Abstract: A process for preparing phenoxyphenylsulfonyl halides, which are useful intermediates for the preparation of matrix metalloproteinase inhibitors.
Abstract: This invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LTB.sub.4 antagonists. The compounds of this invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.
Type:
Grant
Filed:
February 1, 1999
Date of Patent:
September 12, 2000
Assignee:
Pfizer Inc.
Inventors:
Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
Abstract: The present invention relates to a process for alkylating hindered sulfonamides useful as intermediates in the preparation of matrix metalloproteinase inhibitors.
Type:
Grant
Filed:
April 9, 1999
Date of Patent:
September 5, 2000
Assignee:
Pfizer Inc.
Inventors:
Brian Michael Andresen, Phillip Dietrich Hammen, Joel Michael Hawkins
Abstract: A method of treating atherosclerosis, independent of lipid lowering, in mammals, including humans, in need of treatment by inhibiting progression of an atherogenic lesion or by stabilizing plaque. Such lesion progression inhibition or plaque stabilization is achieved by directly inhibiting chemokine expression leading to excessive inflammatory cell recruitment by administering a therapeutically effective amount of a compound of formula I.
Abstract: The present invention is directed to a topical composition for the treatment of psoriasis. The composition comprises a film forming agent, a plasticizer, an aqueous alcoholic solution and an amount of alkali effective to prevent the gellation of the film forming agent.
Type:
Grant
Filed:
July 1, 1998
Date of Patent:
September 5, 2000
Assignee:
Pfizer Inc.
Inventors:
Debbie L. Burnett, Victor M. Wong, Darius D. Dubash, Athanasios S. Ladas
Abstract: Antibacterial quinolone carboxylic acids and naphthyridone carboxylic acids, having an external amino group attached to their 7-substituent are prepared without the use, and subsequent removal, of blocking groups on the external amino group. In a preferred embodiment, the naphthyridone carboxylic acid is the antibiotic trovafloxacin.
Abstract: The present invention relates to a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are as defined above, to pharmaceutical compositions and methods of treatment.
Abstract: This invention relates to isoxazoline compounds which are inhibitors of tumor necrosis factor (TNF). The isoxazoline compounds are useful for inhibiting TNF in a mammal in need thereof and in the treatment or alleviation of inflammatory conditions or disease, including but not limited to rheumatoid arthritis, osteoarthritis, asthma, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, dermatitis and inflammatory bowel disease, sepsis, septic shock, tuberculosis, graft versus host disease and cachexia associated with AIDS or cancer. This invention also relates to pharmaceutical compositions useful therefor comprising such compounds.
Type:
Grant
Filed:
November 6, 1998
Date of Patent:
September 5, 2000
Assignee:
Pfizer Inc
Inventors:
Victoria Lee Cohan, Edward Fox Kleinman
Abstract: Mesylate Trihydrate Salt of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydr o-2(1H)-indol-2-one (=Ziprasidone), Its Preparation and Its Use as Dopamine D2 AntagonistThe invention relates to the mesylate trihydrate salt of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydr o-2(1H)-indol-2-one ("ziprasidone mesylate trihydrate"), to pharmaceutical compositions containing ziprasidone mesylate trihydrate, and to methods of administering ziprasidone mesylate trihydrate to treat psychotic diseases.
Abstract: The present invention relates to hydrobromide salts of 3-(N-methyl-2(R)-pyrrolidinylmethyl)-5-(2-phenylsulphonylethyl)-1H-indole having the formula (I): ##STR1##
Type:
Grant
Filed:
February 2, 1997
Date of Patent:
August 29, 2000
Assignee:
Pfizer Inc.
Inventors:
Valerie Denise Harding, Ross James Macrae, Ronald James Ogilvie
Abstract: A compound of the formula: ##STR1## and it pharmaceutically acceptable salt, wherein A is hydrogen, hydroxy or OY, where Y is a hydroxy protecting group;Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, C.sub.1 -C.sub.4 alkyloxy, and carboxy-C.sub.1 -C.sub.4 alkyloxy;X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiopheny, 1-tetralone-6-yl, C.sub.1 -C.sub.4 alkylenedioxy, pyridyl, furyl and thienyl, these groups optionally being substituted with up to three substituents selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, NO.sub.2, CF.sub.3 and SO.sub.2 CH.sub.3 ; andR is hydrogen, C.sub.1 -C.sub.4 alkyl or a hydroxy protecting group.
Abstract: A compound of the formula ##STR1## wherein Z and Q are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use.
Abstract: The present invention relates to processes for the preparation of 3-(1-piperazinyl)-1,2-benzoisothiazole or its pharmaceutically acceptable salt and to novel intermediates used in the process.
Type:
Grant
Filed:
October 15, 1998
Date of Patent:
August 29, 2000
Assignee:
Pfizer, Inc.
Inventors:
Darrell E. Fox, John F. Lambert, Terry G. Sinay, Stanley W. Walinsky
Abstract: This invention is directed to compounds of the formula ##STR1## 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 would 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.
Type:
Grant
Filed:
March 1, 1999
Date of Patent:
August 29, 2000
Assignee:
Pfizer Inc.
Inventors:
Philip A Carpino, Paul A DaSilva-Jardine, Bruce A Lefker, John A Ragan
Abstract: The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R.sup.1, R.sup.2, R.sup.3, R.sup.4.sub.1 R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification. The compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, bone resorption, loosening of artificial joint implants, atherosclerosis, multiple sclerosis, occular angiogenisis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.
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