Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
Abstract: Compounds for treating diseases by altering mitochondrial function that affects cellular processes, as well as to compositions and methods related thereto. The compounds have the structure
wherein R1, R2, R3 and A are as defined herein.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
April 22, 2003
Assignee:
MitoKor
Inventors:
Yazhong Pei, Walter H. Moos, Soumitra S. Ghosh
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: The present invention provides novel compounds of the Formula
and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.
Type:
Grant
Filed:
September 27, 2001
Date of Patent:
April 8, 2003
Assignee:
Pfizer Inc.
Inventors:
Yuan-Ching Phoebe Chiang, Robert L. Dow
Abstract: The present invention relates to a compound of the formula (I)
The compound according to the invention is suitable for the preparation of herbicidal active substances such as sulfonylureas.
Type:
Grant
Filed:
July 20, 2001
Date of Patent:
March 25, 2003
Assignee:
Aventis CropScience GmbH
Inventors:
Klaus Lorenz, Hans-Joachim Ressel, Lothar Willms
Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-&ggr; by adipose tissue.
Type:
Grant
Filed:
November 8, 1999
Date of Patent:
February 25, 2003
Assignee:
Calyx Therapeutics Inc.
Inventors:
Partha Neogi, Bishwajit Nag, Frederick J. Lakner, Debendranath Dey, Satyanarayana Medicherla
Abstract: The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.
Type:
Grant
Filed:
April 26, 2001
Date of Patent:
February 4, 2003
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Ramesh N. Patel, Amit Banerjee, Venkata B. Nanduri, Steven L. Goldberg, Robert M. Johnston, Thomas P. Tully, Laszlo J. Szarka, Shankar Swaminathan, John J. Venit, Jerome L. Moniot, William J. Winter, Neal G. Anderson, David A. Lust, Gerard Crispino, Sushil K. Srivastava
Abstract: Compounds of the formula (I) in which R1 is C1-10 allyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system
Type:
Grant
Filed:
November 16, 2001
Date of Patent:
January 7, 2003
Assignee:
Eli Lilly and Company
Inventors:
Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente
Abstract: Disclosed is a novel class of compounds of formula (I)
wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
Type:
Grant
Filed:
May 16, 2000
Date of Patent:
January 7, 2003
Assignee:
Noro Nordisk A/S
Inventors:
Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Josef Vagner, Inge Thøger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thøgersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Shenghua Shi
Abstract: Propanolamine derivatives represented by the following formula (I):
These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.
Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula:
wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
Type:
Grant
Filed:
January 12, 2001
Date of Patent:
November 5, 2002
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
Abstract: A process for the preparation of &agr;-(2,4-disulfophenyl)-N-tert-butylnitrone diacids and pharmaceutically acceptable salts thereof by the reaction of the corresponding disulfophenyl aldehyde with N-tert-butylhydroxylammonium acetate is disclosed.
Type:
Application
Filed:
April 5, 2001
Publication date:
September 12, 2002
Inventors:
Henry Kruk, John McGinley, Sergei Pouhov, John Vajda, Jorgen Blixt
Abstract: The invention relates to novel o-aminophenolcarboxylic acids or o-aminothiophenolcarboxylic acids of the following structure
in which:
A1 to A7 are—independently of one another—H, CH3, OCH3, CH2CH3 or OCH2CH3;
T is O or S, and m is 0 or 1;
Z is a carbocyclic or heterocyclic aromatic radical.
Abstract: Indane compounds of general formulae (1) to (4) and their pharmaceutical use, particularly to achieve mast cell stabilising activity and/or anti-inflammatory activity are described.
Type:
Grant
Filed:
December 3, 1999
Date of Patent:
August 13, 2002
Assignee:
Venantius Limited
Inventors:
Neil Frankish, Helen Sheridan, John Walsh, Michael Jordan
Abstract: 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.
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 12, 1999
Date of Patent:
June 4, 2002
Assignees:
Athena Neurosciences, Inc., Eli Lilly & Company
Inventors:
James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Jon K. Reel, Eugene D. Thorsett, Celia A. Whitesitt
Abstract: Ureins are obtained by reaction, in basic medium, between an N&ohgr;-(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.
Type:
Application
Filed:
September 4, 2001
Publication date:
May 16, 2002
Inventors:
Roland Callens, Georges Blondeel, Marc Anteunis, Frank Becu
Abstract: The present invention relates to a process for preparing a compound of the formula
wherein b, Y and R3 are defined as above, useful for preparing novel aralkyl and aralkylidene heterocyclic lactams and imides which are selective agonists and antagonists of serotonin 1 (5-HT1) receptors.
Type:
Grant
Filed:
March 28, 2000
Date of Patent:
May 14, 2002
Assignee:
Pfizer INC
Inventors:
George Joseph Quallich, Jeffrey William Raggon, Paul D. Hill
Abstract: Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
Type:
Grant
Filed:
June 1, 1999
Date of Patent:
April 30, 2002
Assignees:
Merck & Co., Inc., Tularik Inc.
Inventors:
Steven D. Young, Melissa Egbertson, Linda S. Payne, John S. Wai, Thorsten E. Fisher, James P. Guare, Jr., Mark W. Embrey, Lekhanh Tran, Linghang Zhuang, Joseph P. Vacca, H. Marie Langford, Jeffrey Melamed, Juan C. Jaen, David L. Clark, Julio C. Medina
Abstract: The present invention relates to a crystalline polymorph of 2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methylethyl]amino]ethyl]phenoxy]acetic acid having strong diffraction peaks (diffraction angle: 2&thgr;±0.1°) at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0° in powder X-ray diffraction pattern, which has potent &bgr;2- and &bgr;3-adrenoceptor stimulating effects and is useful as an agent for relieving pain and promoting the removal of calculi in urolithiasis, and the like. For example, the crystalline polymorph can be prepared by hydrolyzing ethyl 2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]-amino]ethyl]phenoxy]acetate phosphate by sodium hydroxide, adding an aqueous phosphoric acid solution at 40° C. and over, adding a mixed solvent of water and methanol or methanol to the resulting compound, and stirring the suspension at 40° C. to reflux temperature for 30 minutes to several hours.
Abstract: An aldehyde compound is reacted with an amino compound and hydrogen cyanate in the presence of a chiral zirconium catalyst obtained by mixing a zirconium alkoxide with an optically active binaphthol compound.
Type:
Grant
Filed:
July 13, 2001
Date of Patent:
January 15, 2002
Assignee:
Japan Science and Technology Corporation
Abstract: The naphthyloxyacetic acid derivatives of the formula (I)
wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)—(CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.
Abstract: The invention relates to compounds having the formula (I) or a pharmaceutically acceptable salt thereof. In the formula (I), X represents a group having the structural formula (II), and Y represents O or S. The compounds of the invention can be used a chloride channel blockers.
Abstract: The caged amino acid in accordance with the present invention has the structure represented by the following formula 1:
where X and Y each represent a halogen atom, an alkyl group, an alkyloxy group, an alkylamino group, or a benzo group; R1 represents a hydrogen atom or an alkyl group; R2 and R3 each represent a hydrogen atom or an alkyl group; A represents an amino acid residue; and M represents a hydrogen atom, an alkali metal, or an alkaline-earth metal.
Abstract: Compounds of formula (1) are described:
wherein
L1 is a covalent bond or a linker atom or group;
R is a carboxylic acid (—CO2H) or a derivative threof;
R6 and R7 which may be the same or different is each an atom or group —L2(Alk2)tL3R12 in which L2, L3, Alk2 and t are as previously defined and R12 is a hydrogen or halogen atom or an —OR9, —NR9R10, —NO2, —CN, —CO2R9, —CONR9R10, —COR9, —N(R9)COR10, —N(R9)CSR10, —SO2N(R9)(R10), —N(R9)SO2R9, —N(R9)CON(R10)(R11), —N(R9)CSN(R10)(R11), —N(R9)SO2N(R10)(R11), or an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group provided that R6 and R7 are not both hydrogen atoms and when R7 is a hydrogen atom then R4 and R5 is each a hydrogen or halogen atom or an alkyl, alkoxy or nitro group; and the salts, solvates, hydrates and N-oxides thereof, for use in modulating cell adhesion.
Type:
Grant
Filed:
March 16, 1999
Date of Patent:
December 11, 2001
Assignee:
Celltech Therapeutics Limited
Inventors:
Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
Abstract: The present invention provides novel compounds of the Formula
and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.
Type:
Grant
Filed:
February 28, 2000
Date of Patent:
December 4, 2001
Assignee:
Pfizer Inc.
Inventors:
Yuan-Ching Phoebe Chiang, Robert L. Dow
Abstract: Process for producing an optically active ester by reaction of a racemic alcohol with an optically active amino or tartaric acid derivative, a process for producing an optically active alcohol by hydrolysis of the optically active ester, a process for converting an alcohol into a ketone by oxidation, a method for stably storing an optically active ketone, and a new optically active amino acid ester and a new optically active tartaric acid ester.
Abstract: The invention relates to novel o-aminophenolcarboxylic acids or o-aminothiophenolcarboxylic acids of the following structure
in which:
A1 to A7 are—independently of one another—H, CH3, OCH3, CH2CH3 or OCH2CH3;
T is O or S, and m is 0 or 1;
Z is a carbocyclic or heterocyclic aromatic radical.
Abstract: 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 that bind to neutral sphingomyelinase and inhibit its activity.
Abstract: Methods, compositions, and devices for alleviating the problems of toxic discharge of aldehydes present in waste streams are disclosed. The methods relate to reducing neutralized aldehydes wherein the neutalized aldehydes are formed by treating aldehydes with amino acids and thereinafter are reduced. These reduced, neutralized aldehydes do not revert back to toxic aldehydes, but form amino acids and thus allow waste containing aldehyde to be more environmentally safely disposed.
Type:
Application
Filed:
December 22, 2000
Publication date:
September 27, 2001
Inventors:
Peter Zhu, Xiaolan Chen, Charles G. Roberts
Abstract: The present invention relates to an improved process for the hydrogenation of phthalic acids over a supported palladium catalyst. Phthalic acids are hydrogenated with improved selectivity in aqueous solution over palladium on carbon catalyst to give cyclohexanedicarboxylic acids (CHDA).
Type:
Grant
Filed:
June 17, 1999
Date of Patent:
September 18, 2001
Assignee:
Eastman Chemical Company
Inventors:
Charles Edwan Sumner, Jr., Bruce LeRoy Gustafson
Abstract: The present invention relates to a simple method for preparing a quinolinone derivative, which is effective as a medicine, e.g., as an agent for treating allergic diseases and the like; novel amide derivatives effective as an intermediate in the method, novel quinolinone derivatives obtained according to the method; and an anti-allergic agent containing a quinolinone derivative and/or physiological salt of the same as the active ingredients.
Abstract: The present invention relates to a hydrogenation process for the preparation of aromatic amino compounds containing directly on the aryl ring or in a side chain one or more entities that may also undergo hydrogenation, such as carbon multiple bonds, nitrile groups, imino groups or carbonyl groups. The preparation is carried out by catalytic hydrogenation of the corresponding aromatic nitro compounds in the presence of a phosphorus-modified noble metal catalyst. The invention relates also to the use of modified noble metal catalysts for the hydrogenation of aromatic nitro compounds containing carbon multiple bonds and/or substituted by nitrile, imino or carbonyl groups.
Type:
Grant
Filed:
March 10, 1999
Date of Patent:
July 10, 2001
Assignee:
Novartis AG
Inventors:
Peter Baumeister, Urs Siegrist, Martin Studer
Abstract: The present invention is directed to a class of compounds that are made by neutralizing the amino group in an amphoteric surfactant with the carboxylic acid group. The complex has (a) lower irritation, (b) better foaming properties and (c) improved substantivity to a variety of substrates.
Type:
Grant
Filed:
January 18, 2000
Date of Patent:
June 26, 2001
Inventors:
Anthony J. O'Lenick, Jr., Charles W. Buffa
Abstract: This invention features methods of biphasic synthesis for synthesizing combinatorial libraries and combinatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.
Type:
Grant
Filed:
October 28, 1997
Date of Patent:
June 12, 2001
Assignee:
DuPont Pharmaceuticals Research Laboratories, Inc.
Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula:
wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
Type:
Grant
Filed:
December 14, 1999
Date of Patent:
June 5, 2001
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
Abstract: The present invention discloses the use, in the manufacture of a preventive and therapeutic drug of a brain disease, of a compound represented by formula (1):
CH2═CH—CH2—S(O)n—R (1)
[wherein R represents a hydrogen atom, an alkyl group, an alkenyl group, a substituted alkyl group, a substituted alkenyl group, an alkylthio group, an alkenylthio group, a phenyl group, a substituted phenyl group, a heterocyclic group, or a group derived from an amino acid or an oligopeptide by deletion of one hydrogen atom, and which group may have a protective group; and n is 0, 1, or 2], a glycoside thereof, or a salt of the compound or the glycoside.
The drug of the present invention for ameliorating brain diseases, inhibiting reduction of brain neurons and promoting branching of neurites, is useful for the prevention and treatment of brain diseases such as dementia in association with degeneration and sloughing of brain neurons.
Abstract: The present invention provides new methods for the treatment of viral hepatitis C involving the administration of vitamin E and other compounds with antioxidant properties. Treatment with high doses of vitamin E is effective in treating chronic hepatitis C in patients refractory to interferon. In addition, new methods are described for the treatment of hepatic fibrosis and hepatic conditions manifesting hepatic fibrosis involving the administration of butylated hydroxytoluene and a metabolite of pentoxifylline, 1-[3-carboxypropyl]-3, 7-dimethylxanthine. Furthermore, new methods are described for the treatment and prevention of hepatic disorders involving the use of 2,6-di-tert-butylphenol derivatives.
Type:
Grant
Filed:
September 21, 1999
Date of Patent:
April 17, 2001
Assignee:
The Regents of the University of California
Abstract: Novel polyketides and novel methods of efficiently producing both new and known polyketides, using recombinant technology, are disclosed. In particular, a novel host-vector system is described which is used to produce polyketide synthases which in turn catalyze the production of a variety of polyketides.
Type:
Grant
Filed:
March 5, 1999
Date of Patent:
April 10, 2001
Assignees:
The Leland Stanford Junior Univ., The John Innes Institute
Inventors:
Chaitan Khosla, David A. Hopwood, Suzanne Ebert-Khosla, Robert McDaniel, Hong Fu
Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
Type:
Grant
Filed:
March 11, 1998
Date of Patent:
March 27, 2001
Assignee:
G. D. Searle & Company
Inventors:
Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
Abstract: The invention relates to a compound having the general Formula I:
including its salts, where Z is either the group having the general Formula II:
where
R1 is alkyl having 1-4 C atoms, alkoxyalkyl having 2-5 C atoms or aryloxyalkyl whose alkyl group has 1-4 C atoms,
R2 is alkyl having 1-4 C atoms or alkoxyalkyl having 2-5 C atoms,
R3 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2,
Y is H2 or O and
L is a luminophoric moiety in a position para or meta to the nitrogen,
or is the group having the general Formula III:
where
n is 2 or 3,
R4 is alkyl having 1-4 C atoms or alkoxyalkyl having 2-5 C atoms,
R5 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2 and
L is a luminophoric moiety in a position para or meta to the nitrogen,
or is the group having the general Formula IV:
where
R6 is alkyl having 1-3 C atoms or phenyl,
R7 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2 and
L is a luminophoric moiety in a position para