Acyclic Carbon Bonded Directly To The -c(=x)- (e.g., N-oleoylpyrrolidine, Etc.) Patents (Class 548/540)
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Publication number: 20110172444Abstract: The present invention herein provides a simple, efficient and industrially useful method for purifying an aminoacetylpyrrolidinecarbonitrile derivative which is useful as a DPP-IV inhibitor. The method comprises the steps of acting an acid such as maleic acid on an aminoacetylpyrrolidinecarbonitrile derivative represented by the following Formula 1 to form a salt, isolating the salt and then regenerating the foregoing derivative from the salt: (In the formula, A represents CH2, CHF or CF2; R represents a C1 to C6 alkyl group which may have a substitutent, a C3 to C8 cycloalkyl group which may have a substitutent, an arylmethyl group which may have a substitutent, an arylethyl group which may have a substitutent, an aromatic hydrocarbon ring which may have a substitutent, an aromatic hetero ring which may have a substitutent, or an aliphatic hetero ring which may have a substitutent; and n represents 1 or 2).Type: ApplicationFiled: September 15, 2009Publication date: July 14, 2011Inventor: Futoshi Shiga
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Publication number: 20110166354Abstract: The present application relates to a method for producing an optically active ?-amino acid derivative, comprising steps of reacting an ?-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative, with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active ?-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity.Type: ApplicationFiled: June 2, 2009Publication date: July 7, 2011Inventors: Shohei Yamamoto, Akio Fujii, Masaru Mitsuda
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Publication number: 20110144170Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.Type: ApplicationFiled: February 18, 2011Publication date: June 16, 2011Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
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Publication number: 20110136752Abstract: The invention relates generally to novel antibiotics and their analogs, to processes for the preparation of these novel antibiotics, to pharmaceutical compositions comprising the novel antibiotics; and to methods of using the novel antibiotics to treat or inhibit various disorders.Type: ApplicationFiled: December 6, 2010Publication date: June 9, 2011Applicant: NOVOBIOTIC PHARMACEUTICALS LLCInventors: Aaron PEOPLES, Lucy Losee LING, Kim LEWIS, Zhizhen ZHANG
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Patent number: 7951960Abstract: The black color material includes a condensation product of a pyrrole compound represented by the following formula (1) and a squaric acid represented by the following formula (2):Type: GrantFiled: September 30, 2008Date of Patent: May 31, 2011Assignee: Fuji Xerox Co., Ltd.Inventors: Shinji Hasegawa, Minquan Tian, Yuka Ito, Kazuhiko Hirokawa, Miho Watanabe, Makoto Furuki
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Publication number: 20110124881Abstract: Disclosed is a process of forming a pyrrole compound. The process comprises contacting an ?-carbonyl oxime compound 1 and an ?,?-unsaturated aldehyde 2 R1 and R2 in compound 1 are independently selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. R3 in aldehyde 2 is selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. The ?-carbonyl oxime compound 1 an the ?,?-unsaturated aldehyde 2 are contacted in a suitable solvent in the presence of a secondary amine.Type: ApplicationFiled: May 18, 2010Publication date: May 26, 2011Inventors: Guofu Zhong, Bin Tan, Zugui Shi, Pei Juan Chua
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Publication number: 20110112051Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.Type: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Applicant: Alantos Pharmaceuticals Holding, Inc.Inventors: Heiko KROTH, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
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Patent number: 7939668Abstract: The invention relates to novel metathesis catalysts of the formula a process for making the same and their use in metathesis reactions such as ring closing or cross metathesis. The invention further relates to a process for the manufacture of a macrocyclic compound of formula VII which have the potential to be useful as HCV protease inhibitors.Type: GrantFiled: April 10, 2009Date of Patent: May 10, 2011Assignee: Roche Palo Alto LLCInventors: Kurt Puentener, Michelangelo Scalone
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Publication number: 20110105567Abstract: Disclosed herein are compounds represented by: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 21, 2008Publication date: May 5, 2011Applicant: Allergan, Inc.Inventors: Richard L. Beard, Hiaqing Yuan, John E. Donello, Ken Chow, Liming Wang
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Publication number: 20110098334Abstract: The present invention relates to a novel anhydrous crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt or hemi-calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium, its use in pharmaceutical compositions and the use of the new crystalline form and compositions in the treatment of hypertension and various other diseases.Type: ApplicationFiled: August 8, 2008Publication date: April 28, 2011Applicant: Generics [UK] LimitedInventor: Axel Becker
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Publication number: 20110098319Abstract: The invention relates to novel derivatives of short-chain fatty acids, in particular derivatives of butyric acid, useful for all the known clinical applications of the latter, which show physicochemical characteristics suitable for an easy oral administration, being devoid of the unpleasant organoleptic properties that characterize butyrate. The new compounds are amide derivatives which can be synthesized by reaction of the corresponding fatty acid halide with a naturally occurring amino acid, phenylalanine or a suitable derivative thereof, and which are in a poorly hygroscopic, easily weighable form, stable to acids and alkalis and able to release the acid at the small and large bowel level in a constant manner over time. They do not have disagreeable odors and are practically tasteless, thus allowing the manufacture of preparations for oral administration also suitable for the therapy of chronic diseases and in the pediatric field.Type: ApplicationFiled: April 21, 2009Publication date: April 28, 2011Inventors: Roberto Berni Canani, Antonio Calignano, Orietta Mazzoni, Anna Coruzzo
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Patent number: 7932269Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3 and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.Type: GrantFiled: January 14, 2009Date of Patent: April 26, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Patent number: 7928137Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.Type: GrantFiled: March 2, 2007Date of Patent: April 19, 2011Assignee: Tularik LimitedInventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan
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Publication number: 20110086311Abstract: A photosensitive resin composition which is excellent in resolution, low in cost, and usable in a wide range of structures of polymer precursors each of which is reacted into a final product by a basic substance or by heating in the presence of a basic substance. The photosensitive resin composition includes a base generator which has a specific structure and generates a base by exposure to electromagnetic radiation and heating, and a polymer precursor which is reacted into a final product by the base generator and by a basic substance or by heating in the presence of a basic substance.Type: ApplicationFiled: March 30, 2009Publication date: April 14, 2011Inventors: Mami Katayama, Shunji Fukuda, Katsuya Sakayori
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Publication number: 20110054190Abstract: Disclosed is a technology for enabling an efficient asymmetric Michael addition reaction which does not require a large amount of a malonic ester, while having a short reaction time. Specifically disclosed is a catalyst which is composed of MX2 (wherein M is Be, Mg, Ca, Sr, Ba or Ra and X is an arbitrary group) and a compound represented by general formula [I]. [In the formula, R7, R8, R9 and R10 each represents a substituted cyclic group or an unsubstituted cyclic group.Type: ApplicationFiled: January 28, 2009Publication date: March 3, 2011Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCYInventors: Shu Kobayashi, Magno Agostinho, Uwe Schneider, Miyuki Yamaguchi
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Publication number: 20110040090Abstract: The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in W02007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.Type: ApplicationFiled: April 30, 2009Publication date: February 17, 2011Applicant: Nerviano Medical Sciences S.r.l.Inventors: Matteo D'Anello, Carlo Battistini, Maria Gioia Fornaretto, Ermes Vanotti
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Patent number: 7851411Abstract: ?-Cyanoacrylates of the formula I, where: R1 is ORa wherein Ra is hydrogen, substituted alkyl, branched alkyl, branched alkenyl, cycloloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; is NRbRc wherein Rb is hydrogen, alkyl which may be substituted, alkenyl, alkynyl; Rc is hydrogen, alkyl which may be substituted alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; or Rb and Rc form an alkandiyl-chain which may be substituted; or is SRd wherein Rd is hydrogen, alkyl which may be substituted, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; R2 is alkyl which may be substituted; is alkenyl or alkynyl; R3 is alkyl may be substituted; is alkenyl or alkynyl; R4 is hydrogen, halogen, cyano or alkyl; and their agriculturally useful salts, processes and intermediates for their preparation; and the use of these compounds or of compositions comprising these compounds for controlling undesirable plants are described.Type: GrantFiled: December 17, 2002Date of Patent: December 14, 2010Assignee: BASF SEInventors: Peter Plath, Norbert Götz, Michael Rack, Andreas Landes, Cyrill Zagar, Matthias Witschel, Klaus Groβmann
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Patent number: 7842707Abstract: The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.Type: GrantFiled: July 21, 2005Date of Patent: November 30, 2010Assignee: Nuada, LLCInventors: Susan Marie Royalty, James Ford Burns, Jan Jozef Scicinski, Gunnar Erik Jagdmann, Jr., Robert James Foglesong, Kellee Griffin Ring, Tatyana Dyakonov, David Middlemiss
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Publication number: 20100292206Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 17, 2008Publication date: November 18, 2010Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20100286112Abstract: The present invention is directed to therapeutic compounds which have dual activity as agonists of GPR119 and inhibitors of DPP-IV and are useful for the treatment of metabolic disorders including type II diabetes.Type: ApplicationFiled: September 10, 2008Publication date: November 11, 2010Inventors: Oscar Barba, Stuart Edward Bradley, Matthew Colin Thor Fyfe, Patrick Eric Hanrahan, Thomas Martin Krulle, Martin James Procter, Christine Reynet McCormack, Karen Lesley Schofield, Donald Smyth, Alan John William Stewart, Simon Andrew Swain, Peter Widdowson
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Publication number: 20100280412Abstract: The present invention relates to a method for the anticoagulation of human blood ex vivo in which blood calcium concentration remains the same, no thrombin is formed and thrombocyte function is not affected. The invention further relates to a blood coagulation factor Xa inhibitor that can be advantageously used in this method, an agent that contains an inhibitor of the blood coagulation factor Xa, and a kit for diagnosing cellular blood components. The anticoagulated blood obtained according to the invention can be used for examining cellular blood components, for example for the diagnosis of thrombocyte function.Type: ApplicationFiled: January 26, 2007Publication date: November 4, 2010Inventors: Peter Hellstern, Jörg Stürzebecher
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Publication number: 20100280018Abstract: A compound of formula (I), or an enantiomer or diastereoisomer thereof, or a salt, hydrate or solvate thereof: for the treatment or prophylaxis of arthritis in mammals.Type: ApplicationFiled: July 20, 2010Publication date: November 4, 2010Applicants: Laboratoires Serono S.A., Vernalis (Oxford) LimitedInventors: Gilles Pain, Stephen John Davies, Agnes Bombrun
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100251603Abstract: Succinimide dispersant produced by reacting a hydrocarbyl-substituted succinic anhydride and an amine having at least one primary amino group and at least one secondary amino group where the succinimide detergents are useful as additives in fuels.Type: ApplicationFiled: October 23, 2008Publication date: October 7, 2010Inventors: Mark C. Davies, David J. Moreton
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Publication number: 20100247471Abstract: The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.Type: ApplicationFiled: July 28, 2008Publication date: September 30, 2010Applicant: Graceway Pharmaceuticals, LLCInventors: Jin Li, Nicole Lee Kolosko
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Publication number: 20100227894Abstract: The present invention provides novel benzamide derivatives of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: ApplicationFiled: June 7, 2007Publication date: September 9, 2010Inventors: Eldon Scott Priestley, Xiaojun Zhang
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Publication number: 20100204199Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.Type: ApplicationFiled: April 14, 2010Publication date: August 12, 2010Inventors: Xiang-Yang Ye, Jeffrey A. Robl, Ronald L. Hanson, Zhiwei Guo, Ramesh N. Patel
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Publication number: 20100190822Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: March 19, 2010Publication date: July 29, 2010Applicant: ABBOTT LABORATORIESInventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
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Patent number: 7754757Abstract: Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).Type: GrantFiled: February 1, 2005Date of Patent: July 13, 2010Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Kohei Ohata, Kazuya Yokota, Koji Murakami, Toshiyuki Matsui
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Patent number: 7741364Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: June 27, 2007Date of Patent: June 22, 2010Assignee: Abbott LaboratoriesInventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li
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Publication number: 20100152098Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: November 5, 2009Publication date: June 17, 2010Applicant: Mpex Pharmaceuticals, Inc.Inventors: Tomasz Glinka, Olga Rodny, Keith A. Bostian, David M. Wallace, Robert I. Higuchi, Chun Chow, Chi Ching Mak, Gavin Hirst, Brian Eastman
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Publication number: 20100152125Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: ApplicationFiled: March 20, 2008Publication date: June 17, 2010Applicant: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R.P. Novak
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Patent number: 7737139Abstract: Selected sulfonic acids, their derivatives and pharmaceutical compositions containing such compounds are useful in inhibiting the chernotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, the selected sulfonic acids and their derivativas are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: March 11, 2004Date of Patent: June 15, 2010Assignee: Dompe PHA.R.MA S.p.A.Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta
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Publication number: 20100113801Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: January 10, 2008Publication date: May 6, 2010Inventors: David Hook, Thomas Ruch, Bernhard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar M. Waykole
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Publication number: 20100099892Abstract: It is to provide a method for efficiently producing an aminoacetylpyrrolidinecarbonitrile derivative which is useful as a DPP-IV inhibitor. It is a method for producing an aminoacetylpyrrolidinecarbonitrile derivative represented by the formula (2): (in the formula, A and R1 are as defined in the following), comprising allowing an acid to act on an aminoacetylpyrrolidinecarboxamide derivative represented by the formula (1): (in the formula, A represents CH2, CHF or CF2; and R1 represents a secondary amino group which may be substituted), and then allowing a dehydrating agent to act thereon.Type: ApplicationFiled: March 21, 2008Publication date: April 22, 2010Inventors: Kazuo Orita, Takayuki Gotoh
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Publication number: 20100081702Abstract: Object The present invention provides a pharmaceutical composition for prophylaxis or treatment of hepatitis. Solution A pharmaceutical composition for prophylaxis or treatment of hepatitis, comprising a compound represented by the general formula (I): wherein R1 represents a C1-C4 alkyl group, R2 and R3 which are the same or different represent a hydrogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group, X represents a sulfur atom or a nitrogen atom substituted by a methyl group, and n represents an integer of 3 or 4, or a pharmacologically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: November 23, 2009Publication date: April 1, 2010Inventors: Takaichi Shimozato, Takashi Kagari, Hiromi Doi
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Publication number: 20100081701Abstract: The present invention concerns compounds, according to general formula (I), which find utility preferably for the treatment of cancer.Type: ApplicationFiled: August 31, 2006Publication date: April 1, 2010Inventor: David Michael EVANS
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Patent number: 7678826Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.Type: GrantFiled: May 22, 2006Date of Patent: March 16, 2010Inventors: Jake Axford, Urs Baettig, Brian Cox, Kamlesh Jagdis Bala, Catherine LeBlanc, David Andrew Sandham
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Patent number: 7678785Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: GrantFiled: July 24, 2007Date of Patent: March 16, 2010Assignee: UCB Pharma S.A.Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
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Publication number: 20100048589Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.Type: ApplicationFiled: August 11, 2009Publication date: February 25, 2010Inventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
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Publication number: 20100035930Abstract: The invention relates to compounds of the formula I as defined herein, which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. The compounds of the formula I are suitable for manufacturing medicaments for the prophylaxis, secondary prevention and therapy of one or more disorders which are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: June 8, 2009Publication date: February 11, 2010Applicant: SANOFI-AVENTISInventors: Christopher KALLUS, Mark BROENSTRUP, Werngard CZECHTIZKY, Andreas EVERS, Markus FOLLMANN, Nis HALLAND, Herman SCHREUDER
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Patent number: 7638638Abstract: Pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound with the formula: where the labeled substituents are as described herein.Type: GrantFiled: May 13, 2004Date of Patent: December 29, 2009Assignee: Takeda San Diego, Inc.Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Michael B. Wallace, Xiao-Yi Xiao, Zhiyuan Zhang
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Publication number: 20090286792Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: November 19, 2008Publication date: November 19, 2009Inventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Publication number: 20090281085Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: February 3, 2009Publication date: November 12, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
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Publication number: 20090275714Abstract: The invention relates to novel metathesis catalysts of the formula a process for making the same and their use in metathesis reactions such as ring closing or cross metathesis. The invention further relates to a process for the manufacture of a macrocyclic compound of formula VII which have the potential to be useful as HCV protease inhibitors.Type: ApplicationFiled: April 10, 2009Publication date: November 5, 2009Inventors: Kurt Puentener, Michelangelo Scalone
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Publication number: 20090247547Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, Y, Z, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: March 26, 2009Publication date: October 1, 2009Inventors: Michael SHULTZ, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Jianmei Fan, Gang Liu, Dyuti Majumdar
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Publication number: 20090240065Abstract: The black color material includes a condensation product of a pyrrole compound represented by the following formula (1) and a squaric acid represented by the following formula (2):Type: ApplicationFiled: September 30, 2008Publication date: September 24, 2009Applicant: FUJI XEROX CO., LTD.Inventors: Shinji HASEGAWA, Minquan TIAN, Yuka ITO, Kazuhiko HIROKAWA, Miho WATANABE, Makoto FURUKI
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Patent number: 7589216Abstract: The present invention is directed to a process for preparing intermediates that are useful to prepare certain antibacterial N-formyl hydroxylamine compounds which are peptide deformylase inhibitors. The process makes use ? ?-lactarn intermediate. Certain optically pure intermediates are also claimed.Type: GrantFiled: September 18, 2003Date of Patent: September 15, 2009Assignee: Novartis AGInventors: Prasad Koteswara Kapa, Xinglong Jiang, Eric M. Loeser, Joel Slade, Mahavir Prashad, George Tien-San Lee
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Publication number: 20090186920Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3 and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.Type: ApplicationFiled: January 14, 2009Publication date: July 23, 2009Inventors: HENNER KNUST, MATTHIAS NETTEKOVEN, EMMANUEL PINARD, OLIVIER ROCHE, MARK ROGERS-EVANS
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Publication number: 20090176847Abstract: The present invention relates to new dicyclooctane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and to uses for treatment especially for dipeptidyl peptidase inhibitor (DPPIV), in which each substituent group of general formula (I) is as defined in specification.Type: ApplicationFiled: March 28, 2007Publication date: July 9, 2009Inventors: Peng Cho Tang, Zhigang Lin, Lei Zhang, Qian Wang, Jialiang Yang, Yang Wang, Fuqiang Zhao