Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/233)
  • Patent number: 4988711
    Abstract: Inhibiting HMG-CoA reductase, as in treating hyperlipopproteinaemia, lipoproteinaemia and arteriosclerosis, with the new N-substituted N-amino-pyrroles of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is an aryl or heteroaryl radical,R.sup.3 is a hydrogen or an organic radical,R.sup.4 and R.sup.5 each independently is hydrogen or an organic radical or, together, they complete a heterocylic ring,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.10 is hydrogen or alkyl, and R.sup.11 is hydrogen, an organic radical or a cation.
    Type: Grant
    Filed: April 12, 1989
    Date of Patent: January 29, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Walter Hubsch, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
  • Patent number: 4987146
    Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.
    Type: Grant
    Filed: July 14, 1989
    Date of Patent: January 22, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
  • Patent number: 4968709
    Abstract: Fungicidal substituted acrylic acid esters of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each stand for hydrogen, alkyl, alkenyl or for in each case optionally substituted aralkyl, aralkenyl, aryl or heteroaryl,R.sup.3 stands for alkyl or for optionally substituted aralkyl,R.sup.4 stands for dialkylamino or for a radical --Z--R.sup.5,X stands for oxygen or sulphur andY stands for oxygen, sulphur or for a radical ##STR2## wherein R.sup.5 stands for alkyl or for optionally substituted aralkyl,R.sup.6 stands for hydrogen, alkyl, alkanoyl or for in each case optionally substituted aralkyl or aryl andZ stands for oxygen or sulphur.Some intermediates are also new.
    Type: Grant
    Filed: March 2, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerd Kleefeld, Alexander Klausener, Wolfgang Kramer, Wilhelm Brandes, Stefan Dutzmann, Gerd Hanssler
  • Patent number: 4962117
    Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, antiallergic, anti-inflammatory, and cytoprotective agents.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: October 9, 1990
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Joseph G. Atkinson
  • Patent number: 4959390
    Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.
    Type: Grant
    Filed: December 15, 1988
    Date of Patent: September 25, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
  • Patent number: 4948898
    Abstract: The manufacture of 1-sulpho-2-oxazetidine derivatives of the formula ##STR1## in which Het is an optionally amino-substituted, 5- or 6-membered, aromatic heterocycle containing 1 or 2 nitrogen atoms and optionally also an oxygen or sulphur atom, R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl-lower-alkoxycarbonyl-lower alkyl, nitrophenyl-lower-alkoxycarbonyl-lower alkyl or carboxy-lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, lower alkanoyloxy-lower alkyl, lower alkoxycarbonyl-lower alkenyl, hydroxyiminomethyl, lower alkoxyiminomethyl, carbamoyl, carbamoyl-lower alkenyl or carbamoyloxy-lower alkyl, the group .dbd.NOR.sup.
    Type: Grant
    Filed: February 28, 1989
    Date of Patent: August 14, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Werner Hofheinz, Christian N. Hubschwerlen, Hans P. Isenring
  • Patent number: 4931471
    Abstract: Derivatives with amide function obtained by reaction between derivatives of linear, branched or cyclic amines having an amino acid or peptidic structure and paramethoxycinnamic acid or urocanic acid. Application of said compounds as specific solar filter, absorbing about 310 nm and avoiding erythematous phenomena during exposures to the sun and as active principles of dermo-pharmaceutical and cosmetological preparations.
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: June 5, 1990
    Assignee: Universite Louis Pasteur
    Inventors: Louis Jung, Dominique Robert
  • Patent number: 4914112
    Abstract: A compound of the formula: ##STR1## wherein A is the group of the formula:Ar.sup.1 --D--Ar.sup.2 --wherein Ar.sup.1 is a phenyl or thienyl group which may be optionally substituted with at least one of the same or different halogen atom; Ar.sup.2 is a phenylene or thienylene group which may be optionally substituted with at least one of the same or different halogen atom; D is a divalent radical selected from the group consisting of >C.dbd.N--OR.sup.4 [wherein R.sup.4 is a hydrogen atom or lower alkyl group], >C.dbd.O, ##STR2## >CHOH, >NH radical, or single bond, ##STR3## wherein R.sup.5 is a lower alkoxy or a phenyl group which may be optionally substituted with at least one of the same or different halogen atom; E is a methine group or a nitrogen atom; F is a vinylene group or an oxygen atom, ##STR4## wherein R.sup.6 is a lower alkoxy group; R.sup.7 is a lower alkyl group; R.sup.
    Type: Grant
    Filed: May 28, 1987
    Date of Patent: April 3, 1990
    Assignee: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Yukinori Ozato, Nobuhiko Tamura, Hiroaki Masumori, Michihiro Yamamoto, Atsuyuki Kojima, Fumio Nishikaku, Yoshihiko Kimura
  • Patent number: 4909828
    Abstract: Herbicidal 2,5-dihydropyrroles of the formula ##STR1## wherein A represents hydroxy, halogen, an alkylcarbonyloxy group having alkyl with 1 to 4 carbon atoms optionally substituted by halogen, or an alkylsulfonyloxy group having 1 to 4 carbon atoms optionally substituted by halogen,X represents CH or N, andR.sup.1, R.sup.2 and R.sup.3 each represent hydrogen, or an alkyl group having 1 to 4 carbon atoms optionally substituted by halogen, with the proviso that all of R.sup.1, R.sup.2 and R.sup.3 do not simultaneously represent hydrogen,or R.sup.2 and R.sup.3, together with the carbon atom to which they are bonded, may form an alicyclic ring with 3 to 6 carbon atoms.Intermediates of the formula ##STR2## are also new.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: March 20, 1990
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi
  • Patent number: 4904660
    Abstract: Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.
    Type: Grant
    Filed: February 25, 1988
    Date of Patent: February 27, 1990
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
  • Patent number: 4889953
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.
    Type: Grant
    Filed: July 22, 1987
    Date of Patent: December 26, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
  • Patent number: 4882342
    Abstract: The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl ring of the formula: ##STR2## or R.sub.1 is naphthyl, heterocycle or a bicyclic heterocycle and R.sub.1 -R.sub.7 are described in claim 1.These compounds are useful for prophylaxis or treatment of heart and circulatory disease especially to increase contractility of the heart, lower blood pressure and/or influence the thrombocyte function and improve the microcirculation.
    Type: Grant
    Filed: October 6, 1987
    Date of Patent: November 21, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Jens-Peter Holck, Alfred Mertens, Bernd Muller-Beckmann, Lothar Kling
  • Patent number: 4874864
    Abstract: Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors use as anti-plasmin and anti-thrombin agents.
    Type: Grant
    Filed: May 24, 1988
    Date of Patent: October 17, 1989
    Assignee: Pfizer Inc.
    Inventors: Rodney C. Schnur, Anton F. J. Fliri
  • Patent number: 4863947
    Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.
    Type: Grant
    Filed: August 11, 1986
    Date of Patent: September 5, 1989
    Assignee: Rohm and Haas
    Inventor: Richard M. Jacobson
  • Patent number: 4835280
    Abstract: The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
    Type: Grant
    Filed: July 14, 1987
    Date of Patent: May 30, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
  • Patent number: 4831032
    Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: May 16, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
  • Patent number: 4826990
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## Y is ##STR3## Z is ##STR4## R.sup.1 is ##STR5## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is ##STR6## W represents a bond or ##STR7## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR8## R.sup.6 is hydrogen, lower alkyl, ##STR9## and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: May 2, 1989
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III
  • Patent number: 4818273
    Abstract: Novel substituted triazolo[1,5-a]pyrimidine-2-sulfonamides, e.g., 5,7-dimethyl-N-(2,6-dichlorophenyl)-1,2,4-triazolo[1,5-a]pyrimidine-2-sulf onamide and their agriculturally acceptable salts are prepared. These compounds and compositions containing them are useful for the control of unwanted vegetation. Novel substituted triazolo[1,5-a]pyrimidine-2-sulfonyl chlorides and substituted anilines and their use as intermediates are also described.
    Type: Grant
    Filed: December 10, 1986
    Date of Patent: April 4, 1989
    Assignee: The Dow Chemical Company
    Inventors: William A. Kleschick, Robert J. Ehr, Mark J. Costales, Ben C. Gerwick, III, Richard W. Meikle, deceased, William T. Monte, Pearson, Norman R.
  • Patent number: 4818270
    Abstract: 2-(Heteroamino)-4,5-substituted-oxazole/thiazole compounds are antidotes for thiocarbamate, triazine and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds in sorghum.
    Type: Grant
    Filed: August 28, 1986
    Date of Patent: April 4, 1989
    Assignee: Monsanto Company
    Inventors: Raymond C. Grabiak, Robert K. Howe, Cheryl Yearell-Vinson
  • Patent number: 4810717
    Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: March 7, 1989
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Sheung T. Kam, William L. Matier
  • Patent number: 4808588
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: February 28, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Francis D. King
  • Patent number: 4798893
    Abstract: A method for the synthesis of the 2-propanone (I) is described starting from alkoxide (II) through the lactone (IV). ##STR1## Excellent control of the location of the substitution on the phenyl ring is achieved and the reaction proceeds in high yield.
    Type: Grant
    Filed: September 21, 1987
    Date of Patent: January 17, 1989
    Assignee: McNeilab, Inc.
    Inventors: David A. Cherry, Cynthia A. Maryanoff, John E. Mills, Roy A. Olofson, James D. Rodgers
  • Patent number: 4792568
    Abstract: This invention relates to new lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: ##STR1## and salts thereof; wherein, R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aralkyl, phenyl, naphthyl, or a nitrogen oxygen or sulfur heterocyclic; andY.sub.1 and Y are independently hydrogen, lower alkyl, hydroxy, lower alkoxy, aryloxy, lower aralkoxy, aryl, lower aralkyl, carboxy, lower carbalkoxy, lower carbaralkoxy, carbaryloxy, formyl, or alkyl, alkenyl or alkynyl containing up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms;provided that when Y and Y.sub.1 are both hydrogen or when Y.sub.1 is hydrogen and Y is CHO, the R is other than hydrogen, unsubstituted phenyl, or lower alkyl.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: December 20, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventor: Joseph Auerbach
  • Patent number: 4791131
    Abstract: Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.
    Type: Grant
    Filed: December 31, 1987
    Date of Patent: December 13, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4791113
    Abstract: Mitomycin derivatives having potent antitumor activity having the formula: ##STR1## wherein A is ON--or R.sub.4 N.dbd.N--[wherein R.sub.4 is selected from ##STR2## and optionally substituted heterocyclic groups (wherein R.sub.5 and R.sub.8 are each independently selected from hydrogen, lower alkyl and lower cycloalkyl; R.sub.6 is selected from hydrogen, halogen, hydroxy, lower alkoxy, amino and nitro; R.sub.7 is selected from lower alkyl and lower cycloalkyl; and X is selected from oxygen, sulphur and imino)];R.sub.1 and R.sub.2 are each independently selected from hydrogen, lower alkyl, lower cycloalkyl, optionally substituted aralkyl, optionally substituted alkanoyl, optionally substituted arylcarbonyl, optionally substituted alkanesulfonyl, arylsulfonyl and aralkylsulfonyl;R.sub.3 is hydrogen or carbamoyl;Y is hydrogen or methyl;Z is selected from hydrogen, methyl and acetyl;and is an .alpha. or .beta. bond.
    Type: Grant
    Filed: May 12, 1987
    Date of Patent: December 13, 1988
    Assignee: Kyowa Hakko Kogyo Kabushiki Kaisha
    Inventors: Tokuyuki Kuroda, Koji Hisamura, Tohru Sugaya, Yutaka Ohsawa, Hideo Ueno, Makoto Morimoto, Tadashi Ashizawa
  • Patent number: 4791129
    Abstract: 1,3,-Dicarboxamidooxindoles as antiinflammatory agents prepared by reaction of the 1-carbamoyloxindole with an isocyanate or by aminolysis of the corresponding alkyl 1-carbamoyloxindole-3-carboxylate.
    Type: Grant
    Filed: November 9, 1987
    Date of Patent: December 13, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4786646
    Abstract: The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer from 0 to 4, R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: November 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4771061
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: May 6, 1987
    Date of Patent: September 13, 1988
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4754041
    Abstract: Antibacterial activity is exhibited by 2-azetidinones activated in the 1-position with an --SO.sub.3 H group and having in the 3-position an acylamino group of the formula ##STR1## wherein X is --(CH.sub.2).sub.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: June 28, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: David Kronenthal
  • Patent number: 4740231
    Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: April 26, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4739083
    Abstract: A new process for preparing a pyrone-3-carboxamide compound of the formula (IV): ##STR1## wherein R.sub.1 is aryl or heterocyclic group optionally substituted, R.sub.2 is alkyl, aralkyl or like group, comprising reacting a compound of the formula (I) or (I'): ##STR2## wherein R.sub.3 is dialkylamino group and n is 0 to 6, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II): ##STR3## wherein R.sub.4 and R.sub.5 are hydrogen atom, alkyl or like group, or reacting a compound of the formula (III): ##STR4## wherein R.sub.6 is alkyl, aryl or like group, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II) or diketene in the presence of a tertiary organic base.
    Type: Grant
    Filed: January 2, 1986
    Date of Patent: April 19, 1988
    Assignee: Daicel Chemical Industries Ltd.
    Inventors: Yoichiro Ueda, Yukihisa Goto, Kazuhisa Masamoto
  • Patent number: 4730004
    Abstract: Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.
    Type: Grant
    Filed: February 2, 1987
    Date of Patent: March 8, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4725616
    Abstract: 1,3-Dicarboxamidooxindoles as antiinflammatory agents prepared by reaction of the 1-carbamoyloxindole with an isocyanate or by aminolysis of the corresponding alkyl 1-carbamoyloxindole-3-carboxylate.
    Type: Grant
    Filed: January 20, 1987
    Date of Patent: February 16, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4695567
    Abstract: The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 17, 1986
    Date of Patent: September 22, 1987
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Mertens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein, Egon Roesch
  • Patent number: 4695571
    Abstract: Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: April 2, 1986
    Date of Patent: September 22, 1987
    Assignee: Pfizer Inc.
    Inventor: Lawrence S. Melvin
  • Patent number: 4687857
    Abstract: Novel alkyl .beta.-oxo-benzenepropanoates of the formula ##STR1## wherein X is in the 5-,6-,7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF.sub.3 --, CF.sub.3 S-- and CF.sub.3 O--, R.sub.1 ' is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 ' is selected from the group consisting of hydrogen, thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, thienyl, benzothiazolyl and phenyl optionally substituted with at least one member of the group consisting of halogen, alkoxy of 1 to 4 carbon atoms, hydroxy, phenyl, CF.sub.3 --, NO.sub.2 -- alkyl of 1 to 4 carbon atoms and alkyl of 1 to 4 carbon atoms substituted with amino, alkylamino or dialkylamino with alkyls of 1 to 3 carbon atoms or R.sub.1 ' and R.sub.
    Type: Grant
    Filed: October 12, 1984
    Date of Patent: August 18, 1987
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Odile Le Martret
  • Patent number: 4681883
    Abstract: This invention relates to aminoalkylphenoxyalkyl substituted heterocycles. These compounds antagonize the action of histamine on histamine H.sub.2 -receptors in the brain. A compound of the invention is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]benzthiazole.
    Type: Grant
    Filed: October 17, 1985
    Date of Patent: July 21, 1987
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Robert C. Mitchell, Ian R. Smith, Rodney C. Young
  • Patent number: 4670448
    Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the substituents are defined in the detailed description.The compounds show pharmaceutical activity as selective histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: February 10, 1983
    Date of Patent: June 2, 1987
    Assignee: Glaxo Group Limited
    Inventors: John W. Clitherow, John Bradshaw, John W. M. Mackinnon, Duncan B. Judd, David E. Bays, Roger Hayes, Andrew Pearce
  • Patent number: 4666502
    Abstract: The invention provides 5-membered heteroaromatic compounds of formula IArN(Y)COCH.sub.2 Cl Iwherein Ar is a 5-membered heteroaromatic group comprising 1 or 2 heteroatoms selected from O, S and N and linked by a ring C-atom to the N-atom of the N(Y)COCH.sub.2 Cl group to which it is bound, whereby where Ar is pyrazolyl, said N(Y)COCH.sub.2 Cl group is in the 4-position,and Y is as specified in the description,the use of these compounds as herbicides, compositions for facilitating such use and the preparation of the chloroacetamides.
    Type: Grant
    Filed: February 3, 1983
    Date of Patent: May 19, 1987
    Assignee: Sandoz Ltd.
    Inventors: Karl Seckinger, Fred Kuhnen, Karlheinz Milzner
  • Patent number: 4663341
    Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.
    Type: Grant
    Filed: January 11, 1985
    Date of Patent: May 5, 1987
    Assignee: Rohm and Haas Company
    Inventor: Richard M. Jacobson
  • Patent number: 4652651
    Abstract: The manufacture of 1-sulpho-2-oxazetidine derivatives of the formula ##STR1## in which Het is an optionally amino-substituted, 5- or 6-membered, aromatic heterocycle containing 1 or 2 nitrogen atoms and optionally also an oxygen or sulphur atom, R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl-lower-alkoxycarbonyl-lower alkyl, nitrophenyl-lower-alkoxycarbonyl-lower alkyl or carboxy-lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, lower alkanoyloxy-lower alkyl, lower alkoxycarbonyl-lower alkenyl, hydroxyiminomethyl, lower alkoxyiminomethyl, carbamoyl, carbamoyl-lower alkenyl or carbamoyloxy-lower alkyl, the group .dbd.NOR.sup.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: March 24, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Werner Hofheinz, Christian N. Hubschwerlen, Hans P. Isenring
  • Patent number: 4647660
    Abstract: Antibacterial activity is exhibited by 2-azetidinones activated in the 1-position with an --SO.sub.
    Type: Grant
    Filed: May 2, 1985
    Date of Patent: March 3, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, Hermann Breuer, Glenn A. Jacobs
  • Patent number: 4645841
    Abstract: Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is straight or branched alkyl, optionally interrupted by heteroatoms such as oxygen, sulfur or nitrogen; straight or branched alkenyl; alkynyl; cyano; cycloalkyl or cycloaliphatic alkyl; a bicyclic group; aryl; or a heterocyclic group; orR.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, form a heterocyclic group;R.sub.4 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; andHet is a substituted or unsubstituted heterocycle containing two or three heteroatoms; tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
    Type: Grant
    Filed: June 24, 1985
    Date of Patent: February 24, 1987
    Assignee: Istituto de Angeli, S.p.A.
    Inventors: Giuseppe Bietti, Enzo Cereda, Arturo Donetti, Piero Del Soldato, Antonio Giachetti, Rosamaria Micheletti
  • Patent number: 4638062
    Abstract: Antibacterial activity is exhibited by 2-azetidinones activated in the 1-position with an --SO.sub.3 H group and having in the 3-position an acylamino group of the formula ##STR1## wherein X is --(CH.sub.2).sub.
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: January 20, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: David Kronenthal
  • Patent number: 4636516
    Abstract: Novel 3,5-di-tert-butyl-4-hydroxyphenyl-substituted heterocyclic compounds shown by the formula ##STR1## wherein .circle.Het -- represents a specific heterocyclic group and the salts thereof.The compounds have an anti-inflammatory, an anti-pyretic, an analgesic, an anti-arthritic, and an immunoregulatory activity. Hence, they are particularly useful as an antirheumatics.
    Type: Grant
    Filed: February 11, 1982
    Date of Patent: January 13, 1987
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kazuo Kubo, Yasuo Isomura, Shuichi Sakamoto, Hiroshige Homma
  • Patent number: 4629794
    Abstract: A series of novel antibacterially active derivatives of indolmycin as well as some prodrug forms of indolmycin is disclosed. A novel process for the production of these compounds is also disclosed.
    Type: Grant
    Filed: January 23, 1986
    Date of Patent: December 16, 1986
    Assignee: Pfizer Inc.
    Inventor: John P. Dirlam
  • Patent number: 4604132
    Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B and D are selected from CH and N;E is selected from oxygen and sulfur;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, phenyl, substituted phenyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;R.sup.
    Type: Grant
    Filed: April 27, 1984
    Date of Patent: August 5, 1986
    Assignee: ICI Australia Limited
    Inventors: Richard J. Conway, Keith G. Watson, Graeme J. Farquharson
  • Patent number: 4584385
    Abstract: A series of novel antibacterially active derivatives of indolmycin as well as some prodrug forms of indolmycin is disclosed. A novel process for the production of these compounds is also disclosed.
    Type: Grant
    Filed: February 4, 1985
    Date of Patent: April 22, 1986
    Assignee: Pfizer Inc.
    Inventor: John P. Dirlam
  • Patent number: 4582855
    Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 momoered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.
    Type: Grant
    Filed: November 12, 1981
    Date of Patent: April 15, 1986
    Assignee: American Hospital Supply Corporation
    Inventors: Sheung T. Kam, William L. Matier
  • Patent number: RE33125
    Type: Grant
    Filed: July 11, 1986
    Date of Patent: December 5, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas