摘要:
A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2, therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.
摘要:
New compounds having the formula ##STR1## in which m is 1 or 2; when m is 1, A is a residue selected from those of the formulae ##STR2## and, when m is 2, A is a residue of the formula ##STR3## B is --O--, --NH-- or --SO.sub.2 --, and D is as defined herein, are useful as ultraviolet absorbing agents (UVAs) and a method of improving the sun protection factor of textile fibre material by treating the material with the new compounds.
摘要:
Compounds of formula ##STR1## wherein R, R', R", R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X, Y, m, n and p have the meanings reported in the description; and their pharmaceutically acceptable salts are described. The compounds of formula I are useful in the treatment of arterial hypertension and congestive heart failure, of renal failure, of peripheral arteriopathies, of cerebrovascular insufficiencies and of ischemic cardiopathy.
摘要:
Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by the formula ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R.sup.1 or R.sup.2 is hydrogen while the other is alkyl or R.sup.1 and R.sup.2 are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.
摘要:
Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and synthesis are disclosed. Also, pharmaceutical formulations are disclosed for use in applications treating diseases or conditions characterized by excessive release of leukotriene B.sub.4, one of the metabolites of arachidonic acid.The primary LTB.sub.4 antagonistic structures are represented as: ##STR1##
摘要:
The phenylalkan(en)oic acids of the formula: ##STR1## wherein A isi) --NHCO--,ii) --O--iii) --NHSO.sub.2 --,iv) --CO--v) --CH.sub.2 -- orvi) --CH(OH)--;W isi) C1-13 alkylene,ii) phenylene oriii) ##STR2## R.sup.1 is i) hydrogen,ii) C1-4 alkyl,iii) --COOH,iv) saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom or saturated or unsaturated, 4-7 member mono-cyclic hetero ring containing one nitrogen as a hetero atom substituted by an oxo group,v) ##STR3## vi) --CH.sub.2 OH; or A, taken together with W and R.sup.1, isi) ##STR4## ii) ##STR5## iii) --N--(SO.sub.2 R.sup.6).sub.2, iv) ##STR6## or v) ##STR7## two R.sup.2 are, same or different, i) hydrogen,ii) C1-4 alkyl oriii) 4-7 membered saturated or unsaturated, mono-cyclic hetero ring containing two or three of nitrogen and sulfur in total, or two R.sup.2, taken together with a nitrogen to which they are attached, form saturated or unsaturated,i) 7-14 membered, bi- or tri-cyclic hetero ring containing one nitrogen as a hetero atom, orii) 4-7 mebered, mono-cyclic hetero ring containing two or three of nitrogen and oxygen in total;Y is ethylene or vinylene;D isi) --Z--B orii) ##STR8## Z is C3-11 alkylene or alkenylene R is ##STR9## or Z taken together with B, is C3-22 alkyl;R.sup.3 isi) hydrogen,ii) halogen,iii) C1-8 alkyl, alkoxy or alkylthio, oriv) C2-8 alkenyl, alkenyloxy or alkenylthio;n is 1-3;R.sup.4 is C1-7 alkylene;R.sup.5 isi) C1-12 alkyl,ii) C2-12 alkenyl,iii) C5-7 cycloalkyl or pp2 iv) phenethyl or phenethyl wherein the ring is substituted by one C1-4 alkoxy;Two R.sup.6 are, same or different,i) C1-7 alkyl,ii) benzyl oriii) phenyl or phenyl wherein the ring is substituted by one C1-4 alkyl; andTwo R.sup.7 are, same or different, C1-4 alky; with the proviso thati) --A--W--R.sup.1 should bind to 3- or 4- carbon in benzene ring, andii) when W phenylene or ##STR10## A should not represent --O--, --CO--, --CH.sub.2 -- or --CH(OH)--; and non-toxic salts thereof,possess an antagonistic activity on leukotriene B.sub.4, and therefore, are useful for the prevention and treatment of several diseases induced by leukotriene B.sub.4.
摘要:
The invention relates to an anti-inflammatory or antiallergic composition containing a compound of the formula ##STR1## wherein A is ##STR2## R.sup.1 is aryl which may have cyano or carbamoyl, or heterocyclic group which may have lower alkyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is lower alkyl,X is hydrogen, halogen, hydroxy or lower alkyl,m is an integer 1 or 2, andn is an integer 1 to 4, or pharmaceutically acceptable salts thereof.
摘要:
The present invention relates to new compounds of the formula I ##STR1## as well as their preparation, pharmaceutical preparations containing same, and method of treating acute myocardial infarction.The compounds which possess beta-adrenoceptor blocking activity are very shortacting and are preferably intended for treatment of acute myocardial infarction by administration by means of injection.
摘要:
This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.