Isoquinolines (including Hydrogenated) Patents (Class 514/253.05)
  • Patent number: 11229644
    Abstract: The present disclosure relates to methods of initiating brexpiprazole treating in patients with schizophrenia or major depressive disorder. The present disclosure further relates to modified dosing regimens for obese patients and/or patients that are CYP2D6 poor metabolizers. In embodiments, the modified dosing regimens administers double the daily dose while initiating treatment.
    Type: Grant
    Filed: December 31, 2020
    Date of Patent: January 25, 2022
    Assignee: LAKE O'HARA LLC
    Inventors: Sundar Srinivasan, Christina Chow
  • Patent number: 10464931
    Abstract: The present invention relates to quinolin-2(1H)-one derivatives polymorph and its process thereof. Formula (I).
    Type: Grant
    Filed: December 28, 2016
    Date of Patent: November 5, 2019
    Assignee: Honour (R&D)
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Bandi Vamsi Krishna, Kesireddy Subhash Chander Reddy, Guda Yadava Reddy
  • Patent number: 10316000
    Abstract: The present invention relates to novel fluorophores and their use in combination with novel nucleic acid molecules, called aptamers, that bind specifically to the fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: June 11, 2019
    Assignee: Cornell University
    Inventors: Samie R. Jaffrey, Jeremy S. Paige
  • Patent number: 10160778
    Abstract: This invention relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein Y1a, Y1b, Y2a, Y2b, Y3a, and Y3b are each independently selected from hydrogen and deuterium, Y4a, Y4b, Y5a, Y5b, Y6a, Y6b, Y7a, Y7b, Y8a, Y8b, Y9a, Y9b, Y10a, Y10b, Y11a, Y11b, Y12a, Y12b, Y13a, Y13b, Y14a, Y14b, Y15a, Y15b, Y16a, Y16b, Y17a, Y17b, Y18a, and Y18b are each deuterium, X1a, X1b, X2a, X2b, X3, X4a, X4b, X5, and X6 are each independently selected from hydrogen and deuterium; and R is CD3. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a viral DNA polymerase inhibitor.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: December 25, 2018
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Julie F. Liu
  • Patent number: 9949980
    Abstract: A method of inhibiting HPV virus infection is disclosed. In one embodiment, the method involves exposing a papillomavirus to an effective amount of a compound selected from the group consisting of Compound 13, Compound 14, and analogs of Compounds 13 and 14. In another embodiment, the method involves administering an inhibitor selected from the group consisting of Compound 13, Compound 14, and analogs of Compounds 13 and 14 to a susceptible tissue or cell.
    Type: Grant
    Filed: June 2, 2015
    Date of Patent: April 24, 2018
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Paul F. Lambert, Paul G. Ahlquist, Dohun Pyeon, Hao Shun Huang
  • Patent number: 9499525
    Abstract: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same.
    Type: Grant
    Filed: April 23, 2013
    Date of Patent: November 22, 2016
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Yamashita, Tetsuya Sato, Takuya Minowa, Yusuke Hoshika, Hidekazu Toyofuku, Tatsuya Yamaguchi, Masahiro Sota, Shuuji Kawano, Takayuki Nakamura, Ryohei Eto, Takuma Ikebuchi, Kei Moriyama, Nobuaki Ito
  • Patent number: 9408885
    Abstract: The present disclosure relates to the field of oncology, more particularly to the field of melanoma. Provided are methods of treating melanoma, particularly advanced cutaneous melanoma, with a combination of pharmaceutical agents comprising MDM4-specific antagonists (such as an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e., molecules that disrupt the interactions between p53 and MDM2 and p53 and MDM4) and one or more chemotherapeutic agents such as for example alkylating agents (i.e., Dacarbazine (DITC) or melphalan), alkylating-like agents (i.e., cisplatin or carboplatin) or mitotic inhibitors (taxanes docetaxel or paclitaxel) and PI3K-AKT, B-RAF and MEK inhibitors. Further provided are pharmaceutical formulations of MDM4-specific antagonists (be it an inhibitor of the MDM4-p53 interaction or a molecule that decreases MDM4 protein stability) or MDM4-MDM2 dual inhibitors (i.e.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: August 9, 2016
    Assignees: VIB VZW, KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D
    Inventor: Jean-Christophe Marine
  • Patent number: 9301530
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: April 5, 2016
    Assignee: Syngenta Participations AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
  • Patent number: 9206167
    Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: December 8, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Yamashita, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Hideaki Kuroda, Haruka Takahashi, Satoshi Shimizu, Tatsuyoshi Tanaka
  • Patent number: 9180127
    Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: November 10, 2015
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
  • Patent number: 9040515
    Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: May 26, 2015
    Assignee: Pfizer Inc.
    Inventors: Martin Paul Edwards, Robert Arnold Kumpf, Pei-Pei Kung, Indrawan James McAlpine, Sacha Ninkovic, Eugene Yuanjin Rui, Scott Channing Sutton, John Howard Tatlock, Martin James Wythes, Luke Raymond Zehnder
  • Publication number: 20150141424
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 21, 2015
    Inventors: Qingping ZENG, Andras TORO, John Bruce PATTERSON, Warren Stanfield WADE, Zoltan ZUBOVICS, Yun YANG, Zhipeng WU
  • Publication number: 20150133427
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: October 15, 2014
    Publication date: May 14, 2015
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Publication number: 20150099732
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
    Type: Application
    Filed: March 7, 2013
    Publication date: April 9, 2015
    Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
  • Publication number: 20150051189
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: January 23, 2013
    Publication date: February 19, 2015
    Inventors: Thierry Le Diguarher, Patrick Casara, Jérôme-Benoît Starck, Jean-Michel Henlin, James Edward Paul Davidson, James Brooke Murray, Christopher John Graham, I-Jen Chen, Olivier Geneste, John Hickman, Stéphane Depil, Arnaud Le Tiran, Miklos Nyerges, Guillaume De Nanteuil
  • Publication number: 20150031673
    Abstract: Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: July 21, 2014
    Publication date: January 29, 2015
    Inventors: Arnaud LE TIRAN, Thierry LE DIGUARHER, Jérôme-Benoît STARCK, Jean-Michel HENLIN, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL, Olivier GENESTE, Imre FEJES, Janos TATAI, Miklos NYERGES, James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN, Didier DURAND
  • Publication number: 20150018352
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 15, 2015
    Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
  • Publication number: 20150011562
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R10 and X have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 8, 2015
    Inventors: Henry Yu, Thomas E. Richardson, Pandi Bharathi, Brian H. Heasley, Matthew G. Jenks, Robert J. Foglesong
  • Publication number: 20140350014
    Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
    Type: Application
    Filed: December 12, 2012
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Daniel Ford, John Robert Porter, Michael Scott Visser, Naeem Yusuff
  • Patent number: 8889676
    Abstract: The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-ox
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: November 18, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Markus Gude, Christian Hubschwerlen, Philippe Panchaud
  • Publication number: 20140336142
    Abstract: Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and/or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and/or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.
    Type: Application
    Filed: July 30, 2014
    Publication date: November 13, 2014
    Inventors: Claire Mitchell, Alan Laties
  • Patent number: 8883792
    Abstract: The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R1 and R2 each independently represent a hydrogen atom, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like; R5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: November 11, 2014
    Assignee: D. Western Therapeutics Institute, Inc.
    Inventors: Hiroyoshi Hidaka, Kengo Sumi, Kouichi Takahashi, Yoshihiro Inoue
  • Publication number: 20140329794
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 6, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20140323482
    Abstract: The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 30, 2014
    Inventors: Yao Ma, Manami Shizuka, Timothy J. Guzi, Yuan Liu, Yuan Tian, Brian R. Lahue, Craig R. Gibeau, Gerald W. Shipps, JR., Yaolin Wang, Stephane L. Bogen, Latha G. Nair, Weidong Pan, Mark A. McCoy, Matthew E. Voss, Margarita Kirova-Snover, W. Bent Clayton
  • Patent number: 8871757
    Abstract: 6- and 7-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6- and 7-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: October 28, 2014
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Geoffrey Richard Heintzelman, Susan M. Royalty
  • Publication number: 20140315884
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 23, 2014
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Publication number: 20140296214
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: October 2, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Publication number: 20140288088
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 25, 2014
    Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
  • Publication number: 20140274960
    Abstract: The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 18, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Patent number: 8822495
    Abstract: The invention relates to azacyclyl-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the azacyclyl-substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: September 2, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
  • Publication number: 20140243333
    Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
    Type: Application
    Filed: May 13, 2014
    Publication date: August 28, 2014
    Applicants: University of Kansas, University of North Carolina
    Inventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
  • Publication number: 20140243345
    Abstract: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 28, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20140228343
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 14, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Publication number: 20140221345
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 7, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20140213580
    Abstract: Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.
    Type: Application
    Filed: June 18, 2012
    Publication date: July 31, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
  • Publication number: 20140213582
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 31, 2014
    Applicant: EPIZYME, INC.
    Inventors: KENNETH W. DUNCAN, RICHARD CHESWORTH, MICHAEL JOHN MUNCHHOF
  • Publication number: 20140206673
    Abstract: Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses for treating cancers are also provided.
    Type: Application
    Filed: June 18, 2012
    Publication date: July 24, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
  • Publication number: 20140206689
    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: March 21, 2014
    Publication date: July 24, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
  • Patent number: 8785446
    Abstract: Patients are subject to a post-seizure treatment regime to separately inhibitor consecutive targets of an epileptogenic cascade comprising neurotransmitter receptor signaling, kinase/phosphatase activity, protein translation, and apoptosis or inflammation.
    Type: Grant
    Filed: January 17, 2010
    Date of Patent: July 22, 2014
    Assignee: Children's Medical Center Corporation
    Inventors: Frances E. Jensen, Sanjay N. Rakhade
  • Publication number: 20140179667
    Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Applicant: PFIZER INC.
    Inventors: Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCAPLINE, Sacha NINKOVIC, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES, Luke Raymond Zehnder
  • Publication number: 20140179634
    Abstract: The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 3, 2014
    Publication date: June 26, 2014
    Applicant: NOVARTIS AG
    Inventors: Nigel Graham COOKE, Rita RAMOS, Karen KAMMERTOENS, Maurice VAN EIS
  • Publication number: 20140163039
    Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: November 25, 2013
    Publication date: June 12, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Nobuaki ITO, Shin MIYAMURA, Kunio OSHIMA, Jun MATSUBARA, Hideaki KURODA, Haruka TAKAHASHI, Satoshi SHIMIZU, Tatsuyoshi TANAKA
  • Publication number: 20140148436
    Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicant: Array BioPharma, Inc.
    Inventors: Ian S. Mitchell, Keith L. Spencer, Peter Stengel, Yongxin Han, Nicolas C. Kallan, Mark Munson, Guy P.A. Vigers, James Blake, Anthony Piscopio, John Josey, Scott Miller, Dengming Xiao, Rui Xu, Chang Rao, Bing Wang, April L. Bernacki
  • Publication number: 20140135327
    Abstract: This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are accordingly expected to be useful for their anti-proliferative activity and in methods of treatment of the human or animal body, for example in preventing or inhibiting tumour growth and metastasis in cancers. The invention also relates to processes for the manufacture of the compounds defined herein, or pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 15, 2014
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Ronald Ernest Grigg, Martyn Inman, Graham Packham
  • Patent number: 8697703
    Abstract: The present invention relates to novel piperazine compounds; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial and to treat diseases for which blocking the Cav2.2 and Cav3.2 calcium channels is beneficial, e.g. to treat pain.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: April 15, 2014
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Jag Paul Heer, Andrew Peter Cridland, David Norton
  • Patent number: 8685981
    Abstract: Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: wherein A is selected from among a 3- to 10-membered heterocyclyl group, B is selected from among an amino group, and X is selected from N and CH.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: April 1, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Daigo Asano
  • Publication number: 20140088076
    Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
    Type: Application
    Filed: October 31, 2013
    Publication date: March 27, 2014
    Applicant: Genentech, Inc.
    Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel S. Kintz, Hans Edward Purkey
  • Publication number: 20140088057
    Abstract: A method of treating pre-term labor in pregnant human patient expressing melatonin receptors in her myometrial cells comprises administering an inhibitor of MT2R, an inhibitor of protein kinase C, an inhibitor of phospholipase C, or a combination thereof to the patient.
    Type: Application
    Filed: May 17, 2013
    Publication date: March 27, 2014
    Applicant: The Florida State University Research Foundation, Inc.
    Inventor: James Olcese
  • Publication number: 20140045846
    Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 13, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
  • Publication number: 20140038986
    Abstract: The invention provides methods of monitoring differential gene expression of biomarkers to determine patient sensitivity to Human Double Minute inhibitors (MDM2i), methods of determining the sensitivity of a cell to an MDM2i by measuring biomarkers and methods of screening for candidate MDM2i.
    Type: Application
    Filed: July 25, 2013
    Publication date: February 6, 2014
    Inventors: Swann Gaulis, Sebastien Jeay