Exactly Five Ring Nitrogens In The Bicyclo Ring System (e.g., Triazolo[4,5-d]pyrimidine, Etc.) Patents (Class 514/261.1)
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Patent number: 11466019Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: GrantFiled: November 3, 2020Date of Patent: October 11, 2022Assignee: Vernalis (R&D) LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Patent number: 11354990Abstract: Disclosed are methods for treating kidney disease including autosomal dominant polycystic kidney disease (ADPKD) in a subject, comprising the step of administering to the subject a composition comprising a therapeutically effective amount of ticagrelor or a derivative thereof, thereby treating ADPKD. Disclosed are methods of decreasing arginine vasopressin (AVP) production in a subject comprising the step of administering to the subject a composition comprising an effective amount of ticagrelor, thereby decreasing AVP production. Disclosed are methods for treating dilutional hyponatremia in a subject comprising the step of administering to the subject a composition comprising an effective amount of ticagrelor, thereby decreasing AVP production.Type: GrantFiled: April 6, 2020Date of Patent: June 7, 2022Inventors: Bellamkonda K. Kishore, Yue Zhang, Noel G. Carlson
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Patent number: 11266649Abstract: The disclosure provides, inter alia, pharmaceutical compositions comprising micronized drug particles of adenosine A2A receptor antagonists, and methods of treating cancer using the pharmaceutical compositions.Type: GrantFiled: February 1, 2019Date of Patent: March 8, 2022Assignee: Corvus Pharmaceuticals, Inc.Inventors: Jingrong Xu, William Jones, Felicia Flicker, Bret Berner
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Patent number: 10968205Abstract: The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 19, 2019Date of Patent: April 6, 2021Assignee: Theravance Biopharma R&D IP, LLCInventors: Robert Murray McKinnell, Erik Fenster, Tom M. Lam, Jerry Nzerem, Marta Dabros, Venkat R. Thalladi, Miroslav Rapta
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Patent number: 10954308Abstract: The disclosure generally provides antibodies and antigen binding fragments of antibodies that bind ticagrelor and metabolites of ticagrelor. The disclosure also provides compositions comprising the antibodies, nucleic acid molecules encoding the antibodies, methods of treating a patient comprising administering the antibodies, and methods of making and using the antibodies.Type: GrantFiled: July 16, 2018Date of Patent: March 23, 2021Assignee: MEDIMMUNE LIMITEDInventors: Andrew Buchanan, Sven Nylander, Mark Penney, Philip Newton, Feenagh Keyes, Tord Inghardt
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Patent number: 10729655Abstract: The present invention relates to rapidly disintegrating oral dosage forms, more particularly to rapidly disintegrating tablets containing (1S,2S,3R,5S)-3-[7-{[1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-[1,2,3]-triazolo[4,5-d]pyrimidin-3-yl]-5 5-(2-hydroxyethoxy)cyclopentane-1,2-diol and a disintegrating excipient. Blister packs suitable for use with the rapidly disintegrating oral dosage form are also disclosed.Type: GrantFiled: April 20, 2017Date of Patent: August 4, 2020Assignee: AstraZeneca ABInventors: Farhan Abdel Karim Mohammad Al Husban, Lars Håkan Christer Glad, Jenny Malin Christina Hallstein, Andrea Jane Moir, Michael Peter Thompson
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Patent number: 10618899Abstract: Various [1,2,3]triazolo[4,5-d]pyrimidines are provided that are effective to lower p-tau and/or to prevent or reduce elevation of p-tau, particularly in response to stress (e.g., elevated cortisol levels). The compounds are useful in the treatment or prophylaxis of pathologies characterized by abnormal amyloid plaque and or tangle formation and/or deposition.Type: GrantFiled: February 17, 2016Date of Patent: April 14, 2020Assignee: Buck Institute for Research on AgingInventors: Varghese John, Dale E. Bredesen
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Patent number: 10614684Abstract: Disclosed are methods for treating kidney disease including autosomal dominant polycystic kidney disease (ADPKD) in a subject, comprising the step of administering to the subject a composition comprising a therapeutically effective amount of ticagrelor or a derivative thereof, thereby treating ADPKD. Disclosed are methods of decreasing arginine vasopressin (AVP) production in a subject comprising the step of administering to the subject a composition comprising an effective amount of ticagrelor, thereby decreasing AVP production. Disclosed are methods for treating dilutional hyponatremia in a subject comprising the step of administering to the subject a composition comprising an effective amount of ticagrelor, thereby decreasing AVP production.Type: GrantFiled: January 31, 2018Date of Patent: April 7, 2020Assignee: THE UNITED STATES GOVERNMENT AS REPRESENTED BY THEInventors: Bellamkonda K. Kishore, Yue Zhang, Noel G. Carlson
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Patent number: 10538526Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: GrantFiled: September 15, 2018Date of Patent: January 21, 2020Assignee: Vernalis (R&D) LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Patent number: 10183946Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 and n are defined as in the description and in the claims. The compound of formula (I) can be for treating.Type: GrantFiled: April 4, 2017Date of Patent: January 22, 2019Assignee: HOFFMANN-LA ROCHE INC.Inventors: Uwe Grether, Matthias Nettekoven, Mark Rogers-Evans, Sebastien Schmitt, Benjamin James Stenton
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Patent number: 10106547Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: GrantFiled: August 21, 2017Date of Patent: October 23, 2018Assignee: Vernalis (R&D) LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Patent number: 10017515Abstract: The present invention relates to a stable amorphous ticagrelor and a process for its preparation.Type: GrantFiled: August 11, 2015Date of Patent: July 10, 2018Assignee: Sun Pharmaceutical Industries LimitedInventors: Nagaraju Gottumukkala, Anil Saini, Ram Thaimattam, Mahavir Singh Khanna, Mohan Prasad
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Patent number: 9982061Abstract: The disclosure generally provides antibodies and antigen binding fragments of antibodies that bind ticagrelor and metabolites of ticagrelor. The disclosure also provides compositions comprising the antibodies, nucleic acid molecules encoding the antibodies, methods of treating a patient comprising administering the antibodies, and methods of making and using the antibodies.Type: GrantFiled: September 30, 2015Date of Patent: May 29, 2018Assignee: MEDIMMUNE LIMITEDInventors: Andrew Buchanan, Sven Nylander, Mark Penney, Philip Newton, Feenagh Keyes, Tord Inghardt
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Patent number: 9795669Abstract: The compound N-(4-{[4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl]oxyl}butyl)octadecanamide is a useful drug compound for enhancing immune response and can be used, for example, as a vaccine adjuvant and a cancer treatment.Type: GrantFiled: December 15, 2015Date of Patent: October 24, 2017Assignee: 3M INNOVATIVE PROPERTIES COMPANYInventor: Paul D. Wightman
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Patent number: 9376443Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: GrantFiled: February 10, 2015Date of Patent: June 28, 2016Assignee: VERNALIS (R&D) LIMITEDInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Publication number: 20150099751Abstract: The in situ gel loaded with phosphodiesterase Type V (PDE5) inhibitors nanoemulsion was prepared using an innovative approach to reformulate the PDE5 inhibitors in a nanoemulsion, and then loading the nanoemulsion into an in situ gel base. These preparations are administered by intramuscular injection in order to give a depot effect for a period of time that exceeds 15 days. The in situ gel composition gives slow, controlled release of the PDE5 inhibitor. The in situ gel composition is useful for prophylaxis and treatment of some important chronic diseases, such as diabetic complications, benign prostatic hyperplasia, erectile dysfunction, and diseases associated with endothelial dysfunction.Type: ApplicationFiled: October 7, 2013Publication date: April 9, 2015Applicant: KING ABDULAZIZ UNIVERSITYInventors: HISHAM AHMED MOHAMMED MOSLI, SALAH ABDELMONEIM GHAREIB ATTEIAH, KHALED MOHAMED HOSNY OMAR, HANY MOHAMED ABD EL-MALIK EL-BASSOSSY, MOHAMED HANY ABDULWAHAB MOSILHY HELAL
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Publication number: 20150094310Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.Type: ApplicationFiled: April 23, 2013Publication date: April 2, 2015Inventor: Florian Holsboer
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Patent number: 8987279Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: GrantFiled: May 8, 2013Date of Patent: March 24, 2015Assignee: Vernalis (R&D) LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Publication number: 20150072970Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: May 19, 2014Publication date: March 12, 2015Applicant: MELINTA THERAPEUTICS, INC.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20140378431Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Guenter Hoelzemann, Kai Schiemann, Ansgar Wegener
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Patent number: 8883802Abstract: The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4-hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2-methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).Type: GrantFiled: December 3, 2010Date of Patent: November 11, 2014Assignee: Astrazeneca ABInventors: Stephen David Cosgrove, Matthew Jonathan Jones, Anna Polyakova-Akkus, Valeriya Nikolayevna Smolenskaya, Brenton Skylar Wolfe
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Publication number: 20140329781Abstract: The present invention relates to a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more antiplatelet agent along with one or more rate controlling excipients.Type: ApplicationFiled: November 1, 2012Publication date: November 6, 2014Applicant: WOCKHARDT LIMITEDInventors: Mandar Kodgule, Amit Gupta, Premchand Nakhat, Girish Kumar Jain
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Publication number: 20140296258Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: October 31, 2013Publication date: October 2, 2014Applicant: AstraZeneca UK LimitedInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
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Publication number: 20140288046Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: April 11, 2014Publication date: September 25, 2014Applicant: HOFFMANN-LA ROCHE INC.Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
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Publication number: 20140288032Abstract: Agents that inhibit or prevent restenosis are identified by assaying test agents in a battery of assays to measure the effect of the test agent on cell proliferation, thrombosis, tissue modeling, and inflammation. Treatment for restenosis is provided using compositions of the invention.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: DiscoveRx CorporationInventors: Eric J. Kunkel, Evangelos Hytopoulos, Ivan Plavec
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Publication number: 20140286943Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 9, 2014Publication date: September 25, 2014Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20140256747Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.Type: ApplicationFiled: October 26, 2012Publication date: September 11, 2014Applicant: LEK PHARMACEUTICALS D.D.Inventors: Borut Zupancic, Nenad Maras, Damjan Sterk
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Publication number: 20140235593Abstract: In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 24, 2012Publication date: August 21, 2014Applicants: ST. JUDE CHILDREN'S RESEARCH HOSPITAL, RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, MMV MEDICINES FOR MALARIA VENTUREInventors: Rodney Kiplin Guy, Fangyi Zhu, Wendyam Armand Guiguemde, David Floyd, Spencer Knapp, Philip Stein, Steve Castro
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Patent number: 8791124Abstract: The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy-phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylendioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy)benzyl)amino)-6,7,8-trimethoxy-quinazoline; g) 1-methly-3-propyl-6-(5-(N-(4-methylmorpholino)sulfonyl)-2-ethoxyphenyl)pyrazole[4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6-(4-pyridinyl)pyrazolo(3,4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxypropoxy)-2-carboxy-2,3-didehydro-chronan-4-one (PPL-557212); k) quinazolines and their trimethoxy derivatives; l) Pyrazolopyrimidones; as well as pharmacologically compatible salts thereof, quinazolinType: GrantFiled: December 29, 2011Date of Patent: July 29, 2014Assignee: Uropep Biotech GBRInventors: Wolf-Georg Forssmann, Christian Georg Stief, Michael Carsten Truβ, Stefan Uckert, Udo Jonas
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Publication number: 20140179518Abstract: The present invention relates to pesticidal mixtures comprising as active components 1) at least one cyanosulfoximine compound I of the formula I wherein R1, R2 and G are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: BASF SEInventors: Delphine BREUNINGER, Henricus Maria Martinus BASTIAANS, Wolfgang VON DEYN, Matthias POHLMAN, Juergen LANGEWALD, Egon HADEN
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Publication number: 20140162970Abstract: The present invention relates to new methods for treating and/or preventing cardiac arrhythmias, heart failure, stroke and/or peripheral artery disease by administering a composition comprising triazolopyrimidine, or derivative or metabolite thereof. In particular, the present invention relates to methods for treating cardiac arrhythmias, heart failure, stroke and/or peripheral artery disease by administering CycloPentyl-TriazoloPyrimidine.Type: ApplicationFiled: August 7, 2013Publication date: June 12, 2014Applicant: HearlDrug Research, L.L.C.Inventor: Victor L. Serebruany
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Patent number: 8741906Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: November 6, 2012Date of Patent: June 3, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
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Publication number: 20140147505Abstract: The present invention relates to a solid pharmaceutical dosage form comprising ticagrelor as pharmaceutically active ingredient, to certain particles of ticagrelor and to processes of preparing the same.Type: ApplicationFiled: January 29, 2014Publication date: May 29, 2014Applicant: ratiopharm GmbHInventors: Sandra BRUECK, Dominique MEERGANS
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Publication number: 20140148472Abstract: Disclosed are compounds able to modulate the activity of the GPR17 receptor in a highly specific way, which are useful in the treatment and diagnosis of diseases or dysfunctions involving the activation of said receptor. In particular, the compounds according to the invention can be used for neuroprotective and/or reparatory purposes, in cerebral, cardiac and renal ischaemia, in cerebral trauma, in chronic neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), and in demyelinating diseases such as multiple sclerosis.Type: ApplicationFiled: November 2, 2011Publication date: May 29, 2014Applicant: CENTRO CARDIOLOGICO MONZINO SpAInventors: Mariapia Abbracchio, Ivano Eberini, Chiara Parravicini, Claudia Martini, Maria Letizia Trincavelli, Simona Daniele
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Publication number: 20140148433Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: August 31, 2011Publication date: May 29, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
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Publication number: 20140128399Abstract: Methods and compositions are provided for treating a urinary tract infection (UTI). The methods involve administering to a subject in need thereof a cAMP elevator or agent that mimics cAMP, particularly a labdane diterpene such as forskolin or a derivative or analog thereof in a therapeutically effective amount to treat a UTI. The methods may further include administration of at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs. Compositions of the invention include pharmaceutical compositions and kits for treating a UTI in a subject in need thereof that include therapeutically effective amounts of at least two cAMP elevators, particularly where one of the cAMP elevators is a labdane diterpene such as forskolin or a derivative or analog thereof.Type: ApplicationFiled: December 6, 2013Publication date: May 8, 2014Applicant: DUKE UNIVERSITYInventors: Soman N. Abraham, Brian L. Bishop, Matthew J. Duncan, K. Ranga Rama Krishnan, Jeongmin Song, Guojie Li, David W. Zaas
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Publication number: 20140073624Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: February 19, 2013Publication date: March 13, 2014Applicant: RIB-X PHARMACEUTICALS, INC.Inventor: Rib-X Pharmaceuticals, Inc.
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Patent number: 8623901Abstract: The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V?W?*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.Type: GrantFiled: March 30, 2010Date of Patent: January 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Riccardo Giovannini, Cornelia Dorner-Ciossek, Christian Eickmeier, Dennis Fiegen, Thomas Fox, Klaus Fuchs, Niklas Heine, Holger Rosenbrock, Gerhard Schaenzle
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Patent number: 8598184Abstract: The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: February 28, 2009Date of Patent: December 3, 2013Assignee: Tiger PharmatechInventor: Junhu Zhang
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Publication number: 20130310401Abstract: The invention relates to methods and kits for determining platelet susceptibility to activation in a patient. More particularly, the present invention relates to a method for determining platelet susceptibility to activation in a patient, comprising a step consisting of measuring the level of GPVI dimers at the platelet surface in a blood sample obtained from said patient.Type: ApplicationFiled: December 1, 2011Publication date: November 21, 2013Applicants: UNIVERSITE PARIS DIDEROT, Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Martine Jandrot-Perrus, Laurent Feldman, Stéphane Loyau
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Patent number: 8569295Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: GrantFiled: July 28, 2010Date of Patent: October 29, 2013Assignee: Merck Patent GmbHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
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Publication number: 20130245044Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: ApplicationFiled: May 8, 2013Publication date: September 19, 2013Applicant: Vernalis Research LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Patent number: 8536138Abstract: This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.Type: GrantFiled: December 5, 2011Date of Patent: September 17, 2013Assignee: Vivus, Inc.Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
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Publication number: 20130224255Abstract: Embodiments of the present invention include methods for the treatment, prevention, or amelioration of vascular disease in diabetic patients. The methods include both implantation of a stent including a first drug. Some embodiments include additional therapy, such as the co-administration of another drug. Some embodiments involve different stent selection for a diabetic patient compared to a non-diabetic patient.Type: ApplicationFiled: February 23, 2012Publication date: August 29, 2013Applicant: Abbott Cardiovascular Systems Inc.Inventors: Syed F.A. Hossainy, Paul M. Consigny
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Publication number: 20130210826Abstract: The present invention features methods and compositions for preventing, reducing, or treating a traumatic, metabolic, or toxic peripheral nerve lesion or pain including neuropathic pain, inflammatory, and nociceptive pain by administering to a mammal a compound that reduces expression or activity of BH4. This reduction may be achieved by reducing activity of a BH4 synthetic enzyme, including GTP cyclohydrolase, sepiapterin reductase, or dihydropteridine reductase; antagonizing the cofactor function of BH4 or BH4-dependent enzymes; or blocking BH4 binding to membrane bound receptors. The invention provides methods for diagnosing pain or a peripheral nerve lesion in a mammal by measuring levels of BH4 or its metabolites in biological sample or the levels or activity of any one of the BH4 synthetic enzyme in tissue samples of a mammal.Type: ApplicationFiled: October 11, 2012Publication date: August 15, 2013Applicant: The General Hospital CorporationInventor: The General Hospital Corporation
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Patent number: 8501811Abstract: Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.Type: GrantFiled: June 17, 2011Date of Patent: August 6, 2013Assignee: Washington UniversityInventors: James Hsieh, Emily Cheng
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Publication number: 20130184295Abstract: The present invention is directed to a method of screening for a therapeutic agent useful for treating pulmonary hypertension comprising: contacting an erythrocyte with a candidate therapeutic agent; and detecting a presence or absence of erythrocyte-derived adenosine triphosphate, wherein a greater erythrocyte-derived adenosine triphosphate level indicates the candidate therapeutic agent has greater activity in treating pulmonary hypertension. Additionally, the present invention is directed to methods of treating pulmonary arterial hypertension by stimulating ATP release from erythrocytes through co-administration to a subject in need thereof an amount of a PDE5 inhibitor compound, and an amount of a prostacyclin compound.Type: ApplicationFiled: January 10, 2013Publication date: July 18, 2013Applicant: United Therapeutics CorporationInventor: United Therapeutics Corporation
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Publication number: 20130137676Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 19, 2012Publication date: May 30, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8450328Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: GrantFiled: June 25, 2009Date of Patent: May 28, 2013Assignee: Vernalis (R&D) LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Publication number: 20130131087Abstract: The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing the compound {1S-[1?, 2?, 3?(1S*,2R*),5?]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol.Type: ApplicationFiled: December 21, 2012Publication date: May 23, 2013Applicant: AstraZeneca ABInventor: Simon Banks