Spiro Ring System Patents (Class 514/278)
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Publication number: 20140228333Abstract: In one aspect, the invention relates to methods for treating muscle atrophy by providing to an animal in need thereof an effective amount of a compound. The compound can modulate the expression levels of multiple mRNA of a muscle atrophy signature. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 6, 2012Publication date: August 14, 2014Applicants: UNIVERSITY OF IOWA RESEARCH FOUNDATION, The United States of America as Represented by the Department of Veterans AffairsInventors: Christopher M. Adams, Steven D. Kunkel, Michael Welsh
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Patent number: 8802690Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: July 11, 2013Date of Patent: August 12, 2014Assignee: Pfizer Inc.Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Patent number: 8802689Abstract: Described herein, inter alia, are compounds useful for the prevention or treatment of hyperproliferative diseases or disorders.Type: GrantFiled: September 13, 2012Date of Patent: August 12, 2014Assignee: The Regents of the University of CaliforniaInventors: Michael E. Jung, Charles L. Sawyers, Samedy Ouk, Chris Tran, John Wongvipat
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Patent number: 8802688Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: April 21, 2012Date of Patent: August 12, 2014Assignee: Pfizer Inc.Inventors: Robert Lee Dow, David James Edmonds, David Andrew Griffith, James Alfred Southers, Jr.
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Publication number: 20140221412Abstract: The invention provides compounds of formula I: and salts thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer using compounds of formula I.Type: ApplicationFiled: August 30, 2012Publication date: August 7, 2014Applicants: WAYNE STATE UNIVERSITY, REGENTS OF THE UNIVERSITY OF MICHIGAN, DEPARTMENT OF VETERANS AFFAIRSInventors: Arun K. Rishi, Scott D. Larsen
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Publication number: 20140221362Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
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Publication number: 20140221349Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Matthias ECKHARDT
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Patent number: 8796299Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: GrantFiled: September 24, 2012Date of Patent: August 5, 2014Assignee: OPKO Health, Inc.Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
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Patent number: 8796257Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: November 30, 2012Date of Patent: August 5, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 8796278Abstract: The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I). Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: August 5, 2014Assignee: SanofiInventors: Zhongli Gao, Daniel Hall, David Stefany
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Publication number: 20140213568Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 22, 2014Publication date: July 31, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Patent number: 8791091Abstract: 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 monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.Type: GrantFiled: November 29, 2012Date of Patent: July 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
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Patent number: 8791133Abstract: The disclosure relates to compounds of formula I: wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.Type: GrantFiled: October 16, 2012Date of Patent: July 29, 2014Assignee: SanofiInventors: Karl Schoenafinager, Henning Steinhagen, Bodo Scheiper, Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Jacques Mauger, Pavel Safar
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Publication number: 20140206693Abstract: Certain embodiments are directed to methods of treating a pathophysiological state or symptoms thereof resulting from aldose reductase-mediated signaling in a cytotoxic pathway using an aldose reductase specific inhibitor.Type: ApplicationFiled: January 27, 2014Publication date: July 24, 2014Applicant: The Board of Regents of the University of Texas SystemInventors: Satish K Srivastava, Kota V Ramana
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Publication number: 20140206691Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: ApplicationFiled: March 27, 2014Publication date: July 24, 2014Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
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Publication number: 20140200223Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.Type: ApplicationFiled: December 18, 2013Publication date: July 17, 2014Inventors: Salvacion Cacatian, David A. Claremon, Lawrence Wayne Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian Mckeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
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Patent number: 8778925Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.Type: GrantFiled: October 6, 2009Date of Patent: July 15, 2014Assignee: Cancer Research Technology Ltd.Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
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Patent number: 8778956Abstract: The present invention is directed to novel hydroxy alkyl substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives of the general formula wherein all variables are as defined herein, useful in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor. More particularly, the compounds of the present invention are useful in the treatment of disorders and conditions such as anxiety, depression, panic, dementia, mania, bipolar disorder, substance abuse, neuropathic pain, acute pain, chronic pain, migraine, asthma, cough, psychosis, schizophrenia, epilepsy, hypertension, obesity, eating disorders, cravings, diabetes, cardiac arrhythmia, irritable bowel syndrome, Crohn's disease, urinary incontinence, adrenal disorders, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), Alzheimer's disease, for improved cognition or memory and for mood stabilization.Type: GrantFiled: December 3, 2008Date of Patent: July 15, 2014Assignee: Janssen Pharmaceutica NVInventors: Kathleen Battista, Gilles Bignan, Peter J. Connolly, Allen B. Reitz, Tina Morgan Ross, Malcolm Scott, Steven A. Middleton, Michael Orsini
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Patent number: 8778957Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: GrantFiled: March 8, 2010Date of Patent: July 15, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley
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Patent number: 8778938Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 3, 2011Date of Patent: July 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Publication number: 20140193529Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of inflammation are provided which employ active agents, other than a retinoid, that stimulate thymosin beta-4 expression in the skin and inhibit production of pro-inflammatory chemokines and/or cytokines. Also provided are methods for screening for substances which stimulate thymosin beta-4 expression levels and the methods of using active agents identified by the screening protocol in the treatment of skin.Type: ApplicationFiled: January 7, 2013Publication date: July 10, 2014Applicant: AVON PRODUCTS, INC.Inventors: Ying Cheng, Qian Zheng, Russell J. Wyborski
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Publication number: 20140194424Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.Type: ApplicationFiled: December 12, 2013Publication date: July 10, 2014Inventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma
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Publication number: 20140194454Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: TheraVida, Inc.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Publication number: 20140194433Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.Type: ApplicationFiled: March 12, 2014Publication date: July 10, 2014Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Patent number: 8772286Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.Type: GrantFiled: December 13, 2010Date of Patent: July 8, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Tjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fademrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
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Patent number: 8772288Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: April 3, 2009Date of Patent: July 8, 2014Assignee: Almirall, S.A.Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
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Patent number: 8772307Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.Type: GrantFiled: May 17, 2006Date of Patent: July 8, 2014Assignee: Gruenenthal GmbHInventors: Robert Frank, Melanie Reich, Ruth Jostock, Gregor Bahrenberg, Hans Schick, Birgitta Henkel, Helmut Sonnenschein
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Publication number: 20140187530Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: ApplicationFiled: November 27, 2013Publication date: July 3, 2014Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
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Patent number: 8765735Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: GrantFiled: May 18, 2010Date of Patent: July 1, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 8765791Abstract: The present invention relates to methods for treating cancer by administering a therapeutically effective amount of compound of formula (I), such as selective NPY5R antagonist MK-0557 (trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1?-cyclohexane]-4?-carboxamide), or a pharmaceutically acceptable salt thereof, to a subject in need thereof The methods can further comprise administering a chemotherapeutic agent to the subject in need thereof.Type: GrantFiled: March 10, 2009Date of Patent: July 1, 2014Assignee: University Health NetworkInventor: Guohua Pan
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Patent number: 8765752Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: GrantFiled: March 15, 2013Date of Patent: July 1, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
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Publication number: 20140179695Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.Type: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
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Publication number: 20140179724Abstract: The application is directed to compounds of Formula I?-A especially to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein R1a-R5a, Y, Z are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I?-A, and especially compounds of Formula I-A, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: December 13, 2013Publication date: June 26, 2014Applicant: Purdue Pharma L.P.Inventors: R. Richard GOEHRING, Laykea TAFESSE, Mark A. YOUNGMAN
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Publication number: 20140179725Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.Type: ApplicationFiled: February 24, 2014Publication date: June 26, 2014Inventors: Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, John E. Macor, Joanne J. Bronson, Carolyn Diane Dzierba, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu
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Patent number: 8758830Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: August 23, 2013Date of Patent: June 24, 2014Assignee: Array BioPharma, Inc.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
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Patent number: 8759367Abstract: The present invention relates to compounds for modulating sonic hedgehog signaling and preventing or treating cancer.Type: GrantFiled: October 4, 2011Date of Patent: June 24, 2014Assignees: The Wistar Institute, The Trustees of the University of PennsylvaniaInventors: Nadia Dahmane, Jeffrey D. Winkler, Andre Isaacs
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Patent number: 8759377Abstract: In one aspect, the invention relates to compounds having a general structure: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: November 23, 2010Date of Patent: June 24, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers
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Publication number: 20140171452Abstract: Disclosed is an antidepressant, neuroprotectant, amyloid ? deposition inhibitor, or age retardant composition containing a heterocyclic compound having the general formula (I):Type: ApplicationFiled: February 12, 2014Publication date: June 19, 2014Applicant: ZENYAKU KOGYO KABUSHIKI KAISHAInventors: Yoshimasa YAMAGUCHI, Ryogo YUI, Toshiyuki MATSUNO, Kenichi SAITOH, Hitoshi MIYASHITA, Takeshi NAGATA
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Publication number: 20140171427Abstract: The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: November 25, 2013Publication date: June 19, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina HADIDA-RUAH, Edward Adam KALLEL, Mark Thomas MILLER, Joseph PONTILLO, Vijayalaksmi ARUMUGAM, Nicole HILGRAF, Jason McCARTNEY, Peter Diederik Jan GROOTENHUIS, Corey ANDERSON, Mehdi NUMA, Bryan A. Frieman, Brian Richard BEAR, Jason Philip JOHNSON, JR.
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Publication number: 20140171439Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, 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: ApplicationFiled: February 21, 2014Publication date: June 19, 2014Applicant: Janssen Pharmaceutica, N.V.Inventors: Kristof VAN EMELEN, Marc Gustaaf Celine VERDONCK, Sven Franciscus Anna VAN BRANDT, Patrick Rene ANGIBAUD, Lieven MEERPOEL, Alexey Borisovich DYATKIN
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Patent number: 8754107Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: November 16, 2007Date of Patent: June 17, 2014Assignee: AbbVie Inc.Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
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Patent number: 8754097Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumors.Type: GrantFiled: August 22, 2012Date of Patent: June 17, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Patent number: 8754095Abstract: The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). wherein R, R1, R2, R3, R4, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: June 17, 2014Assignee: SanofiInventor: Zhongli Gao
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Patent number: 8754096Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: November 10, 2011Date of Patent: June 17, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Heather E. Stevenson, Cheng Wang, C. Blair Zartman
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Publication number: 20140163011Abstract: 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: ApplicationFiled: December 19, 2013Publication date: June 12, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20140163055Abstract: Disclosed are methods of treating HIV infections comprising, in one aspect, administering compounds that are phospholipase D inhibitors. 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: ApplicationFiled: December 11, 2013Publication date: June 12, 2014Inventors: H. Alex Brown, Craig W. Lindsley
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Publication number: 20140163001Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.Type: ApplicationFiled: July 27, 2012Publication date: June 12, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
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Publication number: 20140163056Abstract: This invention relates to novel spiroindoline compounds of formula (I) that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: August 3, 2012Publication date: June 12, 2014Inventors: Christophe Pierre Alain Chassaing, Sandra Koch, Jürgen LUTZ
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Patent number: 8748446Abstract: Halo-organic heterocyclic compounds are described, which have the formulas Ring A is an aromatic ring bound to at least two halogen atoms, at least one of which is iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.Type: GrantFiled: March 3, 2012Date of Patent: June 10, 2014Assignee: Nanoquantum Sciences, Inc.Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker