Nitrogen Attached Directly At 2-position By Nonionic Bonding And Sulfur Bonded Directly To The Nitrogen Patents (Class 544/297)
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Publication number: 20140205641Abstract: The present invention relates to co-crystals of cyprodinil and dithianon as defined in the description, processes for preparing these co-crystals and also to compositions comprising at least such co-crystals. The invention also relates to the use of such co-crystals or compositions for combating harmful fungi.Type: ApplicationFiled: August 30, 2012Publication date: July 24, 2014Applicant: BASF SEInventors: Christian Sowa, Randall Evan Gold, Tiziana Chiodo, Ralf Vogel
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Publication number: 20140194452Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.Type: ApplicationFiled: January 10, 2014Publication date: July 10, 2014Applicant: Grünenthal GmbHInventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
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Publication number: 20140194451Abstract: Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit, the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.Type: ApplicationFiled: November 22, 2013Publication date: July 10, 2014Inventors: Qun Lu, Huchen Zhou, Yanhua Chen, Amy Friesland
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Patent number: 8765947Abstract: A preparation method of rosuvastatin calcium (Formula 1), which can be used for the production of medicament lowering the levels of LDL-cholesterol and triglycerides in vivo, is provided. Such preparation method is suitable for industrial production. Furthermore, the intermediate crystallines used in the preparation method are provided.Type: GrantFiled: March 5, 2013Date of Patent: July 1, 2014Assignee: Changzhou Pharmaceutical FactoryInventors: Benshun Chen, Bing Wang, Xiaofeng Jin, Lin Zou
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Publication number: 20140179681Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.Type: ApplicationFiled: January 8, 2014Publication date: June 26, 2014Inventor: Joseph P. Errico
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Patent number: 8759347Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: June 13, 2013Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
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Patent number: 8759518Abstract: A compound of Formula (1), is disclosed wherein P1 and P2 are alcohol protecting groups or 1,3-diol protecting group, R is selected from: wherein R4a is selected from alkyl, aryl, arylalkyl and cycloalkyl, Rc is selected from H, alkyl, aryl, alkaoxy, haloalkyl, monohaloalkyloxy, and dihaloalkyloxy, Rd is selected from alkyl, aryl, arylalkyl, CF3, halo and NO2 and X is selected from O, N—H, N-alkyl and S, Ra and Rb are same or different and each represents hydrogen, an alkyl group of 1 to 12 carbon atoms, an aryl group of 6 to 12 carbon atoms, or an aralkyl group of 7 to 12 carbon atoms.Type: GrantFiled: February 23, 2011Date of Patent: June 24, 2014Assignee: Cadila Healthcare LimitedInventors: Shriprakash Dhar Dwivedi, Dhimant Jasubhai Patel, Mahesh Laljibhai Rupapara
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Publication number: 20140171439Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: February 21, 2014Publication date: June 19, 2014Applicant: Janssen Pharmaceutica, N.V.Inventors: Kristof VAN EMELEN, Marc Gustaaf Celine VERDONCK, Sven Franciscus Anna VAN BRANDT, Patrick Rene ANGIBAUD, Lieven MEERPOEL, Alexey Borisovich DYATKIN
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Patent number: 8748445Abstract: The present disclosure provides for method of treatment and/or prevention of disease states that require cystine for maintenance or progression of the disease state. In addition, methods for screening and identifying novel therapeutic agents useful in the treatment of such disease states are described. In one embodiment, the disease state is a cancer, such as, but not limited to, glioma. In this embodiment, methods for the treatment and prevention of glioma by inhibiting cystine uptake or decreasing intracellular cystine concentrations are provided. The present disclosure teaches that glioma cells are dependent on system Xc for cystine uptake. Pharmacological inhibition of system Xc causes a rapid depletion of intracellular glutathione, resulting in decreased cell growth. In contrast, non-malignant astrocytes and cortical neurons remain viable in the presence of Xc inhibitors and continue to take up cystine via alternate amino acid transporters.Type: GrantFiled: October 27, 2005Date of Patent: June 10, 2014Assignee: The UAB Research FoundationInventors: W. Joon Chung, Harald Sontheimer
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Publication number: 20140155602Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2?, R3, R3?, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: ApplicationFiled: November 20, 2013Publication date: June 5, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20140155367Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.Type: ApplicationFiled: November 18, 2013Publication date: June 5, 2014Applicants: Novartis AG, IRM LLCInventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan KS Yeung, Bin Zou, Venkatataiah Bollu
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Patent number: 8729092Abstract: The invention discloses a method for the treatment of diseases, particularly those diseases characterized by diminished or aberrant cellular function, including AIDS, cancer, and Alzheimer's Disease. The method comprises administering a therapeutically effective amount of rosuvastatin enantiomer compounds in their (3R,5R), (3S,5R), or (3S,5S) configurations, or pharmaceutically acceptable salts thereof. Biologically-active rosuvastatin enantiomer compounds with (3R,5R), (3S,5R), and (3S,5S) stereochemistry are also disclosed.Type: GrantFiled: September 24, 2012Date of Patent: May 20, 2014Inventor: Terence J. Scallen
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Publication number: 20140128368Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Patent number: 8716305Abstract: A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior.Type: GrantFiled: April 16, 2012Date of Patent: May 6, 2014Assignee: BASF SEInventors: Andreas Hafner, Fritz Blatter, Martin Szelagiewicz, Bernd Siebenhaar
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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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Publication number: 20140107339Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.Type: ApplicationFiled: September 4, 2013Publication date: April 17, 2014Applicant: Cornell UniversityInventors: Geoffrey W. Coates, John W. Kramer
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Publication number: 20140100214Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: December 6, 2013Publication date: April 10, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20140094480Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death.Type: ApplicationFiled: December 9, 2013Publication date: April 3, 2014Applicant: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Joseph M. Ready, Andrew A. Pieper, Jef K. De Brabander
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Patent number: 8686155Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: June 28, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
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Publication number: 20140088126Abstract: The invention discloses a method for the treatment of diseases, particularly those diseases characterized by diminished or aberrant cellular function, including AIDS, cancer, and Alzheimer's Disease. The method comprises administering a therapeutically effective amount of rosuvastatin enantiomer compounds in their (3R, 5R), (3S, 5R), or (3S, 5S) configurations, or pharmaceutically acceptable salts thereof. Biologically-active rosuvastatin enantiomer compounds with (3R, 5R), (3S, 5R), and (3S, 5S) stereochemistry are also disclosed.Type: ApplicationFiled: September 24, 2012Publication date: March 27, 2014Inventor: Terence J. Scallen
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Publication number: 20140058097Abstract: A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.Type: ApplicationFiled: November 1, 2013Publication date: February 27, 2014Applicant: Shionogi & Co., Ltd.Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuuji Kooriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
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Publication number: 20140057913Abstract: Described herein are inhibitors of Aurora kinase and their use in the treatment of cancer. Methods of screening for selective inhibitors of Aurora kinases are also disclosed.Type: ApplicationFiled: March 30, 2012Publication date: February 27, 2014Applicant: H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: Said M. Sebti, Ernst Schönbrunn, Nicholas J. Lawrence, Harshani R. Lawrence, Matthew P. Martin
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Publication number: 20140051854Abstract: 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: ApplicationFiled: July 25, 2011Publication date: February 20, 2014Applicant: LEK PHARMACEUTICALS D.D.Inventors: Zdenko Casar, Damjan Sterk, Marko Jukic
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Patent number: 8653265Abstract: A preparation method of rosuvastatin calcium (Formula 1), which can be used for the production of medicament lowering the levels of LDL-cholesterol and triglycerides in vivo, is provided. Such preparation method is suitable for industrial production. Furthermore, the intermediate crystallines used in the preparation method are provided.Type: GrantFiled: May 27, 2009Date of Patent: February 18, 2014Assignee: Changzhou Pharmaceutical FactoryInventors: Benshun Chen, Bing Wang, Xiaofeng Jin, Lin Zou
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Publication number: 20140038990Abstract: The present invention relates to a compound having the general formula (Di), (Dii), or (Diii), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: August 5, 2013Publication date: February 6, 2014Applicants: SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORATORY, F. HOFFMANN-LA ROCHE AGInventors: Helmut BUSCHMANN, Andrea WOLKERSTORFER, Oliver SZOLAR, Norbert HANDLER, Stephen CUSACK, Mark SMITH, Sung-Sau SO
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Patent number: 8614222Abstract: The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.Type: GrantFiled: November 13, 2009Date of Patent: December 24, 2013Assignee: The Trustees of Columbia University in the City of New YorkInventors: Gerard Karsenty, Patricia F. Ducy, Vijay Kumar Yadav, Donald Landry, Shi-Xian Deng
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Publication number: 20130338179Abstract: The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.Type: ApplicationFiled: February 24, 2012Publication date: December 19, 2013Applicant: YUHAN CORPORATIONInventors: Hyun-Joo Lee, Dong-Hoon Kim, Tae-Kyun Kim, Young-Ae Yoon, Jae-Young Sim, Myung-Hun Cha, Eun-Jung Jung, Kyoung-Kyu Ahn, Tai-Au Lee
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Patent number: 8609679Abstract: The present invention provides 2,4-diaminopyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: November 7, 2012Date of Patent: December 17, 2013Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell C. Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Patent number: 8604055Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.Type: GrantFiled: June 28, 2006Date of Patent: December 10, 2013Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dagar, Shanavas Alikunju
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Patent number: 8592432Abstract: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-1R), and/or insulin receptor (InsR) or a combination thereof.Type: GrantFiled: April 3, 2009Date of Patent: November 26, 2013Inventors: Bei Chen, Tao Jiang, Thomas H. Marsilje, Pierre-Yves Michellys, Truc Ngoc Nguyen, Wei Pei, Baogen Wu, Zhaobo Gao, Yonghui Ge, Chen Huang, Yuncheng Li, Xuefeng Zhu
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Publication number: 20130296561Abstract: The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.Type: ApplicationFiled: January 13, 2012Publication date: November 7, 2013Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.Inventors: Karin Henderika Maria Bessembinder, Dennis Heemskerk, Ben De Lange
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Publication number: 20130296353Abstract: The present invention is related to crystalline forms of rosuvastatin zinc (2:1) salt. The polymorphs are suitable for use as pharmaceutically active ingredients in the treatment of the diseases of the lipid metabolism including hypercholesterolemia, hyperlipidemia, dyslipidemia or atherosclerosis.Type: ApplicationFiled: November 16, 2011Publication date: November 7, 2013Applicant: EGIS Gyogyszergyar Nyilvanosan Mukodo Reszvenytar- sasagInventors: Imre Markovits, Ferenc Jurak, Gyorgyi Kovanyine Lax, Csaba Hamori, Balazs Havasi, Eva Sipos, Balazs Volk, Zsolt Runge, Krisztina Fodorne Kocsmar, Gyula Lukacs, Katalin Kataine Fadgyas, Monika Mezovari
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Patent number: 8575342Abstract: Compounds of formula (I), N-oxides, pharmaceutical acceptable salts, quaternary amines or stereoisomeric forms thereof, and their use as HIV replication inhibitors, In the formula, -a1=a2-a3=a4- and -b1=b2-b3=b4- may be —C?C—C?C—; X1 may be O, NR1, etc.; R1, R2, R2a, R3, R4 and R5 are assorted substituents as defined in the specification.Type: GrantFiled: September 29, 2005Date of Patent: November 5, 2013Assignee: Tibotech Pharmaceuticals Ltd.Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Patent number: 8575343Abstract: The present invention provides an improved process for the preparation of (E)-N-(4-(4-fluorophenyl)-6-isopropyl-5-(3-oxoprop-1-enyl)pyrimidin-2-yl)-N-methyl methanesulfon-amide, which is a useful intermediate for the preparation of (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl methylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxy hept-6-enoic acid, commonly known as Rosuvastatin.Type: GrantFiled: June 7, 2010Date of Patent: November 5, 2013Assignee: Pharmathen S.A.Inventors: Theoharis V. Koftis, Thanos Andreou, Aristotelis Menisiou, Efstratios Neokosmidis, Asteria Zitrou
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Publication number: 20130281475Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: June 13, 2013Publication date: October 24, 2013Inventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
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Publication number: 20130281694Abstract: The present invention is related to methods for the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S,6E)-dihydroxy-hept-6-enoic acid, intermediates thereof and methods for producing said intermediates.Type: ApplicationFiled: November 29, 2011Publication date: October 24, 2013Applicant: EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENY-TARSASAGInventors: Marta Porcs-Makkay, Ferenc Lorant Bartha, Gyorgy Krasznai, Balazs Volk, Gyorgy Ruzsics, Laszlo Pongo, Gyula Lukacs, Tibor Szabo, Jozsef Barkoczy, Jozsef Debreczeni, Adrienn Keszthelyi, Angela Pandur, Eniko Molnar, Matyas Milen, Maria Tothne Lauritz
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Publication number: 20130261141Abstract: The present application relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which also include arthropods and especially insects.Type: ApplicationFiled: October 17, 2011Publication date: October 3, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Thomas Bretschneider, Adeline Köhler, Joachim Kluth, Martin Füsslein, Peter Jeschke, Reiner Fischer, Friedrich August Mühlthau, Olga Malsam, Arnd Voerste, Klaus-Helmut Müller, Yoshitaka Sato
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Patent number: 8536330Abstract: The present invention provides a process for preparing novel intermediates of Formula wherein, R1 can be hydrogen, C1-C4 alkyl, halogen, nitro, hydroxy, or C1-C4 alkoxy; Rx can be selected from hydrophobic residue of HMG-CoA reductase inhibitors; which can be effectively used for the preparation of HMG-CoA reductase inhibitors such as rosuvastatin and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 21, 2011Date of Patent: September 17, 2013Assignee: Ranbaxy Laboratories LimitedInventors: Vishwesh Pravinchandra Pandya, Santosh Richhariya, Prabhakar Divya, Hashim Nizar Poovanathil Nagoor Meeran, Neera Tewari
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Publication number: 20130237553Abstract: A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and sorbitol. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystal-lization behaviour and stability.Type: ApplicationFiled: November 21, 2011Publication date: September 12, 2013Applicant: BASF SEInventors: Andreas Hafner, Fritz Blatter, Martin Szelagiewicz, Bernd Siebenhaar
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Publication number: 20130225622Abstract: Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.Type: ApplicationFiled: April 8, 2013Publication date: August 29, 2013Applicant: AstraZeneca UK LimitedInventor: AstraZeneca UK Limited
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Patent number: 8513412Abstract: This invention relates to the discovery of novel rosuvastatin and atorvastatin analogues.Type: GrantFiled: March 10, 2010Date of Patent: August 20, 2013Assignee: RedX Pharna LimitedInventors: Derek Lindsay, Peter Jackson, Stephen Hindley, Inder Bhamra
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Publication number: 20130210848Abstract: The present invention relates to a salt of a pyrimidin derivative of the acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic, to a method for preparing same and to the use thereof in formulating pharmaceutical formulations.Type: ApplicationFiled: October 4, 2011Publication date: August 15, 2013Applicant: LABORATORIOS SENOSIAIN S.A. DE C.V.Inventors: Juan Pablo Senosiain Peláez, Héctor Senosiain Arroyo, Manuel Francisco Lara Ochoa
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Patent number: 8507515Abstract: Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterization are disclosed.Type: GrantFiled: July 15, 2011Date of Patent: August 13, 2013Assignee: Novartis AGInventor: Michael Mutz
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Patent number: 8507512Abstract: This inventions relates to compounds having the structure Formula I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.Type: GrantFiled: February 24, 2010Date of Patent: August 13, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Ronald M. Kim, Emma R. Parmee, Christopher Joseph Sinz, Olga A. Ziouzina
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Publication number: 20130197224Abstract: A preparation method of rosuvastatin calcium (Formula 1), which can be used for the production of medicament lowering the levels of LDL-cholesterol and triglycerides in vivo, is provided. Such preparation method is suitable for industrial production. Furthermore, the intermediate crystallines used in the preparation method are provided.Type: ApplicationFiled: March 5, 2013Publication date: August 1, 2013Applicant: CHANGZHOU PHARMACEUTICAL FACTORYInventor: Changzhou Pharmaceutical Factory
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Patent number: 8476432Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.Type: GrantFiled: June 30, 2011Date of Patent: July 2, 2013Assignee: Yuhan CorporationInventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Publication number: 20130158263Abstract: A compound of Formula (1), is disclosed wherein P1 and P2 are alcohol protecting groups or 1,3-diol protecting group, R is selected from: wherein R4a is selected from alkyl, aryl, arylalkyl and cycloalkyl, Rc is selected from H, alkyl, aryl, alkaoxy, haloalkyl, monohaloalkyloxy, and dihaloalkyloxy, Rd is selected from alkyl, aryl, arylalkyl, CF3, halo and NO2 and X is selected from O, N—H, N-alkyl and S, Ra and Rb are same or different and each represents hydrogen, an alkyl group of 1 to 12 carbon atoms, an aryl group of 6 to 12 carbon atoms, or an aralkyl group of 7 to 12 carbon atoms.Type: ApplicationFiled: February 23, 2011Publication date: June 20, 2013Inventors: Shriprakash Dhar Dwivedi, Dhimant Jasubhai Patel, Mahesh Laljibhai Rupapara
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Publication number: 20130150579Abstract: The present invention provides a process for preparing novel intermediates of Formula wherein, R1 can be hydrogen, C1-C4 alkyl, halogen, nitro, hydroxy, or C1-C4 alkoxy; Rx can be selected from hydrophobic residue of HMG-CoA reductase inhibitors; which can be effectively used for the preparation of HMG-CoA reductase inhibitors such as rosuvastatin and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 21, 2011Publication date: June 13, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Vishwesh Pravinchandra Pandya, Santosh Richhariya, Prabhakar Divya, Hashim Nizar Poovanathil Nagoor Meeran, Neera Tewari
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Publication number: 20130143890Abstract: Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.Type: ApplicationFiled: December 3, 2012Publication date: June 6, 2013Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventor: F.I.S. Fabbrica Italiana Sintetici S.p.A.
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Patent number: 8455497Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 12, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill