Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/245)
-
Publication number: 20090053192Abstract: Disclosed herein are tissue-nonspecific alkaline phosphatase (TNAP) activators and uses thereof for promoting bone mineral deposition.Type: ApplicationFiled: August 9, 2008Publication date: February 26, 2009Applicant: BURNHAM INSTITUTE FOR MEDICAL RESEARCHInventors: Jose Luis Millan, Eduard Sergienko
-
Publication number: 20090041751Abstract: Methods for treating sepsis or septic shock in a patient comprising administering to said patient a therapeutically effective amount of a composition containing an adenosine A2a receptor antagonist.Type: ApplicationFiled: February 1, 2006Publication date: February 12, 2009Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Gyorgy Hasko, Zoltan Nemeth, David Bleich, Edwin Deitch
-
Patent number: 7485654Abstract: The amide compound of the formula (I) [each symbol is as defined in the description] has a promoting action on neuritogenesis of trigeminal nerve cells, and the compound is useful as a corneal neuritogenesis promoter, an agent for recovering corneal sensitivity by promotion of corneal neuritogenesis, and an agent for treating dry eye.Type: GrantFiled: June 3, 2005Date of Patent: February 3, 2009Assignees: Senju Pharmaceutical Co., Ltd., Mitsubishi Tanabe Pharma CorporationInventors: Yoshiko Takayama, Yoshikuni Nakamura, Jun Inoue, Mitsuyoshi Azuma
-
Patent number: 7485641Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.Type: GrantFiled: June 18, 2007Date of Patent: February 3, 2009Assignee: Pfizer, Inc.Inventors: David W. Piotrowski, Yu Hui, John W. Benbow
-
Publication number: 20090030001Abstract: A therapeutic agent for a corneal disease comprising irsogladine or a salt thereof as an active ingredient. The purpose is to find a substance capable of effectively treating/ameliorating a corneal disease which has been increased in the number of cases thereof in recent years and to provide a therapeutic agent for a corneal disease comprising the substance as an active ingredient.Type: ApplicationFiled: April 27, 2006Publication date: January 29, 2009Applicant: TEIKA PHARMACEUTICAL CO., LTD.Inventors: Takahito Kimura, Shigeto Fujishita, Hiroyoshi Kawada
-
Publication number: 20090029993Abstract: Methods and compounds are disclosed for affecting gastrointestinal motility and gastric emptying, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.Type: ApplicationFiled: July 17, 2008Publication date: January 29, 2009Inventors: Qingyun Liu, Brian Zambrowicz
-
Publication number: 20090023727Abstract: A compound of the formula (I): wherein: R represents one or more optional substituents on the fused cyclohexene ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; if X=NRX, then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted ester, optionally substituted acyl, and optionally substituted sulfonyl groups; if X=CRXRY then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted sulfonamino, optionally substituted ether, optionally substituted ester, optionally substituted acyl, optionally substituted acylamido, and optionally substituted sulfonyl groups and RY is selected from H, hydroxy, optType: ApplicationFiled: July 3, 2008Publication date: January 22, 2009Inventors: Muhammad Hashim Javaid, Keith Allan Menear, Niall Morrison Barr Martin, Graeme Cameron Murray Smith, David Alan Rudge, Craig Anthony Roberts
-
Publication number: 20090005381Abstract: Methods are disclosed for treating serotonin-mediated diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.Type: ApplicationFiled: June 24, 2008Publication date: January 1, 2009Inventors: Philip Manton Brown, Qingyun Liu, Brian Zambrowicz
-
Publication number: 20090005382Abstract: Methods and compositions comprising tryptophan hydroxylase inhibitors are disclosed. Particular methods are directed at reducing or avoiding serotonin-mediated adverse effects associated with some drugs.Type: ApplicationFiled: June 24, 2008Publication date: January 1, 2009Inventors: Philip Manton Brown, Qingyun Liu
-
Patent number: 7470695Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: March 31, 2006Date of Patent: December 30, 2008Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
-
Patent number: 7468372Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: March 31, 2006Date of Patent: December 23, 2008Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Chad Knutson, Brian McKittrick, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
-
Publication number: 20080305137Abstract: The invention relates to a coating material for protection against microorganism invasion on surfaces which are exposed to the effects of damp or water. The coating material has either a pH-value of at least 11.0 or is provide with a base material for the coating whereby the pH-value is at least 11. The coating material is characterized in that it contains a biocide which bonds to solid particles in a carrier material and is released in a delayed manner therefrom.Type: ApplicationFiled: August 14, 2008Publication date: December 11, 2008Inventors: Rudiger Baum, Dagmar Antoni-Zimmermann, Thomas Wunder, Hans-Jurgen Schmidt
-
Publication number: 20080305102Abstract: Inhibition of synoviolin function was found to activate the cancer-suppressing protein p53. Substances inhibiting the function of synoviolin are useful as cancer therapeutic agents. The inhibition of synoviolin function was also found to lead to the inhibition of p53 ubiquitination, increased activity of p53 phosphorylation proteins, and the like. Based on these findings, the present invention provides methods capable of efficiently screening for cancer therapeutic agents. Further, it was also found that regulation of the autoubiquitination of synoviolin protein suppresses the proliferation of rheumatoid arthritis synovial cells. Substances regulating the autoubiquitination of synoviolin protein are useful as anti-rheumatic agents. Moreover, the present invention provides methods of efficiently screening for anti-rheumatic agents.Type: ApplicationFiled: June 23, 2006Publication date: December 11, 2008Inventors: Toshihiro Nakajima, Yukihiro Kato, Tadayuki Yamadera, Tetsuya Amano
-
Publication number: 20080305055Abstract: Compounds of the formulae (1), (2) and selected hindered nitroxyl, hydroxylamine and hydroxylamine salt compounds such as the compound of formula (3), wherein Gi is hydrogen; C1-C22alkyl; C1-C22alkylthio; C2-C22alkylthioalkyl; C5-C7cycloalkyl; phenyl; C7-C9phenylalkyl; or SO3M; G2 is C1-C22alkyl; C5-C7cycloalkyl; phenyl; or C7-C9phenylalkyl; E is oxyl or hydroxyl; V is —O—; or —NH—; a is 0 or 1 or 2; b, c and d and g are each independently of one another 0 or 1; e is an integer from 1 to 4; f, m, n and p are each independently of one another an integer from 1 to 3; q is 0 or an integer from 1 to 3; Q, T and G3 are as defined in claim 1; G4 and G5 are each independently of the other hydrogen; or C1-C22alkyl; exhibit marked antiinflammatory action.Type: ApplicationFiled: October 24, 2005Publication date: December 11, 2008Inventors: Werner Baschong, Oliver Reich, Sebastien Mongiat
-
Patent number: 7462617Abstract: The invention relates to compounds of formula wherein the substituents are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention further relates to methods for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other d 1iseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: GrantFiled: September 1, 2004Date of Patent: December 9, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
-
Publication number: 20080287445Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for the treatment of prokineticin 2 or prokinetin 2 receptor mediated disorders.Type: ApplicationFiled: December 28, 2006Publication date: November 20, 2008Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara Miskowski, Janet L. Ralbovsky, Mark Schulz
-
Publication number: 20080287444Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: ApplicationFiled: April 25, 2008Publication date: November 20, 2008Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
-
Patent number: 7452883Abstract: The invention concerns compounds of general formula (I) wherein: R1, R2, R3, R4, R5 and R6 are as defined in Claim 1. The compounds are useful in the treatment of pathologies related to the insulin-resistance syndrome.Type: GrantFiled: March 22, 2005Date of Patent: November 18, 2008Assignee: Merck SanteInventors: Gerard Moinet, Daniel Cravo, Liliane Doare, Micheline Kergoat, Didier Mesangeau
-
Publication number: 20080275049Abstract: A novel method of identifying compounds capable of upregulating GATA activity is disclosed. The method includes providing a sample of cells that express GATA, providing a sample of a candidate compound, contacting the cell sample and the compound sample, and measuring a quantitative indicator of GATA activity within the cell sample after the contacting step. GATA inducers identified by the method and uses therefore to upregulate GATA activity in subjects and to prevent or treat atherosclerosis or diabetes in subjects are also described.Type: ApplicationFiled: May 1, 2008Publication date: November 6, 2008Applicant: REDDY US THERAPEUTICS, INC.Inventors: John Anastasios Polikandriotis, Sivaram Pillarisetti, Ish Khanna, Uday Saxena
-
Publication number: 20080269225Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.Type: ApplicationFiled: December 28, 2006Publication date: October 30, 2008Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara Miskowski, Janet L. Ralbovsky, Mark Schulz
-
Publication number: 20080269224Abstract: Compounds of formula (I) wherein R1 and R2 are the same or different and are each optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl groups; R3 is hydrogen or an aryl group substituent or R3 is a solid support optionally attached via a spacer; Z represents an oxygen atom, a sulphur atom or NR4; Y represents an oxygen atom, a sulphur atom or NR5; in which R4 and R5, which may be the same or different, represent hydrogen, optionally substituted alkyl containing 1 to 6 carbon atoms, optionally substituted phenyl, optionally substituted benzyl or optionally substituted ?-phenylethyl; and one of X1 and X2 represents a nitrogen atom and the other of X1 and X2 represents a nitrogen atom or CR6, in which R6 represents hydrogen or an aryl group substituent; are useful for the affinity binding of a prion protein.Type: ApplicationFiled: July 25, 2005Publication date: October 30, 2008Applicant: PROMETIC BIOSCIENCES LIMITEDInventors: James Christopher Pearson, Helen Rosemary Tatton, Patrick Vasconcelos Gurgel
-
Publication number: 20080261953Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihy-dropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.Type: ApplicationFiled: September 16, 2005Publication date: October 23, 2008Applicants: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH, FOLDRX PHARMACEUTICALS, INC.Inventors: Susan L. Lindquist, Tiago Outeiro, Richard Labaudiniere
-
Publication number: 20080260829Abstract: This invention relates to BMP fusion genes, BMP fusion proteins. The invention further relates to methods for treatment using BMP fusion genes and BMP fusion proteins. Additionally, the invention relates to BMP fusion gene and BMP fusion protein pharmaceutical compositions.Type: ApplicationFiled: October 26, 2005Publication date: October 23, 2008Applicant: New YORK Society for the Ruptured and Crippled Maintaining The Hospital for Special SurgeryInventors: Chisa Hidaka, Wei Zhu
-
Publication number: 20080255127Abstract: Pesticide formulations with a crystallization risk are provided. Also provided are methods of making and using such formulations.Type: ApplicationFiled: September 25, 2006Publication date: October 16, 2008Applicant: Bayer CropScience AGInventors: Victor Casana Giner, Miguel Gimeno Sierra, Barbara Gimeno Sierra
-
Publication number: 20080255126Abstract: Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula —CH2—X2—(CH2)a-G3 and G2 is H or a group according to the formula —CH2—(CH29a-G3, provided that one of G1 and G2 is H and the other is not H. X2 is O, S, or CH2, and a is 0, 1 or 2, provided that when a is 1 then X2 is CH2. G3 is a group according to one of general formulae 2-4, where the variables have meaning given in the description. The compounds are useful in the treatment of i.a. type 2 diabetes and impaired glucose tolerance.Type: ApplicationFiled: December 20, 2007Publication date: October 16, 2008Inventors: David M. Evans, Doreen M. Ashworth
-
Publication number: 20080255136Abstract: The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.Type: ApplicationFiled: April 22, 2008Publication date: October 16, 2008Applicant: IRM LLCInventors: Baogen Wu, Yun He, Truc Nguyen, Kelli L. Kuhen, David Archer Ellis, Tao Jiang, Xiaohui He, Kunyong Yang, Badry Bursulaya
-
Publication number: 20080249097Abstract: The present invention provides hydrophobic prodrugs of bases, nucleosides, and nucleotides as well as methods of using the prodrugs as antiviral and anti-cancer chemotherapeutic agents.Type: ApplicationFiled: December 27, 2006Publication date: October 9, 2008Applicant: Koronis Pharmaceuticals, IncorporationInventors: Richard Daifuku, Alexander Gall, Dmitri Sergueev, Dina Sologub, Kevin Harris
-
Publication number: 20080234275Abstract: Compounds represented by the formula 1: wherein each R individually is H, an aliphatic acyl group or an aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, halo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro; are used to treat or prevent arthritis including rheumatoid arthritis.Type: ApplicationFiled: March 24, 2008Publication date: September 25, 2008Applicant: Southern Research InstituteInventors: John A. Secrist, William R. Waud, Zhican Qu, Xiangmin Cui
-
Publication number: 20080227785Abstract: This invention relates to an anti-dementia agent which uses a BEC 1 potassium channel inhibitor as the active ingredient. It was proved that the BEC 1 potassium channel inhibitor has an action to improve learning disorder and is useful as a preventive or therapeutic agent for diseases, preferably dementia, in which the BEC 1 potassium channel is considered to be concerned. Illustratively, it was confirmed by an in vivo test that the BEC 1 potassium channel inhibitor has an action to improve learning disorder. Also, it was found that a compound having 2,4,6-triamino-1,3,5-triazine has a BEC 1 potassium channel inhibitory action.Type: ApplicationFiled: February 6, 2008Publication date: September 18, 2008Applicant: Astellas Pharma Inc.Inventors: Hideki Kubota, Takeshi Suzuki, Masanori Miura, Eiichi Nakai, Kiyoshi Yahiro, Akira Miyake, Shinobu Mochizuki, Kazuhiro Nakatou
-
Patent number: 7425451Abstract: Compounds, compositions, methods for sequencing proteins and peptides, and methods for identifying proteins and peptides in a mixture, are disclosed. Compounds of formula A-B-C wherein A is a nucleophilic reactive group, B is a detectable moiety capable of being isotopically labeled, and C is a charge replacement group, are used to label the peptides at the N-terminus or the C-terminus. The tagged peptides can then be analyzed by mass spectroscopy.Type: GrantFiled: December 13, 2002Date of Patent: September 16, 2008Assignee: Agilent Technologies, Inc.Inventors: Karla M. Robotti, James Alexander Apffel, Jr.
-
Publication number: 20080213399Abstract: The present invention pertains to a method for treating cancer, such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount or dose of another chemotherapeutic agent, such as dexamethasone or 5-fluorouracil, or an epidermal growth factor receptor (EGFR) inhibitor, such as TarcevaÚ, wherein the first and second amounts or doses together comprise a therapeutically effective amount.Type: ApplicationFiled: February 3, 2006Publication date: September 4, 2008Applicants: TOPOTARGET UK LIMITED, CURAGEN CORPORATIONInventors: Henri Lichenstein, Mike Jeffers, Xiaozhang Qian, Maxwell Sehested, Kamille Dumong Petersen, James Ritchie
-
Publication number: 20080194545Abstract: The present invention is directed to compounds of formula I, pharmaceutical compositions comprising the compounds, and methods for making and using the inventive compounds.Type: ApplicationFiled: February 7, 2008Publication date: August 14, 2008Applicant: TRIUS THERAPEUTICSInventors: Xiaoming Li, John M. Finn, Mark T. Hilgers
-
Publication number: 20080182846Abstract: The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).Type: ApplicationFiled: February 6, 2008Publication date: July 31, 2008Applicant: BTG International LimitedInventors: Masaki Meguro, Tomichiro Oda, Yasuhiro Nakagami, Shinji Marumoto, Kazuo Koyama, Isao Kaneko
-
Publication number: 20080176853Abstract: The invention provides for Triazine derivatives and their use to modulate protein kinase activity in a variety of conditions and diseases.Type: ApplicationFiled: December 14, 2007Publication date: July 24, 2008Applicant: Abraxis BioScience, Inc.Inventors: Chunlin Tao, Qinwei Wang, Neil P. Desai, Patrick Soon-Shiong
-
Publication number: 20080175814Abstract: Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.Type: ApplicationFiled: October 12, 2007Publication date: July 24, 2008Applicant: SUPERGEN, INC.Inventors: Pasit Phiasivongsa, Sanjeev Redkar, Swarna Gamage, Darby Brooke, William Denny, David J. Bearss, Hariprasad Vankayalapati
-
Publication number: 20080176852Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.Type: ApplicationFiled: June 27, 2007Publication date: July 24, 2008Inventors: David P. Jacobus, Guy A. Schiehser, Hong-Ming Shieh, Norman P. Jensen, Jacek Terpinski
-
Publication number: 20080167302Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 12, 2004Publication date: July 10, 2008Inventors: Kelly M. Aubart, Andrew B. Benowitz, Siegfried B. Christensen IV, Jinhwa Lee, Domingos J. Silva
-
Publication number: 20080161310Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.Type: ApplicationFiled: March 5, 2008Publication date: July 3, 2008Applicant: Sanofi-AventisInventors: Peter Aranyi, Laszlo Balazs, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Karoly Kanai, Zoltan Kapui, Edit Susan, Tibor Szabo, Lajos T. Nagy, Katalin Urban-Szabo, Marton Varga
-
Publication number: 20080146574Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: February 12, 2008Publication date: June 19, 2008Inventors: Darren Whitehouse, Shaojing Hu, Haiquan Fang, Kerry Combs, Michael C. Van Zandt
-
Publication number: 20080140036Abstract: The present invention relates to a composition for use as an antimicrobial medicament comprising a biocidally active compound. The invention also relates to a medicament comprising at least one biocidally active compound and a fungal cell or fungal cell fragment wherein molecules of the at least one biocidally active compound are encapsulated or partially encapsulated by the fungal cell or fungal cell fragment.Type: ApplicationFiled: January 18, 2005Publication date: June 12, 2008Inventors: Rachael Buck, Michael Edward Donald Crothers, Gordon Nelson
-
Publication number: 20080139567Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and its use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: ApplicationFiled: February 13, 2008Publication date: June 12, 2008Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventor: Paul J. Gilligan
-
Publication number: 20080139566Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: ApplicationFiled: January 24, 2008Publication date: June 12, 2008Inventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
-
Publication number: 20080119461Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: November 5, 2007Publication date: May 22, 2008Inventors: Ny Sin, Brian Lee Venables, Li-Qiang Sun, Sing-Yuen Sit, Yan Chen, Paul Michael Scola
-
Publication number: 20080119402Abstract: The Wnt signaling pathways are involved in embryo development as well as in tumorigenesis. Dishevelled (Dvl) tranduces Wnt signals from the receptor Frizzled (Fz) to downstream components in canonical and non-canonical Wnt signaling pathways, and the Dvl PDZ domain plays an essential role in both pathways, and the Dvl PDZ domain binds directly to Fz receptors. In the present invention using NMR-assisted virtual ligand screening, several compounds were identified and were found to bind to the Dvl PDZ domain. Molecular dynamics simulation was used to analyze the binding between the PDZ domain and these compounds in detail. These compounds provide a basis for rational design of high-affinity inhibitors of the PDZ domain, which can block Wnt signaling by interrupting the Fz-Dvl interaction.Type: ApplicationFiled: April 1, 2005Publication date: May 22, 2008Inventors: Jie Zheng, Jufang Shan, Dianqing Wu
-
Patent number: 7375222Abstract: This invention relates to an anti-dementia agent which uses a BEC 1 potassium channel inhibitor as the active ingredient. It was proved that the BEC 1 potassium channel inhibitor has an action to improve learning disorder and is useful as a preventive or therapeutic agent for diseases, preferably dementia, in which the BEC 1 potassium channel is considered to be concerned. Illustratively, it was confirmed by an in vivo test that the BEC 1 potassium channel inhibitor has an action to improve learning disorder. Also, it was found that a compound having 2,4,6-triamino-1,3,5-triazine has a BEC 1 potassium channel inhibitory action.Type: GrantFiled: February 3, 2003Date of Patent: May 20, 2008Assignee: Astellas Pharma Inc.Inventors: Hideki Kubota, Takeshi Suzuki, Masanori Miura, Eiichi Nakai, Kiyoshi Yahiro, Akira Miyake, Shinobu Mochizuki, Kazuhiro Nakatou
-
Patent number: 7371398Abstract: Animals have been domesticated and kept as a source of milk for tens of thousands of years. When humans keep animals for their ability to produce milk, the animals are usually kept in confined spaces. As a result of this confinement the animals are exposed to high levels of urine and fecal matter which originated with the animals which are being kept. This exposure contaminates the animal and in particular the udder and teats of the animal, with bacteria. In the milking process this bacteria can further contaminate the milk which is destine for human consumption. The bacteria can further cause mastitis in the bovine. The above set forth problems are eliminated in the subject invention wherein the udder and teat areas of the bovine are sanitized with a solution which contains both Cl+ and I+ ions wherein the I+ ion is produced by the oxidation of a solution of a dry iodine salt, without an N-chloro organic compound. The iodine salt may be an alkali metal iodide, an exemplary oxidizer is tricholormelamine.Type: GrantFiled: September 24, 2004Date of Patent: May 13, 2008Assignee: H&S Chemical Company, Inc.Inventors: David J. Schneider, Charles A. Schneider
-
Publication number: 20080076771Abstract: A compound of the formula (I) useful as promoters of thrombopoiesis and megakaryocytopoiesis, wherein A, B, D, E, W, X, Y, Z, R1 and R2 are defined as above.Type: ApplicationFiled: September 12, 2005Publication date: March 27, 2008Inventors: Lawrence A. Reiter, Robert G. Linde
-
Patent number: 7344727Abstract: Animals have been domesticated and kept as a source of milk for tens of thousands of years, When humans keep animals for their ability to produce milk, the animals are usually kept in confined spaces. As a result of this confinement the animals are exposed to high levels of urine and fecal matter which originated with the animals which are being kept. This exposure contaminates the animal and in particular the udder and teats of the animal, with bacteria. In the milking process this bacteria can further contaminate the milk which is destine for human consumption. The bacteria can further cause mastitis in the bovine. The above set forth problems are eliminated in the subject invention wherein the udder and teat areas of the bovine are sanitized with a solution of trichloromelamine.Type: GrantFiled: December 10, 2003Date of Patent: March 18, 2008Assignee: H&S Chemical Company, Inc.Inventors: David J. Schneider, Charles A. Schneider
-
Patent number: 7335770Abstract: The present invention relates to triazine compounds and their analogs and derivatives, and methods and compositions comprising these compounds. The compounds and compositions of this invention are useful for, among other things, treating pathophysiological conditions arising from inflammatory responses, inhibiting or blocking glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells, inhibiting smooth muscle proliferation, treating vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis, and the like.Type: GrantFiled: March 24, 2004Date of Patent: February 26, 2008Assignee: Reddy U5 Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Sesha Sridevi Alluri, Velagala Venkata Rama Murali Krishna Reddy, Manojit Pal, Jangalgar Tirupathy Reddy, Koteswar Rao Yeleswarapu, Gaddam Om Reddy, Potlapally Rajender Kumar
-
Patent number: 7335656Abstract: The present invention relates to methods, compounds, and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses, and is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention also relates to compounds that inhibit smooth muscle proliferation, for example, by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis. This invention also relates to medical devices, such as a stent, comprising a compound or composition of this invention disposed on or within the medical device.Type: GrantFiled: August 30, 2006Date of Patent: February 26, 2008Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Sesha Sridevi Alluri, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Potlapally Rajender Kumar, Gaddam Om Reddy