Patents Issued in August 11, 2016
  • PHOTOREACTIVE SYNTHETIC REGULATOR OF PROTEIN FUNCTION AND METHODS OF USE THEREOF
    Publication number: 20160229794
    Abstract: The present disclosure provides a photoreactive synthetic regulator of protein function. The present disclosure further provides a light-regulated polypeptide that includes a subject synthetic regulator. Also provided are cells and membranes comprising a subject light-regulated polypeptide. The present disclosure further provides methods of modulating protein function, involving use of light.
    Type: Application
    Filed: April 19, 2016
    Publication date: August 11, 2016
    Inventors: Dirk Trauner, Ehud Y. Isacoff, Richard H. Kramer, Matthew R. Banghart, Doris L. Fortin, Alexandre Mourot
  • COMPOUNDS AND MESOGENIC MEDIA
    Publication number: 20160229795
    Abstract: Disclosed are compounds of formula I the use of compounds of formula I in liquid crystal media and in particular to flexoelectric liquid crystal devices containing the liquid crystal media.
    Type: Application
    Filed: September 8, 2014
    Publication date: August 11, 2016
    Applicant: MERCK PATENT GMBH
    Inventors: Kevin ADLEM, Owain Llyr PARRI
  • METFORMIN SALTS TO TREAT TYPE2 DIABETES
    Publication number: 20160229796
    Abstract: Metformin salts of 2,4-thiazolidinediones are described for the treatment of diabetes mellitus Type2, gestational diabetes, polycystic ovary syndrome, non-alcoholic fatty liver disease, coronary artery disease, pancreatic cancer, premature puberty, and other diseases which manifest insulin resistance.
    Type: Application
    Filed: September 20, 2014
    Publication date: August 11, 2016
    Applicant: Jiva Pharma, Inc.
    Inventor: Om P Goel
  • LOW PH METAL-FREE PREPARATION OF AMINATED ORGANIC ACID
    Publication number: 20160229797
    Abstract: The invention provides a process for making compounds according to Formula I: where R1, R1a, R2, R2a, R3 and R3a are defined as set forth in the specification. Formula I compounds are useful as chelants and stabilizers of cations in aqueous media and the invention therefore provides a method for using the compounds in the treatment of subterranean formations, such as in acidizing operations.
    Type: Application
    Filed: October 17, 2014
    Publication date: August 11, 2016
    Inventors: Antonio Recio III, Enrique Antonio Reyes
  • POLYTHIOL COMPOUND AND METHOD FOR PRODUCING SAME
    Publication number: 20160229798
    Abstract: According to the present invention, a polythiol compound having a total nitrogen content of 50 to 600 ppm inclusive can be provided. According to the present invention, a method for producing the polythiol compound can also be provided, said method being characterized by comprising the steps of: reacting a polyalcohol with thiourea to prepare a thiuronium salt; and adding at least one base selected from the group consisting of hydrazine (hydrate), ammonia and an amine and an inorganic base (that is different from hydrazine (hydrate) or ammonia) to the thiuronium salt in the presence of an organic solvent to hydrolyze the thiuronium salt.
    Type: Application
    Filed: October 28, 2014
    Publication date: August 11, 2016
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Yoshihiko NISHIMORI, Teruo KAMURA, Hiroshi HORIKOSHI
  • PROCESS FOR OBTAINING METHIONINE
    Publication number: 20160229799
    Abstract: The invention relates to a method for crystallizing D,L-methionine from aqueous solutions and/or suspensions containing D,L-methionine and D,L-methionine ammonium salts, having a Met content of 70-180 g/kg, an NH4+ content of 1-5 g/kg, in the presence of a crystallization additive, which comprises a nonionic or anionic surfactant or a mixture of various nonionic or anionic surfactants, in which the temperature of the solution and/or suspension is lowered directly or stepwise from T1=85-110° C. to T2=30-50° C., so that D,L-methionine precipitates as a solid.
    Type: Application
    Filed: September 10, 2014
    Publication date: August 11, 2016
    Applicant: EVONIK DEGUSSA GmbH
    Inventors: Stefan REICHERT, Harald JAKOB, Hans Joachim HASSELBACH, Martin KÖRFER
  • ALLYL DISULFIDE-CONTAINING ADDITION-FRAGMENTATION OLIGOMERS
    Publication number: 20160229800
    Abstract: A Addition-fragmentation oligomers containing allylic disulfide groups are described. The oligomers may be added to polymerizable compositions to provide labile crosslinks that can cleave and reform during the polymerization process.
    Type: Application
    Filed: October 6, 2014
    Publication date: August 11, 2016
    Inventors: Ann R. Fornof, William H. Moser, Ahmed S. Abuelyaman, Guy D. Joly, Larry R. Krepski
  • ONIUM SALT AND COMPOSITION COMPRISING THE SAME
    Publication number: 20160229801
    Abstract: The onium salt of the present invention contains predetermined compound A represented by the general formula (1). The composition of the present invention contains the onium salt of the present invention, and an onium salt containing predetermined compound B represented by the general formula (2). The onium salt and the composition of the present invention exert well-balanced excellent physical properties in terms of cold curing properties, storage stability, thermal shock resistance after curing, and moisture resistance.
    Type: Application
    Filed: September 24, 2014
    Publication date: August 11, 2016
    Applicant: ASAHI KASEI E-MATERIALS CORPORATION
    Inventors: Tadashi SHIMURA, Naoya KAMIMURA, Akira OTANI, Hitoshi SHIMADA
  • C5AR ANTAGONISTS
    Publication number: 20160229802
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Application
    Filed: September 4, 2015
    Publication date: August 11, 2016
    Inventors: Pingchen FAN, Kevin Lloyd GREENMAN, Manmohan Reddy LELETI, Yandong LI, Jay POWERS, Hiroko TANAKA, Ju YANG, Yibin ZENG
  • ELECTROCHROMIC COMPOUNDS WITH IMPROVED COLOR STABILITY IN THEIR RADICAL STATES
    Publication number: 20160229803
    Abstract: The invention relates to an electrochromic device and uses thereof, wherein the electrochromic device includes an electrochromic compound with reduced intermolecular interactions resulting in uncontrolled color changes represented by Formula (I):
    Type: Application
    Filed: February 10, 2016
    Publication date: August 11, 2016
    Inventors: Rongguang LIN, Kelvin L. BAUMANN, Punam GIRI, Joel C. NEMES, Leroy J. KLOEPPNER, David A. THEISTE
  • TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20160229804
    Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: September 17, 2014
    Publication date: August 11, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
  • Process for Preparing Quinoline Derivatives
    Publication number: 20160229805
    Abstract: A process for preparing a compound of Formula I is disclosed, comprising the steps: wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted with heterocycloalkyl; R4 is (C1-C6)alkyl; and Q is CH or N; comprising: (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; (b) adding and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and (c) coupling a compound of Formula A with an amine of Formula B to form a compound of Formula 1.
    Type: Application
    Filed: April 20, 2016
    Publication date: August 11, 2016
    Inventors: Jo Ann Wilson, Sriram Naganathan, Neil G. Andersen, Matthew Pfeiffer
  • SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE
    Publication number: 20160229806
    Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
    Type: Application
    Filed: September 14, 2015
    Publication date: August 11, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
  • NEW PHENYL-DIHYDROPYRIDINE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS
    Publication number: 20160229807
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1 and n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: April 14, 2016
    Publication date: August 11, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Kurt Amrein, Robert Britton, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Xuefei Tan
  • PROCEDURE FOR THE SYNTHESIS OF N-BENZYL-N-CYCLOPROPYL-1H-PYRAZOLE-4-CARBOXAMIDE DERIVATIVES
    Publication number: 20160229808
    Abstract: A new one-step process for the preparation of pyrazole carboxamide derivatives of the general formula (I) by reaction of 3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carbaldehyde with an amine or its salt.
    Type: Application
    Filed: September 4, 2014
    Publication date: August 11, 2016
    Inventors: Peter BRÜCHNER, Sergii PAZENOK
  • HETEROCYCLIC VINYL AUTOTAXIN INHIBITOR COMPOUNDS
    Publication number: 20160229809
    Abstract: Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
    Type: Application
    Filed: September 16, 2014
    Publication date: August 11, 2016
    Inventors: John Howard HUTCHINSON, Timothy Andrew PARR, Kevin Duane BUNKER, David LONERGAN
  • Selective Inhibition of Bacterial Topoisomerase I
    Publication number: 20160229810
    Abstract: The present invention provides novel bisbenzimidazole compounds and methods of using the compounds as antibacterial agents.
    Type: Application
    Filed: September 19, 2014
    Publication date: August 11, 2016
    Applicant: The Florida International University Board of Trustees
    Inventors: Nihar RANJAN, Dev P. ARYA, Fenfei LENG
  • TETRA-ARYL CYCLOBUTANE INHIBITORS OF ANDROGEN RECEPTOR ACTION FOR THE TREATMENT OF HORMONE REFRACTORY CANCER
    Publication number: 20160229811
    Abstract: The present disclosure provides tetra-substituted cyclobutane inhibitors of Androgen Receptor Action, and methods of using such inhibitors, for the treatment of hormone-refractory cancers.
    Type: Application
    Filed: September 25, 2014
    Publication date: August 11, 2016
    Inventors: John Katzenelienbogen, Donald McDonneli, John D, Norris, Alexander Parent, Julie Pollock, Jillian Gunther, Kathryn E. Carlson, Teresa Martin
  • SALT OF NITROGEN-CONTAINING HETEROCYCLIC COMPOUND OR CRYSTAL THEREOF, PHARMACEUTICAL COMPOSITION, AND FLT3 INHIBITOR
    Publication number: 20160229812
    Abstract: An object of the present invention is to provide a compound and pharmaceutical composition showing superior stability and/or solubility, etc. and having superior FLT3 inhibitory activity. The present invention provides a salt of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide, or a crystal thereof. Since the salt or a crystal thereof has superior FLT3 inhibitory activity and shows superior physicochemical properties as drugs, such as storage stability, solubility, and so forth, it is useful for treatments of diseases or conditions relating to FLT3. The present invention also provides a pharmaceutical composition and FLT3 inhibitor containing the salt or a crystal thereof.
    Type: Application
    Filed: April 15, 2016
    Publication date: August 11, 2016
    Applicant: FUJIFILM Corporation
    Inventors: Shinsuke MIZUMOTO, Takuya MATSUMOTO
  • ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20160229813
    Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: August 17, 2015
    Publication date: August 11, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng Di Marco, Thomas J. Greshock
  • HETEROCYCLIC COMPOUND
    Publication number: 20160229814
    Abstract: The present invention provides a heterocyclic compound having an ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I): wherein Ar is a the partial structure (1) to the partial structure (5), Q is a bivalent group selected from the group consisting of (Ia)-(If), and B is a ring optionally having substituent(s), or a salt thereof.
    Type: Application
    Filed: March 13, 2014
    Publication date: August 11, 2016
    Inventors: Satoshi Yamamoto, Junya Shirai, Yoshiyuki Fukase, Ayumu Sato, Mitsunori Kouno, Yoshihide Tomata, Atsuko Ochida, Kazuko Yonemori, Tsuneo Oda, Takashi Imada, Tomoya Yukawa
  • HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
    Publication number: 20160229815
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: October 19, 2015
    Publication date: August 11, 2016
    Inventors: John M. McCall, Donna L. Romero, John McKearn, Michael Clare
  • CYANOTRIAZOLE COMPOUNDS
    Publication number: 20160229816
    Abstract: This invention relates to a cyanotriazole compound represented by the formula (1): wherein each symbols are defined in the specification, or a salt thereof. The compound or a salt thereof stimulates the citric acid cycle activity and/or improves hyperglycemia with less side effects, and excellent safety, and therefore, it is useful for treating and/or preventing diseases or disorders on which citric acid cycle activation and/or improvement of hyperglycemia has a prophylactic and/or therapeutic effect, for example, diabetes, impaired glucose tolerance, insulin resistance, diabetic complications, obesity, dyslipidemia, hepatic steatosis, atherosclerosis and/or cardiovascular disease, as well as diseases or disorders that would benefit from stimulating energy expenditure.
    Type: Application
    Filed: July 16, 2014
    Publication date: August 11, 2016
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Seiji SATO, Satoshi MATSUDA, Chiharu MATSUMURA, Motohire ITOTANI, Toshio SHINOHARA, Shigekazu FUJITA, Yohji SAKURAI, Kuninori TAI, Tae FUKUSHIMA, Naohide KANEMOTO, Takashi OKAMOTO
  • ANTIFUNGAL COMPOUNDS OF (ARYLALKYL) AZOLE DERIVATIVES IN THE STRUCTURE OF OXIME ESTER
    Publication number: 20160229817
    Abstract: This invention is related to the antifungal compounds having azole structure in Formula (1), and hydrates, solvates, pharmaceutically acceptable salts or geometric isomers thereof.
    Type: Application
    Filed: September 16, 2014
    Publication date: August 11, 2016
    Inventors: Sevim DALKARA, Selma SARAC TARHAN, Arzu KARAKURT
  • Compounds for Nonsense Suppression, and Methods for Their Use
    Publication number: 20160229818
    Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.
    Type: Application
    Filed: April 15, 2016
    Publication date: August 11, 2016
    Applicant: PTC Therapeutics, Inc.
    Inventors: Neil Almstead, Gary M. Karp, Richard Wilde, Ellen Welch, Hongyu Ren
  • FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE
    Publication number: 20160229819
    Abstract: Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.
    Type: Application
    Filed: February 8, 2015
    Publication date: August 11, 2016
    Inventor: Mark Quang Nguyen
  • PROCESS FOR PREPARING SUBSTITUTED ISATOIC ACID ANHYDRIDE COMPOUNDS AND DERIVATIVES THEREOF
    Publication number: 20160229820
    Abstract: The present invention relates to a process for preparing substituted isatoic acid anhydride compounds of the formula (I) in which R1 is Cl, Br, I, or CN; and R2 is CH3, Cl, Br; using anthranilic acid derivative compounds of formula (III) and/or carbamate compounds of formula (II) wherein R1 and R2 are as defined above; RAr is CH3, Cl, NO2 and n is 0, 1, 2, 3, 4 or 5; The present invention relates also to the compounds of formula (II) and to processes comprising further preceding and/or subsequent reaction steps, leading to anthranilamide pesticides or to precursors for them.
    Type: Application
    Filed: October 6, 2014
    Publication date: August 11, 2016
    Inventors: Thomas ZIERKE, Jonas HILZENDEGEN, Christopher KORADIN, Karsten KOERBER, Roland GOETZ
  • ARYLPIPERAZINE DERIVATIVES AND METHODS OF UTILIZING SAME
    Publication number: 20160229821
    Abstract: The present invention provides arylpiperazine derivatives having Formula I as shown below, which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression,
    Type: Application
    Filed: February 8, 2016
    Publication date: August 11, 2016
    Inventors: Laxminarayan BHAT, Prabhu Prasad MOHAPATRA, Kouacou ADIEY
  • CRYSTAL MODIFICATIONS OF ELOBIXIBAT
    Publication number: 20160229822
    Abstract: The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.
    Type: Application
    Filed: April 21, 2016
    Publication date: August 11, 2016
    Inventors: Martin Bohlin, Erica Tjerneld, Andreas Vestermark, Ingvar Ymen
  • DEUTERATED COMPOUNDS USEFUL FOR TREATING NEURODEGENERATIVE DISEASES
    Publication number: 20160229823
    Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.
    Type: Application
    Filed: March 31, 2014
    Publication date: August 11, 2016
    Inventor: Damodara GOPAL
  • ASSAY FOR THE DETECTION OF THE PHENYLPIPERAZINE FAMILY
    Publication number: 20160229824
    Abstract: The current invention describes novel immunogens which are used in the production of novel antibodies with unique binding properties in that they cross-react with a variety of phenylpiperazine derivatives. These antibodies enable methods and kits to detect and/or determine phenylpiperazine derivatives (for example mCPP, TFMPP and MeOPP) in an in vitro sample which are advantageous over currently available analytical methods in terms of cost, ease of use, speed and sensitivity.
    Type: Application
    Filed: April 15, 2016
    Publication date: August 11, 2016
    Inventors: Elouard BENCHIKH, Ivan McConnell, Philip Lowry, Peter Fitzgerald
  • SYNTHETIC PROCESS FOR PREPARING 2-FUROIC ACID DERIVATIVES
    Publication number: 20160229825
    Abstract: Disclosed herein are processes for forming 2-furoic acid derivatives represented by Formula (I):
    Type: Application
    Filed: February 4, 2016
    Publication date: August 11, 2016
    Inventors: Anthony Adrian Shaw, Kanjai Khumtaveeporn, Pavel Krasik
  • SYNTHETIC PROCESS FOR PREPARING 2-((2-ETHOXY-2-OXOETHYL)(METHYL)AMINO)-2-OXOETHYL 5-TETRADECYLOXY)FURAN-2-CARBOXYLATE
    Publication number: 20160229826
    Abstract: Disclosed herein are processes for forming 2-((2-ethoxy-2-oxoethyl)(methyl)amino)-2-oxoethyl 5-tetradecyloxy)furan-2-carboxylate:
    Type: Application
    Filed: February 4, 2016
    Publication date: August 11, 2016
    Inventors: Anthony Adrian Shaw, Kanjai Khumtaveeporn, Pavel Krasik
  • A PROCESS FOR THE PREPARATION OF ANTI-INFLAMMATORY AROYLBENZOFURAN COMPOUNDS
    Publication number: 20160229827
    Abstract: Disclosed herein an efficient process for synthesis of benzofuran analogues having anti-inflammatory activity which comprises, Ru-catalyzed branched and linear selective alkylation of aroylbenzofurans formula-I with alpha, beta unsaturated esters of formula-II via C—H activation in presence of base, additives and organic solvent at suitable temperature to give high yield of desired linear alkylated benzofuran compounds of formula-III or branched alkylated benzofuran compounds of formula-IV or mixture thereof.
    Type: Application
    Filed: August 25, 2014
    Publication date: August 11, 2016
    Inventors: Chepuri Venkata RAMANA, Yadagiri KOMMAGALLA, Kolluru SRINIVAS
  • R TYPE OF RESVERATROL DIMER, PREPARATION PROCESS THEREFOR AND PURPOSE THEREOF IN LOWERING BLOOD SUGAR LEVEL
    Publication number: 20160229828
    Abstract: The present invention relates to the field of natural pharmaceutical chemistry, and in particular, to a resveratrol dimer (7R,8R)-trans-?-viniferin (I), a preparation process therefor and a purpose thereof in lowering a blood sugar level. According to the present invention, an R type of resveratrol dimer is separated from the resveratrol dimer by using high-speed countercurrent chromatography. Pharmacodynamic tests proved that the R type of resveratrol dimer has a better effect in lowering a blood sugar level than a racemate.
    Type: Application
    Filed: June 5, 2014
    Publication date: August 11, 2016
    Applicant: CHINA PHARMACEUTICAL UNIVERSITY
    Inventors: Lingyi KONG, Jianguang LUO, Chao HAN, Xiaobing WANG, Hao HONG
  • Method for Producing Asymmetric Conjugated Diyne Compound and Method for Producing Z,Z-Conjugated Diene Compound Using the Same
    Publication number: 20160229829
    Abstract: Provided are a method for efficiently producing an asymmetric conjugated diyne from an inexpensive and safe alternative compound to hydroxylamine hydrochloride and a method for producing a Z,Z-conjugated diene compound from the asymmetric conjugated diyne compound thus obtained. More specifically, provided is a method for producing an asymmetric conjugated diyne compound comprising a step of subjecting a terminal alkyne compound (1): HC?C—Z1—Y1 to a coupling reaction with an alkynyl halide (2) Y2—Z2—C?C—X by using sodium borohydride in water and an organic solvent in the presence of a copper catalyst and a base to obtain the asymmetric conjugated diyne compound (3): Y2—Z2—C?C—C?C—Z1—Y1. In addition, provided is a method for producing a Z,Z-conjugated diene compound by reducing the resulting asymmetric conjugated diyne compound, or the like.
    Type: Application
    Filed: February 3, 2016
    Publication date: August 11, 2016
    Inventors: Yuki Miyake, Takeshi Kinsho, Miyoshi Yamashita, Naoki Ishibashi, Yusuke Nagae, Akihiro Baba
  • GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
    Publication number: 20160229830
    Abstract: Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
    Type: Application
    Filed: September 19, 2014
    Publication date: August 11, 2016
    Inventors: Bing Wang, Daniel Chu, Alexander James Bridges
  • SUBSTITUTED 3-PHENYLPROPYLAMINE DERIVATIVES FOR THE TREATMENT OF OPHTHALMIC DISEASES AND DISORDERS
    Publication number: 20160229831
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: September 10, 2015
    Publication date: August 11, 2016
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • POLYMER-FIXED DERIVATIVES OF DITHIOLANE OR DITHIANE
    Publication number: 20160229832
    Abstract: Derivatives of 1,3-dithianes and 1,3-dithiolanes of the general formula 1a or salts thereof of the general formula 1b where P=polymeric support, m=1 or 2, Z is an organic linker or X=inorganic or organic anion, processes for preparation thereof and use thereof.
    Type: Application
    Filed: September 23, 2014
    Publication date: August 11, 2016
    Inventors: Nicole JUNG, Simone GRAESSLE, Stefan BRAESE
  • QUINAZOLINONES AND AZAQUINAZOLINONES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS
    Publication number: 20160229833
    Abstract: The present disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R4?, X1, Y1, Y2, Y3, Y4, n, and m are described herein.
    Type: Application
    Filed: February 4, 2016
    Publication date: August 11, 2016
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, David Lancia, JR.
  • QUINAZOLINE DERIVATIVES AND THEIR USE AS DNA METHYLTRANSFERASE INHIBITORS
    Publication number: 20160229834
    Abstract: The present invention relates to compounds of the following formula (I): and pharmaceutically acceptable salts and solvates thereof, their methods of preparation, their use as a drug, notably in the treatment of cancer, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: September 19, 2014
    Publication date: August 11, 2016
    Applicants: PIERRE FABRE MEDICAMENT, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: Ludovic HALBY, Paola Barbara ARIMONDO
  • NOVEL PYRIDYLOXYACETYL TETRAHYDROISOQUINOLINE COMPOUNDS USEFUL AS NAMPT INHIBITORS
    Publication number: 20160229835
    Abstract: The present invention provides novel pyridyloxyacetyl tetrahydroisoquinoline compounds that inhibit NAMPT and may be useful in the treatment of cancer.
    Type: Application
    Filed: October 3, 2014
    Publication date: August 11, 2016
    Inventors: Timothy Paul Burkholder, Miriam Filadelfa Del Prado, Maria Carmen Fernandez, Lawrence Joseph Heinz, II, Lourdes Prieto, Genshi Zhao
  • MULTIVALENT RAS BINDING COMPOUNDS
    Publication number: 20160229836
    Abstract: The present invention provides, inter alia, compounds that selectively bind a RAS protein at two or more sites and methods for their synthesis. Compositions and kits containing the compounds, as well as methods of using the compounds and compositions for ameliorating or treating the effects of a disease associated with altered RAS signaling, such as a cancer, in a subject and methods for effecting cancer cell death are also provided herein. Methods of identifying a multivalent compound which binds selectively to a target protein also are provided herein.
    Type: Application
    Filed: March 22, 2016
    Publication date: August 11, 2016
    Inventors: Brent R. Stockwell, Matthew Welsch
  • SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
    Publication number: 20160229837
    Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
    Type: Application
    Filed: October 10, 2015
    Publication date: August 11, 2016
    Applicants: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLC
    Inventors: Ning Xi, Minxiong Li, Xiaobo Li, Weilong Dai, Haiyang Hu, Tao Zhang, Wuhong Chen
  • AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME
    Publication number: 20160229838
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: January 12, 2016
    Publication date: August 11, 2016
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Factor XIa Inhibitors
    Publication number: 20160229839
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Application
    Filed: September 23, 2014
    Publication date: August 11, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Eric Mertz, Scott D. Edmondson, Ning Shao, Santhosh Neelamkavil, Corey Poker, Zahid Hussain, Zhuyan Guo, Nancy Jo Kevin, Yi Zang, Jiafang He
  • ACTIVATABLE FLUOROGENIC COMPOUNDS AND USES THEREOF AS NEAR INFRARED PROBES
    Publication number: 20160229840
    Abstract: Novel fluorogenic compounds designed such that upon a chemical event, compounds capable of emitting NIR light are generated, are disclosed. The compounds comprise two or more acceptor-containing moieties and a cleavable donor-containing moiety, being in complete pi-electrons conjugation and being such that no delocalization of pi-electrons is enabled. Also disclosed are fluorescent compounds generated upon subjecting the fluorogenic compounds to a chemical event (e.g., deprotonation). Also disclosed are uses of the fluorogenic compounds as NIR probed with a Turn-ON mechanism in monitoring presence and/or level of various analytes.
    Type: Application
    Filed: April 18, 2016
    Publication date: August 11, 2016
    Applicant: Ramot at Tel-Aviv University Ltd.
    Inventors: Doron SHABAT, Ronit SATCHI-FAINARO
  • NOVEL BETA LACTAMS AS MODULATORS OF GLUTAMATE UPTAKE AND METHODS FOR USE THEREOF
    Publication number: 20160229841
    Abstract: Pharmaceutical compositions of the invention comprise compounds, compositions, methods useful for the treatment of drug addiction, drug withdrawal, and diseases or conditions that involve dysregulation of glutamate homeostasis in it etiology.
    Type: Application
    Filed: June 4, 2014
    Publication date: August 11, 2016
    Inventors: Magid ABOU-GHARBIA, Wayne E. CHILDERS, Rogelio L. MARTINEZ, Mercy M. RAMANJULU, Benjamin E. BLASS
  • Process for the Preparation of Voriconazole and Analogues Thereof
    Publication number: 20160229842
    Abstract: The present invention provides a process for preparing a compound of formula: (Formula XI and XII) (XI) (XII) wherein X, Y, Z, A, B and E are as defined herein, by reacting a compound of formula: (Formula XIII) (XIII) with a compound of formula: (Formula XIV and XV) (XIV) (XV) respectively, in the presence of a transition metal catalyst, a ligand suitable for use with 15 the catalyst and a reducing agent. The invention also provides novel intermediates.
    Type: Application
    Filed: April 20, 2016
    Publication date: August 11, 2016
    Inventors: Adam James Musgrave Burrell, Padraig Mary O'Neill, Alan John Pettman
  • AZA-HETEROARYL COMPOUNDS AS PI3K-GAMMA INHIBITORS
    Publication number: 20160229843
    Abstract: The present invention provides aza-heteroaryl derivatives of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A, W, R4, R5, and R6 are defined herein, that inhibit the activity of phosphoinositide 3-kinases-gamma (PI3K?) and are useful in the treatment of diseases related to the activity of PI3K? including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Application
    Filed: February 9, 2016
    Publication date: August 11, 2016
    Inventors: Ge Zou, Andrew P. Combs, Andrew W. Buesking