NO963254L - Makrocykliske difluorstatonderivater som er anvendbare som antivirale midler - Google Patents
Makrocykliske difluorstatonderivater som er anvendbare som antivirale midlerInfo
- Publication number
- NO963254L NO963254L NO963254A NO963254A NO963254L NO 963254 L NO963254 L NO 963254L NO 963254 A NO963254 A NO 963254A NO 963254 A NO963254 A NO 963254A NO 963254 L NO963254 L NO 963254L
- Authority
- NO
- Norway
- Prior art keywords
- pct
- hiv
- macrocyclic
- useful
- antivirals
- Prior art date
Links
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
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0205—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)3-C(=0)-, e.g. statine or derivatives thereof
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Oncology (AREA)
- Biochemistry (AREA)
- Communicable Diseases (AREA)
- Crystallography & Structural Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Foreliggende oppfinnelse tilveie- bringer nye makrocykliske difluor- statonderivater som er anvendbare som . antivirale midler. Nærmere spesifikt 1 er disse nye forbindelser anvendbare l som inhibitorer av retrovirale prote- iaser som er nødvendige for replikasjon, i særdeleshet HIV-1 og HIV-2 virale ,proteaser, ved forhindring eller behandling av infeksjon med humant 1immunosvekkelsesvirus (HIV), og ved behandling av påfølgende patologiske tilstander slik som det ervervede immunosvekkelsessyndrom (AIDS) i pattedyr som er i stand til å bli i infisert med HIV-virus. foi Dir.::- ai ^v :o»melen: (CH2),-0 ! og stereoisomerer, hydrater og £armas«ytislc akseptable salter derav hvori P2 er C, ,-a)k'/l, cykJopentyJ, hydroxy C,6-aJJcyl, fenyj, benzyl eJler 3-tetrahydrofuryJ; P-. er valgt fra gruppen bestående av hydrogen, -CHj, -Cfl(CH3)j, -CH2Ca(Ca])j, -CH(CH])(CH2CHj), -CHjSH, -CHjCSjSCHj, -CHjOH, -CS(CHj)OB, -CH2(CHj)]NH2, -CH,(CHj)2NHC(=NH)NHj, -CH2COjH, -CH2CHjCO2H, -CHjCONH2, -CHjCH2CONHj, -'benzyl. -CH2 . hydrogen, C. j.-alkyJ, hydfoxy C^j.-a CH([ {Cli2)d-0-C!:2) f-R;l alkyJen] -OR,, CHIY) IZ) , l , POL, -( hvori PDL ei -ICH2)a-2-, 3- el)er 4-pyridyJ; Y er hydroxy C^jj-aJkyl, Cl.6-alkyl eller (CHj) e-C6H4- (v) e , ; 2 er (CHj) - 0-CHO, Ci_5-alkylen-0-(CH2ld-(0-CH2-CH2)e-o-C1_6-aJkyl, r.HO . 4, CONHR4, (CH)-0-(CH eJJer (CHjJ, hvori V er OR. eller hydroxy C, ,-aJkylen; forutsatt at d* *> 2 når RS er piperazinyl, substituert piperazinyl, piperidyl eller tnorfolinyl; R, er som definert for R,, forutsatt at R, er forskjelJig fra hydrogen når R, er hydrogen, eller R. og R, tatt sammen med nitrogenatomet tiJ hvilket de er bundet, er valgt fra gruppen bestående av: (O (i) R4 er hydrogen, c,_g-aJkyJ, fenyl eJJer benzyj; R5 er piperazinyl, substituert pipcrazinyl, piperidyj, morfoJinyJ, pyridyl, pyrazinyl, pyrimidinyj eJJer fenyl, hvori substituert piperazinyj er piperazinyl substituert med ett nifogenatom derav med CHO, C (O) NHH., c, -alkvl eller rn D . 4 1-4 r R-, er pyrimidyl, pyridyl, pyrazinyj eller fenyJ; R8 er C1_6-alkylen, hydroxy C, ,-alkyl eller c._,-alkyl; a er null, l, 2 eller 3; b er null eller 1; d og d' er hver uavhengig l eller 2; e og e1 er hver uavhengig null, l eJler 2; \ f er null elJer en; og x er l, 2, 3 eller 4.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19208094A | 1994-02-04 | 1994-02-04 | |
| PCT/US1994/013711 WO1995021186A1 (en) | 1994-02-04 | 1994-11-28 | Macrocyclic difluorostatone derivatives useful as antiviral agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO963254L true NO963254L (no) | 1996-08-02 |
| NO963254D0 NO963254D0 (no) | 1996-08-02 |
Family
ID=22708156
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO963254A NO963254D0 (no) | 1994-02-04 | 1996-08-02 | Makrocykliske difluorstatonderivater som er anvendbare som antivirale midler |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US5969132A (no) |
| EP (1) | EP0742791B1 (no) |
| JP (1) | JP3574455B2 (no) |
| KR (1) | KR100367379B1 (no) |
| CN (1) | CN1142830A (no) |
| AT (1) | ATE198602T1 (no) |
| AU (1) | AU684875B2 (no) |
| CA (1) | CA2182476C (no) |
| DE (1) | DE69426574T2 (no) |
| DK (1) | DK0742791T3 (no) |
| ES (1) | ES2155515T3 (no) |
| FI (1) | FI963073A (no) |
| GR (1) | GR3035623T3 (no) |
| HU (1) | HUT74384A (no) |
| IL (1) | IL112514A0 (no) |
| NO (1) | NO963254D0 (no) |
| NZ (1) | NZ277410A (no) |
| PT (1) | PT742791E (no) |
| WO (1) | WO1995021186A1 (no) |
| ZA (1) | ZA95756B (no) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004111077A1 (en) | 2003-06-18 | 2004-12-23 | Tranzyme Pharma Inc. | Macrocyclic antagonists of the motilin receptor |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH672792A5 (no) * | 1985-02-19 | 1989-12-29 | Sandoz Ag | |
| DE3674131D1 (de) * | 1985-04-19 | 1990-10-18 | Upjohn Co | Substituierte dihalo-statin-reninhemmungsmittel. |
| WO1990000399A1 (en) * | 1988-07-08 | 1990-01-25 | Smithkline Beckman Corporation | Retroviral protease binding peptides |
| US5071837A (en) * | 1990-11-28 | 1991-12-10 | Warner-Lambert Company | Novel renin inhibiting peptides |
| HU210647B (en) * | 1991-01-02 | 1995-06-28 | Merrell Dow Pharma | Process for producing antiviral difluoro-statone derivatives and pharmaceutical compositions containing them |
| HUT76648A (en) * | 1994-07-15 | 1997-10-28 | Merrell Pharma Inc | Difluorostatone, pharmaceutical compositions containing them and process for producing them |
-
1994
- 1994-11-28 JP JP52059495A patent/JP3574455B2/ja not_active Expired - Fee Related
- 1994-11-28 CA CA002182476A patent/CA2182476C/en not_active Expired - Fee Related
- 1994-11-28 KR KR1019960704227A patent/KR100367379B1/ko not_active IP Right Cessation
- 1994-11-28 ES ES95903633T patent/ES2155515T3/es not_active Expired - Lifetime
- 1994-11-28 EP EP95903633A patent/EP0742791B1/en not_active Expired - Lifetime
- 1994-11-28 WO PCT/US1994/013711 patent/WO1995021186A1/en active IP Right Grant
- 1994-11-28 DE DE69426574T patent/DE69426574T2/de not_active Expired - Fee Related
- 1994-11-28 AT AT95903633T patent/ATE198602T1/de not_active IP Right Cessation
- 1994-11-28 PT PT95903633T patent/PT742791E/pt unknown
- 1994-11-28 HU HU9602158A patent/HUT74384A/hu unknown
- 1994-11-28 US US08/676,208 patent/US5969132A/en not_active Expired - Fee Related
- 1994-11-28 DK DK95903633T patent/DK0742791T3/da active
- 1994-11-28 CN CN94194939A patent/CN1142830A/zh active Pending
- 1994-11-28 NZ NZ277410A patent/NZ277410A/en unknown
- 1994-11-28 AU AU12622/95A patent/AU684875B2/en not_active Ceased
-
1995
- 1995-01-31 ZA ZA95756A patent/ZA95756B/xx unknown
- 1995-02-01 IL IL11251495A patent/IL112514A0/xx unknown
-
1996
- 1996-08-02 NO NO963254A patent/NO963254D0/no not_active Application Discontinuation
- 1996-08-02 FI FI963073A patent/FI963073A/fi not_active IP Right Cessation
-
2001
- 2001-03-23 GR GR20010400468T patent/GR3035623T3/el not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| ZA95756B (en) | 1995-10-05 |
| EP0742791B1 (en) | 2001-01-10 |
| WO1995021186A1 (en) | 1995-08-10 |
| AU1262295A (en) | 1995-08-21 |
| CN1142830A (zh) | 1997-02-12 |
| CA2182476C (en) | 2000-12-26 |
| NZ277410A (en) | 1997-02-24 |
| DE69426574T2 (de) | 2001-08-09 |
| DE69426574D1 (de) | 2001-02-15 |
| HU9602158D0 (en) | 1996-09-30 |
| HUT74384A (en) | 1996-12-30 |
| KR100367379B1 (ko) | 2003-04-11 |
| DK0742791T3 (da) | 2001-04-02 |
| ES2155515T3 (es) | 2001-05-16 |
| FI963073A0 (fi) | 1996-08-02 |
| AU684875B2 (en) | 1998-01-08 |
| IL112514A0 (en) | 1995-05-26 |
| US5969132A (en) | 1999-10-19 |
| JPH09508417A (ja) | 1997-08-26 |
| ATE198602T1 (de) | 2001-01-15 |
| PT742791E (pt) | 2001-06-29 |
| GR3035623T3 (en) | 2001-06-29 |
| EP0742791A1 (en) | 1996-11-20 |
| JP3574455B2 (ja) | 2004-10-06 |
| FI963073A (fi) | 1996-08-02 |
| NO963254D0 (no) | 1996-08-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC2A | Withdrawal, rejection or dismissal of laid open patent application |