Oxygen Bonded Directly To The Diazine Ring Patents (Class 544/123)
  • Patent number: 5250533
    Abstract: Fungicidal pyridinylpyrimidines of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, alkoxy, alkylthio, halogenoalkyl, amino or dialkylamino, where, in the case of dialkylamino, the two radicals may, together with the nitrogen to which they are bonded, form a 5- to 7-membered, saturated or unsaturated ring which optionally contains a further hetero atom and which is optionally substituted by 1 or 2 alkyl groups; orR.sup.1 represents in each case optionally substituted aryloxy, arylthio, aralkyloxy or aralkylthio,R.sup.2 and R.sup.3 are independent of one another and are identical or different and in each case represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio or alkoxycarbonyl,orR.sup.2 and R.sup.3 together represent anaylene chain having 3 to 6 carbon atoms which are linked via the ring positions 3 and 4 or 4 and 5,R.sup.
    Type: Grant
    Filed: March 2, 1992
    Date of Patent: October 5, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Alexander Klausener, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes
  • Patent number: 5234923
    Abstract: Novel compounds are disclosed having the formula ##STR1## or its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
    Type: Grant
    Filed: December 16, 1991
    Date of Patent: August 10, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Michael A. Poss, Karnail S. Atwal
  • Patent number: 5223505
    Abstract: This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.
    Type: Grant
    Filed: April 20, 1990
    Date of Patent: June 29, 1993
    Assignee: Imperial Chemical Industries Plc
    Inventors: Rodney B. Hargreaves, Paul W. Marshall, Bernard J. McLoughlin, Stuart D. Mills
  • Patent number: 5223017
    Abstract: Compounds of formula (I) or salts thereof, ##STR1## in which J is a radical of the formula R.sup.1 SO.sub.2 --CR.sup.2 R.sup.3 --, R.sup.4 R.sup.5 N--SO.sub.2 --CR.sup.2 R.sup.3 --, or ##STR2## and wherein the radicals R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.*, A, W, m, n and 0 are defined as set forth in the specification, are suitable as selective herbicides and plant growth regulators.
    Type: Grant
    Filed: July 3, 1991
    Date of Patent: June 29, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5215569
    Abstract: Substituted pyridines of the formula ##STR1## in which A represents nitrogen or a C-X group where X represents hydrogen or halogen,Q represents oxygen or sulphur,R.sup.1 and R.sup.2 are identical or different and represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, alkylamino or dialkylamino,R.sup.3 represents hydrogen, amino, nitro, hydroxyl, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylamino, dialkylamino, alkylcarbonylamino, alkoxycarbonylamino or alkysulphonylamino,R.sup.4 represents hydrogen or alkyl andZ represents oxygen or one of the groups below: ##STR2## where R.sup.5, R.sup.6 and R.sup.7 are defined herein and their use in herbicide compositions.
    Type: Grant
    Filed: July 31, 1991
    Date of Patent: June 1, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark W. Drewes, Peter Muller, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
  • Patent number: 5196533
    Abstract: 6,6-Disubstituted pteridines which are useful for the regulation of enzymes are disclosed, along with a general method of synthesizing these compounds.
    Type: Grant
    Filed: March 14, 1991
    Date of Patent: March 23, 1993
    Assignee: South Alabama Medical Science Foundation, USA
    Inventors: June E. Ayling, Steven W. Bailey
  • Patent number: 5194608
    Abstract: A dipeptide derivative of formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.
    Type: Grant
    Filed: June 24, 1991
    Date of Patent: March 16, 1993
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tatsuo Toyoda, Toshihiro Fujioka, Kunio Hayashi, Masuhisa Nakamura, Naofumi Hashimoto
  • Patent number: 5169430
    Abstract: A compound having the structural formula ##STR1## wherein: R is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, formyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.3 -C.sub.4 alkenyl or C.sub.3 -C.sub.4 alkynyl, or alkali metal;X is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.8 alkoxy, cyano, or halogen;Y is hydrogen, halogen, or C.sub.1 -C.sub.4 dialkylamino;R.sup.1 is hydrogen, C.sub.1 -C.sub.8 straight chain or branched alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 alkoxy or C.sub.3 -C.sub.8 hydroxyalkyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 straight chain or branched alkyl, C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, halo substituted C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.1 -C.sub.4 alkoxy, hydroxy C.sub.1 -C.sub.4 alkyl, cyano C.sub.1 -C.sub.4 alkyl, 2,3-epoxypropyl, 2,2-dialkoxyethyl, alkoxyalkyl, phenyl, aralkyl, C.sub.1 -C.sub.4 acyl, C.sub.1 -C.sub.4 carbalkoxyalkyl, C.sub.1 -C.sub.4 carbalkoxyalkyl substituted by C.sub.1 -C.sub.
    Type: Grant
    Filed: August 9, 1991
    Date of Patent: December 8, 1992
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Richard J. Strunk, Allyn R. Bell
  • Patent number: 5167693
    Abstract: Herbicidal substituted azines of the formula ##STR1## in which m represents the numbers 0, 1, 2 or 3,A represents nitrogen or a C-X group where X represents hydrogen or halogen,Q represents oxygen or sulphur,R.sup.1 and R.sup.2 are identical or different and represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy-alkyl, alkoxy, halogenoalkoxy, alkylthio, alkylamino or dialkylamino,R.sup.3 represents amino, hydroxyl, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylamino, dialkylamino, alkylcarbonylamino, alkoxycarbonyl-amino or alkylsulphonylamino,R.sup.4 represents hydrogen or alkyl andZ represents N--R.sup.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: December 1, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark W. Drewes, Rolf Kirsten, Wolfgang Kramer, Bernd W. Kruger, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
  • Patent number: 5162326
    Abstract: Novel pyrimidinedione derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydrogen or a hydrocarbon residue which may be substituted; R.sup.2 is hydrogen, halogen, nitro, optionally substituted amino, formyl or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrocarbon residue which may be substituted; R.sup.4 is hydrogen, halogen or nitro; R.sup.5 is a residue capable of forming an anion or a residue convertible into an anion; X is a direct bond or a spacer having one atomic length and containing an oxygen, nitrogen or sulfur atom; Y is a direct bond or a spacer having atomic length of two or less between the phenylene group and the phenyl group; n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof have potent angiotensin II antagonistic activity and hypotensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.
    Type: Grant
    Filed: February 13, 1991
    Date of Patent: November 10, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Kohei Nishikawa
  • Patent number: 5147876
    Abstract: 2,6-di-, 2,4,6-, 2,5,6-tri- or 2,4,5,6-tetra-substituted pyrimidines, and 2,6-di-substituted pyridines. These compounds are useful for treatment of neurological diseases.
    Type: Grant
    Filed: December 29, 1989
    Date of Patent: September 15, 1992
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Akira Mizuchi, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Mitsuyuki Takesue, Noriaki Kihara
  • Patent number: 5142047
    Abstract: A composition of polymer molecules effective to bind, with substantially uniform binding affinity, to a single-stranded polynucleotide containing a target sequence of bases. The polymer molecules are composed of a sequence of base-pairing moieties effective to hydrogen bond to corresponding, complementary bases in the target sequence, under selected binding conditions, and a predominantly uncharged, achiral backbone supporting the base-pairing moieties at positions and in orientations which allow hydrogen bonding between the pairing moieties of the polymer and the corresponding complementary bases in the target sequence. The composition has diagnostic uses, in a solid-support assay system, and therapeutic uses involving inhibition or inactivation of target polynucleotides.
    Type: Grant
    Filed: September 23, 1987
    Date of Patent: August 25, 1992
    Assignee: Anti-Gene Development Group
    Inventors: James Summerton, Dwight Weller, Eugene Stirchak
  • Patent number: 5135563
    Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.
    Type: Grant
    Filed: July 5, 1991
    Date of Patent: August 4, 1992
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saitoh, Hideyuki Shibata
  • Patent number: 5130317
    Abstract: Pyrimidine-4,6-dicarboxylic acid diamides, processes for the use thereof, and pharmaceuticals based on these compoundsThe invention relates to pyrimidine-4,6-dicarboxylic acid diamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The compounds according to the invention inhibit proline hydroxylase and lysine hydroxylase and can be employed as fibrosuppressants and immunosuppressants.
    Type: Grant
    Filed: September 19, 1990
    Date of Patent: July 14, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall, Stephan Henke
  • Patent number: 5125957
    Abstract: A pyrimidine derivative represented by the formula ##STR1## wherein the variables are defined below in the specification, and their production and herbicidal activities are described.
    Type: Grant
    Filed: October 24, 1990
    Date of Patent: June 30, 1992
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
  • Patent number: 5120843
    Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: June 9, 1992
    Assignee: Upjohn
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Patent number: 5102444
    Abstract: This invention relates to herbicidal pyridine-sulfonylureas which are highly active as preemergence and postemergence herbicides.
    Type: Grant
    Filed: April 12, 1990
    Date of Patent: April 7, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Paul H. Liang
  • Patent number: 5102884
    Abstract: A substituted benzoylurea compound of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a halogen atom or a nitro group, each of R.sup.2 and R.sup.3 is a hydrogen atom, an alkyl group, --COR.sup.6 (wherein R.sup.6 is an alkyl group or an alkoxy group) or --SO.sub.2 R.sup.6 (wherein R.sup.6 is as defined above), or R.sup.2 and R.sup.3 may form together with the adjacent nitrogen atom a heterocyclic ring, R.sup.4 is a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkylthio group or a nitro group, and R.sup.5 is a halogen atom, a nitro group or a substituted or unsubstituted alkyl group, or its salt.
    Type: Grant
    Filed: July 19, 1990
    Date of Patent: April 7, 1992
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Takahiro Haga, Nobutoshi Yamada, Hideo Sugi, Toru Koyanagi, Hiroshi Okada
  • Patent number: 5093336
    Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: March 3, 1992
    Assignee: Hoechat-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5093492
    Abstract: Methine dyes of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y and the rings A and B each have specific meanings, and methine dyes obtainable by reacting an organic mono- or polyisocyanate with such a methine dye of the abovementioned formal where only the radicals R.sup.1 and/and R.sup.4 have a group reacting with an organic mono- or polyisocyanate are useful in optical recording media.
    Type: Grant
    Filed: August 7, 1990
    Date of Patent: March 3, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Acker, Mathias Dust, Peter Neumann, Sibylle Brosius, Klaus D. Schomann, Harald Kuppelmaier
  • Patent number: 5084459
    Abstract: There is provided a pest control composition containing a compound represented by the formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof.The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.
    Type: Grant
    Filed: October 25, 1989
    Date of Patent: January 28, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideki Uneme, Isao Minamida, Tetsuo Okauchi, Noriko Higuchi
  • Patent number: 5075316
    Abstract: Novel compounds of the formula ##STR1## in which: R.sub.1 and R.sub.2 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.2 halogenoalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 halogenoalkoxy; R.sub.3 is C.sub.3 -C.sub.6 cycloalkyl or C.sub.3 -C.sub.6 cycloalkyl which is substituted by up to three identical or different methyl or halogen groups; R.sub.4 is halogen, thiocyano, --OR.sub.5, --SR.sub.5 or --NR.sub.5 R.sub.6, in which R.sub.5 and R.sub.6 are halogen groups; R.sub.4 is halogen, thiocyano, --OR.sub.5, --SR.sub.5 or --NR.sub.5 R.sub.6, in which R.sub.5 and R.sub.6 are as defined herein, are novel active compounds for preventing attack of plants by microorganisms. The compounds can be employed as microbicides as such or in the form of suitable agents.
    Type: Grant
    Filed: March 20, 1990
    Date of Patent: December 24, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Adolf Hubele
  • Patent number: 5073544
    Abstract: This invention provides compositions for enhancing penetration of physiologically active agents through the skin or mucosal membranes and for retaining these agents in body tissues, said composition comprising effective amounts of a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms, ##STR2## wherein R" is H or
    Type: Grant
    Filed: March 23, 1989
    Date of Patent: December 17, 1991
    Assignee: Whitby, Inc.
    Inventors: James V. Peck, Gevork Minaskanian
  • Patent number: 5064826
    Abstract: This invention relates to novel triazolopyrimidine derivatives of formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen, a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group and containing one or more oxygen and/or nitrogen atoms or a group of formula--SR.sup.1 wherein R.sup.1 is alkyl or aralkyl, or a group of formula--NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or a heterocyclic group,m and n are independently 0, 1, 2, 3 or 4, with the provision that if m stands for 0, then n is different from 0, and if both n and m are 1 or m stands for 0 and n is 2, the Q is different from methylthio or morpholino group, their mixtures or pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The compounds of formulae (Ia) and (Ib) are able to inhibit the ptosis caused by tetrabenazine and they have analgetic activity.
    Type: Grant
    Filed: March 2, 1990
    Date of Patent: November 12, 1991
    Inventors: Klara Reiter nee Esses, Jozsef Reiter, Zoltan Budai, Endre Rivo, Peter Trinka, Lujza Petocz, Gabor Gigler, Istvan Gyertyan, Istvan Gacsalyi
  • Patent number: 5053072
    Abstract: Compounds of the formula I or salts thereof ##STR1## where R.sup.1 is H or an aliphatic radical; R.sup.2 and R.sup.3 are H, alkyl or phenyl; W is O, S, NR.sup.4 or NOR.sup.4 ; X is CHR.sup.2, O or NR.sup.4 ; L is a (substituted) phenyl, naphthyl or monocyclic heteroaryl radical, A is a (substituted) pyrimidyl, triazinyl, triazolyl or bicyclic heteroaryl radical, and m and n are 0 or 1, have advantageously herbicidal or plant growth-regulating properties.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: October 1, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz
  • Patent number: 5047409
    Abstract: Salts of thiazolidine-4-carboxylic acids with 6-Piperidino-2,4-diaminopyrimidine-3-oxide are described of Formula I. ##STR1## Compounds I are useful in the field of cosmetics and pharmaceuticals for the treatment of loss of hair or in pathological forms such as alopecia, flaking dermatitis, etc. . . . Topical formulations containing compounds I are also described.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: September 10, 1991
    Assignee: Serono OTC S.A.
    Inventors: Michele G. Di Schiena, Vittoria Orru
  • Patent number: 5043337
    Abstract: Insecticidal pyrimidin-4-yl carbamates of the formula ##STR1## in which R.sup.1 represents alkoxy, alkylthio, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl or dialkylamino,R.sup.2 represents hydrogen or alkyl,R.sup.3 represents hydrogen, alkyl or alkoxy orR.sup.2 and R.sup.3 together represent a double-linked alkanediyl radical,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents hydrogen or alkyl andA represents oxygen, sulphur or a radical ##STR2## where R.sup.6 represents alkyl.
    Type: Grant
    Filed: April 4, 1990
    Date of Patent: August 27, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Kurt Findeisen, Jurgen Hartwig, Benedikt Becker
  • Patent number: 5043443
    Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.
    Type: Grant
    Filed: July 24, 1990
    Date of Patent: August 27, 1991
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
  • Patent number: 5032166
    Abstract: The invention relates to certain 6-amino-substituted 2-pyridinesulfonylureas, intermediates thereof, and compositions and methods of their use.
    Type: Grant
    Filed: February 9, 1990
    Date of Patent: July 16, 1991
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Eric D. Taylor
  • Patent number: 5032167
    Abstract: Substituted sulfonylureas of the formula I ##STR1## where the substituents and indices have the following meanings: x is oxygen or sulfur;z is nitrogen or methine (=CH--);R.sup.1 is halogen or substituted or unsubstituted C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.3 -alkoxy, or a radical --CONR.sup.6 R.sup.7, whereR.sup.6 is hydrogen, C.sub.1 -C.sub.8 -alkyl or C.sub.1 -C.sub.6 -alkoxy andR.sup.7 is hydrogen or C.sub.1 -C.sub.8 -alkyl;R.sup.2 is halogen or substituted or unsubstituted C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkyl;R.sup.3 is C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -haloalkylthio, halogen, cyano, nitro, amino, mono-C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, C.sub.2 -C.sub.6 -alkenyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: December 12, 1989
    Date of Patent: July 16, 1991
    Assignee: BASF
    Inventors: Horst Mayer, Gerhard Hamprecht, Bruno Wuerzer, Karl-Otto Westphalen
  • Patent number: 5026418
    Abstract: Pyrimidine compounds useful as plant growth regulators have the formula (I): ##STR1## wherein Y is an optionally substituted secondary or tertiary alkyl group containing from 3 to 7 carbon atoms or an optionally substituted cycloalkyl or alkylcycloalkyl group containing from 3 to 7 carbon atoms; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or a lower alkyl group; A is an optionally substituted heterocyclic group, for example thienyl or pyridyl; n is an integer which may be from 0 to 2 and is preferably 0; and R.sup.3 is hydrogen, an alkyl group containing from 1 to 4 carbon atoms, or an alkenyl or alkynyl group containing from 2 to 4 carbon atoms.
    Type: Grant
    Filed: February 20, 1990
    Date of Patent: June 25, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventor: Kevin R. Lawson
  • Patent number: 5022915
    Abstract: 2,4-Diarylpyrimidines of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## R.sub.1 and R.sub.2 are independently selected from the group consisting of H, Br, Cl, F, C.tbd.N, CF.sub.3 and OCF.sub.3 ;R.sub.3 is selected from the group consisting of H, C.sub.1 -C.sub.4 alkyl, CO.sub.2 CH.sub.3, CO.sub.2 CH.sub.2 CH.sub.3, CH.sub.2 Cl, CH.sub.2 OCH.sub.3, CH.dbd.CH.sub.2, C.sub.1 -C.sub.3 thioalkyl, and C.sub.1 -C.sub.3 alkoxy;R.sub.4 is selected from the group consisting of H, --OH, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 thioalkyl, C.sub.1 -C.sub.3 alkoxy; andR.sub.5 is selected from the group consisting of H and F are useful as herbicidal agents.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: June 11, 1991
    Assignee: ICI Americas Inc.
    Inventor: Michael P. Prisbylla
  • Patent number: 5017211
    Abstract: The invention is concerned with novel compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the significances given in the description, as well as enol ethers and salts thereof and their manufacture, weed control compositions which contain such compounds as the active substance and the use of the active substances or compositions for the control of weeds. The invention is also concerned with certain novel starting materials and their production.
    Type: Grant
    Filed: May 19, 1989
    Date of Patent: May 21, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean Wenger, Paul Winternitz, Martin Zeller
  • Patent number: 5015284
    Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: May 14, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 4987135
    Abstract: A substituted benzene derivative represented by a formula: ##STR1## where A represents: ##STR2## wherein X is a hydrogen atom, a halogen atom or a nitro group, R.sup.1 is --X.sup.1 Z.sup.1 (X.sup.1 is an oxygen atom or a sulfur atom and Z.sup.1 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group), --COZ.sup.1 group (Z.sup.1 is as defined above), ##STR3## group (Z.sup.1 is as defined above, Z.sup.2 is --CO.sub.2 Z.sup.3 wherein Z.sup.3 is the same as Z.sup.1, or --SO.sub.2 Z.sup.3 wherein Z.sup.3 is as defined above and n is 0 or 1), ##STR4## (Z.sup.1 and Z.sup.3 are as defined above) or ##STR5## (X.sup.2, X.sup.3 and X.sup.4 are, respectively, an oxygen atom or a sulfur atom and Z.sup.4 and Z.sup.5 are the same as Z.sup.1), and R.sup.3 is a nitro group or ##STR6## (R.sup.4 and R.sup.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: January 22, 1991
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Takahiro Haga, Nobutoshi Yamada, Hideo Sugi, Toru Koyanagi, Hiroshi Okada
  • Patent number: 4980355
    Abstract: Novel substituted isonicotinic acid amides of the general formula ##STR1## in which X in ortho/ortho'-position are equal and represent fluorine, chlorine, bromine or iodine;Q.sub.1 is unsubstituted pyridimin-4-yl, or pyrimidin-4-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.2 is unsubstituted pyrimidin-2-yl, or pyrimidin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.3 is unsubstituted pyrimidin-5-yl, or pyrimidin-5-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.4 is pyridin-2-yl, pyridin-3-yl or pyridin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.5 is pyridazin-3-yl or pyridazin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.6 is unsubstituted pyrazin-2-yl, or pyrazin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;R.sub.1, R.sub.2, R.sub.3 are hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl having from 1 to 3 halogen atoms, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.
    Type: Grant
    Filed: March 3, 1989
    Date of Patent: December 25, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Helmut Zondler, Alfred Meyer, Wolfgang Eckhardt, Walter Kunz
  • Patent number: 4975433
    Abstract: A compound of the formula: ##STR1## wherein: R and R.sub.1 may be the same or different and are selected from the group consisting of H; cycloalkyl groups having up to 10 carbon atoms; or straight or branched chain alkyl, alkenyl or alkynyl of 1 to 10 carbon atoms;R.sub.2 and R.sub.3 together with the nitrogen atom to which they are bonded form a pyrrolidine, piperidine, N-methyl piperazine, piperazine or morpholine ring;or a non-toxic pharmaceutically acceptable salt, adduct, oxide or other derivative thereof; and pharmaceutical compositions adapted for topical administration to a human or non-human animal and methods of topically administering the compositions to humans and non-human animals.
    Type: Grant
    Filed: January 31, 1989
    Date of Patent: December 4, 1990
    Assignee: University of Florida
    Inventor: Kenneth B. Sloan
  • Patent number: 4962109
    Abstract: This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally substituted by alkyl or halogen;R.sup.2 is selected from alkyl; haloalkyl; alkoxy; alkylamino; dialkylamino; halogen; cycloalkyl optionally substituted by halogen or alkyl; and phenyl optionally substituted by alkyl, haloalkyl, halogen or alkoxy;R.sup.3 is selected from hydrogen and halogen;R.sup.4 is the residue of an alcohol of formula R.sup.4 --OH which forms an insecticidal ester when combined with chrysanthemic acid, permethrin acid or cyhalothrin acid; andX is selected from oxygen and sulphur.
    Type: Grant
    Filed: June 13, 1988
    Date of Patent: October 9, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: Edward McDonald, Roger Salmon, Alan J. Whittle
  • Patent number: 4960777
    Abstract: Heteroaryloxy-.beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is an optionally substituted heteroaryl residue,R.sup.2 is hydrogen, lower alkyl or lower alkoxyalkyl,X is a COOR.sup.3 -group wherein R.sup.3 means H or lower alkyl, or represents a CONR.sup.4 R.sup.5 -group wherein R.sup.4 and R.sup.5 mean respectively hydrogen or lower alkyl, R.sup.4 and R.sup.5 being capable of forming, together with the nitrogen atom, a 5- to 6-membered heterocycle, or means an oxadiazolyl residue of the formula ##STR2## wherein R.sup.6 means hydrogen, lower alkyl or cycloalkyl, are valuable pharmaceuticals.
    Type: Grant
    Filed: September 20, 1989
    Date of Patent: October 2, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Biere, Andreas Huth, Dieter Rahtz, Ralph Schmiechen, Dieter Seidelmann, David Stephens, Mogens Engelstoft, John B. Hansen
  • Patent number: 4957921
    Abstract: Substituted cyclohexanols are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: December 6, 1989
    Date of Patent: September 18, 1990
    Assignee: Warner-Lambert Company
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
  • Patent number: 4958043
    Abstract: A composition useful for incorporation into polymer compositions employed for food packaging or the like comprising a bis- or tris-methine compound having the structural formula ##STR1## wherein A is selected from the radicals ##STR2## wherein R' and R" are each selected from chlorine, bromine, fluorine, alkyl, alkoxy, aryl, aryloxy and arylthio;each n is independently 0, 1, 2;R.sub.1 is selected from a large variety of radicals such as cycloalkyl, phenyl, and straight or branched alkyl which may be substituted;R.sub.2 is alkylene or the like;R.sub.3, R.sub.4, and R.sub.5 are each selected from hydrogen and alkyl; andP and Q and P.sup.1 and Q.sup.1 are selected from cyano, carbalkoxy, carbaryloxy, carbaralkyloxy, or the like.The invention compositions are especially useful in combination with molding or fiber-grade condensation polymer; most preferably such polymer having copolymerized therein a total of from 1.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: September 18, 1990
    Assignee: Eastman Kodak Company
    Inventors: Max A. Weaver, Wayne P. Pruett, Samuel D. Hilbert
  • Patent number: 4956366
    Abstract: Substituted thienoimidazole derivatives, a process for the preparation thereof, pharmaceutical compositions containing them, and the use thereof as inhibitors of gastric acid secretion, as gastroprotectives and as medicaments for intestinal inflammationsThe invention relates to compounds of the formula ##STR1## in which A represents ##STR2## T denotes --S--, --SO-- or --SO.sub.2 --, R.sup.1 to R.sup.10, X, Y and Z have the meanings indicated in the description, to a process for the preparation thereof, to pharmaceutical compositions containing them, and to the use thereof as inhibitors of gastric acid secretion, as gastroprotectives and as medicaments for intestinal inflammations.
    Type: Grant
    Filed: July 13, 1988
    Date of Patent: September 11, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hildegard Nimmesgern, Klaus Weidmann, Hans-Jochen Lang, Robert Rippel, Andreas W. Herling
  • Patent number: 4948416
    Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: August 14, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Robert J. Pasteris
  • Patent number: 4945093
    Abstract: A compound having formula: ##STR1## is described, where R.sub.3 and R.sub.4 may be identical or different and represent a hydrogen atom, alkyl, alkenyl, cycloalkyl;or R.sub.3 and R.sub.4 represent aryl aralkyl;or R.sub.3 and R.sub.4 together with the nitrogen atom linked thereto form a heterocycle;R.sub.1 and/or R.sub.2, independent of each other, represent hydrogen or carbanoyl having formula: ##STR2## where R.sub.7 represents alkyl, alkenyl, cycloalkyl, aryl or aralkyl. The compounds of formula (I) can be used in cosmetic or pharmaceutical compositions for the cosmetic treatment of hair, the treatment of alopecia, and also for the treatment of desquamating dermatitis.
    Type: Grant
    Filed: July 29, 1988
    Date of Patent: July 31, 1990
    Assignee: L'Oreal
    Inventors: Jean Maignan, Serge Restle, Gerard Lang
  • Patent number: 4940792
    Abstract: Novel substituted N-sulfonyl-N'-pyrimidinylureas or N-sulfonyl-N'-triazinylureas of the formula I ##STR1## have good pre- and postemergence selective herbicidal and growth regulating properties.In this formulaE is nitrogen or --CH.dbd.,the group ##STR2## is a phenyl, naphthyl, furyl, thiophenyl, pyrrole or pyridinyl radical which is substituted in accordance with the definitions ofR.sup.1 and R.sup.2,R.sup.3 and R.sup.4 are hydrogen, lower alkyl or lower alkoxy, or one of R.sup.3 and R.sup.4 may also be halogen, lower alkenyl, lower haloalkenyl, lower haloalkoxy, amino, lower alkylamino, --CH(OCH.sub.3).sub.2, a cyclized ketal group or a saturated 5- or 7-membered heterocycle which is bound through the nitrogen atom,R.sup.5 is hydrogen, lower alkyl, lower haloalkyl, or an unsubstituted or substituted phenyl, benzyl or naphthyl radical, andR.sup.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: July 10, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Topfl, Willy Meyer, Hans-Dieter Schneider
  • Patent number: 4929726
    Abstract: A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.
    Type: Grant
    Filed: February 9, 1988
    Date of Patent: May 29, 1990
    Assignee: Georgia State University Foundation, Inc.
    Inventors: Lucjan Strekowski, Maria Mokrosz, Donald B. Harden
  • Patent number: 4921527
    Abstract: The invention relates to sulfonylurea compounds with a substituted or unsubstituted bicyclic nine-membered ring having one to five heteroatoms which are preemergent and/or postemergent herbicides or plant growth regulants.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: May 1, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4920134
    Abstract: Novel compounds having the formula: ##STR1## wherein ##STR2## represents a nitrogen-containing aromatic 6-membered ring; R.sup.1 represents a higher alkyl group which may be substituted; R.sup.2 represents a tertiary amino group or a quaternary ammonium group; and m represents 2 or 3; and salts thereof have superior antitumor activities including differentiation-inducing activity, and are useful as antitumor agents.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: April 24, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keizo Inoue, Hiroaki Nomura, Eiko Imamiya
  • Patent number: 4908056
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: March 13, 1990
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4906283
    Abstract: This invention relates to herbicidally active sulfonamide compounds having a heterocyclic carbonyl group ortho to the sulfonyl bridge.
    Type: Grant
    Filed: April 25, 1988
    Date of Patent: March 6, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Joel R. Christensen