Patents Examined by Cecilia Shen
  • Patent number: 5037830
    Abstract: The present invention relates to novel compounds of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently from each other, for hydrogen, C.sub.1-4 alkyl, phenyl, phenyl-C.sub.1-4 alkyl, piridyl or piridyl-C.sub.1-4 alkyl group;E means a straight or branched, saturated hydrocarbon chain containing 1 to 6 carbon atoms;R.sub.3 represents: a phenyl group ortho-substituted by a C.sub.2-5 alkanoylamino, N-C.sub.2-5 alkanoyl-N-C.sub.1-4 alkylamino or di(C.sub.1-4 alkyl)amino group and optionally further substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.2-5 alkanoyloxy group; or a pyridyl group optionally mono- or polysubstituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 alkanoyloxy or phenyl-C.sub.1-4 alkoxy groupas well as their acid addition salts and tautomeric forms of these compounds.
    Type: Grant
    Filed: March 29, 1990
    Date of Patent: August 6, 1991
    Assignee: Richter Gedeon Vegyeszeti Gyar RT
    Inventors: Gabor Zolyomi, Ferenc Andrasi, Pal Berzsenyi, Elemer Ezer, Tibor Hasko, Erzsebet F. Birkas, Erno Koltai, Judit Matuz, Lajos Toldy, Laszlo Sebestyen, Zsuzsanna Fittler, Katalin Saghy, Laszlo Szporny, Peter Aranyi
  • Patent number: 5037827
    Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: August 6, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Kazuo Okano, Osamu Asano, Naoyuki Shimomura, Tetsuya Kawahara, Shinya Abe, Shuhei Miyazawa, Mitsuaki Miyamoto, Hiroyuki Yoshimura, Koukichi Harada, Junsaku Nagaoka, Tsutomu Kawata, Tsutomu Yoshimura, Hiromasa Suzuki, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
  • Patent number: 5037832
    Abstract: 2-Substituted ergolines ##STR1## wherein C.sub.2 C.sub.3 and C.sub.9 C.sub.10 represent a single or double bond;X is oxygen or sulfur;R.sup.2 is C.sub.1-10 alkyl, optionally halogen-substituted C.sub.2-10 alkenyl, CH.sub.2 YR.sup.3, CR.sup.12 (OR.sup.4)R.sup.5, CH.sub.2 -CHR.sup.9 -COR.sup.10 or COR.sup.12, whereinY is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1-4 alkyl, phenyl, C.sub.2-5 acyl or phenyl C.sub.1-4 alkyl,R.sup.4 is hydrogen or C.sub.2-5 acyl,R.sup.5 is C.sub.1-9 alkyl,R.sup.9 is COCH.sub.3 or COO-C.sub.1-4 alkyl,R.sup.10 is C.sub.1-4 alkyl or O-C.sub.1-4 alkyl,R.sup.12 is hydrogen or C.sub.1-9 alkyl; andR.sup.6 is C.sub.2-10 alkyl, C.sub.3-10 alkenyl or C.sub.4-10 cycloalkyl-C.sub.1-3 -alkyl,and acid addition salts, isomers and isomeric mixtures thereof are dopaminergic agonists and useful for treating Parkinson's Disease.
    Type: Grant
    Filed: July 17, 1989
    Date of Patent: August 6, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Thomas Brumby, Gerhard Sauer, Josef Heindl, Jonathan Turner, Gerhard Kuhne, Helmut Wachtel
  • Patent number: 5036058
    Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is an aromatic radical, n is 0, 1, 2 or 3, X is an oxy group, a thio group which can be oxidized or an imino group which is unsubstituted or has aliphatic substituents, alk.sub.1 and alk.sub.2 are identical or different divalent aliphatic radicals, and R.sub.2 is hydrogen or a monovalent aliphatic radical and salts thereof have properties which regulate calcium metabolism and can be employed for the treatment of diseases connected with disturbances in this metabolism. They are prepared, for example, by reacting a compound of the formula ##STR2## in which X.sub.3 is carboxyl with a phosphorylating agent and hydrolysing the primary product.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: July 30, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • Patent number: 5036070
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, or phenyl, or R.sup.1 and R.sup.2 taken together represent --(CH.sub.2).sub.4 -- or ##STR2## where the dotted line represents an optional double bond; R.sup.3 is hydrogen, alkyl, alkoxy, or halo;Z is oxygen, or --N(R.sup.6), where R.sup.6 is hydrogen or alkyl;m is 1-4;n is 0-2; ##STR3## wherein R.sup.7 is unsubstituted or substituted phenyl, 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl, or diphenylmethyl, where the substituents are selected from the group of alkyl, alkoxy, halo, cyano, nitro and trifluoromethyl;R.sup.8 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, or NHR.sup.9 where R.sup.9 is hydrogen, alkyl, phenyl, tolyl, xylyl, mesityl, methoxyphenyl, or halophenyl with the proviso when Z is oxygen, R.sup.
    Type: Grant
    Filed: June 13, 1990
    Date of Patent: July 30, 1991
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Patent number: 5034390
    Abstract: The present invention concerns novel compounds of the general formula; ##STR1## wherein R.sub.1 is halogen or hydrogen and R.sub.2 is halogen; X is either oxygen, sulfor or methyleneR.sub.3 and R.sub.4 are the same or different and selected from hydrogen and lower alkyl;n is 2 or 3;A is selected from the following pyrimidyl or pyridyl groups ##STR2## wherein R.sub.5 is selected from hydrogen, lower alkyl or halogen; R.sub.6 and R.sub.7 are the same or different and selected from hydrogen, halogen, lower alkyl, electron donor groups such as lower alkoxy or hydroxy, electron acceptor groups such as cyano, nitro, trifluoromethyl, COOR.sub.8, CONR.sub.9 R.sub.10 or CO-B;wherein R.sub.8 is hydrogen or lower alkyl;R.sub.9 and R.sub.10 are the same or different and selected from hydrogen, lower alkyl and cycloalkyl;B is selected from ##STR3## wherein m is 1, 2, 3 or 4. R.sub.11 is selected from hydrogen or lower alkyl, and the pharmacologically active salts thereof.
    Type: Grant
    Filed: September 28, 1989
    Date of Patent: July 23, 1991
    Assignee: Pharmacia AB
    Inventors: Knut G. Olsson, Aina L. Abramo, Erik T. Lundstedt, Curt Nordvi
  • Patent number: 5034541
    Abstract: A method of preparing 1-phenyl-1-diethylaminocarbonyl-2-phthalimidomethyl-cyclopropane-Z and key intermediates therefor are disclosed.This method is characterized by the following successive steps:opening of the 1-phenyl-2-oxo-3-oxa-bicyclo(3:1:0)-hexane by diethylamine or a tertiary amine with the aid of a Lewis acid/amine complex:the 1-phenyl-1-diethylaminocarbonyl-2-hydroxymethyl-cyclopropane-Z thus obtained is converted into a 2-chlorinated derivative by the action of a chlorination reagent such as thionyl chloride; andthe 1-phenyl-1-diethylaminocarbonyl-2-chloromethylcyclopropane-Z is reacted with a phthalimide salt in an organic solvent to produce the 1-phenyl-1-diethylaminocarbonyl-2-phthaliumidomethyl-cyclopropane-Z.
    Type: Grant
    Filed: December 27, 1989
    Date of Patent: July 23, 1991
    Assignee: Pierre Fabre Medicament
    Inventors: Dennis C. H. Bigg, Patrick Lesimple
  • Patent number: 5034388
    Abstract: This invention relates to derivatives of acrylic acid of the formula: ##STR1## useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants. The values of the variables are provided herein.
    Type: Grant
    Filed: March 7, 1990
    Date of Patent: July 23, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey
  • Patent number: 5034394
    Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. Also provided are pharmaceutical formulations and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: December 22, 1989
    Date of Patent: July 23, 1991
    Assignee: Burroughs Wellcome Co.
    Inventor: Susan M. Daluge
  • Patent number: 5034392
    Abstract: This invention relates to compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are independently hydrogen or loweralkyl or R.sub.1 and R.sub.2 taken together with the carbon atom to which they are attached form a spiro-fused cycloalkane of 5 to 8 carbons; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a spiro-fused cycloalkane of 5 to 8 carbons; R.sub.5 and R.sub.6 taken together with the nitrogen atom to which they are attached are ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, amino, cyano, trifluoromethyl or methoxy; and m is 0, 1 or 2; the pharmaceutically acceptable acid addition salts thereof and where applicable the optical and geometrical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesic and antihypertensive agents.
    Type: Grant
    Filed: April 16, 1990
    Date of Patent: July 23, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventor: Nicholas J. Hrib
  • Patent number: 5032592
    Abstract: A compound of the formula ##STR1## wherein X has the formula ##STR2## wherein ring a is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl; wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent selected from halogeno, nitro, cyano, trifluoromethyl, alkylthio, alkylsulphinyl, and alkylsulphonyl or each is hydrogen, alkyl, alkoxy or dialkylamino provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent; wherein R.sup.5 and R.sup.6, which may be the same or different, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 is carbamoyl, alkyl, cycloalkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalkenyl, halogenoalkynyl, alkanoyl, alkylcarbamoyl, dialkylcarbamoyl or aroyl; or wherein R.sup.
    Type: Grant
    Filed: May 30, 1989
    Date of Patent: July 16, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: Leslie R. Hughes, John Oldfield, Howard Tucker
  • Patent number: 5032588
    Abstract: Compounds of the formulae: ##STR1## and pharmaceutically acceptable salts, esters and prodrugs thereof, wherein M and R.sub.1 are independently selected from among optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, reduced heteroaryl and reduced heteroarylalkyl groups, andZ is the residue of a compound selected from the class of compounds known as non-steroidal antiinflammatory grugs containing a carboxylic acid group, of the general form Z-COOH.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: July 16, 1991
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Francis A. J. Kerdesky
  • Patent number: 5032604
    Abstract: Compounds of structural formula: ##STR1## wherein R' is hydrogen or an aromatic ring system, and Q is a substituted nitrogen or a nitrogen containing heterocycle, and E is --S-- or --O--, are Class III antiarrhythmic agents.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: July 16, 1991
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
  • Patent number: 5032598
    Abstract: Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members and Q is a nitrogen containing heterocycle, are antiarrhythmic agents.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: July 16, 1991
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
  • Patent number: 5030728
    Abstract: A molecule capable of forming stable complexes with urea, guanidine or amidine compounds and the acid addition salts thereof comprises a nucleus of heterocyclic rings.
    Type: Grant
    Filed: June 2, 1989
    Date of Patent: July 9, 1991
    Assignee: The Research Foundation State University of New York
    Inventor: Thomas W. Bell
  • Patent number: 5028711
    Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: July 2, 1991
    Assignee: Beiersdorf Aktiengesellschaft
    Inventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
  • Patent number: 5028606
    Abstract: (1H-azol-1-ylmethyl)substituted quinoxaline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: July 2, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marc G. Venet, Gerard C. Sanz, Alfons H. M. Raeymaekers, Eddy J. E. Freyne
  • Patent number: 5026707
    Abstract: This invention provides ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes which are selective inhibitors of serotonin reuptake.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: June 25, 1991
    Assignee: Eli Lilly and Company
    Inventors: James A. Nixon, Richard P. Pioch, John M. Schaus, Robert D. Titus
  • Patent number: 5026853
    Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.
    Type: Grant
    Filed: September 20, 1990
    Date of Patent: June 25, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
  • Patent number: 5026704
    Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is C.sub.1-12 -alkyl, which may optionally be substututed by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C.sub.3-8 -cycloalkyl, aryl, aralkyl; and wherein R.sup.6 is, hydrogen, halogen, CN, CF.sub.3, NO.sub.2, or OR', wherein R' is C.sub.1-4 -alkyl and R.sup.5, R.sup.7 and R.sup.8 is hydrogen, provided R.sup.6 is not CF.sub.3, OCH.sub.3, NO.sub.2, Cl or Br when R.sup.1 is CH.sub.3 ; orR.sup.6 and R.sup.7 independently are NO.sub.2, halogen, CN, CF.sub.3, or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.8 are each hydrogen; orR.sup.5 and R.sup.6 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.7 and R.sup.8 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 - alkyl; orR.sup.7 and R.sup.
    Type: Grant
    Filed: December 26, 1989
    Date of Patent: June 25, 1991
    Assignee: Novo Nordisk A/S
    Inventors: Tage Honore, Poul Jacobsen, Flemming E. Nielsen, Lars Naerum