Carbonyl In Substituent Q Patents (Class 564/169)
  • Patent number: 7955815
    Abstract: Provided are two-photon fluorescent probes for imaging acidic vesicles in live cells and tissue. The probes are represented by The probes can selectively bind to vesicles in cytosol to emit two-photon excited fluorescence with high intensity. Therefore, the use of the probes enables effective imaging of acidic vesicles. Further provided is a method for imaging acidic vesicles in live cells and tissue using the probes.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: June 7, 2011
    Assignee: Korea University Industrial & Academic Collaboration Foundation
    Inventor: Bong-Rae Cho
  • Publication number: 20110118476
    Abstract: The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds.
    Type: Application
    Filed: July 23, 2008
    Publication date: May 19, 2011
    Inventors: David W. Bauer, Padraig M. O'Nell, Timothy J. Watson, Shanghui Hu
  • Publication number: 20110117055
    Abstract: Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.
    Type: Application
    Filed: November 18, 2010
    Publication date: May 19, 2011
    Inventors: James E. MacDonald, McKelvy F. Jeffrey, Flossie Wong-Staal
  • Publication number: 20110082109
    Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 7, 2011
    Applicant: AJINOMOTO CO., INC.
    Inventors: Wataru MIYANAGA, Yoichiro Shima, Misato Noguchi, Akiko Oonuki, Yayoi Kawato, Hiroshi Iwata, Eri Harada, Ryuta Takashita, Hirokazu Ueno, Tadakiyo Nakagawa
  • Publication number: 20110077430
    Abstract: The present invention is related to a precursor for no-carrier-added fluorine-18 labeled ethacrynic acid, N-(4-[18F]fluorobutyl)-Ethacrynic amide([18F]FBuEA) and the preparation method for HPLC non-radioactive standards. Its chemical structure is shown in the following: In the precursor, R1 represents a protective group for the amide functional group; R2 represents leaving group; or R1 represents carboxyl group, R2 represents p-tosyloxy, methane sulfonyloxy group or trifluoromethane sulfonyloxy group or bromine (Br). For the HPLC non-radioactive standards, R1 represents a protective group for the amide functional group and hydrogen, R2 represents fluorine.
    Type: Application
    Filed: September 30, 2009
    Publication date: March 31, 2011
    Inventors: Chung-Shan Yu, Li-Wu Chiang, Hao-Lien Huang, Yu-Hsuan Ku, Chia-Jung Chen, Shao Wei Chen, Yean-Hung Tu, Mao-Hsung Chang, Jenn-Tzong Chen, Wuu-Jyn Lin
  • Publication number: 20110071142
    Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.
    Type: Application
    Filed: March 19, 2010
    Publication date: March 24, 2011
    Applicant: BETH ISRAEL DEACONESS MEDICAL CENTER
    Inventors: Peter Oettgen, Alan C. Rigby, Towia Libermann
  • Publication number: 20110060164
    Abstract: A method for the preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of ?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butanamide, about 0.05% or less of difluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.
    Type: Application
    Filed: November 11, 2010
    Publication date: March 10, 2011
    Applicant: ARCH PHARMALABS LIMITTED
    Inventors: Ganesh Gurpur Pai, K. Nanda Kishore, Narendra P. Chaudhari, N. Anjaneyulu, B. N. Ghogare
  • Patent number: 7872154
    Abstract: A method for the preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of ?-[2-methyl-1-oxopropyl]-?-oxo-N-p-diphenylbenzene butanamide, about 0.05% or less of difluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.
    Type: Grant
    Filed: October 22, 2008
    Date of Patent: January 18, 2011
    Assignee: Arch Pharmalabs Limited
    Inventors: Ganesh Gurpur Pai, K. Nanda Kishore, Narendra P. Chaudhari, N. Anjaneyulu, B. N. Ghogare
  • Publication number: 20110009638
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.
    Type: Application
    Filed: April 8, 2009
    Publication date: January 13, 2011
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventor: Gary David Annis
  • Patent number: 7851658
    Abstract: A novel palladium-mediated carbon-carbon bond forming reaction has been discovered using DNA-templated chemistry. The inventive reaction involves the palladium-mediated coupling of a terminal alkyne with an alkene to form an enone. A catalytic amount of palladium may be used in the reaction if an oxidant is present. The reactions is also compatible with a variety of organic solvent as well as aqueous solution. Both intermolecular and intramolecular reactions have been demonstrated. This novel carbon-carbon bond forming reaction is particularly useful in the synthesis of macrocycles. Kits, reagents, catalysts, solvents, oxidants, salts, acids, instructions, and other materials useful in the practice of the inventive reaction are also provided.
    Type: Grant
    Filed: August 17, 2005
    Date of Patent: December 14, 2010
    Assignee: President and Fellows of Harvard College
    Inventors: David R. Liu, Matthew W. Kanan, Mary M. Rozenman
  • Publication number: 20100312013
    Abstract: A process for synthesis of a compound of Formula (X) wherein: R1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl, wherein each substituent group of R1 is optionally independently substituted with one to three substituents selected from C1-C3 alkyl, C1-C3 alkoxy, phenyl, and alkoxyphenyl; and R2 and R3 are each independently C1-C5 alkyl.
    Type: Application
    Filed: May 27, 2010
    Publication date: December 9, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Daniel R. FANDRICK, Nathan K. YEE, Jinhua J. SONG, Jonathan T. REEVES
  • Publication number: 20100292289
    Abstract: The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.
    Type: Application
    Filed: November 26, 2008
    Publication date: November 18, 2010
    Applicant: AMPLA Pharmaceuticals Inc.
    Inventor: James R. Hauske
  • Publication number: 20100286427
    Abstract: A compound represented by the following general formula (I): [R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(COR6)—CO—, —CO—N(COR7)— (R6 and R7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents —Y—CH(R12)—COOH, —CHO, —CH?CH—COOH, or —COOR13 (Y represents a single bond, —CH2—, —CH(OH)—, —CO—, —CO—NH—, or —CO—NH—CH2—CO—NH—, R12 represents hydrogen atom or a lower alkyl group, and R13 represents hydrogen atom, —CH(R14)—COOH(R14 represents hydrogen atom, a lower alkyl group, or hydroxy group), —[CH2CH2—O]n—CH2—CH2—OH, —CH2—O—[CH2CH2—O]m—CH2—OH, or —[CH(CH3)—CO—O]p—CH(CH3)—COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.
    Type: Application
    Filed: October 31, 2007
    Publication date: November 11, 2010
    Applicant: RESEARCH FOUNDATION ITSUU LABORATORY
    Inventors: Hideaki Muratake, Koichi Shudo
  • Publication number: 20100249424
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.
    Type: Application
    Filed: August 4, 2008
    Publication date: September 30, 2010
    Applicant: E.I.DuPont De Nemours and Company
    Inventors: Gary David Annis, Brenton Todd Smith
  • Patent number: 7799954
    Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: September 21, 2010
    Assignee: Abraxis BioScience, LLC
    Inventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
  • Publication number: 20100234404
    Abstract: Compounds and compositions for modulating the activity of p38 kinases are provided, including p38?, and p38? kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.
    Type: Application
    Filed: May 28, 2010
    Publication date: September 16, 2010
    Inventors: Hengyuan Lang, Jiong Lan, Yungeng Fang
  • Patent number: 7763750
    Abstract: A novel process for producing a 2-halogenobenzamide compound useful as a raw material or active ingredient for medicines and agricultural chemicals. The process, which is for producing a 2-halogenobenzamide compound represented by the general formula (I): (wherein R1, R2, R3, R4, and R6 may be the same or different and each represents hydrogen or C1-6 alkyl; R5 represents C1-6 alkyl; k is 1 or 2; Y1, Y2, Y3, and Y4 may be the same or different and each represents hydrogen, halogeno, etc.; and X represents chlorine, bromine, or iodine), is characterized by reacting an benzamide compound with a halogenating agent in the presence of a palladium catalyst to obtain a substituted benzamide compound and then reacting the resultant substituted benzamide compound with an oxidizing agent after or without isolating the substituted benzamide compound.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: July 27, 2010
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Noboru Abe, Hiroki Kodama, Akihiko Yoshiura
  • Publication number: 20100120939
    Abstract: The invention provide a new class of silicone-containing prepolymers containing ethylenically unsaturated groups and latent UV-activated free radical generating moieties. This class of silicone-containing prepolymer is capable of being actinically crosslinked in the presence of one or more hydrophilic vinylic monomers to form a silicone hydrogel material with a hydrophilic surface without post curing surface treatment. The present invention is also related to silicone hydrogel contact lenses made from this class of silicone-containing prepolymers and a vinylic monomer having a latent UV-activated free radical generating moiety.
    Type: Application
    Filed: November 11, 2009
    Publication date: May 13, 2010
    Inventor: John Christopher Phelan
  • Publication number: 20100120789
    Abstract: There is provided a compound having Formula I R1—Z—R2 ??Formula I wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(?O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S?O, and S(?O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p- NR10—S(?O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)v-Y—(CR15R16)w- where Y is a heteroaryl group in which a bond in the hetero
    Type: Application
    Filed: September 7, 2009
    Publication date: May 13, 2010
    Inventors: Nigel Vicker, Xiangdong Su, Fabienne Praduax, Michael John Reed, Barry Victor Lloyd Potter
  • Publication number: 20100104979
    Abstract: Compounds of the Formula (I) wherein x is an integer from 1-4; p is an integer from 1-3; q is an integer from 0-3; Ar is phenyl, naphthyl, anthryl or phenanthryl each of which optionally is substituted by one or more Cl, CN, OR5, C3-C5alkenyl or C1-C6alkyl which optionally is substituted by one or more OR6, COOR or halogen; R1 if x is 1, is ORS, O—X+, NR8R9, C1-C20alkyl optionally substituted by one or more COOR10, or is C2-C20alkyl interrupted by one ore more O, or is C2-C5alkenyl or phenyl-C1-C4alkyl; R1 if x is 2, is for example C1-C20alkylene; R1 if x is 3, is for example a tri-valent radical; R1if x is 4, is for example a tetravalent radical; R2and R3are hydrogen or C1-C8alkyl, or R2and R3 together are O, C1-C3alkylene or CH?CH; R4 is C1-C4alkyl; R5, R6, R7, R8, R9 and R10 are for example hydrogen or C1-C4alkyl; and X is a x-valent cationic counter ion; are in particular suitable as photoinitiators for the curing with UV-A light (320-450 nm).
    Type: Application
    Filed: March 25, 2008
    Publication date: April 29, 2010
    Inventors: Kurt Dietliker, Peter Murer, Rinaldo Hüsler, Tunja Jung
  • Patent number: 7700808
    Abstract: There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6 haloalkyl group or C3-C8 halocycloalkyl group, R2 represents methyl group, halogen atom, cyano group or the like, m represents an integer of 1 to 5, and n represents an integer of 1 to 4).
    Type: Grant
    Filed: December 25, 2006
    Date of Patent: April 20, 2010
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takashi Mizukoshi, Yasuhiro Sakurai, Kazutaka Matoba, Manabu Yaosaka
  • Patent number: 7687662
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: March 30, 2010
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20100036163
    Abstract: Process for the industrial synthesis of the compound of formula (I)
    Type: Application
    Filed: August 3, 2009
    Publication date: February 11, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Christophe Hardouin, Jean-Pierre Lecouve
  • Patent number: 7632850
    Abstract: The present invention provides a compound of the formula (I): in which R1, R2, R3, A and n are described and set forth more fully herein. Also provided are their preparation and their application in therapy.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: December 15, 2009
    Assignee: Sanofi-aventis
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Antoine Ravet
  • Publication number: 20090298907
    Abstract: A method for the preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-y-oxo-N-?-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of ?-[2-methyl-1-oxopropyl]-?-oxo-N-p-diphenylbenzene butanamide, about 0.05% or less of difluoro-?-[2-methyl-1-oxopropyl]-y-oxo-N-?-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.
    Type: Application
    Filed: October 22, 2008
    Publication date: December 3, 2009
    Inventors: Ganesh Gurpur PAI, K. Nanda KISHORE, Narendra P. CHAUDHARI, N. ANJANEYULU, B N. GHOGARE
  • Publication number: 20090281154
    Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Application
    Filed: June 7, 2007
    Publication date: November 12, 2009
    Inventors: James B. Doherty, Swaminathan R. Natarajan, Dong-Ming Shen, Fengqi Zhang
  • Publication number: 20090270423
    Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.
    Type: Application
    Filed: March 27, 2009
    Publication date: October 29, 2009
    Inventors: Helen E. Blackwell, Matthew D. Bowman, Joseph R. Stringer
  • Patent number: 7605288
    Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: October 20, 2009
    Assignee: University of Kansas
    Inventors: Brian Blagg, Gang Shen, Randell C. Clevenger
  • Publication number: 20090239909
    Abstract: The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.
    Type: Application
    Filed: March 24, 2009
    Publication date: September 24, 2009
    Applicant: AMPLA Pharmaceuticals Inc.
    Inventor: James R. Hauske
  • Publication number: 20090221852
    Abstract: The diketone of atorvastatin is prepared by first washing a reaction vessel with a non-ketonic solvent, especially tetrahydrofuran, to remove water.
    Type: Application
    Filed: September 9, 2005
    Publication date: September 3, 2009
    Inventors: Susan O'Sullivan, Elizabeth Fox
  • Publication number: 20090186790
    Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising: a) a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-fragrance unit; and b) a pro-fragrance unit, which when so released is either i) a pro-fragrance compound capable of releasing a fragrance raw material; or ii) a fragrance raw material. The present invention relates to systems for delivering fragrances to a situs, and to laundry detergent compositions, fine fragrances, personal care and hair care compositions comprising said systems.
    Type: Application
    Filed: March 26, 2009
    Publication date: July 23, 2009
    Inventors: Robert Richard Dykstra, Gregory Scot Miracle, Lon Montgomery Gray
  • Publication number: 20090163549
    Abstract: The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R1 and R2 are hydrogen etc., R3 is lower alkyl, R4 is lower alkyl or aryloxy, or R3 and R4 taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.
    Type: Application
    Filed: December 13, 2006
    Publication date: June 25, 2009
    Inventor: Hiroyuki Kai
  • Publication number: 20090155837
    Abstract: Provided are two-photon fluorescent probes for imaging acidic vesicles in live cells and tissue. The probes are represented by The probes can selectively bind to vesicles in cytosol to emit two-photon excited fluorescence with high intensity. Therefore, the use of the probes enables effective imaging of acidic vesicles. Further provided is a method for imaging acidic vesicles in live cells and tissue using the probes.
    Type: Application
    Filed: October 15, 2008
    Publication date: June 18, 2009
    Inventor: Bong-Rae Cho
  • Publication number: 20090105223
    Abstract: To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.
    Type: Application
    Filed: April 26, 2007
    Publication date: April 23, 2009
    Applicant: NATIONAL UNIVERSITY CORPORATION CHIBA UNIVERSITY
    Inventors: Kazuei Igarashi, Hiromitsu Takayama
  • Publication number: 20090075989
    Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula 1, the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.
    Type: Application
    Filed: December 20, 2007
    Publication date: March 19, 2009
    Inventors: Wolfgang Schwede, Carsten Moeller, Anja Schmidt, Ulrike Fuhrmann, Andrea Rotgeri, Thomas Andrew Kirkland, Ralf Wyrwa
  • Publication number: 20090069430
    Abstract: The invention is directed to a compound of formula (I) Having VDCC blocking activity. These compounds are useful for the treatment of a series of human diseases and conditions, especially cognitive or neurodegenerative diseases or conditions.
    Type: Application
    Filed: June 16, 2008
    Publication date: March 12, 2009
    Applicant: NEUROPHARMA, S.A.
    Inventors: Ana MARTINEZ GIL, Ana Castro Morera, Miguel Medina Padilla, Pilar Munoz Ruiz, Laura Rubio Arrieta, Esther Garcia Palomero, Celia De Austria De Luque, Jorge Sanchez-Quesada, Daniel Ignacio Perez Fernandez, Javier Lopez Ogalla, Diana Alonso Gordillo
  • Publication number: 20090060873
    Abstract: The present invention overcomes limitations of the prior art by providing new compounds and methods for the treatment of conditions, such as neurodegenerative diseases (e.g., multiple sclerosis), psychiatric disorders (e.g., psychosis, bipolar disorder, depression, neuropathic pain), conditions involving CNS-mediated chronic pain, spinal cord injuries, and other diseases or injuries.
    Type: Application
    Filed: May 5, 2008
    Publication date: March 5, 2009
    Applicant: Reata Pharmaceuticals, Inc.
    Inventors: Michael B. Sporn, Karen T. Liby, Gordon W. Gribble, Tadashi Honda, John Letterio
  • Publication number: 20090054450
    Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors.
    Type: Application
    Filed: June 17, 2008
    Publication date: February 26, 2009
    Applicant: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: Mark G. CURRIE, John Jeffrey TALLEY, Brian CALI
  • Publication number: 20090048258
    Abstract: The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R1 and R2 are each independently a hydrogen atom or a substituent, R3 is a hydrogen atom or a C1-6 alkyl group, or R3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra1 is an optionally substituted hydrocarbon group, and Ra2 and Ra3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.
    Type: Application
    Filed: January 31, 2006
    Publication date: February 19, 2009
    Inventors: Masaki Ogino, Yoshihisa Nakada, Mitsuyuki Shimada, Kouhei Asano, Norikazu Tamura, Minori Masago
  • Publication number: 20090023923
    Abstract: There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6 haloalkyl group or C3-C8 halocycloalkyl group, R2 represents methyl group, halogen atom, cyano group or the like, m represents an integer of 1 to 5, and n represents an integer of 1 to 4).
    Type: Application
    Filed: December 25, 2006
    Publication date: January 22, 2009
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD
    Inventors: Takashi Mizukoshi, Yasuhiro Sakurai, Kazutaka Matoba, Manabu Yaosaka
  • Patent number: 7476763
    Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I: methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical formulations and related methods of treating or inhibiting certain diseases or conditions.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: January 13, 2009
    Assignee: Gruenenthal GmbH
    Inventors: Corinna Sundermann, Bernd Sundermann
  • Patent number: 7442830
    Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: August 6, 2007
    Date of Patent: October 28, 2008
    Assignee: Millenium Pharmaceuticals, Inc.
    Inventors: Edward J. Olhava, Mihaela Diana Danca
  • Publication number: 20080249137
    Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.
    Type: Application
    Filed: September 6, 2006
    Publication date: October 9, 2008
    Inventors: Jack Lin, Patrick Womack, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
  • Patent number: 7429669
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: September 30, 2008
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20080200467
    Abstract: Disclosed are alpha keto amide and alpha hydroxy amide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.
    Type: Application
    Filed: November 2, 2007
    Publication date: August 21, 2008
    Inventors: Dinesh Patel, Richard D. Gless, Heather K. Webb Hsu, Sampath Kumar Anandan, Bhaskar R. Aavula
  • Publication number: 20080146586
    Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.
    Type: Application
    Filed: November 14, 2007
    Publication date: June 19, 2008
    Applicant: Abraxis BioScience
    Inventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
  • Publication number: 20080125350
    Abstract: The present invention provides a branched polyalkylene glycol wherein three or more single-chain polyalkylene glycols and a group having reactivity with an amino acid side chain, the N-terminal amino group or the C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity are bound; and a physiologically active polypeptide modified with the branched polyalkylene glycol.
    Type: Application
    Filed: October 23, 2007
    Publication date: May 29, 2008
    Applicant: KYOWA HAKKO KOGYO CO., LTD.
    Inventors: Motoo Yamasaki, Toshiyuki Suzawa, Tatsuya Murakami, Noriko Sukurai, Kinya Yamashita, Mayumi Mukai, Takashi Kuwabara
  • Patent number: 7348322
    Abstract: The present invention relates to compounds of formula I: wherein A, X, R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: March 25, 2008
    Assignee: Roche Palo Alto LLC
    Inventors: Leyi Gong, Counde O'Yang, Yun-chou Tan
  • Patent number: 7326813
    Abstract: Disclosed is a process for producing a benzylamine derivative represented by the general formula (3): wherein X1, R1 and R2 are as defined below, which comprises reacting a benzyl derivative represented by the general formula (1): wherein X1 represents a halogen atom and R1 represents an acyl group, with a haloacyl compound represented by the general formula (2): R2—X2??(2) wherein X2 represents a halogen atom and R2 represents an acyl group, in the presence of Lewis acid. According to this method, a benzylamine derivative as an intermediate, which is useful for the preparation of a carbamate-based agricultural or horticultural bactericide, can be preferably prepared.
    Type: Grant
    Filed: December 26, 2003
    Date of Patent: February 5, 2008
    Assignee: Ihara Chemical Industry
    Inventors: Akinori Ito, Hideaki Ohashi, Kagetomo Magaribuchi
  • Patent number: 7300948
    Abstract: Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table R1 R2 R4 R5 R8a F CF3 Me H —OH F CF3 Cl H —OH F CF3 Me H —O—CH2CO2H Cl CN Cl H —OH.
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: November 27, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pierre Bonneau, Patrick Deroy, Alexandre Gagnon, Jeffrey O′Meara, Bruno Simoneau, Christiane Yoakim