Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/335.5)
  • Publication number: 20070167506
    Abstract: This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
    Type: Application
    Filed: January 4, 2007
    Publication date: July 19, 2007
    Applicant: PFIZER INC.
    Inventors: NATHAN ANTHONY LOGAN CHUBB, MARK ROGER COX, JEROME SEBASTIEN DAUVERGNE, RICHARD ANDREW EWIN, CHRISTELLE LAURET
  • Patent number: 7220914
    Abstract: Zwitterionic compounds, photovoltaic cell charge carrier layers containing such compounds, photovoltaic cells including such charge carrier layers, and related methods are disclosed.
    Type: Grant
    Filed: November 30, 2004
    Date of Patent: May 22, 2007
    Assignee: Konarka Technologies, Inc.
    Inventors: Kethinni G. Chittibabu, Savvas Hadjikyriacou, David Waller
  • Patent number: 7202383
    Abstract: There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R1, R2 and R3 are each independently selected from OH, C1-6alkyl, OC1-6alkyl, OC(O)C1-6alkyl, C(O)OC1-6alkyl, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), C(O)NHC1-6alkyl, C(O)N(C1-6alkyl)(C1-6alkyl), SH, SC1-6alkyl, NO2, CF3, OCF3 and halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1–4 substituents independently selected from OH, C1-6alkyl, C1-6alkoxy, C1-3alkylenedioxy, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6)(C1-6alkyl), SH, S—C1-6alkyl, NO2, CF3, OCF3 and halogen. The compounds of Formula I are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.
    Type: Grant
    Filed: September 14, 2004
    Date of Patent: April 10, 2007
    Assignee: The Hospital For Sick Children
    Inventors: Chaim Roifman, Peter Demin, Olga Rounova, Tom Grunberger
  • Patent number: 7202263
    Abstract: N-Heterocyclic derivatives of the following formula: where m, n, p, A1, R1, R2, R3 and R4 are described herein, as well as other N-heterocyclic derivatives, are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: April 10, 2007
    Assignee: Schering Aktiengesellschaft
    Inventors: David Davey, Raju Mohan, Gary Phillips, Guo Ping Wei, Wei Xu
  • Patent number: 7192975
    Abstract: Compounds of the formula wherein the substituents are as defined in the specification which are useful for the treatment of pain.
    Type: Grant
    Filed: July 24, 2003
    Date of Patent: March 20, 2007
    Assignee: Societe de Conseils de Recherches Et d''Applications Scientifiques (S.C.R.A.S.)
    Inventors: Dennis Bigg, Anne-Marie Liberatore, Pierre-Etienne Chabrier De Lassauniere
  • Patent number: 7192453
    Abstract: The present invention relates to a method of coloring keratin-containing fibres, especially human hair, in which method a compound of formula (I), wherein R is hydroxy or NHR1, R1 being hydrogen or C1–C4alkyl, and B is an aromatic or heterocyclic ring, is diazotised, and the resulting diazonium salt is applied at a pH of from 2 to 5 to the material being colored and then, by means of increasing the pH to from 7 to 12, is fixed on the material in the form of an oligomeric or polymeric colorant
    Type: Grant
    Filed: October 8, 2002
    Date of Patent: March 20, 2007
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Jean-Marie Adam, Taher Yousaf
  • Patent number: 7183279
    Abstract: The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activities.
    Type: Grant
    Filed: May 25, 2006
    Date of Patent: February 27, 2007
    Assignee: University of Ottawa
    Inventors: Simon Lemaire, Irma Bernatchez-Lemaire, Hoang-Thanh Le
  • Patent number: 7169797
    Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: January 30, 2007
    Assignee: Abbott Laboratories
    Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
  • Patent number: 7115646
    Abstract: The present application describes cyclic diamino compounds, derivatives thereof, and pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: October 6, 2004
    Date of Patent: October 3, 2006
    Assignee: Bristol Myers Squibb, Co.
    Inventor: Jennifer X. Qiao
  • Patent number: 7074786
    Abstract: The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activities.
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: July 11, 2006
    Assignee: University of Ottawa
    Inventors: Simon Lemaire, Irma Bernatchez-Lemaire, Hoang-Thanh Le
  • Patent number: 7030239
    Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: May 18, 2004
    Date of Patent: April 18, 2006
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
  • Patent number: 6989399
    Abstract: A series of N-alkanol-N-phenyl benzenesulfonamide and related derivatives of the Formula I are disclosed, wherein R1, R2, R3, X, and Y are defined herein. The compounds are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extracellular deposition of amyloid. Pharmaceutical compositions and methods of treatment are also disclosed.
    Type: Grant
    Filed: July 24, 2003
    Date of Patent: January 24, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: David W. Smith, Michael F. Parker
  • Patent number: 6972299
    Abstract: This invention relates to a compound and the use of the compound of the formula wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH?CH— or —C?C—; and B signifies wherein R6 to R26, X and Y are as defined in the specification or a pharmaceutically acceptable salt thereof, for use in pharmaceutical compositions for the treatment or prevention of mGluR5 receptor mediated disorders.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: December 6, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
  • Patent number: 6972287
    Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: December 6, 2005
    Assignee: Pfizer Inc.
    Inventors: Corinne Elizabeth Augelli-Szafran, Mark Robert Barvian, Christopher Franklin Bigge, Shelly Ann Glase, Shunichiro Hachiya, John Steven Kiely, Takenori Kimura, Yingjie Lai, Annette Theresa Sakkab, Mark James Suto, Larry Craswell Walker, Tomoyuki Yasunaga, Nian Zhuang
  • Patent number: 6969728
    Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.
    Type: Grant
    Filed: May 10, 2001
    Date of Patent: November 29, 2005
    Assignee: Genzyme Corporation
    Inventors: Scott F. Sneddon, John L. Kane, Bradford H. Hirth, Fred Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
  • Patent number: 6965036
    Abstract: The present application describes intermediates for nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D—E represent guanidine mimics, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: June 24, 2003
    Date of Patent: November 15, 2005
    Inventors: Mimi L. Quan, Renhua Li
  • Patent number: 6960600
    Abstract: The invention concerns novel azole or triazole derivatives of formula (I), wherein: X, Ar1, Ar3, A, R1, R5, R6, R7 and B are such as defined in the description, their preparation method and their use as antifungal medicines.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: November 1, 2005
    Assignee: Aventis Pharma S.A.
    Inventors: Didier Babin, John Bernard Weston
  • Patent number: 6946460
    Abstract: The invention concerns novel azole or triazole derivatives of formula (I), wherein X, Ar1, Ar2, Ar3, A, B, and R1 are as defined herein, their preparation method and their use as fungicides.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: September 20, 2005
    Assignee: Aventis Pharma S.A.
    Inventors: Didier Babin, John Bernard Weston
  • Patent number: 6936627
    Abstract: The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase and/or at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent.
    Type: Grant
    Filed: October 29, 2002
    Date of Patent: August 30, 2005
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, Chia-En Lin, Tiansheng Wang
  • Patent number: 6933390
    Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.
    Type: Grant
    Filed: July 15, 2004
    Date of Patent: August 23, 2005
    Assignee: Warner-Lambert Company
    Inventors: Hubert Barth, Klaus Steiner, Simon Schneider, Ulrich Bayer, Manfred Westermayer, Ulrike Wolfsperger, Hans-Jürgen Betche
  • Patent number: 6900161
    Abstract: The invention concerns novel azole or triazole derivatives of formula (Ia) or (Ib), wherein: X, Ar1, Ar2, Ar3, A, B and R1 are such as defined in the description, the method for preparing same and their use as fungicides.
    Type: Grant
    Filed: January 9, 2004
    Date of Patent: May 31, 2005
    Assignee: Aventis Pharma S.A.
    Inventors: Didier Babin, John Bernard Weston
  • Patent number: 6887877
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.
    Type: Grant
    Filed: June 11, 2002
    Date of Patent: May 3, 2005
    Assignee: ViroChem Pharma Inc.
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Stephen Joseph Shuttleworth, Mohammad Arshad Siddiqui, Wuyi Wang
  • Patent number: 6884821
    Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: April 26, 2005
    Assignee: Eisai Co., Ltd.
    Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
  • Patent number: 6881754
    Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: April 19, 2005
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
  • Patent number: 6875884
    Abstract: Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: April 5, 2005
    Assignee: Kirin Beer Kabushiki Kaisha
    Inventors: Janak Padia, Michael Hocker, Tsuyoshi Nishitoba, Hirohi Ohashi, Eiji Sawa
  • Patent number: 6849634
    Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
    Type: Grant
    Filed: December 7, 2001
    Date of Patent: February 1, 2005
    Assignee: ICAgen
    Inventors: Serge Beaudoin, Aimee D. Reed, Michael F. Gross
  • Patent number: 6838561
    Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): where R1, and R2 are each individually selected from a hydrogen atom, a C1 to C3 alkyl group, a C1 to C5 mono or dihydroxyalkyl group; phenyl or benzyl optionally substituted with an alkoxy group, or R1 and R2 together with the nitrogen atom to which they are attached form a piperazine, piperidine, imidazole, or morpholine ring.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: January 4, 2005
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan
  • Publication number: 20040214870
    Abstract: The present invention is directed to compounds of formula (I), 1
    Type: Application
    Filed: February 4, 2004
    Publication date: October 28, 2004
    Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
  • Publication number: 20040210064
    Abstract: A production method of an optically active &bgr;-amino acid represented by the formula (I) 1
    Type: Application
    Filed: January 29, 2004
    Publication date: October 21, 2004
    Applicant: Ajinomoto Co., Inc.
    Inventor: Kiyoshi Tomioka
  • Publication number: 20040204410
    Abstract: The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.
    Type: Application
    Filed: April 28, 2004
    Publication date: October 14, 2004
    Inventors: Norman Kong, Emily Aijun Liu, Binh Thanh Vu
  • Publication number: 20040198795
    Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise substituted imidazolium compounds capable of inhibiting the formation of, as well as reversing already formed, advanced glycosylation endproducts of target proteins. 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.
    Type: Application
    Filed: April 20, 2004
    Publication date: October 7, 2004
    Inventors: Dilip R. Wagle, San-Bao Hwang, Veronica M. Mallon, Sara Vasan, John J. Egan, Peter Ulrich, Anthony Cerami
  • Patent number: 6800097
    Abstract: The oxidation hair dye precursor composition contains from 0.005 to 20.0 percent by weight of at least one coupler compound and from 0.005 to 20.0 percent by weight of at least one developer compound, which includes at least one substituted 2-aminoalkyl-1,4-diaminobenzene compound of the formula (I): New substituted 2-aminoalkyl-1,4-diaminobenzene compound of formula (I) are also described.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: October 5, 2004
    Assignee: Wella Aktiengesellschaft
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Publication number: 20040192928
    Abstract: The invention concerns novel compounds of the family of 3-Alkyl-(4,5 diphenyl-imidazol-1-yl), their synthesis method and cosmetic, hygienic or pharmaceutical compositions containing them. The invention also concerns the use, in a physiologically acceptable medium, in or for preparing a soothing composition, of at least a compound of the family of 3-Alkyl-(4,5 diphenyl-imidazol-1-yl). The invention further concerns the use, in a physiologically acceptable medium, in or for producing a composition, of at least a compound of the family of 3-Alkyl-(4,5 diphenyl-imidazol-1-yl), the compound or the composition being designed to soothe skin troubles such as sensitive skins, discomfort, gnawing, itching, irritations, red spots, heat and/or flush sensations, advantageously sensitive and/or irritable and/or reactive and/or allergic symptoms of the skin and/or the scalp and/or mucosa.
    Type: Application
    Filed: May 4, 2004
    Publication date: September 30, 2004
    Inventors: Jean-Baptiste Galey, Maria Dalko, Yann Mahe, Jacqueline Dumats
  • Publication number: 20040186151
    Abstract: This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.
    Type: Application
    Filed: February 12, 2004
    Publication date: September 23, 2004
    Inventors: Adnan M.M. Mjalli, Robert C. Andrews, Ravindra R. Yarragunta, Rongyuan Xie, Tan Ren, Govindan Subramanian, James C. Quada
  • Publication number: 20040171616
    Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Application
    Filed: February 19, 2003
    Publication date: September 2, 2004
    Inventors: Michael S. South, John J. Parlow
  • Publication number: 20040167129
    Abstract: The present invention relates to compounds of formula (I) 1
    Type: Application
    Filed: December 22, 2003
    Publication date: August 26, 2004
    Inventors: Alexander Mayweg, Hans Peter Marty, Werner Mueller, Robert Narquizian, Werner Neidhart, Philippe Pflieger, Stephan Roever
  • Patent number: 6780998
    Abstract: The oxidation hair dye precursor composition contains from 0.005 to 20.0 percent by weight of one or more coupler compounds and from 0.005 to 20.0 percent by weight of one or more developer compounds. The one or more developer compounds include at least one substituted 2-aminoalkyl-1,4-diaminobenzene compound of the formula (I): New substituted 2-aminoalkyl-1,4-diaminobenzene compounds of formula (I) are described.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: August 24, 2004
    Assignee: Wella Aktiengesellschaft
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Patent number: 6780999
    Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): where R1 and R2 are each individually selected from a hydrogen atom, a C1 to C3 alkyl group, a C1 to C5 mono or dihydroxyalkyl group; phenyl or benzyl optionally substituted with an alkoxy group, or R1 and R2 together with the nitrogen atom to which they are attached form a piperazine, piperidine, imidazole, or morpholine ring.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: August 24, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan
  • Publication number: 20040162328
    Abstract: The invention concerns novel compounds of the family of 3-Alkyl-(4,5 diphenyl-imidazol-1-yl), their synthesis method and cosmetic, hygienic or pharmaceutical compositions containing them The invention also concerns the use, in a physiologically acceptable medium, in or for preparing a soothing composition, of at least a compound of the family of 3-Alkyl-(4,5 diphenyl-imidazol-1-yl). The invention further concerns the use, in a physiologically acceptable medium, in or for preparing a composition, a compound of the family of 3-Alkyl-(4,5 diphenyl-imidazol-1-yl), the compound and the composition being designed for soothing skin troubles such as sensitive skins, discomfort, gnawing, itching, irritations, red spots, heat and/or flush sensations, advantageously sensitive and/or irritable and/or reactive and/or allergic symptoms of the skin and/or the scalp and/or mucosa.
    Type: Application
    Filed: April 8, 2004
    Publication date: August 19, 2004
    Inventors: Jean-Baptiste Galey, Yann Mahe, Maria Dalko, Jacqueline Dumats
  • Publication number: 20040147559
    Abstract: There are disclosed compounds of the formula 1
    Type: Application
    Filed: July 30, 2003
    Publication date: July 29, 2004
    Applicant: Schering Corporation and Pharmacopeia, Inc.
    Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Laura L. Rokosz, James P. Jakway, Gaifa Lai, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
  • Publication number: 20040127524
    Abstract: Hydroxamic acids having the formula 1
    Type: Application
    Filed: December 19, 2003
    Publication date: July 1, 2004
    Applicant: Wyeth Holdings Corporation
    Inventors: Jeremy Ian Levin, Mila Ti Du
  • Publication number: 20040122225
    Abstract: Nitrone derivatives are efficiently prepared by increasing reagent concentrations in reaction solutions. Aldehydes and amines may be condensed to prepare an imine intermediate. Elimination of the solution media generally renders the imine formation more efficient. The imine is then reacted with a peroxysulfate oxidizing agent in a solution having at least about 0.1M concentration of the imine. The oxaziridine is rearranged to produce the nitrone derivative in high yield and good purity.
    Type: Application
    Filed: December 20, 2002
    Publication date: June 24, 2004
    Applicant: The Goodyear Tire & Rubber Company
    Inventor: Dane Kenton Parker
  • Publication number: 20040116424
    Abstract: The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula 1
    Type: Application
    Filed: March 28, 2003
    Publication date: June 17, 2004
    Applicant: Neurogen Corporation
    Inventors: George P. Luke, George D. Maynard, Scott Mitchell, Andrew Thurkauf, Linghong Xie, LuYan Zhang, Suoming Zhang, He Zhao, Bertrand L. Chenard, Yang Gao, Bingsong Han, Xiao Shu He
  • Publication number: 20040110804
    Abstract: The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds.
    Type: Application
    Filed: July 9, 2003
    Publication date: June 10, 2004
    Inventors: Michael A. Walker, Zhuping Ma, B. Narasimhulu Naidu, Margaret E. Sorenson, Annapurna Pendri, Jacques Banville, Serge Plamondon, Roger Remillard
  • Patent number: 6747047
    Abstract: This invention provides compounds of Formula (1), their N-oxides and agriculturally suitable salts wherein A, B, J, R1, R2, R3 and R4 and n are as defined in the disclosure. Also disclosed are methods for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula (1) and compositions containing the compounds of Formula (1).
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: June 8, 2004
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George P. Lahm, Brian J. Myers, Thomas P. Selby, Thomas M. Stevenson
  • Publication number: 20040106802
    Abstract: The invention discloses a novel series of compound represented by general formula (I), 1
    Type: Application
    Filed: November 26, 2003
    Publication date: June 3, 2004
    Applicant: TORRENT PHARMACEUTICALS LTD.
    Inventor: Alangudi Sankaranarayanan
  • Patent number: 6737418
    Abstract: This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: May 18, 2004
    Assignee: Euro-Celtique S.A.
    Inventors: Derk Hogenkamp, Ravindra Upasani, Phong Nguyen
  • Patent number: 6737423
    Abstract: Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (I a), wherein Rn, Het, A, B and T have the meanings given in the claims. These compounds have a variety of uses. They can be used as antihypertensives, for the reduction or prevention of is chemically induced damage, as pharmaceuticals for surgical interventions, for the treatment of ischemia of the nervous system, including stroke and cerebral edema, for the treatment of ischemia due to shock and disturbed respiratory drive, for the treatment of snoring, as a laxative, as an agent against ectoparasites, for the prevention of gallstone formation, as an antiatherosclerotic, as an agent against diabetic late complications, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophy, and organ hyperplasia.
    Type: Grant
    Filed: December 18, 2001
    Date of Patent: May 18, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Hans-Willi Jansen
  • Publication number: 20040082577
    Abstract: Amino methyl imidazoles of Formula I are provided: 1
    Type: Application
    Filed: August 21, 2003
    Publication date: April 29, 2004
    Applicant: Neurogen Corporation
    Inventors: Andrew Thurkauf, He Zhao, Suoming Zhang, Yang Gao
  • Patent number: 6723743
    Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at
    Type: Grant
    Filed: September 28, 2000
    Date of Patent: April 20, 2004
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, Xiao-shu He, He Zhao, John Peterson, Xiaoyan Zhang, Robbin Brodbeck, James Krause, George Maynard, Alan Hutchison