Abstract: 4-aminoquinazoline derivatives which are selective inhibitors of cGMP PDE are useful in the treatment of erectile dysfunction (impotence) in male animals, including man.
Type:
Grant
Filed:
May 22, 1997
Date of Patent:
October 9, 2001
Assignee:
Pfizer Inc.
Inventors:
Simon Fraser Campbell, Alexander Roderick Mackenzie, Anthony Wood
Abstract: Compounds of the formulae (IA) and (IB):
wherein R1 is C1 to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from C1 to C4 alkoxy; halo; CN; CF3; OCF3 or C1 to C4 alkyl wherein said C1 to C4 alkyl group is optionally substituted by C1 to C4 haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2 is C1 to C6 alkyl and R13 is OR3 or NR5R6, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).
Type:
Grant
Filed:
September 29, 1999
Date of Patent:
June 26, 2001
Assignee:
Pfizer Inc.
Inventors:
Mark Edward Bunnage, John Paul Mathias, Stephen Derek Albert Street, Anthony Wood
Abstract: Methods of treating congestive heart failure in a mammal, especially a human, by co-administration of (1) amlodipine, a pharmaceutically acceptable salt of amlodipine; (2) an ACE inhibitor; and optionally (3) a diuretic and/or (4) digoxin.
Abstract: Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex or an aqueous solution. The salt/cyclodextrin inclusion complex preferably provides an amount of ziprasidone of at least 2.5 mgA/ml when the complex is dissolved in water at 40% w/v. A variety of ziprasidone salts are preferred, including the mesylate, esylate, besylate, tartrate, napsylate, and tosylate.
Type:
Grant
Filed:
November 5, 1998
Date of Patent:
May 15, 2001
Assignee:
Pfizer Inc.
Inventors:
Yesook Kim, Kevin C. Johnson, Ravi M. Shanker
Abstract: A dosage form containing cetirizine as an immediate release component and pseudoephedrine or a pharmaceutically acceptable salt thereof as a controlled release component. A portion of the pseudoephedrine can also be incorporated as an immediate release component. The dosage form is free of alcohols having a molecular weight lower than 100 and reactive derivatives thereof.
Type:
Grant
Filed:
May 28, 1997
Date of Patent:
January 9, 2001
Assignee:
Pfizer Inc.
Inventors:
Barbara A. Johnson, Richard W. Korsmeyer, Cynthia A. Oksanen
Abstract: The present invention provides an aqueous pharmaceutical composition comprising 5 to 200 mg/ml of eletriptan hemisulfate and from 0.5 to 2.0% weight/volume of caffeine.
Abstract: Sulfoalkyl ether cyclodextrins are produced by a process of treating an unsubstituted cyclodextrin starting material with an alkyl sultone in the presence of a base. The base is added in a stepwise, pH controlled manner so that substantially the entire initial charge of cyclodextrin starting material is at least partially reacted. Additional base is then added to complete the reaction, and residual alkyl suftone is destroyed. The product advantageously contains low levels of both residual cyclodextrin and residual alkyl sultone.
Abstract: Compositions comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size less than 85 .mu.m, and a pharmaceutically acceptable carrier, are substantially bioequivalent and can be used to treat psychoses such as schizophrenia.
Type:
Grant
Filed:
May 27, 1999
Date of Patent:
November 21, 2000
Assignee:
Pfizer Inc.
Inventors:
Daniel R. Arenson, Frank Robert Busch, Angela G. Hausberger, Bijan Rasadi
Abstract: There is provided a pharmaceutical dosage form adapted for administration to the gastrointestinal tract of a patient, comprising darifenacin, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable adjuvant, diluent or carrier, characterized in that the dosage form is adapted to deliver at least 10% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, to the lower gastrointestinal tract of the patient. The formulation minimizes unwanted side-effects and increases the bioavailability of darifenacin.
Type:
Grant
Filed:
March 3, 1998
Date of Patent:
August 22, 2000
Assignee:
Pfizer Inc.
Inventors:
Thomas Francis Dolan, Michael John Humphrey, Donald John Nichols
Abstract: The R(+) isomer of amlodipine is a potent inhibitor of smooth muscle cell migration despite its lack of calcium channel-blocking activity. It is useful for treating atherosclerosis, re-stenosis after angioplasty and endometriosis.
Type:
Grant
Filed:
February 21, 1996
Date of Patent:
June 27, 2000
Assignee:
Pfizer Inc.
Inventors:
Suresh Bababhai Chahwala, Derek Paul Winslow
Abstract: A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein X, O R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the specification; compositions containing such compounds; intermediates used in the preparation of such compounds; and methods for treating a disease associated with the altered tone and/or motility of smooth muscle, for example chronic obstructive airways disease, asthma, urinary incontinence, irritable bowel syndrome, diverticular disease, oesophageal achalasia, and hypertension.
Type:
Grant
Filed:
April 9, 1999
Date of Patent:
June 6, 2000
Assignee:
Pfizer Inc.
Inventors:
Alexander Roderick MacKenzie, Sandra Marina Monaghan
Abstract: A controlled-release dosage form of azithromycin having an improved side effect profile; a process for preparing the dosage form; and a method of treating a microbial infection, comprising administering azithromycin in such a controlled-release dosage form to a mammal, including a human patient, in need of such treatment.
Type:
Grant
Filed:
November 4, 1996
Date of Patent:
May 30, 2000
Assignee:
Pfizer Inc.
Inventors:
William J. Curatolo, Hylar L. Friedman, Richard W. Korsmeyer, Steven R. LeMott
Abstract: A method for the separation of R-(+)- and S-(-)-isomers of amlodipine (I) from mixtures thereof, which comprises the reaction of the mixture of isomers with either L- or D-tartaric acid in an organic solvent containing sufficient dimethyl sulphoxide (DMSO) for the precipitation of, respectively, a DMSO, solvate of an L-tartate salt of R-(+)-amlodipine, or a DMSO solvate of a D-tartrate salt of S-(-)-amlodipine.
Abstract: .beta.-adrenergic agonists for the treatment of diseases/conditions such as obesity and diabetes. The compounds have formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, W, X, Y and Z are as defined in the specification.
Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.
Type:
Grant
Filed:
December 10, 1997
Date of Patent:
September 14, 1999
Assignee:
Pfizer Inc.
Inventors:
James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof,wherein Y is a direct link, --(CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O-- or CH.sub.2 S--; R is --CN or --CONH.sub.2 ;and R.sup.1 is a group of the formula: ##STR1## where R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.n OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.n NR.sup.4 R.sup.5, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), --CH(OH) (C.sub.1 -C.sub.4 alkyl), --C(OH) (C.sub.1 -C.sub.4 alkyl).sub.2, --SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n CONR.sup.4 R.sup.5 or --(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4 alkyl; R.sub.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2;and "Het" is pyridyl, pyrazinyl or thienyl.The compounds are muscarinic receptor antagonists usedful in the treatment of diseases associated with the altered motility and/or tone of smooth muscle, especially irritable bowel syndrome.
Type:
Grant
Filed:
April 24, 1995
Date of Patent:
August 3, 1999
Assignee:
Pfizer, Inc.
Inventors:
Peter Edward Cross, Alexander Roderick MacKenzie