Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/300)
  • Publication number: 20130116285
    Abstract: 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 a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, 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: Application
    Filed: July 6, 2011
    Publication date: May 9, 2013
    Applicant: Pfizer Limited
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Manuel Perez-Pacheco, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Publication number: 20130116443
    Abstract: The present invention relates to a process for the preparation of substituted 3-(2-hydroxyethyl)-1-[4-nitrophenyl]pyridin-2(1H)-ones which serve as important intermediate compounds for producing drugs.
    Type: Application
    Filed: April 26, 2011
    Publication date: May 9, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Joachim Krüger, Danja Grossbach, Holger Paulsen, Walter Kroh
  • Publication number: 20130109708
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: July 4, 2011
    Publication date: May 2, 2013
    Applicant: Pfizer Limited
    Inventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Patent number: 8431712
    Abstract: The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): and salts thereof. The invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: April 30, 2013
    Assignee: NephroGenex, Inc.
    Inventors: Raja G. Khalifah, Roland Keilitz, Christoph Koellner, Thorsten Degenhardt, Stephen Robert Brand
  • Patent number: 8426449
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: April 23, 2013
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Yen Pham Truong, Thomas Jon Seiders
  • Publication number: 20130096161
    Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: July 8, 2011
    Publication date: April 18, 2013
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • Publication number: 20130096162
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Patent number: 8410088
    Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: April 2, 2013
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Masashi Seki, Syuji Shirotori
  • Publication number: 20130065929
    Abstract: Methods for treating and/or preventing at least one symptom of a disorder associated with oxidative stress, carbonyl stress, or combinations thereof in a subject. In some embodiments, the methods include administering to the subject an effective amount of pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods for treating or preventing a nephropathy, acute renal injury, acute renal failure, or combinations thereof in a subject, and formulations adapted for intravenous administration comprising pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing.
    Type: Application
    Filed: October 24, 2012
    Publication date: March 14, 2013
    Applicant: VANDERBILT UNIVERSITY
    Inventor: VANDERBILT UNIVERSITY
  • Publication number: 20130039944
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: April 20, 2011
    Publication date: February 14, 2013
    Applicant: Kineta, Inc.
    Inventors: Shawn P. Iadonato, Kristin Bedard
  • Publication number: 20130012530
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20130005689
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 3, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Patent number: 8334308
    Abstract: The present invention relates to biphenyl-based renin inhibitor compounds having amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: December 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Rejean Fortin, Patrick Lacombe, Daniel McKay, Tom Yao-Hsiang Wu
  • Patent number: 8324392
    Abstract: The present invention relates to a novel solid form of 4-[[(6-chloropyridin-3-yl)methyl](2,2-difluoroethyl)amino]furan-2(5H)-one, to processes for its preparation and to its use in agrochemical preparations.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: December 4, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Britta Olenik, Robert Velten, Peter Jeschke, Norbert Lui, Christian Funke, Wolfgang Wirth
  • Patent number: 8309610
    Abstract: This invention relates to solid crystalline forms of (1RS,3RS,6RS)-6-Dimethylaminomethyl-1-(3-methoxy-phenyl)cyclohexane-1,3-diol hydrochloride (1), methods of producing 1, methods of use of 1, use of 1 as analgesics and pharmaceutical compositions comprising 1.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: November 13, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Michael Gruss, Helmut Buschmann, Andreas Fischer, Wolfgang Hell, Dagmar Lischke
  • Publication number: 20120259094
    Abstract: The present invention relates generally to affinity ligands and chemical affinity ligand-matrix conjugates for use as chromatographic adsorbents and methods which utilise the adsorbents in the purification of proteins by affinity chromatography. The affinity ligand-matrix conjugates of the present invention comprise ligands of general formula (I): wherein m represents an integer from 0-2, n represents an integer from 0-6, p represents an integer from 0-4, R1 represents H or C1-3 alkyl, R2 is an optional substituent, and X is the position at which the ligand is immobilized, optionally via a linker.
    Type: Application
    Filed: October 15, 2010
    Publication date: October 11, 2012
    Inventors: Milton TW Hearn, Anjali Makarand Bhagwat, William Roy Jackson, Simon John Mountford
  • Patent number: 8273773
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: September 25, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
  • Publication number: 20120232111
    Abstract: The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin—inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.
    Type: Application
    Filed: April 28, 2006
    Publication date: September 13, 2012
    Applicant: Shiseido Company, Ltd.
    Inventors: Mikiko Kaminuma, Masaru Suetsugu, Toshii Iida, Shinji Inomata
  • Patent number: 8263627
    Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels 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 T-type calcium channels are involved.
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Thomas S. Reger, Zhi-Qiang Yang
  • Publication number: 20120214785
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
  • Patent number: 8242145
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: August 14, 2012
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Thomas Jonathan Seiders, Brian Andrew Stearns, Bowei Wang, Yen Pham Truong, Jeannie M. Arruda
  • Publication number: 20120202781
    Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
    Type: Application
    Filed: April 8, 2010
    Publication date: August 9, 2012
    Inventors: Kevin James Gillen, Jonathan Gillespie, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
  • Publication number: 20120202795
    Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.
    Type: Application
    Filed: April 18, 2012
    Publication date: August 9, 2012
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: Philip M. WEINTRAUB, Paul R. EASTWOOD, Shujaath MEHDI, David W. STEFANY, Kwon Yon MUSICK, Neil MOORCROFT, Sungtaek LIM, John Z. JIANG, Hartmut RUTTEN, Stefan PEUKERT, Uwe SCHWAHN
  • Publication number: 20120196838
    Abstract: The invention relates to certain compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders and immune disorders.
    Type: Application
    Filed: January 25, 2012
    Publication date: August 2, 2012
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
  • Patent number: 8232271
    Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: October 30, 2009
    Date of Patent: July 31, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
  • Patent number: 8227617
    Abstract: A process for preparing a 2-hydroxy-4-substituted pyridine compound using a microbiological method, a novel microorganism, and a novel compound are provided.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: July 24, 2012
    Assignee: Yuki Gosei Kogyo Co., Ltd.
    Inventors: Mie Sasaki, Seiichiro Matsumoto
  • Patent number: 8227490
    Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: July 24, 2012
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
  • Publication number: 20120184749
    Abstract: The invention relates to a process for the production of radiotracers. In particular, this invention relates the isolation of radiotracers with containers filled with a stationary phase.
    Type: Application
    Filed: July 6, 2010
    Publication date: July 19, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Holger Siebeneicher, Keith Graham, Mathias Berndt
  • Patent number: 8211919
    Abstract: This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
    Type: Grant
    Filed: August 29, 2006
    Date of Patent: July 3, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Kouzo Sawada, Tatsuya Zenkoh, Takeshi Terasawa, Yoshimasa Imamura, Hiroki Fukudome, Satoru Kuroda, Jun Maeda, Junko Watanabe, Hiroshi Inami, Nobuaki Takeshita
  • Publication number: 20120142688
    Abstract: A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.
    Type: Application
    Filed: May 24, 2010
    Publication date: June 7, 2012
    Applicant: CENTRAL SOUTH UNIVERSITY
    Inventors: Gaoyun Hu, Lijian Tao, Jun Chen
  • Patent number: 8188291
    Abstract: The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: May 29, 2012
    Assignee: Sanofi-Aventis
    Inventors: Hartmut Strobel, Paulus Wohlfart, Heinz-Werner Kleemann, Gerhard Zoller, David William Will
  • Publication number: 20120129859
    Abstract: 1-(substituted benzyl)-5-trifluoromethyl-2(1H)pyridone compounds and their pharmaceutical acceptable salts are disclosed. The preparation methods of the compounds and their salts and the use of the same for preparing the medicaments for treating fibrosis are also disclosed. New pyridine compounds and their salts are obtained from trifluoromethyl pyridone as starting material.
    Type: Application
    Filed: May 24, 2010
    Publication date: May 24, 2012
    Inventors: Gaoyun Hu, Lijian Tao, Jun Chen
  • Patent number: 8183266
    Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: May 22, 2012
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Lawrence P. Wennogle, Peng Li, Jun Zhao
  • Patent number: 8173821
    Abstract: A serotonin and norepinephrine reuptake inhibitor of the formula: its uses, and methods for its preparation are described.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: May 8, 2012
    Assignee: Eli Lilly and Company
    Inventors: Nicolas Jacques Francois Dreyfus, Sandra Ann Filla, Anette Margareta Johansson, Thierry J. Masquelin, Jikesh Arvind Shah, Eric George Tromiczak, Magnus Wilhelm Walter
  • Patent number: 8173685
    Abstract: A compound of formula (I) or of formula (II) wherein X is oxygen or sulfur, and Y is a residue of pipecolic acid or a residue of an amino acid, preferably a naturally occurring amino acid.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: May 8, 2012
    Assignee: Nabriva Therapeutics AG
    Inventors: Klaus Thirring, Werner Heilmayer
  • Publication number: 20120108572
    Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
    Type: Application
    Filed: August 26, 2009
    Publication date: May 3, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
  • Publication number: 20120101105
    Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.
    Type: Application
    Filed: May 31, 2010
    Publication date: April 26, 2012
    Inventors: Tadashi Inoue, Shuzo Watanabe, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Kaoru Shimada
  • Patent number: 8158659
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: April 17, 2012
    Assignee: Theravance, Inc.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Publication number: 20120041033
    Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.
    Type: Application
    Filed: October 26, 2011
    Publication date: February 16, 2012
    Inventors: Julio A. Munoz, John Genus, James R. Moore
  • Publication number: 20120035175
    Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 9, 2012
    Applicant: 4SC AG
    Inventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
  • Patent number: 8110587
    Abstract: This invention relates to new aryl ureas and methods for their synthesis. The inventive compounds are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
    Type: Grant
    Filed: February 11, 2003
    Date of Patent: February 7, 2012
    Assignee: Bayer Healthcare LLC
    Inventors: Jacques Dumas, William J. Scott, Bernd Riedl, Du-Schieng Chien, Ala Nassar, Wendy Lee, Susan Bjorge, Laszlo Musza
  • Publication number: 20120029034
    Abstract: The present invention relates to calcium salts of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1, and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 2, 2012
    Applicant: 4SC AG
    Inventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
  • Publication number: 20120015943
    Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: July 18, 2011
    Publication date: January 19, 2012
    Applicant: Millennium Pharmacuticals, Inc.
    Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
  • Publication number: 20120004262
    Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.
    Type: Application
    Filed: January 21, 2010
    Publication date: January 5, 2012
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • Publication number: 20120004227
    Abstract: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)?(C(?O)N(R1), C(?O)N(R2)), (C(?O)N(R1), imidazole-1,3-diyl), (N(R1), C(?O)N(R2)), (O, C(?O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(?O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.
    Type: Application
    Filed: March 5, 2010
    Publication date: January 5, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Hiroshi Yoshida, Keisuke Tonogaki, Masahiro Sakagami, Kenji Takaya
  • Publication number: 20120003154
    Abstract: The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.
    Type: Application
    Filed: March 19, 2010
    Publication date: January 5, 2012
    Inventors: Harry John Wadsworth, William John Trigg
  • Publication number: 20110319449
    Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
    Type: Application
    Filed: March 9, 2010
    Publication date: December 29, 2011
    Inventors: Saleem Ahmad, William N. Washburn, Andres S. Hernandez, Jeffrey A. Robl, Khehyong Ngu, Zhenghua Wang
  • Publication number: 20110312911
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: February 3, 2010
    Publication date: December 22, 2011
    Inventors: Roman Kats-Kagan, Christian P. Stevenson, Xibin Liao, Qinghong Fu, Emma R. Parmee, Songnian Lin
  • Publication number: 20110306621
    Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT5A receptor modulating action. It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
    Type: Application
    Filed: February 8, 2010
    Publication date: December 15, 2011
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Nobuyuki Shiraishi, Yuichiro Kawamoto, Takuya Washio
  • Publication number: 20110306600
    Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.
    Type: Application
    Filed: June 10, 2011
    Publication date: December 15, 2011
    Applicant: Grunenthal GmbH
    Inventor: Ramesh SESHA