Patents Issued in May 2, 2019
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Publication number: 20190127368Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonize or partially agonize) NLRP3 and TLR7 and/or TLR8 that are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 and TLR7 and/or TLR8 activities (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 and TLR7 and/or TLR8 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.Type: ApplicationFiled: April 19, 2017Publication date: May 2, 2019Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush
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Publication number: 20190127369Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).Type: ApplicationFiled: August 27, 2018Publication date: May 2, 2019Inventors: Johannes Platzek, Gunnar Garke, Alfons Grunenberg
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Publication number: 20190127370Abstract: Diazanaphthalene compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a diazanaphthalene compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.Type: ApplicationFiled: October 31, 2018Publication date: May 2, 2019Inventors: Sunil Kumar KC, Chi Ching Mak, Jianguo Cao, Venkataiah Bollu, Chandramouli Chiruta, Gopi Kumar Mittapalli, Brian Walter Eastman, Brian Joseph Hofilena
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Publication number: 20190127371Abstract: The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: December 19, 2018Publication date: May 2, 2019Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: PAUL R. FATHEREE, GARY E.L. BRANDT, CAMERON SMITH, STEVEN D.E. SULLIVAN, LORI JEAN VAN ORDEN, MELANIE A. KLEINSCHEK, GLENN D. CRATER
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Publication number: 20190127372Abstract: Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are compounds which contain bioisosteric replacements of the urea group of JTE-013 and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis.Type: ApplicationFiled: December 27, 2018Publication date: May 2, 2019Applicant: DALHOUSIE UNIVERSITYInventors: Christopher McMaster, Gordon Simms
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Publication number: 20190127373Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.Type: ApplicationFiled: January 7, 2019Publication date: May 2, 2019Inventors: Steven W. Andrews, James F. Blake, Mark J. Chicarelli, Adam Golos, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski
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Publication number: 20190127374Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.Type: ApplicationFiled: January 7, 2019Publication date: May 2, 2019Inventors: Steven W. Andrews, James F. Blake, Mark J. Chicarelli, Adam Golos, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski
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Publication number: 20190127375Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.Type: ApplicationFiled: January 10, 2019Publication date: May 2, 2019Inventors: Steven W. Andrews, James F. Blake, Mark J. Chicarelli, Adam Golos, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski
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Publication number: 20190127376Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: October 5, 2018Publication date: May 2, 2019Inventors: Liangxing Wu, Colin Zhang, Chunhong He, Yaping Sun, Liang Lu, Ding-Quan Qian, Meizhong Xu, Jincong Zhuo, Wenqing Yao
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Publication number: 20190127377Abstract: The invention described herein pertains to selective Janus kinase (JAK) inhibitors and methods of use thereof. Also described are methods for treating diseases involved abnormal JAK/STAT signaling pathway in mammals using the described selective JAK inhibitors or a pharmaceutical formulation thereof.Type: ApplicationFiled: October 31, 2018Publication date: May 2, 2019Applicant: Purdue Research FoundationInventors: Mark Stanley Cushman, Mohamed S. A. Elsayed
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Publication number: 20190127378Abstract: Provided are certain novel pyrazine derivatives (I) as SHP2 inhibitors which is shown as formula (I), their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided are fused heterocyclic derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.Type: ApplicationFiled: June 7, 2017Publication date: May 2, 2019Inventors: Cunbo MA, Panliang GAO, Jie CHU, Xinping WU, Chunwei WEN, Di KANG, Jinlong BAI, Xiaoyan PEI
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Publication number: 20190127379Abstract: The present invention relates to a compound suitable for use as a kinase inhibitor according to general formula (I) [compound (C), herein after], or the N-oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or stereoisomer thereof, formula (I) wherein A, R1, R2, R3, R3?, R4, R4?, X, Y, Z, T are as defined in the claims. The invention further relates to an in vitro method of inhibiting protein kinase activity which comprises contacting a protein kinase with a compound of formula (I), or the N-oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or stereoisomer thereof. The invention further relates to the compounds of formula (I) per se, as well as to their use as a medicament, and for use or in a method of treatment of a disease mediated by a protein kinase selected from cancer, inflammatory disorders, cardiovascular diseases, viral induced diseases, circulatory diseases, fibro-proliferative diseases and pain sensitization disorders.Type: ApplicationFiled: May 4, 2017Publication date: May 2, 2019Applicant: B.C.I. PHARMAInventors: Dominique Surleraux, Claire Amiable, Rémi Guillon
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Publication number: 20190127380Abstract: Disclosed are compounds of Formula (I), or a salt thereof, wherein: X is CR4 or N; Y is CR4 or N, provided that Y is N only if X is N; R1 is Formulae (A) or (B); each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, R3, R4, L1, R1a, R1b, R1c, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.Type: ApplicationFiled: April 19, 2017Publication date: May 2, 2019Inventors: Prashantha Gunaga, Jeremy Richter, Navnath Dnyanoba Yadav, Manoranjan Panda, Sreenivasulu Godesi
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Publication number: 20190127381Abstract: Provided herein are novel fused pyrimidinone derivatives of Formula I and synthetic intermediates that are useful in preparing the compounds of formula (I). Further provided herein is a method for preparation of a compound of formula (I) or intermediates, a pharmaceutical composition comprising a compound of formula (I), and use of a compound of formula (I).Type: ApplicationFiled: April 25, 2017Publication date: May 2, 2019Applicant: TORRENT PHARMACEUTICALS LIMITEDInventors: Chaitanya DUTT, Deepa JOSHI, Milind RODE, Sanjay SRIVASTAVA, Davinder TULI, Ramesh Chandra GUPTA, Deepak RAI, Prashant JAMADARKHANA, Shailesh DESHPANDE, Vivek MISHRA, Jaya ABRAHAM
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Publication number: 20190127382Abstract: The invention provides novel compounds having the general formula I: wherein R1, RB1, RB2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.Type: ApplicationFiled: October 30, 2018Publication date: May 2, 2019Applicant: Genentech, Inc.Inventors: Snahel Patel, Gregory Hamilton, Craig Stivala, Huifen Chen, Blake Daniels
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Publication number: 20190127383Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Applicant: Hoffmann-La Roche Inc.Inventors: Luca GOBBI, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer Martin, Matthias Valentin Westphal
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Publication number: 20190127384Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 and n are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Applicant: Hoffmann-La Roche Inc.Inventors: Luca GOBBI, Uwe GRETHER, Wolfgang GUBA, Julian KRETZ, Rainer E. MARTIN, Matthias Valentin WESTPHAL, Adriaan Pieter IJZERMAN
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Publication number: 20190127385Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Applicant: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal, Adriaan Pieter Ijzerman
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Publication number: 20190127386Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Applicant: Hoffmann-La Roche Inc.Inventors: Luca GOBBI, Uwe GRETHER, Wolfgang GUBA, Julian KRETZ, Rainer E. MARTIN, Matthias Valentin WESTPHAL
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Publication number: 20190127387Abstract: The present disclosure provides compounds represented by Formula I-A: A1-L1-B1 I-A and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein A1, B1, and L1 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a condition or disorder responsive to degradation of MDM2 protein such as cancer.Type: ApplicationFiled: April 6, 2017Publication date: May 2, 2019Inventors: Shaomeng Wang, Yangbing Li, Jiuling Yang, Angelo Aguilar, Bing Zhou, Jiantao Hu, Fuming Xu, Rohan Rej, Xin Han
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Publication number: 20190127388Abstract: Processes are provided for the production of methenamine mandelate that do not require the isolation of produced methenamine prior to production of the methenamine mandelate.Type: ApplicationFiled: May 26, 2017Publication date: May 2, 2019Inventors: Bryce Kelly ASSINK, Tino Jon CAVIGGIOLA, III
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Publication number: 20190127389Abstract: The present invention relates to processes useful in the preparation of morphine analogs and derivatives, such as naltrexone, naloxone and nalbuphine and intermediates in the synthesis of said morphine analogs and derivatives. In a particular example, the process begins with for example oxymorphone, oxycodone, 14-hydroxycodeinone or 14-hydroxymorphinone, and includes the formation of an oxazolidine-containing intermediate using catalytic oxidation.Type: ApplicationFiled: April 21, 2017Publication date: May 2, 2019Applicant: Noramco, Inc.Inventors: Christopher Oliver Kappe, Bernhard Gutmann, Ulrich Weigl, Patrick Egli, Douglas Phillip Cox, David Cantillo
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Publication number: 20190127390Abstract: The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.Type: ApplicationFiled: September 17, 2015Publication date: May 2, 2019Applicant: ONCODESIGN S.A.Inventors: Jan Hoflack, Petra Blom, Pascal Benderitter
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Publication number: 20190127391Abstract: This disclosure provides novel imidazopyridazine compounds of formula (I) and pharmaceutical acceptable salt thereof, pharmaceutical compositions containing them, a process for preparing them, and their practical effect in inhibiting PI3K and potential use in treating a disease responsive to inhibition of PI3K, for example, an inflammatory disease, autoimmune disease or cancer.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Inventors: Wei-Guo Su, Guangxiu Dai, Weihan Zhang, Wei Deng
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Publication number: 20190127392Abstract: A quantum device for interfacing Lanthanide ions with optical fields or microwave fields or both. The device includes waveguides or resonators or both for optical fields or microwave fields or for both. The device includes at least one surface to which a single customized Lanthanide molecular complex, or an ensemble, layer, multilayer or crystal of such, are attached or bonded. This places the Lanthanide ions within the optical or microwave fields or both. The ability to customize the molecular structure around each Lanthanide ion, and to control their orientation and position and nano-environment in general, enables minimizing the host lattice effects and non-radiative loss channels for each ion, and increasing their homogeneity. Accordingly, the advantages of the present invention include reduced inhomogeneities, narrower linewidths, extended fluorescence and coherence times, and higher operation temperatures.Type: ApplicationFiled: October 24, 2018Publication date: May 2, 2019Applicant: YEDA RESEARCH AND DEVELOPMENT CO. LTD.Inventors: Barak DAYAN, Abraham SHANZER, Ori Ezrah MOR MARKOVSKY
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Publication number: 20190127393Abstract: Provided herein are lanthanide complexes that exhibit specific subcellular localization to primary cilium. The lanthanide complexes provided herein are useful for imaging, tagging, and pull down of binding targets located in primary cilium.Type: ApplicationFiled: October 31, 2018Publication date: May 2, 2019Inventors: Ka Leung WONG, Hongguang LI, Chi Fai CHAN, Rongfeng LAN
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Publication number: 20190127394Abstract: This invention relates to water-soluble mono-alkoxy and mono-alkyne BODIPY derivatives, including methods for making the same. For examples, provided herein are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: is a BODIPY ligand system; X is a halogen; L is absent or a linker; and Z is selected from the group consisting of: a group reactive with a biologically active molecule and a detectable agent.Type: ApplicationFiled: June 25, 2018Publication date: May 2, 2019Inventors: Ralph Mazitschek, Alexandra M. Courtis, James Adam Hendricks
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Publication number: 20190127395Abstract: The present invention is directed to arginase inhibitor compounds of formula IA or formula IB: or a pharmaceutically acceptable salt thereof, compositions containing these compounds, and methods of their use for the treatment and diagnosis of conditions characterized by upregulation of arginase, abnormally high arginase activity, or by abnormally low nitric oxide synthase activity.Type: ApplicationFiled: September 28, 2018Publication date: May 2, 2019Applicants: AstraZeneca AB, The Trustees of the University of PennsylvaniaInventors: David W. Christianson, Bruce Edward Tomczuk, Richard Scott Pottorf, Andrew Vargha Colasanti, Gary Lee Olson
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Publication number: 20190127396Abstract: Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.Type: ApplicationFiled: October 31, 2018Publication date: May 2, 2019Inventors: Serge Henri Boyer, Scott J. Hecker, Gerardus K.M. Verzijl, Petrus J. Hermsen
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Publication number: 20190127397Abstract: Disclosed herein are borazine complexes and use of the same in perfluoroalkylation reactions.Type: ApplicationFiled: June 23, 2017Publication date: May 2, 2019Inventors: Nathaniel Szymczak, Jacob Geri
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Publication number: 20190127398Abstract: A process for producing organochlorosilanes in a fluidized bed reaction comprises reacting haloorganic reaction gas with a catalytic composition comprising silicon, copper catalysts and promoters, in a fluidized bed reactor, wherein the hydraulic diameter of the fluidized bed reactor dhyd, the superficial gas velocity in the fluidized bed reactor uL and the particle Sauter diameter of the catalytic composition d32 are selected such that, in a Cartesian coordination system in which Ar is plotted against Re, points on the surface are formed wherein the surface is limited by equations 1 and 2 Ar=2·10?5·Re2+0.08*Re?120 ??Equation 1 Ar=2·10?5·Re2?1.07*Re+14100 ??Equation 2 wherein the lower limit Ar=0.5 and the upper limit Ar=3000. The invention also relates to a method for selecting reaction parameters for producing organochlorosilanes.Type: ApplicationFiled: May 12, 2016Publication date: May 2, 2019Applicant: Wacker Chemie AGInventors: Michael MUELLER, Natalia SOFINA
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Publication number: 20190127399Abstract: Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Applicant: HANGZHOU DAC BIOTECH CO., LTD.Inventors: Robert Yongxin ZHAO, Xing LI, Yuangyuang HUANG, Qingliang YANG
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Publication number: 20190127400Abstract: Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Applicant: HANGZHOU DAC BIOTECH CO., LTD.Inventors: Robert Yongxin ZHAO, Xing LI, Yuangyuang HUANG, Qingliang YANG
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Publication number: 20190127401Abstract: Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Applicant: HANGZHOU DAC BIOTECH CO., LTD.Inventors: Robert Yongxin ZHAO, Xing LI, Yuangyuang HUANG, Qingliang YANG
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Publication number: 20190127402Abstract: Described herein is an enzyme-mediated approach to bioconjugation at nanoparticle (NP) surfaces. This process is enabled by a new synthetic linker compatible with the covalent attachment of alkyne modified substrates, including dyes, peptides and nucleic acids. The methods described herein specifically allow for the linkage of molecules to a DNA-functionalized nanoparticle surface. Enzymatic ligation of molecules to the terminal hydroxyl group of DNA using T4 DNA ligase is achieved through incorporation of a single monophosphate on the approaching substrate. In contrast to previous strategies, the linkers disclosed herein are compatible with alkyne modified molecules of a variety of sizes and charges indicating that the ligase minimally requires the monophosphate and the incoming hydroxyl for conjugation to be successful.Type: ApplicationFiled: January 10, 2019Publication date: May 2, 2019Inventor: Jessica Lynn ROUGE
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Publication number: 20190127403Abstract: Provided is a silicon-containing sulfuric acid ester salt comprising a silicon-containing sulfuric acid ester anion represented by formula (1) and a cation selected from cations respectively represented by formulae (2) to (5).Type: ApplicationFiled: March 7, 2017Publication date: May 2, 2019Applicant: Nisshinbo Holdings, Inc.Inventor: Gen Masuda
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Publication number: 20190127404Abstract: The present invention provides a new method for making TH-302 and solid forms thereof. The compound in its solid form is an effective anti-cancer agent and may be used in various pharmaceutical compositions, and are particularly effective for the treatment of cancer. The invention also provides a method for preparing such compounds and forms and for treating cancer in a mammal comprising the step of administering a therapeutically effective amount of a solid form of TH-302 thereof.Type: ApplicationFiled: November 16, 2018Publication date: May 2, 2019Applicant: Molecular Templates, Inc.Inventors: Jian-Xin Duan, Mark Matteucci, Nipun Davar, Denise Andersen
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Publication number: 20190127405Abstract: Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.Type: ApplicationFiled: November 7, 2018Publication date: May 2, 2019Inventors: Christopher Bieniarz, Julia Ashworth-Sharpe, Brian D. Kelly, Nathan Polaske
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Publication number: 20190127406Abstract: Fluorenyl thienopyrimidine luminescent materials are disclosed. These novel compounds have a pyrimidine heterocycles structure, which can be used as emitters in an organic electroluminescent device. Due to the specific structure and groups of the compounds, the novel compounds offer the desired deep red color and better device performance than existing iridium emitters that have thienopyrimidine containing ligands. Also disclosed are an electroluminescent device and a formulation.Type: ApplicationFiled: September 23, 2018Publication date: May 2, 2019Inventor: Chuanjun Xia
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Publication number: 20190127407Abstract: The present invention relates to: a compound as a ligand in a variety of catalytic organic synthetic reactions; a method for producing the compound; a synthetic intermediate of the compound; and a transition metal complex which has the compound as a ligand.Type: ApplicationFiled: March 30, 2017Publication date: May 2, 2019Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventors: Yuji NAKAYAMA, Naota YOKOYAMA
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Publication number: 20190127408Abstract: A process for preparing transition metal carbonates with a mean particle diameter in the range from 6 to 19 ?m (D50), which comprises combining, in a stirred vessel, at least one solution of at least one transition metal salt with at least one solution of at least one alkali metal carbonate or alkali metal hydrogencarbonate to prepare an aqueous suspension of transition metal carbonate, and, in at least one further compartment, continuously introducing a mechanical power in the range from 50 to 10 000 W/l in a proportion of the suspension in each case, based on the proportion of the suspension, and then recycling the proportion into the stirred vessel.Type: ApplicationFiled: December 19, 2018Publication date: May 2, 2019Applicant: BASF SEInventors: Martin SCHULZ-DOBRICK, Simon SCHROEDLE
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Publication number: 20190127409Abstract: The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies.Type: ApplicationFiled: July 31, 2018Publication date: May 2, 2019Inventors: Emil KAKKIS, Steven JUNGLES, He ZHAO
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Publication number: 20190127410Abstract: The present invention provides a mangiferin-6-O-calcium salt and a preparation process thereof. In addition, use of the mangiferin-6-O-calcium salt as defined in claim 1 as an intermediate in the preparation of a mangiferin-6-O-berberine salt is also provided.Type: ApplicationFiled: December 25, 2018Publication date: May 2, 2019Inventors: HOULEI TENG, Wei Wu
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Publication number: 20190127411Abstract: Surfactants based on a newly discovered class of compounds include a hydrophobic lipid oligomer covalently linked to a peptide or peptide-like chain and a carbohydrate moiety, and a serine-leucinol dipeptide linked to the lipid oligomer. Such surfactants can be used to create an oil-in-water or water-in-oil emulsion by mixing together a polar component; a non-polar component; and the surfactant. Biosurfactants of the newly discovered class can be made by isolating and culturing a microorganism which produces the biosurfactant, and then isolating the biosurfactant from the culture. A microorganism can be engineered to produce biosurfactant of this newly discovered class by expressing a set of heterologous genes involved in the biosynthesis of the biosurfactant in the microorganism.Type: ApplicationFiled: April 6, 2017Publication date: May 2, 2019Applicant: Croda International PLCInventors: Russell Greig Kerr, Bradley Arnold Haltli, Douglas Hubert Marchbank, Fabrice Berrué
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Publication number: 20190127412Abstract: Disclosed is a simplified, readily scalable series of individual methods that collectively constitute a method for the synthesis of C2?epiAmB, an efficacious and reduced-toxicity derivative of amphotericin B (AmB), beginning from AmB. Also provided are various compounds corresponding to intermediates in accordance with the series of methods.Type: ApplicationFiled: October 1, 2018Publication date: May 2, 2019Inventors: Martin D. BURKE, Brice E. Uno, Souvik Rakshit
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Publication number: 20190127413Abstract: The subject matter of the instant invention is pertinent to the field of treatment of hormone-dependent conditions. New compounds and methods for treating these conditions are disclosed. Embodiments of the instant invention disclose methods for treating endometriosis, dysmenorrhea, breast cancer, uterine fibroids and endometrial hyperproliferation.Type: ApplicationFiled: May 14, 2018Publication date: May 2, 2019Inventors: Joseph S. Podolski, Ronald D. Wiehle
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Publication number: 20190127414Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3a, R3b, R4, R5a, R5b, R6a, and R6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.Type: ApplicationFiled: December 20, 2018Publication date: May 2, 2019Inventors: Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro
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Publication number: 20190127415Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.Type: ApplicationFiled: November 6, 2018Publication date: May 2, 2019Applicant: Kythera Biopharmaceuticals, Inc.Inventors: Robert M. Moriarty, Nathaniel E. David, Nadir Ahmeduddin Mahmood
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Publication number: 20190127416Abstract: Provided herein are crystalline solid forms of squalamine phosphate designated as Form 1 and Form 2, compositions containing one or both forms, and methods of their preparation and of their use.Type: ApplicationFiled: October 26, 2018Publication date: May 2, 2019Applicant: Enterin, Inc.Inventors: Denise Barbut, Michael Zasloff
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Publication number: 20190127417Abstract: Provided is a crystalline polymorphic form A of 15?-hydroxy-osaterone acetate having an improved stability (storage stability, pulverization stability, and absorption characteristics). In a powder X-ray diffraction spectrum, characteristic diffraction peaks of the crystalline polymorphic form A of 15?-hydroxy-osaterone acetate appear at diffraction angles 2? of 9.6°±0.2°, 17.1°±0.2°, and 20.2°±0.2°. The crystalline polymorphic form A has a melting point of 280 to 283° C. and is a prism crystal.Type: ApplicationFiled: May 10, 2017Publication date: May 2, 2019Applicant: ASKA Pharmaceutical Co., Ltd.Inventors: Takayoshi NAKAGAWA, Hiroyuki HAYASHI, Koichi MIYAZAKI, Shigeki IWASHITA