The Five-membered Hetero Ring Is Unsubstituted Or Is Alkyl Substituted Only (e.g., Pyrrolidine, Etc.) Patents (Class 548/579)
  • Publication number: 20120083603
    Abstract: Polyionic liquid salts are provided comprising polycationic or polyanionic molecules. Further provided are solvents comprising one or more polyionic liquid salts, and the use of such polyionic liquid salts as stationary phases in gas chromatography, and as a reagent in electrospray ionization-mass spectrometry (ESI-MS).
    Type: Application
    Filed: December 13, 2011
    Publication date: April 5, 2012
    Applicant: Sigma-Aldrich Co. LLC
    Inventors: Daniel W. Armstrong, Junmin Huang
  • Publication number: 20120053181
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: April 28, 2010
    Publication date: March 1, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Publication number: 20120000118
    Abstract: A fuel additive composition comprising (A) polyisobutyl-based nitrogen-containing dispersants with MN of the polyisobutyl group of from 650 to 1800 Dalton, (B) carrier oils substantially free of nitrogen and (C) polyisobutyl-based dispersant boosters with MN of the polyisobutyl group of from 200 to 650 Dalton, with the proviso that the difference between the MN of the polyisobutyl group of component (A) and the MN of the polyisobutyl group of component (C) is more than 100 Dalton. Said component (C) is especially useful as an intake valve clean-up booster in gasoline-operated port fuel injection internal combustion engines.
    Type: Application
    Filed: June 1, 2011
    Publication date: January 5, 2012
    Applicant: BASF SE
    Inventors: Arno LANGE, Peter Schreyer, Robert Stuart Grace
  • Publication number: 20110313159
    Abstract: A novel camphor-derived ?-amino alcohol compound is disclosed. The novel camphor-derived ?-amino alcohol compound can be used in asymmetric addition of organozinc to aromatic and aliphatic aldehydes, including linear aliphatic ones, thus generating corresponding secondary alcohols in high yields and enantiomeric excess.
    Type: Application
    Filed: June 18, 2010
    Publication date: December 22, 2011
    Inventors: Biing-Jiun UANG, Chi-Rui Wu, Hsyueh-Liang Wu
  • Patent number: 8053435
    Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: November 8, 2011
    Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.
    Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
  • Publication number: 20110220514
    Abstract: Copper plating baths containing a leveling agent that is a reaction product of a certain imidazole with a certain epoxide-containing compound that deposit copper on the surface of a conductive layer are provided. Such plating baths deposit a copper layer that is substantially planar on a substrate surface across a range of electrolyte concentrations. Methods of depositing copper layers using such copper plating baths are also disclosed.
    Type: Application
    Filed: March 15, 2010
    Publication date: September 15, 2011
    Applicant: Rohm and Haas Electronic Materials LLC
    Inventor: Zukhra I. Niazimbetova
  • Patent number: 8017772
    Abstract: Substituted tetrahydropyrrolopyrazine compounds corresponding to the formula I: processes for their preparation, pharmaceutical compositions comprising these compounds and the use of these compounds for the treatment and/or inhibition of pain and other disorders or disease states at least partly mediated by KCNQ2/3 K+ channels.
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: September 13, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Thomas Christoph, Stefan Oberboersch, Klaus Schiene, Gregor Bahrenberg, Robert Frank, Sven Kuehnert, Wolfgang Schroeder
  • Patent number: 8012955
    Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: September 6, 2011
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
  • Patent number: 7999111
    Abstract: The invention relates to a process for the preparation of onium alkylsulfonates by reaction of an onium halide or carboxylate with a symmetrically substituted dialkyl sulfite or with an asymmetrically substituted dialkyl sulfite at temperatures of 50 to 170° C.
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: August 16, 2011
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Nikolai (Mykola) Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
  • Patent number: 7982053
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: July 19, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Michael Axten, Jesus R. Medina
  • Publication number: 20110172430
    Abstract: Process for the continuous preparation of an amine by reaction of a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary and secondary amines at a temperature in the range from 60 to 300° C. in the presence of a catalyst comprising copper oxide and aluminum oxide, wherein the reaction takes place in the gas phase and the catalytically active composition of the catalyst before reduction with hydrogen comprises PS from 20 to 75% by weight of aluminum oxide (Al2O3), from 20 to 75% by weight of oxygen-comprising compounds of copper, calculated as CuO, from 0 to 2% by weight of oxygen-comprising compounds of sodium, calculated as Na2O, and less than 5% by weight of oxygen-comprising compounds of nickel, calculated as NiO, and the shaped catalyst body has a pellet shape having a diameter in the range from 1 to 4 mm and a height in the range from 1 to 4 mm.
    Type: Application
    Filed: September 9, 2009
    Publication date: July 14, 2011
    Inventors: Martin Ernst, Bernd Stein, Steffen Maas, Jörg Pastre, Thorsten Johann, Johann-Peter Melder
  • Patent number: 7947828
    Abstract: The present invention provides dipyrrin substituted porphyrinic macrocycles, intermediates useful for making the same, and methods of making the same. Such compounds may be used for purposes including the making of molecular memory devices, solar cells and light harvesting arrays.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: May 24, 2011
    Assignee: North Carolina State University
    Inventors: Lianhe Yu, Kannan Muthukumaran, Prathapan Sreedharan, Jonathan S. Lindsey
  • Publication number: 20110111068
    Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and Alzheimer's disease with a derivative of ginger oil are also provided. Also provided is a method of conditioning biological extracts, such as a medicinal plant extract, by a reductive amination process to give nitrogen-containing derivatives.
    Type: Application
    Filed: May 17, 2010
    Publication date: May 12, 2011
    Inventors: Gilbert M. Rishton, Hiromi Arai, Zoya Kai, Cody Lee Fullenwider, Kristin Beierle
  • Patent number: 7939513
    Abstract: In accordance with one aspect, the present invention provides a compound of general formula (I), its stereoisomers thereof and/or its pharmaceutically acceptable salts thereof, which have antibacterial activity; with methods of treating infectious diseases in warm blooded animals employing these new compounds. wherein R1 is selected from optionally substituted alkyl.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: May 10, 2011
    Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.
    Inventors: Mohamed Takhi, Natesan Selvakumar, Sreenivas Kandepu, Gavara Govinda Rajulu, Javed Iqbal
  • Publication number: 20110098485
    Abstract: Compounds of the formula I, in the form of mixtures comprising predominantly one enantiomer or in the form of pure enantiomers, secondary phosphine-Q-P*(?O)HR1 (I) in which secondary phosphine is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton, and in which base skeletons a secondary phosphine group is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group, and in which base skeletons a P-chiral group —P*(O)HR1 is bonded to a carbon atom such that the phosphorus atoms are linked via 1 to 7 atoms of a carbon chain optionally interrupted by heteroatoms from the group of O, S, N, Fe or Si; P* is a chiral phosphorus atom; and R1 is a hydrocarbon radi
    Type: Application
    Filed: November 14, 2008
    Publication date: April 28, 2011
    Inventors: Benoît Pugin, Heidi Landert, Björn Gschwend, Andreas Pfaltz, Felix Spindler
  • Publication number: 20110040105
    Abstract: Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.
    Type: Application
    Filed: April 15, 2009
    Publication date: February 17, 2011
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Christian H. Huber, Young Mi Khulman, Sagun K. Tandel, Stephen R. Johannsen, Tingmin Wang, Paul Angell
  • Publication number: 20110034698
    Abstract: The present invention relates to oxonium salts having [(Ro)3O]+ cations and sulfonium salts having [(Ro)3S]+ cations, where Ro denotes straight-chain or branched alkyl groups having 1-8 C atoms or phenyl which is unsubstituted or substituted by Ro, ORo, N(Ro)2, CN or halogen, and anions selected from the group of [PFx(CyF2y+1?xHz)6?x]? anions, where 2?x?5, 1?y?8 and 0?z?2y+1, or anions selected from the group of [BFn(CN)4?n]? anions, where n=0, 1, 2 or 3, or anions selected from the group of [(Rf1SO2)2N]9? anions or anions selected from the group of [BFWRf24?w]? anions, to processes for the preparation thereof, and to the use thereof, in particular for the preparation of ionic liquids.
    Type: Application
    Filed: October 20, 2010
    Publication date: February 10, 2011
    Inventors: Nikolai(Mykola) Ignatyev, German Bissky, Helge Willner
  • Publication number: 20100291299
    Abstract: Cyclopentadienyl and Indenyl barium/strontium metal precursors and Lewis base adducts thereof are described. Such precursors have utility for forming Ba- and/or Sr-containing films on substrates, in the manufacture of microelectronic devices or structures.
    Type: Application
    Filed: August 3, 2008
    Publication date: November 18, 2010
    Applicant: ADVANCED TECHNOLOGY MATERIALS, INC.
    Inventors: Thomas M. Cameron, Chongying Xu
  • Publication number: 20100286349
    Abstract: Novel group 4 organometallic compounds, supported on anions by means of at least one covalent metal-oxygen bond, are obtained by reaction of at least one borate or aluminium comprising at least one hydroxy group with at least one group 4 transition metal compound. These compounds are used in a catalytic composition implemented in an olefin oligomerization or polymerization method.
    Type: Application
    Filed: July 3, 2008
    Publication date: November 11, 2010
    Applicant: IFP
    Inventors: Christine Bibal, Catherine Santini, Yves Chauvin, Helene Olivier-Bourbigou, Christophe Vallee
  • Publication number: 20100282081
    Abstract: An absorbent liquid according to the present invention is an absorbent liquid for absorbing CO2 or H2S or both from gas, in which the absorbent liquid includes an alkanolamine as a first compound component, and a second component including a nitrogen-containing compound having in a molecule thereof two members or more selected from a primary nitrogen, a secondary nitrogen, and a tertiary nitrogen or a nitrogen-containing compound having in a molecule thereof all of primary, secondary, and tertiary nitrogens. The absorbent liquid has an excellent absorption capacity performance and an excellent absorption reaction heat performance, as compared to an aqueous solution containing solely an alkanolamine and a nitrogen-containing compound in the same concentration in terms of wt %, and can recover CO2 or H2S or both from gas with smaller energy.
    Type: Application
    Filed: June 11, 2010
    Publication date: November 11, 2010
    Inventors: Ryuji YOSHIYAMA, Masazumi Tanoura, Noriko Watari, Shuuji Fujii, Yukihiko Inoue, Mitsuru Sakano, Tarou Ichihara, Masaki Iijima, Tomio Mimura, Yasuyuki Yagi, Kouki Ogura
  • Publication number: 20100222580
    Abstract: The invention relates to a process for the preparation of onium alkylsulfates by reaction of an onium halide with a symmetrically substituted dialkyl sulfate, in which the alkyl group can have 1 to 14 C atoms, with an asymmetrically substituted dialkyl sulfate, in which one alkyl group can have 4 to 20 C atoms and the second alkyl group denotes methyl or ethyl, with an alkyl trialkylsilyl sulfate, with an alkyl acyl sulfate or with an alkyl sulfonyl sulfate, where the reaction with a dialkyl sulfate is carried out at room temperature.
    Type: Application
    Filed: November 18, 2005
    Publication date: September 2, 2010
    Applicant: MERCK PATENT GMBH
    Inventors: Nikolai Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
  • Publication number: 20100216958
    Abstract: Isobutene, isoprene, and butadiene are obtained from mixtures of C4 and/or C5 olefins by dehydrogenation. The C4 and/or C5 olefins can be obtained by dehydration of C4 and C5 alcohols, for example, renewable C4 and C5 alcohols prepared from biomass by thermochemical or fermentation processes. Isoprene or butadiene can be polymerized to form polymers such as polyisoprene, polybutadiene, synthetic rubbers such as butyl rubber, etc. in addition, butadiene can be converted to monomers such as methyl methacrylate, adipic acid, adiponitrile, 1,4-butadiene, etc. which can then be polymerized to form nylons, polyesters, polymethylmethacrylate etc.
    Type: Application
    Filed: February 24, 2010
    Publication date: August 26, 2010
    Inventors: Matthew W. Peters, Joshua D. Taylor, Leo E. Manzer, David E. Henton
  • Patent number: 7771611
    Abstract: Novel compositions are provided containing a compound represented by the formula YOSF5 or ZOSF5, where: (a) Y is: (i) an organic cation other than (Me2N)3S+ or (ii) an inorganic cation, provided that when Y is the inorganic cation, the composition further includes a complexing agent; and (b) Z is C1-20 alkyl, aryl, cycloalkyl, combinations thereof, or analogues thereof containing at least one heteroatom, provided that the compound represented by the formula ZOSF5 is a molecular compound. Processes of making the cationic compounds are disclosed as are processes for using the compositions containing cationic compounds in nucleophilic replacement reactions to prepare the compositions containing molecular compounds including the OSF5 group.
    Type: Grant
    Filed: July 10, 2006
    Date of Patent: August 10, 2010
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Robert George Syvret, Gauri Sankar Lal, Kristen Elaine Minnich
  • Publication number: 20100173195
    Abstract: It is an object of the present invention to provide a material for electrolytic solutions suited for use as material in electrolytic solutions serving as ionic conductors in electrochemical devices, such as large-capacity cells or batteries. The present invention is related to a material for electrolytic solutions which comprises, as an essential constituent, an anion represented by the general formula (1): wherein X represents at least one element selected from among B, N, O, Al, Si, P, S, As and Se; M1 and M2 are the same or different and each represents an organic linking group; a is an integer of not less than 1, and b, c and d each independently is an integer of not less than 0.
    Type: Application
    Filed: March 17, 2010
    Publication date: July 8, 2010
    Applicant: Nippon Shokubai Co., Ltd.
    Inventors: Keiichiro Mizuta, Yukiko Yamamoto
  • Patent number: 7732453
    Abstract: The present invention discloses pyrido[2,3-B]pyrazin-3(4h)-ones for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: June 8, 2010
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrey Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov
  • Publication number: 20100121055
    Abstract: The present invention provides a short, safe, inexpensive, commercially scalable process for preparing (R)- or (S)-2-methylpyrrolidine from 2-methylpyrroline, which does not require the isolation of synthetic intermediates.
    Type: Application
    Filed: November 3, 2009
    Publication date: May 13, 2010
    Applicant: CEPHALON, INC.
    Inventors: Michael Christie, Joseph J. Petraitis
  • Patent number: 7714089
    Abstract: Rubbery polymers can be formed having the general formula: R1R2N—(CH2)n—X—CH2—CHR3R4 wherein R1 and R2 are independently selected from a group consisting of alkyls, cycloalkyls, alkenyls, cycloalkenyls, aryls, phenyls, heterocycles, acyls, and silanes, or R1 in combination with R2 forms a heterocyclic ring; n is an integer from 1 to 20; X is selected from a group consisting of sulfur, a phosphorus moiety, and a silicon moiety; R3 and R4 are one of hydrogen, alkyls, alkenyls, and at least one of which includes reactive unsaturation such as an alkenyl group. Moreover, this invention discloses a process of making functionalized rubbery polymers from the functionalized monomers.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: May 11, 2010
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Adel Farhan Halasa, Wen-Liang Hsu, Leh-Yeh Hsu, legal representative, Shingo Futamura, Joe Zhou, Chad Aaron Jasiunas
  • Patent number: 7700585
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: April 20, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
  • Publication number: 20100093985
    Abstract: A subject of the invention is the use of at least one cytosolic phospholipase A2 (cPLA2) inhibitor in the preparation of a medicament intended for the preventive and/or curative symptomatic treatment of cystic fibrosis, particularly of the increased secretion of mucus in cystic fibrosis.
    Type: Application
    Filed: April 5, 2007
    Publication date: April 15, 2010
    Applicants: INSTITUT PASTEUR, INST NAT DE LA SANTE ET DE LA RECHER. MED (INSERM)
    Inventors: Fariel Dif, Lhousseine Touqui
  • Patent number: 7691863
    Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB2 receptors.
    Type: Grant
    Filed: September 24, 2007
    Date of Patent: April 6, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michel Dietz, Sabine Gruener, Paul Hebeisen, Sylvie C. Meyer Reigner, Matthias Nettekoven, Bernd Puellmann, Stephan Roever, Christoph Ullmer
  • Patent number: 7687522
    Abstract: Selected pyridine and pyrimidine compounds of Formula I are effective for prophylaxis and treatment of diseases, such as c-met mediated diseases and/or HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: March 30, 2010
    Assignee: Amgen Inc.
    Inventors: Steven Bellon, Shon Booker, Noel D'Angelo, Ingrid M. Fellows, Jean-Christophe Harmange, Tae-Seong Kim, Matthew Lee, Longbin Liu, Mark H. Norman
  • Patent number: 7655680
    Abstract: Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) —CO—B— wherein B is a C1-6 alkylene group and (ii) —CO—Ba— wherein Ba is a C2-6 alkenylene group, and include optical isomers and salts of the compounds.
    Type: Grant
    Filed: May 16, 2005
    Date of Patent: February 2, 2010
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Isao Takemura, Kenji Watanabe, Kunio Oshima, Nobuaki Ito, Junpei Haruta, Hidetaka Hiyama, Masatoshi Chihiro, Hideki Kawasome, Yoko Sakamoto, Hironobu Ishiyama, Takumi Sumida, Kazuhiko Fujita, Hideki Kitagaki
  • Patent number: 7655666
    Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.
    Type: Grant
    Filed: April 10, 2006
    Date of Patent: February 2, 2010
    Assignee: Novartis AG
    Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
  • Publication number: 20100004461
    Abstract: The present invention relates to compounds containing organofluorochlorophosphate anions, the preparation thereof and the use thereof, in particular as ionic liquids.
    Type: Application
    Filed: December 7, 2007
    Publication date: January 7, 2010
    Applicant: MERCK PATENT GESELLSCHAFT
    Inventors: Nikolai Ignatyev, German Bissky, Helge Willner
  • Patent number: 7642264
    Abstract: The present invention relates to compounds of formula (Ia), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, R1, R2, R3 and R4 are as defined in the description and claims.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: January 5, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
  • Patent number: 7632840
    Abstract: A quinazoline derivative of the formula I: wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula I, are useful in the treatment of hyperproliferative disorders such as a cancer.
    Type: Grant
    Filed: January 31, 2005
    Date of Patent: December 15, 2009
    Assignee: AstraZeneca AB
    Inventors: Benedicte Delouvrie, Craig Steven Harris, Laurent Francois Andre Hennequin, Christopher Thomas Halsall, Janet Elizabeth Pease, Peter Mark Smith
  • Patent number: 7625900
    Abstract: Substituted tetrahydropyrrolopyrazine compounds corresponding to the formula I: processes for their preparation, pharmaceutical compositions comprising these compounds and the use of these compounds for the treatment and/or inhibition of pain and other disorders or disease states at least partly mediated by KCNQ2/3 K+ channels.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: December 1, 2009
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Thomas Christoph, Stefan Oberboersch, Klaus Schiene, Gregor Bahrenberg, Robert Frank, Sven Kuehnert, Wolfgang Schroeder
  • Publication number: 20090286976
    Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.
    Type: Application
    Filed: August 15, 2008
    Publication date: November 19, 2009
    Inventors: Hyun Joo Lee, Dong Jin Suh, Byoung Sung Ahn, Hong Gon Kim, Chang Soo Kim, Hoon Sik Kim
  • Publication number: 20090253912
    Abstract: The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium tetrafluoroborate.
    Type: Application
    Filed: November 18, 2005
    Publication date: October 8, 2009
    Inventors: Nikolai (Mykola) Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
  • Publication number: 20090253905
    Abstract: The invention relates to a method for producing onium salts comprising alkyl anions or aryl sulfonate anions or alkyl carboxylate anions or acryl carboxylate anions by reacting an onium halide with an alkyl silyl ester or trialkyl silyl ester of an alkyl sulfonic acid or aryl sulfonic acid or an alkyl carboxylic acid or aryl carboxylic acid or the anhydrides thereof.
    Type: Application
    Filed: November 18, 2005
    Publication date: October 8, 2009
    Inventors: Nikolai (Mykola) Ignatyev, Urs Weiz-Biermann, Andriy Kucheryna, Helge Willner
  • Patent number: 7595405
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: September 29, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
  • Publication number: 20090240066
    Abstract: The present invention provides intermediates needed for production of an optically active compound represented by formula (6), which enable the compound (6) to be readily synthesized in simple production steps without optical resolution, and also provides a process for producing the intermediates. A process for producing an optically active compound represented by formula (4): wherein R1 represents a protecting group for the amino group, or a salt thereof, characterized in that a reagent prepared from an titanium(IV) reagent and an alkylmetal compound is reacted with an optically active compound represented by formula (3): wherein R1 has the same meaning as defined above, if needed, in the presence of a Lewis acid.
    Type: Application
    Filed: April 24, 2009
    Publication date: September 24, 2009
    Applicant: DAIICHI PHARMACEUTICAL CO., LTD.
    Inventors: Masao FUJITA, Yutaka KITAGAWA, Makoto MUTO
  • Patent number: 7585885
    Abstract: The present invention provides BACE inhibitors of Formula I: methods for their use and preparation, and intermediates for their preparation.
    Type: Grant
    Filed: April 8, 2005
    Date of Patent: September 8, 2009
    Assignee: Eli Lilly and Company
    Inventors: Timothy Alan Shepherd, Isabel Rojo Garcia
  • Patent number: 7550589
    Abstract: Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: June 23, 2009
    Assignee: Hoffman-La Roche Inc.
    Inventors: Konrad Honold, Wolfgang Schaefer, Stefan Scheiblich
  • Publication number: 20090156824
    Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.
    Type: Application
    Filed: October 14, 2008
    Publication date: June 18, 2009
    Applicant: BOARD OF TRUSTEES OF UNIVERSITY OF ILLINOIS
    Inventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
  • Publication number: 20090101514
    Abstract: An objective of the present invention is to provide an electrodeposition method for metals using a molten salt, which easily enables the electrodeposition of various types of metals such as refractory metals and rare earth metals. In order to solve this problem, the invention is characterized in that it is effected at the electrodeposition temperature in a range of from 100° C. to 200° C.
    Type: Application
    Filed: September 5, 2006
    Publication date: April 23, 2009
    Applicant: KYOTO UNIVERSITY
    Inventors: Toshiyuki Nohira, Rika Hagiwara, Jun Shimano
  • Publication number: 20090060813
    Abstract: The present invention is directed to a new crystalline molecular sieve designated SSZ-82, a method for preparing SSZ-82 using a 1,6-bis(N-cyclohexylpyrrolidinium)hexane dication as a structure directing agent, and uses for SSZ-82.
    Type: Application
    Filed: October 10, 2008
    Publication date: March 5, 2009
    Applicant: Chevron U.S.A. Inc.
    Inventor: Allen W. Burton
  • Publication number: 20090045373
    Abstract: There are provided compounds represented by formula (I): in which R1 is F, Cl, —N(R5)2 or —CN and Q+ is selected among various organic cations that include an heterocyle. These compounds are useful as electrolytes, ionic liquids or molten salts.
    Type: Application
    Filed: March 9, 2007
    Publication date: February 19, 2009
    Inventors: Amer Hammami, Benoit Marsan
  • Publication number: 20090036628
    Abstract: The present invention relates to oxonium salts having [(Ro)3O]+ cations and sulfonium salts having [(Ro)3S]+ cations, where Ro denotes straight-chain or branched alkyl groups having 1-8 C atoms or phenyl which is unsubstituted or substituted by Ro, ORo, N(Ro)2, CN or halogen, and anions selected from the group of [PFx(CyF2y+1?zHz)6?x]? anions, where 2?x?5, 1?y?8 and 0?z?2y+1, or anions selected from the group of [BFn(CN)4?n]? anions, where n=0, 1 , 2 or 3, or anions selected from the group of [(Rf1SO2)2N]? anions or anions selected from the group of [BFwRf24?w]? anions, to processes for the preparation thereof, and to the use thereof, in particular for the preparation of ionic liquids.
    Type: Application
    Filed: January 5, 2007
    Publication date: February 5, 2009
    Inventors: Nikolai (Mykola) Ignatyev, German Bissky, Helge Willner
  • Publication number: 20080275003
    Abstract: The present invention relates to bis-cationic compounds comprising quaternary ammonium groups and/or quaternary phosphonium groups. The invention also relates to the use of bis-cationic compounds as Phospholipase B inhibitors and the use of bis cationic compounds for the treatment or prevention of microbial infection.
    Type: Application
    Filed: November 12, 2004
    Publication date: November 6, 2008
    Applicant: THE UNIVERSITY OF SYDNEY
    Inventors: Alfred Werner Widmer, Katrina Anne Jolliffe, Lesley Catherine Wright, Tania Christine Sorrell