Oxy In Acid Moiety Patents (Class 560/39)
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Patent number: 8519175Abstract: 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: GrantFiled: October 8, 2012Date of Patent: August 27, 2013Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Publication number: 20130217874Abstract: Disclosed embodiments concern a method for making substantial quantities of desired macrocycles. Disclosed ring closing reactions make the macrocycle with desired olefin geometry in excellent yield and E/Z ratio. Particular embodiments of the current method concern intermediates that are obtained from commercially available starting materials in a small number of steps, thereby illustrating the commercial importance and applicability of the disclosed method. The macrocycle produced by the ring closing reaction can be further derivatized to provide analogs of the macrocyclic compounds.Type: ApplicationFiled: November 1, 2011Publication date: August 22, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Thilo J. Heckrodt, Rajinder Singh
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Patent number: 8501809Abstract: The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 8, 2010Date of Patent: August 6, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Sumihiro Nomura, Mikiko Tsukimoto, Toshiyuki Kume, Ila Sircar
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Publication number: 20130190397Abstract: Disclosed is a compound having an acceleration effect on the secretion of human ?-defensin, LL-37, which is a human-derived anti-microbial peptide, a method for preparing same, and a composition for accelerating the secretion of anti-microbial peptide having same as an active ingredient, and the compound and the composition using same of the present invention enhance the anti-microbial effect and the immunity control effect that the anti-microbial peptide has in the body by accelerating the secretion of the anti-microbial peptide in the body.Type: ApplicationFiled: February 27, 2013Publication date: July 25, 2013Applicant: NEOPHARM CO., LTD.Inventor: Neopharm Co., Ltd.
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Patent number: 8481044Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: February 16, 2012Date of Patent: July 9, 2013Assignee: Theravance, Inc.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
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Patent number: 8471054Abstract: The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.Type: GrantFiled: March 7, 2012Date of Patent: June 25, 2013Assignee: Tyrx, Inc.Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
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Publication number: 20130143926Abstract: The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.Type: ApplicationFiled: June 10, 2011Publication date: June 6, 2013Inventors: Alastair David Graham Donald, Joanne McDermott, Sanjay Ratilal Patel, David Festus Charles Moffat
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Patent number: 8435562Abstract: Pharmaceutical compositions and oral dosage forms of (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and methods of treating diseases comprising orally administering such pharmaceutical compositions and dosage forms are disclosed.Type: GrantFiled: November 8, 2010Date of Patent: May 7, 2013Assignee: XenoPort, Inc.Inventors: Chen Mao, Nikhil Pargaonkar, Laura E. Maurer, Sarina Grace Harris Ma
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Publication number: 20130109639Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: November 1, 2012Publication date: May 2, 2013Inventors: Adam D. HUGHES, Erik FENSTER, Melissa FLEURY, Roland GENDRON
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Publication number: 20130102649Abstract: Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.Type: ApplicationFiled: October 16, 2012Publication date: April 25, 2013Applicant: BioTheryX, Inc.Inventor: BioTheryX, Inc.
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Publication number: 20130090493Abstract: This invention relates to a “one pot” process for the preparation of isoserine derivatives in high diastereoselective way. The process according to the invention includes the steps of reacting a protected glycidic acid with imines to yield isoserines protected both at the —OH and at the —COOH groups, deprotection of the obtained intermediates to isoserines or isoserine 1-4C— alkyl esters. Pure threo derivatives as the main isomer are obtained.Type: ApplicationFiled: April 13, 2011Publication date: April 11, 2013Applicant: INDENA S.P.AInventors: Gabriele Fontana, Maria Luisa Gelmi, Federico Gassa
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Publication number: 20130072438Abstract: Disclosed herein are opioid peptide conjugates (for example, opioid peptide esters). In some embodiments, the disclosed conjugates include an opioid peptide consisting of two to six amino acids and a moiety conjugated to the opioid peptide by an ester bond. In some examples, the moiety is an alcohol, a sugar, a lipid, or dehydroascorbic acid. Also disclosed are methods of altering nociception including administering an effective amount of one or more disclosed opioid peptide conjugates to a subject (such as a human subject).Type: ApplicationFiled: September 13, 2012Publication date: March 21, 2013Inventor: Joel S. Goldberg
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Patent number: 8399513Abstract: Crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate, hydrate, methods of making the hydrate, pharmaceutical compositions containing the hydrate, and methods of using the hydrate to treat diseases or disorders such as Parkinson's disease are provided.Type: GrantFiled: October 19, 2009Date of Patent: March 19, 2013Assignee: XenoPort, Inc.Inventors: Sami Karaborni, Manshiu Leung, Chen Mao, Venkat Thalladi
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Publication number: 20130059998Abstract: Amino acid-based poly(ester amide) (PEA) macromers (e.g., functional PEA macromers) and methods for preparing amino acid-based poly(ester amide) (PEA) macromers. The functional PEA macromers can comprise functional groups such as hydroxyl, amine, sulfonic acids, carboxyl, thiol and acryloyl at the two terminuses of the PEA macromers. The content of the terminal functional groups on the macromers can be precisely controlled by adjusting the molar ratio of reactive monomers. The resulting versatility of these new functional PEA macromers can be used to fabricate a wide range of PEAs and PEA hybrid derivatives with very different chemical, physical, mechanical, thermal and biological properties. The functional PEA macromers can also be polycondensed into forming block PEA polymers.Type: ApplicationFiled: March 9, 2011Publication date: March 7, 2013Inventors: Chih-Chang Chu, Mingxiao Deng
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Patent number: 8389769Abstract: A polymerizable Type II photoinitiator according to Formula (I): wherein: A represents a Norrish Type II initiating group; L represents a divalent linking group positioning the Norrish Type II initiating group A and the CR2R3-group in a 1-5 to a 1-8 position wherein position 1 is defined as the first atom in the aromatic or alicyclic ring of A to which L is covalently bonded and the position 5 to 8 is defined as the carbon atom of the CR2R3-group to which L is covalently bonded, with the proviso that L does not contain an amine. Radiation curable compositions and inks include the multifunctional Type II photoinitiator.Type: GrantFiled: May 28, 2009Date of Patent: March 5, 2013Assignee: Agfa Graphics NVInventors: Johan Loccufier, Jaymes Van Luppen
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Patent number: 8367108Abstract: The present invention relates to compound of formula I, which are functionalized, non-phenolic 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: GrantFiled: August 29, 2007Date of Patent: February 5, 2013Assignee: Bezwada Biomedical, LLCInventor: Rao S. Bezwada
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Publication number: 20130030061Abstract: 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: ApplicationFiled: October 8, 2012Publication date: January 31, 2013Applicant: BEZWADA BIOMEDICAL, LLCInventor: BEZWADA BIOMEDICAL, LLC
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Patent number: 8350076Abstract: The present invention is directed to novel phenyloin derivative compounds and the use of such compounds as sodium channel blockers. Such compositions have utility as anti-cancer agents and can be used to limit or prevent PCa growth and/or metastasis.Type: GrantFiled: September 11, 2008Date of Patent: January 8, 2013Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Patent number: 8338478Abstract: The invention concerns novel derivatives of 3,3-diphenyl-propylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.Type: GrantFiled: June 15, 2011Date of Patent: December 25, 2012Assignee: UCB Pharma GmbHInventors: Claus Meese, Bengt Sparf
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Publication number: 20120322066Abstract: This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.Type: ApplicationFiled: June 8, 2012Publication date: December 20, 2012Applicant: Life Technologies CorporationInventors: Parul Angrish, Zhiwei Yang, Jonathan Wang
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Publication number: 20120308588Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20120302719Abstract: New bioresorbable polymers are synthesized from monomer analogs of natural metabolites In particular, polymers are polymerized from analogs of amino acids that contribute advantageous synthesis, processing and material properties to the polymers prepared therefrom, including particularly advantageous degradation profilesType: ApplicationFiled: May 29, 2012Publication date: November 29, 2012Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Joachim B. Kohn, Durgadas Bolikal
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Publication number: 20120296109Abstract: (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Applicant: XenoPort, Inc.Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
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Patent number: 8309754Abstract: 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: GrantFiled: December 24, 2011Date of Patent: November 13, 2012Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Patent number: 8309610Abstract: This invention relates to solid crystalline forms of (1RS,3RS,6RS)-6-Dimethylaminomethyl-1-(3-methoxy-phenyl)cyclohexane-1,3-diol hydrochloride (1), methods of producing 1, methods of use of 1, use of 1 as analgesics and pharmaceutical compositions comprising 1.Type: GrantFiled: February 21, 2006Date of Patent: November 13, 2012Assignee: Gruenenthal GmbHInventors: Michael Gruss, Helmut Buschmann, Andreas Fischer, Wolfgang Hell, Dagmar Lischke
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Publication number: 20120277310Abstract: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.Type: ApplicationFiled: June 25, 2012Publication date: November 1, 2012Applicants: Bar-Ilan University, Ramot at Tel-Aviv University Ltd.Inventors: Gideon STEIN, Abraham NUDELMAN, Ada REPHAELI, Irit GIL-AD, Abraham WEIZMAN
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Patent number: 8293948Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.Type: GrantFiled: January 9, 2012Date of Patent: October 23, 2012Assignee: Jitsubo Co., Ltd.Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono
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Publication number: 20120258063Abstract: An object is to provide an external preparation for skin preferably usable to prevent or ameliorate pigmentation. The object is achieved by providing a preventing or ameliorating agent for pigmentation, consisting of a compound represented by the following general formula (1), an isomer thereof, and/or a pharmacologically acceptable salt thereof, and an external preparation for skin containing the same as a component: [wherein R1 represents an unsubstituted aromatic group or an aromatic group having any substituent; R2 represents a hydrogen atom, a linear chain or branched chain alkyl group having a number of carbon atom or atoms of 1 to 4, or an acyl group having a linear or branched alkyl chain having a number of carbon atom or atoms of 1 to 4; and R3 represents a hydrogen atom or a linear chain or branched chain alkyl group having a number of carbon atom or atoms of 1 to 4.Type: ApplicationFiled: December 16, 2010Publication date: October 11, 2012Applicant: Pola Chemical Industries Inc.Inventors: Yuko Saitoh, Chihiro Kondo, Takashi Yamasaki
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Publication number: 20120238740Abstract: The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vector in a nucleophilic reaction which offers a convenient and time-saving way to purify the product from non-reacted precursors vector-LM and by-products LM.Type: ApplicationFiled: July 6, 2010Publication date: September 20, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Keith Graham, Mathias Berndt, Dae Yoon Chi, Byoung Se Lee, Sandip S. Shinde, Hee Seup Kil, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
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Patent number: 8247603Abstract: 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: GrantFiled: February 16, 2007Date of Patent: August 21, 2012Assignee: Birds Pharma GmbH Berolina InnovativeInventors: Rudolf-Giesbert Alken, Frank Schneider
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Publication number: 20120190816Abstract: The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR8, where R8 is C1-6 alkyl, C6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC (O)— occurs without racemisation. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.Type: ApplicationFiled: July 20, 2011Publication date: July 26, 2012Inventors: Laurence M. Harwood, Ran Yan
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Publication number: 20120190649Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: BIOGEN IDEC MA INC.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Publication number: 20120189713Abstract: The invention relates to novel monomers of Formula (I) useful for preparation of phase-separated biocompatible polymers or polymer compositions. These polymers or polymer compositions may be bioresorbable and/or biodegradable and have desirable mechanical properties, such as fracture and/or fatigue toughness, which have not been a primary design criteria for such polymers previously. The polymers or polymer compositions are useful in a variety of medical applications, such as in the fabrication of medical devices. Therefore, methods for preparing these polymers or polymer compositions and medical devices are also encompassed by this disclosure.Type: ApplicationFiled: July 31, 2010Publication date: July 26, 2012Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Joachim B. Kohn, Durgadas Bolikal, Ramiro Rojas
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Publication number: 20120178957Abstract: The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin.Type: ApplicationFiled: September 25, 2010Publication date: July 12, 2012Inventors: Guoliang Zhu, Jian Zhang, Lljun Yang, Qingdan Yao, Jie Ying
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Publication number: 20120165495Abstract: The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.Type: ApplicationFiled: March 7, 2012Publication date: June 28, 2012Applicant: TYRX, Inc.Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
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Publication number: 20120157386Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Applicant: THERAVANCE, INC.Inventors: Cameron SMITH, Melissa FLEURY, Roland GENDRON, Ryan HUDSON, Adam D. HUGHES
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Publication number: 20120157383Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Applicant: THERAVANCE, INC.Inventors: Roland GENDRON, Melissa FLEURY, Adam D. HUGHES
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Publication number: 20120157544Abstract: The present invention relates to a compound of formula A, wherein R is alkyl. Compound A may be used as an intermediate in the preparation of O-desmethyl venlafaxine or a salt thereof, and the present invention provides such a preparation, as well as a process for preparing the compound of formula A.Type: ApplicationFiled: July 14, 2010Publication date: June 21, 2012Applicant: CIPLA LIMITEDInventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Manohar Raghunath Surve
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Publication number: 20120135523Abstract: The present invention is directed to polyarylates comprising repeating units having the structure: as well as their preparation and use as cell growth substrates.Type: ApplicationFiled: January 30, 2012Publication date: May 31, 2012Applicant: Rutgers, The State University of New JerseyInventors: Ken James, Brochini Stephen, Varawut Tangpasuthadol, Joachim B. Kohn
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Patent number: 8178675Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed as Formula (I).Type: GrantFiled: November 9, 2006Date of Patent: May 15, 2012Assignee: Wellstat Therapeutics CorporationInventors: Fedor Evgenievich Romantsev, Shalini Sharma, Reid W. von Borstel, Stephen D. Wolpe
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Patent number: 8168820Abstract: 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: GrantFiled: December 18, 2003Date of Patent: May 1, 2012Assignee: BDD Berolina Drug Development GmbHInventor: Rudolf-Giesbert Alken
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Patent number: 8153801Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: GrantFiled: September 11, 2008Date of Patent: April 10, 2012Assignee: Gilead Sciences, Inc.Inventors: Eric Dowdy, Steven Pfeiffer
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Patent number: 8153837Abstract: The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.Type: GrantFiled: November 3, 2006Date of Patent: April 10, 2012Assignee: TYRX, Inc.Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
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Publication number: 20120052110Abstract: Provided herein are compositions and methods that inhibit expression of Adam12 gene products, such as ADAM12 mRNA and/or ADAM12 polypeptides, as a therapeutic approach for the treatment of, or promotion of healing of, wounds.Type: ApplicationFiled: August 4, 2011Publication date: March 1, 2012Applicant: Hospital for Special SurgeryInventors: Marjana TOMIC, Carl Peter Blobel, Asheesh Harsha
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Publication number: 20120035226Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: ApplicationFiled: March 29, 2010Publication date: February 9, 2012Applicant: MERCK SERONO SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnés Bombrun
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Publication number: 20110312875Abstract: The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.Type: ApplicationFiled: August 2, 2011Publication date: December 22, 2011Applicant: UNIVERSITY OF WOLLONGONGInventors: Timothy Patrick Boyle, John Barnard Bremner, Zinka Brkic, Jonathan Alan Victor Coates, Neal Kevin Dalton, John Deadman, Paul Anthony Keller, Jody Morgan, Stephen Geoffrey Pyne, David Ian Rhodes, Mark James Robertson
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Publication number: 20110313154Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.Type: ApplicationFiled: August 26, 2011Publication date: December 22, 2011Applicant: AJINOMOTO CO., INC.Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
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Patent number: 8063105Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.Type: GrantFiled: July 20, 2006Date of Patent: November 22, 2011Assignee: Merck Canada Inc.Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
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Publication number: 20110275782Abstract: New bioresorbable polymers are synthesized from monomer analogs of natural metabolites In particular, polymers are polymerized from analogs of amino acids that contribute advantageous synthesis, processing and material properties to the polymers prepared therefrom, including particularly advantageous degradation profilesType: ApplicationFiled: September 16, 2009Publication date: November 10, 2011Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Joachim B. Kohn, Durgadas Bolikal
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Publication number: 20110275784Abstract: The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR8, where R8 is C1-6 alkyl, C6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC (O)— occurs without racemisation. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.Type: ApplicationFiled: July 20, 2011Publication date: November 10, 2011Inventors: Laurence M. Harwood, Ran Yan