Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/357)
  • Publication number: 20140031398
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Application
    Filed: January 27, 2012
    Publication date: January 30, 2014
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Publication number: 20140031399
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
    Type: Application
    Filed: September 30, 2013
    Publication date: January 30, 2014
    Inventors: Leslie Wighton MCQUIRE, Olivier ROGEL, Michael SHULTZ, Ruben Alberto TOMMASI, Sven WEILER
  • Publication number: 20140031204
    Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) 2,6-dichloro-N-[3-chloro-5-(trifluoromethyl)-2-pyridylmethyl]benzamide (CAS-No 239110-15-7, common name fluopicolide) of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively combating undesirable microorganisms of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Application
    Filed: March 21, 2012
    Publication date: January 30, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marie-Pascale Latorse, Sylvain Tafforeau, Luis Julian Ledesma Perez
  • Publication number: 20140024641
    Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.
    Type: Application
    Filed: January 7, 2013
    Publication date: January 23, 2014
    Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
  • Publication number: 20140024642
    Abstract: An ophthalmic formulation having an effective amount of a parasympathomimetic agent comprising pilocarpine, or a pharmaceutically acceptable salt thereof, and one or more ?1 adrenergic agonists or antagonists is disclosed. The ophthalmic formulation may enable treatment of conditions adversely affecting the visual acuity of a patient, including presbyopia. A method of using the disclosed ophthalmic formulation to treat or ameliorate symptoms of presbyopia is also disclosed.
    Type: Application
    Filed: July 19, 2012
    Publication date: January 23, 2014
    Inventor: Luis Felipe Vejarano Restrepo
  • Publication number: 20140024684
    Abstract: The invention relates to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate, and to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
    Type: Application
    Filed: March 27, 2012
    Publication date: January 23, 2014
    Applicant: SANOFI
    Inventors: Norbert Nagel, Bruno Baumgartner, Harald Berchtold, Timothy Ayers
  • Publication number: 20140024532
    Abstract: A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of formula I wherein R1 is difluoromethyl or trifluoromethyl and X is chloro, fluoro or bromo; and (B) at least one compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants, especially rust diseases on soybean plants.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 23, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Hans Tobler, Harald Walter, Ulrich Johannes Haas
  • Publication number: 20140018398
    Abstract: The invention relates to a pharmaceutical composition comprising methyl (2R.3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable acidic reacting compound or to an aqueous solution or dispersion of the composition as well as a process for the preparation of the same, methods of using such compositions to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
    Type: Application
    Filed: March 27, 2012
    Publication date: January 16, 2014
    Applicant: SANOFI
    Inventors: Walter Kamm, Till Bussemer, Doris Andert, Bernd Kuehn, Ernst-Josef Todt
  • Publication number: 20140018368
    Abstract: The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.
    Type: Application
    Filed: July 1, 2013
    Publication date: January 16, 2014
    Applicants: Genetech, Inc., Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Publication number: 20140018377
    Abstract: This application claims priority to European Patent Application No. 09173304.8, filed Oct. 16, 2009, and the benefit of U.S. Provisional Application No. 61/253,091, filed Oct. 20, 2009, the disclosure of each of which is incorporated by reference herein in its entirety. The present invention relates to aminopropenoate derivatives, the process of their preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.
    Type: Application
    Filed: June 12, 2013
    Publication date: January 16, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Christophe Dubost, Jacky Vadal, Philippe Rinolfi, Marie-Claire Grosjean-Cournoyer, Mazen Es-Sayed, Jürgen Benting, Ulrike Wachendorff-Neumann, Shinichi Narabu, Koichi Ishikawa, Hiroyuki Hadano, Pierre Genix, Jean-Pierre Vors, Angela Becker, Ulrich Görgens
  • Publication number: 20140005175
    Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.
    Type: Application
    Filed: August 26, 2013
    Publication date: January 2, 2014
    Applicants: Cephalon, Inc., University of Utah Research Foundation, University of Hawaii
    Inventors: Bruce D. Dorsey, Scott K. Kuwada, Jay P. Theroff, Craig A. Zificsak
  • Publication number: 20140005235
    Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein A1, A2, A3, A4, A5, A6, G1, G2, R1, R2, R3, L, Q1, Q2, R4, R5, R6, R7, Q2, Y1, Y2, Y3, Y4, Y5, Y6, Y7, Y8, and Y9 are as defined in claim 1; or salts or N-oxides thereof.
    Type: Application
    Filed: March 19, 2012
    Publication date: January 2, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph, Marcel Jung, Ottmar Franz Hueter, Peter Renold, Thomas Pitterna
  • Publication number: 20140005047
    Abstract: The present invention relates to novel active ingredient combinations which consist of fluopyram and other known active ingredients and are very well suited for the control of animal pests, such as insects and/or unwanted acarids and/or nematodes, in foliar and soil application and/or in the treatment of seeds, and are also suitable for increasing yields.
    Type: Application
    Filed: November 30, 2011
    Publication date: January 2, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Heike Hungenberg, Heiko Rieck, Robert Masters
  • Publication number: 20140005234
    Abstract: N-substituted sulfilimine and sulfoximine pyridine N-oxides and their use in controlling insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects, and benefits shall become apparent from the description.
    Type: Application
    Filed: June 17, 2013
    Publication date: January 2, 2014
    Inventors: Douglas C. Bland, Ronald Ross, JR., Peter L. Johnson, Timothy C. Johnson
  • Patent number: 8618143
    Abstract: Non-peptide, azole-substituted nitric oxide snythase inhibitor compounds, compositions and related methods, as can be used to enhance bioavailability and inhibit production of nitric oxide.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: December 31, 2013
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, James M. Kraus
  • Patent number: 8617614
    Abstract: The present invention provides a microsphere with a slow-release period from about two weeks to about four weeks following administration, to enable a higher content of a drug to be included, to suppress an initial burst of the drug, and to maintain an optimal, effective blood concentration during the slow-release period. In a microsphere containing a drug and polylactic acid/glycolic acid (PLGA) copolymer, the amount of PLGA copolymer per part by weight of the drug is from about 3 to about 10 parts by weight; the average particle size of the microsphere is from about 20 to about 50 ?m; and (3) the PLGA copolymer has a weight-average molecular weight from about 10,000 to about 50,000 and a PLGA compositional ratio from about 75/25 to about 50/50. The microsphere promotes the production of various endogenous repair factors useful against various tissue disorders.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: December 31, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yoshiki Sakai, Takahiro Uchida
  • Patent number: 8618068
    Abstract: Disclosed herein are methods and low dose regimens for increasing fetal hemoglobin levels in patients with red blood cell disorders, such as beta thalassemia, sickle cell disease, other anemias, or blood loss. Fetal and total hemoglobin levels and red blood cell counts are increased by administering 2,2-dimethylbutyrate (DMB) alone or in combination with hydroxyurea, decitabine or an HDAC inhibitor. Treatment can be continued for at least two weeks.
    Type: Grant
    Filed: December 8, 2010
    Date of Patent: December 31, 2013
    Assignees: Trustees of Boston University, Hemaquest Pharmaceuticals, Inc.
    Inventors: Susan P Perrine, Douglas V Faller, Ronald J Berenson
  • Publication number: 20130345164
    Abstract: This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.
    Type: Application
    Filed: April 21, 2011
    Publication date: December 26, 2013
    Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY
    Inventors: Alexei Vazquez, Darren Carpizo, Arnold Levine
  • Publication number: 20130337082
    Abstract: This disclosure relates to compounds and compositions for forming bone and methods related thereto. In certain embodiments, the disclosure relates to methods of forming bone comprising implanting a bone graft composition comprising a growth factor such as BMP in a subject at a site of desired bone growth or enhancement in combination with a Noggin blocker.
    Type: Application
    Filed: February 23, 2012
    Publication date: December 19, 2013
    Applicant: EMORY UNIVERSITY
    Inventors: Scott D. Boden, Sreedhara Sangadala
  • Publication number: 20130338143
    Abstract: Disclosed herein are compositions that are useful in effecting the transdermal delivery of therapeutic agents. More particularly, the disclosed transdermal compositions may include a fatty alcohol (for example, octanol), a terpene (for example, limonene), and an active agent comprising an amine moiety.
    Type: Application
    Filed: November 15, 2011
    Publication date: December 19, 2013
    Applicant: Neuroderm, Ltd.
    Inventors: Oron Yacoby-Zeevi, Mara Nemas, Eduardo Zawozink
  • Publication number: 20130338095
    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: December 19, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Publication number: 20130331328
    Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.
    Type: Application
    Filed: February 14, 2012
    Publication date: December 12, 2013
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Ziad Sahab
  • Patent number: 8604066
    Abstract: A medication, a pharmaceutical composition, and method for the treatment of respiratory poisoning in animals and humans caused by organophosphorus compounds, whereby said medication and said pharmaceutical composition comprise at least one oxime and one blocker of organic cation transporters (OCT).
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: December 10, 2013
    Assignee: SERB
    Inventors: Frédéric J. Baud, Pascal Houze, Maya Kayouka
  • Publication number: 20130324540
    Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.
    Type: Application
    Filed: August 7, 2013
    Publication date: December 5, 2013
    Applicant: Obschestvo Ogranichennoi Otvetstvennostyu "Pharmenterprises"
    Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
  • Publication number: 20130324400
    Abstract: Provided are methods for reducing the occurrence of sudden death syndrome in plants, such as soybeans, using compounds of the general formula (I).
    Type: Application
    Filed: November 23, 2011
    Publication date: December 5, 2013
    Applicant: Bayer Cropscience LP
    Inventors: Jennifer Riggs, David Doran
  • Patent number: 8597876
    Abstract: Disclosed is a method of treating human immunodeficiency virus (HIV) infection in an antiretroviral treatment-experienced mammal, which involves administering to the mammal an effective amount of a compound of the formula: or a pharmaceutically acceptable salt, a prodrug, or an ester thereof, or a pharmaceutically acceptable composition of the compound, the salt, the prodrug, or the ester thereof, wherein A, X, Q, W, m, and R2-R6 are as defined herein.
    Type: Grant
    Filed: October 11, 2007
    Date of Patent: December 3, 2013
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Board of Trustees of the University of Illinois
    Inventors: John W. Erickson, Sergei V. Gulnik, Hiroaki Mitsuya, Arun K. Ghosh
  • Patent number: 8598213
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: December 3, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Patent number: 8598214
    Abstract: N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: December 3, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers, Yuanming Zhu, James M. Renga, Vidyadhar B. Hegde, Joseph J. DeMark
  • Publication number: 20130317040
    Abstract: The present invention is directed to a method of treating systemic lupus erythematosus (SLE) in a subject comprising administering to the subject an amount of an HIV protease inhibitor effective to treat SLE. The present invention is also directed to a pharmaceutical product comprising an HIV protease inhibitor formulated in a pharmaceutically acceptable carrier, and a package insert providing instructions for the administration of the HIV protease inhibitor for the treatment of SLE. In addition, the present invention is directed to the use of an HIV protease inhibitor for the preparation of a medicament for the treatment of SLE.
    Type: Application
    Filed: December 21, 2011
    Publication date: November 28, 2013
    Applicant: The Feinstein Institute of Medical Research
    Inventors: Yousef Al-Abed, Betty A. Diamond
  • Publication number: 20130317027
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 28, 2013
    Applicant: Myrexis, Inc.
    Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup, Christophe Hoarau, David A. Gerrish, Paul R. Sebahar, Dange Vijay Kumar
  • Patent number: 8592419
    Abstract: The invention provides the compounds of formula (): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, A, X, Y, a, b and n are as defined herein. Also disclosed are methods for making the compounds of formula (I) and their use in treating or preventing diseases associated with cell overproliferation and dysfunctional sphingolipid signal transduction. The invention also encompasses the use of the compounds in combination with an apoptosis-signaling ligand, such as Fas ligand. Preferably, the Fas ligand is administered in the form of a gene therapy agent.
    Type: Grant
    Filed: October 31, 2005
    Date of Patent: November 26, 2013
    Assignee: MUSC Foundation for Research Development
    Inventors: Alicja Bielawska, Yusuf A. Hannun, James Norris, Zdzislaw M. Szulc, Jian-yun Dong, Jacek Bielawski, David A. Schwartz, David H. Holman, Ahmed M. El-Zawahry, John McKillop
  • Publication number: 20130310384
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2011
    Publication date: November 21, 2013
    Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, Hanxun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130310378
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: April 23, 2013
    Publication date: November 21, 2013
    Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co KG
    Inventors: AbbVie Deutschland GmbH & Co KG, AbbVie Inc.
  • Publication number: 20130303575
    Abstract: Methods of treating patients with SNDX-275 are provided.
    Type: Application
    Filed: July 11, 2013
    Publication date: November 14, 2013
    Applicant: SYNDAX PHARMACEUTICALS, INC.
    Inventors: Konrad BURKE, Peter ORDENTLICH, Robert S. Goodenow
  • Publication number: 20130303576
    Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH—Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)O—, —C(?O)NR?—, —C(?S)—NR?, —C(?NH)NR? or —S(?O)2NR— wherein R? is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q.
    Type: Application
    Filed: July 19, 2013
    Publication date: November 14, 2013
    Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
  • Publication number: 20130303527
    Abstract: What are described are novel active compound combinations comprising a known oxime ether derivative (trifloxystrobin) and imidacloprid, which combinations are highly suitable for controlling phytopathogenic fungi and insects.
    Type: Application
    Filed: April 11, 2013
    Publication date: November 14, 2013
    Inventors: Ulrike WACHENDORFF-NEUMANN, Astrid Mauler-Machnik, Christoph Erdelen, Hirohisa Ohtake
  • Publication number: 20130303526
    Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 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: September 16, 2011
    Publication date: November 14, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: Chiyou NI, Bin Shao, Laykea Tafesse, Jiangchao Yao, Jianming Yu, Xiaoming Zhou
  • Publication number: 20130303572
    Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.
    Type: Application
    Filed: December 19, 2011
    Publication date: November 14, 2013
    Inventors: Péter Ferdinandy, Tamás Bálint Csont, Csaba Csonka, Krisztina Kedvesné Kupai, László Kovács, Attila Kis-Tamás, Ferenc Tamás Takács, Dénes Kónya, Gábor Medgyes, Sándor Cseh, István Hajdú, Zsolt Lõrincz, György Dormán, Anikó Görbe
  • Publication number: 20130303549
    Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.
    Type: Application
    Filed: July 10, 2013
    Publication date: November 14, 2013
    Inventors: Jean-Guy BOITEAU, Laurence CLARY, Corinne Millois BARBUIS
  • Patent number: 8580855
    Abstract: A pharmaceutical dosage form is provided comprising a non-steroidal anti-inflammatory agent and acetaminophen, and methods for their use. In one embodiment, the dosage form is comprised of ibuprofen and acetaminophen as the sole pharmaceutically effective agents, wherein the ibuprofen and acetaminophen are in a weight ratio of about 12 parts:about 88 parts.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: November 12, 2013
    Assignee: McNeil-PPC, Inc.
    Inventors: Jim Swann, Peter Cummins
  • Patent number: 8580856
    Abstract: A pharmaceutical dosage form is provided comprising a non-steroidal anti-inflammatory agent and acetaminophen, and methods for their use. In one embodiment, the dosage form is comprised of ibuprofen and acetaminophen as the sole pharmaceutically effective agents, wherein the ibuprofen and acetaminophen are in a weight ratio of about 12 parts:about 88 parts.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: November 12, 2013
    Assignee: NcNeil-PPC, Inc.
    Inventors: Jim Swann, Peter Cummins
  • Patent number: 8580826
    Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.
    Type: Grant
    Filed: October 26, 2011
    Date of Patent: November 12, 2013
    Assignee: Targacept, Inc.
    Inventors: Julio A. Munoz, John Genus, James R. Moore
  • Publication number: 20130296167
    Abstract: Active compound combinations are disclosed which comprise (A) a dithiino-tetracarboximide of formula (I) and a further insecticidally active compound (B). Methods for controlling animal pests such as insects and/or unwanted acarids and for curatively or preventively controlling the phytopathogenic fungi of plants or crops are also disclosed as well as the use of a composition according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.
    Type: Application
    Filed: April 17, 2013
    Publication date: November 7, 2013
    Inventors: Thomas SEITZ, Ulrike Wachendorff-Neumann, Heike Hungenberg, Peter Dahmen
  • Publication number: 20130296385
    Abstract: The present invention relates to processes for the preparation of tablets which dissolve rapidly in the mouth and provide an excellent mouthfeel. The tablets of the invention comprise a compound which melts at about 37° C. or lower, have a low hardness, high stability and generally comprise few insoluble disintegrants which may cause a gritty or chalky sensation in the mouth. Convenient and economically feasible processes by which the tablets of the invention may be produced are also provided.
    Type: Application
    Filed: July 11, 2013
    Publication date: November 7, 2013
    Inventors: Janos Szamosi, Kevin Scott Kinter, Vincent H. Li, Khawka Abdullah Abu-Izza
  • Publication number: 20130296346
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.
    Type: Application
    Filed: November 22, 2011
    Publication date: November 7, 2013
    Applicant: Faes Farma, S.A.
    Inventors: Rosa Rodes Solanes, Neftali Garcia Dominguez, Beatriz Lopez Ortega, Melchor Alvarez De Mon Soto, Antonio De La Hera Martinez, Ana Munoz Munoz, Francisco Ledo Gomez
  • Publication number: 20130296369
    Abstract: The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.
    Type: Application
    Filed: November 11, 2011
    Publication date: November 7, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Desbordes, Christophe Dubost, Pierre Genix, Shinichi Narabu, Jean-Pierre Vors
  • Publication number: 20130296309
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: July 11, 2013
    Publication date: November 7, 2013
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • Publication number: 20130296384
    Abstract: Methods of using N-substituted(6-haloalkylpyridin-3-yl)alkyl sulfoximines, such as sulfoxaflor, as a seed treatment to control Coleopteran insects, such as flea beetles.
    Type: Application
    Filed: April 12, 2013
    Publication date: November 7, 2013
    Inventors: William H. Hendrix, III, Gary Turnbull
  • Publication number: 20130289034
    Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
    Type: Application
    Filed: June 21, 2013
    Publication date: October 31, 2013
    Inventors: Orion D. JANKOWSKI, Kieron E. WESSON, Paul MOLLARD, William D. SHRADER