Claims
- 1. A heterocycle of the formula I
- wherein Q is isoquinolinyl which may optionally bear one or two substituents selected from halogeno, oxo and (1-4C)alkyl;
- wherein A is (1-6C)alkylene, (3-6C)alkenylene or (3-6C)alkynylene;
- wherein X is oxy, thio or imino;
- wherein Ar is phenylene which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, ureido, (1-4C)alkyl, (1-4C)alkoxy, fluoro-(1-4C)alkyl and cyano-(1-4C)alkoxy;
- wherein R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl;
- and wherein R.sup.2 and R.sup.3 together form a group of the formula --A.sub.2 --X.sub.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-3C)alkylene and X.sup.2 is oxy, and which ring may bear one or two substituents, which may be the same or different, selected from hydroxy, (1-4C)alkyl and (1-4C)alkoxy;
- or a pharmaceutically-acceptable salt thereof.
- 2. A heterocycle of the formula I as claimed in claim 1 wherein Q is isoquinolinyl which may optionally bear one or two substitutents selected from fluoro, chloro, oxo, methyl, ethyl and propyl;
- wherein A is methylene, 1-propenylene or 1-propynylene;
- wherein X is oxy or imino;
- wherein Ar is 1,3-phenylene or 1,4-phenylene which may optionally bear one or two substituents selected from fluoro, chloro, hydroxy, amino, ureido, methyl, methoxy, trifluoromethyl and cyanomethoxy;
- wherein R.sup.1 is methyl, ethyl, allyl or 2-propynyl; and
- wherein R.sup.2 and R.sup.3 together form a group of the formula --A.sub.2 --X.sub.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 which may be the same or different, each in methylene, ethylene or trimethylene and X.sup.2 is oxy, and which ring may bear one or two substituents selected from hydroxy, methyl, ethyl and methoxy;
- or a pharmaceutically-acceptable salt thereof.
- 3. A heterocycle of the formula I as claimed in claim 1 wherein Q is 3-isoquinolinyl, 6-isoquinolinyl or 7-isoquinolinyl which may optionally bear one or two substituents selected from fluoro, chloro and methyl;
- A is methylene or 1-propynylene;
- X is oxy;
- Ar is 1,3-phenylene or 1,4-phenylene which may optionally bear one substituent selected from fluoro, chloro, hydroxy, amino, methyl, methoxy, trifluoromethyl and cyanomethoxy;
- R.sup.1 is methyl, ethyl, allyl or 2-propynyl; and
- R.sup.2 and R.sup.3 together form a group of the formula --A.sub.2 --X.sub.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is methylene, ethylene or trimethylene and X.sup.2 is oxy, and which ring may bear a substituent selected from hydroxy, methyl, methoxy and ethoxy;
- or a pharmaceutically-acceptable salt thereof.
- 4. A heterocycle of the formula I as claimed in claim 1 wherein Q is 3-isoquinolinyl which may optionally bear one or two substituents selected from fluoro, methyl and ethyl;
- wherein A is methylene;
- wherein X is oxy;
- wherein Ar is 1,3-phenylene or 1,4-phenylene which may optionally bear one or two substituents selected from fluoro, hydroxy, amino, ureido, methoxy, trifluoromethyl and cyanomethoxy;
- wherein R.sup.1 is methyl, ethyl or allyl; and
- wherein R.sup.2 and R.sup.3 together form a group of the formula --A.sub.2 --X.sub.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached defines a ring having 5 or 6 ring atoms, wherein A.sup.2 is ethylene, A.sup.3 is methylene or ethylene and X.sup.2 is oxy, and which ring may bear one or two substituents selected from hydroxy, methyl and methoxy;
- or a pharmaceutically-acceptable salt thereof.
- 5. A heterocycle of the formula I as claimed in claim 1 selected from the group consisting of:
- 4-[5-fluoro-3-(3-(1-isoquinolinyl)prop-2-ynyloxy)phenyl]-4-methoxytetrahydropyran and
- 4-[5-fluoro-3-(isoquinolin-3-ylmethoxy)phenyl]-4-methoxytetrahydropyran;
- or a pharmaceutically-acceptable salt thereof.
- 6. A pharmaceutical composition which comprises a heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, as claimed in claim 1 in association with a pharmaceutically-acceptable diluent or carrier.
- 7. A method of treating a disease or medical condition mediated alone or in part by one or more leukotrienes which comprises administering to a warm-blooded animal requiring such treatment an effective amount of a heterocycle of the formula I, or a pharmaceutically-acceptable salt thereof, as claimed in claim 1.
Priority Claims (2)
Number |
Date |
Country |
Kind |
89400560 |
Feb 1989 |
EPX |
|
89401493 |
May 1989 |
EPX |
|
Parent Case Info
This is a division of application No. 07/881,133 filed May 11, 1992, now U.S. Pat. No. 5,236,919, which is a division of application No. 07/758,491 filed Sep. 5, 1991, now U.S. Pat. No. 5,134,148, which is a file wrapper continuation of application No. 07/485,875 filed Feb. 27, 1990, now abandoned.
US Referenced Citations (18)
Foreign Referenced Citations (6)
Number |
Date |
Country |
0110405 |
Jun 1984 |
EPX |
0181568 |
May 1986 |
EPX |
0190722 |
Aug 1986 |
EPX |
0200101 |
Dec 1986 |
EPX |
0271287 |
Jun 1988 |
EPX |
0349062 |
Jan 1990 |
EPX |
Non-Patent Literature Citations (1)
Entry |
Musser et al. Journal of Medicinal Chemistry, vol. 30, No. 1, Jan. 1987, pp. 96-104. |
Divisions (2)
|
Number |
Date |
Country |
Parent |
881133 |
May 1992 |
|
Parent |
758491 |
Sep 1991 |
|
Continuations (1)
|
Number |
Date |
Country |
Parent |
485875 |
Feb 1990 |
|