Abstract: Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.
Abstract: The present invention relates to a composition for the modulation of the activity of non-structure proteins and a compound contained therein.
Type:
Application
Filed:
January 30, 2019
Publication date:
May 30, 2019
Inventors:
Bernhard Hirt, Claus Zeyher, Corinna Gleiser, Lothar Just
Abstract: The present invention relates to indole compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.
Abstract: The present invention relates to a compound represented by formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
Type:
Application
Filed:
May 19, 2017
Publication date:
May 30, 2019
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Gregory L. Adams, Jason M. Cox, John S. Debenham, Scott Edmondson, Eric J. Gilbert, Yan Guo, Yu Jiang, Hubert Josien, Hyunjin M. Kim, Ping Lan, Shouwu Miao, Christopher W. Plummer, Murali Rajagopalan, Unmesh Shah, Zhongxiang Sun, Quang T. Truong, Feroze Ujjainwalla, Francisco Velazquez, Srikanth Venkatraman, Takao Suzuki, Nengxue Wang
Abstract: Compounds of Formula I or pharmaceutically acceptable salts or esters thereof capable of binding to and modulating the activity of a stimulator of interferon genes (STING) protein are provided. Methods involving compounds of Formula I as effective modulators of STING are also provided.
Type:
Application
Filed:
November 20, 2018
Publication date:
May 30, 2019
Inventors:
Brian T. CHAMBERLAIN, James M. RICE, Finith E. JERNIGAN, III, Woody SHERMAN, Meghana M. KULKARNI, Sharon SHECHTER, Bryce K. ALLEN, Dazhi TAN, Kristen A. MARINO, Zhixiong LIN
Abstract: Described herein are compounds and formulations thereof that can bind PTEN. Also described herein are methods of using the compounds and formulations thereof that can bind PTEN. In some embodiments, the method can include administering an amount of a compound or formulation described herein to a subject in need thereof.
Abstract: The present invention relates to the pyrimidine compounds of formula (I), or their agriculturally acceptable salts or derivatives as herbicides, wherein the variables are defined according to the description, use of pyrimidine compounds of formula (I) as herbicides, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one pyrimidine compound of the formula (I) to act on plants, their seed and/or their habitat.
Type:
Application
Filed:
July 10, 2017
Publication date:
May 30, 2019
Inventors:
Florian VOGT, Matthias WITSCHEL, Tobias SEISER, Veronica LOPEZ CARRILLO, Thomas SEITZ, Gerd KRAEMER, Trevor William NEWTON, Klaus REINHARD
Abstract: Process for the preparation of azidoperfluoroalkanes and azidopolyfluoroalkanes of general formula RF—N3, where RF is chosen from a group containing CnF2n+1, CnFxH2n+1?x, CnFxX2n+1?x or R1CF2CF2, where n is an integer in the range of 1 to 10, x is an integer in the range of 2 to 20, X is Cl, Br, or I, R1 is C1-10 alkyl, ArO, ArS, imidazolyl, benzimidazolyl, or pyrazolyl and Ar is phenyl or substituted phenyl, by the reaction of electrophilic azidation reagent of general formula R2—N3, where R2 is n-C4F9SO2, ArSO2, Br, I, with synthetic equivalent of polyfluoroalkylated carbanion of general formula [RF]?.
Type:
Application
Filed:
November 30, 2017
Publication date:
May 30, 2019
Applicants:
Ustav organicke chemie a biochemie AV CR, v.v.i., CF Plus Chemicals s.r.o.
Inventors:
Petr BEIER, Vaclav MATOUSEK, Zsofia E. BLASTIK, Svatava VOLTROVA
Abstract: The present invention relates to novel Oxoalkyl-substituted 1-phenyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular and renal diseases.
Type:
Application
Filed:
May 2, 2017
Publication date:
May 30, 2019
Inventors:
Carsten SCHMECK, Anna ENGELEN, Peter KOLKHOF, Klemens LUSTIG, Elisabeth POOK, Pierre WASNAIRE
Abstract: The present invention relates to novel 5-(carboxamide)-1-phenyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
Type:
Application
Filed:
May 2, 2017
Publication date:
May 30, 2019
Inventors:
Marie-Pierre COLLIN-KRÖPELIN, Peter KOLKHOF, Thomas NEUBAUER, Chantal FÜRSTNER, Elisabeth POOK, Matthias Beat WITTWER, Klemens LUSTIG, Anja BUCHMÜLLER, Hanna TINEL, Karoline DRÖBNER, Thomas MONDRITZKI, Heiko SCHIRMER, Axel KRETSCHMER, Carsten SCHMECK, Pierre WASNAIRE, Hana CERNECKA
Abstract: A method for producing an isocyanuric acid derivative having one hydrocarbon group. The method having a hydrocarbon group including a first step of obtaining a compound of the following formula (1) from the compound of formula (0), a second step of obtaining a compound of the following formula (2) from the compound of formula (1), a third step of obtaining a compound of the following formula (3) from the compound of formula (2), and a fourth step of obtaining a compound of the following formula (4) from the compound of formula (3): (wherein X1s are each a chlorine atom, a fluorine atom, or a bromine atom, Bn is a benzyl group in which at least one hydrogen atom in a benzene ring is optionally substituted with methyl group, and R is a C1-10 hydrocarbon group), wherein all the steps are carried out at a temperature of not exceeding 100° C.
Abstract: 12(S)-hydroxyeicosatrienoic acid (12(S)-HETrE) compounds and compositions comprising the same are disclosed. Methods of using the compounds in the prevention and treatment of thrombosis and thrombotic disorders are also disclosed.
Type:
Application
Filed:
June 23, 2017
Publication date:
May 30, 2019
Inventors:
Michael Holinstat, Theodore R. Holman, Andrew White
Abstract: A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be recycled without significantly losing any catalytic activity in a variety of chemical transformations, a method for producing the solid-supported catalyst ligand and a method for catalyzing a palladium cross-coupling reaction, such as the Suzuki-Miyaura, Mizoroki-Heck, and Sonagashira reactions.
Type:
Application
Filed:
February 1, 2019
Publication date:
May 30, 2019
Applicant:
KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS
Inventors:
Bassam El Ali, Rami Khalid Suleiman, Mansur Bala Ibrahim
Abstract: A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be recycled without significantly losing any catalytic activity in a variety of chemical transformations, a method for producing the solid-supported catalyst ligand and a method for catalyzing a palladium cross-coupling reaction, such as the Suzuki-Miyaura, Mizoroki-Heck, and Sonagashira reactions.
Type:
Application
Filed:
February 1, 2019
Publication date:
May 30, 2019
Applicant:
KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS
Inventors:
Bassam EL ALI, Rami Khalid SULEIMAN, Mansur Bala IBRAHIM
Abstract: Disclosed are polyfunctional compounds of formula: as well as methods for preparing same and the uses thereof, in particular in orthogonal or bioorthogonal processes.
Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
Abstract: The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds Sand compositions for use in wound healing are also described.
Type:
Application
Filed:
November 21, 2018
Publication date:
May 30, 2019
Inventors:
Paul Warren Reddell, Victoria Anne Gordon, Ryan Moseley, Robert Steadman, Rachael Louise Moses, Glen Mathew Boyle, Peter Gordon Parsons
Abstract: A method of converting a lignocellulosic biomass to monosaccharides, and optionally further converting the monosaccharides to one or both of furfural and HMF, includes contacting the biomass with a reactive liquid phase comprising LiBr, H2SO4. and water, wherein H2SO4 preferably constitutes at most 1.0 wt %, more preferably at most 0.5 wt %, and most preferably at most 0.1 wt % of the reactive liquid phase, and water preferably constitutes at most at most 60 wt %, more preferably at most 50 wt %, and most preferably at most 30 wt % of the reactive liquid phase.
Abstract: O-substituted hydroxamic acids with carbon-based leaving groups as HNO donors are disclosed. Pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions also are disclosed.
Type:
Application
Filed:
July 27, 2017
Publication date:
May 30, 2019
Inventors:
John P. Toscano, Saghar Nourian, Daryl A. Guthrie
Abstract: A method for producing a red colorant composition derived from iridoid compounds, including a step of performing red color development that involves reaction of iridoid aglycones having a carboxyl group at position 4 of an iridoid skeleton with amino group-containing compounds, said red color development being performed in a solution in which ascorbic acid, similar compounds thereof, or two or more compounds selected from the group consisting of said ascorbic acid and said similar compounds are contained at a molar ratio of 5 or more with respect to all iridoid compounds in the solution, whereby red colorant compounds having acid resistance are generated.
Type:
Application
Filed:
June 16, 2017
Publication date:
May 30, 2019
Inventors:
Keiko Izumida, Koji Hamasaki, Takamasa Yokoyama
Abstract: The present invention relates to a process for synthesizing lactide, comprising the steps of: adding thermal energy to at least one of one or more components; providing the one or more components to at least one reactor, the one or more components comprising lactic acid and at least one solvent; converting at least part of the lactic acid into lactide and water; recovering at least part of the lactide; recovering at least part of the at least one solvent; recovering at least part of the thermal energy, wherein at least part of the recovered thermal energy is recovered from the recovered solvent; and adding the recovered thermal energy to at least one of the one or more components.
Type:
Application
Filed:
June 20, 2017
Publication date:
May 30, 2019
Inventors:
Mahdi Yazdanpanah, Jamal Chaouki, Pieter Van Wouwe, Bert Sels
Abstract: Novel compounds of N-Lipoic-amino acid, N-Lipoic-peptides and their derivatives are described. Also described are compositions and method of compositions containing the derivatives of the amino acids or peptides, and their uses including treating and preventing dermatological or cosmetic conditions or other disorders of the cutaneous system. Compositions and methods of using the compositions for skin lightening and cosmetics are also disclosed.
Abstract: It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
Type:
Application
Filed:
November 17, 2017
Publication date:
May 30, 2019
Inventors:
Fusheng ZHOU, Shuchun GUO, Jinzhu ZHAO, Hui XU, Xia SHI, Yi HU, Yufeng LI, Jiong LAN
Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
Type:
Application
Filed:
January 7, 2019
Publication date:
May 30, 2019
Inventors:
William J. Hoekstra, Christopher M. Yates, Mark Behnke, Asaf Alimardanov, Scott A. David, Douglas Franklin Fry
Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
Type:
Application
Filed:
January 22, 2019
Publication date:
May 30, 2019
Inventors:
William J. HOEKSTRA, Christopher M. YATES
Abstract: This present disclosure is directed to compounds of formula (I): where R1a, R3, Y, and Z are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions including the compounds described herein and methods of preparing the compounds described herein are also provided.
Type:
Application
Filed:
January 31, 2019
Publication date:
May 30, 2019
Inventors:
Kurt Roinestad, William Guilford, Thomas Kirkland, Lopa Bhatt, Eric B. Springman
Abstract: The present invention relates to novel antibacterial compounds (1) as defined below, pharmaceutical compositions containing them and their use as antimicrobials. A compound of formula (1): A-L1-Y-L2-R-B, wherein A is a cyclic group having one of the following formulae (I), (II) and (III), and wherein B is cyclic group having one of the following formulae (IV) to (IX).
Type:
Application
Filed:
June 5, 2017
Publication date:
May 30, 2019
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
Inventors:
Rosella OMBRATO, Gabriele MAGARO, Barbara GAROFALO, Guido FURLOTTI, Giorgina MANGANO, Alessandra CAPEZZONE DE JOANNON
Abstract: Provided are a chemical compound of an isocitrate dehydrogenase inhibitor, and an application thereof, belonging to the field of medicinal chemistry; specifically provided is the chemical compound represented by formula I, or its isomer, pharmaceutically acceptable salt, crystal, solvate, or prodrug, as well as their preparation methods and pharmaceutical compositions containing said chemical compound, and an application of said chemical compound or composition. The chemical compound has very good ability to inhibit mutant IDH2 enzyme activity and to inhibit mutant IDH2 neoplastic cells, and may be used for preventing and/or treating a tumor characterized by the presence of mutant IDH2.
Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I) to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.
Type:
Application
Filed:
July 18, 2017
Publication date:
May 30, 2019
Inventors:
Luca ARISTA, Sreehari BABU, Jianwei BIAN, Kai CUI, Michael Patrick DILLON, Rene LATTMANN, Jialiang LI, Lv LIAO, Dimitrios LIZOS, Rita RAMOS, Nikolaus Johannes STIEFL, Thomas ULLRICH, Peggy USSELMANN, Xiaoyang WANG, Liladhar Murlidhar WAYKOLE, Sven WEILER, Yubo ZHANG, Yizong ZHOU, Tingying ZHU
Abstract: The present invention aims to provide a new method for producing an indole compound or a salt thereof, which has an ITK inhibitory action, and is useful for the prophylaxis or treatment of inflammatory disease.
Type:
Application
Filed:
January 31, 2019
Publication date:
May 30, 2019
Applicant:
JAPAN TOBACCO INC.
Inventors:
Teruhiko INOUE, Koji MATSUMURA, Shinichi KIKUCHI
Abstract: The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.
Abstract: The present invention relates to certain novel 2,3-dihydro-1H-indole compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer selected from the group consisting of melanoma, acute myeloid leukemia, chronic lymphocytic leukemia, colorectal cancer, breast cancer, lung cancer, ovarian cancer, fallopian tube carcinoma, primary peritoneal carcinoma, cervical cancer, gastric cancer, liver cancer, pancreatic cancer, thyroid cancer, glioblastoma, non-Hodgkin's lymphoma, and Hodgkin's lymphoma.
Type:
Application
Filed:
May 31, 2017
Publication date:
May 30, 2019
Inventors:
Jolie Anne BASTIAN, Jiehao CHEN, Jeffrey Daniel COHEN, James Robert HENRY, William Thomas MCMILLEN, Bradley Earl REAMAN, Almudena RUBIO, Daniel Jon SALL, Gaiying ZHAO
Abstract: The present invention refers to a method for controlling undesired vegetation at a plant cultivation site, the method comprising the steps of providing, at said site, a plant that comprises at least one nucleic acid comprising a nucleotide sequence encoding protoporphyrinogen oxidase (PPO) which is resistant or tolerant to a PPO-inhibiting herbicide by applying to said site an effective amount of said herbicide. The invention further refers to plants comprising wild-type or mutated PPO enzymes, and methods of obtaining such plants.
Type:
Application
Filed:
July 26, 2017
Publication date:
May 30, 2019
Inventors:
Raphael Aponte, Stefan Tresch, Liliana Parra Rapado, Tobias Seiser, Jill Marie Paulik, Matthias Witschel
Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.
Type:
Application
Filed:
August 7, 2017
Publication date:
May 30, 2019
Applicant:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Inventors:
Sebastien Andre CAMPOS, Samuel Edward DALTON, Vipulkumar Kantibhai PATEL
Abstract: This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.
Type:
Application
Filed:
September 27, 2018
Publication date:
May 30, 2019
Inventors:
Doris Riether, Florian Paul Christian Binder, Henri Doods, Stephan Georg Mueller, Janet Rachel Nicholson, Achim Sauer
Abstract: Compounds, compositions, and methods for the treatment of infections, inflammation, cancers, tinnitus, Meniere's disease, hearing loss, or bipolar disorder, or for providing cytoprotection against Clostridium difficile toxins, are disclosed.
Type:
Application
Filed:
June 21, 2017
Publication date:
May 30, 2019
Applicant:
The University of Toledo
Inventors:
Steven Sucheck, Sandeep Thanna, Donald Ronning, Alexander Landgraf
Abstract: The invention provides methods for modulating the activity of farnesoid X receptors (FXRs) using specific doses of tropifexor, in particular for treating or preventing liver diseases.
Type:
Application
Filed:
November 28, 2018
Publication date:
May 30, 2019
Inventors:
Michael Badman, Clifford Brass, Bryan Laffitte
Abstract: Forms of 4-(6-(3,5-dimethylisoxazol-4-yl)-1-[(1S)-1-(2-pyridyl)ethyl]pyrrolo[3,2-b]pyridin-3-yl)benzoic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the forms of Compound I.
Type:
Application
Filed:
October 11, 2018
Publication date:
May 30, 2019
Inventors:
Prabha N. Ibrahim, Hamid Rezaei, Marika Nespi, Ben Powell, Rashmin Patel
Abstract: The present invention provides an organic compound represented by Chemical Formula 1 below: In Chemical Formula 1, R1 to R9 are each, independently, any one selected from the group consisting of hydrogen, a halogen, a nitro group, a substituted or unsubstituted C1-C6 alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group, a substituted or unsubstituted C6-C40 aryl group, and a substituted or unsubstituted C5-C40 heteroaryl group; L represents a single bond and is any one selected from the group consisting of an alkylene group, a cycloalkylene group, a heterocycloalkylene group, an arylene group, and a heteroarylene group; and Ar1 and Ar2 are each, independently, any one selected from the group consisting of hydrogen, a substituted or unsubstituted C3-C6 cycloalkyl group, a substituted or unsubstituted C3-C6 heterocycloalkyl group, a substituted or unsubstituted C6-C40 aryl group, and a substituted or unsubstituted C2-C40 heteroaryl group.
Type:
Application
Filed:
November 22, 2018
Publication date:
May 30, 2019
Inventors:
Jong Jin HA, Hyun Young YOO, Sung Soo KIM, Seok Jong LEE
Abstract: A chiral heterocyclic compound with hedgehog pathway antagonist activity, method and use thereof are provided. The chiral heterocyclic compound with hedgehog pathway antagonist activity has the structure represented by formula I. A pharmaceutical composition and combined application composition are also provided. Novel molecules of formula II that inhibit hedgehog pathway signaling and therapeutic applications for the treatment of malignancies, prevention of tumor regrowth, sensitization of radio-chemo therapies, and other diseases related to hedgehog signaling are also provided.
Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N oxides, and salts thereof, wherein A, X1, X2, X3 and R2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
Type:
Application
Filed:
July 10, 2017
Publication date:
May 30, 2019
Inventors:
Wenming Zhang, Moumita Kar, Kasinath Sana
Abstract: The present invention relates to 4-aminopyrazolo[3,4-d]pyrimidinylazabicyclo derivatives and pharmaceutical compositions containing the same, wherein the 4-aminopyrazolo[3,4-d]pyrimidinylazabicyclo derivatives and pharmaceutical compositions containing them not only have BTK inhibitory activity but also has remarkably high selectivity for the inhibitory activity of BTK vs. ITK, and thereby can be usefully used for the prevention or treatment of autoimmune diseases or cancers as BTK inhibitors.
Type:
Application
Filed:
July 7, 2017
Publication date:
May 30, 2019
Applicant:
Daewoong Pharmaceutical Co., Ltd.
Inventors:
Youn-Jung YOON, Jung-Eun PARK, Yeon-Jung PARK, Min-June SHIM, Keuk-Chan BANG, Joon-Seok PARK
Abstract: Provided are certain compounds or pharmaceutically acceptable salts thereof which can inhibit kinase activity of Bruton's tyrosine kinase (BTK) and may be useful for the treatment of diseases like cancer, immunological disease and inflammation.
Abstract: The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERR?) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.
Type:
Application
Filed:
September 13, 2016
Publication date:
May 30, 2019
Inventors:
Sung Yeoun HWANG, Sung Jin CHO, Jina KIM, Jungwook CHIN, Hayoung HWANG, In-Kyu LEE, Yong-Hyun JEON, Jaetae LEE, Jae-Han JEON, Sang Wook KIM
Abstract: The present invention in various aspects relates to the synthesis of pyrrole-linked bivalent compounds, including but not limited to norBNI, as well as pharmaceutical compositions comprising the same.
Abstract: In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.
Type:
Application
Filed:
January 30, 2019
Publication date:
May 30, 2019
Inventors:
Robert CHAPMAN, Lonn S. RIDER, Qi HONG, Donald KYLE, Robert KUPPER
Abstract: The present invention concerns harringtonines salts never described in the crystalline state exhibiting a protonated nitrogen seen in solid state analysis and having general formula 1, comprising solvates, made by reacting a cephalotaxine ester alkaloid base having formula 2, in which R1 is, but not limited to, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, and R2 is, independently, but not limited to H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, with an acid having general formula AH in a non-aqueous crystallization solvent, wherein said salt has a large water solubility. The invention also relates to a process for preparing and purifying these salts and their use as chemostherapeutic drugs, alone or combined with radiotherapy, or as immunomodulating agents.
Abstract: The present invention discloses a composition comprising at least one or more stereoisomers of a compound represented by the following Formula (1), wherein, in a gas chromatogram obtained by analyzing the composition by gas chromatography, the ratio of the area of the maximum peak with respect to the total area of peaks derived from the stereoisomers is 60% or more; and wherein the maximum peak is present within the range of retention time of from 27.6 to 28.0 minutes. The present invention also discloses: a curable composition comprising the above described composition, and one selected from the group consisting of a thermal cationic polymerization initiator, an acid anhydride-based curing agent and a curing accelerator, and a photo-cationic polymerization initiator; as well as a cured product therefrom. The above described curable composition is useful in that it allows for the production of a cured product having a high heat resistance.