Oxy Patents (Class 562/444)
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Publication number: 20110269834Abstract: Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).Type: ApplicationFiled: August 21, 2009Publication date: November 3, 2011Applicants: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS, PURDUE RESEARCH FOUNDATIONInventors: Arun K. Ghosh, Jun Takayama, Andrew David Mesecar, Michael E. Johnson, Kiira M. Ratia, Rima Chaudhuri, Debbie C. Mulhearn
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Publication number: 20110257374Abstract: Described herein are methods, compositions and articles of manufacture involving neutral conjugated polymers including methods for synthesis of neutral conjugated water-soluble polymers with linkers along the polymer main chain structure and terminal end capping units. Such polymers may serve in the fabrication of novel optoelectronic devices and in the development of highly efficient biosensors. The invention further relates to the application of these polymers in assay methods.Type: ApplicationFiled: January 19, 2011Publication date: October 20, 2011Applicant: Sirigen, Inc.Inventors: Brent S. Gaylord, Jean M. Wheeler, Glenn P. Bartholomew, Yongchao Liang, Janice W. Hong, William H. Huisman, Frank Peter Uckert, Lan T. Tran, Adrian Charles Vernon Palmer, Trung Nguyen, Russell A. Baldocchi
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Patent number: 8039495Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: October 15, 2010Date of Patent: October 18, 2011Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Publication number: 20110251418Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 4, 2011Publication date: October 13, 2011Applicant: AJINOMOTO CO., INC.Inventors: Masayuki Sugiki, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
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Publication number: 20110212072Abstract: Described are a method and a composition for preventing and/or treating a disease related to mitochondrial dysfunction by inhibiting the fatty acid oxidation of one or more cells of an organism. Particularly, the fatty acid oxidation is inhibited by inhibiting the expression and/or activity of the enzyme Camitin-Palmitoyl-Transferase-1 (CPT-1) by means of an arylalkyl- or arlyoxyalkyl-substitued oxirane carboxylic acid or pharmaceutically acceptable salts and derivatives of the arylalkyl-substituted oxirane carboxylic acid.Type: ApplicationFiled: April 19, 2011Publication date: September 1, 2011Applicant: MediGene AGInventors: Thomas Henkel, Christoph Rehfuess
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Patent number: 8003697Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: GrantFiled: December 18, 2009Date of Patent: August 23, 2011Assignees: Emisphere Technologies, Inc., Novartis AGInventors: William Elliot Bay, Rajesh K. Agarwal, Kiran Chaudhary, Michael M. Goldberg, JoAnne P. Corvino, Shingai Majura, Moise Azria, Joseph Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph Zielinski
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Publication number: 20110189779Abstract: The present invention provides an iron chelating agent which can selectively chelate iron ions. The iron chelating agent of the present invention includes a compound represented by the following formula (1) or a salt thereof (wherein, ring Z represents an aromatic hydrocarbon ring or an aromatic heterocyclic ring; R1 represents an alkylene group; R2 and R3 each independently represent a hydrogen atom, a hydrocarbon group or a group having chelating ability; and the total coordination number of the groups represented by R2 and R3 is 1 or 2.Type: ApplicationFiled: September 18, 2009Publication date: August 4, 2011Applicants: YAMAGATA UNIVERSITY, National University Corporation ASAHIKAWA MEDICAL COLLEGEInventors: Yutaka Kohg, Katsuya Ikuta, Katsunori Sasaki, Yuzo Nishida
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Publication number: 20110172442Abstract: The amino acid derivative of the present invention provides a novel compound that shows excellent analgesic action. The amino acid derivative of the present invention is a novel compound that shows excellent analgesic action to not only a model animal for nociceptive pains but also a model animal for neuropathic pains, so that the amino acid derivative is very useful as a drug for treating various pain diseases.Type: ApplicationFiled: September 17, 2009Publication date: July 14, 2011Applicant: NIPPON ZOKI PHARMACEUTICAL CO., LTD.Inventors: Tomohiro Ookubo, Ko Nakamura, Hiroyoshi Nanba, Hiroyuki Yoshida, Yoshitaka Nakazawa
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Publication number: 20110160252Abstract: First, the present inventors assessed the effect of the compound represented by formula (III) below on Huh-7 cells infected with HBV, and demonstrated that the compound alone had an anti-HBV effect in vitro. Formula (III) Then, the present inventors revealed that the HBV replication-suppressing effect of PEG-IFN is enhanced in chimeric mice having a human liver infected with genotype C or A HBV when PEG-IFN is used in combination with the compound represented by formula (III) above. The present inventors also revealed that the HBV replication-suppressing effect of Entecavir is enhanced in chimeric mice having a human liver infected with genotype C HBV (wild-type and Entecavir-resistant strains) when Entecavir is used in combination with the compound represented by formula (III) above.Type: ApplicationFiled: June 18, 2009Publication date: June 30, 2011Inventors: Masashi Mizokami, Yasuhito Tanaka, Masaya Sugiyama, Masayuki Sudoh
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Publication number: 20110152220Abstract: The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.Type: ApplicationFiled: March 30, 2009Publication date: June 23, 2011Inventors: Gerard Karsenty, Patricia F. Ducy, Yuli Xie, Donald Landry, Vijay Kumar Yadav
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Publication number: 20110136792Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 20, 2010Publication date: June 9, 2011Inventors: David Robert Bolin, Stuart Hayden, Yimin Qian, Kshitij Chhabilbhai Thakkar
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Publication number: 20110136911Abstract: Methods and compositions are disclosed for the use of dextrothyroxine (D-T4) to treat sepsis, inflammation, and conditions and diseases in which it is desirable to inhibit macrophage migration inhibitory factor (MIF).Type: ApplicationFiled: December 18, 2008Publication date: June 9, 2011Applicant: The Feinstein Institute for Medical ResearchInventor: Yousef Al-Abed
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Publication number: 20110123976Abstract: A method is provided for the parallel identification of one or more metabolite species within a biological sample. The method comprises analyzing the sample to produce a spectrum containing individual spectral peaks representative of the one or more metabolite species contained within the sample; subjecting each of the individual spectral peaks to a statistical pattern recognition analysis to identify the one or more metabolite species contained within the sample; and identifying the one or more metabolite species contained within the sample by analyzing the individual spectral peaks of the spectra.Type: ApplicationFiled: October 13, 2010Publication date: May 26, 2011Applicant: Purdue Research FoundationInventors: M. Daniel Raftery, Vincent Asiago
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Publication number: 20110124648Abstract: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: ApplicationFiled: January 25, 2011Publication date: May 26, 2011Applicant: ELI LILLY AND COMPANYInventors: Scott Eugene CONNER, Guoxin ZHU, Jianke LI
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Publication number: 20110118322Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 15, 2010Publication date: May 19, 2011Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Publication number: 20110118353Abstract: The present invention relates to a glycine transporter-1 inhibitor having the formula (I) wherein X is 1-3 substituents selected from H, halogen, methyl, methoxy, trifluoromethyl and trifluoromethoxy and Y is 1-3 substituents selected from H, methyl and halogen or a pharmaceutically acceptable salt thereof for use in a treatment in humans to suppress the level of one or more hormone selected from luteinizing hormone, follicle-stimulating hormone, estradiol and testosterone. The present invention further relates to such a glycine transporter-1 inhibitor as part of a contraceptive regimen or as a treatment for hypersexuality.Type: ApplicationFiled: November 4, 2008Publication date: May 19, 2011Inventors: Robert Gerard Jules Marie Hanssen, Jacques Schipper, Josephus Hubertus Schoemaker
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Patent number: 7932420Abstract: The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.Type: GrantFiled: March 14, 2008Date of Patent: April 26, 2011Assignee: Allergan, Inc.Inventor: Robert M. Burk
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Patent number: 7915314Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: GrantFiled: December 18, 2009Date of Patent: March 29, 2011Assignees: Emisphere Technologies, Inc., Novartis AGInventors: William Elliot Bay, Rajesh K. Agarwal, Kiran Chaudhary, Michael M. Goldberg, JoAnne P. Corvino, Shingai Majura, Moise Azria, Joseph Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph Zielinski
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Publication number: 20110059924Abstract: A method for preventing or treating colorectal cancer in a patient possessing human tropomyocin isoform TC22 is presented. Also presented is a method for evaluating TC22 expression reduction activity of a compound.Type: ApplicationFiled: May 17, 2006Publication date: March 10, 2011Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Kiron M. Das, Jim Chung-Chin Lin
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Publication number: 20110020324Abstract: A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like. wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.Type: ApplicationFiled: September 10, 2010Publication date: January 27, 2011Applicant: ONO PHARMACEUTICAL CO., LTDInventors: Shinji NAKADE, Hirotaka Mizuno, Takeji Ono, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
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Publication number: 20100317854Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20100286416Abstract: The present invention provides the production method of carboxylic acid compound, as shown in Scheme I.Type: ApplicationFiled: March 26, 2010Publication date: November 11, 2010Applicant: Japan Tobacco Inc.Inventors: Katsuya Matsumoto, Katsuyuki Yokota, Yuko Shinagawa, Teruhiko Inoue
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Publication number: 20100286227Abstract: The present invention relates to compounds from mycelium of Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) infection.Type: ApplicationFiled: January 28, 2008Publication date: November 11, 2010Applicant: SIMPSON BIOTECH CO., LTD.Inventors: Chia-Chin Sheu, Tun-Tschu Chang, Masao Hattori
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Publication number: 20100274026Abstract: The object of the present invention is to provide a pharmaceutical composition for preventing or treating viral infectious diseases. The compounds of the present invention have extremely potent anti-HCV activity and HCV growth inhibitory effects, and since they also only demonstrate mild cytotoxicity in vivo, a pharmaceutical composition containing the compound of the present invention is extremely useful as an anti-HCV preventive/therapeutic agent.Type: ApplicationFiled: July 6, 2010Publication date: October 28, 2010Inventors: Masahiro Aoki, Hideyuki Kato, Masayuki Sudoh, Takuo Tsukuda, Miyako Masubuchi, Kenichi Kawasaki
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Publication number: 20100240678Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.Type: ApplicationFiled: March 10, 2010Publication date: September 23, 2010Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
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Publication number: 20100217009Abstract: A process for preparing a compound of formula (22), comprising reducing a compound of formula (21), to produce a compound of formula (23), followed by the hydrogenolysis of the compound of formula 23 in a solvent comprising a C1 to C6 alkyl sulfonic acid and optionally a chlorinated solvent.Type: ApplicationFiled: May 21, 2008Publication date: August 26, 2010Applicant: BIAL - PORTELA & CA, S.A.Inventors: David Alexander Learmonth, Alexander Beliaev
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Publication number: 20100210792Abstract: Formulations of drugs and crystalline side chain polymers to provide controlled and/or sustained release drug formulations.Type: ApplicationFiled: December 4, 2007Publication date: August 19, 2010Inventors: David Taft, Steven Bitler, Qiang Zheng, Adam Bell, Stelios Tzannis
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Publication number: 20100197924Abstract: The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.Type: ApplicationFiled: December 16, 2009Publication date: August 5, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Alexandra E. Gould, Sean J. Harrison, Hirotake Mizutani, Ming Shen, Thomas E. Smyser, Stephen G. Stroud
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Publication number: 20100168468Abstract: A wrinkle-preventing and -improving composition comprising one or more than one compound selected from the group consisting of ?-amino acid derivatives represented by the following general formula (1) and salts thereof: wherein, R1 represents hydrogen atom, CH3 group or CH2OH group, R2 and R3 each independently represent hydrogen atom, alkyl group having 1 to 4 carbons, provided that R2 and R3 cannot be hydrogen atom at the same time, or R2 and R3 together with N atom to which they are bound may form a ring structure having a total carbon number of 4 to 6, in which case said ring structure may optionally contain an oxygen atom as a heteroatom, R4 represents hydrogen atom, alkyl group having 1 to 18 carbons, wherein when R1 and R4 are hydrogen atom, it cannot be that one of R2 and R3 is benzyloxycarbonyl group and the other is hydrogen atom.Type: ApplicationFiled: July 26, 2006Publication date: July 1, 2010Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Makoto TSUNENAGA, Haruhi IWAKI, Toshii IDIDA, Mikiko KAMINUMA, Masaru SUETSUGU, Keiko TAKADA, Shinji INOMATA
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Publication number: 20100075926Abstract: The invention provides methods and compounds for the treatment of neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (Amyotrophic Lateral Sclerosis), traumatic brain injury, ischemic brain injury or a stroke. In one aspect the compounds are HDAC1 activators. Exemplary HDAC1 activators include metal chelators, iron chelators, deferoxamin, flavonoids, compounds comprising a catechol moity, ginkgetin K, Chembridge 5104434, sciadopilysin, tetrahydrogamboic acid, TAM-11, LY 235959, CGS 19755, SK&F 97541, etidronic acid, levonordefrin, methyldopa, ampicillin trihydrate, D-aspartic acid, gamma-D-glutamylaminomethylsulfonic acid, phenazopyridine to hydrochloride, oxalamine citrate salt, podophyllotoxin, SK&F 97541, (+-)-4-amino-3-(5-chloro-2-thienyl)-butanoic acid, (RS)-(tetrazol-5-yl) glycine, R(+)-SKF-81297, gambogic acid, and derivatives thereof.Type: ApplicationFiled: July 23, 2009Publication date: March 25, 2010Inventors: Li-Huei Tsai, Stephen J. Haggarty, Dohoon Kim
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Patent number: 7659311Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: GrantFiled: April 29, 2008Date of Patent: February 9, 2010Assignee: Novartis AGInventors: William Elliott Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Corvino, Moise Azria, Joseph Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph L. Zielinski
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Patent number: 7659428Abstract: There is provided a method for producing easily highly-purified acylphenylalanine that is useful as a raw material of pharmaceutical products and the like, which comprises the step of reacting an acid chloride with phenylalanine in a mixed solvent of an organic solvent and water, while keeping the solvent under the alkali condition by using potassium hydroxide.Type: GrantFiled: December 28, 2005Date of Patent: February 9, 2010Assignee: Ajinomoto Co., Inc.Inventors: Michito Sumikawa, Takao Ohgane
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Publication number: 20100016403Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias. wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.Type: ApplicationFiled: December 14, 2007Publication date: January 21, 2010Inventors: Guy Higgins, Abdelmalik Slassi, Methvin Isaac
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Publication number: 20100009927Abstract: The present invention relates in part to nettle extracts that are useful for treating or preventing seasonal allergies, allergic rhinitis, and other inflammatory conditions.Type: ApplicationFiled: July 14, 2009Publication date: January 14, 2010Applicant: HerbalScience Group LLCInventors: Randall S. Alberte, William P. Roschek, JR., Dan Li
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Publication number: 20090324540Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: ApplicationFiled: June 10, 2009Publication date: December 31, 2009Applicant: Emisphere Technologies, Inc.Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
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Publication number: 20090286781Abstract: The present invention relates to the use of compounds of the formulae I-VI for manufacturing a pharmaceutical for the treatment of acute and chronic lung disorders such as the respiratory distress syndromes [acute lung injury (ALI), acute respiratory distress syndrome (ARDS)] and the treatment of COPD.Type: ApplicationFiled: September 23, 2006Publication date: November 19, 2009Applicant: Bayer HealtHCare AGInventors: Thomas Krahn, Johannes-peter Stasch, Gerrit Weimann, Wolfgang Thielemann
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Publication number: 20090234010Abstract: The present invention relates to a method of preparing N-substituted salicylamides or derivatives thereof and their derivatives, e.g. their salts. In particular, the present invention relates to a method of preparing (N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC) and its corresponding disodium monohydrate.Type: ApplicationFiled: December 14, 2005Publication date: September 17, 2009Inventor: Bernhard Riss
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Publication number: 20090227625Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B, Z and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 17, 2008Publication date: September 10, 2009Applicant: sanofi-aventisInventors: Stephanie HACHTEL, Juergen DEDIO, Elisabeth DeFOSSA, Sven GRUENEBERG, Holger HEITSCH, William BOCK, Charlie CHEN, Raymond KOSLEY, Chung-Yi KUNG, Marcel PATEK, Rosy SHER, Stephen SHIMSHOCK, Aleksandra WEICHSEL
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Publication number: 20090209564Abstract: 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: March 19, 2007Publication date: August 20, 2009Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Ashley Rouse Lins, Jiang Chang, Cangming Yang
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Publication number: 20090209768Abstract: The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.Type: ApplicationFiled: May 14, 2007Publication date: August 20, 2009Inventors: Yasuhiro Saka, Akio Fujii, Kazumi Okuro, Masaru Mitsuda
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Publication number: 20090198051Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.Type: ApplicationFiled: April 25, 2007Publication date: August 6, 2009Inventors: Tohru FUKUYAMA, Toshiyuki KAN
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Patent number: 7569726Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: GrantFiled: April 9, 2008Date of Patent: August 4, 2009Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Roland Burli, Jennifer E. Golden, Kristine M. Muller, Anthony B. Reed
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Publication number: 20090170908Abstract: The Spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereofType: ApplicationFiled: October 24, 2008Publication date: July 2, 2009Applicant: Japan Tobacco Inc.Inventors: Takashi Shimada, Hiroshi Ueno, Kazuhiro Tsutsumi, Kouichi Aoyagi, Tomoyuki Manabe, Shin-Ya Sasaki, Susumu Katoh
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Patent number: 7544833Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid.Type: GrantFiled: August 30, 2007Date of Patent: June 9, 2009Assignees: Hoffmann-La Roche Inc., Emisphere Technologies, Inc.Inventors: William Elliott Bay, Joseph Norman Bernadino, George Frederick Klein, Yi Ren, Pingsheng Zhang
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Patent number: 7544834Abstract: A method for producing B-type crystals of nateglinide substantially free of H-type crystals is provided, which comprises drying solvated wet crystals of nateglinide at a low temperature until no solvent remains and making a crystal conversion thereof. According to this method, B-type crystals of nateglinide can be produced at an industrial scale without allowing other forms of the crystalline polymorphism to coexist.Type: GrantFiled: June 4, 2007Date of Patent: June 9, 2009Assignee: Ajinomoto Co., Inc.Inventors: Michito Sumikawa, Makoto Maruo, Kazuo Miyazaki, Shigehiro Nishina, Yukiko Matsuzawa
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Publication number: 20090118199Abstract: A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].Type: ApplicationFiled: May 11, 2006Publication date: May 7, 2009Applicant: Daiichi Sankyo Company , LimitedInventors: Kazumasa Aoki, Koji Suda, Toshio Kaneko, Tomio Kimura
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Publication number: 20090093483Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: ApplicationFiled: December 17, 2007Publication date: April 9, 2009Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Marian C. Bryan, Roland Burli, Guo-Qiang Cao, Michael J. Frohn, Jennifer E. Golden, Stephanie Mercede, Susana Neira, Tanya Peterkin, Alexander J. Pickrell, Anthony Reed, Christopher M. Tegley, Xiang Wang
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Patent number: 7514471Abstract: The present invention provides the S enantiomer of a compound of formula (I) wherein n is 1 or 2 as well as pharmaceutically acceptable salts, solvates, crystalline forms and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: December 18, 2002Date of Patent: April 7, 2009Assignee: AstraZeneca ABInventors: Eva-Lotte Alstermark Lindstedt, Anna Christina Olsson, Lanna Li
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Publication number: 20090088475Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: April 9, 2008Publication date: April 2, 2009Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Roland Burli, Jennifer E. Golden, Kristine M. Muller, Anthony B. Reed
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Publication number: 20090074691Abstract: This invention relates to certain hydroxyaryl alkanols, alkyl amines, alkyl amino acids, alkyl amino esters, and alkyl amino alkanols (“Hydroxyaryl compounds”) of formula (I). A method of topical application of said hydroxyaryl compounds is also disclosed.Type: ApplicationFiled: November 29, 2008Publication date: March 19, 2009Applicant: BIODERM RESEARCHInventor: SHYAM K. GUPTA