Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
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Patent number: 10118904Abstract: The invention relates to triazole compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.Type: GrantFiled: June 3, 2016Date of Patent: November 6, 2018Assignee: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Robert J. Davies, Jingrong Cao, Meghan Elise Cockerill, Philip Noel Collier, Elisabeth Doyle, James Daniel Frantz, Huai Gao, Brian Anthony Goldman, Ronald Lee Grey, Jr., Anne-Laure Grillot, Wenxin Gu, James A. Henderson, Raul Eduardo Krauss Irarrazaval, Adrianne Lynn Kolpak, Yusheng Liao, Sanjay Shivayogi Magavi, David Messersmith, Albert Charles Pierce, Emanuele Perola, Elizabeth Jin-Sun Ryu, Joshua Syken, Jian Wang, Michael Paul DeNinno, Francois Maltais
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Patent number: 10111864Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: GrantFiled: April 25, 2017Date of Patent: October 30, 2018Assignee: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Chenggeng Qian
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Patent number: 10106536Abstract: Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related to seizures, pain, neurotransmitter release, etc.Type: GrantFiled: May 10, 2017Date of Patent: October 23, 2018Assignee: Knopp Biosciences LLCInventors: Lynn Resnick, George T. Topalov, Charles A. Flentge, James S. Hale, David A. Mareska
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Patent number: 10064868Abstract: Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.Type: GrantFiled: June 3, 2015Date of Patent: September 4, 2018Assignee: MEI PHARMA, INC.Inventors: S. David Brown, David J. Matthews
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Patent number: 10053465Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.Type: GrantFiled: August 25, 2016Date of Patent: August 21, 2018Assignee: Incyte CorporationInventors: Yun-Long Li, David M. Burns, Hao Feng, Joseph Glenn, Chunhong He, Taisheng Huang, Song Mei, Jun Pan, Xiaozhao Wang, Yingda Ye
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Patent number: 10039846Abstract: Bradykinin B1 receptor (B1R) targeting peptides and compounds are radiolabelled with radioisotopes that are suitable for imaging and/or radiotherapy. The radiolabelled peptides and compounds have utility in imaging tissues expressing or overexpressing B1R and/or treating diseases or conditions in which B1R is expressed or overexpressed, including cancer.Type: GrantFiled: September 13, 2013Date of Patent: August 7, 2018Assignee: BRITISH COLUMBIA CANCER AGENCY BRANCHInventors: Kuo-shyan Lin, Francois Benard, Jinhe Pan, Felix Mesak, Zhengxing Zhang
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Patent number: 10022461Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.Type: GrantFiled: October 4, 2017Date of Patent: July 17, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Abbas M. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
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Patent number: 9994562Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: GrantFiled: March 12, 2014Date of Patent: June 12, 2018Assignee: Celgene Quanticel Research, Inc.Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
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Patent number: 9980961Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: GrantFiled: May 1, 2017Date of Patent: May 29, 2018Assignee: AGIOS PHARMACEUTICALS, INC.Inventors: Shin-San Michael Su, Lenny Dang
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Patent number: 9969731Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.Type: GrantFiled: December 22, 2016Date of Patent: May 15, 2018Assignee: Lupin LimitedInventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 9949981Abstract: The present invention relates to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-(3-morpholinophenyl)-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or N-(1-(3-(3-(4-(1-aminocyclobutyl)phenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-5-yl)phenyl)piperidin-4-yl)-N-methylacetamide. The methods of the present invention can also relate to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing the above compounds in combination with ((R)-6-(2-fluorophenyl)-N-(3-(2-((2-methoxyethyl)amino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine).Type: GrantFiled: September 4, 2015Date of Patent: April 24, 2018Assignee: ArQule, Inc.Inventors: Daniel T. Dransfield, Sudharshan Eathiraj, Jean-Marc Lapierre, Brian Schwartz, Yi Yu
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Patent number: 9938281Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.Type: GrantFiled: November 15, 2013Date of Patent: April 10, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Abdelghani Abe Achab, Michael D. Altman, Yongqi Deng, Solomon Kattar, Jason D. Katz, Joey L. Methot, Hua Zhou, Meredeth McGowan, Matthew P. Christopher, Yudith Garcia, Neville John Anthony, Francesc Xavier Fradera Llinas, Liping Yang, Changwei Mu, Xiaona Wang, Feng Shi, Baijun Ye, Sixing Zhang, Xiaoli Zhao, Rong Zhang, Kin Chiu Fong, Xiansheng Leng
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Patent number: 9938291Abstract: The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is alkyl; A is absent or present, and when present is —C(O)— or —C(O)NH—; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is —C(O)—, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 13, 2014Date of Patent: April 10, 2018Assignee: THE TRUSTESS OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Nicoleta Dobri, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
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Patent number: 9932324Abstract: The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, wherein R1, R2, R3, R4, X, and Z have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).Type: GrantFiled: January 7, 2016Date of Patent: April 3, 2018Assignee: Boehringer Ingelheim International GmbHInventors: Joerg Kley, Joerg P. Hehn, Armin Heckel
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Patent number: 9926324Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: GrantFiled: November 10, 2013Date of Patent: March 27, 2018Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.Inventor: Ning Xi
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Patent number: 9868729Abstract: Provided are methods of treating inflammatory disorders, autoimmune disorders, or a hematological malignancies using compounds of formula I and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof. Such disorders and conditions include leukemia and Non Hodgkin's Lymphoma.Type: GrantFiled: December 5, 2014Date of Patent: January 16, 2018Assignee: PORTOLA PHARMACEUTICALS, INC.Inventors: Shawn M. Bauer, Anjali Pandey
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Patent number: 9850232Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.Type: GrantFiled: March 22, 2016Date of Patent: December 26, 2017Assignee: PFIZER INC.Inventors: David Lawrence Firman Gray, Lei Zhang, Michael Aaron Brodney, Michael Eric Green, Chakrapani Subramanyam
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Patent number: 9834554Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.Type: GrantFiled: December 16, 2014Date of Patent: December 5, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Jian Liu, Ronald M. Kim, Joseph Kozlowski, Deodialsingh Guiadeen, Arto D. Krikorian, Younong Yu
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Patent number: 9737522Abstract: This disclosure relates to NMDA modulators and used related thereto such as for treatment of central nervous system disorders. In certain embodiments, compounds disclosed herein are NR2C subunit-selective NMDA potentiators. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiments, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof. In certain embodiments, the disclosure relates to methods of treating or preventing nervous system disorders comprising administering an effective amount of a composition comprising compound disclosed herein to a subject in need thereof.Type: GrantFiled: August 7, 2013Date of Patent: August 22, 2017Assignee: Emory UniversityInventors: Stephen F. Traynelis, Praseeda Mullasseril, Ethel C Garnier, Dennis C. Liotta, Sommer Zimmerman
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Patent number: 9708318Abstract: The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 and/or FGFR4 enzyme and are useful in the treatment of FGFR-associated diseases.Type: GrantFiled: February 19, 2016Date of Patent: July 18, 2017Assignee: Incyte CorporationInventors: Liang Lu, Bo Shen, Alexander Sokolsky, Xiaozhao Wang, Liangxing Wu, Wenqing Yao, Yingda Ye
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Patent number: 9694001Abstract: Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect. An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).Type: GrantFiled: September 29, 2014Date of Patent: July 4, 2017Assignee: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Hiromi Muraoka, Akira Kanoh
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Patent number: 9682080Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: GrantFiled: October 19, 2015Date of Patent: June 20, 2017Assignee: AGIOS PHARMACEUTICALS, INCInventor: Shin-San Michael Su
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Patent number: 9675612Abstract: The present invention relates to substituted thiazolopyrimidine compounds of general formula I as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful 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 hyperproliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: GrantFiled: March 3, 2014Date of Patent: June 13, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Klar, Lars Wortmann, Keith Graham, Florian Puehler, Detlev Sülzle, Georg Kettschau, Philip Lienau
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Patent number: 9668482Abstract: Provided are: a fused heterocyclic compound by formula (1) or an N-oxide thereof, having excellent control effects against pests: a pest control composition containing the abovementioned compound and an inert carrier; and a pest control method for applying an effective dose of the abovementioned compound to a pest or pest habitat.Type: GrantFiled: March 6, 2015Date of Patent: June 6, 2017Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Takamasa Tanabe, Hajime Mizuno, Hiroshi Okamoto
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Patent number: 9669032Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.Type: GrantFiled: October 15, 2015Date of Patent: June 6, 2017Assignee: Intellikine LLCInventors: Yi Liu, Lynne Bui, Michael Martin, Troy Edward Wilson, Christian Rommel
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Patent number: 9624256Abstract: A coordination complex having a physiologically acceptable pKa includes a metal and a biologically active agent. The pKa of the coordination complex is less than the pKa of the biologically active agent. A pharmaceutical solution for treating a patient includes a coordination complex and water, wherein the coordination complex is at least partially soluble in the water at physiological pH and in a therapeutically efficacious concentration. A method for treating a patient includes administering a pharmaceutical solution including a coordination complex and water to a patient in need of a biologically active agent.Type: GrantFiled: May 29, 2014Date of Patent: April 18, 2017Assignee: SYNTHONICS, INC.Inventors: Thomas Piccariello, John D. Price, Robert A. Oberlender, Michaela E. Mulhare, Mary C. Spencer, Scott B. Palmer
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Patent number: 9624205Abstract: The present invention relates to substituted bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: July 18, 2014Date of Patent: April 18, 2017Assignee: Epizyme, Inc.Inventor: John Emmerson Campbell
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Patent number: 9604939Abstract: Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologs and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.Type: GrantFiled: May 28, 2014Date of Patent: March 28, 2017Assignee: Signal Pharmaceuticals, LLCInventors: Marie Georges Beauchamps, Antonio Christian Ferretti, Juan Antonio Gamboa, Kevin Klopfer, William Edward Konnecke, Matthew Michael Kreilein, Anil Menon, Amanda Nicole Miklos, John Fitzgerald Traverse
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Patent number: 9561245Abstract: The present invention relates to combination therapies for melanoma, and in particular, metastatic melanoma. Drugs for use in such therapies in include BRAF inhibitors such as PLX 4720 and PLX 4734 in combination with RO 31-8220, bafetinib or cardiac glycosides.Type: GrantFiled: September 5, 2013Date of Patent: February 7, 2017Assignee: The Board of Regents of the University of Texas SystemInventors: Sean Morrison, Elena Piskounova, Ugur Eskiocak
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Patent number: 9546168Abstract: Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.Type: GrantFiled: December 12, 2014Date of Patent: January 17, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Kathryn Lipford, Danielle Falcone, David L. Sloman, David J. Witter
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Patent number: 9527847Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).Type: GrantFiled: July 31, 2014Date of Patent: December 27, 2016Assignee: Infinity Pharmaceuticals, Inc.Inventors: Vito J. Palombella, David G. Winkler
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Patent number: 9522916Abstract: This invention relates to compounds of formula (I), Wherein R1-R4 are defined in the Specification, their uses in the practice of medicine, their medicinal formulations, their use in medical diagnosis, and their preparation.Type: GrantFiled: December 19, 2008Date of Patent: December 20, 2016Inventor: Constance Neely Wilson
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Patent number: 9504251Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula I, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X1, Q, and n are as described herein.Type: GrantFiled: May 13, 2015Date of Patent: November 29, 2016Assignee: Dow AgroSciences LLCInventors: Daniel I. Knueppel, Maurice C. Yap, Michael T. Sullenberger, Ricky Hunter, Monica B. Olson, Frank J. Wessels
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Patent number: 9481667Abstract: Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof.Type: GrantFiled: March 13, 2014Date of Patent: November 1, 2016Assignee: Infinity Pharmaceuticals, Inc.Inventors: Daniel G. Genov, Louis Grenier, Andrew B. Hague, Alexander Redvers Eberlin, Ludovic Sylvain Marc Renou, Susana Del Rio Gancedo
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Patent number: 9422283Abstract: The present application relates to salts of Compound A, 3-(3-(4-(1-aminocyclobutyl) phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine, solid state forms of Compound A free base or of salts of Compound A, amorphous forms of Compound A free base or of salts of Compound A, crystalline forms of Compound A free base or of salts of Compound A, polymorphs of Compound A free base or of salts of Compound A, and mesomorphs of Compound A free base or of salts of Compound A. The present application also relates to pharmaceutical compositions comprising these salts, solid state forms, amorphous forms, crystalline forms, polymorphs, or mesomorphs of Compound A free base or of salts of Compound A. The present application provides methods for preparing these salts, solid state forms, amorphous forms, crystalline forms, polymorphs, or mesomorphs of Compound A free base or of salts of Compound A.Type: GrantFiled: April 22, 2015Date of Patent: August 23, 2016Assignee: ArQule, Inc.Inventors: Craig Bates, Jianmin Mao, David Reed
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Patent number: 9409915Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: GrantFiled: February 17, 2015Date of Patent: August 9, 2016Assignee: Janssen Pharmaceutica NVInventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel J. Parks, William J. Parsons, Scott Ballentine, Shawn Branum
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Patent number: 9403827Abstract: The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of as MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: January 21, 2014Date of Patent: August 2, 2016Assignee: NOVARTIS AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Robert Mah, Keiichi Masuya, Achim Schlapbach, Andrea Vaupel
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Patent number: 9403792Abstract: Described herein are compounds that activate pyruvate kinase, for use in a method for increasing lifetime of the red blood cells, for regulating 2,3-diphosphoglycerate levels in blood and for treating sickle cell anemia.Type: GrantFiled: May 3, 2012Date of Patent: August 2, 2016Assignee: AGIOS PHARMACEUTICALS, INCInventor: Shin-San M. Su
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Patent number: 9404081Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: GrantFiled: May 3, 2012Date of Patent: August 2, 2016Assignee: AGIOS PHARMACEUTICALS, INC.Inventor: Shin-San Michael Su
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Patent number: 9388164Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: GrantFiled: May 3, 2012Date of Patent: July 12, 2016Assignee: AGIOS PHARMACEUTICALS, INCInventor: Shin-San M. Su
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Patent number: 9334269Abstract: The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: February 16, 2011Date of Patent: May 10, 2016Assignee: AMGEN INC.Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Bingfan Du, Hanh Nho Nguyen, Xiao Mei Zheng
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Patent number: 9328119Abstract: Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.Type: GrantFiled: September 10, 2014Date of Patent: May 3, 2016Assignee: Alios BioPharma, Inc.Inventors: Robert Than Hendricks, Leonid Beigelman, David Bernard Smith, Antitsa Dimitrova Stoycheva
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Patent number: 9320815Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.Type: GrantFiled: March 11, 2013Date of Patent: April 26, 2016Assignee: President and Fellows of Harvard CollegeInventor: Amin I. Kassis
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Patent number: 9314464Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.Type: GrantFiled: June 28, 2013Date of Patent: April 19, 2016Assignee: Novartis AGInventors: Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
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Patent number: 9278099Abstract: A granulation formulation of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide or pharmaceutically acceptable salt thereof, which is adapted for reconstitution with an aqueous vehicle, and associated oral suspension.Type: GrantFiled: October 16, 2012Date of Patent: March 8, 2016Assignee: Novartis AGInventors: Gossett Augustus Campbell, Helen Richardson, Peter A. Williams
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Patent number: 9249156Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: GrantFiled: March 5, 2014Date of Patent: February 2, 2016Assignee: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian, Rudi Bao
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Patent number: 9242980Abstract: The compound N-(4-{[4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl]oxy}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: August 16, 2011Date of Patent: January 26, 2016Assignee: 3M Innovative Properties CompanyInventor: Paul D. Wightman
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Patent number: 9216964Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: GrantFiled: July 9, 2013Date of Patent: December 22, 2015Assignee: Novartis AGInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Patent number: 9206195Abstract: The present invention relates to dihydrothienopyrimidines, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.Type: GrantFiled: July 27, 2012Date of Patent: December 8, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Kai Gerlach, Niklas Heine, Scott Hobson, Christoph Hoenke, Alexander Weber
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Patent number: RE46856Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyperproliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: GrantFiled: January 5, 2017Date of Patent: May 22, 2018Assignee: Bayer Intellectual Property GMBHInventors: Martin Hentemann, Jill Wood, William Scott, Martin Michels, Ann-Marie Campbell, Ann-Marie Bullion, Bruce R. Rowley, Aniko Redman