Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 546/284.1)
  • Patent number: 10351577
    Abstract: Ether analogues of galiellalactone, methods of preparing the analogues, and use of the analogues in the treatment of cancer are disclosed.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: July 16, 2019
    Assignee: Glactone Pharma Development AB
    Inventors: Johansson Martin, Olov Sterner, Anders Bjartell, Rebecka Hellsten, Zilma Escobar
  • Patent number: 10144746
    Abstract: Provided herein are kallikrein modulating compounds, pharmaceutical compositions comprising the same, and uses thereof.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: December 4, 2018
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Manuel Zancanella, Chul Yu, Lina Q. Setti, Hing Sham, Qing Xu, Calvin W. Yee, Ming Yu
  • Patent number: 9815853
    Abstract: Provided herein are kallikrein modulating compounds, pharmaceutical compositions comprising the same, and uses thereof.
    Type: Grant
    Filed: June 9, 2016
    Date of Patent: November 14, 2017
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Manuel Zancanella, Chul Yu, Lina Setti, Hing Sham, Qing Xu, Calvin Yee, Ming Yu
  • Patent number: 9309267
    Abstract: The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: April 12, 2016
    Assignee: AstraZeneca AB
    Inventors: Seth Björk, Peter Johnström, Nils A. Nilsson, Katinka Ruda, Per M. Schou, Britt-Marie Swahn, Vern Delisser
  • Patent number: 9255093
    Abstract: The present invention provides a compound of formula I, in which R1, R2, X and R3 are defined in the Summary of the Invention, or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: February 9, 2016
    Assignee: NOVARTIS AG
    Inventors: Gregory Raymond Bebernitz, Emma Cody, Tajesh Patel, Ming Qian, Lewis Whitehead, Thomas Zabawa, Frederic Zecri
  • Publication number: 20150133444
    Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
  • Publication number: 20150126372
    Abstract: 4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 7, 2015
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Stephen Craig Fields, Lindsey G. Fischer, Natalie C. Giampietro, Katherine A. Guenthenspberger, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbet M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Nick X. Wang
  • Publication number: 20150119397
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine 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: January 8, 2015
    Publication date: April 30, 2015
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20150094341
    Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.
    Type: Application
    Filed: September 29, 2014
    Publication date: April 2, 2015
    Inventors: Fangzheng Li, Kevin G. Meyer, James M. Renga, Chenglin Yao, Jeremy Wilmot, Jessica Herrick, Karla Bravo-Altamirano, Timothy Boebel
  • Publication number: 20150093339
    Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 2, 2015
    Inventors: Catherine TACHDJIAN, Andrew P. PATRON, Sara L. ADAMSKI-WERNER, Farid BAKIR, Qing CHEN, Vincent DARMOHUSODO, Stephen Terrence HOBSON, Xiaodong LI, Ming QI, Daniel H. ROGERS, Marketa RINNOVA, Guy SERVANT, Xiao-Qing TANG, Mark ZOLLER, David WALLACE, Amy XING, Klaus GUBERNATOR
  • Publication number: 20150087676
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: December 9, 2014
    Publication date: March 26, 2015
    Inventors: Michael Eissenstat, Dehui Duan
  • Publication number: 20150069332
    Abstract: [This] charge transport material which comprises a compound expressed by the following formula has a high efficiency and drive durability after high-temperature storage and resists the occurrence of dark spots (X101 represents a sulfur atom or an oxygen atom; R101 and R102 represent each independently an alkyl group, an aryl group, a heteroaryl group, a fluorine atom, or a silyl group, and may further be substituted with these groups; n101 represents an integer from 0 to 11; n102 represents an integer from 0 to 7; a plurality of R101 and R102 [groups] may be the same or different; and L101 represents a single bond or a divalent linking group; however, one of R101, L101, and R102 includes a fluorine atom, a fluoroalkyl group, a cycloalkyl group, a cycloalkylene group, a silyl group, an alkylsilyl group, an arylsilyl group, or a silicon atom linking group.
    Type: Application
    Filed: March 29, 2012
    Publication date: March 12, 2015
    Applicant: UDC IRELAND LIMITED
    Inventors: Tetsu Kitamura, Kousuke Watanabe
  • Publication number: 20150065494
    Abstract: The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.
    Type: Application
    Filed: April 1, 2013
    Publication date: March 5, 2015
    Inventors: Dong Jin Kim, Kyung Ho Yoo, Young Soo Kim, Woong Seo Park, Yong Koo Kang, Hye Yun Kim, Yun Kyung Kim, Ki Duk Park, Maeng Sup Kim, Kwee Hyun Suh, Young Gil Ahn
  • Patent number: 8952151
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine 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: Grant
    Filed: December 23, 2013
    Date of Patent: February 10, 2015
    Assignee: Quanticel Pharmaceuticals, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20150031725
    Abstract: Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases.
    Type: Application
    Filed: October 2, 2014
    Publication date: January 29, 2015
    Inventors: Richard J. Pietras, Michael E. Jung, Diana C. Marquez-Garban, Gang Deng
  • Publication number: 20150021577
    Abstract: A novel organic compound that can be used as a carrier-transport material, a host material, or a light-emitting material in a light-emitting element is provided. Specifically, an organic compound that can give a light-emitting element having favorable characteristics even when the organic compound is used in a light-emitting element emitting phosphorescence is provided. The organic compound has a bipyridine skeleton formed by two pyridine skeletons to each of which a dibenzothiophenyl group or a dibenzofuranyl group is bonded via an arylene group.
    Type: Application
    Filed: July 16, 2014
    Publication date: January 22, 2015
    Inventors: Hiroshi Kadoma, Satomi Mitsumori, Yuko Kawata, Takao Hamada, Satoshi Seo
  • Publication number: 20150025046
    Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.
    Type: Application
    Filed: February 27, 2013
    Publication date: January 22, 2015
    Inventors: Mihir Mandal, Timothy A. Blizzard, Helen Chen, Harry Chobanian, Yan Guo, Barbara Pio, Zhicai Wu, Tesfaye Biftu, William J. Greenlee, Johnny Zhaoning Zhu
  • Publication number: 20150018542
    Abstract: Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, wherein R1 and R2 are each independently hydrogen, straight or branched chained C1-C4 alkyl, C3-C4 cycloalkyl or saturated 5- or 6-membered heterocyclyl containing oxygen or nitrogen; or R1 and R2 together with N form an unsubstituted or substituted saturated 5- or 6-membered heterocyclyl containing at least one heteroatom, wherein the heteroatom is O, N and S, the substituent is a methyl on N; R3 is a hydrogen atom or a chlorine atom; R4 is a hydrogen atom or a fluorine atom; X is CH, CF or N; and Y is CH, CF or N.
    Type: Application
    Filed: January 14, 2013
    Publication date: January 15, 2015
    Inventors: Chunhao Yang, Zehong Miao, Jian Ding, Meng Wang, Jinxue He, Cun Tan, Yi Chen
  • Publication number: 20150014666
    Abstract: An aromatic amine derivative is represented by a formula (1) below. In the formula (1), R2, R3, R4, R5, R7, R8, R9 and R10 each independently represent a hydrogen atom and a substituent. In the formula (1), R1 and R6 are represented by a formula (2) below, and L1 to L2 are each independently a single bond, a divalent residue of an aryl group, and the like. L3 is a divalent residue of an aryl group and the like. In the formula (2); Ar1 is a monovalent substituent having a partial structure represented by the following formula (3); X represents an oxygen atom or a sulfur atom; and A and B represent a six-membered ring. In the formula (2), Ar2 is an aryl group, a monovalent substituent having a partial structure represented by the formula (3), and the like.
    Type: Application
    Filed: September 21, 2012
    Publication date: January 15, 2015
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Yumiko Mizuki, Hirokatsu Ito
  • Publication number: 20150018547
    Abstract: The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 15, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Takakura, Yoshihiro Banno, Yoshito Terao, Atsuko Ochida, Sachie Morimoto, Shuji Kitamura, Yoshihide Tomata, Tsuneo Yasuma, Minoru Ikoma, Kei Masuda
  • Patent number: 8927544
    Abstract: The present invention relates to benzofuran-2-sulfonamide derivatives with the following formula: or pharmaceutically acceptable salts thereof. The derivatives are useful as modulators of chemokine receptors.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: January 6, 2015
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20150005282
    Abstract: Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutic agents, especially the GPR40 agonist and in preparation of drugs for treating diseases such as diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
    Type: Application
    Filed: December 27, 2012
    Publication date: January 1, 2015
    Inventors: Fanglong Yang, Qing Dong, Jihui Han, Chunfei Wang, Ling Zhang, Yang Wang
  • Publication number: 20150005165
    Abstract: The invention relates to a carboxylic acid derivatives of benzoheterocyclyl pyridines and benzoheterocyclyl pyrimidines of general formula (I) and to the use thereof as herbicides.
    Type: Application
    Filed: July 24, 2012
    Publication date: January 1, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Gerhard Hoffmann, Marco Bruenjes, Uwe Doeller, Hans-Joerg Dietrich, Isolde Haeuser-Hahn, Christopher Hugh Rosinger, Elmar Gatzweiler, Ines Heinemann
  • Publication number: 20150005349
    Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I or II or a stereoisomer, tautomer, racemic, metabolite, pro- or pre-drug, salt, hydrate, or solvate thereof, wherein Ar, Cy, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
    Type: Application
    Filed: July 1, 2014
    Publication date: January 1, 2015
    Inventors: Robert Owen Messing, Michael A. Pleiss, Jon D. Levine
  • Publication number: 20140378492
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 10, 2014
    Publication date: December 25, 2014
    Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
  • Publication number: 20140350034
    Abstract: The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: January 25, 2013
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Trixi Brandl, Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard, Martin Renatus
  • Publication number: 20140346482
    Abstract: An aromatic amine derivative is represented by the following formula (1). In the formula (1), R1 to R10 each independently represent a hydrogen atom and a substituent. In the formula (1); R1 is represented by the following formula (2); any one of R2 to R5 and R7 to R10 is represented by the following formula (2); and L1 to L3 each independently represent a single bond, a divalent residue of an aryl group, or the like. In the formula (2); Ar1 is a monovalent substituent having a partial structure represented by the following formula (3); X represents an oxygen atom or a sulfur atom; and A and B represent a six-membered ring. In the formula (2), Ar2 is an aryl group, a monovalent substituent having a partial structure represented by the formula (3), and the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: November 27, 2014
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Yumiko Mizuki, Hirokatsu Ito
  • Publication number: 20140343078
    Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.
    Type: Application
    Filed: July 29, 2014
    Publication date: November 20, 2014
    Inventors: Michael EISSENSTAT, Dehui DUAN, Ji-Hye KANG
  • Publication number: 20140332772
    Abstract: A styryl-based compound represented by Formula 1 below is disclosed. An organic light-emitting diode including the styryl-based compound is also disclosed.
    Type: Application
    Filed: November 8, 2013
    Publication date: November 13, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Sang-Hyun Han, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jin-O Lim, Soo-Yon Kim, Eun-Jae Jeong, Jun-Ha Park, Eun-Young Lee, Jong-Hyuk Lee
  • Publication number: 20140336198
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 13, 2014
    Applicants: MERCK PATENT GMBH, BIONOMICS LIMITED
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Publication number: 20140315949
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 19, 2012
    Publication date: October 23, 2014
    Applicant: CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Nasveschuk
  • Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140296534
    Abstract: The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.
    Type: Application
    Filed: January 7, 2014
    Publication date: October 2, 2014
    Applicant: AstraZeneca AB
    Inventors: Seth Björk, Peter Johnström, Nils A. Nilsson, Katinka Ruda, Per M. Schou, Britt-Marie Swahn, Vern Delisser
  • Publication number: 20140275172
    Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Nalin Subasinghe
  • Publication number: 20140274695
    Abstract: 4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Stephen Craig Fields, Lindsey G. Fischer, Natalie C. Giampietro, Katherine A. Guenthenspberger, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbert M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Nick X. Wang
  • Publication number: 20140275132
    Abstract: The present invention relates to novel pyridine or pyrimidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with chemokine receptor modulation.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, John E. Donello, Veena Viswanath, Michael E. Garst, Haiqing Yuan, Xiaoxia Liu
  • Publication number: 20140274701
    Abstract: Novel 4-amino-6-(heterocyclic)picolinic acids and their derivatives and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives are useful to control undesirable vegetation.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Lindsey G. Fischer, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbert M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall
  • Patent number: 8815864
    Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: August 26, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Elke Langkopf, Holger Wagner
  • Patent number: 8809545
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 19, 2014
    Assignee: Novartis AG
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • Patent number: 8809376
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: August 19, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Stefan Peters
  • Publication number: 20140228408
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and respiratory diseases.
    Type: Application
    Filed: August 31, 2012
    Publication date: August 14, 2014
    Applicant: AMAKEM NV
    Inventors: Jo Alen, Sandro Boland, Arnaud Pierre, Jean Bourin, Olivier Defert, Dirk Leysen
  • Patent number: 8796312
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: August 5, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • Publication number: 20140213591
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine 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: December 23, 2013
    Publication date: July 31, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 8791157
    Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.
    Type: Grant
    Filed: April 1, 2013
    Date of Patent: July 29, 2014
    Assignee: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael Eissenstat, Dehui Duan, Ji-Hye Kang
  • Patent number: 8765791
    Abstract: The present invention relates to methods for treating cancer by administering a therapeutically effective amount of compound of formula (I), such as selective NPY5R antagonist MK-0557 (trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1?-cyclohexane]-4?-carboxamide), or a pharmaceutically acceptable salt thereof, to a subject in need thereof The methods can further comprise administering a chemotherapeutic agent to the subject in need thereof.
    Type: Grant
    Filed: March 10, 2009
    Date of Patent: July 1, 2014
    Assignee: University Health Network
    Inventor: Guohua Pan
  • Publication number: 20140179735
    Abstract: A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.
    Type: Application
    Filed: April 25, 2012
    Publication date: June 26, 2014
    Inventors: Zhong-Yin Zhang, Yantao He, Li-Fan Zeng
  • Publication number: 20140175419
    Abstract: A compound represented by the following formula (1). In the formula, A1 is O, S, Si(Ar1)(Ar2), P(?O)(Ar3)(Ar4), a substituted or unsubstituted arylene group including 6 to 30 ring carbon atoms, or a substituted or unsubstituted heteroarylene group including 5 to 30 ring atoms.
    Type: Application
    Filed: September 11, 2012
    Publication date: June 26, 2014
    Inventors: Yuki Nakano, Kei Yoshida, Hideaki Nagashima, Ryohei Hashimoto
  • Publication number: 20140167007
    Abstract: A pyrene-based compound and an organic light-emitting diode including the pyrene-based compound are provided.
    Type: Application
    Filed: October 8, 2013
    Publication date: June 19, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jun-Ha Park, Eun-Young Lee, Chang-Ho Lee, Jong-Hyuk Lee
  • Publication number: 20140171642
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.
    Type: Application
    Filed: February 19, 2014
    Publication date: June 19, 2014
    Applicant: BIONOMICS LIMITED
    Inventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
  • Publication number: 20140163025
    Abstract: The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R1 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 12, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Elke LANGKOPF, Holger WAGNER