Abstract: This invention relates to a novel crystalline form (Form A) of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this crystalline form, to processes for forming it and to its use in medical treatment.
Type:
Grant
Filed:
December 17, 2009
Date of Patent:
May 8, 2012
Assignee:
Novartis AG
Inventors:
Yugang Liu, Dimitris Papoutsakis, Elizabeth Roddy
Abstract: Purification process for the preparation of the allylamine pharmaceutical terbinafine of formula I in free base form or acid addition salt form, by distilling crude terbinafine base, preferably by short path distillation, e.g. at a temperature above 100° C. and reduced pressure, e.g. 0.2 mbar, and recovering the purified product in free base or acid addition salt form.
Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
Type:
Grant
Filed:
February 1, 2008
Date of Patent:
May 10, 2011
Assignee:
Novartis AG
Inventors:
Shifeng Pan, Wenqi Gao, Nathanael S Gray, Yuan Mi, Yi Fan
Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
Type:
Grant
Filed:
February 24, 2009
Date of Patent:
March 8, 2011
Assignee:
Novartis AG
Inventors:
Rainer Albert, Eric Francotte, Frederic Zecri, Markus Zollinger
Abstract: This invention relates to novel tetrazole and oxadiazalone ?-amino acids derivatives of the formula wherein G is wherein R1 through R4 are defined as in the specification, pharmaceutical compositions containing them and their use for the treatment of various central nervous system and other disorders. The cyclopropyl ?-amino acids derivatives of this invention exhibit activity as alpha2delta ligands (?2? ligands). Such compounds have affinity for the ?2? subunit of a calcium channel.
Type:
Grant
Filed:
March 8, 2004
Date of Patent:
July 31, 2007
Assignee:
Warner Lambert Company LLC
Inventors:
Nancy Sue Barta, Norman Lloyd Colbry, Raymond Hudack, Jr., Kristin Knapp Lin, Jacob Bradley Schwarz, Andrew John Thorpe, David Juergen Wustrow, Zhijian Zhu
Abstract: This invention relates to compounds of the formula 1 wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.
Type:
Grant
Filed:
November 7, 2003
Date of Patent:
September 5, 2006
Assignee:
Warner Lambert Company
Inventors:
Stephen Sung Yong Cho, Jamie Marie Singer, James M. Graham, Tracy Fay Gregory, Harry Ralph Howard, Jr., Sham Shridhar Nikam, Michael Anthony Walters
Abstract: This invention relates to certain ?-amino acids that bind to the alpha-2-delta (?2?) subunit of a calcium channel. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders.
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
June 20, 2006
Assignee:
Warner-Lambert Company
Inventors:
Nancy Sue Barta, Jacob Bradley Schwarz, Andrew John Thorpe, David Juergen Wustrow
Abstract: This invention provides a method of making (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid (pregabalin) or a salt thereof via an asymmetric hydrogenation synthesis. Pregabalin is useful for the treatment and prevention of seizure disorders, pain, and psychotic disorders. The invention also provides intermediates useful in the production of pregabalin.
Type:
Grant
Filed:
January 11, 2001
Date of Patent:
May 10, 2005
Assignee:
Warner-Lambert Company
Inventors:
Mark Joseph Burk, Om Prakash Goel, Marvin Simon Hoekstra, Thomas Frederick Mich, Thomas Mulhern, James A. Ramsden
Abstract: The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula I
The compounds are useful as therapeutic agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, arthritis, sleep disorders, IBS, and gastric damage. Methods of preparing the compounds and useful intermediates are also part of the invention.
Type:
Grant
Filed:
December 20, 2002
Date of Patent:
November 4, 2003
Assignee:
Warner-Lambert Company
Inventors:
Thomas Richard Belliotti, Justin Stephen Bryans, Ihoezo Victor Ekhato, Augustine Tobi Osuma, Robert Michael Schelkun, Jacob Bradley Schwarz, Andrew John Thorpe, Lawrence David Wise, David Juergen Wustrow, Po-Wai Yuen
Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
Type:
Grant
Filed:
February 8, 2000
Date of Patent:
October 21, 2003
Assignee:
Warner-Lambert Company
Inventors:
Justin Stephen Bryans, David Christopher Horwell, Andrew John Thorpe, David Juergen Wustrow, Po-Wai Yuen
Abstract: Cyclic amino acids, such as gabapentin and pregabalin, are used for treating physiological conditions associated with the use, or sequelae of use, of cocaine or other psychomotor stimulants and other addictive drugs/substances. Physiological conditions include stimulant-induced toxicities.
Type:
Grant
Filed:
August 29, 2000
Date of Patent:
May 20, 2003
Assignee:
Pfizer Inc.
Inventors:
Hyacinth Chi Akunne, Ann Elizabeth Corbin, David James Dooley, Alysia Latrese Green, Thomas Gary Heffner
Abstract: The present invention is directed to novel combinations of one or more anti-epileptic compounds that demonstrate pain alleviating properties, with one or more compounds selected from the group consisting of analgesics, NMDA receptor antagonists, NSAIDs, and combinations thereof, and pharmaceutical compositions comprising same. It has been discovered that the administration of anti-epileptic compounds that demonstrates pain alleviating properties in these novel combinations results in an improved reduction in the frequency and severity of pain. It is also believed that the incidence of unwanted side effects can be reduced by these novel combinations in comparison to using higher doses of a single agent treatment to achieve a similar therapeutic effect. The present invention is also directed to methods of using effective amounts of the novel pharmaceutical compositions to treat pain in mammals.
Abstract: The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active substituted 2-phenyl-3-benzylaminopiperidines. The substituted 2-phenyl-3-benzylaminopiperidines that can be prepared by the processes of this invention are substance P receptor antagonists and are useful in the treatment and prevention of inflammatory and central nervous system disorders, as well as several other disorders.
Type:
Grant
Filed:
September 18, 1995
Date of Patent:
August 20, 2002
Assignee:
Pfizer INC
Inventors:
Harry A. Watson, Jr., William M. Snyder, Glenn E. Wilcox
Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.
Abstract: Compounds of the formula
wherein R1 is methoxy and R2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds.
These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.
Type:
Grant
Filed:
January 24, 1995
Date of Patent:
April 24, 2001
Inventors:
Fumitaka Ito, Hiroshi Kondo, Masami Nakane, John Adams Lowe, III, Terry Jay Rosen, Kaoru Shimada
Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.
Abstract: This invention relates to the quinuclidine derivative (2S, 3S)-N-(5-n-propyl-2-methoxyphenyl)methyl-2-diphenylmethyl-1-azabicyclo?2.2 .2!octan-3-amine and its pharmaceutically acceptable salts. These compounds are substance P antagonists and are useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.
Abstract: This invention relates to novel, pharmaceutically active benzimidazolone derivatives of the formula ##STR1## wherein the dashed line, R.sup.0 through R.sup.6 and X.sup.1 through X.sup.3 are defined as in the specification. These compounds exhibit central dopaminergic activity and are u in the treatment of CNS disorders.
Type:
Grant
Filed:
March 11, 1997
Date of Patent:
March 16, 1999
Assignee:
Pfizer Inc.
Inventors:
Anton F-J. Fliri, Brian T. O'Neill, William S. Faraci, Mark A. Sanner, Stevin H. Zorn