Abstract: The invention relates to compounds of the formula 1
and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3 and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals with administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
Type:
Grant
Filed:
January 20, 2000
Date of Patent:
September 4, 2001
Assignee:
Pfizer Inc.
Inventors:
John Charles Kath, Norma Jacqueline Tom, Zhengyu Liu, Eric David Cox, Joel Morris, Samit Kumar Bhattacharya
Abstract: The present invention provides polynucleotide molecules encoding portions of the S protein from feline infectious peritonitis virus (FIPV). The present invention further provides polynucleotide molecules encoding the entire S protein or portions thereof from feline enteric coronavirus (FECV). The polynucleotide molecules of the present invention are useful as diagnostic reagents.
Type:
Grant
Filed:
February 22, 1995
Date of Patent:
August 28, 2001
Assignee:
Pfizer Inc
Inventors:
Timothy J. Miller, Albert Paul Reed, Sharon R. Klepfer, Nancy E. Pfeiffer, Brian T. Suiter, Elaine V. Jones
Abstract: A method of combatting atherosclerosis by administering an effective amount of a macrolide antibiotic, for example an azalide such as azithromycin, optionally together with one or more pharmaceutically acceptable carriers or excipients, to a subject.
Abstract: The invention provides a process for the production of a compound of formula I, which comprises reacting a compound of formula II with a compound of formula III, in the presence of a strong base and a palladium(0) catalyst, at an elevated temperature, in a solvent which does not adversely affect the reaction. Compounds of formula I may be further processed to compounds of formula V, which are useful in the treatment of inter alia migraine.
Abstract: This invention is directed to compounds of the formula
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 wound 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:
December 22, 1999
Date of Patent:
August 21, 2001
Assignee:
Pfizer Inc.
Inventors:
Philip A Carpino, Paul A DaSilva-Jardine, Bruce A Lefker, John A Ragan
Abstract: This invention provides a compound of the following formula:
or the pharmaceutically acceptable salts thereof wherein R1 is H or C1-4 alkyl; R2 is C(═L′)R3 or So2R4; Y is a direct bond or C1-4 alkylene; L and L′ are independently oxygen or sulfur; Q is selected from the following: C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl or naphthyl, optionally substituted 5 or 6-membered monocyclic aromatic group;
R3 is —OR6, —NR7R8, N(OR1)R7 or a group of formula:
Z is a direct bond, O, S or NR5; R4 is C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted phenyl or naphthyl; R5 is C1-4 alkyl or halo-substituted C1-4 alkyl; R6 is C1-4 alkyl C3-7 cycloalkyl, C1-4 alkyl-C3-7 cycloalkyl, halo-substituted C1-4 alkyl, optionally substituted C1-4 alkyl-phenyl or phenyl; R7 and R8 are each selected from the following: H, optionally substituted C1-6 alkyl, optionally substituted C3-7 cyclo
Type:
Grant
Filed:
August 26, 1999
Date of Patent:
August 21, 2001
Assignee:
Pfizer Inc
Inventors:
Kazunari Nakao, Rodney W. Stevens, Kiyoshi Kawamura, Chikara Uchida
Abstract: A compound of the formula
or the pharmaceutically acceptable salt thereof, wherein
Z is oxygen, S(O)m wherein m is 0, 1 or 2; or NQ wherein Q is hydrogen, (C1-C6)alkyl or phenyl;
X is hydrogen, chloro, fluoro, bromo, iodo, hydroxy, nitro, cyano, (C1-C6)alkyl, trifluoromethyl, (C1-C6)alkoxy, (C1-C6)alkyl S(O)a wherein a is 0, 1 or 2; or phenyl wherein the phenyl group is optionally substituted;
Y is
wherein M is oxygen or sulfur;
X2 is hydrogen, fluoro, chloro, trifluoromethyl, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkyl S(O)c wherein c is 0, 1 or 2;
R1 is selected from
wherein R6 is selected from the group consisting of hydrogen, optionally substituted (C1-C6)alkyl; and wherein R6 in G5 together with R7 form a 2 carbon chain; and R9 and R10 are independently hydrogen or (C1-C6)alkyl;
R2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally substituted; and
R3 is —(CH2)tB, wherein t is 0-3 and B is hydrog
Abstract: Compounds of Formula (I)
wherein
R6 is carboxy, (C1-C8)alkoxycarbonyl, benzyloxycarbonyl, C(O)NR8R9 or C(O)R12 as glycogen phosphorylase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat diabetes, hyperglycemia, hypercholesterolemia, hypertension, hyperisulinemia, hyperlipidemia, atherosclerosis and myocardial ischemia in mammals.
Type:
Grant
Filed:
August 15, 2000
Date of Patent:
August 21, 2001
Assignee:
Pfizer, Inc.
Inventors:
Dennis J. Hoover, Bernard Hulin, William H. Martin, Douglas Phillips, Judith L. Treadway
Abstract: This invention provides a compound of formula (I):
or pharmaceutically acceptable salts thereof, wherein X1 and X2 are C or N, respectively; R1 and R2 are independently phenyl optionally substituted with a hydroxy group with proviso that X1 and X2 are not simultaneously C or N, when X1 is N, R1 is absent, and when X2 is N, R2 is absent; R3 is methyl or hydroxymethyl; R4 is formyl, hydroxymethyl or hydroxy C3-6 alkenyl; R5 is hydroxy, C3-6 alkenyl or hydroxy C3-6 alkenyl; or R4 and R5, together with the carbon atoms in the furopyridine ring to which they are attached, may form the following ring (to be fused with the furopyridine ring):
with the proviso that when R3 is methyl and R5 is 2-buten-2-yl, X2 is not N. These compounds and pharmaceutical compositions containing such compounds are useful for treating infectious diseases caused by bacteria.
Type:
Grant
Filed:
October 29, 1999
Date of Patent:
August 21, 2001
Assignee:
Pfizer Inc
Inventors:
Yutaka Sugie, Akemi Sugiura, Nobuji Yoshikawa, Susan J. I Truesdell, John W. Wong
Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.
Type:
Grant
Filed:
October 28, 1999
Date of Patent:
August 14, 2001
Assignee:
Pfizer Inc.
Inventors:
Thomas G. LaCour, Charles William Murtiashaw, III
Abstract: The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I
Abstract: This invention relates to methods of preparing compounds of Formula 1:
and to pharmaceutically acceptable salts and solvates thereof, and to methods for preparing same. The compounds of Formula 1 are antibacterial agents that may be used to treat various bacterial and protozoal infections, and may also be used to treat cancer. The invention also relates to pharmaceutical compositions comprising the compounds of Formula 1, and to methods of treating sbacterial and protozoal infections by administering compounds of Formula 1.
Type:
Grant
Filed:
January 26, 2000
Date of Patent:
August 7, 2001
Assignee:
Pfizer Inc
Inventors:
Thomas N. O'Connell, Brook K. Morse, Hamish Alastair Irvine McArthur, John Philip Dirlam
Abstract: A method for stabilizing blood pressure during hemodialysis is described which uses a phosphodiesterase inhibitor, in particular, a cGMP PDEv inhibitor in the treatment of humans.
Abstract: Erythromycins, particularly with C-13 substituents R1 (e.g. C3-C6 cycloalkyl or cycloalkenyl groups) are prepared by fermenting suitable organisms in the presence of R1CO2H. A preferred organism is Saccharopolyspora erythraea preferably containing an integrated plasmid capable of directing synthesis of desired compounds.
Type:
Grant
Filed:
September 16, 1999
Date of Patent:
August 7, 2001
Assignees:
Biotica Technology Limited, Pfizer, Inc.
Inventors:
Peter Francis Leadlay, James Staunton, Jesus Cortes, Michael Stephen Pacey
Abstract: The present invention relates to an improved method for synthesizing nucleosides with a low &agr;:&bgr; anomeric ratio. The method comprises coupling a protected furanosyl halide and an appropriately protected heterocycle in the presence of a nucleophilic polar solvent and a strong base.
Abstract: A microencapsulated subunit component from bovine herpes virus-1 (BHV-1) is disclosed. Vaccines, kits, and methods for using the same to vaccinate a member of a bovine species are also disclosed.
Type:
Grant
Filed:
April 21, 1998
Date of Patent:
August 7, 2001
Assignee:
Pfizer Inc.
Inventors:
Tully J. Speaker, H. Fred Clark, Charlotte A. Moser, Paul A. Offit, Manuel Campos, Patrick J. Frenchick
Abstract: A method of treating diseases caused by sebaceous gland disorders, in humans and animals, which comprises administering to said humans and animals a composition comprising a sebaceous gland secretion inhibiting amount of an active compound comprising an acyl coA cholesterol acyl transferase (ACAT) inhibitor or prodrug therefor.
A composition for use in treating diseases caused by sebaceous gland disorders such as acne in humans and animals which comprises a sebaceous gland secretion inhibiting amount of an acyl coA cholesterol acyl tanferase (ACAT) inhibitor or prodrug therefor and, optionally, a pharmaceutically acceptable carrier.
Abstract: Compounds of formula (I)
or pharmaceutically, veterinarily or agriculturally acceptable salts thereof, or pharmaceutically, veterinarily or agriculturally acceptable solvates of either entity, wherein R1 is 2,4,6-trisubsituted phenyl or 3,5-disubstituted pyridin-2-yl; R3 is C1-C4 alkyl optionally substituted with hydroxy or with one or more halo; cyano, C1 to C5 alkanoyl or phenyl R5 is hydrogen, C1 to C4 alkyl, amino or halo; R2 and R4 are each independently selected from hydrogen, C1 to C4 alkyl, fluoro, chloro and bromo or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group; R6 and R8 are each independently selected from hydrogen, C1 to C4 alkyl, fluoro, chloro and bromo; or; when R2 and R4 do not form part of a cycloalkyl group, R2 and R6, together with the carbon atoms to which they are attached, may form a C5 to C7 cycloalkyl group; and R7 is hydrogen, C1 to C4 alkyl optionally substituted with one or more halo; or C1 to C4 alkoxy; are parasitici
Abstract: The present invention relates to methods for treating congestive heart failure in a mammal by administering a congestive heart failure treating amount of a compound which inhibits phosphodiesterase type IV and the production of tumor necrosis factor, such as, for example, a substituted indazol derivative, e.g., of the formula
or a pharmaceutically acceptable salt thereof, wherein R, R1 and R2 are as defined herein. The invention further relates to pharmaceutical compositions for the treatment of congestive heart failure comprising a congestive heart failure treating amount of a compound which inhibits phosphodiesterase type IV and the production of tumor necrosis factor, such as, for example, a substituted indazol derivative, e.g., of formula (I) herein, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable vehicle, diluent or carrier.