Substituent On Ring Carbon Of The Bicyclo Ring System Contains The Additional Hetero Ring Patents (Class 548/467)
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Publication number: 20130065882Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxyType: ApplicationFiled: October 3, 2012Publication date: March 14, 2013Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
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Publication number: 20130059853Abstract: Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions.Type: ApplicationFiled: April 28, 2011Publication date: March 7, 2013Applicant: LEO PHARMA A/SInventors: Simon Feldbaek Nielsen, Anne Marie Horneman, Jesper Lau, Jens Christian Hojland Larsen
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Publication number: 20130041008Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.Type: ApplicationFiled: October 5, 2012Publication date: February 14, 2013Applicant: ONYX THERAPEUTICS, INC.Inventor: Onyx therapeutics, Inc.
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Patent number: 8357683Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.Type: GrantFiled: December 16, 2011Date of Patent: January 22, 2013Assignee: Onyx Therapeutics, Inc.Inventors: Kevin D. Shenk, Francesco Parlati, Han-jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
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Publication number: 20130018073Abstract: The present invention provides an indole derivative having a melanin-concentrating hormone receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: January 5, 2011Publication date: January 17, 2013Inventors: Shinichi Masada, Yoshito Terao, Toshiki Murata
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Publication number: 20120329775Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: June 4, 2012Publication date: December 27, 2012Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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Patent number: 8329686Abstract: Novel isatin analogues, including isatin analogues comprising Michael Acceptors (IMAs) are disclosed. Further disclosed are methods of synthesis of the isatin analogues, and uses of the analogues, including inhibition of caspase-3 and caspase-7, and in vivo imaging of apoptosis by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).Type: GrantFiled: August 29, 2007Date of Patent: December 11, 2012Assignee: Washington UniversityInventors: Robert H. Mach, Michael Welch, Wenhua Chu, Justin Rothfuss
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Publication number: 20120309757Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120309769Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120295884Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: January 2, 2012Publication date: November 22, 2012Applicant: NOVARTIS AGInventors: Eva ALTMANN, Ulrich HOMMEL, Edwige Liliane Jeanne LORTHIOIS, Juergen Klaus MAIBAUM, Nils OSTERMANN, Jean Quancard, Stefan Andreas RANDL, Olivier ROGEL, Oliver SIMIC, Anna VULPETTI, Veronique Stark-Rogel
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Publication number: 20120270859Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 14, 2012Publication date: October 25, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias TREU, Ulrich GUERTLER, Thomas KARNER, Oliver KRAEMER, Jens Juergen QUANT, Stephan Karl ZAHN
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Patent number: 8288435Abstract: The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: GrantFiled: December 28, 2007Date of Patent: October 16, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Patent number: 8288429Abstract: The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: GrantFiled: July 25, 2008Date of Patent: October 16, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20120252853Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.Type: ApplicationFiled: March 30, 2012Publication date: October 4, 2012Applicant: H. Lundbeck A/SInventors: Anette Graven Sams, Jørgen Eskildsen, Jesper Frank Bastlund
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Publication number: 20120232063Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: September 13, 2012Inventors: Ralph Mazitschek, Jon C. Clardy, Dyann Wirth, Roger Wiegand, Sameer Urgaonkar, Mary Lynn Baniecki, Joseph Cortese, Cassandra Celatka, Yibin Xiang, Renato Skerlj, Elyse M.J. Bourque
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Patent number: 8242163Abstract: The present invention relates to a method for treating insulin resistance, neuronal loss associated with stroke, ischemia, central nervous system trauma, a central nervous system disorder, a neurodegenerative disease, the adverse consequences of the over-stimulation of excitatory amino acids, a psychiatric disease, epilepsy or other convulsive disorder, chronic pain, CMV retinitis, urinary incontinence, or for inducing anesthesia; which comprises administering to an animal or human in need thereof an effective amount of a pharmaceutical formulation comprising an effective amount of a pyrone-indole derivative of formula (I): Ar—B—Ar???(I) wherein Ar represents an indole nucleus ring system: Ar? represents an alpha-, beta- or gamma-pyrone nucleus ring system: and each of B, R1-4, and R1-2? are one of the groups as defined herein.Type: GrantFiled: November 4, 2009Date of Patent: August 14, 2012Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Moshe Laudon, Tal Peleg-Shulman
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Publication number: 20120202773Abstract: A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).Type: ApplicationFiled: April 23, 2012Publication date: August 9, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Toru Maruyama, Kaoru Kobayashi, Tohru Kambe, Takayuki Maruyama, Hideyuki Yoshida, Akio Nishiura, Nobutaka Abe
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Patent number: 8232297Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.Type: GrantFiled: September 8, 2006Date of Patent: July 31, 2012Assignee: 4SC AGInventors: Thomas Maier, Thomas Beckers, Rolf-Peter Hummel, Martin Feth, Matthias Müller, Thomas Bär, Jürgen Volz
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Patent number: 8227504Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.Type: GrantFiled: March 15, 2010Date of Patent: July 24, 2012Assignee: SanofiInventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
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Publication number: 20120165320Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.Type: ApplicationFiled: June 22, 2010Publication date: June 28, 2012Applicant: PANACEA BIOTEC LTD.Inventors: Rajseh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
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Publication number: 20120157437Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy group, or an optionally-substituted benzyloxy group; and R3a, R3b and R3c independently represent H, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group.Type: ApplicationFiled: February 1, 2012Publication date: June 21, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Nobuo MACHINAGA, Shin Ilmura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
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Patent number: 8188138Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.Type: GrantFiled: September 8, 2006Date of Patent: May 29, 2012Assignee: 4SC AGInventors: Thomas Maier, Thomas Beckers, Rolf-Peter Hummel, Martin Feth, Matthias Müller, Thomas Bär
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Publication number: 20120129829Abstract: The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: November 10, 2011Publication date: May 24, 2012Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Michael M. Garst, Wha Bin Im
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Publication number: 20120121540Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).Type: ApplicationFiled: August 8, 2008Publication date: May 17, 2012Inventors: Franz Ulrich Schmitz, Vincent W.F Tai, Roopa Ral, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Subramanian Baskaran, Irina Slobodov, Jack Maung, Martin Leon Neitzel
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Publication number: 20120114696Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).Type: ApplicationFiled: July 29, 2010Publication date: May 10, 2012Inventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K. Mishra, Jon Davis, Charles B. Millard, James J. Schmidt
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Patent number: 8173693Abstract: The present invention is related to derivatives of benzenesulfonamide represented by formula (I), and the pharmaceutical composition thereof. In addition, the benzenesulfonamide derivatives disclosed in the present invention can serve as potential cell cycle inhibitors, and thereby these benzenesulfonamide derivatives and the pharmaceutical composition thereof can be antitumor drug candidates, which might aim at cell cycle. Particularly, the benzenesulfonamide derivatives disclosed in the present invention may function as antitumor drugs to treat solid cancers.Type: GrantFiled: February 23, 2011Date of Patent: May 8, 2012Assignee: Purzer Pharmaceutical Co., Ltd.Inventors: Ji-Wang Chern, Grace Shiahuy Chen, Pei-Teh Chang, Kuan-Yu Chen, Meng-Ling Chen, Hsueh-Yun Lee, Chiung Hua Huang, Chun-Tang Chiou
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Publication number: 20120095000Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.Type: ApplicationFiled: December 12, 2011Publication date: April 19, 2012Applicants: SRI International, The Board of Trustees of the Leland Stanford Junior UniversityInventors: Anton Wyss-Coray, Mary J. Tanga
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Patent number: 8158671Abstract: The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: February 22, 2008Date of Patent: April 17, 2012Assignee: Merck Canada Inc.Inventors: Michael Boyd, John Colucci, Yongxin Han
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Publication number: 20120088762Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.Type: ApplicationFiled: December 16, 2011Publication date: April 12, 2012Applicant: ONYX THERAPEUTICS, INC.Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
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Publication number: 20120083475Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.Type: ApplicationFiled: June 11, 2010Publication date: April 5, 2012Inventors: Gerard Griffioen, Tom Van Dooren, Veronica Rojas De La Parra, Arnaud Marchand, Sara Allasia, Amuri Kilonda, Patrick Chaltin
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Publication number: 20120053181Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: April 28, 2010Publication date: March 1, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
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Publication number: 20120028963Abstract: The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives.Type: ApplicationFiled: March 18, 2010Publication date: February 2, 2012Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Sung Sook Lee, Kyung Joo Lee, Chang Sik Lee, Hyun Mo Yang, Do Hoon Kim, Dae Kyu Choi, Ho Jin Choi, Dal Hyun Kim, In Chang Hwang, Mi Jeong Kim, Byeong Hoon Han
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Publication number: 20120009142Abstract: In accordance with the present invention, compounds that inhibit viral replication, preferably Hepatitis C Virus (HCV) replication, have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the treatment or prevention of a viral infection are provided. In another aspect of the invention, compounds useful in the treatment or prevention of HCV infection are provided.Type: ApplicationFiled: June 13, 2011Publication date: January 12, 2012Applicant: PTC THERAPEUTICS, INC.Inventors: Gary Mitchell Karp, Peter Seongwoo Hwang, James Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell, Christine Espiritu, Concetta Freund, Zhengxian Gu, Takashi Komatsu
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Patent number: 8093284Abstract: A process for producing an aqueous solution of doripenem while decomposition of doripenem by heat is suppressed is found out. It was found out that decomposition of doripenem by heat can be suppressed by continuous heating an aqueous suspension of doripenem, and it was found out that an aqueous solution of doripenem can be produced.Type: GrantFiled: May 25, 2006Date of Patent: January 10, 2012Assignee: Shionogi & Co., Ltd.Inventor: Hayao Nakanishi
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Publication number: 20110311483Abstract: Compounds of Formulae I-1 to I-9 are disclosed, which are modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders.Type: ApplicationFiled: March 29, 2011Publication date: December 22, 2011Applicant: IRONWOOD PHARMACEUTICALS, INC.Inventors: James JIA, Regina GRAUL, Bo PENG, Colleen HUDSON, Joel MOORE, Ara MERMERIAN
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Publication number: 20110301133Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.Type: ApplicationFiled: December 8, 2009Publication date: December 8, 2011Applicant: VM Pharma LLCInventors: Jay Jie-Qiang Wu, Ling Wang
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Patent number: 8071388Abstract: The invention provides compositions and methods for the detection of biological targets, (e.g. nucleic acids and proteins) by nucleic acid-templated chemistry, for example, by generating fluorescent polymethine dyes.Type: GrantFiled: February 24, 2009Date of Patent: December 6, 2011Assignee: Ensemble Therapeutics CorporationInventors: Yumei Huang, James M. Coull
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Publication number: 20110294850Abstract: The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group.Type: ApplicationFiled: February 3, 2010Publication date: December 1, 2011Applicants: TOKYO INSTITUTE OF TECHNOLOGY, KYOTO UNIVERSITYInventors: Hachiro Sugimoto, Jun Takahashi, Takashi Takahashi, Ichiro Hijikuro
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Patent number: 8063099Abstract: The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: GrantFiled: July 25, 2008Date of Patent: November 22, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, David Lehman, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20110281870Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: May 24, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Xenia B. Searle, Ming C. Yeung, Stanley DiDomenico, Andrew O. Stewart, Daria Darczak, Michael Schrimpf, Michael J. Rozema
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Publication number: 20110281927Abstract: The present application describes deuterium-enriched doripenem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: November 11, 2010Publication date: November 17, 2011Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20110275673Abstract: The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders.Type: ApplicationFiled: September 17, 2009Publication date: November 10, 2011Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
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Patent number: 8044088Abstract: Compounds of general formula (I) wherein R1 is halo or cyano; R2 is C1-C4 alkyl; and R3 is phenyl substituted with one or more substituents chosen from C1-C6 alkyl, halo or —SO2(C1-C6 alkyl); or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof; are useful in the treatment of diseases and conditions mediated by the action of PGD2 at the CRTH2 receptor.Type: GrantFiled: March 10, 2006Date of Patent: October 25, 2011Assignee: Oxagen LimitedInventors: Richard Edward Armer, Edward Andrew Boyd, Judith Helen Boyd, legal representative, Philip Andrew Hay
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Publication number: 20110257222Abstract: The present invention relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of MMP inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP inhibitors for the treatment of pain and other diseases such as cancer. Additionally, the present invention relates to methods for treating pain in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.Type: ApplicationFiled: December 21, 2009Publication date: October 20, 2011Applicant: AQUILUS PHARMACEUTICALS, INC.Inventor: Irving Sucholeiki
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Publication number: 20110230350Abstract: Use of substituted sulfonamides of the formula (I) or salts thereof for enhancing stress tolerance in plants to abiotic stress, especially for enhancing plant growth and/or for increasing plant yield.Type: ApplicationFiled: March 17, 2011Publication date: September 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Jens Frackenpohl, Ines Heinemann, Thomas Müller, Pascal Von Koskull-Döring, Jan Dittgen, Dirk Schmutzler, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Martin Jeffrey Hills
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Publication number: 20110212860Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.Type: ApplicationFiled: February 22, 2011Publication date: September 1, 2011Inventors: Helen E. Blackwell, Grant D. Geske, Jennifer C. Campbell
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Patent number: 8008339Abstract: The invention relates to a compound of formula (I), or a pharmacologically or cosmetically acceptable salt or derivative thereof, wherein R1 to R5 are selected from the groups R1 representing -alkyl, -vinyl, —CHOH—CH2OH, R2 representing H, —OH, —Oalkyl, —Oacyl, saccharide groups, modified saccharide groups (e.g. malonylated), R3 representing —H, —OH, —Oalkyl, —Oacyl, modified —Oacyl (e.g. malonylated), saccharide groups, modified saccharide groups (e.g. malonylated), R4, R5 representing —COOH, -carbonic esters, for use as drug, antioxidant, food supplement. The invention also relates to a method for producing the compound of formula (I).Type: GrantFiled: March 11, 2008Date of Patent: August 30, 2011Assignee: Leopold-Franzens-Universitat InnsbruckInventors: Bernhard Kräutler, Thomas Müller
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Patent number: 8008491Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: GrantFiled: June 17, 2008Date of Patent: August 30, 2011Assignee: Aventis Pharmaceuticals, Inc.Inventors: John Ziqi Jiang, Jack Roger Koehl, Shujaath Mehdi, Neil Moorcroft, Kwon Yon Musick, Philip Marvin Weintraub, Paul Robert Eastwood
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Publication number: 20110207726Abstract: The present invention is directed to novel protease inhibitors that are specific for cathepsin L, cathepsin B, and cathepsin S. Accordingly, the present invention encompasses compositions and methods for treating and preventing diseases and disorders associated with cathepsin L, cathepsin B, or cathepsin S function or activity.Type: ApplicationFiled: April 17, 2009Publication date: August 25, 2011Inventors: Scott L. Diamond, Mary Pat Beavers, Donna Huryn, Michael C. Myers, Amos B. Smith, Parag P. Shah, Zhuqing Liu
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Patent number: 7989447Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, or chronic pain.Type: GrantFiled: April 13, 2007Date of Patent: August 2, 2011Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi