Abstract: The present invention provides pharmaceutical preparations and the uses thereof for preventing and/or treating seizures and other electroconvulsive disorders by administering a pharmaceutically effective amount of a therapeutic compound having the following formula (I): 1
Type:
Application
Filed:
May 14, 2004
Publication date:
December 30, 2004
Applicant:
University of Kentucky
Inventors:
Peter A. Crooks, Aimee Karis Bence, David Robert Worthern
Abstract: Optically impure tamsulosin including racemic tamsulosin can be resolved into optically pure (R)- or (S)-tamsulosin by the use of diastereomeric sulfonate salts of tamsulosin in a fractional crystallization technique. Racemic tamsulosin free base is a useful starting material for the resolution process and a method of obtaining the same in solid form, including two crystalline polymorphic forms, is also provided.
Type:
Grant
Filed:
July 31, 2002
Date of Patent:
December 28, 2004
Assignee:
Synthon BV
Inventors:
Hans J Hoorn, Theodorus H. A. Peters, Jaroslav Pis, Radim Scigel
Abstract: The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAr1 is a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ar2 a substituted or unsubstituted arylene or heteroarylene group; R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group.
Type:
Application
Filed:
June 30, 2004
Publication date:
December 9, 2004
Inventors:
Arthur A. Aykanian, Steve Billingsley, Philip M. Hodge, Kevin L. Simpson, John Spisak, Jim Strahan
Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
Type:
Application
Filed:
March 25, 2004
Publication date:
December 9, 2004
Applicant:
Tularik Inc.
Inventors:
Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein
Abstract: A process for the sulfonation of an aromatic compound wherein the aromatic compound and sulfonating agent are admixed in the presence of an ionic liquid is described. The method for the sulfonation of aromatic compounds in (e.g. water stable) ionic liquids offers advantages over conventional sulfonation reactions. These are that no by-products form, the ionic liquid is not consumed, and the sulfonating agent (e.g. SO3) is relatively inexpensive.
Type:
Application
Filed:
June 16, 2003
Publication date:
December 2, 2004
Inventors:
Martyn John Earle, Suhas Prabhakar Katdare
Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
March 30, 2004
Publication date:
November 18, 2004
Applicant:
G.D. Searle & Co.
Inventors:
Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: The present invention pertains to compounds of the formula (I) which are, inter alia, antiprolilferative agents, anticancer agents, anitimycohacterial agents, antituberculosis agents, and/or thioredoxin/thioredoxin reductase inhibitor: wherein: Q is ═O or ═N—S(═O)2—RQ; RQ is -II or optionally substituted C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; Ar is optionally substituted C5-20aryl; RO is an oxy substituent; the bond marked &agr; is a single bond or a double bond; the bond marked &bgr; is a single bond or a double bond; R3 and R5 are each independently ring substituents; R2 and R6 are each independently ring substituents; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for example, in the treatment of proliferative conditions, (e.g.
Type:
Application
Filed:
April 27, 2004
Publication date:
November 4, 2004
Inventors:
Malcolm Francis Graham Stevens, Geoffrey Wells, Andrew David Westwell, Tracey Dawn Poole
Abstract: Novel compounds of the formula (I) in which R1, R2, R3, R4, X and Z are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.
Type:
Application
Filed:
October 16, 2003
Publication date:
November 4, 2004
Inventors:
Werner Mederski, Bertram Cezanne, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
Abstract: The present invention provides new acylsulfonamide derivatives such as 4-(3-trifluoromethyl)phenylethynyl-N-(2-(5-ketohexanoylamino)sulfonylphenyl)benzamide, 4-(3-trifluoromethyl)phenylethynyl-N-(2-(2-propyloxyacetylamino)sulfonylphenyl)benzamide or analogues thereof. These acylsulfonamide derivatives have a hypoglycemic effect equal to or superior to the effects of the conventional hypoglycemic agents and they are free from the side effects unlike the glitazone compounds.
Abstract: The invention relates to novel pesticidally active N-bisaryl-and N-aryl-cycloalkylidenyl-&agr;-sulfin-and &agr;-sulfonamino acid amides of the general formula I, including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl; C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR11R12 wherein R11 and R12 are each independently of the other C1-C6alkyl, or together are tetra- or penta-methylene; R2 and R3 ae each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; optionally substituted aryl; optionally substituted heteroaryl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- t
Type:
Application
Filed:
December 17, 2003
Publication date:
October 28, 2004
Inventors:
Andre Jeanguenat, Clemens Lamberth, Martin Zeller
Abstract: The present invention provides a new process and intermediates for the production of antiviral compound 4′,4-bis-{4,6-bis-[3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino]-[1,3,5]triazin-2-ylamino}-biphenyl-2,2′-disulfonic acid and its pharmaceutically acceptable salts.
Type:
Grant
Filed:
January 31, 2002
Date of Patent:
October 19, 2004
Assignee:
Wyeth
Inventors:
Silvio Iera, Christopher A. Demerson, Jacqueline F. Lunetta, Maria Papamichelakis, Michael F. MacEwan, Wayne G. McMahon, John R. Potoski, Arthur G. Mohan
Abstract: The present invention provides compounds of formula (I), useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
Type:
Application
Filed:
January 30, 2003
Publication date:
October 7, 2004
Inventors:
David Michael Bender, Scott Louis Forman, Winton Dennis Jones, Daryl Lynn Smith, Dennis Michael Zimmermann
Abstract: Disclosed are compounds of Formula I, their N-oxides and agricultually suitable salts (I) wherein J is a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system wherein each ring or ring system is substituted with from one to four substituents independently selected from R5; and A, B, G, R1, R2, R3, R4, R5, R6 and n are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the pests or their environment with a biologically effective amount of a compound of Formula (I) and compositions containing the compounds of Formula (I).
Type:
Application
Filed:
January 7, 2004
Publication date:
September 30, 2004
Inventors:
Bruce Lawrence Finkelstein, George Philip Lahm, Tom Paul Selby, Thomas Martin Stevenson
Abstract: The present invention provides matriptase inhibitors and compositions thereof useful for treating cancer. Martripase is a trypsin-like serine protease active in the development of cancerous conditions, such as tumors and metastasis of cancer.
Type:
Application
Filed:
December 18, 2003
Publication date:
September 23, 2004
Applicant:
Dendreon Corporation
Inventors:
David F. Duncan, L. Josue Alfaro-Lopez, Mallareddy Komandla, Odile Esther Levy, Ofir Moreno, Joseph E. Semple, Amir P. Tamiz
Abstract: The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.
Type:
Application
Filed:
February 9, 2004
Publication date:
September 16, 2004
Inventors:
Keith Biggadike, Diane Mary Coe, Dean David Edney, Stephen Barry Guntrip, Abigail Halton, Brian Edgar Looker, Michael John Monteith, Rajnikant Patel, Panayiotis Alexandrou Procopiou
Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): 1
Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
Type:
Application
Filed:
August 29, 2003
Publication date:
September 9, 2004
Applicant:
Pfizer Inc
Inventors:
Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
Type:
Application
Filed:
November 17, 2003
Publication date:
September 2, 2004
Inventors:
Solomon Ugashe, Zheng Wei, J. J. Wright, Andrew Pennell
Abstract: A process for preparing (S)-(-)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide (IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[4-[ethyl(6-fluoro-6-metylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide (I) anll then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-lId.
Type:
Application
Filed:
November 20, 2003
Publication date:
August 26, 2004
Inventors:
Sonja Suzanne Mackey, Michael e Matison, Haifeng Wu, Paul M Herrinton, Michael Paul Goble, Moses W McMillian, Vikram Gurudath Kalthod
Abstract: The invention relates to substituted octahydrophenanthrene compounds of general formula (I), to a method for their production, to medicaments containing these compounds and to the use of said compounds for producing medicaments.
Type:
Application
Filed:
February 13, 2004
Publication date:
August 19, 2004
Inventors:
Helmut Buschmann, Werner Englberger, Michael Przewosny, Hans Schick, Birgitta Henkel, Michael Sattlegger
Abstract: The present invention relates to novel compounds of formula (I), to a process for their menufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.
Type:
Application
Filed:
March 5, 2004
Publication date:
August 12, 2004
Inventors:
Keith Biggadike, Rita Field, Stephen Barry Guntrip, Brian Edgar Looker
Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Application
Filed:
October 3, 2003
Publication date:
July 29, 2004
Applicant:
G.D. Searle & Co.
Inventors:
Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, Joseph J. McDonald
Abstract: The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.
Type:
Application
Filed:
July 14, 2003
Publication date:
July 15, 2004
Applicant:
Sugen, Inc.
Inventors:
Ping Huang, Chung Chen Wei, Peng Cho Tang, Congxin (Chris) Liang, John Ramphal, Bahija Jallal, John Biltz, Xiaoyuan (Sharon) Li, Matt Mattson, Gerald McMahon, Marcel Koenig
Abstract: There is provided a series of novel &agr;-(N-sulfonamido)acetamide compounds of the Formula (I) 1
Type:
Application
Filed:
December 20, 2002
Publication date:
July 1, 2004
Inventors:
Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.
Type:
Application
Filed:
September 26, 2003
Publication date:
July 1, 2004
Inventors:
Natesan Murugesan, John E. Tellew, John E. Macor, Zhengxiang Gu
Abstract: Compounds of general formula (I), wherein R1, R2, R3, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.
Abstract: The present invention is directed to benzophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.
Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
September 6, 2000
Date of Patent:
June 1, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.
Type:
Grant
Filed:
April 2, 2002
Date of Patent:
May 11, 2004
Assignee:
Synaptic Pharmaceutical Corporation
Inventors:
Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
Type:
Application
Filed:
September 25, 2003
Publication date:
May 6, 2004
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Jeffrey O. Saunders, Daniel Elbaum, Perry M. Novak, Douglas Naegele, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Catharine Frank, Dean P. Stamos, William Walters, David Pearlman
Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.
Type:
Application
Filed:
October 10, 2003
Publication date:
April 22, 2004
Inventors:
Yuan-Ching P. Chiang, Gary E. Aspnes, Kimberly G. Estep
Abstract: A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough: 1
Abstract: Novel quaternary amine containing compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.
Type:
Application
Filed:
November 3, 2003
Publication date:
April 8, 2004
Inventors:
Penglie Zhang, Robert M. Scarborough, Bing-Yan Zhu
Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.
Abstract: A novel fluorescent group-containing carbodiimide compound having at least one group selected from a carboxyl group, a sulfo group, a phosphono group and a phospho group which have substitution of an alkali metal, an alkaline earth metal or a basic group containing a nitrogen or phosphorus atom, which is prepared by using a novel fluorescent group-containing carbodiimide compound precursor having a halogen atom or a sulfonic acid group; and a method for detecting a nucleic acid by hybridization utilizing a nucleic acid labeled with a labeling substance, which utilizes the fluorescent group-containing carbodiimide compound as the labeling substance.
Abstract: The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.
Type:
Application
Filed:
February 21, 2003
Publication date:
March 18, 2004
Inventors:
Nicole Chantel Barvian, Patrick Michael O.Brien, William Chester Patt, Joseph Armand Picard, Drago Robert Sliskovic