Nitrogen In Substituent Q Patents (Class 564/163)
The substituent nitrogen is an amino nitrogen attached indirectly to a ring by acyclic nonionic bonding (Class 564/164)
Nitro in substituent q (Class 564/166)
Hydroxy, bonded directly to carbon, or ether in substituent q (h of -oh may be replaced by a substituted or unsubstituted ammonium ion or a group ia or iia light metal) (Class 564/167)
Ring in a substituent e (Class 564/168)
  • Non-racemic hexafluoreleucine, and methods of making and using it
    Publication number: 20040138493
    Abstract: 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: Application
    Filed: March 15, 2004
    Publication date: July 15, 2004
    Inventors: Alfio Fichera, Zihni Bilgicer, Krishna Kumar, Xuechao Xing
  • Heterocyclic selective androgen receptor modulators and methods of use thereof
    Publication number: 20040138244
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: October 14, 2003
    Publication date: July 15, 2004
    Inventors: James T. Dalton, Duane D. Miller
  • Aspartyl protease inhibitors
    Publication number: 20040132782
    Abstract: The present invention provides compounds having formula (I): 1
    Type: Application
    Filed: June 16, 2003
    Publication date: July 8, 2004
    Inventors: Wenjin Yang, Douglas R. Cary, Jeffrey W. Jacobs, Wanli Lu, Yafan Lu, Jian Sun, Min Zhong
  • Benzophenones as inhibitors of reverse transcriptase
    Publication number: 20040122064
    Abstract: The present invention is directed to benzophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.
    Type: Application
    Filed: February 5, 2004
    Publication date: June 24, 2004
    Inventor: Joseph Howing Chan
  • Antiangiogenic drug to treat cancer, arthritis and retinopathy
    Publication number: 20040110959
    Abstract: Compounds having Formula I 1
    Type: Application
    Filed: July 10, 2003
    Publication date: June 10, 2004
    Inventors: Megumi Kawai, Jack Henkin, George S. Sheppard, Richard A. Craig
  • Polyhaloalkylaryls
    Publication number: 20040092762
    Abstract: The present invention relates to polyhaloalkylaryls, to a process for preparing them and to the use of the polyhaloalkylaryls for preparing active ingredients.
    Type: Application
    Filed: November 7, 2003
    Publication date: May 13, 2004
    Inventors: Albrecht Marhold, Axel Pleschke
  • Anilino liver X-receptor modulators
    Publication number: 20040087632
    Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.
    Type: Application
    Filed: May 23, 2003
    Publication date: May 6, 2004
    Applicant: Pharmacia Corporation
    Inventors: Jennifer Ann Van Camp, James W. Malecha, Julie M. Miyashiro, Gary A. DeCrescenzo, Joe T. Collins, Monica J. Kalman
  • Inhibitors of IMPDH enzyme
    Publication number: 20040087650
    Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Application
    Filed: September 25, 2003
    Publication date: May 6, 2004
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jeffrey O. Saunders, Daniel Elbaum, Perry M. Novak, Douglas Naegele, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Catharine Frank, Dean P. Stamos, William Walters, David Pearlman
  • New carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
    Publication number: 20040077729
    Abstract: Carboxylic acid amides of general formula 1
    Type: Application
    Filed: July 21, 2003
    Publication date: April 22, 2004
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Uwe Ries, Henning Priepke, Wolfgang Wienen, Herbert Nar, Sandra Handschuh
  • NK1 antagonists
    Publication number: 20040072854
    Abstract: A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough: 1
    Type: Application
    Filed: March 12, 2003
    Publication date: April 15, 2004
    Applicant: Schering Corporation
    Inventors: Michelle Laci Wrobleski, Gregory A. Reichard, Neng-Yang Shih, Dong Xiao
  • Adamantane derivatives
    Patent number: 6720452
    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.
    Type: Grant
    Filed: June 10, 2002
    Date of Patent: April 13, 2004
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Mark Furber, Timothy Luker, Michael Mortimore, Philip Thorne
  • Quaternary amines and related inhibitors of factor xa
    Publication number: 20040067938
    Abstract: Novel quaternary amine containing compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.
    Type: Application
    Filed: November 3, 2003
    Publication date: April 8, 2004
    Inventors: Penglie Zhang, Robert M. Scarborough, Bing-Yan Zhu
  • Use of aryl N-substituted carboxamides directly and as radio-and chemosensitizers for killing tumor and cancer cells and novel compounds for such use
    Patent number: 6713517
    Abstract: Methods of killing tumor or cancer cells in human patients using an aryl N-substituted carboxamide having one or more aryl halo or one or more aromatic nitrogens, and/or acid addition salts thereof. The carboxamide may be an N-substituted nicotinamide or an N-substituted benzamide having such features, and may be used directly as a chemotherapeutic agent, or as a sensitizer for radiation or other chemotherapeutic agents. New compositions for such use include N-(2-diethylamino-ethyl)-4-amino-3-chlorobenzamide, N-(2-diethylamino-ethyl) nicotinamide, and their acid addition salts, e.g. hydrochlorides.
    Type: Grant
    Filed: February 27, 1997
    Date of Patent: March 30, 2004
    Assignee: OXiGENE, Inc.
    Inventors: Ronald W. Pero, Anders Olsson, Tomas Ekberg, Alan Schwartz, David Chaplin
  • Fluorescent group-containing carbodiimide compound precursor, fluorescent group-containing carbodiimide compound and methods for producing them
    Publication number: 20040059111
    Abstract: A novel fluorescent group-containing carbodiimide compound having at least one group selected from a carboxyl group, a sulfo group, a phosphono group and a phospho group which have substitution of an alkali metal, an alkaline earth metal or a basic group containing a nitrogen or phosphorus atom, which is prepared by using a novel fluorescent group-containing carbodiimide compound precursor having a halogen atom or a sulfonic acid group; and a method for detecting a nucleic acid by hybridization utilizing a nucleic acid labeled with a labeling substance, which utilizes the fluorescent group-containing carbodiimide compound as the labeling substance.
    Type: Application
    Filed: September 2, 2003
    Publication date: March 25, 2004
    Inventors: Naoki Kimura, Namiko Shiohata, Yoko Yoshikawa
  • Aminoguanidines and alkoxyguanidines as protease inhibitors
    Patent number: 6706765
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: February 6, 2003
    Date of Patent: March 16, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
  • 3-(2,5-diaminophenyl)-acrylamide derivatives and coloring agents containing said compounds
    Patent number: 6699990
    Abstract: The present patent application relates to 3-(2,5-diaminophenyl)acrylamide derivatives of general formula (I) or to physiologically tolerated, water-soluble-salts thereof and to agents containing said compounds and used for oxidative dyeing of fibers.
    Type: Grant
    Filed: October 21, 2002
    Date of Patent: March 2, 2004
    Assignee: Wella Aktiengesellschaft
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Photostable cationic organic sunscreen compounds with antioxidant properties and compositions obtained therefrom
    Patent number: 6699463
    Abstract: Compounds of Formula I Each R is independently linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy or one R is H and the other R is linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy; R1 is selected from the group consisting of COCH3, CO2R3, CONH2, CONH(R4)2, CN, COX(CH2)n-N—(R2)(R4)(R3), and the quaternized salt form of the formula COX(CH2)n-N—(R2)(R4)(R3)+Y−; X is O or NH; n is an integer of 1 to 5; Y is an anion; and R2, R3 and R4 are independently linear or branched C1 to C20. Hair care formulations and other compounds containing compounds of Formula I, and methods for protecting hair and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: March 2, 2004
    Assignee: EM Industries
    Inventor: Ratan K. Chaudhuri
  • Process for preparing &agr;-hydroxyamides and &agr;-ketoamides on a solid phase support
    Patent number: 6696605
    Abstract: The present invention relates to a process for preparing a &agr;-hydroxyamide or &agr;-ketoamide, said process comprising the steps of: a) reacting a resin which comprises a polymer-supported isocyanide with an aldehyde in the presence of a catalyst, to form a resin-bound &agr;-hydroxyamide; b) optionally reacting said resin-bound &agr;-hydroxyamide with a reagent which is capable of oxidizing said resin-bound &agr;-hydroxyamide to a resin-bound &agr;-ketoamide; and c) reacting said resin-bound &agr;-hydroxyamide or resin-bound &agr;-ketoamide with a reagent which cleaves the nitrogen-resin bond to form a &agr;-hydroxyamide &agr;-ketoamide.
    Type: Grant
    Filed: January 1, 2003
    Date of Patent: February 24, 2004
    Assignee: The Procter & Gamble Company
    Inventor: Jian Chen
  • Halogenated selective androgen receptor modulators and methods of use thereof
    Publication number: 20040029913
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: February 24, 2003
    Publication date: February 12, 2004
    Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
  • Intermediates of CETP inhibitors
    Patent number: 6689897
    Abstract: This invention relates to intermediates useful in the preparation of CETP inhibitors and methods of preparation thereof.
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: February 10, 2004
    Assignee: Pfizer Inc.
    Inventors: David B. Damon, Robert W. Dugger, Robert W. Scott
  • Aminediols for the treatment of Alzheimer's disease
    Publication number: 20040019086
    Abstract: The present invention relates to compounds of formula (I): 1
    Type: Application
    Filed: July 10, 2002
    Publication date: January 29, 2004
    Inventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
  • Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
    Publication number: 20040010020
    Abstract: A compound of Formula (IA) or Formula (IB) 1
    Type: Application
    Filed: May 28, 2003
    Publication date: January 15, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Thomas Martin Kirrane, Daniel Kuzmich, John Robert Proudfoot, David Thomson
  • Plasminogen activator inhibitor antagonists
    Patent number: 6677473
    Abstract: Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers, benzils, benzyl ethers, benzoate esters, sulfones and benzophenones are provided.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: January 13, 2004
    Assignee: Corvas International INC
    Inventors: Edwin L. Madison, Terence K. Brunck, Joseph Edward Semple, Marguerita Lim-Wilby, Kent E. Pryor, Ronald D. Lewis, II, David F. Duncan, C. Maxwell Lawrence
  • N-(4-substituted phenyl)-anthranilic acid hydroxamate esters
    Publication number: 20040006245
    Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: January 23, 2003
    Publication date: January 8, 2004
    Inventors: Gordon William Rewcastle, Julie Ann Spicer, Stephen Douglas Barrett, Michael David Kaufman, Jared Bruce John Milbank, Haile Tecle
  • N-(4-substituted phenyl)-anthranilic acid hydroxamate esters
    Publication number: 20030232889
    Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.
    Type: Application
    Filed: January 23, 2003
    Publication date: December 18, 2003
    Inventors: Stephen Douglas Barrett, Michael David Kaufman, Gordon William Rewcastle, Julie Ann Spicer
  • N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups, their preparation and their therapeutic uses
    Publication number: 20030225087
    Abstract: The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Application
    Filed: June 5, 2003
    Publication date: December 4, 2003
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Won-Yeob Kim, Kyung-Hwa Kim, Dennis W. Choi, Laura L. Dugan, Tae-Cheon Kang, Jae-Young Koh, Kyung-Mi Kim, In-Jae Shin
  • Inhibitors of IMPDH enzyme technical field of the invention
    Patent number: 6653309
    Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: November 25, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jeffrey O. Saunders, Daniel Elbaum, Perry M. Novak, Douglas Naegele, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Catharine Frank, Dean P. Stamos, William Walters, David Pearlman
  • Naphthylsulfonic acids and related compounds as glucose uptake agonists
    Patent number: 6653321
    Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: November 25, 2003
    Assignee: Telik, Inc.
    Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
  • Small molecule printing
    Publication number: 20030215876
    Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction.
    Type: Application
    Filed: February 20, 2003
    Publication date: November 20, 2003
    Inventors: Seung Bum Park, David Barnes-Seeman, Angela N. Koehler, Stuart L. Schreiber
  • Substituted alkylene diamine compounds
    Patent number: 6638970
    Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.
    Type: Grant
    Filed: February 22, 2001
    Date of Patent: October 28, 2003
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfaith Elzein, Jeff Zablocki, Tim Marquart
  • Guanidinobenzamides
    Patent number: 6638927
    Abstract: Compounds of formula IA and IB are new 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: Grant
    Filed: August 31, 2001
    Date of Patent: October 28, 2003
    Assignee: Chiron Corporation
    Inventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, Zhi-Jie Ni, David Duhl, Effie Tozzo, Kirk Johnson, David C. Myles
  • Retroviral protease inhibitors
    Publication number: 20030195227
    Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: September 18, 2002
    Publication date: October 16, 2003
    Applicant: Monsanto Company
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
  • New amphetamine derivatives, antibodies against them and pharmaceutical compositions containing them
    Publication number: 20030171435
    Abstract: Hapten-carrier conjugates capable of eliciting anti-hapten antibodies in vivo to amphetamines are disclosed. Methods of preparing the hapten-carrier conjugates and therapeutic compositions are also disclosed. A therapeutic composition containing the hapten-carrier conjugate is useful in the treatment of addiction to amphetamines. Passive immunization using antibodies raised against conjugates of the instant invention also is disclosed. The therapeutic composition is suitable for co-therapy with other conventional drugs for treatment of amphetamine abuse.
    Type: Application
    Filed: January 23, 2002
    Publication date: September 11, 2003
    Applicant: Drug Abuse Sciences, Inc.
    Inventors: Philippe Pouletty, Jacques Kusmierek, Frederic Koralewski, Herve Galons, Dominique Blanchard, Caroline Gadjou
  • Hydroxy alkyl amines
    Publication number: 20030166717
    Abstract: Disclosed are compounds of formula X, 1
    Type: Application
    Filed: May 31, 2002
    Publication date: September 4, 2003
    Inventors: John Freskos, David L. Brown, Yvette M. Fobian, Larry Fang, Arthur Glenn Romero, Varghese John
  • Intermediate for preparing midodrine
    Patent number: 6610886
    Abstract: The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2′,5′-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula (5), wherein Ar and Ar′ are aryl groups.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: August 26, 2003
    Assignee: Chemagis Ltd.
    Inventors: Michael Brand, Ronit Chen, Deby Yigal, Joseph Kaspi
  • Alkyl urea retinoid agonists
    Publication number: 20030158226
    Abstract: 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: Application
    Filed: September 17, 2002
    Publication date: August 21, 2003
    Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLC
    Inventors: Paula Nanette Belloni, Denis John Kertesz, Michael Klaus, Jean-Marc Lapierre
  • Process for solid supported synthesis of pyruvate-derived compounds
    Patent number: 6608196
    Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: August 19, 2003
    Assignee: Galileo Pharmaceuticals, Inc.
    Inventors: Bing Wang, Satyanarayana Janagani, Wyeth B. Callaway, Jonathan L. Sessler
  • 1,3-Diarylprop-2-en-1-ones, compositions containing them and use thereof
    Publication number: 20030153611
    Abstract: 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: Application
    Filed: December 4, 2002
    Publication date: August 14, 2003
    Applicant: AVENTIS PHARMA S.A.
    Inventors: Patrick Mailliet, Cacile Combeau, Marie-Christine Bissery, Thomas Caulfield, Gilles Tiraboschi, Marie-Pierre Cherrier
  • Substituted urea retinoid agonists
    Publication number: 20030125383
    Abstract: 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: Application
    Filed: September 17, 2002
    Publication date: July 3, 2003
    Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLC
    Inventors: Michael Klaus, Jean-Marc Lapierre
  • Azomethine yellow dye compound
    Publication number: 20030125556
    Abstract: A azomethine yellow dye compound of general formula (I):
    Type: Application
    Filed: September 26, 2002
    Publication date: July 3, 2003
    Inventors: Kiyoshi Takeuchi, Shigeki Uehira
  • Novel aminobenzoephenones
    Publication number: 20030119902
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Application
    Filed: August 28, 2002
    Publication date: June 26, 2003
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Process to prepare (2S)-2-(dipropylamino)-6-ethoxy-2,3-dihydro-1H-indene-5-carboxamide
    Patent number: 6576769
    Abstract: The present invention is a process, including intermediates, to produce (2S)-2-dipropylamino)-6-ethoxy-2,3-dihydro-1H-indene-5-carboxamide which is a useful pharmaceutical agent.
    Type: Grant
    Filed: June 6, 2002
    Date of Patent: June 10, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: Jiong Jack Chen, Arthur Glenn Romero, Styrbjorn Bystrom
  • Method for the preparation of enantiomerically enriched compounds
    Publication number: 20030097005
    Abstract: Process for the preparation of a diasteromerically enriched phenylglycine amide derivative in which an enantomerically enriched phenylglycine amide is converted into the corresponding Schiff base with the aid of compound R2—C(O)—R3, and the Schiff base obtained is subsequently converted into the diastereomerically enriched phenyglycine amide derivative with the aid of a cyanide source, a reducing agent or an allyl organometallic compound. The phenylglycine amide derivatives obtained are interesting starting materials for the preparation of for example enantimerically enriched &agr;- and or &bgr;-amino acids and derivatives thereof, such as amides and esters, and amines.
    Type: Application
    Filed: October 9, 2002
    Publication date: May 22, 2003
    Inventors: Wilhelmus Hubertus Joseph Boesten, Harold Monro Moody, Bernardus Kaptein, Johannes Paulus Gerardus Seerden, Marcelles Van Der Sluis, Ben Lange De, Quirinus Bernardus Broxterman
  • Amine reaction compounds comprising one or more active ingredient
    Patent number: 6566312
    Abstract: The present invention relates to a product of reaction between a primary and/or secondary amine and one or more active ingredients. By the present invention, there is provided a release of the active component over a longer period of time than by the use of the active itself.
    Type: Grant
    Filed: May 29, 2002
    Date of Patent: May 20, 2003
    Assignee: Procter & Gamble Company
    Inventors: Jean-Luc Philippe Bettiol, Alfred Busch, Hugo Denutte, Christophe Laudamiel, Peter Marie Kamiel Perneel, Marie Montserrat Sanchez-Pena, Johan Smets
  • Process for preparing resorcinol derivatives
    Publication number: 20030088113
    Abstract: The present invention relates to an improved process for preparing 4-substituted resorcinol derivatives, and intermediate compounds useful in the preparation of such resorcinol derivatives.
    Type: Application
    Filed: October 28, 2002
    Publication date: May 8, 2003
    Inventors: Stuart Edward Bradley, John Kitchin, Graham Michael Wynne
  • Oxime derivatives for the treatment of dyslipidemia and hypercholesteremia
    Publication number: 20030083357
    Abstract: The present invention relates to compounds of Formula (I) which may be useful in the treatment of diseases, such as, metabolic disorders, dyslipidemia and/or hyperchloesterolemia: 1
    Type: Application
    Filed: August 19, 2002
    Publication date: May 1, 2003
    Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma
  • Method for preparing substituted 4-phenyl-4-cyanocylohexanoic acids
    Publication number: 20030083507
    Abstract: This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carbosyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and water.
    Type: Application
    Filed: October 9, 2002
    Publication date: May 1, 2003
    Applicant: SmithKline Beecham Corporation
    Inventors: Kevin Webb, Wilford Mendelson, Jianhao Chen
  • Fungicidal compounds having a fluorovinyl-or fluoropropenyl-oxyphenyloxime moiety and process for the preparation thereof
    Patent number: 6552080
    Abstract: A fungicidal compound of formula (I) having a fluorovinye- or fluoropropenyl-oxyphenyloxime moiety and stereoisomers thereof are useful for protecting crops from fungal diseases: wherein, X is CH or N; Y is O or NH; R1 is hydrogen, C1-4 alkyl, or halogen-substituted C1-4 alkyl, R2 is a phenyl group optionally carrying one or more substituents selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, methylenedioxy and halogen; or a naphthyl group; and R3 is hydrogen or CF3.
    Type: Grant
    Filed: February 7, 2002
    Date of Patent: April 22, 2003
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Bum Tae Kim, No Kyun Park, Gyung Ja Choi, Jin Cheol Kim, Chwang Siek Pak
  • Calcium channel blockers
    Publication number: 20030060632
    Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.
    Type: Application
    Filed: September 23, 2002
    Publication date: March 27, 2003
    Inventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
  • Thiourea and benzamide compounds, compositions and methods of treating or preventing inflammatory diseases and atherosclerosis
    Patent number: 6528528
    Abstract: The present invention provides compounds of Formula I shown below. The present invention also provides methods of treating or preventing 3 inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of Formula I.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: March 4, 2003
    Assignee: Warner-Lambert Company
    Inventors: David Thomas Connor, William Howard Roark, Karen Elaine Sexton, Roderick Joseph Sorenson