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US 5,457,122 AGranted
Phenylalkan(en)oic acid
AssigneeOno Pharmaceutical Co., Ltd.
InventorsMitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
Life of this patent
Estimating the term…
Abstract
The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.
Claims13
A phenylalkan(en)oic acid represented by the following formula:
- ##STR191## wherein A is:
- i) --NHCO--,
- ii) --O--,
- iii) --NHSO.sub.2 --,
- iv) --CO--,
- v) --CH.sub.2 --, or
- vi) --CH(OH)--;
- W is:
- i) C.sub.1-13 alkylene,
- ii) phenylene, or
- iii) ##STR192## R.sup.1 is:
- i) a saturated or unsaturated, unsubstituted 4-7 membered monocyclic hetero ring containing one nitrogen as a hetero atom,
- ii) a saturated or unsaturated, 4-7 membered monocyclic hetero ring containing one nitrogen as a hetero atom, wherein said ring is substituted by an oxo group, and wherein said oxo group is present on the carbon atom adjacent to said nitrogen atom, or
- iii) ##STR193## where one of R.sup.2 is a thiazole ring, isothiazole ring, thiadiazoline ring or partially or fully saturated ring thereof, and the other R.sup.2 is a:
- i) hydrogen,
- ii) C.sub.1-4 alkyl, or
- iii) thiazole ring, isothiazole ring, thiadiazoline ring or partially or fully saturated ring thereof, or
- two R.sup.2, taken together with the nitrogen, form an indole ring, an isoindole ring, a quinoline ring, an isoquinoline ring, a carbazole ring, an acridine ring, an oxazole ring, an isooxazole ring, a furazan ring, or a partially or fully saturated ring thereof, or a morpholine ring;
- Y is ethylene or vinylene;
- D is:
- i) --Z--B, or
- ii) ##STR194## Z is C.sub.3-11 alkylene or alkenylene;
- B is ##STR195## or Z, taken together with B, is C.sub.3-22 alkyl;
- R.sup.3 is:
- i) hydrogen,
- ii) halogen,
- iii) C.sub.1-8 alkyl, alkoxy or alkylthio or
- iv) C.sub.2-8 alkenyl, alkenyloxy or alkenylthio;
- n is 1-3;
- R.sup.4 is C.sub.1-7 alkylene;
- R.sup.5 is:
- i) C.sub.1-12 alkyl,
- ii) C.sub.2-12 alkenyl,
- iii) C.sub.5-7 cycloalkyl, or
- iv) phenethyl or phenethyl, wherein the ring is substituted by one C.sub.1-4 alkoxy;
- with the proviso that:
- i) --A--W--R.sup.1 binds to the 3- or 4-carbon in the benzene ring, and
- ii) when W is phenylene or ##STR196## does not represent --O--, --CO--, --CH.sub.2 -- or --CH(OH)--;
- and non-toxic salts thereof.
36 more elements
Dependencies are inferred from the claim text.