Patents Examined by Philip I. Datlow
  • Patent number: 5952494
    Abstract: There is disclosed a method for the preparation of pyrido benzoxazine derivative having the following formula I, that is improved in both production coat and yield.The method comprises reacting a compound of the following general formula II with tetraalkyl ammonium fluoride or with a mixture of tetraalkyl ammonium halide and metal fluoride in an organic solvent at a reaction temperature of about 30 to about 100.degree. C. for 1 to 3 hours under stirring; and reacting the resulting solution with a metal hydroxide or a metal carboxylate dissolved in water or in a mixture of water and alcohol, for 1 to 3 hours under heat. ##STR1## wherein X is a fluorine or chlorine atom and X.sub.1 and X.sub.2 each is a halogen atom or a nitro group, R is an alkyl group containing 1 to 4 carbon atoms and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each is an alkyd group or allyl group containing 1 to 8 carbon atoms.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: September 14, 1999
    Inventors: Youseung Kim, Soon Bang Kang, Seonhee Park
  • Patent number: 5847121
    Abstract: Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin, as well as related compounds, are described. Articles of manufacture useful in pretargeting methods are also discussed.
    Type: Grant
    Filed: December 13, 1995
    Date of Patent: December 8, 1998
    Assignee: NeoRx Corporation
    Inventors: Eric K. Yau, Louis J. Theodore, Linda M. Gustavson
  • Patent number: 5834609
    Abstract: The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds. The bicyclic aminoimidazole compounds of the invention have anti-tumor and anti-microbial activity.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: November 10, 1998
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: David A. Horne, Kenichi Yakushijin
  • Patent number: 5767272
    Abstract: Transition metal complexes of meso-haloalkylporphyrins, wherein the haloalkyl groups contain 2 to 8 carbon atoms have been found to be highly effective catalysts for oxidation of alkanes and for the decomposition of hydroperoxides. Also disclosed is a process for the preparation of meso-halocarbyl-porphyrins which comprises contacting a halocarbyl dipyrromethane with a halocarbyl-substituted aldehyde in the presence of an acid granular solid catalyst. Also disclosed is a process for the preparation of meso-halocarbyl-porphyrins which comprises contacting a halocarbyl dipyrromethane with a halocarbyl-substituted aldehyde in the presence of an acid granular solic catalyst.
    Type: Grant
    Filed: December 19, 1996
    Date of Patent: June 16, 1998
    Assignee: Sun Company, Inc. (R&M)
    Inventors: Tilak Wijesekera, James E. Lyons, Paul E. Ellis, Jr., Manoj V. Bhinde
  • Patent number: 5723457
    Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme and neutral endopeptidase and thus are useful as cardiovascular agents.
    Type: Grant
    Filed: July 8, 1996
    Date of Patent: March 3, 1998
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Jeffrey A. Robl
  • Patent number: 5721231
    Abstract: N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno ?3,2-f!?1,2,4!triazolo?4,3-a!?1,4!diazepin-6-yl )-N'- (2-methoxyphenyl)urea, optical isomers thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention strongly and selectively inhibit the expression of VCAM-1 and have an inhibitory effect on leukocyte adhesion to vascular endothelial cells. Accordingly, the compounds of the present invention can be used as cell adhesion inhibitors for prophylaxis or treatment of various diseases in which cell adhesion is involved in the onset and progress thereof.
    Type: Grant
    Filed: September 28, 1995
    Date of Patent: February 24, 1998
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Minoru Moriwaki, Hiroyuki Kitani, Syuji Ehara, Hirotsugu Komatsu, Mariko Amano
  • Patent number: 5708006
    Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 13, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
  • Patent number: 5707990
    Abstract: The invention relates to benzoxazine and pyrido-oxazine antibacterial compounds of the general formula: ##STR1## wherein the moiety Q is a fused phenyl or fused pyridyl moiety and R is a substituted amine or substituted thio moiety as herein described, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.
    Type: Grant
    Filed: January 30, 1996
    Date of Patent: January 13, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Roger Frechette, Michael Beach
  • Patent number: 5707988
    Abstract: Compounds of formula (I) ##STR1## in which X represents a group >O, >S, >C.dbd.O or >NR wherein R is hydrogen, C.sub.1-6 alkyl, phenyl or C.sub.7-12 phenalkyl, R.sub.1 and R.sub.2 each represent hydrogen or together represent an oxo group and R.sub.3, R.sub.4 and R.sub.5 each represent hydrogen or R.sub.1 represents hydrogen and two of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 together represent the second bond of a double bond joining positions 7 and 8, 8 and 9 or 9 and 10 with the remaining two of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 representing hydrogen, the compound optionally being in the form of a salt thereof formed with a physiologically acceptable inorganic or organic acid, are of value for the treatment of anxiety and in the improvement of learning ability and/or the reversal of amnesia.
    Type: Grant
    Filed: July 11, 1995
    Date of Patent: January 13, 1998
    Assignee: British Technology Group Ltd.
    Inventors: Edward Andrew Boyd, Brenda Costall, Mary Elizabeth Kelly, Philip James Parsons
  • Patent number: 5705639
    Abstract: This invention includes compounds of Formula II and IV and a process for preparing Formula I compounds by first preparing the compounds of Formula IV and then further reacting to form the compounds of Formula II and further reacting to prepare the compounds of Formula I wherein Q, Z, R.sup.2 are as defined within.
    Type: Grant
    Filed: September 21, 1995
    Date of Patent: January 6, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Rafael Shapiro
  • Patent number: 5703231
    Abstract: The present invention provides a process for making a compound having a structure according to Formula (I) ##STR1## wherein A.sup.1, A.sup.2 and A.sup.3 are independently carbon or nitrogen and R.sup.1, R.sup.3, R.sup.4 and R.sup.6 are known quinolone substituents; and wherein one of R.sup.1, R.sup.3 or R.sup.6 may be a lactam-containing moiety;or a protected form, salt, pharmaceutically-acceptable salt, biohydrolyzable ester, or solvate thereof;the process comprising reacting one or more organosilicon compounds with a compound having a structure according to Formula (II) ##STR2## wherein A.sup.1, A.sup.2 and A.sup.3, R.sup.1, R.sup.3, R.sup.4 and R.sup.6 as described above; wherein one of R.sup.1, R.sup.3 or R.sup.6 may be a lactam-containing moiety; and X is a leaving group;or a protected form, salt, biohydrolyzable ester, or solvate thereof.
    Type: Grant
    Filed: November 14, 1996
    Date of Patent: December 30, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Jared Lynn Randall, Jane Ellen Godlewski
  • Patent number: 5703072
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, substituted or unsubstituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from O, S, SO, SO.sub.2, CH.sub.2, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, and C.dbd.CHCN;X.sub.2 --- is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O)--;n is 1 or 2;R.sub.1 is selected from H and the .alpha.-carbon side chain of an amino acid;R.sub.2 and R.sub.3 are selected independently from H, OH, --NH.sub.2, --C(O)NH.sub.2 .dbd.O, .dbd.S,halo,cyano, C.sub.1-9 alkyl, C.sub.1-9 alkoxy, C.sub.1-4 alkylS--, C.sub.1-4 alkylSO--, C.sub.1-4 alkylSO.sub.2 --, phenoxy, benzyloxy and piperonyloxy; andH* is in either the R- or the S-configuration,and acid addition salts, solvates and hydrates thereof.
    Type: Grant
    Filed: April 1, 1996
    Date of Patent: December 30, 1997
    Assignee: Allelix Biopharmaceuticals
    Inventors: Patricia L. Power, Sumanas Rakhit
  • Patent number: 5700796
    Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.
    Type: Grant
    Filed: June 27, 1996
    Date of Patent: December 23, 1997
    Assignee: American Cyanamid Company
    Inventors: Jay Donald Albright, Aranapakam M. Venkatesan, John P. Dusza, Fuk-Wah Sum
  • Patent number: 5698563
    Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises bis(guanylhydrazone) of the formula ##STR1## capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: December 16, 1997
    Assignee: Alteon Inc.
    Inventors: Dilip R. Wagle, Michael E. Lankin, David H. Shih
  • Patent number: 5698552
    Abstract: The present invention relates to thienodiazepines of formula Ib: ##STR1## wherein U, V, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. This invention also relates to processes for preparing these thienodiazepines and their use in pharmaceutical compositions with PAF-antagonistic activity.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: December 16, 1997
    Assignee: Boehringer Ingelheim KG
    Inventors: Karl-Heinz Weber, Werner Stransky, Ulrike Kufner-Muhl, Hubert Heuer, Franz Birke, Wolf-Dietrich Bechtel
  • Patent number: 5698586
    Abstract: O-substituted fumagillol derivatives and its salts have an angiogenesis inhibiting activity and are useful for prophylaxis and treatment of diseases induced by abnormally stimulated neovascularization.
    Type: Grant
    Filed: July 21, 1992
    Date of Patent: December 16, 1997
    Assignee: Takeda Chemical Industries, Ltd
    Inventors: Shoji Kishimoto, Takeshi Fujita, Tsuneo Kanamaru, Moses Judah Folkman, Donald Ingber
  • Patent number: 5696112
    Abstract: This invention relates to bicyclic non-peptide vasopressin antagonists useful in treating conditions where decreased vasopressin levels are desired, in conditions with excess renal water reabsorption and in conditions with increased vascular resistance and coronary vasoconstriction, the compounds of this invention having the core structure of ##STR1## wherein: E--Y is selected from the moieties --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, and ##STR2## the moiety ##STR3## includes an optionally substituted, fused 6-membered heterocyclic aromatic ring containing two nitrogen atoms, a fused 5-membered heterocyclic aromatic ring containing either a) one heteroatom selected from O, S or N; b) two N atoms; or one N atom and one O or S atom;and R.sup.1, R.sup.2, R.sup.3 and R.sub.b are as defined herein.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: December 9, 1997
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Efren G. Delos Santos
  • Patent number: 5696117
    Abstract: The invention relates to benzoxazine and pyrido-oxazine antibacterial compounds of the general formula: ##STR1## wherein the moiety Q is a fused phenyl or fused pyridyl moiety as herein described, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.
    Type: Grant
    Filed: November 7, 1995
    Date of Patent: December 9, 1997
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Roger Frechette, Michele Ann Weidner-Wells
  • Patent number: 5696123
    Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 9, 1997
    Assignee: Boehringer Ingelheim KG
    Inventors: Horst Dollinger, Gerd Schorrenberg, Hans Briem, Birgit Jung, Georg Speck
  • Patent number: 5696258
    Abstract: According to the invention, a process for the preparation of triphendioxazines symmetrically or asymmetrically amidated on both sides comprises reducing a triphendioxazine chromophore, which is optionally already amidated on one side, to give the leuco form and amidating and re-oxidizing the leuco form. Products amidated on both sides are obtained in this manner with a high yield and product quality. Novel triphendioxazine dyestuffs are furthermore prepared in this manner.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: December 9, 1997
    Assignee: DyStar Textilfarben GmbH
    Inventors: Christian Schumacher, Karl-Josef Herd