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US 6,001,877 AGranted
Phenylalkan(en)oic acid
AssigneeOno Pharmaceutical Co., Ltd.
InventorsMitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
Life of this patent
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Abstract
The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.
Claims15
A phenylakan(en)oic acid of formula:
- ##STR191## wherein A is
- i) --NHCO--,
- ii) --NHSO.sub.2 --,
- iii) --CO--,
- iv) --CH.sub.2 --, or
- v) --CH(OH)--;
- W is
- i) C1-13 alkylene,
- ii) phenylene, or ##STR192## R.sup.1 is i) hydrogen,
- ii) C1-4 alkyl,
- iii) --COOH, ##STR193## or v) --CH.sub.2 OH;
- A, taken together with W and R.sup.1, is
- i) --N--(SO.sub.2 R.sup.6).sub.2, or ##STR194## two R.sup.2 are, same or different, i) hydrogen, or
- ii) C1-4 alkyl;
- Y is ethylene or vinylene;
- D is
- i) --Z--B, or ##STR195## Z is C3-11 alkylene or alkenylene;
- B is ##STR196## or Z, taken together with B, is C3-22 alkyl;
- R.sup.3 is
- i) hydrogen,
- ii) halogen,
- iii) C1-8 alkyl, alkoxy or alkylthio, or
- iv) C2-8 alkenyl, alkenyloxy or alkenylthio;
- n is 1-3;
- R.sup.4 is C1-7 alkylene;
- R.sup.5 is
- i) C1-12 alkyl,
- ii) C2-12 alkenyl,
- iii) C5-7 cycloalkyl, or
- iv) phenethyl or phenethyl wherein the ring is substituted by one C1-4 alkoxy;
- two R.sup.6 are the same or different,
- i) C1-7 alkyl,
- ii) benzyl, or
- iii) phenyl or phenyl wherein the ring is substituted by one C1-4 alkyl;
- and
- two R.sup.7 are the same or different, C1-4 alkyl;
- with the proviso that
- i) --A--W--R.sup.1 should bind to 3- or 4- carbon in benzene ring, and
- ii) when W is phenylene or ##STR197## A should not represent --CO--, --CH.sub.2 -- or --CH(OH)--;
- and non-toxic salts thereof.
37 more elements
Dependencies are inferred from the claim text.