Plural Hetero Rings Patents (Class 549/414)
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Patent number: 7442793Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: December 11, 2003Date of Patent: October 28, 2008Assignee: SmithKline Beecham CorporationInventors: Jinhwa Lee, Siegfried B. Christensen, IV
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Publication number: 20080249165Abstract: The invention relates to new polysulfated glycosides of formula (I), the salts thereof formed with alkali metals or alkaline-earth metals, as well as the pharmaceutical compositions containing these compounds as active ingredients. Furthermore the invention provides a method of preventing, treating or alleviating the symptoms of acute and chronic inflammatory disorders of the airways of mammals—including asthma and asthma-related pathologies.Type: ApplicationFiled: August 5, 2005Publication date: October 9, 2008Applicant: Ivax Drug Research Institute Ltd.Inventors: Janos Kuszmann, Istvan Kurucz, Gabor Medgyes, Nicholas Bodor
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Publication number: 20080249322Abstract: Processes are provided for preparing mupirocin calcium dihydrate from pseudomonic acid in a two phase system by using an organic carboxylate. A highly pure composition of amorphous mupirocin calcium is provided, and processes for its preparation by solvent removal, lyophilization and precipitation with use of an anti-solvent. Pharmaceutical compositions of amorphous form, and methods of using them to treat infections are also provided. Also provided are combined processes for preparing mupirocin calcium dihydrate and amorphous, by producing amorphous form first, followed by conversion of amorphous form into the dihydrate through crystallization from an aqueous solution. Also provided are processes for removing the water of crystallization of the dihydrate to obtain mupirocin calcium anhydrate.Type: ApplicationFiled: July 7, 2006Publication date: October 9, 2008Inventors: Lorant Gyuricza, Erszebet Meszaros-Sos, Csaba Szabo, Claude Singer
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Publication number: 20080234503Abstract: A method for purification of the antibiotic mupirocin (pseudomonic acid A) which comprises: a) Causing or allowing precipitation of mupirocin from an aqueous solution thereof; b) Recovering the precipitate; c) Dissolving the recovered precipitate in an organic solvent.Type: ApplicationFiled: February 21, 2006Publication date: September 25, 2008Applicant: ALPHARMA APSInventors: Marc Antonius Theodorus Bisschops, Tiemen Geert Pieter Reijns, Anita Mathiesen, Lene Aassveen
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Patent number: 7351730Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.Type: GrantFiled: June 22, 2005Date of Patent: April 1, 2008Assignee: WyethInventors: Scott Christian Mayer, Eric Gould Gundersen, Hassan Mahmoud Elokdah, David LeRoy Crandall
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Publication number: 20070247585Abstract: Disclosed are hexahydrodibenzofuran compounds of formula I, the preparation thereof, the use thereof as components in liquid-crystalline media, and to electro-optical display elements which contain the liquid-crystalline media according to the invention.Type: ApplicationFiled: April 24, 2007Publication date: October 25, 2007Inventors: Axel Jansen, Andreas Taugerbeck, Melanie Klasen-Memmer
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Patent number: 7230114Abstract: Compounds of formula (I), methods for their preparation and their use in the manufacture of neuraminidase inhibitor conjugates.Type: GrantFiled: August 30, 2002Date of Patent: June 12, 2007Assignee: Biota Scientific Management Pty LtdInventors: Brian David Judkins, Simon John Fawcett MacDonald, Derek Anthony Demaine, Graham George Adam Inglis, Julie Nicole Hamblin
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Patent number: 7153885Abstract: Naturally occurring stolonoxide compounds, and derivatives thereof, have antitumor activity.Type: GrantFiled: May 4, 2001Date of Patent: December 26, 2006Assignee: Universidad de CadizInventors: Rosario Duran, Eva Zubia, Maria J. Ortega, Javier Salva, Jose Luis Fernandez Puentes, Dolores Garcia Gravalos, Santiago Naranjo Lozano
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Patent number: 7045535Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.Type: GrantFiled: March 8, 2002Date of Patent: May 16, 2006Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Pooran Chand, Yarlagadda S. Babu, R. Scott Rowland, Tsu-Hsing Lin
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Patent number: 6992083Abstract: The invention relates to compounds of formula wherein R is phenyl, unsubstituted or substituted by halogen or —CH2N(CH3)(CH2)nOCH3, or is benzyl, lower alkyl, lower alkoxy, —(CH2)nOCH3, or is pyridin 3 -or 4-yl, unsubstituted or substituted by lower alkyl, halogen, morpholinyl, —(CH2)n-halogen, —(CH2)nOCH3, —(CH2)n-morpholin-4-yl, or —(CH2)n-pyrrolidin-1-yl; R1 is phenyl, unsubstituted or substituted by halogen, tetrahydropyran-4-yl, 3,6-dihydro-2H-pyran-4-yl or morpholin-4-yl; n is independently from each other 1 or 2; and to pharmaceutically acceptable salts thereof for the treatment of diseases related to the adenosine A2A-receptor.Type: GrantFiled: January 9, 2004Date of Patent: January 31, 2006Assignee: Hoffman-La Roche Inc.Inventor: Roger David Norcross
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Patent number: 6939886Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.Type: GrantFiled: July 20, 2004Date of Patent: September 6, 2005Assignee: WyethInventors: Scott Christian Mayer, Eric Gould Gundersen, Hassan Mahmoud Elokdah, David LeRoy Crandall
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Patent number: 6902777Abstract: A liquid-crystalline mediums which contain one or more compounds of the formula A and at least one compound of the formula B wherein compounds of formula A contain at least one ring selected from and in which Ra, Rb, ring A and ring B, Y, Z1, Z2, a, L1, L2, L3, L4, L5, L6, L7, L8 and L9 are as defined herein, are suitable for use in twisted nematic (TN) and supertwisted nematic (STN) liquid-crystal displays. Such displays have very short response times and good steepnesses and angle dependencies.Type: GrantFiled: December 22, 2003Date of Patent: June 7, 2005Assignee: Merck Patent GmbHInventors: Harald Hirschmann, Eike Poetsch, Peer Kirsch, Sabine Schoen
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Patent number: 6900160Abstract: The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.Type: GrantFiled: September 21, 2001Date of Patent: May 31, 2005Assignee: Gesellschaft fuer Biotechnologische Forschung mbHInventors: Gerhard Hoefle, Nicole Glaser
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Patent number: 6869696Abstract: The invention concerns an electro-luminescent device in which the luminescent layer contains a compound of general formula I as doping agent or as luminescent compound, whereby the radicals R1 to R12 are identical or are different, and mean hydrogen, straight chain or branched C1-C6 alkyl, aralkyl, aryl or substituted aryl; R1 and R2 and/or R3 and R4 and/or R4 and R5 and/or R5 and R11 and/or R8 and R5 and/or R4 and R12 can form an alicyclic, heterocyclic or aromatic ring; R5 can furthermore be H, OH, OR9, N,N-di-(C1-C6) alkylamino, acetylamino or halogen; R6 and R7 together can form an alicyclic or heterocyclic ring; A1 and A2 are identical or different and are —CN, —NO2 or —COOR8; X is —CH, —CR11 or N; and Y is O, —NH, —NR12, S or Se. The doping agents together luminesce predominately red with very good quantum efficiency together with the luminescent compound as a function of concentration.Type: GrantFiled: May 10, 2002Date of Patent: March 22, 2005Assignee: Sensient Imaging Technologies GmbHInventors: Andreas Richter, Dietmar Keil, Gerhard Diener
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Patent number: 6835845Abstract: A is a novel methine compound, for example, which is represented by the following formula (I): wherein R1, R2, R3, R4 and R5 each represents a hydrogen atom or a substituent; X represents an oxygen atom, a sulfur atom, or N—R6; Z represents —NR7R8, or —OG; R6, R7 and R8 each represents a hydrogen atom or a substituent; G represents a hydrogen atom, a cation or a substituent; L1, L2 and L3 each represents a substituted or unsubstituted methine group; n represents 1 or 2; and W represents an electron attractive group. Also, a material for organic luminescence element and organic luminescence element using the same are disclosed.Type: GrantFiled: July 26, 2002Date of Patent: December 28, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Okada, Terukazu Yanagi
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Patent number: 6800654Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are eachH, alkyl,, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.Type: GrantFiled: June 13, 2002Date of Patent: October 5, 2004Assignee: WyethInventors: Scott Christian Mayer, Eric Gould Gundersen, Hassan Mahmoud Elokdah, David LeRoy Crandall
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Patent number: 6740649Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.Type: GrantFiled: September 16, 2002Date of Patent: May 25, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
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Publication number: 20040059138Abstract: The present invention provides novel dihydropyrancarboxamide compounds of formula (I): 1Type: ApplicationFiled: August 27, 2003Publication date: March 25, 2004Inventors: Stuart L. Schreiber, Robert A. Stavenger, Timothy J. Mitchison, Zoltan Maliga
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Publication number: 20040024052Abstract: Processes are provided for preparing mupirocin calcium dihydrate from pseudomonic acid in a two phase system by using an organic carboxylate.Type: ApplicationFiled: November 6, 2002Publication date: February 5, 2004Inventors: Lorant Gyuricza, Erszebet Meszaros-Sos, Csaba Szabo, Claude Singer
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Patent number: 6677355Abstract: Compounds of the formula; are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues. Also disclosed are methods for the preparation of such compounds, pharmaceutical compositions including the same, and methods of treating diseases in which matrix metalloproteinases are involved including multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: February 13, 2002Date of Patent: January 13, 2004Assignee: Warner-Lambert CompanyInventors: Christopher Alan Conrad, Patrick Michael O'Brien, Daniel Fred Ortwine, Joseph Armand Picard, Drago Robert Sliskovic
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Publication number: 20040006227Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: January 31, 2003Publication date: January 8, 2004Inventors: Michael S. South, Chun C Ma, Kevin J Koeller, Hayat K Rahman, William L Neumann
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Publication number: 20030236299Abstract: The present invention provides hydroxy pyranone derivatives and a method for preparing the hydroxy pyranone derivatives. The hydroxy pyranone derivatives of the present invention are significantly effective in promoting the biosynthesis of collagen and in inhibiting the activity of collagenase, i.e. an enzyme for decomposing collagen, to have anti-wrinkle efficacy, and can be incorporated into medicines or external applications for lessening skin-wrinkles.Type: ApplicationFiled: May 9, 2003Publication date: December 25, 2003Inventors: Ho Sik Roh, Su Nam Kim, Bae Hwan Kim, Hae Kwang Lee, Duck Hee Kim, Ih Seop Chang, Ok Sub Lee
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Publication number: 20030228486Abstract: The invention concerns an electro-luminescent device in which the luminescent layer contains a compound of general formula I as doping agent or as luminescent compound, whereby the radicals R1 to R12 are identical or are different, and mean hydrogen, straight chain or branched C1-C6 alkyl, aralkyl, aryl or substituted aryl; R1 and R2 and/or R3 and R4 and/or R4 and R5 and/or R5 and R11 and/or R8 and R5 and/or R4 and R12 can form an alicyclic, heterocyclic or aromatic ring; R5 can furthermore be H, OH, OR9, N,N-di-(C1-C6) alkylamino, acetylamino or halogen; R6 and R7 together can form an alicyclic or heterocyclic ring; A1 and A2 are identical or different and are -CN, -NO2 or -COOR8; X is -CH, -CR11 or N; and Y is O, -NH, -NR12, S or Se. The doping agents together luminesce predominately red with very good quantum efficiency together with the luminescent compound as a function of concentration.Type: ApplicationFiled: May 10, 2002Publication date: December 11, 2003Applicant: SynTec Gesellschaft fuer Chemie und Technologie der Informationsaufzeichnung mbHInventors: Andreas Richter , Dietmar Keil , Gerhard Diener
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Patent number: 6642395Abstract: There are provided an acetalsulfonate derivative useful as an intermediate for medicines and agricultural chemicals, a process for industrially producing the derivative, and a process for industrially producing a styrene oxide derivative from the acetalsulfonate derivative or from a mandelic acid derivative. A process for producing an acetalsulfonate derivative which comprises a first step of esterifying a mandelic acid derivative to form a mandelic ester derivative, a second step of protecting the mandelic ester derivative by an acetal to form an acetal derivative, a third step of reducing the acetal derivative to form an ethanediol derivative and a fourth step of reacting the ethanediol derivative with a sulfonyl chloride derivative. A process for producing a styrene oxide derivative which comprises a deprotecting step of deacetalizing the acetalsulfonate derivative and a step of epoxidizing the sulfonate derivative obtained in the deprotecting step with the aid of a base catalyst.Type: GrantFiled: May 29, 2002Date of Patent: November 4, 2003Assignee: Mitsubishi Rayon Co., Ltd.Inventors: Hiroyuki Mori, Hikari Morita, Yoshimasa Kobayashi
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Patent number: 6613743Abstract: The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. The sulfonamides of formula I have the structure: wherein A, B, D, D′, E, G and R7 are as defined above.Type: GrantFiled: December 6, 2000Date of Patent: September 2, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Robin Hale, Clarence Webster Andrews, III, Eric Steven Furfine, Ronald George Sherrill, Andrew Spaltenstein, Gregory Thomas Lowen
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Patent number: 6599925Abstract: This invention provides compounds which act as inhibitors of plasminogen activator inhibitor-1 (PAI-1) of the formula: wherein: R, R1, R2, and R3 are H, alkyl, cycloalkyl, —CH2-(cycloalkyl), alkanoyl, halo, hydroxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, perfluoroalkyl, alkoxy, amino, —NH(alkyl), —N(alkyl)2, or perfluoroalkoxy; R4 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl, aryl, —CH2R5, —CH(OH)R5, —C(O)R5, —CH(SH)R5, or —C(S)R5; R5 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl; R6 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkylaryl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is an integer of 0-6; A is COOH, or an acid mimic; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds to treatType: GrantFiled: June 18, 2002Date of Patent: July 29, 2003Assignee: WyethInventors: Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, Scott Christian Mayer, David LeRoy Crandall
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Publication number: 20030127975Abstract: A red-emitting organic electroluminescent compound, the structure of the compound as follows: 1Type: ApplicationFiled: December 5, 2002Publication date: July 10, 2003Applicant: CHI MEI OPTOELECTRONICS CORPORATIONInventors: Ruey-Min Chen, Jun-Wen Chung, Chun-Che Hsu
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Publication number: 20030080323Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1Type: ApplicationFiled: July 26, 2002Publication date: May 1, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Hisashi Okada, Terukazu Yanagi
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Publication number: 20030013744Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders.Type: ApplicationFiled: July 1, 2002Publication date: January 16, 2003Applicant: G.D. Searle & Co.Inventors: John J. Talley, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Roland S. Rogers
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Patent number: 6500958Abstract: The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.Type: GrantFiled: June 24, 2002Date of Patent: December 31, 2002Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Publication number: 20020177723Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.Type: ApplicationFiled: April 11, 2000Publication date: November 28, 2002Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T.Y. Shen
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Patent number: 6469182Abstract: Novel intermediates of the formula They are used in the preparation of macrocyclic analogs.Type: GrantFiled: April 26, 2001Date of Patent: October 22, 2002Assignee: Eisai Co., Ltd.Inventors: Bruce A. Littlefield, Monica H. Palme, Boris M. Seletsky, Murray J. Towle, Melvin J. Yu, Wanjun Zheng
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Patent number: 6420334Abstract: 2-Alkoxydecahydro-2,3a,4,4,7-pentamethyl-3,7a-methano-7aH-indeno[5,6-b]furans are valuable novel woody fragrances for the preparation of perfume oils.Type: GrantFiled: June 30, 2000Date of Patent: July 16, 2002Assignee: Haarmann & Reimer GmbHInventors: Horst Surburg, Peter Wörner
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Patent number: 6413947Abstract: This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an, optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.Type: GrantFiled: September 13, 2000Date of Patent: July 2, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
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Patent number: 6403636Abstract: This invention relates to novel xanthone compounds, their preparation and use as medicament. More particularly this invention is directed to the isolation of the novel xanthone natural product sootepenseone from Dasymaschalon sootepense Craib, Annonaceae, its identification and derivatization, and the use of sootepenseone and its derivatives as anticancer agents.Type: GrantFiled: June 28, 2000Date of Patent: June 11, 2002Assignee: Zentaris AGInventors: Vichai Reutrakul, Thaiwatchai Santisuk, Gerhard Noessner, Juergen Schmidt, Bernd Nickel, Thomas Klenner, Sebastian Hose
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Patent number: 6403777Abstract: Transition metal complexes, referred to hereinafter as “metalloligands”, that catalyze the degradation of DNA and the cleavage of RNA at select sites are provided. In one embodiment, the metalloligand has the following structure: wherein R1 is an amino group, i.e. an NH, or an alkylamino group comprising 1 or 2 carbon atoms; wherein R2 is selected from the group consisting of an amino group, a hydroxyl group, i.e., O(H), an alkylamino group comprising 1 or 2 carbon atoms; and an alkylhydroxyl group comprising 1 or 2 carbon atoms; wherein J is a ligand which comprises at least one carbon-containing five-membered or six-membered ring structure; and wherein M is a transition metal ion which is bound via coordinate bonds to R1 and R2.Type: GrantFiled: July 6, 1999Date of Patent: June 11, 2002Assignee: The Ohio State University Research FoundationInventor: James A. Cowan
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Patent number: 6399786Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: July 9, 2001Date of Patent: June 4, 2002Assignee: Merck & Co., Inc.Inventors: Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Matthew J. Wyvratt
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Patent number: 6365751Abstract: The invention concerns a compound of the formula (I): wherein, for example: R1 is of the formula —NHC(═O)Rb wherein Rb is, for example, (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; R2 and R3 are hydrogen or fluoro; D is O; R4 and R5 are hydrogen, (1-4C)alkyl or AR-oxymethyl; AR is phenyl or phenyl(1-4C)alkyl; R6 is hydrogen; >A—B— is of the formula >C═C(Ra)—, >CHCHRa—, or >C(OH)CHRa— (> represents two single bonds) wherein Ra is hydrogen or (1-4C)alkyl; and pharmaceutically-acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.Type: GrantFiled: April 17, 2001Date of Patent: April 2, 2002Assignee: Zeneca Ltd.Inventor: Michael Barry Gravestock
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Patent number: 6365759Abstract: Intermediate compounds of the formulas for use in the preparation of macrocyclic analogs.Type: GrantFiled: October 2, 2000Date of Patent: April 2, 2002Assignee: Eisai Co., Ltd.Inventors: Bruce A. Littlefield, Monica H. Palme, Boris M. Seletsky, Murray J. Towle, Melvin J. Yu, Wanjun Zheng
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Patent number: 6331563Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: GrantFiled: June 5, 2000Date of Patent: December 18, 2001Inventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jannie Lea Baker
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Patent number: 6319946Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 9, 2000Date of Patent: November 20, 2001Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, Francois Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano
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Patent number: 6306893Abstract: An object of the invention is to develop galactose or mannose derivatives of docetaxel, etc. having improved solubility and physiological activity, to alleviate burden imposed on patients and to provide effective therapeutic drug for tumors. The present invention provides taxoid derivatives comprising any of paclitaxel, docetaxel and 10-deacetyl-baccatin III to which galactose or mannose is linked through a spacer, and methods for producing taxoid derivatives comprising reacting paclitaxel, docetaxel or 10-deacetyl-baccatin III with tetrabenzyl acetyloxygalactoside or tetrabenzyl acetyloxymannoside, subjecting the product to debenzylation reaction, and optionally to detriethylsilylation reaction.Type: GrantFiled: April 7, 2000Date of Patent: October 23, 2001Assignees: Ensuiko Sugar Refining Company, Ltd, Bio Research Corporation of Yokohama, Kaken Pharmaceutical Company, Ltd.Inventors: Tadakatsu Mandai, Hiroshi Okumoto, Koji Hara, Katsuhiko Mikuni, Kozo Hara, Yoshinori Tsuchiya, Kosho Nakamura, Teruhiko Umetsu
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Patent number: 6245804Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.Type: GrantFiled: May 29, 1998Date of Patent: June 12, 2001Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Patent number: 6150532Abstract: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.Type: GrantFiled: December 11, 1998Date of Patent: November 21, 2000Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 6133442Abstract: Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.Type: GrantFiled: March 5, 1999Date of Patent: October 17, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz -
Patent number: 6127157Abstract: The present invention provides a coating suitable for coating woods, and the coating is obtained by dissolving proanthocyanidine into water or a water-containing alcohol.Type: GrantFiled: May 3, 1999Date of Patent: October 3, 2000Assignees: Kikkoman Corporation, Noda Institute for Scientific ResearchInventors: Osamu Hatamoto, Eiichi Nakano
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Patent number: 6113812Abstract: A photochromic article that includes a host material and a photochromic amount of a benzopyran compound, the benzopyran compound represented by one of the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.Type: GrantFiled: August 4, 1997Date of Patent: September 5, 2000Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6054475Abstract: Compounds of formula (I) ##STR1## and the salts of these compounds, are efficacious PDE (phosphodiesterase) inhibitors.Type: GrantFiled: April 16, 1999Date of Patent: April 25, 2000Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventors: Thomas Martin, Wolf-Rudiger Ulrich
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Patent number: RE37035Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: October 7, 1997Date of Patent: January 30, 2001Assignee: Boehringer Ingelheim KGInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht