidases Proteins 0.000 title abstract description 9
- 239000004365 Protease Substances 0.000 title abstract description 7
- 239000003112 inhibitor Substances 0.000 title description 7
- 108700012707 hepatitis C virus NS3 Proteins 0.000 title description 4
- -1 aiyl Chemical group 0.000 abstract description 20
- 150000001875 compounds Chemical class 0.000 abstract description 12
- 125000000753 cycloalkyl group Chemical group 0.000 abstract description 9
- 125000001072 heteroaryl group Chemical group 0.000 abstract description 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract description 5
- 101800001838 Serine protease/helicase NS3 Proteins 0.000 abstract description 4
- 125000000217 alkyl group Chemical group 0.000 abstract description 4
- 230000002401 inhibitory effect Effects 0.000 abstract description 4
- 125000003342 alkenyl group Chemical group 0.000 abstract description 2
- 125000000304 alkynyl group Chemical group 0.000 abstract description 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 description 14
- 241000711549 Hepacivirus C Species 0.000 description 12
- 102000012479 Serine Proteases Human genes 0.000 description 9
- 108010022999 Serine Proteases Proteins 0.000 description 9
- 125000003118 aryl group Chemical group 0.000 description 8
- 238000000034 method Methods 0.000 description 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 5
- 239000003443 antiviral agent Substances 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 5
- 238000003776 cleavage reaction Methods 0.000 description 5
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 208000006454 hepatitis Diseases 0.000 description 5
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 5
- 150000003254 radicals Chemical class 0.000 description 5
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 4
- 108010076039 Polyproteins Proteins 0.000 description 4
- 229910052799 carbon Inorganic materials 0.000 description 4
- 230000007017 scission Effects 0.000 description 4
- 239000003001 serine protease inhibitor Substances 0.000 description 4
- 238000002560 therapeutic procedure Methods 0.000 description 4
- 230000003612 virological effect Effects 0.000 description 4
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- 208000005176 Hepatitis C Diseases 0.000 description 3
- 102000014150 Interferons Human genes 0.000 description 3
- 108010050904 Interferons Proteins 0.000 description 3
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
- 231100000283 hepatitis Toxicity 0.000 description 3
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 3
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 3
- 229940079322 interferon Drugs 0.000 description 3
- 229940047124 interferons Drugs 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 235000019419 proteases Nutrition 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 108090000623 proteins and genes Proteins 0.000 description 3
- 238000012552 review Methods 0.000 description 3
- 229920006395 saturated elastomer Polymers 0.000 description 3
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 3
- 238000011282 treatment Methods 0.000 description 3
- 230000029812 viral genome replication Effects 0.000 description 3
- WSLDOOZREJYCGB-UHFFFAOYSA-N 1,2-Dichloroethane Chemical compound ClCCCl WSLDOOZREJYCGB-UHFFFAOYSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 206010019799 Hepatitis viral Diseases 0.000 description 2
- 102000005741 Metalloproteases Human genes 0.000 description 2
- 108010006035 Metalloproteases Proteins 0.000 description 2
- 108060004795 Methyltransferase Proteins 0.000 description 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 2
- IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 description 2
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- RHQDFWAXVIIEBN-UHFFFAOYSA-N Trifluoroethanol Chemical compound OCC(F)(F)F RHQDFWAXVIIEBN-UHFFFAOYSA-N 0.000 description 2
- 108700010756 Viral Polyproteins Proteins 0.000 description 2
- 241000700605 Viruses Species 0.000 description 2
- SORGEQQSQGNZFI-UHFFFAOYSA-N [azido(phenoxy)phosphoryl]oxybenzene Chemical compound C=1C=CC=CC=1OP(=O)(N=[N+]=[N-])OC1=CC=CC=C1 SORGEQQSQGNZFI-UHFFFAOYSA-N 0.000 description 2
- DKNWSYNQZKUICI-UHFFFAOYSA-N amantadine Chemical compound C1C(C2)CC3CC2CC1(N)C3 DKNWSYNQZKUICI-UHFFFAOYSA-N 0.000 description 2
- 229960003805 amantadine Drugs 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 description 2
- 150000001721 carbon Chemical group 0.000 description 2
- 239000011203 carbon fibre reinforced carbon Substances 0.000 description 2
- PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 description 2
- 230000001684 chronic effect Effects 0.000 description 2
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 description 2
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 description 2
- 230000002519 immonomodulatory effect Effects 0.000 description 2
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N indane Chemical compound C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 230000008520 organization Effects 0.000 description 2
- 235000019833 protease Nutrition 0.000 description 2
- 229960000329 ribavirin Drugs 0.000 description 2
- HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 150000003457 sulfones Chemical class 0.000 description 2
- 201000001862 viral hepatitis Diseases 0.000 description 2
- UERNRFHISLXQFU-DFWYDOINSA-N (2S)-5-oxopyrrolidine-2-carboxylic acid pyridine Chemical compound c1ccncc1.OC(=O)[C@@H]1CCC(=O)N1 UERNRFHISLXQFU-DFWYDOINSA-N 0.000 description 1
- ASOKPJOREAFHNY-UHFFFAOYSA-N 1-Hydroxybenzotriazole Chemical compound C1=CC=C2N(O)N=NC2=C1 ASOKPJOREAFHNY-UHFFFAOYSA-N 0.000 description 1
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 description 1
- 108010017640 Aspartic Acid Proteases Proteins 0.000 description 1
- 102000004580 Aspartic Acid Proteases Human genes 0.000 description 1
- 206010008909 Chronic Hepatitis Diseases 0.000 description 1
- 206010010144 Completed suicide Diseases 0.000 description 1
- 206010016654 Fibrosis Diseases 0.000 description 1
- 229940124771 HCV-NS3 protease inhibitor Drugs 0.000 description 1
- 241000725303 Human immunodeficiency virus Species 0.000 description 1
- 102000006992 Interferon-alpha Human genes 0.000 description 1
- 108010047761 Interferon-alpha Proteins 0.000 description 1
- ZKGNPQKYVKXMGJ-UHFFFAOYSA-N N,N-dimethylacetamide Chemical compound CN(C)C(C)=O.CN(C)C(C)=O ZKGNPQKYVKXMGJ-UHFFFAOYSA-N 0.000 description 1
- 101800000515 Non-structural protein 3 Proteins 0.000 description 1
- 101710144111 Non-structural protein 3 Proteins 0.000 description 1
- 101800001020 Non-structural protein 4A Proteins 0.000 description 1
- 208000037581 Persistent Infection Diseases 0.000 description 1
- 241000208474 Protea Species 0.000 description 1
- YZCKVEUIGOORGS-IGMARMGPSA-N Protium Chemical compound [1H] YZCKVEUIGOORGS-IGMARMGPSA-N 0.000 description 1
- 241000710772 Yellow fever virus Species 0.000 description 1
- 101900322197 Yellow fever virus Serine protease NS3 Proteins 0.000 description 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
- YBCVMFKXIKNREZ-UHFFFAOYSA-N acoh acetic acid Chemical compound CC(O)=O.CC(O)=O YBCVMFKXIKNREZ-UHFFFAOYSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 150000001335 aliphatic alkanes Chemical class 0.000 description 1
- 150000001336 alkenes Chemical class 0.000 description 1
- 150000001345 alkine derivatives Chemical class 0.000 description 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 description 1
- QWCKQJZIFLGMSD-UHFFFAOYSA-N alpha-aminobutyric acid Chemical compound CCC(N)C(O)=O QWCKQJZIFLGMSD-UHFFFAOYSA-N 0.000 description 1
- 229940124277 aminobutyric acid Drugs 0.000 description 1
- 125000002178 anthracenyl group Chemical group C1(=CC=CC2=CC3=CC=CC=C3C=C12)* 0.000 description 1
- 150000005840 aryl radicals Chemical class 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 208000020403 chronic hepatitis C virus infection Diseases 0.000 description 1
- 230000007882 cirrhosis Effects 0.000 description 1
- 208000019425 cirrhosis of liver Diseases 0.000 description 1
- 150000001924 cycloalkanes Chemical class 0.000 description 1
- 150000001925 cycloalkenes Chemical class 0.000 description 1
- 125000000392 cycloalkenyl group Chemical group 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 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 description 1
- 125000000058 cyclopentadienyl group Chemical group C1(=CC=CC1)* 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- DEZRYPDIMOWBDS-UHFFFAOYSA-N dcm dichloromethane Chemical compound ClCCl.ClCCl DEZRYPDIMOWBDS-UHFFFAOYSA-N 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- UXGNZZKBCMGWAZ-UHFFFAOYSA-N dimethylformamide dmf Chemical compound CN(C)C=O.CN(C)C=O UXGNZZKBCMGWAZ-UHFFFAOYSA-N 0.000 description 1
- 231100000676 disease causative agent Toxicity 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- ZSWFCLXCOIISFI-UHFFFAOYSA-N endo-cyclopentadiene Natural products C1C=CC=C1 ZSWFCLXCOIISFI-UHFFFAOYSA-N 0.000 description 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 208000010710 hepatitis C virus infection Diseases 0.000 description 1
- 125000005980 hexynyl group Chemical group 0.000 description 1
- 239000004030 hiv protease inhibitor Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 208000018191 liver inflammation Diseases 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000004949 mass spectrometry Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000010369 molecular cloning Methods 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- LLYKPZOWCPVRPD-UHFFFAOYSA-N n,n-dimethylpyridin-2-amine;n,n-dimethylpyridin-4-amine Chemical compound CN(C)C1=CC=NC=C1.CN(C)C1=CC=CC=N1 LLYKPZOWCPVRPD-UHFFFAOYSA-N 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 125000005981 pentynyl group Chemical group 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 description 1
- 230000006337 proteolytic cleavage Effects 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 description 1
- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229960005486 vaccine Drugs 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 230000006514 viral protein processing Effects 0.000 description 1
- 230000017613 viral reproduction Effects 0.000 description 1
- 229940051021 yellow-fever virus Drugs 0.000 description 1
Classifications
-
- 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
- C07K5/10—Tetrapeptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P31/12—Antivirals
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- 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
- C07K5/10—Tetrapeptides
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
-
- 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
- C07K5/10—Tetrapeptides
- C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Crystallography & Structural Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2829096P | 1996-10-18 | 1996-10-18 | |
| PCT/US1997/018968 WO1998017679A1 (en) | 1996-10-18 | 1997-10-17 | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AP9901512A0 AP9901512A0 (en) | 1999-06-30 |
| AP1019A true AP1019A (en) | 2001-10-16 |
Family
ID=21842625
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| APAP/P/1999/001512A AP1019A (en) | 1996-10-18 | 1997-10-17 | Inhibitors of serinre proteases, particularly hepatitis C virus NS3 protease. |
Country Status (33)
Families Citing this family (354)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7135584B2 (en) | 1995-08-07 | 2006-11-14 | Wake Forest University | Lipid analogs for treating viral infections |
| DE69535758D1 (de) | 1994-08-29 | 2008-07-03 | Univ Wake Forest | Lipid-analoge zur behandlung von viralen infektionen |
| JP4080541B2 (ja) * | 1996-10-18 | 2008-04-23 | バーテックス ファーマシューティカルズ インコーポレイテッド | セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子 |
| GB9707659D0 (en) * | 1997-04-16 | 1997-06-04 | Peptide Therapeutics Ltd | Hepatitis C NS3 Protease inhibitors |
| US6767991B1 (en) | 1997-08-11 | 2004-07-27 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis C inhibitor peptides |
| NZ503263A (en) * | 1997-08-11 | 2002-10-25 | Boehringer Ingelheim Ca Ltd | Hepatitis C NS3 protease inhibitor peptides and peptide analogues |
| JP4354632B2 (ja) * | 1997-08-11 | 2009-10-28 | ベーリンガー インゲルハイム （カナダ） リミテッド | Ｃ型肝炎抑制剤ペプチド |
| GB9806815D0 (en) * | 1998-03-30 | 1998-05-27 | Hoffmann La Roche | Amino acid derivatives |
| DE69934104T2 (de) * | 1998-03-31 | 2007-06-28 | Vertex Pharmaceuticals Inc., Cambridge | Inhibitoren von serinproteasen, insbesondere von hepatitis c virus ns3 protease |
| GB9809664D0 (en) * | 1998-05-06 | 1998-07-01 | Hoffmann La Roche | a-Ketoamide derivatives |
| GB9812523D0 (en) | 1998-06-10 | 1998-08-05 | Angeletti P Ist Richerche Bio | Peptide inhibitors of hepatitis c virus ns3 protease |
| US6323180B1 (en) | 1998-08-10 | 2001-11-27 | Boehringer Ingelheim (Canada) Ltd | Hepatitis C inhibitor tri-peptides |
| 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. |
| EP1159273A1 (en) | 1999-03-02 | 2001-12-05 | Boehringer Ingelheim Pharmaceuticals Inc. | Compounds useful as reversible inhibitors of cathepsin s |
| UA74546C2 (en) * | 1999-04-06 | 2006-01-16 | Boehringer Ingelheim Ca Ltd | Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition |
| US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
| AU5788800A (en) * | 1999-07-07 | 2001-01-22 | Du Pont Pharmaceuticals Company | Peptide boronic acid inhibitors of hepatitis c virus protease |
| WO2001007407A1 (en) * | 1999-07-26 | 2001-02-01 | Bristol-Myers Squibb Pharma Company | Lactam inhibitors of hepatitis c virus ns3 protease |
| US7122627B2 (en) | 1999-07-26 | 2006-10-17 | Bristol-Myers Squibb Company | Lactam inhibitors of Hepatitis C virus NS3 protease |
| US6420364B1 (en) | 1999-09-13 | 2002-07-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compound useful as reversible inhibitors of cysteine proteases |
| US7026469B2 (en) | 2000-10-19 | 2006-04-11 | Wake Forest University School Of Medicine | Compositions and methods of double-targeting virus infections and cancer cells |
| WO2001040262A1 (en) * | 1999-12-03 | 2001-06-07 | Bristol-Myers Squibb Pharma Company | Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease |
| US7238709B2 (en) * | 1999-12-07 | 2007-07-03 | Theravance, Inc. | Therapeutic carbamates |
| JP2003525294A (ja) | 2000-02-29 | 2003-08-26 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | Ｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害剤 |
| ES2240446T3 (es) | 2000-04-03 | 2005-10-16 | Vertex Pharma | Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c. |
| AU2006202124B2 (en) * | 2000-04-03 | 2010-01-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of Serine Proteases, Particularly Hepatitis C Virus NS3 Protease |
| KR20030036152A (ko) | 2000-04-05 | 2003-05-09 | 쉐링 코포레이션 | Ｎ-사이클릭 ｐ2 잔기를 포함하는 ｃ형 간염 바이러스의매크로사이클릭 ｎｓ3-세린 프로테아제 억제제 |
| CN1935833A (zh) | 2000-04-19 | 2007-03-28 | 先灵公司 | 含有烷基和芳基丙氨酸p2部分的丙型肝炎病毒的大环ns3－丝氨酸蛋白酶抑制剂 |
| PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
| MY164523A (en) | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
| EP1294735A2 (en) | 2000-05-26 | 2003-03-26 | Novirio Pharmaceuticals Limited | Methods and compositions for treating flaviviruses and pestiviruses |
| US20020007324A1 (en) * | 2000-06-09 | 2002-01-17 | Centner David J. | System and method for effectively conducting transactions between buyers and suppliers |
| AR029851A1 (es) * | 2000-07-21 | 2003-07-16 | Dendreon Corp | Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c |
| US7012066B2 (en) * | 2000-07-21 | 2006-03-14 | Schering Corporation | Peptides as NS3-serine protease inhibitors of hepatitis C virus |
| CZ2003195A3 (cs) | 2000-07-21 | 2003-04-16 | Schering Corporation | Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostředek |
| AR034127A1 (es) * | 2000-07-21 | 2004-02-04 | Schering Corp | Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento |
| 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 |
| DK1326632T3 (da) * | 2000-10-12 | 2007-01-15 | Viromics Gmbh | Protease-inhibitorer til behandling af infektioner af hepatitisvirus |
| AU2874902A (en) | 2000-10-18 | 2002-04-29 | Pharmasset Ltd | Modified nucleosides for treatment of viral infections and abnormal cellular proliferation |
| US7309696B2 (en) | 2000-10-19 | 2007-12-18 | Wake Forest University | Compositions and methods for targeting cancer cells |
| US6846806B2 (en) | 2000-10-23 | 2005-01-25 | Bristol-Myers Squibb Company | Peptide inhibitors of Hepatitis C virus NS3 protein |
| ATE430166T1 (de) * | 2000-12-12 | 2009-05-15 | Schering Corp | Diarylrest entfassende peptide als inhibitoren des ns-3 serinproteases von hepatitis c virus |
| US6727366B2 (en) | 2000-12-13 | 2004-04-27 | Bristol-Myers Squibb Pharma Company | Imidazolidinones and their related derivatives as hepatitis C virus NS3 protease inhibitors |
| US6653295B2 (en) | 2000-12-13 | 2003-11-25 | Bristol-Myers Squibb Company | Inhibitors of hepatitis C virus NS3 protease |
| ATE526339T1 (de) | 2001-01-22 | 2011-10-15 | Merck Sharp & Dohme | Nukleosidderivate als inhibitoren der rna- abhängigen viralen rna-polymerase |
| CA2449504A1 (en) | 2001-07-11 | 2003-01-23 | Vertex Pharmaceuticals Incorporated | Bridged bicyclic serine protease inhibitors |
| IL160080A0 (en) | 2001-08-31 | 2004-06-20 | Thomson Licensing Sa | Sequence counter for an audio visual stream |
| AU2002330154A1 (en) | 2001-09-28 | 2003-04-07 | Centre National De La Recherche Scientifique | Methods and compositions for treating hepatitis c virus using 4'-modified nucleosides |
| WO2003035060A1 (en) * | 2001-10-24 | 2003-05-01 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4a protease, incorporating a fused ring system |
| MY151199A (en) * | 2001-11-02 | 2014-04-30 | Rigel Pharmaceuticals Inc | Substituted diphenyl heterocycles useful for treating hcv infection |
| KR20040077767A (ko) | 2002-01-23 | 2004-09-06 | 쉐링 코포레이션 | Ｃ형 간염 바이러스 감염 치료용 ｎｓ3-세린 프로테아제억제제로서의 프롤린 화합물 |
| US7119072B2 (en) | 2002-01-30 | 2006-10-10 | Boehringer Ingelheim (Canada) Ltd. | Macrocyclic peptides active against the hepatitis C virus |
| US7091184B2 (en) | 2002-02-01 | 2006-08-15 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| US6642204B2 (en) | 2002-02-01 | 2003-11-04 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| RU2004133044A (ru) * | 2002-04-11 | 2006-01-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Ингибиторы сериновых протеаз, в частности, протеазы ns3-ns4a hcv |
| WO2004043339A2 (en) | 2002-05-20 | 2004-05-27 | Bristol-Myers Squibb Company | Substituted cycloalkyl p1' hepatitis c virus inhibitors |
| JP4312711B2 (ja) | 2002-05-20 | 2009-08-12 | ブリストル−マイヤーズ スクイブ カンパニー | ヘテロ環式スルホンアミドｃ型肝炎ウイルス阻害剤 |
| JP4312718B2 (ja) * | 2002-05-20 | 2009-08-12 | ブリストル−マイヤーズ スクイブ カンパニー | Ｃ型肝炎ウイルス阻害剤 |
| MY140680A (en) * | 2002-05-20 | 2010-01-15 | Bristol Myers Squibb Co | Hepatitis c virus inhibitors |
| JP2005533817A (ja) | 2002-06-28 | 2005-11-10 | イデニクス（ケイマン）リミテツド | フラビウィルス科ウィルス感染治療用の修飾２′および３′−ヌクレオシドプロドラッグ |
| AU2003277891A1 (en) * | 2002-09-23 | 2004-04-08 | Medivir Ab | Hcv ns-3 serine protease inhibitors |
| US20050075279A1 (en) | 2002-10-25 | 2005-04-07 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis C virus |
| PL377342A1 (pl) | 2002-11-15 | 2006-01-23 | Idenix (Cayman) Limited | Nukleozydy rozgałęzione w pozycji 2' oraz mutacja Flaviviridae |
| AU2011203054B2 (en) * | 2003-04-11 | 2012-04-26 | Vertex Pharmaceuticals, Incorporated | Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease |
| ATE547412T1 (de) * | 2003-04-11 | 2012-03-15 | Vertex Pharma | Inhibitoren von serinproteasen, insbesondere hcv- ns3-ns4a-protease |
| EP1620412A2 (en) | 2003-05-02 | 2006-02-01 | Rigel Pharmaceuticals, Inc. | Heterocyclic compounds and hydro isomers thereof |
| RS51294B (sr) | 2003-05-21 | 2010-12-31 | Boehringer Ingelheim International Gmbh. | Inhibitorna jedinjenja za hepatitis c |
| EP4032897B1 (en) | 2003-05-30 | 2025-01-29 | Gilead Pharmasset LLC | Modified fluorinated nucleoside analogues |
| NZ544789A (en) * | 2003-07-18 | 2010-01-29 | Vertex Pharma | Dithia-azaspiro-nonane and decane derivatives as inhibitors of serine proteases |
| DK1658302T3 (da) | 2003-07-25 | 2010-11-22 | Idenix Pharmaceuticals Inc | Purinnukleosidanaloge til behandling af sygdomme forårsaget af Flavirividae, herunder hepatitis C |
| US7576206B2 (en) | 2003-08-14 | 2009-08-18 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| US7223745B2 (en) | 2003-08-14 | 2007-05-29 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| JP4527722B2 (ja) | 2003-08-26 | 2010-08-18 | シェーリング コーポレイション | Ｃ型肝炎ウイルスの新規のペプチド模倣性ｎｓ３−セリンプロテアーゼインヒビター |
| TWI359147B (en) * | 2003-09-05 | 2012-03-01 | Vertex Pharma | Inhibitors of serine proteases, particularly hcv n |
| AU2004274468B2 (en) * | 2003-09-18 | 2009-07-23 | Vertex Pharmaceuticals, Incorporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| PE20050431A1 (es) | 2003-09-22 | 2005-07-19 | Boehringer Ingelheim Int | Peptidos macrociclicos activos contra el virus de la hepatitis c |
| AR046166A1 (es) | 2003-09-26 | 2005-11-30 | Schering Corp | Inhibidores macrociclicos de la serina proteasa ns3 del virus de la hepatitis c |
| AU2004282148A1 (en) * | 2003-10-10 | 2005-04-28 | Vertex Pharmaceuticals Incoporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| US7365092B2 (en) | 2003-10-10 | 2008-04-29 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| BRPI0415373A (pt) | 2003-10-14 | 2006-12-12 | Intermune Inc | ácidos carboxìlicos macrocìclicos e acilsulfonamidas como inibidores de replicação de hcv |
| JP4890254B2 (ja) | 2003-10-27 | 2012-03-07 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｈｃｖｎｓ３−ｎｓ４ａプロテアーゼ耐性突然変異体 |
| EP1944042A1 (en) | 2003-10-27 | 2008-07-16 | Vertex Pharmceuticals Incorporated | Combinations for HCV treatment |
| US8187874B2 (en) | 2003-10-27 | 2012-05-29 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
| US7132504B2 (en) | 2003-11-12 | 2006-11-07 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7309708B2 (en) | 2003-11-20 | 2007-12-18 | Birstol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7253160B2 (en) | 2003-11-20 | 2007-08-07 | Schering Corporation | Depeptidized inhibitors of hepatitis C virus NS3 protease |
| US7135462B2 (en) | 2003-11-20 | 2006-11-14 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| GB0500020D0 (en) | 2005-01-04 | 2005-02-09 | Novartis Ag | Organic compounds |
| CA2549851C (en) | 2004-01-21 | 2012-09-11 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis c virus |
| AU2005207815B2 (en) * | 2004-01-30 | 2011-08-04 | Medivir Ab | HCV NS-3 serine protease inhibitors |
| CN1938332B (zh) | 2004-02-04 | 2011-10-19 | 沃泰克斯药物股份有限公司 | 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂 |
| WO2005080399A1 (ja) | 2004-02-24 | 2005-09-01 | Japan Tobacco Inc. | ４環縮合複素環化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用 |
| US20070049593A1 (en) | 2004-02-24 | 2007-03-01 | Japan Tobacco Inc. | Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor |
| TWI314927B (en) | 2004-02-27 | 2009-09-21 | Schering Corporatio | Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease |
| US7816326B2 (en) | 2004-02-27 | 2010-10-19 | Schering Corporation | Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease |
| ES2349328T3 (es) | 2004-02-27 | 2010-12-30 | Schering Corporation | Nuevos compuestos como inhibidores de la serina proteasa ns3 del virus de la hepatitis c. |
| EP1730165A1 (en) | 2004-02-27 | 2006-12-13 | Schering Corporation | Inhibitors of hepatitis c virus ns3 protease |
| RU2006134005A (ru) | 2004-02-27 | 2008-04-10 | Шеринг Корпорейшн (US) | Новые соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с |
| AU2005223767B2 (en) * | 2004-03-12 | 2011-12-01 | Vertex Pharmaceuticals Incorporated | Processes and intermediates for the preparation of aspartic acetal caspase inhibitors |
| US8198270B2 (en) * | 2004-04-15 | 2012-06-12 | Onyx Therapeutics, Inc. | Compounds for proteasome enzyme inhibition |
| SG185306A1 (en) | 2004-04-15 | 2012-11-29 | Onyx Therapeutics Inc | Compounds for proteasome enzyme inhibition |
| EP2564834A3 (en) * | 2004-05-10 | 2013-08-21 | Onyx Therapeutics, Inc. | Compounds for Proteasome Enzyme Inhibition |
| US7399749B2 (en) | 2004-05-20 | 2008-07-15 | Schering Corporation | Substituted prolines as inhibitors of hepatitis C virus NS3 serine protease |
| CA2571984C (en) * | 2004-07-16 | 2012-04-10 | Gilead Sciences, Inc. | Antiviral compounds |
| UY29016A1 (es) | 2004-07-20 | 2006-02-24 | Boehringer Ingelheim Int | Analogos de dipeptidos inhibidores de la hepatitis c |
| JP4914355B2 (ja) | 2004-07-20 | 2012-04-11 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃ型肝炎インヒビターペプチド類似体 |
| CN101023094B (zh) | 2004-07-21 | 2011-05-18 | 法莫赛特股份有限公司 | 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备 |
| WO2006020580A2 (en) * | 2004-08-09 | 2006-02-23 | Alios Biopharma Inc. | Synthetic hyperglycosylated, protease-resistant polypeptide variants, oral formulations and methods of using the same |
| US7597884B2 (en) | 2004-08-09 | 2009-10-06 | Alios Biopharma, Inc. | Hyperglycosylated polypeptide variants and methods of use |
| MX2007002371A (es) | 2004-08-27 | 2007-04-23 | Schering Corp | Compuestos de acilsulfonamida como inhibidores de la serina proteasa ns3 del virus de la hepatitis c. |
| ES2769377T3 (es) | 2004-09-14 | 2020-06-25 | Gilead Pharmasset Llc | Intermedios de D-ribonolactona con sustitución de 2-fluoro-2-alquilo |
| SG191661A1 (en) | 2004-10-01 | 2013-07-31 | Vertex Pharma | Hcv ns3-ns4a protease inhibition |
| US7659263B2 (en) | 2004-11-12 | 2010-02-09 | Japan Tobacco Inc. | Thienopyrrole compound and use thereof as HCV polymerase inhibitor |
| US7323447B2 (en) | 2005-02-08 | 2008-01-29 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7468383B2 (en) | 2005-02-11 | 2008-12-23 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| US7592336B2 (en) | 2005-05-10 | 2009-09-22 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7569600B2 (en) | 2005-05-13 | 2009-08-04 | Virochem Pharma Inc. | Compounds and methods for the treatment of prevention of Flavivirus infections |
| EP1881828A4 (en) * | 2005-05-20 | 2009-06-03 | Valeant Res & Dev | TREATMENT OF HEPATITIS C (HCV) USING SUB-THERAPEUTIC DOSES OF RIBAVIRIN |
| US20070237818A1 (en) * | 2005-06-02 | 2007-10-11 | Malcolm Bruce A | Controlled-release formulation of HCV protease inhibitor and methods using the same |
| WO2006130628A2 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Combination of hcv protease inhibitors with a surfactant |
| US20060276404A1 (en) * | 2005-06-02 | 2006-12-07 | Anima Ghosal | Medicaments and methods combining a HCV protease inhibitor and an AKR competitor |
| WO2006130686A2 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Hcv protease inhibitors in combination with food |
| AR054778A1 (es) | 2005-06-17 | 2007-07-18 | Novartis Ag | Uso de sangliferina en hcv |
| US7608592B2 (en) * | 2005-06-30 | 2009-10-27 | Virobay, Inc. | HCV inhibitors |
| US7601686B2 (en) | 2005-07-11 | 2009-10-13 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2007015824A2 (en) | 2005-07-25 | 2007-02-08 | Intermune, Inc. | Novel macrocyclic inhibitors of hepatitis c virus replication |
| US7666834B2 (en) | 2005-07-29 | 2010-02-23 | Tibotec Pharmaceuticals Ltd. | Macrocyclic inhibitors of hepatitis C virus |
| PE20070211A1 (es) * | 2005-07-29 | 2007-05-12 | Medivir Ab | Compuestos macrociclicos como inhibidores del virus de hepatitis c |
| PE20070210A1 (es) | 2005-07-29 | 2007-04-16 | Tibotec Pharm Ltd | Compuestos macrociclicos como inhibidores del virus de hepatitis c |
| DE602006019741D1 (de) | 2005-07-29 | 2011-03-03 | Medivir Ab | Makrocyclische inhibitoren des hepatitis-c-virus |
| TWI393723B (zh) | 2005-07-29 | 2013-04-21 | Tibotec Pharm Ltd | Ｃ型肝炎病毒之大環抑制劑（九） |
| WO2007014920A1 (en) | 2005-07-29 | 2007-02-08 | Tibotec Pharmaceuticals Ltd. | Macrocyclic inhibitors of hepatitis c virus |
| ME01318B (me) | 2005-07-29 | 2013-12-20 | Tibotec Pharm Ltd | Makrociklički inhibitori virusa hepatitisa C |
| PL1913015T3 (pl) | 2005-07-29 | 2014-04-30 | Janssen R&D Ireland | Makrocykliczne inhibitory wirusa zapalenia wątroby typu C |
| JO2768B1 (en) | 2005-07-29 | 2014-03-15 | تيبوتيك فارماسيوتيكالز ليمتد | Large cyclic inhibitors of hepatitis C virus |
| US20090325889A1 (en) * | 2005-08-01 | 2009-12-31 | David Alan Campbell | Hepatitis c serine protease inhibitors and uses therefor |
| MX2008001528A (es) | 2005-08-02 | 2008-04-04 | Vertex Pharma | Inhibidores de serina proteasas. |
| ES2344156T3 (es) | 2005-08-19 | 2010-08-19 | Vertex Pharmaceuticals Incorporated | Procedimientos e intermedios. |
| US8399615B2 (en) | 2005-08-19 | 2013-03-19 | Vertex Pharmaceuticals Incorporated | Processes and intermediates |
| US7964624B1 (en) | 2005-08-26 | 2011-06-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| AR055395A1 (es) | 2005-08-26 | 2007-08-22 | Vertex Pharma | Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c |
| US20090099186A1 (en) * | 2005-10-11 | 2009-04-16 | Leonid Beigelman | Inhibitors of viral replication |
| KR20080056295A (ko) | 2005-10-11 | 2008-06-20 | 인터뮨, 인크. | Ｃ형 간염 바이러스 복제를 억제하기 위한 화합물 및 방법 |
| US7772183B2 (en) | 2005-10-12 | 2010-08-10 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7741281B2 (en) | 2005-11-03 | 2010-06-22 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| EP1948678B1 (en) | 2005-11-09 | 2013-05-01 | Onyx Therapeutics, Inc. | Compounds for enzyme inhibition |
| US7705138B2 (en) | 2005-11-11 | 2010-04-27 | Vertex Pharmaceuticals Incorporated | Hepatitis C virus variants |
| EP2392588A3 (en) | 2005-11-11 | 2012-03-07 | Vertex Pharmaceuticals Incorporated | Hepatitis C virus variants |
| PT1966130E (pt) | 2005-12-23 | 2014-01-30 | Zealand Pharma As | Compostos miméticos de lisina modificados |
| EP2029153A2 (en) * | 2006-01-27 | 2009-03-04 | Phenomix Corporation | Hepatitis c serine protease inhibitors and uses therefor |
| CA2641859A1 (en) * | 2006-02-09 | 2007-08-16 | Schering Corporation | Combinations comprising hcv protease inhibitor(s) and hcv polymerase inhibitor(s), and methods of treatment related thereto |
| JP5436864B2 (ja) | 2006-02-27 | 2014-03-05 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｖｘ−９５０を含む共結晶体およびそれを含む医薬組成物 |
| WO2007109080A2 (en) * | 2006-03-16 | 2007-09-27 | Vertex Pharmaceuticals Incorporated | Deuterated hepatitis c protease inhibitors |
| BRPI0710878A2 (pt) | 2006-04-11 | 2015-03-31 | Novartis Ag | Compostos orgânicos e seus usos |
| US8017612B2 (en) | 2006-04-18 | 2011-09-13 | Japan Tobacco Inc. | Piperazine compound and use thereof as a HCV polymerase inhibitor |
| RU2419626C2 (ru) | 2006-05-23 | 2011-05-27 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы |
| MY183014A (en) | 2006-06-19 | 2021-02-05 | Onyx Therapeutics Inc | Compounds for enzyme inhibition |
| EP2049474B1 (en) | 2006-07-11 | 2015-11-04 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| EP1886685A1 (en) | 2006-08-11 | 2008-02-13 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods, uses and compositions for modulating replication of hcv through the farnesoid x receptor (fxr) activation or inhibition |
| KR20090057035A (ko) * | 2006-08-21 | 2009-06-03 | 유나이티드 세러퓨틱스 코오포레이션 | 바이러스 감염의 치료를 위한 병용 요법 |
| AU2007290535A1 (en) * | 2006-08-28 | 2008-03-06 | Vertex Pharmaceuticals Incorporated | Method for identifying protease inhibitors |
| US8343477B2 (en) | 2006-11-01 | 2013-01-01 | Bristol-Myers Squibb Company | Inhibitors of hepatitis C virus |
| US7772180B2 (en) | 2006-11-09 | 2010-08-10 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| AU2007321677B2 (en) | 2006-11-15 | 2013-04-11 | Vertex Pharmaceuticals (Canada) Incorporated | Thiophene analogues for the treatment or prevention of flavivirus infections |
| US7888464B2 (en) | 2006-11-16 | 2011-02-15 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US8003604B2 (en) | 2006-11-16 | 2011-08-23 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7763584B2 (en) | 2006-11-16 | 2010-07-27 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| EP2099430A2 (en) | 2006-12-07 | 2009-09-16 | Schering Corporation | Ph sensitive matrix formulation |
| EP2468724B1 (en) | 2006-12-21 | 2015-11-18 | Zealand Pharma A/S | Synthesis of pyrrolidine compounds |
| CA2674831A1 (en) | 2006-12-22 | 2008-11-13 | Schering Corporation | 5,6-ring annulated indole derivatives and methods of use thereof |
| MX2009006878A (es) | 2006-12-22 | 2009-07-07 | Schering Corp | Derivados indolicos con anillo unido en las posiciones 4,5 para tratar o prevenir infecciones virales por virus de la hepatitis c e infecciones virales relacionadas. |
| CN101631773A (zh) | 2006-12-22 | 2010-01-20 | 先灵公司 | 治疗或预防hcv和相关病毒感染的4,5-环化吲哚衍生物 |
| JP5554569B2 (ja) | 2007-02-08 | 2014-07-23 | ヤンセン・アールアンドデイ・アイルランド | ピリミジン置換された大環状ｈｃｖ阻害剤 |
| WO2008097676A1 (en) * | 2007-02-09 | 2008-08-14 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| EP2134717A2 (en) | 2007-02-27 | 2009-12-23 | Vertex Pharmceuticals Incorporated | Inhibitors of serine proteases |
| PT2114924E (pt) * | 2007-02-27 | 2012-04-03 | Vertex Pharma | Co-cristais e composições farmacêuticas que compreendem os mesmos |
| CA2696053A1 (en) | 2007-02-28 | 2008-09-04 | Conatus Pharmaceuticals, Inc. | Methods for the treatment of liver diseases |
| WO2008106167A1 (en) * | 2007-02-28 | 2008-09-04 | Conatus Pharmaceuticals, Inc. | Combination therapy comprising matrix metalloproteinase inhibitors and caspase inhibitors for the treatment of liver diseases |
| US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| MX2009011930A (es) | 2007-05-04 | 2009-11-18 | Vertex Pharma | Terapia de combinacion para el tratamiento de infeccion de virus de hepatitis c. |
| BRPI0813733A2 (pt) | 2007-06-29 | 2019-11-05 | Gilead Sciences Inc | composto com atividade inibidora de hcv, sua composição farmacêutica e seu uso. |
| WO2009005676A2 (en) | 2007-06-29 | 2009-01-08 | Gilead Sciences, Inc. | Antiviral compounds |
| CA2697454C (en) | 2007-08-29 | 2015-11-03 | Schering Corporation | 2-carboxy substituted indole derivatives and methods of use thereof |
| MX2010002319A (es) | 2007-08-29 | 2010-03-22 | Schering Corp | Derivados indolicos 2,3 sustituidos para el tratamiento de infecciones virales. |
| EP2195317B1 (en) | 2007-08-29 | 2012-01-18 | Schering Corporation | 2,3-substituted azaindole derivatives for treating viral infections |
| EP2185546B1 (en) * | 2007-08-30 | 2011-10-26 | Vertex Pharmceuticals Incorporated | Co-crystals and pharmaceutical compositions comprising the same |
| GB0718575D0 (en) | 2007-09-24 | 2007-10-31 | Angeletti P Ist Richerche Bio | Nucleoside derivatives as inhibitors of viral polymerases |
| NZ584814A (en) | 2007-10-04 | 2012-03-30 | Onyx Therapeutics Inc | Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides |
| EP2222660B1 (en) | 2007-11-16 | 2014-03-26 | Merck Sharp & Dohme Corp. | 3-heterocyclic substituted indole derivatives and methods of use thereof |
| US8377928B2 (en) | 2007-11-16 | 2013-02-19 | Merck Sharp & Dohme Corp. | 3-aminosulfonyl substituted indole derivatives and methods of use thereof |
| US8202996B2 (en) | 2007-12-21 | 2012-06-19 | Bristol-Myers Squibb Company | Crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N- ((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide |
| AU2009210789B2 (en) | 2008-02-04 | 2014-01-30 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors |
| TW200946541A (en) | 2008-03-27 | 2009-11-16 | Idenix Pharmaceuticals Inc | Solid forms of an anti-HIV phosphoindole compound |
| US8163921B2 (en) | 2008-04-16 | 2012-04-24 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7964560B2 (en) | 2008-05-29 | 2011-06-21 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| EP2300491B1 (en) | 2008-05-29 | 2016-01-06 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| CA2727620A1 (en) | 2008-06-13 | 2009-12-17 | Schering Corporation | Tricyclic indole derivatives and methods of use thereof |
| EP2476690A1 (en) | 2008-07-02 | 2012-07-18 | IDENIX Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of viral infections |
| TWI409265B (zh) | 2008-08-20 | 2013-09-21 | Merck Sharp & Dohme | 經取代之吡啶及嘧啶衍生物及彼等於治療病毒感染之用途 |
| US8470834B2 (en) | 2008-08-20 | 2013-06-25 | Merck Sharp & Dohme Corp. | AZO-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| CA2734487A1 (en) | 2008-08-20 | 2010-02-25 | Southern Research Institute | Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| ES2439009T3 (es) | 2008-08-20 | 2014-01-21 | Merck Sharp & Dohme Corp. | Derivados de piridina y pirimidina sustituidos con etenilo y su uso en el tratamiento de infecciones virales |
| US8207341B2 (en) | 2008-09-04 | 2012-06-26 | Bristol-Myers Squibb Company | Process or synthesizing substituted isoquinolines |
| US8044087B2 (en) | 2008-09-29 | 2011-10-25 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US8563505B2 (en) | 2008-09-29 | 2013-10-22 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| EP2341924A4 (en) | 2008-10-02 | 2013-01-23 | David Gladstone Inst | METHOD FOR THE TREATMENT OF HEPATITIS C VIRUS INFECTIONS |
| MX2011004225A (es) | 2008-10-21 | 2011-06-21 | Onyx Therapeutics Inc | Terapia de combinacion con epoxicetonas peptidicas. |
| WO2010065668A1 (en) | 2008-12-03 | 2010-06-10 | Presidio Pharmaceuticals, Inc. | Inhibitors of hcv ns5a |
| PE20150939A1 (es) | 2008-12-03 | 2015-07-19 | Presidio Pharmaceuticals Inc | Inhibidores de la proteina no estructural 5a del virus de la hepatitis c |
| US8283310B2 (en) | 2008-12-15 | 2012-10-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US8914351B2 (en) | 2008-12-16 | 2014-12-16 | Clinton A. Krislov | Method and system for secure automated document registration from social media networks |
| US8589372B2 (en) | 2008-12-16 | 2013-11-19 | Clinton A. Krislov | Method and system for automated document registration with cloud computing |
| WO2010080389A1 (en) * | 2008-12-19 | 2010-07-15 | Gilead Sciences, Inc. | Hcv ns3 protease inhibitors |
| JP5713919B2 (ja) | 2008-12-23 | 2015-05-07 | ギリアド ファーマセット エルエルシー | ヌクレオシドホスホラミデート |
| PA8855701A1 (es) | 2008-12-23 | 2010-07-27 | Análogos de nucleósidos | |
| CL2009002206A1 (es) | 2008-12-23 | 2011-08-26 | Gilead Pharmasset Llc | Compuestos derivados de pirrolo -(2-3-d]-pirimidin-7(6h)-tetrahidrofuran-2-il fosfonamidato, composicion farmaceutica; y su uso en el tratamiento de enfermedades virales. |
| US8102720B2 (en) * | 2009-02-02 | 2012-01-24 | Qualcomm Incorporated | System and method of pulse generation |
| WO2010101967A2 (en) | 2009-03-04 | 2010-09-10 | Idenix Pharmaceuticals, Inc. | Phosphothiophene and phosphothiazole hcv polymerase inhibitors |
| JP2012520884A (ja) | 2009-03-18 | 2012-09-10 | ザ ボード オブ トラスティーズ オブ ザ リランド スタンフォード ジュニア ユニバーシティー | フラビウイルス科ウイルス感染症を治療する方法および組成物 |
| TWI504598B (zh) | 2009-03-20 | 2015-10-21 | Onyx Therapeutics Inc | 結晶性三肽環氧酮蛋白酶抑制劑 |
| JP5735482B2 (ja) | 2009-03-27 | 2015-06-17 | プレシディオ ファーマシューティカルズ インコーポレイテッド | 縮合環のｃ型肝炎阻害剤 |
| EP2416772A1 (en) | 2009-04-06 | 2012-02-15 | PTC Therapeutics, Inc. | Combinations of a hcv inhibitor such as bicyclic pyrrole derivatives and a therapeutic agent |
| EP2416765B1 (en) | 2009-04-06 | 2016-03-30 | PTC Therapeutics, Inc. | Hcv inhibitor and therapeutic agent combinations |
| TW201040181A (en) | 2009-04-08 | 2010-11-16 | Idenix Pharmaceuticals Inc | Macrocyclic serine protease inhibitors |
| US8512690B2 (en) | 2009-04-10 | 2013-08-20 | Novartis Ag | Derivatised proline containing peptide compounds as protease inhibitors |
| US20110182850A1 (en) | 2009-04-10 | 2011-07-28 | Trixi Brandl | Organic compounds and their uses |
| TWI598358B (zh) | 2009-05-20 | 2017-09-11 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
| US8618076B2 (en) | 2009-05-20 | 2013-12-31 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
| US8980920B2 (en) | 2009-05-29 | 2015-03-17 | Merck Sharp & Dohme Corp. | Antiviral compounds of three linked aryl moieties to treat diseases such as hepatitis C |
| CA2769652A1 (en) | 2009-08-05 | 2011-02-10 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv |
| HRP20161025T1 (hr) | 2009-09-15 | 2016-11-04 | Taigen Biotechnology Co., Ltd. | Inhibitori proteaze hcv-a |
| US8853147B2 (en) | 2009-11-13 | 2014-10-07 | Onyx Therapeutics, Inc. | Use of peptide epoxyketones for metastasis suppression |
| US20110117055A1 (en) | 2009-11-19 | 2011-05-19 | Macdonald James E | Methods of Treating Hepatitis C Virus with Oxoacetamide Compounds |
| CA2781614A1 (en) | 2009-11-25 | 2011-06-09 | Vertex Pharmaceuticals Incorporated | 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections |
| WO2011066241A1 (en) | 2009-11-25 | 2011-06-03 | Schering Corporation | Fused tricyclic compounds and derivatives thereof useful for the treatment of viral diseases |
| TW201136942A (en) | 2009-12-18 | 2011-11-01 | Idenix Pharmaceuticals Inc | 5,5-fused arylene or heteroarylene hepatitis C virus inhibitors |
| CA2785488A1 (en) | 2009-12-22 | 2011-07-21 | Merck Sharp & Dohme Corp. | Fused tricyclic compounds and methods of use thereof for the treatment of viral diseases |
| MX2012007341A (es) | 2009-12-22 | 2012-07-20 | Cephalon Inc | Inhibidores de proteasoma y procesos para su preparacion, purificacion y uso. |
| CN102883718A (zh) | 2009-12-24 | 2013-01-16 | 顶点制药公司 | 用于治疗或预防黄病毒感染的类似物 |
| BR112012018897A2 (pt) | 2010-01-27 | 2017-10-03 | Ab Pharma Ltd | Compostos poli-heterocíclicos altamente potentes como inibidores de hcv |
| EP2536410B1 (en) | 2010-02-18 | 2015-09-23 | Merck Sharp & Dohme Corp. | Substituted pyrimidine derivatives and their use in treating viral infections |
| BR112012022060A2 (pt) | 2010-03-01 | 2018-05-08 | Onyx Therapeutics Inc | composto para a inibição de imunoproteassoma |
| WO2011112516A1 (en) | 2010-03-08 | 2011-09-15 | Ico Therapeutics Inc. | Treating and preventing hepatitis c virus infection using c-raf kinase antisense oligonucleotides |
| AU2011224698A1 (en) | 2010-03-09 | 2012-11-01 | Merck Sharp & Dohme Corp. | Fused Tricyclic Silyl Compounds and methods of use thereof for the treatment of viral diseases |
| MX2012010919A (es) | 2010-03-24 | 2013-02-01 | Vertex Pharma | Analogos para el tratamiento o prevencion de infecciones por flavivirus. |
| JP2013522375A (ja) | 2010-03-24 | 2013-06-13 | バーテックス ファーマシューティカルズ インコーポレイテッド | フラビウイルス感染を処置または予防するためのアナログ |
| TW201141857A (en) | 2010-03-24 | 2011-12-01 | Vertex Pharma | Analogues for the treatment or prevention of flavivirus infections |
| WO2011119858A1 (en) | 2010-03-24 | 2011-09-29 | Vertex Pharmaceuticals Incorporated | Analogues for the treatment or prevention of flavivirus infections |
| TW201139457A (en) | 2010-03-31 | 2011-11-16 | Pharmasset Inc | Stereoselective synthesis of phosphorus containing actives |
| BR112012024661A2 (pt) | 2010-04-01 | 2015-09-15 | Centre Nat Rech Scient | composto, composição farmacêutica e método de tratamento de um hospedeiro infectado com vírus de hepatite c |
| US8697646B2 (en) | 2010-04-07 | 2014-04-15 | Onyx Therapeutics, Inc. | Crystalline peptide epoxyketone immunoproteasome inhibitor |
| WO2011149856A1 (en) | 2010-05-24 | 2011-12-01 | Presidio Pharmaceuticals, Inc. | Inhibitors of hcv ns5a |
| WO2011156545A1 (en) | 2010-06-09 | 2011-12-15 | Vertex Pharmaceuticals Incorporated | Viral dynamic model for hcv combination therapy |
| EP2582717A2 (en) | 2010-06-15 | 2013-04-24 | Vertex Pharmaceuticals Incorporated | Hcv ns5b polymerase mutants |
| MX2012014918A (es) | 2010-06-28 | 2013-04-08 | Vertex Pharma | Compuestos y metodos para tratamiento o prevencion de infecciones por flavivirus. |
| EP2585448A1 (en) | 2010-06-28 | 2013-05-01 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| WO2012006070A1 (en) | 2010-06-28 | 2012-01-12 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| AU2011286276A1 (en) | 2010-07-26 | 2013-01-24 | Merck Sharp & Dohme Corp. | Substituted biphenylene compounds and methods of use thereof for the treatment of viral diseases |
| WO2012020036A1 (en) | 2010-08-13 | 2012-02-16 | F. Hoffmann-La Roche Ag | Hepatitis c virus inhibitors |
| MX2013001869A (es) | 2010-08-17 | 2013-06-28 | Vertex Pharma | Compuestos y metodos para el tratamiento o prevencion de infecciones virales por flaviviridae. |
| CA2812779A1 (en) | 2010-09-29 | 2012-04-19 | Merck Sharp & Dohme Corp. | Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases |
| BR112013008510A2 (pt) | 2010-10-08 | 2016-07-05 | Novartis Ag | vitamina e formulações de inibidores de sulfamida ns3 |
| WO2012061248A2 (en) | 2010-11-01 | 2012-05-10 | Rfs Pharma, Llc | Novel specific hcv ns3 protease inhibitors |
| EP3042910B1 (en) | 2010-11-30 | 2019-01-09 | Gilead Pharmasset LLC | 2'-spiro-nucleosides for use in the therapy of hepatitis c |
| WO2012109398A1 (en) | 2011-02-10 | 2012-08-16 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating hcv infections |
| WO2012107589A1 (en) | 2011-02-11 | 2012-08-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment and prevention of hcv infections |
| WO2012123298A1 (en) | 2011-03-11 | 2012-09-20 | F. Hoffmann-La Roche Ag | Antiviral compounds |
| WO2012154321A1 (en) | 2011-03-31 | 2012-11-15 | Idenix Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of viral infections |
| US20120252721A1 (en) | 2011-03-31 | 2012-10-04 | Idenix Pharmaceuticals, Inc. | Methods for treating drug-resistant hepatitis c virus infection with a 5,5-fused arylene or heteroarylene hepatitis c virus inhibitor |
| EP2697242B1 (en) | 2011-04-13 | 2018-10-03 | Merck Sharp & Dohme Corp. | 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases |
| US8957203B2 (en) | 2011-05-05 | 2015-02-17 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US10501493B2 (en) | 2011-05-27 | 2019-12-10 | Rqx Pharmaceuticals, Inc. | Broad spectrum antibiotics |
| US8691757B2 (en) | 2011-06-15 | 2014-04-08 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| CA2857705A1 (en) | 2011-06-16 | 2012-12-20 | AB Pharma Ltd. | Macrocyclic heterocyclic compounds for inhibiting hepatitis c virus and preparation and use thereof |
| CN103732242A (zh) | 2011-06-23 | 2014-04-16 | 迪格纳生物技术公司 | 用与IFN-α2b组合的IFN-α5在患者群体中治疗慢性丙型肝炎 |
| WO2012175581A1 (en) | 2011-06-24 | 2012-12-27 | F. Hoffmann-La Roche Ag | Antiviral compounds |
| CN102807607B (zh) * | 2011-07-22 | 2013-10-23 | 爱博新药研发(上海)有限公司 | 抑制丙肝病毒的稠环杂环类化合物、其中间体及其应用 |
| WO2013016490A1 (en) | 2011-07-26 | 2013-01-31 | Vertex Pharmaceuticals Incorporated | Thiophene compounds |
| WO2013016499A1 (en) | 2011-07-26 | 2013-01-31 | Vertex Pharmaceuticals Incorporated | Methods for preparation of thiophene compounds |
| WO2013033901A1 (en) | 2011-09-08 | 2013-03-14 | Merck Sharp & Dohme Corp. | Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases |
| WO2013033900A1 (en) | 2011-09-08 | 2013-03-14 | Merck Sharp & Dohme Corp. | Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases |
| WO2013033899A1 (en) | 2011-09-08 | 2013-03-14 | Merck Sharp & Dohme Corp. | Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases |
| WO2013039920A1 (en) | 2011-09-12 | 2013-03-21 | Idenix Pharmaceuticals, Inc. | Substituted carbonyloxymethylphosphoramidate compounds and pharmaceutical compositions for the treatment of viral infections |
| CA2847892A1 (en) | 2011-09-12 | 2013-03-21 | Idenix Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of viral infections |
| US20140378416A1 (en) | 2011-09-14 | 2014-12-25 | Michael P. Dwyer | Silyl-containing heterocyclic compounds and methods of use thereof for the treatment of viral diseases |
| KR101621181B1 (ko) | 2011-10-10 | 2016-05-13 | 에프. 호프만-라 로슈 아게 | 항바이러스성 화합물 |
| US8507460B2 (en) | 2011-10-14 | 2013-08-13 | Idenix Pharmaceuticals, Inc. | Substituted 3′,5′-cyclic phosphates of purine nucleotide compounds and pharmaceutical compositions for the treatment of viral infections |
| WO2013072328A1 (en) | 2011-11-14 | 2013-05-23 | Sanofi | Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases |
| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
| ES3018133T3 (en) | 2011-11-30 | 2025-05-14 | Univ Emory | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| WO2013086133A1 (en) | 2011-12-06 | 2013-06-13 | The Board Of Trustees Of The Leland Stanford Junior University | Methods and compositions for treating viral diseases |
| KR20140104030A (ko) | 2011-12-16 | 2014-08-27 | 에프. 호프만-라 로슈 아게 | Hcv ns5a의 억제제 |
| CN104011060A (zh) | 2011-12-20 | 2014-08-27 | 弗·哈夫曼-拉罗切有限公司 | 作为hcv rna复制抑制剂的4‘-叠氮基,3’-氟取代的核苷衍生物 |
| MY171577A (en) | 2011-12-20 | 2019-10-21 | Hoffmann La Roche | 2',4'-difluoro-2'-methyl substituted nucleoside derivatives as inhibitors of hcv rna replication |
| US8809354B2 (en) | 2011-12-31 | 2014-08-19 | Sheikh Riazuddin | 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone or derivatives thereof for treating or preventing antiviral infections |
| CA2858814A1 (en) | 2012-01-12 | 2013-07-18 | Rfs Pharma, Llc | Hcv ns3 protease inhibitors |
| WO2013133927A1 (en) | 2012-02-13 | 2013-09-12 | Idenix Pharmaceuticals, Inc. | Pharmaceutical compositions of 2'-c-methyl-guanosine, 5'-[2-[(3-hydroxy-2,2-dimethyl-1-oxopropyl)thio]ethyl n-(phenylmethyl)phosphoramidate] |
| CN104254518A (zh) * | 2012-02-16 | 2014-12-31 | 阿奇克斯制药公司 | 线性肽抗生素 |
| CA2857262A1 (en) * | 2012-02-24 | 2013-08-29 | F. Hoffmann-La Roche Ag | Antiviral compounds |
| EP2827876A4 (en) | 2012-03-22 | 2015-10-28 | Alios Biopharma Inc | PHARMACEUTICAL COMBINATIONS WITH A THIONUCLEOTIDE ANALOG |
| EP2852604B1 (en) | 2012-05-22 | 2017-04-12 | Idenix Pharmaceuticals LLC | 3',5'-cyclic phosphoramidate prodrugs for hcv infection |
| US9296778B2 (en) | 2012-05-22 | 2016-03-29 | Idenix Pharmaceuticals, Inc. | 3′,5′-cyclic phosphate prodrugs for HCV infection |
| JP6165848B2 (ja) | 2012-05-22 | 2017-07-19 | イデニク ファーマシューティカルズ エルエルシー | 肝疾患のためのｄ−アミノ酸化合物 |
| US20140010783A1 (en) | 2012-07-06 | 2014-01-09 | Hoffmann-La Roche Inc. | Antiviral compounds |
| TW201414751A (zh) | 2012-07-09 | 2014-04-16 | 歐尼克斯治療公司 | 肽環氧酮蛋白酶抑制劑之前驅藥物 |
| WO2014053533A1 (en) | 2012-10-05 | 2014-04-10 | Sanofi | Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation |
| MX353422B (es) | 2012-10-08 | 2018-01-12 | Idenix Pharmaceuticals Llc | Análogos de 2'-cloronucleósido para infección por vhc. |
| US20140112886A1 (en) | 2012-10-19 | 2014-04-24 | Idenix Pharmaceuticals, Inc. | Dinucleotide compounds for hcv infection |
| RS55592B1 (sr) | 2012-10-19 | 2017-06-30 | Bristol Myers Squibb Co | 9-metil supstituisani heksadekahidrociklopropa(e)pirolo(1,2-a)(1,4)diazaciklopentadecinil karbamat derivati kao nestrukturalni 3 (ns3) proteazni inhibitori za lečenje infekcijavirusom hepatitisa c |
| EP2909222B1 (en) | 2012-10-22 | 2021-05-26 | Idenix Pharmaceuticals LLC | 2',4'-bridged nucleosides for hcv infection |
| US10260089B2 (en) | 2012-10-29 | 2019-04-16 | The Research Foundation Of The State University Of New York | Compositions and methods for recognition of RNA using triple helical peptide nucleic acids |
| US9598433B2 (en) | 2012-11-02 | 2017-03-21 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2014071007A1 (en) | 2012-11-02 | 2014-05-08 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| US9643999B2 (en) | 2012-11-02 | 2017-05-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2014070974A1 (en) | 2012-11-05 | 2014-05-08 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| WO2014078436A1 (en) | 2012-11-14 | 2014-05-22 | Idenix Pharmaceuticals, Inc. | D-alanine ester of sp-nucleoside analog |
| US20140140951A1 (en) | 2012-11-14 | 2014-05-22 | Idenix Pharmaceuticals, Inc. | D-Alanine Ester of Rp-Nucleoside Analog |
| WO2014099941A1 (en) | 2012-12-19 | 2014-06-26 | Idenix Pharmaceuticals, Inc. | 4'-fluoro nucleosides for the treatment of hcv |
| BR112015017414A2 (pt) | 2013-01-23 | 2017-07-11 | Hoffmann La Roche | derivados de triazol antivirais |
| TW201526899A (zh) | 2013-02-28 | 2015-07-16 | Alios Biopharma Inc | 醫藥組成物 |
| US9339541B2 (en) | 2013-03-04 | 2016-05-17 | Merck Sharp & Dohme Corp. | Thiophosphate nucleosides for the treatment of HCV |
| WO2014137926A1 (en) | 2013-03-04 | 2014-09-12 | Idenix Pharmaceuticals, Inc. | 3'-deoxy nucleosides for the treatment of hcv |
| EP2964637B1 (en) | 2013-03-05 | 2017-04-12 | F. Hoffmann-La Roche AG | Antiviral compounds |
| WO2014137869A1 (en) | 2013-03-07 | 2014-09-12 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| EP2981542B1 (en) | 2013-04-01 | 2021-09-15 | Idenix Pharmaceuticals LLC | 2',4'-fluoro nucleosides for the treatment of hcv |
| US20180200280A1 (en) | 2013-05-16 | 2018-07-19 | Riboscience Llc | 4'-Fluoro-2'-Methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication |
| CA2912682C (en) | 2013-05-16 | 2021-07-06 | Riboscience Llc | 4'-fluoro-2'-methyl substituted nucleoside derivatives |
| SG11201509427RA (en) | 2013-05-16 | 2015-12-30 | Riboscience Llc | 4'-azido, 3'-deoxy-3'-fluoro substituted nucleoside derivatives |
| EP3004130B1 (en) | 2013-06-05 | 2019-08-07 | Idenix Pharmaceuticals LLC. | 1',4'-thio nucleosides for the treatment of hcv |
| WO2015017713A1 (en) | 2013-08-01 | 2015-02-05 | Idenix Pharmaceuticals, Inc. | D-amino acid phosphoramidate pronucleotides of halogeno pyrimidine compounds for liver disease |
| CN105636978A (zh) * | 2013-08-14 | 2016-06-01 | 阿奇克斯制药公司 | 线性肽抗生素 |
| KR102239196B1 (ko) | 2013-08-27 | 2021-04-12 | 길리애드 파마셋 엘엘씨 | 2종의 항바이러스 화합물의 조합 제제 |
| EP3046924A1 (en) | 2013-09-20 | 2016-07-27 | IDENIX Pharmaceuticals, Inc. | Hepatitis c virus inhibitors |
| WO2015061683A1 (en) | 2013-10-25 | 2015-04-30 | Idenix Pharmaceuticals, Inc. | D-amino acid phosphoramidate and d-alanine thiophosphoramidate pronucleotides of nucleoside compounds useful for the treatment of hcv |
| EP3063140A4 (en) | 2013-10-30 | 2017-11-08 | Merck Sharp & Dohme Corp. | Pseudopolymorphs of an hcv ns5a inhibitor and uses thereof |
| US20160271162A1 (en) | 2013-11-01 | 2016-09-22 | Idenix Pharmacueticals, Llc | D-alanine phosphoramide pronucleotides of 2'-methyl 2'-fluro guanosine nucleoside compounds for the treatment of hcv |
| US20170198005A1 (en) | 2013-11-27 | 2017-07-13 | Idenix Pharmaceuticals Llc | 2'-dichloro and 2'-fluoro-2'-chloro nucleoside analogues for hcv infection |
| WO2015095419A1 (en) | 2013-12-18 | 2015-06-25 | Idenix Pharmaceuticals, Inc. | 4'-or nucleosides for the treatment of hcv |
| EP2899207A1 (en) | 2014-01-28 | 2015-07-29 | Amikana.Biologics | New method for testing HCV protease inhibition |
| WO2015134561A1 (en) | 2014-03-05 | 2015-09-11 | Idenix Pharmaceuticals, Inc. | Pharmaceutical compositions comprising a 5,5-fused heteroarylene flaviviridae inhibitor and their use for treating or preventing flaviviridae infection |
| WO2015134560A1 (en) | 2014-03-05 | 2015-09-11 | Idenix Pharmaceuticals, Inc. | Solid forms of a flaviviridae virus inhibitor compound and salts thereof |
| EP3113763A1 (en) | 2014-03-05 | 2017-01-11 | Idenix Pharmaceuticals LLC | Solid prodrug forms of 2'-chloro-2'-methyl uridine for hcv |
| EP3131914B1 (en) | 2014-04-16 | 2023-05-10 | Idenix Pharmaceuticals LLC | 3'-substituted methyl or alkynyl nucleosides for the treatment of hcv |
| US11072635B2 (en) | 2015-11-20 | 2021-07-27 | Rqx Pharmaceuticals, Inc. | Macrocyclic broad spectrum antibiotics |
| US10526315B2 (en) | 2016-06-21 | 2020-01-07 | Orion Ophthalmology LLC | Carbocyclic prolinamide derivatives |
| KR102512201B1 (ko) | 2016-06-21 | 2023-03-20 | 오리온 옵탈몰로지 엘엘씨 | 지방족 프롤린아미드 유도체 |
| EP3472149B1 (en) | 2016-06-21 | 2023-08-30 | Orion Ophthalmology LLC | Heterocyclic prolinamide derivatives |
| CN109661389A (zh) * | 2016-08-23 | 2019-04-19 | 豪夫迈·罗氏有限公司 | 作为htra1抑制剂的新型二氟酮酰胺衍生物 |
| WO2018202865A1 (en) | 2017-05-05 | 2018-11-08 | Zealand Pharma A/S | Gap junction intercellular communication modulators and their use for the treatment of diabetic eye disease |
| GB2563396B (en) * | 2017-06-12 | 2020-09-23 | Ustav Organicke Chemie A Biochemie Av Cr V V I | Inhibitors of Rhomboid Intramembrane Proteases |
| EP3684374B1 (en) | 2017-09-21 | 2025-07-30 | Riboscience LLC | 4'-fluoro-2'-methyl substituted nucleoside derivatives as inhibitors of hcv rna replication |
| EP3891508A1 (en) | 2018-12-04 | 2021-10-13 | Bristol-Myers Squibb Company | Methods of analysis using in-sample calibration curve by multiple isotopologue reaction monitoring |
| US11208387B2 (en) | 2019-05-28 | 2021-12-28 | Genentech, Inc. | Macrocyclic broad spectrum antibiotics |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0195212A2 (en) * | 1985-02-04 | 1986-09-24 | Merrell Dow Pharmaceuticals Inc. | Novel peptidase inhibitors |
| EP0363284A2 (en) * | 1988-10-07 | 1990-04-11 | Merrell Pharmaceuticals Inc. | Use of peptidase inhibitors for the preparation of medicaments useful for the treatment of strokes |
| WO1995035308A1 (en) * | 1994-06-17 | 1995-12-28 | Vertex Pharmaceuticals Incorporated | INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME |
Family Cites Families (184)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3226768A1 (de) | 1981-11-05 | 1983-05-26 | Hoechst Ag, 6230 Frankfurt | Derivate der cis, endo-2-azabicyclo-(3.3.0)-octan-3-carbonsaeure, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung |
| DE3211676A1 (de) | 1982-03-30 | 1983-10-06 | Hoechst Ag | Neue derivate von cycloalka (c) pyrrol-carbonsaeuren, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung sowie neue cycloalka (c) pyrrol-carbonsaeuren als zwischenstufen und verfahren zu deren herstellung |
| US4499082A (en) | 1983-12-05 | 1985-02-12 | E. I. Du Pont De Nemours And Company | α-Aminoboronic acid peptides |
| FR2575753B1 (fr) | 1985-01-07 | 1987-02-20 | Adir | Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US5496927A (en) | 1985-02-04 | 1996-03-05 | Merrell Pharmaceuticals Inc. | Peptidase inhibitors |
| EP0204571B1 (en) | 1985-06-07 | 1992-01-22 | Ici Americas Inc. | Selected difluoro derivatives |
| US5231084A (en) | 1986-03-27 | 1993-07-27 | Hoechst Aktiengesellschaft | Compounds having a cognition adjuvant action, agents containing them, and the use thereof for the treatment and prophylaxis of cognitive dysfuncitons |
| NZ223148A (en) * | 1987-01-16 | 1989-10-27 | Merrell Dow Pharma | Peptide derivatives having peptidase inhibition activity |
| US4820691A (en) * | 1987-06-24 | 1989-04-11 | E. R. Squibb & Sons, Inc. | Amino acid 1,2-diketo derivatives as renin inhibitors |
| EP0356595A1 (en) * | 1988-09-01 | 1990-03-07 | Merrell Dow Pharmaceuticals Inc. | Novel peptidase inhibitors |
| US5736520A (en) | 1988-10-07 | 1998-04-07 | Merrell Pharmaceuticals Inc. | Peptidase inhibitors |
| EP0371179A1 (en) * | 1988-10-28 | 1990-06-06 | Merrell Dow Pharmaceuticals Inc. | Novel analogs of peptidase substrates |
| NZ235155A (en) | 1989-09-11 | 1993-04-28 | Merrell Dow Pharma | Peptidase substrates in which the carboxy terminal group has been replaced by a tricarbonyl radical |
| JPH0480541A (ja) * | 1990-07-24 | 1992-03-13 | Matsushita Seiko Co Ltd | 加湿機 |
| CA2137832C (en) * | 1992-06-12 | 2000-09-26 | Dennis J. Hoover | Inhibitors of angiotensin i chymase(s) including human heart chymase |
| US5484410A (en) * | 1992-06-24 | 1996-01-16 | Science Incorporated | Mixing and delivery system |
| US5371072A (en) | 1992-10-16 | 1994-12-06 | Corvas International, Inc. | Asp-Pro-Arg α-keto-amide enzyme inhibitors |
| ES2150933T3 (es) * | 1992-12-22 | 2000-12-16 | Lilly Co Eli | Inhibidores de la proteasa vih utiles para el tratamiento del sida. |
| JP2637847B2 (ja) | 1992-12-29 | 1997-08-06 | アボツト・ラボラトリーズ | レトロウィルス蛋白分解酵素を阻害する化合物 |
| US5384410A (en) | 1993-03-24 | 1995-01-24 | The Du Pont Merck Pharmaceutical Company | Removal of boronic acid protecting groups by transesterification |
| US5656600A (en) | 1993-03-25 | 1997-08-12 | Corvas International, Inc. | α-ketoamide derivatives as inhibitors of thrombosis |
| US5672582A (en) | 1993-04-30 | 1997-09-30 | Merck & Co., Inc. | Thrombin inhibitors |
| EP0639585A1 (en) * | 1993-08-20 | 1995-02-22 | Banyu Pharmaceutical Co., Ltd. | Elastase inhibitor |
| IL110752A (en) | 1993-09-13 | 2000-07-26 | Abbott Lab | Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor |
| US5559158A (en) | 1993-10-01 | 1996-09-24 | Abbott Laboratories | Pharmaceutical composition |
| US5468858A (en) | 1993-10-28 | 1995-11-21 | The Board Of Regents Of Oklahoma State University Physical Sciences | N-alkyl and n-acyl derivatives of 3,7-diazabicyclo-[3.3.1]nonanes and selected salts thereof as multi-class antiarrhythmic agents |
| IL111991A (en) | 1994-01-28 | 2000-07-26 | Abbott Lab | Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent |
| RU95104898A (ru) | 1994-03-31 | 1996-12-27 | Бристоль-Мейерз Сквибб Компани (US) | Имидазолсодержащие ингибиторы фарнезид-протеинтрансферазы, способ лечения связанных с ней заболеваний |
| US6420522B1 (en) | 1995-06-05 | 2002-07-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US5756466A (en) | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5847135A (en) | 1994-06-17 | 1998-12-08 | Vertex Pharmaceuticals, Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US5861267A (en) | 1995-05-01 | 1999-01-19 | Vertex Pharmaceuticals Incorporated | Methods, nucleotide sequences and host cells for assaying exogenous and endogenous protease activity |
| US6037157A (en) | 1995-06-29 | 2000-03-14 | Abbott Laboratories | Method for improving pharmacokinetics |
| AU715558B2 (en) | 1995-11-23 | 2000-02-03 | Merck Sharp & Dohme Limited | Spiro-piperidine derivatives and their use as tachykinin antagonists |
| AU728373B2 (en) | 1995-12-07 | 2001-01-11 | Scripps Research Institute, The | HIV protease inhibitors |
| US6054472A (en) | 1996-04-23 | 2000-04-25 | Vertex Pharmaceuticals, Incorporated | Inhibitors of IMPDH enzyme |
| US5807876A (en) | 1996-04-23 | 1998-09-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of IMPDH enzyme |
| ZA972195B (en) | 1996-03-15 | 1998-09-14 | Du Pont Merck Pharma | Spirocycle integrin inhibitors |
| CN1515248A (zh) | 1996-04-23 | 2004-07-28 | ��̩��˹ҩ��ɷ�����˾ | 用作肌苷-5'-一磷酸脱氢酶抑制剂的脲衍生物 |
| US5990276A (en) | 1996-05-10 | 1999-11-23 | Schering Corporation | Synthetic inhibitors of hepatitis C virus NS3 protease |
| US6153579A (en) | 1996-09-12 | 2000-11-28 | Vertex Pharmaceuticals, Incorporated | Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex |
| US6046195A (en) | 1996-09-25 | 2000-04-04 | Merck Sharp & Dohme Ltd. | Spiro-azacyclic derivatives, their preparation and their use as tachykinin antagonists |
| AU4898797A (en) | 1996-10-08 | 1998-05-05 | Colorado State University Research Foundation | Catalytic asymmetric epoxidation |
| JP4080541B2 (ja) | 1996-10-18 | 2008-04-23 | バーテックス ファーマシューティカルズ インコーポレイテッド | セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子 |
| GB9623908D0 (en) | 1996-11-18 | 1997-01-08 | Hoffmann La Roche | Amino acid derivatives |
| DE19648011A1 (de) | 1996-11-20 | 1998-05-28 | Bayer Ag | Cyclische Imine |
| DE19648793A1 (de) | 1996-11-26 | 1998-05-28 | Basf Ag | Neue Benzamide und deren Anwendung |
| DK0966465T3 (da) | 1997-03-14 | 2003-10-20 | Vertex Pharma | Inhibitorer af IMPDH-enzymer |
| GB9708484D0 (en) | 1997-04-25 | 1997-06-18 | Merck Sharp & Dohme | Therapeutic agents |
| GB9711114D0 (en) | 1997-05-29 | 1997-07-23 | Merck Sharp & Dohme | Therapeutic agents |
| NZ503263A (en) | 1997-08-11 | 2002-10-25 | Boehringer Ingelheim Ca Ltd | Hepatitis C NS3 protease inhibitor peptides and peptide analogues |
| US6767991B1 (en) | 1997-08-11 | 2004-07-27 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis C inhibitor peptides |
| US6183121B1 (en) | 1997-08-14 | 2001-02-06 | Vertex Pharmaceuticals Inc. | Hepatitis C virus helicase crystals and coordinates that define helicase binding pockets |
| US20040058982A1 (en) | 1999-02-17 | 2004-03-25 | Bioavailability System, Llc | Pharmaceutical compositions |
| US20020017295A1 (en) | 2000-07-07 | 2002-02-14 | Weers Jeffry G. | Phospholipid-based powders for inhalation |
| AU1416099A (en) | 1997-11-28 | 1999-06-16 | Schering Corporation | Single-chain recombinant complexes of hepatitis c virus ns3 protease and ns4a cofactor peptide |
| DE69934104T2 (de) | 1998-03-31 | 2007-06-28 | Vertex Pharmaceuticals Inc., Cambridge | Inhibitoren von serinproteasen, insbesondere von hepatitis c virus ns3 protease |
| US6251583B1 (en) | 1998-04-27 | 2001-06-26 | Schering Corporation | Peptide substrates for HCV NS3 protease assays |
| GB9812523D0 (en) | 1998-06-10 | 1998-08-05 | Angeletti P Ist Richerche Bio | Peptide inhibitors of hepatitis c virus ns3 protease |
| US6323180B1 (en) | 1998-08-10 | 2001-11-27 | Boehringer Ingelheim (Canada) Ltd | Hepatitis C inhibitor tri-peptides |
| DE19836514A1 (de) | 1998-08-12 | 2000-02-17 | Univ Stuttgart | Modifikation von Engineeringpolymeren mit N-basischen Gruppe und mit Ionenaustauschergruppen in der Seitenkette |
| US6117639A (en) | 1998-08-31 | 2000-09-12 | Vertex Pharmaceuticals Incorporated | Fusion proteins, DNA molecules, vectors, and host cells useful for measuring protease activity |
| US6025516A (en) | 1998-10-14 | 2000-02-15 | Chiragene, Inc. | Resolution of 2-hydroxy-3-amino-3-phenylpropionamide and its conversion to C-13 sidechain of taxanes |
| US6117870A (en) | 1998-11-12 | 2000-09-12 | Fujirebio Kabushiki Kaisha | Cyclic amide derivatives |
| DE60039377D1 (de) | 1999-02-09 | 2008-08-21 | Pfizer Prod Inc | Zusammensetzungen basischer Arzneistoffe mit verbesserter Bioverfügbarkeit |
| US20020042046A1 (en) | 1999-02-25 | 2002-04-11 | Vertex Pharmaceuticals, Incorporated | Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex |
| CN1196687C (zh) | 1999-03-19 | 2005-04-13 | 沃泰克斯药物股份有限公司 | Impdh酶抑制剂 |
| US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
| US7122627B2 (en) | 1999-07-26 | 2006-10-17 | Bristol-Myers Squibb Company | Lactam inhibitors of Hepatitis C virus NS3 protease |
| US20020183249A1 (en) | 1999-08-31 | 2002-12-05 | Taylor Neil R. | Method of identifying inhibitors of CDC25 |
| WO2001040262A1 (en) | 1999-12-03 | 2001-06-07 | Bristol-Myers Squibb Pharma Company | Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease |
| JP2003525294A (ja) | 2000-02-29 | 2003-08-26 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | Ｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害剤 |
| ES2240446T3 (es) | 2000-04-03 | 2005-10-16 | Vertex Pharma | Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c. |
| KR20030036152A (ko) | 2000-04-05 | 2003-05-09 | 쉐링 코포레이션 | Ｎ-사이클릭 ｐ2 잔기를 포함하는 ｃ형 간염 바이러스의매크로사이클릭 ｎｓ3-세린 프로테아제 억제제 |
| CN1935833A (zh) | 2000-04-19 | 2007-03-28 | 先灵公司 | 含有烷基和芳基丙氨酸p2部分的丙型肝炎病毒的大环ns3－丝氨酸蛋白酶抑制剂 |
| EP2289888A3 (en) | 2000-06-30 | 2011-07-13 | Seikagaku Corporation | Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them |
| US7244721B2 (en) | 2000-07-21 | 2007-07-17 | Schering Corporation | Peptides as NS3-serine protease inhibitors of hepatitis C virus |
| US7012066B2 (en) | 2000-07-21 | 2006-03-14 | Schering Corporation | Peptides as NS3-serine protease inhibitors of hepatitis C virus |
| AR034127A1 (es) | 2000-07-21 | 2004-02-04 | Schering Corp | Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento |
| AR029851A1 (es) | 2000-07-21 | 2003-07-16 | Dendreon Corp | Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c |
| WO2002008251A2 (en) | 2000-07-21 | 2002-01-31 | Corvas International, Inc. | Peptides as ns3-serine protease inhibitors of hepatitis c virus |
| CZ2003195A3 (cs) | 2000-07-21 | 2003-04-16 | Schering Corporation | Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostředek |
| US6777400B2 (en) | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| US6939692B2 (en) | 2000-09-12 | 2005-09-06 | Degussa Ag | Nucleotide sequences coding for the pknB gene |
| US6846806B2 (en) | 2000-10-23 | 2005-01-25 | Bristol-Myers Squibb Company | Peptide inhibitors of Hepatitis C virus NS3 protein |
| US6602718B1 (en) | 2000-11-08 | 2003-08-05 | Becton, Dickinson And Company | Method and device for collecting and stabilizing a biological sample |
| CA2429359A1 (en) | 2000-11-20 | 2002-08-08 | Bristol-Myers Squibb Company | Hepatitis c tripeptide inhibitors |
| ATE430166T1 (de) | 2000-12-12 | 2009-05-15 | Schering Corp | Diarylrest entfassende peptide als inhibitoren des ns-3 serinproteases von hepatitis c virus |
| US6653295B2 (en) | 2000-12-13 | 2003-11-25 | Bristol-Myers Squibb Company | Inhibitors of hepatitis C virus NS3 protease |
| US6727366B2 (en) | 2000-12-13 | 2004-04-27 | Bristol-Myers Squibb Pharma Company | Imidazolidinones and their related derivatives as hepatitis C virus NS3 protease inhibitors |
| JP4848528B2 (ja) | 2000-12-28 | 2011-12-28 | 株式会社Ｉｈｉ | イオン質量分離方法及び装置、並びにイオンドーピング装置 |
| ATE526339T1 (de) | 2001-01-22 | 2011-10-15 | Merck Sharp & Dohme | Nukleosidderivate als inhibitoren der rna- abhängigen viralen rna-polymerase |
| WO2002061149A2 (en) | 2001-01-30 | 2002-08-08 | Vertex Pharmaceuticals Incorporated | A quantitative assay for nucleic acids |
| GB0102342D0 (en) | 2001-01-30 | 2001-03-14 | Smithkline Beecham Plc | Pharmaceutical formulation |
| CN100362095C (zh) | 2001-03-27 | 2008-01-16 | 沃泰克斯药物股份有限公司 | 用于hcv感染的组合物和方法 |
| GB0107924D0 (en) | 2001-03-29 | 2001-05-23 | Angeletti P Ist Richerche Bio | Inhibitor of hepatitis C virus NS3 protease |
| WO2003003804A2 (en) | 2001-07-03 | 2003-01-16 | Altana Pharma Ag | Process for the production of optically active 3-phenylisoserine |
| CA2449504A1 (en) | 2001-07-11 | 2003-01-23 | Vertex Pharmaceuticals Incorporated | Bridged bicyclic serine protease inhibitors |
| JP2003055389A (ja) | 2001-08-09 | 2003-02-26 | Univ Tokyo | 錯体及びそれを用いたエポキシドの製法 |
| US6824769B2 (en) | 2001-08-28 | 2004-11-30 | Vertex Pharmaceuticals Incorporated | Optimal compositions and methods thereof for treating HCV infections |
| WO2003035060A1 (en) | 2001-10-24 | 2003-05-01 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4a protease, incorporating a fused ring system |
| IL161970A0 (en) | 2001-11-14 | 2005-11-20 | Teva Pharma | Amorphous and crystalline forms of losartion potassium and process fortheir preparation |
| CA2369711A1 (en) | 2002-01-30 | 2003-07-30 | Boehringer Ingelheim (Canada) Ltd. | Macrocyclic peptides active against the hepatitis c virus |
| CA2369970A1 (en) | 2002-02-01 | 2003-08-01 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis c inhibitor tri-peptides |
| AR038375A1 (es) | 2002-02-01 | 2005-01-12 | Pfizer Prod Inc | Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo |
| US7091184B2 (en) | 2002-02-01 | 2006-08-15 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| US6642204B2 (en) | 2002-02-01 | 2003-11-04 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| RU2004133044A (ru) | 2002-04-11 | 2006-01-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Ингибиторы сериновых протеаз, в частности, протеазы ns3-ns4a hcv |
| US7655804B2 (en) | 2002-04-25 | 2010-02-02 | Ono Pharmaceutical Co., Ltd. | Diketohydrazine derivative compounds and drugs containing the compounds as the active ingredient |
| EP1545545A4 (en) | 2002-08-01 | 2008-09-03 | Pharmasset Inc | COMPOUNDS WITH THE BICYCLO 4.2.1 NONAN SYSTEM FOR THE TREATMENT OF FLAVIVIRIDAE / I INFECTIONS |
| US20040138109A1 (en) | 2002-09-30 | 2004-07-15 | Boehringer Ingelheim Pharmaceuticals, Inc. | Potent inhibitor of HCV serine protease |
| US20050075279A1 (en) | 2002-10-25 | 2005-04-07 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis C virus |
| US20050159345A1 (en) | 2002-10-29 | 2005-07-21 | Boehringer Ingelheim International Gmbh | Composition for the treatment of infection by Flaviviridae viruses |
| CA2413705A1 (en) | 2002-12-06 | 2004-06-06 | Raul Altman | Use of meloxicam in combination with an antiplatelet agent for treatment of acute coronary syndrome and related conditions |
| US7601709B2 (en) | 2003-02-07 | 2009-10-13 | Enanta Pharmaceuticals, Inc. | Macrocyclic hepatitis C serine protease inhibitors |
| US7098231B2 (en) | 2003-01-22 | 2006-08-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
| US7223785B2 (en) | 2003-01-22 | 2007-05-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
| US20040180815A1 (en) | 2003-03-07 | 2004-09-16 | Suanne Nakajima | Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors |
| WO2004072243A2 (en) | 2003-02-07 | 2004-08-26 | Enanta Pharmaceuticals, Inc. | Macrocyclic hepatitis c serine protease inhibitors |
| BRPI0407587A (pt) | 2003-02-18 | 2006-02-14 | Pfizer | inibidores do vìrus da hepatite c, composições e tratamentos que os utilizam |
| EP1601685A1 (en) | 2003-03-05 | 2005-12-07 | Boehringer Ingelheim International GmbH | Hepatitis c inhibiting compounds |
| CA2516018C (en) | 2003-03-05 | 2011-08-23 | Boehringer Ingelheim International Gmbh | Hepatitis c inhibitor peptide analogs |
| WO2004089974A1 (en) | 2003-04-10 | 2004-10-21 | Boehringer Ingelheim International Gmbh | Process for the preparation of macrocyclic compounds by ruthenium complex catalysed metathesis reaction |
| ATE547412T1 (de) | 2003-04-11 | 2012-03-15 | Vertex Pharma | Inhibitoren von serinproteasen, insbesondere hcv- ns3-ns4a-protease |
| RS51294B (sr) | 2003-05-21 | 2010-12-31 | Boehringer Ingelheim International Gmbh. | Inhibitorna jedinjenja za hepatitis c |
| US7125845B2 (en) | 2003-07-03 | 2006-10-24 | Enanta Pharmaceuticals, Inc. | Aza-peptide macrocyclic hepatitis C serine protease inhibitors |
| NZ544789A (en) | 2003-07-18 | 2010-01-29 | Vertex Pharma | Dithia-azaspiro-nonane and decane derivatives as inhibitors of serine proteases |
| WO2005018330A1 (en) | 2003-08-18 | 2005-03-03 | Pharmasset, Inc. | Dosing regimen for flaviviridae therapy |
| TWI359147B (en) | 2003-09-05 | 2012-03-01 | Vertex Pharma | Inhibitors of serine proteases, particularly hcv n |
| JP2007505603A (ja) | 2003-09-12 | 2007-03-15 | ヴァーテックス ファーマシューティカルズ、 インコーポレイテッド | プロテアーゼ活性および肝障害のための動物モデル |
| AU2004274468B2 (en) | 2003-09-18 | 2009-07-23 | Vertex Pharmaceuticals, Incorporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| US6933760B2 (en) | 2003-09-19 | 2005-08-23 | Intel Corporation | Reference voltage generator for hysteresis circuit |
| PE20050431A1 (es) | 2003-09-22 | 2005-07-19 | Boehringer Ingelheim Int | Peptidos macrociclicos activos contra el virus de la hepatitis c |
| AR046166A1 (es) | 2003-09-26 | 2005-11-30 | Schering Corp | Inhibidores macrociclicos de la serina proteasa ns3 del virus de la hepatitis c |
| AU2004282148A1 (en) | 2003-10-10 | 2005-04-28 | Vertex Pharmaceuticals Incoporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| US7365092B2 (en) | 2003-10-10 | 2008-04-29 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| AR045870A1 (es) | 2003-10-11 | 2005-11-16 | Vertex Pharma | Terapia de combinacion para la infeccion de virus de hepatitis c |
| US8187874B2 (en) | 2003-10-27 | 2012-05-29 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
| ZA200603863B (en) | 2003-10-27 | 2007-11-28 | Vertex Pharma | Combination for HCV treatment |
| JP4890254B2 (ja) | 2003-10-27 | 2012-03-07 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｈｃｖｎｓ３−ｎｓ４ａプロテアーゼ耐性突然変異体 |
| US7250520B2 (en) | 2003-10-28 | 2007-07-31 | Vertex Pharmaceuticals Incorporated | Processes for preparing pyrroles |
| US20050119318A1 (en) | 2003-10-31 | 2005-06-02 | Hudyma Thomas W. | Inhibitors of HCV replication |
| US7132504B2 (en) | 2003-11-12 | 2006-11-07 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7253160B2 (en) | 2003-11-20 | 2007-08-07 | Schering Corporation | Depeptidized inhibitors of hepatitis C virus NS3 protease |
| US7135462B2 (en) | 2003-11-20 | 2006-11-14 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2005054450A1 (en) | 2003-12-01 | 2005-06-16 | Vertex Pharmaceuticals Incorporated | Compositions comprising fetal liver cells and methods useful for hcv infection |
| TW200518746A (en) | 2003-12-11 | 2005-06-16 | Schering Corp | Novel inhibitors of hepatitis C virus NS3/NS4A serine protease |
| CA2549851C (en) | 2004-01-21 | 2012-09-11 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis c virus |
| CN1938332B (zh) | 2004-02-04 | 2011-10-19 | 沃泰克斯药物股份有限公司 | 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂 |
| US20050187192A1 (en) | 2004-02-20 | 2005-08-25 | Kucera Pharmaceutical Company | Phospholipids for the treatment of infection by togaviruses, herpes viruses and coronaviruses |
| CN1922174A (zh) | 2004-02-20 | 2007-02-28 | 贝林格尔·英格海姆国际有限公司 | 病毒聚合酶抑制剂 |
| EP1730165A1 (en) | 2004-02-27 | 2006-12-13 | Schering Corporation | Inhibitors of hepatitis c virus ns3 protease |
| TWI314927B (en) | 2004-02-27 | 2009-09-21 | Schering Corporatio | Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease |
| ES2328589T3 (es) | 2004-02-27 | 2009-11-16 | Schering Corporation | Compuestos de la prolina 3,4(ciclopentil) fusionados como inhibidores de la proteasa serina ns3 del virus de la hepatitis c. |
| EP1730142B1 (en) | 2004-02-27 | 2011-06-29 | Schering Corporation | Novel ketoamides with cyclic p4's as inhibitors of ns3 serine protease of hepatitis c virus |
| AU2005223767B2 (en) | 2004-03-12 | 2011-12-01 | Vertex Pharmaceuticals Incorporated | Processes and intermediates for the preparation of aspartic acetal caspase inhibitors |
| US7901707B2 (en) | 2004-03-15 | 2011-03-08 | Christine Allen | Biodegradable biocompatible implant and method of manufacturing same |
| PE20060309A1 (es) | 2004-05-06 | 2006-04-13 | Schering Corp | (1r,2s,5s)-n-[(1s)-3-amino-1-(ciclobutilmetil)-2,3-dioxopropil]-3-[(2s)-2[[[(1,1-dimetiletil)amino]carbonil]amino]-3,3-dimetil-1-oxobutil]-6,6-dimetil-3-azabiciclo[3.1.o]hexan-2-carboxamida como inhibidor de la ns3/ns4a serina proteasa del virus de l |
| US7399749B2 (en) | 2004-05-20 | 2008-07-15 | Schering Corporation | Substituted prolines as inhibitors of hepatitis C virus NS3 serine protease |
| CN102512372A (zh) | 2004-06-08 | 2012-06-27 | 沃泰克斯药物股份有限公司 | 药物组合物 |
| CA2556669C (en) | 2004-06-28 | 2012-05-01 | Boehringer Ingelheim International Gmbh | Hepatitis c inhibitor peptide analogs |
| CA2538624C (en) | 2004-07-02 | 2009-03-24 | The Governors Of The University Of Alberta | Aqueous solutions containing .beta.-glucan and gums |
| JP4914355B2 (ja) | 2004-07-20 | 2012-04-11 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃ型肝炎インヒビターペプチド類似体 |
| UY29016A1 (es) | 2004-07-20 | 2006-02-24 | Boehringer Ingelheim Int | Analogos de dipeptidos inhibidores de la hepatitis c |
| MX2007002371A (es) | 2004-08-27 | 2007-04-23 | Schering Corp | Compuestos de acilsulfonamida como inhibidores de la serina proteasa ns3 del virus de la hepatitis c. |
| SG191661A1 (en) | 2004-10-01 | 2013-07-31 | Vertex Pharma | Hcv ns3-ns4a protease inhibition |
| TW201424733A (zh) | 2004-10-29 | 2014-07-01 | Vertex Pharma | 劑量型式 |
| US7863274B2 (en) | 2005-07-29 | 2011-01-04 | Concert Pharmaceuticals Inc. | Deuterium enriched analogues of tadalafil as PDE5 inhibitors |
| MX2008001528A (es) | 2005-08-02 | 2008-04-04 | Vertex Pharma | Inhibidores de serina proteasas. |
| ES2344156T3 (es) | 2005-08-19 | 2010-08-19 | Vertex Pharmaceuticals Incorporated | Procedimientos e intermedios. |
| US7964624B1 (en) | 2005-08-26 | 2011-06-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| AR055395A1 (es) | 2005-08-26 | 2007-08-22 | Vertex Pharma | Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c |
| US7705138B2 (en) | 2005-11-11 | 2010-04-27 | Vertex Pharmaceuticals Incorporated | Hepatitis C virus variants |
| JP5436864B2 (ja) | 2006-02-27 | 2014-03-05 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｖｘ−９５０を含む共結晶体およびそれを含む医薬組成物 |
| WO2007109080A2 (en) | 2006-03-16 | 2007-09-27 | Vertex Pharmaceuticals Incorporated | Deuterated hepatitis c protease inhibitors |
| WO2007109023A1 (en) | 2006-03-16 | 2007-09-27 | Vertex Pharmaceuticals Incorporated | Processes and intermediates for preparing steric compounds |
| EP2001498A4 (en) | 2006-03-20 | 2013-01-23 | Vertex Pharma | PHARMACEUTICAL COMPOSITIONS |
| SG170087A1 (en) | 2006-03-20 | 2011-04-29 | Vertex Pharma | Pharmaceutical compositions |
| US7651520B2 (en) | 2006-05-30 | 2010-01-26 | Ostial Solutions, Llc | Means and method for the accurate placement of a stent at the ostium of an artery |
| WO2007142951A2 (en) | 2006-05-31 | 2007-12-13 | Vertex Pharmaceuticals Incorporated | Oral controlled release formulations of an interleukin-1 beta converting enzyme inihibitor |
| US7708294B2 (en) | 2006-11-02 | 2010-05-04 | Gm Global Technology Operations, Inc. | Detachable dual-use platform apparatus and method |
| EP2134717A2 (en) | 2007-02-27 | 2009-12-23 | Vertex Pharmceuticals Incorporated | Inhibitors of serine proteases |
| US7959488B2 (en) | 2007-10-15 | 2011-06-14 | Tania Alessandra Talamo | Brassiere pad system |
-
1997
- 1997-10-17 JP JP51956898A patent/JP4080541B2/ja not_active Expired - Fee Related
- 1997-10-17 NZ NZ335276A patent/NZ335276A/xx not_active IP Right Cessation
- 1997-10-17 AP APAP/P/1999/001512A patent/AP1019A/en active
- 1997-10-17 PT PT97946273T patent/PT932617E/pt unknown
- 1997-10-17 MX MXPA05003026A patent/MXPA05003026A/es active IP Right Grant
- 1997-10-17 HU HU0000152A patent/HU227742B1/hu not_active IP Right Cessation
- 1997-10-17 GE GEAP19974759A patent/GEP20012471B/en unknown
- 1997-10-17 AT AT97946273T patent/ATE212037T1/de active
- 1997-10-17 CZ CZ0134099A patent/CZ298749B6/cs not_active IP Right Cessation
- 1997-10-17 UA UA20031212227A patent/UA79749C2/uk unknown
- 1997-10-17 CA CA002268391A patent/CA2268391A1/en not_active Abandoned
- 1997-10-17 TR TR1999/01602T patent/TR199901602T2/xx unknown
- 1997-10-17 IL IL12940797A patent/IL129407A0/xx unknown
- 1997-10-17 EA EA199900388A patent/EA001915B1/ru not_active IP Right Cessation
- 1997-10-17 PL PL97372333A patent/PL194025B1/pl not_active IP Right Cessation
- 1997-10-17 PL PL332872A patent/PL192280B1/pl not_active IP Right Cessation
- 1997-10-17 ZA ZA9709327A patent/ZA979327B/xx unknown
- 1997-10-17 ID IDW990198A patent/ID21649A/id unknown
- 1997-10-17 EP EP10013053A patent/EP2314598A1/en not_active Withdrawn
- 1997-10-17 DE DE69709671T patent/DE69709671T2/de not_active Expired - Lifetime
- 1997-10-17 EP EP10013054.1A patent/EP2409985A3/en not_active Withdrawn
- 1997-10-17 UA UA99042172A patent/UA66767C2/uk unknown
- 1997-10-17 CN CNB971801517A patent/CN1133649C/zh not_active Expired - Fee Related
- 1997-10-17 SK SK510-99A patent/SK286105B6/sk not_active IP Right Cessation
- 1997-10-17 KR KR10-1999-7003372A patent/KR100509388B1/ko not_active Expired - Fee Related
- 1997-10-17 EE EEP199900161A patent/EE04023B1/xx not_active IP Right Cessation
- 1997-10-17 ES ES97946273T patent/ES2169880T3/es not_active Expired - Lifetime
- 1997-10-17 WO PCT/US1997/018968 patent/WO1998017679A1/en active Application Filing
- 1997-10-17 DK DK97946273T patent/DK0932617T3/da active
- 1997-10-17 BR BRPI9712544-0B1A patent/BR9712544B1/pt not_active IP Right Cessation
- 1997-10-17 EP EP97946273A patent/EP0932617B1/en not_active Expired - Lifetime
- 1997-10-17 IN IN1951CA1997 patent/IN183120B/en unknown
- 1997-10-18 TW TW086115382A patent/TW530065B/zh not_active IP Right Cessation
-
1999
- 1999-04-13 IL IL129407A patent/IL129407A/en not_active IP Right Cessation
- 1999-04-15 IS IS5028A patent/IS5028A/is unknown
- 1999-04-16 NO NO19991832A patent/NO329751B1/no not_active IP Right Cessation
- 1999-04-16 US US09/293,247 patent/US6265380B1/en not_active Expired - Lifetime
- 1999-05-11 BG BG103392A patent/BG103392A/xx unknown
-
2001
- 2001-06-06 US US09/875,390 patent/US6617309B2/en not_active Expired - Fee Related
-
2003
- 2003-06-27 US US10/607,716 patent/US7388017B2/en not_active Expired - Fee Related
-
2007
- 2007-11-08 JP JP2007290832A patent/JP4783353B2/ja not_active Expired - Fee Related
-
2008
- 2008-02-14 US US12/031,486 patent/US8314141B2/en not_active Expired - Fee Related
- 2008-06-03 IL IL191905A patent/IL191905A0/en unknown
-
2010
- 2010-01-29 NO NO20100145A patent/NO20100145L/no not_active Application Discontinuation
- 2010-12-15 JP JP2010279518A patent/JP5301523B2/ja not_active Expired - Fee Related
-
2012
- 2012-06-27 US US13/534,531 patent/US20130012430A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0195212A2 (en) * | 1985-02-04 | 1986-09-24 | Merrell Dow Pharmaceuticals Inc. | Novel peptidase inhibitors |
| EP0363284A2 (en) * | 1988-10-07 | 1990-04-11 | Merrell Pharmaceuticals Inc. | Use of peptidase inhibitors for the preparation of medicaments useful for the treatment of strokes |
| WO1995035308A1 (en) * | 1994-06-17 | 1995-12-28 | Vertex Pharmaceuticals Incorporated | INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AP1019A (en) | Inhibitors of serinre proteases, particularly hepatitis C virus NS3 protease. | |
| CN1938332B (zh) | 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂 | |
| EP1636208B1 (en) | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease | |
| RU2440368C2 (ru) | 2-амидо-4-арилокси-1-карбонилпирролидиновые производные в качестве ингибиторов серинпротеаз, в частности протеазы ns3-ns4a hcv | |
| AU2010257200B2 (en) | Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease | |
| CN101857631A (zh) | 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂 | |
| WO2005007681A9 (en) | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease | |
| WO2005028502A1 (en) | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease | |
| ZA200401538B (en) | Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system. | |
| AU2002348414A1 (en) | Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system | |
| ZA200408243B (en) | Inhibitors of serine proteases, particularly hepatitus C virus NS3-NS4 protease | |
| EP1136498A1 (en) | Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease | |
| ZA200309156B (en) | Bridged bicyclic serine protease inhibitors. Bridged bicyclic serine protease inhibitors. | |
| HK1144824A (zh) | 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂 | |
| HK1098164B (en) | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease | |
| AU2012202822A1 (en) | Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease | |
| HK1023779B (en) | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease | |
| AU2011250779A1 (en) | Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease |