Nitrogen Attached Directly To The Diazine Ring By Nonionic Bonding Patents (Class 544/407)
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Publication number: 20110250140Abstract: In some embodiments, the invention provides modified pyrazine derivatives containing a central pyrazine ring with two secondary amine groups attached directly to the central pyrazine ring and two amino carbonyl groups attached directly to the central pyrazine ring. The secondary amine groups are terminated by alkyl groups containing from 1 to 6 carbons. The amino carbonyl groups can be terminated by a wide range of substituents including, but not limited to, alkyl and alkylene groups, polyether groups, including poly(ethylene glycol) groups, secondary and tertiary amine groups, polyhydroxylated alkyl groups, amino carbonyl groups, amino thioketone groups, and combinations thereof. In some embodiments, the invention provides modified pyrazine derivatives useful as optical agents in a wide variety of biomedical imaging procedures, including diagnostic and imaging procedures.Type: ApplicationFiled: December 17, 2009Publication date: October 13, 2011Inventors: Amruta Poreddy, William L. Neumann
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Publication number: 20110236313Abstract: Methods for identifying modulators of the epithelial sodium ion channel and for identifying modulators of salty taste perception are described. Also featured are isolated human salty taste receptors, artificial lipid bilayers comprising an epithelial sodium ion channels, and kits for practicing the claimed methods.Type: ApplicationFiled: January 18, 2011Publication date: September 29, 2011Applicant: MONELL CHEMICAL SENSES CENTERInventors: Joseph G. Brand, Taufiqul Huque
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Publication number: 20110230483Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: March 14, 2011Publication date: September 22, 2011Inventors: Urs BAETTIG, Kamlesh Jagdis BALA, Emma BUDD, Lee EDWARDS, Catherine Howsham, Glyn HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Patent number: 8022210Abstract: The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where X, Y and R1-R4 are as defined herein. The compounds of the present invention are useful as sodium channel blockers.Type: GrantFiled: March 17, 2008Date of Patent: September 20, 2011Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Publication number: 20110212969Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
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Patent number: 8008494Abstract: The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where X, Y and R1-R4 are as defined herein. The compounds of the present invention are useful as sodium channel blockers.Type: GrantFiled: March 17, 2008Date of Patent: August 30, 2011Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Publication number: 20110201625Abstract: A compound of Formula I or a hydrate or solvate thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: June 8, 2009Publication date: August 18, 2011Inventors: Stephen Paul Collingwood, Nicholas James Devereux, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt
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Publication number: 20110195973Abstract: The present invention relates to sodium channel blockers. The present Invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: June 11, 2007Publication date: August 11, 2011Applicant: PARION SCIENCES, Inc.Inventor: Michael Ross Johnson
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Publication number: 20110158947Abstract: We disclose agents useful in the treatment of diseases or conditions that would benefit from improved muscle function and including pharmaceutical compositions and diagnostic tests for determining the predisposition of a subject, in particular a male subject, to cardiovascular disease.Type: ApplicationFiled: July 9, 2009Publication date: June 30, 2011Inventor: Aleksandar Jovanovic
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Publication number: 20110144338Abstract: Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided comprising administering a sodium channel blocker or pharmaceutically acceptable salts thereof to one or more members of a population at risk of exposure to or already exposed to one or more airborne pathogens, either from natural sources or from intentional release of pathogens into the environment.Type: ApplicationFiled: August 8, 2007Publication date: June 16, 2011Applicant: Parion Sciences, Inc.Inventors: Michael R. JOHNSON, Samuel E. Hopkins
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Publication number: 20110136831Abstract: An N-2-(hetero)arylethylcarboxamide derivative represented by the formula (I) wherein R1 and R2 are each independently a hydrogen atom etc., R3 and R4 are each independently a hydrogen atom etc., each Y is independently a halogen atom; a (C1-C6)alkyl group optionally substituted by halogen atom(s) etc., n is an integer of 1 to 5, A is a specific substituted cyclic group, E is C—H; C—Y (Y is as defined above); or a nitrogen atom, a salt thereof, and a pest controlling agent containing the derivative or salt as an active ingredient show superior performance as compared to the prior art technique, and are is useful particularly as plant disease controlling agents or nematocides having a broad control spectrum at a low dose.Type: ApplicationFiled: March 20, 2007Publication date: June 9, 2011Inventors: Masatsugu Oda, Yoshihiro Matsuzaki, Koji Tanaka, Eiji Takizawa, Motohiro Haseba, Nobutaka Kuroki, Akiyuki Suwa, Kenji Oshima
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Publication number: 20110118272Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: ApplicationFiled: July 26, 2010Publication date: May 19, 2011Inventors: Richard E. Lee, Jianjun Qi, Juilian G. Hurdle, Bernd Meibohm, Vnr Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Patent number: 7932256Abstract: The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, pharmaceutical compositions of the compound, and methods of using the compound for the treatment of psychiatric disorders and neurological diseases including depression, anxiety related disorders, irritable bowel syndrome, addiction and negative aspects of drug and alcohol withdrawal, and other conditions associated with CRF.Type: GrantFiled: April 24, 2009Date of Patent: April 26, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Richard A. Hartz, Vijay T. Ahuja, Vivekananda M. Vrudhula, Joanne J. Bronson
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Publication number: 20110071163Abstract: The disclosure relates to a method of treating or preventing a condition in a subject associated with the activation of an opioid receptor in the periphery by administering an effective amount of 5-(2-methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl}-phenoxy)-pyrazine-2-carboxamide (Compound I). In particular, the disclosure relates to a method of treating or preventing opioid-induced constipation or opioid-induced bowel dysfunction in a human without reducing centrally-mediated opioid analgesia or producing central opioid withdrawal symptoms by administering an effective amount of Compound I. The disclosure further relates to the use of Compound I for the preparation of a medicament for the treatment or prevention of a condition in a subject associated with the activation of an opioid receptor in the periphery.Type: ApplicationFiled: September 17, 2010Publication date: March 24, 2011Applicant: ADOLOR CORPORATIONInventor: Richard M. WOODWARD
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Publication number: 20110059989Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: May 11, 2009Publication date: March 10, 2011Inventors: Stephen Paul Collingwood, Catherine Howsham, Thomas Anthony Hunt
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Publication number: 20110059957Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 29, 2009Publication date: March 10, 2011Applicant: R-TECH UENO, LTD.Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Akiko Kawasaki, Akiko Akasaka, Yosuke Kawai
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Publication number: 20110054174Abstract: The present invention relates to a process for the preparation of a compound of formula I, wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen. (R)-2-phenyl propionic acid derivatives of formula I are key intermediates in the synthesis of 5-substituted-pyrazine or pyridine glucokinase activators of the formula Xa, which have the potential to be useful for the treatment and/or prophylaxis of type II diabetes.Type: ApplicationFiled: August 20, 2010Publication date: March 3, 2011Inventors: Stephan Bachmann, Alec Fettes, Hans Iding, Beat Wirz, Ulrich Zutter
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Publication number: 20110046158Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: November 4, 2010Publication date: February 24, 2011Applicant: PARION SCIENCES, Inc.Inventors: Michael R. JOHNSON, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
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Publication number: 20110009424Abstract: The invention relates to co-crystals and compositions each comprising VX-950 and a co-crystal former selected from the group consisting of 3-methoxy-4-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, and 2,5-dihydroxybenzoic acid. Also within the scope of this invention are methods of making and using the same.Type: ApplicationFiled: August 29, 2008Publication date: January 13, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Yuegang Zhang, Patrick R. Connelly, Steve Johnston
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Publication number: 20110008268Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: June 11, 2007Publication date: January 13, 2011Applicant: PARION SCIENCES, Inc.Inventors: Michael Ross Johnson, Andrew J. Hirsh, Richard C. Boucher, Jianzhong Zhang
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Publication number: 20110003832Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: September 7, 2010Publication date: January 6, 2011Applicant: PARION SCIENCES, Inc.Inventors: Michael R. JOHNSON, Bruce F. Molino, Bruce Sargent, Jianzhong Zhang
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Publication number: 20100323889Abstract: The present invention relates to compounds of formula (I), wherein R1, R2, R3, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to intermediates used in the preparation of compounds of formula (I), to methods of controlling plants and compositions comprising compounds of formula (I).Type: ApplicationFiled: November 10, 2008Publication date: December 23, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Nigel James Willetts, Matthew Robert Cordingley, Patrick Jelf Crowley, Suzanna Jane Riley, Michael Drysdale Turnbull
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Patent number: 7842697Abstract: The present invention relates to pyrazinoylguanidine compounds represented by the formula: where the structural variables are defined herein. The compounds are useful as sodium channel blockers.Type: GrantFiled: March 17, 2008Date of Patent: November 30, 2010Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Publication number: 20100298568Abstract: This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 wherein the variables R1, R?1 and R2 are defined herein and the compound of Formula 1 has an enantiomeric excess (ee) of 55% or greater.Type: ApplicationFiled: August 4, 2010Publication date: November 25, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Gerald J. Tanoury, Minzhang Chen, Young Chun Jung, Raymond E. Forslund
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Publication number: 20100298340Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: April 12, 2007Publication date: November 25, 2010Applicants: AstraZeneca AB, Astex Therapeutics Ltd.Inventors: Stefan Berg, Karin Kolmodin
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Publication number: 20100267746Abstract: The present invention provides sodium channel blockers possessing beta-adrenergic receptor agonist activity.Type: ApplicationFiled: June 11, 2007Publication date: October 21, 2010Applicant: PARION SCIENCES, INC.Inventor: Michael Ross Johnson
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Patent number: 7807834Abstract: The present invention relates to group of pyrazinoylguanidine compounds useful as sodium channel blockers. The compounds may be used to promote promoting hydration of mucosal surfaces.Type: GrantFiled: August 3, 2005Date of Patent: October 5, 2010Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Bruce F. Molino, Bruce Sargent, Jianzhong Zhang
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Publication number: 20100221315Abstract: The present invention relates to vesicular formulations containing a prodrug, characterized for comprising the combination of a prodrug of weak organic acids having the following general formula: R1COOH (I) or R1SO2H (II) wherein R1 is preferably selected from the group containing a benzenic, pyridinic, pyrazinic or pyrimidinic aromatic ring, or a linear chain substituted or unsubstituted, saturated or unsaturated, such as benzoic, benzenesulphinic, cinnamic, salicylic, pyrazinoic, nicotinic, carboxylic pyridazine and carboxylic pyrimidine, caproic, caprylic, capric, lauric, myristic, palmitic and estearic acids; with a liposomal or micellar carrier, which protects the prodrug from plasma degradation. The invention further relates to the process of preparation of liposomal formulations, novel prodrugs and pharmaceutical compositions intended for use in the treatment of tuberculosis and other mycobacterioses.Type: ApplicationFiled: June 4, 2007Publication date: September 2, 2010Applicant: UNIVERSIDADE DE LISBOAInventors: Luis Filipe Vicente Constantino, Elsa Maria Ribeiro Santos Anes, Marta Filipa Jesus de Freitas Simoes, Emilia Alice dos Reis Torroaes Valente
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Publication number: 20100222350Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
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Publication number: 20100196460Abstract: The present invention discloses a number of photoactive compounds designed to bind and inhibit serine proteases. Compounds disclosed herein may be utilized in a number of appropriate medical diagnostic and/or therapeutic procedures such as the monitoring of hemostasis, imaging and/or treatment of vulnerable plaques, and/or tumor imaging and/or treatment.Type: ApplicationFiled: July 31, 2008Publication date: August 5, 2010Inventors: William L. Neumann, Richard B. Dorshow
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Patent number: 7745442Abstract: Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided including administering a sodium channel blocker or pharmaceutically acceptable salts thereof to one or more members of a population at risk of exposure to or already exposed to one or more airborne pathogens, either from natural sources or from intentional release of pathogens into the environment.Type: GrantFiled: August 18, 2004Date of Patent: June 29, 2010Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Samuel E. Hopkins
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Publication number: 20100130447Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: November 15, 2007Publication date: May 27, 2010Inventors: Christopher John Burns, Michael Francis Harte, James T. Palmer
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Publication number: 20100130506Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: December 10, 2008Publication date: May 27, 2010Inventors: Gurdip BHALAY, Emma Budd, Graham Charles Bloomfield, Stephen Paul Collingwood, Andrew Dunstan, Lee Edwards, Peter Gedeck, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt, Paul Oakley, Nichola Smith
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Publication number: 20100105899Abstract: This invention is directed to the general method of transforming non-photoactive bioactive small molecule compounds of known structure and function into photoactive analogs of the small molecules which exhibit both photoactivity and the original biological targeting activity. The general method for the design of the photoactive analogs of the small molecules includes: (a) selecting a desired bioactive molecule; (b) identifying the region of the molecule that contains an aromatic or a heteroaromatic motif; and (c) either replacing said motif with a photoactive functional group of similar size, or modifying said motif to make it photoactive. Other aspects include photoactive analog compounds and photodiagnostic and phototherapeutic uses thereof.Type: ApplicationFiled: February 26, 2008Publication date: April 29, 2010Inventors: William L. Neumann, Raghavan Rajagopalan, Dennis A. Moore, Richard B. Dorshow
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Patent number: 7704995Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.Type: GrantFiled: May 2, 2003Date of Patent: April 27, 2010Assignee: Exelixis, Inc.Inventors: Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
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Publication number: 20100099673Abstract: The present invention relates to compounds represented by Formula (I): and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.Type: ApplicationFiled: January 11, 2008Publication date: April 22, 2010Inventors: Mark T. Bilodeau, Nathan R. Kett, Craig Lindsley, Peter J. Manley, Jeffrey Y. Melamed, Daniel Vincent Paone, B. Wesley Trotter, Zhicai Wu
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Patent number: 7691858Abstract: Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as uveitis, retinopathies or macular degeneration, macular edema or other vitreoretinal diseases, inflammatory diseases such as autoimmune diseases, vascular leakage syndrome, edema, or diseases involving leukocyte activation, transplant rejection, respiratory diseases such as asthma, adult or acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease, and the like.Type: GrantFiled: April 25, 2007Date of Patent: April 6, 2010Assignee: TargeGen, Inc.Inventors: John Doukas, Chi Ching Mak, Elena Dneprovskaia, Glenn Noronha
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Publication number: 20100075987Abstract: Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: December 10, 2007Publication date: March 25, 2010Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang, Ralph T. Mosley
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Patent number: 7683068Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: June 23, 2006Date of Patent: March 23, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
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Publication number: 20100056546Abstract: The present invention relates to new sulfonylurea inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 2, 2009Publication date: March 4, 2010Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Manoucher M. Shahbaz
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Publication number: 20100021382Abstract: Disclosed herein are pyrazine derivatives and methods of using the same.Type: ApplicationFiled: January 12, 2009Publication date: January 28, 2010Applicant: Mallinckrodt Inc.Inventors: Richard B. Dorshow, John Freskos, William L. Neumann, Amruta Reddy Poreddy, Raghavan Rajagopalan
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Publication number: 20100010223Abstract: The present invention relates to methods for producing N,N?-alkylated diaminopyrazines.Type: ApplicationFiled: January 7, 2009Publication date: January 14, 2010Applicant: Mallinckrodt Inc.Inventors: Richard B. Dorshow, John Freskos, William L. Neumann, Amruta Reddy Poreddy, Raghavan Rajagopalan
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Patent number: 7645764Abstract: Compounds of formula I: wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds, pharmaceutical compositions, methods of using the compounds for treatment of p38 MAP kinase-mediated diseases, and methods of using the compounds for treatment of Raf kinase-mediated diseases.Type: GrantFiled: November 8, 2007Date of Patent: January 12, 2010Assignee: Roche Palo Alto LLCInventors: Tobias Gabriel, Joel McIntosh, Kin-Chun Thomas Luk
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Publication number: 20090324724Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: May 20, 2005Publication date: December 31, 2009Applicant: PARION SCIENCES, INC.Inventor: Michael R. Johnson
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Patent number: 7629346Abstract: The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.Type: GrantFiled: May 30, 2007Date of Patent: December 8, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Hans Iding, Matthias Heinrich Nettekoven, Ulrike Obst Sander, Stephan Roever, Urs Weiss, Beat Wirz
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20090233944Abstract: The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.Type: ApplicationFiled: May 22, 2009Publication date: September 17, 2009Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Phillip Porter, Eric Vieira
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Publication number: 20090227594Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: August 18, 2005Publication date: September 10, 2009Inventor: Michael R. Johnson
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Publication number: 20090227530Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: July 24, 2008Publication date: September 10, 2009Applicant: PARION SCIENCES, INC.Inventor: Michael R. JOHNSON
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Publication number: 20090214444Abstract: Polyaromatic sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: February 26, 2009Publication date: August 27, 2009Applicant: PARION SCIENCES, Inc.Inventor: Michael Ross Johnson