Heterocyclic compounds having tachykinin receptor antagonist activity their preparation and their use
US6159967A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 2, 1996 |
| Grant date | Dec 12, 2000 |
| Priority date | — |
| Expiry date | Dec 2, 2016 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D495/10
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Compounds of the formula and quaternary ammonium ions thereof, wherein R.sup.1 and R.sup.2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4, alkenylene; D is oxygen; E is C.sub.2 alkylene; G is C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene; and L is --C(R.sup.4)(R.sup.5), wherein R.sup.4 and R.sup.5 together with the carbon atom to which they are attached represent a C.sub.5 -C.sub.10 cycloalkyl or a C.sub.5 -C.sub.10 heterocyclic. Especially preferred are compounds wherein L represents ##STR1## wherein J is a C.sub.1 -C.sub.6 alkylene; Ar is a ring carbocyclic or aromatic heterocyclic and S*.fwdarw.O is a sulfoxide in which the sulfur atom is in the 5-configuration. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK.sub.1 and NK.sub.2 receptors.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.