The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/252.03)
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Publication number: 20120157432Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: August 17, 2010Publication date: June 21, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent j. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
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Publication number: 20120149674Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: February 23, 2012Publication date: June 14, 2012Applicant: Merck Sharpe & Dohme Corp.Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Publication number: 20120149710Abstract: Bacterial infections, including Methicillin resistant Staphylococcus aureus (MRSA) infections are a major health problem that has created a pressing need for new antibiotics. Pyridazinone, rhodanine, and pyrazolethione compounds effective inhibit the enzymatic activity of sortase A (srtA) found in gram positive bacteria are disclosed. A structure activity relationship (SAR) analysis led to the identification of several pyridazinone and pyrazolethione analogs that inhibit SrtA with IC50 values in the sub-micromolar range. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Many of these molecules also inhibit the sortase enzyme from B. anthracis suggesting that they may be generalized sortase inhibitors. The novel compounds, compositions, uses, formulations, medicaments, articles of manufacture provide improved materials, uses, and treatments useful in combating infectious disorders.Type: ApplicationFiled: August 23, 2010Publication date: June 14, 2012Inventors: Michael E. Jung, Robert T. Clubb, Sung Wook Yi, Nutee Suree, Jeremy Justin Clemens
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Publication number: 20120142695Abstract: Compounds of the formula I wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.Type: ApplicationFiled: February 22, 2011Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert HAUEL, Angelo CECI, Henri DOODS, Ingo KONETZKI, Juergen MACK, Henning PRIEPKE, Annette SCHULER-METZ, Rainer WALTER, Dieter WIEDENMAYER
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Patent number: 8193352Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: GrantFiled: September 2, 2009Date of Patent: June 5, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud LeTiran, Joseph Drumm
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Patent number: 8188084Abstract: 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: GrantFiled: May 25, 2007Date of Patent: May 29, 2012Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA.Inventors: Philip Jones, Olaf Kinzel, Giovanna Pescatore, Laura Llauger Bufi, Carsten Schultz-Fademrecht, Federica Ferrigno
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Publication number: 20120128630Abstract: The present invention concerns a 1-(6 members azo-heterocyclic)-pyrrolin-2-one compound of the following formula I or a salt, solvate, tautomer, isotope, enantiomer, diastereoisomer or racemic mixture thereof: the pharmaceutical composition thereof and their therapeutic use as inhibitors of Hepatitis C NS5B polymerase.Type: ApplicationFiled: July 9, 2010Publication date: May 24, 2012Applicant: VIVALISInventors: Amaya Berecibar, Philippe Guedat, Céline Mohamed-Arab
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Publication number: 20120115861Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R7 and Y have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours and for the treatment of inflammatory diseases.Type: ApplicationFiled: June 17, 2010Publication date: May 10, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Michel Calderini, Margarita Wucherer-Plietker, Ulrich Graedler, Christina Esdar
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Publication number: 20120095012Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.Type: ApplicationFiled: December 30, 2009Publication date: April 19, 2012Applicant: Elara Pharmaceuticals GmbHInventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen
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Publication number: 20120095010Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: ApplicationFiled: December 22, 2011Publication date: April 19, 2012Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
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Publication number: 20120094993Abstract: The present invention relates to compounds of formula I, wherein A, R1 to R7 are defined in the description, and to pharmaceutically acceptable salts thereof. The present invention also relates to the manufacture of such compounds or their pharmaceutically acceptable salts, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: October 7, 2011Publication date: April 19, 2012Inventors: Uwe Grether, Paul Hebeisen, Torsten Hoffmann, Stephan Roever
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Publication number: 20120095001Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: June 7, 2010Publication date: April 19, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Patent number: 8158627Abstract: The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: GrantFiled: April 27, 2007Date of Patent: April 17, 2012Assignee: Northwestern UniversityInventors: D. Martin Watterson, Linda Van Eldik, Wenhui Hu
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Publication number: 20120087913Abstract: Methods and compositions for enhancing the ability of hypoxia-activated bioreductive agents to kill tumor cells within solid tumors are provided. Local regions of hypoxia are created within a tumor, or within a region containing a tumor, resulting in enhanced activation of hypoxia-activated bioreductive agents (e.g. tirapazamine) within the local region. The activated hypoxia-activated bioreductive agents kill tumor cells in the hypoxic region by catalyzing DNA stand breakage within the tumor cells. Because the activity is localized, side effects that typically occur as a result of systemic administration of bioreductive agents are reduced.Type: ApplicationFiled: April 8, 2009Publication date: April 12, 2012Inventors: Ruey-min Lee, Peck-sun Lee
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Publication number: 20120077812Abstract: The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: November 30, 2011Publication date: March 29, 2012Inventors: JING FANG, Jun Tang, Andrew J. Carpenter, Gregory Peckham, Christopher R. Conlee, Kien S. Du, Subba Reddy Katamreddy
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Publication number: 20120071467Abstract: Compounds or pharmacologically acceptable salts thereof are provided. In various embodiments the compounds have an antagonistic effect on a neurokinin NK1 receptor, a neurokinin NK2 receptor, and a muscarine M3 receptor. The compounds are useful as therapeutic agents for bronchial asthma, chronic obstructive pulmonary disease, or the like.Type: ApplicationFiled: September 16, 2011Publication date: March 22, 2012Applicant: Daiichi Sankyo Company, LimitedInventors: Takuya Ikeda, Takanori Yamazaki, Hiroshi Tsuchida
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Patent number: 8138188Abstract: The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.Type: GrantFiled: February 19, 2007Date of Patent: March 20, 2012Assignee: Pfizer Inc.Inventors: Mark David Andrews, Alan Daniel Brown, Mark Ian Lansdell, Nicholas William Summerhill
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Publication number: 20120065165Abstract: Compositions and methods of treating endothelial disorders, including: asthma, erectile dysfunction, pulmonary hypertension, cardiovascular disorders, and other disorders, using a synergistic combination of at least one arginase inhibitor and at least one phosphodiesterase (PDE1), (PDE2) and/or (PDE5) inhibitor are described.Type: ApplicationFiled: November 2, 2009Publication date: March 15, 2012Applicant: ARGINETIX, INCInventors: Simon E. Aspland, Dan E. Berkowitz, Trinity Bivalacqua, Hunter Champion
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Publication number: 20120059014Abstract: The present invention is directed to therapeutic compounds of the following formula (I) which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.Type: ApplicationFiled: March 12, 2010Publication date: March 8, 2012Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Tom Banksia Dupree, Peter Timothy Fry, Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Karen Lesley Schofield, Donald Smyth, Thomas Staroske, Alan John William Stewart, David French Stonehouse, Simon Andrew Swain, David Matthew Withall
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Publication number: 20120058939Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: March 8, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, Mark HADDEN, Emily Elizabeth FREEMAN
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Patent number: 8124628Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: April 6, 2007Date of Patent: February 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Publication number: 20120046289Abstract: The present invention is directed to pyridazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.Type: ApplicationFiled: October 26, 2009Publication date: February 23, 2012Inventors: Paul J. Coleman, Christopher D. Cox, Swati P. Mercer, Anthony J. Roecker, John D. Schreier
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Publication number: 20120040964Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Meizhong Xu, Colin Zhang, Yanlong Li, Jincong Zhuo, Brian W. Metcalf
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Publication number: 20120040953Abstract: The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.Type: ApplicationFiled: March 12, 2010Publication date: February 16, 2012Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Susan Helen Davis, Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, Karen Lesley Schofield, Thomas Staroske, Alan John William Stewart, Simon Andrew Swain, David Matthew Withall
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Publication number: 20120035164Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Inventors: Jianghe DENG, Jeffrey K. KERNS, Qi JIN, Guoliang LIN, Xichen LIN, Michael LINDENMUTH, Christopher NEIPP, Hong NIE, Sonia M. THOMAS, Katherine L. WIDDOWSON
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Publication number: 20120028988Abstract: Since a pyridazinone compound shown by formula (I) has an activity for controlling arthropod pests, the pyridazinone compound is effective for a use for controlling arthropod pests.Type: ApplicationFiled: March 24, 2010Publication date: February 2, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Norihisa Sakamoto, Takafumi Fusaka
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Publication number: 20120028951Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: February 4, 2010Publication date: February 2, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takahiko Taniguchi, Akira Kawada, Mitsuyo Kondo, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
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Publication number: 20120028986Abstract: The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes.Type: ApplicationFiled: September 2, 2009Publication date: February 2, 2012Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Marc Dietrich Voss, Hans Matter, Andreas Herling
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Publication number: 20120028987Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.Type: ApplicationFiled: September 20, 2011Publication date: February 2, 2012Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef DeCleyn, Michel Surkyn
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Publication number: 20120022073Abstract: The present invention relates to the treatment, alleviation, prevention or reduction in the incidence of symptoms, diseases or conditions resulting from or associated with enteroviruses, more particularly the enteroviral infections they cause.Type: ApplicationFiled: June 24, 2011Publication date: January 26, 2012Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: Johan Neyts, Armando De Palma, Hendrik Jan Thibaut, Pieter Leyssen, Simon Tucker
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Publication number: 20120022067Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: ApplicationFiled: July 26, 2010Publication date: January 26, 2012Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20120010185Abstract: The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U, V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk STENKAMP, Stephan Georg MUELLER, Gerald Juergen ROTH, Joerg KLEY, Klaus RUDOLF, Armin HECKEL, Marcus SCHINDLER, Ralf LOTZ, Thorsten LEHMANN-LINTZ
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Publication number: 20120010212Abstract: The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: June 29, 2011Publication date: January 12, 2012Inventors: Matthias Nettekoven, Hasane Ratni, Walter Vifian
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Publication number: 20120010182Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 8, 2011Publication date: January 12, 2012Applicants: ICAGEN INC., PFIZER LIMITEDInventors: Alan Daniel Brown, Marcel John De Groot, Brian Edward Marron, David James Rawson, Thomas Ryckmans, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West
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Publication number: 20120004231Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.Type: ApplicationFiled: September 13, 2011Publication date: January 5, 2012Applicant: CEPHALON, INC.Inventors: Robert L. Hudkins, Lars J.S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
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Publication number: 20120004217Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: ApplicationFiled: August 8, 2011Publication date: January 5, 2012Applicant: Purdue Pharma L.P.Inventors: Qun SUN, Laykea TAFESSE, Sam VICTORY
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Publication number: 20110312958Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20110305689Abstract: This invention relates, e.g., to a method for treating a subject having a chronic inflammatory respiratory disorder, comprising administering to the subject an effective amount of an inhibitor of the expression of and/or the activity of VEGF-A and/or VEGFR1 and/or VEGFR2 and/or NP1, or a combination thereof. Also described are screeing assays for agents for treating a subject having a chronic inflammatory respiratory disorder, and kits for performing one of the methods of the invention.Type: ApplicationFiled: November 6, 2009Publication date: December 15, 2011Applicant: The Johns Hopkins UniversityInventor: Jean Kim
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Patent number: 8076331Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.Type: GrantFiled: July 29, 2010Date of Patent: December 13, 2011Assignee: Cephalon, Inc.Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
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Publication number: 20110288100Abstract: The present invention discloses a compound of formula: where Ar1, Ar2, X, Z1, Z2, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Pyridylene Compound”); compositions comprising an effective amount of a Pyridylene Compound; and methods for treating or preventing pain or other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Pyridylene Compound.Type: ApplicationFiled: June 23, 2011Publication date: November 24, 2011Applicant: Purdue Pharma L.P.Inventor: Qun Sun
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Publication number: 20110288075Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.Type: ApplicationFiled: August 3, 2011Publication date: November 24, 2011Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Allison L. Zulli
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Publication number: 20110288092Abstract: Disclosed are methods of treating hyperproliferative disorders, method of treating inflammatory disorders, and methods of inhibiting MEK activity in a mammal, comprising administering an effective amount of one or more compounds of the Formula V or pharmaceutically acceptable salts thereof, wherein R1, R2, R7, R8, R9 and W are as defined in the specification.Type: ApplicationFiled: November 22, 2010Publication date: November 24, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Publication number: 20110269771Abstract: Compounds of the formula (I), in which D, R1, R2, R3, R4 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: December 10, 2009Publication date: November 3, 2011Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Publication number: 20110269712Abstract: This invention is directed to compounds of Formula (1) including all geometric and stereoisomers, N oxides, and agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides, (1) provided that the compound of Formula 1 is other than 2-[1-[(2-chlorophenyl)acetyl]-4-piperidinyl]-N-methyl-N-[(1R)-1-phenylethyl]-4-thiazolecarboxamide and R1 is other than 4-fluorophenyl; wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, Also disclosed are compositions containing the a compound having a formula corresponding to Formula (1) where the provisos are both omitted; and methods for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound having a formula corresponding to Formula (1) where the provisos are both omitted.Type: ApplicationFiled: July 26, 2006Publication date: November 3, 2011Inventors: John Joseph Bisaha, Patrick Ryan Kovacs, Renne M. Lett, Jeffrey Keith Long, Robert James Pasteris, Boris Abramovich Klyashchitsky, Bruce Lawrence Finkelstein, Brenton Todd Smith
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Publication number: 20110269769Abstract: The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: June 4, 2009Publication date: November 3, 2011Inventors: Linus S. Lin, Marc D. Chioda, Ping Liu, Ravi P. Nargund
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Publication number: 20110269770Abstract: The present invention relates to pyrazole compounds of formulae I or II and the salts and N-oxides thereof, wherein A is a pyrazole radical of formulae A1, A2 or A3, wherein # denotes the binding site; R41, R42, R43, R51 are H, halogen, CN, NO2, C1-C10-alkyl and the like; R52, R53 are H, halogen, CN, NO2, C1-C10-alkyl, and the like; R61, R62, R63 are H, CN, NO2, C1-C10-alkyl, and the like; T is C(Rt) or N; U is C(Ru) or N; V is C(Rv) or N; W is C(Rw) or N; with the proviso that at least one of the groups T, U, V and W is N; Rt, Ru, Rv, Rw are H, halogen, C1-C4-alkyl and the like; X1 is S, O or NR1a, wherein R1a is selected H, C1-C10-alkyl and the like; X2 is OR2a, NR2bR2c, S(O)mR2d, wherein m is 0, 1 or 2, R2a is C1-C4-alkyl, C1-C4-haloalkyl and the like, R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl and the like, or R2b and R2c together with the nitrogen atom to which they are bound form a heterocycle, and R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl and the like; and R1 is H, CN, C1-C10-alkyType: ApplicationFiled: September 23, 2009Publication date: November 3, 2011Applicant: BASF SEInventors: Steffen Gross, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Prashant Deshmukh, Joachim Dickhaut, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Faraneh Oloumi
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Publication number: 20110269734Abstract: Compounds of formula (I):or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.Type: ApplicationFiled: July 10, 2009Publication date: November 3, 2011Applicant: Prosidion LimitedInventors: Lisa Sarah Bertram, Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, John Keily, Thomas Martin Krulle, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Simon Andrew Swain
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Publication number: 20110263590Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.Type: ApplicationFiled: June 7, 2011Publication date: October 27, 2011Applicant: Biota Europe LimitedInventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
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Publication number: 20110263567Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.Type: ApplicationFiled: September 11, 2009Publication date: October 27, 2011Applicant: Semmelweis EgyetemInventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
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Publication number: 20110262525Abstract: This invention relates to compositions and methods useful for treating various cancers. Therapeutic combinations and methods of use thereof are also covered in the present application.Type: ApplicationFiled: December 11, 2007Publication date: October 27, 2011Applicant: SCHERING CORPORATIONInventors: Yan Wang, Chen Zong, Cynthia Seidel-Dugan, Yaolin Wang, Siu-Long Yao, Brian Der-Hua Lu, Mohamad H. Ladha