The Second Ring Of The Bicyclo Ring System Is A Five-membered Hetero Ring Including Three Ring Nitrogens (e.g., Triazolo[1,5-a]pyrimidine, Etc.) Patents (Class 514/259.31)
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Patent number: 8268835Abstract: The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4).Type: GrantFiled: July 15, 2009Date of Patent: September 18, 2012Assignee: Pfizer Inc.Inventors: Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Angelica Linton, John Howard Tatlock
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Patent number: 8268836Abstract: The present invention relates to a c-Met inhibitor or a pharmaceutically acceptable salt thereof useful in treating cancer mediated by activity of c-Met receptors.Type: GrantFiled: July 22, 2011Date of Patent: September 18, 2012Assignee: Eli Lilly and CompanyInventor: Zhipei Wu
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Publication number: 20120225884Abstract: The present invention relates to compounds of formula I hetaryl I, hetaryl II, R1, R2, R3, Y, m, and o or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: ApplicationFiled: February 27, 2012Publication date: September 6, 2012Inventors: Karlheinz Baumann, Luke Green, Anja Limberg, Thomas Luebbers, Andrew Thomas
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Publication number: 20120220566Abstract: 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: August 30, 2012Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
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Publication number: 20120208700Abstract: The present disclosure relates to the use of dibenzylidene sorbitol or derivatives of dibenzylidene sorbitol as rheology additives to provide stability to oil dispersion formulations of agrochemical active ingredients.Type: ApplicationFiled: February 11, 2011Publication date: August 16, 2012Applicant: DOW AGROSCIENCES LLCInventors: Derek J. Hopkins, Franklin N. Keeney, Lei Liu, Kuide Qin
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Publication number: 20120190542Abstract: The present invention relates to pesticidal mixtures, compositions and uses thereof comprising a component (A) and a component (B), wherein components (A) and (B) are: (A) a carboxylic acid amide fungicide; and (B) a benzamide fungicide; with the proviso that the mixture does not comprise: 1). fluopicolide and mandipropamid and clothianidin; or 2). fluopicolide and mandipropamid and imidacloprid; or 3). fluopicolide and mandipropamid and thiamethoxam. The invention also relates to mixtures, compositions and uses thereof wherein component (A) is metalaxyl-M and component (B) is a benzamide fungicide.Type: ApplicationFiled: March 29, 2010Publication date: July 26, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Patrick John Doyle, Gilberto Olaya-Huertas, Paul John Kuhn, Allison Tally
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Publication number: 20120190696Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: October 1, 2010Publication date: July 26, 2012Applicant: Schering CorporationInventors: Gerald W. Shipps, JR., Clifford C. Cheng, Xioahua Huang, Abdelghani Achab, Peter Orth, Johannes H. Voigt
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Publication number: 20120183496Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: July 19, 2012Applicant: COCRYSTAL DISCOVERY, INC.Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Publication number: 20120178748Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: January 10, 2012Publication date: July 12, 2012Applicant: Sunovion Pharmaceuticals Inc.Inventors: John Emmerson CAMPBELL, Philip JONES, Michael Charles HEWITT
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Patent number: 8211828Abstract: Fungicidal mixtures comprising as active components: 1) at least one 1-methylpyrazol-4-ylcarboxanilide of the formula I ?in which the substituents are defined according to the description and 2) at least one azolopyrimidinylamine of the formula II ?in which the substituents are defined according to the description in a synergistically effective amount. Methods for controlling harmful fungi using mixtures of the compound I and compound II and also the use of the compound I and the compound II for preparing such mixtures, and compositions comprising such mixtures.Type: GrantFiled: January 17, 2008Date of Patent: July 3, 2012Assignee: BASF SEInventors: Jochen Dietz, Ulrich Schoefl, Egon Haden
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Publication number: 20120135981Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 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: July 13, 2010Publication date: May 31, 2012Inventors: Tongfei Wu, Henricus Jacobus Maria Gijsen, Frederik Jan Rita Rombouts, François Paul Bischoff, Didier Jean-Claude Berthelot, Daniel Oehlrich, Michel Anna Jozef De Cleyn, Serge Maria Aloysius Pieters, Garrett Berlond Minne, Adriana Ingrid Velter', Sven Franciscus Anna Van Brandt, Michel Surkyn
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Publication number: 20120136010Abstract: A synergistic antimicrobial composition comprising: (a) 3-iodo-2-propynyl-butylcarbamate; and (b) flumetsulam. A synergistic antimicrobial composition comprising: (a) 3-iodo-2-propynyl-butylcarbamate; (b) diclosulam.Type: ApplicationFiled: July 29, 2010Publication date: May 31, 2012Inventors: Emerentiana Sianawati, Sangeeta Ganguly
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Patent number: 8183238Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: GrantFiled: June 16, 2010Date of Patent: May 22, 2012Assignee: Pfizer Inc.Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Publication number: 20120122680Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 0, 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: August 3, 2010Publication date: May 17, 2012Applicant: E.I. Du Pont de Nemours and CompanyInventors: Caleb William Holyoke, JR., Wenming Zhang, kanu Maganbhai Patel, George Philip Lahm, My-Hanh Thi Tong
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Publication number: 20120121540Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).Type: ApplicationFiled: August 8, 2008Publication date: May 17, 2012Inventors: Franz Ulrich Schmitz, Vincent W.F Tai, Roopa Ral, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Subramanian Baskaran, Irina Slobodov, Jack Maung, Martin Leon Neitzel
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Publication number: 20120115725Abstract: A synergistic antimicrobial composition containing flumetsulam and thiabendazole.Type: ApplicationFiled: November 4, 2011Publication date: May 10, 2012Inventor: Emerentiana Sianawati
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Publication number: 20120115888Abstract: A synergistic antimicrobial composition containing flumetsulam or diclosulam; and diiodomethyl-p-tolylsulfone.Type: ApplicationFiled: November 4, 2011Publication date: May 10, 2012Inventor: Emerentiana Sianawati
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Publication number: 20120115887Abstract: A synergistic antimicrobial composition containing flumetsulam and an isothiazolone biocide chosen from among 4,5-dichloro-2-n-octyl-4-isothiazolin-3-one, 2-n-octyl-4-isothiazolin-3-one and N-n-butyl-1,2-benzisothiazolin-3-one. A synergistic antimicrobial composition containing diclosulam and an isothiazolone biocide chosen from 4,5-dichloro-2-n-octyl-4-isothiazolin-3-one and 2-n-octyl-4-isothiazolin-3-one.Type: ApplicationFiled: October 31, 2011Publication date: May 10, 2012Inventor: Emerentiana Sianawati
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Publication number: 20120108595Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.Type: ApplicationFiled: June 28, 2010Publication date: May 3, 2012Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
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Publication number: 20120101112Abstract: This invention relates to novel substituted [1,2,4]triazolo[1,5-a]pyrimidines and their use as modulators of potassium channels. In other aspects the invention relates to the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: March 30, 2010Publication date: April 26, 2012Applicant: NEUROSEARCH A/SInventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dorte Strøbæk, Palle Christophersen
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Publication number: 20120095025Abstract: This invention relates to novel substituted [1,2,4]triazolo[1,5-a]pyrimidines useful as modulators of potassium channels. In other aspects the invention relates to the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. Formula (I).Type: ApplicationFiled: March 30, 2010Publication date: April 19, 2012Applicant: NEUROSEARCH A/SInventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Dorte Strøbæk, Palle Christophersen
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Publication number: 20120088665Abstract: The present invention relates to fungicidal mixtures comprising, as active components, 1) sulfur-containing triazole compounds I as described in the application, and 2) a fungicidal compound II, where the compounds II of component 2 are selected from among the compounds described in the application, and to the use of the fungicidal mixtures for controlling phytopathogenic fungi and to compositions comprising them.Type: ApplicationFiled: June 11, 2010Publication date: April 12, 2012Applicant: BASF SEInventors: Jochen Dietz, Thomas Grote, Egon Haden, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glättli, Marianna Vrettou-Schultes, Wassilios Grammenos
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Publication number: 20120088780Abstract: This invention relates to novel substituted [1,2,4]triazolo[1,5-a]pyrimidines and their use as modulators of potassium channels. In other aspects the invention relates to the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: March 30, 2010Publication date: April 12, 2012Applicant: NEUROSEARCH A/SInventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dorte Strøbaek, Palle Christophersen
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Patent number: 8148383Abstract: Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.Type: GrantFiled: January 29, 2010Date of Patent: April 3, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuyoshi Maekawa, Hideyuki Igawa
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Publication number: 20120077810Abstract: The instant invention provides for substituted fused pyrimidine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: March 29, 2010Publication date: March 29, 2012Inventors: Qi Chen, Mingxiang Cui, Bin Hu, Shuangxi Hu, Zhifa Pu, Philip E. Sanderson, Richard Soll, Xue Tang, Jiabing Wang, Yongjin Yan, Jinfeng Yao, Hongjie Zhang
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Publication number: 20120070421Abstract: The present invention relates to fungicidal mixtures, comprising a compound of formula I and one fungicidal component II selected from groups A?) to C?) as defined in the description, and to compositions comprising these mixtures.Type: ApplicationFiled: May 31, 2010Publication date: March 22, 2012Applicant: BASF SEInventors: Jochen Dietz, Egon Haden, Thomas Grote, Markus Gewehr, Silke Stoltz
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Publication number: 20120071417Abstract: Methods of inhibiting cancer cell growth using HDAC10 inhibitors are provided. Methods of treating cancer in a subject using HDAC10 inhibitors are also provided. In certain embodiments, at least one second inhibitor selected from an autophagy inhibitor, an AMPK inhibitor, and methyl pyruvate is also used in the methods. Dose packs comprising HDAC10 inhibitors and at least one second inhibitor are provided. Methods of identifying HDAC10 inhibitors are also provided.Type: ApplicationFiled: November 10, 2009Publication date: March 22, 2012Inventors: Tso-pang Yao, Hitoshi Sasajima, Yoshiharu Kawaguchi, Kai Cui, Chun-Hsiang Lai
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Patent number: 8133897Abstract: This invention is directed to phenylimidazole compounds, which are PDE10A enzyme inhibitors useful for the treatment of neurological and psychiatric disorders.Type: GrantFiled: June 19, 2009Date of Patent: March 13, 2012Assignee: H. Lundbeck A/SInventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn
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Publication number: 20120041003Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, and R3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.Type: ApplicationFiled: October 20, 2011Publication date: February 16, 2012Applicant: Abbott LaboratoriesInventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
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Publication number: 20120035050Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.Type: ApplicationFiled: March 25, 2009Publication date: February 9, 2012Applicant: BAYER CROPSCIENCE AGInventors: Peter Jeschke, Robert Velten, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20120035135Abstract: The Invention relates to methods for increasing the production potential of plants and/or controlling pests in plants with at least one transgenic modification related to yield increase as compared to a corresponding wild-type plant, comprising treating the location where the plant with at least one transgenic modification is growing or is expected to grow and/or the transgenic plant with at least one transgenic modification or propagation material of the plant with at least one transgenic modification with an effective amount of an insecticidal composition comprising a component A, selected from the group consisting of imidacloprid, thiacloprid, clothianidin, acetamiprid, dinotefuran, nitenpyram, and thiamethoxam; and a component B, selected from the group consisting of fipronil and ethiprole.Type: ApplicationFiled: December 22, 2009Publication date: February 9, 2012Applicant: Bayer CropScience AGInventors: Wolfram Andersch, Heike Hungenberg, Bernd Springer, Stefan Sachau, Casper Isaak Rooijen
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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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Patent number: 8110580Abstract: The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and the use of such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.Type: GrantFiled: September 13, 2007Date of Patent: February 7, 2012Assignee: Eli Lilly and CompanyInventors: Zhaogen Chen, Shaojuan Jia, James Lee Toth
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Publication number: 20120015910Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: Bayer CropScience AGInventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
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Publication number: 20120004203Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: December 29, 2009Publication date: January 5, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
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Publication number: 20110319432Abstract: Fungicidal compositions comprising as active components Fluopyram and 5-Ethyl-6-octyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamine in a synergistically effective amount, methods for controlling phytopathogenic harmful fungi using mixtures of Fluopyram and 5-Ethyl-6-octyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamine, the use of Fluopyram and 5-Ethyl-6-octyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamine for preparing such mixtures, and also compositions and seed comprising such mixtures.Type: ApplicationFiled: March 8, 2010Publication date: December 29, 2011Applicant: BASF SEInventors: Markus Gewehr, Ulf Groeger, Egon Haden, Michael Vonend
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Patent number: 8076344Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, and R3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.Type: GrantFiled: April 30, 2008Date of Patent: December 13, 2011Assignee: Abbott LaboratoriesInventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
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Patent number: 8071506Abstract: An herbicidal composition containing (a) florasulam and (b) at least one preemergent annual grass herbicide selected from the group consisting of dithiopyr and pendimethalin provides synergistic control of selected weeds in turf.Type: GrantFiled: April 14, 2010Date of Patent: December 6, 2011Assignee: Dow AgroSciences LLCInventors: Daniel L. Loughner, Randy L. Smith, Michael W. Melichar
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Publication number: 20110288087Abstract: Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.Type: ApplicationFiled: January 29, 2010Publication date: November 24, 2011Inventors: Tsuyoshi Maekawa, Hideyuki Igawa
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Publication number: 20110281859Abstract: Compounds of the formula I, in which D, X, Y, Z, R and R1 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.Type: ApplicationFiled: December 22, 2009Publication date: November 17, 2011Applicant: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Timo Heinrich, Frank Zenke, Mireille Krier, Kai Schiemann
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Publication number: 20110244020Abstract: The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1-3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 ?m, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided. The device contained in the kit typically, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Also disclosed, are methods for using these aerosols and kits.Type: ApplicationFiled: April 1, 2011Publication date: October 6, 2011Applicant: Alexza Pharmaceuticals, Inc.Inventors: Ron L. HALE, Craig C. Hodges, Peter M. Lloyd, Amy T. Lu, Daniel J. Myers, Joshua D. Rabinowitz, Martin J. Wensley, Jeffrey A. McKinney, Alejandro C. Zaffaroni
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Publication number: 20110245275Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a pyrazolopyrimidine compound such as ocinaplon, zaleplon, indiplon, or divaplon.Type: ApplicationFiled: October 16, 2009Publication date: October 6, 2011Inventor: David Reed Helton
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Publication number: 20110237575Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: November 10, 2009Publication date: September 29, 2011Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Abdelghani Abe Achab, Peter Orth, Johannes H. Voigt, Kyle Ann Soucy
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Publication number: 20110229484Abstract: The present invention provides several networks of cellular protein kinases as potential targets for medical intervention against hepatitis C virus (HCV) infection and HCV-related diseases and disorders in mammals, including humans. The invention relates to therapeutic protocols and pharmaceutical compositions designed to inhibit the activity of one or more of these protein kinases for the prevention and/or treatment of infections and diseases caused by HCV. The invention also relates to methods for the identification of kinase inhibitors that may be used to treat and/or prevent HCV infections and HCV-related diseases.Type: ApplicationFiled: September 18, 2009Publication date: September 22, 2011Applicant: INSERM (Institut National de la Sant et de la Recherche Medicale)Inventors: Thomas Baumert, Joachim Lupberger
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Publication number: 20110224198Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Scott D. Kuduk, Douglas C. Beshore, ChristinaNg Di Marco, Thomas J. Greshock
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Patent number: 8012973Abstract: Adenosine A2A receptor antagonists are useful for the preparation of medicaments against atrial fibrillation in mammals, including humans. It has been found that the adenosine A2A receptor is present in human atrial cardiomyocytes and participates in the pathological mechanisms underlying atrial fibrillation. An advantage of using A2A antagonists over other agents known in the art is that the A2A antagonists specifically target patients with atrial fibrillation.Type: GrantFiled: October 10, 2006Date of Patent: September 6, 2011Assignee: Proyecto de Biomedicina Cima S.L.Inventors: Rafael Franco Fernández, Franciso Ciruela Alférez, Carmen Lluís Biset, Christa Müller, Joan Cinca Cuscullola, Leif Hove-Madsen
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Publication number: 20110207736Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.Type: ApplicationFiled: December 22, 2010Publication date: August 25, 2011Inventors: Nathanael S. GRAY, Wenjun Zhou
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Publication number: 20110190269Abstract: The invention relates to compounds of formula wherein R1, R1?, R2, R3, n, A, and hetaryl are defined herein or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: ApplicationFiled: January 24, 2011Publication date: August 4, 2011Inventors: Karlheinz Baumann, Erwin Goetschi, Luke Green, Synese Jolidon, Henner Knust, Anja Limberg, Thomas Luebbers, Andrew Thomas
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Publication number: 20110178078Abstract: The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.Type: ApplicationFiled: October 6, 2009Publication date: July 21, 2011Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Yan Lavrovsky, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Publication number: 20110165183Abstract: The invention provides a compound of formula (I): wherein W is a bicyclic heteroaromatic group; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).Type: ApplicationFiled: July 31, 2009Publication date: July 7, 2011Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar