Four Or More Ring Nitrogens In The Tricyclo Ring System Patents (Class 544/251)
  • Patent number: 11926628
    Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
    Type: Grant
    Filed: June 21, 2022
    Date of Patent: March 12, 2024
    Assignee: Gilead Sciences, Inc.
    Inventors: Julian A. Codelli, Michael Graupe, Juan A. Guerrero, Jesse M. Jacobsen, Tetsuya Kobayashi, Jonathan William Medley, Yasamin Moazami, Leena B. Patel, Jie Xu, Suet C. Yeung
  • Patent number: 11884669
    Abstract: The pyrrolo[3,2-c][1,7]naphthyridine-2-carboxylic acid compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
    Type: Grant
    Filed: September 13, 2023
    Date of Patent: January 30, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Michelyne Haroun, Christophe Tratrat
  • Patent number: 11661422
    Abstract: The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
    Type: Grant
    Filed: August 26, 2021
    Date of Patent: May 30, 2023
    Assignee: Incyte Corporation
    Inventors: Kai Liu, Brent Douty, Daniel Levy, Liangxing Wu, Wenqing Yao, Eddy W. Yue
  • Patent number: 11591661
    Abstract: An example system for purifying a supply stream including lactose includes a clarification system configured to separate insoluble impurities from the stream to produce a clarified stream. The system includes an adsorption system fluidically coupled to the clarification system. The adsorption system includes an adsorbent resin configured to purify the clarified stream. An example technique for purifying a supply stream including lactose includes separating insoluble impurities from the supply stream to produce a clarified stream and passing the clarified stream over an adsorbent resin to produce a decolorized stream.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: February 28, 2023
    Assignee: Keller Technologies, Inc.
    Inventors: A. Kent Keller, James P. Mullen, Eric A. Keller
  • Patent number: 11508914
    Abstract: A condensed cyclic compound represented by Formula 1: wherein in Formula 1, Ar1 and R1 to R8 are the same as described in the specification.
    Type: Grant
    Filed: November 30, 2018
    Date of Patent: November 22, 2022
    Assignees: SAMSUNG ELECTRONICS CO., LTD., SAMSUNG SDI CO., LTD.
    Inventors: Hyunjung Kim, Miyoung Chae, Eunsuk Kwon, Sangmo Kim, Soonok Jeon, Yeonsook Chung, Dalho Huh, Youngseok Park, Youngmok Son
  • Patent number: 11377451
    Abstract: The present disclosure relates to compounds, compositions and methods for treating cancer, including compounds that are capable of penetrating the blood brain barrier to modulate the activity of EGFR tyrosine kinase. The disclosure further relates to methods of treating cancer in the brain, including glioblastoma and other EGFR mediated cancers. The disclosure further relates to methods of treating cancers such as glioblastoma and other EGFR mediated cancers that have been determined to have altered glucose metabolism in the presence of inhibitors. The present disclosure also provides methods of administering to a subject a glucose metabolism inhibitor and a cytoplasmic p53 stabilizer.
    Type: Grant
    Filed: September 14, 2021
    Date of Patent: July 5, 2022
    Assignee: The Regents of the University of California
    Inventors: David A. Nathanson, Michael E. Jung, Jonathan Tsang, Lorenz Urner, Peter M. Clark, Timothy F. Cloughesy, Gyudong Kim
  • Patent number: 11365196
    Abstract: An azatricyclic compound (as represented by Formula I) which acts as an inhibitor of fibroblast growth factor receptors (FGFR), as well as a pharmaceutical composition thereof, a preparation method, and a use therefor in the treatment of FGFR-mediated diseases are provided. The azatricyclic compound exerts an effect by means of participating in the regulation of a plurality of processes such as cell proliferation, apoptosis, migration, neovascularization, and the like.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: June 21, 2022
    Assignee: Betta Pharmaceuticals Co., Ltd.
    Inventors: Xiaofeng Xu, Jiabing Wang, Lieming Ding, Xiangyong Liu
  • Patent number: 11267815
    Abstract: The present invention discloses a class of amino-substituted nitrogen-containing fused ring compounds, a preparation method therefor, and a use thereof. The structure of the amino-substituted nitrogen-containing fused ring compounds of the present invention is as shown in formula (I) below, and each group therein is as defined in the specification. The amino-substituted nitrogen-containing fused ring compounds of the present invention are novel specific FGFR kinase inhibitors, having excellent inhibitory activity for FGFR-related tumor cell proliferation, and is applicable to the treatment of diseases such as tumors associated with FGFR kinase mutations or abnormal expressions.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: March 8, 2022
    Assignee: SHANGHAI RINGENE BIOPHARMA CO., LTD.
    Inventor: Hui Wang
  • Patent number: 11220510
    Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: April 8, 2019
    Date of Patent: January 11, 2022
    Assignee: Incyte Corporation
    Inventors: Xiaozhao Wang, Peter Niels Carlsen, Chunhong He, Taisheng Huang
  • Patent number: 11168088
    Abstract: The present disclosure relates to pyridinamine-substituted heterotricyclo compounds, a preparation method thereof, and a use thereof in medicines. Specifically, a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method and a use thereof are disclosed, wherein the groups in the formula (I) are as defined in the Description and claims.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: November 9, 2021
    Inventors: Yang Liu, Jiangwei Wang, Qing Zhang, Yonggang Chen, Baoxin Xi, Wangbin Sun, Yingtao Liu, Xi Chen
  • Patent number: 11136321
    Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 27, 2020
    Date of Patent: October 5, 2021
    Assignee: Aligos Therapeutics, Inc.
    Inventor: Sandrine Vendeville
  • Patent number: 10464940
    Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.
    Type: Grant
    Filed: January 2, 2018
    Date of Patent: November 5, 2019
    Assignee: GI Therapeutics, Inc.
    Inventor: Francis Xavier Tavares
  • Patent number: 10336710
    Abstract: The present invention belongs to the pharmaceutical field, and relates to a preparation method for a series of benzimidazole derivatives, their pharmaceutical salts and pharmaceutically acceptable prodrugs, a pharmaceutical composition containing the derivatives, and the uses of the derivatives and pharmaceutical composition in the preparation of antigout drugs and in the treatment of related diseases.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: July 2, 2019
    Inventors: Yan Yang, Wenfeng Wang, Zhankun Hu, Xiangyu Sun, Huijun Yin, Xuewei Tian
  • Patent number: 10113065
    Abstract: A two-photon absorbing (TPA) compound is provided, along with a method of making same. The TPA compound has a general structural formula: where A is an acceptor moiety that is connected to m number of diarylaminofluorene arms (m=1-3); in each diarylaminofluorene arms, R is selected from linear or branched alkyl chains having a general formula CnH2n+1, where n is in a range from 2 to 25; where R1, R2, and R3 are independently selected from H or C1-C4 alkyls; where R4 is selected from C1-C5 alkyls; and wherein R5 through R10 are independently selected from H, alkoxyls, alkyls, or aryls. A may be benzothiazol-2-yl, benzo[1,2-d:4,5-d?]bisthiazole-2,6-diyl, thiazolo[5,4-d]thiazole-2,5-diyl-, 1,3,5-triazine-2,4,6-triyl, 1,3,5-triazine-2,4,6-triyl, benzo[1,2-d:3,4-d?:5,6-d?]tristhiazole-2,5,8-triyl-, or dithieno[3,2-b:2?,3?-d]thiophene-2,6-diyl-.
    Type: Grant
    Filed: September 21, 2017
    Date of Patent: October 30, 2018
    Inventors: Loon-Seng Tan, Ramamurthi Kannan
  • Patent number: 9856268
    Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.
    Type: Grant
    Filed: November 10, 2016
    Date of Patent: January 2, 2018
    Assignee: G1 Therapeutics, Inc.
    Inventor: Francis Xavier Tavares
  • Patent number: 9802937
    Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
    Type: Grant
    Filed: April 23, 2012
    Date of Patent: October 31, 2017
    Assignee: ORIGENIS GMBH
    Inventors: Michael Thormann, Andreas Treml, Michael Almstetter, Nadine Traube
  • Patent number: 9745316
    Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.
    Type: Grant
    Filed: December 29, 2015
    Date of Patent: August 29, 2017
    Assignee: G1 Therapeutics, Inc.
    Inventor: Francis Xavier Tavares
  • Patent number: 9637491
    Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: May 2, 2017
    Assignee: ORIGENIS GMBH
    Inventors: Michael Almstetter, Michael Thormann, Andreas Treml, Nadine Traube
  • Patent number: 9579351
    Abstract: Cells derived from postpartum placenta and methods for their isolation are provided by the invention. The invention further provides cultures and compositions of the placenta-derived cells. The placenta-derived cells of the invention have a plethora of uses, including but not limited to research, diagnostic, and therapeutic applications.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: February 28, 2017
    Assignee: DePuy Synthes Products, Inc.
    Inventors: Anthony J. Kihm, Ian Ross Harris, Sanjay Mistry, Alexander M. Harmon, Darin J. Messina, Agnieszka Seyda, Chin-Feng Yi, Anna Gosiewska
  • Patent number: 9184399
    Abstract: Novel asymmetric host compounds containing an electron-transport moiety, a hole-transport moiety, an aromatic spacer, and a triaryl silane group are provided. These compounds are useful materials that can be incorporated into OLED devices.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: November 10, 2015
    Assignee: Universal Display Corporation
    Inventors: Alexey Dyatkin, Lichang Zeng, Chuanjun Xia
  • Patent number: 9090623
    Abstract: The present invention relates to a compound [4-(2-amino-10-methyl-4-oxo-6,7,8,9-tetrahydro-4a,7-cycloimino-pyrimido[4,5-b][1,4]diazepine-5(4H)-yl)benzoyl]-glutamate (JK12A for short) with the structure in Formula I. The present invention also relates to the crystal form and salt of the compound JK12A, and preparation method and applications thereof. The compound JK12A of the present invention can be used to prepare drugs as an active ingredient for medicament or food additives.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: July 28, 2015
    Assignee: Lianyungang Jinkang Hexin Pharmaceutical Co., Ltd.
    Inventors: Yongzhi Cheng, Zhi Cheng, Min Zhou, Zhaojun Wang, Huizhen Li, Shenggang Fan
  • Publication number: 20150133426
    Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
  • Publication number: 20150126502
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 7, 2015
    Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
  • Publication number: 20150126449
    Abstract: The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Jorma Haßfeld, Tom KINZEL, Johannes Köbberling, Yolanda CANCHO GRANDE, Kristin BEYER, Susanne Röhrig, Maria Köllnberger, Michael SPERZEL, Nils BURKHARDT, Karl-Heinz SCHLEMMER, Christian STEGMANN, Joachim SCHUHMACHER, Matthias WERNER, Manuel ELLERMANN
  • Patent number: 9012466
    Abstract: The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: April 21, 2015
    Assignee: ArQule Inc.
    Inventors: Nivedita Namdev, Jianqiang Wang, Mark Ashwell, Audra Dalton, Jason Hill, Eugene Kelleher, Jeffrey Link, Rocio Palma, Sudharshan Eathiraj, Neil Westlund, Hui Wu, Rui-Yang Yang
  • Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Patent number: 9006258
    Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: April 14, 2015
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Allen A. Fienberg, Sharon Mates, Lawrence P. Wennogle
  • Patent number: 9006226
    Abstract: The present invention relates to dihydropteridinones, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: April 14, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Christian Eickmeier, Claudia Heine, Niklas Heine, Alexander Weber
  • Publication number: 20150099879
    Abstract: Methods for producing phycotoxins from natural sources, wherein the phycotoxins have a definite compositional profile are described herein. In one embodiment, the phycotoxins are produced by cyanobacteria. In one embodiment, the phycotoxins are produced by continuously culturing cyanobacteria under strictly controlled conditions in order to produce a definite compositional profile. In another embodiment, organic nutrients are added to the culture that allows for higher concentrations of neosaxitoxin and saxitoxin or gonyaulatoxins 2 and 3 per weight of the algae. The phycotoxins are isolated primarily from the bacteria but can also be isolated from the culture medium. In one embodiment, the cyanobacteria produce only neosaxitoxin and saxitoxin in a ratio of about 6:1, 5:1, 4:1, or 3:1. In a preferred embodiment, the amount of saxitoxin is less than 20% by weight of the total amount of neosaxitoxin and saxitoxin produced. In another embodiment, the cyanobacteria produce only GTX2 and GTX 3.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventor: Marcelo Santiago Logas Gonzalez
  • Publication number: 20150099878
    Abstract: Phycotoxins are purified from a mixture of phycotoxins produced in a continuous process. Cyanobacteria are produced in a continuous culture, then lyzed, the cells pelleted and extracted, and the extract purified using an organic solvent-aqueous mixture and repeated passage through a diatomaceous earth column. The column is washed with acetic acid, then the neosaxitoxin extracted with an alcohol-water mixture. The eluate is passed through activated charcoal columns, which are washed with distilled water to remove the retained pigments and impurities, the further purified by HPLC. In one embodiment, the process produces only neosaxitoxin and saxitoxin. In another embodiment, the process produces only GTX2/3.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventor: Marcelo Santiago Logas Gonzalez
  • Publication number: 20150099877
    Abstract: An electrode active material for a lithium secondary battery using a heterocyclic compound and a lithium secondary battery including the same are provided. The heterocyclic compound, which is useful as a cathode or anode active material, includes a six-membered ring and a five-membered ring containing one or more elements selected from the group consisting of nitrogen (N), oxygen (O) and sulfur (S), and the heterocyclic compound is configured such that two pairs of carbons which form double bonds with nitrogen atoms contain a functional group linked by a single bond, thus exhibiting redox activity.
    Type: Application
    Filed: January 6, 2014
    Publication date: April 9, 2015
    Applicant: AGENCY FOR DEFENSE DEVELOPMENT
    Inventors: Sanghyeon HA, Dongik CHEONG, Chanbeum PARK, Minah LEE, Jihyun HONG, Kisuk KANG
  • Patent number: 9000001
    Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2H]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-9 alkyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: April 7, 2015
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Peng Li, Haiyan Wu
  • Publication number: 20150087831
    Abstract: Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC—OR—NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam.
    Type: Application
    Filed: April 24, 2013
    Publication date: March 26, 2015
    Inventor: Francis Xavier Tavares
  • Patent number: 8980903
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: March 17, 2015
    Assignee: Amgen Inc.
    Inventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. McGee, Rajiv Sharma, Xiaodong Wang, Dustin L. McMinn, Jeffrey T. Mihalic, Jeffrey Deignan
  • Publication number: 20150065708
    Abstract: The present invention relates to a compound [4-(2-amino-10-methyl-4-oxo-6,7,8,9-tetrahydro-4a,7-cycloimino-pyrimido[4,5-b][1,4]diazepine-5(4H)-yl)benzoyl]-glutamate (JK12A for short) with the structure in Formula I. The present invention also relates to the crystal form and salt of the compound JK12A, and preparation method and applications thereof. The compound JK12A of the present invention can be used to prepare drugs as an active ingredient for medicament or food additives.
    Type: Application
    Filed: April 9, 2013
    Publication date: March 5, 2015
    Inventors: Yongzhi Cheng, Zhi Cheng, Min Zhou, Zhaojun Wang, Huizhen Li, Shenggang Fan
  • Publication number: 20150057274
    Abstract: Provided herein are small molecule triazolothienopyrimidine compounds that inhibit urea transport activity of solute transporters, particularly the UT-B transporter. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating refractory edema associated with cardiovascular, renal, and metabolic diseases, disorders, and conditions.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Marc Anderson, Alan S. Verkman
  • Patent number: 8957207
    Abstract: Methods for producing phycotoxins from natural sources, wherein the phycotoxins have a definite compositional profile are described herein. In one embodiment, the phycotoxins are produced by cyanobacteria. In one embodiment, the phycotoxins are produced by continuously culturing cyanobacteria under strictly controlled conditions in order to produce a definite compositional profile. In another embodiment, organic nutrients are added to the culture that allows for higher concentrations of neosaxitoxin and saxitoxin or gonyaulatoxins 2 and 3 per weight of the algae. The phycotoxins are isolated primarily from the bacteria but can also be isolated from the culture medium. In one embodiment, the cyanobacteria produce only neosaxitoxin and saxitoxin in a ratio of about 6:1, 5:1, 4:1, or 3:1. In a preferred embodiment, the amount of saxitoxin is less than 20% by weight of the total amount of neosaxitoxin and saxitoxin produced. In another embodiment, the cyanobacteria produce only GTX2 and GTX 3.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: February 17, 2015
    Assignee: Proteus S.A.
    Inventor: Marcelo Santiago Lagos González
  • Patent number: 8952152
    Abstract: Phycotoxins are purified from a mixture of phycotoxins produced in a continuous process. Cyanobacteria are produced in a continuous culture, then lyzed, the cells pelleted and extracted, and the extract purified using an organic solvent-aqueous mixture and repeated passage through a diatomaceous earth column. The column is washed with acetic acid, then the neosaxitoxin extracted with an alcohol-water mixture. The eluate is passed through activated charcoal columns, which are washed with distilled water to remove the retained pigments and impurities, the further purified by HPLC. In one embodiment, the process produces only neosaxitoxin and saxitoxin. In another embodiment, the process produces only GTX2/3.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: February 10, 2015
    Assignee: Proteus S.A.
    Inventor: Marcelo Santiago Lagos González
  • Publication number: 20150031880
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Application
    Filed: August 5, 2014
    Publication date: January 29, 2015
    Inventors: Francis X. Tavares, Jay C. Strum
  • Publication number: 20150018343
    Abstract: The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
    Type: Application
    Filed: November 30, 2012
    Publication date: January 15, 2015
    Inventors: Dominique Swinnen, Cyril Montagne, Vincent Pomel, Anna Quattropani, Jerome Molette, Patrick Gerber
  • Publication number: 20150018361
    Abstract: The present invention relates to methylene-tetrahydrofolate for use in the treatment of cancer, based on its intrinsic antitumor activity. The cancers that may be treated include breast cancer, gastric cancer, gastrointestinal cancer, gall bladder cancer, bile duct cancer, colon cancer, rectal cancer, liver cancer, pancreatic cancer, head and neck cancer, esophageal cancer, mesothelioma cancer, lung cancer including non-small-cell lung cancer, ovarian cancer, endometrial cancer, cervical cancer, peripheral cell lymphoma (PTCL), melanoma, brain tumors, adenocarcinoma, esophageal cancer, and osteosarcoma.
    Type: Application
    Filed: January 18, 2013
    Publication date: January 15, 2015
    Applicant: ISOFOL MEDICAL AB
    Inventors: Bengt Gustavsson, Björn Carlsson
  • Publication number: 20150018348
    Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Inventor: Francis Xavier Tavares
  • Patent number: 8927562
    Abstract: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, Panduranga Adulla Reddy, M. Arshad Siddiqui
  • Patent number: 8916577
    Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: December 23, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
  • Publication number: 20140371249
    Abstract: To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Yasusi Ueda, Nobuyuki Suzuki, Hitoshi Ohki
  • Publication number: 20140371216
    Abstract: The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.
    Type: Application
    Filed: April 18, 2014
    Publication date: December 18, 2014
    Applicant: Incyte Corporation
    Inventors: Changsheng Zheng, Chu-Biao Xue, Ganfeng Cao, Michael Xia, Anlai Wang, Hai Fen Ye, Brian Metcalf
  • Publication number: 20140357606
    Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: August 15, 2014
    Publication date: December 4, 2014
    Inventor: Peng LI
  • Patent number: 8901142
    Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine and dipyrazolopyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine or dipyrazolopyrimidine compounds.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: December 2, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, M. Arshad Siddiqui, Panduranga Adulla P. Reddy, Mehul F. Patel, Yang Nan
  • Publication number: 20140350244
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Inventors: Richard V. Connors, Kang DAI, John EKSTEROWICZ, Pingchen FAN, Benjamin FISHER, Jiasheng FU, Kexue LI, Zhihong LI, Lawrence R. MCGEE, Rajiv SHARMA, Xiaodong WANG, Dustin L. MCMINN, Jeffrey T. MIHALIC, Jeffrey DEIGNAN
  • Publication number: 20140350036
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides dermatological compositions comprising a compound of formula I or mixtures of one or more compounds of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for protecting skin or DNA from photodamage or repairing photodamaged skin or DNA.
    Type: Application
    Filed: January 11, 2013
    Publication date: November 27, 2014
    Inventors: Robert Vince, Abbas Raza, Christine Dreis