Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/367)
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Patent number: 8097758Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.Type: GrantFiled: March 9, 2009Date of Patent: January 17, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Markus Follmann, Jochen Goerlitzer, Herman Schreuder
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Publication number: 20120010176Abstract: Methods are provided for increasing utrophin promoter activity, utrophin expression or utrophin activity, and treating or reducing the symptoms of muscular dystrophy by administering to a subject in need thereof an effective amount of a composition comprising a utrophin promoter or activity upregulator. Muscular dystrophy includes but is not limited to Duchenne muscular dystrophy, Becker's muscular dystrophy, limb girdle muscular dystrophy, or a disease characterized by mutation or dysregulation of the dystrophin gene or an aberrant or dysfunctional dystrophin.Type: ApplicationFiled: November 12, 2009Publication date: January 12, 2012Inventors: Tejvir S. Khurana, Scott L. Diamond, Catherine Moorwood, Olga Lozynska, Andrew D. Napper, Emidio Pistilli, Neha Suri
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Publication number: 20120010184Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 21, 2011Publication date: January 12, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Alessandra BARTOLOZZI, Angela BERRY, Eugene Richard HICKEY, Markus OSTERMEIER, Doris RIETHER, Achim SAUER, David Smith THOMSON, Lifen WU, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Stephen Peter EAST, Monika ERMANN, Someina KHOR, Innocent MUSHI
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Publication number: 20120009141Abstract: A compound of Formula 1: or a salt thereof, and methods for the use thereof, especially as an IAP inhibitor, as well as related compounds, compositions, and methods.Type: ApplicationFiled: August 7, 2009Publication date: January 12, 2012Applicant: PHARMASCIENCE INC.Inventors: Alain Laurent, Melanie Proulx, James B. Jaquith, Irina Denissova
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Patent number: 8093396Abstract: Inhibitors of poly(ADP-ribose)polymerase having a structure of Formula (I), ways to make them and methods of treating patients using them are disclosed.Type: GrantFiled: January 19, 2010Date of Patent: January 10, 2012Assignee: Abbott LaboratoriesInventors: Magdalena K. Przytulinska, Thomas D. Penning, Yunsong Tong
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Patent number: 8093236Abstract: Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.Type: GrantFiled: March 11, 2008Date of Patent: January 10, 2012Assignee: Takeda Pharmaceuticals Company LimitedInventor: Atsushi Ogawa
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Publication number: 20120003282Abstract: Pharmaceutical compositions are provided comprising an active agent and a dextran polymer derivative. The compositions include from 0.01 to 99 wt % of an active agent and from 1 to 99.99 wt % of a dextran polymer derivative. The dextran polymer derivative is selected from dextran acetate, dextran propionate, dextran succinate, dextran acetate propionate, dextran acetate succinate, dextran propionate succinate, dextran acetate propionate succinate, and mixtures thereof.Type: ApplicationFiled: March 3, 2010Publication date: January 5, 2012Inventors: Warren K. Miller, David T. Vodak, Daniel E. Dobry, David K. Lyon, Dwayne T. Friesen, Michael M. Morgen, Corey J. Bloom, Daniel t. Smithey
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Publication number: 20120004165Abstract: Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments The invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R10, X, n, B1, B2, B3 and B4 are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: June 7, 2011Publication date: January 5, 2012Applicant: SANOFIInventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
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Patent number: 8088791Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)— or ?N—; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2—, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(?O)—, —O—(C?O)—, —C(?O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—; and Q is hydrogen, halogen, nitType: GrantFiled: March 22, 2007Date of Patent: January 3, 2012Assignee: Biots Scientific Management Pty LtdInventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
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Patent number: 8088805Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 16, 2007Date of Patent: January 3, 2012Assignee: MethylGene Inc.Inventors: Daniel Delorme, Silvana Marcela Leit de Moradei, Sylvie Frechette
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Publication number: 20110319404Abstract: The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating non-Hodgkin's lymphoma, in a subject in need thereof.Type: ApplicationFiled: September 7, 2011Publication date: December 29, 2011Inventor: Kevin Foley
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Publication number: 20110319416Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-E, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.Type: ApplicationFiled: January 28, 2010Publication date: December 29, 2011Applicant: EMORY UNIVERSITYInventors: Stephen F. Traynelis, Dennis C. Liotta, Cara Mosley, Timothy M. Acker, Sommer Zimmerman
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Publication number: 20110319387Abstract: The invention relates to a compound of the following formula (I), or to a pharmaceutically acceptable salt thereof or to a stereoisomer or mixture of stereoisomers at any proportions, where: X1 is a CH2 or C?O group; X2 is a linear saturated or unsaturated carbohydrate chain with 8 to 24 carbon atoms; R1 is a hydrogen atom or an OH or (C1-C6)alkoxy group such as methoxy; and R2 is a CH3 or CH2OR3 group, with R3 being a hydrogen atom or a (C1-C6)alkyl, CO—(C1-C6)alkyl or NH—(C1-C6)alkyl group. The invention also relates to the use of said compound as a drug, in particular for treating neurodegenerative diseases, and to a method for preparing same.Type: ApplicationFiled: March 2, 2010Publication date: December 29, 2011Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)Inventors: Fanny Schmidt, Bruno Figadere, Rita Raisman-Vozari, Pierre Champy
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Publication number: 20110319456Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.Type: ApplicationFiled: December 29, 2009Publication date: December 29, 2011Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Hoh-Gyu Hahn, Kee-Dal Nam, Dong-Yun Shin, Chan-Ho Park, Sung-Woo Cho, Eun-A Kim, Ghil-Soo Nam, Kyung-Il Chol, Seon-Hee Seo, Hee-Sup Shin, Dong-JIn Kim, Ae-Nim Pae, Hye-JIn Chung, Hyun-Ah Choo, Hye-Whon Rhim, Yong-Seo Cho, Eun-Jon Roh, Gyo-Chang Keum, Kee-Hyun Choi, Kye-Jung Shin, Chan-Seong Cheong, Jae-Kyun Lee, Yong-Koo Kang, Young-Soo Kim, Woong-Seo Park, Key-Sun Kim, He-Sson Chung, Chi-Man Song, Sun-Joon Min, Eunlce Eun-Kyeong Kim, Cheol-Ju Lee, Soon-Bang Kang
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Publication number: 20110312911Abstract: 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: ApplicationFiled: February 3, 2010Publication date: December 22, 2011Inventors: Roman Kats-Kagan, Christian P. Stevenson, Xibin Liao, Qinghong Fu, Emma R. Parmee, Songnian Lin
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Publication number: 20110312935Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.Type: ApplicationFiled: September 25, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
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Publication number: 20110312932Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: August 25, 2011Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Angela BERRY, Eugene Richard HICKEY, Markus OSTERMEIER, Doris RIETHER, Achim SAUER, David Smith THOMSON, Lifen WU, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Stephen Peter EAST, Monika ERMANN, Someina KHOR, Innocent MUSHI
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Publication number: 20110312996Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Publication number: 20110306615Abstract: According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, —ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C1-6 alkyl group; m is selected from integers from 0 to 3; R2 and R3 are independently selected from a C1-6 alkyl group; X1 and X2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E1; E1 is independently selected from a hydroxyl group, a halogen atom, a C1-4 alkyl group, a cyano group, a C1-4 alkoky group, a carbamoyl group, a C1-4 alkylcarbamoyl group, a di(C1-4 alkyl)carbamoyl group, an amino group, a C1-4 alkylamino group, a di(C1-4 alkylamino group, a sulfamoyl group, a C1-4 alkylsulfamoyl group and a di(C1-4 alkyl)suType: ApplicationFiled: September 9, 2005Publication date: December 15, 2011Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Hitoshi Yoshino, Takashi Emura, Akie Honma, Etsuro Onuma, Hiromitsu Kawata, Kenji Taniguchi
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Publication number: 20110306542Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Applicant: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
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Publication number: 20110306614Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Patent number: 8076489Abstract: Compounds of formula (I) in free or salt or solvate form, wherein T has the meaning as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: November 28, 2005Date of Patent: December 13, 2011Assignee: Novartis AGInventor: Robin A Fairhurst
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Publication number: 20110301128Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.Type: ApplicationFiled: August 22, 2011Publication date: December 8, 2011Applicant: EXELIXIS, INC.Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T. Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B. Mac, Larry W. Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C. Stevens, Tie-Lin Wang, Yong Wang, Jason H. Wu
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Publication number: 20110301210Abstract: The present invention is directed to compositions comprising pramipexole and the use of such compositions to treat neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS). As shown in FIG. 6B the mean +/?SEM serum 2,3-DHBA levels for the 12 ALS participants decreased significantly after pramipexole treatment.Type: ApplicationFiled: August 1, 2011Publication date: December 8, 2011Applicant: University of Virginia Patent FoundationInventor: James P. Bennett, JR.
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Publication number: 20110301183Abstract: A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.Type: ApplicationFiled: August 19, 2011Publication date: December 8, 2011Inventors: Kyriacos C. Nicolaou, Benjamin Pratt, Stellios Arseniyadis
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Publication number: 20110301150Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.Type: ApplicationFiled: February 25, 2010Publication date: December 8, 2011Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
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Publication number: 20110293718Abstract: Compositions of predetermined amounts of R(+) pramipexole and S(?) pramipexole and methods of using the same, including for the treatment and prevention of Parkinson's disease, are provided.Type: ApplicationFiled: August 5, 2011Publication date: December 1, 2011Applicant: KNOPP NEUROSCIENCES, INC.Inventors: Michael E. BOZIK, Thomas PETZINGER, JR., Valentin GRIBKOFF
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Publication number: 20110293750Abstract: The present invention is directed to a method of determining the prospects for survival of a melanoma patient. This method involves providing a biological sample from a patient diagnosed with melanoma, determining the level of an indicator of Wnt/?-catenin activation in the sample, comparing the level of the indicator of Wnt/?-catenin activation in the sample against a standard level of the indicator of Wnt/?-catenin activation correlated to survival of melanoma, and determining a patient's prospects for survival of melanoma based on the comparison. The present invention also relates to a method of improving survival of melanoma patients, decreasing metastases in melanoma patients, decreasing proliferation of cancer cells in melanoma patients, decreasing melanoma recurrence in melanoma patients, and/or decreasing tumor size in melanoma patients. This involves selecting melanoma patients and subsequently determining and monitoring therapy based on their level of Wnt/?-catenin activation.Type: ApplicationFiled: November 10, 2009Publication date: December 1, 2011Applicants: YALE UNIVERSITY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Andy J. Chien, David L. Rimm
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Publication number: 20110288161Abstract: Certain embodiments in the present invention provide for methods for therapy of lung diseases and other conditions such as infection are provided. In certain embodiments, the methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e., ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments can include the use of agents to modulate transport of thiol-containing compounds from the cell such as thiocyanate. In certain embodiments, therapeutic methods involve the administration of such agents to a patient afflicted with an inflammatory condition or infection responsive to stimulation of thiol-containing compound transport.Type: ApplicationFiled: March 15, 2011Publication date: November 24, 2011Inventor: Brian J. Day
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Publication number: 20110288083Abstract: The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK.Type: ApplicationFiled: May 19, 2011Publication date: November 24, 2011Applicant: NEW YORK UNIVERSITYInventors: Timothy CARDOZO, Hong WANG, David Ron
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Patent number: 8063067Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.Type: GrantFiled: July 23, 2009Date of Patent: November 22, 2011Assignee: Merck Patent GmbHInventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
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Publication number: 20110281879Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: January 12, 2011Publication date: November 17, 2011Applicant: ViroBay, Inc.Inventor: Craig Mossman
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Publication number: 20110281883Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, r, Y and G have the meanings given above as insecticides and/or acaricides and/or fungicides.Type: ApplicationFiled: January 14, 2010Publication date: November 17, 2011Applicant: Bayer Cropscience AGInventors: Reiner Fischer, Stefan Lehr, Arnd Voerste
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Patent number: 8058294Abstract: A pharmaceutically acceptable salt of N-[2-(Diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-naphthyl)ethoxy]propanamide provided it is not the dihydrobromide or dihydrochloride salt; and the use of such a compound as a medicament (for example in the treatment of respiratory diseases (such as asthma or COPD).Type: GrantFiled: February 7, 2008Date of Patent: November 15, 2011Assignee: AstraZeneca ABInventors: Robert Whittock, Jane Withnall
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Publication number: 20110268729Abstract: The invention relates to methods for the treatment or prophylaxis of amyotrophic lateral sclerosis, comprising administering to a patient in need thereof a therapeutically effective amount of a Nogo-A antagonist.Type: ApplicationFiled: July 10, 2009Publication date: November 3, 2011Inventors: Bams Abila, Sean Matthew Cleveland, Paul Andrew Hamblin, Rabinder Kumar Prinjha
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Patent number: 8048889Abstract: The present invention relates to 3,4-disubstituted coumarin and quinolone derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 3,4-disubstituted coumarin or quinolone derivative.Type: GrantFiled: March 29, 2005Date of Patent: November 1, 2011Assignee: XTL Biopharmaceuticals Ltd.Inventors: Bin Xu, Qiang Zhu, Hyun-Joon Cho, Reza Fathi, Zhen Yang, Anthony Sandrasagra, Yixin Liu
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Publication number: 20110262388Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: April 21, 2011Publication date: October 27, 2011Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme
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Publication number: 20110263590Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.Type: ApplicationFiled: June 7, 2011Publication date: October 27, 2011Applicant: Biota Europe LimitedInventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
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Publication number: 20110263556Abstract: 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 such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Patent number: 8044078Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.Type: GrantFiled: March 19, 2008Date of Patent: October 25, 2011Assignee: Sanofi-AventisInventors: Agnes Pappne Behr, Zoltan Kapui, Peter Aranyi, Sandor Batori, Veronika Bartane Bodor, Lajos T. Nagy, Mihalyne Santa, legal representative, Marton Varga, Endre Mikus, Katalin Urban-Szabo, Judit Vargane Szeredi, Tibor Szabo, Edit Susan, Marianna Kovacs
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Publication number: 20110253135Abstract: The present disclosure provides a drug delivery device comprising a housing defining an airway, wherein the airway comprises at least one air inlet and a mouthpiece having at least one air outlet, at least one heated metal substrate disposed within the airway, at least one drug disposed on the at least one heated metal substrate. Drugs that can be complexed with metals or metal salts and could be deposited as thin films on heated metal substrate for generating thermal condensation aerosols are particularly suited. The metal substrate could be electrically or chemically heated. Further, the chemically heated metal source could be activated by an igniter that generates heat or spark.Type: ApplicationFiled: April 1, 2011Publication date: October 20, 2011Applicant: ALEXZA PHARMACEUTICALS, INC.Inventors: Ron L. HALE, C.V Krishnamohan Sharma, Mingzu Lei
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Publication number: 20110257211Abstract: Small molecule choline kinase inhibitors having the following formula: are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting choline kinase enzymatic activity, and methods of treating tumors by administering an effective amount of a Formula I compound.Type: ApplicationFiled: December 22, 2010Publication date: October 20, 2011Applicants: ADVANCED CANCER THERAPEUTICS, LLC, UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: Pooran Chand, Jason A. Chesney, Brian F. Clem, Gilles H. Tapolsky, Sucheta Telang, John O. Trent
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Publication number: 20110257153Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: ApplicationFiled: April 21, 2011Publication date: October 20, 2011Inventors: Genesis M. Bacani, Scott D. Bembenek, Wendy Eccles, James P. Edwards, Matthew T. Epperson, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Kelly J. Mcclure, Taraneh Mirzadegan, Alexandro Santillan, JR.
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Patent number: 8039668Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.Type: GrantFiled: April 14, 2010Date of Patent: October 18, 2011Assignee: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Publication number: 20110251200Abstract: The invention provides to a family of aryl guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.Type: ApplicationFiled: September 11, 2009Publication date: October 13, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Gary D. Glick, Peter Toogood, Gina Ney
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Publication number: 20110251216Abstract: The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in cancer (e.g., prostate cancer, breast cancer, other solid tumors, multiple myeloma).Type: ApplicationFiled: February 10, 2011Publication date: October 13, 2011Applicant: The Regents of The University of MichiganInventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao
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Publication number: 20110251144Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject at least one compound selected from the group consisting of those set forth in Table 1, Table 2, Table 3, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: September 16, 2009Publication date: October 13, 2011Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20110245261Abstract: This present invention relates to an antiprolactinic veterinary composition to be administered to ruminants. Said composition comprises at least one antiprolactinic compound which is an agonist of dopamine receptors, and is particularly useful for promoting a substantial reduction of lactation, mammary involution, and for treating and/or intra-mammary diseases or infections of ruminants.Type: ApplicationFiled: April 7, 2011Publication date: October 6, 2011Applicant: CEVA SANTE ANIMALE SAInventors: Anouck LAGARDE, Stephane FLOCH, Thierry BERTAIM
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Patent number: RE42889Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: April 23, 2007Date of Patent: November 1, 2011Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw