Nitrogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/189)
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Publication number: 20150038483Abstract: The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ?C(R4)—, or ?N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, subType: ApplicationFiled: March 26, 2013Publication date: February 5, 2015Inventors: Akira Yukimasa, Naotake Kobayashi, Kenji Takaya, Yoshio Hato
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Patent number: 8835467Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: GrantFiled: January 23, 2013Date of Patent: September 16, 2014Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
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Publication number: 20140065095Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: June 5, 2013Publication date: March 6, 2014Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
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Patent number: 8513252Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X1, X2, (A)m and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: GrantFiled: July 14, 2010Date of Patent: August 20, 2013Assignee: Addex Pharma S.A.Inventor: Christelle Boléa
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Publication number: 20130143927Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: June 8, 2012Publication date: June 6, 2013Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Patent number: 8383653Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: GrantFiled: June 30, 2004Date of Patent: February 26, 2013Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
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Publication number: 20120122907Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X1, (A)m and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 14, 2010Publication date: May 17, 2012Inventor: Christelle Boléa
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Patent number: 7982048Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: GrantFiled: July 23, 2010Date of Patent: July 19, 2011Assignee: Magnesium Diagnostics, Inc.Inventor: Ibert Clifton Wells
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Publication number: 20110009261Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6 together with the adjacent nitrogen forms a 3 to 10-membered saturated ring, wherein the ring may contain, in addition to the nitrogen and carbon ring members, 1, 2 or 3 heteroatoms and/or heteroatom groups as ring members, independently of one another, selected from the group consisting of sulfur, CO, SO, SO2 and N—R7 and/or the ring may carry 1, 2 or 3 radicals, independently of one another, each selected, for example, from the group consisting of halogen, cyano, nitro, amino, and C1-C6-alkyl. R2 is, for example, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy or C1-C6-alkoxy-C1-C6-alkoxy, and R7 is for example, R10C(?O), C1-C6 alkyl or C1-C6-haloalkyl; and/or salts thereof; and their use as pesticidal agents.Type: ApplicationFiled: March 2, 2009Publication date: January 13, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Peter Maienfisch, Ottmar Hueter, Peter Renold, Werner Zambach, Thomas Pitterna
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Publication number: 20100285957Abstract: The present invention relates to thiazolyloxyphenylamidines or thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.Type: ApplicationFiled: December 9, 2008Publication date: November 11, 2010Applicant: Bayer CropScience AGInventors: Klaus Kunz, Pierre Cristau, Joerg Nico Greul, Ulrich Heinemann, Kerstin Ilg, Amos Mattes, Oswald Ort, Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Heinz Kehne, Dirk Schmutzler, Hiroyuki Hadano
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Publication number: 20100222392Abstract: A compound of formula (I) wherein A1, A2, A3, A4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.Type: ApplicationFiled: October 13, 2008Publication date: September 2, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Werner Zambach, Peter Renold
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Patent number: 7541373Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: GrantFiled: March 1, 2006Date of Patent: June 2, 2009Assignee: Novo Nordisk A/SInventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M. M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen, Jesper Lau
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Patent number: 7498445Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: GrantFiled: November 4, 2005Date of Patent: March 3, 2009Assignee: Renopharm Ltd.Inventors: Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Publication number: 20080255196Abstract: The present invention relates to aryloxy substituted phenylamidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions (I).Type: ApplicationFiled: September 12, 2006Publication date: October 16, 2008Applicant: Bayer CropScience AGInventors: Klaus Kunz, Jorg Greul, Oliver Guth, Benoit Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Ralf Dunkel, Ronald Ebbert, Eva-Maria Franken, Olga Malsam
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Patent number: 7388098Abstract: Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and thType: GrantFiled: September 24, 2001Date of Patent: June 17, 2008Assignee: Bristol-Myers Squibb CompanyInventors: John J. Venit, Gary D. Madding, Victor W. Rosso, Francis J. Okuniewicz, Robert P. Discordia, Susanne Kiau, Atul S. Kotnis, Michael E. Randazzo, D. David Hennings, Jingyang Zhu, Jason G. Chen
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Patent number: 7335778Abstract: The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I): wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a): wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.Type: GrantFiled: December 4, 2002Date of Patent: February 26, 2008Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Masahiko Seki, Toshiaki Shimizu, Shin-ichi Yoshida, Masanori Hatsuda
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Patent number: 7323564Abstract: The present invention is directed to a process for preparing a compound having the formula: wherein R is a range of organic groups and X is a leaving group. The process may include reacting a compound of the formula with a water-removing reagent. Also, when X is a halogen, the process may include reacting a compound of the formula with a halogenating agent or a sulfonylating agent. Alternatively, when X is a halogen, the process may be carried out by reacting a compound of the formula IV where R2 and R3 are defined organic groups with a compound of the formula halogen-C(—O)—O—C1 -C8alkyl, halogen-C(—O)—O-aryl or halogen-C(—O)—O-benzyl.Type: GrantFiled: October 24, 2006Date of Patent: January 29, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Huter, Thomas Rapold, Marcel Senn, Thomas Gobel, Anthony O'Sullivan
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7202404Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1–C2 alkoxy; C1–C2 haloalkoxy; cyano; or C1–C2 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; R2 is hydrogen; halogen; or C1–C4 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; R3 is hydrogen; halogen; C1–C4 alkoxy; C1–C4 haloalkoxy; or C1–C4 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; or R2 and R3 can be taken together as —CH2CH2—; R4 is C1–C2 alkyl; R5 is R6, CH(R8)OR6, CH(R8)CH(R7)R6 or C(R8)?C(R7)R6; R6, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.Type: GrantFiled: November 25, 2002Date of Patent: April 10, 2007Inventors: Gregory S. Basarab, Lee Dalton Jennings, Dennis R. Rayner
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Patent number: 7183301Abstract: The present invention relates to novel oxazolidinone compounds of the general formula (I). where R1, R2, R3, Y1, Y2, Y3, and Z are as defined in the description; their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.Type: GrantFiled: August 1, 2003Date of Patent: February 27, 2007Assignee: Dr. Reddy's Research FoundationInventors: Selvakumar Natesan, Jagattaran Das, Javed Iqbal, Sitaram Kumar Magadi, Srinivasa Rao Naga Venkata Mamidi, Rajagopalan Ramanujam, Baskaran Sundarababu, Braj Bhushan Lohray
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Patent number: 7129243Abstract: The present invention relates to a compound of the formula (I) wherein R1 is benzofuranyl substituted by halogen, or styryl substituted by halogen; R2 is substituted hydroxy, substituted mercapto or substituted sulfonyl; and X is or pharmaceutically acceptable salts thereof.Type: GrantFiled: December 18, 2001Date of Patent: October 31, 2006Assignee: Astellas Pharma Inc.Inventors: Ichiro Shima, Takehiko Ohkawa, Kentaro Sato, Naoki Ishibashi, Kenichiro Imamura
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Patent number: 7109223Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.Type: GrantFiled: August 25, 2003Date of Patent: September 19, 2006Assignee: Merck & Co. Inc.Inventors: Yongxin Han, John Colucci, Xavier Billot, Marie-Claire Wilson, Robert Young
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Patent number: 6908939Abstract: Novel pharmaceutical/cosmetic compositions contain at least one biaromatic ligand activator of a PPAR? receptor, such biaromatic ligand having the structural formula (I): and are well suited, inter alia, for regulating and/or restoring skin lipid metabolism, for treating a wide variety of dermatological afflictions, and for preventing and/or treating the signs of aging and/or dry skin.Type: GrantFiled: December 23, 2002Date of Patent: June 21, 2005Assignee: Galderma Research & Development S.N.C.Inventors: Jean-Michel Bernardon, Laurence Clary, Eric Terranova
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Patent number: 6762198Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: March 25, 2003Date of Patent: July 13, 2004Assignee: The Procter & Gamble CompanyInventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
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Publication number: 20030229127Abstract: Compounds of Formula (I), 1Type: ApplicationFiled: June 5, 2003Publication date: December 11, 2003Applicants: Wyeth, ArQule Inc.Inventors: Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
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Publication number: 20030216579Abstract: Described is a process for the preparation of a compound of the formula 1Type: ApplicationFiled: March 27, 2003Publication date: November 20, 2003Inventors: Thomas Pitterna, Thomas Rapold, Marcel Senn, Thomas Gobel, Anthony Cornelius O'Sullivan
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Publication number: 20030203951Abstract: The present invention relates to novel compounds that can be used as antiinflammatory, immunomodulatory and antiproliferatory agents. In particular the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehydrogenase (DHODH).Type: ApplicationFiled: July 9, 2002Publication date: October 30, 2003Applicant: 4SC AGInventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
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Patent number: 6566381Abstract: Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.Type: GrantFiled: March 1, 2000Date of Patent: May 20, 2003Assignee: The Procter & Gamble CompanyInventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
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Patent number: 6528652Abstract: Thiazole esters are suitable for detecting the presence of leukocytes in urine. Such thiazole esters are suitable for use in compositions, diagnostic devices, and methods for detecting the presence of leukocytes. A thiazole ester of the invention is of the formula: or a salt or solvated salt thereof, in which A is an N-blocked amino acid residue or N-blocked peptide chain, preferably an alanine residue or polyalanine chain; and R1 and R2 are each independently hydrogen, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkoxy, amino, unsubstituted or substituted acyl, halo, nitro, cyano, —SO3H, or hydroxy, with the proviso that R1 and R2 are not both hydrogen. In one embodiment, at least one of R1 and R2 is methoxy, ethoxy, propoxy, or butoxy. In still another embodiment, R1 is hydrogen and R2 is methoxy, ethoxy, propoxy, or butoxy.Type: GrantFiled: July 30, 1999Date of Patent: March 4, 2003Assignee: ChronimedInventor: Nam-Won Huh
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Patent number: 6452014Abstract: Thiazolidinedione compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatment of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are methods for assaying or screening for inhibitors of telomerase activity.Type: GrantFiled: December 22, 2000Date of Patent: September 17, 2002Assignee: Geron CorporationInventors: Tsutomu Akama, Ryan Holcomb, Richard L. Tolman
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Patent number: 6432993Abstract: Substituted fused heterocyclic compounds of the formula (I) and pharmacologically acceptable salts thereof: wherein R1 is a group of the formula (II) or (III): R4 is a substituted phenyl or a pyridyl which may have a substituent. R5 is hydrogen or the like. R6 is hydrogen, a C1-6 alkyl group or the like. D is oxygen or sulfur. E is a CH group or nitrogen. R2 is hydrogen or the like. R3 is a 2,4-dioxothiazolidin-5-ylmethyl group or the like. A is a C1-6 alkylene group. B is oxygen or sulfur. These compounds and salts are useful as the active ingredient of pharmaceutical compositions which can be used to treat patients because these compounds and salts have excellent insulin-resistance improving action, lipid-peroxide-production inhibitory action, 5-lipoxygenase inhibitory action and the like.Type: GrantFiled: April 7, 2000Date of Patent: August 13, 2002Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Kunio Wada, Toshihiko Fujiwara
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Patent number: 6413997Abstract: 3-(Substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.Type: GrantFiled: October 22, 1999Date of Patent: July 2, 2002Assignee: Dow AgroSciences LLCInventors: Francis E. Tisdell, Peter L. Johnson, James T. Pechacek, Robert G. Suhr, Donald H. DeVries, Carl P. Denny, Mary L. Ash
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Patent number: 6369233Abstract: The Invention relates to a process for the preparation of a compound of the formula wherein Q, Y, Z, R1, R2, R3, R4 and R5 are as defined in the specification, which comprises a) reacting a compound of the formula with a halogenating agent to form a compound of the formula b) converting a compound of formula (II) by means of a halogenating agent into a compound of the formula optionally c) converting the compound of formula (IV) into a compound of formula (III); d) converting a compound of formula (III) by means of a compound of the formula e) converting a compound (IV) by means of a compound (V) into a compound (VI); and f) converting a compound (VI) by means of a chlorinating agent into a compound (I); a compound (IV); to a process for the preparation of a compound (III) and to a process for the preparation of a compound (IV).Type: GrantFiled: August 1, 2000Date of Patent: April 9, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Hüter, Thomas Rapold, Marcel Senn, Thomas Göbel, Anthony Cornelius O'Sullivan, Gottfried Seifert
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Publication number: 20020019383Abstract: The present invention relates to pharmaceutical compositions containing, as active ingredient, a compound of formula: 1Type: ApplicationFiled: March 2, 2001Publication date: February 14, 2002Inventors: Daniel Achard, Herve Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
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Patent number: 6252083Abstract: Carbamates of the formula I where the substituents have the following meanings: Z is methoxy, NH2, NHCH3, N(CH3)2, CH3, C2H5, CF3 or CCl3, X and Y are identical or different and each is hydrogen, F, Cl, Br, CF3, CN, NO2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring, R1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O—CO2-alkyl, A is —O—, —S—, —CR2═CR3—, CHR2—O—, —CHR2—S—, —CHR2—O—N═C(R4)—, —CR2═N—O—, —O—N═C(R4)—, —C≡C—, —CHR2—CHR3—, —CHR2—O—CO—, —O—CHR2— or a single bond, B is substituted or unsubstituted and is alkyl, alkeType: GrantFiled: March 16, 2000Date of Patent: June 26, 2001Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 6177571Abstract: A method for removing heavy metals, selected from palladium, tin and nickel, from heavy metal complexes with thiazole compounds in aqueous or alcoholic solution, by precipitation as sulfides, characterised in that such solutions are treated with a water-soluble ammonium, alkaline or alkaline-earth sulfide.Type: GrantFiled: September 27, 1999Date of Patent: January 23, 2001Assignee: Zambon Group S.p.A.Inventor: Mario Fantucci
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Patent number: 6174908Abstract: Certain thiazolidinone and metathiazanone compounds, as described, are useful as potassium channel inhibitors and are especially useful for the treatment of cardiac arrhythmias and other diseases, conditions and disorders.Type: GrantFiled: May 1, 1999Date of Patent: January 16, 2001Assignees: ICAGen, Inc., Eli Lilly & Company Lilly Corporate CenterInventors: Michael F. Gross, Neil A. Castle, Jose S. Mendoza
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Patent number: 6110946Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.Type: GrantFiled: July 1, 1998Date of Patent: August 29, 2000Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
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Patent number: 6096898Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.Type: GrantFiled: October 22, 1999Date of Patent: August 1, 2000Assignee: Dow AgroSciences LLCInventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
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Patent number: 6075148Abstract: Carbamates of the formula I where the substituents have the following meanings:Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.Type: GrantFiled: March 25, 1999Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 6063800Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.Type: GrantFiled: February 19, 1999Date of Patent: May 16, 2000Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 6057349Abstract: The present invention concerns novel compounds represented by the Formula: ##STR1## wherein: A is R.sup.1.sub.q (R.sup.3 R.sup.60 N).sub.m (Z)(NR.sup.2).sub.n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C.dbd.O or SO.sub.2 ; n is 1 with the proviso that, when Z is C.dbd.O, m is 1; X is --NH--, --CH.sub.2 --, or --OCH.sub.2 --; Y is [2-imidazoline, 2-oxazolin] 2-thiazoline, [or 4-imidazole] R.sup.1 is H, lower alkyl, or phenyl, with the proviso that, when R.sup.1 is H, m is 1; R.sup.2, R.sup.3, R.sup.60 are each independently H, lower alkyl, or phenyl; R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are each independently hydrogen, lower alkyl, --CF.sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R.sup.2 and R.sup.Type: GrantFiled: March 8, 1999Date of Patent: May 2, 2000Assignee: F. Hoffman La Roche AGInventors: Richard Leo Cournoyer, Paul Francis Keitz, Counde O'Yang, Dennis Mitsugu Yasuda
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Patent number: 6037354Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: June 17, 1998Date of Patent: March 14, 2000Assignee: Merck & Co., Inc.Inventors: Michael A. Patane, Harold G. Selnick, Mark G. Bock
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Patent number: 5990135Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: November 23, 1999Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing Leung Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5981532Abstract: Carbamates of the formula I ##STR1## wherein B is a saturated or unsaturated heterocyclic group, and the other substituents are defined in the specification, and having crop protection properties.Type: GrantFiled: July 7, 1998Date of Patent: November 9, 1999Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5968958Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: June 19, 1997Date of Patent: October 19, 1999Assignee: Merck Frosst Canada, Inc.Inventors: Daniel Guay, Chun-Sing Li, Nathalie Ouimet
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Patent number: 5914328Abstract: Novel heterocyclic ether compounds of the formula: ##STR1## wherein *, A,B, n, R.sup.1, R.sup.2 and X are specifically defined, or pharmaceutically-acceptable salts or prodrugs thereof, which are useful in selectively activating or inhibiting neurotransmitter release; to therapeutically-effective pharmaceutical compositions of these compounds; and to the use of said compositions to activate or inhibit neurotransmitter release in mammals.Type: GrantFiled: June 7, 1995Date of Patent: June 22, 1999Assignee: Abbott LaboratoriesInventors: Nan-Horng Lin, Mark W. Holladay, Melwyn A. Abreo, David E. Gunn, Suzanne A. Lebold, Richard L. Elliott, Yun He
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Patent number: RE37355Abstract: 6-dimethylaminomethyl-1-phenyl-cyclohexane compounds, methods of preparing them and the use of these compounds in drugs are described.Type: GrantFiled: March 30, 2000Date of Patent: September 4, 2001Assignee: Gruenenthal GmbHInventors: Helmut Heinrich Buschmann, Wolfgang Werner Alfred Strassburger, Norma Selve, Elmar Josef Friderichs