Assignee: Merck Frosst Canada & Co.

Location: Kirkland, CA
No. of patents: 74

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Number	Title	Issue Date
7163932	Aryldifluoromethylphosphonic acids for treatment of diabetes The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compo...	01/16/2007
7144913	Dihydropyrrolo[1,2-a]indole and tetrahydropyrido[1,2-a]-indole derivatives as prostaglandin d2 receptor antagonists Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma. ...	12/05/2006
7019022	Substituted tetrahydrocarbazole and cyclopentanoindole derivatives The present invention provides substituted tetrahydrocarbazole and cyclopentanoindole derivatives as antagonists of DP receptor, and as such are useful for the treatment of prostaglandin D2 mediated diseases such as rhinitis, asthma and nasal congestion. ...	03/28/2006
6919353	Substituted 8-arylquinolune PDE4 inhibitors 8-arylquinolines of formula (I) wherein the aryl group at the 8-position contains a meta two atom bridge to an optionally substituted phenyl or pyridyl group, are PDE4 inhibitors useful to treat asthma, chronic bronchitis, chronic obstructive pulmonary disease, arth...	07/19/2005
6841564	Tri-aryl-substituted-ethane PDE4 inhibitors Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors. ...	01/11/2005
6812346	Substituted pyridines as selective cyclooxygenase-2 inhibitors The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.	11/02/2004
6777433	Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing...	08/17/2004
6743802	Alkyne-aryl phosphodiesterase-4 inhibitors Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation. ...	06/01/2004
6740666	Substituted 8-arylquinoline phosphodiesterase-4 inhibitors Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl grou...	05/25/2004
6639077	Tri-aryl-substituted-ethane PDE4 inhibitors Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors....	10/28/2003
6610720	Method for treating or preventing emesis Alpha-2 adrenoreceptor agonists are useful for the treatment and/or prevention of emesis in patients....	08/26/2003
6583126	Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, ...	06/24/2003
6552168	Gamma-ketoacid tetrapeptides as inhibitors of caspase-3 The invention encompasses the novel class of compounds represented by formula I, which are caspase-3 inhibitors. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of caspase-3 mediated diseases comprising compounds ...	04/22/2003
6525025	Gamma-ketoacid dipeptides as inhibitors of caspase-3 This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods...	02/25/2003
6498151	Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated d...	12/24/2002
6486141	Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, ...	11/26/2002
6486142	Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases,...	11/26/2002
6465509	Pyrones as inhibitors of cyclooxygenase-2 The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as m...	10/15/2002
6465444	Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated d...	10/15/2002
6448274	Fluoroalkoxy-substituted benzamide dichloropyridinyl N-oxide PDE4 inhibitor A PDE4 inhibiting compound is represented by ##STR1##...	09/10/2002
6448429	Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases,...	09/10/2002
6441002	Polymorphic, amorphous and hydrated forms of 5-chloro-3-(4-methanesulfonyphenyl)-6'- methyl-[2,3']bipyridinyl Polymorphic, amorphous and hydrated forms of the title compound having the following structure: ##STR1## are disclosed. The compound is a potent and selective cyclooxygenase-2 (COX-2) inhibitor....	08/27/2002
6436965	PDE IV inhibiting amides, compositions and methods of treatment Compounds represented by formula I: ##STR1## as well as pharmaceutically acceptable salts and hydrates thereof are disclosed as useful for treating or preventing diseases and conditions mediated by PDE-IV. Pharmaceutical compositions and methods of treatm...	08/20/2002
6420565	Process for making 2, 5-substituted pyridine 2-lithio-5-halopyridine is formed as a predominant component of a reaction mixture by reacting BuLi with 2,5-dihalopyridine in a non-coordinating solvent....	07/16/2002
6414006	Methods for inhibiting bone resorption The present invention relates to methods for inhibiting bone resorption in a mammal comprising administering to a mammal in need thereof a therapeutically effective amount of an EP4 receptor subtype antagonist....	07/02/2002
6410563	Substituted 8-arylquinoline phosphodiesterase-4 inhibitors Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors....	06/25/2002
6410583	Cyclopentanoindoles, compositions containing such compounds and methods of treatment Substituted cyclopentanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases....	06/25/2002
6399636	Tri-aryl-substituted-ethane PDE4 inhibitors Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors....	06/04/2002
6395499	Methods of identifying modulators of a DP prostaglandin receptor A human prostaglandin receptor has been identified and DNA encoding the receptor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the human prostaglandin receptor and host cells expressing the receptor are used to iden...	05/28/2002
6369084	Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases, ##STR1## or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses certain pharmaceuti...	04/09/2002
6369082	Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases, ##STR1## or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses pharmaceutical comp...	04/09/2002
6365360	Methods of identifying modulators of human IP prostaglandin receptor A novel prostaglandin receptor has been identified and DNA encoding the receptor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the novel prostaglandin receptor and host cells expressing the receptor are used to iden...	04/02/2002
6358694	Methods of identifying modulators of a prostaglandin receptor A novel prostaglandin receptor has been identified and DNA encoding the receptor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the novel prostaglandin receptor and host cells expressing the receptor are used to iden...	03/19/2002
6348572	Ligands for phosphatase binding assay Disclosed are new ligands for use in a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in ...	02/19/2002
6346373	Whole cell assay for cathepsin K activity The present invention relates to a whole cell assay for cathepsin K. The present invention is useful for determining cathepsin K activity in a mammalian cell systems and for identifying and evaluating inhibitors of cathepsin K....	02/12/2002
6316472	Heterosubstituted pyridine derivatives as PDE 4 inhibitors The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4). ##STR1## The ...	11/13/2001
6316434	Assay for emetic activity An assay for emetic activity among inhibitors of type 4 phosphodiesterase (PDE 4) is disclosed. The assay comprises: (A) administering to a test mammal an anesthetic compound in an amount sufficient to cause an anesthetic effect; (B) administering to the test ...	11/13/2001
6281391	Synthesis of methylthiophenyl hydroxyketones This invention encompasses a novel process for synthesizing compounds represented by formula A: ##STR1## These compounds are intermediates useful in the preparation of certain agents that are selective COX-2 inhibitors....	08/28/2001
6277839	Biphenylene lactams as prostaglandin receptor ligands The present invention relates to biphenylene lactams of Formula II which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of such a treatment of a n...	08/21/2001
6242493	Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed. The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such com...	06/05/2001

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Assignee: Merck Frosst Canada & Co.