Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
Type:
Grant
Filed:
July 21, 2003
Date of Patent:
March 28, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer, Hidenori Takahashi, Thomas A. Gilmore, Rajiv Sharma
Abstract: The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.
Type:
Grant
Filed:
June 4, 2002
Date of Patent:
January 3, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Eugene R. Hickey, Younes Bekkali, Usha R. Patel, Denice Mary Spero, David S. Thomson, Erick Richard Roush Young
Abstract: Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
Abstract: A novel family of amine azides having a cyclic structure therein is disclosed. These compounds have attractive properties as rocket propellants.
Type:
Grant
Filed:
March 18, 2003
Date of Patent:
November 8, 2005
Assignee:
The United States of America as represented by the Secretary of the Army
Abstract: The present invention relates to aliphatic compounds of the formula I, or stereoisomers thereof, or their pharmaceutically acceptable salts: wherein A represents an optionally substituted CH3CnH(2n-2m)— (wherein n denotes an integer of 4 to 22, and m represents an unsaturation number which is an integer of 0 to 7), l represents an integer of 0 to 10, s represents 0 or 1, provided that when s is 0, p+q=4 or 5, but when s is 1, p+q=3 or 4, and in each case, either p or q is an integer of 1 or more, R represents an alkyl group having 1 to 10 carbon atoms which may be straight-chain or branched-chain, and RA represents hydrogen or an alkyl group having 1 to 10 carbon atoms which may be straight-chain or branched-chain, and their use in suppression of platelet aggregation, in suppression of inflammation, and in prevention and treatment of circulatory diseases.
Abstract: Novel pyrrolidinyl-substituted para-phenylenediamine derivatives comprising a cationic radical, the dye compositions comprising them and the process for dyeing keratin fibers using these compositions, making it possible to obtain a chromatic, powerful, unselective and fast coloration of keratin fibers.
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
September 20, 2005
Assignee:
L'Oreal S.A.
Inventors:
Stéphane Sabelle, Laure Ramos, Madeleine Leduc, Michel Philippe
Abstract: The invention relates to certain novel compounds having Vanilloid Receptor (VR1) antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.
Type:
Grant
Filed:
May 2, 2002
Date of Patent:
September 6, 2005
Assignee:
SmithKline Beecham, PLC
Inventors:
Harshad Kantilal Rami, Mervyn Thompson, Paul Adrian Wyman
Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNF? and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNF? and/or one or more other involved cytokines, alone or in combination with other agents.
Type:
Grant
Filed:
May 23, 2003
Date of Patent:
July 19, 2005
Assignee:
Mediquest Therapeutics, Inc.
Inventors:
Mark R. Burns, Maralee McVean, Kevin J. Kennedy, Arthur Yeung, Bruce H. Devens
Abstract: The invention provides compounds of general formula (I) wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
June 14, 2001
Date of Patent:
June 28, 2005
Assignee:
Astra Zeneca
Inventors:
Tomas Eriksson, Tomas Klingstedt, Tesfaledet Mussie
Abstract: A method for stereochemically controlled production of azacyclic compounds of general formula (I) in which the substituents have the meanings given in the specification. The invention also relates to intermediate products of this method and to novel azacyclenes.
Type:
Grant
Filed:
May 10, 1999
Date of Patent:
May 31, 2005
Assignee:
Solvay Pharmaceuticals GmbH
Inventors:
Michael Reggelin, Timo Heinrich, Bernd Junker, Jochen Antel, Ulf Preuschoff
Abstract: The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula wherein R1 signifies hydrogen or an amino protecting group; Z signifies hydrogen or an amino protecting group; and * represents a center of chirality. 3-Amino-pyrrolidine derivatives, especially optically active 3-amino-pyrrolidine derivatives, are intermediates for the production of agrochemicals and of pharmaceutically active substances such as, for example, of vinylpyrrolidinone-cephalosporin derivatives.
Type:
Grant
Filed:
July 29, 2003
Date of Patent:
March 29, 2005
Assignee:
Basilea Pharmaceutica AG, A Swiss Company
Abstract: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.
Type:
Grant
Filed:
July 3, 2003
Date of Patent:
March 8, 2005
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
December 28, 2004
Assignees:
Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd., Axys Pharmaceuticals, Inc.
Abstract: The present invention relates to a 2-phenyl-3-heteroarylpropionic acid derivative or a salt thereof, and also relates to a pharmaceutical agent and a VLA-4 and/or LPAM-1 antagonist each of which contains the same as an active ingredient.
Abstract: A new ligands that include a benzene ring in the backbone can be combined with a metal or metal precursor compound or formed into a metal-ligand complex catalyze a number of different chemical transformations, including olefin polymerization reactions. The ligands, complexes formed with the ligands and compositions including the ligands are useful catalysts, depending on the reaction.
Type:
Application
Filed:
June 29, 2004
Publication date:
December 9, 2004
Applicant:
Symyx Technologies, Inc.
Inventors:
Anil Guram, Cheryl Lund, Howard W. Turner, Tetsuo Uno
Abstract: The present invention provides a method to improve the optical purity of 1-benzyl-3-aminopyrrolidine having a low optical purity using an inexpensive agent via a simple procedure. The present invention provides a method for improving the optical purity of 1-benzyl-3-aminopyrrolidine including the steps of converting 1-benzyl-3-aminopyrrolidine into an equimolar salt with an optically inactive acid, and recovering the salt as crystals. The present invention also provides a salt of 1-benzyl-3-aminopyrrolidine that is used in the method.
Abstract: The present invention relates to novel substituted imidates of the formula (I) 1
Type:
Application
Filed:
April 7, 2004
Publication date:
November 25, 2004
Inventors:
Achim Hense, Rudiger Fischer, Ernst-Rudolf Gesing, Stefan Herrmann, Kristian Kather, Stefan Lehr, Katharina Jansen, Hans-Jochem Riebel, Peter Jeschke, Christoph Erdelen, Angelika Lubos-Erdelen, Wolfram Andersch, Peter Losel, Udo Reckmann
Abstract: Disclosed are compounds of the formula: 1
Type:
Application
Filed:
June 16, 2004
Publication date:
November 25, 2004
Applicant:
Schering Corporation
Inventors:
Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jonathan A. Pachter, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
Abstract: The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the process of the present invention.
Type:
Application
Filed:
February 10, 2004
Publication date:
November 18, 2004
Inventors:
John R. Snoonian, Patricia Ann Oliver-Shaffer
Abstract: The invention relates to processes for converting amino acids and amides to desirable conversion products including pyrrolidines, pyrrolidinones, and other N-substituted products. L-glutamic acid and L-pyroglutamic acid provide general reaction pathways to numerous and valuable selective conversion products with varied potential industrial uses.
Abstract: Stable, topically applicable cosmetic/dermatological sunscreen compositions, well suited for the UV-photoprotection of human skin/keratinous materials, contain a thus effective amount of at least one novel amine, amide, sulphonamide or carbamate substituted benzalmalonic salt compound.
Abstract: This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia, inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity.
Type:
Application
Filed:
June 25, 2003
Publication date:
August 26, 2004
Inventors:
Daniel P. Becker, Yiyuan Chen, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Donald W. Hansen, Robert M. Heintz, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Sergio Mantegani, Mark A. Massa, Joseph J. McDonald, Deborah A. Mischke, Mark A. Nagy, Ettore Perrone, Joseph G. Rico, Michelle A. Schmidt, Dale P. Spangler, John J. Talley, Mahima Trivedi, Thomas A. Wynn
Abstract: This invention provides compounds of Formula I having the structure
wherein R1, R2, R3, R4, W, X, and Y are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
Abstract: The invention relates to novel compounds which are substituted amino-aza-cycloalkane derivatives of the general formula I. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula I and especially their use as inhibitors of the plasmodium falciparum protease plasmepsin II or related aspartic proteases.
Type:
Application
Filed:
March 25, 2003
Publication date:
May 27, 2004
Inventors:
Christoph Boss, Walter Fischli, Solange Meyer, Sylvia Richard-Bildstein, Thomas Weller
Abstract: The present invention is to provide a process for producing an optically active amino alcohol which is useful for the synthesis of natural substances and as an intermediate for drugs and agricultural chemicals in a high yield, a high selectivity and an economical manner with a good working efficiency and the present invention relates to a process for producing an optically active amino alcohol represented by the following formula (2) 1
Abstract: Tropolone derivatives represented by the formula (I), which have retinoid actions and are useful as active ingredients of medicaments [R1 to R4 represent hydrogen atom, an alkyl group, or an alkoxyl group; the ring represented by Ar represents an aryl ring or a heteroaryl ring; X represents a single bond, —N═N—, —CON(R5)—, —(C═C)nCON(R6)—, —N(R7)CON(R8)—, —SO2N(R9)—, —N(R10)— (R5 to R9 represent hydrogen atom or an alkyl group, n represents 1 to 3, R10 represents hydrogen atom, an alkyl group, or an acyl group), an alkylene group, an aryldiyl group, or a heterocyclic diyl group; Y represents hydrogen atom, —OR11 (R11 represents hydrogen atom, an alkyl group, or an acyl group), —NHR12 (R12 represents hydrogen atom, an alkyl group, an acyl group, or amino group), or a halogen atom.
Abstract: A novel process for the asymmetric synthesis of substituted cyclic &bgr;-amino-carboxylates of the type shown in the specification from appropriate &bgr;-enamino-ester starting materials is described. These compounds are useful as intermediates for MMP and TACE inhibitors.
Type:
Application
Filed:
September 11, 2003
Publication date:
April 29, 2004
Inventors:
Joerg Deerberg, Douglas D. McLeod, Tai-Yuen Yue
Abstract: New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
Type:
Application
Filed:
August 21, 2003
Publication date:
April 22, 2004
Inventors:
Manoj C. Desai, Simon Ng, Zhi-Jie Ni, Keith B. Pfister, Savithri Ramurthy, Sharadah Subramanian, Allan S. Wagman
Abstract: Compounds of (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling invertebrate pests (Formula) wherein J is selected from the group consisting of J-1, J-2, J-3, J-4, J-5, J-6, J-7 and J-8 (I) and R1, R2, R3, R4, R5, R7, R9 and n are as defined in the disclosure. Also disclosed are compositions for controlling an invertebrate pest comprising a biologically effective amount of a compound of (I) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of (I) (e.g., as a composition described herein).
Abstract: Pyrrolylquinones and indolylquinones useful for treating diseases such as neurodegenerative disease, viral infections and proliferative disease are described, along with methods of making such compounds and pharmaceutical formulations containing such compounds.
Abstract: An alkanoic acid derivative useful as a prophylactic or therapeutic agent of diabetes mellitus, hyperlipidemia, impaired glucose tolerance and the like can be provided by a compound represented by the formula 1
Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.
Type:
Grant
Filed:
September 24, 2001
Date of Patent:
March 23, 2004
Assignee:
President and Fellows of Harvard College
Abstract: Compounds of general formula (I)
wherein m is 0 or 1, and n is 1 or 2;
are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
Abstract: Novel cyclic compounds 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 and oncologic disorders.
Type:
Application
Filed:
March 24, 2003
Publication date:
March 18, 2004
Inventors:
Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek J. Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak, Louis J. Lombardo, Francis Y.F. Lee