Additional Hetero Ring Which Is Unsaturated Patents (Class 544/310)
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Publication number: 20120035157Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AstraZeneca ABInventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
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Publication number: 20120028997Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.Type: ApplicationFiled: December 16, 2010Publication date: February 2, 2012Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara Miskowski, Janet L. Ralbovsky, Mark Schulz
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Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Publication number: 20120015966Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Inventors: Jack Lin, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
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Publication number: 20120010192Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 30, 2011Publication date: January 12, 2012Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Publication number: 20110319400Abstract: Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.Type: ApplicationFiled: June 27, 2011Publication date: December 29, 2011Inventors: Christopher M. Flores, Paul R. Wade
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Publication number: 20110319439Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.Type: ApplicationFiled: March 9, 2010Publication date: December 29, 2011Inventor: Saleem Ahmad
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Publication number: 20110312974Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Nicholas Simone Stock, Yen Pham Truong, Jeffrey Roger Roppe, Deborah Volkots, Jill Melissa Scott, Timothy Andrew Parr, Bowei Wang, Thomas Jon Seiders, Ryan Clark, Heather Renee Coate
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Publication number: 20110281874Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Ronald Jay HINKLIN, Ajay SINGH
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Publication number: 20110269960Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).Type: ApplicationFiled: July 11, 2011Publication date: November 3, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Naoya ONO, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Makoto Yagi, Masakazu Sato
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Publication number: 20110257169Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.Type: ApplicationFiled: May 19, 2011Publication date: October 20, 2011Applicant: NYCOMED GmbHInventor: Ulrich KAUTZ
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Publication number: 20110245241Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: October 8, 2010Publication date: October 6, 2011Inventors: B. Narasimhulu Naidu, Kevin Peese, Ira B. Dicker, Chen Li, Manoj Patel, Nicholas A. Meanwell, Michael A. Walker
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Publication number: 20110245227Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.Type: ApplicationFiled: June 14, 2011Publication date: October 6, 2011Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Patent number: 8030322Abstract: The present invention relates to compounds of formula (I) or salts thereof wherein A, X, R2, R4 and n are defined herein, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g., to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or to enhance cognition.Type: GrantFiled: April 24, 2007Date of Patent: October 4, 2011Assignee: Glaxo Group LimitedInventors: Barbara Bertani, Romano Di Fabio, Fabrizio Micheli, Alessandra Pasquarello, Luca Tarsi, Silvia Terreni
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Patent number: 8030339Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: October 12, 2006Date of Patent: October 4, 2011Assignee: Neurosearch A/SInventors: William Dalby Brown, Janus S. Larsen, Lene Teuber, David Tristram Brown, Philip K. Ahring, Naheed Mirza, Elsebet Østergaard Nielsen
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Publication number: 20110236312Abstract: The invention provides compounds that comprise a 4?-thio nucleoside that is a derivative of 4?-thiothymidine or 4?-thio-2?-deoxyuridine comprising a positron or single photon emitting radioisotope or corresponding non-radioactive isotope attached via a triazole link to the N-3 position. Methods for preparing such compounds and uses of the compounds in medicine are also provided.Type: ApplicationFiled: August 28, 2009Publication date: September 29, 2011Applicant: IMPERIAL INNOVATIONS LIMITEDInventors: Eric Ofori Aboagye, Graham Smith
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Patent number: 8026244Abstract: There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.Type: GrantFiled: April 12, 2007Date of Patent: September 27, 2011Assignee: AstraZeneca ABInventors: Anna-Karin Tiden, Jenny Viklund
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Publication number: 20110230472Abstract: It is an object of the present invention to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused azole compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 25, 2009Publication date: September 22, 2011Applicant: Shionogi & Co., Ltd.Inventors: Yasunori Mitsuoka, Manami Masuda, Daisuke Taniyama
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Patent number: 8022221Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: February 12, 2009Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
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Patent number: 8017785Abstract: Phosphoric acid, edisylic acid (1,2-ethanedisulfonic acid), citric acid, orotic acid (uracil-6-carboxylic acid), R-mandelic acid, sulfuric acid, 1,5-naphthalenedisulfonic acid, D-aspartic acid, and lysine monohydrochloride salts of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine, and methods for their preparation, pharmaceutical compositions comprising said salts, and use, are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.Type: GrantFiled: May 8, 2007Date of Patent: September 13, 2011Assignees: AstraZeneca AB, Targacept, Inc.Inventors: Caroline Ericsson, Martin Bohlin, Tesfai Sebhatu, Gary M. Dull, Julio A. Munoz, Craig H. Miller
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Publication number: 20110184173Abstract: The present invention is a compound having the general formula (I), (II), or (III) or a pharmacologically acceptable salt, solvate, or hydrate thereof, and a pharmaceutical composition containing such a compound, or its pharmacologically acceptable ester, or other pharmacologically acceptable derivative thereof as an active ingredient. The compound has an excellent ACAT 2-inhibiting activity by a mechanism different from that of a statin drug and is useful as a therapeutic or prophylactic agent for obesity, adiposis, hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, and arteriosclerosis, as well as obesity-derived hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, arteriosclerosis, and hypertension.Type: ApplicationFiled: December 17, 2008Publication date: July 28, 2011Applicant: THE KITASATO INSTITUTEInventors: Hiroshi Tomoda, Tohru Nagamitsu, Satoshi Omura
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Publication number: 20110178294Abstract: Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: ApplicationFiled: December 3, 2010Publication date: July 21, 2011Applicant: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Vogelbacher, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Manfred Raschack
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Publication number: 20110165118Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 13, 2008Publication date: July 7, 2011Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
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Publication number: 20110136796Abstract: Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: ApplicationFiled: April 24, 2009Publication date: June 9, 2011Applicants: NEWLINK GENETICS, LANKEANAU INSTITUTE FOR MEDICAL RESEARCHInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Nicholas N. Vahanian, Charles J. Link, Judith Lalonde, George Prendergast, Alexander Muller, William Malachowski
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Publication number: 20110123490Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: December 14, 2010Publication date: May 26, 2011Applicant: Roche Palo Alto LLCInventors: RYAN CRAIG SCHOENFELD, Leanna Renee Staben, Francisco Xavier Talamas
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Publication number: 20110124619Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: November 17, 2010Publication date: May 26, 2011Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Publication number: 20110112080Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Inventors: Guido Galley, Roger Norcross, Alessandra Polara
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Publication number: 20110104109Abstract: The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Frank Bennett, Qingbei Zeng, Srikanth Venkatraman, Mousumi Sannigrahi, Kevin X. Chen, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20110105483Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperprolif erative disorders, such as cancer, in a subject in need thereof.Type: ApplicationFiled: February 8, 2008Publication date: May 5, 2011Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan Michael Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Przewloka
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Publication number: 20110105455Abstract: 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 R1, Y, R2, R3, and Ra are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: STEVEN J. COATS, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A. Miskowski, Scott L. Dax, Henry Breslin, Bart L. De Corte, Wei He
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Publication number: 20110082163Abstract: Provided is a uracil compound or a salt thereof, which has potent human dUTPase inhibitory activity and is useful as, for example, an antitumor drug. A uracil compound represented by the general formula (I) or a salt thereof: wherein n represents an integer of 1 to 3; X represents a bond, an oxygen atom, a sulfur atom, or the like; Y represents a linear or branched alkylene group having 1 to 8 carbon atoms, or the like; and Z represents —SO2NR1R2 or —NR3SO2—R4, wherein R1 and R2 each represent an alkyl group having 1 to 6 carbon atoms, an aralkyl group which is optionally substituted, or the like; R3 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R4 represents an aromatic hydrocarbon group, an unsaturated heterocyclic group, or the like.Type: ApplicationFiled: June 2, 2009Publication date: April 7, 2011Applicant: Taiho Pharmaceutical Co., Ltd.Inventors: Masayoshi Fukuoka, Tatsushi Yokogawa, Seiji Miyahara, Hitoshi Miyakoshi, Wakako Yano, Junko Taguchi, Yayoi Takao
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Publication number: 20110076276Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: June 26, 2008Publication date: March 31, 2011Applicants: Gilead Sciences, Inc., Korean Research Institute of Chemical TechnologyInventors: Hongyan Guo, Choung U. Kim, Ill Y. Lee, Michael L. Mitchell, Gerry Rhodes, Jong C. Son, Lianhong Xu
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Publication number: 20110077241Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.Type: ApplicationFiled: July 20, 2010Publication date: March 31, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste, Andrea Hager-Wernet
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Publication number: 20110077402Abstract: Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.Type: ApplicationFiled: December 10, 2010Publication date: March 31, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Ronald J. Christopher, Paul Covington, Atsushi Ogawa
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Patent number: 7915270Abstract: Certain oxazole ketone compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as MS).Type: GrantFiled: February 20, 2007Date of Patent: March 29, 2011Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20110070193Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: March 17, 2010Publication date: March 24, 2011Applicant: Abbott LaboratoriesInventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
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Publication number: 20110060141Abstract: The present invention relates to a method of making pyrimidines of formula (III), wherein X1, X2, R1 and R2 have the meanings as defined herein.Type: ApplicationFiled: March 19, 2009Publication date: March 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Guenter Linz, Adil Duran, Gerd Kraemer
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Patent number: 7902192Abstract: In general, the present invention relates to compounds capable of inhibiting p38, methods for inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity.Type: GrantFiled: May 14, 2004Date of Patent: March 8, 2011Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Syed Ali, Jifeng Liu, Yanbin Liu, Peter Lohse, Belew Mekonnen, Robert Selliah, Manish Tandon, Woj Wrona, Valery Antonenko
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Patent number: 7884100Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: June 12, 2007Date of Patent: February 8, 2011Assignee: PGxHealth, LLCInventors: Guoquan Wang, Robert D. Thompson, Jayson M. Rieger
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Publication number: 20110021491Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1, Y2, A, R1, R2, R3, R4, m, n, p, and q are as defined herein, including stereoisomers, esters, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof in a patient in need thereof.Type: ApplicationFiled: June 23, 2010Publication date: January 27, 2011Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.Inventors: Joe A. TRAN, Chen CHEN
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Patent number: 7875608Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: December 17, 2008Date of Patent: January 25, 2011Inventors: Robert D. Thompson, Guoquan Wang, Anthony Beauglehole, Frank Schmidtmann
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Publication number: 20100330069Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: ApplicationFiled: January 8, 2010Publication date: December 30, 2010Applicant: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Patent number: 7855194Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: March 15, 2007Date of Patent: December 21, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Andreas Christ, Hans-Peter Maerki, Rainer Eugen Martin
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Publication number: 20100311760Abstract: Compounds having the formula I wherein wherein R1, R2, R3, R4, X1, X2, X3 and X4 and as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: June 9, 2010Publication date: December 9, 2010Inventors: Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas, Joshua Paul Gergely Taygerly
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Publication number: 20100311736Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.Type: ApplicationFiled: October 22, 2008Publication date: December 9, 2010Inventors: Nicholas D. Adams, Michael Gerard Darcy, Neil W. Johnson, Jiri Kasparec, Steven David Knight, Kenneth Allen Newlander, Xin Peng, Lance H. Ridgers
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Patent number: 7838675Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: GrantFiled: August 23, 2005Date of Patent: November 23, 2010Assignee: AstraZeneca ABInventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Jeffrey Paul Stonehouse
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Patent number: RE42462Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: October 7, 1995Date of Patent: June 14, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: RE42477Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: March 27, 1997Date of Patent: June 21, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack