Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
-
Patent number: 7872015Abstract: The invention relates to the field of biology, genetics and medicine. In particular, the invention relates to novel methods for the detection, characterization and/or treatment (or management) of neurodegenerative pathologies. The invention also relates to methods for the identification or screening of compounds active in the aforementioned pathologies. The invention further relates to the compounds, genes, cells, plasmids or compositions which are used to carry out said methods. In particular, the invention is based on the identification of the role of phosphodiesterase 4B, the peripheral benzodiazepine receptor (PBR) and GABA receptors of the type GABA(A) in neurodegenerative pathologies and describes the use of same as therapeutic, diagnostic or experimental markers or targets for said disorders.Type: GrantFiled: February 18, 2004Date of Patent: January 18, 2011Assignee: Exonhit Therapeutics SAInventors: Fabien Schweighoffer, Annelies Resink, Laurent Desire, Magali Rouquette
-
Publication number: 20110009454Abstract: Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NRZ; and E represents a furyl group, a thienyl group, a pyrrolyl group, a tetrazolyl group, a thiazolyl group, a pyrazolyl group, a phenyl group or the like.Type: ApplicationFiled: February 27, 2009Publication date: January 13, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yuichi Matsuzaki, Takashi Komori, Tohru Inoue
-
Patent number: 7868026Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.Type: GrantFiled: January 9, 2007Date of Patent: January 11, 2011Assignee: Pfizer Inc.Inventors: Mitchell David Nambu, Leena Bharat Kumar Patel, Brian Douglas Patterson, Sylvie Kim Sakata, John Howard Tatlock
-
USE OF POLYMERIC GUANIDINE DERIVATIVES FOR THE CONTROL OF UNWANTED MICROORGANISMS IN CROP PROTECTION
Publication number: 20110003689Abstract: The present invention relates to the use of polymeric guanidine derivatives for the curative and/or preventive treatment of unwanted microorganisms such as bacteria and phytopathogenic fungi in crop protection including the treatment of seed. The invention furthermore relates to novel active compound combinations comprising at least one polymeric guanidine derivative and at least one further fungicidally active compound, their use for the curative or preventive treatment of unwanted microorganisms in crop protection including the treatment of seed and not least the treated seed itself.Type: ApplicationFiled: December 6, 2008Publication date: January 6, 2011Applicant: AKA TECHNOLOGY GMBHInventors: Hans-Juergen Rosslenbroich, Arnd Voerste, Martin Schoepfer, Hilmar Wolf, Ulrike Wachendorff-Neumann, Peter Dahmen, Dirk Ebbinghaus, Oskar Schmidt -
Publication number: 20110003865Abstract: This invention relates to novel 2-diethylamino-3-amido-6-amino-pyridine derivatives having medical utility, to use of the 2-diethylamino-3-amido-6-amino-pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-diethylamino-3-amido-6-amino-pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.Type: ApplicationFiled: December 10, 2008Publication date: January 6, 2011Inventors: Carsten Jessen, William Dalby Brown, Dorte Strøbæk
-
Publication number: 20110003867Abstract: This invention relates to novel 2-ethyl-methyl-amino-3-amido-6-amino-pyridine derivatives having medical utility, to use of the 2-ethyl-methyl-amino-3-amido-6-amino-pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-ethyl-methyl-amino-3-amido-6-amino-pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.Type: ApplicationFiled: December 10, 2008Publication date: January 6, 2011Applicant: NeuroSearch A/SInventors: Carsten Jessen, William Dalby Brown, Dorte Strøbaek
-
Publication number: 20110003868Abstract: A process for treating neuropathy includes administration to a patient suffering from a neuropathy more than 5 and less than 18 mg of aminopyridine in a dose. The aminopyridine is formulated in an immediate release formulation. At least two such doses are provided per day to create spike serum plasma levels of aminopyridine sufficient to drive the aminopyridine across the blood-nerve barrier.Type: ApplicationFiled: September 15, 2010Publication date: January 6, 2011Applicant: The UAB Research FoundationInventor: Jay M. Meythaler
-
Publication number: 20110003866Abstract: This invention relates to novel 2-dimethylamino-3-amido-6-amino-pyridine derivatives having medical utility, to use of the 2-dimethylamino-3-amido-6-amino-pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-dimethylamino-3-amido-6-amino-pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.Type: ApplicationFiled: December 10, 2008Publication date: January 6, 2011Inventors: William Dalby Brown, Carsten Jessen, Dorte Strøbæk
-
Publication number: 20110003826Abstract: This invention relates to new chemical compounds, application of these compounds as anticoagulants, pharmaceutical compositions, and plasma-substituting solutions on their basis, and can be used for treating thromboembolic complications of diseases such as myocardial infarction, stroke, and thrombosis of deep veins or a pulmonary artery; and for preventing hypercoagulation conditions in consequence of injuries, surgeries, sepsis, various obstetric pathologies, in disaster medicine, resuscitation, and so on.Type: ApplicationFiled: June 27, 2008Publication date: January 6, 2011Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyu "BioInventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
-
Publication number: 20110003859Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: February 27, 2009Publication date: January 6, 2011Applicant: Array Biopharma Inc.Inventor: Kateri A. Ahrendt
-
Publication number: 20100331376Abstract: This invention is generally directed to a method for recovering flunixin and flunixin analogs from pharmaceutical compositions. The recovered flunixin and analogs can be, for example, reused to make new pharmaceutical compositions and thereby reduce the need and expense of manufacturing new flunixin and flunixin analogs.Type: ApplicationFiled: December 12, 2008Publication date: December 30, 2010Inventors: James C. Towson, Donal Coveney
-
Publication number: 20100331234Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.Type: ApplicationFiled: March 3, 2010Publication date: December 30, 2010Applicant: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher Gerard Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel G. Anderson
-
Publication number: 20100331304Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: October 30, 2008Publication date: December 30, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
-
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
-
Patent number: 7858646Abstract: The present invention provides compounds of formula (I); pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.Type: GrantFiled: November 15, 2005Date of Patent: December 28, 2010Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Dana Rae Benesh, Maria-Jesus Blanco-Pillado, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsäter, Jeffrey Michael Schkeryantz, Tony Pisal Tang
-
Publication number: 20100324093Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: August 26, 2010Publication date: December 23, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
-
Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
-
Publication number: 20100324099Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.Type: ApplicationFiled: June 25, 2010Publication date: December 23, 2010Inventors: Andrew R. BLIGHT, Ron COHEN
-
Publication number: 20100324098Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.Type: ApplicationFiled: June 25, 2010Publication date: December 23, 2010Inventors: Andrew R. BLIGHT, Ron COHEN
-
Publication number: 20100324058Abstract: This invention relates to new chemical compounds, application of these compound as thrombin inhibitors, and pharmaceutical compositions based on them, and can be used to treat and prevent thrombin-dependent thromboembolic events, and in research.Type: ApplicationFiled: June 27, 2008Publication date: December 23, 2010Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyou "Bionika"Inventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
-
Publication number: 20100324092Abstract: The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Richard W. Heidebrecht, JR., Thomas A. Miller, Matthew G. Stanton, David J. Witter
-
Publication number: 20100324100Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.Type: ApplicationFiled: June 25, 2010Publication date: December 23, 2010Inventors: Andrew R. BLIGHT, Ron COHEN
-
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
-
Publication number: 20100317643Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereofType: ApplicationFiled: June 10, 2010Publication date: December 16, 2010Applicant: GENENTECH, INC.Inventors: SIMON CHARLES GOODACRE, YINGJIE LAI, JUN LIANG, STEVEN R. MAGNUSON, KIRK D. ROBARGE, MARK S. STANLEY, VICKIE HSIAO-WEI TSUI, KAREN WILLIAMS, BIRONG ZHANG, AIHE ZHOU
-
Publication number: 20100310493Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: October 7, 2008Publication date: December 9, 2010Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITEDInventors: Debnath Bhuniya, Sandeep Bhausaheb Bhosale, Gobind Sing Kapkoti, Venkata Poornapragnacharyulu Palle, Siddhartha De, Kasim A. Mookhtiar, Bhavesh Dave, Anil Deshpande, Santosh Kurhade, Balasaheb Kobal, Keshav Naik, Sachin Kandalkar
-
Publication number: 20100311736Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.Type: ApplicationFiled: October 22, 2008Publication date: December 9, 2010Inventors: Nicholas D. Adams, Michael Gerard Darcy, Neil W. Johnson, Jiri Kasparec, Steven David Knight, Kenneth Allen Newlander, Xin Peng, Lance H. Ridgers
-
Patent number: 7846915Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.Type: GrantFiled: October 20, 2005Date of Patent: December 7, 2010Assignee: Resverlogix CorporationInventors: Norman C. W. Wong, Joseph E. L. Tucker, Henrik C. Hansen, Fabrizio S. Chiacchia, David McCaffrey
-
Publication number: 20100305131Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates 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: May 27, 2010Publication date: December 2, 2010Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
-
Publication number: 20100298284Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: April 7, 2010Publication date: November 25, 2010Inventors: Bing-Yan ZHU, Penglie ZHANG, Lingyan WANG, Wenrong HUANG, Erick A. GOLDMAN, Wenhao LI, Jingmei ZUCKETT, Yonghong SONG, Robert M. SCARBOROUGH
-
Patent number: 7838513Abstract: The present invention relates to the treatment of a mammal with a pharmaceutical composition comprising an H2-blocker, at least one anti-inflammatory agent, a cytotoxic agent and, optionally, levamisole, a retinoid, an NFkB inhibitor, a redox quinone, an agent that enhances the intracellular accumulation of NADH+H+, a poly-alcohol, an inhibitor of pro-angiogenic growth factor(s) and an MMP inhibitor, such pharmaceutical composition allowing for the enhanced therapy and/or prevention of neoplastic diseases and disorders.Type: GrantFiled: July 4, 2007Date of Patent: November 23, 2010Assignee: Tiltan Pharma Ltd.Inventor: Shmuel A. Ben-Sasson
-
Publication number: 20100292300Abstract: The present invention provides compositions and methods for inhibiting or reversing fibrotic disorders by administering a Hic-5 antagonist to a mammal in need thereof. The invention also includes methods for screening compounds to identify Hic-5 antagonists useful in inhibiting or reversing fibrotic disorders.Type: ApplicationFiled: February 15, 2008Publication date: November 18, 2010Applicant: ALBANY MEDICAL COLLEGEInventors: Livingston Van De Water, Ganary Dabiri, Christopher E. Turner, Andres J. Melendez
-
Publication number: 20100292225Abstract: 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: May 14, 2010Publication date: November 18, 2010Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
-
Publication number: 20100286214Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.Type: ApplicationFiled: May 8, 2009Publication date: November 11, 2010Applicant: Pfizer, Inc.Inventors: Hengmiao (Henry) Cheng, Xiao Hu, Kevin D. Jerome, Mark Obukowicz, Lisa Olson, Paul V. Rucker, Ronald Keith Webber
-
Publication number: 20100280081Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, for the use as a medicament.Type: ApplicationFiled: May 3, 2010Publication date: November 4, 2010Applicant: 4SC AGInventors: Daniel VITT, Manfred GROEPPEL, Roland BAUMGARTNER, Johann LEBAN
-
Publication number: 20100280074Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: December 3, 2009Publication date: November 4, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
-
Publication number: 20100272795Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.Type: ApplicationFiled: November 25, 2009Publication date: October 28, 2010Inventors: Sean CUNNINGHAM, Seamus Mulligan, Michael Myers
-
Publication number: 20100272796Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.Type: ApplicationFiled: November 25, 2009Publication date: October 28, 2010Inventors: Sean CUNNINGHAM, Seamus Mulligan, Michael Myers
-
Patent number: 7820663Abstract: The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.Type: GrantFiled: June 15, 2006Date of Patent: October 26, 2010Assignee: The Regents of the University of CaliforniaInventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
-
Publication number: 20100267754Abstract: The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action.Type: ApplicationFiled: June 10, 2010Publication date: October 21, 2010Inventors: Toshiaki WAKABAYASHI, Yasuhiro Funahashi, Naoko Hata, Taro Semba, Yuji Yamamoto, Toru Haneda, Takashi Owa, Akihiko Tsuruoka, Junichi Kamata, Tadashi Okabe, Keiko Takahashi, Kazumasa Nara, Shinichi Hamaoka, Norihiro Ueda
-
Publication number: 20100266539Abstract: The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.Type: ApplicationFiled: March 25, 2010Publication date: October 21, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Hiroshi Ochiai, Natsuko Tokuda, Shiro Shibayama, Noriki Watanabe, Takaki Komiya, Kazuhiko Takeda
-
Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
-
Patent number: 7816389Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.Type: GrantFiled: January 11, 2007Date of Patent: October 19, 2010Assignee: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
-
Patent number: 7812025Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whicType: GrantFiled: August 11, 2006Date of Patent: October 12, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Matsumoto, Masakuni Kori, Mitsunori Kouno
-
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
-
Patent number: 7812038Abstract: A method for the inhibition of the binding of ?4?1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either a above, or in formulations for the control or prevention of diseases states in which ?4?1 is involved.Type: GrantFiled: June 14, 2005Date of Patent: October 12, 2010Assignee: Encysive Pharmaceuticals, Inc.Inventors: Ronald J. Biediger, Qi Chen, E. Radford Decker, George W. Holland, Jamal M. Kassir, Wen Li, Robert V. Market, Ian L. Scott, Chengde Wu, Jian Li
-
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
-
Publication number: 20100256145Abstract: The invention relates, inter alia, to a method for reducing symptoms of, or for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, the method comprising administering to a host in need thereof an effective amount of a compound that is able to increase the ion flow through KCNQ potassium channels.Type: ApplicationFiled: July 31, 2008Publication date: October 7, 2010Applicant: H. LUNDBECK A/SInventors: Henriette Husum Bak-Jensen, Klaus Peter Hertel
-
Publication number: 20100256110Abstract: A composition comprises a solid dispersion comprising a low-solubility drug and at least one polymer. At least a major portion of the drug in the dispersion is amorphous. The polymer has a glass transition temperature of at least 100° C. measured at a relative humidity of fifty percent. Another aspect of the invention comprises the same composition except that the dispersion has a glass transition temperature of at least 50° C. at a relative humidity of fifty percent. In another aspect of the invention, a composition comprises a solid dispersion comprising a low-solubility drug and a stabilizing polymer. At least a major portion of the drug in the dispersion is amorphous. The composition also includes a concentration-enhancing polymer that increases the concentration of the drug in a use environment. The stabilizing polymer has a glass transition temperature that is greater than the glass transition temperature of the concentration-enhancing polymer at a relative humidity of 50%.Type: ApplicationFiled: May 25, 2010Publication date: October 7, 2010Inventors: Walter C. Babcock, Dwayne T. Friesen, James A.S. Nightingale, Ravi M. Shanker
-
Publication number: 20100255116Abstract: A fungicidal composition is provided. A fungicidal composition comprising synergistically effective amounts of (a) a carboxylic acid amide derivative of the formula (I) or its salt: wherein B is a heterocyclic group which may be substituted; each of R1 and R2 which are independent of each other, is alkyl; X is halogen, alkyl or alkoxy; and n is an integer of from 0 to 5, and (b) at least one fungicidal compound selected from the group consisting of an azole compound, an anilinopyrimidine compound, a triazolopyrimidine compound, a strobilurin compound, an N-halogenothioalkyl compound, a pyridinamine compound, a bicarbonate, an inorganic sulfur compound, a dithiocarbamate compound, an organic chlorine compound, a dicarboxyimide compound, an amine compound, a phenylpyrrole compound, a benzophenone compound, a dinitrobenzene compound, a piperidine compound, a morpholine compound, etc.Type: ApplicationFiled: October 20, 2008Publication date: October 7, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Shigeru Mitani, Shintaro Tsukuda
-
Publication number: 20100256149Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 14, 2010Publication date: October 7, 2010Applicant: MERCK SERONO S.A.Inventors: Andreas Goutopoulos, Benny C. Askew, JR., Nhut Kiet Diep, Srinivasa Karra, Matthias Schwarz, Henry Yu