Abstract: The present invention relates to compounds of formula 1
and to pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein n is 0 or 1 and R1, R2, R3, R4, and R5 are as defined herein. The above compounds of formula 1 are useful in the treatment of hyperproliferative disorders, such as cancer, in mammals. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of formula 1 to a mammal requiring such treatment, and to methods of preparing compounds of formula 1.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
July 1, 2003
Assignee:
Pfizer Inc
Inventors:
Joseph Peter Lyssikatos, Bingwei Vera Yang
Abstract: The present invention relates to compounds of the formula I,
wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.
Type:
Grant
Filed:
May 31, 2000
Date of Patent:
July 1, 2003
Assignee:
Pfizer Inc
Inventors:
Spiros Liras, Martin P. Allen, Barbara E. Segelstein
Abstract: There is provided compounds of formula IA and of formula IB,
wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
Abstract: Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
Type:
Grant
Filed:
October 10, 2000
Date of Patent:
July 1, 2003
Assignee:
Pfizer Inc.
Inventors:
Michael P. DeNinno, George T. Magnus-Aryitey, Roger B. Ruggeri, Ronald T. Wester
Abstract: Novel crystalline forms of a compound of Formula 1 are disclosed:
Also disclosed are pharmaceutical compositions comprising these forms, and methods of their preparation and use.
Type:
Grant
Filed:
May 2, 2000
Date of Patent:
June 24, 2003
Assignee:
Pfizer Inc.
Inventors:
Douglas J. M. Allen, Barry J. Morton, Robert J. Rafka, Colman B. Ragan
Abstract: The present invention relates to compounds of formula 1
and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are as defined herein. The above compounds of formula 1 are useful in the treatment of hyperproliferative disorders, such as cancer, in mammals.
Type:
Grant
Filed:
July 6, 2001
Date of Patent:
June 17, 2003
Assignee:
Pfizer Inc
Inventors:
Joseph P. Lyssikatos, Susan D. La Greca
Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula
wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.
Abstract: The present invention relates to compounds of formula I
and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R1, R2, R3, R4, R5, R10, R11, b, m, n, p and v are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and methods of treating hyperproliferative disorders in mammals by administering the above compounds.
Type:
Grant
Filed:
April 13, 2000
Date of Patent:
June 10, 2003
Assignee:
Pfizer Inc
Inventors:
Steven W. Goldstein, Kelly P. Longo, James F. Blake, Mohamed M. A. Awad, Kenneth P. Raiche, Kevin W. Kramer
Abstract: This invention relates to compounds of Formula I
or stereoisomers, pharmaceutically acceptable salts or prodrugs thereof or a pharmaceutically acceptable salts of the prodrugs. This invention also relates to pharmaceutical compositions comprising a compound of Formula I, and to methods of treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, or tissue ischemia.
Abstract: This invention relates to methods for preparing anhydrous CETP inhibitor, (2R,4S)-4-[(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester.
Abstract: Compounds of formulae (IA) and (IB):
wherein R1, R2, R3, Ar1 and X are as defined above, are endothelin antagonists. The compounds are therefore useful in the treatment of a variety of conditions mediated by endothelin, such as restenosis, renal failure and systemic and pulmonary hypertension.
Type:
Grant
Filed:
August 21, 2001
Date of Patent:
June 3, 2003
Assignee:
Pfizer Inc.
Inventors:
Bernard Joseph Banks, Nathan Anthony Logan Chubb, James John Eshelby, Darren John Schulz
Abstract: The present invention relates to method for the preparation of dialkylpyridylboranes by reacting a pyridine Grignard reagent with an alkoxydialkylborane or a trialkylborane. The reaction can be conducted at a temperature ranging from about 0° C. to about 40° C. The pyridine Grignard reagent is preferably prepared in situ by the reaction of a Grignard reagent (RMgX) and a halopyridine in a suitable solvent, such as tetrahydrofuran, followed by the addition of an alkoxydialkylborane or a trialkylborane to form a dialkylpyridylborane.
Abstract: A shaving preparation that undergoes a change discernible to the user when the hair to be shaved has had time to absorb water and soften, when the shaving preparation has been sufficiently hydrated, after a period of time in which proper hair hydration would normally be expected to have been achieved, or any combinations thereof. Shaving preparations of this type advantageously alert the user when at least one desired shaving condition exists.
Abstract: This invention relates to [4-oxo-(5-trifluoromethyl-benzothiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid ethanolamine salt, pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to said mammals said salt and said compositions. This invention is also directed to combinations of said diethylamine salt with NHE-1 inhibitors, selective serotonin retuptake inhibitors (SSRIs), glycogen phosphorylase inhibitors (GPIs), sorbitol dehydrogenase inhibitors (SDIs) and antihypertensive agents. Said combinations are useful in treating diabetic complications in mammals.
Abstract: The present invention is directed to a novel process for the preparation of the mesylate trihydrate of the compound of formula (I), (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol:
The present invention is further directed to a process for the preparation of a (2S)-(+)-compound of formula (II):
wherein R1 is a protecting group. In addition, the present invention relates to intermediates useful in said processes.
Type:
Grant
Filed:
April 23, 2001
Date of Patent:
May 27, 2003
Assignee:
Pfizer Inc
Inventors:
Stanley Walter Walinsky, Terry Gene Sinay, Jr., Joseph Philip Rainville
Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I),
the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.
Abstract: This invention relates to a series of substituted aromatic ethers of the formula I
wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, 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 relates to compounds of the formula 1
and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X, Y, V, W1, W2, Z1 and Z2 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods of treating bacterial and protozoal infections in mammals by administering the above compounds.
Type:
Grant
Filed:
October 20, 2000
Date of Patent:
May 13, 2003
Assignee:
Pfizer Inc.
Inventors:
Katherine E. Brighty, Robert G. Linde, Takushi Kaneko, Matthew M. Hayward