Abstract: Fumaric acid monoesters can be prepared by introducing a hydroxyl compound at a rate corresponding to the progress of the reaction into a solution or a melt of maleic anhydride, which may optionally be substituted, if appropriate in the presence of a cis-trans catalyst. New fumaric acid monoesters can be formed by the process.
Abstract: This invention discloses a process for the preparation of (.+-.)-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives which comprises conducting an intramolecular cyclization reaction of the compounds of formulas II III in an acid medium.
Type:
Grant
Filed:
July 8, 1983
Date of Patent:
February 5, 1985
Assignee:
Korea Advanced Institute of Science and Technology
Inventors:
Choong S. Kim, Nam J. Lee, Joong H. Kim
Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
Type:
Grant
Filed:
February 12, 1982
Date of Patent:
October 16, 1984
Assignee:
Toyama Chemical Co., Ltd.
Inventors:
Takako Hori, Chosaku Yoshida, Yasuo Kiba, Ryuko Takeno, Joji Nakano, Jun Nitta, Sumiko Kishimoto, Shohachi Murakami, Hisatsugu Tsuda, Isamu Saikawa
Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
Type:
Grant
Filed:
July 16, 1980
Date of Patent:
March 13, 1984
Assignee:
Toyama Chemical Co., Ltd.
Inventors:
Takako Hori, Chosaku Yoshida, Yasuo Kiba, Ryuko Takeno, Joji Nakano, Jun Nitta, Sumiko Kishimoto, Shohachi Murakami, Hisatsugu Tsuda, Isamu Saikawa
Abstract: Compounds useful in making crosslinkable polymers having the formula (I): ##STR1## wherein R is hydrogen or methyl; R.sup.1 is cyano or ##STR2## wherein R.sup.2 is alkyl; Z is --X--R.sup.3 --X-- or ##STR3## wherein each --X-- is --O-- or --NR.sup.4 --, provided at least one --X-- is --NR.sup.4 -- wherein R.sup.4 is hydrogen or alkyl R.sup.3 is divalent hydrocarbon and D.sub.1 and D.sub.2 together are the carbon atoms necessary to complete a 5 to 7 membered ring. These compounds can be homopolymerized or copolymerized with each other or with other polymerizable ethylenically unsaturated monomers to give crosslinkable polymers. Such polymers can be purified by conventional purification techniques such as dialysis, diafiltration, ultrafiltration without losing their capability of crosslinking. The resulting purified polymers are particularly useful in photographic materials as gelatin extenders, binders or polymeric color couplers.
Type:
Grant
Filed:
April 19, 1982
Date of Patent:
December 20, 1983
Assignee:
Eastman Kodak Company
Inventors:
Ignazio S. Ponticello, Kenneth R. Hollister, Richard C. Tuites
Abstract: Novel 1-aryloxy-3-amidoamidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. Representative of the compounds disclosed is 1-(o-cyanophenoxy)-3-.beta.-(2-thenamidoacetamido)ethylaminopropan-2-ol.
Abstract: Immunoregulatory 2,5-diketopiperazine compounds of formula: ##STR1## wherein m is 1 or 2 and n is 3 or 4 possess the ability to regulate the immune system of humans and animals. Administration of the compounds will return to a normal state an immune system in need of regulation.
Type:
Grant
Filed:
June 23, 1980
Date of Patent:
September 15, 1981
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
George Heavner, Foe-Siong Tjoeng, Gideon Goldstein
Abstract: Novel quinoxaline-di-N-oxide derivatives of the general formula ##STR1## in which R.sub.1 is hydrogen or straight-chain or branched-chain alkyl having 1 to 4 carbon atoms,R.sub.2 and R.sub.3 independently of one another are each straight-chain or branched-chain alkyl having 1 to 4 carbon atoms, or together with the N atom they form a heterocyclic ring which is unsubstituted or is substituted by alkyl having 1 to 4 carbon atoms, and which has 4 to 5 ring carbon atoms and optionally an oxygen atom as further hetero atom,R.sub.4 is hydrogen, methoxy, methylthio, hydroxyl, fluorine, chlorine, bromine or cyano,A is alkylene having 1 to 4 carbon atoms, with the proviso that if R.sub.4 has a meaning other than cyano, A is 1,2-ethylene, and R.sub.1 is hydrogen,including the acid addition salts thereof; processes for producing them; compositions containing these compounds; and the use thereof. The novel active substances serve to combat pathogenic microorganisms in the field of veterinary medicine.
Abstract: This disclosure describes 4-[(unsaturated or cyclopropylated alkyl)amino]benzoic acids and derivatives useful as hypolipidemic and antiatherosclerotic agents.
Abstract: Substituted piperazine diones are stabilizers for synthetic polymeric materials normally subject to deterioration caused by ultraviolet light. The compounds are prepared by the alkylation reaction between a substituted piperazine dione and an organic halide. Polymeric compositions containing these stabilizers may also contain a hindered phenolic compound. A typical embodiment is 15,15'-dodecamethylenebis(7,15-diazadispiro[5,1,5,3]hexadecane-14,16-dione ).
Abstract: New dioxo-piperazine derivatives suitable for use as medicaments and .beta.-lactam antibiotic intermediates of the formula ##STR1## in which Z is ##STR2## and, R.sup.1 and R.sup.2 each independently is hydrogen or various optionally substituted aliphatic, aromatic or heterocyclic radicals or together form an optionally substituted ring,are formed by reacting(a) 1-amino-2,3-dioxo-piperazine of the formula ##STR3## with a compound of the formula ##STR4## or a hydrate, acetal, ketal, sulphite, hydrogen halide or hydrocyanic acid addition product thereof or, ##STR5## with an oxalic acid ester in the presence of a diluent, thereby to effect cyclization. The new derivatives are anti-virally active and can also be chlorocarbonated with phosgene to form a reactive derivative which can be condensed with the amino group of .alpha.-amino penicillins to form antibiotics.
Abstract: 1,4-Di-(2,6-dimethylphenyl)-2,5-piperazinedione has been found to be highly effective for the control of late blight, downy mildew and Phytophthora crown and root rot fungal diseases.
Abstract: N-substituted cyclic imides of diacids such as oxydiacetic acid and N-substituted iminodiacetic acid are produced by contacting a hydroxy amide of the formulaHOCH.sub.2 CH.sub.2 --A--CH.sub.2 --CONHRwith a reduced copper dehydrogenation catalyst at a temperature of about 200.degree.-30 .degree. C, A representing --O-- or ##STR1## and R and R' being hydrocarbon groups of 1-8 carbon atoms. The reaction is preferably conducted in the presence of hydrogen and the diol corresponding to the hydroxyamide. The process is essentially a means of making oxydiacetic acid or iminodiacetic acid from diethylene glycol or diethanolamine respectively as the original starting material. These dicarboxylic acids are useful chelating agents, particularly for Ca and Mg ions, they are intermediates in chemical syntheses, and they are difunctional monomers for making polyester plastics.
Abstract: Substituted piperazine diones are stabilizers for synthetic polymeric materials normally subject to deterioration caused by ultraviolet light. The compounds are prepared by the alkylation reaction between a substituted piperazine dione and an organic halide. Polymeric compositions containing these stabilizers may also contain a hindered phenolic compound. A typical embodiment is 15,15'-dodecamethylene-bis(7,15-diazadispiro[5,1,5,3]hexadecane-14,16-dion e).
Abstract: Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.
Abstract: Disclosed are broad spectrum antibiotics derived from 7-[D(-)-.alpha.-(4-alkyl-2,3-dioxopiperazin-1-yl-carbonylamino)-substitute dphenylacetamido]-3-(5-substituted or unsubstituted-1,3,4-thiadiazol-2-yl-thiomethyl)-3-cephem-4-carboxylic acids and salts thereof.
Abstract: A cheese flavor is improved or enhanced by the addition to food-products of a diketo-piperazine, defined as cyclo-(Asn--Phe); the typical "mouth-feel" character is thus developed.A new process for the preparation of the said ingredient is also disclosed.
Type:
Grant
Filed:
April 5, 1977
Date of Patent:
May 9, 1978
Assignee:
Firmenich S.A.
Inventors:
Alistair Y. Smith, Paul Dietrich, Wilhelm Pickenhagen