Patents Examined by Mark W. Russell
  • Patent number: 5234946
    Abstract: The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R.sup.1 represents (a) substituted or unsubstituted C.sub.2-6 alkenyl group, (b) substituted or unsubstituted C.sub.3-6 cycloalkenyl group, (c) substituted or unsubstituted C.sub.2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru.sup.11 -Ar wherein R.sup.11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; ##STR2## represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R.sup.7,X and Y are linking groups,R.sup.2 is H or lower alkyl,R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl,R.sup.4 and R.sup.5 are independently hydrogen or halogen atoms,R.sup.
    Type: Grant
    Filed: August 30, 1991
    Date of Patent: August 10, 1993
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
  • Patent number: 5232948
    Abstract: Monocyclic aryl compounds having selective LTB.sub.4 antagonists properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, therapeutic compositions and methods of treatment of disorders which result from LTB.sub.4 activity using the monocyclic aryl compounds are disclosed.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: August 3, 1993
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Fu-Chih Huang, Wan K. Chan, Charles A. Sutherland, Robert A. Galemmo, Jr., Michael N. Chang
  • Patent number: 5230882
    Abstract: Liposomes suitable as ultrasound contrast agents which contain media of various types including gases, gaseous precursors activated by pH, temperature or pressure, as well as other solid or liquid contrast enhancing agents, are described. Methods of using the same as ultrasound contrast agents are also disclosed. The present invention also comprises novel methods for synthesizing liposomes having encapsulated therein gases.
    Type: Grant
    Filed: January 8, 1992
    Date of Patent: July 27, 1993
    Inventor: Evan C. Unger
  • Patent number: 5229419
    Abstract: Screening of crude extracts of the bark of Annona bullata Rich. (Annonaceae) showed cytotoxic and pesticidal activities. By monitoring with brine shrimp lethality, two novel extremely potent acetogenins, bullatacin (1) and bullatacinone (2), were isolated. Spectral and chemical methods identified bullatacin as a diastereomer of asimicin. Bullatacinone represents bullatacin with the lactone cleaved and reformed at the 4-OH. Unlike asimicin, which is more generally cytotoxic, 1 and 2 show some selective cytotoxicities in human tumor cell lines, and certain susceptible cells give ED.sub.50 values as low as 10.sup.-12 -10.sup.-15 mcg/ml. Bullatacin was pesticidal at concentration as low as 1 ppm, while bullatacinone lacked pesticidal activities.
    Type: Grant
    Filed: September 29, 1992
    Date of Patent: July 20, 1993
    Assignee: Purdue Research Foundation
    Inventors: Jerry L. McLaughlin, Yu-Hua Hui
  • Patent number: 5223630
    Abstract: A process for preparing suture-grade .beta.-glycolide by purifying crude glycolide which comprises contacting the crude glycolide with a primary solvent which will dissolve the crude glycolide and residual impurities without dissolving primary impurities; removing the primary impurities; recovering the glycolide and residual impurities by evaporating the primary solvent at a temperature below C.; removing residual impurities by washing the glycolide with a washing solvent in which the residual impurities are soluble; and isolating the .beta.-glycolide crystals which remain.
    Type: Grant
    Filed: June 3, 1991
    Date of Patent: June 29, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Kang Lin
  • Patent number: 5223531
    Abstract: Disclosed is a 1,3,2-dioxathiolan-S-oxide derivative as represented by the general formula (I): ##STR1## (where R.sub.1 and R.sub.2 are identical to or different from each other and each is a hydrogen atom or a lower alkyl group;X is a halogen atom, a cyano group, a lower alkyl group, a haloalkyl group or a phenyl group;m is 0 or an integer from 1 to 5; and when small m is greater than 1 each x can be the same or different andn is 1 or 2).A 1,3,2-dioxathiolan-2-oxide derivative of the compound as represented by the general formula (I-I) is prepared by reacting a hydroxymethylcyclopentanol derivative with thionyl chloride; and a 1,3,2-dioxathiolan-2,2-dioxide derivative (I-II) thereof is prepared by oxidizing the compound (I-I). The compounds (I) can be employed as fungicides and intermediate compounds for the preparation of azolylmethylcyclopentanol derivatives.
    Type: Grant
    Filed: August 20, 1992
    Date of Patent: June 29, 1993
    Assignee: Kureha Chemical Industry Co., Ltd.
    Inventors: Satoru Kumazawa, Masanori Minoguchi
  • Patent number: 5221753
    Abstract: A process for the preparation of 1-(4-tetrahydropyranyl)- or 1-(4-tetrahydrothiopyranyl)prop-1-en-3-ones of the general formula I ##STR1## where R.sup.1 is hydrogen, C.sub.1 - to C.sub.10 -alkyl, C.sub.1 - to C.sub.10 -alkoxy or aryloxy,R.sup.2 is hydrogen, C.sub.1 - to C.sub.4 -alkyl, or aryl which is unsubstituted or substituted by C.sub.1 - to C.sub.4 -alkyl and/or halogen, andX is oxygen or sulfur,by reacting 1-aminoprop-1-en-3-ones of the general formula II ##STR2## where R.sup.1 and R.sup.2 are as defined above, andR.sup.3 and R.sup.4, independently of one another, are hydrogen, C.sub.1 - to C.sub.4 -alkyl, aryl or together are a C.sub.2 - to C.sub.7 -alkylene chain,with a 4-tetrahydropyranyl- or 4-tetrahydrothiopyranylmagnesium halide of the general formula III ##STR3## where X is as defined above and Y is halogen, at from to C.,and novel 1-(4-tetrahydropyranyl)- or 1-(4-tetrahydrothiopyranyl)prop-1-en-3-ones are described.
    Type: Grant
    Filed: July 3, 1990
    Date of Patent: June 22, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Shigeru Kozima, Masami Hatano
  • Patent number: 5219886
    Abstract: Novel mercapto-acylamino acids of the formula ##STR1## wherein Q is hydrogen or R.sup.7 CO--;R.sup.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sup.3 is --OR.sup.5 or --NR.sup.5 R.sup.6 ;R.sup.4 and R.sup.9 are independently --(CH.sub.2).sub.q R.sup.8, provided that when R.sup.4 and R.sup.9 are both hydrogen, R.sup.2 is biphenylyl, phenoxyphenyl, phenylthiophenyl, naphthyl, heteroaryl, or lower alkyl substituted with hydroxy, lower alkoxy, mercapto or lower alkylthio;R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached form a 5-7 membered ring;R.sup.7 is hydrogen, lower alkyl or aryl;R.sup.
    Type: Grant
    Filed: October 1, 1991
    Date of Patent: June 15, 1993
    Assignee: Schering Corporation
    Inventors: Elizabeth M. Smith, Philip M. DeCapite, Bernard R. Neustadt
  • Patent number: 5216020
    Abstract: Substituted 4,5-dihydrothieno[2,3-b]thiophene-2-sulfonamides and 6,6-dioxides thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
    Type: Grant
    Filed: August 9, 1991
    Date of Patent: June 1, 1993
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Kenneth L. Shepard, Ronald J. Hudcosky, Theresa M. Williams
  • Patent number: 5214056
    Abstract: A 1,3,2-dioxathiolane oxide derivative is represented by the following formula: ##STR1## wherein X represents --S(O)-- or --S(O).sub.2 --;R.sup.1 represents a hydrogen atom, an alkali metal atom, a benzyl group, or a lower alkyl group;R.sup.2 represents a lower alkyl group which may be substituted with a methylthio group, or a benzyl group, andR.sup.3 and R.sup.4 may be the same or different and independently represent a hydrogen atom, an alkyl group having one to ten carbon atoms, a lower alkyl group substituted with a guanidyl group, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group, a benzyl group, or a phenethyl group, or together form an alkylene group.
    Type: Grant
    Filed: August 20, 1991
    Date of Patent: May 25, 1993
    Assignee: Japan Tobacco Inc.
    Inventors: Jun-ichi Haruta, Masahiro Tanaka, Itsuo Uchida, Akira Ohta, Shin Hara
  • Patent number: 5210219
    Abstract: Novel conjugated stilbenylene polymers are disclosed having non-linear optical properties, and which can be converted to electrically conductive polymers. Such polymers are produced by reacting a novel bis-cycloalkylene sulfonium salt of 2,5-dimethyl stilbene, e.g. 2,5-(4'-methoxy)-stilbene dimethylene bis-(tetramethylene sulfonium bromide), with alkali metal hydroxide to form a cycloalkylene sulfonium salt precursor polymer, and then heating the precursor polymer under conditions to produce the stilbenylene vinylene polymer, e.q. poly(2,5-(4'-methoxy) stilbenylene vinylene).
    Type: Grant
    Filed: July 14, 1992
    Date of Patent: May 11, 1993
    Inventor: John Stenger-Smith
  • Patent number: 5208252
    Abstract: This invention relates to aminoethylthiophene derivatives and more particularly 2-and 3-aminoethylthiophene derivatives which are useful as antiarrhythmic agents, their methods of use as antiarrhythmic agents, and novel intermediate compounds useful for preparation of the aminoethylthiophene derivatives of the invention.
    Type: Grant
    Filed: July 24, 1992
    Date of Patent: May 4, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ronald K. Russell, Joseph J. Salata
  • Patent number: 5208253
    Abstract: 3-Alkyloxy-, aryloxy-, or arylalkyloxy-benzo[b]thiophene-2-carboxamides are described as agents which block leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases. Certain of these compounds are novel and methods of preparation are also described.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: May 4, 1993
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Clifford D. Wright
  • Patent number: 5206388
    Abstract: The reaction of 5,6,11,12-tetrachlorotetracene with thiourea and sulfur in a polar aprotic solvent yields 5,6,11,12-tetrathiotetracene in high yield and purity. This compound is an electron donor for forming electrically conductive radical cation salts with electron donors.
    Type: Grant
    Filed: April 22, 1992
    Date of Patent: April 27, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Alex Alder
  • Patent number: 5206389
    Abstract: These acrylates are those of formulae: ##STR1## where R=C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.12 cycloalkyl, aryl, arylalkyl or alkylaryl; Y=C.sub.1 -C.sub.12 alkyl, C.sub.6 -C.sub.12 aryl, heterocyclic radical whose ring contains from 5 to 10 members and whose heteroatom is chosen from N, O and S, an alkylaryl in which the alkyl part contains from 1 to 4 carbon atoms, Y not being able to denote 1,4-phenylene when R denotes methyl; and Z=hydrocarbon radical containing at least 2 C forming with O and the 2 adjacent Cs a ring containing from 4 to 8 members.To prepare them, an acrylate of formula CH.sub.2 .dbd.CH--COOR is reacted with a dialdehyde OHC--Y--CHO in the presence of an effective quantity of at least one functionalisation catalyst.The invention also relates to the preparation of new polymers and copolymers from the said acrylates.
    Type: Grant
    Filed: June 27, 1991
    Date of Patent: April 27, 1993
    Assignee: Atochem
    Inventors: Marie-Christine Berthe, Paul Caubere, Yves Fort
  • Patent number: 5206438
    Abstract: Disclosed is an aromatic diamine compound represented by the formula (I) ##STR1## wherein R is H or CH.sub.3. Also disclosed is a bismaleimide compound represented by the formula (IV) ##STR2## wherein R is H or CH.sub.3, A resin forming composition comprising these compounds is also disclosed. The compounds are useful as raw materials for resins, and the resin forming composition and the resin can provide excellent heat resistance and impact resistance and low hygroscopicity.
    Type: Grant
    Filed: October 23, 1990
    Date of Patent: April 27, 1993
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Keizaburo Yamaguchi, Tatsuhiro Urakami, Yoshimitsu Tanabe, Midori Yamazaki, Shoji Tamai, Norimasa Yamaya, Masahiro Ohta, Akihiro Yamaguchi
  • Patent number: 5204334
    Abstract: Benzoheterocyclylalkylaminoalkanediphosphonic acids of formula I ##STR1## wherein R.sub.1 and R.sub.2, independently of one another, are hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or lower alkyl, X and Y, independently of one another, are oxy or thio, alk.sub.1 and alk.sub.2 are identical or different lower alkylene radicals, n is 0 or 1 and m and m', independently of one another, are 0, 1 or 2, the sum of n, m and m' being 1, 2 or 3, and their salts exhibit a pronounced regulatory action on the calcium metabolism of warm-blooded animals. They are prepared, for example, as follows: in a compound of the formula ##STR2## wherein R.sub.1, R.sub.2, n, m, m', X, Y, alk.sub.1 and alk.sub.2 are as defined above, R'.sub.3 is one of the groups R.sub.3 mentioned above or is an amino-protecting group R.sub.0, Z.sub.1 is a functionally modified phosphono group, and Z.sub.2 is a free or functionally modified phosphono group, converting functionally modified phosphono Z.sub.
    Type: Grant
    Filed: September 25, 1991
    Date of Patent: April 20, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Wolfgang Frostl, Knut A. Jaeggi
  • Patent number: 5202349
    Abstract: Substituted phenylacetylenes of the formula ##STR1## wherein one of the groups R.sub.1 is a hydrogen atom and the other represents the group of the formula ##STR2## in which R.sub.3 is hydrogen, methyl or ethyl and R.sub.4 is a methyl or an amino group and wherein R.sub.2 represents mono- or binuclear aromatic or heterocyclic residues containing sulfur, nitrogen or oxygen as hetero atoms and optionally being substituted by 1 to 3 substituents as defined, which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leukotrienes.The compounds may be prepared by reacting a compound of the formula ##STR3## wherein R.sub.2 has the same meaning as above and one of the groups R.sub.7 is a hydrogen atom and the other represents the group of the formula --COR.sub.3, with hydroxylamine to form the oxime which then is reduced to the corresponding hydroxylamine compound into which the group of the formula --COR.sub.4 is introduced.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: April 13, 1993
    Assignee: Gruenenthal GmbH
    Inventors: Oswald Zimmer, Werner Vollenberg, Ulrich Seipp, Werner Englberger, Michael Haurand, Brigitte J. Bosman, Johannes Schneider
  • Patent number: 5202348
    Abstract: This invention pertains to a novel group of Thiarubrine substances and closely related derivatives, useful as antifungal and antibiotic agents.
    Type: Grant
    Filed: August 17, 1990
    Date of Patent: April 13, 1993
    Assignee: The University of British Columbia
    Inventors: G. H. Neil Towers, Reimer C. Bruening, Felipe Balza, Zyta A. Abramowski, Isabel Lopez-Bazzochi
  • Patent number: 5198583
    Abstract: The optically active antiviral compound [1R-(1.alpha., 2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)-cyclobutyl]-1,9-dihydro-6H-pu rin-6-one and novel intermediates useful in its preparation are described.
    Type: Grant
    Filed: October 3, 1991
    Date of Patent: March 30, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt