Chalcogen Or Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/491)
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Publication number: 20110081294Abstract: A method of detecting a contrast agent for photoacoustic imaging provides a high signal intensity. In a contrast agent for photoacoustic imaging, each particle containing an inorganic material supports at least an organic dye having an absorption coefficient in the near infrared region by means of chemical bonding.Type: ApplicationFiled: September 29, 2010Publication date: April 7, 2011Applicant: CANON KABUSHIKI KAISHAInventors: Tatsuki Fukui, Fumio Yamauchi, Satoshi Yuasa, Sachiko Inoue
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Publication number: 20110053955Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: February 7, 2008Publication date: March 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
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Publication number: 20110009448Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.Type: ApplicationFiled: July 23, 2010Publication date: January 13, 2011Inventors: Nigel Vicker, Su Xiangdong, Dharshini Ganeshapillai, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
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Patent number: 7868037Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: GrantFiled: January 13, 2006Date of Patent: January 11, 2011Assignee: PTC Therapeutics, Inc.Inventors: Gary Mitchell Karp, Peter Seongwoo Hwang, James Jan Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony Allan Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell
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Publication number: 20100331302Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 8, 2010Publication date: December 30, 2010Applicant: Chemocentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20100324009Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 23, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Publication number: 20100324266Abstract: Novel compounds are provided, which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Y, wherein Y is a chemical structure as shown in FIG. 1. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.Type: ApplicationFiled: June 9, 2010Publication date: December 23, 2010Applicant: Affymetrix, INC.Inventors: Anthony D. Barone, Glenn H. McGall
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Publication number: 20100317644Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 16, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Publication number: 20100304074Abstract: A novel indolium compound of general formula (I) and an optical recording material containing the indolium compound. In general formula (I), ring A is a benzene ring, etc.; R1 is a group of general formula (II), etc.; R2 is a C1-C30 organic group, etc.; Y1 is a C1-C10 alkyl group, etc.; Z1 is, e.g., a C1-C8 alkyl group optionally substituted with a halogen group and optionally interrupted by —O—, etc.; Z2 is, e.g., a C1-C8 alkyl group optionally substituted with a halogen group and optionally interrupted by —O—, etc.; a is an integer of 0 to 6; b is an integer of 0 to 5; Anq- is a q-valent anion; q is 1 or 2; and p is a number necessary to neutralize an electric charge.Type: ApplicationFiled: September 26, 2008Publication date: December 2, 2010Applicant: ADEKA CORPORATIONInventors: Toru Yano, Yohei Aoyama
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Publication number: 20100298572Abstract: The present application relates to novel methods for the preparation of secondary carbinamine compounds, particularly the preparation of secondary carbinamine compounds of the formula Ia, formula Ib or formula IV from aldehydes of the formula II and boronic acids of the formula III or formula V, in the presence of ammonia or an ammonia equivalent of the formula NH4+X?.Type: ApplicationFiled: March 28, 2008Publication date: November 25, 2010Applicant: PANASONIC CORPORATIONInventors: Avinash N. Thadani, Bhartesh Dhudshia
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Patent number: 7834193Abstract: The present invention provides an industrial method production of silodosin, which is useful for a therapeutic agent for dysuria associated with benign prostatic hyperplasia. The production of silodosine is characterized by mixing 3-{7-cyano-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)-phenoxy]ethyl}amino]propyl]-2,3-dihydro-1H-indol-1-yl}-propyl benzoate and oxalic acid to yield the oxalate, subsequently hydrolyzing the oxalate salt to yield 1-(3-hydroxypropyl)-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino]propyl]-2,3-dihydro-1H-indole-7-carbonitrile and hydrolyzing the same, and manufacturing intermediates used therefore.Type: GrantFiled: April 16, 2007Date of Patent: November 16, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Toshiaki Yamaguchi, Ikuo Tsuchiya, Ken Kikuchi, Takashi Yanagi
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Publication number: 20100286204Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0Type: ApplicationFiled: November 19, 2008Publication date: November 11, 2010Applicant: Sterix LimitedInventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
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Publication number: 20100286189Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.Type: ApplicationFiled: December 16, 2008Publication date: November 11, 2010Applicant: Aziende Chim. Riun.Ang.Franc. A.C.R.A.F.S.P.A.Inventors: Maria Alessandra Alisi, Guido Furlotti, Nicola Cazzolla, Caterina Maugeri, Patrizia Dragone, Barbara Garofalo, Isabella Coletta, Giorgina Mangano, Beatrice Garrone
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Patent number: 7829613Abstract: The present invention relates to a splayant, that is, an intercalant/exfoliant, comprising an azinium compound capable of splaying a layered material.Type: GrantFiled: March 11, 2009Date of Patent: November 9, 2010Assignee: Eastman Kodak CompanyInventors: Debasis Majumdar, Deepak Shukla
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Publication number: 20100256106Abstract: Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.Type: ApplicationFiled: November 25, 2008Publication date: October 7, 2010Applicant: MERCK & CO., INC.Inventors: Alexander Pasternak, Michael J. Szymonifka
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Patent number: 7807705Abstract: Compounds and methods for treating cancer and inducing apoptosis in unwanted rapidly proliferating cells. The compounds are shown in formula I: wherein X is hydroxyl or amino; Y is carboxyl or sulfonyl; R1, R2, R3, and R4 can be the same or different and are selected from hydrogen, halogen, methoxy, trifluoromethyl, hydroxyl and combinations thereof, R5, R6, and R7 may be the same or different and are selected from hydrogen, chloro, bromo, nitro, phenyl, amino, methoxy, and combinations thereof, and derivatives or metabolites thereof.Type: GrantFiled: May 9, 2008Date of Patent: October 5, 2010Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Dasheng Wang, Jing-Ru Weng
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Publication number: 20100248261Abstract: The invention provides improved crosslinkers which permit more efficient determination of protein interactions in biological samples.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Inventors: Jeff RANISH, Jie Luo
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Patent number: 7803835Abstract: The present invention relates generally to substituted acetic acid derivatives and methods of using them.Type: GrantFiled: July 7, 2008Date of Patent: September 28, 2010Assignee: Wyeth LLCInventors: Ariamala Gopalsamy, Scott Lee Kincaid
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Patent number: 7799933Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: December 6, 2007Date of Patent: September 21, 2010Assignee: Hoffman-La Roche Inc.Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Publication number: 20100233166Abstract: Compounds, compositions and methods for the treatment of malignancy are disclosed.Type: ApplicationFiled: April 13, 2010Publication date: September 16, 2010Inventors: George C. Prendergast, Alexander J. Muller, James B. Duhadaway, William Malachowski
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Patent number: 7795450Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans,trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: GrantFiled: October 16, 2009Date of Patent: September 14, 2010Assignee: Magnesium Diagnostics, Inc.Inventor: Ibert Clifton Wells
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Publication number: 20100216803Abstract: Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.Type: ApplicationFiled: March 25, 2008Publication date: August 26, 2010Applicant: Astellas Pharma Inc.Inventors: Tatsuya Zenkoh, Eisuke Nozawa, Keisuke Matsuura, Ryushi Seo
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Patent number: 7781478Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: GrantFiled: January 16, 2007Date of Patent: August 24, 2010Assignee: PTC Therapeutics, Inc.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Jin Zhu, Xiaoyan Zhang
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Publication number: 20100210564Abstract: A pharmaceutical or a foodstuff including as an active ingredient a peptide containing Tyr (Y), Phe (F), Trp (W), or His (H) and a hydrophobic amino acid adjacent thereto, or an analog thereof.Type: ApplicationFiled: February 1, 2010Publication date: August 19, 2010Applicants: Kyoto University, Kyowa Hakko Bio Co., Ltd.Inventors: Kousaku OHINATA, Norimasa KANEGAWA
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Patent number: 7772271Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: GrantFiled: January 16, 2007Date of Patent: August 10, 2010Assignee: PTC Therapeutics, Inc.Inventors: Gary Mitchell Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Patent number: 7759380Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: May 8, 2007Date of Patent: July 20, 2010Assignee: Janssen Pharmaceutica, NVInventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker
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Publication number: 20100179325Abstract: The present invention provides compounds having excellent 11?-HSD1 inhibitory activity. A compound represented by the following formula (I): [wherein X1 represents an oxygen atom, or the formula —(CR11R12)p—, etc., Y1 represents a hydrogen atom, a hydroxyl group, etc., Z1 represents an oxygen atom or the formula —(NR14)—, R1 represents a hydrogen atom, a halogen atom, a cyano group, a C1-4 alkyl group, a C1-4 alkyl group substituted with 1 to 3 halogen atoms, a C1-4 alkoxy group, a C1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, and R2 represents a hydrogen atom or a C1-4 alkyl group, and n represents an integer of 1 or 2].Type: ApplicationFiled: June 28, 2008Publication date: July 15, 2010Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Ryo Suzuki, Ayako Mikami, Hiroaki Tanaka, Hiroshi Fukushima
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Patent number: 7754896Abstract: The present invention relates to agonists of the S1P4 receptor, which are selective for the S1P4 receptor over one or more of the S1P1, S1P2, S1P3 or S1P5 receptors of at least 10 fold, in particular new indol-alanine derivatives of structure I, process for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them wherein R1 is phenyl or naphthyl, wherein phenyl is substituted by one or two of halogen, C1-6alkyl, C1-6alkoxy or phenylC1-6alkyl; and R2 is hydrogen or C1-6alkyl; in free or salt form.Type: GrantFiled: January 20, 2005Date of Patent: July 13, 2010Assignee: Novartis AGInventors: Kamal Azzaoui, Rochdi Bouhelal, Peter Buehlmayer, Danilo Guerini, Manuel Koller
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Publication number: 20100174075Abstract: The present invention relates to the use of nitric oxide-releasing statins of formula (I) for the treatment of pulmonary arterial hypertension.Type: ApplicationFiled: May 12, 2008Publication date: July 8, 2010Applicant: NICOX S.A.Inventors: John Wharton, Angela Monopoli
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Patent number: 7745451Abstract: Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: GrantFiled: May 4, 2006Date of Patent: June 29, 2010Assignee: Renovis, Inc.Inventors: Michael G. Kelly, John Kincaid, Carl J. Kaub
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Publication number: 20100158996Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.Type: ApplicationFiled: February 12, 2010Publication date: June 24, 2010Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
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Publication number: 20100160632Abstract: The present invention relates to zinc amide bases of the general formula (I) (R1R2N)2—Zn.aMgX12.bLiX2??(I) wherein R1 and R2 are each independently selected from substituted or unsubstituted, linear or branched alkyl, alkenyl, alkynyl or silyl derivatives thereof, and substituted or unsubstituted aryl or heteroaryl, and wherein R1 and R2 can form together a ring structure, or R1 and/or R2 can be part of a polymer structure; X12 is a divalent anion or two monovalent anions that are independent from each other; X2 is a monovalent anion; a is >0; and b is >0. The zinc amide bases can be used, amongst other things, for deprotonation and metallization of aromatics.Type: ApplicationFiled: May 14, 2008Publication date: June 24, 2010Inventors: Paul Knochel, Stefan Wunderlich
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Patent number: 7737169Abstract: Anionically substituted 7-nitroindoline derivatives are disclosed and their uses as caged compounds from which effector species such as neurotransmitters and amino acids are releasable on irradiation with light.Type: GrantFiled: August 22, 2006Date of Patent: June 15, 2010Assignee: Medical Research CouncilInventors: John Corrie, David Ogden, George Papageorgiou
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Publication number: 20100137599Abstract: The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds.Type: ApplicationFiled: June 18, 2008Publication date: June 3, 2010Applicant: NICOX S.A.Inventors: Achim Hack, Gunter Weingarner, Matthias Kramer
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Publication number: 20100130557Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: ApplicationFiled: March 14, 2008Publication date: May 27, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
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Publication number: 20100130570Abstract: The present invention relates N-5-membered, fused, heteroaryl-methylene-N-cycloalkyl-carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3; W1 to W5; Y1 to Y3 and p represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: May 27, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Arounarith Tuch, Jean-Pierre Vors
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Patent number: 7723373Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: GrantFiled: July 15, 2003Date of Patent: May 25, 2010Assignee: AstraZeneca ABInventors: Roger Bonnert, Mark Dickinson, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
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Publication number: 20100120886Abstract: The present invention relates to aryl-substituted sulfonamides with 5-HT6 receptor affinity, and compositions thereof, and the use of said compounds for the treatment or prophylaxis of various disorders.Type: ApplicationFiled: January 30, 2008Publication date: May 13, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventor: Jose-Luis Diaz-Fernandez
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Patent number: 7713996Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, A, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: September 12, 2006Date of Patent: May 11, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Konrad Bleicher, Simona M Ceccarelli Grenz, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch
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Publication number: 20100099891Abstract: A data processing method for an estimation of compound-protein interaction using both chemical substance information, such as a chemical property of the compound, and biological information, such as sequence information of genes to rationally and efficiently screen compounds. First space representing space coordinates of a first chemical substance group and second space representing space coordinates of a second chemical substance group are defined, and the first chemical substance group is characterized by a first characteristic amount and the second chemical substance group is characterized by a second characteristic amount, and map transformation of the coordinates of the first space and the coordinates of the second space results in the solution so as to increase the correlation between the first space and the second space using a multivariable analysis technique or a machine learning method.Type: ApplicationFiled: November 20, 2008Publication date: April 22, 2010Applicant: Kyoto UniversityInventors: Yasushi OKUNO, Kei TANEISHI, Gozoh TSUJIMOTO
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Publication number: 20100096252Abstract: The present invention relates to photolabile or photoreleasable compounds including a caging moiety linked to an effector moiety, wherein the compounds are capable of releasing the effector moiety on irradiation, typically by flash irradiation with light. These compounds are particularly suitable for focal 2-photon uncaging The photoreleasable compounds can be used to deliver effector moieties such as carboxylic acids, preferably, neuroactive amino acids to sites where their activity is required. In preferred embodiments of the invention, the caging moiety is based on 4-carboxymethoxy-5,7-dinitroinlinyl and derivatives thereof.Type: ApplicationFiled: January 29, 2008Publication date: April 22, 2010Applicant: PHILADELPHIA HEALTH & EDUCATION CORPORATION, d/b/a DREXEL UNIVERSITY COLLEGE OFInventor: Graham Ellis-Davies
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Patent number: 7700642Abstract: The present invention provides a process for producing an aromatic unsaturated compound of the formula (4) wherein Ar represents an optionally substituted aromatic group or an optionally substituted heteroaromatic group, and Y represents an electron withdrawing group, which comprises reacting (a) a compound of the formula (1) Ar—H??(1) wherein Ar has the same meaning as defined above with (b) a compound of the formula (2) wherein Y has the same meaning as defined above, and Z represents a lower alkoxy, or a compound of the formula (3) wherein Y and Z have the same meanings as defined above, in the presence of (c) an acid or a compound which generates a mineral acid by its hydrolysis.Type: GrantFiled: August 25, 2004Date of Patent: April 20, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Weiqi Wang, Tetsuya Ikemoto
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Publication number: 20100076010Abstract: This invention relates to novel compounds that are dihydroindoles derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel dihydroindoles derivatives that are derivatives of silodosin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?-1A-adrenoreceptor antagonist, such as silodosin.Type: ApplicationFiled: August 31, 2009Publication date: March 25, 2010Inventor: Julie F. Liu
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Publication number: 20100063128Abstract: Compounds of formula (I): wherein: R1 represents an alkyl, cycloalkyl or cycloalkylalkyl group, R2 represents a linear or branched (C1-C6)alkyl group, and n represents from 1 to 6.Type: ApplicationFiled: October 17, 2007Publication date: March 11, 2010Inventors: Pascal Marchand, Vincent Babonneau, Sylvie Piessard, Muriel Duflos, Jean Albert, Valerie Audinot, Philippe Delagrange, Daniel-Henri Caignard
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Patent number: 7674816Abstract: The invention provides 2 aryl substituted derivatives of melatonin. The invention further provides pharmaceutical compositions comprising such derivatives, methods for preparing such derivatives, and methods of using such derivatives to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient, and to treat conditions affected by melatonin activity in a patient.Type: GrantFiled: December 23, 2004Date of Patent: March 9, 2010Assignee: Abraxis BioScience, LLCInventors: Chunlin Tao, Cheng-Zhi Yu, Neil P. Desai, Vuong Trieu
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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: 20100048589Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.Type: ApplicationFiled: August 11, 2009Publication date: February 25, 2010Inventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
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Publication number: 20100029645Abstract: This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLA2?). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.Type: ApplicationFiled: June 19, 2009Publication date: February 4, 2010Inventors: John C. McKew, Katherine L. Lee, Lihren Chen, Richard Vargas, James D. Clark, Cara Williams, Valerie Clerin, Suzana Marusic, Kevin Pong
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Patent number: 7655691Abstract: Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.Type: GrantFiled: September 27, 2005Date of Patent: February 2, 2010Inventors: Howard P. Sard, Louis Shuster, Bryan Roth, Cynthia Morency, Govindaraj Kumaran, Liang Xu
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Publication number: 20100022613Abstract: Compounds of general formula (I) W is chloro or fluoro; Z is a —SO2YR1 group wherein R1 is C3-C8 heterocyclyl, aryl or heteroaryl any of which may optionally be substituted with one or more substituents selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, and —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; Y is a straight or branched C1-C4 alkylene chain; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.Type: ApplicationFiled: January 22, 2009Publication date: January 28, 2010Applicant: Oxagen LimitedInventors: Richard Edward Armer, Graham Michael Wynne