Patents Examined by L. Eric Crane
  • 2'-deoxy-2',2'-difluoro (4-substituted pyrimidine) nucleosides, bicyclic derivatives,pharmaceutical compositions, and synthetic precursors
    Patent number: 5430026
    Abstract: The invention provides certain 2-Deoxy-2,2-Difluoro (4-Substituted) Pyrimidine Nucleosides that are effective as anti-cancer agents and in treating viral infections.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: July 4, 1995
    Assignee: Eli Lilly and Company
    Inventors: Larry Hertel, Julian S. Kroin
  • 2-chloro-N.sup.6 -substituted adenosines, their pharmaceutical compositions, and activity in treating ischemias
    Patent number: 5430027
    Abstract: Adenosine compounds having the following structure ##STR1## wherein X is halogen, perhalomethyl, acetamido, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio or C.sub.1-6 -alkylamino; andR.sup.1 is --NR.sup.2 R.sup.3 or YR.sup.4, wherein Y is oxygen or sulfur;R.sup.2 is phenyl, C.sub.1-6 -alkyl or substituted C.sub.1-6 -alkyl; andR.sup.4 is naphthyl, partly saturated naphthyl; optionally phenyl or phenoxy substituted C.sub.1-6 -alkyl wherein the phenyl and phenoxy substituents are also optionally substituted, or optionally phenyl or phenoxy substituted C.sub.3-8 -cycloalkyl and their pharmaceutically acceptable salts are useful in the treatment of myocardial and cerebral ischemias.
    Type: Grant
    Filed: May 14, 1993
    Date of Patent: July 4, 1995
    Assignee: Novo Nordisk A/S
    Inventors: Lars J. S. Knutsen, Jesper Lau
  • N.sup.4 - acylated cytidinyl compounds useful in oligonucleotide synthesis
    Patent number: 5428148
    Abstract: Disclosed herein are protecting groups for exocyclic amino groups of the bases adenine, guanine and cytosine for use in the synthesis of oligonucleotides, the protecting groups being represented by the formula: --CO-- (CH.sub.2).sub.0-9 --CH.sub.3. In a particularly preferred embodiment, the base cytosine is protected with acetyl (--CO--CH.sub.3), and the oligonucleotide incorporating said protected cytosine is subjected to a cleavage/deprotection reagent comprising at least one straight chain alkylamine having from 1 to about 10 carbon atoms.
    Type: Grant
    Filed: April 24, 1992
    Date of Patent: June 27, 1995
    Assignee: Beckman Instruments, Inc.
    Inventors: Parameswara M. Reddy, Naeem B. Hanna
  • 2-Halo-2'-deoxyadenosines as therapeutic agents against malignant astrocytoma
    Patent number: 5424296
    Abstract: A process for the treatment of malignant astrocytoma in mammals is disclosed that utilizes a 2-halo-2'-deoxyadenosine derivative as the active treating agent.
    Type: Grant
    Filed: April 15, 1993
    Date of Patent: June 13, 1995
    Assignee: The Scripps Research Institute
    Inventors: Alan Saven, Lawrence D. Piro
  • Process for preparation of 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy protected-1-alkyl and aryl sulfonates and their use in preparation of 2',2'-difluoro-2'-deoxy nucleosides
    Patent number: 5424416
    Abstract: A stereoselective process for preparing a .beta.-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy protected-1-alkyl and aryl sulfonate intermediates by contacting an .alpha.-anomer enriched 2-deoxy-2,2-difluoro-D- ribofuranosyl-3,5-hydroxy protected-1-fluoroalkyl and fluoroaryl sulfonate with a conjugate anion of a sulfonic acid containing the desired alkyl or aryl sulfonate.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: June 13, 1995
    Assignee: Eli Lilly and Company
    Inventor: Charles D. Jones
  • Topical powder compositions containing a cyclic AMP derivative
    Patent number: 5424298
    Abstract: A topical powder composition containing a cyclic AMP derivative and a water-absorptive powdery material. The topical powder composition is useful for wet dermatoses. Release of drug can be controlled.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: June 13, 1995
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Norio Takasugi, Eiichi Mafune, Toshiyuki Takayasu
  • Method of characterizing genomic DNA by reference to a genetic variable
    Patent number: 5413908
    Abstract: It has been a problem that the identification of genomic DNA by restriction fragment length polymorphisms is limited, owing to the low level of genetic variation ordinarily detectable by cloned DNA in this method. The invention provides for improved identification by making use of the existence of DNA regions of hypervariability, otherwise called minisatellite regions in which the DNA contains tandem repeats or quasi-block copolymer sequences and the number of repeats or copolymer units varies considerably from one individual to another. It has now been found that many such regions can be probed simultaneously in such a way as to display this variability using a DNA or other polynucleotide probe of which the essential constituent is a short core sequence tandemly repeated at least 3 and preferably at least 10 times.
    Type: Grant
    Filed: July 29, 1992
    Date of Patent: May 9, 1995
    Assignee: Lister Institute of Preventive Medicine
    Inventor: Alec J. Jeffreys
  • Non-nucleoside linkers for convenient attachment of labels to oligonucleotides using standard synthetic methods
    Patent number: 5414077
    Abstract: Pseudonucleosides and pseudonucleotides are useful in the synthesis of oligomers which contain these components as a means to derivatize the resulting oligonucleotide to useful substituents such as chelators, intercalators, or lipophilic compounds. In general, these pseudonucleotide components are of the formula: ##STR1## wherein each Y is independently O or S; each X is independently H, PO.sub.3.sup.-2, an activated nucleotide synthesis coupling moiety, a protecting group, a nucleoside, a nucleotide or a nucleotide sequence, or comprises a solid support;F is a functional group capable of linking an additional moiety or said group already reacted to effect the binding of said additional moiety;.quadrature.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: May 9, 1995
    Assignee: Gilead Sciences
    Inventors: Kuei-Ying Lin, Mark Matteucci
  • Deoxygenation of cis vicinal diols to make didehydro dideoxy nucleosidies and synthetic intermediates
    Patent number: 5410033
    Abstract: Cis vicinal diols are converted to olefins using tellurides or selenide reagents. The diol is reacted to convert the hydroxyl groups into good leaving groups for nucleophilic substitution. Alkyl and aryl sulfonate groups such as mesylate or tosylate are preferred. The product is then reacted with a source of Te.sup.2- or Se.sup.2- ions, preferably an alkali metal telluride or selenide, to form the desired olefin. The process is particularly useful for generating 2',3'-unsaturation in the sugar moiety of nucleosides. Novel intermediate mesylate, tosylate and olefin derivatives of nucleosides are also provided.
    Type: Grant
    Filed: February 3, 1993
    Date of Patent: April 25, 1995
    Assignee: Terochem Laboratories Limited
    Inventors: Derrick L. J. Clive, Philip L. Wickens
  • N.sup.4 -substituted cytidines and process for incorporation into an oligonucleotides
    Patent number: 5405950
    Abstract: An oligonucleotide containing at least one cytidine analog labeled at C4 with a reporter group.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: April 11, 1995
    Assignee: Amoco Corporation
    Inventors: Graham A. Mock, Douglas H. Lovern
  • 2',5'-phosphorothioate oligoadenylates and their covalent conjugates with polylysine
    Patent number: 5405939
    Abstract: Optically active compounds of the formula ##STR1## wherein n is 1 or 2 and m is 0, 1, 2 or 3 have antiviral activity. Compounds of the formula wherein at least one of the internucleotide phosphorothioate linkages is of the Sp configuration possess increased antiviral activity and/or metabolic stability.
    Type: Grant
    Filed: July 16, 1992
    Date of Patent: April 11, 1995
    Assignee: Temple University of the Commonwealth System of Higher Education
    Inventors: Robert J. Suhadolnik, Wolfgang Pfleiderer
  • Topical powder compositions containing a cyclic AMP derivative
    Patent number: 5405838
    Abstract: A topical powder composition containing a cyclic AMP derivative and a water-absorptive powdery material. The topical powder composition is useful for wet dermatoses. Release of drug can be controlled.
    Type: Grant
    Filed: September 27, 1991
    Date of Patent: April 11, 1995
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Norio Takasugi, Eiichi Mafune, Toshiyuki Takayasu
  • Therapeutic treatment of chronic myelogenous leukemia by administration of 2-chloro-2'-deoxy adenosine
    Patent number: 5401724
    Abstract: A process for the treatment of chronic myelogenous leukemia in mammals is disclosed that utilizes a 2-halo-2'-deoxyadenosine derivative as the active treating agent.
    Type: Grant
    Filed: February 25, 1994
    Date of Patent: March 28, 1995
    Assignee: The Scripps Research Institute
    Inventor: Ernest Beutler
  • Neovascularization inhibition by adenosine-5'-phosphosulfates
    Patent number: 5401725
    Abstract: The present invention provides, as a noval and safe vascularization inhibitor having an excellent effect, a vascularization inhibitor which is characterized by containing, as the effective ingredient, 3-phosphoadenosine 5'-phosphosulfate or adenosine 5'-phosphosulfate which is expressed by the following general formula: ##STR1## (where, x represents a phosphate or hydroxide group) or a pharmaceutically allowable salt thereof.
    Type: Grant
    Filed: October 25, 1993
    Date of Patent: March 28, 1995
    Assignee: Unitika Ltd.
    Inventors: Satoshi Kawanaka, Munehiko Dombou, Hiroshi Nakajima
  • Method for preparing N.sup.6 -substituted NAD, NADP or FAD
    Patent number: 5399681
    Abstract: The invention relates to a method of preparing N.sup.6 -substituted NAD, NADP or FAD by Dimroth rearrangement, wherein the rearrangement is carried out without preceding reduction and subsequent reoxidation.
    Type: Grant
    Filed: January 24, 1990
    Date of Patent: March 21, 1995
    Assignees: Gesellschaft fur Biotechnologische Forschung mbH (GBF), Degussa AG
    Inventor: Andreas F. Buckman
  • Linkers for the synthesis of multiple oligonucleotides in seriatim from a single support attachment
    Patent number: 5393877
    Abstract: A method for the synthesis of a plurality of oligonucleotides comprising the steps of(i) forming a first oligonucleotide on a first cleavable link attached to a solid support;(ii) attaching to the first oligonucleotide a cleavable linker moiety;(iii) forming a second oligonucleotide on the cleavable linker moiety; and(iv) cleaving the first cleavable link and the cleavable linker moiety to give a plurality of oligonucleotides; wherein the cleavable linker moiety is of the Formula (1): ##STR1## in which A.sup.1, A.sup.2 and E are as defined herein, and novel compounds which may be used in the operation of the method.
    Type: Grant
    Filed: April 5, 1993
    Date of Patent: February 28, 1995
    Assignee: Zeneca Limited
    Inventors: Michael J. McLean, David Holland, Andrew J. Garman, Robert C. Sheppard
  • Intermediates for providing functional groups on the 5' end of oligonucleotides
    Patent number: 5391785
    Abstract: Phosphoramidites of the formula ##STR1## where R is a base-labile protecting group, R.sup.1 and R.sup.
    Type: Grant
    Filed: July 15, 1992
    Date of Patent: February 21, 1995
    Assignee: La Jolla Pharmaceutial Company
    Inventors: David S. Jones, John P. Hachmann, Michael J. Conrad, Stephen Coutts, Douglas A. Livingston
  • 2'-fluoro-2-haloarabinoadinosines and their pharmaceutical compositions
    Patent number: 5384310
    Abstract: The present invention is directed to certain 2'-fluoro, 2-substituted purine nucleosides which are toxic to cancerous cell lines.
    Type: Grant
    Filed: May 10, 1991
    Date of Patent: January 24, 1995
    Assignee: Southern Research Institute
    Inventors: John A. Montgomery, John A. Secrist, III
  • Ap.sub.4 A as a hypotensive agent
    Patent number: 5380715
    Abstract: A deliberated hypotensive agent is composed of diadenosine 5', 5'"-p.sup.1,p.sup.
    Type: Grant
    Filed: February 25, 1993
    Date of Patent: January 10, 1995
    Assignees: Fujirebio Inc., Unitika Ltd.
    Inventors: Akihiro Sekine, Yoshinori Kikuta, Shinkichi Tezuka, Kazuo Okada, Hiroshi Nakajima
  • 2'-halomethylidene cytidine, uridine and guanosine compounds and their pharmaceutical compositions
    Patent number: 5378693
    Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
    Type: Grant
    Filed: August 27, 1993
    Date of Patent: January 3, 1995
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews