Patents Examined by Y. N. Gupta
  • Patent number: 5446145
    Abstract: There are disclosed polychelant compounds, that is multi-site metal chelating agents, and chelates formed therewith. The polychelants and especially their paramagnetic metal, heavy metal or radioactive metal polychelates are particularly suitable for use in diagnostic imaging, heavy metal detoxification or radiotherapy. The polychelants have a linear or branched oligomeric structure comprising alternating chelant and linker moieties bound together by amide or ester moieties the carbonyl groups whereof being adjacent the chelant moieties, each polychelant comprising at least two said chelant moieties capable of complexing a metal ion.
    Type: Grant
    Filed: July 7, 1993
    Date of Patent: August 29, 1995
    Assignee: Nycomed Salutar, Inc.
    Inventors: David B. Love, William C. Dow, Richard J. Himmelsbach, Alan D. Watson, Scott M. Rocklage
  • Patent number: 5414094
    Abstract: A process for making a dianhydride product, said process comprising reacting two moles of maleic anhydride and one mole of a vinyl benzene compound in a reaction mixture comprising about 1.5 to 2.0 moles of the vinyl benzene compound per mole of maleic anhydride at reaction temperature in the range from to C. for time to complete the reaction, adding a polar organic liquid to the reaction product mixture and refluxing the mixture, cooling the mixture following reflux and adding a hydrocarbon liquid to precipitate the product, separating the solid dianhydride product by filtration, washing the solids on the filter and drying the solids to make the finished dianhydride product.
    Type: Grant
    Filed: January 26, 1990
    Date of Patent: May 9, 1995
    Assignee: Cytec Technology Corp.
    Inventor: Joseph Csapilla
  • Patent number: 5410051
    Abstract: Disclosed are novel nitrogen containing heterocyclic compounds and novel vinyl terminated polyurethane/polyamide polymers together with the use of both of these compounds in a novel adhesive and coating composition. The nitrogen containing heterocyclic compounds of the invention contain two vinyl-terminated substituents and at least one carbamylmethyl substituent and have a nucleus selected from melamine, oligomers of melamine, benzoguanamine, and oligomers of benzoguanamine, glycoluril and oligomers of glycoluril, cyclohexylguanamine, oligomers of cyclohexylguanamine, acetoguanamine, and oligomers of acetoguanamine. The vinyl terminated polyurethane compounds of the invention have a molecular weight of from about 3000 to about 80000, and contain at least two vinyl end groups.
    Type: Grant
    Filed: June 17, 1993
    Date of Patent: April 25, 1995
    Assignee: Cytec Technology Corp.
    Inventors: Peter S. Forgione, William A. Henderson, Balwant Singh, Yuhshi Luh
  • Patent number: 5410057
    Abstract: The present invention relates to new 1-heteroarylazetidines and new 1-heteroarylpyrrolidines endowed with 5-HT.sub.3 agonist activity of formula (IV): ##STR1## The substituents A, R', R.sub.1 and P, and the variables n and m, are as herein described.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: April 25, 1995
    Assignee: Sanofi
    Inventors: Marco Baroni, Umberto Guzzi, Antonina Giudice, Marco Landi, Vivian Mazza
  • Patent number: 5410063
    Abstract: A compound of the formula II ##STR1## in which R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkoxy or CF.sub.3 and A is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl, each of which is monosubstituted to trisubstituted by halogen, or is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl, each of which is substituted by C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.2 -C.sub.4 alkenyl, C.sub.5 -C.sub.6 cycloalkenyl, amino, C.sub.1 -C.sub.4 alkylamino, C.sub.1 -C.sub.4 dialkylamino or C.sub.2 -C.sub.4 alkynyl, it being possible for the C.sub.2 -C.sub.4 alkenyl radical and the C.sub.5 -C.sub.6 cycloalkenyl radical to be additionally monosubstituted to trisubstituted by halogen; or A is a 4- to 6-membered saturated heterocycle which contains a hetero atom selected from the group consisting of O, N and SO.sub.2 ; or A is C.sub.1 -C.sub.
    Type: Grant
    Filed: April 1, 1994
    Date of Patent: April 25, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Fory, Rolf Schurter
  • Patent number: 5405959
    Abstract: This invention provides a process for preparing amide derivatives of acids by the reaction of haloaminotriazines and acid halides.This invention also provides a process for preparing isocyanates and isocyanate adducts from amide derivatives derived from haloaminotriazines and acid halides such as oxalyl chloride, phosgene and phosgene analogs.Melamine derived acid amides are prepared by reaction of trichloro and hexachloromelamines with chloroformates and acid chlorides. The by-product chlorine may be recycled in this process.Amides, carbamates, sulfonamides, phosphoramides, and related amide derivatives may be prepared by the novel processes of the invention.
    Type: Grant
    Filed: November 10, 1993
    Date of Patent: April 11, 1995
    Assignee: Cytec Technology Corp.
    Inventor: Ram B. Gupta
  • 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: 5401737
    Abstract: The invention relates to a compound of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is a bond or lower alkylene which may have lower alkyl group(s), andR.sup.2 is arylcarbamoyl which may have halogen or lower alkoxy,or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.
    Type: Grant
    Filed: July 23, 1993
    Date of Patent: March 28, 1995
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
  • Patent number: 5401877
    Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted sibyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH=CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.
    Type: Grant
    Filed: July 22, 1994
    Date of Patent: March 28, 1995
    Assignee: Shionogi Seiyaku Kabushiki Kaisha
    Inventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
  • Patent number: 5401756
    Abstract: Benzamide platelet activating factor antagonists of the following formula (I): ##STR1## wherein ##STR2## B, D: hydrogen atom, etc. E: pyridyl group, etc.n: integer from 0 to 2R.sup.2 : R.sup.3 R.sup.4 N-- etc.(R.sup.3, R.sup.4 : optionally substituted C.sub.6 -C.sub.12 aryl group, etc.) ##STR3## optical antipodes thereof or pharmaceutically acceptable salts thereof, show excellent PAF antagonism and are effective for therapy and prophylaxis of diseases caused by PAF (bronchial asthma, nephritis, shocks, cardiac infarction, cerebral hemorrhage, ulcer, DIC, autoimmune diseases, thrombosis, etc.).
    Type: Grant
    Filed: February 2, 1994
    Date of Patent: March 28, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Akihiro Yamamoto, Shuji Morita, Yoshio Hayashi, Noboru Yamada, Toshihito Kitamura
  • Patent number: 5399692
    Abstract: An ultraviolet radiation absorbing agent for bonding to an ocular lens. The agent has the formulaA--NH--Bwherein A is an ultraviolet absorbing compound and B is a specific reactive group or a moiety containing reactive group.
    Type: Grant
    Filed: July 14, 1993
    Date of Patent: March 21, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: William M. Hung, Kai C. Su
  • Patent number: 5399560
    Abstract: The mechanism of the inhibition of advanced glycosylation by aminoguanidine and other hydrazine type compounds was investigated using a solution of one or two molecules of aminoguanidine or other hydrazine type compound incubated with an Amadori product (1-propylamine-1-deoxy-D-fructose) under physiological conditions. This inhibition was found to proceed through the reactive intermediate 1-propylamino-1, 4-dideoxyosone to form the corresponding triazine and the dehydrazone of 1,4-dideoxyglucosone, respectively.The triazine and dehydrazone products are useful as macrophage stimulants to activate a macrophage to effect removal of advanced glycosylation endproducts (AGEs). Additionally, they can be used in a variety of investigative methods in an effort to measure the extent of nonenzymatic glycosylation of a protein sample wherein aminoguanidine or other hydrazine-type compound is or was present during the glycosylation process.
    Type: Grant
    Filed: October 1, 1992
    Date of Patent: March 21, 1995
    Assignee: The Rockefeller University
    Inventors: Anthony Cerami, Hauh-Jyun C. Chen
  • Patent number: 5399775
    Abstract: The present invention relates to a process for the preparation of substituted cyclobutanes and their use as intermediates for the preparation of anti-viral nucleoside analogs.
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: March 21, 1995
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Richard J. Pariza, Steven M. Hannick, Thomas J. Sowin, Elizabeth M. Doherty
  • Patent number: 5393788
    Abstract: Novel oxamide derivatives are described which inhibit the production of TNF and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds of the present invention are also useful as inhibitors of PDE IV and are therefor useful in the treatment of disease states mediated or exacerbated thereby.
    Type: Grant
    Filed: March 2, 1993
    Date of Patent: February 28, 1995
    Assignee: SmithKline Beecham Corporation
    Inventors: Paul E. Bender, Siegfried B. Christensen, IV, Klaus M. Esser, Cornelia J. Forster, Michael D. Ryan, Philip L. Simon
  • Patent number: 5391571
    Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl, phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R.sup.2 is hydrogen, alkyl or R.sup.1 taken with R.sup.2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: ##STR2## wherein ##STR3## in which R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: February 21, 1995
    Assignee: American Home Products Corporation
    Inventors: Richard E. Mewshaw, Thomas J. Commons, Donald P. Strike
  • Patent number: 5385900
    Abstract: A quinolone carboxylic acid derivative having the following formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH.sub.2, O, S, SO, SO.sub.2, or N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms; or a salt thereof; and an antimicrobial agent comprising the same. The compound exhibits a superior antimicrobial activity, especially against gram positive microorganisms, and is thus useful for the treatments and prevention of various infectious diseases in clinics.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: January 31, 1995
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Fujiko Konno, Akihiro Shibata, Hideaki Matsuda, Takemitsu Asaoka, Ryuichi Kawahara, Naokata Taido, Tadayuki Kuraishi, Sunao Takeda
  • Patent number: 5384404
    Abstract: An improved process for manufacturing melamine from urea simplifies the recovery of melamine, carbamate and ammonia from a fluidized bed reactor effluent stream by operating the process at a pressure between 1.4 and 2 MPa. In such a manner, a carbamate solution can be produced at a sufficiently high concentration for use in a urea plant without an intervening concentration step. In addition, ammonia recycled as a fluidizing gas can be condensed against cooling water to permit easy separation of noncondensables such as oxygen which used in the process as a passivator for carbamate corrosion inhibition. The melamine product is produced as an aqueous solution free of melamine solids. Heat is recovered from the carbamate condensation and used for the vaporization of ammonia which is recycled to the reactor for fluidization.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: January 24, 1995
    Inventor: Jing M. Lee
  • Patent number: 5384407
    Abstract: A compound of the formula ##STR1## V, W, Y, and Z are each independently C--H, oxygen, nitrogen, or sulfur; T is C--H or nitrogen;n is 0 or 1;R.sup.4 is hydrogen or one, two or three substituents independently selected from C.sub.1 -C.sub.4 -alkyl, halo-substituted C.sub.1 -C.sub.4 -alkyl, hydroxy-substituted C.sub.1 -C.sub.4 -alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 -alkoxy, mercapto, amino, mono-(C.sub.1 -C.sub.4 -alkyl)amino, di-(C.sub.1 -C.sub.4 -alkyl)amino, formamido, mono-(C.sub.1 -C.sub.4 -alkyl)amido, di-(C.sub.1 -C.sub.4 -alkyl)amido, cyano, nitro, C.sub.1 -C.sub.4 -alkoxycarbonyl, carboxyl, aminomethyl, mono-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, di-(C.sub.1 -C.sub.4 -alkyl)aminomethyl, wherein free hydroxy and amino groups may be protected.
    Type: Grant
    Filed: March 30, 1994
    Date of Patent: January 24, 1995
    Assignee: Warner-Lambert Company
    Inventors: Edgardo Laborde, Mel Schroeder
  • Patent number: 5382590
    Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl, alkoxycarbonyl or an unsubstituted or substituted phenyl radical,R.sub.2 represents a hydrogen atom or an unsubstituted or substituted alkyl radical,R.sub.3 represents an alkyl, phenylalkyl, indanyl, cycloalkylalkyl or an unsubstituted or substituted phenyl radical, orR.sub.2 and R.sub.3 form a heterocycle together with the nitrogen atom to which they are attached, andR.sub.4 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl or quinolyl radical or a phenylamino radical in which the phenyl ring is unsubstituted or substituted, their preparation and medicaments containing them.
    Type: Grant
    Filed: July 8, 1992
    Date of Patent: January 17, 1995
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
  • Patent number: 5382668
    Abstract: This invention relates to intermediates and processes thereto, for the preparation of 5,6-dihydropyrro[2,3-d]pyrimidines which are useful for the treatment of susceptible neoplasms.
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: January 17, 1995
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson