Chalcogen Attached Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/58)
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Patent number: 8198464Abstract: The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.Type: GrantFiled: December 20, 2007Date of Patent: June 12, 2012Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Kousuke Komenoi, Atsushi Nakamura, Makoto Kasai, Masakazu Imamura, Ryota Shiraki, Keita Nakanishi
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Patent number: 8143069Abstract: A compound represented by the following general formula (II): wherein R21 represents hydrogen atom or one to four monovalent substituents substituting on the benzene ring, and when R21 represents two or more substituents, the substituents may be the same or different; R22, R24, R25, and R27 independently represent hydrogen atom, or a monovalent substituent; R23 represents —OH or —N(R28)(R29) (wherein R28 and R29 independently represent an alkyl group which may be substituted); R26 represents —N(R30)(R31) (wherein R30 and R31 independently represent an alkyl group which may be substituted); n represents an integer of 1 to 3; and Y represents —S— or —O—, which is useful for selective measurement of hypochlorite ion.Type: GrantFiled: March 1, 2007Date of Patent: March 27, 2012Assignee: The University of TokyoInventors: Tetsuo Nagano, Yasuteru Urano, Suguru Kenmoku
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Patent number: 8138218Abstract: A family of peptides and peptidomimetic compounds useful as GHS analogs according to either formula (I) or (II) as depicted below: or a pharmaceutically acceptable salts thereof, wherein the variables are as defined in the specification.Type: GrantFiled: July 24, 2006Date of Patent: March 20, 2012Assignee: Ipsen Pharma S.A.S.Inventors: Zheng Xin Dong, John S. Eynon, Yeelana Shen
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Publication number: 20120059012Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five- to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.Type: ApplicationFiled: May 12, 2010Publication date: March 8, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Akihito Fujii, Kazumi Niidome, Chiaki Migihashi, Toshiyuki Kamei, Takafumi Matsumoto, Tomoyuki Hirata
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Patent number: 8129425Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.Type: GrantFiled: April 27, 2006Date of Patent: March 6, 2012Assignee: Curis, Inc.Inventors: Anthony David Baxter, Edward Andrew Boyd, Maria Frank-Kamenetsky, Oivin Guicherit, Jeffery Porter, Stephen Price, Lee Rubin, John Harry Alexander Stibbard
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Publication number: 20120049174Abstract: A conjugated compound having a group represented by formula (I) and/or formula (II). [In the formulas, Ar represents an optionally substituted trivalent aromatic hydrocarbon or optionally substituted trivalent heterocyclic group, and A represents hydrogen, a halogen atom or a monovalent group. When multiple A groups are present they may be the same or different, and at least one A represents an electron-withdrawing group. Ar? represents an optionally substituted C6 or greater divalent aromatic hydrocarbon or optionally substituted C4 or greater divalent heterocyclic group, and R1 and R2 are the same or different and each represents hydrogen, a halogen atom or a monovalent group, while A? represents hydrogen, a halogen atom or a monovalent group. When multiple A? groups are present they may be the same or different, and at least one A? represents an electron-withdrawing group.Type: ApplicationFiled: March 10, 2010Publication date: March 1, 2012Applicants: OSAKA UNIVERSITY, SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yutaka Ie, Makoto Okabe, Yoshio Aso, Masato Ueda
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Publication number: 20120046307Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.Type: ApplicationFiled: October 16, 2009Publication date: February 23, 2012Applicant: UNIVERSITAET DES SAARLANDESInventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
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Publication number: 20120035371Abstract: The current invention describes novel chiral synthetic routes and intermediates for the manufacture of chiral anti-inflammatory agents of general formula VIII in which at least one of the groups X1, X2, X3 is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X1, X2, X3 have the meaning of a hydrogen atom, in which at least one of the groups Z1, Z2, Z3 is selected from —O—, —S—, —NH—, —N(—CH3)—, whereas the other groups Z1, Z2, Z3 have the meaning of a —CH2— group, and in which Ar is an aromatic group.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Inventor: Steffen SCHWEIZER
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Publication number: 20120035175Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.Type: ApplicationFiled: July 1, 2011Publication date: February 9, 2012Applicant: 4SC AGInventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
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Novel calcium salts of Compound as Anti-Inflammatory, Immunomodulatory and Anti-Proliferatory Agents
Publication number: 20120029034Abstract: The present invention relates to calcium salts of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1, and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.Type: ApplicationFiled: July 1, 2011Publication date: February 2, 2012Applicant: 4SC AGInventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT -
Publication number: 20110313003Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: June 16, 2010Publication date: December 22, 2011Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
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Publication number: 20110313032Abstract: The present invention is directed to a compound of formula (I), its diastereoisomers, its enantiomers or its pharmaceutically acceptable salts or solvates, formula (I), to procedures of obtaining the same, to intermediates thereof, and use as competitive inhibitors of the third enzyme of the shikimic acid pathway, the type II dehydroquinase.Type: ApplicationFiled: December 23, 2009Publication date: December 22, 2011Applicant: UNIVERSIDADE DE SANTIAGO DE COMPOSTELAInventors: Cóncepcion González Bello, Verónica Filipa Vieira Prazeres, Sonia Paz Gómez, Cristina Sánchez Sixto, Lorena Tizón Valverde
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Patent number: 8080576Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.Type: GrantFiled: February 19, 2010Date of Patent: December 20, 2011Assignee: Onyx Therapeutics, Inc.Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
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Publication number: 20110288300Abstract: The present invention discloses organic and inorganic photosensitizer dyes as the following formulas (1) to (3), wherein the substituents “A, B, D and G” are as defined in claim 1.Type: ApplicationFiled: October 5, 2010Publication date: November 24, 2011Applicant: NAIONAL CENTRAL UNIVERSITYInventors: Chun-Guey Wu, Jheng-Ying Li, Chia-Yuan Chen, Shi-Jhang Wu
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Patent number: 8063067Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.Type: GrantFiled: July 23, 2009Date of Patent: November 22, 2011Assignee: Merck Patent GmbHInventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
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Publication number: 20110281795Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: January 15, 2010Publication date: November 17, 2011Inventors: Songnian Lin, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
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Publication number: 20110275703Abstract: The present invention provides a compound represented by Formula (II): wherein R1 is a chlorine atom, a fluorine atom, a methyl group or an ethynyl group; Ar is a group represented by the following Formula (a), Formula (b), Formula (c) or Formula (d): wherein R2 is a C1-6 alkyl group which may be substituted with one or more halogen atoms, a C1-6 alkoxy group which may be substituted with one or more halogen atoms, a C1-3 alkylthio group, a halogen atom, a C1-3 alkylcarbonyl group or a C2-5 alkynyl group which may be substituted with —OR4; R3 is a hydrogen atom or a C1-3 alkyl group; R4 is a hydrogen atom or a C1-3 alkyl group; provided that Ar is a group represented by Formula (a) when R1 is a fluorine atom, methyl group or an ethynyl group, and that R2 is methoxy group, an ethoxy group, an isopropyl group, a propyl group, a trifluoromethyl group, a trifluoromethoxy group, 2-fluoroethyl group or 1-propynyl group when R1 is a methyl group or a pharmaceutically acceptable salt or a solvate thereof aType: ApplicationFiled: July 27, 2007Publication date: November 10, 2011Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Tsutomu Sato, Kiyofumi Honda, Takahiro Kawai, Koo Hyeon Ahn
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Publication number: 20110272681Abstract: A light-emitting element has high luminous efficiency and excellent durability. The light-emitting element includes at least a light-emitting layer between a positive electrode and a negative electrode, and emits light by electrical energy. The light-emitting element is characterized by containing a naphthacene compound that has a specific structure and organic fluorescent substance that has a fluorescence peak wavelength of not less than 500 nm but not more than 690 nm.Type: ApplicationFiled: January 19, 2010Publication date: November 10, 2011Applicant: TORAY INDUSTRIES, INC.Inventors: Kazunori Sugimoto, Tsuyoshi Tominaga
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Patent number: 8048897Abstract: A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity.Type: GrantFiled: July 26, 2005Date of Patent: November 1, 2011Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroharu Matsuoka, Tsutomu Sato, Masahiro Nishimoto, Nobuo Shimma
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Publication number: 20110245244Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: ApplicationFiled: April 4, 2011Publication date: October 6, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
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Publication number: 20110230488Abstract: The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.Type: ApplicationFiled: November 25, 2009Publication date: September 22, 2011Applicant: TRT PHARMA INC.Inventors: Jian Hui Wu, Gerald Batist, Jinming Zhou, Guoyan Geng, Rongtuan Lin
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Publication number: 20110220884Abstract: A compound for an organic thin film transistor having a structure represented by the following formula (1): wherein R1 and R2, and R3 and R4 are respectively combined with each other to form an aromatic hydrocarbon ring having 6 to 60 carbon atoms or an aromatic heterocyclic ring having 3 to 60 carbon atoms; the ring being fused to the ring to which the groups are bonded, whereby the structure of the formula (1) has 5 or more aromatic rings that are fused; and the fused rings formed by R1 and R2, and R3 and R4 each may have a substituent.Type: ApplicationFiled: August 20, 2009Publication date: September 15, 2011Inventors: Masatoshi Saito, Yuki Nakano, Hiroaki Nakamura, Hirofumi Kondo
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Patent number: 8013171Abstract: To provide an axially asymmetric optically active biaryl ester compound that can easily produced without the step of optical resolution which was almost indispensable in conventional methods. There is provided a method for producing an axially asymmetric ester compound, comprising a cycloaddition of a compound having a triple bond with the use of a catalyst containing rhodium metal and an optically active bisphosphine.Type: GrantFiled: June 1, 2009Date of Patent: September 6, 2011Assignees: National University Corporation Tokyo University of Agriculture and Technology, Takasago International CorporationInventor: Ken Tanaka
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Patent number: 8003684Abstract: Crystalline forms of (+)-R-zileuton, which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of (+)-R-zileuton are characterized by a variety of properties and physical measurements. As well, methods of producing crystalline (+)-R-zileuton, and using it to inhibit 5-lipoxygenase activity in subjects to treat a number of diseases, are also discussed.Type: GrantFiled: February 21, 2007Date of Patent: August 23, 2011Assignee: Cornerstone Therapeutics, Inc.Inventor: Jason A. Hanko
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Publication number: 20110184189Abstract: A method of preparation of N-(1-benzo[b]thien-2-ylethyl)-N-hydroxyurea of formula (I) with the use of a reaction of 1-(benzo[b]thien-2-yl)-ethanol of formula (II) with hydroxyurea of formula (III) in organic solvents, organic acids, their mixtures or in mixtures thereof with water, being catalyzed by strongly acidic cation exchangers or various hydrogen sulphates.Type: ApplicationFiled: April 6, 2009Publication date: July 28, 2011Inventors: Kamil Koristek, Pavel Hradil, Martin Grepl, Petr Slezar
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Patent number: 7981925Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: August 26, 2009Date of Patent: July 19, 2011Assignee: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110172435Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.Type: ApplicationFiled: November 12, 2010Publication date: July 14, 2011Applicant: ALLERGAN, INC.Inventors: Yariv Donde, Jeremiah H. Nguyen, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Wha-Bin Im
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Publication number: 20110165188Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Inventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Way Tsun Yue
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Publication number: 20110155242Abstract: A fluorescent material of Formula (I) is provided. In Formula (I), all the variables thereof are described in the specification. The invention also provides a solar cell with the disclosed fluorescent material. The solar cell with the fluorescent material includes a solar cell and a fluorescent layer including the disclosed fluorescent material of Formula (I) coating on the solar cell.Type: ApplicationFiled: April 3, 2010Publication date: June 30, 2011Applicants: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE, NEO SOLAR POWER CORPInventors: Ching-Yen Wei, Yi-Ling Chen, Wei-Jen Liu, Yi-Chen Chiu, Yang-Fang Chen, Kao-Chiang Hsu, Yu-Wei Tai, Chia-Ching Wang, Meng-Hsiu Wu
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Patent number: 7951963Abstract: A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein X1 represents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.Type: GrantFiled: March 27, 2006Date of Patent: May 31, 2011Assignee: Toyama Chemical Co., Ltd.Inventors: Akihito Saitoh, Yoshiaki Suzuki, Kenji Yonezawa, Mitsuhide Kawamura, Takahiko Kusanagi, Takashi Nakai
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Publication number: 20110112142Abstract: The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt: wherein R3 is selected from the group consisting of ORA; —CHO; —C(O)C1-4alkyl; —C(O)phenyl; —O—C(O)RA; and N(RB)2; R6 is selected from certain cyclic groups defined in the specification; and the remaining groups are defined in the specification; together with a pharmaceutically acceptable carrier. Most of the compounds are novel. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: April 8, 2009Publication date: May 12, 2011Inventors: Daniel Nöteberg, Elisabet Kallin, Mattias Wennerstål
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Patent number: 7939531Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: February 20, 2009Date of Patent: May 10, 2011Assignee: Roche Palo AltoInventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
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Publication number: 20110098480Abstract: A compound represented by the formula (I) or a pharmacologically acceptable salt thereof is used as an activator of PPAR. wherein each of R1 and R2 is hydrogen, C1-8 alkyl, C1-8 alkyl substituted with halogen, or the like; each of R3, R4, R5, and R6 is hydrogen, C1-8 alkyl, or the like; X is sulfur or the like; Y is oxygen, a bond, or the like; p is 0 or 1; A is oxygen, CH2, N—NH2, or the like; when p is 1, B is phenyl, which can have a substituent; when p is 0, B is a condensed ring such as benzisoxazole, which can have a substituent; m is an integer of 1 to 4; and n is an integer of 0 to 5.Type: ApplicationFiled: April 15, 2009Publication date: April 28, 2011Inventors: Shogo Sakuma, Rie Takahashi, Hideki Nakamura
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Publication number: 20110098484Abstract: A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein X1 represents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.Type: ApplicationFiled: January 6, 2011Publication date: April 28, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Akihito SAITOH, Yoshiaki Suzuki, Kenji Yonezawa, Mitsuhide Kawamura, Takahiko Kusanagi, Takashi Nakai
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Publication number: 20110092578Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present.Type: ApplicationFiled: December 20, 2010Publication date: April 21, 2011Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski
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Publication number: 20110092612Abstract: A novel polymerizable high-refractive index compound which is useful as an optical material, and a holographic recording medium using the same, which has high diffraction efficiency, high light transmittance and small rate of shrinkage, are provided. A composition for forming a holographic recording layer containing a reactive compound represented by the following formula 1, a holograph recording material, and a holographic recording medium provided with a recording layer containing the same, are disclosed.Type: ApplicationFiled: June 9, 2009Publication date: April 21, 2011Applicant: Mitsubishi Chemical CorporationInventors: Yasuaki Miki, Akiko Yabe, Jun Enda
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Publication number: 20110086877Abstract: Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.Type: ApplicationFiled: October 1, 2010Publication date: April 14, 2011Inventors: SINA BAVARI, RICK GUSSIO, JAMES C. BURNETT
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Publication number: 20110087034Abstract: A dihydroindacene compound represented by the following formula (1): wherein R1 is identical or different from each other, and each denotes a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, alkoxy which may be substituted, alkylthio which may be substituted, aryl which may be substituted, aryloxy which may be substituted, or the like; R2 to R5 are identical or different from each other, and each denote a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted, or the like; p is 0, 1, or 2; and ring structures A and B are identical or different from each other, and each denote a benzene ring which may be substituted, a thiophene ring which may be substituted, or the like.Type: ApplicationFiled: February 3, 2009Publication date: April 14, 2011Applicant: Sumitomo Chemical Company LimitedInventors: Yasuo Miyata, Hidenori Hanaoka
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Patent number: 7919519Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: GrantFiled: March 21, 2007Date of Patent: April 5, 2011Assignee: Epix Pharmaceuticals Inc.Inventors: Roland Burli, Victor J. Cee, Jennifer Golden, Brian Alan Lanman, Susana Neira, Ashis Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert C. Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker, Zhaoda Zhang
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Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions
Patent number: 7872024Abstract: The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: April 14, 2006Date of Patent: January 18, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Joey Methot, Thomas A. Miller, David J. Witter -
Publication number: 20100314615Abstract: Provided are: an aromatic amine derivative in which a terminal substituent such as a dibenzofuran ring or a dibenzothiophene ring is bonded to a nitrogen atom directly or through an arylene group or the like; an organic electroluminescence device including an organic thin film layer formed of one or more layers including a light emitting layer and interposed between a cathode and an anode in which a layer of the organic thin film layer contains the aromatic amine derivative by itself or as a component of a mixture, and the device has a long lifetime and high luminous efficiency; and an aromatic amine derivative for realizing the device.Type: ApplicationFiled: December 22, 2008Publication date: December 16, 2010Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Yumiko Mizuki, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
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Patent number: 7834034Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: April 14, 2006Date of Patent: November 16, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Dawn M. Mampreian, Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Publication number: 20100280250Abstract: A compound comprising a prodrug of a prostaglandin EP4 agonist, wherein said prodrug is an ester, ether, or amide of an amino acid is disclosed herein. Maintenance of the colonic mucosal barrier by method comprising administering a therapeutically effective amount of a prostaglandin EP4 agonist to a colon of a mammal is also disclosed herein. Dosage forms, medicaments, and compositions, related thereto are also disclosed.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Wha-Bin Im, Robert M. Burk, Mark Holoboski
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Publication number: 20100273824Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: January 18, 2008Publication date: October 28, 2010Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Publication number: 20100267780Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful inter alia for the treatment of obesity.Type: ApplicationFiled: September 8, 2008Publication date: October 21, 2010Inventors: Jason Bloxham, Stuart Edward Bradley, Thomas Martin Krulle, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth
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Publication number: 20100243971Abstract: The present invention relates to photochromic benzopyrans and to the use thereof in plastics of all kinds, especially for ophthalmic purposes. The inventive compounds are photochromic benzopyran compounds in which a polycyclic aromatic is joined to the 5 and 6 positions of a benzopyran, where the bond in the 6 position is direct and the bond in the 5 position is via a mono- or diatomic bridge.Type: ApplicationFiled: November 25, 2008Publication date: September 30, 2010Inventors: Manfred Melzig, Yven Rohlfing, Udo Weigand
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Publication number: 20100240720Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, for the targeted delivery of chemotherapeutic agents.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Publication number: 20100228015Abstract: This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.Type: ApplicationFiled: April 23, 2010Publication date: September 9, 2010Inventors: Mitchell A. deLong, Jill M. McFadden, Susan M. Royalty, Eric J. Toone, Jeffrey D. Yingling
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Publication number: 20100227898Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: June 30, 2008Publication date: September 9, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Harald Walter, Daniel Stierli, Hans Tobler
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Patent number: RE43372Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.Type: GrantFiled: June 5, 2009Date of Patent: May 8, 2012Assignee: Duke UniversityInventors: Mitchell Anthony deLong, David Lindsey Soper, John August Wos, Biswanath De