Abstract: The present invention relates to novel base stable ionic liquids and uses thereof as solvents in chemical reactions, especially base catalysed chemical reactions and reactions comprising the use of strong basis.
Type:
Application
Filed:
January 4, 2006
Publication date:
August 27, 2009
Applicant:
The Queen's University of Belfast
Inventors:
Martyn J. Earle, Ute Frohlich, Susanne Huq, Suhas Katdare, Rafal Marcin Lukasik, Ewa Bogel, Natalia Vladimirovna Plechkova, Kenneth Richard Seddon
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.
Type:
Application
Filed:
May 29, 2007
Publication date:
August 20, 2009
Inventors:
Philip Jones, Olaf Kinzel, Laura Llauger, Ester Muraglia, Giovanna Pescatore, Caterina Torrisi
Abstract: Substituted sulfonamide compounds corresponding to the formula I? wherein m, n, p, X, Y, Z, R1, RA and RB have specified meanings, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these substituted sulfonamide compounds for the treatment and/or inhibition of pain or other conditions.
Type:
Application
Filed:
January 16, 2009
Publication date:
August 13, 2009
Applicant:
GRUENENTHAL GmbH
Inventors:
Beatrix Merla, Stefan Oberboersch, Ruth Jostock, Michael Engels, Stefan Schunk, Melanie Reich, Sabine Hees
Abstract: Compositions are provided that include an electron donor and a sensitizing compound. More specifically, the electron donor is an arylsulfinate salt. Methods of polymerization are also provided that can be used to prepare polymeric material from a photopolymerizable composition that includes ethylenically unsaturated monomers and a photoinitiator system. The photoinitiator system includes an electron donor and a sensitizing compound.
Type:
Application
Filed:
April 23, 2009
Publication date:
August 13, 2009
Inventors:
Rajdeep S. Kalgutkar, Michael C. Palazzotto
Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.
Type:
Grant
Filed:
August 25, 2006
Date of Patent:
August 11, 2009
Assignee:
Biovitrum AB
Inventors:
Patrizia Caldirola, Ulf Bremberg, Gary Johansson, Andrew Mott, Annika Jenmalm Jensen, Katarina Beierlien, Markus Thor, Lars Tedenborg
Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.
Type:
Grant
Filed:
August 30, 2005
Date of Patent:
July 28, 2009
Assignee:
Biovitrum AB
Inventors:
Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Lori Sutin, Andrew Mott, Jan Tejbrant
Abstract: Substituted sulfonamide compounds corresponding to the formula I wherein m, n, p, Q, R1, R2, R3, R4, X, Y and Z have the respective meanings defined herein, pharmaceutical compositions containing such compounds, a process for their preparation, and the use of such compounds for the treatment and/or inhibition of pain and other conditions mediated by bradykinin receptor 1 (B1R) and/or bradykinin receptor 2 (B2R).
Type:
Application
Filed:
January 16, 2009
Publication date:
July 23, 2009
Applicant:
GRUENENTHAL GmbH
Inventors:
Beatrix Merla, Stefan Oberboersch, Ruth Jostock, Michael Engels, Stefan Schunk, Melanie Reich, Sabine Hees
Abstract: The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing A?40 and A?42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? such as Alzheimer's disease or Down's syndrome.
Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
Abstract: The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.
Type:
Application
Filed:
October 26, 2006
Publication date:
June 25, 2009
Inventors:
Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
Abstract: The present invention relates to ?-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
Type:
Application
Filed:
December 12, 2006
Publication date:
June 18, 2009
Inventors:
Jitendra A. Sattigeri, Shahadat Ahmed, Murugaiah M.S. Andappan, Sachin Sethi, Lalima Sharma, Chanchal Kumar Pal, Sachin Ramesh Kandalkar, Dipak C. Mahajan, Kaushal Kishore, Sumati Bhatia, Anil G. Gadhave, Vinay S. Bansal, Joseph Alexanand Davis
Abstract: This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, COPD and micturition disorders such as urinary incontinence.
Type:
Grant
Filed:
April 4, 2005
Date of Patent:
June 9, 2009
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frans Eduard Janssens, Bruno Schoentjes, Sophie Coupa, Alain Philippe Poncelet, Yvan René Ferdinand Simonnet
Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.
Type:
Grant
Filed:
October 25, 2006
Date of Patent:
May 26, 2009
Assignee:
Adolor Corporation
Inventors:
Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
Abstract: Compound of formula (I): wherein: represents 1-oxidopyridyl substituted by the remainder of the molecule in any one of the positions 2, 3 and 4, m and n, which may be identical or different, each represent an integer of from 1 to 3, R1 represents hydrogen or alkyl, R2 and R3, which may be identical or different, each represent an atom or group selected from hydrogen, halogen, alkyl, hydroxy, acyloxy and alkoxy, or, together with the carbon atom carrying them, form a cycloalkane having from 3 to 6 carbon atoms, R4 and R5 each represent hydrogen, or are adjacent and, together with the carbon atoms carrying them, form a benzo ring, Ar represents aryl or heteroaryl. Medicinal products containing the same which are useful as thrombin inhibitors.
Type:
Application
Filed:
January 22, 2009
Publication date:
May 21, 2009
Applicant:
LES LABORATOIRES SERVIER
Inventors:
Guillaume De Nanteuil, Philippe Gloanec, Jean-Gilles Parmentier, Alain Benoist, Alain Rupin, Marie-Odile Vallez, Tony Verbeuren
Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Type:
Application
Filed:
November 18, 2008
Publication date:
May 7, 2009
Inventors:
Wenge Xie, Brian Herbert, Jianguo MA, Truc Minh NGUYEN, Richard SCHUMACHER, Carla Maria Gauss, Ashok TEHIM
Abstract: The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.
Type:
Grant
Filed:
February 11, 2005
Date of Patent:
April 28, 2009
Inventors:
Patrizia Caldirola, Björn M. Nilsson, Gary Johansson
Abstract: The present invention relates to a novel class of substituted nicotinamides. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
Type:
Application
Filed:
October 30, 2006
Publication date:
April 23, 2009
Inventors:
Christopher Hamblett, Dawn M. Mampreian, Joey L. Methot, Thomas Miller, David L. Sloman, Matthew G. Stanton, Kevin Wilson
Abstract: Certain substituted tetrahydroisoquinoline compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
Type:
Application
Filed:
February 28, 2008
Publication date:
April 16, 2009
Inventors:
Cheryl A. Grice, Michael A. Letavic, Alejandro Santillan, JR., Kimberly L. Schwarz
Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
Abstract: 8,9-Dihydroxydihydropyridopyrazine-1,6-diones and 8,9-dihydroxypyridopyrazine-1,6-diones are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the pyridopyrazinediones are of Formula (I): (I), wherein R1, R2, R3, R4 and R5 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.
Type:
Grant
Filed:
September 10, 2003
Date of Patent:
April 14, 2009
Assignee:
Merck & Co., Inc.
Inventors:
John S. Wai, Boyoung Kim, Thorsten E. Fisher, Peter D. Williams, H. Marie Langford
Abstract: The disclosure relates to the dyeing of keratin materials using indole-derived styryl dyes comprising an alkylene linker. Disclosed herein is a dye composition comprising an indole-derived styryl dye comprising an alkylene linker, and a dyeing process with, for example, a lightening effect on keratin materials such as hair, using said composition. Disclosed herein are novel indole-derived styryl dyes comprising an alkylene linker and the uses thereof in lightening keratin materials. This composition makes it possible to obtain a coloring with a lightening effect which can be resistant and visible on dark keratin fibers.
Abstract: This invention relates to novel diaza-bicyclo-alkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Type:
Application
Filed:
February 13, 2007
Publication date:
March 19, 2009
Inventors:
Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Jeppe Kejser Christensen, Tino Dyhring
Abstract: The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.
Type:
Application
Filed:
August 28, 2008
Publication date:
March 5, 2009
Applicant:
KALYPSYS, INC.
Inventors:
Timothy C. Gahman, Cunxiang Zhao, Hengyuan Lang, Mark Eben Massari
Abstract: This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
Type:
Application
Filed:
February 9, 2007
Publication date:
February 5, 2009
Inventors:
Dan Peters, John Paul Redrobe, Elsebet Ostergaard Nielsen
Abstract: Novel substituted arylpiperazine derivatives with activity as 5-hydroxytryptamine 1A (5-HT1A) receptor subtype ligands, to their stereochemical isomers, methods of their preparation, and to their use and to pharmaceutical compositions containing them for the treatment of Parkinson disease, cerebral damage by thromboembolic ictus, craneoencephalic traumatisms, depression, migraine, pain, psychosis, anxiety disorders, aggressive disorders or urinary tract disorders.
Type:
Application
Filed:
December 27, 2005
Publication date:
February 5, 2009
Applicant:
CEPA SCHWARZ PHARMA, S.L.
Inventors:
Maria Luz Lopez-Rodriguez, Bellinda Benhamu Salama
Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
Type:
Grant
Filed:
November 21, 2006
Date of Patent:
January 27, 2009
Inventors:
Meng-Hsin Chen, James B. Doherty, Robert Tynebor
Abstract: The present invention relates to a composition for modulating the activation of Nurr1, the composition comprising an agonist or an antagonist of a dopamine D2 receptor, methods for modulating the activation of Nurr1 by the dopamine D2 receptor, a method and composition for treating Nurr1-related diseases using the dopamine D2 receptor, and methods for screening a modulator of a dopamine D2 receptor of a test compound. Accordingly, the activation of Nurr1 can be modulated by treating the dopaminergic neurons with the agonist or the antagonist of the dopamine D2 receptor, thereby enhancing or inhibiting generation of the dopaminergic neurons.
Type:
Application
Filed:
June 22, 2006
Publication date:
January 15, 2009
Applicant:
Korea University Industry And Academy Cooperation Foundation
Abstract: The present invention relates to novel pyrrolopyrazine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
Type:
Application
Filed:
January 30, 2007
Publication date:
January 15, 2009
Inventors:
Andrew John Eatherton, Gerard Martin Paul Giblin, William Leonard Mitchell
Abstract: Eszopiclone is prepared by reacting zopiclone with an enatiomerically pure di-p-toluoyl tartaric acid, recovering a solid salt, and reacting a solid salt with a base. Zopiclone is prepared by reacting 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]-pyrazine with 1-chlorocarbonyl-4-methylpiperazine hydrochloride.
Type:
Grant
Filed:
September 5, 2006
Date of Patent:
January 13, 2009
Assignees:
Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.
Abstract: An object of the present invention is to provide a battery which is high in capacity density and superior in stability. An electrode containing a compound having a diazine-N,N?-dioxide structure shown by a general formula (1) described below as an electrode active material is used, where x, y, x?, and y? independently shows integer numbers of 0 or more respectively, and the order of condensation of diazine rings and benzene rings may be alternate or random. One of substituents R1, R2, R3, R4, Ra, Rb, Rc, and Rd shows a part of main chain or side chain of oligomer or polymer, and the other independently shows hydrogen atom, halogen atom, or a specific group.
Abstract: This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Type:
Application
Filed:
February 9, 2007
Publication date:
January 1, 2009
Inventors:
Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Jeppe Kejser Christensen
Abstract: 2,5-diaza-bicyclo[2.2.1]heptane derivatives represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, Hy, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR5-mediated disorders.
Type:
Application
Filed:
August 4, 2006
Publication date:
December 18, 2008
Applicant:
AstraZeneca AB
Inventors:
Louise Edwards, Methvin Isaac, Abdelmalik Slassi, Guang-Ri Sun, Tao Xin, Alexander Minidis, Peter Dove
Abstract: This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
Type:
Application
Filed:
February 9, 2007
Publication date:
December 11, 2008
Inventors:
Dan Peters, John Paul Redrobe, Elsebet Ostergaard Nielsen
Abstract: Compounds of Formula I: wherein R1 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
Type:
Application
Filed:
June 6, 2008
Publication date:
December 11, 2008
Applicant:
AstraZeneca AB
Inventors:
Joshua Clayton, Ian Egle, James Empfield, James Folmer, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi
Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.
Type:
Grant
Filed:
March 18, 2005
Date of Patent:
December 2, 2008
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.
Abstract: This invention relates to novel diazabicyclic aryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Type:
Application
Filed:
December 5, 2006
Publication date:
November 13, 2008
Inventors:
Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Tino Dyhring
Abstract: New pyridine-based compounds of Formula I, compositions, and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3-mediated disorders in vivo are provided. The methods, compounds, and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
Type:
Grant
Filed:
September 6, 2005
Date of Patent:
September 16, 2008
Assignee:
Novartis Vaccines and Diagnostics, Inc.
Inventors:
John M Nuss, Stephen D Harrison, David B Ring, Rustum S Boyce, Kirk Johnson, Keith B Pfister, Savithri Ramurthy, Lynn Seely, Allan S Wagman, Manoj C Desai, Barry H Levine
Abstract: The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1—R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Type:
Application
Filed:
February 19, 2008
Publication date:
August 21, 2008
Applicant:
MEMORY PHARMACEUTICALS CORPORATION
Inventors:
Robert Dunn, Truc Minh Nguyen, Wenge Xie, Ashok Tehim
Abstract: The present invention relates to certain derivatives of cycloalkanediones invariably substituted with a chroman-2-yl, 2-quinolyl or —O-phenyl residue which are serotonin (5-hydroxytryptamine, 5-HT) 5-HT1A receptor subtype agonists modulators, to their stereochemical isomers and to their use in the preparation of a medicament for the treatment of pathological states for which an agonist a modulator of these receptors is indicated.
Type:
Application
Filed:
January 28, 2005
Publication date:
August 21, 2008
Inventors:
Maria Luz Lopez-Rodriguez, Bellinda Benhamu Salama, Joaquin Del Rio Zambrana, Diana Frechilla Manso
Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, B, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR 5 mediated disorders.
Type:
Application
Filed:
August 4, 2006
Publication date:
August 14, 2008
Applicant:
AstraZeneca AB
Inventors:
Louise Edwards, Mithvin Isaac, Abdelmalik Slassi, Guang-Ri Sun, Peter Dove, Erwan Arzel
Abstract: 8-Hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds are inhibitors of HIV integrase and inhibitors of HIV replication. More particularly, the compounds are of Formula (I): wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful in the prevention and treatment of infection by ITV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.
Abstract: Substituted tetrahydropyrrolopyrazine compounds corresponding to the formula I: processes for their preparation, pharmaceutical compositions comprising these compounds and the use of these compounds for the treatment and/or inhibition of pain and other disorders or disease states at least partly mediated by KCNQ2/3 K+ channels.
Type:
Application
Filed:
October 17, 2007
Publication date:
July 10, 2008
Applicant:
GRUENENTHAL GmbH
Inventors:
Beatrix Merla, Thomas Christoph, Stefan Oberboersch, Klaus Schiene, Gregor Bahrenberg, Robert Frank, Sven Kuehnert, Wolfgang Schroeder
Abstract: The present invention provides compounds of the formula: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
Type:
Application
Filed:
February 15, 2008
Publication date:
July 10, 2008
Applicant:
Lncyte Corporation
Inventors:
Yun Long Li, Jincong Zhuo, David Burns, Wanqing Yao, Ravi Kumar Jalluri
Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Type:
Grant
Filed:
December 22, 2004
Date of Patent:
July 8, 2008
Assignee:
Memory Pharmaceuticals Corporation
Inventors:
Wenge Xie, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Type:
Application
Filed:
February 13, 2006
Publication date:
July 3, 2008
Applicant:
NeuroSearch A/S
Inventors:
Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Tino Dyhring
Abstract: The invention relates to a novel 3,9-diazabicycl?[3.3.1]nonene derivative of formula (I) and the enantiomers thereof and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing at least one compound of formula (I) or (I?) and especially their use as inhibitors of renin.(I).
Type:
Application
Filed:
January 26, 2006
Publication date:
July 3, 2008
Applicant:
ACTELION PHARMACEUTICALS LTD
Inventors:
Oliver Bezencon, Daniel Bur, Walter Fischli, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Thomas Weller