Spiro Patents (Class 548/216)
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Publication number: 20110224211Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Ron Roberts, Wieslaw Kazmierski, Richard Grimes
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Patent number: 7999115Abstract: The invention relates to compounds of formula (I) wherein R1 represents H, alkyl, alkoxy, cyano or halogen; one of U and X represents CH or N and the other represents CH, or, in the case of U, may also represent CRa and, in the case of X, may also represent CRb; Ra represents halogen; Rb represents halogen or alkoxy; B represents N, D represents CH2 and A represents CH(OH)CH2 or CH2CH2, or B represents CH, D represents CH2 or O and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH?CH, CH2CH2 or NHCO, or also B represents C(OH), D represents CH2 and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH?CH, CH2CH2 Or NHCO; R2 represents H, alkyl, alkenyl, hydroxyalkyl or alkoxycarbonylalkyl; and E represents naphthyl or a binuclear heterocyclic group; and to salts of such compounds. These compounds are useful as antimicrobial agents.Type: GrantFiled: August 29, 2007Date of Patent: August 16, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110144106Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1.Type: ApplicationFiled: December 3, 2010Publication date: June 16, 2011Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Hongying Yun
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Publication number: 20110118250Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: October 21, 2010Publication date: May 19, 2011Applicant: Amgen Inc.Inventors: Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Wenge Zhong
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Publication number: 20110092368Abstract: The present invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y and CKE have the meanings given in the disclosure, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention further relates to selectively herbicidal compositions containing 2,4,6-phenyl-substituted cyclic ketoenols and a compound which improves crop plant tolerance.Type: ApplicationFiled: December 17, 2010Publication date: April 21, 2011Inventors: Reiner Fischer, Klaus Kunz, Stefan Lehr, Michael Ruther, Udo Schneider, Markus Dollinger, Mark Wilhelm Drewes, Dieter Feucht, Jörg Konze, Ulrike Wachendorff-Neumann, Guido Bojack, Thomas Auler, Martin Jeffrey Hills, Thomas Bretschneider, Olga Malsam, Christoph Erdelen, Angelika Lubos-Erdelen, Alfred Angermann, Hein Kehne, Christopher Hugh Rosinger
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Patent number: 7923446Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: May 31, 2007Date of Patent: April 12, 2011Assignee: Wyeth LLCInventors: Jason Shaoyun Xiang, Steve Yikkai Tam, Yonghan Hu, Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini, Thomas Saltmarsh Rush, III, Elisabeth Ann Morris, Katy Evangelia Georgiadis
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Publication number: 20110082301Abstract: It comprises a process for the production of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by subjecting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6) alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6) cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4) alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.Type: ApplicationFiled: December 20, 2010Publication date: April 7, 2011Inventors: Alexander Comely, Llorenç Rafecas Jane, Nicolas Tesson, Antoni Riera Escale
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Patent number: 7893258Abstract: It comprises a preparation process of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by submitting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6)-alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6)-cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4)-alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.Type: GrantFiled: January 10, 2007Date of Patent: February 22, 2011Assignee: Sinclair Pharmaceuticals LimitedInventors: Alexander Comely, Llorenç Rafecas Jane, Nicolas Tesson, Antoni Riera Escale
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Publication number: 20110021549Abstract: The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.Type: ApplicationFiled: July 21, 2010Publication date: January 27, 2011Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR JOSHI
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Patent number: 7863291Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: GrantFiled: April 14, 2009Date of Patent: January 4, 2011Assignee: Bristol-Myers Squibb CompanyInventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
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Publication number: 20100298378Abstract: The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description, as well as to pharmaceutical compositions containing them and to methods of treatment using them.Type: ApplicationFiled: July 29, 2010Publication date: November 25, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Petra LENNIG
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Publication number: 20100286151Abstract: The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z1 is H, C1-C4 alkyl or F; Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond; A is a 5 membered heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, Cl C4 haloalkoxy, cyano; B is hydrogen or is a 5-6 membered heteroaryl, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.Type: ApplicationFiled: January 30, 2008Publication date: November 11, 2010Inventors: Jonathan Bentley, Matteo Biagetti, Romano Di Fabio, Thorsten Genski, Sebastien Guery, Silvia Rosalia Kopf, Colin philip Leslie, Angelica Mazzali, Sergio Melotto, Domenica Antonia Pizzi, Fabio Maria Sabbatini, Catia Seri
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Publication number: 20100286171Abstract: A phenylacetamide derivative having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide has an excellent GK activation action, thereby completing the present invention. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, since it has an excellent GK activation action.Type: ApplicationFiled: January 16, 2009Publication date: November 11, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Masahiko Hayakawa, Yoshiyuki Kido, Takahiro Nigawara, Mitsuaki Okumura, Akira Kanai, Keisuke Maki, Nobuaki Amino
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Patent number: 7825152Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: April 9, 2007Date of Patent: November 2, 2010Assignee: Novartis AGInventors: Trixi Brandl, Jiping Fu, Francois Lenoir, David Thomas Parker, Michael Patane, Branko Radetich, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic, Aregahegn Yifru, Rui Zheng
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Publication number: 20100272681Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: ApplicationFiled: February 20, 2008Publication date: October 28, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc Farmer, Randy Scott Bethiel, Dylan Jacobs, Robert B. Perni, John Maxwell, Kevin Cottrell, Summer Halas
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Patent number: 7807684Abstract: Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: July 17, 2006Date of Patent: October 5, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Sandeep A. Saggar, John T. Sisko, Thomas J. Tucker, Robert M. Tynebor, Dai-Shi Su, Neville J. Anthony
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Patent number: 7807841Abstract: Described herein are compounds that have a spiro structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of steroid hormone nuclear receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent diseases or conditions associated with the activity of steroid hormone nuclear receptors.Type: GrantFiled: February 16, 2006Date of Patent: October 5, 2010Assignee: IRM LLCInventors: Pierre-Yves Michellys, Chi Ching Mak, Wei Pei
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Publication number: 20100216821Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, R1 may be C1-C4 alkyl, aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; R2 may be halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano, nitro; or aryl, heteroaryl or heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R2 may correspond to —O—R3; R3 is a 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen X is carbon or oxygen; Z is carbon or nitrogen; G is a fused 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen; m may be 0 or an integer ranging from 1 to 4; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY-Y5 receptor antagonists.Type: ApplicationFiled: April 18, 2008Publication date: August 26, 2010Inventors: Nicholas Paul Barton, Benjamin Richard Bellenie, Jonathan Bentley, Matteo Biagetti, Thorsten Genski, Colin Philip Leslie, Angelica Mazzali, Domenica Antonia Pizzi, Fabio Maria Sabbatini, Catia Seri
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Publication number: 20100210837Abstract: This disclosure describes the molecular cloning of a pactamycin biosynthetic gene cluster from Streptomyces pactum ATCC 27456, characterization of individual genes in the gene cluster and the proteins encoded thereby as well as uses thereof. The pactamycin gene cluster is located within an 86.35 kilobases genetic locus and includes 53 open reading frames, 26 of which are considered to be the core cluster directly involved in the biosynthesis of pactamycin.Type: ApplicationFiled: April 18, 2008Publication date: August 19, 2010Inventor: Taifo Mahmud
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Publication number: 20100197699Abstract: The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; W is —CZ1 or nitrogen; Z1 is hydrogen, C1-C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is —CZ1, compounds of formula (I) have a trans stereochemistry; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the tType: ApplicationFiled: January 30, 2008Publication date: August 5, 2010Inventors: Jonathan Bentley, Matteo Biagetti, Francesca Cardullo, Thorsten Genski, Silvia Rosalia Kopf, Colin Philip Leslie, Sergio Melotto, Mirco Meniconi, Giancarlo Merlo, Domenica Antonia Pizzi, Catia Seri
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Patent number: 7767818Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease.Type: GrantFiled: February 10, 2009Date of Patent: August 3, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Murray Douglas Bailey, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Montse Llinas-Brunet, Marc-Andre Poupart, Jean Rancourt
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Patent number: 7763734Abstract: One aspect of the invention relates to chiral bisoxazolidines and their use in asymmetric catalysis. The chiral bisoxazolidines are a novel class of compounds that is expected to find multiple applications, for example, in asymmetric synthesis. For example, a bisoxazolidine ligand enabled the catalytic enantioselective alkynylation and alkylation of a range of aromatic and aliphatic aldehydes, generating chiral propargylic alcohols and secondary alcohols in high yields and enantiomeric excess.Type: GrantFiled: April 19, 2007Date of Patent: July 27, 2010Assignee: Georgetown UniversityInventors: Christian Wolf, Shuanglong Liu
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Publication number: 20100145050Abstract: The present invention relates to chemical compounds that can be used in electrooptical applications. The electrically conductive and optical properties of these compounds, e.g. hole transporting, electron transporting and/or light emitting properties can be predetermined by substituting the core structure of these compounds with respective residues. The core structure (1) of the compounds according to the invention comprises two opposing aromatic moieties which are chemically bonded through an intermediate central atom. This central atom has a tetraedric configuration and therefore provides an orthogonal orientation to the organic moieties.Type: ApplicationFiled: January 10, 2005Publication date: June 10, 2010Applicant: TECHNISCHE UNIVERSITAT BRAUNSCHWEIGInventors: Hans-Hermann Johannes, Wolfgang Kowalsky, Martin Dümeland, Ulfla Wrenz
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Publication number: 20100137299Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 13, 2009Publication date: June 3, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Patent number: 7713963Abstract: The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1—R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.Type: GrantFiled: October 11, 2006Date of Patent: May 11, 2010Assignee: sanofi-aventis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart, Alena Safarova, Armin Walser, Teri Suzuki, Karl Schoenafinger, Ramalinga M. Dharanipragada
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Publication number: 20100093788Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.Type: ApplicationFiled: October 9, 2009Publication date: April 15, 2010Inventors: Mark R. Player, Daniel J. Parks, William Parsons, Senath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
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Publication number: 20100087429Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, T1, T2, W, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: September 11, 2009Publication date: April 8, 2010Applicant: Amgen Inc.Inventors: Ryan White, Albert Amegadzie, Marian C. Bryan, Jian Jeffrey Chen, Alan C. Cheng, Thomas Dineen, Oleg Epstein, Vijay Keshav Gore, Zihao Hua, Jason Brooks Human, Hongbing Huang, Charles Kreiman, Daniel La, Qingyian Liu, Vu Van Ma, Isaac Marx, Vinod F. Patel, Wenyuan Qian, Matthew Weiss, Chester Chenguang Yuan
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Publication number: 20100087442Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).Type: ApplicationFiled: September 24, 2009Publication date: April 8, 2010Applicant: ONO PHARMACEUTICAL CO., LTDInventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
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Publication number: 20100069449Abstract: Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including Haemophilus influenza and Coagulase negative staphylococci and resistant bacteria including vancomycin-resistant enterococci (VRE), the pharmaceutical composition is useful as an antibiotic.Type: ApplicationFiled: November 25, 2008Publication date: March 18, 2010Applicant: Korea Institute of Science & TechnologyInventors: Chang Hyun Oh, Jung Hyuck Cho
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Publication number: 20100063117Abstract: Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including Haemophilus influenza and Coagulase negative staphylococci and resistant bacteria including vancomycin-resistant enterococci (VRE), the pharmaceutical composition is useful as an antibiotic.Type: ApplicationFiled: November 20, 2008Publication date: March 11, 2010Applicant: Korea Institute of Science & TechnologyInventors: Chang Hyun Oh, Jung Hyuck Cho
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Publication number: 20100063078Abstract: The present invention relates to novel compounds of formula (I) or salts thereof: wherein A is a substituent selected in the group consisting of P, P1, P2 and P3 wherein P is P1 is P2 is P3 is p is an integer ranging from 0 to 4; R4 is selected in the group consisting of halogen, hydroxy, cyano, C1-4 alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl, SF5 and a 5- or 6-membered monocyclic heteroaryl group; and when p is an integer ranging from 2 to 4, each R4 may be the same or different; R2 is hydrogen or C1-4alkyl; q is 3, 4 or 5; n is 0, 1 or 2; X is —CR1R3— or —O—; R1 is selected in the group consisting of hydrogen, C1-4 alkyl and fluorine; R3 is selected in the group consisting of hydrogen, C1-4alkyl and fluorine; R5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR?R?; or R5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heteroType: ApplicationFiled: April 24, 2007Publication date: March 11, 2010Inventors: Barbara Bertani, Romano Di Fabio, Fabrizio Micheli, Alessandra Pasquarello, Luca Tarsi, Silvia Terreni
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Patent number: 7662995Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.Type: GrantFiled: February 19, 2004Date of Patent: February 16, 2010Assignee: Chiesi Farmaceutici S.p.A.Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
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Publication number: 20090162474Abstract: A chemical compound of the general formula I or II is useful as feed additive: wherein X=O or NR, and R=H, C1-C6-alkyl (optionally branched), C3-C6-cycloalkyl, aryl, or aralkyl, and wherein R1, R2, are identical or different and in each case H, C1-C6-alkyl (optionally branched), C3-C6-cycloalkyl, allyl, aryl, or aralkyl; or R1 and R2 together are an C2- to C6-alkylene group (optionally C1-C6-alkyl substituted).Type: ApplicationFiled: December 19, 2008Publication date: June 25, 2009Applicant: EVONIK DEGUSSA GmbHInventors: Christoph Kobler, Philipp Roth, Christoph Weckbecker, Klaus Huthmacher
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Publication number: 20090156822Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease.Type: ApplicationFiled: February 10, 2009Publication date: June 18, 2009Applicant: Boehringer Ingelheim International GmbHInventors: Murray D. BAILEY, Punit BHARDWAJ, Elise GHIRO, Nathalie GOUDREAU, Teddy HALMOS, Montse LLINAS-BRUNET, Marc-Andre POUPART, Jean RANCOURT
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Patent number: 7538130Abstract: A compound in which n is 0, 1, 2, or 3; R1, R2, R7, and R8 are each independently alkyl group, including cycloalkyl, an alkylaryl group, or an aryl group, optionally with one or more heteroatoms, with the proviso that R1 and R2 can together form a cycloalkylene group and, independently, R7 and R8 can together form a cycloalkylene group; Y is an oxygen free radical, a sulfur free radical, OR9 or SR9; R3, R4, R5, R6, and R9 are each independently H or an alkyl group, a cycloalkyl group, an aryl group, or an alkylaryl group, optionally with one or more heteroatoms; and compositions, such as basecoat and clearcoat coating compositions, containing such compounds.Type: GrantFiled: September 26, 2005Date of Patent: May 26, 2009Assignee: BASF CorporationInventors: Donald H. Campbell, Donald L. St. Aubin, Walter H. Ohrbom, John E. Boisseau
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Publication number: 20090131661Abstract: Novel raw material compounds are provided that are useful for producing novel cycloalkane carboxamide derivatives having cathepsin K inhibitory action. An oxazolone derivative represented by formula (I): [wherein, R1 represents a substituted or unsubstituted alkyl group, substituted or unsubstituted alkenyl group, substituted or unsubstituted alkynyl group, substituted phenyl group, substituted or unsubstituted naphthyl group or substituted or unsubstituted heterocyclic group, and ring A represents a saturated cyclic alkylidene group having 6 to 7 carbon atoms].Type: ApplicationFiled: January 10, 2007Publication date: May 21, 2009Applicant: SEIKAGAKU CORPORATIONInventors: Tsuneo Koji, Hisatomo Kunii, Nobuo Kobayashi
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Publication number: 20090111183Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.Type: ApplicationFiled: October 9, 2007Publication date: April 30, 2009Inventors: Colin M. Tice, Enrique L. Michelotti, Robert E. Hormann
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Publication number: 20090098410Abstract: Disclosed is a trimethine dimer compound represented by the following general formula (I) and optical recording medium containing such a compound in a recording layer. (I)(In the formula, symbols are as in the description. When both Xa2 and Xb2 are imino groups, one of Xa1, Xb1, Xa3 and Xb3 is necessarily a 1-alkyl-1-benzylmethylene group which may have a substituent, a 1,1-dibenzylmethylene group which may have a substituent or a cycloalkane-1,1-diyl group having 3 to 6 carbon atoms which may have a substituent.Type: ApplicationFiled: May 16, 2006Publication date: April 16, 2009Applicant: Mitsui Chemicals, Inc.Inventors: Taizo Nishimoto, Eiichi Takahashi, Shunsuke Murayama, Yoshiaki Aso, Akira Ogiso, Akihiro Kohsaka, Takafumi Yoshida, Hiroyuki Sasaki, Kenichi Kato, Hiroshi Terao, Yojiro Kumagae
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Patent number: 7514567Abstract: Compounds of formula I: and pharmaceutically-acceptable salts thereof, wherein Q, Ar1, A and Ar2 are as defined in the specification, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them, uses of them as medicaments for therapy, uses of them in the manufacture of medicaments and uses of them for diagnostic and analytic purposes.Type: GrantFiled: July 6, 2004Date of Patent: April 7, 2009Assignee: AstraZeneca ABInventors: Hui-Fang Chang, Eifion Phillips
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Publication number: 20090042892Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.Type: ApplicationFiled: December 29, 2006Publication date: February 12, 2009Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li, Christopher F. Thompson
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Publication number: 20090042897Abstract: The present invention relates to novel compounds or a pharmaceutically acceptable salt or solvate thereof, selected from a group consisting of: (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(2-fluoro-3-pyridinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(3-pyridazinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(1-methyl-1H-pyrazol-3-yl)-1-oxa-3-azaspiro[4.5]decan-2-one; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.Type: ApplicationFiled: January 30, 2008Publication date: February 12, 2009Applicant: GLAXO GROUP LIMITEDInventors: Jonathan Bentley, Matteo Biagetti, Thorsten Genski, Silvia Rosalia Kopf, Colin Philip Leslie, Sergio Melotto
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Patent number: 7485722Abstract: Compounds in accord with Formula I: wherein R1, L, A, B, D, E, m, n, x and y are as defined in the description, processes for the preparation of such compounds and to new intermediates employed in the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds in therapy and for the treatment of diseases mentioned in the specification.Type: GrantFiled: September 12, 2007Date of Patent: February 3, 2009Assignee: AstraZeneca ABInventors: Ian Egle, Babu Joseph, Abdelmalik Slassi, Methvin Isaac, Fupeng Ma, Joshua Clayton
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Publication number: 20090029947Abstract: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.Type: ApplicationFiled: March 11, 2008Publication date: January 29, 2009Inventors: Grier A. Wallace, Eric C. Breinlinger, Kevin P. Cusack, Shannon R. Fix-Stenzel, Thomas D. Gordon, Adrian D. Hobson, Martin E. Hayes, Graham K. Ansell, Pintipa Grongsaard
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Publication number: 20090022689Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: July 9, 2008Publication date: January 22, 2009Inventors: Yat Sun Or, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20080255057Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein Q, Q2, R1, R2, R2a, R3, R3a, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 28, 2008Publication date: October 16, 2008Applicant: WYETHInventors: Sayed Elmarakby, Ping Cai, Appavu Chandrasekaran, Mark Ruppen, Rasmy Talaat
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Patent number: 7402548Abstract: The present invention relates to benzoxazole compounds represented by the following formula (I): wherein R1 to R4 may be the same or different from each other, and each represent a hydrogen atom, alkyl group having 1 to 6 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, halogen atom, nitro group, cyano group, R12S(O)n, alkoxycarbonyl group having 1 to 4 carbon atoms, amino group, —NHCOR11 or carbonyl group, where R11 and R12 each represent an alkyl group having 1 to 6 carbon atoms, and n is an integer of 0 to 2, A represents a single bond, CHR5—Y, CR5?CR6, CR5R7—CHR6 or CHR5, where R5 represents a hydrogen atom, hydroxyl group, halogen atom or alkyl group, R6 and R7 each represent a hydrogen atom, hydroxyl group, alkyl group, halogen atom or substituted sulfonyloxy group, Y represents O, S or NH, and W represents a substituted or unsubstituted benzene ring or hetero ring, and processes for preparing the same.Type: GrantFiled: December 1, 2004Date of Patent: July 22, 2008Assignee: Kyoyu Agri Co., Ltd.Inventors: Shohei Fukuda, Akira Nakamura, Motohisa Shimizu, Tatsuo Okada, Satoshi Oohida, Takehiko Asahara
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Publication number: 20080125465Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.Type: ApplicationFiled: August 17, 2007Publication date: May 29, 2008Applicant: Intrexon CorporationInventors: Colin M. Tice, Enrique L. Michelotti, Robert E. Hormann
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Publication number: 20080125431Abstract: Compounds in accord with Formula I: wherein R1, L, A, B, D, E, m, n, x and y are as defined in the description, processes for the preparation of such compounds and to new intermediates employed in the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds in therapy and for the treatment of diseases mentioned in the specification.Type: ApplicationFiled: September 12, 2007Publication date: May 29, 2008Applicant: ASTRAZENECAInventors: Ian Egle, Babu Joseph, Abdelmalik Slassi, Methvin Isaac, Fupeng Ma, Joshua Clayton
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Patent number: 7354946Abstract: The present invention relates to a compound of Formula (I) and the manufacturing method(s) thereof and the use thereof: Formula (I) wherein: Ar is a nitrogen-containing heteroaromatic ring group; X and Z are each a carbon atom, and so on; Y is CO, and so on; R1 is a hydrogen atom, and so on; R2 and R3 are each a hydrogen atom, and so on; R4 and R5 are each a hydrogen atom, and so on; and the formula is a single bond or a double bond. According to the present invention, the compound of the present invention can provide Cdk4 and/or Cdk6 inhibitors for treating malignant tumors, because the compounds of the present invention exhibit a prominent growth inhibitory activity against tumor cells.Type: GrantFiled: December 3, 2004Date of Patent: April 8, 2008Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Hayama, Kyoko Hayashi, Teruki Honma, Ikuko Takahashi
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Patent number: 7332500Abstract: This invention relates to piperidine derivatives of formulae Ia and Ib with substituents as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. More particularly, the present invention relates to 1-oxa-3,8-diaza-spiro[4.5]decan-2-one and 1-oxa-3,9-diaza-spiro[5.5]undecan-2-one compounds and related derivatives, to compositions containing and to uses of such derivatives. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), diseases of the immune system and inflammatory diseases.Type: GrantFiled: February 10, 2005Date of Patent: February 19, 2008Assignee: Roche Palo Alto LLCInventors: Stephen Deems Gabriel, David Mark Rotstein