Nitrogen Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/55)
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Publication number: 20150025068Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.Type: ApplicationFiled: December 21, 2012Publication date: January 22, 2015Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
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Publication number: 20140235702Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: October 8, 2012Publication date: August 21, 2014Inventors: Zaneta Nikolovska-Coleska, Hollis D. Showalter, Chenzhong Liao, Ramzi Mohammad, Fardokht Abulwerdi
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Publication number: 20140024608Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, 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 14, 2013Publication date: January 23, 2014Applicant: METHYLGENE INC.Inventors: Robert Deziel, Alain Ajamian
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Patent number: 8574607Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.Type: GrantFiled: May 21, 2010Date of Patent: November 5, 2013Assignee: Syngenta Crop Protection, Inc.Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
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Publication number: 20130289057Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.Type: ApplicationFiled: January 12, 2012Publication date: October 31, 2013Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZINInventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
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Patent number: 8530512Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present and when x=0, W is not phenyl.Type: GrantFiled: December 20, 2010Date of Patent: September 10, 2013Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski, Ranjit Verma, Leah Defoe
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Publication number: 20130172339Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.Type: ApplicationFiled: September 19, 2011Publication date: July 4, 2013Applicant: KANCERA ABInventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
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Publication number: 20130017491Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Publication number: 20130017490Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Publication number: 20130017489Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Publication number: 20130011788Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Publication number: 20130011789Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Publication number: 20130011786Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Publication number: 20130011790Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Publication number: 20130011787Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Patent number: 8283479Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: GrantFiled: April 4, 2011Date of Patent: October 9, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, Jr., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
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Publication number: 20110306614Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Publication number: 20110183259Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.Type: ApplicationFiled: January 25, 2010Publication date: July 28, 2011Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Sen Liu, Pushkara R. Varanasi
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Publication number: 20110184177Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: April 4, 2011Publication date: July 28, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, JR., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
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Publication number: 20110092578Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present.Type: ApplicationFiled: December 20, 2010Publication date: April 21, 2011Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski
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Patent number: 7655641Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.Type: GrantFiled: February 10, 2004Date of Patent: February 2, 2010Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Lynn Stacy Gossett, Jonathan Edward Green, Winton Dennis Jones, Jr., Nathan Bryan Mantlo, Donald Paul Matthews, Daniel Ray Mayhugh, Daryl Lynn Smith, Jennifer Ann Vance, Xiaodong Wang, Alan M Warshawsky, Leonard Larry Winneroski, Jr., Yanping Xu, Guoxin Zhu
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Publication number: 20090227625Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B, Z and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 17, 2008Publication date: September 10, 2009Applicant: sanofi-aventisInventors: Stephanie HACHTEL, Juergen DEDIO, Elisabeth DeFOSSA, Sven GRUENEBERG, Holger HEITSCH, William BOCK, Charlie CHEN, Raymond KOSLEY, Chung-Yi KUNG, Marcel PATEK, Rosy SHER, Stephen SHIMSHOCK, Aleksandra WEICHSEL
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Publication number: 20090227667Abstract: Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.Type: ApplicationFiled: May 5, 2009Publication date: September 10, 2009Applicant: WyethInventors: Anthony Frank Kreft, Lynn Resnick, Scott Christian Mayer, George Diamantidis, Derek Cecil Cole, Boyd Lynn Harrison, Minsheng Zhang, Molly Hoke, Tingzhong Wang, Rocco John Galante
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Patent number: 7582673Abstract: Embodiments of the present invention provide bissulfonamide compounds that are agonists of GalR1. The present invention further provides compositions comprising bissulfonamide compounds that are agonists of GalR1, and methods of use of such compounds and compositions.Type: GrantFiled: October 20, 2005Date of Patent: September 1, 2009Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, Bapu Gaddam, Mohan Rao, Muralidhar Bondlela, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Suvi Simila, Tan Ren
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Publication number: 20090192213Abstract: The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.Type: ApplicationFiled: February 20, 2009Publication date: July 30, 2009Applicant: H. Lundbeck A/SInventors: Jan Kehler, Karsten Juhl, Morten Bang Norgaard
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Publication number: 20090163547Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: November 7, 2006Publication date: June 25, 2009Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
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Patent number: 7417066Abstract: The invention relates to compounds of general Formula I, the production thereof, and the use thereof as a medicinal product.Type: GrantFiled: June 7, 2006Date of Patent: August 26, 2008Assignee: Schering AGInventors: Bernd Buchmann, Martin Fritsch, Duy Nguyen, Bernd Menzenbach, Ulf Boemer
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Publication number: 20080146623Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: December 18, 2007Publication date: June 19, 2008Applicant: METHYLGENE INC.Inventors: Robert Deziel, Alain Ajamian
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Patent number: 7282595Abstract: The present invention provides antitumor compounds of the formula (I); and antitumor methods.Type: GrantFiled: November 13, 2003Date of Patent: October 16, 2007Assignee: Eli Lilly and CompanyInventors: Mary Margaret Mader, Luisa Maria Martin-Cabrejas, Michael Enrico Richett
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Patent number: 7217723Abstract: The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the General Formula (I) [where R1 and R2 independently represent a C1-6 alkyl group and the like that may have a hydrogen atom or a substituent; R3 represents a C1-6 alkyl group and the like that may have a substituent; R4 and R5 independent represents a hydrogen atom or a C1-6 alkyl group and the like that may have a substituent; R6 represents a hydrogen atom and the like; W represents —SO2—and the like; and X represents a sulphur atom and the like.] or a salt thereof, or a hydrate thereof.Type: GrantFiled: February 2, 2005Date of Patent: May 15, 2007Assignee: Eisai Co., Ltd.Inventors: Ichiro Yoshida, Shuichi Suzuki
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Patent number: 7179896Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: July 15, 2005Date of Patent: February 20, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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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: 7126012Abstract: The invention concerns compounds of formula (I): R-A-R? wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R? represents a —(CH2)t-R5 group wherein t and R5 are as defined in the descriptionType: GrantFiled: September 23, 2004Date of Patent: October 24, 2006Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renaud, Philippe Delagrange
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Patent number: 7071225Abstract: Arylaminopropane analogues are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.Type: GrantFiled: November 26, 2003Date of Patent: July 4, 2006Assignee: Alcon, Inc.Inventors: Mark R. Hellberg, Abdelmoula Namil
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6969766Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: April 25, 2003Date of Patent: November 29, 2005Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 6861444Abstract: Compounds of the general formula (I): or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.Type: GrantFiled: April 25, 2001Date of Patent: March 1, 2005Assignee: Asahi Kasei Pharma CorporationInventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
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Publication number: 20040223909Abstract: A method for assessing levels of soluble A-beta as an indicator of Alzheimer's disease, and other amyloid-related diseases, in vitro, ex vivo, in vivo, and in situ which employs an imaging agent binds specifically to soluble A-beta and is labeled for detection.Type: ApplicationFiled: December 26, 2003Publication date: November 11, 2004Inventors: Michael Christopher Montalto, Eric Dustin Agdeppa, Tiberiu Mircea Siclovan, Amy Casey Williams
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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: 20040176435Abstract: There is provided a heretoaryloxy 3-substituted propanamine compound of formula (I): wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents selected from halo, C1-C4 alkyl and C1-C4 alkoxy, and thienyl optionally substituted with up to 3 substituents selected from halo and C1-C4 alkyl; Y is selected from benzothienyl, indolyl and benzofuranyl, optionally substituted with up to 5 substituents selected from halo, C1-C4 alkyl, C1-C4 alkoxy, nitro, acetyl and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 23, 2003Publication date: September 9, 2004Inventors: Peter Gallagher, Richard Edmund Rathmell, Maria Ann Fagan
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Publication number: 20040127546Abstract: Compounds of the general formula (I): 1Type: ApplicationFiled: January 22, 2004Publication date: July 1, 2004Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
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Publication number: 20040110791Abstract: Arylaminopropane analogues are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.Type: ApplicationFiled: November 26, 2003Publication date: June 10, 2004Inventors: Mark R. Hellberg, Abdelmoula Namil
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Patent number: 6723848Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: in which X, R1, R2, R3, R4, R5 and n are as defined in claim 1, by reacting tetrahydrobenzo-fused heterocycles of formula II: in which X, R1, R2, R3, R4, R5, n and Ac are as defined in claim 1, with a catalytic amount of a noble metal catalyst in the presence of a hydrogen acceptor and then deacylating the acylated amino group by the addition of an amine.Type: GrantFiled: October 9, 2002Date of Patent: April 20, 2004Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
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Patent number: 6710071Abstract: This invention relates to a series of difluoromethylene aromatic ethers of the formula wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: August 15, 2002Date of Patent: March 23, 2004Assignee: Pfizer IncInventor: John Adams Lowe, III
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Publication number: 20040044224Abstract: The present invention relates to a one pot process for preparing a compound of formula I: I; from a compound of formula II and III: I; III.Type: ApplicationFiled: September 2, 2003Publication date: March 4, 2004Inventors: Preston Charles Conrad, John Paul Gardner
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Patent number: 6699860Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.Type: GrantFiled: December 7, 2001Date of Patent: March 2, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich
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Publication number: 20040010029Abstract: This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.Type: ApplicationFiled: April 23, 2003Publication date: January 15, 2004Inventors: Gregory H. Merriman, Philip M. Weintraub, Jeffrey S. Sabol, Ramalinga M. Dharanipragada, Nicholas J. Hrib, John G. Jurcak, Alexandre Gross, Brian Whiteley, Kwon Yon Musick, Joseph T. Klein
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Publication number: 20030220367Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented.Type: ApplicationFiled: May 9, 2003Publication date: November 27, 2003Inventors: Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
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Publication number: 20030199702Abstract: The present invention provides an efficient process for the preparation of benzothiophenecarboxamide PGD2 antagonist, S-5751.Type: ApplicationFiled: June 6, 2003Publication date: October 23, 2003Inventors: Robert Larsen, Dongwei Cai, Michel Journet, Kevin Campos