EP 0756590 A1 19970205 - SYNTHESIS OF PROTOTYPES FOR RENIN INHIBITORS
Title (en)
SYNTHESIS OF PROTOTYPES FOR RENIN INHIBITORS
Title (de)
SYNTHESE VON RENIN-INHIBITOR-PROTOTYPEN
Title (fr)
SYNTHESE DES PROTOTYPES DES INHIBITEURS DE LA RENINE
Publication
Application
Priority
- CA 2121898 A 19940421
- IB 9500257 W 19950412
Abstract (en)
[origin: WO9529150A1] Prototype renin inhibitors having general structure (I), where n is 0-3 inclusive, A are either both hydrogen atoms or together are a single carbon-nitrogen bond, R1 is hydrogen, or hydrocarbylcarboxy wherein the hydrocarbyl entity is selected from the group consisting of alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 10 carbon atoms, R2 and R3 or independently alkyl of 1 to 4 carbon atoms, R4 is alkyl of 1 to 6 carbon atoms or a substituent of aliphatic character such as, for example, butyl, 2-morpholinoethyl or 2-carbamoyl-2-methyl-propyl, R5 is selected from aromatics, substitued aromatics and heteroaromatics, substituted or unsubstituted cycloalkyls, cycloalkenes having 3 to 8 carbon atoms, with substituents selected from alkyl, alkoxy of 3 to 10 carbon atoms and alkoxy derivatives such as 3-methoxy-propyloxy, primary and secondary amides, alkyl derivatives, are prepared by novel multistep synthesis. Such compounds are valuable intermediates for the manufacture of pharmaceutical such as Renin inhibitors and HIV-protease inhibitors.
IPC 1-7
C07C 231/12; C07C 231/02; C07D 405/04; C07C 237/20; C07C 271/22
IPC 8 full level
C12N 9/99 (2006.01); C07B 61/00 (2006.01); C07C 231/02 (2006.01); C07C 231/12 (2006.01); C07C 237/20 (2006.01); C07C 237/22 (2006.01); C07C 269/02 (2006.01); C07C 271/22 (2006.01); C07D 405/04 (2006.01)
CPC (source: EP)
C07C 231/12 (2013.01); C07C 269/02 (2013.01); C07D 405/04 (2013.01)
Citation (search report)
See references of WO 9529150A1
Designated contracting state (EPC)
AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9529150 A1 19951102; AU 2082395 A 19951116; CA 2121898 A1 19951022; CN 1147810 A 19970416; CZ 306596 A3 19970115; EP 0756590 A1 19970205; FI 963743 A0 19960920; FI 963743 A 19960920; HU 9602892 D0 19961230; HU T74743 A 19970228; IL 113401 A0 19950731; JP H09512266 A 19971209; PL 316677 A1 19970203; ZA 953187 B 19951023
DOCDB simple family (application)
IB 9500257 W 19950412; AU 2082395 A 19950412; CA 2121898 A 19940421; CN 95192655 A 19950412; CZ 306596 A 19950412; EP 95913311 A 19950412; FI 963743 A 19960920; HU 9602892 A 19950412; IL 11340195 A 19950417; JP 52750095 A 19950412; PL 31667795 A 19950412; ZA 953187 A 19950420