Nitrigen Attached Directly To The Six-membered Hetero Ring Or To The Additional Hetero Ring By Nonionic Bonding Patents (Class 546/281.4)
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Patent number: 8088925Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.Type: GrantFiled: November 15, 2007Date of Patent: January 3, 2012Assignee: Sanofi-AventisInventors: Michael Wagner, Matthias Urmann, Volkmar Wehner, Martin Lorenz, Armin Bauer, Marc Nazare, Hans Matter
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Patent number: 8058271Abstract: Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurological, or proliferative diseases or disorders.Type: GrantFiled: May 10, 2007Date of Patent: November 15, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Jingrong Cao, Upul Bandarage, Jon Come, Craig Marhefka
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Publication number: 20110224225Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Patent number: 8013164Abstract: N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.Type: GrantFiled: February 16, 2010Date of Patent: September 6, 2011Assignee: Dow AgroScience LLCInventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers, Yuanming Zhu, James M. Renga, Vidyadhar B. Hegde, Joseph J. DeMark
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Publication number: 20110213156Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 represent an alkyl group, X represents —S—, —O— or —NH—, Y represents C or N, R3 represents hydrogen atom or a C1-10 alkyl group, Z represents —CO—N(R5)— (R5 represents hydrogen atom or a C1-6 alkyl group) or —C(R6)?C(R7)—CO—NH— (R6 and R7 represent hydrogen atom or a C1-6 alkyl group), Ar represents an aryldiyl group or a heteroaryldiyl group, and R4 represents —COOH, —OCH2—COOH, —CH2—COOH, or —CH2—CH2—COOH], which has a retinoid action and is useful as an active ingredient of a medicament.Type: ApplicationFiled: August 14, 2008Publication date: September 1, 2011Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Hideaki Muratake, Masayuki Noguchi, Koichi Shudo
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Publication number: 20110207698Abstract: The present application relates to novel heteroaryl-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: February 26, 2009Publication date: August 25, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Daniel Meibom, Alexandros Vakalopoulos, Barbara Albrecht-Küpper, Katja Zimmermann, Peter Nell, Frank Süßmeier
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Publication number: 20110112081Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: July 1, 2009Publication date: May 12, 2011Inventors: Kevin Wilson, Gabriela de Almeida, Andrew Haidle, Kaleen Konrad, Michelle Machacek, Ann Zabierek
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Patent number: 7932272Abstract: The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula —NH—C(?O)—, a group represented by the formula —C(?O)—NH—, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].Type: GrantFiled: September 27, 2004Date of Patent: April 26, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Kazutaka Nakamoto, Itaru Tsukada, Keigo Tanaka, Masayuki Matsukura, Toru Haneda, Satoshi Inoue, Norihiro Ueda, Shinya Abe, Katsura Hata, Naoaki Watanabe
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Publication number: 20110077237Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 1, 2010Publication date: March 31, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Guy W. Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
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Publication number: 20110077244Abstract: The present invention relates to synthetic studies of a novel thiophenediamine derivative having a urea structure and to finding pharmaceutical actions thereof. The present invention provides a compound represented by the following general formula (1) or a salt thereof. In the formula (1), R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, etc. R3 represents a hydroxy group, a lower alkoxy group which may have a substituent, a lower cycloalkyloxy group which may have a substituent, etc. R4 and R5 are the same or different and represent a halogen atom, a lower alkyl group, a hydroxy group, etc. X represents a lower alkylene group which may have a substituent, etc. Y represents a single bond or a lower alkylene group which may have a substituent, etc. W1-W2 represents N—CH, CH—N, etc. and l and m are the same or different and represent 0, 1, etc.Type: ApplicationFiled: May 25, 2009Publication date: March 31, 2011Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyaki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe
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Publication number: 20110077160Abstract: Compounds having the following generic formula are disclosed.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Inventors: Nneka T. Breaux, Michael R. Loso, Timothy C. Johnson, Jonathan M. Babcock, Benjamin M. Nugent, Timothy P. Martin, Annette V. Brown, Ronald Ross, JR., William C. Lo, Matthias S. Ober
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Publication number: 20110039892Abstract: The present invention aims to provide a compound having a superior selective ?1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: April 21, 2009Publication date: February 17, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masato Yoshida, Yasuhisa Kohara, Nobuki Sakauchi, Ayumu Sato
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Publication number: 20110024725Abstract: The present invention relates to a novel anthracene derivative and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent characteristics in efficiency, driving voltage, and life time.Type: ApplicationFiled: May 16, 2008Publication date: February 3, 2011Inventors: Dong-Hoon Lee, Jae-Chol Lee, Jae-Soon Bae, Jun-Gi Jang, Kong-Kyeom Kim, Dae-Woong Lee
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Publication number: 20110003826Abstract: This invention relates to new chemical compounds, application of these compounds as anticoagulants, pharmaceutical compositions, and plasma-substituting solutions on their basis, and can be used for treating thromboembolic complications of diseases such as myocardial infarction, stroke, and thrombosis of deep veins or a pulmonary artery; and for preventing hypercoagulation conditions in consequence of injuries, surgeries, sepsis, various obstetric pathologies, in disaster medicine, resuscitation, and so on.Type: ApplicationFiled: June 27, 2008Publication date: January 6, 2011Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyu "BioInventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
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Publication number: 20100331338Abstract: Novel compounds of the Formula (I) in which R1, R2, R3, and R4 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Type 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: February 2, 2009Publication date: December 30, 2010Applicant: Merck Patent GMBHInventors: Lars Burgdorf, Ulrich Emde, Johannes Gleitz, Norbert Beier, Christine Charon
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Patent number: 7855219Abstract: This invention relates to compounds of formula (I) in which the variable groups are as defined in the text and claims. A pharmaceutical composition and methods of using these materials in treatment of various conditions are also disclosed and claimed.Type: GrantFiled: February 20, 2002Date of Patent: December 21, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
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Publication number: 20100280036Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100267945Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Applicant: Shionogi & Co., Ltd.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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Publication number: 20100267774Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: formula (I) wherein: G is —N? or —CH?; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z—X1-L1-Y—NH—CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L1, and X1 are as defined in the specification; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 is the side chain of a natural or non-natural alpha amino acid.Type: ApplicationFiled: November 7, 2007Publication date: October 21, 2010Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Festus Charles Moffat, Stéphane Pintat, Stephen Davies
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Publication number: 20100234428Abstract: The invention relates to substituted 2-mercapto-3-aminopyridines, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRUNENTHAL GMBHInventors: Sven Kühnert, Beatrix Merla, Achim Kless, Gregor Bahrenberg, Wolfgang Schröder
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Publication number: 20100190777Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: PLEXXIKON INC.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Publication number: 20100174088Abstract: The present invention is an improved process for the preparation of a sodium/proton exchange inhibitor of sub-type 3 (NHE-3) useful in the treatment of sleep apnea and other related respiratory disorders.Type: ApplicationFiled: December 14, 2009Publication date: July 8, 2010Applicant: SANOFI-AVENTIS U.S. LLCInventors: Timothy Allen Ayers, Nakyen Choy, Harpal S. Gill, Andrea Hillegass, John J. Shay, JR., Volker Derdau
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Publication number: 20100152245Abstract: N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: February 16, 2010Publication date: June 17, 2010Inventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers, Yuanming Zhu, James M. Renga, Vidyadhar B. Hegde, Joseph J. DeMark
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Patent number: 7732452Abstract: The invention is concerned with novel substituted thiophene derivatives of formula (I) wherein R1 to R8, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.Type: GrantFiled: December 13, 2006Date of Patent: June 8, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Robert Narquizian, Constantinos G. Panousis
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Patent number: 7727981Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: October 25, 2007Date of Patent: June 1, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: 7700628Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).Type: GrantFiled: November 10, 2005Date of Patent: April 20, 2010Assignee: Eli Lilly and CompanyInventors: Ankush Baburao Argade, Theodore Goodson, Jr., David Kent Herron, Sajan Joseph, Salvatore Donato Lepore, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Anne Louise Tebbe, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 7683078Abstract: The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAr1 is a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ar2 a substituted or unsubstituted arylene or heteroarylene group; R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group.Type: GrantFiled: July 15, 2002Date of Patent: March 23, 2010Assignee: Laboratoires Serono S.A.Inventors: Thomas Rueckle, Jean-Pierre Gotteland, Russel J. Thomas, Marco Biamonte
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Patent number: 7678918Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are disclosed.Type: GrantFiled: December 6, 2007Date of Patent: March 16, 2010Assignees: 3M Innovative Properties Company, Graceway Pharmaceuticals, LLCInventors: John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
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Publication number: 20100056578Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: ApplicationFiled: November 11, 2009Publication date: March 4, 2010Applicant: DOW AGROSCIENCES LLCInventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
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Publication number: 20100022594Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.Type: ApplicationFiled: October 9, 2009Publication date: January 28, 2010Applicants: Wyeth, ArQule, Inc.Inventors: Anthony F. Kreft, Derek Cecil Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
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Publication number: 20090281145Abstract: The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.Type: ApplicationFiled: May 7, 2009Publication date: November 12, 2009Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
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Publication number: 20090227799Abstract: Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula —C(?O)—NH— or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.Type: ApplicationFiled: August 8, 2005Publication date: September 10, 2009Inventors: Kazutaka Nakamoto, Masayuki Matsukura, Keigo Tanaka, Satoshi Inoue, Itaru Tsukada, Toru Haneda, Norihiro Ueda, Shinya Abe, Koji Sagane
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Publication number: 20090215828Abstract: Substituted indole derivatives, processes for the preparation thereof, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted indole derivatives to treat pain and other conditions and for other medical purposes.Type: ApplicationFiled: February 19, 2009Publication date: August 27, 2009Applicant: GRUNENTHAL GMBHInventors: Stefan Schunk, Stefan Oberborsch, Werner Englberger, Bernd Sunderman
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Publication number: 20090215829Abstract: The invention relates to thiophene carboxamides of formula (I), wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 4, 2009Publication date: August 27, 2009Inventors: Andrew David Morley, Jeffrey Philip POYSER
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Publication number: 20090209554Abstract: The present invention provides N-3?-pyridyl-methyl or N-2?-pyrazinylmethyl thiazolium derivatives of formula (I) which are useful as transketolase inhibitors wherein R1, R2, R3, Y, R5-R9, Ra-Rd, n and X? are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.Type: ApplicationFiled: March 23, 2005Publication date: August 20, 2009Applicant: ARRAY BIOPHARMA INC.Inventors: Steven A. Boyd, Kevin R. Condroski, Jason De Meese, Stephen S. Gonzales, Indrani W. Gunawardana, Tomas Kaplan, Yvan Le Huerou, Joseph Lyssikatos, Todd T. Romoff, Francis X. Sullivan, Allen Thomas
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Publication number: 20090131411Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: October 25, 2007Publication date: May 21, 2009Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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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: 20090069305Abstract: The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H4 receptor activity modulation and the treatment of states mediated by histamine H4 receptor activity.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Inventors: Michael D. Gaul, Bao-Ping Zhao, Xizhen Zhu
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Publication number: 20090062267Abstract: The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: January 29, 2008Publication date: March 5, 2009Applicant: ASTRAZENECA ABInventors: Jean-Claude Arnould, Benedicte Delouvrie, Christine Marie Paul Lambert-Van Der Brempt
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Publication number: 20090054396Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.Type: ApplicationFiled: September 8, 2008Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Susan Ashwell, Thomas Gero, Stephanos Ioannidis, James Janetka, Paul Lyne, Vibha Oza, Mei Su, Dingwei Yu, Stephanie Springer
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Publication number: 20090042227Abstract: Amino(oligo)thiophene dyes useful for studying the electrophysiology of organelles, cells, and tissues are described. Compared to previously known dyes, the amino(oligo)thiophene dyes exhibit improved (faster) response to membrane potential changes, as well as the ability to be excited by 1064 nanometer femtosecond pulses. Methods of preparing the amino(oligo)thiophene dyes are also described.Type: ApplicationFiled: July 30, 2008Publication date: February 12, 2009Inventors: Leslie M. Loew, Ping Yan
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Publication number: 20080312161Abstract: The invention relates to novel compounds with formula I and their use in stabilization of Factor Vila or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.Type: ApplicationFiled: February 24, 2006Publication date: December 18, 2008Inventors: Anders Klarskov Petersen, Andrew Neil Bowler
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Patent number: 7435743Abstract: Pyrimidine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 30, 2005Date of Patent: October 14, 2008Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshiro, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuiyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Publication number: 20080108666Abstract: N-Substituted heteroaryl (substituted)alkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: February 9, 2007Publication date: May 8, 2008Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Gregory T. Whiteker, Nneka T. Breaux, John F. Daeuble
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Publication number: 20070299264Abstract: N-Substituted sulfoximines are effective at controlling insects resistant to common insecticides.Type: ApplicationFiled: February 9, 2007Publication date: December 27, 2007Inventors: Jim X. Huang, Richard B. Rogers, Nailah Orr, Thomas C. Sparks, James M. Gifford, Michael R. Loso, Yuanming Zhu, Thomas Meade
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Patent number: 7291580Abstract: 4-Aminopicolinic acids having (1,1-difluoroalkyl) substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: August 4, 2004Date of Patent: November 6, 2007Assignee: Dow AgroSciences LLCInventors: Terry William Balko, Stephen Craig Fields, Nicholas Martin Irvine, Christian Thomas Lowe, Paul Richard Schmitzer
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7125896Abstract: The invention relates to thiophene carboxanmides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: July 19, 2002Date of Patent: October 24, 2006Assignee: AstraZeneca ABInventors: Alan Faull, Craig Johnstone, Andrew Morley, Philip Jeffrey Poyser
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Patent number: 7084159Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative o thereof, wherein A, B, Ra, R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; Lck and Src kinase. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: May 14, 2003Date of Patent: August 1, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jingrong Cao, Jeremy Green, Young-Choon Moon, Jian Wang, Mark Ledeboer, Edmund Harrington, Huai Gao
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Patent number: 6989398Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: GrantFiled: February 2, 2004Date of Patent: January 24, 2006Assignee: ICAgen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden