Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Acyclic Nitrogen Patents (Class 546/265)
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Publication number: 20120157462Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.Type: ApplicationFiled: January 30, 2008Publication date: June 21, 2012Inventors: Alan T. Johnson, Guan-Sheng Jiao
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Patent number: 8183239Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.Type: GrantFiled: October 27, 2006Date of Patent: May 22, 2012Assignee: Janssen Pharmaceutica NVInventors: Pascal Bonaventure, Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Mark Seierstad, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Publication number: 20120115827Abstract: The present invention relates to a novel 3-aminobenzamide, compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide, compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such as pain, acute pain, chronic pain, neuropathicpain, rheumatoid arthritis pain, and neuralgia.Type: ApplicationFiled: June 7, 2011Publication date: May 10, 2012Applicant: Japan Tobacco Inc.Inventors: Yoshihisa Koga, Shinji Yata, Takashi Watanabe, Takuya Matsuo, Masahiro Sakata, Wataru Kondo
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Publication number: 20120064121Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Shoujun Chen
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Publication number: 20120004381Abstract: A method of preparing polymer, the method comprising polymerising one or more ethylenically unsaturated monomers of formula (I) where U is selected from H, C1-C4 alkyl or halogen; V is halogen or of the form O-G where G is selected from —C(O)R1 and —R1, or V is of the form NGGa where G is as defined above and Ga is selected from H and R1, G and Ga form together with N a heterocyclic ring, or V is of the form CH2Gb where Gb is selected from H, R1, OH, OR1, NR12, PR12, P(O)R12, P(OR1)2, SR1, SOR1, and SO2R1; and where the or each R1 is independently selected from optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted alkylaryl, optionally substituted alkylheteroaryl, and an optionally substituted polymer chain, under the control of a RAType: ApplicationFiled: January 22, 2010Publication date: January 5, 2012Applicant: COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATIONInventors: Ezio Rizzardo, John Chiefari, Massimo Benaglia, San Thang, Graeme Moad
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Publication number: 20110312875Abstract: The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.Type: ApplicationFiled: August 2, 2011Publication date: December 22, 2011Applicant: UNIVERSITY OF WOLLONGONGInventors: Timothy Patrick Boyle, John Barnard Bremner, Zinka Brkic, Jonathan Alan Victor Coates, Neal Kevin Dalton, John Deadman, Paul Anthony Keller, Jody Morgan, Stephen Geoffrey Pyne, David Ian Rhodes, Mark James Robertson
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Publication number: 20110312974Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds 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: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Nicholas Simone Stock, Yen Pham Truong, Jeffrey Roger Roppe, Deborah Volkots, Jill Melissa Scott, Timothy Andrew Parr, Bowei Wang, Thomas Jon Seiders, Ryan Clark, Heather Renee Coate
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Publication number: 20110305729Abstract: Compounds of the invention are of the formula (I); wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.Type: ApplicationFiled: January 26, 2010Publication date: December 15, 2011Inventors: Stephen Joseph Shuttleworth, Cyrille Davy Tomassi
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Publication number: 20110275674Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.Type: ApplicationFiled: November 5, 2009Publication date: November 10, 2011Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos A. Petasis
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Publication number: 20110269966Abstract: An amic acid or amic ester precursor can be applied to a substrate and thermally converted into a thin organic semiconducting layer of the corresponding arylene diimide. This semiconducting layer can be used in various semiconductive articles such as organic light emitting diode (OLED), photodetector, sensor, logic circuit, memory element, capacitor, photovoltaic (PV) cell, or electronic devices. In this manner, the arylene diimide need not be coated but is generated in situ from a solvent-soluble and easily coated precursor compound.Type: ApplicationFiled: April 30, 2010Publication date: November 3, 2011Inventors: Deepak Shukla, Dianne M. Meyer, Wendy G. Ahearn
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Publication number: 20110269967Abstract: Novel amic acids and amic esters can be thermally converted into corresponding arylene diimides. These amic acids and amic ester can be used as precursors to prepare semiconducting thin films that can be used in various articles including thin-film transistor devices that can be incorporated into a variety of electronic devices. In this manner, the arylene diimides need not be coated out of solvent in which they may be insoluble, but they can be generated in situ from a solvent-soluble, easily coated amic acid or amic ester.Type: ApplicationFiled: April 30, 2010Publication date: November 3, 2011Inventors: Deepak Shukla, Dianne M. Meyer, Wendy G. Ahearn
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Publication number: 20110237573Abstract: The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.Type: ApplicationFiled: March 1, 2010Publication date: September 29, 2011Applicant: IRM LLCInventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
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Publication number: 20110237578Abstract: Compounds are provided according to formula (I), where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: ApplicationFiled: September 14, 2009Publication date: September 29, 2011Inventors: Zhi-Liang Wei, Sumithra Gowlugari, Carl Kaub, Zhan Wang, Yeyu Cao, John Kincaid
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Publication number: 20110224225Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Publication number: 20110166132Abstract: The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: December 12, 2008Publication date: July 7, 2011Applicant: Amgen Inc.Inventors: Stephen A. Hitchcock, Jian J. Chen, Mqhele Vellah Ncube, Thomas Nixey, Albert Amegadzie, Roxanne Kunz, Wenyan Qian, Ning Chen, Christopher M. Tegley, Frenel F. De Morin, Chester Chenguang Yuan, Qingyian Liu, Jiawang Zhu, Tanya A.N. Peterkin, Jeffrey A. Adams, Essa Hu, Frank Chavez, JR.
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Patent number: 7973037Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: April 8, 2008Date of Patent: July 5, 2011Assignees: Axys Pharmaceuticals, Inc., Merck Canada Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
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Patent number: 7973059Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: October 17, 2006Date of Patent: July 5, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Wolkenberg, Mark T. Bilodeau, M. Brad Nolt
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Publication number: 20110152323Abstract: The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation.Type: ApplicationFiled: June 9, 2009Publication date: June 23, 2011Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jianqi Li, Juan Feng, Wangping Cai
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Publication number: 20110118234Abstract: The present invention provides compounds Formula (I) that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: May 4, 2009Publication date: May 19, 2011Inventors: Kaustav Biswas, Jian J. Chen, James R. Falsey, Vijay Keshav Gore, Qingyian Liu, Vu Van Ma, Stephanie J. Mercede, Robert M. Rzasa, Christopher M. Tegley, Jiawang Zhu
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Publication number: 20110077160Abstract: Compounds having the following generic formula are disclosed.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Inventors: Nneka T. Breaux, Michael R. Loso, Timothy C. Johnson, Jonathan M. Babcock, Benjamin M. Nugent, Timothy P. Martin, Annette V. Brown, Ronald Ross, JR., William C. Lo, Matthias S. Ober
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Publication number: 20110064657Abstract: The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.Type: ApplicationFiled: June 26, 2008Publication date: March 17, 2011Applicant: The Johns Hopkins UniversityInventors: Martin Gilbert Pomper, Ray Sangeeta, Ronnie C. Mease, Catherine Foss
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Patent number: 7901559Abstract: It is intended to provide a method for easily detecting a phosphorylated peptide (protein) in a test sample by using SDS-polyacrylamide gel electrophoresis (SDS-PAGE) which has been conventionally employed in analyzing a protein; a polyacrylamide gel for electrophoresis to be used in the method; a method of producing the gel; and a synthesizing intermediate in producing the gel. The polyacrylamide gel for electrophoresis to be used in the method of the invention is characterized in that at least a part of the structure thereof has a structure represented by the following formula (I); wherein M2+represents a transition metal ion; and X represents a linker group.Type: GrantFiled: August 1, 2005Date of Patent: March 8, 2011Assignee: Nard Institute, Ltd.Inventors: Tohru Koike, Akihiko Kawasaki, Tatsuhiro Kobashi
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Patent number: 7879839Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 27, 2005Date of Patent: February 1, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Douglas C. Beshore, B. Wesley Trotter, Kausik K. Nanda, Richard Isaacs, Linda S. Payne, Lou Anne Neilson, Zhicai Wu, Mark T. Bilodeau, Peter J. Manley, Adrienne E. Balitza
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Publication number: 20110003859Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: February 27, 2009Publication date: January 6, 2011Applicant: Array Biopharma Inc.Inventor: Kateri A. Ahrendt
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Publication number: 20100331549Abstract: There is described compounds of Formulæ I, II, III, IV and V. The compounds of Formulæ I, II, III, IV and/or V are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.Type: ApplicationFiled: August 26, 2010Publication date: December 30, 2010Inventors: Chaim Roifman, Peter Demin, Olga Rounova, Tom Grunberger
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Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Publication number: 20100324092Abstract: The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Richard W. Heidebrecht, JR., Thomas A. Miller, Matthew G. Stanton, David J. Witter
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Patent number: 7829584Abstract: The present invention describes compounds of Formula I: wherein W, X, Y, Z, and Q are defined herein, or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal.Type: GrantFiled: March 13, 2007Date of Patent: November 9, 2010Assignee: Janssen Pharmaceutica NVInventors: Mark R. Player, Tianbao Lu, Huaping Hu, Xizhen Zhu, Christopher Teleha, Kevin Kreutter
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Publication number: 20100266714Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: October 29, 2008Publication date: October 21, 2010Inventors: Christopher S Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Patent number: 7812025Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whicType: GrantFiled: August 11, 2006Date of Patent: October 12, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Matsumoto, Masakuni Kori, Mitsunori Kouno
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Patent number: 7803946Abstract: Disclosed herein is a class of tunable phenylacetylene compounds as well as compositions and methods for their use as host compounds for ligand binding. In certain examples the hosts report binding events by exhibiting altered spectroscopic properties, such as different fluorescent emission spectra.Type: GrantFiled: December 14, 2007Date of Patent: September 28, 2010Inventors: Michael M. Haley, Darren W. Johnson, Orion B. Berryman, Charles A. Johnson, Calden N. Stimpson
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Patent number: 7799807Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R1, R2, R3, m, and n are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.Type: GrantFiled: March 20, 2006Date of Patent: September 21, 2010Assignee: Purdue Pharma L.P.Inventor: Qun Sun
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Patent number: 7772254Abstract: 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: GrantFiled: March 21, 2006Date of Patent: August 10, 2010Assignee: Purdue Pharma L.P.Inventor: Qun Sun
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Publication number: 20100190788Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 11, 2006Publication date: July 29, 2010Inventors: Olivier Defert, Philippe Van Rompaey, Petra Blom, Dirk Leysen, Gert De Wilde, Thomas Brown
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Publication number: 20100178247Abstract: A compound that recognizes and binds to the CA-IX protein has Formula I, II, III, or IV. The compounds may include a radioactive element for radioimaging or therapeutic applications. Thus, pharmaceutical compositions may be prepared with one or more of the compounds of Formula I, II, III, or IV.Type: ApplicationFiled: December 4, 2009Publication date: July 15, 2010Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Publication number: 20100178246Abstract: A compound of Formula I, a pharmaceutically acceptable salt, or solvate thereof: complexes with metals such as rhenium, technetium, and others to provide a complex for imaging tissues or treating disease, particularly where the metal is radioactive. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.Type: ApplicationFiled: December 4, 2009Publication date: July 15, 2010Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Publication number: 20100168070Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Inventors: Niklas Heine, Klaus Fuchs, Christian Eickmeier, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Publication number: 20100099881Abstract: An object of the invention is to provide a novel sphingosine compound with an inhibitory activity against sphingomyelinase, and a method for producing the sphingosine compound. The novel sphingosine compound or a salt thereof according to the invention is represented by Formula (1): wherein one of R1 and R2 is hydrogen, and the other is a group represented by Formula (G): wherein n is 0 or 1; and R3 is hydrogen, C1-23 alkyl, C3-8 cycloalkyl, C2-6 alkenyl, C1-6 alkoxy, C3-8 cycloalkyloxy, phenyl, or furil.Type: ApplicationFiled: March 5, 2008Publication date: April 22, 2010Applicant: OTSUKA CHEMICAL CO., LTD.Inventors: Mugio Nishizawa, Hiroshi Imagawa, Jun Sakurai, Masataka Oda
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Publication number: 20100081673Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: September 28, 2009Publication date: April 1, 2010Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard HUTCHINSON, Nicholas Simon STOCK, Jeffrey Roger ROPPE, Jill Melissa SCOTT, Brian Andrew STEARNS, Yen Pham TRUONG, Deborah VOLKOTS, Timothy PARR
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Publication number: 20100062937Abstract: Benzanilides of the formula: in which X represents hydrogen, halogen, nitro, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl or C1-6 alkylsulfonyloxy; Y represents halogen or C1-6 alkyl; R1 represents C1-6 alkyl, C1-6 alkylthio C1-6 alkyl, C1-6 alkylsulfinyl-C1-6 alkyl or C1-6 alkylsulfonyl-C1-6 alkyl; R2 represents hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 represents hydrogen or hydroxy; W represents CH or N; and Q represents optionally substituted phenyl or optionally substituted pyridyl wherein the substituent is at least one group selected from the group consisting of halogen, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl and C1-6 haloalkylsulfoxy; provided that when R3 is hydroxy, R2 is not C1-6 alkyl, or when R2 is C1-6 haloalkyl, R3 is hydroxy, W is CH, and the substituents of Q are two or more C1-6 haloalkyl. Insecticides comprising the benzanilides are herein provided.Type: ApplicationFiled: June 2, 2006Publication date: March 11, 2010Applicant: BAYER CROPSCIENCE AGInventors: Katsuaki Wada, Tetsuya Murata, Katsuhiko Shibuya, Eiichi Shimojo
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Publication number: 20100000028Abstract: Disclosed are styryl sulfide dyes of formula (1), wherein R1, R?1, R2, R?2, R3 and R?3, independently from each other are hydrogen; C1-C20alkyl or C1-C20alkoxy, which may be substituted by one or more C1-C5alkoxy, halogen, —NH2, mono-C1-C5alkylamino, di-C1-C5alkylamino, —NO2 or hydroxy; C3-C6cycloalkyl; —C(O)H; —C(O)—C1-C5alkyl; halogen; NO2; OH; phenyl, which may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, halogen, —NH2, mono-C1-C5alkylamino, di-C1-C5alkylamino, —NO2 or hydroxy; or a radical of formula —NR4R5, wherein R4 and R5 independently from each other are hydrogen; C1-C12alkyl, which may be substituted by one or more C1-C5alkyl, C1-C5-alkoxy, hydroxy or —(CO)—H; —(CO)—C1-C5alkyl; phenyl or phenyl-C1-C4alkyl, wherein the phenyl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, halogen, —N2, mono-C1-C5alkylamino, di-C1-C5alkylamino, —NO2, carboxy or hydroxy; W1, W?1, W2, W?2, W3, W?3, W4 or W?4, independently from each other are —CH— or —N+—; wherein only one of W1/W?1, W2/W?2,Type: ApplicationFiled: June 7, 2006Publication date: January 7, 2010Inventors: Victor Paul Eliu, Beate Fröhling, Dominique Kauffmann
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Publication number: 20090312314Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists that may be useful in the treatment of disorders, in which orexin pathways are involved.Type: ApplicationFiled: June 10, 2009Publication date: December 17, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20090275550Abstract: 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: ApplicationFiled: April 11, 2007Publication date: November 5, 2009Inventors: James C. Barrow, Kelly-Ann S. Bieber, Rowena V. Cube, Mamio Christa Mattern, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
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Patent number: 7598242Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.Type: GrantFiled: October 20, 2005Date of Patent: October 6, 2009Assignee: Schering CorporationInventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
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Publication number: 20090172897Abstract: The disclosure relates to the dyeing of keratin materials using styryl hydroxy(cyclo)alkylamino thiol/disulfide fluorescent dyes. Disclosed herein is a dye composition comprising a styryl hydroxy(cyclo)alkylamino thiol/disulfide fluorescent dye and a dyeing process with, for example, a lightening effect on keratin materials such as hair, using said composition. Disclosed herein are novel thiol/disulfide fluorescent dyes and the uses thereof in lightening keratin materials. This composition makes it possible to obtain a lightening effect which can be resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: July 9, 2009Inventors: Nicolas DAUBRESSE, Andrew GREAVES, Franco MANFRE
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Publication number: 20090042867Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1 to R13, A, B, L, and i are defined as indicated in the description and the claims, as well as the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: February 12, 2009Inventors: Klaus Fuchs, Christian Eickmeier, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Publication number: 20090030042Abstract: A method of making a compound of formula II comprising the reaction of a compound of formula RCONH2 with a compound of formula III R being a moiety having between 1 and 15 carbon atoms and optionally from 1 to 5 heteroatoms independently selected from oxygen, nitrogen and sulfur, and X and Y being independently selected front the group consisting of H, methyl, ethyl, OMe, OEt, and mixtures thereof; the reaction being performed in a solvent in the presence of a base. The method is useful for the inexpensive manufacture of certain commercially-valuable compounds, including some that have desirable cooling properties.Type: ApplicationFiled: July 15, 2008Publication date: January 29, 2009Applicant: Givaudan, SA.Inventors: Stefan Michael Furrer, David C. Bom, David Max Dastrup, Ioana Maria Ungureanu
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Publication number: 20090018141Abstract: Provided herein are Compounds having the following structure: wherein A, L, X and ring B are as defined herein, compositions comprising an effective amount of a Compound and methods for treating or preventing cancer, hypoxia, diabetes, stroke, autoimmune disease or a condition treatable or preventable by inhibition of Chk2, the ATM-Chk2 pathway or RSK2 comprising administering an effective amount of a Compound to a patient in need thereof.Type: ApplicationFiled: June 9, 2008Publication date: January 15, 2009Inventors: Robert Shoemaker, John Cardellina, Michael Currens, Sudhir Kondapaka, Yves Pommier, Andy Jobson, Dominic Scudiero, David Waugh, George Lountos, Charles M. Cook, Guangtao Zhang, Andrew Colasanti, Christopher R. Self, Janet Cicariello Cook
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Publication number: 20080242702Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.Type: ApplicationFiled: March 20, 2008Publication date: October 2, 2008Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono, Zhi-Qiang Xia