Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
Abstract: Compounds of formula I: wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.
Type:
Application
Filed:
November 3, 2008
Publication date:
February 3, 2011
Applicant:
BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
Inventors:
Youla S. Tsantrizos, Murray D. Bailey, François Bilodeau, Rebekah J. Carson, Lee Fader, Teddy Halmos, Stephen Kawai, Serge R. Landry, Steven Laplante, Bruno Simoneau
Abstract: Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radiolabelled 2?-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic antidepressant in vitro and in vivo pharmacological binding profiles in rodent brain and cells expressing human serotonin transporter (hSERT). Twelve 2?-alkyl-6-nitroquipazine ligands potently bind in sub-nanomolar concentrations to the pre-synaptic SERT binding site where established antidepressant drugs bind and inhibit the re-uptake of the neurotransmitter serotonin (5-HT). In vivo tracer studies in rats as well as monkey PET scan trial have demonstrated the fluorine-18 and carbon-11 positron radionuclide labeled tracers perform as quantitative tracers of specific binding the SERT protein in live brain.
Type:
Application
Filed:
September 22, 2010
Publication date:
January 13, 2011
Inventors:
John M. Gerdes, David B. Bolstad, Brian R. Kusche
Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
Type:
Application
Filed:
June 29, 2010
Publication date:
December 30, 2010
Inventors:
Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
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:
Grant
Filed:
April 10, 2007
Date of Patent:
December 28, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
Abstract: This invention is directed to a crystalline 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile monohydrate having an x-ray diffraction pattern wherein 2? angles (°) of significant peaks are at about: 9.19, 11.48, 14.32, 19.16, 19.45, 20.46, 21.29, 22.33, 23.96, 24.95, 25.29, 25.84, 26.55, 27.61, and 29.51, and a transition temperature of about 109° C. to about 115° C.
Type:
Application
Filed:
June 22, 2010
Publication date:
December 23, 2010
Applicant:
Wyeth LLC
Inventors:
Marc Sadler Tesconi, Gregg Feigelson, Henry Strong, Hong Wen
Abstract: Methods are provided for modulating post-natal migration of neurons. Activation of the 5-HT3A receptor increases migration, while pharmacological blockade of the 5-HT3A receptor disrupts neuroblast migration into the cortex and hippocampus. These neuroblasts mature into GABAergic interneurons, and thus are relevant to conditions associated with disturbances in 5-HT levels and GABAergic inhibition.
Abstract: Aspects of the invention relate to substituted aryl propylamino-oxy-analogs and uses thereof. Aspects of the invention relate to compositions that are inhibitors of ?-secretase and uses thereof for treating subjects having, or at risk of developing, Alzheimer's disease.
Type:
Application
Filed:
October 10, 2008
Publication date:
November 11, 2010
Applicant:
The Brigham and Women's Hospital, Inc
Inventors:
Corinne Elizabeth Augelli-Szafran, Michael S. Wolfe, Han-Xun Wei
Abstract: The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell.
Type:
Application
Filed:
January 24, 2007
Publication date:
November 4, 2010
Inventors:
Kristjan Gudmundsson, Sharon Davis Boggs, John Franklin Miller, Angilique Christina Svolto
Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
Type:
Application
Filed:
December 11, 2008
Publication date:
October 21, 2010
Applicant:
THE UNIVERSITY OF EDINBURGH
Inventors:
Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
Abstract: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.
Type:
Grant
Filed:
March 10, 2006
Date of Patent:
October 19, 2010
Assignee:
The Regents of The University of California
Inventors:
Dennis A. Carson, Howard B. Cottam, Sylvie Barchéchath, Mary Patricia Corr
Abstract: Methods of treating or preventing diseases associated with low bone mass in a mammal in need of such treatment or prevention comprising administering to the mammal a therapeutically effective amount of an agent that increases tryptophan hydroxylase 2 activity or of an agonist of the brain serotonin HT2C receptor. Diseases associated with low bone mass include osteoporosis, osteopenia, Paget's disease, osteomalacia, and renal osteodystrophy.
Type:
Application
Filed:
September 26, 2008
Publication date:
October 14, 2010
Applicant:
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
Abstract: Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radio-labelled 2?-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic antidepressant in vitro and in vivo pharmacological binding profiles in rodent brain and cells expressing human serotonin transporter (hSERT). Twelve 2?-alkyl-6-nitroquipazine ligands potently bind in sub-nanomolar concentrations to the pre-synaptic SERT binding site where established antidepressant drugs bind and inhibit the re-uptake of the neurotransmitter serotonin (5-HT). In vivo tracer studies in rats as well as monkey PET scan trial have demonstrated the fluorine-18 and carbon-11 positron radionuclide labeled tracers perform as quantitative tracers of specific binding the SERT protein in live brain.
Type:
Grant
Filed:
April 26, 2007
Date of Patent:
October 12, 2010
Assignee:
The University of Montana
Inventors:
John M. Gerdes, David B. Bolstad, Brian R. Kusche
Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
Type:
Application
Filed:
April 10, 2008
Publication date:
September 30, 2010
Inventors:
Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
Type:
Application
Filed:
September 8, 2009
Publication date:
September 23, 2010
Applicant:
ChemoCentryx, Inc.
Inventors:
Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi, Wei Chen, Penglie Zhang
Abstract: The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.
Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.
Type:
Application
Filed:
May 26, 2010
Publication date:
September 16, 2010
Applicant:
DOW AGROSCIENCES LLC
Inventors:
Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster
Abstract: The present disclosure relates to a combination of therapeutic agents for use in treating a patient a subject suffering from cancer. In addition, the present disclosure also relates to diagnostic assays useful in classification of patients for treatment with one or more therapeutic agents.
Type:
Application
Filed:
December 4, 2009
Publication date:
September 9, 2010
Applicant:
ABBOTT LABORATORIES
Inventors:
Omar Jameel Shah, Yu Shen, Xiaoyu Lin, Mark Anderson, Xiaoli Huang, Junling Li, Leiming Li
Abstract: The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.
Type:
Application
Filed:
August 22, 2008
Publication date:
September 2, 2010
Inventors:
Wilhelm Amberg, Michael Ochse, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
Type:
Application
Filed:
February 9, 2010
Publication date:
August 5, 2010
Applicant:
Gilead Palo Alto, Inc.
Inventors:
Matthew Abelman, Robert Jiang, Jeff Zablocki
Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with hydroxysteroid dehydrogenases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
Type:
Grant
Filed:
March 28, 2006
Date of Patent:
July 20, 2010
Assignee:
Takeda San Diego, Inc.
Inventors:
Kathleen Aertgeerts, Nancy K. Brennan, Sheldon X. Cao, Edcon Chang, Andre A. Kiryanov, Yan Liu
Abstract: The invention provides new oxazolidinone compounds of formula (I) wherein A is certain heterocycles optionally substituted; R1, R2, R3 and R4 are independently selected from —H and halogen; X is selected from O, S, NR9 and CR9R10; R9 and R10 having different meanings; Y is selected from O, S, SO, SO2, NO, NR12 and CR12R13; R12 and R13 having different meanings. It also provides different processes for the preparation of such compounds. Oxazolidinone compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections.
Type:
Grant
Filed:
June 26, 2006
Date of Patent:
July 20, 2010
Assignee:
Ferrer Internacional, S.A.
Inventors:
Montserrat Cano, Albert Palomer, Antonio Guglietta
Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, X, Y, Z, Ar, R1, R2, R3, R4, R5, R6 and R7 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
Type:
Grant
Filed:
August 17, 2007
Date of Patent:
July 13, 2010
Assignee:
Roche Palo Alto LLC
Inventors:
David Scott Carter, Ryan Craig Schoenfeld, Robert James Weikert
Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
Abstract: The present invention relates in general to anti-cancer drug design. More specifically, the invention provides methods of mapping and screening for anti-cancer agents using pharmacophore models. The invention demonstrates that, conformational sampling of a small lead molecule, followed by representative pharmacophore model development, is an efficient approach for rational design of novel anticancer agents with similar or better potency than the original lead but with different physicochemical properties.
Abstract: The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) a pyrimidylaminobenzamide compound; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukemia, especially chronic myelogenous leukemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, in combination with a pyrimidylaminobenzamide compound, in particular 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide.
Abstract: A triazole derivative of formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.
Type:
Application
Filed:
June 12, 2008
Publication date:
June 10, 2010
Applicants:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, CHEMON INC.
Inventors:
Bum Tae Kim, Yong Ki Min, Jung Nyoung Heo, Hyuk Lee, Sung Youn Chang, No Kyun Park, Si-Whan Song, Jung-Ja Oh
Abstract: The invention provides novel 1,2,4-thiadiazole derivatives useful for preventing or treating an ?-synucleopathy such as Parkinson's disease, as well as pharmaceutical compositions including them as biologically active ingredients, and methods for manufacturing them.
Type:
Application
Filed:
November 22, 2007
Publication date:
June 10, 2010
Inventors:
Gerard Griffioen, Stefaan Wera, Hein Roger Duhamel, Ellen Gommé, Nele Van Damme
Abstract: Compounds of Formula (I): are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class (3) and class (5) receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.
Type:
Application
Filed:
March 27, 2008
Publication date:
June 10, 2010
Applicant:
ARRAY BIOPHARMA INC.
Inventors:
Fredrik P. Marmsater, Mark C. Munson, James P. Rizzi, John E. Robinson, Stephen T. Schlacter, George T. Topalov, Joseph P. Lyssikatos
Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.
Type:
Application
Filed:
February 8, 2010
Publication date:
June 3, 2010
Applicant:
SANOFI-EVENTIS
Inventors:
Ahmed ABOUABDELLAH, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Type:
Application
Filed:
October 5, 2009
Publication date:
June 3, 2010
Applicant:
SANOFI-AVENTIS
Inventors:
Marc Nazaré, Gernot ZECH, Melitta JUST, Tilo WEISS, Gerhard HESSLER, Joerg Czech
Abstract: An aryl amide compound of Formula (I): or a pharmaceutically acceptable form thereof is disclosed. The compound is an ACC inhibitor and therefore useful in treating an ACC-mediated condition.
Abstract: A means for decreasing bacterial virulence in a mammal including man or in a plant by inhibition of the Type III secretion system at concentrations that do not prevent or substantially reduce bacterial growth comprises an N-substituted 7-quinolylmethyl amine, in particular one that is further substituted in 5- and 8-position on the quinoline ring. A corresponding therapeutic method and a pharmaceutical composition are also disclosed.
Abstract: The present invention relates to clotrimazole/quinoline hybrids useful as active ingredients of anti-malaria drugs. The compounds show a remarkable in vitro biological activity especially against the chloroquine-resistant Plasmodium falciparum strains and in vivo activity against P. berghei.
Abstract: This invention provides novel aryl piperazine derivatives represented by Formula (I) having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, incl. schizophrenia.
Type:
Application
Filed:
October 12, 2007
Publication date:
April 8, 2010
Applicant:
Universita degli Studi di Siena
Inventors:
Giuseppe Campiani, Stefania Butini, Caterina Fattorusso, Silvia Franceschini, Irene Zia Thale, Karin Sandager Nielsen, Jørgen Scheel-Krüeger, Lars Siim Madsen
Abstract: Methods of cancer diagnosis and prognosis using biomarkers.
Type:
Application
Filed:
July 14, 2009
Publication date:
April 1, 2010
Applicant:
Wyeth
Inventors:
Christina M. COUGHLIN, Michael E. BURCZYNSKI, Marisa P. DOLLED-FILHART, Robert PINARD, Donald WALDROM, Charles ZACHARCHUK, Frederick IMMERMANN, Maha KARNOUB, Jason CHRISTIANSEN, Mark GUSTAVSON, Annette MOLINARO, Alpana Waldron
Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.
Type:
Grant
Filed:
June 22, 2006
Date of Patent:
March 30, 2010
Assignee:
Sanofi-Aventis
Inventors:
Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
Abstract: This invention is directed to a pharmaceutical composition comprising an Src kinase inhibitor and an aromatase inhibitor, and to the use of a combination of an Src kinase inhibitor and an aromatase inhibitor in treating abnormal cell proliferation and abnormal angiogenesis associated with cancer, including breast cancer.
Type:
Application
Filed:
September 11, 2009
Publication date:
March 18, 2010
Applicant:
Wyeth
Inventors:
Charles Michael Zacharchuk, Frank Charles Boschelli, Jennifer Michele Golas, Kim Timothy Arndt
Abstract: A method for administering a spill-resistant pharmaceutical formulation comprises delivery from a squeezable container of a pharmaceutical agent in a suitable vehicle comprising a liquid base and a thickening agent.
Abstract: The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression and sexual dysfunction. The invention relates to compounds and pharmaceutically acceptable salts of formula (I?): wherein R1-R16, Ra, Rb, and n are set forth in the specification. The invention also relates to pharmaceutical compositions comprising compounds and pharmaceutically acceptable salts of formula (I?).
Type:
Grant
Filed:
June 9, 2006
Date of Patent:
March 2, 2010
Assignee:
Wyeth LLC
Inventors:
Magda Asselin, George Theodore Grosu, Annmarie Louise Sabb, Wayne Everett Childers, Lisa Marie Havran, Zhongqi Shen, James Jacob Bicksler, Dan Chaekoo Chong
Abstract: The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.
Abstract: The use of 5-HT6 serotonin receptor antagonists of formula (I): or pharmaceutically acceptable salts thereof, is described for the treatment of Irritable Bowel Syndrome and pain in mammals, more particularly inflammatory, neuropathic or visceral pain.
Type:
Application
Filed:
March 19, 2008
Publication date:
February 18, 2010
Applicant:
GLAXO GROUP LIMITED
Inventors:
Gordon Bruton, Barry Sidney Orlek, Geoffrey Stemp
Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof.
Type:
Application
Filed:
March 30, 2009
Publication date:
February 4, 2010
Inventors:
Michael P. Clark, Florence F. Wagner, Brandon C. Doroh, Tricia L. Johnson, Yesim Altas Tahirovic, Lawrence Wilson, John M. Wiseman, Jason W. Skudlarek, Mark A. Lockwood, Michael G. Natchus
Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.
Abstract: The present invention provides a therapeutic combination comprising (a) a compound 1 of formula (A) as set forth in the specification and (b) a BCR-ABL kinase inhibitor selected from the group consisting of Imatinib, Dasatinib, Nilotinib, Bosutinib and Inno-406, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
Type:
Application
Filed:
July 15, 2009
Publication date:
January 28, 2010
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Jürgen Moll, Dario Ballinari, Enrico Pesenti
Abstract: A subject of the invention is the compounds of formula (I): wherein R1, R2, R3, R?3, R4, R?4, R5, R6 and R7 are as described in the application, in the form of enantiomers or mixtures, as well as their salts with acids and bases, their preparation and their application as anti-bacterials, in both human and veterinary medicine.
Type:
Application
Filed:
June 23, 2009
Publication date:
January 14, 2010
Applicant:
Vetoquinol SA
Inventors:
Sandrine Ropp, Christophe Morice, Bruno Giethlen, Paola Ciapetti, Florence Chery-Mozziconacci, Camille G. Wermuth, Francoise Leblanc, Marc Schneider
Abstract: Non-peptide compounds having activity as selective antagonists of bradykinin (BK) B2 receptor are disclosed. The compounds have the general formula (I) in which R is hydrogen or methyl; W is a single bond or an oxygen atom; n=3; X is hydrogen or a —NR1R2 amino group in which R1 and R2 can be independently hydrogen or a group which is methyl, ethyl, n-propyl, or isopropyl; Y is a —NR3R4R5 quaternary ammonium group in which R3, R4, R5 can be independently a group which is methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or n-pentyl; and the enantiomers and enantiomeric mixtures thereof. Pharmaceutical compositions containing these compounds and methods of using the compounds to treat patients having conditions, disorders or diseases involving activation of bradykinin B2 receptors are also disclosed.
Type:
Grant
Filed:
April 10, 2007
Date of Patent:
January 12, 2010
Assignee:
Istituto Luso Farmaco D'Italia S.p.A.
Inventors:
Patrizia Felicetti, Christopher Ingo Fincham, Alessandro Giolitti, Carlo Alberto Maggi, Laura Quartara, Cristina Rossi
Abstract: Certain piperazinyl and piperidinyl urea compounds 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. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
Type:
Application
Filed:
September 11, 2009
Publication date:
January 7, 2010
Inventors:
Richard Apodaca, J. Guy Breitenbucher, Kanaka Pattabiraman, Mak Seierstad, Wei Xiao
Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using thiazolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiazolidinedione derivatives.
Type:
Application
Filed:
April 11, 2007
Publication date:
December 10, 2009
Inventors:
Michael Gerard Darcy, Steven David Knight, Nicholas D. Adams, Stanley J. Schmidt