Abstract: The present invention relates to tetrahydronaphthyridine derivatives of the general formula (I): or of the general formula (I?) in which A and R1 are as defined within, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, including the treatment diseases mediated by H3 ligands, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
May 12, 2005
Date of Patent:
July 7, 2009
Assignee:
Pfizer Inc
Inventors:
Graham Lunn, John Paul Mathias, Ross Sinclair Strang
Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
Type:
Grant
Filed:
January 20, 2006
Date of Patent:
July 7, 2009
Assignee:
Pfizer Inc
Inventors:
Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
Abstract: Pharmaceutical compositions having uniform drug distribution and potency utilizing laxofoxifene as an active ingredient and containing a silicon dioxide to reduce loss of the active ingredient during the manufacturing process and methods for manufacturing such compositions are disclosed.
Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
July 3, 2007
Date of Patent:
June 16, 2009
Assignee:
Pfizer Inc
Inventors:
Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
March 21, 2005
Date of Patent:
May 26, 2009
Inventors:
Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
July 3, 2007
Date of Patent:
May 5, 2009
Assignee:
Pfizer Inc.
Inventors:
Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
Abstract: Compounds of the general formula (I): pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1 receptor by administering a compound of general formula (I) to a subject.
Abstract: A compound of formula (I), or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof; and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airways diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.
Type:
Grant
Filed:
August 10, 2005
Date of Patent:
March 31, 2009
Assignee:
Pfizer Inc.
Inventors:
John Paul Mathias, David Simon Millan, Russell Andrew Lewthwaite, Christopher Phillips
Abstract: The present invention is directed to a new class of 4-cyano-phenoxy-alkyl carboxyl derivatives and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.
Type:
Grant
Filed:
April 1, 2005
Date of Patent:
March 24, 2009
Assignee:
Pfizer Inc.
Inventors:
Lain-Yen Hu, Huangshu Lei, Daniel Y. Du, Bruce A. Lefker, Yvonne Dorothy Smith, Victor Fedij
Abstract: The invention provides compounds of formula (I): wherein: m is 0, 1 or 2; X is O, S or N—CN; R is F, Cl or CN; A is a C3-6 cycloalkylene group optionally substituted with a C1-4 alkyl group; and B is a single bond or a C1-2 alkylene group; or a pharmaceutically acceptable salt, solvate, polymorph or prodrug thereof. The compounds are PDE7 inhibitors and have a number of therapeutic applications, particularly in the treatment of pain, especially neuropathic pain.
Abstract: 6,7-Dihydro-5H-cyclopenta[b]pyridine and 5,6,7,8-tetrahydroquinoline compounds of Formula (I), including salts, hydrates and solvates thereof, that act as 5-HT2 receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2c receptors are described herein.
Type:
Grant
Filed:
March 31, 2006
Date of Patent:
March 24, 2009
Assignee:
Pfizer Inc.
Inventors:
Bruce A. Lefker, Kevin K. -C. Liu, Hou Chen, Steven Blair Coffey
Abstract: This invention relates to a novel salt form of dopamine agonist 5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine (I): More particularly, this invention relates to 5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine di-(1S)-camphorsulfonate (di-S-camsylate) and to processes for the preparation of, intermediates used in the preparation of, compositions containing, and the uses of this salt.
Type:
Grant
Filed:
February 6, 2006
Date of Patent:
March 3, 2009
Assignee:
Pfizer Inc.
Inventors:
Stuart Peter Green, Olivier Alain Lazzari, Duncan Charles Miller, Fabrice Henri Salingue
Abstract: The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid compound of this invention as an effective ingredient in an antiparasitic formulation. More particularly, the present invention relates to derivatives of the terpene alkaloid (1S,2R,4aS,5R,8R,8aR)-2-(acetyloxy)-8a-hydroxy-3,8-dimethyl-5-(1-methylethenyl)-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl (2S,3aR,9bR)-6-chloro-9b-hydroxy-5-methyl-1,2,3,3a,5,9b-hexahydropyrrolo[2,3-c][2,1]benzoxazine-2-carboxylate. Pharmaceutical compositions comprising the same are also disclosed.
Type:
Grant
Filed:
February 12, 2004
Date of Patent:
February 24, 2009
Assignee:
Pfizer Inc.
Inventors:
Nathan A. Chubb, Douglas J. Critcher, James J. Eshelby, Graham Lunn, Andrew J. Rudge, Nigel D. Walshe, Paul H Wiedenau, David H. Williams
Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.
Type:
Grant
Filed:
June 18, 2007
Date of Patent:
February 3, 2009
Assignee:
Pfizer, Inc.
Inventors:
David W. Piotrowski, Yu Hui, John W. Benbow
Abstract: The present invention provides for compounds of Formula I: wherein R2, R3, R4, R5, R6, R7, X, and L have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of central nervous disorders and conditions including attention deficit hyperactivity disorder, neuropathic pain, urinary incontinence, anxiety, depression, and schizophrenia and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
Abstract: A palatable chewable tablet is described herein for oral administration of cetirizine dihydrochloride. The formulation is made more palatable by incorporating a combination of a grape flavoring agent with a vanilla flavoring agent.
Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii)one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating e
Type:
Grant
Filed:
April 18, 2006
Date of Patent:
January 27, 2009
Assignee:
Pfizer Inc.
Inventors:
Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
March 10, 2005
Date of Patent:
January 27, 2009
Assignee:
Pfizer Inc
Inventors:
Alan Daniel Brown, Justin Stephen Bryans, Paul Alan Glossop, Charlotte Alice Louise Lane, Simmon John Mantell
Abstract: The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
Type:
Grant
Filed:
March 17, 2005
Date of Patent:
January 20, 2009
Assignee:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Stephane Caron, Christopher John Helal, Jeffrey W. Raggon, Yong Tao, Nga M. Do
Abstract: The subject invention relates to 2-azabicyclo[3.3.1]nonane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject invention also particularly relates to using such derivatives to treat certain disorders and conditions, for example irritable bowel syndrome, drug addiction, including alcohol addiction, depression, anxiety, schizophrenia and eating disorders, among others, as are more fully described herein.