Abstract: The present invention provides a process for the preparation of 6-[(substituted)phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein: R1 is CF3 or C2F5; R2 is H or C1-C3 alkyl; n is an integer of 2, 3, or 4; X is Cl or Br; R3 and R4 are each independently H or C1-C3 alkyl; or R3 and R4 when optionally taken together with the nitrogen atom to which each is attached form a 4 to 6 membered saturated heterocyclic ring having 1-2 nitrogen atoms and 0-1 oxygen atoms or 0-1 sulfur atoms, and optionally substituted with R5; R5 is C1-C3 alkyl; wherein the dotted line is an optional bond.
Type:
Grant
Filed:
December 8, 2004
Date of Patent:
July 8, 2008
Assignee:
Wyeth
Inventors:
Yanzhong Wu, Jean Schmid, Jay Thomas Afragola, David Blum, Semiramis Ayral-Kaloustian
Abstract: The present invention relates to Dibenzonaphthyridine Derivatives, compositions comprising an effective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of a Dibenzonaphthyridine Derivative.
Type:
Grant
Filed:
December 6, 2006
Date of Patent:
June 17, 2008
Assignee:
Wyeth
Inventors:
Ariamala Gopalsamy, Mengxiao Shi, Kristina Kutterer, Kim Timothy Arndt
Abstract: This invention provides compounds of the formula: wherein A?, X and Y are defined in the specification. These compounds are useful as antibacterial agents.
Type:
Grant
Filed:
December 13, 2006
Date of Patent:
April 29, 2008
Assignee:
Wyeth
Inventors:
Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini
Abstract: The invention provides a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof and further provides a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by interacting with tubulin and microtubules and promoting microtubule polymerization which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 29, 2001
Date of Patent:
February 12, 2008
Assignee:
Wyeth
Inventors:
Mark R. Schmitt, Donald R. Kirsch, Jane E. Harris, Carl F. Beyer, Klaus-Jüergen Pees, Paul A. Carter, Waldemar Pfrengle, Guido Albert
Abstract: The invention relates to an enzymatic process for the production of an intermediate, bicyclic-heteroaryl-2-carboxylic acid 7, of the formula wherein X and Y are defined in the specification and which are useful in the preparation of beta-lactamase inhibitors, by selective enzymatic hydrolysis of a mixture of positional hydrolyzable esters of the formulae where X, Y, and R1 are defined in the specification.
Type:
Grant
Filed:
May 12, 2004
Date of Patent:
January 8, 2008
Assignee:
Wyeth Holdings Corporation
Inventors:
Ramesh Venkat Matur, Mark Edward Ruppen
Abstract: This invention relates to certain 6-aryl-7-halo-imidazo[1,2-a]pyrimidines or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals by promotion of microtubule polymerization. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof.
Abstract: There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of ?-lactamase inhibitors.
Type:
Grant
Filed:
May 12, 2004
Date of Patent:
October 2, 2007
Assignee:
Wyeth Holdings Corporation
Inventors:
Michael William Winkley, Anita Wai-Yin Chan, Ivo L. Jirkovsky, Kenneth Alfred Martin Kremer, Joseph Zeldis, Antonia Aristotelevna Nikitenko, Henry Lee Strong, Tarek Mansour, Gulnaz Khafizova, Aranapakam M. Venkatesan
Abstract: The invention provides 6-chloro-5-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-2-pyrazin-2-yl-N-[(1S)-2,2,2-trifluoro-1-methylethyl]pyrimidin-4-amine hemifumarate which is a tubulin inhibitor useful in the treatment of cancer and processes of making hemifumarate compounds and compositioning of the present invention.
Type:
Grant
Filed:
June 12, 2006
Date of Patent:
July 17, 2007
Assignee:
Wyeth
Inventors:
David Michael Blum, Yanzhong Wu, Jean Schmid, Timothy John Doyle, Jay Thomas Afragola
Abstract: This invention relates to a new antibiotic designated P175-A, to production of fermentation of Micromonospora echinospora NRRL 30633, to methods for recovery and concentration from the crude solutions, and to a process for purification and to semisynthetic esters and ethers of P175-A.
Type:
Grant
Filed:
April 28, 2004
Date of Patent:
May 1, 2007
Assignee:
Wyeth Holdings Corporation
Inventors:
Haiyin He, Hui Yu Yang, Scott William Luckman, Valerie S. Bernan
Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-?, such as rheumatoid arthritis, graft rejection, cachexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease or HIV infection.
Abstract: The invention provides new substantially pure antibiotics designated AC-98-1, AC-98-2, AC-98-3, AC-98-4 and AC-98-5 derived from the microorganism Streptomyces hygroscopicus.
Abstract: This invention provides compounds of the formula: wherein A?, X and Y are defined in the specification. These compounds are useful as antibacterial agents.
Type:
Grant
Filed:
December 8, 2004
Date of Patent:
February 13, 2007
Assignee:
Wyeth
Inventors:
Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini
Abstract: The invention relates to a new antibiotic designated Cyan426-A, to its production by fermentation, to methods for its recovery and concentration from the crude solutions, and to a process for its purification and to semisynthetic ethers of Cyan426-A, Cyan426-A-ethers.
Abstract: This invention relates to new antibiotics designated AA-896-A1, AA-896-A2, AA-896-A3, AA-896-A4, AA-896-A5, AA-896-A6, AA-896-Bl, AA-896-B2, AA-896-B3, AA-896-B4, AA-896-B5, AA-896-B6, AA-896-B7, AA-896-C1, AA-896-C2, AA-896-C3, AA-896-C4, AA-896-C5, AA-896-D1, AA-896-D2, AA-896-D3 and AA-896-D4 derived from the microorganism Streptomyces spp. LL-AA896 which are useful an anti-bacterial agents.
Type:
Grant
Filed:
November 14, 2003
Date of Patent:
July 18, 2006
Assignee:
Wyeth Holdings Corporation
Inventors:
Guy Thomas Carter, Jason Arnold Lotvin, Leonard Alexander McDonald
Abstract: The invention relates to new antibiotics designated Cyan-416A, Cyan 416B, Cyan-416C, Cyan-416D and Cyan-416E to their production by fermentation of Acremonium sp. NRRL 30631 to methods for recovery and concentration from the crude solutions, and to a process for purification and to semisynthetic ethers of Cyan-416B.
Abstract: The invention relates to new antibiotics designated Cyan-416A, Cyan 416B, Cyan-416C, Cyan-416D and Cyan-416E to their production by fermentation of Acremonium sp. NRRL 30631 to methods for recovery and concentration from the crude solutions, and to a process for purification and to semisynthetic ethers of Cyan-416B.
Abstract: The disclosure describes the production of anticancer agent LL-D45042, having the structure: by fermentation, to methods for the recovery and concentration of this anticancer agent from crude solutions, and to processes for the purification of this anticancer agent as well as a new microorganism of the species Streptomyces hygroscopicus LL-D45042 and mutants thereof useful in the preparation of this compound.
Abstract: This invention relates to antibiotics selected from the group AW998A, AW998B, AW998C and AW998D derived from the microorganism Streptomyces designated LL-AW998, which are useful as antibacterial agents.
Type:
Grant
Filed:
July 11, 2003
Date of Patent:
March 28, 2006
Assignee:
Wyeth Holdings Corporation
Inventors:
Fangming Kong, Guy Thomas Carter, Scott William Luckman
Abstract: The invention provides compounds of formula Wherein R1, R2, R3, R4, R5, R6a, R6b, R6c, R6d, R6e and R7 are defined in the specification. These compounds are useful as antibiotic agents.
Type:
Grant
Filed:
April 25, 2002
Date of Patent:
November 15, 2005
Assignee:
Wyeth Holdings Corporation
Inventors:
Darren Robert Abbanat, Arthur Emery Bailey, Valerie Sue Bernan, Michael Greenstein, Jason Arnold Lotvin, Mark Edward Ruppen, Alan Gordon Sutherland, Haiyin He
Abstract: The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.
Type:
Grant
Filed:
September 26, 2003
Date of Patent:
September 27, 2005
Assignee:
Wyeth Holdings Corporation
Inventors:
Joseph William Epstein, Semiramis Ayral-Kaloustian