Abstract: A process for producing a lactone-substituted aniline wherein a 3-halo-tetrahydro-2-oxofuran is reacted with an aniline in the presence of water and a base at a temperature between 80.degree. and 160.degree. C. and wherein the base is added at a sufficiently slow rate so that the pH does not exceed about 7.5.
Abstract: D-Homopregnanes of the formula ##STR1## wherein X is hydrogen, Y is hydroxy or X and Y taken together denote an oxygen to carbon bond; R.sup.6 is hydrogen, R.sup.7 is hydrogen, lower alkanoylthio or aroylthio, or R.sup.6 and R.sup.7 taken together denote a carbon to carbon bond and the dotted line in the 1,2-position of the A-ring together with the corresponding solid line denotes a single or double carbon to carbon bondor a pharmaceutically acceptable basic addition salt thereof when Y is hydroxy having diuretic activity are disclosed.
Type:
Grant
Filed:
June 30, 1978
Date of Patent:
May 13, 1980
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Andor Furst, Peter Keller, Marcel Muller
Abstract: Derivatives of 2-hydroxy-5-[1-hydroxy-2-[4-(2-oxo-1-benzimidazolinyl)piperidino]ethyl]ben zoic acid are prepared which are useful for their blocking action on .alpha. and .beta.-adrenergic receptors. In addition, these compounds are useful for their spasmolytic and anti-hypertensive activity.
Abstract: Compounds having the structures: ##STR1## wherein R is CH.sub.3 or CF.sub.3 and wherein R.sup.1 is H or CH.sub.3. compounds are prepared by a four step method involving (1) the formation of a benzylaminophenol or benzylaminohydroxypyridine, (2) the formation of a coumarin or azacoumarin, (3) sulfonation of the coumarin or azacoumarin and (4) neutralization of the sulfonate with sodium bicarbonate. The compounds are useful as water-soluble lasing dyes.
Type:
Grant
Filed:
November 17, 1978
Date of Patent:
April 29, 1980
Assignee:
The United States of America as represented by the Secretary of the Navy
Abstract: The present invention relates to a process for the preparation of certain known imidazo[2,1-a]isoindoles of the general formula I: ##STR1## wherein X represents a hydrogen atom, a halogen atom or a lower alkoxy group. The said isoindoles, which may be prepared from novel lactams, have been shown to have utility as psychic energizers and anorectics.
Abstract: Antiinflammatory 4,5-diaryl-2-nitroimidazoles, such as 4,5-bis(4-fluorophenyl)-2-nitroimidazole, useful for treating arthritis and related diseases.
Abstract: A process for the preparation of carboxylic acids represented by a formula ##STR1## wherein R.sub.1 represents hydrogen atom or a lower alkyl radical, R.sub.2 represents hydrogen atom, lower alkyl or allyl radical and R.sub.3 represents phenyl, substituted phenyl, substituted naphthyl, dibenzofuranyl or substituted biphenyl. Following novel enamine and amidine compounds as intermediates for manufacturing the carboxylic acids and processes for the manufacture of said enamine and amidine compounds ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 represent the meanings as referred to and R.sub.4 represents dimethylamino, pyrrolidyl, piperidyl or morpholyl.
Abstract: A process for the production of 3-substituted pyrazolanthrones of the formula ##STR1## wherein X is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or a group --COR, in which R is hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxyl, C.sub.1 -C.sub.6 alkoxy, --NH.sub.2, --NH--C.sub.1 -C.sub.6 alkyl or --NR.sub.1 R.sub.2, in which R.sub.1 and R.sub.2, each independently of the other, are C.sub.1 -C.sub.6 alkyl, which comprises reacting 1-nitroanthraquinones of the formula ##STR2## wherein X is as defined in formula (1), in aprotic dipolar solvents, with hydrazine or hydrazine hydrate, at normal or slightly elevated temperature, to give 3-substituted pyrazolanthrones of the formula (1).
Abstract: Compounds having the formula ##STR1## wherein X is oxygen or sulfur, R is selected from the group consisting of alkyl and alkoxy, R.sub.1 is alkoxy, R.sub.2 is selected from the group consisting of hydrogen and methyl and R.sub.3 is selected from the group consisting of hydrogen, methyl and phenyl; these compounds are active as insecticides.
Abstract: The invention of this application is directed to dipotassium phthalocyanine glyme and crown ether complexes, such as for example dipotassium phthalocyanine bis (methoxy ethyl) ether and dipotassium phthalocyanine bis (18-crown-6) ether. Methods for obtaining these complexes by reacting metal free phthalocyanine with potassium hydroxide and the appropriate glyme or crown ethers in the presence of water is also described. Further methods for obtaining purified metal free phthalocyanines from the glyme and crown ether complexes are disclosed. These materials have many uses including pigments, electrophotographic photoreceptors and photoreceptor devices.
Abstract: The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H.sub.2 -antagonists.
Type:
Grant
Filed:
March 31, 1978
Date of Patent:
March 11, 1980
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young
Abstract: Metal salts and amides of alkyl-lactam acetic acids are prepared by reacting gamma-hydrocarbyl butyrolactone acetic acid compounds derived from alkenylsuccinic anhydrides with metal compounds and amines or amines alone. High molecular weight lactam acid salts and amides and metal complexes and metal carbamates thereof are useful as detergents or dispersants in organic industrial fluids. Another aspect of this invention is a method of preparing lactone acetic acids in yields up to 90% conversion from alkenylsuccinic anhydrides.
Abstract: Disclosed are N-derivatives of thienamycin having structures I and II. ##STR1## wherein: the bifunctional radical may contain additional unsaturation in the ring; and wherein n is an integer selected from 1-6; p is 0, 1 or 2; R.sup.1 is selected from hydrogen, alkyl having 1-6 carbon atoms, and aryl having 6-10 carbon atoms; and Z is imino (.dbd.NH), oxo (.dbd.O), hydrogen, amino, or alkyl having 1-6 carbon atoms. Such compounds and their pharmaceutically acceptable salt and ester derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Type:
Grant
Filed:
December 28, 1977
Date of Patent:
February 19, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, John Hannah, David H. Shih
Abstract: A process for making substituted imidazoline substantially completely free from diamide and preferably from byproduct ester. The process involves contacting an aminoethyl lower alkanol amine with a methyl carboxylate at elevated temperature and thereafter subjecting the reaction product to two successive heat treatments under specified conditions. A feature of the process is that it contains an optional step which can be employed to correct the formation of unwanted amounts of ester in the product. The product imidazoline is useful as a starting material for making amphoteric surfactants.
Type:
Grant
Filed:
May 1, 1978
Date of Patent:
February 19, 1980
Inventors:
Joseph R. Wechsler, Thomas G. Baker, George T. Battaglini, Frank L. Skradski
Abstract: Prostaglandin type compounds of the formula ##STR1## where X is CH.sub.2 --CH.sub.2, CH.dbd.CH or C.tbd.C; Y is CH.sub.2 or O; Z is OH, CH.sub.3 or CH.sub.2 OH, R" is H or loweralkyl and R is a linear, branched or cyclic alkyl group of 3 to 7 carbon atoms, can be prepared by essentially a one-step reaction from a new intermediate of the formula ##STR2## wherein R' is hydrogen, R and Z are the same as shown above, and P is a removable protective group. The new compounds are useful as antihypertensives, gastric acid secretion inhibitors and smooth muscle stimulants.
Type:
Grant
Filed:
April 26, 1978
Date of Patent:
February 12, 1980
Assignee:
Abbott Laboratories
Inventors:
Andre G. Pernet, Hiromasa Nakamoto, Naoyasu Ishizuka
Abstract: Pyrazoline compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 denote hydrogen or chlorine,R.sub.3 denotes C.sub.1 -C.sub.4 -alkyl andX.sup..crclbar. denotes a colorless anion,are suitable for the whitening of polyacrylonitrile and wool.
Type:
Grant
Filed:
January 10, 1978
Date of Patent:
January 15, 1980
Assignee:
Bayer Aktiengesellschaft
Inventors:
Josef Schroeder, Carl-Wolfgang Schellhammer