Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
Type:
Grant
Filed:
August 17, 2000
Date of Patent:
February 21, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel
Abstract: Compounds which are 2-ureido-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group optionally further substituted, selected from: i) straight or branched C1-C6 alkyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C6 alkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R2 is hydrogen, a straight or branched C1-C6 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom so which they are bonded, R1 and R2 form a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptab
Type:
Grant
Filed:
October 27, 1999
Date of Patent:
March 8, 2005
Assignee:
Pharmacia & Upjohn S.p.A.
Inventors:
Paolo Pevarello, Raffaella Amici, Gabriella Traquandi, Manuela Villa, Anna Vulpetti, Antonella Isacchi
Abstract: Novel benzothiazoles and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.
Type:
Grant
Filed:
October 26, 2001
Date of Patent:
November 30, 2004
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Jagabandhu Das, Joel C. Barrish, John Wityak
Abstract: Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline compounds are also included.
Type:
Grant
Filed:
March 30, 2001
Date of Patent:
November 16, 2004
Assignees:
Paratek Pharmaceuticals, Inc., Trustees of Tufts College
Inventors:
Mark L. Nelson, Stuart B. Levy, Roger Frechette, Todd E. Bowser, Mohamed Y. Ismail
Abstract: Disclosed are compounds of the formula:
wherein
R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may together form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents;
and the pharmaceutically acceptable addition salts thereof,
which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
Type:
Grant
Filed:
March 18, 2002
Date of Patent:
September 28, 2004
Assignee:
Neurogen Corporation
Inventors:
Andrew Thurkauf, Raymond F. Horvath, Jun Yuan, John M. Peterson
Abstract: In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated coupling of proteins, lipids, nucleic acids, and other biomaterials, and any combination thereof. In another embodiment, the compositions and associated methods have utility in vivo to reduce the deleterious effects of sugar-mediated coupling processes in an organism, when the organism is exposed to the compound or composition internally, by ingestion, transdermal application, or other means. In yet another embodiment, the compositions and associated methods are useful for the ex-vivo treatment of organs, cells and tissues and external treatment of hair, nails and skin to rejuvenate them by changing deformability and increase the tissue diffusion coefficient. In a further embodiment, the present invention relates to novel compounds and pharmaceutical compositions.
Type:
Grant
Filed:
February 7, 2002
Date of Patent:
August 17, 2004
Inventors:
Peter C Ulrich, Sheng Ding Fang, Michael L Brines, Qiao-Wen Xie, Anthony Cerami
Abstract: The present invention relates to the use of 4-hydroxyisothiazole compounds as antimicrobially active substances, certain new 4-hydroxyisothiazole compounds and a process for their preparation.
Type:
Grant
Filed:
October 3, 2001
Date of Patent:
July 6, 2004
Assignee:
Ciba Specialty Chemicals Corporation
Inventors:
Werner Hölzl, Wolfgang Haap, Dietmar Ochs, Karin Puchtler, Marcel Schnyder, Dinesh Narendra Rele, Sitaram Pal, Asawari Bhikaji Mahtre, Surendra Umesh Kulkarni, Arakali Srinivasarao Radhakrishna
Abstract: A compound selected from those of formula (I):
wherein R1a, R1b, R2, R3, are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of phosphosdiesterase-7 (PDE-7).
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
June 22, 2004
Assignee:
Warner-Lambert Company LLC
Inventors:
Fabrice Vergne, Patrick Bernardelli, Edwige Lorthiois, Pierre Ducrot
Abstract: Process for making 5FVN, comprising contacting in a reactor 3PN with CO and hydrogen in the presence of a catalyst, the catalyst comprising recycled catalyst that is reactivated using hydrogen.
Type:
Grant
Filed:
March 12, 2002
Date of Patent:
June 15, 2004
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
Emilio E. Bunel, Marisa Bonilla, Ronnie Ozer
Abstract: A novel antirheumatic agent comprising as an active ingredient a compound of formula I:
or a pharmaceutically acceptable salt or hydrate thereof.
Abstract: Compounds of Formula (1) and processes for their preparation, their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation wherein Q, X1, X2, X3, R1, R2, R6 and R7 are as defined in the disclosure. Also disclosed are novel intermediates of Formula (5), Formula (8) and Formula (20) wherein R27 is —(CR6R7)q—Q; R6, R7, q, Q, X1 and X2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula (1).
Type:
Grant
Filed:
June 29, 2001
Date of Patent:
May 18, 2004
Assignee:
The Regents of the University of California
Inventors:
Gary David Annis, George Chih-Shu Chiang, David Raymond Forney, Kanu Maganbhai Patel, Morris Padgett Rorer, William Francis Smith, III, Thomas Martin Stevenson, King-Mo Sun, Chi-Ping Tseng
Abstract: Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolyzable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1-10C)alkyl or R14C(O)O(1-6C)alkyl wherein R14 is optionally substituted (1-10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
Abstract: Provided are chromophores of the formula
Q—(—L—Z)x,
wherein x is 2 or 3, wherein Q is selected from the group consisting of
wherein L is
wherein R is an alkyl group having 1 to 20 carbon atoms, and wherein Z is selected from the group consisting of
Type:
Grant
Filed:
June 13, 2002
Date of Patent:
May 4, 2004
Assignee:
The United States of America as represented by the Secretary
of the Air Force
Inventors:
Ramamurthi Kannan, Loon-Seng Tan, Bruce A. Reinhardt, Richard A. Vaia
Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
September 9, 2002
Date of Patent:
April 27, 2004
Assignee:
G.D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: Compounds, compositions and methods are provided that are useful in the treatment and prevention of certain viral infections and associated diseases. In particular, the compounds of the invention inhibit the activity of a viral RNA polymerase. The subject methods are particularly useful in the treatment of diseases causes by hepatitis C virus infection.
Abstract: Disclosed are the compounds of formula I
wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
Type:
Grant
Filed:
July 23, 2002
Date of Patent:
April 27, 2004
Assignee:
Novartis AG
Inventors:
Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer
Abstract: A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided in which the carboxylic acid group of 5-methylisoxazole-4-carboxylic acid is chlorinated, forming 5-methylisoxazole-4-carboxylic acid chloride. The acid chloride is then reacted without intermediate distillation with 4-trifluoromethylaniline in the presence of an alkali metal or alkaline-earth metal bicarbonate acid scavenger.
Abstract: The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical or veterinary compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
Abstract: The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by formula I:
wherein:
Q is selected from the group consisting of
M is O, NR9, or CR10R11; X is O or NH; and the R groups are as defined, and therapeutic compositions containing them alone or in combination with other therapeutic agents useful in the treatment of cancer or other proliferative diseases.
Abstract: The invention relates to compounds of Formula (I) wherein R1, (R2)v, R3 and n are defined in the specification and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
April 6, 2004
Assignee:
Wyeth Holdings Corporation
Inventors:
Edward James Salaski, Semiramis Ayral-Kaloustian, Joseph William Epstein