Carbonyl Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/314)
  • Patent number: 10081616
    Abstract: The present invention features compounds having soluble epoxide hydrolase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cardiovascular diseases, respiratory diseases, inflammation, and diabetes.
    Type: Grant
    Filed: August 26, 2015
    Date of Patent: September 25, 2018
    Inventors: Ying Zhang, Anthony D. Keefe, Christoph Dumelin
  • Patent number: 9512078
    Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.
    Type: Grant
    Filed: September 1, 2015
    Date of Patent: December 6, 2016
    Assignee: PAION UK LIMITED
    Inventors: Gary Stuart Tilbrook, Andreas Schumacher, Rene Emmenegger
  • Patent number: 9072788
    Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: July 7, 2015
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
  • Patent number: 9040709
    Abstract: The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: May 26, 2015
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Markus Jachmann, Takayuki Wakamatsu, Mitsuharu Anryu
  • Patent number: 9028854
    Abstract: A pesticidal composition comprising 4-phenoxyphenyl 2-(2-pyridyloxy)propyl ether; a hydrophobic organic solvent capable of dissolving 0.1-fold by weight of 4-phenoxyphenyl 2-(2-pyridyloxy)propyl ether at 0° C.; polyvinyl alcohol; a nonionic surfactant selected from the group consisting of alkoxylated castor oil, alkoxylated hydrogenated castor oil and alkoxylated hydrogenated castor oil fatty acid ester; and water, is excellent in storage stability.
    Type: Grant
    Filed: December 13, 2005
    Date of Patent: May 12, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Toshiyuki Tanedani
  • Patent number: 9029559
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: May 12, 2015
    Assignee: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
  • Publication number: 20150045397
    Abstract: The invention relates to substituted pyridine and pyrimidine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1, R2a, R2b, A1, A2, X, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: March 15, 2013
    Publication date: February 12, 2015
    Inventors: Laykea Tafesse, Jiangchao Yao
  • Patent number: 8937182
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Grant
    Filed: April 18, 2011
    Date of Patent: January 20, 2015
    Assignee: Metabolic Solutions Development Company, LLC
    Inventors: James R. Zeller, Steven P. Tanis, Scott D. Larsen, Timothy Parker
  • Patent number: 8937091
    Abstract: The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3: wherein R1 is a substituted or unsubstituted aryl or heterocyclyl group, R2, R3, and R4 are hydrogen atoms, n is 2, X is halogen, R5 and R6 independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R5 and R6 are not hydrogen atoms at the same time, or R5 and R6 may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: January 20, 2015
    Assignee: Japan Science and Technology Agency
    Inventors: Katsuhiko Mikoshiba, Kozo Hamada, Akiko Terauchi, Shouichirou Ozaki, Jun-ichi Goto, Etsuko Ebisui, Akinobu Suzuki
  • Patent number: 8889719
    Abstract: The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: November 18, 2014
    Assignee: Merck Patent GmbH
    Inventors: Andreas Goutopoulos, Henry Yu, Benny C. Askew, Jr., Lesley Liu-Bujalski
  • Patent number: 8871981
    Abstract: A method for oxidizing an alcohol, wherein oxidation is performed in the presence of a compound represented by the following formula (I) and a bulk oxidant, which enables efficient oxidation of secondary alcohols as well as primary alcohols, and can attain high reaction efficiency even when air is used as a bulk oxidant.
    Type: Grant
    Filed: May 30, 2011
    Date of Patent: October 28, 2014
    Assignee: Tohoku University
    Inventors: Yoshiharu Iwabuchi, Masaki Hayashi
  • Patent number: 8841459
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: September 23, 2014
    Assignee: Merck Serono SA
    Inventors: Holger Deppe, Matthias Schwarz, Ulrich Abel, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Xuliang Jiang
  • Publication number: 20140275543
    Abstract: A method for stabilization of potent alkanone-heterocyclic flavorants in dry powder form is provided. Coordination of alkanone-heterocyclic flavorants to transition metal salts results in the formation of stable crystalline complexes, which upon hydration release the free flavorant. Food and topping products containing the stabilized alkanone-heterocyclic flavorant are provided as are methods for stabilizing the alkanone-heterocyclic flavorant.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Keith R. Cadwallader, Ming-Chih Fang
  • Publication number: 20140243349
    Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Application
    Filed: February 21, 2014
    Publication date: August 28, 2014
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Publication number: 20140231729
    Abstract: A negative-type photosensitive resin composition capable of forming a pattern having favorable adhesiveness at a low light exposure; a pattern forming method using the resin composition; a cured film, an insulating film, a color filter formed using resin composition; and a display device provided with the cured film, insulating film, or color filter. The resin composition contains a compound represented by the following formula (1). In the formula, R1 and R2 each independently indicate a hydrogen atom or an organic group, but at least one indicates an organic group. R1 and R2 may be bonded to form a ring structure and may contain a hetero atom bond. R3 indicates a single bond or an organic group. R4 to R9 each independently indicate a hydrogen atom, an organic group, etc., but R6 and R7 are never hydroxyl groups. R10 indicates a hydrogen atom or an organic group.
    Type: Application
    Filed: June 15, 2012
    Publication date: August 21, 2014
    Applicant: TOKYO OHKA KOGYO CO., LTD.
    Inventors: Dai Shiota, Mayumi Kuroko, Kunihiro Noda, Yoshinori Tadokoro
  • Publication number: 20140228579
    Abstract: The present application relates to methods for the catalytic reduction of acid chlorides and/or imidoyl chlorides. The methods comprise reacting the acid chloride or imidoyl chloride with a silane reducing agent in the presence of a catalyst such as [Cp(Pri3P)Ru(NCMe)2]+[PF6]?.
    Type: Application
    Filed: September 11, 2013
    Publication date: August 14, 2014
    Applicant: Brock Unviersity
    Inventors: Georgii Nikonov, Dmitry Gutsulyak, Sun Hwa Lee
  • Publication number: 20140171444
    Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.
    Type: Application
    Filed: March 3, 2014
    Publication date: June 19, 2014
    Applicant: THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
  • Patent number: 8754110
    Abstract: Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenyl-boronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. The organic phase and the aqueous phase are separated. The 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate, which is deacetylated to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 17, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Jossian Oppenheimer, Mark V. M. Emonds, Christopher W. Derstine, Robert C. Clouse
  • Patent number: 8741927
    Abstract: The present invention relates to a novel method for preparing a compound of formula (2) as the intermediate, which can be effectively used for preparation of a compound of formula (1) exhibiting good inhibitory activity against dipeptidyl peptidase IV enzyme.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: June 3, 2014
    Assignee: LG Life Sciences Ltd.
    Inventors: Bong Chan Kim, Kyu Young Kim, Hee Bong Lee, Ji Eun An, Kyu Woong Lee
  • Patent number: 8741261
    Abstract: Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
    Type: Grant
    Filed: March 22, 2005
    Date of Patent: June 3, 2014
    Assignee: GE Healthcare Limited
    Inventors: Bengt Langstrom, Julien Barletta, Hisashi Doi, Masaaki Suzuki, Ryoji Noyori, Yasuyoshi Watanabe, Farhad Karimi
  • Patent number: 8729095
    Abstract: A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ?CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: May 20, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tatsuya Nishi, Masashi Hasegawa, Yumi Nakamoto, Yuichi Ochiai, Ryoko Kitazawa, Hiroshi Susaki
  • Patent number: 8722895
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: May 13, 2014
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Richard M. Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
  • Patent number: 8710234
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: April 29, 2014
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Patent number: 8669370
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: March 11, 2014
    Assignee: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
  • Patent number: 8653277
    Abstract: It is to provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: February 18, 2014
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Hisaya Nishide, Shigeyuki Nishimura, Shigeru Mitani, Koji Minamida, Fumio Kanamori, Munekazu Ogawa, Shigehisa Kanbayashi, Toyoshi Tanimura, Koji Higuchi, Hidemasa Kominami, Tomohiro Okamoto, Akihiro Nishimura
  • Patent number: 8653276
    Abstract: The present invention is directed to compounds of the general formula: as defined herein, and pharmaceutical compositions thereof. The invention is also directed to their therapeutic use as urotensin II receptor antagonists, e.g., in the treatment of cardiac, coronary, and central nervous system disorders. In particular embodiments, the invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: February 18, 2014
    Assignee: SANOFI
    Inventors: Jean-Michel Altenburger, Valerie Fossey, Daniel Galtier, Frederic Petit
  • Publication number: 20140031558
    Abstract: Provided herein are fluoropicolinoyl fluorides and processes for their preparation. In some embodiments, provided herein is a process for the preparation of 5-fluoro-6-aryl-picolinoyl fluorides from chloropicolinoyl chlorides.
    Type: Application
    Filed: July 23, 2013
    Publication date: January 30, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: James M. Renga, Yang Cheng, Joseck M. Muhuhi, David E. Podhorez, Gary A. Roth, Scott P. West, Gregory T. Whiteker, Yuanming Zhu
  • Publication number: 20140018542
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 16, 2014
    Applicant: Metabolic Solutions Development Company, LLC
    Inventors: Timothy Parker, Robert C. Gadwood, Steven P. Tanis, Scott D. Larsen, James R. Zeller
  • Patent number: 8623942
    Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: January 7, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
  • Publication number: 20130303466
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: November 14, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley, Alain D. Baron
  • Patent number: 8563736
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: October 22, 2013
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Publication number: 20130267708
    Abstract: Provided are a process for preparing an N ortho acyl substituted nitrogen-containing heterocyclic compound and an aminal iron (II) complex thereof, and the use of the complexes obtained by the process in an olefin oligomerization catalyst. The N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is for example 2-acyl-1,10-phenanthroline or 2,6-diacetyl pyridine as shown in formula b, and the N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is produced by a reaction of a precursor thereof in a substituted or unsubstituted nitrobenzene. Preferably the precursor shown in formula I in the present invention is produced by 1,10-phenanthroline reacting with trialkyl aluminum, or a halogenoalkyl aluminum RnAlXm, or a substituted or unsubstituted benzyl lithium 2Li, followed by hydrolysis.
    Type: Application
    Filed: December 1, 2011
    Publication date: October 10, 2013
    Inventors: Jun Liu, Mingfang Zheng, Weizhen Li, Haiying Zhang, Huaijie Wang, Yu Zhou, Tonglin Li, Lan Zhao, Hongfei Wu, Wingjun Xie, Chunhong Wu, Zhiguang Jia, Qi Yanping, Jilong Wang
  • Patent number: 8552201
    Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: October 8, 2013
    Assignee: Sanofi
    Inventors: Jean-Michel Altenburger, Valérie Fossey, Philip Janiak, Gilbert Lassalle, Frédéric Petit, Jean Claude Vernieres
  • Patent number: 8541590
    Abstract: The invention provides boronic esters of Formula I wherein R1, R2, R3, and R4 are as described herein, and methods for the preparation and purification thereof.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: September 24, 2013
    Assignee: Cephalon, Inc.
    Inventor: Renee Caroline Roemmele
  • Publication number: 20130245127
    Abstract: A compound of formula (I) R-L-CO—X ??(I) (wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds; L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO; and X is an electron withdrawing group) for use in the treatment of rheumatoid arthritis.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 19, 2013
    Applicant: Avexxin AS
    Inventors: Astrid Jullumstro Feuerherm, Berit Johansen
  • Patent number: 8524911
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: September 3, 2013
    Assignee: Merck Serono SA
    Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
  • Patent number: 8519143
    Abstract: The present invention relates to derivatives of ((phenyl)-3,6-dihydropyridin-1-yl)(bridged piperazinyl)-1-alkanone derivatives and ((phenyl)-2,5-dihydropyrrol-1-yl) (bridged piperazinyl)-1-alkanone corresponding to Formula (I): in which the variables are as defined herein, to the preparation thereof and to the therapeutic use thereof.
    Type: Grant
    Filed: May 17, 2012
    Date of Patent: August 27, 2013
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart
  • Publication number: 20130211095
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: August 15, 2013
    Applicant: Metabolic Solutions Development Company, LLC
    Inventors: Timothy Parker, Robert C. Gadwood, Steven P. Tanis, Scott D. Larsen, James R. Zeller
  • Publication number: 20130204004
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: August 8, 2013
    Applicant: Metabolic Solutions Development Company, LLC
    Inventors: James R. Zeller, Steven P. Tanis, Scott D. Larsen, Timothy Parker
  • Publication number: 20130172543
    Abstract: A method for oxidizing an alcohol, wherein oxidation is performed in the presence of a compound represented by the following formula (I) and a bulk oxidant, which enables efficient oxidation of secondary alcohols as well as primary alcohols, and can attain high reaction efficiency even when air is used as a bulk oxidant.
    Type: Application
    Filed: May 30, 2011
    Publication date: July 4, 2013
    Applicant: TOHOKU UNIVERSITY
    Inventors: Yoshiharu Iwabuchi, Masaki Hayashi
  • Patent number: 8455654
    Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: June 4, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Patent number: 8410155
    Abstract: The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, R3, R4, R8a, R11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: April 2, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Donald J. P. Pinto
  • Patent number: 8404725
    Abstract: The invention provides novel substituted phenylamino isonicotinamide compounds (I), pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined in the specification. Said compounds are MEK inhibitors useful in the treatment of hyperproliferative diseases related to the hyperactivity of MEK, such as restenosis, as well as diseases modulated by the MEK cascade, such as cancer and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: March 26, 2013
    Assignee: Merck Patent GmbH
    Inventors: Andreas Goutopoulos, Henry Yu, Benny C. Askew, Jr., Lesley Liu-Bujalski
  • Publication number: 20120323014
    Abstract: A method for producing an ?-acyloxycarbonyl compound of the present invention includes performing an intermolecular reaction between a carboxylic acid and a carbonyl compound selected from the group consisting of ketones, aldehydes, and esters, which have a hydrogen atom at the ?-position, using a hydroperoxide as an oxidizer and an iodide salt as a catalyst precursor, thereby introducing an acyloxy group derived from the carboxylic acid into the ?-position of the carbonyl compound.
    Type: Application
    Filed: March 4, 2011
    Publication date: December 20, 2012
    Applicants: MITSUBISHI RAYON CO., LTD., National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Muhammet Uyanik
  • Publication number: 20120289518
    Abstract: The present invention relates to derivatives of 4-{2-[phenyl-3,6-dihydropyridin-1-yl]-2-oxoalkyl}-1-piperazin-2-one and 4-{2-[phenyl-2,5-dihydropyrrol-1-yl]-2-oxoalkyl}-1-piperazin-2-one having general formula (I): in which A, B, m, R3 and n are as defined herein. The invention also relates to the preparation thereof and to the therapeutic use thereof.
    Type: Application
    Filed: July 24, 2012
    Publication date: November 15, 2012
    Applicant: SANOFI
    Inventors: Marco BARONI, Francoise BONO, Sandrine DELBARY-GOSSART
  • Publication number: 20120232279
    Abstract: The invention concerns processes for oxidizing an alcohol to produce a carbonyl compound. The processes comprise contacting the alcohol with (i) a gaseous mixture comprising oxygen; and (ii) an amine compound in the presence of a catalyst, having the formula: where each of R1-R12 are independently H, alkyl, aryl, CF3, halogen, OR13, SO3R14, C(O)R15, CONR16R17 or CO2R18; each of R13-R18 is independently alkyl or aryl; and Z is alkl or aryl.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 13, 2012
    Applicant: LOS ALAMOS NATIONAL SECURITY, LLC
    Inventors: Susan Kloek Hanson, Louis A. Silks, Ruilian Wu
  • Publication number: 20120232280
    Abstract: The present invention relates to derivatives of ((phenyl)-3,6-dihydropyridin-1-yl)(bridged piperazinyl)-1-alkanone derivatives and ((phenyl)-2,5-dihydropyrrol-1-yl) (bridged piperazinyl)-1-alkanone corresponding to Formula (I): in which the variables are as defined herein, to the preparation thereof and to the therapeutic use thereof.
    Type: Application
    Filed: May 17, 2012
    Publication date: September 13, 2012
    Applicant: SANOFI-AVENTIS
    Inventors: Marco BARONI, Françoise BONO, Sandrine DELBARY-GOSSART
  • Patent number: 8227619
    Abstract: The invention relates to a process for the preparation of fungicidally active compounds such as tricyclic amine derivatives (I). The process involves coupling of a carboxylic 5 acid e.g. a compound of formula (II) with an aniline, e.g. a compound of formula (III) in the presence of a boronic acid catalystor an antimony catalyst (II)(III)(I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Het are defined in the specification.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: July 24, 2012
    Assignee: Syngenta Limited
    Inventors: Martin Charles Bowden, David Anthony Jackson, Alexandre Christian Saint-Dizier, George Robert Hodges
  • Patent number: 8211896
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: July 3, 2012
    Assignee: Chemocentryx, Inc.
    Inventors: Solomon Ungashe, Zheng Wei, J. J. Wright, Andrew Pennell
  • Patent number: 8198457
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: June 12, 2012
    Assignee: Merck Serono S.A.
    Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang