Bicyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/235)
  • Patent number: 9364481
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Grant
    Filed: November 18, 2015
    Date of Patent: June 14, 2016
    Assignee: Nivalis Therapeutics, Inc.
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Patent number: 9174947
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Grant
    Filed: October 26, 2006
    Date of Patent: November 3, 2015
    Assignee: Exelixus, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
  • Patent number: 9133200
    Abstract: New imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Grant
    Filed: November 24, 2011
    Date of Patent: September 15, 2015
    Assignee: Almirall, S.A.
    Inventors: Jacob Gonzalez Rodriguez, Bernat Vidal Juan, Laura Vidal Gispert, Jordi Bach Taña
  • Patent number: 9120723
    Abstract: The present disclosure relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is selected from OH, NHCH2CH2F, NHCH(Me)CH2OH and NHCH2CH2OH; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is phenyl or pyridyl; and B is (CH2)n where n is 0; with the proviso that: (i) when A is phenyl, and Z is OH, X—Y is other than C?C—(CH2)2CO2H, C?C—(CH2)2CO2Me, (CH2)4CO2H. Uses of such compounds as medicaments for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors are provided.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: September 1, 2015
    Assignee: CANBEX THERAPEUTICS LIMITED
    Inventors: Masahiro Okuyama, David Selwood, Cristina Visintin, David Baker, Gareth Pryce
  • Publication number: 20150126487
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, a sleep disorder and the like. The present invention relates to a compound represented by the formula (I): wherein R1 is an optionally substituted amino group or an optionally substituted cyclic amino group, R2 and R3 are each independently a hydrogen atom or a substituent, X is —CH? or —N?, and ring A is an optionally substituted 5- to 10-membered ring, or a salt thereof.
    Type: Application
    Filed: February 28, 2013
    Publication date: May 7, 2015
    Inventors: Hiroki Sakamoto, Takahiro Sugimoto
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Publication number: 20150111894
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
  • Publication number: 20150099277
    Abstract: Provided herein, inter alia, are compositions and methods of synthesis and detection of tetrazines and diazonorcaradienes.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Neal K. Devaraj, Jun Yang, Jolita Seckute
  • Publication number: 20150087043
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 11, 2014
    Publication date: March 26, 2015
    Applicants: Coferon, Inc, Cornell University
    Inventors: Lee Daniel Arnold, Maneesh Pingle, Douglas S. Werner
  • Patent number: 8987268
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, Jingwu Duan, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Zhonghui Lu, William J. Pitts, Steven H. Spergel, Hong Wu, Bingwei Vera Yang
  • Patent number: 8987273
    Abstract: The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacture and their use for the treatment of benign and malignant neoplasia.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
  • Patent number: 8980871
    Abstract: Provided herein are methods of treating hemolysis by administering an active compound in an amount sufficient to treat said hemolysis. It has been found that nitroxyl donors or similar compounds preferentially react with cell-free OxyHb, as compared to OxyHb encapsulated in a red blood cell, and reacts with MetHb to form iron-nitrosyl Hb or nitrite bound MetHb. It has also been found that such compounds reduce cell-free Hb and hemolysis. Active compounds are also contemplated for use in combination therapies, for example, in combination with the administration of red blood cells and/or an agent that promotes hematopoiesis, or in combination with the administration of a nitric oxide donor.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: March 17, 2015
    Assignees: Wake Forest University Health Sciences, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Daniel B. Kim-Shapiro, S. Bruce King, Daniel A. Sweeney, Mark T. Gladwin
  • Publication number: 20150072987
    Abstract: Novel compound having the following formula: wherein Y is N, O, or S. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.
    Type: Application
    Filed: July 17, 2014
    Publication date: March 12, 2015
    Inventor: Zhanggui WU
  • Publication number: 20150065501
    Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Patent number: 8962626
    Abstract: The present invention relates to thienopyridazine compounds of formula (I), their pharmaceutically acceptable salts or hydrates, wherein R1 and R2 are independently H or C1-4 alkyl, R3 is a saturated or unsaturated 5- or 6-membered ring containing N, S or O, or its optical isomers, R4 is a halophenyl monosubstituted or disubstituted at any position. The present invention provides the preparation methods of these compounds, pharmaceutical compositions containing these compounds and the uses of these compounds, particularly in treating cancer.
    Type: Grant
    Filed: January 7, 2009
    Date of Patent: February 24, 2015
    Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical Factory
    Inventor: Zhanggui Wu
  • Patent number: 8957073
    Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: February 17, 2015
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
  • Publication number: 20150038510
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined in the specification. The compounds are inhibitors of Bruton's tyrosine kinase (BTK). This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with BTK.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 5, 2015
    Inventors: John David Lawson, Mark Sabat, Christopher Smith, Haixia Wang, Young K. Chen, Toufike Kanouni
  • Publication number: 20150031686
    Abstract: Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 29, 2015
    Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
  • Publication number: 20150018309
    Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: February 23, 2013
    Publication date: January 15, 2015
    Inventors: Craig W Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, James C. Tarr, James M. Salovich
  • Publication number: 20150004100
    Abstract: Pyridazinone compounds of Formula I: (I) wherein: R? is alkyl or Ar, optionally substituted with at least one alkyl, halogen, hydroxyl, alkoxy, haloalkoxy, acid, ester, amino, nitro, amide, or alkoxyhalo; 2 R is independently alkyi, alkynyl, ester, amino, amide, acid, aryl, heteroaryl, aminoalkyl, —C(=0)alkyl, —C(=0)aryl, —C(=0)heteroaryl, —C(=0)heterocycloalkyl, —C(=0)heterocycloalkylAr, —C(=0)(CH2)nhalo, —C(?O)(CH2)nheterocyclyl, or —SC?Ar, optionally substituted with at least one alkyi, alkylhalo, halogen, nitro, aryl, heteroaryl, or heteroaryl(CH2)nhalo; R3 and R4 are independently hydrogen, alkyi, alkenyl, alkynyl, aryl, heteroaryl; Ar is an aryl, heteroaryl, cycloalkyl, heterocycloalkyl group; n is an integer from 0-10; or a radiolabeled derivative thereof. The compounds are useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
    Type: Application
    Filed: December 13, 2012
    Publication date: January 1, 2015
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Clare Jones, Matthias Eberhard Glaser, Duncan Wynn, James Nairne, Umamaheshwar P. Mokkapati, Ian Martin Newington, Chitralekha Rangswamy, Jinto Jose, Saga Johansson
  • Patent number: 8921368
    Abstract: Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: December 30, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Gregory D. Brown, Lidia M. Doweyko, Jingwu Duan, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Zhonghui Lu, Steven H. Spergel, John S. Tokarski, Hong Wu, Bingwei Vera Yang
  • Patent number: 8916554
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Publication number: 20140364431
    Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
  • Patent number: 8883787
    Abstract: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: November 11, 2014
    Assignee: Eisai Inc.
    Inventors: Weizheng Xu, Greg Delahanty, Jie Zhang
  • Patent number: 8883786
    Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch
  • Patent number: 8865709
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: October 21, 2014
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Patent number: 8865719
    Abstract: The present invention is related to heterocycles represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs and/or GABAA receptors. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs and negative allosteric modulation of GABAA receptors in a mammal by administering an effective amount of a compound of Formula I.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: October 21, 2014
    Assignee: The Regents of the University of California
    Inventors: Timothy B. C. Johnstone, Derk J. Hogenkamp, Kelvin W. Gee
  • Patent number: 8859549
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: May 8, 2012
    Date of Patent: October 14, 2014
    Assignee: AbbVie, Inc.
    Inventors: Brian S. Brown, Tongmei Li, Sridhar Peddi, Arturo Perez-Medrano, David DeGoey
  • Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Publication number: 20140288052
    Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 25, 2014
    Inventors: Charles A. Blum, Jeremy S. Disch, Stephanie K. Springer
  • Publication number: 20140283218
    Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.
    Type: Application
    Filed: June 27, 2012
    Publication date: September 18, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Roger Graham Hall, Andrew Edmunds, Andre Jeanguenat, Thomas Pitterna, Sebastian Rendler
  • Publication number: 20140275069
    Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: February 25, 2014
    Publication date: September 18, 2014
    Inventors: Katja JANTOS, Michael OCHSE, Hervé GENESTE, Jayne FROGGETT, Clarissa JAKOB, Karla DRESCHER, Jürgen DINGES
  • Publication number: 20140249151
    Abstract: [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11?-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. [Means for Solution] A bicyclic heterocyclic compound (the bicyclic heterocycle is formed when a cyclohexane ring is fused with a 5- to 6-membered monocyclic heterocycle that has only a nitrogen atom as a hetero atom) substituted with an acylamino group such as a (hetero)aroylamino group or the like or a pharmaceutically acceptable salt thereof was found to have an excellent selective inhibitory action against 11?-HSD1.
    Type: Application
    Filed: October 17, 2012
    Publication date: September 4, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shimpei Kawakami, Minoru Sakurai, Noriyuki Kawano, Takayuki Suzuki, Nobuyuki Shiraishi, Wataru Hamaguchi, Ryuichi Sekioka, Hiroyuki Moritomo, Ayako Motitomo
  • Publication number: 20140235855
    Abstract: Compounds of formula (I), wherein A1 represents —O—, —S— or —CH2—; A2 represents —CH2— or —O—; A3 represents C3-C8-cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, —C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; m is 0 or 1; n is 1; the —(CH2)n— group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.
    Type: Application
    Filed: June 11, 2012
    Publication date: August 21, 2014
    Inventors: Berangere Gaucher, Franck Hubert Danel, Tong Xie, Lin Xu
  • Patent number: 8809427
    Abstract: Provided is a phthalocyanine compound which is halogen-free and which has a green hue, excellent resistance to organic solvents and acids, and high chroma. Also provided are a metal-free phthalocyanine compound or a metal phthalocyanine compound represented by specified general formula (1-1) or (1-2) and having a N,N?-disubstituted imidazolone structure or piperazinedione structure introduced therein, and a coloring composition including the compound and a synthetic resin. The phthalocyanine compound of the present invention exhibits a clear green color and is halogen-free, and is thus useful as a clear green pigment for coloring materials such as a coating material, plastic, a printing ink, rubber, leather, textile printing, a color filter, a jet ink, a heat transfer ink, etc.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: August 19, 2014
    Assignee: DIC Corporation
    Inventors: Hitoshi Kondou, Yoshiyuki Sano, Yutaka Tachikawa
  • Patent number: 8785643
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 22, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Patent number: 8765691
    Abstract: The present invention relates to the use of osmolytes for treating allergic or viral respiratory diseases, e.g. allergic rhinitis (hay fever) as well as rhinovirus and/or adenovirus infections. The invention also relates to a medicament preparation containing one or more compounds from the group of osmolytes. The group of osmolytes used in the invention comprises various low-molecular substances, more specifically ectoine, 4,5,6,7-tetrahydro-2-methyl-1H-[1,3]-diazepine-4-S-carboxylic acid (homoectoine), hydroxyectoine, di-myo-inositol-phosphate (DIP), to cyclic 2,3-diphosphoglycerate (cDPG), 1,1-diglycerol phosphate (DGP), ?-mannosylglycerate (firoin), ?-mannosylglyceramide (firoin-A), dimannosyl-diinositol phosphate (DMIP), glucosylglycerol, taurine, betaine, citrulline, and/or a derivative, e.g. an acid, salt, or ester of said compounds.
    Type: Grant
    Filed: August 25, 2008
    Date of Patent: July 1, 2014
    Assignee: Bitop AG
    Inventors: Jean Krutmann, Georg Lentzen, Thomas Schwarz
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Patent number: 8754082
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: June 17, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
  • Publication number: 20140163035
    Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: July 20, 2012
    Publication date: June 12, 2014
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Kurt Hilpert, Francis Hubler, Thierry Kimmerlin, Dorte Renneberg, Simon Stamm, Mark Murphy
  • Publication number: 20140155404
    Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
    Type: Application
    Filed: February 10, 2014
    Publication date: June 5, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Chu-Biao Xue, Genfeng Cao, Taisheng Huang, Lihua Chen, Ke Zhang, Anlai Wang, David J. Meloni, Rajan Anand, Joseph Glenn, Brian W. Metcalf
  • Publication number: 20140142088
    Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.
    Type: Application
    Filed: November 18, 2013
    Publication date: May 22, 2014
    Applicant: CEPHALON, INC.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Alison L. Zulli
  • Publication number: 20140114068
    Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: April 24, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
  • Publication number: 20140105898
    Abstract: This invention relates generally to methods and agents for modulating adiposity-related conditions. More particularly, the present invention relates to the use of TRAIL death receptor agonists, including nucleic acids such as TRAIL polynucleotides, peptides and polypeptides including TRAIL polypeptides, TRAIL DR agonist antigen-binding molecules, TRAIL DR peptide agonists as well as small molecule TRAIL DR agonists in compositions and methods for treating or preventing adiposity-related conditions such as obesity, diabetes mellitus and metabolic syndrome.
    Type: Application
    Filed: February 27, 2012
    Publication date: April 17, 2014
    Applicant: Istituto Di Ricovero E Cura A Carattere Scientific Materno-Infantile Burlo Garo
    Inventors: Merlin C. Thomas, Giorgio Zauli, Paola Secchiero, Bruno Fabris, Stella Bernardi
  • Patent number: 8680108
    Abstract: The present invention provides fused aryl and heteroaryl derivatives of Formula I: wherein X, V, Y, U, W, Z, R1, R2, Cy, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: March 25, 2014
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Hui-Yin Li
  • Publication number: 20140066448
    Abstract: The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R1, R2, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: March 13, 2012
    Publication date: March 6, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Andrew P. Combs, Yun-Long Li, Song Mei, Eddy W. Yue
  • Publication number: 20140066430
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Application
    Filed: October 3, 2013
    Publication date: March 6, 2014
    Applicant: Amgen Inc.
    Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Hanh Nho NGUYEN, Philip R. Olivieri, Vinod F. Patel, Karina ROMERO, Laurie Schenkel
  • Publication number: 20140051694
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: NEOSOME LIFE SCIENCES, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Publication number: 20140031355
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.
    Type: Application
    Filed: November 4, 2011
    Publication date: January 30, 2014
    Applicant: Amgen Inc.
    Inventor: Amy Kaizerman
  • Patent number: RE47047
    Abstract: The present invention relates to compounds of formula I, processes for their production and their use as anti-inflammatory agents.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: September 18, 2018
    Assignees: ASTRAZENECA AB, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Berger, Hartmut Rehwinkel, Thomas Zollner, Ekkehard May, Jorma Hassfeld, Heike Schaecke