Patents Examined by L. Eric Crane
  • Patent number: 5484774
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein X is halogen, trifluoromethyl, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, C.sub.1-6 -alkylamino or C.sub.1-6 -dialkylamino;R.sup.1 and R.sup.4 are H or straight or branched C.sub.1-6 -alkyl or trifluoromethyl or R.sup.1 and R.sup.4 together form a cycloalkyl ring;Y is O, S, SO.sub.2, NH or N-alkyl;R.sup.5 is selected from optionally substituted heterocycles.R.sup.6 and R.sup.7 are hydrogen, benzoyl or C.sub.1-6 -alkanoyl.The compounds have been found useful for treating central nervous system and cardiovascular ailments.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: January 16, 1996
    Assignee: Novo Nordisk A/S
    Inventors: Jesper Lau, Lars J. S. Knutsen, Malcolm Sheardown, Anker J. Hansen
  • Patent number: 5480982
    Abstract: The present invention relates to a novel crystalline thio-NADP potassium salt, which is produced by preparing thionicotinamide adenine dinucleotide phosphate (thio-NADP) into the potassium salt thereof and thereafter crystallizing the salt. Conventionally known non-crystalline thio-NADP sodium salt has a strong hygroscopic property to deliquesce on contact with air, of which the storage is therefore difficult. The crystalline thio-NADP potassium salt of the present invention has no hygroscopic property so that it does not deliquesce on contact with air, which can be used as research reagents, diagnostic agents and the like for a long period of time and which can be stored for a long period of time.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: January 2, 1996
    Assignee: Oriental Yeast Company, Ltd.
    Inventors: Kouji Sugita, Tetsuo Kitahara, Masatsugu Nonobe, Tsuyosi Fujita
  • Patent number: 5478928
    Abstract: 2',3'-dideoxy-4'-thioribonucleosides useful as antiviral agents in the treatment and prevention of AIDS are disclosed. In accordance with one aspect of the invention there are provided compounds of the formula ##STR1## where X.dbd.H, N.sub.3 or F, and B is a member selected from the group consisting of pyrimidine, 5-azapyrimidine, 6-azapyrimidine, 3-deazapyrimidine, purine, 3-deazapurine, 7-deazapurine, 8-azapurine, and 2-azapurine bases. The intermediate 1-O-acetyl-5-O-t-butyldiphenylsilyl-4-thio-2,3-dideoxyribofuranose is useful in the production of certain of the 2',3'-dideoxy-4'-thioribonucleosides. Other intermediates include the 4-thio-2,3-dideoxyribofuranose having different hydroxyl protecting groups and leaving groups.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: December 26, 1995
    Assignee: Southern Research Institute
    Inventors: John A. Montgomery, John A. Secrist, III
  • Patent number: 5476925
    Abstract: Novel oligonucleotides, method for improving the hybridization properties of oligonucleotides and novel processes for preparing 3'-phosphorylated oligonucleotides.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: December 19, 1995
    Assignee: Northwestern University
    Inventors: Robert L. Letsinger, Sergei M. Gryaznov
  • Patent number: 5472947
    Abstract: A composition for the treatment or prevention of multiple sclerosis is disclosed. It comprises mizoribine (4-carbamoyl-1-.beta.-D-ribofuranosyl imidazolium-5-olate) as the effective component. It is a safe drug, exhibiting a minimal degree of side-effects, and thus can be administered over a long period of time. Administration of the drug, usually 1-20 mg/kg (body weight) per day for adults, improves the functional disturbances of multiple sclerosis.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: December 5, 1995
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Takahiko Saida, Kyoko Saida
  • Patent number: 5473063
    Abstract: Compounds of formulae ##STR1## wherein X is O;R.sup.1 is OH, phosphate, diphosphate, triphosphate or (CH.sub.2).sub.n --O--CH.sub.2 --O--P(.dbd.O)(OH).sub.2 wherein n is 0-2;R.sup.2 is H and R.sup.3 is CH.sub.3, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 SH, CH.sub.2 F or CH.sub.2 N.sub.3 ; orR3 is H and R.sup.2 is CH.sub.3, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 SH, CH.sub.2 F or CH.sub.2 N.sub.3 ;and Z is Cl, Br, I, acyloxy or alkoxy;are synthesized from acyclic intermediates and are subsequently useful in the preparation of nucleoside analogues with antiviral activity against retroviruses such as HIV and hepatitis B.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: December 5, 1995
    Assignee: Medivir AB
    Inventors: Bjorn O. Classon, Bengt B. Samuelsson, Imgemar S. Kvarnstrom, Lars G. Svansson, Stefan C. T. Svensson
  • Patent number: 5470837
    Abstract: The present invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of certain 5'-vinylhalo-aristeromycin/adenosine analogs.
    Type: Grant
    Filed: June 16, 1994
    Date of Patent: November 28, 1995
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Jeffrey A. Wolos, Niall S. Doherty, Esa T. Jarvi, James R. McCarthy
  • Patent number: 5466678
    Abstract: A pharmaceutical composition for use as a nephrotoxicity alleviator for alleviating the nephrotoxicity caused by a drug administered into the living organism, which composition contains S-adenosyl-L-methionine or a salt thereof as an active ingredient is provided. Also provided is a pharmaceutical composition for use as an agent for potentiating the antitumor activity of platinum complex compounds, which composition contains S-adenosyl-L-methionine as an active ingredient.
    Type: Grant
    Filed: April 7, 1994
    Date of Patent: November 14, 1995
    Assignee: Fuji Kagaku Kogyo Kabushiki Kaisha
    Inventors: Hironori Kawabata, Koei Moriguchi, Takeshi Endo
  • Patent number: 5466677
    Abstract: A dinucleotide analogue of formula ##STR1## where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical;R.sup.1 is R.sup.1.sub.a or Z;R.sup.1.sub.a, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, halogen or hydroxy;R.sup.5 is R.sup.5.sub.a or Z;R.sup.6 is hydrogen or R.sup.6.sub.a ;R.sup.7 is hydrogen, alkyl-N,N-dialkylphosphoramidyl or R.sup.7.sub.a, R.sup.8 is R.sup.8.sub.a or Z, or the indicated R.sup.7 O and R.sup.8 together denote an isopropylidenedioxy group;R.sup.5.sub.a and R.sup.8.sub.a are each independently hydrogen, halogen, hydroxy, --OR.sup.10, --OCOR.sup.10 or silyloxy substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.6.sub.a and R.sup.7.sub.a are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.30 araliphatic radical, --COR.sup.11, --SO.sub.2 R.sup.11 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.9 is hydrogen, a C.sub.1 -C.sub.
    Type: Grant
    Filed: February 28, 1994
    Date of Patent: November 14, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Anthony D. Baxter, Eric K. Baylis, Stephen P. Collingwood, Roger J. Taylor, Alain De Mesmaeker, Chantal Schmit
  • Patent number: 5462929
    Abstract: A composition for curing proliferative skin diseases containing 4-carbamoyl-1-.beta.-D-ribofuranosyl-imidazolium 5-olate (mizoribine) as an active ingredient. It has a potent activity of inhibiting the growth of keratinocytes and an improved effect of curing psoriasis, so that it is useful for curing proliferative skin diseases. Further it has only an extremely reduced toxicity, is highly safe, and can be administered for long and perorally.
    Type: Grant
    Filed: April 11, 1994
    Date of Patent: October 31, 1995
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Makoto Kawashima, Kazuhiro Nagano, Kazuyoshi Hori, Hiroaki Ishikawa, Masataka Morishita
  • Patent number: 5459132
    Abstract: The present invention relates to the derivatives of the formula ##STR1## and their addition salts, and to their use in therapeutics as analgesics, as antihypertensives and as drugs with antiproliferative properties.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: October 17, 1995
    Assignee: Laboratoires UPSA
    Inventors: Nicole Bru-Magniez, Timur Gungor, Jean-Marie C. Teulon
  • Patent number: 5459254
    Abstract: The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## [I] A=a leaving group, [II] A=NH.sub.2,[V] A=NHR.sup.4,wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.
    Type: Grant
    Filed: November 10, 1993
    Date of Patent: October 17, 1995
    Assignees: Yamasa Shoyu Kabushiki Kaisha, Toa Eiyo Ltd.
    Inventors: Toyofumi Yamaguchi, Takanori Miyashita, Shinji Sakata, Toichi Abiru, Akira Matsuda, Tohru Ueda, Kentaro Kogi
  • Patent number: 5455234
    Abstract: Mammalian hair growth is reduced by applying to the skin an inhibitor of a cysteine synthetic pathway enzyme.
    Type: Grant
    Filed: March 16, 1994
    Date of Patent: October 3, 1995
    Inventors: Gurpreet S. Ahluwalia, Douglas Shander
  • Patent number: 5451671
    Abstract: A crude 2',3'-dideoxynucleoside compound is purified by extracting with an organic solvent, or crystallizing, the 2',3'-dideoxynucleoside compound from a basic aqueous solution having a pH of not less than 12 containing the same. In another embodiment of purification a basic aqueous solution having a pH of not less than 11 of a crude 2',3'-dideoxynucleoside derivative is brought into contact with a nonpolar porous resin, whereby the derivative is adsorbed on the resin, and then the thus adsorbed derivative is desorbed with an aqueous alcoholic solution.2',3'-Dideoxynucleoside compounds which have utility as anti-AIDS drugs or anti-virus drugs can be isolated and purified in high purity and in high yield from their crude products containing impurities.
    Type: Grant
    Filed: June 16, 1993
    Date of Patent: September 19, 1995
    Assignee: Ajinomoto Co., Inc.
    Inventors: Hiroshi Shiragami, Masayuki Arai, Kunisuke Izawa, Yutaka Honda, Yasuhiro Tanaka, Toshihide Yukawa, Satoji Takahashi
  • Patent number: 5449665
    Abstract: This invention is concerned with the use of adenosine as an agent for the treatment of human beings. More particularly, this invention is concerned with the administration of adenosine to human patients by continuous intravenous infusion for, inter alia, control of blood pressure, use as a selective vasodilator, decreasing pulmonary vascular resistance, treating acute pulmonary hypertension in conjunction with idiopathic respiratory distress syndrome, in diagnosing pulmonary hypertension in conjunction with cardiac septum defects, in percutaneous transluminal angioplasty (PTCA), in coronary thrombolysis (CTL) and in radionucleide scintography.
    Type: Grant
    Filed: December 15, 1993
    Date of Patent: September 12, 1995
    Assignee: Item Development Aktiebolag
    Inventor: Alf Sollevi
  • Patent number: 5446031
    Abstract: The present invention relates to a novel 1-.beta.-D-arabinofuranosyl-(E)-5-(2-halogenovinyl)uracil derivative represented by the following formula (I), whose concentration in blood as XVAU can be kept high for many hours when it is administered orally.The present invention also relates to an antiviral agent comprising as an active ingredient the compound of the present invention.Further, the present invention relates to a method for treating viral diseases which comprises administering to a patient with a viral disease a safe and effective amount of the compound of the present invention. ##STR1## wherein X represents a halogen; and R.sup.1, R.sup.2, and R.sup.3, which may be the same or different, each represent a hydrogen atom, a lower alkyl group or an aralkyl group, provided that R.sup.1, R.sup.2 and R.sup.3 are not hydrogen at the same time.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: August 29, 1995
    Assignee: Yamasa Shuyu Kabushiki Kaisha
    Inventors: Shinji Sakata, Haruhiko Machida, Katsushi Ijichi, Fumitaka Kano
  • Patent number: 5441942
    Abstract: Immunostimulating 7,8-disubstituted guanine derivatives that also contain a .beta.-9,1'-linked-2',3'-dideoxy-2',3'-didehydroribosyl substituent are disclosed whose structures are represented by Formula I ##STR1## wherein X is O or S; R.sup.1 is a hydrocarbyl or substituted hydrocarbyl moiety having a length of about one to about seven carbon atoms; R.sup.2 is hydrogen or C.sub.1 -C.sub.8 acyl; and the pharmaceutically acceptable base addition salts thereof. Also disclosed are compositions containing an immunostimulating guanine derivative and processes for using the same.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: August 15, 1995
    Assignee: The Scripps Research Institute
    Inventors: Michael G. Goodman, Robert Chen, Allen Reitz
  • Patent number: 5438130
    Abstract: A compound consisting of a base, a ribose and a fucose, in which the base is a purine or a pyrimidine, the ribose has R.sub.1 and R.sub.2 attached respectively to any two of 2'-O, 3'-O and 5'-O, and the fucose has R.sub.3, R.sub.4 and R.sub.5 attached respectively to any three of 1"-O, 2"-O, 3"-O and 4"-O, wherein each R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is H, acetate, sulfate, phosphate, or a metallic salt of acetate, sulfate or phosphate; and the base is linked to the ribose via a bond between 9-N of the base and 1'-O of the ribose when the base is a purine or via a bond between 1-N of the base and 1'-C of the ribose when the base is a pyrimidine and the ribose is linked to the fucose via a bond between any one of 2'-O, 3'-O and 5'-O of the ribose and 1"-C of the fucose.
    Type: Grant
    Filed: January 15, 1993
    Date of Patent: August 1, 1995
    Assignees: Cambridge NeuroScience, Inc., Cornell Research Foundation, Inc.
    Inventors: Stanley Goldin, James Fisher, Kazumi Kobayashi, Laxma Reddy, Andy Knapp, Lee Margolin, Kevin D. McCormick
  • Patent number: 5438127
    Abstract: The present invention relates to modified glass fiber membranes which exhibit sufficient hydrophilicity and sufficient electropositivity to bind DNA from a suspension containing DNA and permit elution of the DNA from the membrane. Generally, the hydrophilic and electropositive characteristics are expressed at the surface of the modified glass fiber membrane. Preferred modified glass fiber membranes of the present invention include glass fiber membranes that have been modified by treatment with trifluoroacetic acid (TFA), BCl.sub.3, SiCl.sub.4, NaOH, F.sup.-, AlCl.sub.3 alone or in combination, with or without water. The modified glass fiber membranes of the present invention are particularly useful in processes for purification of DNA from other cellular components.
    Type: Grant
    Filed: September 27, 1993
    Date of Patent: August 1, 1995
    Assignee: Becton Dickinson and Company
    Inventors: Daniel L. Woodard, Adriann J. Howard, James A. Down
  • Patent number: 5434086
    Abstract: Cystic fibrosis (CF), a lethal genetic disease associated with a defect in Cl transport, is caused by mutations in the gene coding for cystic fibrosis transmembrane conductance regulator (CFTR). Surprisingly, not only wild type CFTR, but several naturally-occurring CFTR mutants carrying a defect in the first nucleotide binding fold (NFB1) all expressed cAMP-activatable Cl currents. Treatment of the CFTR mutants with appropriate concentrations of methylxanthine phosphodiesterase inhibitor (which increases cAMP levels) activated Cl conductance to near wild type levels. The present invention thus provides a new avenue for treating cystic fibrosis by the administration of therapeutically effective amounts of compounds which elevate cAMP levels. Dosage and patient responsiveness to treatment, as well as relative efficacies of the compounds being or to be administered can also be determined in accordance with the methods of present invention.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: July 18, 1995
    Assignee: The Regents of the University of Michigan
    Inventors: Francis S. Collins, Mitchell L. Drumm, David C. Dawson, Daniel J. Wilkinson