Ring Oxygen In The Bicyclo Ring System Patents (Class 514/302)
  • Patent number: 10806724
    Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 23, 2019
    Date of Patent: October 20, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Iyassu K. Sebhat, Ashok Arasappan, Scott B. Hoyt, Robert R. Wilkening, Duane DeMong
  • Patent number: 10335399
    Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 25, 2017
    Date of Patent: July 2, 2019
    Inventors: Iyassu K. Sebhat, Ashok Arasappan, Scott B. Hoyt, Robert R. Wilkening, Duane DeMong
  • Patent number: 10301320
    Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: May 28, 2019
    Assignees: University of Kentucky Research Foundation, Case Western Reserve University, Board of Regents of the University of Texas System
    Inventors: Sanford Markowitz, James K. V. Willson, Bruce Posner, Joseph Ready, Youngyou Zhang, Hsin-Hsiung Tai, Monika Antczak, Stanton Gerson, KiBeom Bae, Sung Yeun Yang, Amar Desai
  • Patent number: 10214535
    Abstract: The present invention is directed to hydroxymethyl piperidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: February 26, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Nigel Liverton, Yunfu Luo
  • Patent number: 10111865
    Abstract: Methods of sedating a patient undergoing critical care treatment using intravenous gaboxadol are provided.
    Type: Grant
    Filed: June 27, 2017
    Date of Patent: October 30, 2018
    Assignee: OVID THERAPEUTICS INC.
    Inventors: Matthew During, Anna Kazanchyan
  • Patent number: 9890171
    Abstract: The present invention relates to compounds of the formulas (IA) and (IB) and pharmaceutically acceptable salts thereof, wherein A and R1-R6, are as defined herein. The invention 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 1, 2015
    Date of Patent: February 13, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Zhidong Chen, Derek Cogan, Xin Guo, Daniel Richard Marshall, Kenneth Michael Meyers, Yunlong Zhang
  • Patent number: 9801864
    Abstract: Methods of increasing tonic inhibition in a subject in need thereof, for example a subject with Fragile X syndrome or Angelman syndrome are disclosed. Methods of treating secondary insomnia in a subject with a neurodegenerative disease or disorder are also disclosed.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: October 31, 2017
    Assignee: OVID THERAPEUTICS INC
    Inventor: Matthew During
  • Patent number: 9790233
    Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
    Type: Grant
    Filed: April 16, 2013
    Date of Patent: October 17, 2017
    Assignees: Case Western Reserve University, Board of Regents of the University of Texas System, University of Kentucky Research Foundation
    Inventors: Sanford Markowitz, James K. V. Willson, Bruce A. Posner, Joseph Ready, Yongyou Zhang, Hsin-Hsiung Tai, Monika Antczak, Stanton Gerson, KiBeom Bae, Sung Yeun Yang, Amar Desai
  • Patent number: 9764015
    Abstract: The present invention in general relates Hemoglobin receptor or its part as a novel vaccine candidate against Leishmaniasis. Specifically, the present invention envisages HbR DNA for eliciting immune response in a mammal against Leishmaniasis. Additional aspect of the present invention is related to a vaccine composition for inducing immune response against Leishmaniasis in mammals. In a preferred aspect, the present invention relates to use of HbR-polypeptide as marker for diagnosis of Leishmania in kala-azar patients.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: September 19, 2017
    Assignees: National Institute of Immunology, Indian Institute of Chemical Biology
    Inventors: Amitabha Mukhopadhyay, Syamal Roy, Deepika Gupta, Rajan Guha, Ruchir Rastogi
  • Patent number: 9744159
    Abstract: Methods of increasing tonic inhibition in a subject in need thereof, for example a subject with Fragile X syndrome or Angelman syndrome are disclosed. Methods of treating secondary insomnia in a subject with a neurodegenerative disease or disorder are also disclosed.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: August 29, 2017
    Assignee: OVID THERAPEUTICS INC
    Inventor: Matthew During
  • Patent number: 9717716
    Abstract: Methods of sedating a patient undergoing critical care treatment using intravenous gaboxadol are provided.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: August 1, 2017
    Assignee: OVID THERAPEUTICS INC
    Inventors: Matthew During, Anna Kazanchyan
  • Patent number: 9603831
    Abstract: The present invention relates compounds according to Formula (I) wherein R1 and R2 are independently H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl, and R3 and R4 taken together form a carbonyl (?O); or wherein R1 and R2 are independently H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl, R3 is H and R4 is H or —OR5, wherein R5 is H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl; or pharmaceutically acceptable salts or esters thereof, for use in the treatment of kidney disease, in particular in the treatment of acute kidney injury. The present invention also relates to methods of treatment of the same and methods of kidney transplant surgery and coronary artery bypass graft surgery using the compounds of Formula (I).
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: March 28, 2017
    Assignee: Queen Mary & Westfield College, University of London
    Inventor: Christoph Thiemermann
  • Patent number: 9522913
    Abstract: Compounds of the formula (I), and the agrochemically acceptable salts and N-oxides of those compounds, including all stereoisomers and tautomeric forms, and wherein the substituents are as defined in claim 1, are useful for controlling animal pests and can be prepared in a manner known per se.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: December 20, 2016
    Assignee: Syngenta Participations AG
    Inventors: Michel Muehlebach, Andrew Edmunds, Andre Stoller
  • Patent number: 9522138
    Abstract: Methods and compounds for research and treatment of portal hypertension. The use of racemic or non-racemic mixtures of furopyridine isomers to stimulate eNOS function in sinusoidal endothelial cells and to increase NO production in both normal sinusoidal endothelial cells and injured endothelial cells.
    Type: Grant
    Filed: December 31, 2014
    Date of Patent: December 20, 2016
    Inventors: Don C. Rockey, Songling Liu, Glenn Cornett
  • Patent number: 9505772
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: November 29, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
  • Patent number: 9399034
    Abstract: Methods of sedating a patient undergoing critical care treatment using intravenous gaboxadol are provided.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: July 26, 2016
    Assignee: OVID THERAPEUTICS INC
    Inventors: Matthew During, Anna Kazanchyan
  • Patent number: 9382234
    Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: July 5, 2016
    Assignee: GlaxoSmithKline LLC
    Inventors: Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Carla A. Donatelli
  • Publication number: 20150148308
    Abstract: A harmful arthropod control composition comprising a compound represented by the following Formula (1) wherein each symbol represents definitions described in the specification, and one or more fungicidal compounds, which are selected from among azoles, strobilurins, phenylamides, rice blast controlling compounds, rice sheath blight disease controlling compounds, and other fungicidal compounds. The composition has an excellent controlling effect against harmful arthropods.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Applicant: Sumitomo Chemical Company, Limited
    Inventors: Tatsuya Suzuki, Atsushi Iwata, Yoshihiko Nokura
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Patent number: 9034896
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene) Heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 21, 2014
    Date of Patent: May 19, 2015
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
  • Publication number: 20150133527
    Abstract: Methods are provided herein for treating cardiac arrhythmias, such as for treating an arrhythmia syndrome, for example Brugada syndrome, in a subject. In some embodiments, the methods include selecting a subject with Brugada syndrome and administering to the subject an effective amount of an agent that increases the expression or activity of SIRT1 in the subject. In some embodiments, the agent increases Nav1.5 activation. In some embodiments, the agent increases the expression or activity of SRIT1 and increases Nav1.5 activation.
    Type: Application
    Filed: May 6, 2013
    Publication date: May 14, 2015
    Inventors: Barry London, Kaikobad J. Irani
  • Publication number: 20150133446
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, Rx, R1, R2, R3, X1, X2 and s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 14, 2015
    Inventors: R. Michael Lawrence, Michael M. Miller, Dietmar Alfred Seiffert, Shoshana L. Posy, Pancras C. Wong, Jacques Banville, Edward H. Ruediger, Daniel H. Deon, Alain Martel, François Tremblay, Julia Guy, Jean-François Lavallée, Marc Gagnon
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Patent number: 9023839
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
    Type: Grant
    Filed: April 22, 2014
    Date of Patent: May 5, 2015
    Assignee: IRM LLC
    Inventors: Valentina Molteni, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
  • Patent number: 9018209
    Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: April 28, 2015
    Assignee: Yale University
    Inventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
  • Publication number: 20150111894
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
  • Patent number: 9012456
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: April 21, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Bernd Nosse
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Patent number: 9006440
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and/or systemic lupus.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Patent GmbH
    Inventors: Lars Burgdorf, Melanie Schultz, Tatjana Ross, Brian Hodous, Justin Potnick, Amanda E. Sutton, Bayard R. Huck
  • Publication number: 20150087672
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 26, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
  • Publication number: 20150080377
    Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a
    Type: Application
    Filed: August 31, 2013
    Publication date: March 19, 2015
    Inventor: Daljit Singh Dhanoa
  • Patent number: 8975235
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 10, 2015
    Assignee: InterMune, Inc.
    Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 8975277
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LQ and Ar are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: March 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf
  • Publication number: 20150065497
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: March 5, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Publication number: 20150065501
    Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Publication number: 20150057268
    Abstract: Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor.
    Type: Application
    Filed: December 6, 2012
    Publication date: February 26, 2015
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Scott Runyon, Yanan Zhang, Carla Hassler, Brian Gilmour
  • Publication number: 20150057265
    Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Yun-Long Li, David M. Burns, Hao Feng, Taisheng Huang, Song Mei, Jun Pan, Oleg Vechorkin, Hai-Fen Ye, Wenyu Zhu, Maria Rafalski, Anlai Wang, Chu-Biao Xue
  • Patent number: 8962651
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: February 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kyle J. Eastman, Kyle E. Parcella, John F. Kadow
  • Patent number: 8957062
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: February 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
  • Publication number: 20150038527
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: February 5, 2015
    Applicant: Merck Patent GmbH
    Inventors: Lars Burgdorf, Tatjana Ross, Carl Deutsch
  • Publication number: 20150038509
    Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
    Type: Application
    Filed: June 12, 2014
    Publication date: February 5, 2015
    Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
  • Publication number: 20150038438
    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: February 5, 2015
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20150038502
    Abstract: The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: October 19, 2012
    Publication date: February 5, 2015
    Inventors: Dansu Li, Anthony J. Roecker
  • Publication number: 20150031668
    Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 29, 2015
    Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, James Brown, Wenge Zhong, Thomas T. Nguyen
  • Patent number: 8940758
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: January 27, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Ando
  • Publication number: 20150025106
    Abstract: The invention provides a drug delivery system for a combination of therapeutic agents. The system includes a water soluble biodegradable ABA-type triblock copolymer that possesses thermosensitive gelation properties. The system can form a stable thermogel that includes a combination of therapeutic agents including, for example, rapamycin, paclitaxel, and 17-AAG. After administration to a subject, the drugs are released at a controlled rate from the thermogel, which biodegrades into non-toxic components. The polymer system can also function to increase the solubility and stability of drugs in the composition.
    Type: Application
    Filed: July 22, 2014
    Publication date: January 22, 2015
    Inventors: Glen S. Kwon, Hyunah Cho
  • Publication number: 20150025070
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 22, 2015
    Applicant: Novartis AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser