Chalcogen Bonded Directly To A Ring Carbon Of The Six-membered Hetero Ring Patents (Class 514/335)
  • Publication number: 20110288092
    Abstract: Disclosed are methods of treating hyperproliferative disorders, method of treating inflammatory disorders, and methods of inhibiting MEK activity in a mammal, comprising administering an effective amount of one or more compounds of the Formula V or pharmaceutically acceptable salts thereof, wherein R1, R2, R7, R8, R9 and W are as defined in the specification.
    Type: Application
    Filed: November 22, 2010
    Publication date: November 24, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Publication number: 20110288033
    Abstract: The invention relates generally to optical agents for biomedical applications, including phototherapy. Provided are disulfide compounds having an acyclic S—S bond with at least one aromatic and/or heterocyclic aromatic group providing phototherapeutic agents, including Type 1 phototherapeutic agents. Optical agents of the invention enable a versatile phototherapy platform for treatment of a range of pathological conditions, including the treatment of cancers, stensosis and inflammation. The invention further provides preparations and formulations comprising the disulfide optical agents and related methods of making and using disulfide optical agents in an in vivo or ex vivo biomedical procedure.
    Type: Application
    Filed: May 18, 2011
    Publication date: November 24, 2011
    Applicant: Mallinckrodt Inc.
    Inventor: Raghavan Rajagopalan
  • Publication number: 20110263530
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Application
    Filed: June 28, 2011
    Publication date: October 27, 2011
    Applicant: Amgen Inc.
    Inventors: Victor J. CEE, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
  • Publication number: 20110230517
    Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy1 is pyridinonyl, pyridinyl, quinolinyl or 9-ethyl-9H-beta-carbolinyl, each of which optionally substituted and where Cy2 is phenyl naphthyl.
    Type: Application
    Filed: October 7, 2009
    Publication date: September 22, 2011
    Inventors: Christopher Fotsch, Paul Harrington
  • Publication number: 20110230522
    Abstract: The present invention relates to combinations of a thiol group modulating enzyme inhibitor and a pyrion compound which provide an improved protecting effect against fouling organisms, fungi or bacteria. More particularly, the present invention relates to compositions comprising a combination of a thiol group modulating enzyme inhibitor selected from dichlofluanid, tolylfluanid, dithane, thiram, ziram, or zineb, together with a pyrion compound selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine, rilopirox, pyrion disulfide, sodium pyrithione and zinc pyrithione; in respective proportions to provide a synergistic effect against fouling organisms, fungi or bacteria and the use of these compositions for protecting materials against fouling organisms, fungi or bacteria.
    Type: Application
    Filed: November 26, 2009
    Publication date: September 22, 2011
    Inventors: Jan Pieter Hendrik Bosselaers, Dany Leopold Jozefien Bylemans, Tony Mathilde Jozef Kempen
  • Publication number: 20110224204
    Abstract: Di-substituted phenyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. The disclosure also relates to methods for treating neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.
    Type: Application
    Filed: June 25, 2009
    Publication date: September 15, 2011
    Inventors: Richard Chesworth, Gideon Shapiro, Amy Ripka
  • Publication number: 20110218232
    Abstract: The invention relates to inhibitors of Multi drug Resistant Protein 4 (MRP4) for the treatment and/or the prevention of cardiac disorders, such as acute or chronic heart failure and cardiogenic shock. The invention also relates to agents stimulating MRP4 activity for the treatment and/or the prevention of cardiac hypertrophy.
    Type: Application
    Filed: July 17, 2009
    Publication date: September 8, 2011
    Applicant: INSERM (Institut National de la Sante et de la Recherche Medicale)
    Inventors: Jean-Sebastien Hulot, Anne-Marie Lompre, Yassine Sassi
  • Publication number: 20110212930
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Application
    Filed: May 5, 2011
    Publication date: September 1, 2011
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
  • Publication number: 20110201616
    Abstract: [Object] A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.
    Type: Application
    Filed: June 22, 2009
    Publication date: August 18, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Hideki Kubota, Issei Tsukamoto, Kazunori Kamijo, Koji Kato, Yuta Fukuda, Hidenori Azami
  • Publication number: 20110201603
    Abstract: The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an aromatic ring group of Q1 to Q7 described in the detailed description, G1 and G2 represent O or S, R1 represents hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl or a heterocyclic group and R2 and R3 represent hydrogen, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl or haloalkoxycarbonyl.
    Type: Application
    Filed: July 30, 2009
    Publication date: August 18, 2011
    Applicant: Bayer CropScience AG
    Inventors: Jun Mihara, Tetsuya Murata, Kei Domon, Yukiyoshi Watanabe, Yasushi Yoneta, Takuma Mori, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Masashi Ataka, Ulrich Görgens
  • Publication number: 20110195997
    Abstract: The invention is concerned with dicarboxamide derivatives of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used in pharmaceutical compositions.
    Type: Application
    Filed: April 18, 2011
    Publication date: August 11, 2011
    Inventors: Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Narendra Panday, Fabienne Ricklin
  • Patent number: 7989477
    Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: August 2, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Lyndon A. M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
  • Publication number: 20110183966
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: February 4, 2011
    Publication date: July 28, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Francois Maltais, Guy W. Bemis, Tiansheng Wang, Juan Miguel Jimenez, Luca Settimo, Stephen Young, Dean Boyall, Damien Fraysse, Christopher John Davis
  • Publication number: 20110183981
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: March 30, 2011
    Publication date: July 28, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Publication number: 20110183980
    Abstract: In one aspect, the invention relates to O-benzyl nicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: September 21, 2010
    Publication date: July 28, 2011
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Shaun Stauffer, Richard Williams, Gregor MacDonald, Ya Zhou, José Manuel Bartolomé-Nebreda
  • Publication number: 20110178089
    Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: January 13, 2011
    Publication date: July 21, 2011
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ulmer
  • Publication number: 20110178120
    Abstract: The present invention relates to pyridoxine (vitamin B6) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R1, R2, R4, A, L B1 and B2 are as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS.
    Type: Application
    Filed: June 4, 2009
    Publication date: July 21, 2011
    Applicant: AMBRILIA BIOPHARMA, INC.
    Inventors: Brent Stranix, Francis Beaulieu, Jean-Emmanuel Bouchard, Guy Milot, Wang Zhigang, Réjean Ruel
  • Patent number: 7981901
    Abstract: Methods and compositions for targeting cerebral circulation and treatment of headache include formulations comprising a pharmacologically active substance in a transdermal formulation, which is topically applied to an area of skin superficial to a carotid artery, a temporal artery, a vertebral artery, or to a tender spot associated with a headache. Particularly preferred formulations include a xanthine derivative (e.g., theophylline, caffeine, aminophylline), and may further comprise ketoprofen. Contemplated methods further include methods of advertising use of contemplated compositions.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: July 19, 2011
    Inventor: Bruce Frome
  • Publication number: 20110172247
    Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions.
    Type: Application
    Filed: September 17, 2010
    Publication date: July 14, 2011
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates
  • Publication number: 20110172248
    Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: September 17, 2010
    Publication date: July 14, 2011
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates
  • Publication number: 20110166158
    Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: September 17, 2010
    Publication date: July 7, 2011
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates, Brian A. Chauder
  • Patent number: 7973059
    Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: October 17, 2006
    Date of Patent: July 5, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, Mark T. Bilodeau, M. Brad Nolt
  • Publication number: 20110136871
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: May 22, 2009
    Publication date: June 9, 2011
    Applicant: BAYER SCHERING AKTIENGESELLSCHAFT
    Inventors: Walter Hübsch, Daniel Meibom, Alexandros Vakalopoulos, Barbara albrecht-Küpper, Peter Nell, Katja Zimmermann, Frank Süssmeier, Joerg Keldenich
  • Publication number: 20110130365
    Abstract: The present invention provides Formula (1A) XN O R 3 HN R 5 O R 4 R 2 R 1 (1A) 5 compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the glucokinase enzyme, where X, R 1, R 2, R 3, R 4, and R 5 are as described herein.
    Type: Application
    Filed: July 15, 2009
    Publication date: June 2, 2011
    Inventors: John W. Benbow, Jihong Lou, Jeffrey A. Pferfferkorn, Meihua M. Tu
  • Publication number: 20110118248
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: January 13, 2009
    Publication date: May 19, 2011
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
  • Patent number: 7943638
    Abstract: A carboxamide compound represented by the formula (1): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, one of ring constitutional atoms of the heterocyclic group is a nitrogen atom and the heterocyclic group may be substituted with a group selected from the group consisting of a C1-C3 alkyl and the like, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom or the like] and a plant disease controlling agent comprising this as an active ingredient.
    Type: Grant
    Filed: July 12, 2006
    Date of Patent: May 17, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shin-ichiro Souma, Yoshiharu Kinoshita
  • Publication number: 20110112064
    Abstract: 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: Application
    Filed: January 18, 2011
    Publication date: May 12, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Kelly-Ann S. Bieber, Rowena V. Cube, Mamio Christa Mattern, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
  • Publication number: 20110104235
    Abstract: The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include non-temperature dependent phase change compositions that may be formulated as solutions, solids, semisolids, microparticles, or crystals.
    Type: Application
    Filed: January 6, 2011
    Publication date: May 5, 2011
    Inventors: Frank Kochinke, Corinne Bright
  • Patent number: 7902372
    Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
    Type: Grant
    Filed: April 2, 2008
    Date of Patent: March 8, 2011
    Assignee: Eli Lilly and Company
    Inventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
  • Publication number: 20110052583
    Abstract: The invention is directed to pyridinone compounds useful for modulating Met kinase, having the following structure: and is further directed to pharmaceutical compositions comprising the compound; and methods for treating proliferative diseases, such as cancer by the administration of this compound.
    Type: Application
    Filed: November 8, 2010
    Publication date: March 3, 2011
    Inventors: Robert M. Borzilleri, Gretchen M. Schroeder, Zhen-Wei Cai
  • Patent number: 7897621
    Abstract: The present invention relates to compounds formula I: and pharmaceutically acceptable salts thereof, wherein R1 to R8 are as defined in the description and claims for use as HDL-cholesterol raising agents in the treatment and/or prophylaxis of diseases or disorders that can be treated with such agents such as dyslipidemia.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: March 1, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Constantinos G. Panousis, Stephan Roever, Pius Waldmeier, Matthew Wright
  • Publication number: 20110046088
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: February 20, 2008
    Publication date: February 24, 2011
    Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMTIED
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Patent number: 7893061
    Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A1-3, R1 and R3-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: February 22, 2011
    Assignee: Amgen Inc.
    Inventor: Ryan White
  • Publication number: 20110034416
    Abstract: Disclosed are compounds of Formula (I): and salts thereof. Also, disclosed are methods of using the compounds in the treatment of proliferative diseases, such as cancer, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a pharmaceutically acceptable salt.
    Type: Application
    Filed: January 22, 2009
    Publication date: February 10, 2011
    Inventors: Robert M. Borzilleri, Zhen-Wei Cai
  • Publication number: 20110028509
    Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.
    Type: Application
    Filed: April 8, 2009
    Publication date: February 3, 2011
    Applicant: MERCK SERONO SA
    Inventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
  • Patent number: 7880004
    Abstract: The invention is directed to compounds that are useful for the treatment of cancer having the following Formula:
    Type: Grant
    Filed: September 14, 2006
    Date of Patent: February 1, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhen-wei Cai, Donna D. Wei, John S. Tokarski
  • Publication number: 20110021486
    Abstract: 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: Application
    Filed: December 3, 2008
    Publication date: January 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Terrebonne, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
  • Publication number: 20110021487
    Abstract: The present application relates to novel cycloalkoxy-substituted 4-phenyl-3,5-dicyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.
    Type: Application
    Filed: January 31, 2009
    Publication date: January 27, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Walter Hübsch, Peter Nell, Frank Süssmeier, Alexandros Vakalopoulos, Daniel Meibom, Barbara Albrecht-Küpper, Katja Zimmermann
  • Publication number: 20110009407
    Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.
    Type: Application
    Filed: April 27, 2010
    Publication date: January 13, 2011
    Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
  • Publication number: 20110009454
    Abstract: 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: Application
    Filed: February 27, 2009
    Publication date: January 13, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yuichi Matsuzaki, Takashi Komori, Tohru Inoue
  • Publication number: 20110003826
    Abstract: 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: Application
    Filed: June 27, 2008
    Publication date: January 6, 2011
    Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyu "Bio
    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: 20110003858
    Abstract: The invention provides compounds of formula (I) and formula (IV) (M)-(L)-(M) (I) [(M)-(L4)]t-G (VI) wherein M, L, L4, G and t are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.
    Type: Application
    Filed: September 3, 2007
    Publication date: January 6, 2011
    Inventors: Lena Bergström, Hans Lönn, Michael Lundkvist, Peter Sjö
  • Publication number: 20110003013
    Abstract: The present invention provides a method for increasing metabolism and/or energy expenditure in a subject, e.g., to treat or prevent obesity and/or a related condition and/or to reduce adiposity, the method comprising increasing the level and/or activity of Hypoxia Induced Factor 1? (HIF-1?) in a cell, tissue or organ of the subject, thereby increasing metabolism in the subject. The present invention also provides a method for increasing metabolism in a subject, the method comprising administering an iron chelating agent to the subject, thereby increasing metabolism in the subject.
    Type: Application
    Filed: January 5, 2009
    Publication date: January 6, 2011
    Inventor: Jenny Gunton
  • Publication number: 20110003783
    Abstract: An orally administered antihyperlipidemia composition according to the present invention includes from about 250 to about 3000 parts by weight of nicotinic acid, and from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose. Also, a method of treating hyperlipidemia in a hyper lipidemic having a substantially periodic physiological loss of consciousness, includes the steps of forming a composition having an effective antihyperlipidemic amount of nicotinic acid and a time release sustaining amount of a swelling agent.
    Type: Application
    Filed: April 8, 2010
    Publication date: January 6, 2011
    Inventor: David J. Bova
  • Publication number: 20100324058
    Abstract: 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: Application
    Filed: June 27, 2008
    Publication date: December 23, 2010
    Applicant: 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
  • Patent number: 7855219
    Abstract: This invention relates to compounds of formula (I) in which the variable groups are as defined in the text and claims. A pharmaceutical composition and methods of using these materials in treatment of various conditions are also disclosed and claimed.
    Type: Grant
    Filed: February 20, 2002
    Date of Patent: December 21, 2010
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
  • Publication number: 20100311748
    Abstract: The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z).
    Type: Application
    Filed: August 29, 2008
    Publication date: December 9, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Leslie Dakin, Benjamin Fauber, Alexander Hird, James Janetka, Daniel John Russell, Qibin Su, Bin Yang, Xiaolan Zheng
  • Publication number: 20100305162
    Abstract: 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: Application
    Filed: August 12, 2010
    Publication date: December 2, 2010
    Inventors: Raja Khalifah, Roland Keilitz, Christoph Koellner, Thorsten Degenhardt, Stephen Robert Brand
  • Publication number: 20100305161
    Abstract: The present invention relates to combinations of a fungicidal triazole, or a salt thereof, and a pyrion compound, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of a fungicidal triazole, or a salt thereof, selected from the group consisting of azaconazole, bromuconazole, cyproconazole, difenoconazole, epoxiconazole, fenbuconazole, fluquinconazole, flusilazole, hexaconazole, ipconazole, metconazole, penconazole, propiconazole, prothioconazole, simeconazole, tebuconazole, tetraconazole, and triticonazole, together with a pyrion compound selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine, rilopirox and pyrion disulfide in respective proportions to provide a synergistic biocidal effect.
    Type: Application
    Filed: November 27, 2008
    Publication date: December 2, 2010
    Inventors: Jan Peter Hendrik Bosselaers, Dany Leopold Jozefien Bylemans, Tony Mathilde Jozef Kempen, Hans Bernhard Leithoff, Amber Paula Marcella Thys, Mark Arthur Josepha Van Der Flaas
  • Publication number: 20100305124
    Abstract: The present invention relates to aminopyridine and aminopyridazine derivatives of the general formula (I) in which R1, X, W and Q have the definitions given in the description, to a number of processes for preparing them, and to their use as insecticides.
    Type: Application
    Filed: April 2, 2010
    Publication date: December 2, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Martin FUSSLEIN, Ernst Rudolf Gesing, Markus Heil, Bernd Alig, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Koichi Araki, Norio Sasaki, Sachio Kudo, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya