Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Patent number: 6569874Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: November 17, 2000Date of Patent: May 27, 2003Assignee: Bristol-Myers Squibb CompanyInventors: James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
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Patent number: 6566508Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: March 11, 2002Date of Patent: May 20, 2003Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
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Patent number: 6562850Abstract: The invention relates to a new class of compounds herein identified generally as “sultams”, which may be represented by the following formula V, in FIG. 1, in which numbering of the atoms is started with the sulfur atom of the isothiazole. Two of the rings (rings A and C) are aromatic, and the third is a heterocyclic ring (ring B), a cyclic sulfonamide. Of particular importance are the enantiomerically pure sultams since they are especially potent HIV-1 inhibitors.Type: GrantFiled: July 15, 1999Date of Patent: May 13, 2003Assignee: The University of Tennessee Research CorporationInventors: David C. Baker, Anand Mayasundari, Jianmin Mao, Stephen C. Johnson, Shijia Yan
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Patent number: 6559142Abstract: Matrix metalloproteinase inhibitors are tricyclic substituted cyclic sulfonamides of the formula or a pharmaceutically acceptable salt thereof wherein R1 and R2 include hydrogen, alkyl, and substituted alkyl; R3 and R4 include hydrogen, halo, and alkyl; X is OH or NHOH, V is O, S, SO2, NR5, or CH2, R5 is a hydrogen or alkyl, and Z is (CH2)n, wherein n is an integer from 0 to 2.Type: GrantFiled: February 8, 2002Date of Patent: May 6, 2003Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, William Chester Patt, Joseph Armand Picard, Kevon Ray Shuler, Drago Robert Sliskovic
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Patent number: 6555535Abstract: Matrix metalloproteinase inhibitors are tricyclic sulfonamides of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1 and R2 include hydrogen, alkyl, and substituted alkyl; R3 is OH or NHOH; X is O or S(O)n; n is 0, 1, or 2; p is 0, 1, 2, or 3; — is absent or a bond; and the sulfur atom bearing (O)q is bonded to the benzo ring at position a or position b.Type: GrantFiled: February 13, 2002Date of Patent: April 29, 2003Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Drago Robert Sliskovic
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Publication number: 20030078433Abstract: The present invention relates to an improved and more economical process for the synthesis of 4,5-dihydro-1,3-thiazoles carried out in a single vessel without the isolation of intermediates.Type: ApplicationFiled: August 28, 2002Publication date: April 24, 2003Inventors: Katrin Joschek, Anton Vidal-Ferran, Manfred Jautelat, Michael Schelhaas
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Patent number: 6548481Abstract: Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group, and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.Type: GrantFiled: November 28, 2000Date of Patent: April 15, 2003Assignee: Probiodrug AGInventors: Hans-Ulrich Demuth, Konrad Glund, Dagmar Schlenzig, Susanne Kruber
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Patent number: 6548524Abstract: This invention provides, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-&agr; converting enzyme (TACE. tumor necrosis factor-&agr; converting enzyme) which arc useful for the treatment of diseases in which these enzymes are implicated.Type: GrantFiled: December 11, 2000Date of Patent: April 15, 2003Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Arie Zask, Yansong Gu, Jay D. Albright, Xuemei Du
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Publication number: 20030069223Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: ApplicationFiled: June 14, 2002Publication date: April 10, 2003Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
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Publication number: 20030055052Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug having a cleavage site which is recognised by FAP&agr;, and said drug being cytotoxic or cytostatic under physiological conditions.Type: ApplicationFiled: November 9, 2001Publication date: March 20, 2003Inventors: Stefan Peters, Dietmar Leipert, John Edward Park, Martin Lenter, Pilar Garin-Chesa
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Patent number: 6534659Abstract: Novel sulfidoamidocarboxylic acids (salts), a method for the production thereof, and uses therefor are provided. Sulfidoamidocarboxylic acids (salt) with a thiazolidine residue such as dimethylthiazolidine or methylthiazolidine or thiazolidine residue (residues), or a polycarboxylic acid (salt) residue such as dicarboboxylic acid (salt) or tricarboxylic acid (salt) or tetracarboxylic acid (salt) residue, a method for the production thereof, and uses therefor are also provided.Type: GrantFiled: April 23, 2001Date of Patent: March 18, 2003Assignee: Nippon Shokubai Co., Ltd.Inventor: Yoshihisa Oda
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Patent number: 6534532Abstract: The invention concerns novel carbanilides of formula (I), in which A, Q, R, X, Z and m have the meanings given in the description. The invention further concerns a plurality of processes for preparing these substances, in their use as microbiocides for controlling undesirable microorganisms both in crop protection and in the protection of materials. Additionally, they are suitable for controlling animal pests.Type: GrantFiled: September 18, 2001Date of Patent: March 18, 2003Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Bernd-Wieland Krüger, Robert Markert, Ralf Tiemann, Dietmar Kuhnt, Stefan Dutzmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Hans-Ulrich Buschhaus
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Patent number: 6534530Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: August 3, 2000Date of Patent: March 18, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Peter Scott Dragovich, Ru Zhou, Stephen Evan Webber, Thomas J. Prins, Siegfried Heinz Reich, Susan E. Kephart, Yuanjin Rui
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Patent number: 6531474Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.Type: GrantFiled: September 19, 2000Date of Patent: March 11, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
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Patent number: 6531612Abstract: Compounds of the formula: wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.Type: GrantFiled: December 21, 2000Date of Patent: March 11, 2003Assignee: Hoffman-La Roche Inc.Inventors: Tobias Gabriel, Michael Pech, Sabine Wallbaum
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Patent number: 6521626Abstract: Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates theType: GrantFiled: March 23, 1999Date of Patent: February 18, 2003Assignee: Celltech R&D LimitedInventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
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Publication number: 20030032635Abstract: This invention relates to neurotrophic low molecular weight, small molecule heterocyclic ester and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: ApplicationFiled: June 24, 2002Publication date: February 13, 2003Inventors: Jia-He Li, Gregory S. Hamilton
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Patent number: 6518290Abstract: A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein; X1 represents O or S; R1 and R2 independently represent H, halogen, —CH3 and —OCH3; n represents 1 or 2; X2 represents NH, NCH3 or O; One of Y and Z is N, and the other is O or S; R3 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one or more halogen, NO2, NH2, CF3, OCF3, OC1-6 straight or branched alkyl, C1-6 straight or branched alkyl, alkenyl or alkynyl with the provision that when R3 is pyridyl, the N is unsubstituted; R4 represents CF3 or CH3Type: GrantFiled: May 31, 2002Date of Patent: February 11, 2003Inventor: Michael Lawrence Sierra
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Patent number: 6509379Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.Type: GrantFiled: April 23, 1998Date of Patent: January 21, 2003Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Müller, Ruth Müller, Franz Röhl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann, Norbert Götz, Albrecht Harreus
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Patent number: 6506780Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: July 2, 2001Date of Patent: January 14, 2003Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Publication number: 20030004354Abstract: The invention relates to novel thienylsulphonylamino(thio)carbonyl compounds of the formula (I), 1Type: ApplicationFiled: November 9, 2001Publication date: January 2, 2003Inventors: Klaus-Helmut Muller, Ernst Rudolf F. Gesing, Mark Wilhelm Drewes, Johannes Rudolf Jansen, Rolf Kirsten, Joachim kluth, Klaus Konig, Ulrich Philipp, Markus Dollinger
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Publication number: 20020198200Abstract: Substituted benzene acetamide compounds and pharmaceutically acceptable salts thereof are useful as glucokinase activators.Type: ApplicationFiled: June 25, 2002Publication date: December 26, 2002Inventors: Robert F. Kester, Ramakanth Sarabu
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Patent number: 6495581Abstract: A compound represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond, —CO—, —CH(OH)— or a group represented by —NR6— wherein R6 is a hydrogen atom or an optionally substituted alkyl group; n is an integer of 1 to 3; Y is an oxygen atom, a sulfur atom, —SO—, —SO2— or a group represented by —NR7— wherein R7 is a hydrogen atom or an optionally alkyl group; ring A is a benzene ring optionally having additional one to three substituents; p is an integer of 1 to 8; R2 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; q is an integer of 0 to 6; m is 0 or 1; R3 is a hydroxy group, OR8 (R8 is an optionally substituted hydrocarbon group.Type: GrantFiled: November 16, 2000Date of Patent: December 17, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Hiroyuki Odaka, Hiroshi Imoto, Hiroyuki Kimura, Junichi Sakamoto
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Patent number: 6492405Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound is a) a compound containing one or more sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; b) a 5-membered ring heterocyclic compound containing a sulfur atom and a nitrogen atom, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; c) a 5-membered ring compound containing two conjugate S-atoms, which ring is linked to one or more substituents bearing a terminal —ONO2 group; or d) a compound containing an acyclic —S—S group, linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group.Type: GrantFiled: January 9, 2002Date of Patent: December 10, 2002Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventor: Abdullah Haj-Yehia
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Patent number: 6472526Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1): and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.Type: GrantFiled: December 3, 2001Date of Patent: October 29, 2002Assignee: LG Chemical Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6469036Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.Type: GrantFiled: January 13, 2000Date of Patent: October 22, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael J. Costanzo, Bruce E. Maryanoff, Stephen C. Yabut
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Patent number: 6458960Abstract: The present invention relates to a compound of the following Formula (1) or the pharmaceutically acceptable salts thereof, having low toxicity and a potent effect of inhibiting tubulin polymerization, and the use thereof as a pharmaceutical composition: (wherein R1 and R2 may be the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a hydroxy group; each R3, R4, R5 and R6 represents a hydrogen atom; A represents any group of (1) 5-membered heterocyclic group (except triazoyl group) optionally substituted by a lower alkyl group or phenyl group whose ring members include at least 1 nitrogen atom and may include any atom(s) selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom, and (2) a 3 to 10-membered alicyclic group whose ring members include at least 1 nitrogen atom and may include any atom(s) selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atType: GrantFiled: November 21, 2000Date of Patent: October 1, 2002Assignee: Nippon Kayaku Kabushiki KaishaInventors: Hirohisa Morohashi, Hiroshi Sato
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Patent number: 6451824Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: September 17, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Patent number: 6419857Abstract: A novel composition of thiazolidines of the following formula and a method to prepare the same are disclosed. The method involves reacting a dihydrothiazole with a mixture comprising formic acid and an aldehyde. These new thiazolidines are useful as corrosion inhibitors.Type: GrantFiled: December 6, 1999Date of Patent: July 16, 2002Assignee: Baker Hughes IncorporatedInventors: Bernardus Antonius Maria Oude Alink, Benjamin T. Outlaw
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Publication number: 20020091089Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: ApplicationFiled: April 16, 2001Publication date: July 11, 2002Inventors: Donald S. Karanewsky, Vincent J. Kalish, Edward D. Robinson, Brett R. Ullman
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Patent number: 6417209Abstract: This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neurodegenerative diseases.Type: GrantFiled: December 11, 2000Date of Patent: July 9, 2002Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Jia-He Li
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Patent number: 6413997Abstract: 3-(Substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.Type: GrantFiled: October 22, 1999Date of Patent: July 2, 2002Assignee: Dow AgroSciences LLCInventors: Francis E. Tisdell, Peter L. Johnson, James T. Pechacek, Robert G. Suhr, Donald H. DeVries, Carl P. Denny, Mary L. Ash
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Patent number: 6410576Abstract: An object of the present invention is to provide novel thiazolidine derivatives which are useful as drugs. The thiazolidine derivatives according to the present invention are compounds represented by the following general formula [I] and salts thereof, wherein R1 is alkyl, hydroxy, alkoxy, alkoxyalkyl, phenyl, phenylalkyl, phenylalkoxy, phenoxy, phenoxyalkyl, amino, alkylamino or a nonaromatic heterocycle; R2 is H or alkyl; R3 is H, alkyl or phenyl; R4 is H or alkyl; R5 is alkyl, halogenoalkyl, hydroxy, alkoxy, phenyl, phenylalkoxy, phenoxy, carboxyl, alkoxycarbonyl, phenylalkoxycarbonyl or an aromatic heterocycle; A1 is alkylene; and A2 is alkylene.Type: GrantFiled: January 29, 2001Date of Patent: June 25, 2002Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuo Nishimura, Ken-ichi Fujimura, Junzo Matsumoto, Tadayuki Kobayashi
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Patent number: 6403612Abstract: A thrombin receptor antagonist having the formula or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.Type: GrantFiled: January 30, 2001Date of Patent: June 11, 2002Assignee: Merck & Co., Inc.Inventors: Philippe G. Nantermet, James C. Barrow, Harold G. Selnick
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Patent number: 6392054Abstract: The present invention provides for novel 3-thiazolines comprising the formula where R1, R2 and R3 are identical or different and denote hydrogen or a lower alkyl, wherein said lower alkyl denotes an unbranched or branched hydrocarbon having 1 to 3 carbon atoms. These novel 3-thiazolines can be used as odorants and flavorings having an olfactory impression.Type: GrantFiled: July 6, 2000Date of Patent: May 21, 2002Assignee: Haarmann & Reimer GmbHInventors: Matthias Güntert, Stefan Lambrecht, Wolfgang Engel, Peter Schieberle
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Publication number: 20020052510Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: ApplicationFiled: December 3, 1998Publication date: May 2, 2002Inventors: GREGORY S. HAMILTON, MARK H. NORMAN, YONG-QIAN WU
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Publication number: 20020049165Abstract: A novel dipeptide compound inhibiting the enzymatic activity of HIV protease, an anti-AIDS medicine comprising this dipeptide compound as an effective component.Type: ApplicationFiled: August 27, 2001Publication date: April 25, 2002Inventors: Tsutomu Mimoto, Keisuke Terashima, Haruso Takaku, Shinji Matsumoto, Makoto Shintani, Satoshi Nojima
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Publication number: 20020049202Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.Type: ApplicationFiled: April 13, 2001Publication date: April 25, 2002Inventors: Margaret L. Grapperhaus, James A. Sikorski, Alok K. Awasthi, Lijuan J. Wang, Barnett S. Pitzele, Donald W. Hansen, Pamela T. Manning
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Publication number: 20020049193Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: ApplicationFiled: August 10, 2001Publication date: April 25, 2002Applicant: GPI NIL HOLDINGS, INC.Inventors: Gregory S. Hamilton, Jai-He Li, Wei Huang
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Patent number: 6376489Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory disease and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: December 7, 2000Date of Patent: April 23, 2002Assignee: ICOS CorporationInventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Laurence E. Burgess, Stephen T. Schlachter
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Patent number: 6372912Abstract: Process for the hydrolytic ring cleavage of thiazolidine derivatives to give 2-aminomercaptan derivatives and carbonyl compounds, which comprises bringing an aqueous solution of the thiazolidine derivative into contact with an acidic cation exchanger in the H+ form, giving a solution L1 which contains the carbonyl compound and eluting the cation exchanger with a suitable eluent, giving a solution L2 which contains the 2-aminomercaptan derivative.Type: GrantFiled: April 5, 2000Date of Patent: April 16, 2002Assignee: Consortium fur Elektrochemische Industrie GmbHInventors: Wolfgang Döring, Günther Karl Staudinger
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Patent number: 6372769Abstract: The present invention provides 5-carboxanilido-2,4-bis-trifluoromethylthiazoles and their compositions. The compounds and compositions are effective for controlling fungal diseases on plants. They are particularly effective for controlling rice blast.Type: GrantFiled: December 5, 2000Date of Patent: April 16, 2002Assignee: Dow AgroSciences LLCInventor: Frisby Davis Smith
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Patent number: 6372895Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: July 7, 2000Date of Patent: April 16, 2002Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6362341Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, wherein the disease may be, for example, asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 31, 1998Date of Patent: March 26, 2002Assignees: Athena Neurosciences, Inc., American Home ProductsInventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Louis John Lombardo, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen
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Patent number: 6362204Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; and R5 is a group —L2(CH2)tR6 in which L2 is a —N(R7)CO— or —N(R7)CS— group. The compounds are able to inhibit the binding &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: May 20, 1999Date of Patent: March 26, 2002Assignee: Celltech Therapeutics, LtdInventors: John Clifford Head, Sarah Catherine Archibald, Graham John Warrellow, John Robert Porter
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Patent number: 6344562Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.Type: GrantFiled: June 11, 2001Date of Patent: February 5, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
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Publication number: 20020010316Abstract: 1Type: ApplicationFiled: June 11, 2001Publication date: January 24, 2002Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
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Patent number: 6331537Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.Type: GrantFiled: December 2, 1999Date of Patent: December 18, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Patent number: 6331639Abstract: A compound represented by the formula (1) which is useful as an agricultural fungicide or an intermediate thereof can be obtained by reacting a compound of the general formula (2) with a compound of the general formula (3) in the presence of an acid and reducing the resulted reaction mixture. wherein, each of R1 to R4 and R1a to R4a independently represents a hydrogen atom or an alkyl group, and R represents an alkyl group, alkoxy group, phenyl group or 5-membered or 6-membered heterocyclic group.Type: GrantFiled: February 20, 2001Date of Patent: December 18, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Hiroyuki Katsuta, Seiichi Ishii, Kanji Tomiya, Kenji Kodaka