Plural Nitrogens Patents (Class 562/448)
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Patent number: 7696377Abstract: It is the objective to provide a method of stabilizing hydroxylamine at a high temperature and a high concentration or in a case that metal impurities such as Fe got mixed therewith, and a stabilized hydroxylamine solution. A method for stabilizing hydroxylamine related to the present invention is characterized by adding ethylenediamine-N,N?-di(o-hydroxyphenylacetic acid) as a preservation stabilizer.Type: GrantFiled: October 19, 2006Date of Patent: April 13, 2010Assignee: Showa Denko K.K.Inventors: Takanori Aoki, Toshitaka Hiro
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Patent number: 7692038Abstract: The present invention relates to crystalline forms of (3S)-3-[N—(N?-(2-tert-butylphenyl)oxamyl)alaninyl]amino-5-(2?,3?,5?,6?-tetrafluorophenoxy)-4-oxopentanoic acid (see formula I). The invention further relates to pharmaceutical compositions comprising such crystalline forms and to the use of said pharmaceutical compositions and said crystalline forms in the treatment of various conditions, particularly in the treatment of liver fibrosis.Type: GrantFiled: December 6, 2007Date of Patent: April 6, 2010Assignee: Pfizer, Inc.Inventors: Eric Hagen, Jason A. Hanko, Stuart Dimock
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Publication number: 20100056825Abstract: Formulations of canfosfamide and their preparation.Type: ApplicationFiled: July 29, 2009Publication date: March 4, 2010Inventor: Betsy R. Hughes
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Patent number: 7662994Abstract: The present invention describes a novel method for the purification of dexloxiglumide by crystallization from isopropyl ether which permits the production, in a reproducible manner, of a product with morphological and particle-size characteristics such as to favor its use in the preparation of oral pharmaceutical forms on an industrial scale.Type: GrantFiled: June 21, 2004Date of Patent: February 16, 2010Assignee: Rottapharm S.p.A.Inventors: Francesco Makovec, Lucio Claudio Rovati
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Publication number: 20100016631Abstract: The disclosure relates to a method for the synthesis of a compound of the formula (I) in which: n is an integer higher than or equal to 1; Rb and each Rn are independently a hydrogen atom, a C1-C6 arylalkyl group or a C1-C6 alkyl group substituted or not by an aryl group, —COOH, C1-C6, —COO-(alkyl), —CONH2, —SH, heteroaryl, —NH2, —NHC(NH)(NH2), C1-C6-s-(alkyl), —OH or phenol; Ra is a N-protective group; Rc is a ORd group in which Rd is a C1-C6 alkyl group or a NReRf group in which Re and Rf Re independently an N-protective group.Type: ApplicationFiled: March 21, 2007Publication date: January 21, 2010Applicant: Centre National de la Recherche Scientifique(CNRS)Inventors: Jean Martinez, Frédéric Lamaty, Valérle Declerck
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Publication number: 20090312286Abstract: The invention provides a new class of compounds capable of inhibiting carnitine palmitoyl transferase (CPT) having formula (I) The invention also relates to pharmaceutical compositions, which comprise at least one new compound according to the invention, and their therapeutic use in the treatment of hyperglycaemic conditions such as diabetes and the pathologies associated with it, such as for example congestive heart failure and obesity.Type: ApplicationFiled: July 10, 2007Publication date: December 17, 2009Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Fabio Giannessi, Emanuela Tassoni, Natalina Dell' Uomo, Roberto Conti, Maria Ornella Tinti
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Publication number: 20090306424Abstract: The present invention refers to a process for preparing a compound of formula (I) through a carboxymethylation reaction occurring in the presence of a suitable alkylating agent and of a base, without the need of monitoring the pH of the reaction environment. The compound of formula (I) is a useful intermediate in the preparation of diagnostic contrast agents for MRI techniques.Type: ApplicationFiled: August 12, 2009Publication date: December 10, 2009Applicant: BRACCO IMAGING S.P.A.Inventors: Silvia Ceragioli, Giovanni Luca Ciarciello, Luciano Castiglia
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Patent number: 7592482Abstract: The present invention refers to a process for preparing a compound of formula (I) through a carboxymethylation reaction occurring in the presence of a suitable alkylating agent and of a base, without the need of monitoring the pH of the reaction environment. The compound of formula (I) is a useful intermediate in the preparation of diagnostic contrast agents for MRI techniques.Type: GrantFiled: August 24, 2006Date of Patent: September 22, 2009Assignee: Bracco Imaging S.p.A.Inventors: Silvia Ceragioli, Giovanni Luca Ciarciello, Luciano Castiglia
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Publication number: 20090118537Abstract: The present invention refers to a process for preparing a compound of formula (I) through a carboxymethylation reaction occurring in the presence of a suitable alkylating agent and of a base, without the need of monitoring the pH of the reaction environment. The compound of formula (I) is a useful intermediate in the preparation of diagnostic contrast agents for MRI techniques.Type: ApplicationFiled: August 24, 2006Publication date: May 7, 2009Applicant: Bracco Imaging S.p.A.Inventors: Silvia Ceragioli, Giovanni Luca Ciarcello, Castiglia Luciano
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Publication number: 20080249031Abstract: The present invention relates to crystalline forms of (3S)-3-[N—(N?-(2-tert-butylphenyl)oxamyl)alaninyl]amino-5-(2?,3?,5?,6?-tetrafluorophenoxy)-4-oxopentanoic acid (see formula I). The invention further relates to pharmaceutical compositions comprising such crystalline forms and to the use of said pharmaceutical compositions and said crystalline forms in the treatment of various conditions, particularly in the treatment of liver fibrosis.Type: ApplicationFiled: December 6, 2007Publication date: October 9, 2008Inventors: Eric Hagen, Jason A. Hanko, Stuart Dimock
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Publication number: 20080095704Abstract: The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.Type: ApplicationFiled: July 1, 2005Publication date: April 24, 2008Inventors: Alan Cuthbertson, Magne Solbakken
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Patent number: 7205336Abstract: The present invention provides compounds that are inhibitors of the proteolytic activity of the enzyme ?-secretase, pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, processes for making the compounds, and methods of using the compounds to treat Alzheimers disease.Type: GrantFiled: May 14, 2003Date of Patent: April 17, 2007Assignee: Merck & Co., Inc.Inventors: Ming-Tain Lai, Ming-Chih Crouthamel, Stephen F. Brady
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Patent number: 7202381Abstract: This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.Type: GrantFiled: March 14, 2005Date of Patent: April 10, 2007Assignee: Janssen Pharmaceutica, NVInventors: Henry J. Breslin, Wei He, Robert W. Kavash
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Patent number: 7199265Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor ?, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.Type: GrantFiled: June 15, 2001Date of Patent: April 3, 2007Assignee: Karo Bio ABInventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg
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Patent number: 7183430Abstract: The invention relates to compounds having formula (I), which can block the response to chemical substances or thermal stimuli or mediators of inflammation of nociceptors, a production method thereof and compositions containing same.Type: GrantFiled: May 16, 2003Date of Patent: February 27, 2007Assignee: Diverdrugs, S.L.Inventors: Antonio Ferrer Montiel, Asia Fernández Carvajal, Carolina Garcia Martínez, Carlos Belmonte Martínez, Wim Van Den Nest, Cristina Carreño Serraïma
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Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 7145040Abstract: The present invention provides process useful for the preparation of intermediates which are useful in the preparation of amino acids useful in preparing peptide receptor modulators, for example agonists or partial agonists of such peptide receptors. Such peptide receptor modulators include, for example glucagon like peptide-1 receptor modulators which are useful for the amelioration of the diabetic condition.Type: GrantFiled: June 30, 2005Date of Patent: December 5, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Arvind Mathur, K. Selva Kumar
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Patent number: 6855706Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ? 4 integrin. They are used as therapeutic agents for various diseases concerning ? 4 integrin.Type: GrantFiled: May 20, 2002Date of Patent: February 15, 2005Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
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Patent number: 6835851Abstract: The instant invention relates to a process for preparing a compound of formula (I): said process comprising a step (B) which consists in performing a Michael addition of a thioacid RS4H on to an &agr;-substituted acrylamide derivative.Type: GrantFiled: November 9, 2001Date of Patent: December 28, 2004Assignee: BioprojetInventors: Thierry Monteil, Denis Danvy, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Serge Piettre
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Patent number: 6806365Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: April 5, 2002Date of Patent: October 19, 2004Assignee: Hoffmann-La Rocher Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6777440Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1, R2 and B1 are as defined herein.Type: GrantFiled: December 6, 2002Date of Patent: August 17, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Jacques Banville, Roger Remillard, Serge Plamondon
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Patent number: 6743929Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 6, 2000Date of Patent: June 1, 2004Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 6610710Abstract: Phenylalanine derivatives of the following formula and analogues thereof have an antagonistic activity to &agr;4&bgr;7 integrin and a selectivity toward &agr;4&bgr;1 integrin. They are used as therapeutic agents for various diseases to which &agr;4&bgr;7 integrin relates.Type: GrantFiled: June 28, 2002Date of Patent: August 26, 2003Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Chieko Ejima, Mitsuhiko Kojima, Eiji Nakanishi, Hiroyuki Izawa, Yuko Satake, Nobuyasu Suzuki, Manabu Suzuki, Masahiro Murata
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Patent number: 6586403Abstract: This invention relates to methods and compositions of tripeptides and dipeptides having anti-inflammatory activities that can be used for the treatment of allergic and inflammatory reactions. A peptide of the formula: X-R.sub. 1 -R.sub.2 -R.sub.3 -Y (I) or X-R.sub. 1 -R.sub.2 -Y (II) wherein X is selected from the group consisting of H and acetyl; R.sub. 1 is selected from the group consisting of D or L-phenylalanine; tyrosine; tryptophan; phenylglycine; Nor-methylphenylalanine; cyclohexylalanine; and norleucine; R.sub.2 is selected from the group consisting of D or L-glutamate; and aspartate; and in the case of peptide (II), R.sub.3 is selected from the group consisting of glycine; D or L-alanine; beta-alanine; valine; leucine; isoleucine; sarcosine; and gamma-aminobutyric acid or another aliphatic amino acid; and Y is selected from the group consisting of OH and NH.sub.2, but excluding the dipeptides H-L-Phe-L-Glu-OH, H-L-Trp-L-Glu-OH, H-D-Phe-D-Glu-OH and H-D-Trp-D-Glu-OH.Type: GrantFiled: July 20, 2000Date of Patent: July 1, 2003Assignee: Salpep Biotechnology, Inc.Inventors: Ronald Mathison, Essam Metwally
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Patent number: 6528655Abstract: A compound of formula I′ and pharmaceutically acceptable derivatives thereof including, for example, where applicable or appropriate pharmaceutically acceptable salts thereof. Ar and Ar′ are aromatic or aryl type groups. The compounds have HIV integrase inhibitory properties. Ar, Ar′ and W may be as defined in the specification.Type: GrantFiled: September 26, 2001Date of Patent: March 4, 2003Assignee: Pharmacor, Inc.Inventors: Blaise Magloire N'Zemba, Gilles Sauvé, Guy Sévigny, Jocelyn Yelle
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Publication number: 20020132833Abstract: This invention provides novel compounds that are effective as inhibitors of caspase and cellular apoptosis. The invention also provides methods for using the compounds to treat caspase-mediated diseases in mammals.Type: ApplicationFiled: April 3, 2001Publication date: September 19, 2002Inventors: Julian M.C. Golec, Paul Charifson, Guy Brenchley
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Patent number: 6362165Abstract: An hydroxyphenyl derivative selected from the group consisting of a compound of formula and when a compound of formula I comprises a carboxylic acid group pharmaceutically acceptable salts thereof and when a compound of formula I comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein n is 1, 2 or 3, e is 1, 2 or 3, Hal represents a halogen atom (e.g. Cl, Br, F or I), p is 0, 1 or 2, r is 0, 1 or 2, X and X′ each independently represents a single bond, a saturated straight or branched hydrocarbon group of 1 to 4 carbon atoms or a straight or branched hydrocarbon group of 2 to 4 carbon atoms comprising a carbon to carbon double bond, Ra represents H or —CH3, and Raa represents H or —CH3; W may represent an amino acid residue or fragment. These compounds may be used to inhibit the activity of HIV integrase.Type: GrantFiled: March 27, 2000Date of Patent: March 26, 2002Assignee: Pharmacor Inc.Inventors: Gilles Sauvé, Jocelyn Yelle
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Patent number: 6350907Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitorsType: GrantFiled: April 11, 2000Date of Patent: February 26, 2002Assignee: Pfizer IncInventors: Michael Jonathan Fray, Roger Peter Dickinson, Kevin Neil Dack
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Publication number: 20020004608Abstract: N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: 1Type: ApplicationFiled: May 16, 2001Publication date: January 10, 2002Inventors: Leo Alig, Katrin G. Zbinden, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Hans Peter Wessl
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Publication number: 20010043942Abstract: Herein is disclosed an aqueous stable lysine solution containing an acid radical in such amount that the solubility of lysine therein has been increased than in the corresponding aqueous lysine base solution, whereby during storage of lysine in the form of a free-lysine solution (liquid composition), the precipitation of lysine base crystals due to the drop in temperature is prevented thereby improving the handling thereof during transportation (transfer) etc.Type: ApplicationFiled: June 18, 2001Publication date: November 22, 2001Applicant: AJINOMOTO, CO., INC.Inventors: Kazuhiro Hasegawa, Toshiya Tanabe, Keita Minami
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Patent number: 6310078Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 3, 2000Date of Patent: October 30, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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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
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Patent number: 6274733Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.Type: GrantFiled: October 28, 1999Date of Patent: August 14, 2001Assignee: Pfizer Inc.Inventors: Thomas G. LaCour, Charles William Murtiashaw, III
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Patent number: 6255285Abstract: The present invention has as its object providing phenethylamine derivatives that typically function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds represented by the general formula (1): (wherein A is typically an amino acid residue, R1 is typically R6—CO—, R2 is typically a hydrogen atom, R3 is typically —CO—R7, R4 is typically an alkyl group, R5 is typically a hydroxyl group, R6 is typically an alkyl group, and R7 is typically an amino group).Type: GrantFiled: February 15, 2000Date of Patent: July 3, 2001Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Ken-ichiro Kotake, Toshiro Kozono, Tsutomu Sato, Hisanori Takanashi
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Patent number: 6242607Abstract: The invention relates to glutarimides of formula (I): in which Ar represents a phenyl non substituted or substituted one or more times with one of the substituents selected from a halogen atom, a hydroxyl, a (C1-C4)alkoxy, a trifluoromethyl, a (C1-C4)alkyl, said substituents being identical or different; a pyridyl group; a thienyl group and X is methylene or ethylene, their salts and their enantiomers, as well as their method of preparation and their use for the preparation of the corresponding 3,3-disubstituted piperidines.Type: GrantFiled: November 10, 1999Date of Patent: June 5, 2001Assignee: Sanofi-SynthelaboInventors: Philippe Camus, Marcel Descamps, Joël Radisson
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Patent number: 6229011Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: August 21, 1998Date of Patent: May 8, 2001Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6197750Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
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Patent number: 6162947Abstract: A novel a process for the preparation of the chelating agent of formula (I) ##STR1## 4-carboxy-5,8,11-tris(carboxymethyl)-1-phenyl-2-oxa-5,8,11-triazatridecan- 13-oic acid, commonly named BOPTA.Type: GrantFiled: July 8, 1999Date of Patent: December 19, 2000Assignee: Dibra S.p.A.Inventors: Marina Ausonio, Carlo Distaso, Giuseppe Gerardo Elia, Alessandro Lesignoli, Rodolfo Piva, Carlo Secchi, Carlo Felice Viscardi
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Patent number: 6153591Abstract: The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: March 16, 1999Date of Patent: November 28, 2000Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John Drewe, Yan Wang, Eckard Weber
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Patent number: 6127341Abstract: Compounds of the general formula I ##STR1## compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are described.Type: GrantFiled: June 1, 1998Date of Patent: October 3, 2000Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Jesper Lau, Bernd Peschke, Michael Ankersen, Kjeld Madsen, Nils Langeland Johansen
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Patent number: 6100423Abstract: The present invention is directed to compounds of the formula ##STR1## where R.sup.1 is BOC or H, R is H or lower alkyl; X and Y are the same or different halo atoms selected from the group consisting of Cl, Br or I and pharmaceutically acceptable salts and isomers thereof.Type: GrantFiled: March 3, 1999Date of Patent: August 8, 2000Assignee: G. D. Searle & Co.Inventors: Joe T. Collins, Balekudru Devadas, Hwang-fun Lu, James W. Malecha, Julie Marion Miyashiro, Srinivasan Nagarajan, Joseph Gerace Rico, Thomas E. Rogers
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Patent number: 6010733Abstract: Novel aspartylamide derivatives such as N-(.alpha.-L-aspartyl-(1R,2S,4S)-1-methyl-2-hydroxy-4-phenylhexylamide, N-.alpha.-7(N'-3,3-dimethylbutylaspartyl)-(1R,2S,4S)-1-methyl-2-hydroxy-4- phenylhexylamide) and the like, and a sweetener containing the above-mentioned derivatives or salts thereof as an active ingredient, is low-calory and which exhibits a high level of stability, an excellent safety and an excellent sweetness.Type: GrantFiled: January 13, 1997Date of Patent: January 4, 2000Assignee: Ajinomoto Co., Inc.Inventors: Tadashi Takemoto, Yusuke Amino, Ryoichiro Nakamura
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Patent number: 5965588Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 26, 1998Date of Patent: October 12, 1999Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5929112Abstract: The derivatives of N,N'-di(aralkyl)-N,N'-di(carboxyalkyl) alkylene di- or triamine and N-(aralkyl)-N'-(carboxyalkyl)-N'N'-di(carboxyalkyl) alkylene di- or triamine of the formula: ##STR1## and the salts and metallic complexes thereof are disclosed. Use in pharmaceutical or cosmetic compositions used to protect the organism from oxidizing stress situations linked to certain pathological states.Type: GrantFiled: July 23, 1996Date of Patent: July 27, 1999Assignee: L'OrealInventors: Jean-Baptiste Galey, Sylvie Genard
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Patent number: 5840974Abstract: Compound of formula (I) ##STR1## wherein Ar represents an optionally substituted phenyl or heteroaryl group, m is 1 or 2, n is 0, 1, 2, 3 or 4, X represents --COOH or --CONHOH and R.sub.1, R.sub.3 and Y are as defined in the specification,are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: September 8, 1997Date of Patent: November 24, 1998Assignee: Britisch Biotech Pharmaceuticals, Ltd.Inventors: Mark Whittaker, Raymond Paul Beckett, Zoe Marie Spavold, Fionna Mitchell Martin
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Patent number: 5770620Abstract: The present invention provides novel protein tyrosine phosphatase modulating compounds having an aryl acrylic acid structure, compositions comprising the compounds, and methods of making and using the same.Type: GrantFiled: October 16, 1995Date of Patent: June 23, 1998Assignee: Ontogen CorporationInventors: Adnan M. M. Mjalli, Xiaodong Cao, Edmund J. Moran
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Patent number: 5767085Abstract: Compounds of the formula A--B--C--D(--E).sub.p are used to stimulate the release of growth hormone from the pituitary.Type: GrantFiled: June 6, 1995Date of Patent: June 16, 1998Assignee: Novo Nordisk A/SInventors: Nils Langeland Johansen, Jesper Lau, Kjeld Madsen, Behrend Friedrich Lundt, Henning Th.o slashed.gersen, Birgit Sehested Hansen, Bernd Peschke
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Patent number: 5756825Abstract: The present disclosure details the preparation of hydroxamic-acid based bifunctional chelators and their use in conjugating metal ions to proteins and nucleic acids for tumor or tissue imaging or therapy purposes. Some preferred aspects of the disclosure involve the preparation of trisuccin, chemical name N-?tris(2-N- benzyloxyaminocarbonylethyl)! methylsuccinamic acid, which is a hydroxamic acid/succinate based structure that is particularly useful for binding radionuclides such as .sup.99m Tc, .sup.186 Re and .sup.67 Cu.Type: GrantFiled: April 16, 1993Date of Patent: May 26, 1998Inventors: Ahmad Safavy, Donald J. Buchsbaum, Mohammad Bagher Kazaeli
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Patent number: 5714631Abstract: A group of functionalized amine chelants having ortho ligating functionality that form complexes with rare-earth type metal ions are disclosed. The complexes can be covalently attached to an antibody or antibody fragment and used for therapeutic and/or diagnostic purposes. In addition certain of the chelant-radionuclide complexes can be effectively employed in compositions useful as therapeutic and/or diagnostic agents for calcific tumors and/or relief of bone pain.Type: GrantFiled: February 6, 1996Date of Patent: February 3, 1998Assignee: The Dow Chemical CompanyInventors: David A. Wilson, Joseph R. Garlich, R. Keith Frank, Kenneth McMillan, Jaime Simon
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Patent number: 5710282Abstract: The present invention provides a novel one-step process for preparing substituted aryls which can be used as end-capping monomers for preparing highly branched macromolecule polymers that have highly controlled molecular architectures. The process comprises the steps of (a) reacting an aromatic acid with an activating carbodiimide for a sufficient period of time and under suitable conditions of temperature and pressure to form an activated aromatic intermediate, and (b) reacting said intermediate with a suitable nucleophile for a sufficient period of time and under suitable conditions of temperature and pressure to form said substituted aryl compound.Type: GrantFiled: August 18, 1995Date of Patent: January 20, 1998Assignee: Hoechst Celanese CorporationInventors: Kathleen Nelson Juneau, Richard Vicari, Carl David Murphy