Substituted-di-t-butylphenols

Claim 2

A compound of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, amino, lower alkylamino, di(lower alkylamino), lower acylamido, or hydroxy, and n is 0, 1 or 2, with the proviso that if n is 2, all R substituents combined contain no more than 6 carbon atoms; R' is hydrogen, lower alkyl, acetyl or trifluoroacetyl; A is carboxyl, tetrazolyl, N-methyltetrazolyl or and when A is carboxyl, B is a carbon-carbon bond, lower alkylene, lower alkenylene, lower alkylene containing one ether or thioether link in the alkylene chain, or when A is tetrazolyl or N-methyltetrazolyl, B is a carbon-carbon bond, -CH 2 - or and when A is B is a carbon-carbon bond; or a derivative of a compound wherein A is carboxyl, said derivative selected from the group consisting of a lower alkyl ester, a (lower)alkylamino(lower)alkyl ester, a pharmaceutically acceptable (lower)alkylamino(lower)alkyl ester acid-addition salt, and a pharmaceutically acceptable carboxylate salt, or a derivative of a compound wherein A is tetrazolyl, said derivative selected from a pharmaceutically acceptable alkali metal and an alkaline earth salt of the tetrazolyl moiety.

Claim 3

A compound accotding to Claim 1, wherein A is carboxyl.

Claim 4

A compound according to Claim 1, wherein A is tetrazolyl.

Claim 5

A compound according to Claim 2, wherein B is a carbon-carbon bond or methylene.

Claim 6

A compound according to Claim 1 wherein R is hydrogen.

Claim 7

A compound according to Claim 1, wherein -B-A is oriented meta or para to the Linking.

Claim 8

A compound according to Claim 1, wherein B is a carbon-carbon bond.

Claim 9

A pharmaceutical anti-allergic composition comprising a compound according to any one of claims 1 to 7 and a pharmaceutically acceptable vehicle, said compound being present in an amount effective for providing an anti-allergic response.

Claim 10

Use of a compound according to any one of claims 1 to 7 for preparation of a medicament for inhibiting bronchoconstriction due to an allergic response in a mammal.

Claim 11

A composition according to claim 8, wherein said composition is in a form for administration by inhalation.

Claim 12

A composition according to claim 8, wherein said composition is in a form for oral administration.

Claim 13

A method for inhibiting leukotriene synthesis in a mammal comprising administering to said mammal a compound according to Claim 1 in an amount effective to inhibit said synthesis.

Claim 14

A method for inhibiting lipoxygenase activity in a mammal comprising administering to said mammal a compound according to Claim 1 in an amount effective to inhibit said activity.

Claim 15

A compound of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, hydroxy or halogen; n is 0, 1 or 2, with the proviso that when n is 2, the R substituents combined contain no more than 6 carbon atoms; and B is a carbon-carbon bond, lower alkylene, lower alkenylene, lower alkylene containing one I ether or thioether link in the alkylene chain, or

Claim 16

A compound of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, hydroxy or halogen; n is 0, 1 or 2, with the proviso that when n is 2, the R substituents combined contain no more than 6 carbon atoms; and B is a carbon-carbon bond, lower alkylene, lower alkenylene, lower alkylene containing one I ether or thioether link in the alkylene chain, or

Claim 17

A compound of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, hydroxy, halogen, amino or lower acylamino; n is 0, 1 or 2, with the proviso that when n is 2, the R substituents combined contain no more than 6 carbon atoms; and B is a carbon-carbon bond, lowet alkylene, lowet alkenylene, lower alkylene containing one ether or thioether link in the alkylene chain, or with the proviso that -BCOOH is bonded to the phenyl ring ortho or meta when B is a carbon-carbon bond.

Claim 18

A compound of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, hydroxy, halogen, amino or lower acylamino; n is 0, 1 or 2, with the proviso that when n is 2, the R substituents combined contain no more than 6 carbon atoms; and B is a carbon-carbon bond, lowet alkylene, lowet alkenylene, lower alkylene containing one ether or thioether link in the alkylene chain, or with the proviso that -BCOOH is bonded to the phenyl ring ortho or meta when B is a carbon-carbon bond.

Claim 19

A compound of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, hydroxy or halogen; n is 0, 1 or 2, with the proviso that when n is 2, the R substituents combined contain no more than 6 carbon atoms; and B is a carbon-carbon bond, lower alkylene, lower alkenylene, lower alkylene containing one ether or thioether link in the alkylene chain, or,

Claim 20

A compound of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, hydroxy or halogen; n is 0, 1 or 2, with the proviso that when n is 2, the R substituents combined contain no more than 6 carbon atoms; and B is a carbon-carbon bond, lower alkylene, lower alkenylene, lower alkylene containing one ether or thioether link in the alkylene chain, or,

Claim 21

Use of a compound for preparation of a medicament for inhibiting bronchoconstriction due to an allergic response in a mammal, said antiallergic compound being of the formula: wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, amino, lower alkylamino, di(lower alkylamino), lower acylamido, or hydroxy, and n is 0, 1 or 2, with the proviso that if n is 2, all R substituents combined contain no more than 6 carbon atoms; A is carboxyl, tetrazolyl, N -methyltetrazolyl or and when A is carboxyl, B is a carbon-carbon bond, lower alkylene, lower alkenylene, lower alkylene containing one ether or thioether link in the alkylene chain, or when A is tetrazolyl or N-methyltetrazolyl, B is a carbon-carbon bond, -CH ? - or and when A is B is a carbon-carbon bond; or a derivative of a compound wherein A is carboxyl, said derivative selected from the group consisting of a lower alkyl ester, a (lower)alkylamino(lower)alkyl ester, a pharmaceutically acceptable (lower)alkylamino(lower)alkyl ester acid-addition salt, and a pharmaceutically acceptable carboxylate salt, or a derivative of a compound wherein A is tetrazolyl, said derivative selected from a pharmaceutically acceptable alkali metal and an alkaline earth salt of the tetrazolyl moiety.

Claim 22

Use of a compound for preparation of a medicament for inhibiting bronchoconstriction due to an allergic response in a mammal, said antiallergic compound being of the formula: wherein R is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, amino, lower alkylamino, di(lower alkylamino), lower acylamido, or hydroxy, and n is 0, 1 or 2, with the proviso that if n is 2, all R substituents combined contain no more than 6 carbon atoms; A is carboxyl, tetrazolyl, N -methyltetrazolyl or and when A is carboxyl, B is a carbon-carbon bond, lower alkylene, lower alkenylene, lower alkylene containing one ether or thioether link in the alkylene chain, or when A is tetrazolyl or N-methyltetrazolyl, B is a carbon-carbon bond, -CH ? - or and when A is B is a carbon-carbon bond; or a derivative of a compound wherein A is carboxyl, said derivative selected from the group consisting of a lower alkyl ester, a (lower)alkylamino(lower)alkyl ester, a pharmaceutically acceptable (lower)alkylamino(lower)alkyl ester acid-addition salt, and a pharmaceutically acceptable carboxylate salt, or a derivative of a compound wherein A is tetrazolyl, said derivative selected from a pharmaceutically acceptable alkali metal and an alkaline earth salt of the tetrazolyl moiety.