Benzene Ring In A Substituent E Patents (Class 564/92)
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Publication number: 20130018207Abstract: A compound having the formula (I) where each of R1, R2, R3 and R4 is independently C6-C18 aryl-, C5-C8 cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl s?bstituent, C4-C20 branched alkyl-, C16-C20 linear alkyl-, RO—, —NRR?, —PRR?, —SR, fluoro substituted forms thereof, and perfluoro forms thereof: and R5 is C6-C18 aryl-, C5-C8cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl substituent, C3-C20 branched alkyl-, C2-C30 linear alkyl-, fluoro substituted forms thereof, and perfluoro forms thereof; where R and R? are each independently C6-C18 aryl-, C5 -C8 cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl substituent, C4-C20 branched alkyl-, C2-C30 linear alkyl-, fluoro substituted forms thereof, and perfluoro forms thereof; A is N, P, S, or O with the proviso that when A is S, R2 is a nullity; and M isType: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: STEPHAN CONSULTING CORPORATIONInventors: Douglas W. Stephan, Preston A. Chase, Gregory C. Welch
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Patent number: 8350084Abstract: The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with ?-amyloid peptide.Type: GrantFiled: November 18, 2011Date of Patent: January 8, 2013Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Kevin W. Gillman, Richard E. Olson, Lawrence R. Marcin, Bang-Chi Chen, Huiping Zhang
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Publication number: 20120329877Abstract: The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R1 is H or C1-6alkyl and R2 is H, C1-6 alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and X is O or N; as well as tautomers and pharmaceutically acceptable salt forms thereof. Uses of these compounds are also described.Type: ApplicationFiled: June 6, 2012Publication date: December 27, 2012Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Onur Atasoylu, Carlo Ballatore, Kurt R. Brunden, Longchun Huang, Donna M. Huryn, Michael James, Virginia M.Y. Lee, Francesco Piscitelli, Amos B. Smith, III, James Soper, John Q. Trojanowski
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Patent number: 8314148Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: GrantFiled: May 11, 2012Date of Patent: November 20, 2012Assignee: Novartis AGInventors: Thomas Leutert, Jonathan E. Grob, Ruben Alberto Tommasi, Erin Keaney, Ayako Honda
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Publication number: 20120270902Abstract: The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3?, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).Type: ApplicationFiled: February 13, 2012Publication date: October 25, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Martin Neitzel, Jennifer Marugg
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Publication number: 20120220635Abstract: The present invention relates to aromatic compounds of the formula (I) and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.Type: ApplicationFiled: February 27, 2012Publication date: August 30, 2012Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
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Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
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Patent number: 8232427Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: GrantFiled: March 27, 2007Date of Patent: July 31, 2012Assignee: Novartis AGInventors: Thomas Leutert, Jonathan E Grob, Ruben Alberto Tommasi, Erin E. Pusateri, Ayako Honda
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Publication number: 20120178747Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: ApplicationFiled: November 14, 2006Publication date: July 12, 2012Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
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Patent number: 8207378Abstract: The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrien, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.Type: GrantFiled: April 24, 2009Date of Patent: June 26, 2012Assignee: The Medicines Company (Leipzig) GmbHInventors: Torsten Steinmetzer, Andrea Schweinitz, Joerg Stuerzebecher, Peter Steinmetzer, Anett Soeffing, Andreas Van De Locht, Silke Nicklisch, Claudia Reichelt, Friedrich-Alexander Ludwig, Alexander Schulze, Mohammed Daghisch, Jochen Heinicke
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Patent number: 8207167Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”).Type: GrantFiled: September 18, 2009Date of Patent: June 26, 2012Assignee: PIMCO 2664 LimitedInventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
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Publication number: 20120157487Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: December 9, 2011Publication date: June 21, 2012Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20120149909Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.Type: ApplicationFiled: December 21, 2011Publication date: June 14, 2012Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
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Publication number: 20120142917Abstract: Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl4. The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.Type: ApplicationFiled: September 6, 2011Publication date: June 7, 2012Applicants: H. Lee Moffitt Cancer Center and Research Institute, Inc., UNIVERSITY OF SOUTH FLORIDAInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Patent number: 8183293Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.Type: GrantFiled: December 18, 2008Date of Patent: May 22, 2012Assignee: Amgen Inc.Inventors: Mark Grillo, An-Rong Li, Jiwen Liu, Julio C. Medina, Yongli Su, Yingcai Wang, Janan Jona, Alan Allgeier, Jacqueline Milne, Jerry Murry, Joseph F. Payack, Thomas Storz
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Publication number: 20120123142Abstract: The present invention relates to a process for hydrogenating a substrate comprising a carbon-heteroatom double bond, the process comprising the step of reacting the substrate with hydrogen gas in the presence of a hydrogenation catalyst, wherein the hydrogenation catalyst is a complex of formula (I): R1-10, A and Hal are as defined in the specification. The present invention also provides processes for the preparation of the complex of formula (I) and intermediates thereof.Type: ApplicationFiled: March 17, 2010Publication date: May 17, 2012Applicant: JOHNSON MATTHEY PUBLIC LIMITED COMPANYInventors: Alan Dyke, Damian Mark Grainger, Jonathan Alan Medlock, Hans Guenter Nedden, Jacques Jean Marie Le Paih, Stephen James Roseblade, Andreas Seger, Vilvanathan Sivakumar, Antonio Zanotti-Gerosa
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Publication number: 20120108573Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula fare capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Inventors: Ursula SCHINDLER, Karl SCHÖNAFINGER, Hartmut STROBEL
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Publication number: 20120094971Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.Type: ApplicationFiled: September 3, 2009Publication date: April 19, 2012Applicant: REPLIGEN CORPORATIONInventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
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Publication number: 20120094964Abstract: The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.Type: ApplicationFiled: May 6, 2010Publication date: April 19, 2012Inventors: Tadashi Inoue, Masashi Ohmi, Kiyoshi Kawamura, Kazuo Ando, Yuji Shishido
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Publication number: 20120095024Abstract: The present invention provides novel compounds that inhibit cell proliferation 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. In a first aspect the present invention relates to a compound having a structure according to formula (I).Type: ApplicationFiled: December 30, 2009Publication date: April 19, 2012Applicants: Elara Pharmaceuticals GmbH, European Molecular Biology Laboratory (EMBL)Inventors: Jorge Alonson, Arantxa Encionas Lopez, Marcel Muelbaler, Lochen Ammenn, Bernd Vendt, Joe Lewis, Christoph Schultes, Bernd Janssen
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Publication number: 20120088925Abstract: The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with ?-amyloid peptide.Type: ApplicationFiled: November 18, 2011Publication date: April 12, 2012Inventors: John E. Starrett, JR., Kevin W. Gillman, Richard E. Olson, Lawrence R. Marcin, Bang-Chi Chen, Huiping Zhang
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Patent number: 8101799Abstract: This invention concerns N—(2-arylamino) aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: July 30, 2007Date of Patent: January 24, 2012Assignee: Ardea BiosciencesInventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoui, Zhi Hong
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Publication number: 20110313000Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Patent number: 8076376Abstract: Aniline sulfonamide derivatives according to formula I have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R1, R2, R3, R4, R5, R6, and L are set forth in the description.Type: GrantFiled: July 21, 2006Date of Patent: December 13, 2011Inventors: Jay P. Powers, Xiao He, Dustin McMinn, Yosup Rew, Daqing Sun
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Publication number: 20110275635Abstract: Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors.Type: ApplicationFiled: January 8, 2010Publication date: November 10, 2011Applicant: THE UAB RESEARCH FOUNDATIONInventors: Wayne J. Brouillette, Christie G. Brouillette, Whitney B. Moro
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Patent number: 8039493Abstract: The invention is concerned with novel biaryl sulfonamide derivatives of formula (I) wherein R1 to R3 and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: September 17, 2008Date of Patent: October 18, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Ulrike Obst Sander, Tanja Schulz-Gasch, Matthew Wright
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Patent number: 8030517Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: December 3, 2009Date of Patent: October 4, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
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Publication number: 20110190302Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”).Type: ApplicationFiled: September 18, 2009Publication date: August 4, 2011Applicant: PIMCO 2664 LIMITEDInventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
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Patent number: 7973197Abstract: The present invention provides (I) a method of manufacturing a triphenylmethane colorant that can suppress the sub-reactions in conversion to a sulfonamide and is industrially advantageous, (II) a colorant compound that has both excellent spectral characteristics and a high solubility relative to organic solvents or polymers as a coloring agent to be used in color filters and (III) a blue resist composition for use in a color filter that shows a high lightness and an excellent hue particularly for blue color and can be used to display an image that is excellent in terms of spectral characteristics and contrast.Type: GrantFiled: August 19, 2010Date of Patent: July 5, 2011Assignee: Canon Kabushiki KaishaInventors: Yasuaki Murai, Takayuki Toyoda, Yuko Yamagishi, Takeshi Miyazaki
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Patent number: 7968534Abstract: The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R1 and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.Type: GrantFiled: July 21, 2008Date of Patent: June 28, 2011Assignee: Sanofi-AventisInventors: Pierre Despeyroux, Evelyne Fontaine, Gilles Courtemanche, Pierrick Rochard, Claudine Serradeil-Le Gal
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Publication number: 20110136877Abstract: The present invention provides novel phenoxyacetic acids useful for the prevention and treatment of inflammatory disorders, including those affecting the respiratory system and skin.Type: ApplicationFiled: January 6, 2009Publication date: June 9, 2011Applicant: LIGAND PHARMACEUTICALS INC.Inventors: Brian F. McGuinness, Thuy X. H. Le, Jingqi Duo, Koc-Kan Ho
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Publication number: 20110136735Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 30, 2010Publication date: June 9, 2011Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
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Publication number: 20110118248Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: January 13, 2009Publication date: May 19, 2011Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
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Publication number: 20110105485Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: July 21, 2010Publication date: May 5, 2011Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
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Patent number: 7932252Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: GrantFiled: May 12, 2005Date of Patent: April 26, 2011Assignee: ChemoCentryx, Inc.Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
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Publication number: 20110077305Abstract: The use of compounds of the formula (I) Ar1-L1-Ar2-L2-C(R3)(R4)N(OR1)C(?Y)—R2 (I) where Y is selected from O or S; R1 is H, a salt or readily hydrolysable substituent; R2 is selected from H or CH3, CH2F, CF2H or CF3; R3 and R4 are selected independently from H, C 1-4 alkyl or alkenyl, CF3, CH2F, CF2H and F, with the proviso that if either R3 or R4 is H, then the other is not H; L1 is a linker group; L2 is a linker group comprising an optionally substituted or unsubstituted unsaturated branched or straight chain alkyl group; Ar1 is an optionally substituted or unsubstituted aryl or heterocyclic group; and Ar2 is an optionally substituted or unsubstituted aryl or heterocyclic group, in the treatment of 5-lipoxygenase mediated cancer provide improved therapies due to the effective inhibition of 5-lipoxygenase and long duration of activity in vivo after oral administration.Type: ApplicationFiled: June 1, 2009Publication date: March 31, 2011Inventor: William Paul Jackson
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Publication number: 20110065760Abstract: The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y.Type: ApplicationFiled: November 23, 2009Publication date: March 17, 2011Applicant: Jerini AGInventors: Jochen KNOLLE, Mike Schutkowski, Gerd Hummel, Thomas Tradler, Laurence Jobron, Claudia Christner, Dirk Scharn, Roland Stragies, Christoph Gibson, Frank Osterkamp
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Publication number: 20110065799Abstract: The invention relates to novel inhibitors of urokinase and to their preparation and use for the therapy, prophylaxis and diagnosis of a tumor, in particular for reducing the formation of tumor metastases.Type: ApplicationFiled: November 22, 2010Publication date: March 17, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz
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Publication number: 20110065631Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.Type: ApplicationFiled: March 29, 2007Publication date: March 17, 2011Applicant: Gilead Sciences, IncInventors: Kenneth R. Crawford, Eric D. Dowdy, Arnold Gutierrez, Richard Polniaszek, Richard H. Yu
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Publication number: 20110059940Abstract: The disclosure provides compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their uses in inhibiting ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: May 7, 2009Publication date: March 10, 2011Inventors: Paul J. Gilligan, Michael G. Yang, Jianliang Shi
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Publication number: 20110028509Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.Type: ApplicationFiled: April 8, 2009Publication date: February 3, 2011Applicant: MERCK SERONO SAInventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
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Publication number: 20100298308Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: ApplicationFiled: November 14, 2006Publication date: November 25, 2010Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
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Publication number: 20100286266Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as ‘BPSAAA compounds’), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds.Type: ApplicationFiled: March 20, 2008Publication date: November 11, 2010Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEENInventors: Iain Robert Greig, Robert Jurgen Van't Hof, Stuart Hamilton Ralston
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Publication number: 20100280074Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: December 3, 2009Publication date: November 4, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20100273739Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: February 16, 2010Publication date: October 28, 2010Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
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Patent number: 7820717Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: October 16, 2008Date of Patent: October 26, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Shaowu Chen
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Patent number: 7816397Abstract: The invention relates to compounds of general formula (1): in which R1, R2, R3, R4, R5, A, B, D and E are as defined in Claim 1, and also to the preparation process therefor and the therapeutic use thereof. These compounds can be used in the treatment of pathologies associated with hyperglycaemia.Type: GrantFiled: June 1, 2005Date of Patent: October 19, 2010Assignee: Merck Patent GmbHInventors: Gérard Moinet, Gérard Botton, Micheline Kergoat
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Publication number: 20100261788Abstract: Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.Type: ApplicationFiled: June 22, 2010Publication date: October 14, 2010Inventors: John C. Reed, Maurizio Pellecchia
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Publication number: 20100234364Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 10, 2007Publication date: September 16, 2010Inventors: Arindrajit Basak, Jeff Jin, Jimmie Moore, Andrew M.K. Pennell, Sreenlvas Punna, Solomon Ungashe, Zheng Wei
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Publication number: 20100227902Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.Type: ApplicationFiled: May 14, 2010Publication date: September 9, 2010Applicant: CHEMOCENTRYX, INC.Inventors: Solomon Ungashe, Zheng Wei, J. J. Wright, Andrew Pennell, Brett Permack, Thomas Schall