Abstract: Novel substituted nitroimidazoles are provided, for example, 2-(4,5-substituted-isoxazol-3-yl)-1-substituted-5-nitroimidazole; 2-(4,5-disubstituted-.DELTA..sup.2 -isoxazolin-3-yl)-1-substituted-5-nitroimidazole; or 2-(4,5-disubstituted-2-loweralkyl-isoxazolidin-3-yl)-1-substituted-5-nitro imidazole. These compounds have antibacterial and antiprotozoal activity, especially against human and animal trypanosomiasis and trichomoniasis.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, alkyl of 1 to 4 carbon atoms, phenyl, hydroxyl, alkoxy of 1 to 3 carbon atoms, alkylmercapto of 1 to 3 carbon atoms, hydroxycarbonyl or ##STR2## where R.sub.3 and R.sub.4 are each alkyl of 1 to 4 carbon atoms or, together with each other and the nitrogen atom to which they are attached, morpholino, piperidino, methylpiperidino or phenyl-piperidino; orR.sub.1 and R.sub.2, together with each other and adjacent carbon atoms of the benzene ring to which they are attached, --CH=CH--CH=CH--, --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or --O--CH.sub.2 --O--;and salts thereof. The compounds are useful as antiallergics.
Type:
Grant
Filed:
September 23, 1975
Date of Patent:
March 1, 1977
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Friedrich Karl Hess, Patrick Brian Stewart
Abstract: Racemates and optically active isomers of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, lower alkyl optionally substituted with a member of the group consisting of hydroxy and halogen, lower alkenyl, lower alkynyl, --(CH.sub.2).sub.n -- COCH.sub.3 where n is 0 or 1, ##STR2## wherein X is selected from the group consisting of lower alkyl and optionally substituted phenyl, aralkyl or 7 to 8 carbon atoms, acyl of an organic carboxylic acid of 1 to 6 carbon atoms optionally substituted with ##STR3## where m is an integer from 0 to 6 and X.sub.1 is selected from the group consisting of hydrogen and lower alkyl, ##STR4## where p is an integer from 1 to 6 and X.sub.1 is as before and ##STR5## wherein X.sub.2 is lower alkyl and R.sub.1 and R.sub.
Abstract: The invention relates to novel 5,6,7,8-tetrahydroquinoline derivatives which have a group X situated at the 8-position said group X is CONHR.sup.3, or CO.sub.2 R.sup.5 wherein R.sup.3 is hydrogen lower alkyl and R.sup.5 is hydrogen, lower alkyl or a lower aralkyl radical.The compounds are intermediates for corresponding compounds where X is CSNHR.sup.3 and these are anti-ulcer agents.
Type:
Grant
Filed:
October 20, 1975
Date of Patent:
February 22, 1977
Assignee:
John Wyeth & Brother Limited
Inventors:
Adrian Charles Ward Curran, Roger Crossley, David George Hill
Abstract: Novel antibacterial agents consisting of a 2,3,5,8-tetrahydro-5-alkoxy-8-oxofuro(2,3-g)quinoline-7-carboxylic acid of the formula: ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl, a process for producing the derivatives and pharmaceutical compositions containing the same. The above-identified derivatives possess antibacterial activity against gram-negative bacteria at test concentration levels of about 0.0001 to 1.0 mg/cc.
Abstract: 7-Substituted imidazo[2,1-b]thiazolium and 9-substituted thiazolo-[3,2-a]benzimidazolium salts as blood-sugar lowering agents and growth promotants.
Type:
Grant
Filed:
July 8, 1975
Date of Patent:
February 15, 1977
Assignee:
Pfizer Inc.
Inventors:
Richard M. Acheson, John K. Stubbs, Charles A. R. Baxter, Donald E. Kuhla
Abstract: Oxazolidine and thiazolidine carbodithioates of sodium, potassium and specified alkyl substituted ammonium which are useful as vulcanization accelerators for EPDM elastomers while demonstrating non-blooming characteristics.
Type:
Grant
Filed:
August 15, 1975
Date of Patent:
February 15, 1977
Assignee:
Pennwalt Corporation
Inventors:
Ivan Christoff Popoff, Paul Gordon Haines
Abstract: Disclosed are disperse dyes of formula I, ##STR1## in which X signifies O or NH, either R.sub.1 and R.sub.2 each signify an alkyl or phenyl radical,Or R.sub.1 is as defined above, and R.sub.2 is hydrogen,Or R.sub.1 and R.sub.2, together with the nitrogen atom, signify a heterocyclic ringR.sub.3 signifies acyl, alkyl, phenyl or a heterocyclic, andR.sub.4 signifies a chain forming a carbocyclic or heterocyclic ring of aromatic character.
Abstract: N-(7- or 8-substituted-quinolyl-4)-anthranilates of the formula ##STR1## wherein X in the 7 or 8 position is trihalomethylthio, Z is --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --O--(CH.sub.2).sub.p --, n is a whole number from 2 to 6, m and p are whole numbers from 2 to 3 and Y.sub.1 and Y.sub.2 are alkyl having 1 to 6 carbon atoms, as well as their non-toxic, pharmaceutically acceptable acid addition salts having analgesic and anti-inflammatory activity and their preparation.
Abstract: Cephalosporins with a .alpha.-amino-(ureidophenyl)acetamido substituent at position 7 are prepared by acylation of a 7-aminocephalosporin with a derivative of .alpha.-amino-p(or m)-ureidophenylacetic acid. These compounds are antibacterial agents.
Type:
Grant
Filed:
May 7, 1973
Date of Patent:
February 8, 1977
Assignee:
SmithKline Corporation
Inventors:
John Russel Eugene Hoover, Jerry Arnold Weisbach
Abstract: A method for O-acylating the 3-hydroxymethyl group of 7-acylaminocephalosporadesic acids by reaction with an azolide and new O-acyl-7-acylaminocephalosporadesic acids in which the O-acyl group is derived from an alkoxyalkanoic acid or an amino acid.
Abstract: Novel antibacterial agents; namely, 7-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives having the formula: ##STR1## wherein R.sup.1 is thienyl, 2-furyl, phenyl, substituted thienyl or substituted phenyl; R is hydroxyl; R.sup.2 is hydrogen, hydroxy, acetoxy, carbamoyloxy, N-pyridyl, azido or heterocyclic thio group; R and R.sup.2 when taken together represent an oxygen atom; R.sup.3 is sulpho or COOR.sup.4.sup.' wherein R.sup.4.sup.' is hydrogen or R.sup.4 wherein R.sup.4 is lower alkyl, 5-indanyl, naphthyl, phenyl, or substituted phenyl, CONR.sup.5 R.sup.6, wherein each of R.sup.5 and R.sup.6 is hydrogen, lower alkyl or cycloalkyl; or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a saturated heterocyclic group; X is oxygen or sulphur, a direct link, carbonyl, methylene, hydroxymethylene, sulphinyl, sulphonyl or an imino group of the formula --NR.sup.7 --, wherein R.sup.7 is hydrogen, lower alkyl, lower alkenyl, or benzyl; and each of alk.sup.1 and alk.
Abstract: A class of pyrylium dyes, having at least one rigidized, nitrogen-containing heterocyclic ring fused thereto is described. The rigidized dyes are useful lasing components in lasing media.
Abstract: Process for the preparation of 7-substituted amino-desacetoxycephalosporanic derivatives comprising converting a 6-substituted amino-penicillanic acid sulfoxide into an anhydride of a 6-substituted amino-penicillanic acid sulfoxide, heating the said acid anhydride intermediate at a temperature up to at most 160.degree. C in a dry inert organic solvent with an anhydrous acid which is capable of causing ring expansion of the penam ring to a .DELTA..sup.3 -cephem ring, in the presence of a silicon-containing compound capable of (a) removing water formed during the ring enlargement of the penam structure fast enough to prevent water hydrolysis of the acid anhydride moiety present and (b) forming neutral or basic products on hydrolysis, the aforesaid acid being strong enough not to be, or not to a substantial extent to be, silylated under the reaction conditions employed, and hydrolyzing the resulting compound in situ to form the .DELTA..sup.
Type:
Grant
Filed:
May 5, 1975
Date of Patent:
January 18, 1977
Assignee:
Gist-Brocades N.V.
Inventors:
Jan Verweij, Hong Sheng Tan, Hermanus Jacobus Kooreman
Abstract: Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano[3,4-b]indole or thiopyrano[3,4-b]indole nucleus or having said radical attached to the 1 position of a pyrano[4,3-b]indole or thiopyrano[4,3-b]indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3,4,5,6,7,8, and 9.
Type:
Grant
Filed:
March 5, 1975
Date of Patent:
January 18, 1977
Assignee:
Ayerst McKenna and Harrison Ltd.
Inventors:
Christopher A. Demerson, Lesie G. Humber, Andre A. Asselin, Ivo Jirkovsky, Thomas A. Dobson
Abstract: A lactone compound represented by the following formula ##STR1## or ##STR2## or a mixture thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined hereinafter and a process for preparing the same are disclosed.