Two Double Bonds Between Ring Members Of The Five-membered Hetero Ring (e.g., Pyrrole, Etc.) Patents (Class 514/427)
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Patent number: 7906501Abstract: Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.Type: GrantFiled: April 27, 2005Date of Patent: March 15, 2011Assignee: Rottapharm S.p.A.Inventors: Francesco Makovec, Roberto Artusi, Antonio Giordani, Simona Zanzola, Lucio Claudio Rovati
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Publication number: 20110053974Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.Type: ApplicationFiled: September 29, 2010Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
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Publication number: 20110044898Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.Type: ApplicationFiled: December 2, 2008Publication date: February 24, 2011Applicant: University of SydneyInventors: Michael Kassiou, Michelle Louise James, Christopher Andrew Luus
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Publication number: 20110039908Abstract: Small molecules are used to inhibit specific receptor-ligand interaction between Alzheimer's amyloid-? peptide (A?) and Receptor for Advanced Gly-cation Endproducts (RAGE). Objectives include treating Alzheimer's disease and other pathologies involving cerebral amyloid angiopathy; improving blood flow to or within the brain; decreasing the level of A? in the brain; reducing neuropathology associated with Alzheimer's disease; reducing inflammation and/or oxidant stress in the brain; improving memory and/or learning; treating other conditions involving A?/RAGE interaction at the blood-brain barrier, RAGE-mediated transport of A? into the brain, or RAGE activation in brain vasculature and/or brain parenchyma (e.g., diabetic complications); or any combination thereof.Type: ApplicationFiled: January 26, 2007Publication date: February 17, 2011Inventors: Berislav V. Zlokovic, Rashid Deane, Benjamin L. Miller
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Publication number: 20110028500Abstract: Combinations, compositions and methods of use for modulating plant pathogen infection using plant extracts containing anthraquinone derivatives which induce resistance to plant phytopathogens and an antimicrobial agent, a biological control agent and/or a surfactant having fungicidal activityType: ApplicationFiled: July 29, 2010Publication date: February 3, 2011Applicant: Marrone Bio Innovations, Inc.Inventors: Hai Su, Marja Koivunen, Pamela G. Marrone
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Publication number: 20110028468Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: ApplicationFiled: April 20, 2009Publication date: February 3, 2011Applicant: Shinonogi & Co., LtdInventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka, Takayuki Okuno, Hiroshi Yari, Keisuke Tonogaki, Naoki Kouyama
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20110002998Abstract: A process for the production of insecticide-modified bead material composed of expandable polystyrene (EPS) by extrusion, encompassing the steps of a) mixing, in a mixer, to incorporate a blowing agent and at least one insecticide from the group of the phenylpyrazoles, chlorfenapyr and hydramethylnon into a polymer melt which comprises at least one polystyrene, based on a vinylaromatic monomer, b) discharging the polymer melt comprising blowing agent, and c) pelletizing the polymer melt comprising blowing agent.Type: ApplicationFiled: December 5, 2008Publication date: January 6, 2011Applicant: BASF SEInventors: Michael Ishaque, Olaf Kriha, Carsten Schips, Norbert Güntherberg, Daniela Longo, Klaus Hahn, Bernhard Schmied, Clark D. Klein, Keith A. Holmes
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Publication number: 20100305056Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.Type: ApplicationFiled: November 26, 2008Publication date: December 2, 2010Applicant: Merck Frosst Canada Ltd.Inventors: Elise Isabel, Christophe Mellon, Christian Beaulieu
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Patent number: 7833996Abstract: The present invention relates to an insecticidal composition comprising i) zeta cypermethrin and ii) a granular fertilizer, and a method for controlling rice water weevil comprising applying an effective amount of the composition to a rice field prior to flooding.Type: GrantFiled: December 21, 2006Date of Patent: November 16, 2010Assignee: FMC CorporationInventors: John C. Braun, Jr., Henry R. Mitchell, Robert M. Herrick, D. Craig Heim, Henry Stefanski
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Publication number: 20100286174Abstract: Treatment of myocardial infarction to reduce infarct size and organogenesis is provided by administration of agents selected from the group consisting ofType: ApplicationFiled: May 18, 2010Publication date: November 11, 2010Applicant: Duke UniversityInventors: Jonathan S. Stamler, Howard A. Rockman
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Publication number: 20100286109Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: ApplicationFiled: July 22, 2010Publication date: November 11, 2010Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
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Publication number: 20100267726Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: DOMPE PHA.R.MA S.P.A.Inventors: Alessio MORICONI, Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Francesco Colotta
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Patent number: 7812041Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein R1 is independently hydrogen; alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1;Type: GrantFiled: July 29, 2005Date of Patent: October 12, 2010Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20100256115Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: March 18, 2010Publication date: October 7, 2010Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20100256156Abstract: The present invention provides a heterocyclic compound represented by the following formula (I), which has a glucagon antagonistic action and is useful for the prophylaxis or treatment of diabetes and the like, a compound represented by wherein ring A is an optionally substituted benzene ring and the like; Y is a nitrogen atom and the like; X is —O— and the like; R4 is a hydrogen atom and the like; R5 and R6 are each independently a hydrogen atom and the like; R1 is an optionally substituted hydrocarbon group and the like; R2 is a hydrogen atom and the like; and R3 is —(CH2)3—COOH and the like, or a salt thereof.Type: ApplicationFiled: October 31, 2008Publication date: October 7, 2010Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
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Patent number: 7790738Abstract: The present invention provides a method of treating or preventing a disorder typified by an immunodificiency (e.g. HIV), wherein the patient is administered a COX-2 inhibitor or derivative or pharmaceutically acceptable salt thereof, preferably diisopropylfluorophasphate. L-745337, rofecoxib, NS 398, SC 58125, etodolac, meloxicam, celecoxib or nimesulide, and compositions and products containing the same or use of the same in preparing medicaments and for treatment.Type: GrantFiled: July 20, 2001Date of Patent: September 7, 2010Assignee: Lauras ASInventors: Kjetil Taskén, Michel Moutschen, Souad Rahmouni-Piette, Einar Martin Aandahl, Pål Aukrust, Stig S. Frøland, Christian C. Johansson, Vidar Hansson, Jo Klaveness
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Publication number: 20100221238Abstract: Embodiments of the present invention relate to insecticidal Bacillus thuringiensis Cry1 and Cry2 polypeptides. Methods for using the polypeptides and nucleic acids of embodiments of the invention to synergistically enhance resistance of plants to insect predation are encompassed in embodiments of the present invention.Type: ApplicationFiled: January 22, 2010Publication date: September 2, 2010Applicants: PIONEER HI-BRED INTERNATIONAL, INC., E.I. DU PONT DE NEMOURS AND COMPANYInventors: JOHN L. FLEXNER, DEIRDRE M. KAPKA-KITZMAN, LISA PROCYK, BRUCE STANLEY, JIANZHOU ZHAO
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Publication number: 20100216862Abstract: Novel pyrrole derivatives are disclosed as A?42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the A?42 peptide.Type: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
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Publication number: 20100210524Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: July 21, 2008Publication date: August 19, 2010Inventors: Theresa Apelqvist, Joakim Löfstedt, Thomas Norin, Mattias Wennerstål, Xiongyu Wu, Lars Hagberg
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Patent number: 7776903Abstract: Pharmaceutical preparations containing substituted 2,5-diaminomethyl-1H-pyrrole compounds corresponding to formula I, and the use of these compounds for the production of pharmaceutical preparations and in related treatment methods.Type: GrantFiled: June 20, 2005Date of Patent: August 17, 2010Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Corinna Sundermann, Utz-Peter Jagusch, Werner Englberger, Hagen-Heinrich Hennies
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Publication number: 20100204162Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.Type: ApplicationFiled: June 26, 2008Publication date: August 12, 2010Inventors: Mary Frances Platt, Emyr Lloyd-Evans, Forbes Dennison Porter
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Publication number: 20100204228Abstract: In one embodiment, compounds of the following structure are described, wherein R1 to R7 are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.Type: ApplicationFiled: April 15, 2010Publication date: August 12, 2010Applicant: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome, Michael Anthony Marella
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Patent number: 7745481Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.Type: GrantFiled: August 13, 2004Date of Patent: June 29, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Patent number: 7723332Abstract: In one embodiment, compounds of the following structure are described, wherein R1to R7are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.Type: GrantFiled: March 4, 2008Date of Patent: May 25, 2010Assignee: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome, Michael Anthony Marella
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Patent number: 7714022Abstract: Novel pyrrole derivatives are disclosed as A?42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the A?42 peptide.Type: GrantFiled: March 27, 2008Date of Patent: May 11, 2010Assignee: Myriad Pharmaceuticals, Inc.Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
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Patent number: 7705038Abstract: 2-Phenyl-3-(1H-pyrrol-2-yl)acrylonitrile compounds useful for controlling parasites in animals and methods of treatment of parasite infestation in animals using the compounds are disclosed.Type: GrantFiled: November 16, 2005Date of Patent: April 27, 2010Assignee: Intervet, Inc.Inventors: Kevin N. Winzenberg, Simon Saubern, David G. Sawutz
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Publication number: 20100056605Abstract: The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.Type: ApplicationFiled: November 6, 2009Publication date: March 4, 2010Applicant: LEK PHARMACEUTICALS D.D.Inventors: Rok Grahek, Darko Kocjan, Andrej Bastarda, Andrej Kocijan, Matjaz Kracun
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Publication number: 20100048664Abstract: Disclosed herein is a compound represented by a formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 17, 2009Publication date: February 25, 2010Applicant: ALLERGAN, INC.Inventor: David W. Old
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Patent number: 7652062Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. These compounds are useful for contraception and hormone replacement therapy. Also provided are products containing these compounds.Type: GrantFiled: September 12, 2007Date of Patent: January 26, 2010Assignee: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome, Edward George Melenski
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Publication number: 20100016383Abstract: Compounds of formula wherein A0 is a bond or a C1-C6alkylene bridge; A1, A2 and A3 are a C1-C6alkylene bridge; D is CH or N; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is a bond or, for example, O, NH, S, SO or SR2; Q is, for example, O, S, SO or SO2; Y is, for example, O, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN or nitro; R4 is, for example, H, halogen, OH, SH, CN, nitro or C1-C6alkyl; R5 is, for example, H, CN, OH, C1-C6alkyl or C3-C8cycloalkyl; k is 1, 2 or 3 when D is nitrogen; or is 1, 2, 3 or 4 when D is CH; m is 1 or 2; E is heteroaryl which is unsubstituted or substituted—depending upon the substitutions possible on the ring—by from one to four identical or different substituents selected from R10; and R10 is, for example, halogen, CN, NO2, OH, SH or C1-C6alkyl; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free formType: ApplicationFiled: September 23, 2009Publication date: January 21, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Werner Zambach, Arthur Steiger, Peter Renold, Stephan Trah, Roger Graham Hall
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Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
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Publication number: 20090325916Abstract: Compounds of formula I or II and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I, formula II, or formula III.Type: ApplicationFiled: September 2, 2009Publication date: December 31, 2009Applicant: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Publication number: 20090326038Abstract: A method for treating an immunology-related disease. The method involves administering to a mammal in need thereof a pharmaceutically effective amount of an amino acid compound, a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof. The compound has the following formula: , wherein R1 and R2 are each hydrogen; R3 is hydrogen; R4 is C1-C2 alkyl; n is 2; X is ?N-D, wherein D is hydrogen, C1-C4 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2 or phenylene; Z is ethylene or trimethylene; R5 is unsubstituted C3-C10 cycloalkyl, unsubstituted C3-C10 aryl, or C3-C10 cycloalkyl or C6-C10 aryl substituted with 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, halogeno lower alkyl and lower alkoxy; and R6 and R7 are each hydrogen.Type: ApplicationFiled: August 12, 2009Publication date: December 31, 2009Applicant: SANKYO COMPANY, LIMITEDInventors: Takahide Nishi, Takaichi Shimozato, Futoshi Nara, Shojiro Miyazaki
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Publication number: 20090318495Abstract: Compounds of the formula (I), which are suitable for use as microbiocides, and in which A is A1, or A is A2, or A is A3, or A is A4 and B is a phenyl, naphthyl or quinolinyl group.Type: ApplicationFiled: June 14, 2007Publication date: December 24, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington
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Publication number: 20090306060Abstract: The present invention relates to a method for improving seed lot quality, seed shelf life, and seed lot retention, comprising applying to a seed within the seed lot an effective amount of a strobilurin fungicide alone, or in combination with at least one additional fungicide. In a preferred embodiment, the additional fungicide is at least one phenylpyrrole type fungicide and/or at least one phenylpyrrole type fungicide.Type: ApplicationFiled: December 7, 2005Publication date: December 10, 2009Applicant: Syngenta Crop Protection, Inc.Inventor: Clifford Watrin
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Publication number: 20090298905Abstract: This invention is related to new nitrogenated trans-stilbene analog compounds, more specifically, imine, pyrrol and Indole derivatives, with procedures for the preparation and use thereof as pharmaceutical compositions for the treatment and/or chemoprevention of those mammalian diseases such as cancer, fibrosclerosis and acute/chronic inflammation, graft-versus-host reaction, ischemic-reperfusion tissue injury in stroke and heart attack, neurodegeneration, and during organ transplantation, whose pathogenic and pathophysiological mechanisms depend on or are significantly contributed by undesirable oxidative stress, angiogenic and proliferative responses.Type: ApplicationFiled: April 12, 2006Publication date: December 3, 2009Inventors: Fernando Pedro Cossio, Eneko Aldaba Arevalo, Yosu Ion Vara Salazar, Aizpea Zubia Olascoaga, Silvia Vivanco Amato, Miren Lorea Mendoza Arteche, Clarisa Salado Pogonza, Natalia Gallot Escobal, Fernando Vidal Vanaclocha
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Patent number: 7625949Abstract: The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein.Type: GrantFiled: April 22, 2005Date of Patent: December 1, 2009Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Donald Roy Hirschfeld, Tania Silva, Zachary Kevin Sweeney, Harit Vora
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Patent number: 7619097Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: GrantFiled: June 24, 2008Date of Patent: November 17, 2009Assignee: Magnesium Diagnostics, Inc.Inventor: Ibert Clifton Wells
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Patent number: 7618995Abstract: The invention relates to compounds having formula (I): Wherein X, R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to the preparation method thereof and the use of same in therapeutics.Type: GrantFiled: December 7, 2007Date of Patent: November 17, 2009Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
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Patent number: 7608633Abstract: The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.Type: GrantFiled: February 6, 2004Date of Patent: October 27, 2009Assignee: Merckle GmbHInventors: Matthias Lehr, Joachim Ludwig
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Publication number: 20090264500Abstract: This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position-3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position-1 and -5 are variously substituted, but compounds of particular interest are those substituted in position-5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.Type: ApplicationFiled: August 3, 2006Publication date: October 22, 2009Inventors: Andrea Cappelli, Maurizio Anzini, Mariangela Biava, Francesco Makovec, Antonio Giordani, Gianfranco Caselli, Lucio Claudio Rovati
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Publication number: 20090253768Abstract: Pyrrole derivatives are disclosed as agents for the treatment and prevention of neuropathies and neurodegenerative diseases characterized by the presence of axonal blockages, impaired axonal transport or impaired trafficking of vesicles in neurons.Type: ApplicationFiled: March 9, 2009Publication date: October 8, 2009Applicant: Myriad Genetics, IncorporatedInventors: Christine Klein, Andrew Gassman, Leena Bhoite, John Manfredi
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Publication number: 20090253670Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: ApplicationFiled: March 26, 2009Publication date: October 8, 2009Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
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Publication number: 20090253675Abstract: The instant invention provides a pharmaceutical composition comprised of a cholesterol absorption inhibitor and an HMG-CoA reductase inhibitor, one or more anti-oxidants, microcrystalline cellulose, hydroxypropyl methylcellulose, magnesium stearate and lactose. The composition need not contain ascorbic acid in order to obtain desirable stability.Type: ApplicationFiled: May 26, 2009Publication date: October 8, 2009Inventor: Wing-Kee Philip Cho
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Publication number: 20090232886Abstract: Pharmaceutical fixed dose combination products are formed by merging a fixed dose of a first pharmaceutical formulation from primary module, with a fixed dose of a second pharmaceutical formulation from a secondary module In a preferred embodiment the first and second pharmaceutical formulations are separated from one another in a three piece capsule, a capsule-in-a-capsule or a tablet-in-a-capsule, and the primary and secondary modules are interchangeable.Type: ApplicationFiled: May 22, 2009Publication date: September 17, 2009Inventor: Raymundo A. Sison
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Publication number: 20090162442Abstract: The present invention discloses a pharmaceutical formulation containing a multi-phasic pharmaceutical composition in an oral dosage form. The multi-phasic pharmaceutical composition contains: (a) a fibrate, or a pharmaceutically acceptable salt, ester, hydrate, or prodrug thereof; (b) a statin, or a pharmaceutically acceptable salt, ester, hydrate, or prodrug thereof; (c) a solvent; (d) a non-miscible liquid; (e) a stabilizer; and (f) water. The fibrate or the statin or both is in a particulate state and/or a solubilized state. Such pharmaceutical formulations are capable of reducing the fed/fast variability and improving oral bioavailability to which a number of active pharmaceutical ingredients are susceptible. The pharmaceutical formulations of the invention, therefore are bioequivalent in fed and fasted states and have improved oral bioavailability.Type: ApplicationFiled: September 8, 2008Publication date: June 25, 2009Inventors: Dinesh B. Shenoy, Robert Lee
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Patent number: 7550491Abstract: The present invention relates to salts comprising bis(trifluoromethyl)imide anions and saturated, partially or fully unsaturated, heterocyclic cations, to a process for the preparation thereof, and to the use thereof as ionic liquids.Type: GrantFiled: November 17, 2003Date of Patent: June 23, 2009Assignee: Merck Patent GmbHInventors: Nikolai Ignatyev, Urs Welz-Biermann, Michale Schmidt, Helge Willner, Andriy Kucheryna