Patents Issued in April 20, 2017
  • Publication number: 20170107178
    Abstract: 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 atom
    Type: Application
    Filed: March 19, 2015
    Publication date: April 20, 2017
    Applicant: IOMET PHARMA LTD.
    Inventors: Phillip M. COWLEY, Alan WISE, Michael KICZUN, Susan DAVIS
  • Publication number: 20170107179
    Abstract: 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: Application
    Filed: May 25, 2016
    Publication date: April 20, 2017
    Inventors: Xiao-Yi Xiao, Roger B. Clark, Diana Katharine Hunt, Magnus P. Ronn, Louis Plamondon, Minsheng He, Joyce A. Sutcliffe, Trudy Grossman
  • Publication number: 20170107180
    Abstract: 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: Application
    Filed: December 19, 2016
    Publication date: April 20, 2017
    Inventors: Ernest J. MCEACHERN, David J. VOCADLO, Yuanxi ZHOU, Harold G. SELNICK
  • Publication number: 20170107181
    Abstract: 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: Application
    Filed: March 31, 2015
    Publication date: April 20, 2017
    Applicant: Syngenta Participations AG
    Inventors: Thomas James HOFFMAN, Sarah SULZER-MOSSE, Kurt NEBEL, Fredrik Emil Malcolm CEDERBAUM
  • Publication number: 20170107182
    Abstract: Process for preparing 3,5-bis(haloalkyl)pyrazole derivatives of the formula (I), via acylation of Hydrazones.
    Type: Application
    Filed: June 8, 2015
    Publication date: April 20, 2017
    Applicant: Bayer CropScience Aktiengesellschaft
    Inventors: Sergii PAZENOK, Norbert LUI
  • Publication number: 20170107183
    Abstract: 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: Application
    Filed: May 19, 2015
    Publication date: April 20, 2017
    Inventors: Hartmut AHRENS, Jörg TIEBES, Christian WALDRAFF, Hansjörg DIETRICH, Dirk SCHMUTZLER, Elmar GATZWEILER, Christopher ROSINGER
  • Publication number: 20170107184
    Abstract: 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: Application
    Filed: March 16, 2015
    Publication date: April 20, 2017
    Inventors: 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
  • Publication number: 20170107185
    Abstract: 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: Application
    Filed: May 28, 2015
    Publication date: April 20, 2017
    Inventors: 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
  • Publication number: 20170107186
    Abstract: 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: Application
    Filed: March 3, 2015
    Publication date: April 20, 2017
    Inventors: Kazuyuki FUKUDA, Hideaki OTSUKA, Tsutomu YOSHIDA, Tatsuya NAKASHIMA, Toshiaki MORIYA, Shirou HONMA
  • Publication number: 20170107187
    Abstract: 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: Application
    Filed: December 28, 2016
    Publication date: April 20, 2017
    Inventors: Stacy BREMNER, Jerry EVARTS, Keiko SUJINO, Duong TRAN, Dragos VIZITIU
  • Publication number: 20170107188
    Abstract: To provide a novel technique capable of further reducing the argon purge amount in a process for producing ethylene oxide.
    Type: Application
    Filed: March 31, 2015
    Publication date: April 20, 2017
    Inventors: Yukimasa KAWAGUCHI, Hideto SUZUKI
  • Publication number: 20170107189
    Abstract: 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: Application
    Filed: October 13, 2016
    Publication date: April 20, 2017
    Inventors: David J. Brennan, Gregoire Cardoen, Robert E. Hefner, JR., Antony K. Van Dyk
  • Publication number: 20170107190
    Abstract: 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: Application
    Filed: October 13, 2016
    Publication date: April 20, 2017
    Applicants: University of Pittsburgh - Of the Commonwealth System of Higher Education, Medical University of South Carolina
    Inventors: Peter Wipf, Carol A. Feghali-Bostwick
  • Publication number: 20170107191
    Abstract: 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: Application
    Filed: January 2, 2017
    Publication date: April 20, 2017
    Inventors: Dylan J. Boday, Joseph Kuczynski, Jason T. Wertz, Jing Zhang
  • Publication number: 20170107192
    Abstract: 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: Application
    Filed: December 29, 2016
    Publication date: April 20, 2017
    Inventors: Graciela B. Arhancet, Matthew Mahoney, Xiaojun Wang
  • Publication number: 20170107193
    Abstract: 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: Application
    Filed: August 1, 2014
    Publication date: April 20, 2017
    Applicant: SHILPA MEDICARE LIMITED
    Inventors: SRIRAM RAMPALLI, LAVKUMAR UPALLA, PRASHANT PUROHIT, AKSHAYKANT CHATURVEDI
  • Publication number: 20170107194
    Abstract: 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: Application
    Filed: December 28, 2016
    Publication date: April 20, 2017
    Inventors: Zenon D. Konteatis, Janeta Popovici-Muller, Jeremy M. Travins, Robert Zahler, Zhenwei Cai, Ding Zhou
  • Publication number: 20170107195
    Abstract: 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: Application
    Filed: March 17, 2015
    Publication date: April 20, 2017
    Applicant: AstraZeneca AB
    Inventors: Susanne Elisabeth BERGLUND, Stephen CONNOLLY, Martin HEMMERLING, Nafizal HOSSAIN, Anna KRISTOFFERSSON, Johan Rune Michael LUNDKVIST, Grigorios NIKITIDIS, Lena Elisabeth RIPA, Igor SHAMOVSKY
  • Publication number: 20170107196
    Abstract: 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: Application
    Filed: March 26, 2015
    Publication date: April 20, 2017
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Koichiro DOTA
  • Publication number: 20170107197
    Abstract: 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: Application
    Filed: May 23, 2016
    Publication date: April 20, 2017
    Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
  • Publication number: 20170107198
    Abstract: 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: Application
    Filed: December 19, 2016
    Publication date: April 20, 2017
    Inventors: Prakash Jagtap, Andrew Lurie Salzman
  • Publication number: 20170107199
    Abstract: 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: Application
    Filed: December 27, 2016
    Publication date: April 20, 2017
    Inventors: Brian W. METCALF, Chihyuan CHUANG, Jeffrey WARRINGTON, Matthew P. JACOBSON
  • Publication number: 20170107200
    Abstract: 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: Application
    Filed: March 18, 2015
    Publication date: April 20, 2017
    Applicant: Syngenta Participations AG
    Inventors: Andre Jeanguenat, Andrew Edmunds, Roger Graham Hall
  • Publication number: 20170107201
    Abstract: 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: Application
    Filed: March 27, 2015
    Publication date: April 20, 2017
    Applicant: Syngenta Participations AG
    Inventors: Michel Muehlebach, Ruud Titulaer, Daniel Emery, Andrew Edmunds, Andre Stoller, Pierre Joseph Marcel Jung, Anke Buchholz, Peter Renold
  • Publication number: 20170107202
    Abstract: 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: Application
    Filed: October 11, 2016
    Publication date: April 20, 2017
    Inventors: 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
  • Publication number: 20170107203
    Abstract: 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: Application
    Filed: February 26, 2015
    Publication date: April 20, 2017
    Applicants: Epirus Biopharmaceuticals, Inc., Epirus Biopharmaceuticals, Inc.
    Inventors: Hassan PAJOUHESH, Richard HOLLAND, Lingyun ZHANG, Hossein PAJOUHESH, Jason LAMONTAGNE, Brendan WHELAN
  • Publication number: 20170107204
    Abstract: 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: Application
    Filed: March 23, 2015
    Publication date: April 20, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Harold B. Wood, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • Publication number: 20170107205
    Abstract: 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: Application
    Filed: June 1, 2016
    Publication date: April 20, 2017
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. HADIDA RUAH, Matthew M. Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • Publication number: 20170107206
    Abstract: 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: Application
    Filed: June 3, 2016
    Publication date: April 20, 2017
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. HADIDA RUAH, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • Publication number: 20170107207
    Abstract: 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: Application
    Filed: February 17, 2015
    Publication date: April 20, 2017
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Masayuki Ebisawa, Takashi Suzuki, Noriyasu Haginoya, Tomoaki Hamada, Takeshi Murata, Kouichi Uoto, Ryo Murakami, Takehiko Takata
  • Publication number: 20170107208
    Abstract: 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: Application
    Filed: March 24, 2015
    Publication date: April 20, 2017
    Inventors: Jianliang XIAO, Jianjun WU
  • Publication number: 20170107209
    Abstract: 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: Application
    Filed: December 27, 2016
    Publication date: April 20, 2017
    Applicant: 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
  • Publication number: 20170107210
    Abstract: 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: Application
    Filed: May 23, 2016
    Publication date: April 20, 2017
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang
  • Publication number: 20170107211
    Abstract: 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: Application
    Filed: December 30, 2016
    Publication date: April 20, 2017
    Inventors: Masafumi Komiya, Kohei Iwamoto, Toshio Kanai, Shingo Mizushima, Keiji Adachi, Kuniko Urashima
  • Publication number: 20170107212
    Abstract: 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: Application
    Filed: March 18, 2015
    Publication date: April 20, 2017
    Inventors: 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
  • Publication number: 20170107213
    Abstract: 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: Application
    Filed: March 21, 2015
    Publication date: April 20, 2017
    Inventors: Xiaowu DONG, Jia LI, Bo YANG, Yongzhou HU, Yubo ZHOU, Qinjie WENG, Wenhu ZHAN, Lei XU, Tao LIU, Qiaojun HE
  • Publication number: 20170107214
    Abstract: 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: Application
    Filed: March 23, 2015
    Publication date: April 20, 2017
    Applicant: ACTELION PHARMACEUTICALS LTD
    Inventors: Eva CAROFF, Rémy CASTRO, Emmanuel MEYER, Thierry KIMMERLIN
  • Publication number: 20170107215
    Abstract: Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.
    Type: Application
    Filed: September 26, 2016
    Publication date: April 20, 2017
    Inventors: Qingping Zeng, Mary Faris, Alexis Mollard, Steven L. Warner, Gary A. Flynn
  • Publication number: 20170107216
    Abstract: 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: Application
    Filed: October 18, 2016
    Publication date: April 20, 2017
    Inventors: Liangxing Wu, Bo Shen, Jingwei Li, Zhenwu Li, Kai Liu, Fenglei Zhang, Wenqing Yao
  • Publication number: 20170107217
    Abstract: 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: Application
    Filed: May 15, 2015
    Publication date: April 20, 2017
    Applicant: 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
  • Publication number: 20170107218
    Abstract: 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: Application
    Filed: May 29, 2015
    Publication date: April 20, 2017
    Inventors: Ming-MIng Zhou, Guillermo Gerona-Navarro, Yoel Rodriguez-Fernandez, Patrizia Casaccia
  • Publication number: 20170107219
    Abstract: 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: Application
    Filed: December 27, 2016
    Publication date: April 20, 2017
    Applicant: Shionogi & Co., Ltd.
    Inventors: Eiichi KOJIMA, Keisuke Tonogaki, Nobuyuki Tanaka, Manabu Katou, Akira Ino, Masafumi Iwatsu, Masahiko Fujioka, Yu Hinata, Naoki Ohyabu
  • Publication number: 20170107220
    Abstract: 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: Application
    Filed: June 12, 2015
    Publication date: April 20, 2017
    Inventors: Jae Hyun Park, Laykea Tafesse
  • Publication number: 20170107221
    Abstract: 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: Application
    Filed: March 30, 2015
    Publication date: April 20, 2017
    Inventors: Kim D. Janda, Nicholas T. Jacob, Jonathan W. Lockner
  • Publication number: 20170107222
    Abstract: 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: Application
    Filed: March 10, 2015
    Publication date: April 20, 2017
    Applicants: MERCK PATENT GMBH, Cancer Research Technology Limited
    Inventors: Kai SCHIEMANN, Frank STIEBER, Michel CALDERINI, Julian BLAGG, Aurelie MALLINGER, Dennis WAALBOER, Christian RINK, Simon Ross CRUMPLER
  • Publication number: 20170107223
    Abstract: 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: Application
    Filed: March 3, 2015
    Publication date: April 20, 2017
    Inventors: Gaelle CHAPOUX, Jean-Christophe GAUVIN, Azely MIRRE, Philippe PANCHAUD, Christine SCHMITT, Jean-Luc SPECKLIN, Jean-Philippe SURIVET
  • Publication number: 20170107224
    Abstract: 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: Application
    Filed: September 15, 2016
    Publication date: April 20, 2017
    Inventors: Chae Won PAK, Hye Won SEO, Myoung Youp SHIN, Eui Soo JEONG, Seung Jib CHOI
  • Publication number: 20170107225
    Abstract: 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: Application
    Filed: October 19, 2016
    Publication date: April 20, 2017
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • Publication number: 20170107226
    Abstract: 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: Application
    Filed: December 22, 2016
    Publication date: April 20, 2017
    Inventors: Takeshi HONDO, Keita NAKANISHI, Tatsuya NIIMI, Masaichi WARIZAYA, Ichiji NAMATAME, Katsuya HARADA
  • Publication number: 20170107227
    Abstract: 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: Application
    Filed: December 23, 2016
    Publication date: April 20, 2017
    Applicant: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: Ulla Hansen, Scott Schaus, Trevor Grant, Joshua Bishop, John Kavouris, Lisa M. Christadore