1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 548/136)
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Publication number: 20090181943Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.Type: ApplicationFiled: April 9, 2008Publication date: July 16, 2009Applicant: METHYLGENE INC.Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
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Patent number: 7557138Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).Type: GrantFiled: October 4, 2004Date of Patent: July 7, 2009Assignee: The Regents of the University of CaliforniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Publication number: 20090118286Abstract: Use of heterobicyclic acrylamides of the formula (I) in which A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description, for controlling pests, novel heterobicyclic acrylamides and processes for preparing these compounds, and also compounds of the formula (IA) in which A2, R1, R2, R5 and R6 are as defined in the description.Type: ApplicationFiled: February 27, 2006Publication date: May 7, 2009Applicant: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Jurgen Scherkenbeck, Graham Holmwood, Jurgen Wieschemeyer, Peter Losel, Olga Malsam, Mark Wilhelm Drewes, Karl-Heinz Kuck, Ulrike Wachendorf-Neumann, Christian Arnold, Vincent Lee Salgado, Thomas Bretschneider
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Patent number: 7524863Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: June 21, 2006Date of Patent: April 28, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
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Publication number: 20090105306Abstract: The present invention relates compounds of formula (I) wherein A and R1 are as defined in the specification, pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions.Type: ApplicationFiled: October 7, 2008Publication date: April 23, 2009Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Jennifer Frost, Teodozyj Kolasa, Bo Liu, Steven P. Latshaw, Xueqing Wang
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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Publication number: 20090099209Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; and R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treatiType: ApplicationFiled: December 12, 2008Publication date: April 16, 2009Inventors: Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
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Publication number: 20090099233Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: October 10, 2008Publication date: April 16, 2009Inventors: Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20090060874Abstract: 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: September 5, 2008Publication date: March 5, 2009Inventors: Yao-Ling QIU, Ce WANG, Lu YING, Yat Sun OR
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Publication number: 20090048228Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: December 9, 2005Publication date: February 19, 2009Inventors: Barbara Attenni, Federica Ferrigno, Philip Jones, Raffaele Ingenito, Olaf Kinzel, Laura Llauger Bufi, Jesus Maria Ontoria, Giovanna Pescatore, Michael Rowley, Rita Scarpelli, Carsten Schultz
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Publication number: 20080280915Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: ApplicationFiled: February 9, 2007Publication date: November 13, 2008Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble
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Patent number: 7449486Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: GrantFiled: October 17, 2005Date of Patent: November 11, 2008Assignee: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R Laird, John Robinson, Shelley Allen
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Patent number: 7439242Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: April 15, 2002Date of Patent: October 21, 2008Assignee: Amgen Inc.Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
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Publication number: 20080255123Abstract: The present invention relates to compounds of formula (I) wherein A, E, L2, R1, R3, R4 and R5 are as defined in the herein, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: October 12, 2007Publication date: October 16, 2008Applicant: Abbott LaboratoriesInventors: Michael D. Meyer, Michael J. Dart, William A. Carroll, Meena V. Patel, Tedozyi Kolasa, Xueqing Wang
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Publication number: 20080249093Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.Type: ApplicationFiled: December 13, 2004Publication date: October 9, 2008Applicant: MERCK & CO., INC.Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan
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Patent number: 7414142Abstract: Compounds of formula I, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.Type: GrantFiled: September 18, 2006Date of Patent: August 19, 2008Assignee: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Publication number: 20080182992Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: March 6, 2008Publication date: July 31, 2008Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R. Laird, John Robinson, Shelley Allen
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Patent number: 7388097Abstract: The present invention relates to novel difluoromethylthiazolylcarboxanilides of the formula (I) in which R1, R2, R3, R4 and R5 are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: January 22, 2003Date of Patent: June 17, 2008Assignee: Bayer CropScience AGInventors: Hans-Ludwig Elbe, Heiko Rieck, Ralf Dunkel, Ulrike Wachendorff-Neumann, Karl-Heinz Kuck, Astrid Mauler-Machnik, Martin Kugler, Thomas Jaetsch, Peter Wachtler
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Publication number: 20080132551Abstract: The invention provides compounds of Formula I: wherein A, B, and X are described herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which ?7 nAChR is known to be involved.Type: ApplicationFiled: March 24, 2004Publication date: June 5, 2008Inventors: Bruce Nelsen Rogers, David Walter Piotrowski, Brandon J. Margolis, Jason K. Myers, Vincent Edward Groppi, Daniel G. Rudmann
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Publication number: 20080113990Abstract: Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.Type: ApplicationFiled: October 12, 2006Publication date: May 15, 2008Inventors: Esther Martinborough, Danielle Lehsten, Timothy Neubert, Aarti Sameer Kawatkar, Nicole Zimmermann, Andreas Termin
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Patent number: 7316851Abstract: An electroluminescent element is disclosed, comprising an electroluminescent material and a fluorescent substance emitting light having an emission maximum at the wavelength different from that of light emitted from the electroluminescent material upon absorption of the light emitted from the electroluminescent material. A color conversion filter is also disclosed, comprising a fluorescent substance emitting light having an emission maximum at the wavelengths of 400 to 700 nm upon absorption of the light emitted from the electroluminescent material.Type: GrantFiled: September 4, 2003Date of Patent: January 8, 2008Assignee: Konica CorporationInventors: Hiroshi Kita, Yoshiyuki Suzuri, Taketoshi Yamada, Kazuaki Nakamura, Noriko Ueda, Yasushi Okubo
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Publication number: 20070281978Abstract: This invention relates an inhibitory modulator of AQP4 protein regarding its transmembrane water transport properties, wherein the modulator selectively binds to the AQP4 protein, and inhibits AQP4 mediated water transport.Type: ApplicationFiled: June 1, 2007Publication date: December 6, 2007Applicant: NIIGATA UNIVERSITYInventors: Tsutomu Nakada, Vincent J. Huber
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Publication number: 20070232808Abstract: The present invention relates to a novel process, useful for preparing key intermediates of formula (I) in the synthesis of various compounds, among them compounds which are potent and specific antagonists of D3 receptors, in which X may be Nitrogen or Sulfur; Het means aryl or heteroaryl; each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl C1-C6 alkoxy, halo C1-C6 alkyl C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R1, nitro, hydroxy, —NR2R3, cyano or a group Z; R1 is a C1-C4 alkyl —OR3 or —NR3R4; R2 is hydrogen or C1-C6 alkyl; R3 is hydrogen or C1-C6 alkyl; R is H, C1-C6 alkyl aryl, benzyl; each of which may be substituted by 1 to 4 groups J; according to the following Scheme 1: in which step a means a reaction in basic conditions of compounds (IIA) with 3-thiosemicarbazide derivatives, followed by a treatment with an inorganic base and n-propane phosphonic cyclic anhydride and final pH adjustment with inorganic acids to give compounds of formType: ApplicationFiled: March 30, 2007Publication date: October 4, 2007Inventor: Sergio Bacchi
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Patent number: 7271406Abstract: 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: GrantFiled: April 15, 2003Date of Patent: September 18, 2007Assignee: 3M Innovative Properties CompanyInventors: James G. Bentsen, Nicholas P. Goplen, Yingbo Li, Ralph R. Roberts
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Patent number: 7211668Abstract: 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 sulfur or oxygen; J is nitrogen or C—R?; R1, R? is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 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 nucType: GrantFiled: April 6, 2004Date of Patent: May 1, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Sung Hee Lee
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Patent number: 7189755Abstract: Melanocortin receptor-specific pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group or from one to three additional amino acid residues, optionally with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.Type: GrantFiled: February 10, 2004Date of Patent: March 13, 2007Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Zhijun Wu, Ramesh Rajpurohit
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Patent number: 7189748Abstract: Novel compounds, compositions comprising compounds, and methods for methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyl transferase activity.Type: GrantFiled: October 12, 2005Date of Patent: March 13, 2007Assignee: Forbes Medi-Tech (Research), Inc.Inventor: John Nestor
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Patent number: 7183303Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.Type: GrantFiled: November 5, 2004Date of Patent: February 27, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Ian James Collins, Timothy Harrison
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Patent number: 7169797Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.Type: GrantFiled: February 4, 2004Date of Patent: January 30, 2007Assignee: Abbott LaboratoriesInventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
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Patent number: 7157470Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: May 5, 2003Date of Patent: January 2, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
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Patent number: 7153873Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.Type: GrantFiled: June 6, 2006Date of Patent: December 26, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Sundermann
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Patent number: 7119099Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.Type: GrantFiled: February 4, 2004Date of Patent: October 10, 2006Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Christiane Yoakim, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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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: 7041670Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.Type: GrantFiled: April 8, 2003Date of Patent: May 9, 2006Assignee: Schering-Plough Animal Health CorporationInventors: Constantine G. Boojamra, Lee S. Chong, Scott J. Hecker, Tomasz W. Glinka, Dale E. Shuster
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Patent number: 6987122Abstract: 2-(1H-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.Type: GrantFiled: July 12, 2001Date of Patent: January 17, 2006Assignee: Novuspharma S.p.A.Inventors: Ernesto Menta, Nicoletta Pescalli
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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: 6908937Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 3 to 10, n represents 0, 1 or 2, Het represents the groups where R1 represents hydrogen; mercapto; optionally halogen-substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl or alkenyl; optionally substituted aryl; or optionally substituted heterocyclyl, Y represents oxygen or sulphur, and R2 represents hydrogen, alkyl or optionally substituted aryl, and to processes for their preparation and to their use as pesticides.Type: GrantFiled: July 2, 2001Date of Patent: June 21, 2005Assignee: Bayer Cropscience AGInventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
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Patent number: 6835725Abstract: Optical data carrier comprising a preferably transparent substrate which may, if desired, have previously been coated with one or more reflection layers and to whose surface a light-writeable information layer, if desired one or more reflection layers and if desired a protective layer or a further substrate or a covering layer have been applied, which can be written on or read by means of blue, red or infrared light, preferably laser light, where the information layer comprises a light-absorbent compound and, if desired, a binder, characterized in that at least one cyanine dye is used as light-absorbent compound.Type: GrantFiled: March 20, 2002Date of Patent: December 28, 2004Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Friedrich-Karl Bruder, Wilfried Haese, Rainer Hagen, Karin Hassenrück, Serguei Kostromine, Peter Landenberger, Rafael Oser, Thomas Sommermann, Josef-Walter Stawitz, Thomas Bieringer
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Publication number: 20040254227Abstract: 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: April 30, 2004Publication date: December 16, 2004Inventors: Rajinder Singh, Dane Goff, John J. Partridge
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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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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
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Patent number: RE40558Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: October 20, 2005Date of Patent: October 28, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko