Patents Issued in November 17, 2016
  • Publication number: 20160332949
    Abstract: The invention relates to a method for producing a (meth)acrylic anhydride A-C(?O)—O—(O?)C-A, comprising the following steps: a) a step of reacting an anhydride B—C(?O)—O—(O?)C—B with an acid A-COOH, resulting in the formation of mixed anhydride A-C(?O)—O—(O?)C—B and acid B—COOH; and b) a step of reacting the mixed anhydride with A-COOH, resulting in the (meth)acrylic anhydride. According to the invention, reaction steps (a) and (b) are carried out in the presence of hydrated triflic acid, and the anhydride A-C(?O)—O—(O?)C-A is isolated from the reaction medium produced in step (b) as follows: e1) heavy compounds having a volatility less than or equal to that of the anhydride A-C(?O)—O—(O?)C-A are separated from the reaction medium, said compounds including the anhydride and the hydrated triflic acid; e2) the anhydride is separated from the heavy compounds by difference in volatility.
    Type: Application
    Filed: January 20, 2015
    Publication date: November 17, 2016
    Inventors: Pierre ARDAUD, Thierry VIDAL, Rabih RACHED
  • Publication number: 20160332950
    Abstract: The disclosures herein provide compounds of Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI and Formula VII or its pharmaceutical acceptable compositions and salts, as well as polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. The pharmaceutical compositions may be formulated for oral administration, delayed release or sustained release, transmucosal, syrup, topical, parenteral administration, injection, subdermal, oral solution, rectal administration, nanoparticle, buccal administration or transdermal administration. Such compositions may be used to treatment of urea cycle disorders and gout or its associated complications.
    Type: Application
    Filed: November 11, 2015
    Publication date: November 17, 2016
    Inventor: Mohan Murali Alapati
  • Publication number: 20160332951
    Abstract: A perfluorovinyloxy polyether carboxylic acid alkali metal salt represented by the general formula is provided: CF2?CF[OCF2CF(CF3)]bO(CF2)aO[CF(CF3)CF2O]cCF(CF3)COOM??[I], wherein M is alkali metal, preferably sodium or potassium, a is an integer of 1 to 6, preferably 2, and b+c is an integer of 0 to 6, preferably 0 or 1. This perfluorovinyloxy polyether carboxylic acid alkali metal salt is produced by subjecting a perfluorovinyloxy polyether carboxylic acid alkyl ester represented by the general formula: CF2?CF[OCF2CF(CF3)]bO(CF2)aO[CF(CF3)CF2O]cCF(CF3)COOR??[II], wherein R is an alkyl group having 1 to 12 carbon atoms, a is an integer of 1 to 6, and b+c is an integer of 0 to 6; to hydrolysis or solvolysis in the presence of an alkali metal hydroxide.
    Type: Application
    Filed: December 19, 2014
    Publication date: November 17, 2016
    Inventors: Keisuke Kokin, Mitsuru Maeda, Daisuke Murai
  • Publication number: 20160332952
    Abstract: The invention relates to terpene-derived acids and esters thereof as well as to processes for synthesizing them.
    Type: Application
    Filed: January 13, 2015
    Publication date: November 17, 2016
    Inventors: Patrick FOLEY, Yonghua YANG, Robert BEDOUKIAN, Thomas KILLINGER
  • Publication number: 20160332953
    Abstract: A process for vapor-phase methanol carbonylation to methyl formate, a supported nano-scaled platinum group metal heterogeneous catalyst used in said process and a method for preparing said catalyst are disclosed. A feed gas containing methanol, carbon monoxide, hydrogen and oxygen is passed through a reactor loaded with supported nano-scaled platinum group metal heterogeneous catalyst to produce methyl formate by vapor-phase carbonylation reaction, in the reaction conditions with a space velocity of 500-5000 h?1, a temperature of 50-150° C. and a pressure of 0.01-2 MPa. The active component of the supported nano-scaled platinum group metal heterogeneous catalyst is platinum group metal with a particle size of 0.5-10 nm.
    Type: Application
    Filed: June 12, 2014
    Publication date: November 17, 2016
    Applicant: FUJIAN INSTITUTE OF RESEARCH ON THE STRUCTURE OF MATTER, CHINESE ACADEMY OF SCIENCES
    Inventors: Zhongning Xu, Guocong Guo, Siyan Peng, Zhiqiao Wang, Qingsong Chen, Mingsheng Wang, Yuangen Yao
  • Publication number: 20160332954
    Abstract: Esters or salts of 2-hydroxy-4-propyleyclohepta-2,4,6-trienone, and applications thereof in preparation of animal antibacterial agents and growth promoters used in feed. The esters or salts of 2-hydroxy-4-propylcyclohepta-2,4,6-trienone has a structural formula as shown in formula 1 or 2: in formula 1, R1 represents heptadecyl; and in formula 2, L is sodium, potassium, calcium, magnesium, zinc, copper or manganese. The esters or salts of 2-hydroxy-4-propyleyclohepta-2,4,6-trienone, as shown in formula 1 or 2, have high stability and safety, and good antibacterial and growth promotion effects, which make them preferable to be used as animal antibacterial agents and growth promoters in feed, and have a very good application prospect in the cultivation industry.
    Type: Application
    Filed: February 17, 2014
    Publication date: November 17, 2016
    Applicant: GUANGZHOU INSIGHTER BIOTECHNOLOGY CO., LTD.
    Inventors: Xianfeng PENG, Zonghua QIN, Fang LI, Jijun HUANG, Xiaolan YE, Zaolong LI
  • Publication number: 20160332955
    Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms, treatments, or sequelae of disease. The phorbol esters described are particularly useful in the treatment of neoplastic diseases and/or managing the side effects of chemotherapeutic and radiotherapeutic treatments of neoplastic diseases.
    Type: Application
    Filed: September 12, 2013
    Publication date: November 17, 2016
    Applicant: Biosuccess Biotech Co. Ltd.
    Inventors: Zheng Tao Han, Hung-Fong Chen
  • Publication number: 20160332956
    Abstract: Position-1 halogen can be selectively reduced by reacting a compound represented by formula (3): [wherein X represents a chlorine atom, a bromine atom, or an iodine atom] with halogen in the presence of a heterogeneous transition metal catalyst to produce 2-(halogenomethyl)-1-methyl-3-nitrobenzene represented by formula (1): [wherein the symbol is as defined above].
    Type: Application
    Filed: February 16, 2015
    Publication date: November 17, 2016
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Satoru Ujita, Takashi Miyamoto
  • Publication number: 20160332957
    Abstract: A process for purifying linear a-olefins, comprises: providing an organic phase comprising a linear a-olefin; providing an alkaline aqueous phase I; providing an amine; mixing the linear a-olefin, alkaline aqueous phase I, and amine; separating the aqueous phase I from the organic phase; adding water to the organic phase thereby forming an aqueous phase II; bringing into contact the organic phase with carbon dioxide; separating the aqueous phase II which comprises a solid formed in the organic phase when contacted with carbon dioxide; wherein the purified linear a-olefins are obtained in the organic phase.
    Type: Application
    Filed: January 19, 2015
    Publication date: November 17, 2016
    Inventors: Syed Azhar Hashmi, Mohammed H. Al-Hazmi, Shahid Azam
  • Publication number: 20160332958
    Abstract: The present invention provides a novel method for preparing lacosamide with high chiral purity from D-serine. The method of the present invention can obtain lacosamide with high chiral purity in a high yield through a simple and environmentally-friendly process and thus can be easily applied to mass production.
    Type: Application
    Filed: October 27, 2014
    Publication date: November 17, 2016
    Inventors: Geun Jho LIM, Sun Ki CHANG, Jae Hun KIM, Jong Moon PARK
  • Publication number: 20160332959
    Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R2?, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urolological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    Type: Application
    Filed: July 27, 2016
    Publication date: November 17, 2016
    Inventor: Paolo Pevarello
  • Publication number: 20160332960
    Abstract: The present invention relates to a novel ?-oximester fluorene derivative compound, a photopolymerization initiator comprising the same, and a photoresist composition.
    Type: Application
    Filed: January 19, 2015
    Publication date: November 17, 2016
    Applicants: SAMYANG CORPORATION, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Chun-Rim OH, Min-Sun LEE, Won-Jung LEE, Yong-Il CHO, Seung-Rim SHIN, Jong-Il SHIN, Sang-Oh LEE, Kun JUN
  • Publication number: 20160332961
    Abstract: The present invention provides a method for producing a high-quality internal olefin sulfonate in which the content of any internal olefin and inorganic substance is small. This method for producing an internal olefin sulfonate, comprising: a sulfonating step of causing an internal olefin to react with sulfur trioxide to yield a sulfonated internal olefin; a neutralizing step of mixing the resultant sulfonated internal olefin with an aqueous alkaline solution at 40° C. or lower to yield a mixture, and applying shearing force to the mixture until the particle diameter of oil droplets of an oily product of the mixture turns to 10 ?m or less to yield a neutralized product; and a hydrolyzing step of hydrolyzing the resultant neutralized product.
    Type: Application
    Filed: November 27, 2014
    Publication date: November 17, 2016
    Applicant: KAO CORPORATION
    Inventors: Hiroshi HORI, Yohei YOSHIKAWA, Yoshinori MITSUDA, Toku FUJIOKA, Yoshifumi NISHIMOTO
  • Publication number: 20160332962
    Abstract: The present invention is directed to processes for the preparation of esketamine. The present invention is further directed to processes for the resolution of S-ketamine from a racemic or enantiomerically enriched mixture of ketamine. The present invention is further directed to an (S)-CSA salt of S-ketamine, more particularly a monohydrate form of the (S)-CSA salt of S-ketamine, and to an (R)-CSA salt of R-ketamine.
    Type: Application
    Filed: May 12, 2016
    Publication date: November 17, 2016
    Applicant: Janssen Pharmaceutica NV
    Inventors: Cheng Yi Chen, Oliver Floegel, Michael Justus, Adrian Maurer, Karl Reuter, Tobias Strittmatter, Tobias Wedel
  • Publication number: 20160332963
    Abstract: A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of
    Type: Application
    Filed: January 21, 2015
    Publication date: November 17, 2016
    Inventors: Klaus Thirring, Werner Heilmayer, Rosemarie Riedl, Hermann Kollmann, Zrinka Ivezic-Schoenfeld, Wolfgang Wicha, Susanne Paukner, Dirk Strickmann
  • Publication number: 20160332964
    Abstract: According to the present invention, there can be provided A process for producing 7-dehydrocholesterol (hereinafter, “7DHC”), comprising culturing, in a medium, a 7DHC-producing Labyrinthulea microorganism in which the 7DHC reducing activity is reduced or lost as compared to a parent strain through deletion, substitution, or addition of at least one base in a gene which is present in the chromosomal DNA of the parent strain and encodes a protein having 7DHC reducing activity, and the microorganism produces 7DHC, allowing 7DHC to be produced and accumulated in the culture, and collecting the 7DHC from the culture; and a process for producing vitamin D3, comprising irradiating, with ultraviolet light, the 7DHC produced by the production process.
    Type: Application
    Filed: January 14, 2015
    Publication date: November 17, 2016
    Inventors: Tetsuro Ujihara, Satoshi Mitsuhashi
  • Publication number: 20160332965
    Abstract: Processes for annealing amorphous atorvastatin is described. Pharmaceutical compositions and formulations containing annealed amorphous atorvastatin are also described.
    Type: Application
    Filed: July 27, 2016
    Publication date: November 17, 2016
    Inventors: Renuka Devi Reddy, Evgenyi Shalaev, Ravi Mysore Shanker, Carl Bernard Ziegler
  • Publication number: 20160332966
    Abstract: [Problem] To provide a compound useful as a MT1 and/or MT2 receptor agonist. [Solution] The present inventors have studied on MT1 and/or MT2 receptor agonists, and have confirmed that indole compounds have the activity. As a result, the present invention is accomplished. That is, a compound represented by formula (I) or a salt thereof according to the present invention has a MT1 and/or MT2 receptor agonistic activity and has a low ability of migrating into central nervous system. Therefore, the compound or a salt thereof can be used as a peripheral MT1 and/or MT2 receptor agonist, and therefore can be used as a therapeutic and/or prophylactic agent for urinary incontinence, particularly stress urinary incontinence and mixed urinary incontinence.
    Type: Application
    Filed: January 13, 2015
    Publication date: November 17, 2016
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shunichiro MATSUMOTO, Takafumi SHIMIZU, Tomoyuki SAITO, Takatoshi KANAYAMA, Hiroaki TANAKA, Chiharu MORI, Kazuhiro YOKOYAMA, Shigeo MATSUI
  • Publication number: 20160332967
    Abstract: This invention relates to crystalline forms of (R)-1-(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)indoline-5-carbonitrile, a modulator of the androgen receptor, and methods for the use in treatment.
    Type: Application
    Filed: January 20, 2015
    Publication date: November 17, 2016
    Inventors: Istvan KALDOR, Dalin TANG
  • Publication number: 20160332968
    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: February 3, 2015
    Publication date: November 17, 2016
    Inventors: Harry Chobanian, Duane DeMong, Yan Guo, Zhiyong Hu, Michael Miller, Barbara Pio, Christopher W. Plummer, Dong Xiao, Michael Yang
  • Publication number: 20160332969
    Abstract: The present invention relates to substituted benzene 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: May 23, 2016
    Publication date: November 17, 2016
    Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah K. Knutson, Timothy J. N. Wigle, Masashi Seki
  • Publication number: 20160332970
    Abstract: The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: July 26, 2016
    Publication date: November 17, 2016
    Inventors: Amogh Boloor, Young K. Chen, Michael Brennan Wallace
  • Publication number: 20160332971
    Abstract: Arylquinoline derivatives and their use for treating cancer or cancer metastasis is disclosed. The compounds of the subject technology promote cells to secrete a pro-apoptotic tumor suppressor, i.e., prostate apoptosis response-4 (Par-4), which in turn promote apoptosis in cancer cells or metastatic cells.
    Type: Application
    Filed: May 11, 2016
    Publication date: November 17, 2016
    Inventors: David S. WATT, Chunming LIU, Vivek M. RANGNEKAR, Vitaliy M. SVIRIPA, Ravshan BURIKHANOV, Wen ZHANG
  • Publication number: 20160332972
    Abstract: The present invention relates to urea hydantoin compounds, processes for preparing them, pharmaceutical compositions containing them, and their use as pharmaceuticals as modulators of the FPR2 receptor, and to methods of treating inflammatory diseases or conditions in a subject in need thereof by administering the compound(s) or pharmaceutical composition to the subject.
    Type: Application
    Filed: January 27, 2015
    Publication date: November 17, 2016
    Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Huy Vu, Michael E. Garst
  • Publication number: 20160332973
    Abstract: This disclosure is directed to: (a) processes for preparing compounds and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compounds and salts; (c) pharmaceutical compositions comprising the compounds or salts; and (d) methods of use of such compositions.
    Type: Application
    Filed: July 27, 2016
    Publication date: November 17, 2016
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Publication number: 20160332974
    Abstract: The present invention provides, inter alia, compounds having the structure of formula (I): Compositions containing such compounds are also provided. Methods for using such compounds or compositions for treating or ameliorating the effects of a cancer having a cell that harbors an oncogenic RAS mutation, for modulating a lipoxygenase in a ferroptosis cell death pathway, and for depleting reduced glutathione (GSH) in a cell harboring an oncogenic RAS mutation are further provided.
    Type: Application
    Filed: January 14, 2015
    Publication date: November 17, 2016
    Inventors: Brent R. Stockwell, Wan Seok Yang, Marie-Helene Larraufie
  • Publication number: 20160332975
    Abstract: This invention relates to methods for controlling parasitic infestations of animals and their environments, and, more particularly, to methods using isoxazolines to control parasites in or on animals or in their environments, as well as treat parasitoses of animals. The isoxazolines include 4-(isoxazolinyl)-benzamides (specifically, substituted 4-(5-(halomethyl)-5-phenyl-isoxazolin-3-yl)-benzamides) and 4-(isoxazolinyl)-benzothioamides (specifically, substituted 4-(5-(halomethyl)-5-phenyl-isoxazolin-3-yl)-benzothioamides). This invention also relates to compositions comprising the isoxazolines for use in such methods, the use of the isoxazolines to make medicaments for use in such methods, and kits comprising the isoxazolines for carrying out such methods. This invention further relates to the use of the isoxazolines as medicaments, particularly medicaments that can be used in the above-referenced method.
    Type: Application
    Filed: July 28, 2016
    Publication date: November 17, 2016
    Applicant: Intervet Inc.
    Inventors: Anja Regina Heckeroth, Jürgen Lutz, Christina Mertens, Heike Williams, Hartmut Zoller, Takeshi Mita
  • Publication number: 20160332976
    Abstract: The present disclosure provides processes for the preparation of a compound of formula: which is a selective late sodium current inhibitor. The disclosure also provides compounds that are synthetic intermediates.
    Type: Application
    Filed: May 2, 2016
    Publication date: November 17, 2016
    Inventors: Anna Chiu, Yanshu Feng, Hanrong Gao, James A. Kerschen, John Reichwein, Keshab Sarma, Andrew S. Thompson, Xinjun Zhao
  • Publication number: 20160332977
    Abstract: The present disclosure provides processes for the preparation of a compound of formula: which is a selective late sodium current inhibitor. The disclosure also provides compounds that are synthetic intermediates.
    Type: Application
    Filed: May 2, 2016
    Publication date: November 17, 2016
    Inventors: Anna Chiu, Yanshu Feng, Hanrong Gao, James A. Kerschen, John Reichwein, Keshab Sarma, Andrew S. Thompson, Xinjun Zhao
  • Publication number: 20160332978
    Abstract: Disclosed is a process for making HMF or a derivative of HMF by dehydrating one or more hexose sugars in a reduced oxygen environment. In another, related aspect, a method for improving the stability and resistance to degradation of an HMF product involves adding one or more antioxidants to the HMF product.
    Type: Application
    Filed: July 19, 2016
    Publication date: November 17, 2016
    Inventors: Alexandra Sanborn, Erik Hagberg, Stephen Howard, Erin M. Rockafellow
  • Publication number: 20160332979
    Abstract: Disclosed is an oxidation process to produce a crude carboxylic acid product carboxylic acid product. The process comprises oxidizing a feed stream comprising at least one oxidizable compound to generate a crude carboxylic acid slurry comprising furan-2,5-dicarboxylic acid (FDCA) and compositions thereof. Also disclosed is a process to produce a dry purified carboxylic acid product by utilizing various purification methods on the crude carboxylic acid.
    Type: Application
    Filed: July 22, 2016
    Publication date: November 17, 2016
    Applicant: EASTMAN CHEMICAL COMPANY
    Inventors: Kevin John Fontenot, Mesfin Ejerssa Janka, Kenny Randolph Parker, Ashfaq Shahanawaz Shaikh, Lee Reynolds Partin, Charles Edwan Sumner, JR., Shane Kipley Kirk, Paula Moody, Bradford Russell Bowers, Michael Charles Morrow
  • Publication number: 20160332980
    Abstract: The present invention relates to a novel 2-phenylbenzofuran derivative or a pharmaceutically acceptable salt thereof, a production method for the same, and a pharmaceutical composition for preventing or treating an inflammatory disease comprising the same as an active ingredient, and the novel 2-phenylbenzofuran derivative or the pharmaceutically acceptable salt thereof according to the present invention is outstandingly effective in suppressing NO, IL-6, and TNF-alpha induced by macrophages, and therefore can advantageously be used in a pharmaceutical composition for preventing or treating an inflammatory disease.
    Type: Application
    Filed: July 27, 2016
    Publication date: November 17, 2016
    Applicants: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY, DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION
    Inventors: Kyeong LEE, Sei-Ryang OH, Kyung Seop AHN, Ok-Kyoung KWON, Doo-Young KIM, Hyung Won RYU, Jung Hee KIM, Xuezhen XU
  • Publication number: 20160332981
    Abstract: Isoflavonoids or pharmaceutically acceptable salts thereof or pharmaceutically acceptable compositions thereof for the treatment of prostate cancer or for the treatment or inhibition of prostate cancer metastasis in a patient in need thereof are disclosed.
    Type: Application
    Filed: May 9, 2016
    Publication date: November 17, 2016
    Inventors: Svitlana P. BONDARENKO, Mykhaylo S. FRASINYUK, Chunming LIU, David S. WATT
  • Publication number: 20160332982
    Abstract: The invention provides compounds of formula (I) or salts thereof: wherein: A, B, C, D, W, X, Y and Z are as defined in the specification, and at least one of A, B, C, D, W, X, Y and Z is OR1; each R1 being independently H or C(?O)R2, and at least one R1 group being C(?O)R2; where each R2 is selected from: CHR3NHR4, where R4 is H and R3 is a group selected from CH3, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-3-(1H-indole), CH2CH2SCH3, CH2OH, CHOHCH3, CH2SH, CH2SeH and CH2PhpOH, wherein said R3 group can optionally be substituted by one or more groups selected from halogen, cyano, nitro, ORA or C1-C4 alkyl; or R3 and R4 together with the C and N atoms to which they are attached form a 5-membered heteroalkyl ring, wherein said heteroalkyl ring can optionally be substituted by one or more groups selected from halogen, cyano, nitro, ORA or C1-C3 alkyl, wherein RA is C1-C4 alkyl optionally substituted with one or more halogen, cyano or nitro groups.
    Type: Application
    Filed: December 23, 2014
    Publication date: November 17, 2016
    Applicant: AMAZENTIS SA
    Inventors: Christopher Lawrence RINSCH, Rune Andreas RINGOM
  • Publication number: 20160332983
    Abstract: The invention describes methods of preparation and compositions of plasticizers. The plasticizers include at least 2 alkyl ketal ester moieties and have a molecular weight of greater than 300. In one aspect, the alkyl ketal ester moieties are levulinic ester ketals. Certain compositions contain at least one of an antioxidant, a UV stabilizer, a thermal stabilizer or mixtures thereof, present in the composition from about 0.01 to about 5.0 percent by weight of the total composition.
    Type: Application
    Filed: July 29, 2016
    Publication date: November 17, 2016
    Inventors: Brian D. Mullen, Vivek Badarinarayana, Eric S. Hall, Matthew J. Tjossas, Cora M. Leibig
  • Publication number: 20160332984
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: December 28, 2015
    Publication date: November 17, 2016
    Inventors: Brian W. Metcalf, Jason R. Harris, Zhe Li, Stephen L. Gwaltney, II
  • Publication number: 20160332985
    Abstract: The present disclosure is generally directed to compounds of formula (I) which can inhibit AAKI (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAKI.
    Type: Application
    Filed: January 23, 2015
    Publication date: November 17, 2016
    Applicant: Bristol-Meyers Squibb Company
    Inventors: Richard A. Hartz, Vijay T. Ahuja, John E. Macor, Joanne J. Bronson, Bireshwar Dasgupta, Carolyn Diane Dzierba, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu
  • Publication number: 20160332986
    Abstract: This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the preparation of certain pesticides.
    Type: Application
    Filed: July 28, 2016
    Publication date: November 17, 2016
    Inventors: Xiaoyong LI, Qiang YANG, Beth LORSBACH
  • Publication number: 20160332987
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Application
    Filed: July 29, 2016
    Publication date: November 17, 2016
    Inventors: Qiang YANG, Beth LORSBACH, Gary ROTH, Noormohamed M. NIYAZ, Jeffrey NISSEN, Ronald ROSS, JR., Greg WHITEKER, Carl DeAMICIS, Kaitlyn GRAY, Yu ZHANG
  • Publication number: 20160332988
    Abstract: Provided herein herein are pentafluorosulfanyl (SF5) mefloquine derivatives, formulations, methods of making the SF5 derivatives, and uses thereof.
    Type: Application
    Filed: May 12, 2016
    Publication date: November 17, 2016
    Inventors: William R. Dolbier, JR., Oleksandr S. Kanishchev
  • Publication number: 20160332989
    Abstract: The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase.
    Type: Application
    Filed: December 30, 2014
    Publication date: November 17, 2016
    Inventors: Frank WU, Bo CHEN
  • Publication number: 20160332990
    Abstract: The present invention is directed to certain fused pyrimidines having a homo or hetero cyclopentyl, cyclohexyl or cycloheptyl ring as the pyrimidine fusion partner; having an amino benzyl or substituted amino benzyl group at the 4 position of the pyrimidine ring; and a 5:6 heterobicyclo ring with at least one N, O or S at the 2 position of the pyrimidine ring. These compounds are useful for treatment of cancer by inhibition of the p97 complex.
    Type: Application
    Filed: January 19, 2015
    Publication date: November 17, 2016
    Applicant: Cleave Biosciences, Inc.
    Inventors: Han-Jie Zhou, David Wustrow
  • Publication number: 20160332991
    Abstract: Disclosed are pyrazolyl pyrimidinamine compounds with structures as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a broad spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, anthracnosis of cucumber and the like, and especially have better control effect on downy mildew of cucumber, powdery mildew of wheat and anthracnosis of cucumber. The compounds of present invention also show good insecticidal activity, part of the compounds, at very low doses, have excellent control effect on diseases caused by Plutella xylostella, armyworm, Myzus persicae, Tetranychus cinnabarinus etc.
    Type: Application
    Filed: December 11, 2014
    Publication date: November 17, 2016
    Applicant: SHENYANG SINOCHEM AGROCHEMICALS R&D CO., LTD.
    Inventors: Changling LIU, Xufeng SUN, Jie ZHAO, Lizeng WANG, Keke LI, Jinbo ZHANG, Xuanming CHEN, Aiying GUAN, Yuquan SONG, Jie LAN, Sen MA, Lijun RU
  • Publication number: 20160332992
    Abstract: The present disclosure provides pyrimidines of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein A1, X, A2, G, Y, n, R2a, R2b, and R3 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, compounds of the present disclosure are useful for treating pain.
    Type: Application
    Filed: September 19, 2014
    Publication date: November 17, 2016
    Inventors: Chiyou Ni, Jae Hyun Park, Bin Shao, Xiaoming Zhou
  • Publication number: 20160332993
    Abstract: The present invention provides compounds of Formula (II) (e.g., compounds of Formula (I)), and pharmaceutically compositions thereof. Compounds of Formula (II) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
    Type: Application
    Filed: February 2, 2015
    Publication date: November 17, 2016
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: James E. BRADNER, Jun QI, Minoru TANAKA
  • Publication number: 20160332994
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: July 29, 2016
    Publication date: November 17, 2016
    Inventors: Kwangho Lee, Deqiang Niu, Matthew Frank Baevsky
  • Publication number: 20160332995
    Abstract: A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N3, —CN, —COOR?, —CCR?, —C(R?)C(R?)R?, —OCOR?, —OCOOR?, —SR?, —OSO2R??, and/or —CON(R?)R?, wherein each R? is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R?? is —CF3 or a perfluorinated alkyl group having from 2 to 18 carbon atoms The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound.
    Type: Application
    Filed: July 26, 2016
    Publication date: November 17, 2016
    Inventors: Meng He, Darrin R. Dabideen, Terry A. Kellar, II, Anil Kumar
  • Publication number: 20160332996
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y—Z-L-R1??(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: May 12, 2016
    Publication date: November 17, 2016
    Inventors: Yao-Ling Qiu, Wei Li, Hui Cao, Meizhong Jin, Xuri Gao, Xiaowen Peng, Jorden Kass, Yat Sun Or
  • Publication number: 20160332997
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: May 24, 2016
    Publication date: November 17, 2016
    Inventors: Sara S. HADIDA RUAH, Peter D.J. GROOTENHUIS, Fredrick VAN GOOR, Jinglan ZHOU, Brian BEAR, Mark T. MILLER, Jason McCARTNEY, Mehdi Michel Jamel NUMA, Xiaoqing YANG
  • Publication number: 20160332998
    Abstract: Compounds useful for inhibiting the immunoproteasome have the formula of Methods and compounds for inhibiting the immunoproteasome, particularly, immunoproteasome inhibitors with non-peptide scaffolds, are described.
    Type: Application
    Filed: May 16, 2016
    Publication date: November 17, 2016
    Inventors: Chang-Guo Zhan, Kyung Bo Kim, Vinod Kasam, Na-Re Lee