Abstract: The present invention relates to the derivatives of the compound of formula (I), which are useful in the treatment of inflammatory and central nervous system disorders, as well as other diorders ##STR1##
Abstract: The present invention relates to compounds of the formula ##STR1## The present invention also relates to intermediates for the preparation of compounds of the formula I, pharmaceutical compositions and method of use.
Abstract: The present invention relates to novel spirocyclic piperidine derivatives and related compounds and, specifically, to compounds of the formula ##STR1## wherein X, Z, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and m are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
Abstract: This invention relates to 3-aryl-2-isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The 3-aryl-2-isoxazolines are useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.
Abstract: This invention relates to composite somatotropin peptides and fusion protein thereof useful in the potentiating of growth hormone activity. Also disclosed are vector and host cells useful in the recombinant production of such molecules. Vaccines containing composite somatotropin and fusion proteins thereof and methods of using same as disclosed.
Type:
Grant
Filed:
January 27, 1995
Date of Patent:
November 11, 1997
Assignee:
Pfizer Inc.
Inventors:
Hector Wasunna Alila, Michael Thomas Clark, Elaine Verne Jones, Timothy Joe Miller, Shawn Patrick O'Brien, Ganesh Madhusudan Sathe
Abstract: This invention relates to a novel nucleic acid sequence encoding a novel human phosphodiesterase IV (hPDE IV) isozyme. It also relates to a polypeptide encoded by such sequence.This invention also relates to an assay method for detecting the presence of such novel isozyme in human cells, and to a method of identifying compounds or other substances that inhibit or modify the activity of such isozyme.
Abstract: A process for separating a natural B avermectin from a natural avermectin containing fermentation broth by using an aqueous precipitation. The process comprises extracting natural avermectins from the fermentation broth with a water miscible solvent and adding sufficient water to precipitate the natural B avermectins. Preferably, the water miscible solvent is a C.sub.1 -C.sub.3 alcohol, acetone, or acetonitrile. In addition, an acid, base, salt or surfactant may be added to facilitate the precipitation. This invention provides an isolation technique that substitutes the use of an aqueous precipitation for nonaqueous solvent precipitations. The reduction in use of nonaqueous solvents provides economic, environmental and safety benefits.
Abstract: A compound having formula (III). Also, a process of making azithromycin comprising reducing the compound of formula (III) and N-methylating the reduced product.
Abstract: Novel processes are disclosed for the stereoselective preparation of substituted piperidine derivatives of the formulae ##STR1## wherein R.sup.1 and R.sup.2 are defined as below, useful as substance P receptor antagonists and in treating diseases mediated by an excess of substance P.
Abstract: In a process for dehydrating 5-hydroxy-11a-chlorotetracycline-6,12-hemiketal to 5-hydroxy-6-demethyl-6-desoxy-6-methylene-11a-chlorotetracycline, utilizing an acid which is not decomposable by water, formic acid serves as a solvent free from chlorinated hydrocarbons.
Abstract: Described herein are Benzopyran and other benzo-fused leukotriene B.sub.4 antagonists have the formula ##STR1## wherein R.sup.1 is a phenyl or substituted phenyl group, and A, n, R.sup.2 and R.sup.3 are as defined herein.
Abstract: The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C.sub.1 -C.sub.6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C.sub.1 -C.sub.4 alkyl groups attached to the chain: X is oxygen or sulfur, n is an integer of 3 to 6; M is hydrogen, pharmaceutically acceptable cation or a metabolically cleavable group: and X and A may be attached at any available position on the ring. These compounds are useful for treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
Type:
Grant
Filed:
October 3, 1995
Date of Patent:
October 28, 1997
Assignee:
Pfizer Inc.
Inventors:
Rodney William Stevens, Takashi Mano, Yoshiyuki Okumura, Masami Nakane
Abstract: Actinomadura roseorufa mutants characterized by the ability to produce by fermentation UK-61,689, an acidic polycyclic ether anticoccidial antibiotic previously available only by selective acid hydrolysis of UK-58,852; and Actinomadura roseorufa having the identifying characteristics of ATCC 53,666, ATCC 53,665, ATCC 53,664 and ATCC 53,674.
Abstract: The present invention relates to C-20 olefin derivatives of 16-membered macrolide antibiotics repromicin, rosaramicin, 5-mycaminosyltylonolide, desmycosin, lactenocin, O-demethyllactenocin, 4'-deoxymycaminosyltylonolide and 23-deoxymycaminosyltylonolide, which are useful against bacterial and mycoplasmic pathogens in animals. Also claimed are a pharmaceutical composition of such derivatives and their use in treating bacterial and mycoplasmic infections in animals.
Abstract: This invention is directed to novel antiparasitic compounds of formula (I), wherein the broken line represents an optional bond, R.sup.1 and R.sup.4 being absent when this bond is present, R.sup.1, R.sup.3, R.sup.4 are independently H, OH, halo mercapto, oxo, oximino, or an organic radical, R.sup.2 and R.sup.7 are organic radicals, R.sup.6 is H or an organic radical and R.sup.12 is OH, halo, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.9 alkanoyloxy, or oximino optionally O-substituted by a C.sub.1 -C.sub.8 alkyl, alkenyl, alkynyl, aryl, trialkylsilyl, aralkyl or C.sub.1 -C.sub.9 alkanoyl group.
Abstract: Compounds of the formula ##STR1## which are intermediates in the preparation of hydantoin aldose reductase inhibitors and methods of preparing these intermediates.
Abstract: The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein the dashed line represents an optional covalent bond; X is O, NH, S or a direct link; R.sup.3 is hydroxy when the dashed line does not represent a covalent bond and R.sup.3 is absent when the dashed line represents a covalent bond; R.sup.4 is (a), when X is O, a group of formula (i), (b), when X is O, NH or S, optionally substituted hydroxyphenyl, (c) an optionally substituted 4- to 7-membered heterocyclic ring, or (d), when X is NH, a group of formula (ii). The compounds are useful for the treatment of disease associated with the altered tone or motility of smooth muscle.
Type:
Grant
Filed:
August 4, 1995
Date of Patent:
October 14, 1997
Assignee:
Pfizer Inc.
Inventors:
Alexander Roderick Mackenzie, Sandra Marina Monaghan
Abstract: The present invention provides a novel culture which belongs to Actinoplanes (Actinoplanes sp. FERM BP-3832). This culture is capable of producing rapamycin more than ten times efficiently than the cultures which have been reported (e.g., Streptomyces hygroscopicus ATCC 29253). The present invention provides a process for the production of rapamycin which comprises cultivating Actinoplanes sp. FERM BP-3832 and thereafter isolating rapamycin from the fermentation mixture.
Abstract: A non-lymphoid continuous cell line adapted for propagation of avian coccidia is provided. This cell line is useful for the production of vaccine antigens for prophylactic treatment of poultry, particularly in a vaccine for coccidia.
Type:
Grant
Filed:
July 11, 1994
Date of Patent:
October 7, 1997
Assignee:
Pfizer Inc.
Inventors:
Timothy J. Miller, Robert A. Clare, Patricia Lufburrow
Abstract: This invention relates to a novel nucleic acid sequence encoding a novel human phosphodiesterase IV (hPDE IV) isozyme. It also relates to a polypeptide encoded by such sequence.This invention also relates to an assay method for detecting the presence of such novel isozyme in human cells, and to a method of identifying compounds or other substances that inhibit or modify the activity of such isozyme.