4485104 1,2,4-triazole-3-amines and their pharmaceutical use

New Patents

4485104 1,2,4-TRIAZOLE-3-AMINES AND THEIR PHARMACEUTICAL USE John W Clitherow, Barry J Price, Roger Hayes, David E Bays, Hertfordshire, United Kingdom assigned to Glaxo Group Limited

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4485258 PHARMACEUTICALLY ACTIVE (3-AMINOPROPOXY)BIBENZYL DERIVATIVES

RiR2N__Alk__Q__X~(CH2)nY(Cit2)mNH_..~.~. N : B\\ /{CH2)p\ --Ctl Ctt~ I I O O

Ryoj Kikumoto, Harukazu Fukami, Hiroto Hara, Kunihiro Ninomiya, Mamoru Sugano, Machida, Japan assigned to Mitsubishi Chemical Industries Limited

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R6

methyl-l-piperazyl, optionally substituted by one or two methyl groups in the 2-, 4- or 6- positions as apt, or l-pyrrolidyl substituted by one or two methyl groups, m is 0 or 1; and n is 0 to 3 a process for their preparation and compositions containing them.

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R2

R7

Compounds of the general formula (I) See Patent for Chemical Structure (I) and physiologically acceptable salts, hydrates and bioprecursors thereof have been found to show pharmacological activity as selective histamine H2-antagonists. The substituents in the compounds of formula (I) are defined in the main body of the disclosure.

R,._~: l~ 4' y 6 '

CH2CH2-'~ r~"~5 2~ 4 OCH2CHCH2~R4 IO~R3

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-- C-- Y--COOH C4-C6cycloalkylene~CH

CH--

4485108 cyclohexenylene--CH~CH-- or --C ........ Cw;

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and R4 is ~N

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R5

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Ljerka Jozic, Hanover, Federal Republic Of Germany assigned to Beecham Wuelfing GmbH & Co KG R2N--(CIi2)n--CIt~(Cli2)mmNtlSO2~AR4[~ R !

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Ctl2 \ / C!!2 CH2 \ / CIt2 Ctl~Ctt CH2--Ct12

NAPHTHALENESULFONAMIDES, THEIR PHARMACEUTICAL COMPOSITIONS AND METHOD OF USE

(3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.

(1)

4486429 R2

Compounds of the formula (I) and salts thereof: See Patent for Chemical Structure (I) wherein: A is a bond, -CH2- or -CH double bondCH-; R2 is hydrogen and R1 is selected from C1-4 alkyl, hydroxyl, C1-4 alkoxy, C1-4 alkanoyloxy, hydrogen, halogen, nitro, cyano, and amino optionally substituted by one or two C1-4 alkyl groups or by C1-4 alkanoyl; R4 is C1-4 alkyl, hydroxy, C1-4 alkoxy, C1-4 alkanoyloxy or nitrato; R2N is 1-piperidyl, morpholino or 4-

AMINO DERIVATIVES OF 4-PHENYL 4-OXOBUTEN-2-OIC ACID, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND METHODS FOR PREPARING AND THERAPEUTICALLY USING THEM Mario Bianchi, Fernand Barzaghi, Milan, Italy assigned to Roussel Uclaf