The Additional Polycyclo Ring System Is A Bicyclo Ring System Having Nitrogen As The Only Ring Hetero Atom [e.g., 5-(indolyl-3-methylene)- Hydantoin, Etc.] Patents (Class 548/312.1)
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Publication number: 20130264554Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers of organic compound arranged between the pair of electrodes, wherein the organic compound layer, or one or more of the organic compound layers, comprises a compound represented by a substituted imidazole. The substituents on the imidazole ring may be selected from a range of suitable substituents, including: substituted or unsubstituted aryl groups, substituted or unsubstituted heterocyclic groups, substituted or unsubstituted alkyl groups or cyano groups. In various aspects of the invention, at least one of the substituent groups may be a substituted or unsubstituted imidazole or thiophene group.Type: ApplicationFiled: October 21, 2011Publication date: October 10, 2013Inventors: James Matthew MacDonald, Kazunori Ueno, Karl Peter Weber, Tadahiko Hirai, Juo-Hao Li
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Publication number: 20130263390Abstract: The invention relates to 4-aminoindole derivatives of formula (I), and the addition salts thereof, mesomers thereof, isomers thereof and solvates thereof: and to their use for the oxidation dyeing of keratin fibres, and in particular of human keratin fibres such as the hair. The present invention makes it possible to achieve dark shades, natural shades and dark natural shades. The present invention also makes it possible to obtain powerful, chromatic, aesthetic, sparingly selective coloration of keratin fibres in varied shades, which is resistant to the various attacking factors to which the hair may be subjected. In particular, when the 4-aminoindole derivatives are combined with one or more heterocyclic oxidation bases, they make it possible to obtain a wide range of colours and coloration of keratin fibres that shows good chromaticity and good selectivity.Type: ApplicationFiled: December 14, 2011Publication date: October 10, 2013Applicant: L'OREALInventors: Aziz Fadli, Fatima Makhlouf
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Patent number: 8541572Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.Type: GrantFiled: November 9, 2009Date of Patent: September 24, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K. C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20130225617Abstract: Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.Type: ApplicationFiled: January 31, 2013Publication date: August 29, 2013Applicant: PULMAGEN THERAPEUTICS (ASTHMA) LIMITEDInventor: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
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Publication number: 20130210880Abstract: The present invention relates to isoindoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such isoindoline derivatives, and the use of such isoindoline derivatives for therapeutic purposes.Type: ApplicationFiled: February 11, 2013Publication date: August 15, 2013Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130211079Abstract: MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula I are selective antagonists of MDM2 and MDM4 proteins, disrupting the p53/MDM2 and p53/MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Inventor: Alexander DOEMLING
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Patent number: 8507521Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.Type: GrantFiled: November 2, 2010Date of Patent: August 13, 2013Assignee: Merck Sharp + Dohme B.V.Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
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Patent number: 8501747Abstract: In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: February 11, 2008Date of Patent: August 6, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Manuel de lera Ruiz, Kevin D. McCormick, Christopher W. Boyce, Robert G. Aslanian, Younong Yu, Pietro Mangiaracina, Junying Zheng, Michael Y. Berlin, Stephanie Louise Ciesla, Chia-Yu Huang, Bo Liang
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Publication number: 20130196971Abstract: This invention relates to the use of imidazole, triazole, and tetrazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of imidazoles, triazoles, and tetrazoles in the treatment of cancer.Type: ApplicationFiled: September 15, 2011Publication date: August 1, 2013Inventors: Christopher Joseph Aquino, Dennis Heyer, Terence John Kiesow, David Lee Musso, Cynthia A. Parrish
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Patent number: 8492556Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: GrantFiled: November 9, 2012Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8487113Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.Type: GrantFiled: December 18, 2009Date of Patent: July 16, 2013Assignee: Farmak, A.S.Inventors: Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny
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Publication number: 20130177632Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.Type: ApplicationFiled: February 27, 2013Publication date: July 11, 2013Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
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Patent number: 8470831Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: GrantFiled: September 23, 2009Date of Patent: June 25, 2013Assignee: Cogenia SRLInventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Patent number: 8455529Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: September 9, 2011Date of Patent: June 4, 2013Assignee: Allergan, Inc.Inventors: Julie A. Wurster, Richard C. Yee
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Publication number: 20130137740Abstract: The present invention relates to specific analogs of combretastatin, in particular the compounds of formula (I) as described and defined herein, and pharmaceutical compositions comprising the compounds, as well as their medical use, in particular in the treatment or prevention of cancer, including multidrug-resistant cancer.Type: ApplicationFiled: May 5, 2011Publication date: May 30, 2013Inventors: Rainer Schobert, Bernhard Biersack, Thomas Müller
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Publication number: 20130131132Abstract: The present invention relates to N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives of the formula (I), (II), (III) or (IV) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives, and the use of such N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives for therapeutic purposes. The N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: November 19, 2012Publication date: May 23, 2013Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130123215Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: November 9, 2012Publication date: May 16, 2013Applicant: ALLERGAN, INC.Inventor: Allergan, Inc.
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Publication number: 20130121957Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: May 7, 2012Publication date: May 16, 2013Inventors: Qi Chen, Omar D. Lopez, John A. Bender, Gan Wang, Van N. Nguyen, John F. Kadow, Nicholas A. Meanwell, Makonen Belema
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Publication number: 20130102629Abstract: Compounds represented by formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: September 24, 2012Publication date: April 25, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130102592Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: December 5, 2012Publication date: April 25, 2013Applicant: SAREUM LIMITEDInventor: Sareum Limited
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Patent number: 8426442Abstract: A compound of formula (I): Or its salts or pharmaceutically acceptable derivatives thereof wherein: A represents a chemical moiety with the general formula (II): X and Y are independently selected from a group consisting of CH2, CH(R5) or C(R5)(R6); R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein, n=0, 1, 2 or 3; o=0, 1 or 2, with the proviso that when o=0, then n is 1, 2 or 3 and when o=1, then n is 1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. These compounds are useful in the treatment of various disorders including arrhythmia.Type: GrantFiled: June 4, 2010Date of Patent: April 23, 2013Assignee: Xention LtdInventors: Richard John Hamlyn, Mushtaq Mulla, David Madge, Basil Hartzoulakis, Simon Mark Jones, Derek Edward John, Oliver Gareth Dugdale
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Publication number: 20130081213Abstract: The present invention relates to a cationic 6-aminoindoline of general formula (I), the addition salts thereof with an acid and the solvates thereof: the present invention is also directed towards a method for synthesizing this cationic 6-aminoindoline, the compositions, the uses, the hair dyeing methods and the devices using this cationic 6-aminoindoline.Type: ApplicationFiled: March 2, 2011Publication date: April 4, 2013Inventor: Aziz Fadli
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Publication number: 20130065897Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.Type: ApplicationFiled: December 22, 2010Publication date: March 14, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
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Publication number: 20130040963Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 4, 2012Publication date: February 14, 2013Applicant: Ardea Biosciences, Inc.Inventors: Esmir GUNIC, Jean-Luc GIRARDET, David A. PAISNER
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Publication number: 20130025618Abstract: The present invention relates to a cationic 4-aminoindole of general formula (I), addition salts thereof with an acid and solvates thereof: in which: R1 is a linear or branched, saturated C2-C20 alkyl radical, substituted and/or interrupted with a cationic radical. The present invention is also directed towards a process for synthesizing this cationic 4-aminoindole, to the compositions, the uses, the hair dyeing processes and the devices using this cationic 4-aminoindole.Type: ApplicationFiled: December 6, 2010Publication date: January 31, 2013Inventor: Aziz Fadli
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Publication number: 20130028859Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: January 30, 2012Publication date: January 31, 2013Inventors: John A. Bender, Omar D. Lopez, Gan Wang, Makonen Belema, John F. Kadow
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Publication number: 20130012540Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: September 12, 2012Publication date: January 10, 2013Inventors: Rico Lavoie, John A. Bender, Jeffrey Lee Romine, Edward H. Ruediger, Carol Bachand, Omar D. Lopez, Qi Chen, Makonen Belema, John F. Kadow, Lawrence G. Hamann
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Publication number: 20130004457Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Inventors: Carol Bachand, Makonen Bekema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20120283298Abstract: Methods for administering a therapeutically effective amount of a somatostatin receptor-4 (SSTR4) agonist in order to treat learning and memory impairment for Alzheimer's disease is disclosed.Type: ApplicationFiled: October 14, 2010Publication date: November 8, 2012Inventors: Albert Michael Crider, Kenneth A. Witt, Karin E. Sandoval
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Publication number: 20120277217Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, 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: October 27, 2010Publication date: November 1, 2012Applicant: NewLink Genetics CorporationInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Xiaoxia Zhang
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Publication number: 20120277266Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: July 13, 2012Publication date: November 1, 2012Inventors: Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
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Publication number: 20120252699Abstract: The present invention relates to novel fluorophores and their use in combination with novel nucleic acid molecules, called aptamers, that bind specifically to the fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.Type: ApplicationFiled: February 18, 2010Publication date: October 4, 2012Applicant: CORNELL UNIVERSITYInventors: Samie R. Jaffrey, Jeremy S. Paige
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Publication number: 20120231972Abstract: The present invention relates to a probe compound that can comprise any substrate or metabolite of an enzymatic reaction in addition to an indicator component, such as, for example, a fluorescence dye, or the like. Moreover, the present invention relates to means for detecting enzymes in form of an array, which comprises any number of probe compounds of the invention which each comprise a different metabolite of interconnected metabolites representing the central pathways in all forms of life. Moreover, the present invention relates to a method for detecting enzymes involving the application of cell extracts or the like to the array of the invention which leads to reproducible enzymatic reactions with the substrates. These specific enzymatic reactions trigger the indicator (e.g. a fluorescence signal) and bind the enzymes to the respective cognate substrates. Moreover, the invention relates to means for isolating enzymes in form of nanoparticles coated with the probe compound of the invention.Type: ApplicationFiled: March 19, 2010Publication date: September 13, 2012Inventors: Peter N. Golyshin, Olga V. Golyshina, Kenneth N. Timmis, Tatyana Chernikova, Agnes Waliczek, Manuel Ferrer, Ana Beloqul, Maria E. Guazzaroni, Jose M. Vieltes, Florencio Pazos, Antonio Lopez De Lacey, Victor M. Fernandez
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Publication number: 20120220622Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.Type: ApplicationFiled: November 2, 2010Publication date: August 30, 2012Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
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Patent number: 8252923Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: GrantFiled: September 8, 2008Date of Patent: August 28, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
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Publication number: 20120195857Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 4, 2011Publication date: August 2, 2012Inventors: Makonen Belema, Pothukanuri Srinivasu, John A. Bender, Omar D. Lopez, Qi Chen, Richard A. Rampulla, Samayamunthula Venkata Satya Arun Kumar Gupta, Nicholas A. Meanwell
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Patent number: 8232312Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: GrantFiled: March 14, 2008Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
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Publication number: 20120190680Abstract: Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib: In certain embodiments, the heteroaryl amide analogues are agonists and/or ligands of dopamine receptors and may be useful, inter alia, for the treatment of a condition responsive to P2X7 receptor modulation, for example, pain, inflammation, a neurological or neurodegenerative disorder, a cardiovascular disorder, an ocular disorder or an immune system disorder.Type: ApplicationFiled: August 11, 2008Publication date: July 26, 2012Applicant: H. LUNDBECK A/SInventors: Rajagopal Bakthavatchalam, David C. Ihle, Scott M. Capitosti, David J. Wustrow, Jun Yuan
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Publication number: 20120184582Abstract: The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same.Type: ApplicationFiled: October 4, 2010Publication date: July 19, 2012Inventors: Jeong Uk Song, Geun Tae Kim, Sung Pil Choi, Cheol Kyu Jung, Deok Seong Park, Eun Sil Choi, Tae Hun Kim, Hyun Jung Park, Wan Su Park, Heui Sul Park, Ki Chul Koo, Vasily Artemov
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Publication number: 20120178764Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: January 5, 2012Publication date: July 12, 2012Inventors: Roger Bonnert, Rukhsana (née RASUL, Rukhsana) Mohammed, Mark Robert Dickinson
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Publication number: 20120149702Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard CollegeInventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
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Publication number: 20120135997Abstract: The present invention provides, for example, the following compounds as a pharmaceutical composition for treating diseases induced by production, secretion or deposition of amyloid ? proteins. The present invention provides a pharmaceutical composition for suppressing amyloid ? production comprising a compound of the formula: wherein A is a benzene ring, a pyridine ring or a pyrimidine ring, X is sultam, lactam, sulfonamide or the like, C is substituted or unsubstituted imidazolyl, substituted or unsubstituted oxazolyl or the like, R2, R3 and R4 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy or the like, its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 31, 2012Applicant: Shionogi & Co., Ltd.Inventors: Issei Kato, Kazuya Kano
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Publication number: 20120122854Abstract: The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Narendra Panday, Fabienne Ricklin, Martin Stahl, Petra Schmitz
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Patent number: 8178687Abstract: Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R?1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1, 2 and m=0, 1; R1 and/or R?1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products beingType: GrantFiled: December 16, 2010Date of Patent: May 15, 2012Assignee: Sanofi-AventisInventors: Marcel Alasia, Hervé Minoux, Jean-Marie Ruxer
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Patent number: 8178553Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: GrantFiled: January 20, 2010Date of Patent: May 15, 2012Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta Maria Kosinski, Seong-Heon Kim, De-Yi Yang, Razia K. Rizvi
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Publication number: 20120077811Abstract: The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.Type: ApplicationFiled: March 11, 2010Publication date: March 29, 2012Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Michael Patrick Hay, William Alexander Denny, William Robert Wilson, Guo-Liang Lu, Robert Forbes Anderson, Ho Huat Lee, Amir Ashoorzadeh
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Publication number: 20120071524Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.Type: ApplicationFiled: August 24, 2011Publication date: March 22, 2012Inventors: Yan Lu, Chien-Ming Li, Zhao Wang, Jianjun Chen, Wei Li, James T. DALTON, Duane D. Miller, Charles Duke, Sunjoo Ahn
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Publication number: 20120053165Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: March 2, 2010Publication date: March 1, 2012Applicant: Pfizer Inc.Inventors: Martin Patrick Allen, Christopher William Am Ende, Michael Aaron Brodney, Amy Beth Dounay, Douglas Scott Johnson, Martin Youngjin Pettersson, Jacob Bradley Schwartz, Tuan Phong Tran
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Publication number: 20120022057Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).Type: ApplicationFiled: March 16, 2010Publication date: January 26, 2012Applicant: Schering CorporationInventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, Jianhua Cao
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Patent number: 8101608Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-II, Rsk1, SGK, TrkA, TrkB and TrkC kinases.Type: GrantFiled: November 7, 2005Date of Patent: January 24, 2012Assignee: IRM LLC, a Delware Limited CorporationInventors: Yongqin Wan, Yuan Mi, Yi Fan, Dai Cheng, Yi Liu, Nathanael S. Gray, Pamela Albaugh