Patents Examined by Mark Russell
  • Patent number: 5271928
    Abstract: Gas or air filled microbubble suspensions in aqueous phases usable as imaging contrast agents in ultrasonic echography. They contain laminarized surfactants and, optionally, hydrophilic stabilizers. The laminarized surfactants can be in the form of liposomes. The suspensions are obtained by exposing the laminarized surfactants to air or a gas before or after admixing with an aqueous phase.
    Type: Grant
    Filed: November 20, 1991
    Date of Patent: December 21, 1993
    Assignee: Sintetica S.A.
    Inventors: Michel Schneider, Daniel Bichon, Philippe Bussat, Jerome Puginier, Eva Hybl-Sutherland
  • Patent number: 5266705
    Abstract: A process for production of 2-acetylbenzo[b]thiophene represented by the formula (I): ##STR1## comprising the steps of: (1) reacting 2-halogenobenzaldehyde represented by the formula (II): ##STR2## wherein X represents a halogen atom, with a compound represented by the formula (III):H.sub.i S.sub.j M.sub.kwherein M represents an alkali metal, i represents zero or 1, j represents an integer of at least 1, and k represents an integer of 1 or 2, and preferably also with sulfur; and(2) reacting the reaction product with a monohalogenoacetone represented by the formula (IV) ##STR3## wherein X.sup.1 represents a halogen atom.
    Type: Grant
    Filed: December 29, 1992
    Date of Patent: November 30, 1993
    Assignee: Ihara Chemical Industry Co., Ltd.
    Inventors: Naoto Yazawa, Yoshinori Saito, Hidetaka Hiyoshi
  • Patent number: 5264577
    Abstract: Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.
    Type: Grant
    Filed: April 22, 1992
    Date of Patent: November 23, 1993
    Assignee: Warner-Lambert Company
    Inventors: Vladimir Beylin, Huai G. Chen, Om P. Goel, Mark E. Marlatt, John G. Topliss
  • Patent number: 5264629
    Abstract: A process for preparing fluorinated compounds belonging to the classes:XH--Y--CZ.sub.1 Z.sub.2 --(CF.sub.2).sub.n F (I)andYH--X--(CF.sub.2).sub.n --CZ.sub.1 Z.sub.2 F (II)wherein:X is NR.sub.x, O, S, CFR.sub.x, C(R.sub.x).sub.2, or CF.sub.2 ;Y is NR.sub.x, O, S, CFR.sub.x, C(R.sub.x).sub.2, or CF.sub.2 ;X is different from Y;R.sub.x is a perhalogenated alkyl group, containing from 1 to 4 carbon atoms;n is either 0 or 1;Z.sub.1 and Z.sub.2, which may be either equal to, or different from, each other, represent F, Cl, Br, H or R.sub.x.The process is characterized in that a fluorinated cyclic compound of the formula: ##STR1## is reacted, at a temperature within the range of from -80.degree. to +300.degree., with HF in the presence of a Lewis acid. Some of the so-obtained compounds per se are novel.
    Type: Grant
    Filed: March 27, 1991
    Date of Patent: November 23, 1993
    Assignee: Ausimont S.r.l.
    Inventors: Darryl D. DesMarteau, Stefan P. Kotun, Alessandro Malacrida
  • Patent number: 5252562
    Abstract: An acetohydroxamic acid compound of formula I ##STR1## as such or in form of a complex with .beta.-cyclodextrin or hydroxypropyl-.beta.-cyclodextrin specifically inhibits 5-lipoxygenase and is useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leucotrienes. The acetohydroxamic acid compound may be prepared by reacting 3-thiophenecarboxaldehyde with hydroxylamine or a salt thereof to form the corresponding oxime, reducing the oxime with a boron-containing reducing agent to form N-(thien-3-yl)methyl-hydroxylamine, and introducing an acetyl group.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: October 12, 1993
    Assignee: Gruenenthal GmbH
    Inventors: Ulrich Seipp, Werner Englberger, Michael Haurand, Johannes Schneider
  • Patent number: 5247098
    Abstract: Thiophene derivatives represented by the general formula (I): ##STR1## where R is an aldehyde, carboxyl, C.sub.1-5 -alkyl ester or C.sub.1-5 -alkyl acetal group and n is 3 to 5, are prepared. These compounds are reversibly converted to their respective isomers by light irradiation, accompanied with a large shift of absorption and emission bands, thus suitable for a photo-responsive material.
    Type: Grant
    Filed: June 27, 1991
    Date of Patent: September 21, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Hiroaki Kumagai, Tomokazu Iyoda, Takeo Shimizu
  • Patent number: 5242942
    Abstract: Compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n and p are as herein defined; exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Compounds of this class are also useful for the treatment of glaucoma, peptic ulcers, hypertension, congestive heart failure and other types of edema. Furthermore, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and novel intermediates are disclosed.
    Type: Grant
    Filed: April 28, 1992
    Date of Patent: September 7, 1993
    Assignee: McNeilab, Inc.
    Inventors: Michael J. Costanzo, Bruce E. Maryanoff
  • Patent number: 5242945
    Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is --CH.sub.2 R;R is ##STR2## and further when Y=S, R may also be --(CH.sub.2).sub.e CH.sub.3 ; Y is --O--or --S--;R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl;R.sup.3 is indolyl, furyl, phenyl or phenyl optionally mono- or disubstituted independently by alkyl of 1-7 carbon atoms, --C(CH.sub.3).sub.3, --C(CH.sub.3).sub.2 CH.sub.2 C(CH.sub.3).sub.3, --C(CH.sub.3).sub.2 CH.sub.2 CH.sub.3, haloloweralkyl, perfluoroalkyl, lower alkoxy, aryl alkoxy, halo or nitro;R.sup.4 and R.sup.5 are, independently, --COCH.sub.2 R.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, geranyl or CH.sub.2 R.sup.3 ;R.sup.6 is hydrogen or lower alkyl;R.sup.7 is geranyl and any moiety selected from R other than ##STR3## A and B are, independently, --O--, --S-- or --NR.sup.6 --; and a is 0-8;b is 1-10 when Y=S, and 2-10 when Y=O;c is 1-3;d is 0-9; ande is 3-18;which by virtue of their ability to inhibit PLA.sub.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: September 7, 1993
    Assignee: American Home Products Corporation
    Inventors: Craig E. Caufield, James M. Rinker
  • Patent number: 5242917
    Abstract: 1-(2,3-Dicarboxyphenyl)-3-(3,4-dicarboxyphenyl)-1,1,3,3-tetramethyldisiloxa ne dianhydride is useful as a curing agent for epoxy resins.
    Type: Grant
    Filed: March 13, 1991
    Date of Patent: September 7, 1993
    Assignee: Hitachi Chemical Company, Ltd.
    Inventors: Tohru Kikuchi, Koichi Kamijima, Takayuki Saito
  • Patent number: 5242931
    Abstract: Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: September 7, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5240958
    Abstract: Compounds of general formula I: ##STR1## wherein: R.sup.1 represents a C.sub.1 -C.sub.6 alkyl, phenyl, thiophenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl phenacyl or substituted phenacyl group; or, when n=O, R.sup.1 represents SR.sup.x, wherein R.sup.x represents a group: ##STR2## R.sup.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl (C.sub.1 -C.sub.6) alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.3 represents an amino acid residue with R or S stereochemistry or a C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6 alkoxy)benzyl or benzyloxy(C.sub.1 -C.sub.6 alkyl) group;R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sup.5 represents a hydrogen atom or a methyl group;n is an integer having the value 0, 1 or 2; andA represents a C.sub.1 -C.sub.6 hydrocarbon chain, optionaly substituted with one or more C.sub.1 -C.sub.
    Type: Grant
    Filed: July 8, 1991
    Date of Patent: August 31, 1993
    Assignee: British Bio-Technology Limited
    Inventors: Colin Campion, Alan H. Davidson, Jonathan P. Dickens, Michael J. Crimmin
  • Patent number: 5237057
    Abstract: The present invention is directed to novel THC derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to the THC metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.
    Type: Grant
    Filed: April 6, 1992
    Date of Patent: August 17, 1993
    Assignee: Biosite Diagnostics, Inc.
    Inventors: Kenneth F. Buechler, Si S. Moi
  • Patent number: 5235069
    Abstract: A process for producing difluoromaleic anhydride by reacting sulfur trioxide with a fluorinated precursor selected from the group consisting of hexafluoro-2,5-dihydrofuran, hexafluoro-2,5-dihydrothiophene, difluoro-2,5-dihydrothiophene-2,5-dione and tetrafluoro-2,5-dihydrothiophene-2-one. Also disclosed are the compounds difluoro-2,5-dihydrothiophene-2,5-dione and tetrafluoro-2,5-dihydrothiophene-2-one.
    Type: Grant
    Filed: February 14, 1991
    Date of Patent: August 10, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Carl G. Krespan
  • Patent number: 5231183
    Abstract: A process for producing an enyne derivative, and intermediate, which is useful for preparing compounds showing strong inhibiting activities against squalane.epoxidase of Eumycetes and strong anti-cholesterol activities. The process comprises reacting a compound of the formula:Z--CH.sub.2 --CH.dbd.CH--W [I]wherein W is a halogen atom, and Z is a leaving group, with an amine in the presence of a base, if necessary, to obtain a compound of the formula: ##STR1## then reacting an acetylene derivative to this compound in the presence of a palladium catalyst, to obtain a compound of the formula: ##STR2## and, if necessary, N-alkylating this compound.
    Type: Grant
    Filed: March 27, 1992
    Date of Patent: July 27, 1993
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Susumu Nakagawa, Akira Asai, Satoru Kuroyanagi, Makoto Ishihara, Yoshiharu Tanaka
  • Patent number: 5124322
    Abstract: Novel compounds of formula (I), salts, solvates and hydrates thereof: ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen; alkyl; alkoxy; halogen; or CF.sub.3 ;R.sub.3 is hydrogen; acyl, such as ##STR2## where Z is optionally substituted aryl; or a group R--S-- where R is an organic residue such that the group R--S-- provides an in vivo-cleavable disulphide bond;R.sub.4 is C.sub.3-6 alkyl;R.sub.5 is hydrogen; alkyl; --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or a group ##STR3## where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 --Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl; andR.sub.6 is hydrogen; alkyl; or a group ##STR4## where R.sub.13 is hydrogen; or alkyl; and R.sub.14 is hydroxy; alkoxy; or --NR.sub.7a R.sub.8 where each of R.sub.7a and R.sub.8 is hydrogen or alkyl, or R.sub.7a and R.sub.
    Type: Grant
    Filed: June 19, 1989
    Date of Patent: June 23, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Ian Hughes
  • Patent number: 5106407
    Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: April 21, 1992
    Assignee: The Dow Chemical Company
    Inventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
  • Patent number: 5047432
    Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof; in which R.sub.1 and R.sub.2, which are the same or different, are H or an optionally substituted hydrocarbon group or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;R.sub.3 is an optionally substituted aromatic hydrocarbon group; andR.sub.4 is a hydrocarbon group containing at least one substituent selected from the group consisting of hydroxy and acylated derivatives thereof, optionally substituted alkoxy groups, optionally substituted cycloalkyloxy groups, optionally substituted alkylenedioxy groups, oxo and groups of formula S(O).sub.p R.sub.5 in which p is 0, 1 or 2 and R.sub.5 is an alkyl group, said hydrocarbon group being optionally substituted by additional substituents,are useful in the treatment of depression.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: September 10, 1991
    Assignee: The Boots Company Plc
    Inventors: John R. Housley, James E. Jeffery, David N. Johnston, Bruce J. Sargent
  • Patent number: 4939168
    Abstract: Novel lactone compounds having remarkable immunomodulatory and antitumor activities, pharmaceutical compositions comprising such compounds, methods for the preparation of the novel compounds and compositions and methods of their use for therapeutic purposes are described. The new lactone compounds have the structure according to the formula: ##STR1## wherein: R=--H, --A, --CH.sub.2 --Q, --COA or --COZ,A=lower alkyl,Z=monocyclicaryl,Q=phenyl, tolyl or xylyl,X=--H, --A, --Z or --CH.sub.2 --Z, andY=--H, --A, --Z, --CH.sub.2 --Z, --COA, --COZ,the acid-addition salts, the octahydro and 23,24-dihydro derivatives thereof.
    Type: Grant
    Filed: August 11, 1989
    Date of Patent: July 3, 1990
    Assignee: Harbor Branch Oceanographics Institution, Inc.
    Inventors: Malika Gunasekera, Sarath P. Gunasekera, Ross E. Longley, Neal S. Burres