Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Five- Membered Ring By Nonionic Bonding Patents (Class 546/279.1)
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Publication number: 20110178077Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: June 17, 2009Publication date: July 21, 2011Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
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Patent number: 7977371Abstract: Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease.Type: GrantFiled: February 26, 2008Date of Patent: July 12, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kenji Kawashima, Hiroshi Enomoto, Noriko Ishizaka, Minoru Yamamoto, Kazuhiro Kudou, Masaaki Murai, Takaaki Inaba, Kazuyoshi Okamoto
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Publication number: 20110166096Abstract: Disclosed are uracil derivatives of the formula (I): wherein R1, R2, R3, and X are as defined herein, and use thereof as therapeutic agents. The uracil derivatives are used in particular together with a cytostatic agent for suppressing or reducing resistance building up on cytostatic treatment.Type: ApplicationFiled: June 25, 2009Publication date: July 7, 2011Applicant: RESPROTECT GMBHInventors: Rudolf Fahrig, Kurt Eger, Martin Führer, Nicole Heinze, Matthias Klemm, Jörg-Christian Heinrich
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Publication number: 20110160163Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: March 1, 2011Publication date: June 30, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: John Cochran, Vincent Galullo, Guy W. Bemis
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Publication number: 20110160192Abstract: Compounds of formula (I): Z?-CO-A-B—NH-Z (I) wherein: Z is H or an amino protecting group; Z? is OH, a protected or activated hydroxyl group or Cl; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.Type: ApplicationFiled: March 7, 2011Publication date: June 30, 2011Applicant: SPIROGEN LIMITEDInventors: Philip Wilson Howard, Geoffrey Wells
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Patent number: 7968550Abstract: The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.Type: GrantFiled: January 11, 2007Date of Patent: June 28, 2011Assignees: Aventis Pharma Deutschland GmbH, Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Thomas Boehme, Gerhard Hessler, Petra Stahl, Dirk Gretzke
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Patent number: 7968591Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.Type: GrantFiled: December 9, 2008Date of Patent: June 28, 2011Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
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Publication number: 20110152533Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Applicant: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20110135691Abstract: The present invention is directed to immune adjuvants containing IAP inhibitors, including Smac mimetics. The invention further provides pharmaceutical compositions and vaccines containing an IAP inhibitor and an antigen. Methods of enhancing an immune response by administration of an IAP inhibitor, methods of treating or preventing cancer, methods of treating or preventing infections, methods of treating autoimmune disorders, and methods of potentiating cytokine or antibody production are also provided.Type: ApplicationFiled: May 14, 2009Publication date: June 9, 2011Inventors: Leigh Zawel, Christopher S. Straub, Brant G. Firestone, Glenn Dranoff, Michael Dougan
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Publication number: 20110136874Abstract: The present invention relates to fungicide N-(2-pyridylpropyl)carboxamide derivative and its oxa, aza and thia analogues of formula (I), their process of preparation and intermediate compound for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. wherein A, T, W, X, n and Z3 to Z7 represent various substituents.Type: ApplicationFiled: August 6, 2009Publication date: June 9, 2011Inventors: Samir Bennabi, Pierre-Yves Coqueron, Philippe Desbordes, Stéphanie Gary, Rachel Rama, Philippe Rinolfi, Jürgen Benting, Peter Dahmen
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Patent number: 7951826Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.Type: GrantFiled: March 13, 2006Date of Patent: May 31, 2011Assignee: Eli Lilly and CompanyInventors: Lisa Selsam Beavers, Don Richard Finley, Robert Alan Gadski, Philip Arthur Hipskind, Cynthia Darshini Jesudason, Richard Todd Pickard, Freddie Craig Stevens, Takako Takakuwa
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Publication number: 20110118283Abstract: There are provided compounds of the formula wherein R1, R2, R3, R3, R4, R5 are as described herein and enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: ApplicationFiled: October 6, 2010Publication date: May 19, 2011Inventors: Qingjie Ding, Nan Jiang, Jin-Jun Liu, Jing Zhang, Zhuming Zhang
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Publication number: 20110118320Abstract: The invention relates to substituted pyrrole compounds of Formula (I) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: June 10, 2009Publication date: May 19, 2011Inventors: Lewis J. Gazzard, Joseph Lyssikatos
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Patent number: 7943642Abstract: Certain novel N,N-di(heteroarylalkyl)amine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein Ar Ar1, a, b, c, R, Rd, Re, Rf, Rg, Rh, R?, R3 and Rk are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: October 27, 2005Date of Patent: May 17, 2011Assignee: FMC CorporationInventors: David M. Roush, John F. Chiarello, George Theodoridis, Hongyan Qi
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Patent number: 7939547Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.Type: GrantFiled: May 15, 2007Date of Patent: May 10, 2011Assignee: IRM LLCInventors: David C. Tully, Arnab K. Chatterjee, Hank Michael James Petrassi, Badry Bursulaya, Glen Spraggon
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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: 20110092474Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: June 11, 2009Publication date: April 21, 2011Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
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Publication number: 20110086854Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.Type: ApplicationFiled: October 6, 2010Publication date: April 14, 2011Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Publication number: 20110077395Abstract: 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: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R6, R7, and R8 are defined herein.Type: ApplicationFiled: December 2, 2010Publication date: March 31, 2011Inventors: James J. Li, Lawrence G. Hamann, Zheming Ruan, Christopher B. Cooper, Shung C. Wu, Ligaya M. Simpkins, Haixia Wang, Akbar Nayeem, Stanley R. Krystek
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Publication number: 20110077160Abstract: Compounds having the following generic formula are disclosed.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Inventors: Nneka T. Breaux, Michael R. Loso, Timothy C. Johnson, Jonathan M. Babcock, Benjamin M. Nugent, Timothy P. Martin, Annette V. Brown, Ronald Ross, JR., William C. Lo, Matthias S. Ober
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Patent number: 7915291Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: GrantFiled: September 2, 2008Date of Patent: March 29, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
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Publication number: 20110071298Abstract: The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.Type: ApplicationFiled: October 12, 2010Publication date: March 24, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Gerald J. Tanoury, Minzhang Chen, Andrew D. Jones, Philip L. Nyce, Martin Trudeau, David J. Guerin, John R. Snoonian
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Publication number: 20110071291Abstract: A hydrazide compound represented by the formula (1): (wherein R1, R2, R3, R4, A1, A2, J, Q and n are defined in the specification) has excellent pesticidal activity.Type: ApplicationFiled: November 19, 2010Publication date: March 24, 2011Inventors: Hiroshi Ikegami, Markus Jachmann, Yoshihiko Nokura, Chiemi Iwata
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Publication number: 20110065726Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: ApplicationFiled: July 31, 2007Publication date: March 17, 2011Inventors: Zhuoliang CHEN, Sushil Kumar Sharma, Christopher Straub, Mark G. Charest, Feng He, Run-Ming David Wang, Leigh Zawel, Christine Hiu-Tung Chen, Miao Dai, Huangshu Lei, Ly Pham, Fan Yang
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Publication number: 20110059942Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.Type: ApplicationFiled: October 20, 2008Publication date: March 10, 2011Inventors: Matthew ColinThor Fyfe, William Gattrell, Colin Peter Sambrook-Smith, Simon Andrew Swain
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Publication number: 20110060015Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.Type: ApplicationFiled: May 12, 2009Publication date: March 10, 2011Inventors: Giuseppe Alvaro, Agostino Marasco
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Publication number: 20110052552Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosedType: ApplicationFiled: November 4, 2010Publication date: March 3, 2011Inventors: Judith KELLEHER-ANDERSSON, Karl K. Johe
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Publication number: 20110041262Abstract: The invention relates to the dyeing of keratin fibres using azomethine direct dyes or reduced precursors of azomethine direct dyes of formula (I) and (II) obtained from 2-amino-3-hydroxypyridine. The invention relates to a dye composition comprising at least one azomethine direct dye or a reduced precursor of an azomethine direct dye, to a process for dyeing keratin fibres, using the said composition, and to their uses in the dyeing of keratin fibres. This composition allows a particularly stable and fast coloration to be obtained.Type: ApplicationFiled: December 9, 2008Publication date: February 24, 2011Inventors: Madeleine Leduc, Eric Metais, Stéphane Sabelle, Christophe Rondot
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Publication number: 20110034378Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.Type: ApplicationFiled: January 21, 2009Publication date: February 10, 2011Inventors: Chaitanya Dutt, Deepa Joshi, Ram Gupta, Kumarprafull Chandra
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Patent number: 7879852Abstract: The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.Type: GrantFiled: July 13, 2007Date of Patent: February 1, 2011Assignee: LG Life Sciences Ltd.Inventors: Sung Pil Choi, In Ae Ahn, Sang Hyup Lee, Sang Dae Lee, Mi Sook Shin, Koo Lee, Deog Young Choi, Dong Sup Shim, Hyeon Joo Yim, Min Kyung Yoon, Soo Yong Chung, Jung Ae Lee, Yong Hwa Ha, Young Kwan Kim, Oeuk Park, Hyun Min Lee, Youn Hoa Kim
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Publication number: 20110015232Abstract: The present invention relates to novel IAP inhibitor compounds of: Formula (I).Type: ApplicationFiled: October 10, 2007Publication date: January 20, 2011Inventors: Mark G. Charest, Christine Hiu-Tung CHEN, Ming Chen, Zhuoliang Chen, Miao Dai, Feng He, Huangshu Lei, Christopher Straub, Run-Ming David Wang, Leigh Zawel
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Patent number: 7872141Abstract: The invention is concerned with processes for the manufacture of the pyrrolidine-3,4-dicarboxamide derivative of formula (I), and the intermediates useful for those processes of manufacture.Type: GrantFiled: December 19, 2007Date of Patent: January 18, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Michel Adam, Pascal Dott, Hans Iding, Hans-Juergen Mair, Reinhard Reents, Beat Wirz
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Publication number: 20110005947Abstract: The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.Type: ApplicationFiled: May 6, 2010Publication date: January 13, 2011Applicant: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Jack W. Rose, Yonghong Song, Qing Xu, Mukund Mehrotra, Wolin Huang, Anjali Pandey
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Patent number: 7868014Abstract: The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.Type: GrantFiled: October 13, 2005Date of Patent: January 11, 2011Assignee: Eli Lilly and CompanyInventors: Thomas Charles Britton, Veronique Dehlinger, Colin Peter Dell, Bruce Anthony Dressman, Jason Kenneth Myers, Eric Samuel Nisenbaum
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Publication number: 20100331303Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: August 20, 2010Publication date: December 30, 2010Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
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Publication number: 20100324010Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: October 14, 2008Publication date: December 23, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Amano
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Patent number: 7855290Abstract: A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.Type: GrantFiled: August 23, 2006Date of Patent: December 21, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Tomohiro Matsushima, Keiko Takahashi, Setsuo Funasaka, Shuji Shirotori
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Publication number: 20100317568Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: June 10, 2010Publication date: December 16, 2010Applicant: ABBOTT LABAORATORIESInventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd N. Soltwedel, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Michael J. Lavin, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi
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Publication number: 20100305200Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: December 10, 2008Publication date: December 2, 2010Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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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: 20100280009Abstract: The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: December 10, 2008Publication date: November 4, 2010Inventors: Shawn J. Stachel, Thomas Steele, Alessia Petrocchi
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Patent number: 7820699Abstract: The invention is concerned with cyclic amines of formula (I) wherein X1 to X3, Y1 to Y3, R1?, R1? and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit coagulation factor Xa and can be used as medicaments and for treating diseases associated with coagulation factor Xa.Type: GrantFiled: April 13, 2006Date of Patent: October 26, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Narendra Panday, Fabienne Ricklin, Beat Wirz
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Publication number: 20100256144Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: ApplicationFiled: June 26, 2008Publication date: October 7, 2010Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Adreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Patent number: 7807672Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: GrantFiled: February 13, 2007Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
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Publication number: 20100249049Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 7, 2010Publication date: September 30, 2010Inventors: Hiroshi MIYAZAKI, Junko TSUBAKIMOTO, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAL, Tetsuya YANAGIDA, Yataka HISADA
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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: 20100216748Abstract: 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: ApplicationFiled: May 7, 2010Publication date: August 26, 2010Applicant: 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: 20100216806Abstract: Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu, Zhenshan Zhang
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Publication number: 20100216813Abstract: The present invention relates to a compound represented by the following formula I or a pharmaceutically acceptable salt thereof; wherein R1, R2, and y are defined herein. The present invention further relates to compositions that include the compound of the present invention as well as a method of treating a patient from endometreosis or uterine fibroids.Type: ApplicationFiled: November 29, 2006Publication date: August 26, 2010Inventor: James S. Frazee
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Patent number: 7767699Abstract: The invention provides a compound of formula (I): (where R1, Q, A and R2 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Pyridine-alkynyl Compound”); pharmaceutical compositions comprising an effective amount of a Pyridine-alkynyl Compound; and methods for treating or preventing a condition such as pain, urinary incontinence, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, a seizure, stroke, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a Pyridine-alkynyl Compound.Type: GrantFiled: December 22, 2005Date of Patent: August 3, 2010Assignee: Purdue Pharma, L.P.Inventors: Donald J. Kyle, Qun Sun, Xiaoming Zhou