Tricyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/344)
  • Patent number: 10392514
    Abstract: The present invention relates to storage-stable dye salts, solutions and compositions thereof a process for their preparation and their use for dyeing and/or printing substrates.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: August 27, 2019
    Assignee: Archroma IP GmbH
    Inventor: Friedrich Lehr
  • Patent number: 10035798
    Abstract: Disclosed is a preparation method for praziquantel and intermediates thereof. The method includes: obtaining a target product praziquantel by using ?-phenethylamine as an initial raw material through a condensation reaction with chloroacetyl chloride, a substitution reaction with ethanolamine, and an acylation reaction with cyclohexanecarbonyl chloride, followed by an oxidation reaction and cyclization reaction. Also disclosed are two key intermediates, namely, a compound of formula IV and a compound of formula V for preparing praziquantel. The preparation method is reasonable and simple in its technological design, uses moderate reaction conditions, and is economical and environmentally friendly. Additionally, the raw materials are inexpensive and easy to obtain, the key intermediates are easy to prepare, and the total reaction yield and purity of the obtained target compound praziquantel is high, so that industrialized mass production is easy to achieve.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: July 31, 2018
    Assignees: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical Industry
    Inventors: Fuli Zhang, Zhezhou Yang, Rusheng Bao, Weiwei Xu, Hua Bai
  • Patent number: 9932337
    Abstract: The present invention relates to methods for the production of enantiopure or enantioenriched Praziquantel precursors and to methods for the production of enantiopure or enantioenriched Praziquantel comprising the methods for the production of the Praziquantel precursors. The present invention further relates to compounds or intermediates useful in such methods.
    Type: Grant
    Filed: November 19, 2015
    Date of Patent: April 3, 2018
    Assignee: Merck Patent GmbH
    Inventors: David Maillard, Andreas Waechtler, Jeremy Maurin, Ewgenij Wakaresko, Christian Jasper
  • Patent number: 9802934
    Abstract: The present disclosure relates to a process and new intermediates for the synthesis of (R)-praziquantel, which is obtained through four steps in proper order, that is, condensation reaction, reduction reaction, acylation reaction and ring-closing reaction, using (1R)-2-substituted-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid as starting material. Overall, the present disclosure provides a (R)-praziquantel product with higher optical purity through a process route that is more cost effective and environmentally friendly.
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: October 31, 2017
    Assignee: TONGLI BIOMEDICAL CO., LTD.
    Inventor: Mingxin Qian
  • Patent number: 9711738
    Abstract: The design and synthesis of six nickel charge transfer (CT) complexes are described herein. The six nickel CT complexes have a nickel center, two organic ligands coordinated with the nickel center to form a dianionic square planar supramolecule and an organic counter-cation as represented by The ligands and counter-cations are selected to optimize properties, such as molecular alignment, film morphology, and molecular packaging. Described herein, the ligands can be 2,3-pyrazinedithiol (L1), 1,2-benzenedithol (L2) or 2,3-quinoxalinedithol (L3) and the counter-cations can be diquat (2,2?-ebpy) or methyl viologen (4,4?-mbpy). The six nickel CT complexes can also be utilized semiconductor devices, such as thin film transistors or inverters. Processes are also provided for the fabrication of semiconductors devices. The processes can include fabricating a substrate with a bilayer octadecylphosphonic acid (ODPA)/Al2O3 dielectric and applying one of the six nickel charge transfer (CT) complexes to the substrate.
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: July 18, 2017
    Assignee: CITY UNIVERSITY OF HONG KONG
    Inventors: Vellaisamy A. L. Roy, Zong-Xiang Xu, Paul Kim Ho Chu, Tat Kun Kwok
  • Patent number: 9206179
    Abstract: This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: December 8, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Scott L. Harbeson, Roger D. Tung
  • Patent number: 9199986
    Abstract: This invention relates to novel compounds that are pyrazinoisoquinoline derivatives of Formula I: and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: December 1, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Scott L. Harbeson, Roger D. Tung
  • Patent number: 9045483
    Abstract: According to the embodiments described herein, a methods for inhibiting small ubiquitin-like modifier enzymes in a cell are provided. Such methods may include administering certain substituted pyrrolo[2,3-b]-quinoxalines to the cell. In some aspects, the small ubiquitin-like modifier enzyme is SUMO E1 or SUMO E2. In some aspects, the methods may be used to inhibit a cancer cell in vitro (e.g., grown in culture) or in vivo (e.g., as part of a tumor in a subject). In other embodiments, methods for treating a cancer, degenerative diseases and viral infection are provided. Such methods may include administering an effective amount of a pharmaceutical composition to a subject having cancer. The pharmaceutical composition may include a small ubiquitin-like modifier inhibitor compound. In some embodiments, the method for treating a disease may further comprise administering one or more DNA-damaging therapy in combination with administration of the pharmaceutical composition.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: June 2, 2015
    Assignees: City of Hope, Sanford-Burnham Medical Research Institute
    Inventors: Yuan Chen, Yi-Jia Li, Daniela Divlianska, Ekaterina Bobkova, Greg Roth, Jun Pu, Pasha Khan
  • Patent number: 9040536
    Abstract: The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: May 26, 2015
    Assignee: ASKA PHARMACEUTICAL CO., LTD.
    Inventors: Makoto Okada, Shuichiro Sato, Kenji Kawade, Kotaro Gotanda, Atsushi Shinbo, Youichi Nakano, Hideo Kobayashi
  • 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
  • Publication number: 20150141431
    Abstract: This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
    Type: Application
    Filed: October 20, 2014
    Publication date: May 21, 2015
    Applicant: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Scott L. Harbeson, Roger D. Tung
  • Publication number: 20150094302
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Applicant: Genentech, Inc.
    Inventors: James John Crawford, Wendy B. Young
  • Patent number: 8981096
    Abstract: The design and synthesis of six nickel charge transfer (CT) complexes are described herein. The six nickel CT complexes have a nickel center, two organic ligands coordinated with the nickel center to form a dianionic square planar supramolecule and an organic counter-cation as represented by The ligands and counter-cations are selected to optimize properties, such as molecular alignment, film morphology, and molecular packaging. Described herein, the ligands can be 2,3-pyrazinedithiol (L1), 1,2-benzenedithol (L2) or 2,3-quinoxalinedithol (L3) and the counter-cations can be diquat (2,2?-ebpy) or methyl viologen (4,4?-mbpy). The six nickel CT complexes can also be utilized semiconductor devices, such as thin film transistors or inverters. Processes are also provided for the fabrication of semiconductors devices. The processes can include fabricating a substrate with a bilayer octadecylphosphonic acid (ODPA)/Al2O3 dielectric and applying one of the six nickel charge transfer (CT) complexes to the substrate.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: March 17, 2015
    Assignee: City University of Hong Kong
    Inventors: Vellaisamy A. L. Roy, Zong-Xiang Xu, Paul Kim Ho Chu, Tat Kun Kwok
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20150011461
    Abstract: Heteroaryl pyridone and aza-pyridone amide compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Applicant: GENENTECH, INC.
    Inventors: James John Crawford, Wendy Lee, Wendy B. Young
  • Publication number: 20140378432
    Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Patent number: 8889687
    Abstract: This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: November 18, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Roger Tung, Scott L. Harbeson
  • Publication number: 20140336197
    Abstract: The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 13, 2014
    Inventors: Makoto OKADA, Shuichiro SATO, Kenji KAWADE, Kotaro GOTANDA, Atsushi SHINBO, Youichi NAKANO, Hideo KOBAYASHI
  • Publication number: 20140322229
    Abstract: The present document describes compounds of Formula I, pharmaceutical compositions comprising the same as well as methods of treating diseases such as a cancer, neurological disease, neurodegenerative disorder, stroke, traumatic brain injury, parasitic infection, inflammation or an autoimmune disease with said compounds.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 30, 2014
    Inventors: Zhaoyin Wang, Lianhai Li
  • Publication number: 20140309213
    Abstract: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds 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: Application
    Filed: October 25, 2012
    Publication date: October 16, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
  • Publication number: 20140200209
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.
    Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
  • Patent number: 8779154
    Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: July 15, 2014
    Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
  • Patent number: 8772484
    Abstract: A simple process for producing v-coelenterazine compounds has been desired. Described is a process for producing a v-coelenterazine compound represented by general formula (II) comprising (1) the step of reacting a compound of general formula (VIII) with a methyltriphenylphosphonium salt in the presence of a base to give a compound represented by general formula (IX), (2) the step of performing a ring-closing metathesis reaction on any one selected from the group consisting of the compound represented by general formula (IX) and a compound of general formula (X) which is the compound of general formula (IX) wherein the amino is protected with R5, and then deprotecting R4 and, if any, R5 to give a v-coelenteramine compound represented by general formula (XIV), and (3) the step of reacting the compound of general formula (XIV) with a compound represented by general formula (XV) to give the compound of general formula (II).
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: July 8, 2014
    Assignees: JNC Corporation, National University Corporation Tokyo Medical and Dental University
    Inventors: Satoshi Inouye, Yuiko Miura, Suguru Yoshida, Takamitsu Hosoya
  • Patent number: 8754086
    Abstract: The disclosure describes compounds of formula I, wherein the wedged bonds, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, X and Y have meanings given in the description, and pharmaceutically-acceptable salts thereof; and methods of using such compounds useful in the treatment of cancer and conditions affected by inhibition of angiogenesis. Also provided, are processes for the preparation of formula I, by reacting formula I with other compounds; and processes for the preparation of a pharmaceutical formulation by bringing into association, a compound of formula I, with therapeutic agents and/or a pharmaceutically-acceptable adjuvant, diluent, or carrier.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: June 17, 2014
    Assignee: Everest Biosciences, Inc.
    Inventors: Jenny Persson, Rikard Larsson, Olov Sterner, Martin Johansson
  • Patent number: 8754215
    Abstract: The present disclosure describes a novel, cost-effective process for preparation of a 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2,1-a]isoquinoline derivatives. Specifically, it discloses a process for the preparation of the anthelmintic drug praziquantel through the use of a novel intermediate, 2-[(2,2-dimethoxyethyl)benzyl amino]-N-phenethylacetamide. This present disclosure also describes a novel crystalline form of 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: June 17, 2014
    Assignee: Sequent Scientific Limited
    Inventors: Lingappa Balaya, Mahalinga Manjathuru, Yogeesh Derambala, Pejakala Kakrannaya Vasudeva, Thangavel Arulmoli
  • Patent number: 8729072
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: May 20, 2014
    Assignee: F. Hoffman-La Roche AG
    Inventors: James John Crawford, Wendy B. Young
  • Patent number: 8716274
    Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: May 6, 2014
    Assignee: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Patent number: 8686144
    Abstract: The invention relates to the use of specific compounds of formula (I) and their pharmaceutically-acceptable salts: (Formula 1) (I) as a new family of protein kinase CK2 inhibitors; the invention also relates to the use of compounds of formula (I) for the preparation of pharmaceutical compositions for the prevention and/or treatment of disorders and/or diseases chosen amongst cancers; autoimmune and inflammatory diseases; infectious diseases; diabetes angiogenesis related disorders; retinopathies and cardiac hypertrophy.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: April 1, 2014
    Assignees: Commissariat a l'Energie Atomique et aux Energie Alternative, Institut National de la Sante et de la Recherche Medicale (INSERM), Institut Curie, Centre National de la Recherche Scientifique
    Inventors: Claude Cochet, Renaud Prudent, Virginie Moucadel, Chi-Hung N'guyen
  • Patent number: 8673915
    Abstract: A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein each of R11 and R12 is hydrogen, C1-8 alkyl or the like; R13 is hydrogen, C1-8 alkyl or the like; R14 is hydrogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkyl having 1-3 halogens, C1-8 hydroxyalkyl, halogen, hydroxyl, nitro, cyano, amino, C1-8 alkylamino, benzenesulfonylamino optionally having a substituent, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene, tetrahydronaphthalene, or indan ring.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: March 18, 2014
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Masatoshi Ushioda, Shogo Sakuma, Atsushi Tendo, Toshiyasu Imai, Kazuhide Inoue
  • Publication number: 20140066449
    Abstract: Compounds of Formula (I): ?-x-? (I) and pharmaceutically acceptable salts and solvates thereof, wherein ?, x, and ? have the meanings as indicated in the specification, are useful for treating a disease or disorder characterised by pathologically proliferating cells, particularly cancer. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: March 2, 2012
    Publication date: March 6, 2014
    Applicant: SABREPHARM LIMITED
    Inventor: John Charles Marshall Stewart
  • Publication number: 20140057896
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 27, 2014
    Inventors: Antonio J.M. BARBOSA, Peter A. BLOMGREN, Kevin S. CURRIE, Ravi KRISHNAMOORTHY, Jeffrey E. KROPF, Seung H. LEE, Scott A. MITCHELL, Daniel ORTWINE, Aaron C. SCHMITT, Xiaojing WANG, Jianjun XU, Wendy YOUNG, Honglu ZHANG, Zhongdong ZHAO, Pavel E. ZHICHKIN
  • Patent number: 8653079
    Abstract: The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Scott D. Kuduk
  • Patent number: 8648076
    Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: February 11, 2014
    Assignee: Hybrigenics SA
    Inventors: Philippe Guedat, Guillaume Boissy, Catherine Borg-Capra, Frédéric Colland, Laurent Daviet, Etienne Formstecher, Xavier Jacq, Jean-Christophe Rain, Rémi Delansorne, Stefania Vallese, Matteo Colombo
  • Publication number: 20130296564
    Abstract: Herein we describe compositions and methods for the synthesis of [2.2.2]-diazabicyclic structures comprising a domino reaction sequence involving aldol condensation, alkene isomerization, and intramolecular hetero-Diels-Alder cycloaddition. Excellent diastereofacial control during the cycloaddition is enforced with a removable chiral phenyl aminal diketopiperazine substituent. The reaction sequence rapidly generates molecular complexity and is competent with both enolizable and non-enolizable aldehyde substrates. This method provides an efficient route to [2.2.2]-diazabicyclic structures, common to bioactive prenylated indole alkaloids such as the brevianamides and stephacidins.
    Type: Application
    Filed: May 1, 2013
    Publication date: November 7, 2013
    Applicant: College of William and Mary
    Inventor: Jonathan R. Scheerer
  • Publication number: 20130289041
    Abstract: Disclosed herein are compounds of formula (I) and methods of inhibiting IKK? and the NF-?B signaling and mTOR pathways.
    Type: Application
    Filed: November 22, 2011
    Publication date: October 31, 2013
    Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
    Inventors: Amarnath Natarajan, Qianyi Chen, Vashti C. Bryant, Rajkumar Rajule
  • Publication number: 20130289275
    Abstract: The present disclosure describes a novel, cost-effective process for preparation of a 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2,1-a]isoquinoline derivatives. Specifically, it discloses a process for the preparation of the anthelmintic drug praziquantel through the use of a novel intermediate, 2-[(2,2-dimethoxyethyl)benzyl amino]-N-phenethylacetamide. This present disclosure also describes a novel crystalline form of 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 31, 2013
    Inventors: Lingappa BALAYA, Mahalinga MANJATHURU, Yogeesh DERAMBALA, Pejakala Kakrannaya VASUDEVA, Thangavel ARULMOLI
  • Publication number: 20130281664
    Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.
    Type: Application
    Filed: October 11, 2011
    Publication date: October 24, 2013
    Inventors: David Milstein, Ekambaram Balaraman, Chidambaram Gunanathan, Boopathy Gnanaprakasam, Jing Zhang
  • Patent number: 8557876
    Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers that when m is 0, n is 1; when m is 1, n is 0 or 1; or when m is 2, n is 0; wherein (CH)m and (CH)n are each independently optionally substituted with a substituent selected from the group consisting of methyl and ethyl; wherein X is selected from the group consisting of N, O, and S; and wherein R1 and R2 each independently represent H or a hydrocarbon group, or R1 and R2 together represent a fused ring or a ring system, with the proviso that when R1 is H, R2 is not H.
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: October 15, 2013
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Robert P. Belko, Paul D. Jones, Anthony T. Levorse, Jr., Michael G. Monteleone, Anubhav P. S. Narula, Franc T. Schiet
  • Publication number: 20130225572
    Abstract: The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 29, 2013
    Inventors: Makoto OKADA, Shuichiro SATO, Kenji KAWADE, Kotaro GOTANDA, Atsushi SHINBO, Youichi NAKANO, Hideo KOBAYASHI
  • Patent number: 8513241
    Abstract: Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
    Type: Grant
    Filed: May 29, 2012
    Date of Patent: August 20, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Giovanni Cervi, Matteo D'Anello, Gianluca Mariano Enrico Papeo, Barbara Salom
  • Publication number: 20130178625
    Abstract: A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein each of R11 and R12 is hydrogen, C1-8 alkyl or the like; R13 is hydrogen, C1-8 alkyl or the like; R14 is hydrogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkyl having 1-3 halogens, C1-8 hydroxyalkyl, halogen, hydroxyl, nitro, cyano, amino, C1-8 alkylamino, benzenesulfonylamino optionally having a substituent, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene, tetrahydronaphthalene, or indan ring.
    Type: Application
    Filed: July 27, 2011
    Publication date: July 11, 2013
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Masatoshi Ushioda, Shogo Sakuma, Atsushi Tendo, Toshiyasu Imai, Kazuhide Inoue
  • Publication number: 20130156761
    Abstract: The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX3CR1 or fractalkine antagonist.
    Type: Application
    Filed: February 25, 2013
    Publication date: June 20, 2013
    Applicants: Alliance Discovery, Inc., Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
    Inventors: Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine, Alliance Discovery, Inc.
  • Publication number: 20130116262
    Abstract: Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 9, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130116245
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 9, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130116235
    Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 9, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130109679
    Abstract: Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention.
    Type: Application
    Filed: November 30, 2010
    Publication date: May 2, 2013
    Inventors: Stephen James Boyer, Donghong Amy Gao, Xin Guo, Thomas Martin Kirrane, JR., Christopher Ronald Sarko, Roger John Snow, Fariba Soleymanzadeh, Yunlong Zhang
  • Patent number: 8420646
    Abstract: The present invention is directed to tricyclic tetrahydroquinoline compounds of formula I, and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R5, R20 and X are as described herein and to pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: April 16, 2013
    Assignee: PAH P&U LLC
    Inventors: Michael Robert Barbachyn, Paul Joseph Dobrowolski, Alexander Ross Hurd, Dennis Joseph McNamara, John Raymond Palmer, Arthur Glenn Romero, J. Craig Ruble, Debra Ann Sherry, Lisa Marie Thomasco, Peter Laurence Toogood
  • Publication number: 20130029997
    Abstract: This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
    Type: Application
    Filed: March 2, 2012
    Publication date: January 31, 2013
    Applicant: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Roger Tung, Scott L. Harbeson
  • Patent number: 8309734
    Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: November 13, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Rainer E. Martin, Ulrike Obst Sander, Hans Richter, Christoph Ullmer
  • Publication number: 20120277325
    Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers that when m is 0, n is 1; when m is 1, n is 0 or 1; or when m is 2, n is 0; wherein (CH)m and (CH)n are each independently optionally substituted with a substituent selected from the group consisting of methyl and ethyl; wherein X is selected from the group consisting of N, O, and S; and wherein R1 and R2 each independently represent H or a hydrocarbon group, or R1 and R2 together represent a fused ring or a ring system, with the proviso that when R1 is H, R2 is not H.
    Type: Application
    Filed: July 3, 2012
    Publication date: November 1, 2012
    Inventors: Robert P. Belko, Paul D. Jones, Anthony T. Levorse, JR., Michael G. Monteleone, Anubhav P.S. Narula, Franc T. Schiet