Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
  • Patent number: 9561227
    Abstract: The present disclosure provides a method of treating a subject that is resistant to one or more drugs by identifying a subject having one or more drug resistant cells; administering to the subject a pharmaceutically effective amount of an inhibitor compound, and contacting one or more drug resistant cells with the inhibitor compound to reduce the export of the inhibitor compound from the one or more drug resistant tumor cells and to block the transport of drug(s) from the one or more drug resistant cells.
    Type: Grant
    Filed: January 15, 2015
    Date of Patent: February 7, 2017
    Assignee: Southern Methodist University
    Inventors: John G. Wise, Pia D. Vogel, Frances K. Brewer, Courtney A. Follit
  • Patent number: 9562051
    Abstract: The invention provides compounds of formula I: wherein A, B, X, and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds, processes for preparing such compounds, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: February 7, 2017
    Assignee: Rutgers, the State University of New Jersey
    Inventors: Edmond J. LaVoie, Wei Feng, Leroy F. Liu
  • Patent number: 9556147
    Abstract: This application discloses compounds according to generic Formula I: (I) wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: January 31, 2017
    Assignee: HOFFMANN-LA INC.
    Inventors: Christine E. Brotherton-Pleiss, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou
  • Patent number: 9549915
    Abstract: A compound having the following structure: or a pharmaceutically acceptable salt or derivative thereof. The compound may be used in the treatment or prevention of a disorder selected from appetite regulation, obesity, metabolic disorders, cachexia, anorexia, pain, inflammation, neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, Parkinson's disease, levodopa-induced dyskinesia, Huntington's disease, Gilles de la Tourette's syndrome, tardive dyskinesia, dystonia, amyotrophic lateral sclerosis, Alzheimer's disease, epilepsy, schizophrenia, anxiety, depression, insomnia, nausea, emesis, alcohol disorders, drug addictions such as opiates, nicotine, cocaine, alcohol and psychostimulants, hypertension, circulatory shock, myocardial reperfusion injury, atherosclerosis, asthma, glaucoma, retinopathy, cancer, inflammatory bowel disease, acute and chronic liver disease such as hepatitis and liver cirrhosis, arthritis and osteoporosis.
    Type: Grant
    Filed: July 24, 2013
    Date of Patent: January 24, 2017
    Assignee: BIAL-PORTELA & CA, S.A.
    Inventors: Carla Patricia da Costa Pereira Rosa, Rita Gusmao De Noronha, Laszlo Erno Kiss, Patricio Manuel Vieira Araujo Soares Da Silva, Domenico Russo, Jorge Bruno Reis Wahnon, William Maton
  • Patent number: 9550807
    Abstract: The present invention relates to the use of compounds selected from the group consisting of Lys-(D)Pro-Thr, N-acyl Lys-(D)Pro-Thr, C-amide Lys-(D)Pro-Thr, and C-esters of Lys-(D)Pro-Thr; or a pharmaceutically acceptable salt of said compound for the treatment of inflammatory disorders. The invention also relates to the use of ?MSH for inducing tolerance.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: January 24, 2017
    Inventor: Thomas Luger
  • Patent number: 9532977
    Abstract: Provided herein are controlled release oral dosage forms of poorly soluble drugs, methods of making the dosage forms, and methods of their use for the treatment of various diseases and/or disorders.
    Type: Grant
    Filed: November 11, 2015
    Date of Patent: January 3, 2017
    Assignee: Celgene Corporation
    Inventors: Ming J. Chen, Ho-Wah Hui, Xiaole Shen
  • Patent number: 9533954
    Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.
    Type: Grant
    Filed: May 1, 2014
    Date of Patent: January 3, 2017
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Wenqing Yao, Colin Zhang, Meizhong Xu, Jincong Zhuo, Chunhong He
  • Patent number: 9527869
    Abstract: Compounds of formula (I), defined herein, inhibit phosphoinositide 3-kinases (PI3K) and are useful for the treatment of disorders associated with PI3K enzymes.
    Type: Grant
    Filed: June 17, 2015
    Date of Patent: December 27, 2016
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Matteo Biagetti, Alessandro Accetta, Anna Maria Capelli, Matilde Guala, Michele Retini
  • Patent number: 9512130
    Abstract: The present invention relates to substituted imidazopyridazine compounds, to methods of 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: Grant
    Filed: February 25, 2014
    Date of Patent: December 6, 2016
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Marcus Koppitz, Ulrich Klar, Antje Margret Wengner, Roland Neuhaus, Gerhard Siemeister, Michael Brüning
  • Patent number: 9493470
    Abstract: Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyljbenzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methyl piperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein. The instant application is directed to novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl}phenyl}benzamide and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, compositions comprising such crystalline forms, and to methods of their preparation and use.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: November 15, 2016
    Assignee: ARIAD PHARMACEUTICALS, INC.
    Inventors: Christopher K. Murray, Leonard W. Rozamus, John J. Chaber, Pradeep Sharma
  • Patent number: 9457029
    Abstract: The present invention relates to methods for preventing or treating of metabolic disorders and related conditions, such as in certain patient groups.
    Type: Grant
    Filed: November 26, 2010
    Date of Patent: October 4, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Michael Mark, Hans-Juergen Woerle, Heike Zimdahl-Gelling
  • Patent number: 9440976
    Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: September 13, 2016
    Assignee: GENENTECH, INC.
    Inventors: Hazel Joan Dyke, Lewis Gazzard, Karen Williams, Huifen Chen, Samuel Kintz, Joy Drobnick, Joseph P. Lyssikatos, Simon Goodacre, Calum Macleod, Charles Ellwood
  • Patent number: 9427439
    Abstract: The present invention provides methods and compositions for promoting recovery of function from neurologic injury, such as ischemic injury caused by acute stroke.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: August 30, 2016
    Assignee: EIP Pharma, LLC
    Inventor: John Jahangir Alam
  • Patent number: 9415107
    Abstract: The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamo-pituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: August 16, 2016
    Assignee: Board Of Supervisors Of Louisiana State University & Agricultural & Mechanical College
    Inventor: Nicholas E. Goeders
  • Patent number: 9416132
    Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: August 16, 2016
    Assignee: Tolero Pharmaceuticals, Inc.
    Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
  • Patent number: 9399019
    Abstract: The described invention provides a biodegradable, biocompatible delivery system of flowable sustained release microparticulate composition of a substantially pure crystalline form of a bioactive agent such as, for example, nimodipine, a process of preparing a therapeutic form of a substantially pure crystalline form of the bioactive agent and a method for treating an interruption of a cerebral artery in a subarachnoid space at risk of interruption caused by brain injury in a mammal, which reduces signs or symptoms of at least one delayed complication associated with brain injury.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: July 26, 2016
    Assignees: Evonik Corporation, Edge Therapeutics, Inc.
    Inventors: R. Loch Macdonald, Cara R. Davis, Kevin Burton, Gary Winchester, Angela R. Stella, Parissa Heshmati
  • Patent number: 9394299
    Abstract: The present application discloses Rilyazine analogs, methods for their preparation, and the treatment of cancer by the administration of an effective amount of the Rilyazine analogs to a patient in need thereof.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: July 19, 2016
    Assignee: Warner Babcock Institute for Green Chemistry, LLC
    Inventors: John C. Warner, Jeffery A. Gladding, Thomas W. Gero, Srinivasa R. Cheruku
  • Patent number: 9382277
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: July 5, 2016
    Assignee: Asana Biosciences, LLC
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Patent number: 9370515
    Abstract: Provided herein are imidazopyridine compounds having an inhibitory effect on mixed lineage kinases (MLKs), methods of their synthesis, and methods of their therapeutic. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: June 21, 2016
    Assignees: CALIFIA BIO, INC., UNIVERSITY OF ROCHESTER
    Inventors: Val S. Goodfellow, Thong X. Nguyen, Satheesh B. Ravula, Harris A. Gelbard
  • Patent number: 9328111
    Abstract: The present invention provides a compound of Formula (I): wherein the variables Z, n, Y and p are as defined herein, and pharmaceutically acceptable salts thereof, which can inhibit the activity of poly (ADP-ribose)polymerases, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: December 31, 2011
    Date of Patent: May 3, 2016
    Assignee: BeiGene Ltd.
    Inventors: Changyou Zhou, Bo Ren, Hexiang Wang
  • Patent number: 9328059
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating autophagy-related diseases, angiogenic diseases or hypermelanosis, comprising: (a) a pharmaceutically effective amount of an indatraline derivative or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier. The composition of the present invention effectively induces autophagy of cells, and thus is very effective for preventing or treating autophagy-related diseases. In addition, the composition of the present invention inhibits angiogenesis through the mechanism of inhibiting angiogenesis, invasion and metastasis and inhibits melanogenesis, and thus can also be effective for preventing or treating angiogenic diseases or melanin-related diseases.
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: May 3, 2016
    Assignee: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
    Inventors: Ho Jeong Kwon, Yoon Sun Cho
  • Patent number: 9321781
    Abstract: The invention provides compounds of formula I: (I) wherein A, B, W, Y, Z, R1, R3 and R4 have any of the meanings defined in the specification and their salts as well as additional compounds and their salts. The invention also provides pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treating cancer, a bacterial infection or a fungal infection using compounds of the invention.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: April 26, 2016
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. Lavoie, Ajit K. Parhi
  • Patent number: 9315509
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: April 19, 2016
    Assignee: Celtaxsys, Inc.
    Inventors: Damian O. Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, Guo Ping Wei, Bin Ye
  • Patent number: 9310374
    Abstract: The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: April 12, 2016
    Assignee: REDWOOD BIOSCIENCE, INC.
    Inventors: Romas Alvydas Kudirka, Aaron Edward Albers, Robyn M. Barfield, David Rabuka
  • Patent number: 9308177
    Abstract: The invention relates to a controlled release composition comprising a combination of isosorbide dinitrate and hydralazine, such as hydralazine hydrochloride, that in operation delivers the drug in a pulsed or multi-modal manner for the treatment of angina, ischaemic heart disease, arterial hypertension and related disease conditions. Preferably, the isosorbide dinitrate and hydralazine hydrochloride can be released from the dosage form in an erodable, diffusion and/or osmotic-controlled release profile.
    Type: Grant
    Filed: March 4, 2015
    Date of Patent: April 12, 2016
    Assignee: Recro Technology LLC
    Inventors: Gurvinder Singh Rekhi, Richard Sidwell, Sharon Hamm
  • Patent number: 9295664
    Abstract: In one aspect, the invention relates to methods for treating muscle atrophy by providing to an animal in need thereof an effective amount of a compound. The compound can modulate the expression levels of multiple mRNA of a muscle atrophy signature. 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: Grant
    Filed: June 6, 2012
    Date of Patent: March 29, 2016
    Assignee: UNIVERSITY OF IOWA RESEARCH FOUNDATION
    Inventors: Christopher M. Adams, Steven D. Kunkel, Michael Welsh
  • Patent number: 9290468
    Abstract: Disclosed are compound of formula (I) and pharmaceutically accepted salts and prodrugs thereof, wherein each of R1, R2, R3, R4, R5, R6, X1 and X2 is as defined in the description. These compounds are protein kinases inhibitors, especially the inhibitors of Mek, which are useful in the treatment of cancers and inflammation of mammals. Disclosed are the treatment methods of cancers and inflammation of mammals as well as pharmaceutical compositions comprising the compounds described herein. The preparation of benzoheterocyclic compounds are disclosed. Disclosed are the preparation of potential drug candidates, such as benzooxazol, benzothiazol, benzothiadiazol and the like.
    Type: Grant
    Filed: January 16, 2013
    Date of Patent: March 22, 2016
    Assignee: SHANGHAI KECHOW PHARMA, INC.
    Inventors: Hongqi Tian, Conghui Ji, Chunlei Liu, Li Kong, Ying Cheng, Gongchao Huang
  • Patent number: 9283222
    Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: March 15, 2016
    Assignee: AbbVie Inc.
    Inventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
  • Patent number: 9278965
    Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A??I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: March 8, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael J. Mayer, Jason L. Davis, Shuangyi Wan
  • Patent number: 9272022
    Abstract: The invention provides methods for treating or decreasing the likelihood of developing a stress-granule related disorder and/or cancer by administering one or more poly-ADP-ribose polymerase (PARP) inhibitors, one or more PARP activators, one or more poly-ADP-ribose glycosylase (PARG) activators, and/or one or more poly-ADP-ribose glycohydrolase ARH3 activators. The invention also provides corresponding methods of decreasing stress granule formation and/or proliferation in a cell or a population of cells. The invention further provides methods of increasing the number of stress granules and proliferation in a cell or a population of cells by administering one or more PARP activators, one or more PARP inhibitors, one or more PARG inhibitors, and/or one or more ARH3 inhibitors.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: March 1, 2016
    Assignee: Massachusetts Institute of Technology
    Inventors: Paul Chang, Sejal K. Vyas, Anthony Leung, Phillip A. Sharp
  • Patent number: 9266888
    Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
    Type: Grant
    Filed: August 19, 2014
    Date of Patent: February 23, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Peter Sieger, Dirk Kemmer, Peter Kohlbauer, Thomas Nicola, Martin Renz
  • Patent number: 9260381
    Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: February 16, 2016
    Assignee: USHER III INITIATIVE, INC.
    Inventors: Roland Werner Bürli, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E Harte
  • Patent number: 9254288
    Abstract: This disclosure provides tyrosine kinase protein and nucleic acid variants, particularly FGFR2 variants, which are linked to drug resistance. The disclosure further provides methods of diagnosis and theranosis, using these molecules and fragments thereof, and kits for employing these methods and compositions.
    Type: Grant
    Filed: May 7, 2013
    Date of Patent: February 9, 2016
    Assignees: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE, QUEENSLAND UNIVERSITY OF TECHNOLOGY
    Inventor: Pamela Michelle Pollock
  • Patent number: 9249154
    Abstract: Novel compound having the following formula: Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: February 2, 2016
    Inventor: Zhanggui Wu
  • Patent number: 9242966
    Abstract: A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: January 26, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Heather Finlay, Ashok Kumar Adisechan, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
  • Patent number: 9227975
    Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: January 5, 2016
    Assignee: Array BioPharma, Inc.
    Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
  • Patent number: 9221767
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: December 29, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter W. Glunz, Yan Zou, Mimi L. Quan
  • Patent number: 9216995
    Abstract: An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Grant
    Filed: April 11, 2011
    Date of Patent: December 22, 2015
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Kazunari Hattori, Kenji Tomita
  • Patent number: 9206161
    Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: December 8, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Patent number: 9200005
    Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Grant
    Filed: February 25, 2014
    Date of Patent: December 1, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Katja Jantos, Michael Ochse, Hervé Geneste, Jayne Froggett, Clarissa Jakob, Karla Drescher, Jürgen Dinges
  • Patent number: 9187473
    Abstract: Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.
    Type: Grant
    Filed: May 29, 2014
    Date of Patent: November 17, 2015
    Assignee: ARRIEN PHARMACEUTICALS LLC
    Inventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
  • Patent number: 9187475
    Abstract: The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Grant
    Filed: April 25, 2013
    Date of Patent: November 17, 2015
    Assignee: RaQualia Pharma Inc.
    Inventors: Kiyoshi Kawamura, Mikio Morita, Tatsuya Yamagishi
  • Patent number: 9186392
    Abstract: The present invention relates to methods for treating and/or preventing metabolic diseases comprising the combined administration of a GLP-1 receptor agonist and a DPP-4 inhibitor.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: November 17, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thomas Klein, Rolf Grempler, Michael Mark
  • Patent number: 9181244
    Abstract: The present invention pertains to field of medical technology, specifically relates to a pyridino-oxopyridazine derivative of formula (I), its pharmaceutically acceptable salts, its stereoisomers or its solvates, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R7?, R8?, R9?, L and ring A are defined as the description; the present invention further relates to methods for preparing the compounds, a pharmaceutical composition comprising the compound, and use of the compound and the pharmaceutical composition in manufacture of a medicament for treatment and/or prophylaxis of an inflammatory disease, symptom and condition characterized in undesired inflammatory immunoreaction or associated with undesired inflammatory immunoreaction, as well as all diseases induced by oversecretion of TNF-? and PDE-4 or associated with oversecretion of TNF-? and PDE-4.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: November 10, 2015
    Assignee: XUANZHU PHARMA CO., LTD.
    Inventors: Frank Wu, Liang Sun
  • Patent number: 9174996
    Abstract: The present invention relates to compounds of Formula VIII with absolute configuration R or S: as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula VIII, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
    Type: Grant
    Filed: August 26, 2014
    Date of Patent: November 3, 2015
    Assignee: Astar Biotech LLC
    Inventors: Chunrong Yu, Haihong Huang, Dongfeng Zhang, Peng Li
  • Patent number: 9173884
    Abstract: The present intervention generally relates to compositions comprising a PDE11 inhibitor for increasing cortisol levels in a subject, or for increasing the production of cortisol from adenocortical cells in a subject. Aspects of the invention relate to the use of a PDE11 inhibitor in a method of treatment of low cortisol levels and/or adrenal insufficiency in a subject, or a method of treating a disease or disorders associated with adrenal insufficiency. Aspects of the invention relate to PDE11 inhibitors belonging to compounds of formula (I)-(VI), and their use alone or in combination with long-term corticosteroid treatment to elevate cortisol levels in a subject, and/or to treat adrenal insufficiency.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: November 3, 2015
    Assignee: Trustees of Boston College
    Inventors: Charles Stuart Hoffman, Ozge Ceyhan
  • Patent number: 9173864
    Abstract: Described herein are compositions and methods of treating and/or preventing inner ear conditions by administering to a patient in need thereof a modulator of a metabotropic glutamate receptor.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: November 3, 2015
    Assignee: House Ear Institute
    Inventors: Rick Friedman, Benedikt Vollrath
  • Patent number: 9169235
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: October 27, 2015
    Assignee: KUDOS PHARMACEUTICALS LIMITED
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • Patent number: 9162953
    Abstract: The present invention relates to a process for creating a Carbon-Carbon bond (C—C) or a Carbon-Heteroatom bond (C-HE) by reacting a compound carrying a leaving group with a nucleophilic compound carrying a carbon atom or a heteroatom (HE) that can substitute for the leaving group, creating a C—C or C-HE bond, wherein the reaction takes place in the presence of an effective quantity of a catalytic system comprising iron and copper.
    Type: Grant
    Filed: July 4, 2007
    Date of Patent: October 20, 2015
    Assignees: CENTRE NATIONALE DE RECHERCHE SCIENTIFIQUE, ECOLE NATIONALE SUPERIEURE DE CHIMIE DE MONTPELLIER
    Inventors: Marc Taillefer, Ning Xia, Armelle Ouali
  • Patent number: 9156820
    Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: October 13, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak