Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond Patents (Class 514/275)
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Patent number: 9289441Abstract: Methods for the safe administration of imidazole or imidazolium compounds, and conditions that may be treated by these methods, are described herein.Type: GrantFiled: March 4, 2015Date of Patent: March 22, 2016Assignee: ANTECIP BIOVENTURES II LLCInventors: Herriot Tabuteau, Jaro I. Karppinen
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Patent number: 9284304Abstract: This invention relates to alkylpyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.Type: GrantFiled: August 9, 2013Date of Patent: March 15, 2016Assignee: Janssen Sciences Ireland UCInventors: David Craig McGowan, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson
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Patent number: 9283224Abstract: The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: GrantFiled: April 5, 2012Date of Patent: March 15, 2016Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Tiziano Bandiera, Jay Aaron Bertrand, Paola Gnocchi, Danilo Mirizzi, Marcella Nesi, Achille Panzeri
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Patent number: 9278981Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: GrantFiled: May 9, 2013Date of Patent: March 8, 2016Assignee: Novartis AGInventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer, Erich Alois Spieser
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Patent number: 9273077Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use as protein kinase inhibitors.Type: GrantFiled: March 15, 2013Date of Patent: March 1, 2016Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
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Patent number: 9265764Abstract: Aspects of this invention are related, at least in part, to the use of chemical compounds able to inhibit GSK-3 and/or to stabilize ?-catenin and formulations thereof. Some aspects of this invention relate to compositions comprising such compounds. Some aspects of the invention provide methods of using such compounds and/or compositions in the treatment of subjects having a neurological disease and/or psychiatric disorder. Some aspects of this invention provide methods of using ruboxistaurin, enzastaurin, sunitinib, midostaurin, lestaurtinib, 7-hydroxystaurosporine, and/or Chir99021 in the treatment of subjects having a neurological disease and/or psychiatric disorder. In some embodiments, compounds are administered in combination with Lithium.Type: GrantFiled: February 27, 2010Date of Patent: February 23, 2016Assignees: Massachusetts Institute of Technology, The General Hospital CorporationInventors: Stephen J. Haggarty, Daniel Fass, Jennifer Pan, Josh Ketterman, Edward Holson, Tracey Lynn Petryshen, Michael C. Lewis
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Patent number: 9265772Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.Type: GrantFiled: May 10, 2013Date of Patent: February 23, 2016Assignee: RESET THERAPEUTICS, INC.Inventors: Ross Bersot, Paul Humphries
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Patent number: 9249146Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.Type: GrantFiled: June 26, 2014Date of Patent: February 2, 2016Assignees: Biogen MA Inc., Sunesis Pharmaceuticals, Inc.Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
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Patent number: 9248190Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.Type: GrantFiled: June 25, 2014Date of Patent: February 2, 2016Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
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Patent number: 9242937Abstract: The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.Type: GrantFiled: March 1, 2012Date of Patent: January 26, 2016Assignees: Bayer Intellectual Property GmbH, LEAD DISCOVERY CENTER GMBHInventors: Gerd Rühter, Peter Nussbaumer, Axel Choidas, Carsten Schulz-Fademrecht, Bert Klebl, Jan Eickhoff
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Patent number: 9238628Abstract: The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: GrantFiled: June 7, 2013Date of Patent: January 19, 2016Assignee: YM Biosicences Australia PTY LTDInventors: Christopher John Burns, Andrew Donohue, John Thomas Feutrill, Thao Lien Thi Nguyen, Andrew Frederick Wilks, Jun Zeng
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Patent number: 9238651Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: GrantFiled: August 13, 2014Date of Patent: January 19, 2016Assignee: MERCK PATENT GMBHInventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
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Patent number: 9233935Abstract: The present invention provides a novel process for the preparation of rilpivirine. The present invention also provides a novel process for the preparation of rilpivirine hydrochloride. The present invention further provides a rilpivirine hydrochloride monohydrate, process for its preparation and pharmaceutical compositions comprising it.Type: GrantFiled: September 10, 2012Date of Patent: January 12, 2016Assignee: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Adulla Venkat Narsimha Reddy, Bandi Vamsi Krishna
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Patent number: 9221798Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.Type: GrantFiled: September 5, 2011Date of Patent: December 29, 2015Assignee: Zhejian Hisun Pharmaceutical Co., Ltd.Inventors: Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
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Patent number: 9212173Abstract: Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: GrantFiled: November 3, 2014Date of Patent: December 15, 2015Assignee: Genentech, Inc.Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Bryan K. Chan, Mark Chambers, Huifen Chen, Anthony Estrada, Zachary Kevin Sweeney
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Patent number: 9206176Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. 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: GrantFiled: March 27, 2014Date of Patent: December 8, 2015Assignee: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Patent number: 9205085Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.Type: GrantFiled: November 7, 2012Date of Patent: December 8, 2015Assignee: Emory UniversityInventors: Michael G. Natchus, Richard Arrendale, Dennis Liotta
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Patent number: 9168257Abstract: Disclosed are compositions and methods for the treatment of disorders such as myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML). The disclosed methods include administering to an individual in need of such treatment a composition that may include an IRAK1/4 inhibitor. In other aspects, the method may include administration of a BLC2 inhibitor.Type: GrantFiled: May 22, 2014Date of Patent: October 27, 2015Assignee: Children's Hospital Medical CenterInventors: Daniel Starczynowski, Garrett W. Rhyasen
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Patent number: 9162988Abstract: A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect.Type: GrantFiled: December 12, 2012Date of Patent: October 20, 2015Assignee: TORAY INDUSTRIES, INC.Inventors: Mie Kaino, Hiroyuki Meguro
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Patent number: 9163005Abstract: Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.Type: GrantFiled: October 11, 2013Date of Patent: October 20, 2015Assignee: Novartis AGInventors: Paul W Manley, Wen-Chung Shieh, Paul Allen Sutton, Piotr H Karpinski, Raeann Wu, Stéphanie Monnier, Jörg Brozio
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Patent number: 9155317Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.Type: GrantFiled: February 8, 2012Date of Patent: October 13, 2015Assignee: DSM IP ASSETS B.V.Inventors: Jacobus Stark, Angelique De Rijk
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Patent number: 9150543Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: April 3, 2014Date of Patent: October 6, 2015Assignee: Janssen Pharmaceutica N. V.Inventors: Marc Gustaaf Celine Verdonck, Patrick Rene Angibaud, Bruno Roux, Isabelle Noelle Constance Pilatte, Peter Ten Holte, Janine Arts, Kristof Van Emelen
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Patent number: 9145387Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: GrantFiled: February 7, 2014Date of Patent: September 29, 2015Assignee: Celgene Avilomics Research, Inc.Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
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Patent number: 9145402Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: GrantFiled: November 28, 2012Date of Patent: September 29, 2015Assignee: Genentech, Inc.Inventors: Charles Baker-Glenn, Mark Chambers, Bryan K. Chan, Anthony Estrada, Daniel Shore, Zachary Kevin Sweeney, Huifen Chen
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Patent number: 9133133Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: June 19, 2014Date of Patent: September 15, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 9133163Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.Type: GrantFiled: November 15, 2013Date of Patent: September 15, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Bruce A. Ellsworth, Jun Shi, William R. Ewing, Elizabeth A. Jurica, Andres S. Hernandez, Ximao Wu
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Patent number: 9108926Abstract: The present invention relates to disubstituted 5-fluoro-pyrimidines of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).Type: GrantFiled: September 13, 2012Date of Patent: August 18, 2015Assignee: Bayer Intellectual Property GmbHInventors: Ulrich Lücking, Dirk Kosemund, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Rolf Bohlmann
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Patent number: 9102656Abstract: This invention relates to the discovery of novel rosuvastatin analogs. More specifically, the invention relates to novel rosuvastatin analogs which have utility in treating conditions treatable by the inhibition of HMG-CoA reductase.Type: GrantFiled: September 17, 2013Date of Patent: August 11, 2015Assignee: RedX Pharma LimitedInventors: Derek Lindsay, Peter Jackson
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Patent number: 9102676Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.Type: GrantFiled: June 5, 2014Date of Patent: August 11, 2015Assignee: Merck Sharp & Dohme B.V.Inventors: Tjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fadermrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
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Patent number: 9096597Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: GrantFiled: May 7, 2014Date of Patent: August 4, 2015Assignee: Kineta Four, LLCInventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
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Patent number: 9085572Abstract: The present application relates to novel dipyridyl-dihydropyrazolones, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: GrantFiled: August 24, 2012Date of Patent: July 21, 2015Assignee: Bayer Intellectual Property GmbHInventors: Ingo Flamme, Jens-Kerim Ergüden, Felix Oehme, Kai Thede, Gunter Karig, Alexander Kuhl, Hanno Wild, Joachim Schuhmacher, Peter Kolkhof, Lars Bärfacker, Joachim Hütter
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Patent number: 9067918Abstract: The present invention relates to polymorphs and hydrates of 2-(2-methylamino-pyrimidin-4-yl)-1H-indole-5-carboxylic acid [(S)-1-carbamoyl-2-(phenyl-pyrimidin-2-yl-amino)-ethyl]-amide, processes for their preparation and their use, in particular in pharmaceutical compositions.Type: GrantFiled: December 4, 2012Date of Patent: June 30, 2015Assignee: SANOFIInventors: Olaf Ritzeler, Mandy Mohnicke, Guenter Billen, Bruno Baumgartner, Martin Brockelmann, Norbert Nagel
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Patent number: 9061029Abstract: The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I wherein the radicals as defined herein, or of a pharmaceutically acceptable salt thereof, for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-Abl oncoprotein, the cell transmembrane tyrosine kinase receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity, wherein the pyrimidylaminobenzamide of formula I and, optionally, pharmaceutically acceptable carriers, are dispersed in a fruit preparation.Type: GrantFiled: November 17, 2010Date of Patent: June 23, 2015Assignee: Novartis AGInventors: Neil Gallagher, Ophelia Yin
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Patent number: 9062033Abstract: The invention relates to a novel compound of formula (I) or a stereoisomer, or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein: R is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from S, N and O, such rings may be optionally substituted with n groups Q; Q is selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, SO2CH3 or a group —O[(CR1R2]pQ1; or Q may be a group Q2; Q1 is phenyl, which may be optionally substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, or a group Q2; or corresponds to 2,2-difluoro-benzo[d][1,3]dioxol-4-yl; Q2 is a 5- or 6-membered heteroaryl containing at least one nitrogen atom, which may optionally substituted with n substituents selected from a group consisting of: C1 C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; P is a 6-membered heteroaryl or a 8-1 1 membered bicyclic heteroaryl group, whichType: GrantFiled: December 20, 2012Date of Patent: June 23, 2015Assignee: Rottapharm Biotech S.R.L.Inventors: Luigi Piero Stasi, Lucio Claudio Rovati, Roberto Artusi, Fabrizio Colace, Stefano Mandelli, Lorenzo Perugini
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Patent number: 9056854Abstract: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: November 3, 2014Date of Patent: June 16, 2015Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
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Patent number: 9049862Abstract: This invention provides a composition comprising a a compound selected from Formula 1, an N-oxide and an agriculturally suitable salt thereof; and pymetrozine, wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure.Type: GrantFiled: March 8, 2013Date of Patent: June 9, 2015Assignee: E I DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20150148327Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: June 17, 2013Publication date: May 28, 2015Applicant: Merck Canada Inc.Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
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Publication number: 20150148360Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.Type: ApplicationFiled: July 19, 2013Publication date: May 28, 2015Inventors: Jung-Hsin Lin, Jim-Min Fang, Ting-Rong Chen, Jhih-Bin Chen, Ching-Chow Chen, Tzu-Tang Wei
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Publication number: 20150148361Abstract: Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: January 28, 2015Publication date: May 28, 2015Inventors: James P. Edwards, David E. Kindrachuk, Christopher M. Mapes, Daniel J. Pippel, Jennifer D. Venable
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Patent number: 9040550Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: July 16, 2014Date of Patent: May 26, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 9040558Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.Type: GrantFiled: December 28, 2005Date of Patent: May 26, 2015Assignee: DR. REDDY'S LABORATORIES LTD.Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
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Publication number: 20150141449Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin.Type: ApplicationFiled: January 29, 2015Publication date: May 21, 2015Inventors: Zdenko CASAR, Janez Kosmrlj
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Publication number: 20150141434Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R1, R4, X, G, n, p, W1, W2, W3, W4, and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.Type: ApplicationFiled: September 5, 2014Publication date: May 21, 2015Inventor: Jae Hyun Park
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Publication number: 20150141448Abstract: The present invention relates to topical ophthalmological pharmaceutical compositions containing pazopanib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders.Type: ApplicationFiled: June 10, 2013Publication date: May 21, 2015Applicant: BAYER HEALTHCARE LLCInventors: Michael Böttger, Georges Degenfeld, Julia Freundlieb, Claudia Hirth-Dietrich, Joerg Keldenich, Jürgen Klar, Uwe Muenster, Andreas Ohm, Annett Richter, Bernd Riedl, Joachim Telser
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Publication number: 20150136143Abstract: The present invention provides improved intravaginal drug delivery devices, i.e., intravaginal rings, useful for the prophylactic administration of dapivirine in combination with either an antimicrobial compound or a contraceptive to a human. The present invention also provides methods of blocking DNA polymerization by an HIV reverse transcriptase enzyme, methods of preventing HIV infection in a female human, methods of treating HIV infection in a female human, methods of preventing unintended pregnancy in a female human, and methods of preparing intravaginal rings.Type: ApplicationFiled: November 13, 2014Publication date: May 21, 2015Inventors: Brid Devlin, Jonathon Daryll Holt, Andrew Nathan Brimer, Jeremy Peter Nuttall, Karl Malcolm, Susan Margaret Fetherston, Peter John James Boyd
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Publication number: 20150141407Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.Type: ApplicationFiled: May 30, 2013Publication date: May 21, 2015Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
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Publication number: 20150141418Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.Type: ApplicationFiled: January 26, 2015Publication date: May 21, 2015Applicant: PTC Therapeutics, Inc.Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
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Publication number: 20150139979Abstract: The present invention provides methods of treating, stabilizing or lessening the severity or progression of a disease or disorder associated with BTK.Type: ApplicationFiled: November 19, 2013Publication date: May 21, 2015Applicant: Celgene Avilomics Research, Inc.Inventors: Tom Daniel, Kenichi Takeshita, Kenneth Foon, Jay Mei
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Patent number: 9034311Abstract: New pyridin-2(1H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: GrantFiled: July 23, 2012Date of Patent: May 19, 2015Assignee: ALMIRALL, S.A.Inventors: Paul Robert Eastwood, Jordi Bach Taña, Lluis Miquel Pages Santacana
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Patent number: 9034881Abstract: Compounds I and II, as well as prodrugs, hydrates, solvates, N-oxides, salts and pharmaceutical compositions containing them, are useful for treating vitiligo. In certain embodiments, the compounds are provided in topical compositions.Type: GrantFiled: September 12, 2013Date of Patent: May 19, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventor: Daniel Magilavy