Patents Examined by Jacqueline Haley
  • Patent number: 5403812
    Abstract: Unsaturated cyclohexenone oxime ethers I ##STR1## (Q=H, alkylcarbonyl, benzoyl, alkali metal or alkaline earth metal ion, substituted or unsubstituted ammonium ion, phosphonium ion, sulfonium ion, sulfoxonium ion, an equivalent of a transition metal cation;W=--C.ident.C-- or --CH=CH--;R.sup.1 =substituted or unsubstituted cycloalkyl, cycloalkenyl or 6-membered heterocyclic group which has 1-2 oxygen and/or sulfur atoms and can be saturated or partially unsaturated; substituted or unsubstituted 5-membered saturated heterocycle with 1-2 oxygen and/or sulfur atoms; substituted or unsubstituted 5-membered heteroaromatic group with 1-2 nitrogen atoms and/or 1 oxygen or sulfur atom; substituted or unsubstituted phenyl, pyridyl or R.sup.9 -X-substituted alkyl with X=O, S, --SO--, --SO.sub.2 -- andR.sup.9 =alkyl, phenyl, 5/6-membered hetaryl with 1-3 hetero atoms;R.sup.2 =alkyl;R.sup.3 =H, alkyl;R.sup.4 =H, halogen, alkyl;R.sup.5 =H, alkyl;or R.sup.3 +R.sup.4, R.sup.3 +R.sup.5 or R.sup.4 +R.sup.5 together form C.sub.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: April 4, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Juergen Kast, Norbert Meyer, Ulf Misslitz, Albrecht Harreus, Harald Rang, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 5399702
    Abstract: Compounds of the formula: ##STR1## wherein the substituents are as defined herein, and enantiomers, diastereomers, racemates and salts with pharmaceutically acceptable bases, antagonize LTD.sub.4 action and thus, are useful in treating bronchial asthma, pulmonary anaphylaxis, cystic fibrosis, chronic bronchitis, bronchiectasis, respiratory distress syndrome and pulmonary oedema.
    Type: Grant
    Filed: September 2, 1993
    Date of Patent: March 21, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: George W. Holland, John R. Vermeulen, William J. Zally
  • Patent number: 5397798
    Abstract: The present invention provides novel benzamides and sulfonamides, formulations thereof, and intermediates thereto. The benzamides and sulfonamides of the present invention are useful as hypoglycemic agents and, accordingly, a method of using such compounds to lower a mammal's blood glucose level is also provided.
    Type: Grant
    Filed: July 21, 1992
    Date of Patent: March 14, 1995
    Assignee: Eli Lilly and Company
    Inventors: Lora L. Fitch, Klaus K. Schmiegel
  • Patent number: 5397799
    Abstract: Crystalline 4-(di-n-propyl)amino-6-aminocarbonyl-1,3,4,5-tetrahydrobenz[cd]indole hippurate and its method of preparation and use are provided.
    Type: Grant
    Filed: May 19, 1993
    Date of Patent: March 14, 1995
    Assignee: Eli Lilly and Company
    Inventors: Thomas J. Kress, David L. Varie
  • Patent number: 5395943
    Abstract: The invention provides a method of purifying 2-alkyl-4-halo-5-formylimidazoles, which comprises dissolving an 2-alkyl-4-halo-5-formylimidazole in an aqueous solution of a sulfonating agent, adjusting the solution to pH 1-6, and removing the impurity 2-alkyl-4,5-dihaloimidazole by filtration or extraction.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: March 7, 1995
    Assignee: Nippon Gohsei Kagaku Kogyo Kabushiki Kaisha
    Inventors: Toshio Yamamoto, Yoshihiro Hibi, Toshimi Ogawa
  • Patent number: 5395945
    Abstract: The compound, 3,3-dinitroazetidine, and a process of preparing 3,3-dinitroazetidine including reacting a mixture of 1-tertiary-butyl-3,3-dinitroazetidine and benzyl chloroformate to form 1-(benzyloxycarbonyl)-3,3-dinitroazetidine, reacting the 1-(benzyloxycarbonyl)-3,3-dinitroazetidine and trifluoromethanesulfonic acid to form 3,3-dinitroazetidinium trifluoromethanesulfonate, and neutralizing the 3,3-dinitroazetidinium trifluoromethanesulfonate with a base to form 3,3-dinitroazetidine are provided. Salts of the 3,3-dinitroazetidine and preparation of such salts are also disclosed.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: March 7, 1995
    Assignee: The United States of America as represented by the United States Department of Energy
    Inventor: Michael A. Hiskey
  • Patent number: 5391567
    Abstract: Malignancy-induced hypercalcemia is treated with thionapthene-2-carboxylic acid (TNCA) and the pharmaceutically acceptable salts thereof. The treatment is also effective in tumor bearing hosts even before there is significant abnormal serum calcium levels. There is no "escape" from the hypocalcemic effects of these compounds as with e.g., calcitonin. The useful dosage in humans for TNCA itself ranges from about 1 to about 60 mg/kg/day preferably from about 2 to about 30 mg/kg/day and more preferably from about 5 to about 20 mg/kg/day (20 mg is approximately 0.106 mmol) Orally administered TNCA or salts thereof, is a much desired and obviously clinically advantageous mode of administering compounds to control or ameliorate hypercalcemia.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: February 21, 1995
    Assignee: Macrochem Corporation
    Inventors: Lawrence G. Raisz, Carlos M. Samour
  • Patent number: 5391566
    Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh
  • Patent number: 5387603
    Abstract: Indoline compounds represented by the formula: ##STR1## wherein R represents a saturated or unsaturated aliphatic acyl group which may have one or more halogen atoms, a hydroxy group, a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, a cycloalkyl group or an aryl group as substituents; a hydroxyalkyl group; an aliphatic acyloxyalkyl group; a lower alkyl group having a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, an aryl substituted lower alkoxycarbonyl group, a carbamoyl group, a mono- or dialkyl substituted carbamoyl group or a cyano group as substituents; an aromatic acyl group which may have one or more halogen atoms as substituents; a furoyl group or a pyridylcarbonyl group; R.sup.
    Type: Grant
    Filed: December 1, 1993
    Date of Patent: February 7, 1995
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Makio Kitazawa, Masaaki Ban, Kosuke Okazaki, Motoyasu Ozawa, Toshikazu Yazaki, Ryoichi Yamagishi
  • Patent number: 5385923
    Abstract: 4-R.sup.4 --R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 --R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.
    Type: Grant
    Filed: August 20, 1993
    Date of Patent: January 31, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Lee H. Latimer, Richard P. Dunlap
  • Patent number: 5385927
    Abstract: New 2-hydroxyl-3-[1-(1H-imidazol-4-yl)alkyl]-benzenecarboximidamides as well as their salts, having the formula ##STR1## wherein R.sub.1 is hydrogen or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 is hydrogen a hydroxyl group, an amino group or an alkyl radical having 1 to 4 carbon atoms,R.sub.3 is hydrogen, or R.sub.2 and R.sub.3 together are --CH.sub.2 -CH.sub.2 --;processes for the preparation thereof, and ophthalmic compositions comprising the same are also described. These compounds are capable of lowering intraocular pressure and can be used in the prevention and treatment of glaucoma.
    Type: Grant
    Filed: May 24, 1994
    Date of Patent: January 31, 1995
    Assignee: U C B, S.A.
    Inventors: Philippe Michel, Eric Cossement, Jean Gobert, Ernst Wulfert
  • Patent number: 5384413
    Abstract: The present invention relates to a process for the preparation of tetrafluorophthalic acid and/or tetrafluorophthalic anhydride by reacting a compound of the formula ##STR1## in which X is a radical ##STR2## which is optionally mono- or polysubstituted on the aromatic nucleus by fluorine and/or chlorine and/or alkyl groups having 1 to 4 carbon atoms, or is a radical ##STR3## in which R.sub.1, R.sub.2 and R.sub.3 are as defined, with water, and subsequently removing the water still present by azeotropic distillation or extracting the tetrafluorophthalic acid and/or its anhydride with a water-insoluble solvent or solvent mixture.
    Type: Grant
    Filed: July 12, 1993
    Date of Patent: January 24, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ralf Pfirmann, Theodor Papenfuhs
  • Patent number: 5384322
    Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: A represents, with the nitrogen and carbon atoms to which it is bound, a heterocycle,B represents, with the nitrogen atom to which it is bound, a heterocycle,R.sub.1 represents alkoxy, benzyloxy, phenoxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or substituted or unsubstituted cycloalkyl,their enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid, medicinal products containing the same.
    Type: Grant
    Filed: September 30, 1993
    Date of Patent: January 24, 1995
    Assignee: Adir et Compagnie
    Inventors: Michel Vincent, Georges Remond, Bernard Portevin, Yolande Herve, Jean Lepagnol, Guillaume de Nanteuil
  • Patent number: 5382592
    Abstract: A series of serotonergic 5-cyclobutenedionylamino-substituted tryptamine derivatives of Formula I is disclosed for use in the alleviation of vascular headaches. ##STR1## The formula I substituents, as further defined in the specification, are: R.sup.1 is hydrogen, halogen, and alkyl; R.sup.2 and R.sup.3 can be hydrogen or alkyl; R.sup.4 is hydrogen, alkyl, acyl or alkylsulfonyl; m is 0 to 3 and n is 1 to 5; and X is amino, alkoxy, hydrogen, alkyl, aryl or alkylaryl.
    Type: Grant
    Filed: September 16, 1993
    Date of Patent: January 17, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jonas A. Gylys, Edward H. Ruediger, David W. Smith, Carola Solomon, Joseph P. Yevich
  • Patent number: 5380742
    Abstract: Pyrrole derivatives of formula: ##STR1## in which R.sub.1 represents a hydrogen or halogen atom, a linear or branched C.sub.1-6 alkyl group, a C.sub.3-6 alkenyl group, a C.sub.1-4 alkoxymethyl group, benzyl, a phenyl group optionally substituted by one or more halogen atoms or alkyl radicals, a CO.sub.2 R group in which R represents a linear or branched C.sub.1-4 alkyl radical, phenyl or benzyl, or a CONR'R" group in which R' and R" each represent, independently of one another, a hydrogen atom or a linear or branched C.sub.1-4 alkyl radical,R.sub.2 represents a hydrogen or halogen atom or a linear or branched C.sub.1-4 alkyl group,and R.sub.3 represents a 4,5-dihydro-1H-imidazol-2-yl or 1H-imidazol-4-yl group, and their addition salts with pharmaceutically acceptable acids are useful in therapeutics as .alpha..sub.2 -antagonists, and .alpha..sub.1 -agonists.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: January 10, 1995
    Assignee: Synthelabo
    Inventors: Mireille Sevrin, Jacques Menin, Christian Maloizel, Juan A. Diaz Martin, Ulpiano Martin Escudero Perez, Manuel Bedoya Zurita, Gregorio Del Sol Moreno, Maria D. Jimenez Bargueno, Magali Romanach Ferrer
  • Patent number: 5380737
    Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L-R.sup.1 is a leaving group, H-L-R.sup.1 is the conjugate acid thereof and, when L is N, H-L-R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H-L-R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H-L-R.sup.1 has a pK.sub.a value less than or equal to 5;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.
    Type: Grant
    Filed: August 27, 1993
    Date of Patent: January 10, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Albert A. Mura, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam
  • Patent number: 5378680
    Abstract: Dicarboximides of the formulae Ia, Ib and Ic ##STR1## where X is oxygen or sulfur,R.sup.1 is hydrogen, halogen, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, haloalkoxy, haloalkylthio, alkylsulfonyl, haloalkylsulfonyl, phenyl, phenylalkyl, phenoxy or phenylthio, a 5-membered or 6-membered saturated or aromatic heterocyclic radical containing one or two hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen, where the stated organic radicals may be further substituted, andR.sup.2 is hydrogen, hydroxyl, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, di-C.sub.1 -C.sub.
    Type: Grant
    Filed: August 19, 1992
    Date of Patent: January 3, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Maywald, Klaus Ditrich, Thomas Kuekenhoehner, Gerhard Hamprecht, Wolfgang Freund, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 5378713
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: January 3, 1995
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5376653
    Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.
    Type: Grant
    Filed: August 19, 1993
    Date of Patent: December 27, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Lee H. Latimer, Chakrapani Subramanyam
  • Patent number: 5376685
    Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
    Type: Grant
    Filed: May 7, 1993
    Date of Patent: December 27, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Jaroslav Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro