Abstract: This invention relates to a novel salt form of dopamine agonist 5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine (I): More particularly, this invention relates to 5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine di-(1S)-camphorsulfonate (di-S-camsylate) and to processes for the preparation of, intermediates used in the preparation of, compositions containing, and the uses of this salt.
Type:
Grant
Filed:
February 6, 2006
Date of Patent:
March 3, 2009
Assignee:
Pfizer Inc.
Inventors:
Stuart Peter Green, Olivier Alain Lazzari, Duncan Charles Miller, Fabrice Henri Salingue
Abstract: The present invention relates to antibodies including human antibodies and antigen-binding portions thereof that specifically bind to c-Met, preferably human c-Met, and that function to inhibit c-Met. The invention also relates to human anti-c-Met 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-c-Met antibodies and nucleic acid molecules encoding such immunoglobulins. The present invention also relates to methods of making human anti-c-Met 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-c-Met antibodies.
Type:
Grant
Filed:
August 3, 2004
Date of Patent:
March 3, 2009
Assignees:
Amgen Fremont Inc., Pfizer Inc,
Inventors:
Neil R. Michaud, Shama Kajiji, Gary Borzillo, Vahe Bedian, Kevin Coleman, Larry L. Green, Xiao-Chi Jia
Abstract: The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid compound of this invention as an effective ingredient in an antiparasitic formulation. More particularly, the present invention relates to derivatives of the terpene alkaloid (1S,2R,4aS,5R,8R,8aR)-2-(acetyloxy)-8a-hydroxy-3,8-dimethyl-5-(1-methylethenyl)-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl (2S,3aR,9bR)-6-chloro-9b-hydroxy-5-methyl-1,2,3,3a,5,9b-hexahydropyrrolo[2,3-c][2,1]benzoxazine-2-carboxylate. Pharmaceutical compositions comprising the same are also disclosed.
Type:
Grant
Filed:
February 12, 2004
Date of Patent:
February 24, 2009
Assignee:
Pfizer Inc.
Inventors:
Nathan A. Chubb, Douglas J. Critcher, James J. Eshelby, Graham Lunn, Andrew J. Rudge, Nigel D. Walshe, Paul H Wiedenau, David H. Williams
Abstract: The present invention relates to compounds of the formula (I): and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
Type:
Application
Filed:
May 2, 2008
Publication date:
February 19, 2009
Applicant:
Pfizer, Inc.
Inventors:
Sharanjeet Kaur Bagal, Karl Richard Gibson, Mark Ian Kemp, Cedric Poinsard, Blanda Luzia Christa Stammen, Stephen Martin Denton, Melanie Susanne Glossop
Abstract: The invention relates to salts and free base forms of N,2-dimethyl-6-[7-(2-morpholinoethoxy)quinolin-4-yloxy]benzofuran-3-carboxamide. The invention further relates to pharmaceutical compositions of these salts and free base forms and methods of treating disorders such as cancer using such compositions.
Type:
Application
Filed:
July 27, 2006
Publication date:
February 19, 2009
Applicant:
PFIZER INC.
Inventors:
Yi Li, Jia Liu, Anand Sistla, Bruce Joseph Elder, Yufeng Hong, Paul Kenneth Isbester, Grant Jackson Palmer, Jonathon Stuart Salsbury, Luckner Gerard Ulysse
Abstract: This invention relates to prodrugs of certain amino acids that bind to the alpha-2-delta (?2?) subunit of a calcium channel. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders.
Type:
Grant
Filed:
September 21, 2004
Date of Patent:
February 17, 2009
Assignee:
Pfizer Inc
Inventors:
Sean D. Donevan, Augustine Tobi Osuma, Andrew J. Thorpe, David Juergen Wustrow
Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
Abstract: The present invention provides for compounds of Formula I: wherein R2, R3, R4, R5, R6, R7, X, and L have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of central nervous disorders and conditions including attention deficit hyperactivity disorder, neuropathic pain, urinary incontinence, anxiety, depression, and schizophrenia and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
Abstract: Bicyclo-pyrazoles of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.
Type:
Grant
Filed:
June 18, 2007
Date of Patent:
February 3, 2009
Assignee:
Pfizer, Inc.
Inventors:
David W. Piotrowski, Yu Hui, John W. Benbow
Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii)one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating e
Type:
Grant
Filed:
April 18, 2006
Date of Patent:
January 27, 2009
Assignee:
Pfizer Inc.
Inventors:
Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
Abstract: A palatable chewable tablet is described herein for oral administration of cetirizine dihydrochloride. The formulation is made more palatable by incorporating a combination of a grape flavoring agent with a vanilla flavoring agent.
Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
March 10, 2005
Date of Patent:
January 27, 2009
Assignee:
Pfizer Inc
Inventors:
Alan Daniel Brown, Justin Stephen Bryans, Paul Alan Glossop, Charlotte Alice Louise Lane, Simmon John Mantell
Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
Type:
Grant
Filed:
August 2, 2005
Date of Patent:
January 27, 2009
Assignee:
Pfizer Inc
Inventors:
Peter Bertinato, Brian Bronk, Alan E. Blize, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
Abstract: The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
Type:
Grant
Filed:
March 17, 2005
Date of Patent:
January 20, 2009
Assignee:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Stephane Caron, Christopher John Helal, Jeffrey W. Raggon, Yong Tao, Nga M. Do
Abstract: The invention concerns the use of essential fatty acids with a high content in eicosapentaenoic acid ethyl ester (EPA) or docosahexaenoic acid ethyl ester (DHA) or a high concentration mixture thereof in the preparation of a medicament useful for preventing mortality, in particular due to sudden death, in patients who have suffered from a myocardial infarction.
Abstract: Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory compound of low water solubility in a therapeutically effective amount, wherein the compound is present in the form of solid particles, about 25% to 100% by weight of which are smaller than 1 micrometer. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders and have particular advantages where rapid onset of therapeutic effect is desired. The novel Form I and Form II crystalline forms of celecoxib are described. The crystalline forms have unique chemical and physical properties relative to other solid state forms of celecoxib and are characterized by their powder x-ray diffraction (PXRD) patterns, differential scanning calorimetric (DSC) thermograms, and other physical characterizations.
Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
Type:
Grant
Filed:
May 8, 2006
Date of Patent:
January 6, 2009
Assignee:
Pfizer Inc.
Inventors:
Allen Borchardt, Javier Gonzalez, Hui Li, Maria Angelica Linton, John Howard Tatlock
Abstract: The present invention relates to a series of substituted bicyclic[3.1.0]amines of the Formula I: wherein A, B, D, Q, V, W, X, Y, Z, R2, R3, R4, R5, R14, R15, R30. o, p, s,t and q are as defined in the specification, their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.
Abstract: The present invention is directed to a class of 4-cyano-phenoxy derivatives of formula I and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.
Type:
Grant
Filed:
April 15, 2005
Date of Patent:
January 6, 2009
Assignee:
Pfizer Inc.
Inventors:
Lain-Yen Hu, Huangshu Lei, Daniel Y. Du, Bruce A. Lefker