Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 548/192)
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Patent number: 9376430Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: GrantFiled: July 30, 2014Date of Patent: June 28, 2016Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, Jr.
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Publication number: 20150133656Abstract: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 22, 2013Publication date: May 14, 2015Applicants: CARNA BIOSCIENCES INC., NATIONAL CANCER CENTERInventors: Masaaki Sawa, Hideki Moriyama, Tesshi Yamada, Miki Shitashige, Yusuke Kawase, Yuko Uno
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Publication number: 20150057279Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: March 27, 2013Publication date: February 26, 2015Inventors: Michael Berger, Marko Eck, Christopher Kern
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Publication number: 20150018330Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: July 30, 2014Publication date: January 15, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
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Patent number: 8907092Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3?, R4, R4? and R5, are as described herein.Type: GrantFiled: April 29, 2008Date of Patent: December 9, 2014Assignee: Genentech, Inc.Inventors: John A. Flygare, Frederick Cohen, Kurt Deshayes, Michael F. T. Koehler, Lewis J. Gazzard, Lan Wang, Chudi Ndubaku
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Patent number: 8835644Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: GrantFiled: March 16, 2010Date of Patent: September 16, 2014Assignee: University of Virginia Patent FoundationInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, Jr.
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Publication number: 20130317218Abstract: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 24, 2012Publication date: November 28, 2013Inventors: Masaaki Sawa, Hideki Moriyama, Tesshi Yamada, Miki Shitashige, Yusuke Kawase, Yuko Uno
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Patent number: 8507690Abstract: The invention provides a thiazole derivative useful as a VAP-1 inhibitor, as well as a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like, a method of inhibiting VAP-1 in a subject, and a method for the prophylaxis or treatment of VAP-1 associated disease in a subject. The thiazole derivative is a compound represented by the formula (I): R1—NH—X—Y—Z wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 30, 2009Date of Patent: August 13, 2013Assignee: R-Tech Ueno, Ltd.Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Yosuke Kawai, Akiko Kawasaki, Akiko Akasaka, Makoto Takewaki
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Publication number: 20120283268Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: ApplicationFiled: June 15, 2012Publication date: November 8, 2012Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Vasudevan Sudarsanam, Swapnil G. Yerande, Gajanan S. Inamdar
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Patent number: 8152861Abstract: The present invention relates to a) a non-oxidative coloring agent for keratin fibers, in particular human hair, comprising at least one dye according to formula (I) or (II), b) an oxidative coloring agent for keratin fibers, in particular human hair, which comprises at least one oxidizing agent (e.g. hydrogen peroxide), at least one oxidative dye precursor and at least one dye according to formula (I) or (II), and c) a lightening agent for keratin fibers, in particular human hair, which comprises at least one oxidizing agent (e.g. hydrogen peroxide) and at least one dye according to formula (I) or (II), with R4 being a cationic group.Type: GrantFiled: June 3, 2011Date of Patent: April 10, 2012Assignee: The Procter & Gamble CompanyInventors: Markus Speckbacher, Jessica Chassot, Hans-Jürgen Braun
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Publication number: 20120010187Abstract: The invention provides FIG. 1 novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: March 16, 2010Publication date: January 12, 2012Applicant: University of Virginia Patent FoundationInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, JR.
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Publication number: 20110212983Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 18, 2009Publication date: September 1, 2011Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
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Patent number: 7915405Abstract: Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: September 30, 2009Date of Patent: March 29, 2011Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Taeho Lee, Moon-Kook Jeon, Heeyeong Cho, Jae Yang Kong, Gildon Choi, Dae Young Jeong, Soon-Hee Hwang
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Publication number: 20100234350Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 14, 2009Publication date: September 16, 2010Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
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Publication number: 20100168419Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Shiming Li, Lee Apostle McDermott, Yimin Qian, Weiya Yun
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Publication number: 20100143500Abstract: A method of treating a glial cell related disorder in a mammalian subject includes administering a drug which enhances or prolongs GSK-3 ? or ? inactivation.Type: ApplicationFiled: October 31, 2007Publication date: June 10, 2010Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Sean E. Lawler, Michal Oskar Nowicki, E. Antonio Chiocca
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Publication number: 20090306073Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: ApplicationFiled: April 5, 2007Publication date: December 10, 2009Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Swapnil G. Yerande, Gajanan S. Inamdar, Jitendra C. Kaila, H. Padh Ahmedabad, Vasudevan Sudarsanam
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Publication number: 20090298866Abstract: The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein X, R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: July 9, 2007Publication date: December 3, 2009Inventors: Adrian Hall, David Nigel Hurst, Tiziana Scoccitti, Pamela Joan Theobald
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Patent number: 7056939Abstract: The present invention relates to a new compound of formula I as a free base or a pharmaceutically acceptable salt thereof, a process for the preparation, pharmaceutical formulations containing said therapeutically active compound and to the use of said compound in therapy.Type: GrantFiled: July 3, 2002Date of Patent: June 6, 2006Assignee: Astrazeneca ABInventors: Stefan Berg, Sven Hellberg
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Publication number: 20040192926Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: ApplicationFiled: February 11, 2004Publication date: September 30, 2004Inventors: George D. Hartman, Thomas J. Tucker, John T. Sisko, Anthony M. Smith, William C. Lumma Jr
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Publication number: 20040106795Abstract: PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: September 29, 2003Publication date: June 3, 2004Inventors: Ajita Bhat, Siegfried B. Christensen IV, James S. Frazee, Martha S. Head, Jack D. Leber, Mei Li
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Publication number: 20040077875Abstract: 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: ApplicationFiled: March 3, 2003Publication date: April 22, 2004Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek J. Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
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Patent number: 6716850Abstract: Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CHR8)n-—D—(CHR8)m—; D is —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl; R9 is H, C1-C3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularType: GrantFiled: March 5, 2002Date of Patent: April 6, 2004Assignee: Medivir ABInventors: Stefan Lindström, Christer Sahlberg, Hans Wallberg, Genaidy Kalyanov, Lourdes Salvador Odén, Lotta Naeslund
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Publication number: 20040039029Abstract: Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: July 30, 2003Publication date: February 26, 2004Applicant: Amgen Inc.Inventors: Benny C. Askew, Frenel F. De Morin, Andrew Hague, Ellen Laber, Aiwen Li, Gang Liu, Patricia Lopez, Rana Nomak, Vincent Santora, Christopher Tegley, Kevin Yang
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Publication number: 20040014968Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: ApplicationFiled: July 9, 2003Publication date: January 22, 2004Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Publication number: 20040002506Abstract: The present invention provides the compound having the formula: 1Type: ApplicationFiled: October 25, 2002Publication date: January 1, 2004Applicants: 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: 20030225087Abstract: 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: ApplicationFiled: June 5, 2003Publication date: December 4, 2003Inventors: 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
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Publication number: 20030187040Abstract: 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-C4 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom to 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 acceptaType: ApplicationFiled: April 30, 2001Publication date: October 2, 2003Inventors: Paolo Pevarello, Raffaella Amici, Gabriella Traquandi, Manuela Villa, Anna Vulpetti, Antonella Isacchi
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Publication number: 20030181718Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: ApplicationFiled: February 10, 2003Publication date: September 25, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Publication number: 20030134802Abstract: Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.Type: ApplicationFiled: February 10, 2003Publication date: July 17, 2003Inventors: Hans-Ulrich Demuth, Konrad Glund, Dagmar Schlenzig, Susanne Kruber
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Patent number: 6552054Abstract: The invention provides chromone derivatives of the following general formula, a process for preparing such chromone derivatives and a prophylactic and therapeutic agent comprising such chromone derivatives for bone diseases and chondropathy: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 is a hydrogen atom or hydrocarbon group; R3 is a hydrogen atom, hydrocarbon group or halogen; n is an integer of 0-3; or a salt thereof.Type: GrantFiled: March 1, 2002Date of Patent: April 22, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Masahiro Kawase, Akira Mori
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Patent number: 6486184Abstract: Substituted benzene acetamide compounds which are glucokinase activators and pharmaceutically acceptable salts thereof.Type: GrantFiled: July 13, 2001Date of Patent: November 26, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Robert Francis Kester, Ramakanth Sarabu
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Publication number: 20020115826Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: March 26, 2001Publication date: August 22, 2002Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
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Publication number: 20020002190Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: ApplicationFiled: May 1, 2001Publication date: January 3, 2002Inventors: Wendy L. Corbett, Nancy-Ellen Haynes, Ramakanth Sarabu
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Patent number: 6239152Abstract: 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: GrantFiled: January 22, 1999Date of Patent: May 29, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
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Patent number: 6211373Abstract: This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor.Type: GrantFiled: July 8, 1998Date of Patent: April 3, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
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Patent number: 6190923Abstract: The present invention relates to the field of immunoassays for metal ions. The invention presents: chelators, chelates, antibodies specific for the chelates, tracers comprising chelates conjugated to detectable labels, and immunoassays utilizing the foregoing.Type: GrantFiled: September 4, 1998Date of Patent: February 20, 2001Inventor: David K. Johnson
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Patent number: 6140330Abstract: A thiazole compound of the formula: ##STR1## wherein T is lower alkylene; u is 0 or 1; R.sup.1 and R.sup.2 are the same or different and are each H, or lower alkyl, etc.; R.sup.3 is ##STR2## R.sup.4 is H or lower alkanoyloxy-lower alkyl, which shows inhibitory activity on protein kinase C (PKC, Ca.sup.2+ /phospholipid-depending serine/threonine protein phosphatase), and are useful as a protein kinase C inhibitor.Type: GrantFiled: March 24, 1998Date of Patent: October 31, 2000Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Toyoki Mori, Michiaki Tominaga, Fujio Tabusa, Kazuyoshi Nagami, Kaoru Abe, Kenji Nakaya, Isao Takemura, Tomoichi Shinohara, Yoshihisa Tanada, Takahito Yamauchi
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Patent number: 6117894Abstract: The present invention relates to a pharmaceutical composition containing as active agent, solid particles of a compound selected from the group consisting of:compound of formula I: ##STR1## compound of formula II: ##STR2## and mixtures thereof. said particles having a particle size smaller than 200 .mu.m, the mean particle size of the said active solid particles being greater than 10 .mu.m.It also relates to a pharmaceutical composition which contains at least one pharmaceutically acceptable acid.Type: GrantFiled: May 6, 1998Date of Patent: September 12, 2000Assignee: Romark Laboratories, L.C.Inventor: Jean-Fran.cedilla.ois Rossignol
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Patent number: 6100282Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.Type: GrantFiled: December 22, 1998Date of Patent: August 8, 2000Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
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Patent number: 6096898Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.Type: GrantFiled: October 22, 1999Date of Patent: August 1, 2000Assignee: Dow AgroSciences LLCInventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
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Patent number: 5968961Abstract: The present invention relates to a pharmaceutical composition containing as active agent, solid particles of a compound selected from the group consisting of:compound of formula I ##STR1## and mixtures thereof, said particles having a particle size smaller than 200 .mu.m, the mean particle size of the said active solid particles being greater than 10 .mu.m.It also relates to a pharmaceutical composition which contains at least one pharmaceutically acceptable acid.Type: GrantFiled: May 7, 1997Date of Patent: October 19, 1999Assignee: Romark Laboratories, L.C.Inventor: Jean-Fran.cedilla.ois Rossignol
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5925622Abstract: An aryl glucuronide of 2-hydroxy-N-(5-nitro-2-thiazolyl)benzamide, preferably an O-aryl glucuronide, as well as methods for the convenient synthesis of these aryl glucuronides, highly stable and low toxicity pharmaceutical composition containing these aryl glucuronides, and methods for use of these pharmaceutical compositions, for example, for treatment of inflammation, infections, etc.Type: GrantFiled: July 13, 1998Date of Patent: July 20, 1999Assignee: Romark Laboratories, L.C.Inventors: Jean-Fran.cedilla.ois Rossignol, Marc S. Ayers
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5917048Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.Type: GrantFiled: March 19, 1997Date of Patent: June 29, 1999Assignee: Allergan Sales Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5808085Abstract: A highly efficient and practical means has been developed which enables compounds of the formula: ##STR1## wherein R.sup.1 is lower alkoxy, lower alkylamino, di-(loweralkyl) amino, or the monovalent radical A--NR.sup.3, wherein A is lower alkyl or A is R.sup.4 R.sup.5 NC(O)CH.sub.2 wherein, for example, R.sup.4 is hydrogen or alkyl and R.sup.5 is hydrogen, alkyl or a substituted alkyl, or R.sup.5 is R.sup.6 R.sup.7 N-Alk wherein R.sup.6 and R.sup.7 each is hydrogen or lower alkyl and Alk is a divalent alkyl radical; R.sup.3 is, for example, benzyl, alkyl or a substituted alkyl; and R.sup.2 is, inter alia, alkyl, cycloalkyl, 1H-imidazol-4-yl, 4-thiazolyl or 2-amino-4-thiazolyl; to be prepared through the kinetic resolution of a compound of the formula: ##STR2## wherein R.sup.1 is as defined herein, R.sup.2 is as defined herein, and B is lower alkyl. These compounds are useful intermediates in the synthesis of renin inhibiting compounds.Type: GrantFiled: December 17, 1996Date of Patent: September 15, 1998Assignee: Boehringer Ingelheim (Canada) Ltd.Inventor: Murray Douglas Bailey
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Patent number: 5747514Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.Type: GrantFiled: July 19, 1996Date of Patent: May 5, 1998Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller, Fionna Mitchell Martin
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Patent number: 5712393Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.Type: GrantFiled: November 24, 1995Date of Patent: January 27, 1998Assignee: SynthelaboInventors: Jean Michel Altenburger, Gilbert Lassalle