Plural Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 544/148)
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Patent number: 7057040Abstract: The present invention relates to novel compounds possessing specific hot, pungent and spicy taste when subjected to direct pungency evaluation, which may be useful as food additives and anti-oxidants, however the said compounds do not add to any nutritional value but the synthesised compounds can possess useful pharmacological properties which is expected to find application in new test models for the development of anti-inflammatory drugs, bioavailability enhancers and for the study of hepatic drug metabolising mechanism; also relates to a process for preparing the said compounds.Type: GrantFiled: February 7, 2002Date of Patent: June 6, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Subhash Chandra Taneja, Surrinder Koul, Jawahir Lal Koul, Beenu Moza, Sukhdev Swami Handa
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Patent number: 6916802Abstract: 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: GrantFiled: May 5, 2004Date of Patent: July 12, 2005Assignees: Genzyme Corporation, The Regents of the University of MichiganInventors: James A. Shayman, David J. Harris, Craig Siegel, Carol A. Nelson, Diane P. Copeland
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Patent number: 6887869Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.Type: GrantFiled: January 11, 2002Date of Patent: May 3, 2005Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Olivier Lavergne, Christophe Lanco, Grégoire Prevost, Beng Poon Teng
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Patent number: 6878728Abstract: The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.Type: GrantFiled: June 9, 2000Date of Patent: April 12, 2005Assignee: Vertex Pharmaceutical IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger
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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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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: 20040087585Abstract: Nobel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 28, 2003Publication date: May 6, 2004Inventors: Jia-Ning Xiang, Siegfried B Christensen, Jinhwa Lee, Daniel J Mercer
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Publication number: 20030232986Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”) , apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.Type: ApplicationFiled: December 6, 2002Publication date: December 18, 2003Applicant: Vertex Pharmaceuticals IncorporatedInventors: Marion M. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
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Patent number: 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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Patent number: 6645960Abstract: A compound of general formula (I) and physiologically acceptable salts wherein R represents phthalidyl, (2-oxo-5-methyl-1,3-diox-olen-4-yl)methyl or the group CHR4 OCO(O)pR5 wherein R4 is hydrogen or C1-4 alcyl, p is zero or I, R5 is C1-6 alkly, C5-8 cycloalyl (optionally substituted by C1-3 alkyl or carboxyl), C1-4 alkyl substituted by C1-3 alkoxy or carboxy), C1-4 alkyl substituted by one or more groups selected from amino, (C1-4 alkylamino di(C1-4 alkyl)amino or carboxyl, phenyl (optionally substituted by carboxyl or aminoalkyl, C1-4 alkylaminoalkyl or di(C1-4 alkyl)aminoalcyl, or R5 is a 5-8 membered heterocyclic group containing 1 or 2 heteroatoms selected from oxygen or nitrogen, processes for their preparation, pharmaceutical compositions containing them and their use in medicine.Type: GrantFiled: September 24, 2002Date of Patent: November 11, 2003Assignee: Glaxo Wellcome S.A.Inventors: Jose Maria Fiandor, Sophie Huss
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Patent number: 6632816Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may be, for example, iso-butyl, wherein X and Y, same or different, may be, for example, NH2 and F, and wherein R2 and R3 are as defined herein.Type: GrantFiled: December 23, 2002Date of Patent: October 14, 2003Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Jean-François Lavallée, Nicolas LeBerre, Valérie Perron
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Publication number: 20030161860Abstract: The present invention relates to novel compounds possessing specific hot, pungent and spicy taste when subjected to direct pungency evaluation, which may be useful as food additives and anti-oxidants, however the said compounds do not add to any nutritional value but the synthesised compounds can possess useful pharmacological properties which is expected to find application in new test models for the development of anti-inflammatory drugs, bioavailability enhancers and for the study of hepatic drug metabolising mechanism; also relates to a process for preparing the said compounds.Type: ApplicationFiled: February 7, 2002Publication date: August 28, 2003Inventors: Subhash Chandra Taneja, Surrinder Koul, Jawahir Lal Koul, Beenu Moza, Sukhdev Swami Handa
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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: 6486332Abstract: Compounds of formula A(B)x, (I) wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: February 6, 2001Date of Patent: November 26, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 6451791Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: September 17, 2002Assignee: Monsanto CompanyInventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
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Publication number: 20020086863Abstract: The invention relates to new arylglycinamide derivatives of general formula I 1Type: ApplicationFiled: October 5, 2001Publication date: July 4, 2002Applicant: Boehringer Ingelheim KG.Inventors: Gerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 6376538Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: September 19, 1997Date of Patent: April 23, 2002Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao, Julio Hernan Cuervo, Juswinder Singh
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Patent number: 6358885Abstract: This invention relates to certain phenylheterocyclic compounds, herbicidal compositions thereof and a method for their use as general and selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: April 15, 1999Date of Patent: March 19, 2002Assignees: Mississippi State University, Research Technology Corporation Mississippi StateInventors: Thomas P. Selby, Thomas M. Stevenson
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Patent number: 6340704Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.Type: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
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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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Publication number: 20010041796Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1).Type: ApplicationFiled: January 16, 2001Publication date: November 15, 2001Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyma
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Patent number: 6316505Abstract: Block copolymers containing a fluorinated hydrocarbon unit, a hydrocarbon unit, and a poly(oxyethylene) unit are useful in fluid formulations of pharmaceutical agents. A typical embodiment is: C11H23—CONHC2H4NHCO—C8F16—CONHC2H4NHCOO—(C2H4O)34—H.Type: GrantFiled: August 5, 1999Date of Patent: November 13, 2001Assignee: Supratek Pharma, Inc.Inventors: Alexander V. Kabanov, Serguei V. Vinogradov
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Patent number: 6271401Abstract: Compounds of formula A(B)x, (I), wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: July 9, 1996Date of Patent: August 7, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 6218135Abstract: The present invention has its objects to provide a compound not only which is easy to handle, thermally stable, and high in emission efficiency, but also which can show high emission efficiency without coexisting enhancer in the system even in a protic solvent. The present invention is related to a 1,2-dioxetane derivative of general formula (I). [wherein R1, R2, R3, R4 and R5 each independently represents hydrogen, alkyl or aryl; a pair of R2 and R3 and a pair of R4 and R5 may respectively be joined to each other to form a cycloalkyl group.Type: GrantFiled: March 15, 1999Date of Patent: April 17, 2001Inventors: Masakatsu Matsumoto, Nobuko Watanabe
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Patent number: 6211363Abstract: 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: February 25, 2000Date of Patent: April 3, 2001Assignee: Daiichi Pharamaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Patent number: 6149841Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: December 17, 1999Date of Patent: November 21, 2000Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar
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Patent number: 6150539Abstract: Compounds useful in immunosuppressive and anti-inflammatory treatment are described. The compounds are hydrolyzable triptolide analogs with improved water solubility and generally lower toxicity than the parent compound.Type: GrantFiled: September 2, 1999Date of Patent: November 21, 2000Assignee: Pharmagenesis, Inc.Inventor: John H. Musser
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Patent number: 6146554Abstract: What is described here are photochromic naphthopyrane dyes with different substituents whose properties can be set by controlled selection of the substituents. In this manner it is possible to take an influence on the migration characteristics, the absorption characteristics and the brightening rate and kinetics. The inventive compounds display good darkening and brightening properties at a very good service life.The invention excels itself by the fact that a method is made available which is substantially improved over prior art, in addition to the surprising influence on specific properties of the inventive compounds. The described compounds are suitable for application in synthetic materials of any kind.A photochromic object is also the subject matter of the invention, which comprises one or several photochromic naphthopyrane dyes as well as at least one polymer material, with the photochromic object being producible by mass-dyeing or superficial dyeing.Type: GrantFiled: May 21, 1999Date of Patent: November 14, 2000Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Claudia Mann, Udo Weigand
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Patent number: 6133263Abstract: Novel nonpeptide endothelin antagonists with ether-linked groups are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemnic bowel disease, Chrohn's disease, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, acute respiratory distress syndrome, chronic obstructive pulmonary diseases, male penile erectile dysfunction, cancer, especially malignant hemangicendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nepbrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arhythmias, benign prostatic hyperplasia, and elevated levType: GrantFiled: August 3, 1998Date of Patent: October 17, 2000Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
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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: 6117870Abstract: A cyclic amide derivative of formula (I): ##STR1## wherein R.sup.1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl group, a substituted sulfonamide group or a substituted amide group; the ring A represents a saturated cyclic alkyl group with 5 to 7 carbon atoms or a hetero-atom-containing saturated heterocyclic group with 3 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a hydrogen atom, a group represented by the general formula R.sup.4 O-- or a group represented by the general formula R.sup.5 (R.sup.6)N-- wherein R.sup.Type: GrantFiled: November 10, 1999Date of Patent: September 12, 2000Assignee: Fujirebio Kabushiki KaishaInventors: Akihiko Hosoda, Nobuo Kobayashi, Naoko Tanabe, Tsuneo Koji, Masahiro Shibata, Akihiro Sekine, Masaharu Dozen
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Patent number: 6087359Abstract: A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: September 10, 1999Date of Patent: July 11, 2000Inventors: Daniel P. Getman, Daniel P. Becker, Thomas E. Barta, Clara I. Villamil, Susan L. Hockerman, Louis J. Bedell, Hui Li, John N. Freskos, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo
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Patent number: 6075140Abstract: The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). ##STR1## [In the formula (I), R.sup.1 : a phenyl group, R.sup.2 : an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R.sup.3 : a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group --O--R.sup.31, an acyloxy group or a group --O--CO--R.sup.31, (in which R.sup.31 : an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R.sup.4 and R.sup.5 : a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z.sup.1 : a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z.sup.2 : a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z.sup.3 : an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: February 5, 1998Date of Patent: June 13, 2000Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Patent number: 6043241Abstract: Compounds of the Formula I ##STR1## are nonpeptide antagonists of endothelin which are useful in treating a variety of diseasses such as elevated levels of endothelin, acute respiratory distress syndrome (ARDS), atherosclerosis, restenosis, Raynaud's phenomenon etc. The compounds are prepared by reacting an alpha-hydroxy butenolide with one or more equivalents of a suitable base, and exposing the solution to UV light.Type: GrantFiled: July 31, 1998Date of Patent: March 28, 2000Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, Timothy Robert Hurley, Michael James Lovdahl, William Chester Patt, Joseph Thomas Repine
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Patent number: 6022495Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, nenzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: July 10, 1998Date of Patent: February 8, 2000Assignee: Transitions Optical, Inc.Inventor: Anil Kumar
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Patent number: 6017915Abstract: The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 15, 1998Date of Patent: January 25, 2000Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Uffe Bang Olsen, Peter Madsen, Zdenek Polivka, Otylie Konigova, Frantisek Miksik, Martina Kovandova, Alexandra Silhankova, Karel Sindelar
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Patent number: 5972939Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: October 26, 1998Date of Patent: October 26, 1999Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min Xiang, John B. Moore, Jr., Mary Pat Beavers
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 5962682Abstract: 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, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.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.Type: GrantFiled: August 18, 1997Date of Patent: October 5, 1999Assignee: 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: 5955520Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and having certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12 or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans and spiro(indoline)type compounds, are also described.Type: GrantFiled: June 17, 1996Date of Patent: September 21, 1999Assignee: PPG Industries, Inc.Inventors: Harry G. Heller, Julian R. Levell
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Patent number: 5922706Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: November 13, 1997Date of Patent: July 13, 1999Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Tamara Ladduwahetty
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5847168Abstract: A photochromic article that includes a host material and a photochromic amount of a naphthopyran compound, the naphthopyran compound represented by the formula: ##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 ', R.sub.10 ', 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 each selected from the following group: a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.Type: GrantFiled: December 1, 1997Date of Patent: December 8, 1998Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 5753660Abstract: Selected sulfonylalkanoylamino 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: November 13, 1996Date of Patent: May 19, 1998Assignee: G. D. Searle & Co.Inventors: James A. Sikorski, Daniel P. Getman, Gary A. DeCrescenzo, Balekudru Devadas, John N. Freskos, Hwang-Fun Lu, Joseph J. McDonald
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Patent number: 5719147Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: September 8, 1995Date of Patent: February 17, 1998Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Patent number: 5705500Abstract: Selected sulfonylalkanoylamino hydroxyethylamine 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: June 7, 1995Date of Patent: January 6, 1998Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
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Patent number: 5686484Abstract: Compounds of formula (I): ##STR1## and of formula (I).sub.w : ##STR2## in which: A represents group having one of the following formulae: ##STR3## wherein R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen atoms, halogen atoms, alkyl groups having from 1 to 4 carbon atoms, and alkoxy groups having from 1 to 4 carbon atoms;R.sup.1, R.sub.w.sup.1 and R.sub.w.sup.2 are, for example, hydrogen, halogen, cyano, nitro, optically substituted alkyl, alkoxy or alkoxyalkoxy;X or X.sub.w is hydroxy, alkanoyloxy, substituted alkanoyloxy or hydroxyimino; R.sup.3.sub.w and R.sup.4.sub.w are each hydrogen, alkyl or alkoxy; R.sup.5 and R.sup.5.sub.w are methyl, ethyl, isopropyl or sec-butyl; and salts thereof have valuable anthelmintic, acaricidal and insecticidal activities.Type: GrantFiled: March 1, 1995Date of Patent: November 11, 1997Assignees: Sankyo Co., Ltd., Ciba-Geigy CorporationInventors: Yasuhiro Morisawa, Akio Saito, Satoru Naito, Toshimitsu Toyama, Susumu Kaneko, Louis-Pierre Molleyres, Jean-Claude Gehret
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Patent number: 5656656Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.Type: GrantFiled: May 23, 1995Date of Patent: August 12, 1997Assignee: Dompe Farmaceutici S.p.A.Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
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Patent number: 5654122Abstract: Pyridone dyes useful for thermal transfer have the formula ##STR1## where R.sup.1 is hydrogen or C.sub.1 -C.sub.4 - alkyl,R.sup.2 and R.sup.3 are identical or different and each is, independently of the other, hydrogen, substituted or unsubstituted C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted pyridyl, substituted or unsubstituted C.sub.1 -C.sub.12 -alkanoyl, C.sub.1 -C.sub.12 -alkoxycarbonyl, substituted or unsubstituted C.sub.1 -C.sub.12 -alkylsulfonyl, C.sub.5 -C.sub.7 -cycloalkylsulfonyl, substituted or unsubstituted phenylsulfonyl, substituted or unsubstituted pyridylsulfonyl, substituted or unsubstituted benzoyl, pyridylcarbonyl or thienylcarbonyl or are together with the nitrogen atom to which they are bonded unsubstituted or C.sub.1 -C.sub.4 - alkyl-substituted succinimido, unsubstituted or C.sub.1 -C.sub.Type: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Ernst Schefczik, Ruediger Sens, Matthias Wiesenfeldt
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Patent number: 5646143Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.Type: GrantFiled: July 25, 1996Date of Patent: July 8, 1997Assignee: Ciba-Geigy CorporationInventors: Richard Goschke, Jurgen Klaus Maibaum, Walter Schilling, Stefan Stutz, Pascal Rigollier, Yasuchika Yamaguchi, Nissim Claude Cohen, Peter Herold