Sulfur In Substituent Q Patents (Class 564/162)
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Patent number: 6872851Abstract: The invention concerns compounds of formula (I): R—A—R? wherein: A is as defined in the description; R represent, a group (V), wherein R?a and R?a are as defined in the description, or R forms with A a cyclic structure as defined in the description; R? represents a (CH2)t—R2 group wherein q, t, and R2 are as defined in the description. The invention is useful for preparing medicines.Type: GrantFiled: May 10, 1999Date of Patent: March 29, 2005Assignee: Les Laboratories ServierInventors: Daniel Lesieur, Frédérique Klupsch, Gérald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
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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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Publication number: 20040254166Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1Type: ApplicationFiled: April 1, 2004Publication date: December 16, 2004Inventors: Kevin D. Kreutter, Lily Lee, Tianbao Lu, Venkatraman Mohan, Sharmila Patel, Hui Huang, Guozhang Xu, Mark Fitzgerald
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Patent number: 6825236Abstract: Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group —C(O)—(CHR4)m—AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R1 is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R2 (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R3; R3 (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R2; and R4 is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed.Type: GrantFiled: April 14, 2003Date of Patent: November 30, 2004Assignees: California Pacific Medical Center, Catholic Healthcare WestInventor: Li-Xi Yang
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Publication number: 20040229923Abstract: A method for resolving enantiomers of a compound containing the structure of the formula: 1Type: ApplicationFiled: June 16, 2004Publication date: November 18, 2004Inventors: Glenn E. Wilcox, Mark E. Flanagan, Michael J. Munchhof, Ton Vries, Christian Koecher
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Publication number: 20040192929Abstract: A process for the oxidation of thioethers to sulfoxides or sulfones or for the oxidation of sulfoxides to sulfones by treatment of thioethers or sulfoxides with an oxidizing amount of &egr;-phthalimidoperhexanoic acid is particularly useful for the preparation of compounds of industrial interest, in particular pharmaceuticals for human or veterinary use.Type: ApplicationFiled: March 17, 2004Publication date: September 30, 2004Applicant: DINAMITE DIPHARMA S.P.A. abbreviated DIPHARMA S.P.A.Inventors: Pietro Allegrini, Caterina Napoletano, Gabriele Razzetti, Graziano Castaldi
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Patent number: 6777442Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.Type: GrantFiled: February 26, 2002Date of Patent: August 17, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Peter Ellinghaus
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Publication number: 20040142979Abstract: This invention is directed generally to heteroarylsulfonylmethyl hydroxamic acids and amides that, inter alia, tend to inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to compositions of such compounds; intermediates for the syntheses of such compounds; methods for making such compounds; and methods for treating conditions associated with MMP, tumor necrosis factors (or “TNFs”), and/or aggrecanase activity, particularly pathological conditions.Type: ApplicationFiled: November 25, 2003Publication date: July 22, 2004Inventors: Daniel P. Becker, Jeffery N. Carroll, Yvette M. Fobian, Margaret L. Grapperhaus, Donald W. Hansen, Robert M. Heintz, Darren J. Kassab, Mark A. Massa, Joseph J. McDonald, Mark A. Nagy, Barnett S. Pitzele, Joseph G. Rico, Michelle A. Schmidt, Dale P. Spangler
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Publication number: 20040122064Abstract: The present invention is directed to benzophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.Type: ApplicationFiled: February 5, 2004Publication date: June 24, 2004Inventor: Joseph Howing Chan
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Publication number: 20040116518Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases and cerebral vasospasm, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: ApplicationFiled: December 1, 2003Publication date: June 17, 2004Applicant: Abbott LaboratoriesInventor: Indrani W. Gunawardana
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Publication number: 20040106829Abstract: The present invention relates to a process for the preparation of 2-(benzhydrylthio)acetamide (II), key intermediate for the synthesis of modafinil, by reaction of benzhydryl chloride with thiourea and chloroacetamide.Type: ApplicationFiled: November 10, 2003Publication date: June 3, 2004Applicant: PROCOS S.P.A.Inventors: Mirco Fornaroli, Francesco Velardi, Corrado Colli, Roberto Baima
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Publication number: 20040102523Abstract: Modafinil polymorphic forms of modafinil racemate, methods of preparation thereof, pharmaceutical compositions and methods of therapeutic treatment involving modafinil polymorphic forms.Type: ApplicationFiled: August 7, 2003Publication date: May 27, 2004Inventors: Michel Broquaire, Laurent Courvoisier, Armand Frydman, Gerard Coquerel, Franck Mallet, Veronique Broquaire, Ludovic Broquaire
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Patent number: 6720452Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: June 10, 2002Date of Patent: April 13, 2004Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Timothy Luker, Michael Mortimore, Philip Thorne
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Publication number: 20040068016Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.Type: ApplicationFiled: September 22, 2003Publication date: April 8, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Patent number: 6706921Abstract: The invention relates to a method for producing acid addition salts of compounds of formula (I), wherein R1, R2 and R3 represent alkyl with 1 to 12 C-atoms.Type: GrantFiled: November 6, 2002Date of Patent: March 16, 2004Assignee: Merck Patent GmbHInventors: Ekkehard Bartmann, Michael Kirschbaum
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Publication number: 20040044249Abstract: The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio) propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof. The present invention further discloses a new process for the isolation and purification of racemic and optically active bicalutamide.Type: ApplicationFiled: June 25, 2003Publication date: March 4, 2004Inventors: Ben-Zion Dolitzky, Ofer Reany, Jenny Shammai
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Publication number: 20040043920Abstract: The present invention provides a compound for chelating a metal or a metal complex, characterized in that it consists of a bis-dithiocarbamate structure (F) having the formula below: 1Type: ApplicationFiled: May 28, 2003Publication date: March 4, 2004Inventors: Laurent Mauclaire, Eric Berthommier
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Publication number: 20040039034Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: April 30, 2003Publication date: February 26, 2004Inventors: John A. Tucker, Brian A. Sherer, Ying Zi Xu, Louis Brogley, Shon R. Pulley, Jon S. Jacobs, James P. Beck, Varghese John
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Publication number: 20040029903Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, a trihalomethylcarbonyl group, such as a trifluoromethylcarbonyl group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.Type: ApplicationFiled: May 21, 2003Publication date: February 12, 2004Applicant: Beacon Laboratories, Inc.Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
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Publication number: 20040019086Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: July 10, 2002Publication date: January 29, 2004Inventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Publication number: 20040014969Abstract: The invention relates to compound of formula (I): 1Type: ApplicationFiled: March 14, 2003Publication date: January 22, 2004Inventors: Carole Descamps-Francois, Said Yous, Daniel Lesieur, Gerald Guillaumet, Marie-Claude Viaud, Herve Da Costa, Caroline Bennejean, Philippe Delagranes, Pierre Renard
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Patent number: 6677473Abstract: Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers, benzils, benzyl ethers, benzoate esters, sulfones and benzophenones are provided.Type: GrantFiled: November 17, 2000Date of Patent: January 13, 2004Assignee: Corvas International INCInventors: Edwin L. Madison, Terence K. Brunck, Joseph Edward Semple, Marguerita Lim-Wilby, Kent E. Pryor, Ronald D. Lewis, II, David F. Duncan, C. Maxwell Lawrence
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Publication number: 20040006245Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: January 23, 2003Publication date: January 8, 2004Inventors: Gordon William Rewcastle, Julie Ann Spicer, Stephen Douglas Barrett, Michael David Kaufman, Jared Bruce John Milbank, Haile Tecle
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Publication number: 20040002547Abstract: The present invention provides processes for the preparation of modafinil which includes the step of reacting benzhydrylthiol and chloroacetamide.Type: ApplicationFiled: May 22, 2003Publication date: January 1, 2004Inventors: Denis Largeau, Gilles Oddon
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Publication number: 20030232996Abstract: A novel process for preparing 3,4-di(carbocyclyl or heterocyclyl)thiophenes comprising reacting a compound of Formula IV with a ring cyclizing reagent to form the compound of Formula V to yield a compound of Formula V wherein R1, R2 and R3 are as defined in the specification.Type: ApplicationFiled: April 16, 2003Publication date: December 18, 2003Inventors: David L Brown, Cindy L Ludwig
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Patent number: 6653309Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: October 30, 2000Date of Patent: November 25, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeffrey O. Saunders, Daniel Elbaum, Perry M. Novak, Douglas Naegele, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Catharine Frank, Dean P. Stamos, William Walters, David Pearlman
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Publication number: 20030215876Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction.Type: ApplicationFiled: February 20, 2003Publication date: November 20, 2003Inventors: Seung Bum Park, David Barnes-Seeman, Angela N. Koehler, Stuart L. Schreiber
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Patent number: 6649796Abstract: The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH2CONH2, wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.Type: GrantFiled: April 2, 2002Date of Patent: November 18, 2003Assignee: Chemagis, Ltd.Inventors: Vladimir Naddaka, Naim Menashe, Jael Lexner, Shadi Saeed, Joseph Kaspi, Ori Lerman
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Patent number: 6638970Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: October 28, 2003Assignee: CV Therapeutics, Inc.Inventors: Elfaith Elzein, Jeff Zablocki, Tim Marquart
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Patent number: 6635650Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 8, 2001Date of Patent: October 21, 2003Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Publication number: 20030195354Abstract: An amide compound given by formula [I]: 1Type: ApplicationFiled: December 12, 2002Publication date: October 16, 2003Inventor: Hiroshi Sakaguchi
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Publication number: 20030191337Abstract: The present invention relates to a crystal of bicalutamide having a defined form, as well as economical and industrially practical production methods of bicalutamide and a crystal thereof, which are superior in environmental benignity and safety.Type: ApplicationFiled: February 24, 2003Publication date: October 9, 2003Inventors: Tetsuya Shintaku, Tadashi Katsura, Nobushige Itaya
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Patent number: 6630600Abstract: Novel 3-aryl propionic acid derivatives and analogs, process and intermediate for their manufacture, pharmaceutical preparations containing them and the use of the compounds in clinical conditions associated with insulin resistance.Type: GrantFiled: July 20, 1999Date of Patent: October 7, 2003Assignee: AstraZeneca ABInventors: Kjell Andersson, Maria Boije, Johan Gottfries, Tord Inghardt, Lanna Li, Eva-Lotte Lindstedt Alstermark
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New amphetamine derivatives, antibodies against them and pharmaceutical compositions containing them
Publication number: 20030171435Abstract: Hapten-carrier conjugates capable of eliciting anti-hapten antibodies in vivo to amphetamines are disclosed. Methods of preparing the hapten-carrier conjugates and therapeutic compositions are also disclosed. A therapeutic composition containing the hapten-carrier conjugate is useful in the treatment of addiction to amphetamines. Passive immunization using antibodies raised against conjugates of the instant invention also is disclosed. The therapeutic composition is suitable for co-therapy with other conventional drugs for treatment of amphetamine abuse.Type: ApplicationFiled: January 23, 2002Publication date: September 11, 2003Applicant: Drug Abuse Sciences, Inc.Inventors: Philippe Pouletty, Jacques Kusmierek, Frederic Koralewski, Herve Galons, Dominique Blanchard, Caroline Gadjou -
Publication number: 20030166693Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: March 14, 2003Publication date: September 4, 2003Applicant: AJINOMOTO CO., INCInventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Patent number: 6610747Abstract: A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d=0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; Z or Y is —SR3 and the other Z or Y is halogen or —R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R4 and R5, which may be the same or different, are: A—X, wherein A=—CH═CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(═O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; or a 5- or 6-membered hetType: GrantFiled: August 27, 2001Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: Mavis Diane Adam, Mark David Andrews, Mark Leonard Elliott, Geoffrey Edward Gymer, David Hepworth, Harry Ralph Howard, Jr., Donald Stuart Middleton, Alan Stobie
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Patent number: 6610701Abstract: Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.Type: GrantFiled: February 8, 2002Date of Patent: August 26, 2003Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Craig Coburn, Harold G. Selnick, Phung L. Ngo
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Patent number: 6608196Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.Type: GrantFiled: May 3, 2002Date of Patent: August 19, 2003Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Satyanarayana Janagani, Wyeth B. Callaway, Jonathan L. Sessler
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Patent number: 6603043Abstract: Process for the preparation of a Schiff base of an &agr;-alkyl-&agr;-amino acid amide and an aldehyde, wherein the corresponding &agr;-aminonitrile is contacted with a base and the aldehyde and wherein it is ensured that the reagents are in good contact. The Schiff base obtained may be further hydrolysed to form the &agr;-alkyl-&agr;-amino acid amide and the aldehyde. Preferably a substituted or unsubstituted benzaldehyde is used as the aldehyde. The reaction is preferably carried out in a practically homogeneously mixed phase obtained by using a solvent, for example methanol or ethanol. Preferably NaOH or KOH is used as the base.Type: GrantFiled: July 13, 2001Date of Patent: August 5, 2003Assignee: DSM N.V.Inventors: Dominique Monique Charles Callant, Daniel Mink, Anna Maria Cornelia Francisca Castelijns
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Publication number: 20030119902Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: ApplicationFiled: August 28, 2002Publication date: June 26, 2003Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Publication number: 20030105078Abstract: The invention relates to novel diphenyl derivatives, to processes for their preparation and to their use in medicaments.Type: ApplicationFiled: February 26, 2002Publication date: June 5, 2003Inventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vohringer, Peter Ellinghaus
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Patent number: 6573404Abstract: The invention relates to a process for the preparation of ortho-alkylated benzoic acid derivatives of the formula I characterized in that an aryl bromide of the formula II is reacted with a secondary or tertiary organolithium compound and CO2.Type: GrantFiled: October 8, 2002Date of Patent: June 3, 2003Assignee: Merck Patent GmbHInventors: Ekkehard Bartmann, Ingeborg Stein
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Patent number: 6552226Abstract: A novel tandem acyl-Claisen rearrangement reaction is provided. An allylic reactant such as an allylic amine or an allylic thioether, having at least two functional groups that enable the reactant to undergo at least two successive Claisen rearrangement reactions, is reacted with an acid chloride in the presence of a Lewis acid catalyst composition composed of a Lewis acid and a second catalyst component selected from the group consisting of tertiary amines and non-nitrogenous bases. The stereochemistry of the reaction product is readily controlled by the positioning and size of substituents on the allylic reactant. The reaction may be carried out on a solid support, i.e., on the surface of a substrate suitable for conducting solid phase chemical reactions.Type: GrantFiled: September 26, 2000Date of Patent: April 22, 2003Assignee: The Regents of the University of CaliforniaInventor: David W. C. MacMillan
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Patent number: 6552061Abstract: Provided are an anti-inflammatory agent containing, as an active ingredient, at least one selected from amino acid derivatives represented by formula (I) wherein Ar represents an optionally substituted 2-hydroxyaryl group, n is 0 or 1, R2 represents a hydrogen atom or a side chain of an &agr;-amino acid or &bgr;-amino acid, X represents —O— or —NH—, R1 represents a hydrogen atom or a group that forms, together with R2 and an adjacent atoms, a cyclic structure of pyroglutamic acid, and R3 represents a hydrogen atom, an alkyl group having from 1 to 22 carbon atoms or an alkenyl group having from 2 to 22 carbon atoms, and salts thereof, and toiletries or skin external products containing the same. The anti-inflammatory agent of the invention inhibits expression of an inflammatory protein and activation of a gene transcription control factor that participates therein, and exhibits a good feeling upon use and a safety.Type: GrantFiled: April 2, 1999Date of Patent: April 22, 2003Assignee: Ajinomoto Co., Inc.Inventors: Manabu Kitazawa, Keiji Iwasaki, Eiji Shiojiri
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Publication number: 20030073833Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1Type: ApplicationFiled: October 3, 2002Publication date: April 17, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
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Patent number: 6548702Abstract: The invention relates to a process for the preparation of 2-methoxy-4-(N-t-butylaminocarbonyl)benzenesulfonyl chloride by sulfonating m-hydroxybenzoic acid, methylating the hydroxy group of the resulting sulfonic acid or its salt, transforming the carboxylic acid group and the sulfonic acid group to acid chloride groups and reacting the 4-chlorosulfonyl-3-methoxy-benzoyl chloride with t-butylamine, which comprises carrying out the sulfonation of the 3-methoxy-benzoic acid of general formula (II) with 96% sulfuric acid, separating the resulting 3-hydroxy-4-sulfobenzoic acid of general formula (III) in the form of its salt of general formula (IV), wherein Z stands for alkali metal or ammonium group, methylating the compound of general formula (IV) in the presence of a phase transfer catalyst at a pH value of about 11.Type: GrantFiled: April 26, 2002Date of Patent: April 15, 2003Assignee: Sanofi-SynthelaboInventors: Csaba Gönczi, Éva Csikós, Félix Hajdú, István Hermecz, Gergely Héja, Gergelyné Héja, Lajos Nagy, Andrea Sántáné Csutor, Kálmán Simon, Ágota Smelkóné Esek, Tiborné Szomor, Györgyné Szvoboda
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Patent number: 6528528Abstract: The present invention provides compounds of Formula I shown below. The present invention also provides methods of treating or preventing 3 inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of Formula I.Type: GrantFiled: May 15, 2001Date of Patent: March 4, 2003Assignee: Warner-Lambert CompanyInventors: David Thomas Connor, William Howard Roark, Karen Elaine Sexton, Roderick Joseph Sorenson
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Publication number: 20030023096Abstract: The naphthyloxyacetic acid derivatives of the formula (I) 1Type: ApplicationFiled: December 19, 2001Publication date: January 30, 2003Inventors: Yuuki Nagao, Kazuhiko Torisu, Nobuyuki Hamanaka
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Publication number: 20030018056Abstract: A compound represented by the following formula: 1Type: ApplicationFiled: June 17, 2002Publication date: January 23, 2003Inventors: Masahumi Kitano, Masatoshi Yuri, Naohito Ohashi