Acyclic Nitrogen Bonded Directly To The Carbonyl Patents (Class 546/316)
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Patent number: 11174229Abstract: Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, having the structure of a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.Type: GrantFiled: October 29, 2019Date of Patent: November 16, 2021Assignee: KemPharm, Inc.Inventors: Sven Guenther, Guochen Chi, Travis Mickle
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Patent number: 10766858Abstract: The invention provides compounds having the general formula I: (i) and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, ring B, R1, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: GrantFiled: March 28, 2017Date of Patent: September 8, 2020Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Steven McKerrall, Daniel Sutherlin
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Patent number: 10364225Abstract: 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: GrantFiled: January 9, 2017Date of Patent: July 30, 2019Assignee: JIANGSU ROTAM CHEMISTRY CO., LTD.Inventor: James Timothy Bristow
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Patent number: 10098859Abstract: 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: GrantFiled: September 4, 2013Date of Patent: October 16, 2018Assignee: AMRI SSCI, LLCInventors: Melanie Janelle Bevill, Nate Schultheiss
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Patent number: 9771376Abstract: 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: GrantFiled: April 19, 2016Date of Patent: September 26, 2017Assignees: 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
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Patent number: 9738589Abstract: 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: GrantFiled: June 15, 2016Date of Patent: August 22, 2017Assignee: DAIKIN INDUSTRIES, LTD.Inventors: Tatsuya Ohtsuka, Akihiro Gotou, Sumi Ishihara, Yoshihiro Yamamoto, Akinori Yamamoto, Yoshichika Kuroki, Yuzo Komatsu, Yousuke Kishikawa
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Patent number: 9278136Abstract: 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: GrantFiled: May 15, 2014Date of Patent: March 8, 2016Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 9227923Abstract: 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: GrantFiled: August 3, 2010Date of Patent: January 5, 2016Assignee: Bayer Intellectual Property GmbHInventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Yukiyoshi Watanabe, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Gorgens
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Publication number: 20150126462Abstract: 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: ApplicationFiled: June 14, 2013Publication date: May 7, 2015Applicant: CONARIS RESEARCH INSTITUTE AGInventors: Georg Waetzig, Dirk Seegert
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Publication number: 20150126493Abstract: 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: ApplicationFiled: May 3, 2013Publication date: May 7, 2015Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
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Publication number: 20150119428Abstract: 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: ApplicationFiled: March 29, 2013Publication date: April 30, 2015Inventors: Joanne Holland, Christopher Frampton
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Publication number: 20150099636Abstract: 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: ApplicationFiled: October 9, 2014Publication date: April 9, 2015Inventors: Robert Eugene HORMANN, Bing Li
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Publication number: 20150072416Abstract: 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: ApplicationFiled: April 26, 2013Publication date: March 12, 2015Applicant: Korea Research Institute of Bioscience and BiotechInventors: Yee Sook Cho, Myung Jin Son, Mi Young Son
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Publication number: 20150065721Abstract: 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: ApplicationFiled: March 29, 2013Publication date: March 5, 2015Applicant: Mitsui Chemicals Agro, Inc.Inventor: Hironari Okura
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Patent number: 8962656Abstract: 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: GrantFiled: May 26, 2011Date of Patent: February 24, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
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Publication number: 20150050497Abstract: 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: ApplicationFiled: April 4, 2013Publication date: February 19, 2015Inventors: Detlef Gerritzen, Norbert Clausen, Heike Irle, Uwe Zacher
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Publication number: 20150045367Abstract: 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: ApplicationFiled: December 19, 2012Publication date: February 12, 2015Inventors: Erik Verner, Wei Chen, Sriram Balasubramanian
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Patent number: 8952169Abstract: 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: GrantFiled: May 21, 2013Date of Patent: February 10, 2015Assignees: 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
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Publication number: 20150037268Abstract: 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: ApplicationFiled: August 22, 2012Publication date: February 5, 2015Inventors: Sung-Ae Choi, Hyuk-Kwang Jeong, Young-Mi Byoun, Jun-Seob Shin, Seo Joon Yoo, Sang-Chul Yoo
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Patent number: 8940903Abstract: 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: GrantFiled: April 2, 2012Date of Patent: January 27, 2015Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 8933236Abstract: 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: GrantFiled: May 21, 2013Date of Patent: January 13, 2015Assignees: 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
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Patent number: 8921391Abstract: 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: GrantFiled: April 22, 2010Date of Patent: December 30, 2014Assignee: RaQualia Pharma Inc.Inventors: Yukinori Take, Shinichi Koizumi, Takako Okumura, Kazuhiko Nonomura
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Publication number: 20140364457Abstract: 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: ApplicationFiled: August 26, 2014Publication date: December 11, 2014Inventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
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Publication number: 20140343086Abstract: 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: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Applicant: NOVARTIS AGInventors: 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
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Publication number: 20140329854Abstract: 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: ApplicationFiled: December 12, 2012Publication date: November 6, 2014Applicant: SMB InnovationInventors: Bjarne Due Larsen, Soren Andersen, Marianne Spanget Larsen
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Publication number: 20140323736Abstract: 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: ApplicationFiled: November 23, 2012Publication date: October 30, 2014Inventors: Hans-Georg Schwarz, Axel Trautwein, Lothar Willms, Maike Hink, Peter Lummen, Ulrich Gorgens, Pierre-Yves Coqueron, Achim Harder, Claudia Welz
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Publication number: 20140315786Abstract: 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: ApplicationFiled: March 16, 2012Publication date: October 23, 2014Applicant: Catabasis Pharmaceuticals, Inc.Inventors: Michael R. Jirousek, Jill C. Milne, David Carney, Jean E. Bemis, Chi B. Vu
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Patent number: 8846012Abstract: 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: GrantFiled: December 22, 2009Date of Patent: September 30, 2014Assignee: Pola Chemical Industries Inc.Inventors: Kouji Yokoyama, Makoto Kimura, Masashi Tamai, Yuko Saitoh, Tomomi Kato, Yu Ikeda
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Patent number: 8846721Abstract: 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: GrantFiled: January 22, 2011Date of Patent: September 30, 2014Assignee: Kareus Therapeutics SAInventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
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Publication number: 20140275008Abstract: 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: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Qing Xu, Zhe Li
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Publication number: 20140272601Abstract: 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: ApplicationFiled: November 16, 2012Publication date: September 18, 2014Inventors: Erlendur Jónsson, Michel Bernard Armand, Jens Patrik Johansson
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Patent number: 8835467Abstract: 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: GrantFiled: January 23, 2013Date of Patent: September 16, 2014Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
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Patent number: 8829195Abstract: 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: GrantFiled: May 13, 2013Date of Patent: September 9, 2014Assignee: Novartis AGInventors: 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
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Patent number: 8815905Abstract: 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: GrantFiled: March 8, 2011Date of Patent: August 26, 2014Assignee: Promentis Pharmaceuticals, Inc.Inventors: Mark A. Wolf, Keith D. Barnes
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Patent number: 8815857Abstract: 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: GrantFiled: August 9, 2012Date of Patent: August 26, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Todd Bosanac, Angela Berry, John David Ginn, Tamara Denise Hopkins, Sabine Schlyer, Fariba Soleymanzadeh, John Westbrook, Maolin Yu, Zhonghua Zhang
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Publication number: 20140228413Abstract: 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: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu, Amal Ting
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
Patent number: 8802720Abstract: 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: GrantFiled: April 22, 2013Date of Patent: August 12, 2014Assignee: SanofiInventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek -
Publication number: 20140220050Abstract: 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: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan MUTHUPPALANIAPPAN, Prashant Kashinath Bhavar, Srikant Viswanadha, Swaroop Kumar V.S. Vakkalanka, Gayatri Swaroop Merikapudi
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Patent number: 8791102Abstract: 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: GrantFiled: October 16, 2009Date of Patent: July 29, 2014Assignee: 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
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Patent number: 8765964Abstract: 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: GrantFiled: December 30, 2013Date of Patent: July 1, 2014Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 8765963Abstract: 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: GrantFiled: April 19, 2012Date of Patent: July 1, 2014Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu, Amal Ting
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Publication number: 20140171446Abstract: 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: ApplicationFiled: May 3, 2012Publication date: June 19, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Gary Bohnert, Jun Jiang, Zhiqiang Xia
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Publication number: 20140147529Abstract: 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: ApplicationFiled: December 20, 2011Publication date: May 29, 2014Applicant: DSM IP ASSETS B.V.Inventors: Stephane Duval, Maik Kindermann
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Process for the production of particles comprising active agrochemical ingredients in amorphous form
Patent number: 8735321Abstract: 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: GrantFiled: May 6, 2009Date of Patent: May 27, 2014Assignee: BASF SEInventors: Ulrike Troppmann, Winfried Mayer, Sebastian Koltzenburg, Rafel Israels, Andreas Bauder, Ulf Schlotterbeck -
Publication number: 20140135328Abstract: 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: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Publication number: 20140121367Abstract: 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: ApplicationFiled: April 9, 2012Publication date: May 1, 2014Inventors: Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
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Patent number: 8710073Abstract: 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: GrantFiled: February 6, 2009Date of Patent: April 29, 2014Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite Paul Sabatier Toulouse IIIInventors: Jean Bernadou, Vania Bernardes-Genisson, Tamara Delaine, Annaïck Quemard
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Patent number: 8710234Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: GrantFiled: September 20, 2013Date of Patent: April 29, 2014Assignee: 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
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Patent number: RE45261Abstract: 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: GrantFiled: December 16, 2013Date of Patent: November 25, 2014Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: RE45275Abstract: 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: GrantFiled: December 16, 2013Date of Patent: December 2, 2014Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu