Abstract: Compounds of Formula I, and their N-oxides and agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein: X and Y are independently N or CH;Z is O, S(O).sub.n, NR.sup.7, C(.dbd.O), C(.dbd.S), C(.dbd.N--OR.sup.8), CH(OR.sup.9), or CR.sup.10 (R.sup.11);n is 0, 1 or 2; andR.sup.1 -R.sup.11 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.
Type:
Grant
Filed:
December 3, 1996
Date of Patent:
April 14, 1998
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
Thomas Paul Selby, Michael Peter Winters
Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R1, R2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
Type:
Grant
Filed:
March 20, 1997
Date of Patent:
April 14, 1998
Assignee:
Eli Lilly and Company
Inventors:
William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
Abstract: Heterotricyclic derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.
Type:
Grant
Filed:
September 4, 1996
Date of Patent:
April 14, 1998
Assignee:
Fujisawa Pharmaceutical Co., Ltd.
Inventors:
Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
April 14, 1998
Assignee:
Bristol-Myers Squibb Company
Inventors:
Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Richard B. Sulsky, Joseph A. Tino
Abstract: 6-Aryl pyrazolo?3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.
Abstract: 6-Aryl pyrido?2,3-d!pyrimidines and naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating atherosclerosis, restenosis, psoriasis, as well as bacterial infections.
Type:
Grant
Filed:
November 6, 1995
Date of Patent:
March 31, 1998
Inventors:
Clifton John Blankley, Annette Marian Doherty, James Marino Hamby, Robert Lee Panek, Mel Conrad Schroeder, Howard Daniel Hollis Showalter, Cleo Connolly
Abstract: Novel cephem derivatives represented by the general formula ##STR1## wherein Ar is an optionally substituted lipophilic phenyl, naphthyl, benzthiazolyl or pyridyl group; R.sup.1 represents a group of the formula ##STR2## in which R.sup.8 and R.sup.9 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl or (C.sub.1 -C.sub.6)alkoxycarbonyl, said C.sub.1 -C.sub.6 alkyl group being optionally substituted by 1-5 hydroxy or C.sub.1 -C.sub.6 alkoxy groups; m is either 0 or 1; A is a C.sub.2 -C.sub.10 alkyl group optionally substituted by 1-5 hydroxy groups; and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.
Type:
Grant
Filed:
December 5, 1996
Date of Patent:
March 31, 1998
Assignee:
Bristol-Myers Squibb Company
Inventors:
Choung U. Kim, Muzammil M. Mansuri, Peter F. Misco, John A. Wichtowski
Abstract: A substituted cyclic amine compound represented by the following general formula (1) ##STR1## wherein each of R.sup.1 to R.sup.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or the like, A represents a carbonyl group or a sulfonyl group, B represents a methine moiety or a nitrogen atom, D represents a methine moiety, a nitrogen atom or .dbd.N(.fwdarw.O)-- and n is an integer of 2 to 3; and synthetic methods thereof. The inventive compound is useful in preventing and treating circulatory organ-related diseases such as hypertension, ischemic heart disease, cerebrovascular disease, peripheral circulatory disease and the like.
Abstract: Novel nitriles are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-Phthalimido-3-(3,4-dimethoxyphenyl)propionitrile.
Abstract: Novel amides are inhibitors of TNF.alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-phthalimido-3-(3-cyclopentyloxy-4-methoxyphenyl)propionamide.
Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are as set forth below.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
March 17, 1998
Assignee:
Roussel Uclaf
Inventors:
Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert, Christophe Dini
Abstract: The salts are prepared by reacting a benzhydrylamine of the formula I (or a salt thereof) with clavulanic acid (or a salt thereof) in solvent, and isolating the resulting salt. In formula I, each of R.sup.1 and R.sup.2 is hydrogen (preferred) or an acceptable substituent. ##STR1## The clavulanic acid salts can be used in pharmaceutical formulations together with a pharmaceutically acceptable carrier, and, preferably, a beta-lactam antibiotic.
Abstract: This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) ##STR1## (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R.sup.1 and R.sup.2 : these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group,A: a single bond; a group represented by the formula--NHCO--(CR.sup.3 R.sup.4).sub.n --,n: 0 or an integer of from 1 to 3,R.sup.3 and R.sup.4 : these may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group (provided that R.sup.3 and R.sup.
Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, halogen, an aliphatic radical or an aromatic radical, X is O, S or optionally substituted imino, Y is a bond or an optionally substituted bivalent hydrocarbon radical and Z is optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and their use as pesticides, in particular as insecticides, acaricides and fungicides.
Type:
Grant
Filed:
September 12, 1994
Date of Patent:
March 3, 1998
Assignee:
Hoechst Schering AgrEvo GmbH
Inventors:
Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
Abstract: A process of synthesizing HBIW using a mineral acid, such as perchloric acid, as the acid catalyst is disclosed. According to the process, glyoxal, adjusted to a pH from 4 to 7, and benzylamine are reacted in the presence of the mineral acid for sufficient time to form HBIW. The resulting HBIW is then isolated according to conventional separation techniques.
Type:
Grant
Filed:
June 22, 1995
Date of Patent:
March 3, 1998
Assignee:
Thiokol Corporation
Inventors:
Louis F. Cannizzo, William W. Edwards, Robert B. Wardle, Thomas K. Highsmith
Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
Type:
Grant
Filed:
October 18, 1995
Date of Patent:
February 24, 1998
Assignee:
Novo Nordisk A/S
Inventors:
Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
Abstract: Compounds represented by the Formula I: ##STR1## wherein: R.sup.1 is hydrogen or lower alkyl;R.sup.2 is heteroaryl; andR.sup.3 and R.sup.4 are independently hydrogen or lower alkyl;and the pharmaceutically acceptable salts thereof, are useful as chemotherapeutic agents.
Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.
Type:
Grant
Filed:
May 31, 1996
Date of Patent:
February 17, 1998
Assignee:
American Cyanamid Company
Inventors:
Jay D. Albright, Efren G. Delos Santos, Xuemei Du, Marvin F. Reich
Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sup.25)(R.sup.48), are disclosed.Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
Type:
Grant
Filed:
March 24, 1995
Date of Patent:
February 17, 1998
Assignee:
Schering Corporation
Inventors:
W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski