Ring Nitrogen In The Polycyclo Ring System Patents (Class 544/80)
  • Patent number: 11479558
    Abstract: Disclosed herein are tetrahydropyranoindole compounds and derivatives thereof, as well as their methods of synthesis and use. The disclosed compounds may be synthesized by methods that utilize a cooperative hydrogen bond donor/Brønsted acid system. The disclosed compounds may be useful for treating a disease, disorder, or a symptom thereof in a subject in need thereof, such as pain, swelling, and joint stiffness. The disclosed compounds also may be useful for treating cell proliferative diseases and disorders such as cancer.
    Type: Grant
    Filed: July 9, 2020
    Date of Patent: October 25, 2022
    Assignee: NORTHWESTERN UNIVERSITY
    Inventors: Karl A. Scheidt, Mark A. Maskeri
  • Patent number: 11248012
    Abstract: The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)-active and toll-like receptor (TLR8)-active imidazoquinolines and oxoadenines.
    Type: Grant
    Filed: August 10, 2020
    Date of Patent: February 15, 2022
    Assignee: GLAXO SMIIHKLINE BIOLOGICALS SA
    Inventors: Helene G. Bazin-Lee, Laura S. Bess, David A. Johnson
  • Patent number: 10035796
    Abstract: The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an A? pathology and/or a symptom or symptoms thereof. Non-limiting examples of such A? pathologies, including Alzheimer's disease, are disclosed herein.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: July 31, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Irina Kazakevich, Scott Trzaska, Tao Feng
  • Patent number: 10017505
    Abstract: The present invention provides four crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an A? pathology and/or a symptom or symptoms thereof. Non-limiting examples of such A? pathologies, including Alzheimer's disease, are disclosed herein.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: July 10, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Trzaska, Zachary E. Dance, Yong Liu, Richard John Varsolona, Gregory York
  • Publication number: 20150148328
    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 28, 2015
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
  • Publication number: 20150051203
    Abstract: A compound of structural formula (I) or (II): as HSP90 inhibitors that possess significantly improved bioavailability over comparative compounds, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 19, 2015
    Inventors: Dinesh Chimmanamada, Zachary Demko, Weiwen Ying
  • Publication number: 20150031669
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: January 29, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Steven John Woodhead, Christopher William Murray, Valerio Berdini, Gordon Saxty, Gilbert Ebai Besong, Lieven Meerpoel, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
  • Patent number: 8940724
    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, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: January 27, 2015
    Assignee: Amgen Inc.
    Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez de Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
  • Publication number: 20140275062
    Abstract: The invention relates to novel compounds which are naphthalene diimides of general formula (I): The compounds are used in therapy, particularly in cancer treatment.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Inventors: Stephen NEIDLE, Stephan A. OHNMACHT, Mekala GUNARATNAM, Aaron Grainger DALE, Marialuisa MICCO, Gavin William COLLIE
  • Publication number: 20140275024
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Publication number: 20140256706
    Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Xu Ran, Yujun Zhao, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachern, Jeanne Stuckey, Jennifer Lynn Meagher, Duxin Sun, Xiaoqin Li, Bing Zhou, Hacer Karatas, Ruijuan Luo, Arul Chinnaiyan, Irfan A. Asangani
  • Publication number: 20140187545
    Abstract: PI3K? selective compounds having the structure
    Type: Application
    Filed: June 29, 2012
    Publication date: July 3, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Hong Lin, Juan Luengo, Michael Lee Moore, Junya Qu, Ralph A. Rivero, Rosanna Tedesco, Hongyi Yu
  • Patent number: 8765731
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: July 1, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, Jr., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
  • Publication number: 20140163023
    Abstract: The invention relates to compounds of formula (I) wherein X, R1, R2, T0, o have the meaning as cited in the description and the claims. The compounds of formula I are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including the compounds of formula I, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: April 2, 2012
    Publication date: June 12, 2014
    Applicant: Cellzome Limited
    Inventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Jane Elizabeth Scanlon, Rita Joana Rodrigues Adrego
  • Publication number: 20140157443
    Abstract: Provided herein is a novel mTOR-comprising complex, mT-ORC3, which comprises mTOR and the Ets transcription factor TEL2. Specific mTORC3 binding agents and modulating agents are provided, along with kits and methods for the detection of mTORC3. Methods of modulating the activity of mTORC3 or modulating cell growth and/or survival are also provided. Further provided are methods for screening for mTORC3 binding agents and for mTORC3 modulating agents. Various methods of diagnosis and treatment are further provided.
    Type: Application
    Filed: April 12, 2012
    Publication date: June 5, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Gerard C. Grosveld, Frank C. Harwood, Ramon I. Klein-Geltink
  • Publication number: 20140135315
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Application
    Filed: April 9, 2013
    Publication date: May 15, 2014
    Applicant: KuDOS Pharmaceuticals Limited
    Inventor: KuDOS Pharmaceuticals Limited
  • Publication number: 20140121200
    Abstract: Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.
    Type: Application
    Filed: June 7, 2012
    Publication date: May 1, 2014
    Applicant: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Wei-Guo Su, Wei Deng, Jianguo Ji
  • Publication number: 20140045811
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: July 18, 2013
    Publication date: February 13, 2014
    Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
  • Publication number: 20140045832
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicants: PIRAMAL ENTERPRISES LIMITED, MERCK SHARP & DOHME CORP.
    Inventors: Sarala Balachandran, Christopher J. Dinsmore, Abhijit Roychowdhury, Rajiv Sharma, Ram Asrey Vishwakarma
  • Publication number: 20140005383
    Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.
    Type: Application
    Filed: September 5, 2013
    Publication date: January 2, 2014
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Publication number: 20140005188
    Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.
    Type: Application
    Filed: March 8, 2012
    Publication date: January 2, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventors: Francis Louis Atkinson, Stephen John Atkinson, Michael David Barker, Clement Douault, Neil Stuart Garton, John Liddle, Vipulkumar Kantibhai Patel, Alexander G. Preston, Tracy Jane Shipley, David Matthew Wilson, Robert J. Watson
  • Publication number: 20130296302
    Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.
    Type: Application
    Filed: May 3, 2013
    Publication date: November 7, 2013
    Applicant: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Publication number: 20130267496
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: May 23, 2013
    Publication date: October 10, 2013
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
  • Publication number: 20130261113
    Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: June 3, 2013
    Publication date: October 3, 2013
    Inventors: Martin HENTEMANN, Jill WOOD, William SCOTT, Martin MICHELS, Ann-Marie CAMPBELL, Ann BULLION, Ronald ROWLEY, Aniko REDMAN
  • Publication number: 20130245005
    Abstract: Compounds of Formula (I): able to inhibit kinase activity, in particular Phosphatidylinositol 3-Kinases activity. The disclosure also relates to the use of compounds of Formula (I) for treatment of pathological conditions associated to alterations in Phosphatidylinositol 3-Kinases activity.
    Type: Application
    Filed: November 28, 2011
    Publication date: September 19, 2013
    Applicants: UNIVERSITA DEGLI STUDI DEL PIEMONTE ORIENTALE "AMEDEO AVOGADRO", UNIVERSITA DEGLI STUDI DI TORINO
    Inventors: Giovanni Sorba, Gian Cesare Tron, Ubaldina Galli, Alberto Massarotti, Emilio Hirsch, Elisa Ciraolo, Tracey Pirali
  • Publication number: 20130203656
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: May 23, 2011
    Publication date: August 8, 2013
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20130157997
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: November 16, 2012
    Publication date: June 20, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130102587
    Abstract: Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.
    Type: Application
    Filed: March 14, 2011
    Publication date: April 25, 2013
    Applicant: PROXIMAGEN LIMITED
    Inventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
  • Patent number: 8383619
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof; wherein either R1 is R1a and R2 is R2a; or R1 is R1b and R2 is R2b; provided that in each case at least one of R1 and R2 is other than hydrogen; R1a and R2a are the same or different and each is selected from hydrogen, C1-4 alkyl, C2-4 alkenyl and C2-4 alkynyl wherein the C1-4 alkyl is optionally substituted by C1-2 alkoxy; R1b and R2b are the same or different and are selected from hydrogen, C(O)NR4R5, C(O)R6 and C(O)OR6 where R6 is C1-4 alkyl, R4 and R5 are both C1-4 alkyl, or NR4R5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidized forms of N and S, the heterocyclic ring being optionally substituted by one or two C1-4 alkyl groups and/or one or two oxo groups; and R3 is a group D: wherein the asterisk denotes the point of attachment to the isoindoline ring; but excluding acetic acid 5-acetoxy-4-isopro
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: February 26, 2013
    Assignee: Astex Therapeutics Limited
    Inventors: Martyn Frederickson, Marian Williams
  • Publication number: 20130040931
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
    Type: Application
    Filed: January 14, 2011
    Publication date: February 14, 2013
    Applicant: Amgen Inc.
    Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
  • Publication number: 20130023502
    Abstract: The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
    Type: Application
    Filed: January 25, 2012
    Publication date: January 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Georg Dahmann, Dennis Fiegen, Martin Fleck, Matthias Hoffmann, Jasna Klicic, Stephen Peter East, Spencer Charles R. Napier, John Scott
  • Publication number: 20130012489
    Abstract: The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in claim 1, and/or physiologically acceptable salts, tautomers and stereo-isomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.
    Type: Application
    Filed: February 17, 2011
    Publication date: January 10, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Werner Mederski, Thomas Fuchss, Frank Zenke
  • Publication number: 20120329792
    Abstract: The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
    Type: Application
    Filed: March 8, 2011
    Publication date: December 27, 2012
    Inventors: José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James MacDonald, Joaquin Pastor-Fernández, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Greta Constantia Peter Vanhoof
  • Publication number: 20120283256
    Abstract: The present invention relates to compounds having the following Formula (I) for use in the prevention and/or the treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.
    Type: Application
    Filed: December 16, 2010
    Publication date: November 8, 2012
    Inventors: Andre Delacourte, Patricia Melnyk, Stephane Burlet, Nicolas Lefur
  • Publication number: 20120277424
    Abstract: Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.
    Type: Application
    Filed: October 15, 2010
    Publication date: November 1, 2012
    Applicant: Korea Institute of Science and Technology
    Inventors: Tae Bo Sim, Hwan Geun Choi, Jung Mi Hah, Young Jin Ham, Eun Jin Jun, Jung Hun Lee, Hwan Kim
  • Publication number: 20120263708
    Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: August 24, 2010
    Publication date: October 18, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
  • Publication number: 20120237475
    Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
    Type: Application
    Filed: March 16, 2012
    Publication date: September 20, 2012
    Applicant: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck
  • Publication number: 20120238545
    Abstract: This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 20, 2012
    Applicant: MERCK SERONO SA
    Inventors: Pascale Gaillard, Isabelle Jeanclaude-Etter, Vincent Pomel, Eric Sebille, Seenisamy Jeyaprakashnarayanan, Mathilde Muzerelle
  • Patent number: 8263584
    Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: September 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati, Ruben Alvarez Sanchez, Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • Publication number: 20120220581
    Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
    Type: Application
    Filed: October 27, 2010
    Publication date: August 30, 2012
    Applicant: Janssen-Cilag, S.A.
    Inventors: Joaquin Pastor-Fernández, José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Óscar Delgado-González, Greta Constantia Peter Vanhoof, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Sergio-Alvar Alonso-De Diego
  • Publication number: 20120220576
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
    Type: Application
    Filed: January 30, 2012
    Publication date: August 30, 2012
    Inventors: Branko RADETICH, Bing YU, Yanyi ZHU
  • Publication number: 20120190673
    Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.
    Type: Application
    Filed: December 19, 2011
    Publication date: July 26, 2012
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Valerio BERDINI, Maria Grazia CARR, Adrian Liam GILL, Steven HOWARD, Eva Figueroa NAVARRO, Gary TREWARTHA, David Charles REES, Mladen VINKOVIC, Paul Graham WYATT
  • Publication number: 20120178736
    Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is 0, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: March 22, 2012
    Publication date: July 12, 2012
    Inventors: Georgette Castanedo, Bryan Chan, David Goldstein, Rama Kondru, Matthew Lucas, Wylie Palmer, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Zachary K. Sweeney
  • Publication number: 20120178737
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N-(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110?, and therefore have utility in therapy.
    Type: Application
    Filed: August 19, 2010
    Publication date: July 12, 2012
    Inventors: Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Thomas James Hill, Franck Alexandre Silva
  • Publication number: 20120165309
    Abstract: [Object] A novel and excellent method for preventing or treating rejection in the transplantation of various organs, allergy diseases, autoimmune diseases, hematologic tumor, or the like, based on a PI3K?-selective inhibitory action and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), is provided [Means for Solution] It was found that a 3-substituted triazine or 3-substituted pyrimidine derivative exhibits a PI3K?-selective inhibitory action, and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), and can be an agent for preventing or treating rejection in the transplantation of various organs, allergy diseases (asthma, atopic dermatitis, etc.), autoimmune diseases (rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus, etc.), hematologic tumor (leukemia etc.
    Type: Application
    Filed: February 10, 2010
    Publication date: June 28, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Fumie Takahashi, Sunao Imada, Masahiko Shiwaku, Yasumasa Shiwaku, Atsuko Shiwaku, Koji Kato, Hidehiko Fukahori
  • Publication number: 20120165313
    Abstract: Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
    Type: Application
    Filed: March 1, 2012
    Publication date: June 28, 2012
    Applicant: Genentech, Inc.
    Inventors: Philippe Bergeron, Frederick Cohen, Anthony Estrada, Michael F.T. Koehler, Kevin Hon Luen Lau, Coung Ly, Joseph P. Lyssikatos, Daniel Ortwine, Zhonghua Pei, Xianrui Zhao
  • Patent number: 8203001
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: June 19, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
  • Publication number: 20120142679
    Abstract: The invention relates to the novel materials of formula (I), where R1 is an optionally substituted L-aryl or -heteroaryl, such that L is: an alkyl or CO, or LX, with Lbeing an alkyl and X being O or S; R2 is H or an alkyl; R3 is an alkyl optionally substituted by Hal; and R4 is Hou Hal, wherein said materials are in any isomeric form and the salts thereof, to be used as drugs.
    Type: Application
    Filed: July 1, 2010
    Publication date: June 7, 2012
    Applicant: SANOFI
    Inventors: Maurice Brolio, Annie Clauss, Youssef El Ahmad, Bruno Filoche-Romme, Frank Halley, Karl Andreas Karlsson, Gilbert Marciniak, Baptiste Ronan, Laurent Schio, Bertrand Vivet, Fabrice Viviani, Andre Zimmermann
  • Publication number: 20120142673
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Application
    Filed: November 30, 2011
    Publication date: June 7, 2012
    Applicant: KuDOS PHARMACEUTICALS LIMITED
    Inventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Malagu, Niall Morrison Barr Martin, Keith Allan Menear, Graeme Cameron Murray Smith
  • Publication number: 20120130069
    Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.
    Type: Application
    Filed: December 4, 2009
    Publication date: May 24, 2012
    Inventors: Tae Bo Sim, Jung Beom Son, Hwan Kim, Dong Sik Park, Hwan Geun Choi, Young Jin Ham, Jung Mi Hah, Kyung Ho Yoo, Chang Hyun Oh, So Ha Lee, Jae Du Ha, Sung Yun Cho, Byoung Mog Kwon, Dong Cho Han