Nitro Or Nitroso Patents (Class 562/434)
-
Patent number: 8314214Abstract: Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes.Type: GrantFiled: April 26, 2011Date of Patent: November 20, 2012Assignee: Biocon LimitedInventors: Jennifer A. Riggs-Sauthier, Nnochiri N. Ekwuribe
-
Patent number: 8269039Abstract: The invention provides novel compounds and methods to carry out organocatalytic Michael additions of aldehydes to nitroethylene catalyzed by a proline derivative to provide ?-substituted-?-nitroaldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96-99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to protected ?2-amino acids, which are essential for systematic conformational studies of ?-peptide foldamers.Type: GrantFiled: March 23, 2009Date of Patent: September 18, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Samuel Helmer Gellman, Yonggui Chi, Li Guo
-
Patent number: 8211878Abstract: The present invention provides methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death in a patient. The invention includes use of 5-benzylamino salicylic acid (BAS) and its derivatives. Thus, the present invention provides methods for reducing neuronal death in nervous system injuries resulting from amyotrophic lateral sclerosis.Type: GrantFiled: May 24, 2010Date of Patent: July 3, 2012Assignee: Neurotech Pharmaceuticals Co., Ltd.Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
-
Publication number: 20120158127Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the corresponding diamines or diisocyanates thereof, wherein each X independently represents —CH2COO—, —CH(CH3)COO—, —CH2CH2OCH2COO—, —CH2CH2CH2CH2CH2COO—, —(CH2)yCOO— where y is 2 to 4 or 6 to 24, or —(CH2CH2O)z?CH2COO— where z? is 2 to 24; each Y represents —COCH2O—, —COCH(CH3)O—, —COCH2OCH2CH2O—, —COCH2CH2CH2CH2CH2O—, —CO(CH2)mO— where m is 2 to 4 or 6 to 24, or —COCH2O(CH2CH2O)n— where n is 2 to 24; R? is hydrogen, benzyl or straight-chained or branched alkyl; p is 1 to 4; and Rn represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid and —NO2, which is attached directly to an aromatic ring or attached through an aliphatic chain. Absorbable polymers prepared from these compounds are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention and other implantable medical devices.Type: ApplicationFiled: February 22, 2012Publication date: June 21, 2012Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
-
Publication number: 20110245110Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.Type: ApplicationFiled: May 9, 2011Publication date: October 6, 2011Applicant: AFFYMETRIX, INC.Inventors: Glenn H. McGall, Andrea Cupoletti
-
Publication number: 20100331566Abstract: The invention provides synthetic methods that utilize bromo or chloro substituents as blocking groups during the functionalization of aromatic rings, as well as compounds that are prepared from such methods.Type: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Inventors: Leslie S. Jimenez, Ahalya Ramanathan
-
Publication number: 20100191011Abstract: The present invention has its object to provide a method for producing an optically active hydroxycarboxylic acid derivative which is an intermediate important for production of medicines, agrochemicals, chemical products, and so on. The production method of the present invention comprises: carrying out a hydrogen-transfer reduction of a ketocarboxylic acid or a salt thereof by the reaction of an optically active diamine complex to produce an optically active hydroxycarboxylic acid derivative. According to the present invention, it is possible to safely and efficiently produce an industrially-useful optically active hydroxycarboxylic acid derivative.Type: ApplicationFiled: August 8, 2007Publication date: July 29, 2010Applicant: Kaneka CorporationInventors: Susumu Amano, Akio Fujii, Shohei Yamamoto, Masaru Mitsuda
-
Patent number: 7696247Abstract: Novel nitric-oxide releasing lipid molecules are provided which comprise a lipid molecule selected from (a) phosphoglycerides, (b) lipids having a sphingosine base as a backbone, (c) monoacylglyerols, (d) diacylglycerols, (e) glycosylacylglycerols, and (f) sterol compounds of the formula: where R is a branched aliphatic chain of eight or more carbon atoms, wherein the lipid molecule is provided with a nitric-oxide containing group which comprises (a) a —S—N?O moiety, (b) a —O—N?O moiety, or (c) a a moiety. Also provided are methods of forming such nitric oxide releasing lipid molecules. Various pharmaceutical compositions, topical liquids and drug delivery systems comprising the nitric-oxide releasing lipid molecules are also described.Type: GrantFiled: July 6, 2004Date of Patent: April 13, 2010Assignee: Boston Scientific Scimed, Inc.Inventors: Robert A. Herrmann, Wendy Naimark
-
Patent number: 7608731Abstract: The present invention provides a process for the preparation 6-[3-(hetero)aryloxy-2-fluoro-benzyl]-2H-pyridazin-3-one compounds 1 where R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R6 is NO2, NH2, alkyl, halogen, or a function group readily derived therefrom and R4c is hydrogen or alkyl. There also is provided a process for the preparation of phenylacetic acid compounds 2, wherein R2 and R6 are as defined previously and R5a is hydrogen or alkyl, which are useful for the preparation of pyridazinone compounds.Type: GrantFiled: October 23, 2007Date of Patent: October 27, 2009Assignee: Roche Palo Alto LLCInventors: Denis John Kertesz, Michael Martin, Wylie Solang Palmer
-
Patent number: 7427689Abstract: A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is “compound B17”=methyl-(p-nitrophenyl)-2-propynoate.Type: GrantFiled: July 30, 2001Date of Patent: September 23, 2008Assignee: Georgetown UniversityInventors: Shaomeng Wang, Dajun Yang, Istvan Enyedy
-
Publication number: 20080188680Abstract: The present invention is directed to a process of maximizing the solubility of a nonelectrolyte solute in a solvent by operating within an optimal temperature range at conditions wherein the nonelectrolyte solute is not a pure liquid. In particular, the process of the present invention is directed to conversion of a carboxylic acid compound to an ester under conditions wherein the solubility of the ester in an alcoholic solvent approaches ideal solubility behavior.Type: ApplicationFiled: February 21, 2006Publication date: August 7, 2008Inventor: Michael J. Gentilcore
-
Patent number: 7294740Abstract: The invention claimed herein provides a process to oxidize N-(5-alkoxy-2-methyl-4-nitrophenyl)acetamides to N-acyl-2-amino-4-alkoxy-5-nitrobenzoic acids using potassium permanganate in the presence of magnesium sulfate in aqueous sulfolane or aqueous pyridine.Type: GrantFiled: May 18, 2007Date of Patent: November 13, 2007Assignee: WyethInventors: Scott Mason Duncan, Augustine Tobi Osuma, Sylvain Daigneault, Michel Bernatchez
-
Patent number: 7138538Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiomers.Type: GrantFiled: May 7, 2004Date of Patent: November 21, 2006Assignee: Solvay (Societe Anonyme)Inventors: Thierry Delplanche, Roland Callens
-
Patent number: 7094923Abstract: The present invention relates to the preparation of nitrobenzoic acids by oxidizing particular nitrotoluenes, nitrobenzyl alcohols, esters and/or ethers in the presence of nitric acid at elevated temperature and elevated pressure. It has been found that the particular nitrotoluenes, nitrobenzyl alcohols, esters and/or ethers may be oxidized particularly reliably and in high yields using nitric acid to the benzoic acid derivatives when they are metered into the nitric acid.Type: GrantFiled: March 17, 2005Date of Patent: August 22, 2006Assignee: Bayer AktiengesellschaftInventors: Reinhard Langer, Lars Rodefeld, Karl Heinz Neumann
-
Patent number: 7074536Abstract: The present invention provides an alkylenebisnaphthol derivative represented by formula [I]: and a salt thereof. The compound of the present invention has an excellent triboelectric charge property and useful as charge control agent for electrophotographic toners.Type: GrantFiled: July 30, 2002Date of Patent: July 11, 2006Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori, Nobuhiro Yonetani
-
Patent number: 7056903Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.Type: GrantFiled: May 9, 2003Date of Patent: June 6, 2006Assignee: Syntex (U.S.A.) LLCInventors: Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Jr., Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
-
Patent number: 7049308Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.Type: GrantFiled: September 27, 2001Date of Patent: May 23, 2006Assignee: Duke UniversityInventors: Jonathan S. Stamler, Eric J. Toone
-
Patent number: 7012151Abstract: The present invention relates to a process for the highly regioselective aromatic nitration of alkyl 4-alkanoylamino-3-alkyl-benzoates in the 5-position in a mixture containing nitric acid and the use of the resulting products for preparing, in particular, pharmaceutically active benzimidazole derivatives.Type: GrantFiled: April 12, 2000Date of Patent: March 14, 2006Assignee: Boehringer Ingelheim Pharma KGInventors: Margarete Schneider, Heinrich Schneider
-
Patent number: 6900349Abstract: The present invention relates to the preparation of nitrobenzoic acids by oxidizing particular nitrotoluenes, nitrobenzyl alcohols, esters and/or ethers in the presence of nitric acid at elevated temperature and elevated pressure. It has been found that the particular nitrotoluenes, nitrobenzyl alcohols, esters and/or ethers may be oxidized particularly reliably and in high yields using nitric acid to the benzoic acid derivatives when they are metered into the nitric acid.Type: GrantFiled: March 30, 2001Date of Patent: May 31, 2005Assignee: Bayer AktiengesellschaftInventors: Reinhard Langer, Lars Rodefeld, Karl Heinz Neumann
-
Patent number: 6884907Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: May 10, 2002Date of Patent: April 26, 2005Assignee: Guilford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
-
Patent number: 6855842Abstract: The invention concerns novel nitroaromatic compounds of general formula (I?) wherein: R, R?1, R2, Z and n are as defined in claim 1. The invention also concerns a method for preparing nitroaromatic compounds nitrated in position 4. The invention further concerns the use of said compounds for preparing heterocyclic benzofuran or benzothiophene derivatives nitrated in position 5. The invention concerns particularly the preparation of 2-alkyl-5-nitrobezofuran.Type: GrantFiled: October 23, 2000Date of Patent: February 15, 2005Assignee: Rhodia ChimieInventors: Thierry Schlama, Armand Mettling, Philippe Karrer
-
Publication number: 20040248026Abstract: The present invention provides an alkylenebisnaphthol derivative represented by formula [I]: 1Type: ApplicationFiled: July 12, 2004Publication date: December 9, 2004Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori, Nobuhiro Yonetani
-
Publication number: 20040209957Abstract: The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.Type: ApplicationFiled: December 22, 2003Publication date: October 21, 2004Inventors: Byoung-Joo Gwag, Sung-Hwa Yoon, Ho-Sang Moon, Eun-Chan Park, Seok-Joon Won, Young-Ae Lee, Hae-Un Lee
-
Publication number: 20040192961Abstract: A method for the regioselective ortho-directed nitration of phenolic compounds useful for the preparation of ortho-nitro-phenols according to formula (I) is described.Type: ApplicationFiled: May 20, 2004Publication date: September 30, 2004Inventor: David Alexander Learmonth
-
Patent number: 6780849Abstract: Novel nitric-oxide releasing lipid molecules are provided which comprise a lipid molecule selected from (a) phosphoglycerides, (b) lipids having a sphingosine base as a backbone, (c) monoacylglyerols, (d) diacylglycerols, (e) glycosylacylglycerols, wherein the lipid molecole is provided with a nitric-oxide contianing group which comprises a (a) a —S—N═O moiety, (b) a —O—N═O moiety, or (c) a moiety. Also provided are methods of forming such nitric oxide releasing lipid molecules. Various pharmaceutical compositions, topical liquids and drug delivery systems comprising the ntric-oxide releasing lipid molecules are also described. Further provided are methods for therapeutically administering nitric oxide to patients, methods for treating or preventing various conditions, methods for promoting wound healing and methods for reducing the cells present in an atherosclerotic lesion which methods utilize the nitric-oxide releasing lipid molecules.Type: GrantFiled: December 21, 2000Date of Patent: August 24, 2004Assignee: SciMed Life Systems, Inc.Inventors: Robert A. Herrmann, Wendy Naimark
-
Patent number: 6780995Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: November 25, 2002Date of Patent: August 24, 2004Assignee: Isotechnika Inc.Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
-
Patent number: 6743373Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiometers.Type: GrantFiled: April 14, 2000Date of Patent: June 1, 2004Assignee: Solvay (Societe Anonyme)Inventors: Thierry Delplanche, Roland Callens
-
Publication number: 20030220517Abstract: A novel process affords &ohgr;-ketocarboxylic acid derivatives of the formula (I) 1Type: ApplicationFiled: March 14, 2003Publication date: November 27, 2003Inventor: Albrecht Marhold
-
Publication number: 20030194371Abstract: The invention relates to (ethylene)-(propylene)-triaminepentaacetic acid derivatives that are substituted on both the ethylene bridge and the propylene bridge, as well as conjugates of these compounds with biomolecules. The compounds and conjugates are suitable as agents for NMR diagnosis and radiodiagnosis as well as for radiotherapy.Type: ApplicationFiled: July 10, 2002Publication date: October 16, 2003Applicant: Schering AGInventors: Lutz Lehmann, Matthias Friebe, Christoph-Stephan Hilger, Ulrich Niedballa, Johannes Platzek, Bernd Raduchel
-
Publication number: 20030191341Abstract: A process for the preparation of a compound of general formula I: 1Type: ApplicationFiled: May 16, 2003Publication date: October 9, 2003Inventors: Stephen Martin Brown, James Peter Muxworthy
-
Publication number: 20030176497Abstract: The invention relates to carboxamide-substituted phenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: May 24, 2002Publication date: September 18, 2003Inventors: Elisabeth Defossa, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Erich von Roedern, Stefan Peukert, Alfons Enhsen, Armin Bauer, Bernd Neises, Karl Ulrich Wendt
-
Publication number: 20030149003Abstract: Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.Type: ApplicationFiled: October 28, 2002Publication date: August 7, 2003Inventors: David J. Chaplin, Charles Manly Garner, Robert Ronald Kane, Kevin G. Pinney, Joseph Anthony Prezioso, Klaus Edvardsen
-
Publication number: 20030100607Abstract: The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.Type: ApplicationFiled: May 30, 2002Publication date: May 29, 2003Inventors: Takashi Tsukamoto, Doris Stoermer, Dilrukshi Vitharana
-
Publication number: 20030097018Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.Type: ApplicationFiled: July 29, 2002Publication date: May 22, 2003Applicant: Neurotech Co., Ltd.Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
-
Patent number: 6562807Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.Type: GrantFiled: June 22, 2001Date of Patent: May 13, 2003Assignee: Novo Nordisk A/SInventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
-
Publication number: 20030073862Abstract: The present invention relates to 2-(benzoylamino)benzoic acid derivatives of the formula I 1Type: ApplicationFiled: July 3, 2002Publication date: April 17, 2003Inventors: Anna-Lena Gustavsson, Lena Jendeberg, Patrick Roussel, Martin Slater, Markus Thor
-
Publication number: 20030045754Abstract: A process for producing fomesafen from acifluorfen comprises the steps of (a) converting acifluorfen to its acid chloride, (b) coupling the acid chloride so formed with methanesulphonamide to form crude fomesafen and (c) purifying the crude fomesafen, characterized in that each of the steps is carried out in a single common solvent, which is preferably a chloroalkane.Type: ApplicationFiled: June 20, 2002Publication date: March 6, 2003Inventors: Stephen Martin Brown, Brian David Gott, James Peter Muxworthy
-
Patent number: 6511988Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: August 10, 2001Date of Patent: January 28, 2003Assignee: Isotechnika Inc.Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
-
Publication number: 20030013746Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions.Type: ApplicationFiled: August 8, 2002Publication date: January 16, 2003Applicant: University of Kansas Medical Center.Inventors: Billy G. Hudson, Parvin Todd, Raja Gabriel Khalifah, Aaron Ashley Booth
-
Publication number: 20020151720Abstract: Novel naphthol derivatives, and various azo compounds and metal complexes prepared by using the derivatives are provided.Type: ApplicationFiled: January 16, 2002Publication date: October 17, 2002Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
-
Patent number: 6452044Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neutopathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.Type: GrantFiled: May 30, 2001Date of Patent: September 17, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Takashi Tsukamoto, Barbara S. Slusher, Eric Wang
-
Publication number: 20020072500Abstract: The present invention relates to a class of compounds represented by the Formula I.Type: ApplicationFiled: September 26, 2001Publication date: June 13, 2002Inventors: Thomas Rogers, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Peter Ruminiski, Jennifer VanCamp, Chester Yuan
-
Patent number: 6403638Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.Type: GrantFiled: March 21, 2000Date of Patent: June 11, 2002Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
-
Publication number: 20020019538Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: ApplicationFiled: August 10, 2001Publication date: February 14, 2002Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
-
Patent number: 6344484Abstract: The present invention relates to novel tyrosine alkoxyguanidine compounds that are inhibitors of alpha V (&agr;v) integrins, for example &agr;v&bgr;3 and &agr;v&bgr;5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &agr;v&bgr;3 and &agr;v&bgr;5 integrins, including conditions such as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, m and n are defined herein.Type: GrantFiled: February 11, 2000Date of Patent: February 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Yu Kai Lee
-
Patent number: 6329547Abstract: The present invention provides compounds represented by the following general formula [I] and salts thereof, which are useful as therapeutic agents for glaucoma, wherein R1 is H, lower alkyl or phenyl, and the phenyl can be substituted by lower alkyl, hydroxy, lower alkoxy, halogen, nitro or phenyl; R2 and R3, being the same or different, are H, halogen or lower alkyl; R4 and R5, being the same or different, are H, lower alkyl or carboxyl or ester thereof; and R6 is carboxyl or phosphono or ester thereof.Type: GrantFiled: November 22, 2000Date of Patent: December 11, 2001Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Eiichi Shirasawa, Koji Konomi, Masaki Ichikawa, Hiroshi Suhara
-
Patent number: 6326403Abstract: Compounds of the formula I wherein X, Y, Z, R1 and R2 are as defined in claim 1, and their salts and solvates, can be used as integrin inhibitors in particular for the prophylaxis and treatment of circulatory disorders, for thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, for pathological processes which are maintained or propagated by angiogenesis and in tumour therapy.Type: GrantFiled: January 12, 2001Date of Patent: December 4, 2001Assignee: Merck Patent Gesellschaft mitInventors: Günter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Jörg Simon Schmitt
-
Patent number: 6306871Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: September 19, 2000Date of Patent: October 23, 2001Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
-
Publication number: 20010025084Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12.Type: ApplicationFiled: January 22, 2001Publication date: September 27, 2001Inventors: Vinh D. Tran, Vu Van Ma, Ruiyan Liu
-
Patent number: 6284914Abstract: New compounds of general formulae (III), (IV) and (V).Type: GrantFiled: January 27, 2000Date of Patent: September 4, 2001Assignee: Fuji Yakuhin Kogyo Kabushiki KaishaInventors: Junko Fujisawa, Eiko Suda, Katsuhiro Igeta, Tadanori Morikawa, Tetsunori Fujisawa, Shinjiro Odake, Yasuo Morita, Tomoko Hongo, Hajime Ito