Claims
- 1. A compound of formula I: wherein
- X.sup.j is hydrogen or (C.sub.1 -C.sub.6)alkyl;
- B.sup.j is --N(R.sup.jh)-- and L.sup.j is a hydrocarbon chain selected from trimethylene, 2,2-dimethylprop-1,3-yl or B.sup.j is --N.dbd. and L.sup.j is a hydrocarbon chain in which the 1-position is bound to B.sup.j and L.sup.j is cis,cis-prop-2-en-1-ylidin-3-yl;
- J.sup.j is independently oxygen or sulfur;
- R.sup.jh is independently hydrogen or (C.sub.1 -C.sub.6)alkyl;
- Q.sup.2 is a nitrogen-linked five-membered aromatic ring containing 1-4 nitrogens, which is substituted at a ring position adjacent to the nitrogen-link by a group Q.sup.5 ;
- Q.sup.3 is hydrogen or (C.sub.1 -C.sub.3)alkyl;
- Q.sup.4 is phenyl which may bear one or two substituents independently selected from halo, trifluoromethyl, hydroxy, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkyl and methylenedioxy; or Q.sup.4 is thienyl, imidazolyl, benzothiophenyl or naphthyl any of which may bear a halo substituent; or Q.sup.4 is biphenylyl; or Q.sup.4 is carbon-linked indolyl which may bear a benzyl substituent at the 1-position; and
- Q.sup.5 is selected from the group consisting of phenyl, benzyl, phenethyl and naphthyl, wherein any phenyl ring or naphthyl may bear one or more substituents selected from (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, methylenedioxy, halogeno, hydroxy, (C.sub.1 -C.sub.4)acyloxy and NR.sup.A R.sup.B in which R.sup.A and R.sup.B are independently hydrogen or (C.sub.1 -C.sub.3)alkyl, or R.sup.A is hydrogen or (C.sub.1 -C.sub.3)alkyl and R.sup.B is (C.sub.1 -C.sub.4)acyl;
- or the N-oxide of the piperidino nitrogen indicated by .DELTA.;
- or a pharmaceutically acceptable salt thereof;
- or a quaternary ammonium salt thereof in which the piperidino nitrogen indicated by .DELTA. is a quadricovalent ammonium nitrogen wherein the fourth radical on the nitrogen R.sup.1 is (C.sub.1 -C.sub.4)alkyl or benzyl and the associated counterion A is a pharmaceutically acceptable anion.
- 2. The compound according to claim 1, wherein:
- Bj is --N(R.sup.jh)--;
- L.sup.j is a hydrocarbon chain selected from trimethylene, 2,2-dimethylprop-1,3-yl; and
- Q.sup.4 is phenyl, which may bear one or two substituents independently selected from halo, trifluoromethyl, hydroxy, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkyl and methylenedioxy.
- 3. The compound according to claim 1, wherein:
- B.sup.j is --N(R.sup.jh)--;
- L.sup.j is trimethylene;
- J.sup.j and J.sup.ja is oxygen;
- Q.sup.3 is hydrogen;
- Q.sup.4 is phenyl, which may bear one or two substituents independently selected from halo, trifluoromethyl, hydroxy, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkyl and methylenedioxy; and
- Q.sup.5 is phenyl.
- 4. The compound according to claim 3, wherein:
- X.sup.j is hydrogen;
- R.sup.jh is hydrogen;
- Q.sup.4 is 3,4,-dichlorophenyl; and
- Q.sup.2 and Q.sup.4 together form a substituent selected from ##STR3##
- 5. A pharmaceutical composition, comprising: a compound according to claim 1; and
- a pharmaceutically acceptable diluent or carrier.
- 6. A pharmaceutical composition, comprising:
- a compound according to claim 3; and
- a pharmaceutically acceptable diluent or carrier.
- 7. A method of treating asthma and related conditions involving bronchoconstriction, increased microvascular permeability, vasodilation or activation of mast cells, comprising the step of administering an effective amount of a compound according to claim 1.
- 8. A method of treating asthma and related conditions involving bronchoconstriction, increased microvascular permeability, vasodilation or activation of mast cells, comprising the step of administering an effective amount of a compound according to claim 3.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9508786 |
Apr 1995 |
GBX |
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Parent Case Info
This is a division of application Ser. No. 08/635,161 filed Apr. 23, 1996 U.S. Pat. No. 5,889,024.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
5236921 |
Emonds-Al et al. |
Aug 1993 |
|
5731309 |
Bernstein et al. |
Mar 1998 |
|
Divisions (1)
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Number |
Date |
Country |
Parent |
635161 |
Apr 1996 |
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