Abstract: The present invention relates to the use of certain NK-1 receptor antagonists (e.g., substance P receptor antagonists) to treat cancer patients, particularly cancer patients afflicted with a small cell lung carcinoma, APUDoma, astrocytoma, neuroendocrine tumor or extrapulmonary small cell carcinoma.
Abstract: This invention relates to a method for evaluating the susceptibility of pharmaceutical drugs to metabolism by a specific cytochrome P-450 isozyme, which comprises contacting the sample compound with a reagent composition prepared by adding the specific cytochrome P-450 isozyme to liver microsomes lacking said specific cytochrome P-450 isozyme in a carrier material. More particularly, this invention relates to a useful in vitro quantitative assay for drug metabolism by P-450 isozymes such as CYP2D6, CYP2C19, and CYP2A6. This invention also relates to a reagent composition which is useful for said in vitro assay.
Abstract: This invention relates to the use of aldose reductase inhibitors in the treatment, prevention or reversal of diabetic cardiomyopathy in a human subject.
Abstract: The present invention provides novel methods of inhibition of autoimmune diseases comprising administering to a mammal in need of treatment an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different provided that, when R.sup.1 and R.sup.2 are the same, each is a methyl or ethyl group, and, when R.sup.1 and R.sup.2 are different, one of them is a methyl or ethyl group and the other is hydrogen or a benzyl group; or a pharmaceutically acceptable salt thereof.
Abstract: A 5-oximino-25-substituted avermectin B1 or B2 monosaccharide of formula I herein has use in the treatment of parasitic infections in animals and humans. The compounds may be prepared from corresponding 5-keto substituted derivatives.
Type:
Grant
Filed:
May 9, 1997
Date of Patent:
November 9, 1999
Assignee:
Pfizer Inc.
Inventors:
Bernard Frank Bishop, Michael Stephen Pacey, David Austen Perry
Abstract: An antifungal compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of either entity, wherein X is CH or N; R.sup.1 is phenyl substituted with 1 to 3 substituents each independently selected from halo and CF.sub.3 ; R.sup.2 is (hydroxy)C.sub.1 -C.sub.4 alkyl, CONH.sub.2, S(O).sub.m (C.sub.1 -C.sub.4 alkyl), Ar or Het; m is 1 or 2; Ar is phenyl optionally monosubstituted with halo or CF.sub.3 ; and Het is a C-linked 6-membered nitrogen-containing aromatic heterocyclic group containing 1 or 2 nitrogen atoms, or a C- or N-linked 5-membered nitrogen-containing aromatic heterocyclic group containing from 2 to 4 nitrogen atoms, wherein either of said heterocyclic groups is optionally substituted with C.sub.1 -C.sub.4 alkyl or (C.sub.1 -C.sub.4 alkoxy)methyl.
Type:
Grant
Filed:
March 18, 1997
Date of Patent:
November 9, 1999
Assignee:
Pfizer Inc.
Inventors:
Andrew Simon Bell, Peter Thomas Stephenson
Abstract: A process for the preparation of CCK antagonists of the formula ##STR1## wherein X, Y.sup.1 and Y.sup.2 are defined above and to novel intermediates used in the process.
Abstract: A compound of formula (I) ##STR1## wherein R.sup.1 is C.sub.1-6 alkyl, halo-(C.sub.1-6 alkyl), C.sub.3-7 cycloalkyl, C.sub.2-6 alkylnyl, hydroxy-(C.sub.2-6 alkylnyl), (C.sub.1-4 alkoxy)-(C.sub.2-6 alkylnyl), aryl, aryl-(C.sub.1-4 alkyl), heteroaryl or heteroaryl-(C.sub.1-4 alkyl); R.sup.2 is H or C.sub.1-4 alkyl; R.sup.3 is aryl, heteroaryl, 2,3-dihydrobenzofuranyl or C.sub.4-7 cycloalkyl; X is O or S; Y is bond, --CH.sub.2 --, --(CH.sub.2).sub.2 -- or --CH.sub.2 O--, a pharmaceutically acceptable salt thereof, which are useful muscarinic receptor antagonists in treaatment of e.g. irritable bowel syndrome, urinary incontinence, etc.
Type:
Grant
Filed:
July 31, 1998
Date of Patent:
November 2, 1999
Assignee:
Pfizer Inc.
Inventors:
Robert John Bass, Alexander Roderick MacKenzie, Anthony Wood
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: This invention provides a compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein Ar.sup.1 is selected from groups of the following formulae: ##STR2## wherein, R.sup.1 and R.sup.2 are independently hydrogen or C.sub.1 -C.sub.6 alkyl;W is (CH.sub.2).sub.n wherein n is from 1 to 3, or --CH.dbd.CH--;X is C.sub.1 -C.sub.6 alkoxy or halo C.sub.1 -C.sub.6 alkoxy; andAr.sup.2 is phenyl optionally substituted by halogen atom.These compounds are useful in the treatment of a gastrointestinal disorder, a central nervous system (CNS) disorder, an inflammatory disease, emesis, urinary incontinence, pain, migraine, sunburn, angiogenesis, diseases, disorders and adverse conditions caused by Helicobacter pylori, or the like in a mammalian subject, especially humans.
Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, COOH, --COO(C.sub.1 -C.sub.4 alkyl), C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro (C.sub.1 -C.sub.4) alkyl and fluoro (C.sub.1 -C.sub.4) Alkoxy; R.sub.1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo and trifluormethyl; R.sup.2 is --CO.sub.2 H, --CONR.sup.3 R.sup.4, --CONR.sup.5 (C.sub.3 -C.sub.7 cycloalkyl), --NR.sup.5 (C.sub.2 -C.sub.5 alkanoyl), --NR.sup.
Type:
Grant
Filed:
February 10, 1997
Date of Patent:
October 19, 1999
Assignee:
Pfizer Inc.
Inventors:
Alexander Roderick MacKenzie, Allan Patrick Marchington, Sandra Dora Meadows, Donald Stuart Middleton
Abstract: Calcium, magnesium, lidocaine and benzathine salts of 2-oxindole-1-carboxamides are useful for the treatment of joint disease by intra-articular administration.
Abstract: The compounds of the formula wherein A, R.sub.1, R.sub.3, X.sub.1, Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.
Abstract: Apparatus for spectrophotometric analysis of material in vials 16 in which material in each vial is subjected to a beam 4 at a scanning station 20. An array of the vials 16 is carried by a carousel 60 for each vial 16 automatically and sequentially to be delivered to the scanning station and thereafter removed following scanning by the beam 4. Rotation of the carousel 60 to feed the vials to the scanning station and to remove them from that station is controlled by a computer 3 which also controls spectrophotometric measurement of the material in the respective vials whilst at the scanning station.
Abstract: A hydrochloride salt of an Apo B secretion/MTP inhibitor, methods of making the salt, methods of using the salt and pharmaceutical compositions containing the salt are disclosed.
Type:
Grant
Filed:
March 2, 1998
Date of Patent:
October 19, 1999
Assignee:
Pfizer Inc
Inventors:
George J. Quallich, George Chang, Lewin T. Wint