Plural Rings Patents (Class 562/435)
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Patent number: 6849742Abstract: The present invention provides a binaphthol compound represented by formula [1]: and a salt thereof. The binaphthol compound of the present invention is useful for manufacturing antiseptic compounds or chiral catalysts. According to the method of the present invention, binaphthol compounds can be prepared in high yield with low cost.Type: GrantFiled: April 18, 2002Date of Patent: February 1, 2005Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
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Patent number: 6806365Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: April 5, 2002Date of Patent: October 19, 2004Assignee: Hoffmann-La Rocher Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Publication number: 20040198977Abstract: Stable, topically applicable cosmetic/dermatological sunscreen compositions, well suited for the UV-photoprotection of human skin/keratinous materials, contain a thus effective amount of at least one novel amine, amide, sulphonamide or carbamate substituted benzalmalonic salt compound.Type: ApplicationFiled: February 27, 2004Publication date: October 7, 2004Applicant: SOCIETE L'OREAL S.A.Inventors: Herve Richard, Bernadette Luppi
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Publication number: 20040122254Abstract: Disclosed are the compounds of formula I 1Type: ApplicationFiled: December 4, 2003Publication date: June 24, 2004Inventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. Van Duzer, Daqiang Xu
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Patent number: 6747170Abstract: A thermosensitive recording material has a support and a thermosensitive coloring layer formed thereon containing a leuco dye and a color developer capable of inducing color formation in the leuco dye upon application of heat thereto, with the color developer including at least one compound (A) having in a molecule thereof at least two aromatic ring moieties with specific structures, selected from the group consisting of an aromatic ring moiety having at least one carboxyl group and electron-attracting functional group, an aromatic ring moiety having at least one carboxyl group and electron-donating functional group, and an aromatic ring moiety having at least one carboxyl group, free of the electron-attracting and electron-donating functional groups. An aromatic carboxylic acid compound serving as the above-mentioned compound (A) and the producing method thereof are also disclosed.Type: GrantFiled: May 23, 2002Date of Patent: June 8, 2004Assignee: Ricoh Company, Ltd.Inventors: Kunio Hayakawa, Mitsunobu Morita
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Patent number: 6743373Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiometers.Type: GrantFiled: April 14, 2000Date of Patent: June 1, 2004Assignee: Solvay (Societe Anonyme)Inventors: Thierry Delplanche, Roland Callens
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Publication number: 20030220382Abstract: The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: R1 and R2 include alkyl and phenylalkyl; R3 is hydrogen or alkyl; and R4 and R5 include alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using compounds of Formula (I).Type: ApplicationFiled: November 4, 2002Publication date: November 27, 2003Inventors: Nancy Sue Barta, Christopher Franklin Bigge
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Patent number: 6590118Abstract: Disclosed are compounds of formula I wherein A, R1, R2, R3, R4 and R5 are described in the specification, pharmaceutical formulations comprising these compounds, the use of these compounds are medicaments, the use of these medicaments in the treatment of and/or prevention of diabetes, especially non-insulin dependent diabetes (NIDDM or Type 2 diabetes), as well as methods for treating diabetes comprising administration of these compounds.Type: GrantFiled: September 28, 2000Date of Patent: July 8, 2003Assignee: Novo Nordisk A/SInventors: Marit Kristiansen, Palle Jakobsen, Jane Marie Lundbeck
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Patent number: 6573402Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.Type: GrantFiled: July 29, 2002Date of Patent: June 3, 2003Assignee: Neurotech Co., Ltd.Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
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Patent number: 6562807Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.Type: GrantFiled: June 22, 2001Date of Patent: May 13, 2003Assignee: Novo Nordisk A/SInventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
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Patent number: 6541521Abstract: Benzene butyric acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, renal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: July 12, 1999Date of Patent: April 1, 2003Assignee: Warner-Lambert CompanyInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Andrew David White
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Patent number: 6521646Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.Type: GrantFiled: October 15, 2001Date of Patent: February 18, 2003Assignee: Merck Patent GmbHInventors: Wolfgang Stähle, Rudolf Gottschlich, Simon Goodman
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Patent number: 6506798Abstract: The invention provides compounds of formula (II), wherein Ar, R3, R4, R5, R6, R7, R8 and W have the meanings given in the description. They are selective MEK inhibitors.Type: GrantFiled: July 11, 2001Date of Patent: January 14, 2003Assignee: Warner-Lambert CompanyInventors: Stephen Barrett, Haile Tecle
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Patent number: 6504052Abstract: Compounds of the formula (I) in which R1 is C1-10 allyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous systemType: GrantFiled: November 16, 2001Date of Patent: January 7, 2003Assignee: Eli Lilly and CompanyInventors: Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Publication number: 20020151594Abstract: Applicants' invention includes a method to treat a patient having congestive heart failure by administering a therapeutically effective amount of 3,5-diidothyropropionic acid. Applicants' invention further includes a method to lower cholesterol blood levels of a patient by administering a therapeutically effective amount of 3,5-diidothyropropionic acid. Applicants' invention further includes a synthetic method to prepare 3,5-diidothyropropionic acid.Type: ApplicationFiled: January 31, 2001Publication date: October 17, 2002Applicant: Arizona Board of Regents on Behalf of The University of ArizonaInventors: Eugene Morkin, Gregory D. Pennock, Joseph J. Bahl, Steven Goldman
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Publication number: 20020132853Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.Type: ApplicationFiled: July 20, 2001Publication date: September 19, 2002Inventors: Rajagopal Bakthavatchalam, Alan Hutchison, Robert W. DeSimone, Kevin J. Hodgetts, James E. Krause, Geoffrey G. White
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Patent number: 6452044Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neutopathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.Type: GrantFiled: May 30, 2001Date of Patent: September 17, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Takashi Tsukamoto, Barbara S. Slusher, Eric Wang
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Patent number: 6423780Abstract: In accordance with the present invention, there are provided novel heterobifunctional monomers and uses for the same. Invention compounds have many of the properties required by the microelectronics industry, such as, for example, hydrophobicity, high Tg values, low dielectric constant, ionic purity, low coefficient of thermal expansion (CTE), and the like. These properties result in a thermoset that is particularly well suited to high performance applications where typical operating temperatures are often significantly higher than those at which prior art materials were suitable. Invention compounds are particularly ideal for use in the manufacture of electronic components, such as, for example, printed circuit boards, and the like.Type: GrantFiled: February 7, 2001Date of Patent: July 23, 2002Assignee: LoctiteInventors: Stephen M. Dershem, Kevin J. Forrestal
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Patent number: 6376546Abstract: Compounds represented by general formula I or salts thereof, wherein n is an integer of 2 or 3; R represents a straight-chain or branched saturated alkyl group having 4 or 4 carbon atoms, a cyclopentyl group, a cyclohexyl group or the like, Y represents a hydroxyl or amino group, A represents a hydrogen atom, a hydroxyl, methoxy, nitro group or the like, Q represents a hydrogen atom or a hydroxyl or methoxy group. They can be formulated to give pharmaceutical compositions that are effective as prophylactic or therapeutic agents for allergic diseases associated with IgE production inhibitors or IgE antibodies.Type: GrantFiled: June 8, 2000Date of Patent: April 23, 2002Assignee: Asahi Kasei Kabushiki KaishaInventors: Motoshi Shoda, Hiromichi Itoh
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Patent number: 6342630Abstract: A process for the purification of a compound of general formula I: wherein: R1 is hydrogen or C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl (any of which may optionally be substituted with one or more substituents selected from halogen and OH) or COOR4, COR6, CONR4R5 or CONHSO2R4; R4 and R5 are each independently hydrogen or C1-C4 alkyl optionally substituted with one or more halogen atoms; R6 is a halogen atom or a group R4; R2 is hydrogen or halo; R3 is C1-C4 alkyl, C2-C4 alkenyl or C2-C4 alkynyl, any of which may optionally be substituted with one or more halogen atoms, or halo; or, where appropriate, a salt thereof; from a mixture containing the compound of general formula I together with one or more isomers or di-nitrated analogues thereof; the process comprising dissolving the mixture in a suitable crystallisation solvent and recrystallising the product from the resulting crystallisation solution; characterised in that the crystallisation solution contains not more than 25% loadinType: GrantFiled: September 11, 1996Date of Patent: January 29, 2002Assignee: Zeneca LimitedInventors: Stephen Martin Brown, Brian David Gott, Thomas Gray, Seyed Mehdi Tavana
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Publication number: 20020004608Abstract: N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: 1Type: ApplicationFiled: May 16, 2001Publication date: January 10, 2002Inventors: Leo Alig, Katrin G. Zbinden, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Hans Peter Wessl
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Patent number: 6310078Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 3, 2000Date of Patent: October 30, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 6306840Abstract: 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: January 23, 1995Date of Patent: October 23, 2001Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao
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Publication number: 20010025084Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12.Type: ApplicationFiled: January 22, 2001Publication date: September 27, 2001Inventors: Vinh D. Tran, Vu Van Ma, Ruiyan Liu
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Patent number: 6215007Abstract: Novel polyketides and novel methods of efficiently producing both new and known polyketides, using recombinant technology, are disclosed. In particular, a novel host-vector system is described which is used to produce polyketide synthases which in turn catalyze the production of a variety of polyketides.Type: GrantFiled: March 5, 1999Date of Patent: April 10, 2001Assignees: The Leland Stanford Junior Univ., The John Innes InstituteInventors: Chaitan Khosla, David A. Hopwood, Suzanne Ebert-Khosla, Robert McDaniel, Hong Fu
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Patent number: 6177463Abstract: The invention relates to new oxime derivatives, to a plurality of processes for their preparation, and to their use as pesticides.Type: GrantFiled: September 3, 1996Date of Patent: January 23, 2001Assignee: Bayer AktiengesellschaftInventors: Peter Gerdes, Herbert Gayer, Bernd-Wieland Kr{umlaut over (u)}ger, Bernd Gallenkamp, Heinz-Wilhelm Dehne, Stefan Dutzmann, Gerd H{umlaut over (a)}nssler, Klaus Stenzel
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Patent number: 6172058Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.Type: GrantFiled: April 3, 1998Date of Patent: January 9, 2001Assignee: Lilly, SAInventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
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Patent number: 6172112Abstract: The present invention provides new retinoid compounds and uses of the compounds in humans and animals for chemoprevention of skin and/or breast cancer and for therapy of leukemia.Type: GrantFiled: April 6, 1999Date of Patent: January 9, 2001Assignee: UAB Research FoundationInventors: Wayne J. Brouillette, Donald D. Muccio
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Patent number: 6127392Abstract: Compounds of the formula: wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4,R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 arylsufinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 arylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.Type: GrantFiled: August 3, 1998Date of Patent: October 3, 2000Assignee: American Home Products CorporationInventors: Joseph Richard Lennox, Schuyler Adam Antane, John Anthony Butera
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Patent number: 6072080Abstract: A process for the purification of a compound of general formula I: ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, any of which may optionally be substituted with one or more substituents selected from halogen and hydroxy; or COOR.sup.4, COR.sup.6, CONR.sup.4 R.sup.5 or CONHSO.sub.2 R.sup.4 ;R.sup.4 and R.sup.5 independently represent hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted with one or more halogen atoms;R.sup.6 is a halogen atom or a group R.sup.4 ;R.sup.2 is hydrogen or halo; andR.sup.3 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.Type: GrantFiled: March 12, 1998Date of Patent: June 6, 2000Assignee: Zeneca LimitedInventors: Louie Akos Nady, Seyed Mehdi Tavana, Thomas Gray, Stephen Martin Brown, Brian David Gott
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Patent number: 6028219Abstract: A process for the preparation of a compound of general formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, any of which may optionally be substituted with one or more substituents selected from halogen and OH; or COOR.sup.4, COR.sup.6, CONR.sup.4 R.sup.5 or CONHSO.sub.2 R.sup.4 ;R.sup.4 and R.sup.5 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted with one or more halogen atoms;R.sup.6 is a halogen atom or a group R.sup.4 ;R.sup.2 is hydrogen or halo;R.sup.3 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl, any of which may optionally be substituted with one or more halogen atoms; or halo;the process comprising reacting a compound of general formula II: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.Type: GrantFiled: July 28, 1997Date of Patent: February 22, 2000Assignee: Zeneca LimitedInventors: John Heathcote Atherton, Stephen Martin Brown, James Peter Muxworthy, Martin Lennon
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Patent number: 5955505Abstract: A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.Type: GrantFiled: August 20, 1997Date of Patent: September 21, 1999Assignee: Nippon Suisan Kaisha, Ltd.Inventors: Jiro Takeo, Shinya Yamashita, Keiji Wada, Yoshiyuki Chiba
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Patent number: 5952531Abstract: A process for the nitration of an aromatic or heteroaromatic compound with a nitrating agent comprising nitric acid or a mixture of nitric and sulphuric acids, characterised in that nitration is performed in a solvent comprising at least 50% v/v of a C.sub.1 -C.sub.6 alkyl ester of a C.sub.1 -C.sub.4 carboxylic acid. The process is of particular use for the nitration of diphenyl ethers to give compounds which are useful as herbicides or as intermediates in the synthesis of herbicides.Type: GrantFiled: October 30, 1997Date of Patent: September 14, 1999Assignee: Zeneca LimitedInventors: Ian Jeffrey Grassham Priestley, James Peter Muxworthy, John Heathcote Atherton, Martin Lennon, Stephen Martin Brown
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Patent number: 5910604Abstract: A process for the purification of a compound of general formula I: ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, any of which may optionally be substituted with one or more substituents selected from halogen and hydroxy; or COOR.sup.4, COR.sup.6, CONR.sup.4 R.sup.5 or CONHSO.sub.2 R.sup.4 ;R.sup.4 and R.sup.5 independently represent hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted with one or more halogen atoms;R.sup.6 is a halogen atom or a group R.sup.4 ;R.sup.2 is hydrogen or halo; andR.sup.3 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.Type: GrantFiled: March 13, 1997Date of Patent: June 8, 1999Assignee: Zeneca LimitedInventors: Stephen Martin Brown, Brian David Gott, Thomas Gray, Seyed Mehdi Tavana
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Patent number: 5892106Abstract: The present invention relates to novel intermediates of the formula ##STR1## wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt; or solvate thereof; and to the use thereof in a process for the preparation of certain 3-fluoro oxindole derivatives.Type: GrantFiled: June 18, 1998Date of Patent: April 6, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Yadagiri R. Pendri, Eduardo J. Martinez, John K. Thottathil, Piyasena Hewawasam
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Patent number: 5852199Abstract: The present invention provides a novel carbamazepine hydrazide compound suitable for covalent attachment to a polymer particle reagent, having the general formula ##STR1## The present invention provides a novel carbamazepine acid compound suitable for attachment to proteins for the production of carbamazepine immunogens. The carbamazepine antigen of the present invention has the following general structure: ##STR2## where X is C.dbd.O, CH.sub.2 or SO.sub.2 ; Y is C.dbd.O, CH.sub.2, SO.sub.2 ; R is an alkyl and P is a protein or a hapten.Type: GrantFiled: July 25, 1997Date of Patent: December 22, 1998Assignee: Dade Behring Inc.Inventor: Chengrong Wang
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Patent number: 5849732Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.Type: GrantFiled: February 14, 1997Date of Patent: December 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5719306Abstract: The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.Type: GrantFiled: June 6, 1995Date of Patent: February 17, 1998Assignee: G.D. Searle & Co.Inventors: Nizal Samuel Chandrakumar, Barbara Baosheng Chen, Michael Clare, Bipinchandra Nanubhai Desai, Stevan Wakefield Djuric, Stephen Hermann Docter, Alan Frank Gasiecki, Richard Arthur Haack, Chi-Dean Liang, Julie Marion Miyashiro, Thomas Dale Penning, Mark Andrew Russell, Stella Siu-tzyy Yu
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Patent number: 5717109Abstract: The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.Type: GrantFiled: July 10, 1995Date of Patent: February 10, 1998Assignee: Eli Lilly and CompanyInventors: M. Brian Arnold, Thomas J. Bleisch, David R. Helton, Mary Jeanne Kallman, Paul L. Ornstein, Darryle D. Schoepp, Joseph P. Tizzano
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Patent number: 5703095Abstract: N-arylmethylene ethylenediaminetriacetate, N-arylmethylene iminodiacetate or N,N'-diarylmethylene ethylenediaminediacetate type compounds and their use in combatting oxidative stress, and pharmaceutical and cosmetic compositions comprising said compounds. The invention also concerns a process for the preparation of said compounds.Type: GrantFiled: June 27, 1995Date of Patent: December 30, 1997Assignee: L'OrealInventors: Jean Baptiste Galey, Jacqueline Dumats
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Patent number: 5688997Abstract: Combinatorial libraries are disclosed which are represented by Formula I:(T'-L).sub.q -S-C(O)-L'-II' Iwherein:S is a solid support; T'-L- is an identifier residue; and -L'-II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: ##STR1## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.Type: GrantFiled: June 7, 1995Date of Patent: November 18, 1997Assignee: Pharmacopeia, Inc.Inventors: John J. Baldwin, John C. Reader, Lawrence W. Dillard, Ge Li, Jonathan J. Burbaum, Wenguang Zeng
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Patent number: 5672708Abstract: N-arylaminoacrylic acid derivatives are obtained in good yields and in high purities when benzoylacetic acid derivatives are reacted with N-arylimino ethers. The products thus prepared are used, in particular, for the preparation of 4-quinolone-3-carboxylic acid derivatives, which have an outstanding bactericidal action.Type: GrantFiled: August 31, 1995Date of Patent: September 30, 1997Assignee: Bayer AktiengesellschaftInventors: Gunter Rauchschwalbe, Bernhard Beitzke, Wolfgang Eymann, Helmut Fiege
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Patent number: 5629436Abstract: N-arylmethylene ethylenediaminetriacetate, N-arylmethylene iminodiacetate or N,N'-diarylmethylene ethylenediaminediacetate type compounds and their use in combatting oxidative stress, and pharmaceutical and cosmetic compositions comprising said compounds. The invention also concerns a process for the preparation of said compounds.Type: GrantFiled: June 6, 1995Date of Patent: May 13, 1997Assignee: L'OrealInventors: Jean-Baptiste Galey, Jacqueline Dumats
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Patent number: 5623088Abstract: A method of producing 4-ADPA is disclosed wherein aniline or substituted aniline derivatives and nitrobenzene are reacted under suitable conditions to produce 4-nitrodiphenylamine or substituted derivatives thereof and/or 4-nitrosodiphenylamine or substituted derivatives thereof and/or their salts, either or both of which are subsequently reduced to produce 4-ADPA or substituted derivatives thereof. The 4-ADPA or substituted derivatives thereof can be reductively alkylated to produce p-phenylenediamine products or substituted derivatives thereof which are useful as antiozonants.Type: GrantFiled: May 10, 1995Date of Patent: April 22, 1997Assignee: Flexsys America L. P.Inventors: Michael K. Stern, James K. Bashkin
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Patent number: 5612483Abstract: Nitro-substituted aromatics can be directly aminated with amines in the presence of simple bases and oxygen.Type: GrantFiled: September 6, 1995Date of Patent: March 18, 1997Assignee: Bayer AktiengesellschaftInventor: Manfred Jautelat
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Patent number: 5578639Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.Type: GrantFiled: May 30, 1995Date of Patent: November 26, 1996Assignee: Warner-Lambert CompanyInventor: Reynold Homan
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Patent number: 5550160Abstract: A physiologically acceptable, radiolabelled compound of general formula ##STR1## where k is an integer from 2 to 5l is an integer from 1 to 5X and Y are independently selected from phenyl or naphthyl radical each of which can be substituted by one or more amino, mono- or di- substituted amino, halogen, hydroxy, mercapto, nitro, cyano, thiocyano, alkyl, alkoxy, halogenoalkyl, acyl, acylamino, acyloxy, carboxyl, alkoxycarbonyl, carbamoyl, pyridoylamino, N-carboxyalkyl-carbamoyl, sulpho, sulphamoyl, mono- or dialkylated or phenylated sulphamoyl which can also carry one or more substituents R', alkylsulphonyl, alkoxysulphonyl, --(CH.sub.2).sub.p NHCOR", --COR" or by an optionally hydroxy-containing phenylsulphonyl or phenoxysulphonyl; or X and Y are independently selected from pyridine or quinoline radical each of which can be substituted by amine, halogen, hydroxy, alkyl, or carbamoyl; where R' is as defined for X and Y; R" is alkyl-L where L is halogen or other leaving group; 2,5-diketo-pyrrolinyl, --Het--CH.Type: GrantFiled: July 29, 1993Date of Patent: August 27, 1996Assignee: Australian Nuclear Science & Technology OrganizationInventors: Suzanne V. Smith, Richard M. Lambrecht, Peter F. Schmidt, Fook-Thean Lee
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Patent number: 5536868Abstract: Compounds of Formula 1 bind to the opioid receptors: ##STR1## wherein R.sub.1 is a group of the formula ##STR2## where W is --(CH.sub.2).sub.a -- (where a is 0, 1, or 2), --O--, --NH--, --S--, --SO--, or --SO.sub.2 --, and Ar is phenyl, phenyl-alkyl, phenyl substituted with 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups, and n is 0, 1, 2, 3, or 4;R.sub.2 and R.sub.3 are each independently H, lower alkyl, or ##STR3## where X is H, OH, lower alkyl, or lower alkoxy, and p is 0, 1, 2, or 3; R.sub.4 is ##STR4## where m is 0, 1, 2, or 3, and R is 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups;R.sub.5 is cycloalkyl, bicycloalkyl, or tricycloalkyl; andR.sub.6, R.sub.7, R.sub.8, and R.sub.9 are each independently H or lower alkyl.Type: GrantFiled: February 21, 1995Date of Patent: July 16, 1996Assignee: Chiron CorporationInventors: Simon Ng, Robert L. Warne, Ronald N. Zuckermann, Eric J. Martin, Reyna J. Simon