Patents by Inventor Raphael Pappo

Raphael Pappo 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: 4670569
    Abstract: The present invention relates to 5-fluoro-PGI.sub.2 derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction. Also disclosed is the process for preparing them and the appropriate intermediates.
    Type: Grant
    Filed: March 8, 1985
    Date of Patent: June 2, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Leonard N. Nysted, Raphael Pappo
  • Patent number: 4540801
    Abstract: The present invention relates to 5-fluoro-PGI.sub.2 derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction. Also disclosed is the process for preparing them and the appropriate intermediates.
    Type: Grant
    Filed: July 13, 1983
    Date of Patent: September 10, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Leonard N. Nysted, Raphael Pappo
  • Patent number: 4522814
    Abstract: A water extract of homogenized Cryptosiphonia woodii is useful for the treatment of herpes simplex viral infections. The active agent in the extract is a polysaccharide containing glucose and galactose.Herpes infections may be treated in subjects, e.g. human patients, by administering to the subject an effective amount of an aqueous extract of C. woodii, particularly a water extract. This treatment method is effective for treating subjects both prior to and subsequent to infection. It may involve topical application to alleviate symptoms associated with herpes infections or desirably may be systemic, e.g. by oral administration, to eradicate the virus and thereby prevent symptom recurrence.
    Type: Grant
    Filed: November 5, 1982
    Date of Patent: June 11, 1985
    Assignee: Raphael Pappo
    Inventors: Arthur M. Nonomura, Raphael Pappo
  • Patent number: 4388462
    Abstract: A composition useful for relieving the symptoms of psoriasis in humans are disclosed. The composition is an N-trialkylsilyl-substituted 6-aminonicotinamide. The composition is applied in a suitable pharmaceutical base, such as a cream or ointment, to the affected area of skin.
    Type: Grant
    Filed: July 20, 1981
    Date of Patent: June 14, 1983
    Assignee: International Plant Research Institute, Inc.
    Inventors: Raphael Pappo, Kenneth M. Otteson
  • Patent number: 4385052
    Abstract: The use of a composition for relieving the symptoms of psoriasis in humans is disclosed. The composition is an N-trialkylsilyl-substituted 6-aminonicotinamide. The composition is applied in a suitable pharmaceutical base, such as a cream or ointment, to the affected area of skin.
    Type: Grant
    Filed: July 20, 1981
    Date of Patent: May 24, 1983
    Assignee: International Plant Research Institute, Inc.
    Inventors: Herschel S. Zackheim, Raphael Pappo
  • Patent number: 4348388
    Abstract: 11-Amino-11-deoxydaunorubicin and analogs represented by the formula: ##STR1## wherein: R is hydrogen, hydroxy or methoxy; R.sub.1 is hydrogen or hydroxy; and the pharmaceutically acceptable salts thereof.The compounds are useful in ameliorating tumor growth.
    Type: Grant
    Filed: April 2, 1980
    Date of Patent: September 7, 1982
    Assignee: G.D. Searle & Co.
    Inventors: Robert B. Garland, Raphael Pappo, Paul B. Sollman
  • Patent number: 4328355
    Abstract: A compound of the formula ##STR1## wherein R is hydrogen or lower alkyl having 1-7 carbon atoms; R', R", and R'" are each individually hydrogen or methyl; n is 0-3; and Ar is phenyl, halosubstituted phenyl, lower alkyl substituted phenyl wherein the lower alkyl contains 1-4 carbon atoms, lower alkoxy substituted phenyl wherein the lower alkoxy contains 1-4 carbon atoms, p-biphenyl, or trifluoromethyl substituted phenyl. Compounds of the present invention are useful as antifertility agents.
    Type: Grant
    Filed: September 10, 1979
    Date of Patent: May 4, 1982
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4322543
    Abstract: 4,5-Unsaturated 16-hydroxy prostanoic acid derivatives displaying valuable pharmacological properties, e.g. gastric antisecretory, are described herein.
    Type: Grant
    Filed: October 24, 1980
    Date of Patent: March 30, 1982
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4275192
    Abstract: The present invention relates to bis(4-demethoxydaunorubicin)dihydrazone of the formula ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen or alkyl having from 1 to 4 carbon atoms and X represents(a) alkylene having from 3 to 20 carbon atoms and optionally substituted by one or more hydroxy and/or primary amino groups, or(b) alkylene optionally interrupted by one or more secondary amino groups, the total number of carbon and nitrogen atoms in the resultant chain being 3 to 20and to pharmacologically acceptable salts thereof which are potent inhibitors of neoplastic disease and are also useful as antiviral agents.
    Type: Grant
    Filed: May 3, 1979
    Date of Patent: June 23, 1981
    Assignee: G. D. Searle & Co.
    Inventors: Martin A. Apple, Raphael Pappo
  • Patent number: 4271314
    Abstract: 4,5-Unsaturated 16-hydroxy prostanoic acid derivatives displaying valuable pharmacological properties, e.g. gastric antisecretory, are described herein.
    Type: Grant
    Filed: November 28, 1979
    Date of Patent: June 2, 1981
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4223158
    Abstract: 2,3,5-Trisubstituted cyclopentanealkenoic acids display anti-microbial activity, e.g. anti-bacterial and anti-fungal, and are, in addition, useful as intermediates in the manufacture of prostanoic acid derivatives.
    Type: Grant
    Filed: May 4, 1979
    Date of Patent: September 16, 1980
    Assignee: G. D. Searle & Co.
    Inventors: Mildred S. Bruhn, Raphael Pappo
  • Patent number: 4172953
    Abstract: 2,3,5-Trisubstituted cyclopentanealkenoic acids display anti-microbial activity, e.g. anti-bacterial and anti-fungal, and are, in addition, useful as intermediates in the manufacture of prostanoic acid derivatives.
    Type: Grant
    Filed: March 30, 1973
    Date of Patent: October 30, 1979
    Assignee: G. D. Searle & Co.
    Inventors: Mildred S. Bruhn, Raphael Pappo
  • Patent number: 4161480
    Abstract: The present invention encompasses novel intermediates having the following structural formulas: ##STR1## wherein X is hydrogen, methoxy, or hydroxy; ##STR2## wherein X is hydrogen, methoxy, or hydroxy; and ##STR3## wherein X is hydrogen, methoxy, or hydroxy. Compounds of the present invention are useful in synthesizing 4-demethoxydaunorubicin, daunorubicin, adriamycin, and carminomycin which are potent antitumor agents.
    Type: Grant
    Filed: June 5, 1978
    Date of Patent: July 17, 1979
    Assignee: G. D. Searle & Co.
    Inventors: Raphael Pappo, Robert B. Garland
  • Patent number: 4151187
    Abstract: Compounds of the formula ##STR1## wherein R is phenyl cyclohexyl or lower alkyl containing 1-6 carbon atoms; R" is hydrogen or methyl; R'" is alkenyl or alkynyl having 3-5 carbon atoms; R' is hydrogen, tetrahydrofuran-2-yl tetrahydropyran-2-yl or trialkylsilyl wherein the alkyl contains 1-4 carbon atoms. Compounds of the present invention are useful in synthesizing prostaglandin like molecules which are active anti-secretory agents.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: April 24, 1979
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4149006
    Abstract: The present invention encompasses compounds of the formula: ##STR1## wherein n is 0 or 1; Y represents ethylene or vinylene; R represents hydrogen or lower alkyl having 1-7 carbon atoms; R', R", R'" each individually represent hydrogen or methyl; Ar represents phenyl, halosubstituted phenyl, alkyl substituted phenyl wherein the alkyl contains 1-4 carbon atoms, alkoxy substituted phenyl wherein the alkoxy contains 1-4 carbon atoms, trifluoromethylphenyl, or biphenyl; and the wavy line indicates R or S stereochemistry.
    Type: Grant
    Filed: January 24, 1977
    Date of Patent: April 10, 1979
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4087447
    Abstract: The present invention encompasses novel intermediates of the formula: ##STR1## wherein R is phenyl, cyclohexyl or lower alkyl having 1-6 carbon atoms; R' is trialkylsilyl wherein the alkyls have 1-4 carbon atoms, tetrahydropyran-2-yl, or tetrahydrofuran-2-yl; and R" is lower alkyl having 1 to 3 carbon atoms. Compounds of the present invention are useful in synthesizing prostaglandin-like molecules which are active anti-secretory agents.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: May 2, 1978
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4087621
    Abstract: 7-{3-Hydroxy-2.beta.-[4-hydroxy-4-(lower alkyl)-trans-1-octen-1-yl]-5-oxocyclopent-1.alpha.-yl}hept-5-cis-enoic acids, displaying valuable pharmacological properties, e.g., gastric anti-secretory, are produced by the reaction of 7-(3-oxygenated-5-oxocyclopent-1-en-1-yl)hept-5-cis-enoic acid or ester with the appropriate organometallic reagent.
    Type: Grant
    Filed: November 10, 1975
    Date of Patent: May 2, 1978
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4064350
    Abstract: The present invention encompasses compounds of the formula: ##STR1## wherein one of A and B is methyl and the other is hydrogen, the wavy line represents R or S stereochemistry, n is 2-5, and R is hydrogen or lower alkyl having 1-7 carbon atoms.
    Type: Grant
    Filed: November 22, 1976
    Date of Patent: December 20, 1977
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4060691
    Abstract: 7-{3-Hydroxy-2-[4-hydroxy-4-(lower alkyl)-trans-1-octen-1-yl]-5-oxocyclopent-1-yl{heptanoic acids and esters, displaying valuable pharmacological properties, e.g., gastric anti-secretory, are produced by the reaction of a 7-(3-oxygenated-5-oxocyclopent-1-en-1-yl)heptanoic acid or ester with the appropriate organometallic reagent.
    Type: Grant
    Filed: December 22, 1975
    Date of Patent: November 29, 1977
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Raphael Pappo
  • Patent number: 4053476
    Abstract: The preparation of 7-aza-6-alkoxy-1-tetralones which originates with dihydroresorcinol is disclosed herein. The subject compounds are useful intermediates in the synthesis of various compounds which possess valuable pharmacological properties.
    Type: Grant
    Filed: August 9, 1976
    Date of Patent: October 11, 1977
    Assignee: G. D. Searle & Co.
    Inventors: Robert J. Chorvat, Raphael Pappo