Nitrogen Attached To The Acid Group Directly Or Indirectly By Acyclic Nonionic Bonding (e.g., N-hydroxy Ureas, Dihydroxamic Acids, Etc.) Patents (Class 562/623)
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Patent number: 7154002Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3–12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.Type: GrantFiled: October 7, 2003Date of Patent: December 26, 2006Assignee: Takeda San Diego, Inc.Inventors: Jerome C. Bressi, Sheldon X. Cao, Jeffrey A. Stafford, Phong H. Vu
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Patent number: 7148198Abstract: A compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof for the inhibition of activity of bacterial PDF enzyme: wherein A represents a group of formula (IA) or (IB) and wherein R1 is hydrogen, R2 is n-butyl, benzyl or cyclopentylmethyl, R3 is hydrogen, R4 is tert-butyl, iso-butyl, benzyl or methyl, R5 is hydrogen or methyl and R6 is methyl.Type: GrantFiled: July 29, 2004Date of Patent: December 12, 2006Assignee: British Biotech Pharmaceuticals, Ltd.Inventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Patent number: 7126001Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.Type: GrantFiled: October 25, 2002Date of Patent: October 24, 2006Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
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Patent number: 7091378Abstract: The present invention provides a novel method for the formation of hydroxamic acids comprising reacting under suitable conditions an ester with hydroxylamine in the presence of cyanide anion.Type: GrantFiled: July 6, 2004Date of Patent: August 15, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Chih Yung Ho, Eric David Strobel
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Patent number: 7001905Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: GrantFiled: March 12, 2001Date of Patent: February 21, 2006Assignee: Warner-Lambert CompanyInventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
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Patent number: 6967220Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: April 4, 2002Date of Patent: November 22, 2005Assignee: SmithKline Beecham CorporationInventors: Ajita Bhat, Siegfried B. Christensen, IV, James S. Frazee, Martha S. Head, Jack D. Leber, Mei Li
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Patent number: 6960685Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; X is an ether heteroatom, and is —O— or —S—; and, R2 and R3 are each independently an ether group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.Type: GrantFiled: September 27, 2001Date of Patent: November 1, 2005Assignee: TopoTarget UK LimitedInventors: Clare J Watkins, Maria Rosario Romero-Martin, Paul W Finn, Ivars Kalvinsh, Einars Loza, Daina Lolya, Igor Starchenkov, Rasma M Bokaldere, Valentina Semenikhina, C. John Harris, James E. S. Duffy
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Patent number: 6858414Abstract: The present invention provides a purification process whereby deferoxamine B produced by a microorganism and in mixture with other polyhydroxamates produced by the microorganism may be converted into its mesylate salt substantially free of the other polyhydroxamates and substantially free of chloride ion. The process includes adsorption and desorption of the deferoxamine B on an adsorption resin, direct precipitation of the deferoxamine free base out of the eluent from the adsorption resin, contacting of the deferoxamine B free base with methanesulfonic acid and isolation of the deferoxamine B mesylate salt by precipitation. This process minimizes decomposition of deferoxamine B.Type: GrantFiled: November 30, 2000Date of Patent: February 22, 2005Assignee: Biogal Gyógyszergyár Rt.Inventors: Vilmos Keri, Zoltan Czovek, Attila Mezo
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Patent number: 6852882Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: June 4, 2002Date of Patent: February 8, 2005Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Maxwell D. Cummings, Joseph M. Karpinski
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Publication number: 20040229924Abstract: Compounds of the formula: 1Type: ApplicationFiled: June 17, 2004Publication date: November 18, 2004Applicant: WYETHInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Publication number: 20040225006Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; and R1 is bicyclyl or heterobicyclyl; are useful in the treatment and prophylaxis of conditions mediated by s-CD23 or TNF.Type: ApplicationFiled: May 14, 2004Publication date: November 11, 2004Applicant: SmithKline Beecham p.l.c.Inventors: Gordon Bruton, Andrew Faller, Barry Sidney Orlek, Kishore Kalidas Rana, Graham Walker
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Publication number: 20040198830Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula(l) wherein: A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is an amide linkage selected from: —NR1C(═O)— and —C(═O)NR1—; R1 is an amido substituent; X is an ether heteroatom, and is —O— or —S—; and, R2 and R3 are each independently an ether group; and pharmaceutically acceptable salts, solvates, amides, esters, ether chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.Type: ApplicationFiled: July 28, 2003Publication date: October 7, 2004Inventors: Clare J. Watkins, Maria Rosario Romero-Martin, Paul W Finn, Ivars Kalvinsh, Einars Loza, Daina Lolya, Igor Starchenkov, Rasma M Bokaldere, Valentina Semenikhina, C. John Harris, James E.S. Duffy
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Patent number: 6787522Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, anType: GrantFiled: April 30, 2002Date of Patent: September 7, 2004Assignee: British Biotech PharmaceuticalsInventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Publication number: 20040157916Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: November 17, 2003Publication date: August 12, 2004Inventors: Siegfried B. Christensen IV, Maxwell D. Cummings, Joseph M. Karpinski
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Publication number: 20040116414Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.Type: ApplicationFiled: May 7, 2003Publication date: June 17, 2004Inventors: Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
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Publication number: 20040092598Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(═O)—and —C(═O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.Type: ApplicationFiled: August 27, 2003Publication date: May 13, 2004Inventors: Clare J. Watkins, Maria Rosario Romero-Martin, Kathryn G. Moore, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Seminkhina, Andris Amolins, C.John Harris, James E. S. Duffy
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Publication number: 20040087585Abstract: Nobel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 28, 2003Publication date: May 6, 2004Inventors: Jia-Ning Xiang, Siegfried B Christensen, Jinhwa Lee, Daniel J Mercer
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Publication number: 20040086460Abstract: New types of hydroxamic acid-based bifunctional chelators are provided. These chelators are designed to chelate metal ions that can be detected either by their paramagnetic or radioactive properties. Conjugation with peptides or protein can be achieved by the presence of a linker moiety in the molecular structure of these chelators.Type: ApplicationFiled: August 4, 2003Publication date: May 6, 2004Inventor: Jean-Marc DuFour
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Publication number: 20040082630Abstract: The invention relates to &agr;-amino-N-hydroxy-acetamide derivatives of formula (I), wherein R is di-lower alkyl amino, 1,2,3-triazol-2yl or 1,2,4-triazol-4-yl, m represents an integer from 1 up to and including 10, and n represents an integer from 0 up to and including 10, and salts thereof; to processes for their preparation, pharmaceutical compositions comprising said hydroxamic acid derivatives, the use of such hydroxamic acid derivatives as medicaments, and a method of treating conditions or diseases mediated by matrix-degrading metalloproteinases (MMP's) using said derivatives alone or in combination with one or more other therapeutic agents.Type: ApplicationFiled: August 7, 2003Publication date: April 29, 2004Inventors: Kenji Hayakawa, Genji Iwasaki, Shinichi Koizumi, Ichiro Umemura
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Publication number: 20040077727Abstract: A compound of formula (I) wherein: R is isopropyl; n is 0; R1 is naphthylmethyl; R2 is t-butyl; and R3 is methyl; is useful in the treatment of disorders mediated by s-CD23.Type: ApplicationFiled: October 3, 2003Publication date: April 22, 2004Applicant: SmithKline Beecham P.L.C.Inventors: John Gerard Ward, Andrew Faller
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Patent number: 6716878Abstract: Compounds of formula (I) are antibacterial agents: wherein Z represents a radical of formula —N(OH)CH(═O) or of formula —C(═O)NH(OH), and R1-R4 are as defined in the specification. A method for the treatment of bacterial or protozoal infections in humans and non-human mammals, which comprises administering to a subject suffering such infection an antibacterially or antiprotozoally effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof.Type: GrantFiled: October 5, 2001Date of Patent: April 6, 2004Assignee: Vernalis (Oxford) LimitedInventors: Richard Simon Todd, Daniel Christopher Brookings, Helen Katherine Smith, Alison Jane Thompson, Raymond Paul Beckett
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Patent number: 6710208Abstract: This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and &agr;,&bgr;-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.Type: GrantFiled: March 27, 2002Date of Patent: March 23, 2004Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph M. Salvino, George C. Morton, Helen J. Mason, Richard F. Labaudiniere
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Publication number: 20040034071Abstract: A thioaryl sulfonamide hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: ApplicationFiled: January 21, 2003Publication date: February 19, 2004Inventors: Daniel P. Getman, Daniel P. Becker, Thomas E. Barta, Clara I. Villamil, Susan L. Hockerman, Louis J. Bedell, Madeleine Hui Li, John N. Freskos, Robert M. Heintz, Joseph J. Mc.Donald, Gary A. DeCrescenzo
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Publication number: 20040033988Abstract: Compounds of the formula: 1Type: ApplicationFiled: February 27, 2003Publication date: February 19, 2004Applicant: WyethInventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
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Patent number: 6689788Abstract: A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: and a pharmaceutically acceptable carrier therefor.Type: GrantFiled: August 25, 2000Date of Patent: February 10, 2004Assignee: University of FloridaInventor: Raymond J. Bergeron, Jr.
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Patent number: 6686502Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.Type: GrantFiled: March 11, 2003Date of Patent: February 3, 2004Assignee: UCB S.A.Inventors: Xiong Cai, Timothy Lewis
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Patent number: 6683200Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: GrantFiled: October 4, 2001Date of Patent: January 27, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
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Publication number: 20030212049Abstract: Compounds of the formula: 1Type: ApplicationFiled: February 27, 2003Publication date: November 13, 2003Applicant: WyethInventors: Jeremy I. Levin, James Ming Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
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Publication number: 20030212140Abstract: The present invention relates to thiourea compounds and the pharmaceutical compositions containing the same, and particularly, to novel thiourea compounds as an antagonist against vanilloid receptor (VR) and the pharmaceutical compositions thereof. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.Type: ApplicationFiled: February 20, 2003Publication date: November 13, 2003Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Young Ho Park, Jung Bum Yi
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Publication number: 20030207923Abstract: Compounds of formula (I): wherein X1 is alkyl, sulphonyl or carboxy: X2 is hydrogen or alkyl; R1 is arylmethyl or heterocyclylmethyl; R2 is alkyl, alkenyl, aryl, cycloalkyl or cycloalkenyl; and R3 is hydrogen, alkyl, alkenyl, alkynyl or aryl; are useful in the treatment of disorders mediated by s-CD23.Type: ApplicationFiled: May 14, 2003Publication date: November 6, 2003Inventors: Andrew Faller, Anne-Geraldine Rousseau, David Timothy Macpherson, Peter Henry Milner
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Publication number: 20030199571Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; and R1 is bicyclyl or heterobicyclyl; are useful in the treatment and prophylaxis of conditions mediated by s-CD23 or TNF.Type: ApplicationFiled: March 24, 2003Publication date: October 23, 2003Inventors: Gordon Bruton, Andrew Faller, Barry Sidney Orlek, Kishore Kalidas Rana, Graham Walker
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Publication number: 20030191309Abstract: The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.Type: ApplicationFiled: November 12, 2002Publication date: October 9, 2003Inventor: Wen-Bin Ho
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Publication number: 20030176486Abstract: The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.Type: ApplicationFiled: February 14, 2003Publication date: September 18, 2003Inventors: Kazuhiro Maeda, Shuji Sonda, Tadahiro Takemoto, Tomokazu Goto, Fujio Kobayashi, Masahiko Kajii, Naruyasu Komorita, Fumihiro Hirayama
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Publication number: 20030139379Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: ApplicationFiled: July 3, 2002Publication date: July 24, 2003Applicant: Shionogi & Co., Ltd.Inventors: Fumihiko Watanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Publication number: 20030130238Abstract: Compounds of the formula 1Type: ApplicationFiled: November 1, 2002Publication date: July 10, 2003Applicant: American Cyanamid CompanyInventors: Vincent Premaratna Sandanayaka, Efren Guillermo Delos Santos
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Patent number: 6576628Abstract: The invention relates to inhibitors of matrix metalloproteases, more specifically a 3-aryl-succinamido-hydroxamic acid of formula (I) and its salt, ester and derivative thereof, along with methods of producing a compound of formula (I) and pharmaceutical compositions thereof.Type: GrantFiled: July 6, 2000Date of Patent: June 10, 2003Assignee: Roche Diagnostics GmbHInventors: Frank Grams, Gerd Zimmermann, Hans-Willi Krell, Ernesto Menta, Herbert Leinert
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Patent number: 6569636Abstract: An assay is disclosed for determining whether a test compound modulates the activity of an enzyme having a metallated active site. The assay method employs a comparison of the binding ability of the metallated and unmetallated forms of the enzyme to the test compound.Type: GrantFiled: May 27, 1999Date of Patent: May 27, 2003Assignee: Hawaii Biotechnology Group, Inc.Inventors: Paul G. Grothaus, Dana E. Davis, Sean O'Malley
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Publication number: 20030083521Abstract: Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Inhibition of histone deacetylase can lead to the histone deacetylase-mediated transcriptional repression of tumor suppressor genes. For example, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, such as hematopoiesis, and genetic related metabolic disorders, such as, cystic fibrosis and adrenoleukodystrophy.Type: ApplicationFiled: December 2, 2002Publication date: May 1, 2003Applicant: CircaGen Pharmaceutical, a Maryland corporationInventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman, Norbert L. Wiech
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Patent number: 6512121Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: GrantFiled: June 11, 2001Date of Patent: January 28, 2003Assignee: G.D. Searle & Co.Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Hwang-Fun Lu
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Patent number: 6512123Abstract: Compounds of formula I wherein R1, R2, A, X, Y and Z have the meanings provided in the specification, and their enantiomers, diastereoisomers, racemates, pharmaceutically acceptable salts and mixtures thereof. These compounds have HDAC inhibitory activity for inhibiting cell proliferation. Also provided is a process of manufacturing these compounds.Type: GrantFiled: April 22, 2002Date of Patent: January 28, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Adelbert Grossmann, Wolfgang von der Saal, Tim Sattelkau, Ulrich Tibes
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Patent number: 6511990Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.Type: GrantFiled: August 24, 2000Date of Patent: January 28, 2003Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
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Publication number: 20030013910Abstract: A method of synthesizing &agr;-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound &agr;-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.Type: ApplicationFiled: May 15, 2002Publication date: January 16, 2003Inventors: Eugene Campian, Boliang Lou, Adnan M.M. Mjalli
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Patent number: 6500983Abstract: Novel hydroxamic acid compounds, e.g., of formula I, wherein R1, R2, R3 and R4 are as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of autoimmune and inflammatory diseases, e.g., multiple sclerosis and rheumatoid arthritis. Methods of making the compounds, novel intermediates, and pharmaceutical compositions comprising the compounds are provided.Type: GrantFiled: October 9, 2001Date of Patent: December 31, 2002Assignee: Novartis AGInventors: Georg Kottirsch, Ulf Neumann
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Patent number: 6492422Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 27, 2002Date of Patent: December 10, 2002Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic
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Publication number: 20020177084Abstract: The present invention relates to a silver halide color photographic light-sensitive material wherein at least one of light-sensitive silver halide emulsion layers includes a silver halide emulsion having a silver chloride content of at least 95 mol % and a silver iodide content of 0.05 mol % to 0.75 mol % and/or a silver bromide content of 0.05 mol % to 4.Type: ApplicationFiled: February 26, 2002Publication date: November 28, 2002Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Atsushi Matsunaga, Tadashi Inaba, Shinichi Ichikawa
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Publication number: 20020165166Abstract: The present invention relates to compounds that are capable of modulating CD154 mobilization and that are useful for stabilizing the thrombotic process and reducing the activation of cells involved in an inflammatory response. The present invention also relates to methods useful for identifying such compounds. The present invention also relates to the treatment of platelets for transfusion with metalloproteinase inhibitors to treat or prevent inflammation. The present invention also includes compositions and methods to treat injury and disease related to such biological processes.Type: ApplicationFiled: November 30, 2001Publication date: November 7, 2002Inventors: Yibing Yan, David Phillips, Lisa Alaimo, Patrick Andre, Veronica Alves
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Patent number: 6476027Abstract: An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: December 6, 1999Date of Patent: November 5, 2002Assignee: Monsanto CompanyInventors: Clara I. Villamil, John N. Freskos, Brent V. Mischke, Patrick B. Mullins, Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Thomas E. Barta, Daniel P. Becker
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Patent number: 6465468Abstract: The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with matrix metalloproteinase, ADAM or ADAM-TS enzymes, a condition that is mediated by TNF &agr; or a condition involving a membrane-shedding event that is mediated by a metalloproteinase. Compounds of the invention are of formula I (B)2N—X—(CH2)m—W—(CR1R2)n—COY (I) wherein n=0 or 1; m=0 or 1; X is S(O)1-2; Y is OH or NHOH; W is aryl or heteroaryl; and the other groups are as defined herein.Type: GrantFiled: March 22, 2000Date of Patent: October 15, 2002Assignee: Darwin Discovery LimitedInventors: Andrew Douglas Baxter, David Alan Owen, Duncan Batty, Robert John Watson
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Patent number: 6462042Abstract: Compounds having therapeutic utility are of formula (I) wherein B1, B2, R1 and R2 are each various sub-stituents, or R1 and R2 together form a ring.Type: GrantFiled: March 28, 2001Date of Patent: October 8, 2002Assignee: Darwin Discovery LimitedInventors: David Alan Owen, Andrew Douglas Baxter, Robert John Watson, John Gary Montana
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Patent number: 6458779Abstract: Compounds of Formula (1) wherein: R is methyl substituted by one to three groups from alkyl, aryl, alkenyl, and alkynyl; n is ) or 1; R1 is arylmethyl or heterocyclylmethyl; R2 is alkyl, alkenyl, cycloalkyl or cycloalkenyl; and R3 is hydrogen, alkyl, alkenyl, alkynyl or aryl; are useful in the treatment of disorders mediated y s-CD23.Type: GrantFiled: April 5, 2001Date of Patent: October 1, 2002Assignee: SmithKline Beecham p.l.c.Inventors: Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Jayshree Mistry, John Gerald Ward