Nitrogen Or Halogen In Acid Moiety Patents (Class 560/153)
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Publication number: 20140121202Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: January 6, 2014Publication date: May 1, 2014Applicant: Promentis Pharmaceuticals, Inc.Inventors: Edward M. Johnson, Daniel G. Lawton
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Publication number: 20140037961Abstract: The invention relates to a lock-release method to be applied to biomolecules, such as antibodies, to improve the purification, production, stability and storage of biomolecules. A biomolecule is covalently bound to a polymer support comprising a diketone group so that the biomolecule can be purified, produced and/or stored before being released from the support. The diketone group of the polymer support is a 1,3-ketoester, 1,3-ketothioester or 1,3-ketoamide is a group of Formula (1): R1 is an optionally substituted hydrocarbyl, perhalogenated hydrocarbyl, or a heterocyclyl group; Y is hydrogen, an optionally substituted hydrocarbyl, or a heterocyclyl group; X is —O, —NR2 or —S, wherein the free valence of —O, —NR2 or —S is bonded to the support optionally via a linker; and R2 is hydrogen, an optionally substituted hydrocarbyl, or a heterocyclyl group. The invention also relates to a polymer support comprising the diketone group.Type: ApplicationFiled: April 12, 2012Publication date: February 6, 2014Applicant: ADC BIOTECHNOLOGY LIMITEDInventor: David Evans
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Patent number: 8623919Abstract: A pharmaceutical composition and methods of producing and application of the composition for treating myocardial infarction of a subject are disclosed. The pharmaceutical composition comprises a therapeutically effective amount of at least one synthesized compound selected from the group consisting of SEC, SPC, SBC, SPEC, SAC, SAMC, and SPRC, and a pharmaceutically acceptable carrier.Type: GrantFiled: August 1, 2008Date of Patent: January 7, 2014Assignee: Fudan UniversityInventors: Yizhun Zhu, Qian Wang, Yichun Zhu, Qing Mu
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Publication number: 20130281726Abstract: To provide a method for recovering a precious metal from a solution containing precious metal ions, an extracting agent or adsorbent used therefor, and a back-extracting agent or desorbent. An extracting agent or adsorbent in which precious metal ions are extracted or adsorbed, is brought into contact with a back-extracting agent or desorbent containing a sulfur-containing amino acid derivative represented by the following formula (I): wherein R1 is a methyl group, an ethyl group, a vinyl group, a C3-8 linear, branched or cyclic hydrocarbon group, or a C6-14 aromatic hydrocarbon group, R2's are each independently a hydrogen atom, a methyl group, an ethyl group, a vinyl group, a C3-8 linear, branched or cyclic hydrocarbon group or a C6-14 aromatic hydrocarbon group, and n is 0 or 1, to obtain a solution containing the precious metal ions, which is subjected to a reduction treatment to obtain a precious metal.Type: ApplicationFiled: December 28, 2011Publication date: October 24, 2013Applicant: TOSOH CORPORATIONInventors: Yukinori Suso, Takashi Sakaki
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Publication number: 20130158021Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.Type: ApplicationFiled: October 26, 2012Publication date: June 20, 2013Applicant: Massachusetts Institute of TechnologyInventor: Massachusetts Institute of Technology
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Publication number: 20120197028Abstract: Crosslinked polymers, methods for their preparation and use, are described in which the crosslinked polymers are formed from at least two polymer precursors, one of which is designed, upon degradation of the crosslinked polymer, to release the second polymer precursor in its original, unmodified chemical form.Type: ApplicationFiled: January 31, 2011Publication date: August 2, 2012Applicant: Confluent Surgical, IncInventors: Rachit Ohri, Phillip Blaskovich, Joshua Kennedy, Steven L. Bennett, Arthur Driscoll
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Publication number: 20120178913Abstract: A method for the modification of an amino acid, protein or peptide is disclosed. The method comprises reacting a carbon-carbon double bond-containing compound with an amino acid, a protein or a peptide containing an allyl sulfide group in the presence of a catalyst which promotes olefin metathesis, to form a modified amino acid, protein or peptide. Preferred carbon-carbon double bond-containing compounds include carbohydrates.Type: ApplicationFiled: June 5, 2009Publication date: July 12, 2012Applicant: ISIS INNOVATION LIMITEDInventors: Yuya Angel Lin, Justin Mark Chalker, Benjamin Guy Davis
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Publication number: 20120122793Abstract: S-protected cysteine analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: PROMENTIS PHARMACEUTICALS, INC.Inventors: Edward M. Johnson, Daniel G. Lawton
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Publication number: 20120122792Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: PROMENTIS PHARMACEUTICALS, INC.Inventors: Edward M. Johnson, II, Daniel G. Lawton
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Publication number: 20120101294Abstract: Disclosed is a process for producing a (fluoroalkylthio)acetic acid ester represented by the formula (3) wherein R, R1 and R2 have the same meanings as defined below, which comprises reacting a thioglycolic acid ester represented by the formula (1) wherein R represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, and R1 represents an alkyl group having 1 to 4 carbon atoms, with fluoroolefin represented by the formula (2) wherein R2 represents a fluoroalkyl group having 1 to 5 carbon atoms, in the presence of a radical generator.Type: ApplicationFiled: August 6, 2010Publication date: April 26, 2012Inventors: Masaji Hirota, Hiroyuki Miyazaki, Tadayoshi Itoh
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Publication number: 20120093726Abstract: The invention provides compound which is an 18F-radiolabelled S-propylhomocysteine or a derivative thereof. The compound has an enantiomeric purity of at least about 90%. 18F-radiolabelled S-propylhomocysteine may be made by treating an N-protected ester of a substituted S-propylhomocysteine with a complexed F? salt in the presence of a base to form a protected product and then deprotecting the protected product to form the 18F-radiolabelled S-propylhomocysteine. In this method the N-protected ester has a leaving group on the S-propyl group and has an enantiomeric purity of at least about 90%. The base should be such that it does not cause racemisation of the protected product.Type: ApplicationFiled: March 24, 2009Publication date: April 19, 2012Inventors: Andrew Katsifis, Christopher John Reginald Fookes, Ivan Greguric, Thomas Bourdier
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Patent number: 8153689Abstract: Disclosed are pleuromutilin derivatives of formula (I) and their use in the treatment of diseases mediated by microbes.Type: GrantFiled: October 4, 2011Date of Patent: April 10, 2012Assignee: Nabriva Therapeutics AGInventors: Rosemarie Mang, Werner Heilmayer, Rudolf Badegruber, Dirk B. Strickmann, Rodger Novak, Mathias Ferencic, Atchyuta Rama Chandra Murty Bulusu
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Patent number: 8119689Abstract: Bisacyloxycysteine type conjugates have been found to be useful as adjuvants and/or immunomodulators for prophylactic and/or therapeutic vaccination in the treatment of infectious diseases, inflammatory diseases, autoimmune diseases, tumors, and allergies, as well as in the control of fertility in human or animal populations. The compounds can be administered by system or mucosal routes and are particularly useful as mucosal adjuvants. These compounds can function as active ingredients in pharmaceutical compositions.Type: GrantFiled: November 22, 2006Date of Patent: February 21, 2012Assignee: Helmholtz-Zentrum Fuer Infektionsforschung GmbHInventors: Thomas Ebensen, Michael Morr, Carlos Guzman
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Patent number: 8071643Abstract: A pleuromutilin derivative compound of general formula (I)Type: GrantFiled: March 19, 2008Date of Patent: December 6, 2011Assignee: Nabriva Therapeutics AGInventors: Rosemarie Mang, Werner Heilmayer, Rudolf Badegruber, Dirk B. Strickmann, Rodger Novak, Mathias Ferencic, Atchyuta Rama Chandra Murty Bulusu
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Patent number: 8067467Abstract: The present invention relates to compounds of the formula (I) wherein X1 and X2 independently represent O, NH or S, R1 and R2 are independently selected from the group consisting of a C1-C30 hydrocarbyl group, an amino acid bonded via an amide bond or a peptide bonded via an amide bond each having up to 200 amino acids, the conjugated residue X1 or X2 in this case being NH, and hydrogen, both radicals R1 and R2 preferably not being H, wherein R3 is a residue selected from group consisting of —S—R6, wherein R6 is a C1-C30 hydrocarbyl group, at least one of R1 and R2 not being H when X1 and X2 are oxygen, —S—CH2—CH(NH2)(COOH) (cysteine-S-yl), a homologue or derivative (e.g.Type: GrantFiled: May 3, 2006Date of Patent: November 29, 2011Assignee: Biogen Idec International GmbHInventors: Rajendra Kumar Joshi, Hans-Peter Strebel, Jitka Ulrichová, Thomas J. Schmidt
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Publication number: 20110224156Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: March 8, 2011Publication date: September 15, 2011Inventors: Mark A. Wolf, Keith D. Barnes
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Publication number: 20110065904Abstract: H3LMN series compounds used as radioactive agents for treatment of liver cancer and a manufacturing method thereof are revealed. 2-thioethylamine hydrochloride is reacted with triphenylmethanol for protection of thiol to obtain 2-[(triphenylmethyl)thio]ethylamine. Then obtain N-[2-((triphenylmethyl)thio)ethyl]chloroacetamide by a transamidation reaction between 2-[(triphenylmethyl)thio]ethylamine and chloroactyl chloride. Next produce a amine-amide-thiol ligand-N-[2-((triphenylmethyl)thio)ethyl][2-((triphenylmethyl)thio)ethylamino]acetamide by a substitution reaction of N-[2-((triphenylmethyl)thio)ethyl]chloroacetamide and 2-[(triphenylmethyl)thio]ethylamine. After respective reaction with 1-bromotetradecane, 1-bromohexadecane and ethyl 16-bromohexadecanoate, H3LMN series compounds are obtained. These amine-amide-dithiols quadridentate ligands can react with MO3+ (M=Tc or Re) to produce electrically neutral complexes.Type: ApplicationFiled: September 14, 2009Publication date: March 17, 2011Inventors: Show-Wen Liu, Cheng-Hsien Lin, Tsyh-Lang Lin, Cheng-Fang Hsu
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Publication number: 20100222549Abstract: A dechalcogenative method for the preparation of an allylic sulfide comprises contacting an activated chalcogenide of Formula (I) with a thiol of Formula (II) for a period of time sufficient to form an intermediate of Formula (III), and supplying sufficient activation energy to the intermediate of Formula (III), in a suitable solvent, preferably in the absence of a phosphine or other thiophile, to induce a [2,3]-sigmatropic rearrangement therein to form an allylic sulfide of Formula (IV), with concomitant loss of chalcogen Z, as set forth in the following reaction scheme, wherein X is an activating group selected from the group consisting of CN, S-pyridyl, S-heteroaryl, SO2-aryl, and SO3Y; Y is an alkali metal ion; Z is Se or S; R1, R2, R3, R4, and R5 are each independently H or a hydrocarbon moiety; and R is an organic moiety.Type: ApplicationFiled: April 29, 2008Publication date: September 2, 2010Inventors: David Crich, Maheswaran Karatholuvhu, Venkataramanan Krishnamurthy, Thomas K. Hutton, Franck Brebion, Venkataraman Subramanian
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Publication number: 20100179088Abstract: Cysteine derivatives of formula (I) wherein R1-R7 are as defined in the description, and their use as malodor counteractant. Furthermore, a process of their production and consumer products comprising them are described.Type: ApplicationFiled: June 18, 2008Publication date: July 15, 2010Applicant: Givaudan SAInventors: Felix Flachsmann, Markus Gautschi, Thomas McGee, Richard P. Sgaramella
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Publication number: 20100087526Abstract: Inhibitors of the enzyme prenylated methylated protein methyl esterase (PMPMEase), the last step in the prenylation process for many eukaryotic proteins, having the general structure R1—X-A-B(R2)—Y or R1—X-A(R2)—B—Y, where R1 is preferably a polyisoprenyl group, X is a linking group, Y is a group that promotes affinity interactions to the active site of PMPMEase and imparts hydrolysis resistance to the inhibitor, A and B are bridge atoms, and R2 is a characteristic-providing substituent.Type: ApplicationFiled: April 6, 2009Publication date: April 8, 2010Inventor: Nararius Saah Lamango
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Publication number: 20090156674Abstract: The invention relates to the production of a new salt form of valnemulin, a compound of formula I, which is notable for its good crystallinity in higher purity, its simpler technical usability and improved storage stability.Type: ApplicationFiled: January 26, 2006Publication date: June 18, 2009Inventors: Ingolf Macher, Annett Geissler, Susanne Christine Wieland-Berghausen, Uwe Thomas Schote, Ferenc Jozsef Rakoczi
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Publication number: 20090076289Abstract: The invention provides novel compounds that may be used as intermediates in the preparation of epothilones, epothilone analogs and derivative, as well as new synthetic methods for producing the intermediates and products.Type: ApplicationFiled: May 9, 2008Publication date: March 19, 2009Applicant: Kosan Biosciences IncorporatedInventors: John R. Carney, Yong Li, Hugo Menzella, Ralph C. Reid
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Publication number: 20090042996Abstract: A surfactant of formula 1 (Rf-A)a-Q-([B]k—R)b??Formula 1 wherein a and b are each independently 1 or 2; Rf is a linear or branched perfluoroalkyl radical having from 2 to about 20 carbon atoms, optionally interrupted with at least one oxygen; R is a C1 to C20 linear, branched or cyclic alkyl, or a C6 to C10 aryl; B is —(CH2CHR1O)x—, k is 0 or 1, x is 1 to about 20, A is —(CH2)m[(CHR1CH2O)]s—[(CH2)m(CH)tCHOH(CH2)m]e—, wherein each m is independently 0 to 3, s is 0 to about 30, t is 0 or 1, and e is 0 or 1, R1 is H or CH3, Q is: —OP(O)(O?M+)(O)—, —O—, —S—(CH2)m—C(O)—O—, —SO2—O— —CH2CH2O—C(O)CH2C(OH)(V)CH2C(O)O—; —(CH2CH2O)xCH2CH(OH)—(CH2CH2O)x—(CH2)m—Si[OSi(R2)3]2—, —SO2NR2—, —(CH2CH2O)zC(O)CH(SO3?M+)CH2C(O)(OCH2CH2)z— wherein z is 1 to about 15, or a bond when s is a positive integer, V is —C(O)OR3 and R3 is H, CH3 or Rf; R2 is C1 to C4 alkyl, and M+ is a Group 1 metal or an ammonium (NHxR2y)+ cation wherein x+y=4, and R2 is C1 to C4 alkyl, provided that when Q is —OP(O)(O?M+)(O)— or when Q is —(Type: ApplicationFiled: August 6, 2007Publication date: February 12, 2009Inventors: Charles Kenneth Taylor, Michael Joseph Michalczyk, Erick Jose Acosta
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Publication number: 20090036534Abstract: A pharmaceutical composition and methods of producing and application of the composition for treating myocardial infarction of a subject are disclosed. The pharmaceutical composition comprises a therapeutically effective amount of at least one synthesized compound selected from the group consisting of SEC, SPC, SBC, SPEC, SAC, SAMC, and SPRC, and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 1, 2008Publication date: February 5, 2009Inventors: YIZHUN ZHU, Qian Wang, Yichun Zhu, Qing Mu
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Publication number: 20090017106Abstract: The present invention relates to new adjuvants and the uses in pharmaceutical compositions, like in vaccines. In particular, the present invention provides new conjugates of the bisacyloxycysteine type useful as adjuvants and/or immunomodulators for prophylactic and/or therapeutic vaccination in the treatment of infectious diseases, inflammatory diseases, autoimmune diseases, tumours, allergies as well as for the control of fertility in human or animal populations. The compounds are particularly useful not only as systemic, but preferably as mucosal adjuvants. In addition, the invention relates to its uses as active ingredients in pharmaceutical compositions.Type: ApplicationFiled: November 22, 2006Publication date: January 15, 2009Inventors: Thomas Ebensen, Michael Morr, Carlos Guzman
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Patent number: 7285676Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: GrantFiled: March 21, 2005Date of Patent: October 23, 2007Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda
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Patent number: 7115769Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present invention provides methods of preparing 2-alkylcysteine derivatives. In another embodiment, the method comprises forming a 2-alkylcysteine derivative from a cysteine derivative in the presence of a phase transfer catalyst. In particular, the present invention provides methods for preparing 2-methylcysteine derivatives. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In one aspect, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine. The present invention also relates to the preparation of 4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-alkyl-thiazole-4-carboxylic acids, such as 4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-methyl-thiazole-4-carboxylic acid.Type: GrantFiled: May 15, 2003Date of Patent: October 3, 2006Assignee: Genzyme CorporationInventors: Rayomand H. Gimi, Mukund S. Chorghade
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Patent number: 6972340Abstract: Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.Type: GrantFiled: August 29, 2001Date of Patent: December 6, 2005Assignee: Abbott LaboratoriesInventors: Gang Liu, Bruce G. Szczepankiewicz, Zhonghua Pei, Zhili Xin, David A. Janowick
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Patent number: 6927236Abstract: The present invention relates to compounds of the formula which are formed during fermentation by the microorganism Coniochaeta ellipsoidea Udagawa, DSM 13856, or by one of its mutations and/or variants, and chemically derivatized if appropriate. The invention furthermore relates to a process for preparing compounds of the formula (I), and to their use as pharmaceuticals. In addition, the invention relates to the use of a compound of the formula (VI) for producing a pharmaceutical for the treatment and prophylaxis of degenerative neuropathics or of Alzheimer's disease.Type: GrantFiled: September 19, 2002Date of Patent: August 9, 2005Assignee: Aventis Pharma Deutschland GmbH.Inventors: Laszlo Vertesy, Klaus Ehrlich, Michael Kurz, Marian Paul Segeth, Luigi Toti
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Patent number: 6916850Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.Type: GrantFiled: May 3, 2002Date of Patent: July 12, 2005Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Guy Miller, Wei Zhang
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Patent number: 6903220Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: GrantFiled: May 15, 2003Date of Patent: June 7, 2005Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda
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Patent number: 6878845Abstract: Oligomers from multifunctional acrylates and organonitro compounds are provided. Films obtained from crosslinked oligomers of the present invention are useful as protective or decorative coatings as well as components in adhesives and composites.Type: GrantFiled: October 15, 2002Date of Patent: April 12, 2005Assignee: Ashland Inc.Inventors: Matthew S. Sheridan, Laurence G. Dammann, Sridevi Narayan-Sarathy
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Publication number: 20040235910Abstract: A compound of formula 1Type: ApplicationFiled: June 14, 2004Publication date: November 25, 2004Inventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
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Publication number: 20040186178Abstract: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.Type: ApplicationFiled: April 1, 2004Publication date: September 23, 2004Applicant: Pharmacia CorporationInventors: Ronald Keith Webber, Richard C. Durley, Alok K. Awasthi, Arija A. Bergmanis, Kam F. Fok, Scott S. Ganser, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Brian S. Hickory, Pamela T. Manning, Michael Mao, Alan E. Moormann, Barnett S. Pitzele, Michelle A. Promo, Richard R. Schartman, Jeffrey A. Scholten, Jeffrey S. Snyder, Mihaly V. Toth, Mahima Trivedi, Sofya Tsymabalov, Foe Siong Tjoeng
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Publication number: 20040158095Abstract: The present invention relates to series of compounds with aqueous metal decontamination activity and their uses in removing metals from aqueous media. The compounds are esters of organic acids or alcohols with polyols that contain a sulfhydral group (—SH). The compounds release sulfhydral slowly into the water providing activity over extended periods of time and exhibit biodegradable characteristics. The compounds may be used to remediate aqueous media.Type: ApplicationFiled: February 7, 2003Publication date: August 12, 2004Inventors: William A. Farone, Tracy Palmer
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Patent number: 6770776Abstract: Fluorocarbon compounds are synthesized by reacting a substrate hydrocarbyl compound containing at least one sp3-hybridized halophoric carbon atom bearing at least two halogen atom substituents, at least one of which is a halogen atom having an atomic number greater than that of fluorine and the at least one halophoric carbon atom being bonded to at least one chalcogen, with at least one reactant which comprises a complex of a Bronstedt base with a defined amount n of hydrofluoric acid, n being at least 3 and not greater than 20.Type: GrantFiled: September 25, 2001Date of Patent: August 3, 2004Assignee: Rhone-Poulenc ChimieInventors: Robert Janin, Laurent Saint-Jalmes
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Publication number: 20040122004Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the Formula (I) 1Type: ApplicationFiled: November 17, 2003Publication date: June 24, 2004Applicant: Bayer AktiengesellschaftInventors: Erwin Bischoff, Thomas Krahn, Stephan-Nicholas Muller, Holger Paulsen, Joachim Schuhmacher, Henning Steinhagen, Wolfgang Thielemann
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Patent number: 6747169Abstract: Disclosed is a silver halide photographic light-sensitive material having one or more layers including a light-sensitive silver halide emulsion layer on a support, wherein any of the layers contains the specific fluorine compound. The silver halide photographic light-sensitive material can be stably produced and is imparted with antistatic property.Type: GrantFiled: August 2, 2002Date of Patent: June 8, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Terukazu Yanagi, Akira Ikeda, Nobuo Hamamoto, Takahiro Ishizuka
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Publication number: 20040024224Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: ApplicationFiled: May 15, 2003Publication date: February 5, 2004Applicant: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra
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Patent number: 6586474Abstract: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.Type: GrantFiled: March 23, 2001Date of Patent: July 1, 2003Assignee: Pharmacia CorporationInventors: Ronald Keith Webber, Richard C. Durley, Alok K. Awasthi, Arija A. Bergmanis, Kam F. Fok, Scott S. Ganser, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Brian S. Hickory, Pamela T. Manning, Michael Mao, Alan E. Moormann, Barnett S. Pitzele, Michelle A. Promo, Richard R. Schartman, Jeffrey A. Scholten, Jeffrey S. Snyder, Mihaly V. Toth, Mahima Trivedi, Sofya Tsymbalov, Foe Siong Tjoeng
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Patent number: 6559334Abstract: The invention relates to novel optically active polymerizable dipeptides, to the process for the preparation thereof, to the polymerization thereof and to the use of the polymers as adsorbents for the chromatographic separation of enantiomers.Type: GrantFiled: August 12, 1994Date of Patent: May 6, 2003Assignee: Bayer AktiengesellschaftInventors: Walter Lange, Michael Grosse-Bley, Bruno Bömer, Rolf Grosser, Franz-Peter Hoever
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Publication number: 20030013657Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.Type: ApplicationFiled: May 3, 2002Publication date: January 16, 2003Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani
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Patent number: 6495680Abstract: Helical oligomer and polymer compositions that form nanotubes are described. The compositions comprise a plurality of aromatic substituents linked by at least one amide group. The compositions have a curved backbone due to intramolecular hydrogen bonds that rigidify the amide linkage of each amide group to each aromatic substituent and due to an interaction between the aromatic substituents such that the curved backbone is stabilized. The helical compositions are formed by ridigifying the amide group, which is flanked on each side by the aromatic substituents, by introducing intramolecular hydrogen bonds into a linkage between the amide group and each aromatic substituent such that the compositions fold into a helical shape when the amide linkages are meta to each other.Type: GrantFiled: March 24, 2000Date of Patent: December 17, 2002Assignee: The University of ToledoInventor: Bing Gong
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Publication number: 20020169337Abstract: A process for producing optically active cysteine derivatives with high optical purity and good quality which is economically advantageous and is high in productivity even on a commercial scale is provided.Type: ApplicationFiled: May 13, 2002Publication date: November 14, 2002Applicant: Kaneka CorporationInventors: Yasuyoshi Ueda, Hiroshi Murao, Takeshi Kondo, Noboru Ueyama, Hajime Manabe, Kenji Yoneda, Akira Nishiyama
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Patent number: 6407281Abstract: A process for producing optically active cysteine derivatives with high optical purity and good quality which is economically advantageous and is high in productivity even on a commercial scale is provided.Type: GrantFiled: August 25, 2000Date of Patent: June 18, 2002Assignee: Kaneka CorporationInventors: Yasuyoshi Ueda, Hiroshi Murao, Takeshi Kondo, Noboru Ueyama, Hajime Manabe, Kenji Yoneda, Akira Nishiyama
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Patent number: 6316636Abstract: Fluorocarbon compounds are synthesized by reacting a substrate hydrocarbyl compound containing at least one sp3-hybridized halophoric carbon atom bearing at least two halogen atom substituents, at least one of which is a halogen atom having an atomic number greater than that of fluorine and the at least one halophoric carbon atom being bonded to at least one chalcogen, with at least one reactant which comprises a complex of a Bronstedt base with a defined amount n of hydrofluoric acid, n being at least 3 and not greater than 20.Type: GrantFiled: February 28, 1996Date of Patent: November 13, 2001Assignee: Rhone-Poulenc ChimieInventors: Robert Janin, Laurent Saint-Jalmes
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Patent number: 6180667Abstract: Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, staight or branched alkanoyl having 2-26 carbon atoms, optionally &ohgr;-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.Type: GrantFiled: March 28, 1997Date of Patent: January 30, 2001Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Foresta, Vito Ruggiero, Maria Ornella Tinti, Nazareno Scafetta
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Patent number: 6172057Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: February 19, 1998Date of Patent: January 9, 2001Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell
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Patent number: 6051733Abstract: Polymeric compositions for the preparation of optical grade materials, and the optical materials prepared thereby, are provided. The compositions include a class of reactive and non-reactive additives, referred to as additive, in combination with a polymer and optionally a diluent. The additives are preferably the reaction product of a thiol containing compound and an unsaturated compound. The additives optimally have a refractive index between about 1.40 and 1.70, and preferably between 1.50 and 1.70; a relatively high Abbe number (between 25 and 60) and minimal color.Type: GrantFiled: July 25, 1997Date of Patent: April 18, 2000Assignee: UCB, S.A.Inventor: Peter Weissman
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Patent number: 5994539Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.Type: GrantFiled: December 18, 1997Date of Patent: November 30, 1999Assignee: Zambon Group S.p.A.Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Mario Fantucci, Claudio Semeraro