The Hetero Ring Contains At Least Eight Members Including Nitrogen And Carbon Patents (Class 540/450)
  • Patent number: 5811552
    Abstract: A novel cyclobutenedione derivative prepared in accordance with the following reaction formula, a process for the preparation thereof, and a nonlinear optical element comprising such a derivative are provided: ##STR1## wherein R.sup.1 and R.sup.2 each represents an alkyl group, an alkenyl group or an alkynyl group; R.sup.3 and R.sup.4 each represents a hydrogen atom, an alkyl group, an alkenyl group or an alkynyl group; and C.sup.* represents an asymmetric carbon atom, with the proviso that R.sup.1, R.sup.2 and the nitrogen atom to which they are connected may form a cyclic structure larger than 3-membered ring, R.sup.1 and R.sup.3, and R.sup.2 and R.sup.4 each may be connected to each other to form a methylene chain --(CH.sub.2).sub.n -, and the hydrogen atoms in R.sup.1 and R.sup.2 may be substituted by halogen atom, alkyloxy group or cyano group.
    Type: Grant
    Filed: April 14, 1995
    Date of Patent: September 22, 1998
    Assignee: Fuji Xerox Co., Ltd.
    Inventors: Yasunari Nishikata, Lyong Sun Pu
  • Patent number: 5792820
    Abstract: An organolithium compound according to the present invention containing a cyclic amino group, has the general formula: ##STR1## wherein R.sub.1 is a divalent alkylene, an oxy- or amino-alkylene, or substituted alkylene having from 6 to about 20 carbon atoms; R.sub.2 is a linear-, branched-, or cyclo-alkylene having from about 2 to about 20 carbon atoms; and the lithium, Li, is bonded directly to a carbon atom of R.sub.2. A method of preparing an organolithium compound containing a cyclic amino group, comprising reacting a cyclic amino organo halide having the general formula ##STR2## where R.sub.1 and R.sub.2 are as above, and X is bromine or chlorine bonded directly to a carbon atom of R.sub.2, with a lithium reactant selected from lithium metal or an organolithium compound.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: August 11, 1998
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, Thomas A. Antkowiak, James E. Hall, Mark L. Stayer, Jr., John R. Schreffler
  • Patent number: 5789585
    Abstract: A family of aza-ether based compounds including linear, multi-branched and aza-crown ethers is provided. When added to non-aqueous battery electrolytes, the new family of aza-ether based compounds acts as neutral receptors to complex the anion moiety of the electrolyte salt thereby increasing the conductivity and the transference number of LI.sup.+ ion in alkali metal batteries.
    Type: Grant
    Filed: May 23, 1997
    Date of Patent: August 4, 1998
    Assignee: Brookhaven Science Associates LLC
    Inventors: Hung Sui Lee, Xiao-Oing Yang, James McBreen
  • Patent number: 5777125
    Abstract: A process for the preparation of tertiary diphenyl carbinols containing a primary or secondary amine substituent on the aliphatic moiety attached to the carbinol function which consists in contacting a Grignard phenyl reagent with an aminoacid wherein the mobile protons are not masked in an aprotic inert organic solvent or a mixture thereof at a temperature between 20.degree. C. and the boiling temperature by the reaction mixture.The reaction products are useful as active ingredients of medicaments and intermediates for the manufacture thereof.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: July 7, 1998
    Assignee: Gruppo Lepetit SpA
    Inventor: Elvio Bellasio
  • Patent number: 5773660
    Abstract: A process for preparing amines of the formula I ##STR1## where R.sup.1,R.sup.2,R.sup.3,R.sup.4,R.sup.5 and R.sup.6 are each hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.2 -C.sub.20 -alkynyl, C.sub.3 -C.sub.20 -cycloalkyl, C.sub.4 -C.sub.20 -alkylcycloalkyl, C.sub.4 -C.sub.20 -cycloalkylalkyl, aryl, C.sub.7 -C.sub.20 -alkylaryl or C.sub.7 -C.sub.20 -aralkyl,R.sup.1 and R.sup.2 are together a saturated or unsaturated C.sub.3 -C.sub.9 -alkylene dichain, andR.sup.3 or R.sup.5 is C.sub.21 -C.sub.200 -alkyl or C.sub.21 -C.sub.200 -alkenyl or together they are a C.sub.2 -C.sub.12 -alkylene dichain,by reacting olefins of the formula II ##STR2## where R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each as defined above, with ammonia or primary or secondary amines of the formula III ##STR3## where R.sup.1 and R.sup.2 are each as defined above, at temperatures from 200.degree. to 350.degree. C.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: June 30, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Karsten Eller, Rudolf Kummer, Eugen Gehrer
  • Patent number: 5773609
    Abstract: A broad class of photosensitive compounds having enhanced in vivo target tissue selectivity and versatility in photodynamic therapy. Many furocoumarin compounds, such as psoralens, exhibit cytostatic activity when photoactivated but exhibit little in vivo specificity for selectively accumulating in any particular target tissue such as atheromatous plaques. Reactive Oxygen Producing Photosensitizers ("ROPPs") are photoactivatable compounds having an affinity for hyperproliferating cells (such as atheromatous plaque cells), which when photoactivated, produce cytotoxic reaction products. The photoactivity of a ROPP, such as a porphyrin, may be reduced by metalating the porphyrin while the selective affinity of the metalized ROPP for hyperproliferating tissue remains substantially unchanged.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: June 30, 1998
    Assignee: PDT Pharmaceuticals, Inc.
    Inventors: Byron Robinson, Alan R. Morgan, Hugh L. Narciso, Jr.
  • Patent number: 5733924
    Abstract: DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, ?wherein R.sup.1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4 or the like; R.sup.2 represents hydrogen or COR.sup.5 ; R.sup.3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6, with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.
    Type: Grant
    Filed: April 17, 1997
    Date of Patent: March 31, 1998
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yutaka Kanda, Yutaka Saitoh, Hiromitsu Saito, Tadashi Ashizawa, Kazuyo Sugiyama, Katsushige Gomi, Shingo Kakita, Yuichi Takahashi, Chikara Murakata
  • 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: 5731305
    Abstract: There are disclosed anti-hypertensive compositions and a method of lowering blood pressure in mammals. The active component in the anti-hypertensive compositions is a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from straight chain and branched chain C.sub.1 -C.sub.12 alkyl groups and benzyl, with the proviso that no branch occur on the alpha carbon atom of the alkyl group; or R.sub.1 and R.sub.2 together with the nitrogen atom they are bonded to form a heterocyclic ring; M.sup.+x is a pharmaceutically acceptable cation, wherein x is the valence of the cation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 24, 1998
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Larry Kay Keefer, David Anderson Wink, Tambra Marie Dunams, Joseph Anthony Hrabie
  • Patent number: 5731441
    Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.
    Type: Grant
    Filed: October 29, 1996
    Date of Patent: March 24, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
  • Patent number: 5721361
    Abstract: A process for preparing a substituted polyazamacrocycle is provided which comprises contacting a diamine or triamine and a dicarboxylic acid or ester or anhydride thereof in the presence of a suitable base and a suitable solvent to produce the substituted polyazamacrocycle provided that when an ester of said dicarboxylic acid is used, said suitable base is optional, and when said dicarboxylic acid or an anhydride of said dicarboxylic acid is used, the reaction mixture further comprises a suitable coupling agent.
    Type: Grant
    Filed: June 11, 1996
    Date of Patent: February 24, 1998
    Assignee: The Monsanto Company
    Inventors: Patrick J. Lennon, Susan L. Henke, Karl W. Aston
  • Patent number: 5718845
    Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: February 17, 1998
    Assignee: Enichem S.p.A.
    Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
  • Patent number: 5714604
    Abstract: A novel process for the preparation of azamacrocyclic or acyclic aminophosphonate ester derivatives is disclosed. The process concerns the reaction of an appropriate azamacrocyclic or acyclic primary or secondary amine with trialkyl phosphite and paraformaldehyde.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: February 3, 1998
    Assignee: The Dow Chemical Company
    Inventor: Garry E. Kiefer
  • 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: 5710241
    Abstract: The present invention relates to monoanhydride monomer compounds, methods of making such compounds and reaction products of the monoanhydride-diacid compounds with other monomers. The inventive monomer compounds exhibit selective reactivity, that is, the dianhydride locus is substantially more reactive towards amines than the diacid locus making it possible to sequentially synthesize a new class of materials suitable for membranes, catalytic substrates or any speciality material required for advanced applications.
    Type: Grant
    Filed: March 2, 1994
    Date of Patent: January 20, 1998
    Assignee: Hoechst Celanese Corp.
    Inventors: Michael Haubs, Paul Foley, Dominick L. Cangiano
  • Patent number: 5705509
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: January 6, 1998
    Assignee: SmithKline Beecham plc
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5693630
    Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.
    Type: Grant
    Filed: October 26, 1994
    Date of Patent: December 2, 1997
    Assignee: Astra Aktiebolag
    Inventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
  • Patent number: 5688783
    Abstract: Salinamides A and B are disclosed. These two bicyclic depsipeptides are produced by fermentation of a specific marine actinomycete, a Streptomyces sp, (CNB-091) in saltwater-based media. Salinamides A and B are useful as anti-biotic and anti-inflammatory agents.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: November 18, 1997
    Assignee: The Regents of the University of California
    Inventors: William H. Fenical, Robert S. Jacobs, Paul R. Jensen
  • Patent number: 5686446
    Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: November 11, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
  • Patent number: 5686483
    Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: November 11, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
  • Patent number: 5686447
    Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: November 11, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
  • Patent number: 5684021
    Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: November 4, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
  • Patent number: 5676923
    Abstract: Diethylenetriaminepentaacetic acid monoamide derivatives, their complexes and complex salts, containing an element of atomic numbers 21-29, 31, 32, 39, 42-44, 49 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and process for their production.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 14, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Johannes Platzek, Ulrich Niedballa, Peter Mareski, Bernd Raduchel, Hanns-Joachim Weinmann, Andreas Muhler, Bernd Misselwitz
  • Patent number: 5665756
    Abstract: Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl, and p is 1 or 2; b. A is a group of the formula ##STR3## c. R.sup.1 and R.sup.2 are independently hydrogen or lowerakyl; and d. m is 2 to 6 and n is 0, or 2 to 6, inclusive, serotonin reuptake inhibitors, useful for treating depression and obsessive compulsive disorders are described. Also described are precursors of and processes for the preparation of such aminoakyloximes.
    Type: Grant
    Filed: August 3, 1994
    Date of Patent: September 9, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
  • Patent number: 5659035
    Abstract: A method for the production of azacycloalkane-2,2-diphosphonic acids of general formula; ##STR1## where n is a whole number of from 2 to 16, Y is H, an alkyl or alkenyl, a substituted alkyl, or an aryl, such that the group "Y" remains unchanged during the reaction,by reaction of a lactam with a phosphorus trihalide in the presence of phosphorous acid and/or water, in which the reaction mixture also includes an organic amine and/or or an organic amine salt, said reaction being followed by hydrolysis of the reaction mixture and purification of the reaction product to obtain the diphosphonic acid.The method is exemplified by the preparation of azacycloheptane-2,2-diphosphonic acid, and azacyclononane-2,2-diphosphonic acid.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: August 19, 1997
    Assignee: Albright & Wilson Limited
    Inventors: Michael Bamber, Gary Woodward
  • Patent number: 5643848
    Abstract: An acyclic alkane soluble anionic polymerization initiator includes a mixture of from about 90 to about 10 parts by weight of a lithio amine having the general formula A.sub.1 Li and from about 10 to about 90 parts by weight of at least one other lithio amine having the general formula A.sub.2 Li. A.sub.1 and A.sub.2 are selected from the dialkyl, alkyl, cycloalkyl and dicycloalkyl amine radicals and cyclic amine radicals. There is also provided a method of forming a mixture of anionic polymerization initiators, a functionalized polymer and a method of forming a functionalized polymer.
    Type: Grant
    Filed: May 3, 1995
    Date of Patent: July 1, 1997
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, James E. Hall, Yoichi Ozawa
  • Patent number: 5632969
    Abstract: Novel N.sub.3 S.sub.2 chelating ligands can be chelated to a radiodetectable element, Tc or Re, and are useful for radiolabeling peptides. A group of peptides especially useful are somatostatin derivatives which are valuable of the selective detection or treatment of tumors with somatostatin receptors.
    Type: Grant
    Filed: October 13, 1994
    Date of Patent: May 27, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Flanagan, Jean-Marc Dufour, Keith T. Hogan
  • Patent number: 5631368
    Abstract: The present invention relates to tribenzylcyclen compounds of formula I ##STR1## (where R is hydrogen, or a C.sub.1-12 alkyl group optionally substituted by hydroxy, alkoxy or aryl groups or R is an amphiphilic aralkyl group comprising a N, S, O or P interrupted C.sub.2-25 alkylene chain, e.g. a polyalkylene oxide chain or R provides a bridge to a second tribenzylcyclen group, but with the proviso that R is other than benzyl; X is CHR.sub.1, or where R is hydrogen two X groups may each represent CO groups; and R.sub.1 is hydrogen, a C.sub.1-6 alkyl group optionally substituted by hydroxy, alkoxy or carboxy groups or an aralkyl group having 1 to 6 carbons in the alkyl moiety and optionally substituted in the aryl moiety by alkyl, alkoxy, hydroxy or isothiocyanate groups). These compounds are useful in the preparation of DO3A, N-substituted-1,4,7,10-tetraazacyclododecane-N',N",N"'-triacetic acids, and the phosphonic acid analogs.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 20, 1997
    Assignee: Nycomed Imaging AS
    Inventors: Lisa Schultze, Alan R. Bulls
  • Patent number: 5624949
    Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: April 29, 1997
    Assignee: Eli Lilly and Company
    Inventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
  • Patent number: 5622821
    Abstract: The invention provides lanthanide chelates capable of intense luminescence. The celates comprise a lanthanide chelator covalently joined to a coumarin-like or quinolone-like sensitizer. Exemplary sensitzers include 2- or 4-quinolones, 2- or 4-coumarins, or derivatives thereof e.g. carbostyril 124 (7-amino-4-methyl-2-quinolone), coumarin 120 (7-amino-4-methyl-2-coumarin), coumarin 124 (7-amino-4-(trifluoromethyl)-2-coumarin), aminomethyltrimethylpsoralen, etc.The chelates form high affinity complexes with lanthanides, such as terbium or europium, through chelator groups, such as DTPA. The chelates may be coupled to a wide variety of compounds to create specific labels, probes, diagnostic and/or therapeutic reagents, etc. The chelates find particular use in resonance energy transfer between chelate-lanthanide complexes and another luminescent agent, often a fluorescent non-metal based resonance energy acceptor.
    Type: Grant
    Filed: June 29, 1994
    Date of Patent: April 22, 1997
    Assignee: The Regents of the University of California
    Inventors: Paul R. Selvin, John Hearst
  • Patent number: 5616704
    Abstract: The present invention is directed toward anionic polymerization initiators which are soluble in acyclic alkane solvents. The initiators include a solubilized lithio amine having the general formula (A)Li(SOL).sub.y. SOL is a solubilizing component and A is an alkyl, dialkyl or cycloalkyl amine radical or a cyclic amine and y is from about 1 to 4. The cyclic amine has an alkylene, oxy- or amino-alkylene group having from about 3 to about 16 methylene groups. The invention is also directed toward polymers and other products made using the initiator, and methods therefor. Further, the invention contemplates a polymer, a polymer composition and products therefrom, which include a functional group from the reaction product of an amine and an organolithium compound. The resulting polymers may be terminated with a terminating, coupling or linking agent, which may provide the polymer with a multifunctionality.
    Type: Grant
    Filed: April 29, 1996
    Date of Patent: April 1, 1997
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, Mark L. Stayer, Jr., David Saffles, H. James Harwood
  • Patent number: 5610227
    Abstract: The present invention provides anionic polymerization initiators, comprising lithium amino magnesiate complexes, resulting in diene polymer and copolymer elastomers. The invention initiators have stable living ends at high polymerization temperatures and produce polymers containing a high level of tertiary amine functionality. Such polymers exhibit an increased efficiency in coupling termination reactions, and elastomers and products prepared from such polymers exhibit reduced hysteresis properties. Methods are also provided for preparing the initiators, the polymers and the elastomers.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 11, 1997
    Assignee: Bridgestone/Firestone, Inc.
    Inventors: Thomas A. Antkowiak, James E. Hall
  • Patent number: 5608061
    Abstract: An improved process for preparing 1,4,8,11-tetraazacyclotetradecane comprising the tetratosylation of an acyclic tetraamine to obtain a tetratoluenesulfonamide compound in a first step, the cyclization of said sulfonamide compound to obtain tetratosyl cyclam in a second step, and the detosylation of tetratosyl cyclam in a third step followed by basification to obtain the desired 1,4,8,11-tetraazacyclotetradecane.
    Type: Grant
    Filed: August 2, 1995
    Date of Patent: March 4, 1997
    Assignee: Johnson Matthey PLC
    Inventors: Lech Ciszewski, John Amedio, Prasad Kapa, Andrew Kucerovy, George T. Lee
  • Patent number: 5580900
    Abstract: A compound of the formula: ##STR1## in which each R.sup.1 to R.sup.4 group is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-carbonyl, halo, hydroxy, nitro, cyano, trihalomethyl or optionally substituted phenyl, each R.sup.5 to R.sup.16 group is hydrogen or C.sub.1-4 alkyl, each Z', Z", Z'" and Z"" group is an alkylene radical, and X and Y are each --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --A--(CH.sub.2).sub.p -- where A is --CH.dbd.CH--, optionally substituted phenylene or optionally substituted naphthalenyl, n is 2 to 10, and m and p are each 1 or 2, salts thereof, and intermediates for the production thereof.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: December 3, 1996
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, John R. Harris
  • Patent number: 5578542
    Abstract: An acyclic alkane soluble anionic polymerization initiator includes a mixture of from about 90 to about 10 parts by weight of a lithio amine having the general formula A.sub.1 Li and from about 10 to about 90 parts by weight of at least one other lithio amine having the general formula A.sub.2 Li. A.sub.1 and A.sub.2 are selected from the dialkyl, alkyl, cycloalkyl and dicycloalkyl amine radicals and cyclic amine radicals. There is also provided a method of forming a mixture of anionic polymerization initiators, a functionalized polymer and a method of forming a functionalized polymer.
    Type: Grant
    Filed: March 30, 1994
    Date of Patent: November 26, 1996
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, James E. Hall, Yoichi Ozawa
  • Patent number: 5574158
    Abstract: A compound of the formula: ##STR1## in which each R.sup.1 to R.sup.4 group is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-carbonyl, halo, hydroxy, nitro, cyano, trihalomethyl or optionally substituted phenyl, each R.sup.5 to R.sup.16 group is hydrogen or C.sub.1-4 alkyl, each Z', Z", Z'" and Z"" group is an alkylene radical, and X and Y are each --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --A--(CH.sub.2).sub.p -- where A is --CH.dbd.CH--, optionally substituted phenylene or optionally substituted naphthalenyl, n is 2 to 10, and m and p are each 1 or 2, salts thereof, and intermediates for the production thereof.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: November 12, 1996
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, John R. Harris
  • Patent number: 5556968
    Abstract: Macrocyclic chelating agents, optionally possessing more than one macrocyclic ring having at least two peptide linkages within the macrocyclic skeleton. The chelating agents are used for the preparation of paramagnetic metal chelates for use as MRI contrast agents.
    Type: Grant
    Filed: May 7, 1993
    Date of Patent: September 17, 1996
    Assignee: Nycomed Salutar, Inc.
    Inventors: Joan F. Carvalho, Shaun P. Crofts, John Varadarajan
  • Patent number: 5554749
    Abstract: The present invention provides new and structurally diverse compositions comprising compounds of the general formula: ##STR1## Wherein U is --(CH.sub.2).sub.n X or --(CH.sub.2).sub.n NR.sub.1 (CH.sub.2)X; R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl or C.sub.1 -C.sub.8 alkoxyalkyl; V is --(CH.sub.2).sub.n X, --(CH.sub.2).sub.n NR.sub.1 (CH.sub.2)X, hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl or C.sub.1 -C.sub.8 alkoxyalkyl; V and R.sub.1 may jointly be --(CH.sub.2).sub.m -- to form a heterocyclic ring; X is --CO.sub.2 H, --PO.sub.3 H.sub.2, --SO.sub.3 H or --CONHOH; a, b, c, d, n and m may be the same or different and are from one to about ten, preferably from one to about three.Methods for imaging using compositions of the invention are also provided.
    Type: Grant
    Filed: January 14, 1994
    Date of Patent: September 10, 1996
    Assignee: Mallinckrodt Medical, Inc.
    Inventors: Rebacca A. Wallace, Dennis A. Moore
  • Patent number: 5550233
    Abstract: Aryl, alkyl, alkenyl and alkynyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and alkylation at C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
    Type: Grant
    Filed: June 21, 1994
    Date of Patent: August 27, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Kathleen M. Rupprecht, Robert K. Baker, Hyun O. Ok, William H. Parsons
  • Patent number: 5545734
    Abstract: Aryl and heteroaryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by olefination at C-27. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases, and illnesses.
    Type: Grant
    Filed: October 25, 1994
    Date of Patent: August 13, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Gerard R. Kieczykowski, Hyun O. Ok, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5545608
    Abstract: Pyrazole-glycolic acid amides of the following formula (1) (in which R.sup.1 to R.sup.5 each represent a hydrogen atom or a substituent having a broad definition), and herbicides containing them. The compounds have a high herbicidal effect against paddy weeds, especially Echinochloa crus-galli, while highly safe for paddy rice plants.
    Type: Grant
    Filed: April 25, 1994
    Date of Patent: August 13, 1996
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Katsushi Morimoto, Masatoshi Ohnari, Tsutomu Nawamaki, Shigeomi Watanabe, Kimihiro Ishikawa
  • 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: 5521309
    Abstract: An anionic polymerization initiator includes the C-lithio reaction product of an organolithium compound and a tertiary-amino allyllithium or a tertiary-amino xylyllithium. When used in an anionic polymerization, a functional group from the initiator is incorporated onto the head of the growing polymer and a lithium atom is incorporated at the "living" end of the polymer chain prior to quenching. The initiator may be used to polymerize a monomer(s) including diolefin monomers, monovinyl aromatic monomers and trienes, and the living ends of the polymers are effectively maintained even at temperatures of up to 300.degree. F. and higher. Such polymers exhibit an increased efficiency in coupling termination reactions, and products prepared from such polymers exhibit improved hysteresis characteristics. Products such as tires and the like can be prepared from such polymers and from vulcanizable elastomer compositions employing the polymers.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: May 28, 1996
    Assignee: Bridgestone Corporation
    Inventors: Thomas A. Antkowiak, James E. Hall, David F. Lawson, John R. Schreffler, Mark L. Stayer, Jr.
  • Patent number: 5519023
    Abstract: The invention relates to 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 and Z are as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base and medicaments containing the same, useful in the treatment and prevention of stress, anxiety, and related ailments.
    Type: Grant
    Filed: July 2, 1993
    Date of Patent: May 21, 1996
    Assignee: Adir et Compagnie
    Inventors: Marc Payard, Genevieve Baziard-Mouysset, Gilbert De Saqui-Sannes, Beatrice Guardiola, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
  • Patent number: 5496940
    Abstract: An organolithium compound according to the present invention containing a cyclic amino group, has the general formula: ##STR1## wherein R.sub.1 is a divalent alkylene, an oxy- or amino-alkylene, or substituted alkylene having from 6 to about 20 carbon atoms; R.sub.2 is a linear-, branched-, or cyclo-alkylene having from about 2 to about 20 carbon atoms; and the lithium, Li, is bonded directly to a carbon atom of R.sub.2. A method of preparing an organolithium compound containing a cyclic amino group, comprising reacting a cyclic amino organo halide having the general formula ##STR2## where R.sub.1 and R.sub.2 are as above, and X is bromine or chlorine bonded directly to a carbon atom of R.sub.2, with a lithium reactant selected from lithium metal or an organolithium compound.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: March 5, 1996
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, Thomas A. Antkowiak, James E. Hall, Mark L. Stayer, Jr., John R. Schreffler
  • Patent number: 5491230
    Abstract: An anionic polymerization initiator includes a carbon-lithio salt of the adduct of a cyclic secondary amine with a conjugated diene. A method of preparing an anionic polymerization initiator includes reacting an excess of a cyclic secondary amine with a conjugated diene to form an adduct; and, reacting the adduct with an organolithium compound. A method of preparing a polymer includes forming a solution of one or more anionically polymerizable monomers in a hydrocarbon solvent; and, polymerizing the monomer with an anionic polymerization initiator comprising a carbon-lithio salt of the adduct of a cyclic secondary amine with a conjugated diene. A functionalized polymer includes the termination product of a living polymer having the general formula AYLi, wherein A is a functional group derived from an anionic polymerization initiator; and, Y is a divalent polymer radical; wherein the anionic polymerization initiator is a carbon-lithio salt of the adduct of a cyclic secondary amine with a conjugated diene.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: February 13, 1996
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, Thomas A. Antkowiak, James E. Hall, Mark L. Stayer, Jr.
  • Patent number: 5457111
    Abstract: Immunomodulatory macrocyclic compounds having the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, wherein X is selected from one of the formulae ##STR2## as well as pharmaceutical compositions containing the same.
    Type: Grant
    Filed: November 9, 1993
    Date of Patent: October 10, 1995
    Assignee: Abbott Laboratories
    Inventors: Jay R. Luly, Megumi Kawai, Yat S. Or, Paul Wiedeman, Rolf Wagner
  • Patent number: 5453220
    Abstract: Calixarene-based, noncentrosymmetric transition metal complexes that exhibit large second order nonlinear optical and related electro-optical properties are provided, as are materials and devices comprising the same.
    Type: Grant
    Filed: January 29, 1993
    Date of Patent: September 26, 1995
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Timothy M. Swager, Bing Xu
  • Patent number: 5441946
    Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
    Type: Grant
    Filed: April 14, 1994
    Date of Patent: August 15, 1995
    Assignee: Rhone-Poulenc-Rorer Pharmaceuticals, Inc.
    Inventors: Henry W. Pauls, Yong-Mi Choi, Dilip V. Amin
  • Patent number: 5438133
    Abstract: Cyclodextrin catenanes capable of forming inclusion complexes and a method of preparing them are disclosed. The catenanes comprise one or two per-2,6- di-O-alkyl-.beta.-cyclodextrin macrocycles wherein each per-2,6-di-O-alkyl-.beta.-cyclodextrin macrocycle is interpenetrated by another macrocycle. Such modified cyclodextrins may be used for the electrochemical and optical sensing of small organic molecules, especially small aromatic molecules.
    Type: Grant
    Filed: January 27, 1994
    Date of Patent: August 1, 1995
    Assignee: Eastman Kodak Company
    Inventors: Christopher P. Moore, Trevor J. Wear, James F. Stoddart, Dominique Armspach