The Nitrogen Is Not Bonded Directly To A Ring Patents (Class 560/37)
  • Patent number: 9434696
    Abstract: The disclosure relates to a process for the preparation of the enantiomeric forms of 2,3-diaminopropionic acid derivatives of formula I, wherein R1, R2 and R3 are defined as in the disclosure, by racemate resolution. The separation of the racemate into its enantiomers takes place through formation of diastereomeric salts upon addition of an enantiomerically pure auxiliary, and subsequent separation by fractional crystallization.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: September 6, 2016
    Assignee: Sanofi
    Inventors: Claus-Dieter Graf, Joerg Rieke-Zapp
  • Patent number: 9382194
    Abstract: The invention discloses a improved process for the preparation of 3,5-disubstituted-2,4,6-triiodo aromatic amines of formula (II), wherein R1 and R2 are defined as herein. The compounds of formula (II) are the key intermediates for the synthesis of a series of non-ionic contrast agents such as Iopamidol, Iohexol and Iodixanol. The process comprises reacting chlorine-free iodinating reagents with 3,5-disubstituted-2,4,6-triiodo aromatic amines to obtain 3,5-disubstituted-2,4,6-triiodo aromatic amines of formula (II), wherein the molar yield of the iodination reaction can reach to 89%.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: July 5, 2016
    Assignee: IMAX Diagnostic Imaging Holding Limited
    Inventors: Hongdeng Xing, Lei Li, Zhiqi Hu
  • Publication number: 20150119251
    Abstract: Provided is an agricultural plant-protecting agent including a dipeptide derivative or an agro-pharmaceutically acceptable salt thereof as an active ingredient, which has a plant disease-preventing effect, a plant growth-promoting effect, and a plant immunity-activating effect.
    Type: Application
    Filed: April 18, 2013
    Publication date: April 30, 2015
    Inventors: Kyung Seok Park, Jin Woo Park, Se Won Lee, Surk Sik Moon, In Seok Hong
  • Publication number: 20150065711
    Abstract: Disclosed are linear discrete PEG constructs, which can be created and produced in a precise and reproducible way. Key to being able to do these things, where x in the discrete PEGx can vary from about 2 to about 64, is that the processes used to make each linear portion is controlled to give essentially one oligomer/one compound. Having a variable length linear discrete PEG construct that is (a) primarily an linear discrete PEG construct with diagnostic or therapeutic groups attached along a chain of attachment cores, which is attached to a preferential locator; (b) is an m-discrete PEG as the terminal construct on the linear portion, and “hidden”; (c or linear discrete PEG with a terminus group that can be either negatively or positively charged, or neutral; and any of the discrete PEG portions can be designed to be cleaved after entering the cell.
    Type: Application
    Filed: August 15, 2014
    Publication date: March 5, 2015
    Applicant: EquIP, LLC
    Inventor: Paul D. Davis
  • Publication number: 20140228591
    Abstract: The invention relates to the use of a substituted, chiral amino alcohol, comprising one or more structural units of the following formula (1), wherein the abbreviations A, Y, R1 and R3 to R5 have the following meanings: is a covalent bond or a hydrocarbon group, Y is a covalent bond or a hydrocarbon group that can have an oxygen atom at one of its ends through which it is bonded to R1, R1 is an aliphatic or heterocyclic or aromatic radical, the carbon chain of which may be interrupted by one or more B groups, R5 is selected from the group consisting of (a) aliphatic radicals, wherein individual carbon atoms may be replaced by oxygen atoms or carbonyl groups, and wherein the carbon chains of same radicals may be optionally interrupted by a B group, and (b) araliphatic, cycloaliphatic, aromatic and heterocyclic radicals, wherein the carbon chain can be interrupted by one or more B structural elements and/or by one or more D coupling groups, R3, R4 are hydrogen or aliphatic or araliphatic substituents, which are
    Type: Application
    Filed: October 10, 2012
    Publication date: August 14, 2014
    Applicant: Fraunhofer-Gesellschaft zur Förderung der Angewandten Forschung E.V.
    Inventors: Monika Bauer, Lutz Hartmann, Frank Kuschel, Wolfgang Weissflog
  • Patent number: 8791260
    Abstract: The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: July 29, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Kley, Daniel Haerle, Guenter Linz, Sandra Stehle
  • Patent number: 8722921
    Abstract: The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding ?-acyloxy sulfides.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: May 13, 2014
    Assignee: ScinoPharm Singapore PTE, Ltd.
    Inventors: JyhHsiung Liao, LungHuang Kuo
  • Patent number: 8691869
    Abstract: The present invention relates to a pharmaceutical formulation comprising: a) one or more NO-releasing NSAID(s) of formula (I); b) one or more surfactants; c) a carbonyl scavenger compound selected from free acid forms, salts, carboxylic acid esters derivatives of a compound of formula (II) H2N—(CH2)m—(C6H4)—COOH??(II) wherein m=0-10; and d) optionally an oil or semi-solid fat and/or a short-chain alcohol.
    Type: Grant
    Filed: June 29, 2006
    Date of Patent: April 8, 2014
    Assignee: Nicox S.A.
    Inventors: Ulla Gasslander, Christina Holmberg
  • Patent number: 8664426
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: March 4, 2014
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Publication number: 20140045936
    Abstract: The disclosure relates to cyclopropyl derivatives and methods of use. In some embodiments, the disclosure relates to methods of managing medical disorders with pharmaceutical compositions disclosed herein administered to subject in need thereof. In certain embodiments, the disclosure relates to methods of managing mental disorders, mood disorders, pain, and fibromyalgia and related conditions with pharmaceutical compositions disclosed herein.
    Type: Application
    Filed: April 13, 2012
    Publication date: February 13, 2014
    Applicants: WAKE FOREST UNIVERSITY HEALTH SCIENCES, EMORY UNIVERSITY
    Inventors: Huw M. Davies, Spandan Chennamadhavuni, Thomas J. Martin, Steven R. Childrens
  • Publication number: 20140039189
    Abstract: The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: October 7, 2013
    Publication date: February 6, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Joerg KLEY, Daniel HAERLE, Guenter LINZ, Sandra STEHLE
  • Publication number: 20140031545
    Abstract: Processes for making an organozinc reagents are disclosed comprising reacting (A) organomagnesium or organozinc complexes with (B) at least one coordination compound comprising one or more carboxylate groups and/or alcoholate groups and/or tertiary amine groups, optionally in combination with zinc ions and/or lithium ions and/or halide ions, wherein the halide ions are selected from chloride, bromide and iodide, the organozinc complex comprises an aryl group, a heteroaryl group or a benzyl group when the coordinating compound is a chelating polyamine, and the reaction is conducted in the presence of zinc complexed with at least one coordinating compound when reactant (A) comprises at least one organomagnesium complex. The resulting organozinc reagents may optionally be isolated from solvents to obtain a solid reagent. The reagents may be used for making organic compounds via Negishi cross-coupling reactions or via aldehyde and/or ketone oxidative addition reactions.
    Type: Application
    Filed: December 21, 2011
    Publication date: January 30, 2014
    Applicant: LUDWIG-MAXIMILIAN-UNIVERSITAT MUNCHEN
    Inventors: Paul Knochel, Sebastian Bernhardt, Georg Manolikakes
  • Publication number: 20140031368
    Abstract: This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 30, 2014
    Applicants: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Ronald Breslow, Paul A. Marks, K. G. Abhilash, Jianing Wang
  • Publication number: 20130281705
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Application
    Filed: June 18, 2013
    Publication date: October 24, 2013
    Inventor: Shalini SHARMA
  • Patent number: 8563714
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Patent number: 8563765
    Abstract: Provided is an efficient technology for synthesizing diamino acids (diamino acid derivatives). Disclosed is a manufacturing method for diamino acid derivatives wherein the fluorenyl groups of the diamino acid derivative starting materials represented by General Formula [II] or [IV] are removed.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: October 22, 2013
    Assignee: Japan Science and Technology Agency
    Inventors: Shu Kobayashi, Yasuhiro Yamashita, Kazutaka Seki
  • Publication number: 20130245133
    Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
    Type: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Applicant: BEZWADA BIOMEDICAL, LLC.
    Inventor: Rao S. BEZWADA
  • Patent number: 8530270
    Abstract: An amic acid or amic ester precursor can be applied to a substrate and thermally converted into a semiconducting layer of the corresponding arylene diimide. This semiconducting thin film can be used in various articles including thin-film transistor devices that can be incorporated into a variety of electronic devices. In this manner, the arylene diimide need not be coated but is generated in situ from a solvent-soluble, easily coated precursor compound.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: September 10, 2013
    Assignee: Eastman Kodak Company
    Inventors: Deepak Shukla, Dianne M. Meyer, Wendy G. Ahearn
  • Patent number: 8519175
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: October 8, 2012
    Date of Patent: August 27, 2013
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Patent number: 8507714
    Abstract: A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.
    Type: Grant
    Filed: January 4, 2011
    Date of Patent: August 13, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsuyoshi Muto, Taisaku Tanaka, Hiroshi Maruoka, Seiichi Imajo, Yoshiaki Tomimori
  • Publication number: 20130189287
    Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 25, 2013
    Applicants: Innate Pharma
    Inventors: Innate Pharma, Paul Scherrer Institut
  • Patent number: 8486999
    Abstract: [PROBLEMS TO BE SOLVED] It is an object of the present invention to provide a gelator containing a long chain oxyaminopolyol capable of forming a gel with a small amount thereof over a liquid property range from acidic to alkaline, and a gel having high environmental suitability, biocompatibility and biodegradability. [MEANS FOR SOLVING THE PROBLEMS] A gelator, characterized by containing a long chain oxyaminopolyol of Formula (I): (where R1 is a C12-16 saturated aliphatic group or a C12-16 unsaturated aliphatic group having one double bond; R2 is a substituent which an amino acid has; and X is an oxygen atom or NH) and a pharmaceutically acceptable salt thereof; a self-assembly formed by the self-assembly of the gelator; and a gel containing the gelator or the self-assembly, and water, an aqueous solution, a hydrophilic organic solvent or a hydrophilic organic solution, or a hydrophobic organic solvent or a hydrophobic organic solution.
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: July 16, 2013
    Assignee: Nissan Chemical Industries, Ltd.
    Inventor: Tatsuo Maruyama
  • Patent number: 8461371
    Abstract: The present invention relates to a method of enantioselective addition to imines, including: reacting R3CH?NY with R4ZnR5 in the presence of a compound represented by the following formula (I), in which Y, R1, R2, R3, R4 and R5 are defined the same as the specification. Accordingly, the present invention can prepare secondary amines in high yields and enantiomeric excess by the above-mentioned method.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: June 11, 2013
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Wei-Ming Huang
  • Patent number: 8440716
    Abstract: The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: May 14, 2013
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: Weiping Tang, James Elliot Bradner, Stuart L. Schreiber
  • Patent number: 8314265
    Abstract: Novel amic acids and amic esters can be thermally converted into corresponding arylene diimides. These amic acids and amic ester can be used as precursors to prepare semiconducting thin films that can be used in various articles including thin-film transistor devices that can be incorporated into a variety of electronic devices. In this manner, the arylene diimides need not be coated out of solvent in which they may be insoluble, but they can be generated in situ from a solvent-soluble, easily coated amic acid or amic ester.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: November 20, 2012
    Assignee: Eastman Kodak Company
    Inventors: Deepak Shukla, Dianne M. Meyer, Wendy G. Ahearn
  • Patent number: 8309754
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: December 24, 2011
    Date of Patent: November 13, 2012
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Publication number: 20120260825
    Abstract: Dispersants for pigments as well as dispersions containing them, and compositions such as inks and coatings containing them are described. The dispersants are the reaction product of at least one dianhydride with at least two different reactants, each of which can be an amine, alcohol, or thiol, and at least one of which is polymeric.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 18, 2012
    Inventors: Tatiana N. ROMANOVA, Russell J. SCHWARTZ
  • Patent number: 8288530
    Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: October 16, 2012
    Assignee: The United States of America, as represented by the Department of Health and Human Services
    Inventors: Martin W. Brechbiel, Heng Xu
  • Publication number: 20120251461
    Abstract: The present invention pertains generally to the field of coolants and medical therapy. More particularly, the present invention relates to certain anti-nociceptive agents, such as [((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-acetic acid isopropyl ester, that are potent and long-acting and selectively cooling for non-keratinized epithelial tissues as compared to keratinized epithelial tissues, and are useful, for example, for the treatment of (e.g., the alleviation of symptoms of; the amelioration of) sensory discomfort of non-keratinized stratified epithelial (NKSE) tissue; and so for treatment of: sensory discomfort of an ocular surface, an eyelid, a margin of an eyelid, an anterior part of an eyeball, a conjunctiva, a lachrymal system, a pre-corneal film, or a cornea, a lining of the oral cavity, an internal portion of the lips, a pharyngeal surface, an esophageal surface, or an anogenital surface; eye discomfort, e.g.
    Type: Application
    Filed: April 4, 2011
    Publication date: October 4, 2012
    Inventor: Edward T. Wei
  • Patent number: 8252923
    Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: August 28, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
  • Patent number: 8247603
    Abstract: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically acceptable salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: August 21, 2012
    Assignee: Birds Pharma GmbH Berolina Innovative
    Inventors: Rudolf-Giesbert Alken, Frank Schneider
  • Patent number: 8217076
    Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: July 10, 2012
    Assignees: Colorado State University Research Foundation, Dana-Farber Cancer Institute
    Inventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk
  • Patent number: 8211878
    Abstract: The present invention provides methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death in a patient. The invention includes use of 5-benzylamino salicylic acid (BAS) and its derivatives. Thus, the present invention provides methods for reducing neuronal death in nervous system injuries resulting from amyotrophic lateral sclerosis.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: July 3, 2012
    Assignee: Neurotech Pharmaceuticals Co., Ltd.
    Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
  • Publication number: 20120138506
    Abstract: The invention relates a pharmaceutical composition comprising a combination of (i) the AT 1-antagonist valsartan or a pharmaceutically acceptable salt thereof and (ii) a NEP inhibitor or a pharmaceutically acceptable salt thereof and optionally a pharmaceutically acceptable carrier and to a method for the treatment or prevention of selected conditions or diseases.
    Type: Application
    Filed: December 16, 2011
    Publication date: June 7, 2012
    Inventors: Gary Michael Ksander, Randy Lee Webb
  • Patent number: 8168820
    Abstract: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically compatible salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: May 1, 2012
    Assignee: BDD Berolina Drug Development GmbH
    Inventor: Rudolf-Giesbert Alken
  • Publication number: 20120101184
    Abstract: Presently described are curable compositions comprising a mixture of at least one (e.g. free-radically) polymerizable ionic liquid and at least one other ethylenically unsaturated monomer, oligomer, or polymer. The polymerizable ionic liquid is characterized as having an air to nitrogen curing exotherm ratio of at least 0.70. Also described are articles and methods of making articles from such curable compositions. A monofunctional polymerizable ionic liquid is also described comprising a non-polymerizable substituted imidazolium cationic group and a polymerizable sulfonate anion.
    Type: Application
    Filed: August 26, 2010
    Publication date: April 26, 2012
    Inventors: Yizhong Wang, Joel D. Oxman, Larry R. Krepski, Peiwang Zhu, Kevin M. Lewandowski, Brian N. Holmes, Richard L. Severance, Joseph D. Rule, Thomas P. Klun
  • Publication number: 20120064002
    Abstract: Enantiomer-pure compounds of general formulas VIIa and VIIb in which A stands for a group —COO—, and Z and R have different meanings, as well as use thereof are described.
    Type: Application
    Filed: March 31, 2011
    Publication date: March 15, 2012
    Inventors: Lutz LEHMANN, Matthias FRIEBE, Thomas BRUMBY, Detlev SUELZLE, Johannes PLATZEK
  • Patent number: 8124802
    Abstract: The invention provides novel N-benzyl-N-propargyl-amines that are monoamine oxidase inhibitors, but generally exhibit little or no CNS effects.
    Type: Grant
    Filed: January 25, 2008
    Date of Patent: February 28, 2012
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • Patent number: 8106231
    Abstract: A process for the enantioselective preparation of (2R,3S)-3-phenylisoserine methyl ester acetate salt of formula (I) which is an useful building block for the synthesis of taxane derivatives. The process involves the resolution of racemic threo-phenylisoserine amide and its conversion into (I).
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: January 31, 2012
    Assignee: Indena S.p.A.
    Inventors: Daniele Ciceri, Bruno Gabetta, Nicola Vignola, Frieder Mitzel, Beat T. Weber
  • Patent number: 8093420
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: January 10, 2012
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S. Bezwada
  • Patent number: 8093291
    Abstract: Methods and compositions comprising tryptophan hydroxylase inhibitors are disclosed. Particular methods are directed at reducing or avoiding serotonin-mediated adverse effects associated with some drugs.
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: January 10, 2012
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Philip Manton Brown, Qingyun Liu
  • Publication number: 20120004441
    Abstract: The present invention relates to a method of enantioselective addition to imines, including: reacting R3CH?NY with R4ZnR5 in the presence of a compound represented by the following formula (I), in which Y, R1, R2, R3, R4 and R5 are defined the same as the specification. Accordingly, the present invention can prepare secondary amines in high yields and enantiomeric excess by the above-mentioned method.
    Type: Application
    Filed: October 6, 2010
    Publication date: January 5, 2012
    Inventors: Biing-Jiun UANG, Wei-Ming Huang
  • Patent number: 8053590
    Abstract: The invention relates to a method for producing enantiomers form of 2,3-diaminopropionic acid derivatives of formula (I) by asymmetric hydrogenation from compounds of formula (II).
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: November 8, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Joerg Rieke-Zapp, Guenter Billen
  • Publication number: 20110269966
    Abstract: An amic acid or amic ester precursor can be applied to a substrate and thermally converted into a thin organic semiconducting layer of the corresponding arylene diimide. This semiconducting layer can be used in various semiconductive articles such as organic light emitting diode (OLED), photodetector, sensor, logic circuit, memory element, capacitor, photovoltaic (PV) cell, or electronic devices. In this manner, the arylene diimide need not be coated but is generated in situ from a solvent-soluble and easily coated precursor compound.
    Type: Application
    Filed: April 30, 2010
    Publication date: November 3, 2011
    Inventors: Deepak Shukla, Dianne M. Meyer, Wendy G. Ahearn
  • Publication number: 20110223058
    Abstract: Novel compounds generally referred to herein as cationic oligomeric phenylene ethynylenes (OPEs), methods of synthesizing OPEs and various uses for the OPEs are described. The compounds can be synthesized in both symmetrical (S-OPE) and non-symmetrical (N-OPE) forms. Suitable uses include sensor and biocidal applications. Reusable structures incorporating the OPEs that are able to capture and release biological species of interest are also described.
    Type: Application
    Filed: June 26, 2009
    Publication date: September 15, 2011
    Applicant: STC.UNM
    Inventors: David Whitten, Yanli Tang, Zhijun Zhou, Linnea Ista, Motokatsu Ogawa, David Keller, Brett Andrzejewski, Gabriel Lopez, Kirk Schanze
  • Publication number: 20110212943
    Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.
    Type: Application
    Filed: October 14, 2009
    Publication date: September 1, 2011
    Applicant: ORCHID RESEARCH LABORATORIES LIMITED
    Inventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
  • Patent number: 8003083
    Abstract: The present invention is benzilidene malonamide represented by the following formula (1) and salts thereof, an ultraviolet absorbent consisting of said new compound, and an external preparation containing this ultraviolet absorbent. The object of the present invention is to provide a new ultraviolet absorbent that is highly soluble in water, has superior absorption capacity over a wide ultraviolet wavelength range, has no absorption in the visible region, and is also highly stable and safe.
    Type: Grant
    Filed: June 11, 2007
    Date of Patent: August 23, 2011
    Assignee: Shiseido Company, Ltd.
    Inventors: Takuya Hiruma, Masaru Suetsugu
  • Publication number: 20110172303
    Abstract: The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.
    Type: Application
    Filed: July 22, 2009
    Publication date: July 14, 2011
    Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard College
    Inventors: Weiping Tang, James Elliot Bradner, Stuart L. Schreiber
  • Patent number: 7956212
    Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
    Type: Grant
    Filed: February 2, 2009
    Date of Patent: June 7, 2011
    Assignee: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
  • Publication number: 20110124859
    Abstract: The present invention relates to a process for preparing betamimetics of formula 1, wherein n denotes 1 or 2; R1 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R3 denotes hydrogen, C1-4-alkyl, OH, halogen, O—C1-4-alkyl, O—C1-4-alkylene-COOH, O—C1-4-alkylene-COO—C1-4-alkyl.
    Type: Application
    Filed: February 7, 2011
    Publication date: May 26, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thomas KRUEGER, Uwe RIES, Juergen SCHNAUBELT, Werner RALL, Zeno A. LEUTER, Adil DURAN, Rainer SOYKA