Additional Hetero Ring Containing Patents (Class 540/524)
  • Patent number: 5482920
    Abstract: Pyrimidinyloxy- and triazinyloxy- and pyrimidinylthio- and triazinylthio-butyric acid derivatives of formula I ##STR1## wherein Q is ##STR2## A is hydroxy or a group ##STR3## and the other substituents are as described in patent claim 1, and salts of compounds of formula I, have herbicidal action and are suitable as active ingredients in weed control compositions.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: January 9, 1996
    Assignee: Ciba-Geigy Corporation
    Inventor: Christoph Luthy
  • Patent number: 5470849
    Abstract: This invention relates to a method of inhibiting platelet aggregation, and compounds which are mimics of the peptide sequence Arg-Gly-Asp.
    Type: Grant
    Filed: April 30, 1993
    Date of Patent: November 28, 1995
    Assignee: SmithKline Beecham Corp.
    Inventors: James F. Callahan, William F. Huffman
  • Patent number: 5434148
    Abstract: Disclosed are .beta.-carboline derivatives represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen atom, a lower alkyl group, a lower alkoxy group or hydroxy group; R.sup.5 represents hydrogen atom, or R.sup.1 and R.sup.5 are bonded to represent a lower alkylenedioxy group; R.sup.2 represents hydrogen atom, a halogen atom, a lower alkoxy group or hydroxy group; R.sup.3 represents hydrogen atom, a carbamoyl lower alkyl group, a lower alkyl group, a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group; R.sup.4 represents hydrogen atom, a lower alkyl group, a carboxy lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower alkanoyl group, an arylcarbonyl group, a lower alkanesulfonyl group, a lower alkoxycarbonyl group, an aralkyl group, formyl group or a di(lower alkyl)sulfamoyl group; n represents 0, 1 or 2; and the symbol * represents an asymmetric carbon atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.
    Type: Grant
    Filed: May 27, 1993
    Date of Patent: July 18, 1995
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Masataka Hikota, Takeshi Yura, Toshiro Shikano, Masaaki Nagasaki
  • Patent number: 5426091
    Abstract: A compound of formula (I): ##STR1## or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X.sup.1 and X.sup.2 are independently oxygen or sulphur, R.sup.1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C.sub.2 -C.sub.4 alkylene group which is optionally interposed by an oxygen atom, a group ##STR2## or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and R.sup.b is alkyl or alkoxy; provided that when X, X.sup.1 and X.sup.2 are oxygen, R.sup.1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.
    Type: Grant
    Filed: August 4, 1993
    Date of Patent: June 20, 1995
    Assignee: Zeneca Limited
    Inventors: John E. D. Barton, David Cartwright, John M. Cox, Glynn Mitchell, Charles G. Carter, David L. Lee, Francis H. Walker, Frank X. Woolard
  • Patent number: 5424455
    Abstract: A heterocyclic compound of the formula, ##STR1## wherein A and B are each hydrogen, halogen, alkyl or alkoxy, R.sup.1 is alkylene having upto 6 carbon atoms, X is direct linkage or divalent group such as --O--, --S--and the like, T and U are each hydrogen or alkyl, l is 0 or 1 to 3, Q is 5-, 6- or 7- membered saturated or unsaturated heterocyclic residue, and Y is hydrogen, halogen, alkyl, alkoxy or ##STR2## and B are taken together with each other to form methylene-dioxy, which is useful for dyeing or printing hydrophobic fiber materials with superior dyeability to give a dyed or printed product of a red color excellent in fastness properties, particularly those such as washing fastness.
    Type: Grant
    Filed: July 28, 1993
    Date of Patent: June 13, 1995
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Jun Yamamoto, Yasuyoshi Ueda, Junichi Sekihachi, Yosuke Yamamoto, Takashi Omura
  • Patent number: 5378713
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: January 3, 1995
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5360800
    Abstract: The invention relates to tricyclic lactams of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenyl C.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl or phenoxymethyl,one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkhyl group;n represents 2 or 3; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: November 1, 1994
    Assignee: Glaxo Group Limited
    Inventors: Ian H. Coates, Peter C. North, Alexander W. Oxford
  • Patent number: 5356891
    Abstract: The present invention relates to compounds having anti-ischaemic activity of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and Z are as defined herein. The present invention further relates to a method of preparing such compounds, as well as compositions having anti-ischaemic activity which comprise such compounds and a method of treating ischaemia.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: October 18, 1994
    Inventors: Donald T. Witiak, Ineke van Wijngaarden, Raghunathan V. Nair, Josephus H. M. Lange, Jacobus A. J. den Hartog
  • Patent number: 5340822
    Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## where Y. m. Ar', n, p, Q, T, q and Z are defined herein. The invention also relates to methods of making the compounds of formula (I) and pharmaceutical compositions which contain the compounds of formula (I). The inventive compounds are useful as neurokinin receptor antagonists, and are useful for the treatment of any substance P-dependent and neurokinin-dependent pathological condition.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: August 23, 1994
    Assignee: Elf Sanofi
    Inventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
  • Patent number: 5317017
    Abstract: There are disclosed certain compounds identified as N-biphenyl-3-amido substituted benzolactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzolactams as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: May 31, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Hyun O. Ok, William R. Schoen, Matthew Wyvratt
  • Patent number: 5300647
    Abstract: Hindered amines based on various 2,2,6,6-tetraalkylated nitrogen-containing heterocyclic moieties wherein the hindered nitrogen atom on the ring is substituted with O-acyl, O-carbamoyl or O-carbonate substituents and the 4-position of the ring is substituted with a variety of groups, are effective as light stabilizers in diverse substrate systems.
    Type: Grant
    Filed: May 28, 1993
    Date of Patent: April 5, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Roger F. Malherbe, Roland A. E. Winter, James P. Galbo
  • Patent number: 5292734
    Abstract: This disclosure describes novel 2, 3, 6 substituted quinazolinones having the formula: ##STR1## wherein X, R, and R.sup.6 are described in the specification which have activity as angiotensin II (AII) antagonists.
    Type: Grant
    Filed: April 23, 1993
    Date of Patent: March 8, 1994
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan
  • Patent number: 5284857
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: February 8, 1994
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5281585
    Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: January 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Nathan Ihle, George D. Hartman, Laura M. Turchi, William F. Hoffman
  • Patent number: 5248683
    Abstract: Compounds of the formula ##STR1## in which A.sub.1 and A.sub.2 independently of one another are CO--C.sub.1 -C.sub.4 alkyl, COO--C.sub.1 -C.sub.4 alkyl, CO--CF.sub.3, CO--N(R).sub.2 or cyano;A.sub.1 and A.sub.2 together are CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO, CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO which is substituted by C.sub.1 -C.sub.4 alkyl, COOR, CON(R).sub.2, cyano or phenyl, it being possible for the phenyl ring, in turn, to be substituted by halogen, methyl, trifluoromethyl, methoxy, nitro or cyano; CO--N(R)--CO--N(R)--CO;R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl;X is oxygen, sulfur or N(CH.sub.3);X.sub.1, X.sub.2 and X.sub.3 independently of one another are hydrogen, halogen, methyl, methylthio, methoxy or nitro;n is 0 or 1;including the salts of the compounds of the formula I with agriculturally acceptable organic or inorganic bases, and including the metal complexes; have valuable microbicidal properties.
    Type: Grant
    Filed: June 4, 1992
    Date of Patent: September 28, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans-Georg Brunner, Walter Kunz, Rolf Schurter
  • Patent number: 5247081
    Abstract: Processes for the preparation of biotinylated polynucleotides and analogues thereof and protected intermediate products for use in such processes are described and claimed. The processes may be conveniently used in the automated synthesis of biotinylated polynucleotide on a DNA synthesizer. The polynucleotides so prepared may be used as labelled probes e.g. as diagnostic tools for clinical and research uses.
    Type: Grant
    Filed: August 23, 1988
    Date of Patent: September 21, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventor: Michael D. Edge
  • Patent number: 5244888
    Abstract: Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.
    Type: Grant
    Filed: July 9, 1991
    Date of Patent: September 14, 1993
    Assignee: Abbott Laboratories
    Inventors: John F. DeBernardis, Michael D. Meyer, Kevin B. Sippy
  • Patent number: 5240919
    Abstract: Compounds of general formula (I): ##STR1## where R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: August 31, 1993
    Assignee: Adir et Compagnie
    Inventors: Said Yous, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5236935
    Abstract: The present invention relates to novel benzopyran derivatives of formula (I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relates to processes for preparing such compounds; and to a pharmaceutical compositions containing such compounds as an active ingredient. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, a fluorine, chlorine or hydrogen atom; R.sup.A and R.sup.B are, each independently, an amino, C.sub.1-6 alkoxy, C.sub.1-6 alkyl group or an optionally substituted phenyl group; and R.sup.C and R.sup.D are a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is ##STR3## wherein R.sup.
    Type: Grant
    Filed: May 21, 1992
    Date of Patent: August 17, 1993
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Sung-Eun Yoo, Kyu Y. Yi, Nak C. Jeong, Jee H. Suh, Seon-Ju Kim, Hwa-Sup Shin, Byung H. Lee, Kyu S. Jung
  • Patent number: 5223616
    Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: June 29, 1993
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
  • Patent number: 5223523
    Abstract: Compounds for an methods of controlling plant diseases using thiooxazolidinones, oxazolidindiones and agriculturally suitable compositions containing them are disclosed.
    Type: Grant
    Filed: December 12, 1991
    Date of Patent: June 29, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: John B. Adams, Jr., Detlef Geffken, Dennis R. Rayner
  • Patent number: 5206149
    Abstract: This invention relates to a method of high sensitivity luminescence analysis using, as an enhancer, 2-hydroxy-9-fluorenone, the compound expressed by the following formula ##STR1## or an oxazole compound expressed by the formula ##STR2## in the formula R.sub.1 representing hydrogen, C.sub.n H.sub.2n+1 (here, n representing a positive integer of 1 to 4), XC.sub.n H.sub.2n (here, X representing F, Cl, Br or I, and n representing a positive integer of 1 to 4), C.sub.n H.sub.2n+1 CO.sub.2 (n being as defined above), a phenyl group, a naphthyl group, C.sub.n H.sub.2n+1 C.sub.6 H.sub.4 (n being as defined above), YC.sub.6 H.sub.4 (Y representing F, Cl, Br, I or a phenyl group) or XYC.sub.6 H.sub.3 (X and Y being as defined above).
    Type: Grant
    Filed: February 5, 1991
    Date of Patent: April 27, 1993
    Assignee: Toray Industries, Inc.
    Inventors: Yoshihiro Oyama, Shuntaro Hosaka, Tetsuya Makino
  • Patent number: 5190937
    Abstract: Novel compounds of formula (I), and pharmaceutically acceptable salts thereof; their preparation; compositions containing them; and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R.sub.1 is --OH; alkoxy; aryloxy or aralkyloxy in each of which the aryl group is optionally substituted; --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is independently hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom or an optionally substituted second nitrogen atom in the ring; or a group:--NH--CH(R.sub.8)--C(O)--R.sub.9where R.sub.8 is hydrogen; alkyl optionally substituted by --OH, alkoxy, --NR.sub.6 R.sub.7 as defined for R.sub.1, guanidine, --CO.sub.2 H, --CONH.sub.2, --SH, or --S--alkyl; or --CH.sub.2 --Ar where Ar is optionally substituted aryl or heteroaryl; and R.sub.
    Type: Grant
    Filed: January 11, 1991
    Date of Patent: March 2, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Ian Hughes
  • Patent number: 5175157
    Abstract: Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.
    Type: Grant
    Filed: July 3, 1991
    Date of Patent: December 29, 1992
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Manfred Psiorz, Joachim Heider, Andreas Bomhard, Manfred Reiffen, Norbert Hauel, Klaus Noll, Berthold Narr, Christian Lillie, Walter Kobinger, Jurgen Dammgen
  • Patent number: 5169844
    Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in inhibition of absorption of cholesterol and thus lowers serum cholesterol levels. Compounds of the formula below: ##STR1## where R.sup.1 is selected from alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or arylalkyl and R.sup.2 is hydrogen or alkyl or --NR.sup.1 R.sup.2 is morpholine, thiomorpholine or 4-substituted or unsubstituted piperidine and R.sup.3, R.sup.4, R.sup.5, R.sup.6 are hydrogen, alkyl, alkoxy, halogen, nitro, cyano, perhaloalkyl, alkanoyloxy, alkoxycarbonyl or hydroxycarbonyl have been shown to inhibit the enzymes CEH and/or ACAT in in vitro tests to inhibit absorption of radio-labeled cholesterol in rats.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: December 8, 1992
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Donald P. Strike
  • Patent number: 5164386
    Abstract: Pharmacologically active R(-) 3-quinuclidinol derivatives are described which are muscarinic receptor blocking agents useful for the treatment of gastrointestinal and respiratory tract disorders of the following formula (I) ##STR1## wherein R represents a linear or branched lower alkyl group, a cycloalkyl-C.sub.1-2 alkyl or an aralkyl group, or it is absent;X represents the anion of an organic or inorganic acid, or it is absent, when R is absent;R.sub.1 represents H, a linear or branched lower alkyl group or an acyl group of the type R.sub.2 --CO, in which R.sub.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: November 17, 1992
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Enzo Cereda, Giuseppe Bietti, Giovanni B. Schiavi, Arturo Donetti, Antonio Schiavone, Henri N. Doods
  • Patent number: 5157034
    Abstract: Antipsychotic compounds having the formula ##STR1## wherein Z is H or Cl; Y is O or S; n is 1-4; separately, X is H or (C.sub.1 -C.sub.2)alkyl and L is R(CH.sub.2).sub.m CO, m is 0 or 1-3, R is (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, phenyl, naphthyl, furyl, benzofuranyl, thienyl, benzothienyl, pyrrolyl, indolyl, isoindolyl or one of said groups substituted on aromatic or heteroaromatic ring with fluoro, chloro, (C.sub.1 -C.sub.2)alkyl or (C.sub.1 -C.sub.2)alkoxy; or together L and X, in combination with the nitrogen to which they are attached, form certain cyclic imides, 4-substituted piperidines or a cyclic sulfonamide.
    Type: Grant
    Filed: February 27, 1991
    Date of Patent: October 20, 1992
    Assignee: Pfizer Inc.
    Inventors: Gene M. Bright, Kishor A. Desai, Thomas F. Seeger
  • Patent number: 5149823
    Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: September 22, 1992
    Assignee: Shell Oil Company
    Inventor: Pen-Chung Wang
  • Patent number: 5134140
    Abstract: The antipsychotic, antidepressant, anxiolytic compounds of the formula: ##STR1## wherein Z is phenyl or phenyl substituted with alkyl, alkoxy, hydroxy, halogen or methylenedioxy or Z is one of the structures ##STR2## in which m is one of the integers 0, 1 or 2; R.sup.6 is hydrogen or alkyl; Y is H.sub.2 or O; or Z, taken with R.sup.1, forms one of the structures ##STR3## R.sup.1 is hydrogen or alkyl; R.sup.2 is hydrogen alkyl or phenyl; R.sup.3 is hydrogen or alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido of 2 to 6 carbon atoms or sulfonamido, or R.sup.4 and R.sup.5 together form methylenedioxy, ethylenedioxy, or propylenedioxy; n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: July 28, 1992
    Assignee: American Home Products Corporation
    Inventor: Gary P. Stack
  • Patent number: 5116958
    Abstract: Disperse dyes, which produce dyeings of excellent thermomigration fastness, consisting of a chromophore and a lactam or oxime radical which detaches on heating to leave an isocyanate or isothiocyanate group, which reacts with a suitable group in the environment. The disclosed dyes are described by the formula ##STR1## where F is the radical of a dye which is free of water-solubilizing groups,B is a bridge member or a direct bond,Z is O or S andV is the radical of a group H--V, where H--V is an oxime of the formula ##STR2## or a lactam of the formula ##STR3## in which R.sup.1 and R.sup.2 are each independently of the other substituted or unsubstituted alkyl or aryl, orR.sup.1 and R.sup.2 together with the carbon atom linking them form a cycloaliphatic ring,R is hydrogen or alkyl andn is an integer from 4 to 11.
    Type: Grant
    Filed: January 5, 1990
    Date of Patent: May 26, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Liechti, Martin Trottmann
  • Patent number: 5110585
    Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing at least 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is an anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.
    Type: Grant
    Filed: March 1, 1989
    Date of Patent: May 5, 1992
    Assignee: ISP Investments Inc.
    Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login, Michael W. Helioff
  • Patent number: 5106971
    Abstract: The prior art solvent process for the manufacture of an oxo-piperazinyl triazine (PIP-T) compound required carrying out the reaction between an appropriately hindered cyclic amine and cyanuric chloride in the presence of caustic catalyst, in alkylbenzene solution, typically toluene. The chloride ions generated during the reaction, in presence of water present in the reaction zone, produced serious corrosion and resulted in off-color product which had a melt absorptivity greater than 3.5 mL/gm.cm. This "color" in the product made the product generally unmarketable. Another process to make a PIP-T termed "the solventless" process used no toluene solvent, and no caustic but required such a very large excess of amine that the catalytic function of the amine.HCl salt went unnoticed.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: April 21, 1992
    Assignee: The B. F. Goodrich Company
    Inventors: George Kletecka, Victor L. Ledesma, Ronald M. Kovach
  • Patent number: 5104869
    Abstract: Renin inhibiting compounds containing a single .alpha.-amino acid of the formula: ##STR1## and analogs thereof which inhibit the substrate-cleaving acting or renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.
    Type: Grant
    Filed: October 25, 1990
    Date of Patent: April 14, 1992
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Charles Frederick, Jeremy I. Levin, Fuk-Wah Sum, Marvin F. Reich
  • 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: 5079356
    Abstract: Urea derivatives with .alpha.,.beta.-ethylenically unsaturated carboxyl or carboxamide radicals, produced by reaction of ethylenically unsaturated isocyanates with ammonia or amines or by reaction of ethylenically unsaturated amines with isocyanates in the absence of water, optionally in bulk, it being possible to carry out the reaction for improved reaction control advantageously in inert organic solvents or also in so-called reactive diluents, i.e. copolymerizable ethylenically unsaturated monomeric compounds which remain inert under the reaction conditions, such as for example vinyl esters, (meth)acrylates, vinyl aromatics.The urea derivatives produced according to the invention have in their monomeric form slight to moderate or in some cases good solubility in water and/or in organic solvents. They are polymerizable or copolymerizable via their .alpha., .beta.
    Type: Grant
    Filed: July 2, 1990
    Date of Patent: January 7, 1992
    Assignee: Hoechst AG
    Inventor: Hans-Ullrich Huth
  • Patent number: 5075302
    Abstract: Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR.sup.5).sub.n (CR.sup.3 R.sup.4)- or -(CR.sup.3 R.sup.4).sub.p X(CR.sup.3 R.sup.4).sub.q -,wherein two substituents selected from the group consisting of R.sup.3, R.sup.4 and R.sup.5, can form a benzene, cyclopentane or cyclohexane ring;X is -O-, -S-, -SO- or -SO.sub.2 -;Q is hydrogen or R.sup.6 CO-;m is 1 or 2;n is 1, 2, 3 or 4;p is 1 or 2;q is 2 or 3;R.sup.1 is lower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R.sup.
    Type: Grant
    Filed: March 9, 1990
    Date of Patent: December 24, 1991
    Assignee: Schering Corporation
    Inventor: Bernard R. Neustadt
  • Patent number: 5070088
    Abstract: Novel calcium channel blockers having the formula ##STR1## wherein X is oxygen or sulfur and wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 are as defined herein, are disclosed. These compounds are useful, for example, as anti-ischemic agents.
    Type: Grant
    Filed: December 19, 1989
    Date of Patent: December 3, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5051436
    Abstract: Novel N-acyl- and N-sulfonylbenzo-1,2,3-thiadiazole-7-carboxylic acid amides of formula ##STR1## in which X.sub.1 and X.sub.2 independently of one another are each hydrogen or together 1 to 3 halogen atoms; A is sulfonyl or carbonyl; Y is phenyl or phenyl substituted by C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 alkoxy, halogen, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 alkoxycarbonyl, C.sub.1 -C.sub.3 alkanoyloxymethyl, cyano and/or by nitro; R is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.3 -C.sub.5 alkenyl or C.sub.3 -C.sub.5 alkynyl; and in which, furthermore, the group ##STR2## wherein A.sub.1 is methylene, carbonyl or sulfonyl; X.sub.3 is hydrogen, methyl or halogen; m is 2, 3 or 4; and n is zero, 1 or 2.The novel active ingredients have plant-protecting properties and are suitable especially for the preventive protection of plants against attack by phytopathogenic microorganisms such as fungi, bacteria and viruses.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: September 24, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Kunz, Rolf Schurter
  • Patent number: 5041545
    Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: August 20, 1991
    Assignee: Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 5041454
    Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.
    Type: Grant
    Filed: April 19, 1990
    Date of Patent: August 20, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn
  • Patent number: 5028711
    Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: July 2, 1991
    Assignee: Beiersdorf Aktiengesellschaft
    Inventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
  • Patent number: 5001137
    Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: March 19, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
  • Patent number: 4999371
    Abstract: 3,4-Dihydro-2H-benzo[b]pyrans of the formula I ##STR1## are described, in which R.sup.1 is H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5,R.sup.4 and R.sup.5 being identical or different and representing H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkylcarbonyl,R.sup.2 and R.sup.3 are identical or different and are alkyl having 1-4 carbon atoms,Ar is an aromatic or heteroaromatic system which is unsubstituted or substituted,n is 1 or 2 andX is a (CH.sub.2).sub.r chain which can be interrupted by a heteroatom O, S or NR.sup.6, R.sup.6 being H or (C.sub.1 -C.sub.4)-alkyl andr being one of the numbers 2, 3, 4 or 5.Processes for the preparation of these compounds, their use and pharmaceutical products based on these compounds are also described.
    Type: Grant
    Filed: February 2, 1988
    Date of Patent: March 12, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich C. Englert, Hans-Jochen Lang, Dieter Mania, Bernward Scholkens
  • Patent number: 4992435
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: September 23, 1988
    Date of Patent: February 12, 1991
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 4992434
    Abstract: A microbicidal compostion contains as active ingredient 2-chloro-4-trifluoromethylthiazol-5-carbonic acid derivatives of the formula I ##STR1## R is organic radical with up to 40 carbon atoms, which optionally contains nitrogen, oxygen or sulfur atoms and which can be transformed by hydrolosis or oxydation into the directly to the thiazol ring bound carboxyl rest. These compounds have good microbicidal activity and are used for the control and prevention of infestation of plants by phytophathogenic microorganisms.
    Type: Grant
    Filed: April 11, 1989
    Date of Patent: February 12, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Topfl, Robert Nyfeler, Werner Fory
  • Patent number: 4990506
    Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl;R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl:or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.
    Type: Grant
    Filed: October 24, 1989
    Date of Patent: February 5, 1991
    Assignee: Synthelabo
    Inventors: Pascal George, Claudie Giron, Jacques Froissant
  • Patent number: 4985444
    Abstract: The invention relates to pyrazolopyridine compounds for the treatment of melancholia, heart failure, hypertension, renal insufficiency, edema, obesity, bronchial asthma, gout, hyperuricemia, sudden infant death syndrome, immunosuppression, diabetes, myocardiac infection, thrombosis, obstruction, arteriosclerosis obliterans, thrombophlebitis, cerebral infarction, transient ischemic attack or angina pectoris, said compounds being of the formula ##STR1## wherein R.sup.1 is aryl, andR.sup.2 is unsaturated heterocyclic group which contains at least one heteroatom selected from the group consisting of N, O and S, which may have one or more suitable substituent(s),or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 18, 1990
    Date of Patent: January 15, 1991
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Youichi Shiokawa, Atsushi Akahane, Hirohito Katayama, Takafumi Mitsunaga
  • Patent number: 4983623
    Abstract: The invention relates to derivatives of cyclic amino acids of the general formula ##STR1## in which R.sup.1 denotes hydrogen, alkyl, alkenyl or (subst.) aryl,R.sup.2 is hydrogen, alkyl, hydroxyl, alkoxy, (subst.) aryl, (subst.) aryloxy or (subst.) aroyl, or R.sup.1 and R.sup.2 together represent (subst.) benzylidene, or R.sup.1 and R.sup.2, together with the carbon atom carrying them, represent (subst.) cycloalkyl, R.sup.3 denotes hydrogen, hydroxymethyl, formyl, (subst.) alkenyl, (subst.) carboxycarbonyl, (subst.) carbamoylcarbonyl or (subst.) trifluoromethylcarbonyl, A represents a cyclic amino acid, X denotes oxygen, imino or N-alkylimino, m is 0-5 and n is 0 or 1, to a process for the preparation thereof, to agents containing them, and to the use thereof.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: January 8, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Hansjorg Urbach, Franz Hock
  • Patent number: 4980368
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is selected from C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-4 alkyl, COR.sub.8 where R.sub.8 is hydroxy, C.sub.1-6 alkoxy or NR.sub.9 R.sub.10 where R.sub.9 and R.sub.10 are independently hydrogen or C.sub.1-4 alkyl and CH.sub.2 OR.sub.11 and R.sub.11 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkanoyl;R.sub.5 is hydrogen, C.sub.1-6 alkyl or phenyl C.sub.1-4 alkyl;R.sub.6 is phenyl C.sub.1-7 alkyl in which the phenyl moiety is optionally substituted by one or two of halogen, ortho-nitro, meta- or para-methoxy, methyl or NR.sub.12 R.sub.13 wherein R.sub.12 and R.sub.13 are independently hydrogen or C.sub.1-6 alkyl or R.sub.12 and R.sub.13 together are C.sub.2-6 polymethylene or the phenyl moiety is 3,4-disubstituted by methylenedioxy or ethylenedioxy; andR.sub.7 is hydrogen or C.sub.
    Type: Grant
    Filed: December 23, 1986
    Date of Patent: December 25, 1990
    Assignee: Beecham-Wuelfing GmbH & Co. KG
    Inventors: Dietrich Thielke, Dagmar Hoeltje
  • Patent number: 4975439
    Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.
    Type: Grant
    Filed: September 2, 1988
    Date of Patent: December 4, 1990
    Assignee: Janssen Pharmaceutical N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn