Patents Issued in October 20, 2016
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Publication number: 20160304449Abstract: The object of the present invention is to provide a method of efficiently manufacturing an optically active D- and/or L-form amino acid possessing a thiol group in the side chain by a simple method. The present invention provides a method of manufacturing an amino acid derivative possessing a thiol group in the side chain, characterized in manufacturing an intermediate composition comprising D- and L-forms of an amino acid derivative possessing a thiol group at the ?-position, reacting a hydrolase selective for D- or L-amino acids, and separating the hydrolyzed D- or L-amino acid derivative, as well as an intermediate thereof.Type: ApplicationFiled: October 22, 2014Publication date: October 20, 2016Inventors: Yasuhiro Kajihara, Yasuhito Morishita, Takefumi Murase
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Publication number: 20160304450Abstract: Described herein are compounds that are estrogen receptor modulators of Formula (I): and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: December 17, 2015Publication date: October 20, 2016Applicant: Genentech, Inc.Inventors: Jun Liang, Daniel Fred Ortwine, Xiaojing Wang, Steven P. Govek, Mehmet Kahraman, Johnny Y. Nagasawa, Nicholas D. Smith, Simon Charles Goodacre, Nicholas Charles Ray
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Publication number: 20160304451Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: February 19, 2016Publication date: October 20, 2016Inventors: Steven W. Elmore, Aaron R. Kunzer, Robert A. Mantei, Andrew J. Souers, Gerard M. Sullivan, Gary T. Wang, Le Wang, Michael D. Wendt
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Publication number: 20160304452Abstract: Provided is a method for preparing silodosin. Also provided is a method for preparing an organic acid salt of a new intermediate 3-(7-cyano-5-((R)-2-((R)-1-phenylethylamino)propyl)-1-hydrogen-indolyl) propyl alcohol (ester or ether), and a new intermediate 3-(7-cyano-5-((R)-2-(((R)-1-phenethyl)(2-(2-(trifluoroethoxy)phenoxy) ethyl)amino)propyl)1-hydrogen-indolyl)propyl alcohol (ester or ether) and a salt thereof. The method has the following advantages: raw materials are cheap and easy to obtain, the operation is simple, the intermediate and product are easy to purify, the yield is high, and the method is applicable to industrial production.Type: ApplicationFiled: October 20, 2014Publication date: October 20, 2016Inventors: Hong GU, Jian CAO, Liushan CHEN, Luning HUANG
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Publication number: 20160304453Abstract: The present disclosure describes a method to treat conditions, including bacterial infections and cancer, using a photosensitive compound that, upon exposure to white light, can be activated. The photosensitive compound can also interact synergistically with antibiotics used concomitantly to kill drug-resistant bacteria. The photosensitive compounds can also be used to inhibit the proliferation of cancer cells.Type: ApplicationFiled: April 20, 2016Publication date: October 20, 2016Inventors: Snezna ROGELJ, Liliya FROLOVA, Alexander KORNIENKO, Leslie D. EDWARDS, Cody CHAMPION, Kailee ZINGLER
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Publication number: 20160304454Abstract: The invention relates to a process to produce phthalimides by heating diammonium phthalate in the presence of aromatic solvents and to a process to produce phthalimides by heating diammonium phthalate in the presence of aromatic solvents for their recycled use during the on exchanger production process. The diammonium phthalate is prepared by making use of the phthalic add salts solution resulted from the on exchanger production process.Type: ApplicationFiled: December 19, 2014Publication date: October 20, 2016Inventors: Wolfgang ZARGES, Georg MARTIN, Uwe BOEGER, Michael PIES, Guido ISSLING, Markus KOSCHORRECK
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Publication number: 20160304455Abstract: The invention relates to a novel process for the preparation of rac-6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide (I) in pharmaceutically acceptable polymorphic form, through the conversion of a 3-bromo-2-oxo-cyclohexanecarboxylic acid alkyl ester into 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxylic acid alkyl ester, which in turn is processed to yield the final product.Type: ApplicationFiled: April 20, 2016Publication date: October 20, 2016Inventors: Enrica DIODATO, Katia MARCUCCI, Russell THOMAS, Paul WIEDENAU, Martin RETTIG, Huw ROBERTS
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Publication number: 20160304456Abstract: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6 and HDAC11, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.Type: ApplicationFiled: April 15, 2016Publication date: October 20, 2016Inventors: Pui Yee Ng, Heather Davis, Kenneth W. Bair, Aleksandra Rudnitskaya, Xiaozhang Zheng, Bingsong Han, Nicholas Barczak, David R. Lancia, JR.
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Publication number: 20160304457Abstract: Provided is a method for preparing a structure directing agent (SDA) for crystalline molecular sieve synthesis comprising the steps of (a) hydrolyzing analkyl sulfate counterion of a quaternary ammonium salt to produce an organic ammonium salt having a hydrogen sulfate counterion; and (b) contacting the organic ammonium salt having the hydrogen sulfate counterion with a source of hydroxide in solution to form an organic ammonium salt having a hydroxide counterion; wherein the organic ammonium salt is a structure directing agent (SDA) for crystalline molecular sieve synthesis.Type: ApplicationFiled: April 20, 2016Publication date: October 20, 2016Inventors: Steven COLLIER, Da-Ming GOU, Jeremy WILT
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Publication number: 20160304458Abstract: Process for the preparation of intermediates useful in the synthesis of miglustat and their use in its manufacture.Type: ApplicationFiled: April 14, 2016Publication date: October 20, 2016Applicant: DIPHARMA FRANCIS s.r.l.Inventors: Andrea MALVESTITI, Enrico BRUNOLDI, Emanuele ATTOLINO
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Publication number: 20160304459Abstract: [Problems] To provide a novel peptide synthesis technique that is completely different than heretofore, and to provide a novel compound that enables the synthesis/creation of a novel artificial functional protein and the synthesis/creation of a novel functional peptide, as well as a method for producing the same. [Solution] A compound represented by formula (I) or a salt thereof.Type: ApplicationFiled: October 2, 2014Publication date: October 20, 2016Applicants: TOKYO UNIVERSITY OF PHARMACY & LIFE SCIENCES, KOKUSAN CHEMICAL CO., LTD.Inventors: Yoshio HAYASHI, Akihiro KAJIYAMA, Akihiro TAGUCHI, Kentarou FUKUMOTO
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Publication number: 20160304460Abstract: The present invention relates to novel oxodihydropyridinecarbohydrazide derivatives with excellent antifungal activities, an antifungal composition containing the same, and its use for the prevention and treatment of fungal infectious diseases. The oxodihydropyridinecarbohydrazide derivatives of the present invention have excellent antifungal and fungicidal activities, and thus will be useful for the prevention and treatment of various fungal infections by Candida spp., Aspergillus spp., Cryptococcus neoformans and Trichophyton spp., etc. Additionally, the oxodihydropyridinecarbohydrazide derivatives of the present invention, unlike other fungicidal preparations, can be orally administered.Type: ApplicationFiled: October 21, 2014Publication date: October 20, 2016Applicant: DAEWOONG PHARMACEUTICAL CO., LTD.Inventors: Joon Seok Park, Youn Jung Yoon, Chang Min Park, Yun Soo Na, Min Jae Cho, Ho Bin Lee, Mi Ryeong Han, Yeon Jung Park, Ji Duck Kim
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Publication number: 20160304461Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.Type: ApplicationFiled: June 27, 2016Publication date: October 20, 2016Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Yuji OCHI, Masami NAKAI, Atsushi MORI
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Publication number: 20160304462Abstract: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.Type: ApplicationFiled: April 15, 2016Publication date: October 20, 2016Inventors: Pui Yee Ng, Heather Davis, Kenneth W. Bair, David S. Millan, Aleksandra Rudnitskaya, Xiaozhang Zheng, Bingsong Han, Nicholas Barczak, David R. Lancia, JR.
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Publication number: 20160304463Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: April 25, 2016Publication date: October 20, 2016Inventors: Bradley Teegarden, Yifeng Xiong, Sonja Strah-Pleynet, Honnappa Jayakumar, Peter I. Dosa, Konrad Feichtinger, Martin Casper, Juerg Lehmann, Robert M. Jones, David J. Unett, Jin Sun Karoline Choi
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Publication number: 20160304464Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: December 10, 2014Publication date: October 20, 2016Inventors: Thomas D. Aicher, Donald J. Skalitzky, Clarke B. Taylor
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Publication number: 20160304465Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: December 10, 2014Publication date: October 20, 2016Inventors: Donald J. Skalitzky, Chad A. VanHuis
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Publication number: 20160304466Abstract: The present invention is directed to modulators, such as inhibitors, of JNK isoform 2 (JNK2) or isoform 3 (JNK3) comprising compounds of formula (I) or formula (II) as described herein. Compounds of the invention can be used for treatment of a medical disorder in a patient wherein modulation of JNK3 is medically indicated, such as when the disorder is Parkinson disease (PD) Alzheimer's disease (AD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), myocardial infarction (MI), glaucoma, obesity, diabetes, cancer, rheumatoid arthritis, fibrotic disease, pulmonary fibrosis, kidney disease, liver inflammation, Crohns disease, hearing loss, Prader Willi syndrome, or a condition where modification of feeding behavior is medically indicated.Type: ApplicationFiled: December 3, 2014Publication date: October 20, 2016Inventors: Yangbo Feng, Philip Lograsso, Ke Zheng, Chul Min Park
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Publication number: 20160304467Abstract: An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2, 6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.Type: ApplicationFiled: June 29, 2016Publication date: October 20, 2016Applicant: ADAMA MAKHTESHIM LTD.Inventors: Anat Levin, Michael Grabarnick
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Publication number: 20160304468Abstract: The present invention relates to process for the preparation of 7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-(3R,5S)-dihydroxy-(E)-6-heptenoic acid calcium having formula (I). The compound of formula (I) has adopted name “Rosuvastatin Calcium”. The present invention is also related to novel intermediates of formula (4) and formula (5) used in preparation of formula (I), and process of their preparation.Type: ApplicationFiled: November 18, 2013Publication date: October 20, 2016Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Udaya Bhaskara Rao SIRIPALLI, Veera Reddy ARAVA, Rajendiran CHINNAPILLAI, Anji Reddy MIDDEKADI, Naresh Raju MAKARAJU, Venkateswarlu JASTI
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Publication number: 20160304469Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.Type: ApplicationFiled: June 24, 2016Publication date: October 20, 2016Applicant: Pfizer Inc.Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
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Publication number: 20160304470Abstract: A series of substituted heteroaromatic compounds containing two fused six-membered rings, tivity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: ApplicationFiled: December 8, 2014Publication date: October 20, 2016Inventors: Rikki Peter Alexander, Gregory Foulkes, Martin Clive Hutchings, Victoria Elizabeth Jackson, Boris Kroeplien, James Thomas Reuberson, Sarah Margaret Rook, Zhaoning Zhu
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Publication number: 20160304471Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.Type: ApplicationFiled: February 16, 2016Publication date: October 20, 2016Inventors: Xiangping Qian, Yong-Liang Zhu
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Publication number: 20160304472Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.Type: ApplicationFiled: November 13, 2015Publication date: October 20, 2016Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
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Publication number: 20160304473Abstract: The present application is directed to excimer forming compounds of Formula I: W—V—[Y]n wherein W is an excimer forming fluorophore, V is a linker moiety, Y is a metal ion coordinating moiety and n is 1, 2 or 3. In particular, the application is directed to excimer forming compounds for the detection of proximally phosphorylated sites including those found on polypeptides, proteins, pyrophosphate and RNA, for example in aqueous solution, polyacrylamide gels blotting membranes, solid-support assays and in cell culture samples.Type: ApplicationFiled: December 19, 2014Publication date: October 20, 2016Inventors: Patrick Thomas Gunning, Dziyana Kraskouskaya
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Publication number: 20160304474Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.Type: ApplicationFiled: May 19, 2016Publication date: October 20, 2016Inventor: Gary David Annis
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Publication number: 20160304475Abstract: Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.Type: ApplicationFiled: June 24, 2016Publication date: October 20, 2016Applicant: Supernus Pharmaceuticals, Inc.Inventors: Likan LIANG, Padmanabh P. BHATT, David DAIN, Jean-Philippe TAQUET, Aleksandr PECHENOV, Alexei TCHESNOKOV, Reynold MARIAUX
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Publication number: 20160304476Abstract: The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.Type: ApplicationFiled: December 19, 2014Publication date: October 20, 2016Inventors: Thomas D. Aicher, Chad A. VanHuis, William D. Thomas, John K. MacLean, Brian M. Andresen, Kenneth J. Barr, Corey E. Bienstock, Neville J. Anthony, Matthew Daniels, Kun Liu, Yuan Liu, Catherine M. White, Blair T. Lapointe, Nunzio Sciammetta, Vladimir Simov
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Publication number: 20160304477Abstract: Disclosed embodiments are related to pharmaceutical compositions comprising novel piperazine compounds and methods of administration of the same to a patient for termination acute episodes of cardiac arrhythmias, maintaining normal sinus rhythm, restoring normal sinus rhythm, and preventing recurrence of cardiac arrhythmia.Type: ApplicationFiled: April 25, 2014Publication date: October 20, 2016Inventor: Arthur M. Brown
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Publication number: 20160304478Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.Type: ApplicationFiled: June 29, 2016Publication date: October 20, 2016Inventors: Veronique BIRAULT, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
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Publication number: 20160304479Abstract: A process for preparing furanic mono- and/or di-sulfonate molecules from the reduction products of HMF, in particular, from either 2,5-bis-hydroxymethyltetrahydrofurans (THF-diols) or furan-2,5-dimethanol (FDM) under relatively mild conditions is described. The process involves reacting THF-diols or FDM with at least a sulfonate species, and a reagent of either 1) a nucleophilic base or 2) combination of a non-nucleophilic base and a nucleophile, as two separate reagents. The furanic sulfonates synthesized according to the process and some of the associated compounds that can be derivatized from the sulfonates are also provided.Type: ApplicationFiled: December 12, 2014Publication date: October 20, 2016Inventor: Kenneth Stensrud
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Publication number: 20160304480Abstract: The present invention relates to a method for preparing for a furan derivative from biomass, comprising step (1) of preparing 5-hydroxymethylfurfural by reacting biomass and a solid acid catalyst in butanol; and step (2) of preparing a furan derivative by reacting the butanol solution of 5-hydroxymethylfurfural, obtained in step (1), with a hydrogenation catalyst.Type: ApplicationFiled: April 14, 2016Publication date: October 20, 2016Inventors: Dong Won HWANG, Pravin P. UPARE, Jong San CHANG, Young Kyu HWANG, U Hwang LEE, Do Young HONG
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Publication number: 20160304481Abstract: Described is a method for producing furfural from one or more substances selected from the group consisting of xylose, oligosaccharides comprising xylose units and polysaccha-rides comprising xylose units.Type: ApplicationFiled: December 10, 2014Publication date: October 20, 2016Inventors: Stefan Koch, Alois Kindler
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Publication number: 20160304482Abstract: An object of the present invention is to provide a method for suppressing the corrosion of a reactor and reducing waste in the production of 2-furaldehyde from a sugar raw material containing a hexose as a constituent component, and another object of the invention is to provide an industrially advantageous method for producing 2-furaldehyde, which suppresses a decrease in the activity of a catalyst in a case of using an acid catalyst and provides a higher yield. The present invention relates to a method for producing 2-furaldehyde comprising heating a sugar raw material containing a hexose as a constituent component in an aprotic polar solvent in the presence of a solid acid catalyst.Type: ApplicationFiled: June 27, 2016Publication date: October 20, 2016Applicant: MITSUBISHI CHEMICAL CORPORATIONInventors: Toru OKOSHI, Hideto TSUJI
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Publication number: 20160304483Abstract: The present invention provides new therapeutic compounds for treatment of diseases caused or influenced by microtubule stability, such as proliferative diseases. The compounds are phenyl-analogs of the naturally occurring peloruside. The analogs are easier to synthesize, and hence open up the possibility to produce said compounds in large quantities for therapeutic use.Type: ApplicationFiled: November 28, 2014Publication date: October 20, 2016Inventors: Johan Van Der Eycken, Gert Smans, Jelle Cornelus, Dries Van Den Bossche, Nick Jacobs
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Publication number: 20160304484Abstract: The present invention discloses an improved oxidation process using carbon nitride nanotubes as metal free catalyst and molecular O2 as the oxidant to obtain desired adipic acid and other oxygenated hydrocarbons with improved conversion and selectivity.Type: ApplicationFiled: December 2, 2014Publication date: October 20, 2016Applicant: Council of Scientific and Industrial ResearchInventors: Satyanarayana Vera Venkata Chilukuri, Narasimharao Kanna, Lakshmiprasad Gurrala
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Publication number: 20160304485Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having benzoic acid structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: April 20, 2016Publication date: October 20, 2016Inventors: Zaneta Nikolovska-Coleska, Jeanne A. Stuckey, Ahmed Mady, Lei Miao
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Publication number: 20160304486Abstract: This invention relates to indoline compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.Type: ApplicationFiled: June 30, 2016Publication date: October 20, 2016Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lina Yin, Rolf Hartmann, Qingzhong Hu, Ralf Heim, Christina Zimmer
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Publication number: 20160304487Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.Type: ApplicationFiled: July 1, 2016Publication date: October 20, 2016Inventors: Takeshi KUBOYAMA, Tomohiro ERA, Tomoyuki NAOI
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Publication number: 20160304488Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: November 13, 2015Publication date: October 20, 2016Inventors: John Hood, Sunil Kumar KC
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Publication number: 20160304489Abstract: The present invention relates to particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, to a process of making said particles, to pharmaceutical compositions comprising said particles and to method of treating cancers using said pharmaceutical compositions.Type: ApplicationFiled: March 18, 2016Publication date: October 20, 2016Applicant: NOVARTIS AGInventors: Nicole BUSCHMANN, Robin Alec FAIRHURST, Pascal FURET, Bo HAN, Thomas KNÖPFEL, Catherine LEBLANC, Lv LIAO, Robert MAH, Franck MALLET, Julie MARTZ, Can WANG, Jing XIONG, Xianglin ZHAO
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Publication number: 20160304490Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: December 4, 2014Publication date: October 20, 2016Applicant: MERCK SHARP & DOHME CORP.Inventors: SCOTT D. KUDUK, JASON W. SKUDLAREK
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Publication number: 20160304491Abstract: The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.Type: ApplicationFiled: December 16, 2014Publication date: October 20, 2016Applicant: Bayer Pharma AktiengesellschaftInventors: Eva Maria BECKER-PELSTER, Philipp BUCHGRABER, Anja BUCHMÜLLER, Karen ENGEL, Volker GEISS, Andreas GÖLLER, Herbert HIMMEL, Raimund KAST, Andreas KNORR, Dieter LANG, Gorden REDLICH, Carsten SCHMECK, Hanna TINEL, Frank WUNDER
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Publication number: 20160304492Abstract: The invention relates to novel substituted bipiperidinyl derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.Type: ApplicationFiled: December 16, 2014Publication date: October 20, 2016Applicant: Bayer Pharma AktiengesellschaftInventors: Eva Maria BECKER-PELSTER, Philipp BUCHGRABER, Anja BUCHMÜLLER, Karen ENGEL, Andreas GÖLLER, Herbert HIMMEL, Raimund KAST, Joerg KELDENICH, Carsten SCHMECK, Hanna TINEL, Frank WUNDER
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Publication number: 20160304493Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: June 24, 2016Publication date: October 20, 2016Inventors: Ian Collins, Michael Lainchbury, Thomas Peter Matthews, John Charles Reader
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Publication number: 20160304494Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.Type: ApplicationFiled: June 29, 2016Publication date: October 20, 2016Inventors: Brian T. Hopkins, Timothy R. Chan, Tracy J. Jenkins, Patrick Conlon, Xiongwei Cai, Michael Humora, Xianglin Shi, Ross A. Miller, Andrew Thompson
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Publication number: 20160304495Abstract: Monocyclic pyrimidine and pyridine compounds having a benzyl amine substituent at the 4 position and a 5:6 bicyclic heteroaryl substituent at the 2 position of the pyrimidine or pyridine ring as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the ring are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.Type: ApplicationFiled: December 10, 2014Publication date: October 20, 2016Applicant: Cleave Biosciences, Inc.Inventors: David Wustrow, Han-Jie Zhou
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Publication number: 20160304496Abstract: The disclosure provides indazolone compounds, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the disclosure may be useful for treating immunological and oncological conditions.Type: ApplicationFiled: April 15, 2016Publication date: October 20, 2016Inventors: Maria Argiriadi, Eric Breinlinger, Justin D. Dietrich, Michael Friedman, David Ihle, Michael Morytko, Kelly Mullen, Augustine Osuma, Glora Y. Lo Schiavo, Noel S. Wilson
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Publication number: 20160304497Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: December 10, 2014Publication date: October 20, 2016Inventors: Romyr Dominique, Norman Kong, Yan Lou, Francisco Javier Lopez-Tapia, Sung-Sau So
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Publication number: 20160304498Abstract: A compound having the following structure (I): or a pharmaceutically acceptable salt, prodrug, stereoisomer or tautomer thereof, is provided. Related compounds, methods for preparation of the same and uses of the compounds for treatment of various indications, including treatment of necrotic cell diseases and/or inflammation, are also provided.Type: ApplicationFiled: June 27, 2016Publication date: October 20, 2016Inventors: Junying Yuan, Yijun Zhou, Shan Qian, Dawei Ma
