Quinoxalines (including Hydrogenated) Patents (Class 544/353)
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Publication number: 20110198574Abstract: The present invention provides a novel organic compound having excellent heat resistance. By using the novel organic compound, a light-emitting device and an electronic device having excellent heat resistance can be provided. A quinoxaline derivative represented by the general formula (1) is provided. Since the quinoxaline derivative represented by the general formula (1) has excellent heat resistance, when it is used for a light-emitting element, a light-emitting device using the light-emitting element also have excellent heat resistance. Further, electronic devices having excellent heat resistance can be provided.Type: ApplicationFiled: April 25, 2011Publication date: August 18, 2011Inventors: Masakazu Egawa, Nobuharu Ohsawa
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Publication number: 20110201607Abstract: The present invention is directed to fused heterocyclic compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: October 13, 2009Publication date: August 18, 2011Inventors: Scott D. Kuduk, Christina Ng Di Marco
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Publication number: 20110195963Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: ApplicationFiled: April 30, 2008Publication date: August 11, 2011Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
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Patent number: 7994170Abstract: The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.Type: GrantFiled: October 12, 2009Date of Patent: August 9, 2011Assignee: Novartis AGInventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
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Patent number: 7993761Abstract: The present invention provides a quinoxaline derivative represented by a general formula (G1). In the formula, ?1 and ?2 each independently represent an arylene group which has 13 or less carbon atoms forming a ring; Ar represents an aryl group which has 13 or less carbon atoms forming a ring; R1 and R6 each independently represent any of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an aryl group which has 13 or less carbon atoms forming a ring; and R2 to R5 and R7 to R10 each independently represent any of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, or a substituted or unsubstituted biphenyl group.Type: GrantFiled: December 2, 2008Date of Patent: August 9, 2011Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Harue Osaka, Nobuharu Ohsawa, Sachiko Kawakami
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Patent number: 7994169Abstract: The present invention relates to 3,4-diaminopyridine derivatives of formula (I) wherein R1 and R2 are, independently of each other, electron donors, wherein R2 is optionally H; and R3, R4, R5, and R6 are, independently of each other, H, optionally substituted straight-chain or branched alkyl, alkenyl, alkynyl, alkoxyl, or aryl, wherein R3 and/or R4 together with R5 and/or R6, optionally define a ring; processes for their preparation, and their use as catalysts.Type: GrantFiled: December 6, 2007Date of Patent: August 9, 2011Assignee: Bayer MaterialScience AGInventors: Hendrik Zipse, Ingmar Held
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Publication number: 20110183988Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line.Type: ApplicationFiled: December 21, 2010Publication date: July 28, 2011Inventors: Prabha N. Ibrahim, Guoxian Wu, Jack Lin, Wayne Spevak, Hanna Cho, Todd Ewing, Chao Zhang
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Publication number: 20110183976Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 25, 2009Publication date: July 28, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110178089Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ulmer
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Publication number: 20110178091Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.Type: ApplicationFiled: September 23, 2009Publication date: July 21, 2011Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
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Patent number: 7981925Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: August 26, 2009Date of Patent: July 19, 2011Assignee: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110160210Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.Type: ApplicationFiled: March 8, 2011Publication date: June 30, 2011Applicant: ALCON, INC.Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shapard, Mark R. Hellberg, Abbot F. Clark, Peter G. Klimko
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Publication number: 20110147720Abstract: The present invention relates to novel quinoxaline derivatives and their use in an organic light-emitting diode device. The quinoxaline derivative is of luminescence and rigidity, can increase glass transition temperature (Tg) and has better thermal stability, and thus can be used as a hole transporting layer, a host or guest of an emitting layer or an electron transporting layer of an organic light-emitting diode device.Type: ApplicationFiled: June 8, 2010Publication date: June 23, 2011Inventors: Min Sheng Chen, Yue Lin Du, Hsiao Chan Liu
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Publication number: 20110152271Abstract: The invention provides compositions and methods for treating nasal congestion through ophthalmic delivery. The provided compositions and methods utilize low concentrations of selective ?-2 adrenergic receptor agonists. The compositions preferably include brimonidine.Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Inventor: Gerald Horn
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Patent number: 7960384Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound of the formula: wherein the substituents are as defined herein.Type: GrantFiled: March 27, 2007Date of Patent: June 14, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Michael B. Wallace, Zhiyuan Zhang
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Publication number: 20110127513Abstract: The present invention provides a novel nitrogen-containing heterocyclic derivative and an organic electronic device using the same. The organic electronic device according to the present invention has excellent properties in terms of efficiency, driving voltage, and a life span.Type: ApplicationFiled: November 3, 2009Publication date: June 2, 2011Applicant: LG CHEM, LTD.Inventors: Dong-Hoon Lee, Tae-Yoon Park, Jae-Soon Bae, Hyun Nam, Jun-Gi Jang, Sung-Kil Hong
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Publication number: 20110121721Abstract: The present invention provides light-emitting element having long lifetime, and light-emitting devices and electronic devices having long lifetime. A light-emitting element comprises a first layer and a second layer including a light-emitting substance between a first electrode and a second electrode. The first layer includes a first organic compound and a second organic compound, the first layer is formed between the second layer and the second electrode, the first layer includes the first organic compound more than the second organic compound, the first organic compound is an organic compound having an electron-transporting property, the second organic compound is an organic compound having an electron-trapping property, an energy gap of the second organic compound is larger than that of the light-emitting substance; and a voltage is applied such that a potential of the first electrode is higher than that of the second electrode, so that the light-emitting layer emits light.Type: ApplicationFiled: January 21, 2011Publication date: May 26, 2011Inventors: Tsunenori Suzuki, Satoshi Seo, Sachiko Kawakami
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Patent number: 7947833Abstract: Certain methods that are useful in the preparation of amidophenyl-sulfonylamino-quinoxaline compounds are disclosed. The compounds are of the class of quinoxaline sulfonamides and constitute CCK2 receptor modulators, useful in the treatment of gastrointestinal diseases.Type: GrantFiled: October 30, 2007Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica NVInventors: Xiaohu Deng, Jimmy T. Liang, Neelakandha Mani, Chennagiri R. Pandit
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Publication number: 20110118270Abstract: The present invention relates to compounds of Formula (I) below, to their pharmaceutically acceptable salts and to their isomers or mixtures of isomers: HetAr—X—CHR1R2 (I) in which: -HetAr represents a group chosen from: —X represents a linear, saturated or unsaturated, hydrocarbon-based chain comprising from 8 to 22 carbon atoms, optionally interrupted by an —NH— or —NH—CO— group, —R1 represents a hydrogen atom or an —OH, —O(C1-C6)alkyl, —OCO((C1-C6)alkyl), —OSO2((C1-C6)alkyl) or —OSO3H group, and —R2 represents a hydrogen atom or a (C2-C6)alkynyl, (C2-C6)alkenyl or (C3-C6)cycloalkyl group. The present invention also relates to a process for preparing the compounds of Formula (I), and also to the use thereof, especially in the treatment of neurodegenerative diseases.Type: ApplicationFiled: July 20, 2009Publication date: May 19, 2011Inventor: Fanny Schmidt
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Publication number: 20110112077Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: January 15, 2009Publication date: May 12, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. KUDUK, Ronald K, CHANG
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Publication number: 20110112100Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HCV replication.Type: ApplicationFiled: August 25, 2010Publication date: May 12, 2011Inventors: Jared Bruce John Milbank, David Cameron Pryde, Thien Duc Tran
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Publication number: 20110112058Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: October 6, 2010Publication date: May 12, 2011Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: MEYYAPPAN MUTHUPPALANIAPPAN, Srikant Viswanadha, Kanthikiran V. Varanasi, Gayatri S. Merikapudi, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20110105329Abstract: Substituted quinolinones of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one compound of the formula I to act on plants, their seed and/or their habitat.Type: ApplicationFiled: October 29, 2010Publication date: May 5, 2011Applicant: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree van der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska, Anja Simon, Richard Roger Evans
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Publication number: 20110092504Abstract: The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein Q, X1, X2, R1 and Z are as defined herein.Type: ApplicationFiled: May 29, 2009Publication date: April 21, 2011Inventors: Yunxin Y. Bo, Shon Booker, Marian Bryan, Holly L. Deak, Longbin Liu, Kristin Andrews, Nobuko Nishimura, Mark H. Norman, Kathleen Panter, Laurie Schenkel, Aaron C. Siegmund, Nuria A. Tamayo, Kevin Yang
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Patent number: 7927720Abstract: An object is to provide a novel quinoxaline derivative. Another object is to provide a light-emitting element with low driving voltage. Another object is to provide a light-emitting element with low power consumption. Another object is to provide a light-emitting device and an electronic device with low power consumption by using such a light-emitting element. A quinoxaline derivative which has a structure in which at least one of carbon at a 2-position and carbon at a 3-position of quinoxaline, and carbon of 1,3,4-oxadiazole ring are bound via an arylene group is provided.Type: GrantFiled: November 25, 2008Date of Patent: April 19, 2011Assignee: Semiconductor Energy laboratory Co., Ltd.Inventors: Hiroko Nomura, Hiroshi Kadoma, Sachiko Kawakami, Satoko Shitagaki, Satoshi Seo
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Publication number: 20110081316Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David Messersmith, Alex Aronov, David J. Lauffer, Anne-Laure Grillot, Robert J. Davies
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Patent number: 7914706Abstract: The present invention relates to charge transport compositions. The invention further relates to electronic devices in which there is at least one active layer comprising such charge transport compositions.Type: GrantFiled: May 23, 2008Date of Patent: March 29, 2011Assignee: E. I. du Pont de Nemours and CompanyInventors: Daniel David LeCloux, Mark A. Guidry, Norman Herron, Nora Sabina Radu, Eric Maurice Smith, Ying Wang
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Publication number: 20110071149Abstract: The present invention relates to methods of modulating (for example, inhibiting) activity of JAK3, comprising contacting the JAK3 with a compound of Formula I: or pharmaceutically acceptable salt thereof, wherein constituent members are provided hereinwith. The present invention further provides novel compounds and compositions as well as their methods of preparation and use of the same as JAK3 inhibitors in the treatment of JAK3-associated diseases including, for example, inflammatory and autoimmune disorders.Type: ApplicationFiled: February 11, 2010Publication date: March 24, 2011Applicants: REACTION BIOLOGY CORP., SYNERGA LIMITEDInventors: Haiching MA, Sorin Vasile FILIP
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Publication number: 20110059964Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.Type: ApplicationFiled: February 3, 2010Publication date: March 10, 2011Applicant: sanofi-aventisInventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
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Patent number: 7901792Abstract: A quinoxaline derivative expressed by the general formula (1) is provided. (Each of R1 to R12 represents one of a hydrogen atom, a halogen atom, an alkyl group, an alkoxyl group, an acyl group, a dialkyl amino group, a diarylamino group, a substituted or unsubstituted vinyl group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocycle group. Ar1 represents one of a substituted or unsubstituted biphenyl group and a substituted or unsubstituted terphenyl group, and Ar2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, a substituted or unsubstituted terphenyl group, and a substituted or unsubstituted monocyclic heterocycle group.Type: GrantFiled: September 8, 2006Date of Patent: March 8, 2011Assignee: Semiconductor Energy laboratory Co., Ltd.Inventors: Masakazu Egawa, Sachiko Kawakami, Nobuharu Ohsawa, Hideko Inoue, Satoshi Seo, Ryoji Nomura
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Publication number: 20110049495Abstract: A quinoxaline derivative represented by Formula (I) or (II) is provided. In Formula (I) or (II), R1 and R2 are, independently, hydrogen, halogen, methyl, ethyl, propyl, butyl, aryl or heteroaryl, for example phenyl, furyl, thienyl, pyridyl, pyrimidyl, benzothiazolyl or benzoimidazolyl. The invention also provides an organic light-emitting diode including the quinoxaline derivative.Type: ApplicationFiled: August 27, 2010Publication date: March 3, 2011Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventors: Heh-Lung Huang, Teng-Chih Chao, Hao-Chun Lee
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Publication number: 20110046113Abstract: It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1): In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(?O) or NR11; and D is a group represented by the following general formula (4) or (6). In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). —(CR18R19)m3— Or —(CR20R21)m4-z-(CR22R23)m5??(7) z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26.Type: ApplicationFiled: October 12, 2010Publication date: February 24, 2011Applicant: KUREHA CORPORATIONInventors: Toru YAMAZAKI, Shigeyuki KIKUMOTO, Masahiro ONO, Atsushi SAITOU, Haruka TAKAHASHI, Sei KUMAKURA, Kunitaka HIROSE, Mikiro YANAKA, Yoshiyuki TAKEMURA, Shigeru SUZUKI, Ryo MATSUI
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Publication number: 20110046133Abstract: The present invention provides compounds of the following structure; A-L1-B-C-D that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: October 17, 2007Publication date: February 24, 2011Inventors: Moo Je Sung, Gary Mark Coppola, Taeyoung Yoon, Thomas A. Gilmore
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Publication number: 20110039864Abstract: Disclosed herein is an alpha-adrenergic compound having a structure. Therapeutic methods, compositions, and medicaments for treating pain are also disclosed herein.Type: ApplicationFiled: August 14, 2008Publication date: February 17, 2011Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
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Patent number: 7888359Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).Type: GrantFiled: March 22, 2007Date of Patent: February 15, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Rueedi Georg, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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Patent number: 7888358Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: July 1, 2008Date of Patent: February 15, 2011Assignee: Neurosearch A/SInventors: Dan Peters, Birgitte L. Eriksen, Elsebet Østergaard Nielsen, Jørgen Scheel-Krüger, Gunnar M. Olsen
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Publication number: 20110028482Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: ApplicationFiled: May 18, 2010Publication date: February 3, 2011Applicant: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 7875879Abstract: A substrate including a semiconductor layer, where characteristics of an element can be evaluated with high reliability, and an evaluating method thereof are provided. A substrate including a semiconductor layer of the invention has a closed-loop circuit in which an antenna coil and a semiconductor element are connected in series, and a surface of an area over which the circuit is formed is covered with an insulating film. By using such a circuit, a contactless inspection can be carried out. Further, a ring oscillator can be substituted for the closed-loop circuit.Type: GrantFiled: February 19, 2008Date of Patent: January 25, 2011Assignee: Semiconductor Energy laboratory Co., Ltd.Inventors: Tsunenori Suzuki, Satoshi Seo, Sachiko Kawakami
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Patent number: 7875618Abstract: The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.Type: GrantFiled: November 25, 2008Date of Patent: January 25, 2011Assignees: Wyeth, elbion GmbHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Norbert Höfgen, Hans Stange, Rudolf Schindler, Ute Egerland, Barbara Langen
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Publication number: 20110006295Abstract: A compound of the formula R1(CR3?CR4)nAr(CR4?CR3)nR2 wherein: n is 0 or 1; Ar represents aryl or heteroaryl having 1-5 aromatic rings which may be chain or fused or a combination of chain and fused, which may be substituted with alkoxy, fluoro, fluoroalkyl or cyano and which in the case of a 5-membered ring nitrogen heteroatom may be N-substituted with aryl or substituted aryl optionally further substituted with alkoxy, fluoro, fluoroalkyl or cyano; R1 and R2 independently represent aryl or nitrogen, oxygen or sulphur-containing heteroaryl having two to four fused aromatic rings one of which may be 5-membered and optionally substituted by aryl or heteroaryl having 1-5 chain or fused aromatic rings which may be further substituted with alkoxy, fluoro, fluoroalkyl or cyano; and R3 and R4 independently represent hydrogen, methyl, ethyl or benzyl.Type: ApplicationFiled: February 24, 2009Publication date: January 13, 2011Inventors: Poopathy Kathirgamanathan, Sivagnanasundram Surendrakumar
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Publication number: 20110009391Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: July 26, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Alain Jean BRAUN, Olivier CRESPIN, Claudie NAMANE, Eric NICOLAI, Francois PACQUET, Cecile PASCAL, Christophe PHILIPPO, Olivier VENIER
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Publication number: 20110003823Abstract: The invention provides compositions and methods for treating diseases and conditions, including systemic diseases and conditions, through an intravenous administration of a selective ?-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for ?-2 over ?-1 adrenergic receptors. The amounts of the selective ?-2 adrenergic receptor agonists are substantially lower than the amounts normally used to cause sedation. The compositions preferably include dexmedetomidine.Type: ApplicationFiled: May 26, 2010Publication date: January 6, 2011Inventor: Gerald Horn
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Publication number: 20100331326Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Inventors: Mark G. BOCK, Christoph GAUL, Venkateshwar Rao GUMMADI, Saumitra SENGUPTA
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Publication number: 20100331335Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 5, 2010Publication date: December 30, 2010Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
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Patent number: 7858799Abstract: An ionic organic compound having a repeating unit of formula (I) can be synthesized easily from a readily available organic compound through a small number of reaction steps, can be produced without any purification technique such as chromatography, and can be used in a quite small amount for gelation of water or an ionic liquid without any other auxiliary solvent: [-(A-B-C)n-]•m(X)??(I) wherein A represents a group having a quaternary ammonium cation which is formed from a heterocyclic compound having at least one nitrogen atom; B represents a functional group, which may have a substituent, selected from amide, urea, urethane and peptide groups; C represents a divalent hydrocarbon group, which may have a substituent, capable of linking between A and B; X represents an anion; n represents the number of repeating units; m represents the total number of anions; and n and m are the same integer.Type: GrantFiled: January 30, 2006Date of Patent: December 28, 2010Assignee: National Institute of Advanced Industrial Science and TechnologyInventors: Masaru Yoshida, Nagatoshi Koumura, Nobuyuki Tamaoki, Hajime Kawanami, Hajime Matsumoto, Said Kazaoui, Nobutsugu Minami
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Publication number: 20100324030Abstract: The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.Type: ApplicationFiled: April 11, 2008Publication date: December 23, 2010Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Glenn Dale, Sabine Pierau, Michael W. Cappi, Christopher Gray, Christian Hubschwerlen, Jean P. Surivet, Cornelia Zumbrunn
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Patent number: 7855292Abstract: Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.Type: GrantFiled: November 20, 2007Date of Patent: December 21, 2010Assignee: Janssen Pharmaceutica NVInventors: Brett Allison, Victor K. Phuong, Marna C. W. Pippel, Michael H. Rabinowitz, Hariharan Venkatesan
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Publication number: 20100316605Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: June 9, 2010Publication date: December 16, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Kevin Michael Cottrell, Alex Aronov, Robert J. Davies, Jon H. Come, David Messersmith
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Publication number: 20100317646Abstract: A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; —O—C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C4-7-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-hType: ApplicationFiled: March 19, 2010Publication date: December 16, 2010Applicant: Medical Research Council TechnologyInventors: Edward Giles Mciver, Ela Smiljanic, Denise Jamilla Harding, Joanne Hough
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Publication number: 20100317667Abstract: Provided herein are 1-aryl or 1-heteroarylsubstituted phenanthrene diketo acid compounds. These compounds comprise a ?-carboline ring structure substituted at C1 with an aryl or heteroaryl moiety and individually substituted at C3-C8 and N9 with a C1-C4 alkyl, a C1-C4 alkoxy, a C1-C4 alkoxyphenyl, halogen, thiol, alkylthiol, sulfonyl, sulfomainde, amide, substituted amide, ester, nitrile, OH, amino, substituted amine, haloalkyl, haloalkoxy, acyl, or a hydrogen. Also provided are methods for inhibiting proliferation of a cancer cell or for treating a cell proliferative disease by contacting the cancer cell or tumor comprising the same with the compounds provided herein or by administering the compounds to a subject with a cell proliferative disease.Type: ApplicationFiled: April 26, 2010Publication date: December 16, 2010Inventors: John K. Buolamwini, Shivaputra Patil, James K. Addo, D. Parker Suttle, Ruiwen Zhang, Zhengxiang Zhu, Sharma Horrick