In Same Chain As Carboxyl, Or Salt Thereof Patents (Class 562/443)
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Publication number: 20120010161Abstract: The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.Type: ApplicationFiled: January 25, 2010Publication date: January 12, 2012Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE CLAUDE BERNARD LYON IInventor: Joelle Paris
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Patent number: 8022173Abstract: The present invention herein provides a combination of stable isotope-labeled aliphatic amino acids, which permits the structural analysis of a high molecular weight protein, in particular, a high molecular weight protein whose molecular weight exceeds 60 kDa. This is a combination of stable isotope-labeled amino acids which is characterized in that arginine (Arg), glutamine (Gln), glutamic acid (Glu), lysine (Lys), methionine (Met) and proline (Pro) satisfy the following requirements concerning the labelling pattern: (b) one of the methylene hydrogen atoms of at least one of the methylene groups is deuterated and the both of the two methylene hydrogen atoms of at least one of the methylene groups are likewise deuterated; and (d) when they each have a methyl group, the hydrogen atoms of the methyl group except for one of the same are deuterated, or the methyl group is completely deuterated.Type: GrantFiled: August 26, 2008Date of Patent: September 20, 2011Assignee: Japan Science and Technology AgencyInventors: Masatsune Kainosho, Tsutomu Terauchi
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Publication number: 20110218342Abstract: Disclosed are ?-amino acids that are unsubstituted in the ? position; that are substituted in the ? position with an aryl group; that are substituted in the ? position with an aryl group; that bear two substituents in the ? position; and/or that are substituted in the ? and ? positions with groups which, together with the carbon atoms at the ? and ? positions, form a ring. Also disclosed are methods for making the above-mentioned ?-amino acids and other ?-amino acids which involve providing an ?,?-unsaturated imide; converting the ?,?-unsaturated imide to a 2-substituted-isoxazolidin-5-one; and converting the 2-substituted-isoxazolidin-5-one to a ?-amino acid.Type: ApplicationFiled: July 21, 2004Publication date: September 8, 2011Inventors: Mukund P. Sibi, Craig P. Jasperse, Prabagaran Narayanasamy, Sandeep R. Ghorpade
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Publication number: 20110218200Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.Type: ApplicationFiled: August 28, 2009Publication date: September 8, 2011Inventors: Christopher J. Barden, Michael D. Carter, Mark A. Reed, Donald F. Weaver, Arun Yadav, Shengguo Sun
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Publication number: 20110195936Abstract: 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: December 23, 2010Publication date: August 11, 2011Applicant: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. MacDonald
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Patent number: 7989480Abstract: The present invention relates to a chemical genus of 3-(triaryl)-2-aminopropanol derivative inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention of inflammatory diseases and disorders.Type: GrantFiled: August 3, 2007Date of Patent: August 2, 2011Assignee: Decode Genetics EHFInventors: Vincent Sandanayaka, Jasbir Singh, David Sullins, Mark E. Gurney
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Publication number: 20110178316Abstract: Fullerene compounds represented by the formulae Cm[C(R)CON3]n, Cm[C(R)NCO]n, Cm[C(R)NHCORd]n, and Cm[C(R)NH2]n, wherein Cm represents a fullerene moiety having m carbon atoms, m represents an even integer from about 60 to about 200, n represents an integer of about 1 or more, R represents an electron-withdrawing group, and Rd represents an alkoxy or alkylamino group. In addition, processes for preparing these fullerene compounds involving reacting an acyl azide with a fullerene in the presence of a base.Type: ApplicationFiled: July 28, 2009Publication date: July 21, 2011Applicant: Luna Innovations IncorporatedInventor: Jing Zhang
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Publication number: 20110166380Abstract: The invention provides derivative compounds of N-6-trimethyl-L-lysine (TML) for potential treatment of disorders resulting from deficiencies in the TML-carnitine pathway. The invention also provides a method of purification of TML and TML derivative compounds. The treatment of conditions of the diseases late infantile neuronal ceroid lipofuscinosis (LINCL) and neuronal ceroid lipofuscinosis (NCL) with TML were shown in the original parent application.Type: ApplicationFiled: March 9, 2011Publication date: July 7, 2011Inventors: Suresh C. Srivastava, Sant K. Srivastay, Stanley J. Szymanski, JR.
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Publication number: 20110137000Abstract: The invention relates to a process for preparing a polymeric material doped with metal elements, comprising a step of polymerization of at least one monomer comprising at least one ethylenic function, said monomer being complexed with a metal element. Use of the materials obtained by means of this process as catalysts, or luminescent or magnetic materials, or as elements for laser targets.Type: ApplicationFiled: October 7, 2008Publication date: June 9, 2011Inventors: Balland Longeau Alexia, Moreau Louis, Thibonnet Jérôme, Velasquez Emilie
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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: 20110124865Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds are disclosed.Type: ApplicationFiled: November 18, 2010Publication date: May 26, 2011Inventors: Shinya IIMURA, Wenxue WU, Matthew Mangzhu ZHAO
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Publication number: 20110118353Abstract: The present invention relates to a glycine transporter-1 inhibitor having the formula (I) wherein X is 1-3 substituents selected from H, halogen, methyl, methoxy, trifluoromethyl and trifluoromethoxy and Y is 1-3 substituents selected from H, methyl and halogen or a pharmaceutically acceptable salt thereof for use in a treatment in humans to suppress the level of one or more hormone selected from luteinizing hormone, follicle-stimulating hormone, estradiol and testosterone. The present invention further relates to such a glycine transporter-1 inhibitor as part of a contraceptive regimen or as a treatment for hypersexuality.Type: ApplicationFiled: November 4, 2008Publication date: May 19, 2011Inventors: Robert Gerard Jules Marie Hanssen, Jacques Schipper, Josephus Hubertus Schoemaker
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Publication number: 20110110914Abstract: Methods and formulations for treating oncological disorders in humans using epimetabolic shifters, multidimensional intracellular molecules or environmental influencers are described.Type: ApplicationFiled: May 11, 2010Publication date: May 12, 2011Inventors: Niven Rajin Narain, John Patrick McCook, Rangaprasad Sarangarajan
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Publication number: 20110077396Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.Type: ApplicationFiled: May 21, 2010Publication date: March 31, 2011Applicant: General Electric CompanyInventors: Brian James Grimmond, Michael James Rishel, Michael Todd Luttrell
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Publication number: 20110065905Abstract: A ligand of Formula (I) is provided: wherein A4 represents a hydrogen atom, a nitro group, an amino group, a thiocyanato group, or —Z—Y, in which Z is a divalent linking group and Y is a group derived from a biocompatible molecule, with the proviso that when X is methylene, A4 cannot be a hydrogen atom or a nitro group. A metal complex having the ligand is also provided and is useful as a blood pool contrast agent or a targeting contrast agent.Type: ApplicationFiled: February 8, 2010Publication date: March 17, 2011Applicant: National Chiao Tung UniversityInventors: Yun-Ming Wang, Ting-Jung Chen
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Publication number: 20110004010Abstract: The invention has an object to obtain an organic inorganic composite material having high activity and high selectivity, and suitable as a catalyst material having small elution of an active metal from a carrier, and further to obtain an organosilicon compound suitable for the preparation of the composite material. The composite material is an organic inorganic composite material comprising an organosilicon compound having at least two groups containing reactive silicon at a molecular end, bonded to one silicon atom constituting the organosilicon compound, and an inorganic oxide material, the organosilicon compound and the inorganic oxide material being bonded to each other through a plurality of groups containing reactive silicon of the organosilicon compound. The organosilicon compound is represented by the following general formula (1) or (2). Formula (1) wherein symbols are the same as defined in claim 17. Formula (2) wherein symbols are the same as defined in claim 18.Type: ApplicationFiled: March 5, 2008Publication date: January 6, 2011Applicants: National Instit of Advanced Indust Sci and Tech, N.E. Chemcat CorporationInventors: Shun-ya Onozawa, Norihisa Fukaya, Kaori Saitou, Toshiyasu Sakakura, Hiroyuki Yasuda, Yukio Takagi, Masae Ueda
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Publication number: 20100324319Abstract: New bifunctional chelation complexes are described. These are based on the structure of the so-called “TAME-HexA” molecule. The compounds are especially useful for forming chelation complexes with metal ions, including radioisotopes.Type: ApplicationFiled: July 7, 2010Publication date: December 23, 2010Inventors: Enver ARSLANTAS, Richard R. SCHMIDT, Peter M. SMITH-JONES, Gerd RITTER
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Publication number: 20100319091Abstract: A method of enhancing production of a phenylpropanoid compound in a plant or plant cell is disclosed. The method comprising: (a) expressing in the plant or plant cell a heterologous polynucleotide which produces a myb gene of the phenylpropanoid pathway; and (b) contacting the plant or plant cell with at least one substrate of the phenylpropanoid pathway, the substrate being upstream to the production of the phenylpropanoid compound, thereby enhancing the production of a phenylpropanoid compound in the plant or plant cell.Type: ApplicationFiled: November 13, 2008Publication date: December 16, 2010Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREWInventors: Alexander Vainstein, Michal Moyal-Ben-Zvi, Ben Rimon-Spitzer
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Publication number: 20100298538Abstract: The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D-mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.Type: ApplicationFiled: November 19, 2008Publication date: November 25, 2010Applicant: BCN PÉPTIDES, S.A.Inventors: Llorenç Rafecas Jane, Antonio Riera Escale, Rosario Ramon Albalate, Monica Alonso Xalma
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Publication number: 20100256923Abstract: One embodiment includes a material exhibiting an optical response signature for neutrons that is different than an optical response signature for gamma rays, said material exhibiting performance comparable to or superior to stilbene in terms of distinguishing neutrons from gamma rays, wherein the material is not stilbene. Another embodiment includes a substantially pure crystal exhibiting an optical response signature for neutrons that is different than an optical response signature for gamma rays, the substantially pure crystal comprising a material selected from a group consisting of: 1-1-4-4-tetraphenyl-1-3-butadiene; 2-fluorobiphenyl-4-carboxylic acid; 4-biphenylcarboxylic acid; 9-10-diphenylanthracene; 9-phenylanthracene; 1-3-5-triphenylbenzene; m-terphenyl; bis-MSB; p-terphenyl; diphenylacetylene; 2-5-diphenyoxazole; 4-benzylbiphenyl; biphenyl; 4-methoxybiphenyl; n-phenylanthranilic acid; and 1-4-diphenyl-1-3-butadiene.Type: ApplicationFiled: April 3, 2009Publication date: October 7, 2010Inventors: Stephen A. Payne, Wolfgang Stoeffl, Natalia P. Zaitseva, Nerine J. Cherepy, M. Leslie Carman
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Publication number: 20100234596Abstract: [Problem] The present invention aims to provide a novel organometallic compound that can be used as a general-use highly active catalyst with superior selectivity for functional groups. [Means for Solving Problem] The present invention relates to an organometallic compound having a novel specific structure of general formula (1): and to a general-use highly active catalyst used in reductive amination reaction with superior selectivity for functional groups that comprises said organometallic compound, and to a process for preparing amine compounds by reductive amination reaction using said catalyst.Type: ApplicationFiled: March 12, 2010Publication date: September 16, 2010Applicant: Kanto Kagaku Kabushiki KaishaInventors: Masahito Watanabe, Junichi Hori, Kunihiko Murata
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Patent number: 7777073Abstract: This invention relates to certain hydroxyaryl alkanols, alkyl amines, alkyl amino acids, alkyl amino esters, and alkyl amino alkanols (“Hydroxyaryl compounds”) of formula (I). A method of topical application of said hydroxyaryl compounds is also disclosed.Type: GrantFiled: November 29, 2008Date of Patent: August 17, 2010Assignee: Bioderm ResearchInventor: Shyam K Gupta
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Patent number: 7772426Abstract: Disclosed is a method for efficiently and highly selectively producing L-2-amino-4-(hydroxymethylphosphinyl)-butanoic acid, which is useful as a herbicide, through a catalytic asymmetric synthesis reaction. Specifically disclosed is a method for producing L-2-amino-4-(hydroxymethylphosphinyl)-butanoic acid which is characterized in that a dehydroamino acid is subjected to an asymmetric hydrogenation by using a rhodium catalyst represented by the formula (2) below and having an optically active cyclic phosphine ligand, and then the resulting product is subjected to hydrolysis: [Rh(R4)(L)]X??(2) [where R4 represents 1,5-cyclooctadien or norbornadien; L represents a substance represented by the following formula (6): (wherein R5 and R8 respectively represent a C1-4 alkyl group; R6 and R7 respectively represent hydrogen atom or hydroxyl group; and Y represents a group selected from groups represented by the following formula (7): (where Me represents methyl group)).].Type: GrantFiled: March 28, 2006Date of Patent: August 10, 2010Assignee: Meiji Seika Kaisha, Ltd.Inventors: Nobuto Minowa, Nozomu Nakanishi, Masaaki Mitomi
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Patent number: 7767811Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: June 5, 2006Date of Patent: August 3, 2010Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Patent number: 7750181Abstract: This invention relates to certain dioxodihydropyridine derivatives and certain methacrylic acid and furan derivative precursors thereof, processes for their preparation, pharmaceutical compositions containing such compounds and their use as anti-proliferative agents, especially tumour growth inhibitors and anti-cancer agents, antibiotics and/or antiviral agents.Type: GrantFiled: March 9, 2005Date of Patent: July 6, 2010Assignee: EPX Research LimitedInventors: Washington Odur Ayuko, Michael John Tisdale, Eric Lattmann
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Publication number: 20100160285Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 18, 2009Publication date: June 24, 2010Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20100087539Abstract: The invention relates to the field of organic chemistry and medicine, in particular to virology. More specifically the invention relates to a novel chemical compound N?-{N-[3-oxo-lupan-28-oyl]-9-aminononanoyl}-3-amino-3-phenylpropionic acid of formula 1 and to pharmaceutically acceptable salts and prodrug forms thereof exhibiting an anti-viral (anti-HIV) and immunostimulating activity. A method for producing the compound of formula 1 and the use thereof for the manufacture of a medicinal agent exhibiting an anti-viral (anti-HIV) and immunostimulating activity is also disclosed.Type: ApplicationFiled: October 24, 2007Publication date: April 8, 2010Inventors: Usein Memetovich Dzhemilev, Genrikh Alexandrovich Tolstikov, Andrei Georgievich Pokrovsky, Nariman Faridovich Salakhutdinov, Tatyana Genrikhovna Tolstikova, Elvira Eduardovna Shults
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Publication number: 20100061936Abstract: An unnatural amino acid including a phosphate mimicking group for mimicking a phosphate group in phosphoamino acids and a protein phosphatase modifying group for covalently binding protein phosphatases. A probe for detecting disease including a phosphate mimicking group for mimicking a phosphate group in phosphoamino acids and a protein phosphatase modifying group for covalently binding protein phosphatases. A method for detecting the presence of disease by administering the unnatural amino acid, binding the unnatural amino acid with a phosphatase, detecting a signal, and detecting the presence of disease. A method of identifying a known protein phosphatase, and a method of identifying an unknown protein phosphatase. A method of making the unnatural amino acid.Type: ApplicationFiled: September 1, 2009Publication date: March 11, 2010Inventor: Kui Shen
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Publication number: 20100036132Abstract: The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestinal disorders.Type: ApplicationFiled: October 16, 2009Publication date: February 11, 2010Inventors: Chaozhong Cai, Wei He
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Patent number: 7659428Abstract: There is provided a method for producing easily highly-purified acylphenylalanine that is useful as a raw material of pharmaceutical products and the like, which comprises the step of reacting an acid chloride with phenylalanine in a mixed solvent of an organic solvent and water, while keeping the solvent under the alkali condition by using potassium hydroxide.Type: GrantFiled: December 28, 2005Date of Patent: February 9, 2010Assignee: Ajinomoto Co., Inc.Inventors: Michito Sumikawa, Takao Ohgane
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Publication number: 20100022394Abstract: The present invention consists on the synthesis of new products for the treatment of the iron chlorosis. These products may have improved properties regarding the currently known treatments. The new products are non-symmetrical ethylene diamino hidroxyphenyl acetic acid derivatives possessing only five coordination sites able to chelate metals.Type: ApplicationFiled: December 20, 2007Publication date: January 28, 2010Applicant: TRADECORP, S.A.Inventors: Miguel A. Sierra, Mar Gomez-Gallego, Juan J. Lucena, Sonia Garcia-Marco, Rosa Escudero
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Publication number: 20100004336Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.Type: ApplicationFiled: August 29, 2008Publication date: January 7, 2010Applicant: SHIRE LLCInventors: Travis Mickle, Suma Krishnan, Barney Bishop, Christopher Lauderback, James Scott Moncrief, Robert Oberlender, Thomas Piccariello, Bernhard J. Paul, Christopher A. Verbicky
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Publication number: 20090306340Abstract: The present invention provides: a method for purifying an oligopeptide, which comprises a step of contacting a solution comprising the oligopeptide and a neutral amino acid with an ion exchange resin in an effective pH range; the method for purifying an oligopeptide, which comprises (a) a step of passing a solution comprising the oligopeptide and the neutral amino acid through a column packed with an ion exchange resin, and (b) a step of eluting the oligopeptide contacted with the ion exchange resin with an eluting solvent; the above method using a weakly acidic cation exchange resin; the above method using a weakly basic anion exchange resin, etc.Type: ApplicationFiled: June 28, 2007Publication date: December 10, 2009Applicant: KYOWA HAKKO BIO CO., LTD.Inventors: Shizuo Tsuchiya, Tetsuo Nishimura, Toshikatsu Shindo
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Patent number: 7622499Abstract: The present invention relates to photosensitive derivatives of optically active L-threo-?-benzyloxyaspartate or its benzene ring-substituted analogs, represented by the following formula (1) or (2): (1) (2) wherein R1 represents hydrogen atom, amino group, straight or branched lower aliphatic acylamino group optionally substituted at the acyl group portion, alicyclic acylamino group or aromatic acylamino group optionally having a substituent on the aromatic ring, R2 represents hydrogen atom or one or more straight or branched optionally substituted lower aliphatic alkyloxy groups on the benzene ring, R3 represents hydrogen atom, methyl group or carboxyl group, and R4 and R5 each represent hydrogen atom, hydroxyl group, straight or branched lower alkyloxy group optionally substituted at the alkyl portion, amino group, straight or branched lower alkyl-substituted amino group, or a halogen atom, which upon photoirradiation can produce compounds exhibiting a function of suppressing the glutamate uptake activity oType: GrantFiled: May 30, 2003Date of Patent: November 24, 2009Assignee: Suntory Holdings LimitedInventors: Keiko Shimamoto, Kiyo Takaoka
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Publication number: 20090240029Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one heterocycle, aldol-based, dicarbonyl, and/or diamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one heterocycle, aldol-based, dicarbonyl, and/or diamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: December 27, 2006Publication date: September 24, 2009Applicant: AMBRX, INC.Inventors: Zhenwei Miao, Junjie Liu
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Publication number: 20090221573Abstract: The present invention relates to a method for promoting wound healing by administering one or more compounds identified in the claims, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: July 6, 2006Publication date: September 3, 2009Applicant: Bayer HealthCare AGInventors: Thomas Krahn, Johannes-Peter Stasch, Gerrit Weimann, Wolfgang Thielemann, Beatrix Stelte-Ludwig
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Publication number: 20090209768Abstract: The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.Type: ApplicationFiled: May 14, 2007Publication date: August 20, 2009Inventors: Yasuhiro Saka, Akio Fujii, Kazumi Okuro, Masaru Mitsuda
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Publication number: 20090197315Abstract: 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: ApplicationFiled: January 14, 2005Publication date: August 6, 2009Applicant: William Marsh Rice UniversityInventors: Andrew R. Barron, Jianzhong Yang
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Publication number: 20090105328Abstract: An Amino Acid Compound is described. The Amino Acid Compound may comprise an Amino Acid and one of a Nitrate and a Nitrite. The Amino Acid may be one of Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, and Phenylalanine.Type: ApplicationFiled: December 17, 2008Publication date: April 23, 2009Inventors: Ronald Kramer, Alexander Nikolaidis
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Patent number: 7514471Abstract: The present invention provides the S enantiomer of a compound of formula (I) wherein n is 1 or 2 as well as pharmaceutically acceptable salts, solvates, crystalline forms and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: December 18, 2002Date of Patent: April 7, 2009Assignee: AstraZeneca ABInventors: Eva-Lotte Alstermark Lindstedt, Anna Christina Olsson, Lanna Li
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Patent number: 7501538Abstract: This invention provides aryl and heteroaryl compounds of Formula (I) as described herein, and methods of their preparation. Also provided are pharmaceutical compositions made with the compounds of Formula (I) and methods for making such compositions. The compounds of Formula (I) may activate an erythropoietin receptor and thus, may be useful to induce red blood cell production. The compounds of Formula (I) and compositions including compounds of Formula (I) may be useful in a variety of applications including the management, treatment and/or control of diseases caused at least in part by deficient (or inefficient) EPO production relative to hemoglobin level.Type: GrantFiled: August 6, 2004Date of Patent: March 10, 2009Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Guoxiang Huang, Murty N. Arimilli, Thomas Scott Yokum, Jeff Jiqun Zhu, Muralidhar Bondlela
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Patent number: 7485742Abstract: A new class of non-glycosidic and non-peptidic inhibitors of selectins with low molecular weight according to the general formula 1 is described, as well as methods for their production. These compounds represent a new class of non-toxic, in vivo anti-inflammatory effective inhibitors of selectins, and do not exhibit the disadvantages of the glycosidic inhibitor complexes, and are furthermore more potent in vitro, compared to the known drug bimosiamose. Furthermore, medicaments containing the compounds and their uses in the treatment of diseases are described.Type: GrantFiled: July 26, 2005Date of Patent: February 3, 2009Assignee: Johannes Gutenberg-Universität MainzInventors: Gerd Dannhardt, Holger Ulbrich, Philip Prech, Andreas Luxenburger
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Publication number: 20080317670Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one aromatic amine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one alkylated amine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: December 13, 2006Publication date: December 25, 2008Applicant: Ambrx, Inc.Inventors: Zhenwei Miao, Junjie Liu, Thea Norman
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Publication number: 20080280982Abstract: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: ApplicationFiled: November 14, 2006Publication date: November 13, 2008Inventors: Jianke Li, Guoxin Zhu
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Publication number: 20080268519Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: October 26, 2007Publication date: October 30, 2008Applicant: AMBRX, INC.Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
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Publication number: 20080268518Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: October 26, 2007Publication date: October 30, 2008Applicant: AMBRX, INC.Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
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Patent number: 7423172Abstract: Compounds of general formula I, and the salts and solvates thereof, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH2)s—N(COR3)-A-J-T or —(CH2)s—N(R4)—B-J-T; and s. R3, R4, A, B, J and T have the meanings disclosed in the description. These compounds are PPAR? modulators and, therefore, are useful for the treatment or prevention of a condition or a disease mediated by these receptors.Type: GrantFiled: July 29, 2005Date of Patent: September 9, 2008Assignee: Laboratorios Salvat, S.A.Inventors: Carmen Serra Comas, Anna Fernández Serrat, Dolors Balsa López, Isabel Masip Masip, Juan Lorenzo Catena Ruiz, José Hidalgo Rodriguez, Carmen Lagunas Arnal, Carolina Salcedo Roca, Andrés Fernández García
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Publication number: 20080194459Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one aromatic amine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one alkylated amine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: October 26, 2007Publication date: August 14, 2008Applicant: AMBRX, INC.Inventors: Zhenwei Miao, Junjie Liu, Thea Norman
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Publication number: 20080182968Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: October 17, 2007Publication date: July 31, 2008Applicant: AMBRX, INC.Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
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Publication number: 20080182969Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: December 7, 2007Publication date: July 31, 2008Applicant: AMBRX, INC.Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER