The Polycyclo Ring System Contains Nitrogen As The Only Ring Hetero Atom Patents (Class 548/364.7)
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Patent number: 8673911Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.Type: GrantFiled: November 3, 2008Date of Patent: March 18, 2014Assignee: MethylGene Inc.Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
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Publication number: 20140066457Abstract: 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 characterized 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: October 22, 2013Publication date: March 6, 2014Applicants: reMYND, Katholieke Universiteit Leuven, K.U.Leuven R&DInventors: Gerard Griffioen, Tom Van Dooren, Veronica Rojas De La Parra, Arnaud Marchand, Sara Allasia, Amuri Kilonda, Patrick Chaltin
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Patent number: 8663990Abstract: A subject of the present invention is to provide a measurement method using an internal standard substance in an electrophoresis where an analyte is a protein or a compound. The present invention relates to a measurement method for an analyte by an electrophoresis, characterized in that a peak of the analyte is identified by using as an internal standard substance (1) a combination of a compound I having 3 or more anion groups in a molecule and a compound II where 1 to 3 groups of the anion groups of said compound I have been substituted by cation groups, or (2) a combination of a compound III having 3 or more cation groups in a molecule and a compound IV where 1 to 3 groups of the cation groups of said compound III have been substituted by cation groups.Type: GrantFiled: April 27, 2010Date of Patent: March 4, 2014Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Naoyuki Yamamoto, Tatsuo Kurosawa
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Patent number: 8658635Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: February 25, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20140018377Abstract: This application claims priority to European Patent Application No. 09173304.8, filed Oct. 16, 2009, and the benefit of U.S. Provisional Application No. 61/253,091, filed Oct. 20, 2009, the disclosure of each of which is incorporated by reference herein in its entirety. The present invention relates to aminopropenoate derivatives, the process of their preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.Type: ApplicationFiled: June 12, 2013Publication date: January 16, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Christophe Dubost, Jacky Vadal, Philippe Rinolfi, Marie-Claire Grosjean-Cournoyer, Mazen Es-Sayed, Jürgen Benting, Ulrike Wachendorff-Neumann, Shinichi Narabu, Koichi Ishikawa, Hiroyuki Hadano, Pierre Genix, Jean-Pierre Vors, Angela Becker, Ulrich Görgens
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Publication number: 20140005165Abstract: Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.Type: ApplicationFiled: March 14, 2012Publication date: January 2, 2014Inventors: Anilkumar G. Nair, Jose S. Duca, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
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Patent number: 8614229Abstract: 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: GrantFiled: August 27, 2008Date of Patent: December 24, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: 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
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Publication number: 20130303524Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Inventors: Ross Bersot, Paul Humphries
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Publication number: 20130302378Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.Type: ApplicationFiled: July 8, 2013Publication date: November 14, 2013Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
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Publication number: 20130303492Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: November 14, 2013Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
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Patent number: 8563723Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.Type: GrantFiled: March 17, 2009Date of Patent: October 22, 2013Assignee: Abbott Healthcare Products, B.V.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A. M. Rensink, Jennifer Venhorst, Martina A. W. Van Der Neut, Martin De Haan, Cornelis G. Kruse
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Publication number: 20130274278Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: June 6, 2013Publication date: October 17, 2013Inventors: Stephen M. CONDON, Yijun DENG, Matthew D. ALEXANDER, Matthew G. LAPORTE
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Publication number: 20130274260Abstract: 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. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.Type: ApplicationFiled: December 13, 2011Publication date: October 17, 2013Inventors: Gerard Griffioen, Tom Van Dooren, Verónica Rojas De La Parra, Sara Allasia, Arnaud Marchand, Amuri Kilonda, Patrick Chaltin
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Publication number: 20130267493Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Applicant: PFIZER INC.Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
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Patent number: 8551625Abstract: A derivative with a heteroaromatic ring represented by General Formula (G1) is provided. R11 to R20 in the formula independently represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an aryl group having 6 to 10 carbon atoms in a ring. J represents a substituted or unsubstituted arylene group having 6 to 12 carbon atoms in a ring. Note that ? and ? may be bonded to each other to form a carbazole skeleton. Het is a substituent represented by General Formula (S1-1) or (S1-2). In General Formulae (S1-1) and (S1-2), Ar1 to Ar4 are independently a substituted or unsubstituted aryl group having 6 to 10 carbon atoms in a ring. R1 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an aryl group having 6 to 10 carbon atoms in a ring.Type: GrantFiled: March 30, 2010Date of Patent: October 8, 2013Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroko Nomura, Hiroshi Kadoma, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
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Patent number: 8546586Abstract: A cyanine dye derivative having high fluorescence intensity in a short wavelength region, and also a controllable migration velocity by further introducing a quaternary ammonium cation.Type: GrantFiled: April 27, 2010Date of Patent: October 1, 2013Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Naoyuki Yamamoto, Tatsuo Kurosawa, Satoshi Hasaba, Matsuhiro Date
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Publication number: 20130231378Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: February 22, 2013Publication date: September 5, 2013Applicant: GlaxoSmithKline LLCInventors: Mark A. SEEFELD, Meagan B. Rouse, Dirk A. Heerding, Dennis S. Yamashita, Kenneth C. McMulty
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Patent number: 8518945Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X? and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: March 4, 2011Date of Patent: August 27, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
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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: 20130184307Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.Type: ApplicationFiled: March 6, 2013Publication date: July 18, 2013Applicant: Arena Pharmaceuticals, Inc.Inventor: Arena Pharmaceuticals, Inc.
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Publication number: 20130172351Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: June 26, 2012Publication date: July 4, 2013Applicant: MERCK PATENT GMBHInventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
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Patent number: 8470866Abstract: The present invention relates to compounds of the formula I, as well as pharmaceutically-acceptable salts thereof, pharmaceutical compositions containing said compounds and methods of using said compounds in the treatment or prophylaxis of diseases and disorders. The compounds and compositions disclosed herein are glucokinase activators useful for the treatment or prophylaxis of metabolic diseases and disorders, for example diabetes mellitus, including type II diabetes mellitus.Type: GrantFiled: April 25, 2012Date of Patent: June 25, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Robert Francis Kester, Lucja Orzechowski
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Patent number: 8466149Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.Type: GrantFiled: August 12, 2008Date of Patent: June 18, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
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Publication number: 20130150326Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.Type: ApplicationFiled: August 19, 2011Publication date: June 13, 2013Applicant: Amira Pharmaceuticals, Inc.Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
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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: 20130131084Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.Type: ApplicationFiled: August 17, 2012Publication date: May 23, 2013Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Catherine GUILLOU, Frank Kozielski, Christophe Labriere, Francoise Gueritte, Sergey Tcherniuk, Dimitrios Skoufias, Claude Thal, Henri-Philippe Husson
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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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Patent number: 8445679Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.Type: GrantFiled: April 16, 2008Date of Patent: May 21, 2013Assignee: AbbVie Inc.Inventors: Xilu Wang, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron K. Kunzer
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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: 20130096144Abstract: The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Incyte CorporationInventor: Incyte Corporation
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Patent number: 8415353Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: GrantFiled: March 3, 2009Date of Patent: April 9, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
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Publication number: 20130065902Abstract: The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.Type: ApplicationFiled: March 21, 2011Publication date: March 14, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Heinz Fretz, Julien Hazemann, Sylvia Richard-Bildstein, Romain Siegrist
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Publication number: 20130060041Abstract: This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.Type: ApplicationFiled: January 27, 2011Publication date: March 7, 2013Inventors: Arnold van Loevezijn, Josephus H.M. Lange, Gerrit A. Barf, Arnold P. den Hartog
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Patent number: 8378118Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.Type: GrantFiled: January 10, 2012Date of Patent: February 19, 2013Assignee: Torrent Pharmaceuticals Ltd.Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
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Publication number: 20130040977Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: August 24, 2012Publication date: February 14, 2013Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Publication number: 20130023576Abstract: Pyrazole compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof, wherein Ra, Rb, Rc, Rd, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, n and R3 have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical formulations containing the compounds and to pharmaceutical formulations containing the compounds in combination with one or more active substances.Type: ApplicationFiled: January 19, 2012Publication date: January 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ralf Anderskewitz, Domnic Martyres, Thorsten Oost, Wolfgang Rist, Peter Seither
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Publication number: 20130012545Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: THE UNIVERSITY OF EDINBURGHInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20120319099Abstract: A material for organic electroluminescence devices comprising a compound in which a heterocyclic group having nitrogen is bonded to an arylcarbazolyl group or a carbazolylalkylene group and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer comprising at least one layer and disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the material for organic electroluminescence devices described above. The material can provide an organic electro-luminescence device emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.Type: ApplicationFiled: August 31, 2012Publication date: December 20, 2012Applicant: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro IWAKUMA, Hiroshi Yamamoto, Yoshio Hironaka, Hidetsugu Ikeda, Chishio Hosokawa, Seiji Tomita, Takashi Arakane
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Patent number: 8334061Abstract: An object is to provide a novel heterocyclic compound having a bipolar property. Another object is to provide a light-emitting element, a light-emitting device, and an electronic appliance each having high emission efficiency. A heterocyclic compound represented by a general formula (G1), a light-emitting element, a light-emitting device, and an electronic appliance each formed using the heterocyclic compound represented by the general formula (G1) are provided. By use of the heterocyclic compound represented by the general formula (G1) to a light-emitting element, a light-emitting device, and an electronic appliance, the light-emitting element, the light-emitting device, and the electronic appliance can each have high emission efficiency.Type: GrantFiled: March 29, 2010Date of Patent: December 18, 2012Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroko Nomura, Hiroshi Kadoma, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
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Publication number: 20120316171Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.Type: ApplicationFiled: November 4, 2010Publication date: December 13, 2012Inventor: Tamas Oravecz
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Patent number: 8329899Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: February 14, 2011Date of Patent: December 11, 2012Assignee: Synta Pharmaceuticals, Corp.Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
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Patent number: 8324384Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: February 3, 2010Date of Patent: December 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20120302609Abstract: The invention relates to pyrazoline substituted compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Applicant: Dynamix Pharmaceuticals LTD.Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Daniel Sherman, Vered Behar, Osnat Kashtan, Alexander Konson
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Publication number: 20120283271Abstract: The present invention relates to compounds of the formula I, as well as pharmaceutically-acceptable salts thereof, pharmaceutical compositions containing said compounds and methods of using said compounds in the treatment or prophylaxis of diseases and disorders. The compounds and compositions disclosed herein are glucokinase activators useful for the treatment or prophylaxis of metabolic diseases and disorders, for example diabetes mellitus, including type II diabetes mellitus.Type: ApplicationFiled: April 25, 2012Publication date: November 8, 2012Inventors: Steven Joseph Berthel, Robert Francis Kester, Lucja Orzechowski
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Publication number: 20120277205Abstract: The present invention relates to compounds corresponding to formula (I): in which: A represents a divalent aromatic radical; X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R3 represents a hydroxyl or a group —NR7R8; R4 represents a hydrogen atom, a halogen atom, a cyano, a phenyl, a group Alk, a group OAlk or a group —NR9R10; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.Type: ApplicationFiled: September 13, 2011Publication date: November 1, 2012Applicant: SANOFIInventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
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Patent number: 8273269Abstract: A composition, for producing dispersions, thermoplastic masses and/or color filters, comprising (a) a colorant of formula (1) wherein 20-100 mol % R1 are Br and 80-100 mol % R3 are H, especially of formula (Ib) and/or (Ic); (b) from 0 to 150% by weight, based on (a), of C. I. Pigment Red 144, 188, 190, 224, 242 or 2,4,6-trimethylphenylperylene diimide; (c) from 3 to 25% by weight, based on (a), of a di- or tri-azacyclopentylmethyl-substituted colorant (formulae given); (d) from 0 to 10% by weight, preferably from 0.01 to 8% by weight, based on the sum of (a) and (b), of an additionally sulfonated colorant of the same kernels as in (c); and (e) from 0 to 30% by weight, preferably from 3 to 25% by weight, especially from 5 to 20% by weight, based on (a), of a diketopyrrolopyrrole colorant substituted by at least one chain containing a plurality of nitrogen atoms (cf. formula (V)).Type: GrantFiled: May 5, 2009Date of Patent: September 25, 2012Assignee: BASF SEInventors: Roman Lenz, Gerardus De Keyzer, Mathias Duggeli, Patrick Christopher Holzhuter
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Publication number: 20120232070Abstract: Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.Type: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Applicant: Laboratoires Fournier SAInventors: Jerome Amaudrut, Benaissa Boubia, Maria Johanna Petronella Van Dongen, Fabrice Guillier, Olivia Poupardin-Olivier
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Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
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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