EP1150956A1 - Inhibiteurs non nucleosidiques de la transcriptase inverse - Google Patents

Inhibiteurs non nucleosidiques de la transcriptase inverse

Info

Publication number
EP1150956A1
EP1150956A1 EP99943591A EP99943591A EP1150956A1 EP 1150956 A1 EP1150956 A1 EP 1150956A1 EP 99943591 A EP99943591 A EP 99943591A EP 99943591 A EP99943591 A EP 99943591A EP 1150956 A1 EP1150956 A1 EP 1150956A1
Authority
EP
European Patent Office
Prior art keywords
fluoro
valyloxy
urea
cyclopropyl
propionylphenyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP99943591A
Other languages
German (de)
English (en)
Inventor
Xiao-Xiong Zhou
Nils-Gunnar Johansson
Horst Wähling
Christian Sund
Lourdes Salvador
Stefan LINDSTRÖM
Hans Wallberg
Christer Sahlberg
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Medivir AB
Original Assignee
Medivir AB
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US09/249,317 external-priority patent/US6458772B1/en
Application filed by Medivir AB filed Critical Medivir AB
Priority claimed from PCT/SE1999/001403 external-priority patent/WO2000047561A1/fr
Publication of EP1150956A1 publication Critical patent/EP1150956A1/fr
Withdrawn legal-status Critical Current

Links

Definitions

  • N-protecting group or “N-protected” as used herein refers to those groups intended to protect the N-terminus of an amino acid or peptide or to protect an amino group against undesirable reactions during synthetic procedures. Commonly used N-protecting groups are disclosed in Greene, "Protective Groups in Organic Synthesis” (John Wiley & Sons, New York, 1981 ), which is hereby incorporated by reference.
  • the release of a compound of Formula P-2 from orally administered prodrugs of Formulae P3 to P8 were monitored in rats.
  • the compounds of Examples 1 to 6 were made up in a propylene glycol vehicle and orally administered to paired fasted male Sprague Dawley rats at a dose corresponding to 0.027 mmol/kg. At 30, 60, 120, 240 & 360 minutes, 0.2 ml blood were collected, centrifuged and frozen for later analysis.

Abstract

L'invention se rapporte à des inhibiteurs non nucléosidiques de la transcriptase inverse, représentés par la formule (P-1), dans laquelle Ar1 est une structure en anneau, mono ou bicyclique, insaturée, éventuellement substituée, comportant 0 à 3 hétéroatomes sélectionnés parmi S, O et N; Ar2 est une structure en anneau monocyclique, aromatique, éventuellement substituée, comportant au moins un hétéroatome d'azote et 0 à 2 hétéroatomes sélectionnés parmi S, O et N; R4 et R5 sont indépendamment H ou cycloalkyle C3-C8, alkyle C1-C6, alcényle C2-C6, alkynyle C2-C8, alcoxy C1-C5, alcanoyloxy C1-C4, alkylthio C1-C4, amino, carboxy, carbamoyle, cyano, halo, hydroxy, aminométhyle, hydroxyméthyle, carboxyméthyle ou mercapto alkyle C1-C6 à substitution halo, nitro; ou R4 et R5 forment ensemble une structure en anneau ayant de 3 à 6 éléments et éventuellement substituée; R6 est O ou S; Rx est le reste d'un acide aminé naturel ou non naturel et L* est une fraction de liaison qui est liée par éther-, carbonate- ou ester- à l'oxygène adjacent et associée par liaison ester à Rx. L'invention se rapporte également à des sels pharmaceutiquement acceptables de ces inhibiteurs qui s'avèrent être des agents anti-VIH dotés de propriétés pharmacocinétiques intéressantes.
EP99943591A 1999-02-12 1999-08-18 Inhibiteurs non nucleosidiques de la transcriptase inverse Withdrawn EP1150956A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US249317 1999-02-12
US09/249,317 US6458772B1 (en) 1909-10-07 1999-02-12 Prodrugs
PCT/SE1999/000194 WO1999041275A1 (fr) 1998-02-13 1999-02-15 Promedicaments
WOPCT/SE99/00194 1999-02-15
PCT/SE1999/001403 WO2000047561A1 (fr) 1999-02-12 1999-08-18 Inhibiteurs non nucleosidiques de la transcriptase inverse

Publications (1)

Publication Number Publication Date
EP1150956A1 true EP1150956A1 (fr) 2001-11-07

Family

ID=26663485

Family Applications (1)

Application Number Title Priority Date Filing Date
EP99943591A Withdrawn EP1150956A1 (fr) 1999-02-12 1999-08-18 Inhibiteurs non nucleosidiques de la transcriptase inverse

Country Status (3)

Country Link
EP (1) EP1150956A1 (fr)
AU (1) AU770801B2 (fr)
CA (1) CA2362135A1 (fr)

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0047561A1 *

Also Published As

Publication number Publication date
CA2362135A1 (fr) 2000-08-17
AU5665899A (en) 2000-08-29
AU770801B2 (en) 2004-03-04

Similar Documents

Publication Publication Date Title
WO2000047561A1 (fr) Inhibiteurs non nucleosidiques de la transcriptase inverse
US6458772B1 (en) Prodrugs
KR20010033595A (ko) 아스파틸 프로테아제 억제제의 전구약물
WO1999033792A2 (fr) Promedicaments des inhibiteurs de l'aspartyl-transferase
BRPI0611435A2 (pt) derivados de 2-amido-6-amino-8-oxopurina, composições farmacêuticas, uso e processo de preparo dos mesmos
EP2956437B1 (fr) Dérivés d'albicidine pour le traitement d'infections bactériennes
JP3844654B2 (ja) レトロウイルス逆転写酵素およびｂ型肝炎ウイルス（ｈｂｖ）のｄｎａポリメラーゼのインヒビターを含む抗ウイルス剤などのヌクレオシドアナログ
JP2018501268A (ja) チゾキサニドホスフェート及びアルカンスルホネート並びにその医薬用途
CN114591201A (zh) 具有HDACi药效团的β-榄香烯衍生物及其制备方法和应用
JP2021519320A (ja) 新規のアルビシジン誘導体、それらの使用および合成
US20020128301A1 (en) Non-nucleoside reverse transcriptase inhibitors
CA2318694C (fr) Antiviraux
JP4652647B2 (ja) セラミド類似体類、それらの調製方法及び抗腫瘍剤としてのそれらの使用
EP1150956A1 (fr) Inhibiteurs non nucleosidiques de la transcriptase inverse
ES2211116T3 (es) Nucleosidos.
JPH10500394A (ja) 多重薬剤耐性細胞を抗腫瘍剤に対して感受性にするための多環式ラクタム誘導体
WO2011061590A1 (fr) Nouveaux dérivés carboxamides comme inhibiteurs du vih
AU775578B2 (en) Nucleosides analgoues, such as antivirals including inhibitors of retroviral reverse transcriptase and the DNA polymerase of hepatitis B virus (HBV)
AU750407B2 (en) Prodrugs of phosphorous-containing pharmaceuticals
WO2008069611A1 (fr) Procédé de préparation de dérivées de n-phénylamide et composition prévenant ou traitant les troubles ischémiques les comprenant
MXPA00001593A (es) Analogos de nucleosidos, tales como antivirales incluyendo inhibidores de transcriptasa inversa retroviral y la adn-polimerasa del virus de hepatitis b (vhb)

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 20010810

AK Designated contracting states

Kind code of ref document: A1

Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

AX Request for extension of the european patent

Free format text: AL;LT;LV;MK;RO;SI

17Q First examination report despatched

Effective date: 20021021

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN

18D Application deemed to be withdrawn

Effective date: 20040615