The Benzene Ring Is Part Of A Substituent Which Contains Oxygen Patents (Class 564/52)
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Patent number: 11084781Abstract: The present invention provides novel diarylurea derivatives (compounds of formula (I)) and their uses. The compounds of the present invention are demonstrated to be allosteric modulators of the CB1 receptor, and therefore useful for the treatment of diseases and conditions mediated by CB1.Type: GrantFiled: May 10, 2018Date of Patent: August 10, 2021Assignee: Research Triangle InstituteInventors: Yanan Zhang, Thuy Nguyen, Nadezhda German
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Patent number: 9029401Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: GrantFiled: February 14, 2012Date of Patent: May 12, 2015Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Publication number: 20150056213Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.Type: ApplicationFiled: March 7, 2013Publication date: February 26, 2015Inventors: Eduardo M. Sotomayor, Joel Bergman, Alan Kozikowski, Karrune Veeraprasert Woan, Alejandro V. Villagra
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Patent number: 8940681Abstract: The present invention improves dye transfer inhibition in the washing of textiles by the use of SO3M substituted urea derivatives of aromatic amines.Type: GrantFiled: August 21, 2014Date of Patent: January 27, 2015Assignee: Henkel AG & Co. KGaAInventors: Mareile Job, Birgit Gluesen, John Taylor, Anthony Lawrence
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Publication number: 20140288183Abstract: This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Inventors: Alan D. Snow, Qubai Hu, Thomas Lake, Judy Cam
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Patent number: 8759531Abstract: A fluoro-substituted deuterated diphenylurea compound, especially 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-2-(N-(methyl-d3))picolinamide, preparing method and use for treating or preventing tumor and relative diseases thereof.Type: GrantFiled: March 17, 2011Date of Patent: June 24, 2014Assignee: Suzhou Zelgen Biopharmaccceutical Co., Ltd.Inventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
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Patent number: 8697758Abstract: A urea compound of the present invention is represented by general formula (I) shown below: wherein each of X1, X2 and X3 independently represents a hydrogen atom, an alkyl group or an aryl group. The aryl group may have one or more functional groups selected from the group consisting of halogen groups, alkyl groups and alkoxy groups.Type: GrantFiled: September 15, 2009Date of Patent: April 15, 2014Assignees: National University Corporation Shizuoka University, Nissian Chemical Industries, Ltd.Inventor: Masamichi Yamanaka
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Publication number: 20140088156Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: ApplicationFiled: February 14, 2012Publication date: March 27, 2014Applicant: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Patent number: 8653304Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:Type: GrantFiled: September 30, 2010Date of Patent: February 18, 2014Assignee: Toray Industries, Inc.Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
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Publication number: 20140012038Abstract: The present invention relates to compounds 1, 1a (S-enantiomer) and 1b (R-enantiomer) of the following formula 1, and a method for preparing the same. [formula 1] The novel compound of the formula 1 is used as an important intermediate for preparing compounds 6, 6a (S-enantiomer) and 6b (R-enantiomer) of the following formula 6, which are 2,2?-binaphthol-3-aldehyde derivatives. Also, the present invention provides a method for preparing the compound of formula 1 with a very safe method at low cost.Type: ApplicationFiled: December 13, 2011Publication date: January 9, 2014Applicant: Aminologics Co., Ltd.Inventors: Rae Kyu Chang, Yun Soo Ahn, Heejung Jung, Hyerim Ga, Juwan Maeng, Young-Kook Koh, Young Hee Lee, Kwang Jae Lee, Joonseo Kim, Hyunil Lee
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SUBSTITUTED AROMATIC COMPOUND, HYDROGELATION AGENT, HYDROGEL, AND METHOD FOR GELATING AQUEOUS SAMPLE
Publication number: 20140005279Abstract: According to the present invention, a substituted aromatic compound represented by the following general formula (I) is provided. In general formula (I), A1, A2, and A3 each independently represent an aryl group substituted by a hydrophilic group.Type: ApplicationFiled: March 9, 2012Publication date: January 2, 2014Applicants: NISSAN CHEMICAL INDUSTRIES, LTD., NATIONAL UNIVERSITY CORPORATION SHIZUOKA UNIVERSITYInventors: Masamichi Yamanaka, Daisuke Higashi -
Publication number: 20130261178Abstract: A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C3 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; Z is linear C2-3 alkylene; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR92, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR92SO2NR92, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10 aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or further substituted by one or more F, Cl, Br, CN, NH2, NR32, NO2, CF3;Type: ApplicationFiled: July 5, 2010Publication date: October 3, 2013Inventors: Shailesh Mistry, Etienne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
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Publication number: 20130158067Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, Rz, A, m, n, p, q, s, and positions a and b are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: December 17, 2012Publication date: June 20, 2013Applicant: ABBVIE INC.Inventor: AbbVie Inc.
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Patent number: 8466200Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.Type: GrantFiled: February 7, 2012Date of Patent: June 18, 2013Assignee: Merck Patent GmbHInventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
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Patent number: 8455687Abstract: This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.Type: GrantFiled: January 20, 2011Date of Patent: June 4, 2013Assignee: ProteoTech, Inc.Inventors: Alan D Snow, Qubai Hu, Thomas Lake
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Publication number: 20130096138Abstract: Disclosed are novel thiourea or urea derivatives inhibitory of HIV activity. Also provided are a method for preparing the thiourea or urea derivatives, and a pharmaceutical composition for the prophylaxis or therapy of AIDS comprising the derivatives. Having high inhibitory activity against HIV, the thiourea or urea derivatives can be effectively used in the prophylaxis or therapy of AIDS.Type: ApplicationFiled: June 17, 2011Publication date: April 18, 2013Applicant: AVIXGEN INC.Inventors: Ji Chang You, Gyoon Hee Han, Chul Ho Lee, Doo Na Song, Koo Hwan Chung
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Publication number: 20130092047Abstract: To provide a water/oil repellent agent and a water/oil repellent composition which are capable of imparting sufficient water/oil repellency to the surface of an article and which have low environmental impact. One comprising a reaction product obtained by reacting a fluorinated alcohol or amine having a polyfluoroalkyl moiety having at most 6 carbon atoms with a polyisocyanate compound, which is, when applied to an article, capable of imparting sufficient water/oil repellency, while presenting little environmental impact. When applied to an article, the water/oil repellent composition of the present invention is capable of imparting a high quality water/oil repellency to the article.Type: ApplicationFiled: December 4, 2012Publication date: April 18, 2013Applicant: Asahi Glass Company, LimitedInventor: Asahi Glass Company, Limited
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Publication number: 20130060043Abstract: A fluoro-substituted deuterated diphenylurea compound, especially 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-2-(N-(methyl-d3))picolinamide, preparing method and use for treating or preventing tumor and relative diseases thereof.Type: ApplicationFiled: March 17, 2011Publication date: March 7, 2013Applicant: SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTDInventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
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Publication number: 20130018194Abstract: This invention relates to octahydro-binaphthol derivatives, which can recognize amino acids and amino alcohols enantioselectively and transform L-amino acids into D-amino acids and optically resolve amino acids or amino alcohol with high efficiency.Type: ApplicationFiled: April 1, 2011Publication date: January 17, 2013Applicants: AMINOLUX, INC, EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATIONInventor: Kwan-Mook Kim
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Publication number: 20130011417Abstract: The present invention relates to colchicine derivatives expressed in chemical formula 1, or to pharmaceutically acceptable salts thereof, to a method for preparing said derivatives, and to a pharmaceutical composition comprising said derivatives. The colchicine derivatives according to the present invention exhibit superior immunomodulatory effects as compared with conventional immunomodulators or colchicines, and therefore can be valuably used as an immunomodulator for modulating an acute or chronic immune response in organ transplantation.Type: ApplicationFiled: February 18, 2011Publication date: January 10, 2013Inventors: Duck Jong Han, Sung-eun Yoo, Jeehee Suh
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Publication number: 20120301177Abstract: An electrophotographic photosensitive member that includes the outermost surface layer formed by curing a mixture of a charge transporting substance having a chain-polymerizable functional group and a urea compound represented by the following formula (1) or (2), and a process cartridge and an electrophotographic apparatus each including the electrophotographic photosensitive member.Type: ApplicationFiled: May 22, 2012Publication date: November 29, 2012Applicant: CANON KABUSHIKI KAISHAInventors: Masato Tanaka, Masaki Nonaka
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Publication number: 20120270918Abstract: The invention relates to pyrazole derivatives of general formula (I): in which X represents chlorine or fluorine; to a process for preparing said derivatives, and to therapeutic uses of said derivatives.Type: ApplicationFiled: December 23, 2011Publication date: October 25, 2012Applicant: SanofiInventors: Pierre Yves ABECASSIS, Pascal DESMAZEAU, Michel TABART
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Patent number: 8293948Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.Type: GrantFiled: January 9, 2012Date of Patent: October 23, 2012Assignee: Jitsubo Co., Ltd.Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono
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Publication number: 20120245163Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, wherein X1, X2, X3, X4, J, K, L, X5, X6, Rb, G2, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: March 22, 2012Publication date: September 27, 2012Applicant: ABBOTT LABORATORIESInventors: Arthur Gomtsyan, Jerome F. Daanen, Gregory A. Gfesser, Michael E. Kort, Chih-Hung Lee, Heath A. McDonald, Pamela S. Puttfarcken, Eric A. Voight, Philip R. Kym
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Publication number: 20120214808Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Prosidion LimitedInventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Simon Andrew Swain, Philippe Wong-Kai-In
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Patent number: 8227643Abstract: This invention relates to bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable salts and their use in the modulation of Sirtuin 1 (Sirt1) and there use in neuroprotection for subject suffering from neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Amyotrophic lateral sclerosis, frontotemporal dementia, Parkinson's disease, including Parkinson's plus diseases such as multiple system atrophy, progressive supranuclear palsy, corticobasal degeneration and dementia with Lewy bodies, and in the manufacture of medicaments for such Sirt1 modulation and neuroprotection.Type: GrantFiled: January 12, 2010Date of Patent: July 24, 2012Assignee: ProteoTech, Inc.Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
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Publication number: 20120184735Abstract: A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: September 30, 2010Publication date: July 19, 2012Applicant: TORAY INDUSTRIES, INC.Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
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Publication number: 20120149934Abstract: Described herein is a linking agent that includes a polymeric or non-polymeric core molecule and one or more photoreactive groups covalently attached to the core molecule by one or more linking elements that include a urea linkage, a carbamate linkage, or a combination thereof.Type: ApplicationFiled: December 9, 2011Publication date: June 14, 2012Applicant: SURMODICS, INC.Inventor: Aleksey V. Kurdyumov
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Patent number: 8143364Abstract: Process for preparing a composition by reacting a polyisocyanate, a monoalkoxy polyoxyalkylene monoamine and water. The composition and its use in making cellular products are claimed as well.Type: GrantFiled: February 12, 2007Date of Patent: March 27, 2012Assignee: Huntsman International LLCInventors: Gerhard Jozef Bleys, Hans Godelieve Guido Verbeke
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Publication number: 20120022103Abstract: The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.Type: ApplicationFiled: September 29, 2011Publication date: January 26, 2012Applicant: ABBOTT LABORATORIESInventors: Erol K. Bayburt, Jerome F. Daanen, Arthur R. Gomtsyan, Steven P. Latshaw, Chih-hung Lee, Robert G. Schmidt, JR.
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Patent number: 8058474Abstract: A process for preparing a compound (C) represented by the following formula: wherein R1 represents hydrogen, C1-6 alkyl or C3-8 cycloalkyl, and R2 represents hydrogen or methoxy, characterized by reacting a compound (A-1) represented by the following formula: wherein R1 has the same definition as above, with a compound (B) represented by the following formula: wherein R2 has the same definition as above, and L represents a leaving group, is provided. Compound (C) is effective for prevention or treatment of various diseases associated with angiogenesis neoplasia.Type: GrantFiled: March 9, 2009Date of Patent: November 15, 2011Assignee: Eisai R&D Management Co., Ltd.Inventor: Toshihiko Naito
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Publication number: 20110178088Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: ApplicationFiled: March 21, 2011Publication date: July 21, 2011Applicant: XENTION LIMITEDInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Patent number: 7919530Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as Parkinson's disease, and the manufacture of medicaments for such treatment.Type: GrantFiled: July 10, 2009Date of Patent: April 5, 2011Assignee: Proteotech, Inc.Inventors: Luke A. Esposito, Joel Cummings, F. Michael Hudson, Alan D. Snow
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Publication number: 20110071178Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.Type: ApplicationFiled: April 16, 2010Publication date: March 24, 2011Applicant: Northeastern UniversityInventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
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Publication number: 20110065760Abstract: The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y.Type: ApplicationFiled: November 23, 2009Publication date: March 17, 2011Applicant: Jerini AGInventors: Jochen KNOLLE, Mike Schutkowski, Gerd Hummel, Thomas Tradler, Laurence Jobron, Claudia Christner, Dirk Scharn, Roland Stragies, Christoph Gibson, Frank Osterkamp
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Publication number: 20100311980Abstract: There is provided a process for preparing sorafenib or a salt thereof comprising the use of a compound of formula (A) wherein R? is selected from the group consisting of hydrogen, —C(O)OA, —C(O)CX3, —C(O)NH2, —C(O)—NHOH or There is also provided intermediate compounds of general formula (A), N-methyl-4-(4-ureidophenoxy)picolinamide, 4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenylcarbamate derivative and N-methyl-4-(4-(2,2,2-trihaloacetamido)phenoxy)picolinamide, processes for their preparation and their use in the preparation of sorafenib.Type: ApplicationFiled: September 10, 2008Publication date: December 9, 2010Applicant: CIPLA LIMITEDInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ghagare, Sandip Chikhalikar
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Publication number: 20100168108Abstract: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.Type: ApplicationFiled: January 18, 2010Publication date: July 1, 2010Applicant: Adolor CorporationInventors: Roland E. Dolle, Karin Worm, Q. Jean Zhou
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Patent number: 7714170Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, use in the reduction of A? peptide in vivo, use in modulating APP processing, and use in modulating the activity of APP secretase.Type: GrantFiled: December 8, 2008Date of Patent: May 11, 2010Assignee: Proteotech, Inc.Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
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Patent number: 7645903Abstract: The present invention relates to an IgG-binding compound, which more specifically has affinity for human IgGs of ?-type and functional derivatives thereof. More specifically, the compound according to the invention comprises an N,N-alkylated urea moiety located between an aromatic part and another part, which is a linear or cyclic substituted or unsubstituted aliphatic group. The compound binds to a pocket-shaped binding site present on all human IgG ?-Fabs, which site is located between the two domains (CH1 and CL) of its constant part. Accordingly, the compound according to the invention is a ligand for human IgGs of ?-type, and consequently, the invention also relates to a separation matrix for affinity chromatography, which matrix comprises said compound, as well as to other uses of the compound.Type: GrantFiled: September 12, 2003Date of Patent: January 12, 2010Assignee: GE Healthcare Bio-Sciences ABInventors: Andreas Axén, Herbert Baumann, Enrique Carredano, Anna Grönberg, Elles Steensma
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Patent number: 7612113Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence, inflammatory disorders such as asthma and COPD.Type: GrantFiled: April 28, 2003Date of Patent: November 3, 2009Assignee: Xention LimitedInventors: Takeshi Yura, Muneto Mogi, Klaus Urbahns, Hiroshi Fujishima, Tsutomu Masuda, Toshiya Moriwaki, Nagahiro Yoshida, Toshio Kokubo, Masahiro Shiroo, Masaomi Tajimi, Yasuhiro Tsukimi, Noriyuki Yamamoto
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Patent number: 7601876Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, AA/SAA amyloidosis, such as observed in systemic AA amyloidosis and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: GrantFiled: March 5, 2007Date of Patent: October 13, 2009Assignee: Proteotech, Inc.Inventors: Alan D. Snow, Beth P. Nguyen, Gerardo M. Castillo, Virginia J. Sanders, Thomas P. Lake, Lesley Larsen, Rex T. Weavers, Stephen D. Lorimer, David S. Larsen, David L. Coffen, Charlotte Coffen, legal representative
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Publication number: 20090239841Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.Type: ApplicationFiled: October 24, 2005Publication date: September 24, 2009Inventors: Alan J. Hutchison, Jun Yuan
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Publication number: 20090227631Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.Type: ApplicationFiled: November 22, 2006Publication date: September 10, 2009Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
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Publication number: 20090197965Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: ApplicationFiled: November 11, 2008Publication date: August 6, 2009Inventors: Alan D. Snow, Beth P. Nguyen, Gerardo M. Castillo, Virginia J. Sanders, Thomas P. Lake, Lesley Larsen, Rex T. Weavers, David S. Lorimer, David S. Larsen, David L. Coffen, Charlotte Coffen, Stephen D. Lorimer
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Publication number: 20090171112Abstract: A process for preparing a compound (C) represented by the following formula: wherein R1 represents hydrogen, C1-6 alkyl or C3-8 cycloalkyl, and R2 represents hydrogen or methoxy, characterized by reacting a compound (A-1) represented by the following formula: wherein R1 has the same definition as above, with a compound (B) represented by the following formula: wherein R2 has the same definition as above, and L represents a leaving group, is provided. Compound (C) is effective for prevention or treatment of various diseases associated with angiogenesis neoplasia.Type: ApplicationFiled: March 9, 2009Publication date: July 2, 2009Inventors: Toshihiko Naito, Kazuhiro Yoshizawa
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Patent number: 7544716Abstract: This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.Type: GrantFiled: November 28, 2003Date of Patent: June 9, 2009Assignee: Xention LimitedInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Patent number: 7501442Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: March 10, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, Craig Husfeld
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Publication number: 20090023931Abstract: Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided.Type: ApplicationFiled: February 8, 2008Publication date: January 22, 2009Applicant: Ewha University - Industry Collaboration FoundationInventors: Kim Kwan Mook, Tang Lijun
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Publication number: 20090012061Abstract: The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: ApplicationFiled: September 9, 2005Publication date: January 8, 2009Inventors: Timothy A. Blizzard, Carolyn A. Buser-Doepner, Douglas E. Frantz, Kelly Hamilton, Myle Hoang, Ling Lee, Christopher R. Moyes, Jerry A. Murry, Arash Soheili
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Publication number: 20080242539Abstract: The present invention provides a reversible thermosensitive recording medium including a support and a thermosensitive recording layer thereon, in which the thermosensitive recording layer contains an electron-donating coloring compound and an electron-accepting compound, and the thermosensitive recording layer is capable of forming a relatively developed condition and a relatively erased condition depending on at least one of the difference of heating temperatures and the difference of cooling rates following to heating, and in which the electron-accepting compound contains a phenol compound expressed by General Formula (1): where, in the General Formula (1), “l” represents an integer of 1 to 3 and “m” represents an integer of 23 or more.Type: ApplicationFiled: March 16, 2006Publication date: October 2, 2008Inventors: Satoshi Yamamoto, Kyoji Tsutsui, Hiromi Furuya, Kyohji Okada