Additional Hetero Ring Which Is Unsaturated Patents (Class 544/324)
  • Publication number: 20010011094
    Abstract: This invention concerns the use of the compounds of formula 1
    Type: Application
    Filed: December 27, 2000
    Publication date: August 2, 2001
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
  • Patent number: 6254669
    Abstract: A compound of the Formula (1) and salts thereof: wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially ink jet printing inks, for reducing color bleed between adjacent printed regions. Also claimed are inks containing a compound of the Formula (1), a method of ink jet printing using the inks, a substrate printed with the ink and an ink jet printer cartridge containing the ink.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: July 3, 2001
    Assignee: Zeneca Limited
    Inventors: Aidan Joseph Lavery, Prahalad Manibhai Mistry, Ronald Wynford Kenyon
  • Patent number: 6251900
    Abstract: Heterocyclic compounds in which s-triazine or pyrimidine is substituted with benzimidazole and morpholine and which are represented by the Formula I or phermaceutically acceptable acid addition salts thereof: wherein X and Y respectively represent nitrogen atom or one of them represents nitrogen atom and the other represents C—R7 wherein R7 represents hydrogen or halogen atom; R1, R2, R4, R5 and R6 represent hydrogen atom or C1-C6 alkyl; R3 represents morpholino, piperidino, piperazinyl, thiomorpholino, benzimidazolyl, cyano or the like.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: June 26, 2001
    Assignee: Zenyaku Kogyo Kabushiki Kaisha
    Inventors: Seiichiro Kawashima, Toshiyuki Matsuno, Shinichi Yaguchi, Tetsuo Watanabe, Masahiro Inaba
  • Patent number: 6218537
    Abstract: 1,4,5,-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: April 17, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry Leroy Adams, Timothy Francis Gallagher, Joseph Sisko, Irennegbe Kelly Osifo, Jeffrey Charles Boehm
  • Patent number: 6187781
    Abstract: A 4-tetrahydropyridylpyrimidine compound represented by formula (I): wherein Ar represents a phenyl group substituted with 1 to 3 substituents selected from a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, and a trifluoromethyl group, a phenyl group, a thienyl group or a furanyl group; R1 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms; R2 represents an alkyl group having 1 to 5 carbon atoms, a cycloalkylalkyl group having 4 to 7 carbon atoms, an alkenyl group having 2 to 5 carbon atoms or an alkynyl group having 2 to 5 carbon atoms; and X1, X2, and X3, which may be the same or different, each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, an alkylthio group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or
    Type: Grant
    Filed: September 21, 1999
    Date of Patent: February 13, 2001
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Atsuro Nakazato, Toshihito Kumagai, Taketoshi Okubo, Izumi Aibe, Hideo Tanaka, Shigeyuki Chaki, Shigeru Okuyama, Kazuyuki Tomisawa
  • Patent number: 6174901
    Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: January 16, 2001
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
  • Patent number: 6172005
    Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation and Q, W, X, Y, Z, and R1 through R8 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: September 1, 1999
    Date of Patent: January 9, 2001
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas P. Selby
  • Patent number: 6172066
    Abstract: This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: January 9, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Dhanapalan Nagarathnam, Wai C. Wong, Shou Wu Miao, Michael A. Patane, Charles Gluchowski
  • Patent number: 6159982
    Abstract: The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl or C.sub.3-6 alkenediyl; R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 and R.sup.3 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; or R.sup.2 and R.sup.3 may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R.sup.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: December 12, 2000
    Assignee: Janssen Pharmaceutica N. V.
    Inventors: Jean-Paul Rene Marie Andre Bosmans, Christopher John Love, Guy Rosalia Eugene Van Lommen
  • Patent number: 6136971
    Abstract: The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M.sub.1 XCH.sub.2 CH.sub.2 YR.sub.5 and removing the protecting group, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, Z, X, Y, M, M.sub.1 and W are defined herein.
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: October 24, 2000
    Assignee: Roche Colorado Corporation
    Inventors: Peter J. Harrington, Hiralal N. Khatri, Bradley S. Dehoff
  • Patent number: 5990311
    Abstract: The present invention relates to a process for preparation of 5,6-dimethyl-2-(4-fluorophenyl-amino)-4-(1-methyl-1,2,3,4-tetrahydroisoqui nolin-2-yl)pyrimidine represented by the following formula (I), ##STR1## and its acid addition salts by reacting a pyrimidine derivative represented by the formula (II-A), ##STR2## in which Hal represents a halogen, with 1-methyl-1,2,3,4-tetrahydroisoquinoline represented by the formula (III), ##STR3##
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: November 23, 1999
    Assignee: Uhan Corporation
    Inventors: You Wha Hong, Young Nam Lee, Hong Bae Kim
  • Patent number: 5985884
    Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: November 16, 1999
    Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor Inc.
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti, Sarma K. S. Pakala
  • Patent number: 5977367
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: November 2, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5972947
    Abstract: The present invention concerns new oxazolidinone derivatives, processes for their production as well as pharmaceutical agents containing these substances. The present invention concerns compounds of the general formula I ##STR1## in which the symbols have the meanings as listed in the claims.
    Type: Grant
    Filed: December 31, 1998
    Date of Patent: October 26, 1999
    Assignee: Roche Diagnostics GmbH
    Inventors: Christos Tsaklakidis, Wolfgang Schafer, Liesel Dorge, Walter-Gunar Friebe, Angelika Esswein
  • Patent number: 5939424
    Abstract: The invention relates to 4-Amino-2-ureidopyrimidine-5-carboxamides of the formula I ##STR1## in which R.sup.1 is H or (C.sub.1 -C.sub.8)-alkyl, where one or more H can be replaced by F; R.sup.2 is selected from the group consisting of F, Cl, Br, H, -O-(C.sub.1 -C.sub.8)-alkyl, and -S-(C.sub.1 -C.sub.8)-alkyl, where the alkyl groups have one or more H replaced by F; R.sup.3 is -O-(C.sub.1 -C.sub.8)-alkyl or -S-(C.sub.1 -C.sub.8)-alkyl, where the alkyl groups have one or more H replaced by F; or R.sup.2 and R.sup.3 together form -O-(C.sub.1 -C.sub.5)-alkylene-O-, where the alkylene portion has one or more H replaced by F; and their physiologically tolerable salts. The invention further provides processes for preparing the compounds of formula I. The compounds are suitable for the treatment of disorders of lipid metabolism.
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: August 17, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans Georg Boger, Axel Hoffmann, Gerhard Jahne, Norbert Krass, Hans-Ludwig Schafer
  • Patent number: 5936085
    Abstract: Disclosed and claimed is a process for the preparation of a carbamate (IV)Ar--O--CO--NR--B (IV)by reaction of a saltM.sup..sym. .crclbar.NR--B (II-S)with a diaryl carbonate(ArO).sub.2 CO (III).The carbamate can be reacted, without any necessity of intermediate isolation, with a sulfonamide A--SO.sub.2 NH.sub.2 (V) to give a sulfonylurea (I) or salts thereofA--SO.sub.2 --NH--CO--NR--B (I).And thus, disclosed and claimed too is a process for the preparation of sulfonylurea (I) by (i) contacting a salt (II-S) with a diaryl carbonate (III) to form a carbamate (IV), and (ii) contacting carbamate (IV) from step (i) with or without intermediate isolation, with a sulfonamide (V). These processes avoid the use of alkali metal hydrides as a base. And, these processes can additionally include the preparation of salt (II-S) from a compound H--NR--B (II) and base M.sup..sym. Base.sup..crclbar..
    Type: Grant
    Filed: July 11, 1996
    Date of Patent: August 10, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Harald Knorr, Klemens Minn, Jan Vermehren
  • Patent number: 5922645
    Abstract: Compounds of the formula (I) and salts thereof ##STR1## in which R.sup.1 to R.sup.6, W, X, Y and Z are defined as in claim 1, have herbicidal or plant growth-regulatory properties.They can be prepared by processes analogous to known processes (cf. claim 5), in some cases via novel intermediate products (cf.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: July 13, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5889012
    Abstract: Substituted cycloalkylamino and cycloalkoxy heterocycles, processes for preparing them and their use as pesticides The invention relates to (I) ##STR1## in which R.sup.1 to R.sup.5, A, X, E, U, p and n are as defined in claim 1, to processes for their preparation and their use as pesticides, such as insecticides, acaricides and fungicides.
    Type: Grant
    Filed: October 16, 1995
    Date of Patent: March 30, 1999
    Assignee: Hoechst-Schering AgrEvo GmbH
    Inventors: Martin Markl, Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin, Adolf Linkies, Dieter Bernd Reuschling
  • Patent number: 5886176
    Abstract: The invention relates to a novel process for preparing herbicidal sulphonylurea salts of the formula (I) ##STR1## in which M.sup.+ represents an alkali metal ion or an alkaline earth metal ion equivalent,Z represents N, CH or C-halogen,R.sup.1 represents in each case optionally substituted aryl, aralkyl or heteroaryl,(where R.sup.2, X and Y have the meanings given in the description).
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: March 23, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventor: Klaus-Helmut Muller
  • Patent number: 5869428
    Abstract: A pyridonesulfonylurea compound of the formula (I) or its salt: ##STR1## wherein Q is ##STR2## for use as a herbicide, wherein the variables are hereinbelow defined.
    Type: Grant
    Filed: March 4, 1996
    Date of Patent: February 9, 1999
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Yasuo Morishima, Shigeo Murai, Yoshiyuki Aoyama, Hiroshi Sasaki, Hiroshi Kikugawa, Soichiro Nagayama, Makiko Mitani
  • Patent number: 5866583
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is bromine, lower-alkoxy or hydroxy, R.sup.3 is hydrogen, lower-alkyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclyl-lower-alkyl or cyano, R.sup.4 and R.sup.5 each independently are hydrogen, lower-alkyl, lower-alkoxy, halogen, hydroxy, amino, di(lower alkyl)amino, cyano or nitro and Q is ethynylene or vinylene, or pharmaceutically usable salts thereof, the use of these compounds and their salts as therapeutically active substances; medicaments based on these substances and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula I and their pharmaceutically acceptable salts and intermediates for their manufacture.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: February 2, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Guerry, Henri Stalder, Pierre-Charles Wyss
  • Patent number: 5863924
    Abstract: The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.
    Type: Grant
    Filed: May 20, 1997
    Date of Patent: January 26, 1999
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
  • Patent number: 5854179
    Abstract: Sulfur-substituted phenylsulfonylureas; processes for their preparation and their use as herbicides and plant growth regulatorsCompounds of the formula (I) and salts thereof ##STR1## in which R*, R.sup.1, R.sup.2, R.sup.3, X, Y, Z, W, n and m are defined as in claim 1, and specifically R* is a formyl equivalent of the formula CHO, --CH.dbd.NR or CH(X.sup.1 R')(X.sup.2 R"), are suitable as herbicides and plant growth regulators. They are prepared analogously to known methods, in some cases using novel intermediate products of the formula (XVII) ##STR2## in which U*.dbd.NH.sub.2, Cl or (substituted) amino.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: December 29, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5852019
    Abstract: The present invention provides a novel compound which is represented by formula (I): ##STR1## wherein preferable examples of R.sup.1 to R.sup.6 are as follows; R.sup.1 and R.sup.2 are each an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a hydrogen atom, a halogen atom or an alkoxyl group; R.sup.3 is a hydrogen atom; R.sup.4 is a methyl group; R.sup.5 is a hydrogen atom or an alkyl group; and R.sup.6 is a group of the formula: ##STR2## wherein Z is a phenyl group; and has an antitumor effect.
    Type: Grant
    Filed: February 4, 1998
    Date of Patent: December 22, 1998
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Akio Ejima, Masamichi Sugimori, Ikuo Mitsui
  • Patent number: 5849666
    Abstract: N-substituted hydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulatorsCompounds of the formula (I) or salts thereof ##STR1## in which R.sup.1 to R.sup.6, W, Q, X, Y and Z are defined as in formula (I) as claimed in claim 1, are suitable as herbicides and plant growth regulators.The compounds (I) are prepared by processes analogous to known processes (cf.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: December 15, 1998
    Assignee: Hoechst Schering Agrevo GmbH
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5792765
    Abstract: The present invention relates to new substituted oxazolidinones of the general formula (1) ##STR1## in which the substituents have the meaning indicated in the description, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
    Type: Grant
    Filed: February 3, 1997
    Date of Patent: August 11, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Riedl, Dieter Habich, Andreas Stolle, Martin Ruppelt, Stephan Bartel, Walter Guarnieri, Rainer Endermann, Hein-Peter Kroll
  • Patent number: 5783576
    Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: July 21, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
  • Patent number: 5780473
    Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin.
    Type: Grant
    Filed: July 25, 1996
    Date of Patent: July 14, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
  • Patent number: 5773446
    Abstract: Compounds of formula I ##STR1## wherein either R.sup.1 signifies straight-chain C.sub.5-10 -alkyl, branched C.sub.3-5 -alkyl, C.sub.3-6 -cycloalkyl or C.sub.3-5 .omega.-carboxyalkyl and R.sup.2 and R.sup.3 signify C.sub.1-5 -alkyl; orR.sup.1 signifies hydrogen, R.sup.2 signifies C.sub.3-5 .omega.-carboxyalkyl and R.sup.3 signifies C.sub.1-5 -alkyl;or their pharmaceutically acceptable acid addition salts have antibiotic properties and can be used in the control or prevention of infectious diseases.
    Type: Grant
    Filed: December 2, 1996
    Date of Patent: June 30, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Raffaello Masciadri
  • Patent number: 5763450
    Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is lower alkoxy, R.sup.2 is bromine or lower alkoxy, and R.sup.3 is aryl, heteroaryl or a group --Q--R.sup.30, wherein Q is ethylene, vinylene or ethynylene and R.sup.30 is aryl, heteroaryl, lower alkoxycarbonyl or carbamoyl;hydrolyzable esters of carboxylic acids of formula I; and pharmaceutically acceptable salts of these compounds are useful for treating infectious diseases.
    Type: Grant
    Filed: May 21, 1997
    Date of Patent: June 9, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Guerry, Synese Jolidon, Raffaello Masciadri, Henri Stalder, Rudolf Then
  • Patent number: 5760038
    Abstract: Compounds of the formula ##STR1## in which the symbols are as defined herein, inhibit the activity of endothelin.
    Type: Grant
    Filed: February 6, 1995
    Date of Patent: June 2, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
  • Patent number: 5747421
    Abstract: Formylaminophenylsulfonylureas; processes for their preparation, and their use as herbicides and plant growth regulatorsCompounds of the formula (I) ##STR1## in which R.sup.1 is H, a substituted or unsubstituted hydrocarbon radical or an unsubstituted or substituted heterocyclic radical,R.sup.2 is H, (C.sub.1 -C.sub.6)-alkyl or (C.sub.1 -C.sub.6)-alkoxy,R.sup.3 is halogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy, (C.sub.1 -C.sub.6)-haloalkyl, (C.sub.1 -C.sub.6)-haloalkoxy, NO.sub.2, CN, NH.sub.2, (C.sub.1 -C.sub.4) -mono- or dialkylamino, each independently of other radicals R.sup.3 if n is 2 or 3,n is 0, 1, 2 or 3,W is an oxygen atom or a sulfur atom,X and Y independently of one another are halogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy or (C.sub.1 -C.sub.6)-alkylthio, each of the three last-mentioned radicals being unsubstituted or substituted by one or more radicals selected from the group consisting of halogen, (C.sub.1 -C.sub.4)-alkoxy and (C.sub.1 -C.sub.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: May 5, 1998
    Assignee: Hoechst Schering Agrevo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5747423
    Abstract: The novel 6-thienyl pyridines and 4-thienyl pyrimidines of formula I: ##STR1## (A, R.sub.1 to R.sub.5 and Z are defined in the specification) show selective herbicidal activity.The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: May 5, 1998
    Assignee: American Cyanamid Company
    Inventors: Stefan Scheiblich, Thomas Maier, Helmut Siegfried Baltruschat, Joseph Luke Pont
  • Patent number: 5739333
    Abstract: Novel sulfonamide derivatives of the formula ?I!: ##STR1## wherein Ring A and Ring B are substituted or unsubstituted monocyclic, bicyclic or tricyclic hydrocarbon, or substituted or unsubstituted heterocyclic group, Q is single bond, --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is --0--, --S-- or --NH--, Alk is lower alkylene or alkenylene, Z is --O-- or --NH --, R is substituted or unsubstituted aromatic heterocyclic or aryl, R.sup.1 is H, substituted or unsubstituted amino, substituted or unsubstituted lower alkyl, alkenyl, alkynyl, substituted or unsubstituted lower alkylthio, or alkoxy, or substituted or unsubstituted heterocyclic or aryl, or pharmaceutically acceptable salts thereof, which are useful in the prophylaxis or treatment of disorders associated with endothelin activities such as hypertension, pulmonary hypertension, renal hypertension, Raynaud disease, bronchial asthma, gastric ulcer, chronic heart failure, etc.
    Type: Grant
    Filed: May 9, 1996
    Date of Patent: April 14, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
  • Patent number: 5723409
    Abstract: The compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, W, X, Y and Z are as defined in claim 1 are suitable for controlling harmful plants in crops.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: March 3, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5723473
    Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: March 3, 1998
    Assignee: Zeneca Limited
    Inventor: Brian Leslie Pilkington
  • Patent number: 5712285
    Abstract: A class of pyrrolo?2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or heteroaryl-substituted divalent monocyclic radical, are ligands for dopamine receptorsubtypes within the body, in particular the D.sub.4 subtype, and are accordingly of use in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia and depression.
    Type: Grant
    Filed: April 3, 1996
    Date of Patent: January 27, 1998
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Mark Peter Ridgill
  • Patent number: 5708171
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## having antagonist properties to histamine H.sub.3 -receptors.
    Type: Grant
    Filed: June 14, 1996
    Date of Patent: January 13, 1998
    Assignees: Institut National de la Sante et de la Recherche Medicale, Societe Civile Bioprojet
    Inventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Charon Robin Ganellin, Abdellatif Fkyerat, Wasyl Tertiuk, Walter Schunack, Ralph Lipp, Holger Stark, Katja Purand
  • Patent number: 5688798
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each individually are lower-alkyl or amino,A is ##STR2## B is hydrogen in A.sup.4, A.sup.5 and A.sup.6 ; ##STR3## in A.sup.1 -A.sup.6 ; lower-alkoxy in A.sup.4 -A.sup.6 ;and lower-alkyl, styryl, phenylethynyl or benzoyloxy-lower-alkyl in A.sup.1 and A.sup.2 ;n is 0, 1 or 2;m, p are, independently 0, 1 andR.sup.3, R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halogen, lower-alkyl, trifluoromethyl, lower-alkoxy or nitro,and pharmaceutically acceptable acid addition salts thereof. These compounds are useful in the control or prevention of illnesses which are caused by disorders of the dopamine system, in particular psychotic illnesses such as schizophrenia.
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: November 18, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thierry Godel, Claus Riemer
  • Patent number: 5683964
    Abstract: An N-(substituted amino)imide derivative represented by the formula (I) is a novel compound which can be utilized as an effective ingredient of herbicidal compositions. ##STR1## wherein, R.sup.1 is hydrogen atom, C.sub.1 -C.sub.4 alkyl group, C.sub.7 -C.sub.9 aralkyl group, C.sub.1 -C.sub.4 haloalkyl group, (C.sub.1 -C.sub.4 alkyl)carbonyl group or (C.sub.1 -C.sub.4 alkyl)sulfonyl group;A represents a structure selected from the group consisting of the following formulas (A-1), (A-2), (A-3), (A-4) and (A-5) ##STR2## wherein R.sup.2 and R.sup.3 in the formula (A-1) are independently hydrogen atom or C.sub.1 -C.sub.4 alkyl group, but not R.sup.2 =R.sup.3 =H, R.sup.4 in the formula (A-4) is halogen atom, C.sub.1 -C.sub.4 alkyl group and/or nitro group, m is an integer of 0-4, the substituents of m not less than 2 being same or different;X.sup.1 and X.sup.2 are independently hydrogen atom, halogen atom, C.sub.1 -C.sub.4 alkyl group, C.sub.1 -C.sub.4 alkoxy group, C.sub.1 -C.sub.4 alkylthio group, C.sub.1 -C.sub.
    Type: Grant
    Filed: July 20, 1995
    Date of Patent: November 4, 1997
    Assignee: Kureha Kagaku Kogyo K.K.
    Inventors: Yoichi Kanda, Hideo Arabori, Masato Arahira, Tsutomu Sato
  • Patent number: 5665724
    Abstract: This invention relates to substituted thiazole derivatives of the following general formula, the substituent groups of which are as defined in the specification herein: ##STR1## These compounds are useful as inhibitors of platelet aggregation and inhibitors of adhesion molecules and may be provided in pharmaceutical compositions and in methods of treating reperfusion thrombosis injury in patients. Also included are novel intermediates for preparing the compounds of the invention.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: September 9, 1997
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Pauline J. Sanfilippo, Maud Urbanski
  • Patent number: 5658854
    Abstract: Acylated aminophenylureas, preparation and use as herbicides and plant growth regulatorsThe compounds of the formula I or their salts ##STR1## in which G is a radical G1, G2 or G3 ##STR2## R.sup.1 is H or alkyl, R.sup.2 is COOH, CSOH or a derivative of the carboxyl or thiocarboxyl group, of 1 to 20 carbon atoms, or acyl of the type CO-R.degree. of 1-12 carbon atoms, or an imino, hydrazone or oxime derivative of the group CO-R.degree., and R.degree. , R.sup.3a, R.sup.4a, R.sup.3b, R.sup.4b, W, X, Y and Z are as defined in claim 1, are suitable as selective herbicides and plant growth regulators in crops.The preparation is carried out in analogy to known processes (see claim 5) by way of intermediates, some of which are new, from the group consisting of benzene-sulfonamides (II), benzenesulfonyl isocyanates (IV) and benzesulfonyl chlorides (VI) and heterocyclically substituted carbamates (III), amines (V) and/or (thio)-isocyanates (XIX).
    Type: Grant
    Filed: June 30, 1994
    Date of Patent: August 19, 1997
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5658903
    Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
    Type: Grant
    Filed: June 3, 1996
    Date of Patent: August 19, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry Leroy Adams, Timothy Francis Gallagher, Joseph Sisko, Zhi-Qiang Peng, Irennegbe Kelly Osifo, Jeffrey Charles Boehm
  • Patent number: 5648315
    Abstract: Compounds of the formula (I) and their salts as defined below, ##STR1## in which R.sup.1 is CO--Q--R.sup.8, where R.sup.8 .dbd.H or RR.sup.2 and R.sup.3 are H or (C.sub.1 -C.sub.4)alkyl,R.sup.4 is H, R, RO, OH, RCO, RSO.sub.2, PhSO.sub.2R.sup.5 is RSO.sub.2, PhSO.sub.2, PhCO, RNHSO.sub.2, R.sub.2 NSO.sub.2, RCO, CHO, COCOR', CW--T--R.sup.9, CW--NR.sup.10 R.sup.11, CW--N(R.sup.12).sub.2 orR.sup.4 and R.sup.5 together are the chain (CH.sub.2).sub.m B or --B.sup.1 --(CH.sub.2).sub.m1 B-- where B.dbd.SO.sub.2, CO; m=3, 4; m.sup.1 =2, 3;T and W.dbd.O, S; Q.dbd.O, S, NR.sup.13 where R.sup.13 .dbd.H, R;R.sup.6 .dbd.H, R, RO, RCO, ROCO, Hal, NO.sub.2, CN;R.sup.7 .dbd.H, CH.sub.3 ; R.sup.9 .dbd.R; R.sup.10, R.sup.11 .dbd.H, R; N(R.sup.12).sub.2 =heterocycleA=pyrimidinyl and triazinyl radical or an analog thereof,where R=(substituted) aliphatic hydrocarbon radical, are suitable as selective herbicides. They are prepared by analogous processes via sulfonamides.
    Type: Grant
    Filed: October 13, 1994
    Date of Patent: July 15, 1997
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Klaus Lorenz, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5616537
    Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## (wherein R is a hydroxyl group, R.sup.3 or R.sup.4 is an alkoxy group, W is an oxygen atom, Yn is a hydrogen atom, Z is a methine group, and A is a 5- or 6-membered heterocyclic ring which may be substituted, and a herbicide, are presented. When used for paddy field treatment, upland soil treatment and foliage treatment, the condensed heterocyclic derivative of the present invention exhibits excellent herbicidal activities against gramineous and non-gramineous weeds without adversely affecting crop plants.
    Type: Grant
    Filed: March 1, 1994
    Date of Patent: April 1, 1997
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Sumio Yokota, Masafumi Matsuzawa, Nobuyuki Ohba, Toshihiro Nagata, Shigehiko Tachikawa, Takeshige Miyazawa, Katsutada Yanagisawa
  • Patent number: 5612287
    Abstract: This invention is to provide an N-(substituted amino)pyrrole derivative represented by the formula (I): which is used as an effective ingredient of herbicidal compositions: ##STR1## wherein R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is independently hydrogen atom halogen atom, C.sub.1 -C.sub.4 alkyl group, (C.sub.1 -C.sub.4 alkyl)carbonyl group, (C.sub.3 -C.sub.6 cycloalkyl)carbonyl group, (C.sub.1 -C.sub.4 haloalkyl)carbonyl group, (C.sub.3 -C.sub.5 alkenyl)carbonyl group, benzoyl group which may be substituted with 1-3 halogen atoms and/or C.sub.1 -C.sub.4 alkyl groups, N,N-[(di-C.sub.1 -C.sub.4 alkyl)amino]carbonyl group, (C.sub.1 -C.sub.4 alkoxy)carbonyl group, etc., X.sup.1 and X.sup.2 are independently hydrogen atom, halogen atom, C.sub.1 -C.sub.4 alkyl group, C.sub.1 -C.sub.4 alkoxy group, etc., and Z is nitrogen atom or CH.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Kureha Kagaku Kogyo K.K.
    Inventors: Yoichi Kanda, Hideo Arabori, Masato Arahira, Tsutomu Sato
  • Patent number: 5585381
    Abstract: A pyrimidine derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, or --NHR.sup.11 group; R.sup.2 is a hydrogen or halogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, --(CH.sub.2).sub.m C.sub.6 H.sub.5, --NH.sub.2, --NHR.sup.12, --NH(CH.sub.2).sub.n C.sub.6 H.sub.5, --NH(CH.sub.2).sub.p C.sub.6 H.sub.4 --OR.sup.13, --N(R.sup.14)(CH.sub.2).sub.q C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.15, --NHC(.dbd.O)(CH.sub.2).sub.r C.sub.6 H.sub.5, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --OR.sup.16, or --O(CH.sub.2).sub.s C.sub.6 H.sub.5 group; R.sup.3 is --COOH, --COOR.sup.17, hydroxyl, --OR.sup.18, --NH.sub.2, --N(R.sup.19).sub.2, --NHR.sup.20, azole, or sulfonic acid group; R.sup.11 is alkyl of 1 to 6 carbon atoms or haloalkyl of 1 to 6 carbon atoms; R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, and R.sup.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: December 17, 1996
    Assignee: Kureha Chemical Industry Co., Ltd.
    Inventors: Mikiro Yanaka, Fuyuhiko Nishijima, Hiroyuki Enari, Michihito Ise
  • Patent number: 5585328
    Abstract: This invention relates to certain herbicidal pyrrolesulfonylureas, compositions thereof and a method for their use as herbicides or plant growth regulants.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: December 17, 1996
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: William T. Zimmerman, Bruce A. Lockett, John Cuomo
  • Patent number: 5559113
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having antagonist properties to histamine H.sub.3 -receptors.
    Type: Grant
    Filed: January 28, 1994
    Date of Patent: September 24, 1996
    Assignees: Institut National de la Sante et de la Recherche Medicale, Societe Civile Bioprojet
    Inventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Charon R. Ganellin, Abdellatif Fkyerat, Wasyl Tertiuk, Walter Schunack, Ralph Lipp, Holger Stark, Katja Purand
  • Patent number: RE37303
    Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as in the specification having antagonist properties to histamine H3-receptors.
    Type: Grant
    Filed: April 6, 2000
    Date of Patent: July 31, 2001
    Assignees: Institut National del la Sante et de la Recherche Medicale, Societe Civile Bioprojet
    Inventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Charon R. Ganellin, Abdellatif Fkyerat, Wasyl Tertiuk, Walter Schunack, Ralph Lipp, Holger Stark, Katja Purand