1
New Patents 4939141 (FUSED) BENZ (THIO) AMIDES AND PHARMACEUTICAL COMPOSITIONS, THEREOF Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai, Osaka, Japan assigned to Ono Pharma- ceutical Co Ltd A (fused) benz(thio)amides of the general See Patent for Chemical Structure (I) (wherein, symbol A represents a single bond or a group of methylene, ethylene, trimethylene, tetramethy- lene, vinylene, propenylene, butenylene, butadienylene or ethynylene group optionally being substituted by one, two or three of straight or branched alkyl groups(s) of from 1 to 10 car: bon atom(s) and/or phenyl group(s); Symbol B represents (i) a heterocyclic ring of from 4 to 8 members containing one, two or three hetero atoms selected from oxygen, nitrogen and/or sul- phur atom(s), wherein the ring may optionally be substituted by group(s) of oxo, thioxo and/or hydroxy group(s) with the exclusion of a ring of the formula: See Patent for Chemical Structure Symbol T represents an oxygen atom or a sul- phur atom; R 1 represents a group of general for- mula: (i) See Patent for Chemical Structure (ii) See Patent for Chemical Structure or (iii) See Pa- tent for Chemical Structure or (iv) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s); (wherein R5 and R6 independently represent a hydrogen atom or a halogen atom or a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s) being unreplaced or replaced one, two, three, four or five of optional carbon atom(s) by oxygen atom(s), sulphur atom(s), halogen atom(s), nitrogen atom(s), benzene ring(s), thiopene ring(s), naphthalene ring(s), carbocy- clic ring(s) of from 4 to 7 carbon atom(s), car- bonyl group(s), carbonyloxy group(s), hydroxy group(s), carboxy group(s), azido group(s) and/or nitro group(s); R2 represents a hydrogen atom or a straight or branched alkyl group of from 1 to 6 carbon atom(s); R3 represents a hydrogen atom, a halogen atom, a hydroxy group, a nitro group, a group of general formula: -COOR7 (wherein R7 represents a hydrogen atom or a straight or branched alkyl group of from 1 to 6 carbon atom(s)) or a straight or branched alkyl, alkoxy or alkylthio group of from 1 to 6 carbon atom(s); R4 represents (i) when symbol B represents a closed ring, a group of general formula: See Patent for Chemical Structure (CH2)pCOOR8 or (CH2)qNNHNN (wherein symbol U represents an oxygen atom or a sulphur atom. R8 represents a hydrogen atom or a straight or branched alkyl group of from 1 6 carbon atom(s), n and m represent an integer from I to 10, respectively, p and q represent ze or an integer of from 1 to 10, respectively) non-toxic salts thereof posses an antagonistic tivity on leukotrienes (SRS), inhibitory activi of 5 alpha-reductase, on phospholipase and ( aldose reductase and are therefore useful for tl prevention and/or treatment for diseases i duced by leukotrienes, 5 alpha-reducta, phospholipase and aldose reductase in mai reals, especially human beings. 4940575 4-HYDROXYISOXAZOLE DERIVATIVES, METHOD OF PREPARING SAME, AND COSMETIC AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Alexandre Zysman, Henri Sebag, Paris, Fran assigned to Societe Anonyme dite:L'Oreal 4-Hydroxyisoxazole derivatives correspondi to the formula: See Patent for Chemical Strt ture (I) wherein: R represents a linear branched alkyl or hydroxyalkyl radical with 1 23 carbon atoms, a linear or branched alker radical with 2 to 23 carbon atoms, a pher radical, or a benzyl radical, and R1 represel OR2, -NHR3, or -NH-NHR4, R2 represent., hydrogen atom or an alkyl radical with 1 to carbon atoms, R3 represents a hydrogen ato~ an alkyl radical with 1 to 20 carbon atoms, ol See Patent for Chemical Structure radical, wh¢ n is 2 to 3 and r' and r" are identical or differel representing a hydrogen atom or a lower all radical or forming a heterocycle when tak together such as morpholine, pipcridine, piperazine, R4 represents a hydrogen atom ol benzyl radical, and the salts of the formula compounds. These derivatives are applicable therapeutic and cosmetic fields, in particular counteract the harmful effects of the sun. 4940587 ORAL PHARMACEUTICAL COMPOSITION THROUGH MUCOSA Anthony Jenkins, Stewart Leslie, Ronald Mill, Cambridge, United Kingdom assigned to Em celtique S A

4940587 Oral pharmaceutical composition through mucosa

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New Patents

4939141

(FUSED) BENZ (THIO) AMIDES AND PHARMACEUTICAL

COMPOSITIONS, THEREOF

Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai, Osaka, Japan assigned to Ono Pharma- ceutical Co Ltd

A (fused) benz(thio)amides of the general See Patent for Chemical Structure (I) (wherein, symbol A represents a single bond or a group of methylene, ethylene, trimethylene, tetramethy- lene, vinylene, propenylene, butenylene, butadienylene or ethynylene group optionally being substituted by one, two or three of straight or branched alkyl groups(s) of from 1 to 10 car: bon atom(s) and/or phenyl group(s); Symbol B represents (i) a heterocyclic ring of from 4 to 8 members containing one, two or three hetero atoms selected from oxygen, nitrogen and/or sul- phur atom(s), wherein the ring may optionally be substituted by group(s) of oxo, thioxo and/or hydroxy group(s) with the exclusion of a ring of the formula: See Patent for Chemical Structure Symbol T represents an oxygen atom or a sul- phur atom; R 1 represents a group of general for- mula: (i) See Patent for Chemical Structure (ii) See Patent for Chemical Structure or (iii) See Pa- tent for Chemical Structure or (iv) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s); (wherein R5 and R6 independently represent a hydrogen atom or a halogen atom or a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s) being unreplaced or replaced one, two, three, four or five of optional carbon atom(s) by oxygen atom(s), sulphur atom(s), halogen atom(s), nitrogen atom(s), benzene ring(s), thiopene ring(s), naphthalene ring(s), carbocy- clic ring(s) of from 4 to 7 carbon atom(s), car- bonyl group(s), carbonyloxy group(s), hydroxy group(s), carboxy group(s), azido group(s) and/or nitro group(s); R2 represents a hydrogen atom or a straight or branched alkyl group of from 1 to 6 carbon atom(s); R3 represents a hydrogen atom, a halogen atom, a hydroxy group, a nitro group, a group of general formula: -COOR7 (wherein R7 represents a hydrogen atom or a straight or branched alkyl group of from 1 to 6 carbon atom(s)) or a straight or branched alkyl, alkoxy or alkylthio group of from 1 to 6 carbon atom(s); R4 represents (i) when symbol B represents a closed ring, a group of general formula: See Patent for Chemical Structure (CH2)pCOOR8 or (CH2)qNNHNN (wherein symbol U represents an oxygen atom or a sulphur atom. R8 represents a hydrogen atom

or a straight or branched alkyl group of from 1 6 carbon atom(s), n and m represent an integer from I to 10, respectively, p and q represent ze or an integer of from 1 to 10, respectively) non-toxic salts thereof posses an antagonistic tivity on leukotrienes (SRS), inhibitory activi of 5 alpha-reductase, on phospholipase and ( aldose reductase and are therefore useful for tl prevention and/or treatment for diseases i duced by leukotrienes, 5 alpha-reducta, phospholipase and aldose reductase in mai reals, especially human beings.

4940575

4-HYDROXYISOXAZOLE DERIVATIVES, METHOD OF

PREPARING SAME, AND COSMETIC AND

PHARMACEUTICAL COMPOSITIONS CONTAINING

THEM

Alexandre Zysman, Henri Sebag, Paris, Fran assigned to Societe Anonyme dite:L'Oreal

4-Hydroxyisoxazole derivatives correspondi to the formula: See Patent for Chemical Strt ture (I) wherein: R represents a linear branched alkyl or hydroxyalkyl radical with 1 23 carbon atoms, a linear or branched alker radical with 2 to 23 carbon atoms, a pher radical, or a benzyl radical, and R1 represel OR2, -NHR3, or -NH-NHR4, R2 represent., hydrogen atom or an alkyl radical with 1 to carbon atoms, R3 represents a hydrogen ato~ an alkyl radical with 1 to 20 carbon atoms, ol See Patent for Chemical Structure radical, wh¢ n is 2 to 3 and r' and r" are identical or differel representing a hydrogen atom or a lower all radical or forming a heterocycle when tak together such as morpholine, pipcridine, piperazine, R4 represents a hydrogen atom ol benzyl radical, and the salts of the formula compounds. These derivatives are applicable therapeutic and cosmetic fields, in particular counteract the harmful effects of the sun.

4940587

ORAL PHARMACEUTICAL COMPOSITION THROUGH

MUCOSA

Anthony Jenkins, Stewart Leslie, Ronald Mill, Cambridge, United Kingdom assigned to Em celtique S A