Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The Oxazole Ring By Nonionic Bonding Patents (Class 548/248)
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Patent number: 6620832Abstract: The invention is directed to physiologically active compounds of general formula (I): wherein R1 is lower alkyl, R2 is aryl, arylalkyl, heteroaryl or heteroarylalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a cyclic amine, Ar1 is aryldiyl or heteroaryldiyl, Ar2 is optionally substituted phenylene or heteroaryldiyl, L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z1)—NR4—, —NR4—C(═Z1)—, —Z1—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z1)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—, —NR4—C(═O)—O— or —O—C(═O)—NR4—, L2 is a direct bond, an optionally substituteType: GrantFiled: November 2, 2001Date of Patent: September 16, 2003Assignee: Aventis Pharma Ltd.Inventor: Paul Robert Eastwood
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Publication number: 20030166945Abstract: The invention relates to a crystal modification of the compound of the formula I 1Type: ApplicationFiled: November 25, 2002Publication date: September 4, 2003Applicant: Hoechst Marion Deutschland GmbHInventors: Holger Faasch, Udo Hedtmann, Uwe Westenfelder, Erich Paulus
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Patent number: 6610718Abstract: New leflunomide Form III is disclosed, along with processes for preparing it. The present invention also provides an economic process for preparing leflunomide Form II and a process for preparing leflunomide Form I from leflunomide Form III. Pharmaceutical compositions and dosage forms containing the new form and methods of using them for the treatment of rheumatoid arthritis are also disclosed.Type: GrantFiled: December 14, 2000Date of Patent: August 26, 2003Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Ilya Avrutov, Neomi Gershon, Judith Aronhime
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Publication number: 20030153465Abstract: The invention relates to novel substituted aryl ketones of the general formula (I) 1Type: ApplicationFiled: July 15, 2002Publication date: August 14, 2003Inventors: Otto Schallner, Stefan Lehr, Hans-Georg Schwarz, Klaus-Helmut Muller, Dorothee Hoischen, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Akihiko Yanagi, Shinichi Narabu, Toshio Goto
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Publication number: 20030139606Abstract: A process for preparing 5-methylisoxazole-4-carboxylic-(4′-trifluoromethyl)-anilide comprising: (a) reacting ethylacetoacetate, triethylorthoformate, and acetic anhydride at a temperature of from about 75° C. to about 150° C., to form ethyl ethoxymethyleneacetoacetic ester; (b) combining the ethyl ethoxymethyleneacetoacetic ester with sodium acetate or a salt of trifluoroacetic acid in the presence of hydroxylamine sulfate at a temperature of from about −20° C. to 10° C., to form ethyl-5-methylisoxazole-4-carboxylate; (c) reacting the ethyl-5-methylisoxazole-4-carboxylate with a strong acid to form 5-methylisoxazole-4-carboxylic acid; (d) reacting the crystallized 5-methylisoxazole-4-carboxylic acid with thionyl chloride to form 5-methylisoxazole-4-carbonyl chloride; and (e) reacting the 5-methylisoxazole-4-carbonyl chloride with trifluoromethyl aniline and an amine base at a temperature of from about 0° C. to about 50° C.Type: ApplicationFiled: November 5, 2002Publication date: July 24, 2003Inventors: Anup Kumar Ray, Hiren Kumar V. Patel, Mahendra R. Patel
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Patent number: 6579880Abstract: The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of IL-8 and are thus useful as anti-inflammatory agents for a variety of diseases.Type: GrantFiled: June 6, 2001Date of Patent: June 17, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michele A. Weidner-Wells, Todd C. Henninger, Dennis J. Hlasta
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Patent number: 6562816Abstract: The invention provides compounds of Formula I: compounds of the Formula I: wherein R1, R2, R4, R6, X, and W are defined herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which &agr;7 is known to be involved.Type: GrantFiled: August 14, 2002Date of Patent: May 13, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Donn G. Wishka, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, David W. Piotrowski, Jeffrey W. Corbett, Alice L. Bodnar, Vincent E. Groppi, Jr.
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Publication number: 20030083348Abstract: 1 This invention relates to compounds of formula (1) that inhibit farnesylation of gene products through inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation.Type: ApplicationFiled: April 17, 2002Publication date: May 1, 2003Inventors: James Michael Wardleworth, Francis Thomas Boyle, Zbigniew Matusiak
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Patent number: 6552202Abstract: The invention relates to a crystal modification of the compound of the formula I and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type 11 diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.Type: GrantFiled: January 19, 2001Date of Patent: April 22, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Faasch, Udo Hedtmann, Uwe Westenfelder, Erich Paulus
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Patent number: 6531452Abstract: Peptido and peptidomimetic compounds of the formula: wherein 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 provided.Type: GrantFiled: April 29, 1999Date of Patent: March 11, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Peter Scott Dragovich, Stephen Evan Webber, Thomas Jay Prins, Ru Zhou, Joseph Timothy Marakovits, Theodore O. Johnson, Jr.
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Patent number: 6531498Abstract: The invention relates to compounds of formula I and to their physiologically acceptable salts and solvates which act as phosphodiesterse VII inhibitors and are thus useful for the treatment of allergic disorders, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin disorders, inflammatory disorders, autoimmune diseases, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumor growth, tumor metastases, sepsis, memory disturbances, atherosclerosis and AIDS.Type: GrantFiled: May 3, 2002Date of Patent: March 11, 2003Assignee: Merck PatentgesellschaftInventors: Hans-Michael Eggenweiler, Rochus Jonas, Michael Wolf, Michael Gassen, Thomas Welge
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Publication number: 20030045560Abstract: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: 1Type: ApplicationFiled: June 13, 2002Publication date: March 6, 2003Applicant: WyethInventors: Thomas Joseph Commons, Susan Christman Croce, Richard Page Woodworth, Eugene John Trybulski, Hassan Mohmoud Elokdah, David LeRoy Crandall
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Publication number: 20030027851Abstract: The invention relates to a crystal modification of the compound of the formula I 1Type: ApplicationFiled: January 19, 2001Publication date: February 6, 2003Applicant: Hoechst Marion Deutschland GmbHInventors: Holger Faasch, Udo Hedtmann, Uwe Westenfelder, Erich Paulus
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Patent number: 6495696Abstract: A process for the preparation of a compound of formula (I) wherein: R1 is cycloalkyl having from three to six ring carbon atoms which is unsubstituted or which has one or more substituents selected from the group consisting of R4 and halogen.Type: GrantFiled: May 10, 2002Date of Patent: December 17, 2002Assignee: EagleView Technologies, Inc.Inventor: Jack S. Warren
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Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
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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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Publication number: 20020123493Abstract: The present invention relates to cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: September 5, 2002Inventors: Michael Mullican, David Lauffer
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Publication number: 20020086985Abstract: Novel linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye are provided. These linkers faciliate the efficient transfer of energy between a donor and acceptor dye in an energy transfer dye. One of these linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye has the general structure R21Z1C(O)R22R28 where R21 is a C1-5 alkyl attached to the donor dye, C(O) is a carbonyl group, Z1 is either NH, sulfur or oxygen, R22 is a substituent which includes an alkene, diene, alkyne, a five and six membered ring having at least one unsaturated bond or a fused ring structure which is attached to the carbonyl carbon, and R28 includes a functional group which attaches the linker to the acceptor dye.Type: ApplicationFiled: October 29, 2001Publication date: July 4, 2002Inventors: Linda G. Lee, Sandra L. Spurgeon, Barnett Rosenblum
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Publication number: 20020077485Abstract: The present invention relates to leflunomide having relatively small particles, and corresponding relatively large surface area. In one embodiment, the invention relates to leflunomide and formulations containing leflunomide having a mean particle diameter of less than 200 micrometers.Type: ApplicationFiled: August 14, 2001Publication date: June 20, 2002Inventor: Ilya Avrutov
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Patent number: 6395724Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.Type: GrantFiled: June 7, 1999Date of Patent: May 28, 2002Assignee: Advanced Medicine, Inc.Inventors: J. Kevin Judice, Deborah L. Higgins, John H. Griffin
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Patent number: 6391901Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: May 21, 2002Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Alan D Palkowitz, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Publication number: 20020045551Abstract: 4-Benzoylisoxazole derivatives of formula (I), wherein R 1Type: ApplicationFiled: September 28, 2001Publication date: April 18, 2002Inventors: Tibor Musil, Simon Neil Pettit, Philip Henry Gaunt Smith
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Patent number: 6355807Abstract: Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes.Type: GrantFiled: August 23, 2000Date of Patent: March 12, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Qingping Tian, Naresh K. Nayyar, Srinivasan Babu, Junhua Tao, Terence Jarold Moran, Raymond Dagnino, Jr., Lennert J. Mitchell, Jr., Travis Paul Remarchuk, Michael Joseph Melnick, Steven Lee Bender
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Publication number: 20020022646Abstract: A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided. Further provided is the leflunomide prepared by the inventive process, which is substantially free of difficult-to-separate impurities often found in leflunomide prepared by known methods, including N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 5-methyl-N-(4-methylphenyl)-isoxazole-4-carboxamide and N-(4-trifluoromethylphenyl)-3-methyl-isoxazole-4-carboxamide. The invention further provides pharmaceutical compositions and dosage forms containing highly pure leflunomide and methods of treating disease using the leflunomide.Type: ApplicationFiled: February 8, 2001Publication date: February 21, 2002Inventors: Ilya Avrutov, Neomi Gershon, Anita Liberman
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Patent number: 6331640Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.Type: GrantFiled: September 29, 1999Date of Patent: December 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6323155Abstract: 4-Benzoylisoxazole derivatives of the formula wherein R is H or an ester; R1 is alkyl, haloalkyl or optionally substituted cycloalkyl; R2 is halogen, optionally halogenated alkyl, alkenyl or alkynyl; alkyl substituted with one or more —OR5; —NO2, —CN, —CO2R5, —S(O)pR6, —O(CH2)mOR5, —COR5, —NR5R6, —N(R8)SOqR7, —CONR9R10 or —OR51; or optionally substituted phenyl; R3 is —S(O)qR7; X is —N(R8)—; n is 0, 1, 2, 3, or 4; R5, R51 and R6 are independently H; optionally halogenated alkyl, alkenyl or alkynyl; optionally substituted phenyl; or cycloalkyl; R7 is optionally halogenated alkyl, alkenyl or alkynyl; cycloalkyl; optionally substituted phenyl; or optionally substituted amino; R8 is H; optionally halogenated alkyl, alkenyl or alkynyl; cycloalkyl; optionally substituted phenyl; or alkoxy; m is 1, 2 or 3; p is 0, 1 or 2; q is 0 or 2; and their use as herbicides are described.Type: GrantFiled: November 1, 1995Date of Patent: November 27, 2001Assignee: Rhone-Poulenc Agriculture LimitedInventors: Tibor Musil, Simon Neil Pettit, Philip Henry Gaunt Smith
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Patent number: 6316479Abstract: The present invention relates to novel isoxazole-4-carboxamides which modulate the activity of protein tyrosine kinases and therefore are expected to be useful in the treatment of abnormal protein tyrosine kinase activity driven disorders including cancer.Type: GrantFiled: May 19, 1998Date of Patent: November 13, 2001Assignee: Sugen, Inc.Inventors: Gerald McMahon, Peng Cho Tang, Laura Kay Shawver, Klaus Peter Hirth
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Patent number: 6306890Abstract: A compound of the formula where: n, and X are as defined in the specification, and the compound possesses selectivity for inhibition of cyclooxygenase-2.Type: GrantFiled: August 30, 1999Date of Patent: October 23, 2001Assignee: Vanderbilt UniversityInventors: Amit S. Kalgutkar, Lawrence J. Marnett
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Patent number: 6303792Abstract: The invention relates to a process for obtaining N-(4-trifluoromethylphenyl)-5-methyl-isoxazole-4-carboxamide in crystalline form, which is essentially free of byproducts. For this purpose, N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide is transferred into an organic solvent or into mixtures of organic solvents and water, the amount of byproduct in the solution is determined by quantitative analysis and an equimolar amount of a base is added. N-(4-Trifluoromethylphenyl)-5-methyl-isoxazole-4-carboxamide is isolated from the resulting solution by crystallization.Type: GrantFiled: February 22, 2000Date of Patent: October 16, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Hans-Hermann Lau, Udo Hedtmann, Holger Faasch, Andreas Gappisch
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Patent number: 6277849Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eacType: GrantFiled: August 24, 1999Date of Patent: August 21, 2001Assignee: Syngenta Crop Protection, Inc.Inventor: Martin Zeller
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Patent number: 6265423Abstract: Novel aromatic polycyclic retinoid-type derivatives of general formula (I), wherein groupings R3 and R4 attached to the double bond between carbons 11 and 12 are cis groupings, and pharmaceutical and cosmetic compositions containing same, are disclosed.Type: GrantFiled: July 15, 1998Date of Patent: July 24, 2001Assignee: Centre Europeen de Bioprospective-CebInventors: Bertrand Leblond, Francis Darro, Abdallah Devine, Véronique Sales-Sallans, Pierre Duhamel, Robert Kiss, Alain-René Schoofs, Pierre Germain, Bernard Pourrias
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Patent number: 6265588Abstract: A compound of the formula where R1 is the radical of the formula II or III is suitable for the production of a pharmaceutical for the treatment of inflammations, carcinomatous diseases, or autoimmune diseases. A compound of the formula IV is suitable for the production of specific antibodies against a compound of the formula I for the discovery of specific-binding proteins from cell extracts, serum, blood, or synovial fluids, for the purification of proteins, for the modification of microtiter plates, or for the preparation of chromatography material, in particular of affinity chromatography material, and for use in diagnostics.Type: GrantFiled: May 30, 2000Date of Patent: July 24, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Stefan MĂ¼llner, Bernd Kirschbaum, Wilfried Schwab
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Patent number: 6265351Abstract: The invention relates to phenylpyrazoles having general formula (I): The compounds having formula (I) have a high herbicidal activity and are used for controlling weeds in the agronomic field.Type: GrantFiled: August 3, 2000Date of Patent: July 24, 2001Assignee: Isagro Ricerca S.r.L.Inventors: Piero La Porta, Franco Bettarini, Giovanni Meazza, Gregorio Valea, Ernesto Signorini, Domenico Portoso
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Patent number: 6251926Abstract: This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.Type: GrantFiled: November 15, 1999Date of Patent: June 26, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Hiroyuki Odaka, Hiroshi Imoto, Hiroyuki Kimura, Junichi Sakamoto
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Patent number: 6251949Abstract: Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof wherein R1 represents an optionally substituted aryl, an optionally substituted alkyl or the like; R2 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R3 represents an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R4 and R5, which may be the same or different, represent each a hydrogen atom, an optionally substituted alkyl, or an optionally substituted alkoxy, or R4 and R5 may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR6 wherein R6 represents a hydrogeType: GrantFiled: December 9, 1999Date of Patent: June 26, 2001Assignee: Shionogi & Co., Ltd.Inventors: Moriyasu Masui, Norihiko Tanimoto, Kuniyoshi Nishida
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Patent number: 6221891Abstract: The invention relates to a crystal modification of the compound of the formula I and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type II diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.Type: GrantFiled: October 28, 1999Date of Patent: April 24, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Faasch, Udo Hedtmann, Uwe Westenfelder, Erich Paulus
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Patent number: 6218418Abstract: Compounds which are 3-amino-pyrazole derivatives represented by formula (I): where R is a C3-C6 cycloalkyl group, which may optionally be substituted by a straight or branched C1-C6 alkyl group, and R1 is a straight or branched C1-C6 alkyl group or a C2-C4 alkenyl, cycloalkyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl and arylalkenyl, which may be optionally substituted; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.Type: GrantFiled: September 22, 2000Date of Patent: April 17, 2001Assignees: Pharmacia & Upjohn S.p.A, Pharmacia & Upjohn Co.Inventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Mario Varasi, Edward L. Fritzen, Martha A. Warpehoski, Betsy S. Pierce, Maria Gabriella Brasca
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Patent number: 6197798Abstract: Compounds of the formula I wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, cycloalkyl or heterocyclyl; R2, R3, R4 and R5 are independently hydrogen, optionally substituted alkyl, halo, amino, substituted amino, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aralkoxycarbonyl, (alkyl, aryl or aralkyl)-thio, (alkyl, aryl or aralkyl)-oxy, acyloxy, (alkyl, aryl or aralkyl)-aminocarbonyloxy; or any two of R2, R3, R4 and R5 at adjacent positions are alkylenedioxy; R6 is hydrogen, optionally substituted alkyl, amino, substituted amino, acylamino, wherein Ra is hydrogen or optionally substituted alkyl, Rb and Rc are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; or Rb and Rc together represent lower alkylene or lower alkylene interrupted by O, S, or N—(H, alkyl or aralkyl); Rd is optionally substituted alkyl, cycloalkyl, aryl or heterocyclyl; and Re is opType: GrantFiled: July 20, 1999Date of Patent: March 6, 2001Assignee: Novartis AGInventors: Cynthia A. Fink, Gary M. Ksander, Paivi J. Kukkola, Eli M. Wallace, Mahavir Prashad
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Patent number: 6187797Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula 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: December 22, 1997Date of Patent: February 13, 2001Assignee: Dupont Pharmaceuticals CompanyInventors: James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
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Patent number: 6177425Abstract: According to the invention there are provided Hexahydro-Pyrrolo[3,4-b]pyrrol-2-one compounds of formula (1), (relative stereochemistry indicated), wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (1) are useful inter alia in the treatment or chronic bronchitis.Type: GrantFiled: May 5, 2000Date of Patent: January 23, 2001Assignee: Glaxo Wellcome Inc.Inventors: Michael Dennis Dowle, Harry Finch, Lee Andrew Harrison, Graham George Adam Inglis, Martin Redpath Johnson, Simon John Fawcett MacDonald, Pritom Shah
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Patent number: 6153752Abstract: Process for the preparation of heterocycles by reacting 2-substituted acetals of malondialdehyde with a reactant selected from hydroxylamines and their salts, hydrazines and their salts, formamid, amidines and their salts, guanidines and their salts, aminoguanidines and their salts, nitroguanidine and their salts, O-alkyl-isoureas and their salts, O-cycloalkyl-isoureas and their salts, O-aralkyl-isoureas and their salts, O-aryl-isoureas and their salts, S-alkyl-isothioureas, S-cycloalkyl-isothioureas, S-aralkyl-isothioureas, S-arylisothioureas, S-alkyl-isothiouronium salts, S-cycloalkyl-isothiouronium salts, S-aralkyl-isothiouronium salts, S-aryl-isothiuronium salts, thiourea and urea.Type: GrantFiled: January 28, 2000Date of Patent: November 28, 2000Assignee: Creanova, Inc.Inventors: Frank Bauer, Chitoor Subramaniam
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Patent number: 6140272Abstract: 4-Benzoylpyrazoles of the formula I where:A is a group of the formula IIIa, IIIb or IV ##STR1## Q is a pyrazole of the formula II, ##STR2## useful as herbicides.Type: GrantFiled: November 2, 1999Date of Patent: October 31, 2000Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Joachim Rheinheimer, Oliver Wagner, Matthias Witschel, Ulf Misslitz, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6121273Abstract: 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: GrantFiled: December 22, 1997Date of Patent: September 19, 2000Assignee: GPI NIL Holdings, IncInventors: Gregory S. Hamilton, Jai-He Li, Wei Huang
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Patent number: 6114328Abstract: This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 25, 1997Date of Patent: September 5, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: John Wityak, Chu-Biao Xue, Thais Motria Sielecki-Dzurdz, Richard Eric Olson, William Frank Degrado, Gary Avonn Cain, Douglas Guy Batt, Donald Pinto, Munir Alwan Hussain, Shaker Ahmed Mousa
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Patent number: 6114538Abstract: Compounds of the formula are useful as intermediates to new herbicidal 4-benzoylisoxazoles.Type: GrantFiled: October 19, 1999Date of Patent: September 5, 2000Assignee: Rhone Poulenc Agriculture LimitedInventors: Angela Jacqueline Bailey, Michael Gingell, David William Hawkins
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Patent number: 6107311Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: April 9, 1998Date of Patent: August 22, 2000Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 6107316Abstract: A method for treating protozoal infections is described. The method employs N-acetonylbenzamide compounds provided in an effective amount to inhibit the growth of protozoans. The compounds are useful in controlling such protozoan parasites as Giardia lamblia, Leishmania major, Entamoeba histolytica, Cryptosporidium parvum, Toxoplasma gondii and microsporidia.Type: GrantFiled: April 29, 1998Date of Patent: August 22, 2000Assignee: Rohm and Haas CompanyInventors: David Hamilton Young, Enrique Luis Michelotti, Thomas David Edlind, Santosh Kumar Katiyar
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Patent number: 6096747Type: GrantFiled: May 28, 1996Date of Patent: August 1, 2000Assignee: Celltech Therapeutics LimitedInventors: Nigel Robert Arnold Beeley, Thomas Andrew Millican
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Patent number: 6096770Abstract: Compounds of the formula: ##STR1## wherein: R.sub.1, R.sub.2 and R.sub.3 are, independently, hydrogen, nitro, cyano, C.sub.1-10 haloalkoxy, amino, C.sub.1-10 alkylamino, sulfo, sulfamoyl, C.sub.1-10 alkylsulfonamido, C.sub.2-10 alkylcarboxamido C.sub.2-10 alkanoyl, C.sub.1-10 alkylsulfonyl, C.sub.1-10 haloalkylsulfonyl, C.sub.1-10 carboxyl, C.sub.1-10 haloalkyl and C.sub.6-12 aryl; with the provisos: (1) that R.sub.1, R.sub.2 and R.sub.3 may not all simultaneously be hydrogen, and (2) when R.sub.1 and R.sub.2 are hydrogen, R.sub.3 may not be meta-CF.sub.3 ;R.sub.4, R.sub.5 and R.sub.6 are, independently, hydrogen, halogen, nitro, cyano, C.sub.1-10 carboalkoxy, C.sub.1-10 haloalkoxy, amino C.sub.1-10 alkylamino, sulfo, sulfamoyl, C.sub.1-10 alkylsulfonamido, C.sub.2-10 alkylcarboxamido C.sub.2-10 alkanoyl, C.sub.1-10 alkylsulfonyl, C.sub.1-10 haloalkylsulfonyl, C.sub.1-10 carboxyl, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl and C.sub.6-12 aryl;R.sub.Type: GrantFiled: August 3, 1998Date of Patent: August 1, 2000Assignee: American Home Products CorporationInventors: Joseph Richard Lennox, Schuyler Adam Antane, John Anthony Butera