Plural Ring Chalcogens In The Polycyclo Ring Sytem (e.g., Methylenedioxyphenyl Containing, Etc.) Patents (Class 548/526)
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Patent number: 7037669Abstract: Methods, compositions and kits are disclosed. Enzyme conjugates of Formula I may be employed in assays for the determination of an amphetamine and/or a methamphetamine. Immunogenic conjugates of Formula I may be employed to prepare antibodies for an amphetamine and/or for a methamphetamine for use in assays for the determination of an amphetamine and/or a methamphetamine. The enzyme conjugates may also be employed to screen antibodies for use in such methods.Type: GrantFiled: March 22, 2004Date of Patent: May 2, 2006Assignee: Dade Behring Inc.Inventors: Yi Feng Zheng, Khaled A. Yamout, Donald E. Berger, Jr., Mae W. Hu, Hshiou-ting Liu
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Patent number: 7022492Abstract: Methods, compositions and kits are disclosed. Enzyme conjugates of Formula I are employed in assays for the determination of an methylenedioxyamphetamine, a methylene-dioxyethamphetamine, and/or a methylenedioxymethamphetamine. Immunogenic conjugates of Formula I are employed to prepare antibodies for an methylenedioxyamphetamine, a methylenedioxyethamphetamine, and/or for a methylene-dioxymethamphetamine for use in assays for the determination of an methylenedioxyamphetamine, a methylenedioxyethamphetamine, and/or a methylene-dioxymethamphetamine. The enzyme conjugates may also be employed to screen antibodies for use in such methods.Type: GrantFiled: December 15, 2003Date of Patent: April 4, 2006Assignee: Dade Behring Inc.Inventors: Yi Feng Zheng, Yali Yang
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Patent number: 6991911Abstract: Methods, compositions and kits are disclosed. The methods are directed to determining the presence of entactogen analytes such as, for example, 3,4-methylenedioxyamphetamine (MDA), 3,4-methylenedioxy-methamphetamine (MDMA), 3,4-methylenedioxy-ethylamphetamine (MDEA) and 4-hydroxy-3-methoxy-methamphetamine (HMMA). The method comprises providing in combination in a medium (i) a sample suspected of containing the compound and (ii) an antibody raised against a compound of Formula I that comprises a protein. The medium is examined for the presence a complex comprising the compound and the antibody where the presence of such as complex indicates the presence of the compound in the sample. In one aspect of the above embodiment, the combination further comprises a label conjugate of the compound Formula I.Type: GrantFiled: December 15, 2003Date of Patent: January 31, 2006Assignee: Dade Behring Inc.Inventors: Yi Feng Zheng, Hshiou-ting Liu
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6960667Abstract: The present invention is directed to maleimides and preparation of compounds of the formula I wherein R1 and R2 independently from each other stand for variously substituted, and R3 stands for allyl, variously substituted, with the proviso, that R1 and R2 not simultaneously stand for phenyl.Type: GrantFiled: October 10, 2002Date of Patent: November 1, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
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Patent number: 6906098Abstract: Disclosed herein are mixed steroidal tetraoxanes having the following structural formula 1 wherein n is 0, 1, 2, or 3; R is H; ethanoyl, propanoyl, or benzoyl; R1 is H, methyl, ethyl, or isopropyl; R2 is H, methyl, or ethyl; R3 is H, methyl, or ethyl; R4 is H, methyl, ethyl, tert-butyl, phenyl, p-hydroxyphenyl, p-methoxyphenyl, or p-nitrophenyl, or wherein Y is a C1-C4 straight or branched-chain alkoxy, or wherein W is N, R5 is hydrogen, methyl, ethyl, n-propyl, isopropyl, or methyl ethanoate 2-yl, and R6 is hydrogen, methyl, ethyl, or n-propyl, or R5 and R6 are part of a pyrrolidine or piperidine ring; X is a C1-C4 straight or branched-chain alkoxy, a primary amino, a N-alkylamino wherein the alkyl is a straight-chain alkyl groups containing from 1 to 4 carbon atoms, methyl ethanoate-2-yl, N-phenylamino, p-nitrophenyl, N,N-dimethylamino, N,N-diethylamino, N,N-di(n-propyl)amino, N-pyrrolidino, or N-piperidino as single compounds, and any mixture of all possible stereoisomers at C(4?).Type: GrantFiled: February 7, 2003Date of Patent: June 14, 2005Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Bogdan Solaja, Dejan M. Opsenica, Gabriella Pocsfalvi, Wilbur K. Milhous, Dennis E. Kyle
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Patent number: 6903116Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequenc in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.Type: GrantFiled: January 9, 2003Date of Patent: June 7, 2005Assignee: Kaneka Corp.Inventors: Shin-ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara
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Patent number: 6900227Abstract: The present invention relates to compounds of the general formula and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such as obesity by selective modulation of CB1 receptors.Type: GrantFiled: July 24, 2003Date of Patent: May 31, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Konrad Bleicher, Wolfgang Guba, Wolfgang Haap, Dagmar Kube, Thomas Luebbers, Jean-Marc Plancher, Olivier Roche, Mark Rogers-Evans, Gisbert Schneider, Jochen Zuegge
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Patent number: 6890949Abstract: Novel amino ceramide-like compounds (1) are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: July 7, 2000Date of Patent: May 10, 2005Assignee: The Regents of the University of MichiganInventors: James A. Shayman, Norman S. Radin
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Patent number: 6887893Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.Type: GrantFiled: December 16, 1998Date of Patent: May 3, 2005Assignee: Sankyo Company, LimitedInventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
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Patent number: 6867230Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: June 1, 2001Date of Patent: March 15, 2005Assignee: Pfizer, Inc.Inventors: Matthew Merrill Hayward, Michael S. Visser, Robert G. Linde, II, Takushi Kaneko
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Patent number: 6855830Abstract: Disclosed is a novel enantiomeric synthesis cermamide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.Type: GrantFiled: July 16, 2002Date of Patent: February 15, 2005Assignee: Genzyme CorporationInventors: Bradford H. Hirth, Craig Siegel
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Patent number: 6849639Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a ?v?3, ?v?5, ?v?6, ?5?1 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 8, 2000Date of Patent: February 1, 2005Assignee: Amgen Inc.Inventors: Celia Dominguez, Guoqing Chen, Ning Xi, Shimin Xu, Nianhe Han, Qingyian Liu, Qi Huang, Aaron Siegmund, Michael Handley, Longbin Liu, Alexander Kiselyov
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Patent number: 6838478Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: April 30, 2001Date of Patent: January 4, 2005Assignee: AstraZeneca ABInventors: David Gustafsson, Jan-Erik Nyström
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Patent number: 6784167Abstract: 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl.Type: GrantFiled: September 28, 2001Date of Patent: August 31, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Jill E. Wood, Jeremy L. Baryza, Catherine R. Brennan, Soongyu Choi, James H. Cook, Brian R. Dixon, Paul P. Ehrlich, David E. Gunn, Ian McAlexander, Peiying Liu, Derek B. Lowe, Anikó M. Redman, William J. Scott, Yamin Wang
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Publication number: 20040142922Abstract: The present invention relates to compounds of the general formula 1Type: ApplicationFiled: July 24, 2003Publication date: July 22, 2004Inventors: Alexander Alanine, Konrad Bleicher, Wolfgang Guba, Wolfgang Haap, Dagmar Kube, Thomas Luebbers, Jean-Marc Plancher, Olivier Roche, Mark Rogers-Evans, Gisbert Schneider, Jochen Zuegge
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Publication number: 20040138288Abstract: This invention features compounds having formula (I): 1Type: ApplicationFiled: October 14, 2003Publication date: July 15, 2004Inventors: Qian Shi, Hui-Kang Wang, Masayoshi Oyama, John Robert Vance, Ming S. Chen
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Patent number: 6750213Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: April 11, 2002Date of Patent: June 15, 2004Assignee: Merck & Co., Inc.Inventors: Frank P. DiNinno, Jane Y. Wu, Seongkon Kim, Helen Y. Chen
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Patent number: 6747160Abstract: A 1,2-dioxetane derivative of the formula (I): wherein Ar is an aryl group which may have an alkyl group, an aryl group, a halogen atom, an alkoxyl group, a carboxyl group, a formyl group, an alkyl ester, an aryl ester, an alkylketone, an arylketone or a hetero ring bonded thereto, X is a substituent capable of labeling an organic compound or a biological molecule, or an ester, Y is a hydrogen atom, an acyl group or a group of the formula —Si(R4R5R6) (wherein each of R4, R5 and R6 which are independent of one another, is an alkyl group or an aryl group), Z is an alkyl group, an aryl group, an oxygen atom, a sulfur atom, a carbonyl group, —(CO)—O—, —O—(CO)—, —NH—, —NH—CO—, —CO—NH—, —OSi(R7R8)— (wherein each of R7 and R8 which are independent of each other, is an alkyl group or aryl group) or a group of the formula —(R9R10)SiO— (wherein each of R9 and R10 which are independent of eType: GrantFiled: March 7, 2003Date of Patent: June 8, 2004Assignee: Tosoh CorporationInventors: Masakatsu Matsumoto, Nobuko Watanabe, Masashi Yamada
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Publication number: 20040044058Abstract: The present invention provides a novel 4′-demethyl-4′-O-substituted-1-deoxypodophyllotoxin derivative, a geometric isomer thereof, a process for the preparation thereof, and an anticancer composition comprising the same.Type: ApplicationFiled: April 28, 2003Publication date: March 4, 2004Inventors: Song-Bae Kim, Byung-Zun Ahn, Yong Kim, Young-Jae You
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Patent number: 6673829Abstract: Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.Type: GrantFiled: September 12, 2002Date of Patent: January 6, 2004Assignee: Novo Nordisk A/SInventors: Florencio Zaragoza Dorwald, Rolf Hohlweg
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Publication number: 20030225132Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: ApplicationFiled: March 11, 2003Publication date: December 4, 2003Inventors: Frank P. DiNinno, Milton Lloyd Hammond
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Publication number: 20030216435Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: ApplicationFiled: July 23, 2002Publication date: November 20, 2003Applicant: G. D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6646123Abstract: The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R311 an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: April 22, 2002Date of Patent: November 11, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Publication number: 20030207864Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: ApplicationFiled: March 11, 2003Publication date: November 6, 2003Applicant: Tulark Inc.Inventor: Jonathan B. Houze
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Patent number: 6632833Abstract: The invention relates to novel 2-(2-methylphenyl)-3,4-dihydro-2H-pyrrole derivatives of the formula (I) in which Ar represents substituted phenyl, to a plurality of processes for their preparation and to their use as pesticides.Type: GrantFiled: November 13, 2000Date of Patent: October 14, 2003Assignee: Bayer AktiengesellschaftInventors: Andrew Plant, Dirk Backhaus, Christoph Erdelen, Andreas Turberg, Norbert Mencke
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Publication number: 20030189191Abstract: Fluorescent maleimides of the formula I 1Type: ApplicationFiled: October 10, 2002Publication date: October 9, 2003Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
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Patent number: 6613780Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.Type: GrantFiled: August 27, 2001Date of Patent: September 2, 2003Assignee: Kaneka CorporationInventors: Shin-ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara
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Publication number: 20030153768Abstract: Disclosed is a method of preparing a composition comprising a compound represented Structural Formula (I): 1Type: ApplicationFiled: November 26, 2002Publication date: August 14, 2003Applicant: Genzyme CorporationInventor: Bradford H. Hirth
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Publication number: 20030149077Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor.Type: ApplicationFiled: January 9, 2003Publication date: August 7, 2003Inventors: Shin-Ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara
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Publication number: 20030139389Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: December 11, 2002Publication date: July 24, 2003Applicant: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Publication number: 20030134852Abstract: This invention concerns the compounds of formula (I), 1Type: ApplicationFiled: November 12, 2002Publication date: July 17, 2003Inventors: Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea, Pilar Gil-Lopetegui, Adolfo Diaz-Martinez
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Patent number: 6569889Abstract: Novel amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: May 31, 2001Date of Patent: May 27, 2003Assignee: The Regents of the University of MichiganInventors: James A. Shayman, Norman S. Radin
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Publication number: 20030087945Abstract: Compounds of formula (I) 1Type: ApplicationFiled: June 13, 2002Publication date: May 8, 2003Applicant: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Publication number: 20030087955Abstract: This invention provides estrogen receptor modulators of formula 1, having the structure 1Type: ApplicationFiled: May 15, 2002Publication date: May 8, 2003Applicant: WyethInventors: Christopher P. Miller, Michael D. Collini, Heather A. Harris, James C. Keith
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Patent number: 6552016Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: GrantFiled: October 13, 2000Date of Patent: April 22, 2003Assignee: Curis, Inc.Inventors: Anthony David Baxter, Edward Andrew Boyd, Oivin M. Guicherit, Stephen Price, Lee Rubin
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Publication number: 20030073680Abstract: The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: ApplicationFiled: April 29, 2002Publication date: April 17, 2003Applicant: The Regents of The University of MichiganInventors: James A. Shayman, Norman S. Radin
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Patent number: 6545151Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31 (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: January 16, 2001Date of Patent: April 8, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Patent number: 6544992Abstract: The present invention relates to pyrrolyl and pyridyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of urotensin II.Type: GrantFiled: June 13, 2002Date of Patent: April 8, 2003Assignee: SmithKline Beecham CorporationInventors: Dashyant Dhanak, Steven David Knight, Jian Jin, Richard McCulloch Keenan
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Publication number: 20030060472Abstract: New compounds of formula I are described: 1Type: ApplicationFiled: June 20, 2001Publication date: March 27, 2003Inventors: David Alexander Learmonth, Patricio Manuel Vieira Araujo Soares da Silva
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Patent number: 6534491Abstract: This invention provides, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stroinelysins and collagenases) and TNF-&agr; converting enzyme (TACE, tumor necrosis factor-&agr;converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated.Type: GrantFiled: December 11, 2000Date of Patent: March 18, 2003Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Arie Zask, Yansong Gu, Jay D. Albright, Xuemei Du
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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: 6514970Abstract: The present invention relates to pyrrolidiones, pharmaceutical compostions containing them and their use as antagonist of urotensin II.Type: GrantFiled: June 13, 2002Date of Patent: February 4, 2003Assignee: SmithKline Beecham CorporationInventors: Dashyant Dhanak, Steven David Knight, Gregory Lee Warren, Jian Jin, Katherine L. Widdowson, Richard McCulloch Keenan
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Patent number: 6511976Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.Type: GrantFiled: April 6, 2000Date of Patent: January 28, 2003Assignee: Jannsen Pharmaceutica, N.V.Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui, Adolfo Díaz-Martinez
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Publication number: 20020193419Abstract: Compounds which are prodrugs of triptolide or its derivatives, containing an amino acid or oligopeptide moiety, are used for anticancer or immunosuppressive treatment.Type: ApplicationFiled: March 14, 2002Publication date: December 19, 2002Inventors: Dongcheng Dai, John M. Fidler, John H. Musser
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Publication number: 20020156107Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: ApplicationFiled: January 10, 2002Publication date: October 24, 2002Inventors: James A. Shayman, Norman S. Radin
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Patent number: 6462041Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.Type: GrantFiled: February 1, 2000Date of Patent: October 8, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe
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Patent number: 6440899Abstract: Cyclohexenonedioxothiochromanoyl derivatives of the formula I where X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, the other substituents are as defined in the specification, and and agriculturally useful salts thereof; processes for preparing the cyclohexenonedioxotheiochromanoyl derivatives; compositions comprising them, and the use of these derivatives or of compositions comprising them for controling undesirable piants.Type: GrantFiled: October 30, 2000Date of Patent: August 27, 2002Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Roland Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6407134Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: February 5, 2001Date of Patent: June 18, 2002Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Publication number: 20020058679Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor.Type: ApplicationFiled: August 27, 2001Publication date: May 16, 2002Inventors: Shin-Ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara