Patents by Inventor Saul B. Kadin

Saul B. Kadin has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4808601
    Abstract: Certain novel 2-oxindole compounds, having an acyl substituent at both the 1-position and the 3-position, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and antiinflammatory agents in mammalian subjects. These 1,3-diacyl-2-oxindole compounds are of particular value for acute administration for ameliorating pain in human patients recovering from surgery or trauma, and also for chronic administration to human subjects for alleviating the symptoms of chronic diseases such as rheumatoid arthritis and osteoarthritis.
    Type: Grant
    Filed: May 19, 1988
    Date of Patent: February 28, 1989
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4791131
    Abstract: Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.
    Type: Grant
    Filed: December 31, 1987
    Date of Patent: December 13, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4791129
    Abstract: 1,3,-Dicarboxamidooxindoles as antiinflammatory agents prepared by reaction of the 1-carbamoyloxindole with an isocyanate or by aminolysis of the corresponding alkyl 1-carbamoyloxindole-3-carboxylate.
    Type: Grant
    Filed: November 9, 1987
    Date of Patent: December 13, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4752609
    Abstract: Certain novel 2-oxindole compounds, having an acyl substituent at both the 1-position and the 3-position, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and antiinflammatory agents in mammalian subjects. These 1,3-diacyl-2-oxindole compounds are of particular value for acute administration for ameliorating pain in human patients recovering from surgery or trauma, and also for chronic administration to human subjects for alleviating the symptoms of chronic diseases such as rheumatoid arthritis and osteoarthritis.
    Type: Grant
    Filed: January 7, 1987
    Date of Patent: June 21, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4730004
    Abstract: Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.
    Type: Grant
    Filed: February 2, 1987
    Date of Patent: March 8, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4725616
    Abstract: 1,3-Dicarboxamidooxindoles as antiinflammatory agents prepared by reaction of the 1-carbamoyloxindole with an isocyanate or by aminolysis of the corresponding alkyl 1-carbamoyloxindole-3-carboxylate.
    Type: Grant
    Filed: January 20, 1987
    Date of Patent: February 16, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4721712
    Abstract: Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also on the carboxamide nitrogen atom, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and anti-inflammatory agents in mammalian subjects. These 2-oxindole-1-carboxamide compounds are of particular value for acute administration for ameliorating pain in human patients recovering from surgery or trauma, and also for chronic administration to human subjects for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis. Certain 2-oxindole-1-carboxamide compounds unsubstituted at C-3, but having an acyl substituent on the carboxamide nitrogen atom, are useful as intermediates to the aforementioned analgesic and anti-inflammatory agents.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: January 26, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4690943
    Abstract: Certain novel 2-oxindole compounds, having an acyl substituent at both the 1-position and the 3-position, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and antiinflammatory agents in mammalian subjects. These 1,3-diacyl-2-oxindole compounds are of particular value for acute administration for ameliorating pain in human patients recovering from surgery or trauma, and also for chronic administration to human subjects for alleviating the symptoms of chronic diseases such as rheumatoid arthritis and osteoarthritis.
    Type: Grant
    Filed: June 20, 1985
    Date of Patent: September 1, 1987
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4678802
    Abstract: 1-Acylcarbamoyloxindole-3-carboxamides as antiinflammatory agents prepared by reaction of the 1-acylcarbamoyloxindole with an isocyanate in the presence of a basic reagent.
    Type: Grant
    Filed: January 31, 1986
    Date of Patent: July 7, 1987
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4658037
    Abstract: Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also on the carboxamide nitrogen atom, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and anti-inflammatory agents in mammalian subjects. Certain 2-oxindole compounds unsubstituted at the 1-position but having an acyl substituent at C-3 of the formula ##STR1## and the base salts thereof, wherein X is hydrogen, 5-fluoro, 5-chloro or 5-trifluoromethyl; Y is hydrogen, 6-fluoro, 6-chloro or 6-trifluoromethyl; and R.sup.1 is benzyl, furyl, thienyl or thienylmethyl; provided that when X and Y are both hydrogen, R.sup.1 is not benzyl are useful as intermediates to the aforementioned analgesic and anti-inflammatory agents.
    Type: Grant
    Filed: December 30, 1985
    Date of Patent: April 14, 1987
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4623725
    Abstract: A series of novel [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives wherein the amine group is optionally substituted with lower alkyl, phenylalkyl having up to three carbon atoms in the alkyl moiety or alkanoyl having from two to five carbon atoms, or the amine group alternatively completes a piperazino ring, the quinoxaline ring is optionally substituted with fluorine, chlorine, bromine or methoxy, and the triazolo ring is optionally substituted with lower alkyl, lower perfluoroalkyl or phenyl are disclosed. These novel compounds are useful for treatment of symptoms associated with depression. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention.
    Type: Grant
    Filed: November 8, 1985
    Date of Patent: November 18, 1986
    Assignee: Pfizer Inc.
    Inventors: Saul B. Kadin, Reinhard Sarges
  • Patent number: 4569942
    Abstract: Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also further substituted on the carboxamide nitrogen by an alkyl, cycloalkyl, phenyl or substituted phenyl group, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and antiinflammatory agents in mammalian subjects. These 2-oxindole-1-carboxamide compounds are of particular value for ameliorating pain in human patients recovering from surgery or trauma, and alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.Certain 2-oxindole-1-carboxamide compounds unsubstituted at C-3, but having a substituent on the carboxamide nitrogen, are useful as intermediates to the analgesic and antiinflammatory agents of the invention.
    Type: Grant
    Filed: March 22, 1985
    Date of Patent: February 11, 1986
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4556672
    Abstract: Certain new 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and in alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: December 3, 1985
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4535081
    Abstract: Antiallergy and antiulcer agents having the formula (I), ##STR1## and their pharmaceutically acceptable salts, wherein R.sub.1 and R.sub.2 taken separately are each hydrogen or lower alkyl; and R.sub.1 and R.sub.2 taken together are alkylene of 3-9 carbon atoms or phenylalkylene of 9-11 carbon atoms, with the proviso that the ring so formed is between 5- and 8-membered; acids of the formula (II), ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.3 is hydrogen, which are useful as intermediates for compounds of the formula (I), but in many instances also possess the same useful biological activity as do formula I compounds; and intermediates of the formula II wherein R.sub.1 and R.sub.2 are defined as above, and R.sub.3 is alkyl of 1 to 4 carbon atoms, carbalkoxy of 2 to 5 carbon atoms, carbophenoxy or carbobenzoxy, are also described.
    Type: Grant
    Filed: August 17, 1983
    Date of Patent: August 13, 1985
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4423048
    Abstract: Antiallergy and antiulcer agents having the formula (I), ##STR1## and their pharmaceutically acceptable salts, wherein R.sub.1 and R.sub.2 taken separately are each hydrogen or lower alkyl; and R.sub.1 and R.sub.2 taken together are alkylene of 3-9 carbon atoms or phenylalkylene of 9-11 carbon atoms, with the proviso that the ring so formed is between 5- and 8-membered; acids of the formula (II), ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.3 is hydrogen, which are useful as intermediates for compounds of the formula (I), but in many instances also possess the same useful biological activity as do formula I compounds; and intermediates of the formula II wherein R.sub.1 and R.sub.2 are defined as above, and R.sub.3 is alkyl of 1 to 4 carbon atoms, carbalkoxy of 2 to 5 carbon atoms, carbophenoxy or carbobenzoxy, are also described.
    Type: Grant
    Filed: October 19, 1981
    Date of Patent: December 27, 1983
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4414388
    Abstract: Antiallergy and antiulcer agents having the formula (I), ##STR1## and their pharmaceutically acceptable salts, wherein R.sub.1 and R.sub.2 taken separately are each hydrogen or lower alkyl; and R.sub.1 and R.sub.2 taken together are alkylene of 3-9 carbon atoms or phenylalkylene of 9-11 carbon atoms, with the proviso that the ring so formed is between 5- and 8-membered; acids of the formula (II), ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.3 is hydrogen, which are useful as intermediates for compounds of the formula (I), but in many instances also possess the same useful biological activity as do formula I compounds; and intermediates of the formula II wherein R.sub.1 and R.sub.2 are defined as above, and R.sub.3 is alkyl of 1 to 4 carbon atoms, carbalkoxy of 2 to 5 carbon atoms, carbophenoxy or carbobenzoxy, are also described.
    Type: Grant
    Filed: December 14, 1981
    Date of Patent: November 8, 1983
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4343813
    Abstract: The compounds of the invention are certain new propenamide and 2-butenamide compounds, having a (4-carboxy-2-oxo-pyrrolidino)phenyl substituent at the 3-position, and certain esters thereof, and certain cyclopropanecarboxamide compounds, having a (4-carboxy-2-oxo-pyrrolidino)phenyl substituent at the 2-position, and certain esters thereof. The compounds of the invention are useful for antagonizing the spasmogenic activity of the slow-reacting substance of anaphylaxis (SRS-A) in a human subject. In particular, the compounds of the invention are useful for preventing and treating certain obstructive airways diseases, notably allergic bronchial asthma, allergic rhinitis and certain skin disorders, in human subjects.
    Type: Grant
    Filed: May 18, 1981
    Date of Patent: August 10, 1982
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4342781
    Abstract: Certain new diphenylpropenamides having a carboxyalkanamido or a carboxyalkenamido group on one of the phenyl rings and their use for antagonizing the spasmogenic activity of the slow-reacting substance of anaphylaxis (SRS-A) in a human subject. In particular, the compounds of the invention are useful for preventing and treating certain obstructive airways diseases, notably allergic bronchial asthma, allergic rhinitis and certain skin disorders, in human subjects.
    Type: Grant
    Filed: May 29, 1981
    Date of Patent: August 3, 1982
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4331683
    Abstract: The compounds of the invention are certain new propenamides and 2-butenamides having a (carboxyalkanamido)phenyl or a (carboxyalkenamido)phenyl group at the 3-position, and certain esters thereof, and certain cyclopropanecarboxamide compounds having a (carboxyalkanamido)phenyl group or a (carboxyalkenamido)phenyl group at the 2-position, and certain esters thereof. The compounds are useful for antagonizing the spasmogenic activity of slow-reacting substance of anaphylaxis (SRS-A) in a human subject. In particular, the compounds of the invention are useful for preventing and treating certain obstructive airways diseases, notably allergic bronchial asthma, allergic rhinitis and certain skin disorders, in human subjects.
    Type: Grant
    Filed: August 13, 1981
    Date of Patent: May 25, 1982
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4321372
    Abstract: This invention encompasses orally effective antiulcer agents of the formula ##STR1## wherein X is hydroxy, (C.sub.1 -C.sub.5)-alkoxy, phenoxy, benzyloxy, or --NH(CH.sub.2).sub.n Y wherein n is an integer of value 2 to 4 and Y is di-(C.sub.1 -C.sub.3)-alkylamino, 1-pyrrolidinyl, 1-piperidinyl or 4-morpholinyl;R' and R" when taken together are (C.sub.3 -C.sub.8)-alkylene, with the proviso that the ring so formed is 5- to 8-membered;R' and R" when taken separately are each independently hydrogen, (C.sub.1 -C.sub.6)-alkyl or (C.sub.5 -C.sub.6)-cycloalkyl, with the proviso that when X is other than --NH(CH.sub.2).sub.n Y, at least one of R' and R" is other than hydrogen;the pharmaceutically acceptable cationic salts thereof when X is hydroxyl, and the pharmaceutically acceptable anionic salts thereof when X is --NH(CH.sub.2).sub.n Y.
    Type: Grant
    Filed: June 16, 1980
    Date of Patent: March 23, 1982
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin