Acyclic Nitrogen Bonded Directly To The Carbonyl Patents (Class 546/316)
  • Patent number: 10364225
    Abstract: A process for preparing the polymorph I of the anhydrate of 2-Chloro-N-(4?-chlorobiphenyl-2-yl)-nicotinamide (boscalid) of the formula I: is provided. The process comprises the steps of: a) dissolving the polymorph II of the anhydrate of boscalid in a first solvent in an amount and at conditions allowing dissolution of the polymorph II of the anhydrate of boscalid; b) combining the resulting solution with water; c) isolating the solid from the solvent mixture; and d) drying the solid to obtain the polymorph I of the anhydrate of boscalid.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: July 30, 2019
    Assignee: JIANGSU ROTAM CHEMISTRY CO., LTD.
    Inventor: James Timothy Bristow
  • Patent number: 10098859
    Abstract: Disclosed herein are cocrystals of p-coumaric acid and nicotinamide. A 1:1 molar ratio and a 2:1 molar ratio of p-coumaric acid to nicotinamide are herein disclosed.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: October 16, 2018
    Assignee: AMRI SSCI, LLC
    Inventors: Melanie Janelle Bevill, Nate Schultheiss
  • Patent number: 9771376
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: April 19, 2016
    Date of Patent: September 26, 2017
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel F. Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Patent number: 9738589
    Abstract: The object of the present invention is to provide a process for producing ?-fluoroacrylic acid ester at a high starting material conversion, high selectivity, and high yield. The present invention provides a process for producing the compound represented by the formula (1) wherein R represents alkyl optionally substituted with one or more fluorine atoms, the process comprising step A of reacting a compound represented by the formula (2) wherein X represents a bromine atom or a chlorine atom with an alcohol represented by the formula (3) wherein the symbol is as defined above, and carbon monoxide in the presence of a transition metal catalyst and a base to thereby obtain the compound represented by the formula (1).
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: August 22, 2017
    Assignee: DAIKIN INDUSTRIES, LTD.
    Inventors: Tatsuya Ohtsuka, Akihiro Gotou, Sumi Ishihara, Yoshihiro Yamamoto, Akinori Yamamoto, Yoshichika Kuroki, Yuzo Komatsu, Yousuke Kishikawa
  • Patent number: 9278136
    Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: March 8, 2016
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Patent number: 9227923
    Abstract: The object of the present invention is to provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Disclosed are the carboxamides represented by the following Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite controlling agents.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: January 5, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Yukiyoshi Watanabe, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Gorgens
  • Publication number: 20150126462
    Abstract: The present invention relates to a new pharmaceutical composition containing nicotinic acid, nicotinamide, tryptophanor related compounds for positively influencing the intestinal microbiota. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.
    Type: Application
    Filed: June 14, 2013
    Publication date: May 7, 2015
    Applicant: CONARIS RESEARCH INSTITUTE AG
    Inventors: Georg Waetzig, Dirk Seegert
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150119428
    Abstract: Mew tranilast complexes and new tranilast cocrystals are disclosed. These include all tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-amtnoben2oic acid complex, a 1:1 tranilast 4-am!nobers2oic acid cocrystal, a 1:1 tranilast 2,4-di?hydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystais as well as the pharmaceutical compositions are disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: April 30, 2015
    Inventors: Joanne Holland, Christopher Frampton
  • Publication number: 20150099636
    Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 9, 2015
    Inventors: Robert Eugene HORMANN, Bing Li
  • Publication number: 20150072416
    Abstract: According to the present invention, when nicotinamide is added in a culture process for producing pluripotent stem cells from human differentiated cells, it can increase the efficiency of reprogramming and can significantly reduce the time required for induction of reprogramming. It was verified that nicotinamide inhibits the induction of senescence and oxidative stress in the reprogramming process and increases cell proliferation and mitochondrial activity to effectively improve culture conditions for induction of reprogramming. Particularly, the present invention will contribute to optimizing a process of producing induced pluripotent stem cells from a small amount of patient-specific somatic cells obtained from various sources, and thus it will significantly improve a process of developing clinically applicable personalized stem cell therapy agents and new drugs and will facilitate the practical application of these agents and drugs.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 12, 2015
    Applicant: Korea Research Institute of Bioscience and Biotech
    Inventors: Yee Sook Cho, Myung Jin Son, Mi Young Son
  • Publication number: 20150065721
    Abstract: Provided is a method for producing an aromatic amide derivative represented by Formula (4), the method including a process in which an aromatic amide derivative represented by Formula (1) and a haloalkyl compound represented by Formula (3) are reacted with each other in the presence of a base and a metal or metal salt. In the formulae, each of X and Y represents a hydrogen atom, a halogen atom, or the like. A represents a hydrogen atom, an alkyl group, a group represented by Formula (2), or the like. Each of G1 and G2 represents an oxygen atom or the like. Q1 represents a phenyl group or the like. R1 represents a hydrogen atom, an alkyl group, or the like. Z1 represents a haloalkyl group or the like. Xa represents an iodine atom or the like. m represents a number of from 1 to 4, n1 represents a number from 1 to 5, and n2 represents a number of from 1 to 4.
    Type: Application
    Filed: March 29, 2013
    Publication date: March 5, 2015
    Applicant: Mitsui Chemicals Agro, Inc.
    Inventor: Hironari Okura
  • Patent number: 8962656
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (Ia) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
  • Publication number: 20150050497
    Abstract: The invention relates to a process for the preparation of a nicotinamide powder, comprising the steps of providing an aqueous solution of nicotinamide and spray drying the solution. The invention also relates to a nicotinamide powder, devices for its production and uses.
    Type: Application
    Filed: April 4, 2013
    Publication date: February 19, 2015
    Inventors: Detlef Gerritzen, Norbert Clausen, Heike Irle, Uwe Zacher
  • Publication number: 20150045367
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: December 19, 2012
    Publication date: February 12, 2015
    Inventors: Erik Verner, Wei Chen, Sriram Balasubramanian
  • Patent number: 8952169
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: February 10, 2015
    Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.
    Inventors: Jean-Christophe Andrez, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Daniel F. Ortwine, Brian Safina, Tao Sheng, Shaoyi Sun, Daniel P. Sutherlin, Michael Scott Wilson, Alla Yurevna Zenova
  • Publication number: 20150037268
    Abstract: Provided is niacin-peptide which has skin whitening activity. The peptide of the present invention has skin whitening activity by inhibiting melanogenesis, that is, by inhibiting the expression of a gene related to melanogenesis (for example, TRP-1, TRP2, or MIFT). The peptide of the present invention has high stability and skin permeability. Also provided is a cosmetic composition for skin whitening which contains the niacin-peptide.
    Type: Application
    Filed: August 22, 2012
    Publication date: February 5, 2015
    Inventors: Sung-Ae Choi, Hyuk-Kwang Jeong, Young-Mi Byoun, Jun-Seob Shin, Seo Joon Yoo, Sang-Chul Yoo
  • Patent number: 8940903
    Abstract: The invention relates to niacin conjugated fatty acid mixtures; compositions comprising an effective amount of a niacin conjugated fatty acid mixture; and methods for treating or preventing an metabolic disorder comprising the administration of an effective amount of a niacin conjugated fatty acid mixture.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: January 27, 2015
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Patent number: 8933236
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: January 13, 2015
    Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Patent number: 8921391
    Abstract: This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: December 30, 2014
    Assignee: RaQualia Pharma Inc.
    Inventors: Yukinori Take, Shinichi Koizumi, Takako Okumura, Kazuhiko Nonomura
  • Publication number: 20140364457
    Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer's disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Inventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
  • Publication number: 20140343086
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Applicant: NOVARTIS AG
    Inventors: Stephanie Kay DODD, Pascal FURET, Robert Martin GROTZFELD, Wolfgang JAHNKE, Darryl Brynley JONES, Paul William MANLEY, Andreas MARZINZIK, Xavier Francois Andre PELLE, Bahaa SALEM, Joseph SCHOEPFER
  • Publication number: 20140329854
    Abstract: Provided are novel heterocyclic sirtuin binding agents, e.g., N-aryl substituted pyridine dicarboxamides, which are useful as sirtuin modulators. Also provided are methods of using the pyridine dicarboxamide compounds for treating sirtuin mediated disorders and conditions, such as diabetes, cancers, and obesity and diseases related to aging.
    Type: Application
    Filed: December 12, 2012
    Publication date: November 6, 2014
    Applicant: SMB Innovation
    Inventors: Bjarne Due Larsen, Soren Andersen, Marianne Spanget Larsen
  • Publication number: 20140323736
    Abstract: The present application relates to known and novel aryl- and hetarylcarboxamides of the formula (I) and to their use as medicaments for controlling endoparasites in animals or humans, and also to parasiticidal compositions, in particular endoparasites, comprising aryl- and hetarylcyclylcarboxamides.
    Type: Application
    Filed: November 23, 2012
    Publication date: October 30, 2014
    Inventors: Hans-Georg Schwarz, Axel Trautwein, Lothar Willms, Maike Hink, Peter Lummen, Ulrich Gorgens, Pierre-Yves Coqueron, Achim Harder, Claudia Welz
  • Publication number: 20140315786
    Abstract: The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalently linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.
    Type: Application
    Filed: March 16, 2012
    Publication date: October 23, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Michael R. Jirousek, Jill C. Milne, David Carney, Jean E. Bemis, Chi B. Vu
  • Patent number: 8846721
    Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer?s Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: January 22, 2011
    Date of Patent: September 30, 2014
    Assignee: Kareus Therapeutics SA
    Inventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
  • Patent number: 8846012
    Abstract: Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor is represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: September 30, 2014
    Assignee: Pola Chemical Industries Inc.
    Inventors: Kouji Yokoyama, Makoto Kimura, Masashi Tamai, Yuko Saitoh, Tomomi Kato, Yu Ikeda
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Publication number: 20140272601
    Abstract: Salts with formula X?M+ wherein M+ is Li, Na, K, an ammonium, a phosphonium, an imidazolium, a pyridinium, or a pyrazolium and X? is an anion formed from covalent linking of two negative moieties to a positive onium-type core are provided. Also provided are electrolytes and batteries produced from these salts.
    Type: Application
    Filed: November 16, 2012
    Publication date: September 18, 2014
    Inventors: Erlendur Jónsson, Michel Bernard Armand, Jens Patrik Johansson
  • Patent number: 8835467
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: September 16, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Patent number: 8829195
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Grant
    Filed: May 13, 2013
    Date of Patent: September 9, 2014
    Assignee: Novartis AG
    Inventors: Stephanie Kay Dodd, Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Patent number: 8815857
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: August 26, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Todd Bosanac, Angela Berry, John David Ginn, Tamara Denise Hopkins, Sabine Schlyer, Fariba Soleymanzadeh, John Westbrook, Maolin Yu, Zhonghua Zhang
  • Patent number: 8815905
    Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).
    Type: Grant
    Filed: March 8, 2011
    Date of Patent: August 26, 2014
    Assignee: Promentis Pharmaceuticals, Inc.
    Inventors: Mark A. Wolf, Keith D. Barnes
  • Publication number: 20140228413
    Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu, Amal Ting
  • Patent number: 8802720
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: August 12, 2014
    Assignee: Sanofi
    Inventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek
  • Publication number: 20140220050
    Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant Kashinath Bhavar, Srikant Viswanadha, Swaroop Kumar V.S. Vakkalanka, Gayatri Swaroop Merikapudi
  • Patent number: 8791102
    Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: July 29, 2014
    Assignee: Exelixis, Inc.
    Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
  • Patent number: 8765963
    Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: July 1, 2014
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu, Amal Ting
  • Patent number: 8765964
    Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.
    Type: Grant
    Filed: December 30, 2013
    Date of Patent: July 1, 2014
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Publication number: 20140171446
    Abstract: The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 3, 2012
    Publication date: June 19, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Gary Bohnert, Jun Jiang, Zhiqiang Xia
  • Publication number: 20140147529
    Abstract: The present invention relates to a method for reducing the production of methane emanating from the digestive activities of a ruminant and/or for improving ruminant animal performance by using, as active compound at least one organic molecule substituted at any position with at least one nitrooxy group, or a salt thereof, which is administrated to the animal together with the feed. The invention also relates to the use of these compounds in feed and feed additives such as premix, concentrates and total mixed ration (TMR) or in the form of a bolus.
    Type: Application
    Filed: December 20, 2011
    Publication date: May 29, 2014
    Applicant: DSM IP ASSETS B.V.
    Inventors: Stephane Duval, Maik Kindermann
  • Patent number: 8735321
    Abstract: An object of the present invention is a process for the preparation of particles which comprise two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is the use of an agrochemical active ingredient for inhibiting the crystallization of another agrochemical active ingredient in a preparation process for particles which comprise the two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is particles which comprise two agrochemical active ingredients in amorphous form. The use in plant protection is also described.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: May 27, 2014
    Assignee: BASF SE
    Inventors: Ulrike Troppmann, Winfried Mayer, Sebastian Koltzenburg, Rafel Israels, Andreas Bauder, Ulf Schlotterbeck
  • Publication number: 20140135328
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Applicant: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
  • Publication number: 20140121367
    Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
    Type: Application
    Filed: April 9, 2012
    Publication date: May 1, 2014
    Inventors: Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
  • Patent number: 8710073
    Abstract: The present invention relates to bi-substrate inhibitor molecules combining (i) a pyridine, pyridinium or dihydropyridine-type structure allied to active metabolites of isoniazide, or related structures, and (ii) a hydrophobic substituent. The invention also relates to the method for preparing said molecules, to the pharmaceutical compositions containing said molecules, and to the use thereof as inhibitors of enoyl reductase for the preparation of a drug, especially an anti-infective drug for the treatment of tuberculosis.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: April 29, 2014
    Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite Paul Sabatier Toulouse III
    Inventors: Jean Bernadou, Vania Bernardes-Genisson, Tamara Delaine, Annaïck Quemard
  • Patent number: 8710234
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: April 29, 2014
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Publication number: 20140113898
    Abstract: The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.
    Type: Application
    Filed: November 4, 2011
    Publication date: April 24, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan A. Pajouhesh, Richard Holland, Yuanxi Zhou, Yongbao Zhu, Michael Edward Grimwood, Navjot Chahal
  • Publication number: 20140107076
    Abstract: Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 17, 2014
    Applicant: THAR PHARMACEUTICALS, INC.
    Inventor: THAR PHARMACEUTICALS, INC.
  • Patent number: RE45261
    Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: November 25, 2014
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Patent number: RE45275
    Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: December 2, 2014
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu