Nitrogen, Other Than As Nitro Or Nitroso, Attached Indirectly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/176)
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Publication number: 20100152185Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: December 7, 2009Publication date: June 17, 2010Inventors: Lin Chu, Mark T. Goulet, Feroze Ujjainwalla, Linda Chang, Richard Frenette, Yves Girard, Michel Therien, Dwight MacDonald, John H. Hutchinson
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Publication number: 20100152453Abstract: This invention relates to novel compounds and a process for preparation of montelukast sodium.Type: ApplicationFiled: February 22, 2010Publication date: June 17, 2010Applicant: FORMOSA LABORATORIES, INC.Inventors: Jui-Te Hung, Ching-Peng Wei
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Publication number: 20100130545Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
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Publication number: 20100113516Abstract: Disclosed herein is a compound of the formula (I):(I). Therapeutic methods, compositions and medicaments related thereto are also disclosed.Type: ApplicationFiled: January 4, 2008Publication date: May 6, 2010Applicant: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Phong X. Nguyen, Ken Chow, Michael E. Garst
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Patent number: 7709641Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.Type: GrantFiled: June 30, 2005Date of Patent: May 4, 2010Assignee: OPKO Health, Inc.Inventors: Sapna S. Shah, Neng-Yang Shih, Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang
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Publication number: 20100104985Abstract: The present invention relates to a compound for photoresist, selected from the group consisting of a compound comprising an oxonol dye skeleton, a cyanine dye, a styryl dye, a compound comprising a merocyanine dye skeleton, a compound comprising a phthalocyanine dye skeleton, an azo compound, and a complex compound of an azo compound and a metal ion. The present invention further provides a photoresist liquid comprising at least one of the compound for photoresist and a method of etching a surface being processed using the photoresist liquid.Type: ApplicationFiled: March 5, 2008Publication date: April 29, 2010Inventor: Tetsuya Watanabe
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Patent number: 7704997Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: GrantFiled: September 7, 2005Date of Patent: April 27, 2010Assignee: Abbott LaboratoriesInventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biqin C. Li
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Publication number: 20100093743Abstract: This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C1 7alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the ?-position; and with the proviso that A is not benzimidazol-2-yl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.Type: ApplicationFiled: December 14, 2009Publication date: April 15, 2010Applicant: TOPOTARGET UK LIMITEDInventors: Paul W. FINN, Ivars Kalvinsh, Einars Loza, Victor Andrianov, Olga Habarova, Daina Lolya, Irina Piskunova
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Patent number: 7692017Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 17, 2004Date of Patent: April 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman
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Publication number: 20100076020Abstract: Disclosed herein is a compound of the formula (I): (I). Therapeutic methods, compositions and medicaments related thereto are also disclosed.Type: ApplicationFiled: January 4, 2008Publication date: March 25, 2010Applicant: Allergan, INC.Inventors: Todd M. Heidelbaugh, Phong X. Nguyen, Ken Chow, Michael E. Garst
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Publication number: 20100068752Abstract: The present invention provides dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes provided in this invention can comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been substituted with specific groups to provide beneficial properties.Type: ApplicationFiled: September 21, 2009Publication date: March 18, 2010Inventors: Praveen Pande, Hilary J. Cox, Yuejun Xiang, Wayne Forrest Patton
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Patent number: 7678812Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.Type: GrantFiled: October 23, 2007Date of Patent: March 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
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Publication number: 20100063089Abstract: The present invention relates to a succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline, and to a method for treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal the succinate salt. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and the succinate salt.Type: ApplicationFiled: December 3, 2007Publication date: March 11, 2010Inventors: Caroline Proulx-Lafrance, Patrick Robert Verhoest
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Publication number: 20100056783Abstract: Novel process for the preparation of statins and their pharmaceutically acceptable salts thereof represented by the general formula-(1) through novel intermediate compounds of general formula-(4).Type: ApplicationFiled: October 5, 2007Publication date: March 4, 2010Inventors: Manne Satyanarayana Reddy, Srinivasan Thirumalai Rajan, Maramreddy Sahadeva Reddy
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Publication number: 20100041568Abstract: A tri-podal compound according to formula (I) wherein, each Z is the same and is a substituted or unsubstituted N-heteroaromatic single-, multiple-, or fused-ring; and each A is the same, and can represent a direct bond between the cyclohexane ring and Z, or a carboxamide group (—C(O)—N(H)—). Use of the compounds in combinatorial libraries, methods of making the tripodal compounds, sensor devices for detecting carbohydrate targets, and methods of using the tripodal compounds to detect carbohydrate targets in a sample are also disclosed.Type: ApplicationFiled: October 16, 2007Publication date: February 18, 2010Applicant: UNIVERSITY OF ROCHESTERInventors: Benjamin L. Miller, Prakash B. Palde, Peter C. Gareiss
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Publication number: 20100041700Abstract: The present invention relates to 1-(Azolin-2-yl)-amino-1,2-heterocyclyl-ethane compounds, which are useful for combating insects, arachnids and nematodes. The present invention also relates to methods for combating animal pests and to compositions for combating animal pests. It has been found that animal pests can be combated by 1-(Azolin-2-yl)-amino-1,2-heterocyclyl-ethane compounds of the general formula (I): wherein A is a radical of the formulae A1 or A2: and wherein X is sulfur, oxygen or NR7, and HetA, HetB and R1 to R7 are defined as in the description.Type: ApplicationFiled: December 11, 2007Publication date: February 18, 2010Applicant: BASF SEInventors: Markus Kordes, Ronan Le Vezouet, Christopher Koradin, Ernst Baumann, Deborah L. Culbertson
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Patent number: 7662995Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.Type: GrantFiled: February 19, 2004Date of Patent: February 16, 2010Assignee: Chiesi Farmaceutici S.p.A.Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
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Publication number: 20100035872Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: August 4, 2009Publication date: February 11, 2010Applicant: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler
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Publication number: 20100035849Abstract: The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.Type: ApplicationFiled: August 5, 2009Publication date: February 11, 2010Applicants: OHIO STATE UNIVERSITY RESEARCH FOUNDATION, INVASC THERAPEUTICS, INC.Inventors: Sampath Parthasarathy, Sanjay Rajagopalan, Desikan Rajagopal
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Patent number: 7659286Abstract: N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide, pharmaceutically acceptable salts thereof, and/or mixtures thereof, as well as, pharmaceutical compositions thereof, methods of treatment therewith, and processes of making N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide and intermediates thereof.Type: GrantFiled: October 19, 2007Date of Patent: February 9, 2010Assignee: AstraZeneca ABInventors: Cathy Dantzman, Glen Ernst, Megan Murphy King
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Publication number: 20100029623Abstract: The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 represents H or F, or U and V represent N, W represents CH and R2 represents H, or U represents N. V represents CH, W represents CRa and R2 represents H; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH?CH—B or a binuclear heterocyclic system D, B representing a mono- or di-substituted phenyl group wherein the substituents are halogen atoms and D representing one of the following groups wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds. These compounds are useful as antibacterial agents.Type: ApplicationFiled: December 21, 2007Publication date: February 4, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Phillippe Surivet, Cornelia Zumbrunn
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Patent number: 7655801Abstract: The present invention relates to new substituted carbamic acid quinoline-6-yl esters of formulae 1 and 2 where R1=alkyl, aryl; R2=H, alkyl, aralkyl useful as acetylcholinesterase inhibitors, and which show potent antiacetylcholinesterase activity and have potential therapeutic use for prevention or cure of acetylcholinesterase related disorders including peripheral as well as central nervous system.Type: GrantFiled: December 28, 2004Date of Patent: February 2, 2010Assignee: Council of Scientific and Industrial ResearchInventors: Neeraj Shakya, Zeeshan Fatima, Chandishwar Nath, Anil Kumar Saxena
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Publication number: 20100022772Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.Type: ApplicationFiled: July 28, 2004Publication date: January 28, 2010Applicant: RIB-X PHARMACEUTICALS, INC.Inventors: Yusheng Wu, Chen Shili, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
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Publication number: 20100016354Abstract: The present invention relates to Compounds represented by the formula (I) or salts thereof. In the formula (I), the ring A represents a benzene ring, a thiophene ring, or a pyridine ring; Ra represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group; the ring B represents a pyridine ring, a pyrimidine ring, or a quinoline ring; the ring C represents a benzene ring; a pyridine ring, a quinoline ring, or an isoquinoline ring; X and Y, the same or different, represent an oxygen atom or a sulfur atom, with the proviso that the case X is a sulfur atom and Y is an oxygen atom be excluded; R1 represents a hydrogen atom, a halogen atom, an amino group, a cycloalkylamino group, an alkylcarbonylamino group, an alkyloxycarbonylamino group, an alkylaminocarbonyl group, or a non-aromatic heterocyclic group; and R2 and R2?, the same or different, represent a hydrogen atom, a halogen atom, an alkyl group, a halogeno-alkyl group, or a halogeno-alkoxy group.Type: ApplicationFiled: January 29, 2008Publication date: January 21, 2010Inventors: Takahiro Honda, Koushi Fujisawa, Hiroyuki Aono, Masakazu Ban
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Publication number: 20100016578Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: September 18, 2009Publication date: January 21, 2010Applicant: Idenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Dominique Surleraux, Michel Derock, Frederic Leroy
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Publication number: 20100001635Abstract: The present invention relates to novel organic electroluminescent compounds, and organic electroluminescent devices employing the same in an electroluminescent layer. Specifically, the organic electroluminescent compounds according to the invention are characterized in that they are represented by Chemical Formula (1) or Chemical Formula (2): provided that the total number of carbons in R1 or R2 is from 21 to 60. Since the organic electroluminescent compounds according to the invention have good luminous efficiency and excellent life property of material, organic electroluminescent devices having high color purity and luminance with very good operation life can be manufactured therefrom.Type: ApplicationFiled: July 7, 2009Publication date: January 7, 2010Applicant: Gracel Display Inc.Inventors: Mi Ae Lee, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
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Publication number: 20090326009Abstract: An object of the present invention is to study synthesis of a novel 1,2-dihydroquinoline derivative and to find a pharmacological action of the derivative. A compound represented by the general formula (1) or a salt thereof is effective in the treatment of a glucocorticoid receptor-related disease. In the formula, the ring X represents a benzene ring or a pyridine ring; R1 represents a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, an amino group or the like; p represents an integer of 0 to 5; R2 represents a halogen atom, an alkyl group, a hydroxy group or the like; q represents an integer of 0 to 2; R3 represents a hydrogen atom, an alkyl group, an alkenyl group or the like; R4 and R5 represent a hydrogen atom or the like; R6 represents a hydrogen atom or the like; A represents an alkylene group or the like; and R7 represents OR8, NR8R9, SR8, S(O)R8 or S(O)2R8, wherein R8 represents an aryl group, a heterocyclic group or the like and R9 represents a hydrogen atom or the like.Type: ApplicationFiled: September 14, 2006Publication date: December 31, 2009Applicant: Santen Pharmaceutical Co.,Inventors: Mamoru Matsuda, Toshiyuki Mori, Kenji Kawashima, Masato Nagatsuka, Sachiko Kobayashi, Minoru Yamamoto, Masatomo Kato, Miwa Takai, Tomoko Oda
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Publication number: 20090318440Abstract: Carbonylamino Pyrrolopyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: ApplicationFiled: December 12, 2006Publication date: December 24, 2009Inventors: Junhu Zhang, Anle Yang, Susan Elizabeth Kephart, Liming Dong, Chuangxing Guo, Yufeng Hong, Mary Catherine Johnson, Indrawan James Mc Alpine, Jayashree Tikhe, Haitao Li
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Publication number: 20090300856Abstract: One subject of the present invention is monocationic monochromophoric compounds of formula (I) and/or (II) below: in which: R1 represents a hydrogen or an alkyl, phenyl, benzyl, alkylcarbonyl, alkylsulphonyl, aminosulphonyl or aminocarbonyl radical; R5 represents an alkyl, phenyl or benzyl radical; R2 and R3, represent a halogen or an alkyl, aryloxy, arylamino, hydroxyl, alkoxy, (poly)hydroxyalkoxy, alkoxycarbonyl, alkylcarbonyloxy, amino, alkylcarbonylamino, aminocarbonyl, ureido, aminosulphonyl, alkylthio, alkylsulphonylamino, cyano, trifluoromethyl, thio, alkylsulphinyl or alkylsulphonyl radical; R4 represents a hydrogen or an alkyl, amino, alkylcarbonylamino, ureido, alkylsulphonylamino, hydroxycarbonyl, alkoxycarbonyl, cyano, phenyl or benzyl radical; R6 and R7, represent a hydrogen or an alkyl, alkylcarbonyl, alkoxycarbonyl, alkoxyaryl, aminoaryl, aminocarbonyl or alkylsulphonyl radical; and n is between 0 and 4, n? is between 0 and 4, the electroneutrality of the compounds of formulae (I) and (II)Type: ApplicationFiled: April 13, 2007Publication date: December 10, 2009Inventors: Herve David, Nadege Murguet, Andrew Greaves
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Patent number: 7629340Abstract: Disclosed are compounds having Formula (I) and the compositions and methods relating to these compounds, for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.Type: GrantFiled: December 12, 2006Date of Patent: December 8, 2009Assignee: SmithKline Beecham CorporationInventors: Franz Ulrich Schmitz, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Ronald Conrad Griffith, Martin Robert Leivers
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Publication number: 20090298827Abstract: The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represents a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; and P represents 0, 1, 2 or 3.Type: ApplicationFiled: November 14, 2007Publication date: December 3, 2009Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Publication number: 20090291956Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.Type: ApplicationFiled: May 20, 2009Publication date: November 26, 2009Inventors: Lingkai Weng, Lei Qiao, Jiacheng Zhou, Pingli Liu, Yongchun Pan
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Publication number: 20090275611Abstract: Compounds are provided which bind to and are agonist, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein R1, R2, R3, X and Ar have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: April 2, 2007Publication date: November 5, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
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Patent number: 7612069Abstract: There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.Type: GrantFiled: June 20, 2006Date of Patent: November 3, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Samuel Gerritz, Weixu Zhai, Shuhao Shi, Shirong Zhu, Andrew C. Good, Lorin A. Thompson, III
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Publication number: 20090258885Abstract: The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: ApplicationFiled: November 2, 2006Publication date: October 15, 2009Inventors: Helen M. Armstrong, Linda L. Chang, Lin Chu, Rosemary Sisco, Hyun O. Ok, Jinyou Xu, Feroze Ujjainwalla
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Publication number: 20090253740Abstract: This invention provides a compound of the formula (I): And their use for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.Type: ApplicationFiled: July 2, 2007Publication date: October 8, 2009Inventors: Tadashi Kawashima, Satoshi Nagayama, Kazunari Nakao, Hirotaka Tanaka
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Patent number: 7598360Abstract: A bisstyryl compound. The bisstyryl compound has formula (I): wherein Z1 and Z2 are benzene, naphthalene, or heterocyclic ring, R1 is H, C1-5 alkyl, hydroxyl, halogen atoms, or alkoxy, R2 is H, halogen atoms, C1-5 alkyl, nitro, ester, carboxyl, sulfo, sulfonamide, sulfuric ester, amide, C1-3 alkoxy, amino, alkylamino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, R3, R4, R5, and R6 are H, halogen atoms, alkyl, aralkyl, or heterocyclic ring containing O, S, or N, or R3 and R4 are joined to a nitrogen atom or R5 and R6 are joined together to form a ring, R7 and R8 are H or alkyl, W is nitrogen with or without Z1 and Z2 or aromatic group without Z1 and Z2, Y is carbon, oxygen, sulfur, selenium, —NR, or —C(CH3)2, m is 1-3, n is 1-18, and X1 and X2 are anionic groups or anionic organometallic complexes.Type: GrantFiled: October 21, 2005Date of Patent: October 6, 2009Assignee: Industrial Technology Research InstituteInventors: Shin-Shin Wang, Chien-Wen Chen, Jong-Lieh Yang, Chii-Chang Lai, Hui-Ping Tsai, Wen-Ping Chu, Wen-Yih Liao, Chien-Liang Huang, Tzuan-Ren Jeng, Ching-Yu Hsieh, An-Tse Lee
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Publication number: 20090247579Abstract: The present invention pertains to certain 2-[3H-thiazol-2-ylidinemethyl]pyridine compounds and analogs thereof, which, inter alia, inhibit cell proliferation, treat cancer, etc., and more specifically to compounds of the following formula, wherein RA1, RA2, RA3, RA4, RB1, RB2, RNA, RNB, and X? are as defined herein: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative conditions such as cancer, etc.Type: ApplicationFiled: February 21, 2007Publication date: October 1, 2009Inventors: Robert Brown, Jane Plumb, Gladys Wynne Aherne, Edward McDonald, Keith Jones, Stephen Hilton
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Patent number: 7585878Abstract: There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).Type: GrantFiled: June 10, 2004Date of Patent: September 8, 2009Assignee: Astellas Pharma Inc.Inventors: Takahiro Kuramochi, Norio Asai, Kazuhiro Ikegai, Seijiro Akamatsu, Hironori Harada, Noriko Ishikawa, Shohei Shirakami, Satoshi Miyamoto, Toshihiro Watanabe, Tetsuo Kiso
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Publication number: 20090221636Abstract: Formulations comprising argatroban and methods of making and using the formulations are provided. In an embodiment, the formulation comprises a solution having an argatroban concentration ranging from greater than about 10 to about 500 mg/mL. The solution can comprise an aqueous solution. The solution can be packaged in a sealed container that may either be aseptically-filled or subjected to sterilization to reduce the microbiological burden of the formulation. The solution can further be diluted and administered to persons needing same.Type: ApplicationFiled: February 29, 2008Publication date: September 3, 2009Applicants: BAXTER INTERNATIONAL INC., BAXTER HEALTHCARE S.A.Inventors: George Owoo, Richard A. Burgos
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Patent number: 7576100Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: GrantFiled: May 3, 2006Date of Patent: August 18, 2009Assignee: Acadia Pharmaceuticals, Inc.Inventors: Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
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Publication number: 20090182010Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a and bare as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: March 26, 2009Publication date: July 16, 2009Inventors: Mathai Mammen, Trevor Mischkl
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Publication number: 20090153039Abstract: The present invention relates to novel organic electroluminescent compounds, organic electroluminescent devices and organic solar cells comprising the same. Specifically, the organic electroluminescent compounds according to the invention are represented by Chemical Formula (1): wherein, R1 and R2 independently represent hydrogen, deuterium, linear or branched (C1-C20)alkyl, (C2-C20)alkenyl, (C2-C20)alkynyl, (C3-C15)cycloalkyl, tri(C1-C20)alkylsilyl, di(C1-C20)alkyl(C6-C20)arylsilyl, tri(C6-C20)arylsilyl, adamantyl, (C7-C15)bicycloalkyl or (C4-C20)heteroaryl, and the alkyl, alkenyl, alkynyl, cycloalkyl, trialkylsilyl, dialkylarylsilyl, triarylsilyl, adamantyl, bicycloalkyl or heteroaryl of R1 and R2 may be further substituted by one or more substituent(s) selected from deuterium, linear or branched (C1-C20)alkyl, (C1-C20)alkenyl, (C1-C20)alkynyl, halogen, phenyl, fluorenyl, naphthyl and anthryl.Type: ApplicationFiled: November 19, 2008Publication date: June 18, 2009Applicant: Gracel Display Inc.Inventors: Bo Ra Kim, Mi Ae Lee, Chi Sik Kim, Soo Yong Lee, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
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Patent number: 7541465Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: May 31, 2006Date of Patent: June 2, 2009Assignee: Purdue Neuroscience CompanyInventors: Nancy Lan, Yan Wang, Sui Xiong Cai
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Patent number: 7541467Abstract: A compound represented by the following general formula (I) or a salt thereof: wherein R1, R2, R3, and R4 independently represent 2-quinolyl group which may be substituted, 1-isoquinolyl group which may be substituted, or 3-isoquinolyl group which may be substituted; m, n, p, and q independently represent 1 or 2; and L represents a single bond, or an alkylene group having 1 to 5 carbon atoms wherein said alkylene group may contain one or more heteroatoms in the main chain, and may have one or more substituents on the main chain, which is useful as a fluorescent zinc ion sensor.Type: GrantFiled: July 30, 2004Date of Patent: June 2, 2009Assignees: Sekisui Medical Co., Ltd.Inventors: Shigenobu Yano, Yuji Mikata
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Publication number: 20090093479Abstract: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur.Type: ApplicationFiled: December 17, 2008Publication date: April 9, 2009Applicant: LOCUS PHARMACEUTICALS, INC.Inventors: Martha KELLY, Younghee LEE, Bin LIU, Ted FUJIMOTO, Joel FREUNDLICH, Bruce D. DORSEY, Gary A. FLYNN, Arifa HUSAIN
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Publication number: 20090082367Abstract: [Problem] To provide a compound which may be used in treating diseases in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, especially diabetes and insulin resistance. [Means for Solution] It was found that a triazole derivative or a pharmaceutically acceptable salt thereof, in which the 3-position of triazole ring is substituted with a trisubstituted methyl group and the 5-position is substituted with a lower alkyl, cycloalkyl or the like, has a strong 11?-HSD1-inhibitory activity. In addition, since the triazole derivative of the present invention shows excellent blood glucose-lowering action, it may be used in the treatment of diabetes and insulin resistance.Type: ApplicationFiled: March 14, 2007Publication date: March 26, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Seiji Yoshimura, Ryota Shiraki, Tomoaki Kawano, Daisuke Sasuga, Mitsuru Hosaka, Hiroki Fukudome, Kazuo Kurosawa, Hirofumi Ishii, Takanori Koike
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Publication number: 20090069316Abstract: The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).Type: ApplicationFiled: March 31, 2008Publication date: March 12, 2009Inventors: Yufeng Hong, Robert Steven Kania