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
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
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.
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
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
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
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.
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
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.
Inventors:
David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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.
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
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
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.
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
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
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.
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
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
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
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
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
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
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
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
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
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
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
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
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
Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.