Patents Examined by G. Hendricks
  • Patent number: 4709035
    Abstract: 2,6-Disubstituted derivatives of 3-nitropyrazine are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.
    Type: Grant
    Filed: September 4, 1984
    Date of Patent: November 24, 1987
    Assignee: Merck & Co., Inc.
    Inventor: George D. Hartman
  • Patent number: 4681880
    Abstract: 9-thia ergot cyclic peptide alkaloids produced by fermentation or synthetic methods have interesting anti-parkinson and other pharmacological activities.
    Type: Grant
    Filed: July 2, 1985
    Date of Patent: July 21, 1987
    Assignee: Sandoz Ltd.
    Inventors: Hans Kobel, Jean-Jacques Sanglier, Hans Tscherter, Georg Bolliger
  • Patent number: 4681877
    Abstract: Disclosed herein are 7-beta-[2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-(2-amino-1,3,4- thiadiazolyl-5-thiomethyl)-3-cepheme-4-carboxylic acid, salts thereof and pivaloyloxymethyl ester thereof, and a pharmaceutical composition containing the same as an active ingredient.
    Type: Grant
    Filed: December 16, 1983
    Date of Patent: July 21, 1987
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Shigeaki Muto, Takao Ando, Takayoshi Fujii, Akihiko Kanno, Yoko Onishi, Isamu Motokawa, Takao Furusho, Chikao Yoshikumi
  • Patent number: 4680412
    Abstract: Fluorophthalimides are prepared by a process in which a fluorophthalic anhydride is reacted, in the presence of an aliphatic sulfone, with from 0.4 to 0.8 mole of urea per mole of fluorophthalic anhydride, and the reaction is carried out first at C. and then at C.
    Type: Grant
    Filed: May 31, 1984
    Date of Patent: July 14, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Juergen Varwig, Wolfgang Rohr
  • Patent number: 4675404
    Abstract: Ergoline derivatives of formula: ##STR1## wherein n=0,1,2; R.sub.1 =H, CH.sub.3 ; R.sub.2 =H, CH.sub.3, halogen; R.sub.3 =H, OCH.sub.3 ; R.sub.4 =hydrocarbon group and R.sub.5 is a residue of general formula II, III, IV, V, VI, VII: ##STR2## wherein R.sub.6 =H, Cl, OCH.sub.3, NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 =H, lower alkyl; phenyl or are bonded together to form a heterocyclic ring, R.sub.7, R.sub.8 and R.sub.9 and R.sub.10 =H or C.sub.1 -C.sub.3 alkyl, with the proviso that if R.sub.5 is of formula II and R.sub.2 =R.sub.7 =R.sub.8 =H, then R.sub.4 is not methyl or n is not 0.Pharmaceutically acceptable acid addition salts are also provided. A method for their preparation is also provided.The compounds have anti-depressive, anti-hypertensive and antiprolactin activity.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: June 23, 1987
    Assignee: Farmitala Carlo Erba S.p.A.
    Inventors: Luigi Bernardi, Aldemio Temperilli, Germano Bosisio, Gabriella Traquandi, Rosanna Eccel, Alessandro Rossi, Patricia Salvati
  • Patent number: 4675047
    Abstract: The invention concerns novel compounds of the formula I ##STR1## The compounds are herbicides and in further embodiments the invention provides: processes for the preparation of compounds of formula I; intermediates useful in the preparation of compounds of formula I; compositions containing as active ingredient compounds of formula I; and processes for severely damaging or killing unwanted plants by applying to the plants or to the growth medium of the plants an effective amount of a compound of formula I.
    Type: Grant
    Filed: June 16, 1981
    Date of Patent: June 23, 1987
    Inventors: Alexander Serban, Wendy A. Jensen
  • Patent number: 4673746
    Abstract: Novel 1,2-benzisoxazoloxyacetic acids and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretic, uricosuric and antihypertensive agents.
    Type: Grant
    Filed: October 27, 1980
    Date of Patent: June 16, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Gregory M. Shutske, Linda L. Setescak, Richard C. Allen
  • Patent number: 4672067
    Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents CHO, COR.sub.8, CO.sub.2 R.sub.8, CONR.sub.9 R.sub.10, CSNR.sub.9 R.sub.10 or SO.sub.2 NR.sub.9 R.sub.10, whereR.sub.8 represents alkyl, cycloalkyl, aryl or aralkyl,R.sub.9 represents hydrogen or alkyl, andR.sub.10 represents hydrogen or alkyl, cycloalkyl, aryl or aralkyl;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7 each independently represents hydrogen or C.sub.1-3 alkyl;R.sub.5 represents hydrogen, or alkyl, cycloalkyl, alkenyl or aralkyl, orR.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the attached nitrogen atom form a saturated monocyclic 5- to 7-membered ring; andAlk represents C.sub.2-3 alkylene chain optionally substituted by not more than two C.sub.1-3 alkyl groups;and physiologically acceptable salts and solvates thereof.
    Type: Grant
    Filed: June 28, 1984
    Date of Patent: June 9, 1987
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, Keith Mills, Colin F. Webb, Michael D. Dowle, David E. Bays
  • Patent number: 4668278
    Abstract: A compound of the formula: ##STR1## wherein R is a hydrogen atom, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 alkenyloxy group, a C.sub.3 -C.sub.4 alkynyloxy group, a C.sub.1 -C.sub.4 alkylthio group, a dichlorocyclopropylmethoxy group or a methyldichlorocyclopropylmethoxy group, X is a chlorine atom or a bromine atom and Y is a hydrogen atom, a fluorine atom or a chlorine atom, which is useful as a herbicide.
    Type: Grant
    Filed: October 1, 1984
    Date of Patent: May 26, 1987
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Toru Haga, Eiki Nagano, Masayuki Takase, Ryo Sato
  • Patent number: 4666930
    Abstract: Compounds of the formula ##STR1## in which R.sup.1 is alkyl, cycloalkyl, aryl or hydrogen,R.sup.2 is --CO--R.sup.3,R.sup.3 is alkyl, alkenyl or cycloalkyl, or is phenyl which is optionally substituted, or is alkoxy or benzyl, or is phenoxy which is optionally substituted, or is phenoxymethyl, alkylamino, cycloalkylamino or phenylamino, orR.sup.1 and R.sup.2 together are a ##STR2## group, R.sup.4 and R.sup.5 each independently is hydrogen, alkyl, cycloalkenyl or phenylalkenyl, or is phenyl which is optionally substituted by alkyl, halogen and/or alkoxy, or is furyl, orR.sup.4 and R.sup.5 together are alkylene having 4 to 6 carbon atoms,are fungicidally active. Those compounds wherein R.sup.3 is alkylamino, cycloalkylamino or phenylamino, with the exception of the compound in which R.sup.1 is hydrogen and R.sup.6 is phenylamino, are new.
    Type: Grant
    Filed: March 1, 1985
    Date of Patent: May 19, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Salzburg, Manfred Hajek, Gerd Hanssler
  • Patent number: 4667041
    Abstract: A process for the preparation of a 3-hydrazino-1, 2-benzisothiazole 1,1-dioxide of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, halogen, amino, hydroxyl or carboxyl, andR.sup.3 and R.sup.4 each independently is hydrogen, alkyl, cycloalkyl or aryl,comprising reacting a 3-keto-2H,3H-1,2-benzisothiazole 1,1-dioxide of the formula ##STR2## with a hydrazine of the formula ##STR3## in a molar ratio of 1:1 to 1:50, in an inert solvent, at a temperature between C. and C. and for a reaction time of 15 to 40 hours. The products, some of which are known, are fungicidally active and can also be used as intermediates.
    Type: Grant
    Filed: February 28, 1985
    Date of Patent: May 19, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Salzburg, Manfred Hajek, Gerd Hanssler
  • Patent number: 4666911
    Abstract: An analgesic compositon containing as active ingredient an allophanoylpiperazine compound represented by the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group or phenyl group; R.sup.2 and R.sup.3 each represents a hydrogen atom or a lower alkyl group; and R.sup.4 represents a phenyl group or a substituted phenyl group having as substituent a halogen atom or methyl, trifluoromethyl, hydroxyl, methoxy, methylenedioxy, nitro, or carboxyl group; pyridyl group, pyrimidyl group, thiazolyl group, benzyl group, cinnamyl group, cyclohexyl group, a lower alkyl group, a substituted lower alkyl group having chlorine atom or hydroxyl group as substituent; or a lower alkenyl group.
    Type: Grant
    Filed: July 8, 1981
    Date of Patent: May 19, 1987
    Assignee: Taiho Pharmaceutical Company Limited
    Inventors: Hajime Fujimura, Yasuzo Hiramatu, Takahiro Yabuuchi, Masakatu Hisaki, Katsuo Takikawa, Takaji Honna, Hidekazu Miyake, Makoto Kajitani
  • Patent number: 4665087
    Abstract: 1-(Carbamyl, thiocarbamyl, and iminocarbamyl)-indoline derivatives of the formula ##STR1## where each R.sub.1 is independently alkyl, alkoxy, acyloxy, hydroxy, halo or trifluoromethyl, n is 0, 1, 2 or 3, R.sub.2 and R.sub.3 are independently hydroxy, alkoxy, amino or substituted amino, R.sub.4 and R.sub.5 are independently hydrogen, alkyl or substituted alkyl, R.sub.6 is hydrogen, alkyl or substituted alkyl, and Y is O, S or N--R.sub.7 where R.sub.7 is hydrogen, alkyl, cyano or substituted alkyl, and salts thereof, which are useful as antihypertensive and cardioactive agents, methods of preparing the same, and pharmaceutical compositions thereof, are provided.
    Type: Grant
    Filed: September 5, 1985
    Date of Patent: May 12, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Isidoros Vlattas
  • Patent number: 4665066
    Abstract: 7.beta.-[2-(2-Aminothiazol(oxazol)-4-yl)-2-oximinoacetamido]-3-(thiazolium or substituted thiazolium-3-yl)methyl-3-cephem-4-carboxylates and the correspondingly substituted 1-oxadethia and 1-carbadethia 3-cephem compounds are potent antibacterials useful in a therapeutic method for treating bacterial diseases. Also provided are pharmaceutical formulations of these thiazolium-substituted compounds and intermediates useful in the preparation thereof.
    Type: Grant
    Filed: December 24, 1984
    Date of Patent: May 12, 1987
    Assignee: Eli Lilly and Company
    Inventor: John M. Morin, Jr.
  • Patent number: 4661511
    Abstract: Pharmaceutical compositions are provided containing a 2-(hydroxyphenyl)-indole or a 2-(C.sub.2 -C.sub.6 -alkanoxyloxyphenyl) indole and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 27, 1984
    Date of Patent: April 28, 1987
    Assignee: Degussa Aktiengesellschaft
    Inventors: Erwin von Angerer, Helmut Schonenberger
  • Patent number: 4659360
    Abstract: Benzoxazole compounds of the following structural formula modify the growth and development of plants: ##STR1## wherein U is selected from -hydrogen, -halogen, -lower alkyl, -lower alkenyl, -phenylmethyl, -phenyl, -nitro, -hydroxycarbonyl, -phenylcarbonyl, -halophenylcarbonyl, -phenylthio, -phenylsulfoxy, -phenylsulfonyl, and a substituent of the formula--OZin which Z is -aryl or -aryl carring 1 or 2 substituents independently selected from -halogen, -lower alkyl, -lower haloalkyl, -lower alkoxy, -acetamido, and -phenyl;V is selected from -hydrogen, -halogen and -lower alkyl, or U and V taken together are -C.sub.4 H.sub.4 -- joining adjacent ring positions; andW is selected from -hydrogen, -lower alkyl optionally substituted with -alkoxycarbonyl, and an agriculturally acceptable cation.
    Type: Grant
    Filed: November 30, 1984
    Date of Patent: April 21, 1987
    Assignee: FMC Corporation
    Inventors: Jonathan S. Baum, Tsong M. Chen
  • Patent number: 4657914
    Abstract: There are provided ergoline compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methyl group; R.sub.2 is a hydrogen or halogen atom, a methyl or thiomethyl group; R.sub.3 is a hydrogen atom or a methoxy group; R.sub.4 is a hydrocarbon group having from 1 to 4 carbon atoms; n is 1 or 2; each of R.sub.5 and R.sub.6 independently is a hydrogen atom, an alkyl group having from 1 to 3 carbon atoms, or a phenyl or hydroxy or alkoxy group having from 1 to 4 carbon atoms, and X is an oxygen atom or a group of the formula NR.sub.7 wherein R.sub.7 is selected from the group consisting of a hydrogen atom, an alkyl having from 1 to 4 carbon atoms and a phenyl group, or a group of the formula N.dbd.C--R.sub.8 wherein the carbon atom is positioned between the nitrogen atoms in the ring and R.sub.8 is an amino, substituted amino, methyl, phenyl, thiomethyl or mercapto group. The compounds have antihypertensive and antiprolactin activity.
    Type: Grant
    Filed: April 25, 1983
    Date of Patent: April 14, 1987
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Luigi Bernardi, Aldemio Temperilli, Sergio Mantegani, Gabriella Traquandi, Patricia Salvati
  • Patent number: 4656166
    Abstract: The compounds according to the invention correspond to the formula: ##STR1## in which: The COOA group at the 4 position is an acid radical, or an alkaline or alkaline-earth salt, or an amino acid or amine salt, for example triethylamine or ethanolamines, or an easily hydrolyzable or metabolically labile and pharmaceutically acceptable ester radical.X denotes an oxygen atom or a sulfur atomn is zero or 1R.sub.1 and R.sub.2 each denote independently hydrogen or a lower alkyl group, preferably a methyl group, orR.sub.1 and R.sub.2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl nucleus.B is the residue of a primary or secondary amine.
    Type: Grant
    Filed: May 22, 1984
    Date of Patent: April 7, 1987
    Assignee: Sanofi
    Inventors: Ali Salhi, Dominique Olliero
  • Patent number: 4644064
    Abstract: Novel 1,2-benzisoxazoloxyethylamines and intermediates for the preparation thereof are described. The 1,2-benzisoxazoloxyethylamines are useful as diuretic agents.
    Type: Grant
    Filed: October 14, 1983
    Date of Patent: February 17, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4632928
    Abstract: The invention relates to novel pyrazole derivatives with an ergoline skeleton of the general formula I, ##STR1## wherein x . . . y stands for a ##STR2## R is a hydrogen atom or methyl group, R.sub.1 stands for a hydrogen atom, C.sub.1-4 alkyl, carbethoxy or pyridyl-group,R.sub.2 stands for a hydrogen atom, C.sub.1-4 alkyl, allyl, C.sub.2-4 oxoalkyl-, C.sub.2-4 hydroxyalkyl or C.sub.2-4 hydroxyiminoalkyl group,R.sub.3 stands for a hydrogen atom, C.sub.1-4 alkyl, hydroxy or pyridyl group, furthermoreR.sub.2 and R.sub.3 may stand together for a group of general formula (II), ##STR3## wherein Z stands for a methylene, carbonyl, hydroxymethylene or hydroxyiminomethylene group,R.sub.4 stands for a hydrogen atom or one or two C.sub.1-4 alkyl group(s), andn is 1 or 2,and pharmaceutically acceptable salts thereof.Furthermore the invention relates to a process for the preparation of these compounds.The novel compounds are potent PGF.sub.2.alpha. receptor antagonists.
    Type: Grant
    Filed: May 30, 1984
    Date of Patent: December 30, 1986
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Tivadar Rettegi, Erzsebet Mago nee Karacsony, Lajos Toldy, Jozsef Borsy, Ilona Berzetei, Andras Ronai, Aliz Druga, Gyorgy Cseh