Diazoles (including Hydrogenated) Patents (Class 514/94)
  • Patent number: 6162820
    Abstract: Methods for removing parasites and in particular ectoparasites of vertebrates, in particular of mammals, and compositions for the implementation of this method.Methods for removing parasites of vertebrates, and in particular arthropods, mainly insects and Arachnida, wherein an effectively parasiticidal amount of a compound of formula (I) ##STR1## in particular of fipronil, is administered to the animal via an administration route which makes possible systemic distribution and good absorption.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: December 19, 2000
    Assignee: Merial
    Inventors: Philippe Jeannin, Marc Teichner, Philid Reid Timmons, Kenneth Anthony Kukorowski, Bruno Julia, Jean-Yves Vienot, Tai-Teh Wu
  • Patent number: 6121296
    Abstract: This invention is directed to transition-state analog compounds and to the use of said compounds as inhibitors of nucleoside hydrolase and transferase enzyme activity of parasites. This invention is further directed to the use of said compounds to treat infections and diseases caused by certain bacterial and plant toxins.
    Type: Grant
    Filed: February 2, 1998
    Date of Patent: September 19, 2000
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Benjamin Horenstein
  • Patent number: 5998390
    Abstract: Tissue-destructive conditions related to excess proteinase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amounts.
    Type: Grant
    Filed: September 28, 1998
    Date of Patent: December 7, 1999
    Assignee: The Research Foundation of State University of New York
    Inventors: Nungavarm S. Ramamurthy, Lorne M. Golub, Timo A. Sorsa, Olli P. Teronen, Tuula A. Salo
  • Patent number: 5998447
    Abstract: Compounds of the formula I ##STR1## in which B, D, E, R, W, Y, Z, b, c, d, e, f, g and have the meanings indicated in the claims, are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to the group of integrins. The invention relates to the use of compounds of the formula I, and of pharmaceutical preparations which contain such compounds, for the treatment and prophylaxis of diseases which are caused by an un desired extent of leucocyte adhesion and/or leucocyte migration or which are associated therewith or in which cell--cell or cell-matrix interactions play a part which are based on interactions of VLA-4 receptors with their ligands, for example of inflammatory processes, rheumatoid arthritis or allergic disorders, and it also relates to the use of compounds of the formula I for the production of pharmaceuticals for use in such diseases. It further relates to novel compounds of the formula I.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: December 7, 1999
    Assignee: Hoechst Aktiengesellschaft AG
    Inventors: Hans Ulrich Stilz, Volkmar Wehner, Christoph Huels, Dirk Seiffge
  • Patent number: 5972915
    Abstract: A pesticide comprising an active ingredient combination consisting ofa) tetrahydro-3,5-dimethyl-1,3,5-thiadiazine-2-thione of the formula ##STR1## and b) O-(O-ethyl-S-n-propylphosphoryl)-O-(N-methylcarbamoyl)pyrocatechol of the formula ##STR2## and/or c) O-ethyl S,S-dipropyl phosphorodithioate of the formula ##STR3## and/or d) 2-methyl-2-methylthiopropionaldehyde O-methylcarbamoyloxime of the formula ##STR4## and/or e) N,N-dimethyl-2-methylcarbamoyloximino-2-methylthioacetamide of the formula ##STR5## and/or f) ethyl-4-methylthio-m-tolylisopropylphosphoramide of the formula ##STR6## and/or g) (RS)-S-sec-butyl O-ethyl 2-oxo-1,3-thiazolidin-3-ylphosphono-thioate of the formula ##STR7## and/or h) 2,3-dihydro-2,2-dimethylbenzofuran-7-yl methylcarbamate of the formula ##STR8## and/or i) S-tert-butylthiomethyl O,O-diethyl phosphorodithioate of the formula ##STR9## and/or j) S,S-di-sec-butyl O-ethyl phosphorodithioate of the formula ##STR10## and/or k) (RS)-O-1-(4-chlorophenyl)pyrazol-4-yl O-ethyl S-propyl phosphoro
    Type: Grant
    Filed: October 9, 1997
    Date of Patent: October 26, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Hofmeister, Ulrich Neumann, Volker Harries, Jurgen von der Heyde, Manfred Schroeder, Jorn Tidow, Matthias Bratz, Karl-Friedrich Jager
  • Patent number: 5958905
    Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.
    Type: Grant
    Filed: March 26, 1996
    Date of Patent: September 28, 1999
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Erik Joel Verner
  • Patent number: 5952305
    Abstract: The invention involves a method for treating a human survivor of a heart attack and provides further improvement in survival following the heart attack by the early initiation and long-term administration of a renin-angiotensin system inhibitor, preferably an angiotensin converting enzyme inhibitor. The inhibitor may be used on its own, or in conjunction with other therapeutic compounds such as data blockers and thrombolytic agents. The preferred inhibitor is captopril.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 14, 1999
    Assignee: Brigham and Women's Hospital, Inc.
    Inventors: Marc A. Pfeffer, Janice M. Pfeffer, Eugene Braunwald
  • Patent number: 5914351
    Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: June 22, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
  • Patent number: 5880111
    Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 9, 1999
    Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
  • Patent number: 5856314
    Abstract: The present invention relates to thio-substituted, nitrogen-containing heterocyclic phosphonate compounds, including bisphosphonates, phosphonoalkylphosphinates, phosphonocarboxylates, and phosphonosulfonates, and the pharmaceutically-acceptable salts and esters thereof useful for the treatment and prevention of osteoporosis and arthritis. These compounds have the general structure: ##STR1## (a) Z is a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N, at least one of which is N;(b) Q is covalent bond; O, S, N, or NR.sub.1 ;(c) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is substituted or unsubstituted C.sub.1 -C.sub.8 alkyl;(d) each R1 is independently selected from --SR.sup.6 ; --R.sup.8 SR.sup.6 ; nil; hydrogen; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; unsubstituted or substituted aryl; hydroxy; --CO.sub.2 R.sup.3 ; --O.sub.2 CR.sup.3 ; --NR.sup.3.sub.2 ; --OR.sup.3 ; --C(O)N(R.sup.3).sub.2 ; --N(R.sup.
    Type: Grant
    Filed: May 9, 1994
    Date of Patent: January 5, 1999
    Assignee: The Procter & Gamble Company
    Inventors: Susan Mary Kaas, Frank Hallock Ebetino, Marion David Francis
  • Patent number: 5770586
    Abstract: The present invention relates to quaternary nitrogen-containing phosphate compounds, and the pharmaceutically-acceptable salts and esters thereof having the general structure: ##STR1## wherein: Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N;Y is N.sup.+ (R.sup.8).sub.2 or C(R.sup.1).sub.2 and when Y is C(R.sup.1).sub.2, at least one R.sup.2 must be N.sup.+ (R.sup.8).sub.3 ;R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10;R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbons atoms.The present invention further relates to pharmaceutical compostions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: June 23, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Frank Hallock Ebetino, Susan Mary Kaas, Marion David Francis, Dennis George Anthony Nelson, John Michael Janusz
  • Patent number: 5741784
    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; ....... 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: August 30, 1996
    Date of Patent: April 21, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
  • Patent number: 5731299
    Abstract: The present invention relates to phosphonsulfonates and the pharmaceutically-acceptable salts and esters thereof, having the following structure according to formula (I): ##STR1## The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention.
    Type: Grant
    Filed: May 7, 1993
    Date of Patent: March 24, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Frank Hallock Ebetino, Allan Vincent Bayless, Susan Mary Dansereau
  • Patent number: 5712396
    Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.
    Type: Grant
    Filed: July 5, 1994
    Date of Patent: January 27, 1998
    Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
  • Patent number: 5707978
    Abstract: Therapeutically active, heteroaryl-substituted deoxy glycero-phosphoethanolamines are disclosed having the general Formula I: ##STR1## wherein one of X, Y or Z is a fatty ether substituent, one is a heteroaryl ring substituent with 1-4 nitrogens as the only heteroatoms, one of which is bonded to a carbon of the glyceryl backbone, and one is a phosphoethanolamine substituent substituted at the nitrogen, provided that each of X, Y and Z is a different substituent, and the pharmaceutical compositions comprising the therapeutically active compounds and methods of using the therapetically active compounds to treat cancerous tumors, psoriasis and inflammation are also disclosed.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 13, 1998
    Assignee: Clarion Pharmaceuticals Inc.
    Inventors: Friedrich Paltauf, Albin Hermetter, Rudolf Franzmair
  • Patent number: 5705517
    Abstract: Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R' is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: January 6, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Kohei Nishikawa
  • Patent number: 5698541
    Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: December 16, 1997
    Assignee: Boehringer Mannheim GmbH
    Inventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
  • Patent number: 5691323
    Abstract: Compounds, 1,3-dihydro-1-{1-?piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: November 25, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Wayne J. Thompson, Michael F. Sugrue, Richard W. Ransom, Pierre J. Mallorga, Ian M. Bell, Anthony M. Smith
  • Patent number: 5665714
    Abstract: The present invention relates to novel, therapeutically active fatty alkyl and alkenyl ether glycerophospholipids bearing a 3-(2-imidazolinyl)-2-imidazolinyl or 2-imidazolinyl substituent on the ethanolamine nitrogen, methods of using the compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing same. The novel, therapeutically active compounds and salts of the invention possess anti-tumor, anti-psoriatic, anti-inflammatory, and anti-asthma activities.
    Type: Grant
    Filed: December 3, 1996
    Date of Patent: September 9, 1997
    Assignee: Clarion Pharmaceuticals Inc.
    Inventors: Friedrich Paltauf, Albin Hermetter, Rudolf Franzmair
  • Patent number: 5663053
    Abstract: Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme inhibits the production of these inflammatory mediators and will be of therapeutic utility in a broad range of allergic and inflammatory diseases and disorders. Compounds are described herein which inhibit the action of CoA-IT and are therefore useful in the treatment of disease states caused thereby.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: September 2, 1997
    Assignees: SmithKline Beecham Corporation, The Johns Hopkins University
    Inventors: James David Winkler, Deirdre Mary Bernadette Hickey, Floyd Harold Chilton, III
  • 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: 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: 5571792
    Abstract: Novel inhibitors of protein farnesyltransferase enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue proliferative diseases, including cancer and restenosis.
    Type: Grant
    Filed: June 30, 1994
    Date of Patent: November 5, 1996
    Assignee: Warner-Lambert Company
    Inventors: Gary L. Bolton, John C. Hodges, Michael W. Wilson
  • Patent number: 5545647
    Abstract: 3-Phenylpyrrolidine compounds of the formula ##STR1## effectively inhibit phosphodiesterase (PDE) IV activities and can be used as medicaments for conditions such as asthma.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: August 13, 1996
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Toshihiko Tanaka, Akihiro Yamamoto, Akira Amenomori
  • Patent number: 5543396
    Abstract: Peptidyl derivatives of diesters of .alpha.-aminoalkylphosphonic acids, particularly those with proline or related structures, their use in inhibiting serine proteases with chymotrypsin-like, trypsin-like, elastase-like, and dipeptidyl peptidase IV specificity and their roles as anti-inflammatory agents, anticoagulants, and anti-tumor agents.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: August 6, 1996
    Assignee: Georgia Tech Research Corp.
    Inventors: James C. Powers, Bogdan Boduszek, Jozef Oleksyszyn
  • Patent number: 5484780
    Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.
    Type: Grant
    Filed: December 14, 1994
    Date of Patent: January 16, 1996
    Assignee: Eli Lilly and Company
    Inventors: Donald B. Boyd, Kenneth L. Hauser, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Kumiko Takeuchi, K. Jeff Thrasher, Celia A. Whitesitt
  • 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: 5474974
    Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: December 12, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Kruger, Reiner Fischer, Heinz-Jurgen Bertram, Thomas Bretschneider, Stefan Bohm, Andreas Krebs, Thomas Schenke, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
  • Patent number: 5475016
    Abstract: Sulphonylbenzyl-substituted imidazolylpropenoic acid derivatives can be prepared by reacting sulphonylbenzyl-substituted aldehydes with appropriate CH-acidic compounds and then dehydrating.The sulphonylbenzyl-substituted imidazolylpropenoic acid derivatives can be used in medicaments, in particular for the treatment of high blood pressure and atherosclerosis.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: December 12, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Hanko, Jurgen Dressel, Peter Fey, Walter Hubsch, Thomas Kramer, Ulrich E. Muller, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Claudia Hirth-Dietrich, Andreas Knorr, Johannes-Peter Stasch, Stefan Wohlfeil, Ozkan Yalkinoglu
  • 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: 5441945
    Abstract: The heterocyclic iminobismethylenebisphosphonic acid derivatives of the general formula (I) ##STR1## wherein n is an integer of 0-5 and the group of the formula ##STR2## represents a 4-7 membered monocyclic or 7-11 membered condensed heterocyclic ring group which may be substituted by a halogen atom or a lower alkyl group and contains 1-2 nitrogen atoms their esters and salts thereof are described. The said compounds are useful as a bone resorption inhibitor, a dental calculus formation inhibitory agent or a polyvalent metal ion complex salt forming agent.
    Type: Grant
    Filed: April 13, 1994
    Date of Patent: August 15, 1995
    Assignee: Hoechst Japan Limited
    Inventor: Katsuhiro Yoshikawa
  • Patent number: 5436245
    Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##
    Type: Grant
    Filed: November 17, 1993
    Date of Patent: July 25, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Patent number: 5405841
    Abstract: The invention relates to new phosphorylated aza compounds, to processes for their preparation and to their use as pesticides, in particular as soil-acting insecticides and nematicide.The new compounds have the general formula (I) ##STR1## in which R.sup.1 -R.sup.5, X and Y are defined as in the specification, with the exception of compound O-ethyl S-propyl 3-(6-chloro-3-pyridinylmethyl)-2-nitroimino-imidazolidine-1-thiophosphate.
    Type: Grant
    Filed: November 30, 1993
    Date of Patent: April 11, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Jurgen Hartwig, Christoph Erdelen
  • Patent number: 5326776
    Abstract: Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.
    Type: Grant
    Filed: February 24, 1993
    Date of Patent: July 5, 1994
    Assignee: Abbott Laboratories
    Inventors: Martin Winn, Biswanath De, Thomas M. Zydowsky, Daniel J. Kerkman, John F. DeBernardis, Saul H. Rosenberg, Kazumi Shiosaki, Fatima Z. Basha, Kenneth P. Spina, Thomas W. von Geldern, Steven Boyd, Diane M. Yamamoto, Anthony K. L. Fung
  • Patent number: 5318980
    Abstract: Sulphonylbenzyl-substituted imidazoles can be prepared by first reacting imidazolylaldehydes with sulphonylbenzyl compounds and then oxidising or reducing the aldehyde function in the customary manner.The sulphonylbenzyl-substituted imidazoles can be used as active compounds in medicaments.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: June 7, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Hanko, Jurgen Dressel, Peter Fey, Walter Hubsch, Thomas Kramer, Ulrich E. Muller, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Claudia Hirth-Dietrich, Andreas Knorr, Johannes-Peter Stasch, Stefan Wohlfeil, Ozkan Yalkinoglu
  • Patent number: 5300494
    Abstract: The invention relates to a method for topical application of a pharmaceutically or therapeutically active agent through the use of a covalent chitosan derivative or chitosonium polymer. The present invention is particularly well suited for the topical delivery of pharmaceutically active quaternary ammonia compounds of the formula: ##STR1## wherein R is alkyl having between 5 and 11 carbon atoms.
    Type: Grant
    Filed: July 12, 1989
    Date of Patent: April 5, 1994
    Assignee: Union Carbide Chemicals & Plastics Technology Corporation
    Inventors: George L. Brode, II, George A. Salensky
  • Patent number: 5264426
    Abstract: The present invention relates to new phosphorylated diazacycloalkanes, to processes for their preparation, and to their use as pesticides, in particular as insecticides and nematicides. The new compounds have the general formula (I) ##STR1## in which R.sup.1 represents hydrogen, or represents alkyl, alkenyl or aryl, each of which is optionally substituted by halogen or alkoxy,A represents an alkanediyl radical which is optionally substituted by alkyl,R.sup.2 represents alkyl,R.sup.3 represents alkyl andR.sup.4 represents hydrogen, or represents alkyl, alkenyl or aryl, each of which is optionally substituted by halogen or alkoxy.
    Type: Grant
    Filed: September 18, 1992
    Date of Patent: November 23, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Sommer, Jurgen Hartwig
  • 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: 5210079
    Abstract: Substituted imidazoles such as 2-butyl-4-chloro-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]-5-(hydroxy methyl)imidazole and 2-butyl-4-chloro-1-[(2'-carboxybiphenyl-4-yl)-methyl]-5-(hydroxymethyl)imi dazole and pharmaceutically acceptable salts thereof are useful for treating chronic renal failure, mediated by angiotensin-II.
    Type: Grant
    Filed: February 7, 1992
    Date of Patent: May 11, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: David J. Carini, John Jonas V. Duncia, Pancras C. Wong
  • Patent number: 5190929
    Abstract: Cyclophosphamides possessing anti-tumor activity and having the formula ##STR1## and salts thereof; wherein R is lower alkyl, aryl, aryl-lower alkyl or a nitrogen, sulfur or oxygen containing heterocyclic or heterocyclic lower alkyl, andR' is hydrogen, hydroxy or OOH with the proviso that when R' is hydrogen, R is other than methyl or phenyl and when R' is hydroxy, R is other than methyl.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: March 2, 1993
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Gregory W. Canute
  • Patent number: 5190930
    Abstract: Araliphatylaminoalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is an aromatically substituted aliphatic radical, R.sub.2 is hydrogen or a monovalent aliphatic radical and alk is a divalent aliphatic radical, and their salts, exhibit a pronounced regulatory action on the calcium metabolism and can be used as medicaments for the treatment of diseases that are attributable to calcium metabolsim disorders. They are prepared, for example, by reacting a compound of formula ##STR2## wherein X.sub.3 is carboxy and R.sub.0 is a radical R.sub.2, with phosphorous acid and phosphorus trichloride and hydrolysing the primary product.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • 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: 5158967
    Abstract: 7-Oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs are provided which are thromboxane A.sub.2 (TXA.sub.2) receptor antagonists or combined thromboxane A.sub.2 receptor antagonist/thromboxane synthetase inhibitors and have the structural formula ##STR1## wherein R is SO.sub.3 H, P(O)OR.sup.3 OH or P(O)R.sup.4 OH, X is O or NH, and Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein.
    Type: Grant
    Filed: June 12, 1991
    Date of Patent: October 27, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Steven E. Hall
  • 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: 5155118
    Abstract: Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: October 13, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: David J. Carini, John J. V. Duncia, Pancras C. B. Wong
  • Patent number: 5153197
    Abstract: Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: October 6, 1992
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: David J. Carini, John J. V. Duncia
  • 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: 5145990
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.
    Type: Grant
    Filed: January 9, 1991
    Date of Patent: September 8, 1992
    Assignee: Merck & Co., Inc.
    Inventors: William H. Parsons, William R. Schoen, Arthur A. Patchett
  • Patent number: 5140019
    Abstract: Compositions which contain, as the active ingredients, a combination of heterocyclic compounds of the general formula (I) and organophosphorous compounds, in addition to one or more compounds having a polyethyleneglycol or polypropyleneglycol chain or an ethyleneglycol-propyleneglycol copolymeric chain, or a mixture of these compounds which results in a stabilization of the active ingredients without any adverse influences on the physical properties of the formulations.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: August 18, 1992
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Yuzuru Wada, Shigeharu Koyama