Additional Hetero Ring Which Is Not Part Of The Bicyclo Ring System Patents (Class 514/414)
  • Patent number: 10279044
    Abstract: Aspects of the present disclosure generally relate to compounds for targeting and healing bone fractures. Some of these compounds include a negatively charged oligopeptide comprising an acidic oligopeptide, a linker, which may be hydrolyzable or may be a substrate for the protease cathepsin K, and at least one molecule that promotes bone healing. In some compounds the molecule that promotes bone healing is an anabolic compound that inhibits GSK3?, in some compounds the molecule that promotes the healing of bone fracture is a pro-inflammatory agent such as PGE1. Other embodiments include methods of treating a bone fracture comprising administering a therapeutic amount of any one of the compounds disclosed herein.
    Type: Grant
    Filed: May 29, 2016
    Date of Patent: May 7, 2019
    Assignees: Purdue Research Foundation, University of Utah Research Foundation
    Inventors: Stewart Andrew Low, Philip S. Low, Christopher Galliford, Jindrich Kopecek, Jiyan Yang
  • Patent number: 10266490
    Abstract: Radioprotector compounds including 3,3?-diindolylmethane (DIM) analogs, are provided. Further provided are methods for their use in reducing or preventing radiation damage, killing a tumor cell and protecting a non-tumor cell, and treating cancer.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: April 23, 2019
    Assignee: Georgetown University
    Inventors: Eliot M. Rosen, Milton Brown, Saijun Fan, Thomas Walls, Kathryn E. Ditmer
  • Patent number: 10206900
    Abstract: Disclosed herein are methods for treatment for fibrosis, ocular pathologies associated with fibrosis, including proliferative vitreoretinopathy (PVR) by inhibiting the activity of activated transforming growth factor ? activated kinase 1 (TAK1), or activation thereof. Pharmaceutical compositions for use in the described treatments are also provided.
    Type: Grant
    Filed: March 29, 2016
    Date of Patent: February 19, 2019
    Assignee: Mor Research Applications Ltd.
    Inventors: Ayala Pollack, Zeev Dvashi
  • Patent number: 10149833
    Abstract: The present invention provides a composition comprising an indirubin derivative for stimulating longitudinal bone growth. Because the composition for stimulating longitudinal bone growth according to the present invention is shown to be effective in longitudinal bone growth, it may be used not only as a composition for stimulating longitudinal bone growth, but also as a pharmaceutical composition for treating or preventing short stature, microplasia, dwarfism, or precocious puberty.
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: December 11, 2018
    Assignee: Industry-Academic Cooperation Foundation, Yonsei University
    Inventors: Kang-Yell Choi, Hyun-Yi Kim, Sehee Choi
  • Patent number: 10071979
    Abstract: The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: September 11, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, Cristian Harrison, Benjamin Joseph Littler, Peter Jamison Rose, Robert Michael Hughes, Young Chun Jung, David Andrew Siesel, Elaine Chungmin Lee, Daniel T. Belmont, William A. Nugent
  • Patent number: 10022352
    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: Grant
    Filed: March 23, 2016
    Date of Patent: July 17, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason McCartney, Mehdi Michel Djamel Numa
  • Patent number: 9969685
    Abstract: Compounds according to formula (I) or (II), wherein R1, R2, and R3 are as defined in the specification, are versatile intermediates for the synthesis of DNA minor groove binder-alkylators having a cyclopropapyrroloindole (CPI) or seco-CPI alkylating subunit.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: May 15, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventor: Michael Anthony Schmidt
  • Patent number: 9969686
    Abstract: Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: May 15, 2018
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Weiping Tang, Xiaoxun Li, Dongxu Shu, Gabrielle N. Winston-McPherson
  • Patent number: 9834530
    Abstract: Disclosed are a 3-furyl-2-cyano-2-acrylamide derivative with epidermal growth factor receptor (EGFR) inhibitory activity and pharmaceutical acceptable salt thereof, together with preparation method thereof, pharmaceutical composition comprising the compound, and application of the compound in treating senile dementia (AD). The new compound is shown as formula I, wherein R1 is selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl and C3-C6 cycloalkyl; R2 is selected from the group consisting of alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, aralkyl and heteroaralkyl; X is selected from the group consisting of CH2, NH, O and S; m and n are all integers greater than or equal to zero.
    Type: Grant
    Filed: June 1, 2016
    Date of Patent: December 5, 2017
    Assignee: Jenkem Technology Co., Ltd. (Beijing)
    Inventors: Zewang Feng, Jianhuan Jia, Yan Liu, Zhenguo Wang, Xuan Zhao
  • Patent number: 9834801
    Abstract: Provided are methods for synthesizing compounds, including chiral kynurenine compounds. The methods are suitable for large-scale manufacture and produce the chiral kynurenines compounds in high chemical purity and high chiral purity.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 5, 2017
    Assignee: VISTAGEN THERAPEUTICS, INC.
    Inventors: Stefan Abele, Klaus Laue, Roland A. Breitenmoser
  • Patent number: 9827196
    Abstract: The present invention relates to the use of pharmaceutical preparations comprising paclitaxel for administration to a human patient in need thereof.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: November 28, 2017
    Assignee: SynCore Biotechnology Co., Ltd.
    Inventors: Axel Mescheder, Matthias Karrasch
  • Patent number: 9655882
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: May 23, 2017
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald J. Zack, Zhiyong Yang, Cynthia Berlinicke, Harry Quigley
  • Patent number: 9642831
    Abstract: The invention provides for compounds of formula (I) wherein R1, X, Y, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, and R? have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: May 9, 2017
    Assignees: AbbVie S.á.r.l., Galapagos NV
    Inventors: Robert J. Altenbach, Andrew Bogdan, Stephen N. Greszler, John R. Koenig, Philip R. Kym, Bo Liu, Xenia B. Searle, Eric Voight, Xueqing Wang, Ming C. Yeung
  • Patent number: 9642851
    Abstract: The present invention relates to a compound represented by general formula (I), a method for preparing said compound, a pharmaceutical formulation containing said compound, and the use of said compound in manufacture of a medicament for treating or preventing the fibrous degeneration disease and treating the excessive proliferation disease: wherein ring A, X, R1, R2, R3, R4, R5, R6, R7, R8, R9, a, b and n are defined as those in the description.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: May 9, 2017
    Assignee: KBP BioSciences Co., Ltd.
    Inventors: Hoyin Lo, Aichen Wang, Qian Zhang
  • Patent number: 9604968
    Abstract: The present invention relates to pure crystalline Form II of an L-malic acid salt of sunitinib and a process for its preparation. The invention further provides crystalline Form II of an L-malic acid salt of sunitinib having a purity of at least 97.0%. The invention also provides crystalline Form II of an L-malic acid salt of sunitinib substantially free of an anti-oxidant. The invention also provides crystalline Form II of L-malic acid salt of sunitinib which remains chemically pure on storage at 25° C.±2° C. and 40° C.±2° C. at a relative humidity of 60%±5% and 75%±5%, respectively, for at least 1 month.
    Type: Grant
    Filed: January 6, 2014
    Date of Patent: March 28, 2017
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Hari Babu Matta, Mahavir Singh Khanna, Mohan Prasad
  • Patent number: 9447057
    Abstract: One embodiment of the invention relates to treating diseases associated with increased urease enzyme activity comprising administering an effective amount of a compound selected from a group consisting of 28 thiazoles Schiff bases. Kinetic studies were performed on ten (10) of the most active compounds.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: September 20, 2016
    Inventors: Muhammad Iqbal Choudhary, Ajmal Khan, Khalid M. Khan, Nida Ambreen, Atia-tul Wahab, Atta-ur Rahman
  • Patent number: 9433607
    Abstract: The present invention relates to ethyl(2-methyl-3{(E)-[(naphtho[2,1-b]furan-2-ylcarbonyl)hydrazono]methyl}-1H-indole-1-yl)acetate, the novel mitosis inhibitor. The said ethyl(2-methyl-3{(E)-[(naphtho[2,1-b]furan-2-ylcarbonyl)hydrazono]methyl}-1H-indole-1-yl)acetate not only induces apoptosis by inhibiting tubulin polymerization in the course of mitosis but also displays an excellent anticancer effect in the multi-drug resistant cancer cells, so that it can be effectively used for the treatment of cell proliferative disease including various cancers.
    Type: Grant
    Filed: March 6, 2015
    Date of Patent: September 6, 2016
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Bo Yeon Kim, Krisada Sakchaisri, Sun Ok Kim, Ramegowda Thimmegowda Naraganahalli, Nak Kyun Soung, Jong Seog Ahn, Joonsung Hwang, In Ja Ryoo, Jae-Hyuk Jang
  • Patent number: 9364001
    Abstract: A quaternary fungicide mixture for controlling diseases of turfgrass and/or ornamentals.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: June 14, 2016
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: Allan S. Las, Jerry L. Corbett, Paul R. Moore
  • Patent number: 9295666
    Abstract: Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, the compositions comprise an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: March 29, 2016
    Assignee: Spectrum Pharmaceuticals, Inc.
    Inventors: Bastiaan Nuijen, Ernie Pfadenhauer, Jos H. Beijnen, Dorla Mirejovsky, Guru Reddy, Luigi Lenaz
  • Patent number: 9290479
    Abstract: The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: March 22, 2016
    Assignee: Zoetis Services LLC
    Inventors: Michael Hawley, Changquan Calvin Sun
  • Patent number: 9278955
    Abstract: The present invention relates to an ascorbic acid salt of sunitinib and a process for its preparation. The present invention further provides a crystalline Form I of an L-ascorbic acid salt of sunitinib.
    Type: Grant
    Filed: January 6, 2014
    Date of Patent: March 8, 2016
    Assignee: SUN PHARMACEUTICAL INDUSTRIES LIMITED
    Inventors: Hari Babu Matta, Mahavir Singh Khanna, Mohan Prasad
  • Patent number: 9271960
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Grant
    Filed: January 26, 2015
    Date of Patent: March 1, 2016
    Assignee: PTC Therapeutics, Inc.
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Patent number: 9144594
    Abstract: This invention relates generally to the treatment of cathepsin or dynamin mediated diseases, such as proteinuria, cancer, and cognitive disease and related products. Diagnostic and other assays are also provided, as well as methods for podocyte cell gene transfer.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: September 29, 2015
    Assignees: University of Miami, The General Hospital Corporation
    Inventors: Jochen Reiser, Sanja Sever
  • Publication number: 20150148349
    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: Application
    Filed: June 27, 2013
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Patent number: 9040508
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 9029406
    Abstract: The present application relates to new derivatives, substituted on the N terminus by a carboxyalkyl group, of monomethylauristatin E and monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and to the use of these derivatives for producing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments may be applied as a monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: May 12, 2015
    Assignee: Seattle Genetics, Inc
    Inventors: Hans-Georg Lerchen, Sherif El Sheikh, Beatrix Stelte-Ludwig, Joachim Schuhmacher, Mark Gnoth
  • Publication number: 20150126559
    Abstract: The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 7, 2015
    Applicant: UNIVERSITA DEGLI STUDI DI FERRARA
    Inventors: Jan Balzarini, Wim Dehaen, Joice Thomas, Sandra Liekens, Romeo Romagnoli, Pier Giovanni Baraldi
  • Publication number: 20150125389
    Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R4, R5, X1, X2, X3 and X4 are as defined herein, and wherein the compound comprises at least one F, Cl, Br, I or 123I moiety, are provided. Uses of such compounds for imaging diagnostics in cancer and therapeutics methods for treatment of subjects in need thereof, including prostate cancer as well as methods and intermediates for preparing such compounds are also provided.
    Type: Application
    Filed: September 9, 2014
    Publication date: May 7, 2015
    Applicants: THE UNIVERSITY OF BRITISH COLUMBIA, BRITISH COLUMBIA CANCER AGENCY BRANCH
    Inventors: Raymond John Andersen, Carmen Adriana Banuelos, Javier GARCIA FERNANDEZ, Yusuke IMAMURA, Jian KUNZHONG, Nasrin R. MAWJI, Marianne Dorothy Sadar, Jun Wang, Amy (Hsing Chen) Tien
  • Patent number: 9023885
    Abstract: The invention relates to pharmaceutical compositions and methods of treating inflammatory-related diseases associated with pro-inflammatory cytokine expression and/or reduced expression of anti-inflammatory cytokines. The method typically comprises administration of one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA. Preferably the pharmaceutical composition comprises one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, an anti-inflammatory agent, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: May 5, 2015
    Assignee: Natrogen Therapeutics International, Inc.
    Inventors: Longgui Wang, Xiao Mei Liu, Lian Mo, Simon K. Mencher, James P. McCarron, Jr.
  • Publication number: 20150119441
    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: November 4, 2014
    Publication date: April 30, 2015
    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
  • Patent number: 9018211
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Yuping Zhu, Aurash Shahripour, Haifeng Tang, Lihu Yang, Shawn P. Walsh, Nardos H. Teumelsan
  • Patent number: 9018242
    Abstract: Provided are acid addition salts of (Z)—N-[2-(diethylamino)ethyl]-2-methyl-7-(1,2 -dihydro-5-fluoro-2-oxo-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indol-3-carboxamide, wherein the salt comprising at least one of a number of salts including L-malate, hydrochloride, phosphate, L-tartrate, benzenesulfonate, sulfate, methanesulfonate, succinate, citrate, fumarate, p-toluenesulfonate, hydrobromate, L-mandelate, lactate, acetate or maleate salt. Also provided is a pharmaceutical composition comprising the salt compounds, and a method of treatment by administering a therapeutically effective amount of the salt compounds as preparation of medicaments.
    Type: Grant
    Filed: September 11, 2013
    Date of Patent: April 28, 2015
    Assignee: Jiangsu Simcere Pharmaceutical R&D Co., Ltd
    Inventors: Feng Tang, Qiu Jin, Wei Li, Tian Zhu, Yang Hu, Feng Shao
  • Publication number: 20150110878
    Abstract: The disclosure provides nanoparticles of indirubin and methods of making and using these particles for the treatment of cancer, neurodegenerative disorders and inflammatory diseases. The effective average particle size of the nanoparticles is less than 2000 nm.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 23, 2015
    Applicant: Phosphorex, Inc.
    Inventor: Bin Wu
  • Publication number: 20150110713
    Abstract: A method for treating cancer, preventing cancer or delaying the progression of a cancer in an animal or human comprising the step of: administering to the animal or the human having a cancer a composition in an amount effective to treat cancer, prevent cancer or delay the progression of cancer in the animal or the human. The composition comprises a pharmaceutically acceptable excipient, and ascorbate which is joined to a carrier structure containing an anti-cancer active agent, said carrier structure being capable of releasing the anti-cancer agent in the presence of a reactive oxygen species.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Anthony Manganaro, Karen Rockwell
  • Publication number: 20150111940
    Abstract: The present invention relates to an ascorbic acid salt of sunitinib and a process for its preparation. The present invention further provides a crystalline Form I of an L-ascorbic acid salt of sunitinib.
    Type: Application
    Filed: January 6, 2014
    Publication date: April 23, 2015
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Hari Babu MATTA, Mahavir Singh KHANNA, Mohan PRASAD
  • Publication number: 20150111890
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 23, 2015
    Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
  • Patent number: 9012659
    Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and R3 are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: April 21, 2015
    Assignee: Johannes Gutenberg—Universitat Mainz
    Inventors: Gerd Dannhardt, Jan-Peter Kramb, Stanislav Plutizki
  • Publication number: 20150105375
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
  • Publication number: 20150104387
    Abstract: Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.
    Type: Application
    Filed: April 2, 2014
    Publication date: April 16, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN G. POMPER, RONNIE C. MEASE, YING CHEN, Sangeeta Ray
  • Patent number: 9006256
    Abstract: The present invention provides pharmaceutical compositions and therapeutic methods for treating diseases such as multiple endocrine neoplasia type IIA, multiple endocrine neoplasia type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. The therapeutic methods and pharmaceutical compositions use a RET kinase inhibiting substance, such as 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and pharmacologically acceptable salts thereof, and involve a step of administering the RET kinase inhibiting substance to a patient.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: April 14, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Junji Matsui
  • Publication number: 20150099012
    Abstract: The present invention relates to a method for increasing retrovirus transcription in an infected eukaryotic cell, comprising increasing Wnt pathway signaling in said cell such that transcription of said retrovirus is increased. Also, the present invention relates to a method of treating a subject infected with a retrovirus, said method comprising administering to said subject an activator of the Wnt pathway in an amount that increased Wnt pathway signaling in resting memory CD4+ T cells of said subject such that the retroviral long terminal repeat (LTR) in said cells is activated or de-repressed.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 9, 2015
    Inventor: Tokameh Mahmoudi
  • Publication number: 20150099746
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 9, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Publication number: 20150094304
    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: December 11, 2014
    Publication date: April 2, 2015
    Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
  • Publication number: 20150093391
    Abstract: A method of treating cancer or metastasis is provided involving administering at least one oncostatin M (OSM) antagonist to a subject, wherein the subject has been diagnosed with cancer. Administration of an OSM antagonist such as a small molecule pharmaceutical is provided as well as an anti-OSM antibody, an anti-OSM aptamer, and an OSM mRNA antagonist. The OSM antagonists were found to inhibit or prevent tumor cell detachment, proliferation and metastasis in several cancer types.
    Type: Application
    Filed: September 5, 2014
    Publication date: April 2, 2015
    Applicant: BOISE STATE UNIVERSITY
    Inventors: Cheryl Jorcyk, Dong Xu
  • Publication number: 20150094330
    Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.
    Type: Application
    Filed: September 26, 2014
    Publication date: April 2, 2015
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 8993615
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Grant
    Filed: August 8, 2009
    Date of Patent: March 31, 2015
    Assignee: The Johns Hopkins University
    Inventors: Donald J. Zack, Zhiyong Yang, Cynthia Berlinicke, Harry Quigley
  • Publication number: 20150087687
    Abstract: The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutically active agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to therapeutically active agents selected from the group consisting of: (i) indirubin; (ii) an analog of indirubin; (iii) a derivative of indirubin or of an analog of indirubin; and (iv) a pharmaceutical composition comprising indirubin, an analog of indirubin, or a derivative of indirubin or of an analog of indirubin, especially meisoindigo.
    Type: Application
    Filed: March 22, 2013
    Publication date: March 26, 2015
    Inventor: Dennis BROWN
  • Patent number: 8987320
    Abstract: The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1, 2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.
    Type: Grant
    Filed: February 6, 2012
    Date of Patent: March 24, 2015
    Assignee: Zoetis LLC
    Inventors: Changquan C. Sun, Michael Hawley
  • Patent number: 8986993
    Abstract: A SMAC mimetic and pharmaceutical compositions thereof and methods of use.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: March 24, 2015
    Assignee: TetraLogic Pharmaceuticals Corporation
    Inventors: Stephen M. Condon, Yijun Deng, Matthew G. LaPorte, Susan R. Rippin
  • Publication number: 20150079111
    Abstract: Mechanisms for complications of renal failure and processes for treating the same are disclosed. They include contacting a biological fluid (e.g. blood) with a filter body, the filter body having immobilized thereon either a CD36 receptor or a CD36 receptor fragment or a SCARB1 receptor or a SCARB1 receptor fragment, the blood having a reduced quantity of oxidatively modified proteins after contacting the filter body. They also include administering an antagonist drug to a patient that blocks the binding activity of the RAGE receptor or the CD36 receptor or the SCARB1 receptor. Diagnostic methods are also provided.
    Type: Application
    Filed: June 5, 2013
    Publication date: March 19, 2015
    Inventor: Jonas AXELSSON