Amide Patents (Class 562/450)
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Publication number: 20130071863Abstract: The present invention provides a method of measuring an endogenous low-molecular-weight compound specifically and conveniently with high sensitivity. Using the particular sulfur-containing amino acid derivative, a method of measuring an endogenous low-molecular-weight compound specifically and conveniently with high sensitivity can be provided.Type: ApplicationFiled: November 16, 2012Publication date: March 21, 2013Applicant: AJINOMOTO CO., INC.Inventor: AJINOMOTO CO., INC.
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Publication number: 20130059799Abstract: The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.Type: ApplicationFiled: May 2, 2011Publication date: March 7, 2013Inventors: Liping Liu, Lawrence Gu
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Publication number: 20130053543Abstract: A peptide clearing agent is provided for clearance of a conjugate of an enzyme and a binding molecule which binds specifically at a target location from a non-target location in a subject. The peptide clearing agent binds the active site of the enzyme. The peptide also binds to the asialoglycoprotein receptor expressed by hepatic cells to facilitate clearance through the liver. The peptide may be glycosylated to facilitate clearance through the liver by binding to hepatic cells expressing an asialoglyco-protein receptor. Typically, the peptide prevents or inhibits enzyme activity upon binding to the enzyme and is not substantially modified by the enzyme activity. The peptide may be based upon the dipeptide amino-naphthoic acid (ANA)-glutamate (GIu) and may comprise the amino acid sequence serine (Ser)-Alanine (Ala)-amino-naphthoic acid (ANA)-glutamate (GIu). In such cases, the enzyme of interest is typically CPG2.Type: ApplicationFiled: September 23, 2010Publication date: February 28, 2013Applicant: MOLOGIC LTDInventors: Paul James Davis, James Alexander Schouten
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Publication number: 20130012728Abstract: Provided herein are processes for the preparation of N-acylated amines. In particular, the processes comprise contacting an amine with an acid comprising a carboxylic acid group to form the N-acylated amine.Type: ApplicationFiled: March 9, 2011Publication date: January 10, 2013Applicant: NOVUS INTERNATIONAL INC.Inventors: Richard Vonder Embse, Michael Hayes, James C. Peterson
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Patent number: 8344177Abstract: The invention relates to portable albumin binders, which are useful for improving the pharmacokinetic properties of diagnostic or therapeutic agents, in particular increasing the blood circulations time and/or the tissue penetration capacity of such agents.Type: GrantFiled: November 2, 2007Date of Patent: January 1, 2013Assignee: Philochem AGInventors: Dario Neri, Christoph Dumelln
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Publication number: 20120329716Abstract: The instant invention relates to peptides obtained from the enzymatic hydrolysis of yellow pea seed proteins that are capable of lowering the blood pressure and reducing the effects of kidney disease in a subject b\ inhibiting or reducing the affinity of the enzymes in the renin-angiotensin system for their substrates, specifically renin, to compositions comprising said peptides and to uses thereof.Type: ApplicationFiled: October 28, 2010Publication date: December 27, 2012Inventors: Rotimi Aluko, Jianping Wu, Harold Aukema
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Publication number: 20120328514Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.Type: ApplicationFiled: July 8, 2010Publication date: December 27, 2012Applicant: Lantheus Medical Imaging, Inc.Inventors: Richard R. Cesati, Thomas D. Harris, Simon P. Robinson, Richard J. Looby, Edward H. Cheesman, Padmaja Yalamanchili, David S. Casebier
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Publication number: 20120309674Abstract: The invention relates to compounds, in particular MMP inhibitors. The compounds of the invention have formula (1). The invention can be used in particular in the pharmaceutical field. The present invention also relates to labeled compounds of formula (2), and to the use thereof as contrast agents for detecting extracellular matrix metalloproteinases.Type: ApplicationFiled: August 26, 2010Publication date: December 6, 2012Applicant: Commissariat A L'Energie Atomique ET Aux Ene AltInventors: Laurent Devel, Fabrice Beau, Bertrand Czarny, Vincent Dive
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Publication number: 20120295943Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: August 20, 2009Publication date: November 22, 2012Inventors: Shinji Marumoto, Toyoki Nishimata, Masayuki Ebisawa, Yusuke Asoh, Yasuo Fukushima, Mikio Kato
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Patent number: 8309766Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.Type: GrantFiled: March 24, 2006Date of Patent: November 13, 2012Assignee: Obschestvo S. Organichennoi Otvetstvennostiyu PharmenterprisesInventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina, Violetta Leonidovna Kovaleva
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Publication number: 20120270813Abstract: A process for producing a peptide product having cholecystokinin secretion promoting effect, said process comprising hydrolyzing soybean residues with one or more proteases so that the peptide product having cholecystokinin secretion promoting effect is obtained. Also disclosed is the composition containing the peptide product and the use thereof.Type: ApplicationFiled: October 5, 2011Publication date: October 25, 2012Applicant: Food Industry Research and Development InstituteInventors: Yi-Hong Chen, Yu-Hui Liu, Chu-Chin Chen, Shiao-Cheng Chuang, Hsiang-Ling Lai, Chien-Ti Chang, Ming-Yu Hung, Su-Er Liou, Fu-Ning Chien
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Patent number: 8293943Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: February 18, 2012Date of Patent: October 23, 2012Assignee: Island Kinetics, Inc.Inventors: Shyam K Gupta, Linda Walker
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Patent number: 8288368Abstract: (R)-2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of the chemotaxis of neutrophils and monocytes induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes.Type: GrantFiled: February 25, 2002Date of Patent: October 16, 2012Assignee: Dompé Pha.R.Ma S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Valerio Berdini, Cinzia Bizzarri, Maria Candida Cesta, Vito Di Cioccio, Gianfranco Caselli, Fracesco Colotta, Carmelo Gandolfi, Janete Peloia Barroso Gandolfi, legal representative, Giulio Agostino Gandolfi, legal representative, Maria Carla Gandolfi, legal representative, Arrigo Aldo Gandolfi, legal representative
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Publication number: 20120252830Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 7, 2012Publication date: October 4, 2012Applicant: NOVARTIS AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Patent number: 8263658Abstract: Compounds of formula (I) are provided, wherein X is CH?CH, CH2O wherein the oxygen atom is bound to ring B, or OCH2 wherein the oxygen atom is bound to ring A; Y is hydrogen, straight or branched C1-C6 alkyl or a pharmaceutically acceptable inorganic cation; R1 is ethyl or cyclopropyl; and R2 and R3 are the same or different and are selected from F, Cl, Br, CF3 and OCF3. The compounds are useful for the treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection, and malignant neoplasia. Pharmaceutical compositions comprising the compounds, methods of using the compounds, and methods for preparing the compounds are also provided.Type: GrantFiled: August 4, 2009Date of Patent: September 11, 2012Assignee: Chelsea Therapeutics, Inc.Inventors: Helén Tuvesson Andersson, Ulf Vellmar, Ingrid Hallin, Leif Svenson, Ingela Fritzson
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Patent number: 8258343Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: February 15, 2012Date of Patent: September 4, 2012Assignee: Island Kinetics, Inc.Inventors: Shyam K Gupta, Linda Walker
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Patent number: 8217137Abstract: The present invention is directed to a series of new compounds, combining the unique properties of fullerenes and bio-active amino acid residues, and to methods for making such compounds. The present invention is directed toward fullerene-based amino acids, and to amino acid residues, peptide chains, proteins, and polypeptides made from such fullerene-based amino acids. The present invention is further directed to amino acid residues, peptide chains, proteins, and polypeptides comprising such fullerene-based amino acids and into which such fullerene-based amino acids have been incorporated. Exemplary compounds have been prepared, and these compounds have been characterized and confirmed with infrared (IR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry (MS), etc.Type: GrantFiled: January 14, 2005Date of Patent: July 10, 2012Assignee: William Marsh Rice UniversityInventors: Andrew R. Barron, Jianzhong Yang
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Patent number: 8212076Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: April 12, 2011Date of Patent: July 3, 2012Assignee: Covalence, Inc.Inventors: Shyam K Gupta, Linda Walker
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Patent number: 8207227Abstract: 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-C16alkylene, 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: March 22, 2011Date of Patent: June 26, 2012Assignees: Emisphere Technologies, Inc., Novartis AGInventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Michael M. Goldberg, Joanne P. Corvino, Shingai Majuru, Moise Azria, Joseph Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph Zielinski
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Publication number: 20120149736Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)O—, —C(?O)NR?—, —C(?5)—NR?, —C(?NH)NR? or —S(?O)2NR — wherein R? is hydrogen or optionally substituted C1—C6 alkyl; L1 is a divalent radical of formula —(Alk1)m,(Q)n(Alk2)p— wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—,— NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1Type: ApplicationFiled: February 25, 2010Publication date: June 14, 2012Applicant: Chroma Therapeutics Ltd.Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
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Publication number: 20120120551Abstract: A method of fabricating a device is disclosed. The method comprises coating a solid structure by nanostructures selected from the group consisting of peptides and amino acids, under conditions that at least partially prevent assembly of the nanostructures into supramolecular structures.Type: ApplicationFiled: November 16, 2011Publication date: May 17, 2012Applicant: Ramot at Tel-Aviv University LtdInventors: Peter BEKER, Gil Rosenman
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Publication number: 20120122764Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.Type: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Applicant: NOVARTIS AGInventors: Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Qian LIU, Muneto MOGI, Nikolaus SCHIERING, Robert SUN
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Publication number: 20120122941Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: August 20, 2009Publication date: May 17, 2012Inventors: Shinji Marumoto, Toyoki Nishimata, Masayuki Ebisawa, Yusuke Asoh, Yasuo Fukushima, Mikio Kato
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Publication number: 20120108632Abstract: The invention concerns in one embodiment a method of treating glaucoma or elevated intraocular pressure comprising administering a pharmaceutically effective amount of a composition comprising at least one prenyltransferase inhibitor. In another embodiment, the invention concerns a composition for the treatment of elevated intraocular pressure and glaucoma comprising a pharmaceutically effective amount of a prenyltransferase inhibitor.Type: ApplicationFiled: January 5, 2012Publication date: May 3, 2012Applicant: ALCON RESEARCH, LTD.Inventors: Allan R. Shepard, Debra L. Fleenor
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Publication number: 20120053243Abstract: To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for external use having these capabilities. There are provide a parakeratosis inhibitor and a pore reducing agent each comprising at least one compound selected from the group consisting of a glycine derivative, an aminodicarboxylic acid derivative, an acylaminodicarboxylic acid derivative, a pyrrolidinecarboxylic acid derivative, a piperidinecarboxylic acid derivative, a hexamethyleneiminecarboxylic acid, a beta-alanine derivative and salts of these derivatives.Type: ApplicationFiled: November 7, 2011Publication date: March 1, 2012Applicant: SHISEIDO COMPANY, LTD.Inventors: Mikiko Kaminuma, Masaru Suetsugu, Toshii Iida, Shinji Inomata, Keiko Takada, Yuji Katsuta
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Publication number: 20120016151Abstract: The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.Type: ApplicationFiled: January 12, 2010Publication date: January 19, 2012Inventors: Guoliang Zhu, Lijun Yang, Ying Lin, Jie Ying
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Patent number: 8076374Abstract: 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: GrantFiled: November 10, 2006Date of Patent: December 13, 2011Assignee: Eli Lilly and CompanyInventors: Mark Donald Chappell, Scott Eugene Conner, Philip Arthur Hipskind, Jason Eric Lamar, Guoxin Zhu
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Publication number: 20110288239Abstract: The present invention discloses a polymeric polyamine which can be produced by polymerizing polyoxyalkylene-amine and a linker. The linker can be anhydride, carboxylic acid, epoxy, isocyanate or poly(styrene-co-maleic anhydride) copolymers (SMA). The present invention also discloses a method for stabilizing the Ag nanoparticles with polymeric polyamine. The polymeric polyamine serving as a stabilizer or dispersant is mixed with a water solution of silver salt and then a reducer is provided to reduce the silver ions and form an organic or a water solution of Ag nanoparticles. Water or solvent of this solution can be further removed through a heating, freezing or decompression process, and thus solid content of the solution can be increased. The concentrated solution also can be diluted to obtain a stable dispersion without aggregation.Type: ApplicationFiled: August 1, 2011Publication date: November 24, 2011Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Jiang-Jen Lin, Wei-Cheng Tsai, Yen-Chi Hsu, Wen-Hsin Chang
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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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Patent number: 8026392Abstract: The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same.Type: GrantFiled: September 18, 2006Date of Patent: September 27, 2011Assignee: Emisphere Technologies, Inc.Inventors: Nikhil Dhoot, Steven Dinh, Shingai Majuru, William Elliott Bay, JoAnne P. Corvino, Doris C. O'Toole
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Publication number: 20110229940Abstract: The present invention relates to a method for producing an L-amino acid by reacting an enantiomeric mixture of an N-succinyl amino acid with L-succinylase in the presence of N-acylamino acid racemase to specifically hydrolyze the L-form. In particular, the present invention relates to a method for producing an L-amino acid in high yield by using an N-succinyl amino acid whose dissolved concentration is particularly low as a raw material to perform a reaction while precipitating the produced L-amino acid out of the reaction system. The present invention enables efficient production of an L-amino acid having high optical purity, particularly an L-amino acid useful as a raw material for products such as pharmaceutical products and agricultural chemicals.Type: ApplicationFiled: October 28, 2009Publication date: September 22, 2011Applicant: KANEKA CORPORATIONInventors: Masutoshi Nojiri, Tozo Nishiyama, Naoaki Taoka
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Patent number: 8013184Abstract: 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: GrantFiled: December 14, 2005Date of Patent: September 6, 2011Assignee: Novartis AGInventor: Bernhard Riss
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Publication number: 20110213157Abstract: A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH2)3— or —(CH2)4—, X represents —N(R2)—CO— (R2 represents hydrogen atom or a C1-6 alkyl group), —CO—N(R3)— (R3 represents hydrogen atom or a C1-6 alkyl group), —C(R4)?C(R5)— (R4 and R5 represent hydrogen atom or a C1-6 alkyl group), or —N(R6)—SO2— (R6 represents hydrogen atom or a C1-6 alkyl group), and Ar represents an aryldiyl group or a heteroaryldiyl group], which has a retinoid action and is useful as an active ingredient of a medicament.Type: ApplicationFiled: August 14, 2008Publication date: September 1, 2011Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Yohei Amano, Masayuki Noguchi, Koichi Shudo
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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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Patent number: 8003819Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: February 12, 2010Date of Patent: August 23, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Edward J. Olhava, Mihaela Diana Danca
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Patent number: 7998933Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.Type: GrantFiled: July 26, 2010Date of Patent: August 16, 2011Assignee: L'Oreal S.A.Inventors: Maria Dalko, Yann Mahe, Lionel Breton
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Patent number: 7977506Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: November 8, 2006Date of Patent: July 12, 2011Assignee: Emisphere Technologies, Inc.Inventors: Maria Aurora P. Boyd, Andrea Leone-Bay, Doris C. O'Toole
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Publication number: 20110130587Abstract: Disclosed is a process for preparing single enantiomers of beta-amino phenylbutyric acid derivatives and pharmaceutically acceptable salts thereof, which affords the desired compounds having special optical configuration. The process comprises a step of chemical synthesis and a step of resolving the optical isomers of beta-amino phenylbutyric acid derivatives with a resolving agent. The resolving step comprises reacting the optical isomers with resolving agents, such as di-para-toluoyl-L-tartaric acid and di-para-toluoyl-D-tartaric acid. The obtained R-beta-amino phenylbutyric acid derivatives (I) have high optical purity, and the total yield of the accumulative resolution of the laevo and the dextro isomer is up to above 70%.Type: ApplicationFiled: April 14, 2009Publication date: June 2, 2011Applicant: Jiangsu Hengrui Medicine Co., Ltd.Inventors: Piaoyang Sun, Yongjiang Chen, Guangliang Yu
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Publication number: 20110118482Abstract: Compounds of the formula (I), in the form of mixtures comprising predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1 (I) in which Z1 is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals, or Z1 is the —P*R0R1 group; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton, and in which base skeletons a secondary phosphine group Z1 is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group, and in which base skeletons a P-chiral group —P*R0R1 is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group to a carbon atom such that the phosphorus atoms are linked via 1 to 7 atoms of a carbon chain optionally iType: ApplicationFiled: November 14, 2008Publication date: May 19, 2011Inventors: Benoît Pugin, Matthias Lotz, Heidi Landert, Adrian Wyss, Raphael Aardoom, Bjõrn Gschwend, Andreas Pfaltz, Felix Spindler
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Patent number: 7939666Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers.Type: GrantFiled: May 4, 2006Date of Patent: May 10, 2011Assignee: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Publication number: 20110092733Abstract: Nateglinide M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2?)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble.Type: ApplicationFiled: December 15, 2010Publication date: April 21, 2011Applicant: Ajinomoto Co., Inc.Inventors: Yoshihito KOGUCHI, Tomoko NAKAO, Michito SUMIKAWA
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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: 20110064673Abstract: The present invention relates to fluorinated glutamic acid (glutamate) and glutamine derivatives wherein the fluorine atom is 19F. The glutamic acid (glutamate) and glutamine derivatives are compound(s) of general Formula I, which encompasses all possible diastereoisomers and/or enantiomere derivatives or mixtures thereof.Type: ApplicationFiled: May 14, 2009Publication date: March 17, 2011Inventors: Ludger Dinkelborg, Heribert Schmitt-Willich, Keith Graham, Norman Koglin, Mathias Berndt, Matthias Friebe, Andre Muller
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Publication number: 20110065681Abstract: Compounds are provided according to formula 1: where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: ApplicationFiled: February 27, 2009Publication date: March 17, 2011Inventors: Zhi-Liang Wei, Sumithra Gowlugari, Carl Kaub, Zhan Wang, Yeyu Cao, John Kincaid
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Publication number: 20110046397Abstract: The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.Type: ApplicationFiled: January 16, 2009Publication date: February 24, 2011Inventors: David Hook, Bernhard Riss, Daniel Kaufmann, Matthias Napp, Erhard Bappert, Phillippe Polleux, Jonathan Medlock, Antonio Zanotti-Gerosa
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Patent number: 7893297Abstract: The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.Type: GrantFiled: July 2, 2008Date of Patent: February 22, 2011Assignee: Emisphere Technologies, Inc.Inventors: Satej Bhandarkar, Shingai Majuru, Halina Leuchyk
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Publication number: 20110039933Abstract: The invention provides compounds formula (I), their preparation, and their use as pharmaceutically active immuno-suppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 7, 2007Publication date: February 17, 2011Applicant: PRAECIS PHARMACEUTICALS INCORPORATIONInventors: Ghotas Evindar, Hongfeng Deng
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Patent number: 7863329Abstract: 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: GrantFiled: November 14, 2006Date of Patent: January 4, 2011Assignee: Eli Lilly and CompanyInventors: Jianke Li, Guoxin Zhu
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Publication number: 20100331552Abstract: The present invention relates to an acid salt of tolterodine with superior stabililty and useful as a transdermal drug delivery system. More specifically, the present invention relates to a novel acid salt of tolterodine with superior stabililty to the conventional acid salts of tolterodine, which is useful as a pharmaceutical composition for the treatment of overactive bladder and can be formulated into a transdermal drug delivery system.Type: ApplicationFiled: February 20, 2009Publication date: December 30, 2010Applicant: SK Chemicals Co., Ltd.Inventors: Yong Youn Hwang, Nam Ho Kim, Won Jae Choi, Yong Han Kim
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Patent number: 7858665Abstract: The present invention relates to nitrooxyderivatives or salts thereof having the following general formula (I): R—NR1c—(K)k0—(B)b0—(C)c0—NO2??(I) wherein c0, b0 and k0 are 0 or 1; R is the radical of an analgesic drug for chronic pain, for instance neurophatic pain; R1c is H or alkyl with from 1 to 5 carbon atoms; B is such that its precursor is selected from amino acids, hydroxy acids, polyalcohol, compounds; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: GrantFiled: June 2, 2009Date of Patent: December 28, 2010Assignee: Nicox S.A.Inventors: Ennio Ongini, Nicoletta Almirante, Piero Del Soldato