At 2-position Patents (Class 544/330)
  • Patent number: 10323020
    Abstract: The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: June 18, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Eva Maria Becker-Pelster, Philipp Buchgraber, Anja Buchmüller, Karen Engel, Volker Geiss, Andreas Göller, Herbert Himmel, Raimund Kast, Andreas Knorr, Dieter Lang, Gorden Redlich, Carsten Schmeck, Hanna Tinel, Frank Wunder
  • Patent number: 10246423
    Abstract: The present invention relates to a process for preparing a statin precursor, which process comprises a first reaction step, wherein a hydroxy-pyrimidine-carbonitrile is reacted with an organic sulfonyl halide to form the sulfonate-pyrimidine-carbonitrile; a second reaction step, wherein the sulfonate-pyrimidine-carbonitrile is reacted with N-methylmethane sulfonamide to form a pyrimidinyl-sulfonamide; and optionally a third reaction step, wherein the pyrimidinyl-sulfonamide is reacted with a reducing agent. All steps are conducted in toluene as the main solvent.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: April 2, 2019
    Assignee: Centrient Pharmaceuticals Netherlands B.V.
    Inventors: Ben De Lange, Karin Henderika Maria Bessembinder, Dennis Heemskerk
  • Patent number: 9944621
    Abstract: The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: April 17, 2018
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Eva Maria Becker-Pelster, Philipp Buchgraber, Anja Buchmüller, Karen Engel, Volker Geiss, Andreas Göller, Herbert Himmel, Raimund Kast, Andreas Knorr, Dieter Lang, Gorden Redlich, Carsten Schmeck, Hanna Tinel, Frank Wunder
  • Patent number: 9884850
    Abstract: The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: February 6, 2018
    Assignee: ACETYLON PHARMACEUTICALS, INC.
    Inventors: Ralph Mazitschek, John H. van Duzer
  • Patent number: 9790189
    Abstract: The present invention relates to 5-fluoro pyrimidine derivatives containing a sulfondiimine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: October 17, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich Lücking, Arne Scholz, Philip Lienau, Gerhard Siemeister, Rolf Bohlmann, Ulf Bömer
  • Patent number: 9790191
    Abstract: This invention relates to acylaminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: October 17, 2017
    Assignee: JANSSEN SCIENCES IRELAND UC
    Inventors: David Craig Mc Gowan, Serge Marie Aloysius Pieters, Werner Embrechts, Stefaan Julien Last, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 9707232
    Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: July 18, 2017
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
  • Patent number: 9499492
    Abstract: The present invention relates to 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: November 22, 2016
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich Lücking, Dirk Kosemund, Rolf Bohlmann, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer
  • Patent number: 9199971
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is hydrogen or halogen; R2 is C1-3-alkyl or —(CH2)n—O—CH3; n is 2 or 3; m is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) with improved properties for the treatment of schizophrenia, cognitive diseases, fragile X syndrome or autism.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: December 1, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Patent number: 9174967
    Abstract: The present invention relates to substituted pyrazole-containing compounds of formula (I), and the stereoisomers and salts thereof, wherein the substituents are as defined in the description. The present invention further relates to a method for combating or controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites, to a process for the preparation of a composition for treating infested or infected animals and/or for protecting animals against infestation or infection by parasites, and to a compound according to the invention for use as a medicament.
    Type: Grant
    Filed: April 29, 2013
    Date of Patent: November 3, 2015
    Assignee: BASF SE
    Inventors: Karsten Korber, Florian Kaiser, Gemma Veitch, Wolfgang Von Deyn, Nina Gertrud Bandur, Joachim Dickhaut, Arun Narine, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Patent number: 9079883
    Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 14, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Christopher M. Mapes, David C. Palmer, Daniel J. Pippel, Kirk L. Sorgi, Tong Xiao
  • Patent number: 9079882
    Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
    Type: Grant
    Filed: October 29, 2012
    Date of Patent: July 14, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Christopher M. Mapes, David C. Palmer, Daniel J. Pippel, Kirk L. Sorgi, Tong Xiao
  • Patent number: 9073931
    Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: July 7, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Katerina Leftheris, Linghang Zhuang
  • Patent number: 9024025
    Abstract: Provided are a compound of formula (5) and a process for its preparation wherein: R1 represents an alkyl group; R2 represents an aryl group; R3 represents a protecting group or an alkyl group; R4 represents a protecting group or a SO2R5 group where R5 is an alkyl group; R6 represents (PR7R8)+X? or P(?O)R7R8 in which X is an anion and R7 and R8 each independently is an alkyl, aryl, alkoxy, or aryloxy group; P1 represents hydrogen or a protecting group; and W represents ?O or OP2, in which P2 represents hydrogen or a protecting group.
    Type: Grant
    Filed: March 25, 2014
    Date of Patent: May 5, 2015
    Assignee: Redx Pharma Limited
    Inventors: David J. Moody, Jonathan W. Wiffen
  • Patent number: 9017827
    Abstract: A compound for an organic optoelectronic device, an organic light emitting diode, and a display device, the compound including sequentially combined substituents represented by the following Chemical Formulae 1 to 3:
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: April 28, 2015
    Assignee: Cheil Industries, Inc.
    Inventors: Sung-Hyun Jung, Hyung-Sun Kim, Ho-Jae Lee, Eun-Sun Yu, Mi-Young Chae, Ja-Hyun Kim
  • Patent number: 9012431
    Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: April 21, 2015
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventor: Tsutomu Akama
  • Patent number: 9006244
    Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: April 14, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
  • Patent number: 9006245
    Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: April 14, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Katerina Leftheris, Linghang Zhuang
  • Patent number: 9006143
    Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
  • Publication number: 20150087651
    Abstract: The present invention relates to novel compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the integers are as defined in the description. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 26, 2015
    Inventors: Jean-Francois Bonfanti, Philippe Muller, Frederic Marc Maurice Doubler, Jerome Michel Claude Fortin, Nacer Lounis
  • Patent number: 8933090
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: January 13, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
  • Patent number: 8906906
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: December 9, 2014
    Assignee: Katholieke Universiteit Leuven
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Patent number: 8906916
    Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: December 9, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Christina Esdar, Hartmut Greiner
  • Patent number: 8901120
    Abstract: In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the Axl kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: March 31, 2012
    Date of Patent: December 2, 2014
    Assignee: University of Utah Research Foundation
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Alexis Mollard, Steven L. Warner, Sunil Sharma
  • Publication number: 20140350249
    Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Haruto NAKAGAWA, Naoko Ando
  • Publication number: 20140350250
    Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Haruto NAKAGAWA, Naoko ANDO
  • Patent number: 8877766
    Abstract: The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: November 4, 2014
    Inventor: Peter F. Kador
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20140316135
    Abstract: Provided are a compound of formula (5) and a process for its preparation wherein: R1 represents an alkyl group; R2 represents an aryl group; R3 represents a protecting group or an alkyl group; R4 represents a protecting group or a SO2R5 group where R5 is an alkyl group; R6 represents (PR7R8)+X? or P(?O)R7R8 in which X is an anion and R7 and R8 each independently is an alkyl, aryl, alkoxy, or aryloxy group; P1 represents hydrogen or a protecting group; and W represents ?O or OP2, in which P2 represents hydrogen or a protecting group.
    Type: Application
    Filed: March 25, 2014
    Publication date: October 23, 2014
    Applicant: Redx Pharma Limited
    Inventors: David J. Moody, Jonathan W. Wiffen
  • Patent number: 8865741
    Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.
    Type: Grant
    Filed: February 18, 2012
    Date of Patent: October 21, 2014
    Assignee: Asana Biosciences, LLC
    Inventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
  • Publication number: 20140309237
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Publication number: 20140291646
    Abstract: A pyrene-based compound and an organic light-emitting diode including the same, the pyrene-based compound being represented by Formula 1, below:
    Type: Application
    Filed: March 25, 2014
    Publication date: October 2, 2014
    Applicant: Samsung Display Co., Ltd.
    Inventors: Dong-Woo SHIN, O-Hyun KWON, Mie-Hwa PARK, Seul-Ong KIM, Byoung-Ki CHOI
  • Publication number: 20140288065
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
  • Publication number: 20140235858
    Abstract: The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 21, 2014
    Inventor: PETER F. KADOR
  • Patent number: 8809359
    Abstract: The present invention relates to phenyl amino pyrimidine bicyclic compounds formula I which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: August 19, 2014
    Assignee: YM Biosciences Australia Pty Ltd
    Inventor: Christopher John Burns
  • Publication number: 20140228385
    Abstract: The present invention provides a novel process for the preparation of 4-(4-hydroxypyrimidin-2-ylamino)benzonitrile. The present invention also provides a novel process for the preparation of 4-iodo-2,6-dimethyl benzenamine. The present invention further provides an improved process for the preparation of rilpivirine. The present invention further provides a tosylate salt of rilpivirine, process for its preparation and pharmaceutical compositions comprising it.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 14, 2014
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Adulla Venkat Narsimha Reddy, Bandi Vamsi Krishna
  • Publication number: 20140228388
    Abstract: Provided herein are phenyl-guanidine derivatives for the inhibition of Rac1 which blocks its interaction with guanosine exchange factors (GEFs) belonging to the DBL family as agents for the treatment of aggressive and/or resistant tumours, as well as pharmaceutical compositions comprising them, their use in therapy and processes for their preparation.
    Type: Application
    Filed: October 10, 2012
    Publication date: August 14, 2014
    Applicants: Universidad Nacional de Quilmes, Chemo Research, S.L.
    Inventors: Pablo Lorenzano Menna, Julieta Comín, Daniel Eduardo Gómez, Daniel Fernando Alonso
  • Publication number: 20140206585
    Abstract: A compound of Formula I, Formula IA, Formula IB, or Formula II, or an acid or base addition salt thereof, and use of these compounds as antioxidants. In one embodiment, a compound of Formula II, wherein each of X, Y, and Z are independently a carbon or nitrogen atom; R1 and R2 are each independently a hydrogen or an electron donating group, but are not both hydrogen, and wherein R1, and R2 are each bonded to a carbon atom in their own respective aryl ring.
    Type: Application
    Filed: June 4, 2012
    Publication date: July 24, 2014
    Applicants: UNIVERSITA DI BOLOGNA, Queen's University at Kingston
    Inventors: Derek A. Pratt, Jason J. Hanthorn, Luca Valgimigli
  • Patent number: 8785630
    Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: July 22, 2014
    Assignee: Vestaron Corporation
    Inventors: Robert M. Kennedy, Bruce A. Steinbaugh
  • Patent number: 8785464
    Abstract: The present invention includes compounds of general formula (1) wherein A, X, R1 and R2 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Bodo Betzemeier, Ioannis Sapountzis
  • Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8741915
    Abstract: The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: June 3, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Xicheng Sun, Jian Qiu
  • Patent number: 8716285
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: May 6, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
  • Publication number: 20140121374
    Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
    Type: Application
    Filed: November 12, 2013
    Publication date: May 1, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Daniel J. Pippel
  • Patent number: 8710076
    Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: April 29, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
  • Patent number: 8703944
    Abstract: A method for preparing a rosuvastatin calcium intermediate represented by formula I. The method includes: hydrolyzing an ester compound represented by formula II (in which, R represents C1-C5) in the presence of a metal compound to obtain a carboxylic acid compound represented by formula III; and reducing the carboxylic acid compound in the presence of a reductant.
    Type: Grant
    Filed: February 3, 2013
    Date of Patent: April 22, 2014
    Assignee: Porton Fine Chemicals Ltd.
    Inventors: Wenqing Lin, Hongjie Zheng, Peng Yang
  • Patent number: 8703945
    Abstract: There is provided a process for the preparation of a compound of formula (7) wherein R1 represents an alkyl group; R2 represents an aryl group; R3 represents hydrogen, a protecting group or an alkyl group; and R4 represents hydrogen, a protecting group or a SO2R5 group where R5 is an alkyl group, which comprises a) hydroxylating a compound of formula (1) wherein Y represents a halo group; P1 represents hydrogen or a protecting group, and W represents ?O or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2), b) oxidixing the compound of formula (2) to give a compound of formula (3), c) coupling the compound of formula (3) with a compound of formula (4), wherein R3 represents a protecting group or an alkyl group; R4 represents a protecting group or a SO2R5 group where R5 is an alkyl group; and R6 represents (PR7R8)+X? or P(?O)R7R8 in which X is an anion and R7 and R8 each independently is an alkyl, aryl.
    Type: Grant
    Filed: March 23, 2005
    Date of Patent: April 22, 2014
    Assignee: Redx Pharma Limited
    Inventors: David J. Moody, Jonathan W. Wiffen
  • Patent number: 8686143
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: April 1, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
  • Publication number: 20140066624
    Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
    Type: Application
    Filed: November 11, 2013
    Publication date: March 6, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Christopher M. Mapes, David C. Palmer, Daniel J. Pippel, Kirk L. Sorgi, Tong Xiao
  • Publication number: 20140051854
    Abstract: The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
    Type: Application
    Filed: July 25, 2011
    Publication date: February 20, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Damjan Sterk, Marko Jukic