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:
July 5, 2005
Assignee:
Wyeth Holdings Corporation
Inventors:
Darren Robert Abbanat, Valerie Sue Bernan, Russell George Dushin, Michael Greenstein, Haiyin He, Stanley Albert Lang, Howard Newman, Subas Sakya, Phaik-Eng Sum, Alan Gordon Sutherland, Ting-Zhong Wang, Jason Arnold Lotvin, Mark Edward Ruppen, Arthur Emergy Bailey, Ping Cai, Bo Shen, Fangming Kong
Abstract: The invention pertains to pharmaceutical compositions of Zosyn® piperacillin with tazobactam in the presence of a buffer, preferably citrate, a particulate formation inhibitor, preferably EDTA optionally an aminoglycoside which when frozen and thawed or lyophilized and reconstituted reform a solution which has decreased particulate formation.
Type:
Grant
Filed:
April 14, 2003
Date of Patent:
May 31, 2005
Assignee:
Wyeth Holdings Corporation
Inventors:
Jonathan Marc Cohen, Syed M. Shah, Christian Luther Ofslager, Mahdi Fawzi
Abstract: The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects of chemotherapeutic drugs.
Type:
Grant
Filed:
February 28, 2002
Date of Patent:
April 12, 2005
Assignee:
Wyeth Holdings Corporation
Inventors:
Sridhar Krishna Rabindran, Haiyin He, Lee Martin Greenberger
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:
March 1, 2005
Assignee:
Wyeth Holdings Corporation
Inventors:
Joseph William Epstein, Semiramis Ayral-Kaloustian
Abstract: The invention provides compounds of the Formula 1 wherein the definitions of m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are in the specification. These compounds are useful as antibacterial agents.
Abstract: This disclosure describes new antibiotic Cytosporacin having the structure:
The invention relates to a new antibiotic designated Cytosporacin, to its production by fermentation, to methods for its recovery and concentration from the crude solutions, and to process for its purification. The invention includes within its scope the agent in dilute form, as a crude concentrate, and in pure form. The invention also relates to the use of the compound according to the invention in antimicrobial compositions and as antiseptics or disinfectants.
Type:
Grant
Filed:
October 14, 2003
Date of Patent:
August 31, 2004
Assignee:
Wyeth Holdings Corporation, Five Giralda Farms
Abstract: This invention relates to a method of using novel 5-(arylsulfonyl)-,5-(arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar′, R6, m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras-oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
August 31, 2004
Assignee:
Wyeth Holdings Corporation
Inventors:
Joseph William Epstein, Semiramis Ayral-Kaloustian, Gary Harold Birnberg, Edward James Salaski, Gloria Jean Macewan, Katherine Cheung
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:
August 23, 2002
Date of Patent:
May 25, 2004
Assignee:
Wyeth Holdings Corporation
Inventors:
Joseph William Epstein, Semiramis Ayral-Kaloustian
Abstract: This invention relates to antibiotic compounds AA896 of the formula
wherein:
R1 is H, aryl, alkyl (C1-C20), —CH2-aryl, —C(O)alkyl(C1-C20), —C(O)NHalkyl(C1-C20), or —C(O)NHaryl;
R2 is H, alkyl (C1-C20), —CH2aryl, alkyl (C1-C20) or —C(O)alkyl(C1-C20);
R3 is —OH;
R2 and R3 may optionally be taken together to form a moiety
R4 is alkyl (C1-C20), or aryl;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 25, 2002
Date of Patent:
April 27, 2004
Assignee:
Wyeth Holdings Corporation
Inventors:
Yang-I Lin, Zhong Li, Gerardo DelaCruz Francisco, Leonard Alexander McDonald
Abstract: The invention relates to compounds of Formula (I) wherein R1, (R2)v, R3 and n are defined in the specification 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:
August 23, 2002
Date of Patent:
April 6, 2004
Assignee:
Wyeth Holdings Corporation
Inventors:
Edward James Salaski, Semiramis Ayral-Kaloustian, Joseph William Epstein
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: Compounds of Formula (I):
wherein R1, R2, R3, X, Y, Z and Q are as defined in the specification which compounds are inhibitors of Ras farnesyl-protein transferase enzyme (FPTase), and useful in treating ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid and processes for the preparation of said compounds of Formula (I).
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
March 23, 2004
Assignee:
Wyeth Holdings Corporation
Inventors:
Semiramis Ayral-Kaloustian, Irwin Hollander, Ann Aulabaugh
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-B1, 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:
April 25, 2002
Date of Patent:
February 10, 2004
Assignee:
Wyeth Holdings Corporation
Inventors:
Guy Thomas Carter, Jason Arnold Lotvin, Leonard Alexander McDonald
Abstract: The invention is a process improvement for producing the carbapenem antibacterial agent (4R, 5S, 6S)-3-[[2R,3R)-2-[[[(S)-2-amino-3-methyl-1-oxobutyl]amino]methyl]tetrahydro-3-furanyl]thio]-6-[R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid by hydrogenation of 4-nitrobenzyl (4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-3-{[2R,3R)-2-({[(2S)-3-methyl-2-({[4-nitrobenzyl)oxy]carbonyl}amino)butanoyl]amino}methyl)-tetrahydrofuran-3-yl]thio}-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate in a biphasic solvent mixture comprising a water portion and an organic solvent portion, not containing an acid acceptor.
Type:
Grant
Filed:
July 9, 2001
Date of Patent:
November 18, 2003
Assignee:
Wyeth, Five Giralda Farms
Inventors:
Tarek Mansour, Phaik-Eng Sum, Yang-I Lin, Zhong Li
Abstract: The invention pertains to adjuvant and vaccine compositions of monophosphoryl lipid A, sugar and optionally an amine based surfactant, which when frozen and thawed or lyophilized and reconstituted reform a colloidal suspension having a light transmission of greater than or equal to 88% as measured spectrophotometrically.
Type:
Grant
Filed:
August 30, 2001
Date of Patent:
October 21, 2003
Assignee:
Wyeth Holdings Corporation
Inventors:
Vincent James LaPosta, John Hayward Eldridge
Abstract: This invention relates to a method of using novel 5-(arylsulfonyl)-5-(arylsulfinyl)- and 5-(arylsulfanyl)thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar′, R6, m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras- oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
August 12, 2003
Assignee:
Wyeth Holdings Corporation
Inventors:
Semiramis Ayral-Kaloustian, Joseph William Epstein, Gary H. Birnberg, Edward James Salaski, Gloria Jean Macewan, Katherine Cheung
Abstract: The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects of chemotherapeutic drugs.
Abstract: This invention provides compounds of Formula (I), having the structure
where T, Z, X, A, R1, R2a, R2b, R2c, R3, R4, and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.
Type:
Grant
Filed:
March 28, 2001
Date of Patent:
February 18, 2003
Assignee:
Wyeth
Inventors:
Diane Harris Boschelli, Yanong Wang, Frank Charles Boschelli, Dan Maarten Berger, Nan Zhang, Dennis William Powell, Fei Ye, Ayako Yamashita, Frenel Fils DeMorin, Biqi Wu, Hwei-Ru Tsou, Elsebe Geraldine Overbeek-Klumpers, Allan Wissner
Abstract: The present invention relates to novel substituted pyridine compounds of Formula (I)
wherein the moiety Z, R1, R2 and R3 are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 1, 2000
Date of Patent:
January 7, 2003
Assignee:
Wyeth, Five Giralda Farms
Inventors:
Chingfan Chiu, Zhilian Tang, John W. Ellingboe
Abstract: The 6-(spirocyclopropyl)-penicillanic acid 4,4-dioxides of the general Formula (I):
as defined herein above which exhibit beta-lactamase inhibiting activity, use of such compounds in combination with beta-lactam antibiotics for inhibiting beta-lactamases, pharmaceutical compositions and processes for preparing such compounds.
Type:
Grant
Filed:
January 26, 2001
Date of Patent:
December 3, 2002
Assignee:
American Cyanamid Company
Inventors:
Vincent P. Sandanayaka, Amarnauth S. Prashad