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)
  • Patent number: 8268835
    Abstract: 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: Grant
    Filed: July 15, 2009
    Date of Patent: September 18, 2012
    Assignee: Pfizer Inc.
    Inventors: Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Angelica Linton, John Howard Tatlock
  • Patent number: 8268836
    Abstract: 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: Grant
    Filed: July 22, 2011
    Date of Patent: September 18, 2012
    Assignee: Eli Lilly and Company
    Inventor: Zhipei Wu
  • Publication number: 20120225884
    Abstract: 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: Application
    Filed: February 27, 2012
    Publication date: September 6, 2012
    Inventors: Karlheinz Baumann, Luke Green, Anja Limberg, Thomas Luebbers, Andrew Thomas
  • Publication number: 20120220566
    Abstract: 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: Application
    Filed: October 15, 2010
    Publication date: August 30, 2012
    Applicant: 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
  • Publication number: 20120208700
    Abstract: 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: Application
    Filed: February 11, 2011
    Publication date: August 16, 2012
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Derek J. Hopkins, Franklin N. Keeney, Lei Liu, Kuide Qin
  • Publication number: 20120190542
    Abstract: 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: Application
    Filed: March 29, 2010
    Publication date: July 26, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Patrick John Doyle, Gilberto Olaya-Huertas, Paul John Kuhn, Allison Tally
  • Publication number: 20120190696
    Abstract: 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: Application
    Filed: October 1, 2010
    Publication date: July 26, 2012
    Applicant: Schering Corporation
    Inventors: Gerald W. Shipps, JR., Clifford C. Cheng, Xioahua Huang, Abdelghani Achab, Peter Orth, Johannes H. Voigt
  • Publication number: 20120183496
    Abstract: 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: Application
    Filed: December 16, 2011
    Publication date: July 19, 2012
    Applicant: COCRYSTAL DISCOVERY, INC.
    Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Publication number: 20120178748
    Abstract: 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: Application
    Filed: January 10, 2012
    Publication date: July 12, 2012
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: John Emmerson CAMPBELL, Philip JONES, Michael Charles HEWITT
  • Patent number: 8211828
    Abstract: 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: Grant
    Filed: January 17, 2008
    Date of Patent: July 3, 2012
    Assignee: BASF SE
    Inventors: Jochen Dietz, Ulrich Schoefl, Egon Haden
  • Publication number: 20120135981
    Abstract: 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: Application
    Filed: July 13, 2010
    Publication date: May 31, 2012
    Inventors: 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
  • Publication number: 20120136010
    Abstract: 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: Application
    Filed: July 29, 2010
    Publication date: May 31, 2012
    Inventors: Emerentiana Sianawati, Sangeeta Ganguly
  • Patent number: 8183238
    Abstract: 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: Grant
    Filed: June 16, 2010
    Date of Patent: May 22, 2012
    Assignee: Pfizer Inc.
    Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
  • Publication number: 20120122680
    Abstract: 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: Application
    Filed: August 3, 2010
    Publication date: May 17, 2012
    Applicant: E.I. Du Pont de Nemours and Company
    Inventors: Caleb William Holyoke, JR., Wenming Zhang, kanu Maganbhai Patel, George Philip Lahm, My-Hanh Thi Tong
  • Publication number: 20120121540
    Abstract: 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: Application
    Filed: August 8, 2008
    Publication date: May 17, 2012
    Inventors: 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
  • Publication number: 20120115725
    Abstract: A synergistic antimicrobial composition containing flumetsulam and thiabendazole.
    Type: Application
    Filed: November 4, 2011
    Publication date: May 10, 2012
    Inventor: Emerentiana Sianawati
  • Publication number: 20120115888
    Abstract: A synergistic antimicrobial composition containing flumetsulam or diclosulam; and diiodomethyl-p-tolylsulfone.
    Type: Application
    Filed: November 4, 2011
    Publication date: May 10, 2012
    Inventor: Emerentiana Sianawati
  • Publication number: 20120115887
    Abstract: 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: Application
    Filed: October 31, 2011
    Publication date: May 10, 2012
    Inventor: Emerentiana Sianawati
  • Publication number: 20120108595
    Abstract: 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: Application
    Filed: June 28, 2010
    Publication date: May 3, 2012
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Publication number: 20120101112
    Abstract: 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: Application
    Filed: March 30, 2010
    Publication date: April 26, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dorte Strøbæk, Palle Christophersen
  • Publication number: 20120095025
    Abstract: 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: Application
    Filed: March 30, 2010
    Publication date: April 19, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Dorte Strøbæk, Palle Christophersen
  • Publication number: 20120088665
    Abstract: 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: Application
    Filed: June 11, 2010
    Publication date: April 12, 2012
    Applicant: BASF SE
    Inventors: Jochen Dietz, Thomas Grote, Egon Haden, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glättli, Marianna Vrettou-Schultes, Wassilios Grammenos
  • Publication number: 20120088780
    Abstract: 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: Application
    Filed: March 30, 2010
    Publication date: April 12, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dorte Strøbaek, Palle Christophersen
  • Patent number: 8148383
    Abstract: 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: Grant
    Filed: January 29, 2010
    Date of Patent: April 3, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuyoshi Maekawa, Hideyuki Igawa
  • Publication number: 20120077810
    Abstract: 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: Application
    Filed: March 29, 2010
    Publication date: March 29, 2012
    Inventors: 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
  • Publication number: 20120070421
    Abstract: 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: Application
    Filed: May 31, 2010
    Publication date: March 22, 2012
    Applicant: BASF SE
    Inventors: Jochen Dietz, Egon Haden, Thomas Grote, Markus Gewehr, Silke Stoltz
  • Publication number: 20120071417
    Abstract: 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: Application
    Filed: November 10, 2009
    Publication date: March 22, 2012
    Inventors: Tso-pang Yao, Hitoshi Sasajima, Yoshiharu Kawaguchi, Kai Cui, Chun-Hsiang Lai
  • Patent number: 8133897
    Abstract: This invention is directed to phenylimidazole compounds, which are PDE10A enzyme inhibitors useful for the treatment of neurological and psychiatric disorders.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: March 13, 2012
    Assignee: H. Lundbeck A/S
    Inventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn
  • Publication number: 20120041003
    Abstract: 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: Application
    Filed: October 20, 2011
    Publication date: February 16, 2012
    Applicant: Abbott Laboratories
    Inventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
  • Publication number: 20120035050
    Abstract: 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: Application
    Filed: March 25, 2009
    Publication date: February 9, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Peter Jeschke, Robert Velten, Heike Hungenberg, Wolfgang Thielert
  • Publication number: 20120035135
    Abstract: 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: Application
    Filed: December 22, 2009
    Publication date: February 9, 2012
    Applicant: Bayer CropScience AG
    Inventors: Wolfram Andersch, Heike Hungenberg, Bernd Springer, Stefan Sachau, Casper Isaak Rooijen
  • Publication number: 20120034315
    Abstract: 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: Application
    Filed: April 19, 2010
    Publication date: February 9, 2012
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Mary Ann Hanagan, Matthew Richard Oberholzer, Robert James Pasteris, Rafael Shapiro
  • Patent number: 8110580
    Abstract: 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: Grant
    Filed: September 13, 2007
    Date of Patent: February 7, 2012
    Assignee: Eli Lilly and Company
    Inventors: Zhaogen Chen, Shaojuan Jia, James Lee Toth
  • Publication number: 20120015910
    Abstract: 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: Application
    Filed: September 23, 2011
    Publication date: January 19, 2012
    Applicant: Bayer CropScience AG
    Inventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
  • Publication number: 20120004203
    Abstract: 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: Application
    Filed: December 29, 2009
    Publication date: January 5, 2012
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
  • Publication number: 20110319432
    Abstract: 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: Application
    Filed: March 8, 2010
    Publication date: December 29, 2011
    Applicant: BASF SE
    Inventors: Markus Gewehr, Ulf Groeger, Egon Haden, Michael Vonend
  • Patent number: 8076344
    Abstract: 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: Grant
    Filed: April 30, 2008
    Date of Patent: December 13, 2011
    Assignee: Abbott Laboratories
    Inventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
  • Patent number: 8071506
    Abstract: 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: Grant
    Filed: April 14, 2010
    Date of Patent: December 6, 2011
    Assignee: Dow AgroSciences LLC
    Inventors: Daniel L. Loughner, Randy L. Smith, Michael W. Melichar
  • Publication number: 20110288087
    Abstract: 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: Application
    Filed: January 29, 2010
    Publication date: November 24, 2011
    Inventors: Tsuyoshi Maekawa, Hideyuki Igawa
  • Publication number: 20110281859
    Abstract: 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: Application
    Filed: December 22, 2009
    Publication date: November 17, 2011
    Applicant: Merck Patent Gesellschaft MIT Beschrankter Haftung
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Kai Schiemann
  • Publication number: 20110244020
    Abstract: 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: Application
    Filed: April 1, 2011
    Publication date: October 6, 2011
    Applicant: 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
  • Publication number: 20110245275
    Abstract: 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: Application
    Filed: October 16, 2009
    Publication date: October 6, 2011
    Inventor: David Reed Helton
  • Publication number: 20110237575
    Abstract: 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: Application
    Filed: November 10, 2009
    Publication date: September 29, 2011
    Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Abdelghani Abe Achab, Peter Orth, Johannes H. Voigt, Kyle Ann Soucy
  • Publication number: 20110229484
    Abstract: 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: Application
    Filed: September 18, 2009
    Publication date: September 22, 2011
    Applicant: INSERM (Institut National de la Sant et de la Recherche Medicale)
    Inventors: Thomas Baumert, Joachim Lupberger
  • Publication number: 20110224198
    Abstract: 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: Application
    Filed: November 19, 2009
    Publication date: September 15, 2011
    Inventors: Scott D. Kuduk, Douglas C. Beshore, ChristinaNg Di Marco, Thomas J. Greshock
  • Patent number: 8012973
    Abstract: 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: Grant
    Filed: October 10, 2006
    Date of Patent: September 6, 2011
    Assignee: Proyecto de Biomedicina Cima S.L.
    Inventors: Rafael Franco Fernández, Franciso Ciruela Alférez, Carmen Lluís Biset, Christa Müller, Joan Cinca Cuscullola, Leif Hove-Madsen
  • Publication number: 20110207736
    Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.
    Type: Application
    Filed: December 22, 2010
    Publication date: August 25, 2011
    Inventors: Nathanael S. GRAY, Wenjun Zhou
  • Publication number: 20110190269
    Abstract: 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: Application
    Filed: January 24, 2011
    Publication date: August 4, 2011
    Inventors: Karlheinz Baumann, Erwin Goetschi, Luke Green, Synese Jolidon, Henner Knust, Anja Limberg, Thomas Luebbers, Andrew Thomas
  • Publication number: 20110178078
    Abstract: 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: Application
    Filed: October 6, 2009
    Publication date: July 21, 2011
    Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Yan Lavrovsky, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
  • Publication number: 20110165183
    Abstract: 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: Application
    Filed: July 31, 2009
    Publication date: July 7, 2011
    Applicant: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar