Patents Issued in August 3, 2017
  • Publication number: 20170217926
    Abstract: The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Application
    Filed: April 17, 2017
    Publication date: August 3, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Rainer E. Martin, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20170217927
    Abstract: An amorphous form of 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile and a solid dispersion containing the amorphous form can be used extremely advantageously as drugs for oral administration.
    Type: Application
    Filed: August 7, 2015
    Publication date: August 3, 2017
    Applicant: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Koji SHIRAKI, Tadanobu NAKAYAMA, Tomoaki OTA
  • Publication number: 20170217928
    Abstract: 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: Application
    Filed: March 26, 2015
    Publication date: August 3, 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: 20170217929
    Abstract: Methods and compounds are described for treating solid tumors, and in particular, malignant, neoplastic solid tumors such as glioblastoma and medulloblastoma, by inhibiting protein kinase MRK/ZAK activity. Also provided are pharmaceutical composition containg a MRK/ZAK inhibitor compound and a pharmaceutically acceptable carrier and a method of sensitizing tumor cells to radiation therapy comprising administering an effective amount of the MRK/ZAK inhibitor compound.
    Type: Application
    Filed: April 21, 2015
    Publication date: August 3, 2017
    Applicant: The Feinstein Institute For Medical Research
    Inventors: Rosamaria Ruggieri, Yousef Al-Abed, Marc Symons
  • Publication number: 20170217930
    Abstract: The present invention provides compounds of Formula (I) or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Application
    Filed: May 6, 2015
    Publication date: August 3, 2017
    Applicant: Bristol-Meyers Squibb Company
    Inventor: Chongqing Sun
  • Publication number: 20170217931
    Abstract: Disclosed are compounds of formula (I) which possess anthelminthic properties wherein the structural elements have the meaning as indicated in the description. Further disclosed are such compounds for the control, treatment and/or prevention of infections with helminths in animals and humans.
    Type: Application
    Filed: July 22, 2015
    Publication date: August 3, 2017
    Applicant: Bayer Animal Health GMBH
    Inventors: Claudia WELZ, Adeline KÖHLER, Kirsten BÖRNGEN, Ulrich GÖRGENS, Hans-Georg SCHWARZ
  • Publication number: 20170217932
    Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include 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: Application
    Filed: February 1, 2017
    Publication date: August 3, 2017
    Inventors: Matthew Duncton, Rajinder Singh
  • Publication number: 20170217933
    Abstract: The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.
    Type: Application
    Filed: April 19, 2017
    Publication date: August 3, 2017
    Inventor: Gregory Notte
  • Publication number: 20170217934
    Abstract: The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) in which R1, R2, R3 and R4 are each as defined in the description, by conversion of compounds of the general formula (IV) in the presence of a palladium catalyst and carbon monoxide. The present invention likewise relates to compounds of the general formula (IV).
    Type: Application
    Filed: April 20, 2017
    Publication date: August 3, 2017
    Inventors: Thomas HIMMLER, Sergii PAZENOK, Frank VOLZ, Norbert LUI
  • Publication number: 20170217935
    Abstract: The present invention provides salts consisting of an organocarboxylic acid selected from the group consisting of succinic acid and maleic acid and a compound represented by formula (I) and crystals thereat which can be used as bulk materials for pharmaceuticals.
    Type: Application
    Filed: August 17, 2015
    Publication date: August 3, 2017
    Inventors: Shunsuke Ozaki, Kenshi Yoshida
  • Publication number: 20170217936
    Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(?X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Application
    Filed: December 16, 2016
    Publication date: August 3, 2017
    Applicant: Array BioPharma Inc.
    Inventors: Shelley Allen, Steven W. Andrews, James F. Blake, Kevin R. Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Gabrielle R. Kolakowski, Jeongbeob Seo
  • Publication number: 20170217937
    Abstract: Provided is an additive for imparting ultraviolet absorbency, or an additive for imparting a high refractive index, which has satisfactory compatibility with a resin serving as a matrix and can maintain high transparency even if added in high concentrations. Also provided is an additive with which the function of imparting both ultraviolet absorbency and a high refractive index can be realized by means of one kind of additive. This additive is represented by the following Formula (I): wherein at least one of R1a to R9a is a monovalent sulfur-containing group represented by the following Formula (i-1) or Formula (i-2): wherein R10a to R12a each represent a divalent hydrocarbon group or the like; and R13a represents a monovalent hydrocarbon group or the like.
    Type: Application
    Filed: August 5, 2015
    Publication date: August 3, 2017
    Applicants: Miyoshi Oil & Fat Co., Ltd., Tokai Optical Co., Ltd.
    Inventors: Koji KAWAI, Kotaro KANEKO, Nobuhiro KANEKO, Yuichi SHISHINO, Kuniyoshi OKAMOTO
  • Publication number: 20170217938
    Abstract: The present invention relates to fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Application
    Filed: October 14, 2015
    Publication date: August 3, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Dirk KOSEMUND, Ulrich LÜCKING, Gerhard SIEMEISTER, Arne SCHOLZ, Philip LIENAU
  • Publication number: 20170217939
    Abstract: The present application relates to crystalline and amorphous Vilazodone hydrochloride. The present application further relates to amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carriers. The present application also relates to a process for the preparation of form I of vilazodone free base.
    Type: Application
    Filed: April 13, 2017
    Publication date: August 3, 2017
    Inventors: Javed IQBAL, Srinivas ORUGANTI, Rajesh Kumar RAPOLU, Vishweshwar PEDDY, Rajesham BOGE, Deepika PATHIVADA, Dharma Jagannadha Rao VELAGA, Sesha Reddy YARRAGUNTLA, Sudhakar Reddy BADDAM, Anitha NAREDLA, Kiran Kumar DONIPARTHI, Ramesh Kumar NADGOUD, Narasimha Rao PAGADALA, Syam Kumar UNNIARAN, Srividya RAMAKRISHNAN
  • Publication number: 20170217940
    Abstract: The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A?, R2A, R2B, R7, R8, R9, and R10 are defined herein. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The present invention also relates to pharmaceutical compositions comprising at least one Fused Tetracyclic Heterocyclic Compound, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines, and methods of using the Fused Tetracyclic Heterocyclic Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: December 15, 2014
    Publication date: August 3, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph Kozlowski, Craig Coburn, Wensheng Yu, Ling Tong, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang, Tao Ji
  • Publication number: 20170217941
    Abstract: The present invention relates to substituted benzene compounds and bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: June 25, 2015
    Publication date: August 3, 2017
    Inventor: John Emmerson CAMPBELL
  • Publication number: 20170217942
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Application
    Filed: August 5, 2015
    Publication date: August 3, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Duane DeMong, Christopher W. Plummer, Minghai Fang, Bin Hu
  • Publication number: 20170217943
    Abstract: Described herein are compounds and compositions for the treatment of a fibrotic disease.
    Type: Application
    Filed: April 14, 2017
    Publication date: August 3, 2017
    Inventors: Luke LAIRSON, Michael BOLLONG, Peter G. SCHULTZ, Arnab K. CHATTERJEE, Baiyuan YANG, Puneet KUMAR, Kaveri URKALAN
  • Publication number: 20170217944
    Abstract: Disclosed are taxifolin derivative with superior antioxidant effect, a method of synthesizing the same and a cosmetic composition containing the same. In accordance with the method, taxifolin derivatives having higher antioxidant activity than taxifolin can be synthesized using lipoic acid. As such, a novel taxifolin derivative synthesized according to the present invention can exhibit anti-aging effects when used for cosmetics and the like.
    Type: Application
    Filed: August 9, 2016
    Publication date: August 3, 2017
    Applicant: Yeomyung Biochem Co., Ltd
    Inventors: Jae Duk LEE, Hyun Jin AN, Da Hye PARK, Yong Sub YI, Yong Hwa LEE
  • Publication number: 20170217945
    Abstract: Disclosed are certain derivatives of benzoxazinone amides of formula (I), or pharmaceutically acceptable salts thereof, (Formula (I)) that act as mineralocorticoid (MR) receptor modulators that may reduce oxidative stress in endothelium and hence improve vascular function, to methods for their potential therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.
    Type: Application
    Filed: June 26, 2015
    Publication date: August 3, 2017
    Applicant: AstraZeneca AB
    Inventors: Gavin O'Mahony, Michael Kossenjans, Karl Edman, Johan Kajanus, Carl Anders Hogner, Philip Cornwall, Andrew Turner
  • Publication number: 20170217946
    Abstract: The present invention relates to amino-substituted isoxazoles of general formula (I): in which A, R1 and R2 are as defined in the claims, 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 neoplasms, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: July 22, 2015
    Publication date: August 3, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Lars BÄRFACKER, Tobias HEINRICH, Gerhard SIEMEISTER, Stefan PRECHTL, Detlef STÖCKIGT, Antje ROTTMANN
  • Publication number: 20170217947
    Abstract: The present invention relates to a process for the preparation of a compound of formula (A), Further, the present invention relates to the respective compound (A) as such and to its use in the preparation of antifungal agent.
    Type: Application
    Filed: August 4, 2015
    Publication date: August 3, 2017
    Applicant: Sandoz AG
    Inventors: Roland Barth, Kathrin Höferl-Prantz, Frank Richter, Gerhard Schwenter
  • Publication number: 20170217948
    Abstract: Provided are a xanthine oxidase inhibitor, a drug for improving vascular endothelial function, and an excellent therapeutic or prophylactic drug for diseases associated with xanthine oxidase such as gout, hyperuricaemia, and for diseases associated with vascular endothelial functional disorder containing a compound represented in a formula (I) or the pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: July 29, 2015
    Publication date: August 3, 2017
    Applicant: Teijin Pharma Limited
    Inventors: Takashi SHIRAKURA, Yoshimasa TAKAHASHI, Asahi KAWANA, Chikashi KANAZAWA
  • Publication number: 20170217949
    Abstract: The present invention relates to 4-aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group of general formula (I) or (Ia) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I) or (Ia).
    Type: Application
    Filed: April 14, 2017
    Publication date: August 3, 2017
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Ulrich LÜCKING, Rolf BOHLMANN, Arne SCHOLZ, Gerhard SIEMEISTER, Mark Jean GNOTH, Ulf BÖMER, Dirk KOSEMUND, Philip LIENAU, Gerd RÜHTER, Carsten SCHULTZ-FADEMRECHT
  • Publication number: 20170217950
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Application
    Filed: April 18, 2017
    Publication date: August 3, 2017
    Applicant: H. Lundbeck A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Publication number: 20170217951
    Abstract: Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: June 9, 2015
    Publication date: August 3, 2017
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Nicholas David Peter COSFORD, DHANYA Raveendra-Panickar, Douglas J. SHEFFLER
  • Publication number: 20170217952
    Abstract: The invention provides a crystalline form of the compound of formula (Ia), methods for making the crystalline form of the compound of formula (Ia), and therapeutic methods for the use of the crystalline form of the compound of formula (Ia).
    Type: Application
    Filed: January 24, 2017
    Publication date: August 3, 2017
    Inventors: Chiajen Lai, Lok Him Lawrence Yu, Richard Hung Chiu Yu
  • Publication number: 20170217953
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is C1-C4alkyl, C1-C4haloalkyl or C3-C6cycloalkyl; each R2 is independently bromo, chloro, fluoro or trifluoromethyl; R3 is hydrogen; R4 is hydrogen, halogen, methyl, halomethyl or cyano; or R3 and R4 together form a bridging 1,3-butadiene group; R5 is chlorodifluoro-methyl or trifluoromethyl; n is 2 or 3; by reacting a compound of formula (II) wherein A1, A2, R1, R2, R3, R4, R5 and n is as defined under formula (I) above, with hydroxylamine, a base and a chiral catalyst, characterized in that the chiral catalyst is a dimeric chiral catalyst of formula (III) wherein R6, R7, R8, R9, R10 and X are as defmed in claim 1.
    Type: Application
    Filed: August 4, 2015
    Publication date: August 3, 2017
    Applicant: Syngenta Participations AG
    Inventors: Tomas SMEJKAL, Helmars SMITS
  • Publication number: 20170217954
    Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: March 18, 2015
    Publication date: August 3, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Alexandros VAKALOPOULOS, Philipp BUCHGRABER, Niels LINDNER, Markus FOLLMANN, Frank WUNDER, Johannes-Peter STASCH, Tobias MARQUARDT, Gorden REDLICH, Lisa DIETZ, Volkhart Min-Jian LI
  • Publication number: 20170217955
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R1a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Application
    Filed: May 5, 2016
    Publication date: August 3, 2017
    Applicants: The Broad Institute, Inc., The General Hospital Corporation d/b/a Massachusetts General Hospital, Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
  • Publication number: 20170217956
    Abstract: Provided herein are compounds of the formulas (I) and (II), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
    Type: Application
    Filed: July 24, 2015
    Publication date: August 3, 2017
    Applicant: INNOV17 LLC
    Inventors: Anderson Gaweco, Jefferson Tilley, James Blinn
  • Publication number: 20170217957
    Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).
    Type: Application
    Filed: July 29, 2015
    Publication date: August 3, 2017
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Johannes PLATZEK, Gunnar GARKE, Alfons GRUNENBERG
  • Publication number: 20170217958
    Abstract: The present invention provides a method for manufacturing a compound represented by formula (I). With this method, provided are a method for manufacturing a 4-heteroaryl-N-(2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1H-pyrazole-5-carboxylic acid amide derivative; and an intermediate for this manufacturing method.
    Type: Application
    Filed: July 29, 2015
    Publication date: August 3, 2017
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Tsutomu SATOH, Takashi KUDOH, Tetsuo IWAMA
  • Publication number: 20170217959
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: December 14, 2016
    Publication date: August 3, 2017
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Cameron Smith, Ryan Hudson, Adam D. Hughes
  • Publication number: 20170217960
    Abstract: The invention provides compounds of formula I: wherein R1—R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.
    Type: Application
    Filed: January 27, 2017
    Publication date: August 3, 2017
    Inventor: David Ferguson
  • Publication number: 20170217961
    Abstract: A compound of formula I, or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1.
    Type: Application
    Filed: March 2, 2017
    Publication date: August 3, 2017
    Inventors: MARTIN SCOBIE, THOMAS HELLEDAY, TOBIAS KOOLMEISTER, SYLVAIN JACQUES, MATTHIEU DESROSES, MARIE-CAROLINE JACQUES-CORDONNIER
  • Publication number: 20170217962
    Abstract: The present invention relates to a process for the preparation of palbociclib utilizing a silyl-protected crotonic acid derivative to produce a silyl-protected 2-chloro-4-(cyclopentylamino)-5-(1-methyl-2-carboxy-ethen-1-yl)pyrmidine followed by intramolecular cyclization of the pyrmidine intermediate to produce 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one which is then converted to palbociclib.
    Type: Application
    Filed: July 21, 2015
    Publication date: August 3, 2017
    Inventors: Vipin TYAGI, Kallimulla MOHAMMAD, Bishwa Prakash RAI, Mohan PRASAD
  • Publication number: 20170217963
    Abstract: The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis.
    Type: Application
    Filed: September 28, 2015
    Publication date: August 3, 2017
    Inventors: Edward Roberts, Hugh Rosen, Mariangela Urbano, Miguel A. Guerrero
  • Publication number: 20170217964
    Abstract: Provided is an Aminotetrahydropyran derivative represented by general formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, and the use of the derivative to prepare a therapeutic agent, especially a dipeptidyl peptidase-IV inhibitor.
    Type: Application
    Filed: May 15, 2015
    Publication date: August 3, 2017
    Applicant: FUJIAN BORO MEDICAL CO., LTD.
    Inventor: Dequn LI
  • Publication number: 20170217965
    Abstract: The present invention relates to a new benzodiazepine derivative, pharmaceutically acceptable salt thereof, preparation method therefor, and use thereof. The benzodiazepine derivative and the pharmaceutically acceptable salt thereof of the present invention have obvious anesthetic effect and low toxicity in body, thereby enhancing the medication safety. The benzodiazepine derivative and the pharmaceutically acceptable salt thereof of the present invention have sedative, hypnotic, and anesthetic effect, and can be used as sedative, hypnotic, and anesthetic drugs.
    Type: Application
    Filed: July 22, 2015
    Publication date: August 3, 2017
    Inventor: Qingeng LI
  • Publication number: 20170217966
    Abstract: The present teachings provide a compound represented by structural formula (I-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: February 16, 2017
    Publication date: August 3, 2017
    Inventors: Yong Liu, Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Peter Brent Sampson, Miklos Feher, Grace Ng, Narendra Kumar B. Patel, Yunhui Lang
  • Publication number: 20170217967
    Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.
    Type: Application
    Filed: April 11, 2017
    Publication date: August 3, 2017
    Inventors: Tim G. Elford, Peter Chee-Chu Fung, Michael Laird Hurrey, Dimitrios Stefanidis, Dragos Vizitiu
  • Publication number: 20170217968
    Abstract: Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
    Type: Application
    Filed: April 17, 2017
    Publication date: August 3, 2017
    Inventors: Roushan AFROZE, lndu T. BHARATHAN, Jeffrey P. CIAVARRI, Paul E. FLEMING, Jeffrey L. GAULIN, Mario GIRARD, Steven P. LANGSTON, Francois SOUCY, Tzu-Tshin WONG, Yingchun YE
  • Publication number: 20170217969
    Abstract: Calcium reacting photoproteins are a class of self-illuminating proteins that emit light upon contact with calcium. Fluorescent Proteins are small proteins that change the color of light when excited. Fluorescent Proteins and Calcium Activated Photoproteins can be used to enhance, dazzle, amaze, startle, and otherwise entertain an audience by their direct application on to the audience, surroundings, the actors, or sprayed on settings as in the newer 4D movies. The disclosure comprises novel Coelenterazine compounds and methods of use, including a simple delivery device for the photoprotein to create unique and novel cinematic, theatrical, stage, movie and musical concert optical effects by their luminous reaction upon contact with surfaces that contain calcium. Calcium is ubiquitous in and on most surfaces and in the environment; it is this unique property of calcium that makes this a novel use of the photoproteins for entertainment.
    Type: Application
    Filed: April 18, 2017
    Publication date: August 3, 2017
    Inventors: Bruce Bryan, Hendrik Schmidt, Millard Cull
  • Publication number: 20170217970
    Abstract: To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 inhibitory effect. The present invention provides a compound of formula (I) wherein X, Y, Z1, Z2, Z3, Z4, W, n, R1, R2, and R3 have meanings as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: April 20, 2017
    Publication date: August 3, 2017
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Yuichi KAWAI, Hiroki IRIE, Takeshi SAGARA, Kazutaka MIYADERA
  • Publication number: 20170217971
    Abstract: 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: Application
    Filed: July 30, 2015
    Publication date: August 3, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Sergio-Alvar Alonso-de Diego, Michiel Luc, Maria Van Gool, Maria Luz Martín-Martín, Susana Conde-Ceide, José Ignacio Andrés-Gil, Óscar Delgado-González, Gary John Tresadern, Andrés Avelino Trabanco-Suárez
  • Publication number: 20170217972
    Abstract: 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: Application
    Filed: July 30, 2015
    Publication date: August 3, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Sergio-Alvar Alonso-de Diego, Michiel Luc, Maria Van Gool, Óscar Delgado-González, José Ignacio Andrés-Gil, Andrés Avelino Trabanco-Suárez
  • Publication number: 20170217973
    Abstract: Novel compounds for use in cognition improvement It relates to certain compounds having a polycyclic structure and a —(C?O)NRaRb moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neared-generative diseases.
    Type: Application
    Filed: August 3, 2015
    Publication date: August 3, 2017
    Inventors: María del Mar CUADRADO TEJEDOR, Ana Maria GARCÍA OSTA, Julen OYARZABAL SANTAMARINA, Maria Obdulia RABAL GRACIA, Juan Antonio SÁNCHEZ ARIAS, Ana UGARTE BAZTÁN
  • Publication number: 20170217974
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-Z-R??(I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 1, 2017
    Publication date: August 3, 2017
    Inventors: Yat Sun Or, Meizhong Jin, Jorden Kass, Hui Cao, Xuri Gao, Wei Li, Xiaowen Peng, Yao-Ling Qiu
  • Publication number: 20170217975
    Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
    Type: Application
    Filed: August 6, 2015
    Publication date: August 3, 2017
    Inventors: Peng LI, Hailin ZHENG, Jun ZHAO, Lawrence P. WENNOGLE