Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Diazine Ring Patents (Class 544/406)
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Patent number: 8034954Abstract: The present invention provides novel calcium channel antagonists, and methods of treating disease sates using the novel antagonists.Type: GrantFiled: December 20, 2006Date of Patent: October 11, 2011Assignee: Icagen, Inc.Inventors: Gregory J. Pacofsky, Mark J. Suto, Paul Christopher Fritch
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Publication number: 20110245226Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.Type: ApplicationFiled: June 8, 2011Publication date: October 6, 2011Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
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Publication number: 20110245444Abstract: A method for processing biomass comprising heating an aqueous slurry comprising biomass, water and a phosphate catalyst in a pressure vessel at a temperature of about 150° C. to about 500° C. to produce a mixture comprising a dispersion of an organic phase and an aqueous phase.Type: ApplicationFiled: September 11, 2009Publication date: October 6, 2011Applicant: AQUAFLOW BIONOMIC CORPORATION LIMITEDInventors: Ian James Miller, Rhys Antony Batchelor
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Patent number: 8017771Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.Type: GrantFiled: January 16, 2009Date of Patent: September 13, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Carl Alan Busacca, Rogelio Perez Frutos, Nizar Haddad, Suresh R. Kapadia, Jon Charles Lorenz, Anjan Saha, Chris Hugh Senanayake, Xudong Wei
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Publication number: 20110212968Abstract: The invention relates to novel phenethylamide derivatives and their wherein A, B, R1, R2 and R3 are as described in the application, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: October 13, 2009Publication date: September 1, 2011Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen, Daniel Trachsel, Jodi T. Williams
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Patent number: 8008297Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: GrantFiled: April 4, 2008Date of Patent: August 30, 2011Assignee: Ambrilia Biopharma Inc.Inventors: Brent Richard Stranix, Valerie Perron
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Publication number: 20110207737Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.Type: ApplicationFiled: November 11, 2009Publication date: August 25, 2011Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
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Publication number: 20110201603Abstract: 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: ApplicationFiled: July 30, 2009Publication date: August 18, 2011Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Kei Domon, Yukiyoshi Watanabe, Yasushi Yoneta, Takuma Mori, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Masashi Ataka, Ulrich Görgens
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Patent number: 7994179Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ?O; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.Type: GrantFiled: December 19, 2008Date of Patent: August 9, 2011Assignee: AstraZeneca ABInventors: Petra Johannesson, Jan Magnus Johansson, Annika Ulrika Petersson, Alan Martin Birch, Roger John Butlin
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Patent number: 7994093Abstract: The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, provided that the ring is not 1,2,3-triazole, the ring being substituted by groups R8, R9 and R10; X is a single or double bond; Y is O, S, N(R11) or (CR12R13)(CR14R15)m(CR16R17)n; m is 0 or 1; n is 0 or 1; and R1 to R17 each, independently, have a range of values; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: GrantFiled: August 28, 2009Date of Patent: August 9, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Josef Ehrenfreund, Hans Tobler, Harald Walter
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Publication number: 20110182828Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.Type: ApplicationFiled: December 18, 2008Publication date: July 28, 2011Applicant: Schering CorporationInventors: John C. Anthes, Kevin D. Mccormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Daniel M. Solomon, Phillippa H. Solomon, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar
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Publication number: 20110183955Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases.Type: ApplicationFiled: March 21, 2011Publication date: July 28, 2011Applicant: NOVARTIS AGInventors: Robert ECKL, Roswitha TAUBE, Michael ALMSTETTER, Michael THORMANN, Andreas TREML, Christopher STRAUB, Zhuoliang CHEN
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Publication number: 20110166161Abstract: This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.Type: ApplicationFiled: September 17, 2009Publication date: July 7, 2011Applicant: Astellas Pharma Inc.Inventors: Takeshi Terasawa, Shinji Shigenaga, Shinji Itoh, Jun Maeda, Hideyuki Watanabe, Satoshi Kubo, Noe Iahii
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Publication number: 20110166141Abstract: Cathepsin S inhibitors having formula (I), (II), (III) or (IV) as shown in the specification. These inhibitors can be used to treat cancer and autoimmune/inflammatory diseases.Type: ApplicationFiled: December 6, 2010Publication date: July 7, 2011Applicants: DCB-USA, LLC, National Tsing Hua University, National Health Research InstitutesInventors: Chun-Cheng Lin, Wun-Shaing Wayne Chang, Biing-Jiun Uang, Jang-Yang Chang, Jo-Chun Chen, Hsing-Pang Hsieh
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Publication number: 20110112114Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.Type: ApplicationFiled: June 9, 2010Publication date: May 12, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Roger D. Tung, Govinda Rao Bhisetti, Luc J. Farmer
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Publication number: 20110092698Abstract: The invention is concerned with novel bicyclic compounds of formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, and R10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor may be used, for example, in the prevention and/or treatment of inflammatory diseases, particularly peripheral arterial occlusive diseases or atherothrombosis.Type: ApplicationFiled: October 11, 2010Publication date: April 21, 2011Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei
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Publication number: 20110082156Abstract: The invention relates to fatty acid acipimox derivatives; compositions comprising an effective amount of a fatty acid acipimox derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid acipimox derivative.Type: ApplicationFiled: October 5, 2010Publication date: April 7, 2011Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 7919497Abstract: Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.Type: GrantFiled: September 20, 2006Date of Patent: April 5, 2011Assignee: Nereus Pharmaceuticals, Inc.Inventors: Michael Palladino, George Kenneth Lloyd, Yoshio Hayashi
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Patent number: 7910735Abstract: Substituted pyrazinecarboxylic acid anilide derivatives represented by the general formula (I) or salts thereof; intermediates of them; pesticides (such as insecticides and acaricides) for agricultural and horticultural use, containing the compounds as the active ingredient; and usage thereof: wherein R1 is H, C1-6 alkyl, halo C1-6 alkyl, or the like; R2 is halogeno, C1-6 alkyl, or the like; G is C2-10 alkyl or the like; Z is oxygen or sulfur; X's are each independently H, halogeno, or the like; Y's are each independently H, halogeno, cyano, or the like; and m and n are each an integer of 1 to 3.Type: GrantFiled: May 26, 2005Date of Patent: March 22, 2011Assignee: Nihon Nohyaku Co., Ltd.Inventors: Takashi Furuya, Kozo Machiya, Akiyuki Suwa, Shinsuke Fujioka
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Patent number: 7888351Abstract: The present invention relates to compounds of the formula; and their use in therapy.Type: GrantFiled: April 10, 2007Date of Patent: February 15, 2011Assignee: Novartis AGInventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
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Patent number: 7884108Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/ or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: GrantFiled: September 19, 2008Date of Patent: February 8, 2011Assignee: CGI Pharmaceuticals, Inc.Inventors: Peter A. Blomgren, Kevin S. Currie, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Zhongdong Zhao, Pavel E. Zhichkin, Douglas G. Stafford, Jeffrey E. Kropf
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Publication number: 20110021523Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: CHEMOCENTRYX, INC.Inventors: Solomon Ugashe, Zheng Wei, J.J. Wright, Andrew Pennell
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Patent number: 7875619Abstract: The present invention relates to group of butylphenyl-pyrazinoylguanidine compounds useful as sodium channel blockers. The compounds may be used to promote promoting hydration of mucosal surfaces.Type: GrantFiled: February 18, 2004Date of Patent: January 25, 2011Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Publication number: 20110009426Abstract: The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.Type: ApplicationFiled: August 6, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Jean-Michel Altenburger, Valérie Fossey, Daniel Galtier, Frédéric Petit
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Publication number: 20100328600Abstract: The invention provides a liquid crystal compound having stability to heat, light and so forth, a wide temperature range of a nematic phase, a small viscosity, a suitable optical anisotropy, a suitable elastic constant K33, a suitable and negative dielectric anisotropy, and an excellent compatibility with other liquid crystal compounds. The invention provides a liquid crystal composition containing the compound described above and having stability to heat, light and so forth, a small viscosity, a suitable optical anisotropy, a suitable and negative dielectric anisotropy, a suitable elastic constant K33, a low threshold voltage, a high maximum temperature of a nematic phase, and a low minimum temperature of the nematic phase. The invention also provides a liquid crystal display device having a short response time, a small power consumption, a low driving voltage, and a large contrast, and containing the composition described above which can be used in a large temperature range.Type: ApplicationFiled: September 1, 2008Publication date: December 30, 2010Applicants: CHISSO CORPORATION, CHISSO PETROCHEMICAL CORPORATIONInventors: Teru Shimada, Masahide Kobayashi
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Publication number: 20100324071Abstract: Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Yan Shi, Peter T. W. Cheng, Ying Wang, Denis E. Ryono
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Publication number: 20100324068Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X2 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or —CONHSO2Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.Type: ApplicationFiled: June 18, 2010Publication date: December 23, 2010Applicant: AstraZeneca ABInventors: Alan Martin Birch, Roger John Butlin, Leonie Campbell, Clive Green, Andrew Leach, Michael James Waring, Paul Michael Murray, Per Olof Ryberg
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Patent number: 7851476Abstract: Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine its salts and solvates thereof are herein set forth, as are pharmaceutical compositions comprising the crystalline form(s), as well of methods of using the crystalline form(s) in the treatment of HIV and/or AIDS, and methods for obtaining such crystalline form(s).Type: GrantFiled: December 11, 2006Date of Patent: December 14, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Chung-Pin H. Chen, Dawn DiGiugno Parker, Qi Gao, Chong-Hui Gu, Jaquan Kalani Levons, Bing-Shiou Yang
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Publication number: 20100311974Abstract: Substituted pyrazinecarboxylic acid anilide derivatives represented by the general formula (I) or salts thereof; intermediates of them; pesticides (such as insecticides and acaricides) for agricultural and horticultural use, containing the compounds as the active ingredient; and usage thereof: wherein R1 is H, C1-6 alkyl, halo C1-6 alkyl, or the like; R2 is halogeno, C1-6 alkyl, or the like; G is C2-10 alkyl or the like; Z is oxygen or sulfur; X's are each independently H, halogeno, or the like; Y's are each independently H, halogeno, cyano, or the like; and m and n are each an integer of 1 to 3.Type: ApplicationFiled: July 29, 2010Publication date: December 9, 2010Inventors: Takashi FURUYA, Kozo Machiya, Akiyuki Suwa, Shinsuke Fujioka
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Patent number: 7838673Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: October 16, 2007Date of Patent: November 23, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Edward J. Olhava, Mihaela Diana Danca
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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
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Patent number: 7820671Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: GrantFiled: August 31, 2001Date of Patent: October 26, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Edward Babine, Shu Hui Chen, Ivan Collado, Cristina Garcia-Paredes, John Irvin Glass, Deqi Guo, Ling Jin, Jason Eric Lamar, Raymond Samuel Parker, III, Nancy June Snyder, Xicheng David Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Robert B. Perni, Luc Farmer
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Publication number: 20100267745Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.Type: ApplicationFiled: June 29, 2010Publication date: October 21, 2010Inventors: Mirjana Andjelkovic, Agnès Bénardeau, Evelyne Chaput, Paul Hebeisen, Matthias Nettekoven, Ulrike Obst Sander, Constantinos G. Panousis, Stephan Roever
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Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Publication number: 20100249124Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20100226597Abstract: The present application provides a process for the preparation of Bortezomib, its intermediates and process for crystalline forms of Bortezomib.Type: ApplicationFiled: September 12, 2008Publication date: September 9, 2010Applicants: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.Inventors: Raghavendracharyulu Venkata Palle, Rajasekhar Kadaboina, Veerendeer Murki, Amarendhar Manda, Nageshwar Gunda, Ramaseshagiri Rao Pulla, Mallesha Hanmanthu, Narasimha Naidu Mopidevi, Suresh Kumar Ramdoss
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Publication number: 20100222366Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.Type: ApplicationFiled: July 23, 2008Publication date: September 2, 2010Inventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
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Publication number: 20100210841Abstract: A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defined in the specification, is described. Novel intermediates are also described and claimed.Type: ApplicationFiled: February 15, 2010Publication date: August 19, 2010Applicant: AstraZeneca ABInventors: Michael Butters, Jeffrey Crabb, Philip Hopes, Bharti Patel
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Publication number: 20100174077Abstract: The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.Type: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Gerald J. Tanoury, Minzhang Chen, John E. Cochran, Valdas Jurkauskas
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Patent number: 7745442Abstract: Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided including administering a sodium channel blocker or pharmaceutically acceptable salts thereof to one or more members of a population at risk of exposure to or already exposed to one or more airborne pathogens, either from natural sources or from intentional release of pathogens into the environment.Type: GrantFiled: August 18, 2004Date of Patent: June 29, 2010Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Samuel E. Hopkins
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Patent number: 7745444Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: GrantFiled: April 10, 2008Date of Patent: June 29, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert B. Perni, John J. Court, Shawn D. Britt, Janos Pitlik, John H. van Drie
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Patent number: 7732449Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: wherein Q is an optionally substituted piperazinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.Type: GrantFiled: January 28, 2009Date of Patent: June 8, 2010Assignee: IRM LLCInventors: Hong Liu, Arnab K. Chatterjee, David C. Tully, Phillip B. Alper, David H. Woodmansee
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Publication number: 20100056786Abstract: The present invention relates to a novel process for preparing known fungicidally active alkylanilides from 2-alkylhaloaromatics and heterocyclylamides.Type: ApplicationFiled: July 12, 2007Publication date: March 4, 2010Applicant: Bayer CropScience AGInventor: Alexander Straub
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Publication number: 20100041653Abstract: The present disclosure provides compounds having the general structure A or pharmaceutically acceptable salts thereof: R—X??(A) wherein R is an alkyl or aryl moiety comprising heterocyclic structures; and X is a metal-chelatin group selected from: This disclosure further provides a focused library of compounds for use in the discovery and design of metallo-enzyme inhibitors. This fragment-based approach provides an assembly of a library of low molecular weight compounds (MW<300 Da) containing a variety of potential metal-chelating groups. The identification of the inhibitory scaffolds among these compounds provides the initial hit fragments that may be optimized for affinity against a particular target using common medicinal chemistry, structure-based or NMR-based approaches.Type: ApplicationFiled: August 14, 2009Publication date: February 18, 2010Applicants: BURNHAM INSTITUTE FOR MEDICAL RESEARCH, THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Maurizio Pellecchia, Seth M. Cohen
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Publication number: 20100041887Abstract: Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: October 20, 2009Publication date: February 18, 2010Inventors: Stephen Paul Collingwood, Brian Cox, Urs Baettig, Gurdip Bhalay, Nicholas James Devereux
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Patent number: 7662825Abstract: The invention provides N-pyrazinyl-phenyl-sulphonamides of formula (I) for use in the treatment of chemokine mediated diseases. Particularly inflammatory diseases, such as asthma.Type: GrantFiled: January 14, 2003Date of Patent: February 16, 2010Assignee: AstraZeneca ABInventors: Andrew Baxter, Timothy Johnson, Nicholas Kindon, Bryan Roberts, Michael Stocks
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Patent number: 7659272Abstract: 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: GrantFiled: October 16, 2007Date of Patent: February 9, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Chen Shaowu
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Publication number: 20100029687Abstract: [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. [Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).Type: ApplicationFiled: November 14, 2007Publication date: February 4, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
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Publication number: 20100029686Abstract: This invention relates to: (a) compounds of formula I and salts thereof that, inter alia, are useful as hepatitis C virus (HCV) inhibitors; (b) intermediates useful for the preparation of such compounds and salts; (c) pharmaceutical compositions comprising such compounds and salts; and (d) methods of use of such compounds, salts, and compositions.Type: ApplicationFiled: June 26, 2009Publication date: February 4, 2010Applicant: Abbott LaboratoriesInventors: Brian E. Green, David D. Anderson, Todd D. Bosse, Curt S. Cooper, Larry L. Klein, Allan C. Krueger, Daniel P. Larson, Dachun Liu, Keith F. McDaniel, Christopher E. Motter, John K. Pratt, Todd W. Rockway, Teresa A. Rosenberg, Ming C. Yeung, Hui-Ju Chen, Jason P. Shanley