Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
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Patent number: 9556147Abstract: 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: GrantFiled: March 3, 2014Date of Patent: January 31, 2017Assignee: HOFFMANN-LA INC.Inventors: Christine E. Brotherton-Pleiss, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou
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Patent number: 9549915Abstract: 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: GrantFiled: July 24, 2013Date of Patent: January 24, 2017Assignee: 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
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Patent number: 9550807Abstract: 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: GrantFiled: August 25, 2014Date of Patent: January 24, 2017Inventor: Thomas Luger
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Patent number: 9532977Abstract: 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: GrantFiled: November 11, 2015Date of Patent: January 3, 2017Assignee: Celgene CorporationInventors: Ming J. Chen, Ho-Wah Hui, Xiaole Shen
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Patent number: 9533954Abstract: 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: GrantFiled: May 1, 2014Date of Patent: January 3, 2017Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Wenqing Yao, Colin Zhang, Meizhong Xu, Jincong Zhuo, Chunhong He
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Patent number: 9527869Abstract: Compounds of formula (I), defined herein, inhibit phosphoinositide 3-kinases (PI3K) and are useful for the treatment of disorders associated with PI3K enzymes.Type: GrantFiled: June 17, 2015Date of Patent: December 27, 2016Assignee: CHIESI FARMACEUTICI S.p.A.Inventors: Matteo Biagetti, Alessandro Accetta, Anna Maria Capelli, Matilde Guala, Michele Retini
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Patent number: 9512130Abstract: 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: GrantFiled: February 25, 2014Date of Patent: December 6, 2016Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Marcus Koppitz, Ulrich Klar, Antje Margret Wengner, Roland Neuhaus, Gerhard Siemeister, Michael Brüning
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Patent number: 9493470Abstract: 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: GrantFiled: December 12, 2013Date of Patent: November 15, 2016Assignee: ARIAD PHARMACEUTICALS, INC.Inventors: Christopher K. Murray, Leonard W. Rozamus, John J. Chaber, Pradeep Sharma
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Patent number: 9457029Abstract: The present invention relates to methods for preventing or treating of metabolic disorders and related conditions, such as in certain patient groups.Type: GrantFiled: November 26, 2010Date of Patent: October 4, 2016Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Michael Mark, Hans-Juergen Woerle, Heike Zimdahl-Gelling
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Patent number: 9440976Abstract: 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: GrantFiled: June 18, 2015Date of Patent: September 13, 2016Assignee: 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
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Patent number: 9427439Abstract: The present invention provides methods and compositions for promoting recovery of function from neurologic injury, such as ischemic injury caused by acute stroke.Type: GrantFiled: October 26, 2015Date of Patent: August 30, 2016Assignee: EIP Pharma, LLCInventor: John Jahangir Alam
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Patent number: 9416132Abstract: 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: GrantFiled: July 20, 2012Date of Patent: August 16, 2016Assignee: Tolero Pharmaceuticals, Inc.Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
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Patent number: 9415107Abstract: 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: GrantFiled: November 13, 2006Date of Patent: August 16, 2016Assignee: Board Of Supervisors Of Louisiana State University & Agricultural & Mechanical CollegeInventor: Nicholas E. Goeders
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Patent number: 9399019Abstract: 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: GrantFiled: March 13, 2013Date of Patent: July 26, 2016Assignees: Evonik Corporation, Edge Therapeutics, Inc.Inventors: R. Loch Macdonald, Cara R. Davis, Kevin Burton, Gary Winchester, Angela R. Stella, Parissa Heshmati
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Patent number: 9394299Abstract: 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: GrantFiled: August 29, 2014Date of Patent: July 19, 2016Assignee: Warner Babcock Institute for Green Chemistry, LLCInventors: John C. Warner, Jeffery A. Gladding, Thomas W. Gero, Srinivasa R. Cheruku
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Patent number: 9382277Abstract: 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: GrantFiled: April 3, 2014Date of Patent: July 5, 2016Assignee: Asana Biosciences, LLCInventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
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Patent number: 9370515Abstract: 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: GrantFiled: March 7, 2014Date of Patent: June 21, 2016Assignees: CALIFIA BIO, INC., UNIVERSITY OF ROCHESTERInventors: Val S. Goodfellow, Thong X. Nguyen, Satheesh B. Ravula, Harris A. Gelbard
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Patent number: 9328059Abstract: 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: GrantFiled: September 6, 2011Date of Patent: May 3, 2016Assignee: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITYInventors: Ho Jeong Kwon, Yoon Sun Cho
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Patent number: 9328111Abstract: 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: GrantFiled: December 31, 2011Date of Patent: May 3, 2016Assignee: BeiGene Ltd.Inventors: Changyou Zhou, Bo Ren, Hexiang Wang
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Patent number: 9321781Abstract: 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: GrantFiled: November 4, 2010Date of Patent: April 26, 2016Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. Lavoie, Ajit K. Parhi
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Patent number: 9315509Abstract: 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: GrantFiled: June 24, 2014Date of Patent: April 19, 2016Assignee: 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
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Patent number: 9310374Abstract: 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: GrantFiled: March 11, 2013Date of Patent: April 12, 2016Assignee: REDWOOD BIOSCIENCE, INC.Inventors: Romas Alvydas Kudirka, Aaron Edward Albers, Robyn M. Barfield, David Rabuka
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Patent number: 9308177Abstract: 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: GrantFiled: March 4, 2015Date of Patent: April 12, 2016Assignee: Recro Technology LLCInventors: Gurvinder Singh Rekhi, Richard Sidwell, Sharon Hamm
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Patent number: 9295664Abstract: 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: GrantFiled: June 6, 2012Date of Patent: March 29, 2016Assignee: UNIVERSITY OF IOWA RESEARCH FOUNDATIONInventors: Christopher M. Adams, Steven D. Kunkel, Michael Welsh
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Patent number: 9290468Abstract: 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: GrantFiled: January 16, 2013Date of Patent: March 22, 2016Assignee: SHANGHAI KECHOW PHARMA, INC.Inventors: Hongqi Tian, Conghui Ji, Chunlei Liu, Li Kong, Ying Cheng, Gongchao Huang
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Patent number: 9283222Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.Type: GrantFiled: May 24, 2013Date of Patent: March 15, 2016Assignee: AbbVie Inc.Inventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
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Patent number: 9278965Abstract: 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: GrantFiled: October 2, 2013Date of Patent: March 8, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael J. Mayer, Jason L. Davis, Shuangyi Wan
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Patent number: 9272022Abstract: 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: GrantFiled: March 30, 2012Date of Patent: March 1, 2016Assignee: Massachusetts Institute of TechnologyInventors: Paul Chang, Sejal K. Vyas, Anthony Leung, Phillip A. Sharp
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Patent number: 9266888Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.Type: GrantFiled: August 19, 2014Date of Patent: February 23, 2016Assignee: Boehringer Ingelheim International GmbHInventors: Peter Sieger, Dirk Kemmer, Peter Kohlbauer, Thomas Nicola, Martin Renz
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Patent number: 9260381Abstract: 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: GrantFiled: June 4, 2015Date of Patent: February 16, 2016Assignee: USHER III INITIATIVE, INC.Inventors: Roland Werner Bürli, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E Harte
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Patent number: 9254288Abstract: 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: GrantFiled: May 7, 2013Date of Patent: February 9, 2016Assignees: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE, QUEENSLAND UNIVERSITY OF TECHNOLOGYInventor: Pamela Michelle Pollock
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Patent number: 9249154Abstract: 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: GrantFiled: November 2, 2012Date of Patent: February 2, 2016Inventor: Zhanggui Wu
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Patent number: 9242966Abstract: 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: GrantFiled: March 7, 2014Date of Patent: January 26, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Heather Finlay, Ashok Kumar Adisechan, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
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Patent number: 9227975Abstract: 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: GrantFiled: September 13, 2012Date of Patent: January 5, 2016Assignee: Array BioPharma, Inc.Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
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Patent number: 9221767Abstract: 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: GrantFiled: January 17, 2014Date of Patent: December 29, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Peter W. Glunz, Yan Zou, Mimi L. Quan
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Patent number: 9216995Abstract: 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: GrantFiled: April 11, 2011Date of Patent: December 22, 2015Assignee: SHIONOGI & CO., LTD.Inventors: Kazunari Hattori, Kenji Tomita
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Patent number: 9206161Abstract: 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: GrantFiled: January 9, 2015Date of Patent: December 8, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
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Patent number: 9200005Abstract: 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: GrantFiled: February 25, 2014Date of Patent: December 1, 2015Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.Inventors: Katja Jantos, Michael Ochse, Hervé Geneste, Jayne Froggett, Clarissa Jakob, Karla Drescher, Jürgen Dinges
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Patent number: 9187473Abstract: 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: GrantFiled: May 29, 2014Date of Patent: November 17, 2015Assignee: ARRIEN PHARMACEUTICALS LLCInventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
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Patent number: 9186392Abstract: 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: GrantFiled: May 5, 2011Date of Patent: November 17, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Thomas Klein, Rolf Grempler, Michael Mark
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Patent number: 9187475Abstract: 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: GrantFiled: April 25, 2013Date of Patent: November 17, 2015Assignee: RaQualia Pharma Inc.Inventors: Kiyoshi Kawamura, Mikio Morita, Tatsuya Yamagishi
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Patent number: 9181244Abstract: 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: GrantFiled: July 23, 2014Date of Patent: November 10, 2015Assignee: XUANZHU PHARMA CO., LTD.Inventors: Frank Wu, Liang Sun
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Patent number: 9173864Abstract: 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: GrantFiled: October 19, 2009Date of Patent: November 3, 2015Assignee: House Ear InstituteInventors: Rick Friedman, Benedikt Vollrath
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Patent number: 9173884Abstract: 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: GrantFiled: November 29, 2012Date of Patent: November 3, 2015Assignee: Trustees of Boston CollegeInventors: Charles Stuart Hoffman, Ozge Ceyhan
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Patent number: 9174996Abstract: 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: GrantFiled: August 26, 2014Date of Patent: November 3, 2015Assignee: Astar Biotech LLCInventors: Chunrong Yu, Haihong Huang, Dongfeng Zhang, Peng Li
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Patent number: 9169235Abstract: 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: GrantFiled: September 11, 2014Date of Patent: October 27, 2015Assignee: KUDOS PHARMACEUTICALS LIMITEDInventors: 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
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Patent number: 9162953Abstract: 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: GrantFiled: July 4, 2007Date of Patent: October 20, 2015Assignees: CENTRE NATIONALE DE RECHERCHE SCIENTIFIQUE, ECOLE NATIONALE SUPERIEURE DE CHIMIE DE MONTPELLIERInventors: Marc Taillefer, Ning Xia, Armelle Ouali
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Patent number: 9156820Abstract: 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: GrantFiled: April 24, 2014Date of Patent: October 13, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Patent number: 9139579Abstract: The invention relates to novel heteroaryl carboxamides, a process for their preparation, and pharmaceutical compositions containing them. These materials are useful for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.Type: GrantFiled: July 9, 2012Date of Patent: September 22, 2015Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Martin Hendrix, Frank-Gerhard Böβ, Christina Erb, Joachim Krüger, Joachim Luithle, Christoph Methfessel, Rudy Schreiber, Welf-Burkhard Wiese
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Patent number: 9137973Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: December 1, 2011Date of Patent: September 22, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Boyall, Guy Brenchley, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo