Abstract: Processes for using modifying catalysts with improved functionality in the production of neotame are disclosed. The modified catalysts surprisingly have been found to improve the selectivity over conventional catalysts and to reduce the level of certain impurities in neotame production processes.
Abstract: 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:
Grant
Filed:
August 12, 1994
Date of Patent:
May 6, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Walter Lange, Michael Grosse-Bley, Bruno Bömer, Rolf Grosser, Franz-Peter Hoever
Abstract: Low-calory sweeteners comprising novel aspartyl dipeptide ester derivatives and their salts have a sweetening potency of up to 35000 times that of sugar and include compounds such as N-[N-[3-(3-methyl-4-hydroxyphenyl)propyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester and N-[N-[3-(3-hydroxy-4-methoxyphenyl)propyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester.
Abstract: According to the invention, N-butyryl-4amino-3-methyl-methyl benzoate is obtained in a particularly advantageous manner by, initially, reacting o-toluidine with butyric acid chloride, by brominating the reaction product and by reacting the bromide obtained therefrom with carbon monoxide and methanol in the presence of a palladium catalyst. The invention also relates to the important novel chemical compound N-(4-bromine-2-methylphenyl)-butanamide.
Type:
Application
Filed:
September 24, 2002
Publication date:
April 3, 2003
Inventors:
Lars Rodefeld, Thomas Hopfner, Alexander Klausener, Horst Behre
Abstract: Aspartyl dipeptide ester derivatives, such as a N-[N-[3-(3,4-dihydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, or salts thereof, having a high degree of sweetness compared to conventional sweeteners. These derivatives are excellent in sweetening potency and may be used as sweetener components in products such as foods and drinks. They may also be used as low calorie sweeteners and in methods of sweetening products. Foods and drinks comprising these derivatives as well as methods for their production.
Abstract: The invention relates to novel amino- and amido-diphenyl ethers, processes for their preparation and their use in pharmaceuticals, in particular for the indications of arteriosclerosis and hypercholesterolaemia.
Type:
Application
Filed:
July 31, 2001
Publication date:
February 6, 2003
Inventors:
Helmut Haning, Josef Pernerstorfer, Gunter Schmidt, Michael Woltering, Hilmar Bischoff, Verena Vohringer, Axel Kretschmer, Christiane Faeste
Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) useful for oral testosterone replacement therapy. Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds bind reversibly to the androgen receptor.
Type:
Application
Filed:
February 28, 2002
Publication date:
January 30, 2003
Inventors:
James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
Abstract: The present invention is a process to prepare on of a phenylisoserine ester of the formula (II)
&phgr;—CH(NH—CO—CH3)—CH(OH)—CO—O—R1
with reduced amount of diol by-product by the use of a compound of the formula R2—CO—NH2 where R2 is C1-C6 alkyl with the proviso that R2 is not tertiary.
Abstract: 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:
Application
Filed:
May 3, 2002
Publication date:
January 16, 2003
Inventors:
Bing Wang, Guy Miller, Wei Zhang, Satyanarayana Janagani, Jiangao Song
Abstract: N-[N-[3-(3-hydroxy-4-methoxyphenyl)propyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester useful as a sweetener with a high potency of sweetness, is provided in the crystalline form having a high stability and a good purity which is favorable as a commercial product.
Abstract: New secondary amines are described which are prepared from inexpensive, commercially available raw materials, are stable at room temperature, and are reactive toward electrophiles. The secondary amines are prepared by the addition of one or more primary amines with one or more male (amide/ester) and fumar (amide/ester) Michael receptors. The above amines can be used as coreactants with aliphatic polyisocyanates for polyurea coatings. The novel secondary amines are also described as particularly useful as part of a two-part liquid pavement marking composition for pavement markings.
Type:
Application
Filed:
July 22, 2002
Publication date:
January 2, 2003
Applicant:
3M Innovative Properties Company
Inventors:
Richard G. Hansen, Dean M. Moren, Mark D. Purgett
Abstract: Disclosed in the present application are a method for preparing highly-stable A-type crystals by controlling and maintaining the product temperature of B-type N-(3,3-dimethylbutyl)-APM crystals at 25 to 80° C. under an absolute humidity of 0.203 kg/kg or less environment, thereby effecting crystal transition; and a method for preparing A-type crystals by controlling and maintaining the product temperature of D-type crystals of N-(3,3-dimethylbutyl)-APM at 25 to 80° C. under an absolute humidity of 0.0550 kg/kg or less environment, thereby effecting crystal transition. According to these crystal transition methods, highly stable crystals can be prepared stably and at a low cost.
Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Type:
Grant
Filed:
March 30, 1999
Date of Patent:
December 17, 2002
Assignees:
Athena Neurosciences, Inc., Eli Lilly & Company
Inventors:
James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Warren J. Porter, Eugene D. Thorsett, Jing Wu
Abstract: Compounds for treating diseases by altering mitochondrial function that affects cellular processes, as well as to compositions and methods related thereto.
Type:
Application
Filed:
December 14, 2001
Publication date:
November 21, 2002
Applicant:
MitoKor
Inventors:
Yazhong Pei, Walter H. Moos, Soumitra S. Ghosh
Abstract: Novel alkylenediaminediacetic acid or alkylenediaminetriacetic derivatives of formula (I):
or an organic or inorganic salt thereof, their process of preparation, and their use in cosmetic and pharmaceutical compositions, such as for protecting the body against oxidative stress are discussed.
Abstract: The present invention relates to small molecules according to the formula [I]:
which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.
Type:
Grant
Filed:
June 23, 1998
Date of Patent:
November 19, 2002
Assignees:
Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn Company
Inventors:
Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.
Type:
Application
Filed:
January 25, 2002
Publication date:
November 7, 2002
Inventors:
Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis.
Type:
Grant
Filed:
April 3, 2001
Date of Patent:
November 5, 2002
Assignees:
Elan Pharmaceuticals, Inc., Eli Lilly Company
Inventors:
Jing Wu, Jay S. Tung, Eugene D. Thorsett, Jon K. Reel, Warren J. Porter, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Varghese John, Beverly K. Folmer, James J. Droste, Thomas C. Britton, James E. Audia
Abstract: The synthesis of N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester via conversion under reducing conditions of novel imidazolidinone(s) is disclosed.
Type:
Grant
Filed:
November 17, 1999
Date of Patent:
October 15, 2002
Assignee:
The NutraSweet Company
Inventors:
Vladislav Orlovski, Indra Prakash, Mike G. Scaros, Christine M. V. Moore
Abstract: One aspect of the present invention relates to 2-hydroxymethylglutamic acid and congeners thereof. A second aspect of the invention relates to a method of synthesizing 2-hydroxymethylglutamic acid and congeners thereof.
Abstract: 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:
Application
Filed:
June 22, 2001
Publication date:
October 3, 2002
Inventors:
Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Type:
Application
Filed:
October 31, 2001
Publication date:
September 26, 2002
Inventors:
Jing Wu, Eugene D. Thorsett, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Varghese John, Lawrence Y. Fang, James E. Audia
Abstract: The present invention relates to a method of manufacturing aspartyl dipeptide ester compounds, which can be used as sweeteners, and aldehydes that can be used in the manufacturing processes.
Abstract: In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.
Type:
Grant
Filed:
February 28, 2001
Date of Patent:
August 13, 2002
Assignee:
Gene Therapy Systems, Inc.
Inventors:
Philip L. Felgner, Xiang Gao, Jing Ling
Abstract: Compounds of Formula I, and pharmaceutical compositions containing these compounds, activate the insulin receptor kinase, which leads to an increased sensitivity to insulin and an increase in glucose uptake, and are therefore useful for the treatment of animals, especially humans, with hyperglycemia, especially for the treatment of type 2 diabetes. Processes for preparation of the compounds, and their use in assays, are also disclosed.
Type:
Application
Filed:
September 6, 2001
Publication date:
August 1, 2002
Inventors:
Louise Robinson, Prasad V.V.S.V. Manchem, Nicolas Cairns, Steven R. Schow
Abstract: N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester is crystallized in order to give highly pure product in high yield. In a preferred embodiment of the present invention, N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester is crystallized directly from an aqueous methanol reaction mixture.
Type:
Grant
Filed:
November 24, 1999
Date of Patent:
July 23, 2002
Assignee:
The NutraSweet Company
Inventors:
Indra Prakash, Christine M. V. Moore, Kurt Wachholder
Abstract: An amide compound of the formula (I):
wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.
Abstract: The present invention relates to a composition comprising a first monomer having the formula CH2═CHCOOR1, where R1 is a linear alkyl group having from 9 to 16 carbon atoms or a branched alkyl group having from 9 to 30 carbon atoms, and whose homopolymer has a Tg less than 0° C.; and/or a second monomer having the formula CH2═CHCOOR2, where R2 is an alkyl group having at least 9 carbon atoms whose homopolymer has a Tg greater than 15° C.; and a third component which may be another monomer, a polymer, surface-modified particles, or combinations thereof as well as article comprising the composition.
Type:
Grant
Filed:
June 28, 2000
Date of Patent:
July 9, 2002
Assignee:
3M Innovative Properties Company
Inventors:
David S. Arney, Richard E. Bennett, Babu N. Gaddam, Steven M. Heilmann, Brant U. Kolb, Larry R. Krepski, David B. Olson
Abstract: 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:
Grant
Filed:
June 11, 2001
Date of Patent:
June 4, 2002
Assignee:
Pfizer INC
Inventors:
Thomas G. LaCour, Charles William Murtiashaw, III
Abstract: New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I,
wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.
Type:
Grant
Filed:
December 28, 1999
Date of Patent:
May 28, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Elisabeth Defossa, Uwe Heinelt, Otmar Klingler, Gerhard Zoller, Hans Matter, Fahad A. Al-Obeidi, Armin Walser, Peter Wildgoose
Abstract: New thyroid receptor ligands are provided which have the general formula
in which:
X is —O—, —S—, —CH2—, —CO—, or —NH—;
R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons;
R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen;
R4 is methyl, ethyl, n-propyl or trifluoromethyl;
R5 is hydrogen or lower alkyl;
R6 is carboxylic acid, or esters or prodrugs;
R7 is hydrogen or an alkanoyl or an aroyl.
In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
Abstract: Process for preparing benzenesulfonate salts from an appropriately substituted acid chloride and a hydroxybenzenesulfonic acid is conducted in the absence of solvent, in a molar excess of acid chloride and in the presence of a phase transfer catalyst selected from quaternary ammonium and quaternary phosphonium salts and the target reaction product. The molar excess of the acid chloride is used to reduce the occurrence of gelation in the product.
Type:
Application
Filed:
November 15, 2001
Publication date:
May 16, 2002
Inventors:
Victoria Ann Majerczak, Michael Steven Gibson, Robert James Orlando
Abstract: A compound of the formula (I):
wherein:
for example, a compound below:
wherein:
R1 is CH3, H or Na; and X1—X2—X3 is:
or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.
Abstract: It has now been found that N-L-alpha-aspartyl-L-phenylalanine 1-methyl ester (APM) exhibits antisickling properties. In vitro testing verified that APM significantly lowered the frequency of sickling of red blood cells from each of twelve pediatric aged patients being treated for sickle-cell anemia by exchange transfusion. Sickling was also inhibited in an “index” patient after oral administering of APM. These in vitro and in vivo results identify APM as a therapeutic agent for the family of sickle cell molecular diseases.
Abstract: Compounds of formula I activate the insulin receptor kinase. Pharmaceutical compositions comprising the compounds, and methods of treatment of hyperglycemia and other diseases involving imbalance of glucose levels, especially for the treatment of type II diabetes, by administering these compounds to mannnalian hosts, and processes for their preparation, are also described.
Type:
Application
Filed:
May 31, 2001
Publication date:
March 14, 2002
Inventors:
John Patterson, Sophia Jeong-Weon Park, Robert T. Lum, Wayne R. Spevak
Abstract: The present invention comprises small molecular weight, non-peptidic inhibitors of formula I and II of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).
Type:
Grant
Filed:
August 24, 1998
Date of Patent:
March 5, 2002
Assignee:
Pharmacia & Upjohn Company
Inventors:
Scott D. Larsen, Paul D. May, John E. Bleasdale, Charlotta Liljebris, Heinrich Josef Schostarez, Tjeerd Barf
Abstract: A class of novel phenyl acetamides is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
Type:
Grant
Filed:
November 24, 1997
Date of Patent:
March 5, 2002
Assignee:
Eli Lilly and Company
Inventors:
Theodore Goodson, Jr., Richard Waltz Harper, David Kent Herron
Abstract: Haloacetoamido, benzoic acid derivatives having anti-tumorigenic activity. Examples of the haloacetoamido, benzoic acid derivatives include 3-chloroacetoamido, benzoylurea, 3-bromoacetoamido, benzoylurea, 3-iodoacetoamido, benzoylurea, ethyl-3-chloroacetoamido, benzoate, ethyl-3-bromoacetoamido, benzoate and ethyl-3-iodoacetoamido, benzoate. Intermediates for synthesizing the derivatives, along with method of making and using the derivatives, are also provided.
Type:
Application
Filed:
August 29, 2001
Publication date:
February 21, 2002
Inventors:
George J. Bekesi, Jian-Dong Jiang, Imre Weisz, John Roboz, James F. Holland
Abstract: Amphiphilic polyamide compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.
Type:
Grant
Filed:
November 24, 1999
Date of Patent:
February 19, 2002
Assignee:
Gene Therapy Systems, Inc.
Inventors:
Philip L. Felgner, Xiang Gao, Jing Ling
Abstract: 1 The present invention relates to a novel fatty acid derivative of formula (I), wherein R1 is acyl group; R2 is acyl(lower)alkyl; R3 is hydrogen, aryl(lower)alkyl, etc.; R4 is acyl(lower)alkyl; and X is —O—, —NH— or formula (II) [wherein R5 is lower alkyl, etc.]; and a pharmaceutically acceptable salt thereof, which is useful as a medicament; the processes for the preparation of said fatty acid derivative or a salt thereof; a pharmaceutical composition comprising said fatty acid derivative or a pharmaceutically acceptable salt thereof; etc.
Abstract: There is provided a novel mixed crystal comprising aspartame (APM) and N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine methyl ester, which can be used as a sweetener having considerably improved quality of sweetness, etc.
The above mixed crystal can be easily produced industrially by subjecting a solution containing the above-mentioned APM and APM derivative to a crystallizing operation followed by the separation of the mixed crystal thus precipitated.