"PYRROLIDINE DERIVATIVES-CCR-3 RECEPTOR ANTAGONISTS"

Application IN/PCT/2001/693/CHE published 2005-03-04, filed 2001-05-18
This invention relates to certain 3-aminomethylpyrrolidine derivatives of Formula (I), wherein: Z is -N- or -(N+r)- X- wherein R is alkyl, haloalkyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, or cyanoalkyl, and X- is a pharmaceutically acceptable counterion; Ar1 and Ar2 are, independently of each other, aryl or heteroaryl; Q is straight or branched alkylene with 1-3 carbon atoms; R1 is hydrogen or alkyl; A is either: (I) -N(R2)C(O)- when: B is: (i) an alkylene with 1-4 carbon atoms inclusive wherein one of the carbon atoms may optionally be replaced by a group selected from -C(O)-, -N(R4)-, -O-, -S(O)n- (where n is 0, 1 or 2), -NR5C(O)- and -N(R6)SO2-; or (ii) an alkynlene chain; or (II) a group selected from -N(R2)C(S)-, -N(R2)C(O)N(R3)-, -N(R2)SO2-, -N(R2)SO2N(R3)-, -N(R2)C(O)O-, and -OC(O)N(R3)- when: B is: (i) a bond; (ii) an alkylene chain of 1-4 carbon atoms inclusive wherein one of the carbon atoms may optionally be replaced by a group selected from -C(O)-, -N(R4)-, -O-, -S(O)n- (where n is 0, 1 or 2), -NR5C(O)- and -N(R6)SO2-; (iii) an alkenylene chain; or (iv) an alkynylene chain; that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Applicant

F HOFFMANN-LA ROCHE AG
of 124 Grenzacherstrasse,, CH-4070 Basle,, a Swiss Company, SWITZERLAND.

Inventor

International Info

Classification: C07D 207/09, A61K 31/40 & C07D 401/12
Publication Number: PCT/EP99/08665

Priority Information

60/109,297 US 1998-11-20