Plural Chalcogens Bonded Directly To Ring Carbons Of The Six-membered Hetero Ring Patents (Class 546/296)
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Publication number: 20130237515Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.Type: ApplicationFiled: February 28, 2013Publication date: September 12, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP
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Patent number: 8524747Abstract: The object of the present invention is to provide a pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-?B. The pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-?B contains DTCM glutarimide of the Formula (I) as an effective ingredient, thereby being able to inhibit nitric oxide (NO) production and prostaglandin production.Type: GrantFiled: June 25, 2009Date of Patent: September 3, 2013Assignee: Keio UniversityInventors: Kazuo Umezawa, Yuichi Ishikawa, Shigeru Nishiyama, Miyuki Tachibana, Ayumi Kaneda
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Patent number: 8524729Abstract: The present invention relates to a cinnamoyl compound represented by the formula (I):Type: GrantFiled: September 16, 2004Date of Patent: September 3, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshitaka Tomigahara, Kiyoshi Higashi, Junya Takahashi
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Publication number: 20130211093Abstract: Disclosed herein is a cost effective and environmentally friendly process to prepare 1-hydroxy-6-substituted pyridones from 2,6-dichloropyridine.Type: ApplicationFiled: February 8, 2013Publication date: August 15, 2013Applicant: ARCH CHEMICALS, INC.Inventor: Arch Chemicals, Inc.
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Publication number: 20130172551Abstract: The present invention relates to the preparation of carbamoylpyridone derivatives and intermediates.Type: ApplicationFiled: March 22, 2011Publication date: July 4, 2013Inventors: Steven N. Goodman, Huan Wang, Douglas Matthew Mans
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Publication number: 20130157851Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.Type: ApplicationFiled: August 18, 2011Publication date: June 20, 2013Applicant: ISAGRO S.P.A.Inventors: Marilena Gusmeroli, Lucio Filippini, Franco Pellacini, Paolo Bravini, Alexia Elmini, Matteo Santino Vazzola, Christian Badaracco
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Patent number: 8461183Abstract: The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.Type: GrantFiled: May 26, 2009Date of Patent: June 11, 2013Assignee: GenfitInventors: Christophe Masson, Karine Caumont-Bertrand
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Publication number: 20130109708Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 4, 2011Publication date: May 2, 2013Applicant: Pfizer LimitedInventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
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Publication number: 20130084346Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: April 4, 2013Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
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Patent number: 8404856Abstract: Heteroaromatic compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein ring A is: (ii-a), (ii-b), (ii-c), (ii-d), or (ii-e); and wherein n, L, M, U, X, Y, Z, RE, RF, R1, R2A, R2B, R2C, R3, R8, R9 and R10 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts and prodrugs are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts and prodrugs can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: November 14, 2008Date of Patent: March 26, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Thomas J. Tucker, Robert Tynebor, John T. Sisko, Neville Anthony, Robert Gomez, Samson M. Jolly
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Patent number: 8362239Abstract: Disclosed are an oligomer and a phthalonitrile monomer having the formulas: M is a metal or H. The value n is an integer greater than or equal to 1 for the oligomer and greater than or equal to 0 for the phthalonitrile monomer. Ar1 and Ar2 are independently selected aromatic- or heterocyclic-containing groups. Ar1, Ar2, or both are heteroaromatic or heterocyclic groups containing a nitrogen, sulfur, or oxygen heteroatom. Also disclosed are thermosets and pyrolyzed materials made from the phthalonitrile monomer.Type: GrantFiled: May 24, 2012Date of Patent: January 29, 2013Assignee: The United States of America, as represented by the Secretary of the NavyInventors: Matthew Laskoski, Teddy M Keller
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Patent number: 8349876Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: October 14, 2009Date of Patent: January 8, 2013Assignee: The University of Tennesee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20130005744Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: January 3, 2013Inventors: Scott Wolkenberg, James C. Barrow, Scott T. Harrison, B. Wesley Trotter, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao
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Publication number: 20120316200Abstract: The present invention is directed to novel phenylpyridone derivative compounds. The compounds act as a melanin concentrating hormone receptor antagonists, and can be useful in preventing, treating or acting as a remedial agent for various circular system diseases, nervous system diseases, metabolic diseases, genital diseases, respiratory diseases and digestive diseases.Type: ApplicationFiled: April 7, 2011Publication date: December 13, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Linus S. Lin, Richard Soll, Jingchao Dong, Hao Wu, Takao Suzuki, Bin Hu, Dejun Liu, Jinglai Hao, Ming Xu
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Patent number: 8323671Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: August 20, 2010Date of Patent: December 4, 2012Assignee: Akebia Therapeutics Inc.Inventors: Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Richard Masaru Kawamoto
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Patent number: 8309583Abstract: The present invention relates to desferoxamine conjugates, derivatives and analogues thereof. In particular, the present invention relates to desferoxamine conjugates, analogues and derivatives thereof, and methods for reducing levels of metals, especially iron, in a mammal. Uses of the compounds according to the invention are also provided. Compounds of the present invention may also be used to treat iron dyshomeostasis disorders, cancer, malaria and fungal infections. The compounds of the invention may be formulated into a pharmaceutical composition or packaged into kits.Type: GrantFiled: October 31, 2008Date of Patent: November 13, 2012Inventors: Rachel Codd, Liam Grant Schipanski
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Publication number: 20120270882Abstract: Provided are compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Frederich's Ataxia.Type: ApplicationFiled: July 5, 2010Publication date: October 25, 2012Applicant: APOTEX TECHNOLOGIES INC.Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yangqing Zhao, Tao Xin, Birenkumar Shah, Blaise N'zemba, Jolanta Maria Wodzinska, Maryna Premyslova
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Publication number: 20120264790Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 1, 2012Publication date: October 18, 2012Applicant: SANOFIInventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
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Publication number: 20120258924Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: June 20, 2012Publication date: October 11, 2012Applicant: INTERMUNE, INC.Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
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Publication number: 20120259094Abstract: The present invention relates generally to affinity ligands and chemical affinity ligand-matrix conjugates for use as chromatographic adsorbents and methods which utilise the adsorbents in the purification of proteins by affinity chromatography. The affinity ligand-matrix conjugates of the present invention comprise ligands of general formula (I): wherein m represents an integer from 0-2, n represents an integer from 0-6, p represents an integer from 0-4, R1 represents H or C1-3 alkyl, R2 is an optional substituent, and X is the position at which the ligand is immobilized, optionally via a linker.Type: ApplicationFiled: October 15, 2010Publication date: October 11, 2012Inventors: Milton TW Hearn, Anjali Makarand Bhagwat, William Roy Jackson, Simon John Mountford
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Patent number: 8273773Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: July 22, 2009Date of Patent: September 25, 2012Assignee: Roche Palo Alto LLCInventors: Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
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Publication number: 20120232270Abstract: Disclosed are an oligomer and a phthalonitrile monomer having the formulas: M is a metal or H. The value n is an integer greater than or equal to 1 for the oligomer and greater than or equal to 0 for the phthalonitrile monomer. Ar1 and Ar2 are independently selected aromatic- or heterocyclic-containing groups. Ar1, Ar2, or both are heteroaromatic or heterocyclic groups containing a nitrogen, sulfur, or oxygen heteroatom. Also disclosed are thermosets and pyrolyzed materials made from the phthalonitrile monomer.Type: ApplicationFiled: May 24, 2012Publication date: September 13, 2012Applicant: The Government of the United States of America, as represented by the Secretary of the NavyInventors: Matthew Laskoski, Teddy M. Keller
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Patent number: 8263604Abstract: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: March 19, 2007Date of Patent: September 11, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
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Publication number: 20120225890Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: ApplicationFiled: March 6, 2012Publication date: September 6, 2012Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, David Larsen, David L. Coffen, Charlotte Coffen
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Publication number: 20120225891Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: ApplicationFiled: March 22, 2012Publication date: September 6, 2012Applicant: MITSUI CHEMICALS, INC.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Patent number: 8252782Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).Type: GrantFiled: December 18, 2009Date of Patent: August 28, 2012Assignee: Pfizer Inc.Inventors: Steven Joseph Brickner, Mark Edward Flanagan, Manjinder Singh Lall
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Publication number: 20120202781Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: ApplicationFiled: April 8, 2010Publication date: August 9, 2012Inventors: Kevin James Gillen, Jonathan Gillespie, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
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Publication number: 20120196900Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: ApplicationFiled: April 16, 2012Publication date: August 2, 2012Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Publication number: 20120196901Abstract: The present invention is directed to tertiary amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 22, 2010Publication date: August 2, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
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Publication number: 20120190684Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: ApplicationFiled: July 22, 2011Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Patent number: 8222403Abstract: Disclosed are an oligomer and a phthalonitrile monomer having the formulas: M is a metal or H. The value n is an integer greater than or equal to 1 for the oligomer and greater than or equal to 0 for the phthalonitrile monomer. Ar1 and Ar2 are independently selected aromatic- or heterocyclic-containing groups. Ar1, Ar2, or both are heteroaromatic or heterocyclic groups containing a nitrogen, sulfur, or oxygen heteroatom. Also disclosed are thermosets and pyrolyzed materials made from the phthalonitrile monomer.Type: GrantFiled: November 12, 2009Date of Patent: July 17, 2012Assignee: The United States of America, as represented by the Secretary of the NavyInventors: Matthew Laskoski, Teddy M Keller
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Publication number: 20120177634Abstract: This disclosure concerns novel demethylpenclomedine analogs. Also disclosed are pharmaceutical compositions and methods for using such compositions to treat hyperproliferative disorders.Type: ApplicationFiled: February 22, 2012Publication date: July 12, 2012Inventor: Lee Roy Morgan
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Patent number: 8183266Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.Type: GrantFiled: June 4, 2008Date of Patent: May 22, 2012Assignee: Intra-Cellular Therapies, Inc.Inventors: Lawrence P. Wennogle, Peng Li, Jun Zhao
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Publication number: 20120094232Abstract: There is provided a simple production method of a polyhydroxyimide. A production method of a polyhydroxyimide, characterized by comprising adding to a polyhydroxyimide precursor containing a repeating structure of Formula (1): in which X is a tetravalent aliphatic group or aromatic group, Y is an organic group containing an aromatic group substituted with at least one OH group, and n is an integer of 1 or more, at least a compound of Formula (2) or Formula (3): in which R1 to R4 or R5 to R8 are independently a hydrogen atom or a monovalent organic group, and m is a natural number, and heating the resultant reaction mixture at a temperature of 50° C. or more to obtain a polyimide having a weight average molecular weight measured by gel permeation chromatography (GPC) in terms of polystyrene of 5,000 to 100,000.Type: ApplicationFiled: April 22, 2010Publication date: April 19, 2012Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventor: Kazuya Ebara
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Patent number: 8158654Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: May 19, 2009Date of Patent: April 17, 2012Assignee: The University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
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Patent number: 8158804Abstract: The present invention relates to chelating agents, in particular to chelating agents which are capable of forming complexes with paramagnetic metal ions such as iron (III) and gadolinium (III). The invention also relates to the complexes formed and their use as MRI contrast agents.Type: GrantFiled: January 11, 2008Date of Patent: April 17, 2012Assignee: GE Healthcare ASInventors: Harry John Wadsworth, Ian Martin Newington, Clare L. Jones, Amanda Ewan, Dennis O'Shea
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Publication number: 20120077852Abstract: The application of hydroxypyridonone in effective amounts as external agent for patients suffering from skin micro-circulatory disorders (SMD) provides for a significant amelioration of subject conditions. Accordingly, the new use of hydroxypyridonones as external anti-inflammatory agent thereby combined with the depletion of hemosiderin residues offers a suitable treatment to SMD sufferers.Type: ApplicationFiled: December 1, 2011Publication date: March 29, 2012Inventor: Ghisalberti CARLO
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Publication number: 20120071465Abstract: The present invention relates to the compounds useful in the prevention and/or treatment of tumours. More specifically the present invention relates to inhibitors of the activity of the electron transport chains and/or the mitochondrial TCA cycle in glioma-initiating cells (GICs) for use in a method for preventing and/or treating tumours presenting glioma-initiating cells (GICs) in a subject who has undergone a prior removal of a tumour glioma bulk. The present invention further provides a pharmaceutical composition containing the inhibitors of the invention and a screening method for identifying the inhibitors of the invention.Type: ApplicationFiled: May 20, 2010Publication date: March 22, 2012Inventors: Virginie Clement, Ivan Radovanovic
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Publication number: 20120022251Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.Type: ApplicationFiled: March 26, 2010Publication date: January 26, 2012Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
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Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Publication number: 20120010185Abstract: The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U, V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk STENKAMP, Stephan Georg MUELLER, Gerald Juergen ROTH, Joerg KLEY, Klaus RUDOLF, Armin HECKEL, Marcus SCHINDLER, Ralf LOTZ, Thorsten LEHMANN-LINTZ
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Publication number: 20120004349Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.Type: ApplicationFiled: March 9, 2010Publication date: January 5, 2012Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
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Publication number: 20110319347Abstract: Disclosed is an antioxidant which can exhibit a higher antioxidant ability than known antioxidative peptides. The antioxidant according to the present invention comprises mimosine and/or a mimosine-containing peptide(s). The mimosine-containing peptide is a peptide which comprises at least one mimosine residue in its amino acid sequence. Mimosine has stronger antioxidant potency than known antioxidative tripeptides even when used as it is alone, and therefore is useful as an antioxidant. In addition, the antioxidant action of a peptide can be increased by introducing mimosine thereinto, thereby obtaining a peptide with higher antioxidant potency than the original one.Type: ApplicationFiled: March 11, 2010Publication date: December 29, 2011Inventors: Kiyoshi Nokihara, Naeko Miyazato
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Publication number: 20110294800Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.Type: ApplicationFiled: August 7, 2009Publication date: December 1, 2011Applicant: The Trustees Of Columbia University in the City of New YorkInventors: Yuli Xie, Shixian Deng, Donald W. Landry, Paul Harris, Antonella Maffei
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Publication number: 20110294783Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: August 10, 2011Publication date: December 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
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Publication number: 20110263855Abstract: Processes are provided which create an aldehyde methylene, or hydrated or hemiacetal methylene attached to a heteroatom of a 6 membered ring without going through an olefinic group and without the necessity of using an osmium reagent. In particular, a compound of formula (I) can be produced from (II) and avoid the use of an allyl amine: (formulae I and II) where R, P1P3, R3 and Rx are as described herein.Type: ApplicationFiled: December 9, 2009Publication date: October 27, 2011Applicants: SHIONOGI & CO., LTD., GLAXOSMITHKLINE LLCInventors: Brian Alvin Johns, Maosheng Duan, Toshikazu Hakogi
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Publication number: 20110245227Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.Type: ApplicationFiled: June 14, 2011Publication date: October 6, 2011Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Patent number: 8030316Abstract: The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R1-R4 are each independently selected from the group consisting of hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, and di-C1-C6-alkylamino-C2-C6-alkoxy. The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.Type: GrantFiled: June 17, 2010Date of Patent: October 4, 2011Assignee: Biovitrum AB (Publ)Inventors: Tom Fleck, Bruce Fleck, legal representative, Magnus Cernerud, Helena Lundström, Claes Löfström, Margit Pelcman, Alexander Paptchikhine, Emma Andersson, Alf Nygren
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Patent number: 8026261Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.Type: GrantFiled: March 27, 2008Date of Patent: September 27, 2011Assignee: Apotex Technologies Inc.Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao