New York City, NY, United States
New York City, NY, United States

Pfizer, Inc. is an American multinational pharmaceutical corporation headquartered in New York City, and with its research headquarters in Groton, Connecticut, United States. It is one of the world's largest pharmaceutical companies by revenues.Pfizer develops and produces medicines and vaccines for a wide range of medical disciplines, including immunology, oncology, cardiology, diabetologyCelebra , an anti-inflammatory drug.Pfizer was founded by cousins Charles Pfizer and Charles F. Erhart in New York City in 1849 as a manufacturer of fine chemicals. Pfizer's discovery of Terramycin in 1950 put it on a path towards becoming a research-based pharmaceutical company. Pfizer has made numerous acquisitions, including Warner–Lambert in 2000, Pharmacia in 2003 and Wyeth in 2009. The Wyeth acquisition was the largest of the three at US$68 billion. Pfizer is listed on the New York Stock Exchange, and its shares have been a component of the Dow Jones Industrial Average since April 2004.In September 2009, Pfizer pleaded guilty to the illegal marketing of the arthritis drug Bextra for uses unapproved by the U.S. Food and Drug Administration , and agreed to a $2.3 billion settlement, the largest health care fraud settlement at that time. Pfizer also paid the U.S. government $1.3 billion in criminal fines related to the "off-label" marketing of Bextra, the largest monetary penalty ever rendered for any crime. Called a repeat offender by prosecutors, this was Pfizer's fourth such settlement with the U.S. Department of Justice in the previous ten years. Wikipedia.

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The present disclosure generally relates to nanoparticles comprising an endo-lysosomal escape agent, a nucleic acid, and a polymer. Other aspects include methods of making and using such nanoparticles.

Pfizer | Date: 2016-11-03

A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A and A are independently C or N, where C may be unsubstituted or substituted by halo or C_(1)-C_(6 )alkyl; R and R^(0 )are independently selected from the group consisting of H, C_(1)-C_(6 )alkyl, hydroxy(C_(1)-C_(6 )alkyl), phenyl(C_(1)-C_(6 )alkyl), and (CH_(2))_(n)W, where W is C_(3)-C_(8 )cycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1-3 N, S and/or O atoms, SO_(2)R, NHSO_(2)R, NRSO_(2)R and SR, where R and R are independently C_(1)-C_(6 )alkyl or C_(3)-C_(8 )cycloalkyl, etc.; wherein each of said alkyl, cycloalkyl, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, heteroaryl, etc.; or, R and R^(0 )and the N atom to which they are bonded together form a monocyclic or bicyclic heterocyclic ring which may be unsubstituted or substituted by (a) halo, hydroxy, heteroaryl, C_(1)-C_(6 )alkyl, C_(1)-C_(6 )alkoxy, etc., or (b) (CH_(2))_(n)W, where W is C_(3)-C_(8 )cycloalkyl, phenyl, etc.; R^(1 )is H, halo or cyano; R^(2 )and R^(2 )are independently H, C_(1)-C_(6 )alkyl, cyano, C_(1)-C_(6 )alkoxy, C_(1)-C_(6 )alkylthio, or C_(3)-C_(8 )cycloalkyl where alkyl, alkoxy, or cycloalkyl is optionally substituted by one or more fluorine atoms; X is a bond, CO, CONH, SO_(2), SONH, or (CH_(2))_(m); R^(3 )is H, C_(1)-C_(4 )alkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1-3 N atoms, a 5-membered heteroaryl or heterocyclic, etc., or (c) 2 O or S atoms and 0-2 N atoms; wherein each of said phenyl, naphthyl, heteroaryl or heterocyclic is optionally substituted by alkyl, 1 substituent YR^(4 )and/or 1-4 substituents each independently selected from R^(5); with the proviso that when X is CO or SO_(2), R^(3 )is not H; Y is a bond, (CH_(2))_(m) or O; R^(4 )is (a) H, C_(1)-C_(6 )alkyl, C_(3)-C_(8 )cycloalkyl, halo, oxo, OR^(6), NR^(7)R^(8), SR^(6), SOR^(9), SO_(2)R^(9), COR^(6), OCOR^(6), COOR^(6), NR^(6)COR^(6), CONR^(7)R^(8), etc.; (b) phenyl or naphthyl, said phenyl and naphthyl being optionally substituted with 1-5 substituents selected from C_(1)-C_(6 )alkyl, C_(3)-C_(8 )cycloalkyl, halo, cyano, OR^(6), NR^(7)R^(8), etc.; or (c) a 3 to 8-membered saturated or partially unsaturated monocyclic heteroaryl, etc.; R^(6 )is H, C_(1)-C_(6 )alkyl or C_(3)-C_(8 )cycloalkyl, etc.; R^(7 )and R^(8 )are each independently H, C_(1)-C_(6 )alkyl or C_(3)-C_(8 )cycloalkyl or are taken together with the nitrogen atom to which they are attached to form a 4-, 5- or 6-membered saturated heterocyclic ring containing 1-2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, said C_(1)-C_(6 )alkyl is optionally substituted by C_(3)-C_(8 )cycloalkyl, halo, etc., and said heterocyclic ring being optionally substituted by one or more C_(1)-C_(6 )alkyl or C_(3)-C_(8 )cycloalkyl groups; R^(9 )is C_(1)-C_(6 )alkyl or C_(3)-C_(8 )cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.

The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 0.1 to about 50 weight percent of a corticosteroid; and about 50 to about 99 weight percent biocompatible polymer.

Pfizer and Stemcentrx Inc. | Date: 2016-06-08

The present invention provides for anti-EFNA4 antibody-drug conjugates and methods for preparing and using the same.

The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R^(1), R^(1a), R^(1b), R^(2), R^(4), R^(5), R^(6), X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinsons disease or Alzheimers disease, cancer, Crohns disease or leprosy.

Pfizer and Amgen Inc. | Date: 2016-03-31

The present invention relates to antibodies including human antibodies and antigen-binding portions thereof that specifically bind to MAdCAM, preferably human MAdCAM and that function to inhibit MAdCAM. The invention also relates to human anti-MAdCAM antibodies and antigen-binding portions thereof. The invention also relates to antibodies that are chimeric, bispecific, derivatized, single chain antibodies or portions of fusion proteins. The invention also relates to isolated heavy and light chain immunoglobulins derived from human anti-MAdCAM antibodies and nucleic acid molecules encoding such immunoglobulins. The present invention also relates to methods of making human anti-MAdCAM antibodies, compositions comprising these antibodies and methods of using the antibodies and compositions for diagnosis and treatment. The invention also provides gene therapy methods using nucleic acid molecules encoding the heavy and/or light immunoglobulin molecules that comprise the human anti-MAdCAM antibodies. The invention also relates to transgenic animals or plants comprising nucleic acid molecules of the invention.

The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyf}-1,3,4,5-tetrahydro-6H-azepino(5,4,3-cd]indol-6-one;(I), and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.

A procedure to isolate large quantities of capsular polysaccharides (CPS) from culture supernatants as well as bacterial cells of gram-negative arid gram-positive bacteria using base extraction is described. The procedure is simple, rapid, reproducible and applicable to a variety of bacterial species. The method also yields novel CPS characterized by their lack of covalent attachment to extraneous peptidoglycan. Vaccines and methods of immunization against bacterial infection using the CPS obtained by the process of the invention are also disclosed.

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, y and z are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. These compounds are -secretase modulators, useful for the treatment of neurodegenerative and/ or neurological disorders such as Alzheimers disease and Downs syndrome.

Dunn P.J.,Pfizer
Chemical Society Reviews | Year: 2012

Green Chemistry or Sustainable Chemistry is defined by the Environmental Protection Agency as "the design of chemical products that reduce or eliminate the use of hazardous substances" In recent years there is a greater societal expectation that chemists and chemical engineers should produce greener and more sustainable chemical processes and it is likely that this trend will continue to grow over the next few decades. This tutorial review gives information on solvents and solvent selection, basic environmental metrics collection and three industrial case histories. All three case histories involve enzymatic chemistry. Pregabalin (Lyrica®) is produced using a lipase based resolution and is extremely unusual in that all four manufacturing steps to make pregabalin are performed in water. Sitagliptin (Januvia®) uses a transaminase in the final chemical step. Finally a rosuvastatin (Crestor®) intermediate is produced using a deoxy ribose aldolase (DERA) enzyme in which two carbon-carbon bonds and two chiral centres are formed in the same process step. © 2012 The Royal Society of Chemistry.

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