Patents Issued in September 21, 2017
-
Publication number: 20170267671Abstract: The present invention disclosed a novel EGFR inhibitor compound of formula (I), process for preparation thereof and methods of treating abnormal cell growth in mammals by administering the compounds of formula (I). Wherein, R=—H, 3-CH3, 4-NO2, 4-Cl, 2-CH3, 4-CH3, 4-Br, 4-F R1=—H, -4-OCH3, -4-NO2,-2-NO2, -4-Cl, -2,4,6-CH3, -4-CH3, -2-F,4-Br, -4-CF3, -4-S—CH3, -4-Cl,-3-CF3, -3-S—CH3, -3,5-CF3, -2-S—CH3, -3-CF3,-4-OCF3, —Si—(CH3)3, —Si—(C2H5)3, (CH3)2—Si—C2H5.Type: ApplicationFiled: November 20, 2015Publication date: September 21, 2017Inventors: Pradeep KUMAR, Jignesh Kantilal PARIKH, Eeshwaraiah BEGARI
-
Publication number: 20170267672Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.Type: ApplicationFiled: August 18, 2015Publication date: September 21, 2017Applicant: Syngenta Participations AGInventors: Andre Stoller, Andre Jeanguenat, Andrew Edmunds, Pierre Joseph Marcel Jung, Daniel Emery, Michel Muehlebach, Peter Renold
-
Publication number: 20170267673Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.Type: ApplicationFiled: November 17, 2016Publication date: September 21, 2017Applicant: AMGEN INC.Inventors: Jennifer R. ALLEN, Albert AMEGADZIE, Matthew P. BOURBEAU, James A. BROWN, Jian J. CHEN, Yuan CHENG, Michael J. FROHN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Longbin LIU, Qingyian LIU, Jonathan D. LOW, Vu Van MA, James R. MANNING, Ana Elena MINATTI, Thomas T. NGUYEN, Nobuko NISHIMURA, Mark H. NORMAN, Liping H. PETTUS, Alexander J. PICKRELL, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Aaron C. SIEGMUND, Markian M. STEC, Ryan D. WHITE, Qiufen XUE
-
Publication number: 20170267674Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.Type: ApplicationFiled: March 30, 2017Publication date: September 21, 2017Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
-
Publication number: 20170267675Abstract: The invention provides novel substituted indazole compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.Type: ApplicationFiled: July 30, 2015Publication date: September 21, 2017Applicants: Merck Patent GmbH, Cancer Research Technology Ltd.Inventors: Kai SCHIEMANN, Aurelie MALLINGER
-
Publication number: 20170267676Abstract: The present invention relates to compounds of the formula I or II: (I) (II) processes for their preparation and their use as pharmaceutical agents or compositions in the treatment, of neurological disorders.Type: ApplicationFiled: December 2, 2015Publication date: September 21, 2017Inventors: Penelope Jane Huggins, Jack Gordon Parsons, Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Anthony Vincent Robinson
-
Publication number: 20170267677Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: June 1, 2017Publication date: September 21, 2017Applicant: Dr. Reddy's Laboratories Ltd.Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
-
Publication number: 20170267678Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: ApplicationFiled: June 5, 2017Publication date: September 21, 2017Applicant: Novartis AGInventors: Nigel Graham COOKE, Paulo Fernandes Gomes Dos Santos, Nadege GRAVELEAU, Christina HEBACH, Klemens HOEGENAUER, Gregory John HOLLINGWORTH, Alexander Baxter SMITH, Nicolas SOLDERMANN, Frank STOWASSER, Ross Sinclair STRANG, Nicola TUFILLI, Anette von MATT, Romain WOLF, Frederic ZECRI
-
Publication number: 20170267679Abstract: Tricyclic fused pyrimidine compounds having an arylalkyl amine substituent at the P4 position and a substituted 1H-indol-1-yl, 1H-indol-3-yl, indanyl, indazol-1-yl, indazol-3-yl, benzotriazol-1-yl or 1H-benz[d]imidazol-1-yl group at the P2 position well as optional aliphatic, functional and/or aromatic components substituted at other positions of the tricyclic compounds of the invention. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.Type: ApplicationFiled: March 14, 2017Publication date: September 21, 2017Inventors: Han-Jie Zhou, David Wustrow
-
Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
Publication number: 20170267680Abstract: The present invention relates to compounds having the general formula (Ia) or (Ib), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease, in particular influenza.Type: ApplicationFiled: October 28, 2016Publication date: September 21, 2017Inventors: Hans HILPERT, Lukas KREIS, Christian LERNER, Roland HUMM, Thorsten MUSER, Bernd KUHN -
Publication number: 20170267681Abstract: Disclosed are compounds comprising an azasugar attached to a heterocyclic base, including pharmaceutically acceptable salts thereof, suitable for use in inhibiting viral RNA polymerase activity or viral replication, and treating viral infections. The compounds are characterized, in part, by favorable pharmacokinetics for the active pharmaceutical ingredient, particularly in conjunction with enteral administration, including, in particular, oral administration. Also disclosed are pharmaceutical compositions comprising one or more compounds mentioned above, or pharmaceutically acceptable salts thereof, as well as methods for preparing same. Also provided are methods for inhibiting viral RNA polymerase activity, viral replication, and treating viral infections.Type: ApplicationFiled: March 31, 2017Publication date: September 21, 2017Inventors: Yarlagadda S. Babu, Pravin L. Kotian, Shanta Bantia, Minwan Wu, V. S. Kumar
-
Publication number: 20170267682Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.Type: ApplicationFiled: July 30, 2015Publication date: September 21, 2017Applicant: Janssen Pharmaceutica NVInventors: Susana Conde-Ceide, Michiel Luc, Maria Van Gool, Maria Luz Martin-Martin
-
Publication number: 20170267683Abstract: The present disclosure relates to crystalline forms of 4,5,6,7-tetrahydro-11-methoxy-2-[(4-methyl-1-piperazinyl)methyl]-1H-cyclopenta[a]pyrrolo[3,4-c]carbazole-1,3(2H)-dione, including salts forms and free base forms.Type: ApplicationFiled: November 25, 2015Publication date: September 21, 2017Applicant: CEPHALON, INC.Inventors: Stephen J. BIERLMAIER, Ralph C. HALTIWANGER, Martin J. JACOBS
-
Publication number: 20170267684Abstract: The invention is directed to a triazolopyridazine compound of formula (I), N-oxides, pharmaceutically acceptable salts and solvates thereof, wherein D represents deuterium, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: ApplicationFiled: December 3, 2015Publication date: September 21, 2017Applicant: Janssen Pharmaceutica NVInventors: Patrick Blasius Furer, Ronaldus Arnodus Hendrika Joseph Gilissen, Ioannnis Nicolaos Houpis, Lieven Meerpoel, Timothy Pietro Suren Perera, Philip James Pye
-
Publication number: 20170267685Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas.Type: ApplicationFiled: May 25, 2017Publication date: September 21, 2017Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson, Darren Harvey, Andrew Scholte, Sachin Maniar
-
Publication number: 20170267686Abstract: Methods that may be used for the manufacture of a class of chemical compounds known as morphinans, including neopine, are provided. Compositions useful for the synthesis of morphinans, including neopine, are also provided.Type: ApplicationFiled: August 21, 2015Publication date: September 21, 2017Inventor: Peter James Facchini
-
Publication number: 20170267687Abstract: The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.Type: ApplicationFiled: October 28, 2016Publication date: September 21, 2017Applicant: EURO-CELTIQUE S.A.Inventors: Steve WHITELOCK, Deborah Phyllis HARDING, Carl David TURNER
-
Publication number: 20170267688Abstract: The present invention relates to compounds of the formulas (IA) and (IB) and pharmaceutically acceptable salts thereof, wherein A and R1-R6, 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: ApplicationFiled: December 1, 2015Publication date: September 21, 2017Inventors: Zhidong CHEN, Derek COGAN, Xin GUO, Daniel Richard MARSHALL, Kenneth Michael MEYERS, Yunlong ZHANG
-
Publication number: 20170267689Abstract: Stimuli-switchable moieties, monomers incorporating stimuli-switchable moieties, and polymers incorporating such stimuli-switchable moieties are provided. The stimuli-switchable moiety can be a pyrano aryl chromenone-derivative. The stimuli-switchable monomer can be a lactone monomer. The stimuli-switchable monomer can be an amino acid, which can be incorporated into a specific peptide sequence by peptide synthesis.Type: ApplicationFiled: August 25, 2015Publication date: September 21, 2017Inventors: Carlo David MONTEMAGNO, Sinoj ABRAHAM, Surjith Kumar KUMARAN
-
Publication number: 20170267690Abstract: The present invention provides solid forms of compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, methods of producing the same, and methods of using the same in the treatment of ACC-mediated diseases.Type: ApplicationFiled: March 1, 2017Publication date: September 21, 2017Inventors: Katy Alexander, John C. Amedio, JR., Selcuk Calimsiz, Michael Geier, Geraldine C. Harriman, Sijun Hu, Jon P. Lawson, Henry Morrison, Kyle Sabourin, Mark E. Scott, Vimal Varghese, Kunal Arvind Varia, Xiaotin Wang, Xiaowei Yang
-
Publication number: 20170267691Abstract: The present invention provides thieno[2,3-c]pyrrol-4-one compounds that inhibit activity of extracellular-signal-regulated kinase (ERK) and may be useful in the treatment of cancer.Type: ApplicationFiled: December 15, 2015Publication date: September 21, 2017Inventors: Guillermo S. Cortez, Sajan Joseph, Johnathan Alexander McLean, William Thomas McMillen, Michael John Rodriguez, Gaiying Zhao
-
Publication number: 20170267692Abstract: The present invention relates to methods and compositions for inhibiting the activity of skin proteases, especially human kallikrein 7 (KLK7), human kallikrein 5 (KLK5), and human kallikrein 14 (KLK14). More specifically, the invention relates to the use of substituted 3,1-benzoxazin-4-ones being selective inhibitors of human skin kallikreins for the treatment of skin diseases, more specifically for the treatment of inflammatory skins diseases, especially Netherton syndrome.Type: ApplicationFiled: June 5, 2017Publication date: September 21, 2017Inventors: Fredrik WAGBERG, Goran LEONARDSSON
-
Publication number: 20170267693Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: May 18, 2017Publication date: September 21, 2017Applicants: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
-
Publication number: 20170267694Abstract: Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.Type: ApplicationFiled: December 21, 2016Publication date: September 21, 2017Inventors: Dustin Bringley, Johann Chan, Peter Fung, Katie Keaton, Olga Lapina, Henry Morrison, Dominika Pcion
-
Publication number: 20170267695Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).Type: ApplicationFiled: December 10, 2015Publication date: September 21, 2017Applicants: Merck Sharp & Dohme Corp., MSD R&D (China) Co., Ltd.Inventors: Phieng Siliphaivanh, David L. Sloman, David Witter, Umar Faruk Mansoor, Joseph Kozlowski, Ziping Liu, Jianmin Fu, Zhilong Wan, Wei Liu, Yimin Qian, Xianhai Huang
-
Publication number: 20170267696Abstract: Provided are compound of formula (I) as certain CDK4/6 inhibitors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: May 27, 2015Publication date: September 21, 2017Inventors: Weibo Wang, Xingdong Zhao, Tongshuang LI, Qiang TIAN, Huajie ZHANG, Haohan TAN, Xianlong WANG, Qihong LIU, Zhifu LI, Weipeng ZHANG, Zhifang CHEN, Lihua JIANG, Yanxin LIU, Li LINGHU, Min LIN, Jing SUN
-
Publication number: 20170267697Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: November 29, 2016Publication date: September 21, 2017Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
-
Publication number: 20170267698Abstract: The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.Type: ApplicationFiled: June 2, 2017Publication date: September 21, 2017Inventors: Paul Stephen DONNELLY, Michelle Therese Ma, Denis Bernard Scanlon
-
Publication number: 20170267699Abstract: The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.Type: ApplicationFiled: June 2, 2017Publication date: September 21, 2017Inventors: Paul Stephen DONNELLY, Michelle Therese MA, Denis Bernard SCANLON
-
Publication number: 20170267700Abstract: Precursors are prepared and employed in electron beam induced decomposition (EBID). The EBID precursors are complexes of the formula: X-M-Y, where M is Au or Ag; X is F, Cl, Br, I, CN, OR1, O2CR2, or R3; Y is P(OR)3, NR3, unsubstituted or substituted pyrrole, unsubstituted or substituted pyridine, unsubstituted or substituted pyrrolidine, or unsubstituted or substituted piperidine; and where R, R1, R2, R3, and substituents of the substituted pyrrole, pyridine, pyrrolidine, or piperidine are independently H, C1-C8 alkyl, C6-C10 aryl, C1-C8 perfluoroalkyl, C1-C8 partially fluorinated alkyl, and SiR5R6R7 where R5, R6, and R7 are independently H, C1-C8 alkyl, or C1-C8 fluorinated alkyl. The decomposition of the EBID precursor results in the formation of one or more gold, silver, or any combination thereof features on a substrate.Type: ApplicationFiled: August 26, 2015Publication date: September 21, 2017Inventors: Lisa McElwee-White, Jakub Pedziwiatr, D. Howard Fairbrother
-
Publication number: 20170267701Abstract: An object of the present invention is to provide a method for producing tetraalkoxysilane while saving energy at a high yield. Tetraalkoxysilane can be produced while saving energy at a high yield by the method including a first step of reacting alcohol with carbon dioxide in the presence of a dehydrating agent and/or in a reactor provided with a dehydrating means, and a second step of reacting a reaction mixture obtained in the first step with silicon oxide.Type: ApplicationFiled: April 30, 2015Publication date: September 21, 2017Applicant: NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGYInventors: Norihisa Fukaya, Seong-Jib Choi, Jun-Chul Choi, Toshio Horikoshi, Kazuhiko Sato, Hiroyuki Yasuda
-
Publication number: 20170267702Abstract: Disclosed is a method for making alkylhalosilanes from an alkyl halide and silicon in the presence of the catalyst package comprising metallic aluminum dispersed throughout a copper catalyst. Also disclosed in some embodiments is a catalyst package comprising metallic aluminum dispersed throughout a copper catalyst. In some embodiments the catalyst package comprises a copper catalyst comprised of a metallic copper/cuprous oxide/cupric oxide granular particulate catalyst and a copper-aluminum alloy.Type: ApplicationFiled: July 18, 2015Publication date: September 21, 2017Applicant: SCM Metal Products, Inc.Inventor: Mark Kromer BARR
-
Publication number: 20170267703Abstract: A polyorganosiloxane resin represented by the following general formula (5): (R3SiO1/2)l?(R2SiO2/2)m?(RSiO3/2)n?(SiO4/2)o? (5) wherein R is, independently of each other, a hydrogen atom or a monovalent hydrocarbon group having 1 to 18 carbon atoms, and optionally having an oxygen, halogen, nitrogen or sulfur atom; l?, m? and o? are, independently of each other, an integer of from 0 to 10,000; n? is an integer of from 1 to 10,000; a total of l?, m? and n? is from 2 to 30,000; and at least one R is a hydrogen atom and at least one R is an —OX group in the molecule, wherein X is an alkyl group having 1 to 10 carbon atoms or an alkoxyalkyl group having 2 to 10 carbon atoms; and at least one hydrogen atom and at least one —OX group bond to one and the same silicon atom.Type: ApplicationFiled: May 12, 2017Publication date: September 21, 2017Applicant: SHIN-ETSU CHEMICAL CO., LTD.Inventors: Takayuki KUSUNOKI, Tsutomu KASHIWAGI
-
Publication number: 20170267704Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting STAT3 and/or STAT5 activity or for the treatment of a STAT3 or STAT5-dependent cancer using said compounds; or a pharmaceutically acceptable salt, solvate or prodrug thereof.Type: ApplicationFiled: March 30, 2017Publication date: September 21, 2017Applicants: The Governing Council of the University of Toronto, UTI Limited Partnership, Indiana University Research and Technology CorporationInventors: Patrick Thomas Gunning, Sina Haftchenary, Brent David George Page, Samuel Weiss, Hema Artee Luchman, Melissa L. Fishel
-
Publication number: 20170267705Abstract: The invention provides compounds of the formula: R1 is OR11, or NR5R5?; R2 is H or F; R5 is H, OH, C1-C6 alkyl, OH, C(?O)R6, O(C?O)R6 or O(C?O)OR6; R5? is H or C1-C6 alkyl; R6 is C1-C6 alkyl or C3-C7 cycloalkyl; R13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R22; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.Type: ApplicationFiled: August 24, 2015Publication date: September 21, 2017Inventors: Richard BETHEL, Anders ENEROTH, Bjorn KLASSON, Fredrik OBERG
-
Publication number: 20170267706Abstract: A method for the synthesis of a heterocyclic hydrogen phosphine oxide, having the general formula: wherein: R is a aliphatic or aromatic divalent group optionally including one or more heteroatoms and optionally having one or more substituents and X and Y are independently selected from —O—, —C(O)O— and —NR?— wherein R? is a monovalent group optionally having one or more heteroatoms including the steps of: a) forming a reaction mixture by mixing a compound having the general formula HX—R—YH and tetraphosphorus hexaoxide; and b) recovering the resulting compound comprising the heterocyclic hydrogen phosphine oxide.Type: ApplicationFiled: August 18, 2015Publication date: September 21, 2017Applicant: STRAITMARK HOLDING AGInventors: Frederic BRUYNEEL, Patrick Pierre NOTTE
-
Publication number: 20170267707Abstract: Provided herein are ?-aminophosphonates and methods for making same. Also provided are N-heterocyclic phosphines (NHPs) useful in metal-free phosphorus-carbon bond forming reactions such as, for example, in the preparation of ?-aminophosphonates. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: February 17, 2017Publication date: September 21, 2017Inventors: Jun Yong Kang, Karimulla Mulla
-
Publication number: 20170267708Abstract: A useful novel compound that shows superior antibacterial activity also against erythromycin resistant bacteria, for example, resistant pneumococci, streptococci, mycoplasmas, and the like, against which sufficient antibacterial activity cannot be obtained with conventional macrolide antibiotics, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof.Type: ApplicationFiled: August 17, 2015Publication date: September 21, 2017Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Tomohiro SUGIMOTO, Masato HAYASHI, Takanori KAWAGUCHI
-
Publication number: 20170267709Abstract: The present disclosure provides nicotinate/nicotinamide riboside compounds or derivatives of formula (I): wherein X?, Z1, Z2, n, R1, R2, R3, R4, R5, R6, R7, and R8 are described herein, reduced analogs thereof, and synthetic processes for the preparation thereof.Type: ApplicationFiled: March 16, 2017Publication date: September 21, 2017Applicants: ChromaDex Inc., The Queen's University of BelfastInventors: Marie Eugenie Migaud, Philip Redpath, Kerri Crossey, Richard Cunningham, Ryan Dellinger, Troy Rhonemus, Sylesh Venkataraman, Brian Nettles
-
Publication number: 20170267710Abstract: Compounds that modulate the conversion of AMP to adenosine by 5?-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5?-nucleotidase, ecto is also provided.Type: ApplicationFiled: January 6, 2017Publication date: September 21, 2017Inventors: Laurent Pierre Paul DEBIEN, Juan Carlos JAEN, Jaroslaw KALISIAK, Kenneth V. LAWSON, Manmohan Reddy LELETI, Erick Allen LINDSEY, Dillon Harding MILES, Eric NEWCOMB, Jay Patrick POWERS, Brandon Reid Rosen, Ehesan Ul Sharif
-
Publication number: 20170267711Abstract: Compounds and methods of synthesizing oxysterols are provided. The compounds and methods provided allow the oxysterol to be safely produced at a high yield. The compounds and methods provided can produce the oxysterol in a stereoselective manner.Type: ApplicationFiled: May 19, 2017Publication date: September 21, 2017Inventors: Roger E. Harrington, Jerbrena C. Jacobs, Damodaragounder Gopal, Ke-Qing Ling, Marco Burello
-
Publication number: 20170267712Abstract: Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor ? (ROR?) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR? results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).Type: ApplicationFiled: May 11, 2017Publication date: September 21, 2017Inventors: Scott McNear Thacher, Xiaolin Li, Robert Babine, Bruno Tse
-
Publication number: 20170267713Abstract: Pyridyl analogs of 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole and pharmaceutical compositions containing the same are provided. The present invention is a tnterpenoid compound of Formula I, or a hydrate, isomer, prodrug or pharmaceutically acceptable salt thereof: wherein one or more of R, R or R is independently a substituted or unsubstituted aryl group, heteroaryl group, cycloalkyl group or heterocyclyl group, and the remaining R groups are hydrogen. The pyridyl analogs of CD-DO-Im 1 have been developed, which are more stable in human plasma and achieve a higher concentration in target tissues such as liver, pancreas, kidney and lungs.Type: ApplicationFiled: August 26, 2015Publication date: September 21, 2017Inventors: Gordon W. Gribble, Michael B. Sporn, Karen T. Liby, Evans O. Onyango, Martine Cao
-
Publication number: 20170267714Abstract: This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, spleenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention is an anti-adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins. It inhibits excess adhesion and inhibits cell attachment. It modulates angiogenesis. The compounds also use as mediator of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases.Type: ApplicationFiled: June 2, 2017Publication date: September 21, 2017Inventors: Pui-Kwong CHAN, May Sung MAK
-
Publication number: 20170267715Abstract: This invention is in the field of micro-organism and algal cell processing. The invention relates to a method of maximizing migration of micro-organism and/or algal cells to a solvent fraction while simultaneously displacing water in a separate fraction and subsequent extraction of hydrophobic products from the organisms. The invention further relates to a method of sequestration of protein from an aqueous phase to an organic solvent.Type: ApplicationFiled: March 13, 2017Publication date: September 21, 2017Inventors: Sandun D. Fernando, Varun M. Gejji
-
Publication number: 20170267716Abstract: Provided herein are aptamer-polymer conjugates which are responsive to environmental stimuli and are useful in selective purification of untagged target polypeptides.Type: ApplicationFiled: March 16, 2016Publication date: September 21, 2017Inventors: Anthony John Murray, Andrew David Pris, Erik Leeming Kvam, Nandini Nagraj, Eugene Pauling Boden, Ernest William Kovacs, Louisa Ruth Carr, Rui Chen, Tiberiu Mircea Siclovan, Kelly Scott Chichak
-
Publication number: 20170267717Abstract: Novel efficient, time-saving and reliable radiofluorination procedures for the production of 18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with 18F? are described. The active ester including [18F]F-Py-TFP and [18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.Type: ApplicationFiled: August 24, 2015Publication date: September 21, 2017Applicant: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.Inventors: Bernd NEUMAIER, Boris ZLATOPOLSKIY, Raphael RICHARZ, Phillip KRAPF
-
Publication number: 20170267718Abstract: Provided are a tripeptide compound, a preparation method therefor, and an application thereof. The structure of the related compound is represented by formula (I). The provided compound has angiotensin converting enzyme inhibiting bioactivity, and the compound and a pharmaceutical composition thereof play a role in preventing and treating hypertension and other cardiocerebral vascular system diseases.Type: ApplicationFiled: November 27, 2015Publication date: September 21, 2017Inventors: Xiaohui ZHENG, Yajun BAI, Fanggang QIN, Pei LIU, Jiacheng FANG, Xirui HE, Xiaoxiao WANG
-
Publication number: 20170267719Abstract: The present invention discloses a Plectin-1 receptor targeting novel cationic KTLLPTPK-lipopeptide. The present invention further discloses a liposomal formulation comprising the cationic KTLLPTPK-lipopeptide, at least two co-lipids, therapeutic agents and a pharmaceutically acceptable carrier. The present invention also provides a method for regressing established pancreatic tumors comprising administering therapeutically effective amount of the liposomal formulation with the therapeutic agents in combination with targeted genetic immunization (DNA vaccination) i.e. by immunizing mice with electrostatic complexes (direct in-vivo DC-targeting cationic liposomes) of DNA vaccines encoding mesothelin (p-CMV-MSLN).Type: ApplicationFiled: March 16, 2017Publication date: September 21, 2017Inventors: Vijay Sagar Madamsetty, Arabinda Chaudhuri, Debabrata Mukhopadhyay
-
Publication number: 20170267720Abstract: The present invention relates to an opioid peptide represented by general formula TyrGlyGly-X1-X2-X3-X4, wherein: X1 is represented by Thr or Glu; X1 is represented by Gly or Thr or Ala; X3 is represented by Ala or Val or Gly or Glu; and X4 is represented by His or Gln or Thr or SEQ ID NO:1, or HisTyr or GlnTyr or ThrTyr. The invention also relates to pharmaceutical and food compositions comprising the peptide and to the use of the same for analgesic purposes, and/or for providing a feeling of satiety to a subject.Type: ApplicationFiled: August 17, 2015Publication date: September 21, 2017Applicants: Embrapa - Empresa Brasileira de Pesquisa Agropecuá ria, Fundação Universidade de Brasília (FUB)Inventors: Carlos BLOCH JUNIOR, Felipe VINECKY, Karla Graziella MOREIRA, Márcia Renata MORTARI
