Patents Represented by Attorney Roger A. Williams
  • Patent number: 5310951
    Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;R.sup.1 is alkyl;R.sup.2 is hydrogen, alkyl;R.sup.6 is alkyl;n is 1 to 5;p is 0 to 6;x is 0 or 2; andR.sup.4 and R.sup.5 are independently hydrogen or alkyl or together with N form a cycloalkylamine.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in treating disease conditions mediated by LTB.sub.4.
    Type: Grant
    Filed: December 23, 1992
    Date of Patent: May 10, 1994
    Assignee: G.D. Searle & Co.
    Inventors: Stevan W. Djuric, Stephen H. Docter, Stella S. Yu
  • Patent number: 5310060
    Abstract: The present invention concerns a novel tamper-evident, child-resistant blister package for medicaments and nonmedicaments which is user-friendly, but which is difficult to open by young children and impaired adults.Because the blister package has pull tabs which are designed to be pulled away from, rather than towards, article-receiving pockets which may be present in the blister package other than the article-receiving pocket being accessed, a young child or user of the blister package can only access one article-receiving pocket at a time, whether deliberately or inadvertently.The blister package of the invention is an attractive and inexpensive package for the merchandising of pharmaceutical and other products which is constructed in a manner which facilitates mass production.
    Type: Grant
    Filed: October 13, 1992
    Date of Patent: May 10, 1994
    Assignee: G. D. Searle & Co.
    Inventors: John M. Bitner, Craig T. Vanderburg, Curtis E. Hart
  • Patent number: 5304644
    Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: April 15, 1992
    Date of Patent: April 19, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Robert K. Husa, Michael F. Rafferty, Timothy J. Hagen, E. Ann Hallinan
  • Patent number: 5302601
    Abstract: The present invention relates to a class of compounds represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof useful in the treatment of diseases or disorders mediated by platelet activating factor (PAF).
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: April 12, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Ish K. Khannal, Roger Nosal, Richard M. Weier, Kirk T. Lentz
  • Patent number: 5300512
    Abstract: This invention relates to compounds useful in treating 5-HT.sub.4 and/or 5-HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkoxy, halogen, amino, monoalkylamino, dialkylamino, acylamino and alkylsulfonylamino; R.sub.3 is selected from the group consisting of H, alkyl and cycloalkyl; X is NH or O; and Z is selected from the group consisting of ##STR2## pharmaceutical compositions including the compounds and a method for treating serotonin mediated conditions with the compositions which act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: April 5, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Alan E. Moormann
  • Patent number: 5298514
    Abstract: The present invention relates to phenolic thioetheramides of the formula ##STR1## wherein R.sup.1 and R.sup.2 are tert-alkyl or phenyl, Alk.sup.1 and Alk.sup.2 are alkylene; X is sulfur or oxygen, m is 0, 1, or 2; and R is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen or alkyl and Alk.sup.3 is alkylene.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: March 29, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5290561
    Abstract: A patch for the transdermal delivery of pharmaceutical drugs. The patch is characterized by having a single mass of elastomer in which the active drug and a percutaneous absorption enhancer are homogeneously dispersed throughout. The patch is especially well suited to delivering the beta.sub.2 adrenergic agonist drug albuterol.
    Type: Grant
    Filed: April 10, 1992
    Date of Patent: March 1, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Bahram Farhadieh, Rajeev D. Gokhale
  • Patent number: 5288719
    Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a 2-, 3-, 8- and/or 10-substituted dibenzoxazepine compound having a structure of the formula: ##STR1## or a pharmaceutically-acceptable salt thereof, wherein: X is --NH-- or --CH.sub.2 --;Y is(1) --CH.sub.2 -- when X is --NH--, and(2) --NH-- when X is --CH.sub.2 --;R.sup.1 is hydrogen, halogen or --OR.sup.4 ;R.sup.4 is hydrogen, alkyl or ##STR2## Z is oxygen, sulfur, --SO--, --SO.sub.2 -- or --NR.sup.5 --; R.sup.5 is hydrogen or t-butyloxycarbonyl;R.sup.2 is hydrogen, halogen or trifluoromethyl;R.sup.3 is hydrogen, halogen, aryl, heteroaryl in which the heteroatoms are selected from oxygen, nitrogen and/or sulfur, or --NR.sup.6 R.sup.7 ;R.sup.6 and R.sup.7 are each independently hydrogen or alkyl;R.sup.8 is alkyl, aryl or ##STR3## R.sup.9 and R.sup.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: February 22, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Robert K. Husa, Timothy J. Hagen, E. A. Hallinan
  • Patent number: 5283240
    Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a compound of Formula I: ##STR1##
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: February 1, 1994
    Assignee: G. D. Searle & Co.
    Inventors: E. Ann Hallinan, Robert K. Husa, Karen B. Peterson
  • Patent number: 5281590
    Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a compound of Formula I: ##STR1##
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: January 25, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Robert K. Husa, E. Ann Hallinan, Marc Herin, Michel Lesne
  • Patent number: 5281724
    Abstract: A process for the preparation of 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose and 6-(n-substituted amino)-6-deoxy-1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose and derivatives of the formula: ##STR1## wherein R' is benzyl or R, wherein R is hydrogen, alkyl of 1 to 13 carbon atoms, and aralkyl wherein alkyl is a lower alkyl of 2 to 6 carbon atoms and aryl is phenyl, unsubstituted or substituted with lower alkyl of 1 to 6 carbon atoms, halo, lower alkoxy of 1 to 4 carbon atoms or thio lower alkyl of 1 to 4 carbon atoms by the steps of: treating L-sorbose with 2,2-dimethoxy propane to yield 1,2:4,6-di-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; treating the compound with sulfuric acid in a solvent to produce 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; and consecutively treating with sulfonyl chloride and with an amine to yield 6-(substituted amino)-6-deoxy- 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose.
    Type: Grant
    Filed: June 25, 1991
    Date of Patent: January 25, 1994
    Assignee: G. D. Searle & Co.
    Inventors: James R. Behling, Payman Farid, Ish Khanna, John R. Medich, Mike Prunier, Mike G. Scaros, Richard M. Weier
  • Patent number: 5280028
    Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkoxy, halogen, amino, monoalkylamino, dialkylamino, acylamino and alkylsulfonylamino; R.sub.3 is selected from the group consisting of H, alkyl and cycloalkyl; X is NH or O; Z is selected from the group consisting of ##STR2## n and r are independently 1 or 2; p is 0 or 1; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositions which act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: January 18, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Alan E. Moormann
  • Patent number: 5280047
    Abstract: The present invention relates to methods of using and pharmaceutical compositions containing compounds of Formula I: ##STR1## wherein R.sup.1 is hydrogen, --COR.sup.4 wherein R.sup.4 is C.sub.1 -C.sub.4 alkyl, or --COOR.sup.5 wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl; R.sup.2 is C.sub.1 -C.sub.4 alkyl, phenyl, or --OR.sup.6 wherein R.sup.6 is C.sub.1 -C.sub.4 alkyl; and R.sup.3 is C.sub.6 -C.sub.8 alkyl, halogen, or NO.sub.2 ; with the proviso that when R.sup.1 is hydrogen, R.sup.2 is C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable carrier. Compounds of Formula I and pharmaceutical compositions containing them are inhibitors of 5-lipoxygenase and are useful in the treatment of conditions mediated by leukotrienes such as inflammation, allergy, hypersensitivity reactions, and proliferative skin diseases such as psoriasis.
    Type: Grant
    Filed: April 2, 1993
    Date of Patent: January 18, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5280029
    Abstract: The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: January 18, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Clara I. Villamil
  • Patent number: 5276155
    Abstract: A process for the resolution of (.+-.)-.alpha.-[2-[acetyl(1-methylethyl)amino]ethyl-.alpha.-(2-chloropheny l)-1-piperidinebutanamide having the following structure ##STR1## into its (+) and (-) enantiomers using camphorsulfonic acid.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: January 4, 1994
    Assignee: G. D. Searle & Co.
    Inventors: John R. Medich, Gatis Plume
  • Patent number: 5272175
    Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: December 21, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
  • Patent number: 5272178
    Abstract: The present invention relates to compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, phenyl, or hydrogen; R.sup.3 represents hydrogen or alkyl; X represents O, S or (CH.sub.2).sub.m wherein m is 1 or 2; A represents O or S(O).sub.n wherein n is 0, 1, or 2; p is an integer from 0 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl; or NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl, and R.sup.6 is hydrogen, alkyl, heterocyclealkyl, substituted heterocyclealkyl, cycloalkyl, substituted cycloalkyl, phenyl, substituted phenyl, phenylalkyl, or substituted phenylalkyl, or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl; and the pharmaceutically acceptable salts thereof. The compounds are inhibitors or stimulators of superoxide generation.
    Type: Grant
    Filed: April 8, 1993
    Date of Patent: December 21, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5272162
    Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions including the compounds and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: December 21, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Foe S. Tjoeng, Jeffery A. Zablocki
  • Patent number: 5264457
    Abstract: This invention relates to compounds having the following formula ##STR1## which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine sulfones derivatives.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: November 23, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Steven P. Adams, Joseph G. Rico, Masateru Miyano
  • Patent number: 5260303
    Abstract: The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
    Type: Grant
    Filed: March 7, 1991
    Date of Patent: November 9, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil