Nitrogen Bonded Directly To The 1,3-diazine At 2-position Patents (Class 514/272)
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Publication number: 20130150390Abstract: A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect.Type: ApplicationFiled: December 12, 2012Publication date: June 13, 2013Inventors: Mie Kaino, Hiroyuki Meguro
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Patent number: 8461160Abstract: This invention relates to dihydropyrimidinones of the formula wherein X and R1 to R7 are as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.Type: GrantFiled: April 30, 2010Date of Patent: June 11, 2013Assignee: Hoffmann-La Roche, Inc.Inventors: David Banner, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Fabienne Ricklin, Mark Rogers-Evans
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Patent number: 8455497Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 12, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Publication number: 20130137635Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.Type: ApplicationFiled: February 9, 2011Publication date: May 30, 2013Applicant: LEXICON PHARMACEUTICALS, INC.Inventor: Arthur Thomas Sands
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Patent number: 8450335Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same. In some embodiments, the present invention provides a compound of formula I-b: wherein each of Ring A, Ring B, W1, W2, Ry, Rv, Rx, m, p, and R1 is described herein.Type: GrantFiled: June 26, 2009Date of Patent: May 28, 2013Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Patent number: 8445505Abstract: The invention provides novel pyrimidine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).Type: GrantFiled: June 24, 2009Date of Patent: May 21, 2013Assignee: IRM LLCInventors: Thomas H. Marsilje, III, Wenshuo Lu, Bei Chen, Xiaohui He, Songchun Jiang, Kunyong Yang
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Publication number: 20130123284Abstract: Provided herein are compounds useful for kinase inhibition.Type: ApplicationFiled: March 24, 2011Publication date: May 16, 2013Applicant: AMITECH THERAPEUTIC SOLUTIONS INCInventors: Lee Daniel Arnold, Eric A. Murphy
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Publication number: 20130123260Abstract: The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of rhinovirus infection, methods of treating or preventing rhinovirus infection employing said compounds or pharmaceutical composition comprising the same. The disclosure also relates to compounds of formula (I) for use in the treatment or prophylaxis of exacerbation of respiratory disorders (such as asthma, COPD, bronchitis and/or cystic fibrosis) by rhinovirus infection.Type: ApplicationFiled: June 17, 2011Publication date: May 16, 2013Applicant: RESPIVERT LIMITEDInventors: Catherine Elisabeth Charron, Kazuhiro Ito, William Garth Rapeport
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Publication number: 20130096148Abstract: 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile is a key intermediate for the preparation of etravirine. The present invention provides a process for preparation of 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile. The present invention also provides a novel process for the preparation of etravirine crystalline form I. The present invention further provides novel crystalline forms of etravirine, processes for their preparation and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 28, 2010Publication date: April 18, 2013Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Bandi Vamsi Krishna, Adulla Venkat Narsimha Reddy
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Publication number: 20130096127Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 29, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Publication number: 20130090326Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.Type: ApplicationFiled: October 15, 2010Publication date: April 11, 2013Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Yanming Du, Sandra Sinishtaj, Yuanqing Tang, Brian T. Wimberly
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Patent number: 8410124Abstract: This disclosure relates to novel di-aryl-pyrimidine (DAPY) compounds and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a non-nucleoside reverse transcriptase inhibitor (NNRTI).Type: GrantFiled: October 17, 2008Date of Patent: April 2, 2013Assignee: Concert Pharmaceuticals Inc.Inventor: Craig E. Masse
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Patent number: 8410096Abstract: Disclosed are an antitumor preparation comprising a combination of (1) a combination drug of tegafur/gimeracil/oteracil potassium, (2) at least one ingredient selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof, and (3) cis-oxalate(1R,2R-diaminocyclohexane)platinum(II); a kit comprising a combination of pharmaceutical compositions for treating cancer in a mammal, comprising: (a) a combination drug of tegafur/gimeracil/oteracil potassium in a therapeutically effective amount; (b) a composition containing at least one ingredient selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof in an amount effective for enhancing antitumor effects, and (c) a composition containing cis-oxalate(1R,2R-diaminocyclohexane)platinum(II) in an amount effective for enhancing antitumor effects; and a method for treating cancer.Type: GrantFiled: November 12, 2010Date of Patent: April 2, 2013Assignees: Shizuoka Prefecture, Taiho Pharmaceutical Co., Ltd.Inventor: Sung Hwa Park
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Publication number: 20130079338Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: September 24, 2012Publication date: March 28, 2013Applicant: BRISTOL-MYERS SQUIBB COMPANYInventor: Bristol-Myers Squibb Company
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Publication number: 20130065890Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.Type: ApplicationFiled: November 8, 2012Publication date: March 14, 2013Inventor: Hutchison Medipharma Enterprises Limited
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Patent number: 8394808Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.Type: GrantFiled: September 2, 2009Date of Patent: March 12, 2013Assignee: Glaxosmithkline LLCInventors: Ivan Leo Pinto, Shahzad Sharooq Rahman, Neville Hubert Nicholson
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Patent number: 8394809Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.Type: GrantFiled: October 28, 2010Date of Patent: March 12, 2013Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A. Miskowski, Scott L. Dax, Henry Breslin, Bart L. De Corte, Wei He
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Publication number: 20130059849Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: May 5, 2011Publication date: March 7, 2013Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
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Publication number: 20130059871Abstract: The present invention provides (I) these compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes.Type: ApplicationFiled: April 30, 2012Publication date: March 7, 2013Inventors: David Christopher HORWELL, David Ian Carter SCOPES
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Publication number: 20130053409Abstract: The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.Type: ApplicationFiled: July 25, 2012Publication date: February 28, 2013Applicant: ASTRAZENECA ABInventors: Sam BUTTERWORTH, Maurice Raymond Verschoyle FINLAY, Richard Andrew WARD, Vasantha Krishna KADAMBAR, Chandrashekar Reddy C MURUGAN, Andiappan MURUGAN, Heather Marie REDFEARN
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Publication number: 20130053343Abstract: Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.Type: ApplicationFiled: November 2, 2010Publication date: February 28, 2013Applicant: The Trustees of Columbia University in th City ofInventors: Donald Landry, Shi-Xian Deng
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Patent number: 8383640Abstract: The invention relates to substituted pyrimidine ether compounds having general formula I: The groups are as defined as specification. The compounds of formula I show high insecticidal activities for imagoes, larvae and nits of harmful acari and insects in the agricultural, civil and zoic fields, especially show excellent insecticidal activities for harmful acari such as Tetranychus cinnabarinus. Good effects can be obtained at very low dose. The compounds also exhibit preferably fungicidal activity. Wherefore, the invention also comprises the uses of compounds of formula I as insecticides, acaricides and/or fungicides in agricultural and other fields.Type: GrantFiled: May 22, 2008Date of Patent: February 26, 2013Assignees: Shenyang Research Institute of Chemical Industry Co., Ltd., Sinochem CorporationInventors: Changling Liu, Baoshan Chai, Hong Zhang, Huichao Li, Junfeng Wang, Yongwu Peng, Jichun Yang, Guangxin Liu, Zhinian Li
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Publication number: 20130035326Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 18, 2010Publication date: February 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
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Publication number: 20130029990Abstract: There are provided inter alia compounds of formula (I): wherein R1, R2a, R2b, R3, R4, L, X, R5 and R6 are as defined in the description for use in the treatment of inflammatory diseases.Type: ApplicationFiled: April 1, 2011Publication date: January 31, 2013Inventors: John King-Underwood, George Hardy, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
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Patent number: 8362236Abstract: The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.Type: GrantFiled: February 29, 2008Date of Patent: January 29, 2013Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Nobuo Shimma, Takuo Tsukuda, Hiroshi Koyano, Atsushi Suda, Tadakatsu Hayase, Kihito Hada, Ken-Ichi Kawasaki, Susumu Komiyama, Naomi Ono, Toshikazu Yamazaki, Ryoichi Saitoh, Masami Kohchi, Kiyoshi Hasegawa
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Publication number: 20130022629Abstract: Disclosed are an assay to identify modulators of the PD-1:PD-L pathway and PD-1:PD-L pathway modulators, e.g., compounds and pharmaceutical compositions thereof. Methods for treating diseases influenced by modulation of the PD-1:PD-L pathway such as, for example, autoimmune diseases, inflammatory disorders, allergies, transplant rejection, cancer, immune deficiency, and other immune system-related disorders, are also disclosed.Type: ApplicationFiled: January 3, 2011Publication date: January 24, 2013Inventors: Arlene H. Sharpe, Manish J. Butte, Shinji Oyama
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Publication number: 20130022561Abstract: The present invention relates to a cosmetic composition comprising, in a cosmetically acceptable medium, (i) a supramolecular compound that may be obtained by reaction between: at least one oil bearing at least one nucleophilic reactive function chosen from OH and NH2, and at least one junction group capable of establishing hydrogen bonds with one or more partner junction groups, each pairing of a junction group involving at least three hydrogen bonds, the said junction group bearing at least one isocyanate or imidazole reactive function capable of reacting with the reactive function borne by the oil, the said junction group also comprising at least one unit of formula (I) or (II): (I) (II) (ii) at least one oil, chosen from apolar hydrocarbon-based oils and silicone oils, (iii) at least one dyestuff. The invention also relates to a cosmetic treatment process comprising the application of the said composition.Type: ApplicationFiled: December 15, 2010Publication date: January 24, 2013Applicant: L'OREALInventors: Claudia Barba, Roberto Cavazzuti, Nathalie Geffroy
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Publication number: 20130017162Abstract: The invention relates to a cosmetic composition, especially a hair composition, and to a method for the cosmetic treatment of keratin materials, especially of the hair, employing compounds of formula: in which Z represents (i) a hydrogen atom, (ii) a linear or branched C1 to C32 (saturated) alkyl radical; (iii) a linear or branched C2 to C32 (unsaturated) alkene radical, comprising one or two C?C double bonds; (iv) an aryl-substituted alkyl radical; said radicals being optionally substituted and/or interrupted.Type: ApplicationFiled: January 4, 2011Publication date: January 17, 2013Applicant: L'OREALInventors: Anne-Claude Dublanchet, Christian Blaise, Abel Messavussu
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Patent number: 8354420Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: GrantFiled: June 1, 2011Date of Patent: January 15, 2013Assignee: Genentech, Inc.Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Mark Chambers, Bryan K. Chan, Huifen Chen, Anthony Estrada, Janet Gunzner-Toste, Daniel Shore, Zachary Sweeney, Shumei Wang, Guiling Zhao
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Patent number: 8349860Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: GrantFiled: October 17, 2011Date of Patent: January 8, 2013Assignee: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Chandrasekar Venkataramani, Wolin Huang, Mukund Mehrotra, Yonghong Song, Qing Xu, Shawn M. Bauer, Jack W. Rose, Brian Kane, Anjali Pandey
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Patent number: 8349345Abstract: A composition for control of diseases on useful plants or on propagation material thereof caused by phytopathogens, that, in addition to customary inert formulation adjuvants, comprises as active ingredient a mixture of component (A) and a synergistically effective amount of component (B), wherein component (A) is Cyprodinil; and component (B) a compound selected from compounds known for their fungicidal activity, is particularly effective in controlling or preventing fungal diseases of useful plants.Type: GrantFiled: September 27, 2006Date of Patent: January 8, 2013Assignee: Syngenta Crop Protection LLCInventors: Birgit Forster, Duncan McKenzie, Jeremy Godwin
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Publication number: 20130005754Abstract: Solid forms of (S)-ethyl 2-amino-3 -(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed.Type: ApplicationFiled: June 1, 2012Publication date: January 3, 2013Inventors: Mark S. BEDNARZ, Susan De PAUL, Ramanaiah C. KANAMARLAPUDI, Anett PERLBERG, Haiming ZHANG
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Publication number: 20130004438Abstract: The present invention relates to a cosmetic composition comprising, in a cosmetically acceptable medium, (i) a supramolecular compound that may be obtained by reaction between: —at least one oil bearing at least one nucleophilic reactive function chosen from OH and NH2, and —at least one junction group capable of establishing hydrogen bonds with one or more partner junction groups, each pairing of a junction group involving at least three hydrogen bonds, the said junction group bearing at least one isocyanate or imidazole reactive function capable of reacting with the reactive function borne by the oil, the said junction group also comprising at least one unit of formula (I) or (II): (ii) and at least one additional ingredient preferably chosen from: —silicone elastomers, —polyesters that may be obtained by reacting: a tetraol containing from 4 to 10 carbon atoms; a saturated, linear or branched monocarboxylic acid containing from 9 to 23 carbon atoms; a cyclic dicarboxylic acid containing from 6 to 12 carbonType: ApplicationFiled: December 15, 2010Publication date: January 3, 2013Applicant: L'OREALInventors: Claudia Barba, Roberto Cavazzuti
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Publication number: 20120316188Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 14, 2011Publication date: December 13, 2012Inventor: Christelle Boléa
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Patent number: 8324231Abstract: A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways.Type: GrantFiled: April 24, 2008Date of Patent: December 4, 2012Assignee: Exelixis, Inc.Inventors: Elena S. Koltun, Patrick Kearney, Naing Aay, Arlyn Arcalas, Wai Ki Vicky Chan, Jeffry Kimo Curtis, Hongwang Du, Ping Huang, Brian Kane, Moon Hwan Kim, Michael Pack, Amy L. Tsuhako, Wei Xu, Cristiana A. Zaharia, Peiwen Zhou
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Patent number: 8324230Abstract: Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms.Type: GrantFiled: October 3, 2005Date of Patent: December 4, 2012Assignee: Pfizer Inc.Inventor: Jon G. Selbo
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Patent number: 8318755Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: GrantFiled: October 7, 2011Date of Patent: November 27, 2012Assignee: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Chandrasekar Venkataramani, Wolin Huang, Mukund Mehrotra, Yonghong Song, Qing Xu, Shawn M. Bauer, Jack W. Rose, Brian Kane, Anjali Pandey
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Publication number: 20120283095Abstract: The present invention relates to synergistic mixtures comprising, as active components, one insecticidal compound I selected from the group consisting of carbamates; and one fungicidal compound II selected from the group of strobilurines in synergistic effective amounts.Type: ApplicationFiled: November 29, 2010Publication date: November 8, 2012Applicant: BASF SEInventors: Markus Gewehr, Egon Haden, Lutz Brahm
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Patent number: 8303944Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: February 13, 2008Date of Patent: November 6, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20120277230Abstract: The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a NO2 group, a NR1R2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n is 1 or 2, R is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group, a hydroxyl group, a COOR1 group, a NO2 group, a NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating cancer. Some of said compounds are new and also form part of the invention.Type: ApplicationFiled: June 14, 2010Publication date: November 1, 2012Applicants: SOCIETE SPLICOS, UNIVERSITE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Pierre Roux, Florence Mahuteau, Romain Najman, Jamal Tazi, Gilles Gadea, Didier Scherrer, Carsten Brock, Nathalie Cahuzac
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Publication number: 20120277235Abstract: A composition comprising at least one physiologically tolerated film forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I or a stereoisomeric form or a physiologically tolerated salt of any of the foregoing. The composition is suitable for treatment of androgenic alopecia or hirsutism, that is, for avoiding undesirable hair growth, and for treatment of seborrhea and acne, and can furthermore be employed in cosmetics.Type: ApplicationFiled: March 30, 2012Publication date: November 1, 2012Inventors: Karl Theodor Kraemer, Manfred Bohn
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Publication number: 20120270889Abstract: Compound of Formula A and pharmaceutically acceptable salts thereof and crystalline Forms I and II of Compound of Formula A! Also, methods for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for their uses.Type: ApplicationFiled: November 23, 2010Publication date: October 25, 2012Inventors: Wei-Guo Su, Weihan Zhang, Hong Jia, Yumin Cui, Yongxin Ren, Yang Sai, Zhenping Wu, Wenji Li, Jiangyong Shao, Zhenping Tian
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Patent number: 8293769Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.Type: GrantFiled: May 20, 2008Date of Patent: October 23, 2012Assignee: Novartis AGInventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
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Publication number: 20120245118Abstract: Methods of treating stuttering include treating people with gamma-aminobutyric acid (GABA) receptor modulators, including cyclopyrrolones. A second active agent may be used with GABA receptor modulators. Active enantiomers, active metabolites, and pharmaceutically acceptable salts of gamma-aminobutyric acid receptor modulators, including cyclopyrrolones, are acceptable components of the compositions. The cyclopyrrolone class of modulators includes pagoclone, suriclone, zopiclone, 2-(7-chloro-2-naphthyridin-1,8-yl)-3-(5-methyl-2-oxohexyl)isoindolin-1-one, 2-(7-chloro-2-naphthyridin-1,8-yl)isoindolin-1-yl-4-acetamidobutyrate, and 2-(7-chloro-1,8-naphthyridin-2yl)-3-(5-methyl-5-hydroxy-2-oxohexyl)-1-isoindolinone.Type: ApplicationFiled: June 6, 2012Publication date: September 27, 2012Applicant: Endo Pharmaceuticals Solutions Inc.Inventors: John J. Murphy, Kay Jorgenson D'Orlando
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Patent number: 8268809Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.Type: GrantFiled: September 5, 2007Date of Patent: September 18, 2012Assignees: Emory University, M.D. Anderson Cancer CenterInventors: Daniel Kalman, William Bornmann
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Publication number: 20120232064Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: March 15, 2012Publication date: September 13, 2012Applicant: SCHERING CORPORATIONInventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
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Publication number: 20120231018Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Applicants: Pharmacopeia Inc., Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mozzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20120231017Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Applicants: Pharmacopeia Inc., Schering CorporationInventors: ZHAONING ZHU, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mozzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Sainoz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
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Publication number: 20120232102Abstract: The present invention is directed to methods of administering pazopanib or pharmaceutically acceptable salts or solvates thereof as well as methods of treating cancer and age-related macular degeneration in patients in need thereof.Type: ApplicationFiled: September 29, 2010Publication date: September 13, 2012Inventor: Chun-fang Xu
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Publication number: 20120225057Abstract: Compounds of the present invention, alone and in combination with other active agents, find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to for example malignant melanomas, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.Type: ApplicationFiled: September 8, 2011Publication date: September 6, 2012Applicant: DECIPHERA PHARMACEUTICALS, LLCInventors: Daniel L. Flynn, Michael D. Kaufman