Patents Examined by Mary Vaughn
  • Patent number: 4111953
    Abstract: A process is disclosed for preparing 5-sulfamoylbenzoic acids substituted in 4-position by various substituents and in 3-position by a cyclic amino group having sali-diuretic properties. Novel intermediate compounds are also disclosed.
    Type: Grant
    Filed: December 6, 1976
    Date of Patent: September 5, 1978
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Dieter Bormann, Wulf Merkel, Dieter Mania
  • Patent number: 4111951
    Abstract: L-3,4-dehydroproline is produced in good yield from D,L-3,4-dehydroproline by resolution via the tartaric acid salt and thermal racemization of the D-3,4-dehydroproline tartaric acid salt containing mother liquors.
    Type: Grant
    Filed: January 17, 1977
    Date of Patent: September 5, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Urs Oskar Hengartner
  • Patent number: 4110533
    Abstract: The invention concerns a process for the manufacture of 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds by ring closure of esters of 2-[4-(substituted-thio)-3-acylamino-2-oxoazetidin-1-yl]-3-substituted-amin o-crotonic acids and solvolysing the enamino group in the resulting 7.beta.-acylamino-3-substituted-amino-cephem-4-carboxylic acid esters.
    Type: Grant
    Filed: February 10, 1976
    Date of Patent: August 29, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert B. Woodward, Hans Bickel
  • Patent number: 4107174
    Abstract: The imidyl compounds, according to the invention, of the formula I are suitable for the manufacture of polymers which can be crosslinked by light, which polymers can be, for example, polyesters, polyamides, polyamide-imides, polyimides, polyester-polyamides, polyester-amide-imides, polyethers, polyamines, polysaccharides and polysiloxanes. Polymers of this type are suitable for carrying out photochemical processes. Compared with known polymers, the polymers based on the imidyl compounds according to the invention have the advantage that they are photochemically substantially more sensitive. In addition, this sensitivity can also be further increased effectively by a combination with sensitizers.
    Type: Grant
    Filed: June 15, 1976
    Date of Patent: August 15, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Marcus Baumann, Vratislav Kvita, Martin Roth, John Sidney Waterhouse
  • Patent number: 4107165
    Abstract: Novel alkylenetris- and alkylenetetrakis-[1,2,3,4-tetrahydroisoquinoline] and -[3,4-dihydroisoquinoline] compounds, the pharmaceutically acceptable acid addition salts thereof and compositions containing such substances have been found useful for inhibiting the formation of blood clots in mammals and/or dissolving blood clots in mammals after they have been formed.
    Type: Grant
    Filed: September 15, 1976
    Date of Patent: August 15, 1978
    Assignee: Endo Laboratories
    Inventors: Parthasarathi Rajagopalan, Irwin J. Pachter
  • Patent number: 4105776
    Abstract: New proline derivatives and related compounds which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
    Type: Grant
    Filed: December 22, 1976
    Date of Patent: August 8, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Miguel Angel Ondetti, David W. Cushman
  • Patent number: 4103019
    Abstract: Glycyrrhetinic acid esters of the formula: ##STR1## wherein R is hydrogen or an acyl radical of 2 to 20 carbon atoms and R.sub.1 is a lower alkyl of 1 to 4 carbon atoms and the haloacid or alkylsulfate quaternary ammonium salts thereof as well as a process for preparing same are provided. The compounds of the invention display anti-inflammatory, antihistaminic, and anti-ulcer pharmacological activity.
    Type: Grant
    Filed: October 7, 1975
    Date of Patent: July 25, 1978
    Assignee: Laboratorios Landerlan, S. A.
    Inventor: Jose E. Acosta Mira
  • Patent number: 4101553
    Abstract: Imidazo[2,1-a]isoquinolines useful as anorexics and antidepressants are prepared from a dilithium derivative of a 2-(o-tolyl)-2-imidazoline.
    Type: Grant
    Filed: November 4, 1974
    Date of Patent: July 18, 1978
    Assignee: Sandoz, Inc.
    Inventor: William J. Houlihan
  • Patent number: 4100165
    Abstract: Imidazo[2,1-a]isoquinolines useful as anorexics and anti-depressants, e.g. 5-(2-thienyl)-2,3,5,6-tetrahydroimidazo[2,1-a]isoquinolin-5-ol, are prepared from a dilithium derivative of a 2-(o-tolyl)-2-imidazoline.
    Type: Grant
    Filed: July 22, 1976
    Date of Patent: July 11, 1978
    Assignee: Sandoz, Inc.
    Inventor: William J. Houlihan
  • Patent number: 4100166
    Abstract: Cis-1-cyclopropylmethyl-3a-(substituted-phenyl) decahydroisoquinoline, useful as analgetic agonist and analgetic antagonist.
    Type: Grant
    Filed: October 22, 1976
    Date of Patent: July 11, 1978
    Assignee: Eli Lilly and Company
    Inventors: Dennis M. Zimmerman, Winston S. Marshall
  • Patent number: 4098790
    Abstract: Ergolines are chlorinated with SO.sub.2 Cl.sub.2 /BF.sub.3 .multidot.etherate, preferentially in the 2 position.
    Type: Grant
    Filed: September 15, 1976
    Date of Patent: July 4, 1978
    Assignee: Eli Lilly and Company
    Inventor: Nicholas J. Bach
  • Patent number: 4097480
    Abstract: Compounds of the formula (I): ##STR1## and salts thereof wherein X is a group: ##STR2## R is hydrogen, methyl or ethyl; R.sub.1 is phenyl or naphthyl or phenyl substituted by fluorine, chlorine, bromine, methyl, methoxy or trifluoromethyl; R.sub.2 is hydrogen or methyl; R.sub.3 is hydrogen, methyl, ethyl or benzyl; R.sub.4 is hydrogen or methyl; and R.sub.5 is hydrogen or methyl; have been found to be mood modifying agents and anorexic agents.
    Type: Grant
    Filed: June 1, 1976
    Date of Patent: June 27, 1978
    Assignee: Beecham Group Limited
    Inventor: Derek Victor Gardner
  • Patent number: 4097579
    Abstract: Novel 5-(2-pyrroyl) and 5-(N-lower alkyl-2-pyrroyl)-1,2-dihydro-3H-pyrrolo?1,2-a!pyrrole-1-carboxylic acid compounds represented by the formula: ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein each of R and R.sup.1 is independently hydrogen or a lower alkyl group having from 1 to 4 carbon atoms and process for the production of such compounds; 5-(N-methyl-2-pyrroyl)-1,2-dihydro-3H-pyrrolo?1,2-a!pyrrole-1-carboxylic acid is representative of the class. These compounds are useful as anti-inflammatory analgesic and anti-pyretic agents and as smooth muscle relaxants.
    Type: Grant
    Filed: March 31, 1977
    Date of Patent: June 27, 1978
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph Martin Muchowski, Arthur Frederick Kluge
  • Patent number: 4097490
    Abstract: Process for resolving enantiomers of 1-t-butylamino-2,3-dihydroxypropane using a pyroglutamic acid or a tartaric acid as resolving agent. The enantiomers of 1-t-butylamino-2,3-dihydroxypropane are useful in preparing .beta.-adrenergic blocking agents.
    Type: Grant
    Filed: February 9, 1977
    Date of Patent: June 27, 1978
    Assignee: Merck & Co., Inc.
    Inventor: Donald F. Reinhold
  • Patent number: 4097489
    Abstract: This invention relates to certain structural and pharmacological analogs of prostacyclin (PGI.sub.2) wherein a nitrogen atom is substituted for the 6,9.alpha.-epoxy-oxygen of prostacyclin. These novel nitrogen-containing prostacyclin-type compounds are useful for the pharmacological purposes for which prostacyclin is used, e.g., as antithrombotic agents, smooth muscle stimulators, gastric antisecretory agents, antihypertensive agents, antiasthma agents, nasal decongestants, or regulators of fertility and procreation.
    Type: Grant
    Filed: June 17, 1977
    Date of Patent: June 27, 1978
    Assignee: The Upjohn Company
    Inventor: Gordon L. Bundy
  • Patent number: 4096146
    Abstract: Quinine, quinidine, their antipodes or racemates and derivatives thereof, are prepared by (a) cyclizing the correspondingly substituted 4-[3-(1-chloro-3(R)-alkyl(or alkenyl)-4-(R)-piperidyl)-1-oxopropyl]quinolines, antipodes or racemates thereof, to the corresponding 4-[5(R)-alkyl(or alkenyl)-4-(S)-quinuclidin-2(S) or 2(R)-ylcarbonyl]quinolines, antipodes or racemates thereof; and (b) stereoselectively reducing the products of step (a) to .sup.a (S)-[5(R)-alkyl(or alkenyl)-4(S)-quinuclidin-2(R)-yl]-4-quinoline-methanols, antipodes or racemates thereof, and .alpha.(R)-[5(R)-alkyl(or alkenyl)-4(S)-quinuclidin-2(S)-yl]-4-quinolinemethanols, antipodes or racemates thereof. Various intermediates and the end products are useful antimalarial and antiarrhythmic agents.
    Type: Grant
    Filed: August 20, 1975
    Date of Patent: June 20, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Juerg Albert Walter Gutzwiller, Milan Radoje Uskokovic
  • Patent number: 4092328
    Abstract: This invention relates to novel indolothiopyrones having the formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or aryl; R.sub.2 is hydrogen or halogen; and R.sub.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, nitro-substituted-aryl, or .omega.-substituted lower alkyl wherein the substituent is: ##STR2## wherein R.sub.4 and R.sub.5 each represent hydrogen, lower alkyl, or together with the nitrogen atom, form a heterocyclic ring; and R.sub.6 is lower alkoxy or amino, and novel intermediates used in their preparation. The indolothiopyrones are prepared by reacting a 3-mercaptoindole with sodium propiolate or a substituted sodium propiolate followed by acidification to obtain an intermediate acid; the intermediate acid cyclizes in the presence of an acid catalyst to obtain the indolothiopyrone structure which may be additionally subjected to halogenation, alkylation or hydrolysis to obtain derivatives having the various substituent groups disclosed.
    Type: Grant
    Filed: May 10, 1976
    Date of Patent: May 30, 1978
    Assignee: Warner-Lambert Company
    Inventor: Richard E. Brown
  • Patent number: 4091029
    Abstract: An N-perfluoroacyl-L-.alpha.-amino acid is converted to the corresponding acid halide which is useful as a resolving agent for the resolution of racemic amines.
    Type: Grant
    Filed: April 14, 1976
    Date of Patent: May 23, 1978
    Assignee: Eli Lilly and Company
    Inventor: Rex W. Souter
  • Patent number: 4089862
    Abstract: A process is disclosed for the preparation of a compound of the formula I ##STR1## where R is hydrogen or methyl, X is sulphur or the NH group, Y is selected from the class consisting of methyl, methoxy, chlorine, bromine, iodine, nitro or cyano, m is 0, 1 or 2, and n is 1 or 2, characterized in that a compound of the formula II: ##STR2## where R and n have the above-mentioned meanings, is reacted in a suitable polar aprotic solvent, such as dimethylforamide or dimethylsulphoxide, under a nitrogen atmosphere and at a temperature between 50.degree. and 100.degree. C, with the sodium salt of an appropriate 2-aminopyridine or 2-mercaptopyridine to give, after evaporation of the solvent in vacuo, the desired compound of formula I which is then purified by methods known "per se".The invention also includes the compounds of general formula I, where R, X, Y, m and n have the same meanings, and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: January 4, 1977
    Date of Patent: May 16, 1978
    Assignee: Societa' Farmaceutici Italia S.p.A.
    Inventors: Luigi Bernardi, Carlo Elli, Giovanni Falconi, Rosella Ferrari
  • Patent number: 4089969
    Abstract: Novel 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein R is hydrogen or a lower alkyl group containing from 1 to 4 carbon atoms and R.sup.1 is hydrogen, a lower alkyl group having from 1 to 4 carbon atoms, a lower alkoxy group of 1 to 4 carbon atoms, chloro, fluoro or bromo, the R.sup.1 substitution being at the ortho, meta or para positions of the aroyl group and process for the production of such compounds; 5-p-toluoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid is representative of the class. These compounds, as the racemic mixture or the (1)-isomer, are useful as anti-inflammatory, analgesic and antipyretic agents and as smooth muscle relaxants.
    Type: Grant
    Filed: February 23, 1977
    Date of Patent: May 16, 1978
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Arthur F. Kluge