Abstract: The present invention relates to a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension, and the like.
Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).
Type:
Application
Filed:
December 15, 2008
Publication date:
August 13, 2009
Applicant:
SANOFI-AVENTIS
Inventors:
Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
Abstract: The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory conditions.
Type:
Grant
Filed:
April 4, 2006
Date of Patent:
August 11, 2009
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Jin Mi Kim, Rene' Marc Lemieux, Bryan McKibben, Matt Aaron Tschantz, Hui Yu
Abstract: A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
March 27, 2009
Publication date:
July 23, 2009
Inventors:
Alan David Borthwick, Richard Jonathan Hatley, Deirdre Mary Bernadette Hickey, John Liddle, David George Hubert Livermore, Andrew McMurtrie Mason, Neil Derek Miller, Fabrizio Nerozzi, Steven Leslie Sollis, Anna Katrin Szardenings, Paul Graham Wyatt
Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.
Type:
Application
Filed:
December 6, 2006
Publication date:
June 25, 2009
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Tiziano Bandiera, Andrea Lombardi Borgia, Sten Christian Orrenius, Ettore Perrone, Italo Beria, Daniele Fancelli, Arturo Galvani
Abstract: The present invention provides compositions and methods for treating lysosomal disorders using a class of substituted imidazole derivatives or compounds.
Type:
Application
Filed:
November 26, 2008
Publication date:
June 25, 2009
Applicants:
The Hospital for Sick Children, Taiji Biomedical, Inc.
Inventors:
Clifford A. Lingwood, Michael S. McGrath, Arasteh Ari Azhir
Abstract: The present invention relates to a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension, and the like.
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Type:
Application
Filed:
May 8, 2007
Publication date:
June 11, 2009
Inventors:
William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Matthew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi k. Sawyer, Jan Antoinette C. Romero
Abstract: The present invention relates to salts of substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
Type:
Application
Filed:
July 16, 2006
Publication date:
June 11, 2009
Applicant:
Laboratorios Del Dr. Esteve, S.A.
Inventors:
Antonio Torrens Jover, Maria Rosa Cuberes Altisen, Jose Mas Prio, Lluis Sola, Jordi Benet Buchholz
Abstract: The present invention provides for novel piperazinylalkylpyrazole derivatives, the preparation method thereof and the selective T-type calcium channel blocking activity thereof. Particularly, it provides a piperazinylalkylpyrazole derivative as represented by the formula set forth below or its pharmaceutically acceptable salts, and its preparation method thereof. The compound of Formula 1 is a novel piperazinylalkylpyrazole derivative, which particulary has T-type Ca2+ channel blocking effect and thus can be useful as a therapeutic agent for nerve and muscle pain.
Type:
Grant
Filed:
August 25, 2006
Date of Patent:
June 9, 2009
Assignee:
Korea Institute of Science and Technology
Inventors:
Ghilsoo Nam, Kyung-Il Choi, Hun Yeong Koh, Ae Nim Pae, Hyewhon Rhim, In-Sung Choi
Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Abstract: The present invention relates to a pharmaceutical composition comprising gaboxadol or a pharmaceutically acceptable salt thereof and one or more inhibitors of PAT1 and/or one or more inhibitors of OAT. The present invention further relates to a pharmaceutical composition comprising from about 0.5 mg to about 50 mg gaboxadol or a pharmaceutically acceptable salt thereof, wherein the composition provides an in vivo plasma profile comprising a mean Tmax which is longer than about 20 minutes.
Abstract: and the pharmaceutically acceptable salts and esters thereof, wherein X1, X2, X3, Y1, Y2 and R are described herein inhibit the interaction of MDM2 protein with a p53-like peptide and hence have anti proliferative activity.
Type:
Application
Filed:
February 5, 2009
Publication date:
June 4, 2009
Inventors:
Nader Fotouhi, Gregory Jay Haley, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber
Abstract: Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.
Type:
Application
Filed:
February 6, 2009
Publication date:
June 4, 2009
Applicant:
AMGEN, INC.
Inventors:
Christopher Hulme, Paul Tempest, Vu Van Ma, Thomas Nixey, Guity Balow
Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.
Abstract: The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.
Type:
Application
Filed:
October 14, 2008
Publication date:
May 21, 2009
Applicant:
ARQULE, INC.
Inventors:
Rui-Yang Yang, Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Rocio Palma, Neil Westlund
Abstract: The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
Type:
Application
Filed:
November 13, 2008
Publication date:
May 14, 2009
Applicant:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Inventors:
Shaomeng Wang, Haiying Sun, Dongguang Qin, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu, Yuefeng Peng, Qian Cai
Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.
Type:
Application
Filed:
April 10, 2007
Publication date:
May 7, 2009
Inventors:
Richard Berger, Scott Edmondson, Hansen Alexa, Cheng Zhu
Abstract: The present invention is directed to imidazolidinone compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Type:
Application
Filed:
November 10, 2006
Publication date:
April 30, 2009
Inventors:
James C. Barrow, Kenneth E. Rittle, Phung Le Bondiskey
Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,
Type:
Application
Filed:
July 24, 2008
Publication date:
April 30, 2009
Applicant:
The Ohio State University Research Foundation
Inventors:
Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang
Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.
Abstract: The present invention relates to compounds of Formula I, II, III or IV, or pharmaceutically acceptable salts, esters or prodrugs thereof: which can inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. 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 a compound of the present invention.
Type:
Application
Filed:
January 18, 2008
Publication date:
April 16, 2009
Inventors:
Ying SUN, Dong LIU, Yat Sun OR, Zhe WANG
Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
Type:
Grant
Filed:
May 3, 2007
Date of Patent:
April 7, 2009
Assignee:
Cephalon, Inc.
Inventors:
Robert L. Hudkins, Dandu R. Reddy, Ming Tao, Theodore L. Underiner, Allison L. Zulli
Abstract: The present invention discloses novel compounds of Formula I: (I) having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.
Type:
Application
Filed:
April 19, 2007
Publication date:
April 2, 2009
Inventors:
Ashraf Saeed, Owen Brendan Wallace, Yanping Xu, Thomas Edward Mabry, Rebecca Lynn Rezac Guenther, Nancy June Snyder
Abstract: The disclosure relates to compounds of formula (I): wherein Ra, Rb, R, and n are as defined in the disclosure, to pharmaceutical compositions comprising said compounds, and to processes for making and methods of using the same.
Type:
Application
Filed:
July 15, 2008
Publication date:
March 26, 2009
Applicant:
AVENTIS PHARMA S.A.
Inventors:
Frank HALLEY, Youssef EL-AHMAD, Victor CERTAL, Corinne VENOT, Anne DAGALLIER, Hartmut STROBEL, Kurt RITTER, Sven RUF
Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
Type:
Application
Filed:
August 21, 2008
Publication date:
March 19, 2009
Applicant:
ASTRAZENECA AB
Inventors:
James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
Abstract: The present application describes deuterium-enriched itraconazole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hyper-triglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
Type:
Grant
Filed:
March 7, 2005
Date of Patent:
March 17, 2009
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Lieven Meerpoel, Leo Jacobus Jozef Backx, Libuse Jaroskova, Peter Walter Maria Roevens, Louis Jozef Elisabeth Van Der Veken, Marcel Viellevoye, Joannes Theodorus Maria Linders
Abstract: Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(?O) or formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or except when Z is a radical of formula —N(OH)CH(?O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1-C6) alkyl or phenyl(C1-C6)alkyl-; and R5 and R6 are as defined in the specification.
Type:
Application
Filed:
September 26, 2006
Publication date:
March 12, 2009
Applicant:
British Biotech Pharmaceuticals Ltd.
Inventors:
Paul Raymond Beckett, Steven Launchbury, Gilles Pain, Lisa Marie Pratt
Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.
Type:
Application
Filed:
December 22, 2005
Publication date:
March 12, 2009
Applicant:
AstraZeneca AB
Inventors:
Michael Balestra, Heather Bunting, Deborah Chen, Ian Egle, Janet Forst, Jennifer Frey, Methvin Isaac, Fupeng Ma, David Nugiel, Abdelmalik Slassi, Gary Steelman, Guang-Ri Sun, Babu Sundar, Radhakrishnan Ukkiramapandian, Rebecca Urbanek, Sally Walsh
Abstract: The present invention relates to a compound of formula I wherein R1, R2, R3, and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These compounds are NK3 receptor antagonists, useful for the treatment of such disorders as depression, pain, bipolar disorders, psychosis, Parkinson's disease, schizophrenia, anxiety, and attention deficit hyperactivity disorder (ADHD).
Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl 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, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
Type:
Application
Filed:
May 23, 2008
Publication date:
March 5, 2009
Inventors:
Richard Apodaca, J. Guy Breitenbucher, Natalie A. Hawryluk, William M. Jones, John M. Keith, Jeffrey E. Merit, Mark S. Tichenor, Amy K. Timmons
Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors.
Type:
Application
Filed:
June 17, 2008
Publication date:
February 26, 2009
Applicant:
IRONWOOD PHARMACEUTICALS, INC.
Inventors:
Mark G. CURRIE, John Jeffrey TALLEY, Brian CALI
Abstract: The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc.
Type:
Application
Filed:
October 20, 2006
Publication date:
February 19, 2009
Inventors:
Yasunori Moritani, Ritsuo Imashiro, Atsushi Sato
Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
Type:
Application
Filed:
December 9, 2005
Publication date:
February 19, 2009
Inventors:
Barbara Attenni, Federica Ferrigno, Philip Jones, Raffaele Ingenito, Olaf Kinzel, Laura Llauger Bufi, Jesus Maria Ontoria, Giovanna Pescatore, Michael Rowley, Rita Scarpelli, Carsten Schultz
Abstract: The present invention provides triazole derivatives according to formula (I) as ligands of G-protein coupled receptors (GPCR), which are useful for the study of and/or the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, which are mediated by GPCR.
Type:
Application
Filed:
February 14, 2008
Publication date:
February 12, 2009
Applicant:
AETERNA ZENTARIS GmbH
Inventors:
Daniel Perrissoud, Huy Ong, Mukandila Mulumba, Christian Jossart, Yves Lachance
Abstract: The present invention provides a prophylactic or therapeutic agent for depression or anxiety disorders, comprising (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.
Abstract: The present invention relates to substituted phenyl-piperazine compounds of general formula (I), a process for their preparation, medicaments comprising said substituted phenyl-piperazine compounds as well as the use of said substituted phenyl-piperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
Type:
Application
Filed:
December 29, 2005
Publication date:
February 12, 2009
Applicant:
LABORATORIOS DEL DR. ESTEVE S.A.
Inventors:
Andrea Aschenbrenner, Juergen Kraus, Stefan Tasler, Andreas Wuzik, Jordi-Ramon Quintana-Ruiz
Abstract: The invention provides a combination of an ancillary agent and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein the ancillary agent is selected from: a monoclonal antibody, an alkylating agent, an anticancer agent, a further CDK inhibitor and a hormone, hormone agonist, hormone antagonist or hormone modulating agent; X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NR9(C?O) or 0(C?O) wherein R9 is hydrogen or C?hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.
Type:
Application
Filed:
January 20, 2006
Publication date:
February 5, 2009
Applicant:
ASTEX THERAPEUTICS LIMITED
Inventors:
Jayne Elizabeth Curry, John Francis Lyons, Matthew Simon Squires, Neil Thomas Thompson, Kyla Merriom Thompson, Paul Graham Wyatt
Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
Type:
Grant
Filed:
August 22, 2006
Date of Patent:
January 27, 2009
Assignee:
Sanofi-Aventis
Inventors:
Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
Abstract: The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below for the treatment of depression. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one additional antidepressant.
Type:
Application
Filed:
October 22, 2007
Publication date:
December 25, 2008
Inventors:
Yong Moon Choi, Robert Gordon, Magali Haas, Ewa Malatynska
Abstract: Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Type:
Grant
Filed:
March 24, 2005
Date of Patent:
December 23, 2008
Assignee:
Abbott Laboratories Inc.
Inventors:
Lee D. Arnold, Jürgen Dinges, Richard W. Dixon, Stevan W. Djuric, Anna M. Ericsson, Kimba Fischer, Alan F. Gasiecki, Vijaya J. Gracias, James H. Holms, Makoto Takeshita, Michael R. Michaelides, Melanie A. Muckey, Paul Rafferty, Douglas H. Steinman, Carol K. Wada, Zhiren Xia, Irini Akritopoulou-Zanze, Henry Q. Zhang
Abstract: The present invention relates to a pharmaceutical composition containing a pyrazole derivative as an active ingredient, which has antagonistic activity against serotonin 5-HT3A and is effective for the prevention and treatment of central nervous system (CNS) diseases, including emesis, nausea, alcoholism, drug abuse, depression, compulsive neurosis, anxiety, seizure, Alzheimer's disease, Parkinson's disease, Huntington's chorea, psychosis, schizophrenia, suicidal tendency, sleep disorder, appetite disorder and migraine.
Type:
Application
Filed:
June 13, 2008
Publication date:
December 18, 2008
Applicant:
KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
Inventors:
Ghil Soo Nam, Hye Whon Rhim, Ae Nim Pae, Kyung II Choi, Hyun Ah Choo, Seung Yeol Nah
Abstract: The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Type:
Application
Filed:
August 3, 2006
Publication date:
December 11, 2008
Applicant:
ASTRAZENECA AB
Inventors:
James R. Empfield, Michael Laplante, Megan Murphy King, Thomas R. Simpson, Maxime C. Tremblay, James M. Woods, Jingbo Yan
Abstract: The present invention relates to a compound of formula I wherein R1, R2, R3, and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These compounds are NK3 receptor antagonists, useful for the treatment of such disorders as depression, pain, bipolar disorders, psychosis, Parkinson's disease, schizophrenia, anxiety, and attention deficit hyperactivity disorder (ADHD).
Abstract: The present invention relates to heterocyclic compounds which are positive modulators of metabotropic glutamate receptor. The present invention also relates to the use of these compounds for preparing a pharmaceutical composition and to a method of treating a medical disorder, selected from neurological and psychiatric disorders associated with glutamate dysfunction.
Type:
Application
Filed:
May 23, 2008
Publication date:
December 4, 2008
Inventors:
Herve GENESTE, Daryl Sauer, Wilfried Braje, Wilhelm Amberg, Mario Mezler, Margaretha Henrica Maria Bakker