Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/351)
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Patent number: 7994142Abstract: The invention relates to agents that contain folic acid, vitamin B6 and vitamin B12, and to the use thereof in hyperhomocysteinemia for controlling homocysteine levels. The agents are mainly suitable for the preventive and acute treatment of vascular diseases, of pregnant women and neurodegenerative diseases and are particularly advantageous in cases where the homocysteine levels to be controlled are found in an individual suffering from renal failure or being treated with immune suppressors. The invention particularly relates to pharmaceutical agents and food supplements comprising a corresponding active ingredient combination and to agents in the form of commercial packages containing corresponding combination preparations or monopreparations for the combined use.Type: GrantFiled: January 11, 2006Date of Patent: August 9, 2011Assignee: Phrontier S.A.R.L.Inventor: Martin Goerne
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Publication number: 20110189122Abstract: The subject invention relates in part to the oral administration of ecdysteroids for controlling subterranean termites. Preferred ecdysteroids for use according to the subject invention are ecdysone, certain ecdysone analogs, and 20-hydroxyecdysone, for example. In some preferred embodiments, one or more of these compounds is used in a termite bait in combination with one or more chitin synthesis inhibitors. Thus, the subject invention also relates in part to controlling termites by the use of a chitin synthesis inhibitor (CSI), such as hexaflumuron and/or noviflumuron, together with an ecdysteroid (and analogs thereof) or molt-accelerating compound (MAC), such as halofenozide. The subject invention also relates to mixtures comprising these two active ingredients. The MAC/ecdysteroid analog induces a preliminary molting event in termite workers (they could not complete the molting), which then allows the CSI to further disrupt the molt and cause mortality.Type: ApplicationFiled: April 8, 2011Publication date: August 4, 2011Inventors: Nan-Yao SU, James Edward King, Paul Allen Neese
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Publication number: 20110178139Abstract: The present invention provides pharmaceutical compositions comprising dosage units of pyridoxamine, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier, and methods for their use in limiting the progression of renal disease and/or diabetic complications in human diabetic patient.Type: ApplicationFiled: March 31, 2011Publication date: July 21, 2011Inventors: Thorsten Degenhardt, Robert Schotzinger, Wesley J. Fox
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Publication number: 20110136735Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 30, 2010Publication date: June 9, 2011Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
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Publication number: 20110136877Abstract: The present invention provides novel phenoxyacetic acids useful for the prevention and treatment of inflammatory disorders, including those affecting the respiratory system and skin.Type: ApplicationFiled: January 6, 2009Publication date: June 9, 2011Applicant: LIGAND PHARMACEUTICALS INC.Inventors: Brian F. McGuinness, Thuy X. H. Le, Jingqi Duo, Koc-Kan Ho
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Publication number: 20110130428Abstract: The present invention relates to sublingual compositions comprising (2S)-(4E)-N-methyl-5-(3-(5-iso-propoxypyridin)yl)-4-penten-2-amine or pharmaceutically acceptable salts thereof, to the preparation of said compositions and the use of thereof in therapy.Type: ApplicationFiled: June 11, 2009Publication date: June 2, 2011Applicant: ASTRAZENECA ABInventors: Anders X. Lindahl, Anders Ringberg
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Patent number: 7951972Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.Type: GrantFiled: February 2, 2009Date of Patent: May 31, 2011Assignee: Exelixis, Inc.Inventors: S. David Brown, Lynne Canne-Bannen, Erick Wang Co, Vasu Jammalamadaka, Rickard George Khoury, Moon Hwan Kim, Donna T. Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, John M. Nuss, Michael P. Prisbylla, Wei Xu
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Publication number: 20110123489Abstract: Compounds having the formula I wherein wherein R1, R2 and R3 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors with improved bioavailability. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: November 19, 2010Publication date: May 26, 2011Applicant: Roche Palo Alto LLCInventor: Joshua Paul Gergely Taygerly
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Publication number: 20110117213Abstract: The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.Type: ApplicationFiled: November 17, 2010Publication date: May 19, 2011Inventors: Kazuko MATSUDA, Yuichi Iwaki, Kirk W. Johnson
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Publication number: 20110092551Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 21, 2010Publication date: April 21, 2011Applicant: THERAVANCE, INC.Inventors: Paul ALLEGRETTI, Seok-Ki CHOI, Roland GENDRON, Paul R. FATHEREE, Keith JENDZA, Robert Murray McKINNELL, Darren McMURTRIE, Brooke OLSON
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Publication number: 20110082133Abstract: [Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided. [Means for Solution] The present inventors have conducted extensive studies on EP4 receptor agonists, and as a result, have found that a novel pyridone compound, in which a group having an acidic group is substituted at the 1-position of the pyridone ring, the 6-position is bonded with an aromatic ring group via a linking part, and the linking part contains a nitrogen atom, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action, it is useful as a pharmaceutical, in particular, as an agent for treating peripheral arterial occlusive disease.Type: ApplicationFiled: June 16, 2009Publication date: April 7, 2011Inventors: Takashi Kamikubo, Masanori Miura, Takao Okuda, Keisuke Maki, Fukushi Hirayama, Ayako Moritomo, Yuriko Komiya, Keisuke Matsuura, Ryotaro Ibuka
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Publication number: 20110065578Abstract: The present invention relates to the use of pyridin-4-ylmethyl sulfonamides of formula (I) (I) wherein Ra, n, A, Y and D are as defined in the claims and the N-oxides and the salts thereof for combating phytopathogenic harmful fungi, and and to compositions and seeds comprising at least one such compound. The invention also relates to to novel substituted sulfonic acid amide compounds and processes for preparing these compounds.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Applicant: BASF SEInventors: Wassilios Grammenos, Alice Glättli, Jan Klaas Lohmann, Bernd Müller, Marianna Vrettou
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Publication number: 20110065734Abstract: The present invention relates to a bifunctional compound of formula I or its pharmaceutically acceptable salts or solvates A-L-B (I) wherein A is a histone deacetylase (HDAC) inhibitory moiety, L is a single bond or a linker group and B is a protein kinase inhibitory moiety. The bifunctional compound according to formula (I) is useful for the treatment of malignant and non-malignant neoplasia and diseases related to abnormal cell growth.Type: ApplicationFiled: November 14, 2008Publication date: March 17, 2011Applicant: 4SC AGInventors: Thomas Bar, Thomas Maier, Thomas Beckers, Thomas Clossek, Siavosh Mahboobi, Andreas Sellmer
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Publication number: 20110065681Abstract: Compounds are provided according to formula 1: where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: ApplicationFiled: February 27, 2009Publication date: March 17, 2011Inventors: Zhi-Liang Wei, Sumithra Gowlugari, Carl Kaub, Zhan Wang, Yeyu Cao, John Kincaid
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Publication number: 20110059905Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.Type: ApplicationFiled: March 31, 2009Publication date: March 10, 2011Inventors: Theresa A. Zesiewicz, Kelly L. Sullivan
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Publication number: 20110053989Abstract: This document provides methods and materials related to treating orthostatic hypotension and/or postural tachycardia syndrome. For example, methods and materials for using a composition containing 3,4-diaminopyridine, 4-aminopyridine, or both to treat patients with orthostatic hypotension, postural tachycardia syndrome, or both orthostatic hypotension and postural tachycardia syndrome are provided.Type: ApplicationFiled: September 3, 2010Publication date: March 3, 2011Inventor: Wolfgang Singer
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Publication number: 20110053980Abstract: The present invention relates to indane-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: July 4, 2008Publication date: March 3, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover
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Patent number: 7897622Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: August 10, 2007Date of Patent: March 1, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Pierre Beaulieu, René Coulombe, Gulrez Fazal, Sylvie Goulet, Martin Poirier, Jean Rancourt, Tim Stammers, Bounkham Thavonekham
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Publication number: 20110044899Abstract: A compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4) alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6) alkenyl group or a group of formula (y): wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.Type: ApplicationFiled: January 28, 2009Publication date: February 24, 2011Applicants: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, UNIVERSITE D'AUVERGNE CLERMONT 1, LABORATOIRES CYCLOPHARMAInventors: Jean-Michel Chezal, Frederic Dolle, Jean-Claude Madelmont, Aurelie Maisonial, Elisabeth Miot-Noirault, Nicole Moins, Janine Papon, Bertrand Kuhnast, Bertrand Tavitian, Raphael Boisgard
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Publication number: 20110046129Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.Type: ApplicationFiled: September 9, 2010Publication date: February 24, 2011Applicant: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Publication number: 20110028470Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.Type: ApplicationFiled: July 31, 2008Publication date: February 3, 2011Applicants: TOKAI UNIVERSITY EDUCATIONAL SYSTEM, RENASCIENCE CO., LTD., MEDICAL & BIOLOGICAL LABORATORIES CO., LTD.Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
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Patent number: 7879884Abstract: Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: May 14, 2008Date of Patent: February 1, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Frederick Brookfield, Lothar Kling, Ulrike Reiff, Wolfgang Von der Saal, Thomas Von Hirschheydt
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Publication number: 20110021578Abstract: Compounds of formula (I) and salts thereof are provided: wherein n is 0, 1, 2 or 3; R1 is selected from phenyl and pyridyl, each of which is optionally substituted by one or two groups independently selected from C1-4alkyl and halogen; and R2 is selected from H and CH3 when n is 1 and R2 is H when n is 2 or 3. Processes for preparation, pharmaceutical compositions, N and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.Type: ApplicationFiled: December 17, 2008Publication date: January 27, 2011Applicant: GLAXO GROUP LIMITEDInventors: Nicolas Bertheleme, Wai Ngor Chan, Jaqueline Sandra Scott, Simon E. Ward
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Publication number: 20110021579Abstract: It is an objective of the present invention to provide a novel peritoneal membrane protecting agent which can effectively suppress deterioration of peritoneal functions in long-term peritoneal dialysis (PD) patients and the like. The present invention provides a peritoneal membrane protecting agent comprising a pyridoxine or a salt thereof, as an active ingredient.Type: ApplicationFiled: September 3, 2010Publication date: January 27, 2011Applicant: TOKAI UNIVERSITY EDUCATIONAL SYSTEMInventors: Toshio MIYATA, Takatoshi KAKUTA
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Publication number: 20110021577Abstract: The present invention relates generally to the field of therapeutic treatment and compounds having utility therefor, in particular the therapy or management of conditions associated with excessive, unwanted or undesirable sodium ion passage through cellular membranes via voltage-gated sodium channels. In one embodiment the invention is concerned with the treatment of neuropathic pain. The invention contemplates to aryloxy-substituted amines, as sodium channel blockers or modulators. In further embodiments, the invention also relates to compounds which may advantageously have dual sodium channel blocker/modulating and antioxidative (free-radical scavenging) effects. Methods for their manufacture and compositions containing the compounds are also contemplated.Type: ApplicationFiled: October 31, 2008Publication date: January 27, 2011Applicant: HOWARD FLOREY INSTITUTEInventor: Bevyn Jarrott
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Publication number: 20110021486Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: December 3, 2008Publication date: January 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Terrebonne, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Patent number: 7875636Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels 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 T-type calcium channels are involved.Type: GrantFiled: April 11, 2007Date of Patent: January 25, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Thomas S. Reger, Zhi-Qiang Yang
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Publication number: 20100330032Abstract: Compounds having the formula I wherein R1, R2, R3, R4, and R5 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: ApplicationFiled: June 24, 2010Publication date: December 30, 2010Inventors: Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Patent number: 7858621Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.Type: GrantFiled: July 27, 2007Date of Patent: December 28, 2010Assignee: Amorepacific CorporationInventors: Sun-Young Kim, Jin Kwan Kim, Ki-Wha Lee, Byoung Young Woo, Song Seok Shin, Joo-Hyun Moh, Sung-Il Kim, Yeon Su Jeong, Kyung Min Lim, Jin Kyu Choi, Jun Yong Ha, Hyun-Ju Koh, Young-Ho Park, Young-Ger Suh, Hee-Doo Kim, Hyeung-Geun Park, Uh Taek Oh
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Publication number: 20100317698Abstract: Compounds of formula (I): wherein: n represents an integer of from 1 to 6 inclusive, X represents an oxygen atom or an NR6 group, Y represents a carbon atom or a nitrogen atom, Z represents a carbon atom or a nitrogen atom, R1 and R2 represent a hydrogen atom or an alkyl or arylalkyl group, R3 and R4 represent a hydrogen atom or an alkyl group, R5 represents a hydrogen atom or an alkyl, halogen, hydroxy, alkoxy, cyano, nitro, acyl, alkoxycarbonyl, trihaloalkyl, trihaloalkoxy or optionally substituted amino group, R6 represents a hydrogen atom or an alkyl or arylalkyl group, Ra, Rb, Rc, Rd and Re are as defined in the description. Medicinal products containing the same which are useful as specific nicotinic ligands of ?4?2 receptors.Type: ApplicationFiled: January 30, 2007Publication date: December 16, 2010Applicant: LES LABORATOIRES SERVIERInventors: Solo Goldstein, Claude Guillonneau, Yves Charton, Brian Lockhart, Pierre Lestage
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Publication number: 20100305162Abstract: The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): and salts thereof. The invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.Type: ApplicationFiled: August 12, 2010Publication date: December 2, 2010Inventors: Raja Khalifah, Roland Keilitz, Christoph Koellner, Thorsten Degenhardt, Stephen Robert Brand
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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: 7834063Abstract: This invention relates to benzonitryl and nitrobenzyl derivatives that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds. These compounds are useful, for example, in the treatment or prophylaxis of conditions or disorders that respond to selective androgen receptor modulation.Type: GrantFiled: October 13, 2005Date of Patent: November 16, 2010Assignee: GlaxoSmithKline LLCInventors: Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Lee Stewart
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Publication number: 20100272677Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5a, R5b, R5c and R6 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: ApplicationFiled: April 23, 2010Publication date: October 28, 2010Inventors: Eun Kyung Lee, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Publication number: 20100272642Abstract: Disclosed are: a PET probe compound having an alkoxy group substituted by a fluorine and a hydroxy group, which is useful for the early diagnosis of a conformational disease; a pharmaceutical composition for the treatment and/or prevention of a conformational disease, which comprises the compound; and others.Type: ApplicationFiled: June 17, 2008Publication date: October 28, 2010Applicant: TOHOKU UNIVERSITYInventors: Yukitsuka Kudo, Syozo Furumoto, Nobuyuki Okamura
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Patent number: 7812037Abstract: Compounds with antiplatelet aggregation and anticoagulant characteristics for the treatment of cardiovascular, cerebrovascular, and cardiovascular related diseases and symptoms, are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxine and/or substituted pyridoxine analogs.Type: GrantFiled: October 28, 2005Date of Patent: October 12, 2010Assignee: Medicure International, Inc.Inventors: Wasimul Haque, James Diakur, Vinh Pham, Atiq Rehman, Tara Whitney, Mohammed Omar, Seng Yi, A. Qasim Khan
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Publication number: 20100256201Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.Type: ApplicationFiled: March 11, 2010Publication date: October 7, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
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Publication number: 20100256106Abstract: Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.Type: ApplicationFiled: November 25, 2008Publication date: October 7, 2010Applicant: MERCK & CO., INC.Inventors: Alexander Pasternak, Michael J. Szymonifka
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Publication number: 20100249024Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.Type: ApplicationFiled: June 14, 2010Publication date: September 30, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Joann Bohn, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi
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Publication number: 20100249101Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: January 7, 2010Publication date: September 30, 2010Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
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Publication number: 20100249196Abstract: Phosphoric acid, edisylic acid (1,2-ethanedisulfonic acid), citric acid, orotic acid (uracil-6-carboxylic acid), R-mandelic acid, sulfuric acid, 1,5-naphthalenedisulfonic acid, D-aspartic acid, and lysine monohydrochloride salts of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine, and methods for their preparation, pharmaceutical compositions comprising said salts, and use, are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.Type: ApplicationFiled: May 8, 2007Publication date: September 30, 2010Applicants: ASTRAZENECA AB, TARGACEPT, INC.Inventors: Martin Hans Bohlin, Gary M. Dull, Caroline Eriksson, Craig H. Miller, Julio A. Munoz, Tesfai Sebhatu
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Publication number: 20100240710Abstract: Methods for treating and/or preventing at least one symptom of a disorder associated with oxidative stress, carbonyl stress, or combinations thereof in a subject. In some embodiments, the methods include administering to the subject an effective amount of pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods for treating or preventing a nephropathy, acute renal injury, acute renal failure, or combinations thereof in a subject, and formulations adapted for intravenous administration comprising pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing.Type: ApplicationFiled: May 7, 2010Publication date: September 23, 2010Applicant: Vanderbilt UniversityInventors: Billy G. Hudson, Paul Voziyan, Alp Ikizler
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Publication number: 20100234433Abstract: This invention relates to a novel compound which is a glycogen phosphorylase inhibitor and its use in the treatment of diabetes and other conditions associated therewith. The invention further relates to a pharmaceutical composition containing the compound and to processes for preparing the compound and pharmaceutical composition.Type: ApplicationFiled: September 25, 2008Publication date: September 16, 2010Inventors: Pierette Banker, Scott Howard Dickerson, Dulce Maria Garrido, Steven Meagher Sparks, Francis X. Tavares, Stephen Andrew Thomson
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Patent number: 7790758Abstract: This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.Type: GrantFiled: February 13, 2006Date of Patent: September 7, 2010Assignee: Glaxo Group LimitedInventors: Daniele Andreotti, Luca Arista, Francesca Cardullo, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
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Patent number: 7790757Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.Type: GrantFiled: October 31, 2007Date of Patent: September 7, 2010Assignee: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Publication number: 20100216848Abstract: A liquid pharmaceutical composition comprising N-[1S,2S]-3-[(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[(5-trifluoromethyl)pyridine-2-yl]oxy}propanamide is disclosed, together with processes of preparing the liquid pharmaceutical composition, preparing a vessel containing the liquid pharmaceutical composition, the use of the composition for treating and preventing diabetes or obesity and a method of treating or preventing diabetes or obesity comprising administration to a patient in need thereof of an effective amount of the liquid pharmaceutical composition.Type: ApplicationFiled: October 6, 2008Publication date: August 26, 2010Inventors: Andrey V. Peresypkin, Sachin Mittal
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Patent number: 7781463Abstract: Compounds of general formula (I): where A, E, G, X, Y and the bond - - - take various meanings are of use in the preparation of a pharmaceutical formulation, for example in the treatment of a disease in which GSK-3 is involved, including Alzheimer's disease or the non-dependent insulin diabetes mellitus, or hyperproliferative disease such as cancer, displasias or metaplasias of tissue, psoriasis, arteriosclerosis or restenosis.Type: GrantFiled: April 20, 2007Date of Patent: August 24, 2010Assignees: Consejo Superior de Investigaciones Cientificas, Universidad Autonoma de Madrid (UAM)Inventors: Ana Martinez Gil, Ana Castro Morera, Maria Concepcion Martin Perez, Mercedes Alonso Cascon, Isabel Dorronsoro Diaz, Francisco Jose Moreno Munoz, Francisco Wandosell Jurado
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Publication number: 20100190731Abstract: The invention relates to methods of treating patients who have suffered an acute myocardial infarction (AMI) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.Type: ApplicationFiled: January 26, 2010Publication date: July 29, 2010Inventors: Jeff Olgin, Karl Kossen
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Publication number: 20100183606Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Inventors: ROBERT M BORZILLERI, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim