Patents Examined by Natalia Harkaway
  • Process for the production of pyridone compounds
    Patent number: 4243809
    Abstract: The invention provides compounds of the formula ##STR1## wherein each of R.sub.1 and R.sub.2 independently is a hydrogen atom or a substituted or unsubstituted alkyl or aryl radical, R.sub.3 is a hydrogen atom or the carbamoyl radical, and X is a substituted or unsubstituted alkyl or alkenyl radical. A process for preparing these compounds is also disclosed.
    Type: Grant
    Filed: October 26, 1978
    Date of Patent: January 6, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Karl Seitz
  • Process for the chemical catalytic hydrolysis of an .alpha.-aminonitrile or of one of the salts thereof
    Patent number: 4243814
    Abstract: A process for the chemical catalytic hydrolysis of an .alpha.-aminonitrile or of one of the salts thereof, characterized in that an aqueous solution containing at least one carbonyl derivative is reacted with the said .alpha.-amine nitrile or with one of the salts thereof in the presence of hydroxide ions.
    Type: Grant
    Filed: December 1, 1977
    Date of Patent: January 6, 1981
    Inventors: Robert Pascal, Monique Lasperas nee Marnier, Alain Rousset, Auguste Commeyras, Jacques Taillades, Louis Mion
  • 5-(Optionally substituted 2-aminophenyl)-1H-pyrazole-3-methanol
    Patent number: 4239896
    Abstract: Intermediates are provided having the structure ##STR1## wherein X is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl. These intermediates are useful in preparing pyrazolo[1,5-c]quinazoline anti-allergy compounds.
    Type: Grant
    Filed: October 18, 1979
    Date of Patent: December 16, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: B. Richard Vogt, Ligaya M. Simpkins
  • Antimycotic substituted diphenyl-imidazolyl-methanes
    Patent number: 4238498
    Abstract: The invention provides a series of substituted diphenyl-imidazolyl-methanes useful as antimycotic agents. Also included in the invention are pharmaceutical compositions containing said diphenyl-imidazolyl-methanes and methods for the use of said compounds and compositions. The invention additionally includes methods for the manufacture of the diphenyl-imidazolyl-methanes.
    Type: Grant
    Filed: February 1, 1979
    Date of Patent: December 9, 1980
    Assignee: Bayer Aktiengesellschaft
    Inventors: Erik Regel, Karl H. Buchel, Wilfried Draber, Manfred Plempel, Ingo Haller
  • 2-(Substituted amino)-3-nitro-2,3-unsaturated nitrogen heterocycles
    Patent number: 4238493
    Abstract: 2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur or oxygen. The compounds of the invention are preferably dihydropyrroles or tetrahydropyridines or pyrimidines. The compounds of the invention are histamine H.sub.2 -receptor antagonists.
    Type: Grant
    Filed: May 30, 1979
    Date of Patent: December 9, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Process for the preparation of diacylated 4-imidazolin-2-ones
    Patent number: 4238618
    Abstract: A process for the preparation of a diacylated 4-imidazolin-2-one of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, optionally substituted alkyl, cycloalkyl, aryl and alkoxy, which comprises contacting a compound of the formula of II ##STR2## wherein R.sup.1 and R.sup.2 of the previously assigned significance with a source of chlorine at a temperature from 20.degree. to 150.degree. C. in the presence of a radical forming agent or under ultra-violet light and thereafter dehydrohalogenating or dehalogenating the resultant chlorinated product the diacylated 4-imidazolin-2-ones prepared by the process are useful for photochemical cycloadditions and as intermediates for the preparation of compounds in the biotin series.
    Type: Grant
    Filed: March 8, 1978
    Date of Patent: December 9, 1980
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl-Heinz Scholz, Willy Hartmann, Hans-Georg Heine
  • 2-Heterocyclic alkylamino-3-nitropyrroles
    Patent number: 4238494
    Abstract: 3-Nitro-2-substituted aminopyrroles are histamine H.sub.2 -receptor antagonists. The 2-position substituent is a fully-unsaturated heterocyclyl alkyl group preferably with with alkyl group interrupted by sulfur or oxygen. The 4- and 5-positions of the pyrrole ring can also be substituted.
    Type: Grant
    Filed: May 30, 1979
    Date of Patent: December 9, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Process for producing hydrazone derivatives of pyridinaldehydes
    Patent number: 4237275
    Abstract: An improved process for producing pyridinaldehydes and hydrazone derivatives thereof, for example, pyridinaldehyde-phenylhydrazones, is described. This comprises reacting a aminomethylpyridine with an aldehyde or a ketone to give a compound of the formula ##STR1## isomerizing the compound (III), in the presence of suitable catalysts, to a compound of the formula ##STR2## and converting the compound (V), in the presence of an acid and optionally in the presence of a hydrazine, into a pyridinaldehyde or a pyridinaldehyde-hydrazone. It is possible to produce by the process according to the invention pyridinaldehydes and pyridinaldehyde-hydrazones in a simple manner, under mild ecologically favorable conditions and in good to very good yields.
    Type: Grant
    Filed: May 29, 1979
    Date of Patent: December 2, 1980
    Assignee: Ciba-Geigy Corporation
    Inventors: Rolf Bader, Dieter Reinehr
  • Octahydro-2H-pyrrolo[3,4-g]quinolines
    Patent number: 4235909
    Abstract: Octahydro-2H-pyrrolo[3,4-g]quinolines, useful as dopamine agonists, particularly as inhibitors of prolactin secretion and in treatment of Parkinsonism.
    Type: Grant
    Filed: April 19, 1979
    Date of Patent: November 25, 1980
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Edmund C. Kornfeld
  • 3-Nitropyrazole derivatives
    Patent number: 4235995
    Abstract: Novel 1,4-disubstituted-3-nitropyrazoles having antimicrobial, parasiticidal, and herbicidal activity are prepared by a reaction sequence of which the individual steps are conventional. The new 3-nitropyrazoles are characterized by a 1-substituent and a usually carbonyl-containing 4-substituent. The novel 3(5)-nitro-4-pyrazolecarbonitrile is obtained as an intermediate in the preparation of the biologically-active compounds. Preferred compounds are 1-alkyl or -alkenyl-4-pyrazolecarboxamides are carbonitriles. The new compounds are particularly useful for the control of bacterial animal diseases.
    Type: Grant
    Filed: September 25, 1978
    Date of Patent: November 25, 1980
    Assignee: Eli Lilly and Company
    Inventors: Reuben G. Jones, Norman H. Terando
  • 4-[6-(2-Chloro-4-methoxyphenoxy)hexyl] -3,5-diethyl-1-[4-(4-morpholinyl)-1-oxobutyl]-1H-pyrazole
    Patent number: 4234725
    Abstract: 4-(Aryloxyalkyl)pyrazoles of the formula ##STR1## useful as antiviral agents, are prepared by reacting the corresponding diketones of the formula Ar--O--Alk--CH(COR')COR" with hydrazine or a substituted hydrazine H.sub.2 NNHR.
    Type: Grant
    Filed: October 24, 1979
    Date of Patent: November 18, 1980
    Assignee: Sterling Drug Inc.
    Inventors: Guy D. Diana, Philip M. Carabateas
  • Antiandrogenic and schistosomicidal imidazolidine derivatives
    Patent number: 4234736
    Abstract: Imidazolidine derivatives, as well as processes for their preparation, which have antiandrogenic and schistosomicidal activity.
    Type: Grant
    Filed: October 24, 1978
    Date of Patent: November 18, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Helmut Link, Harro Stohler
  • 4-[6-( 2-Chloro-4-methoxyphenoxy)hexyl]-3,5-diethyl-1-(2-pyridinyl)-1H-pyrazole
    Patent number: 4232161
    Abstract: 4-(Aryloxyalkyl)pyrazoles of the formula ##STR1## useful as antiviral agents, are prepared by reacting the corresponding diketones of the formula Ar-O-Alk-CH(COR')COR" with hydrazine or a substituted hydrazine H.sub.2 NNHR.
    Type: Grant
    Filed: October 24, 1979
    Date of Patent: November 4, 1980
    Assignee: Sterling Drug Inc.
    Inventors: Guy D. Diana, Philip M. Carabateas
  • .alpha.-Alkyl-.alpha.-hydroxybenzyl-substituted 1-sulfonylbenzimidazoles
    Patent number: 4230868
    Abstract: Various carbinol substituted benzimidazoles, for example certain .alpha.-alkyl-.alpha.-hydroxybenzyl substituted-1-sulfonylbenzimidazole compounds, are dehydrated to provide alkylidenylmethyl substituted benzimidaloles which are useful as antiviral agents.
    Type: Grant
    Filed: April 17, 1979
    Date of Patent: October 28, 1980
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Paget, James W. Chamberlin, James H. Wikel
  • Process for preparing 5-(4-hydroxyphenyl)hydantoin
    Patent number: 4230869
    Abstract: A process for preparing 5-(4-hydroxyphenyl)hydantoin by reacting glyoxylic acid, urea and phenol in an aqueous medium in the presence of an acid at an elevated temperature. The hydantoin of high purity can be readily prepared in good yields.
    Type: Grant
    Filed: March 16, 1978
    Date of Patent: October 28, 1980
    Assignee: Kanegafuchi Kagaku Kogyo Kabushiki Kaisha
    Inventors: Koji Yoneda, Takehisa Ohashi, Tomoaki Nagamachi, Hirotaka Fukumitsu, Satomi Takahashi
  • Pyrazoles active in the central nervous system
    Patent number: 4226877
    Abstract: Disclosed are pyrazoles of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, or phenyl, R.sub.2 is hydrogen or lower alkyl, R.sub.3 is alkoxy or hydroxy, R.sub.4 is lower alkyl, and the pharmaceutically acceptable acid addition salts thereof. The compounds are useful primarily as antipsychotic agents. As an example, they exhibit central nervous system activity as antischizophrenic agents.
    Type: Grant
    Filed: May 14, 1979
    Date of Patent: October 7, 1980
    Assignee: Abbott Laboratories
    Inventor: David L. Arendsen
  • 2-Substitute d-trans-5-aryl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles
    Patent number: 4224329
    Abstract: 2-Substituted-5-aryl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles of the formula (I): ##STR1## and the pharmaceutically-acceptable salts thereof, wherein the hydrogen atoms in the 4a position and 9b positions are in a trans relationship to each other and the 5-aryl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole moiety is dextrorotatory; X.sub.1 and Y.sub.1 are the same or different and are each hydrogen or fluoro; Z.sub.1 is hydrogen, fluoro or methoxy; M is a member selected from the group consisting of ##STR2## a mixture thereof and C.dbd.O and n is 3 or 4; their use as tranquilizing agents, pharmaceutical compositions containing them and a process for their production.
    Type: Grant
    Filed: January 23, 1979
    Date of Patent: September 23, 1980
    Assignee: Pfizer Inc.
    Inventor: Willard M. Welch, Jr.
  • 3,5,6-Trifluoro-2-pyridinyl phosphorus compounds
    Patent number: 4224318
    Abstract: Compounds are prepared which correspond to the formula ##STR1## wherein R represents alkyl of 1 to 4 carbon atoms and R.sup.1 represents OR, phenyl or ethyl. These compounds have been found to be highly active in the kill and control of soil insects.
    Type: Grant
    Filed: December 1, 1978
    Date of Patent: September 23, 1980
    Assignee: The Dow Chemical Company
    Inventor: Chester E. Pawloski
  • 6-Fluoro-3,5-dichloro-2-pyridinyl phosphorus compounds
    Patent number: 4223025
    Abstract: Compounds are prepared which correspond to the formula ##STR1## wherein R represents alkyl of 1 to 4 carbon atoms and R.sup.1 represents OR, amino or mono- or dialkylamino wherein each alkyl group is of 1 to 4 carbon atoms. These compounds have been found to be highly active in the kill and control of soil insects.
    Type: Grant
    Filed: December 1, 1978
    Date of Patent: September 16, 1980
    Assignee: The Dow Chemical Company
    Inventor: Raymond H. Rigterink
  • 4,5,6,7-Tetrahydroimidazo-[4,5-c]-pyridine derivatives
    Patent number: 4223146
    Abstract: Compounds are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms; R.sub.2 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms; and R.sub.3 is a saturated or unsaturated straight or branched alkyl having from 1 to 4 carbon atoms. A process for making such compounds is also disclosed. These compounds are useful as antiulcer agents and as inhibitors of gastric secretion.
    Type: Grant
    Filed: November 13, 1978
    Date of Patent: September 16, 1980
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Giuliana Arcari, Luigi Bernardi, Giovanni Falconi, Ugo Scarponi