1,3,4-oxadiazoles (including Hydrogenated) Patents (Class 548/143)
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Patent number: 7148219Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: April 29, 2005Date of Patent: December 12, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 7125869Abstract: Novel polycyclic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: GrantFiled: June 10, 2005Date of Patent: October 24, 2006Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Pascal Collette, Michel Rivier, Andre Jomard
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Patent number: 7122565Abstract: The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following Formula I: in which, Y is S or O, R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted, R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted, R3 is X2—R?3, in which X2 is a binding group and R?3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted, or their pharmaceutically acceptable derivatives, a compound of Formula I, for their preparation, and processes for pharmaceutical compositions containing methods of using the compounds for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.Type: GrantFiled: October 1, 2001Date of Patent: October 17, 2006Assignee: Warner-Lambert LLCInventors: Fabrice Vergne, Pierre Ducrot, Charles Andrianjara, Patrick Bernardelli, Edwige Lorth Ois
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Patent number: 7105538Abstract: Substituted 2-pyrrolidin-2-yl compounds corresponding to formula I a method for their production, pharmaceutical compositions containing them, and methods of using them, especially for treating pain and/or depression.Type: GrantFiled: February 28, 2005Date of Patent: September 12, 2006Assignee: Gruenenthal GmbHInventors: Hagen-Heinrich Hennies, Corinna Sundermann, Helmut Buschmann, Bernd Sundermann
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Patent number: 7084279Abstract: Oxadiazole compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: February 11, 2002Date of Patent: August 1, 2006Assignee: Emisphere Technologies Inc.Inventor: David Gschneidner
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Patent number: 7078403Abstract: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)?NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.Type: GrantFiled: June 16, 2000Date of Patent: July 18, 2006Assignee: Biota Scientific Management Pty Ltd.Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
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Patent number: 6995182Abstract: The present invention is a series of compounds that are derivatives of 1-sulfonyl-pyrrolidine and that demonstrate affinity towards metabotropic glutamate receptors. The invention further relates to medicaments containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.Type: GrantFiled: March 26, 2003Date of Patent: February 7, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Vincent Mutel, Juergen Wichmann
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Patent number: 6987104Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: January 17, 2006Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 6982264Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.Type: GrantFiled: June 27, 2002Date of Patent: January 3, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Roy Hom, John Tucker
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6863841Abstract: New oxadiazole derivatives comprising one or more identical or different recurring units of formula I wherein W, M, w, m1, m2, p1, p2, and Y1 to Y4 are as defined herein are suitable for use in liquid crystalline mixtures, polymerizable and polymer materials.Type: GrantFiled: December 13, 2002Date of Patent: March 8, 2005Assignee: Merck Patent GmbHInventors: Peer Kirsch, Alexander Hahn
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Publication number: 20040266840Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.Type: ApplicationFiled: May 3, 2004Publication date: December 30, 2004Inventors: Rajinder Singh, Dane Goff, John J. Partridge
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Publication number: 20040266839Abstract: Compounds of formula (I), wherein R1 is a phenyl group which may be optionally substituted; R2 is selected from hydrogen, C1-6 alkyl and (CH2)p—C3-7cycloalkyl; R3 is the group: (Formula II), R4 is selected from hydrogen and C1-4 alkyl; U is selected from methyl and halogen; X and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4, and may be optionally substituted with up to two groups selected independently from C1-6 alkyl; n is selected from 0, 1 and 2; p is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: ApplicationFiled: April 15, 2004Publication date: December 30, 2004Inventors: Richard Martyn Angell, Paul Bamborough, George Stuart Cockerill, Ann Louise Walker
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Publication number: 20040234814Abstract: In view of the fact that luminescent compounds and polymers capable of emitting blue light for a long time and excellent in durability have not been developed, the present invention provides blue light-emitting compounds having special structures, blue light-emitting polymers having special repeating units, processes of producing the compounds, and luminescent elements including the polymers.Type: ApplicationFiled: May 13, 2004Publication date: November 25, 2004Inventors: Tadao Nakaya, Michiaki Tobita, Tomoyuki Saikawa, Tatsuro Ishitobi, Takashi Ushijima, Shinji Takano, Akio Tajima
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Publication number: 20040236112Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.Type: ApplicationFiled: June 22, 2004Publication date: November 25, 2004Inventors: Rajinder Singh, Dane Goff, Henry Lu, Sarkiz D. Issakani, Thomas Sun
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Patent number: 6822094Abstract: Spiro compounds of the formula (I), in which at least one of the radicals K1, L, M, N1, R1, R2, R3, R4 is one of the following groups are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.Type: GrantFiled: July 26, 2002Date of Patent: November 23, 2004Assignee: Aventis Research & Technologies, GmbH & Co. KGInventors: Josef Salbeck, Donald Lupo
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Publication number: 20040220238Abstract: The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. (I) B is a oxadiazole or thiadiazole group.Type: ApplicationFiled: May 19, 2004Publication date: November 4, 2004Inventors: Matthias Schwarz, Anna Quattropani, Patrick Page, Rusell J Thomas, Vincent Pomel
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Publication number: 20040214870Abstract: The present invention is directed to compounds of formula (I), 1Type: ApplicationFiled: February 4, 2004Publication date: October 28, 2004Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
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Publication number: 20040214036Abstract: Compounds and compositions are provided that can be used as electron transport agents in organic electronic devices such as organic electroluminescent devices. The compounds are non-polymeric and have an aromatic core conjugated to end capping groups. The aromatic core contains a phenylene group arylene or naphthalene group arylene having a pendant heteroaryl group that includes a —C═N— unit.Type: ApplicationFiled: April 15, 2003Publication date: October 28, 2004Applicant: 3M Innovative Properties CompanyInventors: James G. Bentsen, Nicholas P. Goplen, Yingbo Li, Ralph R. Roberts
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Patent number: 6794518Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: December 17, 1999Date of Patent: September 21, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
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Patent number: 6790955Abstract: The invention relates to the preparation of compounds (I) in which A═H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M═H or cation and Het=heterocycle from formula (I), to give compounds (I) (A═H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A═H), or c) reaction of (III) with cyanates and amines (VII) of the formula HNR3-Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A═H) and optional acylation if A is to be other than H.Type: GrantFiled: November 5, 2002Date of Patent: September 14, 2004Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Jan Vermehren, Lothar Willms
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Patent number: 6743811Abstract: Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.Type: GrantFiled: June 27, 2002Date of Patent: June 1, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Robert C. Gadwood
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 6727266Abstract: A compound of the formula (I): wherein: R1 is represented by the formula: wherein R4, R5, R6, R7 and R8 are monovalent radicals such as: hydrogen, halogen, optionally substituted lower alkyl, lower alkyloxy, lower alkylthio, optionally substituted amino, nitro; non-aromatic heterocyclic group, and the like with certain provisos; Y is —OH or —NHOH; R2 is hydrogen, optionally substituted lower alkyl, or optionally substituted aralkyl; R3 is halogen, hydroxy, lower alkyloxy, or lower alkylthio; (b) n is an integer from 1 to 3; its optically active substance, its prodrug, its pharmaceutically acceptable salt, and its solvate.Type: GrantFiled: July 10, 2002Date of Patent: April 27, 2004Assignee: Shionogi & Co., Ltd.Inventor: Fumihiko Watanabe
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Publication number: 20040072881Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: ApplicationFiled: October 28, 2002Publication date: April 15, 2004Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
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Patent number: 6713498Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I:Type: GrantFiled: May 30, 2002Date of Patent: March 30, 2004Assignee: Alteon IncorporatedInventor: Martin Gall
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Publication number: 20040058931Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1Type: ApplicationFiled: November 15, 2002Publication date: March 25, 2004Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
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Patent number: 6696110Abstract: Liquid crystal mixtures comprising at least one of the compounds of formula (I) containing a heterocyclic five-membered ring and with a carbon-carbon double bond in the termninal group are new. RJ=CnH2n+1CH=CHCmH2mZ1; n=1-5; m=0-5; and q=0, 1 or 2; A1 and A2=2,5-disubstituted furan, 2,5-disubstituted thiophene, 2,5-disubstituted oxazole, 2,5-disubstituted thiazole, 2,5-disubstituted 1,3,4-oxadiazole, 2,5-disubstituted 1,3,4-thiadiazole, 1,4-disubstituted benzene, 2,5-disubstituted pyrimidine, 2,5-disubstituted pyridine, 2,6-disubstituted naphthalene; laterally substituted 1,4-disubstituted benzene, laterally substituted 2,5-disubstituted pyrimidine, laterally substituted 2,5-disubstituted pyridine or laterally substituted 2,6-disubstituted naphthalene (lateral substituents=F, Cl, Br or CN); A3=any A1 or 1,4-disubstituted bicyclo(2.2.Type: GrantFiled: November 26, 2001Date of Patent: February 24, 2004Assignee: Qinetiq LimitedInventors: Rachel P Tuffin, Steven M Kelly, Neil L Campbell, Warren L Duffy, Janine H Wild
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Publication number: 20040034073Abstract: The invention provides aminoalkylindole compounds of Formula (I), wherein R1-R5, n and p are as described. Also provided are compositions containing compounds of Formula (I) and the use of compounds of Formula (I) in modulating the activity of a cannabinoid receptor in a subject. In particular, the invention provides the use of such compounds as analgesic agents.Type: ApplicationFiled: August 22, 2003Publication date: February 19, 2004Inventors: Peter Gerard Moloney, Alan Duncan Robertson
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Publication number: 20040029883Abstract: The present invention relates to compounds of general formula (I), wherein the residues R represent organic radicals, X represents a bond, oxygen or —NR12 and Y represents oxygen or sulfur, processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory, autoimmune and immune diseases.Type: ApplicationFiled: November 19, 2002Publication date: February 12, 2004Inventors: Markus Albers, Thomas Lehmann, Thomas Rlle, Gerhard Mller, Gerhard Hessler, Masaomi Tajimi, Karl Ziegelbauer, Hiromi Okigami, Haruki Hasegawa
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Publication number: 20040029935Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: ApplicationFiled: October 28, 2002Publication date: February 12, 2004Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
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Patent number: 6689794Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: May 10, 2002Date of Patent: February 10, 2004Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
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Patent number: 6686363Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: November 27, 2002Date of Patent: February 3, 2004Assignee: Kyorin Pharmaceutical Co., Ltd.Inventor: Yasumichi Fukuda
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Patent number: 6686065Abstract: Organic materials based on [5] helicenes or dibenzofluorenes are shown to have excellent properties for use in electroluminescent devices, including high stability and efficiency and low excimer formation. The materials may advantageously be adapted to have hole transport or electron transport capabilities in addition to emissive properties.Type: GrantFiled: December 12, 2001Date of Patent: February 3, 2004Assignee: Canon Kabushiki KaishaInventor: Jian Ping Chen
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Patent number: 6656911Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: April 18, 2002Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W Spruce
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Patent number: 6656910Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: GrantFiled: August 10, 2001Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Publication number: 20030207869Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1Type: ApplicationFiled: May 6, 2003Publication date: November 6, 2003Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
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Publication number: 20030208073Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1Type: ApplicationFiled: January 29, 2003Publication date: November 6, 2003Inventors: Karl-Heinz Linker, Kurt Findeisen, Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger, Akihiko Yanagi, Toshio Goto
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Publication number: 20030207913Abstract: The invention provides compounds of Formula I:Type: ApplicationFiled: November 6, 2002Publication date: November 6, 2003Inventors: David W. Piotrowski, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, Alice L. Bodnar, Vincent E. Groppi, Daniel Patrick Walker, Brad A. Acker
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Patent number: 6642180Abstract: The present invention relates to novel biphenyl-substituted cyclic ketoenols of the formula (I) in which W represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or halogenoalkoxy, CKE represents one of the groups in which A, B, D, L, M, Q1, Q2, Q3, Q4, Q5 and Q6 are as defined in the description, to preparation and to their use as pesticides and herbicides.Type: GrantFiled: January 25, 2002Date of Patent: November 4, 2003Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
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Publication number: 20030203940Abstract: A pharmaceutical composition for treating or preventing cancer containing a compound of the general formula (I), a prodorug, a pharmaceutically acceptable salt, or a solvate thereof as an active ingredient: 1Type: ApplicationFiled: October 18, 2002Publication date: October 30, 2003Inventors: Takayuki Yoshioka, Ryuji Maekawa, Fumihiko Watanabe
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Patent number: 6632809Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: December 12, 2001Date of Patent: October 14, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Publication number: 20030176642Abstract: The present invention relates to certain substituted oxadiazole peptoids and nonpeptoids useful as inhibitors of serine proteases, especially human neutophil elastase (HNE). Compounds of the present invention are useful for the treatment or amelioration of symptoms of adult respiratory distress syndrome, septic shock, and multiple organ failure. Processes mediated by HNE are also implicated in conditions such as arthritis, periodontal disease, glomerulonephritis, and cystic fibrosis.Type: ApplicationFiled: January 30, 2003Publication date: September 18, 2003Inventors: Albert Gyorkos, Lyle Spruce, Kazuyuki Ohmoto, Kazuhito Kawabata
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Patent number: 6617460Abstract: A process for preparing novel compounds useful in the preparation of 1H-indole-3-glyoxamides.Type: GrantFiled: January 24, 2003Date of Patent: September 9, 2003Assignee: Eli Lilly and CompanyInventors: Benjamin Alan Anderson, Nancy Kay Harn, Richard Duane Miller, Edward Francis Plocharczyk
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Patent number: RE39127Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 4, 2002Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori
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Patent number: RE39129Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 4, 2002Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori
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Patent number: RE39130Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: June 6, 1994Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori
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Patent number: RE39131Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atoms or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5-or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 4, 2002Date of Patent: June 13, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori
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Patent number: RE39140Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 4, 2002Date of Patent: June 20, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori