Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 546/113)
  • Patent number: 8921559
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: December 30, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
  • Patent number: 8921369
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: December 30, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20140378474
    Abstract: The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 25, 2014
    Applicant: NOVARTIS AG
    Inventors: Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • Patent number: 8916571
    Abstract: The invention relates to the treatment of cancer using an inhibitor of 5?-methylthioadenosine phosphorylase (MTAP). The invention particularly relates to the treatment of prostate cancer and head and neck cancer.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: December 23, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Chandan Guha
  • Publication number: 20140371261
    Abstract: Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.
    Type: Application
    Filed: October 17, 2012
    Publication date: December 18, 2014
    Applicants: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, VANDERBILT UNIVERSITY
    Inventors: Lawrence J. Marnett, Andy J. Liedtke, Trevor M. Penning, Adegoke O. Adeniji, Michael C. Byrns
  • Publication number: 20140371138
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, John A. McCauley, Steven W. Ludmerer, Kun Liu, Joseph P. Vacca, Hao Wu, Bin Hu, Richard Soll, Fei Sun, Xinghai Wang, Man Yan, Chengren Zhang, Mingwei Zheng, Bin Zhong, Jian Zhu
  • Patent number: 8912181
    Abstract: A novel bicyclic compound having an HSP90 inhibitory effect and a carcinostatic effect. A pharmaceutical agent based on the HSP90 inhibitory effect and useful in the prevention and/or treatment of a disease involving HSP90, particularly cancer. The compound has a general formula (I) or is a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are each independently C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are each independently CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: December 16, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
  • Publication number: 20140361259
    Abstract: An arylamine-based compound is represented by Formula 1 below. The arylamine-based compound is included in an organic light emitting diode.
    Type: Application
    Filed: October 23, 2013
    Publication date: December 11, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
  • Publication number: 20140364433
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
  • Patent number: 8907089
    Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
    Type: Grant
    Filed: August 25, 2010
    Date of Patent: December 9, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Sasaki, Yuta Tanaka
  • Publication number: 20140357623
    Abstract: 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carbo
    Type: Application
    Filed: September 14, 2011
    Publication date: December 4, 2014
    Applicant: PROXIMAGEN LIMITED
    Inventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
  • Publication number: 20140356322
    Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
  • Publication number: 20140357616
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: December 4, 2014
    Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Alan S. Florjancic, Yunsong Tong
  • Publication number: 20140357612
    Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: May 29, 2014
    Publication date: December 4, 2014
    Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Betsy Burton
  • Publication number: 20140357617
    Abstract: The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: August 20, 2014
    Publication date: December 4, 2014
    Applicant: FAB PHARMA S.A.S.
    Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
  • Patent number: 8901126
    Abstract: Substituted imidazo[1,5-a]quinoxalin-4-one compounds of formula (I) described herein exhibit PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: December 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Mari Sugita, Hirofumi Yamamoto, Kazunori Kamijo, Kazuyuki Tsuchiya, Ryushi Seo, Satoshi Yamamoto
  • Patent number: 8901124
    Abstract: The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: December 2, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Cornelius Hermann, Joshua Kennedy-Smith, Matthew C. Lucas, Fernando Padilla, Michael Soth
  • Patent number: 8901301
    Abstract: Propane-1-sulfonic acid {2,4-difluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phenyl]-amide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-2,5-difluoro-benzenesulfonamide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-3-fluoro-benzenesulfonamide, pyrrolidine-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, N,N-dimethylamino-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: December 2, 2014
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Hongyao Zhu
  • Patent number: 8901111
    Abstract: Certain aryl-substituted heterocyclic urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: December 2, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: J. Guy Breitenbucher, Mark S. Tichenor, Jeffrey E. Merit, Natalie A. Hawryluk, Alison L. Chambers, John M. Keith
  • Patent number: 8901118
    Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described, wherein the compounds have formula I: In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein.
    Type: Grant
    Filed: April 20, 2011
    Date of Patent: December 2, 2014
    Assignee: Plexxikon Inc.
    Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Wayne Spevak, Jianming Tsai, Todd Ewing, Ying Zhang, Chao Zhang
  • Publication number: 20140349989
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated with these diseases and disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 27, 2014
    Applicant: ALZHEIMER'S INSTITUTE OF AMERICA
    Inventors: Dange Vijay Kumar, Paul M. Slattum, Kraig M. Yager, Mark D. Shenderovich, Rajendra Tangallapally, Se-Ho Kim
  • Publication number: 20140350013
    Abstract: Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Inventors: Celine DUQUENNE, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
  • Patent number: 8895571
    Abstract: The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: November 25, 2014
    Assignee: Incyte Corporation
    Inventors: Taisheng Huang, Hao Feng, Lingquan Kong, Anlai Wang, Hai Fen Ye, Chu-Biao Xue
  • Publication number: 20140343092
    Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
    Type: Application
    Filed: September 18, 2012
    Publication date: November 20, 2014
    Inventors: Simon N. Haydar, Brian Alvin Johns, Emile Johann Velthuisen
  • Patent number: 8889869
    Abstract: A method for making the compound is set forth utilizing the starting material
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: November 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H. Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
  • Patent number: 8889870
    Abstract: The present invention relates to compounds of formulae I and II wherein the variables are as defined herein. These compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: November 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Clarence E. Hull, III, Thomas C. Malone
  • Patent number: 8889684
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Heinz Stadtmueller
  • Patent number: 8889868
    Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: November 18, 2014
    Assignee: Syntarga BV
    Inventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgersma, Wiro Michaël Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus de Groot
  • Publication number: 20140336200
    Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: ADAMED SP. Z O.O.
    Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
  • Patent number: 8884029
    Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: November 11, 2014
    Assignee: Adeka Corporation
    Inventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Mitsuhiro Okada, Toru Yano, Yohei Aoyama, Yusuke Kubota
  • Patent number: 8883807
    Abstract: The present invention is directed to piperidinone carboxamide indane 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: Grant
    Filed: November 10, 2011
    Date of Patent: November 11, 2014
    Assignee: 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, Cheng Wang, Blair C. Zartman, Heather E. Stevenson
  • Patent number: 8877772
    Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases, having a structural Formula, Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.
    Type: Grant
    Filed: November 25, 2009
    Date of Patent: November 4, 2014
    Assignee: University of Rochester
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin Loweth, Torsten Wiemann
  • Patent number: 8877742
    Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: November 4, 2014
    Assignee: GlaxoSmithKline Intellectual Property Limited
    Inventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
  • Publication number: 20140323475
    Abstract: The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 14, 2012
    Publication date: October 30, 2014
    Inventors: Antoni Torrens Jover, Ramon Mercé Vidal, Francesc Xavier Caldentey Frontera, Antonio David Rodríguez Garrido, Elena Carceller González, Jordi Salas Solana
  • Publication number: 20140323468
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n 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: Application
    Filed: April 28, 2014
    Publication date: October 30, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael BALESTRA, Jennifer BURKE, Zhidong CHEN, Derek COGAN, Lee FADER, Xin GUO, Bryan MCKIBBEN, Daniel Richard MARSHALL, Peter Allen NEMOTO, Hui YU
  • Publication number: 20140323481
    Abstract: Compounds of the formula (I) in which R1, R2, X and Y have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 30, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Guenter Hoelzemann, Hans-Michael Eggenweiler, Paul Czodrowski
  • Publication number: 20140315880
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Srinivasa V. Murthy, Jon-Paul Strachan, Yunde Xiao
  • Publication number: 20140315928
    Abstract: The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.
    Type: Application
    Filed: April 15, 2014
    Publication date: October 23, 2014
    Applicant: Pfizer Inc.
    Inventors: Etzer Darout, Robert Dullea, Julie Jia Li Hawkins, Allyn T. Londregan, Paula M. Loria, Bruce Maguire, Kim F. McClure, Donna N. Petersen, David W. Piotrowski
  • Publication number: 20140315901
    Abstract: The present invention is directed to arylpyrrolopyridine derivatives of formula (A) The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Lewy body dementia, Parkinson's disease or cancer.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Inventors: Simon Timothy Bedford, I-Jen Chen, Yikang Wang, Douglas Stewart Williamson
  • Publication number: 20140315909
    Abstract: The present invention relates to compounds described by Formula I: salts thereof, their synthesis, and their use as ITK and JAK3 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such disease associated with abnormal cell growth such as autoimmune, inflammation, rheumatoid arthritis, systemic lupus erythematosus, atherosclerosis, ulcerative colitis, psoriatic arthritis, psoriasis, Crohn's, metabolic and cancer diseases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions and processes for preparing the compounds of the invention.
    Type: Application
    Filed: April 16, 2014
    Publication date: October 23, 2014
    Applicant: ARRIEN PHARMACEUTICALS LLC
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy, Paramareddy Gangireddy, Rajendra P. Appalaneni
  • Patent number: 8865735
    Abstract: The present invention provides solid forms of the compound of formula 1 and pharmaceutical uses thereof.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: October 21, 2014
    Assignees: Hoffman-La Roche Inc., Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Gary Conard Visor, Shan-Ming Kuang, Baoshu Zhao, Ralph Diodone, Karsten Fähnrich, Urs Schwitter
  • Publication number: 20140309421
    Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Gerald J. Tanoury, Young Chun Jung, Derek Magdziak, Adam Looker, Billie J. Kline, Václav Jurcík, Beatriz Dominguez Olmo
  • Publication number: 20140309213
    Abstract: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 25, 2012
    Publication date: October 16, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
  • Patent number: 8859581
    Abstract: The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumors and/or diseases in the development or course of which kinases are involved.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: October 14, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Andree Blaukat, Wolfgang Staehle, Hartmut Greiner, Maria Kordowicz
  • Publication number: 20140303142
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 9, 2014
    Inventors: John W. Butcher, David Witter, Christopher Dinsmore, June Kim, John Hendrix, Raksha Acharya, Sean P. Ahearn, Joon Jung, Alexey Rivkin, Philip Jones
  • Publication number: 20140303171
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Publication number: 20140303153
    Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 9, 2014
    Inventors: Hervé GENESTE, Michael OCHSE, Karla DRESCHER, Berthold BEHL, Loic LAPLANCHE, Jürgen DINGES, Clarissa JAKOB
  • Publication number: 20140303164
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are 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 a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: February 28, 2014
    Publication date: October 9, 2014
    Inventors: Gediminas BRIZGYS, Eda CANALES, Chien-Hung CHOU, Michael GRAUPE, Yunfeng Eric HU, John O. LINK, Qi LIU, Yafan LU, Roland D. SAITO, Scott D. SCHROEDER, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
  • Publication number: 20140303121
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 9, 2014
    Inventors: Jiazhong Zhang, Wayne Spevak