Chalcogen In The Six-membered Hetero Ring Patents (Class 514/90)
  • Patent number: 5627173
    Abstract: Phosphonoacetic acid derivatives and their use for treating degenerative joint disorders Compounds of the formula I ##STR1## are suitable for producing pharmaceuticals for the treatment and prophylaxis of degenerative joint disorders, of rheumatic disorders accompanied by cartilage breakdown, such as rheumatoid arthritis, joint trauma and chondrolysis as a consequence of prolonged immobilization of the joint, of inflammations, septic shock, disorders with impaired leukocyte adhesion, disorders caused by an elevated concentration of tumor necrosis factor alpha, such as cachexia or Crohn's disease.
    Type: Grant
    Filed: January 23, 1996
    Date of Patent: May 6, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf Graeve, Werner Thorwart, Ruth Raiss, Klaus U. Weithmann, Stefan M ullner
  • Patent number: 5622917
    Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.
    Type: Grant
    Filed: January 3, 1995
    Date of Patent: April 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5587375
    Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: December 24, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventor: Jeffrey A. Robl
  • Patent number: 5580863
    Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.
    Type: Grant
    Filed: May 13, 1994
    Date of Patent: December 3, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
  • Patent number: 5556614
    Abstract: This invention provides a deodorant composition comprising a phosphoric diester compound of the following formula or a pharmacologically acceptable salt thereof as an active deodorant ingredient. ##STR1## (wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group).The deodorant composition of this invention has a potent deodorizing action and yet does not stimulate the mucosa of the eye, nose and throat. Therefore, it can be used in various industrial and household applications.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: September 17, 1996
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Osamu Kawahira
  • Patent number: 5556841
    Abstract: This invention relates to the compounds of the formula [I] which are useful for the treatment of cataracts, and the synthetic intermediates of the formula [II], ##STR1## wherein R.sup.1 is hydroxy which can be protected by a hydroxy protective group;R.sup.2 is lower alkyl;R.sup.3 is hydrogen, lower alkyl, hydroxy, which can be protected by a hydroxy protective group, or lower alkoxy, and the said lower alkyl can be substituted by hydroxy, which can be protected by a hydroxy protective group, amino or lower alkylamino;R.sup.4 is carboxy which can be converted into ester or amide; tetrazolyl; phosphono which can be converted into ester or amide; or sulfonyl which can be converted into ester or amide;R.sup.5 is cyano or lower alkoxy;A is alkylene;B is C.dbd.O, C.dbd.S or CH.sub.2, andis single bond or double bond.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: September 17, 1996
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Yoichi Kawashima, Atsutoshi Ota, Hiroyuki Mibu
  • Patent number: 5547952
    Abstract: This invention relates to the compounds of the formula [I] which are useful for the treatment of cataracts, and the synthetic intermediates of the formula [II], ##STR1## wherein R.sup.1 is hydroxy which can be protected by a protective group;R.sup.2 is lower alkyl;R.sup.3 is hydrogen, lower alkyl, hydroxy, which can be protected by a protective group, or lower alkoxy, and the said lower alkyl can be substituted by hydroxy, which can be protected by a protective group, amino or lower alkylamino;R.sup.4 is tetrazolyl, phosphonol or lower alkyl ester thereof, or sulfonyl or lower alkyl ester thereof, andA is alkylene.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: August 20, 1996
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Yoichi Kawashima, Atsutoshi Ota, Yuko Morikawa, Hiroyuki Mibu
  • Patent number: 5489580
    Abstract: Novel compounds and use therefor in treating neoplastic and immune system disorders are disclosed. The compound of the present invention comprises a substituted lysophospholipid, which includes a C12 to C20 alkyl ether, a C12 to C20 thioether, or a substituted C3 to C6 heterocycle containing at least two ring heteroatoms, selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof; and also includes a choline group or a C4 to C7 heterocycle containing heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof.The method for treating neoplastic or immune system disorders includes administering an effective dose of a compound of the present invention in a therapeutic manner. Effective doses of these compounds result in cytotoxic effects upon various leukemic cell lines.The compounds of this invention have the advantage that these compounds possess antineoplastic and immunomodulatory characteristics.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: February 6, 1996
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Richard I. Duclos, Jr., Donna J. Fournier
  • Patent number: 5476847
    Abstract: Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R.sub.1 and R.sub.2 form a cycloalkyl ring of 3-8 members and R.sub.3 and R.sub.4 are as defined; or R.sub.3 and R.sub.4 form a cycloalkyl ring of 3-7 members and R.sub.1 and R.sub.2 are as defined; or R.sub.1 and R.sub.2 together, and R.sub.3 and R.sub.4 together, each form a cycloalkyl ring;R.sub.5 is --OR.sub.9 or --NHR.sub.9, wherein R.sub.9 is hydrogen or alkyl;n is 0 or 1;A.sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A.sub.1 and R.sub.5 together form a radical of an .alpha.-aminoacyl derivative; andR.sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or --A.sub.2 --R.sub.
    Type: Grant
    Filed: June 29, 1994
    Date of Patent: December 19, 1995
    Assignee: Schering Corporation
    Inventors: Brian A. McKittrick, Michael F. Czarniecki, Samuel Chackalamannil, Shin Chung, Shawn DeFrees, Andrew W. Stamford
  • Patent number: 5472956
    Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: December 5, 1995
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, James P. Schmidt
  • Patent number: 5447712
    Abstract: A method is provided for reducing side effects caused by chemotherapeutic agents by administering to a patient in need thereof a therapeutically effective amount of a composition including L-2-oxothiazolidine-4-carboxylate specifically for reducing hemorrhagic cystitis in a patient at risk of same.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: September 5, 1995
    Assignee: Free Radical Sciences
    Inventors: Randy D. White, Joseph A. Safron, Donovan E. Gordon, Deborah Rice
  • Patent number: 5432168
    Abstract: Prostate cancer particularly hormone-unresponsive metastatic prostate cancer, is treated by cyclophosphamide or other normally substantially inactive agent. Potentiation of the anti-cancer activity and amelioration of cyclophosphamide-associated toxicity is achieved by an initial intravenous infusion of DPPE over an approximately one hour period prior to cyclophosphamide treatment.
    Type: Grant
    Filed: December 27, 1993
    Date of Patent: July 11, 1995
    Assignee: University of Manitoba
    Inventor: Lorne J. Brandes
  • Patent number: 5418223
    Abstract: A process for preparing a pharmaceutical preparation consisting essentially of a lyophilized cake of cyclophosphamide monohydrate and a bulking agent which comprises freezing cyclophosphamide, a bulking agent, and water, lyophilizing part of the water, obtaining and melting a supersaturated cyclophosphamide-bulking agent solution, precipitating cyclophosphamide as a hydrated polymorph, refreezing the solution and lyophilizing the water not bound to cyclophosphamide or the bulking agent.
    Type: Grant
    Filed: April 22, 1994
    Date of Patent: May 23, 1995
    Assignee: Erbamont, Inc.
    Inventors: Nageswara R. Palepu, Tomaz R. Herzyk
  • Patent number: 5413994
    Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: May 9, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • Patent number: 5304550
    Abstract: Compounds of the formula (I): ##STR1## in which the nitrogen-containing hetero ring portion is 1,4-dihydropyridine ring or a pyridine ring, R.sup.1 is only present when the nitrogen-containing hetero ring is a 1,4-dihydropyridine ring, and Z is a group of the formula (II): ##STR2## in which R.sup.4 and R.sup.5 may be the same or different and together may form one divalent group, are effective agents for enhancing the antitumor effect of antitumor drugs.
    Type: Grant
    Filed: May 7, 1993
    Date of Patent: April 19, 1994
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Shin-ichi Akiyama, Ryozo Sakoda, Kiyotomo Seto, Norimasa Shudo
  • 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: 5250522
    Abstract: The present invention relates to the N-phosphonomethyl-biaryl substituted amino acid derivatives of formula I ##STR1## wherein X represents a direct bond, C.sub.1-4 -alkylene or C.sub.2 -C.sub.4 -alkenylene; R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, .alpha.-(trichloromethyl, carboxyl, esterified carboxyl or amidated carboxyl)substituted-(lower alkyl or aryl-lower alkyl), acyloxymethyl optionally monosubstituted on methyl carbon by C.sub.1-20 -alkyl, by C.sub.5 -C.sub.7 -cycloalkyl, by aryl or by aryl-lower alkyl; R.sub.1 represents monocyclic carbocyclic or monocyclic heterocyclic aryl; COR.sub.3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; R.sub.2 and R.sub.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: October 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Stephane De Lombaert
  • Patent number: 5234917
    Abstract: Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.
    Type: Grant
    Filed: November 30, 1990
    Date of Patent: August 10, 1993
    Inventors: Joseph A. Finkelstein, Judith Hempel, Richard M. Keenan, James Samanen, Joseph Weinstock
  • Patent number: 5229375
    Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: July 20, 1993
    Assignee: Scripps Clinic and Research Foundation
    Inventors: Peter E. Maligres, Kyriacos C. Nicolaou
  • Patent number: 5227506
    Abstract: The invention relates to acyloxymethyl esters of bisphosphonic acids, halo-bisphosphonic acids and hydroxy-bisphosphonic acids which exhibit oral bioavailability and are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.
    Type: Grant
    Filed: July 12, 1990
    Date of Patent: July 13, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Walfred S. Saari, Paul S. Anderson
  • Patent number: 5196434
    Abstract: Compound of general formula (I): ##STR1## where R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description.Medicinal products.
    Type: Grant
    Filed: September 26, 1991
    Date of Patent: March 23, 1993
    Assignee: Adir et Compagnie
    Inventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
  • Patent number: 5185334
    Abstract: Novel 2,2-disubstituted glycerol-like compounds are disclosed for use as anti-allergic and anti-inflammatory compounds. The compounds are antagonists of platelet activating factor ("PAF"). Also disclosed are methods of synthesizing and using the compounds of the invention as well as pharmaceutical compositions thereof. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: February 9, 1993
    Assignee: Schering Corporation
    Inventors: Daniel Solomon, James J. Kaminski, Steven K. White, Laura S. Lehman de Gaeta, Ashit K. Ganguly
  • Patent number: 5164381
    Abstract: 1,5-Diaryl-3-substituted pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.
    Type: Grant
    Filed: July 12, 1991
    Date of Patent: November 17, 1992
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael P. Wachter, Michael P. Ferro
  • Patent number: 5157025
    Abstract: A method is provided for lowering serum cholesterol and thereby inhibiting fatty streak lesions of atherosclerosis by administering to a patient a phosphorus-containing ACE inhibitor, such as fosinopril or ceronapril, alone or in combination with a cholesterol lowering drug, such as pravastatin.
    Type: Grant
    Filed: April 1, 1991
    Date of Patent: October 20, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: A. K. Gunnar Aberg, Mark Kowala, Patricia Ferrer
  • Patent number: 5155100
    Abstract: The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.
    Type: Grant
    Filed: May 1, 1991
    Date of Patent: October 13, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Mark D. Erion, Stephane De Lombaert
  • Patent number: 5153179
    Abstract: A composition useful as a medicament with improved penetration of cell membranes comprising an active material and a compound of general formula: ##STR1## wherein either residue R.sub.1 or R.sub.2 is an alkyl, alkylene, alkynyl or alkoxy group of 3-7 carbon atoms, and the other residue is a hydrogen atom, together with pharmaceutical additives and dilution agents.
    Type: Grant
    Filed: April 22, 1991
    Date of Patent: October 6, 1992
    Assignee: Max-Planck-Gesellschaft zur Foerderung der Wissenschaft e.V.
    Inventor: Hansjorg Eibl
  • Patent number: 5147865
    Abstract: The invention relates to new phosphonopyrrolidine- and piperidine-containing pseudopeptides, to a process for their preparation and to their use as medicaments, in particular as antiviral agents in human and veterinary medicine.
    Type: Grant
    Filed: August 15, 1991
    Date of Patent: September 15, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Habich, Jutta Hansen, Arnold Paessens
  • Patent number: 5130303
    Abstract: Compounds of the formula (I): ##STR1## in which the nitrogen-containing hetero ring portion is a 1,4-dihydropyridine ring or a pyridine ring, R.sup.1 is only present when the nitrogen-containing hetero ring is a 1,4-dihydropyridine ring, and Z is either a CO.sub.2 R.sup.8 group or a group of the formula (II): ##STR2## in which R.sup.4 and R.sup.5 may be the same or different and together may form one divalent group, are effective agents for enhancing the antitumor effect or antitumor drugs.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: July 14, 1992
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Shin-ichi Akiyama, Ryozo Sakoda, Kiyotomo Seto, Norimasa Shudo
  • Patent number: 5128330
    Abstract: A new class of phosphines in which the phosphorous atom is bonded directly to the carbon of an oxazinone: ##STR1## In addition to their anti-inflammatory activity, these phosphines are useful as intermediates in producing compounds where the phosphine is replaced by a benzylidine, compounds which have also been proven useful in the treatment of inflammation and other conditions associated with arthritis.
    Type: Grant
    Filed: February 19, 1991
    Date of Patent: July 7, 1992
    Assignee: Biofor, Ltd.
    Inventor: Sung J. Lee
  • Patent number: 5075293
    Abstract: O,S-Dialkyl ((nitrogen heterocyclyl)carbonyl)-phosphoramidothioates are prepared by the reaction of O,S-dialkyl phosphoroisocyanatidothioates with selected 5 and 6 membered nitrogen heterocycles, such as thiomorpholine and tetrahydroquinoline, and found to be effective plant systemic and contact insecticides. O,S-dimethyl ((4-thiomorpholinyl)carbonyl)phosphoramidothioate, for example, is prepared from O,S-dimethyl phosphoroisocyanatidothioate and thiomorpholine and found to control aster leafhopper when applied to rice plants.
    Type: Grant
    Filed: October 10, 1989
    Date of Patent: December 24, 1991
    Assignee: The Dow Chemical Company
    Inventors: Walter Reifschneider, Barat Bisabri-Ershadi, James E. Dripps, J. Brian Barron
  • Patent number: 5045530
    Abstract: A pharmaceutical preparation is disclosed which is made up of a micelle or a vesicle each consisting of a cationic tenside with a monovalent ion and a hydrophobic cyclic or linear peptide, dispersed in a solvent whose pH value lies between pH 7-pH 8, the critical micellization concentration (cmc) lying in the range of 1.0.10.sup.-7 to 7.0.10.sup.-5 mol/liter. The preparations disclosed have in particular the advantage that by the increasing of the hydrophobicity of the alkyl or aryl chain or the radical at the N.sup.+ tenside both the membrane permeability is increased and furthermore the pharmaceutical active substance, in particular linear and cyclic tyrocidines (A-J), can be transferred actively into the cytosol. They thus act on the transciption level. In addition, linear and cyclic tyrocidines in particular have antiviral effects.
    Type: Grant
    Filed: April 27, 1989
    Date of Patent: September 3, 1991
    Assignee: Medici Chem.-Pharm. Fabrik Putter GmbH
    Inventor: Henrich H. Paradies
  • Patent number: 5036152
    Abstract: Novel alkoxycarbonylalkylphospholipids, alkylaminocarbonylalkylphospholipids, processes for the preparation thereof, and methods for treating inflammation utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: September 5, 1989
    Date of Patent: July 30, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, Kirk D. Shoger, John J. Tegeler
  • Patent number: 5002937
    Abstract: The present invention provides compounds of the formula: ##STR1## The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them useful in treatment and prophylaxis of disorders of calcium metabolism.
    Type: Grant
    Filed: July 5, 1989
    Date of Patent: March 26, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elmar Bosies, Harald Zilch
  • Patent number: 4997822
    Abstract: There are disclosed compounds of the formula ##STR1## The compounds have antitumour and AIDS treatment activity.
    Type: Grant
    Filed: February 20, 1987
    Date of Patent: March 5, 1991
    Assignee: Asta Pharma Aktiengesellschaft
    Inventors: Hans-Jurgen Hohorst, Ludmilla Bielicki, Georg Voelcker, Ulf Niemeyer
  • Patent number: 4971957
    Abstract: Novel carboxamide compounds represented by the general formula (I) possess excellent activities for lowering lipids and thus they are useful as agents for treating and preventing various diseases (hyperlipidemia) such as hypercholesterolemia, hypertriglyceridemia, hyperphospholipidemia, hyperlipacidemia, and the like.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: November 20, 1990
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Kazuhiko Tsutsumi, Eiji Uesaka, Kayoko Shinomiya, Yoshihiko Tsuda, Yauso Shoji, Atsushi Shima
  • Patent number: 4940706
    Abstract: The present invention describes novel 2,4-disubstituted 1,3-dioxolanes having the formula I ##STR1## wherein R.sup.1 represents a long chain alkyl group; X is a covalent single bond, a carbonyl group, a carboxyl group, a carbamoyl group or a --O--P(.dbd.O)(O.sup.z)-- group; z is a negative charge (-) when q is zero, or z is an hydrogen atom when q is one; n is an integer from 2 to 10; R.sup.2, R.sup.3 and R.sup.4 are lower alkyl groups, or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents an aromatic cyclic ammonium group or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents a non-aromatic cyclic ammonium group in which two of the groups (R.sup.2, R.sup.3 or R.sup.4) form a non-aromatic ring together with the quaternary nitrogen atom; and A.sup.- is a pharmaceutically acceptable anion. These compounds are in vitro inhibitors of the platelet aggregation induced by the platelet activating factor (PAF) and, thus, useful for the treatment of the diseases in which this substance is involved.
    Type: Grant
    Filed: October 13, 1988
    Date of Patent: July 10, 1990
    Assignee: J. Uriach & Cia, S.A.
    Inventors: Javier Bartroli, Manuel Anquita, Elena Carceller
  • Patent number: 4937237
    Abstract: Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: June 26, 1990
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4908356
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 may be the same of different and are each independently hydrogen or lower alkyl which may be unsubstituted or monosubstituted with halogen, lower alkoxy or hydroxy with the proviso that the substituent is not the .alpha.-carbon or R.sup.1 and R.sup.2 taken together with the carbon to which they are attached form a morpholino ring;each R.sup.3 is independently hydrogen, lower alkyl, carboxy or carbalkoxy;n is an integer from 0, 1, 2 or 3 andR is hydrogen, lower alkyl, cycloalkyl, arylalkyl aryl or a nitrogen, sulfur or oxygen containing heterocyclic or a heterocyclic lower alkyl and pharmacuetically acceptable salts thereof.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: March 13, 1990
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Ronald R. Valente
  • Patent number: 4891362
    Abstract: Novel substituted N-alkyl-N-alkoxyamidophosphonates or -thiophosphonates and N-alkyl-N-alkoxyamidophosphates or -thiophosphates of formula ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy,R.sub.1 and R.sub.3 are each independently of the other C.sub.1 -C.sub.4 alkyl,R.sub.2 is hydrogen, C.sub.4 -C.sub.4 alkyl, or when taken together with R.sub.1, forms the radical --(CH.sub.2).sub.4 --; andX and Y are each independently of the other oxygen or sulfur, with the proviso that at least one of X or Y is sulfur if R.sub.2 is hydrogen.The preparation of these compounds is described, as well as the use thereof in pest control, especially for controlling insects and representatives of the order Acarina.
    Type: Grant
    Filed: June 27, 1988
    Date of Patent: January 2, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Odd Kristiansen
  • Patent number: 4882319
    Abstract: Invented are phosphonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: November 21, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4870065
    Abstract: The present invention relates to novel compounds of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and stand for alkyl having 1 to 4 carbon atoms optionally substituted by one or more halogen atoms, alkenyl having 2 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl or lower alkoxy-alkyl group,R.sub.3 stands for alkyl having 1 to 6 carbon atoms or alkenyl having 2 to 6 carbon atoms,R.sub.4 and R.sub.5 are the same or different and represent hydrogen, alkyl having 1 to 6 carbon atoms, alkenyl having 2 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl, benzyl, phenyl substituted by one or more alkyl having 1 to 3 carbon atoms and/or by one or more halogen atoms, lower alkoxy-alkyl, a group of the formula --(CH.sub.2).sub.n --R.sub.6, wherein n is an integer between 0 to 3 and R.sub.
    Type: Grant
    Filed: September 26, 1985
    Date of Patent: September 26, 1989
    Assignee: Eszakmagyarorszagi Vegyimuvek
    Inventors: Karoly Balogh, Zsolt Dombay, Karoly Fodor, Gregna nee ToErzsebet, Erno Lorik, Magdolna Magyar nee Tomorkenyi, Jozsef Nagy, Karoly Pasztor, Pal Santha, Gyula Tarpai, Istvan Toth, Eszter Urszin nee Simon
  • Patent number: 4849414
    Abstract: Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: May 20, 1987
    Date of Patent: July 18, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Melanie J. Loots, Donald S. Karanewsky
  • Patent number: 4804654
    Abstract: Compounds of the formula ##STR1## wherein the symbols have assigned meanings, and their use as insecticides and/or miticides.
    Type: Grant
    Filed: March 4, 1987
    Date of Patent: February 14, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Mohamed A. H. Fahmy
  • Patent number: 4742060
    Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
    Type: Grant
    Filed: January 21, 1986
    Date of Patent: May 3, 1988
    Assignee: Nihon Tokushu Noyaku Seizo K. K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
  • Patent number: 4681874
    Abstract: Novel thiazinephosphonic acid derivatives (I): ##STR1## wherein R.sup.1 and R.sup.2 each is lower alkoxy, lower alkynyloxy, lower alkylthio, arylthio (e.g., monocyclic aromatic group), or lower alkylamino; R.sup.3 and R.sup.4 each is hydrogen or lower alkyl; R.sup.5, R.sup.6, and R.sup.7 each is hydrogen, lower alyl, lower alkoxy, halogen, or trifluoromethyl; and X is oxygen or sulfur, are disclosed. A method for the production thereof, and pesticides comprising said compounds (I) are provided.
    Type: Grant
    Filed: September 6, 1985
    Date of Patent: July 21, 1987
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yoshio Hayase, Mitsuhiro Ichinari, Junji Taguchi, Takeo Ishiguro, Toshio Takahashi
  • Patent number: 4656163
    Abstract: The present invention relates to the use of the sulphenic acid amides of the general formula (I) ##STR1## in which X represents identical or different halogen atoms,Y.sup.1 and Y.sup.2 are identical or different and represent hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or NO.sub.2 andZ represents halogen, --OH, --NHOH or the group --OR.sup.1,in whichR.sup.1 denotes optionally substituted radicals from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aryl, aralkyl and heterocyclyl, orZ represents the group ##STR2## in which R.sup.2 and R.sup.3 are identical or different and denote hydrogen or a heterocyclic radical, orZ represents the group --OMin which M denotes ammonium or the equivalent of an alkali metal, alkaline earth metal or heavy metal cation, for prolonging the duration of a high activity in agents for combating soil pests.
    Type: Grant
    Filed: November 14, 1985
    Date of Patent: April 7, 1987
    Assignees: Bayer Aktiengesellschaft, Mobay Corporation
    Inventors: John Anderson, Bernhard Homeyer, Engelbert Kuhle, Hans Scheinpflug, Walter M. Zeck, Donald E. Simonet
  • Patent number: 4650791
    Abstract: A novel phospholipid of the formula: ##STR1## wherein R.sup.1 is an alkyl group of 10 to 24 carbon atoms, R.sup.2 is a cyclic imide group and A.sup.+ is a cyclic ammonio group and a salt thereof have platelet activating factor inhibiting activity and are useful for prevention and treatment of circulatory disorders and allergic bronchial asthma.
    Type: Grant
    Filed: January 8, 1985
    Date of Patent: March 17, 1987
    Assignee: Takedo Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
  • Patent number: 4629491
    Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more diaminophosphinyl compounds having oxidized sulfur functions, and methods and composition for inhibiting the activity of urease through use of such compounds.
    Type: Grant
    Filed: December 20, 1983
    Date of Patent: December 16, 1986
    Assignee: Allied Corporation
    Inventors: Michael D. Swerdloff, Milorad M. Rogic, Larry L. Hendrickson
  • Patent number: 4624695
    Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more o-diaminophosphinyl derivatives of oximes, and methods and composition for inhibiting the activity of urease through use of such compounds.
    Type: Grant
    Filed: December 20, 1983
    Date of Patent: November 25, 1986
    Assignee: Allied Corporation
    Inventors: Michael D. Swerdloff, Milorad M. Rogic, Larry L. Hendrickson
  • Patent number: 4617295
    Abstract: Oxime N-alkyl-N-.alpha.-(alkylthio-phosphorothio)acyl carbamates represented the structure: ##STR1## wherein the R represents various imino radicals, Q is oxygen or sulfur and the numbered R groups represent various alkyl substituents, which exhibit superior insecticidal and miticidal activity.
    Type: Grant
    Filed: October 3, 1985
    Date of Patent: October 14, 1986
    Assignee: Union Carbide Corporation
    Inventor: Themistocles D. J. D'Silva