Acyclic Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/116)
  • Patent number: 10421740
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: September 24, 2019
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Michel Muehlebach, Andrew Edmunds, Girish Rawal, Vikas Sikervar, Jagadish Pabba
  • Patent number: 10099981
    Abstract: Provided are methods for the meta-selective C—H arylations of arene alcohol-based substrates. The methods combine the transient norbornene strategy with a quinoline-based acetal scaffold to achieve the formation of biaryl compounds. These processes establish a foundation for catalytic polyfunctionalization of alcohol-based compounds. The method comprises attaching a heterocyclic hemiacetal scaffold to an aromatic alcohol or a substituted aromatic alcohol; reacting the aromatic or substituted aromatic alcohol having the heterocyclic hemiacetal scaffold attached with an alkyl or aryl iodide in a reaction mix comprising a palladium catalyst, a silver salt, and carboxymethyl norbornene to generate a meta-arylated arene conjugated to the heterocyclic hemiacetal scaffold; and then cleaving the heterocyclic hemiacetal scaffold from the meta-arylated arene alcohol.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: October 16, 2018
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Eric Ferreira, Qiankun Li
  • Patent number: 10087194
    Abstract: Provided herein are compounds, compositions, and methods for treating cancer in a subject in need thereof.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: October 2, 2018
    Assignees: California Pacific Medical Center, Catholic Healthcare West
    Inventor: Li-Xi Yang
  • Patent number: 10005719
    Abstract: A method of preparing ortho-alkenyl and ortho-acetyl benzylic alcohols is disclosed.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: June 26, 2018
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Eric Ferreira, Brian J Knight, Qiankun Li
  • Patent number: 9185786
    Abstract: An apparatus for producing light includes a chamber and an ignition source that ionizes a gas within the chamber. The apparatus also includes at least one laser that provides energy to the ionized gas within the chamber to produce a high brightness light. The laser can provide a substantially continuous amount of energy to the ionized gas to generate a substantially continuous high brightness light.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: November 10, 2015
    Assignee: Energetiq Technology, Inc.
    Inventor: Donald K. Smith
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150111894
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
  • Patent number: 9012643
    Abstract: Hydroxamate substituted azaindoline cyanine dyes, conjugates thereof and methods of using the same are provided. The subject cyanine dyes include an azaindoline ring having a hydroxamate substituent. The dyes may further include a reactive group moieties (RGM) and/or a water soluble group. Also provided are conjugates of the subject dyes. Also provided are tandem conjugates including a fluorescent protein capable of energy transfer to the dye. Methods of detecting an analyte in a sample by contacting the sample with a detection reagent are provided. The detection agent may be a dye-conjugate that specifically binds the analyte, or may be a reactive dye which conjugates to the analyte. Also provided are compositions, e.g., kits, etc., incorporating such dyes which facilitate use in such methods.
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: April 21, 2015
    Assignee: Becton, Dickinson and Company
    Inventors: Zhenjun Diwu, Haitao Guo, Xing Han, Mirion Schultz, Timothy Dubrovsky
  • Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Patent number: 9006440
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and/or systemic lupus.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Patent GmbH
    Inventors: Lars Burgdorf, Melanie Schultz, Tatjana Ross, Brian Hodous, Justin Potnick, Amanda E. Sutton, Bayard R. Huck
  • Publication number: 20150087672
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 26, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
  • Publication number: 20150080377
    Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a
    Type: Application
    Filed: August 31, 2013
    Publication date: March 19, 2015
    Inventor: Daljit Singh Dhanoa
  • Publication number: 20150065501
    Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Patent number: 8957211
    Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: February 17, 2015
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • Publication number: 20150025070
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 22, 2015
    Applicant: Novartis AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
  • Patent number: 8937053
    Abstract: Disclosed herein are a process or method for the preparation of prasugrel and several novel crystalline forms of prasugrel hydrochloride. The process comprises preparation of prasugrel by acetylation in solvents which have low boiling point and/or low toxicity, and the process not only avoids using solvents which have high boiling point and/or high toxicity such as toluene, acetonitrile and so on, but also resolves the problem about thermal instability of prasugrel, and the loss of prasugrel is reduced, as well as the yield is raised. The yield of prasugrel is higher than 85% and the purity is higher than 99.5%. The process can prepare prasugrel and its pharmaceutically acceptable salts. The novel crystalline forms of prasugrel hydrochloride are crystalline form H1, H2 and H3, and their performance in oral absorbability, activating metabolism and inhibiting platelet aggregation is excellent.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: January 20, 2015
    Assignees: Sunshine Lake Pharma Co., Ltd., Yichang Changjiang Pharmaceutical Co., Ltd.
    Inventors: Lijun Li, Hailong Wang, Zhongqing Wang
  • Publication number: 20140378493
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Patent number: 8916571
    Abstract: The invention relates to the treatment of cancer using an inhibitor of 5?-methylthioadenosine phosphorylase (MTAP). The invention particularly relates to the treatment of prostate cancer and head and neck cancer.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: December 23, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Chandan Guha
  • Patent number: 8907093
    Abstract: Carboxylic acid derivatives having an oxazolo[4,5-c]pyridine ring The invention therefore relates to compounds of the formula I in which X, Y, R1, R2 and R3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: December 9, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Thomas Huebschle, Katrin Hiss
  • Patent number: 8871738
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Publication number: 20140275156
    Abstract: There is provided now flavonoid compounds, compositions containing these compounds, methods for their synthesis, and uses of these compounds. In particular, there is provided methods of preventing and or mitigating the damage caused by cell apoptosis or cell necrosis by administration of the novel flavonoid compounds. In some aspects, there is provided methods for inhibiting pro-apoptotic signalling kinases activity in a subject while regulating and activating extracelluar signal regulated kinase (ERK).
    Type: Application
    Filed: August 13, 2012
    Publication date: September 18, 2014
    Applicant: NEUPROTECT PTY LTD
    Inventor: Grant McLachlan
  • Publication number: 20140249170
    Abstract: The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial FabI and can be used for the treatment of Staphylococcal infections.
    Type: Application
    Filed: September 18, 2012
    Publication date: September 4, 2014
    Inventors: Radha Rangarajan, Rajinder Kumar, BV Prabhakar, P Chandrasekhar, P Mallikarjuna, Ankita Banerjee
  • Publication number: 20140243310
    Abstract: 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: Application
    Filed: October 23, 2012
    Publication date: August 28, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tohru Yamashita, Takuya Fujimoto, Ryo Mizojiri, Kazuko Yonemori, Hideki Hirose, Zenichi Ikeda, Ikuo Fujimori, Kyoko Toyofuku, Tsuneo Yasuma, Nobuyuki Matsunaga
  • Patent number: 8809535
    Abstract: Substituted pyridines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: August 19, 2014
    Assignee: BASF SE
    Inventors: Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska-Pianowska, Anja Simon, Ruediger Reingruber, Helmut Kraus, Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Hans Wolfgang Hoeffken, Thomas Mietzner
  • Publication number: 20140228320
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):
    Type: Application
    Filed: April 15, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
  • Patent number: 8796328
    Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, prodrugs, or combinations thereof, wherein X1, L, Rx, Ry, Rz, R1, R2, A, m, n, p, q, and r are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: August 5, 2014
    Inventors: Arthur Gomtsyan, Jerome Daanen, Michael E. Kort, Philip R. Kym, Eric A. Voight, Kevin R. Woller
  • Publication number: 20140206873
    Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 24, 2014
    Applicant: BASF SE
    Inventors: Frederik MENGES, Joachim GEBHARDT, Michael RACK, Michael KEIL, Rodney F. KLIMA, David CORTES, Robert LEICHT, Helmut ZECH, Jochen SCHROEDER
  • Publication number: 20140194462
    Abstract: The present application is related to compounds represented by Formula I, which are novel allosteric modulators of ?7nAChR. The application also discloses the treatment of disorders that are responsive to modulation of acetylcholine action on ?7nAChR in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: October 8, 2013
    Publication date: July 10, 2014
    Applicant: Anvyl LLC
    Inventor: Richard Kanner
  • Patent number: 8759341
    Abstract: This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: June 24, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Mario Lobell, Nicole Teusch, Shendong Yuan
  • Patent number: 8742106
    Abstract: The invention relates to compound of the formula (I?) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: June 3, 2014
    Assignee: Novartis AG
    Inventors: Sangamesh Badiger, Dirk Behnke, Claudia Betschart, Vinod Chaudhari, Murali Chebrolu, Simona Cotesta, Samuel Hintermann, Arndt Meyer, Chetan Pandit
  • Patent number: 8722661
    Abstract: There are provided compounds of the formula (I) wherein Q, R1 and R2 are defined herein. The compounds have activity as anticancer agents.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: May 13, 2014
    Assignees: Hoffmann-La Roche Inc., Genentech, Inc.
    Inventors: Nancy-Ellen Haynes, Johannes Hermann, Kyungjin Kim, Nathan Robert Scott, Lin Yi, Mark Zak
  • Publication number: 20140128365
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 8, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
  • Publication number: 20140113824
    Abstract: Bicyclic (thio)carbonylamidines of the formula (I) in which Q, B, Y, R1 and A are as defined in the description their preparation and their use for controlling plant pests and pests encountered in veterinary medicine.
    Type: Application
    Filed: May 7, 2012
    Publication date: April 24, 2014
    Inventors: Peter Jeschke, Michael Schindler, Katharina Wölfel, Ulrich Ebbinghaus-Kintscher, Arnd Voerste, Olga Malsam, Peter Losel, Ulrich Görgens
  • Patent number: 8680276
    Abstract: The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: March 25, 2014
    Inventors: Riccardo Motterle, Giancarlo Arvotti, Elisabetta Bergantino, Andrea Castellin, Stefano Fogal, Marco Galvagni
  • Patent number: 8680089
    Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 25, 2014
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
  • Publication number: 20140080804
    Abstract: The invention provides novel substituted 6-arylamino pyridone carboxamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, poly-morph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.
    Type: Application
    Filed: November 1, 2011
    Publication date: March 20, 2014
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Shixin Wang, Rong Yu, Wei Hu, Zhi Liang, Xijie Liu, Quan Hu
  • Patent number: 8637542
    Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PB kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: January 28, 2014
    Assignee: Intellikine, Inc.
    Inventors: Yi Liu, Pingda Ren, Liansheng Li, Katrina Chan, Troy Edward Wilson
  • Publication number: 20140024659
    Abstract: The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: BASF SE
    Inventors: Ralph Paulini, Carsten Beyer, Henricus Maria Martinus Bastiaans, Nancy B. Rankl
  • Patent number: 8629279
    Abstract: A process for manufacturing a 5-formyl-pyridine-2,3-dicarboxylic acid ester (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro and R1, R2 are independently C1-C10-alkyl, comprising the steps of (i) reacting a compound of formula (II), wherein the symbols are as in formula (I), with a nitrosation agent (III) R3—O—N?O (III) wherein R3 is C1-C8-alkyl, in the presence of an alkali metal or alkaline earth metal alcoholates or carbonates in a polar aprotic solvent at a temperature of from ?45 to 40° C., to obtain an oxime compound (IV) where Z, Z1, R1 and R2 are as in formula (I), and (ii) reacting oxime compound (IV) with an aliphatic C1-C10-aldehyde in the presence of a Lewis acid at a temperature in the range of from 0 to 100° C. The compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: January 14, 2014
    Assignee: BASF SE
    Inventors: Michael Rack, Joachim Gebhardt, Frederik Menges, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
  • Patent number: 8609686
    Abstract: The present application relates to novel substituted pyrrolopyridine, pyrazolopyridine and isoxazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: December 17, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Peter Nell, Alexandros Vakalopoulos, Frank Süβmeier, Barbara Albrecht-Küpper, Katja Zimmerman, Joerg Keldenich, Daniel Meibom
  • Patent number: 8609648
    Abstract: 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.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: December 17, 2013
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
  • Patent number: 8604028
    Abstract: This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: December 10, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Martin Michels, Hans Briem, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Publication number: 20130303550
    Abstract: Compounds of formula (IIc); wherein X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different; Y1, Y2, Y3 and Y4 independently from each other are N or CR9 wherein R9 may be same or different and wherein up to 3 of the group Y1, Y2, Y3 and Y4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.
    Type: Application
    Filed: November 11, 2011
    Publication date: November 14, 2013
    Applicants: Ruprecht-Karls-Universitat Heidelberg, Deutsches Krebsforschungszentrum
    Inventors: Michael Boutros, Rajendra-Prasad Maskey, Corinna Koch, Florian Fuchs, Sandra Steinbrink, Daniel Gilbert
  • Patent number: 8580956
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: November 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
  • Publication number: 20130296344
    Abstract: Compounds according to the general formula (I) wherein X1, X2, X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different, and wherein up to 3 of the group X1, X2, X3 and X4 may be N; A is a 5- or 6-membered aromatic or heteroaromtic cycle containing 1 to 3 heteroatoms selected from the group consisting of N, O and S wherein A may be substituted by 1 to 5 substituents R which may be same or different; their solvates, hydrates, and pharmaceutically acceptable salts for the treatment of a disorder or disease associated with an aberrant activation of Wnt signalling in a mammal selected from a cell proliferative disorder, rheumatoid arthritis, increased bone density, aging or age-related disorders and/or diseases or Dupuytren disease (superficial fibromatosis).
    Type: Application
    Filed: November 11, 2011
    Publication date: November 7, 2013
    Applicants: Ruprecht-Karls-Universitat Heidelberg, Deutsches Krebsforschungszentrum
    Inventors: Michael Boutros, Rajendra-Prasad Maskey, Corinna Koch, Florian Fuchs, Sandra Steinbrink, Daniel Gilbert
  • Patent number: 8546376
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: October 1, 2013
    Assignee: Almac Discovery Limited
    Inventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
  • Publication number: 20130252943
    Abstract: In one aspect, the invention relates to substituted bicyclic oxazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: February 27, 2013
    Publication date: September 26, 2013
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, María Luz Martín-Martín
  • Publication number: 20130225569
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: July 29, 2011
    Publication date: August 29, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Lars Burgdorf, Melanie Schultz, Tatjana Ross, Brian Hodous, Justin Potnick, Amanda E. Sutton, Bayard R. Huck
  • Publication number: 20130210768
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Application
    Filed: June 6, 2011
    Publication date: August 15, 2013
    Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif