Additional Hetero Ring Containing Patents (Class 546/268.1)
  • Patent number: 10526312
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: January 28, 2019
    Date of Patent: January 7, 2020
    Assignee: Mycovia Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • Patent number: 10407406
    Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.
    Type: Grant
    Filed: February 13, 2018
    Date of Patent: September 10, 2019
    Assignee: Georgetown University
    Inventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu
  • Patent number: 10259784
    Abstract: The present invention relates to methods of synthesizing aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phosphoramide or a phosphoramide-derived catalyst. The present invention also relates to aziridines, modified aziridines and aziridine-derived compounds preparable by the aforementioned methods, and to phosphoramide or phosphoramide-derived catalysts suitable for use in such methods.
    Type: Grant
    Filed: August 14, 2017
    Date of Patent: April 16, 2019
    Assignee: University of East Anglia
    Inventors: Sean Patrick Bew, Sean Michael Thurston, Paolo Pesce
  • Patent number: 10221160
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: March 5, 2019
    Assignee: Mycovia Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • Patent number: 10077250
    Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: September 18, 2018
    Assignees: Mycovia Pharmaceuticals, Inc., Tlie United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: William J. Hoekstra, Christopher M. Yates, Mark Behnke, Asaf Alimardanov, Scott A. David, Douglas Franklin Fry
  • Patent number: 9963441
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. 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: Grant
    Filed: November 17, 2016
    Date of Patent: May 8, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9920046
    Abstract: To provide a novel pesticide, especially a fungicide and a nematocide.
    Type: Grant
    Filed: July 12, 2016
    Date of Patent: March 20, 2018
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Motoyoshi Iwasa, Keisuke Tsuji, Mitsutaka Tomizawa, Takeshi Mita, Hidehito Kuwahara, Miho Asahi, Hotaka Imanaka
  • Patent number: 9902713
    Abstract: Provided herein are compositions and methods for reducing one or both of axonal degeneration and neuronal cell death associated with a disease or traumatic brain injury. An aminopropyl carbazole agent with potent neuroprotective properties is described. Specifically, (?)-(S)-N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine, is proposed as a new pharmacological agent for protecting patients against axonal degeneration and chronic consequences of TBI.
    Type: Grant
    Filed: November 11, 2014
    Date of Patent: February 27, 2018
    Assignees: Board of Regents of the University of Texas System, University of Iowa Research Foundation
    Inventors: Steven L. McKnight, Joseph M. Ready, Andrew A. Pieper
  • Patent number: 9890238
    Abstract: The present invention relates to a curing catalyst for an epoxy resin composition represented by chemical formula 1, an epoxy resin composition comprising the same, and an apparatus manufactured using the same.
    Type: Grant
    Filed: May 16, 2014
    Date of Patent: February 13, 2018
    Assignee: Samsung SDI Co., Ltd.
    Inventors: Jung Seob Kim, Min Gyum Kim, Dong Hwan Lee, Jin Min Cheon, Hwan Sung Cheon, Seung Han
  • Patent number: 9732034
    Abstract: The present invention relates to methods of synthesizing aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phosphoramide or a phosphoramide-derived catalyst. The present invention also relates to aziridines, modified aziridines and aziridine-derived compounds preparable by the aforementioned methods, and to phosphoramide or phosphoramide-derived catalysts suitable for use in such methods.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: August 15, 2017
    Assignee: University of East Anglia
    Inventors: Sean Patrick Bew, Sean Michael Thurston, Paolo Pesce
  • Patent number: 9617275
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced ?-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: April 11, 2017
    Assignee: Pfizer Inc.
    Inventors: Jotham Wadsworth Coe, John Arthur Allen, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Edward Raymond Guilmette, Anthony Richard Harris, Chris John Helal, Jaclyn Louise Henderson, Scot Richard Mente, Deane Milford Nason, Steven Victor O'Neil, Chakrapani Subramanyam, Wenjian Xu
  • Patent number: 9512112
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: December 6, 2016
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • Patent number: 9346784
    Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: May 24, 2016
    Assignees: Georgetown University, Duke University
    Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
  • Patent number: 9303017
    Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 5, 2016
    Assignees: Georgetown University, Duke University
    Inventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu, Edward D. Levin, Amir H. Rezvani
  • Patent number: 9249159
    Abstract: The present invention relates a novel composition for preventing or treating hepatitis C virus, regulating the phosphorylation of a replicase. More specifically, it is possible to prevent or treat hepatitis C using a novel PRK2 inhibitor discovered through structure modeling, and to prevent or treat hepatitis C, particularly, interferon-insensitive hepatitis C through coadministration of an Hsp90 inhibitor.
    Type: Grant
    Filed: April 23, 2012
    Date of Patent: February 2, 2016
    Assignee: Industry-Academic Cooperation Foundation, Yonsei University
    Inventor: Jong-Won Oh
  • Patent number: 9180123
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: November 10, 2015
    Assignee: Pfizer Inc.
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joesph Melnick, Justin Ian Montgomery, Usa Reilly
  • Patent number: 9051283
    Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: June 9, 2015
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Hiroyoshi Yamada, Hisashi Mihara, Norio Seki
  • Patent number: 9040534
    Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
  • Patent number: 9040708
    Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has two or more substituents selected, for example, from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, and cyano; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.
    Type: Grant
    Filed: October 31, 2012
    Date of Patent: May 26, 2015
    Assignees: Syngenta Limited, Syngenta Participations AG
    Inventors: Thomas Pitterna, Olivier Loiseleur, Paul Anthony Worthington, Anthony Cornelius O'Sullivan, Torsten Luksch, Vladimir Bobosik
  • Patent number: 9029392
    Abstract: Disclosed are a series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: May 12, 2015
    Assignee: UCB Pharma S.A.
    Inventors: Andrew Harry Parton, Mezher Hussein Ali, Daniel Christopher Brookings, Julien Alistair Brown, Daniel James Ford, Richard Jeremy Franklin, Judi Charlotte Neuss, Joanna Rachel Quincey, Jackalyn Hinkins
  • Patent number: 9018383
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: April 28, 2015
    Assignee: Sanofi
    Inventors: Josef Pernerstorfer, Heinz-Werner Kleemann, Matthias Schaefer, Alena Safarova, Marcel Patek
  • Patent number: 9012651
    Abstract: Disclosed herein are modulators of TRPV3 of formula (I) wherein X1, X2, R1, R2, Rx, and n are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: April 21, 2015
    Assignee: AbbVie Inc.
    Inventors: Bruce Clapham, Phil B. Cox, Michael J. Dart, Arthur Gomtsyan, Tammie K. Jinkerson, Ryan G. Keddy, Michael E. Kort, Philip R. Kym, Mark Matulenko, Robert G. Schmidt, Clara I. Villamil, Eric A. Voight, Kevin R. Woller
  • Patent number: 8993758
    Abstract: Disclosed herein are compounds of formula (I) and methods of inhibiting IKK? and the NF-?B signaling and mTOR pathways.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: March 31, 2015
    Assignees: Board of Regents of the University of Nebraska, The Board of Regents, University of Texas System
    Inventors: Amarnath Natarajan, Qianyi Chen, Vashti C. Bryant, Rajkumar Rajule
  • Patent number: 8987308
    Abstract: Disclosed are compounds of formula (I): or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Summit Corporation Plc
    Inventors: Peter David Johnson, Richard John Vickers, Francis Xavier Wilson, Colin Richard Dorgan, Lauren Jayne Sudlow, Stephen Paul Wren, Renate van Well
  • Publication number: 20150080578
    Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
    Type: Application
    Filed: July 8, 2014
    Publication date: March 19, 2015
    Inventors: John K. Thottathil, Raymond P. Warrell
  • Publication number: 20150080362
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 19, 2015
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Tamil Arasu, John David Baird, Wu Du, Olya Ginzburg, Yi Jin Kim Gorske, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Anthony Allan Turpoff, Richard Gerald Wilde, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20150065478
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Patrick Rene Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Patent number: 8969352
    Abstract: The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 3, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Christine F. Gelin, Terry P. Lebold, Brock T. Shireman
  • Patent number: 8969553
    Abstract: Process for the selective N-sulfonylation of oxindoles, in particular process for the N-sulfonylation of 3-triazinyloxindoles, and also N-sulfonyl-substituted 3-triazinyloxindoles and the use of N-sulfonyl-substituted oxindoles and of N-sulfonyl-substituted 3-triazinyloxindoles as intermediates for the synthesis of fine chemicals and of active ingredients in the field of pharmacy and agriculture, and also the use of these compounds as active ingredients in the field of agriculture.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: March 3, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Gunter Karig, Mark James Ford, Konrad Siegel, Stefan Schnatterer
  • Patent number: 8969349
    Abstract: Provided herein are compounds of formula A-L-B, and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is R1 and R2 together with the carbon atoms to which they are attached form a 1,2-phenylene ring optionally substituted with one or more R11; L is —C(R6)2—C(R6)2—; B is a heteroaromatic group defined herein; and -A1-A2- , A3, R11 and R6 are defined herein. Also disclosed are methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: March 3, 2015
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: John Emmerson Campbell, Michael Charles Hewitt, Philip Jones, Linghong Xie
  • Patent number: 8969335
    Abstract: Compounds of the formula I, in which R1, R2, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: March 3, 2015
    Assignee: MERCK PATENT GmbH
    Inventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler
  • Patent number: 8962835
    Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 24, 2015
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Patent number: 8962660
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: February 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Hao Zhang, Peter T. W. Cheng, Sean Chen, Shiwei Tao, Shung C. Wu, Lidet A Negash
  • Patent number: 8951831
    Abstract: The present invention relates to a new binaphthalene derivative, a preparation method thereof, and an organic electronic device using the same. The binaphthalene derivative according to the present invention can perform functions of hole injection and transportation, electron injection and transportation, or light emission in an organic electronic device including an organic light-emitting device, and the device according to the present invention has excellent characteristics in terms of efficiency, drive voltage and stability, and in particular excellent effects such as a low voltage and a long life time.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: February 10, 2015
    Assignee: LG Chem, Ltd.
    Inventors: Jae Soon Bae, Dae Woong Lee, Dong Hoon Lee, Jae Chol Lee, Jun Gi Jang
  • Patent number: 8952001
    Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Simon James Anthony Grove, Angus John Morrison, Craig Jamieson, Ronald Palin, John Kinnaird Ferguson Maclean
  • Patent number: 8937055
    Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: January 20, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
  • Patent number: 8927534
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Publication number: 20140378428
    Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.
    Type: Application
    Filed: November 9, 2012
    Publication date: December 25, 2014
    Applicants: Georgetown University, Duke University
    Inventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu, Edward D. Levin, Amir H. Rezvani
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • Patent number: 8901111
    Abstract: Certain aryl-substituted heterocyclic urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: December 2, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: J. Guy Breitenbucher, Mark S. Tichenor, Jeffrey E. Merit, Natalie A. Hawryluk, Alison L. Chambers, John M. Keith
  • Patent number: 8901121
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: December 2, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
  • Patent number: 8901124
    Abstract: The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: December 2, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Cornelius Hermann, Joshua Kennedy-Smith, Matthew C. Lucas, Fernando Padilla, Michael Soth
  • Patent number: 8895559
    Abstract: A variety of specific compounds within the scope of formula I which are useful as PI3K inhibitors and can be employed for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours, and pharmaceutical compositions and kits containing said specific compounds.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Markus Klein, Ulrich Emde, Hans-Peter Buchstaller, Christina Esdar, Oliver Poeschke
  • Patent number: 8895585
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: November 25, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
  • Patent number: 8895747
    Abstract: Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: November 25, 2014
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Dieter Heindl, Heribert Maerz, Axel Schmidt
  • Patent number: 8889683
    Abstract: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Clifford Cheng, Gerald W. Shipps, Jr., Xiaohua Huang, Ying Huang, Ning Shao, Ashwin Rao, Anandan Palani, Peter Orth, Johannes H. Voigt, Robert J. Herr, Lana Michele Rossiter, Qi Zeng, Xianfeng Sun
  • Patent number: 8889872
    Abstract: A bisazole-based compound is represented by formula (I): wherein X represents C—R3 or nitrogen, R1 and R2 independently represent a haloalkyl group, R3 represents H or F. A transition metal complex is represented by formula (II): ML1L2L3??(II) wherein M is a transition metal, L1 represents in which X represents C—R31 or nitrogen, R11 and R21 independently represent a haloalkyl group, and R31 represents H or F; and L2 and L3 independently represent a dipyridine-based ligand.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: November 18, 2014
    Assignee: National Tsing Hua University
    Inventors: Yun Chi, Hsiu-Hsuan Yeh, Shu-Te Ho, Shih-Han Chang
  • Patent number: 8889720
    Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: November 18, 2014
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai
  • Publication number: 20140336168
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 13, 2014
    Inventor: AbbVie Inc.
  • Patent number: 8877782
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: November 4, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas