Patents Examined by Matthew V. Grumbling
  • Tricyclic derivatives
    Patent number: 5569658
    Abstract: The invention concerns tricyclic derivatives of the formula I ##STR1## wherein R.sup.1 and R.sup.2 together form an optionally substituted group of the formula --N.dbd.CH--NH--, --N.dbd.CH--O--, --N.dbd.CH--S--, --N.dbd.N--NH--, --NH--N.dbd.CH--, --NH--CH.dbd.CH--. --NH--CO--NH--, --NH--CO--O--, --NH--CO--S--, --NH--NH--CO--, --N.dbd.CH--CH.dbd.N--, --N.dbd.N--CH.dbd.CH--, --N.dbd.CH--N.dbd.CH--, --N.dbd.CH--CH.dbd.N--, --NH--CO--CH.dbd.CH-- or --N.dbd.CH--CO--NH--; m is 1, 2 or 3 and R.sup.3 includes hydrogen, halogeno 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: July 19, 1994
    Date of Patent: October 29, 1996
    Assignee: Zeneca Limited
    Inventor: Andrew J. Barker
  • Therapeutic heterocycles which antagonize neurokinin receptors
    Patent number: 5567700
    Abstract: Compounds of formula I ##STR1## wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: August 15, 1994
    Date of Patent: October 22, 1996
    Assignee: Zeneca Limited
    Inventor: Scott C. Miller
  • Bradykinin antagonist quinolines
    Patent number: 5563162
    Abstract: This invention relates to new heterocyclic compounds and pharmaceutically acceptable salts thereof. More particularly, this invention relates to new heterocyclic compounds and salts thereof which display bradykinin antagonist activity, to processes for preparing these compounds, to a pharmaceutical composition comprising these compounds, and to methods of using same in the prevention and/or the treatment of bradykinin- or bradykinin analogue-mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like, in human beings or in animals.
    Type: Grant
    Filed: April 26, 1994
    Date of Patent: October 8, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
  • Thymidylate synthase inhibiting quinazolinones
    Patent number: 5561133
    Abstract: Quinazolines of the formula ##STR1## wherein R.sup.1 is typically methyl, hydrogen or amino; R.sup.2 is typically methyl or propargyl; Ar is typically phenylene or 2'-fluorophenylene; R.sup.3 is the residue of a dipeptide substituted, typically by methyl, at position (a), (b) or (c), shown in the following partial formula: ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.8 are typically hydrogen, R.sup.7 is typically hydrogen or methyl; or a pharmaceutically acceptable salt, ester or amide thereof are of value in the treatment of cancer.
    Type: Grant
    Filed: August 9, 1994
    Date of Patent: October 1, 1996
    Assignee: British Technology Group Limited
    Inventors: Graham M. F. Bisset, Vassilios Bavetsias
  • Quinazolinone derivatives possessing calcium uptake inhibiting activity
    Patent number: 5556860
    Abstract: This invention is to provide quinazolinone derivatives, and their acid salts and quaternary ammonium salts, having an effect of preventing or treating diseases caused by calcium ion overload in cells, such as ischemic heart disease, ischemic cerebral disease and ischemic renal disease, and their usage. The quinazolinone derivatives are represented by the formula: ##STR1## typically, T represents an oxygen atom; Y represents a phenyl or cyclohexyl group; R.sup.1 represents a hydrogen or chlorine atom; R.sup.
    Type: Grant
    Filed: May 26, 1994
    Date of Patent: September 17, 1996
    Assignee: Sumitomo Pharmaceuticals Co., Ltd.
    Inventors: Masami Muraoka, Kazuki Matsui, Hirohiko Hasegawa, Atsuyuki Kojima
  • Thiazine or thiomorpholine derivatives
    Patent number: 5556841
    Abstract: This invention relates to the compounds of the formula [I] which are useful for the treatment of cataracts, and the synthetic intermediates of the formula [II], ##STR1## wherein R.sup.1 is hydroxy which can be protected by a hydroxy protective group;R.sup.2 is lower alkyl;R.sup.3 is hydrogen, lower alkyl, hydroxy, which can be protected by a hydroxy protective group, or lower alkoxy, and the said lower alkyl can be substituted by hydroxy, which can be protected by a hydroxy protective group, amino or lower alkylamino;R.sup.4 is carboxy which can be converted into ester or amide; tetrazolyl; phosphono which can be converted into ester or amide; or sulfonyl which can be converted into ester or amide;R.sup.5 is cyano or lower alkoxy;A is alkylene;B is C.dbd.O, C.dbd.S or CH.sub.2, andis single bond or double bond.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: September 17, 1996
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Yoichi Kawashima, Atsutoshi Ota, Hiroyuki Mibu
  • Dihydropyridazinones, pyridazinones and related compounds as fungicides
    Patent number: 5552409
    Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.
    Type: Grant
    Filed: March 31, 1994
    Date of Patent: September 3, 1996
    Assignee: Rohm and Haas Company
    Inventors: Enrique L. Michelotti, Anne R. Egan, Ronald Ross, Jr., Willie J. Wilson
  • Piperazinyl-bis(alkylamino)pyrimidine derivatives and process for preparing same
    Patent number: 5550240
    Abstract: An intermediate compound is disclosed that is useful in the preparation of a lipid-peroxidation inhibiting substance and that is selected from the group consisting of:2,4-bis[1-adamantylamino]-6-(1-piperazinyl)pyrimidine; and4,6-bis(1-adamantylamino)-2-(1-piperazinyl)pyrimidine;or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: August 27, 1996
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: S andor Mah o, Zolt an Tuba, Csaba S anta, G abor Balogh, Eva Czajlikn e Csiz er, M aria Lovasn e Marsai, Gy orgy G alik
  • Process for large-scale production of indolyl alkyl pyrimidinyl piperazine compounds
    Patent number: 5550239
    Abstract: An improved, novel convergent process suitable for large scale preparation of the antimigraine agent 4-(5-methoxy-4-pyrimidinyl)-1-[3-[5-[[(methylamino)sulfonyl]methyl]-1H-ind ol-3-yl]propyl]piperazine (BMS 180048) and close analogs. The improved process provides efficiencies in handling, purification, and product yield and involves a novel heteroannulation reaction that provides the indole ring moiety and propylpiperazinyl-pyrimidine backbone in a single step.
    Type: Grant
    Filed: November 8, 1994
    Date of Patent: August 27, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael J. Humora, Sandeep P. Modi, Sushi K. Srivastava, Andrew D. Williams
  • Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidines and 1,1-dioxo-2H-1,2-benzothiazinoylguanidines, a process for their preparation, their use as medicaments or diagnostic agents, and medicaments containing them
    Patent number: 5547953
    Abstract: Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidines and 1,1-dioxo-2H-1,2-benzothiazinoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and also a medicament containing them. Acylguanidines I ##STR1## with X equal to carbonyl or sulfonyl; R(1) equal to H, (cyclo)alkyl, phenyl; R(2) equal to H, alkyl, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine. The compounds have no unwanted salidiuretic but very good antiarrhythmic properties. They are able, as a consequence of inhibition of the cellular Na.sup.+ /H.sup.+ exchange mechanism, to be used for the treatment of all acute or chronic ischemia-induced damage.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: August 20, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
  • Alfuzosin hydrochloride dihydrate
    Patent number: 5545738
    Abstract: Alfuzosin hydrochloride is stabilized as alfuzosin hydrochloride dihydrate, which is useful for the production of antihypertensive agents or dysuria curing agents.
    Type: Grant
    Filed: December 27, 1994
    Date of Patent: August 13, 1996
    Assignee: Synthelabo
    Inventors: Regis Borrega, Satoshi Kitamura
  • Irreversible inhibitors of adenosine receptors
    Patent number: 5545627
    Abstract: Irreversible ligands for adenosine receptors are derived from agonist and antagonist functionalized congeners which contain electrophilic acylating and alkylating groups for reaction at nucleophilic residues of adenosine receptors. The ligands are based on 8-aryl-substituted xanthines as antagonists and on N.sup.6 -substituted adenosine as agonists.
    Type: Grant
    Filed: March 28, 1994
    Date of Patent: August 13, 1996
    Assignees: The United States of America as represented by the Department of Health and Human Services, Duke University
    Inventors: Kenneth A. Jacobson, Gary Stiles
  • Substituted bicyclic phosphoramides and derivatives thereof
    Patent number: 5543517
    Abstract: This invention relates to substituted bicyclic phosphoramides and derivatives thereof, useful as retroviral protease inhibitors and as standards and reagents in determining the ability of a potential pharmaceutical to inhibit viral replication or HIV protease, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection.
    Type: Grant
    Filed: January 13, 1994
    Date of Patent: August 6, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Joanne M. Smallheer
  • Process for preparation of benzoxazine compounds in solventless systems
    Patent number: 5543516
    Abstract: A method for preparing a desired benzoxazine compound comprises preparing a substantially homogeneous reaction mixture that includes a phenolic compound; a primary amine; and an aldehyde, but no solvent other than for the solvency which the reactants may have for each other. Following its preparation, the reaction mixture is maintained at a temperature, and for a period sufficient to cause the reactants to combine chemically to form the desired compound.
    Type: Grant
    Filed: May 18, 1994
    Date of Patent: August 6, 1996
    Assignee: Edison Polymer Innovation Corporation
    Inventor: Hatsuo Ishida
  • Indolinyl N-hydroxyurea and N-hydroxamic acid derivatives as lipoxygenase inhibitors
    Patent number: 5541218
    Abstract: Certain indoline derivatives of the formula I: ##STR1## wherein the variables Y, A, R.sub.1, R.sub.4 and n have the definitions set forth in the disclosure, have the ability to inhibit the 5-lipoxygenase enzyme. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergic conditions and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: July 30, 1996
    Assignee: Pfizer Inc.
    Inventors: Takafumi Ikeda, Rodney W. Stevens
  • Geneserine derivatives processes as cholinesterase inhibitors
    Patent number: 5538968
    Abstract: Geneserine homologs of formula I ##STR1## in which R is a straight or branched C.sub.2 -C.sub.20 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, an unsubstituted phenyl or benzyl group, or a phenyl or benzyl group substituted by a C.sub.1 -C.sub.4 alkyl group, a halogen atom or a C.sub.1 -C.sub.4 alkoxy group, or a salt with an organic or inorganic non-toxic acid, exhibit anticholinesterase activity and may be useful in the treatment of Alzheimer disease and other conditions due to a neurological deficiency.
    Type: Grant
    Filed: March 3, 1994
    Date of Patent: July 23, 1996
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Paolo Chiesi, Maurizio Del Canale, Vittorino Servadio, Eleonora Ghidini
  • 3-Substituted-7-[3-(imidazol-1-yl)phenyl]-pyrazolo[1,5-a]pyrimidines
    Patent number: 5538977
    Abstract: Disclosed are 3-substituted-7-[3-(imidazol-1-yl)phenyl]-pyrazolo[1,5-a]pyrimidines of the formula: ##STR1## wherein R.sup.1, R.sup.3 and R.sup.4 are defined in the specification which compounds have anxiolytic, anti-convulsant, sedative-hypnotic and skeletal muscle relaxant activity.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: July 23, 1996
    Assignee: American Cyanamid Company
    Inventors: John P. Dusza, Jay D. Albright, Andrew S. Tomcufcik
  • Process for the preparation of substituted quinazoline-2,4,-diones
    Patent number: 5539114
    Abstract: A process for the preparation of quinazoline-2,4-diones of the formula (I) ##STR1## in which R.sup.1 is aryl and R.sub.2, R.sup.3, R.sup.4, and R.sup.5 independently of one another are halogen, alkyl, alkoxy or hydrogen, by reacting anthranilic acid esters of the formula (II) ##STR2## in an aprotic reaction medium with aryl isocyanates R.sup.1 --N.dbd.C.dbd.O to give N-arylcarbamoyl-anthranilic acid esters of the formula (III) ##STR3## and cyclizing these in the presence of a base selected from the group of alkali metal or alkaline earth metal alkoxides, amides, hydrides or tetraalkylammonium hydroxides.
    Type: Grant
    Filed: November 15, 1994
    Date of Patent: July 23, 1996
    Assignee: Hoechst AG
    Inventors: Robert Cosmo, Wolfgang Tronich
  • Carbonic anhydrase inhibitors
    Patent number: 5538966
    Abstract: Compounds of the following formula are disclosed:Compounds of Formula I are the topic of this invention: ##STR1## Wherein G, J and the two atoms of the thiophene ring to which they are attached form a six-membered ring chosen from ##STR2## The compounds are useful as carbonic anhydrase inhibitors.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: July 23, 1996
    Assignee: Alcon Laboratories, Inc.
    Inventors: Jesse A. May, Hwang-Hsing Chen, Brian DuPr e, Thomas R. Dean
  • Endothelin antagonists and their preparation
    Patent number: 5538950
    Abstract: A compound of the formula: ##STR1## in which R.sup.3 is hydrogen or lower alkyl, R.sup.4 is pyridyl (lower) alkyl; andR.sup.1, R.sup.2, R.sup.5 and A are defined in the description;or a pharmaceutically acceptable salt thereof, which have endothelin antagonistic activity.
    Type: Grant
    Filed: May 12, 1994
    Date of Patent: July 23, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Keiji Hemmi, Masahiro Neya, Naoki Fukami, Masashi Hashimoto, Hirokazu Tanaka, Natsuko Kayakiri