Nitrogen Bonded Directly To The Bicyclo Ring System Patents (Class 549/404)
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Publication number: 20100197686Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.Type: ApplicationFiled: March 21, 2008Publication date: August 5, 2010Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTAInventors: Chengguo Xing, Jignesh Doshi
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Publication number: 20100173985Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.Type: ApplicationFiled: February 25, 2010Publication date: July 8, 2010Applicants: University of South Florida, McGill University, The Hong Kong Polytechnic UniversityInventors: Q. Ping Dou, Tak-Hang Chan, David M. Smith
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Publication number: 20100167927Abstract: The invention relates to substituted amino-thiourea compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amino-thiourea compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds. The substituted amino-thiourea compounds are defined by the following formula (I): wherein A, B, R1, R2, R3, R4, R5.1, R5.2 and R6 are defined as in the description.Type: ApplicationFiled: May 13, 2008Publication date: July 1, 2010Applicant: BASF SEInventors: Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
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Publication number: 20100145056Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: ApplicationFiled: November 23, 2009Publication date: June 10, 2010Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth T. TenBrink
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Publication number: 20100137360Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: October 15, 2009Publication date: June 3, 2010Applicant: ABBOTT LABORATORIESInventors: Arthur R. Gomtsyan, Eric A. Voight, Erol K. Bayburt, Jun Chen, Jerome F. Daanen, Stanley DiDomenico, Michael E. Kort, Philip R. Kym, Heath A. McDonald, Richard J. Perner, Robert G. Schmidt
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Patent number: 7718704Abstract: The invention provides a novel class of cyclic oximes of Formula I: wherein A, X, Y, Z, W, R1, R2, R3 and n are as described in the summary of the invention; useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: GrantFiled: February 24, 2005Date of Patent: May 18, 2010Assignee: IRM LLCInventors: Shifeng Pan, Wenqi Gao, Nathanael Schiander Gray, Yuan Mi
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Publication number: 20100121073Abstract: A process for making (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione and pharmaceutically acceptable salts thereof, and for making intermediates useful in the formation of said compound.Type: ApplicationFiled: January 31, 2008Publication date: May 13, 2010Applicant: BIAL - PORTELA & CA S.A.Inventors: Patrício Manuel Vieira Araújo Soares Da Silva, Alexander Beliaev, David Alexander Learmonth
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Publication number: 20100120846Abstract: Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: October 15, 2009Publication date: May 13, 2010Applicant: ABBOTT LABORATORIESInventors: Arthur R. Gomtsyan, Erol K. Bayburt, Jun Chen, Stanley DiDomenico, Jerome F. Daanen, Michael E. Kort, Philip R. Kym, Heath A. McDonald, Richard J. Perner, Robert G. Schmidt, Eric A. Voight
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Patent number: 7714151Abstract: Aminated isoflavonoid synthesized by aminating the 4-keto group of isoflavanone and isoflavanone ring systems, pharmaceutical compositions containing same and uses thereof as therapeutic agents.Type: GrantFiled: November 3, 2003Date of Patent: May 11, 2010Assignee: Novogen Research Pty LtdInventors: Graham Edmund Kelly, Andrew Heaton, Jane Faragalla, John Bremner
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Patent number: 7700646Abstract: There is provided a novel compound of the general formula I in which each of R8 to R10 is hydrogen, aryl, C1-6 alkyl, trialkylsilyl or acyl; R1 to R5 are individually selected from hydrogen, hydroxy, C1-6 alkoxy and acyloxy; R6 and R7 are H, C1-4 alkyl, trialkylsilyl or acyl; X is O or NR, and R is H or Me; in which any of the alkyl groups including alkyl groups in alkoxy, acyl and acyloxy groups may be substituted by aryl, C1-4 alkyl, C1-4 alkoxy, hydroxyl, trialkylsiloxy or acyloxy groups; with the proviso that R2 and R3 are not both OH when R4 is H or OH, R1 and R5 are both H, and X is O. The amide compounds (X is NR) are analogues of epigallocatechin gallate or epicatechin galate, with an amide bond in place of the natural ester bond, with resistance to hydrolysis by esterase enzymes. The ester compounds (X is O) have a different hydroxylation pattern on the B ring as compared to the natural products.Type: GrantFiled: June 20, 2006Date of Patent: April 20, 2010Assignee: The University of London, School of PharmacyInventors: James C. Anderson, Catherine Headley, Paul D. Stapleton, Peter W. Taylor
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Patent number: 7696363Abstract: Disclosed is an improved method for preparing the isoflavonoid compound (+/?)-equol, the method comprising reducing an organic diester of the isoflavone daidzein under hydrogen-transfer conditions using palladium hydroxide catalyst.Type: GrantFiled: December 4, 2006Date of Patent: April 13, 2010Assignee: Yasoo Health Inc.Inventor: John A. Hyatt
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Patent number: 7683189Abstract: There is provided a method for producing aminobenzopyran compound, which results in little wastes, has no influence on reactors and necessitates a simple work-up procedure. Concretely, it is a method for producing aminobenzopyran compound of formula (2) characterized by reducing a nitro group on 2,2-dimethyl 2H-1-benzopyran compound of formula (1) with hydrazine in the presence of a metal catalyst.Type: GrantFiled: August 6, 2003Date of Patent: March 23, 2010Assignee: Nissan Chemical Industries, Ltd.Inventors: Takanori Shimizu, Hiroo Matsumoto
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Publication number: 20100036127Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.Type: ApplicationFiled: December 12, 2007Publication date: February 11, 2010Applicant: BIAL-PORTELA & CA, S.A.Inventors: David Alexander Learmonth, Antonio Zanotti-Gerosa, Gabriela Alexandra Grasa, Alexander Beliaev
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Patent number: 7592488Abstract: The present invention relates to a method of preparing optically active amines and chiral amines prepared thereby. The method includes reacting an amine compound, a metal catalyst, a biocatalyst including a lipase, and an acyl donor compound in an organic solvent to obtain a chiral amide compound, and then hydrolyzing the chiral amide compound to obtain a chiral amine.Type: GrantFiled: August 18, 2007Date of Patent: September 22, 2009Assignee: Postech Academy-Industry FoundationInventors: Mahn-Joo Kim, Jaiwook Park, Won-Hee Kim, Kiwon Han, Yoon Kyung Choi
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Patent number: 7547794Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 25, 2004Date of Patent: June 16, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Alex Aronov, Albert C. Pierce
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Patent number: 7544717Abstract: Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: GrantFiled: March 25, 2005Date of Patent: June 9, 2009Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, John Tucker, Varghese John, Neerav Shah
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Publication number: 20090136561Abstract: The present invention provides compositions and methods for modulating smooth muscle cells. The present invention also provides methods of identifying small molecule candidate therapeutic agents for modulating smooth muscle.Type: ApplicationFiled: October 20, 2008Publication date: May 28, 2009Applicant: Prolexys Pharmaceuticals, Inc.Inventors: Moritz von Rechenberg, John M. Peltier, Sudhir R. Sahasrabudhe, Srdjan Askovic, Robert Selliah, Thomas Zarembinski
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Publication number: 20090118302Abstract: The present invention relates to a novel benzopyran derivative having goodantagonistic activity on TGF-? receptor which can be effectively used as a prophylactic and therapeutic agent for liver disease as well as several fibroplasiadiseases such as hepatic fibrosis, liver cirrhosis, pulmonary fibrosis, dermatosclerosis, glomerular fibrosis and the like; and a pharmaceutical use thereof.Type: ApplicationFiled: June 15, 2005Publication date: May 7, 2009Inventors: Young-Dae Gong, Jin-Soo Seo, Moon-Kook Jeon, Wei-Jong Kwak, Yong-Baik Cho, Nam Kyu Lee, Eun Ju Lee, Jung Bum Lee, Jun Won Lee, Sukho Lee, Mi-Sook Dong, Jeong-Ran Kim
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Patent number: 7528267Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: August 1, 2005Date of Patent: May 5, 2009Assignees: Girindus America, Inc., Children's Hospital Medical CenterInventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
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Publication number: 20090099187Abstract: The present invention relates to new compounds of formula (I), wherein R1 to R12, P, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: May 22, 2006Publication date: April 16, 2009Applicant: AstraZeneca ABInventors: Gunnar Nordvall, Carl Petersson, Laszlo Rakos, Daniel Sohn
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Publication number: 20090092624Abstract: The present invention relates in part to antiinfective flavononol compounds represented by formula I: Another aspect of the invention is a method for treating an infection in a subject by administering the compounds of Formula I to the subject.Type: ApplicationFiled: August 15, 2008Publication date: April 9, 2009Inventors: Randall S. Alberte, William P. Roschek, JR.
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Patent number: 7507761Abstract: The invention relates to novel benzopyran derivatives of formula I, to their method of production, to composition comprising the derivatives and use thereof.Type: GrantFiled: January 21, 2005Date of Patent: March 24, 2009Assignees: Universite de Liege, Universite Libre de BruxellesInventors: Sophie Sebille, Bernard Pirotte, Stéphane Boverie, Pascal De Tullio, Philippe Lebrun, Marie-Hélène Antoine
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Patent number: 7507762Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, Z and R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: March 7, 2005Date of Patent: March 24, 2009Assignee: Cytovia, Inc.Inventors: John A. Drewe, Sui Xiong Cai, Yan Wang
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Publication number: 20090054506Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: March 24, 2006Publication date: February 26, 2009Inventors: Rui Liang, Emma R. Parmee
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Publication number: 20090048224Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, 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: September 5, 2008Publication date: February 19, 2009Applicants: Amgen, Inc., Array BioPharma, Inc.Inventors: Robert D. Groneberg, Benny C. Askew, JR., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
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Publication number: 20090035830Abstract: The present invention relates to a method of preparing optically active amines and chiral amines prepared thereby. The method includes reacting an amine compound, a metal catalyst, a biocatalyst including a lipase, and an acyl donor compound in an organic solvent to obtain a chiral amide compound, and then hydrolyzing the chiral amide compound to obtain a chiral amine.Type: ApplicationFiled: August 18, 2007Publication date: February 5, 2009Applicant: POSTECH ACADEMY-INDUSTRY FOUNDATIONInventors: Mahn-Joo Kim, Jaiwook Park, Won-Hee Kim, Kiwon Han, Yoon Kyung Choi
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Publication number: 20090030038Abstract: The present invention relates to new compounds of formula I. (I) wherein R1 to R12, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: May 22, 2006Publication date: January 29, 2009Applicant: ASTRAZENECA ABInventors: Chester Chu, Andrew Lister, Gunnar Nordvall, Carl Petersson, Didier Rotticci, Daniel Sohn, Stefan Von Berg
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Publication number: 20080306136Abstract: The invention provides compounds of formula I: useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: April 1, 2008Publication date: December 11, 2008Inventors: Shon R. Pulley, John A. Tucker
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Patent number: 7371874Abstract: The present invention relates to a noble 6-alkylamino-2-methyl-2?-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative, a method for preparing the same with high efficiency using a parallel synthetic method, one of combinatorial chemical synthetic techniques, and a use of the novel compound showing a high inhibitory effect to 5-lipoxygenase (5-LO) activity for preventing and treating leukotriene (LTA4, B4, C4, D4) activation-related diseases such as inflammatory diseases, rheumatoid arthritis, colitis, asthma and psoriasis.Type: GrantFiled: July 21, 2006Date of Patent: May 13, 2008Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Hyae-Gyeong Cheon, Moon-Kook Jeon, Cho Young Sik, Jong Yeon Hwang, Choi Hyung Sub, Jeon Hyun Suk, Soon-Hee Hwang, Song Jin Sook, Kim Chi Hyun, Sung-eun Yoo
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Patent number: 7368575Abstract: When a multi-step process reaction is carried out in a solution, it generally requires several treatments and purification procedures to go through with after the reaction, however, the inventive method for preparing 2,2?-disubstituted-3,4-dihydro-7,8-disubstituted-6-amino benzopyran derivative using a solid-phased synthetic method simplifies the treatment and purification procedures after the reaction, which makes possible to efficiently construct numerous drug-like libraries.Type: GrantFiled: October 20, 2004Date of Patent: May 6, 2008Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Hyae-Gyeong Cheon, Young-Sik Cho, Jin-Soo Seo, Jong-Yeon Hwang, Ji-Yeon Park, Sung-Eun Yoo
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Publication number: 20080085328Abstract: The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.Type: ApplicationFiled: July 6, 2007Publication date: April 10, 2008Inventors: Sui Xiong Cai, John A. Drewe, Shailaja Kasibhatla, William E. Kemnitzer, Ben Y. Tseng, Charles Blais, Denis Labrecque, Henriette Gourdeau
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Patent number: 7351738Abstract: The invention provides compounds of formula I: useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: November 26, 2003Date of Patent: April 1, 2008Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn CompanyInventors: Shon R. Pulley, John A. Tucker
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Patent number: 7312232Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; Y is selected from the group consisting of oxygen, nitrogen and sulfur wherein when Y is oxygen or nitrogen, n is 1 and when Y is sulfur, n is 0. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound having said structural formula.Type: GrantFiled: August 20, 2003Date of Patent: December 25, 2007Assignee: Research Development FoundationInventors: Bob G. Sanders, Kimberly Kline, Laurence Hurley, Robb Gardner, Marla Menchaca, Weiping Yu, Puthucode N. Ramanan, Shenquan Liu, Karen Israel
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Patent number: 7265251Abstract: A process for the nitration of conjugated alkenes of formula (I) wherein R, R1, R2, R3 and R4 have the meanings reported in the description, which allows to obtain the corresponding ?-nitro-alkenes, characterised in that the nitrating agent is a mixture of an inorganic nitrite and iodine in the presence of an oxidising agent is described.Type: GrantFiled: October 12, 2005Date of Patent: September 4, 2007Assignee: Zambon Group S.p.A.Inventors: Maurizio Paiocchi, Aldo Belli, Francesco Ponzini, Marco Villa
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Patent number: 7259271Abstract: Compounds of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X is CH2, O or S, and n is 1, 2 or 3, with the proviso that if X is CH2, n is not 1, and a method for their preparation. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.Type: GrantFiled: September 20, 2006Date of Patent: August 21, 2007Assignee: Portela & C.A., S.A.Inventors: David Alexander Learmonth, Patricio Manuel Viera Araújo Soares da Silva, Alexander Beliaev
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Patent number: 7223774Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: April 21, 2004Date of Patent: May 29, 2007Assignee: Elan Pharmaceuticals, Inc.Inventors: Jose Aquino, Varghese John, John Tucker, Roy Hom, Shon Pulley, Ruth Tenbrink
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7122573Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of polyphenol catechins that occur in green tea, such as epigallocatichin-3-gallate (EGCG), and have the structure of formula (I) wherein R1 through R11 are defined herein. Preferred R4 moieties are selected from O, S, NH and CH2, and in exemplary compounds, R4 is O and R5 is a tri-substituted aroyloxy substituent, such as a 3,4,5-substituted benzoyloxy group. Pharmaceutical compositions are provided as well, as are methods of chemotherapy and chemoprevention.Type: GrantFiled: December 6, 2002Date of Patent: October 17, 2006Assignee: SRI InternationalInventors: Nurulain Zaveri, Wan-Ru Chao, Ahlem Bensari
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Patent number: 7115657Abstract: The present invention relates to novel bifunctional agents possessing antioxidant and antiarrhytmic activity, methods for the synthesis of the same and their applications in treating ischemia-reperfusion injury, as well as a variety of disorders related to free radicals and/or arrhythmias. These bifunctional drugs should preferentially segregate in the membrane and produce their antiarrhytmic effects while, at the same time, help in protecting the membrane lipids by scavenging free radicals.Type: GrantFiled: July 4, 2001Date of Patent: October 3, 2006Assignee: Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A.Inventors: Maria Koufaki, Theodora Calogeropoulou, Alexandros Makriyannis
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Patent number: 7109236Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of polyphenol catechins that occur in green tea, such as epigallocatichin-3-gallate (EGCG), and have the structure of formula (I) wherein R1 through R11 are defined herein. Preferred R4 moieties are selected from O, S, NH and CH2, and in exemplary compounds, R4 is O and R5 is a tri-substituted aroyloxy substituent, such as a 3,4,5-substituted benzoyloxy group. Pharmaceutical compositions are provided as well, as are methods of chemotherapy and chemoprevention.Type: GrantFiled: December 8, 2003Date of Patent: September 19, 2006Assignee: SRI InternationalInventors: Nurulain Zaveri, Wan-Ru Chao, Ahlem Bensari
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Patent number: 7053117Abstract: The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the general Formula I: wherein R1–R5, A, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: May 16, 2002Date of Patent: May 30, 2006Assignee: Cytovia, Inc.Inventor: Sui Xiong Cai
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Patent number: 6962929Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: GrantFiled: October 11, 2002Date of Patent: November 8, 2005Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Patent number: 6919371Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.Type: GrantFiled: September 17, 2003Date of Patent: July 19, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
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Patent number: 6903218Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.Type: GrantFiled: September 19, 2003Date of Patent: June 7, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Gaetan H. Ladouceur, Richard D. Connell, Jeremy Baryza, Ann-Marie Campbell, Timothy G. Lease, James H. Cook
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Patent number: 6903227Abstract: Novel processes for producing enantiomerically enriched and enantiomerically pure compositions of 2-acyl substituted chromane compounds, and 2-acylchromane compounds that are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors are disclosed. Further disclosed are processes for producing salts such as acid addition salts for such enantiomerically enriched compositions.Type: GrantFiled: June 1, 2001Date of Patent: June 7, 2005Assignee: Millennium Pharmaceuticals, Inc.Inventors: James Kanter, John J. G. Mullins, Anjali Pandey, Robert Scarborough
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Patent number: 6858645Abstract: A new salt (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen tartrate, particularly the (2R,3R)-tartrate thereof, most particularly the (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate, processes for the manufacture of said tartrate salt, the use of the salt in medicine, the use of the tartrate salt in the manufacture of pharmaceutical formulations, and a method for the treatment of CNS disorders by administration of the tartrate salt to a host in need of such treatment.Type: GrantFiled: May 15, 1998Date of Patent: February 22, 2005Assignee: AstraZeneca ABInventors: Hakan Nyqvist, Daniel D Sohn
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Patent number: 6855833Abstract: Disclosed are processes for producing chromane compounds, preferably chroman-2-yl acetic acid compounds and 6-amino-chroman-2-yl acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.Type: GrantFiled: June 1, 2001Date of Patent: February 15, 2005Assignee: Millennium Pharmaceuticals, Inc.Inventors: James Kanter, John J. G. Mullins, Robert Scarborough, Derek Walker, Thomas Hense
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Patent number: 6809114Abstract: This invention relates to benzopyran derivatives of the formula (I) wherein, R1 and R2 represent each independently a C1-6alkyl group, etc, R3 represents a hydroxyl group, etc, R4 represents a hydrogen atom, etc, R6 represents a hydrogen atom, R7 represents a hydrogen atom, etc, X is absent, or represents C═O, etc, R8 represents a hydrogen atom, a C1-6alkyl group, etc, R9 represents a hydrogen atom or a nitro group, when R9 represents a nitro group, Y represents a C4-8alkylene group, —(CH2)m—CR11R12—(CH2)n— or —(CH2)o—O—(CH2)p—, R5 represents a hydrogen atom, an amino group, a C1-6alkoxy group, a C1-6alkylthio group, a C1-6alkylamino group, a C1-6 alkoxycarbonylamino group, etc, or pharmaceutically acceptable salts thereof. These compounds are useful as an antiarrhythmic agent.Type: GrantFiled: July 14, 2003Date of Patent: October 26, 2004Assignee: Nissan Chemical Industries, Ltd.Inventors: Yoshio Ohara, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
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Patent number: 6803129Abstract: The present invention relates to an organic light emitting diode (OLED) device, comprising an anode disposed on a substrate, an organic EL layer disposed on the anode and a cathode disposed on the organic EL layer.Type: GrantFiled: April 25, 2003Date of Patent: October 12, 2004Assignee: RiTdisplay CorporationInventors: Hsien-Chang Lin, Chih-Hao Kung, Chung-Cheng Pai, Shwu-Ju Shieh, Tzu-Chin Tang
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Patent number: 6800657Abstract: Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.Type: GrantFiled: July 2, 2003Date of Patent: October 5, 2004Assignee: Euro-Celtique S.A.Inventors: Christopher S. Konkoy, David B. Fick, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana