1,4-diazine As One Of The Cyclos Patents (Class 514/249)
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Patent number: 9475820Abstract: A series of imidazo[1,2-a]pyrazine derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: July 5, 2013Date of Patent: October 25, 2016Assignee: UCB Biopharma SPRLInventors: Jonathan Mark Bentley, Daniel Christopher Brookings, Julien Alistair Brown, Thomas Paul Cain, Laura Jane Gleave, Alexander Heifetz, Victoria Elizabeth Jackson, Craig Johnstone, Deborah Leigh, James Madden, John Robert Porter, Matthew Duncan Selby, Zhaoning Zhu
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Patent number: 9474752Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.Type: GrantFiled: February 17, 2014Date of Patent: October 25, 2016Assignee: Gilead Sciences, Inc.Inventors: Michael J. Gerber, Christopher Dufton
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Patent number: 9447098Abstract: The invention relates to new pteridine derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g.Type: GrantFiled: May 30, 2013Date of Patent: September 20, 2016Assignee: ASTEX THERAPEUTICS LTDInventors: Gordon Saxty, Christopher Charles Frederick Hamlett, Valerio Berdini, Christopher William Murray, Patrick René Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
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Patent number: 9434726Abstract: Provided are pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.Type: GrantFiled: June 7, 2012Date of Patent: September 6, 2016Assignee: HUTCHISON MEDIPHARMA LIMITEDInventors: Wei-Guo Su, Wei Deng, Jianguo Ji
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Patent number: 9428510Abstract: The present invention relates to a compound of following formula (I) or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.Type: GrantFiled: July 29, 2013Date of Patent: August 30, 2016Assignee: PIERRE FABRE MEDICAMENTInventors: Anna Kruczynski, Laurent Creancier, El Bachir Kaloun, Karim Bedjeguelal, Rémi Rabot
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Patent number: 9422299Abstract: Novel compounds of Formula I and their use in therapeutic treatments.Type: GrantFiled: April 23, 2015Date of Patent: August 23, 2016Assignee: EUROSCREEN SAInventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
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Patent number: 9388185Abstract: The present invention relates to pyrazine derivatives of Formula I, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: GrantFiled: August 9, 2013Date of Patent: July 12, 2016Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Liang Lu, Chunhong He, Wenqing Yao
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Patent number: 9388143Abstract: Provided herein are various polymorph forms of N-(3-{[(2Z)-3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]sulfamoyl}phenyl)-2-methylalaninamide.Type: GrantFiled: March 12, 2015Date of Patent: July 12, 2016Assignee: SANOFIInventors: Virginie Baulier, Matthieu Fugier, Stephane Kozlovic, Marc-Antoine Perrin, Bruno Baillon, Myriam Comte
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Patent number: 9382256Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.Type: GrantFiled: July 29, 2014Date of Patent: July 5, 2016Assignee: Gilead Connecticut, Inc.Inventors: Melissa Jean Casteel, Bei Li, Rowchanak Pakdaman, Diana Sperger, Dimitrios Stefanidis
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Patent number: 9370525Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.Type: GrantFiled: July 23, 2015Date of Patent: June 21, 2016Assignee: Supernus Pharmaceuticals, Inc.Inventors: Padmanabh P. Bhatt, Argaw Kidane, Kevin Edwards
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Patent number: 9371330Abstract: Provided are: composition and methods for: treating aging or an age-related condition, symptom or disease; stimulating hair growth, regrowth or pigmentation (or preventing hair loss); for increasing adenosine receptor expression in dermal cells (in combination with hair growth); for treating a condition or disease of the skin or at least one symptom thereof, including cosmetic treatment (e.g., wrinkles, hyperpigmentation, redness, rosacea, dryness, cracking, loss of firmness, loss of elasticity, thinning, and loss of vibrancy). The methods comprise administering a sufficient amount of the disclosed CBP/catenin (e.g., CBP/(?-catenin) antagonist compositions, and particularly wherein administration is in an amount and manner sufficient to provide for increasing the number of asymmetric renewing divisions relative to, or at the expense of symmetric divisions in relevant somatic stem cell population. In particular aspects, the CBP/catenin (e.g.Type: GrantFiled: May 15, 2012Date of Patent: June 21, 2016Assignee: University of Southern CaliforniaInventors: Michael Kahn, Jia-Ling Teo, Michael McMillan, Yi Zhao, Yongfeng Wu
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Patent number: 9353068Abstract: The present invention relates to compounds of the formula I, wherein Ht, 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: GrantFiled: July 26, 2012Date of Patent: May 31, 2016Assignee: SANOFIInventors: Sven Ruf, Josef Pernerstorfer, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Klaus Wirth
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Patent number: 9351974Abstract: Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.Type: GrantFiled: November 12, 2012Date of Patent: May 31, 2016Assignee: OSI Pharmaceuticals, LLCInventors: Meizhong Jin, Mridula Kadalbajoo, An-Hu Li, Mark J. Mulvihill, Kam W. Siu, Arno G. Steinig, Jing Wang
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Patent number: 9346809Abstract: The invention relates to compounds of general formula (I) wherein A, R1, R2, R3, R4, R5, R9, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.Type: GrantFiled: July 8, 2010Date of Patent: May 24, 2016Assignee: LEO PHARMA A/SInventors: Simon Feldbæk Nielsen, Daniel Rodriguez Greve, Carsten Ryttersgaard, Gunnar Grue-Sørensen, Erik Rytter Ottosen, Tina Dahlerup Poulsen, Søren Christian Schou, Anthony Murray
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Patent number: 9341637Abstract: A method is provided of determining whether an individual has reduced ability to form platelet thrombi due to inhibition of platelet activation initiation, signal transduction and/or GPIIb/IIIa blockade. A blood sample is obtained from the individual being assessed. The blood sample is mixed in combination with 1) an anticoagulant; 2) sufficient buffer to maintain the pH and salt concentration of the anticoagulated blood within a range suitable for platelet aggregation; 3) a platelet GPIIb/IIIa receptor ligand immobilized on a solid surface; 4) one or more agents to enhance a signal transduction pathway and 5) a receptor activator. The combination is incubated under conditions for agglutinating particles. Platelet-mediated agglutination is assessed in the agitated mixture. The absence of agglutination indicates that the individual has a reduced ability to form platelet thrombi.Type: GrantFiled: November 10, 2010Date of Patent: May 17, 2016Assignee: ACCUMETRICS INC.Inventors: Barry S. Coller, Dennis Durbin
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Patent number: 9340557Abstract: The compounds represented by Formula (I) and pharmaceutically acceptable salts thereof are useful as inhibitors of DNA-PK: where each of R1, R2, X, Ring A, Ring B and Ring C is as described herein. Pharmaceutically acceptable compositions comprise said compounds. These compounds and pharmaceutical compositions are used in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 12, 2014Date of Patent: May 17, 2016Assignee: Vertex Pharmaceuticals IncorporatedInventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux, Jinwang Xu, Kevin M. Cottrell, Mark A. Morris, Nathan D. Waal, John J. Court, Wenxin Gu, Hongbo Deng
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Patent number: 9320436Abstract: A method and devices for detecting deposits, in particular amyloid plaques, in the eye, in particular in the human eye. The subject is an optical method for detecting deposits, in particular ?-amyloid, in the retina, which is locally resolved and wherein the local resolution is better than the layer thickness of individual layers of the retina. The invention includes a device for optically detecting ?-amyloid in the retina, which generates a locally resolved image of the retina and wherein the local resolution is better than the layer thickness of individual layers of the retina.Type: GrantFiled: September 29, 2010Date of Patent: April 26, 2016Assignee: Carl Zeiss Meditec AGInventors: Christoph Russmann, Martin Hacker, Manfred Dick, Ingrid Hilger, Werner A. Kaiser
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Patent number: 9309242Abstract: The invention relates to new pyridopyrazine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: October 26, 2012Date of Patent: April 12, 2016Assignee: ASTEX THERAPEUTICS LTDInventors: Valerio Berdini, Gordon Saxty, Patrick Rene Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet, Bruno Roux, Lieven Meerpoel
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Patent number: 9309250Abstract: The present invention relates to pyrrolopyrazines 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 of 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 I: wherein the variables are as defined herein.Type: GrantFiled: June 22, 2012Date of Patent: April 12, 2016Assignee: Vertex Pharmaceuticals IncorporatedInventors: Pierre-Henri Storck, Jean-Damien Charrier, Alistair Rutherford, Michael Paul Mortimore, Somhairle MacCormick, Ronald Marcellus Alphonsus Knegtel, Steven John Durrant
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Patent number: 9309236Abstract: Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.Type: GrantFiled: October 5, 2012Date of Patent: April 12, 2016Assignees: The Board of Trustees of the Leland Stanford Junior University, The Regents of the University of CaliforniaInventors: Jeffrey S. Glenn, Michael A. Gelman, Brandon Tavshanjian, Kevan Shokat, Ingrid Choong
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Patent number: 9301922Abstract: The administration of levoleucovorin is useful as an antidote to drugs which act as folic acid antagonists and in combination chemotherapy with 5-FU. The most often used calcium salt of levoleucovorin has a limited solubility in water and forms almost insoluble degradation products. Therefore aqueous solutions are unstable and precipitates are resulting. Precipitates in injectable products present an unacceptable safety risk to patients. Stable high strength pharmaceutical aqueous compositions containing calcium salts, magnesium or zinc salts of levoleucovorin and one or more of the compounds sodium gluconate, potassium gluconate, glycerophosphate disodium salt or glycerophosphate dipotassium salt are disclosed.Type: GrantFiled: April 30, 2014Date of Patent: April 5, 2016Assignee: APROFOL AGInventor: Martin Ulmann
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Patent number: 9290505Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: GrantFiled: December 22, 2014Date of Patent: March 22, 2016Assignee: Gilead Sciences, Inc.Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Jennifer R. Lo, Scott A. Mitchell, Aaron C. Schmitt, Jin-Ming Xiong, Jianjun Xu, Zhongdong Zhao, Sundaramoorthi Swaminathan
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Patent number: 9290478Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: November 29, 2011Date of Patent: March 22, 2016Assignee: ASTEX THERAPEUTICS LTDInventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Steven John Woodhead, Yannick Aime Eddy Ligny, Patrick René Angibaud
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Patent number: 9290488Abstract: The disclosure relates to Azetidine-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the R1, R2, R3, Q, Y1, Z, A, B, a, and b are as defined herein, compositions comprising an effective amount of an Azetidine-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Azetidine-Substituted Quinoxaline-Type Piperidine Compound.Type: GrantFiled: November 30, 2012Date of Patent: March 22, 2016Assignee: Purdue Pharma L.P.Inventors: Laykea Tafesse, Naoki Tsuno, Xiaoming Zhou
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Patent number: 9290502Abstract: The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.Type: GrantFiled: December 3, 2013Date of Patent: March 22, 2016Assignee: JANSSEN SCIENCES IRELAND UCInventors: Pierre Jean-Marie Bernard Raboisson, Dominique Louis Nestor Ghislain Surleraux, Tse-I Lin, Oliver Lenz, Kenneth Alan Simmen
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Patent number: 9283223Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.Type: GrantFiled: February 17, 2014Date of Patent: March 15, 2016Assignee: Gilead Sciences, Inc.Inventors: Michael J. Gerber, Christopher Dufton
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Patent number: 9266891Abstract: Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: GrantFiled: November 11, 2013Date of Patent: February 23, 2016Assignee: Boehringer Ingelheim International GmbHInventors: Harald Engelhardt, Davide Gianni, Christian Smethurst
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Patent number: 9265746Abstract: Method for selective targeting of one or more effector moiety such as diagnostic or a therapeutic agent to a cell or population of cells expressing a folate-receptor comprising simultaneous or sequential administration of an antifolate with a folate- or pteroate-conjugate comprising said one or more effector moiety.Type: GrantFiled: May 31, 2006Date of Patent: February 23, 2016Assignee: MERCK & CIEInventors: Rudolf Moser, Viola Groehn, Roger Schibli, Cristina Magdalena Mueller
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Patent number: 9260428Abstract: This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-spiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.Type: GrantFiled: September 27, 2013Date of Patent: February 16, 2016Assignee: OPKO Health, Inc.Inventors: Ingrid Mergelsberg, Dominik Hermann Scherer, Monika Erika Huttenloch, Hon-Chung Tsui, Sunil Paliwal, Neng-Yang Shih
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Patent number: 9259425Abstract: The invention provides compositions and methods for whitening of eyes. The provided compositions and methods utilize low concentrations of selective ?-2 adrenergic receptor agonists. The compositions preferably include brimonidine.Type: GrantFiled: October 3, 2013Date of Patent: February 16, 2016Assignee: Eye Therapies LLCInventor: Gerald Horn
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Patent number: 9255106Abstract: Provided is a piperazinotriazole compound represented by general formula I or a pharmaceutically acceptable salt, stereoisomer, tautomer or hydrate thereof. Also provided are a pharmaceutical composition comprising the compound, a method for preparing the compound and a method of use thereof as a high-selectivity poly(adenosine diphosphate-ribose)polymerase-1 (PARP-1) inhibitor in the preparation of drugs for the prevention and/or treatment of PARP-related diseases.Type: GrantFiled: July 24, 2013Date of Patent: February 9, 2016Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Ao Zhang, Zehong Miao, Na Ye, Xiajuan Huan, Zilan Song, Chuanhuizi Chen, Yi Chen, Jian Ding
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Patent number: 9249110Abstract: Described herein are kinase inhibitors represented by Formula I: and pharmaceutical compositions thereof for use in the treatment of cancer.Type: GrantFiled: September 20, 2012Date of Patent: February 2, 2016Assignee: NEUPHARMA, INC.Inventors: Xiangping Qian, Yong-Liang Zhu
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Patent number: 9249111Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. Specifically quinoxaline derivatives of Formula I: and their use in modulating the activity of B-raf and/or mutant B-raf kinase to regulate and modulate abnormal or inappropriate cell proliferation, differentiation, or metabolism are disclosed. Also disclosed are methods of treating cancer associated with B-raf and/or mutant B-raf kinase activity in a subject, comprising administering the compounds of Formula I.Type: GrantFiled: September 28, 2012Date of Patent: February 2, 2016Assignee: NEUPHARMA, INC.Inventors: Xiangping Qian, Yong-Liang Zhu
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Patent number: 9242963Abstract: The present invention provides novel organic compounds of Formula (I): methods of use, and pharmaceutical compositions thereof.Type: GrantFiled: April 2, 2015Date of Patent: January 26, 2016Assignee: NOVARTIS AGInventors: Christopher Michael Adams, Qi-Ying Hu, Leslie Wighton McQuire, Julien Papillon
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Patent number: 9233965Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.Type: GrantFiled: July 23, 2014Date of Patent: January 12, 2016Assignee: SANOFIInventors: Sylvain Cote-Des-Combes, Jacques Froissant, Jean-Francois Gibert, Frank Marguet, Christophe Pacaud, Frederic Puech, Antoine Ravet
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Patent number: 9216178Abstract: Dry blend powder formulations comprising a pharmaceutical formulation containing tetrahydrobiopterin, and methods of making and using the same, are disclosed herein.Type: GrantFiled: November 1, 2012Date of Patent: December 22, 2015Assignee: BioMarin Pharmaceutical Inc.Inventors: Tianwei Chou, Augustus O. Okhamafe
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Patent number: 9216160Abstract: Compositions and methods for treating hyperlipidemia and elevated LDL cholesterol and for weight reduction are disclosed. The compositions comprise (a) choline, or a salt or hydroxide thereof; (b) niacin, or a salt, amide or ester thereof; (c) folic acid, or a salt thereof; (d) methionine or a salt or ester thereof; and (e) glycine or a salt, ester or methylated form thereof.Type: GrantFiled: October 4, 2012Date of Patent: December 22, 2015Inventor: Jeffrey M. Golini
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Patent number: 9212184Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I): (I) in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: GrantFiled: December 13, 2011Date of Patent: December 15, 2015Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
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Patent number: 9212191Abstract: Provided are imidazopyrazine compounds, particularly including 6-(2,3-dihydro-1H-pyrido-[2,3-b][1,4]oxazin-7-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazine-8-amine, structure below, and methods and formulations for their use in inhibiting Spleen Tyrosine Kinase in treating conditions including B-cell lymphomas or leukemias and inflammatory conditions:Type: GrantFiled: June 9, 2014Date of Patent: December 15, 2015Assignee: GILEAD CONNECTICUT, INC.Inventors: Scott A. Mitchell, Kevin S. Currie
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Patent number: 9192568Abstract: Jorumycin, renieramycin, safracin and saframycin related compounds formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.Type: GrantFiled: October 30, 2006Date of Patent: November 24, 2015Assignee: Pharma Mar, S.A.Inventors: Pilar Calvo Salve, Maria Tobio Barreira
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Patent number: 9193693Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: GrantFiled: September 29, 2014Date of Patent: November 24, 2015Assignee: BioEnergenix LLCInventors: John M. McCall, Donna L. Romero, John McKearn, Michael Clare
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Patent number: 9187481Abstract: The present invention relates to diastereomers of 10-propargyl-10-deazaaminopterin, compositions comprising optically pure diastereomers of 10-propargyl-10-deazaaminopterin, in particular the two (R,S) diastereomers about the C10 position, specifically, diastereomers (2S)-2-[[4-[(1S)-1-[(2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid and/or (2S)-2-[[4-[(1R)-1-[(2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid. Methods of preparation of these diastereomers, compositions containing them, and their use for the treatment of conditions related to inflammatory disorders and cancer are also disclosed.Type: GrantFiled: August 25, 2014Date of Patent: November 17, 2015Assignee: Allos Therapeutics, Inc.Inventor: Gijsbertus J. Pronk
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Patent number: 9187429Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A and n are as described herein, compositions including the compounds and methods of using the compounds.Type: GrantFiled: April 17, 2013Date of Patent: November 17, 2015Assignee: HOFFMANN-LA ROCHE INC.Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
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Patent number: 9181249Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.Type: GrantFiled: December 19, 2014Date of Patent: November 10, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Jason Brown, Steve Hitchcock, Maria Hopkins, Shota Kikuchi, Holger Monenschein, Holly Reichard, Kristin Schleicher, Huikai Sun, Todd Macklin
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Patent number: 9181258Abstract: The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives, of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: October 4, 2012Date of Patent: November 10, 2015Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Francesco Casuscelli, Alessandra Badari, Sten Christian Orrenius, Claudia Piutti, Teresa Disingrini
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Patent number: 9174985Abstract: The invention relates to salts of (7-(2,3-di-p-tolyl-7,8-dihydropyrido[2,3-b]pyrazin-5(6H)-yl)heptanoic acid which are useful for treating diseases affected by the activation of the IP receptor, pharmaceutical compositions that contain the salts and processes for preparing the salts are also described.Type: GrantFiled: January 11, 2013Date of Patent: November 3, 2015Assignee: Novartis AGInventors: Catherine Leblanc, Stephen Carl McKeown, Anett Perlberg, Nicola Tufilli
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Patent number: 9169252Abstract: Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-d]pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-d]pyrimidinyl, 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl, imidazo[4,5-b]pyridinyl, and purinyl, wherein said heteroaryl is substituted with Ra and Rb; and R1 and R2 are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.Type: GrantFiled: January 2, 2015Date of Patent: October 27, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Joseph B. Santella, Sreekantha Ratna Kumar, John V. Duncia, Daniel S. Gardner, Venkatram Reddy Paidi, Satheesh Kesavan Nair, John Hynes, Hong Wu, Natesan Murugesan, Kandhasamy Sarkunam, Piramanayagam Arunachalam
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Patent number: 9163007Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.Type: GrantFiled: December 20, 2013Date of Patent: October 20, 2015Assignee: AbbVie Inc.Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha H. M. Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn M. George, Lu Wang, Biqin Li, Nigel S. Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
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Patent number: 9150592Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: GrantFiled: December 20, 2013Date of Patent: October 6, 2015Assignee: AbbVie Inc.Inventors: Kevin P. Cusack, Thomas D. Gordon, Michael Z. Hoemann, David C. Ihle, Bin Li, Gloria Y. Lo Schiavo, Gagandeep K. Somal, Michael Friedman, Martin E. Hayes, Wouter Iwema Bakker
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Patent number: 9149465Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: GrantFiled: May 18, 2010Date of Patent: October 6, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts