Oxy Patents (Class 562/444)
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Patent number: 6750369Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: August 10, 2001Date of Patent: June 15, 2004Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Publication number: 20040092593Abstract: The invention relates to compounds of formula (I), to methods for their production and to the use thereof as medicaments.Type: ApplicationFiled: August 26, 2003Publication date: May 13, 2004Inventors: Michael Harter, Michael G. Hahn, Claudia Hirth-Dietrich, Andreas Knorr, Elke Stahl, Johannes-Peter Stasch, Frank Wunder
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Publication number: 20040082658Abstract: The invention relates to COOH compounds of formula (I), to a method for their production and to the use thereof as medicaments.Type: ApplicationFiled: August 26, 2003Publication date: April 29, 2004Inventors: Michael Harter, Michael Hahn, Claudia Hirth-Dietrich, Andreas Knorr, Elke Stahl, Johannes-Peter Stasch, Frank Wunder
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Patent number: 6696487Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing them and to methods for combating the phytopathogenic fungi of crops using these compounds and compositions.Type: GrantFiled: August 6, 2001Date of Patent: February 24, 2004Assignee: Bayer Cropscience S.A.Inventors: Vincent Gerusz, Darren James Mansfield, José Perez, David Tickle, Jean-Pierre Vors, Derek Baldwin, Thomas Lawley Hough, Dale Robert Mitchell
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Patent number: 6660756Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: March 12, 2002Date of Patent: December 9, 2003Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
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Publication number: 20030208081Abstract: This invention relates to a series of substituted aromatic ethers of the formula I 1Type: ApplicationFiled: April 16, 2003Publication date: November 6, 2003Applicant: Pfizer Inc.Inventor: John A. Lowe
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Publication number: 20030166719Abstract: The present invention provides novel 2-methylpropionic acid derivatives represented by the general formula: 1Type: ApplicationFiled: February 5, 2003Publication date: September 4, 2003Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Tetsuro Tamai, Nobuyuki Tanaka, Harunobu Mukaiyama, Akihito Hirabayashi, Hideyuki Muranaka, Masaaki Sato, Masuo Akahane
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Patent number: 6610729Abstract: The present invention relates to a hydroxamic acid derivative of the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition containing the derivative or a salt thereof, and to pharmaceutical use thereof. The hydroxamic acid derivative and a pharmacologically acceptable salt thereof of the present invention have an inhibitory activity of TNF &agr; production, and are useful for, for example, the prophylaxis and treatment of the diseases such as autoimmune diseases and inflammatory diseases (e.g., sepsis, MOF, rheumatoid arthritis, Crohn's disease, cachexia, myasthenia gravis, systemic lupus erythematosus, asthma, I type diabetes, psoriasis and the like), and the like.Type: GrantFiled: November 22, 2000Date of Patent: August 26, 2003Assignee: Mitsubishi Pharma CorporationInventors: Tomokazu Gotou, Shinji Takeda, Kazuhiro Maeda, Tomohiro Yoshida, Naoki Sugiyama, Tadahiro Takemoto
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Patent number: 6610710Abstract: Phenylalanine derivatives of the following formula and analogues thereof have an antagonistic activity to &agr;4&bgr;7 integrin and a selectivity toward &agr;4&bgr;1 integrin. They are used as therapeutic agents for various diseases to which &agr;4&bgr;7 integrin relates.Type: GrantFiled: June 28, 2002Date of Patent: August 26, 2003Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Chieko Ejima, Mitsuhiko Kojima, Eiji Nakanishi, Hiroyuki Izawa, Yuko Satake, Nobuyasu Suzuki, Manabu Suzuki, Masahiro Murata
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Patent number: 6605742Abstract: Novel cyclo azaphospha hydrocarbons according to formula I are provided. The compounds are useful as metalloprotease inhibitors.Type: GrantFiled: April 11, 2002Date of Patent: August 12, 2003Assignee: LEO Pharma A/SInventors: Thomas Høyer, Morten Dahl Sørensen
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Publication number: 20030149003Abstract: Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.Type: ApplicationFiled: October 28, 2002Publication date: August 7, 2003Inventors: David J. Chaplin, Charles Manly Garner, Robert Ronald Kane, Kevin G. Pinney, Joseph Anthony Prezioso, Klaus Edvardsen
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Patent number: 6593100Abstract: A method for enhancing the conversion of a phenol substrate to a product by a peroxidase enzyme comprises the steps of reacting a conjugate comprising a detectably labeled phenol with a peroxidase enzyme in the presence of an enhancing reagent, the enhancing reagent comprising an inorganic salt, an organic compound having the formula wherein when X is B(OH)2, Y is I, or wherein when X is OH, Y is a halogen, or Q-R wherein Q is a linear or branched 1-12 heteroatom alkyl wherein tie heteroatoms are selected from C, N, O, and S, wherein the bonds connecting the heteroatom alkyl chain are single or double, wherein any carbon atom in the heteroatom alkyl chain optionally includes a substituent selected from —OH, —COOH, —NH2, and —SH, and wherein R is selected from —OH, —COOH, —NH2, and —CH3; or mixtures of the inorganic salt and the organic compound.Type: GrantFiled: May 17, 2001Date of Patent: July 15, 2003Assignees: NEN Life Science Products, Inc., Washington UniversityInventors: Mark Norman Bobrow, Karl Edwin Adler, Kevin Aaron Roth
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Patent number: 6593493Abstract: The present invention provides a novel class of RXR modulator compounds that exhibit an improved pharmacologic profile relative to the profile of previously studied RXR modulators, including those that share common structural features with the presently claimed modulators. The present invention also provides synthetic methods for preparing these compounds as well as pharmaceutical compositions incorporating these novel compounds and methods for the therapeutic use of such compounds and pharmaceutical compositions.Type: GrantFiled: September 14, 2000Date of Patent: July 15, 2003Assignee: Ligand Pharmaceuticals, Inc.Inventors: Robert J. Ardecky, Marcus F. Boehm, Amy L. Faulkner, Lawrence G. Hamann, Todd K. Jones, Christopher M. Mapes, Pierre-Yves Michellys, John S. Tyhonas, Anthony W. Thompson, Jyun-Hung Chen
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Patent number: 6579987Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioaryl-alkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is seleType: GrantFiled: December 20, 2002Date of Patent: June 17, 2003Assignee: NPS Allelix CorporationInventors: Ian Egle, Jennifer Frey, Methvin Isaac
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Patent number: 6552076Abstract: 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: GrantFiled: December 14, 2001Date of Patent: April 22, 2003Assignee: MitoKorInventors: Yazhong Pei, Walter H. Moos, Soumitra S. Ghosh
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Patent number: 6545029Abstract: The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and antiatherosclerotic activity. The present invention moreover relates to the preparation of these compounds and their use for the production of medicaments, and also medicaments comprising them.Type: GrantFiled: June 12, 2001Date of Patent: April 8, 2003Assignee: Bayer AktiengesellschaftInventor: Andrea Vaupel
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Patent number: 6518450Abstract: The present invention reveals a novel structure of guaiacoxypropanolamines shown in formula I: The composition comprising formula I acts as active intergant and pharmaceutical acceptable vehicle. The composition by perfect administration routes in the mammal when given potential &agr;/&bgr;-adrenergic blocking, is selective for emergency hypertension.Type: GrantFiled: December 20, 2000Date of Patent: February 11, 2003Assignee: National Science CouncilInventor: Ing-Jun Chen
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Publication number: 20030027862Abstract: 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: ApplicationFiled: July 31, 2001Publication date: February 6, 2003Inventors: Helmut Haning, Josef Pernerstorfer, Gunter Schmidt, Michael Woltering, Hilmar Bischoff, Verena Vohringer, Axel Kretschmer, Christiane Faeste
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Patent number: 6515124Abstract: Aromatic dehydroamino acids are disclosed that are active as LFA-1 arnagonists This activity enables these compounds to prevent inflammation which is a consequence of T cell activation and accordingly reduce or eliminate inflammatory skin disease psoriasis.Type: GrantFiled: January 5, 2001Date of Patent: February 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6504052Abstract: 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 systemType: GrantFiled: November 16, 2001Date of Patent: January 7, 2003Assignee: Eli Lilly and CompanyInventors: Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente
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Patent number: 6486343Abstract: The present invention relates to novel compounds of the formula (I) in which Het represents one of the groups in which A, B, D, G, V, W, X, Y and Z are as defined in the description, processes and intermediates for their preparation, and to their use as pesticides and herbicides.Type: GrantFiled: February 12, 2002Date of Patent: November 26, 2002Assignee: Bayer AktiengesellschaftInventors: Volker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Alan Graff, Udo Schneider
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Patent number: 6469210Abstract: A process for producing a phenylalkanoic acid amide of the formula [3] by reacting a carboxylic acid of the formula [1] with a dehydrating agent to produce an oxazolinone compound of the formula [2] and then reacting the oxazolinone compound with methyllithium or a methylmagnesium halide and an intermediate for producing the phenylalkanoic acid compound.Type: GrantFiled: December 27, 2000Date of Patent: October 22, 2002Assignee: Ihara Chemical Industry Co., Ltd.Inventors: Shuji Taniguchi, Hidetaka Hiyoshi, Katsunori Matsumoto
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Publication number: 20020151722Abstract: The present invention provides a production method of an optically active &bgr;-amino-&agr;-hydroxycarboxylic acid, which includes the following steps (a)-(c):Type: ApplicationFiled: April 10, 2002Publication date: October 17, 2002Applicant: AJINOMOTO CO. INCInventors: Yasuyuki Otake, Tomoyuki Onishi, Sachiko Oka, Daisuke Takahashi
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Patent number: 6455726Abstract: A compound of the following formula (II) and a process for preparing of the compound of the following formula (I) its preparation wherein R1 is carboxy or protected carboxy; R2 is lower alkoxy or higher alkoxy; A1 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; and A2 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane, or a salt thereof. The process comprises, reacting a compound of the formula (III): wherein R1, R2, A1 and A2 are each as defined above or a salt thereof, with an acid ammonium salt to give a compound of the formula (II).Type: GrantFiled: February 14, 2001Date of Patent: September 24, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaharu Ichihara, Norio Hashimoto, Atsushi Kanda, Kooji Kagara
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Patent number: 6451788Abstract: A method of treating pain by the co-administration of an antidepressant together with one or more precursors or inducers of neurotransmitters, particularly amino acids selected from L-phenylalanine, L-tyrosine, L-tryptophan and L-DOPA.Type: GrantFiled: January 4, 2000Date of Patent: September 17, 2002Assignee: The WWK Trust of 225-235 High StreetInventors: David Frederick Horrobin, Cari Loder, Graham Cooper
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Patent number: 6426364Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioarylalkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selecType: GrantFiled: November 1, 2000Date of Patent: July 30, 2002Assignee: NPS Allelix Corp.Inventors: Ian Egle, Jennifer Frey, Methvin Isaac
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Patent number: 6420561Abstract: 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.Type: GrantFiled: November 17, 2000Date of Patent: July 16, 2002Assignee: Japan Tobacco Inc.Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe
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Patent number: 6420427Abstract: An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.Type: GrantFiled: April 7, 2000Date of Patent: July 16, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kanji Takahashi, Tsuneyuki Sugiura
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Patent number: 6417395Abstract: The invention concerns a method for preparing methionine aminoamide. The invention also concerns the preparation of methionine without co-production of salts, from an aqueous solution containing essentially methionine aminonitrile by producing during a first step aminoamide followed by two complementary steps.Type: GrantFiled: July 12, 2001Date of Patent: July 9, 2002Assignee: Aventis Animal Nutrition S.A.Inventors: Hervé Ponceblanc, Olivier Favre-Bulle, Georges Gros
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Patent number: 6414180Abstract: The invention herein is directed to a process for the preparation of chiral &bgr;-amino acids and esters of the formula wherein X and Y are the same or different halo groups, R2 is H or lower alkyl and isomers and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 2, 1999Date of Patent: July 2, 2002Assignee: G. D. SearleInventors: Pierre-Jean Colson, Alok K. Awasthi, Srinivasan R. Nagarajan
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Publication number: 20020072500Abstract: The present invention relates to a class of compounds represented by the Formula I.Type: ApplicationFiled: September 26, 2001Publication date: June 13, 2002Inventors: Thomas Rogers, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Peter Ruminiski, Jennifer VanCamp, Chester Yuan
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Publication number: 20020065255Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water.Type: ApplicationFiled: September 24, 2001Publication date: May 30, 2002Applicant: EMISPHERE TECHNOLOGIES, INC.Inventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Russo
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Patent number: 6395930Abstract: A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.Type: GrantFiled: May 25, 2000Date of Patent: May 28, 2002Assignee: Warner LambertInventor: Sham Nikam
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Patent number: 6395784Abstract: 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.Type: GrantFiled: May 31, 2001Date of Patent: May 28, 2002Assignee: Bristol-Myers Squibb CompanyInventor: Denis E. Ryono
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Patent number: 6384236Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, AA and Y are as defined herein, inhibit phosphodiesterase type IV or inhibit the production of tumor necrosis factor, and therefore are useful in the treatment of certain conditions and diseases including asthma, arthritis, and sepsis.Type: GrantFiled: January 25, 2001Date of Patent: May 7, 2002Assignee: Pfizer IncInventor: Edward F. Kleinman
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Publication number: 20020052401Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I 1Type: ApplicationFiled: July 2, 2001Publication date: May 2, 2002Applicant: Pfizer Inc.Inventor: John A. Lowe
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Patent number: 6380181Abstract: Catechol derivatives of general formula (I) in which R1 denotes O-acyl and R2 represents amino acid residues in the 3- and/or 4-position function as siderophores and/or as biological chelating agents for iron in gram-negative bacteria. Conjugates with antibiotics improve penetration into bacterial cells, thereby increasing antibacterial efficacy of the cells.Type: GrantFiled: September 10, 1999Date of Patent: April 30, 2002Assignee: Gruenenthal GmbHInventors: Lothar Heinisch, Ute Moellmann, Matthias Schnabelrauch, Rolf Reissbrodt
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Patent number: 6372937Abstract: A method for enhancing the conversion of a phenol substrate to a product by a peroxidase enzyme comprises the steps of reacting a conjugate comprising a detectably labeled phenol with a peroxidase enzyme in the presence of an enhancing reagent, the enhancing reagent conmprising an inorganic salt, an organic compound having the formula wherein when X is B(OH)2, Y is I, or wherein when X is OH, Y is a halogen, or Q-R wherein Q is a linear or branched 1-12 heteroatom alkyl wherein the heteroatoms are selected from C, N, O, and S, wherein the bonds connecting the heteroatom alkyl chain are single or double, wherein any carbon atom in the heteroatom alkyl chain optionally includes a substituent selected from —OH, —COOH, —NH2, and —SH, and wherein R is selected from —OH, —COOH, —NH2, and —CH3; or mixtures of the inorganic salt and the organic compound.Type: GrantFiled: November 5, 1999Date of Patent: April 16, 2002Inventors: Mark Norman Bobrow, Karl Edwin Adler, Kevin Aaron Roth
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Patent number: 6372941Abstract: An industrially advantageous method of producing &bgr;-halogeno-&agr;-aminocarboxylic acids is provided. Methods are also provided of producing optically active N-protected-S-phenylcysteines having high optical purity and of intermediates thereof, respectively, in which the above production method is utilized. A method of producing &bgr;-halogeno-&agr;-aminocarboxylic acids or salts thereof is disclosed which comprises halogenating the hydroxyl group of a &bgr;-hydroxy-&agr;-aminocarboxylic acid (in which the basicity of the amino group in &agr;-position is not masked by the presence of a substituent on said amino group) or a salt thereof with an acid with a halogenating agent.Type: GrantFiled: August 16, 1999Date of Patent: April 16, 2002Assignee: Kaneka CorporationInventors: Koki Yamashita, Kenji Inoue, Koichi Kinoshita, Yasuyoshi Ueda, Hiroshi Murao
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Patent number: 6353027Abstract: This invention provides compounds and their pharmaceutically-acceptable salts, pharmaceutical formulations of said compounds, and methods for treating hyperglycemia associated with non-insulin dependent diabetes and for treating hyperlipidemia.Type: GrantFiled: March 3, 2000Date of Patent: March 5, 2002Assignee: Eli Lilly and CompanyInventors: Samuel James Dominianni, Margaret Mary Faul, Russell Dean Stucky, Leonard Larry Winneroski, Jr.
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Patent number: 6340560Abstract: An aminopolycarboxylic acid compound represented by the following formula or analogous thereof: The aminopolycarboxylic acid compound of the present invention can be used as a chelating agent for various metals, which is excellent in the biodegradability and masking effect on metals.Type: GrantFiled: October 7, 1998Date of Patent: January 22, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Tadashi Inaba, Kiyoshi Morimoto, Shigeo Hirano
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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
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Patent number: 6331627Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereo-somers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.Type: GrantFiled: July 5, 2000Date of Patent: December 18, 2001Assignee: Reddy's Laboratories Ltd.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6326399Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano and crop protection agents containing these compounds.Type: GrantFiled: April 9, 1996Date of Patent: December 4, 2001Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 6313344Abstract: Compounds of formula (I), wherein either X is CH or N, Y is OR1 and Z is O, or X is N, Y is NHR8 and Z is O, S or S(═O); R1, R2 and R3 are as defined according to the specification; m is 0, 1 or 2; R5 is, for example, halogen, C1-C6alkyl, halo-C1-C6alkyl or C3-C6cycloalkyl; n is 0, 1, 2, 3 or 4; R9 is methyl, fluoromethyl or difluoromethyl; A and R7 are as defined according to the specification; D is O, S, —S(═O) or S(═O)2; G is C1-C6aalkylene; T—R6 is R6, —C(═N—O—A1—R77)—R6; —SiR14(R15)—R6; —C(═O)—R6; —C(R16)═C(R17)—R6, —C≡C—R6 or —D—R6; R6 is C1-C4alkyl or unsubstituted or substituted aryl or heteroaryl; A1 and R77 are as defined above for A and R7; L is U—R18, P(OR)vR11R12, P(S)wR11R12 or N(aryl)R13; v and w are 0 or 1; U—R18 is —C(═O)—C(═O)—R18; —C(OH)—C(OH)—R18; —C(═N&mdType: GrantFiled: May 27, 1998Date of Patent: November 6, 2001Assignee: Bayer AktiengesellschaftInventors: Stephan Trah, Henry Szczepanski, Ottmar Franz Hüter, Roger Graham Hall, Saleem Farooq, Alfons Pascual
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Patent number: 6310084Abstract: The present invention relates to therapeutically active hydroxamic acid, N-formyl-N-hydroxyamino and carboxylic acid derivatives, their preparation, and pharmaceutical compositions containing them. These compounds are useful in the inhibition of metalloproteases, such as stromelysin, gelatinase, matrilysin, and collagenase. These compounds are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.Type: GrantFiled: February 11, 2000Date of Patent: October 30, 2001Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Fionna Mitchell Martin, Richard Simon Todd
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Patent number: 6310078Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 3, 2000Date of Patent: October 30, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 6281379Abstract: This invention to provide a process for producing an optically active threo-phenylnorstatin derivative which does not require a toxic cyanating agent or a costly reagent, or a complicated procedure, and can be practiced on a commercial scale. This invention is directed to a process for producing a &bgr;-amino-&agr;-hydroxy acid derivative which comprises treating either a &ggr;-amino-&bgr;-keto sulfoxide derivative with a halogenating agent to produce a &ggr;-amino-&agr;-halo-&bgr;-keto sulfoxide derivative, treating the same with an acid and an alcohol to produce a &bgr;-amino-&agr;-keto ester derivative or &bgr;-amino-&agr;-keto acid derivative, and followed by reducing.Type: GrantFiled: May 26, 2000Date of Patent: August 28, 2001Assignee: Kaneka CorporationInventors: Akio Fujii, Masanobu Sugawara, Kenji Inoue
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Publication number: 20010008947Abstract: Use in the prevention and/or in the treatment of neurodegenerative diseases of 2-amino-4-phenyl-4-oxo-butyric acid derivatives which act as kynureninase enzyme inhibitors and/or kynurenine-3-hydroxylase enzyme inhibitors.Type: ApplicationFiled: October 14, 1997Publication date: July 19, 2001Inventors: MARIO VARASI, ANTONIO GIORDANI, CARMELA SPECIALE, MASSIMO CINI, ALBERTO BIANCHETTI
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Patent number: 6255285Abstract: The present invention has as its object providing phenethylamine derivatives that typically function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds represented by the general formula (1): (wherein A is typically an amino acid residue, R1 is typically R6—CO—, R2 is typically a hydrogen atom, R3 is typically —CO—R7, R4 is typically an alkyl group, R5 is typically a hydroxyl group, R6 is typically an alkyl group, and R7 is typically an amino group).Type: GrantFiled: February 15, 2000Date of Patent: July 3, 2001Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Ken-ichiro Kotake, Toshiro Kozono, Tsutomu Sato, Hisanori Takanashi