HUP0105235A2 - Bis-amino acid sulfonamides containing n-terminally a substituted benzyl group as hiv protease inhibitors, pharmaceutical compositions comprising thereof and their use - Google Patents
Bis-amino acid sulfonamides containing n-terminally a substituted benzyl group as hiv protease inhibitors, pharmaceutical compositions comprising thereof and their useInfo
- Publication number
- HUP0105235A2 HUP0105235A2 HU0105235A HUP0105235A HUP0105235A2 HU P0105235 A2 HUP0105235 A2 HU P0105235A2 HU 0105235 A HU0105235 A HU 0105235A HU P0105235 A HUP0105235 A HU P0105235A HU P0105235 A2 HUP0105235 A2 HU P0105235A2
- Authority
- HU
- Hungary
- Prior art keywords
- protease inhibitors
- hiv protease
- terminally
- bis
- amino acid
- Prior art date
Links
- 239000004030 hiv protease inhibitor Substances 0.000 title abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229940124530 sulfonamide Drugs 0.000 title 1
- -1 4-aminophenyl- Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 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
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
-
- 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
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- 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
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- 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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
A tal lm ny (I) ltal nos képletű vegyületekre vagy gyógy szatilagelfogadható sóikra vonatkozik, ahol a képletben R1 jelentésefluoratom, R2 jelentése fluor- vagy hidrogénatom és R3 jelentése 4-aminofenil-, 3-aminofenil-, 2,3-dihidrobenzofur n-5-il- vagy 1,3-benzodioxol-5-il-csoport. A tal lm ny szerinti vegyületek HIV prote zinhibitorokként haszn lhatók. A tal lm ny t rgy t képezik az (I) ltalnos képletű vegyületeket tartalmazó gyógy szati készítmények is. ÓThis applies to compounds of formula (I) or their pharmaceutically acceptable salts, where in the formula R1 is a fluorine atom, R2 is a fluorine or hydrogen atom and R3 is 4-aminophenyl-, 3-aminophenyl-, 2,3-dihydrobenzofuran-5 -yl or 1,3-benzodioxol-5-yl. The compounds according to the invention can be used as HIV protease inhibitors. Medicinal preparations containing compounds of the general formula (I) are also part of this product. HE
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11574699P | 1999-01-13 | 1999-01-13 | |
| PCT/US2000/000820 WO2000042060A1 (en) | 1999-01-13 | 2000-01-13 | Bis-amino acid sulfonamides containing n-terminally a substituted benzyl group as hiv protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0105235A2 true HUP0105235A2 (en) | 2002-04-29 |
| HUP0105235A3 HUP0105235A3 (en) | 2002-08-28 |
Family
ID=22363180
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0105235A HUP0105235A3 (en) | 1999-01-13 | 2000-01-13 | Bis-amino acid sulfonamides containing n-terminally a substituted benzyl group as hiv protease inhibitors, pharmaceutical compositions comprising thereof and their use |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP1140983A1 (en) |
| JP (1) | JP2002536298A (en) |
| KR (1) | KR20010101478A (en) |
| CN (1) | CN1336934A (en) |
| AU (1) | AU2725700A (en) |
| BR (1) | BR0007854A (en) |
| CA (1) | CA2353088A1 (en) |
| CZ (1) | CZ20012435A3 (en) |
| HU (1) | HUP0105235A3 (en) |
| IL (1) | IL143763A0 (en) |
| NO (1) | NO20013338L (en) |
| PL (1) | PL349774A1 (en) |
| SK (1) | SK9522001A3 (en) |
| TR (1) | TR200102033T2 (en) |
| WO (1) | WO2000042060A1 (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6861539B1 (en) | 1995-03-10 | 2005-03-01 | G. D. Searle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| EP1188766A1 (en) | 1995-03-10 | 2002-03-20 | G.D. Searle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US7339078B2 (en) | 1995-03-10 | 2008-03-04 | G.D. Searle Llc | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US6617310B2 (en) | 2000-07-19 | 2003-09-09 | Bristol-Myers Squibb Pharma Company | Phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines |
| US20020022659A1 (en) * | 2000-07-19 | 2002-02-21 | Harris Gregory D. | Crystalline and salt forms of an HIV protease inhibitor |
| US20020022742A1 (en) * | 2000-07-19 | 2002-02-21 | Harris Gregory D. | Salt forms of an HIV protease inhibitor |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5843946A (en) * | 1992-08-25 | 1998-12-01 | G.D. Searle & Co. | α-and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| ATE174587T1 (en) * | 1993-08-24 | 1999-01-15 | Searle & Co | HYDROXYAMINOSULFONAMIDES USABLE AS INHIBITORS OF RETROVIRAL PROTEASES |
| US6150556A (en) * | 1995-03-10 | 2000-11-21 | G. D. Dearle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
-
2000
- 2000-01-13 WO PCT/US2000/000820 patent/WO2000042060A1/en not_active Application Discontinuation
- 2000-01-13 HU HU0105235A patent/HUP0105235A3/en unknown
- 2000-01-13 BR BR0007854-9A patent/BR0007854A/en not_active IP Right Cessation
- 2000-01-13 AU AU27257/00A patent/AU2725700A/en not_active Abandoned
- 2000-01-13 PL PL00349774A patent/PL349774A1/en not_active Application Discontinuation
- 2000-01-13 CN CN00802755A patent/CN1336934A/en active Pending
- 2000-01-13 KR KR1020017008803A patent/KR20010101478A/en not_active Application Discontinuation
- 2000-01-13 CZ CZ20012435A patent/CZ20012435A3/en unknown
- 2000-01-13 JP JP2000593627A patent/JP2002536298A/en active Pending
- 2000-01-13 SK SK952-2001A patent/SK9522001A3/en unknown
- 2000-01-13 TR TR2001/02033T patent/TR200102033T2/en unknown
- 2000-01-13 EP EP00905604A patent/EP1140983A1/en not_active Withdrawn
- 2000-01-13 IL IL14376300A patent/IL143763A0/en unknown
- 2000-01-13 CA CA002353088A patent/CA2353088A1/en not_active Abandoned
-
2001
- 2001-07-05 NO NO20013338A patent/NO20013338L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| IL143763A0 (en) | 2002-04-21 |
| CN1336934A (en) | 2002-02-20 |
| KR20010101478A (en) | 2001-11-14 |
| BR0007854A (en) | 2002-01-15 |
| SK9522001A3 (en) | 2002-03-05 |
| WO2000042060A1 (en) | 2000-07-20 |
| PL349774A1 (en) | 2002-09-09 |
| AU2725700A (en) | 2000-08-01 |
| NO20013338D0 (en) | 2001-07-05 |
| NO20013338L (en) | 2001-09-13 |
| CA2353088A1 (en) | 2000-07-20 |
| JP2002536298A (en) | 2002-10-29 |
| TR200102033T2 (en) | 2001-12-21 |
| HUP0105235A3 (en) | 2002-08-28 |
| EP1140983A1 (en) | 2001-10-10 |
| CZ20012435A3 (en) | 2002-02-13 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DE60236541D1 (en) | INHIBITORS OF 11-BETA-HYDROXYSTEROIDDEHYDROGENASE TYPE 1 | |
| HUP0400365A2 (en) | 3-fluoro-pyrrolidines as antidiabetic agents and pharmaceutical compositions containing the compounds | |
| HUP0101999A2 (en) | 4-hydroxyquinoline-3-carboxamides and hydrazides use of them and pharmaceutical compositions containing them | |
| SE0001899D0 (en) | New compounds | |
| SE0102438D0 (en) | New compounds | |
| HUP0104579A2 (en) | Glp-1 analogues, pharmaceutical compositions comprising thereof and their use | |
| HUP0102102A2 (en) | Pyrazoline derivatives, their preparation, pharmaceutical compositions containing them and their use | |
| HUP0104768A2 (en) | 4-amino-3-oxo-azepanes as protease inhibitors and pharmaceutical compositions containing the same | |
| HUP0004559A1 (en) | Aminothiazole inhibitors of cyclin dependent kinases, pharmaceutical compositions containing them and their use | |
| FI972628A (en) | New sulfonamides | |
| HUP0401740A2 (en) | N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase and pharmaceutical compositions containing them | |
| HUP0300684A2 (en) | Somatostatin analogues, pharmaceutical compositions comprising thereof and their use | |
| HUP0400240A2 (en) | Combinations of substituted oxazolidinones and other active ingredients and pharmaceutical compositions containing them | |
| HUP0301194A2 (en) | Pharmaceutical compositions containing combinations of depeptidyl peptidase iv inhibitors and other antidiabetic agents and their use for the treatment of diabete mellitus | |
| EA200501268A1 (en) | HIV-Inhibiting 1,2,4-TRIAZINS | |
| HUP0104973A2 (en) | Novel substituted indolinones with an inhibitory effect on various kinases and cyclin/cdk complexes, process for their use and medicaments containing them | |
| HUP0202570A1 (en) | Compositions and therapeutic methods involving isoflavones and analogues thereof | |
| HUP0402225A2 (en) | Macrolide-compounds, process for their preparation and pharmaceutical compositions containing them | |
| HUP0001555A2 (en) | Tetrahydro-imidazo-naphthyridine derivatives, pharmaceutical compositions thereof and process for their preparation | |
| HUP0303043A2 (en) | Rhinological agents | |
| HUP0300385A2 (en) | Inhibitors of aspartyl protease | |
| HUP0002247A2 (en) | Protease inhibitors | |
| HUP0103431A2 (en) | Pharmaceutical, oral compositions containing 5-ht4 agonists or antagonists as active agent | |
| EA200400708A1 (en) | INHIBITORS 11-BETA-HYDROXYSTEROID DEGYDROGENASE TYPE 1 | |
| HUP0105280A2 (en) | Benzaldehyde derivatives and their pharmaceutical use and medicaments containing the compounds |