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
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- 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
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- 108010006035 Metalloproteases Proteins 0.000 description 2
- 108060004795 Methyltransferase Proteins 0.000 description 2
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- 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
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- 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
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
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- 229960000329 ribavirin Drugs 0.000 description 2
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- 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
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- 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
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- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
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- 238000012512 characterization method Methods 0.000 description 1
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- 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
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- 125000000392 cycloalkenyl group Chemical group 0.000 description 1
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- 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
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- DEZRYPDIMOWBDS-UHFFFAOYSA-N dcm dichloromethane Chemical compound ClCCl.ClCCl DEZRYPDIMOWBDS-UHFFFAOYSA-N 0.000 description 1
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- 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
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- 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
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- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 description 1
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- 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
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- 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)
| Country | Link |
|---|---|
| US (5) | US6265380B1 (2) |
| EP (3) | EP0932617B1 (2) |
| JP (3) | JP4080541B2 (2) |
| KR (1) | KR100509388B1 (2) |
| CN (1) | CN1133649C (2) |
| AP (1) | AP1019A (2) |
| AT (1) | ATE212037T1 (2) |
| BG (1) | BG103392A (2) |
| BR (1) | BR9712544B1 (2) |
| CA (1) | CA2268391A1 (2) |
| CZ (1) | CZ298749B6 (2) |
| DE (1) | DE69709671T2 (2) |
| DK (1) | DK0932617T3 (2) |
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| EE (1) | EE04023B1 (2) |
| ES (1) | ES2169880T3 (2) |
| GE (1) | GEP20012471B (2) |
| HU (1) | HU227742B1 (2) |
| ID (1) | ID21649A (2) |
| IL (3) | IL129407A0 (2) |
| IN (1) | IN183120B (2) |
| IS (1) | IS5028A (2) |
| MX (1) | MXPA05003026A (2) |
| NO (2) | NO329751B1 (2) |
| NZ (1) | NZ335276A (2) |
| PL (2) | PL194025B1 (2) |
| PT (1) | PT932617E (2) |
| SK (1) | SK286105B6 (2) |
| TR (1) | TR199901602T2 (2) |
| TW (1) | TW530065B (2) |
| UA (2) | UA79749C2 (2) |
| WO (1) | WO1998017679A1 (2) |
| ZA (1) | ZA979327B (2) |
Families Citing this family (354)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1852121A3 (en) | 1994-08-29 | 2007-11-21 | Wake Forest University | Lipid analogs for treating viral infections |
| US7135584B2 (en) | 1995-08-07 | 2006-11-14 | Wake Forest University | Lipid analogs for treating viral infections |
| PL194025B1 (pl) | 1996-10-18 | 2007-04-30 | Vertex Pharma | Inhibitory proteaz serynowych, a zwłaszcza proteazy wirusa NS3 zapalenia wątroby C, kompozycja farmaceutyczna i zastosowanie inhibitorów proteaz serynowych |
| GB9707659D0 (en) * | 1997-04-16 | 1997-06-04 | Peptide Therapeutics Ltd | Hepatitis C NS3 Protease inhibitors |
| PT1003775E (pt) * | 1997-08-11 | 2005-07-29 | Boehringer Ingelheim Ca Ltd | Peptidos inibidores da hepatite c |
| EP1012180B1 (en) * | 1997-08-11 | 2004-12-01 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis c inhibitor peptide analogues |
| US6767991B1 (en) | 1997-08-11 | 2004-07-27 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis C inhibitor peptides |
| GB9806815D0 (en) * | 1998-03-30 | 1998-05-27 | Hoffmann La Roche | Amino acid derivatives |
| DK1066247T3 (da) * | 1998-03-31 | 2007-04-02 | Vertex Pharma | Inhibitorer af serinproteaser, især 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 |
| AR022061A1 (es) * | 1998-08-10 | 2002-09-04 | Boehringer Ingelheim Ca Ltd | Peptidos inhibidores de la hepatitis c, una composicion farmaceutica que los contiene, el uso de los mismos para preparar una composicion farmaceutica, el uso de un producto intermedio para la preparacion de estos peptidos y un procedimiento para la preparacion de un peptido analogo de los mismos. |
| US6323180B1 (en) | 1998-08-10 | 2001-11-27 | Boehringer Ingelheim (Canada) Ltd | Hepatitis C inhibitor tri-peptides |
| WO2000051998A1 (en) | 1999-03-02 | 2000-09-08 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compounds useful as reversible inhibitors of cathepsin s |
| US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
| 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 |
| CA2376965A1 (en) * | 1999-07-07 | 2001-01-11 | Timothy Patrick Forsyth | Peptide boronic acid inhibitors of hepatitis c virus protease |
| EP1206449A1 (en) * | 1999-07-26 | 2002-05-22 | Bristol-Myers Squibb 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 |
| EP1252178A1 (en) | 1999-12-03 | 2002-10-30 | Bristol-Myers Squibb Pharma Company | Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease |
| AU783095B2 (en) * | 1999-12-07 | 2005-09-22 | Theravance Biopharma R&D Ip, Llc | Carbamate derivatives having muscarinic receptor antagonist activity |
| WO2001064678A2 (en) * | 2000-02-29 | 2001-09-07 | Bristol-Myers Squibb Pharma Company | Inhibitors of hepatitis c virus ns3 protease |
| AU2001251165A1 (en) * | 2000-04-03 | 2001-10-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
| AU2006202124B2 (en) * | 2000-04-03 | 2010-01-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of Serine Proteases, Particularly Hepatitis C Virus NS3 Protease |
| US6846802B2 (en) | 2000-04-05 | 2005-01-25 | Schering Corporation | Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties |
| CA2406532A1 (en) | 2000-04-19 | 2001-11-01 | Schering Corporation | Macrocyclic ns-3 serine protease inhibitors of hepatitis c virus compri sing alkyl and aryl alanine p2 moieties |
| PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
| PY0111577A (es) | 2000-05-23 | 2017-01-02 | Idenix Cayman Ltd | Métodos y composiciones para el tratamiento del virus de la hepatitis c |
| BR0111196A (pt) | 2000-05-26 | 2004-04-06 | Idenix Cayman Ltd | Composições e uso das mesmas para tratamento de flavivìrus e pestivìrus |
| 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 |
| US7244721B2 (en) | 2000-07-21 | 2007-07-17 | Schering Corporation | Peptides as NS3-serine protease inhibitors of hepatitis C virus |
| SK288064B6 (sk) * | 2000-07-21 | 2013-04-03 | Merck Sharp & Dohme Corp. | Peptide compounds, pharmaceutical compositions comprising them and their use |
| BR0112666A (pt) * | 2000-07-21 | 2003-06-10 | Schering Corp | Peptìdeos como inibidores de ns3-serina protease de vìrus da hepatite c |
| 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 |
| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| US20040106539A1 (en) * | 2000-10-12 | 2004-06-03 | Ulrich Schubert | Agents for the treatment of viral infections |
| CN101862345B (zh) | 2000-10-18 | 2014-06-04 | 吉利德制药有限责任公司 | 用于治疗病毒感染和异常细胞增殖的修饰核苷类化合物 |
| 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 |
| US6911428B2 (en) * | 2000-12-12 | 2005-06-28 | Schering Corporation | Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus |
| AU2002230764A1 (en) | 2000-12-13 | 2002-06-24 | 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 |
| IL156641A0 (en) | 2001-01-22 | 2004-01-04 | Merck & Co Inc | Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase |
| US6909000B2 (en) | 2001-07-11 | 2005-06-21 | Vertex Pharmaceuticals Incorporated | Bridged bicyclic serine protease inhibitors |
| EP1423976A1 (en) | 2001-08-31 | 2004-06-02 | Thomson Licensing S.A. | Sequence counter for an audio visual stream |
| JP2005504087A (ja) | 2001-09-28 | 2005-02-10 | イデニクス(ケイマン)リミテツド | 4’が修飾されたヌクレオシドを使用するc型肝炎ウイルス治療のための方法および組成物 |
| EP2402009A1 (en) | 2001-10-24 | 2012-01-04 | 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 |
| MXPA04007163A (es) | 2002-01-23 | 2004-10-29 | Schering Corp | Compuestos de prolina como inhibidores de la proteasa serina ns3 para utilizarse en el tratamiento de la infeccion por el virus de la hepatitis c. |
| US7119072B2 (en) | 2002-01-30 | 2006-10-10 | Boehringer Ingelheim (Canada) Ltd. | Macrocyclic peptides active against the hepatitis C virus |
| US6642204B2 (en) | 2002-02-01 | 2003-11-04 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| US7091184B2 (en) | 2002-02-01 | 2006-08-15 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| TW200403236A (en) | 2002-04-11 | 2004-03-01 | Vertex Pharma | Inhibitors or serine proteases, particularly HCV NS3-NS4A protease |
| EP1506172B1 (en) * | 2002-05-20 | 2011-03-30 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| US6878722B2 (en) | 2002-05-20 | 2005-04-12 | Bristol-Myers Squibb Company | Substituted cycloalkyl P1′ hepatitis C virus inhibitors |
| WO2003099316A1 (en) | 2002-05-20 | 2003-12-04 | Bristol-Myers Squibb Company | Heterocyclicsulfonamide hepatitis c virus inhibitors |
| MY140680A (en) | 2002-05-20 | 2010-01-15 | Bristol Myers Squibb Co | Hepatitis c virus inhibitors |
| CN104193791A (zh) | 2002-06-28 | 2014-12-10 | 埃迪尼克斯医药公司 | 用于治疗黄病毒感染的修饰的2’和3’-核苷前药 |
| WO2004026896A2 (en) * | 2002-09-23 | 2004-04-01 | 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 |
| RU2005118421A (ru) | 2002-11-15 | 2006-01-20 | Айденикс (Кайман) Лимитед (Ky) | 2'-разветвленные нуклеозиды и мутация flaviviridae |
| TW200510391A (en) * | 2003-04-11 | 2005-03-16 | Vertex Pharma | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| 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 |
| NZ544076A (en) | 2003-05-21 | 2009-04-30 | Boehringer Ingelheim Int | Hepatitis C inhibitor compounds |
| WO2005003147A2 (en) | 2003-05-30 | 2005-01-13 | Pharmasset, Inc. | Modified fluorinated nucleoside analogues |
| EP1646642A2 (en) * | 2003-07-18 | 2006-04-19 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
| AU2004258750A1 (en) | 2003-07-25 | 2005-02-03 | Centre National De La Recherche Scientifique -Cnrs | Purine nucleoside analogues for treating diseases caused by flaviviridae including 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 |
| EP1664090A2 (en) | 2003-08-26 | 2006-06-07 | Schering Corporation | Novel peptidomimetic ns3-serine protease inhibitors of hepatitis c virus |
| PE20050374A1 (es) * | 2003-09-05 | 2005-05-30 | Vertex Pharma | Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc |
| WO2005028502A1 (en) * | 2003-09-18 | 2005-03-31 | Vertex Pharmaceuticals, Incorporated | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
| JP4704342B2 (ja) | 2003-09-22 | 2011-06-15 | 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型肝炎ウイルスに対し活性な大環状ペプチド |
| US7592419B2 (en) | 2003-09-26 | 2009-09-22 | Schering Corporation | Macrocyclic inhibitors of hepatitis C virus NS3-serine protease |
| MXPA06004006A (es) * | 2003-10-10 | 2006-06-28 | Vertex Pharma | Inhibidores de serina proteasas, especialmente de ns3-ns4a proteasa del virus de la hepatitis c. |
| TW201245229A (en) | 2003-10-14 | 2012-11-16 | Hoffmann La Roche | Macrocyclic carboxylic acids and acylsulfonamides as inhibitors of HCV replication |
| EP1678202B1 (en) | 2003-10-27 | 2012-06-13 | Vertex Pharmaceuticals Incorporated | Hcv ns3-ns4a protease resistance mutants |
| WO2005043118A2 (en) | 2003-10-27 | 2005-05-12 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
| EP1944042A1 (en) | 2003-10-27 | 2008-07-16 | Vertex Pharmceuticals Incorporated | Combinations for HCV treatment |
| US7132504B2 (en) | 2003-11-12 | 2006-11-07 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| JP2007532479A (ja) | 2003-11-20 | 2007-11-15 | シェーリング コーポレイション | C型肝炎ウイルスns3プロテアーゼの脱ペプチド化インヒビター |
| US7135462B2 (en) | 2003-11-20 | 2006-11-14 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7309708B2 (en) | 2003-11-20 | 2007-12-18 | Birstol-Myers Squibb Company | Hepatitis C virus inhibitors |
| GB0500020D0 (en) | 2005-01-04 | 2005-02-09 | Novartis Ag | Organic compounds |
| WO2005070955A1 (en) | 2004-01-21 | 2005-08-04 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis c virus |
| DE602005017582D1 (en) * | 2004-01-30 | 2009-12-24 | Medivir Ab | Hcv ns-3 serine protease inhibitoren |
| EP2311851A3 (en) | 2004-02-04 | 2011-05-25 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| RS50815B (sr) | 2004-02-24 | 2010-08-31 | Japan Tobacco Inc. | Kondenzovana heterotetraciklična jedinjenja i njihova upotreba kao inhibitora hcv polimeraza |
| US20070049593A1 (en) | 2004-02-24 | 2007-03-01 | Japan Tobacco Inc. | Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor |
| US7816326B2 (en) | 2004-02-27 | 2010-10-19 | Schering Corporation | Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease |
| WO2005087721A2 (en) | 2004-02-27 | 2005-09-22 | Schering Corporation | Compounds as inhibitors of hepatitis c virus ns3 serine protease |
| TW200536528A (en) | 2004-02-27 | 2005-11-16 | Schering Corp | Novel inhibitors of hepatitis C virus NS3 protease |
| KR20130018418A (ko) | 2004-02-27 | 2013-02-21 | 머크 샤프 앤드 돔 코포레이션 | C형 간염 바이러스 ns3 세린 프로테아제의 억제제로서의 황 화합물 |
| RU2006134002A (ru) | 2004-02-27 | 2008-04-10 | Шеринг Корпорейшн (US) | Новые соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с |
| PT2399916E (pt) * | 2004-03-12 | 2015-03-17 | Vertex Pharma | Processo e intermediários para a preparação de inibidores de caspase de acetal de ácido aspártico |
| CN103554222A (zh) | 2004-04-15 | 2014-02-05 | 欧尼斯治疗公司 | 用于抑制蛋白酶体酶的化合物 |
| US8198270B2 (en) * | 2004-04-15 | 2012-06-12 | Onyx Therapeutics, Inc. | Compounds for proteasome enzyme inhibition |
| ES2510840T3 (es) * | 2004-05-10 | 2014-10-21 | Onyx Therapeutics, Inc. | Compuestos para la inhibición enzimática del proteosoma |
| US7399749B2 (en) | 2004-05-20 | 2008-07-15 | Schering Corporation | Substituted prolines as inhibitors of hepatitis C virus NS3 serine protease |
| US20080311077A1 (en) * | 2004-07-16 | 2008-12-18 | Kleem Chaudhary | Antiviral Compounds |
| CA2573346C (en) | 2004-07-20 | 2011-09-20 | Boehringer Ingelheim International Gmbh | Hepatitis c inhibitor peptide analogs |
| UY29016A1 (es) | 2004-07-20 | 2006-02-24 | Boehringer Ingelheim Int | Analogos de dipeptidos inhibidores de la hepatitis c |
| 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 |
| US7597884B2 (en) | 2004-08-09 | 2009-10-06 | Alios Biopharma, Inc. | Hyperglycosylated polypeptide variants and methods of use |
| JP2008513356A (ja) * | 2004-08-09 | 2008-05-01 | アリオス バイオファーマ インク. | 合成高度糖鎖付加プロテアーゼ耐性ポリペプチド変異体、それを使用する経口製剤および方法 |
| WO2006026352A1 (en) | 2004-08-27 | 2006-03-09 | Schering Corporation | Acylsulfonamide compounds as inhibitors of hepatitis c virus ns3 serine protease |
| MX2007003085A (es) | 2004-09-14 | 2007-08-02 | Pharmasset Inc | Preparacion de 2'-fluoro-2'-alquilo sustituido u otras ribofuranosil pirimidinas y purinas opcionalmente sustituidas y sus derivados. |
| 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 |
| CA2607359C (en) | 2005-05-13 | 2011-08-09 | Virochem Pharma Inc. | Compounds and methods for the treatment or prevention of flavivirus infections |
| WO2006127289A1 (en) * | 2005-05-20 | 2006-11-30 | Valeant Research & Development | Treatment of hcv with subtherapeutic doses of ribavirin |
| WO2006130666A2 (en) * | 2005-06-02 | 2006-12-07 | Schering Corporation | Medicaments and methods combining a hcv protease inhibitor and an akr competitor |
| EP1891089B1 (en) | 2005-06-02 | 2014-11-05 | Merck Sharp & Dohme Corp. | HCV protease inhibitors in combination with food |
| US20070237818A1 (en) * | 2005-06-02 | 2007-10-11 | Malcolm Bruce A | Controlled-release formulation of HCV protease inhibitor and methods using the same |
| KR20080021634A (ko) | 2005-06-02 | 2008-03-07 | 쉐링 코포레이션 | 약제학적 조성물 및 이를 사용한 치료 방법 |
| ATE524183T1 (de) | 2005-06-17 | 2011-09-15 | Novartis Ag | Verwendung von sanglifehrin bei der hcv-therapie |
| 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 |
| EA019888B1 (ru) | 2005-07-25 | 2014-07-30 | Интермьюн, Инк. | Промежуточное соединение для получения макроциклических ингибиторов репликации вируса гепатита с и способ его синтеза |
| PE20070210A1 (es) | 2005-07-29 | 2007-04-16 | Tibotec Pharm Ltd | Compuestos macrociclicos como inhibidores del virus de hepatitis c |
| MY142972A (en) | 2005-07-29 | 2011-01-31 | Tibotec Pharm Ltd | Macrocyclic inhibitors of hepatitis c virus |
| EP1912997B1 (en) | 2005-07-29 | 2011-09-14 | Tibotec Pharmaceuticals | 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 |
| JP5230415B2 (ja) | 2005-07-29 | 2013-07-10 | テイボテク・フアーマシユーチカルズ | C型肝炎ウイルスの大員環状阻害剤 |
| JO2768B1 (en) | 2005-07-29 | 2014-03-15 | تيبوتيك فارماسيوتيكالز ليمتد | Large cyclic inhibitors of hepatitis C virus |
| WO2007014921A1 (en) | 2005-07-29 | 2007-02-08 | Tibotec Pharmaceuticals Ltd. | Macrocyclic inhibitors of hepatitis c virus |
| MY144607A (en) | 2005-07-29 | 2011-10-14 | Tibotec Pharm Ltd | Macrocylic inhibitors of hepatitis c virus |
| TWI383980B (zh) | 2005-07-29 | 2013-02-01 | Tibotec Pharm Ltd | C型肝炎病毒之大環抑制劑 |
| EP1915382A2 (en) * | 2005-08-01 | 2008-04-30 | Phenomix Corporation | Hepatitis c serine protease inhibitors and uses therefor |
| WO2007016589A2 (en) * | 2005-08-02 | 2007-02-08 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| EP2194043B1 (en) | 2005-08-19 | 2013-12-25 | Vertex Pharmaceuticals Incorporated | Processes |
| US8399615B2 (en) | 2005-08-19 | 2013-03-19 | Vertex Pharmaceuticals Incorporated | Processes and intermediates |
| 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 |
| US7964624B1 (en) | 2005-08-26 | 2011-06-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| ATE493409T1 (de) | 2005-10-11 | 2011-01-15 | Intermune Inc | Verbindungen und verfahren zur inhibierung der replikation des hepatitis-c-virus |
| JP2009513576A (ja) * | 2005-10-11 | 2009-04-02 | インターミューン・インコーポレーテッド | ウィルス複製のインヒビター |
| 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 |
| JP5436860B2 (ja) * | 2005-11-09 | 2014-03-05 | オニキス セラピューティクス, インク. | 酵素阻害のための化合物 |
| US7705138B2 (en) | 2005-11-11 | 2010-04-27 | Vertex Pharmaceuticals Incorporated | Hepatitis C virus variants |
| EP1951748B1 (en) | 2005-11-11 | 2013-07-24 | Vertex Pharmaceuticals, Inc. | Hepatitis c virus variants |
| EP2386539B1 (en) * | 2005-12-23 | 2016-07-20 | Zealand Pharma A/S | 4-Aminoproline derivatives useful as lysine mimetics |
| JP2009524681A (ja) * | 2006-01-27 | 2009-07-02 | フェノミックス コーポレーション | C型肝炎ウイルスセリンプロテアーゼインヒビターおよびそのための使用 |
| JP2009526070A (ja) * | 2006-02-09 | 2009-07-16 | シェーリング コーポレイション | Hcvプロテアーゼ阻害薬とhcvポリメラーゼ阻害薬との組み合わせ、ならびにそれらに関連する処置の方法 |
| US8039475B2 (en) | 2006-02-27 | 2011-10-18 | Vertex Pharmaceuticals Incorporated | Co-crystals and pharmaceutical compositions comprising the same |
| WO2007109080A2 (en) * | 2006-03-16 | 2007-09-27 | Vertex Pharmaceuticals Incorporated | Deuterated hepatitis c protease inhibitors |
| RU2448976C2 (ru) | 2006-04-11 | 2012-04-27 | Новартис Аг | Ингибиторы hcv/вич и их применение |
| US8017612B2 (en) | 2006-04-18 | 2011-09-13 | Japan Tobacco Inc. | Piperazine compound and use thereof as a HCV polymerase inhibitor |
| MX2008014839A (es) | 2006-05-23 | 2008-12-05 | Irm Llc | Compuestos y composiciones en la forma de inhibidores de proteasa de activacion mediante canal. |
| 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 |
| CA2666814A1 (en) * | 2006-08-21 | 2008-05-29 | United Therapeutics Corporation | Combination therapy for treatment of viral infections |
| 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 |
| CN101568538B (zh) | 2006-11-15 | 2012-09-05 | Viro化学制药公司 | 用于治疗或预防黄病毒属感染的噻吩类似物 |
| US7763584B2 (en) | 2006-11-16 | 2010-07-27 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| 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 |
| EP2099430A2 (en) * | 2006-12-07 | 2009-09-16 | Schering Corporation | Ph sensitive matrix formulation |
| DK2468724T3 (en) | 2006-12-21 | 2016-02-22 | Zealand Pharma As | 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 |
| CA2673254C (en) | 2006-12-22 | 2013-09-10 | Schering Corporation | 4,5-ring annulated indole derivatives for treating or preventing of hcv and related viral infections |
| JP5079818B2 (ja) | 2006-12-22 | 2012-11-21 | メルク・シャープ・アンド・ドーム・コーポレーション | Hcvおよび関連するウイルス疾患の治療または予防のための4,5−環インドール誘導体 |
| EP2118091B1 (en) | 2007-02-08 | 2015-04-15 | Janssen Sciences Ireland UC | Pyrimidine substituted macrocyclic hcv inhibitors |
| EA016327B1 (ru) * | 2007-02-09 | 2012-04-30 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы |
| US8759353B2 (en) * | 2007-02-27 | 2014-06-24 | Vertex Pharmaceuticals Incorporated | Co-crystals and pharmaceutical compositions comprising the same |
| WO2008106058A2 (en) | 2007-02-27 | 2008-09-04 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| HRP20110713T1 (hr) * | 2007-02-28 | 2011-11-30 | Conatus Pharmaceuticals | Postupci liječenja kroničnog virusnog hepatitisa c uz upotrebu ro 113-0830 |
| 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 |
| JP2010526143A (ja) | 2007-05-04 | 2010-07-29 | 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 | Hcv感染の処置のための併用療法 |
| SG182979A1 (en) | 2007-06-29 | 2012-08-30 | Gilead Sciences Inc | Antiviral compounds |
| CA2691442C (en) | 2007-06-29 | 2014-01-21 | Gilead Sciences, Inc. | Antiviral compounds |
| PE20090994A1 (es) | 2007-08-29 | 2009-08-03 | Schering Corp | Derivados de azaindol 2,3-sustituidos como agentes antivirales |
| AU2008295484B2 (en) | 2007-08-29 | 2013-09-26 | Merck Sharp & Dohme Llc | Substituted indole derivatives and methods of use thereof |
| CN101842353A (zh) | 2007-08-29 | 2010-09-22 | 先灵公司 | 用于治疗病毒感染的2,3-取代的吲哚衍生物 |
| AU2008297015B2 (en) * | 2007-08-30 | 2013-08-22 | Vertex Pharmaceuticals 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 |
| KR20150131405A (ko) * | 2007-10-04 | 2015-11-24 | 오닉스 세라퓨틱스, 인크. | 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성 |
| EP2222660B1 (en) | 2007-11-16 | 2014-03-26 | Merck Sharp & Dohme Corp. | 3-heterocyclic substituted indole derivatives and methods of use thereof |
| JP5416708B2 (ja) | 2007-11-16 | 2014-02-12 | メルク・シャープ・アンド・ドーム・コーポレーション | 3−アミノスルホニル置換インドール誘導体およびそれらの使用方法 |
| 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 |
| BRPI0908021A2 (pt) | 2008-02-04 | 2015-07-21 | Idenix Pharmaceuticals Inc | Composto, composição farmacêutica, e, usos do composto ou da composição farmacêutica |
| 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 |
| US8044023B2 (en) | 2008-05-29 | 2011-10-25 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7964560B2 (en) | 2008-05-29 | 2011-06-21 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2009152200A1 (en) | 2008-06-13 | 2009-12-17 | Schering Corporation | Tricyclic indole derivatives and methods of use thereof |
| CN102177172A (zh) | 2008-07-02 | 2011-09-07 | 埃迪尼克斯医药公司 | 用于治疗病毒感染的化合物和药物组合物 |
| AR072937A1 (es) | 2008-08-20 | 2010-09-29 | Schering Corp | Derivados de piridina y pirimidina sustituida y su uso en el tratamiento de infecciones virales |
| AU2009282574B2 (en) | 2008-08-20 | 2014-08-21 | Merck Sharp & Dohme Corp. | Ethenyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| JP5654990B2 (ja) | 2008-08-20 | 2015-01-14 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | アゾ置換ピリジンおよびピリミジン誘導体ならびにそれらのウイルス感染の治療における使用 |
| JP5674661B2 (ja) | 2008-08-20 | 2015-02-25 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | エチニル置換ピリジンおよびピリミジン誘導体ならびにそれらのウイルス感染の治療における使用 |
| US8207341B2 (en) | 2008-09-04 | 2012-06-26 | Bristol-Myers Squibb Company | Process or synthesizing substituted isoquinolines |
| US8563505B2 (en) | 2008-09-29 | 2013-10-22 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US8044087B2 (en) | 2008-09-29 | 2011-10-25 | 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 |
| JP5675629B2 (ja) | 2008-10-21 | 2015-02-25 | オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. | ペプチドエポキシケトンを用いた併用療法 |
| WO2010065681A1 (en) | 2008-12-03 | 2010-06-10 | Presidio Pharmaceuticals, Inc. | Inhibitors of hcv ns5a |
| AU2009322393B2 (en) | 2008-12-03 | 2017-02-02 | Presidio Pharmaceuticals, Inc. | Inhibitors of HCV NS5A |
| 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 |
| CN102300871A (zh) * | 2008-12-19 | 2011-12-28 | 吉里德科学公司 | Hcv ns3蛋白酶抑制剂 |
| WO2010075554A1 (en) | 2008-12-23 | 2010-07-01 | Pharmasset, Inc. | Synthesis of purine nucleosides |
| AR074897A1 (es) | 2008-12-23 | 2011-02-23 | Pharmasset Inc | Fosforamidatos de nucleosidos |
| WO2010075517A2 (en) | 2008-12-23 | 2010-07-01 | Pharmasset, Inc. | Nucleoside analogs |
| US8102720B2 (en) * | 2009-02-02 | 2012-01-24 | Qualcomm Incorporated | System and method of pulse generation |
| EP2403860B1 (en) | 2009-03-04 | 2015-11-04 | IDENIX Pharmaceuticals, Inc. | Phosphothiophene and phosphothiazole as hcv polymerase inhibitors |
| CN102448458B (zh) | 2009-03-18 | 2015-07-22 | 小利兰·斯坦福大学理事会 | 治疗黄病毒科病毒感染的方法和组合物 |
| AR075899A1 (es) | 2009-03-20 | 2011-05-04 | Onyx Therapeutics Inc | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa |
| MX2011010132A (es) | 2009-03-27 | 2011-10-14 | Presidio Pharmaceuticals Inc | Inhibidores de anillo fusionado de hepatitis c. |
| EP2416765B1 (en) | 2009-04-06 | 2016-03-30 | PTC Therapeutics, Inc. | Hcv inhibitor and therapeutic agent combinations |
| US9198907B2 (en) | 2009-04-06 | 2015-12-01 | Ptc Therapeutics, Inc. | Combinations of a HCV inhibitor such as bicyclic pyrrole derivatives and a therapeutic agent |
| JP2012523419A (ja) | 2009-04-08 | 2012-10-04 | イデニク プハルマセウティカルス,インコーポレイテッド | 大環状セリンプロテアーゼ阻害剤 |
| US20110182850A1 (en) | 2009-04-10 | 2011-07-28 | Trixi Brandl | Organic compounds and their uses |
| US8512690B2 (en) | 2009-04-10 | 2013-08-20 | Novartis Ag | Derivatised proline containing peptide compounds as protease inhibitors |
| TWI583692B (zh) | 2009-05-20 | 2017-05-21 | 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 |
| EP2435424B1 (en) | 2009-05-29 | 2015-01-21 | Merck Sharp & Dohme Corp. | Antiviral compounds composed of three linked aryl moieties to treat diseases such as hepatitis c |
| US9284307B2 (en) | 2009-08-05 | 2016-03-15 | Idenix Pharmaceuticals Llc | Macrocyclic serine protease inhibitors |
| CA2774145C (en) | 2009-09-15 | 2015-10-27 | Taigen Biotechnology Co., Ltd. | Hcv protease inhibitors |
| WO2011060179A1 (en) | 2009-11-13 | 2011-05-19 | 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 |
| MX2012006026A (es) | 2009-11-25 | 2012-08-15 | Vertex Pharma | Derivados de acido 5-alquinil-tiofen-2-carboxilico y usos para tratamiento o prevencion de infecciones por flavivirus. |
| EP2503881B1 (en) | 2009-11-25 | 2015-05-13 | Merck Sharp & Dohme Corp. | Fused tricyclic compounds and derivatives thereof useful for the treatment of viral diseases |
| CA2784748A1 (en) | 2009-12-18 | 2011-06-23 | Idenix Pharmaceuticals, Inc. | 5,5-fused arylene or heteroarylene hepatitis c virus inhibitors |
| AU2010341537A1 (en) | 2009-12-22 | 2012-08-09 | Merck Sharp & Dohme Corp. | Fused Tricyclic Compounds and methods of use thereof for the treatment of viral diseases |
| CA2785300A1 (en) | 2009-12-22 | 2011-07-21 | Cephalon, Inc. | Proteasome inhibitors and processes for their preparation, purification and use |
| 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 |
| JP5833022B2 (ja) | 2010-01-27 | 2015-12-16 | エービー・ファーマ・リミテッド | C型肝炎ウィルス阻害剤としてのポリ複素環式化合物 |
| US9433621B2 (en) | 2010-02-18 | 2016-09-06 | Merck Sharp & Dohme Corp. | Substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| CA2791651C (en) | 2010-03-01 | 2019-08-20 | Onyx Therapeutics, Inc. | Compounds for immunoproteasome inhibition |
| WO2011112516A1 (en) | 2010-03-08 | 2011-09-15 | Ico Therapeutics Inc. | Treating and preventing hepatitis c virus infection using c-raf kinase antisense oligonucleotides |
| JP2013522202A (ja) | 2010-03-09 | 2013-06-13 | メルク・シャープ・エンド・ドーム・コーポレイション | 縮合三環式シリル化合物およびウイルス疾患の治療のためのその使用方法 |
| EP2550262A1 (en) | 2010-03-24 | 2013-01-30 | Vertex Pharmaceuticals Incorporated | Analogues for the treatment or prevention of flavivirus infections |
| 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 |
| CN103038237A (zh) | 2010-03-24 | 2013-04-10 | 沃泰克斯药物股份有限公司 | 用于黄病毒感染治疗或预防的类似物 |
| WO2011119860A1 (en) | 2010-03-24 | 2011-09-29 | Vertex Pharmaceuticals Incorporated | Analogues for the treatment or prevention of flavivirus infections |
| RS54368B1 (sr) | 2010-03-31 | 2016-04-28 | Gilead Pharmasset Llc | Kristalni (s)-izopropil 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-diokso-3,4-dihidropirimidin-1-(2h)-il)-4-fluoro-3-hidroksi-4-metiltetrahidrofuran-2-il)metoksi)(fenoksi)fosforil)amino)propanoat |
| CN102917585A (zh) | 2010-04-01 | 2013-02-06 | 埃迪尼克斯医药公司 | 用于治疗病毒感染的化合物和药物组合物 |
| AU2011245630B2 (en) | 2010-04-07 | 2014-07-03 | 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 |
| WO2011159826A2 (en) | 2010-06-15 | 2011-12-22 | Vertex Pharmaceuticals Incorporated | Hcv ns5b protease mutants |
| WO2012006070A1 (en) | 2010-06-28 | 2012-01-12 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| EP2585448A1 (en) | 2010-06-28 | 2013-05-01 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| EP2585447A2 (en) | 2010-06-28 | 2013-05-01 | Vertex Pharmaceuticals Incorporated | Compounds and methods for the treatment or prevention of flavivirus infections |
| WO2012018534A2 (en) | 2010-07-26 | 2012-02-09 | Schering Corporation | Substituted biphenylene compounds and methods of use thereof for the treatment of viral diseases |
| AR082619A1 (es) | 2010-08-13 | 2012-12-19 | Hoffmann La Roche | Inhibidores del virus de la hepatitis c |
| CN103153978A (zh) | 2010-08-17 | 2013-06-12 | 沃泰克斯药物股份有限公司 | 用于治疗或预防黄病毒科病毒感染的化合物和方法 |
| WO2012050848A1 (en) | 2010-09-29 | 2012-04-19 | Schering Corporation | Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases |
| US9011833B2 (en) | 2010-10-08 | 2015-04-21 | Novartis Ag | Vitamin E formulations of sulfamide NS3 inhibitors |
| MX2013004906A (es) | 2010-11-01 | 2013-12-06 | Genoscience Pharma | Nuevos inhibidores especificos de la proteasa ns3 de hcv. |
| EP3042910B1 (en) | 2010-11-30 | 2019-01-09 | Gilead Pharmasset LLC | 2'-spiro-nucleosides for use in the therapy of hepatitis c |
| AR085352A1 (es) | 2011-02-10 | 2013-09-25 | Idenix Pharmaceuticals Inc | Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv |
| 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 |
| 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 |
| CA2843324A1 (en) | 2011-03-31 | 2012-11-15 | Idenix Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of viral infections |
| 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 |
| AU2012269643A1 (en) | 2011-06-16 | 2014-02-06 | AB Pharma Ltd. | Macrocyclic heterocyclic compound 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 |
| EP2736893A1 (en) | 2011-07-26 | 2014-06-04 | Vertex Pharmaceuticals Incorporated | Thiophene compounds |
| WO2013016499A1 (en) | 2011-07-26 | 2013-01-31 | Vertex Pharmaceuticals Incorporated | Methods for preparation of thiophene compounds |
| 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 |
| 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 |
| 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 |
| TW201329096A (zh) | 2011-09-12 | 2013-07-16 | Idenix Pharmaceuticals Inc | 經取代羰氧基甲基磷酸醯胺化合物及用於治療病毒感染之藥學組成物 |
| CN103906759A (zh) | 2011-09-12 | 2014-07-02 | 埃迪尼克斯医药公司 | 用于治疗病毒感染的化合物和药物组合物 |
| 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 |
| MX2014003705A (es) | 2011-10-10 | 2014-07-22 | Hoffmann La Roche | Compuestos antivirales. |
| WO2013056046A1 (en) | 2011-10-14 | 2013-04-18 | 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 |
| EP3750544B1 (en) | 2011-11-30 | 2025-03-05 | Emory University | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| BR112014013649A2 (pt) | 2011-12-06 | 2020-10-27 | The Board Of Trustees Of The Leland Stanford Junior University | métodos e agentes para o tratamento de doenças virais e usos dos referidos agentes |
| BR112014013972A8 (pt) | 2011-12-16 | 2017-06-13 | Hoffmann La Roche | inibidores de hcv nssa |
| PT2794629T (pt) | 2011-12-20 | 2017-07-20 | Riboscience Llc | Derivados de nucleósidos substituídos em 2¿-4¿-difluor-2¿-metilo, como inibidores da replicação do arn de vhc (vírus da hepatite c) |
| BR112014015066A2 (pt) | 2011-12-20 | 2017-06-13 | Hoffmann La Roche | derivados de nucleosídeos 4'azido-3'-flúor substituídos como inibidores de replicação do rna de hcv |
| 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 |
| EP2802574A4 (en) | 2012-01-12 | 2015-06-24 | Rfs Pharma Llc | INHIBITORS OF HCV NS3 PROTEASE |
| 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] |
| CA2864669A1 (en) | 2012-02-16 | 2013-08-22 | Rqx Pharmaceuticals, Inc. | Linear peptide antibiotics |
| WO2013124335A1 (en) | 2012-02-24 | 2013-08-29 | F. Hoffmann-La Roche Ag | Antiviral compounds |
| WO2013142157A1 (en) | 2012-03-22 | 2013-09-26 | Alios Biopharma, Inc. | Pharmaceutical combinations comprising a thionucleotide analog |
| US9109001B2 (en) | 2012-05-22 | 2015-08-18 | Idenix Pharmaceuticals, Inc. | 3′,5′-cyclic phosphoramidate prodrugs for HCV infection |
| EP2852605B1 (en) | 2012-05-22 | 2018-01-31 | Idenix Pharmaceuticals LLC | 3',5'-cyclic phosphate prodrugs for hcv infection |
| EP2852603B1 (en) | 2012-05-22 | 2021-05-12 | Idenix Pharmaceuticals LLC | D-amino acid compounds for liver disease |
| US20140010783A1 (en) | 2012-07-06 | 2014-01-09 | Hoffmann-La Roche Inc. | Antiviral compounds |
| US9309283B2 (en) | 2012-07-09 | 2016-04-12 | Onyx Therapeutics, Inc. | Prodrugs of peptide epoxy ketone protease inhibitors |
| 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 |
| SG11201502750UA (en) | 2012-10-08 | 2015-06-29 | Idenix Pharmaceuticals Inc | 2'-chloro nucleoside analogs for hcv infection |
| WO2014063019A1 (en) | 2012-10-19 | 2014-04-24 | Idenix Pharmaceuticals, Inc. | Dinucleotide compounds for hcv infection |
| BR112015007879A2 (pt) | 2012-10-19 | 2017-07-04 | Bristol Myers Squibb Co | inibidores do vírus da hepatite 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 |
| US9643999B2 (en) | 2012-11-02 | 2017-05-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2014070964A1 (en) | 2012-11-02 | 2014-05-08 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| WO2014071007A1 (en) | 2012-11-02 | 2014-05-08 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| EP2914614B1 (en) | 2012-11-05 | 2017-08-16 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| EP2920195A1 (en) | 2012-11-14 | 2015-09-23 | IDENIX Pharmaceuticals, Inc. | D-alanine ester of rp-nucleoside analog |
| US20140140952A1 (en) | 2012-11-14 | 2014-05-22 | Idenix Pharmaceuticals, Inc. | D-Alanine Ester of Sp-Nucleoside Analog |
| WO2014099941A1 (en) | 2012-12-19 | 2014-06-26 | Idenix Pharmaceuticals, Inc. | 4'-fluoro nucleosides for the treatment of hcv |
| CA2892589A1 (en) | 2013-01-23 | 2014-07-31 | F. Hoffmann-La Roche Ag | Antiviral triazole derivatives |
| TW201526899A (zh) | 2013-02-28 | 2015-07-16 | Alios Biopharma Inc | 醫藥組成物 |
| EP2970358B1 (en) | 2013-03-04 | 2021-06-30 | Idenix Pharmaceuticals LLC | 3'-deoxy nucleosides for the treatment of hcv |
| WO2014137930A1 (en) | 2013-03-04 | 2014-09-12 | Idenix Pharmaceuticals, Inc. | Thiophosphate nucleosides for the treatment of hcv |
| RU2015136256A (ru) | 2013-03-05 | 2017-04-10 | Ф. Хоффманн-Ля Рош Аг | Противовирусные соединения |
| WO2014137869A1 (en) | 2013-03-07 | 2014-09-12 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| WO2014165542A1 (en) | 2013-04-01 | 2014-10-09 | Idenix Pharmaceuticals, Inc. | 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 |
| WO2014193663A1 (en) | 2013-05-16 | 2014-12-04 | Riboscience Llc | 4'-azido, 3'-deoxy-3'-fluoro substituted nucleoside derivatives |
| KR102241198B1 (ko) | 2013-05-16 | 2021-04-15 | 리보사이언스 엘엘씨 | 4'-플루오로-2'-메틸 치환된 뉴클레오시드 유도체 |
| EP3004130B1 (en) | 2013-06-05 | 2019-08-07 | Idenix Pharmaceuticals LLC. | 1',4'-thio nucleosides for the treatment of hcv |
| EP3027636B1 (en) | 2013-08-01 | 2022-01-05 | Idenix Pharmaceuticals LLC | D-amino acid phosphoramidate pronucleotides of halogeno pyrimidine compounds for liver disease |
| JP2016528257A (ja) * | 2013-08-14 | 2016-09-15 | アールキューエックス ファーマシューティカルズ,インク. | 直鎖ペプチド抗生物質 |
| PT3038601T (pt) | 2013-08-27 | 2020-06-30 | Gilead Pharmasset Llc | Formulação combinada de dois compostos antivirais |
| WO2015042375A1 (en) | 2013-09-20 | 2015-03-26 | 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 |
| US10167298B2 (en) | 2013-10-30 | 2019-01-01 | Merck Sharp & Dohme Corp. | Pseudopolymorphs of an HCV NS5A inhibitor and uses thereof |
| WO2015066370A1 (en) | 2013-11-01 | 2015-05-07 | Idenix Pharmaceuticals, Inc. | D-alanine phosphoramidate pronucleotides of 2'-methyl 2'-fluoro guanosine nucleoside compounds for the treatment of hcv |
| WO2015081297A1 (en) | 2013-11-27 | 2015-06-04 | Idenix Pharmaceuticals, Inc. | 2'-dichloro and 2'-fluoro-2'-chloro nucleoside analogues for hcv infection |
| US10683321B2 (en) | 2013-12-18 | 2020-06-16 | Idenix Pharmaceuticals Llc | 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 |
| WO2015134780A1 (en) | 2014-03-05 | 2015-09-11 | Idenix Pharmaceuticals, Inc. | Solid prodrug forms of 2'-chloro-2'-methyl uridine for hcv |
| 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 |
| EP3114122A1 (en) | 2014-03-05 | 2017-01-11 | Idenix Pharmaceuticals LLC | Solid forms of a flaviviridae virus inhibitor compound and salts thereof |
| EP3131914B1 (en) | 2014-04-16 | 2023-05-10 | Idenix Pharmaceuticals LLC | 3'-substituted methyl or alkynyl nucleosides for the treatment of hcv |
| WO2017084629A1 (en) | 2015-11-20 | 2017-05-26 | Rqx Pharmaceuticals, Inc. | Macrocyclic broad spectrum antibiotics |
| KR102595723B1 (ko) | 2016-06-21 | 2023-10-27 | 오리온 옵탈몰로지 엘엘씨 | 헤테로시클릭 프롤린아미드 유도체 |
| EP3472151A4 (en) | 2016-06-21 | 2020-03-04 | Orion Ophthalmology LLC | CARBOCYCLIC PROLINAMIDE DERIVATIVES |
| ES2917194T3 (es) | 2016-06-21 | 2022-07-07 | Orion Ophthalmology LLC | Derivados de prolinamida alifática |
| JP2019526563A (ja) * | 2016-08-23 | 2019-09-19 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Htra1阻害剤としての新規ジフルオロケタミド誘導体 |
| CN110709096B (zh) | 2017-05-05 | 2023-10-31 | 泽兰德制药公司 | 细胞间隙连接通讯调节剂及其在糖尿病性眼病治疗中的应用 |
| GB2563396B (en) | 2017-06-12 | 2020-09-23 | Ustav Organicke Chemie A Biochemie Av Cr V V I | Inhibitors of Rhomboid Intramembrane Proteases |
| TWI860279B (zh) | 2017-09-21 | 2024-11-01 | 美商里伯賽恩斯有限責任公司 | 作為hcv rna複製抑制劑之經4'-氟-2'-甲基取代之核苷衍生物 |
| 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 |
| PE20240066A1 (es) | 2019-05-28 | 2024-01-11 | Hoffmann La Roche | Antibioticos macrociclicos de amplio espectro |
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 |
| ATE71934T1 (de) | 1985-06-07 | 1992-02-15 | Ici America Inc | Selektionierte difluorverbindungen. |
| 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 |
| JP2668003B2 (ja) * | 1992-06-12 | 1997-10-27 | ファイザー インク. | ヒトの心臓キマーゼを含むアンギオテンシンiキマーゼに関する阻害剤 |
| 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 |
| EP0604182B1 (en) * | 1992-12-22 | 2000-10-11 | Eli Lilly And Company | Inhibitors of HIV protease useful for the treatment of Aids |
| DK0727419T3 (da) | 1992-12-29 | 2002-06-10 | Abbott Lab | Mellemprodukter til fremstilling af forbindelser, som inhiberer retroviral protease |
| 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 |
| IL113196A0 (en) | 1994-03-31 | 1995-06-29 | Bristol Myers Squibb Co | Imidazole derivatives and pharmaceutical compositions containing the same |
| 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 |
| US6420522B1 (en) | 1995-06-05 | 2002-07-16 | 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 |
| JP2000500760A (ja) | 1995-11-23 | 2000-01-25 | メルク シヤープ エンド ドーム リミテツド | スピロピペリジン誘導体およびタキキニン拮抗薬としてのその使用 |
| US6900238B1 (en) | 1995-12-07 | 2005-05-31 | The Scripps Research Institute | HIV protease inhibitors |
| US5807876A (en) * | 1996-04-23 | 1998-09-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of IMPDH enzyme |
| US6054472A (en) * | 1996-04-23 | 2000-04-25 | Vertex Pharmaceuticals, Incorporated | Inhibitors of IMPDH enzyme |
| ZA972195B (en) | 1996-03-15 | 1998-09-14 | Du Pont Merck Pharma | Spirocycle integrin inhibitors |
| NZ332405A (en) * | 1996-04-23 | 2000-06-23 | Vertex Pharma | oxazolyl, thiazolyl or phenyl urea derivatives as inhibitors of inosine monophosphate dehydrogenase enzyme |
| 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 |
| DE69735482T2 (de) | 1996-09-25 | 2006-10-19 | Merck Sharp & Dohme Ltd., Hoddesdon | Spiro-azacyclische derivate, deren herstellung und verwendung als tachykinin-antagonisten |
| ATE250048T1 (de) | 1996-10-08 | 2003-10-15 | Univ Colorado State Res Found | Katalytische asymmetrische epoxidierung |
| PL194025B1 (pl) * | 1996-10-18 | 2007-04-30 | Vertex Pharma | Inhibitory proteaz serynowych, a zwłaszcza proteazy wirusa NS3 zapalenia wątroby C, kompozycja farmaceutyczna i zastosowanie inhibitorów proteaz serynowych |
| 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 |
| CA2282398A1 (en) | 1997-03-14 | 1998-09-17 | Steven M. Ronkin | Inhibitors of impdh enzyme |
| 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 |
| EP1012180B1 (en) | 1997-08-11 | 2004-12-01 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis c inhibitor 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 |
| WO1999028482A2 (en) | 1997-11-28 | 1999-06-10 | Schering Corporation | Single-chain recombinant complexes of hepatitis c virus ns3 protease and ns4a cofactor peptide |
| DK1066247T3 (da) * | 1998-03-31 | 2007-04-02 | Vertex Pharma | Inhibitorer af serinproteaser, især 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 |
| EP1027885B1 (en) | 1999-02-09 | 2008-07-09 | Pfizer Products Inc. | Basic drug compositions with enhanced bioavailability |
| US20020042046A1 (en) | 1999-02-25 | 2002-04-11 | Vertex Pharmaceuticals, Incorporated | Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex |
| CZ301802B6 (cs) * | 1999-03-19 | 2010-06-30 | Vertex Pharmaceuticals Incorporated | Deriváty mocoviny jako inhibitory IMPDH a farmaceutické prostredky s jejich obsahem |
| 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 |
| EP1252178A1 (en) * | 1999-12-03 | 2002-10-30 | Bristol-Myers Squibb Pharma Company | Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease |
| WO2001064678A2 (en) | 2000-02-29 | 2001-09-07 | Bristol-Myers Squibb Pharma Company | Inhibitors of hepatitis c virus ns3 protease |
| AU2001251165A1 (en) * | 2000-04-03 | 2001-10-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
| US6846802B2 (en) | 2000-04-05 | 2005-01-25 | Schering Corporation | Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties |
| CA2406532A1 (en) * | 2000-04-19 | 2001-11-01 | Schering Corporation | Macrocyclic ns-3 serine protease inhibitors of hepatitis c virus compri sing alkyl and aryl alanine p2 moieties |
| EP1295876A4 (en) | 2000-06-30 | 2005-10-19 | EPOXYCARBOXYLIC AMIDE, AZIDE AND AMINO ALCOHOLS AND THEIR USE IN PROCESSES FOR THE PREPARATION OF ALPHA KETOAMIDES | |
| AR029851A1 (es) | 2000-07-21 | 2003-07-16 | Dendreon Corp | Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c |
| SK288064B6 (sk) | 2000-07-21 | 2013-04-03 | Merck Sharp & Dohme Corp. | Peptide compounds, pharmaceutical compositions comprising them and their use |
| US7244721B2 (en) | 2000-07-21 | 2007-07-17 | 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 |
| BR0112666A (pt) | 2000-07-21 | 2003-06-10 | Schering Corp | Peptìdeos como inibidores de ns3-serina protease de vìrus da hepatite c |
| JP2004504407A (ja) | 2000-07-21 | 2004-02-12 | コルバス・インターナショナル・インコーポレイテッド | C型肝炎ウイルスのns3−セリンプロテアーゼ阻害剤としての新規ペプチド |
| 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 |
| ATE327246T1 (de) | 2000-11-20 | 2006-06-15 | Bristol Myers Squibb Co | Hepatitis c tripeptid inhibitoren |
| US6911428B2 (en) | 2000-12-12 | 2005-06-28 | Schering Corporation | Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus |
| US6653295B2 (en) | 2000-12-13 | 2003-11-25 | Bristol-Myers Squibb Company | Inhibitors of hepatitis C virus NS3 protease |
| AU2002230764A1 (en) | 2000-12-13 | 2002-06-24 | 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 |
| IL156641A0 (en) | 2001-01-22 | 2004-01-04 | Merck & Co Inc | Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase |
| GB0102342D0 (en) | 2001-01-30 | 2001-03-14 | Smithkline Beecham Plc | Pharmaceutical formulation |
| CA2436518A1 (en) | 2001-01-30 | 2002-08-08 | Vertex Pharmaceuticals Incorporated | A quantitative assay for nucleic acids |
| DE60232322D1 (de) | 2001-03-27 | 2009-06-25 | Vertex Pharma | Verfahren |
| GB0107924D0 (en) | 2001-03-29 | 2001-05-23 | Angeletti P Ist Richerche Bio | Inhibitor of hepatitis C virus NS3 protease |
| EP1463699A2 (en) | 2001-07-03 | 2004-10-06 | ALTANA Pharma AG | Process for the production of 3-phenylisoserine |
| US6909000B2 (en) | 2001-07-11 | 2005-06-21 | 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 |
| EP2402009A1 (en) * | 2001-10-24 | 2012-01-04 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine protease, particularly hepatitis c virus NS3-NS4A protease, incorporating a fused ring system |
| ES2234451T1 (es) | 2001-11-14 | 2005-07-01 | Teva Pharmaceutical Industries Ltd. | Formas cristalinas y amorfas de losartan potasio y procedimiento para su preparacion. |
| 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 |
| US6642204B2 (en) | 2002-02-01 | 2003-11-04 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| US7091184B2 (en) | 2002-02-01 | 2006-08-15 | Boehringer Ingelheim International Gmbh | 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 |
| TW200403236A (en) * | 2002-04-11 | 2004-03-01 | Vertex Pharma | Inhibitors or serine proteases, particularly HCV NS3-NS4A protease |
| AU2003235118C1 (en) | 2002-04-25 | 2010-01-07 | Ono Pharmaceutical Co., Ltd. | Diketohydrazine derivative compounds and drugs containing the compounds as the active ingredient |
| CA2494340C (en) | 2002-08-01 | 2012-01-24 | Pharmasset Inc. | Compounds with the bicyclo[4.2.1]nonane system for the treatment of flaviviridae 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 |
| US7223785B2 (en) | 2003-01-22 | 2007-05-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
| US7098231B2 (en) | 2003-01-22 | 2006-08-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
| JP2007524576A (ja) | 2003-02-07 | 2007-08-30 | エナンタ ファーマシューティカルズ インコーポレイテッド | 大環状のc型肝炎セリンプロテアーゼ阻害剤 |
| US20040180815A1 (en) | 2003-03-07 | 2004-09-16 | Suanne Nakajima | Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors |
| EP1596846A2 (en) | 2003-02-18 | 2005-11-23 | Pfizer Inc. | Inhibitors of hepatitis c virus, compositions and treatments using the same |
| 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 |
| CN1771257A (zh) | 2003-04-10 | 2006-05-10 | 贝林格尔·英格海姆国际有限公司 | 通过钌络合物催化的易位反应制备大环化合物的方法 |
| ATE547412T1 (de) * | 2003-04-11 | 2012-03-15 | Vertex Pharma | Inhibitoren von serinproteasen, insbesondere hcv- ns3-ns4a-protease |
| TW200510391A (en) | 2003-04-11 | 2005-03-16 | Vertex Pharma | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| NZ544076A (en) | 2003-05-21 | 2009-04-30 | Boehringer Ingelheim Int | Hepatitis C inhibitor compounds |
| US7125845B2 (en) | 2003-07-03 | 2006-10-24 | Enanta Pharmaceuticals, Inc. | Aza-peptide macrocyclic hepatitis C serine protease inhibitors |
| EP1646642A2 (en) * | 2003-07-18 | 2006-04-19 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
| WO2005018330A1 (en) | 2003-08-18 | 2005-03-03 | Pharmasset, Inc. | Dosing regimen for flaviviridae therapy |
| PE20050374A1 (es) | 2003-09-05 | 2005-05-30 | Vertex Pharma | Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc |
| WO2005025517A2 (en) | 2003-09-12 | 2005-03-24 | Vertex Pharmaceuticals Incorporated | Animal model for protease activity and liver damage |
| WO2005028502A1 (en) | 2003-09-18 | 2005-03-31 | 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 |
| JP4704342B2 (ja) | 2003-09-22 | 2011-06-15 | 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型肝炎ウイルスに対し活性な大環状ペプチド |
| US7592419B2 (en) | 2003-09-26 | 2009-09-22 | Schering Corporation | Macrocyclic inhibitors of hepatitis C virus NS3-serine protease |
| MXPA06004006A (es) * | 2003-10-10 | 2006-06-28 | Vertex Pharma | Inhibidores de serina proteasas, especialmente de ns3-ns4a proteasa del virus de la hepatitis c. |
| AR045870A1 (es) | 2003-10-11 | 2005-11-16 | Vertex Pharma | Terapia de combinacion para la infeccion de virus de hepatitis c |
| EP1678202B1 (en) | 2003-10-27 | 2012-06-13 | Vertex Pharmaceuticals Incorporated | Hcv ns3-ns4a protease resistance mutants |
| WO2005043118A2 (en) | 2003-10-27 | 2005-05-12 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
| DK1677827T3 (da) | 2003-10-27 | 2009-03-30 | Vertex Pharma | Kombinationer til HCV-behandling |
| AU2004285972A1 (en) | 2003-10-28 | 2005-05-12 | Vertex Pharmaceuticals, Incorporated | Preparation of 4,5-dialkyl-3-acyl-pyrrole-2-carboxylic acid derivatives by Fischer-Fink type synthesis and subsequent acylation |
| 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 |
| US7135462B2 (en) | 2003-11-20 | 2006-11-14 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| JP2007532479A (ja) | 2003-11-20 | 2007-11-15 | シェーリング コーポレイション | C型肝炎ウイルスns3プロテアーゼの脱ペプチド化インヒビター |
| EP1689857A1 (en) | 2003-12-01 | 2006-08-16 | Vertex Pharmaceuticals Incorporated | Compositions comprising fetal liver cells and methods useful for hcv infection |
| AU2004298498B2 (en) | 2003-12-11 | 2008-09-11 | Schering Corporation | Inhibitors of hepatitis C virus NS3/NS4a serine protease |
| WO2005070955A1 (en) | 2004-01-21 | 2005-08-04 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis c virus |
| EP2311851A3 (en) * | 2004-02-04 | 2011-05-25 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| US20050187192A1 (en) | 2004-02-20 | 2005-08-25 | Kucera Pharmaceutical Company | Phospholipids for the treatment of infection by togaviruses, herpes viruses and coronaviruses |
| TWI368508B (en) | 2004-02-20 | 2012-07-21 | Boehringer Ingelheim Int | Viral polymerase inhibitors |
| KR20130018418A (ko) | 2004-02-27 | 2013-02-21 | 머크 샤프 앤드 돔 코포레이션 | C형 간염 바이러스 ns3 세린 프로테아제의 억제제로서의 황 화합물 |
| TW200536528A (en) | 2004-02-27 | 2005-11-16 | Schering Corp | Novel inhibitors of hepatitis C virus NS3 protease |
| AU2005219824B2 (en) | 2004-02-27 | 2007-11-29 | Merck Sharp & Dohme Corp. | Novel ketoamides with cyclic p4's as inhibitors of ns3 serine protease of hepatitis c virus |
| 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. |
| PT2399916E (pt) | 2004-03-12 | 2015-03-17 | Vertex Pharma | Processo e intermediários para a preparação de inibidores de caspase de acetal de ácido aspártico |
| US7901707B2 (en) | 2004-03-15 | 2011-03-08 | Christine Allen | Biodegradable biocompatible implant and method of manufacturing same |
| AR049635A1 (es) | 2004-05-06 | 2006-08-23 | 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(3.1.0)hexan-2-carboxamida como inhibidor de la ns3/ns4a serina proteasa del virus de la hepatitis c |
| US7399749B2 (en) | 2004-05-20 | 2008-07-15 | Schering Corporation | Substituted prolines as inhibitors of hepatitis C virus NS3 serine protease |
| TWI389688B (zh) * | 2004-06-08 | 2013-03-21 | Vertex Pharma | Vx-950之形態與調配物及其製備方法與用途 |
| EP1763531A4 (en) | 2004-06-28 | 2009-07-01 | Boehringer Ingelheim Int | ANALOGUE OF HEPATITIS-C INHIBITING PEPTIDES |
| EP1786280A1 (en) | 2004-07-02 | 2007-05-23 | The Governors of the University of Alberta | Aqueous solutions containing beta-glucan and gums |
| UY29016A1 (es) | 2004-07-20 | 2006-02-24 | Boehringer Ingelheim Int | Analogos de dipeptidos inhibidores de la hepatitis c |
| CA2573346C (en) | 2004-07-20 | 2011-09-20 | Boehringer Ingelheim International Gmbh | Hepatitis c inhibitor peptide analogs |
| WO2006026352A1 (en) | 2004-08-27 | 2006-03-09 | Schering Corporation | Acylsulfonamide compounds as inhibitors of hepatitis c virus ns3 serine protease |
| 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 |
| WO2007016589A2 (en) * | 2005-08-02 | 2007-02-08 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| EP2194043B1 (en) * | 2005-08-19 | 2013-12-25 | Vertex Pharmaceuticals Incorporated | Processes |
| 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 |
| US8039475B2 (en) | 2006-02-27 | 2011-10-18 | Vertex Pharmaceuticals Incorporated | Co-crystals and pharmaceutical compositions comprising the same |
| CA2646123A1 (en) | 2006-03-16 | 2007-09-27 | Vertex Pharmaceuticals Incorporated | Processes and intermediates for preparing steric compounds |
| WO2007109080A2 (en) | 2006-03-16 | 2007-09-27 | Vertex Pharmaceuticals Incorporated | Deuterated hepatitis c protease inhibitors |
| JP2009530415A (ja) | 2006-03-20 | 2009-08-27 | 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 | 医薬組成物 |
| 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 |
| KR20090018843A (ko) | 2006-05-31 | 2009-02-23 | 버텍스 파마슈티칼스 인코포레이티드 | 인터류킨-1 베타 전환효소 억제제의 경구용 조절 방출 제제 |
| US7708294B2 (en) | 2006-11-02 | 2010-05-04 | Gm Global Technology Operations, Inc. | Detachable dual-use platform apparatus and method |
| WO2008106058A2 (en) * | 2007-02-27 | 2008-09-04 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| US7959488B2 (en) * | 2007-10-15 | 2011-06-14 | Tania Alessandra Talamo | Brassiere pad system |
-
1997
- 1997-10-17 PL PL97372333A patent/PL194025B1/pl not_active IP Right Cessation
- 1997-10-17 ZA ZA9709327A patent/ZA979327B/xx unknown
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- 1997-10-17 EP EP10013053A patent/EP2314598A1/en not_active Withdrawn
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- 1997-10-17 PL PL332872A patent/PL192280B1/pl not_active IP Right Cessation
- 1997-10-17 EP EP10013054.1A patent/EP2409985A3/en not_active Withdrawn
- 1997-10-17 KR KR10-1999-7003372A patent/KR100509388B1/ko not_active Expired - Fee Related
- 1997-10-17 TR TR1999/01602T patent/TR199901602T2/xx unknown
- 1997-10-17 CZ CZ0134099A patent/CZ298749B6/cs not_active IP Right Cessation
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- 1997-10-18 TW TW086115382A patent/TW530065B/zh not_active IP Right Cessation
-
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- 1999-04-13 IL IL129407A patent/IL129407A/en not_active IP Right Cessation
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- 1999-05-11 BG BG103392A patent/BG103392A/xx unknown
-
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-
2003
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-
2007
- 2007-11-08 JP JP2007290832A patent/JP4783353B2/ja not_active Expired - Fee Related
-
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- 2008-02-14 US US12/031,486 patent/US8314141B2/en not_active Expired - Fee Related
- 2008-06-03 IL IL191905A patent/IL191905A0/en unknown
-
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- 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 |
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