Patents Represented by Attorney Richard D. Foggio
  • Patent number: 4623535
    Abstract: The compounds represented by the following structural formula (I) ##STR1## wherein m and n are independently 1, 2 or 3; R.sub.1 is an C.sub.8 to C.sub.13 alkyl radical and pharmaceutically acceptable salts thereof have been found to be leukotriene antagonists and useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.
    Type: Grant
    Filed: January 19, 1984
    Date of Patent: November 18, 1986
    Assignee: SmithKline Beckman Corporation
    Inventor: Carl D. Perchonock
  • Patent number: 4620001
    Abstract: A series of chemical reactions starting from the condensation of uracil with an acid stable heterocyclic aldehyde in an acid medium produces biologically active end products which are 2-heterocyclylmethylthioethylamino-5-heterocyclylmethyl-4-pyrimidinones. The new reactions and intermediates of this invention are particularly useful for preparing 2[2-(5-dimethylaminomethyl-2-furylmethylthio)-ethylamino]-5-(6-methyl-3-py ridylmethyl)-4-pyrimidinone and its salts. This compound is a potent H.sub.2 -antagonist with a long duration of activity.
    Type: Grant
    Filed: September 11, 1984
    Date of Patent: October 28, 1986
    Assignee: SmithKline Beckman Corporation
    Inventors: Bing L. Lam, Lendon N. Pridgen
  • Patent number: 4588740
    Abstract: A series of pharmaceutical compositions which contain 4-aminoalkyl-2(3H)-indolones has been demonstrated to have D.sub.2 -agonist activity useful for treating congestive heart failure and hypertension. A representative ingredient of the compositions is 4-di-n-propylaminoethyl-2(3H)-indolone or a salt thereof.
    Type: Grant
    Filed: April 5, 1984
    Date of Patent: May 13, 1986
    Assignee: SmithKline Beckman Corporation
    Inventor: Gregory Gallagher, Jr.
  • Patent number: 4584381
    Abstract: Compounds of the formula: ##STR1## where R.sup.1 is halogen or nitro; R.sup.2 is C.sub.1-4 alkyl; and R.sup.3 is a C.sub.1-3 alkylene group are intermediates to 2-(3,5-disubstituted pyridyl-alkyl amino)-5-pyridylmethyl-4-pyrimidone derivatives which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: September 17, 1984
    Date of Patent: April 22, 1986
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • Patent number: 4584384
    Abstract: 3-Nitro-2-substituted aminopyrroles are histamine H.sub.2 -receptor antagonists. The 2-position substituent is a fully-unsaturated heterocyclyl alkyl group preferably with alkyl group interrupted by sulfur or oxygen. The 4- and 5-positions of the pyrrole ring can also be substituted.
    Type: Grant
    Filed: August 6, 1984
    Date of Patent: April 22, 1986
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Patent number: 4579972
    Abstract: New intermediates and processes for preparing 6-halo-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi nes involve the reaction of a p-methoxyphenylglyoxal, lower alkyl hemimercaptal with a 2-chloro-3,4-dimethoxyphenethylamine, followed by a borohydride reduction.
    Type: Grant
    Filed: June 28, 1985
    Date of Patent: April 1, 1986
    Assignee: SmithKline Beckman Corporation
    Inventors: Kathleen L. Wert, Alan W. Tremper
  • Patent number: 4578459
    Abstract: Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: March 25, 1986
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Patent number: 4578388
    Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino). N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido) groups. Two compounds of the invention are 1,3-bis-[N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)guanidino]propane and 1,3-bis-[S-(N-2-(5-methyl-4-imidazolylmethylthio)ethyl)isothioureido]p ropane. The compounds of this invention are inhibitors of H-2 histamine receptors.
    Type: Grant
    Filed: June 30, 1983
    Date of Patent: March 25, 1986
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • Patent number: 4576937
    Abstract: A new cephalosporin compound, 7-D-mandelamido-3-(1-sulfomethyltetrazol-5-yl) thiomethyl-3-cephem-4-carbo xylic acid monosodium salt, having unique antibacterial activity and advantageously high stability, is disclosed. Pharmaceutical compositions comprising the new cephalosporin monosodium salt are also disclosed.
    Type: Grant
    Filed: February 29, 1984
    Date of Patent: March 18, 1986
    Assignee: SmithKline Beckman Corporation
    Inventor: Theodore J. Polansky
  • Patent number: 4574126
    Abstract: This invention relates to 2-pyridine derivatives substituted in the 4-position with a dialkylamino- or piperidinyl- or pyrrolidinylalkyl group. The compounds have histamine H.sub.2 -antagonist activity.
    Type: Grant
    Filed: March 9, 1983
    Date of Patent: March 4, 1986
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: David G. Cooper, George S. Sach
  • Patent number: 4571398
    Abstract: This invention relates to cytosine derivatives which have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 4-[3-(3-(piperidinomethyl)phenoxy)propylamino]-pyrimidin-2-thione.
    Type: Grant
    Filed: June 20, 1984
    Date of Patent: February 18, 1986
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Thomas H. Brown
  • Patent number: 4569996
    Abstract: This invention provides a process for the preparation of pyrimidinone compounds with a group R.sup.2 CH(OH)-- at the 5-position thereof, wherein R.sup.2 is an optionally substituted acid-stable 5- or 6-membered nitrogen-containing heteroaryl group. The pyrimidinone ring is further substituted by a side-chain of a H.sub.1 -antagonist or H.sub.2 -antagonist or a precursor thereof.The compounds are convertible to 5-heteroaryl methyl compounds which are either useful H.sub.1 - or H.sub.2 -antagonists or precursors thereof.
    Type: Grant
    Filed: July 27, 1983
    Date of Patent: February 11, 1986
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: John Kitteringham, Brian P. Slingsby
  • Patent number: 4567176
    Abstract: This invention relates to Mannich-furyl(thienyl, pyridyl or phenyl) alkylaminoimidazolinones which have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 2-[2-(5-dimethylaminomethylfuran-2-ylmethylthio)-ethylamino]-1-methyl-imid azolin-4-one.
    Type: Grant
    Filed: April 18, 1984
    Date of Patent: January 28, 1986
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Thomas H. Brown
  • Patent number: 4564363
    Abstract: A device for effecting the delayed release of an active ingredient comprises a container and, within, a dispersible unit of ingredient, a removable closure and a electrical control circuit for removal of said closure at a designated time to release the active ingredient. Several assemblies are combined to control the administration of veterinary medicaments to ruminant animals as a specific application of the invention.
    Type: Grant
    Filed: July 13, 1983
    Date of Patent: January 14, 1986
    Assignee: SmithKline Beckman Corporation
    Inventors: Brian G. Bagnall, Robert J. Gyurik
  • Patent number: 4558128
    Abstract: The compounds are isoureas and isothioureas which have an O- or S- alkylpyrimidone substituent and which are histamine H.sub.2 -antagonists and antiinflammatory agents. A specific compound of this invention is 2-[5-(O-isoureido)pentylamino]-5-(6-methyl-3-pyridylmethyl)-4-pyrimidone.
    Type: Grant
    Filed: November 9, 1983
    Date of Patent: December 10, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Charon R. Ganellin, Robert J. Ife, David A. A. Owen
  • Patent number: 4554284
    Abstract: Certain aminoethyl substituted 1,3-benzthiazol- and 1,3-benzoxazol-2(3H)-ones are D.sub.2 -dopamine agonists. These compounds are prepared by reacting an appropriate o-aminophenol or thiophenol with phosgene.
    Type: Grant
    Filed: September 12, 1984
    Date of Patent: November 19, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: Orum D. Stringer, Joseph Weinstock
  • Patent number: 4554287
    Abstract: 7-[2-Dialkylamino)ethyl]-4-hydroxy-1,3-benzimidazol-2-ones are prepared by oxidative cyclization of a urea, followed by removal of protective groups. The compounds are D.sub.2 -agonists and, thereby, have anti-hypertensive activity. A species of the group is 7[2-N,N-di-n-propylamino)ethyl]-4-hydroxyl-1,3-benzimidazol-2-one.
    Type: Grant
    Filed: September 12, 1984
    Date of Patent: November 19, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: Orum D. Stringer, Joseph Weinstock
  • Patent number: 4552893
    Abstract: The compounds represented by the formula (I) ##STR1## wherein m is 0, 1 or 2; p is 9, 10, 11, 12 or 13; R.sub.1 is hydrogen, amino or ##STR2## R.sub.2 is hydroxyl, amino, --NHCH.sub.2 CO.sub.2 H, ##STR3## or --NHCH.sub.2 CONH.sub.2 ; and X is --CO.sub.2 H, --CH.sub.2 OH or ##STR4## with the proviso that when m is 0, R.sub.1 is hydrogen, or a pharmaceutically acceptable salt thereof have been found to be leukotriene antagonists and useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.
    Type: Grant
    Filed: March 7, 1983
    Date of Patent: November 12, 1985
    Assignee: SmithKline Beckman Corporation
    Inventors: John G. Gleason, Ralph F. Hall, Thomas W. Ku
  • Patent number: 4551466
    Abstract: This invention relates to diaminotriazole derivatives in which one amino group is substituted by a 4-dialkylamino- or piperidinyl- or pyrolidinylmethyl pyrid-2-yloxypropyl group. The compounds have histamine H.sub.2 -antagonist activity. One specific compound is 1-methyl-N.sup.5 -3-(4-[1-piperidinomethyl]-pyridyl-2-oxy)-propyl-1H-1,2,4-triazole-3,5-dia mine.
    Type: Grant
    Filed: March 9, 1983
    Date of Patent: November 5, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: David G. Cooper, George S. Sach
  • Patent number: 4548940
    Abstract: Pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: December 20, 1983
    Date of Patent: October 22, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Robert J. Ife