Patents Issued in August 3, 2017
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Publication number: 20170217926Abstract: 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: ApplicationFiled: April 17, 2017Publication date: August 3, 2017Applicant: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Rainer E. Martin, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20170217927Abstract: 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: ApplicationFiled: August 7, 2015Publication date: August 3, 2017Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Koji SHIRAKI, Tadanobu NAKAYAMA, Tomoaki OTA
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Publication number: 20170217928Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.Type: ApplicationFiled: March 26, 2015Publication date: August 3, 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: 20170217929Abstract: 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: ApplicationFiled: April 21, 2015Publication date: August 3, 2017Applicant: The Feinstein Institute For Medical ResearchInventors: Rosamaria Ruggieri, Yousef Al-Abed, Marc Symons
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Publication number: 20170217930Abstract: 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: ApplicationFiled: May 6, 2015Publication date: August 3, 2017Applicant: Bristol-Meyers Squibb CompanyInventor: Chongqing Sun
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Publication number: 20170217931Abstract: 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: ApplicationFiled: July 22, 2015Publication date: August 3, 2017Applicant: Bayer Animal Health GMBHInventors: Claudia WELZ, Adeline KÖHLER, Kirsten BÖRNGEN, Ulrich GÖRGENS, Hans-Georg SCHWARZ
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Publication number: 20170217932Abstract: 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: ApplicationFiled: February 1, 2017Publication date: August 3, 2017Inventors: Matthew Duncton, Rajinder Singh
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Publication number: 20170217933Abstract: 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: ApplicationFiled: April 19, 2017Publication date: August 3, 2017Inventor: Gregory Notte
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Publication number: 20170217934Abstract: 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: ApplicationFiled: April 20, 2017Publication date: August 3, 2017Inventors: Thomas HIMMLER, Sergii PAZENOK, Frank VOLZ, Norbert LUI
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Publication number: 20170217935Abstract: 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: ApplicationFiled: August 17, 2015Publication date: August 3, 2017Inventors: Shunsuke Ozaki, Kenshi Yoshida
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Publication number: 20170217936Abstract: 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: ApplicationFiled: December 16, 2016Publication date: August 3, 2017Applicant: 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
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Publication number: 20170217937Abstract: 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: ApplicationFiled: August 5, 2015Publication date: August 3, 2017Applicants: Miyoshi Oil & Fat Co., Ltd., Tokai Optical Co., Ltd.Inventors: Koji KAWAI, Kotaro KANEKO, Nobuhiro KANEKO, Yuichi SHISHINO, Kuniyoshi OKAMOTO
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Publication number: 20170217938Abstract: 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: ApplicationFiled: October 14, 2015Publication date: August 3, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Dirk KOSEMUND, Ulrich LÜCKING, Gerhard SIEMEISTER, Arne SCHOLZ, Philip LIENAU
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Publication number: 20170217939Abstract: 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: ApplicationFiled: April 13, 2017Publication date: August 3, 2017Inventors: 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
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Publication number: 20170217940Abstract: 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: ApplicationFiled: December 15, 2014Publication date: August 3, 2017Applicant: Merck Sharp & Dohme Corp.Inventors: Joseph Kozlowski, Craig Coburn, Wensheng Yu, Ling Tong, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang, Tao Ji
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Publication number: 20170217941Abstract: 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: ApplicationFiled: June 25, 2015Publication date: August 3, 2017Inventor: John Emmerson CAMPBELL
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Publication number: 20170217942Abstract: 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: ApplicationFiled: August 5, 2015Publication date: August 3, 2017Applicant: Merck Sharp & Dohme Corp.Inventors: Harry Chobanian, Duane DeMong, Christopher W. Plummer, Minghai Fang, Bin Hu
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Publication number: 20170217943Abstract: Described herein are compounds and compositions for the treatment of a fibrotic disease.Type: ApplicationFiled: April 14, 2017Publication date: August 3, 2017Inventors: Luke LAIRSON, Michael BOLLONG, Peter G. SCHULTZ, Arnab K. CHATTERJEE, Baiyuan YANG, Puneet KUMAR, Kaveri URKALAN
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Publication number: 20170217944Abstract: 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: ApplicationFiled: August 9, 2016Publication date: August 3, 2017Applicant: Yeomyung Biochem Co., LtdInventors: Jae Duk LEE, Hyun Jin AN, Da Hye PARK, Yong Sub YI, Yong Hwa LEE
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Publication number: 20170217945Abstract: 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: ApplicationFiled: June 26, 2015Publication date: August 3, 2017Applicant: AstraZeneca ABInventors: Gavin O'Mahony, Michael Kossenjans, Karl Edman, Johan Kajanus, Carl Anders Hogner, Philip Cornwall, Andrew Turner
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Publication number: 20170217946Abstract: 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: ApplicationFiled: July 22, 2015Publication date: August 3, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Lars BÄRFACKER, Tobias HEINRICH, Gerhard SIEMEISTER, Stefan PRECHTL, Detlef STÖCKIGT, Antje ROTTMANN
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Publication number: 20170217947Abstract: 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: ApplicationFiled: August 4, 2015Publication date: August 3, 2017Applicant: Sandoz AGInventors: Roland Barth, Kathrin Höferl-Prantz, Frank Richter, Gerhard Schwenter
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Publication number: 20170217948Abstract: 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: ApplicationFiled: July 29, 2015Publication date: August 3, 2017Applicant: Teijin Pharma LimitedInventors: Takashi SHIRAKURA, Yoshimasa TAKAHASHI, Asahi KAWANA, Chikashi KANAZAWA
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Publication number: 20170217949Abstract: 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: ApplicationFiled: April 14, 2017Publication date: August 3, 2017Applicant: Bayer Intellectual Property GmbHInventors: Ulrich LÜCKING, Rolf BOHLMANN, Arne SCHOLZ, Gerhard SIEMEISTER, Mark Jean GNOTH, Ulf BÖMER, Dirk KOSEMUND, Philip LIENAU, Gerd RÜHTER, Carsten SCHULTZ-FADEMRECHT
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Publication number: 20170217950Abstract: 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: ApplicationFiled: April 18, 2017Publication date: August 3, 2017Applicant: H. Lundbeck A/SInventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Publication number: 20170217951Abstract: 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: ApplicationFiled: June 9, 2015Publication date: August 3, 2017Applicant: Sanford-Burnham Medical Research InstituteInventors: Nicholas David Peter COSFORD, DHANYA Raveendra-Panickar, Douglas J. SHEFFLER
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Publication number: 20170217952Abstract: 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: ApplicationFiled: January 24, 2017Publication date: August 3, 2017Inventors: Chiajen Lai, Lok Him Lawrence Yu, Richard Hung Chiu Yu
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Publication number: 20170217953Abstract: 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: ApplicationFiled: August 4, 2015Publication date: August 3, 2017Applicant: Syngenta Participations AGInventors: Tomas SMEJKAL, Helmars SMITS
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Publication number: 20170217954Abstract: 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: ApplicationFiled: March 18, 2015Publication date: August 3, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Alexandros VAKALOPOULOS, Philipp BUCHGRABER, Niels LINDNER, Markus FOLLMANN, Frank WUNDER, Johannes-Peter STASCH, Tobias MARQUARDT, Gorden REDLICH, Lisa DIETZ, Volkhart Min-Jian LI
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Publication number: 20170217955Abstract: 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: ApplicationFiled: May 5, 2016Publication date: August 3, 2017Applicants: The Broad Institute, Inc., The General Hospital Corporation d/b/a Massachusetts General Hospital, Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
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Publication number: 20170217956Abstract: 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: ApplicationFiled: July 24, 2015Publication date: August 3, 2017Applicant: INNOV17 LLCInventors: Anderson Gaweco, Jefferson Tilley, James Blinn
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Publication number: 20170217957Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).Type: ApplicationFiled: July 29, 2015Publication date: August 3, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Johannes PLATZEK, Gunnar GARKE, Alfons GRUNENBERG
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Publication number: 20170217958Abstract: 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: ApplicationFiled: July 29, 2015Publication date: August 3, 2017Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Tsutomu SATOH, Takashi KUDOH, Tetsuo IWAMA
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Publication number: 20170217959Abstract: 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: ApplicationFiled: December 14, 2016Publication date: August 3, 2017Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Cameron Smith, Ryan Hudson, Adam D. Hughes
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Publication number: 20170217960Abstract: 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: ApplicationFiled: January 27, 2017Publication date: August 3, 2017Inventor: David Ferguson
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Publication number: 20170217961Abstract: 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: ApplicationFiled: March 2, 2017Publication date: August 3, 2017Inventors: MARTIN SCOBIE, THOMAS HELLEDAY, TOBIAS KOOLMEISTER, SYLVAIN JACQUES, MATTHIEU DESROSES, MARIE-CAROLINE JACQUES-CORDONNIER
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Publication number: 20170217962Abstract: 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: ApplicationFiled: July 21, 2015Publication date: August 3, 2017Inventors: Vipin TYAGI, Kallimulla MOHAMMAD, Bishwa Prakash RAI, Mohan PRASAD
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Publication number: 20170217963Abstract: 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: ApplicationFiled: September 28, 2015Publication date: August 3, 2017Inventors: Edward Roberts, Hugh Rosen, Mariangela Urbano, Miguel A. Guerrero
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Publication number: 20170217964Abstract: 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: ApplicationFiled: May 15, 2015Publication date: August 3, 2017Applicant: FUJIAN BORO MEDICAL CO., LTD.Inventor: Dequn LI
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Publication number: 20170217965Abstract: 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: ApplicationFiled: July 22, 2015Publication date: August 3, 2017Inventor: Qingeng LI
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Publication number: 20170217966Abstract: 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: ApplicationFiled: February 16, 2017Publication date: August 3, 2017Inventors: Yong Liu, Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Peter Brent Sampson, Miklos Feher, Grace Ng, Narendra Kumar B. Patel, Yunhui Lang
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Publication number: 20170217967Abstract: 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: ApplicationFiled: April 11, 2017Publication date: August 3, 2017Inventors: Tim G. Elford, Peter Chee-Chu Fung, Michael Laird Hurrey, Dimitrios Stefanidis, Dragos Vizitiu
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Publication number: 20170217968Abstract: 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: ApplicationFiled: April 17, 2017Publication date: August 3, 2017Inventors: 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
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Publication number: 20170217969Abstract: 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: ApplicationFiled: April 18, 2017Publication date: August 3, 2017Inventors: Bruce Bryan, Hendrik Schmidt, Millard Cull
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Publication number: 20170217970Abstract: 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: ApplicationFiled: April 20, 2017Publication date: August 3, 2017Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Yuichi KAWAI, Hiroki IRIE, Takeshi SAGARA, Kazutaka MIYADERA
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Publication number: 20170217971Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.Type: ApplicationFiled: July 30, 2015Publication date: August 3, 2017Applicant: Janssen Pharmaceutica NVInventors: 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
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Publication number: 20170217972Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.Type: ApplicationFiled: July 30, 2015Publication date: August 3, 2017Applicant: Janssen Pharmaceutica NVInventors: Sergio-Alvar Alonso-de Diego, Michiel Luc, Maria Van Gool, Óscar Delgado-González, José Ignacio Andrés-Gil, Andrés Avelino Trabanco-Suárez
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Publication number: 20170217973Abstract: 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: ApplicationFiled: August 3, 2015Publication date: August 3, 2017Inventors: María del Mar CUADRADO TEJEDOR, Ana Maria GARCÍA OSTA, Julen OYARZABAL SANTAMARINA, Maria Obdulia RABAL GRACIA, Juan Antonio SÁNCHEZ ARIAS, Ana UGARTE BAZTÁN
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Publication number: 20170217974Abstract: 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: ApplicationFiled: February 1, 2017Publication date: August 3, 2017Inventors: Yat Sun Or, Meizhong Jin, Jorden Kass, Hui Cao, Xuri Gao, Wei Li, Xiaowen Peng, Yao-Ling Qiu
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Publication number: 20170217975Abstract: 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: ApplicationFiled: August 6, 2015Publication date: August 3, 2017Inventors: Peng LI, Hailin ZHENG, Jun ZHAO, Lawrence P. WENNOGLE