Patents by Inventor Philippe L. Durette

Philippe L. Durette 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: 4866036
    Abstract: Disclosed are specific dipeptidyl 5-0, 6-0-Acyl-2-amino-2-deoxy-D-glucofuranoses, which, either alone, or in combination with an anti-AIDS drug, e.g. azidothymidine, provide protection in human individuals whose resistance to infection has been specifically suppressed by an AIDS-related (HIV) virus, as well as help to suppress the AIDS-related infection itself.
    Type: Grant
    Filed: October 5, 1987
    Date of Patent: September 12, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4814501
    Abstract: Pyrolysis of substituted salicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)benzamide. Similarly, substituted 6-azasalicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)-6-aza-benzamide.
    Type: Grant
    Filed: December 28, 1987
    Date of Patent: March 21, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Robert K. Baker, Philippe L. Durette, Robert A. Frankshun
  • Patent number: 4800211
    Abstract: 3-Hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by:(1) treating a substituted 2-halobenzoate with a thioacetamide.(2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide; and(3) further synthetic modification of compounds prepared above.These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandins and/or leukotriene mediated diseases.
    Type: Grant
    Filed: August 18, 1986
    Date of Patent: January 24, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Allan N. Tischler, Philippe L. Durette, Bruce E. Witzel, Thomas J. Lanza, Jr.
  • Patent number: 4767766
    Abstract: 3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthio-alkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory diseases and other leukotriene mediated diseases.
    Type: Grant
    Filed: January 30, 1987
    Date of Patent: August 30, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Kathleen M. Rupprecht, Arsenio A. Pessolano, Philippe L. Durette
  • Patent number: 4760161
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit lipoxygenase, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: April 25, 1983
    Date of Patent: July 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Timothy F. Gallagher
  • Patent number: 4760086
    Abstract: N-Alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by:(1) treating a substituted 2-halobenzoate with thioacetamide followed by N-alkenylation with appropriate agents, such as aldehydes, ketones, enol ethers, epoxides, acetals or ketals;(2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide, followed by dehydration; and(3) further synthetic modification of compounds prepared above.These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandins and/or leukotriene mediated diseases.
    Type: Grant
    Filed: February 27, 1985
    Date of Patent: July 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Allan N. Tischler, Bruce E. Witzel, Philippe L. Durette, Kathleen M. Rupprecht, Timothy F. Gallagher, Debra L. Allison, Marvin M. Goldenberg
  • Patent number: 4663344
    Abstract: 3-Hydroxybenzo[b]thiophene derivatives, such as 2-aralkyl, 2-alkyl and 2-alkenyl-3-hydroxybenzo[b]-thiophenes, were prepared by, among other methods, ring closure of 2-(2-carboxy-phenylthio)-.alpha.-substituted acetic acids. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory diseases and other prostaglandin and/or leukotriene mediated diseases.
    Type: Grant
    Filed: March 11, 1985
    Date of Patent: May 5, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Bruce E. Witzel, Kathleen M. Rupprecht, Allan N. Tischler, Timothy F. Gallagher
  • Patent number: 4652553
    Abstract: Described are derivatives of glycolipids with substituted steroids bridged via a medium length hydrocarbon chain to 1-thio-D-mannopyranoses or 1-thio-L-fucopyranoses. These compounds protect an immunocompromised human or animal host against opportunistic infection by virtue of their immunostimulant properties.
    Type: Grant
    Filed: November 25, 1985
    Date of Patent: March 24, 1987
    Assignee: Merck & Co., Inc.
    Inventors: William K. Hagmann, Philippe L. Durette, Mitree M. Ponpipom
  • Patent number: 4544502
    Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R.sup.1 is lower alkyl or aralkyl, such as benzyl and the like; and R.sup.2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
    Type: Grant
    Filed: January 25, 1984
    Date of Patent: October 1, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4526999
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit lipoxygenase, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: April 25, 1983
    Date of Patent: July 2, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Timothy F. Gallagher
  • Patent number: 4515722
    Abstract: Phosphatidyl inositol analogs are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These phosphatidyl inositol analogs are prepared by condensation of a protected inositol with a substituted phosphonic or phosphorous acid followed by removal of protecting groups.
    Type: Grant
    Filed: March 30, 1982
    Date of Patent: May 7, 1985
    Assignee: Merck & Co., Inc.
    Inventors: Shu S. Yang, Thomas R. Beattie, Philippe L. Durette, Timothy F. Gallagher, Tsung-Ying Shen
  • Patent number: 4491659
    Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II, III and IV to known lactone V which is known to be useful via acid VI in the total synthesis of thienamycin (VII): ##STR1## wherein R.sup.1 is hydrogen or a removable protecting group; R is a removable protecting group.
    Type: Grant
    Filed: May 26, 1983
    Date of Patent: January 1, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4448976
    Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R.sup.1 is lower alkyl or aralkyl, such as benzyl and the like; and R.sup.2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
    Type: Grant
    Filed: February 7, 1983
    Date of Patent: May 15, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4429118
    Abstract: Disclosed is methyl 3-azido-4-C-cyano-2,3,4,6-tetradeoxy-.alpha.-D-arabino-hexopyranoside and processes for its preparation from methyl 3-azido-2,3,6-trideoxy-.alpha.-D-arabino-hexopyranoside via the 4-bromo-4-deoxy intermediate; wherein the two inversions of configuration at C-4 result in a net retention of the .alpha.-D-arabino stereochemistry.
    Type: Grant
    Filed: May 3, 1982
    Date of Patent: January 31, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4415731
    Abstract: Disclosed is a process for preparing methyl 2,6-dideoxy-.alpha.-D-arabino-hexopyranoside from methyl 2-deoxy-.alpha.-D-glucopyranoside.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: November 15, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4391800
    Abstract: 2-Amino-2-deoxy-.beta.-D-glucopyranosyl-(1-4)-2-amino-2-deoxy-D-glucoses of the general structural formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl (1-7C), substituted alkyl (1-7C), phenyl, substituted phenyl, benzyl, or substituted benzyl;R.sub.2 is alkyl, substituted alky, phenyl, or substituted phenyl and each R.sub.2 may be the same group or a different group;R.sub.3 is H or ##STR2## wherein R.sub.8 is H or lower alkyl (1-10C), and provided at least one of R.sub.3 is not H,R.sub.9 is H, or R.sub.9 -R.sub.10 together is --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sub.10 is H, alkyl (L-7C), hydroxymethyl, mercaptomethyl, benzyl, or substituted benzyl;R.sub.11 and R.sub.12 each is carboxyl, esterified carboxyl (1-7C), amidated carboxyl, or mono- or di-alkyl- (1-3C) amidated carboxyl;R.sub.4 and R.sub.5 are the same or different and are H, aliphatic or aromatic acyl (2-21C) or substituted acyl (2-21C);when R.sub.8 is lower alkyl, the stereochemistry at asymmetric center I can be either D or L;when R.sub.
    Type: Grant
    Filed: April 27, 1979
    Date of Patent: July 5, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Tsung-Ying Shen
  • Patent number: 4384998
    Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R.sup.1 is lower alkyl or aralkyl, such as benzyl and the like; and R.sup.2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: May 24, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4377570
    Abstract: 2-Amino-2-deoxy-glycoses of the general structural formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl (1-7C), substituted alkyl (1-7C), phenyl, substituted phenyl, benzyl, or substituted benzyl;R.sub.2 is alkyl, substituted alkyl, phenyl, or substituted phenyl;R.sub.3 is H or lower alkyl (1-10C) with the proviso that when the aminoglycose has the 2-amino-2-deoxy-D-glucose configuration, R.sub.3 cannot be H;R.sub.4 and R.sub.5 are same or different and are H, aliphatic or aromatic acyl (2-21C) or substituted acyl (2-21C);R.sub.6 is H, or R.sub.6 -R.sub.7 together is --CH.sub.2 --CH.sub.2 --CH.sub.2 --,R.sub.7 is H, alkyl (1-7C), hydroxymethyl, mercaptomethyl, benzyl, or substituted benzyl;R.sub.8 and R.sub.9 each is carboxyl, esterified carboxyl (1-7C), amidated carboxyl, or mono- or di-alkyl-(1-3C)-amidated carboxyl;provided that when R.sub.
    Type: Grant
    Filed: October 3, 1980
    Date of Patent: March 22, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Tsung-Ying Shen
  • Patent number: 4368190
    Abstract: Immunologically active compounds of the formula: ##STR1## wherein: R.sub.1 is C.sub.1-7 alkyl; substituted C.sub.1-7 alkyl; phenyl; or substituted phenyl;R.sub.2 is hydrogen; C.sub.1-7 alkyl; substituted C.sub.1-7 alkyl; phenyl; substituted phenyl; phenyl C.sub.1-4 alkyl; or substituted phenyl C.sub.1-4 alkyl;R.sub.3 and R.sub.4 may be the same or different and are each independently hydrogen, provided that R.sub.3 and R.sub.4 may not both be hydrogen; or ##STR2## where X is --O--; --S--; or ##STR3## R.sub.10 is hydrogen; C.sub.1-30 alkyl; C.sub.2-30 alkenyl; C.sub.1-30 alkoxy; phenyl; C.sub.1-20 alkylsulfonyl; or cholesteryl;R.sub.11, R.sub.12, R.sub.13, R.sub.14, and R.sub.15 may be the same or different and are each independently hydrogen; C.sub.1-20 alkyl; C.sub.1-20 alkylcarbonyloxy; amino; benzyl; C.sub.1-20 alkoxymethyl; C.sub.1-20 alkylamido; or ##STR4## r is 0 or 1; s is 0 or 1; and t is 0 to 20; provided that s may only be 0 when both r and t are greater than 0 or when r is 0 and R.sub.
    Type: Grant
    Filed: April 17, 1980
    Date of Patent: January 11, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Tsung-Ying Shen, Philippe L. Durette, Conrad P. Dorn, Jr., James B. Doherty, Richard T. Dean
  • Patent number: 4348325
    Abstract: Disclosed is methyl 3-azido-4-C-cyano-2,3,4,6-tetradeoxy-.alpha.-D-arabino-hexopyranoside and processes for its preparation from methyl 3-azido-2,3,6-trideoxy-.alpha.-D-arabino-hexopyranoside via the 4-bromo-4-deoxy intermediate; wherein the two inversions of configuration at C-4 result in a net retention of the .alpha.-D-arabino stereochemistry.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: September 7, 1982
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette