Abstract: A compound of the formula:
and its pharmaceutically effective salts, wherein R1 and R2 are independently selected from the following:
(a) hydrogen, halo, R5—, C2-6 alkenyl, C2-6 alkynyl, hydroxy-R5—, R5—O—R5—, or the like; (b) Ar—, Ar—R5—, Ar—C2-6 alkenyl, Ar—C2-6 alkynyl, Ar—O—, Ar—O—R5— or the like; (c) R5—C(O)—, —NO2, cyano, NH2—C(O)—, R5—NH—C(O)—, (R5)2—N—C(O)—, Ar—C(O)— or the like; and (d) R5—C(O)—NH—, Ar—C(O)—NH— or the like; wherein Ar is optionally substituted aryl or heteroaryl such as phenyl and pyridyl; and wherein R5 is optionally halo-substituted C1-6 alkyl; R3 is selected from the following: (e) cyano, formyl, tetrazolyl, triazolyl, imidazolyl, oxazolyl, thiazolyl, R5—C(O)—, C2-6 alkenyl-C(O)—, C2-6 alkynyl-C(O)—, R5—C(O)—R5—, or the
Abstract: A compound of the formula
wherein R1, R2 and R3 are as defined above, useful as inhibitors of protein kinases, such as the enzyme Janus Kinase 3.
Type:
Grant
Filed:
June 25, 2001
Date of Patent:
February 24, 2004
Assignee:
Pfizer Inc.
Inventors:
Todd A. Blumenkopf, Mark E. Flanagan, Michael J. Munchhof
Abstract: The instant invention provides novel processes and intermediates useful in the preparation of certain N-(indole-2-carbonyl)-&bgr;-alaninamide compounds, which compounds are glycogen phosphorylase inhibitors useful in the treatment of diseases such as hypercholesterolemia, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis, diabetes, diabetic cardiomyopathy, infection, tissue ischemia, myocardial ischemia, and in inhibiting tumor growth.
Type:
Grant
Filed:
January 16, 2003
Date of Patent:
February 24, 2004
Assignee:
Pfizer Inc.
Inventors:
Mark T. Barrila, Frank R. Busch, Michel A. Couturier, Susan L. Orrill, Peter R. Rose, Derek L. Tickner, Harry O. Tobiassen, Gregory J. Withbroe
Abstract: Compounds of formula I:
wherein X, Y, B, E, J, K, L, Z, and R9-R12 have any of the meanings described herein, their pharmaceutically acceptable salts, lower blood glucose levels and are useful for treating diseases in mammals such as Non-Insulin Dependent Diabetes Mellitus. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula (I) and intermediates useful for preparing compounds of formula I.
Abstract: Compounds according to the formula:
and pharmaceutically acceptable salts, solvates or hydrates thereof; wherein group Ar is optionally substituted (C6-C10)aryl or (C1-C9)heteroaryl; X is a direct link, —CH2—, —SO2—, —CO—, —CHR1— where R1 is (C1-C6) alkyl, or —CR1′R1″— where both R1′ and R1″ are, independently, (C1-C6)alkyl; Y is N or CH; and Z and W are as herein defined, and pharmaceutical compositions thereof, and methods useful to facilitate secretion of growth hormone(GH) in mammals.
Type:
Grant
Filed:
July 17, 2000
Date of Patent:
February 24, 2004
Assignee:
Pfizer Inc.
Inventors:
Bruce A. Hay, Anthony P. Ricketts, Bridget M. Cole
Abstract: The present invention relates to novel triazolo-pyridines of the formula I
wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen;
R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents;
R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents;
s is an integer from 0-5;
to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
Type:
Grant
Filed:
March 11, 2002
Date of Patent:
February 24, 2004
Assignee:
Pfizer Inc
Inventors:
Kim F. McClure, Michael A. Letavic, Mark A. Dombroski, Allen J. Duplantier, Ellen R. Laird
Abstract: The invention provides transgenic, non-human animals and transgenic non-human mammalian cells harboring a transgene encoding a p25 (activator of the protein kinase cdk 5) polypeptide. The two neuropathological lesions associated with Alzheimer's disease (AD) are amyloid plaques and neurofibrillary tangles (NFTs), composed predominantly of amyloid &bgr; peptides and hyperphosphorylated tau, respectvely. While animal models for plaque formation exist, there is no animal model that recapitulates the formation of NFTs. This invention provides transgenic mice that overexpress human p25, an activator of cdk5, resulting in tau that is hyperphosphorylated at AD-relevant epitopes. Deposition of tau is detected in the amygdala, thalamus and cortex. Increased phosphorylated neurofilament, silver-positive neurons and neuronal death are also observed in these regions. We conclude that the overexpression of p25, an activator of cdk5, is sufficient to produce hyperphosphorylation of tau and neuronal death.
Abstract: Pharmaceutical kits are provided that reduce or prevent oxidative degradation of oxygen-sensitive pharmaceutically active ingredients in solid unit dosage forms that are supplied in oxygen permeable containers. Stabilization of the active ingredient is accomplished by incorporating an oxygen absorber into a sealed oxygen permeable container.
Abstract: Method for the preparation of enantiomerically pure diazepino-indolone of formula
which comprises the intramolecular cyclization of a product of formula
where A, B, X1, X2, Z, Z1, Z2 and R are as defined in the description, in the presence of a weak Lewis acid catalyst.
Abstract: The present invention provides the tosylate salt of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol, the monohydrate of such salt, processes useful in the preparation of such salt and such monohydrate, pharmaceutical compositions comprising such salt, or such monohydrate, methods of treating &bgr;3-adrenergic receptor-mediated diseases, conditions, and disorders in a mammal using such salt, such monohydrate, or such pharmaceutical compositions; and methods of increasing the content of lean meat in edible animals using such salt, such monohydrate, or such pharmaceutical compositions.
Type:
Grant
Filed:
February 25, 2003
Date of Patent:
February 10, 2004
Assignee:
Pfizer Inc.
Inventors:
Joseph F. Krzyaniak, Jennifer A. Lafontaine
Abstract: A compound of the formula XXXI
or the pharmaceutically acceptable salt thereof; wherein R1, R2, and R3 are as defined herein and the compound is useful in the preparation or use of compounds that treat inflammation and other immune disorders.
Abstract: The present invention provides processes useful in the preparation of certain &bgr;3-adrenergic receptor agonists of the structural formula
the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.
Type:
Grant
Filed:
February 20, 2003
Date of Patent:
February 10, 2004
Assignee:
Pfizer Inc.
Inventors:
Robert J. Chambers, Robert W. Dugger, Ming Kang, Yong Tao, John W. Wong
Abstract: The present invention is directed to compositions and methods for producing avermectins, and is primarily in the field of animal health. The present invention relates to the identification and characterization of two novel genes, herein referred to as the aveR1 and aveR2 genes, that are involved in regulating avermectin polyketide synthase (PKS) expression and avermectin biosynthesis in Streptomyces avermitilis. The present invention is based on the discovery that inactivation of these genes results in an increase in the amount of avermectin produced by S. avermitilis.
Type:
Grant
Filed:
November 16, 2000
Date of Patent:
February 10, 2004
Assignee:
Pfizer Inc.
Inventors:
Kim J. Stutzman-Engwall, Brenda S. Price
Abstract: This invention relates to a process for preparing compounds of the Formula I,
wherein R1, R2 and Pt are as defined in the specification, which are intermediates in the synthesis of certain growth hormone secretagogue compounds. This invention further relates to processes for preparing the growth hormone secretagogues. The invention also relates to the compound of Formula I wherein R1 is H, R2 is 2,2,2-trifluoromethyl and Pt is Boc.
Abstract: This invention is directed to compounds of the formula
and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintanence of skin thickness, metabolic homeostasis or renal homeostasis.
Abstract: A process for the purification of 2-methoxy-5-trifluoro-methoxy benzaldehyde oil in which the oil is converted to amine by reaction of a nitroaniline with the oil; the imine is isolated as a solid; and the solid imine is converted back to the 2-methoxy-5-trifluoromethoxy benzaldehyde oil. The nitroaniline is selected from the group consisting of 3-nitroaniline, 3-methyl-2-nitroaniline, 4-methyl-2-nitroaniline, 2 methyl-3-nitroaniline and 4-methyl-3-nitroaniline.
Type:
Grant
Filed:
December 9, 2002
Date of Patent:
February 3, 2004
Assignee:
Pfizer Inc
Inventors:
Timothy J. N. Watson, Patrice Arpin, Michael G. Vetelino
Abstract: The instant invention provides crystal forms of 5-chloro-N-[(1S,2R)-3-[3R,4S]-3,4-dihydroxy-1-pyrrolidinyl]-2-hydroxy-3-oxo-1-(phenyl) methyl)propyl]-1H-indole-2-carboxamide (I)
processes for the production of such crystal forms; pharmaceutical compositions comprising such crystal forms; and methods of treating glycogen phosphorylase dependent diseases, or conditions with such crystal forms, or such pharmaceutical compositions.
Type:
Grant
Filed:
April 15, 2003
Date of Patent:
January 27, 2004
Assignee:
Pfizer Inc.
Inventors:
Douglas J. M. Allen, Frank R. Busch, Joseph F. Krzyzaniak, Zheng Jane Li, Susan L. Orrill, Peter R. Rose, Derek L. Tickner, Harry O. Tobiassen
Abstract: The present invention provides 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)quinazoline mesylate of the formula
together with processes for preparing, and compositions containing it.
The invention also relates to substantially pure anhydrous crystalline polymorphic forms of the free base.
The compounds are particularly useful in the treatment of benign prostatic hyperplasia.
Type:
Grant
Filed:
March 1, 2001
Date of Patent:
January 27, 2004
Assignee:
Pfizer Inc.
Inventors:
Patricia Ann Basford, Paul Blaise Hodgson