At 2-position Patents (Class 544/330)
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Patent number: 12030873Abstract: This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.Type: GrantFiled: September 1, 2021Date of Patent: July 9, 2024Assignee: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Paul Anthony Baguley, Colin Thomas Lindley, Robert Craig Melling
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Patent number: 11142518Abstract: This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.Type: GrantFiled: April 20, 2018Date of Patent: October 12, 2021Assignee: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Michael Reader, Nicola Elizabeth Wilsher, Mark Henry Saunders, Paul Anthony Baguley, Colin Thomas Lindley, Robert Craig Melling, Bozena Ewa Adamczyk, Mirka Scarati
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Patent number: 10323020Abstract: 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: GrantFiled: December 19, 2017Date of Patent: June 18, 2019Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: 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
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Patent number: 10246423Abstract: 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: GrantFiled: January 22, 2016Date of Patent: April 2, 2019Assignee: Centrient Pharmaceuticals Netherlands B.V.Inventors: Ben De Lange, Karin Henderika Maria Bessembinder, Dennis Heemskerk
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Patent number: 9944621Abstract: 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: GrantFiled: December 16, 2014Date of Patent: April 17, 2018Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: 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
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Patent number: 9884850Abstract: 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: GrantFiled: September 9, 2016Date of Patent: February 6, 2018Assignee: ACETYLON PHARMACEUTICALS, INC.Inventors: Ralph Mazitschek, John H. van Duzer
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Patent number: 9790191Abstract: This invention relates to acylaminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.Type: GrantFiled: October 3, 2013Date of Patent: October 17, 2017Assignee: JANSSEN SCIENCES IRELAND UCInventors: David Craig Mc Gowan, Serge Marie Aloysius Pieters, Werner Embrechts, Stefaan Julien Last, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson
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Patent number: 9790189Abstract: 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: GrantFiled: March 27, 2015Date of Patent: October 17, 2017Assignee: Bayer Pharma AktiengesellschaftInventors: Ulrich Lücking, Arne Scholz, Philip Lienau, Gerhard Siemeister, Rolf Bohlmann, Ulf Bömer
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Patent number: 9707232Abstract: 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: GrantFiled: July 7, 2016Date of Patent: July 18, 2017Assignee: 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
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Patent number: 9499492Abstract: 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: GrantFiled: November 11, 2013Date of Patent: November 22, 2016Assignee: Bayer Pharma AktiengesellschaftInventors: Ulrich Lücking, Dirk Kosemund, Rolf Bohlmann, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer
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Patent number: 9199971Abstract: 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: GrantFiled: February 13, 2015Date of Patent: December 1, 2015Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 9174967Abstract: 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: GrantFiled: April 29, 2013Date of Patent: November 3, 2015Assignee: BASF SEInventors: Karsten Korber, Florian Kaiser, Gemma Veitch, Wolfgang Von Deyn, Nina Gertrud Bandur, Joachim Dickhaut, Arun Narine, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
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Patent number: 9079883Abstract: 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: GrantFiled: March 15, 2013Date of Patent: July 14, 2015Assignee: Janssen Pharmaceutica NVInventors: 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
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Patent number: 9079882Abstract: 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: GrantFiled: October 29, 2012Date of Patent: July 14, 2015Assignee: Janssen Pharmaceutica NVInventors: 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
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Patent number: 9073931Abstract: 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: GrantFiled: March 14, 2013Date of Patent: July 7, 2015Assignee: Vitae Pharmaceuticals, Inc.Inventors: Katerina Leftheris, Linghang Zhuang
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Patent number: 9024025Abstract: 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: GrantFiled: March 25, 2014Date of Patent: May 5, 2015Assignee: Redx Pharma LimitedInventors: David J. Moody, Jonathan W. Wiffen
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Patent number: 9017827Abstract: 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: GrantFiled: December 23, 2011Date of Patent: April 28, 2015Assignee: Cheil Industries, Inc.Inventors: Sung-Hyun Jung, Hyung-Sun Kim, Ho-Jae Lee, Eun-Sun Yu, Mi-Young Chae, Ja-Hyun Kim
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Patent number: 9012431Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: GrantFiled: June 11, 2013Date of Patent: April 21, 2015Assignee: Anacor Pharmaceuticals, Inc.Inventor: Tsutomu Akama
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Patent number: 9006244Abstract: 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: GrantFiled: March 14, 2013Date of Patent: April 14, 2015Assignee: 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
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Patent number: 9006143Abstract: 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: GrantFiled: March 13, 2013Date of Patent: April 14, 2015Assignee: Bayer Intellectual Property GmbHInventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
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Patent number: 9006245Abstract: 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: GrantFiled: November 19, 2014Date of Patent: April 14, 2015Assignee: Vitae Pharmaceuticals, Inc.Inventors: Katerina Leftheris, Linghang Zhuang
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Publication number: 20150087651Abstract: 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: ApplicationFiled: April 30, 2013Publication date: March 26, 2015Inventors: Jean-Francois Bonfanti, Philippe Muller, Frederic Marc Maurice Doubler, Jerome Michel Claude Fortin, Nacer Lounis
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Patent number: 8933090Abstract: 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: GrantFiled: October 19, 2010Date of Patent: January 13, 2015Assignee: Novartis AGInventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
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Patent number: 8906916Abstract: 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: GrantFiled: July 19, 2011Date of Patent: December 9, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Christina Esdar, Hartmut Greiner
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Patent number: 8906906Abstract: 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: GrantFiled: August 5, 2010Date of Patent: December 9, 2014Assignee: Katholieke Universiteit LeuvenInventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
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Patent number: 8901120Abstract: 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: GrantFiled: March 31, 2012Date of Patent: December 2, 2014Assignee: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Alexis Mollard, Steven L. Warner, Sunil Sharma
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Publication number: 20140350250Abstract: 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: ApplicationFiled: August 12, 2014Publication date: November 27, 2014Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Haruto NAKAGAWA, Naoko ANDO
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Publication number: 20140350249Abstract: 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: ApplicationFiled: August 12, 2014Publication date: November 27, 2014Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Haruto NAKAGAWA, Naoko Ando
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Patent number: 8877741Abstract: 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: GrantFiled: January 22, 2014Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
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Patent number: 8877766Abstract: 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: GrantFiled: February 15, 2013Date of Patent: November 4, 2014Inventor: Peter F. Kador
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Publication number: 20140316135Abstract: 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: ApplicationFiled: March 25, 2014Publication date: October 23, 2014Applicant: Redx Pharma LimitedInventors: David J. Moody, Jonathan W. Wiffen
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Patent number: 8865741Abstract: 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: GrantFiled: February 18, 2012Date of Patent: October 21, 2014Assignee: Asana Biosciences, LLCInventors: 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
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Publication number: 20140309237Abstract: 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: ApplicationFiled: June 26, 2014Publication date: October 16, 2014Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Publication number: 20140291646Abstract: A pyrene-based compound and an organic light-emitting diode including the same, the pyrene-based compound being represented by Formula 1, below:Type: ApplicationFiled: March 25, 2014Publication date: October 2, 2014Applicant: Samsung Display Co., Ltd.Inventors: Dong-Woo SHIN, O-Hyun KWON, Mie-Hwa PARK, Seul-Ong KIM, Byoung-Ki CHOI
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Publication number: 20140288065Abstract: 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: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Applicant: 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
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Publication number: 20140235858Abstract: 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: ApplicationFiled: February 15, 2013Publication date: August 21, 2014Inventor: PETER F. KADOR
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Patent number: 8809359Abstract: 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: GrantFiled: March 14, 2013Date of Patent: August 19, 2014Assignee: YM Biosciences Australia Pty LtdInventor: Christopher John Burns
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Publication number: 20140228385Abstract: 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: ApplicationFiled: February 16, 2012Publication date: August 14, 2014Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Adulla Venkat Narsimha Reddy, Bandi Vamsi Krishna
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Publication number: 20140228388Abstract: 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: ApplicationFiled: October 10, 2012Publication date: August 14, 2014Applicants: Universidad Nacional de Quilmes, Chemo Research, S.L.Inventors: Pablo Lorenzano Menna, Julieta Comín, Daniel Eduardo Gómez, Daniel Fernando Alonso
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Publication number: 20140206585Abstract: 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: ApplicationFiled: June 4, 2012Publication date: July 24, 2014Applicants: UNIVERSITA DI BOLOGNA, Queen's University at KingstonInventors: Derek A. Pratt, Jason J. Hanthorn, Luca Valgimigli
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Patent number: 8785630Abstract: 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: GrantFiled: February 6, 2013Date of Patent: July 22, 2014Assignee: Vestaron CorporationInventors: Robert M. Kennedy, Bruce A. Steinbaugh
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Patent number: 8785464Abstract: 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: GrantFiled: October 9, 2013Date of Patent: July 22, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Bodo Betzemeier, Ioannis Sapountzis
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Patent number: 8778628Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 17, 2013Date of Patent: July 15, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Patent number: 8741915Abstract: 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: GrantFiled: September 24, 2010Date of Patent: June 3, 2014Assignee: N30 Pharmaceuticals, Inc.Inventors: Xicheng Sun, Jian Qiu
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Patent number: 8716285Abstract: 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: GrantFiled: September 7, 2011Date of Patent: May 6, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Publication number: 20140121374Abstract: 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: ApplicationFiled: November 12, 2013Publication date: May 1, 2014Applicant: Janssen Pharmaceutica NVInventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Daniel J. Pippel
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Patent number: 8710076Abstract: 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: GrantFiled: October 15, 2009Date of Patent: April 29, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
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Patent number: 8703945Abstract: 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: GrantFiled: March 23, 2005Date of Patent: April 22, 2014Assignee: Redx Pharma LimitedInventors: David J. Moody, Jonathan W. Wiffen
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Patent number: 8703944Abstract: 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: GrantFiled: February 3, 2013Date of Patent: April 22, 2014Assignee: Porton Fine Chemicals Ltd.Inventors: Wenqing Lin, Hongjie Zheng, Peng Yang
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Patent number: 8686143Abstract: 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: GrantFiled: October 25, 2011Date of Patent: April 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: 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