Chalcogen Double Bonded Directly To A Ring Carbon Adjacent To The Ring Nitrogen (e.g., Caprolactam, Etc.) Patents (Class 540/485)
  • Publication number: 20010055798
    Abstract: A method of separating enantiomeric lactam esters. The lactam esters are contacted with a biocatalyst, such as an enzyme or a microorganism, in a solution wherein only one enantiomer is selectively hydrolyzed to give the optically active isomer of the corresponding acid. The hydrolysis product is then separated from the unreacted lactam esters. The enzyme is then recycled for reuse in the next enzymatic resolution. The undesired isomer is also racemized and reused in the next enzymatic resolution.
    Type: Application
    Filed: June 6, 2001
    Publication date: December 27, 2001
    Applicant: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Mahima Trivedi, Rolando E. Gapud, John S. Ng, Alok K. Awasthi, Ping T. Wang
  • Patent number: 6313109
    Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas Each of the R groups is defined in the disclosure.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: November 6, 2001
    Assignee: Societe de Conseils de Recherches d'Applications Scientifiques, Sas
    Inventor: Sun H. Kim
  • Patent number: 6284754
    Abstract: The invention relates to pharmaceutical compositions for topical application containing at least one physiologically active agent and an effective amount of 1-oleylazacycloheptan-2-one as the human or animal epithelial membrane permeability enhancer, to the application of such pharmaceutical compositions by means of locally contacting the skin or other membrane of the human or animal with the above composition and to the 1-oleylazacycloheptan-2-one compound per se.
    Type: Grant
    Filed: January 14, 1993
    Date of Patent: September 4, 2001
    Assignee: Schwarz Pharma AG
    Inventors: Henri Ernest Boddé, Johanna Aaltje Bouwstra, Maria Helène Ponec, Ferdinand Spies, Klaus Sandrock, Johannes Brussee
  • Patent number: 6262222
    Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: July 17, 2001
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
  • Patent number: 6242432
    Abstract: Compounds or compositions containing compounds of the formula A-(X1—NO2)to or salts thereof, for the preparation of antithrombotic medications wherein “to” is the integer 1 or 2X1 is an alkylene connecting bridge and “A” is the residue of timolol or analapril.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: June 5, 2001
    Assignee: Nicox S.A.
    Inventor: Piero del Soldato
  • Patent number: 6207644
    Abstract: The invention concerns pharmaceutically useful peptide derivatives of the formula (I), P—R1—R2—R3—R4, in which P, R1, R2, R3, and R4 have the various meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel peptide derivatives are of value in treating MHC class II dependent T-cell mediated autoimmune or inflammatory diseases, such as rheumatoid arthritis. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds in medical treatment.
    Type: Grant
    Filed: April 16, 1999
    Date of Patent: March 27, 2001
    Assignee: Zeneca Limited
    Inventors: Richard William Arthur Luke, Ronald Cotton
  • Patent number: 6194435
    Abstract: Novel lactams, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of Formula I below: are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Grant
    Filed: October 10, 1997
    Date of Patent: February 27, 2001
    Assignee: Cor Therapeutics, Inc.
    Inventors: Bing-Yan Zhu, Robert M. Scarborough
  • Patent number: 6156907
    Abstract: The invention relates on the one hand to a novel preparation of compounds of the formula (I) ##STR1## in which R.sub.1 is an aromatic or heteroaromatic radical, aromatic-aliphatic or heteroaromatic-aliphatic radical, a heterocyclic radical, a cycloaliphatic radical, a cycloaliphatic-aliphatic radical or an aliphatic radical,and on the other hand to novel compounds of the formula (I).
    Type: Grant
    Filed: January 8, 1999
    Date of Patent: December 5, 2000
    Assignee: Novartis AG
    Inventor: Robert Portmann
  • Patent number: 6077857
    Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: June 20, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
  • Patent number: 6051678
    Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.
    Type: Grant
    Filed: March 13, 1997
    Date of Patent: April 18, 2000
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
  • Patent number: 6013816
    Abstract: Process for the preparation of a linear .omega.-formyl-carboxylic acid or a corresponding linear formylnitrile compound starting from an internally unsaturated C.sub.4 -C.sub.12 carboxylic acid or a corresponding ester or nitrile by means of hydroformylation in the presence of carbon monoxide, hydrogen and a catalyst system, wherein the hydroformylation is carried out in an aqueous medium and in that the catalyst system comprises platinum and a water-soluble organic bidentate ligand.
    Type: Grant
    Filed: July 5, 1996
    Date of Patent: January 11, 2000
    Assignee: DSM NV
    Inventors: Onko J. Gelling, Imre Toth
  • Patent number: 5985815
    Abstract: New compounds useful as bleach activators as well as new percarboxylic acids, which may be formed as intermediates upon reaction of such activators with peroxygen bleach source in aqueous solution, include nitrogen-containing heterocyclic groups. Preferred activators are symmetrical derivatives of dibasic carboxylic acids, having N,N'diacyl N-heterocyclic groups usually lactams. They are produced by reaction of 2 moles of the lactam with one mole of dibasic acid chloride or anhydride.
    Type: Grant
    Filed: April 3, 1997
    Date of Patent: November 16, 1999
    Assignee: Warwick International Group Limited
    Inventors: John Townend, Jan Darrel Crowther
  • Patent number: 5981511
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: March 5, 1997
    Date of Patent: November 9, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Rolando E. Gapud, Timothy J. Hagen, Ann E. Hallinan, Donald W. Hansen, Jr., Robert E. Manning, Suzanne Metz, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, R. Keith Webber
  • Patent number: 5965576
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: October 12, 1999
    Assignee: Zeneca Limited
    Inventors: Ashokkumar Bhikkappa Shenvi, Robert Toms Jacobs, Scott Carson Miller, Cyrus John Ohnmacht, Jr., Chris Allan Veale
  • Patent number: 5945544
    Abstract: A process for producing an N-vinyllactam by reacting a lactam with acetylene in the presence of a particular catalyst (an alkali metal alcoholate between an alicyclic alcohol and an alkali metal) in a nonaqueous system at an acetylene partial pressure of 0 to 10 kg/cm.sup.2 .multidot.G.In the above process, the vinylation of lactam with acetylene is conducted at a low acetylene partial pressure in one step while the formation of by-product is kept minimum, whereby a high conversion and a high selectivity of lactam can be achieved.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: August 31, 1999
    Assignee: Maruzen Petrochemical Co., Ltd.
    Inventors: Hideki Ohmori, Toshiyuki Fukudome, Tomonori Hakozaki, Tomo Oikawa, Satoshi Kakuta, Hidenobu Oda
  • Patent number: 5945408
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: August 31, 1999
    Assignee: G.D. Searle & Co.
    Inventors: R. Keith Webber, Foe S. Tjoeng, Robert E. Manning
  • Patent number: 5928558
    Abstract: Selected derivatives of 1-oxyl-2,2,6,6-tetramethyl-4-aminopiperidine are surprisingly effective as inhibitors to prevent the premature polymerization of acrylic and methacrylic acids, their esters, their amides, vinyl acetate and acrylonitrile in the presence of water.
    Type: Grant
    Filed: April 23, 1998
    Date of Patent: July 27, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Glen T. Cunkle, Matthew E. Gande, Raymond Seltzer
  • Patent number: 5929067
    Abstract: 1-Aryl-2-acylaminoethane compounds of formula I ##STR1## wherein R.sub.1 -R.sub.4, X and Am are as defined in the description, have valuable pharmaceutical properties and are especially effective as NK-1 antagonists.
    Type: Grant
    Filed: August 21, 1997
    Date of Patent: July 27, 1999
    Assignee: Novartis AG
    Inventors: Marc Gerspacher, Andreas Von Sprecher, Silvio Roggo, Robert Mah, Silvio Ofner, Siem Jacob Veenstra, Claudia Betschart, Yves Auberson, Walter Schilling
  • Patent number: 5925754
    Abstract: This invention relates to a composition comprising (a) epsilon caprolactam and (b) one or more of 5-?4,5-di(3-carboxypropyl)-2-pyridyl!pentanoic acid or salt or amide, 4-?4,5-di(2-carboxypropyl)-2-pyridyl!-2-methylbutanoic acid or salt or amide, 2-?2-(2-carboxybutyl)-5-(1-carboxypropyl)-4-pyridyl!butanoic acid or salt or amide, 5-?3,5-di(3-carboxypropyl)-2-pyridyl!pentanoic acid or salt or amide, 4-?3,5-di(2-carboxypropyl)-2-pyridyl!-2-methylbutanoic acid or salt or amide, 2-?-2-(2-carboxybutyl)-5-(1-carboxypropyl)-3-pyridyl!butanoic acid or salt or amide, 5-amino-4-methylpentanamide, 4-amino-3-ethylbutanamide, 5-?4,5-di(4-hydroxybutyl)-2-pyridyl!pentanol, 4-?4,5-di(2-methoxypropyl)-2-pyridyl!-2-methylbutanol, 2-?2-(2-methoxybutyl)-5-(1-methoxypropyl)-4-pyridyl!butanol, 5-?3,5-di(4-hydroxybutyl)-2-pyridyl!pentanol, 4-?3,5-di(2-methoxypropyl)-2-pyridyl!-2-methylbutanol, 2-?2-(2-methoxybutyl)-5-(1-methoxypropyl)-3-pyridyl!butanol, 5-amino-4-methyl-1-pentanol, 5-imino-2-methyl-1-pentanamine, 5-amino-2-methyl-1-p
    Type: Grant
    Filed: October 23, 1997
    Date of Patent: July 20, 1999
    Assignee: Union Carbide Chemicals & Plastics Technology Corporation
    Inventors: John Michael Maher, David Robert Bryant, Johnathan Eugene Holladay, Thomas Carl Eisenschmid, John Robert Briggs, Kurt Damar Olson
  • Patent number: 5919927
    Abstract: A method of removing 1,11-diamino-6-undecanone from the pyrolysis product of nylon comprising: a) pyrolyzing nylon-6 to form a pyrolyzate containing a caprolactam mixture;b) dissolving the caprolactam mixture in a solvent to form a solution;c) passing carbon dioxide gas through the solution to form a precipitate;d) removing the precipitate from the solution; ande) recovering the purified caprolactam from the solution.
    Type: Grant
    Filed: April 9, 1998
    Date of Patent: July 6, 1999
    Assignee: Midwest Research Institute
    Inventor: Luc Moens
  • Patent number: 5856477
    Abstract: The azepine intermediates of the formula ##STR1## wherein R.sub.6 and R.sub.7 are other than hydrogen are disclosed. These intermediates can be reacted with acylmercaptocarboxylic acids of the formula ##STR2## to give the pharmaceutically active products.
    Type: Grant
    Filed: July 30, 1996
    Date of Patent: January 5, 1999
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jeffrey A. Robl
  • Patent number: 5856318
    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: January 5, 1999
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5847213
    Abstract: There is provided a process for producing a tertiary amine compound in one step without using any subsidiary raw material or any solvent, by subjecting a secondary amine compound and an alcohol to an intermolecular dehydration reaction in a gas phase. The process uses, as a catalyst, an oxide containing an alkali metal element and/or an alkaline earth metal element and silicon.
    Type: Grant
    Filed: March 3, 1997
    Date of Patent: December 8, 1998
    Assignee: Nippon Shokubai Co., Ltd.
    Inventors: Akira Kurusu, Yuuji Shimasaki
  • Patent number: 5750680
    Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.
    Type: Grant
    Filed: September 12, 1996
    Date of Patent: May 12, 1998
    Assignees: Hyundai Electronics Industries Co., Ltd., Korea Advanced Institute of Science & Technology
    Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
  • Patent number: 5719287
    Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: February 17, 1998
    Assignee: Eli Lilly and Company
    Inventors: Stephen W. Kaldor, Marlys Hammond
  • Patent number: 5708167
    Abstract: Proposed is a novel and very efficient method for the preparation of an N-vinyl compound such as N-vinyl-2-pyrrolidone and N-vinyl-N-ethyl acetamide by the thermal decomposition of an N-(.alpha.-acyloxyethyl) compound which is a novel compound obtained by the addition reaction between an NH group-containing compound such as 2-pyrrolidone and N-ethyl acetamide and a vinyl carboxylate, e.g., vinyl acetate, in the presence of an alkali, e.g. alkali metal hydroxide. The reaction mixture after completion of this addition reaction as such, i.e. without isolating the N-(.alpha.-acyloxyethyl) compound, such as N-(.alpha.-acetoxyethyl)-2-pyrrolidone and N-(.alpha.-acetoxyethyl)-N-ethyl acetamide, is heated to effect in situ formation of the desired N-vinyl compound which can then be isolated by distillation under reduced pressure in a very high overall yield.
    Type: Grant
    Filed: August 23, 1995
    Date of Patent: January 13, 1998
    Assignee: Shin-Etsu Vinyl Acetate Co., Ltd.
    Inventors: Yoshihiro Honma, Shozo Tanaka, Mitsuyoshi Oshima, Soji Tanioka, Fumiaki Kawamoto
  • Patent number: 5670639
    Abstract: N-Vinyllactams of the general formula I ##STR1## where n is from 1 to 3, are prepared by a process which comprises reaction of a lactam of the general formula II ##STR2## where n is from 1 to 3, with from 10 to 90 percent by weight of an aqueous alkali metal hydroxide solution with distillation at from 50.degree. to 250.degree. C. and from 1 to 100 mbar and with a residence time of from 0.1 to 5 hours and subsequent reaction with acetylene at from 60.degree. to 250.degree. C. and from 1 to 100 bar.
    Type: Grant
    Filed: March 13, 1996
    Date of Patent: September 23, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Martin Schmidt-Radde, Marc Heider, Albrecht Dams, Harald Rust
  • Patent number: 5663333
    Abstract: This invention relates to novel substituted caprolactams, including 4-azacaprolactams, and derivatives thereof which inhibit HIV protease and are useful for treatment of HIV disease. Also included in this invention are pharmaceutical compositions containing such caprolactams, and to methods of using such caprolactams for the treatment of HIV disease.
    Type: Grant
    Filed: March 30, 1993
    Date of Patent: September 2, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Carl Nicholas Hodge, Christina Howard Fernandez, Prabhakar Kondaji Jadhav, Patrick Yuk-Sun Lam
  • Patent number: 5635103
    Abstract: Improved cleaning and/or bleaching compositions including fabric laundry and bleaching compositions, automatic dishwashing compositions, hard surface cleaners, bleach additives and the like, suitable for domestic use, comprising improved bleach activators having particular alpha-modified lactam leaving groups leading to improved in-use performance of bleaching agents such as perborate even under wash conditions less alkaline than those typically encountered or when hydrogen peroxide source is at low levels in a cleaning operation. A preferred class of activators are N-acyl-3-morpholinone compounds with benzoyl being a preferred acyl group and N-Benzoyl-3-oxomorpholine being a highly preferred activator.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: June 3, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Alan D. Willey, Kevin L. Kott, Gregory S. Miracle, Eugene P. Gosselink, James C. T. R. B. St. Laurent
  • Patent number: 5635502
    Abstract: The present invention relates to certain novel mercaptoacetylamide bicyclic lactam derivatives useful as inhibitors of enkephalinase and of ACE.These mercaptoacetylamide bicyclic lactam derivatives can be described by the following formula: ##STR1## wherein R is hydrogen, a C.sub.1 -C.sub.4 alkyl, an Ar--Y--group, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3 or diphenylmethyl;R.sub.1 is hydrogen, acetyl, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3, benzoyl or a group of the formula ##STR2## R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, --CH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or an Ar--Y--group;A is --CH.sub.2 --, --O--, or --S--;B is --S--or --O--; andpharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 3, 1995
    Date of Patent: June 3, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: Gary A. Flynn
  • Patent number: 5633250
    Abstract: Disclosed us a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula 1.0.Further disclosed is a method of treating allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimers, Schizophrenia, and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: May 27, 1997
    Assignee: Schering Corporation
    Inventor: Neng-Yang Shih
  • Patent number: 5624953
    Abstract: This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.
    Type: Grant
    Filed: February 2, 1996
    Date of Patent: April 29, 1997
    Assignee: Eli Lilly and Company
    Inventors: Samantha J. Ambler, William F. Heath, Jr., Jai Pal Singh, Colin W. Smith, Lawrence E. Stramm
  • Patent number: 5608057
    Abstract: Proposed are an N-(.alpha.-acyloxyethyl) compound, e.g., (N-(.alpha.-acetoxyethyl)-2-pyrrolidone, which is a novel compound and can be converted into an industrially very important N-vinyl compound, e.g., N-vinyl-2-pyrrolidone, by a thermal decomposition reaction under relatively mild conditions as well as a method for the preparation of such an N-(.alpha.-acyloxyethyl) compound. The N-(.alpha.-acyloxyethyl) compound can be synthesized in a high yield by the addition reaction of an NH group-containing compound, e.g., 2-pyrrolidone, with a vinyl carboxylate, e.g., vinyl acetate, in the presence of an alkaline compound such as alkali metal hydroxides.
    Type: Grant
    Filed: August 23, 1995
    Date of Patent: March 4, 1997
    Assignee: Shin-Etsu Vinyl Acetate Co., Ltd.
    Inventors: Yoshihiro Honma, Shozo Tanaka, Mitsuyoshi Oshima, Soji Tanioka, Fumiaki Kawamoto
  • Patent number: 5536831
    Abstract: Caprolactam is obtained from caprolactam-containing polymers in the presence of a base under reduced pressure by depolymerizing polymers which contain the repeating unit --[--N(H)--(CH.sub.2).sub.5 --C(O)--] or mixtures consisting essentially offrom 50 to 99.99% by weight of a polymer containing the repeating unit --[--N(H)--(CH.sub.2).sub.5 --C(O)--]--from 0.01 to 50% by weight of additives selected from the group consisting of inorganic fillers, organic and inorganic pigments and dyes,from 0 to 10% by weight of organic and/or inorganic additives,from 0 to 40% by weight of non-polyamide-containing polymers andfrom 0 to 20% by weight of polyamides, with the exception of polycaprolactam and copolyamides prepared from caprolactam,in at least two depolymerization reactors connected in series.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: July 16, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Kopietz, Alan Handerman, Simon Jones, Ulrich Kalck, Claus-Ulrich Priester, Heinz Auer, Josef Ritz, Hugo Fuchs, Paul Pijl
  • Patent number: 5527926
    Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 18, 1996
    Assignee: Bracco International B.V.
    Inventors: Ramachandran S. Ranganathan, Radhakrishna K. Pillai
  • Patent number: 5514706
    Abstract: This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.
    Type: Grant
    Filed: November 21, 1994
    Date of Patent: May 7, 1996
    Assignee: Eli Lilly and Company
    Inventors: Samantha J. Ambler, William F. Heath, Jr., Jai P. Singh, Colin W. Smith, Lawrence E. Stramm
  • Patent number: 5495015
    Abstract: Caprolactam is obtained from caprolactam-containing polymers in the presence of superheated water by bringing polymers which contain the repeating unit--[--N(H)--(CH.sub.2).sub.5 --C(O)--]--or mixtures consisting essentially of______________________________________ from 40 to 99.9% by weight of a polymer containing the repeat- ing unit --[--N(H)--(CH.sub.2).sub.5 --C(O)--]--, from 0.01 to 50% by weight of additives selected from the group consisting of inorganic fillers, organic and inorganic pigments and dyes, from 0 to 10% by weight of organic and/or inorganic additives, from 0 to 40% by weight of non-polyamide-containing polymers and from 0 to 60% by weight of polyamides, with the exception of polycaprolactam and copolyamides prepared from caprolactam, ______________________________________into contact with superheated water at from 280.degree. to 320.degree. C. and from 7.5 to 15 MPa and a weight ratio of water to polymer containing the repeating unit --[--N(H)--(CH.sub.2).sub.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: February 27, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Bassler, Michael Kopietz
  • Patent number: 5462964
    Abstract: The present invention relates to the discovery of new C-terminal boronic acid dipeptide inhibitors of trypsin-like enzymes such as thrombin and pharmaceutical compositions thereof.
    Type: Grant
    Filed: October 20, 1993
    Date of Patent: October 31, 1995
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: John M. Fevig, Matthew M. Abelman, Eugene C. Amparo, Joseph Cacciola, Charles A. Kettner, Gregory J. Pacofsky, Chia-Lin Wang
  • Patent number: 5403843
    Abstract: A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R.sup.1 stands for an optionally substituted cyclic or chain-like group; COOR.sup.2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R.sup.1 denotes a moiety represented by the formula: ##STR2## wherein COOR.sup.16 and COOR.sup.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: April 4, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroshi Akimoto, Koichiro Ootsu, Fumio Itoh
  • Patent number: 5395974
    Abstract: The present invention relates to a method of reacting polyamides or mixtures thereof with ammonia to obtain a mixture of monomers. The reaction is carried out in the presence of certain Lewis Acid catalyst precursors.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: March 7, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Ronald J. McKinney
  • Patent number: 5378699
    Abstract: Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; and salts thereof.
    Type: Grant
    Filed: February 5, 1993
    Date of Patent: January 3, 1995
    Assignees: Lilly Industries Limited, Eli Lilly and Company
    Inventors: Michael Brunavs, Colin P. Dell, Peter T. Gallagher, William M. Owton, Jai P. Singh, Colin W. Smith
  • Patent number: 5376529
    Abstract: This invention relates to novel methods for the release of nucleic acids from cells in complex biological samples or specimens to prepare and make available the nucleic acid material present for a hybridization assay or for extraction. Novel methods for hybridization of nucleic acids are also presented. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with a hybridization medium comprising a lactam which promotes and enables nucleic acid pairing when complementary nucleic acid is introduced. The lactam is preferably about 5 to about 70% of the hybridization medium and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone.
    Type: Grant
    Filed: December 13, 1991
    Date of Patent: December 27, 1994
    Assignee: MicroProbe Corporation
    Inventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
  • Patent number: 5371238
    Abstract: A process for producing an azacycloalkane derivative represented by the following general formula (II): ##STR1## wherein m is an integer of from 1 to 3, n.sub.2 is an integer of from 2 to 10, andR represents an alkyl group having 3 to 12 carbon atoms,characterized by reacting a 1-(n-alkenyl)-azacycloalkan-2-one represented by the following general formula (I): ##STR2## wherein m is an integer of from 1 to 3, and n.sub.1 is an integer of from 0 to 8,with an alkyl mercaptan in the presence of a radical initiator in an organic solvent, treating the reaction mixture thus obtained with a reducing agent in a water-containing organic solvent, and then purifying the treated mixture by distillation.
    Type: Grant
    Filed: April 23, 1993
    Date of Patent: December 6, 1994
    Assignee: Hisamitsu Pharmaceutical Co., Inc.
    Inventors: Masaru Saita, Hisataka Inoue, Terumi Hachiya, Shigenori Yahiro, Kanji Noda
  • Patent number: 5359061
    Abstract: A process of using fast pyrolysis in a carrier gas to convert a plastic waste feedstream having a mixed polymeric composition in a manner such that pyrolysis of a given polymer to its high value monomeric constituent occurs prior to pyrolysis of other plastic components therein comprising: selecting a first temperature program range to cause pyrolysis of said given polymer to its high value monomeric constituent prior to a temperature range that causes pyrolysis of other plastic components; selecting a catalyst and support for treating said feed streams with said catalyst to effect acid or base catalyzed reaction pathways to maximize yield or enhance separation of said high value monomeric constituent in said temperature program range; differentially heating said feed stream at a heat rate within the first temperature program range to provide differential pyrolysis for selective recovery of optimum quantities of the high value monomeric constituent prior to pyrolysis of other plastic components; separating th
    Type: Grant
    Filed: October 27, 1992
    Date of Patent: October 25, 1994
    Assignee: Midwest Research Institute
    Inventors: Robert J. Evans, Helena L. Chum
  • Patent number: 5354761
    Abstract: Compounds of formula I ##STR1## wherein Y, Z, S, S', m, n and R.sub.1 -R.sub.4 are as defined in the description, have valuable pharmaceutical properties and are effective especially against protozoal infections. They are prepared in a manner known per se.
    Type: Grant
    Filed: June 1, 1993
    Date of Patent: October 11, 1994
    Assignee: Ciba-Geigy Corp.
    Inventors: Jaroslav Stanek, Giorgio Caravatti, Hans-Georg Capraro, Jorg Frei
  • Patent number: 5338861
    Abstract: Substituted lactams of the formula ##STR1## can be prepared from lactam N-carboxylates or lactim O-carboxylates of the formulae ##STR2## by thermal or mixed thermal and catalysed CO.sub.2 elimination at 80.degree.-450.degree. C. Lactams substituted on the N atom by aliphatic groups such as those produced herein are useful as industrial aprotic solvents.
    Type: Grant
    Filed: July 24, 1992
    Date of Patent: August 16, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Artur Botta, Hans-Josef Buysch, Otto Immel, Lothar Puppe
  • Patent number: 5308520
    Abstract: Various heterocyclic compounds have been discovered that impart improved fuel economy and friction modification to lubricant and fuel compositions. These heterocyclic compounds of the invention preferably contain nitrogen and may be further reacted with hydrocarbyl carboxylic acid acylating reactants or hydrocarbyl phenolic reactants to give higher molecular materials. These higher molecular weight materials have higher oil-solubility and impart dispersancy properties to lubricant and fuel compositions.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: May 3, 1994
    Assignee: The Lubrizol Corporation
    Inventors: Joseph W. Pialet, Paul E. Adams
  • Patent number: 5304552
    Abstract: Compounds characterized generally as piperidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is selected from a piperidinyl group, an isoindolyl group and an azabicyclononyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: April 19, 1994
    Assignee: G.D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Patent number: 5302756
    Abstract: Useful monomeric products are obtained in the reaction of nylon 6,6 with ammonia. Increased yield of monomer products from nylon 6,6 is obtained from ammonolysis when a mixture with nylon 6 is employed.
    Type: Grant
    Filed: December 23, 1992
    Date of Patent: April 12, 1994
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Ronald J. McKinney
  • Patent number: 5276165
    Abstract: A process for the preparation of N-substituted lactams of the formula I ##STR1## where Z is C.sub.2 - to C.sub.10 -alkylene, C.sub.7 - to C.sub.12 -aralkylene, phenylene or naphthylene, andR.sup.1 is C.sub.1 - to C.sub.20 -alkyl, C.sub.6 - to C.sub.10 -aryl or C.sub.7 - to C.sub.12 -aralkyl,by hydrogenating a compound of the formula II ##STR2## where W is C.sub.2 - to C.sub.10 -alkylene, C.sub.2 - to C.sub.10 -alkenylene, C.sub.7 - to C.sub.12 -aralkylene, phenylene or naphthylene, andX and Y together form an oxa or imido bridge of the formula ##STR3## or alternatively are identical or different and are hydroxyl, C.sub.1 - to C.sub.20 -alkoxy, C.sub.6 - to C.sub.10 -aryloxy or C.sub.7 - to C.sub.12 -aralkoxy, and, if X and Y are different, Y, in addition to the abovementioned meanings, may also be hydrogen,at superatmospheric pressure and at elevated temperature in the presence of a catalyst and in the presence of an amine, which comprises using a secondary and/or tertiary amine of the formula IIINH.sub.n R.
    Type: Grant
    Filed: November 25, 1992
    Date of Patent: January 4, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Juergen Weyer, Rolf Fischer