NO995822L - Sulfate salt of an HIV protease inhibitor which has improved oral absorption and bioavailability - Google Patents
Sulfate salt of an HIV protease inhibitor which has improved oral absorption and bioavailabilityInfo
- Publication number
- NO995822L NO995822L NO995822A NO995822A NO995822L NO 995822 L NO995822 L NO 995822L NO 995822 A NO995822 A NO 995822A NO 995822 A NO995822 A NO 995822A NO 995822 L NO995822 L NO 995822L
- Authority
- NO
- Norway
- Prior art keywords
- protease inhibitor
- sulfate salt
- hiv protease
- bioavailability
- oral absorption
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Sulfatsaltet av en HIV- proteaseinhibitor, Forbindelse A, ¿H2S04 (A) som er anvendelig for behandling av AIDS, ARC eller HIV-infeksjon hos voksne og barn, nærmere bestemt et sul- fatsalt av HIV-proteaseinhibitoren, Forbindelse A, som oppviser forbedret oppløselighet i fortynnet HCl-oppløs- ning (magesyre), hvorved det oppnås meget bedre oral absorpsjon og biotil- gjengelighet i dyremodeller. Det be- skrives også fremgangsmåter for frem- stilling av sulfatsaltet av de angjeld- ende HIV-proteaseinhibitorforbindelser.The sulfate salt of an HIV protease inhibitor, Compound A, ¿H2SO4 (A), useful for the treatment of AIDS, ARC or HIV infection in adults and children, in particular a sulfate salt of the HIV protease inhibitor, Compound A, which exhibits improved solubility in dilute HCl solution (gastric acid), thus achieving much better oral absorption and bioavailability in animal models. Methods are also described for the preparation of the sulfate salt of the HIV protease inhibitor compounds concerned.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4795097P | 1997-05-29 | 1997-05-29 | |
| GBGB9714320.0A GB9714320D0 (en) | 1997-07-07 | 1997-07-07 | Hiv protease inhibitor |
| PCT/US1998/010633 WO1998054178A1 (en) | 1997-05-29 | 1998-05-26 | Sulfate salt of an hiv protease inhibitor having an improved oral absorption and bioavailability |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO995822D0 NO995822D0 (en) | 1999-11-26 |
| NO995822L true NO995822L (en) | 2000-01-28 |
Family
ID=26311845
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO995822A NO995822L (en) | 1997-05-29 | 1999-11-26 | Sulfate salt of an HIV protease inhibitor which has improved oral absorption and bioavailability |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP0986554A1 (en) |
| JP (1) | JP3267632B2 (en) |
| KR (1) | KR20010013042A (en) |
| CN (1) | CN1257497A (en) |
| AU (1) | AU730245B2 (en) |
| BG (1) | BG103923A (en) |
| BR (1) | BR9809498A (en) |
| CA (1) | CA2291086A1 (en) |
| EA (1) | EA199901095A1 (en) |
| EE (1) | EE9900543A (en) |
| HR (1) | HRP980283A2 (en) |
| HU (1) | HUP0004621A3 (en) |
| ID (1) | ID23858A (en) |
| IL (1) | IL132779A0 (en) |
| IS (1) | IS5240A (en) |
| NO (1) | NO995822L (en) |
| PE (1) | PE75099A1 (en) |
| PL (1) | PL336847A1 (en) |
| SK (1) | SK163299A3 (en) |
| TR (1) | TR199902816T2 (en) |
| TW (1) | TW438799B (en) |
| WO (1) | WO1998054178A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003514910A (en) * | 1999-11-24 | 2003-04-22 | メルク エンド カムパニー インコーポレーテッド | Gamma-hydroxy-2- (fluoroalkylaminocarbonyl) -1-piperazinepentanamides as HIV protease inhibitors |
| WO2002022582A2 (en) * | 2000-09-14 | 2002-03-21 | Ortho-Mcneil Pharmaceutical, Inc. | Solid salt forms of n-[2-[4-[2-(1-methylethoxy)phenyl]-1-piperazinyl]ethyl]-2-oxo-1-piperidineacetamide |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ278201A (en) * | 1993-12-15 | 1998-01-26 | Merck & Co Inc | Bicyclic heterocyclically substituted piperazine derivatives as hiv protease inhibitors |
-
1998
- 1998-05-20 TW TW087107834A patent/TW438799B/en active
- 1998-05-26 TR TR1999/02816T patent/TR199902816T2/en unknown
- 1998-05-26 ID IDW991462A patent/ID23858A/en unknown
- 1998-05-26 PL PL98336847A patent/PL336847A1/en unknown
- 1998-05-26 EE EEP199900543A patent/EE9900543A/en unknown
- 1998-05-26 EP EP98923741A patent/EP0986554A1/en not_active Withdrawn
- 1998-05-26 IL IL13277998A patent/IL132779A0/en unknown
- 1998-05-26 BR BR9809498-0A patent/BR9809498A/en not_active Application Discontinuation
- 1998-05-26 KR KR1019997011018A patent/KR20010013042A/en not_active Application Discontinuation
- 1998-05-26 JP JP50079999A patent/JP3267632B2/en not_active Expired - Fee Related
- 1998-05-26 WO PCT/US1998/010633 patent/WO1998054178A1/en not_active Application Discontinuation
- 1998-05-26 CN CN98805372A patent/CN1257497A/en active Pending
- 1998-05-26 HU HU0004621A patent/HUP0004621A3/en unknown
- 1998-05-26 CA CA002291086A patent/CA2291086A1/en not_active Abandoned
- 1998-05-26 SK SK1632-99A patent/SK163299A3/en unknown
- 1998-05-26 EA EA199901095A patent/EA199901095A1/en unknown
- 1998-05-26 AU AU75959/98A patent/AU730245B2/en not_active Ceased
- 1998-05-28 PE PE1998000432A patent/PE75099A1/en not_active Application Discontinuation
- 1998-05-28 HR HR9714320.0A patent/HRP980283A2/en not_active Application Discontinuation
-
1999
- 1999-11-09 IS IS5240A patent/IS5240A/en unknown
- 1999-11-24 BG BG103923A patent/BG103923A/en unknown
- 1999-11-26 NO NO995822A patent/NO995822L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO1998054178A1 (en) | 1998-12-03 |
| KR20010013042A (en) | 2001-02-26 |
| BG103923A (en) | 2000-06-30 |
| HRP980283A2 (en) | 1999-08-31 |
| IL132779A0 (en) | 2001-03-19 |
| NO995822D0 (en) | 1999-11-26 |
| HUP0004621A2 (en) | 2002-03-28 |
| SK163299A3 (en) | 2000-07-11 |
| AU7595998A (en) | 1998-12-30 |
| EE9900543A (en) | 2000-06-15 |
| EA199901095A1 (en) | 2000-08-28 |
| PL336847A1 (en) | 2000-07-17 |
| CN1257497A (en) | 2000-06-21 |
| TW438799B (en) | 2001-06-07 |
| BR9809498A (en) | 2000-06-20 |
| ID23858A (en) | 2000-05-25 |
| CA2291086A1 (en) | 1998-12-03 |
| TR199902816T2 (en) | 2000-02-21 |
| PE75099A1 (en) | 1999-08-11 |
| EP0986554A1 (en) | 2000-03-22 |
| JP2000513747A (en) | 2000-10-17 |
| HUP0004621A3 (en) | 2002-04-29 |
| IS5240A (en) | 1999-11-09 |
| JP3267632B2 (en) | 2002-03-18 |
| AU730245B2 (en) | 2001-03-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC2A | Withdrawal, rejection or dismissal of laid open patent application |