Nitrogen Attached Directly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/161)
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Publication number: 20030013747Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: 1Type: ApplicationFiled: August 6, 2002Publication date: January 16, 2003Applicant: WyethInventors: Robert J. Steffan, Amedeo A. Failli
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Publication number: 20030008906Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds represented by general formula (I) that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.Type: ApplicationFiled: August 2, 2002Publication date: January 9, 2003Applicant: Neurosearch A/SInventors: Bo Skaaning Jensen, Lene Teuber, Dorte Strobaek, Palle Christophersen, Soren Peter Olesen
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Patent number: 6495693Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 30, 1999Date of Patent: December 17, 2002Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Warren J. Porter, Eugene D. Thorsett, Jing Wu
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Publication number: 20020123484Abstract: Novel benzothiazoles and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.Type: ApplicationFiled: October 26, 2001Publication date: September 5, 2002Inventors: Jagabndhu Das, Joel C. Barrish, John Wityak
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Patent number: 6441012Abstract: Compound of formula (I) wherein: A is a bicyclic heteroaryl, optionally substituted with one or more substituents; B is linker group connecting group A to group D and comprising a 3 or 4 atom linker where each atom is independently selected from carbon, oxygen, nitrogen and sulphur and is optionally subsituted with one or more C1-6 alkyl groups or two of such adjacent alkyl substituents may form a ring; C is aryl or a mono or bicyclic heteroaryl, each of which can be optionally substituted; D is an aryl or heteroaryl, both of which are optionally substituted R1 is hydrogen, C1-5 alkyl, C1-3 alkanoyl or C1-3 alkoxycarbonyl; R2 to R5 are each independently selected from hydrogen, C1-6 alkyl, aryl and heteroaryl containing up to 2 heteroatoms chosen from oxygen, sulphur and nitrogen, the aryl and heteroaryl optionally substituted with C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-4 alkoxy, C1-4 alkanoyl, C1-6 alkylamino, C1-4alkylC1-6alkyoxyl, C1-6alkylaminoC1-6alkyl, nitro, cyano, halogeno, triflType: GrantFiled: January 23, 2001Date of Patent: August 27, 2002Assignee: AstraZeneca ABInventors: David R Brittain, Craig Johnstone, Michael S Large, Gareth M Davies
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Patent number: 6441184Abstract: Glucokinase activating amides are useful for increasing insulin secretion in the treatment of type II diabetes.Type: GrantFiled: December 4, 2001Date of Patent: August 27, 2002Assignee: Hoffmann-LA Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Publication number: 20020111372Abstract: Glucokinase activating amides are useful for increasing insulin secretion in the treatment of type II diabetes.Type: ApplicationFiled: December 4, 2001Publication date: August 15, 2002Inventors: Wendy L. Corbett, Joseph S. Grimsby, Nancy-Ellen Haynes, Robert F. Kester, Paige E. Mahaney, Ramakanth Sarabu
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Patent number: 6432962Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.Type: GrantFiled: May 21, 2001Date of Patent: August 13, 2002Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Anne Marie Horneman
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Publication number: 20020103241Abstract: Glucokinase activating amides are useful for increasing insulin secretion in the treatment of type II diabetes.Type: ApplicationFiled: December 4, 2001Publication date: August 1, 2002Inventors: Wendy L. Corbett, Josehp S. Grimsby, Nancy-ellen Haynes, Robert F. Kester, Paige E. Mahaney, Ramakanth Sarabu
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Publication number: 20020103240Abstract: A process for resolving or enriching (R,S) 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole (pramipexole) into optical isomers uses a monovalent salt thereof, e.g. pramipexole monohydrochloride, as a substrate. The monovalent salt is treated with an optically active acid, e.g. with L(+)-tartaric acid, to yield a diastereomeric mixed salt. The mixed salt is subjected to fractional crystallization to yield an optically enriched mixed salt. The mixed salt can be treated with base to liberate the desired isomer of pramipexole.Type: ApplicationFiled: September 18, 2001Publication date: August 1, 2002Inventor: Karel Pospisilik
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Publication number: 20020099074Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same.Type: ApplicationFiled: December 19, 2001Publication date: July 25, 2002Applicant: Kowa Company, Ltd.,JapanInventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
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Publication number: 20020082283Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.Type: ApplicationFiled: September 13, 2001Publication date: June 27, 2002Applicant: Gliatech, Inc.Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
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Patent number: 6399628Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 12, 1999Date of Patent: June 4, 2002Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Jon K. Reel, Eugene D. Thorsett, Celia A. Whitesitt
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Publication number: 20020061914Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds represented by general formula (I) that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.Type: ApplicationFiled: November 9, 2001Publication date: May 23, 2002Inventors: Bo Skaaning Jensen, Lene Teuber, Dorte Strobaek, Palle Christophersen, Soren Peter Olesen
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Publication number: 20020049142Abstract: 1 A compund of formula (I) wherein X is O or S; n is 0 or 1; Y is O, S or NR7; R1 is hydrogen, halogen, C1-6 aklyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylthio, C1-6 haloalkylthio, C3-6 cycloalkyl, C1-6 alkoxy(C1-6)alkyl or SF5, R2 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylthio, C1-6 haloalkylthio, C1-6 alkylsulfinyl, C1-6 haloalkylsulfinyl, C1-6 alkylsulfonyl, C1-6 haloalkylsulfonyl, C1-6 haloalkyl, cyano, nitro, CHO, CH═NOR5, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl or SF5; or together R1 and R2 form a five or six membered saturated or unsturated carbocyclic ring, optionally substituted processes for preparing these compounds, compositions comprising them, methods of using them to combat fungal diseases and methods of using them to combat or control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: January 23, 2001Publication date: April 25, 2002Inventors: Christopher John Mathews, Russell Viner, Susan Patricia Barnett, Christopher John Urch, Stephen Christopher Smith, Patrick Jelf Crowley, William Guy Whittingham, Stephen Paul Heaney, John Williams, Torquil Eoghan Macleod Fraser, Eric Daniel Clarke, David John Hughes, Sarah Armstrong, Nigel John Barnes, Alan John Whittle, Brian Leslie Pilkington, John Pilkington
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Patent number: 6362208Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene or Ar represents an aryl group which may or may not have a substituent; X represents —NH—, oxygen atom or sulfur atom; Y represents —NR4—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z represents single bond or —NR5—; R4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; R5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and n represents an integer of 0 to 15.Type: GrantFiled: December 6, 1999Date of Patent: March 26, 2002Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
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Patent number: 6353006Abstract: This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.Type: GrantFiled: December 3, 1999Date of Patent: March 5, 2002Assignee: Bayer CorporationInventors: Brian R. Dixon, Cedo M. Bagi, Catherine R. Brennan, David R. Brittelli, William H. Bullock, Jinshan Chen, William L. Collibee, Robert Dally, Jeffrey S. Johnson, Harold C. E. Kluender, William F. Lathrop, Peiying Liu, Carol Ann Mase, Anikó M. Redman, William J. Scott, Klaus Urbahns, Donald J. Wolanin
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Publication number: 20020016460Abstract: Disclosed are novel compounds of formula (I): 1Type: ApplicationFiled: August 2, 2001Publication date: February 7, 2002Inventors: Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
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Patent number: 6303643Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 17, 2000Date of Patent: October 16, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Yoon T. Jeon, Charles Gluchowski
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Publication number: 20010020097Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: March 30, 1999Publication date: September 6, 2001Inventors: JAMES E. AUDIA, BEVERLY K. FOLMER, VARGHESE JOHN, LEE H. LATIMER, JEFFREY S. NISSEN, WARREN J. PORTER, EUGENE D. THORSETT, JING WU
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Patent number: 6268313Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: March 7, 2000Date of Patent: July 31, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
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Patent number: 6232470Abstract: Substituted Pyrazol-3-ylbenzazoles I salts thereof, and their use as herbicides or for the desiccation/defoliation of plants.Type: GrantFiled: June 16, 1999Date of Patent: May 15, 2001Assignee: BASF AktiengesellschaftInventors: Cyrill Zagar, Gerhard Hamprecht, Markus Menges, Olaf Menke, Peter Schäfer, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Patent number: 6204278Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.Type: GrantFiled: May 19, 1997Date of Patent: March 20, 2001Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
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Patent number: 6201126Abstract: Compounds of the formula (I) in which A represents N or a cyanomethylene radical, B represents S, O or NH and R1, R2, R3 and x have the meaning given in the description, are highly suitable for dyeing and printing high-molecular-weight materials, in particular automotive cover fabrics.Type: GrantFiled: June 2, 1997Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventor: Manfred Lorenz
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Patent number: 6124242Abstract: There are described ferredoxin:NADP reductase inhibitors, an assay system for the search for such inhibitors, and their use as herbicides.Type: GrantFiled: June 21, 1999Date of Patent: September 26, 2000Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Franz Rohl, Klaus Grossmann, Ralf-Michael Schmidt, Uwe Sonnewald, Mohammad Hajirezaei
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Patent number: 6084101Abstract: The present invention relates to a novel 2-hydroxy-naphthalene-3,6-dicarboxylic acid derivative. The compound is useful as a raw material for dyes, pigments, photosensitive materials and the like.Type: GrantFiled: June 5, 1998Date of Patent: July 4, 2000Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
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Patent number: 6048883Abstract: This invention provides compounds of formula (I):A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --Y.R.sup.2(I)or a tautomeric form thereof or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein A.sup.1, A.sup.2, A.sup.3, R.sup.2, X, Y and n are as defined herein; pharmaceutical composition comprising such compounds and the use of such a compounds for treating hyperglycemia.Type: GrantFiled: March 9, 1995Date of Patent: April 11, 2000Assignee: SmithKline Beecham p.l.c.Inventors: David Haigh, John Thomas Sime
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Patent number: 6007865Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.Type: GrantFiled: November 19, 1997Date of Patent: December 28, 1999Assignees: Alteon Inc., The Picower Institute for Medical ResearchInventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
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Patent number: 6002013Abstract: Compounds of the formula I ##STR1## and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III ##STR2## In the compounds of the formulae I and III: X is halogen,n is 0, 1, 2 or 3;Z is CN, CO--A or CS--A,A is hydrogen, halogen, OR.sub.1, SR.sub.2 and N(R.sub.3)R.sub.4 ;R.sub.1 to R.sub.4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R.sub.3 and R.sub.Type: GrantFiled: September 4, 1998Date of Patent: December 14, 1999Assignee: Novartis CorporationInventors: Walter Kunz, Beat Jau
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5965491Abstract: 1-Aryl-3-iminopyrazoles of the formula: ##STR1## wherein R.sub.31, R.sub.32, R.sub.33, R.sub.4, R.sub.5, R.sub.12, R.sub.13, R.sub.14, R.sub.15 and Z are as defined in the specification, are useful as pesticides or as intermediates to other pesticides. Compositions comprising the compounds of formula (I) and methods for their use, particularly in agriculture or for animal protection, as pesticides, especially for controlling arthropods, are described.Type: GrantFiled: March 9, 1998Date of Patent: October 12, 1999Assignee: Rhone-Poulenc Inc.Inventors: Tai-Teh Wu, David Treadway Manning
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Patent number: 5932600Abstract: The present invention relates to a novel class of compounds which are IMPDH 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 IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: March 14, 1997Date of Patent: August 3, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catharine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
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Patent number: 5919807Abstract: The invention relates to benzothiazoles and benzoxazoles of general formula ##STR1## wherein R.sup.1 to R.sup.3, X, Z and n are defined as in claim 1, the enantiomers, diastereomers and salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Dr. Karl Thomae GmbHInventors: Peter Muller, Rudolph Hurnaus, Roland Maier, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Leo Thomas, Gerhard Hallermayer
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Patent number: 5853703Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.Type: GrantFiled: January 18, 1996Date of Patent: December 29, 1998Assignees: The Picower Institute for Medical Research, Alteon Inc.Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
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Patent number: 5834500Abstract: Sulfur-containing heterocyclic bradykinin antagonists, process for their preparation, and their useCompounds of the formula (I) ##STR1## in which one of the radicals X.sub.1, X.sub.2 or X.sub.3 is C--O--R.sup.2 and the other X.sub.1, X.sub.2, and X.sub.3, in each case, and X.sub.4, are then, identically or differently, N or CR.sup.1 ; R.sup.1 and R.sup.3 are, identically or differently, H, halogen, (C.sub.1 -C.sub.6)-alkyl, O--R.sup.6, S--R.sup.6, NHR.sup.6, (C.sub.6 -C.sub.12)-aryl, (C.sub.6 -C.sub.12)-aryl-(C.sub.1 -C.sub.3)-alkyl, C(O)--OR.sup.6, C(O)--H, (C.sub.2 -C.sub.5)-alkenyl, NO.sub.2, SO.sub.3 R.sup.7, CN or C(O)--NHR.sup.8, where alkyl, aryl and alkenyl can optionally be substituted.Type: GrantFiled: May 16, 1997Date of Patent: November 10, 1998Assignee: Hoechst AktiengesellschaftInventors: Adalbert Wagner, Holger Heitsch, Gerhard Nolken, Klaus Wirth, Bernward Scholkens
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Patent number: 5795903Abstract: Compounds of formula (I): ##STR1## wherein R is a polyfluoroalkoxy or polyfluoroalkyl radical and R.sub.1 is a hydrogen atom and R.sub.2 is a hydroxyl radical, or R.sub.1 is a hydroxyl radical and R.sub.2 is a hydrogen atom, salts thereof, the preparation of said compounds, and drugs containing same.Type: GrantFiled: April 24, 1997Date of Patent: August 18, 1998Assignee: Rhone-Poulenc Rorer S.A.Inventors: Philip Chapelle, Claude Gaillard, Patrick Jimonet, Erik Louvel, Michel Martinet, Serge Mignani, Gerard Sanderink
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Patent number: 5712225Abstract: The present invention relates to oxa(di)azabicyclic and thia(di)azabicyclic compounds, a method for their preparation and their use as herbicides.Type: GrantFiled: February 28, 1996Date of Patent: January 27, 1998Assignees: E. I. du Pont de Nemours and Company, Degussa AktiengesellschaftInventors: Wonpyo Hong, Matthias Schafer, Thomas Martin Stevenson
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Patent number: 5677321Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: February 29, 1996Date of Patent: October 14, 1997Assignee: Synaptic Pharmaceutical CorporationInventors: Yoon T. Jeon, Charles Gluchowski
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Patent number: 5656261Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.Type: GrantFiled: January 18, 1995Date of Patent: August 12, 1997Assignees: The Picower Institute for Medical Research, Alteon Inc.Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
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Patent number: 5654323Abstract: A compound of formula (I): ##STR1## in which X, n, B and Y are as defined in the description. useful as cytokine inhibitors.Type: GrantFiled: June 1, 1995Date of Patent: August 5, 1997Assignee: Adir et CompagnieInventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
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Patent number: 5597819Abstract: New benzothiazine derivatives corresponding to the general formula I: ##STR1## in which: X represents halogen,n represents 0, 1, or 2,B represents the following formula: ##STR2## in which: R.sub.1 & R.sub.2 together with the carbons to which they are attached form a 6-carbon-atom aromatic ring which is optionally substituted by a group X' representing halogen, andY represents the radical --(SO.sub.2).sub.x --Alk--Z, x, Alk, and Z are as defined in the specification;as well as their possible stereoisomers, epimers, N-oxides and pharmaceutically-acceptable acid or base addition salts; and medicinal products containing the same, useful in the treatment of inflammatory disorders requiring an inhibitor of cytokines.Type: GrantFiled: February 13, 1995Date of Patent: January 28, 1997Assignee: Adir Et CompagnieInventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
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Patent number: 5576432Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.Type: GrantFiled: December 23, 1994Date of Patent: November 19, 1996Assignee: Eastman Kodak CompanyInventors: Roger Lok, Antony J. Williams
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Patent number: 5567716Abstract: Traumatic acid salts, wherein B is a cation selected from:a) a quaternary ammonium,b) a cation of a linear or branched C.sub.1 -C.sub.20 mono-, di- or trialkanolamine,c) a cation of a biologically active primary, secondary or tertiary amine,d) silver or zinc cation,and relative pharmaceutical compositions administrable by topical or parenteral route For the therapeutic treatment of cutaneous pathologies in which it is important to associate an a bacteriostatic, antibiotic, antifungal or an antiviral activity, to the cicatrizant effect, typical of traumatic acid.Type: GrantFiled: November 19, 1993Date of Patent: October 22, 1996Assignee: Lifegroup S.p.A.Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
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Patent number: 5552421Abstract: Various substituted benzoxazoles and benzothiazoles, are described and disclosed, which are potent inhibitors of leukotriene synthesis in warm-blooded animals.Type: GrantFiled: April 6, 1995Date of Patent: September 3, 1996Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Edward S. Lazer, Julian Adams, Clara K. Miao, Peter Farina
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Patent number: 5529998Abstract: The invention relates to benzoxazolyl- and benzothiazolyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.Type: GrantFiled: July 27, 1995Date of Patent: June 25, 1996Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Bernd Riedl, Martin Ruppelt, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus D. Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
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Patent number: 5476935Abstract: Dye-donor element for use according to thermal dye transfer comprising least one dye corresponding to the general formula (I): ##STR1## wherein Z is --CN, --COOR.sup.1 or --CONR.sup.2 R.sup.3 ; R.sup.1 is --H, (cyclo)alkyl, or aryl; R.sup.2 and R.sup.3 is --H, (cyclo)alkyl, aryl, or R.sup.2 and R.sup.3 together represent the atoms necessary to complete a heterocyclic nucleus; R.sup.4 and R.sup.5 is --H, (cyclo)alkyl, aryl, a heterocyclic ring, SO.sub.2 R.sup.8, COR.sup.8, CSR.sup.8, POR.sup.8 R.sup.9, OR.sup.6, NR.sup.6 R.sup.7, SR.sup.6, or R.sup.4 and R.sup.5 together represent the atoms necessary to complete a aliphatic ring, a heterocyclic ring including a heterocyclic ring carrying a fused-on aliphatic or aromatic ring; R.sup.6 and R.sup.7 is (cyclo)alkyl, aryl, alkenyl, aralkyl, aryl, a heterocyclic group, or R.sup.6 and R.sup.7 together represent the atoms necessary to complete a 5- or 6-membered ring; R.sup.8 and R.sup.Type: GrantFiled: May 18, 1994Date of Patent: December 19, 1995Assignee: Agfa-Gevert, N.V.Inventors: Luc Vanmaele, Hans Junek, Renate Dworczak
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Patent number: 5475014Abstract: An oxazolidone derivative represented by formula (I) which has a monoamine oxidase inhibition effect: ##STR1## {wherein A and B each represents a nitrogen atom, a sulfur atom or an oxygen atom, with the proviso than at least one of A and B must be a nitrogen atom,R.sup.1 represents a group of the formula: ##STR2## (in which n and m each represents 0 or an integer of 1 to 4, and R.sup.3 and R.sup.4 each represents a hydrogen atom, a hydroxyl group, a lower alkyl group, etc. ), a group represented by the formula: ##STR3## (in which p and q each represents 0 or an integer of 1 to 4 and X represents an oxygen atom, sulfur atom, etc.) and a group represented by the formula: ##STR4## R.sup.2 represents a hydrogen atom or a lower alkyl group}.Type: GrantFiled: March 8, 1994Date of Patent: December 12, 1995Assignee: Eisai Co., Ltd.Inventors: Kozo Akasaka, Akiharu Kajiwara, Satoshi Nagato, Youichi Iimura, Ichirou Yoshida, Atsushi Sasaki, Masanori Mizuno, Atsuhiko Kubota, Takaki Kagaya, Mariko Komatsu
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Patent number: 5432285Abstract: A novel chromogenic substrate to peroxidase enzymes is provided which is comprised of a mixture of an adduct formed from a hydrozone and a dienophile, and an aromatic nucleophile. The mixture undergos an oxidative coupling in the presence of peroxidase enzymes and peroxides forming a purple indamine dye. The mixture is also stable and unaffected by oxygen of the air or by hydrogen peroxide.Type: GrantFiled: May 28, 1993Date of Patent: July 11, 1995Inventors: Spyros Theodoropulos, Natalie S. Rudolph, James E. Woiszwillo
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Patent number: 5403930Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.Type: GrantFiled: October 7, 1993Date of Patent: April 4, 1995Assignee: Pharmacia ABInventors: Hubert Agback, Leif Ahrgren, Thomas Berglindh, Martin Haraldsson, Goran Smedeg.ang.rd, Lars-Inge Olsson
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Patent number: 5391720Abstract: Disclosed is an imidazole azo dye of formula (I), which is useful for image formation and as a filter dye, which has a sharp absorption wave and which is fast to light, heat, air, moisture and chemicals. Also disclosed is a thermal transfer dye-donating material containing imidazole azo dye(s) of formula (I) preferably along with aminopyrazole azo dye(s) of formula (II). The material gives a high-density image with good color reproduction, and the image formed has improved storage stability. ##STR1## In (I), B and C independently represent a hydrogen atom or a substituent capable of being substituted in the imidazole ring; A represents an aryl or heterocyclic group; provided that when B is a hydrogen atom, C is not a hydrogen atom nor an alkyl group having from 1 to 3 carbon atoms; provided that when C is a hydrogen atom, B is not a substituted nor unsubstituted alkyl group; provided that C is not a mercapto group or an alkylthio group; and provided that B is not a carboxyl group.Type: GrantFiled: December 3, 1992Date of Patent: February 21, 1995Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Mikoshiba, Tomomi Tateishi