Ring Sulfur Or Ring Oxygen In The Additional Hetero Ring Patents (Class 546/209)
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Patent number: 8198453Abstract: The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.Type: GrantFiled: September 18, 2007Date of Patent: June 12, 2012Assignee: Vitae Pharmaceuticals, Inc.Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Lanqi Jia, Patrick T. Flaherty
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Publication number: 20120142700Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.Type: ApplicationFiled: August 5, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondex, Laura Quaranta
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Publication number: 20120142668Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.Type: ApplicationFiled: August 11, 2010Publication date: June 7, 2012Inventors: Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
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Publication number: 20120136003Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-IV) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: April 20, 2010Publication date: May 31, 2012Inventors: Michael Geoffrey Neil Russell, Kevin James Doyle
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Publication number: 20120129779Abstract: The present invention relates to novel cytotoxic molecules and their use for the treatment of cancer and other diseases.Type: ApplicationFiled: May 9, 2008Publication date: May 24, 2012Applicant: R&D-BIOPHARMACEUTICALS GMBHInventor: Wolfgang Richter
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Publication number: 20120129842Abstract: This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Paul Francis JACKSON, Brett Andrew Tounge, Kristi Anne Leonard, Yan Zhang, Aihua Wang, Michael Hawkins, Umar S.M. Maharoof, Joseph Kent Barbay
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Publication number: 20120129831Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: May 14, 2010Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
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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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Patent number: 8183383Abstract: PTP1B inhibitors with the following structure (formula I). Experiments indicate that these inhibitors can effectively inhibit the activity of protein tyrosine phosphatase 1B (PTP1B). They can be used as insulin sensitisers. They can be used to prevent, delay or treat diseases which are related to insulin antagonism mediated by PTP1B, especially diabetes type II and obesity. The invention also provides methods for preparing these inhibitors.Type: GrantFiled: February 26, 2008Date of Patent: May 22, 2012Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jia Li, Yi Wei, Wei Zhang, Jingya Li, Lei Shi
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Publication number: 20120122905Abstract: The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.Type: ApplicationFiled: June 17, 2010Publication date: May 17, 2012Applicant: CADILA HEALTHCARE LIMITEDInventors: Harikishore Pingali, Pandurang Zaware, Mukul Jain
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Publication number: 20120122928Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi, and processes for preparing the compounds of the formula (I).Type: ApplicationFiled: August 9, 2011Publication date: May 17, 2012Applicant: Bayer CropScience AGInventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Pierre Cristau, Thomas Seitz, Joachim Kluth, Jürgen Benting, Ulrike Wachendorff-Neumann
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Publication number: 20120122929Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: ApplicationFiled: August 23, 2011Publication date: May 17, 2012Applicant: BAYER CROPSCIENCE AGInventors: Tomoki TSUCHIYA, Pierre WASNAIRE, Sebastian HOFFMANN, Pierre CRISTAU, Thomas SEITZ, Joachim KLUTH, Stefan HILLEBRAND, Jürgen BENTING, Daniela PORTZ, Ulrike WACHENDORFF-NEUMANN
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Patent number: 8178688Abstract: The present invention relates to novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same. The novel benzamidine derivatives of the present invention are useful for the prevention and treatment of osteoporosis, bone fractures and allergic inflammatory diseases.Type: GrantFiled: August 4, 2005Date of Patent: May 15, 2012Assignee: Dong Wha Pharmaceutical Co., Ltd.Inventors: Jin Soo Lee, Seok Hoon Ahn, Young Goo Jin, Sang Mi Jin, Whui-Jung Park, Sae Kwang Ku, Yun Ha Hwang, Pan Soo Kim, Sun Shin Yi, Jei Man Ryu
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Patent number: 8178531Abstract: The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention of organ transplantation rejection, the treatment of immune disorders and inflammation, and treatment of viral (particularly hepatitis C viral) infection.Type: GrantFiled: February 23, 2011Date of Patent: May 15, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Xuri Gao
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Patent number: 8173652Abstract: The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: February 12, 2010Date of Patent: May 8, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Maria-Clemencia Hernandez, Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Patent number: 8173680Abstract: Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I).Type: GrantFiled: December 8, 2008Date of Patent: May 8, 2012Assignee: 7TM Pharma A/SInventors: Jean-Marie Receveur, Emelie Bjurling, Anthony Murray, Thomas Hoegberg, Peter Aadal Nielsen, Jean-Michel Linget, Pia Karina Noerregaard, Dorthe Almholt
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Patent number: 8163728Abstract: The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: April 28, 2010Date of Patent: April 24, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Patent number: 8163775Abstract: The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R1 and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: GrantFiled: September 30, 2011Date of Patent: April 24, 2012Assignee: Addex Pharma SAInventors: Anne-Sophie Bessis, Beatrice Bonnet, Emmanuel Le Poul, Jean-Philippe Rocher, Mark Epping-Jordan
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Patent number: 8163757Abstract: The present invention relates to compounds of formula (IA) or (IB) or pharmaceutically or veterinarily acceptable salt thereof:Type: GrantFiled: September 2, 2010Date of Patent: April 24, 2012Assignee: MediGene AGInventor: Ian Richard Matthews
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Publication number: 20120095047Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.Type: ApplicationFiled: December 22, 2011Publication date: April 19, 2012Applicant: UNIVERSITY OF CONNECTICUTInventors: Alexandros Makriyannis, Rajesh Thotapally, Venkata Kiran Rao Vemuri, Teresa Olszewska
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Publication number: 20120083490Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Applicant: ABBOTT LABORATORIESInventors: Larry L. Klein, Hui-Ju Chen, Ming C. Yeung, Charles A. Flentge, John T. Randolph, Peggy P. Huang, Douglas K. Hutchinson, Dale J. Kempf
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Patent number: 8148401Abstract: The present invention relates to a compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3A, R3B, R4, R5, X, m, and n are as defined herein. Such novel benzamidazole derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: June 19, 2008Date of Patent: April 3, 2012Assignee: Pfizer Inc.Inventors: Michael J. Munchhof, Lawrence A. Reiter, Susan D. La Greca, Christopher S. Jones, Qifang Li
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Publication number: 20120077812Abstract: The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: November 30, 2011Publication date: March 29, 2012Inventors: JING FANG, Jun Tang, Andrew J. Carpenter, Gregory Peckham, Christopher R. Conlee, Kien S. Du, Subba Reddy Katamreddy
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Publication number: 20120071481Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.Type: ApplicationFiled: February 2, 2010Publication date: March 22, 2012Inventors: Ronald Palin, Paul David Ratcliffe, Steven G. Kultgen, Koc-Kan Ho, Andrew Laird Roughton
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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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Patent number: 8138182Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).Type: GrantFiled: September 24, 2009Date of Patent: March 20, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
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Patent number: 8138206Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.Type: GrantFiled: May 29, 2006Date of Patent: March 20, 2012Assignee: MSD. K.K.Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
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Patent number: 8138184Abstract: An isoxazole derivative is provided. The isoxazole derivative has following formula: wherein R1, R2, R3, R4 and R5, independently, include hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis and cancer including an isoxazole derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.Type: GrantFiled: October 1, 2008Date of Patent: March 20, 2012Assignee: Kaohsiung Medical UniversityInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Gwo-Jaw Wang, Mei-Ling Ho, Je-Ken Chang, Yin-Chih Fu
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Patent number: 8133905Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: December 17, 2009Date of Patent: March 13, 2012Assignee: Theravance, Inc.Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
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Patent number: 8133889Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.Type: GrantFiled: August 4, 2010Date of Patent: March 13, 2012Assignee: Les Laboratoires ServierInventors: Jean-Claude Ortuno, Alexis Cordi, Jean-Michel Lacoste, Vincent Lacoste, legal representative, Pauline Lacoste, legal representative, Imre Fejes, Michael Burbridge, John Hickman, Alain Pierre
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Patent number: 8124627Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: October 26, 2009Date of Patent: February 28, 2012Assignee: Theravance, Inc.Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
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Publication number: 20120046268Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: March 12, 2010Publication date: February 23, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
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Publication number: 20120046266Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: April 16, 2010Publication date: February 23, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
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Patent number: 8119663Abstract: The invention relates to novel heteroaryl-substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular diseases and tumor diseases.Type: GrantFiled: November 25, 2008Date of Patent: February 21, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Dirk Heimbach, Susanne Röhrig, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Yolanda Cancho Grande, Mario Jeske, Kersten Matthias Gericke
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Patent number: 8119812Abstract: An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action. The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.Type: GrantFiled: April 19, 2010Date of Patent: February 21, 2012Assignees: SBI Biotech Co., Ltd., Crystalgenomics, Inc.Inventors: Takayuki Irie, Masaaki Sawa, Sayuri Ito, Chika Tanaka, Seong Gu Ro, Choul Hong Park
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Publication number: 20120040998Abstract: The present invention is directed to 2-alkylpiperidines which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: April 22, 2010Publication date: February 16, 2012Inventors: Swati P. Mercer, Anthony J. Roecker, Theresa Williams, Xu-Fang Zhang
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Publication number: 20120034315Abstract: Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed. Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.Type: ApplicationFiled: April 19, 2010Publication date: February 9, 2012Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Mary Ann Hanagan, Matthew Richard Oberholzer, Robert James Pasteris, Rafael Shapiro
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Publication number: 20120028981Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: November 5, 2009Publication date: February 2, 2012Applicant: PRINCIPIA BIOPHARMA INC.Inventor: Richard Miller
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Publication number: 20120028979Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: October 6, 2011Publication date: February 2, 2012Inventors: Gregory BASARAB, Pamela HILL, Brian SHERER, Fei ZHOU
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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: 20120028931Abstract: Compounds I (R1 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotricyclic group containing from 1 to 5 heteroatoms selected from N, O and S; R2 is H, an optionally substituted monocyclic aromatic group, or a C1-C5 heteroaromatic group containing from 1 to 4 heteroatoms selected from N, O and S; R3 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotricyclic group containing from 1 to 5 heteroatoms selected from N, O and S; an optionally substituted mono-, bi- or tricyclic C6-C14 aryl group, an optionally substituted C3-C6 cycloalkyl group, or an optionally substituted C3-C6 cycloalkenyl group; each R4, independently for each position capable of substitution, is H or C1-C6 alkyl; R5 is H, halogen or C1-C6 alkyl; m is 0, 1 or 2; n is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, or 6; and is an optional double bond) and their enantiomers, diastereomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful fType: ApplicationFiled: September 14, 2010Publication date: February 2, 2012Applicant: RECORDATI IRELAND LIMITEDInventors: Amedeo Leonardi, Carlo Riva, Luciano Guarneri, Davide Graziani, Fabio Marinoni, Gianni Motta, Ilaria Bettinelli
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Publication number: 20120022108Abstract: The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R1 and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: ApplicationFiled: September 30, 2011Publication date: January 26, 2012Applicant: Addex Pharma SAInventors: Anne-Sophie Bessis, Beatrice Bonnet, Emmanuel Le Poul, Jean-Philippe Rocher, Mark Eppig-Jordan
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Publication number: 20120022107Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: December 11, 2009Publication date: January 26, 2012Applicant: ASTRAZENECA ABInventors: Shahul Hameed Peer Mohamed, David Waterson
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Publication number: 20120022068Abstract: The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, wherein A is NR2?, S or O; R3a is H, OH, SH, NH2, —C(NR7)NR7?R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, alkoxy, alkylamino, hydroxyalkylamino, halogen, aryl, or heteroaryl; R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, hydroxyalkylamino, alkylamino, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; X is NR2?, O, or S; Z is N or CR2?.Type: ApplicationFiled: September 2, 2011Publication date: January 26, 2012Applicant: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20120022052Abstract: The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof.Type: ApplicationFiled: June 29, 2011Publication date: January 26, 2012Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Publication number: 20120022249Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 26, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Naotake KOBAYASHI, Kazuo UEDA, Naohiro ITOH, Shinji SUZUKI, Gaku SAKAGUCHI, Akira KATO, Akira YUKIMASA, Akihiro HORI, Yuji KORIYAMA, Hidekazu HARAGUCHI, Ken YASUI, Yasuhiko KANDA
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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: 20120015929Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Applicant: ABBOTT LABORATORIESInventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez Medrano, Xueqing Wang, Karin Rose Marie Tietje, Sridhar Peddi, William A. Carroll
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Publication number: 20120016116Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Naotake KOBAYASHI, Kazuo UEDA, Naohiro ITOH, Shinji SUZUKI, Gaku SAKAGUCHI, Akira KATO, Akira YUKIMASA, Akihiro HORI, Yuji KORIYAMA, Hidekazu HARAGUCHI, Ken YASUI, Yasuhiko KANDA
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Publication number: 20120010199Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.Type: ApplicationFiled: September 23, 2011Publication date: January 12, 2012Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama