Patents Examined by Matthew V. Grumbling
  • Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents
    Patent number: 5631369
    Abstract: Novel processes for producing compounds of formula I ##STR1## wherein R.sup.1 and R.sup.2 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; andn is 2 or 3;or a pharmaceutically acceptable salt thereof employing alkylacetate solvents are provided.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: May 20, 1997
    Assignee: Eli Lilly and Company
    Inventors: Douglas P. Kjell, Fred M. Perry
  • Process for preparing compounds containing a fused bicyclic ring
    Patent number: 5627278
    Abstract: A process for preparing compounds of the formula ##STR1## wherein X is O or S; n is one or two; m is zero or one; Y is CH.sub.2, O, or S provided that Y is O or S only when m is one; and A is ##STR2## is disclosed. Also disclosed are processes for preparing the corresponding amino intermediates.
    Type: Grant
    Filed: January 4, 1996
    Date of Patent: May 6, 1997
    Assignee: Bristol-Myers Squibb Co.
    Inventor: Jeffrey A. Robl
  • Carbocyclic nucleoside analogs useful as immunosuppressants
    Patent number: 5624930
    Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: March 22, 1995
    Date of Patent: April 29, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
  • Compounds useful in preparing antiproliferative agents and garft inhibitors
    Patent number: 5625061
    Abstract: Compounds of the invention include those of the following formula: ##STR1## In this formula, A is oxygen, sulfur or selenium; X' is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl group, a substituted or unsubstituted C.sub.2 -C.sub.3 alkenyl group, a substituted or unsubstituted C.sub.2 -C.sub.3 alkynyl group, a substituted or unsubstituted amino group, sulfur or oxygen; Y is oxygen, sulfur or NH; B is hydrogen or a halogen; C is hydrogen, a halogen or a substituted or unsubstituted C.sub.1 -C.sub.6 alkyl group; and R.sub.6 is hydrogen or a moiety that forms with the attached CO.sub.2 a readily hydrolyzable ester group.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 29, 1997
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
  • Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
    Patent number: 5620981
    Abstract: 6-Aryl pyrido[2,3-d]pyrimidine 7-imines, 7-ones, and 7-thiones are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.
    Type: Grant
    Filed: May 3, 1995
    Date of Patent: April 15, 1997
    Assignee: Warner-Lambert Company
    Inventors: Clifton J. Blankley, Diane H. Boschelli, Annette M. Doherty, James M. Hamby, Sylvester Klutchko, Robert L. Panek
  • Biologically active acylated amino acid derivatives
    Patent number: 5620971
    Abstract: The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: April 15, 1997
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David M. Armistead, Jeffrey O. Saunders, Joshua S. Boger
  • 8-aza, 6-aza and 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones and the use thereof as antagonists for the glycine/NMDA receptor
    Patent number: 5620978
    Abstract: Disclosed is a method of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma or hypoglycemia. The method comprises administering to an animal a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof; wherein n is zero or 1; R.sup.4, R.sup.5, R.sup.6 are independently hydrogen, nitro, amino, halo, haloalkyl, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, azido, acylamino, alkylsulfonyl, aryl, substituted aryl, heteroaryl, alkoxy, trialkylsilyl-substituted alkoxy, aryloxy, substituted aryloxy, heteroaryloxy, a heterocyclic group, a heterocyclicoxy group, aralkoxy, or haloalkoxy; and R.sup.c and R.sup.d are defined in the specification. These compounds have high binding to the glycine site of the NMDA receptor.
    Type: Grant
    Filed: January 3, 1995
    Date of Patent: April 15, 1997
    Assignees: State of Oregon, acting by and through The Oregon State Board of Higher Education, acting for and on behalf of The Oregon Health Sciences University and The University of Oregon, Eugene Oregon, The Regents of the University of California, ACEA Pharmaceuticals, Inc.
    Inventors: Sui X. Cai, John F. W. Keana, Eckard Weber
  • Antimigraine 1,2,5-thiadiazole derivatives of indolylalkyl-pyridnyl and pyrimidinylpiperazines
    Patent number: 5618816
    Abstract: A series of novel 5-(3,4-diamino-1,2,5-thiadiazole and S-oxide) derivatives of indolylalkylpiperazinyl pyridines and pyrimidines of Formula I are intended for use in the alleviation of vascular headaches. ##STR1## In Formula I, X is selected from S, SO and SO.sub.2.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: April 8, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronnie R. Crenshaw, Edward H. Ruediger, David W. Smith, Carola Solomon, Joseph P. Yevich
  • Process for preparing homocystein analogs useful as intermediates for compounds containing a fused bicyclic ring
    Patent number: 5616775
    Abstract: Homocysteine analogs of the formula ##STR1## wherein P.sub.1 is a nitrogen protecting group and R.sub.6 is alkyl, substituted alkyl or benzyl are prepared by esterifying N-protected L-methionine, oxidizing, treating the resulting sulfoxide with an acid anhydride, treating the resulting product with an alkali metal hydroxide followed by removal of formaldehyde and the treatment with an acid anhydride or acid halide. The L-homocysteine analogs are useful as intermediates in the preparation of compounds containing a fused bicyclic ring.
    Type: Grant
    Filed: February 5, 1996
    Date of Patent: April 1, 1997
    Assignee: Bristol-Myers Squibb Co.
    Inventors: David R. Kronenthal, Jollie D. Godfrey, Jr.
  • Quinazoline derivatives as anti-proliferative agents
    Patent number: 5616582
    Abstract: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein m is 1, 2 or 3 and each R.sup.1 includes hydroxy, amino, carboxy, carbamoyl, ureido, (1-4C)alkoxycarbonyl, N-(1-4C)alkylcarbamoyl, N,N-di-[(1-4C)alkyl]carbamoyl, hydroxyamino, (1-4C)alkoxyamino, (2-4C)alkanoyloxyamino, trifluoromethoxy, (1-4C)alkyl, (1-4C)alkoxy and (1-3C)alkylenedioxy;n is 1 or 2 and each R.sup.2 includes hydrogen, hydroxy, halogeno, trifluoromethyl, amino, nitro, cyano and (1-4C)alkyl; or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of cancer.
    Type: Grant
    Filed: June 15, 1995
    Date of Patent: April 1, 1997
    Assignee: Zeneca Limited
    Inventor: Andrew J. Barker
  • 2-cyano-1-aminobenzene compounds
    Patent number: 5616718
    Abstract: A compound having the formula: ##STR1## wherein W, X, Y, and Z are as defined in the specification is useful for making 2,4-diaminoquinazolines.
    Type: Grant
    Filed: April 20, 1995
    Date of Patent: April 1, 1997
    Assignee: FMC Corporation
    Inventors: Robert N. Henrie, II, Clinton J. Peake, Thomas G. Cullen, Walter H. Yeager, John W. Buser, James J. Fiordeliso, John A. Dixson
  • Quinazoline compounds
    Patent number: 5614627
    Abstract: It relates to a quinazoline compound useful as a medicine exhibiting an inhibitory action on calmodulin-dependent cGMP-PDE.A quinazoline compound represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group or the like; and R.sup.6 and R.sup.7 may be the same or different from each other and each represents a hydrogen atom, a carboxyl alkyl group or the like).
    Type: Grant
    Filed: June 27, 1995
    Date of Patent: March 25, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Yasutaka Takase, Nobuhisa Watanabe, Hideyuki Adachi, Kohtaro Kodama, Hiroki Ishihara, Takao Saeki, Shigeru Souda
  • Amino acid derivatives of substituted quinoxaline 2,3-dione derivatives as glutamate receptor antagonists
    Patent number: 5614508
    Abstract: A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, Alzheimer's, Parkinson's, and Huntington's diseases.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 25, 1997
    Assignee: Warner-Lambert Company
    Inventor: Sham Nikam
  • N-pyridinyl[1,2,4]triazolo[1,5-c]pyrimidine-2-sulfonamide herbicides
    Patent number: 5614469
    Abstract: Substituted N-pyridinyl[1,2,4]triazolo[1,5-c]-pyrimidine-2-sulfonamide compounds, such as N-(2-fluoro-4-methyl)-7-fluoro-5-methoxy[1,2,4]triazolo[1,5-c]pyrimidine-2 -sulfonamide, were prepared bycondensation of a 2-chlorosulfonyl[1,2,4]triazolo[1,5-c]pyrimidine compound, such as 2-chlorosulfonyl-7-fluoro-5-methoxy[1,2,4]triazolo[1,5-c]pyrimidine, with a substituted 3-aminopyridine compound, such as 3-amino-2-fluoro-4-methylpyridine, and found to possess herbicidal utility.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 25, 1997
    Assignee: DowElanco
    Inventors: Kim E. Arndt, William A. Kleschick, Walter Reifschneider, Beth A. Swisher, Robert J. Ehr, John J. Jachetta, John C. Van Heertum
  • Piperazine derivatives as 5-HT.sub.1 Agonists
    Patent number: 5614524
    Abstract: A class of substituted piperazine derivatives of formula I ##STR1## are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated conditions, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: March 25, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: V. G. Matassa, L. J. Street, A. J. Reeve
  • Triazoloquinazolines for the treatment of central nervous disorders
    Patent number: 5612344
    Abstract: The use of triazoloquinazolines for the production of drugs for controlling central nervous disorders is described. The triazoloquinazolines have the formula ##STR1## where R.sup.1, R.sup.2 and X have the meanings stated in the description.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: March 18, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Rainer Schlecker, Hans-J org Treiber, Berthold Behl, Hans P. Hofmann
  • Process for preparing 5-substituted pyrrolo-[2,3-d]pyrimidines
    Patent number: 5612482
    Abstract: Processes for preparing 5-substituted pyrrolo[2,3-d]pyrimidines which are useful as intermediates for the preparation of pyrrolo[2,3-d]pyrimidine antineoplastic agents or as antineoplastic agents themselves are provided.
    Type: Grant
    Filed: January 31, 1996
    Date of Patent: March 18, 1997
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Risperidone pamoate
    Patent number: 5612346
    Abstract: A compound which is a pamoate acid addition salt of risperidone, compositions comprising the same and processes for preparing said compound and compositions.
    Type: Grant
    Filed: September 22, 1995
    Date of Patent: March 18, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean L. Mesens, Jozef Peeters
  • Process for the regioselective n-alkylation of quinazolinones
    Patent number: 5610301
    Abstract: A process for the regioselective N-alkylation of 2-alkyl-5,6,7 or 8-substituted-4(3H)-quinazolinones in the presence of lithium salts.
    Type: Grant
    Filed: July 1, 1993
    Date of Patent: March 11, 1997
    Assignee: American Cyanamid Company
    Inventors: Arthur G. Mohan, Joseph D'Antuono, III
  • 1,4-disubstituted piperazines useful in the therapy of the asthma and of the inflammation of the respiratory tract
    Patent number: 5607930
    Abstract: Compounds of formula (I): ##STR1## wherein Ra, Rb, B and D have the meanings reported in the disclosure, processes for making the same, and methods of using the same in the treatment of asthma and/or inflammation of the respiratory tract are disclosed.
    Type: Grant
    Filed: March 28, 1995
    Date of Patent: March 4, 1997
    Assignee: Boehringer Mannheim Italia, S.p.A.
    Inventors: Giorgio Long, Silvano Spinelli, Antonella Rozzi, Simonetta D'Alo', Licia Gallico