The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
  • Patent number: 10155732
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: December 18, 2018
    Assignee: City of Hope
    Inventors: David Horne, Christopher Lincoln
  • Patent number: 9951055
    Abstract: This application describes compounds and methods that can inhibit Scavenger receptor class B, type I (SR-BI) activity, which compounds and methods can used, for example, to mediate high-density lipoprotein (HDL) lipid uptake and treat hepatitis C viral infections.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: April 24, 2018
    Assignees: Massachusetts Institute of Technology, The Broad Institute, Inc.
    Inventors: Chris Dockendorff, Willmen Youngsaye, Partha Pratim Nag, Timothy A. Lewis, Sivaraman Dandapani, Benito Munoz, Patrick Faloon, Thomas Nieland, Monty Krieger, Miao Yu
  • Patent number: 9856248
    Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: January 2, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Fredrick Van Goor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
  • Patent number: 9598385
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Grant
    Filed: June 29, 2015
    Date of Patent: March 21, 2017
    Assignee: CITY OF HOPE
    Inventors: David Horne, Christopher Lincoln
  • Patent number: 9550761
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: August 21, 2013
    Date of Patent: January 24, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
  • Patent number: 9254283
    Abstract: Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: February 9, 2016
    Assignee: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Junichi Ikeda, Shunji Ichikawa, Masako Kurokawa, Tomoyuki Kanda
  • Patent number: 9126960
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Grant
    Filed: July 28, 2014
    Date of Patent: September 8, 2015
    Assignee: City of Hope
    Inventors: David Horne, Christopher Lincoln
  • Publication number: 20150148385
    Abstract: The present inventor has found out that the following criteria enable to ensure an effect for increasing the platelet count while preventing an excessive increase in the platelet count; “when the platelet count has increased by a certain amount and reached to a sufficient level of the platelet count during administration of a pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity, administration of the pharmaceutical composition is discontinued thereafter”.
    Type: Application
    Filed: June 28, 2013
    Publication date: May 28, 2015
    Inventors: Takeshi Kano, Takahiro Fukuhara, Takayuki Katsube
  • Publication number: 20150126534
    Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.
    Type: Application
    Filed: October 7, 2014
    Publication date: May 7, 2015
    Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, Lindsey Ann Needham
  • Patent number: 9000222
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: April 7, 2015
    Assignee: Androscience Corporation
    Inventors: Charles Shih, Qian Shi, Hui-Kang Wang
  • Publication number: 20150087844
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Application
    Filed: July 28, 2014
    Publication date: March 26, 2015
    Inventors: David Horne, Christopher Lincoln
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8962856
    Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: February 24, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Fredrick VanGoor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
  • Publication number: 20150051193
    Abstract: Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 19, 2015
    Inventors: Jeffrey S. Glenn, Michael A. Gelman, Brandon Tavshanjian, Kevan Shokat, Ingrid Choong
  • Publication number: 20150045393
    Abstract: The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.
    Type: Application
    Filed: February 1, 2013
    Publication date: February 12, 2015
    Inventors: Greg R. Thatcher, Isaac Thomas Schiefer, Ottavio Arancio, Mauro Fa
  • Publication number: 20150038483
    Abstract: The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ?C(R4)—, or ?N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, sub
    Type: Application
    Filed: March 26, 2013
    Publication date: February 5, 2015
    Inventors: Akira Yukimasa, Naotake Kobayashi, Kenji Takaya, Yoshio Hato
  • Patent number: 8946440
    Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).
    Type: Grant
    Filed: April 27, 2009
    Date of Patent: February 3, 2015
    Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma Limited
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
  • Publication number: 20150031734
    Abstract: Provided is a mirabegron-containing pharmaceutical composition in which the leakage of mirabegron can be inhibited when the pharmaceutical composition is dispersed in a liquid, and in which the change in pharmacokinetics caused by the presence or absence of food intake is decreased. The pharmaceutical composition comprises an acid addition salt of alkyl sulfuric acid and mirabegron, and a base for modified release.
    Type: Application
    Filed: March 29, 2013
    Publication date: January 29, 2015
    Inventors: Yuki Kasashima, Keiichi Yoshihara, Yoshitaka Ito, Takatsune Yoshida, Yumi Matsui
  • Publication number: 20150031627
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Jeremy Travins, Zhenwei Cai, Dawei Cui, Ding Zhou
  • Publication number: 20150031730
    Abstract: The present invention relates to 3-[(1,3-thiazol-4-ylmethoxyimino)(phenyl)methyl]-2-substituted-1,2,4-oxadiazol-5(2H)-one derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: December 19, 2012
    Publication date: January 29, 2015
    Inventors: Christoph Braun, Pierre-Yves Coqueron, Christophe Dubost, Hélène Lachaise, Simon Maechling, Anne-Sophie Rebstock, Philippe Rinolfi, Ulrike Wachendorff-Neumann
  • Patent number: 8940900
    Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.
    Type: Grant
    Filed: February 25, 2008
    Date of Patent: January 27, 2015
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Kasim A. Mookhtiar, Debnath Bhuniya, Bhavesh Dave, Gobind S. Kapkoti, Sujay Basu, Anita Chugh, Siddhartha De, Venkata P. Palle
  • Patent number: 8940271
    Abstract: The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: January 27, 2015
    Assignee: Abbott Laboratories
    Inventors: Mark C. Heit, Antonio M. Benitz, Dennis F. Steadman, David M. Petrick
  • Publication number: 20150025235
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: May 30, 2014
    Publication date: January 22, 2015
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar, Aleksey G. Kazantsev
  • Publication number: 20150018543
    Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: April 28, 2014
    Publication date: January 15, 2015
    Applicants: Institut Pasteur Korea, INSERM (Institut National de la Sante et de la Recherche Medicale)
    Inventors: Priscille BRODIN, Thierry CHRISTOPHE, Zaesung NO, Jaeseung KIM, Auguste GENOVESIO, Denis Philippe Cedric FENISTEIN, Heekyoung JEON, Fanny Anne EWANN, Sunhee KANG, Saeyeon LEE, Min Jung SEO, Eunjung PARK, Monica CONTRERAS DOMINGUEZ, Ji Youn NAM, Eun Hye KIM
  • Patent number: 8920785
    Abstract: Cosmetic or dermatological preparations having an effective content of one or more thiazoles of the general formula.
    Type: Grant
    Filed: February 21, 2011
    Date of Patent: December 30, 2014
    Assignee: Beiersdorf AG
    Inventors: Ludger Kolbe, Cathrin Scherner
  • Publication number: 20140378510
    Abstract: Provided herein are small molecule activators of calcium-activated chloride channels. These small molecules may be used for treatment of diseases and disorders that are treatable by activating calcium-activated chloride channels, such as cystic fibrosis, disorders related to salivary gland dysfunction (for example, Sjogren's syndrome and dysfunction following radiation injury), dry eye syndrome, and intestinal hypomotility.
    Type: Application
    Filed: August 3, 2012
    Publication date: December 25, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Alan S. Verkman, Wan Namkung
  • Publication number: 20140364433
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
  • Patent number: 8895592
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein L1, A1, R1g, z, R2, R3, and R4 are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: November 25, 2014
    Assignee: AbbVie Inc.
    Inventors: Jennifer M. Frost, Steven P. Latshaw, Michael J. Dart, William A. Carroll, Arturo Perez-Medrano, Teodozyj Kolasa, Meena V. Patel, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Xueqing Wang, Bo Liu
  • Patent number: 8895587
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: November 25, 2014
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Patent number: 8883793
    Abstract: Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2—Y—Z-Q-A-R1??Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: November 11, 2014
    Assignee: Development Center for Biotechnology
    Inventors: Meng-Hsin Chen, Shih-Hsien Chuang, Yi-Jen Chen, Lien-Hsiang Chang, Tsung-Hui Li, Ching-Hui Chen, Win-Yin Wei
  • Patent number: 8853415
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: October 7, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D. J. Grootenhuis
  • Patent number: 8846730
    Abstract: The present application relates to cannabinoid receptor ligands of formula (I) wherein X1, A1, Rx, R2, R3, R4, and z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: September 30, 2014
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Tongmei Li, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Sridhar Peddi
  • Patent number: 8841334
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a, Rx, and n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: September 23, 2014
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson, Xueqing Wang
  • Patent number: 8841461
    Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: September 23, 2014
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Masaaki Nagasawa, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
  • Publication number: 20140275189
    Abstract: The present invention relates to compounds and methods for the treatment of bacterial infections. The compounds and methods involve the disruption of the QseC signaling pathway which modulates the virulence of some bacteria. This methodology for treatment of bacterial infections reduces evolutionary pressure to develop resistance because the bacteria are not killed in the process.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 18, 2014
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Vanessa Sperandio, John R. Falck
  • Patent number: 8829034
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: September 9, 2014
    Assignee: Boehringer Ingerlheim International GmbH
    Inventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Parke, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
  • Publication number: 20140234939
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: December 23, 2013
    Publication date: August 21, 2014
    Applicant: Northwestern University
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar
  • Publication number: 20140228365
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: Merck Serono S.A.
    Inventors: Anna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Patent number: 8802861
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: January 11, 2005
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Patent number: 8796463
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: August 5, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
  • Publication number: 20140206726
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.
    Type: Application
    Filed: August 21, 2012
    Publication date: July 24, 2014
    Inventors: Juergen Benting, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Ulrike Wachendorff-Neumann
  • Patent number: 8754053
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: June 17, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Patent number: 8741939
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: March 22, 2013
    Date of Patent: June 3, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D. J. Grootenhuis
  • Publication number: 20140148600
    Abstract: The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase.
    Type: Application
    Filed: May 7, 2012
    Publication date: May 29, 2014
    Inventors: Fajun Nan, Fei Chen, Yangming Zhang, Jia Li, Yubo Zhou, Mingbo Su, Jian DING, Linghua Meng, Xin Xie, Shixian Wang
  • Publication number: 20140148457
    Abstract: Compounds of the formula I in which R, R1, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: April 12, 2012
    Publication date: May 29, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Srinivasa R. Karra, Wolfgang Staehle, Eike Staub, Margarita Wucherer-Plietker
  • Publication number: 20140135331
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 15, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
  • Publication number: 20140128436
    Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:
    Type: Application
    Filed: November 8, 2013
    Publication date: May 8, 2014
    Applicant: ActiveSite Pharmaceuticals, Inc.
    Inventors: Sukanto Sinha, Tamie Jo Chilcote
  • Publication number: 20140121250
    Abstract: Alkylamidothiazoles of general formula (I), wherein R 1=—C1-C24 alkyl (linear and branched), —C1-C24 alkenyl (linear and branched), —C1-C8 cycloalkyl, —C1-C8 cycloalkyl-alkylhydroxy, —C1-C24 alkylhydroxy (linear and branched), —C1-C24 alkylamine (linear and branched), —C1-C24 alkylaryl (linear and branched), —C1-C24 alkylaryl-alkyl-hydroxy (linear and branched), —C1-C24 alkyl-heteroaryl (linear and branched), —C1-C24-alkyl-O—C1-C24-alkyl (linear and branched), —C1-C24 alkyl morpholino, —C1-C24 alkyl piperidino, —C1-C24 alkyl piperazino, —C1-C24 alkyl-piperazino-N-alkyl, as well as cosmetic or dermatological preparations having an effective content of one or more alkylamidothiazoles, as well as the use thereof for the cosmetic or dermatological treatment and/or prophylaxis of undesired skin pigmentation.
    Type: Application
    Filed: September 18, 2012
    Publication date: May 1, 2014
    Applicant: Beiersdorf AG
    Inventors: Ludger Kolbe, Cathrin Scherner, Sabrina Ahlheit, Michael Woehrmann, Tobias Mann, Wolfram Gerwat, Torsten Schlaeger
  • Publication number: 20140121381
    Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.
    Type: Application
    Filed: October 16, 2013
    Publication date: May 1, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Fredrick VanGoor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
  • Patent number: RE45020
    Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: July 15, 2014
    Assignee: City of Hope
    Inventors: David Horne, Christopher Lincoln