AR030558A1 - COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA, - Google Patents
COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA,Info
- Publication number
- AR030558A1 AR030558A1 ARP010101794A ARP010101794A AR030558A1 AR 030558 A1 AR030558 A1 AR 030558A1 AR P010101794 A ARP010101794 A AR P010101794A AR P010101794 A ARP010101794 A AR P010101794A AR 030558 A1 AR030558 A1 AR 030558A1
- Authority
- AR
- Argentina
- Prior art keywords
- conhch
- alkyl
- cycloalkyl
- aryl
- carbamate
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000005764 inhibitory process Effects 0.000 title 1
- -1 arylheteroaryl Chemical group 0.000 abstract 13
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 7
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 229910052760 oxygen Inorganic materials 0.000 abstract 5
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 4
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 4
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 108091005804 Peptidases Proteins 0.000 abstract 2
- 239000004365 Protease Substances 0.000 abstract 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 2
- 150000001299 aldehydes Chemical class 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 150000001346 alkyl aryl ethers Chemical class 0.000 abstract 2
- 150000005215 alkyl ethers Chemical class 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000003368 amide group Chemical group 0.000 abstract 2
- 125000005110 aryl thio group Chemical group 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- 239000004202 carbamide Substances 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 150000002576 ketones Chemical class 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 1
- 101100440695 Dictyostelium discoideum corB gene Proteins 0.000 abstract 1
- 101100134922 Gallus gallus COR5 gene Proteins 0.000 abstract 1
- 241000711549 Hepacivirus C Species 0.000 abstract 1
- 229940100389 Sulfonylurea Drugs 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 150000003973 alkyl amines Chemical class 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004422 alkyl sulphonamide group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000005100 aryl amino carbonyl group Chemical group 0.000 abstract 1
- 125000001769 aryl amino group Chemical group 0.000 abstract 1
- 125000005129 aryl carbonyl group Chemical group 0.000 abstract 1
- 150000008378 aryl ethers Chemical class 0.000 abstract 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 abstract 1
- 125000005362 aryl sulfone group Chemical group 0.000 abstract 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 1
- 125000004421 aryl sulphonamide group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- UZMZVDOOVXLRID-UHFFFAOYSA-N azanylidyne-(nitrosulfonylamino)methane Chemical compound [O-][N+](=O)S(=O)(=O)NC#N UZMZVDOOVXLRID-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 238000005660 chlorination reaction Methods 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 abstract 1
- 125000005226 heteroaryloxycarbonyl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 150000002678 macrocyclic compounds Chemical class 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000004437 phosphorous atom Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- 150000003457 sulfones Chemical class 0.000 abstract 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 abstract 1
- 150000003462 sulfoxides Chemical class 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- RAHZWNYVWXNFOC-UHFFFAOYSA-N sulfur dioxide Inorganic materials O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19820400P | 2000-04-19 | 2000-04-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR030558A1 true AR030558A1 (es) | 2003-08-27 |
Family
ID=22732422
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010101794A AR030558A1 (es) | 2000-04-19 | 2001-04-17 | COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA, |
Country Status (22)
Families Citing this family (134)
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| EA001915B1 (ru) * | 1996-10-18 | 2001-10-22 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы серин-протеаз, в частности ns3 протеазы вируса гепатита c (hvc) |
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| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| EP1343807B1 (en) * | 2000-12-12 | 2009-04-29 | Schering Corporation | Diaryl peptides as ns3-serine protease inhibitors of hepatits c virus |
| BR0206614A (pt) | 2001-01-22 | 2004-02-17 | Merck & Co Inc | Composto, composição farmacêutica, método para inibir a polimerase viral de rna dependente de rna e/ou inibir a replicação viral de rna dependente de rna, método para tratar uma infecção viral de rna dependente de rna, e, uso de um composto |
| US7119072B2 (en) | 2002-01-30 | 2006-10-10 | Boehringer Ingelheim (Canada) Ltd. | Macrocyclic peptides active against the hepatitis C virus |
| US7091184B2 (en) | 2002-02-01 | 2006-08-15 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| US6642204B2 (en) | 2002-02-01 | 2003-11-04 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
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| EP1654261B1 (en) | 2003-05-21 | 2007-11-14 | Boehringer Ingelheim International GmbH | Hepatitis c inhibitor compounds |
| US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
| US8921521B2 (en) | 2003-06-18 | 2014-12-30 | Ocera Therapeutics, Inc. | Macrocyclic modulators of the Ghrelin receptor |
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| KR20060124725A (ko) | 2004-02-27 | 2006-12-05 | 쉐링 코포레이션 | C형 간염 바이러스 ns3 프로테아제의 억제제 |
| CN1972956A (zh) | 2004-02-27 | 2007-05-30 | 先灵公司 | 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的新化合物 |
| RU2428428C9 (ru) | 2004-02-27 | 2012-03-10 | Шеринг Корпорейшн | Серусодержащие соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с |
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2001
- 2001-04-17 CN CNA2009100067369A patent/CN101580536A/zh active Pending
- 2001-04-17 JP JP2001578418A patent/JP4748912B2/ja not_active Expired - Fee Related
- 2001-04-17 BR BR0110104-8A patent/BR0110104A/pt not_active IP Right Cessation
- 2001-04-17 HK HK03100478.8A patent/HK1048479A1/zh unknown
- 2001-04-17 AR ARP010101794A patent/AR030558A1/es unknown
- 2001-04-17 EP EP01927142A patent/EP1274724A2/en not_active Withdrawn
- 2001-04-17 CA CA002406532A patent/CA2406532A1/en not_active Abandoned
- 2001-04-17 PE PE2001000348A patent/PE20011288A1/es not_active Application Discontinuation
- 2001-04-17 CN CNA2006101537103A patent/CN1935833A/zh active Pending
- 2001-04-17 SK SK1495-2002A patent/SK14952002A3/sk not_active Application Discontinuation
- 2001-04-17 PL PL01358591A patent/PL358591A1/xx not_active Application Discontinuation
- 2001-04-17 AU AU2001253621A patent/AU2001253621A1/en not_active Abandoned
- 2001-04-17 KR KR1020027013965A patent/KR20020097220A/ko not_active Withdrawn
- 2001-04-17 WO PCT/US2001/012530 patent/WO2001081325A2/en not_active Ceased
- 2001-04-17 US US09/836,636 patent/US6914122B2/en not_active Expired - Fee Related
- 2001-04-17 RU RU2002131163/04A patent/RU2002131163A/ru not_active Application Discontinuation
- 2001-04-17 HU HU0302957A patent/HUP0302957A2/hu unknown
- 2001-04-17 CN CN01810566A patent/CN1432022A/zh active Pending
- 2001-04-17 MX MXPA02010375A patent/MXPA02010375A/es active IP Right Grant
- 2001-04-17 CZ CZ20023473A patent/CZ20023473A3/cs unknown
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- 2001-04-17 IL IL15193501A patent/IL151935A0/xx unknown
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2002
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- 2002-10-18 NO NO20025030A patent/NO20025030L/no not_active Application Discontinuation
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| CN1432022A (zh) | 2003-07-23 |
| ZA200208014B (en) | 2004-02-12 |
| SK14952002A3 (sk) | 2003-03-04 |
| CN101580536A (zh) | 2009-11-18 |
| HK1048479A1 (zh) | 2003-04-04 |
| BR0110104A (pt) | 2003-01-07 |
| US6914122B2 (en) | 2005-07-05 |
| JP4748912B2 (ja) | 2011-08-17 |
| NO20025030D0 (no) | 2002-10-18 |
| NO20025030L (no) | 2002-12-18 |
| AU2001253621A1 (en) | 2001-11-07 |
| KR20020097220A (ko) | 2002-12-31 |
| NZ521456A (en) | 2004-07-30 |
| RU2002131163A (ru) | 2004-06-27 |
| CZ20023473A3 (cs) | 2003-01-15 |
| WO2001081325A3 (en) | 2002-08-01 |
| EP1274724A2 (en) | 2003-01-15 |
| HUP0302957A2 (hu) | 2003-12-29 |
| CN1935833A (zh) | 2007-03-28 |
| IL151935A0 (en) | 2003-04-10 |
| US20020016294A1 (en) | 2002-02-07 |
| PE20011288A1 (es) | 2001-12-12 |
| CA2406532A1 (en) | 2001-11-01 |
| WO2001081325A2 (en) | 2001-11-01 |
| PL358591A1 (en) | 2004-08-09 |
| JP2003531199A (ja) | 2003-10-21 |
| MXPA02010375A (es) | 2003-04-25 |
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