Nitrogen Attached Directly To The Diazine Ring By Nonionic Bonding Patents (Class 544/407)
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Publication number: 20130178482Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.Type: ApplicationFiled: June 26, 2012Publication date: July 11, 2013Applicant: Parion Sciences, Inc.Inventor: MICHAEL R. JOHNSON
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Patent number: 8481734Abstract: Disclosed herein are pyrazine derivatives of Formula I: Formula I; wherein each of X1 and X2 is independently —CONR7R9; and each of Y1 and Y2 is independently —NR48R49; and methods of using the same. The disclosed pyrazine derivatives include those having urea, amide, sulfonamide, thiourea, and/or carbamate substituents. Among the various aspects of the present invention are pyrazine derivatives that may be detected in vivo and used in a number of medical procedures (e.g., renal function monitoring). Without being bound by a particular theory, the pyrazine derivatives described herein may be designed to be hydrophilic, thus allowing for rapid renal clearance for continuous monitoring of renal function.Type: GrantFiled: January 12, 2009Date of Patent: July 9, 2013Assignee: Medibeacon Development LLCInventors: Richard B. Dorshow, John Freskos, William L. Neumann, Amruta Reddy Poreddy, Raghavan Rajagopalan
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Patent number: 8476269Abstract: 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: GrantFiled: July 9, 2012Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
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Publication number: 20130157981Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: December 18, 2012Publication date: June 20, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Armin HECKEL, Andreas BLUM, Dieter HAMPRECHT, Joerg KLEY
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Publication number: 20130136698Abstract: 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: November 13, 2012Publication date: May 30, 2013Applicant: MEDIBEACON DEVELOPMENT, LLCInventor: MediBeacon Development, LLC
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Publication number: 20130131040Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: ApplicationFiled: November 23, 2012Publication date: May 23, 2013Applicant: Portola Pharmaceuticals, Inc.Inventor: Portola Pharmaceuticals, Inc.
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Publication number: 20130109697Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: October 29, 2012Publication date: May 2, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Armin HECKEL, Sara Frattini, Dieter Hamprecht, Joerg Kley
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Publication number: 20130109665Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. In particular, the compound may be used as a preferential agonist of Cannabinoid Receptor 2.Type: ApplicationFiled: October 24, 2012Publication date: May 2, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130109856Abstract: The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: October 29, 2012Publication date: May 2, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Boehringer Ingelheim International GmbH
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Patent number: 8431579Abstract: Provided are compounds represented by the formula: where the structural variables are as defined herein. The compounds function as sodium channel blockers and my be used for promoting hydration of mucosal surfaces.Type: GrantFiled: November 4, 2010Date of Patent: April 30, 2013Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
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Publication number: 20130060034Abstract: The present application provides sodium channel blockers exemplified by the following structure: The compounds of the invention useful for treating chronic bronchitis, cystic fibrosis, sinusitis, vaginal dryness, dry eye, Sjogren's disease, distal intestinal obstruction syndrome, dry skin, esophagitis, dry mouth (xerostomia), nasal dehydration, ventilator-induced pneumonia, asthma, primary ciliary dyskinesia, otitis media, chronic obstructive pulmonary disease, emphysema, pneumonia, constipation, and chronic diverticulitis, for example.Type: ApplicationFiled: November 6, 2012Publication date: March 7, 2013Inventor: Michael Ross Johnson
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Patent number: 8389767Abstract: The invention relates to methods of using certain compounds of formula (I), (II) and (III) in the synthesis of an insecticide intermediate of formula (IV), wherein the substituents are as defined in claim 1, to processes for preparing these compounds, to processes which use these compounds to prepare insecticide intermediates, and to certain novel compounds of formula (II?) and (III?).Type: GrantFiled: September 2, 2008Date of Patent: March 5, 2013Assignee: Syngenta Crop Protection LLCInventors: Andre Denis Stoller, Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Peter Maienfisch, Werner Zambach
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Patent number: 8378114Abstract: 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: GrantFiled: March 20, 2007Date of Patent: February 19, 2013Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masatsugu Oda, Yoshihiro Matsuzaki, Koji Tanaka, Eiji Takizawa, Motohiro Hasebe, Nobutaka Kuroki, Akiyuki Suwa, Kenji Oshima
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Patent number: 8372845Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: September 14, 2011Date of Patent: February 12, 2013Assignee: Novartis AGInventors: Gurdip Bhalay, Lee Edwards, Catherine Howsham, Peter Hunt, Nichola Smith
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Publication number: 20130035328Abstract: The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections.Type: ApplicationFiled: July 19, 2012Publication date: February 7, 2013Inventors: Peter William Gage, Gary Dinneen Ewart, Lauren Elizabeth Wilson, Wayne Best, Anita Premkumar
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Publication number: 20130012500Abstract: 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: September 13, 2012Publication date: January 10, 2013Inventors: 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: 20130012692Abstract: 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 8, 2012Publication date: January 10, 2013Applicant: Parion Sciences, Inc.Inventor: MICHAEL R. JOHNSON
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Patent number: 8350032Abstract: 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: GrantFiled: July 31, 2008Date of Patent: January 8, 2013Assignee: MediBeacon Development, LLCInventors: William L. Neumann, Richard B. Dorshow
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Publication number: 20120302752Abstract: Methods are described for efficient and regioselective reactions that are Ru-catalyzed and either (i) amide-directed C—H, C—N, C—O activation/C—C bond forming reactions, (ii) ester-directed C—O and C—N activation/C—C bond forming reactions, or (iii) amide-directed C—O activation/hydrodemethoxylation reactions. All of these reactions of directed C—H, C—N, C—O activation/coupling reactions establish a catalytic base-free DoM-cross coupling process at non-cryogenic temperature. High regioselectivity, yields, operational simplicity, low cost, and convenient scale-up make these reactions suitable for industrial applications. Many previously unknown amide-substituted or ester-substituted aryl and heteroaryl compounds are presented with synthetic details also provided.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Inventors: Yigang Zhao, Victor A. Snieckus
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Patent number: 8314105Abstract: 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: GrantFiled: August 8, 2007Date of Patent: November 20, 2012Assignee: Parion Sciences, Inc.Inventor: Michael Ross Johnson
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Publication number: 20120277232Abstract: 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: July 9, 2012Publication date: November 1, 2012Inventors: Urs BAETTIG, Kamlesh Jagdis BALA, Emma BUDD, Lee EDWARDS, Catherine Howsham, Glyn HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Publication number: 20120263706Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: ApplicationFiled: June 29, 2012Publication date: October 18, 2012Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
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Publication number: 20120252809Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 24, 2012Publication date: October 4, 2012Applicant: SANOFIInventors: Sven RUF, Thorsten SADOWSKI, Klaus WIRTH, Herman SCHREUDER, Christian BUNING
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Patent number: 8268834Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.Type: GrantFiled: March 4, 2009Date of Patent: September 18, 2012Assignee: Novartis AGInventors: Ian Bruce, Emma Budd, Lee Edwards, Catherine Howsham
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Publication number: 20120220606Abstract: 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 9, 2012Publication date: August 30, 2012Applicant: PARION SCIENCES, INC.Inventors: Michael R. JOHNSON, Bruce F. Molino, Bruce Sargent, Jianzhong Zhang
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Publication number: 20120214800Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.Type: ApplicationFiled: April 30, 2012Publication date: August 23, 2012Inventors: Ian Bruce, Emma Budd, Lee Edwards, Catherine Howsham
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Patent number: 8236808Abstract: 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: GrantFiled: June 8, 2009Date of Patent: August 7, 2012Assignee: Novartis AGInventors: Stephen Paul Collingwood, Nicholas James Devereux, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt
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Publication number: 20120190692Abstract: The present application describes selective ligands of formula (I) for neuronal nicotinic receptors (NNRs), more specifically for the ?4?2 NNR subtype, compositions thereof, and methods of using the same, wherein X, R1, X, R2, R3, L1, m, n, p, and q are defined in the specification.Type: ApplicationFiled: March 6, 2012Publication date: July 26, 2012Inventors: William H. Bunnelle, Lei Shi, Marc J.C. Scanio
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Patent number: 8211895Abstract: The present application relates to pyrazinoyl guanidine sodium channel blockers having the structure: or a pharmaceutically acceptable salt thereof, where the structural variables are as defined herein. The present invention also relates pharmaceutical compositions comprising the sodium channel blockers and their use in methods of treatment, including the treatment of cardiovascular disease, cystic fibrosis, and chronic bronchitis and in the rehydration of mucosal surfaces and promotion of mucus clearance in a patient.Type: GrantFiled: September 7, 2010Date of Patent: July 3, 2012Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Bruce F. Molino, Bruce Sargent, Jianzhong Zhang
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Patent number: 8211921Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, W, and X are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: January 20, 2009Date of Patent: July 3, 2012Assignee: Array BioPharma Inc.Inventors: James F. Blake, Joseph P. Lyssikatos, Allison L. Marlow, Jeongbeob Seo, Eli M. Wallace, Hong-Woon Yang
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Publication number: 20120165343Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20120149718Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: December 13, 2011Publication date: June 14, 2012Inventors: Christine E. Brotherton-Pleiss, Keith A. M. Walker
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Patent number: 8198286Abstract: 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: GrantFiled: July 24, 2008Date of Patent: June 12, 2012Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Publication number: 20120134930Abstract: Provided are compounds and compositions of general Formula IX: E1-L-Ar-X-PA, that may be utilized in bioconjugation procedures, where Ar is a chromophore and PA is a functional group capable of being attached to any bioactive molecule of interest. The present invention provides Formulas I-III that are capable of being attached to a bioactive vector for the selective delivery of said photoactive pyrazine derivatives to a desired biological target.Type: ApplicationFiled: January 6, 2012Publication date: May 31, 2012Applicant: Mallinckrodt LLCInventors: Raghavan Rajagopalan, Richard B. Dorshow
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Publication number: 20120122884Abstract: The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula IV: wherein the variables are as defined herein.Type: ApplicationFiled: May 12, 2011Publication date: May 17, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Anisa Nizarali Virani, Philip Michael Reaper
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Publication number: 20120116083Abstract: 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: January 18, 2012Publication date: May 10, 2012Applicant: PARION SCIENCES, Inc.Inventor: Michael Ross JOHNSON
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Publication number: 20120100078Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas I and II below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.Type: ApplicationFiled: January 4, 2012Publication date: April 26, 2012Applicant: Mallinckrodt LLCInventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann
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Patent number: 8163758Abstract: Provided is class of sodium channel blockers. One example of such a compound is shown by the following formula: The compounds are useful for promoting hydration of mucosal surfaces and treating a variety of disease conditions.Type: GrantFiled: June 11, 2007Date of Patent: April 24, 2012Assignee: Parion Sciences, Inc.Inventors: Michael Ross Johnson, Andrew J. Hirsh, Richard C. Boucher, Jianzhong Zhang
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Patent number: 8143256Abstract: The present invention provides compounds represented by formula (I): where the structural variables are defined herein. The compound of the present invention are useful as sodium channel blockers.Type: GrantFiled: August 18, 2005Date of Patent: March 27, 2012Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Patent number: 8119635Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: August 19, 2009Date of Patent: February 21, 2012Assignee: 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: 20120040968Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.Type: ApplicationFiled: May 6, 2010Publication date: February 16, 2012Applicant: Waters Technologies CorporationInventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
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Patent number: 8115000Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas (I) and (II) below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.Type: GrantFiled: June 20, 2007Date of Patent: February 14, 2012Assignee: Mallinckrodt LLCInventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann
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Publication number: 20120035407Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula II: wherein the variables are as defined herein.Type: ApplicationFiled: May 12, 2011Publication date: February 9, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Michael O'Donnell, Philip Michael Reaper
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Publication number: 20120035408Abstract: The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula V: wherein the variables are as defined herein.Type: ApplicationFiled: May 12, 2011Publication date: February 9, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, Stephen Clinton Young, Pierre-Henri Storck, Anisa Nizarali Virani, Phillip Michael Reaper, Joanne Pinder
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Publication number: 20120027682Abstract: The invention provides compounds, including compositions, preparations and formulations, and methods of using and making such compounds. Compounds of the present invention include pyrazine derivatives having a pyrazine core and a plurality of substituents. In some embodiments, pyrazine derivatives of the invention are pyrazine core compounds having one or more electron donating groups and one or more electron withdrawing groups optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.Type: ApplicationFiled: April 15, 2010Publication date: February 2, 2012Inventors: William L. Neumann, John N. Freskos
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Publication number: 20120029180Abstract: The invention relates to an isolated or recombinant Na?/H+ exchanger comprising an isolated or recombinant Na+/H+ exchanger, particularly to the PBO-4 Na+/H+ exchanger. Also disclosed is an isolated or recombinant protein component of an H+-grated channel which can be affected by extracellular Ca2+ concentration. In particular, the invention relates to PBO-5 and/or PBO-8 and/or a H+-gated channel composed of PBO-5 and PBO-8. The invention relates to compounds isolated from a vertebrate organism, wherein said compounds comprise at least a part of a H+-gated channel or Na+/H+ exchanger. The invention also relates to a method for identifying a component of a H+-grated channel in a vertebrate organism.Type: ApplicationFiled: August 17, 2011Publication date: February 2, 2012Inventors: Erik M. Jorgensen, Asim A. Beg, Paola Nix
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Publication number: 20110275603Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.Type: ApplicationFiled: May 5, 2011Publication date: November 10, 2011Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant K. BHAVAR, Srikant VISWANADHA, Swaroop Kumar V.S. VAKKALANKA, Gayatri S. MERIKAPUDI
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Patent number: 8048886Abstract: The present invention relates to novel IAP inhibitor compounds of formula I:Type: GrantFiled: December 7, 2007Date of Patent: November 1, 2011Assignee: Novartis AGInventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
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Publication number: 20110250139Abstract: Provided herein are compounds, preparations and formulations comprising pyrazine derivatives having multiple poly(ethylene glycol) containing substituents. Many of the compounds disclosed herein are excretable by the renal system of a subject or patient and are useful for visualizing the renal system of a subject or patient. Upon excitation by electromagnetic radiation, a number of the compounds disclosed herein exhibit luminescence and are externally detectable when present in the body fluid of a patient or subject. Also provided herein are methods for visualizing the renal system of a subject or patient.Type: ApplicationFiled: December 17, 2009Publication date: October 13, 2011Inventors: Amruta Poreddy, William L. Neumann