Patents Represented by Attorney, Agent or Law Firm Lawrence T. Welch
  • Patent number: 4329459
    Abstract: The present invention provides novel 8-heteroaryltetrahydrobenzopyrans and analogs thereof. These novel compounds are useful as inhibitors of endoperoxide cyclooxygenase which prevents the conversion of unsaturated fatty acids to endoperoxides. Because of this pharmacological activity, these compounds represent potent platelet aggregation inhibitors.
    Type: Grant
    Filed: May 5, 1980
    Date of Patent: May 11, 1982
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4324905
    Abstract: Phenacyl-type esters of PGF.sub.2.alpha., 15(S)-15-methyl-PGF.sub.2.alpha., and 15(R)-15-methyl-PGF.sub.2.alpha. are disclosed, represented by the formula ##STR1## wherein M is ##STR2## wherein R.sub.1 is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl; and wherein R.sub.2 is hydrogen or benzoyl. The products are useful for the same pharmacological and medical purposes as the corresponding prostaglandin and analogs, and are also useful as a means for obtaining highly purified products.
    Type: Grant
    Filed: August 14, 1974
    Date of Patent: April 13, 1982
    Assignee: The Upjohn Company
    Inventor: Walter Morozowich
  • Patent number: 4313881
    Abstract: The present invention provides novel 5-hydroxyfurochromones, which are useful as antiatherosclerotic agents.
    Type: Grant
    Filed: October 29, 1980
    Date of Patent: February 2, 1982
    Assignee: The Upjohn Company
    Inventor: Ronald B. Gammill
  • Patent number: 4313883
    Abstract: The present invention provides novel halofurochromones, which are useful as antiatherosclerotic agents.
    Type: Grant
    Filed: October 29, 1980
    Date of Patent: February 2, 1982
    Assignee: The Upjohn Company
    Inventor: Ronald B. Gammill
  • Patent number: 4313882
    Abstract: The present invention provides novel 7-methyl-6-methylthiomethylsulfinyl-, and methylsulfonylmethylfurochromones, which are useful as antiatherosclerotic agents.
    Type: Grant
    Filed: October 29, 1980
    Date of Patent: February 2, 1982
    Assignee: The Upjohn Company
    Inventor: Ronald B. Gammill
  • Patent number: 4304926
    Abstract: Phenacyl-type esters of PGE.sub.2, PGE.sub.1, and 13,14-dihydro-PGE.sub.1 and their 15-methyl, 16,16-dimethyl, and 17-phenyl analogs, including the respective 15(R)epimers, are disclosed, represented by the formula ##STR1## wherein M is ##STR2## wherein R.sub.3 is hydrogen or methyl; wherein Q is ##STR3## wherein each of R.sub.4 and R.sub.5 is hydrogen or methyl, being the same or different, or ##STR4## wherein the moiety--C.sub.t H.sub.2t -- represents a valence bond or alkylene of one to 10 carbon atoms, inclusive, with one to 7 carbon atoms, inclusive, between ##STR5## and the phenyl ring; wherein R.sub.1 is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl; wherein R.sub.2 is hydrogen or benzoyl; and wherein (a) X is --CH.sub.2 CH.sub.2 -- or trans--CH.dbd.CH-- and Y is --CH.sub.2 CH.sub.2 --, or (b) X is trans--CH.dbd.CH-- and Y is cis--CH.dbd.CH--.
    Type: Grant
    Filed: August 14, 1974
    Date of Patent: December 8, 1981
    Assignee: The Upjohn Company
    Inventor: Walter Morozowich
  • Patent number: 4301078
    Abstract: This invention relates to certain structural and pharmacological analogs of prostacyclin (PGI.sub.2) wherein the C-5 to C-6 double bond is isomerized to the C-4 to C-5 position. These novel trans-4,5-didehydro-5,6-dihydro prostacyclin-type compounds are useful as smooth muscle stimulators.
    Type: Grant
    Filed: August 3, 1977
    Date of Patent: November 17, 1981
    Assignee: The Upjohn Company
    Inventor: Herman W. Smith
  • Patent number: 4301175
    Abstract: PGE-type compounds are stabilized in a composition comprising a mixture of triacetin and ethanol. This composition surprisingly and unexpectedly retains virtually all of the stability of triacetin compounds and additionally provides the superior water miscibility of ethanol.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: November 17, 1981
    Assignee: The Upjohn Company
    Inventor: Samuel H. Yalkowsky
  • Patent number: 4292445
    Abstract: The present invention relates to novel amido and sulfonamido derivatives of 2-decarboxy-2-amino-methyl-PG-type compounds. These analogs are useful as nasal decongestants, antifertility agents, and as cytoprotection agents.
    Type: Grant
    Filed: April 28, 1980
    Date of Patent: September 29, 1981
    Assignee: The Upjohn Company
    Inventor: Norman A. Nelson
  • Patent number: 4289785
    Abstract: 5-Oxa-17-phenyl-18,19,20-trinor-PGF.sub.1 .alpha. alkyl esters and 5-oxa-17-phenyl-18,19,20-trinor PGF.sub.1 .alpha. amide are combined with certain other prostaglandins in synergistic combinations to induce menses in female primates, preferably humans. These synergistic prostaglandin compositions have improved efficacy and safety.
    Type: Grant
    Filed: August 6, 1980
    Date of Patent: September 15, 1981
    Assignee: The Upjohn Company
    Inventor: John W. Wilks
  • Patent number: 4289761
    Abstract: This invention provides a method for inducing menses and interrupting early pregnancy in female primate mammals, especially humans, which comprises the concomitant administration of a 5-oxa-17-phenyl-18,19,20-trinor-PGF.sub.1 .alpha., alkyl ester and an estrogenic compound. This invention further provides a pharmaceutical composition having these compounds as active ingredients. This method provides greater efficacy and safety as compared with the prior art.
    Type: Grant
    Filed: August 6, 1980
    Date of Patent: September 15, 1981
    Assignee: The Upjohn Company
    Inventor: John W. Wilks
  • Patent number: 4288440
    Abstract: The present invention relates to certain 6-alkyl-1,2-dihydro-2-oxo-3-substituted pyridine derivatives, their preparation and antihyperglycemic use.
    Type: Grant
    Filed: August 29, 1980
    Date of Patent: September 8, 1981
    Assignee: The Upjohn Company
    Inventor: Gilbert A. Youngdale
  • Patent number: 4287338
    Abstract: The present invention provides novel substituted sulfooxy-pyrimidinium, -pyridinium, and -triazinium hydroxide inner salts. These compounds are useful for the treatment of hypertension and peripheral vascular diseases. They are formed by reacting the corresponding aminopyrimidine, aminotriazine, and aminopyridine N-oxides with a latent sulfate source such as pyridinium-sulfur trioxide complex, triethylamine-sulfur trioxide complex, chlorosulfonic acid or chlorosulfuryl chloride.
    Type: Grant
    Filed: March 10, 1980
    Date of Patent: September 1, 1981
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4284795
    Abstract: The present invention provides novel 19,20-didehydro-PG.sub.2 compounds, methods for their preparation and pharmacological use for the induction of prostaglandin-like effect.
    Type: Grant
    Filed: October 17, 1979
    Date of Patent: August 18, 1981
    Assignee: The Upjohn Company
    Inventor: John C. Sih
  • Patent number: 4284569
    Abstract: The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.
    Type: Grant
    Filed: January 28, 1980
    Date of Patent: August 18, 1981
    Assignee: The Upjohn Company
    Inventor: Ronald B. Gammill
  • Patent number: 4283558
    Abstract: The present invention provides novel 2-decarboxy-2-hydroxymethyl-19,20-didehydro-13,14-dihydro-PG.sub.1 compounds methods for their preparation and pharmacological use for the induction of prostaglandin-like effect.
    Type: Grant
    Filed: October 26, 1979
    Date of Patent: August 11, 1981
    Assignee: The Upjohn Company
    Inventor: John C. Sih
  • Patent number: 4281013
    Abstract: The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic 6-halofurochromones.
    Type: Grant
    Filed: February 13, 1979
    Date of Patent: July 28, 1981
    Assignee: The Upjohn Company
    Inventors: Paul E. Schurr, Charles E. Day
  • Patent number: 4275213
    Abstract: The present invention provides novel isoxazolyl derivatives prepared from 9.alpha.,11.alpha.-epoxyimino-9,11,15-trideoxy-PGF-type compounds. These novel compounds are useful as anti-inflammatory agents, anti-asthma agents, and platelet aggregation inhibitors in mammals and especially in humans.
    Type: Grant
    Filed: May 12, 1980
    Date of Patent: June 23, 1981
    Assignee: The Upjohn Company
    Inventor: Gordon L. Bundy
  • Patent number: 4239780
    Abstract: Phospholipase A.sub.2 inhibition the present invention relates to a method for treating or preventing a phospholipase A.sub.2 mediated condition (PMC) in a mammal suffering from or susceptible to such a condition. The method involves administering to such a mammal an amount effective to treat the condition of a compound selected from a certain group of butyrophenones.
    Type: Grant
    Filed: October 11, 1979
    Date of Patent: December 16, 1980
    Assignee: The Upjohn Company
    Inventor: Donald P. Wallach
  • Patent number: 4226772
    Abstract: The compound of the formula ##STR1## wherein R' and R" are alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2 is phenyl, o-chlorophenyl, o-fluorophenyl, or 2,6-difluorophenyl, is prepared by reacting a 1-halomethyl-6-phenyl-4H-s-triazo[4,3-a][1,4]-benzodiazepine with N,N-dimethylhydroxylamine and a strong base. The compound II and its pharmacologically acceptable acid addition salts have sedative and tranquilizing activity.
    Type: Grant
    Filed: September 8, 1978
    Date of Patent: October 7, 1980
    Assignee: The Upjohn Company
    Inventor: Jackson B. Hester, Jr.