Polycyclo Heterocyclic Ring System Containing Ring Nitrogen Patents (Class 548/181)
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Publication number: 20120252854Abstract: A crystalline form of a hydrate of a dihydrochloride 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by the following formula: wherein the crystalline form shows main peaks at interplanar spacings of 10.42, 5.85, 5.52, 3.84, 3.46 and 2.95 angstroms in X-ray powder diffraction obtained with Cu K? line radiation (wavelength ?=1.54 angstroms).Type: ApplicationFiled: May 7, 2012Publication date: October 4, 2012Applicant: DAIICHI-SANKYO COMPANY, LIMITEDInventors: Hisaki Kajino, Yutaka Ikeuchi, Hiroshi Miyamoto, Eiji Numagami, Satoru Nihei
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Publication number: 20120245185Abstract: In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: November 8, 2010Publication date: September 27, 2012Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Publication number: 20120238569Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.Type: ApplicationFiled: February 17, 2012Publication date: September 20, 2012Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
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Publication number: 20120238571Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: December 3, 2010Publication date: September 20, 2012Applicant: Glaxo Group LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Christian Alan Paul Smethurst
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Publication number: 20120238759Abstract: A method for manufacturing a 6-substituted 1-methyl-1H-benzimidazole derivative represented by the formula (IV) wherein R3 represents a hydrogen atom or a C1-C4 alkyl group. A 4-substituted N2-methylbenzene-1,2-diamine derivative is prepared from a particular 5-substituted N-methyl-2-nitroaniline derivative, subsequently reacting the resulting compound with {4-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]phenoxy}acetic acid or an acid chloride or a mixed acid anhydride thereof, and subsequently subjecting the resulting compound to intramolecular dehydration condensation. A compound of the formula (II) wherein R1 represents a hydrogen atom, a C1-C4 alkyl group, or a protective group for the nitrogen atom, and R2 represents a hydrogen atom or a protective group for the nitrogen atom is prepared and used as an intermediate.Type: ApplicationFiled: November 25, 2010Publication date: September 20, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Yutaka Ikeuchi, Chiharu Satoh, Eiji Numagami, Satoru Nihei, Hisaki Kajino
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Patent number: 8268803Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: December 17, 2007Date of Patent: September 18, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
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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: 20120225909Abstract: [Objective] To provide a drug that selectively stimulates the ?3-adrenergic receptors, particularly a drug capable of preferentially stimulating the ?3-adrenergic receptors over the ?1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like. [Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.Type: ApplicationFiled: September 30, 2010Publication date: September 6, 2012Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Yasuhiro Wada, Akifumi Morimoto
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Publication number: 20120225887Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: April 10, 2012Publication date: September 6, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
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Publication number: 20120214786Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Benjamin PELCMAN, Robert ROENN
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Publication number: 20120207683Abstract: Provided is an evaluation probe capable of optically evaluating permeability of a substance through a central nervous system tissue. Also provided is an evaluation method for permeability of a substance through a central nervous system tissue using an evaluation probe for central nervous system permeability. Also provided is a screening method using an evaluation probe for central nervous system permeability. The evaluation probe for central nervous system permeability includes, as an active ingredient, at least one kind of compound represented by the following general formula (1).Type: ApplicationFiled: February 16, 2012Publication date: August 16, 2012Applicant: CANON KABUSHIKI KAISHAInventors: Toshio Tanaka, Kohei Watanabe, Tsuyoshi Nomoto, Mie Okano, Taichi Shintou, Takeshi Miyazaki, Yuhei Nishimura, Yasuhito Shimada
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Patent number: 8242119Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoType: GrantFiled: September 24, 2009Date of Patent: August 14, 2012Assignee: Medivir ABInventors: Lourdes Salvador Odén, Magnus Nilsson, Pia Kahnberg, Bertil Samuelsson, Urszula Grabowska
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Publication number: 20120202856Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: ApplicationFiled: February 2, 2012Publication date: August 9, 2012Inventors: Mark R. PLAYER, Raul CALVO, Jinsheng CHEN, Carl ILLIG, Sanath MEEGALLA, Daniel PARKS, William PARSONS
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Patent number: 8236964Abstract: The invention relates to novel thiazolidine derivatives of the formula (I) wherein A and R1 are as described in the description and their use as medicaments, especially as orexin receptor antagonists.Type: GrantFiled: March 25, 2008Date of Patent: August 7, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Patent number: 8232293Abstract: This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:Type: GrantFiled: September 15, 2009Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Thilo Berkenbusch, Carl Alan Busacca, Burkhard Jaeger, Richard J. Varsolona
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Publication number: 20120184556Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.Type: ApplicationFiled: July 23, 2010Publication date: July 19, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Patent number: 8221737Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: July 17, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20120178941Abstract: A process for making aziridinyl epothilone compounds according to formula G, starting from a compound according formula C where R1, R2, R3, R4, R5, R6, R12, R13, Z1 and Z2 in formulae (G) and (C) are as defined herein. The aziridinyl epothilone compounds of formula (G) are useful for the treatment of cancer.Type: ApplicationFiled: February 21, 2012Publication date: July 12, 2012Inventors: Luca Parlanti, Jurong Yu
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Patent number: 8217044Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.Type: GrantFiled: March 28, 2011Date of Patent: July 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jing Zhang, Zhuming Zhang
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Publication number: 20120165335Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.Type: ApplicationFiled: June 23, 2011Publication date: June 28, 2012Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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Publication number: 20120142705Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 20, 2011Publication date: June 7, 2012Inventor: Robert Francis Kester
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Publication number: 20120142921Abstract: The invention relates to substituted hydrazide compounds as shown by general formula I, including geometrical isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and use of the same, wherein the substitutents Ar and R have the same meanings as given in the Description. The invention further relates to the use of compounds of general formula I in the preparation of medicament for the treatment and/or prevention of cancer and other proliferative diseases.Type: ApplicationFiled: August 9, 2010Publication date: June 7, 2012Applicant: SHENYANG J & HEALTH PHARMACEUTICAL CO., LTD.Inventor: Xiulan Shi
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Publication number: 20120129872Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Kristi Anne Leonard, Yan Zhang, Brett Andrew Tounge, Aihua Wang, Michael Hawkins, Paul Francis Jackson, Joseph Kent Barbay, Umar S.M. Maharoof
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Publication number: 20120130069Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.Type: ApplicationFiled: December 4, 2009Publication date: May 24, 2012Inventors: Tae Bo Sim, Jung Beom Son, Hwan Kim, Dong Sik Park, Hwan Geun Choi, Young Jin Ham, Jung Mi Hah, Kyung Ho Yoo, Chang Hyun Oh, So Ha Lee, Jae Du Ha, Sung Yun Cho, Byoung Mog Kwon, Dong Cho Han
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Publication number: 20120129842Abstract: This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Paul Francis JACKSON, Brett Andrew Tounge, Kristi Anne Leonard, Yan Zhang, Aihua Wang, Michael Hawkins, Umar S.M. Maharoof, Joseph Kent Barbay
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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: 8178693Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: GrantFiled: June 28, 2010Date of Patent: May 15, 2012Assignee: Array Biopharma Inc.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20120108565Abstract: The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.Type: ApplicationFiled: July 30, 2009Publication date: May 3, 2012Inventors: Lalima Sharma, Jitendra A. Sattigeri, Narest Kumar, Ajay Yadav, Rijwan Momim, Shahadat Ahmed, Ian A. Cliffe, Pradip Kumar Bhatnagar, Sanjay Ghosh, V. Samuel Raj, Dilip J. Upadhyay
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Publication number: 20120101081Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R1, and R2 are defined herein.Type: ApplicationFiled: October 20, 2011Publication date: April 26, 2012Inventors: Yue-Mei Zhang, Peter J. Connolly, Shu-Chen Lin, Mark J. MacIelag
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Publication number: 20120101101Abstract: Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: April 28, 2010Publication date: April 26, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Noriaki Uesaka, Takashi Sawada, Tomoyuki Kanda
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Publication number: 20120095040Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group while the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: April 19, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Luc Even, Aude Fayol, Julien Vache, Philippe Yauche
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Publication number: 20120095236Abstract: The present invention relates to compounds of the formula (I) wherein the substituents are as defined in claim 1, and their use as organic semiconductor in organic devices, like diodes, organic field effect transistors and/or solar cells. The compounds of the formula I have excellent solubility in organic solvents. High efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when said compounds are used in semiconductor devices or organic photovoltaic (PV) devices (solar cells).Type: ApplicationFiled: March 30, 2010Publication date: April 19, 2012Applicant: BASF SEInventors: Pascal Hayoz, Olivier Frederic Aebischer, Mathias Dueggeli, Mathieu G.R. Turbiez, Marta Fonrodona Turon, Natalia Chebotareva
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Publication number: 20120088759Abstract: The present invention relates to thiazolidin-4-one and [1,3]-thiazinan-4-one compounds of formula (I) wherein X, Y, R3 and R4 are as described in the description, or pharmaceutically acceptable salts thereof, for the prevention or treatment of diseases related to the orexin system. The present invention also relates to novel thiazolidin-4-one compounds of formula (II) and their use as pharmaceuticals, pharmaceutical compositions containing one or more compounds of formula (II), and especially their use as orexin receptor antagonists.Type: ApplicationFiled: May 11, 2010Publication date: April 12, 2012Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, John Gatfield, Romain Siegrist, Thierry Sifferlen, Jodi T. Williams
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Patent number: 8153638Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: GrantFiled: August 23, 2010Date of Patent: April 10, 2012Assignee: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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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: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Patent number: 8148413Abstract: This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I) wherein A and B are further defined in the application.Type: GrantFiled: September 30, 2010Date of Patent: April 3, 2012Assignee: TransTech Pharma, Inc.Inventors: Jesper Lau, Per Vedsø, János Tibor Kodra, Anthony Murray, Lone Jeppesen, Michael Ankersen, Govindan Subramanian, Adnan M. M. Mjalli, Robert Carl Andrews, Dharma Rao Polisetti, Daniel Peter Christen
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Patent number: 8143415Abstract: A process for making epi-epothilone compounds according to formula A.1, by reacting a compound according formula C with at least one halogenating agent followed by treatment with base, where R1, R2, R3, R4, R5, R6, R12, R13, Z1 and Z2 in formulae (A.1) and (C) are as defined herein. The epi-epothilone compounds of formula (A.1) can be converted into aziridinyl epothilone compounds, which are useful for the treatment of cancer.Type: GrantFiled: May 23, 2008Date of Patent: March 27, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Luca Parlanti, Jurong Yu
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Patent number: 8143421Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(?O)—, —C(?S)—, —S(?O)2—, C1-6alkanediyl-C(?O)—, C1-6alkanediyl-C(?S)— or C1-6alkanediyl-S(?O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-Type: GrantFiled: April 27, 2009Date of Patent: March 27, 2012Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck, Marieke Christiane Johanna Diepenbeek Voets, Sandrine Marie Helene Vendeville, Herman Augustinus De Kock, Bernhard Joanna Bernard Vergouwen
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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: 20120058986Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.Type: ApplicationFiled: September 2, 2011Publication date: March 8, 2012Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
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Publication number: 20120046303Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.Type: ApplicationFiled: October 27, 2011Publication date: February 23, 2012Applicant: ABBOTT LABORATORIESInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
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Publication number: 20120046250Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: March 2, 2010Publication date: February 23, 2012Applicant: STEMSYNERGY THERAPEUTICS, INCInventor: Darren Orton
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Patent number: 8119641Abstract: Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C?O, or —C(?O)NH—; —R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Aurora kinases activity or IGF-1R activity, like cancer.Type: GrantFiled: May 25, 2007Date of Patent: February 21, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Daniele Fancelli, Maurizio Pulici, Jürgen Moll, Tiziano Bandiera
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Patent number: 8119812Abstract: An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action. The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.Type: GrantFiled: April 19, 2010Date of Patent: February 21, 2012Assignees: SBI Biotech Co., Ltd., Crystalgenomics, Inc.Inventors: Takayuki Irie, Masaaki Sawa, Sayuri Ito, Chika Tanaka, Seong Gu Ro, Choul Hong Park
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Publication number: 20120040974Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.Type: ApplicationFiled: August 18, 2009Publication date: February 16, 2012Applicant: YALE UNIVERSITYInventors: William L. Jorgensen, Richard J. Bucala
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Publication number: 20120040958Abstract: The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
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Patent number: 8106079Abstract: A compound having the following formula (III) wherein R2 is hydrogen, alkyl, cycloalkyl, phenyl or a 5- or 6-membered heterocyclic, and X is oxygen, sulfur or nitrogen, and a method for preparing said compound.Type: GrantFiled: May 19, 2010Date of Patent: January 31, 2012Assignee: Sankyo Company, LimitedInventors: Hisaki Kajino, Hiroshi Miyamoto, Yutaka Ikeuchi
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Publication number: 20120014906Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: September 21, 2011Publication date: January 19, 2012Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AGInventors: Sultan Chowdhury, Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Qi Jia, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
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Publication number: 20120010186Abstract: Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: March 18, 2010Publication date: January 12, 2012Applicant: MERCK FROSST CANADA LTD.Inventors: Nicolas Lachance, Serge Leger, Renata M. Oballa, David Powell, Geoffrey K. Tranmer, Evelyn Martins, Yves Gareau