Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
Type:
Application
Filed:
October 28, 2003
Publication date:
June 3, 2004
Applicant:
Pfizer Inc
Inventors:
Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
Abstract: The present invention provides a process for the preparation of a nonracemic diastereomer of 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanol by hydrogenation of a corresponding nonracemic 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanone using a catalyst system comprising ruthenium, a nonracemic diphosphine ligand, a bidentate amine ligand selected from amino-thioethers and achiral diamines, and a base.
Type:
Grant
Filed:
January 24, 2002
Date of Patent:
June 1, 2004
Assignees:
DSM Catalytica Pharmaceuticals, Inc., Pfizer, Inc.
Abstract: The invention relates to the use of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five (cGMP PDE V) inhibitor for increasing fecundity in a mammal by one or more of (a) promoting the growth of an oocyte, zygote, blastocyst, embryo and/or foetus, (b) increasing the rate or probability of survival of an embryo and/or foetus and (c) increasing the birth weight of a progeny, or for increasing milk productivity.
Type:
Grant
Filed:
August 27, 2002
Date of Patent:
June 1, 2004
Assignee:
Pfizer Inc.
Inventors:
Simon Lempriere Westbrook, Johannes Fridrich Zanzinger
Abstract: A crystallization process for generating a pharmaceutical product from solutions of pharmaceutically active compounds or their reactive intermediates employs fluid jet streams containing pharmaceutically active ingredients, appropriate anti-solvents and/or their reactive intermediates capable of producing a pharmaceutical product with desired particle size characteristics upon mixing, chemical reaction, nucleation and precipitation. The jet streams are directed towards an impinging plate, and mixing occurs as the jet streams impinge the plate at a desired area of impact.
Abstract: This invention is directed to compounds of the formula:
wherein j is 0 or 1; k is 0 or 1; m is 0 or 1; n is 0 or 1; W is —O—; —S(═O)t—, where t is 0, 1, or 2; or —N(R3)—; where R3 is —H, —(C1-C3) alkyl, —OR12, phenyl, or benzyl; RC and RD have the same meaning as RA and RB, except that at least one of RC and RD must be —H; and the other variables are defined as set forth in the specification. The invention is also directed to pharmaceutical compositions comprising the above compounds and to methods of treating a subject suffering from a disease, disorder or condition mediated by the PDE4 isozyme, the method comprising administering a therapeutically effective amount of a compound as described above.
Type:
Grant
Filed:
July 24, 2002
Date of Patent:
May 25, 2004
Assignee:
Pfizer Inc
Inventors:
Thomas Victor Magee, Anthony Marfat, Robert James Chambers
Abstract: This invention relates to the enantiomers of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one, prodrugs thereof, and pharmaceutically acceptable salts and solvates of said compounds and said prodrugs, that are useful in the treatment of hyperproliferative diseases, such as cancers, in mammals. The invention also relates to processes for the production of enantiomerically pure or optically enriched (+)- or (−)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one enantiomers from a mixture containing two enantiomers using continuous chromatography.
Type:
Grant
Filed:
August 27, 2002
Date of Patent:
May 25, 2004
Assignee:
Pfizer Inc
Inventors:
R. Mark Guinn, Subramanian Sam Guhan, Karl K Ng, Derek L. Tickner, Marcus Douglas Ewing, Clifford N. Meltz, Bryan Li, Kees Pouwer
Abstract: Suspension methods and compositions for effecting large-scale in vitro differentiation of mammalian embryonic stem cells are provided, as well as methods comprising the subject large-scale in vitro differentiation methods.
Type:
Application
Filed:
October 31, 2003
Publication date:
May 20, 2004
Applicant:
Pfizer Inc
Inventors:
Timothy D. Gryseels, John E. Hambor, Steven J. Hawrylik, Marsh L. Roach
Abstract: When selamectin is administered to a female animal over a period commencing during pregnancy and ending during lactation, endo- and ecto-parasite infestations are either treated or prevented in that animal's offspring, avoiding the problems of treating the offspring directly. This leads to improvements in the compliance of dosing and hence the efficacy of treatment and reduces the number of doses to be administered leading to economic benefits and greater convenience.
Type:
Application
Filed:
November 12, 2003
Publication date:
May 20, 2004
Applicant:
Pfizer Inc
Inventors:
Hafid Abdelaali Benchaoui, Antoinette Beaton Drain Jernigan, Mark Payne-Johnson, Timothy George Rowan
Abstract: The present invention is directed to a novel strain of feline immunodeficiency virus, designated herein as FIV-141, and to attenuated forms of the virus produced by mutating specific regions of the viral genome. The virus and mutated forms of the virus may be used to induce the production of antibodies to FIV-141, and in vaccines designed to protect cats from FIV.
Abstract: The present invention relates to a mutual prodrug of amlodipine and atorvastatin, pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions thereof and the use of said prodrug and its salts in the manufacture of medicaments for the treatment of atherosclerosis, angina pectoris, combined hypertension and hyperlipidaemia and the management of cardiac risk.
Abstract: This invention is directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth comprising administering prostaglandin agonists which are EP4 receptor selective prostaglandin agonists. This invention is especially directed to those methods wherein the EP4 receptor selective agonist is a compound of Formula I:
wherein the variables are as defined in the specification.
Type:
Grant
Filed:
December 15, 2000
Date of Patent:
May 18, 2004
Assignee:
Pfizer Inc.
Inventors:
Kimberly O. Cameron, HuaZhu Ke, Bruce A. Lefker, David D. Thompson
Abstract: The invention relates to novel erythromycin analogs and azalides, particularly ones with novel C-13 substituents, and to pharmaceutically acceptable salts thereof. The compounds of this invention are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial protozoa infections by administering such compounds. The invention also relates to methods of preparing such compounds and to intermediates useful in such preparation.
Type:
Application
Filed:
July 30, 2002
Publication date:
May 13, 2004
Applicant:
Pfizer Inc.
Inventors:
John Philip Dirlam, Hamish Alastair Irvine McArthur, Alan Elwood Blize
Abstract: The bioavailability of azithromycin can be increased by co-administering azithromycin with a p-glycoprotein (p-gp) inhibitor. The azithromycin and p-gp inhibitor can be administered together in a composition or as separate components. If administered separately, they can be embodied as a kit.
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 and/or frailty, 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, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.
Type:
Grant
Filed:
October 15, 2002
Date of Patent:
June 1, 2004
Assignee:
Pfizer Inc.
Inventors:
Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker