Nitrogen In Substituent Q Patents (Class 564/163)
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Publication number: 20080214869Abstract: The invention is directed to improved processes of purifying tigecycline.Type: ApplicationFiled: March 3, 2008Publication date: September 4, 2008Inventors: Sergei Fine, Slavik Yurkovski, Sofia Gorohovsky-Rosenberg, Evgeny Tsiperman
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Publication number: 20080200551Abstract: This invention relates to a novel fluorene derivative having a characteristic structure in which guanidino group or the like functional group is linked to the fluorene structure via carbonyl group, or a salt thereof. The compound of the invention has an advantage in that it has high affinity for serotonin receptor subtypes, particularly for 5-HT2B receptor and 5-HT7 receptor, and shows excellent pharmacological effects in comparison with the conventional compounds which have only one of the antagonistic activities of 5-HT2B receptor and 5-HT7 receptor, this is useful as a prophylactic antimigraine agent having high safety and excellent effect.Type: ApplicationFiled: February 17, 2005Publication date: August 21, 2008Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Koichiro Harada, Jiro Fujiyasu, Yuji Koga, Makoto Oku, Toshio Okazaki, Shinobu Akuzawa, Toshihiro Watanabe
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Publication number: 20080194536Abstract: The present invention relates to a compound represented by the following formula: (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or a combination thereof, wherein Ro, R1, R1?, R2, R2?, R3 and n are defined herein. The present invention further relates to a method of treating a patient from endometreosis or uterine fibroids.Type: ApplicationFiled: April 14, 2006Publication date: August 14, 2008Inventors: Marlys Hammond, David G. Jones, Istvan Kaldor, Lara S. Kallander, Xi Lang, Scott Kevin Thompson, Philip Stewart Turnbull, David G. Washburn
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Publication number: 20080194859Abstract: The invention is directed to novel compounds that are used in the formation of polyurea compositions, including one-part and two-part polyurea compositions. The invention is also directed to polyureas formed from such compounds, cross-linked polyureas, and UV-stabilized polyureas.Type: ApplicationFiled: May 16, 2005Publication date: August 14, 2008Inventors: Kenneth I. Sawyer, Robert J. Kupper
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Publication number: 20080188468Abstract: The invention relates to substituted para-trifluoromethyl phenyl ether compounds and its preparation and use thereof especially. The substituted para-trifluoromethyl phenyl ether compounds of the invention having general formula (I): The substitutes see Description. The compounds of present invention have broad-spectrum activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete, and it may also provide good control efficacy at very low dosage because of the high activity. The compounds of the invention have good insecticidal activity and have good activity against many pests, especially for Carmine spider mite. The compounds are fit for synthetical control against many kinds of pests.Type: ApplicationFiled: June 15, 2006Publication date: August 7, 2008Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY, SINOCHEM CORPORATIONInventors: Changling Liu, Huiwei Chi, Dongliang Cui, Miao Li, Zhinian Li, Yanmei Luo, Jing Yuan
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Patent number: 7405307Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: September 13, 2007Date of Patent: July 29, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
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Patent number: 7390923Abstract: Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g., in the treatment or prevention of male hypogonadism and age-related conditions such as andropause.Type: GrantFiled: June 24, 2004Date of Patent: June 24, 2008Assignee: Orion CorporationInventors: Jari Ratilainen, Anu Moilanen, Olli Törmäkangas, Arja Karjalainen, Paavo Huhtala, Gerd Wohlfahrt, Pekka Kallio
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Patent number: 7348456Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: GrantFiled: December 15, 2003Date of Patent: March 25, 2008Assignee: Merck & Co., Inc.Inventors: Linus S. Lin, William K. Hagmann, Sanjeev Kumar, Wenji Yin, George Doss
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Patent number: 7345200Abstract: A compound having the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, wherein R1 comprises a chromophore that absorbs light from the visible wavelength range, and wherein n is an integer of at least 12. A solid phase change ink composition is also disclosed containing a colorant comprising a chromophore that absorbs light from the visible wavelength range and has the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, and wherein n is an integer of at least 12. Also disclosed is a method of forming a colorant wherein a first compound having the formula is reacted with a second compound having the formula Z(CH2)nCH3 wherein n is an integer of at least 12 to form a third compound having the formula wherein the third compound comprises a chromophore that absorbs light from the visible wavelength range.Type: GrantFiled: February 16, 2006Date of Patent: March 18, 2008Assignee: Xerox CorporationInventors: Jeffrey H. Banning, Michael B. Meinhardt, Donald R. Titterington, Clifford R. King
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Patent number: 7323595Abstract: A compound having the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, wherein R1 comprises a chromophore that absorbs light from the visible wavelength range, and wherein n is an integer of at least 12. A solid phase change ink composition is also disclosed containing a colorant comprising a chromophore that absorbs light from the visible wavelength range and has the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, and wherein n is an integer of at least 12. Also disclosed is a method of forming a colorant wherein a first compound having the formula is reacted with a second compound having the formula Z(CH2)nCH3 wherein n is an integer of at least 12 to form a third compound having the formula wherein the third compound comprises a chromophore that absorbs light from the visible wavelength range.Type: GrantFiled: February 16, 2006Date of Patent: January 29, 2008Assignee: Xerox CorporationInventors: Jeffrey H. Banning, Michael B. Meinhardt, Donald R. Titterington, Clifford R. King
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Patent number: 7294649Abstract: Compounds of methamphetamine derivatives having a meta-substituted alkyl linker on the benzene ring and a protective group on the nitrogen of the methamphetamine hapten. Such compounds have the structure wherein R1 is an alkyl linker comprising 2-15 carbon atoms and 0-6 heteroatoms, R2 is a leaving group, and R3 is a protecting group.Type: GrantFiled: December 17, 2004Date of Patent: November 13, 2007Assignee: Roche Diagnostics Operatins, Inc.Inventors: Raymond A. Hui, Stephen S. Vitone
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Patent number: 7285680Abstract: A compound of the general formula (I) (wherein the symbols are as defined in the description), or a prodrug or a salt thereof.Type: GrantFiled: May 28, 2003Date of Patent: October 23, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiromu Habashita, Masahiko Terakado, Shinji Nakade, Takuya Seko
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Patent number: 7247736Abstract: The present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains a non-aromatic ring system as a core structure, a group capable of interacting with structural elements of subsite 2 or 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH. Furthermore, the present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains an aromatic ring system as a core structure, a group capable of interacting with residues His 56 and/or Tyr 356 of subsite 3 of the ubiquinone binding site of DHODH and a group capable of interacting hydrophobically with structural elements of subsite 1 of the ubiquinone binding site of DHODH.Type: GrantFiled: November 10, 2004Date of Patent: July 24, 2007Assignee: 4SC AGInventors: Johann Leban, Bernd Kramer, Roland Baumgartner, Katharina Aulinger-Fuchs, Stefan Tasler
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Patent number: 7223888Abstract: Novel compounds and compositions including those compounds, as well as methods of using and making the compounds are herein described. The compounds are useful in therapeutic applications, including modulation of disease or disease symptoms in a subject (e.g., mammal, human, dog, cat, horse). The compounds are useful as modulators of the mu opioid receptor (MOR) through their binding affinity with that receptor.Type: GrantFiled: October 10, 2003Date of Patent: May 29, 2007Assignee: President and Fellows of Harvard CollegeInventors: Bryce A. Harrison, Tiffany M. Gierasch, Gregory L. Verdine, Zhangjie Shi
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Patent number: 7208630Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.Type: GrantFiled: October 27, 2004Date of Patent: April 24, 2007Assignee: University of KansasInventors: Brian Blagg, Gang Shen, Randell C. Clevenger
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Patent number: 7169816Abstract: Phenylamino benzhydroxamic acid derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.Type: GrantFiled: October 12, 2005Date of Patent: January 30, 2007Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
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Patent number: 7151195Abstract: The present invention relates to a phthalamide derivative represented by the general formula (I): wherein R1, R2, R3, X, Y, m, and n are as defined in the disclosure, which can be used as the active ingredient in an agricultural or horticultural insecticide that exhibits an excellent insecticidal effect even when used in a small active-ingredient amount.Type: GrantFiled: May 1, 2003Date of Patent: December 19, 2006Assignee: Bayer CropScience LPInventors: Yoshihiro Matsuzaki, Masayuki Morimoto, Shinsuke Fujioka, Masanori Tohnishi
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Patent number: 7147866Abstract: Highly effective vesicular compositions from UV-absorbing lipids are described in the present invention. Combination of UV-absorbing property and the vesicular delivery system results in higher levels of photoprotection to skin and hair. The vesicular compositions of the present invention are made from cationic UV-absorbing lipids of Formula I wherein, ArCO is selected from cinnamoyl, p-methoxy cinnamoyl, p-N,N-dimethylamino benzoyl and combinations thereof, R1 is selected from saturated or unsaturated alkyl group with carbons ranging from C10 to C22.Type: GrantFiled: September 29, 2004Date of Patent: December 12, 2006Assignee: Galaxy Surfactants LimitedInventors: Nirmal Madhukar Koshti, Shubhangi Dattaram Naik, Tanaji Shamrao Jadhav
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Patent number: 7135587Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5?, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.Type: GrantFiled: November 30, 2001Date of Patent: November 14, 2006Assignee: Merck Patent GmbHInventors: Wolfgang Staehle, Alfred Jonczyk, Oliver Schadt, Simon Goodman
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Patent number: 7132559Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the nvention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluorleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbonfluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.Type: GrantFiled: February 25, 2002Date of Patent: November 7, 2006Assignee: Trustees of Tufts CollegeInventors: Alfio Fichera, Zihni Bilgicer, Krishna Kumar, Xuechao Xing
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Patent number: 7129238Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.Type: GrantFiled: November 21, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
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Patent number: 7060856Abstract: This invention provides a novel polymorphic form of N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, as well a pharmaceutical compositions and therapeutic methods utilizing the polymorphic form.Type: GrantFiled: October 20, 2004Date of Patent: June 13, 2006Assignee: Warner-Lambert CompanyInventors: Dainius Macikenas, Thomas Nanninga
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Patent number: 7049271Abstract: The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): in which Ar, X, Z, Y and K are each as defined in the description, to a plurality of processes for their preparation and to their use as herbicides and pesticides.Type: GrantFiled: April 25, 2001Date of Patent: May 23, 2006Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jutta Böhmer, Ralf Wischnat, Mark Wilhelm Drewes, Peter Dahmen, Rolf Pontzen, Peter Lösel, Christoph Erdelen, Dieter Feucht
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Patent number: 7045660Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: GrantFiled: March 3, 2004Date of Patent: May 16, 2006Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 7041844Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.Type: GrantFiled: November 18, 2002Date of Patent: May 9, 2006Assignee: The University Of Tennessee Research CorporationInventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
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Patent number: 7022879Abstract: The invention encompasses a compound having the formula: wherein R1, Z and the carbonyl can be comprised by a common ring, wherein R1 comprises a chromophore that absorbs light from the visible wavelength range, and wherein n is an integer that is at least 12. The invention also encompasses a solid phase change ink composition. Such composition includes a phase change ink carrier and a colorant. The colorant comprises a chromophore that absorbs light from the visible wavelength range, and has the formula: wherein R1, Z and the carbonyl can be comprised by a common ring, wherein n is an integer that is at least 12. Additionally, the invention encompasses a method of forming a colorant. A first compound having the formula, is reacted with a second compound having the formula Z(CH2)nCH3, wherein n is an integer that is at least 12, to form a third compound having the formula, wherein the third compound comprises a chromophore that absorbs light from the visible wavelength range.Type: GrantFiled: January 30, 2001Date of Patent: April 4, 2006Assignee: Xerox CorporationInventors: Jeffrey H. Banning, Michael B. Meinhardt, Donald R. Titterington, Clifford R. King
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Patent number: 7012081Abstract: Substituted anthranilamides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of anthranilamides are described.Type: GrantFiled: May 7, 2001Date of Patent: March 14, 2006Assignee: Schering AGInventors: Martin Krueger, Andreas Huth, Orlin Petrov, Dieter Seidelmann, Karl-Heinz Thierauch, Martin Haberey, Andreas Menrad, Alexander Ernst
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Patent number: 7005546Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.Type: GrantFiled: June 22, 2004Date of Patent: February 28, 2006Assignee: Renovis, Inc.Inventors: William Flitter, William Garland, Richard Paylor, Allan Wilcox
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Patent number: 7005437Abstract: The present invention relates to new substituted aryl and heteroaryl derivatives of general formula wherein A, Ar, n, X, Y1, Y2, Y3, Y4, R1 and R5 are defined as in claim 1, the prodrugs, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. Thus, the compounds of the above general formula I wherein R5 does not contain a cyano group have, in particular, an antithrombotic effect and a selective factor Xa-inhibiting effect with generally improved compatibility. The compounds of the above general formula I wherein R5 contains a cyano group are valuable intermediate products for preparing the antithrombotic compounds of general formula I.Type: GrantFiled: May 10, 2002Date of Patent: February 28, 2006Assignee: Boehringer Ingelheim Pharma KGInventors: Henning Priepke, Uwe Ries, Herbert Nar, Wolfgang Wienen, Jean-Marie Stassen
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Patent number: 6995284Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: October 22, 2002Date of Patent: February 7, 2006Assignee: The University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
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Patent number: 6995269Abstract: Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.Type: GrantFiled: March 4, 2003Date of Patent: February 7, 2006Assignee: Chiron CorporationInventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, David Duhl
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Patent number: 6960581Abstract: A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: January 3, 2003Date of Patent: November 1, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, David S. Thomson, Yan Zhang, Renee Michele Zindell
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Patent number: 6919377Abstract: Described are compounds of Formula I and Formula II and their pharmaceutically acceptable salts. The compounds of Formulas I and II are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.Type: GrantFiled: April 24, 2001Date of Patent: July 19, 2005Assignee: Warner Lambert Company LLCInventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Patent number: 6858626Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.Type: GrantFiled: June 20, 2002Date of Patent: February 22, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Chu-Biao Xue, Carl P. Decicco, Xiaohua He
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Patent number: 6838472Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: GrantFiled: September 17, 2002Date of Patent: January 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Publication number: 20040266737Abstract: The present invention provides pharmaceutical preparations and the uses thereof for preventing and/or treating seizures and other electroconvulsive disorders by administering a pharmaceutically effective amount of a therapeutic compound having the following formula (I): 1Type: ApplicationFiled: May 14, 2004Publication date: December 30, 2004Applicant: University of KentuckyInventors: Peter A. Crooks, Aimee Karis Bence, David Robert Worthern
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Patent number: 6831197Abstract: The present application relates to a plurality of novel processes for preparing 2-(2-hydroxyphenyl)-2-(alkoxyimino)-N-methylacetamide derivatives, to novel intermediates for their preparation, and to processes for preparing these intermediates.Type: GrantFiled: January 14, 2004Date of Patent: December 14, 2004Assignee: Bayer AktiengesellschaftInventors: Walter Hübsch, Bernd Gallenkamp, Herbert Gayer, Lubbertus Mulder, Thorsten Müh, Reinhard Lantzsch, Holger Weintritt
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Patent number: 6825236Abstract: Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group —C(O)—(CHR4)m—AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R1 is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R2 (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R3; R3 (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R2; and R4 is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed.Type: GrantFiled: April 14, 2003Date of Patent: November 30, 2004Assignees: California Pacific Medical Center, Catholic Healthcare WestInventor: Li-Xi Yang
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Publication number: 20040235911Abstract: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.Type: ApplicationFiled: June 25, 2004Publication date: November 25, 2004Applicant: Tularik Inc.Inventors: Leping Li, Xiaoqi Chen, Pingchen Fan, Jeffrey Thomas Mihalic, Serena Cutler
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Patent number: 6821963Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.Type: GrantFiled: June 4, 2002Date of Patent: November 23, 2004Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
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Patent number: 6812231Abstract: Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.Type: GrantFiled: February 14, 2002Date of Patent: November 2, 2004Assignee: Ajinomoto Co., Inc.Inventors: Tadakiyo Nakagawa, Kazuyuki Sagi, Kaoru Yoshida, Yumiko Fukuda, Masataka Shoji, Shunji Takehana, Takashi Kayahara, Akira Takahara
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Publication number: 20040192731Abstract: Disclosed are compounds of Formula I, their N-oxides and agricultually suitable salts (I) wherein J is a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system wherein each ring or ring system is substituted with from one to four substituents independently selected from R5; and A, B, G, R1, R2, R3, R4, R5, R6 and n are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the pests or their environment with a biologically effective amount of a compound of Formula (I) and compositions containing the compounds of Formula (I).Type: ApplicationFiled: January 7, 2004Publication date: September 30, 2004Inventors: Bruce Lawrence Finkelstein, George Philip Lahm, Tom Paul Selby, Thomas Martin Stevenson
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Publication number: 20040192741Abstract: Novel calcilytic compounds and methods of using them are provided.Type: ApplicationFiled: January 21, 2004Publication date: September 30, 2004Applicant: SmithKline Beecham Corporation & NPS PharmaceuticalsInventors: Maria Amparo Lago, James Francis Callahan, Pradip Kumar Bhatnagar, Eric G. Del Mar, William M. Bryan, Joelle L. Burgess
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Publication number: 20040171881Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: November 8, 2002Publication date: September 2, 2004Inventors: Varghese John, Michel Maillard, Barbara Jagodzinska, James Beck, Andrea Gailunas, John Freskos, John Mickelson, Lakshman Samala, Jennifer Sealy, Ruth TenBrink, Lawrence Fang, Roy Hom
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Patent number: 6777442Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.Type: GrantFiled: February 26, 2002Date of Patent: August 17, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Peter Ellinghaus
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Patent number: 6770778Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.Type: GrantFiled: January 23, 2003Date of Patent: August 3, 2004Assignee: Pfizer IncInventors: Stephen Douglas Barrett, Michael David Kaufman, Gordon William Rewcastle, Julie Ann Spicer
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Publication number: 20040147584Abstract: 1,3-Diarylprop-2-en-1-ones and derivatives, compositions containing them, manufacturing process and use. Substituted 1,3-diarylprop-2-en-1-ones with therapeutic activity may be used in oncology.Type: ApplicationFiled: December 4, 2002Publication date: July 29, 2004Applicant: Aventis Pharma S.A.Inventors: Patrick Mailliet, Cecile Combeau, Marie-Christine Bissery, Mari-Pierre Cherrier, Thomas Caulfield, Gilles Tiraboschi
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Patent number: RE38856Abstract: The invention provides a process by which ultra low salt content triiodinated aromatic compounds may be isolated from a highly acidic hot triiodination raction reaction medium in a straightforward fashion. The process involves increasing the pH to above 5 a value in the range of 3 to 7 with sodium hydroxide, addition of sodium bisulphite and/or sodium dithionite, addition of seed crystals, cooling slowly, and washing the collected precipitate with water.Type: GrantFiled: October 24, 2002Date of Patent: October 25, 2005Assignee: Amersham Health ASInventors: William Thielking, Einar Odd Ingvoldstad, Trygve Gulbrandsen
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Patent number: RE39682Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.Type: GrantFiled: March 30, 2005Date of Patent: June 5, 2007Assignee: Ramot at Tel Aviv University Ltd.Inventor: Yoel Kloog
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Patent number: RE40259Abstract: The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain.Type: GrantFiled: December 12, 1998Date of Patent: April 22, 2008Assignee: Newron Pharmaceuticals, S.p.A.Inventors: Paolo Pevarello, Mario Varasi, Patricia Salvati, Claes Post