1,2,4-oxadiazoles (including Hydrogenated) Patents (Class 548/131)
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Patent number: 8148410Abstract: The invention relates to novel thiophene derivatives (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I).Type: GrantFiled: December 9, 2008Date of Patent: April 3, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
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Publication number: 20120077854Abstract: The present invention relates to compositions and methods for modulating retinol binding to retinol binding protein 4 (RBP4). In particular, the present invention provides compounds having Formula (1) or (2) (Formulae (1), (2)); wherein R1, R2, R3, R4, R5, R6, Y1, Y2, Y3, Y4 and m are as defined above.Type: ApplicationFiled: April 13, 2010Publication date: March 29, 2012Inventors: Hank Michael James Petrassi, David C. Tully, Brian T. Masick, Bao Nguyen
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Publication number: 20120077975Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.Type: ApplicationFiled: December 1, 2011Publication date: March 29, 2012Inventors: Jeffrey Lyle Gray, Kande K. D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
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Publication number: 20120071460Abstract: The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R1, R2 and R3 are as defined in the description.Type: ApplicationFiled: June 7, 2010Publication date: March 22, 2012Applicant: MERCK SERONO SAInventors: Anna Quattropani, Charles Baker-Glenn, Wesley Blackaby, Chris Knight
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Publication number: 20120064181Abstract: 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: March 15, 2010Publication date: March 15, 2012Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem Nguyen, Daniel V. Paone, Craig M. Potteiger, Shaun R. Stauffer, Carolyn Segerdell, Ashley Nomland, John J. Lim
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Patent number: 8133910Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: GrantFiled: July 10, 2007Date of Patent: March 13, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
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Patent number: 8129540Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.Type: GrantFiled: January 21, 2010Date of Patent: March 6, 2012Assignee: PTC Therapeutics, Inc.Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
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Publication number: 20120053150Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.Type: ApplicationFiled: April 22, 2010Publication date: March 1, 2012Inventors: David George Allen, Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Steven Leslie Sollis, Sadie Vile, Caroline Wilson
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Publication number: 20120053210Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2011Publication date: March 1, 2012Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20120046273Abstract: Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.Type: ApplicationFiled: March 5, 2010Publication date: February 23, 2012Applicant: MITHRIDION, INC.Inventors: Trevor M. Twose, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson, Michael L. Hendrickson, Jeffrey C. Ockuly, Melinda L. Verdone
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Publication number: 20120034270Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.Type: ApplicationFiled: October 16, 2009Publication date: February 9, 2012Applicant: Akaal Pharma Pty LtdInventors: Damian W. Grobelny, Gurmit S. Gill
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Publication number: 20120035226Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: ApplicationFiled: March 29, 2010Publication date: February 9, 2012Applicant: MERCK SERONO SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnés Bombrun
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Publication number: 20120028950Abstract: The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: May 9, 2011Publication date: February 2, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael HÄRTER, Hartmut BECK, Susanne GRESCHAT, Peter ELLINGHAUS, Kerstin BERHÖRSTER, Joachim SCHUHMACHER
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Publication number: 20120027777Abstract: The present invention relates to a Ljungan virus with improved replication characteristic and the use of this Ljungan virus, amongst other thing, in the production of a vaccine.Type: ApplicationFiled: January 22, 2010Publication date: February 2, 2012Applicant: APODEMUS ABInventors: Michael Lindberg, Conny Tolf
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Publication number: 20120022109Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: ApplicationFiled: March 29, 2010Publication date: January 26, 2012Applicant: MERCK SERONO SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnès Bombrun
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Publication number: 20120022119Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. 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: ApplicationFiled: November 16, 2009Publication date: January 26, 2012Applicant: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Brian Andrew Stearns, Timothy Parr
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Publication number: 20120022083Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.Type: ApplicationFiled: February 9, 2011Publication date: January 26, 2012Applicant: ADHEREX TECHNOLOGIES, INC.Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
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Patent number: 8101775Abstract: The invention relates to compounds of formula (I) wherein one of R5 and R6 is hydrogen or R2 and the other is (a) pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the S1P1 receptor.Type: GrantFiled: December 19, 2007Date of Patent: January 24, 2012Assignee: Glaxo Group LimitedInventors: Mahmood Ahmed, James Myatt, David Norton, Dean Andrew Rivers
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Patent number: 8101641Abstract: Novel hydroxylated 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising a hydroxylated 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.Type: GrantFiled: September 24, 2007Date of Patent: January 24, 2012Assignee: PTC Therapeutics, Inc.Inventors: Neil G. Almstead, Peter Seongwoo Hwang, Young-Choon Moon, Ellen M. Welch
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Publication number: 20120015988Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: May 4, 2009Publication date: January 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Renee M. Zindell, Patricia Amouzegh, Monika Ermann, Christopher Francis Palmer, Mark Whittaker
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Publication number: 20120010219Abstract: The invention features salvinorin compositions that are selective for kappa opioid receptors; methods of treating mania by using a selective kappa receptor agonist; and methods of treating mood disorders, such as depressive disorders and manic disorders, using salvinorin compositions.Type: ApplicationFiled: December 14, 2009Publication date: January 12, 2012Applicant: The McLean Hospital CorporationInventors: Cecile Beguin, Justin Stephen Potuzak, Thomas Anthony Munro, Katherine K. Duncan, William A. Carlezon, Bruce M. Cohen, Lee-yuan Liu Chen
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Publication number: 20120010200Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20120004198Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: ApplicationFiled: February 2, 2011Publication date: January 5, 2012Applicant: ARGUSINA INC.Inventors: Jiayu LIAO, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Patent number: 8088791Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)— or ?N—; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2—, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(?O)—, —O—(C?O)—, —C(?O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—; and Q is hydrogen, halogen, nitType: GrantFiled: March 22, 2007Date of Patent: January 3, 2012Assignee: Biots Scientific Management Pty LtdInventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
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Publication number: 20110318388Abstract: The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response.Type: ApplicationFiled: October 19, 2009Publication date: December 29, 2011Applicant: Akaal Pharma Pty LtdInventors: Gurmit S. Gill, Damian W. Grobelny
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Patent number: 8084618Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: GrantFiled: January 8, 2010Date of Patent: December 27, 2011Assignee: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Patent number: 8084452Abstract: The present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: GrantFiled: March 19, 2007Date of Patent: December 27, 2011Assignee: Bayer Cropscience AGInventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Olga Malsam, Ralf Nauen, Thomas Müller, Christian Arnold, Erich Sanwald, Ulrich Görgens
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Patent number: 8084477Abstract: 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: October 10, 2008Date of Patent: December 27, 2011Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Kevin W. Gillman, Richard E. Olson
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Publication number: 20110312930Abstract: The present application relates to novel aryl compounds with aminoalkyl substituents, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 31, 2009Publication date: December 22, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Berhörster, Susanne Greschat, Karl-Heinz Thierauch
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Publication number: 20110311459Abstract: The present invention relates to alkaloid aminoester compounds which act as muscarinic receptor antagonists, processes for the preparation of such a compound, compositions which contain such a compound, and therapeutic uses of such a compound.Type: ApplicationFiled: June 22, 2011Publication date: December 22, 2011Applicant: Chiesi Farmaceutici S.p.A.Inventors: Gabriele AMARI, Mauro RICCABONI
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Publication number: 20110311485Abstract: The present disclosure relates to 1, 2, 4 oxadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.Type: ApplicationFiled: December 15, 2009Publication date: December 22, 2011Applicant: ALMIRALL S.A.Inventors: Victor Giulio Matassa, Nuria Aguilar Izquierdo, Marta Mir Cepeda, Marta Carrascal Riera, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Julio Cesar Castro Palomino Laria, Montserrat Erra Sola
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Publication number: 20110301122Abstract: The present application relates to novel substituted aryl compounds, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 31, 2009Publication date: December 8, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Berhörster, Susanne Greschat, Karl-Heinz Thierauch, Frank Süssmeier
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Publication number: 20110301203Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: August 19, 2011Publication date: December 8, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Philip Stewart Turnbull, Rodolfo Cadilla, Andrew Larkin, Huiquiang Zhou, Eugene L. Stewart, Katherine Stetson, Darryl Lynn McDougald, Amarjit Sab Randhawa, John A. Ray
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Publication number: 20110300165Abstract: Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein Q is R1 is alkyl or aryl, said aryl optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: January 22, 2010Publication date: December 8, 2011Applicant: The Board of TRustees of the University of Illinoi University of IlliniosInventors: Scott Hunter Watterson, Alaric J. Dyckman, William J. Pitts, Steven H. Spergel
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Publication number: 20110300149Abstract: The present invention relates to a new group of Ljungan viruses, proteins expressed by the viruses, antibodies to the viruses and proteins, vaccines against the viruses, diagnostic kits for detecting the viruses, uses of the viruses, proteins, antibodies and vaccines in therapy, uses of the viruses, proteins, antibodies and vaccines in treating diseases caused by the viruses and methods of treatment for treating diseases caused by the viruses.Type: ApplicationFiled: December 23, 2009Publication date: December 8, 2011Applicant: Apodemus ABInventors: Bo Niklasson, Conny Tolf, Michael Lindberg
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Publication number: 20110301150Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.Type: ApplicationFiled: February 25, 2010Publication date: December 8, 2011Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
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Patent number: 8071593Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: May 8, 2008Date of Patent: December 6, 2011Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20110294856Abstract: This invention relates to novel oxadiazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: July 29, 2011Publication date: December 1, 2011Inventors: Bjarne H. DAHL, Dan PETERS, Gunnar M. OLSEN, Daniel B. TIMMERMANN, Susanne JØRGENSEN
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20110293520Abstract: The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R1)(R2)—, —C(R3)?, —N(R4)—, —N?, —N+(R5)?, —O— and —S—; M and Z are independently nondirectionally selected from formula (I) and formula (II).Type: ApplicationFiled: June 9, 2009Publication date: December 1, 2011Inventors: Armin Giese, Uwe Bertsch, Hans Kretzschmar, Mathias Habeck, Thomas Hirschberger, Paul Tavan, Christian Griesinger, Andrei Leonov, Sergey Ryazanov, Petra Weber, Markus Geissen, Martin H. Groschup, Jens Wagner
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Patent number: 8063034Abstract: The present invention relates to Compounds represented by the formula (I) or salts thereof. In the formula (I), the ring A represents a benzene ring, a thiophene ring, or a pyridine ring; Ra represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group; the ring B represents a pyridine ring, a pyrimidine ring, or a quinoline ring; the ring C represents a benzene ring; a pyridine ring, a quinoline ring, or an isoquinoline ring; X and Y, the same or different, represent an oxygen atom or a sulfur atom, with the proviso that the case X is a sulfur atom and Y is an oxygen atom be excluded; R1 represents a hydrogen atom, a halogen atom, an amino group, a cycloalkylamino group, an alkylcarbonylamino group, an alkyloxycarbonylamino group, an alkylaminocarbonyl group, or a non-aromatic heterocyclic group; and R2 and R2?, the same or different, represent a hydrogen atom, a halogen atom, an alkyl group, a halogeno-alkyl group, or a halogeno-alkoxy group.Type: GrantFiled: January 29, 2008Date of Patent: November 22, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Takahiro Honda, Koushi Fujisawa, Hiroyuki Aono, Masakazu Ban
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Publication number: 20110281881Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: February 2, 2010Publication date: November 17, 2011Inventors: Henricus, Jacobus, Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, Francois Paul Bischoff, Tongfei Wu, Sven, Franciscus, Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge, Maria, Aloysius Pieters, Didier Jean-Claude Berthelot, Michel, Anna, Josef De Cleyn, Daniel Oehlrich
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Publication number: 20110281875Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: July 8, 2011Publication date: November 17, 2011Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Publication number: 20110275673Abstract: The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders.Type: ApplicationFiled: September 17, 2009Publication date: November 10, 2011Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
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Publication number: 20110275610Abstract: Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, benzyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: January 22, 2010Publication date: November 10, 2011Inventors: Alaric J. Dyckman, William J. Pitts, Scott Hunter Watterson
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Publication number: 20110275631Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: ApplicationFiled: October 13, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Bennett Farmer, II, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
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Publication number: 20110269761Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: April 17, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Frank Himmelsbach, Juergen Mack, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Publication number: 20110269756Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: December 8, 2009Publication date: November 3, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20110263661Abstract: Substituted 3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-phenyl-1,2,4-oxadiazole derivatives which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: ApplicationFiled: April 13, 2011Publication date: October 27, 2011Applicant: ALLERGAN, INC.Inventors: Janet A. Takeuchi, Ken Chow, Ling Li
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Publication number: 20110263613Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.Type: ApplicationFiled: January 11, 2011Publication date: October 27, 2011Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson