Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,3- And 1,4- Benzothiazines, Etc.) Patents (Class 514/224.2)
  • Patent number: 10689401
    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker, including compounds Formula (I) or a tautomer thereof and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, R3, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: June 23, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Jared N. Cumming, Brandon M. Taoka, Xing Dai
  • Patent number: 10675245
    Abstract: Disclosed are formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs which minimize the side effects of unencapsulated non-steroidal anti-inflammatory drugs while maintaining or improving efficacy. Methods of making and administering the formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs and their use as medicaments are also provided.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: June 9, 2020
    Assignee: Pacira Pharmaceuticals, Inc.
    Inventors: Louie Daniel Garcia, Liangjin Zhu, William Joseph Lambert, Gary Patou
  • Patent number: 10519232
    Abstract: The present invention relates to preventive and/or therapeutic agents for use in the treatment of retinal inflammation, and more specifically of Age-related macular degeneration and Retinitis pigmentosa, wherein said agents are selected from an IL-6 inhibitor, an APOE inhibitor and/or a Fas activator as an active ingredient.
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: December 31, 2019
    Assignees: SORBONNE UNIVERSITE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Florian Sennlaub, Xavier Guillonneau, Olivier Levy, José-Alain Sahel
  • Patent number: 10478422
    Abstract: An aspect of the present disclosure is directed to an oral liquid composition comprising valsartan with enhanced solubility and stability. Other aspects are directed to methods of using the oral liquid compositions for the treatment of hypertension, treatment of heart failure and reduction of cardiovascular mortality in clinically stable patients with left ventricular failure or left ventricular dysfunction following myocardial infarction.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: November 19, 2019
    Assignee: ECI PHARMACEUTICALS, LLC
    Inventor: Greg Thomas
  • Patent number: 10428030
    Abstract: The present application relates to novel heterocycle derivatives of Formula (I), to processes for preparing them, pharmaceutical compositions containing them, and their use thereof in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and/or memory deficits, as well as chronic and acute pain and other related CNS disorders.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: October 1, 2019
    Assignee: Trillium Therapeutics
    Inventor: Abdelmalik Slassi
  • Patent number: 10364254
    Abstract: The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods or uses as antibacterials for bacterial infections.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: July 30, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Haifeng Cui, Alan Hennessy, Qi Jin, Timothy James Miles, Stephen Frederick Moss, Neil David Pearson
  • Patent number: 10188659
    Abstract: The present invention provides compounds acting as Insulin/IGF signaling modulators useful in the treatment of neurodegenerative diseases and disorders. The invention provides pharmaceutical compositions including such compounds, and methods of using these compounds and compositions for the treatment of neurodegenerative diseases, in particular neurodegenerative diseases caused by proteotoxicity such as Alzheimer's disease.
    Type: Grant
    Filed: August 24, 2017
    Date of Patent: January 29, 2019
    Assignee: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM, LTD.
    Inventors: Hadas Reuveni, Ehud Cohen, Alexander Levitzki, Shmuel Ben-Sasson
  • Patent number: 10117876
    Abstract: The present invention provides a pharmaceutical composition comprising a compound represented by formula (1): or N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d] [1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt of the foregoing, and a salt of a compound having a C12-22 saturated aliphatic hydrocarbon group.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: November 6, 2018
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yasuhiro Zaima, Kazuo Kazama, Shuntaro Arase, Kentaro Nagane, Kanta Horie, Yosuke Ueki
  • Patent number: 10080758
    Abstract: The present invention provides a tosylate salt of N-[3-[(4aR,7aS)-2-amino-6-(5-fluoropyrimidin-2-yl)-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-7a-yl]-4-fluoro-phenyl]-5-methoxy-pyrazine-2-carboxamide.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: September 25, 2018
    Assignee: Eli Lilly and Company
    Inventors: David Andrew Coates, Craig Daniel Wolfangel
  • Patent number: 10076524
    Abstract: The present invention provides a pharmaceutical composition comprising a compound represented by formula (1): or N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d] [1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt of the foregoing, and a salt of a compound having a C12-22 saturated aliphatic hydrocarbon group.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: September 18, 2018
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yasuhiro Zaima, Kazuo Kazama, Shuntaro Arase, Kentaro Nagane, Kanta Horie, Yosuke Ueki
  • Patent number: 10034891
    Abstract: The invention pertains to the use of compounds represented by the formula, Q-G1-G2-G3-G4-Z, where Q is The compounds can be used as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
    Type: Grant
    Filed: May 11, 2016
    Date of Patent: July 31, 2018
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: K. Raja Reddy, Jeff Stebbins, Serge H. Boyer, Mark D. Erion, Scott J. Hecker, Nicholas Brian Raffaele, Brett C. Bookser, Venkat Reddy Mali
  • Patent number: 9938266
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: April 10, 2018
    Assignee: Eli Lilly and Company
    Inventor: Adam Jan Sanderson
  • Patent number: 9828390
    Abstract: The present invention provides a compound of Formula I: which is crystalline. The compound of Formula (I) is useful in the treatment of Alzheimer's disease (BACE inhibitor).
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: November 28, 2017
    Assignee: Eli Lilly and Company
    Inventors: David Andrew Coates, Pablo Garcia Losada
  • Patent number: 9822114
    Abstract: The invention relates to compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts there
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: November 21, 2017
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Christian Hubschwerlen, Daniel Ritz, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Patent number: 9815833
    Abstract: The present invention relates to the field of pharmaceutical chemistry, specifically to a class of compounds containing lactam and derivative thereof, and especially to a pyridine derivative as shown in general formula (I), preparation method and the use thereof as a Factor Xa inhibitor. The present invention further relates to the medical use of the compound and derivative thereof in preparation of anticoagulant drugs, particularly to the use in preparation of drugs for preventing or treating thrombosis or embolism.
    Type: Grant
    Filed: November 17, 2014
    Date of Patent: November 14, 2017
    Assignee: Chengdu Easton Biopharmaceuticals Co., Ltd.
    Inventors: Ying Wang, Yongzhe Xiang, Guodong Cen, Jibing Zhang, Long Huang, Ning Zhou, Jian Liu, Hui Qiao
  • Patent number: 9708345
    Abstract: The present invention provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 5, 2015
    Date of Patent: July 18, 2017
    Assignee: Eli Lilly and Company
    Inventor: Fionna Mitchell Martin
  • Patent number: 9695195
    Abstract: The present invention provides compounds of the formula: that are 5HT3 receptor antagonists and are therefore useful for the treatment of diseases treatable by inhibition of 5HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: March 8, 2016
    Date of Patent: July 4, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
  • Patent number: 9663502
    Abstract: The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, Ra, Rb, Rc, Rd, Rg, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: May 30, 2017
    Assignees: Lycera Corporation, Merck Sharp & Dohme Corp.
    Inventors: Thomas D. Aicher, Chad A. VanHuis, John MacLean, Brian M. Andresen, Kenneth J. Barr, Corey Bienstock, Neville J. Anthony, Matthew Daniels, Yuan Liu, Catherine White, Blair T. Lapointe, Nunzio Sciammetta, Vladimir Simov, Wesley B. Trotter, Kun Liu
  • Patent number: 9643979
    Abstract: The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: May 9, 2017
    Assignee: Vitas Pharma Research Private Limited
    Inventors: Chandrasekhar Alapati, Ankita Banerjee, Radha Rangarajan, Rajinder Kumar
  • Patent number: 9642843
    Abstract: Disclosed are compounds of formula (1)-(V): where the substituents are as provided herein. Further disclosed are methods of inhibiting tau aggregation, treating or ameliorating a tauopathy or cancer by administration of such a compound. Tau is a microtubule-binding protein that accumulates in a number of neurodegenerative disorders, including frontotemporal dementia and Alzheimer's disease (AD). The presence of abnormal tau correlates with neuron loss and memory deficits in patients with AD and other neurodegenerative disorders that involve tau accumulation.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: May 9, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventor: Jason E. Gestwicki
  • Patent number: 9623121
    Abstract: The present invention relates to an optical imaging probe for detecting a sentinel lymph node, which contains a complex of poly-gamma-glutamic acid and an optical imaging dye, and more particularly to an optical imaging probe for detecting a sentinel lymph node, which contains a poly-gamma-glutamic acid/optical imaging dye complex that, when injected subcutaneously in vivo, remains in the sentinel lymph node for a relatively long period of time and has a low tendency to migrate to other lymph nodes. The present invention provides a poly-gamma-glutamic acid/fluorescent dye complex, which contains no radiopharmaceutical and is harmless to the human body. The use of the poly-gamma-glutamic acid/fluorescent dye complex makes it possible to accurately detect the position of a sentinel lymph node in real time without concerns about radioactive contamination.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: April 18, 2017
    Assignees: BIOLEADERS CORPORATION, THE INDUSTRY AND ACADEMIC COOPERATION IN CHUNGNAM NATIONAL UNIVERSITY, KOOKMIN UNIVERSITY INDUSTRY - ACADEMIC COOPERATION FOUNDATION
    Inventors: Moon-Hee Sung, Yong Taik Lim, Young-Woock Noh, Il Han Lee
  • Patent number: 9556158
    Abstract: The present invention relates to 3-[(pyridin-2-ylmethoxyimino)(phenyl)methyl]-2-substituted-1,2,4-oxadiazol-5(2H)-one derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: January 31, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Christoph Braun, Pierre-Yves Coqueron, Christophe Dubost, Helene Lachaise, Simon Maechling, Anne-Sophie Rebstock, Philippe Rinolfi, Haruko Sawada, Ulrike Wachendorff-Neumann
  • Patent number: 9540352
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: January 10, 2017
    Assignee: Pfizer Inc.
    Inventors: David Lawrence Firman Gray, Lei Zhang, Michael Aaron Brodney, Michael Eric Green, Chakrapani Subramanyam
  • Patent number: 9540399
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1, U, V and A are as defined in the description, to pharmaceutical compositions containing them and uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: January 10, 2017
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Stephanie Enderlin-Paput, Christian Hubschwerlen, Georg Rueedi, Cornelia Zumbrunn
  • Patent number: 9533999
    Abstract: The present invention encompasses compounds of the formulas (I) & (II), wherein the groups A, L and Ar are defined as in claim 1, which are suitable for the treatment of diseases related to KCa3.1, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: January 3, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Michael J. Burke, Bryan McKibben, Matt Aaron Tschantz
  • Patent number: 9486463
    Abstract: Provided herein are methods of modulating hormone concentrations in a subject comprising the administration of a composition comprising a chemosensory receptor ligand, wherein the composition is adapted to deliver the ligand to one or more regions of the intestine of said subject. Also provided are methods directed to the modulation of circulating concentrations of one or more of GLP-1 (total), GLP-1 (active), GLP-2, oxyntomodulin, PYY (total), PYY 3-36, CCK, GIP, insulin, C-peptide, glycentin, uroguanylin amylin, and ghrelin (total), ghrelin (active) and glucagon.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: November 8, 2016
    Assignee: AMBRA BIOSCIENCE LLC
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R. G. Jones, Mark S. Fineman
  • Patent number: 9481683
    Abstract: A compound, having the following formula: or resonance form thereof, or salt thereof, or salt of resonance form thereof is provided, wherein R1-R4 and n are defined herein. Compositions and methods including the compound are also provided.
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: November 1, 2016
    Assignee: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Marvin J. Miller, Rohit Tiwari
  • Patent number: 9453028
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: June 29, 2015
    Date of Patent: September 27, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Haoran Zhao, Rao Kolluri, Carlos Valdez, Kin Tso, Rajinder Singh, John Ramphal
  • Patent number: 9427431
    Abstract: The present invention makes availables assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: August 30, 2016
    Assignee: Johns Hopkins University School of Medicine
    Inventors: Philip A. Beachy, Michael K. Cooper, Jefferey A. Porter
  • Patent number: 9370535
    Abstract: The present invention relates to the use of Volasertib or a salt thereof or a hydrate thereof in combination with Cisplatin or Carboplatin or a salt thereof or a hydrate thereof for treating patients suffering from advanced and/or metastatic solid tumors.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: June 21, 2016
    Assignee: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Tillmann Taube, Gerd Michael Munzert, Dorothea Rudolph
  • Patent number: 9340566
    Abstract: The invention pertains to the use of fused bicyclo heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
    Type: Grant
    Filed: February 23, 2015
    Date of Patent: May 17, 2016
    Assignee: METABASIS THERAPEUTICS, INC.
    Inventors: K. Raja Reddy, Jeff Stebbins, Serge H. Boyer, Mark D. Erion, Scott J. Hecker, Nicholas Brian Raffaele, Brett C. Bookser, Venkat Reddy Mali
  • Patent number: 9326515
    Abstract: The present invention relates to 3-[(1,3-thiazol-4-ylmethoxyimino)(phenyl)methyl]-2-substituted-1,2,4-oxadiazol-5(2H)-one derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: May 3, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Christoph Braun, Pierre-Yves Coqueron, Christophe Dubost, Helene Lachaise, Simon Maechling, Anne-Sophie Rebstock, Philippe Rinolfi, Ulrike Wachendorff-Neumann
  • Patent number: 9238640
    Abstract: Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: January 19, 2016
    Assignee: Resverlogix Corp.
    Inventor: Henrik C. Hansen
  • Patent number: 9198917
    Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: April 24, 2015
    Date of Patent: December 1, 2015
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
  • Patent number: 9192612
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: November 24, 2015
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Erik Alphie LaChapelle, Brian Thomas O'Neill
  • Patent number: 9149475
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: December 18, 2012
    Date of Patent: October 6, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Hui Li, Haoran Zhao, Rao Kolluri, Kin Tso, John Ramphal, Shihai Gu, Carlos Valdez, Jing Zhang, Emily Stauffer, Matthew Duncton, Salvador Alvarez
  • Patent number: 9045499
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: June 2, 2015
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Erik Alphie LaChapelle, Brian Thomas O'Neill
  • Patent number: 9040508
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20150133438
    Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: January 9, 2015
    Publication date: May 14, 2015
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150099719
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
  • Patent number: 8999976
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.
    Type: Grant
    Filed: December 9, 2013
    Date of Patent: April 7, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Dennis Hurley, Lev T. D. Fanning, Peter D. J. Grootenhuis, Martyn Botfield, Fredrick Van Goor
  • Publication number: 20150087637
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: December 4, 2014
    Publication date: March 26, 2015
    Applicant: PFIZER INC.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Christopher John Helal, Brian Thomas O'Neill
  • Patent number: 8987254
    Abstract: The present invention provides a compound of Formula I: wherein R is H or F; and A is: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: March 24, 2015
    Assignee: Eli Lilly and Company
    Inventors: Steven James Green, Dustin James Mergott, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
  • Publication number: 20150080373
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Patent number: 8980883
    Abstract: The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: March 17, 2015
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Publication number: 20150072972
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, L1, L2, X, Y, Q and Z have defined meanings.
    Type: Application
    Filed: November 13, 2014
    Publication date: March 12, 2015
    Inventors: Laurence Anne Mevellec, Edmond J.K. Ludo, Josephus Carolus Mertens, Jacobus A.J. Van Dun, Maria V.F. Somers, Walter B.L. Wouters
  • Publication number: 20150072975
    Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Berangere Gaucher, JR., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin XU
  • Publication number: 20150065487
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Patent number: 8962616
    Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: February 24, 2015
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Brian Thomas O'Neill