Patents Issued in April 20, 2017
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Publication number: 20170107178Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X1, X2, X3, X4, and X5 may be the same or different and each is independently selected from C, N and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom are maintained; each R1, R2, R3, R4, R5, and R7 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X1, X2, X3, X4, and X5 are maintained; one or two R6 groups may be present and are selected from H and a substituted or unsubstituted organic group, provided that the number of R6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R6 is an organic group comprising an atomType: ApplicationFiled: March 19, 2015Publication date: April 20, 2017Applicant: IOMET PHARMA LTD.Inventors: Phillip M. COWLEY, Alan WISE, Michael KICZUN, Susan DAVIS
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Publication number: 20170107179Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.Type: ApplicationFiled: May 25, 2016Publication date: April 20, 2017Inventors: Xiao-Yi Xiao, Roger B. Clark, Diana Katharine Hunt, Magnus P. Ronn, Louis Plamondon, Minsheng He, Joyce A. Sutcliffe, Trudy Grossman
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Publication number: 20170107180Abstract: The invention provides compounds for inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: December 19, 2016Publication date: April 20, 2017Inventors: Ernest J. MCEACHERN, David J. VOCADLO, Yuanxi ZHOU, Harold G. SELNICK
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Publication number: 20170107181Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the claims. The invention further provides compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: ApplicationFiled: March 31, 2015Publication date: April 20, 2017Applicant: Syngenta Participations AGInventors: Thomas James HOFFMAN, Sarah SULZER-MOSSE, Kurt NEBEL, Fredrik Emil Malcolm CEDERBAUM
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Publication number: 20170107182Abstract: Process for preparing 3,5-bis(haloalkyl)pyrazole derivatives of the formula (I), via acylation of Hydrazones.Type: ApplicationFiled: June 8, 2015Publication date: April 20, 2017Applicant: Bayer CropScience AktiengesellschaftInventors: Sergii PAZENOK, Norbert LUI
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Publication number: 20170107183Abstract: 2-(Hetero)arylpyradazinones of the general formula (I) are described as herbicides. In this formula (I), R1, R2, R3, R4 and R5 are each radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. X1, X2 and X3 represent nitrogen or an optionally substituted carbon atom.Type: ApplicationFiled: May 19, 2015Publication date: April 20, 2017Inventors: Hartmut AHRENS, Jörg TIEBES, Christian WALDRAFF, Hansjörg DIETRICH, Dirk SCHMUTZLER, Elmar GATZWEILER, Christopher ROSINGER
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Publication number: 20170107184Abstract: The present invention relates to compounds of the formula I and their use as fungicides, wherein the variables are defined as described in the claims and the specification.Type: ApplicationFiled: March 16, 2015Publication date: April 20, 2017Inventors: Wassilios GRAMMENOS, Nadege BOUDET, Bernd MUELLER, Maria Angelica QUINTERO PALOMAR, Ana ESCRIBANO CUESTA, Erica May Wilson LAUTERWASSER, Jan Klaas LOHMANN, Thomas GROTE, Manuel KRETSCHMER, Ian Robert CRAIG
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Publication number: 20170107185Abstract: The present invention relates to compounds of the formula I wherein the variables are defined in the claims and the specification, and to the preparation and uses of compounds I.Type: ApplicationFiled: May 28, 2015Publication date: April 20, 2017Inventors: Wassilios GRAMMNEOS, Nadege BOUDET, Bernd MUELLER, Maria Angelica QUINTERO PALOMAR, Ana ESCRIBANO CUESTA, Erica May Wilson LAUTERWASSER, Jan Klaas LOHMANN, Thomas GROTE, Manuel KRETSCHMER, Ian Robert CRAIG
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Publication number: 20170107186Abstract: The isocyanurate composition consists essentially of an isocyanurate derivative of 1,3-xylylenediisocyanate, and has a viscosity at 100° C. of 600 mPa·s or more and 20000 mPa·s or less.Type: ApplicationFiled: March 3, 2015Publication date: April 20, 2017Inventors: Kazuyuki FUKUDA, Hideaki OTSUKA, Tsutomu YOSHIDA, Tatsuya NAKASHIMA, Toshiaki MORIYA, Shirou HONMA
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Publication number: 20170107187Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.Type: ApplicationFiled: December 28, 2016Publication date: April 20, 2017Inventors: Stacy BREMNER, Jerry EVARTS, Keiko SUJINO, Duong TRAN, Dragos VIZITIU
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Publication number: 20170107188Abstract: To provide a novel technique capable of further reducing the argon purge amount in a process for producing ethylene oxide.Type: ApplicationFiled: March 31, 2015Publication date: April 20, 2017Inventors: Yukimasa KAWAGUCHI, Hideto SUZUKI
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Publication number: 20170107189Abstract: The present invention relates to a compound having the following structure: where R, R1, and m are as defined herein. The compound is useful as a precursor to a surfactant with a low hydrophilic-lipophylic balance (HLB), which can be used to increase open time for coatings.Type: ApplicationFiled: October 13, 2016Publication date: April 20, 2017Inventors: David J. Brennan, Gregoire Cardoen, Robert E. Hefner, JR., Antony K. Van Dyk
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Publication number: 20170107190Abstract: A compound, or a pharmaceutically acceptable salt thereof, having a structure of wherein Z is aryl or substituted aryl, heteroaryl, or substituted heteroaryl; X is —S—, —S(O)—, or S(O)2—; R20 and R21 are each independently H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, or halogenated alkyl; one of R22, R23, and R24 is —O— and the others of R22, R23 and R24 are independently —CH2—, or —C(R13)— wherein R13 is alkyl, alkenyl, alkynyl, trialkylsilyl group, or —(CH2)mOR15, wherein R15 is alkyl or an aryl and m is an integer in the range of 1 to 10; and R25 is H, alkyl, substituted alkyl, halogen, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, C1-C3 alkoxy, aryloxy, or —(CH2)qOR17, wherein R17 is alkyl an aryl and q is an integer in the range of 1 to 10.Type: ApplicationFiled: October 13, 2016Publication date: April 20, 2017Applicants: University of Pittsburgh - Of the Commonwealth System of Higher Education, Medical University of South CarolinaInventors: Peter Wipf, Carol A. Feghali-Bostwick
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Publication number: 20170107191Abstract: A bioderived based plasticizer is produced by reacting a bioderived diol (and/or a bioderived alcohol) and a bioderived carboxylic acid in the presence of N,N?-dicyclohexylcarbodiimide (DCC), wherein the bioderived carboxylic acid includes a hydrolyzed oil. The bioderived carboxylic acid (e.g., linoleic acid, ?-linolenic acid, oleic acid, and mixtures thereof) may be produced by hydrolyzing a triglyceride, such as canola oil, linseed oil, soybean oil, and mixtures thereof. In one embodiment of the present invention, a bioderived based plasticizer is produced by reacting 2,5-bis-(hydroxymethyl)furan and ?-linolenic acid in the presence of DCC. In some embodiments of the present invention, the bioderived based plasticizer is blended into one or more polymers.Type: ApplicationFiled: January 2, 2017Publication date: April 20, 2017Inventors: Dylan J. Boday, Joseph Kuczynski, Jason T. Wertz, Jing Zhang
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Publication number: 20170107192Abstract: The present invention provides cyclic dimers of alpha acids and polymers derived therefrom. Also provided are processes for preparing and methods of using the cyclic dimers and the polymers derived from the cyclic dimers.Type: ApplicationFiled: December 29, 2016Publication date: April 20, 2017Inventors: Graciela B. Arhancet, Matthew Mahoney, Xiaojun Wang
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Publication number: 20170107193Abstract: The present invention relates to process for the preparation of highly pure Lenalidomide (I). The invention also relates to crystalline Form-SL obtained by the process of the present invention., the said Form-SL being substantially pure and characterized by X-ray powder diffraction pattern comprising of at least seven peaks selected from 7.061, 12.860, 16.531, 18.698, 27.925, 33.212, 34.187, 35.253, 35.921 and 38.765±0.1°2?; a single un-split °2? peak at 7.813±-.1°2?; and a three-way split °2? peak at 20.467±0.1°2?. The invention further relates to pharmaceutical compositions comprising crystalline Form-SL of Lenalidomide, which may be useful for the treatment of cancer.Type: ApplicationFiled: August 1, 2014Publication date: April 20, 2017Applicant: SHILPA MEDICARE LIMITEDInventors: SRIRAM RAMPALLI, LAVKUMAR UPALLA, PRASHANT PUROHIT, AKSHAYKANT CHATURVEDI
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Publication number: 20170107194Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.Type: ApplicationFiled: December 28, 2016Publication date: April 20, 2017Inventors: Zenon D. Konteatis, Janeta Popovici-Muller, Jeremy M. Travins, Robert Zahler, Zhenwei Cai, Ding Zhou
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Publication number: 20170107195Abstract: The present invention provides a compound of a formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an ENaC mediated disease state (such as asthma, CF or COPD).Type: ApplicationFiled: March 17, 2015Publication date: April 20, 2017Applicant: AstraZeneca ABInventors: Susanne Elisabeth BERGLUND, Stephen CONNOLLY, Martin HEMMERLING, Nafizal HOSSAIN, Anna KRISTOFFERSSON, Johan Rune Michael LUNDKVIST, Grigorios NIKITIDIS, Lena Elisabeth RIPA, Igor SHAMOVSKY
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Publication number: 20170107196Abstract: A tetrazolinone compound represented by formula (1): wherein R1 and R2 each independently represents a hydrogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; R3 represents a hydrogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; R4 represents a halogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; h represents any one of integers of 0 to 4; X represents a nitrogen atom or CR5; and R5 represents a hydrogen atom, a halogen atom, etc.; has excellent control activity against pests.Type: ApplicationFiled: March 26, 2015Publication date: April 20, 2017Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Koichiro DOTA
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Publication number: 20170107197Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.Type: ApplicationFiled: May 23, 2016Publication date: April 20, 2017Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
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Publication number: 20170107198Abstract: Multifunctional nitroxide derivatives contain a potassium channel opener and a reactive oxygen species (ROS) degradation catalyst that can act as an anti-oxidant. Pharmaceutical compositions can include the derivatives. The multifunctional compounds and pharmaceutical compositions are useful for treatment of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction.Type: ApplicationFiled: December 19, 2016Publication date: April 20, 2017Inventors: Prakash Jagtap, Andrew Lurie Salzman
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SUBSTITUTED HETEROARYL ALDEHYDE COMPOUNDS AND METHODS FOR THEIR USE IN INCREASING TISSUE OXYGENATION
Publication number: 20170107199Abstract: Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.Type: ApplicationFiled: December 27, 2016Publication date: April 20, 2017Inventors: Brian W. METCALF, Chihyuan CHUANG, Jeffrey WARRINGTON, Matthew P. JACOBSON -
Publication number: 20170107200Abstract: Compounds of formula (I) wherein m is 0 or 1; Z is methine or nitrogen; X is oxygen or sulfur, R1 is C1-C6-alkyl, halo-C1-C6-alkyl, C3-C6-cycloalkyl or C2-C6-alkynyl; R2 is C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, halo-C3-C6-cycloalkyl, fluoro, chloro or bromo; R3 is C1-C3-alkyl; R4 is hydrogen, C1-C6-alkyl, fluoro, chloro, bromo or cyano; Y is CN, COOR9 or CONHR6; n is 0, 1 or 2; R5 is hydrogen, fluoro, chloro or bromo; R6 is C1-C4-alkyl; R9 is C1-C4-alkyl; R10 and R11 are, independently from each other, hydrogen, C1-C3-alkyl or C1-C3-alkoxy; or R10 and R11 taken together form with the carbon atom to which they are bonded a C3-C6-carbocyclic ring; or R10 and R11 taken together form a ketone or a ?NOR12 group; and R12 is hydrogen or C1-C4-alkyl; and agrochemically acceptable salts and enantiomers of those compounds can be used as insecticides an can be prepared in a manner known per se.Type: ApplicationFiled: March 18, 2015Publication date: April 20, 2017Applicant: Syngenta Participations AGInventors: Andre Jeanguenat, Andrew Edmunds, Roger Graham Hall
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Publication number: 20170107201Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoismers, 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: March 27, 2015Publication date: April 20, 2017Applicant: Syngenta Participations AGInventors: Michel Muehlebach, Ruud Titulaer, Daniel Emery, Andrew Edmunds, Andre Stoller, Pierre Joseph Marcel Jung, Anke Buchholz, Peter Renold
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Publication number: 20170107202Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.Type: ApplicationFiled: October 11, 2016Publication date: April 20, 2017Inventors: KAP-SUN YEUNG, Timothy P. Connolly, David B. Frennesson, Katharine A. Grant-Young, Piyasena Hewawasam, David R. Langley, Zhaoxing Meng, Eric Mull, Kyle E. Parcella, Mark George Saulnier, Li-Qiang Sun, Alan Xiangdong Wang, Ningning Xu, Juliang Zhu, Paul Michael Scola
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Publication number: 20170107203Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (1)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.Type: ApplicationFiled: February 26, 2015Publication date: April 20, 2017Applicants: Epirus Biopharmaceuticals, Inc., Epirus Biopharmaceuticals, Inc.Inventors: Hassan PAJOUHESH, Richard HOLLAND, Lingyun ZHANG, Hossein PAJOUHESH, Jason LAMONTAGNE, Brendan WHELAN
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Publication number: 20170107204Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.Type: ApplicationFiled: March 23, 2015Publication date: April 20, 2017Applicant: Merck Sharp & Dohme Corp.Inventors: Helen Mitchell, Harold B. Wood, Chun Sing Li, Qinghua Mao, Zhiqi Qi
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Publication number: 20170107205Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: June 1, 2016Publication date: April 20, 2017Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara S. HADIDA RUAH, Matthew M. Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20170107206Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: June 3, 2016Publication date: April 20, 2017Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara S. HADIDA RUAH, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20170107207Abstract: The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which has an excellent inhibitory action on the ATPase activity of a TIP48/TIP49 complex and as such, is useful for the treatment of tumors. [Solution] The present invention provides a compound having a structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the present specification.Type: ApplicationFiled: February 17, 2015Publication date: April 20, 2017Applicant: Daiichi Sankyo Company, LimitedInventors: Masayuki Ebisawa, Takashi Suzuki, Noriyasu Haginoya, Tomoaki Hamada, Takeshi Murata, Kouichi Uoto, Ryo Murakami, Takehiko Takata
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Publication number: 20170107208Abstract: The present invention relates to a process for preparing substituted piperidine compounds and especially chiral substituted piperidine compounds. The process involves reacting a substituted pyridinium ion with an amine as defined herein, in the presence of a hydrogen donor, a catalysts and a suitable solvent.Type: ApplicationFiled: March 24, 2015Publication date: April 20, 2017Inventors: Jianliang XIAO, Jianjun WU
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Publication number: 20170107209Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: December 27, 2016Publication date: April 20, 2017Applicant: IMAGO PHARMACEUTICALS, INC.Inventors: Hing L. SHAM, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gregely Toth
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Publication number: 20170107210Abstract: This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders.Type: ApplicationFiled: May 23, 2016Publication date: April 20, 2017Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang
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Publication number: 20170107211Abstract: The present invention provides a medicament for treating a disease involving Nav 1.7 such as neuropathic pain, nociceptive pain, inflammatory pain, small-fiber neuropathy, erythromelalgia, paroxysmal extreme pain disorder, dysuria, and multiple sclerosis, which comprises a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c and R1d are hydrogen, halogen, cyano, C1-4 alkyl, C1-4 alkoxy, or the like, provided that at least one of R1a, R1b, R1c and R1d is C6-10 aryl, C6-10 aryloxy, or the like, R2 and R3 are hydrogen, C1-6 alkyl, C3-10 cycloalkyl, or the like, R4 is hydrogen, C1-6 alkyl, C3-7 cycloalkyl, or the like, m is 1, 2 or 3, L is CR7R8, and R7 and R8 are hydrogen, hydroxyl, C1-4 alkyl, C1-4 alkoxy, or the like.Type: ApplicationFiled: December 30, 2016Publication date: April 20, 2017Inventors: Masafumi Komiya, Kohei Iwamoto, Toshio Kanai, Shingo Mizushima, Keiji Adachi, Kuniko Urashima
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Publication number: 20170107212Abstract: The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: March 18, 2015Publication date: April 20, 2017Inventors: Kai THEDE, Eckhard BENDER, William SCOTT, Anja GIESE, Ludwig ZORN, Ningshu LIU, Ursula MÖNNING, Franziska SIEGEL, Stefan GOLZ, Andrea HÄGEBARTH, Philip LIENAU, Florian PUEHLER, Daniel BASTING, Dirk SCHNEIDER, Manfred MÖWES, Jens GEISLER
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Publication number: 20170107213Abstract: Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.Type: ApplicationFiled: March 21, 2015Publication date: April 20, 2017Inventors: Xiaowu DONG, Jia LI, Bo YANG, Yongzhou HU, Yubo ZHOU, Qinjie WENG, Wenhu ZHAN, Lei XU, Tao LIU, Qiaojun HE
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Publication number: 20170107214Abstract: The invention relates to compounds of Formula (I) wherein R1, R2, R3, R4 and R5 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.Type: ApplicationFiled: March 23, 2015Publication date: April 20, 2017Applicant: ACTELION PHARMACEUTICALS LTDInventors: Eva CAROFF, Rémy CASTRO, Emmanuel MEYER, Thierry KIMMERLIN
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Publication number: 20170107215Abstract: Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.Type: ApplicationFiled: September 26, 2016Publication date: April 20, 2017Inventors: Qingping Zeng, Mary Faris, Alexis Mollard, Steven L. Warner, Gary A. Flynn
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Publication number: 20170107216Abstract: Disclosed are compounds of Formula (I?), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.Type: ApplicationFiled: October 18, 2016Publication date: April 20, 2017Inventors: Liangxing Wu, Bo Shen, Jingwei Li, Zhenwu Li, Kai Liu, Fenglei Zhang, Wenqing Yao
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Publication number: 20170107217Abstract: The present application provides a hetero-cyclic compound which may significantly improve the service life, efficiency, electrochemical stability, and thermal stability of an organic light emitting device, and an organic light emitting device in which the hetero-cyclic compound is contained in an organic compound layer.Type: ApplicationFiled: May 15, 2015Publication date: April 20, 2017Applicant: HEESUNG MATERIAL LTD.Inventors: Jung-Hyun LEE, Kee-Yong KIM, Yong-Hoon AN, Jin-Seok CHOI, Dae-Hyuk CHOI, Sung-Jin EUM, Joo-Dong LEE
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Publication number: 20170107218Abstract: This disclosure relates generally to compounds and compositions comprising one or more indole analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory diseases.Type: ApplicationFiled: May 29, 2015Publication date: April 20, 2017Inventors: Ming-MIng Zhou, Guillermo Gerona-Navarro, Yoel Rodriguez-Fernandez, Patrizia Casaccia
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Publication number: 20170107219Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen, or substituted or unsubstituted alkyl, R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or the like, with the proviso that R1, R2 and R3 are not simultaneously hydrogen, X is a single bond, —S—, —O—, —NR5—, —C(?O)— or the like, R5 is hydrogen, or substituted or unsubstituted alkyl, Y is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl or the like.Type: ApplicationFiled: December 27, 2016Publication date: April 20, 2017Applicant: Shionogi & Co., Ltd.Inventors: Eiichi KOJIMA, Keisuke Tonogaki, Nobuyuki Tanaka, Manabu Katou, Akira Ino, Masafumi Iwatsu, Masahiko Fujioka, Yu Hinata, Naoki Ohyabu
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Publication number: 20170107220Abstract: The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, Y, and Z are defined as set forth in the specification. The invention is also directed to use of compounds of any one of Formulae I-VIII, and the pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the invention are especially useful for treating pain.Type: ApplicationFiled: June 12, 2015Publication date: April 20, 2017Inventors: Jae Hyun Park, Laykea Tafesse
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Publication number: 20170107221Abstract: There are disclosed imidazolinopyrimidinone compounds that have activity to induce TRAIL gene expression in macrophages. There is further disclosed a method for treating various cancers comprising administering effective amounts of an imidazolinopyrimidinone having the structure of Formula I herein. The invention is directed, in various embodiments, to a compound and pharmaceutical composition comprising an effective amount of a compound capable of inducing expression of TRAIL gene in cells capable of expressing the TRAIL gene to produce the cytokine TRAIL.Type: ApplicationFiled: March 30, 2015Publication date: April 20, 2017Inventors: Kim D. Janda, Nicholas T. Jacob, Jonathan W. Lockner
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Publication number: 20170107222Abstract: The invention provides novel substituted pyridyl piperidine compounds according to Formula (I) which are Wnt pathway inhibitors, their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.Type: ApplicationFiled: March 10, 2015Publication date: April 20, 2017Applicants: MERCK PATENT GMBH, Cancer Research Technology LimitedInventors: Kai SCHIEMANN, Frank STIEBER, Michel CALDERINI, Julian BLAGG, Aurelie MALLINGER, Dennis WAALBOER, Christian RINK, Simon Ross CRUMPLER
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Publication number: 20170107223Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is one of the groups represented below wherein A is a bond, CH?CH or C?C; U is N or CH; V is N or CH; W represents N or CH; and R1A, R2A, R3A, R1B and R1C are as defined in the claims; and salts thereof.Type: ApplicationFiled: March 3, 2015Publication date: April 20, 2017Inventors: Gaelle CHAPOUX, Jean-Christophe GAUVIN, Azely MIRRE, Philippe PANCHAUD, Christine SCHMITT, Jean-Luc SPECKLIN, Jean-Philippe SURIVET
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Publication number: 20170107224Abstract: A compound represented by Chemical Formula 1 wherein each substituent is the same as defined in the specification, a photosensitive resin composition including the same, and a color filter manufactured using the photosensitive resin composition are provided.Type: ApplicationFiled: September 15, 2016Publication date: April 20, 2017Inventors: Chae Won PAK, Hye Won SEO, Myoung Youp SHIN, Eui Soo JEONG, Seung Jib CHOI
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Publication number: 20170107225Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 19, 2016Publication date: April 20, 2017Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Publication number: 20170107226Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.Type: ApplicationFiled: December 22, 2016Publication date: April 20, 2017Inventors: Takeshi HONDO, Keita NAKANISHI, Tatsuya NIIMI, Masaichi WARIZAYA, Ichiji NAMATAME, Katsuya HARADA
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Publication number: 20170107227Abstract: The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formula (I)-(XXVI) and (III?) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.Type: ApplicationFiled: December 23, 2016Publication date: April 20, 2017Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: Ulla Hansen, Scott Schaus, Trevor Grant, Joshua Bishop, John Kavouris, Lisa M. Christadore