Amide In Acid Moiety Patents (Class 560/41)
-
Patent number: 6339170Abstract: Optically active N-(S-2-acetylthiomethyl-1-oxo-3-phenylpropyl)-glycine benzyl ester useful as an enkephalin inhibitory agent or ACE inhibitory agent can be produced at low cost in an industrial manner, by a method comprising subjecting optically active 2-hydroxymethyl-3-phenylpropionic acid and glycine benzyl ester to condensation to subsequently convert the hydroxyl group into an elimination group, and substituting the elimination group with an acetylthio group.Type: GrantFiled: March 20, 2001Date of Patent: January 15, 2002Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Suzuki, Takayuki Hamada, Kunisuke Izawa
-
Patent number: 6335461Abstract: In the separation and purification of N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine methyl ester produced in the reductive alkylation of aspartame (APM) with 3,3-dimethylbutylaldehyde, the APM used in the starting material for the alkylation, which is difficult to be separated by recrystallization only from the crude crystals of the reaction product, can be separated and removed by extraction or solution thereof with the specified organic solvent from the concentrated reaction solution of the reductive alkylation or from the crude crystals of the product therefrom, and further N,N-di(3,3-dimethylbutyl)-APM as the by-product can be separated and removed by means for separation and purification, such as crystallization, chromatography, extraction, treatment with the activated charcoal, etc.Type: GrantFiled: February 29, 2000Date of Patent: January 1, 2002Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Tadashi Takemoto
-
Patent number: 6333427Abstract: A purified N-t-butoxycarbonylphenylalanine ester preparation having an enhanced optical activity can be obtained by bringing an N-t-butoxycarbonylphenylalanine ester preparation containing an optically active compound into contact with an aliphatic hydrocarbon, extracting the optically active compound with the aliphatic hydrocarbon, and recovering the optically active compound from the resulting extract.Type: GrantFiled: February 22, 2000Date of Patent: December 25, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Hitoki Miyake, Masami Osabe, Mitsuo Koito, Setsuo Yoshino, Nobuhiro Fukuhara
-
Patent number: 6331646Abstract: A novel amorphous N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester compound is disclosed. Also disclosed are processes for preparing the compound. The novel compound has improved solubility and dissolution properties compared to the known monohydrate.Type: GrantFiled: November 19, 1999Date of Patent: December 18, 2001Assignee: The NutraSweet Co.Inventors: Steve A. Schroeder, Run Wang
-
Publication number: 20010046663Abstract: A method to determine whether a test compound modulates the activity of an enzyme that has a metallated active site, comprising:Type: ApplicationFiled: May 27, 1999Publication date: November 29, 2001Inventors: PAUL G. GROTHAUS PH.D, DANA E. DAVIS, SEAN O'MALLEY
-
Patent number: 6316656Abstract: The invention includes selected novel optically active &agr;-ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: GrantFiled: July 5, 2000Date of Patent: November 13, 2001Assignee: Monsanto CompanyInventor: John J. Talley
-
Patent number: 6316657Abstract: There is provided a process for purification of N-(3,3-dimethylbutyl)-&agr;-L-aspartyl-L-phenylalanine methyl ester comprising the step of contacting impure N-(3,3-dimethylbutyl)-&agr;-L-aspartyl-L-phenylalanine methyl ester containing at least &agr;-L-aspartyl-L-phenylalanine methyl ester as an impurity, with the mixed solvents having two layers of one layer given from at least one organic solvent which does not mix with water homogeneously and one layer of water to extract N-(3,3-dimethylbutyl)-&agr;-L-aspartyl-L-phenylalanine methyl ester in the organic solvent layer. In the present invention, the desired compound can be purified or recovered efficiently in a high yield without using burdensome steps or operations.Type: GrantFiled: March 13, 2000Date of Patent: November 13, 2001Assignee: Ajinomoto Co., Inc.Inventor: Tadashi Takemoto
-
Publication number: 20010039293Abstract: Compounds which are specific or selective agonists of RAR&agr; receptors in preference over RAR&bgr; and RAR&ggr; receptors, and particularly compounds of the formula 1Type: ApplicationFiled: April 2, 2001Publication date: November 8, 2001Applicant: Allergan Sales, Inc.Inventors: Alissar Nehme, Richard L. Beard, Roshantha A. Chandraratna
-
Patent number: 6306881Abstract: Compounds of general formula (I) wherein R4 is an ester or thioester group and R, R1, R2, and R3 are as specified in the description, inhibit intracellular Leukotriene A4 hydrolase activity and are therefore of value for the treatment of inflammatory disease.Type: GrantFiled: July 21, 1999Date of Patent: October 23, 2001Assignee: British Biotech PharmaceuticalsInventors: Andrew Paul Ayscough, Mark Whittaker
-
Patent number: 6294686Abstract: The invention provides a method of preparing new crystal forms of aspartame utilizing microemulsions comprising: (a) introducing aspartame into a microemulsion formed from an oil phase, an aqueous phase and at least one emulsifier, (b) destabilizing the microemulsion to effect recrystallization of aspartame; (c) separating solid phase crystals from the liquid phase in which they are contained; and (d) cleaning the crystals to remove traces of the oil phase and surfactant.Type: GrantFiled: June 28, 2000Date of Patent: September 25, 2001Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Helga F. Milhofer, Nissim Garti, Alexey Kamishny
-
Patent number: 6291478Abstract: The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a composition comprising a physiologically acceptable medium, in particular in order to prevent and/or treat certain cutaneous disorders and more particularly in order to treat sensitive skins.Type: GrantFiled: March 13, 2000Date of Patent: September 18, 2001Assignee: L'OrealInventors: Jean-Baptiste Galey, Maria Dalko
-
Patent number: 6291004Abstract: Dipeptide sweeteners are disclosed that are basic salts of N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester represented by the formula wherein Xm+ is selected from the group consisting of Na+, K+, Al3+, Fe2+, Fe3+, Ca2+, Mg2+, NH4+ and Zn2+; Qs− absent or a physiologically acceptable counter anion; and m−s=n. Also disclosed is a liquid low-calorie sweetener containing such basic salts.Type: GrantFiled: September 4, 1998Date of Patent: September 18, 2001Assignee: The NutraSweet CompanyInventors: Indra Prakash, Kurt L. Wachholder
-
Publication number: 20010020097Abstract: 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: ApplicationFiled: March 30, 1999Publication date: September 6, 2001Inventors: JAMES E. AUDIA, BEVERLY K. FOLMER, VARGHESE JOHN, LEE H. LATIMER, JEFFREY S. NISSEN, WARREN J. PORTER, EUGENE D. THORSETT, JING WU
-
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
-
Patent number: 6281380Abstract: N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester is produced by reductive alkylation and crystallization/isolation in methanol and water. The production method is efficient and low cost, as compared with conventional N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester synthesis and results in high purity N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester.Type: GrantFiled: May 18, 2000Date of Patent: August 28, 2001Assignee: The Nutra Sweet CompanyInventors: Indra Prakash, Mike G. Scaros, Kurt L. Wachholder
-
Publication number: 20010014754Abstract: Optically active N-(S-2-acetylthiomethyl-1-oxo-3-phenylpropyl)-glycine benzyl ester useful as an enkephalin inhibitory agent or ACE inhibitory agent can be produced at low cost in an industrial manner, by a method comprising subjecting optically active 2-hydroxymethyl-3-phenylpropionic acid and glycine benzyl ester to condensation to subsequently convert the hydroxyl group into an elimination group, and substituting the elimination group with an acetylthio group.Type: ApplicationFiled: March 20, 2001Publication date: August 16, 2001Applicant: AJINOMOTO CO., INC.Inventors: Takayuki Suzuki, Takayuki Hamada, Kunisuke Izawa
-
Patent number: 6262302Abstract: 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: GrantFiled: September 17, 1999Date of Patent: July 17, 2001Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
-
Patent number: 6262114Abstract: Novel amidinophenol derivatives of formula (IB) and processes for the preparation thereof; compositions containing a compound of formula (IB) as active ingredient useful as antagonists of leukotine B4 and inhibitors of phospholipase A2 and/or trypsin; methods for preventing or treating diseases induced by phospholipase A2 and/or trypsin comprising administering to a patient a compound of formula (IB); and methods for treating diseases induced by leukotine B4 comprising administering to a patient a compound of formula (IB) or a known amidinophenol derivative of formula (IA)Type: GrantFiled: November 21, 1997Date of Patent: July 17, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Koumei Kamiyasu
-
Patent number: 6248919Abstract: A process for the preparation of preparation of farnesyltransferase inhibitors of formula (I) or pharmaceutically acceptable salts or prodrugs thereof, is disclosed.Type: GrantFiled: October 5, 1999Date of Patent: June 19, 2001Assignee: Abbott LaboratoriesInventors: Todd S. McDermott, Anne E. Bailey, Ramiya Premchandran, Lakshima Bhagavatula
-
Patent number: 6245922Abstract: A photoactive compound that is the reaction product of an alkenyl azlactone compound and a nucleophilic aromatic ketone is described. Mer units derived from this compound can be used, for example, to crosslink via a hydrogen abstracting mechanism acrylic polymers in which they are incorporated.Type: GrantFiled: November 19, 1996Date of Patent: June 12, 2001Assignee: 3M Innovative Properties CompanyInventors: Steven M. Heilmann, Gaddam N. Babu, Larry R. Krepski, Howell K. Smith, II, Daniel E. Mickus
-
Patent number: 6245934Abstract: Method for preparing a salt of aspartylphenylalanine methyl ester from N-protected aspartylphenylalanine methyl ester involving cleaving off the protective group by treatment with an acid, in the course of which, first of all, N-protected aspartylphenylalanine methyl ester is caused to react in an aqueous medium and in the presence of methanol at a temperature of from 0 to 80° C. with from 0.8 to 2 equivalents of acesulphamic acid for at least such a time that the conversion to the salt of aspartylphenylalanine methyl ester and acesulphamic acid has been completed to an adequate degree, and then the salt formed in the first step is isolated in precipitated form at a temperature of 30° C. or lower.Type: GrantFiled: December 6, 1999Date of Patent: June 12, 2001Assignee: DSM NVInventors: Jacob Van Soolingen, Wilhelmus H. J. Boesten
-
Patent number: 6235929Abstract: A novel class of tripeptide &agr;-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M1—AA—AA—AA—CO—NR3R4.Type: GrantFiled: December 27, 1996Date of Patent: May 22, 2001Assignee: Georgia Tech Research CorporationInventor: James C Powers
-
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
-
Patent number: 6218432Abstract: 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.Type: GrantFiled: July 14, 1999Date of Patent: April 17, 2001Assignee: L'OrealInventors: Jean-Baptiste Galey, Jacqueline Dumats
-
Patent number: 6211235Abstract: 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: GrantFiled: September 30, 1998Date of Patent: April 3, 2001Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: 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
-
Patent number: 6207710Abstract: 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: GrantFiled: September 30, 1998Date of Patent: March 27, 2001Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Thomas C. Britton, James J. Droste, Beverly K. Folmer, George W. Huffman, Varghese John, Lee H. Latimer, Thomas E. Mabry, Jeffrey S. Nissen, Warren J. Porter, Jon K. Reel, Eugene D. Thorsett, Jay S. Tung, Jing Wu
-
Patent number: 6201023Abstract: A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of &bgr;-amino butyric acid or derivatives thereof to the crop or its locus.Type: GrantFiled: June 10, 1997Date of Patent: March 13, 2001Assignee: Agrogene Ltd.Inventors: Yuji Oka, Yitzhak Spiegel, Yigal Cohen
-
Patent number: 6180156Abstract: Dipeptide sweeteners are disclosed that are salts of N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester represented by the formula wherein X− is selected from the group consisting of Cl−, HSO4−, H2PO3−, citrate, HCO3−, furmarate, malate, maleiate, tartarate, acetate, benzoate or gluconate. Also disclosed is a liquid low-calorie sweetener containing such salts.Type: GrantFiled: September 4, 1998Date of Patent: January 30, 2001Assignee: The NutraSweet CompanyInventors: Indra Prakash, Kurt L. Wachholder
-
Patent number: 6166229Abstract: Amino acids are derivatized for use in peptide synthesis by conversion to N-carboxyanhydrides that are N-protected by either a trityl or a phenylfluorenyl group.Type: GrantFiled: April 24, 2000Date of Patent: December 26, 2000Assignee: The Regents of the University of CaliforniaInventors: Henry Rapoport, Tae Bo Sim
-
Patent number: 6162828Abstract: A pharmaceutical composition for inhibiting cysteine protease which comprises a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an acyl group; R.sup.2, R.sup.3 and R.sup.4, same or different, are a bond, an amino acid residue or a group of the formula:--Y--R.sup.5 --in which R.sup.5 is a group resulting from imino group removal from an amino acid residue;Y is --O--, --S-- or --NR.sup.6 -- in which R.sup.6 is a hydrogen atom or a lower alkyl group;A is ##STR2## Z is a hydrogen atom, an acyl group or an optionally substituted hydrocarbon group; n is 1 or 2;provided that when n is 1, then A is ##STR3## and Y is --S-- or --NR.sup.6 --, and, at least one of R.sup.2, R.sup.3 and R.sup.4 is the formula --Y--R.sup.5 --, provided that when further all Y are --NR.sup.6 --, at least one of the amino acid residues is not bound to amhydrogen atom at the .alpha.-carbon thereof but substituted via carbon;provided that when n is 2 and Z is an aldehyde group, then R.sup.Type: GrantFiled: May 20, 1996Date of Patent: December 19, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsunehiko Fukuda, Yukio Fujisawa, Hiroyuki Watanabe
-
Patent number: 6162933Abstract: A process for the preparation of amido acid phenyl esters of the formula ##STR1## by reaction of a compound of the formula ##STR2## with a compound of the formula ##STR3## in the presence of an acid halide, where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and M are as defined in the description, is claimed. The resulting amido acid phenyl esters are used as bleach activators in detergents and cleaners.Type: GrantFiled: July 30, 1999Date of Patent: December 19, 2000Assignee: Clariant GmbHInventors: Michael Seebach, Peter Naumann, Werner Janitschek
-
Patent number: 6153652Abstract: Disclosed are compounds which inhibit .beta.-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 .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: November 21, 1997Date of Patent: November 28, 2000Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
-
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
-
Patent number: 6146680Abstract: Dipeptide sweeteners are disclosed that are metal complexes of N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester represented by the formula ##STR1## wherein X.sup.p+ is selected from the group consisting of Al.sup.3+, Fe.sup.2+, Fe.sup.3+, Ca.sup.2+, Mg.sup.2+ and Zn.sup.2+ ; Y.sup.q- is selected from the group consisting of Cl.sup.-, SO.sub.4.sup.2-, PO.sub.4.sup.3- and CH.sub.3 COO.sup.- ; x is a number from 1 to 4 and pn=qm. Also disclosed is a liquid low-calorie sweetener containing such metal complexes.Type: GrantFiled: September 4, 1998Date of Patent: November 14, 2000Assignee: The NutraSweet CompanyInventors: Indra Prakash, Zhi Guo
-
Patent number: 6133464Abstract: The invention relates to chiral ferrocenyls of formula (I) ##STR1## wherein R.sub.a is --P(R.sub.10 R.sub.11) or --SR.sub.12 ;R.sub.b is --P(R'.sub.10 R'.sub.11), --SR'.sub.12, --CH.dbd.NR.sub.12, --CH.sub.2 --NH--R.sub.12 or --CH.sub.2 --O--P(R.sub.10 R.sub.11); and the other substituents are as defined in claim 1,which may be used as ligands for transition metal catalysts in enantioselective reactions.Type: GrantFiled: March 8, 1999Date of Patent: October 17, 2000Assignee: Novartis AGInventors: Benoit Pugin, Heidi Landert, Giorgio Pioda
-
Patent number: 6129942Abstract: Dipeptide sweeteners are disclosed that are sweetener salts of N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester represented by the formula ##STR1## wherein X.sup.m- is a conjugate base derived by deprotonation of an acidic sweetener, preferably saccharin, acesulfame, cyclamic acid and glycyrrhizic acid; and m=n. Also disclosed is a liquid low-calorie sweetener containing such basic salts.Type: GrantFiled: September 4, 1998Date of Patent: October 10, 2000Assignee: The NutraSweet CompanyInventors: Indra Prakash, Zhi Guo
-
Patent number: 6127569Abstract: Disclosed is a method of crystallizing .alpha.-L-aspartyl-L-phenylalanine methyl ester, which is a sweetening agent substituting sugar and commonly referred to as aspartame. An aspartame solution is sprayed and droplets of the solution fall downward. Cold airflow is blown to the falling droplets of the aspartame solution to cool them. The aspartame dissolved in the droplets crystallizes, and the slurry including the aspartame crystals and the remaining solution is collected for further processes. Also disclosed is a crystallizer for cooling crystallizing the aspartame solution with this method. The crystallizer has an atomizer for spraying the aspartame solution supplied thereto and an air inlet and an air outlet. The cold air is blown into the crystallizer through the air inlet, cools the droplets of the aspartame solution, and is discharged through air outlet.Type: GrantFiled: October 30, 1998Date of Patent: October 3, 2000Assignee: Daesang CorporationInventors: Hwa Jung Dho, Heon Yong Eohm, Kyung Eun Choi, Bun Sam Lim
-
Patent number: 6107512Abstract: The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: GrantFiled: October 10, 1995Date of Patent: August 22, 2000Assignee: Monsanto CompanyInventor: John J. Talley
-
Patent number: 6100422Abstract: Disclosed is a method of crystallizing .alpha.-L-aspartyl-L-phenylalanine methyl ester, which is a sweetening agent substituting sugar and commonly referred to as aspartame. An aspartame solution is gradually cooled by heat exchanging with a coolant passing by with each other in the opposite direction. This enables that the heat-exchange between the aspartame solution and the coolant occurs at small and almost constant temperature difference. The cooling crystallization with such small temperature difference provides coarse and uniform aspartame crystals. Also, the aspartame solution is forcedly stirred such that crystals and crystal lumps formed are not re-dissolved or broken down. The forced stir of the solution makes the crystals and the lumps be suspended in the solution, which prevents formation of scales on any surfaces.Type: GrantFiled: November 12, 1998Date of Patent: August 8, 2000Assignee: Daesang CorporationInventors: See Young Yu, Jin Man Cho, Bun Sam Lim
-
Patent number: 6096762Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel .alpha.,.alpha.-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: May 21, 1999Date of Patent: August 1, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Gene M. Dubowchik, Bireshwar Dasgupta, Dolatrai M. Vyas
-
Patent number: 6096782Abstract: Disclosed are compounds which inhibit .beta.-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 .beta.-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: GrantFiled: November 21, 1997Date of Patent: August 1, 2000Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Warren J. Porter, Eugene D. Thorsett, Jing Wu
-
Patent number: 6093831Abstract: Amino acids are derivatized for use in peptide synthesis by conversion to N-carboxyanhydrides that are N-proected by either a trityl or a phenylfluorenyl group.Type: GrantFiled: February 26, 1999Date of Patent: July 25, 2000Assignee: The Regents of the University of CaliforniaInventors: Henry Rapoport, Tae Bo Sim
-
Patent number: 6090972Abstract: Disclosed is a method of cooling and crystallizing .alpha.-L-aspartyl-L-phenylalanine methyl ester, which is a sweetening agent, commonly referred to as aspartame. An aspartame solution is cooled such that the solution is flown while being continuously in thermal contact with a coolant. As the cooling of the aspartame solution by the thermal contact with the coolant proceeds, the temperature difference between the aspartame solution and the coolant remains substantially constant. The coolant flows in the opposite direction as the aspartame solution flows and cools an upstream part of the aspartame solution as the coolant flows downstream.Type: GrantFiled: July 19, 1999Date of Patent: July 18, 2000Assignee: Daesang CorporationInventors: See Young Yu, Jin Man Cho, Bun Sam Lim
-
Patent number: 6084065Abstract: The present invention relates to oligopeptidic compounds having the general formula (I):K--[--A--].sub.z --[--B--].sub.w --L (I)The compounds having general formula (I) are antifungals for agricultural purposes.Type: GrantFiled: October 4, 1994Date of Patent: July 4, 2000Assignee: Isagro SpaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Ernesto Signorini
-
Patent number: 6077962Abstract: This invention relates to the chemical synthesis of N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester using peptide coupling methods. The coupling reaction is conducted by condensation of an activated derivative of novel N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester or by enzymatic coupling of N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester. This invention also relates to novel N-(3,3-dimethylbutyl)-L-aspartic acid, derivatives thereof and the preparation thereof. The activated derivative of N-neohexyl-L-aspartic acid may be an anhydride, mixed anhydride, active ester or an intermediate activated derivative thereof.Type: GrantFiled: December 24, 1998Date of Patent: June 20, 2000Assignee: The NutraSweet CompanyInventors: Indra Prakash, Marie-Christine D. Chapeau
-
Patent number: 6075055Abstract: A phenylalkane amide compound having the formula (1): ##STR1## wherein R.sup.1 -R.sup.4, X, n, Y, Z and Q are as defined herein. The compound is useful as an agricultural or horticultural fungicide.Type: GrantFiled: December 1, 1997Date of Patent: June 13, 2000Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Katsumi Masuda, Ikumi Urushibata, Tsuyoshi Asahara, Katsumi Furuse, Yoshiyuki Kojima, Hiroshi Abe
-
Patent number: 6063962Abstract: This invention relates to an improved process for the production of known amine compounds which are useful as medicaments.Type: GrantFiled: February 24, 1998Date of Patent: May 16, 2000Assignee: Astra Pharmaceuticals LimitedInventor: Alan Richard Harris
-
Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
-
Patent number: 6051584Abstract: Novel compounds of the general formula (I) which have hemoregulatory activities and can be used to stimulate haematopolesis and for the treatment of viral, fungal and bacterial infectious diseases ##STR1##Type: GrantFiled: November 23, 1998Date of Patent: April 18, 2000Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbHInventors: Pradip Kumar Bhatnagar, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
-
Patent number: 6046235Abstract: A sulfur-containing amino acid compound having a high inhibitory activity on LTA.sub.4 hydrolase which is represented by the following formula: ##STR1## wherein R.sup.1 represents H, alkyl, optionally substituted phenyl alkyl, alkanoyl or optionally substituted benzoyl; R.sup.2 represents ester, amide or carboxyl; R.sup.3 represents hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, optionally substituted phenyl, optionally substituted phenoxy, optionally substituted phenylthio, halogen atom, alkylsulfonyl, halogenoalkylsulfonyl, nitro or cyano; R.sup.4 represents alkyl; A.sup.1 represents alkylene; and A.sup.2 represents alkylene.Type: GrantFiled: March 1, 1999Date of Patent: April 4, 2000Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Masato Horiuchi, Kenichi Fujimura, Hiroshi Suhara